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NOVEL FUNCTIONALIZED LACTAMS AS MODULATORS OF THE 5-HYDROXYTRYPTAMINE RECEPTOR 7 AND THEIR METHOD OF USE

20220306629 · 2022-09-29

    Inventors

    Cpc classification

    International classification

    Abstract

    Pharmaceutical compositions of the invention comprise functionalized lactam derivatives of formula (I) having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity. A is selected from a group consisting of (group) and (group)

    ##STR00001##

    Claims

    1. A compound having formula (I): ##STR00620## including enantiomers, diastereomers, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, wherein: A is selected from a group consisting of ##STR00621## R.sup.1 is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl; R.sup.2 is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl; or R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having from 5 to 7 ring atoms, optionally containing a double bond; or R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having from 6 to 8 ring atoms containing a moiety selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; R.sup.3 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, optionally substituted 4-pyridyl, and ##STR00622## R.sup.4 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, optionally substituted 4-pyridyl and ##STR00623## R.sup.5 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, optionally substituted 4-pyridyl and ##STR00624## R.sup.6 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, and optionally substituted 4-pyridyl; R.sup.7 is selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, optionally substituted phenyl, optionally substituted benzyl, COR.sup.8, CO.sub.2R.sup.9, CONR.sup.10aR.sup.10b, SO.sub.2NR.sup.10aR.sup.10b, and SO.sub.2R.sup.10c; R.sup.8 is selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.9 is selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.10a is selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.10b is selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.10c is selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, —(CH.sub.2).sub.qCN, —(CH.sub.2).sub.qSO.sub.2R.sup.11, —(CH.sub.2).sub.qOR.sup.12, ##STR00625## R.sup.11 is selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.12 is selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, and R.sup.1e are at each occurrence independently selected from the group consisting of H, OH, NO.sub.2, halogen, CN, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, —S(C.sub.1-6 linear alkyl), S(C.sub.3-7 branched alkyl), —S(C.sub.3-7 cycloalkyl), COR.sup.13, CO.sub.2R.sup.14, CONR.sup.15aR.sup.15b, SO.sub.2NR.sup.15aR.sup.15b, RN.sup.16aR.sup.16b, NR.sup.16aCOR.sup.17, NR.sup.16aSO.sub.2R.sup.18, and NR.sup.16aSO.sub.2NR.sup.19aR.sup.19b; R.sup.13 is at each occurrence independently selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.14 is at each occurrence independently selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.15a is at each occurrence independently selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.15b is at each occurrence independently selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.16a is at each occurrence independently selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.16b is at each occurrence independently selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.17 is at each occurrence independently selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.18 is at each occurrence independently selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.19a is at each occurrence independently selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.19b is at each occurrence independently selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; n is 1, 2, 3, or 4; m is 1, 2, or 3.

    2. The compound of claim 1, wherein: A is ##STR00626## each R.sup.1 and R.sup.2 is independently C.sub.1-6 linear alkyl or C.sub.3-7 branched alkyl; or R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring, wherein said 5- to 8-membered ring is saturated or comprises a carbon-carbon double bond, and/or a ring atom that is O, S, SO, SO.sub.2, or NR.sup.7 each R.sup.3, R.sup.4, and R.sup.5 is independently optionally substituted phenyl, optionally optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, or optionally substituted 4-pyridyl; R.sup.6 is independently optionally substituted phenyl, optionally optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, or optionally substituted 4-pyridyl; R.sup.7 is independently H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, COR.sup.8, or SO.sub.2R.sup.10c; R.sup.8 is selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.10c is C.sub.1-6 linear alkyl or C.sub.3-7 branched alkyl; n is 1, 2, 3, or 4; and m is 1, 2, or 3.

    3. The compound of claim 1 or 2, wherein n is 1, 2 ,or 3.

    4. The compound of any one of claims 1-3, having the formula (II): ##STR00627## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.

    5. The compound of claim 4, having the formula (XXXXII): ##STR00628## or a pharmaceutically acceptable salt thereof.

    6. The compound of claim 4, having the formula (XXXXIII): ##STR00629## or a pharmaceutically acceptable salt thereof.

    7. The compound of claim 1, having the formula (IIa): ##STR00630## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00631## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are hydrogen.

    8. The compound of claim 1, having the formula (IIe): ##STR00632## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00633## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    9. The compound of claim 1, having the formula (III): ##STR00634## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7 cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00635## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are hydrogen.

    10. The compound of claim 1, having the formula (IIm): ##STR00636## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20cd, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7 cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00637## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    11. The compound of claim 1, having the formula (IIq): ##STR00638## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00639## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    12. The compound of claim 1, having the formula (Hu): ##STR00640## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00641## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 5 of R.sup.20, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    13. The compound of claim 1, having the formula (III): ##STR00642## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.

    14. The compound of claim 1, having the formula (IIIa): ##STR00643## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00644## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are hydrogen.

    15. The compound of claim 1, having the formula (IIIe): ##STR00645## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00646## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    16. The compound of claim 1, having the formula (IIIi): ##STR00647## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00648## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are hydrogen.

    17. The compound of claim 1, having the formula (IIIm): ##STR00649## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00650## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of Rma, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    18. The compound of claim 1, having the formula (IIIg): ##STR00651## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00652## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    19. The compound of claim 1, having the formula (IIIu): ##STR00653## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00654## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    20. The compound of claim 1, having the formula (IV): ##STR00655## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.

    21. The compound of claim 20, having the following formula, ##STR00656## or a pharmaceutically acceptable salt thereof.

    22. The compound of claim 20, having the following formula, ##STR00657## or a pharmaceutically acceptable salt thereof.

    23. The compound of claim 1, having the formula (IVa): ##STR00658## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7 cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.20aR.sup.20bNHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00659## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are hydrogen.

    24. The compound of claim 1, having the formula (IVe): ##STR00660## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00661## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    25. The compound of claim 1, having the formula (IVi): ##STR00662## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00663## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of R.sup.20a, R.sup.2b, R.sup.20c, and R.sup.20e are hydrogen.

    26. The compound of claim 1, having the formula (IVm): ##STR00664## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00665## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    27. The compound of claim 1, having the formula (IVq): ##STR00666## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00667## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    28. The compound of claim 1, having the formula (IVu): ##STR00668## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00669## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    29. The compound of claim 1, having the formula (V): ##STR00670## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.

    30. The compound of claim 1, having the formula (Va): ##STR00671## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00672## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are hydrogen.

    31. The compound of claim 1, having the formula (Vb): ##STR00673## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein Q.sup.1 is 1 or 2; and Q.sup.2 is 1 or 2.

    32. The compound of claim 1, having the formula (Ve): ##STR00674## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7 cycloalkyl SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, NR.sub.23aR.sub.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00675## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    33. The compound of claim 1, having the formula (Vi): ##STR00676## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00677## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are hydrogen.

    34. The compound of claim 1, having the formula (Vm): ##STR00678## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00679## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    35. The compound of claim 1, having the formula (Vq): ##STR00680## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00681## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    36. The compound of claim 1, having the formula (Vu): ##STR00682## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00683## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    37. The compound of claim 1, having the formula (VI): ##STR00684## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.

    38. The compound of claim 37, having the formula (XXXXVI): ##STR00685## or a pharmaceutically acceptable salt thereof.

    39. The compound of claim 37, having the formula: ##STR00686## or a pharmaceutically acceptable salt thereof.

    40. The compound of claim 1, having the formula (VIa): ##STR00687## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00688## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are hydrogen.

    41. The compound of claim 1, having the formula (VIe): ##STR00689## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00690## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of Rma, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    42. The compound of claim 1, having the formula (VIi): ##STR00691## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00692## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are hydrogen.

    43. The compound of claim 1, having the formula (VIm): ##STR00693## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein R.sup.20a, R.sup.20b, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7 cycloalkyl SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21 NHSO.sub.2R.sup.22, NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00694## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    44. The compound of claim 1, having the formula (VIq): ##STR00695## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00696## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    45. The compound of claim 1, having the formula (VIu): ##STR00697## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00698## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    46. The compound of claim 1, having the formula (VII): ##STR00699## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.

    47. The compound of claim 1, having the formula (VIIa): ##STR00700## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7 cycloalkyl SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21 NHSO.sub.2R.sup.22, NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00701## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are hydrogen.

    48. The compound of claim 1, having the formula (VIIe): ##STR00702## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00703## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    49. The compound of claim 1, having the formula (VIII): ##STR00704## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00705## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are hydrogen.

    50. The compound of claim 1, having the formula (VIIm): ##STR00706## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00707## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    51. The compound of claim 1, having the formula (VIIq): ##STR00708## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7 cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00709## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    52. The compound of claim 1, having the formula (VIIu): ##STR00710## Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and ##STR00711## R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    53. The compound of any one of claims 1-52, wherein R.sup.1 and R.sup.2 are each independently C.sub.1-6 linear alkyl or C.sub.3-7 branched alkyl.

    54. The compound of claim 53, wherein each of R.sup.1 and R.sup.2 is ethyl.

    55. The compound of any one of claims 1-52, wherein R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring, optionally containing one carbon-carbon double bonds and/or a ring atom selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7.

    56. The compound of claim 55, wherein R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a C.sub.3-C.sub.8 cycloalkyl or a C.sub.5-C.sub.8 cycloalkenyl.

    57. The compound of claim 56 wherein R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, or cyclooctenyl.

    58. The compound of any one of claims 55-57, having the formula (XLIIIa): ##STR00712## or a pharmaceutically acceptable salt thereof, wherein custom-character represents a single or double bond.

    59. The compound of claim 58, wherein custom-character represents a single bond.

    60. The compound of claim 58, wherein custom-character represents a double bond.

    61. The compound of claim 55, wherein R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring containing a ring atom that is NR.sup.7.

    62. The compound of claim 61, wherein R.sup.1 and R.sup.2 are taken together to form a pyrrolidinyl or piperidinyl group where the nitrogen atom is NR.sup.7.

    63. The compound of claim 61 or 62, wherein R.sup.7 is COR.sup.8, and R.sup.8 is C.sub.1-6 linear alkyl.

    64. The compound of claim 63, wherein R.sup.7 is acetyl.

    65. The compound of claim 61 or 62, wherein R.sup.7 is SO.sub.2R.sup.10c, and R.sup.10c is C.sub.1-6 linear alkyl.

    66. The compound of claim 65, wherein R.sup.10c is methyl.

    67. The compound of any one of claims 61-66, having the formula (XLIIIb): ##STR00713## or a pharmaceutically acceptable salt thereof.

    68. The compound of claim 67, having the formula (XLIV): ##STR00714## or a pharmaceutically acceptable salt thereof.

    69. The compound of claim 67, having the formula (XLV): ##STR00715## or a pharmaceutically acceptable salt thereof.

    70. The compound of any one of claims 53-69, wherein R.sup.3 is unsubstituted phenyl.

    71. The compound of any one of claims 53-69, wherein R.sup.3 is substituted phenyl, wherein the substitutents are selected from the group consisting of hydroxyl, halo, cyano, C.sub.1-6 alkoxy, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.1-6 haloalkyl, and heterocylyl.

    72. The compound of claim 71, wherein R.sup.3 is selected from the group consisting of 4-hydroxyphenyl, 3-fluorophenyl, 4-fluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-fluoro-3-chlorophenyl, 4-cyanophenyl, 2-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-isopropylphenyl, 4-trifluoromethylphenyl, 2-morpholinophenyl, and 4-methyl-2-morpholinophenyl.

    73. The compound of any one of claims 53-69, wherein R.sup.3 is 2-pyridyl.

    74. The compound of any one of claims 53-56 and 61-62, wherein A is ##STR00716## and R.sup.5 is optionally substituted phenyl.

    75. The compound of claim 74, having the formula (XLVI), ##STR00717## or a pharmaceutically acceptable salt thereof.

    76. The compound of claim 74, having the formula (XLVIa), ##STR00718## or a pharmaceutically acceptable salt thereof.

    77. The compound of claim 74, wherein R.sup.5 is unsubstituted phenyl.

    78. The compound of claim 74, wherein R.sup.5 is selected from the group consisting of 4-hydroxyphenyl, 3-fluorophenyl, 4-fluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-fluoro-3-chlorophenyl, 4-cyanophenyl, 2-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-isopropylphenyl, 4-trifluoromethylphenyl, 2-morpholinophenyl, and 4-methyl-2-morpholinophenyl.

    79. The compound of any one of claims 1-78, or a pharmaceutically acceptable salt thereof.

    80. The compound of claim 79, wherein the compound is a compound described in any one of Tables 1-39, or a pharmaceutically acceptable salt thereof.

    81. The compound of claim 80, wherein the compound is a compound described in any one of Tables 34-39, or a pharmaceutically acceptable salt thereof.

    82. A composition comprising an effective amount of at least one compound according to any one of claims 1-81, or a pharmaceutically acceptable salt thereof.

    83. A composition according to claim 82, further comprising at least one excipient.

    84. A method of treating a disease associated with dysregulation of 5-hydroxytryptamine receptor 7 activity, said method comprising administering to a subject an effective amount of at least one compound according to any one of claims 1-81, or a pharmaceutically acceptable salt thereof.

    85. The method of claim 84, wherein the at least one compound, or a pharmaceutically acceptable salt thereof, is administered in a composition further comprising at least one excipient.

    86. The method of claim 84 or 85, wherein the disease associated with dysregulation of 5-hydroxytryptamine receptor 7 activity is selected from the group consisting of circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder, attention deficit/hyperactivity disorder, anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), intestinal inflammation, epilepsy, seizure disorders, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestine neuroendocrine tumors, and lung injury.

    87. The method of claim 84 or 85, wherein the disease associated with dysregulation of 5-hydroxytryptamine receptor 7 activity is inflammatory bowel disease (IBD) or intestinal inflammation.

    Description

    DETAILED DESCRIPTION OF THE INVENTION

    [0050] There is evidence that suggests a role for the 5-HT.sub.7 receptor in a number of medical disorders. 5-HT.sub.7 receptor activity modulators are likely to have a beneficial effect on patients suffering from these disorders. The disorders in which 5-HT.sub.7 dysregulation plays a role and modulation of 5-HT.sub.7 receptor activity by a therapeutic agent may be a viable approach to therapeutic relief include, but are not limited to, circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine (Vanhoenacker, P. et al. Trends in Pharmacological Sciences, 2000, 21, 2, 70-77), neuropathic pain, peripheral pain, allodynia (EP1875899), thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder (WO20100197700) attention deficit/hyperactivity disorder (ADHD) (WO20100069390), anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, bipolar disorder (WO20040229874), inflammatory bowel disease (IBD), intestinal inflammation (WO 2012058769, Khan, W. I., et. al. Journal of Immunology, 2013, 190, 4795-4804), epilepsy, seizure disorders (Epilepsy Research (2007) 75, 39), drug addiction, alcohol addiction (Hauser, S. R. et. al. Frontiers in Neuroscience, 2015, 8, 1-9), breast cancer (Gautam, J. Molecular Cancer, 2016, 15, 75, 1-14, Gautam, J. Breast Cancer Research and Treatment, 2017, 161, 29-40), liver fibrosis, chronic liver injury (Halici, Z. International Immunopharmacology, 2017, 43, 227-235), hepatocellular carcinoma (Bian, Z. X. Molecular Oncology, 2016, 10, 195-212), small intestine neuroendocrine tumors (Modlin, I. M. Cancer Science, 2013, 104, 7, 844-855), and lung injury (Halici, Z. Immunology, 2013, 1271-1283.).

    [0051] There is a long felt need for new 5-HT.sub.7 modulators that will provide therapeutic relief from patients suffering from diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity. The invention addresses the need to identify novel 5-HT7 modulators capable of treating disease associated with dysregulation of 5-hydroxytryptamine receptor 7 activity. The present invention addresses the need to develop new therapeutic agents for the treatment and prevention of circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder, attention deficit/hyperactivity disorder, anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), intestinal inflammation epilepsy, seizure disorders, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestine neuroendocrine tumors, and lung injury.

    [0052] The 5-hydroxytryptamine receptor 7 activity modulators of the present invention are capable of treating and preventing diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity, for example circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder, attention deficit/hyperactivity disorder, anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), intestinal inflammation, epilepsy, seizure disorders, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestine neuroendocrine tumors, and lung injury. It has been discovered that the 5-hydroxytryptamine receptor 7 play a role in a number of medical disorders, and therefore, 5-HT.sub.7 receptor activity modulators are likely to have a beneficial effect on patients suffering from these disorders. The disorders in which 5-HT.sub.7 dysregulation plays a role and modulation of 5-HT.sub.7 receptor activity by a therapeutic agent may be a viable approach to therapeutic relief include, but are not limited to, circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine (Vanhoenacker, P.et. al. Trends in Pharmacological Sciences, 2000, 21, 2, 70-77), neuropathic pain, peripheral pain, allodynia (EP1875899), thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder (WO20100197700) attention deficit/hyperactivity disorder (ADHD) (WO20100069390), anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, bipolar disorder (WO20040229874), inflammatory bowel disease (IBD), intestinal inflammation (WO 2012058769) epilepsy, seizure disorders (Epilepsy Research (2007) 75, 39), drug addiction, alcohol addiction (Hauser, S. R. et. al. Frontiers in Neuroscience, 2015, 8, 1-9), breast cancer (Gautam, J. Molecular Cancer, 2016, 15, 75, 1-14, Gautam, J. Breast Cancer Research and Treatment, 2017, 161, 29-40), liver fibrosis, chronic liver injury (Halici, Z. International Immunopharmacology, 2017, 43, 227-235), hepatocellular carcinoma (Bian, Z. X. Molecular Oncology, 2016, 10, 195-212), small intestine neuroendocrine tumors (Modlin, I. M. ancer Science, 2013, 104, 7, 844-855), and lung injury (Halici, Z. Immunology, 2013, 1271-1283.).

    [0053] Without wishing to be limited by theory, it is believed that 5-hydroxytryptamine receptor 7 receptor activity modulators of the present invention can ameliorate, abate, otherwise cause to be controlled, diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity. The diseases include, but are not limited to circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder, attention deficit/hyperactivity disorder, anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), intestinal inflammation, epilepsy, seizure disorders, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestine neuroendocrine tumors, and lung injury.

    [0054] In embodiments, a disease is depression, schizophrenia, anxiety, or bipolar disorder. In embodiments, a disease is depression. In embodiments, a disease is schizophrenia. In embodiments, a disease is anxiety. In embodiments, a disease is bipolar disorder.

    [0055] In embodiments, a disease is attention deficit/hyperactivity disorder.

    [0056] In embodiments, a disease is avoidant personality disorder.

    [0057] In embodiments, a disease is seasonal affective disorder.

    [0058] In embodiments, a disease is circadian rhythm disorder or hippocampal signaling disorder. In embodiments, a disease is circadian rhythm disorder. In embodiments, a disease is hippocampal signaling disorder.

    [0059] In embodiments, a disease is neurogenic inflammation.

    [0060] In embodiments, a disease is neuropathic pain, peripheral pain, or allodynia. In embodiments, a disease is neuropathic pain. In embodiments, a disease is peripheral pain. In embodiments, a disease is allodynia.

    [0061] In embodiments, a disease is migraine.

    [0062] In embodiments, a disease is epilepsy or a seizure disorder. In embodiments, a disease is epilepsy. In embodiments, a disease is a seizure disorder.

    [0063] In embodiments, a disease is a learning disorder or a memory disorder. In embodiments, a disease is a learning disorder. In embodiments, a disease is a memory disorder.

    [0064] In embodiments, a disease is an eating disorder.

    [0065] In embodiments, a disease is drug addiction or alcohol addiction.

    [0066] In embodiments, a disease is a sleep disorder.

    [0067] In embodiments, a disease is hypertension or peripheral vascular disease. In embodiments, a disease is hypertension. In embodiments, a disease is peripheral vascular disease.

    [0068] In embodiments, a disease is thermoregulation disorder.

    [0069] In embodiments, a disease is premature ejaculation.

    [0070] In embodiments, a disease is premenstrual syndrome or premenstrual dysphonic disorder. In embodiments, a disease is premenstrual syndrome. In embodiments, a disease is premenstrual dysphonic disorder.

    [0071] In embodiments, a disease is inflammatory bowel disease (IBD) or intestinal inflammation. In embodiments, a disease is inflammatory bowel disease (IBD). In embodiments, a disease is intestinal inflammation.

    [0072] In embodiments, a disease is breast cancer.

    [0073] In embodiments, a disease is liver fibrosis, chronic liver injury, or hepatocellular carcinoma. In embodiments, a disease is liver fibrosis. In embodiments, a disease is chronic liver injury. In embodiments, a disease is hepatocellular carcinoma.

    [0074] In embodiments, a disease is a small intestine neuroendocrine tumor.

    [0075] In embodiments, a disease is lung injury.

    [0076] In embodiments, a disease is inflammatory bowel disease (IBD).

    [0077] In embodiments, a compound described herein is a selective modulator of the serotonin 5HT7 receptor. In embodiments, a compound described herein can more potently bind a serotonin 5HT7 receptor as compared to other targets (e.g., other serotonin receptors). In embodiments, a compound may selectively bind a serotonin 5HT7 receptor in a particular tissue or organ.

    [0078] In embodiments, compounds described herein may have particularly favorable properties for effective therapy (e.g., of any of the diseases or conditions described herein). For example, in the treatment of CNS or mental disorders, a compound described herein may exhibit favorably effective blood-brain barrier permeability. Alternatively, in the treatment of non-CNS or -mental disorders, a compound described herein will not have high blood-brain barrier permeability (e.g., off-target effects will be reduced). Without being bound by theory, molecular elements of a compound may be an effective strategy for obtaining the desired biological targeting.

    [0079] For example, a compound described herein may selectively bind serotonin 5HT7 receptors in the intestine of a subject. Accordingly, a compound may be used to treat or prevent inflammatory bowel disease (IBD) or intestinal inflammation.

    [0080] Throughout the description, where compositions are described as having, including, or comprising specific components, or where processes are described as having, including, or comprising specific process steps, it is contemplated that compositions of the present teachings also consist essentially of, or consist of, the recited components, and that the processes of the present teachings also consist essentially of, or consist of, the recited processing steps.

    [0081] In the application, where an element or component is said to be included in and/or selected from a list of recited elements or components, it should be understood that the element or component can be any one of the recited elements or components and can be selected from a group consisting of two or more of the recited elements or components.

    [0082] The use of the singular herein includes the plural (and vice versa) unless specifically stated otherwise. In addition, where the use of the term “about” is before a quantitative value, the present teachings also include the specific quantitative value itself, unless specifically stated otherwise.

    [0083] It should be understood that the order of steps or order for performing certain actions is immaterial so long as the present teachings remain operable. Moreover, two or more steps or actions can be conducted simultaneously.

    [0084] As used herein, the term “halogen” shall mean chlorine, bromine, fluorine and iodine.

    [0085] As used herein, unless otherwise noted, “alkyl” and/or “aliphatic” whether used alone or as part of a substituent group refers to straight and branched carbon chains having 1 to 20 carbon atoms or any number within this range, for example 1 to 6 carbon atoms or 1 to 4 carbon atoms. Designated numbers of carbon atoms (e.g. C.sub.1-6) shall refer independently to the number of carbon atoms in an alkyl moiety or to the alkyl portion of a larger alkyl-containing substituent. Non-limiting examples of alkyl groups include methyl, ethyl, n-propyl, iso-propyl, n-butyl, sec-butyl, iso-butyl, tent-butyl, and the like. Alkyl groups can be optionally substituted. Non-limiting examples of substituted alkyl groups include hydroxymethyl, chloromethyl, trifluoromethyl, aminomethyl, 1-chloroethyl, 2-hydroxyethyl, 1,2-difluoroethyl, 3-carboxypropyl, and the like. In substituent groups with multiple alkyl groups such as (C.sub.1-6alkyl)2amino, the alkyl groups may be the same or different.

    [0086] As used herein, the terms “alkenyl” and “alkynyl” groups, whether used alone or as part of a substituent group, refer to straight and branched carbon chains having 2 or more carbon atoms, preferably 2 to 20, wherein an alkenyl chain has at least one double bond in the chain and an alkynyl chain has at least one triple bond in the chain. Alkenyl and alkynyl groups can be optionally substituted. Nonlimiting examples of alkenyl groups include ethenyl, 3-propenyl, 1-propenyl (also 2-methylethenyl), isopropenyl (also 2-methylethen-2-yl), buten-4-yl, and the like. Nonlimiting examples of substituted alkenyl groups include 2-chloroethenyl (also 2-chlorovinyl), 4-hydroxybuten-1-yl, 7-hydroxy-7-methyloct-4-en-2-yl, 7-hydroxy-7-methyloct-3,5-dien-2-yl, and the like. Nonlimiting examples of alkynyl groups include ethynyl, prop-2-ynyl (also propargyl), propyn-1-yl, and 2-methyl-hex-4-yn-1-yl. Nonlimiting examples of substituted alkynyl groups include, 5-hydroxy-5-methylhex-3-ynyl, 6-hydroxy-6-methylhept-3-yn-2-yl, 5-hydroxy-5-ethylhept-3-ynyl, and the like.

    [0087] As used herein, “cycloalkyl,” whether used alone or as part of another group, refers to a non-aromatic carbon-containing ring including cyclized alkyl, alkenyl, and alkynyl groups, e.g., having from 3 to 14 ring carbon atoms, preferably from 3 to 7 or 3 to 6 ring carbon atoms, or even 3 to 4 ring carbon atoms, and optionally containing one or more (e.g., 1, 2, or 3) double or triple bond. Cycloalkyl groups can be monocyclic (e.g., cyclohexyl) or polycyclic (e.g., containing fused, bridged, and/or spiro ring systems), wherein the carbon atoms are located inside or outside of the ring system. Any suitable ring position of the cycloalkyl group can be covalently linked to the defined chemical structure. Cycloalkyl rings can be optionally substituted. Nonlimiting examples of cycloalkyl groups include: cyclopropyl, 2-methyl-cyclopropyl, cyclopropenyl, cyclobutyl, 2,3-dihydroxycyclobutyl, cyclobutenyl, cyclopentyl, cyclopentenyl, cyclopentadienyl, cyclohexyl, cyclohexenyl, cycloheptyl, cyclooctanyl, decalinyl, 2,5-dimethylcyclopentyl, 3,5-dichlorocyclohexyl, 4-hydroxycyclohexyl, 3,3,5-trimethylcyclohex-1-yl, octahydropentalenyl, octahydro-1H-indenyl, 3a,4,5,6,7,7a-hexahydro-3H-inden-4-yl, decahydroazulenyl; bicyclo[6.2.0]decanyl, decahydronaphthalenyl, and dodecahydro-1H-fluorenyl. The term “cycloalkyl” also includes carbocyclic rings which are bicyclic hydrocarbon rings, non-limiting examples of which include, bicyclo-[2.1.1]hexanyl, bicyclo[2.2.1]heptanyl, bicyclo[3.1.1]heptanyl, 1,3-dimethyl[2.2.1]heptan-2-yl, bicyclo[2.2.2]octanyl, and bicyclo[3.3.3]undecanyl

    [0088] “Haloalkyl” is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms, substituted with 1 or more halogen. Haloalkyl groups include perhaloalkyl groups, wherein all hydrogens of an alkyl group have been replaced with halogens (e.g., —CF.sub.3, —CF.sub.2CF.sub.3). Haloalkyl groups can optionally be substituted with one or more substituents in addition to halogen. Examples of haloalkyl groups include, but are not limited to, fluoromethyl, dichloroethyl, trifluoromethyl, trichloromethyl, pentafluoroethyl, and pentachloroethyl groups.

    [0089] The term “alkoxy” refers to the group —O-alkyl, wherein the alkyl group is as defined above. Alkoxy groups optionally may be substituted. The term C.sub.3-C.sub.6 cyclic alkoxy refers to a ring containing 3 to 6 carbon atoms and at least one oxygen atom (e.g., tetrahydrofuran, tetrahydro-2H-pyran). C.sub.3-C.sub.6 cyclic alkoxy groups optionally may be substituted.

    [0090] The term “haloalkoxy” refers to the group —O-haloalkyl, wherein the haloalkyl group is as defined above. Examples of haloalkoxy groups include, but are not limited to, fluoromethoxy, difluoromethoxy, trifluoromethoxy, and pentafluoroethoxyl.

    [0091] The term “aryl,” wherein used alone or as part of another group, is defined herein as an unsaturated, aromatic monocyclic ring of 6 carbon members or to an unsaturated, aromatic polycyclic ring of from 10 to 14 carbon members. Aryl rings can be, for example, phenyl or naphthyl ring each optionally substituted with one or more moieties capable of replacing one or more hydrogen atoms. Non-limiting examples of aryl groups include: phenyl, naphthylen-1-yl, naphthylen-2-yl, 4-fluorophenyl, 2-hydroxyphenyl, 3-methylphenyl, 2-amino-4-fluorophenyl, 2-(N,N-diethylamino)phenyl, 2-cyanophenyl, 2,6-di-tert-butylphenyl, 3-methoxyphenyl, 8-hydroxynaphthylen-2-yl 4,5-dimethoxynaphthylen-1-yl, and 6-cyano-naphthylen-1-yl. Aryl groups also include, for example, phenyl or naphthyl rings fused with one or more saturated or partially saturated carbon rings (e.g., bicyclo[4.2.0]octa-1,3,5-trienyl, indanyl), which can be substituted at one or more carbon atoms of the aromatic and/or saturated or partially saturated rings.

    [0092] The term “arylalkyl” or “aralkyl” refers to the group -alkyl-aryl, where the alkyl and aryl groups are as defined herein. Aralkyl groups of the present invention are optionally substituted. Examples of arylalkyl groups include, for example, benzyl, 1-phenylethyl, 2-phenylethyl, 3-phenylpropyl, 2-phenylpropyl, fluorenylmethyl and the like.

    [0093] The terms “heterocyclic” and/or “heterocycle” and/or “heterocylyl,” whether used alone or as part of another group, are defined herein as one or more ring having from 3 to 20 atoms wherein at least one atom in at least one ring is a heteroatom selected from nitrogen (N), oxygen (O), or sulfur (S), and wherein further the ring that includes the heteroatom is non-aromatic. In heterocycle groups that include 2 or more fused rings, the non-heteroatom bearing ring may be aryl (e.g., indolinyl, tetrahydroquinolinyl, chromanyl). Exemplary heterocycle groups have from 3 to 14 ring atoms of which from 1 to 5 are heteroatoms independently selected from nitrogen (N), oxygen (O), or sulfur (S). One or more N or S atoms in a heterocycle group can be oxidized. Heterocycle groups can be optionally substituted.

    [0094] Non-limiting examples of heterocyclic units having a single ring include: diazirinyl, aziridinyl, urazolyl, azetidinyl, pyrazolidinyl, imidazolidinyl, oxazolidinyl, isoxazolinyl, isoxazolyl, thiazolidinyl, isothiazolyl, isothiazolinyl oxathiazolidinonyl, oxazolidinonyl, hydantoinyl, tetrahydrofuranyl, pyrrolidinyl, morpholinyl, piperazinyl, piperidinyl, dihydropyranyl, tetrahydropyranyl, piperidin-2-onyl (valerolactam), 2,3,4,5-tetrahydro-1H-azepinyl, 2,3-dihydro-1H-indole, and 1,2,3,4-tetrahydro-quinoline. Non-limiting examples of heterocyclic units having 2 or more rings include: hexahydro-1H-pyrrolizinyl, 3a,4,5,6,7,7a-hexahydro-1H-benzo[d]imidazolyl, 3a,4,5,6,7,7a-hexahydro-1H-indolyl, 1,2,3,4-tetrahydroquinolinyl, chromanyl, isochromanyl, indolinyl, isoindolinyl, and decahydro-1H-cycloocta[b]pyrrolyl.

    [0095] The term “heteroaryl,” whether used alone or as part of another group, is defined herein as one or more rings having from 5 to 20 atoms wherein at least one atom in at least one ring is a heteroatom chosen from nitrogen (N), oxygen (O), or sulfur (S), and wherein further at least one of the rings that includes a heteroatom is aromatic. In heteroaryl groups that include 2 or more fused rings, the non-heteroatom bearing ring may be a carbocycle (e.g., 6,7-Dihydro-5H-cyclopentapyrimidine) or aryl (e.g., benzofuranyl, benzothiophenyl, indolyl). Exemplary heteroaryl groups have from 5 to 14 ring atoms and contain from 1 to 5 ring heteroatoms independently selected from nitrogen (N), oxygen (O), or sulfur (S). One or more N or S atoms in a heteroaryl group can be oxidized. Heteroaryl groups can be substituted. Non-limiting examples of heteroaryl rings containing a single ring include: 1,2,3,4-tetrazolyl, [1,2,3]triazolyl, [1,2,4]triazolyl, triazinyl, thiazolyl, 1H-imidazolyl, oxazolyl, furanyl, thiopheneyl, pyrimidinyl, 2-phenylpyrimidinyl, pyridinyl, 3-methylpyridinyl, and 4-dimethylaminopyridinyl. Non-limiting examples of heteroaryl rings containing 2 or more fused rings include: benzofuranyl, benzothiophenyl, benzoxazolyl, benzthiazolyl, benztriazolyl, cinnolinyl, naphthyridinyl, phenanthridinyl, 7H-purinyl, 9H-purinyl, 6-amino-9H-purinyl, 5H-pyrrolo[3,2-d]pyrimidinyl, 7H-pyrrolo[2,3-d]pyrimidinyl, pyrido[2,3-d]pyrimidinyl, 2-phenylbenzo[d]thiazolyl, 1H-indolyl, 4,5,6,7-tetrahydro-1-H-indolyl, quinoxalinyl, 5-methylquinoxalinyl, quinazolinyl, quinolinyl, 8-hydroxy-quinolinyl, 1H-benzo[d]imidazol-2(3H)-onyl, 1H-benzo[d]imidazolyl, and isoquinolinyl.

    [0096] One non-limiting example of a heteroaryl group as described above is C.sub.1-C.sub.5 heteroaryl, which has 1 to 5 carbon ring atoms and at least one additional ring atom that is a heteroatom (preferably 1 to 4 additional ring atoms that are heteroatoms) independently selected from nitrogen (N), oxygen (O), or sulfur (S). Examples of C.sub.1-C.sub.5 heteroaryl include, but are not limited to, triazinyl, thiazol-2-yl, thiazol-4-yl, imidazol-1-yl, 1H-imidazol-2-yl, 1H-imidazol-4-yl, isoxazolin-5-yl, furan-2-yl, furan-3-yl, thiophen-2-yl, thiophen-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyridin-2-yl, pyridin-3-yl, and pyridin-4-yl.

    [0097] Unless otherwise noted, when two substituents are taken together to form a ring having a specified number of ring atoms (e.g., R.sup.2 and R.sup.3 taken together with the nitrogen (N) to which they are attached to form a ring having from 3 to 7 ring members), the ring can have carbon atoms and optionally one or more (e.g., 1 to 3) additional heteroatoms independently selected from nitrogen (N), oxygen (O), or sulfur (S). The ring can be saturated or partially saturated and can be optionally substituted.

    [0098] For the purposed of the present invention fused ring units, as well as spirocyclic rings, bicyclic rings and the like, which comprise a single heteroatom will be considered to belong to the cyclic family corresponding to the heteroatom containing ring. For example, 1,2,3,4-tetrahydroquinoline having the formula:

    ##STR00011##

    is, for the purposes of the present invention, considered a heterocyclic unit. 6,7-Dihydro-5H-cyclopentapyrimidine having the formula:

    ##STR00012##

    is, for the purposes of the present invention, considered a heteroaryl unit. When a fused ring unit contains heteroatoms in both a saturated and an aryl ring, the aryl ring will predominate and determine the type of category to which the ring is assigned. For example, 1,2,3,4-tetrahydro-[1,8]naphthyridine having the formula:

    ##STR00013##

    is, for the purposes of the present invention, considered a heteroaryl unit.

    [0099] Whenever a term or either of their prefix roots appear in a name of a substituent the name is to be interpreted as including those limitations provided herein. For example, whenever the term “alkyl” or “aryl” or either of their prefix roots appear in a name of a substituent (e.g., arylalkyl, alkylamino) the name is to be interpreted as including those limitations given above for “alkyl” and “aryl.”

    [0100] The term “substituted” is used throughout the specification. The term “substituted” is defined herein as a moiety, whether acyclic or cyclic, which has one or more hydrogen atoms replaced by a substituent or several (e.g., 1 to 10) substituents as defined herein below. The substituents are capable of replacing one or two hydrogen atoms of a single moiety at a time. In addition, these substituents can replace two hydrogen atoms on two adjacent carbons to form said substituent, new moiety or unit. For example, a substituted unit that requires a single hydrogen atom replacement includes halogen, hydroxyl, and the like. A two hydrogen atom replacement includes carbonyl, oximino, and the like. A two hydrogen atom replacement from adjacent carbon atoms includes epoxy, and the like. The term “substituted” is used throughout the present specification to indicate that a moiety can have one or more of the hydrogen atoms replaced by a substituent. When a moiety is described as “substituted” any number of the hydrogen atoms may be replaced. For example, difluoromethyl is a substituted C.sub.1 alkyl; trifluoromethyl is a substituted C.sub.1 alkyl; 4-hydroxyphenyl is a substituted aromatic ring; (N,N-dimethyl-5-amino)octanyl is a substituted C.sub.8 alkyl; 3-guanidinopropyl is a substituted C.sub.3 alkyl; and 2-carboxypyridinyl is a substituted heteroaryl.

    [0101] The variable groups defined herein, e.g., alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, aryloxy, aryl, heterocycle and heteroaryl groups defined herein, whether used alone or as part of another group, can be optionally substituted. Optionally substituted groups will be so indicated.

    [0102] The following are non-limiting examples of substituents which can substitute for hydrogen atoms on a moiety: halogen (chlorine (Cl), bromine (Br), fluorine (F) and iodine(I)), —CN, —NO.sub.2, oxo (═O), —OR.sup.26, —SR26, —N(R26).sub.2, —NR.sup.26C(O)R.sup.26, —SO.sub.2R.sup.26, —SO.sub.2OR.sup.26, —SO.sub.2N(R.sup.26).sup.2, —C(O)R.sup.26, —C(O)OR.sup.26, —C(O)N(R.sup.26).sub.2, C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, C.sub.1-6 alkoxy, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, C.sub.3-14 cycloalkyl, aryl, heterocycle, or heteroaryl, wherein each of the alkyl, haloalkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, heterocycle, and heteroaryl groups is optionally substituted with 1-10 (e.g., 1-6 or 1-4) groups selected independently from halogen, —CN, —NO2, oxo, and R.sup.26; wherein R.sup.26, at each occurrence, independently is hydrogen, —OR.sup.27, —SR.sup.27, —C(O)R.sup.27, —C(O)OR.sup.27, —C(O)N(R.sup.27).sub.2, —SO.sub.2R.sup.27, —S(O).sub.2OR.sup.27, —N(R.sup.27).sub.2, —NR.sup.27C(O)R.sup.27, C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, cycloalkyl (e.g., C.sub.3-6 cycloalkyl), aryl, heterocycle, or heteroaryl, or two R.sup.26 units taken together with the atom(s) to which they are bound form an optionally substituted carbocycle or heterocycle wherein said carbocycle or heterocycle has 3 to 7 ring atoms; wherein R.sup.27, at each occurrence, independently is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, cycloalkyl (e.g., C.sub.3-6 cycloalkyl), aryl, heterocycle, or heteroaryl, or two R.sup.27 units taken together with the atom(s) to which they are bound form an optionally substituted carbocycle or heterocycle wherein said carbocycle or heterocycle preferably has 3 to 7 ring atoms.

    [0103] In some embodiments, the substituents are selected from [0104] i) —OR.sup.28; for example, —OH, —OCH.sub.3, —OCH.sub.2CH.sub.3, —OCH.sub.2CH.sub.2CH.sub.3; [0105] ii) —C(O)R.sup.28; for example, —COCH.sub.3, —COCH.sub.2CH.sub.3, —COCH.sub.2CH.sub.2CH.sub.3; [0106] iii) —C(O)OR.sup.28; for example, —CO.sub.2CH.sub.3, —CO.sub.2CH.sub.2CH.sub.3, —CO.sub.2CH.sub.2CH.sub.2CH.sub.3; [0107] iv) —C(O)N(R.sup.28).sub.2; for example, —CONH.sub.2, —CONHCH.sub.3, —CON(CH.sub.3).sub.2; [0108] v) —N(R.sup.28).sub.2; for example, —NH.sub.2, —NHCH.sub.3, —N(CH.sub.3).sub.2, —NH(CH.sub.2CH.sub.3); [0109] vi) halogen: —F, —Cl, —Br, and —I; [0110] vii) —CH.sub.eX.sub.g; wherein X is halogen, m is from 0 to 2, e+g=3; for example, —CH.sub.2F, —CHF.sub.2, —CF.sub.3, —CCl.sub.3, or —CBr.sub.3; [0111] viii) —SO.sub.2R.sup.28; for example, —SO.sub.2H; —SO.sub.2CH.sub.3; —SO.sub.2C.sub.6H.sub.5; [0112] ix) C.sub.1-C.sub.6 linear, branched, or cyclic alkyl; [0113] x) Cyano [0114] xi) Nitro; [0115] xii) N(R.sup.28)C(O)R.sup.28; [0116] xiii) Oxo (═O); [0117] xiv) Heterocycle; and [0118] xv) Heteroaryl.
    wherein each R.sup.28 is independently hydrogen, optionally substituted C.sub.1-C.sub.6 linear or branched alkyl (e.g., optionally substituted C.sub.1-C.sub.4 linear or branched alkyl), or optionally substituted C.sub.3-C.sub.6 cycloalkyl (e.g optionally substituted C.sub.3-C.sub.4 cycloalkyl); or two R.sup.28 units can be taken together to form a ring comprising 3-7 ring atoms. In certain aspects, each R.sup.28 is independently hydrogen, C.sub.1-C.sub.6 linear or branched alkyl optionally substituted with halogen or C.sub.3-C.sub.6 cycloalkyl or C.sub.3-C.sub.6 cycloalkyl.

    [0119] At various places in the present specification, substituents of compounds are disclosed in groups or in ranges. It is specifically intended that the description include each and every individual subcombination of the members of such groups and ranges. For example, the term “C.sub.1-6 alkyl” is specifically intended to individually disclose C.sub.1, C.sub.2, C.sub.3, C.sub.4, C.sub.5, C.sub.6, C.sub.1-C.sub.6, C.sub.1-C.sub.5, C.sub.1-C.sub.4, C.sub.1-C.sub.3, C.sub.1-C.sub.2, C.sub.2-C.sub.6, C.sub.2-C.sub.5, C.sub.2-C.sub.4, C.sub.2-C.sub.3, C.sub.3-C.sub.6, C.sub.3-C.sub.5, C.sub.3-C.sub.4, C.sub.4-C.sub.6, C.sub.4-C.sub.5, and C.sub.5-C.sub.6, alkyl.

    [0120] For the purposes of the present invention the terms “compound,” “analog,” and “composition of matter” stand equally well for the 5-hydroxytryptamine receptor 7 activity modulators described herein, including all enantiomeric forms, diastereomeric forms, salts, and the like, and the terms “compound,” “analog,” and “composition of matter” are used interchangeably throughout the present specification.

    [0121] Compounds described herein can contain an asymmetric atom (also referred as a chiral center), and some of the compounds can contain one or more asymmetric atoms or centers, which can thus give rise to optical isomers (enantiomers) and diastereomers. The present teachings and compounds disclosed herein include such enantiomers and diastereomers, as well as the racemic and resolved, enantiomerically pure R and S stereoisomers, as well as other mixtures of the R and S stereoisomers and pharmaceutically acceptable salts thereof. Optical isomers can be obtained in pure form by standard procedures known to those skilled in the art, which include, but are not limited to, diastereomeric salt formation, kinetic resolution, and asymmetric synthesis. The present teachings also encompass cis and trans isomers of compounds containing alkenyl moieties (e.g., alkenes and imines). It is also understood that the present teachings encompass all possible regioisomers, and mixtures thereof, which can be obtained in pure form by standard separation procedures known to those skilled in the art, and include, but are not limited to, column chromatography, thin-layer chromatography, and high-performance liquid chromatography.

    [0122] Pharmaceutically acceptable salts of compounds of the present teachings, which can have an acidic moiety, can be formed using organic and inorganic bases. Both mono and polyanionic salts are contemplated, depending on the number of acidic hydrogens available for deprotonation. Suitable salts formed with bases include metal salts, such as alkali metal or alkaline earth metal salts, for example sodium, potassium, or magnesium salts; ammonia salts and organic amine salts, such as those formed with morpholine, thiomorpholine, piperidine, pyrrolidine, a mono-, di- or tri-lower alkylamine (e.g., ethyl-tert-butyl-, diethyl-, diisopropyl-, triethyl-, tributyl- or dimethylpropylamine), or a mono-, di-, or trihydroxy lower alkylamine (e.g., mono-, di- or triethanolamine). Specific non-limiting examples of inorganic bases include NaHCO.sub.3, Na.sub.2CO.sub.3, KHCO.sub.3, K.sub.2CO.sub.3, Cs.sub.2CO.sub.3, LiOH, NaOH, KOH, NaH.sub.2PO.sub.4, Na.sub.2HPO.sub.4, and Na.sub.3PO.sub.4. Internal salts also can be formed. Similarly, when a compound disclosed herein contains a basic moiety, salts can be formed using organic and inorganic acids. For example, salts can be formed from the following acids: acetic, propionic, lactic, benzenesulfonic, benzoic, camphorsulfonic, citric, tartaric, succinic, dichloroacetic, ethenesulfonic, formic, fumaric, gluconic, glutamic, hippuric, hydrobromic, hydrochloric, isethionic, lactic, maleic, malic, malonic, mandelic, methanesulfonic, mucic, napthalenesulfonic, nitric, oxalic, pamoic, pantothenic, phosphoric, phthalic, propionic, succinic, sulfuric, tartaric, toluenesulfonic, and camphorsulfonic as well as other known pharmaceutically acceptable acids.

    [0123] When any variable occurs more than one time in any constituent or in any formula, its definition in each occurrence is independent of its definition at every other occurrence (e.g., in N(R.sup.9).sub.2, each R.sup.9 may be the same or different than the other). Combinations of substituents and/or variables are permissible only if such combinations result in stable compounds.

    [0124] The terms “treat” and “treating” and “treatment” as used herein, refer to partially or completely alleviating, inhibiting, ameliorating and/or relieving a condition from which a patient is suspected to suffer.

    [0125] As used herein, “therapeutically effective” and “effective dose” refer to a substance or an amount that elicits a desirable biological activity or effect.

    [0126] Except when noted, the terms “subject” or “patient” are used interchangeably and refer to mammals such as human patients and non-human primates, as well as experimental animals such as rabbits, rats, and mice, and other animals. Accordingly, the term “subject” or “patient” as used herein means any mammalian patient or subject to which the compounds of the invention can be administered. In an exemplary embodiment of the present invention, to identify subject patients for treatment according to the methods of the invention, accepted screening methods are employed to determine risk factors associated with a targeted or suspected disease or condition or to determine the status of an existing disease or condition in a subject. These screening methods include, for example, conventional work-ups to determine risk factors that may be associated with the targeted or suspected disease or condition. These and other routine methods allow the clinician to select patients in need of therapy using the methods and compounds of the present invention.

    [0127] The 5-Hydroxytryptamine Receptor 7 Activity Modulators

    [0128] The present invention is directed toward novel 5-hydroxytryptamine receptor 7 (5-HT7) activity modulators, compounds of formula (I),

    ##STR00014##

    [0129] Including enantiomers, diastereomers, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, wherein:

    [0130] A is selected from a group consisting of

    ##STR00015##

    [0131] R.sup.1 is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl;

    [0132] R.sup.2 is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl;

    [0133] Or R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having from 5 to 7 ring atoms, optionally containing a double bond;

    [0134] Or R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having from 6 to 8 ring atoms containing a moiety selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7;

    [0135] R.sup.3 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, optionally substituted 4-pyridyl, and

    ##STR00016##

    [0136] R.sup.4 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, optionally substituted 4-pyridyl and

    ##STR00017##

    [0137] R.sup.5 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, optionally substituted 4-pyridyl and

    ##STR00018##

    [0138] R.sup.6 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, and optionally substituted 4-pyridyl;

    [0139] R.sup.7 is selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, optionally substituted phenyl, optionally substituted benzyl, COR.sup.8, CO.sub.2R.sup.9, CONR.sup.10aR.sup.10b, SO.sub.2NR.sup.10aR.sup.10b, and SO.sub.2R.sup.10c;

    [0140] R.sup.8 is selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0141] R.sup.9 is selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0142] R.sup.10a is selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0143] R.sup.10b is selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0144] R.sup.10c is selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, —(CH.sub.2).sub.qCN, —(CH.sub.2).sub.qSO.sub.2R.sup.11, —(CH.sub.2).sub.qOR.sup.12,

    ##STR00019##

    [0145] R.sup.11 is selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0146] R.sup.12 is selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0147] R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, and R.sup.1e are at each occurrence independently selected from the group consisting of H, OH, NO.sub.2, halogen, CN, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, —S(C.sub.1-6 linear alkyl), S(C.sub.3-7 branched alkyl), —S(C.sub.3-7 cycloalkyl), COR.sup.13, CO.sub.2R.sup.14, CONR.sup.15aR.sup.15b, SO.sub.2NR.sup.15aR.sup.15b, NR.sup.16aR.sup.16b, NR.sup.16aCOR.sup.17, NR.sup.16aSO.sub.2R.sup.18, and NR.sup.16aSO.sub.2NR.sup.19aR.sup.19b;

    [0148] R.sup.13 is at each occurrence independently selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0149] R.sup.14 is at each occurrence independently selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0150] R.sup.15d is at each occurrence independently selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0151] R.sup.15b is at each occurrence independently selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0152] R.sup.16a is at each occurrence independently selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0153] R.sup.16b is at each occurrence independently selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0154] R.sup.17 is at each occurrence independently selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0155] R.sup.18 is at each occurrence independently selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0156] R.sup.19a is at each occurrence independently selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0157] R.sup.19b is at each occurrence independently selected from the group consisting of C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0158] n is 1, 2, 3, or 4;

    [0159] m is 1, 2, or 3.

    [0160] In embodiments,

    [0161] A is

    ##STR00020##

    [0162] each R.sup.1 and R.sup.2 is independently C.sub.1-6 linear alkyl or C.sub.3-7 branched alkyl; or R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring, [0163] wherein said 5- to 8-membered ring is saturated or comprises a carbon-carbon double bond, and/or a ring atom that is O, S, SO, SO.sub.2, or NR.sup.7

    [0164] each R.sup.3, R.sup.4, and R.sup.5 is independently optionally substituted phenyl, optionally optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, or optionally substituted 4-pyridyl;

    [0165] R.sup.6 is independently optionally substituted phenyl, optionally optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, or optionally substituted 4-pyridyl;

    [0166] R.sup.7 is independently H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, COR.sup.8, or SO.sub.2R.sup.16c;

    [0167] R.sup.8 is selected from the group consisting of H, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0168] R.sup.16c is C.sub.1-6 linear alkyl or C.sub.3-7 branched alkyl;

    [0169] n is 1, 2, 3, or 4; and

    [0170] m is 1, 2, or 3.

    [0171] In embodiments, n is 1, 2, or 3. In embodiments, n is 1. In embodiments, n is 2. In embodiments, n is 3.

    [0172] The embodiments of the present invention include compounds having formula (II):

    ##STR00021##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.

    [0173] In embodiments, a compound has the formula (XLII):

    ##STR00022##

    or a pharmaceutically acceptable salt thereof.

    [0174] In embodiments, a compound has the formula (XLIII):

    ##STR00023##

    or a pharmaceutically acceptable salt thereof.

    [0175] In embodiments, n is 1, 2, or 3. In embodiments, n is 1. In embodiments, n is 2. In embodiments, n is 3. In embodiments, n is 1 or 2.

    [0176] In embodiments, each of R.sup.1 and R.sup.2 is unsubstituted C.sub.1-6 alkyl. In embodiments, each of R.sup.1 and R.sup.2 is ethyl. In embodiments, each of R.sup.1 and R.sup.2 is methyl.

    [0177] In embodiments, R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring, optionally containing one carbon-carbon double bonds and/or a ring atom selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7.

    [0178] In embodiments, R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a C.sub.3-C.sub.8 cycloalkyl or a C.sub.5-C.sub.8 cycloalkenyl.

    [0179] In embodiments, R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a C.sub.3-C.sub.8 cycloalkyl or C.sub.5-C.sub.8 cycloalkenyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, and cyclooctenyl. In embodiments, said C.sub.3-C.sub.8 cycloalkyl or C.sub.5-C.sub.8 cycloalkenyl is unsubstituted. In embodiments, said C.sub.3-C.sub.8 cycloalkyl or C.sub.5-C.sub.8 cycloalkenyl is substituted by 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In embodiments, said substituents are selected from oxo (═O), hydroxyl, halo, cyano, C.sub.1-6 alkoxy, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.1-6 haloalkyl, C.sub.3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, ——, —CN, —OMe, —OEt, —O.sup.nOPr, —O.sup.iPr, —OCF.sub.3, -Me, -Et, —.sup.nPr, —.sup.iPr, —CF.sub.3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

    [0180] In embodiments, a compound has a structure according to formula (XXXXIIIa):

    ##STR00024##

    or

    [0181] a pharmaceutically acceptable salt thereof, wherein custom-character represents a single or double bond.

    [0182] In embodiments, custom-character represents a single bond.

    [0183] In embodiments, custom-character represents a double bond.

    [0184] In embodiments, the lactam stereocenter substituted by nitrogen has the R-configuration.

    [0185] In embodiments, the lactam stereocenter substituted by nitrogen has the S-configuration.

    [0186] In embodiments, R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring containing a ring atom that is NR.sup.7. In embodiments, said 5- to 8-membered ring is not further substituted. In embodiments, said 5- to 8-membered ring further comprises 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In embodiments, said substituents are selected from oxo (═O), hydroxyl, halo, cyano, C.sub.1-6 alkoxy, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.1-6 haloalkyl, C.sub.3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —I, —CN, —OMe, —OEt, —O.sup.nPr, —O.sup.iPr, —OCF.sub.3, -Me, -Et, —.sup.nPr, —.sup.iPr, —CF.sub.3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

    [0187] In embodiments, R.sup.1 and R.sup.2 are taken together to form a pyrrolidinyl or piperidinyl group where the nitrogen atom is NR.sup.7. In embodiments, said pyrrolidinyl or piperidinyl group is not further substituted. In embodiments, said pyrrolidinyl or piperidinyl group further comprises 1, 2, 3, or 4 substituents as described herein.

    [0188] In embodiments, a compound has the formula (XLIIIb)

    ##STR00025##

    or a pharmaceutically acceptable salt thereof.

    [0189] In embodiments, a compound has the formula (XLIV)

    ##STR00026##

    or a pharmaceutically acceptable salt thereof.

    [0190] In embodiments, a compound has the formula (XLV)

    ##STR00027##

    or a pharmaceutically acceptable salt thereof.

    [0191] In embodiments, n is 1, 2, or 3. In embodiments, n is 1. In embodiments, n is 2. In embodiments, n is 3. In embodiments, n is 1 or 2.

    [0192] In embodiments, R.sup.7 is COR.sup.8, and R.sup.8 is C.sub.1-6 linear alkyl.

    [0193] In embodiments, R.sup.7 is acetyl.

    [0194] In embodiments, R.sup.7 is SO.sub.2R.sup.10c, and R.sup.10c is C.sub.1-6 linear alkyl.

    [0195] In embodiments, R.sup.10c is methyl (i.e., R.sup.7 is SO.sub.2Me).

    [0196] In embodiments, R.sup.3 is unsubstituted phenyl.

    [0197] In embodiments, R.sup.3 is substituted phenyl. In embodiments, R.sup.3 is phenyl substituted by 1, 2, 3, 4, or 5 substituents (e.g., phenyl substituted by 1 or 2 substituents as described herein). In embodiments, the substitutents are selected from the group consisting of hydroxyl, halo, cyano, C.sub.1-6 alkoxy, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.1-6 haloalkyl, C.sub.3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —CN, —OMe, —OEt, —O.sup.nPr, —O.sup.iPr, —OCF.sub.3, -Me, -Et, —.sup.nPr, —.sup.iPr, —CF.sub.3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

    [0198] In embodiments, R.sup.3 is selected from the group consisting of hydroxylphenyl, fluorophenyl, chlorophenyl, bromophenyl, cyanophenyl, tolyl, methoxylphenyl, difluorophenyl, dichlorophenyl, chloro-fluorophenyl, dimethylphenyl, trifluoromethylphenyl, di(trifluoromethyl)phenyl,

    [0199] In embodiments, R.sup.3 is selected from the group consisting of 4-hydroxyphenyl, 3-fluorophenyl, 4-fluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-fluoro-3-chlorophenyl, 4-cyanophenyl, 2-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-isopropylphenyl, 4-trifluoromethylphenyl, 2-morpholinophenyl, and 4-methyl-2-morpholinophenyl.

    [0200] In embodiments, R.sup.3 is 2-pyridyl. In embodiments, R.sup.3 is 3-pyridyl. In embodiments, R.sup.3 is 4-pyridyl. In embodiments, said pyridyl is unsubstituted. In embodiments, said pyridyl is substituted by 1, 2, 3, or 4 substituents (e.g., pyridyl substituted by 1 or 2 substituents as described herein). In embodiments, the substitutents are selected from the group consisting of hydroxyl, halo, cyano, C.sub.1-6 alkoxy, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.1-6 haloalkyl, C.sub.3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —CN, —OMe, —OEt, —O.sup.nPr, —O.sup.iPr, —OCF.sub.3, -Me, -Et, —.sup.nPr, —.sup.iPr, —CF.sub.3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

    [0201] The embodiments of the present invention include compounds having formula (IIa):

    ##STR00028##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0202] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00029## [0203] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0204] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0205] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0206] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0207] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0208] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl;

    [0209] and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are hydrogen.

    [0210] The embodiments of the present invention include compounds having formula (IIb):

    ##STR00030##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0211] Q.sup.1 is 1 or 2;

    [0212] and Q.sup.2 is 1 or 2.

    [0213] The embodiments of the present invention include compounds having formula (IIc):

    ##STR00031##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0214] Q.sup.1 is 1 or 2; [0215] and Q.sup.2 is 1 or 2.

    [0216] The embodiments of the present invention include compounds having formula (IId):

    ##STR00032##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0217] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0218] Q.sup.1 is 1 or 2; [0219] and Q.sup.2 is 1 or 2.

    [0220] The embodiments of the present invention include compounds having formula (IId-1):

    ##STR00033##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0221] Q.sup.1 is 1 or 2; [0222] and Q.sup.2 is 1 or 2.

    [0223] The embodiments of the present invention include compounds having formula (IId-2):

    ##STR00034##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0224] Q.sup.1 is 1 or 2; [0225] and Q.sup.2 is 1 or 2.

    [0226] The embodiments of the present invention include compounds having formula (IId-3):

    ##STR00035##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0227] Q.sup.1 is 1 or 2; [0228] and Q.sup.2 is 1 or 2.

    [0229] The embodiments of the present invention include compounds having formula (IId-4):

    ##STR00036##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0230] Q.sup.1 is 1 or 2; [0231] and Q.sup.2 is 1 or 2.

    [0232] The embodiments of the present invention include compounds having formula (IId-5):

    ##STR00037##

    [0233] Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0234] Q.sup.1 is 1 or 2; [0235] and Q.sup.2 is 1 or 2.

    [0236] The embodiments of the present invention include compounds having formula (IIe):

    ##STR00038##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0237] R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sub.22, —NR.sub.23aR.sub.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00039## [0238] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0239] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0240] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0241] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0242] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0243] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0244] and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    [0245] The embodiments of the present invention include compounds having formula (IIf):

    ##STR00040##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0246] Q.sup.1 is 1 or 2; [0247] and Q.sup.2 is 1 or 2.

    [0248] The embodiments of the present invention include compounds having formula (IIg):

    ##STR00041##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0249] Q.sup.1 is 1 or 2; [0250] and Q.sup.2 is 1 or 2.

    [0251] The embodiments of the present invention include compounds having formula (IIh):

    ##STR00042##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0252] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0253] Q.sup.1 is 1 or 2; [0254] and Q.sup.2 is 1 or 2.

    [0255] The embodiments of the present invention include compounds having formula (IIh-1):

    ##STR00043##

    [0256] Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0257] Q.sup.1 is 1 or 2; [0258] and Q.sup.2 is 1 or 2.

    [0259] The embodiments of the present invention include compounds having formula (IIh-2):

    ##STR00044##

    [0260] Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0261] Q.sup.1 is 1 or 2; [0262] and Q.sup.2 is 1 or 2.

    [0263] The embodiments of the present invention include compounds having formula (IIh-3):

    ##STR00045##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0264] Q.sup.1 is 1 or 2; [0265] and Q.sup.2 is 1 or 2.

    [0266] The embodiments of the present invention include compounds having formula (IIh-4):

    ##STR00046##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0267] Q.sup.1 is 1 or 2; [0268] and Q.sup.2 is 1 or 2.

    [0269] The embodiments of the present invention include compounds having formula (IIh-5):

    ##STR00047##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0270] Q.sup.1 is 1 or 2; [0271] and Q.sup.2 is 1 or 2.

    [0272] The embodiments of the present invention include compounds having formula (III):

    ##STR00048##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0273] R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00049## [0274] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0275] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0276] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0277] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0278] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0279] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are hydrogen.

    [0280] The embodiments of the present invention include compounds having formula (IIj):

    ##STR00050##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0281] Q.sup.1 is 1 or 2; [0282] and Q.sup.2 is 1 or 2.

    [0283] The embodiments of the present invention include compounds having formula (IIk):

    ##STR00051##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0284] Q.sup.1 is 1 or 2; [0285] and Q.sup.2 is 1 or 2.

    [0286] The embodiments of the present invention include compounds having formula (IIL):

    ##STR00052##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0287] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0288] Q.sup.1 is 1 or 2; [0289] and Q.sup.2 is 1 or 2.

    [0290] The embodiments of the present invention include compounds having formula (IIL-1):

    ##STR00053##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0291] Q.sup.1 is 1 or 2; [0292] and Q.sup.2 is 1 or 2.
    The embodiments of the present invention include compounds having formula (IIL-2):

    ##STR00054##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0293] Q.sup.1 is 1 or 2; [0294] and Q.sup.2 is 1 or 2.

    [0295] The embodiments of the present invention include compounds having formula (IIL-3):

    ##STR00055##

    [0296] Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0297] Q.sup.1 is 1 or 2; [0298] and Q.sup.2 is 1 or 2.

    [0299] The embodiments of the present invention include compounds having formula (IIL-4):

    ##STR00056##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0300] Q.sup.1 is 1 or 2; [0301] and Q.sup.2 is 1 or 2.

    [0302] The embodiments of the present invention include compounds having formula (IIL-5):

    ##STR00057##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0303] Q.sup.1 is 1 or 2; [0304] and Q.sup.2 is 1 or 2.

    [0305] The embodiments of the present invention include compounds having formula (IIm):

    ##STR00058##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0306] R.sup.20a, R.sup.20b, R.sup.20cd, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00059## [0307] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0308] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0309] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0310] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0311] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0312] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    [0313] The embodiments of the present invention include compounds having formula (IIn):

    ##STR00060##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0314] Q.sup.1 is 1 or 2; [0315] and Q.sup.2 is 1 or 2.

    [0316] The embodiments of the present invention include compounds having formula (IIo):

    ##STR00061##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0317] Q.sup.1 is 1 or 2; [0318] and Q.sup.2 is 1 or 2.

    [0319] The embodiments of the present invention include compounds having formula (IIp):

    ##STR00062##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0320] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0321] Q.sup.1 is 1 or 2; [0322] and Q.sup.2 is 1 or 2.

    [0323] The embodiments of the present invention include compounds having formula (IIp-1):

    ##STR00063##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0324] Q.sup.1 is 1 or 2; [0325] and Q.sup.2 is 1 or 2.

    [0326] The embodiments of the present invention include compounds having formula (IIp-2):

    ##STR00064##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0327] Q.sup.1 is 1 or 2; [0328] and Q.sup.2 is 1 or 2.

    [0329] The embodiments of the present invention include compounds having formula (IIp-3):

    ##STR00065##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0330] Q.sup.1 is 1 or 2; [0331] and Q.sup.2 is 1 or 2.

    [0332] The embodiments of the present invention include compounds having formula (IIp-4):

    ##STR00066##

    [0333] Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0334] Q.sup.1 is 1 or 2; [0335] and Q.sup.2 is 1 or 2.

    [0336] The embodiments of the present invention include compounds having formula (IIp-5):

    ##STR00067##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0337] Q.sup.1 is 1 or 2; [0338] and Q.sup.2 is 1 or 2.

    [0339] The embodiments of the present invention include compounds having formula (IIq):

    ##STR00068##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0340] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00069## [0341] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0342] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0343] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0344] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0345] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0346] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0347] and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20 are hydrogen.

    [0348] The embodiments of the present invention include compounds having formula (IIr):

    ##STR00070##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0349] Q.sup.1 is 1 or 2; [0350] and Q.sup.2 is 1 or 2.

    [0351] The embodiments of the present invention include compounds having formula (Hs):

    ##STR00071##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0352] Q.sup.1 is 1 or 2; [0353] and Q.sup.2 is 1 or 2.

    [0354] The embodiments of the present invention include compounds having formula (IIt):

    ##STR00072##

    [0355] Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0356] Q.sup.1 is 1 or 2; [0357] and Q.sup.2 is 1 or 2.

    [0358] The embodiments of the present invention include compounds having formula (IIt-1):

    ##STR00073##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0359] Q.sup.1 is 1 or 2; [0360] and Q.sup.2 is 1 or 2.

    [0361] The embodiments of the present invention include compounds having formula (IIt-2):

    ##STR00074##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0362] Q.sup.1 is 1 or 2; [0363] and Q.sup.2 is 1 or 2.

    [0364] The embodiments of the present invention include compounds having formula (IIt-3):

    ##STR00075##

    [0365] Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0366] Q.sup.1 is 1 or 2; [0367] and Q.sup.2 is 1 or 2.

    [0368] The embodiments of the present invention include compounds having formula (IIt-4):

    ##STR00076##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0369] Q.sup.1 is 1 or 2; [0370] and Q.sup.2 is 1 or 2.

    [0371] The embodiments of the present invention include compounds having formula (IIt-5):

    ##STR00077##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0372] Q.sup.1 is 1 or 2; [0373] and Q.sup.2 is 1 or 2.

    [0374] The embodiments of the present invention include compounds having formula (IIu):

    ##STR00078##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0375] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00079## [0376] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0377] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0378] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0379] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0380] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0381] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0382] and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    [0383] The embodiments of the present invention include compounds having formula (IIv):

    ##STR00080##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0384] Q.sup.1 is 1 or 2; [0385] and Q.sup.2 is 1 or 2.

    [0386] The embodiments of the present invention include compounds having formula (IIw):

    ##STR00081##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0387] Q.sup.1 is 1 or 2; [0388] and Q.sup.2 is 1 or 2.

    [0389] The embodiments of the present invention include compounds having formula (IIx):

    ##STR00082##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0390] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0391] Q.sup.1 is 1 or 2; [0392] and Q.sup.2 is 1 or 2.

    [0393] The embodiments of the present invention include compounds having formula (IIx-1):

    ##STR00083##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0394] Q.sup.1 is 1 or 2; [0395] and Q.sup.2 is 1 or 2.

    [0396] The embodiments of the present invention include compounds having formula (IIx-2):

    ##STR00084##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0397] Q.sup.1 is 1 or 2; [0398] and Q.sup.2 is 1 or 2.

    [0399] The embodiments of the present invention include compounds having formula (IIx-3):

    ##STR00085##

    [0400] Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0401] Q.sup.1 is 1 or 2; [0402] and Q.sup.2 is 1 or 2.

    [0403] The embodiments of the present invention include compounds having formula (IIx-4):

    ##STR00086##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0404] Q.sup.1 is 1 or 2; [0405] and Q.sup.2 is 1 or 2.

    [0406] The embodiments of the present invention include compounds having formula (IIx-5):

    ##STR00087##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0407] Q.sup.1 is 1 or 2; [0408] and Q.sup.2 is 1 or 2.

    [0409] The embodiments of the present invention include compounds having formula (III):

    ##STR00088##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.

    [0410] The embodiments of the present invention include compounds having formula (IIIa):

    ##STR00089##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0411] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00090## [0412] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0413] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 [0414] linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0415] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0416] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0417] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0418] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0419] and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are hydrogen.

    [0420] The embodiments of the present invention include compounds having formula (IIIb):

    ##STR00091##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0421] Q.sup.1 is 1 or 2; [0422] and Q.sup.2 is 1 or 2.

    [0423] The embodiments of the present invention include compounds having formula (IIIc):

    ##STR00092##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0424] Q.sup.1 is 1 or 2; [0425] and Q.sup.2 is 1 or 2.

    [0426] The embodiments of the present invention include compounds having formula (IIId):

    ##STR00093##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0427] Q.sup.1 is 1 or 2; [0428] and Q.sup.2 is 1 or 2.

    [0429] The embodiments of the present invention include compounds having formula (IIId-1):

    ##STR00094##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0430] Q.sup.1 is 1 or 2; [0431] and Q.sup.2 is 1 or 2.

    [0432] The embodiments of the present invention include compounds having formula (IIId-2):

    ##STR00095##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0433] Q.sup.1 is 1 or 2; [0434] and Q.sup.2 is 1 or 2.

    [0435] The embodiments of the present invention include compounds having formula (IIId-3):

    ##STR00096##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0436] Q.sup.1 is 1 or 2; [0437] and Q.sup.2 is 1 or 2.

    [0438] The embodiments of the present invention include compounds having formula (IIId-4):

    ##STR00097##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0439] Q.sup.1 is 1 or 2; [0440] and Q.sup.2 is 1 or 2.

    [0441] The embodiments of the present invention include compounds having formula (IIId-5):

    ##STR00098##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0442] Q.sup.1 is 1 or 2; [0443] and Q.sup.2 is 1 or 2.

    [0444] The embodiments of the present invention include compounds having formula (IIIe):

    ##STR00099##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0445] R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00100## [0446] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0447] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0448] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0449] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0450] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0451] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0452] and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    [0453] The embodiments of the present invention include compounds having formula (IIIf):

    ##STR00101##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0454] Q.sup.1 is 1 or 2; [0455] and Q.sup.2 is 1 or 2.

    [0456] The embodiments of the present invention include compounds having formula (IIIg):

    ##STR00102##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0457] Q.sup.1 is 1 or 2; [0458] and Q.sup.2 is 1 or 2.

    [0459] The embodiments of the present invention include compounds having formula (IIIh):

    ##STR00103##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0460] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0461] Q.sup.1 is 1 or 2; [0462] and Q.sup.2 is 1 or 2.

    [0463] The embodiments of the present invention include compounds having formula (IIIh-1):

    ##STR00104##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0464] Q.sup.1 is 1 or 2; [0465] and Q.sup.2 is 1 or 2.

    [0466] The embodiments of the present invention include compounds having formula (IIIh-2):

    ##STR00105##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0467] Q.sup.1 is 1 or 2; [0468] and Q.sup.2 is 1 or 2.

    [0469] The embodiments of the present invention include compounds having formula (IIIh-3):

    ##STR00106##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0470] Q.sup.1 is 1 or 2; [0471] and Q.sup.2 is 1 or 2.

    [0472] The embodiments of the present invention include compounds having formula (IIIh-4):

    ##STR00107##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0473] Q.sup.1 is 1 or 2; [0474] and Q.sup.2 is 1 or 2.

    [0475] The embodiments of the present invention include compounds having formula (IIIh-5):

    ##STR00108##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0476] Q.sup.1 is 1 or 2; [0477] and Q.sup.2 is 1 or 2.

    [0478] The embodiments of the present invention include compounds having formula (IIIi):

    ##STR00109##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0479] R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00110## [0480] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0481] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0482] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0483] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0484] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0485] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0486] and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are hydrogen.

    [0487] The embodiments of the present invention include compounds having formula (IIIj):

    ##STR00111##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0488] Q.sup.1 is 1 or 2; [0489] and Q.sup.2 is 1 or 2.

    [0490] The embodiments of the present invention include compounds having formula (IIIk):

    ##STR00112##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0491] Q.sup.1 is 1 or 2; [0492] and Q.sup.2 is 1 or 2.

    [0493] The embodiments of the present invention include compounds having formula (IIIL):

    ##STR00113##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0494] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0495] Q.sup.1 is 1 or 2; [0496] and Q.sup.2 is 1 or 2.

    [0497] The embodiments of the present invention include compounds having formula (IIIL-1):

    ##STR00114##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0498] Q.sup.1 is 1 or 2; [0499] and Q.sup.2 is 1 or 2.

    [0500] The embodiments of the present invention include compounds having formula (IIIL-2):

    ##STR00115##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0501] Q.sup.1 is 1 or 2; [0502] and Q.sup.2 is 1 or 2.

    [0503] The embodiments of the present invention include compounds having formula (IIIL-3):

    ##STR00116##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0504] Q.sup.1 is 1 or 2; [0505] and Q.sup.2 is 1 or 2.

    [0506] The embodiments of the present invention include compounds having formula (IIIL-4):

    ##STR00117##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0507] Q.sup.1 is 1 or 2; [0508] and Q.sup.2 is 1 or 2.

    [0509] The embodiments of the present invention include compounds having formula (IIIL-5):

    ##STR00118##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0510] Q.sup.1 is 1 or 2; [0511] and Q.sup.2 is 1 or 2.

    [0512] The embodiments of the present invention include compounds having formula

    ##STR00119##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0513] R.sup.20a, R.sup.20b, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00120## [0514] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0515] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0516] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0517] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0518] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0519] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0520] and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    [0521] The embodiments of the present invention include compounds having formula (IIIn):

    ##STR00121##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0522] Q.sup.1 is 1 or 2; [0523] and Q.sup.2 is 1 or 2.

    [0524] The embodiments of the present invention include compounds having formula (IIIo):

    ##STR00122##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0525] Q.sup.1 is 1 or 2; [0526] and Q.sup.2 is 1 or 2.

    [0527] The embodiments of the present invention include compounds having formula (IIIp):

    ##STR00123##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0528] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0529] Q.sup.1 is 1 or 2; [0530] and Q.sup.2 is 1 or 2.

    [0531] The embodiments of the present invention include compounds having formula (IIIp-1):

    ##STR00124##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0532] Q.sup.1 is 1 or 2; [0533] and Q.sup.2 is 1 or 2.

    [0534] The embodiments of the present invention include compounds having formula (IIIp-2):

    ##STR00125##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0535] Q.sup.1 is 1 or 2; [0536] and Q.sup.2 is 1 or 2.

    [0537] The embodiments of the present invention include compounds having formula (IIIp-3):

    ##STR00126##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0538] Q.sup.1 is 1 or 2; [0539] and Q.sup.2 is 1 or 2.

    [0540] The embodiments of the present invention include compounds having formula (IIIp-4):

    ##STR00127##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0541] Q.sup.1 is 1 or 2; [0542] and Q.sup.2 is 1 or 2.

    [0543] The embodiments of the present invention include compounds having formula (IIIp-5):

    ##STR00128##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0544] Q.sup.1 is 1 or 2; [0545] and Q.sup.2 is 1 or 2.

    [0546] The embodiments of the present invention include compounds having formula (IIIq):

    ##STR00129##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0547] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00130## [0548] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0549] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0550] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0551] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0552] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0553] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0554] and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    [0555] The embodiments of the present invention include compounds having formula (IIIr):

    ##STR00131##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0556] Q.sup.1 is 1 or 2; [0557] and Q.sup.2 is 1 or 2.

    [0558] The embodiments of the present invention include compounds having formula (IIIs):

    ##STR00132##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0559] Q.sup.1 is 1 or 2; [0560] and Q.sup.2 is 1 or 2.

    [0561] The embodiments of the present invention include compounds having formula (IIIt):

    ##STR00133##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0562] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0563] Q.sup.1 is 1 or 2; [0564] and Q.sup.2 is 1 or 2.

    [0565] The embodiments of the present invention include compounds having formula (IIIt-1):

    ##STR00134##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0566] Q.sup.1 is 1 or 2; [0567] and Q.sup.2 is 1 or 2.

    [0568] The embodiments of the present invention include compounds having formula (IIIt-2):

    ##STR00135##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0569] Q.sup.1 is 1 or 2; [0570] and Q.sup.2 is 1 or 2.

    [0571] The embodiments of the present invention include compounds having formula (IIIt-3):

    ##STR00136##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0572] Q.sup.1 is 1 or 2; [0573] and Q.sup.2 is 1 or 2.

    [0574] The embodiments of the present invention include compounds having formula (IIIt-4):

    ##STR00137##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0575] Q.sup.1 is 1 or 2; [0576] and Q.sup.2 is 1 or 2.

    [0577] The embodiments of the present invention include compounds having formula (IIIt-5):

    ##STR00138##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0578] Q.sup.1 is 1 or 2; [0579] and Q.sup.2 is 1 or 2.

    [0580] The embodiments of the present invention include compounds having formula (IIIu):

    ##STR00139##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0581] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00140## [0582] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0583] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0584] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0585] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0586] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0587] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0588] and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    [0589] The embodiments of the present invention include compounds having formula (IIIv):

    ##STR00141##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0590] Q.sup.1 is 1 or 2; [0591] and Q.sup.2 is 1 or 2.

    [0592] The embodiments of the present invention include compounds having formula (IIIw):

    ##STR00142##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0593] Q.sup.1 is 1 or 2; [0594] and Q.sup.2 is 1 or 2.

    [0595] The embodiments of the present invention include compounds having formula (IIIx):

    ##STR00143##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0596] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0597] Q.sup.1 is 1 or 2; [0598] and Q.sup.2 is 1 or 2.

    [0599] The embodiments of the present invention include compounds having formula (IIIx-1):

    ##STR00144##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0600] Q.sup.1 is 1 or 2; [0601] and Q.sup.2 is 1 or 2.

    [0602] The embodiments of the present invention include compounds having formula (IIIx-2):

    ##STR00145##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0603] Q.sup.1 is 1 or 2; [0604] and Q.sup.2 is 1 or 2.

    [0605] The embodiments of the present invention include compounds having formula (IIIx-3):

    ##STR00146##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0606] Q.sup.1 is 1 or 2; [0607] and Q.sup.2 is 1 or 2.

    [0608] The embodiments of the present invention include compounds having formula (IIIx-4):

    ##STR00147##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0609] Q.sup.1 is 1 or 2; [0610] and Q.sup.2 is 1 or 2.

    [0611] The embodiments of the present invention include compounds having formula (IIIx-5):

    ##STR00148##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0612] Q.sup.1 is 1 or 2; [0613] and Q.sup.2 is 1 or 2.

    [0614] The embodiments of the present invention include compounds having formula (IV):

    ##STR00149##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.

    [0615] In embodiments, a compound has a structure according to Formula (XLVII),

    ##STR00150##

    or a pharmaceutically acceptable salt thereof.

    [0616] In embodiments, a compound has a structure according to Formula (XLVII),

    ##STR00151##

    or a pharmaceutically acceptable salt thereof.

    [0617] In embodiments, n is 1, 2, or 3. In embodiments, n is 1. In embodiments, n is 2. In embodiments, n is 1 or 2.

    [0618] In embodiments, each of R.sup.1 and R.sup.2 is unsubstituted C.sub.1-6 alkyl. In embodiments, each of R.sup.1 and R.sup.2 is ethyl. In embodiments, each of R.sup.1 and R.sup.2 is methyl.

    [0619] In embodiments, R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring, optionally containing one carbon-carbon double bonds and/or a ring atom selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7.

    [0620] In embodiments, R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a C.sub.3-C.sub.8 cycloalkyl or a C.sub.5-C.sub.8 cycloalkenyl.

    [0621] In embodiments, R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a C.sub.3-C.sub.8 cycloalkyl or C.sub.5-C.sub.8 cycloalkenyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, and cyclooctenyl. In embodiments, said C.sub.3-C.sub.8 cycloalkyl or C.sub.5-C.sub.8 cycloalkenyl is unsubstituted. In embodiments, said C.sub.3-C.sub.8 cycloalkyl or C.sub.5-C.sub.8 cycloalkenyl is substituted by 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In embodiments, said substituents are selected from oxo (═O), hydroxyl, halo, cyano, C.sub.1-6 alkoxy, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.1-6 haloalkyl, C.sub.3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of—OH, —F, —Cl, —Br, ——, —CN, —OMe, —OEt, —OnPr, —O.sup.iPr, —OCF.sub.3, -Me, -Et, —.sup.nPr, —.sup.iPr, —CF.sub.3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

    [0622] In embodiments, R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring containing a ring atom that is NR.sup.7. In embodiments, said 5- to 8-membered ring is not further substituted. In embodiments, said 5- to 8-membered ring further comprises 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In embodiments, said substituents are selected from oxo (═O), hydroxyl, halo, cyano, C.sub.1-6 alkoxy, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.1-6 haloalkyl, C.sub.3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —I, —CN, —OMe, —OEt, —O.sup.nPr, —O.sup.iPr, —OCF.sub.3, -Me, -Et, —.sup.nPr, —.sup.iPr, —CF.sub.3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

    [0623] In embodiments, R.sup.1 and R.sup.2 are taken together to form a pyrrolidinyl or piperidinyl group where the nitrogen atom is NR.sup.7. In embodiments, said pyrrolidinyl or piperidinyl group is not further substituted. In embodiments, said pyrrolidinyl or piperidinyl group further comprises 1, 2, 3, or 4 substituents as described herein.

    [0624] In embodiments, R.sup.7 is COR.sup.8, and R.sup.8 is C.sub.1-6 linear alkyl.

    [0625] In embodiments, R.sup.7 is acetyl.

    [0626] In embodiments, R.sup.7 is SO.sub.2R.sup.10c, and R.sup.10c is C.sub.1-6 linear alkyl.

    [0627] In embodiments, R.sup.10c is methyl (i.e., R.sup.7 is SO.sub.2Me).

    [0628] In embodiments, R.sup.4 is phenyl.

    [0629] In embodiments, R.sup.4 is substituted phenyl. In embodiments, R.sup.4 is phenyl substituted by 1, 2, 3, 4, or 5 substituents (e.g., phenyl substituted by 1 or 2 substituents as described herein). In embodiments, the substitutents are selected from the group consisting of hydroxyl, halo, cyano, C.sub.1-6 alkoxy, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.1-6 haloalkyl, C.sub.3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —CN, —OMe, —OEt, —O.sup.nPr, —O.sup.iPr, —OCF.sub.3, -Me, -Et, —.sup.nPr, —.sup.iPr, —CF.sub.3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

    [0630] In embodiments, R.sup.4 is selected from the group consisting of hydroxylphenyl, fluorophenyl, chlorophenyl, bromophenyl, cyanophenyl, tolyl, methoxylphenyl, difluorophenyl, dichlorophenyl, chloro-fluorophenyl, dimethylphenyl, trifluoromethylphenyl, di(trifluoromethyl)phenyl,

    [0631] In embodiments, R.sup.4 is selected from the group consisting of 4-hydroxyphenyl, 3-fluorophenyl, 4-fluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-fluoro-3-chlorophenyl, 4-cyanophenyl, 2-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-isopropylphenyl, 4-trifluoromethylphenyl, 2-morpholinophenyl, and 4-methyl-2-morpholinophenyl.

    [0632] In embodiments, R.sup.4 is pyridyl. In embodiments, R.sup.4 is 2-pyridyl. In embodiments, R.sup.4 is 3-pyridyl. In embodiments, R.sup.4 is 4-pyridyl. In embodiments, said pyridyl is unsubstituted. In embodiments, said pyridyl is substituted by 1, 2, 3, or 4 substituents (e.g., pyridyl substituted by 1 or 2 substituents as described herein). In embodiments, the substitutents are selected from the group consisting of hydroxyl, halo, cyano, C.sub.1-6 alkoxy, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.1-6 haloalkyl, C.sub.3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —I, —CN, —OMe, —OEt, —O.sup.nPr, —O.sup.iPr, —OCF.sub.3, -Me, -Et, —.sup.nPr, —.sup.iPr, —CF.sub.3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

    [0633] The embodiments of the present invention include compounds having formula (IVa):

    ##STR00152##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0634] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00153## [0635] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0636] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0637] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0638] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0639] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0640] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0641] and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are hydrogen.

    [0642] The embodiments of the present invention include compounds having formula (IVb):

    ##STR00154##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0643] Q.sup.1 is 1 or 2; [0644] and Q.sup.2 is 1 or 2.

    [0645] The embodiments of the present invention include compounds having formula (IVc):

    ##STR00155##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0646] Q.sup.1 is 1 or 2; [0647] and Q.sup.2 is 1 or 2.

    [0648] The embodiments of the present invention include compounds having formula (IVd):

    ##STR00156##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0649] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0650] Q.sup.1 is 1 or 2; [0651] and Q.sup.2 is 1 or 2.

    [0652] The embodiments of the present invention include compounds having formula (IVd-1):

    ##STR00157##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0653] Q.sup.1 is 1 or 2; [0654] and Q.sup.2 is 1 or 2.

    [0655] The embodiments of the present invention include compounds having formula (IVd-2):

    ##STR00158##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0656] Q.sup.1 is 1 or 2; [0657] and Q.sup.2 is 1 or 2.

    [0658] The embodiments of the present invention include compounds having formula (IVd-3):

    ##STR00159##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0659] Q.sup.1 is 1 or 2; [0660] and Q.sup.2 is 1 or 2.

    [0661] The embodiments of the present invention include compounds having formula (IVd-4):

    ##STR00160##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0662] Q.sup.1 is 1 or 2; [0663] and Q.sup.2 is 1 or 2.

    [0664] The embodiments of the present invention include compounds having formula (IVd-5):

    ##STR00161##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0665] Q.sup.1 is 1 or 2; [0666] and Q.sup.2 is 1 or 2.

    [0667] The embodiments of the present invention include compounds having formula (IVe):

    ##STR00162##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0668] R.sup.20a, R.sup.20b, R.sup.20c, and R20d are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00163## [0669] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0670] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0671] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0672] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0673] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0674] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0675] and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    [0676] The embodiments of the present invention include compounds having formula (IVf):

    ##STR00164##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0677] Q.sup.1 is 1 or 2; [0678] and Q.sup.2 is 1 or 2.

    [0679] The embodiments of the present invention include compounds having formula (IVg):

    ##STR00165##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0680] Q.sup.1 is 1 or 2; [0681] and Q.sup.2 is 1 or 2.

    [0682] The embodiments of the present invention include compounds having formula (IVh):

    ##STR00166##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0683] Q.sup.1 is 1 or 2; [0684] and Q.sup.2 is 1 or 2.

    [0685] The embodiments of the present invention include compounds having formula (IVh-1):

    ##STR00167##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0686] Q.sup.1 is 1 or 2; [0687] and Q.sup.2 is 1 or 2.

    [0688] The embodiments of the present invention include compounds having formula (IVh-2):

    ##STR00168##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0689] Q.sup.1 is 1 or 2; [0690] and Q.sup.2 is 1 or 2.

    [0691] The embodiments of the present invention include compounds having formula (IVh-3):

    ##STR00169##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0692] Q.sup.1 is 1 or 2; [0693] and Q.sup.2 is 1 or 2.

    [0694] The embodiments of the present invention include compounds having formula (IVh-4):

    ##STR00170##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0695] Q.sup.1 is 1 or 2; [0696] and Q.sup.2 is 1 or 2.

    [0697] The embodiments of the present invention include compounds having formula (IVh-5):

    ##STR00171##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0698] Q.sup.1 is 1 or 2; [0699] and Q.sup.2 is 1 or 2.

    [0700] The embodiments of the present invention include compounds having formula (IVi):

    ##STR00172##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0701] R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00173## [0702] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0703] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0704] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0705] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0706] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0707] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0708] and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are hydrogen.

    [0709] The embodiments of the present invention include compounds having formula (IVj):

    ##STR00174##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0710] Q.sup.1 is 1 or 2; [0711] and Q.sup.2 is 1 or 2.

    [0712] The embodiments of the present invention include compounds having formula (IVk):

    ##STR00175##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0713] Q.sup.1 is 1 or 2; [0714] and Q.sup.2 is 1 or 2.

    [0715] The embodiments of the present invention include compounds having formula (IVL):

    ##STR00176##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0716] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0717] Q.sup.1 is 1 or 2; [0718] and Q.sup.2 is 1 or 2.

    [0719] The embodiments of the present invention include compounds having formula (IVL-1):

    ##STR00177##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0720] Q.sup.1 is 1 or 2; [0721] and Q.sup.2 is 1 or 2.

    [0722] The embodiments of the present invention include compounds having formula (IVL-2):

    ##STR00178##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0723] Q.sup.1 is 1 or 2; [0724] and Q.sup.2 is 1 or 2.

    [0725] The embodiments of the present invention include compounds having formula (IVL-3):

    ##STR00179##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0726] Q.sup.1 is 1 or 2; [0727] and Q.sup.2 is 1 or 2.

    [0728] The embodiments of the present invention include compounds having formula (IVL-4):

    ##STR00180##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0729] Q.sup.1 is 1 or 2; [0730] and Q.sup.2 is 1 or 2.

    [0731] The embodiments of the present invention include compounds having formula (IVL-5):

    ##STR00181##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0732] Q.sup.1 is 1 or 2; [0733] and Q.sup.2 is 1 or 2.

    [0734] The embodiments of the present invention include compounds having formula (IVm):

    ##STR00182##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0735] R.sup.20a, R.sup.20b, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00183## [0736] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0737] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0738] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0739] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0740] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0741] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0742] and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    [0743] The embodiments of the present invention include compounds having formula (IVn):

    ##STR00184##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0744] Q.sup.1 is 1 or 2; [0745] and Q.sup.2 is 1 or 2.

    [0746] The embodiments of the present invention include compounds having formula (IVo):

    ##STR00185##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0747] Q.sup.1 is 1 or 2; [0748] and Q.sup.2 is 1 or 2.

    [0749] The embodiments of the present invention include compounds having formula (IVp):

    ##STR00186##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0750] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0751] Q.sup.1 is 1 or 2; [0752] and Q.sup.2 is 1 or 2.

    [0753] The embodiments of the present invention include compounds having formula (IVp-1):

    ##STR00187##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0754] Q.sup.1 is 1 or 2; [0755] and Q.sup.2 is 1 or 2.

    [0756] The embodiments of the present invention include compounds having formula (IVp-2):

    ##STR00188##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0757] Q.sup.1 is 1 or 2; [0758] and Q.sup.2 is 1 or 2.

    [0759] The embodiments of the present invention include compounds having formula (IVp-3):

    ##STR00189##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0760] Q.sup.1 is 1 or 2; [0761] and Q.sup.2 is 1 or 2.

    [0762] The embodiments of the present invention include compounds having formula (IVp-4):

    ##STR00190##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0763] Q.sup.1 is 1 or 2; [0764] and Q.sup.2 is 1 or 2.

    [0765] The embodiments of the present invention include compounds having formula (IVp-5):

    ##STR00191##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0766] Q.sup.1 is 1 or 2; [0767] and Q.sup.2 is 1 or 2.

    [0768] The embodiments of the present invention include compounds having formula (IVq):

    ##STR00192##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0769] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00193## [0770] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0771] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0772] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0773] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0774] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0775] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0776] and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    [0777] The embodiments of the present invention include compounds having formula (IVr):

    ##STR00194##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0778] Q.sup.1 is 1 or 2; [0779] and Q.sup.2 is 1 or 2.

    [0780] The embodiments of the present invention include compounds having formula (IVs):

    ##STR00195##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0781] Q.sup.1 is 1 or 2; [0782] and Q.sup.2 is 1 or 2.

    [0783] The embodiments of the present invention include compounds having formula (IVt):

    ##STR00196##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0784] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0785] Q.sup.1 is 1 or 2; [0786] and Q.sup.2 is 1 or 2.

    [0787] The embodiments of the present invention include compounds having formula (IVt-1):

    ##STR00197##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0788] Q.sup.1 is 1 or 2; [0789] and Q.sup.2 is 1 or 2.

    [0790] The embodiments of the present invention include compounds having formula (IVt-2):

    ##STR00198##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0791] Q.sup.1 is 1 or 2; [0792] and Q.sup.2 is 1 or 2.

    [0793] The embodiments of the present invention include compounds having formula (IVt-3):

    ##STR00199##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0794] Q.sup.1 is 1 or 2; [0795] and Q.sup.2 is 1 or 2.

    [0796] The embodiments of the present invention include compounds having formula (IVt-4):

    ##STR00200##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0797] Q.sup.1 is 1 or 2; [0798] and Q.sup.2 is 1 or 2.

    [0799] The embodiments of the present invention include compounds having formula (IVt-5):

    ##STR00201##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0800] Q.sup.1 is 1 or 2; [0801] and Q.sup.2 is 1 or 2.

    [0802] The embodiments of the present invention include compounds having formula (IVu):

    ##STR00202##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0803] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00203## [0804] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0805] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0806] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0807] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0808] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0809] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0810] and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    [0811] The embodiments of the present invention include compounds having formula (IVv):

    ##STR00204##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0812] Q.sup.1 is 1 or 2; [0813] and Q.sup.2 is 1 or 2.

    [0814] The embodiments of the present invention include compounds having formula (IVw):

    ##STR00205##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0815] Q.sup.1 is 1 or 2; [0816] and Q.sup.2 is 1 or 2.

    [0817] The embodiments of the present invention include compounds having formula (IVx):

    ##STR00206##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0818] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0819] Q.sup.1 is 1 or 2; [0820] and Q.sup.2 is 1 or 2.

    [0821] The embodiments of the present invention include compounds having formula (IVx-1):

    ##STR00207##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0822] Q.sup.1 is 1 or 2; [0823] and Q.sup.2 is 1 or 2.

    [0824] The embodiments of the present invention include compounds having formula (IVx-2):

    ##STR00208##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0825] Q.sup.1 is 1 or 2; [0826] and Q.sup.2 is 1 or 2.

    [0827] The embodiments of the present invention include compounds having formula (IVx-3):

    ##STR00209##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0828] Q.sup.1 is 1 or 2; [0829] and Q.sup.2 is 1 or 2.

    [0830] The embodiments of the present invention include compounds having formula (IVx-4):

    ##STR00210##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0831] Q.sup.1 is 1 or 2; [0832] and Q.sup.2 is 1 or 2.

    [0833] The embodiments of the present invention include compounds having formula (IVx-5):

    ##STR00211##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0834] Q.sup.1 is 1 or 2; [0835] and Q.sup.2 is 1 or 2.

    [0836] The embodiments of the present invention include compounds having formula (V):

    ##STR00212##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.

    [0837] The embodiments of the present invention include compounds having formula (Va):

    ##STR00213##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0838] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23bNHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00214## [0839] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0840] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0841] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0842] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0843] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0844] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0845] and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are hydrogen.

    [0846] The embodiments of the present invention include compounds having formula (Vb):

    ##STR00215##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0847] Q.sup.1 is 1 or 2; [0848] and Q.sup.2 is 1 or 2.

    [0849] The embodiments of the present invention include compounds having formula (Vc):

    ##STR00216##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0850] Q.sup.1 is 1 or 2; [0851] and Q.sup.2 is 1 or 2.

    [0852] The embodiments of the present invention include compounds having formula (Vd):

    ##STR00217##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0853] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0854] Q.sup.1 is 1 or 2; [0855] and Q.sup.2 is 1 or 2.

    [0856] The embodiments of the present invention include compounds having formula (Vd-1):

    ##STR00218##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0857] Q.sup.1 is 1 or 2; [0858] and Q.sup.2 is 1 or 2.

    [0859] The embodiments of the present invention include compounds having formula (Vd-2):

    ##STR00219##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0860] Q.sup.1 is 1 or 2; [0861] and Q.sup.2 is 1 or 2.

    [0862] The embodiments of the present invention include compounds having formula (Vd-3):

    ##STR00220##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0863] Q.sup.1 is 1 or 2; [0864] and Q.sup.2 is 1 or 2.

    [0865] The embodiments of the present invention include compounds having formula (Vd-4):

    ##STR00221##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0866] Q.sup.1 is 1 or 2; [0867] and Q.sup.2 is 1 or 2.

    [0868] The embodiments of the present invention include compounds having formula (Vd-5):

    ##STR00222##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0869] Q.sup.1 is 1 or 2; [0870] and Q.sup.2 is 1 or 2.

    [0871] The embodiments of the present invention include compounds having formula (Ve):

    ##STR00223##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0872] R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00224## [0873] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0874] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0875] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0876] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0877] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0878] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0879] and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    [0880] The embodiments of the present invention include compounds having formula (Vf):

    ##STR00225##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0881] Q.sup.1 is 1 or 2; [0882] and Q.sup.2 is 1 or 2.

    [0883] The embodiments of the present invention include compounds having formula (Vg):

    ##STR00226##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0884] Q.sup.1 is 1 or 2; [0885] and Q.sup.2 is 1 or 2.

    [0886] The embodiments of the present invention include compounds having formula (Vh):

    ##STR00227##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0887] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0888] Q.sup.1 is 1 or 2; [0889] and Q.sup.2 is 1 or 2.

    [0890] The embodiments of the present invention include compounds having formula (Vh-1):

    ##STR00228##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0891] Q.sup.1 is 1 or 2; [0892] and Q.sup.2 is 1 or 2.

    [0893] The embodiments of the present invention include compounds having formula (Vh-2):

    ##STR00229##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0894] Q.sup.1 is 1 or 2; [0895] and Q.sup.2 is 1 or 2.

    [0896] The embodiments of the present invention include compounds having formula (Vh-3):

    ##STR00230##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0897] Q.sup.1 is 1 or 2; [0898] and Q.sup.2 is 1 or 2.

    [0899] The embodiments of the present invention include compounds having formula (Vh-4):

    ##STR00231##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0900] Q.sup.1 is 1 or 2; [0901] and Q.sup.2 is 1 or 2.

    [0902] The embodiments of the present invention include compounds having formula (Vh-5):

    ##STR00232##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0903] Q.sup.1 is 1 or 2; [0904] and Q.sup.2 is 1 or 2.

    [0905] The embodiments of the present invention include compounds having formula (Vi):

    ##STR00233##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0906] R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00234## [0907] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0908] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0909] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0910] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0911] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0912] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0913] and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are hydrogen.

    [0914] The embodiments of the present invention include compounds having formula (Vj):

    ##STR00235##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0915] Q.sup.1 is 1 or 2; [0916] and Q.sup.2 is 1 or 2.

    [0917] The embodiments of the present invention include compounds having formula (Vk):

    ##STR00236##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0918] Q.sup.1 is 1 or 2; [0919] and Q.sup.2 is 1 or 2.

    [0920] The embodiments of the present invention include compounds having formula (VL):

    ##STR00237##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0921] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0922] Q.sup.1 is 1 or 2; [0923] and Q.sup.2 is 1 or 2.

    [0924] The embodiments of the present invention include compounds having formula (VL-1):

    ##STR00238##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0925] Q.sup.1 is 1 or 2; [0926] and Q.sup.2 is 1 or 2.

    [0927] The embodiments of the present invention include compounds having formula (VL-2):

    ##STR00239##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0928] Q.sup.1 is 1 or 2; [0929] and Q.sup.2 is 1 or 2.

    [0930] The embodiments of the present invention include compounds having formula (VL-3):

    ##STR00240##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0931] Q.sup.1 is 1 or 2; [0932] and Q.sup.2 is 1 or 2.

    [0933] The embodiments of the present invention include compounds having formula (VL-4):

    ##STR00241##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0934] Q.sup.1 is 1 or 2; [0935] and Q.sup.2 is 1 or 2.

    [0936] The embodiments of the present invention include compounds having formula (VL-5):

    ##STR00242##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0937] Q.sup.1 is 1 or 2; [0938] and Q.sup.2 is 1 or 2.

    [0939] The embodiments of the present invention include compounds having formula (Vm):

    ##STR00243##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0940] R.sup.20a, R.sup.20b, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00244## [0941] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0942] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0943] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0944] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0945] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0946] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0947] and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    [0948] The embodiments of the present invention include compounds having formula (Vn):

    ##STR00245##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0949] Q.sup.1 is 1 or 2; [0950] and Q.sup.2 is 1 or 2.

    [0951] The embodiments of the present invention include compounds having formula (Vo):

    ##STR00246##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0952] Q.sup.1 is 1 or 2; [0953] and Q.sup.2 is 1 or 2.

    [0954] The embodiments of the present invention include compounds having formula (Vp):

    ##STR00247##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0955] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0956] Q.sup.1 is 1 or 2; [0957] and Q.sup.2 is 1 or 2.

    [0958] The embodiments of the present invention include compounds having formula (Vp-1):

    ##STR00248##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0959] Q.sup.1 is 1 or 2; [0960] and Q.sup.2 is 1 or 2.

    [0961] The embodiments of the present invention include compounds having formula (Vp-2):

    ##STR00249##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0962] Q.sup.1 is 1 or 2; [0963] and Q.sup.2 is 1 or 2.

    [0964] The embodiments of the present invention include compounds having formula (Vp-3):

    ##STR00250##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0965] Q.sup.1 is 1 or 2; [0966] and Q.sup.2 is 1 or 2.

    [0967] The embodiments of the present invention include compounds having formula (Vp-4):

    ##STR00251##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0968] Q.sup.1 is 1 or 2; [0969] and Q.sup.2 is 1 or 2.

    [0970] The embodiments of the present invention include compounds having formula (Vp-5):

    ##STR00252##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0971] Q.sup.1 is 1 or 2; [0972] and Q.sup.2 is 1 or 2.

    [0973] The embodiments of the present invention include compounds having formula (Vq):

    ##STR00253##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0974] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00254## [0975] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0976] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0977] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0978] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0979] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0980] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [0981] and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    [0982] The embodiments of the present invention include compounds having formula (Vr):

    ##STR00255##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0983] Q.sup.1 is 1 or 2; [0984] and Q.sup.2 is 1 or 2.

    [0985] The embodiments of the present invention include compounds having formula (Vs):

    ##STR00256##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0986] Q.sup.1 is 1 or 2; [0987] and Q.sup.2 is 1 or 2.

    [0988] The embodiments of the present invention include compounds having formula (Vt):

    ##STR00257##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0989] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [0990] Q.sup.1 is 1 or 2; [0991] and Q.sup.2 is 1 or 2.

    [0992] The embodiments of the present invention include compounds having formula (Vt-1):

    ##STR00258##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0993] Q.sup.1 is 1 or 2; [0994] and Q.sup.2 is 1 or 2.

    [0995] The embodiments of the present invention include compounds having formula (Vt-2):

    ##STR00259##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0996] Q.sup.1 is 1 or 2; [0997] and Q.sup.2 is 1 or 2.

    [0998] The embodiments of the present invention include compounds having formula (Vt-3):

    ##STR00260##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [0999] Q.sup.1 is 1 or 2; [1000] and Q.sup.2 is 1 or 2.

    [1001] The embodiments of the present invention include compounds having formula (Vt-4):

    ##STR00261##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1002] Q.sup.1 is 1 or 2; [1003] and Q.sup.2 is 1 or 2.

    [1004] The embodiments of the present invention include compounds having formula (Vt-5):

    ##STR00262##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1005] Q.sup.1 is 1 or 2; [1006] and Q.sup.2 is 1 or 2.

    [1007] The embodiments of the present invention include compounds having formula (Vu):

    ##STR00263##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1008] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00264##

    R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1009] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1010] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1011] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1012] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1013] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1014] and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    [1015] The embodiments of the present invention include compounds having formula (Vv):

    ##STR00265##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1016] Q.sup.1 is 1 or 2; [1017] and Q.sup.2 is 1 or 2.

    [1018] The embodiments of the present invention include compounds having formula (Vw):

    ##STR00266##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1019] Q.sup.1 is 1 or 2; [1020] and Q.sup.2 is 1 or 2.

    [1021] The embodiments of the present invention include compounds having formula (Vx):

    ##STR00267##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1022] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [1023] Q.sup.1 is 1 or 2; [1024] and Q.sup.2 is 1 or 2.

    [1025] The embodiments of the present invention include compounds having formula (Vx-1):

    ##STR00268##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1026] Q.sup.1 is 1 or 2; [1027] and Q.sup.2 is 1 or 2.

    [1028] The embodiments of the present invention include compounds having formula (Vx-2):

    ##STR00269##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1029] Q.sup.1 is 1 or 2; [1030] and Q.sup.2 is 1 or 2.

    [1031] The embodiments of the present invention include compounds having formula (Vx-3):

    ##STR00270##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1032] Q.sup.1 is 1 or 2; [1033] and Q.sup.2 is 1 or 2.

    [1034] The embodiments of the present invention include compounds having formula (Vx-4):

    ##STR00271##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1035] Q.sup.1 is 1 or 2; [1036] and Q.sup.2 is 1 or 2.

    [1037] The embodiments of the present invention include compounds having formula (Vx-5):

    ##STR00272##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1038] Q.sup.1 is 1 or 2; [1039] and Q.sup.2 is 1 or 2.

    [1040] The embodiments of the present invention include compounds having formula (VI):

    ##STR00273##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.

    [1041] In embodiments, a compound has a structure according to Formula (XLVI)

    ##STR00274##

    or a pharmaceutically acceptable salt thereof.

    [1042] In embodiments, a compound has a structure according to Formula (XLVIa)

    ##STR00275##

    or a pharmaceutically acceptable salt thereof.

    [1043] In embodiments, n is 1, 2, or 3. In embodiments, n is 1. In embodiments, n is 2. In embodiments, n is 1 or 2.

    [1044] In embodiments, each of R.sup.1 and R.sup.2 is unsubstituted C.sub.1-6 alkyl. In embodiments, each of R.sup.1 and R.sup.2 is ethyl. In embodiments, each of R.sup.1 and R.sup.2 is methyl.

    [1045] In embodiments, R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring, optionally containing one carbon-carbon double bonds and/or a ring atom selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7.

    [1046] In embodiments, R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a C.sub.3-C.sub.8 cycloalkyl or a C.sub.5-C.sub.8 cycloalkenyl.

    [1047] In embodiments, R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a C.sub.3-C.sub.8 cycloalkyl or C.sub.5-C.sub.8 cycloalkenyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, and cyclooctenyl. In embodiments, said C.sub.3-C.sub.8 cycloalkyl or C.sub.5-C.sub.8 cycloalkenyl is unsubstituted. In embodiments, said C.sub.3-C.sub.8 cycloalkyl or C.sub.5-C.sub.8 cycloalkenyl is substituted by 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In embodiments, said substituents are selected from oxo (═O), hydroxyl, halo, cyano, C.sub.1-6 alkoxy, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.1-6 haloalkyl, C.sub.3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —I, —CN, —OMe, —OEt, —O.sup.nPr, —O.sup.iPr, —OCF.sub.3, -Me, -Et, —.sup.nPr, —.sup.iPr, —CF.sub.3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

    [1048] In embodiments, R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring containing a ring atom that is NR.sup.7. In embodiments, said 5- to 8-membered ring is not further substituted. In embodiments, said 5- to 8-membered ring further comprises 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In embodiments, said substituents are selected from oxo (═O), hydroxyl, halo, cyano, C.sub.1-6 alkoxy, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.1-6 haloalkyl, C.sub.3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —I, —CN, —OMe, —OEt, —O.sup.nPr, —O.sup.iPr, —OCF.sub.3, -Me, -Et, —.sup.nPr, —.sup.iPr, —CF.sub.3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

    [1049] In embodiments, R.sup.1 and R.sup.2 are taken together to form a pyrrolidinyl or piperidinyl group where the nitrogen atom is NR.sup.7. In embodiments, said pyrrolidinyl or piperidinyl group is not further substituted. In embodiments, said pyrrolidinyl or piperidinyl group further comprises 1, 2, 3, or 4 substituents as described herein.

    [1050] In embodiments, R.sup.7 is COR.sup.8, and R.sup.8 is C.sub.1-6 linear alkyl.

    [1051] In embodiments, R.sup.7 is acetyl.

    [1052] In embodiments, R.sup.7 is SO.sub.2R.sup.10c, and R.sup.10c s C.sub.1-6 linear alkyl.

    [1053] In embodiments, R.sup.10c is methyl (i.e., R.sup.7 is SO.sub.2Me).

    [1054] In embodiments, R.sup.5 is phenyl.

    [1055] In embodiments, R.sup.5 is substituted phenyl. In embodiments, R.sup.5 is phenyl substituted by 1, 2, 3, 4, or 5 substituents (e.g., phenyl substituted by 1 or 2 substituents as described herein). In embodiments, the substitutents are selected from the group consisting of hydroxyl, halo, cyano, C.sub.1-6 alkoxy, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.1-6 haloalkyl, C.sub.3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —CN, —OMe, —OEt, —O.sup.nPr, —O.sup.iPr, —OCF.sub.3, -Me, -Et, —.sup.nPr, —.sup.iPr, —CF.sub.3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

    [1056] In embodiments, R.sup.5 is selected from the group consisting of hydroxylphenyl, fluorophenyl, chlorophenyl, bromophenyl, cyanophenyl, tolyl, methoxylphenyl, difluorophenyl, dichlorophenyl, chloro-fluorophenyl, dimethylphenyl, trifluoromethylphenyl, di(trifluoromethyl)phenyl,

    [1057] In embodiments, R.sup.5 is selected from the group consisting of 4-hydroxyphenyl, 3-fluorophenyl, 4-fluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-fluoro-3-chlorophenyl, 4-cyanophenyl, 2-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-isopropylphenyl, 4-trifluoromethylphenyl, 2-morpholinophenyl, and 4-methyl-2-morpholinophenyl.

    [1058] In embodiments, R.sup.5 is pyridyl. In embodiments, R.sup.5 is 2-pyridyl. In embodiments, R.sup.5 is 3-pyridyl. In embodiments, R.sup.5 is 4-pyridyl. In embodiments, said pyridyl is unsubstituted. In embodiments, said pyridyl is substituted by 1, 2, 3, or 4 substituents (e.g., pyridyl substituted by 1 or 2 substituents as described herein). In embodiments, the substitutents are selected from the group consisting of hydroxyl, halo, cyano, C.sub.1-6 alkoxy, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.1-6 haloalkyl, C.sub.3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —I, —CN, —OMe, —OEt, —O.sup.nPr, —O.sup.iPr, —OCF.sub.3, -Me, -Et, —.sup.nPr, —.sup.iPr, —CF.sub.3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

    [1059] The embodiments of the present invention include compounds having formula (VIa):

    ##STR00276##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1060] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00277## [1061] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1062] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1063] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1064] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1065] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1066] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1067] and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are hydrogen.

    [1068] The embodiments of the present invention include compounds having formula (VIb):

    ##STR00278##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1069] Q.sup.1 is 1 or 2; [1070] and Q.sup.2 is 1 or 2.

    [1071] The embodiments of the present invention include compounds having formula (VIc):

    ##STR00279##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1072] Q.sup.1 is 1 or 2; [1073] and Q.sup.2 is 1 or 2.

    [1074] The embodiments of the present invention include compounds having formula (VId):

    ##STR00280##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1075] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [1076] Q.sup.1 is 1 or 2; [1077] and Q.sup.2 is 1 or 2.

    [1078] The embodiments of the present invention include compounds having formula (Vid-1):

    ##STR00281##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1079] Q.sup.1 is 1 or 2; [1080] and Q.sup.2 is 1 or 2.

    [1081] The embodiments of the present invention include compounds having formula (Vid-2):

    ##STR00282##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1082] Q.sup.1 is 1 or 2; [1083] and Q.sup.2 is 1 or 2.

    [1084] The embodiments of the present invention include compounds having formula (Vid-3):

    ##STR00283##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1085] Q.sup.1 is 1 or 2; [1086] and Q.sup.2 is 1 or 2.

    [1087] The embodiments of the present invention include compounds having formula (Vid-4):

    ##STR00284##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1088] Q.sup.1 is 1 or 2; [1089] and Q.sup.2 is 1 or 2.

    [1090] The embodiments of the present invention include compounds having formula (Vid-5):

    ##STR00285##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1091] Q.sup.1 is 1 or 2; [1092] and Q.sup.2 is 1 or 2.

    [1093] The embodiments of the present invention include compounds having formula (VIe):

    ##STR00286##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1094] R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00287## [1095] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1096] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1097] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1098] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1099] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1100] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1101] and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    [1102] The embodiments of the present invention include compounds having formula (VIf):

    ##STR00288##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1103] Q.sup.1 is 1 or 2; [1104] and Q.sup.2 is 1 or 2.

    [1105] The embodiments of the present invention include compounds having formula (VIg):

    ##STR00289##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1106] Q.sup.1 is 1 or 2; [1107] and Q.sup.2 is 1 or 2.

    [1108] The embodiments of the present invention include compounds having formula (VIh):

    ##STR00290##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [1109] Q.sup.1 is 1 or 2; [1110] and Q.sup.2 is 1 or 2.

    [1111] The embodiments of the present invention include compounds having formula (VIh-1):

    ##STR00291##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1112] Q.sup.1 is 1 or 2; [1113] and Q.sup.2 is 1 or 2.

    [1114] The embodiments of the present invention include compounds having formula (VIh-2):

    ##STR00292##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1115] Q.sup.1 is 1 or 2; [1116] and Q.sup.2 is 1 or 2.

    [1117] The embodiments of the present invention include compounds having formula (VIh-3):

    ##STR00293##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1118] Q.sup.1 is 1 or 2; [1119] and Q.sup.2 is 1 or 2.

    [1120] The embodiments of the present invention include compounds having formula (VIh-):

    ##STR00294##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1121] Q.sup.1 is 1 or 2; [1122] and Q.sup.2 is 1 or 2.

    [1123] The embodiments of the present invention include compounds having formula (VIh-5):

    ##STR00295##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1124] Q.sup.1 is 1 or 2; [1125] and Q.sup.2 is 1 or 2.

    [1126] The embodiments of the present invention include compounds having formula (VIi):

    ##STR00296##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1127] R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00297## [1128] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1129] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1130] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1131] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1132] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1133] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1134] and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are hydrogen.

    [1135] The embodiments of the present invention include compounds having formula (VIj):

    ##STR00298##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1136] Q.sup.1 is 1 or 2; [1137] and Q.sup.2 is 1 or 2.

    [1138] The embodiments of the present invention include compounds having formula (VIk):

    ##STR00299##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1139] Q.sup.1 is 1 or 2; [1140] and Q.sup.2 is 1 or 2.

    [1141] The embodiments of the present invention include compounds having formula (VIL):

    ##STR00300##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1142] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [1143] Q.sup.1 is 1 or 2; [1144] and Q.sup.2 is 1 or 2.

    [1145] The embodiments of the present invention include compounds having formula (VIL-1):

    ##STR00301##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1146] Q.sup.1 is 1 or 2; [1147] and Q.sup.2 is 1 or 2.

    [1148] The embodiments of the present invention include compounds having formula (VIL-2):

    ##STR00302##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1149] Q.sup.1 is 1 or 2; [1150] and Q.sup.2 is 1 or 2.

    [1151] The embodiments of the present invention include compounds having formula (VIL-3):

    ##STR00303##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1152] Q.sup.1 is 1 or 2; [1153] and Q.sup.2 is 1 or 2.

    [1154] The embodiments of the present invention include compounds having formula (VIL-4):

    ##STR00304##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1155] Q.sup.1 is 1 or 2; [1156] and Q.sup.2 is 1 or 2.

    [1157] The embodiments of the present invention include compounds having formula (VIL-5):

    ##STR00305##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1158] Q.sup.1 is 1 or 2; [1159] and Q.sup.2 is 1 or 2.

    [1160] The embodiments of the present invention include compounds having formula (VIm):

    ##STR00306##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1161] R.sup.20a, R.sup.20b, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00307## [1162] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1163] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1164] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1165] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1166] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1167] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1168] and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    [1169] The embodiments of the present invention include compounds having formula (VIn):

    ##STR00308##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1170] Q.sup.1 is 1 or 2; [1171] and Q.sup.2 is 1 or 2.

    [1172] The embodiments of the present invention include compounds having formula (VIo):

    ##STR00309##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1173] Q.sup.1 is 1 or 2; [1174] and Q.sup.2 is 1 or 2.

    [1175] The embodiments of the present invention include compounds having formula (VIp):

    ##STR00310##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1176] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [1177] Q.sup.1 is 1 or 2; [1178] and Q.sup.2 is 1 or 2.

    [1179] The embodiments of the present invention include compounds having formula (VIp-1):

    ##STR00311##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1180] Q.sup.1 is 1 or 2; [1181] and Q.sup.2 is 1 or 2.

    [1182] The embodiments of the present invention include compounds having formula (VIp-2):

    ##STR00312##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1183] Q.sup.1 is 1 or 2; [1184] and Q.sup.2 is 1 or 2.

    [1185] The embodiments of the present invention include compounds having formula (VIp-3):

    ##STR00313##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1186] Q.sup.1 is 1 or 2; [1187] and Q.sup.2 is 1 or 2.

    [1188] The embodiments of the present invention include compounds having formula (VIp-4):

    ##STR00314##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1189] Q.sup.1 is 1 or 2; [1190] and Q.sup.2 is 1 or 2.

    [1191] The embodiments of the present invention include compounds having formula (VIp-5):

    ##STR00315##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1192] Q.sup.1 is 1 or 2; [1193] and Q.sup.2 is 1 or 2.

    [1194] The embodiments of the present invention include compounds having formula (VIq):

    ##STR00316##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1195] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00317## [1196] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1197] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1198] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1199] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1200] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1201] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1202] and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    [1203] The embodiments of the present invention include compounds having formula (VIr):

    ##STR00318##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1204] Q.sup.1 is 1 or 2; [1205] and Q.sup.2 is 1 or 2.

    [1206] The embodiments of the present invention include compounds having formula (VIs):

    ##STR00319##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1207] Q.sup.1 is 1 or 2; [1208] and Q.sup.2 is 1 or 2.

    [1209] The embodiments of the present invention include compounds having formula (VIt):

    ##STR00320##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1210] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [1211] Q.sup.1 is 1 or 2; [1212] and Q.sup.2 is 1 or 2.

    [1213] The embodiments of the present invention include compounds having formula (VIt-1):

    ##STR00321##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1214] Q.sup.1 is 1 or 2; [1215] and Q.sup.2 is 1 or 2.

    [1216] The embodiments of the present invention include compounds having formula (VIt-2):

    ##STR00322##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1217] Q.sup.1 is 1 or 2; [1218] and Q.sup.2 is 1 or 2.

    [1219] The embodiments of the present invention include compounds having formula (VIt-3):

    ##STR00323##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1220] Q.sup.1 is 1 or 2; [1221] and Q.sup.2 is 1 or 2.

    [1222] The embodiments of the present invention include compounds having formula (VIt-4):

    ##STR00324##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1223] Q.sup.1 is 1 or 2; [1224] and Q.sup.2 is 1 or 2.

    [1225] The embodiments of the present invention include compounds having formula (VIt-5):

    ##STR00325##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1226] Q.sup.1 is 1 or 2; [1227] and Q.sup.2 is 1 or 2.

    [1228] The embodiments of the present invention include compounds having formula (VIu):

    ##STR00326##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1229] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00327## [1230] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1231] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1232] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1233] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1234] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1235] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1236] and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    [1237] The embodiments of the present invention include compounds having formula (VIv):

    ##STR00328##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1238] Q.sup.1 is 1 or 2; [1239] and Q.sup.2 is 1 or 2.

    [1240] The embodiments of the present invention include compounds having formula (VIw):

    ##STR00329##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1241] Q.sup.1 is 1 or 2; [1242] and Q.sup.2 is 1 or 2.

    [1243] The embodiments of the present invention include compounds having formula (VIx):

    ##STR00330##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1244] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [1245] Q.sup.1 is 1 or 2; [1246] and Q.sup.2 is 1 or 2.

    [1247] The embodiments of the present invention include compounds having formula (VIx-1):

    ##STR00331##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1248] Q.sup.1 is 1 or 2; [1249] and Q.sup.2 is 1 or 2.

    [1250] The embodiments of the present invention include compounds having formula (VIx-2):

    ##STR00332##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1251] Q.sup.1 is 1 or 2; [1252] and Q.sup.2 is 1 or 2.

    [1253] The embodiments of the present invention include compounds having formula (VIx-3):

    ##STR00333##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1254] Q.sup.1 is 1 or 2; [1255] and Q.sup.2 is 1 or 2.

    [1256] The embodiments of the present invention include compounds having formula (VIx-4):

    ##STR00334##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1257] Q.sup.1 is 1 or 2; [1258] and Q.sup.2 is 1 or 2.

    [1259] The embodiments of the present invention include compounds having formula (VIx-5):

    ##STR00335##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1260] Q.sup.1 is 1 or 2; [1261] and Q.sup.2 is 1 or 2.

    [1262] The embodiments of the present invention include compounds having formula (VII):

    ##STR00336##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof

    [1263] The embodiments of the present invention include compounds having formula (VIIa):

    ##STR00337##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1264] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00338## [1265] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1266] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1267] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1268] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1269] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1270] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1271] and at least 3 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, and R.sup.20e are hydrogen.

    [1272] The embodiments of the present invention include compounds having formula (VIIb):

    ##STR00339##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1273] Q.sup.1 is 1 or 2; [1274] and Q.sup.2 is 1 or 2.

    [1275] The embodiments of the present invention include compounds having formula (VIIc):

    ##STR00340##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1276] Q.sup.1 is 1 or 2; [1277] and Q.sup.2 is 1 or 2.

    [1278] The embodiments of the present invention include compounds having formula (VIId):

    ##STR00341##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1279] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [1280] Q.sup.1 is 1 or 2; [1281] and Q.sup.2 is 1 or 2.

    [1282] The embodiments of the present invention include compounds having formula (VIId-1):

    ##STR00342##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1283] Q.sup.1 is 1 or 2; [1284] and Q.sup.2 is 1 or 2.

    [1285] The embodiments of the present invention include compounds having formula (VIId-2):

    ##STR00343##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1286] Q.sup.1 is 1 or 2; [1287] and Q.sup.2 is 1 or 2.

    [1288] The embodiments of the present invention include compounds having formula (VIId-3):

    ##STR00344##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1289] Q.sup.1 is 1 or 2; [1290] and Q.sup.2 is 1 or 2.

    [1291] The embodiments of the present invention include compounds having formula (VIId-4):

    ##STR00345##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1292] Q.sup.1 is 1 or 2; [1293] and Q.sup.2 is 1 or 2.

    [1294] The embodiments of the present invention include compounds having formula (VIId-5):

    ##STR00346##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1295] Q.sup.1 is 1 or 2; [1296] and Q.sup.2 is 1 or 2.

    [1297] The embodiments of the present invention include compounds having formula (VIIe):

    ##STR00347##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1298] R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7 cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00348## [1299] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1300] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1301] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1302] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1303] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1304] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1305] and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    [1306] The embodiments of the present invention include compounds having formula (VIIf):

    ##STR00349##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1307] Q.sup.1 is 1 or 2; [1308] and Q.sup.2 is 1 or 2.

    [1309] The embodiments of the present invention include compounds having formula (VIIg):

    ##STR00350##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1310] Q.sup.1 is 1 or 2; [1311] and Q.sup.2 is 1 or 2.

    [1312] The embodiments of the present invention include compounds having formula (VIIh):

    ##STR00351##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1313] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [1314] Q.sup.1 is 1 or 2; [1315] and Q.sup.2 is 1 or 2.

    [1316] The embodiments of the present invention include compounds having formula (VIIh-1):

    ##STR00352##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1317] Q.sup.1 is 1 or 2; [1318] and Q.sup.2 is 1 or 2.

    [1319] The embodiments of the present invention include compounds having formula (VIIh-2):

    ##STR00353##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1320] Q.sup.1 is 1 or 2; [1321] and Q.sup.2 is 1 or 2.

    [1322] The embodiments of the present invention include compounds having formula (VIIh-3):

    ##STR00354##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1323] Q.sup.1 is 1 or 2; [1324] and Q.sup.2 is 1 or 2.

    [1325] The embodiments of the present invention include compounds having formula (VIIh-4):

    ##STR00355##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1326] Q.sup.1 is 1 or 2; [1327] and Q.sup.2 is 1 or 2.

    [1328] The embodiments of the present invention include compounds having formula (VIIh-5):

    ##STR00356##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1329] Q.sup.1 is 1 or 2; [1330] and Q.sup.2 is 1 or 2.

    [1331] The embodiments of the present invention include compounds having formula (VIII):

    ##STR00357##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1332] R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00358## [1333] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1334] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1335] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1336] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1337] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1338] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1339] and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20e are hydrogen.

    [1340] The embodiments of the present invention include compounds having formula (VIIj):

    ##STR00359##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1341] Q.sup.1 is 1 or 2; [1342] and Q.sup.2 is 1 or 2.

    [1343] The embodiments of the present invention include compounds having formula (VIIk):

    ##STR00360##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1344] Q.sup.1 is 1 or 2; [1345] and Q.sup.2 is 1 or 2.

    [1346] The embodiments of the present invention include compounds having formula (VIIL):

    ##STR00361##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1347] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [1348] Q.sup.1 is 1 or 2; [1349] and Q.sup.2 is 1 or 2.

    [1350] The embodiments of the present invention include compounds having formula (VIIL-1):

    ##STR00362##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1351] Q.sup.1 is 1 or 2; [1352] and Q.sup.2 is 1 or 2.

    [1353] The embodiments of the present invention include compounds having formula (VIIL-2):

    ##STR00363##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1354] Q.sup.1 is 1 or 2; [1355] and Q.sup.2 is 1 or 2.

    [1356] The embodiments of the present invention include compounds having formula (VIIL-3):

    ##STR00364##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1357] Q.sup.1 is 1 or 2; [1358] and Q.sup.2 is 1 or 2.

    [1359] The embodiments of the present invention include compounds having formula (VIIL-4):

    ##STR00365##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1360] Q.sup.1 is 1 or 2; [1361] and Q.sup.2 is 1 or 2.

    [1362] The embodiments of the present invention include compounds having formula (VIIL-5):

    ##STR00366##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1363] Q.sup.1 is 1 or 2; [1364] and Q.sup.2 is 1 or 2.

    [1365] The embodiments of the present invention include compounds having formula (VIIm):

    ##STR00367##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1366] R.sup.20a, R.sup.20b, R.sup.20d, and R.sup.20e are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00368## [1367] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1368] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1369] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1370] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1371] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1372] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1373] and at least 2 of R.sup.20a, R.sup.20b, R.sup.20c, and R.sup.20d are hydrogen.

    [1374] The embodiments of the present invention include compounds having formula (VIIn):

    ##STR00369##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1375] Q.sup.1 is 1 or 2; [1376] and Q.sup.2 is 1 or 2.

    [1377] The embodiments of the present invention include compounds having formula (VIIo):

    ##STR00370##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1378] Q.sup.1 is 1 or 2; [1379] and Q.sup.2 is 1 or 2.

    [1380] The embodiments of the present invention include compounds having formula (VIIp):

    ##STR00371##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1381] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [1382] Q.sup.1 is 1 or 2; [1383] and Q.sup.2 is 1 or 2.

    [1384] The embodiments of the present invention include compounds having formula (VIIp-1):

    ##STR00372##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1385] Q.sup.1 is 1 or 2; [1386] and Q.sup.2 is 1 or 2.

    [1387] The embodiments of the present invention include compounds having formula (VIIp-2):

    ##STR00373##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1388] Q.sup.1 is 1 or 2; [1389] and Q.sup.2 is 1 or 2.

    [1390] The embodiments of the present invention include compounds having formula (VIIp-3):

    ##STR00374##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1391] Q.sup.1 is 1 or 2; [1392] and Q.sup.2 is 1 or 2.

    [1393] The embodiments of the present invention include compounds having formula (VIIp-4):

    ##STR00375##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1394] Q.sup.1 is 1 or 2; [1395] and Q.sup.2 is 1 or 2.

    [1396] The embodiments of the present invention include compounds having formula (VIIp-5):

    ##STR00376##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1397] Q.sup.1 is 1 or 2; [1398] and Q.sup.2 is 1 or 2.

    [1399] The embodiments of the present invention include compounds having formula (VIIq):

    ##STR00377##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1400] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7cycloalkyl, SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23b, NHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00378## [1401] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1402] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1403] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1404] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1405] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1406] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1407] and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    [1408] The embodiments of the present invention include compounds having formula (VIIr):

    ##STR00379##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1409] Q.sup.1 is 1 or 2; [1410] and Q.sup.2 is 1 or 2.

    [1411] The embodiments of the present invention include compounds having formula (VIIs):

    ##STR00380##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1412] Q.sup.1 is 1 or 2; [1413] and Q.sup.2 is 1 or 2.

    [1414] The embodiments of the present invention include compounds having formula (VIIt):

    ##STR00381##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [1415] Q.sup.1 is 1 or 2; [1416] and Q.sup.2 is 1 or 2.

    [1417] The embodiments of the present invention include compounds having formula (VIIt-1):

    ##STR00382##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1418] Q.sup.1 is 1 or 2; [1419] and Q.sup.2 is 1 or 2.

    [1420] The embodiments of the present invention include compounds having formula (VIIt-2):

    ##STR00383##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1421] Q.sup.1 is 1 or 2; [1422] and Q.sup.2 is 1 or 2.

    [1423] The embodiments of the present invention include compounds having formula (VIIt-3):

    ##STR00384##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1424] Q.sup.1 is 1 or 2; [1425] and Q.sup.2 is 1 or 2.

    [1426] The embodiments of the present invention include compounds having formula (VIIt-4):

    ##STR00385##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1427] Q.sup.1 is 1 or 2; [1428] and Q.sup.2 is 1 or 2.

    [1429] The embodiments of the present invention include compounds having formula (VIIt-5):

    ##STR00386##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1430] Q.sup.1 is 1 or 2; [1431] and Q.sup.2 is 1 or 2.

    [1432] The embodiments of the present invention include compounds having formula (VIIu):

    ##STR00387##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1433] R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are independently selected from the group consisting of hydrogen, —CN, —NO.sub.2, —OH, halogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, C.sub.3-7 cycloalkyl, C.sub.1-6 linear alkoxy, C.sub.3-7 branched alkoxy, C.sub.3-7 cycloalkoxy, C.sub.1-6 linear haloalkyl, C.sub.3-7 branched haloalkyl, C.sub.1-6 linear haloalkoxy, C.sub.3-7 branched haloalkoxy, SH, SC.sub.1-6 linear alkyl, SC.sub.3-7 branched alkyl, SC.sub.3-7cycloalkyl, SO.sub.2C.sub.1-6 linear alkyl, SO.sub.2C.sub.3-7 branched alkyl, SO.sub.2C.sub.3-7 cycloalkyl SO.sub.2NH.sub.2, SO.sub.2NHR.sup.21, NHSO.sub.2R.sup.22, —NR.sup.23aR.sup.23bNHC(O)R.sup.24, C(O)NHR.sup.24, C(O)N(R.sup.24).sub.2, morpholino, and

    ##STR00388## [1434] R.sup.21 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1435] R.sup.22 at each occurrence is independently selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1436] R.sup.23a at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1437] R.sup.23b at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1438] R.sup.24 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1439] R.sup.25 at each occurrence is independently is selected from the group consisting of hydrogen, C.sub.1-6 linear alkyl, C.sub.3-7 branched alkyl, and C.sub.3-7 cycloalkyl; [1440] and at least 5 of R.sup.20a, R.sup.20b, R.sup.20c, R.sup.20d, R.sup.20e, R.sup.20f, and R.sup.20g are hydrogen.

    [1441] The embodiments of the present invention include compounds having formula (VIIv):

    ##STR00389##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1442] Q.sup.1 is 1 or 2; [1443] and Q.sup.2 is 1 or 2.

    [1444] The embodiments of the present invention include compounds having formula (VIIw):

    ##STR00390##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1445] Q.sup.1 is 1 or 2; [1446] and Q.sup.2 is 1 or 2.

    [1447] The embodiments of the present invention include compounds having formula (VIIx):

    ##STR00391##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1448] X.sup.1 is selected from the group consisting of O, S, SO, SO.sub.2, and NR.sup.7; [1449] Q.sup.1 is 1 or 2; [1450] and Q.sup.2 is 1 or 2.

    [1451] The embodiments of the present invention include compounds having formula (VIIx-1):

    ##STR00392##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1452] Q.sup.1 is 1 or 2; [1453] and Q.sup.2 is 1 or 2.

    [1454] The embodiments of the present invention include compounds having formula (VIIx-2):

    ##STR00393##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1455] Q.sup.1 is 1 or 2; [1456] and Q.sup.2 is 1 or 2.

    [1457] The embodiments of the present invention include compounds having formula (VIIx-3):

    ##STR00394##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1458] Q.sup.1 is 1 or 2; [1459] and Q.sup.2 is 1 or 2.

    [1460] The embodiments of the present invention include compounds having formula (VIIx-4):

    ##STR00395##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1461] Q.sup.1 is 1 or 2; [1462] and Q.sup.2 is 1 or 2.

    [1463] The embodiments of the present invention include compounds having formula (VIIx-5):

    ##STR00396##

    Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein [1464] Q.sup.1 is 1 or 2; [1465] and Q.sup.2 is 1 or 2.

    [1466] In some embodiments A is

    ##STR00397##

    [1467] In some embodiments A is

    ##STR00398##

    [1468] In some embodiments A is

    ##STR00399##

    [1469] In some embodiments R.sup.1 is hydrogen.

    [1470] In some embodiments R.sup.1 is C.sub.1-6 linear alkyl.

    [1471] In some embodiments R.sup.1 is C.sub.3-7 branched alkyl.

    [1472] In some embodiments R.sup.2 is hydrogen.

    [1473] In some embodiments R.sup.2 is C.sub.1-6 linear alkyl.

    [1474] In some embodiments R.sup.2 is C.sub.3-7 branched alkyl.

    [1475] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 5 ring atoms.

    [1476] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 5 ring atoms and containing a double bond.

    [1477] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 6 ring atoms.

    [1478] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 6 ring atoms and containing a double bond.

    [1479] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 7 ring atoms.

    [1480] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 7 ring atoms and containing a double bond.

    [1481] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 6 ring atoms containing one of which is O.

    [1482] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 7 ring atoms containing one of which is O.

    [1483] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 8 ring atoms containing one of which is O.

    [1484] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 6 ring atoms containing one of which is S.

    [1485] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 7 ring atoms containing one of which is S.

    [1486] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 8 ring atoms containing one of which is S.

    [1487] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 6 ring atoms containing one of which is SO.

    [1488] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 7 ring atoms containing one of which is SO.

    [1489] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 8 ring atoms containing one of which is SO.

    [1490] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 6 ring atoms containing one of which is SO.sub.2.

    [1491] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 7 ring atoms containing one of which is SO.sub.2.

    [1492] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 8 ring atoms containing one of which is SO.sub.2.

    [1493] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 6 ring atoms containing one of which is NR.sup.7.

    [1494] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 7 ring atoms containing one of which is NR.sup.7.

    [1495] In some embodiments R.sup.1 and R.sup.2 are taken together with the atoms to which they are bound to form a ring having 8 ring atoms containing one of which is NR.sup.7.

    [1496] In some embodiments R.sup.3 is optionally substituted phenyl.

    [1497] In some embodiments R.sup.3 is optionally substituted naphthylen-1-yl.

    [1498] In some embodiments R.sup.3 is optionally substituted naphthylen-2-yl.

    [1499] In some embodiments R.sup.3 is optionally substituted 2-pyridyl

    [1500] In some embodiments R.sup.3 is optionally substituted 3-pyridyl.

    [1501] In some embodiments R.sup.3 is optionally substituted 4-pyridyl.

    [1502] In some embodiments R.sup.3 is

    ##STR00400##

    [1503] In some embodiments R.sup.4 is optionally substituted phenyl.

    [1504] In some embodiments R.sup.4 is optionally substituted naphthylen-1-yl.

    [1505] In some embodiments R.sup.4 is optionally substituted naphthylen-2-yl.

    [1506] In some embodiments R.sup.4 is optionally substituted 2-pyridyl

    [1507] In some embodiments R.sup.4 is optionally substituted 3-pyridyl.

    [1508] In some embodiments R.sup.4 is optionally substituted 4-pyridyl.

    [1509] In some embodiments R.sup.4 is

    ##STR00401##

    [1510] In some embodiments R.sup.5 is optionally substituted phenyl.

    [1511] In some embodiments R.sup.5 is optionally substituted naphthylen-1-yl.

    [1512] In some embodiments R.sup.5 is optionally substituted naphthylen-2-yl.

    [1513] In some embodiments R.sup.5 is optionally substituted 2-pyridyl

    [1514] In some embodiments R.sup.5 is optionally substituted 3-pyridyl.

    [1515] In some embodiments R.sup.5 is optionally substituted 4-pyridyl.

    [1516] In some embodiments R.sup.5 is

    ##STR00402##

    [1517] In some embodiments R6 is optionally substituted phenyl.

    [1518] In some embodiments R.sup.6 is optionally substituted naphthylen-1-yl.

    [1519] In some embodiments R.sup.6 is optionally substituted naphthylen-2-yl.

    [1520] In some embodiments R.sup.6 is optionally substituted 2-pyridyl

    [1521] In some embodiments R.sup.6 is optionally substituted 3-pyridyl.

    [1522] In some embodiments R.sup.6 is optionally substituted 4-pyridyl.

    [1523] In some embodiments R.sup.7 is H.

    [1524] In some embodiments R.sup.7 is C.sub.1-6 linear alkyl.

    [1525] In some embodiments R.sup.7 is C.sub.3-7 branched alkyl.

    [1526] In some embodiments R.sup.7 is C.sub.3-7 cycloalkyl.

    [1527] In some embodiments R.sup.7 is optionally substituted phenyl.

    [1528] In some embodiments R.sup.7 is optionally substituted benzyl.

    [1529] In some embodiments R.sup.7 is COR.sup.8.

    [1530] In some embodiments R.sup.7 is CO.sub.2R.sup.9.

    [1531] In some embodiments R.sup.7 is CONR.sup.10aR.sup.10b.

    [1532] In some embodiments R.sup.7 is SO.sub.2NR.sup.10aR.sup.10b.

    [1533] In some embodiments R.sup.7 is SO.sub.2R.sup.10c.

    [1534] In some embodiments R.sup.8 is selected H.

    [1535] In some embodiments R.sup.8 is C.sub.1-6 linear alkyl.

    [1536] In some embodiments R.sup.8 is C.sub.3-7 branched alkyl

    [1537] In some embodiments R.sup.8 is C.sub.3-7 cycloalkyl.

    [1538] In some embodiments R.sup.9 is C.sub.1-6 linear alkyl.

    [1539] In some embodiments R.sup.9 is C.sub.3-7 branched alkyl.

    [1540] In some embodiments R.sup.9 is C.sub.3-7 cycloalkyl.

    [1541] In some embodiments R.sup.10a is H.

    [1542] In some embodiments R.sup.10a is C.sub.1-6 linear alkyl.

    [1543] In some embodiments R.sup.10a is C.sub.3-7 branched alkyl.

    [1544] In some embodiments R.sup.10a is C.sub.3-7 cycloalkyl.

    [1545] In some embodiments R.sup.10b is H.

    [1546] In some embodiments R.sup.10b is C.sub.1-6 linear alkyl.

    [1547] In some embodiments R.sup.10b is C.sub.3-7 branched alkyl.

    [1548] In some embodiments R.sup.10b is C.sub.3-7 cycloalkyl.

    [1549] In some embodiments R.sup.10c is C.sub.1-6 linear alkyl.

    [1550] In some embodiments R.sup.10c is C.sub.3-7 branched alkyl.

    [1551] In some embodiments R.sup.10c is C.sub.3-7 cycloalkyl.

    [1552] In some embodiments R.sup.10c is C.sub.1-6 linear haloalkyl.

    [1553] In some embodiments R.sup.10c is C.sub.3-7 branched haloalkyl.

    [1554] In some embodiments R.sup.10c is —(CH.sub.2).sub.qCN.

    [1555] In some embodiments R.sup.10c is —(CH.sub.2).sub.qSO.sub.2R.sup.11.

    [1556] In some embodiments R.sup.10c is —(CH.sub.2).sub.qOR.sup.12.

    [1557] In some embodiments R.sup.10c s

    ##STR00403##

    [1558] In some embodiments R.sup.10c s

    ##STR00404##

    [1559] In some embodiments R.sup.10c s

    ##STR00405##

    [1560] In some embodiments R.sup.10c s

    ##STR00406##

    [1561] In some embodiments R.sup.10c s

    ##STR00407##

    [1562] In some embodiments R.sup.10c is

    ##STR00408##

    [1563] In some embodiments R.sup.10c s

    ##STR00409##

    [1564] In some embodiments R.sup.10c is

    ##STR00410##

    [1565] In some embodiments R.sup.10c s

    ##STR00411##

    [1566] In some embodiments R.sup.10c s

    ##STR00412##

    [1567] In some embodiments R.sup.10c is

    ##STR00413##

    [1568] In some embodiments R.sup.10c is

    ##STR00414##

    [1569] In some embodiments R.sup.11 C.sub.1-6 linear alkyl.

    [1570] In some embodiments R.sup.11 C.sub.3-7 branched alkyl.

    [1571] In some embodiments R.sup.11 C.sub.3-7 cycloalkyl.

    [1572] In some embodiments R.sup.12 is C.sub.1-6 linear alkyl.

    [1573] In some embodiments R.sup.12 is C.sub.3-7 branched alkyl.

    [1574] In some embodiments R.sup.12 is C.sub.3-7 cycloalkyl.

    [1575] In some embodiments R.sup.1a is H.

    [1576] In some embodiments R.sup.1a is OH

    [1577] In some embodiments R.sup.1a is NO.sub.2.

    [1578] In some embodiments R.sup.1a is halogen.

    [1579] In some embodiments R.sup.1a is CN.

    [1580] In some embodiments R.sup.1a is C.sub.1-6 linear alkyl.

    [1581] In some embodiments R.sup.1a is C.sub.3-7 branched alkyl.

    [1582] In some embodiments R.sup.1a is C.sub.3-7 cycloalkyl.

    [1583] In some embodiments R.sup.1a is C.sub.1-6 linear alkoxy.

    [1584] In some embodiments R.sup.1a is C.sub.3-7 branched alkoxy.

    [1585] In some embodiments R.sup.1a is C.sub.3-7 cycloalkoxy.

    [1586] In some embodiments R.sup.1a is C.sub.1-6 linear haloalkyl.

    [1587] In some embodiments R.sup.1a is C.sub.3-7 branched haloalkyl.

    [1588] In some embodiments R.sup.1a is C.sub.1-6 linear haloalkoxy.

    [1589] In some embodiments R.sup.1a is —S(C.sub.1-6 linear alkyl).

    [1590] In some embodiments R.sup.1a is S(C.sub.3-7 branched alkyl).

    [1591] In some embodiments R.sup.1a is —S(C.sub.3-7 cycloalkyl).

    [1592] In some embodiments R.sup.1a is COR.sup.13.

    [1593] In some embodiments R.sup.1a is CO.sub.2R.sup.14.

    [1594] In some embodiments R.sup.1a is CONR.sup.15aR.sup.15b.

    [1595] In some embodiments R.sup.1a is SO.sub.2NR.sup.15aR.sup.15b.

    [1596] In some embodiments R.sup.1a is NR.sup.16aR.sup.16b.

    [1597] In some embodiments R.sup.1a is NR.sup.16aCOR.sup.17.

    [1598] In some embodiments R.sup.1a is NR.sup.16aSO.sub.2R.sup.18.

    [1599] In some embodiments R.sup.1a is NR.sup.16aSO.sub.2NR.sup.19aR.sup.19b.

    [1600] In some embodiments R.sup.1b is H.

    [1601] In some embodiments R.sup.1b is OH

    [1602] In some embodiments R.sup.1b is NO.sub.2.

    [1603] In some embodiments R.sup.1b is halogen.

    [1604] In some embodiments R.sup.1b is CN.

    [1605] In some embodiments R.sup.1b is C.sub.1-6 linear alkyl.

    [1606] In some embodiments R.sup.1b is C.sub.3-7 branched alkyl.

    [1607] In some embodiments R.sup.1b is C.sub.3-7 cycloalkyl.

    [1608] In some embodiments R.sup.1b is C.sub.1-6 linear alkoxy.

    [1609] In some embodiments R.sup.1b is C.sub.3-7 branched alkoxy.

    [1610] In some embodiments R.sup.1b is C.sub.3-7 cycloalkoxy.

    [1611] In some embodiments R.sup.1b is C.sub.1-6 linear haloalkyl.

    [1612] In some embodiments R.sup.1b is C.sub.3-7 branched haloalkyl.

    [1613] In some embodiments R.sup.1b is C.sub.1-6 linear haloalkoxy.

    [1614] In some embodiments R.sup.1b is —S(C.sub.1-6 linear alkyl).

    [1615] In some embodiments R.sup.1b is S(C.sub.3-7 branched alkyl).

    [1616] In some embodiments R.sup.1b is —S(C.sub.3-7 cycloalkyl).

    [1617] In some embodiments R.sup.1b is COR.sup.13.

    [1618] In some embodiments R.sup.1b is CO.sub.2R.sup.14.

    [1619] In some embodiments R.sup.1b is CONR.sup.15aR.sup.15b.

    [1620] In some embodiments R.sup.1b is SO.sub.2NR.sup.15aR.sup.15b.

    [1621] In some embodiments R.sup.1b is NR.sup.16aR.sup.16b.

    [1622] In some embodiments R.sup.1b is NR.sup.16aCOR.sup.17.

    [1623] In some embodiments R.sup.1b is NR.sup.16aSO.sub.2R.sup.18.

    [1624] In some embodiments R.sup.1b is NR.sup.16aSO.sub.2NR.sup.19aR.sup.19b.

    [1625] In some embodiments R.sup.1c is H.

    [1626] In some embodiments R.sup.1c is OH

    [1627] In some embodiments R.sup.1c is NO.sub.2.

    [1628] In some embodiments R.sup.1c is halogen.

    [1629] In some embodiments R.sup.1c is CN.

    [1630] In some embodiments R.sup.1c is C.sub.1-6 linear alkyl.

    [1631] In some embodiments R.sup.1c is C.sub.3-7 branched alkyl.

    [1632] In some embodiments R.sup.1c is C.sub.3-7 cycloalkyl.

    [1633] In some embodiments R.sup.1c is C.sub.1-6 linear alkoxy.

    [1634] In some embodiments R.sup.1c is C.sub.3-7 branched alkoxy.

    [1635] In some embodiments R.sup.1c is C.sub.3-7 cycloalkoxy.

    [1636] In some embodiments R.sup.1c is C.sub.1-6 linear haloalkyl.

    [1637] In some embodiments R.sup.1c is C.sub.3-7 branched haloalkyl.

    [1638] In some embodiments R.sup.1c is C.sub.1-6 linear haloalkoxy.

    [1639] In some embodiments R.sup.1c is —S(C.sub.1-6 linear alkyl).

    [1640] In some embodiments R.sup.1c is S(C.sub.3-7 branched alkyl).

    [1641] In some embodiments R.sup.1c is —S(C.sub.3-7 cycloalkyl).

    [1642] In some embodiments R.sup.1c is COR.sup.13.

    [1643] In some embodiments R.sup.1c is CO.sub.2R.sup.14.

    [1644] In some embodiments R.sup.1c is CONR.sup.15aR.sup.15b.

    [1645] In some embodiments R.sup.1c is SO.sub.2NR.sup.15aR.sup.15b.

    [1646] In some embodiments R.sup.1c is NR.sup.16aR.sup.16b.

    [1647] In some embodiments R.sup.1c is NR.sup.16aCOR.sup.17.

    [1648] In some embodiments R.sup.1c is NR.sup.16aSO.sub.2R.sup.18.

    [1649] In some embodiments R.sup.1c is NR.sup.16aSO.sub.2NR.sup.19aR.sup.19b.

    [1650] In some embodiments R.sup.id is H.

    [1651] In some embodiments R.sup.1d is OH

    [1652] In some embodiments R.sup.1d is NO.sub.2.

    [1653] In some embodiments R.sup.1d is halogen.

    [1654] In some embodiments R.sup.1d is CN.

    [1655] In some embodiments R.sup.1d is C.sub.1-6 linear alkyl.

    [1656] In some embodiments R.sup.1d is C.sub.3-7 branched alkyl.

    [1657] In some embodiments R.sup.1d is C.sub.3-7 cycloalkyl.

    [1658] In some embodiments R.sup.1d is C.sub.1-6 linear alkoxy.

    [1659] In some embodiments R.sup.1d is C.sub.3-7 branched alkoxy.

    [1660] In some embodiments R.sup.1d is C.sub.3-7 cycloalkoxy.

    [1661] In some embodiments R.sup.1d is C.sub.1-6 linear haloalkyl.

    [1662] In some embodiments R.sup.1d is C.sub.3-7 branched haloalkyl.

    [1663] In some embodiments R.sup.1d is C.sub.1-6 linear haloalkoxy.

    [1664] In some embodiments R.sup.1d is —S(C.sub.1-6 linear alkyl).

    [1665] In some embodiments R.sup.1d is S(C.sub.3-7 branched alkyl).

    [1666] In some embodiments R.sup.1d is —S(C.sub.3-7 cycloalkyl).

    [1667] In some embodiments R.sup.1d is COR.sup.13.

    [1668] In some embodiments R.sup.1d is CO.sub.2R.sup.14.

    [1669] In some embodiments R.sup.1d is CONR.sup.15aR.sup.15b.

    [1670] In some embodiments R.sup.1d is SO.sub.2NR.sup.15aR.sup.15b.

    [1671] In some embodiments R.sup.1d is NR.sup.16aR.sup.16b.

    [1672] In some embodiments R.sup.1d is NR.sup.16aCOR.sup.17.

    [1673] In some embodiments R.sup.1d is NR.sup.16aSO.sub.2R.sup.18.

    [1674] In some embodiments R.sup.1d is NR.sup.16aSO.sub.2NR.sup.19aR.sup.19b.

    [1675] In some embodiments R.sup.1e is H.

    [1676] In some embodiments R.sup.1e is OH

    [1677] In some embodiments R.sup.1e is NO.sub.2.

    [1678] In some embodiments R.sup.1e is halogen.

    [1679] In some embodiments R.sup.1e is CN.

    [1680] In some embodiments R.sup.1e is C.sub.1-6 linear alkyl.

    [1681] In some embodiments R.sup.1e is C.sub.3-7 branched alkyl.

    [1682] In some embodiments R.sup.1e is C.sub.3-7 cycloalkyl.

    [1683] In some embodiments R.sup.1e is C.sub.1-6 linear alkoxy.

    [1684] In some embodiments R.sup.1e is C.sub.3-7 branched alkoxy.

    [1685] In some embodiments R.sup.1e is C.sub.3-7 cycloalkoxy.

    [1686] In some embodiments R.sup.1e is C.sub.1-6 linear haloalkyl.

    [1687] In some embodiments R.sup.1e is C.sub.3-7 branched haloalkyl.

    [1688] In some embodiments R.sup.1e is C.sub.1-6 linear haloalkoxy.

    [1689] In some embodiments R.sup.1e is —S(C.sub.1-6 linear alkyl).

    [1690] In some embodiments R.sup.1e is S(C.sub.3-7 branched alkyl).

    [1691] In some embodiments R.sup.1e is —S(C.sub.3-7 cycloalkyl).

    [1692] In some embodiments R.sup.1e is COR.sup.13.

    [1693] In some embodiments R.sup.1e is CO.sub.2R.sup.14.

    [1694] In some embodiments R.sup.1e is CONR.sup.15aR.sup.15b.

    [1695] In some embodiments R.sup.1e is SO.sub.2NR.sup.15aR.sup.15b.

    [1696] In some embodiments R.sup.1e is NR.sup.16aR.sup.16b.

    [1697] In some embodiments R.sup.1e is NR.sup.16aCOR.sup.17.

    [1698] In some embodiments R.sup.1e is NR.sup.16aSO.sub.2R.sup.18.

    [1699] In some embodiments R.sup.1e is NR.sup.16aSO.sub.2NR.sup.19aR.sup.19b.

    [1700] In some embodiments R.sup.13 is H.

    [1701] In some embodiments R.sup.13 is C.sub.1-6 linear alkyl.

    [1702] In some embodiments R.sup.13 is C.sub.3-7 branched alkyl.

    [1703] In some embodiments R.sup.13 is C.sub.3-7 cycloalkyl.

    [1704] In some embodiments R.sup.14 is C.sub.1-6 linear alkyl.

    [1705] In some embodiments R.sup.14 is C.sub.3-7 branched alkyl.

    [1706] In some embodiments R.sup.14 is C.sub.3-7 cycloalkyl.

    [1707] In some embodiments R.sup.15a is H.

    [1708] In some embodiments R.sup.15a is C.sub.1-6 linear alkyl.

    [1709] In some embodiments R.sup.15a is C.sub.3-7 branched alkyl.

    [1710] In some embodiments R.sup.15a is C.sub.3-7 cycloalkyl.

    [1711] In some embodiments R.sup.15b is H.

    [1712] In some embodiments R.sup.15b is C.sub.1-6 linear alkyl.

    [1713] In some embodiments R.sup.15bis C.sub.3-7 branched alkyl.

    [1714] In some embodiments R.sup.15bis C.sub.3-7 cycloalkyl.

    [1715] In some embodiments R.sup.16a is H.

    [1716] In some embodiments R.sup.16a is C.sub.1-6 linear alkyl.

    [1717] In some embodiments R.sup.16a is C.sub.3-7 branched alkyl.

    [1718] In some embodiments R.sup.16a is C.sub.3-7 cycloalkyl.

    [1719] In some embodiments R.sup.16b is H.

    [1720] In some embodiments R.sup.16b is C.sub.1-6 linear alkyl.

    [1721] In some embodiments R.sup.16b is C.sub.3-7 branched alkyl.

    [1722] In some embodiments R.sup.16b is C.sub.3-7 cycloalkyl.

    [1723] In some embodiments R.sup.17 is H.

    [1724] In some embodiments R.sup.17 is C.sub.1-6 linear alkyl.

    [1725] In some embodiments R.sup.17 is C.sub.3-7 branched alkyl.

    [1726] In some embodiments R.sup.17 is C.sub.3-7 cycloalkyl.

    [1727] In some embodiments R.sup.18 is C.sub.1-6 linear alkyl.

    [1728] In some embodiments R.sup.18 is C.sub.3-7 branched alkyl.

    [1729] In some embodiments R.sup.18 is C.sub.3-7 cycloalkyl.

    [1730] In some embodiments R.sup.19a is C.sub.1-6 linear alkyl.

    [1731] In some embodiments R.sup.19a is C.sub.3-7 branched alkyl.

    [1732] In some embodiments R.sup.19a is C.sub.3-7 cycloalkyl.

    [1733] In some embodiments R.sup.19b is C.sub.1-6 linear alkyl.

    [1734] In some embodiments R.sup.19b is C.sub.3-7 branched alkyl.

    [1735] In some embodiments R.sup.19b is C.sub.3-7 cycloalkyl.

    [1736] In some embodiments n is 1.

    [1737] In some embodiments n is 2.

    [1738] In some embodiments n is 3.

    [1739] In some embodiments n is 4.

    [1740] In some embodiments m is 1.

    [1741] In some embodiments m is 2.

    [1742] In some embodiments m is 3.

    [1743] In some embodiments R.sup.20a is hydrogen.

    [1744] In some embodiments R.sup.20a is —CN.

    [1745] In some embodiments R.sup.20a is —NO.sub.2.

    [1746] In some embodiments R.sup.20a is —OH.

    [1747] In some embodiments R.sup.20a is halogen.

    [1748] In some embodiments R.sup.20a is C.sub.1-6 linear alkyl.

    [1749] In some embodiments R.sup.20a is C.sub.3-7 branched alkyl.

    [1750] In some embodiments R.sup.20a is C.sub.3-7 cycloalkyl.

    [1751] In some embodiments R.sup.20a is C.sub.1-6 linear alkoxy.

    [1752] In some embodiments R.sup.20a is C.sub.3-7 branched alkoxy.

    [1753] In some embodiments R.sup.20a is C.sub.3-7 cycloalkoxy.

    [1754] In some embodiments R.sup.20a is C.sub.1-6 linear haloalkyl.

    [1755] In some embodiments R.sup.20a is C.sub.3-7 branched haloalkyl.

    [1756] In some embodiments R.sup.20a is C.sub.1-6 linear haloalkoxy.

    [1757] In some embodiments R.sup.20a is C.sub.3-7 branched haloalkoxy.

    [1758] In some embodiments R.sup.20a is SH.

    [1759] In some embodiments R.sup.20a is SC.sub.1-6 linear alkyl.

    [1760] In some embodiments R.sup.20a is SC.sub.3-7 branched alkyl.

    [1761] In some embodiments R.sup.20a is SC.sub.3-7cycloalkyl.

    [1762] In some embodiments R.sup.20a is SO.sub.2C.sub.1-6 linear alkyl.

    [1763] In some embodiments R.sup.20a is SO.sub.2C.sub.3-7 branched alkyl.

    [1764] In some embodiments R.sup.20a is SO.sub.2C.sub.3-7cycloalkyl.

    [1765] In some embodiments R.sup.20a is SO.sub.2NH2.

    [1766] In some embodiments R.sup.20a is SO.sub.2NHR.sup.21.

    [1767] In some embodiments R.sup.20a is NHSO.sub.2R.sup.22.

    [1768] In some embodiments R.sup.20a is —NR.sup.23aR.sup.23b.

    [1769] In some embodiments R.sup.20a is NHC(O)R.sup.24.

    [1770] In some embodiments R.sup.20a is C(O)NHR.sup.24.

    [1771] In some embodiments R.sup.20a is C(O)N(R.sup.24).sub.2.

    [1772] In some embodiments R.sup.20a is morpholino.

    [1773] In some embodiments R.sup.20a is

    ##STR00415##

    [1774] In some embodiments R.sup.20b is hydrogen.

    [1775] In some embodiments R.sup.20b is —CN.

    [1776] In some embodiments R.sup.20b is —NO.sub.2.

    [1777] In some embodiments R.sup.20b is —OH.

    [1778] In some embodiments R.sup.20b is halogen.

    [1779] In some embodiments R.sup.20b is C.sub.1-6 linear alkyl.

    [1780] In some embodiments R.sup.20b is C.sub.3-7 branched alkyl.

    [1781] In some embodiments R.sup.20b is C.sub.3-7 cycloalkyl.

    [1782] In some embodiments R.sup.20b is C.sub.1-6 linear alkoxy.

    [1783] In some embodiments R.sup.20b is C.sub.3-7 branched alkoxy.

    [1784] In some embodiments R.sup.20b is C.sub.3-7 cycloalkoxy.

    [1785] In some embodiments R.sup.20b is C.sub.1-6 linear haloalkyl.

    [1786] In some embodiments R.sup.20b is C.sub.3-7 branched haloalkyl.

    [1787] In some embodiments R.sup.20b is C.sub.1-6 linear haloalkoxy.

    [1788] In some embodiments R.sup.20b is C.sub.3-7 branched haloalkoxy.

    [1789] In some embodiments R.sup.20b is SH.

    [1790] In some embodiments R.sup.20b is SC.sub.1-6 linear alkyl.

    [1791] In some embodiments R.sup.20b is SC.sub.3-7 branched alkyl.

    [1792] In some embodiments R.sup.20b is SC.sub.3-7cycloalkyl.

    [1793] In some embodiments R.sup.20b is SO.sub.2C.sub.1-6 linear alkyl.

    [1794] In some embodiments R.sup.20b is SO.sub.2C.sub.3-7 branched alkyl.

    [1795] In some embodiments R.sup.20b is SO.sub.2C.sub.3-7cycloalkyl.

    [1796] In some embodiments R.sup.20b is SO.sub.2NH.sub.2.

    [1797] In some embodiments R.sup.20b is SO.sub.2NHR.sup.21.

    [1798] In some embodiments R.sup.20b is NHSO.sub.2R.sup.22.

    [1799] In some embodiments R.sup.20b is —NR.sup.23aR.sup.23b.

    [1800] In some embodiments R.sup.20b is NHC(O)R.sup.24.

    [1801] In some embodiments R.sup.20b is C(O)NHR.sup.24.

    [1802] In some embodiments R.sup.20b is C(O)N(R.sup.24).sub.2.

    [1803] In some embodiments R.sup.20b is morpholino.

    [1804] In some embodiments R.sup.20b is

    ##STR00416##

    [1805] In some embodiments R.sup.20c is hydrogen.

    [1806] In some embodiments R.sup.20c is —CN.

    [1807] In some embodiments R.sup.20c is —NO.sub.2.

    [1808] In some embodiments R.sup.20c is —OH.

    [1809] In some embodiments R.sup.20c is halogen.

    [1810] In some embodiments R.sup.20c is C.sub.1-6 linear alkyl.

    [1811] In some embodiments R.sup.20c is C.sub.3-7 branched alkyl.

    [1812] In some embodiments R.sup.20c is C.sub.3-7 cycloalkyl.

    [1813] In some embodiments R.sup.20c is C.sub.1-6 linear alkoxy.

    [1814] In some embodiments R.sup.20c is C.sub.3-7 branched alkoxy.

    [1815] In some embodiments R.sup.20c is C.sub.3-7 cycloalkoxy.

    [1816] In some embodiments R.sup.20c is C.sub.1-6 linear haloalkyl.

    [1817] In some embodiments R.sup.20c is C.sub.3-7 branched haloalkyl.

    [1818] In some embodiments R.sup.20c is C.sub.1-6 linear haloalkoxy.

    [1819] In some embodiments R.sup.20c is C.sub.3-7 branched haloalkoxy.

    [1820] In some embodiments R.sup.20c is SH.

    [1821] In some embodiments R.sup.20c is SC.sub.1-6 linear alkyl.

    [1822] In some embodiments R.sup.20c is SC.sub.3-7 branched alkyl.

    [1823] In some embodiments R.sup.20c is SC.sub.3-7cycloalkyl.

    [1824] In some embodiments R.sup.20c is SO.sub.2C.sub.1-6 linear alkyl.

    [1825] In some embodiments R.sup.20c is SO.sub.2C.sub.3-7 branched alkyl.

    [1826] In some embodiments R.sup.20c is SO.sub.2C.sub.3-7cycloalkyl.

    [1827] In some embodiments R.sup.20c is SO.sub.2NH.sub.2.

    [1828] In some embodiments R.sup.20c is SO.sub.2NHR.sup.21.

    [1829] In some embodiments R.sup.20c is NHSO.sub.2R.sup.22.

    [1830] In some embodiments R.sup.20c is —NR.sup.23aR.sup.23b.

    [1831] In some embodiments R.sup.20c is NHC(O)R.sup.24.

    [1832] In some embodiments R.sup.20c is C(O)NHR.sup.24.

    [1833] In some embodiments R.sup.20c is C(O)N(R.sup.24).sub.2.

    [1834] In some embodiments R.sup.20c is morpholino.

    [1835] In some embodiments R.sup.20c is

    ##STR00417##

    [1836] In some embodiments R.sup.20d is hydrogen.

    [1837] In some embodiments R.sup.20d is —CN.

    [1838] In some embodiments R.sup.20d is —NO.sub.2.

    [1839] In some embodiments R.sup.20d is —OH.

    [1840] In some embodiments R.sup.20d is halogen.

    [1841] In some embodiments R.sup.20d is C.sub.1-6 linear alkyl.

    [1842] In some embodiments R.sup.20d is C.sub.3-7 branched alkyl.

    [1843] In some embodiments R.sup.20d is C.sub.3-7 cycloalkyl.

    [1844] In some embodiments R.sup.20d is C.sub.1-6 linear alkoxy.

    [1845] In some embodiments R.sup.20d is C.sub.3-7 branched alkoxy.

    [1846] In some embodiments R.sup.20d is C.sub.3-7 cycloalkoxy.

    [1847] In some embodiments R.sup.20d is C.sub.1-6 linear haloalkyl.

    [1848] In some embodiments R.sup.20d is C.sub.3-7 branched haloalkyl.

    [1849] In some embodiments R.sup.20d is C.sub.1-6 linear haloalkoxy.

    [1850] In some embodiments R.sup.20d is C.sub.3-7 branched haloalkoxy.

    [1851] In some embodiments R.sup.20d is SH.

    [1852] In some embodiments R.sup.20d is SC.sub.1-6 linear alkyl.

    [1853] In some embodiments R.sup.20d is SC.sub.3-7 branched alkyl.

    [1854] In some embodiments R.sup.20d is SC.sub.3-7cycloalkyl.

    [1855] In some embodiments R.sup.20d is SO.sub.2C.sub.1-6 linear alkyl.

    [1856] In some embodiments R.sup.20d is SO.sub.2C.sub.3-7 branched alkyl.

    [1857] In some embodiments R.sup.20d is SO.sub.2C.sub.3-7cycloalkyl.

    [1858] In some embodiments R.sup.20d is SO.sub.2NH.sub.2.

    [1859] In some embodiments R.sup.20d is SO.sub.2NHR.sup.21.

    [1860] In some embodiments R.sup.20d is NHSO.sub.2R.sup.22.

    [1861] In some embodiments R.sup.20d is —NR.sup.23aR.sup.23b.

    [1862] In some embodiments R.sup.20d is NHC(O)R.sup.24.

    [1863] In some embodiments R.sup.20d is C(O)NHR.sup.24.

    [1864] In some embodiments R.sup.20d is C(O)N(R.sup.24).sub.2.

    [1865] In some embodiments R.sup.20d is morpholino.

    [1866] In some embodiments R.sup.20d is

    ##STR00418##

    [1867] In some embodiments R.sup.20e is hydrogen.

    [1868] In some embodiments R.sup.20e is —CN.

    [1869] In some embodiments R.sup.20e is —NO.sub.2.

    [1870] In some embodiments R.sup.20e is —OH.

    [1871] In some embodiments R.sup.20e is halogen.

    [1872] In some embodiments R.sup.20e is C.sub.1-6 linear alkyl.

    [1873] In some embodiments R.sup.20e is C.sub.3-7 branched alkyl.

    [1874] In some embodiments R.sup.20e is C.sub.3-7 cycloalkyl.

    [1875] In some embodiments R.sup.20e is C.sub.1-6 linear alkoxy.

    [1876] In some embodiments R.sup.20e is C.sub.3-7 branched alkoxy.

    [1877] In some embodiments R.sup.20e is C.sub.3-7 cycloalkoxy.

    [1878] In some embodiments R.sup.20e is C.sub.1-6 linear haloalkyl.

    [1879] In some embodiments R.sup.20e is C.sub.3-7 branched haloalkyl.

    [1880] In some embodiments R.sup.20e is C.sub.1-6 linear haloalkoxy.

    [1881] In some embodiments R.sup.20e is C.sub.3-7 branched haloalkoxy.

    [1882] In some embodiments R.sup.20e is SH.

    [1883] In some embodiments R.sup.20e is SC.sub.1-6 linear alkyl.

    [1884] In some embodiments R.sup.20e is SC.sub.3-7 branched alkyl.

    [1885] In some embodiments R.sup.20e is SC.sub.3-7cycloalkyl.

    [1886] In some embodiments R.sup.20e is SO.sub.2C.sub.1-6 linear alkyl.

    [1887] In some embodiments R.sup.20e is SO.sub.2C.sub.3-7 branched alkyl.

    [1888] In some embodiments R.sup.20e is SO.sub.2C.sub.3-7cycloalkyl.

    [1889] In some embodiments R.sup.20e is SO.sub.2NH.sub.2.

    [1890] In some embodiments R.sup.20e is SO.sub.2NHR.sup.21.

    [1891] In some embodiments R.sup.20e isNHSO.sub.2R.sup.22.

    [1892] In some embodiments R.sup.20e is —NR.sup.23aR.sup.23b.

    [1893] In some embodiments R.sup.20e is NHC(O)R.sup.24.

    [1894] In some embodiments R.sup.20e is C(O)NHR.sup.24.

    [1895] In some embodiments R.sup.20e is C(O)N(R.sup.24).sub.2.

    [1896] In some embodiments R.sup.20e is morpholino.

    [1897] In some embodiments R.sup.20e is

    ##STR00419##

    [1898] In some embodiments R.sup.20f is hydrogen.

    [1899] In some embodiments R.sup.20f is —CN.

    [1900] In some embodiments R.sup.20f is —NO.sub.2.

    [1901] In some embodiments R.sup.20f is —OH.

    [1902] In some embodiments R.sup.20f is halogen.

    [1903] In some embodiments R.sup.20f is C.sub.1-6 linear alkyl.

    [1904] In some embodiments R.sup.20f is C.sub.3-7 branched alkyl.

    [1905] In some embodiments R.sup.20f is C.sub.3-7 cycloalkyl.

    [1906] In some embodiments R.sup.20f is C.sub.1-6 linear alkoxy.

    [1907] In some embodiments R.sup.20f is C.sub.3-7 branched alkoxy.

    [1908] In some embodiments R.sup.20f is C.sub.3-7 cycloalkoxy.

    [1909] In some embodiments R.sup.20f is C.sub.1-6 linear haloalkyl.

    [1910] In some embodiments R.sup.20f is C.sub.3-7 branched haloalkyl.

    [1911] In some embodiments R.sup.20f is C.sub.1-6 linear haloalkoxy.

    [1912] In some embodiments R.sup.20f is C.sub.3-7 branched haloalkoxy.

    [1913] In some embodiments R.sup.20f is SH.

    [1914] In some embodiments R.sup.20f is SC.sub.1-6 linear alkyl.

    [1915] In some embodiments R.sup.20f is SC.sub.3-7 branched alkyl.

    [1916] In some embodiments R.sup.20f is SC.sub.3-7cycloalkyl.

    [1917] In some embodiments R.sup.20f is SO.sub.2C.sub.1-6 linear alkyl.

    [1918] In some embodiments R.sup.20f is SO.sub.2C.sub.3-7 branched alkyl.

    [1919] In some embodiments R.sup.20f is SO.sub.2C.sub.3-7cycloalkyl.

    [1920] In some embodiments R.sup.20f is SO.sub.2NH.sub.2.

    [1921] In some embodiments R.sup.20f is SO.sub.2NHR.sup.21.

    [1922] In some embodiments R.sup.20f is NHSO.sub.2R.sup.22.

    [1923] In some embodiments R.sup.20f is —NR.sup.23aR.sup.23b.

    [1924] In some embodiments R.sup.20f is NHC(O)R.sup.24.

    [1925] In some embodiments R.sup.20f is C(O)NHR.sup.24.

    [1926] In some embodiments R.sup.20f is C(O)N(R.sup.24).sub.2.

    [1927] In some embodiments R.sup.20f is morpholino.

    [1928] In some embodiments R.sup.20f is

    ##STR00420##

    [1929] In some embodiments R.sup.20g is hydrogen.

    [1930] In some embodiments R.sup.20g is —CN.

    [1931] In some embodiments R.sup.20g is —NO.sub.2.

    [1932] In some embodiments R.sup.20g is —OH.

    [1933] In some embodiments R.sup.20g is halogen.

    [1934] In some embodiments R.sup.20g is C.sub.1-6 linear alkyl.

    [1935] In some embodiments R.sup.20g is C.sub.3-7 branched alkyl.

    [1936] In some embodiments R.sup.20g is C.sub.3-7 cycloalkyl.

    [1937] In some embodiments R.sup.20g is C.sub.1-6 linear alkoxy.

    [1938] In some embodiments R.sup.20g is C.sub.3-7 branched alkoxy.

    [1939] In some embodiments R.sup.20g is C.sub.3-7 cycloalkoxy.

    [1940] In some embodiments R.sup.20g is C.sub.1-6 linear haloalkyl.

    [1941] In some embodiments R.sup.20g is C.sub.3-7 branched haloalkyl.

    [1942] In some embodiments R.sup.20g is C.sub.1-6 linear haloalkoxy.

    [1943] In some embodiments R.sup.20g is C.sub.3-7 branched haloalkoxy.

    [1944] In some embodiments R.sup.20g is SH.

    [1945] In some embodiments R.sup.20g is SC.sub.1-6 linear alkyl.

    [1946] In some embodiments R.sup.20g is SC.sub.3-7 branched alkyl.

    [1947] In some embodiments R.sup.20g is SC.sub.3-7cycloalkyl.

    [1948] In some embodiments R.sup.20g is SO.sub.2C.sub.1-6 linear alkyl.

    [1949] In some embodiments R.sup.20g is SO.sub.2C.sub.3-7 branched alkyl.

    [1950] In some embodiments R.sup.20g is SO.sub.2C.sub.3-7cycloalkyl.

    [1951] In some embodiments R.sup.20g is SO.sub.2NH.sub.2.

    [1952] In some embodiments R.sup.20g is SO.sub.2NHR.sup.21.

    [1953] In some embodiments R.sup.20g is NHSO.sub.2R.sup.22.

    [1954] In some embodiments R.sup.20g is —NR.sup.23aR.sup.23b

    [1955] In some embodiments R.sup.20g is NHC(O)R.sup.24.

    [1956] In some embodiments R.sup.20g is C(O)NHR.sup.24.

    [1957] In some embodiments R.sup.20g is C(O)N(R.sup.24).sub.2.

    [1958] In some embodiments R.sup.20g is morpholino.

    [1959] In some embodiments R.sup.20g is

    ##STR00421##

    [1960] In some embodiments R.sup.21 is hydrogen.

    [1961] In some embodiments R.sup.21 is C.sub.1-6 linear alkyl.

    [1962] In some embodiments R.sup.21 is C.sub.3-7 branched alkyl.

    [1963] In some embodiments R.sup.21 is C.sub.3-7 cycloalkyl.

    [1964] In some embodiments R.sup.22 is hydrogen.

    [1965] In some embodiments R.sup.22 is C.sub.1-6 linear alkyl.

    [1966] In some embodiments R.sup.22 is C.sub.3-7 branched alkyl.

    [1967] In some embodiments R.sup.22 is C.sub.3-7 cycloalkyl.

    [1968] In some embodiments R.sup.23a is hydrogen.

    [1969] In some embodiments R.sup.23a is C.sub.1-6 linear alkyl.

    [1970] In some embodiments R.sup.23a is C.sub.3-7 branched alkyl.

    [1971] In some embodiments R.sup.23a is C.sub.3-7 cycloalkyl.

    [1972] In some embodiments R.sup.23b is hydrogen.

    [1973] In some embodiments R.sup.23b is C.sub.1-6 linear alkyl.

    [1974] In some embodiments R.sup.23b is C.sub.3-7 branched alkyl.

    [1975] In some embodiments R.sup.23b is C.sub.3-7 cycloalkyl.

    [1976] In some embodiments R.sup.24 is hydrogen.

    [1977] In some embodiments R.sup.24 is C.sub.1-6 linear alkyl.

    [1978] In some embodiments R.sup.24 is C.sub.3-7 branched alkyl.

    [1979] In some embodiments R.sup.24 is C.sub.3-7 cycloalkyl.

    [1980] In some embodiments R.sup.25 is hydrogen.

    [1981] In some embodiments R.sup.25 is C.sub.1-6 linear alkyl.

    [1982] In some embodiments R.sup.25 is C.sub.3-7 branched alkyl.

    [1983] In some embodiments R.sup.25 is C.sub.3-7 cycloalkyl.

    [1984] In some embodiments Q.sup.1 is 1.

    [1985] In some embodiments Q.sup.1 is 2.

    [1986] In some embodiments Q.sup.2 is 1.

    [1987] In some embodiments Q.sup.2 is 2.

    [1988] In some embodiments X.sup.1 is 0.

    [1989] In some embodiments X.sup.1 is S.

    [1990] In some embodiments X.sup.1 is SO.

    [1991] In some embodiments X.sup.1 is SO.sub.2.

    [1992] In some embodiments X.sup.1 is NR.sup.7.

    Exemplary Compounds

    [1993] Exemplary compounds include any of the compounds described herein. In embodiments where the compounds or formulas described herein do not specify the configuration of the lactam stereocenter (i.e., the carbon substituted by the nitrogen of the lactam) is not indicated, said lactam stereocenter can have the R-configuration. In other embodiments, said lactam stereocenter can have the S-configuration.

    [1994] In embodiments, a compound is any compound described herein or a pharmaceutically acceptable salt thereof. In embodiments, a compound that is described in any one of Tables 1-39, or a pharmaceutically acceptable salt thereof. In embodiments, a compound is a compound described in any one of Tables 34-39, or a pharmaceutically acceptable salt thereof.

    [1995] Exemplary embodiments include compounds having the formula (II)

    ##STR00422##

    or a pharmaceutically acceptable salt form thereof defined herein below in Table 1.

    TABLE-US-00001 TABLE 1 Entry R.sup.1 R.sup.2 n R.sup.3 1 Methyl Methyl 1 Phenyl 2 Methyl Methyl 2 Phenyl 3 Methyl Methyl 3 Phenyl 4 Methyl Methyl 4 Phenyl 5 Methyl Methyl 1 4-OH-Phenyl 6 Methyl Methyl 2 4-OH-Phenyl 7 Methyl Methyl 3 4-OH-Phenyl 8 Methyl Methyl 4 4-OH-Phenyl 9 Methyl Methyl 1 3-OH-Phenyl 10 Methyl Methyl 2 3-OH-Phenyl 11 Methyl Methyl 3 3-OH-Phenyl 12 Methyl Methyl 4 3-OH-Phenyl 13 Methyl Methyl 1 2-OH-Phenyl 14 Methyl Methyl 2 2-OH-Phenyl 15 Methyl Methyl 3 2-OH-Phenyl 16 Methyl Methyl 4 2-OH-Phenyl 17 Methyl Methyl 1 4-OMe-Phenyl 18 Methyl Methyl 2 4-OMe-Phenyl 19 Methyl Methyl 3 4-OMe-Phenyl 20 Methyl Methyl 4 4-OMe-Phenyl 21 Methyl Methyl 1 3-OMe-Phenyl 22 Methyl Methyl 2 3-OMe-Phenyl 23 Methyl Methyl 3 3-OMe-Phenyl 24 Methyl Methyl 4 3-OMe-Phenyl 25 Methyl Methyl 1 2-OMe-Phenyl 26 Methyl Methyl 2 2-OMe-Phenyl 27 Methyl Methyl 3 2-OMe-Phenyl 28 Methyl Methyl 4 2-OMe-Phenyl 29 Methyl Methyl 1 4-CN-Phenyl 30 Methyl Methyl 2 4-CN-Phenyl 31 Methyl Methyl 3 4-CN-Phenyl 32 Methyl Methyl 4 4-CN-Phenyl 33 Methyl Methyl 1 3-CN-Phenyl 34 Methyl Methyl 2 3-CN-Phenyl 35 Methyl Methyl 3 3-CN-Phenyl 36 Methyl Methyl 4 3-CN-Phenyl 37 Methyl Methyl 1 2-CN-Phenyl 38 Methyl Methyl 2 2-CN-Phenyl 39 Methyl Methyl 3 2-CN-Phenyl 40 Methyl Methyl 4 2-CN-Phenyl 41 Methyl Methyl 1 4-Me-Phenyl 42 Methyl Methyl 2 4-Me-Phenyl 43 Methyl Methyl 3 4-Me-Phenyl 44 Methyl Methyl 4 4-Me-Phenyl 45 Methyl Methyl 1 3-Me-Phenyl 46 Methyl Methyl 2 3-Me-Phenyl 47 Methyl Methyl 3 3-Me-Phenyl 48 Methyl Methyl 4 3-Me-Phenyl 49 Methyl Methyl 1 2-Me-Phenyl 50 Methyl Methyl 2 2-Me-Phenyl 51 Methyl Methyl 3 2-Me-Phenyl 52 Methyl Methyl 4 2-Me-Phenyl 53 Methyl Methyl 1 4-F-Phenyl 54 Methyl Methyl 2 4-F-Phenyl 55 Methyl Methyl 3 4-F-Phenyl 56 Methyl Methyl 4 4-F-Phenyl 57 Methyl Methyl 1 3-F-Phenyl 58 Methyl Methyl 2 3-F-Phenyl 59 Methyl Methyl 3 3-F-Phenyl 60 Methyl Methyl 4 3-F-Phenyl 61 Methyl Methyl 1 2-F-Phenyl 62 Methyl Methyl 2 2-F-Phenyl 63 Methyl Methyl 3 2-F-Phenyl 64 Methyl Methyl 4 2-F-Phenyl 65 Methyl Methyl 1 4-Cl-Phenyl 66 Methyl Methyl 2 4-Cl-Phenyl 67 Methyl Methyl 3 4-Cl-Phenyl 68 Methyl Methyl 4 4-Cl-Phenyl 69 Methyl Methyl 1 3-Cl-Phenyl 70 Methyl Methyl 2 3-Cl-Phenyl 71 Methyl Methyl 3 3-Cl-Phenyl 72 Methyl Methyl 4 3-Cl-Phenyl 73 Methyl Methyl 1 2-Cl-Phenyl 74 Methyl Methyl 2 2-Cl-Phenyl 75 Methyl Methyl 3 2-Cl-Phenyl 76 Methyl Methyl 4 2-Cl-Phenyl 77 Methyl Methyl 1 4-Br-Phenyl 78 Methyl Methyl 2 4-Br-Phenyl 79 Methyl Methyl 3 4-Br-Phenyl 80 Methyl Methyl 4 4-Br-Phenyl 81 Methyl Methyl 1 3-Br-Phenyl 82 Methyl Methyl 2 3-Br-Phenyl 83 Methyl Methyl 3 3-Br-Phenyl 84 Methyl Methyl 4 3-Br-Phenyl 85 Methyl Methyl 1 2-Br-Phenyl 86 Methyl Methyl 2 2-Br-Phenyl 87 Methyl Methyl 3 2-Br-Phenyl 88 Methyl Methyl 4 2-Br-Phenyl 89 Methyl Methyl 1 4-CF.sub.3-Phenyl 90 Methyl Methyl 2 4-CF.sub.3-Phenyl 91 Methyl Methyl 3 4-CF.sub.3-Phenyl 92 Methyl Methyl 4 4-CF.sub.3-Phenyl 93 Methyl Methyl 1 3-CF.sub.3-Phenyl 94 Methyl Methyl 2 3-CF.sub.3-Phenyl 95 Methyl Methyl 3 3-CF.sub.3-Phenyl 96 Methyl Methyl 4 3-CF.sub.3-Phenyl 97 Methyl Methyl 1 2-CF.sub.3-Phenyl 98 Methyl Methyl 2 2-CF.sub.3-Phenyl 99 Methyl Methyl 3 2-CF.sub.3-Phenyl 100 Methyl Methyl 4 2-CF.sub.3-Phenyl 101 Methyl Methyl 1 4-iPr-Phenyl 102 Methyl Methyl 2 4-iPr-Phenyl 103 Methyl Methyl 3 4-iPr-Phenyl 104 Methyl Methyl 4 4-iPr-Phenyl 105 Methyl Methyl 1 3-iPr-Phenyl 106 Methyl Methyl 2 3-iPr-Phenyl 107 Methyl Methyl 3 3-iPr-Phenyl 108 Methyl Methyl 4 3-iPr-Phenyl 109 Methyl Methyl 1 2-iPr-Phenyl 110 Methyl Methyl 2 2-iPr-Phenyl 111 Methyl Methyl 3 2-iPr-Phenyl 112 Methyl Methyl 4 2-iPr-Phenyl 113 Methyl Methyl 1 4-NH.sub.2-Phenyl 114 Methyl Methyl 2 4-NH.sub.2-Phenyl 115 Methyl Methyl 3 4-NH.sub.2-Phenyl 116 Methyl Methyl 4 4-NH.sub.2-Phenyl 117 Methyl Methyl 1 3-NH.sub.2-Phenyl 118 Methyl Methyl 2 3-NH.sub.2-Phenyl 119 Methyl Methyl 3 3-NH.sub.2-Phenyl 120 Methyl Methyl 4 3-NH.sub.2-Phenyl 121 Methyl Methyl 1 2-NH.sub.2-Phenyl 122 Methyl Methyl 2 2-NH.sub.2-Phenyl 123 Methyl Methyl 3 2-NH.sub.2-Phenyl 124 Methyl Methyl 4 2-NH.sub.2-Phenyl 125 Methyl Methyl 1 2,3-di-Me-Phenyl 126 Methyl Methyl 2 2,3-di-Me-Phenyl 127 Methyl Methyl 3 2,3-di-Me-Phenyl 128 Methyl Methyl 4 2,3-di-Me-Phenyl 129 Methyl Methyl 1 2,4-di-Me-Phenyl 130 Methyl Methyl 2 2,4-di-Me-Phenyl 131 Methyl Methyl 3 2,4-di-Me-Phenyl 132 Methyl Methyl 4 2,4-di-Me-Phenyl 133 Methyl Methyl 1 2,5-di-Me-Phenyl 134 Methyl Methyl 2 2,5-di-Me-Phenyl 135 Methyl Methyl 3 2,5-di-Me-Phenyl 136 Methyl Methyl 4 2,5-di-Me-Phenyl 137 Methyl Methyl 1 2,6-di-Me-Phenyl 138 Methyl Methyl 2 2,6-di-Me-Phenyl 139 Methyl Methyl 3 2,6-di-Me-Phenyl 140 Methyl Methyl 4 2,6-di-Me-Phenyl 141 Methyl Methyl 1 2,6-di-iPr-Phenyl 142 Methyl Methyl 2 2,6-di-iPr-Phenyl 143 Methyl Methyl 3 2,6-di-iPr-Phenyl 144 Methyl Methyl 4 2,6-di-iPr-Phenyl 145 Methyl Methyl 1 2-morpholino-phenyl 146 Methyl Methyl 2 2-morpholino-phenyl 147 Methyl Methyl 3 2-morpholino-phenyl 148 Methyl Methyl 4 2-morpholino-phenyl 149 Methyl Methyl 1 3-morpholino-phenyl 150 Methyl Methyl 2 3-morpholino-phenyl 151 Methyl Methyl 3 3-morpholino-phenyl 152 Methyl Methyl 4 3-morpholino-phenyl 153 Methyl Methyl 1 4-morpholino-phenyl 154 Methyl Methyl 2 4-morpholino-phenyl 155 Methyl Methyl 3 4-morpholino-phenyl 156 Methyl Methyl 4 4-morpholino-phenyl 157 Methyl Methyl 1 4-CN-2-morpholino-phenyl 158 Methyl Methyl 2 4-CN-2-morpholino-phenyl 159 Methyl Methyl 3 4-CN-2-morpholino-phenyl 160 Methyl Methyl 4 4-CN-2-morpholino-phenyl 161 Methyl Methyl 1 4-CH.sub.3-2-morpholino-phenyl 162 Methyl Methyl 2 4-CH.sub.3-2-morpholino-phenyl 163 Methyl Methyl 3 4-CH.sub.3-2-morpholino-phenyl 164 Methyl Methyl 4 4-CH.sub.3-2-morpholino-phenyl 165 Methyl Methyl 1 4-OH-2-morpholino-phenyl 166 Methyl Methyl 2 4-OH-2-morpholino-phenyl 167 Methyl Methyl 3 4-OH-2-morpholino-phenyl 168 Methyl Methyl 4 4-OH-2-morpholino-phenyl 169 Methyl Methyl 1 naphthylen-1-yl 170 Methyl Methyl 2 naphthylen-1-yl 171 Methyl Methyl 3 naphthylen-1-yl 172 Methyl Methyl 4 naphthylen-1-yl 173 Methyl Methyl 1 naphthylen-2-yl 174 Methyl Methyl 2 naphthylen-2-yl 175 Methyl Methyl 3 naphthylen-2-yl 176 Methyl Methyl 4 naphthylen-2-yl 177 Ethyl Ethyl 1 Phenyl 178 Ethyl Ethyl 2 Phenyl 179 Ethyl Ethyl 3 Phenyl 180 Ethyl Ethyl 4 Phenyl 181 Ethyl Ethyl 1 4-OH-Phenyl 182 Ethyl Ethyl 2 4-OH-Phenyl 183 Ethyl Ethyl 3 4-OH-Phenyl 184 Ethyl Ethyl 4 4-OH-Phenyl 185 Ethyl Ethyl 1 3-OH-Phenyl 186 Ethyl Ethyl 2 3-OH-Phenyl 187 Ethyl Ethyl 3 3-OH-Phenyl 188 Ethyl Ethyl 4 3-OH-Phenyl 189 Ethyl Ethyl 1 2-OH-Phenyl 190 Ethyl Ethyl 2 2-OH-Phenyl 191 Ethyl Ethyl 3 2-OH-Phenyl 192 Ethyl Ethyl 4 2-OH-Phenyl 193 Ethyl Ethyl 1 4-OMe-Phenyl 194 Ethyl Ethyl 2 4-OMe-Phenyl 195 Ethyl Ethyl 3 4-OMe-Phenyl 196 Ethyl Ethyl 4 4-OMe-Phenyl 197 Ethyl Ethyl 1 3-OMe-Phenyl 198 Ethyl Ethyl 2 3-OMe-Phenyl 199 Ethyl Ethyl 3 3-OMe-Phenyl 200 Ethyl Ethyl 4 3-OMe-Phenyl 201 Ethyl Ethyl 1 2-OMe-Phenyl 202 Ethyl Ethyl 2 2-OMe-Phenyl 203 Ethyl Ethyl 3 2-OMe-Phenyl 204 Ethyl Ethyl 4 2-OMe-Phenyl 205 Ethyl Ethyl 1 4-CN-Phenyl 206 Ethyl Ethyl 2 4-CN-Phenyl 207 Ethyl Ethyl 3 4-CN-Phenyl 208 Ethyl Ethyl 4 4-CN-Phenyl 209 Ethyl Ethyl 1 3-CN-Phenyl 210 Ethyl Ethyl 2 3-CN-Phenyl 211 Ethyl Ethyl 3 3-CN-Phenyl 212 Ethyl Ethyl 4 3-CN-Phenyl 213 Ethyl Ethyl 1 2-CN-Phenyl 214 Ethyl Ethyl 2 2-CN-Phenyl 215 Ethyl Ethyl 3 2-CN-Phenyl 216 Ethyl Ethyl 4 2-CN-Phenyl 217 Ethyl Ethyl 1 4-Me-Phenyl 218 Ethyl Ethyl 2 4-Me-Phenyl 219 Ethyl Ethyl 3 4-Me-Phenyl 220 Ethyl Ethyl 4 4-Me-Phenyl 221 Ethyl Ethyl 1 3-Me-Phenyl 222 Ethyl Ethyl 2 3-Me-Phenyl 223 Ethyl Ethyl 3 3-Me-Phenyl 224 Ethyl Ethyl 4 3-Me-Phenyl 225 Ethyl Ethyl 1 2-Me-Phenyl 226 Ethyl Ethyl 2 2-Me-Phenyl 227 Ethyl Ethyl 3 2-Me-Phenyl 228 Ethyl Ethyl 4 2-Me-Phenyl 229 Ethyl Ethyl 1 4-F-Phenyl 230 Ethyl Ethyl 2 4-F-Phenyl 231 Ethyl Ethyl 3 4-F-Phenyl 232 Ethyl Ethyl 4 4-F-Phenyl 233 Ethyl Ethyl 1 3-F-Phenyl 234 Ethyl Ethyl 2 3-F-Phenyl 235 Ethyl Ethyl 3 3-F-Phenyl 236 Ethyl Ethyl 4 3-F-Phenyl 237 Ethyl Ethyl 1 2-F-Phenyl 238 Ethyl Ethyl 2 2-F-Phenyl 239 Ethyl Ethyl 3 2-F-Phenyl 240 Ethyl Ethyl 4 2-F-Phenyl 241 Ethyl Ethyl 1 4-Cl-Phenyl 242 Ethyl Ethyl 2 4-Cl-Phenyl 243 Ethyl Ethyl 3 4-Cl-Phenyl 244 Ethyl Ethyl 4 4-Cl-Phenyl 245 Ethyl Ethyl 1 3-Cl-Phenyl 246 Ethyl Ethyl 2 3-Cl-Phenyl 247 Ethyl Ethyl 3 3-Cl-Phenyl 248 Ethyl Ethyl 4 3-Cl-Phenyl 249 Ethyl Ethyl 1 2-Cl-Phenyl 250 Ethyl Ethyl 2 2-Cl-Phenyl 251 Ethyl Ethyl 3 2-Cl-Phenyl 252 Ethyl Ethyl 4 2-Cl-Phenyl 253 Ethyl Ethyl 1 4-Br-Phenyl 254 Ethyl Ethyl 2 4-Br-Phenyl 255 Ethyl Ethyl 3 4-Br-Phenyl 256 Ethyl Ethyl 4 4-Br-Phenyl 257 Ethyl Ethyl 1 3-Br-Phenyl 258 Ethyl Ethyl 2 3-Br-Phenyl 259 Ethyl Ethyl 3 3-Br-Phenyl 260 Ethyl Ethyl 4 3-Br-Phenyl 261 Ethyl Ethyl 1 2-Br-Phenyl 262 Ethyl Ethyl 2 2-Br-Phenyl 263 Ethyl Ethyl 3 2-Br-Phenyl 264 Ethyl Ethyl 4 2-Br-Phenyl 265 Ethyl Ethyl 1 4-CF.sub.3-Phenyl 266 Ethyl Ethyl 2 4-CF.sub.3-Phenyl 267 Ethyl Ethyl 3 4-CF.sub.3-Phenyl 268 Ethyl Ethyl 4 4-CF.sub.3-Phenyl 269 Ethyl Ethyl 1 3-CF.sub.3-Phenyl 270 Ethyl Ethyl 2 3-CF.sub.3-Phenyl 271 Ethyl Ethyl 3 3-CF.sub.3-Phenyl 272 Ethyl Ethyl 4 3-CF.sub.3-Phenyl 273 Ethyl Ethyl 1 2-CF.sub.3-Phenyl 274 Ethyl Ethyl 2 2-CF.sub.3-Phenyl 275 Ethyl Ethyl 3 2-CF.sub.3-Phenyl 276 Ethyl Ethyl 4 2-CF.sub.3-Phenyl 277 Ethyl Ethyl 1 4-iPr-Phenyl 278 Ethyl Ethyl 2 4-iPr-Phenyl 279 Ethyl Ethyl 3 4-iPr-Phenyl 280 Ethyl Ethyl 4 4-iPr-Phenyl 281 Ethyl Ethyl 1 3-iPr-Phenyl 282 Ethyl Ethyl 2 3-iPr-Phenyl 283 Ethyl Ethyl 3 3-iPr-Phenyl 284 Ethyl Ethyl 4 3-iPr-Phenyl 285 Ethyl Ethyl 1 2-iPr-Phenyl 286 Ethyl Ethyl 2 2-iPr-Phenyl 287 Ethyl Ethyl 3 2-iPr-Phenyl 288 Ethyl Ethyl 4 2-iPr-Phenyl 289 Ethyl Ethyl 1 4-NH.sub.2-Phenyl 290 Ethyl Ethyl 2 4-NH.sub.2-Phenyl 291 Ethyl Ethyl 3 4-NH.sub.2-Phenyl 292 Ethyl Ethyl 4 4-NH.sub.2-Phenyl 293 Ethyl Ethyl 1 3-NH.sub.2-Phenyl 294 Ethyl Ethyl 2 3-NH.sub.2-Phenyl 295 Ethyl Ethyl 3 3-NH.sub.2-Phenyl 296 Ethyl Ethyl 4 3-NH.sub.2-Phenyl 297 Ethyl Ethyl 1 2-NH.sub.2-Phenyl 298 Ethyl Ethyl 2 2-NH.sub.2-Phenyl 299 Ethyl Ethyl 3 2-NH.sub.2-Phenyl 300 Ethyl Ethyl 4 2-NH.sub.2-Phenyl 301 Ethyl Ethyl 1 2,3-di-Me-Phenyl 302 Ethyl Ethyl 2 2,3-di-Me-Phenyl 303 Ethyl Ethyl 3 2,3-di-Me-Phenyl 304 Ethyl Ethyl 4 2,3-di-Me-Phenyl 305 Ethyl Ethyl 1 2,4-di-Me-Phenyl 306 Ethyl Ethyl 2 2,4-di-Me-Phenyl 307 Ethyl Ethyl 3 2,4-di-Me-Phenyl 308 Ethyl Ethyl 4 2,4-di-Me-Phenyl 309 Ethyl Ethyl 1 2,5-di-Me-Phenyl 310 Ethyl Ethyl 2 2,5-di-Me-Phenyl 311 Ethyl Ethyl 3 2,5-di-Me-Phenyl 312 Ethyl Ethyl 4 2,5-di-Me-Phenyl 313 Ethyl Ethyl 1 2,6-di-Me-Phenyl 314 Ethyl Ethyl 2 2,6-di-Me-Phenyl 315 Ethyl Ethyl 3 2,6-di-Me-Phenyl 316 Ethyl Ethyl 4 2,6-di-Me-Phenyl 317 Ethyl Ethyl 1 2,6-di-iPr-Phenyl 318 Ethyl Ethyl 2 2,6-di-iPr-Phenyl 319 Ethyl Ethyl 3 2,6-di-iPr-Phenyl 320 Ethyl Ethyl 4 2,6-di-iPr-Phenyl 321 Ethyl Ethyl 1 2-morpholino-phenyl 322 Ethyl Ethyl 2 2-morpholino-phenyl 323 Ethyl Ethyl 3 2-morpholino-phenyl 324 Ethyl Ethyl 4 2-morpholino-phenyl 325 Ethyl Ethyl 1 3-morpholino-phenyl 326 Ethyl Ethyl 2 3-morpholino-phenyl 327 Ethyl Ethyl 3 3-morpholino-phenyl 328 Ethyl Ethyl 4 3-morpholino-phenyl 329 Ethyl Ethyl 1 4-morpholino-phenyl 330 Ethyl Ethyl 2 4-morpholino-phenyl 331 Ethyl Ethyl 3 4-morpholino-phenyl 332 Ethyl Ethyl 4 4-morpholino-phenyl 333 Ethyl Ethyl 1 4-CN-2-morpholino-phenyl 334 Ethyl Ethyl 2 4-CN-2-morpholino-phenyl 335 Ethyl Ethyl 3 4-CN-2-morpholino-phenyl 336 Ethyl Ethyl 4 4-CN-2-morpholino-phenyl 337 Ethyl Ethyl 1 4-CH.sub.3-2-morpholino-phenyl 338 Ethyl Ethyl 2 4-CH.sub.3-2-morpholino-phenyl 339 Ethyl Ethyl 3 4-CH.sub.3-2-morpholino-phenyl 340 Ethyl Ethyl 4 4-CH.sub.3-2-morpholino-phenyl 341 Ethyl Ethyl 1 4-OH-2-morpholino-phenyl 342 Ethyl Ethyl 2 4-OH-2-morpholino-phenyl 343 Ethyl Ethyl 3 4-OH-2-morpholino-phenyl 344 Ethyl Ethyl 4 4-OH-2-morpholino-phenyl 345 Ethyl Ethyl 1 naphthylen-1-yl 346 Ethyl Ethyl 2 naphthylen-1-yl 347 Ethyl Ethyl 3 naphthylen-1-yl 348 Ethyl Ethyl 4 naphthylen-1-yl 349 Ethyl Ethyl 1 naphthylen-2-yl 350 Ethyl Ethyl 2 naphthylen-2-yl 351 Ethyl Ethyl 3 naphthylen-2-yl 352 Ethyl Ethyl 4 naphthylen-2-yl

    [1996] Exemplary embodiments include compounds having the formula (VIII)

    ##STR00423##

    [1997] or a pharmaceutically acceptable salt form thereof defined herein below in Table 2.

    TABLE-US-00002 TABLE 2 Entry n R.sup.3 1 1 Phenyl 2 2 Phenyl 3 3 Phenyl 4 4 Phenyl 5 1 4-OH-Phenyl 6 2 4-OH-Phenyl 7 3 4-OH-Phenyl 8 4 4-OH-Phenyl 9 1 3-OH-Phenyl 10 2 3-OH-Phenyl 11 3 3-OH-Phenyl 12 4 3-OH-Phenyl 13 1 2-OH-Phenyl 14 2 2-OH-Phenyl 15 3 2-OH-Phenyl 16 4 2-OH-Phenyl 17 1 4-OMe-Phenyl 18 2 4-OMe-Phenyl 19 3 4-OMe-Phenyl 20 4 4-OMe-Phenyl 21 1 3-OMe-Phenyl 22 2 3-OMe-Phenyl 23 3 3-OMe-Phenyl 24 4 3-OMe-Phenyl 25 1 2-OMe-Phenyl 26 2 2-OMe-Phenyl 27 3 2-OMe-Phenyl 28 4 2-OMe-Phenyl 29 1 4-CN-Phenyl 30 2 4-CN-Phenyl 31 3 4-CN-Phenyl 32 4 4-CN-Phenyl 33 1 3-CN-Phenyl 34 2 3-CN-Phenyl 35 3 3-CN-Phenyl 36 4 3-CN-Phenyl 37 1 2-CN-Phenyl 38 2 2-CN-Phenyl 39 3 2-CN-Phenyl 40 4 2-CN-Phenyl 41 1 4-Me-Phenyl 42 2 4-Me-Phenyl 43 3 4-Me-Phenyl 44 4 4-Me-Phenyl 45 1 3-Me-Phenyl 46 2 3-Me-Phenyl 47 3 3-Me-Phenyl 48 4 3-Me-Phenyl 49 1 2-Me-Phenyl 50 2 2-Me-Phenyl 51 3 2-Me-Phenyl 52 4 2-Me-Phenyl 53 1 4-F-Phenyl 54 2 4-F-Phenyl 55 3 4-F-Phenyl 56 4 4-F-Phenyl 57 1 3-F-Phenyl 58 2 3-F-Phenyl 59 3 3-F-Phenyl 60 4 3-F-Phenyl 61 1 2-F-Phenyl 62 2 2-F-Phenyl 63 3 2-F-Phenyl 64 4 2-F-Phenyl 65 1 4-Cl-Phenyl 66 2 4-Cl-Phenyl 67 3 4-Cl-Phenyl 68 4 4-Cl-Phenyl 69 1 3-Cl-Phenyl 70 2 3-Cl-Phenyl 71 3 3-Cl-Phenyl 72 4 3-Cl-Phenyl 73 1 2-Cl-Phenyl 74 2 2-Cl-Phenyl 75 3 2-Cl-Phenyl 76 4 2-Cl-Phenyl 77 1 4-Br-Phenyl 78 2 4-Br-Phenyl 79 3 4-Br-Phenyl 80 4 4-Br-Phenyl 81 1 3-Br-Phenyl 82 2 3-Br-Phenyl 83 3 3-Br-Phenyl 84 4 3-Br-Phenyl 85 1 naphthylen-1-yl 86 2 naphthylen-1-yl 87 3 naphthylen-1-yl 88 4 naphthylen-1-yl 89 1 2-Br-Phenyl 90 2 2-Br-Phenyl 91 3 2-Br-Phenyl 92 4 2-Br-Phenyl 93 1 4-CF.sub.3-Phenyl 94 2 4-CF.sub.3-Phenyl 95 3 4-CF.sub.3-Phenyl 96 4 4-CF.sub.3-Phenyl 97 1 3-CF.sub.3-Phenyl 98 2 3-CF.sub.3-Phenyl 99 3 3-CF.sub.3-Phenyl 100 4 3-CF.sub.3-Phenyl 101 1 2-CF.sub.3-Phenyl 102 2 2-CF.sub.3-Phenyl 103 3 2-CF.sub.3-Phenyl 104 4 2-CF.sub.3-Phenyl 105 1 4-iPr-Phenyl 106 2 4-iPr-Phenyl 107 3 4-iPr-Phenyl 108 4 4-iPr-Phenyl 109 1 3-iPr-Phenyl 110 2 3-iPr-Phenyl 111 3 3-iPr-Phenyl 112 4 3-iPr-Phenyl 113 1 2-iPr-Phenyl 114 2 2-iPr-Phenyl 115 3 2-iPr-Phenyl 116 4 2-iPr-Phenyl 117 1 4-NH.sub.2-Phenyl 118 2 4-NH.sub.2-Phenyl 119 3 4-NH.sub.2-Phenyl 120 4 4-NH.sub.2-Phenyl 121 1 3-NH.sub.2-Phenyl 122 2 3-NH.sub.2-Phenyl 123 3 3-NH.sub.2-Phenyl 124 4 3-NH.sub.2-Phenyl 125 1 2-NH.sub.2-Phenyl 126 2 2-NH.sub.2-Phenyl 127 3 2-NH.sub.2-Phenyl 128 4 2-NH.sub.2-Phenyl 129 1 2,3-di-Me-Phenyl 130 2 2,3-di-Me-Phenyl 131 3 2,3-di-Me-Phenyl 132 4 2,3-di-Me-Phenyl 133 1 2,4-di-Me-Phenyl 134 2 2,4-di-Me-Phenyl 135 3 2,4-di-Me-Phenyl 136 4 2,4-di-Me-Phenyl 137 1 2,5-di-Me-Phenyl 138 2 2,5-di-Me-Phenyl 139 3 2,5-di-Me-Phenyl 140 4 2,5-di-Me-Phenyl 141 1 2,6-di-Me-Phenyl 142 2 2,6-di-Me-Phenyl 143 3 2,6-di-Me-Phenyl 144 4 2,6-di-Me-Phenyl 145 1 2,6-di-iPr-Phenyl 146 2 2,6-di-iPr-Phenyl 147 3 2,6-di-iPr-Phenyl 148 4 2,6-di-iPr-Phenyl 149 1 2-morpholino-phenyl 150 2 2-morpholino-phenyl 151 3 2-morpholino-phenyl 152 4 2-morpholino-phenyl 153 1 3-morpholino-phenyl 154 2 3-morpholino-phenyl 155 3 3-morpholino-phenyl 156 4 3-morpholino-phenyl 157 1 4-morpholino-phenyl 158 2 4-morpholino-phenyl 159 3 4-morpholino-phenyl 160 4 4-morpholino-phenyl 161 1 4-CN-2-morpholino-phenyl 162 2 4-CN-2-morpholino-phenyl 163 3 4-CN-2-morpholino-phenyl 164 4 4-CN-2-morpholino-phenyl 165 1 4-CH.sub.3-2-morpholino-phenyl 166 2 4-CH.sub.3-2-morpholino-phenyl 167 3 4-CH.sub.3-2-morpholino-phenyl 168 4 4-CH.sub.3-2-morpholino-phenyl 169 1 4-OH-2-morpholino-phenyl 170 2 4-OH-2-morpholino-phenyl 171 3 4-OH-2-morpholino-phenyl 172 4 4-OH-2-morpholino-phenyl 173 1 naphthylen-2-yl 174 2 naphthylen-2-yl 175 3 naphthylen-2-yl 176 4 naphthylen-2-yl

    [1998] Exemplary embodiments include compounds having the formula (IX)

    ##STR00424##

    [1999] or a pharmaceutically acceptable salt form thereof defined herein below in Table 3.

    TABLE-US-00003 TABLE 3 Entry n R.sup.3 1 1 Phenyl 2 2 Phenyl 3 3 Phenyl 4 4 Phenyl 5 1 4-OH-Phenyl 6 2 4-OH-Phenyl 7 3 4-OH-Phenyl 8 4 4-OH-Phenyl 9 1 3-OH-Phenyl 10 2 3-OH-Phenyl 11 3 3-OH-Phenyl 12 4 3-OH-Phenyl 13 1 2-OH-Phenyl 14 2 2-OH-Phenyl 15 3 2-OH-Phenyl 16 4 2-OH-Phenyl 17 1 4-OMe-Phenyl 18 2 4-OMe-Phenyl 19 3 4-OMe-Phenyl 20 4 4-OMe-Phenyl 21 1 3-OMe-Phenyl 22 2 3-OMe-Phenyl 23 3 3-OMe-Phenyl 24 4 3-OMe-Phenyl 25 1 2-OMe-Phenyl 26 2 2-OMe-Phenyl 27 3 2-OMe-Phenyl 28 4 2-OMe-Phenyl 29 1 4-CN-Phenyl 30 2 4-CN-Phenyl 31 3 4-CN-Phenyl 32 4 4-CN-Phenyl 33 1 3-CN-Phenyl 34 2 3-CN-Phenyl 35 3 3-CN-Phenyl 36 4 3-CN-Phenyl 37 1 2-CN-Phenyl 38 2 2-CN-Phenyl 39 3 2-CN-Phenyl 40 4 2-CN-Phenyl 41 1 4-Me-Phenyl 42 2 4-Me-Phenyl 43 3 4-Me-Phenyl 44 4 4-Me-Phenyl 45 1 3-Me-Phenyl 46 2 3-Me-Phenyl 47 3 3-Me-Phenyl 48 4 3-Me-Phenyl 49 1 2-Me-Phenyl 50 2 2-Me-Phenyl 51 3 2-Me-Phenyl 52 4 2-Me-Phenyl 53 1 4-F-Phenyl 54 2 4-F-Phenyl 55 3 4-F-Phenyl 56 4 4-F-Phenyl 57 1 3-F-Phenyl 58 2 3-F-Phenyl 59 3 3-F-Phenyl 60 4 3-F-Phenyl 61 1 2-F-Phenyl 62 2 2-F-Phenyl 63 3 2-F-Phenyl 64 4 2-F-Phenyl 65 1 4-Cl-Phenyl 66 2 4-Cl-Phenyl 67 3 4-Cl-Phenyl 68 4 4-Cl-Phenyl 69 1 3-Cl-Phenyl 70 2 3-Cl-Phenyl 71 3 3-Cl-Phenyl 72 4 3-Cl-Phenyl 73 1 2-Cl-Phenyl 74 2 2-Cl-Phenyl 75 3 2-Cl-Phenyl 76 4 77 1 78 2 79 3 80 4 81 1 82 2 83 3 84 4 85 1 86 2 87 3 88 4 89 1 2-Br-Phenyl 90 2 2-Br-Phenyl 91 3 2-Br-Phenyl 92 4 2-Br-Phenyl 93 1 4-CF.sub.3-Phenyl 94 2 4-CF.sub.3-Phenyl 95 3 4-CF.sub.3-Phenyl 96 4 4-CF.sub.3-Phenyl 97 1 3-CF.sub.3-Phenyl 98 2 3-CF.sub.3-Phenyl 99 3 3-CF.sub.3-Phenyl 100 4 3-CF.sub.3-Phenyl 101 1 2-CF.sub.3-Phenyl 102 2 2-CF.sub.3-Phenyl 103 3 2-CF.sub.3-Phenyl 104 4 2-CF.sub.3-Phenyl 105 1 4-iPr-Phenyl 106 2 4-iPr-Phenyl 107 3 4-iPr-Phenyl 108 4 4-iPr-Phenyl 109 1 3-iPr-Phenyl 110 2 3-iPr-Phenyl 111 3 3-iPr-Phenyl 112 4 3-iPr-Phenyl 113 1 2-iPr-Phenyl 114 2 2-iPr-Phenyl 115 3 2-iPr-Phenyl 116 4 2-iPr-Phenyl 117 1 4-NH.sub.2-Phenyl 118 2 4-NH.sub.2-Phenyl 119 3 4-NH.sub.2-Phenyl 120 4 4-NH.sub.2-Phenyl 121 1 3-NH.sub.2-Phenyl 122 2 3-NH.sub.2-Phenyl 123 3 3-NH.sub.2-Phenyl 124 4 3-NH.sub.2-Phenyl 125 1 2-NH.sub.2-Phenyl 126 2 2-NH.sub.2-Phenyl 127 3 2-NH.sub.2-Phenyl 128 4 2-NH.sub.2-Phenyl 129 1 2,3-di-Me-Phenyl 130 2 2,3-di-Me-Phenyl 131 3 2,3-di-Me-Phenyl 132 4 2,3-di-Me-Phenyl 133 1 2,4-di-Me-Phenyl 134 2 2,4-di-Me-Phenyl 135 3 2,4-di-Me-Phenyl 136 4 2,4-di-Me-Phenyl 137 1 2,5-di-Me-Phenyl 138 2 2,5-di-Me-Phenyl 139 3 2,5-di-Me-Phenyl 140 4 2,5-di-Me-Phenyl 141 1 2,6-di-Me-Phenyl 142 2 2,6-di-Me-Phenyl 143 3 2,6-di-Me-Phenyl 144 4 2,6-di-Me-Phenyl 145 1 2,6-di-iPr-Phenyl 146 2 2,6-di-iPr-Phenyl 147 3 2,6-di-iPr-Phenyl 148 4 2,6-di-iPr-Phenyl 149 1 2-morpholino-phenyl 150 2 2-morpholino-phenyl 151 3 2-morpholino-phenyl 152 4 2-morpholino-phenyl 153 1 3-morpholino-phenyl 154 2 3-morpholino-phenyl 155 3 3-morpholino-phenyl 156 4 3-morpholino-phenyl 157 1 4-morpholino-phenyl 158 2 4-morpholino-phenyl 159 3 4-morpholino-phenyl 160 4 4-morpholino-phenyl 161 1 4-CN-2-morpholino-phenyl 162 2 4-CN-2-morpholino-phenyl 163 3 4-CN-2-morpholino-phenyl 164 4 2-Cl-Phenyl 165 1 4-Br-Phenyl 166 2 4-Br-Phenyl 167 3 4-Br-Phenyl 168 4 4-Br-Phenyl 169 1 3-Br-Phenyl 170 2 3-Br-Phenyl 171 3 3-Br-Phenyl 172 4 3-Br-Phenyl 173 1 naphthylen-1-yl 174 2 naphthylen-1-yl 175 3 naphthylen-1-yl 176 4 naphthylen-1-yl

    [2000] Exemplary embodiments include compounds having the formula (X)

    ##STR00425##

    [2001] or a pharmaceutically acceptable salt form thereof defined herein below in Table 4.

    TABLE-US-00004 TABLE 4 Entry n R.sup.3 1 1 Phenyl 2 2 Phenyl 3 3 Phenyl 4 4 Phenyl 5 1 4-OH-Phenyl 6 2 4-OH-Phenyl 7 3 4-OH-Phenyl 8 4 4-OH-Phenyl 9 1 3-OH-Phenyl 10 2 3-OH-Phenyl 11 3 3-OH-Phenyl 12 4 3-OH-Phenyl 13 1 2-OH-Phenyl 14 2 2-OH-Phenyl 15 3 2-OH-Phenyl 16 4 2-OH-Phenyl 17 1 4-OMe-Phenyl 18 2 4-OMe-Phenyl 19 3 4-OMe-Phenyl 20 4 4-OMe-Phenyl 21 1 3-OMe-Phenyl 22 2 3-OMe-Phenyl 23 3 3-OMe-Phenyl 24 4 3-OMe-Phenyl 25 1 2-OMe-Phenyl 26 2 2-OMe-Phenyl 27 3 2-OMe-Phenyl 28 4 2-OMe-Phenyl 29 1 4-CN-Phenyl 30 2 4-CN-Phenyl 31 3 4-CN-Phenyl 32 4 4-CN-Phenyl 33 1 3-CN-Phenyl 34 2 3-CN-Phenyl 35 3 3-CN-Phenyl 36 4 3-CN-Phenyl 37 1 2-CN-Phenyl 38 2 2-CN-Phenyl 39 3 2-CN-Phenyl 40 4 2-CN-Phenyl 41 1 4-Me-Phenyl 42 2 4-Me-Phenyl 43 3 4-Me-Phenyl 44 4 4-Me-Phenyl 45 1 3-Me-Phenyl 46 2 3-Me-Phenyl 47 3 3-Me-Phenyl 48 4 3-Me-Phenyl 49 1 2-Me-Phenyl 50 2 2-Me-Phenyl 51 3 2-Me-Phenyl 52 4 2-Me-Phenyl 53 1 4-F-Phenyl 54 2 4-F-Phenyl 55 3 4-F-Phenyl 56 4 4-F-Phenyl 57 1 3-F-Phenyl 58 2 3-F-Phenyl 59 3 3-F-Phenyl 60 4 3-F-Phenyl 61 1 2-F-Phenyl 62 2 2-F-Phenyl 63 3 2-F-Phenyl 64 4 2-F-Phenyl 65 1 4-Cl-Phenyl 66 2 4-Cl-Phenyl 67 3 4-Cl-Phenyl 68 4 4-Cl-Phenyl 69 1 3-Cl-Phenyl 70 2 3-Cl-Phenyl 71 3 3-Cl-Phenyl 72 4 3-Cl-Phenyl 73 1 2-Cl-Phenyl 74 2 2-Cl-Phenyl 75 3 2-Cl-Phenyl 76 4 2-Cl-Phenyl 77 1 4-Br-Phenyl 78 2 4-Br-Phenyl 79 3 4-Br-Phenyl 80 4 4-Br-Phenyl 81 1 3-Br-Phenyl 82 2 3-Br-Phenyl 83 3 3-Br-Phenyl 84 4 3-Br-Phenyl 85 1 naphthylen-1-yl 86 2 naphthylen-1-yl 87 3 naphthylen-1-yl 88 4 naphthylen-1-yl 89 1 2-Br-Phenyl 90 2 2-Br-Phenyl 91 3 2-Br-Phenyl 92 4 2-Br-Phenyl 93 1 4-CF.sub.3-Phenyl 94 2 4-CF.sub.3-Phenyl 95 3 4-CF.sub.3-Phenyl 96 4 4-CF.sub.3-Phenyl 97 1 3-CF.sub.3-Phenyl 98 2 3-CF.sub.3-Phenyl 99 3 3-CF.sub.3-Phenyl 100 4 3-CF.sub.3-Phenyl 101 1 2-CF.sub.3-Phenyl 102 2 2-CF.sub.3-Phenyl 103 3 2-CF.sub.3-Phenyl 104 4 2-CF.sub.3-Phenyl 105 1 4-iPr-Phenyl 106 2 4-iPr-Phenyl 107 3 4-iPr-Phenyl 108 4 4-iPr-Phenyl 109 1 3-iPr-Phenyl 110 2 3-iPr-Phenyl 111 3 3-iPr-Phenyl 112 4 3-iPr-Phenyl 113 1 2-iPr-Phenyl 114 2 2-iPr-Phenyl 115 3 2-iPr-Phenyl 116 4 2-iPr-Phenyl 117 1 4-NH.sub.2-Phenyl 118 2 4-NH.sub.2-Phenyl 119 3 4-NH.sub.2-Phenyl 120 4 4-NH.sub.2-Phenyl 121 1 3-NH.sub.2-Phenyl 122 2 3-NH.sub.2-Phenyl 123 3 3-NH.sub.2-Phenyl 124 4 3-NH.sub.2-Phenyl 125 1 2-NH.sub.2-Phenyl 126 2 2-NH.sub.2-Phenyl 127 3 2-NH.sub.2-Phenyl 128 4 2-NH.sub.2-Phenyl 129 1 2,3-di-Me-Phenyl 130 2 2,3-di-Me-Phenyl 131 3 2,3-di-Me-Phenyl 132 4 2,3-di-Me-Phenyl 133 1 2,4-di-Me-Phenyl 134 2 2,4-di-Me-Phenyl 135 3 2,4-di-Me-Phenyl 136 4 2,4-di-Me-Phenyl 137 1 2,5-di-Me-Phenyl 138 2 2,5-di-Me-Phenyl 139 3 2,5-di-Me-Phenyl 140 4 2,5-di-Me-Phenyl 141 1 2,6-di-Me-Phenyl 142 2 2,6-di-Me-Phenyl 143 3 2,6-di-Me-Phenyl 144 4 2,6-di-Me-Phenyl 145 1 2,6-di-iPr-Phenyl 146 2 2,6-di-iPr-Phenyl 147 3 2,6-di-iPr-Phenyl 148 4 2,6-di-iPr-Phenyl 149 1 2-morpholino-phenyl 150 2 2-morpholino-phenyl 151 3 2-morpholino-phenyl 152 4 2-morpholino-phenyl 153 1 3-morpholino-phenyl 154 2 3-morpholino-phenyl 155 3 3-morpholino-phenyl 156 4 3-morpholino-phenyl 157 1 4-morpholino-phenyl 158 2 4-morpholino-phenyl 159 3 4-morpholino-phenyl 160 4 4-morpholino-phenyl 161 1 4-CN-2-morpholino-phenyl 162 2 4-CN-2-morpholino-phenyl 163 3 4-CN-2-morpholino-phenyl 164 4 4-CN-2-morpholino-phenyl 165 1 4-CH.sub.3-2-morpholino-phenyl 166 2 4-CH.sub.3-2-morpholino-phenyl 167 3 4-CH.sub.3-2-morpholino-phenyl 168 4 4-CH.sub.3-2-morpholino-phenyl 169 1 4-OH-2-morpholino-phenyl 170 2 4-OH-2-morpholino-phenyl 171 3 4-OH-2-morpholino-phenyl 172 4 4-OH-2-morpholino-phenyl 173 1 naphthylen-2-yl 174 2 naphthylen-2-yl 175 3 naphthylen-2-yl 176 4 naphthylen-2-yl

    [2002] Exemplary embodiments include compounds having the formula (XI)

    ##STR00426##

    [2003] or a pharmaceutically acceptable salt form thereof defined herein below in Table 5.

    TABLE-US-00005 TABLE 5 Entry n R.sup.3 1 1 Phenyl 2 2 Phenyl 3 3 Phenyl 4 4 Phenyl 5 1 4-OH-Phenyl 6 2 4-OH-Phenyl 7 3 4-OH-Phenyl 8 4 4-OH-Phenyl 9 1 3-OH-Phenyl 10 2 3-OH-Phenyl 11 3 3-OH-Phenyl 12 4 3-OH-Phenyl 13 1 2-OH-Phenyl 14 2 2-OH-Phenyl 15 3 2-OH-Phenyl 16 4 2-OH-Phenyl 17 1 4-OMe-Phenyl 18 2 4-OMe-Phenyl 19 3 4-OMe-Phenyl 20 4 4-OMe-Phenyl 21 1 3-OMe-Phenyl 22 2 3-OMe-Phenyl 23 3 3-OMe-Phenyl 24 4 3-OMe-Phenyl 25 1 2-OMe-Phenyl 26 2 2-OMe-Phenyl 27 3 2-OMe-Phenyl 28 4 2-OMe-Phenyl 29 1 4-CN-Phenyl 30 2 4-CN-Phenyl 31 3 4-CN-Phenyl 32 4 4-CN-Phenyl 33 1 3-CN-Phenyl 34 2 3-CN-Phenyl 35 3 3-CN-Phenyl 36 4 3-CN-Phenyl 37 1 2-CN-Phenyl 38 2 2-CN-Phenyl 39 3 2-CN-Phenyl 40 4 2-CN-Phenyl 41 1 4-Me-Phenyl 42 2 4-Me-Phenyl 43 3 4-Me-Phenyl 44 4 4-Me-Phenyl 45 1 3-Me-Phenyl 46 2 3-Me-Phenyl 47 3 3-Me-Phenyl 48 4 3-Me-Phenyl 49 1 2-Me-Phenyl 50 2 2-Me-Phenyl 51 3 2-Me-Phenyl 52 4 2-Me-Phenyl 53 1 4-F-Phenyl 54 2 4-F-Phenyl 55 3 4-F-Phenyl 56 4 4-F-Phenyl 57 1 3-F-Phenyl 58 2 3-F-Phenyl 59 3 3-F-Phenyl 60 4 3-F-Phenyl 61 1 2-F-Phenyl 62 2 2-F-Phenyl 63 3 2-F-Phenyl 64 4 2-F-Phenyl 65 1 4-Cl-Phenyl 66 2 4-Cl-Phenyl 67 3 4-Cl-Phenyl 68 4 4-Cl-Phenyl 69 1 3-Cl-Phenyl 70 2 3-Cl-Phenyl 71 3 3-Cl-Phenyl 72 4 3-Cl-Phenyl 73 1 2-Cl-Phenyl 74 2 2-Cl-Phenyl 75 3 2-Cl-Phenyl 76 4 2-Cl-Phenyl 77 1 4-Br-Phenyl 78 2 4-Br-Phenyl 79 3 4-Br-Phenyl 80 4 4-Br-Phenyl 81 1 3-Br-Phenyl 82 2 3-Br-Phenyl 83 3 3-Br-Phenyl 84 4 3-Br-Phenyl 85 1 naphthylen-1-yl 86 2 naphthylen-1-yl 87 3 naphthylen-1-yl 88 4 naphthylen-1-yl 85 1 2-Br-Phenyl 86 2 2-Br-Phenyl 87 3 2-Br-Phenyl 88 4 2-Br-Phenyl 89 1 4-CF.sub.3-Phenyl 90 2 4-CF.sub.3-Phenyl 91 3 4-CF.sub.3-Phenyl 92 4 4-CF.sub.3-Phenyl 93 1 3-CF.sub.3-Phenyl 94 2 3-CF.sub.3-Phenyl 95 3 3-CF.sub.3-Phenyl 96 4 3-CF.sub.3-Phenyl 97 1 2-CF.sub.3-Phenyl 98 2 2-CF.sub.3-Phenyl 99 3 2-CF.sub.3-Phenyl 100 4 2-CF.sub.3-Phenyl 101 1 4-iPr-Phenyl 102 2 4-iPr-Phenyl 103 3 4-iPr-Phenyl 104 4 4-iPr-Phenyl 105 1 3-iPr-Phenyl 106 2 3-iPr-Phenyl 107 3 3-iPr-Phenyl 108 4 3-iPr-Phenyl 109 1 2-iPr-Phenyl 110 2 2-iPr-Phenyl 111 3 2-iPr-Phenyl 112 4 2-iPr-Phenyl 113 1 4-NH.sub.2-Phenyl 114 2 4-NH.sub.2-Phenyl 115 3 4-NH.sub.2-Phenyl 116 4 4-NH.sub.2-Phenyl 117 1 3-NH.sub.2-Phenyl 118 2 3-NH.sub.2-Phenyl 119 3 3-NH.sub.2-Phenyl 120 4 3-NH.sub.2-Phenyl 121 1 2-NH.sub.2-Phenyl 122 2 2-NH.sub.2-Phenyl 123 3 2-NH.sub.2-Phenyl 124 4 2-NH.sub.2-Phenyl 125 1 2,3-di-Me-Phenyl 126 2 2,3-di-Me-Phenyl 127 3 2,3-di-Me-Phenyl 128 4 2,3-di-Me-Phenyl 129 1 2,4-di-Me-Phenyl 130 2 2,4-di-Me-Phenyl 131 3 2,4-di-Me-Phenyl 132 4 2,4-di-Me-Phenyl 133 1 2,5-di-Me-Phenyl 134 2 2,5-di-Me-Phenyl 135 3 2,5-di-Me-Phenyl 136 4 2,5-di-Me-Phenyl 137 1 2,6-di-Me-Phenyl 138 2 2,6-di-Me-Phenyl 139 3 2,6-di-Me-Phenyl 140 4 2,6-di-Me-Phenyl 141 1 2,6-di-iPr-Phenyl 142 2 2,6-di-iPr-Phenyl 143 3 2,6-di-iPr-Phenyl 144 4 2,6-di-iPr-Phenyl 145 1 2-morpholino-phenyl 146 2 2-morpholino-phenyl 147 3 2-morpholino-phenyl 148 4 2-morpholino-phenyl 149 1 3-morpholino-phenyl 150 2 3-morpholino-phenyl 151 3 3-morpholino-phenyl 152 4 3-morpholino-phenyl 153 1 4-morpholino-phenyl 154 2 4-morpholino-phenyl 155 3 4-morpholino-phenyl 156 4 4-morpholino-phenyl 157 1 4-CN-2-morpholino-phenyl 158 2 4-CN-2-morpholino-phenyl 159 3 4-CN-2-morpholino-phenyl 160 4 4-CN-2-morpholino-phenyl 161 1 4-CH.sub.3-2-morpholino-phenyl 162 2 4-CH.sub.3-2-morpholino-phenyl 163 3 4-CH.sub.3-2-morpholino-phenyl 164 4 4-CH.sub.3-2-morpholino-phenyl 165 1 4-OH-2-morpholino-phenyl 166 2 4-OH-2-morpholino-phenyl 167 3 4-OH-2-morpholino-phenyl 168 4 4-OH-2-morpholino-phenyl 173 1 naphthylen-2-yl 174 2 naphthylen-2-yl 175 3 naphthylen-2-yl 176 4 naphthylen-2-yl

    [2004] Exemplary embodiments include compounds having the formula (XII)

    ##STR00427##

    [2005] or a pharmaceutically acceptable salt form thereof defined herein below in Table 6.

    TABLE-US-00006 TABLE 6 Entry R.sup.1 R.sup.2 n R.sup.4 1 Methyl Methyl 1 Phenyl 2 Methyl Methyl 2 Phenyl 3 Methyl Methyl 3 Phenyl 4 Methyl Methyl 4 Phenyl 5 Methyl Methyl 1 4-OH-Phenyl 6 Methyl Methyl 2 4-OH-Phenyl 7 Methyl Methyl 3 4-OH-Phenyl 8 Methyl Methyl 4 4-OH-Phenyl 9 Methyl Methyl 1 3-OH-Phenyl 10 Methyl Methyl 2 3-OH-Phenyl 11 Methyl Methyl 3 3-OH-Phenyl 12 Methyl Methyl 4 3-OH-Phenyl 13 Methyl Methyl 1 2-OH-Phenyl 14 Methyl Methyl 2 2-OH-Phenyl 15 Methyl Methyl 3 2-OH-Phenyl 16 Methyl Methyl 4 2-OH-Phenyl 17 Methyl Methyl 1 4-OMe-Phenyl 18 Methyl Methyl 2 4-OMe-Phenyl 19 Methyl Methyl 3 4-OMe-Phenyl 20 Methyl Methyl 4 4-OMe-Phenyl 21 Methyl Methyl 1 3-OMe-Phenyl 22 Methyl Methyl 2 3-OMe-Phenyl 23 Methyl Methyl 3 3-OMe-Phenyl 24 Methyl Methyl 4 3-OMe-Phenyl 25 Methyl Methyl 1 2-OMe-Phenyl 26 Methyl Methyl 2 2-OMe-Phenyl 27 Methyl Methyl 3 2-OMe-Phenyl 28 Methyl Methyl 4 2-OMe-Phenyl 29 Methyl Methyl 1 4-CN-Phenyl 30 Methyl Methyl 2 4-CN-Phenyl 31 Methyl Methyl 3 4-CN-Phenyl 32 Methyl Methyl 4 4-CN-Phenyl 33 Methyl Methyl 1 3-CN-Phenyl 34 Methyl Methyl 2 3-CN-Phenyl 35 Methyl Methyl 3 3-CN-Phenyl 36 Methyl Methyl 4 3-CN-Phenyl 37 Methyl Methyl 1 2-CN-Phenyl 38 Methyl Methyl 2 2-CN-Phenyl 39 Methyl Methyl 3 2-CN-Phenyl 40 Methyl Methyl 4 2-CN-Phenyl 41 Methyl Methyl 1 4-Me-Phenyl 42 Methyl Methyl 2 4-Me-Phenyl 43 Methyl Methyl 3 4-Me-Phenyl 44 Methyl Methyl 4 4-Me-Phenyl 45 Methyl Methyl 1 3-Me-Phenyl 46 Methyl Methyl 2 3-Me-Phenyl 47 Methyl Methyl 3 3-Me-Phenyl 48 Methyl Methyl 4 3-Me-Phenyl 49 Methyl Methyl 1 2-Me-Phenyl 50 Methyl Methyl 2 2-Me-Phenyl 51 Methyl Methyl 3 2-Me-Phenyl 52 Methyl Methyl 4 2-Me-Phenyl 53 Methyl Methyl 1 4-F-Phenyl 54 Methyl Methyl 2 4-F-Phenyl 55 Methyl Methyl 3 4-F-Phenyl 56 Methyl Methyl 4 4-F-Phenyl 57 Methyl Methyl 1 3-F-Phenyl 58 Methyl Methyl 2 3-F-Phenyl 59 Methyl Methyl 3 3-F-Phenyl 60 Methyl Methyl 4 3-F-Phenyl 61 Methyl Methyl 1 2-F-Phenyl 62 Methyl Methyl 2 2-F-Phenyl 63 Methyl Methyl 3 2-F-Phenyl 64 Methyl Methyl 4 2-F-Phenyl 65 Methyl Methyl 1 4-Cl-Phenyl 66 Methyl Methyl 2 4-Cl-Phenyl 67 Methyl Methyl 3 4-Cl-Phenyl 68 Methyl Methyl 4 4-Cl-Phenyl 69 Methyl Methyl 1 3-Cl-Phenyl 70 Methyl Methyl 2 3-Cl-Phenyl 71 Methyl Methyl 3 3-Cl-Phenyl 72 Methyl Methyl 4 3-Cl-Phenyl 73 Methyl Methyl 1 2-Cl-Phenyl 74 Methyl Methyl 2 2-Cl-Phenyl 75 Methyl Methyl 3 2-Cl-Phenyl 76 Methyl Methyl 4 2-Cl-Phenyl 77 Methyl Methyl 1 4-Br-Phenyl 78 Methyl Methyl 2 4-Br-Phenyl 79 Methyl Methyl 3 4-Br-Phenyl 80 Methyl Methyl 4 4-Br-Phenyl 81 Methyl Methyl 1 3-Br-Phenyl 82 Methyl Methyl 2 3-Br-Phenyl 83 Methyl Methyl 3 3-Br-Phenyl 84 Methyl Methyl 4 3-Br-Phenyl 85 Methyl Methyl 1 2-Br-Phenyl 86 Methyl Methyl 2 2-Br-Phenyl 87 Methyl Methyl 3 2-Br-Phenyl 88 Methyl Methyl 4 2-Br-Phenyl 89 Methyl Methyl 1 4-CF.sub.3-Phenyl 90 Methyl Methyl 2 4-CF.sub.3-Phenyl 91 Methyl Methyl 3 4-CF.sub.3-Phenyl 92 Methyl Methyl 4 4-CF.sub.3-Phenyl 93 Methyl Methyl 1 3-CF.sub.3-Phenyl 94 Methyl Methyl 2 3-CF.sub.3-Phenyl 95 Methyl Methyl 3 3-CF.sub.3-Phenyl 96 Methyl Methyl 4 3-CF.sub.3-Phenyl 97 Methyl Methyl 1 2-CF.sub.3-Phenyl 98 Methyl Methyl 2 2-CF.sub.3-Phenyl 99 Methyl Methyl 3 2-CF.sub.3-Phenyl 100 Methyl Methyl 4 2-CF.sub.3-Phenyl 101 Methyl Methyl 1 4-iPr-Phenyl 102 Methyl Methyl 2 4-iPr-Phenyl 103 Methyl Methyl 3 4-iPr-Phenyl 104 Methyl Methyl 4 4-iPr-Phenyl 105 Methyl Methyl 1 3-iPr-Phenyl 106 Methyl Methyl 2 3-iPr-Phenyl 107 Methyl Methyl 3 3-iPr-Phenyl 108 Methyl Methyl 4 3-iPr-Phenyl 109 Methyl Methyl 1 2-iPr-Phenyl 110 Methyl Methyl 2 2-iPr-Phenyl 111 Methyl Methyl 3 2-iPr-Phenyl 112 Methyl Methyl 4 2-iPr-Phenyl 113 Methyl Methyl 1 4-NH.sub.2-Phenyl 114 Methyl Methyl 2 4-NH.sub.2-Phenyl 115 Methyl Methyl 3 4-NH.sub.2-Phenyl 116 Methyl Methyl 4 4-NH.sub.2-Phenyl 117 Methyl Methyl 1 3-NH.sub.2-Phenyl 118 Methyl Methyl 2 3-NH.sub.2-Phenyl 119 Methyl Methyl 3 3-NH.sub.2-Phenyl 120 Methyl Methyl 4 3-NH.sub.2-Phenyl 121 Methyl Methyl 1 2-NH.sub.2-Phenyl 122 Methyl Methyl 2 2-NH.sub.2-Phenyl 123 Methyl Methyl 3 2-NH.sub.2-Phenyl 124 Methyl Methyl 4 2-NH.sub.2-Phenyl 125 Methyl Methyl 1 2,3-di-Me-Phenyl 126 Methyl Methyl 2 2,3-di-Me-Phenyl 127 Methyl Methyl 3 2,3-di-Me-Phenyl 128 Methyl Methyl 4 2,3-di-Me-Phenyl 129 Methyl Methyl 1 2,4-di-Me-Phenyl 130 Methyl Methyl 2 2,4-di-Me-Phenyl 131 Methyl Methyl 3 2,4-di-Me-Phenyl 132 Methyl Methyl 4 2,4-di-Me-Phenyl 133 Methyl Methyl 1 2,5-di-Me-Phenyl 134 Methyl Methyl 2 2,5-di-Me-Phenyl 135 Methyl Methyl 3 2,5-di-Me-Phenyl 136 Methyl Methyl 4 2,5-di-Me-Phenyl 137 Methyl Methyl 1 2,6-di-Me-Phenyl 138 Methyl Methyl 2 2,6-di-Me-Phenyl 139 Methyl Methyl 3 2,6-di-Me-Phenyl 140 Methyl Methyl 4 2,6-di-Me-Phenyl 141 Methyl Methyl 1 2,6-di-iPr-Phenyl 142 Methyl Methyl 2 2,6-di-iPr-Phenyl 143 Methyl Methyl 3 2,6-di-iPr-Phenyl 144 Methyl Methyl 4 2,6-di-iPr-Phenyl 145 Methyl Methyl 1 2-morpholino-phenyl 146 Methyl Methyl 2 2-morpholino-phenyl 147 Methyl Methyl 3 2-morpholino-phenyl 148 Methyl Methyl 4 2-morpholino-phenyl 149 Methyl Methyl 1 3-morpholino-phenyl 150 Methyl Methyl 2 3-morpholino-phenyl 151 Methyl Methyl 3 3-morpholino-phenyl 152 Methyl Methyl 4 3-morpholino-phenyl 153 Methyl Methyl 1 4-morpholino-phenyl 154 Methyl Methyl 2 4-morpholino-phenyl 155 Methyl Methyl 3 4-morpholino-phenyl 156 Methyl Methyl 4 4-morpholino-phenyl 157 Methyl Methyl 1 4-CN-2-morpholino-phenyl 158 Methyl Methyl 2 4-CN-2-morpholino-phenyl 159 Methyl Methyl 3 4-CN-2-morpholino-phenyl 160 Methyl Methyl 4 4-CN-2-morpholino-phenyl 161 Methyl Methyl 1 4-CH.sub.3-2-morpholino-phenyl 162 Methyl Methyl 2 4-CH.sub.3-2-morpholino-phenyl 163 Methyl Methyl 3 4-CH.sub.3-2-morpholino-phenyl 164 Methyl Methyl 4 4-CH.sub.3-2-morpholino-phenyl 165 Methyl Methyl 1 4-OH-2-morpholino-phenyl 166 Methyl Methyl 2 4-OH-2-morpholino-phenyl 167 Methyl Methyl 3 4-OH-2-morpholino-phenyl 168 Methyl Methyl 4 4-OH-2-morpholino-phenyl 169 Methyl Methyl 1 naphthylen-1-yl 170 Methyl Methyl 2 naphthylen-1-yl 171 Methyl Methyl 3 naphthylen-1-yl 172 Methyl Methyl 4 naphthylen-1-yl 173 Methyl Methyl 1 naphthylen-2-yl 174 Methyl Methyl 2 naphthylen-2-yl 175 Methyl Methyl 3 naphthylen-2-yl 176 Methyl Methyl 4 naphthylen-2-yl 177 Ethyl Ethyl 1 Phenyl 178 Ethyl Ethyl 2 Phenyl 179 Ethyl Ethyl 3 Phenyl 180 Ethyl Ethyl 4 Phenyl 181 Ethyl Ethyl 1 4-OH-Phenyl 182 Ethyl Ethyl 2 4-OH-Phenyl 183 Ethyl Ethyl 3 4-OH-Phenyl 184 Ethyl Ethyl 4 4-OH-Phenyl 185 Ethyl Ethyl 1 3-OH-Phenyl 186 Ethyl Ethyl 2 3-OH-Phenyl 187 Ethyl Ethyl 3 3-OH-Phenyl 188 Ethyl Ethyl 4 3-OH-Phenyl 189 Ethyl Ethyl 1 2-OH-Phenyl 190 Ethyl Ethyl 2 2-OH-Phenyl 191 Ethyl Ethyl 3 2-OH-Phenyl 192 Ethyl Ethyl 4 2-OH-Phenyl 193 Ethyl Ethyl 1 4-OMe-Phenyl 194 Ethyl Ethyl 2 4-OMe-Phenyl 195 Ethyl Ethyl 3 4-OMe-Phenyl 196 Ethyl Ethyl 4 4-OMe-Phenyl 197 Ethyl Ethyl 1 3-OMe-Phenyl 198 Ethyl Ethyl 2 3-OMe-Phenyl 199 Ethyl Ethyl 3 3-OMe-Phenyl 200 Ethyl Ethyl 4 3-OMe-Phenyl 201 Ethyl Ethyl 1 2-OMe-Phenyl 202 Ethyl Ethyl 2 2-OMe-Phenyl 203 Ethyl Ethyl 3 2-OMe-Phenyl 204 Ethyl Ethyl 4 2-OMe-Phenyl 205 Ethyl Ethyl 1 4-CN-Phenyl 206 Ethyl Ethyl 2 4-CN-Phenyl 207 Ethyl Ethyl 3 4-CN-Phenyl 208 Ethyl Ethyl 4 4-CN-Phenyl 209 Ethyl Ethyl 1 3-CN-Phenyl 210 Ethyl Ethyl 2 3-CN-Phenyl 211 Ethyl Ethyl 3 3-CN-Phenyl 212 Ethyl Ethyl 4 3-CN-Phenyl 213 Ethyl Ethyl 1 2-CN-Phenyl 214 Ethyl Ethyl 2 2-CN-Phenyl 215 Ethyl Ethyl 3 2-CN-Phenyl 216 Ethyl Ethyl 4 2-CN-Phenyl 217 Ethyl Ethyl 1 4-Me-Phenyl 218 Ethyl Ethyl 2 4-Me-Phenyl 219 Ethyl Ethyl 3 4-Me-Phenyl 220 Ethyl Ethyl 4 4-Me-Phenyl 221 Ethyl Ethyl 1 3-Me-Phenyl 222 Ethyl Ethyl 2 3-Me-Phenyl 223 Ethyl Ethyl 3 3-Me-Phenyl 224 Ethyl Ethyl 4 3-Me-Phenyl 225 Ethyl Ethyl 1 2-Me-Phenyl 226 Ethyl Ethyl 2 2-Me-Phenyl 227 Ethyl Ethyl 3 2-Me-Phenyl 228 Ethyl Ethyl 4 2-Me-Phenyl 229 Ethyl Ethyl 1 4-F-Phenyl 230 Ethyl Ethyl 2 4-F-Phenyl 231 Ethyl Ethyl 3 4-F-Phenyl 232 Ethyl Ethyl 4 4-F-Phenyl 233 Ethyl Ethyl 1 3-F-Phenyl 234 Ethyl Ethyl 2 3-F-Phenyl 235 Ethyl Ethyl 3 3-F-Phenyl 236 Ethyl Ethyl 4 3-F-Phenyl 237 Ethyl Ethyl 1 2-F-Phenyl 238 Ethyl Ethyl 2 2-F-Phenyl 239 Ethyl Ethyl 3 2-F-Phenyl 240 Ethyl Ethyl 4 2-F-Phenyl 241 Ethyl Ethyl 1 4-Cl-Phenyl 242 Ethyl Ethyl 2 4-Cl-Phenyl 243 Ethyl Ethyl 3 4-Cl-Phenyl 244 Ethyl Ethyl 4 4-Cl-Phenyl 245 Ethyl Ethyl 1 3-Cl-Phenyl 246 Ethyl Ethyl 2 3-Cl-Phenyl 247 Ethyl Ethyl 3 3-Cl-Phenyl 248 Ethyl Ethyl 4 3-Cl-Phenyl 249 Ethyl Ethyl 1 2-Cl-Phenyl 250 Ethyl Ethyl 2 2-Cl-Phenyl 251 Ethyl Ethyl 3 2-Cl-Phenyl 252 Ethyl Ethyl 4 2-Cl-Phenyl 253 Ethyl Ethyl 1 4-Br-Phenyl 254 Ethyl Ethyl 2 4-Br-Phenyl 255 Ethyl Ethyl 3 4-Br-Phenyl 256 Ethyl Ethyl 4 4-Br-Phenyl 257 Ethyl Ethyl 1 3-Br-Phenyl 258 Ethyl Ethyl 2 3-Br-Phenyl 259 Ethyl Ethyl 3 3-Br-Phenyl 260 Ethyl Ethyl 4 3-Br-Phenyl 261 Ethyl Ethyl 1 2-Br-Phenyl 262 Ethyl Ethyl 2 2-Br-Phenyl 263 Ethyl Ethyl 3 2-Br-Phenyl 264 Ethyl Ethyl 4 2-Br-Phenyl 265 Ethyl Ethyl 1 4-CF.sub.3-Phenyl 266 Ethyl Ethyl 2 4-CF.sub.3-Phenyl 267 Ethyl Ethyl 3 4-CF.sub.3-Phenyl 268 Ethyl Ethyl 4 4-CF.sub.3-Phenyl 269 Ethyl Ethyl 1 3-CF.sub.3-Phenyl 270 Ethyl Ethyl 2 3-CF.sub.3-Phenyl 271 Ethyl Ethyl 3 3-CF.sub.3-Phenyl 272 Ethyl Ethyl 4 3-CF.sub.3-Phenyl 273 Ethyl Ethyl 1 2-CF.sub.3-Phenyl 274 Ethyl Ethyl 2 2-CF.sub.3-Phenyl 275 Ethyl Ethyl 3 2-CF.sub.3-Phenyl 276 Ethyl Ethyl 4 2-CF.sub.3-Phenyl 277 Ethyl Ethyl 1 4-iPr-Phenyl 278 Ethyl Ethyl 2 4-iPr-Phenyl 279 Ethyl Ethyl 3 4-iPr-Phenyl 280 Ethyl Ethyl 4 4-iPr-Phenyl 281 Ethyl Ethyl 1 3-iPr-Phenyl 282 Ethyl Ethyl 2 3-iPr-Phenyl 283 Ethyl Ethyl 3 3-iPr-Phenyl 284 Ethyl Ethyl 4 3-iPr-Phenyl 285 Ethyl Ethyl 1 2-iPr-Phenyl 286 Ethyl Ethyl 2 2-iPr-Phenyl 287 Ethyl Ethyl 3 2-iPr-Phenyl 288 Ethyl Ethyl 4 2-iPr-Phenyl 289 Ethyl Ethyl 1 4-NH.sub.2-Phenyl 290 Ethyl Ethyl 2 4-NH.sub.2-Phenyl 291 Ethyl Ethyl 3 4-NH.sub.2-Phenyl 292 Ethyl Ethyl 4 4-NH.sub.2-Phenyl 293 Ethyl Ethyl 1 3-NH.sub.2-Phenyl 294 Ethyl Ethyl 2 3-NH.sub.2-Phenyl 295 Ethyl Ethyl 3 3-NH.sub.2-Phenyl 296 Ethyl Ethyl 4 3-NH.sub.2-Phenyl 297 Ethyl Ethyl 1 2-NH.sub.2-Phenyl 298 Ethyl Ethyl 2 2-NH.sub.2-Phenyl 299 Ethyl Ethyl 3 2-NH.sub.2-Phenyl 300 Ethyl Ethyl 4 2-NH.sub.2-Phenyl 301 Ethyl Ethyl 1 2,3-di-Me-Phenyl 302 Ethyl Ethyl 2 2,3-di-Me-Phenyl 303 Ethyl Ethyl 3 2,3-di-Me-Phenyl 304 Ethyl Ethyl 4 2,3-di-Me-Phenyl 305 Ethyl Ethyl 1 2,4-di-Me-Phenyl 306 Ethyl Ethyl 2 2,4-di-Me-Phenyl 307 Ethyl Ethyl 3 2,4-di-Me-Phenyl 308 Ethyl Ethyl 4 2,4-di-Me-Phenyl 309 Ethyl Ethyl 1 2,5-di-Me-Phenyl 310 Ethyl Ethyl 2 2,5-di-Me-Phenyl 311 Ethyl Ethyl 3 2,5-di-Me-Phenyl 312 Ethyl Ethyl 4 2,5-di-Me-Phenyl 313 Ethyl Ethyl 1 2,6-di-Me-Phenyl 314 Ethyl Ethyl 2 2,6-di-Me-Phenyl 315 Ethyl Ethyl 3 2,6-di-Me-Phenyl 316 Ethyl Ethyl 4 2,6-di-Me-Phenyl 317 Ethyl Ethyl 1 2,6-di-iPr-Phenyl 318 Ethyl Ethyl 2 2,6-di-iPr-Phenyl 319 Ethyl Ethyl 3 2,6-di-iPr-Phenyl 320 Ethyl Ethyl 4 2,6-di-iPr-Phenyl 321 Ethyl Ethyl 1 2-morpholino-phenyl 322 Ethyl Ethyl 2 2-morpholino-phenyl 323 Ethyl Ethyl 3 2-morpholino-phenyl 324 Ethyl Ethyl 4 2-morpholino-phenyl 325 Ethyl Ethyl 1 3-morpholino-phenyl 326 Ethyl Ethyl 2 3-morpholino-phenyl 327 Ethyl Ethyl 3 3-morpholino-phenyl 328 Ethyl Ethyl 4 3-morpholino-phenyl 329 Ethyl Ethyl 1 4-morpholino-phenyl 330 Ethyl Ethyl 2 4-morpholino-phenyl 331 Ethyl Ethyl 3 4-morpholino-phenyl 332 Ethyl Ethyl 4 4-morpholino-phenyl 333 Ethyl Ethyl 1 4-CN-2-morpholino-phenyl 334 Ethyl Ethyl 2 4-CN-2-morpholino-phenyl 335 Ethyl Ethyl 3 4-CN-2-morpholino-phenyl 336 Ethyl Ethyl 4 4-CN-2-morpholino-phenyl 337 Ethyl Ethyl 1 4-CH.sub.3-2-morpholino-phenyl 338 Ethyl Ethyl 2 4-CH.sub.3-2-morpholino-phenyl 339 Ethyl Ethyl 3 4-CH.sub.3-2-morpholino-phenyl 340 Ethyl Ethyl 4 4-CH.sub.3-2-morpholino-phenyl 341 Ethyl Ethyl 1 4-OH-2-morpholino-phenyl 342 Ethyl Ethyl 2 4-OH-2-morpholino-phenyl 343 Ethyl Ethyl 3 4-OH-2-morpholino-phenyl 344 Ethyl Ethyl 4 4-OH-2-morpholino-phenyl 345 Ethyl Ethyl 1 naphthylen-1-yl 346 Ethyl Ethyl 2 naphthylen-1-yl 347 Ethyl Ethyl 3 naphthylen-1-yl 348 Ethyl Ethyl 4 naphthylen-2-yl 349 Ethyl Ethyl 1 naphthylen-2-yl 350 Ethyl Ethyl 2 naphthylen-2-yl 351 Ethyl Ethyl 3 naphthylen-2-yl 352 Ethyl Ethyl 4 naphthylen-2-yl

    [2006] Exemplary embodiments include compounds having the formula (XIII)

    ##STR00428##

    [2007] or a pharmaceutically acceptable salt form thereof defined herein below in Table 7

    TABLE-US-00007 TABLE 7 Entry n R.sup.4 1 1 Phenyl 2 2 Phenyl 3 3 Phenyl 4 4 Phenyl 5 1 4-OH-Phenyl 6 2 4-OH-Phenyl 7 3 4-OH-Phenyl 8 4 4-OH-Phenyl 9 1 3-OH-Phenyl 10 2 3-OH-Phenyl 11 3 3-OH-Phenyl 12 4 3-OH-Phenyl 13 1 2-OH-Phenyl 14 2 2-OH-Phenyl 15 3 2-OH-Phenyl 16 4 2-OH-Phenyl 17 1 4-OMe-Phenyl 18 2 4-OMe-Phenyl 19 3 4-OMe-Phenyl 20 4 4-OMe-Phenyl 21 1 3-OMe-Phenyl 22 2 3-OMe-Phenyl 23 3 3-OMe-Phenyl 24 4 3-OMe-Phenyl 25 1 2-OMe-Phenyl 26 2 2-OMe-Phenyl 27 3 2-OMe-Phenyl 28 4 2-OMe-Phenyl 29 1 4-CN-Phenyl 30 2 4-CN-Phenyl 31 3 4-CN-Phenyl 32 4 4-CN-Phenyl 33 1 3-CN-Phenyl 34 2 3-CN-Phenyl 35 3 3-CN-Phenyl 36 4 3-CN-Phenyl 37 1 2-CN-Phenyl 38 2 2-CN-Phenyl 39 3 2-CN-Phenyl 40 4 2-CN-Phenyl 41 1 4-Me-Phenyl 42 2 4-Me-Phenyl 43 3 4-Me-Phenyl 44 4 4-Me-Phenyl 45 1 3-Me-Phenyl 46 2 3-Me-Phenyl 47 3 3-Me-Phenyl 48 4 3-Me-Phenyl 49 1 2-Me-Phenyl 50 2 2-Me-Phenyl 51 3 2-Me-Phenyl 52 4 2-Me-Phenyl 53 1 4-F-Phenyl 54 2 4-F-Phenyl 55 3 4-F-Phenyl 56 4 4-F-Phenyl 57 1 3-F-Phenyl 58 2 3-F-Phenyl 59 3 3-F-Phenyl 60 4 3-F-Phenyl 61 1 2-F-Phenyl 62 2 2-F-Phenyl 63 3 2-F-Phenyl 64 4 2-F-Phenyl 65 1 4-Cl-Phenyl 66 2 4-Cl-Phenyl 67 3 4-Cl-Phenyl 68 4 4-Cl-Phenyl 69 1 3-Cl-Phenyl 70 2 3-Cl-Phenyl 71 3 3-Cl-Phenyl 72 4 3-Cl-Phenyl 73 1 2-Cl-Phenyl 74 2 2-Cl-Phenyl 75 3 2-Cl-Phenyl 76 4 2-Cl-Phenyl 77 1 4-Br-Phenyl 78 2 4-Br-Phenyl 79 3 4-Br-Phenyl 80 4 4-Br-Phenyl 81 1 3-Br-Phenyl 82 2 3-Br-Phenyl 83 3 3-Br-Phenyl 84 4 3-Br-Phenyl 85 1 naphthylen-1-yl 86 2 naphthylen-1-yl 87 3 naphthylen-1-yl 88 4 naphthylen-1-yl 85 1 2-Br-Phenyl 86 2 2-Br-Phenyl 87 3 2-Br-Phenyl 88 4 2-Br-Phenyl 89 1 4-CF.sub.3-Phenyl 90 2 4-CF.sub.3-Phenyl 91 3 4-CF.sub.3-Phenyl 92 4 4-CF.sub.3-Phenyl 93 1 3-CF.sub.3-Phenyl 94 2 3-CF.sub.3-Phenyl 95 3 3-CF.sub.3-Phenyl 96 4 3-CF.sub.3-Phenyl 97 1 2-CF.sub.3-Phenyl 98 2 2-CF.sub.3-Phenyl 99 3 2-CF.sub.3-Phenyl 100 4 2-CF.sub.3-Phenyl 101 1 4-iPr-Phenyl 102 2 4-iPr-Phenyl 103 3 4-iPr-Phenyl 104 4 4-iPr-Phenyl 105 1 3-iPr-Phenyl 106 2 3-iPr-Phenyl 107 3 3-iPr-Phenyl 108 4 3-iPr-Phenyl 109 1 2-iPr-Phenyl 110 2 2-iPr-Phenyl 111 3 2-iPr-Phenyl 112 4 2-iPr-Phenyl 113 1 4-NH.sub.2-Phenyl 114 2 4-NH.sub.2-Phenyl 115 3 4-NH.sub.2-Phenyl 116 4 4-NH.sub.2-Phenyl 117 1 3-NH.sub.2-Phenyl 118 2 3-NH.sub.2-Phenyl 119 3 3-NH.sub.2-Phenyl 120 4 3-NH.sub.2-Phenyl 121 1 2-NH.sub.2-Phenyl 122 2 2-NH.sub.2-Phenyl 123 3 2-NH.sub.2-Phenyl 124 4 2-NH.sub.2-Phenyl 125 1 2,3-di-Me-Phenyl 126 2 2,3-di-Me-Phenyl 127 3 2,3-di-Me-Phenyl 128 4 2,3-di-Me-Phenyl 129 1 2,4-di-Me-Phenyl 130 2 2,4-di-Me-Phenyl 131 3 2,4-di-Me-Phenyl 132 4 2,4-di-Me-Phenyl 133 1 2,5-di-Me-Phenyl 134 2 2,5-di-Me-Phenyl 135 3 2,5-di-Me-Phenyl 136 4 2,5-di-Me-Phenyl 137 1 2,6-di-Me-Phenyl 138 2 2,6-di-Me-Phenyl 139 3 2,6-di-Me-Phenyl 140 4 2,6-di-Me-Phenyl 141 1 2,6-di-iPr-Phenyl 142 2 2,6-di-iPr-Phenyl 143 3 2,6-di-iPr-Phenyl 144 4 2,6-di-iPr-Phenyl 145 1 2-morpholino-phenyl 146 2 2-morpholino-phenyl 147 3 2-morpholino-phenyl 148 4 2-morpholino-phenyl 149 1 3-morpholino-phenyl 150 2 3-morpholino-phenyl 151 3 3-morpholino-phenyl 152 4 3-morpholino-phenyl 153 1 4-morpholino-phenyl 154 2 4-morpholino-phenyl 155 3 4-morpholino-phenyl 156 4 4-morpholino-phenyl 157 1 4-CN-2-morpholino-phenyl 158 2 4-CN-2-morpholino-phenyl 159 3 4-CN-2-morpholino-phenyl 160 4 4-CN-2-morpholino-phenyl 161 1 4-CH.sub.3-2-morpholino-phenyl 162 2 4-CH.sub.3-2-morpholino-phenyl 163 3 4-CH.sub.3-2-morpholino-phenyl 164 4 4-CH.sub.3-2-morpholino-phenyl 165 1 4-OH-2-morpholino-phenyl 166 2 4-OH-2-morpholino-phenyl 167 3 4-OH-2-morpholino-phenyl 168 4 4-OH-2-morpholino-phenyl 173 1 naphthylen-2-yl 174 2 naphthylen-2-yl 175 3 naphthylen-2-yl 176 4 naphthylen-2-yl

    [2008] Exemplary embodiments include compounds having the formula (XIV)

    ##STR00429##

    [2009] or a pharmaceutically acceptable salt form thereof defined herein below in Table 8.

    TABLE-US-00008 TABLE 8 Entry n R.sup.4 1 1 Phenyl 2 2 Phenyl 3 3 Phenyl 4 4 Phenyl 5 1 4-OH-Phenyl 6 2 4-OH-Phenyl 7 3 4-OH-Phenyl 8 4 4-OH-Phenyl 9 1 3-OH-Phenyl 10 2 3-OH-Phenyl 11 3 3-OH-Phenyl 12 4 3-OH-Phenyl 13 1 2-OH-Phenyl 14 2 2-OH-Phenyl 15 3 2-OH-Phenyl 16 4 2-OH-Phenyl 17 1 4-OMe-Phenyl 18 2 4-OMe-Phenyl 19 3 4-OMe-Phenyl 20 4 4-OMe-Phenyl 21 1 3-OMe-Phenyl 22 2 3-OMe-Phenyl 23 3 3-OMe-Phenyl 24 4 3-OMe-Phenyl 25 1 2-OMe-Phenyl 26 2 2-OMe-Phenyl 27 3 2-OMe-Phenyl 28 4 2-OMe-Phenyl 29 1 4-CN-Phenyl 30 2 4-CN-Phenyl 31 3 4-CN-Phenyl 32 4 4-CN-Phenyl 33 1 3-CN-Phenyl 34 2 3-CN-Phenyl 35 3 3-CN-Phenyl 36 4 3-CN-Phenyl 37 1 2-CN-Phenyl 38 2 2-CN-Phenyl 39 3 2-CN-Phenyl 40 4 2-CN-Phenyl 41 1 4-Me-Phenyl 42 2 4-Me-Phenyl 43 3 4-Me-Phenyl 44 4 4-Me-Phenyl 45 1 3-Me-Phenyl 46 2 3-Me-Phenyl 47 3 3-Me-Phenyl 48 4 3-Me-Phenyl 49 1 2-Me-Phenyl 50 2 2-Me-Phenyl 51 3 2-Me-Phenyl 52 4 2-Me-Phenyl 53 1 4-F-Phenyl 54 2 4-F-Phenyl 55 3 4-F-Phenyl 56 4 4-F-Phenyl 57 1 3-F-Phenyl 58 2 3-F-Phenyl 59 3 3-F-Phenyl 60 4 3-F-Phenyl 61 1 2-F-Phenyl 62 2 2-F-Phenyl 63 3 2-F-Phenyl 64 4 2-F-Phenyl 65 1 4-Cl-Phenyl 66 2 4-Cl-Phenyl 67 3 4-Cl-Phenyl 68 4 4-Cl-Phenyl 69 1 3-Cl-Phenyl 70 2 3-Cl-Phenyl 71 3 3-Cl-Phenyl 72 4 3-Cl-Phenyl 73 1 2-Cl-Phenyl 74 2 2-Cl-Phenyl 75 3 2-Cl-Phenyl 76 4 2-Cl-Phenyl 77 1 4-Br-Phenyl 78 2 4-Br-Phenyl 79 3 4-Br-Phenyl 80 4 4-Br-Phenyl 81 1 3-Br-Phenyl 82 2 3-Br-Phenyl 83 3 3-Br-Phenyl 84 4 3-Br-Phenyl 85 1 naphthylen-1-yl 86 2 naphthylen-1-yl 87 3 naphthylen-1-yl 88 4 naphthylen-1-yl 85 1 2-Br-Phenyl 86 2 2-Br-Phenyl 87 3 2-Br-Phenyl 88 4 2-Br-Phenyl 89 1 4-CF.sub.3-Phenyl 90 2 4-CF.sub.3-Phenyl 91 3 4-CF.sub.3-Phenyl 92 4 4-CF.sub.3-Phenyl 93 1 3-CF.sub.3-Phenyl 94 2 3-CF.sub.3-Phenyl 95 3 3-CF.sub.3-Phenyl 96 4 3-CF.sub.3-Phenyl 97 1 2-CF.sub.3-Phenyl 98 2 2-CF.sub.3-Phenyl 99 3 2-CF.sub.3-Phenyl 100 4 2-CF.sub.3-Phenyl 101 1 4-iPr-Phenyl 102 2 4-iPr-Phenyl 103 3 4-iPr-Phenyl 104 4 4-iPr-Phenyl 105 1 3-iPr-Phenyl 106 2 3-iPr-Phenyl 107 3 3-iPr-Phenyl 108 4 3-iPr-Phenyl 109 1 2-iPr-Phenyl 110 2 2-iPr-Phenyl 111 3 2-iPr-Phenyl 112 4 2-iPr-Phenyl 113 1 4-NH.sub.2-Phenyl 114 2 4-NH.sub.2-Phenyl 115 3 4-NH.sub.2-Phenyl 116 4 4-NH.sub.2-Phenyl 117 1 3-NH.sub.2-Phenyl 118 2 3-NH.sub.2-Phenyl 119 3 3-NH.sub.2-Phenyl 120 4 3-NH.sub.2-Phenyl 121 1 2-NH.sub.2-Phenyl 122 2 2-NH.sub.2-Phenyl 123 3 2-NH.sub.2-Phenyl 124 4 2-NH.sub.2-Phenyl 125 1 2,3-di-Me-Phenyl 126 2 2,3-di-Me-Phenyl 127 3 2,3-di-Me-Phenyl 128 4 2,3-di-Me-Phenyl 129 1 2,4-di-Me-Phenyl 130 2 2,4-di-Me-Phenyl 131 3 2,4-di-Me-Phenyl 132 4 2,4-di-Me-Phenyl 133 1 2,5-di-Me-Phenyl 134 2 2,5-di-Me-Phenyl 135 3 2,5-di-Me-Phenyl 136 4 2,5-di-Me-Phenyl 137 1 2,6-di-Me-Phenyl 138 2 2,6-di-Me-Phenyl 139 3 2,6-di-Me-Phenyl 140 4 2,6-di-Me-Phenyl 141 1 2,6-di-iPr-Phenyl 142 2 2,6-di-iPr-Phenyl 143 3 2,6-di-iPr-Phenyl 144 4 2,6-di-iPr-Phenyl 145 1 2-morpholino-phenyl 146 2 2-morpholino-phenyl 147 3 2-morpholino-phenyl 148 4 2-morpholino-phenyl 149 1 3-morpholino-phenyl 150 2 3-morpholino-phenyl 151 3 3-morpholino-phenyl 152 4 3-morpholino-phenyl 153 1 4-morpholino-phenyl 154 2 4-morpholino-phenyl 155 3 4-morpholino-phenyl 156 4 4-morpholino-phenyl 157 1 4-CN-2-morpholino-phenyl 158 2 4-CN-2-morpholino-phenyl 159 3 4-CN-2-morpholino-phenyl 160 4 4-CN-2-morpholino-phenyl 161 1 4-CH.sub.3-2-morpholino-phenyl 162 2 4-CH.sub.3-2-morpholino-phenyl 163 3 4-CH.sub.3-2-morpholino-phenyl 164 4 4-CH.sub.3-2-morpholino-phenyl 165 1 4-OH-2-morpholino-phenyl 166 2 4-OH-2-morpholino-phenyl 167 3 4-OH-2-morpholino-phenyl 168 4 4-OH-2-morpholino-phenyl 173 1 naphthylen-2-yl 174 2 naphthylen-2-yl 175 3 naphthylen-2-yl 176 4 naphthylen-2-yl

    [2010] Exemplary embodiments include compounds having the formula (XV)

    ##STR00430##

    [2011] or a pharmaceutically acceptable salt form thereof defined herein below in Table 9.

    TABLE-US-00009 TABLE 9 Entry n R.sup.4 1 1 Phenyl 2 2 Phenyl 3 3 Phenyl 4 4 Phenyl 5 1 4-OH-Phenyl 6 2 4-OH-Phenyl 7 3 4-OH-Phenyl 8 4 4-OH-Phenyl 9 1 3-OH-Phenyl 10 2 3-OH-Phenyl 11 3 3-OH-Phenyl 12 4 3-OH-Phenyl 13 1 2-OH-Phenyl 14 2 2-OH-Phenyl 15 3 2-OH-Phenyl 16 4 2-OH-Phenyl 17 1 4-OMe-Phenyl 18 2 4-OMe-Phenyl 19 3 4-OMe-Phenyl 20 4 4-OMe-Phenyl 21 1 3-OMe-Phenyl 22 2 3-OMe-Phenyl 23 3 3-OMe-Phenyl 24 4 3-OMe-Phenyl 25 1 2-OMe-Phenyl 26 2 2-OMe-Phenyl 27 3 2-OMe-Phenyl 28 4 2-OMe-Phenyl 29 1 4-CN-Phenyl 30 2 4-CN-Phenyl 31 3 4-CN-Phenyl 32 4 4-CN-Phenyl 33 1 3-CN-Phenyl 34 2 3-CN-Phenyl 35 3 3-CN-Phenyl 36 4 3-CN-Phenyl 37 1 2-CN-Phenyl 38 2 2-CN-Phenyl 39 3 2-CN-Phenyl 40 4 2-CN-Phenyl 41 1 4-Me-Phenyl 42 2 4-Me-Phenyl 43 3 4-Me-Phenyl 44 4 4-Me-Phenyl 45 1 3-Me-Phenyl 46 2 3-Me-Phenyl 47 3 3-Me-Phenyl 48 4 3-Me-Phenyl 49 1 2-Me-Phenyl 50 2 2-Me-Phenyl 51 3 2-Me-Phenyl 52 4 2-Me-Phenyl 53 1 4-F-Phenyl 54 2 4-F-Phenyl 55 3 4-F-Phenyl 56 4 4-F-Phenyl 57 1 3-F-Phenyl 58 2 3-F-Phenyl 59 3 3-F-Phenyl 60 4 3-F-Phenyl 61 1 2-F-Phenyl 62 2 2-F-Phenyl 63 3 2-F-Phenyl 64 4 2-F-Phenyl 65 1 4-Cl-Phenyl 66 2 4-Cl-Phenyl 67 3 4-Cl-Phenyl 68 4 4-Cl-Phenyl 69 1 3-Cl-Phenyl 70 2 3-Cl-Phenyl 71 3 3-Cl-Phenyl 72 4 3-Cl-Phenyl 73 1 2-Cl-Phenyl 74 2 2-Cl-Phenyl 75 3 2-Cl-Phenyl 76 4 2-Cl-Phenyl 77 1 4-Br-Phenyl 78 2 4-Br-Phenyl 79 3 4-Br-Phenyl 80 4 4-Br-Phenyl 81 1 3-Br-Phenyl 82 2 3-Br-Phenyl 83 3 3-Br-Phenyl 84 4 3-Br-Phenyl 85 1 naphthylen-1-yl 86 2 naphthylen-1-yl 87 3 naphthylen-1-yl 88 4 naphthylen-1-yl 85 1 2-Br-Phenyl 86 2 2-Br-Phenyl 87 3 2-Br-Phenyl 88 4 2-Br-Phenyl 89 1 4-CF.sub.3-Phenyl 90 2 4-CF.sub.3-Phenyl 91 3 4-CF.sub.3-Phenyl 92 4 4-CF.sub.3-Phenyl 93 1 3-CF.sub.3-Phenyl 94 2 3-CF.sub.3-Phenyl 95 3 3-CF.sub.3-Phenyl 96 4 3-CF.sub.3-Phenyl 97 1 2-CF.sub.3-Phenyl 98 2 2-CF.sub.3-Phenyl 99 3 2-CF.sub.3-Phenyl 100 4 2-CF.sub.3-Phenyl 101 1 4-iPr-Phenyl 102 2 4-iPr-Phenyl 103 3 4-iPr-Phenyl 104 4 4-iPr-Phenyl 105 1 3-iPr-Phenyl 106 2 3-iPr-Phenyl 107 3 3-iPr-Phenyl 108 4 3-iPr-Phenyl 109 1 2-iPr-Phenyl 110 2 2-iPr-Phenyl 111 3 2-iPr-Phenyl 112 4 2-iPr-Phenyl 113 1 4-NH.sub.2-Phenyl 114 2 4-NH.sub.2-Phenyl 115 3 4-NH.sub.2-Phenyl 116 4 4-NH.sub.2-Phenyl 117 1 3-NH.sub.2-Phenyl 118 2 3-NH.sub.2-Phenyl 119 3 3-NH.sub.2-Phenyl 120 4 3-NH.sub.2-Phenyl 121 1 2-NH.sub.2-Phenyl 122 2 2-NH.sub.2-Phenyl 123 3 2-NH.sub.2-Phenyl 124 4 2-NH.sub.2-Phenyl 125 1 2,3-di-Me-Phenyl 126 2 2,3-di-Me-Phenyl 127 3 2,3-di-Me-Phenyl 128 4 2,3-di-Me-Phenyl 129 1 2,4-di-Me-Phenyl 130 2 2,4-di-Me-Phenyl 131 3 2,4-di-Me-Phenyl 132 4 2,4-di-Me-Phenyl 133 1 2,5-di-Me-Phenyl 134 2 2,5-di-Me-Phenyl 135 3 2,5-di-Me-Phenyl 136 4 2,5-di-Me-Phenyl 137 1 2,6-di-Me-Phenyl 138 2 2,6-di-Me-Phenyl 139 3 2,6-di-Me-Phenyl 140 4 2,6-di-Me-Phenyl 141 1 2,6-di-iPr-Phenyl 142 2 2,6-di-iPr-Phenyl 143 3 2,6-di-iPr-Phenyl 144 4 2,6-di-iPr-Phenyl 145 1 2-morpholino-phenyl 146 2 2-morpholino-phenyl 147 3 2-morpholino-phenyl 148 4 2-morpholino-phenyl 149 1 3-morpholino-phenyl 150 2 3-morpholino-phenyl 151 3 3-morpholino-phenyl 152 4 3-morpholino-phenyl 153 1 4-morpholino-phenyl 154 2 4-morpholino-phenyl 155 3 4-morpholino-phenyl 156 4 4-morpholino-phenyl 157 1 4-CN-2-morpholino-phenyl 158 2 4-CN-2-morpholino-phenyl 159 3 4-CN-2-morpholino-phenyl 160 4 4-CN-2-morpholino-phenyl 161 1 4-CH.sub.3-2-morpholino-phenyl 162 2 4-CH.sub.3-2-morpholino-phenyl 163 3 4-CH.sub.3-2-morpholino-phenyl 164 4 4-CH.sub.3-2-morpholino-phenyl 165 1 4-OH-2-morpholino-phenyl 166 2 4-OH-2-morpholino-phenyl 167 3 4-OH-2-morpholino-phenyl 168 4 4-OH-2-morpholino-phenyl 173 1 naphthylen-2-yl 174 2 naphthylen-2-yl 175 3 naphthylen-2-yl 176 4 naphthylen-2-yl

    [2012] Exemplary embodiments include compounds having the formula (XVI)

    ##STR00431##

    [2013] or a pharmaceutically acceptable salt form thereof defined herein below in Table 10.

    TABLE-US-00010 TABLE 10 Entry n R.sup.4 Entry n R.sup.4 1 1 Phenyl 85 1 2-Br-Phenyl 2 2 Phenyl 86 2 2-Br-Phenyl 3 3 Phenyl 87 3 2-Br-Phenyl 4 4 Phenyl 88 4 2-Br-Phenyl 5 1 4-OH-Phenyl 89 1 4-CF.sub.3-Phenyl 6 2 4-OH-Phenyl 90 2 4-CF.sub.3-Phenyl 7 3 4-OH-Phenyl 91 3 4-CF.sub.3-Phenyl 8 4 4-OH-Phenyl 92 4 4-CF.sub.3-Phenyl 9 1 3-OH-Phenyl 93 1 3-CF.sub.3-Phenyl 10 2 3-OH-Phenyl 94 2 3-CF.sub.3-Phenyl 11 3 3-OH-Phenyl 95 3 3-CF.sub.3-Phenyl 12 4 3-OH-Phenyl 96 4 3-CF.sub.3-Phenyl 13 1 2-OH-Phenyl 97 1 2-CF.sub.3-Phenyl 14 2 2-OH-Phenyl 98 2 2-CF.sub.3-Phenyl 15 3 2-OH-Phenyl 99 3 2-CF.sub.3-Phenyl 16 4 2-OH-Phenyl 100 4 2-CF.sub.3-Phenyl 17 1 4-OMe-Phenyl 101 1 4-iPr-Phenyl 18 2 4-OMe-Phenyl 102 2 4-iPr-Phenyl 19 3 4-OMe-Phenyl 103 3 4-iPr-Phenyl 20 4 4-OMe-Phenyl 104 4 4-iPr-Phenyl 21 1 3-OMe-Phenyl 105 1 3-iPr-Phenyl 22 2 3-OMe-Phenyl 106 2 3-iPr-Phenyl 23 3 3-OMe-Phenyl 107 3 3-iPr-Phenyl 24 4 3-OMe-Phenyl 108 4 3-iPr-Phenyl 25 1 2-OMe-Phenyl 109 1 2-iPr-Phenyl 26 2 2-OMe-Phenyl 110 2 2-iPr-Phenyl 27 3 2-OMe-Phenyl 111 3 2-iPr-Phenyl 28 4 2-OMe-Phenyl 112 4 2-iPr-Phenyl 29 1 4-CN-Phenyl 113 1 4-NH.sub.2-Phenyl 30 2 4-CN-Phenyl 114 2 4-NH.sub.2-Phenyl 31 3 4-CN-Phenyl 115 3 4-NH.sub.2-Phenyl 32 4 4-CN-Phenyl 116 4 4-NH.sub.2-Phenyl 33 1 3-CN-Phenyl 117 1 3-NH.sub.2-Phenyl 34 2 3-CN-Phenyl 118 2 3-NH.sub.2-Phenyl 35 3 3-CN-Phenyl 119 3 3-NH.sub.2-Phenyl 36 4 3-CN-Phenyl 120 4 3-NH.sub.2-Phenyl 37 1 2-CN-Phenyl 121 1 2-NH.sub.2-Phenyl 38 2 2-CN-Phenyl 122 2 2-NH.sub.2-Phenyl 39 3 2-CN-Phenyl 123 3 2-NH.sub.2-Phenyl 40 4 2-CN-Phenyl 124 4 2-NH.sub.2-Phenyl 41 1 4-Me-Phenyl 125 1 2,3-di-Me-Phenyl 42 2 4-Me-Phenyl 126 2 2,3-di-Me-Phenyl 43 3 4-Me-Phenyl 127 3 2,3-di-Me-Phenyl 44 4 4-Me-Phenyl 128 4 2,3-di-Me-Phenyl 45 1 3-Me-Phenyl 129 1 2,4-di-Me-Phenyl 46 2 3-Me-Phenyl 130 2 2,4-di-Me-Phenyl 47 3 3-Me-Phenyl 131 3 2,4-di-Me-Phenyl 48 4 3-Me-Phenyl 132 4 2,4-di-Me-Phenyl 49 1 2-Me-Phenyl 133 1 2,5-di-Me-Phenyl 50 2 2-Me-Phenyl 134 2 2,5-di-Me-Phenyl 51 3 2-Me-Phenyl 135 3 2,5-di-Me-Phenyl 52 4 2-Me-Phenyl 136 4 2,5-di-Me-Phenyl 53 1 4-F-Phenyl 137 1 2,6-di-Me-Phenyl 54 2 4-F-Phenyl 138 2 2,6-di-Me-Phenyl 55 3 4-F-Phenyl 139 3 2,6-di-Me-Phenyl 56 4 4-F-Phenyl 140 4 2,6-di-Me-Phenyl 57 1 3-F-Phenyl 141 1 2,6-di-iPr-Phenyl 58 2 3-F-Phenyl 142 2 2,6-di-iPr-Phenyl 59 3 3-F-Phenyl 143 3 2,6-di-iPr-Phenyl 60 4 3-F-Phenyl 144 4 2,6-di-iPr-Phenyl 61 1 2-F-Phenyl 145 1 2-morpholino-phenyl 62 2 2-F-Phenyl 146 2 2-morpholino-phenyl 63 3 2-F-Phenyl 147 3 2-morpholino-phenyl 64 4 2-F-Phenyl 148 4 2-morpholino-phenyl 65 1 4-Cl-Phenyl 149 1 3-morpholino-phenyl 66 2 4-Cl-Phenyl 150 2 3-morpholino-phenyl 67 3 4-Cl-Phenyl 151 3 3-morpholino-phenyl 68 4 4-Cl-Phenyl 152 4 3-morpholino-phenyl 69 1 3-Cl-Phenyl 153 1 4-morpholino-phenyl 70 2 3-Cl-Phenyl 154 2 4-morpholino-phenyl 71 3 3-Cl-Phenyl 155 3 4-morpholino-phenyl 72 4 3-Cl-Phenyl 156 4 4-morpholino-phenyl 73 1 2-Cl-Phenyl 157 1 4-CN-2-morpholino-phenyl 74 2 2-Cl-Phenyl 158 2 4-CN-2-morpholino-phenyl 75 3 2-Cl-Phenyl 159 3 4-CN-2-morpholino-phenyl 76 4 2-Cl-Phenyl 160 4 4-CN-2-morpholino-phenyl 77 1 4-Br-Phenyl 161 1 4-CH.sub.3-2-morpholino-phenyl 78 2 4-Br-Phenyl 162 2 4-CH.sub.3-2-morpholino-phenyl 79 3 4-Br-Phenyl 163 3 4-CH.sub.3-2-morpholino-phenyl 80 4 4-Br-Phenyl 164 4 4-CH.sub.3-2-morpholino-phenyl 81 1 3-Br-Phenyl 165 1 4-OH-2-morpholino-phenyl 82 2 3-Br-Phenyl 166 2 4-OH-2-morpholino-phenyl 83 3 3-Br-Phenyl 167 3 4-OH-2-morpholino-phenyl 84 4 3-Br-Phenyl 168 4 4-OH-2-morpholino-phenyl 85 1 naphthylen-1-yl 173 1 naphthylen-2-yl 86 2 naphthylen-1-yl 174 2 naphthylen-2-yl 87 3 naphthylen-1-yl 175 3 naphthylen-2-yl 88 4 naphthylen-1-yl 176 4 naphthylen-2-yl

    [2014] Exemplary embodiments include compounds having the formula (XVII)

    ##STR00432##

    [2015] or a pharmaceutically acceptable salt form thereof defined herein below in Table 11.

    TABLE-US-00011 TABLE 11 Entry R.sup.1 R.sup.2 n R.sup.5 1 Methyl Methyl 1 Phenyl 2 Methyl Methyl 2 Phenyl 3 Methyl Methyl 3 Phenyl 4 Methyl Methyl 4 Phenyl 5 Methyl Methyl 1 4-OH-Phenyl 6 Methyl Methyl 2 4-OH-Phenyl 7 Methyl Methyl 3 4-OH-Phenyl 8 Methyl Methyl 4 4-OH-Phenyl 9 Methyl Methyl 1 3-OH-Phenyl 10 Methyl Methyl 2 3-OH-Phenyl 11 Methyl Methyl 3 3-OH-Phenyl 12 Methyl Methyl 4 3-OH-Phenyl 13 Methyl Methyl 1 2-OH-Phenyl 14 Methyl Methyl 2 2-OH-Phenyl 15 Methyl Methyl 3 2-OH-Phenyl 16 Methyl Methyl 4 2-OH-Phenyl 17 Methyl Methyl 1 4-OMe-Phenyl 18 Methyl Methyl 2 4-OMe-Phenyl 19 Methyl Methyl 3 4-OMe-Phenyl 20 Methyl Methyl 4 4-OMe-Phenyl 21 Methyl Methyl 1 3-OMe-Phenyl 22 Methyl Methyl 2 3-OMe-Phenyl 23 Methyl Methyl 3 3-OMe-Phenyl 24 Methyl Methyl 4 3-OMe-Phenyl 25 Methyl Methyl 1 2-OMe-Phenyl 26 Methyl Methyl 2 2-OMe-Phenyl 27 Methyl Methyl 3 2-OMe-Phenyl 28 Methyl Methyl 4 2-OMe-Phenyl 29 Methyl Methyl 1 4-CN-Phenyl 30 Methyl Methyl 2 4-CN-Phenyl 31 Methyl Methyl 3 4-CN-Phenyl 32 Methyl Methyl 4 4-CN-Phenyl 33 Methyl Methyl 1 3-CN-Phenyl 34 Methyl Methyl 2 3-CN-Phenyl 35 Methyl Methyl 3 3-CN-Phenyl 36 Methyl Methyl 4 3-CN-Phenyl 37 Methyl Methyl 1 2-CN-Phenyl 38 Methyl Methyl 2 2-CN-Phenyl 39 Methyl Methyl 3 2-CN-Phenyl 40 Methyl Methyl 4 2-CN-Phenyl 41 Methyl Methyl 1 4-Me-Phenyl 42 Methyl Methyl 2 4-Me-Phenyl 43 Methyl Methyl 3 4-Me-Phenyl 44 Methyl Methyl 4 4-Me-Phenyl 45 Methyl Methyl 1 3-Me-Phenyl 46 Methyl Methyl 2 3-Me-Phenyl 47 Methyl Methyl 3 3-Me-Phenyl 48 Methyl Methyl 4 3-Me-Phenyl 49 Methyl Methyl 1 2-Me-Phenyl 50 Methyl Methyl 2 2-Me-Phenyl 51 Methyl Methyl 3 2-Me-Phenyl 52 Methyl Methyl 4 2-Me-Phenyl 53 Methyl Methyl 1 4-F-Phenyl 54 Methyl Methyl 2 4-F-Phenyl 55 Methyl Methyl 3 4-F-Phenyl 56 Methyl Methyl 4 4-F-Phenyl 57 Methyl Methyl 1 3-F-Phenyl 58 Methyl Methyl 2 3-F-Phenyl 59 Methyl Methyl 3 3-F-Phenyl 60 Methyl Methyl 4 3-F-Phenyl 61 Methyl Methyl 1 2-F-Phenyl 62 Methyl Methyl 2 2-F-Phenyl 63 Methyl Methyl 3 2-F-Phenyl 64 Methyl Methyl 4 2-F-Phenyl 65 Methyl Methyl 1 4-Cl-Phenyl 66 Methyl Methyl 2 4-Cl-Phenyl 67 Methyl Methyl 3 4-Cl-Phenyl 68 Methyl Methyl 4 4-Cl-Phenyl 69 Methyl Methyl 1 3-Cl-Phenyl 70 Methyl Methyl 2 3-Cl-Phenyl 71 Methyl Methyl 3 3-Cl-Phenyl 72 Methyl Methyl 4 3-Cl-Phenyl 73 Methyl Methyl 1 2-Cl-Phenyl 74 Methyl Methyl 2 2-Cl-Phenyl 75 Methyl Methyl 3 2-Cl-Phenyl 76 Methyl Methyl 4 2-Cl-Phenyl 77 Methyl Methyl 1 4-Br-Phenyl 78 Methyl Methyl 2 4-Br-Phenyl 79 Methyl Methyl 3 4-Br-Phenyl 80 Methyl Methyl 4 4-Br-Phenyl 81 Methyl Methyl 1 3-Br-Phenyl 82 Methyl Methyl 2 3-Br-Phenyl 83 Methyl Methyl 3 3-Br-Phenyl 84 Methyl Methyl 4 3-Br-Phenyl 85 Methyl Methyl 1 2-Br-Phenyl 86 Methyl Methyl 2 2-Br-Phenyl 87 Methyl Methyl 3 2-Br-Phenyl 88 Methyl Methyl 4 2-Br-Phenyl 89 Methyl Methyl 1 4-CF.sub.3-Phenyl 90 Methyl Methyl 2 4-CF.sub.3-Phenyl 91 Methyl Methyl 3 4-CF.sub.3-Phenyl 92 Methyl Methyl 4 4-CF.sub.3-Phenyl 93 Methyl Methyl 1 3-CF.sub.3-Phenyl 94 Methyl Methyl 2 3-CF.sub.3-Phenyl 95 Methyl Methyl 3 3-CF.sub.3-Phenyl 96 Methyl Methyl 4 3-CF.sub.3-Phenyl 97 Methyl Methyl 1 2-CF.sub.3-Phenvl 98 Methyl Methyl 2 2-CF.sub.3-Phenvl 99 Methyl Methyl 3 2-CF.sub.3-Phenvl 100 Methyl Methyl 4 2-CF.sub.3-Phenyl 101 Methyl Methyl 1 4-iPr-Phenyl 102 Methyl Methyl 2 4-iPr-Phenyl 103 Methyl Methyl 3 4-iPr-Phenyl 104 Methyl Methyl 4 4-iPr-Phenyl 105 Methyl Methyl 1 3-iPr-Phenyl 106 Methyl Methyl 2 3-iPr-Phenyl 107 Methyl Methyl 3 3-iPr-Phenyl 108 Methyl Methyl 4 3-iPr-Phenyl 109 Methyl Methyl 1 2-iPr-Phenyl 110 Methyl Methyl 2 2-iPr-Phenyl 111 Methyl Methyl 3 2-iPr-Phenyl 112 Methyl Methyl 4 2-iPr-Phenyl 113 Methyl Methyl 1 4-NH.sub.2-Phenyl 114 Methyl Methyl 2 4-NH.sub.2-Phenyl 115 Methyl Methyl 3 4-NH.sub.2-Phenyl 116 Methyl Methyl 4 4-NH.sub.2-Phenyl 117 Methyl Methyl 1 3-NH.sub.2-Phenyl 118 Methyl Methyl 2 3-NH.sub.2-Phenyl 119 Methyl Methyl 3 3-NH.sub.2-Phenyl 120 Methyl Methyl 4 3-NH.sub.2-Phenyl 121 Methyl Methyl 1 2-NH.sub.2-Phenyl 122 Methyl Methyl 2 2-NH.sub.2-Phenyl 123 Methyl Methyl 3 2-NH.sub.2-Phenyl 124 Methyl Methyl 4 2-NH.sub.2-Phenyl 125 Methyl Methyl 1 2,3-di-Me-Phenyl 126 Methyl Methyl 2 2,3-di-Me-Phenyl 127 Methyl Methyl 3 2,3-di-Me-Phenyl 128 Methyl Methyl 4 2,3-di-Me-Phenyl 129 Methyl Methyl 1 2,4-di-Me-Phenyl 130 Methyl Methyl 2 2,4-di-Me-Phenyl 131 Methyl Methyl 3 2,4-di-Me-Phenyl 132 Methyl Methyl 4 2,4-di-Me-Phenyl 133 Methyl Methyl 1 2,5-di-Me-Phenyl 134 Methyl Methyl 2 2,5-di-Me-Phenyl 135 Methyl Methyl 3 2,5-di-Me-Phenyl 136 Methyl Methyl 4 2,5-di-Me-Phenyl 137 Methyl Methyl 1 2,6-di-Me-Phenyl 138 Methyl Methyl 2 2,6-di-Me-Phenyl 139 Methyl Methyl 3 2,6-di-Me-Phenyl 140 Methyl Methyl 4 2,6-di-Me-Phenyl 141 Methyl Methyl 1 2,6-di-iPr-Phenyl 142 Methyl Methyl 2 2,6-di-iPr-Phenyl 143 Methyl Methyl 3 2,6-di-iPr-Phenyl 144 Methyl Methyl 4 2,6-di-iPr-Phenyl 145 Methyl Methyl 1 2-morpholino-phenyl 146 Methyl Methyl 2 2-morpholino-phenyl 147 Methyl Methyl 3 2-morpholino-phenyl 148 Methyl Methyl 4 2-morpholino-phenyl 149 Methyl Methyl 1 3-morpholino-phenyl 150 Methyl Methyl 2 3-morpholino-phenyl 151 Methyl Methyl 3 3-morpholino-phenyl 152 Methyl Methyl 4 3-morpholino-phenyl 153 Methyl Methyl 1 4-morpholino-phenyl 154 Methyl Methyl 2 4-morpholino-phenyl 155 Methyl Methyl 3 4-morpholino-phenyl 156 Methyl Methyl 4 4-morpholino-phenyl 157 Methyl Methyl 1 4-CN-2-morpholino-phenyl 158 Methyl Methyl 2 4-CN-2-morpholino-phenyl 159 Methyl Methyl 3 4-CN-2-morpholino-phenyl 160 Methyl Methyl 4 4-CN-2-morpholino-phenyl 161 Methyl Methyl 1 4-CH.sub.3-2-morpholino-phenyl 162 Methyl Methyl 2 4-CH.sub.3-2-morpholino-phenyl 163 Methyl Methyl 3 4-CH.sub.3-2-morpholino-phenyl 164 Methyl Methyl 4 4-CH.sub.3-2-morpholino-phenyl 165 Methyl Methyl 1 4-OH-2-morpholino-phenyl 166 Methyl Methyl 2 4-OH-2-morpholino-phenyl 167 Methyl Methyl 3 4-OH-2-morpholino-phenyl 168 Methyl Methyl 4 4-OH-2-morpholino-phenyl 169 Methyl Methyl 1 naphthylen-1-yl 170 Methyl Methyl 2 naphthylen-1-yl 171 Methyl Methyl 3 naphthylen-1-yl 172 Methyl Methyl 4 naphthylen-1-yl 173 Methyl Methyl 1 naphthylen-2-yl 174 Methyl Methyl 2 naphthylen-2-yl 175 Methyl Methyl 3 naphthylen-2-yl 176 Methyl Methyl 4 naphthylen-2-yl 177 Ethyl Ethyl 1 Phenyl 178 Ethyl Ethyl 2 Phenyl 179 Ethyl Ethyl 3 Phenyl 180 Ethyl Ethyl 4 Phenyl 181 Ethyl Ethyl 1 4-OH-Phenyl 182 Ethyl Ethyl 2 4-OH-Phenyl 183 Ethyl Ethyl 3 4-OH-Phenyl 184 Ethyl Ethyl 4 4-OH-Phenyl 185 Ethyl Ethyl 1 3-OH-Phenyl 186 Ethyl Ethyl 2 3-OH-Phenyl 187 Ethyl Ethyl 3 3-OH-Phenyl 188 Ethyl Ethyl 4 3-OH-Phenyl 189 Ethyl Ethyl 1 2-OH-Phenyl 190 Ethyl Ethyl 2 2-OH-Phenyl 191 Ethyl Ethyl 3 2-OH-Phenyl 192 Ethyl Ethyl 4 2-OH-Phenyl 193 Ethyl Ethyl 1 4-OMe-Phenyl 194 Ethyl Ethyl 2 4-OMe-Phenyl 195 Ethyl Ethyl 3 4-OMe-Phenyl 196 Ethyl Ethyl 4 4-OMe-Phenyl 197 Ethyl Ethyl 1 3-OMe-Phenyl 198 Ethyl Ethyl 2 3-OMe-Phenyl 199 Ethyl Ethyl 3 3-OMe-Phenyl 200 Ethyl Ethyl 4 3-OMe-Phenyl 201 Ethyl Ethyl 1 2-OMe-Phenyl 202 Ethyl Ethyl 2 2-OMe-Phenyl 203 Ethyl Ethyl 3 2-OMe-Phenyl 204 Ethyl Ethyl 4 2-OMe-Phenyl 205 Ethyl Ethyl 1 4-CN-Phenyl 206 Ethyl Ethyl 2 4-CN-Phenyl 207 Ethyl Ethyl 3 4-CN-Phenyl 208 Ethyl Ethyl 4 4-CN-Phenyl 209 Ethyl Ethyl 1 3-CN-Phenyl 210 Ethyl Ethyl 2 3-CN-Phenyl 211 Ethyl Ethyl 3 3-CN-Phenyl 212 Ethyl Ethyl 4 3-CN-Phenyl 213 Ethyl Ethyl 1 2-CN-Phenyl 214 Ethyl Ethyl 2 2-CN-Phenyl 215 Ethyl Ethyl 3 2-CN-Phenyl 216 Ethyl Ethyl 4 2-CN-Phenyl 217 Ethyl Ethyl 1 4-Me-Phenyl 218 Ethyl Ethyl 2 4-Me-Phenyl 219 Ethyl Ethyl 3 4-Me-Phenyl 220 Ethyl Ethyl 4 4-Me-Phenyl 221 Ethyl Ethyl 1 3-Me-Phenyl 222 Ethyl Ethyl 2 3-Me-Phenyl 223 Ethyl Ethyl 3 3-Me-Phenyl 224 Ethyl Ethyl 4 3-Me-Phenyl 225 Ethyl Ethyl 1 2-Me-Phenyl 226 Ethyl Ethyl 2 2-Me-Phenyl 227 Ethyl Ethyl 3 2-Me-Phenyl 228 Ethyl Ethyl 4 2-Me-Phenyl 229 Ethyl Ethyl 1 4-F-Phenyl 230 Ethyl Ethyl 2 4-F-Phenyl 231 Ethyl Ethyl 3 4-F-Phenyl 232 Ethyl Ethyl 4 4-F-Phenyl 233 Ethyl Ethyl 1 3-F-Phenyl 234 Ethyl Ethyl 2 3-F-Phenyl 235 Ethyl Ethyl 3 3-F-Phenyl 236 Ethyl Ethyl 4 3-F-Phenyl 237 Ethyl Ethyl 1 2-F-Phenyl 238 Ethyl Ethyl 2 2-F-Phenyl 239 Ethyl Ethyl 3 2-F-Phenyl 240 Ethyl Ethyl 4 2-F-Phenyl 241 Ethyl Ethyl 1 4-Cl-Phenyl 242 Ethyl Ethyl 2 4-Cl-Phenyl 243 Ethyl Ethyl 3 4-Cl-Phenyl 244 Ethyl Ethyl 4 4-Cl-Phenyl 245 Ethyl Ethyl 1 3-Cl-Phenyl 246 Ethyl Ethyl 2 3-Cl-Phenyl 247 Ethyl Ethyl 3 3-Cl-Phenyl 248 Ethyl Ethyl 4 3-Cl-Phenyl 249 Ethyl Ethyl 1 2-Cl-Phenyl 250 Ethyl Ethyl 2 2-Cl-Phenyl 251 Ethyl Ethyl 3 2-Cl-Phenyl 252 Ethyl Ethyl 4 2-Cl-Phenyl 253 Ethyl Ethyl 1 4-Br-Phenyl 254 Ethyl Ethyl 2 4-Br-Phenyl 255 Ethyl Ethyl 3 4-Br-Phenyl 256 Ethyl Ethyl 4 4-Br-Phenyl 257 Ethyl Ethyl 1 3-Br-Phenyl 258 Ethyl Ethyl 2 3-Br-Phenyl 259 Ethyl Ethyl 3 3-Br-Phenyl 260 Ethyl Ethyl 4 3-Br-Phenyl 261 Ethyl Ethyl 1 2-Br-Phenyl 262 Ethyl Ethyl 2 2-Br-Phenyl 263 Ethyl Ethyl 3 2-Br-Phenyl 264 Ethyl Ethyl 4 2-Br-Phenyl 265 Ethyl Ethyl 1 4-CF.sub.3-Phenyl 266 Ethyl Ethyl 2 4-CF.sub.3-Phenyl 267 Ethyl Ethyl 3 4-CF.sub.3-Phenyl 268 Ethyl Ethyl 4 4-CF.sub.3-Phenyl 269 Ethyl Ethyl 1 3-CF.sub.3-Phenyl 270 Ethyl Ethyl 2 3-CF.sub.3-Phenyl 271 Ethyl Ethyl 3 3-CF.sub.3-Phenyl 272 Ethyl Ethyl 4 3-CF.sub.3-Phenyl 273 Ethyl Ethyl 1 2-CF.sub.3-Phenyl 274 Ethyl Ethyl 2 2-CF.sub.3-Phenyl 275 Ethyl Ethyl 3 2-CF.sub.3-Phenyl 276 Ethyl Ethyl 4 2-CF.sub.3-Phenyl 277 Ethyl Ethyl 1 4-iPr-Phenyl 278 Ethyl Ethyl 2 4-iPr-Phenyl 279 Ethyl Ethyl 3 4-iPr-Phenyl 280 Ethyl Ethyl 4 4-iPr-Phenyl 281 Ethyl Ethyl 1 3-iPr-Phenyl 282 Ethyl Ethyl 2 3-iPr-Phenyl 283 Ethyl Ethyl 3 3-iPr-Phenyl 284 Ethyl Ethyl 4 3-iPr-Phenyl 285 Ethyl Ethyl 1 2-iPr-Phenyl 286 Ethyl Ethyl 2 2-iPr-Phenyl 287 Ethyl Ethyl 3 2-iPr-Phenyl 288 Ethyl Ethyl 4 2-iPr-Phenyl 289 Ethyl Ethyl 1 4-NH.sub.2-Phenyl 290 Ethyl Ethyl 2 4-NH.sub.2-Phenyl 291 Ethyl Ethyl 3 4-NH.sub.2-Phenyl 292 Ethyl Ethyl 4 4-NH.sub.2-Phenyl 293 Ethyl Ethyl 1 3-NH.sub.2-Phenyl 294 Ethyl Ethyl 2 3-NH.sub.2-Phenyl 295 Ethyl Ethyl 3 3-NH.sub.2-Phenyl 296 Ethyl Ethyl 4 3-NH.sub.2-Phenyl 297 Ethyl Ethyl 1 2-NH.sub.2-Phenyl 298 Ethyl Ethyl 2 2-NH.sub.2-Phenyl 299 Ethyl Ethyl 3 2-NH.sub.2-Phenyl 300 Ethyl Ethyl 4 2-NH.sub.2-Phenyl 301 Ethyl Ethyl 1 2.3-di-Me-Phenvl 302 Ethyl Ethyl 2 2.3-di-Me-Phenyl 303 Ethyl Ethyl 3 2,3-di-Me-Phenyl 304 Ethyl Ethyl 4 2,3-di-Me-Phenyl 305 Ethyl Ethyl 1 2.4-di-Me-Phenyl 306 Ethyl Ethyl 2 2,4-di-Me-Phenyl 307 Ethyl Ethyl 3 2,4-di-Me-Phenyl 308 Ethyl Ethyl 4 2,4-di-Me-Phenyl 309 Ethyl Ethyl 1 2,5-di-Me-Phenyl 310 Ethyl Ethyl 2 2,5-di-Me-Phenyl 311 Ethyl Ethyl 3 2,5-di-Me-Phenyl 312 Ethyl Ethyl 4 2,5-di-Me-Phenyl 313 Ethyl Ethyl 1 2,6-di-Me-Phenyl 314 Ethyl Ethyl 2 2,6-di-Me-Phenyl 315 Ethyl Ethyl 3 2,6-di-Me-Phenyl 316 Ethyl Ethyl 4 2,6-di-Me-Phenyl 317 Ethyl Ethyl 1 2,6-di-iPr-Phenyl 318 Ethyl Ethyl 2 2,6-di-iPr-Phenyl 319 Ethyl Ethyl 3 2,6-di-iPr-Phenyl 320 Ethyl Ethyl 4 2,6-di-iPr-Phenyl 321 Ethyl Ethyl 1 2-morpholino-phenyl 322 Ethyl Ethyl 2 2-morpholino-phenyl 323 Ethyl Ethyl 3 2-morpholino-phenyl 324 Ethyl Ethyl 4 2-morpholino-phenyl 325 Ethyl Ethyl 1 3-morpholino-phenyl 326 Ethyl Ethyl 2 3-morpholino-phenyl 327 Ethyl Ethyl 3 3-morpholino-phenyl 328 Ethyl Ethyl 4 3-morpholino-phenyl 329 Ethyl Ethyl 1 4-morpholino-phenyl 330 Ethyl Ethyl 2 4-morpholino-phenyl 331 Ethyl Ethyl 3 4-morpholino-phenyl 332 Ethyl Ethyl 4 4-morpholino-phenyl 333 Ethyl Ethyl 1 4-CN-2-morpholino-phenyl 334 Ethyl Ethyl 2 4-CN-2-morpholino-phenyl 335 Ethyl Ethyl 3 4-CN-2-morpholino-phenyl 336 Ethyl Ethyl 4 4-CN-2-morpholino-phenyl 337 Ethyl Ethyl 1 4-CH.sub.3-2-morpholino-phenyl 338 Ethyl Ethyl 2 4-CH.sub.3-2-morpholino-phenyl 339 Ethyl Ethyl 3 4-CH.sub.3-2-morpholino-phenyl 340 Ethyl Ethyl 4 4-CH.sub.3-2-morpholino-phenyl 341 Ethyl Ethyl 1 4-OH-2-morpholino-phenyl 342 Ethyl Ethyl 2 4-OH-2-morpholino-phenyl 343 Ethyl Ethyl 3 4-OH-2-morpholino-phenyl 344 Ethyl Ethyl 4 4-OH-2-morpholino-phenyl 345 Ethyl Ethyl 1 naphthylen-1-yl 346 Ethyl Ethyl 2 naphthylen-1-yl 347 Ethyl Ethyl 3 naphthylen-1-yl 348 Ethyl Ethyl 4 naphthylen-1-yl 349 Ethyl Ethyl 1 naphthylen-2-yl 350 Ethyl Ethyl 2 naphthylen-2-yl 351 Ethyl Ethyl 3 naphthylen-2-yl 352 Ethyl Ethyl 4 naphthylen-2-yl

    [2016] Exemplary embodiments include compounds having the formula (XVIII)

    ##STR00433##

    [2017] or a pharmaceutically acceptable salt form thereof defined herein below in Table 12

    TABLE-US-00012 TABLE 12 Entry n R.sup.5 Entry n R.sup.5 1 1 Phenyl 85 1 2-Br-Phenyl 2 2 Phenyl 86 2 2-Br-Phenyl 3 3 Phenyl 87 3 2-Br-Phenyl 4 4 Phenyl 88 4 2-Br-Phenyl 5 1 4-OH-Phenyl 89 1 4-CF.sub.3-Phenyl 6 2 4-OH-Phenyl 90 2 4-CF.sub.3-Phenyl 7 3 4-OH-Phenyl 91 3 4-CF.sub.3-Phenyl 8 4 4-OH-Phenyl 92 4 4-CF.sub.3-Phenyl 9 1 3-OH-Phenyl 93 1 3-CF.sub.3-Phenyl 10 2 3-OH-Phenyl 94 2 3-CF.sub.3-Phenyl 11 3 3-OH-Phenyl 95 3 3-CF.sub.3-Phenyl 12 4 3-OH-Phenyl 96 4 3-CF.sub.3-Phenyl 13 1 2-OH-Phenyl 97 1 2-CF.sub.3-Phenyl 14 2 2-OH-Phenyl 98 2 2-CF.sub.3-Phenyl 15 3 2-OH-Phenyl 99 3 2-CF.sub.3-Phenyl 16 4 2-OH-Phenyl 100 4 2-CF.sub.3-Phenyl 17 1 4-OMe-Phenyl 101 1 4-iPr-Phenyl 18 2 4-OMe-Phenyl 102 2 4-iPr-Phenyl 19 3 4-OMe-Phenyl 103 3 4-iPr-Phenyl 20 4 4-OMe-Phenyl 104 4 4-iPr-Phenyl 21 1 3-OMe-Phenyl 105 1 3-iPr-Phenyl 22 2 3-OMe-Phenyl 106 2 3-iPr-Phenyl 23 3 3-OMe-Phenyl 107 3 3-iPr-Phenyl 24 4 3-OMe-Phenyl 108 4 3-iPr-Phenyl 25 1 2-OMe-Phenyl 109 1 2-iPr-Phenyl 26 2 2-OMe-Phenyl 110 2 2-iPr-Phenyl 27 3 2-OMe-Phenyl 111 3 2-iPr-Phenyl 28 4 2-OMe-Phenyl 112 4 2-iPr-Phenyl 29 1 4-CN-Phenyl 113 1 4-NH.sub.2-Phenyl 30 2 4-CN-Phenyl 114 2 4-NH.sub.2-Phenyl 31 3 4-CN-Phenyl 115 3 4-NH.sub.2-Phenyl 32 4 4-CN-Phenyl 116 4 4-NH.sub.2-Phenyl 33 1 3-CN-Phenyl 117 1 3-NH.sub.2-Phenyl 34 2 3-CN-Phenyl 118 2 3-NH.sub.2-Phenyl 35 3 3-CN-Phenyl 119 3 3-NH.sub.2-Phenyl 36 4 3-CN-Phenyl 120 4 3-NH.sub.2-Phenyl 37 1 2-CN-Phenyl 121 1 2-NH.sub.2-Phenyl 38 2 2-CN-Phenyl 122 2 2-NH.sub.2-Phenyl 39 3 2-CN-Phenyl 123 3 2-NH.sub.2-Phenyl 40 4 2-CN-Phenyl 124 4 2-NH.sub.2-Phenyl 41 1 4-Me-Phenyl 125 1 2,3-di-Me-Phenyl 42 2 4-Me-Phenyl 126 2 2,3-di-Me-Phenyl 43 3 4-Me-Phenyl 127 3 2,3-di-Me-Phenyl 44 4 4-Me-Phenyl 128 4 2,3-di-Me-Phenyl 45 1 3-Me-Phenyl 129 1 2,4-di-Me-Phenyl 46 2 3-Me-Phenyl 130 2 2,4-di-Me-Phenyl 47 3 3-Me-Phenyl 131 3 2,4-di-Me-Phenyl 48 4 3-Me-Phenyl 132 4 2,4-di-Me-Phenyl 49 1 2-Me-Phenyl 133 1 2,5-di-Me-Phenyl 50 2 2-Me-Phenyl 134 2 2,5-di-Me-Phenyl 51 3 2-Me-Phenyl 135 3 2,5-di-Me-Phenyl 52 4 2-Me-Phenyl 136 4 2,5-di-Me-Phenyl 53 1 4-F-Phenyl 137 1 2,6-di-Me-Phenyl 54 2 4-F-Phenyl 138 2 2,6-di-Me-Phenyl 55 3 4-F-Phenyl 139 3 2,6-di-Me-Phenyl 56 4 4-F-Phenyl 140 4 2,6-di-Me-Phenyl 57 1 3-F-Phenyl 141 1 2,6-di-iPr-Phenyl 58 2 3-F-Phenyl 142 2 2,6-di-iPr-Phenyl 59 3 3-F-Phenyl 143 3 2,6-di-iPr-Phenyl 60 4 3-F-Phenyl 144 4 2,6-di-iPr-Phenyl 61 1 2-F-Phenyl 145 1 2-morpholino-phenyl 62 2 2-F-Phenyl 146 2 2-morpholino-phenyl 63 3 2-F-Phenyl 147 3 2-morpholino-phenyl 64 4 2-F-Phenyl 148 4 2-morpholino-phenyl 65 1 4-Cl-Phenyl 149 1 3-morpholino-phenyl 66 2 4-Cl-Phenyl 150 2 3-morpholino-phenyl 67 3 4-Cl-Phenyl 151 3 3-morpholino-phenyl 68 4 4-Cl-Phenyl 152 4 3-morpholino-phenyl 69 1 3-Cl-Phenyl 153 1 4-morpholino-phenyl 70 2 3-Cl-Phenyl 154 2 4-morpholino-phenyl 71 3 3-Cl-Phenyl 155 3 4-morpholino-phenyl 72 4 3-Cl-Phenyl 156 4 4-morpholino-phenyl 73 1 2-Cl-Phenyl 157 1 4-CN-2-morpholino-phenyl 74 2 2-Cl-Phenyl 158 2 4-CN-2-morpholino-phenyl 75 3 2-Cl-Phenyl 159 3 4-CN-2-morpholino-phenyl 76 4 2-Cl-Phenyl 160 4 4-CN-2-morpholino-phenyl 77 1 4-Br-Phenyl 161 1 4-CH.sub.3-2-morpholino-phenyl 78 2 4-Br-Phenyl 162 2 4-CH.sub.3-2-morpholino-phenyl 79 3 4-Br-Phenyl 163 3 4-CH.sub.3-2-morpholino-phenyl 80 4 4-Br-Phenyl 164 4 4-CH.sub.3-2-morpholino-phenyl 81 1 3-Br-Phenyl 165 1 4-OH-2-morpholino-phenyl 82 2 3-Br-Phenyl 166 2 4-OH-2-morpholino-phenyl 83 3 3-Br-Phenyl 167 3 4-OH-2-morpholino-phenyl 84 4 3-Br-Phenyl 168 4 4-OH-2-morpholino-phenyl 85 1 naphthylen-1-yl 173 1 naphthylen-2-yl 86 2 naphthylen-1-yl 174 2 naphthylen-2-yl 87 3 naphthylen-1-yl 175 3 naphthylen-2-yl 88 4 naphthylen-1-yl 176 4 naphthylen-2-yl

    [2018] Exemplary embodiments include compounds having the formula (XIX)

    ##STR00434##

    [2019] or a pharmaceutically acceptable salt form thereof defined herein below in Table 13.

    TABLE-US-00013 TABLE 13 Entry n R.sup.5 Entry n R.sup.5 1 1 Phenyl 85 1 2-Br-Phenyl 2 2 Phenyl 86 2 2-Br-Phenyl 3 3 Phenyl 87 3 2-Br-Phenyl 4 4 Phenyl 88 4 2-Br-Phenyl 5 1 4-OH-Phenyl 89 1 4-CF.sub.3-Phenyl 6 2 4-OH-Phenyl 90 2 4-CF.sub.3-Phenyl 7 3 4-OH-Phenyl 91 3 4-CF.sub.3-Phenyl 8 4 4-OH-Phenyl 92 4 4-CF.sub.3-Phenyl 9 1 3-OH-Phenyl 93 1 3-CF.sub.3-Phenyl 10 2 3-OH-Phenyl 94 2 3-CF.sub.3-Phenyl 11 3 3-OH-Phenyl 95 3 3-CF.sub.3-Phenyl 12 4 3-OH-Phenyl 96 4 3-CF.sub.3-Phenyl 13 1 2-OH-Phenyl 97 1 2-CF.sub.3-Phenyl 14 2 2-OH-Phenyl 98 2 2-CF.sub.3-Phenyl 15 3 2-OH-Phenyl 99 3 2-CF.sub.3-Phenyl 16 4 2-OH-Phenyl 100 4 2-CF.sub.3-Phenyl 17 1 4-OMe-Phenyl 101 1 4-iPr-Phenyl 18 2 4-OMe-Phenyl 102 2 4-iPr-Phenyl 19 3 4-OMe-Phenyl 103 3 4-iPr-Phenyl 20 4 4-OMe-Phenyl 104 4 4-iPr-Phenyl 21 1 3-OMe-Phenyl 105 1 3-iPr-Phenyl 22 2 3-OMe-Phenyl 106 2 3-iPr-Phenyl 23 3 3-OMe-Phenyl 107 3 3-iPr-Phenyl 24 4 3-OMe-Phenyl 108 4 3-iPr-Phenyl 25 1 2-OMe-Phenyl 109 1 2-iPr-Phenyl 26 2 2-OMe-Phenyl 110 2 2-iPr-Phenyl 27 3 2-OMe-Phenyl 111 3 2-iPr-Phenyl 28 4 2-OMe-Phenyl 112 4 2-iPr-Phenyl 29 1 4-CN-Phenyl 113 1 4-NH.sub.2-Phenyl 30 2 4-CN-Phenyl 114 2 4-NH.sub.2-Phenyl 31 3 4-CN-Phenyl 115 3 4-NH.sub.2-Phenyl 32 4 4-CN-Phenyl 116 4 4-NH.sub.2-Phenyl 33 1 3-CN-Phenyl 117 1 3-NH.sub.2-Phenyl 34 2 3-CN-Phenyl 118 2 3-NH.sub.2-Phenyl 35 3 3-CN-Phenyl 119 3 3-NH.sub.2-Phenyl 36 4 3-CN-Phenyl 120 4 3-NH.sub.2-Phenyl 37 1 2-CN-Phenyl 121 1 2-NH.sub.2-Phenyl 38 2 2-CN-Phenyl 122 2 2-NH.sub.2-Phenyl 39 3 2-CN-Phenyl 123 3 2-NH.sub.2-Phenyl 40 4 2-CN-Phenyl 124 4 2-NH.sub.2-Phenyl 41 1 4-Me-Phenyl 125 1 2,3-di-Me-Phenyl 42 2 4-Me-Phenyl 126 2 2,3-di-Me-Phenyl 43 3 4-Me-Phenyl 127 3 2,3-di-Me-Phenyl 44 4 4-Me-Phenyl 128 4 2,3-di-Me-Phenyl 45 1 3-Me-Phenyl 129 1 2,4-di-Me-Phenyl 46 2 3-Me-Phenyl 130 2 2,4-di-Me-Phenyl 47 3 3-Me-Phenyl 131 3 2,4-di-Me-Phenyl 48 4 3-Me-Phenyl 132 4 2,4-di-Me-Phenyl 49 1 2-Me-Phenyl 133 1 2,5-di-Me-Phenyl 50 2 2-Me-Phenyl 134 2 2,5-di-Me-Phenyl 51 3 2-Me-Phenyl 135 3 2,5-di-Me-Phenyl 52 4 2-Me-Phenyl 136 4 2,5-di-Me-Phenyl 53 1 4-F-Phenyl 137 1 2,6-di-Me-Phenyl 54 2 4-F-Phenyl 138 2 2,6-di-Me-Phenyl 55 3 4-F-Phenyl 139 3 2,6-di-Me-Phenyl 56 4 4-F-Phenyl 140 4 2,6-di-Me-Phenyl 57 1 3-F-Phenyl 141 1 2,6-di-iPr-Phenyl 58 2 3-F-Phenyl 142 2 2,6-di-iPr-Phenyl 59 3 3-F-Phenyl 143 3 2,6-di-iPr-Phenyl 60 4 3-F-Phenyl 144 4 2,6-di-iPr-Phenyl 61 1 2-F-Phenyl 145 1 2-morpholino-phenyl 62 2 2-F-Phenyl 146 2 2-morpholino-phenyl 63 3 2-F-Phenyl 147 3 2-morpholino-phenyl 64 4 2-F-Phenyl 148 4 2-morpholino-phenyl 65 1 4-Cl-Phenyl 149 1 3-morpholino-phenyl 66 2 4-Cl-Phenyl 150 2 3-morpholino-phenyl 67 3 4-Cl-Phenyl 151 3 3-morpholino-phenyl 68 4 4-Cl-Phenyl 152 4 3-morpholino-phenyl 69 1 3-Cl-Phenyl 153 1 4-morpholino-phenyl 70 2 3-Cl-Phenyl 154 2 4-morpholino-phenyl 71 3 3-Cl-Phenyl 155 3 4-morpholino-phenyl 72 4 3-Cl-Phenyl 156 4 4-morpholino-phenyl 73 1 2-Cl-Phenyl 157 1 4-CN-2-morpholino-phenyl 74 2 2-Cl-Phenyl 158 2 4-CN-2-morpholino-phenyl 75 3 2-Cl-Phenyl 159 3 4-CN-2-morpholino-phenyl 76 4 2-Cl-Phenyl 160 4 4-CN-2-morpholino-phenyl 77 1 4-Br-Phenyl 161 1 4-CH.sub.3-2-morpholino-phenyl 78 2 4-Br-Phenyl 162 2 4-CH.sub.3-2-morpholino-phenyl 79 3 4-Br-Phenyl 163 3 4-CH.sub.3-2-morpholino-phenyl 80 4 4-Br-Phenyl 164 4 4-CH.sub.3-2-morpholino-phenyl 81 1 3-Br-Phenyl 165 1 4-OH-2-morpholino-phenyl 82 2 3-Br-Phenyl 166 2 4-OH-2-morpholino-phenyl 83 3 3-Br-Phenyl 167 3 4-OH-2-morpholino-phenyl 84 4 3-Br-Phenyl 168 4 4-OH-2-morpholino-phenyl 85 1 naphthylen-1-yl 173 1 naphthylen-2-yl 86 2 naphthylen-1-yl 174 2 naphthylen-2-yl 87 3 naphthylen-1-yl 175 3 naphthylen-2-yl 88 4 naphthylen-1-yl 176 4 naphthylen-2-yl

    [2020] Exemplary embodiments include compounds having the formula (XX)

    ##STR00435##

    [2021] or a pharmaceutically acceptable salt form thereof defined herein below in Table 14.

    TABLE-US-00014 TABLE 14 Entry n R.sup.5 Entry n R.sup.5 1 1 Phenyl 85 1 2-Br-Phenyl 2 2 Phenyl 86 2 2-Br-Phenyl 3 3 Phenyl 87 3 2-Br-Phenyl 4 4 Phenyl 88 4 2-Br-Phenyl 5 1 4-OH-Phenyl 89 1 4-CF.sub.3-Phenyl 6 2 4-OH-Phenyl 90 2 4-CF.sub.3-Phenyl 7 3 4-OH-Phenyl 91 3 4-CF.sub.3-Phenyl 8 4 4-OH-Phenyl 92 4 4-CF.sub.3-Phenyl 9 1 3-OH-Phenyl 93 1 3-CF.sub.3-Phenyl 10 2 3-OH-Phenyl 94 2 3-CF.sub.3-Phenyl 11 3 3-OH-Phenyl 95 3 3-CF.sub.3-Phenyl 12 4 3-OH-Phenyl 96 4 3-CF.sub.3-Phenyl 13 1 2-OH-Phenyl 97 1 2-CF.sub.3-Phenyl 14 2 2-OH-Phenyl 98 2 2-CF.sub.3-Phenyl 15 3 2-OH-Phenyl 99 3 2-CF.sub.3-Phenyl 16 4 2-OH-Phenyl 100 4 2-CF.sub.3-Phenyl 17 1 4-OMe-Phenyl 101 1 4-iPr-Phenyl 18 2 4-OMe-Phenyl 102 2 4-iPr-Phenyl 19 3 4-OMe-Phenyl 103 3 4-iPr-Phenyl 20 4 4-OMe-Phenyl 104 4 4-iPr-Phenyl 21 1 3-OMe-Phenyl 105 1 3-iPr-Phenyl 22 2 3-OMe-Phenyl 106 2 3-iPr-Phenyl 23 3 3-OMe-Phenyl 107 3 3-iPr-Phenyl 24 4 3-OMe-Phenyl 108 4 3-iPr-Phenyl 25 1 2-OMe-Phenyl 109 1 2-iPr-Phenyl 26 2 2-OMe-Phenyl 110 2 2-iPr-Phenyl 27 3 2-OMe-Phenyl 111 3 2-iPr-Phenyl 28 4 2-OMe-Phenyl 112 4 2-iPr-Phenyl 29 1 4-CN-Phenyl 113 1 4-NH.sub.2-Phenyl 30 2 4-CN-Phenyl 114 2 4-NH.sub.2-Phenyl 31 3 4-CN-Phenyl 115 3 4-NH.sub.2-Phenyl 32 4 4-CN-Phenyl 116 4 4-NH.sub.2-Phenyl 33 1 3-CN-Phenyl 117 1 3-NH.sub.2-Phenyl 34 2 3-CN-Phenyl 118 2 3-NH.sub.2-Phenyl 35 3 3-CN-Phenyl 119 3 3-NH.sub.2-Phenyl 36 4 3-CN-Phenyl 120 4 3-NH.sub.2-Phenyl 37 1 2-CN-Phenyl 121 1 2-NH.sub.2-Phenyl 38 2 2-CN-Phenyl 122 2 2-NH.sub.2-Phenyl 39 3 2-CN-Phenyl 123 3 2-NH.sub.2-Phenyl 40 4 2-CN-Phenyl 124 4 2-NH.sub.2-Phenyl 41 1 4-Me-Phenyl 125 1 2,3-di-Me-Phenyl 42 2 4-Me-Phenyl 126 2 2,3-di-Me-Phenyl 43 3 4-Me-Phenyl 127 3 2,3-di-Me-Phenyl 44 4 4-Me-Phenyl 128 4 2,3-di-Me-Phenyl 45 1 3-Me-Phenyl 129 1 2,4-di-Me-Phenyl 46 2 3-Me-Phenyl 130 2 2,4-di-Me-Phenyl 47 3 3-Me-Phenyl 131 3 2,4-di-Me-Phenyl 48 4 3-Me-Phenyl 132 4 2,4-di-Me-Phenyl 49 1 2-Me-Phenyl 133 1 2,5-di-Me-Phenyl 50 2 2-Me-Phenyl 134 2 2,5-di-Me-Phenyl 51 3 2-Me-Phenyl 135 3 2,5-di-Me-Phenyl 52 4 2-Me-Phenyl 136 4 2,5-di-Me-Phenyl 53 1 4-F-Phenyl 137 1 2,6-di-Me-Phenyl 54 2 4-F-Phenyl 138 2 2,6-di-Me-Phenyl 55 3 4-F-Phenyl 139 3 2,6-di-Me-Phenyl 56 4 4-F-Phenyl 140 4 2,6-di-Me-Phenyl 57 1 3-F-Phenyl 141 1 2,6-di-iPr-Phenyl 58 2 3-F-Phenyl 142 2 2,6-di-iPr-Phenyl 59 3 3-F-Phenyl 143 3 2,6-di-iPr-Phenyl 60 4 3-F-Phenyl 144 4 2,6-di-iPr-Phenyl 61 1 2-F-Phenyl 145 1 2-morpholino-phenyl 62 2 2-F-Phenyl 146 2 2-morpholino-phenyl 63 3 2-F-Phenyl 147 3 2-morpholino-phenyl 64 4 2-F-Phenyl 148 4 2-morpholino-phenyl 65 1 4-Cl-Phenyl 149 1 3-morpholino-phenyl 66 2 4-Cl-Phenyl 150 2 3-morpholino-phenyl 67 3 4-Cl-Phenyl 151 3 3-morpholino-phenyl 68 4 4-Cl-Phenyl 152 4 3-morpholino-phenyl 69 1 3-Cl-Phenyl 153 1 4-morpholino-phenyl 70 2 3-Cl-Phenyl 154 2 4-morpholino-phenyl 71 3 3-Cl-Phenyl 155 3 4-morpholino-phenyl 72 4 3-Cl-Phenyl 156 4 4-morpholino-phenyl 73 1 2-Cl-Phenyl 157 1 4-CN-2-morpholino-phenyl 74 2 2-Cl-Phenyl 158 2 4-CN-2-morpholino-phenyl 75 3 2-Cl-Phenyl 159 3 4-CN-2-morpholino-phenyl 76 4 2-Cl-Phenyl 160 4 4-CN-2-morpholino-phenyl 77 1 4-Br-Phenyl 161 1 4-CH.sub.3-2-morpholino-phenyl 78 2 4-Br-Phenyl 162 2 4-CH.sub.3-2-morpholino-phenyl 79 3 4-Br-Phenyl 163 3 4-CH.sub.3-2-morpholino-phenyl 80 4 4-Br-Phenyl 164 4 4-CH.sub.3-2-morpholino-phenyl 81 1 3-Br-Phenyl 165 1 4-OH-2-morpholino-phenyl 82 2 3-Br-Phenyl 166 2 4-OH-2-morpholino-phenyl 83 3 3-Br-Phenyl 167 3 4-OH-2-morpholino-phenyl 84 4 3-Br-Phenyl 168 4 4-OH-2-morpholino-phenyl 85 1 naphthylen-1-yl 173 1 naphthylen-2-yl 86 2 naphthylen-1-yl 174 2 naphthylen-2-yl 87 3 naphthylen-1-yl 175 3 naphthylen-2-yl 88 4 naphthylen-1-yl 176 4 naphthylen-2-yl

    [2022] Exemplary embodiments include compounds having the formula (XXI)

    ##STR00436##

    [2023] or a pharmaceutically acceptable salt form thereof defined herein below in Table 15.

    TABLE-US-00015 TABLE 15 Entry n R.sup.5 Entry n R.sup.5 1 1 Phenyl 85 1 2-Br-Phenyl 2 2 Phenyl 86 2 2-Br-Phenyl 3 3 Phenyl 87 3 2-Br-Phenyl 4 4 Phenyl 88 4 2-Br-Phenyl 5 1 4-OH-Phenyl 89 1 4-CF.sub.3-Phenyl 6 2 4-OH-Phenyl 90 2 4-CF.sub.3-Phenyl 7 3 4-OH-Phenyl 91 3 4-CF.sub.3-Phenyl 8 4 4-OH-Phenyl 92 4 4-CF.sub.3-Phenyl 9 1 3-OH-Phenyl 93 1 3-CF.sub.3-Phenyl 10 2 3-OH-Phenyl 94 2 3-CF.sub.3-Phenyl 11 3 3-OH-Phenyl 95 3 3-CF.sub.3-Phenyl 12 4 3-OH-Phenyl 96 4 3-CF.sub.3-Phenyl 13 1 2-OH-Phenyl 97 1 2-CF.sub.3-Phenyl 14 2 2-OH-Phenyl 98 2 2-CF.sub.3-Phenyl 15 3 2-OH-Phenyl 99 3 2-CF.sub.3-Phenyl 16 4 2-OH-Phenyl 100 4 2-CF.sub.3-Phenyl 17 1 4-OMe-Phenyl 101 1 4-iPr-Phenyl 18 2 4-OMe-Phenyl 102 2 4-iPr-Phenyl 19 3 4-OMe-Phenyl 103 3 4-iPr-Phenyl 20 4 4-OMe-Phenyl 104 4 4-iPr-Phenyl 21 1 3-OMe-Phenyl 105 1 3-iPr-Phenyl 22 2 3-OMe-Phenyl 106 2 3-iPr-Phenyl 23 3 3-OMe-Phenyl 107 3 3-iPr-Phenyl 24 4 3-OMe-Phenyl 108 4 3-iPr-Phenyl 25 1 2-OMe-Phenyl 109 1 2-iPr-Phenyl 26 2 2-OMe-Phenyl 110 2 2-iPr-Phenyl 27 3 2-OMe-Phenyl 111 3 2-iPr-Phenyl 28 4 2-OMe-Phenyl 112 4 2-iPr-Phenyl 29 1 4-CN-Phenyl 113 1 4-NH.sub.2-Phenyl 30 2 4-CN-Phenyl 114 2 4-NH.sub.2-Phenyl 31 3 4-CN-Phenyl 115 3 4-NH.sub.2-Phenyl 32 4 4-CN-Phenyl 116 4 4-NH.sub.2-Phenyl 33 1 3-CN-Phenyl 117 1 3-NH.sub.2-Phenyl 34 2 3-CN-Phenyl 118 2 3-NH.sub.2-Phenyl 35 3 3-CN-Phenyl 119 3 3-NH.sub.2-Phenyl 36 4 3-CN-Phenyl 120 4 3-NH.sub.2-Phenyl 37 1 2-CN-Phenyl 121 1 2-NH.sub.2-Phenyl 38 2 2-CN-Phenyl 122 2 2-NH.sub.2-Phenyl 39 3 2-CN-Phenyl 123 3 2-NH.sub.2-Phenyl 40 4 2-CN-Phenyl 124 4 2-NH.sub.2-Phenyl 41 1 4-Me-Phenyl 125 1 2,3-di-Me-Phenyl 42 2 4-Me-Phenyl 126 2 2,3-di-Me-Phenyl 43 3 4-Me-Phenyl 127 3 2,3-di-Me-Phenyl 44 4 4-Me-Phenyl 128 4 2,3-di-Me-Phenyl 45 1 3-Me-Phenyl 129 1 2,4-di-Me-Phenyl 46 2 3-Me-Phenyl 130 2 2,4-di-Me-Phenyl 47 3 3-Me-Phenyl 131 3 2,4-di-Me-Phenyl 48 4 3-Me-Phenyl 132 4 2,4-di-Me-Phenyl 49 1 2-Me-Phenyl 133 1 2,5-di-Me-Phenyl 50 2 2-Me-Phenyl 134 2 2,5-di-Me-Phenyl 51 3 2-Me-Phenyl 135 3 2,5-di-Me-Phenyl 52 4 2-Me-Phenyl 136 4 2,5-di-Me-Phenyl 53 1 4-F-Phenyl 137 1 2,6-di-Me-Phenyl 54 2 4-F-Phenyl 138 2 2,6-di-Me-Phenyl 55 3 4-F-Phenyl 139 3 2,6-di-Me-Phenyl 56 4 4-F-Phenyl 140 4 2,6-di-Me-Phenyl 57 1 3-F-Phenyl 141 1 2,6-di-iPr-Phenyl 58 2 3-F-Phenyl 142 2 2,6-di-iPr-Phenyl 59 3 3-F-Phenyl 143 3 2,6-di-iPr-Phenyl 60 4 3-F-Phenyl 144 4 2,6-di-iPr-Phenyl 61 1 2-F-Phenyl 145 1 2-morpholino-phenyl 62 2 2-F-Phenyl 146 2 2-morpholino-phenyl 63 3 2-F-Phenyl 147 3 2-morpholino-phenyl 64 4 2-F-Phenyl 148 4 2-morpholino-phenyl 65 1 4-Cl-Phenyl 149 1 3-morpholino-phenyl 66 2 4-Cl-Phenyl 150 2 3-morpholino-phenyl 67 3 4-Cl-Phenyl 151 3 3-morpholino-phenyl 68 4 4-Cl-Phenyl 152 4 3-morpholino-phenyl 69 1 3-Cl-Phenyl 153 1 4-morpholino-phenyl 70 2 3-Cl-Phenyl 154 2 4-morpholino-phenyl 71 3 3-Cl-Phenyl 155 3 4-morpholino-phenyl 72 4 3-Cl-Phenyl 156 4 4-morpholino-phenyl 73 1 2-Cl-Phenyl 157 1 4-CN-2-morpholino-phenyl 74 2 2-Cl-Phenyl 158 2 4-CN-2-morpholino-phenyl 75 3 2-Cl-Phenyl 159 3 4-CN-2-morpholino-phenyl 76 4 2-Cl-Phenyl 160 4 4-CN-2-morpholino-phenyl 77 1 4-Br-Phenyl 161 1 4-CH.sub.3-2-morpholino-phenyl 78 2 4-Br-Phenyl 162 2 4-CH.sub.3-2-morpholino-phenyl 79 3 4-Br-Phenyl 163 3 4-CH.sub.3-2-morpholino-phenyl 80 4 4-Br-Phenyl 164 4 4-CH.sub.3-2-morpholino-phenyl 81 1 3-Br-Phenyl 165 1 4-OH-2-morpholino-phenyl 82 2 3-Br-Phenyl 166 2 4-OH-2-morpholino-phenyl 83 3 3-Br-Phenyl 167 3 4-OH-2-morpholino-phenyl 84 4 3-Br-Phenyl 168 4 4-OH-2-morpholino-phenyl 85 1 naphthylen-1-yl 173 1 naphthylen-2-yl 86 2 naphthylen-1-yl 174 2 naphthylen-2-yl 87 3 naphthylen-1-yl 175 3 naphthylen-2-yl 88 4 naphthylen-1-yl 176 4 naphthylen-2-yl

    [2024] Exemplary embodiments include compounds having the formula (XXII)

    ##STR00437##

    [2025] or a pharmaceutically acceptable salt form thereof defined herein below in Table 16.

    TABLE-US-00016 TABLE 16 Entry n R.sup.7 R.sup.3 1 1 H Phenyl 2 2 H Phenyl 3 3 H Phenyl 4 4 H Phenyl 5 1 Me Phenyl 6 2 Me Phenyl 7 3 Me Phenyl 8 4 Me Phenyl 9 1 CH.sub.2Ph Phenyl 10 2 CH.sub.2Ph Phenyl 11 3 CH.sub.2Ph Phenyl 12 4 CH.sub.2Ph Phenyl 13 1 COMe Phenyl 14 2 COMe Phenyl 15 3 COMe Phenyl 16 4 COMe Phenyl 17 1 CO.sub.2Me Phenyl 18 2 CO.sub.2Me Phenyl 19 3 CO.sub.2Me Phenyl 20 4 CO.sub.2Me Phenyl 21 1 CO.sub.2tBu Phenyl 22 2 CO.sub.2tBu Phenyl 23 3 CO.sub.2tBu Phenyl 24 4 CO.sub.2tBu Phenyl 25 1 CONHMe Phenyl 26 2 CONHMe Phenyl 27 3 CONHMe Phenyl 28 4 CONHMe Phenyl 29 1 SO.sub.2Me Phenyl 30 2 SO.sub.2Me Phenyl 31 3 SO.sub.2Me Phenyl 32 4 SO.sub.2Me Phenyl 33 1 SO.sub.2NH.sub.2 Phenyl 34 2 SO.sub.2NH.sub.2 Phenyl 35 3 SO.sub.2NH.sub.2 Phenyl 36 4 SO.sub.2NH.sub.2 Phenyl 37 1 H 3-OH-Phenyl 38 2 H 3-OH-Phenyl 39 3 H 3-OH-Phenyl 40 4 H 3-OH-Phenyl 41 1 Me 3-OH-Phenyl 42 2 Me 3-OH-Phenyl 43 3 Me 3-OH-Phenyl 44 4 Me 3-OH-Phenyl 45 1 CH.sub.2Ph 3-OH-Phenyl 46 2 CH.sub.2Ph 3-OH-Phenyl 47 3 CH.sub.2Ph 3-OH-Phenyl 48 4 CH.sub.2Ph 3-OH-Phenyl 49 1 COMe 3-OH-Phenyl 50 2 COMe 3-OH-Phenyl 51 3 COMe 3-OH-Phenyl 52 4 COMe 3-OH-Phenyl 53 1 CO.sub.2Me 3-OH-Phenyl 54 2 CO.sub.2Me 3-OH-Phenyl 55 3 CO.sub.2Me 3-OH-Phenyl 56 4 CO.sub.2Me 3-OH-Phenyl 57 1 CO.sub.2tBu 3-OH-Phenyl 58 2 CO.sub.2tBu 3-OH-Phenyl 59 3 CO.sub.2tBu 3-OH-Phenyl 60 4 CO.sub.2tBu 3-OH-Phenyl 61 1 CONHMe 3-OH-Phenyl 62 2 CONHMe 3-OH-Phenyl 63 3 CONHMe 3-OH-Phenyl 64 4 CONHMe 3-OH-Phenyl 65 1 SO.sub.2Me 3-OH-Phenyl 66 2 SO.sub.2Me 3-OH-Phenyl 67 3 SO.sub.2Me 3-OH-Phenyl 68 4 SO.sub.2Me 3-OH-Phenyl 69 1 SO.sub.2NH.sub.2 3-OH-Phenyl 70 2 SO.sub.2NH.sub.2 3-OH-Phenyl 71 3 SO.sub.2NH.sub.2 3-OH-Phenyl 72 4 SO.sub.2NH.sub.2 3-OH-Phenyl 73 1 H 4-NO.sub.2-Phenyl 74 2 H 4-NO.sub.2-Phenyl 75 3 H 4-NO.sub.2-Phenyl 76 4 H 4-NO.sub.2-Phenyl 77 1 Me 4-NO.sub.2-Phenyl 78 2 Me 4-NO.sub.2-Phenyl 79 3 Me 4-NO.sub.2-Phenyl 80 4 Me 4-NO.sub.2-Phenyl 81 1 CH.sub.2Ph 4-NO.sub.2-Phenyl 82 2 CH.sub.2Ph 4-NO.sub.2-Phenyl 83 3 CH.sub.2Ph 4-NO.sub.2-Phenyl 84 4 CH.sub.2Ph 4-NO.sub.2-Phenyl 85 1 COMe 4-NO.sub.2-Phenyl 86 2 COMe 4-NO.sub.2-Phenyl 87 3 COMe 4-NO.sub.2-Phenyl 88 4 COMe 4-NO.sub.2-Phenyl 89 1 CO.sub.2Me 4-NO.sub.2-Phenyl 90 2 CO.sub.2Me 4-NO.sub.2-Phenyl 91 3 CO.sub.2Me 4-NO.sub.2-Phenyl 92 4 CO.sub.2Me 4-NO.sub.2-Phenyl 93 1 CO.sub.2tBu 4-NO.sub.2-Phenyl 94 2 CO.sub.2tBu 4-NO.sub.2-Phenyl 95 3 CO.sub.2tBu 4-NO.sub.2-Phenyl 96 4 CO.sub.2tBu 4-NO.sub.2-Phenyl 97 1 CONHMe 4-NO.sub.2-Phenyl 98 2 CONHMe 4-NO.sub.2-Phenyl 99 3 CONHMe 4-NO.sub.2-Phenyl 100 4 CONHMe 4-NO.sub.2-Phenyl 101 1 SO.sub.2Me 4-NO.sub.2-Phenyl 102 2 SO.sub.2Me 4-NO.sub.2-Phenyl 103 3 SO.sub.2Me 4-NO.sub.2-Phenyl 104 4 SO.sub.2Me 4-NO.sub.2-Phenyl 105 1 SO.sub.2NH.sub.2 4-NO.sub.2-Phenyl 106 2 SO.sub.2NH.sub.2 4-NO.sub.2-Phenyl 107 3 SO.sub.2NH.sub.2 4-NO.sub.2-Phenyl 108 4 SO.sub.2NH.sub.2 4-NO.sub.2-Phenyl 109 1 H 3-OMe-Phenyl 110 2 H 3-OMe-Phenyl 111 3 H 3-OMe-Phenyl 112 4 H 3-OMe-Phenyl 113 1 Me 3-OMe-Phenyl 114 2 Me 3-OMe-Phenyl 115 3 Me 3-OMe-Phenyl 116 4 Me 3-OMe-Phenyl 117 1 CH.sub.2Ph 3-OMe-Phenyl 118 2 CH.sub.2Ph 3-OMe-Phenyl 119 3 CH.sub.2Ph 3-OMe-Phenyl 120 4 CH.sub.2Ph 3-OMe-Phenyl 121 1 COMe 3-OMe-Phenyl 122 2 COMe 3-OMe-Phenyl 123 3 COMe 3-OMe-Phenyl 124 4 COMe 3-OMe-Phenyl 125 1 CO.sub.2Me 3-OMe-Phenyl 126 2 CO.sub.2Me 3-OMe-Phenyl 127 3 CO.sub.2Me 3-OMe-Phenyl 128 4 CO.sub.2Me 3-OMe-Phenyl 129 1 CO.sub.2tBu 3-OMe-Phenyl 130 2 CO.sub.2tBu 3-OMe-Phenyl 131 3 CO.sub.2tBu 3-OMe-Phenyl 132 4 CO.sub.2tBu 3-OMe-Phenyl 133 1 CONHMe 3-OMe-Phenyl 134 2 CONHMe 3-OMe-Phenyl 135 3 CONHMe 3-OMe-Phenyl 136 4 CONHMe 3-OMe-Phenyl 137 1 SO.sub.2Me 3-OMe-Phenyl 138 2 SO.sub.2Me 3-OMe-Phenyl 139 3 SO.sub.2Me 3-OMe-Phenyl 140 4 SO.sub.2Me 3-OMe-Phenyl 141 1 SO.sub.2NH.sub.2 3-OMe-Phenyl 142 2 SO.sub.2NH.sub.2 3-OMe-Phenyl 143 3 SO.sub.2NH.sub.2 3-OMe-Phenyl 144 4 SO.sub.2NH.sub.2 3-OMe-Phenyl 145 1 H 4-CN-Phenyl 146 2 H 4-CN-Phenyl 147 3 H 4-CN-Phenyl 148 4 H 4-CN-Phenyl 149 1 Me 4-CN-Phenyl 150 2 Me 4-CN-Phenyl 151 3 Me 4-CN-Phenyl 152 4 Me 4-CN-Phenyl 153 1 CH.sub.2Ph 4-CN-Phenyl 154 2 CH.sub.2Ph 4-CN-Phenyl 155 3 CH.sub.2Ph 4-CN-Phenyl 156 4 CH.sub.2Ph 4-CN-Phenyl 157 1 COMe 4-CN-Phenyl 158 2 COMe 4-CN-Phenyl 159 3 COMe 4-CN-Phenyl 160 4 COMe 4-CN-Phenyl 161 1 CO.sub.2Me 4-CN-Phenyl 162 2 CO.sub.2Me 4-CN-Phenyl 163 3 CO.sub.2Me 4-CN-Phenyl 164 4 CO.sub.2Me 4-CN-Phenyl 165 1 CO.sub.2tBu 4-CN-Phenyl 166 2 CO.sub.2tBu 4-CN-Phenyl 167 3 CO.sub.2tBu 4-CN-Phenyl 168 4 CO.sub.2tBu 4-CN-Phenyl 169 1 CONHMe 4-CN-Phenyl 170 2 CONHMe 4-CN-Phenyl 171 3 CONHMe 4-CN-Phenyl 172 4 CONHMe 4-CN-Phenyl 173 1 SO.sub.2Me 4-CN-Phenyl 174 2 SO.sub.2Me 4-CN-Phenyl 175 3 SO.sub.2Me 4-CN-Phenyl 176 4 SO.sub.2Me 4-CN-Phenyl 177 1 SO.sub.2NH.sub.2 4-CN-Phenyl 178 2 SO.sub.2NH.sub.2 4-CN-Phenyl 179 3 SO.sub.2NH.sub.2 4-CN-Phenyl 180 4 SO.sub.2NH.sub.2 4-CN-Phenyl 181 1 H 2-CN-Phenyl 182 2 H 2-CN-Phenyl 183 3 H 2-CN-Phenyl 184 4 H 2-CN-Phenyl 185 1 Me 2-CN-Phenyl 186 2 Me 2-CN-Phenyl 187 3 Me 2-CN-Phenyl 188 4 Me 2-CN-Phenyl 189 1 CH.sub.2Ph 2-CN-Phenyl 190 2 CH.sub.2Ph 2-CN-Phenyl 191 3 CH.sub.2Ph 2-CN-Phenyl 192 4 CH.sub.2Ph 2-CN-Phenyl 193 1 COMe 2-CN-Phenyl 194 2 COMe 2-CN-Phenyl 195 3 COMe 2-CN-Phenyl 196 4 COMe 2-CN-Phenyl 197 1 CO.sub.2Me 2-CN-Phenyl 198 2 CO.sub.2Me 2-CN-Phenyl 199 3 CO.sub.2Me 2-CN-Phenyl 200 4 CO.sub.2Me 2-CN-Phenyl 201 1 CO.sub.2tBu 2-CN-Phenyl 202 2 CO.sub.2tBu 2-CN-Phenyl 203 3 CO.sub.2tBu 2-CN-Phenyl 204 4 CO.sub.2tBu 2-CN-Phenyl 205 1 CONHMe 2-CN-Phenyl 206 2 CONHMe 2-CN-Phenyl 207 3 CONHMe 2-CN-Phenyl 208 4 CONHMe 2-CN-Phenyl 209 1 SO.sub.2Me 2-CN-Phenyl 210 2 SO.sub.2Me 2-CN-Phenyl 211 3 SO.sub.2Me 2-CN-Phenyl 212 4 SO.sub.2Me 2-CN-Phenyl 213 1 SO.sub.2NH.sub.2 2-CN-Phenyl 214 2 SO.sub.2NH.sub.2 2-CN-Phenyl 215 3 SO.sub.2NH.sub.2 2-CN-Phenyl 216 4 SO.sub.2NH.sub.2 2-CN-Phenyl 217 1 H 3-Me-Phenyl 218 2 H 3-Me-Phenyl 219 3 H 3-Me-Phenyl 220 4 H 3-Me-Phenyl 221 1 Me 3-Me-Phenyl 222 2 Me 3-Me-Phenyl 223 3 Me 3-Me-Phenyl 224 4 Me 3-Me-Phenyl 225 1 CH.sub.2Ph 3-Me-Phenyl 226 2 CH.sub.2Ph 3-Me-Phenyl 227 3 CH.sub.2Ph 3-Me-Phenyl 228 4 CH.sub.2Ph 3-Me-Phenyl 229 1 COMe 3-Me-Phenyl 230 2 COMe 3-Me-Phenyl 231 3 COMe 3-Me-Phenyl 232 4 COMe 3-Me-Phenyl 233 1 CO.sub.2Me 3-Me-Phenyl 234 2 CO.sub.2Me 3-Me-Phenyl 235 3 CO.sub.2Me 3-Me-Phenyl 236 4 CO.sub.2Me 3-Me-Phenyl 237 1 CO.sub.2tBu 3-Me-Phenyl 238 2 CO.sub.2tBu 3-Me-Phenyl 239 3 CO.sub.2tBu 3-Me-Phenyl 240 4 CO.sub.2tBu 3-Me-Phenyl 241 1 CONHMe 3-Me-Phenyl 242 2 CONHMe 3-Me-Phenyl 243 3 CONHMe 3-Me-Phenyl 244 4 CONHMe 3-Me-Phenyl 245 1 SO.sub.2Me 3-Me-Phenyl 246 2 SO.sub.2Me 3-Me-Phenyl 247 3 SO.sub.2Me 3-Me-Phenyl 248 4 SO.sub.2Me 3-Me-Phenyl 249 1 SO.sub.2NH.sub.2 3-Me-Phenyl 250 2 SO.sub.2NH.sub.2 3-Me-Phenyl 251 3 SO.sub.2NH.sub.2 3-Me-Phenyl 252 4 SO.sub.2NH.sub.2 3-Me-Phenyl 253 1 H 2-F-Phenyl 254 2 H 2-F-Phenyl 255 3 H 2-F-Phenyl 256 4 H 2-F-Phenyl 257 1 Me 2-F-Phenyl 258 2 Me 2-F-Phenyl 259 3 Me 2-F-Phenyl 260 4 Me 2-F-Phenyl 261 1 CH.sub.2Ph 2-F-Phenyl 262 2 CH.sub.2Ph 2-F-Phenyl 263 3 CH.sub.2Ph 2-F-Phenyl 264 4 CH.sub.2Ph 2-F-Phenyl 265 1 COMe 2-F-Phenyl 266 2 COMe 2-F-Phenyl 267 3 COMe 2-F-Phenyl 268 4 COMe 2-F-Phenyl 269 1 CO.sub.2Me 2-F-Phenyl 270 2 CO.sub.2Me 2-F-Phenyl 271 3 CO.sub.2Me 2-F-Phenyl 272 4 CO.sub.2Me 2-F-Phenyl 273 1 CO.sub.2tBu 2-F-Phenyl 274 2 CO.sub.2tBu 2-F-Phenyl 275 3 CO.sub.2tBu 2-F-Phenyl 276 4 CO.sub.2tBu 2-F-Phenyl 277 1 CONHMe 2-F-Phenyl 278 2 CONHMe 2-F-Phenyl 279 3 CONHMe 2-F-Phenyl 280 4 CONHMe 2-F-Phenyl 281 1 SO.sub.2Me 2-F-Phenyl 282 2 SO.sub.2Me 2-F-Phenyl 283 3 SO.sub.2Me 2-F-Phenyl 284 4 SO.sub.2Me 2-F-Phenyl 285 1 SO.sub.2NH.sub.2 2-F-Phenyl 286 2 SO.sub.2NH.sub.2 2-F-Phenyl 287 3 SO.sub.2NH.sub.2 2-F-Phenyl 288 4 SO.sub.2NH.sub.2 2-F-Phenyl 289 1 H 4-F-Phenyl 290 2 H 4-F-Phenyl 291 3 H 4-F-Phenyl 292 4 H 4-F-Phenyl 293 1 Me 4-F-Phenyl 294 2 Me 4-F-Phenyl 295 3 Me 4-F-Phenyl 296 4 Me 4-F-Phenyl 297 1 CH.sub.2Ph 4-F-Phenyl 298 2 CH.sub.2Ph 4-F-Phenyl 299 3 CH.sub.2Ph 4-F-Phenyl 300 4 CH.sub.2Ph 4-F-Phenyl 301 1 COMe 4-F-Phenyl 302 2 COMe 4-F-Phenyl 303 3 COMe 4-F-Phenyl 304 4 COMe 4-F-Phenyl 305 1 CO.sub.2Me 4-F-Phenyl 306 2 CO.sub.2Me 4-F-Phenyl 307 3 CO.sub.2Me 4-F-Phenyl 308 4 CO.sub.2Me 4-F-Phenyl 309 1 CO.sub.2tBu 4-F-Phenyl 310 2 CO.sub.2tBu 4-F-Phenyl 311 3 CO.sub.2tBu 4-F-Phenyl 312 4 CO.sub.2tBu 4-F-Phenyl 313 1 CONHMe 4-F-Phenyl 314 2 CONHMe 4-F-Phenyl 315 3 CONHMe 4-F-Phenyl 316 4 CONHMe 4-F-Phenyl 317 1 SO.sub.2Me 4-F-Phenyl 318 2 SO.sub.2Me 4-F-Phenyl 319 3 SO.sub.2Me 4-F-Phenyl 320 4 SO.sub.2Me 4-F-Phenyl 321 1 SO.sub.2NH.sub.2 4-F-Phenyl 322 2 SO.sub.2NH.sub.2 4-F-Phenyl 323 3 SO.sub.2NH.sub.2 4-F-Phenyl 324 4 SO.sub.2NH.sub.2 4-F-Phenyl 325 1 H 3-Cl-Phenyl 326 2 H 3-Cl-Phenyl 327 3 H 3-Cl-Phenyl 328 4 H 3-Cl-Phenyl 329 1 Me 3-Cl-Phenyl 330 2 Me 3-Cl-Phenyl 331 3 Me 3-Cl-Phenyl 332 4 Me 3-Cl-Phenyl 333 1 CH.sub.2Ph 3-Cl-Phenyl 334 2 CH.sub.2Ph 3-Cl-Phenyl 335 3 CH.sub.2Ph 3-Cl-Phenyl 336 4 CH.sub.2Ph 3-Cl-Phenyl 337 1 COMe 3-Cl-Phenyl 338 2 COMe 3-Cl-Phenyl 339 3 COMe 3-Cl-Phenyl 340 4 COMe 3-Cl-Phenyl 341 1 CO.sub.2Me 3-Cl-Phenyl 342 2 CO.sub.2Me 3-Cl-Phenyl 343 3 CO.sub.2Me 3-Cl-Phenyl 344 4 CO.sub.2Me 3-Cl-Phenyl 345 1 CO.sub.2tBu 3-Cl-Phenyl 346 2 CO.sub.2tBu 3-Cl-Phenyl 347 3 CO.sub.2tBu 3-Cl-Phenyl 348 4 CO.sub.2tBu 3-Cl-Phenyl 349 1 CONHMe 3-Cl-Phenyl 350 2 CONHMe 3-Cl-Phenyl 351 3 CONHMe 3-Cl-Phenyl 352 4 CONHMe 3-Cl-Phenyl 353 1 SO.sub.2Me 3-Cl-Phenyl 354 2 SO.sub.2Me 3-Cl-Phenyl 355 3 SO.sub.2Me 3-Cl-Phenyl 356 4 SO.sub.2Me 3-Cl-Phenyl 357 1 SO.sub.2NH.sub.2 3-Cl-Phenyl 358 2 SO.sub.2NH.sub.2 3-Cl-Phenyl 359 3 SO.sub.2NH.sub.2 3-Cl-Phenyl 360 4 SO.sub.2NH.sub.2 3-Cl-Phenyl 361 1 H 2-Br-Phenyl 362 2 H 2-Br-Phenyl 363 3 H 2-Br-Phenyl 364 4 H 2-Br-Phenyl 365 1 Me 2-Br-Phenyl 366 2 Me 2-Br-Phenyl 367 3 Me 2-Br-Phenyl 368 4 Me 2-Br-Phenyl 369 1 CH.sub.2Ph 2-Br-Phenyl 370 2 CH.sub.2Ph 2-Br-Phenyl 371 3 CH.sub.2Ph 2-Br-Phenyl 372 4 CH.sub.2Ph 2-Br-Phenyl 373 1 COMe 2-Br-Phenyl 374 2 COMe 2-Br-Phenyl 375 3 COMe 2-Br-Phenyl 376 4 COMe 2-Br-Phenyl 377 1 CO.sub.2Me 2-Br-Phenyl 378 2 CO.sub.2Me 2-Br-Phenyl 379 3 CO.sub.2Me 2-Br-Phenyl 380 4 CO.sub.2Me 2-Br-Phenyl 381 1 CO.sub.2tBu 2-Br-Phenyl 382 2 CO.sub.2tBu 2-Br-Phenyl 383 3 CO.sub.2tBu 2-Br-Phenyl 384 4 CO.sub.2tBu 2-Br-Phenyl 385 1 CONHMe 2-Br-Phenyl 386 2 CONHMe 2-Br-Phenyl 387 3 CONHMe 2-Br-Phenyl 388 4 CONHMe 2-Br-Phenyl 389 1 SO.sub.2Me 2-Br-Phenyl 390 2 SO.sub.2Me 2-Br-Phenyl 391 3 SO.sub.2Me 2-Br-Phenyl 392 4 SO.sub.2Me 2-Br-Phenyl 393 1 SO.sub.2NH.sub.2 2-Br-Phenyl 394 2 SO.sub.2NH.sub.2 2-Br-Phenyl 395 3 SO.sub.2NH.sub.2 2-Br-Phenyl 396 4 SO.sub.2NH.sub.2 2-Br-Phenyl 397 1 H 4-Br-Phenyl 398 2 H 4-Br-Phenyl 399 3 H 4-Br-Phenyl 400 4 H 4-Br-Phenyl 401 1 Me 4-Br-Phenyl 402 2 Me 4-Br-Phenyl 403 3 Me 4-Br-Phenyl 404 4 Me 4-Br-Phenyl 405 1 CH.sub.2Ph 4-Br-Phenyl 406 2 CH.sub.2Ph 4-Br-Phenyl 407 3 CH.sub.2Ph 4-Br-Phenyl 408 4 CH.sub.2Ph 4-Br-Phenyl 409 1 COMe 4-Br-Phenyl 410 2 COMe 4-Br-Phenyl 411 3 COMe 4-Br-Phenyl 412 4 COMe 4-Br-Phenyl 413 1 CO.sub.2Me 4-Br-Phenyl 414 2 CO.sub.2Me 4-Br-Phenyl 415 3 CO.sub.2Me 4-Br-Phenyl 416 4 CO.sub.2Me 4-Br-Phenyl 417 1 CO.sub.2tBu 4-Br-Phenyl 418 2 CO.sub.2tBu 4-Br-Phenyl 419 3 CO.sub.2tBu 4-Br-Phenyl 420 4 CO.sub.2tBu 4-Br-Phenyl 421 1 CONHMe 4-Br-Phenyl 422 2 CONHMe 4-Br-Phenyl 423 3 CONHMe 4-Br-Phenyl 424 4 CONHMe 4-Br-Phenyl 425 1 SO.sub.2Me 4-Br-Phenyl 426 2 SO.sub.2Me 4-Br-Phenyl 427 3 SO.sub.2Me 4-Br-Phenyl 428 4 SO.sub.2Me 4-Br-Phenyl 429 1 SO.sub.2NH.sub.2 4-Br-Phenyl 430 2 SO.sub.2NH.sub.2 4-Br-Phenyl 431 3 SO.sub.2NH.sub.2 4-Br-Phenyl 432 4 SO.sub.2NH.sub.2 4-Br-Phenyl 433 1 H 3-CF.sub.3-Phenyl 434 2 H 3-CF.sub.3-Phenyl 435 3 H 3-CF.sub.3-Phenyl 436 4 H 3-CF.sub.3-Phenyl 437 1 Me 3-CF.sub.3-Phenyl 438 2 Me 3-CF.sub.3-Phenyl 439 3 Me 3-CF.sub.3-Phenyl 440 4 Me 3-CF.sub.3-Phenyl 441 1 CH.sub.2Ph 3-CF.sub.3-Phenyl 442 2 CH.sub.2Ph 3-CF.sub.3-Phenyl 443 3 CH.sub.2Ph 3-CF.sub.3-Phenyl 444 4 CH.sub.2Ph 3-CF.sub.3-Phenyl 445 1 COMe 3-CF.sub.3-Phenyl 446 2 COMe 3-CF.sub.3-Phenyl 447 3 COMe 3-CF.sub.3-Phenyl 448 4 COMe 3-CF.sub.3-Phenyl 449 1 CO.sub.2Me 3-CF.sub.3-Phenyl 450 2 CO.sub.2Me 3-CF.sub.3-Phenyl 451 3 CO.sub.2Me 3-CF.sub.3-Phenyl 452 4 CO.sub.2Me 3-CF.sub.3-Phenyl 453 1 CO.sub.2tBu 3-CF.sub.3-Phenyl 454 2 CO.sub.2tBu 3-CF.sub.3-Phenyl 455 3 CO.sub.2tBu 3-CF.sub.3-Phenyl 456 4 CO.sub.2tBu 3-CF.sub.3-Phenyl 457 1 CONHMe 3-CF.sub.3-Phenyl 458 2 CONHMe 3-CF.sub.3-Phenyl 459 3 CONHMe 3-CF.sub.3-Phenyl 460 4 CONHMe 3-CF.sub.3-Phenyl 461 1 SO.sub.2Me 3-CF.sub.3-Phenyl 462 2 SO.sub.2Me 3-CF.sub.3-Phenyl 463 3 SO.sub.2Me 3-CF.sub.3-Phenyl 464 4 SO.sub.2Me 3-CF.sub.3-Phenyl 465 1 SO.sub.2NH.sub.2 3-CF.sub.3-Phenyl 466 2 SO.sub.2NH.sub.2 3-CF.sub.3-Phenyl 467 3 SO.sub.2NH.sub.2 3-CF.sub.3-Phenyl 468 4 SO.sub.2NH.sub.2 3-CF.sub.3-Phenyl 469 1 H 2-iPr-Phenyl 470 2 H 2-iPr-Phenyl 471 3 H 2-iPr-Phenyl 472 4 H 2-iPr-Phenyl 473 1 Me 2-iPr-Phenyl 474 2 Me 2-iPr-Phenyl 475 3 Me 2-iPr-Phenyl 476 4 Me 2-iPr-Phenyl 477 1 CH.sub.2Ph 2-iPr-Phenyl 478 2 CH.sub.2Ph 2-iPr-Phenyl 479 3 CH.sub.2Ph 2-iPr-Phenyl 480 4 CH.sub.2Ph 2-iPr-Phenyl 481 1 COMe 2-iPr-Phenyl 482 2 COMe 2-iPr-Phenyl 483 3 COMe 2-iPr-Phenyl 484 4 COMe 2-iPr-Phenyl 485 1 CO.sub.2Me 2-iPr-Phenyl 486 2 CO.sub.2Me 2-iPr-Phenyl 487 3 CO.sub.2Me 2-iPr-Phenyl 488 4 CO.sub.2Me 2-iPr-Phenyl 489 1 CO.sub.2tBu 2-iPr-Phenyl 490 2 CO.sub.2tBu 2-iPr-Phenyl 491 3 CO.sub.2tBu 2-iPr-Phenyl 492 4 CO.sub.2tBu 2-iPr-Phenyl 493 1 CONHMe 2-iPr-Phenyl 494 2 CONHMe 2-iPr-Phenyl 495 3 CONHMe 2-iPr-Phenyl 496 4 CONHMe 2-iPr-Phenyl 497 1 SO.sub.2Me 2-iPr-Phenyl 498 2 SO.sub.2Me 2-iPr-Phenyl 499 3 SO.sub.2Me 2-iPr-Phenyl 500 4 SO.sub.2Me 2-iPr-Phenyl 501 1 SO.sub.2NH.sub.2 2-iPr-Phenyl 502 2 SO.sub.2NH.sub.2 2-iPr-Phenyl 503 3 SO.sub.2NH.sub.2 2-iPr-Phenyl 504 4 SO.sub.2NH.sub.2 2-iPr-Phenyl 505 1 H 4-iPr-Phenyl 506 2 H 4-iPr-Phenyl 507 3 H 4-iPr-Phenyl 508 4 H 4-iPr-Phenyl 509 1 Me 4-iPr-Phenyl 510 2 Me 4-iPr-Phenyl 511 3 Me 4-iPr-Phenyl 512 4 Me 4-iPr-Phenyl 513 1 CH.sub.2Ph 4-iPr-Phenyl 514 2 CH.sub.2Ph 4-iPr-Phenyl 515 3 CH.sub.2Ph 4-iPr-Phenyl 516 4 CH.sub.2Ph 4-iPr-Phenyl 517 1 COMe 4-iPr-Phenyl 518 2 COMe 4-iPr-Phenyl 519 3 COMe 4-iPr-Phenyl 520 4 COMe 4-iPr-Phenyl 521 1 CO.sub.2Me 4-iPr-Phenyl 522 2 CO.sub.2Me 4-iPr-Phenyl 523 3 CO.sub.2Me 4-iPr-Phenyl 524 4 CO.sub.2Me 4-iPr-Phenyl 525 1 CO.sub.2tBu 4-iPr-Phenyl 526 2 CO.sub.2tBu 4-iPr-Phenyl 527 3 CO.sub.2tBu 4-iPr-Phenyl 528 4 CO.sub.2tBu 4-iPr-Phenyl 529 1 CONHMe 4-iPr-Phenyl 530 2 CONHMe 4-iPr-Phenyl 531 3 CONHMe 4-iPr-Phenyl 532 4 CONHMe 4-iPr-Phenyl 533 1 SO.sub.2Me 4-iPr-Phenyl 534 2 SO.sub.2Me 4-iPr-Phenyl 535 3 SO.sub.2Me 4-iPr-Phenyl 536 4 SO.sub.2Me 4-iPr-Phenyl 537 1 SO.sub.2NH.sub.2 4-iPr-Phenyl 538 2 SO.sub.2NH.sub.2 4-iPr-Phenyl 539 3 SO.sub.2NH.sub.2 4-iPr-Phenyl 540 4 SO.sub.2NH.sub.2 4-iPr-Phenyl 541 1 H 3-NH.sub.2-Phenyl 542 2 H 3-NH.sub.2-Phenyl 543 3 H 3-NH.sub.2-Phenyl 544 4 H 3-NH.sub.2-Phenyl 545 1 Me 3-NH.sub.2-Phenyl 546 2 Me 3-NH.sub.2-Phenyl 547 3 Me 3-NH.sub.2-Phenyl 548 4 Me 3-NH.sub.2-Phenyl 549 1 CH.sub.2Ph 3-NH.sub.2-Phenyl 550 2 CH.sub.2Ph 3-NH.sub.2-Phenyl 551 3 CH.sub.2Ph 3-NH.sub.2-Phenyl 552 4 CH.sub.2Ph 3-NH.sub.2-Phenyl 553 1 COMe 3-NH.sub.2-Phenyl 554 2 COMe 3-NH.sub.2-Phenyl 555 3 COMe 3-NH.sub.2-Phenyl 556 4 COMe 3-NH.sub.2-Phenyl 557 1 CO.sub.2Me 3-NH.sub.2-Phenyl 558 2 CO.sub.2Me 3-NH.sub.2-Phenyl 559 3 CO.sub.2Me 3-NH.sub.2-Phenyl 560 4 CO.sub.2Me 3-NH.sub.2-Phenyl 561 1 CO.sub.2tBu 3-NH.sub.2-Phenyl 562 2 CO.sub.2tBu 3-NH.sub.2-Phenyl 563 3 CO.sub.2tBu 3-NH.sub.2-Phenyl 564 4 CO.sub.2tBu 3-NH.sub.2-Phenyl 565 1 CONHMe 3-NH.sub.2-Phenyl 566 2 CONHMe 3-NH.sub.2-Phenyl 567 3 CONHMe 3-NH.sub.2-Phenyl 568 4 CONHMe 3-NH.sub.2-Phenyl 569 1 SO.sub.2Me 3-NH.sub.2-Phenyl 570 2 SO.sub.2Me 3-NH.sub.2-Phenyl 571 3 SO.sub.2Me 3-NH.sub.2-Phenyl 572 4 SO.sub.2Me 3-NH.sub.2-Phenyl 573 1 SO.sub.2NH.sub.2 3-NH.sub.2-Phenyl 574 2 SO.sub.2NH.sub.2 3-NH.sub.2-Phenyl 575 3 SO.sub.2NH.sub.2 3-NH.sub.2-Phenyl 576 4 SO.sub.2NH.sub.2 3-NH.sub.2-Phenyl 577 1 H 2,4-di-Me-Phenyl 578 2 H 2,4-di-Me-Phenyl 579 3 H 2,4-di-Me-Phenyl 580 4 H 2,4-di-Me-Phenyl 581 1 Me 2,4-di-Me-Phenyl 582 2 Me 2,4-di-Me-Phenyl 583 3 Me 2,4-di-Me-Phenyl 584 4 Me 2,4-di-Me-Phenyl 585 1 CH.sub.2Ph 2,4-di-Me-Phenyl 586 2 CH.sub.2Ph 2,4-di-Me-Phenyl 587 3 CH.sub.2Ph 2,4-di-Me-Phenyl 588 4 CH.sub.2Ph 2,4-di-Me-Phenyl 589 1 COMe 2,4-di-Me-Phenyl 590 2 COMe 2,4-di-Me-Phenyl 591 3 COMe 2,4-di-Me-Phenyl 592 4 COMe 2,4-di-Me-Phenyl 593 1 CO.sub.2Me 2,4-di-Me-Phenyl 594 2 CO.sub.2Me 2,4-di-Me-Phenyl 595 3 CO.sub.2Me 2,4-di-Me-Phenyl 596 4 CO.sub.2Me 2,4-di-Me-Phenyl 597 1 CO.sub.2tBu 2,4-di-Me-Phenyl 598 2 CO.sub.2tBu 2,4-di-Me-Phenyl 599 3 CO.sub.2tBu 2,4-di-Me-Phenyl 600 4 CO.sub.2tBu 2,4-di-Me-Phenyl 601 1 CONHMe 2,4-di-Me-Phenyl 602 2 CONHMe 2,4-di-Me-Phenyl 603 3 CONHMe 2,4-di-Me-Phenyl 604 4 CONHMe 2,4-di-Me-Phenyl 605 1 SO.sub.2Me 2,4-di-Me-Phenyl 606 2 SO.sub.2Me 2,4-di-Me-Phenyl 607 3 SO.sub.2Me 2,4-di-Me-Phenyl 608 4 SO.sub.2Me 2,4-di-Me-Phenyl 609 1 SO.sub.2NH.sub.2 2,4-di-Me-Phenyl 610 2 SO.sub.2NH.sub.2 2,4-di-Me-Phenyl 611 3 SO.sub.2NH.sub.2 2,4-di-Me-Phenyl 612 4 SO.sub.2NH.sub.2 2,4-di-Me-Phenyl 613 1 H 2,6-di-iPr-Phenyl 614 2 H 2,6-di-iPr-Phenyl 615 3 H 2,6-di-iPr-Phenyl 616 4 H 2,6-di-iPr-Phenyl 617 1 Me 2,6-di-iPr-Phenyl 618 2 Me 2,6-di-iPr-Phenyl 619 3 Me 2,6-di-iPr-Phenyl 620 4 Me 2,6-di-iPr-Phenyl 621 1 CH.sub.2Ph 2,6-di-iPr-Phenyl 622 2 CH.sub.2Ph 2,6-di-iPr-Phenyl 623 3 CH.sub.2Ph 2,6-di-iPr-Phenyl 624 3 CH.sub.2Ph 2,6-di-iPr-Phenyl 625 1 COMe 2,6-di-iPr-Phenyl 626 2 COMe 2,6-di-iPr-Phenyl 627 3 COMe 2,6-di-iPr-Phenyl 628 4 COMe 2,6-di-iPr-Phenyl 629 1 CO.sub.2Me 2,6-di-iPr-Phenyl 630 2 CO.sub.2Me 2,6-di-iPr-Phenyl 631 3 CO.sub.2Me 2,6-di-iPr-Phenyl 632 4 CO.sub.2Me 2,6-di-iPr-Phenyl 633 1 CO.sub.2tBu 2,6-di-iPr-Phenyl 634 2 CO.sub.2tBu 2,6-di-iPr-Phenyl 635 3 CO.sub.2tBu 2,6-di-iPr-Phenyl 636 4 CO.sub.2tBu 2,6-di-iPr-Phenyl 637 1 CONHMe 2,6-di-iPr-Phenyl 638 2 CONHMe 2,6-di-iPr-Phenyl 639 3 CONHMe 2,6-di-iPr-Phenyl 640 4 CONHMe 2,6-di-iPr-Phenyl 641 1 SO.sub.2Me 2,6-di-iPr-Phenyl 642 2 SO.sub.2Me 2,6-di-iPr-Phenyl 643 3 SO.sub.2Me 2,6-di-iPr-Phenyl 644 4 SO.sub.2Me 2,6-di-iPr-Phenyl 645 1 SO.sub.2NH.sub.2 2,6-di-iPr-Phenyl 646 2 SO.sub.2NH.sub.2 2,6-di-iPr-Phenyl 647 3 SO.sub.2NH.sub.2 2,6-di-iPr-Phenyl 648 4 SO.sub.2NH.sub.2 2,6-di-iPr-Phenyl 649 1 H 3-Ph-Phenyl 650 2 H 3-Ph-Phenyl 651 3 H 3-Ph-Phenyl 652 4 H 3-Ph-Phenyl 653 1 Me 3-Ph-Phenyl 654 2 Me 3-Ph-Phenyl 655 3 Me 3-Ph-Phenyl 656 4 Me 3-Ph-Phenyl 657 1 CH.sub.2Ph 3-Ph-Phenyl 658 2 CH.sub.2Ph 3-Ph-Phenyl 659 3 CH.sub.2Ph 3-Ph-Phenyl 660 4 CH.sub.2Ph 3-Ph-Phenyl 661 1 COMe 3-Ph-Phenyl 662 2 COMe 3-Ph-Phenyl 663 3 COMe 3-Ph-Phenyl 664 4 COMe 3-Ph-Phenyl 665 1 CO.sub.2Me 3-Ph-Phenyl 666 2 CO.sub.2Me 3-Ph-Phenyl 667 3 CO.sub.2Me 3-Ph-Phenyl 668 4 CO.sub.2Me 3-Ph-Phenyl 669 1 CO.sub.2tBu 3-Ph-Phenyl 670 2 CO.sub.2tBu 3-Ph-Phenyl 671 3 CO.sub.2tBu 3-Ph-Phenyl 672 4 CO.sub.2tBu 3-Ph-Phenyl 673 1 CONHMe 3-Ph-Phenyl 674 2 CONHMe 3-Ph-Phenyl 675 3 CONHMe 3-Ph-Phenyl 676 4 CONHMe 3-Ph-Phenyl 677 1 SO.sub.2Me 3-Ph-Phenyl 678 2 SO.sub.2Me 3-Ph-Phenyl 679 3 SO.sub.2Me 3-Ph-Phenyl 680 4 SO.sub.2Me 3-Ph-Phenyl 681 1 SO.sub.2NH.sub.2 3-Ph-Phenyl 682 2 SO.sub.2NH.sub.2 3-Ph-Phenyl 683 3 SO.sub.2NH.sub.2 3-Ph-Phenyl 684 4 SO.sub.2NH.sub.2 3-Ph-Phenyl 685 1 H 2-morpholino-phenyl 686 2 H 2-morpholino-phenyl 687 3 H 2-morpholino-phenyl 688 4 H 2-morpholino-phenyl 689 1 Me 2-morpholino-phenyl 690 2 Me 2-morpholino-phenyl 691 3 Me 2-morpholino-phenyl 692 4 Me 2-morpholino-phenyl 693 1 CH.sub.2Ph 2-morpholino-phenyl 694 2 CH.sub.2Ph 2-morpholino-phenyl 695 3 CH.sub.2Ph 2-morpholino-phenyl 696 4 CH.sub.2Ph 2-morpholino-phenyl 697 1 COMe 2-morpholino-phenyl 698 2 COMe 2-morpholino-phenyl 699 3 COMe 2-morpholino-phenyl 700 4 COMe 2-morpholino-phenyl 701 1 CO.sub.2Me 2-morpholino-phenyl 702 2 CO.sub.2Me 2-morpholino-phenyl 703 3 CO.sub.2Me 2-morpholino-phenyl 704 4 CO.sub.2Me 2-morpholino-phenyl 705 1 CO.sub.2tBu 2-morpholino-phenyl 706 2 CO.sub.2tBu 2-morpholino-phenyl 707 3 CO.sub.2tBu 2-morpholino-phenyl 708 4 CO.sub.2tBu 2-morpholino-phenyl 709 1 CONHMe 2-morpholino-phenyl 710 2 CONHMe 2-morpholino-phenyl 711 3 CONHMe 2-morpholino-phenyl 712 4 CONHMe 2-morpholino-phenyl 713 1 SO.sub.2Me 2-morpholino-phenyl 714 2 SO.sub.2Me 2-morpholino-phenyl 715 3 SO.sub.2Me 2-morpholino-phenyl 716 4 SO.sub.2Me 2-morpholino-phenyl 717 1 SO.sub.2NH.sub.2 2-morpholino-phenyl 718 2 SO.sub.2NH.sub.2 2-morpholino-phenyl 719 3 SO.sub.2NH.sub.2 2-morpholino-phenyl 720 4 SO.sub.2NH.sub.2 2-morpholino-phenyl 721 1 H 4-morpholino-phenyl 722 2 H 4-morpholino-phenyl 723 3 H 4-morpholino-phenyl 724 4 H 4-morpholino-phenyl 725 1 CH.sub.2Ph 4-morpholino-phenyl 726 2 CH.sub.2Ph 4-morpholino-phenyl 727 3 CH.sub.2Ph 4-morpholino-phenyl 728 4 CH.sub.2Ph 4-morpholino-phenyl 729 1 COMe 4-morpholino-phenyl 730 2 COMe 4-morpholino-phenyl 731 3 COMe 4-morpholino-phenyl 732 4 COMe 4-morpholino-phenyl 733 1 CO.sub.2Me 4-morpholino-phenyl 734 2 CO.sub.2Me 4-morpholino-phenyl 735 3 CO.sub.2Me 4-morpholino-phenyl 736 4 CO.sub.2Me 4-morpholino-phenyl 737 1 CO.sub.2tBu 4-morpholino-phenyl 738 2 CO.sub.2tBu 4-morpholino-phenyl 739 3 CO.sub.2tBu 4-morpholino-phenyl 740 1 H naphthylen-1-yl 741 2 H naphthylen-1-yl 742 3 H naphthylen-1-yl 743 4 H naphthylen-1-yl 744 1 Me naphthylen-1-yl 745 2 Me naphthylen-1-yl 746 3 Me naphthylen-1-yl 747 4 Me naphthylen-1-yl 748 1 CH.sub.2Ph naphthylen-1-yl 749 2 CH.sub.2Ph naphthylen-1-yl 750 3 CH.sub.2Ph naphthylen-1-yl 751 4 CH.sub.2Ph naphthylen-1-yl 752 1 COMe naphthylen-1-yl 753 2 COMe naphthylen-1-yl 754 3 COMe naphthylen-1-yl 755 4 COMe naphthylen-1-yl 756 1 CO.sub.2Me naphthylen-1-yl 757 2 CO.sub.2Me naphthylen-1-yl 758 3 CO.sub.2Me naphthylen-1-yl 759 4 CO.sub.2Me naphthylen-1-yl 760 1 CO.sub.2tBu naphthylen-1-yl 761 2 CO.sub.2tBu naphthylen-1-yl 762 3 CO.sub.2tBu naphthylen-1-yl 763 4 CO.sub.2tBu naphthylen-1-yl 764 1 CONHMe naphthylen-1-yl 765 2 CONHMe naphthylen-1-yl 767 3 CONHMe naphthylen-1-yl 768 4 CONHMe naphthylen-1-yl 769 1 SO.sub.2Me naphthylen-1-yl 770 2 SO.sub.2Me naphthylen-1-yl 771 3 SO.sub.2Me naphthylen-1-yl 772 4 SO.sub.2Me naphthylen-1-yl 773 1 SO.sub.2NH.sub.2 naphthylen-1-yl 774 2 SO.sub.2NH.sub.2 naphthylen-1-yl 775 3 SO.sub.2NH.sub.2 naphthylen-1-yl 778 4 SO.sub.2NH.sub.2 naphthylen-1-yl 779 1 H 4-OH-Phenyl 780 2 H 4-OH-Phenyl 781 3 H 4-OH-Phenyl 782 4 H 4-OH-Phenyl 783 1 Me 4-OH-Phenyl 784 2 Me 4-OH-Phenyl 785 3 Me 4-OH-Phenyl 786 4 Me 4-OH-Phenyl 787 1 CH.sub.2Ph 4-OH-Phenyl 788 2 CH.sub.2Ph 4-OH-Phenyl 789 3 CH.sub.2Ph 4-OH-Phenyl 790 4 CH.sub.2Ph 4-OH-Phenyl 791 1 COMe 4-OH-Phenyl 792 2 COMe 4-OH-Phenyl 793 3 COMe 4-OH-Phenyl 794 4 COMe 4-OH-Phenyl 795 1 CO.sub.2Me 4-OH-Phenyl 796 2 CO.sub.2Me 4-OH-Phenyl 797 3 CO.sub.2Me 4-OH-Phenyl 798 4 CO.sub.2Me 4-OH-Phenyl 799 1 CO.sub.2tBu 4-OH-Phenyl 800 2 CO.sub.2tBu 4-OH-Phenyl 801 3 CO.sub.2tBu 4-OH-Phenyl 802 4 CO.sub.2tBu 4-OH-Phenyl 803 1 CONHMe 4-OH-Phenyl 804 2 CONHMe 4-OH-Phenyl 805 3 CONHMe 4-OH-Phenyl 806 4 CONHMe 4-OH-Phenyl 807 1 SO.sub.2Me 4-OH-Phenyl 808 2 SO.sub.2Me 4-OH-Phenyl 809 3 SO.sub.2Me 4-OH-Phenyl 810 4 SO.sub.2Me 4-OH-Phenyl 811 1 SO.sub.2NH.sub.2 4-OH-Phenyl 812 2 SO.sub.2NH.sub.2 4-OH-Phenyl 813 3 SO.sub.2NH.sub.2 4-OH-Phenyl 814 4 SO.sub.2NH.sub.2 4-OH-Phenyl 815 1 H 2-OH-Phenyl 816 2 H 2-OH-Phenyl 817 3 H 2-OH-Phenyl 818 4 H 2-OH-Phenyl 819 1 Me 2-OH-Phenyl 820 2 Me 2-OH-Phenyl 821 3 Me 2-OH-Phenyl 822 4 Me 2-OH-Phenyl 823 1 CH.sub.2Ph 2-OH-Phenyl 824 2 CH.sub.2Ph 2-OH-Phenyl 825 3 CH.sub.2Ph 2-OH-Phenyl 826 4 CH.sub.2Ph 2-OH-Phenyl 827 1 COMe 2-OH-Phenyl 828 2 COMe 2-OH-Phenyl 829 3 COMe 2-OH-Phenyl 830 4 COMe 2-OH-Phenyl 831 1 CO.sub.2Me 2-OH-Phenyl 832 2 CO.sub.2Me 2-OH-Phenyl 833 3 CO.sub.2Me 2-OH-Phenyl 834 4 CO.sub.2Me 2-OH-Phenyl 835 1 CO.sub.2tBu 2-OH-Phenyl 836 2 CO.sub.2tBu 2-OH-Phenyl 837 3 CO.sub.2tBu 2-OH-Phenyl 838 4 CO.sub.2tBu 2-OH-Phenyl 839 1 CONHMe 2-OH-Phenyl 840 2 CONHMe 2-OH-Phenyl 841 3 CONHMe 2-OH-Phenyl 842 4 CONHMe 2-OH-Phenyl 843 1 SO.sub.2Me 2-OH-Phenyl 844 2 SO.sub.2Me 2-OH-Phenyl 845 3 SO.sub.2Me 2-OH-Phenyl 846 4 SO.sub.2Me 2-OH-Phenyl 847 1 SO.sub.2NH.sub.2 2-OH-Phenyl 848 2 SO.sub.2NH.sub.2 2-OH-Phenyl 849 3 SO.sub.2NH.sub.2 2-OH-Phenyl 850 4 SO.sub.2NH.sub.2 2-OH-Phenyl 851 1 H 4-OMe-Phenyl 852 2 H 4-OMe-Phenyl 853 3 H 4-OMe-Phenyl 854 4 H 4-OMe-Phenyl 855 1 Me 4-OMe-Phenyl 856 2 Me 4-OMe-Phenyl 857 3 Me 4-OMe-Phenyl 858 4 Me 4-OMe-Phenyl 859 1 CH.sub.2Ph 4-OMe-Phenyl 860 2 CH.sub.2Ph 4-OMe-Phenyl 861 3 CH.sub.2Ph 4-OMe-Phenyl 862 4 CH.sub.2Ph 4-OMe-Phenyl 863 1 COMe 4-OMe-Phenyl 864 2 COMe 4-OMe-Phenyl 865 3 COMe 4-OMe-Phenyl 866 4 COMe 4-OMe-Phenyl 867 1 CO.sub.2Me 4-OMe-Phenyl 868 2 CO.sub.2Me 4-OMe-Phenyl 869 3 CO.sub.2Me 4-OMe-Phenyl 870 4 CO.sub.2Me 4-OMe-Phenyl 871 1 CO.sub.2tBu 4-OMe-Phenyl 872 2 CO.sub.2tBu 4-OMe-Phenyl 873 3 CO.sub.2tBu 4-OMe-Phenyl 874 4 CO.sub.2tBu 4-OMe-Phenyl 875 1 CONHMe 4-OMe-Phenyl 876 2 CONHMe 4-OMe-Phenyl 877 3 CONHMe 4-OMe-Phenyl 878 4 CONHMe 4-OMe-Phenyl 879 1 SO.sub.2Me 4-OMe-Phenyl 880 2 SO.sub.2Me 4-OMe-Phenyl 881 3 SO.sub.2Me 4-OMe-Phenyl 882 4 SO.sub.2Me 4-OMe-Phenyl 883 1 SO.sub.2NH.sub.2 4-OMe-Phenyl 884 2 SO.sub.2NH.sub.2 4-OMe-Phenyl 885 3 SO.sub.2NH.sub.2 4-OMe-Phenyl 886 4 SO.sub.2NH.sub.2 4-OMe-Phenyl 887 1 H 2-OMe-Phenyl 888 2 H 2-OMe-Phenyl 889 3 H 2-OMe-Phenyl 890 4 H 2-OMe-Phenyl 891 1 Me 2-OMe-Phenyl 892 2 Me 2-OMe-Phenyl 893 3 Me 2-OMe-Phenyl 894 4 Me 2-OMe-Phenyl 895 1 CH.sub.2Ph 2-OMe-Phenyl 896 2 CH.sub.2Ph 2-OMe-Phenyl 897 3 CH.sub.2Ph 2-OMe-Phenyl 898 4 CH.sub.2Ph 2-OMe-Phenyl 899 1 COMe 2-OMe-Phenyl 900 2 COMe 2-OMe-Phenyl 901 3 COMe 2-OMe-Phenyl 902 4 COMe 2-OMe-Phenyl 903 1 CO.sub.2Me 2-OMe-Phenyl 904 2 CO.sub.2Me 2-OMe-Phenyl 905 3 CO.sub.2Me 2-OMe-Phenyl 906 4 CO.sub.2Me 2-OMe-Phenyl 907 1 CO.sub.2tBu 2-OMe-Phenyl 908 2 CO.sub.2tBu 2-OMe-Phenyl 909 3 CO.sub.2tBu 2-OMe-Phenyl 910 4 CO.sub.2tBu 2-OMe-Phenyl 911 1 CONHMe 2-OMe-Phenyl 912 2 CONHMe 2-OMe-Phenyl 913 3 CONHMe 2-OMe-Phenyl 914 4 CONHMe 2-OMe-Phenyl 915 1 SO.sub.2Me 2-OMe-Phenyl 916 2 SO.sub.2Me 2-OMe-Phenyl 917 3 SO.sub.2Me 2-OMe-Phenyl 918 4 SO.sub.2Me 2-OMe-Phenyl 919 1 SO.sub.2NH.sub.2 2-OMe-Phenyl 920 2 SO.sub.2NH.sub.2 2-OMe-Phenyl 921 3 SO.sub.2NH.sub.2 2-OMe-Phenyl 922 4 SO.sub.2NH.sub.2 2-OMe-Phenyl 923 1 H 3-CN-Phenyl 924 2 H 3-CN-Phenyl 925 3 H 3-CN-Phenyl 926 4 H 3-CN-Phenyl 927 1 Me 3-CN-Phenyl 928 2 Me 3-CN-Phenyl 929 3 Me 3-CN-Phenyl 930 4 Me 3-CN-Phenyl 931 1 CH.sub.2Ph 3-CN-Phenyl 932 2 CH.sub.2Ph 3-CN-Phenyl 933 3 CH.sub.2Ph 3-CN-Phenyl 934 4 CH.sub.2Ph 3-CN-Phenyl 935 1 COMe 3-CN-Phenyl 936 2 COMe 3-CN-Phenyl 937 3 COMe 3-CN-Phenyl 938 4 COMe 3-CN-Phenyl 939 1 CO.sub.2Me 3-CN-Phenyl 940 2 CO.sub.2Me 3-CN-Phenyl 941 3 CO.sub.2Me 3-CN-Phenyl 942 4 CO.sub.2Me 3-CN-Phenyl 943 1 CO.sub.2tBu 3-CN-Phenyl 944 2 CO.sub.2tBu 3-CN-Phenyl 945 3 CO.sub.2tBu 3-CN-Phenyl 946 4 CO.sub.2tBu 3-CN-Phenyl 947 1 CONHMe 3-CN-Phenyl 948 2 CONHMe 3-CN-Phenyl 949 3 CONHMe 3-CN-Phenyl 950 4 CONHMe 3-CN-Phenyl 951 1 SO.sub.2Me 3-CN-Phenyl 952 2 SO.sub.2Me 3-CN-Phenyl 953 3 SO.sub.2Me 3-CN-Phenyl 954 4 SO.sub.2Me 3-CN-Phenyl 955 1 SO.sub.2NH.sub.2 3-CN-Phenyl 956 2 SO.sub.2NH.sub.2 3-CN-Phenyl 957 3 SO.sub.2NH.sub.2 3-CN-Phenyl 958 4 SO.sub.2NH.sub.2 3-CN-Phenyl 959 1 H 2-Me-Phenyl 960 2 H 2-Me-Phenyl 961 3 H 2-Me-Phenyl 962 4 H 2-Me-Phenyl 963 1 Me 2-Me-Phenyl 964 2 Me 2-Me-Phenyl 965 3 Me 2-Me-Phenyl 966 4 Me 2-Me-Phenyl 967 1 CH.sub.2Ph 2-Me-Phenyl 968 2 CH.sub.2Ph 2-Me-Phenyl 969 3 CH.sub.2Ph 2-Me-Phenyl 970 4 CH.sub.2Ph 2-Me-Phenyl 971 1 COMe 2-Me-Phenyl 972 2 COMe 2-Me-Phenyl 973 3 COMe 2-Me-Phenyl 974 4 COMe 2-Me-Phenyl 975 1 CO.sub.2Me 2-Me-Phenyl 976 2 CO.sub.2Me 2-Me-Phenyl 977 3 CO.sub.2Me 2-Me-Phenyl 978 4 CO.sub.2Me 2-CN-Phenyl 979 1 CO.sub.2tBu 2-Me-Phenyl 980 2 CO.sub.2tBu 2-Me-Phenyl 981 3 CO.sub.2tBu 2-Me-Phenyl 982 4 CO.sub.2tBu 2-Me-Phenyl 983 1 CONHMe 2-Me-Phenyl 984 2 CONHMe 2-Me-Phenyl 985 3 CONHMe 2-Me-Phenyl 986 4 CONHMe 2-Me-Phenyl 987 1 SO.sub.2Me 2-Me-Phenyl 988 2 SO.sub.2Me 2-Me-Phenyl 989 3 SO.sub.2Me 2-Me-Phenyl 990 4 SO.sub.2Me 2-Me-Phenyl 991 1 SO.sub.2NH.sub.2 2-Me-Phenyl 992 2 SO.sub.2NH.sub.2 2-Me-Phenyl 993 3 SO.sub.2NH.sub.2 2-Me-Phenyl 994 4 SO.sub.2NH.sub.2 2-Me-Phenyl 995 1 H 4-Me-Phenyl 996 2 H 4-Me-Phenyl 997 3 H 4-Me-Phenyl 998 4 H 4-Me-Phenyl 999 1 Me 4-Me-Phenyl 1000 2 Me 4-Me-Phenyl 1001 3 Me 4-Me-Phenyl 1002 4 Me 4-Me-Phenyl 1003 1 CH.sub.2Ph 4-Me-Phenyl 1004 2 CH.sub.2Ph 4-Me-Phenyl 1005 3 CH.sub.2Ph 4-Me-Phenyl 1006 4 CH.sub.2Ph 4-Me-Phenyl 1007 1 COMe 4-Me-Phenyl 1008 2 COMe 4-Me-Phenyl 1009 3 COMe 4-Me-Phenyl 1010 4 COMe 4-Me-Phenyl 1011 1 CO.sub.2Me 4-Me-Phenyl 1012 2 CO.sub.2Me 4-Me-Phenyl 1013 3 CO.sub.2Me 4-Me-Phenyl 1014 4 CO.sub.2Me 4-Me-Phenyl 1015 1 CO.sub.2tBu 4-Me-Phenyl 1016 2 CO.sub.2tBu 4-Me-Phenyl 1017 3 CO.sub.2tBu 4-Me-Phenyl 1018 4 CO.sub.2tBu 4-Me-Phenyl 1019 1 CONHMe 4-Me-Phenyl 1020 2 CONHMe 4-Me-Phenyl 1021 3 CONHMe 4-Me-Phenyl 1022 4 CONHMe 4-Me-Phenyl 1023 1 SO.sub.2Me 4-Me-Phenyl 1024 2 SO.sub.2Me 4-Me-Phenyl 1025 3 SO.sub.2Me 4-Me-Phenyl 1026 4 SO.sub.2Me 4-Me-Phenyl 1027 1 SO.sub.2NH.sub.2 4-Me-Phenyl 1028 2 SO.sub.2NH.sub.2 4-Me-Phenyl 1029 3 SO.sub.2NH.sub.2 4-Me-Phenyl 1030 4 SO.sub.2NH.sub.2 4-Me-Phenyl 1031 1 H 3-F-Phenyl 1032 2 H 3-F-Phenyl 1033 3 H 3-F-Phenyl 1034 4 H 3-F-Phenyl 1035 1 Me 3-F-Phenyl 1036 2 Me 3-F-Phenyl 1037 3 Me 3-F-Phenyl 1038 4 Me 3-F-Phenyl 1039 1 CH.sub.2Ph 3-F-Phenyl 1040 2 CH.sub.2Ph 3-F-Phenyl 1041 3 CH.sub.2Ph 3-F-Phenyl 1042 4 CH.sub.2Ph 3-F-Phenyl 1043 1 COMe 3-F-Phenyl 1044 2 COMe 3-F-Phenyl 1045 3 COMe 3-F-Phenyl 1046 4 COMe 3-F-Phenyl 1047 1 CO.sub.2Me 3-F-Phenyl 1048 2 CO.sub.2Me 3-F-Phenyl 1049 3 CO.sub.2Me 3-F-Phenyl 1050 4 CO.sub.2Me 3-F-Phenyl 1051 1 CO.sub.2tBu 3-F-Phenyl 1052 2 CO.sub.2tBu 3-F-Phenyl 1053 3 CO.sub.2tBu 3-F-Phenyl 1054 4 CO.sub.2tBu 3-F-Phenyl 1055 1 CONHMe 3-F-Phenyl 1056 2 CONHMe 3-F-Phenyl 1057 3 CONHMe 3-F-Phenyl 1058 4 CONHMe 3-F-Phenyl 1059 1 SO.sub.2Me 3-F-Phenyl 1060 2 SO.sub.2Me 3-F-Phenyl 1061 3 SO.sub.2Me 3-F-Phenyl 1062 4 SO.sub.2Me 3-F-Phenyl 1063 1 SO.sub.2NH.sub.2 3-F-Phenyl 1064 2 SO.sub.2NH.sub.2 3-F-Phenyl 1065 3 SO.sub.2NH.sub.2 3-F-Phenyl 1066 4 SO.sub.2NH.sub.2 3-F-Phenyl 1067 1 H 2-Cl-Phenyl 1068 2 H 2-Cl-Phenyl 1069 3 H 2-Cl-Phenyl 1070 4 H 2-Cl-Phenyl 1071 1 Me 2-Cl-Phenyl 1072 2 Me 2-Cl-Phenyl 1073 3 Me 2-Cl-Phenyl 1074 4 Me 2-Cl-Phenyl 1075 1 CH.sub.2Ph 2-Cl-Phenyl 1076 2 CH.sub.2Ph 2-Cl-Phenyl 1077 3 CH.sub.2Ph 2-Cl-Phenyl 1078 4 CH.sub.2Ph 2-Cl-Phenyl 1079 1 COMe 2-Cl-Phenyl 1080 2 COMe 2-Cl-Phenyl 1081 3 COMe 2-Cl-Phenyl 1082 4 COMe 2-Cl-Phenyl 1083 1 CO.sub.2Me 2-Cl-Phenyl 1084 2 CO.sub.2Me 2-Cl-Phenyl 1085 3 CO.sub.2Me 2-Cl-Phenyl 1086 4 CO.sub.2Me 2-Cl-Phenyl 1087 1 CO.sub.2tBu 2-Cl-Phenyl 1088 2 CO.sub.2tBu 2-Cl-Phenyl 1089 3 CO.sub.2tBu 2-Cl-Phenyl 1090 4 CO.sub.2tBu 2-Cl-Phenyl 1091 1 CONHMe 2-Cl-Phenyl 1092 2 CONHMe 2-Cl-Phenyl 1093 3 CONHMe 2-Cl-Phenyl 1094 4 CONHMe 2-Cl-Phenyl 1095 1 SO.sub.2Me 2-Cl-Phenyl 1096 2 SO.sub.2Me 2-Cl-Phenyl 1097 3 SO.sub.2Me 2-Cl-Phenyl 1098 4 SO.sub.2Me 2-Cl-Phenyl 1099 1 SO.sub.2NH.sub.2 2-Cl-Phenyl 1100 2 SO.sub.2NH.sub.2 2-Cl-Phenyl 1101 3 SO.sub.2NH.sub.2 2-Cl-Phenyl 1102 4 SO.sub.2NH.sub.2 2-Cl-Phenyl 1103 1 H 4-Cl-Phenyl 1104 2 H 4-Cl-Phenyl 1105 3 H 4-Cl-Phenyl 1106 4 H 4-Cl-Phenyl 1107 1 Me 4-Cl-Phenyl 1108 2 Me 4-Cl-Phenyl 1109 3 Me 4-Cl-Phenyl 1110 4 Me 4-Cl-Phenyl 1111 1 CH.sub.2Ph 4-Cl-Phenyl 1112 2 CH.sub.2Ph 4-Cl-Phenyl 1113 3 CH.sub.2Ph 4-Cl-Phenyl 1114 4 CH.sub.2Ph 4-Cl-Phenyl 1115 1 COMe 4-Cl-Phenyl 1116 2 COMe 4-Cl-Phenyl 1117 3 COMe 4-Cl-Phenyl 1118 4 COMe 4-Cl-Phenyl 1119 1 CO.sub.2Me 4-Cl-Phenyl 1120 2 CO.sub.2Me 4-Cl-Phenyl 1121 3 CO.sub.2Me 4-Cl-Phenyl 1122 4 CO.sub.2Me 4-Cl-Phenyl 1123 1 CO.sub.2tBu 4-Cl-Phenyl 1124 2 CO.sub.2tBu 4-Cl-Phenyl 1125 3 CO.sub.2tBu 4-Cl-Phenyl 1126 4 CO.sub.2tBu 4-Cl-Phenyl 1127 1 CONHMe 4-Cl-Phenyl 1128 2 CONHMe 4-Cl-Phenyl 1129 3 CONHMe 4-Cl-Phenyl 1130 4 CONHMe 4-Cl-Phenyl 1131 1 SO.sub.2Me 4-Cl-Phenyl 1132 2 SO.sub.2Me 4-Cl-Phenyl 1133 3 SO.sub.2Me 4-Cl-Phenyl 1134 4 SO.sub.2Me 4-Cl-Phenyl 1135 1 SO.sub.2NH.sub.2 4-Cl-Phenyl 1136 2 SO.sub.2NH.sub.2 4-Cl-Phenyl 1137 3 SO.sub.2NH.sub.2 4-Cl-Phenyl 1138 4 SO.sub.2NH.sub.2 4-Cl-Phenyl 1139 1 H 3-Br-Phenyl 1140 2 H 3-Br-Phenyl 1141 3 H 3-Br-Phenyl 1142 4 H 3-Br-Phenyl 1143 1 Me 3-Br-Phenyl 1144 2 Me 3-Br-Phenyl 1145 3 Me 3-Br-Phenyl 1146 4 Me 3-Br-Phenyl 1147 1 CH.sub.2Ph 3-Br-Phenyl 1148 2 CH.sub.2Ph 3-Br-Phenyl 1149 3 CH.sub.2Ph 3-Br-Phenyl 1150 4 CH.sub.2Ph 3-Br-Phenyl 1151 1 COMe 3-Br-Phenyl 1152 2 COMe 3-Br-Phenyl 1153 3 COMe 3-Br-Phenyl 1154 4 COMe 3-Br-Phenyl 1155 1 CO.sub.2Me 3-Br-Phenyl 1156 2 CO.sub.2Me 3-Br-Phenyl 1157 3 CO.sub.2Me 3-Br-Phenyl 1158 4 CO.sub.2Me 3-Br-Phenyl 1159 1 CO.sub.2tBu 3-Br-Phenyl 1160 2 CO.sub.2tBu 3-Br-Phenyl 1161 3 CO.sub.2tBu 3-Br-Phenyl 1162 4 CO.sub.2tBu 3-Br-Phenyl 1163 1 CONHMe 3-Br-Phenyl 1164 2 CONHMe 3-Br-Phenyl 1165 3 CONHMe 3-Br-Phenyl 1166 4 CONHMe 3-Br-Phenyl 1167 1 SO.sub.2Me 3-Br-Phenyl 1168 2 SO.sub.2Me 3-Br-Phenyl 1169 3 SO.sub.2Me 3-Br-Phenyl 1170 4 SO.sub.2Me 3-Br-Phenyl 1171 1 SO.sub.2NH.sub.2 3-Br-Phenyl 1172 2 SO.sub.2NH.sub.2 3-Br-Phenyl 1173 3 SO.sub.2NH.sub.2 3-Br-Phenyl 1174 4 SO.sub.2NH.sub.2 3-Br-Phenyl 1175 1 H 2-CF.sub.3-Phenyl 1176 2 H 2-CF.sub.3-Phenyl 1177 3 H 2-CF.sub.3-Phenyl 1178 4 H 2-CF.sub.3-Phenyl 1179 1 Me 2-CF.sub.3-Phenyl 1180 2 Me 2-CF.sub.3-Phenyl 1181 3 Me 2-CF.sub.3-Phenyl 1182 4 Me 2-CF.sub.3-Phenyl 1183 1 CH.sub.2Ph 2-CF.sub.3-Phenyl 1184 2 CH.sub.2Ph 2-CF.sub.3-Phenyl 1185 3 CH.sub.2Ph 2-CF.sub.3-Phenyl 1186 4 CH.sub.2Ph 2-CF.sub.3-Phenyl 1187 1 COMe 2-CF.sub.3-Phenyl 1188 2 COMe 2-CF.sub.3-Phenyl 1189 3 COMe 2-CF.sub.3-Phenyl 1190 4 COMe 2-CF.sub.3-Phenyl 1191 1 CO.sub.2Me 2-CF.sub.3-Phenyl 1192 2 CO.sub.2Me 2-CF.sub.3-Phenyl 1193 3 CO.sub.2Me 2-CF.sub.3-Phenyl 1194 4 CO.sub.2Me 2-CF.sub.3-Phenyl 1195 1 CO.sub.2tBu 2-CF.sub.3-Phenyl 1196 2 CO.sub.2tBu 2-CF.sub.3-Phenyl 1197 3 CO.sub.2tBu 2-CF.sub.3-Phenyl 1198 4 CO.sub.2tBu 2-CF.sub.3-Phenyl 1199 1 CONHMe 2-CF.sub.3-Phenyl 1200 2 CONHMe 2-CF.sub.3-Phenyl 1201 3 CONHMe 2-CF.sub.3-Phenyl 1202 4 CONHMe 2-CF.sub.3-Phenyl 1203 1 SO.sub.2Me 2-CF.sub.3-Phenyl 1204 2 SO.sub.2Me 2-CF.sub.3-Phenyl 1205 3 SO.sub.2Me 2-CF.sub.3-Phenyl 1206 4 SO.sub.2Me 2-CF.sub.3-Phenyl 1207 1 SO.sub.2NH.sub.2 2-CF.sub.3-Phenyl 1208 2 SO.sub.2NH.sub.2 2-CF.sub.3-Phenyl 1209 3 SO.sub.2NH.sub.2 2-CF.sub.3-Phenyl 1210 4 SO.sub.2NH.sub.2 2-CF.sub.3-Phenyl 1211 1 H 4-CF.sub.3-Phenyl 1212 2 H 4-CF.sub.3-Phenyl 1213 3 H 4-CF.sub.3-Phenyl 1214 4 H 4-CF.sub.3-Phenyl 1215 1 Me 4-CF.sub.3-Phenyl 1216 2 Me 4-CF.sub.3-Phenyl 1217 3 Me 4-CF.sub.3-Phenyl 1218 4 Me 4-CF.sub.3-Phenyl 1219 1 CH.sub.2Ph 4-CF.sub.3-Phenyl 1220 2 CH.sub.2Ph 4-CF.sub.3-Phenyl 1221 3 CH.sub.2Ph 4-CF.sub.3-Phenyl 1222 4 CH.sub.2Ph 4-CF.sub.3-Phenyl 1223 1 COMe 4-CF.sub.3-Phenyl 1224 2 COMe 4-CF.sub.3-Phenyl 1225 3 COMe 4-CF.sub.3-Phenyl 1226 4 COMe 4-CF.sub.3-Phenyl 1227 1 CO.sub.2Me 4-CF.sub.3-Phenyl 1228 2 CO.sub.2Me 4-CF.sub.3-Phenyl 1229 3 CO.sub.2Me 4-CF.sub.3-Phenyl 1230 4 CO.sub.2Me 4-CF.sub.3-Phenyl 1231 1 CO.sub.2tBu 4-CF.sub.3-Phenyl 1232 2 CO.sub.2tBu 4-CF.sub.3-Phenyl 1233 3 CO.sub.2tBu 4-CF.sub.3-Phenyl 1234 4 CO.sub.2tBu 4-CF.sub.3-Phenyl 1235 1 CONHMe 4-CF.sub.3-Phenyl 1236 2 CONHMe 4-CF.sub.3-Phenyl 1237 3 CONHMe 4-CF.sub.3-Phenyl 1238 4 CONHMe 4-CF.sub.3-Phenyl 1239 1 SO.sub.2Me 4-CF.sub.3-Phenyl 1240 2 SO.sub.2Me 4-CF.sub.3-Phenyl 1241 3 SO.sub.2Me 4-CF.sub.3-Phenyl 1242 4 SO.sub.2Me 4-CF.sub.3-Phenyl 1243 1 SO.sub.2NH.sub.2 4-CF.sub.3-Phenyl 1244 2 SO.sub.2NH.sub.2 4-CF.sub.3-Phenyl 1245 3 SO.sub.2NH.sub.2 4-CF.sub.3-Phenyl 1246 4 SO.sub.2NH.sub.2 4-CF.sub.3-Phenyl 1247 1 H 3-iPr-Phenyl 1248 2 H 3-iPr-Phenyl 1249 3 H 3-iPr-Phenyl 1250 4 H 3-iPr-Phenyl 1251 1 Me 3-iPr-Phenyl 1252 2 Me 3-iPr-Phenyl 1253 3 Me 3-iPr-Phenyl 1254 4 Me 3-iPr-Phenyl 1255 1 CH.sub.2Ph 3-iPr-Phenyl 1256 2 CH.sub.2Ph 3-iPr-Phenyl 1257 3 CH.sub.2Ph 3-iPr-Phenyl 1258 4 CH.sub.2Ph 3-iPr-Phenyl 1259 1 COMe 3-iPr-Phenyl 1260 2 COMe 3-iPr-Phenyl 1261 3 COMe 3-iPr-Phenyl 1262 4 COMe 3-iPr-Phenyl 1263 1 CO.sub.2Me 3-iPr-Phenyl 1264 2 CO.sub.2Me 3-iPr-Phenyl 1265 3 CO.sub.2Me 3-iPr-Phenyl 1266 4 CO.sub.2Me 3-iPr-Phenyl 1267 1 CO.sub.2tBu 3-iPr-Phenyl 1268 2 CO.sub.2tBu 3-iPr-Phenyl 1269 3 CO.sub.2tBu 3-iPr-Phenyl 1270 4 CO.sub.2tBu 3-iPr-Phenyl 1271 1 CONHMe 3-iPr-Phenyl 1272 2 CONHMe 3-iPr-Phenyl 1273 3 CONHMe 3-iPr-Phenyl 1274 4 CONHMe 3-iPr-Phenyl 1275 1 SO.sub.2Me 3-iPr-Phenyl 1276 2 SO.sub.2Me 3-iPr-Phenyl 1277 3 SO.sub.2Me 3-iPr-Phenyl 1278 4 SO.sub.2Me 3-iPr-Phenyl 1279 1 SO.sub.2NH.sub.2 3-iPr-Phenyl 1280 2 SO.sub.2NH.sub.2 3-iPr-Phenyl 1281 3 SO.sub.2NH.sub.2 3-iPr-Phenyl 1282 4 SO.sub.2NH.sub.2 3-iPr-Phenyl 1283 1 H 4-NH.sub.2-Phenyl 1284 2 H 4-NH.sub.2-Phenyl 1285 3 H 4-NH.sub.2-Phenyl 1286 4 H 4-NH.sub.2-Phenyl 1287 1 Me 4-NH.sub.2-Phenyl 1288 2 Me 4-NH.sub.2-Phenyl 1289 3 Me 4-NH.sub.2-Phenyl 1290 4 Me 4-NH.sub.2-Phenyl 1291 1 CH.sub.2Ph 4-NH.sub.2-Phenyl 1292 2 CH.sub.2Ph 4-NH.sub.2-Phenyl 1293 3 CH.sub.2Ph 4-NH.sub.2-Phenyl 1294 4 CH.sub.2Ph 4-NH.sub.2-Phenyl 1295 1 COMe 4-NH.sub.2-Phenyl 1296 2 COMe 4-NH.sub.2-Phenyl 1297 3 COMe 4-NH.sub.2-Phenyl 1298 4 COMe 4-NH.sub.2-Phenyl 1299 1 CO.sub.2Me 4-NH.sub.2-Phenyl 1300 2 CO.sub.2Me 4-NH.sub.2-Phenyl 1301 3 CO.sub.2Me 4-NH.sub.2-Phenyl 1302 4 CO.sub.2Me 4-NH.sub.2-Phenyl 1303 1 CO.sub.2tBu 4-NH.sub.2-Phenyl 1304 2 CO.sub.2tBu 4-NH.sub.2-Phenyl 1305 3 CO.sub.2tBu 4-NH.sub.2-Phenyl 1306 4 CO.sub.2tBu 4-NH.sub.2-Phenyl 1307 1 CONHMe 4-NH.sub.2-Phenyl 1308 2 CONHMe 4-NH.sub.2-Phenyl 1309 3 CONHMe 4-NH.sub.2-Phenyl 1310 4 CONHMe 4-NH.sub.2-Phenyl 1311 1 SO.sub.2Me 4-NH.sub.2-Phenyl 1312 2 SO.sub.2Me 4-NH.sub.2-Phenyl 1313 3 SO.sub.2Me 4-NH.sub.2-Phenyl 1314 4 SO.sub.2Me 4-NH.sub.2-Phenyl 1315 1 SO.sub.2NH.sub.2 4-NH.sub.2-Phenyl 1316 2 SO.sub.2NH.sub.2 4-NH.sub.2-Phenyl 1317 3 SO.sub.2NH.sub.2 4-NH.sub.2-Phenyl 1318 4 SO.sub.2NH.sub.2 4-NH.sub.2-Phenyl 1319 1 H 2-NH.sub.2-Phenyl 1320 2 H 2-NH.sub.2-Phenyl 1321 3 H 2-NH.sub.2-Phenyl 1322 4 H 2-NH.sub.2-Phenyl 1323 1 Me 2-NH.sub.2-Phenyl 1324 2 Me 2-NH.sub.2-Phenyl 1325 3 Me 2-NH.sub.2-Phenyl 1326 4 Me 2-NH.sub.2-Phenyl 1327 1 CH.sub.2Ph 2-NH.sub.2-Phenyl 1328 2 CH.sub.2Ph 2-NH.sub.2-Phenyl 1329 3 CH.sub.2Ph 2-NH.sub.2-Phenyl 1330 4 CH.sub.2Ph 2-NH.sub.2-Phenyl 1331 1 COMe 2-NH.sub.2-Phenyl 1332 2 COMe 2-NH.sub.2-Phenyl 1333 3 COMe 2-NH.sub.2-Phenyl 1334 4 COMe 2-NH.sub.2-Phenyl 1335 1 CO.sub.2Me 2-NH.sub.2-Phenyl 1336 2 CO.sub.2Me 2-NH.sub.2-Phenyl 1337 3 CO.sub.2Me 2-NH.sub.2-Phenyl 1338 4 CO.sub.2Me 2-NH.sub.2-Phenyl 1339 1 CO.sub.2tBu 2-NH.sub.2-Phenyl 1340 2 CO.sub.2tBu 2-NH.sub.2-Phenyl 1341 3 CO.sub.2tBu 2-NH.sub.2-Phenyl 1342 4 CO.sub.2tBu 2-NH.sub.2-Phenyl 1343 1 CONHMe 2-NH.sub.2-Phenyl 1344 2 CONHMe 2-NH.sub.2-Phenyl 1345 3 CONHMe 2-NH.sub.2-Phenyl 1346 4 CONHMe 2-NH.sub.2-Phenyl 1347 1 SO.sub.2Me 2-NH.sub.2-Phenyl 1348 2 SO.sub.2Me 2-NH.sub.2-Phenyl 1349 3 SO.sub.2Me 2-NH.sub.2-Phenyl 1350 4 SO.sub.2Me 2-NH.sub.2-Phenyl 1351 1 SO.sub.2NH.sub.2 2-NH.sub.2-Phenyl 1352 2 SO.sub.2NH.sub.2 2-NH.sub.2-Phenyl 1353 3 SO.sub.2NH.sub.2 2-NH.sub.2-Phenyl 1354 4 SO.sub.2NH.sub.2 2-NH.sub.2-Phenyl 1355 1 H 2,6-di-Me-Phenyl 1356 2 H 2,6-di-Me-Phenyl 1357 3 H 2,6-di-Me-Phenyl 1358 4 H 2,6-di-Me-Phenyl 1359 1 Me 2,6-di-Me-Phenyl 1360 2 Me 2,6-di-Me-Phenyl 1361 3 Me 2,6-di-Me-Phenyl 1362 4 Me 2,6-di-Me-Phenyl 1363 1 CH.sub.2Ph 2,6-di-Me-Phenyl 1364 2 CH.sub.2Ph 2,6-di-Me-Phenyl 1365 3 CH.sub.2Ph 2,6-di-Me-Phenyl 1366 4 CH.sub.2Ph 2,6-di-Me-Phenyl 1367 1 COMe 2,6-di-Me-Phenyl 1368 2 COMe 2,6-di-Me-Phenyl 1369 3 COMe 2,6-di-Me-Phenyl 1370 4 COMe 2,6-di-Me-Phenyl 1371 1 CO.sub.2Me 2,6-di-Me-Phenyl 1372 2 CO.sub.2Me 2,6-di-Me-Phenyl 1373 3 CO.sub.2Me 2,6-di-Me-Phenyl 1374 4 CO.sub.2Me 2,6-di-Me-Phenyl 1375 1 CO.sub.2tBu 2,6-di-Me-Phenyl 1376 2 CO.sub.2tBu 2,6-di-Me-Phenyl 1377 3 CO.sub.2tBu 2,6-di-Me-Phenyl 1378 4 CO.sub.2tBu 2,6-di-Me-Phenyl 1379 1 CONHMe 2,6-di-Me-Phenyl 1380 2 CONHMe 2,6-di-Me-Phenyl 1381 3 CONHMe 2,6-di-Me-Phenyl 1382 4 CONHMe 2,6-di-Me-Phenyl 1383 1 SO.sub.2Me 2,6-di-Me-Phenyl 1384 2 SO.sub.2Me 2,6-di-Me-Phenyl 1385 3 SO.sub.2Me 2,6-di-Me-Phenyl 1386 4 SO.sub.2Me 2,6-di-Me-Phenyl 1387 1 SO.sub.2NH.sub.2 2,6-di-Me-Phenyl 1388 2 SO.sub.2NH.sub.2 2,6-di-Me-Phenyl 1389 3 SO.sub.2NH.sub.2 2,6-di-Me-Phenyl 1390 4 SO.sub.2NH.sub.2 2,6-di-Me-Phenyl 1391 1 H 2-Ph-Phenyl 1392 2 H 2-Ph-Phenyl 1393 3 H 2-Ph-Phenyl 1394 4 H 2-Ph-Phenyl 1395 1 Me 2-Ph-Phenyl 1396 2 Me 2-Ph-Phenyl 1397 3 Me 2-Ph-Phenyl 1398 4 Me 2-Ph-Phenyl 1399 1 CH.sub.2Ph 2-Ph-Phenyl 1400 2 CH.sub.2Ph 2-Ph-Phenyl 1401 3 CH.sub.2Ph 2-Ph-Phenyl 1402 4 CH.sub.2Ph 2-Ph-Phenyl 1403 1 COMe 2-Ph-Phenyl 1404 2 COMe 2-Ph-Phenyl 1405 3 COMe 2-Ph-Phenyl 1406 4 COMe 2-Ph-Phenyl 1407 1 CO.sub.2Me 2-Ph-Phenyl 1408 2 CO.sub.2Me 2-Ph-Phenyl 1409 3 CO.sub.2Me 2-Ph-Phenyl 1410 4 CO.sub.2Me 2-Ph-Phenyl 1411 1 CO.sub.2tBu 2-Ph-Phenyl 1412 2 CO.sub.2tBu 2-Ph-Phenyl 1413 3 CO.sub.2tBu 2-Ph-Phenyl 1414 4 CO.sub.2tBu 2-Ph-Phenyl 1415 1 CONHMe 2-Ph-Phenyl 1416 2 CONHMe 2-Ph-Phenyl 1417 3 CONHMe 2-Ph-Phenyl 1418 4 CONHMe 2-Ph-Phenyl 1419 1 SO.sub.2Me 2-Ph-Phenyl 1420 2 SO.sub.2Me 2-Ph-Phenyl 1421 3 SO.sub.2Me 2-Ph-Phenyl 1422 4 SO.sub.2Me 2-Ph-Phenyl 1423 1 SO.sub.2NH.sub.2 2-Ph-Phenyl 1424 2 SO.sub.2NH.sub.2 2-Ph-Phenyl 1425 3 SO.sub.2NH.sub.2 2-Ph-Phenyl 1426 4 SO.sub.2NH.sub.2 2-Ph-Phenyl 1427 1 H 4-Ph-Phenyl 1428 2 H 4-Ph-Phenyl 1429 3 H 4-Ph-Phenyl 1430 4 H 4-Ph-Phenyl 1431 1 Me 4-Ph-Phenyl 1432 2 Me 4-Ph-Phenyl 1433 3 Me 4-Ph-Phenyl 1434 4 Me 4-Ph-Phenyl 1435 1 CH.sub.2Ph 4-Ph-Phenyl 1436 2 CH.sub.2Ph 4-Ph-Phenyl 1437 3 CH.sub.2Ph 4-Ph-Phenyl 1438 4 CH.sub.2Ph 4-Ph-Phenyl 1439 1 COMe 4-Ph-Phenyl 1440 2 COMe 4-Ph-Phenyl 1441 3 COMe 4-Ph-Phenyl 1442 4 COMe 4-Ph-Phenyl 1443 1 CO.sub.2Me 4-Ph-Phenyl 1444 2 CO.sub.2Me 4-Ph-Phenyl 1445 3 CO.sub.2Me 4-Ph-Phenyl 1446 4 CO.sub.2Me 4-Ph-Phenyl 1447 1 CO.sub.2tBu 4-Ph-Phenyl 1448 2 CO.sub.2tBu 4-Ph-Phenyl 1449 3 CO.sub.2tBu 4-Ph-Phenyl 1450 4 CO.sub.2tBu 4-Ph-Phenyl 1451 1 CONHMe 4-Ph-Phenyl 1452 2 CONHMe 4-Ph-Phenyl 1453 3 CONHMe 4-Ph-Phenyl 1454 4 CONHMe 4-Ph-Phenyl 1455 1 SO.sub.2Me 4-Ph-Phenyl 1456 2 SO.sub.2Me 4-Ph-Phenyl 1457 3 SO.sub.2Me 4-Ph-Phenyl 1458 4 SO.sub.2Me 4-Ph-Phenyl 1459 1 SO.sub.2NH.sub.2 4-Ph-Phenyl 1460 2 SO.sub.2NH.sub.2 4-Ph-Phenyl 1461 3 SO.sub.2NH.sub.2 4-Ph-Phenyl 1462 4 SO.sub.2NH.sub.2 4-Ph-Phenyl 1463 1 H 3-morpholino-phenyl 1464 2 H 3-morpholino-phenyl 1465 3 H 3-morpholino-phenyl 1466 4 H 3-morpholino-phenyl 1467 1 Me 3-morpholino-phenyl 1468 2 Me 3-morpholino-phenyl 1469 3 Me 3-morpholino-phenyl 1470 4 Me 3-morpholino-phenyl 1471 1 CH.sub.2Ph 3-morpholino-phenyl 1472 2 CH.sub.2Ph 3-morpholino-phenyl 1473 3 CH.sub.2Ph 3-morpholino-phenyl 1474 4 CH.sub.2Ph 3-morpholino-phenyl 1475 1 COMe 3-morpholino-phenyl 1476 2 COMe 3-morpholino-phenyl 1477 3 COMe 3-morpholino-phenyl 1478 4 COMe 3-morpholino-phenyl 1479 1 CO.sub.2Me 3-morpholino-phenyl 1480 2 CO.sub.2Me 3-morpholino-phenyl 1481 3 CO.sub.2Me 3-morpholino-phenyl 1482 4 CO.sub.2Me 3-morpholino-phenyl 1483 1 CO.sub.2tBu 3-morpholino-phenyl 1484 2 CO.sub.2tBu 3-morpholino-phenyl 1485 3 CO.sub.2tBu 3-morpholino-phenyl 1486 4 CO.sub.2tBu 3-morpholino-phenyl 1487 1 CONHMe 3-morpholino-phenyl 1488 2 CONHMe 3-morpholino-phenyl 1489 3 CONHMe 3-morpholino-phenyl 1490 4 CONHMe 3-morpholino-phenyl 1491 1 SO.sub.2Me 3-morpholino-phenyl 1492 2 SO.sub.2Me 3-morpholino-phenyl 1493 3 SO.sub.2Me 3-morpholino-phenyl 1494 4 SO.sub.2Me 3-morpholino-phenyl 1495 1 SO.sub.2NH.sub.2 3-morpholino-phenyl 1496 2 SO.sub.2NH.sub.2 3-morpholino-phenyl 1497 3 SO.sub.2NH.sub.2 3-morpholino-phenyl 1498 4 SO.sub.2NH.sub.2 3-morpholino-phenyl 1499 1 Me 4-morpholino-phenyl 1500 2 Me 4-morpholino-phenyl 1501 3 Me 4-morpholino-phenyl 1502 4 Me 4-morpholino-phenyl 103 1 COMe 4-morpholino-phenyl 1504 2 COMe 4-morpholino-phenyl 1505 3 COMe 4-morpholino-phenyl 1506 4 COMe 4-morpholino-phenyl 1507 1 CO.sub.2tBu 4-morpholino-phenyl 1508 2 CO.sub.2tBu 4-morpholino-phenyl 1509 3 CO.sub.2tBu 4-morpholino-phenyl 1510 4 CO.sub.2tBu 4-morpholino-phenyl 1511 1 SO.sub.2Me 4-morpholino-phenyl 1512 2 SO.sub.2Me 4-morpholino-phenyl 1513 3 SO.sub.2Me 4-morpholino-phenyl 1514 4 SO.sub.2Me 4-morpholino-phenyl 1516 1 H naphthylen-2-yl 1517 2 H naphthylen-2-yl 1518 3 H naphthylen-2-yl 1519 4 H naphthylen-2-yl 1520 1 Me naphthylen-2-yl 1521 2 Me naphthylen-2-yl 1522 3 Me naphthylen-2-yl 1523 4 Me naphthylen-2-yl 1524 1 CH.sub.2Ph naphthylen-2-yl 1525 2 CH.sub.2Ph naphthylen-2-yl 1526 3 CH.sub.2Ph naphthylen-2-yl 1527 4 CH.sub.2Ph naphthylen-2-yl 1528 1 COMe naphthylen-2-yl 1529 2 COMe naphthylen-2-yl 1530 3 COMe naphthylen-2-yl 1531 4 COMe naphthylen-2-yl 1532 1 CO.sub.2Me naphthylen-2-yl 1533 2 CO.sub.2Me naphthylen-2-yl 1534 3 CO.sub.2Me naphthylen-2-yl 1535 4 CO.sub.2Me naphthylen-2-yl 1536 1 CO.sub.2tBu naphthylen-2-yl 1537 2 CO.sub.2tBu naphthylen-2-yl 1538 3 CO.sub.2tBu naphthylen-2-yl 1539 4 CO.sub.2tBu naphthylen-2-yl 1540 1 CONHMe naphthylen-2-yl 1541 2 CONHMe naphthylen-2-yl 1542 3 CONHMe naphthylen-2-yl 1543 4 CONHMe naphthylen-2-yl 1544 1 SO.sub.2Me naphthylen-2-yl 1545 2 SO.sub.2Me naphthylen-2-yl 1546 3 SO.sub.2Me naphthylen-2-yl 1547 4 SO.sub.2Me naphthylen-2-yl 1548 1 SO.sub.2NH.sub.2 naphthylen-2-yl 1549 2 SO.sub.2NH.sub.2 naphthylen-2-yl 1550 3 SO.sub.2NH.sub.2 naphthylen-2-yl 1551 4 SO.sub.2NH.sub.2 naphthylen-2-yl

    [2026] Exemplary embodiments include compounds having the formula (XXIII)

    ##STR00438##

    [2027] or a pharmaceutically acceptable salt form thereof defined herein below in Table 17.

    TABLE-US-00017 TABLE 17 Entry n R.sup.7 R.sup.3 1 1 H Phenyl 2 2 H Phenyl 3 3 H Phenyl 4 4 H Phenyl 5 1 Me Phenyl 6 2 Me Phenyl 7 3 Me Phenyl 8 4 Me Phenyl 9 1 CH.sub.2Ph Phenyl 10 2 CH.sub.2Ph Phenyl 11 3 CH.sub.2Ph Phenyl 12 4 CH.sub.2Ph Phenyl 13 1 COMe Phenyl 14 2 COMe Phenyl 15 3 COMe Phenyl 16 4 COMe Phenyl 17 1 CO.sub.2Me Phenyl 18 2 CO.sub.2Me Phenyl 19 3 CO.sub.2Me Phenyl 20 4 CO.sub.2Me Phenyl 21 1 CO.sub.2tBu Phenyl 22 2 CO.sub.2tBu Phenyl 23 3 CO.sub.2tBu Phenyl 24 4 CO.sub.2tBu Phenyl 25 1 CONHMe Phenyl 26 2 CONHMe Phenyl 27 3 CONHMe Phenyl 28 4 CONHMe Phenyl 29 1 SO.sub.2Me Phenyl 30 2 SO.sub.2Me Phenyl 31 3 SO.sub.2Me Phenyl 32 4 SO.sub.2Me Phenyl 33 1 SO.sub.2NH.sub.2 Phenyl 34 2 SO.sub.2NH.sub.2 Phenyl 35 3 SO.sub.2NH.sub.2 Phenyl 36 4 SO.sub.2NH.sub.2 Phenyl 37 1 H 3-OH-Phenyl 38 2 H 3-OH-Phenyl 39 3 H 3-OH-Phenyl 40 4 H 3-OH-Phenyl 41 1 Me 3-OH-Phenyl 42 2 Me 3-OH-Phenyl 43 3 Me 3-OH-Phenyl 44 4 Me 3-OH-Phenyl 45 1 CH.sub.2Ph 3-OH-Phenyl 46 2 CH.sub.2Ph 3-OH-Phenyl 47 3 CH.sub.2Ph 3-OH-Phenyl 48 4 CH.sub.2Ph 3-OH-Phenyl 49 1 COMe 3-OH-Phenyl 50 2 COMe 3-OH-Phenyl 51 3 COMe 3-OH-Phenyl 52 4 COMe 3-OH-Phenyl 53 1 CO.sub.2Me 3-OH-Phenyl 54 2 CO.sub.2Me 3-OH-Phenyl 55 3 CO.sub.2Me 3-OH-Phenyl 56 4 CO.sub.2Me 3-OH-Phenyl 57 1 CO.sub.2tBu 3-OH-Phenyl 58 2 CO.sub.2tBu 3-OH-Phenyl 59 3 CO.sub.2tBu 3-OH-Phenyl 60 4 CO.sub.2tBu 3-OH-Phenyl 61 1 CONHMe 3-OH-Phenyl 62 2 CONHMe 3-OH-Phenyl 63 3 CONHMe 3-OH-Phenyl 64 4 CONHMe 3-OH-Phenyl 65 1 SO.sub.2Me 3-OH-Phenyl 66 2 SO.sub.2Me 3-OH-Phenyl 67 3 SO.sub.2Me 3-OH-Phenyl 68 4 SO.sub.2Me 3-OH-Phenyl 69 1 SO.sub.2NH.sub.2 3-OH-Phenyl 70 2 SO.sub.2NH.sub.2 3-OH-Phenyl 71 3 SO.sub.2NH.sub.2 3-OH-Phenyl 72 4 SO.sub.2NH.sub.2 3-OH-Phenyl 73 1 H 4-NO.sub.2-Phenyl 74 2 H 4-NO.sub.2-Phenyl 75 3 H 4-NO.sub.2-Phenyl 76 4 H 4-NO.sub.2-Phenyl 77 1 Me 4-NO.sub.2-Phenyl 78 2 Me 4-NO.sub.2-Phenyl 79 3 Me 4-NO.sub.2-Phenyl 80 4 Me 4-NO.sub.2-Phenyl 81 1 CH.sub.2Ph 4-NO.sub.2-Phenyl 82 2 CH.sub.2Ph 4-NO.sub.2-Phenyl 83 3 CH.sub.2Ph 4-NO.sub.2-Phenyl 84 4 CH.sub.2Ph 4-NO.sub.2-Phenyl 85 1 COMe 4-NO.sub.2-Phenyl 86 2 COMe 4-NO.sub.2-Phenyl 87 3 COMe 4-NO.sub.2-Phenyl 88 4 COMe 4-NO.sub.2-Phenyl 89 1 CO.sub.2Me 4-NO.sub.2-Phenyl 90 2 CO.sub.2Me 4-NO.sub.2-Phenyl 91 3 CO.sub.2Me 4-NO.sub.2-Phenyl 92 4 CO.sub.2Me 4-NO.sub.2-Phenyl 93 1 CO.sub.2tBu 4-NO.sub.2-Phenyl 94 2 CO.sub.2tBu 4-NO.sub.2-Phenyl 95 3 CO.sub.2tBu 4-NO.sub.2-Phenyl 96 4 CO.sub.2tBu 4-NO.sub.2-Phenyl 97 1 CONHMe 4-NO.sub.2-Phenyl 98 2 CONHMe 4-NO.sub.2-Phenyl 99 3 CONHMe 4-NO.sub.2-Phenyl 100 4 CONHMe 4-NO.sub.2-Phenyl 101 1 SO.sub.2Me 4-NO.sub.2-Phenyl 102 2 SO.sub.2Me 4-NO.sub.2-Phenyl 103 3 SO.sub.2Me 4-NO.sub.2-Phenyl 104 4 SO.sub.2Me 4-NO.sub.2-Phenyl 105 1 SO.sub.2NH.sub.2 4-NO.sub.2-Phenyl 106 2 SO.sub.2NH.sub.2 4-NO.sub.2-Phenyl 107 3 SO.sub.2NH.sub.2 4-NO.sub.2-Phenyl 108 4 SO.sub.2NH.sub.2 4-NO.sub.2-Phenyl 109 1 H 3-OMe-Phenyl 110 2 H 3-OMe-Phenyl 111 3 H 3-OMe-Phenyl 112 4 H 3-OMe-Phenyl 113 1 Me 3-OMe-Phenyl 114 2 Me 3-OMe-Phenyl 115 3 Me 3-OMe-Phenyl 116 4 Me 3-OMe-Phenyl 117 1 CH.sub.2Ph 3-OMe-Phenyl 118 2 CH.sub.2Ph 3-OMe-Phenyl 119 3 CH.sub.2Ph 3-OMe-Phenyl 120 4 CH.sub.2Ph 3-OMe-Phenyl 121 1 COMe 3-OMe-Phenyl 122 2 COMe 3-OMe-Phenyl 123 3 COMe 3-OMe-Phenyl 124 4 COMe 3-OMe-Phenyl 125 1 CO.sub.2Me 3-OMe-Phenyl 126 2 CO.sub.2Me 3-OMe-Phenyl 127 3 CO.sub.2Me 3-OMe-Phenyl 128 4 CO.sub.2Me 3-OMe-Phenyl 129 1 CO.sub.2tBu 3-OMe-Phenyl 130 2 CO.sub.2tBu 3-OMe-Phenyl 131 3 CO.sub.2tBu 3-OMe-Phenyl 132 4 CO.sub.2tBu 3-OMe-Phenyl 133 1 CONHMe 3-OMe-Phenyl 134 2 CONHMe 3-OMe-Phenyl 135 3 CONHMe 3-OMe-Phenyl 136 4 CONHMe 3-OMe-Phenyl 137 1 SO.sub.2Me 3-OMe-Phenyl 138 2 SO.sub.2Me 3-OMe-Phenyl 139 3 SO.sub.2Me 3-OMe-Phenyl 140 4 SO.sub.2Me 3-OMe-Phenyl 141 1 SO.sub.2NH.sub.2 3-OMe-Phenyl 142 2 SO.sub.2NH.sub.2 3-OMe-Phenyl 143 3 SO.sub.2NH.sub.2 3-OMe-Phenyl 144 4 SO.sub.2NH.sub.2 3-OMe-Phenyl 145 1 H 4-CN-Phenyl 146 2 H 4-CN-Phenyl 147 3 H 4-CN-Phenyl 148 4 H 4-CN-Phenyl 149 1 Me 4-CN-Phenyl 150 2 Me 4-CN-Phenyl 151 3 Me 4-CN-Phenyl 152 4 Me 4-CN-Phenyl 153 1 CH.sub.2Ph 4-CN-Phenyl 154 2 CH.sub.2Ph 4-CN-Phenyl 155 3 CH.sub.2Ph 4-CN-Phenyl 156 4 CH.sub.2Ph 4-CN-Phenyl 157 1 COMe 4-CN-Phenyl 158 2 COMe 4-CN-Phenyl 159 3 COMe 4-CN-Phenyl 160 4 COMe 4-CN-Phenyl 161 1 CO.sub.2Me 4-CN-Phenyl 162 2 CO.sub.2Me 4-CN-Phenyl 163 3 CO.sub.2Me 4-CN-Phenyl 164 4 CO.sub.2Me 4-CN-Phenyl 165 1 CO.sub.2tBu 4-CN-Phenyl 166 2 CO.sub.2tBu 4-CN-Phenyl 167 3 CO.sub.2tBu 4-CN-Phenyl 168 4 CO.sub.2tBu 4-CN-Phenyl 169 1 CONHMe 4-CN-Phenyl 170 2 CONHMe 4-CN-Phenyl 171 3 CONHMe 4-CN-Phenyl 172 4 CONHMe 4-CN-Phenyl 173 1 SO.sub.2Me 4-CN-Phenyl 174 2 SO.sub.2Me 4-CN-Phenyl 175 3 SO.sub.2Me 4-CN-Phenyl 176 4 SO.sub.2Me 4-CN-Phenyl 177 1 SO.sub.2NH.sub.2 4-CN-Phenyl 178 2 SO.sub.2NH.sub.2 4-CN-Phenyl 179 3 SO.sub.2NH.sub.2 4-CN-Phenyl 180 4 SO.sub.2NH.sub.2 4-CN-Phenyl 181 1 H 2-CN-Phenyl 182 2 H 2-CN-Phenyl 183 3 H 2-CN-Phenyl 184 4 H 2-CN-Phenyl 185 1 Me 2-CN-Phenyl 186 2 Me 2-CN-Phenyl 187 3 Me 2-CN-Phenyl 188 4 Me 2-CN-Phenyl 189 1 CH.sub.2Ph 2-CN-Phenyl 190 2 CH.sub.2Ph 2-CN-Phenyl 191 3 CH.sub.2Ph 2-CN-Phenyl 192 4 CH.sub.2Ph 2-CN-Phenyl 193 1 COMe 2-CN-Phenyl 194 2 COMe 2-CN-Phenyl 195 3 COMe 2-CN-Phenyl 196 4 COMe 2-CN-Phenyl 197 1 CO.sub.2Me 2-CN-Phenyl 198 2 CO.sub.2Me 2-CN-Phenyl 199 3 CO.sub.2Me 2-CN-Phenyl 200 4 CO.sub.2Me 2-CN-Phenyl 201 1 CO.sub.2tBu 2-CN-Phenyl 202 2 CO.sub.2tBu 2-CN-Phenyl 203 3 CO.sub.2tBu 2-CN-Phenyl 204 4 CO.sub.2tBu 2-CN-Phenyl 205 1 CONHMe 2-CN-Phenyl 206 2 CONHMe 2-CN-Phenyl 207 3 CONHMe 2-CN-Phenyl 208 4 CONHMe 2-CN-Phenyl 209 1 SO.sub.2Me 2-CN-Phenyl 210 2 SO.sub.2Me 2-CN-Phenyl 211 3 SO.sub.2Me 2-CN-Phenyl 212 4 SO.sub.2Me 2-CN-Phenyl 213 1 SO.sub.2NH.sub.2 2-CN-Phenyl 214 2 SO.sub.2NH.sub.2 2-CN-Phenyl 215 3 SO.sub.2NH.sub.2 2-CN-Phenyl 216 4 SO.sub.2NH.sub.2 2-CN-Phenyl 217 1 H 3-Me-Phenyl 218 2 H 3-Me-Phenyl 219 3 H 3-Me-Phenyl 220 4 H 3-Me-Phenyl 221 1 Me 3-Me-Phenyl 222 2 Me 3-Me-Phenyl 223 3 Me 3-Me-Phenyl 224 4 Me 3-Me-Phenyl 225 1 CH.sub.2Ph 3-Me-Phenyl 226 2 CH.sub.2Ph 3-Me-Phenyl 227 3 CH.sub.2Ph 3-Me-Phenyl 228 4 CH.sub.2Ph 3-Me-Phenyl 229 1 COMe 3-Me-Phenyl 230 2 COMe 3-Me-Phenyl 231 3 COMe 3-Me-Phenyl 232 4 COMe 3-Me-Phenyl 233 1 CO.sub.2Me 3-Me-Phenyl 234 2 CO.sub.2Me 3-Me-Phenyl 235 3 CO.sub.2Me 3-Me-Phenyl 236 4 CO.sub.2Me 3-Me-Phenyl 237 1 CO.sub.2tBu 3-Me-Phenyl 238 2 CO.sub.2tBu 3-Me-Phenyl 239 3 CO.sub.2tBu 3-Me-Phenyl 240 4 CO.sub.2tBu 3-Me-Phenyl 241 1 CONHMe 3-Me-Phenyl 242 2 CONHMe 3-Me-Phenyl 243 3 CONHMe 3-Me-Phenyl 244 4 CONHMe 3-Me-Phenyl 245 1 SO.sub.2Me 3-Me-Phenyl 246 2 SO.sub.2Me 3-Me-Phenyl 247 3 SO.sub.2Me 3-Me-Phenyl 248 4 SO.sub.2Me 3-Me-Phenyl 249 1 SO.sub.2NH.sub.2 3-Me-Phenyl 250 2 SO.sub.2NH.sub.2 3-Me-Phenyl 251 3 SO.sub.2NH.sub.2 3-Me-Phenyl 252 4 SO.sub.2NH.sub.2 3-Me-Phenyl 253 1 H 2-F-Phenyl 254 2 H 2-F-Phenyl 255 3 H 2-F-Phenyl 256 4 H 2-F-Phenyl 257 1 Me 2-F-Phenyl 258 2 Me 2-F-Phenyl 259 3 Me 2-F-Phenyl 260 4 Me 2-F-Phenyl 261 1 CH.sub.2Ph 2-F-Phenyl 262 2 CH.sub.2Ph 2-F-Phenyl 263 3 CH.sub.2Ph 2-F-Phenyl 264 4 CH.sub.2Ph 2-F-Phenyl 265 1 COMe 2-F-Phenyl 266 2 COMe 2-F-Phenyl 267 3 COMe 2-F-Phenyl 268 4 COMe 2-F-Phenyl 269 1 CO.sub.2Me 2-F-Phenyl 270 2 CO.sub.2Me 2-F-Phenyl 271 3 CO.sub.2Me 2-F-Phenyl 272 4 CO.sub.2Me 2-F-Phenyl 273 1 CO.sub.2tBu 2-F-Phenyl 274 2 CO.sub.2tBu 2-F-Phenyl 275 3 CO.sub.2tBu 2-F-Phenyl 276 4 CO.sub.2tBu 2-F-Phenyl 277 1 CONHMe 2-F-Phenyl 278 2 CONHMe 2-F-Phenyl 279 3 CONHMe 2-F-Phenyl 280 4 CONHMe 2-F-Phenyl 281 1 SO.sub.2Me 2-F-Phenyl 282 2 SO.sub.2Me 2-F-Phenyl 283 3 SO.sub.2Me 2-F-Phenyl 284 4 SO.sub.2Me 2-F-Phenyl 285 1 SO.sub.2NH.sub.2 2-F-Phenyl 286 2 SO.sub.2NH.sub.2 2-F-Phenyl 287 3 SO.sub.2NH.sub.2 2-F-Phenyl 288 4 SO.sub.2NH.sub.2 2-F-Phenyl 289 1 H 4-F-Phenyl 290 2 H 4-F-Phenyl 291 3 H 4-F-Phenyl 292 4 H 4-F-Phenyl 293 1 Me 4-F-Phenyl 294 2 Me 4-F-Phenyl 295 3 Me 4-F-Phenyl 296 4 Me 4-F-Phenyl 297 1 CH.sub.2Ph 4-F-Phenyl 298 2 CH.sub.2Ph 4-F-Phenyl 299 3 CH.sub.2Ph 4-F-Phenyl 300 4 CH.sub.2Ph 4-F-Phenyl 301 1 COMe 4-F-Phenyl 302 2 COMe 4-F-Phenyl 303 3 COMe 4-F-Phenyl 304 4 COMe 4-F-Phenyl 305 1 CO.sub.2Me 4-F-Phenyl 306 2 CO.sub.2Me 4-F-Phenyl 307 3 CO.sub.2Me 4-F-Phenyl 308 4 CO.sub.2Me 4-F-Phenyl 309 1 CO.sub.2tBu 4-F-Phenyl 310 2 CO.sub.2tBu 4-F-Phenyl 311 3 CO.sub.2tBu 4-F-Phenyl 312 4 CO.sub.2tBu 4-F-Phenyl 313 1 CONHMe 4-F-Phenyl 314 2 CONHMe 4-F-Phenyl 315 3 CONHMe 4-F-Phenyl 316 4 CONHMe 4-F-Phenyl 317 1 SO.sub.2Me 4-F-Phenyl 318 2 SO.sub.2Me 4-F-Phenyl 319 3 SO.sub.2Me 4-F-Phenyl 320 4 SO.sub.2Me 4-F-Phenyl 321 1 SO.sub.2NH.sub.2 4-F-Phenyl 322 2 SO.sub.2NH.sub.2 4-F-Phenyl 323 3 SO.sub.2NH.sub.2 4-F-Phenyl 324 4 SO.sub.2NH.sub.2 4-F-Phenyl 325 1 H 3-Cl-Phenyl 326 2 H 3-Cl-Phenyl 327 3 H 3-Cl-Phenyl 328 4 H 3-Cl-Phenyl 329 1 Me 3-Cl-Phenyl 330 2 Me 3-Cl-Phenyl 331 3 Me 3-Cl-Phenyl 332 4 Me 3-Cl-Phenyl 333 1 CH.sub.2Ph 3-Cl-Phenyl 334 2 CH.sub.2Ph 3-Cl-Phenyl 335 3 CH.sub.2Ph 3-Cl-Phenyl 336 4 CH.sub.2Ph 3-Cl-Phenyl 337 1 COMe 3-Cl-Phenyl 338 2 COMe 3-Cl-Phenyl 339 3 COMe 3-Cl-Phenyl 340 4 COMe 3-Cl-Phenyl 341 1 CO.sub.2Me 3-Cl-Phenyl 342 2 CO.sub.2Me 3-Cl-Phenyl 343 3 CO.sub.2Me 3-Cl-Phenyl 344 4 CO.sub.2Me 3-Cl-Phenyl 345 1 CO.sub.2tBu 3-Cl-Phenyl 346 2 CO.sub.2tBu 3-Cl-Phenyl 347 3 CO.sub.2tBu 3-Cl-Phenyl 348 4 CO.sub.2tBu 3-Cl-Phenyl 349 1 CONHMe 3-Cl-Phenyl 350 2 CONHMe 3-Cl-Phenyl 351 3 CONHMe 3-Cl-Phenyl 352 4 CONHMe 3-Cl-Phenyl 353 1 SO.sub.2Me 3-Cl-Phenyl 354 2 SO.sub.2Me 3-Cl-Phenyl 355 3 SO.sub.2Me 3-Cl-Phenyl 356 4 SO.sub.2Me 3-Cl-Phenyl 357 1 SO.sub.2NH.sub.2 3-Cl-Phenyl 358 2 SO.sub.2NH.sub.2 3-Cl-Phenyl 359 3 SO.sub.2NH.sub.2 3-Cl-Phenyl 360 4 SO.sub.2NH.sub.2 3-Cl-Phenyl 361 1 H 2-Br-Phenyl 362 2 H 2-Br-Phenyl 363 3 H 2-Br-Phenyl 364 4 H 2-Br-Phenyl 365 1 Me 2-Br-Phenyl 366 2 Me 2-Br-Phenyl 367 3 Me 2-Br-Phenyl 368 4 Me 2-Br-Phenyl 369 1 CH.sub.2Ph 2-Br-Phenyl 370 2 CH.sub.2Ph 2-Br-Phenyl 371 3 CH.sub.2Ph 2-Br-Phenyl 372 4 CH.sub.2Ph 2-Br-Phenyl 373 1 COMe 2-Br-Phenyl 374 2 COMe 2-Br-Phenyl 375 3 COMe 2-Br-Phenyl 376 4 COMe 2-Br-Phenyl 377 1 CO.sub.2Me 2-Br-Phenyl 378 2 CO.sub.2Me 2-Br-Phenyl 379 3 CO.sub.2Me 2-Br-Phenyl 380 4 CO.sub.2Me 2-Br-Phenyl 381 1 CO.sub.2tBu 2-Br-Phenyl 382 2 CO.sub.2tBu 2-Br-Phenyl 383 3 CO.sub.2tBu 2-Br-Phenyl 384 4 CO.sub.2tBu 2-Br-Phenyl 385 1 CONHMe 2-Br-Phenyl 386 2 CONHMe 2-Br-Phenyl 387 3 CONHMe 2-Br-Phenyl 388 4 CONHMe 2-Br-Phenyl 389 1 SO.sub.2Me 2-Br-Phenyl 390 2 SO.sub.2Me 2-Br-Phenyl 391 3 SO.sub.2Me 2-Br-Phenyl 392 4 SO.sub.2Me 2-Br-Phenyl 393 1 SO.sub.2NH.sub.2 2-Br-Phenyl 394 2 SO.sub.2NH.sub.2 2-Br-Phenyl 395 3 SO.sub.2NH.sub.2 2-Br-Phenyl 396 4 SO.sub.2NH.sub.2 2-Br-Phenyl 397 1 H 4-Br-Phenyl 398 2 H 4-Br-Phenyl 399 3 H 4-Br-Phenyl 400 4 H 4-Br-Phenyl 401 1 Me 4-Br-Phenyl 402 2 Me 4-Br-Phenyl 403 3 Me 4-Br-Phenyl 404 4 Me 4-Br-Phenyl 405 1 CH.sub.2Ph 4-Br-Phenyl 406 2 CH.sub.2Ph 4-Br-Phenyl 407 3 CH.sub.2Ph 4-Br-Phenyl 408 4 CH.sub.2Ph 4-Br-Phenyl 409 1 COMe 4-Br-Phenyl 410 2 COMe 4-Br-Phenyl 411 3 COMe 4-Br-Phenyl 412 4 COMe 4-Br-Phenyl 413 1 CO.sub.2Me 4-Br-Phenyl 414 2 CO.sub.2Me 4-Br-Phenyl 415 3 CO.sub.2Me 4-Br-Phenyl 416 4 CO.sub.2Me 4-Br-Phenyl 417 1 CO.sub.2tBu 4-Br-Phenyl 418 2 CO.sub.2tBu 4-Br-Phenyl 419 3 CO.sub.2tBu 4-Br-Phenyl 420 4 CO.sub.2tBu 4-Br-Phenyl 421 1 CONHMe 4-Br-Phenyl 422 2 CONHMe 4-Br-Phenyl 423 3 CONHMe 4-Br-Phenyl 424 4 CONHMe 4-Br-Phenyl 425 1 SO.sub.2Me 4-Br-Phenyl 426 2 SO.sub.2Me 4-Br-Phenyl 427 3 SO.sub.2Me 4-Br-Phenyl 428 4 SO.sub.2Me 4-Br-Phenyl 429 1 SO.sub.2NH.sub.2 4-Br-Phenyl 430 2 SO.sub.2NH.sub.2 4-Br-Phenyl 431 3 SO.sub.2NH.sub.2 4-Br-Phenyl 432 4 SO.sub.2NH.sub.2 4-Br-Phenyl 433 1 H 3-CF.sub.3-Phenyl 434 2 H 3-CF.sub.3-Phenyl 435 3 H 3-CF.sub.3-Phenyl 436 4 H 3-CF.sub.3-Phenyl 437 1 Me 3-CF.sub.3-Phenyl 438 2 Me 3-CF.sub.3-Phenyl 439 3 Me 3-CF.sub.3-Phenyl 440 4 Me 3-CF.sub.3-Phenyl 441 1 CH.sub.2Ph 3-CF.sub.3-Phenyl 442 2 CH.sub.2Ph 3-CF.sub.3-Phenyl 443 3 CH.sub.2Ph 3-CF.sub.3-Phenyl 444 4 CH.sub.2Ph 3-CF.sub.3-Phenyl 445 1 COMe 3-CF.sub.3-Phenyl 446 2 COMe 3-CF.sub.3-Phenyl 447 3 COMe 3-CF.sub.3-Phenyl 448 4 COMe 3-CF.sub.3-Phenyl 449 1 CO.sub.2Me 3-CF.sub.3-Phenyl 450 2 CO.sub.2Me 3-CF.sub.3-Phenyl 451 3 CO.sub.2Me 3-CF.sub.3-Phenyl 452 4 CO.sub.2Me 3-CF.sub.3-Phenyl 453 1 CO.sub.2tBu 3-CF.sub.3-Phenyl 454 2 CO.sub.2tBu 3-CF.sub.3-Phenyl 455 3 CO.sub.2tBu 3-CF.sub.3-Phenyl 456 4 CO.sub.2tBu 3-CF.sub.3-Phenyl 457 1 CONHMe 3-CF.sub.3-Phenyl 458 2 CONHMe 3-CF.sub.3-Phenyl 459 3 CONHMe 3-CF.sub.3-Phenyl 460 4 CONHMe 3-CF.sub.3-Phenyl 461 1 SO.sub.2Me 3-CF.sub.3-Phenyl 462 2 SO.sub.2Me 3-CF.sub.3-Phenyl 463 3 SO.sub.2Me 3-CF.sub.3-Phenyl 464 4 SO.sub.2Me 3-CF.sub.3-Phenyl 465 1 SO.sub.2NH.sub.2 3-CF.sub.3-Phenyl 466 2 SO.sub.2NH.sub.2 3-CF.sub.3-Phenyl 467 3 SO.sub.2NH.sub.2 3-CF.sub.3-Phenyl 468 4 SO.sub.2NH.sub.2 3-CF.sub.3-Phenyl 469 1 H 2-iPr-Phenyl 470 2 H 2-iPr-Phenyl 471 3 H 2-iPr-Phenyl 472 4 H 2-iPr-Phenyl 473 1 Me 2-iPr-Phenyl 474 2 Me 2-iPr-Phenyl 475 3 Me 2-iPr-Phenyl 476 4 Me 2-iPr-Phenyl 477 1 CH.sub.2Ph 2-iPr-Phenyl 478 2 CH.sub.2Ph 2-iPr-Phenyl 479 3 CH.sub.2Ph 2-iPr-Phenyl 480 4 CH.sub.2Ph 2-iPr-Phenyl 481 1 COMe 2-iPr-Phenyl 482 2 COMe 2-iPr-Phenyl 483 3 COMe 2-iPr-Phenyl 484 4 COMe 2-iPr-Phenyl 485 1 CO.sub.2Me 2-iPr-Phenyl 486 2 CO.sub.2Me 2-iPr-Phenyl 487 3 CO.sub.2Me 2-iPr-Phenyl 488 4 CO.sub.2Me 2-iPr-Phenyl 489 1 CO.sub.2tBu 2-iPr-Phenyl 490 2 CO.sub.2tBu 2-iPr-Phenyl 491 3 CO.sub.2tBu 2-iPr-Phenyl 492 4 CO.sub.2tBu 2-iPr-Phenyl 493 1 CONHMe 2-iPr-Phenyl 494 2 CONHMe 2-iPr-Phenyl 495 3 CONHMe 2-iPr-Phenyl 496 4 CONHMe 2-iPr-Phenyl 497 1 SO.sub.2Me 2-iPr-Phenyl 498 2 SO.sub.2Me 2-iPr-Phenyl 499 3 SO.sub.2Me 2-iPr-Phenyl 500 4 SO.sub.2Me 2-iPr-Phenyl 501 1 SO.sub.2NH.sub.2 2-iPr-Phenyl 502 2 SO.sub.2NH.sub.2 2-iPr-Phenyl 503 3 SO.sub.2NH.sub.2 2-iPr-Phenyl 504 4 SO.sub.2NH.sub.2 2-iPr-Phenyl 505 1 H 4-iPr-Phenyl 506 2 H 4-iPr-Phenyl 507 3 H 4-iPr-Phenyl 508 4 H 4-iPr-Phenyl 509 1 Me 4-iPr-Phenyl 510 2 Me 4-iPr-Phenyl 511 3 Me 4-iPr-Phenyl 512 4 Me 4-iPr-Phenyl 513 1 CH.sub.2Ph 4-iPr-Phenyl 514 2 CH.sub.2Ph 4-iPr-Phenyl 515 3 CH.sub.2Ph 4-iPr-Phenyl 516 4 CH.sub.2Ph 4-iPr-Phenyl 517 1 COMe 4-iPr-Phenyl 518 2 COMe 4-iPr-Phenyl 519 3 COMe 4-iPr-Phenyl 520 4 COMe 4-iPr-Phenyl 521 1 CO.sub.2Me 4-iPr-Phenyl 522 2 CO.sub.2Me 4-iPr-Phenyl 523 3 CO.sub.2Me 4-iPr-Phenyl 524 4 CO.sub.2Me 4-iPr-Phenyl 525 1 CO.sub.2tBu 4-iPr-Phenyl 526 2 CO.sub.2tBu 4-iPr-Phenyl 527 3 CO.sub.2tBu 4-iPr-Phenyl 528 4 CO.sub.2tBu 4-iPr-Phenyl 529 1 CONHMe 4-iPr-Phenyl 530 2 CONHMe 4-iPr-Phenyl 531 3 CONHMe 4-iPr-Phenyl 532 4 CONHMe 4-iPr-Phenyl 533 1 SO.sub.2Me 4-iPr-Phenyl 534 2 SO.sub.2Me 4-iPr-Phenyl 535 3 SO.sub.2Me 4-iPr-Phenyl 536 4 SO.sub.2Me 4-iPr-Phenyl 537 1 SO.sub.2NH.sub.2 4-iPr-Phenyl 538 2 SO.sub.2NH.sub.2 4-iPr-Phenyl 539 3 SO.sub.2NH.sub.2 4-iPr-Phenyl 540 4 SO.sub.2NH.sub.2 4-iPr-Phenyl 541 1 H 3-NH.sub.2-Phenyl 542 2 H 3-NH.sub.2-Phenyl 543 3 H 3-NH.sub.2-Phenyl 544 4 H 3-NH.sub.2-Phenyl 545 1 Me 3-NH.sub.2-Phenyl 546 2 Me 3-NH.sub.2-Phenyl 547 3 Me 3-NH.sub.2-Phenyl 548 4 Me 3-NH.sub.2-Phenyl 549 1 CH.sub.2Ph 3-NH.sub.2-Phenyl 550 2 CH.sub.2Ph 3-NH.sub.2-Phenyl 551 3 CH.sub.2Ph 3-NH.sub.2-Phenyl 552 4 CH.sub.2Ph 3-NH.sub.2-Phenyl 553 1 COMe 3-NH.sub.2-Phenyl 554 2 COMe 3-NH.sub.2-Phenyl 555 3 COMe 3-NH.sub.2-Phenyl 556 4 COMe 3-NH.sub.2-Phenyl 557 1 CO.sub.2Me 3-NH.sub.2-Phenyl 558 2 CO.sub.2Me 3-NH.sub.2-Phenyl 559 3 CO.sub.2Me 3-NH.sub.2-Phenyl 560 4 CO.sub.2Me 3-NH.sub.2-Phenyl 561 1 CO.sub.2tBu 3-NH.sub.2-Phenyl 562 2 CO.sub.2tBu 3-NH.sub.2-Phenyl 563 3 CO.sub.2tBu 3-NH.sub.2-Phenyl 564 4 CO.sub.2tBu 3-NH.sub.2-Phenyl 565 1 CONHMe 3-NH.sub.2-Phenyl 566 2 CONHMe 3-NH.sub.2-Phenyl 567 3 CONHMe 3-NH.sub.2-Phenyl 568 4 CONHMe 3-NH.sub.2-Phenyl 569 1 SO.sub.2Me 3-NH.sub.2-Phenyl 570 2 SO.sub.2Me 3-NH.sub.2-Phenyl 571 3 SO.sub.2Me 3-NH.sub.2-Phenyl 572 4 SO.sub.2Me 3-NH.sub.2-Phenyl 573 1 SO.sub.2NH.sub.2 3-NH.sub.2-Phenyl 574 2 SO.sub.2NH.sub.2 3-NH.sub.2-Phenyl 575 3 SO.sub.2NH.sub.2 3-NH.sub.2-Phenyl 576 4 SO.sub.2NH.sub.2 3-NH.sub.2-Phenyl 577 1 H 2,4-di-Me-Phenyl 578 2 H 2,4-di-Me-Phenyl 579 3 H 2,4-di-Me-Phenyl 580 4 H 2,4-di-Me-Phenyl 581 1 Me 2,4-di-Me-Phenyl 582 2 Me 2,4-di-Me-Phenyl 583 3 Me 2,4-di-Me-Phenyl 584 4 Me 2,4-di-Me-Phenyl 585 1 CH.sub.2Ph 2,4-di-Me-Phenyl 586 2 CH.sub.2Ph 2,4-di-Me-Phenyl 587 3 CH.sub.2Ph 2,4-di-Me-Phenyl 588 4 CH.sub.2Ph 2,4-di-Me-Phenyl 589 1 COMe 2,4-di-Me-Phenyl 590 2 COMe 2,4-di-Me-Phenyl 591 3 COMe 2,4-di-Me-Phenyl 592 4 COMe 2,4-di-Me-Phenyl 593 1 CO.sub.2Me 2,4-di-Me-Phenyl 594 2 CO.sub.2Me 2,4-di-Me-Phenyl 595 3 CO.sub.2Me 2,4-di-Me-Phenyl 596 4 CO.sub.2Me 2,4-di-Me-Phenyl 597 1 CO.sub.2tBu 2,4-di-Me-Phenyl 598 2 CO.sub.2tBu 2,4-di-Me-Phenyl 599 3 CO.sub.2tBu 2,4-di-Me-Phenyl 600 4 CO.sub.2tBu 2,4-di-Me-Phenyl 601 1 CONHMe 2,4-di-Me-Phenyl 602 2 CONHMe 2,4-di-Me-Phenyl 603 3 CONHMe 2,4-di-Me-Phenyl 604 4 CONHMe 2,4-di-Me-Phenyl 605 1 SO.sub.2Me 2,4-di-Me-Phenyl 606 2 SO.sub.2Me 2,4-di-Me-Phenyl 607 3 SO.sub.2Me 2,4-di-Me-Phenyl 608 4 SO.sub.2Me 2,4-di-Me-Phenyl 609 1 SO.sub.2NH.sub.2 2,4-di-Me-Phenyl 610 2 SO.sub.2NH.sub.2 2,4-di-Me-Phenyl 611 3 SO.sub.2NH.sub.2 2,4-di-Me-Phenyl 612 4 SO.sub.2NH.sub.2 2,4-di-Me-Phenyl 613 1 H 2,6-di-iPr-Phenyl 614 2 H 2,6-di-iPr-Phenyl 615 3 H 2,6-di-iPr-Phenyl 616 4 H 2,6-di-iPr-Phenyl 617 1 Me 2,6-di-iPr-Phenyl 618 2 Me 2,6-di-iPr-Phenyl 619 3 Me 2,6-di-iPr-Phenyl 620 4 Me 2,6-di-iPr-Phenyl 621 1 CH.sub.2Ph 2,6-di-iPr-Phenyl 622 2 CH.sub.2Ph 2,6-di-iPr-Phenyl 623 3 CH.sub.2Ph 2,6-di-iPr-Phenyl 624 3 CH.sub.2Ph 2,6-di-iPr-Phenyl 625 1 COMe 2,6-di-iPr-Phenyl 626 2 COMe 2,6-di-iPr-Phenyl 627 3 COMe 2,6-di-iPr-Phenyl 628 4 COMe 2,6-di-iPr-Phenyl 629 1 CO.sub.2Me 2,6-di-iPr-Phenyl 630 2 CO.sub.2Me 2,6-di-iPr-Phenyl 631 3 CO.sub.2Me 2,6-di-iPr-Phenyl 632 4 CO.sub.2Me 2,6-di-iPr-Phenyl 633 1 CO.sub.2tBu 2,6-di-iPr-Phenyl 634 2 CO.sub.2tBu 2,6-di-iPr-Phenyl 635 3 CO.sub.2tBu 2,6-di-iPr-Phenyl 636 4 CO.sub.2tBu 2,6-di-iPr-Phenyl 637 1 CONHMe 2,6-di-iPr-Phenyl 638 2 CONHMe 2,6-di-iPr-Phenyl 639 3 CONHMe 2,6-di-iPr-Phenyl 640 4 CONHMe 2,6-di-iPr-Phenyl 641 1 SO.sub.2Me 2,6-di-iPr-Phenyl 642 2 SO.sub.2Me 2,6-di-iPr-Phenyl 643 3 SO.sub.2Me 2,6-di-iPr-Phenyl 644 4 SO.sub.2Me 2,6-di-iPr-Phenyl 645 1 SO.sub.2NH.sub.2 2,6-di-iPr-Phenyl 646 2 SO.sub.2NH.sub.2 2,6-di-iPr-Phenyl 647 3 SO.sub.2NH.sub.2 2,6-di-iPr-Phenyl 648 4 SO.sub.2NH.sub.2 2,6-di-iPr-Phenyl 649 1 H 3-Ph-Phenyl 650 2 H 3-Ph-Phenyl 651 3 H 3-Ph-Phenyl 652 4 H 3-Ph-Phenyl 653 1 Me 3-Ph-Phenyl 654 2 Me 3-Ph-Phenyl 655 3 Me 3-Ph-Phenyl 656 4 Me 3-Ph-Phenyl 657 1 CH.sub.2Ph 3-Ph-Phenyl 658 2 CH.sub.2Ph 3-Ph-Phenyl 659 3 CH.sub.2Ph 3-Ph-Phenyl 660 4 CH.sub.2Ph 3-Ph-Phenyl 661 1 COMe 3-Ph-Phenyl 662 2 COMe 3-Ph-Phenyl 663 3 COMe 3-Ph-Phenyl 664 4 COMe 3-Ph-Phenyl 665 1 CO.sub.2Me 3-Ph-Phenyl 666 2 CO.sub.2Me 3-Ph-Phenyl 667 3 CO.sub.2Me 3-Ph-Phenyl 668 4 CO.sub.2Me 3-Ph-Phenyl 669 1 CO.sub.2tBu 3-Ph-Phenyl 670 2 CO.sub.2tBu 3-Ph-Phenyl 671 3 CO.sub.2tBu 3-Ph-Phenyl 672 4 CO.sub.2tBu 3-Ph-Phenyl 673 1 CONHMe 3-Ph-Phenyl 674 2 CONHMe 3-Ph-Phenyl 675 3 CONHMe 3-Ph-Phenyl 676 4 CONHMe 3-Ph-Phenyl 677 1 SO.sub.2Me 3-Ph-Phenyl 678 2 SO.sub.2Me 3-Ph-Phenyl 679 3 SO.sub.2Me 3-Ph-Phenyl 680 4 SO.sub.2Me 3-Ph-Phenyl 681 1 SO.sub.2NH.sub.2 3-Ph-Phenyl 682 2 SO.sub.2NH.sub.2 3-Ph-Phenyl 683 3 SO.sub.2NH.sub.2 3-Ph-Phenyl 684 4 SO.sub.2NH.sub.2 3-Ph-Phenyl 685 1 H 2-morpholino-phenyl 686 2 H 2-morpholino-phenyl 687 3 H 2-morpholino-phenyl 688 4 H 2-morpholino-phenyl 689 1 Me 2-morpholino-phenyl 690 2 Me 2-morpholino-phenyl 691 3 Me 2-morpholino-phenyl 692 4 Me 2-morpholino-phenyl 693 1 CH.sub.2Ph 2-morpholino-phenyl 694 2 CH.sub.2Ph 2-morpholino-phenyl 695 3 CH.sub.2Ph 2-morpholino-phenyl 696 4 CH.sub.2Ph 2-morpholino-phenyl 697 1 COMe 2-morpholino-phenyl 698 2 COMe 2-morpholino-phenyl 699 3 COMe 2-morpholino-phenyl 700 4 COMe 2-morpholino-phenyl 701 1 CO.sub.2Me 2-morpholino-phenyl 702 2 CO.sub.2Me 2-morpholino-phenyl 703 3 CO.sub.2Me 2-morpholino-phenyl 704 4 CO.sub.2Me 2-morpholino-phenyl 705 1 CO.sub.2tBu 2-morpholino-phenyl 706 2 CO.sub.2tBu 2-morpholino-phenyl 707 3 CO.sub.2tBu 2-morpholino-phenyl 708 4 CO.sub.2tBu 2-morpholino-phenyl 709 1 CONHMe 2-morpholino-phenyl 710 2 CONHMe 2-morpholino-phenyl 711 3 CONHMe 2-morpholino-phenyl 712 4 CONHMe 2-morpholino-phenyl 713 1 SO.sub.2Me 2-morpholino-phenyl 714 2 SO.sub.2Me 2-morpholino-phenyl 715 3 SO.sub.2Me 2-morpholino-phenyl 716 4 SO.sub.2Me 2-morpholino-phenyl 717 1 SO.sub.2NH.sub.2 2-morpholino-phenyl 718 2 SO.sub.2NH.sub.2 2-morpholino-phenyl 719 3 SO.sub.2NH.sub.2 2-morpholino-phenyl 720 4 SO.sub.2NH.sub.2 2-morpholino-phenyl 721 1 H 4-morpholino-phenyl 722 2 H 4-morpholino-phenyl 723 3 H 4-morpholino-phenyl 724 4 H 4-morpholino-phenyl 725 1 CH.sub.2Ph 4-morpholino-phenyl 726 2 CH.sub.2Ph 4-morpholino-phenyl 727 3 CH.sub.2Ph 4-morpholino-phenyl 728 4 CH.sub.2Ph 4-morpholino-phenyl 729 1 CO.sub.2Me 4-morpholino-phenyl 730 2 CO.sub.2Me 4-morpholino-phenyl 731 3 CO.sub.2Me 4-morpholino-phenyl 732 4 CO.sub.2Me 4-morpholino-phenyl 733 1 CONHMe 4-morpholino-phenyl 734 2 CONHMe 4-morpholino-phenyl 735 3 CONHMe 4-morpholino-phenyl 736 4 CONHMe 4-morpholino-phenyl 737 1 SO.sub.2NH.sub.2 4-morpholino-phenyl 738 2 SO.sub.2NH.sub.2 4-morpholino-phenyl 739 3 SO.sub.2NH.sub.2 4-morpholino-phenyl 740 1 H naphthylen-1-yl 741 2 H naphthylen-1-yl 742 3 H naphthylen-1-yl 743 4 H naphthylen-1-yl 744 1 Me naphthylen-1-yl 745 2 Me naphthylen-1-yl 746 3 Me naphthylen-1-yl 747 4 Me naphthylen-1-yl 748 1 CH.sub.2Ph naphthylen-1-yl 749 2 CH.sub.2Ph naphthylen-1-yl 750 3 CH.sub.2Ph naphthylen-1-yl 751 4 CH.sub.2Ph naphthylen-1-yl 752 1 COMe naphthylen-1-yl 753 2 COMe naphthylen-1-yl 754 3 COMe naphthylen-1-yl 755 4 COMe naphthylen-1-yl 756 1 CO.sub.2Me naphthylen-1-yl 757 2 CO.sub.2Me naphthylen-1-yl 758 3 CO.sub.2Me naphthylen-1-yl 759 4 CO.sub.2Me naphthylen-1-yl 760 1 CO.sub.2tBu naphthylen-1-yl 761 2 CO.sub.2tBu naphthylen-1-yl 762 3 CO.sub.2tBu naphthylen-1-yl 763 4 CO.sub.2tBu naphthylen-1-yl 764 1 CONHMe naphthylen-1-yl 765 2 CONHMe naphthylen-1-yl 767 3 CONHMe naphthylen-1-yl 768 4 CONHMe naphthylen-1-yl 769 1 SO.sub.2Me naphthylen-1-yl 770 2 SO.sub.2Me naphthylen-1-yl 771 3 SO.sub.2Me naphthylen-1-yl 772 4 SO.sub.2Me naphthylen-1-yl 773 1 SO.sub.2NH.sub.2 naphthylen-1-yl 774 2 SO.sub.2NH.sub.2 naphthylen-1-yl 775 3 SO.sub.2NH.sub.2 naphthylen-1-yl 778 4 SO.sub.2NH.sub.2 naphthylen-1-yl 779 1 H 4-OH-Phenyl 780 2 H 4-OH-Phenyl 781 3 H 4-OH-Phenyl 782 4 H 4-OH-Phenyl 783 1 Me 4-OH-Phenyl 784 2 Me 4-OH-Phenyl 785 3 Me 4-OH-Phenyl 786 4 Me 4-OH-Phenyl 787 1 CH.sub.2Ph 4-OH-Phenyl 788 2 CH.sub.2Ph 4-OH-Phenyl 789 3 CH.sub.2Ph 4-OH-Phenyl 790 4 CH.sub.2Ph 4-OH-Phenyl 791 1 COMe 4-OH-Phenyl 792 2 COMe 4-OH-Phenyl 793 3 COMe 4-OH-Phenyl 794 4 COMe 4-OH-Phenyl 795 1 CO.sub.2Me 4-OH-Phenyl 796 2 CO.sub.2Me 4-OH-Phenyl 797 3 CO.sub.2Me 4-OH-Phenyl 798 4 CO.sub.2Me 4-OH-Phenyl 799 1 CO.sub.2tBu 4-OH-Phenyl 800 2 CO.sub.2tBu 4-OH-Phenyl 801 3 CO.sub.2tBu 4-OH-Phenyl 802 4 CO.sub.2tBu 4-OH-Phenyl 803 1 CONHMe 4-OH-Phenyl 804 2 CONHMe 4-OH-Phenyl 805 3 CONHMe 4-OH-Phenyl 806 4 CONHMe 4-OH-Phenyl 807 1 SO.sub.2Me 4-OH-Phenyl 808 2 SO.sub.2Me 4-OH-Phenyl 809 3 SO.sub.2Me 4-OH-Phenyl 810 4 SO.sub.2Me 4-OH-Phenyl 811 1 SO.sub.2NH.sub.2 4-OH-Phenyl 812 2 SO.sub.2NH.sub.2 4-OH-Phenyl 813 3 SO.sub.2NH.sub.2 4-OH-Phenyl 814 4 SO.sub.2NH.sub.2 4-OH-Phenyl 815 1 H 2-OH-Phenyl 816 2 H 2-OH-Phenyl 817 3 H 2-OH-Phenyl 818 4 H 2-OH-Phenyl 819 1 Me 2-OH-Phenyl 820 2 Me 2-OH-Phenyl 821 3 Me 2-OH-Phenyl 822 4 Me 2-OH-Phenyl 823 1 CH.sub.2Ph 2-OH-Phenyl 824 2 CH.sub.2Ph 2-OH-Phenyl 825 3 CH.sub.2Ph 2-OH-Phenyl 826 4 CH.sub.2Ph 2-OH-Phenyl 827 1 COMe 2-OH-Phenyl 828 2 COMe 2-OH-Phenyl 829 3 COMe 2-OH-Phenyl 830 4 COMe 2-OH-Phenyl 831 1 CO.sub.2Me 2-OH-Phenyl 832 2 CO.sub.2Me 2-OH-Phenyl 833 3 CO.sub.2Me 2-OH-Phenyl 834 4 CO.sub.2Me 2-OH-Phenyl 835 1 CO.sub.2tBu 2-OH-Phenyl 836 2 CO.sub.2tBu 2-OH-Phenyl 837 3 CO.sub.2tBu 2-OH-Phenyl 838 4 CO.sub.2tBu 2-OH-Phenyl 839 1 CONHMe 2-OH-Phenyl 840 2 CONHMe 2-OH-Phenyl 841 3 CONHMe 2-OH-Phenyl 842 4 CONHMe 2-OH-Phenyl 843 1 SO.sub.2Me 2-OH-Phenyl 844 2 SO.sub.2Me 2-OH-Phenyl 845 3 SO.sub.2Me 2-OH-Phenyl 846 4 SO.sub.2Me 2-OH-Phenyl 847 1 SO.sub.2NH.sub.2 2-OH-Phenyl 848 2 SO.sub.2NH.sub.2 2-OH-Phenyl 849 3 SO.sub.2NH.sub.2 2-OH-Phenyl 850 4 SO.sub.2NH.sub.2 2-OH-Phenyl 851 1 H 4-OMe-Phenyl 852 2 H 4-OMe-Phenyl 853 3 H 4-OMe-Phenyl 854 4 H 4-OMe-Phenyl 855 1 Me 4-OMe-Phenyl 856 2 Me 4-OMe-Phenyl 857 3 Me 4-OMe-Phenyl 858 4 Me 4-OMe-Phenyl 859 1 CH.sub.2Ph 4-OMe-Phenyl 860 2 CH.sub.2Ph 4-OMe-Phenyl 861 3 CH.sub.2Ph 4-OMe-Phenyl 862 4 CH.sub.2Ph 4-OMe-Phenyl 863 1 COMe 4-OMe-Phenyl 864 2 COMe 4-OMe-Phenyl 865 3 COMe 4-OMe-Phenyl 866 4 COMe 4-OMe-Phenyl 867 1 CO.sub.2Me 4-OMe-Phenyl 868 2 CO.sub.2Me 4-OMe-Phenyl 869 3 CO.sub.2Me 4-OMe-Phenyl 870 4 CO.sub.2Me 4-OMe-Phenyl 871 1 CO.sub.2tBu 4-OMe-Phenyl 872 2 CO.sub.2tBu 4-OMe-Phenyl 873 3 CO.sub.2tBu 4-OMe-Phenyl 874 4 CO.sub.2tBu 4-OMe-Phenyl 875 1 CONHMe 4-OMe-Phenyl 876 2 CONHMe 4-OMe-Phenyl 877 3 CONHMe 4-OMe-Phenyl 878 4 CONHMe 4-OMe-Phenyl 879 1 SO.sub.2Me 4-OMe-Phenyl 880 2 SO.sub.2Me 4-OMe-Phenyl 881 3 SO.sub.2Me 4-OMe-Phenyl 882 4 SO.sub.2Me 4-OMe-Phenyl 883 1 SO.sub.2NH.sub.2 4-OMe-Phenyl 884 2 SO.sub.2NH.sub.2 4-OMe-Phenyl 885 3 SO.sub.2NH.sub.2 4-OMe-Phenyl 886 4 SO.sub.2NH.sub.2 4-OMe-Phenyl 887 1 H 2-OMe-Phenyl 888 2 H 2-OMe-Phenyl 889 3 H 2-OMe-Phenyl 890 4 H 2-OMe-Phenyl 891 1 Me 2-OMe-Phenyl 892 2 Me 2-OMe-Phenyl 893 3 Me 2-OMe-Phenyl 894 4 Me 2-OMe-Phenyl 895 1 CH.sub.2Ph 2-OMe-Phenyl 896 2 CH.sub.2Ph 2-OMe-Phenyl 897 3 CH.sub.2Ph 2-OMe-Phenyl 898 4 CH.sub.2Ph 2-OMe-Phenyl 899 1 COMe 2-OMe-Phenyl 900 2 COMe 2-OMe-Phenyl 901 3 COMe 2-OMe-Phenyl 902 4 COMe 2-OMe-Phenyl 903 1 CO.sub.2Me 2-OMe-Phenyl 904 2 CO.sub.2Me 2-OMe-Phenyl 905 3 CO.sub.2Me 2-OMe-Phenyl 906 4 CO.sub.2Me 2-OMe-Phenyl 907 1 CO.sub.2tBu 2-OMe-Phenyl 908 2 CO.sub.2tBu 2-OMe-Phenyl 909 3 CO.sub.2tBu 2-OMe-Phenyl 910 4 CO.sub.2tBu 2-OMe-Phenyl 911 1 CONHMe 2-OMe-Phenyl 912 2 CONHMe 2-OMe-Phenyl 913 3 CONHMe 2-OMe-Phenyl 914 4 CONHMe 2-OMe-Phenyl 915 1 SO.sub.2Me 2-OMe-Phenyl 916 2 SO.sub.2Me 2-OMe-Phenyl 917 3 SO.sub.2Me 2-OMe-Phenyl 918 4 SO.sub.2Me 2-OMe-Phenyl 919 1 SO.sub.2NH.sub.2 2-OMe-Phenyl 920 2 SO.sub.2NH.sub.2 2-OMe-Phenyl 921 3 SO.sub.2NH.sub.2 2-OMe-Phenyl 922 4 SO.sub.2NH.sub.2 2-OMe-Phenyl 923 1 H 3-CN-Phenyl 924 2 H 3-CN-Phenyl 925 3 H 3-CN-Phenyl 926 4 H 3-CN-Phenyl 927 1 Me 3-CN-Phenyl 928 2 Me 3-CN-Phenyl 929 3 Me 3-CN-Phenyl 930 4 Me 3-CN-Phenyl 931 1 CH.sub.2Ph 3-CN-Phenyl 932 2 CH.sub.2Ph 3-CN-Phenyl 933 3 CH.sub.2Ph 3-CN-Phenyl 934 4 CH.sub.2Ph 3-CN-Phenyl 935 1 COMe 3-CN-Phenyl 936 2 COMe 3-CN-Phenyl 937 3 COMe 3-CN-Phenyl 938 4 COMe 3-CN-Phenyl 939 1 CO.sub.2Me 3-CN-Phenyl 940 2 CO.sub.2Me 3-CN-Phenyl 941 3 CO.sub.2Me 3-CN-Phenyl 942 4 CO.sub.2Me 3-CN-Phenyl 943 1 CO.sub.2tBu 3-CN-Phenyl 944 2 CO.sub.2tBu 3-CN-Phenyl 945 3 CO.sub.2tBu 3-CN-Phenyl 946 4 CO.sub.2tBu 3-CN-Phenyl 947 1 CONHMe 3-CN-Phenyl 948 2 CONHMe 3-CN-Phenyl 949 3 CONHMe 3-CN-Phenyl 950 4 CONHMe 3-CN-Phenyl 951 1 SO.sub.2Me 3-CN-Phenyl 952 2 SO.sub.2Me 3-CN-Phenyl 953 3 SO.sub.2Me 3-CN-Phenyl 954 4 SO.sub.2Me 3-CN-Phenyl 955 1 SO.sub.2NH.sub.2 3-CN-Phenyl 956 2 SO.sub.2NH.sub.2 3-CN-Phenyl 957 3 SO.sub.2NH.sub.2 3-CN-Phenyl 958 4 SO.sub.2NH.sub.2 3-CN-Phenyl 959 1 H 2-Me-Phenyl 960 2 H 2-Me-Phenyl 961 3 H 2-Me-Phenyl 962 4 H 2-Me-Phenyl 963 1 Me 2-Me-Phenyl 964 2 Me 2-Me-Phenyl 965 3 Me 2-Me-Phenyl 966 4 Me 2-Me-Phenyl 967 1 CH.sub.2Ph 2-Me-Phenyl 968 2 CH.sub.2Ph 2-Me-Phenyl 969 3 CH.sub.2Ph 2-Me-Phenyl 970 4 CH.sub.2Ph 2-Me-Phenyl 971 1 COMe 2-Me-Phenyl 972 2 COMe 2-Me-Phenyl 973 3 COMe 2-Me-Phenyl 974 4 COMe 2-Me-Phenyl 975 1 CO.sub.2Me 2-Me-Phenyl 976 2 CO.sub.2Me 2-Me-Phenyl 977 3 CO.sub.2Me 2-Me-Phenyl 978 4 CO.sub.2Me 2-CN-Phenyl 979 1 CO.sub.2tBu 2-Me-Phenyl 980 2 CO.sub.2tBu 2-Me-Phenyl 981 3 CO.sub.2tBu 2-Me-Phenyl 982 4 CO.sub.2tBu 2-Me-Phenyl 983 1 CONHMe 2-Me-Phenyl 984 2 CONHMe 2-Me-Phenyl 985 3 CONHMe 2-Me-Phenyl 986 4 CONHMe 2-Me-Phenyl 987 1 SO.sub.2Me 2-Me-Phenyl 988 2 SO.sub.2Me 2-Me-Phenyl 989 3 SO.sub.2Me 2-Me-Phenyl 990 4 SO.sub.2Me 2-Me-Phenyl 991 1 SO.sub.2NH.sub.2 2-Me-Phenyl 992 2 SO.sub.2NH.sub.2 2-Me-Phenyl 993 3 SO.sub.2NH.sub.2 2-Me-Phenyl 994 4 SO.sub.2NH.sub.2 2-Me-Phenyl 995 1 H 4-Me-Phenyl 996 2 H 4-Me-Phenyl 997 3 H 4-Me-Phenyl 998 4 H 4-Me-Phenyl 999 1 Me 4-Me-Phenyl 1000 2 Me 4-Me-Phenyl 1001 3 Me 4-Me-Phenyl 1002 4 Me 4-Me-Phenyl 1003 1 CH.sub.2Ph 4-Me-Phenyl 1004 2 CH.sub.2Ph 4-Me-Phenyl 1005 3 CH.sub.2Ph 4-Me-Phenyl 1006 4 CH.sub.2Ph 4-Me-Phenyl 1007 1 COMe 4-Me-Phenyl 1008 2 COMe 4-Me-Phenyl 1009 3 COMe 4-Me-Phenyl 1010 4 COMe 4-Me-Phenyl 1011 1 CO.sub.2Me 4-Me-Phenyl 1012 2 CO.sub.2Me 4-Me-Phenyl 1013 3 CO.sub.2Me 4-Me-Phenyl 1014 4 CO.sub.2Me 4-Me-Phenyl 1015 1 CO.sub.2tBu 4-Me-Phenyl 1016 2 CO.sub.2tBu 4-Me-Phenyl 1017 3 CO.sub.2tBu 4-Me-Phenyl 1018 4 CO.sub.2tBu 4-Me-Phenyl 1019 1 CONHMe 4-Me-Phenyl 1020 2 CONHMe 4-Me-Phenyl 1021 3 CONHMe 4-Me-Phenyl 1022 4 CONHMe 4-Me-Phenyl 1023 1 SO.sub.2Me 4-Me-Phenyl 1024 2 SO.sub.2Me 4-Me-Phenyl 1025 3 SO.sub.2Me 4-Me-Phenyl 1026 4 SO.sub.2Me 4-Me-Phenyl 1027 1 SO.sub.2NH.sub.2 4-Me-Phenyl 1028 2 SO.sub.2NH.sub.2 4-Me-Phenyl 1029 3 SO.sub.2NH.sub.2 4-Me-Phenyl 1030 4 SO.sub.2NH.sub.2 4-Me-Phenyl 1031 1 H 3-F-Phenyl 1032 2 H 3-F-Phenyl 1033 3 H 3-F-Phenyl 1034 4 H 3-F-Phenyl 1035 1 Me 3-F-Phenyl 1036 2 Me 3-F-Phenyl 1037 3 Me 3-F-Phenyl 1038 4 Me 3-F-Phenyl 1039 1 CH.sub.2Ph 3-F-Phenyl 1040 2 CH.sub.2Ph 3-F-Phenyl 1041 3 CH.sub.2Ph 3-F-Phenyl 1042 4 CH.sub.2Ph 3-F-Phenyl 1043 1 COMe 3-F-Phenyl 1044 2 COMe 3-F-Phenyl 1045 3 COMe 3-F-Phenyl 1046 4 COMe 3-F-Phenyl 1047 1 CO.sub.2Me 3-F-Phenyl 1048 2 CO.sub.2Me 3-F-Phenyl 1049 3 CO.sub.2Me 3-F-Phenyl 1050 4 CO.sub.2Me 3-F-Phenyl 1051 1 CO.sub.2tBu 3-F-Phenyl 1052 2 CO.sub.2tBu 3-F-Phenyl 1053 3 CO.sub.2tBu 3-F-Phenyl 1054 4 CO.sub.2tBu 3-F-Phenyl 1055 1 CONHMe 3-F-Phenyl 1056 2 CONHMe 3-F-Phenyl 1057 3 CONHMe 3-F-Phenyl 1058 4 CONHMe 3-F-Phenyl 1059 1 SO.sub.2Me 3-F-Phenyl 1060 2 SO.sub.2Me 3-F-Phenyl 1061 3 SO.sub.2Me 3-F-Phenyl 1062 4 SO.sub.2Me 3-F-Phenyl 1063 1 SO.sub.2NH.sub.2 3-F-Phenyl 1064 2 SO.sub.2NH.sub.2 3-F-Phenyl 1065 3 SO.sub.2NH.sub.2 3-F-Phenyl 1066 4 SO.sub.2NH.sub.2 3-F-Phenyl 1067 1 H 2-Cl-Phenyl 1068 2 H 2-Cl-Phenyl 1069 3 H 2-Cl-Phenyl 1070 4 H 2-Cl-Phenyl 1071 1 Me 2-Cl-Phenyl 1072 2 Me 2-Cl-Phenyl 1073 3 Me 2-Cl-Phenyl 1074 4 Me 2-Cl-Phenyl 1075 1 CH.sub.2Ph 2-Cl-Phenyl 1076 2 CH.sub.2Ph 2-Cl-Phenyl 1077 3 CH.sub.2Ph 2-Cl-Phenyl 1078 4 CH.sub.2Ph 2-Cl-Phenyl 1079 1 COMe 2-Cl-Phenyl 1080 2 COMe 2-Cl-Phenyl 1081 3 COMe 2-Cl-Phenyl 1082 4 COMe 2-Cl-Phenyl 1083 1 CO.sub.2Me 2-Cl-Phenyl 1084 2 CO.sub.2Me 2-Cl-Phenyl 1085 3 CO.sub.2Me 2-Cl-Phenyl 1086 4 CO.sub.2Me 2-Cl-Phenyl 1087 1 CO.sub.2tBu 2-Cl-Phenyl 1088 2 CO.sub.2tBu 2-Cl-Phenyl 1089 3 CO.sub.2tBu 2-Cl-Phenyl 1090 4 CO.sub.2tBu 2-Cl-Phenyl 1091 1 CONHMe 2-Cl-Phenyl 1092 2 CONHMe 2-Cl-Phenyl 1093 3 CONHMe 2-Cl-Phenyl 1094 4 CONHMe 2-Cl-Phenyl 1095 1 SO.sub.2Me 2-Cl-Phenyl 1096 2 SO.sub.2Me 2-Cl-Phenyl 1097 3 SO.sub.2Me 2-Cl-Phenyl 1098 4 SO.sub.2Me 2-Cl-Phenyl 1099 1 SO.sub.2NH.sub.2 2-Cl-Phenyl 1100 2 SO.sub.2NH.sub.2 2-Cl-Phenyl 1101 3 SO.sub.2NH.sub.2 2-Cl-Phenyl 1102 4 SO.sub.2NH.sub.2 2-Cl-Phenyl 1103 1 H 4-Cl-Phenyl 1104 2 H 4-Cl-Phenyl 1105 3 H 4-Cl-Phenyl 1106 4 H 4-Cl-Phenyl 1107 1 Me 4-Cl-Phenyl 1108 2 Me 4-Cl-Phenyl 1109 3 Me 4-Cl-Phenyl 1110 4 Me 4-Cl-Phenyl 1111 1 CH.sub.2Ph 4-Cl-Phenyl 1112 2 CH.sub.2Ph 4-Cl-Phenyl 1113 3 CH.sub.2Ph 4-Cl-Phenyl 1114 4 CH.sub.2Ph 4-Cl-Phenyl 1115 1 COMe 4-Cl-Phenyl 1116 2 COMe 4-Cl-Phenyl 1117 3 COMe 4-Cl-Phenyl 1118 4 COMe 4-Cl-Phenyl 1119 1 CO.sub.2Me 4-Cl-Phenyl 1120 2 CO.sub.2Me 4-Cl-Phenyl 1121 3 CO.sub.2Me 4-Cl-Phenyl 1122 4 CO.sub.2Me 4-Cl-Phenyl 1123 1 CO.sub.2tBu 4-Cl-Phenyl 1124 2 CO.sub.2tBu 4-Cl-Phenyl 1125 3 CO.sub.2tBu 4-Cl-Phenyl 1126 4 CO.sub.2tBu 4-Cl-Phenyl 1127 1 CONHMe 4-Cl-Phenyl 1128 2 CONHMe 4-Cl-Phenyl 1129 3 CONHMe 4-Cl-Phenyl 1130 4 CONHMe 4-Cl-Phenyl 1131 1 SO.sub.2Me 4-Cl-Phenyl 1132 2 SO.sub.2Me 4-Cl-Phenyl 1133 3 SO.sub.2Me 4-Cl-Phenyl 1134 4 SO.sub.2Me 4-Cl-Phenyl 1135 1 SO.sub.2NH.sub.2 4-Cl-Phenyl 1136 2 SO.sub.2NH.sub.2 4-Cl-Phenyl 1137 3 SO.sub.2NH.sub.2 4-Cl-Phenyl 1138 4 SO.sub.2NH.sub.2 4-Cl-Phenyl 1139 1 H 3-Br-Phenyl 1140 2 H 3-Br-Phenyl 1141 3 H 3-Br-Phenyl 1142 4 H 3-Br-Phenyl 1143 1 Me 3-Br-Phenyl 1144 2 Me 3-Br-Phenyl 1145 3 Me 3-Br-Phenyl 1146 4 Me 3-Br-Phenyl 1147 1 CH.sub.2Ph 3-Br-Phenyl 1148 2 CH.sub.2Ph 3-Br-Phenyl 1149 3 CH.sub.2Ph 3-Br-Phenyl 1150 4 CH.sub.2Ph 3-Br-Phenyl 1151 1 COMe 3-Br-Phenyl 1152 2 COMe 3-Br-Phenyl 1153 3 COMe 3-Br-Phenyl 1154 4 COMe 3-Br-Phenyl 1155 1 CO.sub.2Me 3-Br-Phenyl 1156 2 CO.sub.2Me 3-Br-Phenyl 1157 3 CO.sub.2Me 3-Br-Phenyl 1158 4 CO.sub.2Me 3-Br-Phenyl 1159 1 CO.sub.2tBu 3-Br-Phenyl 1160 2 CO.sub.2tBu 3-Br-Phenyl 1161 3 CO.sub.2tBu 3-Br-Phenyl 1162 4 CO.sub.2tBu 3-Br-Phenyl 1163 1 CONHMe 3-Br-Phenyl 1164 2 CONHMe 3-Br-Phenyl 1165 3 CONHMe 3-Br-Phenyl 1166 4 CONHMe 3-Br-Phenyl 1167 1 SO.sub.2Me 3-Br-Phenyl 1168 2 SO.sub.2Me 3-Br-Phenyl 1169 3 SO.sub.2Me 3-Br-Phenyl 1170 4 SO.sub.2Me 3-Br-Phenyl 1171 1 SO.sub.2NH.sub.2 3-Br-Phenyl 1172 2 SO.sub.2NH.sub.2 3-Br-Phenyl 1173 3 SO.sub.2NH.sub.2 3-Br-Phenyl 1174 4 SO.sub.2NH.sub.2 3-Br-Phenyl 1175 1 H 2-CF.sub.3-Phenyl 1176 2 H 2-CF.sub.3-Phenyl 1177 3 H 2-CF.sub.3-Phenyl 1178 4 H 2-CF.sub.3-Phenyl 1179 1 Me 2-CF.sub.3-Phenyl 1180 2 Me 2-CF.sub.3-Phenyl 1181 3 Me 2-CF.sub.3-Phenyl 1182 4 Me 2-CF.sub.3-Phenyl 1183 1 CH.sub.2Ph 2-CF.sub.3-Phenyl 1184 2 CH.sub.2Ph 2-CF.sub.3-Phenyl 1185 3 CH.sub.2Ph 2-CF.sub.3-Phenyl 1186 4 CH.sub.2Ph 2-CF.sub.3-Phenyl 1187 1 COMe 2-CF.sub.3-Phenyl 1188 2 COMe 2-CF.sub.3-Phenyl 1189 3 COMe 2-CF.sub.3-Phenyl 1190 4 COMe 2-CF.sub.3-Phenyl 1191 1 CO.sub.2Me 2-CF.sub.3-Phenyl 1192 2 CO.sub.2Me 2-CF.sub.3-Phenyl 1193 3 CO.sub.2Me 2-CF.sub.3-Phenyl 1194 4 CO.sub.2Me 2-CF.sub.3-Phenyl 1195 1 CO.sub.2tBu 2-CF.sub.3-Phenyl 1196 2 CO.sub.2tBu 2-CF.sub.3-Phenyl 1197 3 CO.sub.2tBu 2-CF.sub.3-Phenyl 1198 4 CO.sub.2tBu 2-CF.sub.3-Phenyl 1199 1 CONHMe 2-CF.sub.3-Phenyl 1200 2 CONHMe 2-CF.sub.3-Phenyl 1201 3 CONHMe 2-CF.sub.3-Phenyl 1202 4 CONHMe 2-CF.sub.3-Phenyl 1203 1 SO.sub.2Me 2-CF.sub.3-Phenyl 1204 2 SO.sub.2Me 2-CF.sub.3-Phenyl 1205 3 SO.sub.2Me 2-CF.sub.3-Phenyl 1206 4 SO.sub.2Me 2-CF.sub.3-Phenyl 1207 1 SO.sub.2NH.sub.2 2-CF.sub.3-Phenyl 1208 2 SO.sub.2NH.sub.2 2-CF.sub.3-Phenyl 1209 3 SO.sub.2NH.sub.2 2-CF.sub.3-Phenyl 1210 4 SO.sub.2NH.sub.2 2-CF.sub.3-Phenyl 1211 1 H 4-CF.sub.3-Phenyl 1212 2 H 4-CF.sub.3-Phenyl 1213 3 H 4-CF.sub.3-Phenyl 1214 4 H 4-CF.sub.3-Phenyl 1215 1 Me 4-CF.sub.3-Phenyl 1216 2 Me 4-CF.sub.3-Phenyl 1217 3 Me 4-CF.sub.3-Phenyl 1218 4 Me 4-CF.sub.3-Phenyl 1219 1 CH.sub.2Ph 4-CF.sub.3-Phenyl 1220 2 CH.sub.2Ph 4-CF.sub.3-Phenyl 1221 3 CH.sub.2Ph 4-CF.sub.3-Phenyl 1222 4 CH.sub.2Ph 4-CF.sub.3-Phenyl 1223 1 COMe 4-CF.sub.3-Phenyl 1224 2 COMe 4-CF.sub.3-Phenyl 1225 3 COMe 4-CF.sub.3-Phenyl 1226 4 COMe 4-CF.sub.3-Phenyl 1227 1 CO.sub.2Me 4-CF.sub.3-Phenyl 1228 2 CO.sub.2Me 4-CF.sub.3-Phenyl 1229 3 CO.sub.2Me 4-CF.sub.3-Phenyl 1230 4 CO.sub.2Me 4-CF.sub.3-Phenyl 1231 1 CO.sub.2tBu 4-CF.sub.3-Phenyl 1232 2 CO.sub.2tBu 4-CF.sub.3-Phenyl 1233 3 CO.sub.2tBu 4-CF.sub.3-Phenyl 1234 4 CO.sub.2tBu 4-CF.sub.3-Phenyl 1235 1 CONHMe 4-CF.sub.3-Phenyl 1236 2 CONHMe 4-CF.sub.3-Phenyl 1237 3 CONHMe 4-CF.sub.3-Phenyl 1238 4 CONHMe 4-CF.sub.3-Phenyl 1239 1 SO.sub.2Me 4-CF.sub.3-Phenyl 1240 2 SO.sub.2Me 4-CF.sub.3-Phenyl 1241 3 SO.sub.2Me 4-CF.sub.3-Phenyl 1242 4 SO.sub.2Me 4-CF.sub.3-Phenyl 1243 1 SO.sub.2NH.sub.2 4-CF.sub.3-Phenyl 1244 2 SO.sub.2NH.sub.2 4-CF.sub.3-Phenyl 1245 3 SO.sub.2NH.sub.2 4-CF.sub.3-Phenyl 1246 4 SO.sub.2NH.sub.2 4-CF.sub.3-Phenyl 1247 1 H 3-iPr-Phenyl 1248 2 H 3-iPr-Phenyl 1249 3 H 3-iPr-Phenyl 1250 4 H 3-iPr-Phenyl 1251 1 Me 3-iPr-Phenyl 1252 2 Me 3-iPr-Phenyl 1253 3 Me 3-iPr-Phenyl 1254 4 Me 3-iPr-Phenyl 1255 1 CH.sub.2Ph 3-iPr-Phenyl 1256 2 CH.sub.2Ph 3-iPr-Phenyl 1257 3 CH.sub.2Ph 3-iPr-Phenyl 1258 4 CH.sub.2Ph 3-iPr-Phenyl 1259 1 COMe 3-iPr-Phenyl 1260 2 COMe 3-iPr-Phenyl 1261 3 COMe 3-iPr-Phenyl 1262 4 COMe 3-iPr-Phenyl 1263 1 CO.sub.2Me 3-iPr-Phenyl 1264 2 CO.sub.2Me 3-iPr-Phenyl 1265 3 CO.sub.2Me 3-iPr-Phenyl 1266 4 CO.sub.2Me 3-iPr-Phenyl 1267 1 CO.sub.2tBu 3-iPr-Phenyl 1268 2 CO.sub.2tBu 3-iPr-Phenyl 1269 3 CO.sub.2tBu 3-iPr-Phenyl 1270 4 CO.sub.2tBu 3-iPr-Phenyl 1271 1 CONHMe 3-iPr-Phenyl 1272 2 CONHMe 3-iPr-Phenyl 1273 3 CONHMe 3-iPr-Phenyl 1274 4 CONHMe 3-iPr-Phenyl 1275 1 SO.sub.2Me 3-iPr-Phenyl 1276 2 SO.sub.2Me 3-iPr-Phenyl 1277 3 SO.sub.2Me 3-iPr-Phenyl 1278 4 SO.sub.2Me 3-iPr-Phenyl 1279 1 SO.sub.2NH.sub.2 3-iPr-Phenyl 1280 2 SO.sub.2NH.sub.2 3-iPr-Phenyl 1281 3 SO.sub.2NH.sub.2 3-iPr-Phenyl 1282 4 SO.sub.2NH.sub.2 3-iPr-Phenyl 1283 1 H 4-NH.sub.2-Phenyl 1284 2 H 4-NH.sub.2-Phenyl 1285 3 H 4-NH.sub.2-Phenyl 1286 4 H 4-NH.sub.2-Phenyl 1287 1 Me 4-NH.sub.2-Phenyl 1288 2 Me 4-NH.sub.2-Phenyl 1289 3 Me 4-NH.sub.2-Phenyl 1290 4 Me 4-NH.sub.2-Phenyl 1291 1 CH.sub.2Ph 4-NH.sub.2-Phenyl 1292 2 CH.sub.2Ph 4-NH.sub.2-Phenyl 1293 3 CH.sub.2Ph 4-NH.sub.2-Phenyl 1294 4 CH.sub.2Ph 4-NH.sub.2-Phenyl 1295 1 COMe 4-NH.sub.2-Phenyl 1296 2 COMe 4-NH.sub.2-Phenyl 1297 3 COMe 4-NH.sub.2-Phenyl 1298 4 COMe 4-NH.sub.2-Phenyl 1299 1 CO.sub.2Me 4-NH.sub.2-Phenyl 1300 2 CO.sub.2Me 4-NH.sub.2-Phenyl 1301 3 CO.sub.2Me 4-NH.sub.2-Phenyl 1302 4 CO.sub.2Me 4-NH.sub.2-Phenyl 1303 1 CO.sub.2tBu 4-NH.sub.2-Phenyl 1304 2 CO.sub.2tBu 4-NH.sub.2-Phenyl 1305 3 CO.sub.2tBu 4-NH.sub.2-Phenyl 1306 4 CO.sub.2tBu 4-NH.sub.2-Phenyl 1307 1 CONHMe 4-NH.sub.2-Phenyl 1308 2 CONHMe 4-NH.sub.2-Phenyl 1309 3 CONHMe 4-NH.sub.2-Phenyl 1310 4 CONHMe 4-NH.sub.2-Phenyl 1311 1 SO.sub.2Me 4-NH.sub.2-Phenyl 1312 2 SO.sub.2Me 4-NH.sub.2-Phenyl 1313 3 SO.sub.2Me 4-NH.sub.2-Phenyl 1314 4 SO.sub.2Me 4-NH.sub.2-Phenyl 1315 1 SO.sub.2NH.sub.2 4-NH.sub.2-Phenyl 1316 2 SO.sub.2NH.sub.2 4-NH.sub.2-Phenyl 1317 3 SO.sub.2NH.sub.2 4-NH.sub.2-Phenyl 1318 4 SO.sub.2NH.sub.2 4-NH.sub.2-Phenyl 1319 1 H 2-NH.sub.2-Phenyl 1320 2 H 2-NH.sub.2-Phenyl 1321 3 H 2-NH.sub.2-Phenyl 1322 4 H 2-NH.sub.2-Phenyl 1323 1 Me 2-NH.sub.2-Phenyl 1324 2 Me 2-NH.sub.2-Phenyl 1325 3 Me 2-NH.sub.2-Phenyl 1326 4 Me 2-NH.sub.2-Phenyl 1327 1 CH.sub.2Ph 2-NH.sub.2-Phenyl 1328 2 CH.sub.2Ph 2-NH.sub.2-Phenyl 1329 3 CH.sub.2Ph 2-NH.sub.2-Phenyl 1330 4 CH.sub.2Ph 2-NH.sub.2-Phenyl 1331 1 COMe 2-NH.sub.2-Phenyl 1332 2 COMe 2-NH.sub.2-Phenyl 1333 3 COMe 2-NH.sub.2-Phenyl 1334 4 COMe 2-NH.sub.2-Phenyl 1335 1 CO.sub.2Me 2-NH.sub.2-Phenyl 1336 2 CO.sub.2Me 2-NH.sub.2-Phenyl 1337 3 CO.sub.2Me 2-NH.sub.2-Phenyl 1338 4 CO.sub.2Me 2-NH.sub.2-Phenyl 1339 1 CO.sub.2tBu 2-NH.sub.2-Phenyl 1340 2 CO.sub.2tBu 2-NH.sub.2-Phenyl 1341 3 CO.sub.2tBu 2-NH.sub.2-Phenyl 1342 4 CO.sub.2tBu 2-NH.sub.2-Phenyl 1343 1 CONHMe 2-NH.sub.2-Phenyl 1344 2 CONHMe 2-NH.sub.2-Phenyl 1345 3 CONHMe 2-NH.sub.2-Phenyl 1346 4 CONHMe 2-NH.sub.2-Phenyl 1347 1 SO.sub.2Me 2-NH.sub.2-Phenyl 1348 2 SO.sub.2Me 2-NH.sub.2-Phenyl 1349 3 SO.sub.2Me 2-NH.sub.2-Phenyl 1350 4 SO.sub.2Me 2-NH.sub.2-Phenyl 1351 1 SO.sub.2NH.sub.2 2-NH.sub.2-Phenyl 1352 2 SO.sub.2NH.sub.2 2-NH.sub.2-Phenyl 1353 3 SO.sub.2NH.sub.2 2-NH.sub.2-Phenyl 1354 4 SO.sub.2NH.sub.2 2-NH.sub.2-Phenyl 1355 1 H 2,6-di-Me-Phenyl 1356 2 H 2,6-di-Me-Phenyl 1357 3 H 2,6-di-Me-Phenyl 1358 4 H 2,6-di-Me-Phenyl 1359 1 Me 2,6-di-Me-Phenyl 1360 2 Me 2,6-di-Me-Phenyl 1361 3 Me 2,6-di-Me-Phenyl 1362 4 Me 2,6-di-Me-Phenyl 1363 1 CH.sub.2Ph 2,6-di-Me-Phenyl 1364 2 CH.sub.2Ph 2,6-di-Me-Phenyl 1365 3 CH.sub.2Ph 2,6-di-Me-Phenyl 1366 4 CH.sub.2Ph 2,6-di-Me-Phenyl 1367 1 COMe 2,6-di-Me-Phenyl 1368 2 COMe 2,6-di-Me-Phenyl 1369 3 COMe 2,6-di-Me-Phenyl 1370 4 COMe 2,6-di-Me-Phenyl 1371 1 CO.sub.2Me 2,6-di-Me-Phenyl 1372 2 CO.sub.2Me 2,6-di-Me-Phenyl 1373 3 CO.sub.2Me 2,6-di-Me-Phenyl 1374 4 CO.sub.2Me 2,6-di-Me-Phenyl 1375 1 CO.sub.2tBu 2,6-di-Me-Phenyl 1376 2 CO.sub.2tBu 2,6-di-Me-Phenyl 1377 3 CO.sub.2tBu 2,6-di-Me-Phenyl 1378 4 CO.sub.2tBu 2,6-di-Me-Phenyl 1379 1 CONHMe 2,6-di-Me-Phenyl 1380 2 CONHMe 2,6-di-Me-Phenyl 1381 3 CONHMe 2,6-di-Me-Phenyl 1382 4 CONHMe 2,6-di-Me-Phenyl 1383 1 SO.sub.2Me 2,6-di-Me-Phenyl 1384 2 SO.sub.2Me 2,6-di-Me-Phenyl 1385 3 SO.sub.2Me 2,6-di-Me-Phenyl 1386 4 SO.sub.2Me 2,6-di-Me-Phenyl 1387 1 SO.sub.2NH.sub.2 2,6-di-Me-Phenyl 1388 2 SO.sub.2NH.sub.2 2,6-di-Me-Phenyl 1389 3 SO.sub.2NH.sub.2 2,6-di-Me-Phenyl 1390 4 SO.sub.2NH.sub.2 2,6-di-Me-Phenyl 1391 1 H 2-Ph-Phenyl 1392 2 H 2-Ph-Phenyl 1393 3 H 2-Ph-Phenyl 1394 4 H 2-Ph-Phenyl 1395 1 Me 2-Ph-Phenyl 1396 2 Me 2-Ph-Phenyl 1397 3 Me 2-Ph-Phenyl 1398 4 Me 2-Ph-Phenyl 1399 1 CH.sub.2Ph 2-Ph-Phenyl 1400 2 CH.sub.2Ph 2-Ph-Phenyl 1401 3 CH.sub.2Ph 2-Ph-Phenyl 1402 4 CH.sub.2Ph 2-Ph-Phenyl 1403 1 COMe 2-Ph-Phenyl 1404 2 COMe 2-Ph-Phenyl 1405 3 COMe 2-Ph-Phenyl 1406 4 COMe 2-Ph-Phenyl 1407 1 CO.sub.2Me 2-Ph-Phenyl 1408 2 CO.sub.2Me 2-Ph-Phenyl 1409 3 CO.sub.2Me 2-Ph-Phenyl 1410 4 CO.sub.2Me 2-Ph-Phenyl 1411 1 CO.sub.2tBu 2-Ph-Phenyl 1412 2 CO.sub.2tBu 2-Ph-Phenyl 1413 3 CO.sub.2tBu 2-Ph-Phenyl 1414 4 CO.sub.2tBu 2-Ph-Phenyl 1415 1 CONHMe 2-Ph-Phenyl 1416 2 CONHMe 2-Ph-Phenyl 1417 3 CONHMe 2-Ph-Phenyl 1418 4 CONHMe 2-Ph-Phenyl 1419 1 SO.sub.2Me 2-Ph-Phenyl 1420 2 SO.sub.2Me 2-Ph-Phenyl 1421 3 SO.sub.2Me 2-Ph-Phenyl 1422 4 SO.sub.2Me 2-Ph-Phenyl 1423 1 SO.sub.2NH.sub.2 2-Ph-Phenyl 1424 2 SO.sub.2NH.sub.2 2-Ph-Phenyl 1425 3 SO.sub.2NH.sub.2 2-Ph-Phenyl 1426 4 SO.sub.2NH.sub.2 2-Ph-Phenyl 1427 1 H 4-Ph-Phenyl 1428 2 H 4-Ph-Phenyl 1429 3 H 4-Ph-Phenyl 1430 4 H 4-Ph-Phenyl 1431 1 Me 4-Ph-Phenyl 1432 2 Me 4-Ph-Phenyl 1433 3 Me 4-Ph-Phenyl 1434 4 Me 4-Ph-Phenyl 1435 1 CH.sub.2Ph 4-Ph-Phenyl 1436 2 CH.sub.2Ph 4-Ph-Phenyl 1437 3 CH.sub.2Ph 4-Ph-Phenyl 1438 4 CH.sub.2Ph 4-Ph-Phenyl 1439 1 COMe 4-Ph-Phenyl 1440 2 COMe 4-Ph-Phenyl 1441 3 COMe 4-Ph-Phenyl 1442 4 COMe 4-Ph-Phenyl 1443 1 CO.sub.2Me 4-Ph-Phenyl 1444 2 CO.sub.2Me 4-Ph-Phenyl 1445 3 CO.sub.2Me 4-Ph-Phenyl 1446 4 CO.sub.2Me 4-Ph-Phenyl 1447 1 CO.sub.2tBu 4-Ph-Phenyl 1448 2 CO.sub.2tBu 4-Ph-Phenyl 1449 3 CO.sub.2tBu 4-Ph-Phenyl 1450 4 CO.sub.2tBu 4-Ph-Phenyl 1451 1 CONHMe 4-Ph-Phenyl 1452 2 CONHMe 4-Ph-Phenyl 1453 3 CONHMe 4-Ph-Phenyl 1454 4 CONHMe 4-Ph-Phenyl 1455 1 SO.sub.2Me 4-Ph-Phenyl 1456 2 SO.sub.2Me 4-Ph-Phenyl 1457 3 SO.sub.2Me 4-Ph-Phenyl 1458 4 SO.sub.2Me 4-Ph-Phenyl 1459 1 SO.sub.2NH.sub.2 4-Ph-Phenyl 1460 2 SO.sub.2NH.sub.2 4-Ph-Phenyl 1461 3 SO.sub.2NH.sub.2 4-Ph-Phenyl 1462 4 SO.sub.2NH.sub.2 4-Ph-Phenyl 1463 1 H 3-morpholino-phenyl 1464 2 H 3-morpholino-phenyl 1465 3 H 3-morpholino-phenyl 1466 4 H 3-morpholino-phenyl 1467 1 Me 3-morpholino-phenyl 1468 2 Me 3-morpholino-phenyl 1469 3 Me 3-morpholino-phenyl 1470 4 Me 3-morpholino-phenyl 1471 1 CH.sub.2Ph 3-morpholino-phenyl 1472 2 CH.sub.2Ph 3-morpholino-phenyl 1473 3 CH.sub.2Ph 3-morpholino-phenyl 1474 4 CH.sub.2Ph 3-morpholino-phenyl 1475 1 COMe 3-morpholino-phenyl 1476 2 COMe 3-morpholino-phenyl 1477 3 COMe 3-morpholino-phenyl 1478 4 COMe 3-morpholino-phenyl 1479 1 CO.sub.2Me 3-morpholino-phenyl 1480 2 CO.sub.2Me 3-morpholino-phenyl 1481 3 CO.sub.2Me 3-morpholino-phenyl 1482 4 CO.sub.2Me 3-morpholino-phenyl 1483 1 CO.sub.2tBu 3-morpholino-phenyl 1484 2 CO.sub.2tBu 3-morpholino-phenyl 1485 3 CO.sub.2tBu 3-morpholino-phenyl 1486 4 CO.sub.2tBu 3-morpholino-phenyl 1487 1 CONHMe 3-morpholino-phenyl 1488 2 CONHMe 3-morpholino-phenyl 1489 3 CONHMe 3-morpholino-phenyl 1490 4 CONHMe 3-morpholino-phenyl 1491 1 SO.sub.2Me 3-morpholino-phenyl 1492 2 SO.sub.2Me 3-morpholino-phenyl 1493 3 SO.sub.2Me 3-morpholino-phenyl 1494 4 SO.sub.2Me 3-morpholino-phenyl 1495 1 SO.sub.2NH.sub.2 3-morpholino-phenyl 1496 2 SO.sub.2NH.sub.2 3-morpholino-phenyl 1497 3 SO.sub.2NH.sub.2 3-morpholino-phenyl 1498 4 SO.sub.2NH.sub.2 3-morpholino-phenyl 1499 1 Me 4-morpholino-phenyl 1500 2 Me 4-morpholino-phenyl 1501 3 Me 4-morpholino-phenyl 1502 4 Me 4-morpholino-phenyl 103 1 COMe 4-morpholino-phenyl 1504 2 COMe 4-morpholino-phenyl 1505 3 COMe 4-morpholino-phenyl 1506 4 COMe 4-morpholino-phenyl 1507 1 CO.sub.2tBu 4-morpholino-phenyl 1508 2 CO.sub.2tBu 4-morpholino-phenyl 1509 3 CO.sub.2tBu 4-morpholino-phenyl 1510 4 CO.sub.2tBu 4-morpholino-phenyl 1511 1 SO.sub.2Me 4-morpholino-phenyl 1512 2 SO.sub.2Me 4-morpholino-phenyl 1513 3 SO.sub.2Me 4-morpholino-phenyl 1514 4 SO.sub.2Me 4-morpholino-phenyl 1516 1 H naphthylen-2-yl 1517 2 H naphthylen-2-yl 1518 3 H naphthylen-2-yl 1519 4 H naphthylen-2-yl 1520 1 Me naphthylen-2-yl 1521 2 Me naphthylen-2-yl 1522 3 Me naphthylen-2-yl 1523 4 Me naphthylen-2-yl 1524 1 CH.sub.2Ph naphthylen-2-yl 1525 2 CH.sub.2Ph naphthylen-2-yl 1526 3 CH.sub.2Ph naphthylen-2-yl 1527 4 CH.sub.2Ph naphthylen-2-yl 1528 1 COMe naphthylen-2-yl 1529 2 COMe naphthylen-2-yl 1530 3 COMe naphthylen-2-yl 1531 4 COMe naphthylen-2-yl 1532 1 CO.sub.2Me naphthylen-2-yl 1533 2 CO.sub.2Me naphthylen-2-yl 1534 3 CO.sub.2Me naphthylen-2-yl 1535 4 CO.sub.2Me naphthylen-2-yl 1536 1 CO.sub.2tBu naphthylen-2-yl 1537 2 CO.sub.2tBu naphthylen-2-yl 1538 3 CO.sub.2tBu naphthylen-2-yl 1539 4 CO.sub.2tBu naphthylen-2-yl 1540 1 CONHMe naphthylen-2-yl 1541 2 CONHMe naphthylen-2-yl 1542 3 CONHMe naphthylen-2-yl 1543 4 CONHMe naphthylen-2-yl 1544 1 SO.sub.2Me naphthylen-2-yl 1545 2 SO.sub.2Me naphthylen-2-yl 1546 3 SO.sub.2Me naphthylen-2-yl 1547 4 SO.sub.2Me naphthylen-2-yl 1548 1 SO.sub.2NH.sub.2 naphthylen-2-yl 1549 2 SO.sub.2NH.sub.2 naphthylen-2-yl 1550 3 SO.sub.2NH.sub.2 naphthylen-2-yl 1551 4 SO.sub.2NH.sub.2 naphthylen-2-yl

    [2028] Exemplary embodiments include compounds having the formula (XXIV)

    ##STR00439##

    [2029] or a pharmaceutically acceptable salt form thereof defined herein below in Table 18.

    TABLE-US-00018 TABLE 18 Entry n R.sup.7 R.sup.3 1 1 H Phenyl 2 2 H Phenyl 3 3 H Phenyl 4 4 H Phenyl 5 1 Me Phenyl 6 2 Me Phenyl 7 3 Me Phenyl 8 4 Me Phenyl 9 1 CH.sub.2Ph Phenyl 10 2 CH.sub.2Ph Phenyl 11 3 CH.sub.2Ph Phenyl 12 4 CH.sub.2Ph Phenyl 13 1 COMe Phenyl 14 2 COMe Phenyl 15 3 COMe Phenyl 16 4 COMe Phenyl 17 1 CO.sub.2Me Phenyl 18 2 CO.sub.2Me Phenyl 19 3 CO.sub.2Me Phenyl 20 4 CO.sub.2Me Phenyl 21 1 CO.sub.2tBu Phenyl 22 2 CO.sub.2tBu Phenyl 23 3 CO.sub.2tBu Phenyl 24 4 CO.sub.2tBu Phenyl 25 1 CONHMe Phenyl 26 2 CONHMe Phenyl 27 3 CONHMe Phenyl 28 4 CONHMe Phenyl 29 1 SO.sub.2Me Phenyl 30 2 SO.sub.2Me Phenyl 31 3 SO.sub.2Me Phenyl 32 4 SO.sub.2Me Phenyl 33 1 SO.sub.2NH.sub.2 Phenyl 34 2 SO.sub.2NH.sub.2 Phenyl 35 3 SO.sub.2NH.sub.2 Phenyl 36 4 SO.sub.2NH.sub.2 Phenyl 37 1 H 3-OH-Phenyl 38 2 H 3-OH-Phenyl 39 3 H 3-OH-Phenyl 40 4 H 3-OH-Phenyl 41 1 Me 3-OH-Phenyl 42 2 Me 3-OH-Phenyl 43 3 Me 3-OH-Phenyl 44 4 Me 3-OH-Phenyl 45 1 CH.sub.2Ph 3-OH-Phenyl 46 2 CH.sub.2Ph 3-OH-Phenyl 47 3 CH.sub.2Ph 3-OH-Phenyl 48 4 CH.sub.2Ph 3-OH-Phenyl 49 1 COMe 3-OH-Phenyl 50 2 COMe 3-OH-Phenyl 51 3 COMe 3-OH-Phenyl 52 4 COMe 3-OH-Phenyl 53 1 CO.sub.2Me 3-OH-Phenyl 54 2 CO.sub.2Me 3-OH-Phenyl 55 3 CO.sub.2Me 3-OH-Phenyl 56 4 CO.sub.2Me 3-OH-Phenyl 57 1 CO.sub.2tBu 3-OH-Phenyl 58 2 CO.sub.2tBu 3-OH-Phenyl 59 3 CO.sub.2tBu 3-OH-Phenyl 60 4 CO.sub.2tBu 3-OH-Phenyl 61 1 CONHMe 3-OH-Phenyl 62 2 CONHMe 3-OH-Phenyl 63 3 CONHMe 3-OH-Phenyl 64 4 CONHMe 3-OH-Phenyl 65 1 SO.sub.2Me 3-OH-Phenyl 66 2 SO.sub.2Me 3-OH-Phenyl 67 3 SO.sub.2Me 3-OH-Phenyl 68 4 SO.sub.2Me 3-OH-Phenyl 69 1 SO.sub.2NH.sub.2 3-OH-Phenyl 70 2 SO.sub.2NH.sub.2 3-OH-Phenyl 71 3 SO.sub.2NH.sub.2 3-OH-Phenyl 72 4 SO.sub.2NH.sub.2 3-OH-Phenyl 73 1 H 4-NO.sub.2-Phenyl 74 2 H 4-NO.sub.2-Phenyl 75 3 H 4-NO.sub.2-Phenyl 76 4 H 4-NO.sub.2-Phenyl 77 1 Me 4-NO.sub.2-Phenyl 78 2 Me 4-NO.sub.2-Phenyl 79 3 Me 4-NO.sub.2-Phenyl 80 4 Me 4-NO.sub.2-Phenyl 81 1 CH.sub.2Ph 4-NO.sub.2-Phenyl 82 2 CH.sub.2Ph 4-NO.sub.2-Phenyl 83 3 CH.sub.2Ph 4-NO.sub.2-Phenyl 84 4 CH.sub.2Ph 4-NO.sub.2-Phenyl 85 1 COMe 4-NO.sub.2-Phenyl 86 2 COMe 4-NO.sub.2-Phenyl 87 3 COMe 4-NO.sub.2-Phenyl 88 4 COMe 4-NO.sub.2-Phenyl 89 1 CO.sub.2Me 4-NO.sub.2-Phenyl 90 2 CO.sub.2Me 4-NO.sub.2-Phenyl 91 3 CO.sub.2Me 4-NO.sub.2-Phenyl 92 4 CO.sub.2Me 4-NO.sub.2-Phenyl 93 1 CO.sub.2tBu 4-NO.sub.2-Phenyl 94 2 CO.sub.2tBu 4-NO.sub.2-Phenyl 95 3 CO.sub.2tBu 4-NO.sub.2-Phenyl 96 4 CO.sub.2tBu 4-NO.sub.2-Phenyl 97 1 CONHMe 4-NO.sub.2-Phenyl 98 2 CONHMe 4-NO.sub.2-Phenyl 99 3 CONHMe 4-NO.sub.2-Phenyl 100 4 CONHMe 4-NO.sub.2-Phenyl 101 1 SO.sub.2Me 4-NO.sub.2-Phenyl 102 2 SO.sub.2Me 4-NO.sub.2-Phenyl 103 3 SO.sub.2Me 4-NO.sub.2-Phenyl 104 4 SO.sub.2Me 4-NO.sub.2-Phenyl 105 1 SO.sub.2NH.sub.2 4-NO.sub.2-Phenyl 106 2 SO.sub.2NH.sub.2 4-NO.sub.2-Phenyl 107 3 SO.sub.2NH.sub.2 4-NO.sub.2-Phenyl 108 4 SO.sub.2NH.sub.2 4-NO.sub.2-Phenyl 109 1 H 3-OMe-Phenyl 110 2 H 3-OMe-Phenyl 111 3 H 3-OMe-Phenyl 112 4 H 3-OMe-Phenyl 113 1 Me 3-OMe-Phenyl 114 2 Me 3-OMe-Phenyl 115 3 Me 3-OMe-Phenyl 116 4 Me 3-OMe-Phenyl 117 1 CH.sub.2Ph 3-OMe-Phenyl 118 2 CH.sub.2Ph 3-OMe-Phenyl 119 3 CH.sub.2Ph 3-OMe-Phenyl 120 4 CH.sub.2Ph 3-OMe-Phenyl 121 1 COMe 3-OMe-Phenyl 122 2 COMe 3-OMe-Phenyl 123 3 COMe 3-OMe-Phenyl 124 4 COMe 3-OMe-Phenyl 125 1 CO.sub.2Me 3-OMe-Phenyl 126 2 CO.sub.2Me 3-OMe-Phenyl 127 3 CO.sub.2Me 3-OMe-Phenyl 128 4 CO.sub.2Me 3-OMe-Phenyl 129 1 CO.sub.2tBu 3-OMe-Phenyl 130 2 CO.sub.2tBu 3-OMe-Phenyl 131 3 CO.sub.2tBu 3-OMe-Phenyl 132 4 CO.sub.2tBu 3-OMe-Phenyl 133 1 CONHMe 3-OMe-Phenyl 134 2 CONHMe 3-OMe-Phenyl 135 3 CONHMe 3-OMe-Phenyl 136 4 CONHMe 3-OMe-Phenyl 137 1 SO.sub.2Me 3-OMe-Phenyl 138 2 SO.sub.2Me 3-OMe-Phenyl 139 3 SO.sub.2Me 3-OMe-Phenyl 140 4 SO.sub.2Me 3-OMe-Phenyl 141 1 SO.sub.2NH.sub.2 3-OMe-Phenyl 142 2 SO.sub.2NH.sub.2 3-OMe-Phenyl 143 3 SO.sub.2NH.sub.2 3-OMe-Phenyl 144 4 SO.sub.2NH.sub.2 3-OMe-Phenyl 145 1 H 4-CN-Phenyl 146 2 H 4-CN-Phenyl 147 3 H 4-CN-Phenyl 148 4 H 4-CN-Phenyl 149 1 Me 4-CN-Phenyl 150 2 Me 4-CN-Phenyl 151 3 Me 4-CN-Phenyl 152 4 Me 4-CN-Phenyl 153 1 CH.sub.2Ph 4-CN-Phenyl 154 2 CH.sub.2Ph 4-CN-Phenyl 155 3 CH.sub.2Ph 4-CN-Phenyl 156 4 CH.sub.2Ph 4-CN-Phenyl 157 1 COMe 4-CN-Phenyl 158 2 COMe 4-CN-Phenyl 159 3 COMe 4-CN-Phenyl 160 4 COMe 4-CN-Phenyl 161 1 CO.sub.2Me 4-CN-Phenyl 162 2 CO.sub.2Me 4-CN-Phenyl 163 3 CO.sub.2Me 4-CN-Phenyl 164 4 CO.sub.2Me 4-CN-Phenyl 165 1 CO.sub.2tBu 4-CN-Phenyl 166 2 CO.sub.2tBu 4-CN-Phenyl 167 3 CO.sub.2tBu 4-CN-Phenyl 168 4 CO.sub.2tBu 4-CN-Phenyl 169 1 CONHMe 4-CN-Phenyl 170 2 CONHMe 4-CN-Phenyl 171 3 CONHMe 4-CN-Phenyl 172 4 CONHMe 4-CN-Phenyl 173 1 SO.sub.2Me 4-CN-Phenyl 174 2 SO.sub.2Me 4-CN-Phenyl 175 3 SO.sub.2Me 4-CN-Phenyl 176 4 SO.sub.2Me 4-CN-Phenyl 177 1 SO.sub.2NH.sub.2 4-CN-Phenyl 178 2 SO.sub.2NH.sub.2 4-CN-Phenyl 179 3 SO.sub.2NH.sub.2 4-CN-Phenyl 180 4 SO.sub.2NH.sub.2 4-CN-Phenyl 181 1 H 2-CN-Phenyl 182 2 H 2-CN-Phenyl 183 3 H 2-CN-Phenyl 184 4 H 2-CN-Phenyl 185 1 Me 2-CN-Phenyl 186 2 Me 2-CN-Phenyl 187 3 Me 2-CN-Phenyl 188 4 Me 2-CN-Phenyl 189 1 CH.sub.2Ph 2-CN-Phenyl 190 2 CH.sub.2Ph 2-CN-Phenyl 191 3 CH.sub.2Ph 2-CN-Phenyl 192 4 CH.sub.2Ph 2-CN-Phenyl 193 1 COMe 2-CN-Phenyl 194 2 COMe 2-CN-Phenyl 195 3 COMe 2-CN-Phenyl 196 4 COMe 2-CN-Phenyl 197 1 CO.sub.2Me 2-CN-Phenyl 198 2 CO.sub.2Me 2-CN-Phenyl 199 3 CO.sub.2Me 2-CN-Phenyl 200 4 CO.sub.2Me 2-CN-Phenyl 201 1 CO.sub.2tBu 2-CN-Phenyl 202 2 CO.sub.2tBu 2-CN-Phenyl 203 3 CO.sub.2tBu 2-CN-Phenyl 204 4 CO.sub.2tBu 2-CN-Phenyl 205 1 CONHMe 2-CN-Phenyl 206 2 CONHMe 2-CN-Phenyl 207 3 CONHMe 2-CN-Phenyl 208 4 CONHMe 2-CN-Phenyl 209 1 SO.sub.2Me 2-CN-Phenyl 210 2 SO.sub.2Me 2-CN-Phenyl 211 3 SO.sub.2Me 2-CN-Phenyl 212 4 SO.sub.2Me 2-CN-Phenyl 213 1 SO.sub.2NH.sub.2 2-CN-Phenyl 214 2 SO.sub.2NH.sub.2 2-CN-Phenyl 215 3 SO.sub.2NH.sub.2 2-CN-Phenyl 216 4 SO.sub.2NH.sub.2 2-CN-Phenyl 217 1 H 3-Me-Phenyl 218 2 H 3-Me-Phenyl 219 3 H 3-Me-Phenyl 220 4 H 3-Me-Phenyl 221 1 Me 3-Me-Phenyl 222 2 Me 3-Me-Phenyl 223 3 Me 3-Me-Phenyl 224 4 Me 3-Me-Phenyl 225 1 CH.sub.2Ph 3-Me-Phenyl 226 2 CH.sub.2Ph 3-Me-Phenyl 227 3 CH.sub.2Ph 3-Me-Phenyl 228 4 CH.sub.2Ph 3-Me-Phenyl 229 1 COMe 3-Me-Phenyl 230 2 COMe 3-Me-Phenyl 231 3 COMe 3-Me-Phenyl 232 4 COMe 3-Me-Phenyl 233 1 CO.sub.2Me 3-Me-Phenyl 234 2 CO.sub.2Me 3-Me-Phenyl 235 3 CO.sub.2Me 3-Me-Phenyl 236 4 CO.sub.2Me 3-Me-Phenyl 237 1 CO.sub.2tBu 3-Me-Phenyl 238 2 CO.sub.2tBu 3-Me-Phenyl 239 3 CO.sub.2tBu 3-Me-Phenyl 240 4 CO.sub.2tBu 3-Me-Phenyl 241 1 CONHMe 3-Me-Phenyl 242 2 CONHMe 3-Me-Phenyl 243 3 CONHMe 3-Me-Phenyl 244 4 CONHMe 3-Me-Phenyl 245 1 SO.sub.2Me 3-Me-Phenyl 246 2 SO.sub.2Me 3-Me-Phenyl 247 3 SO.sub.2Me 3-Me-Phenyl 248 4 SO.sub.2Me 3-Me-Phenyl 249 1 SO.sub.2NH.sub.2 3-Me-Phenyl 250 2 SO.sub.2NH.sub.2 3-Me-Phenyl 251 3 SO.sub.2NH.sub.2 3-Me-Phenyl 252 4 SO.sub.2NH.sub.2 3-Me-Phenyl 253 1 H 2-F-Phenyl 254 2 H 2-F-Phenyl 255 3 H 2-F-Phenyl 256 4 H 2-F-Phenyl 257 1 Me 2-F-Phenyl 258 2 Me 2-F-Phenyl 259 3 Me 2-F-Phenyl 260 4 Me 2-F-Phenyl 261 1 CH.sub.2Ph 2-F-Phenyl 262 2 CH.sub.2Ph 2-F-Phenyl 263 3 CH.sub.2Ph 2-F-Phenyl 264 4 CH.sub.2Ph 2-F-Phenyl 265 1 COMe 2-F-Phenyl 266 2 COMe 2-F-Phenyl 267 3 COMe 2-F-Phenyl 268 4 COMe 2-F-Phenyl 269 1 CO.sub.2Me 2-F-Phenyl 270 2 CO.sub.2Me 2-F-Phenyl 271 3 CO.sub.2Me 2-F-Phenyl 272 4 CO.sub.2Me 2-F-Phenyl 273 1 CO.sub.2tBu 2-F-Phenyl 274 2 CO.sub.2tBu 2-F-Phenyl 275 3 CO.sub.2tBu 2-F-Phenyl 276 4 CO.sub.2tBu 2-F-Phenyl 277 1 CONHMe 2-F-Phenyl 278 2 CONHMe 2-F-Phenyl 279 3 CONHMe 2-F-Phenyl 280 4 CONHMe 2-F-Phenyl 281 1 SO.sub.2Me 2-F-Phenyl 282 2 SO.sub.2Me 2-F-Phenyl 283 3 SO.sub.2Me 2-F-Phenyl 284 4 SO.sub.2Me 2-F-Phenyl 285 1 SO.sub.2NH.sub.2 2-F-Phenyl 286 2 SO.sub.2NH.sub.2 2-F-Phenyl 287 3 SO.sub.2NH.sub.2 2-F-Phenyl 288 4 SO.sub.2NH.sub.2 2-F-Phenyl 289 1 H 4-F-Phenyl 290 2 H 4-F-Phenyl 291 3 H 4-F-Phenyl 292 4 H 4-F-Phenyl 293 1 Me 4-F-Phenyl 294 2 Me 4-F-Phenyl 295 3 Me 4-F-Phenyl 296 4 Me 4-F-Phenyl 297 1 CH.sub.2Ph 4-F-Phenyl 298 2 CH.sub.2Ph 4-F-Phenyl 299 3 CH.sub.2Ph 4-F-Phenyl 300 4 CH.sub.2Ph 4-F-Phenyl 301 1 COMe 4-F-Phenyl 302 2 COMe 4-F-Phenyl 303 3 COMe 4-F-Phenyl 304 4 COMe 4-F-Phenyl 305 1 CO.sub.2Me 4-F-Phenyl 306 2 CO.sub.2Me 4-F-Phenyl 307 3 CO.sub.2Me 4-F-Phenyl 308 4 CO.sub.2Me 4-F-Phenyl 309 1 CO.sub.2tBu 4-F-Phenyl 310 2 CO.sub.2tBu 4-F-Phenyl 311 3 CO.sub.2tBu 4-F-Phenyl 312 4 CO.sub.2tBu 4-F-Phenyl 313 1 CONHMe 4-F-Phenyl 314 2 CONHMe 4-F-Phenyl 315 3 CONHMe 4-F-Phenyl 316 4 CONHMe 4-F-Phenyl 317 1 SO.sub.2Me 4-F-Phenyl 318 2 SO.sub.2Me 4-F-Phenyl 319 3 SO.sub.2Me 4-F-Phenyl 320 4 SO.sub.2Me 4-F-Phenyl 321 1 SO.sub.2NH.sub.2 4-F-Phenyl 322 2 SO.sub.2NH.sub.2 4-F-Phenyl 323 3 SO.sub.2NH.sub.2 4-F-Phenyl 324 4 SO.sub.2NH.sub.2 4-F-Phenyl 325 1 H 3-Cl-Phenyl 326 2 H 3-Cl-Phenyl 327 3 H 3-Cl-Phenyl 328 4 H 3-Cl-Phenyl 329 1 Me 3-Cl-Phenyl 330 2 Me 3-Cl-Phenyl 331 3 Me 3-Cl-Phenyl 332 4 Me 3-Cl-Phenyl 333 1 CH.sub.2Ph 3-Cl-Phenyl 334 2 CH.sub.2Ph 3-Cl-Phenyl 335 3 CH.sub.2Ph 3-Cl-Phenyl 336 4 CH.sub.2Ph 3-Cl-Phenyl 337 1 COMe 3-Cl-Phenyl 338 2 COMe 3-Cl-Phenyl 339 3 COMe 3-Cl-Phenyl 340 4 COMe 3-Cl-Phenyl 341 1 CO.sub.2Me 3-Cl-Phenyl 342 2 CO.sub.2Me 3-Cl-Phenyl 343 3 CO.sub.2Me 3-Cl-Phenyl 344 4 CO.sub.2Me 3-Cl-Phenyl 345 1 CO.sub.2tBu 3-Cl-Phenyl 346 2 CO.sub.2tBu 3-Cl-Phenyl 347 3 CO.sub.2tBu 3-Cl-Phenyl 348 4 CO.sub.2tBu 3-Cl-Phenyl 349 1 CONHMe 3-Cl-Phenyl 350 2 CONHMe 3-Cl-Phenyl 351 3 CONHMe 3-Cl-Phenyl 352 4 CONHMe 3-Cl-Phenyl 353 1 SO.sub.2Me 3-Cl-Phenyl 354 2 SO.sub.2Me 3-Cl-Phenyl 355 3 SO.sub.2Me 3-Cl-Phenyl 356 4 SO.sub.2Me 3-Cl-Phenyl 357 1 SO.sub.2NH.sub.2 3-Cl-Phenyl 358 2 SO.sub.2NH.sub.2 3-Cl-Phenyl 359 3 SO.sub.2NH.sub.2 3-Cl-Phenyl 360 4 SO.sub.2NH.sub.2 3-Cl-Phenyl 361 1 H 2-Br-Phenyl 362 2 H 2-Br-Phenyl 363 3 H 2-Br-Phenyl 364 4 H 2-Br-Phenyl 365 1 Me 2-Br-Phenyl 366 2 Me 2-Br-Phenyl 367 3 Me 2-Br-Phenyl 368 4 Me 2-Br-Phenyl 369 1 CH.sub.2Ph 2-Br-Phenyl 370 2 CH.sub.2Ph 2-Br-Phenyl 371 3 CH.sub.2Ph 2-Br-Phenyl 372 4 CH.sub.2Ph 2-Br-Phenyl 373 1 COMe 2-Br-Phenyl 374 2 COMe 2-Br-Phenyl 375 3 COMe 2-Br-Phenyl 376 4 COMe 2-Br-Phenyl 377 1 CO.sub.2Me 2-Br-Phenyl 378 2 CO.sub.2Me 2-Br-Phenyl 379 3 CO.sub.2Me 2-Br-Phenyl 380 4 CO.sub.2Me 2-Br-Phenyl 381 1 CO.sub.2tBu 2-Br-Phenyl 382 2 CO.sub.2tBu 2-Br-Phenyl 383 3 CO.sub.2tBu 2-Br-Phenyl 384 4 CO.sub.2tBu 2-Br-Phenyl 385 1 CONHMe 2-Br-Phenyl 386 2 CONHMe 2-Br-Phenyl 387 3 CONHMe 2-Br-Phenyl 388 4 CONHMe 2-Br-Phenyl 389 1 SO.sub.2Me 2-Br-Phenyl 390 2 SO.sub.2Me 2-Br-Phenyl 391 3 SO.sub.2Me 2-Br-Phenyl 392 4 SO.sub.2Me 2-Br-Phenyl 393 1 SO.sub.2NH.sub.2 2-Br-Phenyl 394 2 SO.sub.2NH.sub.2 2-Br-Phenyl 395 3 SO.sub.2NH.sub.2 2-Br-Phenyl 396 4 SO.sub.2NH.sub.2 2-Br-Phenyl 397 1 H 4-Br-Phenyl 398 2 H 4-Br-Phenyl 399 3 H 4-Br-Phenyl 400 4 H 4-Br-Phenyl 401 1 Me 4-Br-Phenyl 402 2 Me 4-Br-Phenyl 403 3 Me 4-Br-Phenyl 404 4 Me 4-Br-Phenyl 405 1 CH.sub.2Ph 4-Br-Phenyl 406 2 CH.sub.2Ph 4-Br-Phenyl 407 3 CH.sub.2Ph 4-Br-Phenyl 408 4 CH.sub.2Ph 4-Br-Phenyl 409 1 COMe 4-Br-Phenyl 410 2 COMe 4-Br-Phenyl 411 3 COMe 4-Br-Phenyl 412 4 COMe 4-Br-Phenyl 413 1 CO.sub.2Me 4-Br-Phenyl 414 2 CO.sub.2Me 4-Br-Phenyl 415 3 CO.sub.2Me 4-Br-Phenyl 416 4 CO.sub.2Me 4-Br-Phenyl 417 1 CO.sub.2tBu 4-Br-Phenyl 418 2 CO.sub.2tBu 4-Br-Phenyl 419 3 CO.sub.2tBu 4-Br-Phenyl 420 4 CO.sub.2tBu 4-Br-Phenyl 421 1 CONHMe 4-Br-Phenyl 422 2 CONHMe 4-Br-Phenyl 423 3 CONHMe 4-Br-Phenyl 424 4 CONHMe 4-Br-Phenyl 425 1 SO.sub.2Me 4-Br-Phenyl 426 2 SO.sub.2Me 4-Br-Phenyl 427 3 SO.sub.2Me 4-Br-Phenyl 428 4 SO.sub.2Me 4-Br-Phenyl 429 1 SO.sub.2NH.sub.2 4-Br-Phenyl 430 2 SO.sub.2NH.sub.2 4-Br-Phenyl 431 3 SO.sub.2NH.sub.2 4-Br-Phenyl 432 4 SO.sub.2NH.sub.2 4-Br-Phenyl 433 1 H 3-CF.sub.3-Phenyl 434 2 H 3-CF.sub.3-Phenyl 435 3 H 3-CF.sub.3-Phenyl 436 4 H 3-CF.sub.3-Phenyl 437 1 Me 3-CF.sub.3-Phenyl 438 2 Me 3-CF.sub.3-Phenyl 439 3 Me 3-CF.sub.3-Phenyl 440 4 Me 3-CF.sub.3-Phenyl 441 1 CH.sub.2Ph 3-CF.sub.3-Phenyl 442 2 CH.sub.2Ph 3-CF.sub.3-Phenyl 443 3 CH.sub.2Ph 3-CF.sub.3-Phenyl 444 4 CH.sub.2Ph 3-CF.sub.3-Phenyl 445 1 COMe 3-CF.sub.3-Phenyl 446 2 COMe 3-CF.sub.3-Phenyl 447 3 COMe 3-CF.sub.3-Phenyl 448 4 COMe 3-CF.sub.3-Phenyl 449 1 CO.sub.2Me 3-CF.sub.3-Phenyl 450 2 CO.sub.2Me 3-CF.sub.3-Phenyl 451 3 CO.sub.2Me 3-CF.sub.3-Phenyl 452 4 CO.sub.2Me 3-CF.sub.3-Phenyl 453 1 CO.sub.2tBu 3-CF.sub.3-Phenyl 454 2 CO.sub.2tBu 3-CF.sub.3-Phenyl 455 3 CO.sub.2tBu 3-CF.sub.3-Phenyl 456 4 CO.sub.2tBu 3-CF.sub.3-Phenyl 457 1 CONHMe 3-CF.sub.3-Phenyl 458 2 CONHMe 3-CF.sub.3-Phenyl 459 3 CONHMe 3-CF.sub.3-Phenyl 460 4 CONHMe 3-CF.sub.3-Phenyl 461 1 SO.sub.2Me 3-CF.sub.3-Phenyl 462 2 SO.sub.2Me 3-CF.sub.3-Phenyl 463 3 SO.sub.2Me 3-CF.sub.3-Phenyl 464 4 SO.sub.2Me 3-CF.sub.3-Phenyl 465 1 SO.sub.2NH.sub.2 3-CF.sub.3-Phenyl 466 2 SO.sub.2NH.sub.2 3-CF.sub.3-Phenyl 467 3 SO.sub.2NH.sub.2 3-CF.sub.3-Phenyl 468 4 SO.sub.2NH.sub.2 3-CF.sub.3-Phenyl 469 1 H 2-iPr-Phenyl 470 2 H 2-iPr-Phenyl 471 3 H 2-iPr-Phenyl 472 4 H 2-iPr-Phenyl 473 1 Me 2-iPr-Phenyl 474 2 Me 2-iPr-Phenyl 475 3 Me 2-iPr-Phenyl 476 4 Me 2-iPr-Phenyl 477 1 CH.sub.2Ph 2-iPr-Phenyl 478 2 CH.sub.2Ph 2-iPr-Phenyl 479 3 CH.sub.2Ph 2-iPr-Phenyl 480 4 CH.sub.2Ph 2-iPr-Phenyl 481 1 COMe 2-iPr-Phenyl 482 2 COMe 2-iPr-Phenyl 483 3 COMe 2-iPr-Phenyl 484 4 COMe 2-iPr-Phenyl 485 1 CO.sub.2Me 2-iPr-Phenyl 486 2 CO.sub.2Me 2-iPr-Phenyl 487 3 CO.sub.2Me 2-iPr-Phenyl 488 4 CO.sub.2Me 2-iPr-Phenyl 489 1 CO.sub.2tBu 2-iPr-Phenyl 490 2 CO.sub.2tBu 2-iPr-Phenyl 491 3 CO.sub.2tBu 2-iPr-Phenyl 492 4 CO.sub.2tBu 2-iPr-Phenyl 493 1 CONHMe 2-iPr-Phenyl 494 2 CONHMe 2-iPr-Phenyl 495 3 CONHMe 2-iPr-Phenyl 496 4 CONHMe 2-iPr-Phenyl 497 1 SO.sub.2Me 2-iPr-Phenyl 498 2 SO.sub.2Me 2-iPr-Phenyl 499 3 SO.sub.2Me 2-iPr-Phenyl 500 4 SO.sub.2Me 2-iPr-Phenyl 501 1 SO.sub.2NH.sub.2 2-iPr-Phenyl 502 2 SO.sub.2NH.sub.2 2-iPr-Phenyl 503 3 SO.sub.2NH.sub.2 2-iPr-Phenyl 504 4 SO.sub.2NH.sub.2 2-iPr-Phenyl 505 1 H 4-iPr-Phenyl 506 2 H 4-iPr-Phenyl 507 3 H 4-iPr-Phenyl 508 4 H 4-iPr-Phenyl 509 1 Me 4-iPr-Phenyl 510 2 Me 4-iPr-Phenyl 511 3 Me 4-iPr-Phenyl 512 4 Me 4-iPr-Phenyl 513 1 CH.sub.2Ph 4-iPr-Phenyl 514 2 CH.sub.2Ph 4-iPr-Phenyl 515 3 CH.sub.2Ph 4-iPr-Phenyl 516 4 CH.sub.2Ph 4-iPr-Phenyl 517 1 COMe 4-iPr-Phenyl 518 2 COMe 4-iPr-Phenyl 519 3 COMe 4-iPr-Phenyl 520 4 COMe 4-iPr-Phenyl 521 1 CO.sub.2Me 4-iPr-Phenyl 522 2 CO.sub.2Me 4-iPr-Phenyl 523 3 CO.sub.2Me 4-iPr-Phenyl 524 4 CO.sub.2Me 4-iPr-Phenyl 525 1 CO.sub.2tBu 4-iPr-Phenyl 526 2 CO.sub.2tBu 4-iPr-Phenyl 527 3 CO.sub.2tBu 4-iPr-Phenyl 528 4 CO.sub.2tBu 4-iPr-Phenyl 529 1 CONHMe 4-iPr-Phenyl 530 2 CONHMe 4-iPr-Phenyl 531 3 CONHMe 4-iPr-Phenyl 532 4 CONHMe 4-iPr-Phenyl 533 1 SO.sub.2Me 4-iPr-Phenyl 534 2 SO.sub.2Me 4-iPr-Phenyl 535 3 SO.sub.2Me 4-iPr-Phenyl 536 4 SO.sub.2Me 4-iPr-Phenyl 537 1 SO.sub.2NH.sub.2 4-iPr-Phenyl 538 2 SO.sub.2NH.sub.2 4-iPr-Phenyl 539 3 SO.sub.2NH.sub.2 4-iPr-Phenyl 540 4 SO.sub.2NH.sub.2 4-iPr-Phenyl 541 1 H 3-NH.sub.2-Phenyl 542 2 H 3-NH.sub.2-Phenyl 543 3 H 3-NH.sub.2-Phenyl 544 4 H 3-NH.sub.2-Phenyl 545 1 Me 3-NH.sub.2-Phenyl 546 2 Me 3-NH.sub.2-Phenyl 547 3 Me 3-NH.sub.2-Phenyl 548 4 Me 3-NH.sub.2-Phenyl 549 1 CH.sub.2Ph 3-NH.sub.2-Phenyl 550 2 CH.sub.2Ph 3-NH.sub.2-Phenyl 551 3 CH.sub.2Ph 3-NH.sub.2-Phenyl 552 4 CH.sub.2Ph 3-NH.sub.2-Phenyl 553 1 COMe 3-NH.sub.2-Phenyl 554 2 COMe 3-NH.sub.2-Phenyl 555 3 COMe 3-NH.sub.2-Phenyl 556 4 COMe 3-NH.sub.2-Phenyl 557 1 CO.sub.2Me 3-NH.sub.2-Phenyl 558 2 CO.sub.2Me 3-NH.sub.2-Phenyl 559 3 CO.sub.2Me 3-NH.sub.2-Phenyl 560 4 CO.sub.2Me 3-NH.sub.2-Phenyl 561 1 CO.sub.2tBu 3-NH.sub.2-Phenyl 562 2 CO.sub.2tBu 3-NH.sub.2-Phenyl 563 3 CO.sub.2tBu 3-NH.sub.2-Phenyl 564 4 CO.sub.2tBu 3-NH.sub.2-Phenyl 565 1 CONHMe 3-NH.sub.2-Phenyl 566 2 CONHMe 3-NH.sub.2-Phenyl 567 3 CONHMe 3-NH.sub.2-Phenyl 568 4 CONHMe 3-NH.sub.2-Phenyl 569 1 SO.sub.2Me 3-NH.sub.2-Phenyl 570 2 SO.sub.2Me 3-NH.sub.2-Phenyl 571 3 SO.sub.2Me 3-NH.sub.2-Phenyl 572 4 SO.sub.2Me 3-NH.sub.2-Phenyl 573 1 SO.sub.2NH.sub.2 3-NH.sub.2-Phenyl 574 2 SO.sub.2NH.sub.2 3-NH.sub.2-Phenyl 575 3 SO.sub.2NH.sub.2 3-NH.sub.2-Phenyl 576 4 SO.sub.2NH.sub.2 3-NH.sub.2-Phenyl 577 1 H 2,4-di-Me-Phenyl 578 2 H 2,4-di-Me-Phenyl 579 3 H 2,4-di-Me-Phenyl 580 4 H 2,4-di-Me-Phenyl 581 1 Me 2,4-di-Me-Phenyl 582 2 Me 2,4-di-Me-Phenyl 583 3 Me 2,4-di-Me-Phenyl 584 4 Me 2,4-di-Me-Phenyl 585 1 CH.sub.2Ph 2,4-di-Me-Phenyl 586 2 CH.sub.2Ph 2,4-di-Me-Phenyl 587 3 CH.sub.2Ph 2,4-di-Me-Phenyl 588 4 CH.sub.2Ph 2,4-di-Me-Phenyl 589 1 COMe 2,4-di-Me-Phenyl 590 2 COMe 2,4-di-Me-Phenyl 591 3 COMe 2,4-di-Me-Phenyl 592 4 COMe 2,4-di-Me-Phenyl 593 1 CO.sub.2Me 2,4-di-Me-Phenyl 594 2 CO.sub.2Me 2,4-di-Me-Phenyl 595 3 CO.sub.2Me 2,4-di-Me-Phenyl 596 4 CO.sub.2Me 2,4-di-Me-Phenyl 597 1 CO.sub.2tBu 2,4-di-Me-Phenyl 598 2 CO.sub.2tBu 2,4-di-Me-Phenyl 599 3 CO.sub.2tBu 2,4-di-Me-Phenyl 600 4 CO.sub.2tBu 2,4-di-Me-Phenyl 601 1 CONHMe 2,4-di-Me-Phenyl 602 2 CONHMe 2,4-di-Me-Phenyl 603 3 CONHMe 2,4-di-Me-Phenyl 604 4 CONHMe 2,4-di-Me-Phenyl 605 1 SO.sub.2Me 2,4-di-Me-Phenyl 606 2 SO.sub.2Me 2,4-di-Me-Phenyl 607 3 SO.sub.2Me 2,4-di-Me-Phenyl 608 4 SO.sub.2Me 2,4-di-Me-Phenyl 609 1 SO.sub.2NH.sub.2 2,4-di-Me-Phenyl 610 2 SO.sub.2NH.sub.2 2,4-di-Me-Phenyl 611 3 SO.sub.2NH.sub.2 2,4-di-Me-Phenyl 612 4 SO.sub.2NH.sub.2 2,4-di-Me-Phenyl 613 1 H 2,6-di-iPr-Phenyl 614 2 H 2,6-di-iPr-Phenyl 615 3 H 2,6-di-iPr-Phenyl 616 4 H 2,6-di-iPr-Phenyl 617 1 Me 2,6-di-iPr-Phenyl 618 2 Me 2,6-di-iPr-Phenyl 619 3 Me 2,6-di-iPr-Phenyl 620 4 Me 2,6-di-iPr-Phenyl 621 1 CH.sub.2Ph 2,6-di-iPr-Phenyl 622 2 CH.sub.2Ph 2,6-di-iPr-Phenyl 623 3 CH.sub.2Ph 2,6-di-iPr-Phenyl 624 3 CH.sub.2Ph 2,6-di-iPr-Phenyl 625 1 COMe 2,6-di-iPr-Phenyl 626 2 COMe 2,6-di-iPr-Phenyl 627 3 COMe 2,6-di-iPr-Phenyl 628 4 COMe 2,6-di-iPr-Phenyl 629 1 CO.sub.2Me 2,6-di-iPr-Phenyl 630 2 CO.sub.2Me 2,6-di-iPr-Phenyl 631 3 CO.sub.2Me 2,6-di-iPr-Phenyl 632 4 CO.sub.2Me 2,6-di-iPr-Phenyl 633 1 CO.sub.2tBu 2,6-di-iPr-Phenyl 634 2 CO.sub.2tBu 2,6-di-iPr-Phenyl 635 3 CO.sub.2tBu 2,6-di-iPr-Phenyl 636 4 CO.sub.2tBu 2,6-di-iPr-Phenyl 637 1 CONHMe 2,6-di-iPr-Phenyl 638 2 CONHMe 2,6-di-iPr-Phenyl 639 3 CONHMe 2,6-di-iPr-Phenyl 640 4 CONHMe 2,6-di-iPr-Phenyl 641 1 SO.sub.2Me 2,6-di-iPr-Phenyl 642 2 SO.sub.2Me 2,6-di-iPr-Phenyl 643 3 SO.sub.2Me 2,6-di-iPr-Phenyl 644 4 SO.sub.2Me 2,6-di-iPr-Phenyl 645 1 SO.sub.2NH.sub.2 2,6-di-iPr-Phenyl 646 2 SO.sub.2NH.sub.2 2,6-di-iPr-Phenyl 647 3 SO.sub.2NH.sub.2 2,6-di-iPr-Phenyl 648 4 SO.sub.2NH.sub.2 2,6-di-iPr-Phenyl 649 1 H 3-Ph-Phenyl 650 2 H 3-Ph-Phenyl 651 3 H 3-Ph-Phenyl 652 4 H 3-Ph-Phenyl 653 1 Me 3-Ph-Phenyl 654 2 Me 3-Ph-Phenyl 655 3 Me 3-Ph-Phenyl 656 4 Me 3-Ph-Phenyl 657 1 CH.sub.2Ph 3-Ph-Phenyl 658 2 CH.sub.2Ph 3-Ph-Phenyl 659 3 CH.sub.2Ph 3-Ph-Phenyl 660 4 CH.sub.2Ph 3-Ph-Phenyl 661 1 COMe 3-Ph-Phenyl 662 2 COMe 3-Ph-Phenyl 663 3 COMe 3-Ph-Phenyl 664 4 COMe 3-Ph-Phenyl 665 1 CO.sub.2Me 3-Ph-Phenyl 666 2 CO.sub.2Me 3-Ph-Phenyl 667 3 CO.sub.2Me 3-Ph-Phenyl 668 4 CO.sub.2Me 3-Ph-Phenyl 669 1 CO.sub.2tBu 3-Ph-Phenyl 670 2 CO.sub.2tBu 3-Ph-Phenyl 671 3 CO.sub.2tBu 3-Ph-Phenyl 672 4 CO.sub.2tBu 3-Ph-Phenyl 673 1 CONHMe 3-Ph-Phenyl 674 2 CONHMe 3-Ph-Phenyl 675 3 CONHMe 3-Ph-Phenyl 676 4 CONHMe 3-Ph-Phenyl 677 1 SO.sub.2Me 3-Ph-Phenyl 678 2 SO.sub.2Me 3-Ph-Phenyl 679 3 SO.sub.2Me 3-Ph-Phenyl 680 4 SO.sub.2Me 3-Ph-Phenyl 681 1 SO.sub.2NH.sub.2 3-Ph-Phenyl 682 2 SO.sub.2NH.sub.2 3-Ph-Phenyl 683 3 SO.sub.2NH.sub.2 3-Ph-Phenyl 684 4 SO.sub.2NH.sub.2 3-Ph-Phenyl 685 1 H 2-morpholino- phenyl 686 2 H 2-morpholino- phenyl 687 3 H 2-morpholino- phenyl 688 4 H 2-morpholino- phenyl 689 1 Me 2-morpholino- phenyl 690 2 Me 2-morpholino- phenyl 691 3 Me 2-morpholino- phenyl 692 4 Me 2-morpholino- phenyl 693 1 CH.sub.2Ph 2-morpholino- phenyl 694 2 CH.sub.2Ph 2-morpholino- phenyl 695 3 CH.sub.2Ph 2-morpholino- phenyl 696 4 CH.sub.2Ph 2-morpholino- phenyl 697 1 COMe 2-morpholino- phenyl 698 2 COMe 2-morpholino- phenyl 699 3 COMe 2-morpholino- phenyl 700 4 COMe 2-morpholino- phenyl 701 1 CO.sub.2Me 2-morpholino- phenyl 702 2 CO.sub.2Me 2-morpholino- phenyl 703 3 CO.sub.2Me 2-morpholino- phenyl 704 4 CO.sub.2Me 2-morpholino- phenyl 705 1 CO.sub.2tBu 2-morpholino- phenyl 706 2 CO.sub.2tBu 2-morpholino- phenyl 707 3 CO.sub.2tBu 2-morpholino- phenyl 708 4 CO.sub.2tBu 2-morpholino- phenyl 709 1 CONHMe 2-morpholino- phenyl 710 2 CONHMe 2-morpholino- phenyl 711 3 CONHMe 2-morpholino- phenyl 712 4 CONHMe 2-morpholino- phenyl 713 1 SO.sub.2Me 2-morpholino- phenyl 714 2 SO.sub.2Me 2-morpholino- phenyl 715 3 SO.sub.2Me 2-morpholino- phenyl 716 4 SO.sub.2Me 2-morpholino- phenyl 717 1 SO.sub.2NH.sub.2 2-morpholino- phenyl 718 2 SO.sub.2NH.sub.2 2-morpholino- phenyl 719 3 SO.sub.2NH.sub.2 2-morpholino- phenyl 720 4 SO.sub.2NH.sub.2 2-morpholino- phenyl 721 1 H 4-morpholino- phenyl 722 2 H 4-morpholino- phenyl 723 3 H 4-morpholino- phenyl 724 4 H 4-morpholino- phenyl 725 1 CH.sub.2Ph 4-morpholino- phenyl 726 2 CH.sub.2Ph 4-morpholino- phenyl 727 3 CH.sub.2Ph 4-morpholino- phenyl 728 4 CH.sub.2Ph 4-morpholino- phenyl 729 1 CO.sub.2Me 4-morpholino- phenyl 730 2 CO.sub.2Me 4-morpholino- phenyl 731 3 CO.sub.2Me 4-morpholino- phenyl 732 4 CO.sub.2Me 4-morpholino- phenyl 733 1 CONHMe 4-morpholino- phenyl 734 2 CONHMe 4-morpholino- phenyl 735 3 CONHMe 4-morpholino- phenyl 736 4 CONHMe 4-morpholino- phenyl 737 1 SO.sub.2NH.sub.2 4-morpholino- phenyl 738 2 SO.sub.2NH.sub.2 4-morpholino- phenyl 739 3 SO.sub.2NH.sub.2 4-morpholino- phenyl 740 1 H naphthylen-1-yl 741 2 H naphthylen-1-yl 742 3 H naphthylen-1-yl 743 4 H naphthylen-1-yl 744 1 Me naphthylen-1-yl 745 2 Me naphthylen-1-yl 746 3 Me naphthylen-1-yl 747 4 Me naphthylen-1-yl 748 1 CH.sub.2Ph naphthylen-1-yl 749 2 CH.sub.2Ph naphthylen-1-yl 750 3 CH.sub.2Ph naphthylen-1-yl 751 4 CH.sub.2Ph naphthylen-1-yl 752 1 COMe naphthylen-1-yl 753 2 COMe naphthylen-1-yl 754 3 COMe naphthylen-1-yl 755 4 COMe naphthylen-1-yl 756 1 CO.sub.2Me naphthylen-1-yl 757 2 CO.sub.2Me naphthylen-1-yl 758 3 CO.sub.2Me naphthylen-1-yl 759 4 CO.sub.2Me naphthylen-1-yl 760 1 CO.sub.2tBu naphthylen-1-yl 761 2 CO.sub.2tBu naphthylen-1-yl 762 3 CO.sub.2tBu naphthylen-1-yl 763 4 CO.sub.2tBu naphthylen-1-yl 764 1 CONHMe naphthylen-1-yl 765 2 CONHMe naphthylen-1-yl 767 3 CONHMe naphthylen-1-yl 768 4 CONHMe naphthylen-1-yl 769 1 SO.sub.2Me naphthylen-1-yl 770 2 SO.sub.2Me naphthylen-1-yl 771 3 SO.sub.2Me naphthylen-1-yl 772 4 SO.sub.2Me naphthylen-1-yl 773 1 SO.sub.2NH.sub.2 naphthylen-1-yl 774 2 SO.sub.2NH.sub.2 naphthylen-1-yl 775 3 SO.sub.2NH.sub.2 naphthylen-1-yl 778 4 SO.sub.2NH.sub.2 naphthylen-1-yl 779 1 H 4-OH-Phenyl 780 2 H 4-OH-Phenyl 781 3 H 4-OH-Phenyl 782 4 H 4-OH-Phenyl 783 1 Me 4-OH-Phenyl 784 2 Me 4-OH-Phenyl 785 3 Me 4-OH-Phenyl 786 4 Me 4-OH-Phenyl 787 1 CH.sub.2Ph 4-OH-Phenyl 788 2 CH.sub.2Ph 4-OH-Phenyl 789 3 CH.sub.2Ph 4-OH-Phenyl 790 4 CH.sub.2Ph 4-OH-Phenyl 791 1 COMe 4-OH-Phenyl 792 2 COMe 4-OH-Phenyl 793 3 COMe 4-OH-Phenyl 794 4 COMe 4-OH-Phenyl 795 1 CO.sub.2Me 4-OH-Phenyl 796 2 CO.sub.2Me 4-OH-Phenyl 797 3 CO.sub.2Me 4-OH-Phenyl 798 4 CO.sub.2Me 4-OH-Phenyl 799 1 CO.sub.2tBu 4-OH-Phenyl 800 2 CO.sub.2tBu 4-OH-Phenyl 801 3 CO.sub.2tBu 4-OH-Phenyl 802 4 CO.sub.2tBu 4-OH-Phenyl 803 1 CONHMe 4-OH-Phenyl 804 2 CONHMe 4-OH-Phenyl 805 3 CONHMe 4-OH-Phenyl 806 4 CONHMe 4-OH-Phenyl 807 1 SO.sub.2Me 4-OH-Phenyl 808 2 SO.sub.2Me 4-OH-Phenyl 809 3 SO.sub.2Me 4-OH-Phenyl 810 4 SO.sub.2Me 4-OH-Phenyl 811 1 SO.sub.2NH.sub.2 4-OH-Phenyl 812 2 SO.sub.2NH.sub.2 4-OH-Phenyl 813 3 SO.sub.2NH.sub.2 4-OH-Phenyl 814 4 SO.sub.2NH.sub.2 4-OH-Phenyl 815 1 H 2-OH-Phenyl 816 2 H 2-OH-Phenyl 817 3 H 2-OH-Phenyl 818 4 H 2-OH-Phenyl 819 1 Me 2-OH-Phenyl 820 2 Me 2-OH-Phenyl 821 3 Me 2-OH-Phenyl 822 4 Me 2-OH-Phenyl 823 1 CH.sub.2Ph 2-OH-Phenyl 824 2 CH.sub.2Ph 2-OH-Phenyl 825 3 CH.sub.2Ph 2-OH-Phenyl 826 4 CH.sub.2Ph 2-OH-Phenyl 827 1 COMe 2-OH-Phenyl 828 2 COMe 2-OH-Phenyl 829 3 COMe 2-OH-Phenyl 830 4 COMe 2-OH-Phenyl 831 1 CO.sub.2Me 2-OH-Phenyl 832 2 CO.sub.2Me 2-OH-Phenyl 833 3 CO.sub.2Me 2-OH-Phenyl 834 4 CO.sub.2Me 2-OH-Phenyl 835 1 CO.sub.2tBu 2-OH-Phenyl 836 2 CO.sub.2tBu 2-OH-Phenyl 837 3 CO.sub.2tBu 2-OH-Phenyl 838 4 CO.sub.2tBu 2-OH-Phenyl 839 1 CONHMe 2-OH-Phenyl 840 2 CONHMe 2-OH-Phenyl 841 3 CONHMe 2-OH-Phenyl 842 4 CONHMe 2-OH-Phenyl 843 1 SO.sub.2Me 2-OH-Phenyl 844 2 SO.sub.2Me 2-OH-Phenyl 845 3 SO.sub.2Me 2-OH-Phenyl 846 4 SO.sub.2Me 2-OH-Phenyl 847 1 SO.sub.2NH.sub.2 2-OH-Phenyl 848 2 SO.sub.2NH.sub.2 2-OH-Phenyl 849 3 SO.sub.2NH.sub.2 2-OH-Phenyl 850 4 SO.sub.2NH.sub.2 2-OH-Phenyl 851 1 H 4-OMe-Phenyl 852 2 H 4-OMe-Phenyl 853 3 H 4-OMe-Phenyl 854 4 H 4-OMe-Phenyl 855 1 Me 4-OMe-Phenyl 856 2 Me 4-OMe-Phenyl 857 3 Me 4-OMe-Phenyl 858 4 Me 4-OMe-Phenyl 859 1 CH.sub.2Ph 4-OMe-Phenyl 860 2 CH.sub.2Ph 4-OMe-Phenyl 861 3 CH.sub.2Ph 4-OMe-Phenyl 862 4 CH.sub.2Ph 4-OMe-Phenyl 863 1 COMe 4-OMe-Phenyl 864 2 COMe 4-OMe-Phenyl 865 3 COMe 4-OMe-Phenyl 866 4 COMe 4-OMe-Phenyl 867 1 CO.sub.2Me 4-OMe-Phenyl 868 2 CO.sub.2Me 4-OMe-Phenyl 869 3 CO.sub.2Me 4-OMe-Phenyl 870 4 CO.sub.2Me 4-OMe-Phenyl 871 1 CO.sub.2tBu 4-OMe-Phenyl 872 2 CO.sub.2tBu 4-OMe-Phenyl 873 3 CO.sub.2tBu 4-OMe-Phenyl 874 4 CO.sub.2tBu 4-OMe-Phenyl 875 1 CONHMe 4-OMe-Phenyl 876 2 CONHMe 4-OMe-Phenyl 877 3 CONHMe 4-OMe-Phenyl 878 4 CONHMe 4-OMe-Phenyl 879 1 SO.sub.2Me 4-OMe-Phenyl 880 2 SO.sub.2Me 4-OMe-Phenyl 881 3 SO.sub.2Me 4-OMe-Phenyl 882 4 SO.sub.2Me 4-OMe-Phenyl 883 1 SO.sub.2NH.sub.2 4-OMe-Phenyl 884 2 SO.sub.2NH.sub.2 4-OMe-Phenyl 885 3 SO.sub.2NH.sub.2 4-OMe-Phenyl 886 4 SO.sub.2NH.sub.2 4-OMe-Phenyl 887 1 H 2-OMe-Phenyl 888 2 H 2-OMe-Phenyl 889 3 H 2-OMe-Phenyl 890 4 H 2-OMe-Phenyl 891 1 Me 2-OMe-Phenyl 892 2 Me 2-OMe-Phenyl 893 3 Me 2-OMe-Phenyl 894 4 Me 2-OMe-Phenyl 895 1 CH.sub.2Ph 2-OMe-Phenyl 896 2 CH.sub.2Ph 2-OMe-Phenyl 897 3 CH.sub.2Ph 2-OMe-Phenyl 898 4 CH.sub.2Ph 2-OMe-Phenyl 899 1 COMe 2-OMe-Phenyl 900 2 COMe 2-OMe-Phenyl 901 3 COMe 2-OMe-Phenyl 902 4 COMe 2-OMe-Phenyl 903 1 CO.sub.2Me 2-OMe-Phenyl 904 2 CO.sub.2Me 2-OMe-Phenyl 905 3 CO.sub.2Me 2-OMe-Phenyl 906 4 CO.sub.2Me 2-OMe-Phenyl 907 1 CO.sub.2tBu 2-OMe-Phenyl 908 2 CO.sub.2tBu 2-OMe-Phenyl 909 3 CO.sub.2tBu 2-OMe-Phenyl 910 4 CO.sub.2tBu 2-OMe-Phenyl 911 1 CONHMe 2-OMe-Phenyl 912 2 CONHMe 2-OMe-Phenyl 913 3 CONHMe 2-OMe-Phenyl 914 4 CONHMe 2-OMe-Phenyl 915 1 SO.sub.2Me 2-OMe-Phenyl 916 2 SO.sub.2Me 2-OMe-Phenyl 917 3 SO.sub.2Me 2-OMe-Phenyl 918 4 SO.sub.2Me 2-OMe-Phenyl 919 1 SO.sub.2NH.sub.2 2-OMe-Phenyl 920 2 SO.sub.2NH.sub.2 2-OMe-Phenyl 921 3 SO.sub.2NH.sub.2 2-OMe-Phenyl 922 4 SO.sub.2NH.sub.2 2-OMe-Phenyl 923 1 H 3-CN-Phenyl 924 2 H 3-CN-Phenyl 925 3 H 3-CN-Phenyl 926 4 H 3-CN-Phenyl 927 1 Me 3-CN-Phenyl 928 2 Me 3-CN-Phenyl 929 3 Me 3-CN-Phenyl 930 4 Me 3-CN-Phenyl 931 1 CH.sub.2Ph 3-CN-Phenyl 932 2 CH.sub.2Ph 3-CN-Phenyl 933 3 CH.sub.2Ph 3-CN-Phenyl 934 4 CH.sub.2Ph 3-CN-Phenyl 935 1 COMe 3-CN-Phenyl 936 2 COMe 3-CN-Phenyl 937 3 COMe 3-CN-Phenyl 938 4 COMe 3-CN-Phenyl 939 1 CO.sub.2Me 3-CN-Phenyl 940 2 CO.sub.2Me 3-CN-Phenyl 941 3 CO.sub.2Me 3-CN-Phenyl 942 4 CO.sub.2Me 3-CN-Phenyl 943 1 CO.sub.2tBu 3-CN-Phenyl 944 2 CO.sub.2tBu 3-CN-Phenyl 945 3 CO.sub.2tBu 3-CN-Phenyl 946 4 CO.sub.2tBu 3-CN-Phenyl 947 1 CONHMe 3-CN-Phenyl 948 2 CONHMe 3-CN-Phenyl 949 3 CONHMe 3-CN-Phenyl 950 4 CONHMe 3-CN-Phenyl 951 1 SO.sub.2Me 3-CN-Phenyl 952 2 SO.sub.2Me 3-CN-Phenyl 953 3 SO.sub.2Me 3-CN-Phenyl 954 4 SO.sub.2Me 3-CN-Phenyl 955 1 SO.sub.2NH.sub.2 3-CN-Phenyl 956 2 SO.sub.2NH.sub.2 3-CN-Phenyl 957 3 SO.sub.2NH.sub.2 3-CN-Phenyl 958 4 SO.sub.2NH.sub.2 3-CN-Phenyl 959 1 H 2-Me-Phenyl 960 2 H 2-Me-Phenyl 961 3 H 2-Me-Phenyl 962 4 H 2-Me-Phenyl 963 1 Me 2-Me-Phenyl 964 2 Me 2-Me-Phenyl 965 3 Me 2-Me-Phenyl 966 4 Me 2-Me-Phenyl 967 1 CH.sub.2Ph 2-Me-Phenyl 968 2 CH.sub.2Ph 2-Me-Phenyl 969 3 CH.sub.2Ph 2-Me-Phenyl 970 4 CH.sub.2Ph 2-Me-Phenyl 971 1 COMe 2-Me-Phenyl 972 2 COMe 2-Me-Phenyl 973 3 COMe 2-Me-Phenyl 974 4 COMe 2-Me-Phenyl 975 1 CO.sub.2Me 2-Me-Phenyl 976 2 CO.sub.2Me 2-Me-Phenyl 977 3 CO.sub.2Me 2-Me-Phenyl 978 4 CO.sub.2Me 2-CN-Phenyl 979 1 CO.sub.2tBu 2-Me-Phenyl 980 2 CO.sub.2tBu 2-Me-Phenyl 981 3 CO.sub.2tBu 2-Me-Phenyl 982 4 CO.sub.2tBu 2-Me-Phenyl 983 1 CONHMe 2-Me-Phenyl 984 2 CONHMe 2-Me-Phenyl 985 3 CONHMe 2-Me-Phenyl 986 4 CONHMe 2-Me-Phenyl 987 1 SO.sub.2Me 2-Me-Phenyl 988 2 SO.sub.2Me 2-Me-Phenyl 989 3 SO.sub.2Me 2-Me-Phenyl 990 4 SO.sub.2Me 2-Me-Phenyl 991 1 SO.sub.2NH.sub.2 2-Me-Phenyl 992 2 SO.sub.2NH.sub.2 2-Me-Phenyl 993 3 SO.sub.2NH.sub.2 2-Me-Phenyl 994 4 SO.sub.2NH.sub.2 2-Me-Phenyl 995 1 H 4-Me-Phenyl 996 2 H 4-Me-Phenyl 997 3 H 4-Me-Phenyl 998 4 H 4-Me-Phenyl 999 1 Me 4-Me-Phenyl 1000 2 Me 4-Me-Phenyl 1001 3 Me 4-Me-Phenyl 1002 4 Me 4-Me-Phenyl 1003 1 CH.sub.2Ph 4-Me-Phenyl 1004 2 CH.sub.2Ph 4-Me-Phenyl 1005 3 CH.sub.2Ph 4-Me-Phenyl 1006 4 CH.sub.2Ph 4-Me-Phenyl 1007 1 COMe 4-Me-Phenyl 1008 2 COMe 4-Me-Phenyl 1009 3 COMe 4-Me-Phenyl 1010 4 COMe 4-Me-Phenyl 1011 1 CO.sub.2Me 4-Me-Phenyl 1012 2 CO.sub.2Me 4-Me-Phenyl 1013 3 CO.sub.2Me 4-Me-Phenyl 1014 4 CO.sub.2Me 4-Me-Phenyl 1015 1 CO.sub.2tBu 4-Me-Phenyl 1016 2 CO.sub.2tBu 4-Me-Phenyl 1017 3 CO.sub.2tBu 4-Me-Phenyl 1018 4 CO.sub.2tBu 4-Me-Phenyl 1019 1 CONHMe 4-Me-Phenyl 1020 2 CONHMe 4-Me-Phenyl 1021 3 CONHMe 4-Me-Phenyl 1022 4 CONHMe 4-Me-Phenyl 1023 1 SO.sub.2Me 4-Me-Phenyl 1024 2 SO.sub.2Me 4-Me-Phenyl 1025 3 SO.sub.2Me 4-Me-Phenyl 1026 4 SO.sub.2Me 4-Me-Phenyl 1027 1 SO.sub.2NH.sub.2 4-Me-Phenyl 1028 2 SO.sub.2NH.sub.2 4-Me-Phenyl 1029 3 SO.sub.2NH.sub.2 4-Me-Phenyl 1030 4 SO.sub.2NH.sub.2 4-Me-Phenyl 1031 1 H 3-F-Phenyl 1032 2 H 3-F-Phenyl 1033 3 H 3-F-Phenyl 1034 4 H 3-F-Phenyl 1035 1 Me 3-F-Phenyl 1036 2 Me 3-F-Phenyl 1037 3 Me 3-F-Phenyl 1038 4 Me 3-F-Phenyl 1039 1 CH.sub.2Ph 3-F-Phenyl 1040 2 CH.sub.2Ph 3-F-Phenyl 1041 3 CH.sub.2Ph 3-F-Phenyl 1042 4 CH.sub.2Ph 3-F-Phenyl 1043 1 COMe 3-F-Phenyl 1044 2 COMe 3-F-Phenyl 1045 3 COMe 3-F-Phenyl 1046 4 COMe 3-F-Phenyl 1047 1 CO.sub.2Me 3-F-Phenyl 1048 2 CO.sub.2Me 3-F-Phenyl 1049 3 CO.sub.2Me 3-F-Phenyl 1050 4 CO.sub.2Me 3-F-Phenyl 1051 1 CO.sub.2tBu 3-F-Phenyl 1052 2 CO.sub.2tBu 3-F-Phenyl 1053 3 CO.sub.2tBu 3-F-Phenyl 1054 4 CO.sub.2tBu 3-F-Phenyl 1055 1 CONHMe 3-F-Phenyl 1056 2 CONHMe 3-F-Phenyl 1057 3 CONHMe 3-F-Phenyl 1058 4 CONHMe 3-F-Phenyl 1059 1 SO.sub.2Me 3-F-Phenyl 1060 2 SO.sub.2Me 3-F-Phenyl 1061 3 SO.sub.2Me 3-F-Phenyl 1062 4 SO.sub.2Me 3-F-Phenyl 1063 1 SO.sub.2NH.sub.2 3-F-Phenyl 1064 2 SO.sub.2NH.sub.2 3-F-Phenyl 1065 3 SO.sub.2NH.sub.2 3-F-Phenyl 1066 4 SO.sub.2NH.sub.2 3-F-Phenyl 1067 1 H 2-Cl-Phenyl 1068 2 H 2-Cl-Phenyl 1069 3 H 2-Cl-Phenyl 1070 4 H 2-Cl-Phenyl 1071 1 Me 2-Cl-Phenyl 1072 2 Me 2-Cl-Phenyl 1073 3 Me 2-Cl-Phenyl 1074 4 Me 2-Cl-Phenyl 1075 1 CH.sub.2Ph 2-Cl-Phenyl 1076 2 CH.sub.2Ph 2-Cl-Phenyl 1077 3 CH.sub.2Ph 2-Cl-Phenyl 1078 4 CH.sub.2Ph 2-Cl-Phenyl 1079 1 COMe 2-Cl-Phenyl 1080 2 COMe 2-Cl-Phenyl 1081 3 COMe 2-Cl-Phenyl 1082 4 COMe 2-Cl-Phenyl 1083 1 CO.sub.2Me 2-Cl-Phenyl 1084 2 CO.sub.2Me 2-Cl-Phenyl 1085 3 CO.sub.2Me 2-Cl-Phenyl 1086 4 CO.sub.2Me 2-Cl-Phenyl 1087 1 CO.sub.2tBu 2-Cl-Phenyl 1088 2 CO.sub.2tBu 2-Cl-Phenyl 1089 3 CO.sub.2tBu 2-Cl-Phenyl 1090 4 CO.sub.2tBu 2-Cl-Phenyl 1091 1 CONHMe 2-Cl-Phenyl 1092 2 CONHMe 2-Cl-Phenyl 1093 3 CONHMe 2-Cl-Phenyl 1094 4 CONHMe 2-Cl-Phenyl 1095 1 SO.sub.2Me 2-Cl-Phenyl 1096 2 SO.sub.2Me 2-Cl-Phenyl 1097 3 SO.sub.2Me 2-Cl-Phenyl 1098 4 SO.sub.2Me 2-Cl-Phenyl 1099 1 SO.sub.2NH.sub.2 2-Cl-Phenyl 1100 2 SO.sub.2NH.sub.2 2-Cl-Phenyl 1101 3 SO.sub.2NH.sub.2 2-Cl-Phenyl 1102 4 SO.sub.2NH.sub.2 2-Cl-Phenyl 1103 1 H 4-Cl-Phenyl 1104 2 H 4-Cl-Phenyl 1105 3 H 4-Cl-Phenyl 1106 4 H 4-Cl-Phenyl 1107 1 Me 4-Cl-Phenyl 1108 2 Me 4-Cl-Phenyl 1109 3 Me 4-Cl-Phenyl 1110 4 Me 4-Cl-Phenyl 1111 1 CH.sub.2Ph 4-Cl-Phenyl 1112 2 CH.sub.2Ph 4-Cl-Phenyl 1113 3 CH.sub.2Ph 4-Cl-Phenyl 1114 4 CH.sub.2Ph 4-Cl-Phenyl 1115 1 COMe 4-Cl-Phenyl 1116 2 COMe 4-Cl-Phenyl 1117 3 COMe 4-Cl-Phenyl 1118 4 COMe 4-Cl-Phenyl 1119 1 CO.sub.2Me 4-Cl-Phenyl 1120 2 CO.sub.2Me 4-Cl-Phenyl 1121 3 CO.sub.2Me 4-Cl-Phenyl 1122 4 CO.sub.2Me 4-Cl-Phenyl 1123 1 CO.sub.2tBu 4-Cl-Phenyl 1124 2 CO.sub.2tBu 4-Cl-Phenyl 1125 3 CO.sub.2tBu 4-Cl-Phenyl 1126 4 CO.sub.2tBu 4-Cl-Phenyl 1127 1 CONHMe 4-Cl-Phenyl 1128 2 CONHMe 4-Cl-Phenyl 1129 3 CONHMe 4-Cl-Phenyl 1130 4 CONHMe 4-Cl-Phenyl 1131 1 SO.sub.2Me 4-Cl-Phenyl 1132 2 SO.sub.2Me 4-Cl-Phenyl 1133 3 SO.sub.2Me 4-Cl-Phenyl 1134 4 SO.sub.2Me 4-Cl-Phenyl 1135 1 SO.sub.2NH.sub.2 4-Cl-Phenyl 1136 2 SO.sub.2NH.sub.2 4-Cl-Phenyl 1137 3 SO.sub.2NH.sub.2 4-Cl-Phenyl 1138 4 SO.sub.2NH.sub.2 4-Cl-Phenyl 1139 1 H 3-Br-Phenyl 1140 2 H 3-Br-Phenyl 1141 3 H 3-Br-Phenyl 1142 4 H 3-Br-Phenyl 1143 1 Me 3-Br-Phenyl 1144 2 Me 3-Br-Phenyl 1145 3 Me 3-Br-Phenyl 1146 4 Me 3-Br-Phenyl 1147 1 CH.sub.2Ph 3-Br-Phenyl 1148 2 CH.sub.2Ph 3-Br-Phenyl 1149 3 CH.sub.2Ph 3-Br-Phenyl 1150 4 CH.sub.2Ph 3-Br-Phenyl 1151 1 COMe 3-Br-Phenyl 1152 2 COMe 3-Br-Phenyl 1153 3 COMe 3-Br-Phenyl 1154 4 COMe 3-Br-Phenyl 1155 1 CO.sub.2Me 3-Br-Phenyl 1156 2 CO.sub.2Me 3-Br-Phenyl 1157 3 CO.sub.2Me 3-Br-Phenyl 1158 4 CO.sub.2Me 3-Br-Phenyl 1159 1 CO.sub.2tBu 3-Br-Phenyl 1160 2 CO.sub.2tBu 3-Br-Phenyl 1161 3 CO.sub.2tBu 3-Br-Phenyl 1162 4 CO.sub.2tBu 3-Br-Phenyl 1163 1 CONHMe 3-Br-Phenyl 1164 2 CONHMe 3-Br-Phenyl 1165 3 CONHMe 3-Br-Phenyl 1166 4 CONHMe 3-Br-Phenyl 1167 1 SO.sub.2Me 3-Br-Phenyl 1168 2 SO.sub.2Me 3-Br-Phenyl 1169 3 SO.sub.2Me 3-Br-Phenyl 1170 4 SO.sub.2Me 3-Br-Phenyl 1171 1 SO.sub.2NH.sub.2 3-Br-Phenyl 1172 2 SO.sub.2NH.sub.2 3-Br-Phenyl 1173 3 SO.sub.2NH.sub.2 3-Br-Phenyl 1174 4 SO.sub.2NH.sub.2 3-Br-Phenyl 1175 1 H 2-CF.sub.3-Phenyl 1176 2 H 2-CF.sub.3-Phenyl 1177 3 H 2-CF.sub.3-Phenyl 1178 4 H 2-CF.sub.3-Phenyl 1179 1 Me 2-CF.sub.3-Phenyl 1180 2 Me 2-CF.sub.3-Phenyl 1181 3 Me 2-CF.sub.3-Phenyl 1182 4 Me 2-CF.sub.3-Phenyl 1183 1 CH.sub.2Ph 2-CF.sub.3-Phenyl 1184 2 CH.sub.2Ph 2-CF.sub.3-Phenyl 1185 3 CH.sub.2Ph 2-CF.sub.3-Phenyl 1186 4 CH.sub.2Ph 2-CF.sub.3-Phenyl 1187 1 COMe 2-CF.sub.3-Phenyl 1188 2 COMe 2-CF.sub.3-Phenyl 1189 3 COMe 2-CF.sub.3-Phenyl 1190 4 COMe 2-CF.sub.3-Phenyl 1191 1 CO.sub.2Me 2-CF.sub.3-Phenyl 1192 2 CO.sub.2Me 2-CF.sub.3-Phenyl 1193 3 CO.sub.2Me 2-CF.sub.3-Phenyl 1194 4 CO.sub.2Me 2-CF.sub.3-Phenyl 1195 1 CO.sub.2tBu 2-CF.sub.3-Phenyl 1196 2 CO.sub.2tBu 2-CF.sub.3-Phenyl 1197 3 CO.sub.2tBu 2-CF.sub.3-Phenyl 1198 4 CO.sub.2tBu 2-CF.sub.3-Phenyl 1199 1 CONHMe 2-CF.sub.3-Phenyl 1200 2 CONHMe 2-CF.sub.3-Phenyl 1201 3 CONHMe 2-CF.sub.3-Phenyl 1202 4 CONHMe 2-CF.sub.3-Phenyl 1203 1 SO.sub.2Me 2-CF.sub.3-Phenyl 1204 2 SO.sub.2Me 2-CF.sub.3-Phenyl 1205 3 SO.sub.2Me 2-CF.sub.3-Phenyl 1206 4 SO.sub.2Me 2-CF.sub.3-Phenyl 1207 1 SO.sub.2NH.sub.2 2-CF.sub.3-Phenyl 1208 2 SO.sub.2NH.sub.2 2-CF.sub.3-Phenyl 1209 3 SO.sub.2NH.sub.2 2-CF.sub.3-Phenyl 1210 4 SO.sub.2NH.sub.2 2-CF.sub.3-Phenyl 1211 1 H 4-CF.sub.3-Phenyl 1212 2 H 4-CF.sub.3-Phenyl 1213 3 H 4-CF.sub.3-Phenyl 1214 4 H 4-CF.sub.3-Phenyl 1215 1 Me 4-CF.sub.3-Phenyl 1216 2 Me 4-CF.sub.3-Phenyl 1217 3 Me 4-CF.sub.3-Phenyl 1218 4 Me 4-CF.sub.3-Phenyl 1219 1 CH.sub.2Ph 4-CF.sub.3-Phenyl 1220 2 CH.sub.2Ph 4-CF.sub.3-Phenyl 1221 3 CH.sub.2Ph 4-CF.sub.3-Phenyl 1222 4 CH.sub.2Ph 4-CF.sub.3-Phenyl 1223 1 COMe 4-CF.sub.3-Phenyl 1224 2 COMe 4-CF.sub.3-Phenyl 1225 3 COMe 4-CF.sub.3-Phenyl 1226 4 COMe 4-CF.sub.3-Phenyl 1227 1 CO.sub.2Me 4-CF.sub.3-Phenyl 1228 2 CO.sub.2Me 4-CF.sub.3-Phenyl 1229 3 CO.sub.2Me 4-CF.sub.3-Phenyl 1230 4 CO.sub.2Me 4-CF.sub.3-Phenyl 1231 1 CO.sub.2tBu 4-CF.sub.3-Phenyl 1232 2 CO.sub.2tBu 4-CF.sub.3-Phenyl 1233 3 CO.sub.2tBu 4-CF.sub.3-Phenyl 1234 4 CO.sub.2tBu 4-CF.sub.3-Phenyl 1235 1 CONHMe 4-CF.sub.3-Phenyl 1236 2 CONHMe 4-CF.sub.3-Phenyl 1237 3 CONHMe 4-CF.sub.3-Phenyl 1238 4 CONHMe 4-CF.sub.3-Phenyl 1239 1 SO.sub.2Me 4-CF.sub.3-Phenyl 1240 2 SO.sub.2Me 4-CF.sub.3-Phenyl 1241 3 SO.sub.2Me 4-CF.sub.3-Phenyl 1242 4 SO.sub.2Me 4-CF.sub.3-Phenyl 1243 1 SO.sub.2NH.sub.2 4-CF.sub.3-Phenyl 1244 2 SO.sub.2NH.sub.2 4-CF.sub.3-Phenyl 1245 3 SO.sub.2NH.sub.2 4-CF.sub.3-Phenyl 1246 4 SO.sub.2NH.sub.2 4-CF.sub.3-Phenyl 1247 1 H 3-iPr-Phenyl 1248 2 H 3-iPr-Phenyl 1249 3 H 3-iPr-Phenyl 1250 4 H 3-iPr-Phenyl 1251 1 Me 3-iPr-Phenyl 1252 2 Me 3-iPr-Phenyl 1253 3 Me 3-iPr-Phenyl 1254 4 Me 3-iPr-Phenyl 1255 1 CH.sub.2Ph 3-iPr-Phenyl 1256 2 CH.sub.2Ph 3-iPr-Phenyl 1257 3 CH.sub.2Ph 3-iPr-Phenyl 1258 4 CH.sub.2Ph 3-iPr-Phenyl 1259 1 COMe 3-iPr-Phenyl 1260 2 COMe 3-iPr-Phenyl 1261 3 COMe 3-iPr-Phenyl 1262 4 COMe 3-iPr-Phenyl 1263 1 CO.sub.2Me 3-iPr-Phenyl 1264 2 CO.sub.2Me 3-iPr-Phenyl 1265 3 CO.sub.2Me 3-iPr-Phenyl 1266 4 CO.sub.2Me 3-iPr-Phenyl 1267 1 CO.sub.2tBu 3-iPr-Phenyl 1268 2 CO.sub.2tBu 3-iPr-Phenyl 1269 3 CO.sub.2tBu 3-iPr-Phenyl 1270 4 CO.sub.2tBu 3-iPr-Phenyl 1271 1 CONHMe 3-iPr-Phenyl 1272 2 CONHMe 3-iPr-Phenyl 1273 3 CONHMe 3-iPr-Phenyl 1274 4 CONHMe 3-iPr-Phenyl 1275 1 SO.sub.2Me 3-iPr-Phenyl 1276 2 SO.sub.2Me 3-iPr-Phenyl 1277 3 SO.sub.2Me 3-iPr-Phenyl 1278 4 SO.sub.2Me 3-iPr-Phenyl 1279 1 SO.sub.2NH.sub.2 3-iPr-Phenyl 1280 2 SO.sub.2NH.sub.2 3-iPr-Phenyl 1281 3 SO.sub.2NH.sub.2 3-iPr-Phenyl 1282 4 SO.sub.2NH.sub.2 3-iPr-Phenyl 1283 1 H 4-NH.sub.2-Phenyl 1284 2 H 4-NH.sub.2-Phenyl 1285 3 H 4-NH.sub.2-Phenyl 1286 4 H 4-NH.sub.2-Phenyl 1287 1 Me 4-NH.sub.2-Phenyl 1288 2 Me 4-NH.sub.2-Phenyl 1289 3 Me 4-NH.sub.2-Phenyl 1290 4 Me 4-NH.sub.2-Phenyl 1291 1 CH.sub.2Ph 4-NH.sub.2-Phenyl 1292 2 CH.sub.2Ph 4-NH.sub.2-Phenyl 1293 3 CH.sub.2Ph 4-NH.sub.2-Phenyl 1294 4 CH.sub.2Ph 4-NH.sub.2-Phenyl 1295 1 COMe 4-NH.sub.2-Phenyl 1296 2 COMe 4-NH.sub.2-Phenyl 1297 3 COMe 4-NH.sub.2-Phenyl 1298 4 COMe 4-NH.sub.2-Phenyl 1299 1 CO.sub.2Me 4-NH.sub.2-Phenyl 1300 2 CO.sub.2Me 4-NH.sub.2-Phenyl 1301 3 CO.sub.2Me 4-NH.sub.2-Phenyl 1302 4 CO.sub.2Me 4-NH.sub.2-Phenyl 1303 1 CO.sub.2tBu 4-NH.sub.2-Phenyl 1304 2 CO.sub.2tBu 4-NH.sub.2-Phenyl 1305 3 CO.sub.2tBu 4-NH.sub.2-Phenyl 1306 4 CO.sub.2tBu 4-NH.sub.2-Phenyl 1307 1 CONHMe 4-NH.sub.2-Phenyl 1308 2 CONHMe 4-NH.sub.2-Phenyl 1309 3 CONHMe 4-NH.sub.2-Phenyl 1310 4 CONHMe 4-NH.sub.2-Phenyl 1311 1 SO.sub.2Me 4-NH.sub.2-Phenyl 1312 2 SO.sub.2Me 4-NH.sub.2-Phenyl 1313 3 SO.sub.2Me 4-NH.sub.2-Phenyl 1314 4 SO.sub.2Me 4-NH.sub.2-Phenyl 1315 1 SO.sub.2NH.sub.2 4-NH.sub.2-Phenyl 1316 2 SO.sub.2NH.sub.2 4-NH.sub.2-Phenyl 1317 3 SO.sub.2NH.sub.2 4-NH.sub.2-Phenyl 1318 4 SO.sub.2NH.sub.2 4-NH.sub.2-Phenyl 1319 1 H 2-NH.sub.2-Phenyl 1320 2 H 2-NH.sub.2-Phenyl 1321 3 H 2-NH.sub.2-Phenyl 1322 4 H 2-NH.sub.2-Phenyl 1323 1 Me 2-NH.sub.2-Phenyl 1324 2 Me 2-NH.sub.2-Phenyl 1325 3 Me 2-NH.sub.2-Phenyl 1326 4 Me 2-NH.sub.2-Phenyl 1327 1 CH.sub.2Ph 2-NH.sub.2-Phenyl 1328 2 CH.sub.2Ph 2-NH.sub.2-Phenyl 1329 3 CH.sub.2Ph 2-NH.sub.2-Phenyl 1330 4 CH.sub.2Ph 2-NH.sub.2-Phenyl 1331 1 COMe 2-NH.sub.2-Phenyl 1332 2 COMe 2-NH.sub.2-Phenyl 1333 3 COMe 2-NH.sub.2-Phenyl 1334 4 COMe 2-NH.sub.2-Phenyl 1335 1 CO.sub.2Me 2-NH.sub.2-Phenyl 1336 2 CO.sub.2Me 2-NH.sub.2-Phenyl 1337 3 CO.sub.2Me 2-NH.sub.2-Phenyl 1338 4 CO.sub.2Me 2-NH.sub.2-Phenyl 1339 1 CO.sub.2tBu 2-NH.sub.2-Phenyl 1340 2 CO.sub.2tBu 2-NH.sub.2-Phenyl 1341 3 CO.sub.2tBu 2-NH.sub.2-Phenyl 1342 4 CO.sub.2tBu 2-NH.sub.2-Phenyl 1343 1 CONHMe 2-NH.sub.2-Phenyl 1344 2 CONHMe 2-NH.sub.2-Phenyl 1345 3 CONHMe 2-NH.sub.2-Phenyl 1346 4 CONHMe 2-NH.sub.2-Phenyl 1347 1 SO.sub.2Me 2-NH.sub.2-Phenyl 1348 2 SO.sub.2Me 2-NH.sub.2-Phenyl 1349 3 SO.sub.2Me 2-NH.sub.2-Phenyl 1350 4 SO.sub.2Me 2-NH.sub.2-Phenyl 1351 1 SO2NH2 2-NH.sub.2-Phenyl 1352 2 SO.sub.2NH.sub.2 2-NH.sub.2-Phenyl 1353 3 SO.sub.2NH.sub.2 2-NH.sub.2-Phenyl 1354 4 SO.sub.2NH.sub.2 2-NH.sub.2-Phenyl 1355 1 H 2,6-di-Me-Phenyl 1356 2 H 2,6-di-Me-Phenyl 1357 3 H 2,6-di-Me-Phenyl 1358 4 H 2,6-di-Me-Phenyl 1359 1 Me 2,6-di-Me-Phenyl 1360 2 Me 2,6-di-Me-Phenyl 1361 3 Me 2,6-di-Me-Phenyl 1362 4 Me 2,6-di-Me-Phenyl 1363 1 CH.sub.2Ph 2,6-di-Me-Phenyl 1364 2 CH.sub.2Ph 2,6-di-Me-Phenyl 1365 3 CH.sub.2Ph 2,6-di-Me-Phenyl 1366 4 CH.sub.2Ph 2,6-di-Me-Phenyl 1367 1 COMe 2,6-di-Me-Phenyl 1368 2 COMe 2,6-di-Me-Phenyl 1369 3 COMe 2,6-di-Me-Phenyl 1370 4 COMe 2,6-di-Me-Phenyl 1371 1 CO.sub.2Me 2,6-di-Me-Phenyl 1372 2 CO.sub.2Me 2,6-di-Me-Phenyl 1373 3 CO.sub.2Me 2,6-di-Me-Phenyl 1374 4 CO.sub.2Me 2,6-di-Me-Phenyl 1375 1 CO.sub.2tBu 2,6-di-Me-Phenyl 1376 2 CO.sub.2tBu 2,6-di-Me-Phenyl 1377 3 CO.sub.2tBu 2,6-di-Me-Phenyl 1378 4 CO.sub.2tBu 2,6-di-Me-Phenyl 1379 1 CONHMe 2,6-di-Me-Phenyl 1380 2 CONHMe 2,6-di-Me-Phenyl 1381 3 CONHMe 2,6-di-Me-Phenyl 1382 4 CONHMe 2,6-di-Me-Phenyl 1383 1 SO.sub.2Me 2,6-di-Me-Phenyl 1384 2 SO.sub.2Me 2,6-di-Me-Phenyl 1385 3 SO.sub.2Me 2,6-di-Me-Phenyl 1386 4 SO.sub.2Me 2,6-di-Me-Phenyl 1387 1 SO.sub.2NH.sub.2 2,6-di-Me-Phenyl 1388 2 SO.sub.2NH.sub.2 2,6-di-Me-Phenyl 1389 3 SO.sub.2NH.sub.2 2,6-di-Me-Phenyl 1390 4 SO.sub.2NH.sub.2 2,6-di-Me-Phenyl 1391 1 H 2-Ph-Phenyl 1392 2 H 2-Ph-Phenyl 1393 3 H 2-Ph-Phenyl 1394 4 H 2-Ph-Phenyl 1395 1 Me 2-Ph-Phenyl 1396 2 Me 2-Ph-Phenyl 1397 3 Me 2-Ph-Phenyl 1398 4 Me 2-Ph-Phenyl 1399 1 CH.sub.2Ph 2-Ph-Phenyl 1400 2 CH.sub.2Ph 2-Ph-Phenyl 1401 3 CH.sub.2Ph 2-Ph-Phenyl 1402 4 CH.sub.2Ph 2-Ph-Phenyl 1403 1 COMe 2-Ph-Phenyl 1404 2 COMe 2-Ph-Phenyl 1405 3 COMe 2-Ph-Phenyl 1406 4 COMe 2-Ph-Phenyl 1407 1 CO.sub.2Me 2-Ph-Phenyl 1408 2 CO.sub.2Me 2-Ph-Phenyl 1409 3 CO.sub.2Me 2-Ph-Phenyl 1410 4 CO.sub.2Me 2-Ph-Phenyl 1411 1 CO.sub.2tBu 2-Ph-Phenyl 1412 2 CO.sub.2tBu 2-Ph-Phenyl 1413 3 CO.sub.2tBu 2-Ph-Phenyl 1414 4 CO.sub.2tBu 2-Ph-Phenyl 1415 1 CONHMe 2-Ph-Phenyl 1416 2 CONHMe 2-Ph-Phenyl 1417 3 CONHMe 2-Ph-Phenyl 1418 4 CONHMe 2-Ph-Phenyl 1419 1 SO.sub.2Me 2-Ph-Phenyl 1420 2 SO.sub.2Me 2-Ph-Phenyl 1421 3 SO.sub.2Me 2-Ph-Phenyl 1422 4 SO.sub.2Me 2-Ph-Phenyl 1423 1 SO.sub.2NH.sub.2 2-Ph-Phenyl 1424 2 SO.sub.2NH.sub.2 2-Ph-Phenyl 1425 3 SO.sub.2NH.sub.2 2-Ph-Phenyl 1426 4 SO.sub.2NH.sub.2 2-Ph-Phenyl 1427 1 H 4-Ph-Phenyl 1428 2 H 4-Ph-Phenyl 1429 3 H 4-Ph-Phenyl 1430 4 H 4-Ph-Phenyl 1431 1 Me 4-Ph-Phenyl 1432 2 Me 4-Ph-Phenyl 1433 3 Me 4-Ph-Phenyl 1434 4 Me 4-Ph-Phenyl 1435 1 CH.sub.2Ph 4-Ph-Phenyl 1436 2 CH.sub.2Ph 4-Ph-Phenyl 1437 3 CH.sub.2Ph 4-Ph-Phenyl 1438 4 CH.sub.2Ph 4-Ph-Phenyl 1439 1 COMe 4-Ph-Phenyl 1440 2 COMe 4-Ph-Phenyl 1441 3 COMe 4-Ph-Phenyl 1442 4 COMe 4-Ph-Phenyl 1443 1 CO.sub.2Me 4-Ph-Phenyl 1444 2 CO.sub.2Me 4-Ph-Phenyl 1445 3 CO.sub.2Me 4-Ph-Phenyl 1446 4 CO.sub.2Me 4-Ph-Phenyl 1447 1 CO.sub.2tBu 4-Ph-Phenyl 1448 2 CO.sub.2tBu 4-Ph-Phenyl 1449 3 CO.sub.2tBu 4-Ph-Phenyl 1450 4 CO.sub.2tBu 4-Ph-Phenyl 1451 1 CONHMe 4-Ph-Phenyl 1452 2 CONHMe 4-Ph-Phenyl 1453 3 CONHMe 4-Ph-Phenyl 1454 4 CONHMe 4-Ph-Phenyl 1455 1 SO.sub.2Me 4-Ph-Phenyl 1456 2 SO.sub.2Me 4-Ph-Phenyl 1457 3 SO.sub.2Me 4-Ph-Phenyl 1458 4 SO.sub.2Me 4-Ph-Phenyl 1459 1 SO.sub.2NH.sub.2 4-Ph-Phenyl 1460 2 SO.sub.2NH.sub.2 4-Ph-Phenyl 1461 3 SO.sub.2NH.sub.2 4-Ph-Phenyl 1462 4 SO.sub.2NH.sub.2 4-Ph-Phenyl 1463 1 H 3-morpholino- phenyl 1464 2 H 3-morpholino- phenyl 1465 3 H 3-morpholino- phenyl 1466 4 H 3-morpholino- phenyl 1467 1 Me 3-morpholino- phenyl 1468 2 Me 3-morpholino- phenyl 1469 3 Me 3-morpholino- phenyl 1470 4 Me 3-morpholino- phenyl 1471 1 CH.sub.2Ph 3-morpholino- phenyl 1472 2 CH.sub.2Ph 3-morpholino- phenyl 1473 3 CH.sub.2Ph 3-morpholino- phenyl 1474 4 CH.sub.2Ph 3-morpholino- phenyl 1475 1 COMe 3-morpholino- phenyl 1476 2 COMe 3-morpholino- phenyl 1477 3 COMe 3-morpholino- phenyl 1478 4 COMe 3-morpholino- phenyl 1479 1 CO.sub.2Me 3-morpholino- phenyl 1480 2 CO.sub.2Me 3-morpholino- phenyl 1481 3 CO.sub.2Me 3-morpholino- phenyl 1482 4 CO.sub.2Me 3-morpholino- phenyl 1483 1 CO.sub.2tBu 3-morpholino- phenyl 1484 2 CO.sub.2tBu 3-morpholino- phenyl 1485 3 CO.sub.2tBu 3-morpholino- phenyl 1486 4 CO.sub.2tBu 3-morpholino- phenyl 1487 1 CONHMe 3-morpholino- phenyl 1488 2 CONHMe 3-morpholino- phenyl 1489 3 CONHMe 3-morpholino- phenyl 1490 4 CONHMe 3-morpholino- phenyl 1491 1 SO.sub.2Me 3-morpholino- phenyl 1492 2 SO.sub.2Me 3-morpholino- phenyl 1493 3 SO.sub.2Me 3-morpholino- phenyl 1494 4 SO.sub.2Me 3-morpholino- phenyl 1495 1 SO.sub.2NH.sub.2 3-morpholino- phenyl 1496 2 SO.sub.2NH.sub.2 3-morpholino- phenyl 1497 3 SO.sub.2NH.sub.2 3-morpholino- phenyl 1498 4 SO.sub.2NH.sub.2 3-morpholino- phenyl 1499 1 Me 4-morpholino- phenyl 1500 2 Me 4-morpholino- phenyl 1501 3 Me 4-morpholino- phenyl 1502 4 Me 4-morpholino- phenyl 103 1 COMe 4-morpholino- phenyl 1504 2 COMe 4-morpholino- phenyl 1505 3 COMe 4-morpholino- phenyl 1506 4 COMe 4-morpholino- phenyl 1507 1 CO.sub.2tBu 4-morpholino- phenyl 1508 2 CO.sub.2tBu 4-morpholino- phenyl 1509 3 CO.sub.2tBu 4-morpholino- phenyl 1510 4 CO.sub.2tBu 4-morpholino- phenyl 1511 1 SO.sub.2Me 4-morpholino- phenyl 1512 2 SO.sub.2Me 4-morpholino- phenyl 1513 3 SO.sub.2Me 4-morpholino- phenyl 1514 4 SO.sub.2Me 4-morpholino- phenyl 1516 1 H naphthylen-2-yl 1517 2 H naphthylen-2-yl 1518 3 H naphthylen-2-yl 1519 4 H naphthylen-2-yl 1520 1 Me naphthylen-2-yl 1521 2 Me naphthylen-2-yl 1522 3 Me naphthylen-2-yl 1523 4 Me naphthylen-2-yl 1524 1 CH.sub.2Ph naphthylen-2-yl 1525 2 CH.sub.2Ph naphthylen-2-yl 1526 3 CH.sub.2Ph naphthylen-2-yl 1527 4 CH.sub.2Ph naphthylen-2-yl 1528 1 COMe naphthylen-2-yl 1529 2 COMe naphthylen-2-yl 1530 3 COMe naphthylen-2-yl 1531 4 COMe naphthylen-2-yl 1532 1 CO.sub.2Me naphthylen-2-yl 1533 2 CO.sub.2Me naphthylen-2-yl 1534 3 CO.sub.2Me naphthylen-2-yl 1535 4 CO.sub.2Me naphthylen-2-yl 1536 1 CO.sub.2tBu naphthylen-2-yl 1537 2 CO.sub.2tBu naphthylen-2-yl 1538 3 CO.sub.2tBu naphthylen-2-yl 1539 4 CO.sub.2tBu naphthylen-2-yl 1540 1 CONHMe naphthylen-2-yl 1541 2 CONHMe naphthylen-2-yl 1542 3 CONHMe naphthylen-2-yl 1543 4 CONHMe naphthylen-2-yl 1544 1 SO.sub.2Me naphthylen-2-yl 1545 2 SO.sub.2Me naphthylen-2-yl 1546 3 SO.sub.2Me naphthylen-2-yl 1547 4 SO.sub.2Me naphthylen-2-yl 1548 1 SO.sub.2NH.sub.2 naphthylen-2-yl 1549 2 SO.sub.2NH.sub.2 naphthylen-2-yl 1550 3 SO.sub.2NH.sub.2 naphthylen-2-yl 1551 4 SO.sub.2NH.sub.2 naphthylen-2-yl

    [2030] Exemplary embodiments include compounds having the formula (XXV)

    ##STR00440##

    [2031] or a pharmaceutically acceptable salt form thereof defined herein below in Table 19.

    TABLE-US-00019 TABLE 19 Entry n R.sup.7 R.sup.20a R.sup.20b R.sup.20c R.sup.20d 1 1 H H H H H 2 2 H H H H H 3 3 H H H H H 4 4 H H H H H 5 1 Me H H H H 6 2 Me H H H H 7 3 Me H H H H 8 4 Me H H H H 9 1 CH.sub.2Ph H H H H 10 2 CH.sub.2Ph H H H H 11 3 CH.sub.2Ph H H H H 12 4 CH.sub.2Ph H H H H 13 1 COMe H H H H 14 2 COMe H H H H 15 3 COMe H H H H 16 4 COMe H H H H 17 1 CO.sub.2Me H H H H 18 2 CO.sub.2Me H H H H 19 3 CO.sub.2Me H H H H 20 4 CO.sub.2Me H H H H 21 1 CO.sub.2tBu H H H H 22 2 CO.sub.2tBu H H H H 23 3 CO.sub.2tBu H H H H 24 4 CO.sub.2tBu H H H H 25 1 CONHMe H H H H 26 2 CONHMe H H H H 27 3 CONHMe H H H H 28 4 CONHMe H H H H 29 1 SO.sub.2Me H H H H 30 2 SO.sub.2Me H H H H 31 3 SO.sub.2Me H H H H 32 4 SO.sub.2Me H H H H 33 1 SO.sub.2NH.sub.2 H H H H 34 2 SO.sub.2NH.sub.2 H H H H 35 3 SO.sub.2NH.sub.2 H H H H 36 4 SO.sub.2NH.sub.2 H H H H 37 1 H H H OH H 38 2 H H H OH H 39 3 H H H OH H 40 4 H H H OH H 41 1 Me H H OH H 42 2 Me H H OH H 43 3 Me H H OH H 44 4 Me H H OH H 45 1 CH.sub.2Ph H H OH H 46 2 CH.sub.2Ph H H OH H 47 3 CH.sub.2Ph H H OH H 48 4 CH.sub.2Ph H H OH H 49 1 COMe H H OH H 50 2 COMe H H OH H 51 3 COMe H H OH H 52 4 COMe H H OH H 53 1 CO.sub.2Me H H OH H 54 2 CO.sub.2Me H H OH H 55 3 CO.sub.2Me H H OH H 56 4 CO.sub.2Me H H OH H 57 1 CO.sub.2tBu H H OH H 58 2 CO.sub.2tBu H H OH H 59 3 CO.sub.2tBu H H OH H 60 4 CO.sub.2tBu H H OH H 61 1 CONHMe H H OH H 62 2 CONHMe H H OH H 63 3 CONHMe H H OH H 64 4 CONHMe H H OH H 65 1 SO.sub.2Me H H OH H 66 2 SO.sub.2Me H H OH H 67 3 SO.sub.2Me H H OH H 68 4 SO.sub.2Me H H OH H 69 1 SO.sub.2NH.sub.2 H H OH H 70 2 SO.sub.2NH.sub.2 H H OH H 71 3 SO.sub.2NH.sub.2 H H OH H 72 4 SO.sub.2NH.sub.2 H H OH H 73 1 H H H OMe H 74 2 H H H OMe H 75 3 H H H OMe H 76 4 H H H OMe H 77 1 Me H H OMe H 78 2 Me H H OMe H 79 3 Me H H OMe H 80 4 Me H H OMe H 81 1 CH.sub.2Ph H H OMe H 82 2 CH.sub.2Ph H H OMe H 83 3 CH.sub.2Ph H H OMe H 84 4 CH.sub.2Ph H H OMe H 85 1 COMe H H OMe H 86 2 COMe H H OMe H 87 3 COMe H H OMe H 88 4 COMe H H OMe H 89 1 CO.sub.2Me H H OMe H 90 2 CO.sub.2Me H H OMe H 91 3 CO.sub.2Me H H OMe H 92 4 CO.sub.2Me H H OMe H 93 1 CO.sub.2tBu H H OMe H 94 2 CO.sub.2tBu H H OMe H 95 3 CO.sub.2tBu H H OMe H 96 1 CO.sub.2tBu H H OMe H 97 1 CONHMe H H OMe H 98 2 CONHMe H H OMe H 99 3 CONHMe H H OMe H 100 4 CONHMe H H OMe H 101 1 SO.sub.2Me H H OMe H 102 2 SO.sub.2Me H H OMe H 103 3 SO.sub.2Me H H OMe H 104 4 SO.sub.2Me H H OMe H 105 1 SO.sub.2NH.sub.2 H H OMe H 106 2 SO.sub.2NH.sub.2 H H OMe H 107 3 SO.sub.2NH.sub.2 H H OMe H 108 4 SO.sub.2NH.sub.2 H H OMe H 109 1 H H H Me H 110 2 H H H Me H 111 3 H H H Me H 112 4 H H H Me H 113 1 Me H H Me H 114 2 Me H H Me H 115 3 Me H H Me H 116 4 Me H H Me H 117 1 CH.sub.2Ph H H Me H 118 2 CH.sub.2Ph H H Me H 119 3 CH.sub.2Ph H H Me H 120 4 CH.sub.2Ph H H Me H 121 1 COMe H H Me H 122 2 COMe H H Me H 123 3 COMe H H Me H 124 4 COMe H H Me H 125 1 CO.sub.2Me H H Me H 126 2 CO.sub.2Me H H Me H 127 3 CO.sub.2Me H H Me H 128 4 CO.sub.2Me H H Me H 129 1 CO.sub.2tBu H H Me H 130 2 CO.sub.2tBu H H Me H 131 3 CO.sub.2tBu H H Me H 132 4 CO.sub.2tBu H H Me H 133 1 CONHMe H H Me H 134 2 CONHMe H H Me H 135 3 CONHMe H H Me H 136 4 CONHMe H H Me H 137 1 SO.sub.2Me H H Me H 138 2 SO.sub.2Me H H Me H 139 3 SO2Me H H Me H 140 4 SO.sub.2Me H H Me H 141 1 SO.sub.2NH.sub.2 H H Me H 142 2 SO.sub.2NH.sub.2 H H Me H 143 3 SO.sub.2NH.sub.2 H H Me H 144 4 SO.sub.2NH.sub.2 H H Me H 145 1 H H H CF.sub.3 H 146 2 H H H CF.sub.3 H 147 3 H H H CF.sub.3 H 148 4 H H H CF.sub.3 H 149 1 Me H H CF.sub.3 H 150 2 Me H H CF.sub.3 H 151 3 Me H H CF.sub.3 H 152 4 Me H H CF.sub.3 H 153 1 CH.sub.2Ph H H CF.sub.3 H 154 2 CH.sub.2Ph H H CF.sub.3 H 155 3 CH.sub.2Ph H H CF.sub.3 H 156 4 CH.sub.2Ph H H CF.sub.3 H 157 1 COMe H H CF.sub.3 H 158 2 COMe H H CF.sub.3 H 159 3 COMe H H CF.sub.3 H 160 4 COMe H H CF.sub.3 H 161 1 CO.sub.2Me H H CF.sub.3 H 162 2 CO.sub.2Me H H CF.sub.3 H 163 3 CO.sub.2Me H H CF.sub.3 H 164 4 CO.sub.2Me H H CF.sub.3 H 165 1 CO.sub.2tBu H H CF.sub.3 H 166 2 CO.sub.2tBu H H CF.sub.3 H 167 3 CO.sub.2tBu H H CF.sub.3 H 168 4 CO.sub.2tBu H H CF.sub.3 H 169 1 CONHMe H H CF.sub.3 H 170 2 CONHMe H H CF.sub.3 H 171 3 CONHMe H H CF.sub.3 H 172 4 CONHMe H H CF.sub.3 H 173 1 SO.sub.2Me H H CF.sub.3 H 174 2 SO.sub.2Me H H CF.sub.3 H 175 3 SO.sub.2Me H H CF.sub.3 H 176 4 SO.sub.2Me H H CF.sub.3 H 177 1 SO.sub.2NH.sub.2 H H CF.sub.3 H 178 2 SO.sub.2NH.sub.2 H H CF.sub.3 H 179 3 SO.sub.2NH.sub.2 H H CF.sub.3 H 180 4 SO.sub.2NH.sub.2 H H CF.sub.3 H 181 1 H H H F H 182 2 H H H F H 183 3 H H H F H 184 4 H H H F H 185 1 Me H H F H 186 2 Me H H F H 187 3 Me H H F H 188 4 Me H H F H 189 1 CH.sub.2Ph H H F H 190 2 CH.sub.2Ph H H F H 191 3 CH.sub.2Ph H H F H 192 4 CH.sub.2Ph H H F H 193 1 COMe H H F H 194 2 COMe H H F H 195 3 COMe H H F H 196 4 COMe H H F H 197 1 CO.sub.2Me H H F H 198 2 CO.sub.2Me H H F H 199 3 CO.sub.2Me H H F H 200 4 CO.sub.2Me H H F H 201 1 CO.sub.2tBu H H F H 202 2 CO.sub.2tBu H H F H 203 3 CO.sub.2tBu H H F H 204 4 CO.sub.2tBu H H F H 205 1 CONHMe H H F H 206 2 CONHMe H H F H 207 3 CONHMe H H F H 208 4 CONHMe H H F H 209 1 SO.sub.2Me H H F H 210 2 SO.sub.2Me H H F H 211 3 SO.sub.2Me H H F H 212 4 SO.sub.2Me H H F H 213 1 SO.sub.2NH.sub.2 H H F H 214 2 SO.sub.2NH.sub.2 H H F H 215 3 SO.sub.2NH.sub.2 H H F H 216 4 SO.sub.2NH.sub.2 H H F H 217 1 H H H Cl H 218 2 H H H Cl H 219 3 H H H Cl H 220 4 H H H Cl H 221 1 Me H H Cl H 222 2 Me H H Cl H 223 3 Me H H Cl H 224 4 Me H H Cl H 225 1 CH.sub.2Ph H H Cl H 226 2 CH.sub.2Ph H H Cl H 227 3 CH.sub.2Ph H H Cl H 228 4 CH.sub.2Ph H H Cl H 229 1 COMe H H Cl H 230 2 COMe H H Cl H 231 3 COMe H H Cl H 232 4 COMe H H Cl H 233 1 CO.sub.2Me H H Cl H 234 2 CO.sub.2Me H H Cl H 235 3 CO.sub.2Me H H Cl H 236 4 CO.sub.2Me H H Cl H 237 1 CO.sub.2tBu H H Cl H 238 2 CO.sub.2tBu H H Cl H 239 3 CO.sub.2tBu H H Cl H 240 4 CO.sub.2tBu H H Cl H 241 1 CONHMe H H Cl H 242 2 CONHMe H H Cl H 243 3 CONHMe H H Cl H 244 4 CONHMe H H Cl H 245 1 SO.sub.2Me H H Cl H 246 2 SO.sub.2Me H H Cl H 247 3 SO.sub.2Me H H Cl H 248 4 SO.sub.2Me H H Cl H 249 1 SO.sub.2NH.sub.2 H H Cl H 250 2 SO.sub.2NH.sub.2 H H Cl H 251 3 SO.sub.2NH.sub.2 H H Cl H 252 4 SO.sub.2NH.sub.2 H H Cl H 253 1 H H H CN H 254 2 H H H CN H 255 3 H H H CN H 256 4 H H H CN H 257 1 Me H H CN H 258 2 Me H H CN H 259 3 Me H H CN H 260 4 Me H H CN H 261 1 v H H CN H 262 2 CH.sub.2Ph H H CN H 263 3 CH.sub.2Ph H H CN H 264 4 CH.sub.2Ph H H CN H 265 1 CH.sub.2Ph H H CN H 266 2 COMe H H CN H 267 3 COMe H H CN H 268 4 COMe H H CN H 269 1 COMe H H CN H 270 2 CO.sub.2Me H H CN H 271 3 CO.sub.2Me H H CN H 272 4 CO.sub.2Me H H CN H 273 1 CO.sub.2Me H H CN H 274 2 CO.sub.2tBu H H CN H 275 3 CO.sub.2tBu H H CN H 276 4 CO.sub.2tBu H H CN H 277 1 CO.sub.2tBu H H CN H 278 2 CONHMe H H CN H 279 3 CONHMe H H CN H 280 4 CONHMe H H CN H 281 1 CONHMe H H CN H 282 2 SO.sub.2Me H H CN H 283 3 SO.sub.2Me H H CN H 284 4 SO.sub.2Me H H CN H 285 1 SO.sub.2Me H H CN H 286 2 SO.sub.2NH.sub.2 H H CN H 287 3 SO.sub.2NH.sub.2 H H CN H 288 4 SO.sub.2NH.sub.2 H H CN H 289 1 SO.sub.2NH.sub.2 H OH H H 290 2 H H OH H H 291 3 H H OH H H 292 4 H H OH H H 293 1 Me H OH H H 294 2 Me H OH H H 295 3 Me H OH H H 296 4 Me H OH H H 297 1 CH.sub.2Ph H OH H H 298 2 CH.sub.2Ph H OH H H 299 3 CH.sub.2Ph H OH H H 300 4 CH.sub.2Ph H OH H H 301 1 COMe H OH H H 302 2 COMe H OH H H 303 3 COMe H OH H H 304 4 COMe H OH H H 305 1 CO.sub.2Me H OH H H 306 2 CO.sub.2Me H OH H H 307 3 CO.sub.2Me H OH H H 308 4 CO.sub.2Me H OH H H 309 1 CO.sub.2tBu H OH H H 310 2 CO.sub.2tBu H OH H H 311 3 CO.sub.2tBu H OH H H 312 4 CO.sub.2tBu H OH H H 313 1 CONHMe H OH H H 314 2 CONHMe H OH H H 315 3 CONHMe H OH H H 316 4 CONHMe H OH H H 317 1 SO.sub.2Me H OH H H 318 2 SO.sub.2Me H OH H H 319 3 SO.sub.2Me H OH H H 320 4 SO.sub.2Me H OH H H 321 1 SO.sub.2NH.sub.2 H OH H H 322 2 SO.sub.2NH.sub.2 H OH H H 323 3 SO.sub.2NH.sub.2 H OH H H 324 4 SO.sub.2NH.sub.2 H OH H H 325 1 H H OMe H H 326 2 H H OMe H H 327 3 H H OMe H H 328 4 H H OMe H H 329 1 Me H OMe H H 330 2 Me H OMe H H 331 3 Me H OMe H H 332 4 Me H OMe H H 333 1 CH.sub.2Ph H OMe H H 334 2 CH.sub.2Ph H OMe H H 335 3 CH.sub.2Ph H OMe H H 336 4 CH.sub.2Ph H OMe H H 337 1 COMe H OMe H H 338 2 COMe H OMe H H 339 3 COMe H OMe H H 340 4 COMe H OMe H H 341 1 CO.sub.2Me H OMe H H 342 2 CO.sub.2Me H OMe H H 343 3 CO.sub.2Me H OMe H H 344 4 CO.sub.2Me H OMe H H 345 1 CO.sub.2tBu H OMe H H 346 2 CO.sub.2tBu H OMe H H 347 3 CO.sub.2tBu H OMe H H 348 4 CO.sub.2tBu H OMe H H 349 1 CONHMe H OMe H H 350 2 CONHMe H OMe H H 351 3 CONHMe H OMe H H 352 4 CONHMe H OMe H H 353 1 SO.sub.2Me H OMe H H 354 2 SO.sub.2Me H OMe H H 355 3 SO.sub.2Me H OMe H H 356 4 SO.sub.2Me H OMe H H 357 1 SO.sub.2NH.sub.2 H OMe H H 358 2 SO.sub.2NH.sub.2 H OMe H H 359 3 SO.sub.2NH.sub.2 H OMe H H 360 4 SO.sub.2NH.sub.2 H OMe H H 361 1 H H Me H H 362 2 H H Me H H 363 3 H H Me H H 364 4 H H Me H H 365 1 Me H Me H H 366 2 Me H Me H H 367 3 Me H Me H H 368 4 Me H Me H H 369 1 CH.sub.2Ph H Me H H 370 2 CH.sub.2Ph H Me H H 371 3 CH.sub.2Ph H Me H H 372 4 CH.sub.2Ph H Me H H 373 1 COMe H Me H H 374 2 COMe H Me H H 375 3 COMe H Me H H 376 4 COMe H Me H H 377 1 CO.sub.2Me H Me H H 378 2 CO.sub.2Me H Me H H 379 3 CO.sub.2Me H Me H H 380 4 CO.sub.2Me H Me H H 381 1 CO.sub.2tBu H Me H H 382 2 CO.sub.2tBu H Me H H 383 3 CO.sub.2tBu H Me H H 384 4 CO.sub.2tBu H Me H H 385 1 CONHMe H Me H H 386 2 CONHMe H Me H H 387 3 CONHMe H Me H H 388 4 CONHMe H Me H H 389 1 SO.sub.2Me H Me H H 390 2 SO.sub.2Me H Me H H 391 3 SO.sub.2Me H Me H H 392 4 SO.sub.2Me H Me H H 393 1 SO.sub.2NH.sub.2 H Me H H 394 2 SO.sub.2NH.sub.2 H Me H H 395 3 SO.sub.2NH.sub.2 H Me H H 396 4 SO.sub.2NH.sub.2 H Me H H 397 1 H H CF.sub.3 H H 398 2 H H CF.sub.3 H H 399 3 H H CF.sub.3 H H 400 4 H H CF.sub.3 H H 401 1 Me H CF.sub.3 H H 402 2 Me H CF.sub.3 H H 403 3 Me H CF.sub.3 H H 404 4 Me H CF.sub.3 H H 405 1 CH.sub.2Ph H CF.sub.3 H H 406 2 CH.sub.2Ph H CF.sub.3 H H 407 3 CH.sub.2Ph H CF.sub.3 H H 408 4 CH.sub.2Ph H CF.sub.3 H H 409 1 COMe H CF.sub.3 H H 410 2 COMe H CF.sub.3 H H 411 3 COMe H CF.sub.3 H H 412 4 COMe H CF.sub.3 H H 413 1 CO.sub.2Me H CF.sub.3 H H 414 2 CO.sub.2Me H CF.sub.3 H H 415 3 CO.sub.2Me H CF.sub.3 H H 416 4 CO.sub.2Me H CF.sub.3 H H 417 1 CO.sub.2tBu H CF.sub.3 H H 418 2 CO.sub.2tBu H CF.sub.3 H H 419 3 CO.sub.2tBu H CF.sub.3 H H 420 4 CO.sub.2tBu H CF.sub.3 H H 421 1 CONHMe H CF.sub.3 H H 422 2 CONHMe H CF.sub.3 H H 423 3 CONHMe H CF.sub.3 H H 424 4 CONHMe H CF.sub.3 H H 425 1 SO.sub.2Me H CF.sub.3 H H 426 2 SO.sub.2Me H CF.sub.3 H H 427 3 SO.sub.2Me H CF.sub.3 H H 428 4 SO.sub.2Me H CF.sub.3 H H 429 1 SO.sub.2NH.sub.2 H CF.sub.3 H H 430 2 SO.sub.2NH.sub.2 H CF.sub.3 H H 431 3 SO.sub.2NH.sub.2 H CF.sub.3 H H 432 4 SO.sub.2NH.sub.2 H CF.sub.3 H H 433 1 H H F H H 434 2 H H F H H 435 3 H H F H H 436 3 H H F H H 437 1 Me H F H H 438 2 Me H F H H 439 3 Me H F H H 440 4 Me H F H H 441 1 CH.sub.2Ph H F H H 442 2 CH.sub.2Ph H F H H 443 3 CH.sub.2Ph H F H H 444 4 CH.sub.2Ph H F H H 445 1 COMe H F H H 446 2 COMe H F H H 447 3 COMe H F H H 448 4 COMe H F H H 449 1 CO.sub.2Me H F H H 450 2 CO.sub.2Me H F H H 451 3 CO.sub.2Me H F H H 452 4 CO.sub.2Me H F H H 453 1 CO.sub.2tBu H F H H 454 2 CO.sub.2tBu H F H H 455 3 CO.sub.2tBu H F H H 456 4 CO.sub.2tBu H F H H 457 1 CONHMe H F H H 458 2 CONHMe H F H H 459 3 CONHMe H F H H 460 4 CONHMe H F H H 461 1 SO.sub.2Me H F H H 462 2 SO.sub.2Me H F H H 463 3 SO.sub.2Me H F H H 464 4 SO.sub.2Me H F H H 465 1 SO.sub.2NH.sub.2 H F H H 466 2 SO.sub.2NH.sub.2 H F H H 467 3 SO.sub.2NH.sub.2 H F H H 468 4 SO.sub.2NH.sub.2 H F H H 469 1 H H Cl H H 470 2 H H Cl H H 471 3 H H Cl H H 472 4 H H Cl H H 473 1 Me H Cl H H 474 2 Me H Cl H H 475 3 Me H Cl H H 476 4 Me H Cl H H 477 1 CH.sub.2Ph H Cl H H 478 2 CH.sub.2Ph H Cl H H 479 3 CH.sub.2Ph H Cl H H 480 4 CH.sub.2Ph H Cl H H 481 1 COMe H Cl H H 482 2 COMe H Cl H H 483 3 COMe H Cl H H 484 4 COMe H Cl H H 485 1 CO.sub.2Me H Cl H H 486 2 CO.sub.2Me H Cl H H 487 3 CO.sub.2Me H Cl H H 488 4 CO.sub.2Me H Cl H H 489 1 CO.sub.2tBu H Cl H H 490 2 CO.sub.2tBu H Cl H H 491 3 CO.sub.2tBu H Cl H H 492 4 CO.sub.2tBu H Cl H H 493 1 CONHMe H Cl H H 494 2 CONHMe H Cl H H 495 3 CONHMe H Cl H H 496 4 CONHMe H Cl H H 497 1 SO.sub.2Me H Cl H H 498 2 SO.sub.2Me H Cl H H 499 3 SO.sub.2Me H Cl H H 500 4 SO.sub.2Me H Cl H H 501 1 SO.sub.2NH.sub.2 H Cl H H 502 2 SO.sub.2NH.sub.2 H Cl H H 503 3 SO.sub.2NH.sub.2 H Cl H H 504 4 SO.sub.2NH.sub.2 H Cl H H 505 1 H H CN H H 506 2 H H CN H H 507 3 H H CN H H 508 4 H H CN H H 509 1 Me H CN H H 510 2 Me H CN H H 511 3 Me H CN H H 512 4 Me H CN H H 513 1 CH.sub.2Ph H CN H H 514 2 CH.sub.2Ph H CN H H 515 3 CH.sub.2Ph H CN H H 516 4 CH.sub.2Ph H CN H H 517 1 COMe H CN H H 518 2 COMe H CN H H 519 3 COMe H CN H H 520 4 COMe H CN H H 521 1 CO.sub.2Me H CN H H 522 2 CO.sub.2Me H CN H H 523 3 CO.sub.2Me H CN H H 524 4 CO.sub.2Me H CN H H 525 1 CO.sub.2tBu H CN H H 526 2 CO.sub.2tBu H CN H H 527 3 CO.sub.2tBu H CN H H 528 4 CO.sub.2tBu H CN H H 529 1 CONHMe H CN H H 530 2 CONHMe H CN H H 531 3 CONHMe H CN H H 532 4 CONHMe H CN H H 533 1 SO.sub.2Me H CN H H 534 2 SO.sub.2Me H CN H H 535 3 SO.sub.2Me H CN H H 536 4 SO.sub.2Me H CN H H 537 1 SO.sub.2NH.sub.2 H CN H H 538 2 SO.sub.2NH.sub.2 H CN H H 539 3 SO.sub.2NH.sub.2 H CN H H 540 4 SO.sub.2NH.sub.2 H CN H H 541 1 H OH H H H 542 2 H OH H H H 543 3 H OH H H H 544 4 H OH H H H 545 1 Me OH H H H 546 2 Me OH H H H 547 3 Me OH H H H 548 4 Me OH H H H 549 1 CH.sub.2Ph OH H H H 550 2 CH.sub.2Ph OH H H H 551 3 CH.sub.2Ph OH H H H 552 4 CH.sub.2Ph OH H H H 553 1 COMe OH H H H 554 2 COMe OH H H H 555 3 COMe OH H H H 556 4 COMe OH H H H 557 1 CO.sub.2Me OH H H H 558 2 CO.sub.2Me OH H H H 559 3 CO.sub.2Me OH H H H 560 4 CO.sub.2Me OH H H H 561 1 CO.sub.2tBu OH H H H 562 2 CO.sub.2tBu OH H H H 563 3 CO.sub.2tBu OH H H H 564 4 CO.sub.2tBu OH H H H 565 1 CONHMe OH H H H 566 2 CONHMe OH H H H 567 3 CONHMe OH H H H 568 4 CONHMe OH H H H 569 1 SO.sub.2Me OH H H H 570 2 SO.sub.2Me OH H H H 571 3 SO.sub.2Me OH H H H 572 4 SO.sub.2Me OH H H H 573 1 SO.sub.2NH.sub.2 OH H H H 574 2 SO.sub.2NH.sub.2 OH H H H 575 3 SO.sub.2NH.sub.2 OH H H H 576 4 SO.sub.2NH.sub.2 OH H H H 577 1 H OMe H H H 578 2 H OMe H H H 579 3 H OMe H H H 580 4 H OMe H H H 581 1 Me OMe H H H 582 2 Me OMe H H H 583 3 Me OMe H H H 584 4 Me OMe H H H 585 1 CH.sub.2Ph OMe H H H 586 2 CH.sub.2Ph OMe H H H 587 3 CH.sub.2Ph OMe H H H 588 4 CH.sub.2Ph OMe H H H 589 1 COMe OMe H H H 590 2 COMe OMe H H H 591 3 COMe OMe H H H 592 4 COMe OMe H H H 593 1 CO.sub.2Me OMe H H H 594 2 CO.sub.2Me OMe H H H 595 3 CO.sub.2Me OMe H H H 596 4 CO.sub.2Me OMe H H H 597 1 CO.sub.2tBu OMe H H H 598 2 CO.sub.2tBu OMe H H H 599 3 CO.sub.2tBu OMe H H H 600 4 CO.sub.2tBu OMe H H H 601 1 CONHMe OMe H H H 602 2 CONHMe OMe H H H 603 3 CONHMe OMe H H H 604 4 CONHMe OMe H H H 605 1 SO.sub.2Me OMe H H H 606 2 SO.sub.2Me OMe H H H 607 3 SO.sub.2Me OMe H H H 608 4 SO.sub.2Me OMe H H H 609 1 SO.sub.2NH.sub.2 OMe H H H 610 2 SO.sub.2NH.sub.2 OMe H H H 611 3 SO.sub.2NH.sub.2 OMe H H H 612 4 SO.sub.2NH.sub.2 OMe H H H 613 1 H Me H H H 614 2 H Me H H H 615 3 H Me H H H 616 4 H Me H H H 617 1 Me Me H H H 618 2 Me Me H H H 619 3 Me Me H H H 620 4 Me Me H H H 621 1 CH.sub.2Ph Me H H H 622 2 CH.sub.2Ph Me H H H 623 3 CH.sub.2Ph Me H H H 624 4 CH.sub.2Ph Me H H H 625 1 COMe Me H H H 626 2 COMe Me H H H 627 3 COMe Me H H H 628 4 COMe Me H H H 629 1 CO.sub.2Me Me H H H 630 2 CO.sub.2Me Me H H H 631 3 CO.sub.2Me Me H H H 632 4 CO.sub.2Me Me H H H 633 1 CO.sub.2tBu Me H H H 634 2 CO.sub.2tBu Me H H H 635 3 CO.sub.2tBu Me H H H 636 4 CO.sub.2tBu Me H H H 637 1 CONHMe Me H H H 638 2 CONHMe Me H H H 639 3 CONHMe Me H H H 640 4 CONHMe Me H H H 641 1 SO.sub.2Me Me H H H 642 2 SO.sub.2Me Me H H H 643 3 SO.sub.2Me Me H H H 644 4 SO.sub.2Me Me H H H 645 1 SO.sub.2NH.sub.2 Me H H H 646 2 SO.sub.2NH.sub.2 Me H H H 647 3 SO.sub.2NH.sub.2 Me H H H 648 4 SO.sub.2NH.sub.2 Me H H H 649 1 H CF.sub.3 H H H 650 2 H CF.sub.3 H H H 651 3 H CF.sub.3 H H H 652 4 H CF.sub.3 H H H 653 1 Me CF.sub.3 H H H 654 2 Me CF.sub.3 H H H 655 3 Me CF.sub.3 H H H 656 4 Me CF.sub.3 H H H 657 1 CH.sub.2Ph CF.sub.3 H H H 658 2 CH.sub.2Ph CF.sub.3 H H H 659 3 CH.sub.2Ph CF.sub.3 H H H 660 4 CH.sub.2Ph CF.sub.3 H H H 661 1 COMe CF.sub.3 H H H 662 2 COMe CF.sub.3 H H H 663 3 COMe CF.sub.3 H H H 664 4 COMe CF.sub.3 H H H 665 1 CO.sub.2Me CF.sub.3 H H H 666 2 CO.sub.2Me CF.sub.3 H H H 667 3 CO.sub.2Me CF.sub.3 H H H 668 4 CO.sub.2Me CF.sub.3 H H H 669 1 CO.sub.2tBu CF.sub.3 H H H 670 2 CO.sub.2tBu CF.sub.3 H H H 671 3 CO.sub.2tBu CF.sub.3 H H H 672 4 CO.sub.2tBu CF.sub.3 H H H 673 1 CONHMe CF.sub.3 H H H 674 2 CONHMe CF.sub.3 H H H 675 3 CONHMe CF.sub.3 H H H 676 4 CONHMe CF.sub.3 H H H 677 1 SO.sub.2Me CF.sub.3 H H H 678 2 SO.sub.2Me CF.sub.3 H H H 679 3 SO.sub.2Me CF.sub.3 H H H 680 4 SO.sub.2Me CF.sub.3 H H H 681 1 SO.sub.2NH.sub.2 CF.sub.3 H H H 682 2 SO.sub.2NH.sub.2 CF.sub.3 H H H 683 3 SO.sub.2NH.sub.2 CF.sub.3 H H H 684 4 SO.sub.2NH.sub.2 CF.sub.3 H H H 685 1 H F H H H 686 2 H F H H H 687 3 H F H H H 688 3 H F H H H 689 1 Me F H H H 690 2 Me F H H H 691 3 Me F H H H 692 4 Me F H H H 693 1 CH.sub.2Ph F H H H 694 2 CH.sub.2Ph F H H H 695 3 CH.sub.2Ph F H H H 696 4 CH.sub.2Ph F H H H 697 1 COMe F H H H 698 2 COMe F H H H 699 3 COMe F H H H 700 4 COMe F H H H 701 1 CO.sub.2Me F H H H 702 2 CO.sub.2Me F H H H 703 3 CO.sub.2Me F H H H 704 4 CO.sub.2Me F H H H 705 1 CO.sub.2tBu F H H H 706 2 CO.sub.2tBu F H H H 707 3 CO.sub.2tBu F H H H 708 4 CO.sub.2tBu F H H H 709 1 CONHMe F H H H 710 2 CONHMe F H H H 711 3 CONHMe F H H H 712 4 CONHMe F H H H 713 1 SO.sub.2Me F H H H 714 2 SO.sub.2Me F H H H 715 3 SO.sub.2Me F H H H 716 4 SO.sub.2Me F H H H 717 1 SO.sub.2NH.sub.2 F H H H 718 2 SO.sub.2NH.sub.2 F H H H 719 3 SO.sub.2NH.sub.2 F H H H 720 4 SO.sub.2NH.sub.2 F H H H 721 1 H Cl H H H 722 2 H Cl H H H 723 3 H Cl H H H 724 4 H Cl H H H 725 1 Me Cl H H H 726 2 Me Cl H H H 727 3 Me Cl H H H 728 4 Me Cl H H H 729 1 CH.sub.2Ph Cl H H H 730 2 CH.sub.2Ph Cl H H H 731 3 CH.sub.2Ph Cl H H H 732 4 CH.sub.2Ph Cl H H H 733 1 COMe Cl H H H 734 2 COMe Cl H H H 735 3 COMe Cl H H H 736 4 COMe Cl H H H 737 1 CO.sub.2Me Cl H H H 738 2 CO.sub.2Me Cl H H H 739 3 CO.sub.2Me Cl H H H 740 4 CO.sub.2Me Cl H H H 741 1 CO.sub.2tBu Cl H H H 742 2 CO.sub.2tBu Cl H H H 743 3 CO.sub.2tBu Cl H H H 744 4 CO.sub.2tBu Cl H H H 745 1 CONHMe Cl H H H 746 2 CONHMe Cl H H H 747 3 CONHMe Cl H H H 748 4 CONHMe Cl H H H 749 1 SO.sub.2Me Cl H H H 750 2 SO.sub.2Me Cl H H H 751 3 SO.sub.2Me Cl H H H 752 4 SO.sub.2Me Cl H H H 753 1 SO.sub.2NH.sub.2 Cl H H H 754 2 SO.sub.2NH.sub.2 Cl H H H 755 3 SO.sub.2NH.sub.2 Cl H H H 756 4 SO.sub.2NH.sub.2 Cl H H H 757 1 H CN H H H 758 2 H CN H H H 759 3 H CN H H H 760 4 H CN H H H 761 1 Me CN H H H 762 2 Me CN H H H 763 3 Me CN H H H 764 4 Me CN H H H 765 1 CH.sub.2Ph CN H H H 766 2 CH.sub.2Ph CN H H H 767 3 CH.sub.2Ph CN H H H 768 4 CH.sub.2Ph CN H H H 769 1 COMe CN H H H 770 2 COMe CN H H H 771 3 COMe CN H H H 772 4 COMe CN H H H 773 1 CO.sub.2Me CN H H H 774 2 CO.sub.2Me CN H H H 775 3 CO.sub.2Me CN H H H 776 4 CO.sub.2Me CN H H H 777 1 CO.sub.2tBu CN H H H 778 2 CO.sub.2tBu CN H H H 779 3 CO.sub.2tBu CN H H H 780 4 CO.sub.2tBu CN H H H 781 1 CONHMe CN H H H 782 2 CONHMe CN H H H 783 3 CONHMe CN H H H 784 4 CONHMe CN H H H 785 1 SO.sub.2Me CN H H H 786 2 SO.sub.2Me CN H H H 787 3 SO.sub.2Me CN H H H 788 4 SO.sub.2Me CN H H H 789 1 SO.sub.2NH.sub.2 CN H H H 790 2 SO.sub.2NH.sub.2 CN H H H 791 3 SO.sub.2NH.sub.2 CN H H H 792 4 SO.sub.2NH.sub.2 CN H H H 793 1 H H H H OH 794 2 H H H H OH 795 3 H H H H OH 796 4 H H H H OH 797 1 Me H H H OH 798 2 Me H H H OH 799 3 Me H H H OH 800 4 Me H H H OH 801 1 CH.sub.2Ph H H H OH 802 2 CH.sub.2Ph H H H OH 803 3 CH.sub.2Ph H H H OH 804 4 CH.sub.2Ph H H H OH 805 1 COMe H H H OH 806 2 COMe H H H OH 807 3 COMe H H H OH 808 4 COMe H H H OH 809 1 CO.sub.2Me H H H OH 810 2 CO.sub.2Me H H H OH 811 3 CO.sub.2Me H H H OH 812 4 CO.sub.2Me H H H OH 813 1 CO.sub.2tBu H H H OH 814 2 CO.sub.2tBu H H H OH 815 3 CO.sub.2tBu H H H OH 816 4 CO.sub.2tBu H H H OH 817 1 CONHMe H H H OH 818 2 CONHMe H H H OH 819 3 CONHMe H H H OH 820 4 CONHMe H H H OH 821 1 SO.sub.2Me H H H OH 822 2 SO.sub.2Me H H H OH 823 3 SO.sub.2Me H H H OH 824 4 SO.sub.2Me H H H OH 825 1 SO.sub.2NH.sub.2 H H H OH 826 2 SO.sub.2NH.sub.2 H H H OH 827 3 SO.sub.2NH.sub.2 H H H OH 828 4 SO.sub.2NH.sub.2 H H H OH 829 1 H H H H OMe 830 2 H H H H OMe 831 3 H H H H OMe 832 4 H H H H OMe 833 1 Me H H H OMe 834 2 Me H H H OMe 835 3 Me H H H OMe 836 4 Me H H H OMe 837 1 CH.sub.2Ph H H H OMe 838 2 CH.sub.2Ph H H H OMe 839 3 CH.sub.2Ph H H H OMe 840 4 CH.sub.2Ph H H H OMe 841 1 COMe H H H OMe 842 2 COMe H H H OMe 843 3 COMe H H H OMe 844 4 COMe H H H OMe 845 1 CO.sub.2Me H H H OMe 846 2 CO.sub.2Me H H H OMe 847 3 CO.sub.2Me H H H OMe 848 4 CO.sub.2Me H H H OMe 849 1 CO.sub.2tBu H H H OMe 850 2 CO.sub.2tBu H H H OMe 851 3 CO.sub.2tBu H H H OMe 852 4 CO.sub.2tBu H H H OMe 853 1 CONHMe H H H OMe 854 2 CONHMe H H H OMe 855 3 CONHMe H H H OMe 856 4 CONHMe H H H OMe 857 1 SO.sub.2Me H H H OMe 858 2 SO.sub.2Me H H H OMe 859 3 SO.sub.2Me H H H OMe 860 4 SO.sub.2Me H H H OMe 861 1 SO.sub.2NH.sub.2 H H H OMe 862 2 SO.sub.2NH.sub.2 H H H OMe 863 3 SO.sub.2NH.sub.2 H H H OMe 864 4 SO.sub.2NH.sub.2 H H H OMe 865 1 H H H H Me 866 2 H H H H Me 867 3 H H H H Me 868 4 H H H H Me 869 1 Me H H H Me 870 2 Me H H H Me 871 3 Me H H H Me 872 4 Me H H H Me 873 1 CH.sub.2Ph H H H Me 874 2 CH.sub.2Ph H H H Me 875 3 CH.sub.2Ph H H H Me 876 4 CH.sub.2Ph H H H Me 877 1 COMe H H H Me 878 2 COMe H H H Me 879 3 COMe H H H Me 880 4 COMe H H H Me 881 1 CO.sub.2Me H H H Me 882 2 CO.sub.2Me H H H Me 883 3 CO.sub.2Me H H H Me 884 4 CO.sub.2Me H H H Me 885 1 CO.sub.2tBu H H H Me 886 2 CO.sub.2tBu H H H Me 887 3 CO.sub.2tBu H H H Me 888 4 CO.sub.2tBu H H H Me 889 1 CONHMe H H H Me 890 2 CONHMe H H H Me 891 3 CONHMe H H H Me 892 4 CONHMe H H H Me 893 1 SO.sub.2Me H H H Me 894 2 SO.sub.2Me H H H Me 895 3 SO.sub.2Me H H H Me 896 4 SO.sub.2Me H H H Me 897 1 SO.sub.2NH.sub.2 H H H Me 898 2 SO.sub.2NH.sub.2 H H H Me 899 3 SO.sub.2NH.sub.2 H H H Me 900 4 SO.sub.2NH.sub.2 H H H Me 901 1 H H H H CF.sub.3 902 2 H H H H CF.sub.3 903 3 H H H H CF.sub.3 904 4 H H H H CF.sub.3 905 1 Me H H H CF.sub.3 906 2 Me H H H CF.sub.3 907 3 Me H H H CF.sub.3 908 4 Me H H H CF.sub.3 909 1 CH.sub.2Ph H H H CF.sub.3 910 2 CH.sub.2Ph H H H CF.sub.3 911 3 CH.sub.2Ph H H H CF.sub.3 912 4 CH.sub.2Ph H H H CF.sub.3 913 1 COMe H H H CF.sub.3 914 2 COMe H H H CF.sub.3 915 3 COMe H H H CF.sub.3 916 4 COMe H H H CF.sub.3 917 1 CO.sub.2Me H H H CF.sub.3 918 2 CO.sub.2Me H H H CF.sub.3 919 3 CO.sub.2Me H H H CF.sub.3 920 4 CO.sub.2Me H H H CF.sub.3 921 1 CO.sub.2tBu H H H CF.sub.3 922 2 CO.sub.2tBu H H H CF.sub.3 923 3 CO.sub.2tBu H H H CF.sub.3 924 4 CO.sub.2tBu H H H CF.sub.3 925 1 CONHMe H H H CF.sub.3 926 2 CONHMe H H H CF.sub.3 927 3 CONHMe H H H CF.sub.3 928 4 CONHMe H H H CF.sub.3 929 1 SO.sub.2Me H H H CF.sub.3 930 2 SO.sub.2Me H H H CF.sub.3 931 3 SO.sub.2Me H H H CF.sub.3 932 4 SO.sub.2Me H H H CF.sub.3 933 1 SO.sub.2NH.sub.2 H H H CF.sub.3 934 2 SO.sub.2NH.sub.2 H H H CF.sub.3 935 3 SO.sub.2NH.sub.2 H H H CF.sub.3 936 4 SO.sub.2NH.sub.2 H H H CF.sub.3 937 1 H H H H F 938 2 H H H H F 939 3 H H H H F 940 3 H H H H F 941 1 Me H H H F 942 2 Me H H H F 943 3 Me H H H F 944 4 Me H H H F 945 1 CH.sub.2Ph H H H F 946 2 CH.sub.2Ph H H H F 947 3 CH.sub.2Ph H H H F 948 4 CH.sub.2Ph H H H F 949 1 COMe H H H F 950 2 COMe H H H F 951 3 COMe H H H F 952 4 COMe H H H F 953 1 CO.sub.2Me H H H F 954 2 CO.sub.2Me H H H F 955 3 CO.sub.2Me H H H F 956 4 CO.sub.2Me H H H F 957 1 CO.sub.2tBu H H H F 958 2 CO.sub.2tBu H H H F 959 3 CO.sub.2tBu H H H F 960 4 CO.sub.2tBu H H H F 961 1 CONHMe H H H F 962 2 CONHMe H H H F 963 3 CONHMe H H H F 964 4 CONHMe H H H F 965 1 SO.sub.2Me H H H F 966 2 SO.sub.2Me H H H F 967 3 SO.sub.2Me H H H F 968 4 SO.sub.2Me H H H F 969 1 SO.sub.2NH.sub.2 H H H F 970 2 SO.sub.2NH.sub.2 H H H F 971 3 SO.sub.2NH.sub.2 H H H F 972 4 SO.sub.2NH.sub.2 H H H F 973 1 H H H H Cl 974 2 H H H H Cl 975 3 H H H H Cl 976 4 H H H H Cl 977 1 Me H H H Cl 978 2 Me H H H Cl 979 3 Me H H H Cl 980 4 Me H H H Cl 981 1 CH.sub.2Ph H H H Cl 982 2 CH.sub.2Ph H H H Cl 983 3 CH.sub.2Ph H H H Cl 984 4 CH.sub.2Ph H H H Cl 985 1 COMe H H H Cl 986 2 COMe H H H Cl 987 3 COMe H H H Cl 988 4 COMe H H H Cl 989 1 CO.sub.2Me H H H Cl 990 2 CO.sub.2Me H H H Cl 991 3 CO.sub.2Me H H H Cl 992 4 CO.sub.2Me H H H Cl 993 1 CO.sub.2tBu H H H Cl 994 2 CO.sub.2tBu H H H Cl 995 3 CO.sub.2tBu H H H Cl 996 4 CO.sub.2tBu H H H Cl 997 1 CONHMe H H H Cl 998 2 CONHMe H H H Cl 999 3 CONHMe H H H Cl 1000 4 CONHMe H H H Cl 1001 1 SO.sub.2Me H H H Cl 1002 2 SO.sub.2Me H H H Cl 1003 3 SO.sub.2Me H H H Cl 1004 4 SO.sub.2Me H H H Cl 1005 1 SO.sub.2NH.sub.2 H H H Cl 1006 2 SO.sub.2NH.sub.2 H H H Cl 1007 3 SO.sub.2NH.sub.2 H H H Cl 1008 4 SO.sub.2NH.sub.2 H H H Cl 1009 1 H H H H CN 1010 2 H H H H CN 1011 3 H H H H CN 1012 4 H H H H CN 1013 1 Me H H H CN 1014 2 Me H H H CN 1015 3 Me H H H CN 1016 4 Me H H H CN 1017 1 CH.sub.2Ph H H H CN 1018 2 CH.sub.2Ph H H H CN 1019 3 CH.sub.2Ph H H H CN 1020 4 CH.sub.2Ph H H H CN 1021 1 COMe H H H CN 1022 2 COMe H H H CN 1023 3 COMe H H H CN 1024 4 COMe H H H CN 1025 1 CO.sub.2Me H H H CN 1026 2 CO.sub.2Me H H H CN 1027 3 CO.sub.2Me H H H CN 1028 4 CO.sub.2Me H H H CN 1029 1 CO.sub.2tBu H H H CN 1030 2 CO.sub.2tBu H H H CN 1031 3 CO.sub.2tBu H H H CN 1032 4 CO.sub.2tBu H H H CN 1033 1 CONHMe H H H CN 1034 2 CONHMe H H H CN 1035 3 CONHMe H H H CN 1036 4 CONHMe H H H CN 1037 1 SO.sub.2Me H H H CN 1038 2 SO.sub.2Me H H H CN 1039 3 SO.sub.2Me H H H CN 1040 4 SO.sub.2Me H H H CN 1041 1 SO.sub.2NH.sub.2 H H H CN 1042 2 SO.sub.2NH.sub.2 H H H CN 1043 3 SO.sub.2NH.sub.2 H H H CN 1044 4 SO.sub.2NH.sub.2 H H H CN

    [2032] Exemplary embodiments include compounds having the formula (XXVI)

    ##STR00441##

    [2033] or a pharmaceutically acceptable salt form thereof defined herein below in Table 20.

    TABLE-US-00020 TABLE 20 Entry n R.sup.7 R.sup.20a R.sup.20b R.sup.20c R.sup.20d 1 1 H H H H H 2 2 H H H H H 3 3 H H H H H 4 4 H H H H H 5 1 Me H H H H 6 2 Me H H H H 7 3 Me H H H H 8 4 Me H H H H 9 1 CH.sub.2Ph H H H H 10 2 CH.sub.2Ph H H H H 11 3 CH.sub.2Ph H H H H 12 4 CH.sub.2Ph H H H H 13 1 COMe H H H H 14 2 COMe H H H H 15 3 COMe H H H H 16 4 COMe H H H H 17 1 CO.sub.2Me H H H H 18 2 CO.sub.2Me H H H H 19 3 CO.sub.2Me H H H H 20 4 CO.sub.2Me H H H H 21 1 CO.sub.2tBu H H H H 22 2 CO.sub.2tBu H H H H 23 3 CO.sub.2tBu H H H H 24 4 CO.sub.2tBu H H H H 25 1 CONHMe H H H H 26 2 CONHMe H H H H 27 3 CONHMe H H H H 28 4 CONHMe H H H H 29 1 SO.sub.2Me H H H H 30 2 SO.sub.2Me H H H H 31 3 SO.sub.2Me H H H H 32 4 SO.sub.2Me H H H H 33 1 SO.sub.2NH.sub.2 H H H H 34 2 SO.sub.2NH.sub.2 H H H H 35 3 SO.sub.2NH.sub.2 H H H H 36 4 SO.sub.2NH.sub.2 H H H H 37 1 H H H OH H 38 2 H H H OH H 39 3 H H H OH H 40 4 H H H OH H 41 1 Me H H OH H 42 2 Me H H OH H 43 3 Me H H OH H 44 4 Me H H OH H 45 1 CH.sub.2Ph H H OH H 46 2 CH.sub.2Ph H H OH H 47 3 CH.sub.2Ph H H OH H 48 4 CH.sub.2Ph H H OH H 49 1 COMe H H OH H 50 2 COMe H H OH H 51 3 COMe H H OH H 52 4 COMe H H OH H 53 1 CO.sub.2Me H H OH H 54 2 CO.sub.2Me H H OH H 55 3 CO.sub.2Me H H OH H 56 4 CO.sub.2Me H H OH H 57 1 CO.sub.2tBu H H OH H 58 2 CO.sub.2tBu H H OH H 59 3 CO.sub.2tBu H H OH H 60 4 CO.sub.2tBu H H OH H 61 1 CONHMe H H OH H 62 2 CONHMe H H OH H 63 3 CONHMe H H OH H 64 4 CONHMe H H OH H 65 1 SO.sub.2Me H H OH H 66 2 SO.sub.2Me H H OH H 67 3 SO.sub.2Me H H OH H 68 4 SO.sub.2Me H H OH H 69 1 SO.sub.2NH.sub.2 H H OH H 70 2 SO.sub.2NH.sub.2 H H OH H 71 3 SO.sub.2NH.sub.2 H H OH H 72 4 SO.sub.2NH.sub.2 H H OH H 73 1 H H H OMe H 74 2 H H H OMe H 75 3 H H H OMe H 76 4 H H H OMe H 77 1 Me H H OMe H 78 2 Me H H OMe H 79 3 Me H H OMe H 80 4 Me H H OMe H 81 1 CH.sub.2Ph H H OMe H 82 2 CH.sub.2Ph H H OMe H 83 3 CH.sub.2Ph H H OMe H 84 4 CH.sub.2Ph H H OMe H 85 1 COMe H H OMe H 86 2 COMe H H OMe H 87 3 COMe H H OMe H 88 4 COMe H H OMe H 89 1 CO.sub.2Me H H OMe H 90 2 CO.sub.2Me H H OMe H 91 3 CO.sub.2Me H H OMe H 92 4 CO.sub.2Me H H OMe H 93 1 CO.sub.2tBu H H OMe H 94 2 CO.sub.2tBu H H OMe H 95 3 CO.sub.2tBu H H OMe H 96 1 CO.sub.2tBu H H OMe H 97 1 CONHMe H H OMe H 98 2 CONHMe H H OMe H 99 3 CONHMe H H OMe H 100 4 CONHMe H H OMe H 101 1 SO.sub.2Me H H OMe H 102 2 SO.sub.2Me H H OMe H 103 3 SO.sub.2Me H H OMe H 104 4 SO.sub.2Me H H OMe H 105 1 SO.sub.2NH.sub.2 H H OMe H 106 2 SO.sub.2NH.sub.2 H H OMe H 107 3 SO.sub.2NH.sub.2 H H OMe H 108 4 SO.sub.2NH.sub.2 H H OMe H 109 1 H H H Me H 110 2 H H H Me H 111 3 H H H Me H 112 4 H H H Me H 113 1 Me H H Me H 114 2 Me H H Me H 115 3 Me H H Me H 116 4 Me H H Me H 117 1 CH.sub.2Ph H H Me H 118 2 CH.sub.2Ph H H Me H 119 3 CH.sub.2Ph H H Me H 120 4 CH.sub.2Ph H H Me H 121 1 COMe H H Me H 122 2 COMe H H Me H 123 3 COMe H H Me H 124 4 COMe H H Me H 125 1 CO.sub.2Me H H Me H 126 2 CO.sub.2Me H H Me H 127 3 CO.sub.2Me H H Me H 128 4 CO.sub.2Me H H Me H 129 1 CO.sub.2tBu H H Me H 130 2 CO.sub.2tBu H H Me H 131 3 CO.sub.2tBu H H Me H 132 4 CO.sub.2tBu H H Me H 133 1 CONHMe H H Me H 134 2 CONHMe H H Me H 135 3 CONHMe H H Me H 136 4 CONHMe H H Me H 137 1 SO.sub.2Me H H Me H 138 2 SO.sub.2Me H H Me H 139 3 SO.sub.2Me H H Me H 140 4 SO.sub.2Me H H Me H 141 1 SO.sub.2NH.sub.2 H H Me H 142 2 SO.sub.2NH.sub.2 H H Me H 143 3 SO.sub.2NH.sub.2 H H Me H 144 4 SO.sub.2NH.sub.2 H H Me H 145 1 H H H CF.sub.3 H 146 2 H H H CF.sub.3 H 147 3 H H H CF.sub.3 H 148 4 H H H CF.sub.3 H 149 1 Me H H CF.sub.3 H 150 2 Me H H CF.sub.3 H 151 3 Me H H CF.sub.3 H 152 4 Me H H CF.sub.3 H 153 1 CH.sub.2Ph H H CF.sub.3 H 154 2 CH.sub.2Ph H H CF.sub.3 H 155 3 CH.sub.2Ph H H CF.sub.3 H 156 4 CH.sub.2Ph H H CF.sub.3 H 157 1 COMe H H CF.sub.3 H 158 2 COMe H H CF.sub.3 H 159 3 COMe H H CF.sub.3 H 160 4 COMe H H CF.sub.3 H 161 1 CO.sub.2Me H H CF.sub.3 H 162 2 CO.sub.2Me H H CF.sub.3 H 163 3 CO.sub.2Me H H CF.sub.3 H 164 4 CO.sub.2Me H H CF.sub.3 H 165 1 CO.sub.2tBu H H CF.sub.3 H 166 2 CO.sub.2tBu H H CF.sub.3 H 167 3 CO.sub.2tBu H H CF.sub.3 H 168 4 CO.sub.2tBu H H CF.sub.3 H 169 1 CONHMe H H CF.sub.3 H 170 2 CONHMe H H CF.sub.3 H 171 3 CONHMe H H CF.sub.3 H 172 4 CONHMe H H CF.sub.3 H 173 1 SO.sub.2Me H H CF.sub.3 H 174 2 SO.sub.2Me H H CF.sub.3 H 175 3 SO.sub.2Me H H CF.sub.3 H 176 4 SO.sub.2Me H H CF.sub.3 H 177 1 SO.sub.2NH.sub.2 H H CF.sub.3 H 178 2 SO.sub.2NH.sub.2 H H CF.sub.3 H 179 3 SO.sub.2NH.sub.2 H H CF.sub.3 H 180 4 SO.sub.2NH.sub.2 H H CF.sub.3 H 181 1 H H H F H 182 2 H H H F H 183 3 H H H F H 184 4 H H H F H 185 1 Me H H F H 186 2 Me H H F H 187 3 Me H H F H 188 4 Me H H F H 189 1 CH.sub.2Ph H H F H 190 2 CH.sub.2Ph H H F H 191 3 CH.sub.2Ph H H F H 192 4 CH.sub.2Ph H H F H 193 1 COMe H H F H 194 2 COMe H H F H 195 3 COMe H H F H 196 4 COMe H H F H 197 1 CO.sub.2Me H H F H 198 2 CO.sub.2Me H H F H 199 3 CO.sub.2Me H H F H 200 4 CO.sub.2Me H H F H 201 1 CO.sub.2tBu H H F H 202 2 CO.sub.2tBu H H F H 203 3 CO.sub.2tBu H H F H 204 4 CO.sub.2tBu H H F H 205 1 CONHMe H H F H 206 2 CONHMe H H F H 207 3 CONHMe H H F H 208 4 CONHMe H H F H 209 1 SO.sub.2Me H H F H 210 2 SO.sub.2Me H H F H 211 3 SO.sub.2Me H H F H 212 4 SO.sub.2Me H H F H 213 1 SO.sub.2NH.sub.2 H H F H 214 2 SO.sub.2NH.sub.2 H H F H 215 3 SO.sub.2NH.sub.2 H H F H 216 4 SO.sub.2NH.sub.2 H H F H 217 1 H H H Cl H 218 2 H H H Cl H 219 3 H H H Cl H 220 4 H H H Cl H 221 1 Me H H Cl H 222 2 Me H H Cl H 223 3 Me H H Cl H 224 4 Me H H Cl H 225 1 CH.sub.2Ph H H Cl H 226 2 CH.sub.2Ph H H Cl H 227 3 CH.sub.2Ph H H Cl H 228 4 CH.sub.2Ph H H Cl H 229 1 COMe H H Cl H 230 2 COMe H H Cl H 231 3 COMe H H Cl H 232 4 COMe H H Cl H 233 1 CO.sub.2Me H H Cl H 234 2 CO.sub.2Me H H Cl H 235 3 CO.sub.2Me H H Cl H 236 4 CO.sub.2Me H H Cl H 237 1 CO.sub.2tBu H H Cl H 238 2 CO.sub.2tBu H H Cl H 239 3 CO.sub.2tBu H H Cl H 240 4 CO.sub.2tBu H H Cl H 241 1 CONHMe H H Cl H 242 2 CONHMe H H Cl H 243 3 CONHMe H H Cl H 244 4 CONHMe H H Cl H 245 1 SO.sub.2Me H H Cl H 246 2 SO.sub.2Me H H Cl H 247 3 SO.sub.2Me H H Cl H 248 4 SO.sub.2Me H H Cl H 249 1 SO.sub.2NH.sub.2 H H Cl H 250 2 SO.sub.2NH.sub.2 H H Cl H 251 3 SO.sub.2NH.sub.2 H H Cl H 252 4 SO.sub.2NH.sub.2 H H Cl H 253 1 H H H CN H 254 2 H H H CN H 255 3 H H H CN H 256 4 H H H CN H 257 1 Me H H CN H 258 2 Me H H CN H 259 3 Me H H CN H 260 4 Me H H CN H 261 1 CH.sub.2Ph H H CN H 262 2 CH.sub.2Ph H H CN H 263 3 CH.sub.2Ph H H CN H 264 4 CH.sub.2Ph H H CN H 265 1 COMe H H CN H 266 2 COMe H H CN H 267 3 COMe H H CN H 268 4 COMe H H CN H 269 1 CO.sub.2Me H H CN H 270 2 CO.sub.2Me H H CN H 271 3 CO.sub.2Me H H CN H 272 4 CO.sub.2Me H H CN H 273 1 CO.sub.2tBu H H CN H 274 2 CO.sub.2tBu H H CN H 275 3 CO.sub.2tBu H H CN H 276 4 CO.sub.2tBu H H CN H 277 1 CONHMe H H CN H 278 2 CONHMe H H CN H 279 3 CONHMe H H CN H 280 4 CONHMe H H CN H 281 1 SO.sub.2Me H H CN H 282 2 SO.sub.2Me H H CN H 283 3 SO.sub.2Me H H CN H 284 4 SO.sub.2Me H H CN H 285 1 SO.sub.2NH.sub.2 H H CN H 286 2 SO.sub.2NH.sub.2 H H CN H 287 3 SO.sub.2NH.sub.2 H H CN H 288 4 SO.sub.2NH.sub.2 H H CN H 289 1 H H OH H H 290 2 H H OH H H 291 3 H H OH H H 292 4 H H OH H H 293 1 Me H OH H H 294 2 Me H OH H H 295 3 Me H OH H H 296 4 Me H OH H H 297 1 CH.sub.2Ph H OH H H 298 2 CH.sub.2Ph H OH H H 299 3 CH.sub.2Ph H OH H H 300 4 CH.sub.2Ph H OH H H 301 1 COMe H OH H H 302 2 COMe H OH H H 303 3 COMe H OH H H 304 4 COMe H OH H H 305 1 CO.sub.2Me H OH H H 306 2 CO.sub.2Me H OH H H 307 3 CO.sub.2Me H OH H H 308 4 CO.sub.2Me H OH H H 309 1 CO.sub.2tBu H OH H H 310 2 CO.sub.2tBu H OH H H 311 3 CO.sub.2tBu H OH H H 312 4 CO.sub.2tBu H OH H H 313 1 CONHMe H OH H H 314 2 CONHMe H OH H H 315 3 CONHMe H OH H H 316 4 CONHMe H OH H H 317 1 SO.sub.2Me H OH H H 318 2 SO.sub.2Me H OH H H 319 3 SO.sub.2Me H OH H H 320 4 SO.sub.2Me H OH H H 321 1 SO.sub.2NH.sub.2 H OH H H 322 2 SO.sub.2NH.sub.2 H OH H H 323 3 SO.sub.2NH.sub.2 H OH H H 324 4 SO.sub.2NH.sub.2 H OH H H 325 1 H H OMe H H 326 2 H H OMe H H 327 3 H H OMe H H 328 4 H H OMe H H 329 1 Me H OMe H H 330 2 Me H OMe H H 331 3 Me H OMe H H 332 4 Me H OMe H H 333 1 CH.sub.2Ph H OMe H H 334 2 CH.sub.2Ph H OMe H H 335 3 CH.sub.2Ph H OMe H H 336 4 CH.sub.2Ph H OMe H H 337 1 COMe H OMe H H 338 2 COMe H OMe H H 339 3 COMe H OMe H H 340 4 COMe H OMe H H 341 1 CO.sub.2Me H OMe H H 342 2 CO.sub.2Me H OMe H H 343 3 CO.sub.2Me H OMe H H 344 4 CO.sub.2Me H OMe H H 345 1 CO.sub.2tBu H OMe H H 346 2 CO.sub.2tBu H OMe H H 347 3 CO.sub.2tBu H OMe H H 348 4 CO.sub.2tBu H OMe H H 349 1 CONHMe H OMe H H 350 2 CONHMe H OMe H H 351 3 CONHMe H OMe H H 352 4 CONHMe H OMe H H 353 1 SO.sub.2Me H OMe H H 354 2 SO.sub.2Me H OMe H H 355 3 SO.sub.2Me H OMe H H 356 4 SO.sub.2Me H OMe H H 357 1 SO.sub.2NH.sub.2 H OMe H H 358 2 SO.sub.2NH.sub.2 H OMe H H 359 3 SO.sub.2NH.sub.2 H OMe H H 360 4 SO.sub.2NH.sub.2 H OMe H H 361 1 H H Me H H 362 2 H H Me H H 363 3 H H Me H H 364 4 H H Me H H 365 1 Me H Me H H 366 2 Me H Me H H 367 3 Me H Me H H 368 4 Me H Me H H 369 1 CH.sub.2Ph H Me H H 370 2 CH.sub.2Ph H Me H H 371 3 CH.sub.2Ph H Me H H 372 4 CH.sub.2Ph H Me H H 373 1 COMe H Me H H 374 2 COMe H Me H H 375 3 COMe H Me H H 376 4 COMe H Me H H 377 1 CO.sub.2Me H Me H H 378 2 CO.sub.2Me H Me H H 379 3 CO.sub.2Me H Me H H 380 4 CO.sub.2Me H Me H H 381 1 CO.sub.2tBu H Me H H 382 2 CO.sub.2tBu H Me H H 383 3 CO.sub.2tBu H Me H H 384 4 CO.sub.2tBu H Me H H 385 1 CONHMe H Me H H 386 2 CONHMe H Me H H 387 3 CONHMe H Me H H 388 4 CONHMe H Me H H 389 1 SO.sub.2Me H Me H H 390 2 SO.sub.2Me H Me H H 391 3 SO.sub.2Me H Me H H 392 4 SO.sub.2Me H Me H H 393 1 SO.sub.2NH.sub.2 H Me H H 394 2 SO.sub.2NH.sub.2 H Me H H 395 3 SO.sub.2NH.sub.2 H Me H H 396 4 SO.sub.2NH.sub.2 H Me H H 397 1 H H CF.sub.3 H H 398 2 H H CF.sub.3 H H 399 3 H H CF.sub.3 H H 400 4 H H CF.sub.3 H H 401 1 Me H CF.sub.3 H H 402 2 Me H CF.sub.3 H H 403 3 Me H CF.sub.3 H H 404 4 Me H CF.sub.3 H H 405 1 CH.sub.2Ph H CF.sub.3 H H 406 2 CH.sub.2Ph H CF.sub.3 H H 407 3 CH.sub.2Ph H CF.sub.3 H H 408 4 CH.sub.2Ph H CF.sub.3 H H 409 1 COMe H CF.sub.3 H H 410 2 COMe H CF.sub.3 H H 411 3 COMe H CF.sub.3 H H 412 4 COMe H CF.sub.3 H H 413 1 CO.sub.2Me H CF.sub.3 H H 414 2 CO.sub.2Me H CF.sub.3 H H 415 3 CO.sub.2Me H CF.sub.3 H H 416 4 CO.sub.2Me H CF.sub.3 H H 417 1 CO.sub.2tBu H CF.sub.3 H H 418 2 CO.sub.2tBu H CF.sub.3 H H 419 3 CO.sub.2tBu H CF.sub.3 H H 420 4 CO.sub.2tBu H CF.sub.3 H H 421 1 CONHMe H CF.sub.3 H H 422 2 CONHMe H CF.sub.3 H H 423 3 CONHMe H CF.sub.3 H H 424 4 CONHMe H CF.sub.3 H H 425 1 SO.sub.2Me H CF.sub.3 H H 426 2 SO.sub.2Me H CF.sub.3 H H 427 3 SO.sub.2Me H CF.sub.3 H H 428 4 SO.sub.2Me H CF.sub.3 H H 429 1 SO.sub.2NH.sub.2 H CF.sub.3 H H 430 2 SO.sub.2NH.sub.2 H CF.sub.3 H H 431 3 SO.sub.2NH.sub.2 H CF.sub.3 H H 432 4 SO.sub.2NH.sub.2 H CF.sub.3 H H 433 1 H H F H H 434 2 H H F H H 435 3 H H F H H 436 3 H H F H H 437 1 Me H F H H 438 2 Me H F H H 439 3 Me H F H H 440 4 Me H F H H 441 1 CH.sub.2Ph H F H H 442 2 CH.sub.2Ph H F H H 443 3 CH.sub.2Ph H F H H 444 4 CH.sub.2Ph H F H H 445 1 COMe H F H H 446 2 COMe H F H H 447 3 COMe H F H H 448 4 COMe H F H H 449 1 CO.sub.2Me H F H H 450 2 CO.sub.2Me H F H H 451 3 CO.sub.2Me H F H H 452 4 CO.sub.2Me H F H H 453 1 CO.sub.2tBu H F H H 454 2 CO.sub.2tBu H F H H 455 3 CO.sub.2tBu H F H H 456 4 CO.sub.2tBu H F H H 457 1 CONHMe H F H H 458 2 CONHMe H F H H 459 3 CONHMe H F H H 460 4 CONHMe H F H H 461 1 SO.sub.2Me H F H H 462 2 SO.sub.2Me H F H H 463 3 SO.sub.2Me H F H H 464 4 SO.sub.2Me H F H H 465 1 SO.sub.2NH.sub.2 H F H H 466 2 SO.sub.2NH.sub.2 H F H H 467 3 SO.sub.2NH.sub.2 H F H H 468 4 SO.sub.2NH.sub.2 H F H H 469 1 H H Cl H H 470 2 H H Cl H H 471 3 H H Cl H H 472 4 H H Cl H H 473 1 Me H Cl H H 474 2 Me H Cl H H 475 3 Me H Cl H H 476 4 Me H Cl H H 477 1 CH.sub.2Ph H Cl H H 478 2 CH.sub.2Ph H Cl H H 479 3 CH.sub.2Ph H Cl H H 480 4 CH.sub.2Ph H Cl H H 481 1 COMe H Cl H H 482 2 COMe H Cl H H 483 3 COMe H Cl H H 484 4 COMe H Cl H H 485 1 CO.sub.2Me H Cl H H 486 2 CO.sub.2Me H Cl H H 487 3 CO.sub.2Me H Cl H H 488 4 CO.sub.2Me H Cl H H 489 1 CO.sub.2tBu H Cl H H 490 2 CO.sub.2tBu H Cl H H 491 3 CO.sub.2tBu H Cl H H 492 4 CO.sub.2tBu H Cl H H 493 1 CONHMe H Cl H H 494 2 CONHMe H Cl H H 495 3 CONHMe H Cl H H 496 4 CONHMe H Cl H H 497 1 SO.sub.2Me H Cl H H 498 2 SO.sub.2Me H Cl H H 499 3 SO.sub.2Me H Cl H H 500 4 SO.sub.2Me H Cl H H 501 1 SO.sub.2NH.sub.2 H Cl H H 502 2 SO.sub.2NH.sub.2 H Cl H H 503 3 SO.sub.2NH.sub.2 H Cl H H 504 4 SO.sub.2NH.sub.2 H Cl H H 505 1 H H CN H H 506 2 H H CN H H 507 3 H H CN H H 508 4 H H CN H H 509 1 Me H CN H H 510 2 Me H CN H H 511 3 Me H CN H H 512 4 Me H CN H H 513 1 CH.sub.2Ph H CN H H 514 2 CH.sub.2Ph H CN H H 515 3 CH.sub.2Ph H CN H H 516 4 CH.sub.2Ph H CN H H 517 1 COMe H CN H H 518 2 COMe H CN H H 519 3 COMe H CN H H 520 4 COMe H CN H H 521 1 CO.sub.2Me H CN H H 522 2 CO.sub.2Me H CN H H 523 3 CO.sub.2Me H CN H H 524 4 CO.sub.2Me H CN H H 525 1 CO.sub.2tBu H CN H H 526 2 CO.sub.2tBu H CN H H 527 3 CO.sub.2tBu H CN H H 528 4 CO.sub.2tBu H CN H H 529 1 CONHMe H CN H H 530 2 CONHMe H CN H H 531 3 CONHMe H CN H H 532 4 CONHMe H CN H H 533 1 SO.sub.2Me H CN H H 534 2 SO.sub.2Me H CN H H 535 3 SO.sub.2Me H CN H H 536 4 SO.sub.2Me H CN H H 537 1 SO.sub.2NH.sub.2 H CN H H 538 2 SO.sub.2NH.sub.2 H CN H H 539 3 SO.sub.2NH.sub.2 H CN H H 540 4 SO.sub.2NH.sub.2 H CN H H 541 1 H OH H H H 542 2 H OH H H H 543 3 H OH H H H 544 4 H OH H H H 545 1 Me OH H H H 546 2 Me OH H H H 547 3 Me OH H H H 548 4 Me OH H H H 549 1 CH.sub.2Ph OH H H H 550 2 CH.sub.2Ph OH H H H 551 3 CH.sub.2Ph OH H H H 552 4 CH.sub.2Ph OH H H H 553 1 COMe OH H H H 554 2 COMe OH H H H 555 3 COMe OH H H H 556 4 COMe OH H H H 557 1 CO.sub.2Me OH H H H 558 2 CO.sub.2Me OH H H H 559 3 CO.sub.2Me OH H H H 560 4 CO.sub.2Me OH H H H 561 1 CO.sub.2tBu OH H H H 562 2 CO.sub.2tBu OH H H H 563 3 CO.sub.2tBu OH H H H 564 4 CO.sub.2tBu OH H H H 565 1 CONHMe OH H H H 566 2 CONHMe OH H H H 567 3 CONHMe OH H H H 568 4 CONHMe OH H H H 569 1 SO.sub.2Me OH H H H 570 2 SO.sub.2Me OH H H H 571 3 SO.sub.2Me OH H H H 572 4 SO.sub.2Me OH H H H 573 1 SO.sub.2NH.sub.2 OH H H H 574 2 SO.sub.2NH.sub.2 OH H H H 575 3 SO.sub.2NH.sub.2 OH H H H 576 4 SO.sub.2NH.sub.2 OH H H H 577 1 H OMe H H H 578 2 H OMe H H H 579 3 H OMe H H H 580 4 H OMe H H H 581 1 Me OMe H H H 582 2 Me OMe H H H 583 3 Me OMe H H H 584 4 Me OMe H H H 585 1 CH.sub.2Ph OMe H H H 586 2 CH.sub.2Ph OMe H H H 587 3 CH.sub.2Ph OMe H H H 588 4 CH.sub.2Ph OMe H H H 589 1 COMe OMe H H H 590 2 COMe OMe H H H 591 3 COMe OMe H H H 592 4 COMe OMe H H H 593 1 CO.sub.2Me OMe H H H 594 2 CO.sub.2Me OMe H H H 595 3 CO.sub.2Me OMe H H H 596 4 CO.sub.2Me OMe H H H 597 1 CO.sub.2tBu OMe H H H 598 2 CO.sub.2tBu OMe H H H 599 3 CO.sub.2tBu OMe H H H 600 4 CO.sub.2tBu OMe H H H 601 1 CONHMe OMe H H H 602 2 CONHMe OMe H H H 603 3 CONHMe OMe H H H 604 4 CONHMe OMe H H H 605 1 SO.sub.2Me OMe H H H 606 2 SO.sub.2Me OMe H H H 607 3 SO.sub.2Me OMe H H H 608 4 SO.sub.2Me OMe H H H 609 1 SO.sub.2NH.sub.2 OMe H H H 610 2 SO.sub.2NH.sub.2 OMe H H H 611 3 SO.sub.2NH.sub.2 OMe H H H 612 4 SO.sub.2NH.sub.2 OMe H H H 613 1 H Me H H H 614 2 H Me H H H 615 3 H Me H H H 616 4 H Me H H H 617 1 Me Me H H H 618 2 Me Me H H H 619 3 Me Me H H H 620 4 Me Me H H H 621 1 CH.sub.2Ph Me H H H 622 2 CH.sub.2Ph Me H H H 623 3 CH.sub.2Ph Me H H H 624 4 CH.sub.2Ph Me H H H 625 1 COMe Me H H H 626 2 COMe Me H H H 627 3 COMe Me H H H 628 4 COMe Me H H H 629 1 CO.sub.2Me Me H H H 630 2 CO.sub.2Me Me H H H 631 3 CO.sub.2Me Me H H H 632 4 CO.sub.2Me Me H H H 633 1 CO.sub.2tBu Me H H H 634 2 CO.sub.2tBu Me H H H 635 3 CO.sub.2tBu Me H H H 636 4 CO.sub.2tBu Me H H H 637 1 CONHMe Me H H H 638 2 CONHMe Me H H H 639 3 CONHMe Me H H H 640 4 CONHMe Me H H H 641 1 SO.sub.2Me Me H H H 642 2 SO.sub.2Me Me H H H 643 3 SO.sub.2Me Me H H H 644 4 SO.sub.2Me Me H H H 645 1 SO.sub.2NH.sub.2 Me H H H 646 2 SO.sub.2NH.sub.2 Me H H H 647 3 SO.sub.2NH.sub.2 Me H H H 648 4 SO.sub.2NH.sub.2 Me H H H 649 1 H CF.sub.3 H H H 650 2 H CF.sub.3 H H H 651 3 H CF.sub.3 H H H 652 4 H CF.sub.3 H H H 653 1 Me CF.sub.3 H H H 654 2 Me CF.sub.3 H H H 655 3 Me CF.sub.3 H H H 656 4 Me CF.sub.3 H H H 657 1 CH.sub.2Ph CF.sub.3 H H H 658 2 CH.sub.2Ph CF.sub.3 H H H 659 3 CH.sub.2Ph CF.sub.3 H H H 660 4 CH.sub.2Ph CF.sub.3 H H H 661 1 COMe CF.sub.3 H H H 662 2 COMe CF.sub.3 H H H 663 3 COMe CF.sub.3 H H H 664 4 COMe CF.sub.3 H H H 665 1 CO.sub.2Me CF.sub.3 H H H 666 2 CO.sub.2Me CF.sub.3 H H H 667 3 CO.sub.2Me CF.sub.3 H H H 668 4 CO.sub.2Me CF.sub.3 H H H 669 1 CO.sub.2tBu CF.sub.3 H H H 670 2 CO.sub.2tBu CF.sub.3 H H H 671 3 CO.sub.2tBu CF.sub.3 H H H 672 4 CO.sub.2tBu CF.sub.3 H H H 673 1 CONHMe CF.sub.3 H H H 674 2 CONHMe CF.sub.3 H H H 675 3 CONHMe CF.sub.3 H H H 676 4 CONHMe CF.sub.3 H H H 677 1 SO.sub.2Me CF.sub.3 H H H 678 2 SO.sub.2Me CF.sub.3 H H H 679 3 SO.sub.2Me CF.sub.3 H H H 680 4 SO.sub.2Me CF.sub.3 H H H 681 1 SO.sub.2NH.sub.2 CF.sub.3 H H H 682 2 SO.sub.2NH.sub.2 CF.sub.3 H H H 683 3 SO.sub.2NH.sub.2 CF.sub.3 H H H 684 4 SO.sub.2NH.sub.2 CF.sub.3 H H H 685 1 H F H H H 686 2 H F H H H 687 3 H F H H H 688 3 H F H H H 689 1 Me F H H H 690 2 Me F H H H 691 3 Me F H H H 692 4 Me F H H H 693 1 CH.sub.2Ph F H H H 694 2 CH.sub.2Ph F H H H 695 3 CH.sub.2Ph F H H H 696 4 CH.sub.2Ph F H H H 697 1 COMe F H H H 698 2 COMe F H H H 699 3 COMe F H H H 700 4 COMe F H H H 701 1 CO.sub.2Me F H H H 702 2 CO.sub.2Me F H H H 703 3 CO.sub.2Me F H H H 704 4 CO.sub.2Me F H H H 705 1 CO.sub.2tBu F H H H 706 2 CO.sub.2tBu F H H H 707 3 CO.sub.2tBu F H H H 708 4 CO.sub.2tBu F H H H 709 1 CONHMe F H H H 710 2 CONHMe F H H H 711 3 CONHMe F H H H 712 4 CONHMe F H H H 713 1 SO.sub.2Me F H H H 714 2 SO.sub.2Me F H H H 715 3 SO.sub.2Me F H H H 716 4 SO.sub.2Me F H H H 717 1 SO.sub.2NH.sub.2 F H H H 718 2 SO.sub.2NH.sub.2 F H H H 719 3 SO.sub.2NH.sub.2 F H H H 720 4 SO.sub.2NH.sub.2 F H H H 721 1 H Cl H H H 722 2 H Cl H H H 723 3 H Cl H H H 724 4 H Cl H H H 725 1 Me Cl H H H 726 2 Me Cl H H H 727 3 Me Cl H H H 728 4 Me Cl H H H 729 1 CH.sub.2Ph Cl H H H 730 2 CH.sub.2Ph Cl H H H 731 3 CH.sub.2Ph Cl H H H 732 4 CH.sub.2Ph Cl H H H 733 1 COMe Cl H H H 734 2 COMe Cl H H H 735 3 COMe Cl H H H 736 4 COMe Cl H H H 737 1 CO.sub.2Me Cl H H H 738 2 CO.sub.2Me Cl H H H 739 3 CO.sub.2Me Cl H H H 740 4 CO.sub.2Me Cl H H H 741 1 CO.sub.2tBu Cl H H H 742 2 CO.sub.2tBu Cl H H H 743 3 CO.sub.2tBu Cl H H H 744 4 CO.sub.2tBu Cl H H H 745 1 CONHMe Cl H H H 746 2 CONHMe Cl H H H 747 3 CONHMe Cl H H H 748 4 CONHMe Cl H H H 749 1 SO.sub.2Me Cl H H H 750 2 SO.sub.2Me Cl H H H 751 3 SO.sub.2Me Cl H H H 752 4 SO.sub.2Me Cl H H H 753 1 SO.sub.2NH.sub.2 Cl H H H 754 2 SO.sub.2NH.sub.2 Cl H H H 755 3 SO.sub.2NH.sub.2 Cl H H H 756 4 SO.sub.2NH.sub.2 Cl H H H 757 1 H CN H H H 758 2 H CN H H H 759 3 H CN H H H 760 4 H CN H H H 761 1 Me CN H H H 762 2 Me CN H H H 763 3 Me CN H H H 764 4 Me CN H H H 765 1 CH.sub.2Ph CN H H H 766 2 CH.sub.2Ph CN H H H 767 3 CH.sub.2Ph CN H H H 768 4 CH.sub.2Ph CN H H H 769 1 COMe CN H H H 770 2 COMe CN H H H 771 3 COMe CN H H H 772 4 COMe CN H H H 773 1 CO.sub.2Me CN H H H 774 2 CO.sub.2Me CN H H H 775 3 CO.sub.2Me CN H H H 776 4 CO.sub.2Me CN H H H 777 1 CO.sub.2tBu CN H H H 778 2 CO.sub.2tBu CN H H H 779 3 CO.sub.2tBu CN H H H 780 4 CO.sub.2tBu CN H H H 781 1 CONHMe CN H H H 782 2 CONHMe CN H H H 783 3 CONHMe CN H H H 784 4 CONHMe CN H H H 785 1 SO.sub.2Me CN H H H 786 2 SO.sub.2Me CN H H H 787 3 SO.sub.2Me CN H H H 788 4 SO.sub.2Me CN H H H 789 1 SO.sub.2NH.sub.2 CN H H H 790 2 SO.sub.2NH.sub.2 CN H H H 791 3 SO.sub.2NH.sub.2 CN H H H 792 4 SO.sub.2NH.sub.2 CN H H H 793 1 H H H H OH 794 2 H H H H OH 795 3 H H H H OH 796 4 H H H H OH 797 1 Me H H H OH 798 2 Me H H H OH 799 3 Me H H H OH 800 4 Me H H H OH 801 1 CH.sub.2Ph H H H OH 802 2 CH.sub.2Ph H H H OH 803 3 CH.sub.2Ph H H H OH 804 4 CH.sub.2Ph H H H OH 805 1 COMe H H H OH 806 2 COMe H H H OH 807 3 COMe H H H OH 808 4 COMe H H H OH 809 1 CO.sub.2Me H H H OH 810 2 CO.sub.2Me H H H OH 811 3 CO.sub.2Me H H H OH 812 4 CO.sub.2Me H H H OH 813 1 CO.sub.2tBu H H H OH 814 2 CO.sub.2tBu H H H OH 815 3 CO.sub.2tBu H H H OH 816 4 CO.sub.2tBu H H H OH 817 1 CONHMe H H H OH 818 2 CONHMe H H H OH 819 3 CONHMe H H H OH 820 4 CONHMe H H H OH 821 1 SO.sub.2Me H H H OH 822 2 SO.sub.2Me H H H OH 823 3 SO.sub.2Me H H H OH 824 4 SO.sub.2Me H H H OH 825 1 SO.sub.2NH.sub.2 H H H OH 826 2 SO.sub.2NH.sub.2 H H H OH 827 3 SO.sub.2NH.sub.2 H H H OH 828 4 SO.sub.2NH.sub.2 H H H OH 829 1 H H H H OMe 830 2 H H H H OMe 831 3 H H H H OMe 832 4 H H H H OMe 833 1 Me H H H OMe 834 2 Me H H H OMe 835 3 Me H H H OMe 836 4 Me H H H OMe 837 1 CH.sub.2Ph H H H OMe 838 2 CH.sub.2Ph H H H OMe 839 3 CH.sub.2Ph H H H OMe 840 4 CH.sub.2Ph H H H OMe 841 1 COMe H H H OMe 842 2 COMe H H H OMe 843 3 COMe H H H OMe 844 4 COMe H H H OMe 845 1 CO.sub.2Me H H H OMe 846 2 CO.sub.2Me H H H OMe 847 3 CO.sub.2Me H H H OMe 848 4 CO.sub.2Me H H H OMe 849 1 CO.sub.2tBu H H H OMe 850 2 CO.sub.2tBu H H H OMe 851 3 CO.sub.2tBu H H H OMe 852 4 CO.sub.2tBu H H H OMe 853 1 CONHMe H H H OMe 854 2 CONHMe H H H OMe 855 3 CONHMe H H H OMe 856 4 CONHMe H H H OMe 857 1 SO.sub.2Me H H H OMe 858 2 SO.sub.2Me H H H OMe 859 3 SO.sub.2Me H H H OMe 860 4 SO.sub.2Me H H H OMe 861 1 SO.sub.2NH.sub.2 H H H OMe 862 2 SO.sub.2NH.sub.2 H H H OMe 863 3 SO.sub.2NH.sub.2 H H H OMe 864 4 SO.sub.2NH.sub.2 H H H OMe 865 1 H H H H Me 866 2 H H H H Me 867 3 H H H H Me 868 4 H H H H Me 869 1 Me H H H Me 870 2 Me H H H Me 871 3 Me H H H Me 872 4 Me H H H Me 873 1 CH.sub.2Ph H H H Me 874 2 CH.sub.2Ph H H H Me 875 3 CH.sub.2Ph H H H Me 876 4 CH.sub.2Ph H H H Me 877 1 COMe H H H Me 878 2 COMe H H H Me 879 3 COMe H H H Me 880 4 COMe H H H Me 881 1 CO.sub.2Me H H H Me 882 2 CO.sub.2Me H H H Me 883 3 CO.sub.2Me H H H Me 884 4 CO.sub.2Me H H H Me 885 1 CO.sub.2tBu H H H Me 886 2 CO.sub.2tBu H H H Me 887 3 CO.sub.2tBu H H H Me 888 4 CO.sub.2tBu H H H Me 889 1 CONHMe H H H Me 890 2 CONHMe H H H Me 891 3 CONHMe H H H Me 892 4 CONHMe H H H Me 893 1 SO.sub.2Me H H H Me 894 2 SO.sub.2Me H H H Me 895 3 SO.sub.2Me H H H Me 896 4 SO.sub.2Me H H H Me 897 1 SO.sub.2NH.sub.2 H H H Me 898 2 SO.sub.2NH.sub.2 H H H Me 899 3 SO.sub.2NH.sub.2 H H H Me 900 4 SO.sub.2NH.sub.2 H H H Me 901 1 H H H H CF.sub.3 902 2 H H H H CF.sub.3 903 3 H H H H CF.sub.3 904 4 H H H H CF.sub.3 905 1 Me H H H CF.sub.3 906 2 Me H H H CF.sub.3 907 3 Me H H H CF.sub.3 908 4 Me H H H CF.sub.3 909 1 CH.sub.2Ph H H H CF.sub.3 910 2 CH.sub.2Ph H H H CF.sub.3 911 3 CH.sub.2Ph H H H CF.sub.3 912 4 CH.sub.2Ph H H H CF.sub.3 913 1 COMe H H H CF.sub.3 914 2 COMe H H H CF.sub.3 915 3 COMe H H H CF.sub.3 916 4 COMe H H H CF.sub.3 917 1 CO.sub.2Me H H H CF.sub.3 918 2 CO.sub.2Me H H H CF.sub.3 919 3 CO.sub.2Me H H H CF.sub.3 920 4 CO.sub.2Me H H H CF.sub.3 921 1 CO.sub.2tBu H H H CF.sub.3 922 2 CO.sub.2tBu H H H CF.sub.3 923 3 CO.sub.2tBu H H H CF.sub.3 924 4 CO.sub.2tBu H H H CF.sub.3 925 1 CONHMe H H H CF.sub.3 926 2 CONHMe H H H CF.sub.3 927 3 CONHMe H H H CF.sub.3 928 4 CONHMe H H H CF.sub.3 929 1 SO.sub.2Me H H H CF.sub.3 930 2 SO.sub.2Me H H H CF.sub.3 931 3 SO.sub.2Me H H H CF.sub.3 932 4 SO.sub.2Me H H H CF.sub.3 933 1 SO.sub.2NH.sub.2 H H H CF.sub.3 934 2 SO.sub.2NH.sub.2 H H H CF.sub.3 935 3 SO.sub.2NH.sub.2 H H H CF.sub.3 936 4 SO.sub.2NH.sub.2 H H H CF.sub.3 937 1 H H H H F 938 2 H H H H F 939 3 H H H H F 940 3 H H H H F 941 1 Me H H H F 942 2 Me H H H F 943 3 Me H H H F 944 4 Me H H H F 945 1 CH.sub.2Ph H H H F 946 2 CH.sub.2Ph H H H F 947 3 CH.sub.2Ph H H H F 948 4 CH.sub.2Ph H H H F 949 1 COMe H H H F 950 2 COMe H H H F 951 3 COMe H H H F 952 4 COMe H H H F 953 1 CO.sub.2Me H H H F 954 2 CO.sub.2Me H H H F 955 3 CO.sub.2Me H H H F 956 4 CO.sub.2Me H H H F 957 1 CO.sub.2tBu H H H F 958 2 CO.sub.2tBu H H H F 959 3 CO.sub.2tBu H H H F 960 4 CO.sub.2tBu H H H F 961 1 CONHMe H H H F 962 2 CONHMe H H H F 963 3 CONHMe H H H F 964 4 CONHMe H H H F 965 1 SO.sub.2Me H H H F 966 2 SO.sub.2Me H H H F 967 3 SO.sub.2Me H H H F 968 4 SO.sub.2Me H H H F 969 1 SO.sub.2NH.sub.2 H H H F 970 2 SO.sub.2NH.sub.2 H H H F 971 3 SO.sub.2NH.sub.2 H H H F 972 4 SO.sub.2NH.sub.2 H H H F 973 1 H H H H Cl 974 2 H H H H Cl 975 3 H H H H Cl 976 4 H H H H Cl 977 1 Me H H H Cl 978 2 Me H H H Cl 979 3 Me H H H Cl 980 4 Me H H H Cl 981 1 CH.sub.2Ph H H H Cl 982 2 CH.sub.2Ph H H H Cl 983 3 CH.sub.2Ph H H H Cl 984 4 CH.sub.2Ph H H H Cl 985 1 COMe H H H Cl 986 2 COMe H H H Cl 987 3 COMe H H H Cl 988 4 COMe H H H Cl 989 1 CO.sub.2Me H H H Cl 990 2 CO.sub.2Me H H H Cl 991 3 CO.sub.2Me H H H Cl 992 4 CO.sub.2Me H H H Cl 993 1 CO.sub.2tBu H H H Cl 994 2 CO.sub.2tBu H H H Cl 995 3 CO.sub.2tBu H H H Cl 996 4 CO.sub.2tBu H H H Cl 997 1 CONHMe H H H Cl 998 2 CONHMe H H H Cl 999 3 CONHMe H H H Cl 1000 4 CONHMe H H H Cl 1001 1 SO.sub.2Me H H H Cl 1002 2 SO.sub.2Me H H H Cl 1003 3 SO.sub.2Me H H H Cl 1004 4 SO.sub.2Me H H H Cl 1005 1 SO.sub.2NH.sub.2 H H H Cl 1006 2 SO.sub.2NH.sub.2 H H H Cl 1007 3 SO.sub.2NH.sub.2 H H H Cl 1008 4 SO.sub.2NH.sub.2 H H H Cl 1009 1 H H H H CN 1010 2 H H H H CN 1011 3 H H H H CN 1012 4 H H H H CN 1013 1 Me H H H CN 1014 2 Me H H H CN 1015 3 Me H H H CN 1016 4 Me H H H CN 1017 1 CH.sub.2Ph H H H CN 1018 2 CH.sub.2Ph H H H CN 1019 3 CH.sub.2Ph H H H CN 1020 4 CH.sub.2Ph H H H CN 1021 1 COMe H H H CN 1022 2 COMe H H H CN 1023 3 COMe H H H CN 1024 4 COMe H H H CN 1025 1 CO.sub.2Me H H H CN 1026 2 CO.sub.2Me H H H CN 1027 3 CO.sub.2Me H H H CN 1028 4 CO.sub.2Me H H H CN 1029 1 CO.sub.2tBu H H H CN 1030 2 CO.sub.2tBu H H H CN 1031 3 CO.sub.2tBu H H H CN 1032 4 CO.sub.2tBu H H H CN 1033 1 CONHMe H H H CN 1034 2 CONHMe H H H CN 1035 3 CONHMe H H H CN 1036 4 CONHMe H H H CN 1037 1 SO.sub.2Me H H H CN 1038 2 SO.sub.2Me H H H CN 1039 3 SO.sub.2Me H H H CN 1040 4 SO.sub.2Me H H H CN 1041 1 SO.sub.2NH.sub.2 H H H CN 1042 2 SO.sub.2NH.sub.2 H H H CN 1043 3 SO.sub.2NH.sub.2 H H H CN 1044 4 SO.sub.2NH.sub.2 H H H CN

    [2034] Exemplary embodiments include compounds having the formula (XXVII)

    ##STR00442##

    [2035] or a pharmaceutically acceptable salt form thereof defined herein below in Table 21.

    TABLE-US-00021 TABLE 21 Entry n R.sup.7 R.sup.20a R.sup.20b R.sup.20c R.sup.20d 1 1 H H H H H 2 2 H H H H H 3 3 H H H H H 4 4 H H H H H 5 1 Me H H H H 6 2 Me H H H H 7 3 Me H H H H 8 4 Me H H H H 9 1 CH.sub.2Ph H H H H 10 2 CH.sub.2Ph H H H H 11 3 CH.sub.2Ph H H H H 12 4 CH.sub.2Ph H H H H 13 1 COMe H H H H 14 2 COMe H H H H 15 3 COMe H H H H 16 4 COMe H H H H 17 1 CO.sub.2Me H H H H 18 2 CO.sub.2Me H H H H 19 3 CO.sub.2Me H H H H 20 4 CO.sub.2Me H H H H 21 1 CO.sub.2tBu H H H H 22 2 CO.sub.2tBu H H H H 23 3 CO.sub.2tBu H H H H 24 4 CO.sub.2tBu H H H H 25 1 CONHMe H H H H 26 2 CONHMe H H H H 27 3 CONHMe H H H H 28 4 CONHMe H H H H 29 1 SO.sub.2Me H H H H 30 2 SO.sub.2Me H H H H 31 3 SO.sub.2Me H H H H 32 4 SO.sub.2Me H H H H 33 1 SO.sub.2NH.sub.2 H H H H 34 2 SO.sub.2NH.sub.2 H H H H 35 3 SO.sub.2NH.sub.2 H H H H 36 4 SO.sub.2NH.sub.2 H H H H 37 1 H H H OH H 38 2 H H H OH H 39 3 H H H OH H 40 4 H H H OH H 41 1 Me H H OH H 42 2 Me H H OH H 43 3 Me H H OH H 44 4 Me H H OH H 45 1 CH.sub.2Ph H H OH H 46 2 CH.sub.2Ph H H OH H 47 3 CH.sub.2Ph H H OH H 48 4 CH.sub.2Ph H H OH H 49 1 COMe H H OH H 50 2 COMe H H OH H 51 3 COMe H H OH H 52 4 COMe H H OH H 53 1 CO.sub.2Me H H OH H 54 2 CO.sub.2Me H H OH H 55 3 CO.sub.2Me H H OH H 56 4 CO.sub.2Me H H OH H 57 1 CO.sub.2tBu H H OH H 58 2 CO.sub.2tBu H H OH H 59 3 CO.sub.2tBu H H OH H 60 4 CO.sub.2tBu H H OH H 61 1 CONHMe H H OH H 62 2 CONHMe H H OH H 63 3 CONHMe H H OH H 64 4 CONHMe H H OH H 65 1 SO.sub.2Me H H OH H 66 2 SO.sub.2Me H H OH H 67 3 SO.sub.2Me H H OH H 68 4 SO.sub.2Me H H OH H 69 1 SO.sub.2NH.sub.2 H H OH H 70 2 SO.sub.2NH.sub.2 H H OH H 71 3 SO.sub.2NH.sub.2 H H OH H 72 4 SO.sub.2NH.sub.2 H H OH H 73 1 H H H OMe H 74 2 H H H OMe H 75 3 H H H OMe H 76 4 H H H OMe H 77 1 Me H H OMe H 78 2 Me H H OMe H 79 3 Me H H OMe H 80 4 Me H H OMe H 81 1 CH.sub.2Ph H H OMe H 82 2 CH.sub.2Ph H H OMe H 83 3 CH.sub.2Ph H H OMe H 84 4 CH.sub.2Ph H H OMe H 85 1 COMe H H OMe H 86 2 COMe H H OMe H 87 3 COMe H H OMe H 88 4 COMe H H OMe H 89 1 CO.sub.2Me H H OMe H 90 2 CO.sub.2Me H H OMe H 91 3 CO.sub.2Me H H OMe H 92 4 CO.sub.2Me H H OMe H 93 1 CO.sub.2tBu H H OMe H 94 2 CO.sub.2tBu H H OMe H 95 3 CO.sub.2tBu H H OMe H 96 1 CO.sub.2tBu H H OMe H 97 1 CONHMe H H OMe H 98 2 CONHMe H H OMe H 99 3 CONHMe H H OMe H 100 4 CONHMe H H OMe H 101 1 SO.sub.2Me H H OMe H 102 2 SO.sub.2Me H H OMe H 103 3 SO.sub.2Me H H OMe H 104 4 SO.sub.2Me H H OMe H 105 1 SO.sub.2NH.sub.2 H H OMe H 106 2 SO.sub.2NH.sub.2 H H OMe H 107 3 SO.sub.2NH.sub.2 H H OMe H 108 4 SO.sub.2NH.sub.2 H H OMe H 109 1 H H H Me H 110 2 H H H Me H 111 3 H H H Me H 112 4 H H H Me H 113 1 Me H H Me H 114 2 Me H H Me H 115 3 Me H H Me H 116 4 Me H H Me H 117 1 CH.sub.2Ph H H Me H 118 2 CH.sub.2Ph H H Me H 119 3 CH.sub.2Ph H H Me H 120 4 CH.sub.2Ph H H Me H 121 1 COMe H H Me H 122 2 COMe H H Me H 123 3 COMe H H Me H 124 4 COMe H H Me H 125 1 CO.sub.2Me H H Me H 126 2 CO.sub.2Me H H Me H 127 3 CO.sub.2Me H H Me H 128 4 CO.sub.2Me H H Me H 129 1 CO.sub.2tBu H H Me H 130 2 CO.sub.2tBu H H Me H 131 3 CO.sub.2tBu H H Me H 132 4 CO.sub.2tBu H H Me H 133 1 CONHMe H H Me H 134 2 CONHMe H H Me H 135 3 CONHMe H H Me H 136 4 CONHMe H H Me H 137 1 SO.sub.2Me H H Me H 138 2 SO.sub.2Me H H Me H 139 3 SO.sub.2Me H H Me H 140 4 SO.sub.2Me H H Me H 141 1 SO.sub.2NH.sub.2 H H Me H 142 2 SO.sub.2NH.sub.2 H H Me H 143 3 SO.sub.2NH.sub.2 H H Me H 144 4 SO.sub.2NH.sub.2 H H Me H 145 1 H H H CF.sub.3 H 146 2 H H H CF.sub.3 H 147 3 H H H CF.sub.3 H 148 4 H H H CF.sub.3 H 149 1 Me H H CF.sub.3 H 150 2 Me H H CF.sub.3 H 151 3 Me H H CF.sub.3 H 152 4 Me H H CF.sub.3 H 153 1 CH.sub.2Ph H H CF.sub.3 H 154 2 CH.sub.2Ph H H CF.sub.3 H 155 3 CH.sub.2Ph H H CF.sub.3 H 156 4 CH.sub.2Ph H H CF.sub.3 H 157 1 COMe H H CF.sub.3 H 158 2 COMe H H CF.sub.3 H 159 3 COMe H H CF.sub.3 H 160 4 COMe H H CF.sub.3 H 161 1 CO.sub.2Me H H CF.sub.3 H 162 2 CO.sub.2Me H H CF.sub.3 H 163 3 CO.sub.2Me H H CF.sub.3 H 164 4 CO.sub.2Me H H CF.sub.3 H 165 1 CO.sub.2tBu H H CF.sub.3 H 166 2 CO.sub.2tBu H H CF.sub.3 H 167 3 CO.sub.2tBu H H CF.sub.3 H 168 4 CO.sub.2tBu H H CF.sub.3 H 169 1 CONHMe H H CF.sub.3 H 170 2 CONHMe H H CF.sub.3 H 171 3 CONHMe H H CF.sub.3 H 172 4 CONHMe H H CF.sub.3 H 173 1 SO.sub.2Me H H CF.sub.3 H 174 2 SO.sub.2Me H H CF.sub.3 H 175 3 SO.sub.2Me H H CF.sub.3 H 176 4 SO.sub.2Me H H CF.sub.3 H 177 1 SO.sub.2NH.sub.2 H H CF.sub.3 H 178 2 SO.sub.2NH.sub.2 H H CF.sub.3 H 179 3 SO.sub.2NH.sub.2 H H CF.sub.3 H 180 4 SO.sub.2NH.sub.2 H H CF.sub.3 H 181 1 H H H F H 182 2 H H H F H 183 3 H H H F H 184 4 H H H F H 185 1 Me H H F H 186 2 Me H H F H 187 3 Me H H F H 188 4 Me H H F H 189 1 CH.sub.2Ph H H F H 190 2 CH.sub.2Ph H H F H 191 3 CH.sub.2Ph H H F H 192 4 CH.sub.2Ph H H F H 193 1 COMe H H F H 194 2 COMe H H F H 195 3 COMe H H F H 196 4 COMe H H F H 197 1 CO.sub.2Me H H F H 198 2 CO.sub.2Me H H F H 199 3 CO.sub.2Me H H F H 200 4 CO.sub.2Me H H F H 201 1 CO.sub.2tBu H H F H 202 2 CO.sub.2tBu H H F H 203 3 CO.sub.2tBu H H F H 204 4 CO.sub.2tBu H H F H 205 1 CONHMe H H F H 206 2 CONHMe H H F H 207 3 CONHMe H H F H 208 4 CONHMe H H F H 209 1 SO.sub.2Me H H F H 210 2 SO.sub.2Me H H F H 211 3 SO.sub.2Me H H F H 212 4 SO.sub.2Me H H F H 213 1 SO.sub.2NH.sub.2 H H F H 214 2 SO.sub.2NH.sub.2 H H F H 215 3 SO.sub.2NH.sub.2 H H F H 216 4 SO.sub.2NH.sub.2 H H F H 217 1 H H H Cl H 218 2 H H H Cl H 219 3 H H H Cl H 220 4 H H H Cl H 221 1 Me H H Cl H 222 2 Me H H Cl H 223 3 Me H H Cl H 224 4 Me H H Cl H 225 1 CH.sub.2Ph H H Cl H 226 2 CH.sub.2Ph H H Cl H 227 3 CH.sub.2Ph H H Cl H 228 4 CH.sub.2Ph H H Cl H 229 1 COMe H H Cl H 230 2 COMe H H Cl H 231 3 COMe H H Cl H 232 4 COMe H H Cl H 233 1 CO.sub.2Me H H Cl H 234 2 CO.sub.2Me H H Cl H 235 3 CO.sub.2Me H H Cl H 236 4 CO.sub.2Me H H Cl H 237 1 CO.sub.2tBu H H Cl H 238 2 CO.sub.2tBu H H Cl H 239 3 CO.sub.2tBu H H Cl H 240 4 CO.sub.2tBu H H Cl H 241 1 CONHMe H H Cl H 242 2 CONHMe H H Cl H 243 3 CONHMe H H Cl H 244 4 CONHMe H H Cl H 245 1 SO.sub.2Me H H Cl H 246 2 SO.sub.2Me H H Cl H 247 3 SO.sub.2Me H H Cl H 248 4 SO.sub.2Me H H Cl H 249 1 SO.sub.2NH.sub.2 H H Cl H 250 2 SO.sub.2NH.sub.2 H H Cl H 251 3 SO.sub.2NH.sub.2 H H Cl H 252 4 SO.sub.2NH.sub.2 H H Cl H 253 1 H H H CN H 254 2 H H H CN H 255 3 H H H CN H 256 4 H H H CN H 257 1 Me H H CN H 258 2 Me H H CN H 259 3 Me H H CN H 260 4 Me H H CN H 261 1 CH.sub.2Ph H H CN H 262 2 CH.sub.2Ph H H CN H 263 3 CH.sub.2Ph H H CN H 264 4 CH.sub.2Ph H H CN H 265 1 COMe H H CN H 266 2 COMe H H CN H 267 3 COMe H H CN H 268 4 COMe H H CN H 269 1 CO.sub.2Me H H CN H 270 2 CO.sub.2Me H H CN H 271 3 CO.sub.2Me H H CN H 272 4 CO.sub.2Me H H CN H 273 1 CO.sub.2tBu H H CN H 274 2 CO.sub.2tBu H H CN H 275 3 CO.sub.2tBu H H CN H 276 4 CO.sub.2tBu H H CN H 277 1 CONHMe H H CN H 278 2 CONHMe H H CN H 279 3 CONHMe H H CN H 280 4 CONHMe H H CN H 281 1 SO.sub.2Me H H CN H 282 2 SO.sub.2Me H H CN H 283 3 SO.sub.2Me H H CN H 284 4 SO.sub.2Me H H CN H 285 1 SO.sub.2NH.sub.2 H H CN H 286 2 SO.sub.2NH.sub.2 H H CN H 287 3 SO.sub.2NH.sub.2 H H CN H 288 4 SO.sub.2NH.sub.2 H H CN H 289 1 H H OH H H 290 2 H H OH H H 291 3 H H OH H H 292 4 H H OH H H 293 1 Me H OH H H 294 2 Me H OH H H 295 3 Me H OH H H 296 4 Me H OH H H 297 1 CH.sub.2Ph H OH H H 298 2 CH.sub.2Ph H OH H H 299 3 CH.sub.2Ph H OH H H 300 4 CH.sub.2Ph H OH H H 301 1 COMe H OH H H 302 2 COMe H OH H H 303 3 COMe H OH H H 304 4 COMe H OH H H 305 1 CO.sub.2Me H OH H H 306 2 CO.sub.2Me H OH H H 307 3 CO.sub.2Me H OH H H 308 4 CO.sub.2Me H OH H H 309 1 CO.sub.2tBu H OH H H 310 2 CO.sub.2tBu H OH H H 311 3 CO.sub.2tBu H OH H H 312 4 CO.sub.2tBu H OH H H 313 1 CONHMe H OH H H 314 2 CONHMe H OH H H 315 3 CONHMe H OH H H 316 4 CONHMe H OH H H 317 1 SO.sub.2Me H OH H H 318 2 SO.sub.2Me H OH H H 319 3 SO.sub.2Me H OH H H 320 4 SO.sub.2Me H OH H H 321 1 SO.sub.2NH.sub.2 H OH H H 322 2 SO.sub.2NH.sub.2 H OH H H 323 3 SO.sub.2NH.sub.2 H OH H H 324 4 SO.sub.2NH.sub.2 H OH H H 325 1 H H OMe H H 326 2 H H OMe H H 327 3 H H OMe H H 328 4 H H OMe H H 329 1 Me H OMe H H 330 2 Me H OMe H H 331 3 Me H OMe H H 332 4 Me H OMe H H 333 1 CH.sub.2Ph H OMe H H 334 2 CH.sub.2Ph H OMe H H 335 3 CH.sub.2Ph H OMe H H 336 4 CH.sub.2Ph H OMe H H 337 1 COMe H OMe H H 338 2 COMe H OMe H H 339 3 COMe H OMe H H 340 4 COMe H OMe H H 341 1 CO.sub.2Me H OMe H H 342 2 CO.sub.2Me H OMe H H 343 3 CO.sub.2Me H OMe H H 344 4 CO.sub.2Me H OMe H H 345 1 CO.sub.2tBu H OMe H H 346 2 CO.sub.2tBu H OMe H H 347 3 CO.sub.2tBu H OMe H H 348 4 CO.sub.2tBu H OMe H H 349 1 CONHMe H OMe H H 350 2 CONHMe H OMe H H 351 3 CONHMe H OMe H H 352 4 CONHMe H OMe H H 353 1 SO.sub.2Me H OMe H H 354 2 SO.sub.2Me H OMe H H 355 3 SO.sub.2Me H OMe H H 356 4 SO.sub.2Me H OMe H H 357 1 SO.sub.2NH.sub.2 H OMe H H 358 2 SO.sub.2NH.sub.2 H OMe H H 359 3 SO.sub.2NH.sub.2 H OMe H H 360 4 SO.sub.2NH.sub.2 H OMe H H 361 1 H H Me H H 362 2 H H Me H H 363 3 H H Me H H 364 4 H H Me H H 365 1 Me H Me H H 366 2 Me H Me H H 367 3 Me H Me H H 368 4 Me H Me H H 369 1 CH.sub.2Ph H Me H H 370 2 CH.sub.2Ph H Me H H 371 3 CH.sub.2Ph H Me H H 372 4 CH.sub.2Ph H Me H H 373 1 COMe H Me H H 374 2 COMe H Me H H 375 3 COMe H Me H H 376 4 COMe H Me H H 377 1 CO.sub.2Me H Me H H 378 2 CO.sub.2Me H Me H H 379 3 CO.sub.2Me H Me H H 380 4 CO.sub.2Me H Me H H 381 1 CO.sub.2tBu H Me H H 382 2 CO.sub.2tBu H Me H H 383 3 CO.sub.2tBu H Me H H 384 4 CO.sub.2tBu H Me H H 385 1 CONHMe H Me H H 386 2 CONHMe H Me H H 387 3 CONHMe H Me H H 388 4 CONHMe H Me H H 389 1 SO.sub.2Me H Me H H 390 2 SO.sub.2Me H Me H H 391 3 SO.sub.2Me H Me H H 392 4 SO.sub.2Me H Me H H 393 1 SO.sub.2NH.sub.2 H Me H H 394 2 SO.sub.2NH.sub.2 H Me H H 395 3 SO.sub.2NH.sub.2 H Me H H 396 4 SO.sub.2NH.sub.2 H Me H H 397 1 H H CF.sub.3 H H 398 2 H H CF.sub.3 H H 399 3 H H CF.sub.3 H H 400 4 H H CF.sub.3 H H 401 1 Me H CF.sub.3 H H 402 2 Me H CF.sub.3 H H 403 3 Me H CF.sub.3 H H 404 4 Me H CF.sub.3 H H 405 1 CH.sub.2Ph H CF.sub.3 H H 406 2 CH.sub.2Ph H CF.sub.3 H H 407 3 CH.sub.2Ph H CF.sub.3 H H 408 4 CH.sub.2Ph H CF.sub.3 H H 409 1 COMe H CF.sub.3 H H 410 2 COMe H CF.sub.3 H H 411 3 COMe H CF.sub.3 H H 412 4 COMe H CF.sub.3 H H 413 1 CO.sub.2Me H CF.sub.3 H H 414 2 CO.sub.2Me H CF.sub.3 H H 415 3 CO.sub.2Me H CF.sub.3 H H 416 4 CO.sub.2Me H CF.sub.3 H H 417 1 CO.sub.2tBu H CF.sub.3 H H 418 2 CO.sub.2tBu H CF.sub.3 H H 419 3 CO.sub.2tBu H CF.sub.3 H H 420 4 CO.sub.2tBu H CF.sub.3 H H 421 1 CONHMe H CF.sub.3 H H 422 2 CONHMe H CF.sub.3 H H 423 3 CONHMe H CF.sub.3 H H 424 4 CONHMe H CF.sub.3 H H 425 1 SO.sub.2Me H CF.sub.3 H H 426 2 SO.sub.2Me H CF.sub.3 H H 427 3 SO.sub.2Me H CF.sub.3 H H 428 4 SO.sub.2Me H CF.sub.3 H H 429 1 SO.sub.2NH.sub.2 H CF.sub.3 H H 430 2 SO.sub.2NH.sub.2 H CF.sub.3 H H 431 3 SO.sub.2NH.sub.2 H CF.sub.3 H H 432 4 SO.sub.2NH.sub.2 H CF.sub.3 H H 433 1 H H F H H 434 2 H H F H H 435 3 H H F H H 436 3 H H F H H 437 1 Me H F H H 438 2 Me H F H H 439 3 Me H F H H 440 4 Me H F H H 441 1 CH.sub.2Ph H F H H 442 2 CH.sub.2Ph H F H H 443 3 CH.sub.2Ph H F H H 444 4 CH.sub.2Ph H F H H 445 1 COMe H F H H 446 2 COMe H F H H 447 3 COMe H F H H 448 4 COMe H F H H 449 1 CO.sub.2Me H F H H 450 2 CO.sub.2Me H F H H 451 3 CO.sub.2Me H F H H 452 4 CO.sub.2Me H F H H 453 1 CO.sub.2tBu H F H H 454 2 CO.sub.2tBu H F H H 455 3 CO.sub.2tBu H F H H 456 4 CO.sub.2tBu H F H H 457 1 CONHMe H F H H 458 2 CONHMe H F H H 459 3 CONHMe H F H H 460 4 CONHMe H F H H 461 1 SO.sub.2Me H F H H 462 2 SO.sub.2Me H F H H 463 3 SO.sub.2Me H F H H 464 4 SO.sub.2Me H F H H 465 1 SO.sub.2NH.sub.2 H F H H 466 2 SO.sub.2NH.sub.2 H F H H 467 3 SO.sub.2NH.sub.2 H F H H 468 4 SO.sub.2NH.sub.2 H F H H 469 1 H H Cl H H 470 2 H H Cl H H 471 3 H H Cl H H 472 4 H H Cl H H 473 1 Me H Cl H H 474 2 Me H Cl H H 475 3 Me H Cl H H 476 4 Me H Cl H H 477 1 CH.sub.2Ph H Cl H H 478 2 CH.sub.2Ph H Cl H H 479 3 CH.sub.2Ph H Cl H H 480 4 CH.sub.2Ph H Cl H H 481 1 COMe H Cl H H 482 2 COMe H Cl H H 483 3 COMe H Cl H H 484 4 COMe H Cl H H 485 1 CO.sub.2Me H Cl H H 486 2 CO.sub.2Me H Cl H H 487 3 CO.sub.2Me H Cl H H 488 4 CO.sub.2Me H Cl H H 489 1 CO.sub.2tBu H Cl H H 490 2 CO.sub.2tBu H Cl H H 491 3 CO.sub.2tBu H Cl H H 492 4 CO.sub.2tBu H Cl H H 493 1 CONHMe H Cl H H 494 2 CONHMe H Cl H H 495 3 CONHMe H Cl H H 496 4 CONHMe H Cl H H 497 1 SO.sub.2Me H Cl H H 498 2 SO.sub.2Me H Cl H H 499 3 SO.sub.2Me H Cl H H 500 4 SO.sub.2Me H Cl H H 501 1 SO.sub.2NH.sub.2 H Cl H H 502 2 SO.sub.2NH.sub.2 H Cl H H 503 3 SO.sub.2NH.sub.2 H Cl H H 504 4 SO.sub.2NH.sub.2 H Cl H H 505 1 H H CN H H 506 2 H H CN H H 507 3 H H CN H H 508 4 H H CN H H 509 1 Me H CN H H 510 2 Me H CN H H 511 3 Me H CN H H 512 4 Me H CN H H 513 1 CH.sub.2Ph H CN H H 514 2 CH.sub.2Ph H CN H H 515 3 CH.sub.2Ph H CN H H 516 4 CH.sub.2Ph H CN H H 517 1 COMe H CN H H 518 2 COMe H CN H H 519 3 COMe H CN H H 520 4 COMe H CN H H 521 1 CO.sub.2Me H CN H H 522 2 CO.sub.2Me H CN H H 523 3 CO.sub.2Me H CN H H 524 4 CO.sub.2Me H CN H H 525 1 CO.sub.2tBu H CN H H 526 2 CO.sub.2tBu H CN H H 527 3 CO.sub.2tBu H CN H H 528 4 CO.sub.2tBu H CN H H 529 1 CONHMe H CN H H 530 2 CONHMe H CN H H 531 3 CONHMe H CN H H 532 4 CONHMe H CN H H 533 1 SO.sub.2Me H CN H H 534 2 SO.sub.2Me H CN H H 535 3 SO.sub.2Me H CN H H 536 4 SO.sub.2Me H CN H H 537 1 SO.sub.2NH.sub.2 H CN H H 538 2 SO.sub.2NH.sub.2 H CN H H 539 3 SO.sub.2NH.sub.2 H CN H H 540 4 SO.sub.2NH.sub.2 H CN H H 541 1 H OH H H H 542 2 H OH H H H 543 3 H OH H H H 544 4 H OH H H H 545 1 Me OH H H H 546 2 Me OH H H H 547 3 Me OH H H H 548 4 Me OH H H H 549 1 CH.sub.2Ph OH H H H 550 2 CH.sub.2Ph OH H H H 551 3 CH.sub.2Ph OH H H H 552 4 CH.sub.2Ph OH H H H 553 1 COMe OH H H H 554 2 COMe OH H H H 555 3 COMe OH H H H 556 4 COMe OH H H H 557 1 CO.sub.2Me OH H H H 558 2 CO.sub.2Me OH H H H 559 3 CO.sub.2Me OH H H H 560 4 CO.sub.2Me OH H H H 561 1 CO.sub.2tBu OH H H H 562 2 CO.sub.2tBu OH H H H 563 3 CO.sub.2tBu OH H H H 564 4 CO.sub.2tBu OH H H H 565 1 CONHMe OH H H H 566 2 CONHMe OH H H H 567 3 CONHMe OH H H H 568 4 CONHMe OH H H H 569 1 SO.sub.2Me OH H H H 570 2 SO.sub.2Me OH H H H 571 3 SO.sub.2Me OH H H H 572 4 SO.sub.2Me OH H H H 573 1 SO.sub.2NH.sub.2 OH H H H 574 2 SO.sub.2NH.sub.2 OH H H H 575 3 SO.sub.2NH.sub.2 OH H H H 576 4 SO.sub.2NH.sub.2 OH H H H 577 1 H OMe H H H 578 2 H OMe H H H 579 3 H OMe H H H 580 4 H OMe H H H 581 1 Me OMe H H H 582 2 Me OMe H H H 583 3 Me OMe H H H 584 4 Me OMe H H H 585 1 CH.sub.2Ph OMe H H H 586 2 CH.sub.2Ph OMe H H H 587 3 CH.sub.2Ph OMe H H H 588 4 CH.sub.2Ph OMe H H H 589 1 COMe OMe H H H 590 2 COMe OMe H H H 591 3 COMe OMe H H H 592 4 COMe OMe H H H 593 1 CO.sub.2Me OMe H H H 594 2 CO.sub.2Me OMe H H H 595 3 CO.sub.2Me OMe H H H 596 4 CO.sub.2Me OMe H H H 597 1 CO.sub.2tBu OMe H H H 598 2 CO.sub.2tBu OMe H H H 599 3 CO.sub.2tBu OMe H H H 600 4 CO.sub.2tBu OMe H H H 601 1 CONHMe OMe H H H 602 2 CONHMe OMe H H H 603 3 CONHMe OMe H H H 604 4 CONHMe OMe H H H 605 1 SO.sub.2Me OMe H H H 606 2 SO.sub.2Me OMe H H H 607 3 SO.sub.2Me OMe H H H 608 4 SO.sub.2Me OMe H H H 609 1 SO.sub.2NH.sub.2 OMe H H H 610 2 SO.sub.2NH.sub.2 OMe H H H 611 3 SO.sub.2NH.sub.2 OMe H H H 612 4 SO.sub.2NH.sub.2 OMe H H H 613 1 H Me H H H 614 2 H Me H H H 615 3 H Me H H H 616 4 H Me H H H 617 1 Me Me H H H 618 2 Me Me H H H 619 3 Me Me H H H 620 4 Me Me H H H 621 1 CH.sub.2Ph Me H H H 622 2 CH.sub.2Ph Me H H H 623 3 CH.sub.2Ph Me H H H 624 4 CH.sub.2Ph Me H H H 625 1 COMe Me H H H 626 2 COMe Me H H H 627 3 COMe Me H H H 628 4 COMe Me H H H 629 1 CO.sub.2Me Me H H H 630 2 CO.sub.2Me Me H H H 631 3 CO.sub.2Me Me H H H 632 4 CO.sub.2Me Me H H H 633 1 CO.sub.2tBu Me H H H 634 2 CO.sub.2tBu Me H H H 635 3 CO.sub.2tBu Me H H H 636 4 CO.sub.2tBu Me H H H 637 1 CONHMe Me H H H 638 2 CONHMe Me H H H 639 3 CONHMe Me H H H 640 4 CONHMe Me H H H 641 1 SO.sub.2Me Me H H H 642 2 SO.sub.2Me Me H H H 643 3 SO.sub.2Me Me H H H 644 4 SO.sub.2Me Me H H H 645 1 SO.sub.2NH.sub.2 Me H H H 646 2 SO.sub.2NH.sub.2 Me H H H 647 3 SO.sub.2NH.sub.2 Me H H H 648 4 SO.sub.2NH.sub.2 Me H H H 649 1 H CF.sub.3 H H H 650 2 H CF.sub.3 H H H 651 3 H CF.sub.3 H H H 652 4 H CF.sub.3 H H H 653 1 Me CF.sub.3 H H H 654 2 Me CF.sub.3 H H H 655 3 Me CF.sub.3 H H H 656 4 Me CF.sub.3 H H H 657 1 CH.sub.2Ph CF.sub.3 H H H 658 2 CH.sub.2Ph CF.sub.3 H H H 659 3 CH.sub.2Ph CF.sub.3 H H H 660 4 CH.sub.2Ph CF.sub.3 H H H 661 1 COMe CF.sub.3 H H H 662 2 COMe CF.sub.3 H H H 663 3 COMe CF.sub.3 H H H 664 4 COMe CF.sub.3 H H H 665 1 CO.sub.2Me CF.sub.3 H H H 666 2 CO.sub.2Me CF.sub.3 H H H 667 3 CO.sub.2Me CF.sub.3 H H H 668 4 CO.sub.2Me CF.sub.3 H H H 669 1 CO.sub.2tBu CF.sub.3 H H H 670 2 CO.sub.2tBu CF.sub.3 H H H 671 3 CO.sub.2tBu CF.sub.3 H H H 672 4 CO.sub.2tBu CF.sub.3 H H H 673 1 CONHMe CF.sub.3 H H H 674 2 CONHMe CF.sub.3 H H H 675 3 CONHMe CF.sub.3 H H H 676 4 CONHMe CF.sub.3 H H H 677 1 SO.sub.2Me CF.sub.3 H H H 678 2 SO.sub.2Me CF.sub.3 H H H 679 3 SO.sub.2Me CF.sub.3 H H H 680 4 SO.sub.2Me CF.sub.3 H H H 681 1 SO.sub.2NH.sub.2 CF.sub.3 H H H 682 2 SO.sub.2NH.sub.2 CF.sub.3 H H H 683 3 SO.sub.2NH.sub.2 CF.sub.3 H H H 684 4 SO.sub.2NH.sub.2 CF.sub.3 H H H 685 1 H F H H H 686 2 H F H H H 687 3 H F H H H 688 3 H F H H H 689 1 Me F H H H 690 2 Me F H H H 691 3 Me F H H H 692 4 Me F H H H 693 1 CH.sub.2Ph F H H H 694 2 CH.sub.2Ph F H H H 695 3 CH.sub.2Ph F H H H 696 4 CH.sub.2Ph F H H H 697 1 COMe F H H H 698 2 COMe F H H H 699 3 COMe F H H H 700 4 COMe F H H H 701 1 CO.sub.2Me F H H H 702 2 CO.sub.2Me F H H H 703 3 CO.sub.2Me F H H H 704 4 CO.sub.2Me F H H H 705 1 CO.sub.2tBu F H H H 706 2 CO.sub.2tBu F H H H 707 3 CO.sub.2tBu F H H H 708 4 CO.sub.2tBu F H H H 709 1 CONHMe F H H H 710 2 CONHMe F H H H 711 3 CONHMe F H H H 712 4 CONHMe F H H H 713 1 SO.sub.2Me F H H H 714 2 SO.sub.2Me F H H H 715 3 SO.sub.2Me F H H H 716 4 SO.sub.2Me F H H H 717 1 SO.sub.2NH.sub.2 F H H H 718 2 SO.sub.2NH.sub.2 F H H H 719 3 SO.sub.2NH.sub.2 F H H H 720 4 SO.sub.2NH.sub.2 F H H H 721 1 H Cl H H H 722 2 H Cl H H H 723 3 H Cl H H H 724 4 H Cl H H H 725 1 Me Cl H H H 726 2 Me Cl H H H 727 3 Me Cl H H H 728 4 Me Cl H H H 729 1 CH.sub.2Ph Cl H H H 730 2 CH.sub.2Ph Cl H H H 731 3 CH.sub.2Ph Cl H H H 732 4 CH.sub.2Ph Cl H H H 733 1 COMe Cl H H H 734 2 COMe Cl H H H 735 3 COMe Cl H H H 736 4 COMe Cl H H H 737 1 CO.sub.2Me Cl H H H 738 2 CO.sub.2Me Cl H H H 739 3 CO.sub.2Me Cl H H H 740 4 CO.sub.2Me Cl H H H 741 1 CO.sub.2tBu Cl H H H 742 2 CO.sub.2tBu Cl H H H 743 3 CO.sub.2tBu Cl H H H 744 4 CO.sub.2tBu Cl H H H 745 1 CONHMe Cl H H H 746 2 CONHMe Cl H H H 747 3 CONHMe Cl H H H 748 4 CONHMe Cl H H H 749 1 SO.sub.2Me Cl H H H 750 2 SO.sub.2Me Cl H H H 751 3 SO.sub.2Me Cl H H H 752 4 SO.sub.2Me Cl H H H 753 1 SO.sub.2NH.sub.2 Cl H H H 754 2 SO.sub.2NH.sub.2 Cl H H H 755 3 SO.sub.2NH.sub.2 Cl H H H 756 4 SO.sub.2NH.sub.2 Cl H H H 757 1 H CN H H H 758 2 H CN H H H 759 3 H CN H H H 760 4 H CN H H H 761 1 Me CN H H H 762 2 Me CN H H H 763 3 Me CN H H H 764 4 Me CN H H H 765 1 CH.sub.2Ph CN H H H 766 2 CH.sub.2Ph CN H H H 767 3 CH.sub.2Ph CN H H H 768 4 CH.sub.2Ph CN H H H 769 1 COMe CN H H H 770 2 COMe CN H H H 771 3 COMe CN H H H 772 4 COMe CN H H H 773 1 CO.sub.2Me CN H H H 774 2 CO.sub.2Me CN H H H 775 3 CO.sub.2Me CN H H H 776 4 CO.sub.2Me CN H H H 777 1 CO.sub.2tBu CN H H H 778 2 CO.sub.2tBu CN H H H 779 3 CO.sub.2tBu CN H H H 780 4 CO.sub.2tBu CN H H H 781 1 CONHMe CN H H H 782 2 CONHMe CN H H H 783 3 CONHMe CN H H H 784 4 CONHMe CN H H H 785 1 SO.sub.2Me CN H H H 786 2 SO.sub.2Me CN H H H 787 3 SO.sub.2Me CN H H H 788 4 SO.sub.2Me CN H H H 789 1 SO.sub.2NH.sub.2 CN H H H 790 2 SO.sub.2NH.sub.2 CN H H H 791 3 SO.sub.2NH.sub.2 CN H H H 792 4 SO.sub.2NH.sub.2 CN H H H 793 1 H H H H OH 794 2 H H H H OH 795 3 H H H H OH 796 4 H H H H OH 797 1 Me H H H OH 798 2 Me H H H OH 799 3 Me H H H OH 800 4 Me H H H OH 801 1 CH.sub.2Ph H H H OH 802 2 CH.sub.2Ph H H H OH 803 3 CH.sub.2Ph H H H OH 804 4 CH.sub.2Ph H H H OH 805 1 COMe H H H OH 806 2 COMe H H H OH 807 3 COMe H H H OH 808 4 COMe H H H OH 809 1 CO.sub.2Me H H H OH 810 2 CO.sub.2Me H H H OH 811 3 CO.sub.2Me H H H OH 812 4 CO.sub.2Me H H H OH 813 1 CO.sub.2tBu H H H OH 814 2 CO.sub.2tBu H H H OH 815 3 CO.sub.2tBu H H H OH 816 4 CO.sub.2tBu H H H OH 817 1 CONHMe H H H OH 818 2 CONHMe H H H OH 819 3 CONHMe H H H OH 820 4 CONHMe H H H OH 821 1 SO.sub.2Me H H H OH 822 2 SO.sub.2Me H H H OH 823 3 SO.sub.2Me H H H OH 824 4 SO.sub.2Me H H H OH 825 1 SO.sub.2NH.sub.2 H H H OH 826 2 SO.sub.2NH.sub.2 H H H OH 827 3 SO.sub.2NH.sub.2 H H H OH 828 4 SO.sub.2NH.sub.2 H H H OH 829 1 H H H H OMe 830 2 H H H H OMe 831 3 H H H H OMe 832 4 H H H H OMe 833 1 Me H H H OMe 834 2 Me H H H OMe 835 3 Me H H H OMe 836 4 Me H H H OMe 837 1 CH.sub.2Ph H H H OMe 838 2 CH.sub.2Ph H H H OMe 839 3 CH.sub.2Ph H H H OMe 840 4 CH.sub.2Ph H H H OMe 841 1 COMe H H H OMe 842 2 COMe H H H OMe 843 3 COMe H H H OMe 844 4 COMe H H H OMe 845 1 CO.sub.2Me H H H OMe 846 2 CO.sub.2Me H H H OMe 847 3 CO.sub.2Me H H H OMe 848 4 CO.sub.2Me H H H OMe 849 1 CO.sub.2tBu H H H OMe 850 2 CO.sub.2tBu H H H OMe 851 3 CO.sub.2tBu H H H OMe 852 4 CO.sub.2tBu H H H OMe 853 1 CONHMe H H H OMe 854 2 CONHMe H H H OMe 855 3 CONHMe H H H OMe 856 4 CONHMe H H H OMe 857 1 SO.sub.2Me H H H OMe 858 2 SO.sub.2Me H H H OMe 859 3 SO.sub.2Me H H H OMe 860 4 SO.sub.2Me H H H OMe 861 1 SO.sub.2NH.sub.2 H H H OMe 862 2 SO.sub.2NH.sub.2 H H H OMe 863 3 SO.sub.2NH.sub.2 H H H OMe 864 4 SO.sub.2NH.sub.2 H H H OMe 865 1 H H H H Me 866 2 H H H H Me 867 3 H H H H Me 868 4 H H H H Me 869 1 Me H H H Me 870 2 Me H H H Me 871 3 Me H H H Me 872 4 Me H H H Me 873 1 CH.sub.2Ph H H H Me 874 2 CH.sub.2Ph H H H Me 875 3 CH.sub.2Ph H H H Me 876 4 CH.sub.2Ph H H H Me 877 1 COMe H H H Me 878 2 COMe H H H Me 879 3 COMe H H H Me 880 4 COMe H H H Me 881 1 CO.sub.2Me H H H Me 882 2 CO.sub.2Me H H H Me 883 3 CO.sub.2Me H H H Me 884 4 CO.sub.2Me H H H Me 885 1 CO.sub.2tBu H H H Me 886 2 CO.sub.2tBu H H H Me 887 3 CO.sub.2tBu H H H Me 888 4 CO.sub.2tBu H H H Me 889 1 CONHMe H H H Me 890 2 CONHMe H H H Me 891 3 CONHMe H H H Me 892 4 CONHMe H H H Me 893 1 SO.sub.2Me H H H Me 894 2 SO.sub.2Me H H H Me 895 3 SO.sub.2Me H H H Me 896 4 SO.sub.2Me H H H Me 897 1 SO.sub.2NH.sub.2 H H H Me 898 2 SO.sub.2NH.sub.2 H H H Me 899 3 SO.sub.2NH.sub.2 H H H Me 900 4 SO.sub.2NH.sub.2 H H H Me 901 1 H H H H CF.sub.3 902 2 H H H H CF.sub.3 903 3 H H H H CF.sub.3 904 4 H H H H CF.sub.3 905 1 Me H H H CF.sub.3 906 2 Me H H H CF.sub.3 907 3 Me H H H CF.sub.3 908 4 Me H H H CF.sub.3 909 1 CH.sub.2Ph H H H CF.sub.3 910 2 CH.sub.2Ph H H H CF.sub.3 911 3 CH.sub.2Ph H H H CF.sub.3 912 4 CH.sub.2Ph H H H CF.sub.3 913 1 COMe H H H CF.sub.3 914 2 COMe H H H CF.sub.3 915 3 COMe H H H CF.sub.3 916 4 COMe H H H CF.sub.3 917 1 CO.sub.2Me H H H CF.sub.3 918 2 CO.sub.2Me H H H CF.sub.3 919 3 CO.sub.2Me H H H CF.sub.3 920 4 CO.sub.2Me H H H CF.sub.3 921 1 CO.sub.2tBu H H H CF.sub.3 922 2 CO.sub.2tBu H H H CF.sub.3 923 3 CO.sub.2tBu H H H CF.sub.3 924 4 CO.sub.2tBu H H H CF.sub.3 925 1 CONHMe H H H CF.sub.3 926 2 CONHMe H H H CF.sub.3 927 3 CONHMe H H H CF.sub.3 928 4 CONHMe H H H CF.sub.3 929 1 SO.sub.2Me H H H CF.sub.3 930 2 SO.sub.2Me H H H CF.sub.3 931 3 SO.sub.2Me H H H CF.sub.3 932 4 SO.sub.2Me H H H CF.sub.3 933 1 SO.sub.2NH.sub.2 H H H CF.sub.3 934 2 SO.sub.2NH.sub.2 H H H CF.sub.3 935 3 SO.sub.2NH.sub.2 H H H CF.sub.3 936 4 SO.sub.2NH.sub.2 H H H CF.sub.3 937 1 H H H H F 938 2 H H H H F 939 3 H H H H F 940 3 H H H H F 941 1 Me H H H F 942 2 Me H H H F 943 3 Me H H H F 944 4 Me H H H F 945 1 CH.sub.2Ph H H H F 946 2 CH.sub.2Ph H H H F 947 3 CH.sub.2Ph H H H F 948 4 CH.sub.2Ph H H H F 949 1 COMe H H H F 950 2 COMe H H H F 951 3 COMe H H H F 952 4 COMe H H H F 953 1 CO.sub.2Me H H H F 954 2 CO.sub.2Me H H H F 955 3 CO.sub.2Me H H H F 956 4 CO.sub.2Me H H H F 957 1 CO.sub.2tBu H H H F 958 2 CO.sub.2tBu H H H F 959 3 CO.sub.2tBu H H H F 960 4 CO.sub.2tBu H H H F 961 1 CONHMe H H H F 962 2 CONHMe H H H F 963 3 CONHMe H H H F 964 4 CONHMe H H H F 965 1 SO.sub.2Me H H H F 966 2 SO.sub.2Me H H H F 967 3 SO.sub.2Me H H H F 968 4 SO.sub.2Me H H H F 969 1 SO.sub.2NH.sub.2 H H H F 970 2 SO.sub.2NH.sub.2 H H H F 971 3 SO.sub.2NH.sub.2 H H H F 972 4 SO.sub.2NH.sub.2 H H H F 973 1 H H H H Cl 974 2 H H H H Cl 975 3 H H H H Cl 976 4 H H H H Cl 977 1 Me H H H Cl 978 2 Me H H H Cl 979 3 Me H H H Cl 980 4 Me H H H Cl 981 1 CH.sub.2Ph H H H Cl 982 2 CH.sub.2Ph H H H Cl 983 3 CH.sub.2Ph H H H Cl 984 4 CH.sub.2Ph H H H Cl 985 1 COMe H H H Cl 986 2 COMe H H H Cl 987 3 COMe H H H Cl 988 4 COMe H H H Cl 989 1 CO.sub.2Me H H H Cl 990 2 CO.sub.2Me H H H Cl 991 3 CO.sub.2Me H H H Cl 992 4 CO.sub.2Me H H H Cl 993 1 CO.sub.2tBu H H H Cl 994 2 CO.sub.2tBu H H H Cl 995 3 CO.sub.2tBu H H H Cl 996 4 CO.sub.2tBu H H H Cl 997 1 CONHMe H H H Cl 998 2 CONHMe H H H Cl 999 3 CONHMe H H H Cl 1000 4 CONHMe H H H Cl 1001 1 SO.sub.2Me H H H Cl 1002 2 SO.sub.2Me H H H Cl 1003 3 SO.sub.2Me H H H Cl 1004 4 SO.sub.2Me H H H Cl 1005 1 SO.sub.2NH.sub.2 H H H Cl 1006 2 SO.sub.2NH.sub.2 H H H Cl 1007 3 SO.sub.2NH.sub.2 H H H Cl 1008 4 SO.sub.2NH.sub.2 H H H Cl 1009 1 H H H H CN 1010 2 H H H H CN 1011 3 H H H H CN 1012 4 H H H H CN 1013 1 Me H H H CN 1014 2 Me H H H CN 1015 3 Me H H H CN 1016 4 Me H H H CN 1017 1 CH.sub.2Ph H H H CN 1018 2 CH.sub.2Ph H H H CN 1019 3 CH.sub.2Ph H H H CN 1020 4 CH.sub.2Ph H H H CN 1021 1 COMe H H H CN 1022 2 COMe H H H CN 1023 3 COMe H H H CN 1024 4 COMe H H H CN 1025 1 CO.sub.2Me H H H CN 1026 2 CO.sub.2Me H H H CN 1027 3 CO.sub.2Me H H H CN 1028 4 CO.sub.2Me H H H CN 1029 1 CO.sub.2tBu H H H CN 1030 2 CO.sub.2tBu H H H CN 1031 3 CO.sub.2tBu H H H CN 1032 4 CO.sub.2tBu H H H CN 1033 1 CONHMe H H H CN 1034 2 CONHMe H H H CN 1035 3 CONHMe H H H CN 1036 4 CONHMe H H H CN 1037 1 SO.sub.2Me H H H CN 1038 2 SO.sub.2Me H H H CN 1039 3 SO.sub.2Me H H H CN 1040 4 SO.sub.2Me H H H CN 1041 1 SO.sub.2NH.sub.2 H H H CN 1042 2 SO.sub.2NH.sub.2 H H H CN 1043 3 SO.sub.2NH.sub.2 H H H CN 1044 4 SO.sub.2NH.sub.2 H H H CN

    [2036] Exemplary embodiments include compounds having the formula (XXVIII)

    ##STR00443##

    [2037] or a pharmaceutically acceptable salt form thereof defined herein below in Table 22.

    TABLE-US-00022 TABLE 22 Entry n R.sup.7 R.sup.20a R.sup.20b R.sup.20c R.sup.20e 1 1 H H H H H 2 2 H H H H H 3 3 H H H H H 4 4 H H H H H 5 1 Me H H H H 6 2 Me H H H H 7 3 Me H H H H 8 4 Me H H H H 9 1 CH.sub.2Ph H H H H 10 2 CH.sub.2Ph H H H H 11 3 CH.sub.2Ph H H H H 12 4 CH.sub.2Ph H H H H 13 1 COMe H H H H 14 2 COMe H H H H 15 3 COMe H H H H 16 4 COMe H H H H 17 1 CO.sub.2Me H H H H 18 2 CO.sub.2Me H H H H 19 3 CO.sub.2Me H H H H 20 4 CO.sub.2Me H H H H 21 1 CO.sub.2tBu H H H H 22 2 CO.sub.2tBu H H H H 23 3 CO.sub.2tBu H H H H 24 4 CO.sub.2tBu H H H H 25 1 CONHMe H H H H 26 2 CONHMe H H H H 27 3 CONHMe H H H H 28 4 CONHMe H H H H 29 1 SO.sub.2Me H H H H 30 2 SO.sub.2Me H H H H 31 3 SO.sub.2Me H H H H 32 4 SO.sub.2Me H H H H 33 1 SO.sub.2NH.sub.2 H H H H 34 2 SO.sub.2NH.sub.2 H H H H 35 3 SO.sub.2NH.sub.2 H H H H 36 4 SO.sub.2NH.sub.2 H H H H 37 1 H H H OH H 38 2 H H H OH H 39 3 H H H OH H 40 4 H H H OH H 41 1 Me H H OH H 42 2 Me H H OH H 43 3 Me H H OH H 44 4 Me H H OH H 45 1 CH.sub.2Ph H H OH H 46 2 CH.sub.2Ph H H OH H 47 3 CH.sub.2Ph H H OH H 48 4 CH.sub.2Ph H H OH H 49 1 COMe H H OH H 50 2 COMe H H OH H 51 3 COMe H H OH H 52 4 COMe H H OH H 53 1 CO.sub.2Me H H OH H 54 2 CO.sub.2Me H H OH H 55 3 CO.sub.2Me H H OH H 56 4 CO.sub.2Me H H OH H 57 1 CO.sub.2tBu H H OH H 58 2 CO.sub.2tBu H H OH H 59 3 CO.sub.2tBu H H OH H 60 4 CO.sub.2tBu H H OH H 61 1 CONHMe H H OH H 62 2 CONHMe H H OH H 63 3 CONHMe H H OH H 64 4 CONHMe H H OH H 65 1 SO.sub.2Me H H OH H 66 2 SO.sub.2Me H H OH H 67 3 SO.sub.2Me H H OH H 68 4 SO.sub.2Me H H OH H 69 1 SO.sub.2NH.sub.2 H H OH H 70 2 SO.sub.2NH.sub.2 H H OH H 71 3 SO.sub.2NH.sub.2 H H OH H 72 4 SO.sub.2NH.sub.2 H H OH H 73 1 H H H OMe H 74 2 H H H OMe H 75 3 H H H OMe H 76 4 H H H OMe H 77 1 Me H H OMe H 78 2 Me H H OMe H 79 3 Me H H OMe H 80 4 Me H H OMe H 81 1 CH.sub.2Ph H H OMe H 82 2 CH.sub.2Ph H H OMe H 83 3 CH.sub.2Ph H H OMe H 84 4 CH.sub.2Ph H H OMe H 85 1 COMe H H OMe H 86 2 COMe H H OMe H 87 3 COMe H H OMe H 88 4 COMe H H OMe H 89 1 CO.sub.2Me H H OMe H 90 2 CO.sub.2Me H H OMe H 91 3 CO.sub.2Me H H OMe H 92 4 CO.sub.2Me H H OMe H 93 1 CO.sub.2tBu H H OMe H 94 2 CO.sub.2tBu H H OMe H 95 3 CO.sub.2tBu H H OMe H 96 1 CO.sub.2tBu H H OMe H 97 1 CONHMe H H OMe H 98 2 CONHMe H H OMe H 99 3 CONHMe H H OMe H 100 4 CONHMe H H OMe H 101 1 SO.sub.2Me H H OMe H 102 2 SO.sub.2Me H H OMe H 103 3 SO.sub.2Me H H OMe H 104 4 SO.sub.2Me H H OMe H 105 1 SO.sub.2NH.sub.2 H H OMe H 106 2 SO.sub.2NH.sub.2 H H OMe H 107 3 SO.sub.2NH.sub.2 H H OMe H 108 4 SO.sub.2NH.sub.2 H H OMe H 109 1 H H H Me H 110 2 H H H Me H 111 3 H H H Me H 112 4 H H H Me H 113 1 Me H H Me H 114 2 Me H H Me H 115 3 Me H H Me H 116 4 Me H H Me H 117 1 CH.sub.2Ph H H Me H 118 2 CH.sub.2Ph H H Me H 119 3 CH.sub.2Ph H H Me H 120 4 CH.sub.2Ph H H Me H 121 1 COMe H H Me H 122 2 COMe H H Me H 123 3 COMe H H Me H 124 4 COMe H H Me H 125 1 CO.sub.2Me H H Me H 126 2 CO.sub.2Me H H Me H 127 3 CO.sub.2Me H H Me H 128 4 CO.sub.2Me H H Me H 129 1 CO.sub.2tBu H H Me H 130 2 CO.sub.2tBu H H Me H 131 3 CO.sub.2tBu H H Me H 132 4 CO.sub.2tBu H H Me H 133 1 CONHMe H H Me H 134 2 CONHMe H H Me H 135 3 CONHMe H H Me H 136 4 CONHMe H H Me H 137 1 SO.sub.2Me H H Me H 138 2 SO.sub.2Me H H Me H 139 3 SO.sub.2Me H H Me H 140 4 SO.sub.2Me H H Me H 141 1 SO.sub.2NH.sub.2 H H Me H 142 2 SO.sub.2NH.sub.2 H H Me H 143 3 SO.sub.2NH.sub.2 H H Me H 144 4 SO.sub.2NH.sub.2 H H Me H 145 1 H H H CF.sub.3 H 146 2 H H H CF.sub.3 H 147 3 H H H CF.sub.3 H 148 4 H H H CF.sub.3 H 149 1 Me H H CF.sub.3 H 150 2 Me H H CF.sub.3 H 151 3 Me H H CF.sub.3 H 152 4 Me H H CF.sub.3 H 153 1 CH.sub.2Ph H H CF.sub.3 H 154 2 CH.sub.2Ph H H CF.sub.3 H 155 3 CH.sub.2Ph H H CF.sub.3 H 156 4 CH.sub.2Ph H H CF.sub.3 H 157 1 COMe H H CF.sub.3 H 158 2 COMe H H CF.sub.3 H 159 3 COMe H H CF.sub.3 H 160 4 COMe H H CF.sub.3 H 161 1 CO.sub.2Me H H CF.sub.3 H 162 2 CO.sub.2Me H H CF.sub.3 H 163 3 CO.sub.2Me H H CF.sub.3 H 164 4 CO.sub.2Me H H CF.sub.3 H 165 1 CO.sub.2tBu H H CF.sub.3 H 166 2 CO.sub.2tBu H H CF.sub.3 H 167 3 CO.sub.2tBu H H CF.sub.3 H 168 4 CO.sub.2tBu H H CF.sub.3 H 169 1 CONHMe H H CF.sub.3 H 170 2 CONHMe H H CF.sub.3 H 171 3 CONHMe H H CF.sub.3 H 172 4 CONHMe H H CF.sub.3 H 173 1 SO.sub.2Me H H CF.sub.3 H 174 2 SO.sub.2Me H H CF.sub.3 H 175 3 SO.sub.2Me H H CF.sub.3 H 176 4 SO.sub.2Me H H CF.sub.3 H 177 1 SO.sub.2NH.sub.2 H H CF.sub.3 H 178 2 SO.sub.2NH.sub.2 H H CF.sub.3 H 179 3 SO.sub.2NH.sub.2 H H CF.sub.3 H 180 4 SO.sub.2NH.sub.2 H H CF.sub.3 H 181 1 H H H F H 182 2 H H H F H 183 3 H H H F H 184 4 H H H F H 185 1 Me H H F H 186 2 Me H H F H 187 3 Me H H F H 188 4 Me H H F H 189 1 CH.sub.2Ph H H F H 190 2 CH.sub.2Ph H H F H 191 3 CH.sub.2Ph H H F H 192 4 CH.sub.2Ph H H F H 193 1 COMe H H F H 194 2 COMe H H F H 195 3 COMe H H F H 196 4 COMe H H F H 197 1 CO.sub.2Me H H F H 198 2 CO.sub.2Me H H F H 199 3 CO.sub.2Me H H F H 200 4 CO.sub.2Me H H F H 201 1 CO.sub.2tBu H H F H 202 2 CO.sub.2tBu H H F H 203 3 CO.sub.2tBu H H F H 204 4 CO.sub.2tBu H H F H 205 1 CONHMe H H F H 206 2 CONHMe H H F H 207 3 CONHMe H H F H 208 4 CONHMe H H F H 209 1 SO.sub.2Me H H F H 210 2 SO.sub.2Me H H F H 211 3 SO.sub.2Me H H F H 212 4 SO.sub.2Me H H F H 213 1 SO.sub.2NH.sub.2 H H F H 214 2 SO.sub.2NH.sub.2 H H F H 215 3 SO.sub.2NH.sub.2 H H F H 216 4 SO.sub.2NH.sub.2 H H F H 217 1 H H H Cl H 218 2 H H H Cl H 219 3 H H H Cl H 220 4 H H H Cl H 221 1 Me H H Cl H 222 2 Me H H Cl H 223 3 Me H H Cl H 224 4 Me H H Cl H 225 1 CH.sub.2Ph H H Cl H 226 2 CH.sub.2Ph H H Cl H 227 3 CH.sub.2Ph H H Cl H 228 4 CH.sub.2Ph H H Cl H 229 1 COMe H H Cl H 230 2 COMe H H Cl H 231 3 COMe H H Cl H 232 4 COMe H H Cl H 233 1 CO.sub.2Me H H Cl H 234 2 CO.sub.2Me H H Cl H 235 3 CO.sub.2Me H H Cl H 236 4 CO.sub.2Me H H Cl H 237 1 CO.sub.2tBu H H Cl H 238 2 CO.sub.2tBu H H Cl H 239 3 CO.sub.2tBu H H Cl H 240 4 CO.sub.2tBu H H Cl H 241 1 CONHMe H H Cl H 242 2 CONHMe H H Cl H 243 3 CONHMe H H Cl H 244 4 CONHMe H H Cl H 245 1 SO.sub.2Me H H Cl H 246 2 SO.sub.2Me H H Cl H 247 3 SO.sub.2Me H H Cl H 248 4 SO.sub.2Me H H Cl H 249 1 SO.sub.2NH.sub.2 H H Cl H 250 2 SO.sub.2NH.sub.2 H H Cl H 251 3 SO.sub.2NH.sub.2 H H Cl H 252 4 SO.sub.2NH.sub.2 H H Cl H 253 1 H H H CN H 254 2 H H H CN H 255 3 H H H CN H 256 4 H H H CN H 257 1 Me H H CN H 258 2 Me H H CN H 259 3 Me H H CN H 260 4 Me H H CN H 261 1 CH.sub.2Ph H H CN H 262 2 CH.sub.2Ph H H CN H 263 3 CH.sub.2Ph H H CN H 264 4 CH.sub.2Ph H H CN H 265 1 COMe H H CN H 266 2 COMe H H CN H 267 3 COMe H H CN H 268 4 COMe H H CN H 269 1 CO.sub.2Me H H CN H 270 2 CO.sub.2Me H H CN H 271 3 CO.sub.2Me H H CN H 272 4 CO.sub.2Me H H CN H 273 1 CO.sub.2tBu H H CN H 274 2 CO.sub.2tBu H H CN H 275 3 CO.sub.2tBu H H CN H 276 4 CO.sub.2tBu H H CN H 277 1 CONHMe H H CN H 278 2 CONHMe H H CN H 279 3 CONHMe H H CN H 280 4 CONHMe H H CN H 281 1 SO.sub.2Me H H CN H 282 2 SO.sub.2Me H H CN H 283 3 SO.sub.2Me H H CN H 284 4 SO.sub.2Me H H CN H 285 1 SO.sub.2NH.sub.2 H H CN H 286 2 SO.sub.2NH.sub.2 H H CN H 287 3 SO.sub.2NH.sub.2 H H CN H 288 4 SO.sub.2NH.sub.2 H H CN H 289 1 H H OH H H 290 2 H H OH H H 291 3 H H OH H H 292 4 H H OH H H 293 1 Me H OH H H 294 2 Me H OH H H 295 3 Me H OH H H 296 4 Me H OH H H 297 1 CH.sub.2Ph H OH H H 298 2 CH.sub.2Ph H OH H H 299 3 CH.sub.2Ph H OH H H 300 4 CH.sub.2Ph H OH H H 301 1 COMe H OH H H 302 2 COMe H OH H H 303 3 COMe H OH H H 304 4 COMe H OH H H 305 1 CO.sub.2Me H OH H H 306 2 CO.sub.2Me H OH H H 307 3 CO.sub.2Me H OH H H 308 4 CO.sub.2Me H OH H H 309 1 CO.sub.2tBu H OH H H 310 2 CO.sub.2tBu H OH H H 311 3 CO.sub.2tBu H OH H H 312 4 CO.sub.2tBu H OH H H 313 1 CONHMe H OH H H 314 2 CONHMe H OH H H 315 3 CONHMe H OH H H 316 4 CONHMe H OH H H 317 1 SO.sub.2Me H OH H H 318 2 SO.sub.2Me H OH H H 319 3 SO.sub.2Me H OH H H 320 4 SO.sub.2Me H OH H H 321 1 SO.sub.2NH.sub.2 H OH H H 322 2 SO.sub.2NH.sub.2 H OH H H 323 3 SO.sub.2NH.sub.2 H OH H H 324 4 SO.sub.2NH.sub.2 H OH H H 325 1 H H OMe H H 326 2 H H OMe H H 327 3 H H OMe H H 328 4 H H OMe H H 329 1 Me H OMe H H 330 2 Me H OMe H H 331 3 Me H OMe H H 332 4 Me H OMe H H 333 1 CH.sub.2Ph H OMe H H 334 2 CH.sub.2Ph H OMe H H 335 3 CH.sub.2Ph H OMe H H 336 4 CH.sub.2Ph H OMe H H 337 1 COMe H OMe H H 338 2 COMe H OMe H H 339 3 COMe H OMe H H 340 4 COMe H OMe H H 341 1 CO.sub.2Me H OMe H H 342 2 CO.sub.2Me H OMe H H 343 3 CO.sub.2Me H OMe H H 344 4 CO.sub.2Me H OMe H H 345 1 CO.sub.2tBu H OMe H H 346 2 CO.sub.2tBu H OMe H H 347 3 CO.sub.2tBu H OMe H H 348 4 CO.sub.2tBu H OMe H H 349 1 CONHMe H OMe H H 350 2 CONHMe H OMe H H 351 3 CONHMe H OMe H H 352 4 CONHMe H OMe H H 353 1 SO.sub.2Me H OMe H H 354 2 SO.sub.2Me H OMe H H 355 3 SO.sub.2Me H OMe H H 356 4 SO.sub.2Me H OMe H H 357 1 SO.sub.2NH.sub.2 H OMe H H 358 2 SO.sub.2NH.sub.2 H OMe H H 359 3 SO.sub.2NH.sub.2 H OMe H H 360 4 SO.sub.2NH.sub.2 H OMe H H 361 1 H H Me H H 362 2 H H Me H H 363 3 H H Me H H 364 4 H H Me H H 365 1 Me H Me H H 366 2 Me H Me H H 367 3 Me H Me H H 368 4 Me H Me H H 369 1 CH.sub.2Ph H Me H H 370 2 CH.sub.2Ph H Me H H 371 3 CH.sub.2Ph H Me H H 372 4 CH.sub.2Ph H Me H H 373 1 COMe H Me H H 374 2 COMe H Me H H 375 3 COMe H Me H H 376 4 COMe H Me H H 377 1 CO.sub.2Me H Me H H 378 2 CO.sub.2Me H Me H H 379 3 CO.sub.2Me H Me H H 380 4 CO.sub.2Me H Me H H 381 1 CO.sub.2tBu H Me H H 382 2 CO.sub.2tBu H Me H H 383 3 CO.sub.2tBu H Me H H 384 4 CO.sub.2tBu H Me H H 385 1 CONHMe H Me H H 386 2 CONHMe H Me H H 387 3 CONHMe H Me H H 388 4 CONHMe H Me H H 389 1 SO.sub.2Me H Me H H 390 2 SO.sub.2Me H Me H H 391 3 SO.sub.2Me H Me H H 392 4 SO.sub.2Me H Me H H 393 1 SO.sub.2NH.sub.2 H Me H H 394 2 SO.sub.2NH.sub.2 H Me H H 395 3 SO.sub.2NH.sub.2 H Me H H 396 4 SO.sub.2NH.sub.2 H Me H H 397 1 H H CF.sub.3 H H 398 2 H H CF.sub.3 H H 399 3 H H CF.sub.3 H H 400 4 H H CF.sub.3 H H 401 1 Me H CF.sub.3 H H 402 2 Me H CF.sub.3 H H 403 3 Me H CF.sub.3 H H 404 4 Me H CF.sub.3 H H 405 1 CH.sub.2Ph H CF.sub.3 H H 406 2 CH.sub.2Ph H CF.sub.3 H H 407 3 CH.sub.2Ph H CF.sub.3 H H 408 4 CH.sub.2Ph.sub.2 H CF.sub.3 H H 409 1 COMe H CF.sub.3 H H 410 2 COMe H CF.sub.3 H H 411 3 COMe H CF.sub.3 H H 412 4 COMe H CF.sub.3 H H 413 1 CO.sub.2Me H CF.sub.3 H H 414 2 CO.sub.2Me H CF.sub.3 H H 415 3 CO.sub.2Me H CF.sub.3 H H 416 4 CO.sub.2Me H CF.sub.3 H H 417 1 CO.sub.2tBu H CF.sub.3 H H 418 2 CO.sub.2tBu H CF.sub.3 H H 419 3 CO.sub.2tBu H CF.sub.3 H H 420 4 CO.sub.2tBu H CF.sub.3 H H 421 1 CONHMe H CF.sub.3 H H 422 2 CONHMe H CF.sub.3 H H 423 3 CONHMe H CF.sub.3 H H 424 4 CONHMe H CF.sub.3 H H 425 1 SO.sub.2Me H CF.sub.3 H H 426 2 SO.sub.2Me H CF.sub.3 H H 427 3 SO.sub.2Me H CF.sub.3 H H 428 4 SO.sub.2Me H CF.sub.3 H H 429 1 SO.sub.2NH.sub.2 H CF.sub.3 H H 430 2 SO.sub.2NH.sub.2 H CF.sub.3 H H 431 3 SO.sub.2NH.sub.2 H CF.sub.3 H H 432 4 SO.sub.2NH.sub.2 H CF.sub.3 H H 433 1 H H F H H 434 2 H H F H H 435 3 H H F H H 436 3 H H F H H 437 1 Me H F H H 438 2 Me H F H H 439 3 Me H F H H 440 4 Me H F H H 441 1 CH.sub.2Ph H F H H 442 2 CH.sub.2Ph H F H H 443 3 CH.sub.2Ph H F H H 444 4 CH.sub.2Ph H F H H 445 1 COMe H F H H 446 2 COMe H F H H 447 3 COMe H F H H 448 4 COMe H F H H 449 1 CO.sub.2Me H F H H 450 2 CO.sub.2Me H F H H 451 3 CO.sub.2Me H F H H 452 4 CO.sub.2Me H F H H 453 1 CO.sub.2tBu H F H H 454 2 CO.sub.2tBu H F H H 455 3 CO.sub.2tBu H F H H 456 4 CO.sub.2tBu H F H H 457 1 CONHMe H F H H 458 2 CONHMe H F H H 459 3 CONHMe H F H H 460 4 CONHMe H F H H 461 1 SO.sub.2Me H F H H 462 2 SO.sub.2Me H F H H 463 3 SO.sub.2Me H F H H 464 4 SO.sub.2Me H F H H 465 1 SO.sub.2NH.sub.2 H F H H 466 2 SO.sub.2NH.sub.2 H F H H 467 3 SO.sub.2NH.sub.2 H F H H 468 4 SO.sub.2NH.sub.2 H F H H 469 1 H H Cl H H 470 2 H H Cl H H 471 3 H H Cl H H 472 4 H H Cl H H 473 1 Me H Cl H H 474 2 Me H Cl H H 475 3 Me H Cl H H 476 4 Me H Cl H H 477 1 CH.sub.2Ph H Cl H H 478 2 CH.sub.2Ph H Cl H H 479 3 CH.sub.2Ph H Cl H H 480 4 CH.sub.2Ph H Cl H H 481 1 COMe H Cl H H 482 2 COMe H Cl H H 483 3 COMe H Cl H H 484 4 COMe H Cl H H 485 1 CO.sub.2Me H Cl H H 486 2 CO.sub.2Me H Cl H H 487 3 CO.sub.2Me H Cl H H 488 4 CO.sub.2Me H Cl H H 489 1 CO.sub.2tBu H Cl H H 490 2 CO.sub.2tBu H Cl H H 491 3 CO.sub.2tBu H Cl H H 492 4 CO.sub.2tBu H Cl H H 493 1 CONHMe H Cl H H 494 2 CONHMe H Cl H H 495 3 CONHMe H Cl H H 496 4 CONHMe H Cl H H 497 1 SO.sub.2Me H Cl H H 498 2 SO.sub.2Me H Cl H H 499 3 SO.sub.2Me H Cl H H 500 4 SO.sub.2Me H Cl H H 501 1 SO.sub.2NH.sub.2 H Cl H H 502 2 SO.sub.2NH.sub.2 H Cl H H 503 3 SO.sub.2NH.sub.2 H Cl H H 504 4 SO.sub.2NH.sub.2 H Cl H H 505 1 H H CN H H 506 2 H H CN H H 507 3 H H CN H H 508 4 H H CN H H 509 1 Me H CN H H 510 2 Me H CN H H 511 3 Me H CN H H 512 4 Me H CN H H 513 1 CH.sub.2Ph H CN H H 514 2 CH.sub.2Ph H CN H H 515 3 CH.sub.2Ph H CN H H 516 4 CH.sub.2Ph H CN H H 517 1 COMe H CN H H 518 2 COMe H CN H H 519 3 COMe H CN H H 520 4 COMe H CN H H 521 1 CO.sub.2Me H CN H H 522 2 CO.sub.2Me H CN H H 523 3 CO.sub.2Me H CN H H 524 4 CO.sub.2Me H CN H H 525 1 CO.sub.2tBu H CN H H 526 2 CO.sub.2tBu H CN H H 527 3 CO.sub.2tBu H CN H H 528 4 CO.sub.2tBu H CN H H 529 1 CONHMe H CN H H 530 2 CONHMe H CN H H 531 3 CONHMe H CN H H 532 4 CONHMe H CN H H 533 1 SO.sub.2Me H CN H H 534 2 SO.sub.2Me H CN H H 535 3 SO.sub.2Me H CN H H 536 4 SO.sub.2Me H CN H H 537 1 SO.sub.2NH.sub.2 H CN H H 538 2 SO.sub.2NH.sub.2 H CN H H 539 3 SO.sub.2NH.sub.2 H CN H H 540 4 SO.sub.2NH.sub.2 H CN H H 541 1 H OH H H H 542 2 H OH H H H 543 3 H OH H H H 544 4 H OH H H H 545 1 Me OH H H H 546 2 Me OH H H H 547 3 Me OH H H H 548 4 Me OH H H H 549 1 CH.sub.2Ph OH H H H 550 2 CH.sub.2Ph OH H H H 551 3 CH.sub.2Ph OH H H H 552 4 CH.sub.2Ph OH H H H 553 1 COMe OH H H H 554 2 COMe OH H H H 555 3 COMe OH H H H 556 4 COMe OH H H H 557 1 CO.sub.2Me OH H H H 558 2 CO.sub.2Me OH H H H 559 3 CO.sub.2Me OH H H H 560 4 CO.sub.2Me OH H H H 561 1 CO.sub.2tBu OH H H H 562 2 CO.sub.2tBu OH H H H 563 3 CO.sub.2tBu OH H H H 564 4 CO.sub.2tBu OH H H H 565 1 CONHMe OH H H H 566 2 CONHMe OH H H H 567 3 CONHMe OH H H H 568 4 CONHMe OH H H H 569 1 SO.sub.2Me OH H H H 570 2 SO.sub.2Me OH H H H 571 3 SO.sub.2Me OH H H H 572 4 SO.sub.2Me OH H H H 573 1 SO.sub.2NH.sub.2 OH H H H 574 2 SO.sub.2NH.sub.2 OH H H H 575 3 SO.sub.2NH.sub.2 OH H H H 576 4 SO.sub.2NH.sub.2 OH H H H 577 1 H OMe H H H 578 2 H OMe H H H 579 3 H OMe H H H 580 4 H OMe H H H 581 1 Me OMe H H H 582 2 Me OMe H H H 583 3 Me OMe H H H 584 4 Me OMe H H H 585 1 CH.sub.2Ph OMe H H H 586 2 CH.sub.2Ph OMe H H H 587 3 CH.sub.2Ph OMe H H H 588 4 CH.sub.2Ph OMe H H H 589 1 COMe OMe H H H 590 2 COMe OMe H H H 591 3 COMe OMe H H H 592 4 COMe OMe H H H 593 1 CO.sub.2Me OMe H H H 594 2 CO.sub.2Me OMe H H H 595 3 CO.sub.2Me OMe H H H 596 4 CO.sub.2Me OMe H H H 597 1 CO.sub.2tBu OMe H H H 598 2 CO.sub.2tBu OMe H H H 599 3 CO.sub.2tBu OMe H H H 600 4 CO.sub.2tBu OMe H H H 601 1 CONHMe OMe H H H 602 2 CONHMe OMe H H H 603 3 CONHMe OMe H H H 604 4 CONHMe OMe H H H 605 1 SO.sub.2Me OMe H H H 606 2 SO.sub.2Me OMe H H H 607 3 SO.sub.2Me OMe H H H 608 4 SO.sub.2Me OMe H H H 609 1 SO.sub.2NH.sub.2 OMe H H H 610 2 SO.sub.2NH.sub.2 OMe H H H 611 3 SO.sub.2NH.sub.2 OMe H H H 612 4 SO.sub.2NH.sub.2 OMe H H H 613 1 H Me H H H 614 2 H Me H H H 615 3 H Me H H H 616 4 H Me H H H 617 1 Me Me H H H 618 2 Me Me H H H 619 3 Me Me H H H 620 4 Me Me H H H 621 1 CH.sub.2Ph Me H H H 622 2 CH.sub.2Ph Me H H H 623 3 CH.sub.2Ph Me H H H 624 4 CH.sub.2Ph Me H H H 625 1 COMe Me H H H 626 2 COMe Me H H H 627 3 COMe Me H H H 628 4 COMe Me H H H 629 1 CO.sub.2Me Me H H H 630 2 CO.sub.2Me Me H H H 631 3 CO.sub.2Me Me H H H 632 4 CO.sub.2Me Me H H H 633 1 CO.sub.2tBu Me H H H 634 2 CO.sub.2tBu Me H H H 635 3 CO.sub.2tBu Me H H H 636 4 CO.sub.2tBu Me H H H 637 1 CONHMe Me H H H 638 2 CONHMe Me H H H 639 3 CONHMe Me H H H 640 4 CONHMe Me H H H 641 1 SO.sub.2Me Me H H H 642 2 SO.sub.2Me Me H H H 643 3 SO.sub.2Me Me H H H 644 4 SO.sub.2Me Me H H H 645 1 SO.sub.2NH.sub.2 Me H H H 646 2 SO.sub.2NH.sub.2 Me H H H 647 3 SO.sub.2NH.sub.2 Me H H H 648 4 SO.sub.2NH.sub.2 Me H H H 649 1 H CF.sub.3 H H H 650 2 H CF.sub.3 H H H 651 3 H CF.sub.3 H H H 652 4 H CF.sub.3 H H H 653 1 Me CF.sub.3 H H H 654 2 Me CF.sub.3 H H H 655 3 Me CF.sub.3 H H H 656 4 Me CF.sub.3 H H H 657 1 CH.sub.2Ph CF.sub.3 H H H 658 2 CH.sub.2Ph CF.sub.3 H H H 659 3 CH.sub.2Ph CF.sub.3 H H H 660 4 CH.sub.2Ph CF.sub.3 H H H 661 1 COMe CF.sub.3 H H H 662 2 COMe CF.sub.3 H H H 663 3 COMe CF.sub.3 H H H 664 4 COMe CF.sub.3 H H H 665 1 CO.sub.2Me CF.sub.3 H H H 666 2 CO.sub.2Me CF.sub.3 H H H 667 3 CO.sub.2Me CF.sub.3 H H H 668 4 CO.sub.2Me CF.sub.3 H H H 669 1 CO.sub.2tBu CF.sub.3 H H H 670 2 CO.sub.2tBu CF.sub.3 H H H 671 3 CO.sub.2tBu CF.sub.3 H H H 672 4 CO.sub.2tBu CF.sub.3 H H H 673 1 CONHMe CF.sub.3 H H H 674 2 CONHMe CF.sub.3 H H H 675 3 CONHMe CF.sub.3 H H H 676 4 CONHMe CF.sub.3 H H H 677 1 SO.sub.2Me CF.sub.3 H H H 678 2 SO.sub.2Me CF.sub.3 H H H 679 3 SO.sub.2Me CF.sub.3 H H H 680 4 SO.sub.2Me CF.sub.3 H H H 681 1 SO.sub.2NH.sub.2 CF.sub.3 H H H 682 2 SO.sub.2NH.sub.2 CF.sub.3 H H H 683 3 SO.sub.2NH.sub.2 CF.sub.3 H H H 684 4 SO.sub.2NH.sub.2 CF.sub.3 H H H 685 1 H F H H H 686 2 H F H H H 687 3 H F H H H 688 3 H F H H H 689 1 Me F H H H 690 2 Me F H H H 691 3 Me F H H H 692 4 Me F H H H 693 1 CH.sub.2Ph F H H H 694 2 CH.sub.2Ph F H H H 695 3 CH.sub.2Ph F H H H 696 4 CH.sub.2Ph F H H H 697 1 COMe F H H H 698 2 COMe F H H H 699 3 COMe F H H H 700 4 COMe F H H H 701 1 CO.sub.2Me F H H H 702 2 CO.sub.2Me F H H H 703 3 CO.sub.2Me F H H H 704 4 CO.sub.2Me F H H H 705 1 CO.sub.2tBu F H H H 706 2 CO.sub.2tBu F H H H 707 3 CO.sub.2tBu F H H H 708 4 CO.sub.2tBu F H H H 709 1 CONHMe F H H H 710 2 CONHMe F H H H 711 3 CONHMe F H H H 712 4 CONHMe F H H H 713 1 SO.sub.2Me F H H H 714 2 SO.sub.2Me F H H H 715 3 SO.sub.2Me F H H H 716 4 SO.sub.2Me F H H H 717 1 SO.sub.2NH.sub.2 F H H H 718 2 SO.sub.2NH.sub.2 F H H H 719 3 SO.sub.2NH.sub.2 F H H H 720 4 SO.sub.2NH.sub.2 F H H H 721 1 H Cl H H H 722 2 H Cl H H H 723 3 H Cl H H H 724 4 H Cl H H H 725 1 Me Cl H H H 726 2 Me Cl H H H 727 3 Me Cl H H H 728 4 Me Cl H H H 729 1 CH.sub.2Ph Cl H H H 730 2 CH.sub.2Ph Cl H H H 731 3 CH.sub.2Ph Cl H H H 732 4 CH.sub.2Ph Cl H H H 733 1 COMe Cl H H H 734 2 COMe Cl H H H 735 3 COMe Cl H H H 736 4 COMe Cl H H H 737 1 CO.sub.2Me Cl H H H 738 2 CO.sub.2Me Cl H H H 739 3 CO.sub.2Me Cl H H H 740 4 CO.sub.2Me Cl H H H 741 1 CO.sub.2tBu Cl H H H 742 2 CO.sub.2tBu Cl H H H 743 3 CO.sub.2tBu Cl H H H 744 4 CO.sub.2tBu Cl H H H 745 1 CONHMe Cl H H H 746 2 CONHMe Cl H H H 747 3 CONHMe Cl H H H 748 4 CONHMe Cl H H H 749 1 SO.sub.2Me Cl H H H 750 2 SO.sub.2Me Cl H H H 751 3 SO.sub.2Me Cl H H H 752 4 SO.sub.2Me Cl H H H 753 1 SO.sub.2NH.sub.2 Cl H H H 754 2 SO.sub.2NH.sub.2 Cl H H H 755 3 SO.sub.2NH.sub.2 Cl H H H 756 4 SO.sub.2NH.sub.2 Cl H H H 757 1 H CN H H H 758 2 H CN H H H 759 3 H CN H H H 760 4 H CN H H H 761 1 Me CN H H H 762 2 Me CN H H H 763 3 Me CN H H H 764 4 Me CN H H H 765 1 CH.sub.2Ph CN H H H 766 2 CH.sub.2Ph CN H H H 767 3 CH.sub.2Ph CN H H H 768 4 CH.sub.2Ph CN H H H 769 1 COMe CN H H H 770 2 COMe CN H H H 771 3 COMe CN H H H 772 4 COMe CN H H H 773 1 CO.sub.2Me CN H H H 774 2 CO.sub.2Me CN H H H 775 3 CO.sub.2Me CN H H H 776 4 CO.sub.2Me CN H H H 777 1 CO.sub.2tBu CN H H H 778 2 CO.sub.2tBu CN H H H 779 3 CO.sub.2tBu CN H H H 780 4 CO.sub.2tBu CN H H H 781 1 CONHMe CN H H H 782 2 CONHMe CN H H H 783 3 CONHMe CN H H H 784 4 CONHMe CN H H H 785 1 SO.sub.2Me CN H H H 786 2 SO.sub.2Me CN H H H 787 3 SO.sub.2Me CN H H H 788 4 SO.sub.2Me CN H H H 789 1 SO.sub.2NH.sub.2 CN H H H 790 2 SO.sub.2NH.sub.2 CN H H H 791 3 SO.sub.2NH.sub.2 CN H H H 792 4 SO.sub.2NH.sub.2 CN H H H 793 1 H H H H OH 794 2 H H H H OH 795 3 H H H H OH 796 4 H H H H OH 797 1 Me H H H OH 798 2 Me H H H OH 799 3 Me H H H OH 800 4 Me H H H OH 801 1 CH.sub.2Ph H H H OH 802 2 CH.sub.2Ph H H H OH 803 3 CH.sub.2Ph H H H OH 804 4 CH.sub.2Ph H H H OH 805 1 COMe H H H OH 806 2 COMe H H H OH 807 3 COMe H H H OH 808 4 COMe H H H OH 809 1 CO.sub.2Me H H H OH 810 2 CO.sub.2Me H H H OH 811 3 CO.sub.2Me H H H OH 812 4 CO.sub.2Me H H H OH 813 1 CO.sub.2tBu H H H OH 814 2 CO.sub.2tBu H H H OH 815 3 CO.sub.2tBu H H H OH 816 4 CO.sub.2tBu H H H OH 817 1 CONHMe H H H OH 818 2 CONHMe H H H OH 819 3 CONHMe H H H OH 820 4 CONHMe H H H OH 821 1 SO.sub.2Me H H H OH 822 2 SO.sub.2Me H H H OH 823 3 SO.sub.2Me H H H OH 824 4 SO.sub.2Me H H H OH 825 1 SO.sub.2NH.sub.2 H H H OH 826 2 SO.sub.2NH.sub.2 H H H OH 827 3 SO.sub.2NH.sub.2 H H H OH 828 4 SO.sub.2NH.sub.2 H H H OH 829 1 H H H H OMe 830 2 H H H H OMe 831 3 H H H H OMe 832 4 H H H H OMe 833 1 Me H H H OMe 834 2 Me H H H OMe 835 3 Me H H H OMe 836 4 Me H H H OMe 837 1 CH.sub.2Ph H H H OMe 838 2 CH.sub.2Ph H H H OMe 839 3 CH.sub.2Ph H H H OMe 840 4 CH.sub.2Ph H H H OMe 841 1 COMe H H H OMe 842 2 COMe H H H OMe 843 3 COMe H H H OMe 844 4 COMe H H H OMe 845 1 CO.sub.2Me H H H OMe 846 2 CO.sub.2Me H H H OMe 847 3 CO.sub.2Me H H H OMe 848 4 CO.sub.2Me H H H OMe 849 1 CO.sub.2tBu H H H OMe 850 2 CO.sub.2tBu H H H OMe 851 3 CO.sub.2tBu H H H OMe 852 4 CO.sub.2tBu H H H OMe 853 1 CONHMe H H H OMe 854 2 CONHMe H H H OMe 855 3 CONHMe H H H OMe 856 4 CONHMe H H H OMe 857 1 SO.sub.2Me H H H OMe 858 2 SO.sub.2Me H H H OMe 859 3 SO.sub.2Me H H H OMe 860 4 SO.sub.2Me H H H OMe 861 1 SO.sub.2NH.sub.2 H H H OMe 862 2 SO.sub.2NH.sub.2 H H H OMe 863 3 SO.sub.2NH.sub.2 H H H OMe 864 4 SO.sub.2NH.sub.2 H H H OMe 865 1 H H H H Me 866 2 H H H H Me 867 3 H H H H Me 868 4 H H H H Me 869 1 Me H H H Me 870 2 Me H H H Me 871 3 Me H H H Me 872 4 Me H H H Me 873 1 CH.sub.2Ph H H H Me 874 2 CH.sub.2Ph H H H Me 875 3 CH.sub.2Ph H H H Me 876 4 CH.sub.2Ph H H H Me 877 1 COMe H H H Me 878 2 COMe H H H Me 879 3 COMe H H H Me 880 4 COMe H H H Me 881 1 CO.sub.2Me H H H Me 882 2 CO.sub.2Me H H H Me 883 3 CO.sub.2Me H H H Me 884 4 CO.sub.2Me H H H Me 885 1 CO.sub.2tBu H H H Me 886 2 CO.sub.2tBu H H H Me 887 3 CO.sub.2tBu H H H Me 888 4 CO.sub.2tBu H H H Me 889 1 CONHMe H H H Me 890 2 CONHMe H H H Me 891 3 CONHMe H H H Me 892 4 CONHMe H H H Me 893 1 SO.sub.2Me H H H Me 894 2 SO.sub.2Me H H H Me 895 3 SO.sub.2Me H H H Me 896 4 SO.sub.2Me H H H Me 897 1 SO.sub.2NH.sub.2 H H H Me 898 2 SO.sub.2NH.sub.2 H H H Me 899 3 SO.sub.2NH.sub.2 H H H Me 900 4 SO.sub.2NH.sub.2 H H H Me 901 1 H H H H CF.sub.3 902 2 H H H H CF.sub.3 903 3 H H H H CF.sub.3 904 4 H H H H CF.sub.3 905 1 Me H H H CF.sub.3 906 2 Me H H H CF.sub.3 907 3 Me H H H CF.sub.3 908 4 Me H H H CF.sub.3 909 1 CH.sub.2Ph H H H CF.sub.3 910 2 CH.sub.2Ph H H H CF.sub.3 911 3 CH.sub.2Ph H H H CF.sub.3 912 4 CH.sub.2Ph H H H CF.sub.3 913 1 COMe H H H CF.sub.3 914 2 COMe H H H CF.sub.3 915 3 COMe H H H CF.sub.3 916 4 COMe H H H CF.sub.3 917 1 CO.sub.2Me H H H CF.sub.3 918 2 CO.sub.2Me H H H CF.sub.3 919 3 CO.sub.2Me H H H CF.sub.3 920 4 CO.sub.2Me H H H CF.sub.3 921 1 CO.sub.2tBu H H H CF.sub.3 922 2 CO.sub.2tBu H H H CF.sub.3 923 3 CO.sub.2tBu H H H CF.sub.3 924 4 CO.sub.2tBu H H H CF.sub.3 925 1 CONHMe H H H CF.sub.3 926 2 CONHMe H H H CF.sub.3 927 3 CONHMe H H H CF.sub.3 928 4 CONHMe H H H CF.sub.3 929 1 SO.sub.2Me H H H CF.sub.3 930 2 SO.sub.2Me H H H CF.sub.3 931 3 SO.sub.2Me H H H CF.sub.3 932 4 SO.sub.2Me H H H CF.sub.3 933 1 SO.sub.2NH.sub.2 H H H CF.sub.3 934 2 SO.sub.2NH.sub.2 H H H CF.sub.3 935 3 SO.sub.2NH.sub.2 H H H CF.sub.3 936 4 SO.sub.2NH.sub.2 H H H CF.sub.3 937 1 H H H H F 938 2 H H H H F 939 3 H H H H F 940 3 H H H H F 941 1 Me H H H F 942 2 Me H H H F 943 3 Me H H H F 944 4 Me H H H F 945 1 CH.sub.2Ph H H H F 946 2 CH.sub.2Ph H H H F 947 3 CH.sub.2Ph H H H F 948 4 CH.sub.2Ph H H H F 949 1 COMe H H H F 950 2 COMe H H H F 951 3 COMe H H H F 952 4 COMe H H H F 953 1 CO.sub.2Me H H H F 954 2 CO.sub.2Me H H H F 955 3 CO.sub.2Me H H H F 956 4 CO.sub.2Me H H H F 957 1 CO.sub.2tBu H H H F 958 2 CO.sub.2tBu H H H F 959 3 CO.sub.2tBu H H H F 960 4 CO.sub.2tBu H H H F 961 1 CONHMe H H H F 962 2 CONHMe H H H F 963 3 CONHMe H H H F 964 4 CONHMe H H H F 965 1 SO.sub.2Me H H H F 966 2 SO.sub.2Me H H H F 967 3 SO.sub.2Me H H H F 968 4 SO.sub.2Me H H H F 969 1 SO.sub.2NH.sub.2 H H H F 970 2 SO.sub.2NH.sub.2 H H H F 971 3 SO.sub.2NH.sub.2 H H H F 972 4 SO.sub.2NH.sub.2 H H H F 973 1 H H H H Cl 974 2 H H H H Cl 975 3 H H H H Cl 976 4 H H H H Cl 977 1 Me H H H Cl 978 2 Me H H H Cl 979 3 Me H H H Cl 980 4 Me H H H Cl 981 1 CH.sub.2Ph H H H Cl 982 2 CH.sub.2Ph H H H Cl 983 3 CH.sub.2Ph H H H Cl 984 4 CH.sub.2Ph H H H Cl 985 1 COMe H H H Cl 986 2 COMe H H H Cl 987 3 COMe H H H Cl 988 4 COMe H H H Cl 989 1 CO.sub.2Me H H H Cl 990 2 CO.sub.2Me H H H Cl 991 3 CO.sub.2Me H H H Cl 992 4 CO.sub.2Me H H H Cl 993 1 CO.sub.2tBu H H H Cl 994 2 CO.sub.2tBu H H H Cl 995 3 CO.sub.2tBu H H H Cl 996 4 CO.sub.2tBu H H H Cl 997 1 CONHMe H H H Cl 998 2 CONHMe H H H Cl 999 3 CONHMe H H H Cl 1000 4 CONHMe H H H Cl 1001 1 SO.sub.2Me H H H Cl 1002 2 SO.sub.2Me H H H Cl 1003 3 SO.sub.2Me H H H Cl 1004 4 SO.sub.2Me H H H Cl 1005 1 SO.sub.2NH.sub.2 H H H Cl 1006 2 SO.sub.2NH.sub.2 H H H Cl 1007 3 SO.sub.2NH.sub.2 H H H Cl 1008 4 SO.sub.2NH.sub.2 H H H Cl 1009 1 H H H H CN 1010 2 H H H H CN 1011 3 H H H H CN 1012 4 H H H H CN 1013 1 Me H H H CN 1014 2 Me H H H CN 1015 3 Me H H H CN 1016 4 Me H H H CN 1017 1 CH.sub.2Ph H H H CN 1018 2 CH.sub.2Ph H H H CN 1019 3 CH.sub.2Ph H H H CN 1020 4 CH.sub.2Ph H H H CN 1021 1 COMe H H H CN 1022 2 COMe H H H CN 1023 3 COMe H H H CN 1024 4 COMe H H H CN 1025 1 CO.sub.2Me H H H CN 1026 2 CO.sub.2Me H H H CN 1027 3 CO.sub.2Me H H H CN 1028 4 CO.sub.2Me H H H CN 1029 1 CO.sub.2tBu H H H CN 1030 2 CO.sub.2tBu H H H CN 1031 3 CO.sub.2tBu H H H CN 1032 4 CO.sub.2tBu H H H CN 1033 1 CONHMe H H H CN 1034 2 CONHMe H H H CN 1035 3 CONHMe H H H CN 1036 4 CONHMe H H H CN 1037 1 SO.sub.2Me H H H CN 1038 2 SO.sub.2Me H H H CN 1039 3 SO.sub.2Me H H H CN 1040 4 SO.sub.2Me H H H CN 1041 1 SO.sub.2NH.sub.2 H H H CN 1042 2 SO.sub.2NH.sub.2 H H H CN 1043 3 SO.sub.2NH.sub.2 H H H CN 1044 4 SO.sub.2NH.sub.2 H H H CN

    [2038] Exemplary embodiments include compounds having the formula (XXIX)

    ##STR00444##

    [2039] or a pharmaceutically acceptable salt form thereof defined herein below in Table 23.

    TABLE-US-00023 TABLE 23 Entry n R.sup.7 R.sup.20a R.sup.20b R.sup.20c R.sup.20e 1 1 H H H H H 2 2 H H H H H 3 3 H H H H H 4 4 H H H H H 5 1 Me H H H H 6 2 Me H H H H 7 3 Me H H H H 8 4 Me H H H H 9 1 CH.sub.2Ph H H H H 10 2 CH.sub.2Ph H H H H 11 3 CH.sub.2Ph H H H H 12 4 CH.sub.2Ph H H H H 13 1 COMe H H H H 14 2 COMe H H H H 15 3 COMe H H H H 16 4 COMe H H H H 17 1 CO.sub.2Me H H H H 18 2 CO.sub.2Me H H H H 19 3 CO.sub.2Me H H H H 20 4 CO.sub.2Me H H H H 21 1 CO.sub.2tBu H H H H 22 2 CO.sub.2tBu H H H H 23 3 CO.sub.2tBu H H H H 24 4 CO.sub.2tBu H H H H 25 1 CONHMe H H H H 26 2 CONHMe H H H H 27 3 CONHMe H H H H 28 4 CONHMe H H H H 29 1 SO.sub.2Me H H H H 30 2 SO.sub.2Me H H H H 31 3 SO.sub.2Me H H H H 32 4 SO.sub.2Me H H H H 33 1 SO.sub.2NH.sub.2 H H H H 34 2 SO.sub.2NH.sub.2 H H H H 35 3 SO.sub.2NH.sub.2 H H H H 36 4 SO.sub.2NH.sub.2 H H H H 37 1 H H H OH H 38 2 H H H OH H 39 3 H H H OH H 40 4 H H H OH H 41 1 Me H H OH H 42 2 Me H H OH H 43 3 Me H H OH H 44 4 Me H H OH H 45 1 CH.sub.2Ph H H OH H 46 2 CH.sub.2Ph H H OH H 47 3 CH.sub.2Ph H H OH H 48 4 CH.sub.2Ph H H OH H 49 1 COMe H H OH H 50 2 COMe H H OH H 51 3 COMe H H OH H 52 4 COMe H H OH H 53 1 CO.sub.2Me H H OH H 54 2 CO.sub.2Me H H OH H 55 3 CO.sub.2Me H H OH H 56 4 CO.sub.2Me H H OH H 57 1 CO.sub.2tBu H H OH H 58 2 CO.sub.2tBu H H OH H 59 3 CO.sub.2tBu H H OH H 60 4 CO.sub.2tBu H H OH H 61 1 CONHMe H H OH H 62 2 CONHMe H H OH H 63 3 CONHMe H H OH H 64 4 CONHMe H H OH H 65 1 SO.sub.2Me H H OH H 66 2 SO.sub.2Me H H OH H 67 3 SO.sub.2Me H H OH H 68 4 SO.sub.2Me H H OH H 69 1 SO.sub.2NH.sub.2 H H OH H 70 2 SO.sub.2NH.sub.2 H H OH H 71 3 SO.sub.2NH.sub.2 H H OH H 72 4 SO.sub.2NH.sub.2 H H OH H 73 1 H H H OMe H 74 2 H H H OMe H 75 3 H H H OMe H 76 4 H H H OMe H 77 1 Me H H OMe H 78 2 Me H H OMe H 79 3 Me H H OMe H 80 4 Me H H OMe H 81 1 CH.sub.2Ph H H OMe H 82 2 CH.sub.2Ph H H OMe H 83 3 CH.sub.2Ph H H OMe H 84 4 CH.sub.2Ph H H OMe H 85 1 COMe H H OMe H 86 2 COMe H H OMe H 87 3 COMe H H OMe H 88 4 COMe H H OMe H 89 1 CO.sub.2Me H H OMe H 90 2 CO.sub.2Me H H OMe H 91 3 CO.sub.2Me H H OMe H 92 4 CO.sub.2Me H H OMe H 93 1 CO.sub.2tBu H H OMe H 94 2 CO.sub.2tBu H H OMe H 95 3 CO.sub.2tBu H H OMe H 96 1 CO.sub.2tBu H H OMe H 97 1 CONHMe H H OMe H 98 2 CONHMe H H OMe H 99 3 CONHMe H H OMe H 100 4 CONHMe H H OMe H 101 1 SO.sub.2Me H H OMe H 102 2 SO.sub.2Me H H OMe H 103 3 SO.sub.2Me H H OMe H 104 4 SO.sub.2Me H H OMe H 105 1 SO.sub.2NH.sub.2 H H OMe H 106 2 SO.sub.2NH.sub.2 H H OMe H 107 3 SO.sub.2NH.sub.2 H H OMe H 108 4 SO.sub.2NH.sub.2 H H OMe H 109 1 H H H Me H 110 2 H H H Me H 111 3 H H H Me H 112 4 H H H Me H 113 1 Me H H Me H 114 2 Me H H Me H 115 3 Me H H Me H 116 4 Me H H Me H 117 1 CH.sub.2Ph H H Me H 118 2 CH.sub.2Ph H H Me H 119 3 CH.sub.2Ph H H Me H 120 4 CH.sub.2Ph H H Me H 121 1 COMe H H Me H 122 2 COMe H H Me H 123 3 COMe H H Me H 124 4 COMe H H Me H 125 1 CO.sub.2Me H H Me H 126 2 CO.sub.2Me H H Me H 127 3 CO.sub.2Me H H Me H 128 4 CO.sub.2Me H H Me H 129 1 CO.sub.2tBu H H Me H 130 2 CO.sub.2tBu H H Me H 131 3 CO.sub.2tBu H H Me H 132 4 CO.sub.2tBu H H Me H 133 1 CONHMe H H Me H 134 2 CONHMe H H Me H 135 3 CONHMe H H Me H 136 4 CONHMe H H Me H 137 1 SO.sub.2Me H H Me H 138 2 SO.sub.2Me H H Me H 139 3 SO.sub.2Me H H Me H 140 4 SO.sub.2Me H H Me H 141 1 SO.sub.2NH.sub.2 H H Me H 142 2 SO.sub.2NH.sub.2 H H Me H 143 3 SO.sub.2NH.sub.2 H H Me H 144 4 SO.sub.2NH.sub.2 H H Me H 145 1 H H H CF.sub.3 H 146 2 H H H CF.sub.3 H 147 3 H H H CF.sub.3 H 148 4 H H H CF.sub.3 H 149 1 Me H H CF.sub.3 H 150 2 Me H H CF.sub.3 H 151 3 Me H H CF.sub.3 H 152 4 Me H H CF.sub.3 H 153 1 CH.sub.2Ph H H CF.sub.3 H 154 2 CH.sub.2Ph H H CF.sub.3 H 155 3 CH.sub.2Ph H H CF.sub.3 H 156 4 CH.sub.2Ph H H CF.sub.3 H 157 1 COMe H H CF.sub.3 H 158 2 COMe H H CF.sub.3 H 159 3 COMe H H CF.sub.3 H 160 4 COMe H H CF.sub.3 H 161 1 CO.sub.2Me H H CF.sub.3 H 162 2 CO.sub.2Me H H CF.sub.3 H 163 3 CO.sub.2Me H H CF.sub.3 H 164 4 CO.sub.2Me H H CF.sub.3 H 165 1 CO.sub.2tBu H H CF.sub.3 H 166 2 CO.sub.2tBu H H CF.sub.3 H 167 3 CO.sub.2tBu H H CF.sub.3 H 168 4 CO.sub.2tBu H H CF.sub.3 H 169 1 CONHMe H H CF.sub.3 H 170 2 CONHMe H H CF.sub.3 H 171 3 CONHMe H H CF.sub.3 H 172 4 CONHMe H H CF.sub.3 H 173 1 SO.sub.2Me H H CF.sub.3 H 174 2 SO.sub.2Me H H CF.sub.3 H 175 3 SO.sub.2Me H H CF.sub.3 H 176 4 SO.sub.2Me H H CF.sub.3 H 177 1 SO.sub.2NH.sub.2 H H CF.sub.3 H 178 2 SO.sub.2NH.sub.2 H H CF.sub.3 H 179 3 SO.sub.2NH.sub.2 H H CF.sub.3 H 180 4 SO.sub.2NH.sub.2 H H CF.sub.3 H 181 1 H H H F H 182 2 H H H F H 183 3 H H H F H 184 4 H H H F H 185 1 Me H H F H 186 2 Me H H F H 187 3 Me H H F H 188 4 Me H H F H 189 1 CH.sub.2Ph H H F H 190 2 CH.sub.2Ph H H F H 191 3 CH.sub.2Ph H H F H 192 4 CH.sub.2Ph H H F H 193 1 COMe H H F H 194 2 COMe H H F H 195 3 COMe H H F H 196 4 COMe H H F H 197 1 CO.sub.2Me H H F H 198 2 CO.sub.2Me H H F H 199 3 CO.sub.2Me H H F H 200 4 CO.sub.2Me H H F H 201 1 CO.sub.2tBu H H F H 202 2 CO.sub.2tBu H H F H 203 3 CO.sub.2tBu H H F H 204 4 CO.sub.2tBu H H F H 205 1 CONHMe H H F H 206 2 CONHMe H H F H 207 3 CONHMe H H F H 208 4 CONHMe H H F H 209 1 SO.sub.2Me H H F H 210 2 SO.sub.2Me H H F H 211 3 SO.sub.2Me H H F H 212 4 SO.sub.2Me H H F H 213 1 SO.sub.2NH.sub.2 H H F H 214 2 SO.sub.2NH.sub.2 H H F H 215 3 SO.sub.2NH.sub.2 H H F H 216 4 SO.sub.2NH.sub.2 H H F H 217 1 H H H Cl H 218 2 H H H Cl H 219 3 H H H Cl H 220 4 H H H Cl H 221 1 Me H H Cl H 222 2 Me H H Cl H 223 3 Me H H Cl H 224 4 Me H H Cl H 225 1 CH.sub.2Ph H H Cl H 226 2 CH.sub.2Ph H H Cl H 227 3 CH.sub.2Ph H H Cl H 228 4 CH.sub.2Ph H H Cl H 229 1 COMe H H Cl H 230 2 COMe H H Cl H 231 3 COMe H H Cl H 232 4 COMe H H Cl H 233 1 CO.sub.2Me H H Cl H 234 2 CO.sub.2Me H H Cl H 235 3 CO.sub.2Me H H Cl H 236 4 CO.sub.2Me H H Cl H 237 1 CO.sub.2tBu H H Cl H 238 2 CO.sub.2tBu H H Cl H 239 3 CO.sub.2tBu H H Cl H 240 4 CO.sub.2tBu H H Cl H 241 1 CONHMe H H Cl H 242 2 CONHMe H H Cl H 243 3 CONHMe H H Cl H 244 4 CONHMe H H Cl H 245 1 SO.sub.2Me H H Cl H 246 2 SO.sub.2Me H H Cl H 247 3 SO.sub.2Me H H Cl H 248 4 SO.sub.2Me H H Cl H 249 1 SO.sub.2NH.sub.2 H H Cl H 250 2 SO.sub.2NH.sub.2 H H Cl H 251 3 SO.sub.2NH.sub.2 H H Cl H 252 4 SO.sub.2NH.sub.2 H H Cl H 253 1 H H H CN H 254 2 H H H CN H 255 3 H H H CN H 256 4 H H H CN H 257 1 Me H H CN H 258 2 Me H H CN H 259 3 Me H H CN H 260 4 Me H H CN H 261 1 CH.sub.2Ph H H CN H 262 2 CH.sub.2Ph H H CN H 263 3 CH.sub.2Ph H H CN H 264 4 CH.sub.2Ph H H CN H 265 1 COMe H H CN H 266 2 COMe H H CN H 267 3 COMe H H CN H 268 4 COMe H H CN H 269 1 CO.sub.2Me H H CN H 270 2 CO.sub.2Me H H CN H 271 3 CO.sub.2Me H H CN H 272 4 CO.sub.2Me H H CN H 273 1 CO.sub.2tBu H H CN H 274 2 CO.sub.2tBu H H CN H 275 3 CO.sub.2tBu H H CN H 276 4 CO.sub.2tBu H H CN H 277 1 CONHMe H H CN H 278 2 CONHMe H H CN H 279 3 CONHMe H H CN H 280 4 CONHMe H H CN H 281 1 SO.sub.2Me H H CN H 282 2 SO.sub.2Me H H CN H 283 3 SO.sub.2Me H H CN H 284 4 SO.sub.2Me H H CN H 285 1 SO.sub.2NH.sub.2 H H CN H 286 2 SO.sub.2NH.sub.2 H H CN H 287 3 SO.sub.2NH.sub.2 H H CN H 288 4 SO.sub.2NH.sub.2 H H CN H 289 1 H H OH H H 290 2 H H OH H H 291 3 H H OH H H 292 4 H H OH H H 293 1 Me H OH H H 294 2 Me H OH H H 295 3 Me H OH H H 296 4 Me H OH H H 297 1 CH.sub.2Ph H OH H H 298 2 CH.sub.2Ph H OH H H 299 3 CH.sub.2Ph H OH H H 300 4 CH.sub.2Ph H OH H H 301 1 COMe H OH H H 302 2 COMe H OH H H 303 3 COMe H OH H H 304 4 COMe H OH H H 305 1 CO.sub.2Me H OH H H 306 2 CO.sub.2Me H OH H H 307 3 CO.sub.2Me H OH H H 308 4 CO.sub.2Me H OH H H 309 1 CO.sub.2tBu H OH H H 310 2 CO.sub.2tBu H OH H H 311 3 CO.sub.2tBu H OH H H 312 4 CO.sub.2tBu H OH H H 313 1 CONHMe H OH H H 314 2 CONHMe H OH H H 315 3 CONHMe H OH H H 316 4 CONHMe H OH H H 317 1 SO.sub.2Me H OH H H 318 2 SO.sub.2Me H OH H H 319 3 SO.sub.2Me H OH H H 320 4 SO.sub.2Me H OH H H 321 1 SO.sub.2NH.sub.2 H OH H H 322 2 SO.sub.2NH.sub.2 H OH H H 323 3 SO.sub.2NH.sub.2 H OH H H 324 4 SO.sub.2NH.sub.2 H OH H H 325 1 H H OMe H H 326 2 H H OMe H H 327 3 H H OMe H H 328 4 H H OMe H H 329 1 Me H OMe H H 330 2 Me H OMe H H 331 3 Me H OMe H H 332 4 Me H OMe H H 333 1 CH.sub.2Ph H OMe H H 334 2 CH.sub.2Ph H OMe H H 335 3 CH.sub.2Ph H OMe H H 336 4 CH.sub.2Ph H OMe H H 337 1 COMe H OMe H H 338 2 COMe H OMe H H 339 3 COMe H OMe H H 340 4 COMe H OMe H H 341 1 CO.sub.2Me H OMe H H 342 2 CO.sub.2Me H OMe H H 343 3 CO.sub.2Me H OMe H H 344 4 CO.sub.2Me H OMe H H 345 1 CO.sub.2tBu H OMe H H 346 2 CO.sub.2tBu H OMe H H 347 3 CO.sub.2tBu H OMe H H 348 4 CO.sub.2tBu H OMe H H 349 1 CONHMe H OMe H H 350 2 CONHMe H OMe H H 351 3 CONHMe H OMe H H 352 4 CONHMe H OMe H H 353 1 SO.sub.2Me H OMe H H 354 2 SO.sub.2Me H OMe H H 355 3 SO.sub.2Me H OMe H H 356 4 SO.sub.2Me H OMe H H 357 1 SO.sub.2NH.sub.2 H OMe H H 358 2 SO.sub.2NH.sub.2 H OMe H H 359 3 SO.sub.2NH.sub.2 H OMe H H 360 4 SO.sub.2NH.sub.2 H OMe H H 361 1 H H Me H H 362 2 H H Me H H 363 3 H H Me H H 364 4 H H Me H H 365 1 Me H Me H H 366 2 Me H Me H H 367 3 Me H Me H H 368 4 Me H Me H H 369 1 CH.sub.2Ph H Me H H 370 2 CH.sub.2Ph H Me H H 371 3 CH.sub.2Ph H Me H H 372 4 CH.sub.2Ph H Me H H 373 1 COMe H Me H H 374 2 COMe H Me H H 375 3 COMe H Me H H 376 4 COMe H Me H H 377 1 CO.sub.2Me H Me H H 378 2 CO.sub.2Me H Me H H 379 3 CO.sub.2Me H Me H H 380 4 CO.sub.2Me H Me H H 381 1 CO.sub.2tBu H Me H H 382 2 CO.sub.2tBu H Me H H 383 3 CO.sub.2tBu H Me H H 384 4 CO.sub.2tBu H Me H H 385 1 CONHMe H Me H H 386 2 CONHMe H Me H H 387 3 CONHMe H Me H H 388 4 CONHMe H Me H H 389 1 SO.sub.2Me H Me H H 390 2 SO.sub.2Me H Me H H 391 3 SO.sub.2Me H Me H H 392 4 SO.sub.2Me H Me H H 393 1 SO.sub.2NH.sub.2 H Me H H 394 2 SO.sub.2NH.sub.2 H Me H H 395 3 SO.sub.2NH.sub.2 H Me H H 396 4 SO.sub.2NH.sub.2 H Me H H 397 1 H H CF.sub.3 H H 398 2 H H CF.sub.3 H H 399 3 H H CF.sub.3 H H 400 4 H H CF.sub.3 H H 401 1 Me H CF.sub.3 H H 402 2 Me H CF.sub.3 H H 403 3 Me H CF.sub.3 H H 404 4 Me H CF.sub.3 H H 405 1 CH.sub.2Ph H CF.sub.3 H H 406 2 CH.sub.2Ph H CF.sub.3 H H 407 3 CH.sub.2Ph H CF.sub.3 H H 408 4 CH.sub.2Ph H CF.sub.3 H H 409 1 COMe H CF.sub.3 H H 410 2 COMe H CF.sub.3 H H 411 3 COMe H CF.sub.3 H H 412 4 COMe H CF.sub.3 H H 413 1 CO.sub.2Me H CF.sub.3 H H 414 2 CO.sub.2Me H CF.sub.3 H H 415 3 CO.sub.2Me H CF.sub.3 H H 416 4 CO.sub.2Me H CF.sub.3 H H 417 1 CO.sub.2tBu H CF.sub.3 H H 418 2 CO.sub.2tBu H CF.sub.3 H H 419 3 CO.sub.2tBu H CF.sub.3 H H 420 4 CO.sub.2tBu H CF.sub.3 H H 421 1 CONHMe H CF.sub.3 H H 422 2 CONHMe H CF.sub.3 H H 423 3 CONHMe H CF.sub.3 H H 424 4 CONHMe H CF.sub.3 H H 425 1 SO.sub.2Me H CF.sub.3 H H 426 2 SO.sub.2Me H CF.sub.3 H H 427 3 SO.sub.2Me H CF.sub.3 H H 428 4 SO.sub.2Me H CF.sub.3 H H 429 1 SO.sub.2NH.sub.2 H CF.sub.3 H H 430 2 SO.sub.2NH.sub.2 H CF.sub.3 H H 431 3 SO.sub.2NH.sub.2 H CF.sub.3 H H 432 4 SO.sub.2NH.sub.2 H CF.sub.3 H H 433 1 H H F H H 434 2 H H F H H 435 3 H H F H H 436 3 H H F H H 437 1 Me H F H H 438 2 Me H F H H 439 3 Me H F H H 440 4 Me H F H H 441 1 CH.sub.2Ph H F H H 442 2 CH.sub.2Ph H F H H 443 3 CH.sub.2Ph H F H H 444 4 CH.sub.2Ph H F H H 445 1 COMe H F H H 446 2 COMe H F H H 447 3 COMe H F H H 448 4 COMe H F H H 449 1 CO.sub.2Me H F H H 450 2 CO.sub.2Me H F H H 451 3 CO.sub.2Me H F H H 452 4 CO.sub.2Me H F H H 453 1 CO.sub.2tBu H F H H 454 2 CO.sub.2tBu H F H H 455 3 CO.sub.2tBu H F H H 456 4 CO.sub.2tBu H F H H 457 1 CONHMe H F H H 458 2 CONHMe H F H H 459 3 CONHMe H F H H 460 4 CONHMe H F H H 461 1 SO.sub.2Me H F H H 462 2 SO.sub.2Me H F H H 463 3 SO.sub.2Me H F H H 464 4 SO.sub.2Me H F H H 465 1 SO.sub.2NH.sub.2 H F H H 466 2 SO.sub.2NH.sub.2 H F H H 467 3 SO.sub.2NH.sub.2 H F H H 468 4 SO.sub.2NH.sub.2 H F H H 469 1 H H Cl H H 470 2 H H Cl H H 471 3 H H Cl H H 472 4 H H Cl H H 473 1 Me H Cl H H 474 2 Me H Cl H H 475 3 Me H Cl H H 476 4 Me H Cl H H 477 1 CH.sub.2Ph H Cl H H 478 2 CH.sub.2Ph H Cl H H 479 3 CH.sub.2Ph H Cl H H 480 4 CH.sub.2Ph H Cl H H 481 1 COMe H Cl H H 482 2 COMe H Cl H H 483 3 COMe H Cl H H 484 4 COMe H Cl H H 485 1 CO.sub.2Me H Cl H H 486 2 CO.sub.2Me H Cl H H 487 3 CO.sub.2Me H Cl H H 488 4 CO.sub.2Me H Cl H H 489 1 CO.sub.2tBu H Cl H H 490 2 CO.sub.2tBu H Cl H H 491 3 CO.sub.2tBu H Cl H H 492 4 CO.sub.2tBu H Cl H H 493 1 CONHMe H Cl H H 494 2 CONHMe H Cl H H 495 3 CONHMe H Cl H H 496 4 CONHMe H Cl H H 497 1 SO.sub.2Me H Cl H H 498 2 SO.sub.2Me H Cl H H 499 3 SO.sub.2Me H Cl H H 500 4 SO.sub.2Me H Cl H H 501 1 SO.sub.2NH.sub.2 H Cl H H 502 2 SO.sub.2NH.sub.2 H Cl H H 503 3 SO.sub.2NH.sub.2 H Cl H H 504 4 SO.sub.2NH.sub.2 H Cl H H 505 1 H H CN H H 506 2 H H CN H H 507 3 H H CN H H 508 4 H H CN H H 509 1 Me H CN H H 510 2 Me H CN H H 511 3 Me H CN H H 512 4 Me H CN H H 513 1 CH.sub.2Ph H CN H H 514 2 CH.sub.2Ph H CN H H 515 3 CH.sub.2Ph H CN H H 516 4 CH.sub.2Ph H CN H H 517 1 COMe H CN H H 518 2 COMe H CN H H 519 3 COMe H CN H H 520 4 COMe H CN H H 521 1 CO.sub.2Me H CN H H 522 2 CO.sub.2Me H CN H H 523 3 CO.sub.2Me H CN H H 524 4 CO.sub.2Me H CN H H 525 1 CO.sub.2tBu H CN H H 526 2 CO.sub.2tBu H CN H H 527 3 CO.sub.2tBu H CN H H 528 4 CO.sub.2tBu H CN H H 529 1 CONHMe H CN H H 530 2 CONHMe H CN H H 531 3 CONHMe H CN H H 532 4 CONHMe H CN H H 533 1 SO.sub.2Me H CN H H 534 2 SO.sub.2Me H CN H H 535 3 SO.sub.2Me H CN H H 536 4 SO.sub.2Me H CN H H 537 1 SO.sub.2NH.sub.2 H CN H H 538 2 SO.sub.2NH.sub.2 H CN H H 539 3 SO.sub.2NH.sub.2 H CN H H 540 4 SO.sub.2NH.sub.2 H CN H H 541 1 H OH H H H 542 2 H OH H H H 543 3 H OH H H H 544 4 H OH H H H 545 1 Me OH H H H 546 2 Me OH H H H 547 3 Me OH H H H 548 4 Me OH H H H 549 1 CH.sub.2Ph OH H H H 550 2 CH.sub.2Ph OH H H H 551 3 CH.sub.2Ph OH H H H 552 4 CH.sub.2Ph OH H H H 553 1 COMe OH H H H 554 2 COMe OH H H H 555 3 COMe OH H H H 556 4 COMe OH H H H 557 1 CO.sub.2Me OH H H H 558 2 CO.sub.2Me OH H H H 559 3 CO.sub.2Me OH H H H 560 4 CO.sub.2Me OH H H H 561 1 CO.sub.2tBu OH H H H 562 2 CO.sub.2tBu OH H H H 563 3 CO.sub.2tBu OH H H H 564 4 CO.sub.2tBu OH H H H 565 1 CONHMe OH H H H 566 2 CONHMe OH H H H 567 3 CONHMe OH H H H 568 4 CONHMe OH H H H 569 1 SO.sub.2Me OH H H H 570 2 SO.sub.2Me OH H H H 571 3 SO.sub.2Me OH H H H 572 4 SO.sub.2Me OH H H H 573 1 SO.sub.2NH.sub.2 OH H H H 574 2 SO.sub.2NH.sub.2 OH H H H 575 3 SO.sub.2NH.sub.2 OH H H H 576 4 SO.sub.2NH.sub.2 OH H H H 577 1 H OMe H H H 578 2 H OMe H H H 579 3 H OMe H H H 580 4 H OMe H H H 581 1 Me OMe H H H 582 2 Me OMe H H H 583 3 Me OMe H H H 584 4 Me OMe H H H 585 1 CH.sub.2Ph OMe H H H 586 2 CH.sub.2Ph OMe H H H 587 3 CH.sub.2Ph OMe H H H 588 4 CH.sub.2Ph OMe H H H 589 1 COMe OMe H H H 590 2 COMe OMe H H H 591 3 COMe OMe H H H 592 4 COMe OMe H H H 593 1 CO.sub.2Me OMe H H H 594 2 CO.sub.2Me OMe H H H 595 3 CO.sub.2Me OMe H H H 596 4 CO.sub.2Me OMe H H H 597 1 CO.sub.2tBu OMe H H H 598 2 CO.sub.2tBu OMe H H H 599 3 CO.sub.2tBu OMe H H H 600 4 CO.sub.2tBu OMe H H H 601 1 CONHMe OMe H H H 602 2 CONHMe OMe H H H 603 3 CONHMe OMe H H H 604 4 CONHMe OMe H H H 605 1 SO.sub.2Me OMe H H H 606 2 SO.sub.2Me OMe H H H 607 3 SO.sub.2Me OMe H H H 608 4 SO.sub.2Me OMe H H H 609 1 SO.sub.2NH.sub.2 OMe H H H 610 2 SO.sub.2NH.sub.2 OMe H H H 611 3 SO.sub.2NH.sub.2 OMe H H H 612 4 SO.sub.2NH.sub.2 OMe H H H 613 1 H Me H H H 614 2 H Me H H H 615 3 H Me H H H 616 4 H Me H H H 617 1 Me Me H H H 618 2 Me Me H H H 619 3 Me Me H H H 620 4 Me Me H H H 621 1 CH.sub.2Ph Me H H H 622 2 CH.sub.2Ph Me H H H 623 3 CH.sub.2Ph Me H H H 624 4 CH.sub.2Ph Me H H H 625 1 COMe Me H H H 626 2 COMe Me H H H 627 3 COMe Me H H H 628 4 COMe Me H H H 629 1 CO.sub.2Me Me H H H 630 2 CO.sub.2Me Me H H H 631 3 CO.sub.2Me Me H H H 632 4 CO.sub.2Me Me H H H 633 1 CO.sub.2tBu Me H H H 634 2 CO.sub.2tBu Me H H H 635 3 CO.sub.2tBu Me H H H 636 4 CO.sub.2tBu Me H H H 637 1 CONHMe Me H H H 638 2 CONHMe Me H H H 639 3 CONHMe Me H H H 640 4 CONHMe Me H H H 641 1 SO.sub.2Me Me H H H 642 2 SO.sub.2Me Me H H H 643 3 SO.sub.2Me Me H H H 644 4 SO.sub.2Me Me H H H 645 1 SO.sub.2NH.sub.2 Me H H H 646 2 SO.sub.2NH.sub.2 Me H H H 647 3 SO.sub.2NH.sub.2 Me H H H 648 4 SO.sub.2NH.sub.2 Me H H H 649 1 H CF.sub.3 H H H 650 2 H CF.sub.3 H H H 651 3 H CF.sub.3 H H H 652 4 H CF.sub.3 H H H 653 1 Me CF.sub.3 H H H 654 2 Me CF.sub.3 H H H 655 3 Me CF.sub.3 H H H 656 4 Me CF.sub.3 H H H 657 1 CH.sub.2Ph CF.sub.3 H H H 658 2 CH.sub.2Ph CF.sub.3 H H H 659 3 CH.sub.2Ph CF.sub.3 H H H 660 4 CH.sub.2Ph CF.sub.3 H H H 661 1 COMe CF.sub.3 H H H 662 2 COMe CF.sub.3 H H H 663 3 COMe CF.sub.3 H H H 664 4 COMe CF.sub.3 H H H 665 1 CO.sub.2Me CF.sub.3 H H H 666 2 CO.sub.2Me CF.sub.3 H H H 667 3 CO.sub.2Me CF.sub.3 H H H 668 4 CO.sub.2Me CF.sub.3 H H H 669 1 CO.sub.2tBu CF.sub.3 H H H 670 2 CO.sub.2tBu CF.sub.3 H H H 671 3 CO.sub.2tBu CF.sub.3 H H H 672 4 CO.sub.2tBu CF.sub.3 H H H 673 1 CONHMe CF.sub.3 H H H 674 2 CONHMe CF.sub.3 H H H 675 3 CONHMe CF.sub.3 H H H 676 4 CONHMe CF.sub.3 H H H 677 1 SO.sub.2Me CF.sub.3 H H H 678 2 SO.sub.2Me CF.sub.3 H H H 679 3 SO.sub.2Me CF.sub.3 H H H 680 4 SO.sub.2Me CF.sub.3 H H H 681 1 SO.sub.2NH.sub.2 CF.sub.3 H H H 682 2 SO.sub.2NH.sub.2 CF.sub.3 H H H 683 3 SO.sub.2NH.sub.2 CF.sub.3 H H H 684 4 SO.sub.2NH.sub.2 CF.sub.3 H H H 685 1 H F H H H 686 2 H F H H H 687 3 H F H H H 688 3 H F H H H 689 1 Me F H H H 690 2 Me F H H H 691 3 Me F H H H 692 4 Me F H H H 693 1 CH.sub.2Ph F H H H 694 2 CH.sub.2Ph F H H H 695 3 CH.sub.2Ph F H H H 696 4 CH.sub.2Ph F H H H 697 1 COMe F H H H 698 2 COMe F H H H 699 3 COMe F H H H 700 4 COMe F H H H 701 1 CO.sub.2Me F H H H 702 2 CO.sub.2Me F H H H 703 3 CO.sub.2Me F H H H 704 4 CO.sub.2Me F H H H 705 1 CO.sub.2tBu F H H H 706 2 CO.sub.2tBu F H H H 707 3 CO.sub.2tBu F H H H 708 4 CO.sub.2tBu F H H H 709 1 CONHMe F H H H 710 2 CONHMe F H H H 711 3 CONHMe F H H H 712 4 CONHMe F H H H 713 1 SO.sub.2Me F H H H 714 2 SO.sub.2Me F H H H 715 3 SO.sub.2Me F H H H 716 4 SO.sub.2Me F H H H 717 1 SO.sub.2NH.sub.2 F H H H 718 2 SO.sub.2NH.sub.2 F H H H 719 3 SO.sub.2NH.sub.2 F H H H 720 4 SO.sub.2NH.sub.2 F H H H 721 1 H Cl H H H 722 2 H Cl H H H 723 3 H Cl H H H 724 4 H Cl H H H 725 1 Me Cl H H H 726 2 Me Cl H H H 727 3 Me Cl H H H 728 4 Me Cl H H H 729 1 CH.sub.2Ph Cl H H H 730 2 CH.sub.2Ph Cl H H H 731 3 CH.sub.2Ph Cl H H H 732 4 CH.sub.2Ph Cl H H H 733 1 COMe Cl H H H 734 2 COMe Cl H H H 735 3 COMe Cl H H H 736 4 COMe Cl H H H 737 1 CO.sub.2Me Cl H H H 738 2 CO.sub.2Me Cl H H H 739 3 CO.sub.2Me Cl H H H 740 4 CO.sub.2Me Cl H H H 741 1 CO.sub.2tBu Cl H H H 742 2 CO.sub.2tBu Cl H H H 743 3 CO.sub.2tBu Cl H H H 744 4 CO.sub.2tBu Cl H H H 745 1 CONHMe Cl H H H 746 2 CONHMe Cl H H H 747 3 CONHMe Cl H H H 748 4 CONHMe Cl H H H 749 1 SO.sub.2Me Cl H H H 750 2 SO.sub.2Me Cl H H H 751 3 SO.sub.2Me Cl H H H 752 4 SO.sub.2Me Cl H H H 753 1 SO.sub.2NH.sub.2 Cl H H H 754 2 SO.sub.2NH.sub.2 Cl H H H 755 3 SO.sub.2NH.sub.2 Cl H H H 756 4 SO.sub.2NH.sub.2 Cl H H H 757 1 H CN H H H 758 2 H CN H H H 759 3 H CN H H H 760 4 H CN H H H 761 1 Me CN H H H 762 2 Me CN H H H 763 3 Me CN H H H 764 4 Me CN H H H 765 1 CH.sub.2Ph CN H H H 766 2 CH.sub.2Ph CN H H H 767 3 CH.sub.2Ph CN H H H 768 4 CH.sub.2Ph CN H H H 769 1 COMe CN H H H 770 2 COMe CN H H H 771 3 COMe CN H H H 772 4 COMe CN H H H 773 1 CO.sub.2Me CN H H H 774 2 CO.sub.2Me CN H H H 775 3 CO.sub.2Me CN H H H 776 4 CO.sub.2Me CN H H H 777 1 CO.sub.2tBu CN H H H 778 2 CO.sub.2tBu CN H H H 779 3 CO.sub.2tBu CN H H H 780 4 CO.sub.2tBu CN H H H 781 1 CONHMe CN H H H 782 2 CONHMe CN H H H 783 3 CONHMe CN H H H 784 4 CONHMe CN H H H 785 1 SO.sub.2Me CN H H H 786 2 SO.sub.2Me CN H H H 787 3 SO.sub.2Me CN H H H 788 4 SO.sub.2Me CN H H H 789 1 SO.sub.2NH.sub.2 CN H H H 790 2 SO.sub.2NH.sub.2 CN H H H 791 3 SO.sub.2NH.sub.2 CN H H H 792 4 SO.sub.2NH.sub.2 CN H H H 793 1 H H H H OH 794 2 H H H H OH 795 3 H H H H OH 796 4 H H H H OH 797 1 Me H H H OH 798 2 Me H H H OH 799 3 Me H H H OH 800 4 Me H H H OH 801 1 CH.sub.2Ph H H H OH 802 2 CH.sub.2Ph H H H OH 803 3 CH.sub.2Ph H H H OH 804 4 CH.sub.2Ph H H H OH 805 1 COMe H H H OH 806 2 COMe H H H OH 807 3 COMe H H H OH 808 4 COMe H H H OH 809 1 CO.sub.2Me H H H OH 810 2 CO.sub.2Me H H H OH 811 3 CO.sub.2Me H H H OH 812 4 CO.sub.2Me H H H OH 813 1 CO.sub.2tBu H H H OH 814 2 CO.sub.2tBu H H H OH 815 3 CO.sub.2tBu H H H OH 816 4 CO.sub.2tBu H H H OH 817 1 CONHMe H H H OH 818 2 CONHMe H H H OH 819 3 CONHMe H H H OH 820 4 CONHMe H H H OH 821 1 SO.sub.2Me H H H OH 822 2 SO.sub.2Me H H H OH 823 3 SO.sub.2Me H H H OH 824 4 SO.sub.2Me H H H OH 825 1 SO.sub.2NH.sub.2 H H H OH 826 2 SO.sub.2NH.sub.2 H H H OH 827 3 SO.sub.2NH.sub.2 H H H OH 828 4 SO.sub.2NH.sub.2 H H H OH 829 1 H H H H OMe 830 2 H H H H OMe 831 3 H H H H OMe 832 4 H H H H OMe 833 1 Me H H H OMe 834 2 Me H H H OMe 835 3 Me H H H OMe 836 4 Me H H H OMe 837 1 CH.sub.2Ph H H H OMe 838 2 CH.sub.2Ph H H H OMe 839 3 CH.sub.2Ph H H H OMe 840 4 CH.sub.2Ph H H H OMe 841 1 COMe H H H OMe 842 2 COMe H H H OMe 843 3 COMe H H H OMe 844 4 COMe H H H OMe 845 1 CO.sub.2Me H H H OMe 846 2 CO.sub.2Me H H H OMe 847 3 CO.sub.2Me H H H OMe 848 4 CO.sub.2Me H H H OMe 849 1 CO.sub.2tBu H H H OMe 850 2 CO.sub.2tBu H H H OMe 851 3 CO.sub.2tBu H H H OMe 852 4 CO.sub.2tBu H H H OMe 853 1 CONHMe H H H OMe 854 2 CONHMe H H H OMe 855 3 CONHMe H H H OMe 856 4 CONHMe H H H OMe 857 1 SO.sub.2Me H H H OMe 858 2 SO.sub.2Me H H H OMe 859 3 SO.sub.2Me H H H OMe 860 4 SO.sub.2Me H H H OMe 861 1 SO.sub.2NH.sub.2 H H H OMe 862 2 SO.sub.2NH.sub.2 H H H OMe 863 3 SO.sub.2NH.sub.2 H H H OMe 864 4 SO.sub.2NH.sub.2 H H H OMe 865 1 H H H H Me 866 2 H H H H Me 867 3 H H H H Me 868 4 H H H H Me 869 1 Me H H H Me 870 2 Me H H H Me 871 3 Me H H H Me 872 4 Me H H H Me 873 1 CH.sub.2Ph H H H Me 874 2 CH.sub.2Ph H H H Me 875 3 CH.sub.2Ph H H H Me 876 4 CH.sub.2Ph H H H Me 877 1 COMe H H H Me 878 2 COMe H H H Me 879 3 COMe H H H Me 880 4 COMe H H H Me 881 1 CO.sub.2Me H H H Me 882 2 CO.sub.2Me H H H Me 883 3 CO.sub.2Me H H H Me 884 4 CO.sub.2Me H H H Me 885 1 CO.sub.2tBu H H H Me 886 2 CO.sub.2tBu H H H Me 887 3 CO.sub.2tBu H H H Me 888 4 CO.sub.2tBu H H H Me 889 1 CONHMe H H H Me 890 2 CONHMe H H H Me 891 3 CONHMe H H H Me 892 4 CONHMe H H H Me 893 1 SO.sub.2Me H H H Me 894 2 SO.sub.2Me H H H Me 895 3 SO.sub.2Me H H H Me 896 4 SO.sub.2Me H H H Me 897 1 SO.sub.2NH.sub.2 H H H Me 898 2 SO.sub.2NH.sub.2 H H H Me 899 3 SO.sub.2NH.sub.2 H H H Me 900 4 SO.sub.2NH.sub.2 H H H Me 901 1 H H H H CF.sub.3 902 2 H H H H CF.sub.3 903 3 H H H H CF.sub.3 904 4 H H H H CF.sub.3 905 1 Me H H H CF.sub.3 906 2 Me H H H CF.sub.3 907 3 Me H H H CF.sub.3 908 4 Me H H H CF.sub.3 909 1 CH.sub.2Ph H H H CF.sub.3 910 2 CH.sub.2Ph H H H CF.sub.3 911 3 CH.sub.2Ph H H H CF.sub.3 912 4 CH.sub.2Ph H H H CF.sub.3 913 1 COMe H H H CF.sub.3 914 2 COMe H H H CF.sub.3 915 3 COMe H H H CF.sub.3 916 4 COMe H H H CF.sub.3 917 1 CO.sub.2Me H H H CF.sub.3 918 2 CO.sub.2Me H H H CF.sub.3 919 3 CO.sub.2Me H H H CF.sub.3 920 4 CO.sub.2Me H H H CF.sub.3 921 1 CO.sub.2tBu H H H CF.sub.3 922 2 CO.sub.2tBu H H H CF.sub.3 923 3 CO.sub.2tBu H H H CF.sub.3 924 4 CO.sub.2tBu H H H CF.sub.3 925 1 CONHMe H H H CF.sub.3 926 2 CONHMe H H H CF.sub.3 927 3 CONHMe H H H CF.sub.3 928 4 CONHMe H H H CF.sub.3 929 1 SO.sub.2Me H H H CF.sub.3 930 2 SO.sub.2Me H H H CF.sub.3 931 3 SO.sub.2Me H H H CF.sub.3 932 4 SO.sub.2Me H H H CF.sub.3 933 1 SO.sub.2NH.sub.2 H H H CF.sub.3 934 2 SO.sub.2NH.sub.2 H H H CF.sub.3 935 3 SO.sub.2NH.sub.2 H H H CF.sub.3 936 4 SO.sub.2NH.sub.2 H H H CF.sub.3 937 1 H H H H F 938 2 H H H H F 939 3 H H H H F 940 3 H H H H F 941 1 Me H H H F 942 2 Me H H H F 943 3 Me H H H F 944 4 Me H H H F 945 1 CH.sub.2Ph H H H F 946 2 CH.sub.2Ph H H H F 947 3 CH.sub.2Ph H H H F 948 4 CH.sub.2Ph H H H F 949 1 COMe H H H F 950 2 COMe H H H F 951 3 COMe H H H F 952 4 COMe H H H F 953 1 CO.sub.2Me H H H F 954 2 CO.sub.2Me H H H F 955 3 CO.sub.2Me H H H F 956 4 CO.sub.2Me H H H F 957 1 CO.sub.2tBu H H H F 958 2 CO.sub.2tBu H H H F 959 3 CO.sub.2tBu H H H F 960 4 CO.sub.2tBu H H H F 961 1 CONHMe H H H F 962 2 CONHMe H H H F 963 3 CONHMe H H H F 964 4 CONHMe H H H F 965 1 SO.sub.2Me H H H F 966 2 SO.sub.2Me H H H F 967 3 SO.sub.2Me H H H F 968 4 SO.sub.2Me H H H F 969 1 SO.sub.2NH.sub.2 H H H F 970 2 SO.sub.2NH.sub.2 H H H F 971 3 SO.sub.2NH.sub.2 H H H F 972 4 SO.sub.2NH.sub.2 H H H F 973 1 H H H H Cl 974 2 H H H H Cl 975 3 H H H H Cl 976 4 H H H H Cl 977 1 Me H H H Cl 978 2 Me H H H Cl 979 3 Me H H H Cl 980 4 Me H H H Cl 981 1 CH.sub.2Ph H H H Cl 982 2 CH.sub.2Ph H H H Cl 983 3 CH.sub.2Ph H H H Cl 984 4 CH.sub.2Ph H H H Cl 985 1 COMe H H H Cl 986 2 COMe H H H Cl 987 3 COMe H H H Cl 988 4 COMe H H H Cl 989 1 CO.sub.2Me H H H Cl 990 2 CO.sub.2Me H H H Cl 991 3 CO.sub.2Me H H H Cl 992 4 CO.sub.2Me H H H Cl 993 1 CO.sub.2tBu H H H Cl 994 2 CO.sub.2tBu H H H Cl 995 3 CO.sub.2tBu H H H Cl 996 4 CO.sub.2tBu H H H Cl 997 1 CONHMe H H H Cl 998 2 CONHMe H H H Cl 999 3 CONHMe H H H Cl 1000 4 CONHMe H H H Cl 1001 1 SO.sub.2Me H H H Cl 1002 2 SO.sub.2Me H H H Cl 1003 3 SO.sub.2Me H H H Cl 1004 4 SO.sub.2Me H H H Cl 1005 1 SO.sub.2NH.sub.2 H H H Cl 1006 2 SO.sub.2NH.sub.2 H H H Cl 1007 3 SO.sub.2NH.sub.2 H H H Cl 1008 4 SO.sub.2NH.sub.2 H H H Cl 1009 1 H H H H CN 1010 2 H H H H CN 1011 3 H H H H CN 1012 4 H H H H CN 1013 1 Me H H H CN 1014 2 Me H H H CN 1015 3 Me H H H CN 1016 4 Me H H H CN 1017 1 CH.sub.2Ph H H H CN 1018 2 CH.sub.2Ph H H H CN 1019 3 CH.sub.2Ph H H H CN 1020 4 CH.sub.2Ph H H H CN 1021 1 COMe H H H CN 1022 2 COMe H H H CN 1023 3 COMe H H H CN 1024 4 COMe H H H CN 1025 1 CO.sub.2Me H H H CN 1026 2 CO.sub.2Me H H H CN 1027 3 CO.sub.2Me H H H CN 1028 4 CO.sub.2Me H H H CN 1029 1 CO.sub.2tBu H H H CN 1030 2 CO.sub.2tBu H H H CN 1031 3 CO.sub.2tBu H H H CN 1032 4 CO.sub.2tBu H H H CN 1033 1 CONHMe H H H CN 1034 2 CONHMe H H H CN 1035 3 CONHMe H H H CN 1036 4 CONHMe H H H CN 1037 1 SO.sub.2Me H H H CN 1038 2 SO.sub.2Me H H H CN 1039 3 SO.sub.2Me H H H CN 1040 4 SO.sub.2Me H H H CN 1041 1 SO.sub.2NH.sub.2 H H H CN 1042 2 SO.sub.2NH.sub.2 H H H CN 1043 3 SO.sub.2NH.sub.2 H H H CN 1044 4 SO.sub.2NH.sub.2 H H H CN

    [2040] Exemplary embodiments include compounds having the formula (XXX)

    ##STR00445##

    [2041] or a pharmaceutically acceptable salt form thereof defined herein below in Table 24.

    TABLE-US-00024 TABLE 24 Entry n R.sup.7 R.sup.20a R.sup.20b R.sup.20c R.sup.20e 1 1 H H H H H 2 2 H H H H H 3 3 H H H H H 4 4 H H H H H 5 1 Me H H H H 6 2 Me H H H H 7 3 Me H H H H 8 4 Me H H H H 9 1 CH.sub.2Ph H H H H 10 2 CH.sub.2Ph H H H H 11 3 CH.sub.2Ph H H H H 12 4 CH.sub.2Ph H H H H 13 1 COMe H H H H 14 2 COMe H H H H 15 3 COMe H H H H 16 4 COMe H H H H 17 1 CO.sub.2Me H H H H 18 2 CO.sub.2Me H H H H 19 3 CO.sub.2Me H H H H 20 4 CO.sub.2Me H H H H 21 1 CO.sub.2tBu H H H H 22 2 CO.sub.2tBu H H H H 23 3 CO.sub.2tBu H H H H 24 4 CO.sub.2tBu H H H H 25 1 CONHMe H H H H 26 2 CONHMe H H H H 27 3 CONHMe H H H H 28 4 CONHMe H H H H 29 1 SO.sub.2Me H H H H 30 2 SO.sub.2Me H H H H 31 3 SO.sub.2Me H H H H 32 4 SO.sub.2Me H H H H 33 1 SO.sub.2NH.sub.2 H H H H 34 2 SO.sub.2NH.sub.2 H H H H 35 3 SO.sub.2NH.sub.2 H H H H 36 4 SO.sub.2NH.sub.2 H H H H 37 1 H H H OH H 38 2 H H H OH H 39 3 H H H OH H 40 4 H H H OH H 41 1 Me H H OH H 42 2 Me H H OH H 43 3 Me H H OH H 44 4 Me H H OH H 45 1 CH.sub.2Ph H H OH H 46 2 CH.sub.2Ph H H OH H 47 3 CH.sub.2Ph H H OH H 48 4 CH.sub.2Ph H H OH H 49 1 COMe H H OH H 50 2 COMe H H OH H 51 3 COMe H H OH H 52 4 COMe H H OH H 53 1 CO.sub.2Me H H OH H 54 2 CO.sub.2Me H H OH H 55 3 CO.sub.2Me H H OH H 56 4 CO.sub.2Me H H OH H 57 1 CO.sub.2tBu H H OH H 58 2 CO.sub.2tBu H H OH H 59 3 CO.sub.2tBu H H OH H 60 4 CO.sub.2tBu H H OH H 61 1 CONHMe H H OH H 62 2 CONHMe H H OH H 63 3 CONHMe H H OH H 64 4 CONHMe H H OH H 65 1 SO.sub.2Me H H OH H 66 2 SO.sub.2Me H H OH H 67 3 SO.sub.2Me H H OH H 68 4 SO.sub.2Me H H OH H 69 1 SO.sub.2NH.sub.2 H H OH H 70 2 SO.sub.2NH.sub.2 H H OH H 71 3 SO.sub.2NH.sub.2 H H OH H 72 4 SO.sub.2NH.sub.2 H H OH H 73 1 H H H OMe H 74 2 H H H OMe H 75 3 H H H OMe H 76 4 H H H OMe H 77 1 Me H H OMe H 78 2 Me H H OMe H 79 3 Me H H OMe H 80 4 Me H H OMe H 81 1 CH.sub.2Ph H H OMe H 82 2 CH.sub.2Ph H H OMe H 83 3 CH.sub.2Ph H H OMe H 84 4 CH.sub.2Ph H H OMe H 85 1 COMe H H OMe H 86 2 COMe H H OMe H 87 3 COMe H H OMe H 88 4 COMe H H OMe H 89 1 CO.sub.2Me H H OMe H 90 2 CO.sub.2Me H H OMe H 91 3 CO.sub.2Me H H OMe H 92 4 CO.sub.2Me H H OMe H 93 1 CO.sub.2tBu H H OMe H 94 2 CO.sub.2tBu H H OMe H 95 3 CO.sub.2tBu H H OMe H 96 1 CO.sub.2tBu H H OMe H 97 1 CONHMe H H OMe H 98 2 CONHMe H H OMe H 99 3 CONHMe H H OMe H 100 4 CONHMe H H OMe H 101 1 SO.sub.2Me H H OMe H 102 2 SO.sub.2Me H H OMe H 103 3 SO.sub.2Me H H OMe H 104 4 SO.sub.2Me H H OMe H 105 1 SO.sub.2NH.sub.2 H H OMe H 106 2 SO.sub.2NH.sub.2 H H OMe H 107 3 SO.sub.2NH.sub.2 H H OMe H 108 4 SO.sub.2NH.sub.2 H H OMe H 109 1 H H H Me H 110 2 H H H Me H 111 3 H H H Me H 112 4 H H H Me H 113 1 Me H H Me H 114 2 Me H H Me H 115 3 Me H H Me H 116 4 Me H H Me H 117 1 CH.sub.2Ph H H Me H 118 2 CH.sub.2Ph H H Me H 119 3 CH.sub.2Ph H H Me H 120 4 CH.sub.2Ph H H Me H 121 1 COMe H H Me H 122 2 COMe H H Me H 123 3 COMe H H Me H 124 4 COMe H H Me H 125 1 CO.sub.2Me H H Me H 126 2 CO.sub.2Me H H Me H 127 3 CO.sub.2Me H H Me H 128 4 CO.sub.2Me H H Me H 129 1 CO.sub.2tBu H H Me H 130 2 CO.sub.2tBu H H Me H 131 3 CO.sub.2tBu H H Me H 132 4 CO.sub.2tBu H H Me H 133 1 CONHMe H H Me H 134 2 CONHMe H H Me H 135 3 CONHMe H H Me H 136 4 CONHMe H H Me H 137 1 SO.sub.2Me H H Me H 138 2 SO.sub.2Me H H Me H 139 3 SO.sub.2Me H H Me H 140 4 SO.sub.2Me H H Me H 141 1 SO.sub.2NH.sub.2 H H Me H 142 2 SO.sub.2NH.sub.2 H H Me H 143 3 SO.sub.2NH.sub.2 H H Me H 144 4 SO.sub.2NH.sub.2 H H Me H 145 1 H H H CF.sub.3 H 146 2 H H H CF.sub.3 H 147 3 H H H CF.sub.3 H 148 4 H H H CF.sub.3 H 149 1 Me H H CF.sub.3 H 150 2 Me H H CF.sub.3 H 151 3 Me H H CF.sub.3 H 152 4 Me H H CF.sub.3 H 153 1 CH.sub.2Ph H H CF.sub.3 H 154 2 CH.sub.2Ph H H CF.sub.3 H 155 3 CH.sub.2Ph H H CF.sub.3 H 156 4 CH.sub.2Ph H H CF.sub.3 H 157 1 COMe H H CF.sub.3 H 158 2 COMe H H CF.sub.3 H 159 3 COMe H H CF.sub.3 H 160 4 COMe H H CF.sub.3 H 161 1 CO.sub.2Me H H CF.sub.3 H 162 2 CO.sub.2Me H H CF.sub.3 H 163 3 CO.sub.2Me H H CF.sub.3 H 164 4 CO.sub.2Me H H CF.sub.3 H 165 1 CO.sub.2tBu H H CF.sub.3 H 166 2 CO.sub.2tBu H H CF.sub.3 H 167 3 CO.sub.2tBu H H CF.sub.3 H 168 4 CO.sub.2tBu H H CF.sub.3 H 169 1 CONHMe H H CF.sub.3 H 170 2 CONHMe H H CF.sub.3 H 171 3 CONHMe H H CF.sub.3 H 172 4 CONHMe H H CF.sub.3 H 173 1 SO.sub.2Me H H CF.sub.3 H 174 2 SO.sub.2Me H H CF.sub.3 H 175 3 SO.sub.2Me H H CF.sub.3 H 176 4 SO.sub.2Me H H CF.sub.3 H 177 1 SO.sub.2NH.sub.2 H H CF.sub.3 H 178 2 SO.sub.2NH.sub.2 H H CF.sub.3 H 179 3 SO.sub.2NH.sub.2 H H CF.sub.3 H 180 4 SO.sub.2NH.sub.2 H H CF.sub.3 H 181 1 H H H F H 182 2 H H H F H 183 3 H H H F H 184 4 H H H F H 185 1 Me H H F H 186 2 Me H H F H 187 3 Me H H F H 188 4 Me H H F H 189 1 CH.sub.2Ph H H F H 190 2 CH.sub.2Ph H H F H 191 3 CH.sub.2Ph H H F H 192 4 CH.sub.2Ph H H F H 193 1 COMe H H F H 194 2 COMe H H F H 195 3 COMe H H F H 196 4 COMe H H F H 197 1 CO.sub.2Me H H F H 198 2 CO.sub.2Me H H F H 199 3 CO.sub.2Me H H F H 200 4 CO.sub.2Me H H F H 201 1 CO.sub.2tBu H H F H 202 2 CO.sub.2tBu H H F H 203 3 CO.sub.2tBu H H F H 204 4 CO.sub.2tBu H H F H 205 1 CONHMe H H F H 206 2 CONHMe H H F H 207 3 CONHMe H H F H 208 4 CONHMe H H F H 209 1 SO.sub.2Me H H F H 210 2 SO.sub.2Me H H F H 211 3 SO.sub.2Me H H F H 212 4 SO.sub.2Me H H F H 213 1 SO.sub.2NH.sub.2 H H F H 214 2 SO.sub.2NH.sub.2 H H F H 215 3 SO.sub.2NH.sub.2 H H F H 216 4 SO.sub.2NH.sub.2 H H F H 217 1 H H H Cl H 218 2 H H H Cl H 219 3 H H H Cl H 220 4 H H H Cl H 221 1 Me H H Cl H 222 2 Me H H Cl H 223 3 Me H H Cl H 224 4 Me H H Cl H 225 1 CH.sub.2Ph H H Cl H 226 2 CH.sub.2Ph H H Cl H 227 3 CH.sub.2Ph H H Cl H 228 4 CH.sub.2Ph H H Cl H 229 1 COMe H H Cl H 230 2 COMe H H Cl H 231 3 COMe H H Cl H 232 4 COMe H H Cl H 233 1 CO.sub.2Me H H Cl H 234 2 CO.sub.2Me H H Cl H 235 3 CO.sub.2Me H H Cl H 236 4 CO.sub.2Me H H Cl H 237 1 CO.sub.2tBu H H Cl H 238 2 CO.sub.2tBu H H Cl H 239 3 CO.sub.2tBu H H Cl H 240 4 CO.sub.2tBu H H Cl H 241 1 CONHMe H H Cl H 242 2 CONHMe H H Cl H 243 3 CONHMe H H Cl H 244 4 CONHMe H H Cl H 245 1 SO.sub.2Me H H Cl H 246 2 SO.sub.2Me H H Cl H 247 3 SO.sub.2Me H H Cl H 248 4 SO.sub.2Me H H Cl H 249 1 SO.sub.2NH.sub.2 H H Cl H 250 2 SO.sub.2NH.sub.2 H H Cl H 251 3 SO.sub.2NH.sub.2 H H Cl H 252 4 SO.sub.2NH.sub.2 H H Cl H 253 1 H H H CN H 254 2 H H H CN H 255 3 H H H CN H 256 4 H H H CN H 257 1 Me H H CN H 258 2 Me H H CN H 259 3 Me H H CN H 260 4 Me H H CN H 261 1 CH.sub.2Ph H H CN H 262 2 CH.sub.2Ph H H CN H 263 3 CH.sub.2Ph H H CN H 264 4 CH.sub.2Ph H H CN H 265 1 COMe H H CN H 266 2 COMe H H CN H 267 3 COMe H H CN H 268 4 COMe H H CN H 269 1 CO.sub.2Me H H CN H 270 2 CO.sub.2Me H H CN H 271 3 CO.sub.2Me H H CN H 272 4 CO.sub.2Me H H CN H 273 1 CO.sub.2tBu H H CN H 274 2 CO.sub.2tBu H H CN H 275 3 CO.sub.2tBu H H CN H 276 4 CO.sub.2tBu H H CN H 277 1 CONHMe H H CN H 278 2 CONHMe H H CN H 279 3 CONHMe H H CN H 280 4 CONHMe H H CN H 281 1 SO.sub.2Me H H CN H 282 2 SO.sub.2Me H H CN H 283 3 SO.sub.2Me H H CN H 284 4 SO.sub.2Me H H CN H 285 1 SO.sub.2NH.sub.2 H H CN H 286 2 SO.sub.2NH.sub.2 H H CN H 287 3 SO.sub.2NH.sub.2 H H CN H 288 4 SO.sub.2NH.sub.2 H H CN H 289 1 H H OH H H 290 2 H H OH H H 291 3 H H OH H H 292 4 H H OH H H 293 1 Me H OH H H 294 2 Me H OH H H 295 3 Me H OH H H 296 4 Me H OH H H 297 1 CH.sub.2Ph H OH H H 298 2 CH.sub.2Ph H OH H H 299 3 CH.sub.2Ph H OH H H 300 4 CH.sub.2Ph H OH H H 301 1 COMe H OH H H 302 2 COMe H OH H H 303 3 COMe H OH H H 304 4 COMe H OH H H 305 1 CO.sub.2Me H OH H H 306 2 CO.sub.2Me H OH H H 307 3 CO.sub.2Me H OH H H 308 4 CO.sub.2Me H OH H H 309 1 CO.sub.2tBu H OH H H 310 2 CO.sub.2tBu H OH H H 311 3 CO.sub.2tBu H OH H H 312 4 CO.sub.2tBu H OH H H 313 1 CONHMe H OH H H 314 2 CONHMe H OH H H 315 3 CONHMe H OH H H 316 4 CONHMe H OH H H 317 1 SO.sub.2Me H OH H H 318 2 SO.sub.2Me H OH H H 319 3 SO.sub.2Me H OH H H 320 4 SO.sub.2Me H OH H H 321 1 SO.sub.2NH.sub.2 H OH H H 322 2 SO.sub.2NH.sub.2 H OH H H 323 3 SO.sub.2NH.sub.2 H OH H H 324 4 SO.sub.2NH.sub.2 H OH H H 325 1 H H OMe H H 326 2 H H OMe H H 327 3 H H OMe H H 328 4 H H OMe H H 329 1 Me H OMe H H 330 2 Me H OMe H H 331 3 Me H OMe H H 332 4 Me H OMe H H 333 1 CH.sub.2Ph H OMe H H 334 2 CH.sub.2Ph H OMe H H 335 3 CH.sub.2Ph H OMe H H 336 4 CH.sub.2Ph H OMe H H 337 1 COMe H OMe H H 338 2 COMe H OMe H H 339 3 COMe H OMe H H 340 4 COMe H OMe H H 341 1 CO.sub.2Me H OMe H H 342 2 CO.sub.2Me H OMe H H 343 3 CO.sub.2Me H OMe H H 344 4 CO.sub.2Me H OMe H H 345 1 CO.sub.2tBu H OMe H H 346 2 CO.sub.2tBu H OMe H H 347 3 CO.sub.2tBu H OMe H H 348 4 CO.sub.2tBu H OMe H H 349 1 CONHMe H OMe H H 350 2 CONHMe H OMe H H 351 3 CONHMe H OMe H H 352 4 CONHMe H OMe H H 353 1 SO.sub.2Me H OMe H H 354 2 SO.sub.2Me H OMe H H 355 3 SO.sub.2Me H OMe H H 356 4 SO.sub.2Me H OMe H H 357 1 SO.sub.2NH.sub.2 H OMe H H 358 2 SO.sub.2NH.sub.2 H OMe H H 359 3 SO.sub.2NH.sub.2 H OMe H H 360 4 SO.sub.2NH.sub.2 H OMe H H 361 1 H H Me H H 362 2 H H Me H H 363 3 H H Me H H 364 4 H H Me H H 365 1 Me H Me H H 366 2 Me H Me H H 367 3 Me H Me H H 368 4 Me H Me H H 369 1 CH.sub.2Ph H Me H H 370 2 CH.sub.2Ph H Me H H 371 3 CH.sub.2Ph H Me H H 372 4 CH.sub.2Ph H Me H H 373 1 COMe H Me H H 374 2 COMe H Me H H 375 3 COMe H Me H H 376 4 COMe H Me H H 377 1 CO.sub.2Me H Me H H 378 2 CO.sub.2Me H Me H H 379 3 CO.sub.2Me H Me H H 380 4 CO.sub.2Me H Me H H 381 1 CO.sub.2tBu H Me H H 382 2 CO.sub.2tBu H Me H H 383 3 CO.sub.2tBu H Me H H 384 4 CO.sub.2tBu H Me H H 385 1 CONHMe H Me H H 386 2 CONHMe H Me H H 387 3 CONHMe H Me H H 388 4 CONHMe H Me H H 389 1 SO.sub.2Me H Me H H 390 2 SO.sub.2Me H Me H H 391 3 SO.sub.2Me H Me H H 392 4 SO.sub.2Me H Me H H 393 1 SO.sub.2NH.sub.2 H Me H H 394 2 SO.sub.2NH.sub.2 H Me H H 395 3 SO.sub.2NH.sub.2 H Me H H 396 4 SO.sub.2NH.sub.2 H Me H H 397 1 H H CF.sub.3 H H 398 2 H H CF.sub.3 H H 399 3 H H CF.sub.3 H H 400 4 H H CF.sub.3 H H 401 1 Me H CF.sub.3 H H 402 2 Me H CF.sub.3 H H 403 3 Me H CF.sub.3 H H 404 4 Me H CF.sub.3 H H 405 1 CH.sub.2Ph H CF.sub.3 H H 406 2 CH.sub.2Ph H CF.sub.3 H H 407 3 CH.sub.2Ph H CF.sub.3 H H 408 4 CH.sub.2Ph H CF.sub.3 H H 409 1 COMe H CF.sub.3 H H 410 2 COMe H CF.sub.3 H H 411 3 COMe H CF.sub.3 H H 412 4 COMe H CF.sub.3 H H 413 1 CO.sub.2Me H CF.sub.3 H H 414 2 CO.sub.2Me H CF.sub.3 H H 415 3 CO.sub.2Me H CF.sub.3 H H 416 4 CO.sub.2Me H CF.sub.3 H H 417 1 CO.sub.2tBu H CF.sub.3 H H 418 2 CO.sub.2tBu H CF.sub.3 H H 419 3 CO.sub.2tBu H CF.sub.3 H H 420 4 CO.sub.2tBu H CF.sub.3 H H 421 1 CONHMe H CF.sub.3 H H 422 2 CONHMe H CF.sub.3 H H 423 3 CONHMe H CF.sub.3 H H 424 4 CONHMe H CF.sub.3 H H 425 1 SO.sub.2Me H CF.sub.3 H H 426 2 SO.sub.2Me H CF.sub.3 H H 427 3 SO.sub.2Me H CF.sub.3 H H 428 4 SO.sub.2Me H CF.sub.3 H H 429 1 SO.sub.2NH.sub.2 H CF.sub.3 H H 430 2 SO.sub.2NH.sub.2 H CF.sub.3 H H 431 3 SO.sub.2NH.sub.2 H CF.sub.3 H H 432 4 SO.sub.2NH.sub.2 H CF.sub.3 H H 433 1 H H F H H 434 2 H H F H H 435 3 H H F H H 436 3 H H F H H 437 1 Me H F H H 438 2 Me H F H H 439 3 Me H F H H 440 4 Me H F H H 441 1 CH.sub.2Ph H F H H 442 2 CH.sub.2Ph H F H H 443 3 CH.sub.2Ph H F H H 444 4 CH.sub.2Ph H F H H 445 1 COMe H F H H 446 2 COMe H F H H 447 3 COMe H F H H 448 4 COMe H F H H 449 1 CO.sub.2Me H F H H 450 2 CO.sub.2Me H F H H 451 3 CO.sub.2Me H F H H 452 4 CO.sub.2Me H F H H 453 1 CO.sub.2tBu H F H H 454 2 CO.sub.2tBu H F H H 455 3 CO.sub.2tBu H F H H 456 4 CO.sub.2tBu H F H H 457 1 CONHMe H F H H 458 2 CONHMe H F H H 459 3 CONHMe H F H H 460 4 CONHMe H F H H 461 1 SO.sub.2Me H F H H 462 2 SO.sub.2Me H F H H 463 3 SO.sub.2Me H F H H 464 4 SO.sub.2Me H F H H 465 1 SO.sub.2NH.sub.2 H F H H 466 2 SO.sub.2NH.sub.2 H F H H 467 3 SO.sub.2NH.sub.2 H F H H 468 4 SO.sub.2NH.sub.2 H F H H 469 1 H H Cl H H 470 2 H H Cl H H 471 3 H H Cl H H 472 4 H H Cl H H 473 1 Me H Cl H H 474 2 Me H Cl H H 475 3 Me H Cl H H 476 4 Me H Cl H H 477 1 CH.sub.2Ph H Cl H H 478 2 CH.sub.2Ph H Cl H H 479 3 CH.sub.2Ph H Cl H H 480 4 CH.sub.2Ph H Cl H H 481 1 COMe H Cl H H 482 2 COMe H Cl H H 483 3 COMe H Cl H H 484 4 COMe H Cl H H 485 1 CO.sub.2Me H Cl H H 486 2 CO.sub.2Me H Cl H H 487 3 CO.sub.2Me H Cl H H 488 4 CO.sub.2Me H Cl H H 489 1 CO.sub.2tBu H Cl H H 490 2 CO.sub.2tBu H Cl H H 491 3 CO.sub.2tBu H Cl H H 492 4 CO.sub.2tBu H Cl H H 493 1 CONHMe H Cl H H 494 2 CONHMe H Cl H H 495 3 CONHMe H Cl H H 496 4 CONHMe H Cl H H 497 1 SO.sub.2Me H Cl H H 498 2 SO.sub.2Me H Cl H H 499 3 SO.sub.2Me H Cl H H 500 4 SO.sub.2Me H Cl H H 501 1 SO.sub.2NH.sub.2 H Cl H H 502 2 SO.sub.2NH.sub.2 H Cl H H 503 3 SO.sub.2NH.sub.2 H Cl H H 504 4 SO.sub.2NH.sub.2 H Cl H H 505 1 H H CN H H 506 2 H H CN H H 507 3 H H CN H H 508 4 H H CN H H 509 1 Me H CN H H 510 2 Me H CN H H 511 3 Me H CN H H 512 4 Me H CN H H 513 1 CH.sub.2Ph H CN H H 514 2 CH.sub.2Ph H CN H H 515 3 CH.sub.2Ph H CN H H 516 4 CH.sub.2Ph H CN H H 517 1 COMe H CN H H 518 2 COMe H CN H H 519 3 COMe H CN H H 520 4 COMe H CN H H 521 1 CO.sub.2Me H CN H H 522 2 CO.sub.2Me H CN H H 523 3 CO.sub.2Me H CN H H 524 4 CO.sub.2Me H CN H H 525 1 CO.sub.2tBu H CN H H 526 2 CO.sub.2tBu H CN H H 527 3 CO.sub.2tBu H CN H H 528 4 CO.sub.2tBu H CN H H 529 1 CONHMe H CN H H 530 2 CONHMe H CN H H 531 3 CONHMe H CN H H 532 4 CONHMe H CN H H 533 1 SO.sub.2Me H CN H H 534 2 SO.sub.2Me H CN H H 535 3 SO.sub.2Me H CN H H 536 4 SO.sub.2Me H CN H H 537 1 SO.sub.2NH.sub.2 H CN H H 538 2 SO.sub.2NH.sub.2 H CN H H 539 3 SO.sub.2NH.sub.2 H CN H H 540 4 SO.sub.2NH.sub.2 H CN H H 541 1 H OH H H H 542 2 H OH H H H 543 3 H OH H H H 544 4 H OH H H H 545 1 Me OH H H H 546 2 Me OH H H H 547 3 Me OH H H H 548 4 Me OH H H H 549 1 CH.sub.2Ph OH H H H 550 2 CH.sub.2Ph OH H H H 551 3 CH.sub.2Ph OH H H H 552 4 CH.sub.2Ph OH H H H 553 1 COMe OH H H H 554 2 COMe OH H H H 555 3 COMe OH H H H 556 4 COMe OH H H H 557 1 CO.sub.2Me OH H H H 558 2 CO.sub.2Me OH H H H 559 3 CO.sub.2Me OH H H H 560 4 CO.sub.2Me OH H H H 561 1 CO.sub.2tBu OH H H H 562 2 CO.sub.2tBu OH H H H 563 3 CO.sub.2tBu OH H H H 564 4 CO.sub.2tBu OH H H H 565 1 CONHMe OH H H H 566 2 CONHMe OH H H H 567 3 CONHMe OH H H H 568 4 CONHMe OH H H H 569 1 SO.sub.2Me OH H H H 570 2 SO.sub.2Me OH H H H 571 3 SO.sub.2Me OH H H H 572 4 SO.sub.2Me OH H H H 573 1 SO.sub.2NH.sub.2 OH H H H 574 2 SO.sub.2NH.sub.2 OH H H H 575 3 SO.sub.2NH.sub.2 OH H H H 576 4 SO.sub.2NH.sub.2 OH H H H 577 1 H OMe H H H 578 2 H OMe H H H 579 3 H OMe H H H 580 4 H OMe H H H 581 1 Me OMe H H H 582 2 Me OMe H H H 583 3 Me OMe H H H 584 4 Me OMe H H H 585 1 CH.sub.2Ph OMe H H H 586 2 CH.sub.2Ph OMe H H H 587 3 CH.sub.2Ph OMe H H H 588 4 CH.sub.2Ph OMe H H H 589 1 COMe OMe H H H 590 2 COMe OMe H H H 591 3 COMe OMe H H H 592 4 COMe OMe H H H 593 1 CO.sub.2Me OMe H H H 594 2 CO.sub.2Me OMe H H H 595 3 CO.sub.2Me OMe H H H 596 4 CO.sub.2Me OMe H H H 597 1 CO.sub.2tBu OMe H H H 598 2 CO.sub.2tBu OMe H H H 599 3 CO.sub.2tBu OMe H H H 600 4 CO.sub.2tBu OMe H H H 601 1 CONHMe OMe H H H 602 2 CONHMe OMe H H H 603 3 CONHMe OMe H H H 604 4 CONHMe OMe H H H 605 1 SO.sub.2Me OMe H H H 606 2 SO.sub.2Me OMe H H H 607 3 SO.sub.2Me OMe H H H 608 4 SO.sub.2Me OMe H H H 609 1 SO.sub.2NH.sub.2 OMe H H H 610 2 SO.sub.2NH.sub.2 OMe H H H 611 3 SO.sub.2NH.sub.2 OMe H H H 612 4 SO.sub.2NH.sub.2 OMe H H H 613 1 H Me H H H 614 2 H Me H H H 615 3 H Me H H H 616 4 H Me H H H 617 1 Me Me H H H 618 2 Me Me H H H 619 3 Me Me H H H 620 4 Me Me H H H 621 1 CH.sub.2Ph Me H H H 622 2 CH.sub.2Ph Me H H H 623 3 CH.sub.2Ph Me H H H 624 4 CH.sub.2Ph Me H H H 625 1 COMe Me H H H 626 2 COMe Me H H H 627 3 COMe Me H H H 628 4 COMe Me H H H 629 1 CO.sub.2Me Me H H H 630 2 CO.sub.2Me Me H H H 631 3 CO.sub.2Me Me H H H 632 4 CO.sub.2Me Me H H H 633 1 CO.sub.2tBu Me H H H 634 2 CO.sub.2tBu Me H H H 635 3 CO.sub.2tBu Me H H H 636 4 CO.sub.2tBu Me H H H 637 1 CONHMe Me H H H 638 2 CONHMe Me H H H 639 3 CONHMe Me H H H 640 4 CONHMe Me H H H 641 1 SO.sub.2Me Me H H H 642 2 SO.sub.2Me Me H H H 643 3 SO.sub.2Me Me H H H 644 4 SO.sub.2Me Me H H H 645 1 SO.sub.2NH.sub.2 Me H H H 646 2 SO.sub.2NH.sub.2 Me H H H 647 3 SO.sub.2NH.sub.2 Me H H H 648 4 SO.sub.2NH.sub.2 Me H H H 649 1 H CF.sub.3 H H H 650 2 H CF.sub.3 H H H 651 3 H CF.sub.3 H H H 652 4 H CF.sub.3 H H H 653 1 Me CF.sub.3 H H H 654 2 Me CF.sub.3 H H H 655 3 Me CF.sub.3 H H H 656 4 Me CF.sub.3 H H H 657 1 CH.sub.2Ph CF.sub.3 H H H 658 2 CH.sub.2Ph CF.sub.3 H H H 659 3 CH.sub.2Ph CF.sub.3 H H H 660 4 CH.sub.2Ph CF.sub.3 H H H 661 1 COMe CF.sub.3 H H H 662 2 COMe CF.sub.3 H H H 663 3 COMe CF.sub.3 H H H 664 4 COMe CF.sub.3 H H H 665 1 CO.sub.2Me CF.sub.3 H H H 666 2 CO.sub.2Me CF.sub.3 H H H 667 3 CO.sub.2Me CF.sub.3 H H H 668 4 CO.sub.2Me CF.sub.3 H H H 669 1 CO.sub.2tBu CF.sub.3 H H H 670 2 CO.sub.2tBu CF.sub.3 H H H 671 3 CO.sub.2tBu CF.sub.3 H H H 672 4 CO.sub.2tBu CF.sub.3 H H H 673 1 CONHMe CF.sub.3 H H H 674 2 CONHMe CF.sub.3 H H H 675 3 CONHMe CF.sub.3 H H H 676 4 CONHMe CF.sub.3 H H H 677 1 SO.sub.2Me CF.sub.3 H H H 678 2 SO.sub.2Me CF.sub.3 H H H 679 3 SO.sub.2Me CF.sub.3 H H H 680 4 SO.sub.2Me CF.sub.3 H H H 681 1 SO.sub.2NH.sub.2 CF.sub.3 H H H 682 2 SO.sub.2NH.sub.2 CF.sub.3 H H H 683 3 SO.sub.2NH.sub.2 CF.sub.3 H H H 684 4 SO.sub.2NH.sub.2 CF.sub.3 H H H 685 1 H F H H H 686 2 H F H H H 687 3 H F H H H 688 3 H F H H H 689 1 Me F H H H 690 2 Me F H H H 691 3 Me F H H H 692 4 Me F H H H 693 1 CH.sub.2Ph F H H H 694 2 CH.sub.2Ph F H H H 695 3 CH.sub.2Ph F H H H 696 4 CH.sub.2Ph F H H H 697 1 COMe F H H H 698 2 COMe F H H H 699 3 COMe F H H H 700 4 COMe F H H H 701 1 CO.sub.2Me F H H H 702 2 CO.sub.2Me F H H H 703 3 CO.sub.2Me F H H H 704 4 CO.sub.2Me F H H H 705 1 CO.sub.2tBu F H H H 706 2 CO.sub.2tBu F H H H 707 3 CO.sub.2tBu F H H H 708 4 CO.sub.2tBu F H H H 709 1 CONHMe F H H H 710 2 CONHMe F H H H 711 3 CONHMe F H H H 712 4 CONHMe F H H H 713 1 SO.sub.2Me F H H H 714 2 SO.sub.2Me F H H H 715 3 SO.sub.2Me F H H H 716 4 SO.sub.2Me F H H H 717 1 SO.sub.2NH.sub.2 F H H H 718 2 SO.sub.2NH.sub.2 F H H H 719 3 SO.sub.2NH.sub.2 F H H H 720 4 SO.sub.2NH.sub.2 F H H H 721 1 H Cl H H H 722 2 H Cl H H H 723 3 H Cl H H H 724 4 H Cl H H H 725 1 Me Cl H H H 726 2 Me Cl H H H 727 3 Me Cl H H H 728 4 Me Cl H H H 729 1 CH.sub.2Ph Cl H H H 730 2 CH.sub.2Ph Cl H H H 731 3 CH.sub.2Ph Cl H H H 732 4 CH.sub.2Ph Cl H H H 733 1 COMe Cl H H H 734 2 COMe Cl H H H 735 3 COMe Cl H H H 736 4 COMe Cl H H H 737 1 CO.sub.2Me Cl H H H 738 2 CO.sub.2Me Cl H H H 739 3 CO.sub.2Me Cl H H H 740 4 CO.sub.2Me Cl H H H 741 1 CO.sub.2tBu Cl H H H 742 2 CO.sub.2tBu Cl H H H 743 3 CO.sub.2tBu Cl H H H 744 4 CO.sub.2tBu Cl H H H 745 1 CONHMe Cl H H H 746 2 CONHMe Cl H H H 747 3 CONHMe Cl H H H 748 4 CONHMe Cl H H H 749 1 SO.sub.2Me Cl H H H 750 2 SO.sub.2Me Cl H H H 751 3 SO.sub.2Me Cl H H H 752 4 SO.sub.2Me Cl H H H 753 1 SO.sub.2NH.sub.2 Cl H H H 754 2 SO.sub.2NH.sub.2 Cl H H H 755 3 SO.sub.2NH.sub.2 Cl H H H 756 4 SO.sub.2NH.sub.2 Cl H H H 757 1 H CN H H H 758 2 H CN H H H 759 3 H CN H H H 760 4 H CN H H H 761 1 Me CN H H H 762 2 Me CN H H H 763 3 Me CN H H H 764 4 Me CN H H H 765 1 CH.sub.2Ph CN H H H 766 2 CH.sub.2Ph CN H H H 767 3 CH.sub.2Ph CN H H H 768 4 CH.sub.2Ph CN H H H 769 1 COMe CN H H H 770 2 COMe CN H H H 771 3 COMe CN H H H 772 4 COMe CN H H H 773 1 CO.sub.2Me CN H H H 774 2 CO.sub.2Me CN H H H 775 3 CO.sub.2Me CN H H H 776 4 CO.sub.2Me CN H H H 777 1 CO.sub.2tBu CN H H H 778 2 CO.sub.2tBu CN H H H 779 3 CO.sub.2tBu CN H H H 780 4 CO.sub.2tBu CN H H H 781 1 CONHMe CN H H H 782 2 CONHMe CN H H H 783 3 CONHMe CN H H H 784 4 CONHMe CN H H H 785 1 SO.sub.2Me CN H H H 786 2 SO.sub.2Me CN H H H 787 3 SO.sub.2Me CN H H H 788 4 SO.sub.2Me CN H H H 789 1 SO.sub.2NH.sub.2 CN H H H 790 2 SO.sub.2NH.sub.2 CN H H H 791 3 SO.sub.2NH.sub.2 CN H H H 792 4 SO.sub.2NH.sub.2 CN H H H 793 1 H H H H OH 794 2 H H H H OH 795 3 H H H H OH 796 4 H H H H OH 797 1 Me H H H OH 798 2 Me H H H OH 799 3 Me H H H OH 800 4 Me H H H OH 801 1 CH.sub.2Ph H H H OH 802 2 CH.sub.2Ph H H H OH 803 3 CH.sub.2Ph H H H OH 804 4 CH.sub.2Ph H H H OH 805 1 COMe H H H OH 806 2 COMe H H H OH 807 3 COMe H H H OH 808 4 COMe H H H OH 809 1 CO.sub.2Me H H H OH 810 2 CO.sub.2Me H H H OH 811 3 CO.sub.2Me H H H OH 812 4 CO.sub.2Me H H H OH 813 1 CO.sub.2tBu H H H OH 814 2 CO.sub.2tBu H H H OH 815 3 CO.sub.2tBu H H H OH 816 4 CO.sub.2tBu H H H OH 817 1 CONHMe H H H OH 818 2 CONHMe H H H OH 819 3 CONHMe H H H OH 820 4 CONHMe H H H OH 821 1 SO.sub.2Me H H H OH 822 2 SO.sub.2Me H H H OH 823 3 SO.sub.2Me H H H OH 824 4 SO.sub.2Me H H H OH 825 1 SO.sub.2NH.sub.2 H H H OH 826 2 SO.sub.2NH.sub.2 H H H OH 827 3 SO.sub.2NH.sub.2 H H H OH 828 4 SO.sub.2NH.sub.2 H H H OH 829 1 H H H H OMe 830 2 H H H H OMe 831 3 H H H H OMe 832 4 H H H H OMe 833 1 Me H H H OMe 834 2 Me H H H OMe 835 3 Me H H H OMe 836 4 Me H H H OMe 837 1 CH.sub.2Ph H H H OMe 838 2 CH.sub.2Ph H H H OMe 839 3 CH.sub.2Ph H H H OMe 840 4 CH.sub.2Ph H H H OMe 841 1 COMe H H H OMe 842 2 COMe H H H OMe 843 3 COMe H H H OMe 844 4 COMe H H H OMe 845 1 CO.sub.2Me H H H OMe 846 2 CO.sub.2Me H H H OMe 847 3 CO.sub.2Me H H H OMe 848 4 CO.sub.2Me H H H OMe 849 1 CO.sub.2tBu H H H OMe 850 2 CO.sub.2tBu H H H OMe 851 3 CO.sub.2tBu H H H OMe 852 4 CO.sub.2tBu H H H OMe 853 1 CONHMe H H H OMe 854 2 CONHMe H H H OMe 855 3 CONHMe H H H OMe 856 4 CONHMe H H H OMe 857 1 SO.sub.2Me H H H OMe 858 2 SO.sub.2Me H H H OMe 859 3 SO.sub.2Me H H H OMe 860 4 SO.sub.2Me H H H OMe 861 1 SO.sub.2NH.sub.2 H H H OMe 862 2 SO.sub.2NH.sub.2 H H H OMe 863 3 SO.sub.2NH.sub.2 H H H OMe 864 4 SO.sub.2NH.sub.2 H H H OMe 865 1 H H H H Me 866 2 H H H H Me 867 3 H H H H Me 868 4 H H H H Me 869 1 Me H H H Me 870 2 Me H H H Me 871 3 Me H H H Me 872 4 Me H H H Me 873 1 CH.sub.2Ph H H H Me 874 2 CH.sub.2Ph H H H Me 875 3 CH.sub.2Ph H H H Me 876 4 CH.sub.2Ph H H H Me 877 1 COMe H H H Me 878 2 COMe H H H Me 879 3 COMe H H H Me 880 4 COMe H H H Me 881 1 CO.sub.2Me H H H Me 882 2 CO.sub.2Me H H H Me 883 3 CO.sub.2Me H H H Me 884 4 CO.sub.2Me H H H Me 885 1 CO.sub.2tBu H H H Me 886 2 CO.sub.2tBu H H H Me 887 3 CO.sub.2tBu H H H Me 888 4 CO.sub.2tBu H H H Me 889 1 CONHMe H H H Me 890 2 CONHMe H H H Me 891 3 CONHMe H H H Me 892 4 CONHMe H H H Me 893 1 SO.sub.2Me H H H Me 894 2 SO.sub.2Me H H H Me 895 3 SO.sub.2Me H H H Me 896 4 SO.sub.2Me H H H Me 897 1 SO.sub.2NH.sub.2 H H H Me 898 2 SO.sub.2NH.sub.2 H H H Me 899 3 SO.sub.2NH.sub.2 H H H Me 900 4 SO.sub.2NH.sub.2 H H H Me 901 1 H H H H CF.sub.3 902 2 H H H H CF.sub.3 903 3 H H H H CF.sub.3 904 4 H H H H CF.sub.3 905 1 Me H H H CF.sub.3 906 2 Me H H H CF.sub.3 907 3 Me H H H CF.sub.3 908 4 Me H H H CF.sub.3 909 1 CH.sub.2Ph H H H CF.sub.3 910 2 CH.sub.2Ph H H H CF.sub.3 911 3 CH.sub.2Ph H H H CF.sub.3 912 4 CH.sub.2Ph H H H CF.sub.3 913 1 COMe H H H CF.sub.3 914 2 COMe H H H CF.sub.3 915 3 COMe H H H CF.sub.3 916 4 COMe H H H CF.sub.3 917 1 CO.sub.2Me H H H CF.sub.3 918 2 CO.sub.2Me H H H CF.sub.3 919 3 CO.sub.2Me H H H CF.sub.3 920 4 CO.sub.2Me H H H CF.sub.3 921 1 CO.sub.2tBu H H H CF.sub.3 922 2 CO.sub.2tBu H H H CF.sub.3 923 3 CO.sub.2tBu H H H CF.sub.3 924 4 CO.sub.2tBu H H H CF.sub.3 925 1 CONHMe H H H CF.sub.3 926 2 CONHMe H H H CF.sub.3 927 3 CONHMe H H H CF.sub.3 928 4 CONHMe H H H CF.sub.3 929 1 SO.sub.2Me H H H CF.sub.3 930 2 SO.sub.2Me H H H CF.sub.3 931 3 SO.sub.2Me H H H CF.sub.3 932 4 SO.sub.2Me H H H CF.sub.3 933 1 SO.sub.2NH.sub.2 H H H CF.sub.3 934 2 SO.sub.2NH.sub.2 H H H CF.sub.3 935 3 SO.sub.2NH.sub.2 H H H CF.sub.3 936 4 SO.sub.2NH.sub.2 H H H CF.sub.3 937 1 H H H H F 938 2 H H H H F 939 3 H H H H F 940 3 H H H H F 941 1 Me H H H F 942 2 Me H H H F 943 3 Me H H H F 944 4 Me H H H F 945 1 CH.sub.2Ph H H H F 946 2 CH.sub.2Ph H H H F 947 3 CH.sub.2Ph H H H F 948 4 CH.sub.2Ph H H H F 949 1 COMe H H H F 950 2 COMe H H H F 951 3 COMe H H H F 952 4 COMe H H H F 953 1 CO.sub.2Me H H H F 954 2 CO.sub.2Me H H H F 955 3 CO.sub.2Me H H H F 956 4 CO.sub.2Me H H H F 957 1 CO.sub.2tBu H H H F 958 2 CO.sub.2tBu H H H F 959 3 CO.sub.2tBu H H H F 960 4 CO.sub.2tBu H H H F 961 1 CONHMe H H H F 962 2 CONHMe H H H F 963 3 CONHMe H H H F 964 4 CONHMe H H H F 965 1 SO.sub.2Me H H H F 966 2 SO.sub.2Me H H H F 967 3 SO.sub.2Me H H H F 968 4 SO.sub.2Me H H H F 969 1 SO.sub.2NH.sub.2 H H H F 970 2 SO.sub.2NH.sub.2 H H H F 971 3 SO.sub.2NH.sub.2 H H H F 972 4 SO.sub.2NH.sub.2 H H H F 973 1 H H H H Cl 974 2 H H H H Cl 975 3 H H H H Cl 976 4 H H H H Cl 977 1 Me H H H Cl 978 2 Me H H H Cl 979 3 Me H H H Cl 980 4 Me H H H Cl 981 1 CH.sub.2Ph H H H Cl 982 2 CH.sub.2Ph H H H Cl 983 3 CH.sub.2Ph H H H Cl 984 4 CH.sub.2Ph H H H Cl 985 1 COMe H H H Cl 986 2 COMe H H H Cl 987 3 COMe H H H Cl 988 4 COMe H H H Cl 989 1 CO.sub.2Me H H H Cl 990 2 CO.sub.2Me H H H Cl 991 3 CO.sub.2Me H H H Cl 992 4 CO.sub.2Me H H H Cl 993 1 CO.sub.2tBu H H H Cl 994 2 CO.sub.2tBu H H H Cl 995 3 CO.sub.2tBu H H H Cl 996 4 CO.sub.2tBu H H H Cl 997 1 CONHMe H H H Cl 998 2 CONHMe H H H Cl 999 3 CONHMe H H H Cl 1000 4 CONHMe H H H Cl 1001 1 SO.sub.2Me H H H Cl 1002 2 SO.sub.2Me H H H Cl 1003 3 SO.sub.2Me H H H Cl 1004 4 SO.sub.2Me H H H Cl 1005 1 SO.sub.2NH.sub.2 H H H Cl 1006 2 SO.sub.2NH.sub.2 H H H Cl 1007 3 SO.sub.2NH.sub.2 H H H Cl 1008 4 SO.sub.2NH.sub.2 H H H Cl 1009 1 H H H H CN 1010 2 H H H H CN 1011 3 H H H H CN 1012 4 H H H H CN 1013 1 Me H H H CN 1014 2 Me H H H CN 1015 3 Me H H H CN 1016 4 Me H H H CN 1017 1 CH.sub.2Ph H H H CN 1018 2 CH.sub.2Ph H H H CN 1019 3 CH.sub.2Ph H H H CN 1020 4 CH.sub.2Ph H H H CN 1021 1 COMe H H H CN 1022 2 COMe H H H CN 1023 3 COMe H H H CN 1024 4 COMe H H H CN 1025 1 CO.sub.2Me H H H CN 1026 2 CO.sub.2Me H H H CN 1027 3 CO.sub.2Me H H H CN 1028 4 CO.sub.2Me H H H CN 1029 1 CO.sub.2tBu H H H CN 1030 2 CO.sub.2tBu H H H CN 1031 3 CO.sub.2tBu H H H CN 1032 4 CO.sub.2tBu H H H CN 1033 1 CONHMe H H H CN 1034 2 CONHMe H H H CN 1035 3 CONHMe H H H CN 1036 4 CONHMe H H H CN 1037 1 SO.sub.2Me H H H CN 1038 2 SO.sub.2Me H H H CN 1039 3 SO.sub.2Me H H H CN 1040 4 SO.sub.2Me H H H CN 1041 1 SO.sub.2NH.sub.2 H H H CN 1042 2 SO.sub.2NH.sub.2 H H H CN 1043 3 SO.sub.2NH.sub.2 H H H CN 1044 4 SO.sub.2NH.sub.2 H H H CN

    [2042] Exemplary embodiments include compounds having the formula (XXXI)

    ##STR00446##

    [2043] or a pharmaceutically acceptable salt form thereof defined herein below in Table 25.

    TABLE-US-00025 TABLE 25 Entry n R.sup.7 R.sup.20a R.sup.20b R.sup.20d R.sup.20e 1 1 H H H H H 2 2 H H H H H 3 3 H H H H H 4 4 H H H H H 5 1 Me H H H H 6 2 Me H H H H 7 3 Me H H H H 8 4 Me H H H H 9 1 CH.sub.2Ph H H H H 10 2 CH.sub.2Ph H H H H 11 3 CH.sub.2Ph H H H H 12 4 CH.sub.2Ph H H H H 13 1 COMe H H H H 14 2 COMe H H H H 15 3 COMe H H H H 16 4 COMe H H H H 17 1 CO.sub.2Me H H H H 18 2 CO.sub.2Me H H H H 19 3 CO.sub.2Me H H H H 20 4 CO.sub.2Me H H H H 21 1 CO.sub.2tBu H H H H 22 2 CO.sub.2tBu H H H H 23 3 CO.sub.2tBu H H H H 24 4 CO.sub.2tBu H H H H 25 1 CONHMe H H H H 26 2 CONHMe H H H H 27 3 CONHMe H H H H 28 4 CONHMe H H H H 29 1 SO.sub.2Me H H H H 30 2 SO.sub.2Me H H H H 31 3 SO.sub.2Me H H H H 32 4 SO.sub.2Me H H H H 33 1 SO.sub.2NH.sub.2 H H H H 34 2 SO.sub.2NH.sub.2 H H H H 35 3 SO.sub.2NH.sub.2 H H H H 36 4 SO.sub.2NH.sub.2 H H H H 37 1 H H H OH H 38 2 H H H OH H 39 3 H H H OH H 40 4 H H H OH H 41 1 Me H H OH H 42 2 Me H H OH H 43 3 Me H H OH H 44 4 Me H H OH H 45 1 CH.sub.2Ph H H OH H 46 2 CH.sub.2Ph H H OH H 47 3 CH.sub.2Ph H H OH H 48 4 CH.sub.2Ph H H OH H 49 1 COMe H H OH H 50 2 COMe H H OH H 51 3 COMe H H OH H 52 4 COMe H H OH H 53 1 CO.sub.2Me H H OH H 54 2 CO.sub.2Me H H OH H 55 3 CO.sub.2Me H H OH H 56 4 CO.sub.2Me H H OH H 57 1 CO.sub.2tBu H H OH H 58 2 CO.sub.2tBu H H OH H 59 3 CO.sub.2tBu H H OH H 60 4 CO.sub.2tBu H H OH H 61 1 CONHMe H H OH H 62 2 CONHMe H H OH H 63 3 CONHMe H H OH H 64 4 CONHMe H H OH H 65 1 SO.sub.2Me H H OH H 66 2 SO.sub.2Me H H OH H 67 3 SO.sub.2Me H H OH H 68 4 SO.sub.2Me H H OH H 69 1 SO.sub.2NH.sub.2 H H OH H 70 2 SO.sub.2NH.sub.2 H H OH H 71 3 SO.sub.2NH.sub.2 H H OH H 72 4 SO.sub.2NH.sub.2 H H OH H 73 1 H H H OMe H 74 2 H H H OMe H 75 3 H H H OMe H 76 4 H H H OMe H 77 1 Me H H OMe H 78 2 Me H H OMe H 79 3 Me H H OMe H 80 4 Me H H OMe H 81 1 CH.sub.2Ph H H OMe H 82 2 CH.sub.2Ph H H OMe H 83 3 CH.sub.2Ph H H OMe H 84 4 CH.sub.2Ph H H OMe H 85 1 COMe H H OMe H 86 2 COMe H H OMe H 87 3 COMe H H OMe H 88 4 COMe H H OMe H 89 1 CO.sub.2Me H H OMe H 90 2 CO.sub.2Me H H OMe H 91 3 CO.sub.2Me H H OMe H 92 4 CO.sub.2Me H H OMe H 93 1 CO.sub.2tBu H H OMe H 94 2 CO.sub.2tBu H H OMe H 95 3 CO.sub.2tBu H H OMe H 96 1 CO.sub.2tBu H H OMe H 97 1 CONHMe H H OMe H 98 2 CONHMe H H OMe H 99 3 CONHMe H H OMe H 100 4 CONHMe H H OMe H 101 1 SO.sub.2Me H H OMe H 102 2 SO.sub.2Me H H OMe H 103 3 SO.sub.2Me H H OMe H 104 4 SO.sub.2Me H H OMe H 105 1 SO.sub.2NH.sub.2 H H OMe H 106 2 SO.sub.2NH.sub.2 H H OMe H 107 3 SO.sub.2NH.sub.2 H H OMe H 108 4 SO.sub.2NH.sub.2 H H OMe H 109 1 H H H Me H 110 2 H H H Me H 111 3 H H H Me H 112 4 H H H Me H 113 1 Me H H Me H 114 2 Me H H Me H 115 3 Me H H Me H 116 4 Me H H Me H 117 1 CH.sub.2Ph H H Me H 118 2 CH.sub.2Ph H H Me H 119 3 CH.sub.2Ph H H Me H 120 4 CH.sub.2Ph H H Me H 121 1 COMe H H Me H 122 2 COMe H H Me H 123 3 COMe H H Me H 124 4 COMe H H Me H 125 1 CO.sub.2Me H H Me H 126 2 CO.sub.2Me H H Me H 127 3 CO.sub.2Me H H Me H 128 4 CO.sub.2Me H H Me H 129 1 CO.sub.2tBu H H Me H 130 2 CO.sub.2tBu H H Me H 131 3 CO.sub.2tBu H H Me H 132 4 CO.sub.2tBu H H Me H 133 1 CONHMe H H Me H 134 2 CONHMe H H Me H 135 3 CONHMe H H Me H 136 4 CONHMe H H Me H 137 1 SO.sub.2Me H H Me H 138 2 SO.sub.2Me H H Me H 139 3 SO.sub.2Me H H Me H 140 4 SO.sub.2Me H H Me H 141 1 SO.sub.2NH.sub.2 H H Me H 142 2 SO.sub.2NH.sub.2 H H Me H 143 3 SO.sub.2NH.sub.2 H H Me H 144 4 SO.sub.2NH.sub.2 H H Me H 145 1 H H H CF.sub.3 H 146 2 H H H CF.sub.3 H 147 3 H H H CF.sub.3 H 148 4 H H H CF.sub.3 H 149 1 Me H H CF.sub.3 H 150 2 Me H H CF.sub.3 H 151 3 Me H H CF.sub.3 H 152 4 Me H H CF.sub.3 H 153 1 CH.sub.2Ph H H CF.sub.3 H 154 2 CH.sub.2Ph H H CF.sub.3 H 155 3 CH.sub.2Ph H H CF.sub.3 H 156 4 CH.sub.2Ph H H CF.sub.3 H 157 1 COMe H H CF.sub.3 H 158 2 COMe H H CF.sub.3 H 159 3 COMe H H CF.sub.3 H 160 4 COMe H H CF.sub.3 H 161 1 CO.sub.2Me H H CF.sub.3 H 162 2 CO.sub.2Me H H CF.sub.3 H 163 3 CO.sub.2Me H H CF.sub.3 H 164 4 CO.sub.2Me H H CF.sub.3 H 165 1 CO.sub.2tBu H H CF.sub.3 H 166 2 CO.sub.2tBu H H CF.sub.3 H 167 3 CO.sub.2tBu H H CF.sub.3 H 168 4 CO.sub.2tBu H H CF.sub.3 H 169 1 CONHMe H H CF.sub.3 H 170 2 CONHMe H H CF.sub.3 H 171 3 CONHMe H H CF.sub.3 H 172 4 CONHMe H H CF.sub.3 H 173 1 SO.sub.2Me H H CF.sub.3 H 174 2 SO.sub.2Me H H CF.sub.3 H 175 3 SO.sub.2Me H H CF.sub.3 H 176 4 SO.sub.2Me H H CF.sub.3 H 177 1 SO.sub.2NH.sub.2 H H CF.sub.3 H 178 2 SO.sub.2NH.sub.2 H H CF.sub.3 H 179 3 SO.sub.2NH.sub.2 H H CF.sub.3 H 180 4 SO.sub.2NH.sub.2 H H CF.sub.3 H 181 1 H H H F H 182 2 H H H F H 183 3 H H H F H 184 4 H H H F H 185 1 Me H H F H 186 2 Me H H F H 187 3 Me H H F H 188 4 Me H H F H 189 1 CH.sub.2Ph H H F H 190 2 CH.sub.2Ph H H F H 191 3 CH.sub.2Ph H H F H 192 4 CH.sub.2Ph H H F H 193 1 COMe H H F H 194 2 COMe H H F H 195 3 COMe H H F H 196 4 COMe H H F H 197 1 CO.sub.2Me H H F H 198 2 CO.sub.2Me H H F H 199 3 CO.sub.2Me H H F H 200 4 CO.sub.2Me H H F H 201 1 CO.sub.2tBu H H F H 202 2 CO.sub.2tBu H H F H 203 3 CO.sub.2tBu H H F H 204 4 CO.sub.2tBu H H F H 205 1 CONHMe H H F H 206 2 CONHMe H H F H 207 3 CONHMe H H F H 208 4 CONHMe H H F H 209 1 SO.sub.2Me H H F H 210 2 SO.sub.2Me H H F H 211 3 SO.sub.2Me H H F H 212 4 SO.sub.2Me H H F H 213 1 SO.sub.2NH.sub.2 H H F H 214 2 SO.sub.2NH.sub.2 H H F H 215 3 SO.sub.2NH.sub.2 H H F H 216 4 SO.sub.2NH.sub.2 H H F H 217 1 H H H Cl H 218 2 H H H Cl H 219 3 H H H Cl H 220 4 H H H Cl H 221 1 Me H H Cl H 222 2 Me H H Cl H 223 3 Me H H Cl H 224 4 Me H H Cl H 225 1 CH.sub.2Ph H H Cl H 226 2 CH.sub.2Ph H H Cl H 227 3 CH.sub.2Ph H H Cl H 228 4 CH.sub.2Ph H H Cl H 229 1 COMe H H Cl H 230 2 COMe H H Cl H 231 3 COMe H H Cl H 232 4 COMe H H Cl H 233 1 CO.sub.2Me H H Cl H 234 2 CO.sub.2Me H H Cl H 235 3 CO.sub.2Me H H Cl H 236 4 CO.sub.2Me H H Cl H 237 1 CO.sub.2tBu H H Cl H 238 2 CO.sub.2tBu H H Cl H 239 3 CO.sub.2tBu H H Cl H 240 4 CO.sub.2tBu H H Cl H 241 1 CONHMe H H Cl H 242 2 CONHMe H H Cl H 243 3 CONHMe H H Cl H 244 4 CONHMe H H Cl H 245 1 SO.sub.2Me H H Cl H 246 2 SO.sub.2Me H H Cl H 247 3 SO.sub.2Me H H Cl H 248 4 SO.sub.2Me H H Cl H 249 1 SO.sub.2NH.sub.2 H H Cl H 250 2 SO.sub.2NH.sub.2 H H Cl H 251 3 SO.sub.2NH.sub.2 H H Cl H 252 4 SO.sub.2NH.sub.2 H H Cl H 253 1 H H H CN H 254 2 H H H CN H 255 3 H H H CN H 256 4 H H H CN H 257 1 Me H H CN H 258 2 Me H H CN H 259 3 Me H H CN H 260 4 Me H H CN H 261 1 CH.sub.2Ph H H CN H 262 2 CH.sub.2Ph H H CN H 263 3 CH.sub.2Ph H H CN H 264 4 CH.sub.2Ph H H CN H 265 1 COMe H H CN H 266 2 COMe H H CN H 267 3 COMe H H CN H 268 4 COMe H H CN H 269 1 CO.sub.2Me H H CN H 270 2 CO.sub.2Me H H CN H 271 3 CO.sub.2Me H H CN H 272 4 CO.sub.2Me H H CN H 273 1 CO.sub.2tBu H H CN H 274 2 CO.sub.2tBu H H CN H 275 3 CO.sub.2tBu H H CN H 276 4 CO.sub.2tBu H H CN H 277 1 CONHMe H H CN H 278 2 CONHMe H H CN H 279 3 CONHMe H H CN H 280 4 CONHMe H H CN H 281 1 SO.sub.2Me H H CN H 282 2 SO.sub.2Me H H CN H 283 3 SO.sub.2Me H H CN H 284 4 SO.sub.2Me H H CN H 285 1 SO.sub.2NH.sub.2 H H CN H 286 2 SO.sub.2NH.sub.2 H H CN H 287 3 SO.sub.2NH.sub.2 H H CN H 288 4 SO.sub.2NH.sub.2 H H CN H 289 1 H H H H OH 290 2 H H H H OH 291 3 H H H H OH 292 4 H H H H OH 293 1 Me H H H OH 294 2 Me H H H OH 295 3 Me H H H OH 296 4 Me H H H OH 297 1 CH.sub.2Ph H H H OH 298 2 CH.sub.2Ph H H H OH 299 3 CH.sub.2Ph H H H OH 300 4 CH.sub.2Ph H H H OH 301 1 COMe H H H OH 302 2 COMe H H H OH 303 3 COMe H H H OH 304 4 COMe H H H OH 305 1 CO.sub.2Me H H H OH 306 2 CO.sub.2Me H H H OH 307 3 CO.sub.2Me H H H OH 308 4 CO.sub.2Me H H H OH 309 1 CO.sub.2tBu H H H OH 310 2 CO.sub.2tBu H H H OH 311 3 CO.sub.2tBu H H H OH 312 4 CO.sub.2tBu H H H OH 313 1 CONHMe H H H OH 314 2 CONHMe H H H OH 315 3 CONHMe H H H OH 316 4 CONHMe H H H OH 317 1 SO.sub.2Me H H H OH 318 2 SO.sub.2Me H H H OH 319 3 SO.sub.2Me H H H OH 320 4 SO.sub.2Me H H H OH 321 1 SO.sub.2NH.sub.2 H H H OH 322 2 SO.sub.2NH.sub.2 H H H OH 323 3 SO.sub.2NH.sub.2 H H H OH 324 4 SO.sub.2NH.sub.2 H H H OH 325 1 H H H H OMe 326 2 H H H H OMe 327 3 H H H H OMe 328 4 H H H H OMe 329 1 Me H H H OMe 330 2 Me H H H OMe 331 3 Me H H H OMe 332 4 Me H H H OMe 333 1 CH.sub.2Ph H H H OMe 334 2 CH.sub.2Ph H H H OMe 335 3 CH.sub.2Ph H H H OMe 336 4 CH.sub.2Ph H H H OMe 337 1 COMe H H H OMe 338 2 COMe H H H OMe 339 3 COMe H H H OMe 340 4 COMe H H H OMe 341 1 CO.sub.2Me H H H OMe 342 2 CO.sub.2Me H H H OMe 343 3 CO.sub.2Me H H H OMe 344 4 CO.sub.2Me H H H OMe 345 1 CO.sub.2tBu H H H OMe 346 2 CO.sub.2tBu H H H OMe 347 3 CO.sub.2tBu H H H OMe 348 4 CO.sub.2tBu H H H OMe 349 1 CONHMe H H H OMe 350 2 CONHMe H H H OMe 351 3 CONHMe H H H OMe 352 4 CONHMe H H H OMe 353 1 SO.sub.2Me H H H OMe 354 2 SO.sub.2Me H H H OMe 355 3 SO.sub.2Me H H H OMe 356 4 SO.sub.2Me H H H OMe 357 1 SO.sub.2NH.sub.2 H H H OMe 358 2 SO.sub.2NH.sub.2 H H H OMe 359 3 SO.sub.2NH.sub.2 H H H OMe 360 4 SO.sub.2NH.sub.2 H H H OMe 361 1 H H H H Me 362 2 H H H H Me 363 3 H H H H Me 364 4 H H H H Me 365 1 Me H H H Me 366 2 Me H H H Me 367 3 Me H H H Me 368 4 Me H H H Me 369 1 CH.sub.2Ph H H H Me 370 2 CH.sub.2Ph H H H Me 371 3 CH.sub.2Ph H H H Me 372 4 CH.sub.2Ph H H H Me 373 1 COMe H H H Me 374 2 COMe H H H Me 375 3 COMe H H H Me 376 4 COMe H H H Me 377 1 CO.sub.2Me H H H Me 378 2 CO.sub.2Me H H H Me 379 3 CO.sub.2Me H H H Me 380 4 CO.sub.2Me H H H Me 381 1 CO.sub.2tBu H H H Me 382 2 CO.sub.2tBu H H H Me 383 3 CO.sub.2tBu H H H Me 384 4 CO.sub.2tBu H H H Me 385 1 CONHMe H H H Me 386 2 CONHMe H H H Me 387 3 CONHMe H H H Me 388 4 CONHMe H H H Me 389 1 SO.sub.2Me H H H Me 390 2 SO.sub.2Me H H H Me 391 3 SO.sub.2Me H H H Me 392 4 SO.sub.2Me H H H Me 393 1 SO.sub.2NH.sub.2 H H H Me 394 2 SO.sub.2NH.sub.2 H H H Me 395 3 SO.sub.2NH.sub.2 H H H Me 396 4 SO.sub.2NH.sub.2 H H H Me 397 1 H H H H CF.sub.3 398 2 H H H H CF.sub.3 399 3 H H H H CF.sub.3 400 4 H H H H CF.sub.3 401 1 Me H H H CF.sub.3 402 2 Me H H H CF.sub.3 403 3 Me H H H CF.sub.3 404 4 Me H H H CF.sub.3 405 1 CH.sub.2Ph H H H CF.sub.3 406 2 CH.sub.2Ph H H H CF.sub.3 407 3 CH.sub.2Ph H H H CF.sub.3 408 4 CH.sub.2Ph H H H CF.sub.3 409 1 COMe H H H CF.sub.3 410 2 COMe H H H CF.sub.3 411 3 COMe H H H CF.sub.3 412 4 COMe H H H CF.sub.3 413 1 CO.sub.2Me H H H CF.sub.3 414 2 CO.sub.2Me H H H CF.sub.3 415 3 CO.sub.2Me H H H CF.sub.3 416 4 CO.sub.2Me H H H CF.sub.3 417 1 CO.sub.2tBu H H H CF.sub.3 418 2 CO.sub.2tBu H H H CF.sub.3 419 3 CO.sub.2tBu H H H CF.sub.3 420 4 CO.sub.2tBu H H H CF.sub.3 421 1 CONHMe H H H CF.sub.3 422 2 CONHMe H H H CF.sub.3 423 3 CONHMe H H H CF.sub.3 424 4 CONHMe H H H CF.sub.3 425 1 SO.sub.2Me H H H CF.sub.3 426 2 SO.sub.2Me H H H CF.sub.3 427 3 SO.sub.2Me H H H CF.sub.3 428 4 SO.sub.2Me H H H CF.sub.3 429 1 SO.sub.2NH.sub.2 H H H CF.sub.3 430 2 SO.sub.2NH.sub.2 H H H CF.sub.3 431 3 SO.sub.2NH.sub.2 H H H CF.sub.3 432 4 SO.sub.2NH.sub.2 H H H CF.sub.3 433 1 H H H H F 434 2 H H H H F 435 3 H H H H F 436 3 H H H H F 437 1 Me H H H F 438 2 Me H H H F 439 3 Me H H H F 440 4 Me H H H F 441 1 CH.sub.2Ph H H H F 442 2 CH.sub.2Ph H H H F 443 3 CH.sub.2Ph H H H F 444 4 CH.sub.2Ph H H H F 445 1 COMe H H H F 446 2 COMe H H H F 447 3 COMe H H H F 448 4 COMe H H H F 449 1 CO.sub.2Me H H H F 450 2 CO.sub.2Me H H H F 451 3 CO.sub.2Me H H H F 452 4 CO.sub.2Me H H H F 453 1 CO.sub.2tBu H H H F 454 2 CO.sub.2tBu H H H F 455 3 CO.sub.2tBu H H H F 456 4 CO.sub.2tBu H H H F 457 1 CONHMe H H H F 458 2 CONHMe H H H F 459 3 CONHMe H H H F 460 4 CONHMe H H H F 461 1 SO.sub.2Me H H H F 462 2 SO.sub.2Me H H H F 463 3 SO.sub.2Me H H H F 464 4 SO.sub.2Me H H H F 465 1 SO.sub.2NH.sub.2 H H H F 466 2 SO.sub.2NH.sub.2 H H H F 467 3 SO.sub.2NH.sub.2 H H H F 468 4 SO.sub.2NH.sub.2 H H H F 469 1 H H H H Cl 470 2 H H H H Cl 471 3 H H H H Cl 472 4 H H H H Cl 473 1 Me H H H Cl 474 2 Me H H H Cl 475 3 Me H H H Cl 476 4 Me H H H Cl 477 1 CH.sub.2Ph H H H Cl 478 2 CH.sub.2Ph H H H Cl 479 3 CH.sub.2Ph H H H Cl 480 4 CH.sub.2Ph H H H Cl 481 1 COMe H H H Cl 482 2 COMe H H H Cl 483 3 COMe H H H Cl 484 4 COMe H H H Cl 485 1 CO.sub.2Me H H H Cl 486 2 CO.sub.2Me H H H Cl 487 3 CO.sub.2Me H H H Cl 488 4 CO.sub.2Me H H H Cl 489 1 CO.sub.2tBu H H H Cl 490 2 CO.sub.2tBu H H H Cl 491 3 CO.sub.2tBu H H H Cl 492 4 CO.sub.2tBu H H H Cl 493 1 CONHMe H H H Cl 494 2 CONHMe H H H Cl 495 3 CONHMe H H H Cl 496 4 CONHMe H H H Cl 497 1 SO.sub.2Me H H H Cl 498 2 SO.sub.2Me H H H Cl 499 3 SO.sub.2Me H H H Cl 500 4 SO.sub.2Me H H H Cl 501 1 SO.sub.2NH.sub.2 H H H Cl 502 2 SO.sub.2NH.sub.2 H H H Cl 503 3 SO.sub.2NH.sub.2 H H H Cl 504 4 SO.sub.2NH.sub.2 H H H Cl 505 1 H H H H CN 506 2 H H H H CN 507 3 H H H H CN 508 4 H H H H CN 509 1 Me H H H CN 510 2 Me H H H CN 511 3 Me H H H CN 512 4 Me H H H CN 513 1 CH.sub.2Ph H H H CN 514 2 CH.sub.2Ph H H H CN 515 3 CH.sub.2Ph H H H CN 516 4 CH.sub.2Ph H H H CN 517 1 COMe H H H CN 518 2 COMe H H H CN 519 3 COMe H H H CN 520 4 COMe H H H CN 521 1 CO.sub.2Me H H H CN 522 2 CO.sub.2Me H H H CN 523 3 CO.sub.2Me H H H CN 524 4 CO.sub.2Me H H H CN 525 1 CO.sub.2tBu H H H CN 526 2 CO.sub.2tBu H H H CN 527 3 CO.sub.2tBu H H H CN 528 4 CO.sub.2tBu H H H CN 529 1 CONHMe H H H CN 530 2 CONHMe H H H CN 531 3 CONHMe H H H CN 532 4 CONHMe H H H CN 533 1 SO.sub.2Me H H H CN 534 2 SO.sub.2Me H H H CN 535 3 SO.sub.2Me H H H CN 536 4 SO.sub.2Me H H H CN 537 1 SO.sub.2NH.sub.2 H H H CN 538 2 SO.sub.2NH.sub.2 H H H CN 539 3 SO.sub.2NH.sub.2 H H H CN 540 4 SO.sub.2NH.sub.2 H H H CN

    [2044] Exemplary embodiments include compounds having the formula (XXXII)

    ##STR00447##

    [2045] or a pharmaceutically acceptable salt form thereof defined herein below in Table 26.

    TABLE-US-00026 TABLE26 Entry n R.sup.7 R.sup.20a R.sup.20b R.sup.20d R.sup.20e 1 1 H H H H H 2 2 H H H H H 3 3 H H H H H 4 4 H H H H H 5 1 Me H H H H 6 2 Me H H H H 7 3 Me H H H H 8 4 Me H H H H 9 1 CH.sub.2Ph H H H H 10 2 CH.sub.2Ph H H H H 11 3 CH.sub.2Ph H H H H 12 4 CH.sub.2Ph H H H H 13 1 COMe H H H H 14 2 COMe H H H H 15 3 COMe H H H H 16 4 COMe H H H H 17 1 CO.sub.2Me H H H H 18 2 CO.sub.2Me H H H H 19 3 CO.sub.2Me H H H H 20 4 CO.sub.2Me H H H H 21 1 CO.sub.2tBu H H H H 22 2 CO.sub.2tBu H H H H 23 3 CO.sub.2tBu H H H H 24 4 CO.sub.2tBu H H H H 25 1 CONHMe H H H H 26 2 CONHMe H H H H 27 3 CONHMe H H H H 28 4 CONHMe H H H H 29 1 SO.sub.2Me H H H H 30 2 SO.sub.2Me H H H H 31 3 SO.sub.2Me H H H H 32 4 SO.sub.2Me H H H H 33 1 SO.sub.2NH.sub.2 H H H H 34 2 SO.sub.2NH.sub.2 H H H H 35 3 SO.sub.2NH.sub.2 H H H H 36 4 SO.sub.2NH.sub.2 H H H H 37 1 H H H OH H 38 2 H H H OH H 39 3 H H H OH H 40 4 H H H OH H 41 1 Me H H OH H 42 2 Me H H OH H 43 3 Me H H OH H 44 4 Me H H OH H 45 1 CH.sub.2Ph H H OH H 46 2 CH.sub.2Ph H H OH H 47 3 CH.sub.2Ph H H OH H 48 4 CH.sub.2Ph H H OH H 49 1 COMe H H OH H 50 2 COMe H H OH H 51 3 COMe H H OH H 52 4 COMe H H OH H 53 1 CO.sub.2Me H H OH H 54 2 CO.sub.2Me H H OH H 55 3 CO.sub.2Me H H OH H 56 4 CO.sub.2Me H H OH H 57 1 CO.sub.2tBu H H OH H 58 2 CO.sub.2tBu H H OH H 59 3 CO.sub.2tBu H H OH H 60 4 CO.sub.2tBu H H OH H 61 1 CONHMe H H OH H 62 2 CONHMe H H OH H 63 3 CONHMe H H OH H 64 4 CONHMe H H OH H 65 1 SO.sub.2Me H H OH H 66 2 SO.sub.2Me H H OH H 67 3 SO.sub.2Me H H OH H 68 4 SO.sub.2Me H H OH H 69 1 SO.sub.2NH.sub.2 H H OH H 70 2 SO.sub.2NH.sub.2 H H OH H 71 3 SO.sub.2NH.sub.2 H H OH H 72 4 SO.sub.2NH.sub.2 H H OH H 73 1 H H H OMe H 74 2 H H H OMe H 75 3 H H H OMe H 76 4 H H H OMe H 77 1 Me H H OMe H 78 2 Me H H OMe H 79 3 Me H H OMe H 80 4 Me H H OMe H 81 1 CH.sub.2Ph H H OMe H 82 2 CH.sub.2Ph H H OMe H 83 3 CH.sub.2Ph H H OMe H 84 4 CH.sub.2Ph H H OMe H 85 1 COMe H H OMe H 86 2 COMe H H OMe H 87 3 COMe H H OMe H 88 4 COMe H H OMe H 89 1 CO.sub.2Me H H OMe H 90 2 CO.sub.2Me H H OMe H 91 3 CO.sub.2Me H H OMe H 92 4 CO.sub.2Me H H OMe H 93 1 CO.sub.2tBu H H OMe H 94 2 CO.sub.2tBu H H OMe H 95 3 CO.sub.2tBu H H OMe H 96 1 CO.sub.2tBu H H OMe H 97 1 CONHMe H H OMe H 98 2 CONHMe H H OMe H 99 3 CONHMe H H OMe H 100 4 CONHMe H H OMe H 101 1 SO.sub.2Me H H OMe H 102 2 SO.sub.2Me H H OMe H 103 3 SO.sub.2Me H H OMe H 104 4 SO.sub.2Me H H OMe H 105 1 SO.sub.2NH.sub.2 H H OMe H 106 2 SO.sub.2NH.sub.2 H H OMe H 107 3 SO.sub.2NH.sub.2 H H OMe H 108 4 SO.sub.2NH.sub.2 H H OMe H 109 1 H H H Me H 110 2 H H H Me H 111 3 H H H Me H 112 4 H H H Me H 113 1 Me H H Me H 114 2 Me H H Me H 115 3 Me H H Me H 116 4 Me H H Me H 117 1 CH.sub.2Ph H H Me H 118 2 CH.sub.2Ph H H Me H 119 3 CH.sub.2Ph H H Me H 120 4 CH.sub.2Ph H H Me H 121 1 COMe H H Me H 122 2 COMe H H Me H 123 3 COMe H H Me H 124 4 COMe H H Me H 125 1 CO.sub.2Me H H Me H 126 2 CO.sub.2Me H H Me H 127 3 CO.sub.2Me H H Me H 128 4 CO.sub.2Me H H Me H 129 1 CO.sub.2tBu H H Me H 130 2 CO.sub.2tBu H H Me H 131 3 CO.sub.2tBu H H Me H 132 4 CO.sub.2tBu H H Me H 133 1 CONHMe H H Me H 134 2 CONHMe H H Me H 135 3 CONHMe H H Me H 136 4 CONHMe H H Me H 137 1 SO.sub.2Me H H Me H 138 2 SO.sub.2Me H H Me H 139 3 SO.sub.2Me H H Me H 140 4 SO.sub.2Me H H Me H 141 1 SO.sub.2NH.sub.2 H H Me H 142 2 SO.sub.2NH.sub.2 H H Me H 143 3 SO.sub.2NH.sub.2 H H Me H 144 4 SO.sub.2NH.sub.2 H H Me H 145 1 H H H CF.sub.3 H 146 2 H H H CF.sub.3 H 147 3 H H H CF.sub.3 H 148 4 H H H CF.sub.3 H 149 1 Me H H CF.sub.3 H 150 2 Me H H CF.sub.3 H 151 3 Me H H CF.sub.3 H 152 4 Me H H CF.sub.3 H 153 1 CH.sub.2Ph H H CF.sub.3 H 154 2 CH.sub.2Ph H H CF.sub.3 H 155 3 CH.sub.2Ph H H CF.sub.3 H 156 4 CH.sub.2Ph H H CF.sub.3 H 157 1 COMe H H CF.sub.3 H 158 2 COMe H H CF.sub.3 H 159 3 COMe H H CF.sub.3 H 160 4 COMe H H CF.sub.3 H 161 1 CO.sub.2Me H H CF.sub.3 H 162 2 CO.sub.2Me H H CF.sub.3 H 163 3 CO.sub.2Me H H CF.sub.3 H 164 4 CO.sub.2Me H H CF.sub.3 H 165 1 CO.sub.2tBu H H CF.sub.3 H 166 2 CO.sub.2tBu H H CF.sub.3 H 167 3 CO.sub.2tBu H H CF.sub.3 H 168 4 CO.sub.2tBu H H CF.sub.3 H 169 1 CONHMe H H CF.sub.3 H 170 2 CONHMe H H CF.sub.3 H 171 3 CONHMe H H CF.sub.3 H 172 4 CONHMe H H CF.sub.3 H 173 1 SO.sub.2Me H H CF.sub.3 H 174 2 SO.sub.2Me H H CF.sub.3 H 175 3 SO.sub.2Me H H CF.sub.3 H 176 4 SO.sub.2Me H H CF.sub.3 H 177 1 SO.sub.2NH.sub.2 H H CF.sub.3 H 178 2 SO.sub.2NH.sub.2 H H CF.sub.3 H 179 3 SO.sub.2NH.sub.2 H H CF.sub.3 H 180 4 SO.sub.2NH.sub.2 H H CF.sub.3 H 181 1 H H H F H 182 2 H H H F H 183 3 H H H F H 184 4 H H H F H 185 1 Me H H F H 186 2 Me H H F H 187 3 Me H H F H 188 4 Me H H F H 189 1 CH.sub.2Ph H H F H 190 2 CH.sub.2Ph H H F H 191 3 CH.sub.2Ph H H F H 192 4 CH.sub.2Ph H H F H 193 1 COMe H H F H 194 2 COMe H H F H 195 3 COMe H H F H 196 4 COMe H H F H 197 1 CO.sub.2Me H H F H 198 2 CO.sub.2Me H H F H 199 3 CO.sub.2Me H H F H 200 4 CO.sub.2Me H H F H 201 1 CO.sub.2tBu H H F H 202 2 CO.sub.2tBu H H F H 203 3 CO2tBu H H F H 204 4 CO.sub.2tBu H H F H 205 1 CONHMe H H F H 206 2 CONHMe H H F H 207 3 CONHMe H H F H 208 4 CONHMe H H F H 209 1 SO.sub.2Me H H F H 210 2 SO.sub.2Me H H F H 211 3 SO.sub.2Me H H F H 212 4 SO.sub.2Me H H F H 213 1 SO.sub.2NH.sub.2 H H F H 214 2 SO.sub.2NH.sub.2 H H F H 215 3 SO.sub.2NH.sub.2 H H F H 216 4 SO.sub.2NH.sub.2 H H F H 217 1 H H H Cl H 218 2 H H H Cl H 219 3 H H H Cl H 220 4 H H H Cl H 221 1 Me H H Cl H 222 2 Me H H Cl H 223 3 Me H H Cl H 224 4 Me H H Cl H 225 1 CH.sub.2Ph H H Cl H 226 2 CH.sub.2Ph H H Cl H 227 3 CH.sub.2Ph H H Cl H 228 4 CH.sub.2Ph H H Cl H 229 1 COMe H H Cl H 230 2 COMe H H Cl H 231 3 COMe H H Cl H 232 4 COMe H H Cl H 233 1 CO.sub.2Me H H Cl H 234 2 CO.sub.2Me H H Cl H 235 3 CO.sub.2Me H H Cl H 236 4 CO.sub.2Me H H Cl H 237 1 CO.sub.2tBu H H Cl H 238 2 CO.sub.2tBu H H Cl H 239 3 CO.sub.2tBu H H Cl H 240 4 CO.sub.2tBu H H Cl H 241 1 CONHMe H H Cl H 242 2 CONHMe H H Cl H 243 3 CONHMe H H Cl H 244 4 CONHMe H H Cl H 245 1 SO.sub.2Me H H Cl H 246 2 SO.sub.2Me H H Cl H 247 3 SO.sub.2Me H H Cl H 248 4 SO.sub.2Me H H Cl H 249 1 SO.sub.2NH.sub.2 H H Cl H 250 2 SO.sub.2NH.sub.2 H H Cl H 251 3 SO.sub.2NH.sub.2 H H Cl H 252 4 SO.sub.2NH.sub.2 H H Cl H 253 1 H H H CN H 254 2 H H H CN H 255 3 H H H CN H 256 4 H H H CN H 257 1 Me H H CN H 258 2 Me H H CN H 259 3 Me H H CN H 260 4 Me H H CN H 261 1 CH.sub.2Ph H H CN H 262 2 CH.sub.2Ph H H CN H 263 3 CH.sub.2Ph H H CN H 264 4 CH.sub.2Ph H H CN H 265 1 COMe H H CN H 266 2 COMe H H CN H 267 3 COMe H H CN H 268 4 COMe H H CN H 269 1 CO.sub.2Me H H CN H 270 2 CO.sub.2Me H H CN H 271 3 CO.sub.2Me H H CN H 272 4 CO.sub.2Me H H CN H 273 1 CO.sub.2tBu H H CN H 274 2 CO.sub.2tBu H H CN H 275 3 CO.sub.2tBu H H CN H 276 4 CO.sub.2tBu H H CN H 277 1 CONHMe H H CN H 278 2 CONHMe H H CN H 279 3 CONHMe H H CN H 280 4 CONHMe H H CN H 281 1 SO.sub.2Me H H CN H 282 2 SO.sub.2Me H H CN H 283 3 SO.sub.2Me H H CN H 284 4 SO.sub.2Me H H CN H 285 1 SO.sub.2NH.sub.2 H H CN H 286 2 SO.sub.2NH.sub.2 H H CN H 287 3 SO.sub.2NH.sub.2 H H CN H 288 4 SO.sub.2NH.sub.2 H H CN H 289 1 H H H H OH 290 2 H H H H OH 291 3 H H H H OH 292 4 H H H H OH 293 1 Me H H H OH 294 2 Me H H H OH 295 3 Me H H H OH 296 4 Me H H H OH 297 1 CH.sub.2Ph H H H OH 298 2 CH.sub.2Ph H H H OH 299 3 CH.sub.2Ph H H H OH 300 4 CH.sub.2Ph H H H OH 301 1 COMe H H H OH 302 2 COMe H H H OH 303 3 COMe H H H OH 304 4 COMe H H H OH 305 1 CO.sub.2Me H H H OH 306 2 CO.sub.2Me H H H OH 307 3 CO.sub.2Me H H H OH 308 4 CO.sub.2Me H H H OH 309 1 CO.sub.2tBu H H H OH 310 2 CO.sub.2tBu H H H OH 311 3 CO.sub.2tBu H H H OH 312 4 CO.sub.2tBu H H H OH 313 1 CONHMe H H H OH 314 2 CONHMe H H H OH 315 3 CONHMe H H H OH 316 4 CONHMe H H H OH 317 1 SO.sub.2Me H H H OH 318 2 SO.sub.2Me H H H OH 319 3 SO.sub.2Me H H H OH 320 4 SO.sub.2Me H H H OH 321 1 SO.sub.2NH.sub.2 H H H OH 322 2 SO.sub.2NH.sub.2 H H H OH 323 3 SO.sub.2NH.sub.2 H H H OH 324 4 SO.sub.2NH.sub.2 H H H OH 325 1 H H H H OMe 326 2 H H H H OMe 327 3 H H H H OMe 328 4 H H H H OMe 329 1 Me H H H OMe 330 2 Me H H H OMe 331 3 Me H H H OMe 332 4 Me H H H OMe 333 1 CH.sub.2Ph H H H OMe 334 2 CH.sub.2Ph H H H OMe 335 3 CH.sub.2Ph H H H OMe 336 4 CH.sub.2Ph H H H OMe 337 1 COMe H H H OMe 338 2 COMe H H H OMe 339 3 COMe H H H OMe 340 4 COMe H H H OMe 341 1 CO.sub.2Me H H H OMe 342 2 CO.sub.2Me H H H OMe 343 3 CO.sub.2Me H H H OMe 344 4 CO.sub.2Me H H H OMe 345 1 CO.sub.2tBu H H H OMe 346 2 CO.sub.2tBu H H H OMe 347 3 CO.sub.2tBu H H H OMe 348 4 CO.sub.2tBu H H H OMe 349 1 CONHMe H H H OMe 350 2 CONHMe H H H OMe 351 3 CONHMe H H H OMe 352 4 CONHMe H H H OMe 353 1 SO.sub.2Me H H H OMe 354 2 SO.sub.2Me H H H OMe 355 3 SO.sub.2Me H H H OMe 356 4 SO.sub.2Me H H H OMe 357 1 SO.sub.2NH.sub.2 H H H OMe 358 2 SO.sub.2NH.sub.2 H H H OMe 359 3 SO.sub.2NH.sub.2 H H H OMe 360 4 SO.sub.2NH.sub.2 H H H OMe 361 1 H H H H Me 362 2 H H H H Me 363 3 H H H H Me 364 4 H H H H Me 365 1 Me H H H Me 366 2 Me H H H Me 367 3 Me H H H Me 368 4 Me H H H Me 369 1 CH.sub.2Ph H H H Me 370 2 CH.sub.2Ph H H H Me 371 3 CH.sub.2Ph H H H Me 372 4 CH.sub.2Ph H H H Me 373 1 COMe H H H Me 374 2 COMe H H H Me 375 3 COMe H H H Me 376 4 COMe H H H Me 377 1 CO.sub.2Me H H H Me 378 2 CO.sub.2Me H H H Me 379 3 CO.sub.2Me H H H Me 380 4 CO.sub.2Me H H H Me 381 1 CO.sub.2tBu H H H Me 382 2 CO.sub.2tBu H H H Me 383 3 CO.sub.2tBu H H H Me 384 4 CO.sub.2tBu H H H Me 385 1 CONHMe H H H Me 386 2 CONHMe H H H Me 387 3 CONHMe H H H Me 388 4 CONHMe H H H Me 389 1 SO.sub.2Me H H H Me 390 2 SO.sub.2Me H H H Me 391 3 SO.sub.2Me H H H Me 392 4 SO.sub.2Me H H H Me 393 1 SO.sub.2NH.sub.2 H H H Me 394 2 SO.sub.2NH.sub.2 H H H Me 395 3 SO.sub.2NH.sub.2 H H H Me 396 4 SO.sub.2NH.sub.2 H H H Me 397 1 H H H H CF.sub.3 398 2 H H H H CF.sub.3 399 3 H H H H CF.sub.3 400 4 H H H H CF.sub.3 401 1 Me H H H CF.sub.3 402 2 Me H H H CF.sub.3 403 3 Me H H H CF.sub.3 404 4 Me H H H CF.sub.3 405 1 CH.sub.2Ph H H H CF.sub.3 406 2 CH.sub.2Ph H H H CF.sub.3 407 3 CH.sub.2Ph H H H CF.sub.3 408 4 CH.sub.2Ph H H H CF.sub.3 409 1 COMe H H H CF.sub.3 410 2 COMe H H H CF.sub.3 411 3 COMe H H H CF.sub.3 412 4 COMe H H H CF.sub.3 413 1 CO.sub.2Me H H H CF.sub.3 414 2 CO.sub.2Me H H H CF.sub.3 415 3 CO.sub.2Me H H H CF.sub.3 416 4 CO.sub.2Me H H H CF.sub.3 417 1 CO.sub.2tBu H H H CF.sub.3 418 2 CO.sub.2tBu H H H CF.sub.3 419 3 CO.sub.2tBu H H H CF.sub.3 420 4 CO.sub.2tBu H H H CF.sub.3 421 1 CONHMe H H H CF.sub.3 422 2 CONHMe H H H CF.sub.3 423 3 CONHMe H H H CF.sub.3 424 4 CONHMe H H H CF.sub.3 425 1 SO.sub.2Me H H H CF.sub.3 426 2 SO.sub.2Me H H H CF.sub.3 427 3 SO.sub.2Me H H H CF.sub.3 428 4 SO.sub.2Me H H H CF.sub.3 429 1 SO.sub.2NH.sub.2 H H H CF.sub.3 430 2 SO.sub.2NH.sub.2 H H H CF.sub.3 431 3 SO.sub.2NH.sub.2 H H H CF.sub.3 432 4 SO.sub.2NH.sub.2 H H H CF.sub.3 433 1 H H H H F 434 2 H H H H F 435 3 H H H H F 436 3 H H H H F 437 1 Me H H H F 438 2 Me H H H F 439 3 Me H H H F 440 4 Me H H H F 441 1 CH.sub.2Ph H H H F 442 2 CH.sub.2Ph H H H F 443 3 CH.sub.2Ph H H H F 444 4 CH.sub.2Ph H H H F 445 1 COMe H H H F 446 2 COMe H H H F 447 3 COMe H H H F 448 4 COMe H H H F 449 1 CO.sub.2Me H H H F 450 2 CO.sub.2Me H H H F 451 3 CO.sub.2Me H H H F 452 4 CO.sub.2Me H H H F 453 1 CO.sub.2tBu H H H F 454 2 CO.sub.2tBu H H H F 455 3 CO.sub.2tBu H H H F 456 4 CO.sub.2tBu H H H F 457 1 CONHMe H H H F 458 2 CONHMe H H H F 459 3 CONHMe H H H F 460 4 CONHMe H H H F 461 1 SO.sub.2Me H H H F 462 2 SO.sub.2Me H H H F 463 3 SO.sub.2Me H H H F 464 4 SO.sub.2Me H H H F 465 1 SO.sub.2NH.sub.2 H H H F 466 2 SO.sub.2NH.sub.2 H H H F 467 3 SO.sub.2NH.sub.2 H H H F 468 4 SO.sub.2NH.sub.2 H H H F 469 1 H H H H Cl 470 2 H H H H Cl 471 3 H H H H Cl 472 4 H H H H Cl 473 1 Me H H H Cl 474 2 Me H H H Cl 475 3 Me H H H Cl 476 4 Me H H H Cl 477 1 CH.sub.2Ph H H H Cl 478 2 CH.sub.2Ph H H H Cl 479 3 CH.sub.2Ph H H H Cl 480 4 CH.sub.2Ph H H H Cl 481 1 COMe H H H Cl 482 2 COMe H H H Cl 483 3 COMe H H H Cl 484 4 COMe H H H Cl 485 1 CO.sub.2Me H H H Cl 486 2 CO.sub.2Me H H H Cl 487 3 CO.sub.2Me H H H Cl 488 4 CO.sub.2Me H H H Cl 489 1 CO.sub.2tBu H H H Cl 490 2 CO.sub.2tBu H H H Cl 491 3 CO.sub.2tBu H H H Cl 492 4 CO.sub.2tBu H H H Cl 493 1 CONHMe H H H Cl 494 2 CONHMe H H H Cl 495 3 CONHMe H H H Cl 496 4 CONHMe H H H Cl 497 1 SO.sub.2Me H H H Cl 498 2 SO.sub.2Me H H H Cl 499 3 SO.sub.2Me H H H Cl 500 4 SO.sub.2Me H H H Cl 501 1 SO.sub.2NH.sub.2 H H H Cl 502 2 SO.sub.2NH.sub.2 H H H Cl 503 3 SO.sub.2NH.sub.2 H H H Cl 504 4 SO.sub.2NH.sub.2 H H H Cl 505 1 H H H H CN 506 2 H H H H CN 507 3 H H H H CN 508 4 H H H H CN 509 1 Me H H H CN 510 2 Me H H H CN 511 3 Me H H H CN 512 4 Me H H H CN 513 1 CH.sub.2Ph H H H CN 514 2 CH.sub.2Ph H H H CN 515 3 CH.sub.2Ph H H H CN 516 4 CH.sub.2Ph H H H CN 517 1 COMe H H H CN 518 2 COMe H H H CN 519 3 COMe H H H CN 520 4 COMe H H H CN 521 1 CO.sub.2Me H H H CN 522 2 CO.sub.2Me H H H CN 523 3 CO.sub.2Me H H H CN 524 4 CO.sub.2Me H H H CN 525 1 CO.sub.2tBu H H H CN 526 2 CO.sub.2tBu H H H CN 527 3 CO.sub.2tBu H H H CN 528 4 CO.sub.2tBu H H H CN 529 1 CONHMe H H H CN 530 2 CONHMe H H H CN 531 3 CONHMe H H H CN 532 4 CONHMe H H H CN 533 1 SO.sub.2Me H H H CN 534 2 SO.sub.2Me H H H CN 535 3 SO.sub.2Me H H H CN 536 4 SO.sub.2Me H H H CN 537 1 SO.sub.2NH.sub.2 H H H CN 538 2 SO.sub.2NH.sub.2 H H H CN 539 3 SO.sub.2NH.sub.2 H H H CN 540 4 SO.sub.2NH.sub.2 H H H CN

    [2046] Exemplary embodiments include compounds having the formula (XXXIV)

    ##STR00448##

    [2047] or a pharmaceutically acceptable salt form thereof defined herein below in Table 27.

    TABLE-US-00027 TABLE27 Entry n R.sup.7 R.sup.20a R.sup.20b R.sup.20d R.sup.20e 1 1 H H H H H 2 2 H H H H H 3 3 H H H H H 4 4 H H H H H 5 1 Me H H H H 6 2 Me H H H H 7 3 Me H H H H 8 4 Me H H H H 9 1 CH.sub.2Ph H H H H 10 2 CH.sub.2Ph H H H H 11 3 CH.sub.2Ph H H H H 12 4 CH.sub.2Ph H H H H 13 1 COMe H H H H 14 2 COMe H H H H 15 3 COMe H H H H 16 4 COMe H H H H 17 1 CO.sub.2Me H H H H 18 2 CO.sub.2Me H H H H 19 3 CO.sub.2Me H H H H 20 4 CO.sub.2Me H H H H 21 1 CO.sub.2tBu H H H H 22 2 CO.sub.2tBu H H H H 23 3 CO.sub.2tBu H H H H 24 4 CO.sub.2tBu H H H H 25 1 CONHMe H H H H 26 2 CONHMe H H H H 27 3 CONHMe H H H H 28 4 CONHMe H H H H 29 1 SO.sub.2Me H H H H 30 2 SO.sub.2Me H H H H 31 3 SO.sub.2Me H H H H 32 4 SO.sub.2Me H H H H 33 1 SO.sub.2NH.sub.2 H H H H 34 2 SO.sub.2NH.sub.2 H H H H 35 3 SO.sub.2NH.sub.2 H H H H 36 4 SO.sub.2NH.sub.2 H H H H 37 1 H H H OH H 38 2 H H H OH H 39 3 H H H OH H 40 4 H H H OH H 41 1 Me H H OH H 42 2 Me H H OH H 43 3 Me H H OH H 44 4 Me H H OH H 45 1 CH.sub.2Ph H H OH H 46 2 CH.sub.2Ph H H OH H 47 3 CH.sub.2Ph H H OH H 48 4 CH.sub.2Ph H H OH H 49 1 COMe H H OH H 50 2 COMe H H OH H 51 3 COMe H H OH H 52 4 COMe H H OH H 53 1 CO.sub.2Me H H OH H 54 2 CO.sub.2Me H H OH H 55 3 CO.sub.2Me H H OH H 56 4 CO.sub.2Me H H OH H 57 1 CO.sub.2tBu H H OH H 58 2 CO.sub.2tBu H H OH H 59 3 CO.sub.2tBu H H OH H 60 4 CO.sub.2tBu H H OH H 61 1 CONHMe H H OH H 62 2 CONHMe H H OH H 63 3 CONHMe H H OH H 64 4 CONHMe H H OH H 65 1 SO.sub.2Me H H OH H 66 2 SO.sub.2Me H H OH H 67 3 SO.sub.2Me H H OH H 68 4 SO.sub.2Me H H OH H 69 1 SO.sub.2NH.sub.2 H H OH H 70 2 SO.sub.2NH.sub.2 H H OH H 71 3 SO.sub.2NH.sub.2 H H OH H 72 4 SO.sub.2NH.sub.2 H H OH H 73 1 H H H OMe H 74 2 H H H OMe H 75 3 H H H OMe H 76 4 H H H OMe H 77 1 Me H H OMe H 78 2 Me H H OMe H 79 3 Me H H OMe H 80 4 Me H H OMe H 81 1 CH.sub.2Ph H H OMe H 82 2 CH.sub.2Ph H H OMe H 83 3 CH.sub.2Ph H H OMe H 84 4 CH.sub.2Ph H H OMe H 85 1 COMe H H OMe H 86 2 COMe H H OMe H 87 3 COMe H H OMe H 88 4 COMe H H OMe H 89 1 CO.sub.2Me H H OMe H 90 2 CO.sub.2Me H H OMe H 91 3 CO.sub.2Me H H OMe H 92 4 CO.sub.2Me H H OMe H 93 1 CO.sub.2tBu H H OMe H 94 2 CO.sub.2tBu H H OMe H 95 3 CO.sub.2tBu H H OMe H 96 1 CO.sub.2tBu H H OMe H 97 1 CONHMe H H OMe H 98 2 CONHMe H H OMe H 99 3 CONHMe H H OMe H 100 4 CONHMe H H OMe H 101 1 SO.sub.2Me H H OMe H 102 2 SO.sub.2Me H H OMe H 103 3 SO.sub.2Me H H OMe H 104 4 SO.sub.2Me H H OMe H 105 1 SO.sub.2NH.sub.2 H H OMe H 106 2 SO.sub.2NH.sub.2 H H OMe H 107 3 SO.sub.2NH.sub.2 H H OMe H 108 4 SO.sub.2NH.sub.2 H H OMe H 109 1 H H H Me H 110 2 H H H Me H 111 3 H H H Me H 112 4 H H H Me H 113 1 Me H H Me H 114 2 Me H H Me H 115 3 Me H H Me H 116 4 Me H H Me H 117 1 CH.sub.2Ph H H Me H 118 2 CH.sub.2Ph H H Me H 119 3 CH.sub.2Ph H H Me H 120 4 CH.sub.2Ph H H Me H 121 1 COMe H H Me H 122 2 COMe H H Me H 123 3 COMe H H Me H 124 4 COMe H H Me H 125 1 CO.sub.2Me H H Me H 126 2 CO.sub.2Me H H Me H 127 3 CO.sub.2Me H H Me H 128 4 CO.sub.2Me H H Me H 129 1 CO.sub.2tBu H H Me H 130 2 CO.sub.2tBu H H Me H 131 3 CO.sub.2tBu H H Me H 132 4 CO.sub.2tBu H H Me H 133 1 CONHMe H H Me H 134 2 CONHMe H H Me H 135 3 CONHMe H H Me H 136 4 CONHMe H H Me H 137 1 SO.sub.2Me H H Me H 138 2 SO.sub.2Me H H Me H 139 3 SO.sub.2Me H H Me H 140 4 SO.sub.2Me H H Me H 141 1 SO.sub.2NH.sub.2 H H Me H 142 2 SO.sub.2NH.sub.2 H H Me H 143 3 SO.sub.2NH.sub.2 H H Me H 144 4 SO.sub.2NH.sub.2 H H Me H 145 1 H H H CF.sub.3 H 146 2 H H H CF.sub.3 H 147 3 H H H CF.sub.3 H 148 4 H H H CF.sub.3 H 149 1 Me H H CF.sub.3 H 150 2 Me H H CF.sub.3 H 151 3 Me H H CF.sub.3 H 152 4 Me H H CF.sub.3 H 153 1 CH.sub.2Ph H H CF.sub.3 H 154 2 CH.sub.2Ph H H CF.sub.3 H 155 3 CH.sub.2Ph H H CF.sub.3 H 156 4 CH.sub.2Ph H H CF.sub.3 H 157 1 COMe H H CF.sub.3 H 158 2 COMe H H CF.sub.3 H 159 3 COMe H H CF.sub.3 H 160 4 COMe H H CF.sub.3 H 161 1 CO.sub.2Me H H CF.sub.3 H 162 2 CO.sub.2Me H H CF.sub.3 H 163 3 CO.sub.2Me H H CF.sub.3 H 164 4 CO.sub.2Me H H CF.sub.3 H 165 1 CO.sub.2tBu H H CF.sub.3 H 166 2 CO.sub.2tBu H H CF.sub.3 H 167 3 CO.sub.2tBu H H CF.sub.3 H 168 4 CO.sub.2tBu H H CF.sub.3 H 169 1 CONHMe H H CF.sub.3 H 170 2 CONHMe H H CF.sub.3 H 171 3 CONHMe H H CF.sub.3 H 172 4 CONHMe H H CF.sub.3 H 173 1 SO.sub.2Me H H CF.sub.3 H 174 2 SO.sub.2Me H H CF.sub.3 H 175 3 SO.sub.2Me H H CF.sub.3 H 176 4 SO.sub.2Me H H CF.sub.3 H 177 1 SO.sub.2NH.sub.2 H H CF.sub.3 H 178 2 SO.sub.2NH.sub.2 H H CF.sub.3 H 179 3 SO.sub.2NH.sub.2 H H CF.sub.3 H 180 4 SO.sub.2NH.sub.2 H H CF.sub.3 H 181 1 H H H F H 182 2 H H H F H 183 3 H H H F H 184 4 H H H F H 185 1 Me H H F H 186 2 Me H H F H 187 3 Me H H F H 188 4 Me H H F H 189 1 CH.sub.2Ph H H F H 190 2 CH.sub.2Ph H H F H 191 3 CH.sub.2Ph H H F H 192 4 CH.sub.2Ph H H F H 193 1 COMe H H F H 194 2 COMe H H F H 195 3 COMe H H F H 196 4 COMe H H F H 197 1 CO.sub.2Me H H F H 198 2 CO.sub.2Me H H F H 199 3 CO.sub.2Me H H F H 200 4 CO.sub.2Me H H F H 201 1 CO.sub.2tBu H H F H 202 2 CO.sub.2tBu H H F H 203 3 CO.sub.2tBu H H F H 204 4 CO.sub.2tBu H H F H 205 1 CONHMe H H F H 206 2 CONHMe H H F H 207 3 CONHMe H H F H 208 4 CONHMe H H F H 209 1 SO.sub.2Me H H F H 210 2 SO.sub.2Me H H F H 211 3 SO.sub.2Me H H F H 212 4 SO.sub.2Me H H F H 213 1 SO.sub.2NH.sub.2 H H F H 214 2 SO.sub.2NH.sub.2 H H F H 215 3 SO.sub.2NH.sub.2 H H F H 216 4 SO.sub.2NH.sub.2 H H F H 217 1 H H H Cl H 218 2 H H H Cl H 219 3 H H H Cl H 220 4 H H H Cl H 221 1 Me H H Cl H 222 2 Me H H Cl H 223 3 Me H H Cl H 224 4 Me H H Cl H 225 1 CH.sub.2Ph H H Cl H 226 2 CH.sub.2Ph H H Cl H 227 3 CH.sub.2Ph H H Cl H 228 4 CH.sub.2Ph H H Cl H 229 1 COMe H H Cl H 230 2 COMe H H Cl H 231 3 COMe H H Cl H 232 4 COMe H H Cl H 233 1 CO.sub.2Me H H Cl H 234 2 CO.sub.2Me H H Cl H 235 3 CO.sub.2Me H H Cl H 236 4 CO.sub.2Me H H Cl H 237 1 CO.sub.2tBu H H Cl H 238 2 CO.sub.2tBu H H Cl H 239 3 CO.sub.2tBu H H Cl H 240 4 CO.sub.2tBu H H Cl H 241 1 CONHMe H H Cl H 242 2 CONHMe H H Cl H 243 3 CONHMe H H Cl H 244 4 CONHMe H H Cl H 245 1 SO.sub.2Me H H Cl H 246 2 SO.sub.2Me H H Cl H 247 3 SO.sub.2Me H H Cl H 248 4 SO.sub.2Me H H Cl H 249 1 SO.sub.2NH.sub.2 H H Cl H 250 2 SO.sub.2NH.sub.2 H H Cl H 251 3 SO.sub.2NH.sub.2 H H Cl H 252 4 SO.sub.2NH.sub.2 H H Cl H 253 1 H H H CN H 254 2 H H H CN H 255 3 H H H CN H 256 4 H H H CN H 257 1 Me H H CN H 258 2 Me H H CN H 259 3 Me H H CN H 260 4 Me H H CN H 261 1 CH.sub.2Ph H H CN H 262 2 CH.sub.2Ph H H CN H 263 3 CH.sub.2Ph H H CN H 264 4 CH.sub.2Ph H H CN H 265 1 COMe H H CN H 266 2 COMe H H CN H 267 3 COMe H H CN H 268 4 COMe H H CN H 269 1 CO.sub.2Me H H CN H 270 2 CO.sub.2Me H H CN H 271 3 CO.sub.2Me H H CN H 272 4 CO.sub.2Me H H CN H 273 1 CO.sub.2tBu H H CN H 274 2 CO.sub.2tBu H H CN H 275 3 CO.sub.2tBu H H CN H 276 4 CO.sub.2tBu H H CN H 277 1 CONHMe H H CN H 278 2 CONHMe H H CN H 279 3 CONHMe H H CN H 280 4 CONHMe H H CN H 281 1 SO.sub.2Me H H CN H 282 2 SO.sub.2Me H H CN H 283 3 SO.sub.2Me H H CN H 284 4 SO.sub.2Me H H CN H 285 1 SO.sub.2NH.sub.2 H H CN H 286 2 SO.sub.2NH.sub.2 H H CN H 287 3 SO.sub.2NH.sub.2 H H CN H 288 4 SO.sub.2NH.sub.2 H H CN H 289 1 H H H H OH 290 2 H H H H OH 291 3 H H H H OH 292 4 H H H H OH 293 1 Me H H H OH 294 2 Me H H H OH 295 3 Me H H H OH 296 4 Me H H H OH 297 1 CH.sub.2Ph H H H OH 298 2 CH.sub.2Ph H H H OH 299 3 CH.sub.2Ph H H H OH 300 4 CH.sub.2Ph H H H OH 301 1 COMe H H H OH 302 2 COMe H H H OH 303 3 COMe H H H OH 304 4 COMe H H H OH 305 1 CO.sub.2Me H H H OH 306 2 CO.sub.2Me H H H OH 307 3 CO.sub.2Me H H H OH 308 4 CO.sub.2Me H H H OH 309 1 CO.sub.2tBu H H H OH 310 2 CO.sub.2tBu H H H OH 311 3 CO.sub.2tBu H H H OH 312 4 CO.sub.2tBu H H H OH 313 1 CONHMe H H H OH 314 2 CONHMe H H H OH 315 3 CONHMe H H H OH 316 4 CONHMe H H H OH 317 1 SO.sub.2Me H H H OH 318 2 SO.sub.2Me H H H OH 319 3 SO.sub.2Me H H H OH 320 4 SO.sub.2Me H H H OH 321 1 SO.sub.2NH.sub.2 H H H OH 322 2 SO.sub.2NH.sub.2 H H H OH 323 3 SO.sub.2NH.sub.2 H H H OH 324 4 SO.sub.2NH.sub.2 H H H OH 325 1 H H H H OMe 326 2 H H H H OMe 327 3 H H H H OMe 328 4 H H H H OMe 329 1 Me H H H OMe 330 2 Me H H H OMe 331 3 Me H H H OMe 332 4 Me H H H OMe 333 1 CH.sub.2Ph H H H OMe 334 2 CH.sub.2Ph H H H OMe 335 3 CH.sub.2Ph H H H OMe 336 4 CH.sub.2Ph H H H OMe 337 1 COMe H H H OMe 338 2 COMe H H H OMe 339 3 COMe H H H OMe 340 4 COMe H H H OMe 341 1 CO.sub.2Me H H H OMe 342 2 CO.sub.2Me H H H OMe 343 3 CO.sub.2Me H H H OMe 344 4 CO.sub.2Me H H H OMe 345 1 CO.sub.2tBu H H H OMe 346 2 CO.sub.2tBu H H H OMe 347 3 CO.sub.2tBu H H H OMe 348 4 CO.sub.2tBu H H H OMe 349 1 CONHMe H H H OMe 350 2 CONHMe H H H OMe 351 3 CONHMe H H H OMe 352 4 CONHMe H H H OMe 353 1 SO.sub.2Me H H H OMe 354 2 SO.sub.2Me H H H OMe 355 3 SO.sub.2Me H H H OMe 356 4 SO.sub.2Me H H H OMe 357 1 SO.sub.2NH.sub.2 H H H OMe 358 2 SO.sub.2NH.sub.2 H H H OMe 359 3 SO.sub.2NH.sub.2 H H H OMe 360 4 SO.sub.2NH.sub.2 H H H OMe 361 1 H H H H Me 362 2 H H H H Me 363 3 H H H H Me 364 4 H H H H Me 365 1 Me H H H Me 366 2 Me H H H Me 367 3 Me H H H Me 368 4 Me H H H Me 369 1 CH.sub.2Ph H H H Me 370 2 CH.sub.2Ph H H H Me 371 3 CH.sub.2Ph H H H Me 372 4 CH.sub.2Ph H H H Me 373 1 COMe H H H Me 374 2 COMe H H H Me 375 3 COMe H H H Me 376 4 COMe H H H Me 377 1 CO.sub.2Me H H H Me 378 2 CO.sub.2Me H H H Me 379 3 CO.sub.2Me H H H Me 380 4 CO.sub.2Me H H H Me 381 1 CO.sub.2tBu H H H Me 382 2 CO.sub.2tBu H H H Me 383 3 CO.sub.2tBu H H H Me 384 4 CO.sub.2tBu H H H Me 385 1 CONHMe H H H Me 386 2 CONHMe H H H Me 387 3 CONHMe H H H Me 388 4 CONHMe H H H Me 389 1 SO.sub.2Me H H H Me 390 2 SO.sub.2Me H H H Me 391 3 SO.sub.2Me H H H Me 392 4 SO.sub.2Me H H H Me 393 1 SO.sub.2NH.sub.2 H H H Me 394 2 SO.sub.2NH.sub.2 H H H Me 395 3 SO.sub.2NH.sub.2 H H H Me 396 4 SO.sub.2NH.sub.2 H H H Me 397 1 H H H H CF.sub.3 398 2 H H H H CF.sub.3 399 3 H H H H CF.sub.3 400 4 H H H H CF.sub.3 401 1 Me H H H CF.sub.3 402 2 Me H H H CF.sub.3 403 3 Me H H H CF.sub.3 404 4 Me H H H CF.sub.3 405 1 CH.sub.2Ph H H H CF.sub.3 406 2 CH.sub.2Ph H H H CF.sub.3 407 3 CH.sub.2Ph H H H CF.sub.3 408 4 CH.sub.2Ph H H H CF.sub.3 409 1 COMe H H H CF.sub.3 410 2 COMe H H H CF.sub.3 411 3 COMe H H H CF.sub.3 412 4 COMe H H H CF.sub.3 413 1 CO.sub.2Me H H H CF.sub.3 414 2 CO.sub.2Me H H H CF.sub.3 415 3 CO.sub.2Me H H H CF.sub.3 416 4 CO.sub.2Me H H H CF.sub.3 417 1 CO.sub.2tBu H H H CF.sub.3 418 2 CO.sub.2tBu H H H CF.sub.3 419 3 CO.sub.2tBu H H H CF.sub.3 420 4 CO.sub.2tBu H H H CF.sub.3 421 1 CONHMe H H H CF.sub.3 422 2 CONHMe H H H CF.sub.3 423 3 CONHMe H H H CF.sub.3 424 4 CONHMe H H H CF.sub.3 425 1 SO.sub.2Me H H H CF.sub.3 426 2 SO.sub.2Me H H H CF.sub.3 427 3 SO.sub.2Me H H H CF.sub.3 428 4 SO.sub.2Me H H H CF.sub.3 429 1 SO.sub.2NH.sub.2 H H H CF.sub.3 430 2 SO.sub.2NH.sub.2 H H H CF.sub.3 431 3 SO.sub.2NH.sub.2 H H H CF.sub.3 432 4 SO.sub.2NH.sub.2 H H H CF.sub.3 433 1 H H H H F 434 2 H H H H F 435 3 H H H H F 436 3 H H H H F 437 1 Me H H H F 438 2 Me H H H F 439 3 Me H H H F 440 4 Me H H H F 441 1 CH.sub.2Ph H H H F 442 2 CH.sub.2Ph H H H F 443 3 CH.sub.2Ph H H H F 444 4 CH.sub.2Ph H H H F 445 1 COMe H H H F 446 2 COMe H H H F 447 3 COMe H H H F 448 4 COMe H H H F 449 1 CO.sub.2Me H H H F 450 2 CO.sub.2Me H H H F 451 3 CO.sub.2Me H H H F 452 4 CO.sub.2Me H H H F 453 1 CO.sub.2tBu H H H F 454 2 CO.sub.2tBu H H H F 455 3 CO.sub.2tBu H H H F 456 4 CO.sub.2tBu H H H F 457 1 CONHMe H H H F 458 2 CONHMe H H H F 459 3 CONHMe H H H F 460 4 CONHMe H H H F 461 1 SO.sub.2Me H H H F 462 2 SO.sub.2Me H H H F 463 3 SO.sub.2Me H H H F 464 4 SO.sub.2Me H H H F 465 1 SO.sub.2NH.sub.2 H H H F 466 2 SO.sub.2NH.sub.2 H H H F 467 3 SO.sub.2NH.sub.2 H H H F 468 4 SO.sub.2NH.sub.2 H H H F 469 1 H H H H Cl 470 2 H H H H Cl 471 3 H H H H Cl 472 4 H H H H Cl 473 1 Me H H H Cl 474 2 Me H H H Cl 475 3 Me H H H Cl 476 4 Me H H H Cl 477 1 CH.sub.2Ph H H H Cl 478 2 CH.sub.2Ph H H H Cl 479 3 CH.sub.2Ph H H H Cl 480 4 CH.sub.2Ph H H H Cl 481 1 COMe H H H Cl 482 2 COMe H H H Cl 483 3 COMe H H H Cl 484 4 COMe H H H Cl 485 1 CO.sub.2Me H H H Cl 486 2 CO.sub.2Me H H H Cl 487 3 CO.sub.2Me H H H Cl 488 4 CO.sub.2Me H H H Cl 489 1 CO.sub.2tBu H H H Cl 490 2 CO.sub.2tBu H H H Cl 491 3 CO.sub.2tBu H H H Cl 492 4 CO.sub.2tBu H H H Cl 493 1 CONHMe H H H Cl 494 2 CONHMe H H H Cl 495 3 CONHMe H H H Cl 496 4 CONHMe H H H Cl 497 1 SO.sub.2Me H H H Cl 498 2 SO.sub.2Me H H H Cl 499 3 SO.sub.2Me H H H Cl 500 4 SO.sub.2Me H H H Cl 501 1 SO.sub.2NH.sub.2 H H H Cl 502 2 SO.sub.2NH.sub.2 H H H Cl 503 3 SO.sub.2NH.sub.2 H H H Cl 504 4 SO.sub.2NH.sub.2 H H H Cl 505 1 H H H H CN 506 2 H H H H CN 507 3 H H H H CN 508 4 H H H H CN 509 1 Me H H H CN 510 2 Me H H H CN 511 3 Me H H H CN 512 4 Me H H H CN 513 1 CH.sub.2Ph H H H CN 514 2 CH.sub.2Ph H H H CN 515 3 CH.sub.2Ph H H H CN 516 4 CH.sub.2Ph H H H CN 517 1 COMe H H H CN 518 2 COMe H H H CN 519 3 COMe H H H CN 520 4 COMe H H H CN 521 1 CO.sub.2Me H H H CN 522 2 CO.sub.2Me H H H CN 523 3 CO.sub.2Me H H H CN 524 4 CO.sub.2Me H H H CN 525 1 CO.sub.2tBu H H H CN 526 2 CO.sub.2tBu H H H CN 527 3 CO.sub.2tBu H H H CN 528 4 CO.sub.2tBu H H H CN 529 1 CONHMe H H H CN 530 2 CONHMe H H H CN 531 3 CONHMe H H H CN 532 4 CONHMe H H H CN 533 1 SO.sub.2Me H H H CN 534 2 SO.sub.2Me H H H CN 535 3 SO.sub.2Me H H H CN 536 4 SO.sub.2Me H H H CN 537 1 SO.sub.2NH.sub.2 H H H CN 538 2 SO.sub.2NH.sub.2 H H H CN 539 3 SO.sub.2NH.sub.2 H H H CN 540 4 SO.sub.2NH.sub.2 H H H CN

    [2048] Exemplary embodiments include compounds having the formula (XXXV)

    ##STR00449##

    [2049] or a pharmaceutically acceptable salt form thereof defined herein below in Table 28.

    TABLE-US-00028 TABLE 28 Entry n X R.sup.3 1 1 O Phenyl 2 2 O Phenyl 3 3 O Phenyl 4 4 O Phenyl 5 1 S Phenyl 6 2 S Phenyl 7 3 S Phenyl 8 4 S Phenyl 9 1 SO Phenyl 10 2 SO Phenyl 11 3 SO Phenyl 12 4 SO Phenyl 13 1 SO.sub.2 Phenyl 14 2 SO.sub.2 Phenyl 15 3 SO.sub.2 Phenyl 16 4 SO.sub.2 Phenyl 17 1 O 3-OH-Phenyl 18 2 O 3-OH-Phenyl 19 3 O 3-OH-Phenyl 20 4 O 3-OH-Phenyl 21 1 S 3-OH-Phenyl 22 2 S 3-OH-Phenyl 23 3 S 3-OH-Phenyl 24 4 S 3-OH-Phenyl 25 1 SO 3-OH-Phenyl 26 2 SO 3-OH-Phenyl 27 3 SO 3-OH-Phenyl 28 4 SO 3-OH-Phenyl 29 1 SO.sub.2 3-OH-Phenyl 30 2 SO.sub.2 3-OH-Phenyl 31 3 SO.sub.2 3-OH-Phenyl 32 4 SO.sub.2 3-OH-Phenyl 33 1 O 4-NO.sub.2-Phenyl 34 2 O 4-NO.sub.2-Phenyl 35 3 O 4-NO.sub.2-Phenyl 36 4 O 4-NO.sub.2-Phenyl 37 1 S 4-NO.sub.2-Phenyl 38 2 S 4-NO.sub.2-Phenyl 39 3 S 4-NO.sub.2-Phenyl 40 4 S 4-NO.sub.2-Phenyl 41 1 SO 4-NO.sub.2-Phenyl 42 2 SO 4-NO.sub.2-Phenyl 43 3 SO 4-NO.sub.2-Phenyl 44 4 SO 4-NO.sub.2-Phenyl 45 1 SO.sub.2 4-NO.sub.2-Phenyl 46 2 SO.sub.2 4-NO.sub.2-Phenyl 47 3 SO.sub.2 4-NO.sub.2-Phenyl 48 4 SO.sub.2 4-NO.sub.2-Phenyl 49 1 O 3-OMe-Phenyl 50 2 O 3-OMe-Phenyl 51 3 O 3-OMe-Phenyl 52 4 O 3-OMe-Phenyl 53 1 S 3-OMe-Phenyl 54 2 S 3-OMe-Phenyl 55 3 S 3-OMe-Phenyl 56 4 S 3-OMe-Phenyl 57 1 SO 3-OMe-Phenyl 58 2 SO 3-OMe-Phenyl 59 3 SO 3-OMe-Phenyl 60 4 SO 3-OMe-Phenyl 61 1 SO.sub.2 3-OMe-Phenyl 62 2 SO.sub.2 3-OMe-Phenyl 63 3 SO.sub.2 3-OMe-Phenyl 64 4 SO.sub.2 3-OMe-Phenyl 65 1 O 4-CN-Phenyl 66 2 O 4-CN-Phenyl 67 3 O 4-CN-Phenyl 68 4 O 4-CN-Phenyl 69 1 S 4-CN-Phenyl 70 2 S 4-CN-Phenyl 71 3 S 4-CN-Phenyl 72 4 S 4-CN-Phenyl 73 1 SO 4-CN-Phenyl 74 2 SO 4-CN-Phenyl 75 3 SO 4-CN-Phenyl 76 4 SO 4-CN-Phenyl 77 1 SO.sub.2 4-CN-Phenyl 78 2 SO.sub.2 4-CN-Phenyl 79 3 SO.sub.2 4-CN-Phenyl 80 4 SO.sub.2 4-CN-Phenyl 81 1 O 2-CN-Phenyl 82 2 O 2-CN-Phenyl 83 3 O 2-CN-Phenyl 84 4 O 2-CN-Phenyl 85 1 S 2-CN-Phenyl 86 2 S 2-CN-Phenyl 87 3 S 2-CN-Phenyl 88 4 S 2-CN-Phenyl 89 1 SO 2-CN-Phenyl 90 2 SO 2-CN-Phenyl 91 3 SO 2-CN-Phenyl 92 4 SO 2-CN-Phenyl 93 1 SO.sub.2 2-CN-Phenyl 94 2 SO.sub.2 2-CN-Phenyl 95 3 SO.sub.2 2-CN-Phenyl 96 4 SO.sub.2 2-CN-Phenyl 97 1 O 3-Me-Phenyl 98 2 O 3-Me-Phenyl 99 3 O 3-Me-Phenyl 100 4 O 3-Me-Phenyl 101 1 S 3-Me-Phenyl 102 2 S 3-Me-Phenyl 103 3 S 3-Me-Phenyl 104 4 S 3-Me-Phenyl 105 1 SO 3-Me-Phenyl 106 2 SO 3-Me-Phenyl 107 3 SO 3-Me-Phenyl 108 4 SO 3-Me-Phenyl 109 1 SO.sub.2 3-Me-Phenyl 110 2 SO.sub.2 3-Me-Phenyl 111 3 SO.sub.2 3-Me-Phenyl 112 4 SO.sub.2 3-Me-Phenyl 113 1 O 2-F-Phenyl 114 2 O 2-F-Phenyl 115 3 O 2-F-Phenyl 116 4 O 2-F-Phenyl 117 1 S 2-F-Phenyl 118 2 S 2-F-Phenyl 119 3 S 2-F-Phenyl 120 4 S 2-F-Phenyl 121 1 SO 2-F-Phenyl 122 2 SO 2-F-Phenyl 123 3 SO 2-F-Phenyl 124 4 SO 2-F-Phenyl 125 1 SO.sub.2 2-F-Phenyl 126 2 SO.sub.2 2-F-Phenyl 127 3 SO.sub.2 2-F-Phenyl 128 4 SO.sub.2 2-F-Phenyl 129 1 O 4-F-Phenyl 130 2 O 4-F-Phenyl 131 3 O 4-F-Phenyl 132 4 O 4-F-Phenyl 133 1 S 4-F-Phenyl 134 2 S 4-F-Phenyl 135 3 S 4-F-Phenyl 136 4 S 4-F-Phenyl 137 1 SO 4-F-Phenyl 138 2 SO 4-F-Phenyl 139 3 SO 4-F-Phenyl 140 4 SO 4-F-Phenyl 141 1 SO.sub.2 4-F-Phenyl 142 2 SO.sub.2 4-F-Phenyl 143 3 SO.sub.2 4-F-Phenyl 144 4 SO.sub.2 4-F-Phenyl 145 1 O 3-Cl-Phenyl 146 2 O 3-Cl-Phenyl 147 3 O 3-Cl-Phenyl 148 4 O 3-Cl-Phenyl 149 1 S 3-Cl-Phenyl 150 2 S 3-Cl-Phenyl 151 3 S 3-Cl-Phenyl 152 4 S 3-Cl-Phenyl 153 1 SO 3-Cl-Phenyl 154 2 SO 3-Cl-Phenyl 155 3 SO 3-Cl-Phenyl 156 4 SO 3-Cl-Phenyl 157 1 SO.sub.2 3-Cl-Phenyl 158 2 SO.sub.2 3-Cl-Phenyl 159 3 SO.sub.2 3-Cl-Phenyl 160 4 SO.sub.2 3-Cl-Phenyl 161 1 O 2-Br-Phenyl 162 2 O 2-Br-Phenyl 163 3 O 2-Br-Phenyl 164 4 O 2-Br-Phenyl 165 1 S 2-Br-Phenyl 166 2 S 2-Br-Phenyl 167 3 S 2-Br-Phenyl 168 4 S 2-Br-Phenyl 169 1 SO 2-Br-Phenyl 170 2 SO 2-Br-Phenyl 171 3 SO 2-Br-Phenyl 172 4 SO 2-Br-Phenyl 173 1 SO.sub.2 2-Br-Phenyl 174 2 SO.sub.2 2-Br-Phenyl 175 3 SO.sub.2 2-Br-Phenyl 176 4 SO.sub.2 2-Br-Phenyl 177 1 O 4-Br-Phenyl 178 2 O 4-Br-Phenyl 179 3 O 4-Br-Phenyl 180 4 O 4-Br-Phenyl 181 1 S 4-Br-Phenyl 182 2 S 4-Br-Phenyl 183 3 S 4-Br-Phenyl 184 4 S 4-Br-Phenyl 185 1 SO 4-Br-Phenyl 186 2 SO 4-Br-Phenyl 187 3 SO 4-Br-Phenyl 188 4 SO 4-Br-Phenyl 189 1 SO.sub.2 4-Br-Phenyl 190 2 SO.sub.2 4-Br-Phenyl 191 3 SO.sub.2 4-Br-Phenyl 192 4 SO.sub.2 4-Br-Phenyl 193 1 O 3-CF.sub.3-Phenyl 194 2 O 3-CF.sub.3-Phenyl 195 3 O 3-CF.sub.3-Phenyl 196 4 O 3-CF.sub.3-Phenyl 197 1 S 3-CF.sub.3-Phenyl 198 2 S 3-CF.sub.3-Phenyl 199 3 S 3-CF.sub.3-Phenyl 200 4 S 3-CF.sub.3-Phenyl 201 1 SO 3-CF.sub.3-Phenyl 202 2 SO 3-CF.sub.3-Phenyl 203 3 SO 3-CF.sub.3-Phenyl 204 4 SO 3-CF.sub.3-Phenyl 205 1 SO.sub.2 3-CF.sub.3-Phenyl 206 2 SO.sub.2 3-CF.sub.3-Phenyl 207 3 SO.sub.2 3-CF.sub.3-Phenyl 208 4 SO.sub.2 3-CF.sub.3-Phenyl 209 1 O 2-iPr-Phenyl 210 2 O 2-iPr-Phenyl 211 3 O 2-iPr-Phenyl 212 4 O 2-iPr-Phenyl 213 1 S 2-iPr-Phenyl 214 2 S 2-iPr-Phenyl 215 3 S 2-iPr-Phenyl 216 4 S 2-iPr-Phenyl 217 1 SO 2-iPr-Phenyl 218 2 SO 2-iPr-Phenyl 219 3 SO 2-iPr-Phenyl 220 4 SO 2-iPr-Phenyl 221 1 SO.sub.2 2-iPr-Phenyl 222 2 SO.sub.2 2-iPr-Phenyl 223 3 SO.sub.2 2-iPr-Phenyl 224 4 SO.sub.2 2-iPr-Phenyl 225 1 O 4-iPr-Phenyl 226 2 O 4-iPr-Phenyl 227 3 O 4-iPr-Phenyl 228 4 O 4-iPr-Phenyl 229 1 S 4-iPr-Phenyl 230 2 S 4-iPr-Phenyl 231 3 S 4-iPr-Phenyl 232 4 S 4-iPr-Phenyl 233 1 SO 4-iPr-Phenyl 234 2 SO 4-iPr-Phenyl 235 3 SO 4-iPr-Phenyl 236 4 SO 4-iPr-Phenyl 237 1 SO.sub.2 4-iPr-Phenyl 238 2 SO.sub.2 4-iPr-Phenyl 239 3 SO.sub.2 4-iPr-Phenyl 240 4 SO.sub.2 4-iPr-Phenyl 241 1 O 3-NH.sub.2-Phenyl 242 2 O 3-NH.sub.2-Phenyl 243 3 O 3-NH.sub.2-Phenyl 244 4 O 3-NH.sub.2-Phenyl 245 1 S 3-NH.sub.2-Phenyl 246 2 S 3-NH.sub.2-Phenyl 247 3 S 3-NH.sub.2-Phenyl 248 1 S 3-NH.sub.2-Phenyl 249 2 SO 3-NH.sub.2-Phenyl 250 3 SO 3-NH.sub.2-Phenyl 251 4 SO 3-NH.sub.2-Phenyl 252 1 SO 3-NH.sub.2-Phenyl 253 2 SO.sub.2 3-NH.sub.2-Phenyl 254 3 SO.sub.2 3-NH.sub.2-Phenyl 255 4 SO.sub.2 3-NH.sub.2-Phenyl 256 1 O 2,4-di-Me-Phenyl 257 2 O 2,4-di-Me-Phenyl 258 3 O 2,4-di-Me-Phenyl 259 4 O 2,4-di-Me-Phenyl 260 1 S 2,4-di-Me-Phenyl 261 2 S 2,4-di-Me-Phenyl 262 3 S 2,4-di-Me-Phenyl 263 4 S 2,4-di-Me-Phenyl 264 1 SO 2,4-di-Me-Phenyl 265 2 SO 2,4-di-Me-Phenyl 266 3 SO 2,4-di-Me-Phenyl 267 4 SO 2,4-di-Me-Phenyl 268 1 SO.sub.2 2,4-di-Me-Phenyl 269 2 SO.sub.2 2,4-di-Me-Phenyl 270 3 SO.sub.2 2,4-di-Me-Phenyl 271 4 SO.sub.2 2,4-di-Me-Phenyl 272 1 O 2,6-di-iPr-Phenyl 273 2 O 2,6-di-iPr-Phenyl 274 3 O 2,6-di-iPr-Phenyl 275 4 O 2,6-di-iPr-Phenyl 276 1 S 2,6-di-iPr-Phenyl 277 2 S 2,6-di-iPr-Phenyl 278 3 S 2,6-di-iPr-Phenyl 279 4 S 2,6-di-iPr-Phenyl 280 1 SO 2,6-di-iPr-Phenyl 281 2 SO 2,6-di-iPr-Phenyl 282 3 SO 2,6-di-iPr-Phenyl 283 4 SO 2,6-di-iPr-Phenyl 284 1 SO.sub.2 2,6-di-iPr-Phenyl 285 2 SO.sub.2 2,6-di-iPr-Phenyl 286 3 SO.sub.2 2,6-di-iPr-Phenyl 287 4 SO.sub.2 2,6-di-iPr-Phenyl 288 1 O 3-Ph-Phenyl 289 2 O 3-Ph-Phenyl 290 3 O 3-Ph-Phenyl 291 4 O 3-Ph-Phenyl 292 1 S 3-Ph-Phenyl 293 2 S 3-Ph-Phenyl 294 3 S 3-Ph-Phenyl 295 4 S 3-Ph-Phenyl 296 1 SO 3-Ph-Phenyl 297 2 SO 3-Ph-Phenyl 298 3 SO 3-Ph-Phenyl 299 4 SO 3-Ph-Phenyl 300 1 SO.sub.2 3-Ph-Phenyl 301 2 SO.sub.2 3-Ph-Phenyl 302 3 SO.sub.2 3-Ph-Phenyl 303 4 SO.sub.2 3-Ph-Phenyl 304 1 O 2-morpholino-phenyl 305 2 O 2-morpholino-phenyl 306 3 O 2-morpholino-phenyl 307 4 O 2-morpholino-phenyl 308 1 S 2-morpholino-phenyl 309 2 S 2-morpholino-phenyl 310 3 S 2-morpholino-phenyl 311 4 S 2-morpholino-phenyl 312 1 SO 2-morpholino-phenyl 313 2 SO 2-morpholino-phenyl 314 3 SO 2-morpholino-phenyl 315 4 SO 2-morpholino-phenyl 316 1 SO.sub.2 2-morpholino-phenyl 317 2 SO.sub.2 2-morpholino-phenyl 318 3 SO.sub.2 2-morpholino-phenyl 319 4 SO.sub.2 2-morpholino-phenyl 320 1 O 4-morpholino-phenyl 321 2 O 4-morpholino-phenyl 322 3 O 4-morpholino-phenyl 323 4 O 4-morpholino-phenyl 324 1 SO 4-morpholino-phenyl 325 2 SO 4-morpholino-phenyl 326 3 SO 4-morpholino-phenyl 327 4 SO 4-morpholino-phenyl 328 1 O naphthylen-1-yl 329 2 O naphthylen-1-yl 330 3 O naphthylen-1-yl 331 4 O naphthylen-1-yl 332 1 S naphthylen-1-yl 333 2 S naphthylen-1-yl 334 3 S naphthylen-1-yl 335 4 S naphthylen-1-yl 336 1 SO naphthylen-1-yl 337 2 SO naphthylen-1-yl 338 3 SO naphthylen-1-yl 339 4 SO naphthylen-1-yl 340 1 SO.sub.2 naphthylen-1-yl 341 2 SO.sub.2 naphthylen-1-yl 342 3 SO.sub.2 naphthylen-1-yl 343 4 SO.sub.2 naphthylen-1-yl 344 1 O 4-OH-Phenyl 345 2 O 4-OH-Phenyl 346 3 O 4-OH-Phenyl 347 4 O 4-OH-Phenyl 348 1 S 4-OH-Phenyl 349 2 S 4-OH-Phenyl 350 3 S 4-OH-Phenyl 351 4 S 4-OH-Phenyl 352 1 SO 4-OH-Phenyl 353 2 SO 4-OH-Phenyl 354 3 SO 4-OH-Phenyl 355 4 SO 4-OH-Phenyl 356 1 SO.sub.2 4-OH-Phenyl 357 2 SO.sub.2 4-OH-Phenyl 358 3 SO.sub.2 4-OH-Phenyl 359 4 SO.sub.2 4-OH-Phenyl 360 1 O 2-OH-Phenyl 361 2 O 2-OH-Phenyl 362 3 O 2-OH-Phenyl 363 4 O 2-OH-Phenyl 364 1 S 2-OH-Phenyl 365 2 S 2-OH-Phenyl 366 3 S 2-OH-Phenyl 367 4 S 2-OH-Phenyl 368 1 SO 2-OH-Phenyl 369 2 SO 2-OH-Phenyl 370 3 SO 2-OH-Phenyl 371 4 SO 2-OH-Phenyl 372 1 SO.sub.2 2-OH-Phenyl 373 2 SO.sub.2 2-OH-Phenyl 374 3 SO.sub.2 2-OH-Phenyl 375 4 SO.sub.2 2-OH-Phenyl 376 1 O 4-OMe-Phenyl 377 2 O 4-OMe-Phenyl 378 3 O 4-OMe-Phenyl 379 4 O 4-OMe-Phenyl 380 1 S 4-OMe-Phenyl 381 2 S 4-OMe-Phenyl 382 3 S 4-OMe-Phenyl 383 4 S 4-OMe-Phenyl 384 1 SO 4-OMe-Phenyl 385 2 SO 4-OMe-Phenyl 386 3 SO 4-OMe-Phenyl 387 4 SO 4-OMe-Phenyl 388 1 SO.sub.2 4-OMe-Phenyl 389 2 SO.sub.2 4-OMe-Phenyl 390 3 SO.sub.2 4-OMe-Phenyl 391 4 SO.sub.2 4-OMe-Phenyl 392 1 O 2-OMe-Phenyl 393 2 O 2-OMe-Phenyl 394 3 O 2-OMe-Phenyl 395 4 O 2-OMe-Phenyl 396 1 S 2-OMe-Phenyl 397 2 S 2-OMe-Phenyl 398 3 S 2-OMe-Phenyl 399 4 S 2-OMe-Phenyl 400 1 SO 2-OMe-Phenyl 401 2 SO 2-OMe-Phenyl 402 3 SO 2-OMe-Phenyl 403 4 SO 2-OMe-Phenyl 404 1 SO.sub.2 2-OMe-Phenyl 405 2 SO.sub.2 2-OMe-Phenyl 406 3 SO.sub.2 2-OMe-Phenyl 407 4 SO.sub.2 2-OMe-Phenyl 408 1 O 3-CN-Phenyl 409 2 O 3-CN-Phenyl 410 3 O 3-CN-Phenyl 411 4 O 3-CN-Phenyl 412 1 S 3-CN-Phenyl 413 2 S 3-CN-Phenyl 414 3 S 3-CN-Phenyl 415 4 S 3-CN-Phenyl 416 1 SO 3-CN-Phenyl 417 2 SO 3-CN-Phenyl 418 3 SO 3-CN-Phenyl 419 4 SO 3-CN-Phenyl 420 1 SO.sub.2 3-CN-Phenyl 421 2 SO.sub.2 3-CN-Phenyl 422 3 SO.sub.2 3-CN-Phenyl 423 4 SO.sub.2 3-CN-Phenyl 424 1 O 2-Me-Phenyl 425 2 O 2-Me-Phenyl 426 3 O 2-Me-Phenyl 427 4 O 2-Me-Phenyl 428 1 S 2-Me-Phenyl 429 2 S 2-Me-Phenyl 430 3 S 2-Me-Phenyl 431 4 S 2-Me-Phenyl 432 1 SO 2-Me-Phenyl 433 2 SO 2-Me-Phenyl 434 3 SO 2-Me-Phenyl 435 4 SO 2-Me-Phenyl 436 1 SO.sub.2 2-Me-Phenyl 437 2 SO.sub.2 2-Me-Phenyl 438 3 SO.sub.2 2-Me-Phenyl 439 4 SO.sub.2 2-Me-Phenyl 440 1 O 4-Me-Phenyl 441 2 O 4-Me-Phenyl 442 3 O 4-Me-Phenyl 443 4 O 4-Me-Phenyl 444 1 S 4-Me-Phenyl 445 2 S 4-Me-Phenyl 446 3 S 4-Me-Phenyl 447 4 S 4-Me-Phenyl 448 1 SO 4-Me-Phenyl 449 2 SO 4-Me-Phenyl 450 3 SO 4-Me-Phenyl 451 4 SO 4-Me-Phenyl 452 1 SO.sub.2 4-Me-Phenyl 453 2 SO.sub.2 4-Me-Phenyl 454 3 SO.sub.2 4-Me-Phenyl 455 4 SO.sub.2 4-Me-Phenyl 456 1 O 3-F-Phenyl 457 2 O 3-F-Phenyl 458 3 O 3-F-Phenyl 459 4 O 3-F-Phenyl 460 1 S 3-F-Phenyl 461 2 S 3-F-Phenyl 462 3 S 3-F-Phenyl 463 4 S 3-F-Phenyl 464 1 SO 3-F-Phenyl 465 2 SO 3-F-Phenyl 466 3 SO 3-F-Phenyl 467 4 SO 3-F-Phenyl 468 1 SO.sub.2 3-F-Phenyl 469 2 SO.sub.2 3-F-Phenyl 470 3 SO.sub.2 3-F-Phenyl 471 4 SO.sub.2 3-F-Phenyl 472 1 O 2-Cl-Phenyl 473 2 O 2-Cl-Phenyl 474 3 O 2-Cl-Phenyl 475 4 O 2-Cl-Phenyl 476 1 S 2-Cl-Phenyl 477 2 S 2-Cl-Phenyl 478 3 S 2-Cl-Phenyl 479 4 S 2-Cl-Phenyl 480 1 SO 2-Cl-Phenyl 481 2 SO 2-Cl-Phenyl 482 3 SO 2-Cl-Phenyl 483 4 SO 2-Cl-Phenyl 484 1 SO.sub.2 2-Cl-Phenyl 485 2 SO.sub.2 2-Cl-Phenyl 486 3 SO.sub.2 2-Cl-Phenyl 487 4 SO.sub.2 2-Cl-Phenyl 488 1 O 4-Cl-Phenyl 489 2 O 4-Cl-Phenyl 490 3 O 4-Cl-Phenyl 491 4 O 4-Cl-Phenyl 492 1 S 4-Cl-Phenyl 493 2 S 4-Cl-Phenyl 494 3 S 4-Cl-Phenyl 495 4 S 4-Cl-Phenyl 496 1 SO 4-Cl-Phenyl 497 2 SO 4-Cl-Phenyl 498 3 SO 4-Cl-Phenyl 499 4 SO 4-Cl-Phenyl 500 1 SO.sub.2 4-Cl-Phenyl 501 2 SO.sub.2 4-Cl-Phenyl 502 3 SO.sub.2 4-Cl-Phenyl 503 4 SO.sub.2 4-Cl-Phenyl 504 1 O 3-Br-Phenyl 505 2 O 3-Br-Phenyl 506 3 O 3-Br-Phenyl 507 4 O 3-Br-Phenyl 508 1 S 3-Br-Phenyl 509 2 S 3-Br-Phenyl 510 3 S 3-Br-Phenyl 511 4 S 3-Br-Phenyl 512 1 SO 3-Br-Phenyl 513 2 SO 3-Br-Phenyl 514 3 SO 3-Br-Phenyl 515 4 SO 3-Br-Phenyl 516 1 SO.sub.2 3-Br-Phenyl 517 2 SO.sub.2 3-Br-Phenyl 518 3 SO.sub.2 3-Br-Phenyl 519 4 SO.sub.2 3-Br-Phenyl 520 1 O 2-CF.sub.3-Phenyl 521 2 O 2-CF.sub.3-Phenyl 522 3 O 2-CF.sub.3-Phenyl 523 4 O 2-CF.sub.3-Phenyl 524 1 S 2-CF.sub.3-Phenyl 525 2 S 2-CF.sub.3-Phenyl 526 3 S 2-CF.sub.3-Phenyl 527 4 S 2-CF.sub.3-Phenyl 528 1 SO 2-CF.sub.3-Phenyl 529 2 SO 2-CF.sub.3-Phenyl 530 3 SO 2-CF.sub.3-Phenyl 531 4 SO 2-CF.sub.3-Phenyl 532 1 SO.sub.2 2-CF.sub.3-Phenyl 533 2 SO.sub.2 2-CF.sub.3-Phenyl 534 3 SO.sub.2 2-CF.sub.3-Phenyl 535 4 SO.sub.2 2-CF.sub.3-Phenyl 536 1 O 4-CF.sub.3-Phenyl 537 2 O 4-CF.sub.3-Phenyl 538 3 O 4-CF.sub.3-Phenyl 539 4 O 4-CF.sub.3-Phenyl 540 1 S 4-CF.sub.3-Phenyl 541 2 S 4-CF.sub.3-Phenyl 542 3 S 4-CF.sub.3-Phenyl 543 4 S 4-CF.sub.3-Phenyl 544 1 SO 4-CF.sub.3-Phenyl 545 2 SO 4-CF.sub.3-Phenyl 546 3 SO 4-CF.sub.3-Phenyl 547 4 SO 4-CF.sub.3-Phenyl 548 1 SO.sub.2 4-CF.sub.3-Phenyl 549 2 SO.sub.2 4-CF.sub.3-Phenyl 550 3 SO.sub.2 4-CF.sub.3-Phenyl 551 4 SO.sub.2 4-CF.sub.3-Phenyl 552 1 O 3-iPr-Phenyl 553 2 O 3-iPr-Phenyl 554 3 O 3-iPr-Phenyl 555 4 O 3-iPr-Phenyl 556 1 S 3-iPr-Phenyl 557 2 S 3-iPr-Phenyl 558 3 S 3-iPr-Phenyl 559 4 S 3-iPr-Phenyl 560 1 SO 3-iPr-Phenyl 561 2 SO 3-iPr-Phenyl 562 3 SO 3-iPr-Phenyl 563 4 SO 3-iPr-Phenyl 564 1 SO.sub.2 3-iPr-Phenyl 565 2 SO.sub.2 3-iPr-Phenyl 566 3 SO.sub.2 3-iPr-Phenyl 567 4 SO.sub.2 3-iPr-Phenyl 568 1 O 4-NH.sub.2-Phenyl 569 2 O 4-NH.sub.2-Phenyl 570 3 O 4-NH.sub.2-Phenyl 571 4 O 4-NH.sub.2-Phenyl 572 1 S 4-NH.sub.2-Phenyl 573 2 S 4-NH.sub.2-Phenyl 574 3 S 4-NH.sub.2-Phenyl 575 4 S 4-NH.sub.2-Phenyl 576 1 SO 4-NH.sub.2-Phenyl 577 2 SO 4-NH.sub.2-Phenyl 578 3 SO 4-NH.sub.2-Phenyl 579 4 SO 4-NH.sub.2-Phenyl 580 1 SO.sub.2 4-NH.sub.2-Phenyl 581 2 SO.sub.2 4-NH.sub.2-Phenyl 582 3 SO.sub.2 4-NH.sub.2-Phenyl 583 4 SO.sub.2 4-NH.sub.2-Phenyl 584 1 O 2-NH.sub.2-Phenyl 585 2 O 2-NH.sub.2-Phenyl 586 3 O 2-NH.sub.2-Phenyl 587 4 O 2-NH.sub.2-Phenyl 588 1 S 2-NH.sub.2-Phenyl 589 2 S 2-NH.sub.2-Phenyl 590 3 S 2-NH.sub.2-Phenyl 591 1 S 2-NH.sub.2-Phenyl 592 2 SO 2-NH.sub.2-Phenyl 593 3 SO 2-NH.sub.2-Phenyl 594 4 SO 2-NH.sub.2-Phenyl 595 1 SO 2-NH.sub.2-Phenyl 596 2 SO.sub.2 2-NH.sub.2-Phenyl 597 3 SO.sub.2 2-NH.sub.2-Phenyl 598 4 SO.sub.2 2-NH.sub.2-Phenyl 599 1 O 2,6-di-Me-Phenyl 600 2 O 2,6-di-Me-Phenyl 601 3 O 2,6-di-Me-Phenyl 602 4 O 2,6-di-Me-Phenyl 603 1 S 2,6-di-Me-Phenyl 604 2 S 2,6-di-Me-Phenyl 605 3 S 2,6-di-Me-Phenyl 606 4 S 2,6-di-Me-Phenyl 607 1 SO 2,6-di-Me-Phenyl 608 2 SO 2,6-di-Me-Phenyl 609 3 SO 2,6-di-Me-Phenyl 610 4 SO 2,6-di-Me-Phenyl 611 1 SO.sub.2 2,6-di-Me-Phenyl 612 2 SO.sub.2 2,6-di-Me-Phenyl 613 3 SO.sub.2 2,6-di-Me-Phenyl 614 4 SO.sub.2 2,6-di-Me-Phenyl 615 1 O 2-Ph-Phenyl 616 2 O 2-Ph-Phenyl 617 3 O 2-Ph-Phenyl 618 4 O 2-Ph-Phenyl 619 1 S 2-Ph-Phenyl 620 2 S 2-Ph-Phenyl 621 3 S 2-Ph-Phenyl 622 4 S 2-Ph-Phenyl 623 1 SO 2-Ph-Phenyl 624 2 SO 2-Ph-Phenyl 625 3 SO 2-Ph-Phenyl 626 4 SO 2-Ph-Phenyl 627 1 SO.sub.2 2-Ph-Phenyl 628 2 SO.sub.2 2-Ph-Phenyl 629 3 SO.sub.2 2-Ph-Phenyl 630 4 SO.sub.2 2-Ph-Phenyl 631 1 O 4-Ph-Phenyl 632 2 O 4-Ph-Phenyl 633 3 O 4-Ph-Phenyl 634 4 O 4-Ph-Phenyl 635 1 S 4-Ph-Phenyl 636 2 S 4-Ph-Phenyl 637 3 S 4-Ph-Phenyl 638 4 S 4-Ph-Phenyl 639 1 SO 4-Ph-Phenyl 640 2 SO 4-Ph-Phenyl 641 3 SO 4-Ph-Phenyl 642 4 SO 4-Ph-Phenyl 643 1 SO.sub.2 4-Ph-Phenyl 644 2 SO.sub.2 4-Ph-Phenyl 645 3 SO.sub.2 4-Ph-Phenyl 646 4 SO.sub.2 4-Ph-Phenyl 647 1 O 3-morpholino-phenyl 648 2 O 3-morpholino-phenyl 649 3 O 3-morpholino-phenyl 650 4 O 3-morpholino-phenyl 651 1 S 3-morpholino-phenyl 652 2 S 3-morpholino-phenyl 653 3 S 3-morpholino-phenyl 654 4 S 3-morpholino-phenyl 655 1 SO 3-morpholino-phenyl 656 2 SO 3-morpholino-phenyl 657 3 SO 3-morpholino-phenyl 658 4 SO 3-morpholino-phenyl 659 1 SO.sub.2 3-morpholino-phenyl 660 2 SO.sub.2 3-morpholino-phenyl 661 3 SO.sub.2 3-morpholino-phenyl 662 4 SO.sub.2 3-morpholino-phenyl 663 1 S 4-morpholino-phenyl 664 2 S 4-morpholino-phenyl 665 3 S 4-morpholino-phenyl 667 4 S 4-morpholino-phenyl 668 1 SO.sub.2 4-morpholino-phenyl 669 2 SO.sub.2 4-morpholino-phenyl 670 3 SO.sub.2 4-morpholino-phenyl 671 4 SO.sub.2 4-morpholino-phenyl 672 1 O naphthylen-2-yl 673 2 O naphthylen-2-yl 674 3 O naphthylen-2-yl 675 4 O naphthylen-2-yl 676 1 S naphthylen-2-yl 678 2 S naphthylen-2-yl 679 3 S naphthylen-2-yl 680 4 S naphthylen-2-yl 681 1 SO naphthylen-2-yl 682 2 SO naphthylen-2-yl 683 3 SO naphthylen-2-yl 684 4 SO naphthylen-2-yl 685 1 SO.sub.2 naphthylen-2-yl 686 2 SO.sub.2 naphthylen-2-yl 687 3 SO.sub.2 naphthylen-2-yl 688 4 SO.sub.2 naphthylen-2-yl

    [2050] Exemplary embodiments include compounds having the formula (XXXXVI)

    ##STR00450##

    [2051] or a pharmaceutically acceptable salt form thereof defined herein below in Table 29.

    TABLE-US-00029 Entry n X R.sup.3 1 1 O Phenyl 2 2 O Phenyl 3 3 O Phenyl 4 4 O Phenyl 5 1 S Phenyl 6 2 S Phenyl 7 3 S Phenyl 8 4 S Phenyl 9 1 SO Phenyl 10 2 SO Phenyl 11 3 SO Phenyl 12 4 SO Phenyl 13 1 SO.sub.2 Phenyl 14 2 SO.sub.2 Phenyl 15 3 SO.sub.2 Phenyl 16 4 SO.sub.2 Phenyl 17 1 O 3-OH-Phenyl 18 2 O 3-OH-Phenyl 19 3 O 3-OH-Phenyl 20 4 O 3-OH-Phenyl 21 1 S 3-OH-Phenyl 22 2 S 3-OH-Phenyl 23 3 S 3-OH-Phenyl 24 4 S 3-OH-Phenyl 25 1 SO 3-OH-Phenyl 26 2 SO 3-OH-Phenyl 27 3 SO 3-OH-Phenyl 28 4 SO 3-OH-Phenyl 29 1 SO.sub.2 3-OH-Phenyl 30 2 SO.sub.2 3-OH-Phenyl 31 3 SO.sub.2 3-OH-Phenyl 32 4 SO.sub.2 3-OH-Phenyl 33 1 O 4-NO.sub.2-Phenyl 34 2 O 4-NO.sub.2-Phenyl 35 3 O 4-NO.sub.2-Phenyl 36 4 O 4-NO.sub.2-Phenyl 37 1 S 4-NO.sub.2-Phenyl 38 2 S 4-NO.sub.2-Phenyl 39 3 S 4-NO.sub.2-Phenyl 40 4 S 4-NO.sub.2-Phenyl 41 1 SO 4-NO.sub.2-Phenyl 42 2 SO 4-NO.sub.2-Phenyl 43 3 SO 4-NO.sub.2-Phenyl 44 4 SO 4-NO.sub.2-Phenyl 45 1 SO.sub.2 4-NO.sub.2-Phenyl 46 2 SO.sub.2 4-NO.sub.2-Phenyl 47 3 SO.sub.2 4-NO.sub.2-Phenyl 48 4 SO.sub.2 4-NO.sub.2-Phenyl 49 1 O 3-OMe-Phenyl 50 2 O 3-OMe-Phenyl 51 3 O 3-OMe-Phenyl 52 4 O 3-OMe-Phenyl 53 1 S 3-OMe-Phenyl 54 2 S 3-OMe-Phenyl 55 3 S 3-OMe-Phenyl 56 4 S 3-OMe-Phenyl 57 1 SO 3-OMe-Phenyl 58 2 SO 3-OMe-Phenyl 59 3 SO 3-OMe-Phenyl 60 4 SO 3-OMe-Phenyl 61 1 SO.sub.2 3-OMe-Phenyl 62 2 SO.sub.2 3-OMe-Phenyl 63 3 SO.sub.2 3-OMe-Phenyl 64 4 SO.sub.2 3-OMe-Phenyl 65 1 O 4-CN-Phenyl 66 2 O 4-CN-Phenyl 67 3 O 4-CN-Phenyl 68 4 O 4-CN-Phenyl 69 1 S 4-CN-Phenyl 70 2 S 4-CN-Phenyl 71 3 S 4-CN-Phenyl 72 4 S 4-CN-Phenyl 73 1 SO 4-CN-Phenyl 74 2 SO 4-CN-Phenyl 75 3 SO 4-CN-Phenyl 76 4 SO 4-CN-Phenyl 77 1 SO.sub.2 4-CN-Phenyl 78 2 SO.sub.2 4-CN-Phenyl 79 3 SO.sub.2 4-CN-Phenyl 80 4 SO.sub.2 4-CN-Phenyl 81 1 O 2-CN-Phenyl 82 2 O 2-CN-Phenyl 83 3 O 2-CN-Phenyl 84 4 O 2-CN-Phenyl 85 1 S 2-CN-Phenyl 86 2 S 2-CN-Phenyl 87 3 S 2-CN-Phenyl 88 4 S 2-CN-Phenyl 89 1 SO 2-CN-Phenyl 90 2 SO 2-CN-Phenyl 91 3 SO 2-CN-Phenyl 92 4 SO 2-CN-Phenyl 93 1 SO.sub.2 2-CN-Phenyl 94 2 SO.sub.2 2-CN-Phenyl 95 3 SO.sub.2 2-CN-Phenyl 96 4 SO.sub.2 2-CN-Phenyl 97 1 O 3-Me-Phenyl 98 2 O 3-Me-Phenyl 99 3 O 3-Me-Phenyl 100 4 O 3-Me-Phenyl 101 1 S 3-Me-Phenyl 102 2 S 3-Me-Phenyl 103 3 S 3-Me-Phenyl 104 4 S 3-Me-Phenyl 105 1 SO 3-Me-Phenyl 106 2 SO 3-Me-Phenyl 107 3 SO 3-Me-Phenyl 108 4 SO 3-Me-Phenyl 109 1 SO.sub.2 3-Me-Phenyl 110 2 SO.sub.2 3-Me-Phenyl 111 3 SO.sub.2 3-Me-Phenyl 112 4 SO.sub.2 3-Me-Phenyl 113 1 O 2-F-Phenyl 114 2 O 2-F-Phenyl 115 3 O 2-F-Phenyl 116 4 O 2-F-Phenyl 117 1 S 2-F-Phenyl 118 2 S 2-F-Phenyl 119 3 S 2-F-Phenyl 120 4 S 2-F-Phenyl 121 1 SO 2-F-Phenyl 122 2 SO 2-F-Phenyl 123 3 SO 2-F-Phenyl 124 4 SO 2-F-Phenyl 125 1 SO.sub.2 2-F-Phenyl 126 2 SO.sub.2 2-F-Phenyl 127 3 SO.sub.2 2-F-Phenyl 128 4 SO.sub.2 2-F-Phenyl 129 1 O 4-F-Phenyl 130 2 O 4-F-Phenyl 131 3 O 4-F-Phenyl 132 4 O 4-F-Phenyl 133 1 S 4-F-Phenyl 134 2 S 4-F-Phenyl 135 3 S 4-F-Phenyl 136 4 S 4-F-Phenyl 137 1 SO 4-F-Phenyl 138 2 SO 4-F-Phenyl 139 3 SO 4-F-Phenyl 140 4 SO 4-F-Phenyl 141 1 SO.sub.2 4-F-Phenyl 142 2 SO.sub.2 4-F-Phenyl 143 3 SO.sub.2 4-F-Phenyl 144 4 SO.sub.2 4-F-Phenyl 145 1 O 3-Cl-Phenyl 146 2 O 3-Cl-Phenyl 147 3 O 3-Cl-Phenyl 148 4 O 3-Cl-Phenyl 149 1 S 3-Cl-Phenyl 150 2 S 3-Cl-Phenyl 151 3 S 3-Cl-Phenyl 152 4 S 3-Cl-Phenyl 153 1 SO 3-Cl-Phenyl 154 2 SO 3-Cl-Phenyl 155 3 SO 3-Cl-Phenyl 156 4 SO 3-Cl-Phenyl 157 1 SO.sub.2 3-Cl-Phenyl 158 2 SO.sub.2 3-Cl-Phenyl 159 3 SO.sub.2 3-Cl-Phenyl 160 4 SO.sub.2 3-Cl-Phenyl 161 1 O 2-Br-Phenyl 162 2 O 2-Br-Phenyl 163 3 O 2-Br-Phenyl 164 4 O 2-Br-Phenyl 165 1 S 2-Br-Phenyl 166 2 S 2-Br-Phenyl 167 3 S 2-Br-Phenyl 168 4 S 2-Br-Phenyl 169 1 SO 2-Br-Phenyl 170 2 SO 2-Br-Phenyl 171 3 SO 2-Br-Phenyl 172 4 SO 2-Br-Phenyl 173 1 SO.sub.2 2-Br-Phenyl 174 2 SO.sub.2 2-Br-Phenyl 175 3 SO.sub.2 2-Br-Phenyl 176 4 SO.sub.2 2-Br-Phenyl 177 1 O 4-Br-Phenyl 178 2 O 4-Br-Phenyl 179 3 O 4-Br-Phenyl 180 4 O 4-Br-Phenyl 181 1 S 4-Br-Phenyl 182 2 S 4-Br-Phenyl 183 3 S 4-Br-Phenyl 184 4 S 4-Br-Phenyl 185 1 SO 4-Br-Phenyl 186 2 SO 4-Br-Phenyl 187 3 SO 4-Br-Phenyl 188 4 SO 4-Br-Phenyl 189 1 SO.sub.2 4-Br-Phenyl 190 2 SO.sub.2 4-Br-Phenyl 191 3 SO.sub.2 4-Br-Phenyl 192 4 SO.sub.2 4-Br-Phenyl 193 1 O 3-CF.sub.3-Phenyl 194 2 O 3-CF.sub.3-Phenyl 195 3 O 3-CF.sub.3-Phenyl 196 4 O 3-CF.sub.3-Phenyl 197 1 S 3-CF.sub.3-Phenyl 198 2 S 3-CF.sub.3-Phenyl 199 3 S 3-CF.sub.3-Phenyl 200 4 S 3-CF.sub.3-Phenyl 201 1 SO 3-CF.sub.3-Phenyl 202 2 SO 3-CF.sub.3-Phenyl 203 3 SO 3-CF.sub.3-Phenyl 204 4 SO 3-CF.sub.3-Phenyl 205 1 SO.sub.2 3-CF.sub.3-Phenyl 206 2 SO.sub.2 3-CF.sub.3-Phenyl 207 3 SO.sub.2 3-CF.sub.3-Phenyl 208 4 SO.sub.2 3-CF.sub.3-Phenyl 209 1 O 2-iPr-Phenyl 210 2 O 2-iPr-Phenyl 211 3 O 2-iPr-Phenyl 212 4 O 2-iPr-Phenyl 213 1 S 2-iPr-Phenyl 214 2 S 2-iPr-Phenyl 215 3 S 2-iPr-Phenyl 216 4 S 2-iPr-Phenyl 217 1 SO 2-iPr-Phenyl 218 2 SO 2-iPr-Phenyl 219 3 SO 2-iPr-Phenyl 220 4 SO 2-iPr-Phenyl 221 1 SO.sub.2 2-iPr-Phenyl 222 2 SO.sub.2 2-iPr-Phenyl 223 3 SO.sub.2 2-iPr-Phenyl 224 4 SO.sub.2 2-iPr-Phenyl 225 1 O 4-iPr-Phenyl 226 2 O 4-iPr-Phenyl 227 3 O 4-iPr-Phenyl 228 4 O 4-iPr-Phenyl 229 1 S 4-iPr-Phenyl 230 2 S 4-iPr-Phenyl 231 3 S 4-iPr-Phenyl 232 4 S 4-iPr-Phenyl 233 1 SO 4-iPr-Phenyl 234 2 SO 4-iPr-Phenyl 235 3 SO 4-iPr-Phenyl 236 4 SO 4-iPr-Phenyl 237 1 SO.sub.2 4-iPr-Phenyl 238 2 SO.sub.2 4-iPr-Phenyl 239 3 SO.sub.2 4-iPr-Phenyl 240 4 SO.sub.2 4-iPr-Phenyl 241 1 O 3-NH.sub.2-Phenyl 242 2 O 3-NH.sub.2-Phenyl 243 3 O 3-NH.sub.2-Phenyl 244 4 O 3-NH.sub.2-Phenyl 245 1 S 3-NH.sub.2-Phenyl 246 2 S 3-NH.sub.2-Phenyl 247 3 S 3-NH.sub.2-Phenyl 248 1 S 3-NH.sub.2-Phenyl 249 2 SO 3-NH.sub.2-Phenyl 250 3 SO 3-NH.sub.2-Phenyl 251 4 SO 3-NH.sub.2-Phenyl 252 1 SO 3-NH.sub.2-Phenyl 253 2 SO.sub.2 3-NH.sub.2-Phenyl 254 3 SO.sub.2 3-NH.sub.2-Phenyl 255 4 SO.sub.2 3-NH.sub.2-Phenyl 256 1 O 2,4-di-Me-Phenyl 257 2 O 2,4-di-Me-Phenyl 258 3 O 2,4-di-Me-Phenyl 259 4 O 2,4-di-Me-Phenyl 260 1 S 2,4-di-Me-Phenyl 261 2 S 2,4-di-Me-Phenyl 262 3 S 2,4-di-Me-Phenyl 263 4 S 2,4-di-Me-Phenyl 264 1 SO 2,4-di-Me-Phenyl 265 2 SO 2,4-di-Me-Phenyl 266 3 SO 2,4-di-Me-Phenyl 267 4 SO 2,4-di-Me-Phenyl 268 1 SO.sub.2 2,4-di-Me-Phenyl 269 2 SO.sub.2 2,4-di-Me-Phenyl 270 3 SO.sub.2 2,4-di-Me-Phenyl 271 4 SO.sub.2 2,4-di-Me-Phenyl 272 1 O 2,6-di-iPr-Phenyl 273 2 O 2,6-di-iPr-Phenyl 274 3 O 2,6-di-iPr-Phenyl 275 4 O 2,6-di-iPr-Phenyl 276 1 S 2,6-di-iPr-Phenyl 277 2 S 2,6-di-iPr-Phenyl 278 3 S 2,6-di-iPr-Phenyl 279 4 S 2,6-di-iPr-Phenyl 280 1 SO 2,6-di-iPr-Phenyl 281 2 SO 2,6-di-iPr-Phenyl 282 3 SO 2,6-di-iPr-Phenyl 283 4 SO 2,6-di-iPr-Phenyl 284 1 SO.sub.2 2,6-di-iPr-Phenyl 285 2 SO.sub.2 2,6-di-iPr-Phenyl 286 3 SO.sub.2 2,6-di-iPr-Phenyl 287 4 SO.sub.2 2,6-di-iPr-Phenyl 288 1 O 3-Ph-Phenyl 289 2 O 3-Ph-Phenyl 290 3 O 3-Ph-Phenyl 291 4 O 3-Ph-Phenyl 292 1 S 3-Ph-Phenyl 293 2 S 3-Ph-Phenyl 294 3 S 3-Ph-Phenyl 295 4 S 3-Ph-Phenyl 296 1 SO 3-Ph-Phenyl 297 2 SO 3-Ph-Phenyl 298 3 SO 3-Ph-Phenyl 299 4 SO 3-Ph-Phenyl 300 1 SO.sub.2 3-Ph-Phenyl 301 2 SO.sub.2 3-Ph-Phenyl 302 3 SO.sub.2 3-Ph-Phenyl 303 4 SO.sub.2 3-Ph-Phenyl 304 1 O 2-morpholino-phenyl 305 2 O 2-morpholino-phenyl 306 3 O 2-morpholino-phenyl 307 4 O 2-morpholino-phenyl 308 1 S 2-morpholino-phenyl 309 2 S 2-morpholino-phenyl 310 3 S 2-morpholino-phenyl 311 4 S 2-morpholino-phenyl 312 1 SO 2-morpholino-phenyl 313 2 SO 2-morpholino-phenyl 314 3 SO 2-morpholino-phenyl 315 4 SO 2-morpholino-phenyl 316 1 SO.sub.2 2-morpholino-phenyl 317 2 SO.sub.2 2-morpholino-phenyl 318 3 SO.sub.2 2-morpholino-phenyl 319 4 SO.sub.2 2-morpholino-phenyl 320 1 O 4-morpholino-phenyl 321 2 O 4-morpholino-phenyl 322 3 O 4-morpholino-phenyl 323 4 O 4-morpholino-phenyl 324 1 SO 4-morpholino-phenyl 325 2 SO 4-morpholino-phenyl 326 3 SO 4-morpholino-phenyl 327 4 SO 4-morpholino-phenyl 328 1 O naphthylen-1-yl 329 2 O naphthylen-1-yl 330 3 O naphthylen-1-yl 331 4 O naphthylen-1-yl 332 1 S naphthylen-1-yl 333 2 S naphthylen-1-yl 334 3 S naphthylen-1-yl 335 4 S naphthylen-1-yl 336 1 SO naphthylen-1-yl 337 2 SO naphthylen-1-yl 338 3 SO naphthylen-1-yl 339 4 SO naphthylen-1-yl 340 1 SO.sub.2 naphthylen-1-yl 341 2 SO.sub.2 naphthylen-1-yl 342 3 SO.sub.2 naphthylen-1-yl 343 4 SO.sub.2 naphthylen-1-yl 344 1 O 4-OH-Phenyl 345 2 O 4-OH-Phenyl 346 3 O 4-OH-Phenyl 347 4 O 4-OH-Phenyl 348 1 S 4-OH-Phenyl 349 2 S 4-OH-Phenyl 350 3 S 4-OH-Phenyl 351 4 S 4-OH-Phenyl 352 1 SO 4-OH-Phenyl 353 2 SO 4-OH-Phenyl 354 3 SO 4-OH-Phenyl 355 4 SO 4-OH-Phenyl 356 1 SO.sub.2 4-OH-Phenyl 357 2 SO.sub.2 4-OH-Phenyl 358 3 SO.sub.2 4-OH-Phenyl 359 4 SO.sub.2 4-OH-Phenyl 360 1 O 2-OH-Phenyl 361 2 O 2-OH-Phenyl 362 3 O 2-OH-Phenyl 363 4 O 2-OH-Phenyl 364 1 S 2-OH-Phenyl 365 2 S 2-OH-Phenyl 366 3 S 2-OH-Phenyl 367 4 S 2-OH-Phenyl 368 1 SO 2-OH-Phenyl 369 2 SO 2-OH-Phenyl 370 3 SO 2-OH-Phenyl 371 4 SO 2-OH-Phenyl 372 1 SO.sub.2 2-OH-Phenyl 373 2 SO.sub.2 2-OH-Phenyl 374 3 SO.sub.2 2-OH-Phenyl 375 4 SO.sub.2 2-OH-Phenyl 376 1 O 4-OMe-Phenyl 377 2 O 4-OMe-Phenyl 378 3 O 4-OMe-Phenyl 379 4 O 4-OMe-Phenyl 380 1 S 4-OMe-Phenyl 381 2 S 4-OMe-Phenyl 382 3 S 4-OMe-Phenyl 383 4 S 4-OMe-Phenyl 384 1 SO 4-OMe-Phenyl 385 2 SO 4-OMe-Phenyl 386 3 SO 4-OMe-Phenyl 387 4 SO 4-OMe-Phenyl 388 1 SO.sub.2 4-OMe-Phenyl 389 2 SO.sub.2 4-OMe-Phenyl 390 3 SO.sub.2 4-OMe-Phenyl 391 4 SO.sub.2 4-OMe-Phenyl 392 1 O 2-OMe-Phenyl 393 2 O 2-OMe-Phenyl 394 3 O 2-OMe-Phenyl 395 4 O 2-OMe-Phenyl 396 1 S 2-OMe-Phenyl 397 2 S 2-OMe-Phenyl 398 3 S 2-OMe-Phenyl 399 4 S 2-OMe-Phenyl 400 1 SO 2-OMe-Phenyl 401 2 SO 2-OMe-Phenyl 402 3 SO 2-OMe-Phenyl 403 4 SO 2-OMe-Phenyl 404 1 SO.sub.2 2-OMe-Phenyl 405 2 SO.sub.2 2-OMe-Phenyl 406 3 SO.sub.2 2-OMe-Phenyl 407 4 SO.sub.2 2-OMe-Phenyl 408 1 O 3-CN-Phenyl 409 2 O 3-CN-Phenyl 410 3 O 3-CN-Phenyl 411 4 O 3-CN-Phenyl 412 1 S 3-CN-Phenyl 413 2 S 3-CN-Phenyl 414 3 S 3-CN-Phenyl 415 4 S 3-CN-Phenyl 416 1 SO 3-CN-Phenyl 417 2 SO 3-CN-Phenyl 418 3 SO 3-CN-Phenyl 419 4 SO 3-CN-Phenyl 420 1 SO.sub.2 3-CN-Phenyl 421 2 SO.sub.2 3-CN-Phenyl 422 3 SO.sub.2 3-CN-Phenyl 423 4 SO.sub.2 3-CN-Phenyl 424 1 O 2-Me-Phenyl 425 2 O 2-Me-Phenyl 426 3 O 2-Me-Phenyl 427 4 O 2-Me-Phenyl 428 1 S 2-Me-Phenyl 429 2 S 2-Me-Phenyl 430 3 S 2-Me-Phenyl 431 4 S 2-Me-Phenyl 432 1 SO 2-Me-Phenyl 433 2 SO 2-Me-Phenyl 434 3 SO 2-Me-Phenyl 435 4 SO 2-Me-Phenyl 436 1 SO.sub.2 2-Me-Phenyl 437 2 SO.sub.2 2-Me-Phenyl 438 3 SO.sub.2 2-Me-Phenyl 439 4 SO.sub.2 2-Me-Phenyl 440 1 O 4-Me-Phenyl 441 2 O 4-Me-Phenyl 442 3 O 4-Me-Phenyl 443 4 O 4-Me-Phenyl 444 1 S 4-Me-Phenyl 445 2 S 4-Me-Phenyl 446 3 S 4-Me-Phenyl 447 4 S 4-Me-Phenyl 448 1 SO 4-Me-Phenyl 449 2 SO 4-Me-Phenyl 450 3 SO 4-Me-Phenyl 451 4 SO 4-Me-Phenyl 452 1 SO.sub.2 4-Me-Phenyl 453 2 SO.sub.2 4-Me-Phenyl 454 3 SO.sub.2 4-Me-Phenyl 455 4 SO.sub.2 4-Me-Phenyl 456 1 O 3-F-Phenyl 457 2 O 3-F-Phenyl 458 3 O 3-F-Phenyl 459 4 O 3-F-Phenyl 460 1 S 3-F-Phenyl 461 2 S 3-F-Phenyl 462 3 S 3-F-Phenyl 463 4 S 3-F-Phenyl 464 1 SO 3-F-Phenyl 465 2 SO 3-F-Phenyl 466 3 SO 3-F-Phenyl 467 4 SO 3-F-Phenyl 468 1 SO.sub.2 3-F-Phenyl 469 2 SO.sub.2 3-F-Phenyl 470 3 SO.sub.2 3-F-Phenyl 471 4 SO.sub.2 3-F-Phenyl 472 1 O 2-Cl-Phenyl 473 2 O 2-Cl-Phenyl 474 3 O 2-Cl-Phenyl 475 4 O 2-Cl-Phenyl 476 1 S 2-Cl-Phenyl 477 2 S 2-Cl-Phenyl 478 3 S 2-Cl-Phenyl 479 4 S 2-Cl-Phenyl 480 1 SO 2-Cl-Phenyl 481 2 SO 2-Cl-Phenyl 482 3 SO 2-Cl-Phenyl 483 4 SO 2-Cl-Phenyl 484 1 SO.sub.2 2-Cl-Phenyl 485 2 SO.sub.2 2-Cl-Phenyl 486 3 SO.sub.2 2-Cl-Phenyl 487 4 SO.sub.2 2-Cl-Phenyl 488 1 O 4-Cl-Phenyl 489 2 O 4-Cl-Phenyl 490 3 O 4-Cl-Phenyl 491 4 O 4-Cl-Phenyl 492 1 S 4-Cl-Phenyl 493 2 S 4-Cl-Phenyl 494 3 S 4-Cl-Phenyl 495 4 S 4-Cl-Phenyl 496 1 SO 4-Cl-Phenyl 497 2 SO 4-Cl-Phenyl 498 3 SO 4-Cl-Phenyl 499 4 SO 4-Cl-Phenyl 500 1 SO.sub.2 4-Cl-Phenyl 501 2 SO.sub.2 4-Cl-Phenyl 502 3 SO.sub.2 4-Cl-Phenyl 503 4 SO.sub.2 4-Cl-Phenyl 504 1 O 3-Br-Phenyl 505 2 O 3-Br-Phenyl 506 3 O 3-Br-Phenyl 507 4 O 3-Br-Phenyl 508 1 S 3-Br-Phenyl 509 2 S 3-Br-Phenyl 510 3 S 3-Br-Phenyl 511 4 S 3-Br-Phenyl 512 1 SO 3-Br-Phenyl 513 2 SO 3-Br-Phenyl 514 3 SO 3-Br-Phenyl 515 4 SO 3-Br-Phenyl 516 1 SO.sub.2 3-Br-Phenyl 517 2 SO.sub.2 3-Br-Phenyl 518 3 SO.sub.2 3-Br-Phenyl 519 4 SO.sub.2 3-Br-Phenyl 520 1 O 2-CF.sub.3-Phenyl 521 2 O 2-CF.sub.3-Phenyl 522 3 O 2-CF.sub.3-Phenyl 523 4 O 2-CF.sub.3-Phenyl 524 1 S 2-CF.sub.3-Phenyl 525 2 S 2-CF.sub.3-Phenyl 526 3 S 2-CF.sub.3-Phenyl 527 4 S 2-CF.sub.3-Phenyl 528 1 SO 2-CF.sub.3-Phenyl 529 2 SO 2-CF.sub.3-Phenyl 530 3 SO 2-CF.sub.3-Phenyl 531 4 SO 2-CF.sub.3-Phenyl 532 1 SO.sub.2 2-CF.sub.3-Phenyl 533 2 SO.sub.2 2-CF.sub.3-Phenyl 534 3 SO.sub.2 2-CF.sub.3-Phenyl 535 4 SO.sub.2 2-CF.sub.3-Phenyl 536 1 O 4-CF.sub.3-Phenyl 537 2 O 4-CF.sub.3-Phenyl 538 3 O 4-CF.sub.3-Phenyl 539 4 O 4-CF.sub.3-Phenyl 540 1 S 4-CF.sub.3-Phenyl 541 2 S 4-CF.sub.3-Phenyl 542 3 S 4-CF.sub.3-Phenyl 543 4 S 4-CF.sub.3-Phenyl 544 1 SO 4-CF.sub.3-Phenyl 545 2 SO 4-CF.sub.3-Phenyl 546 3 SO 4-CF.sub.3-Phenyl 547 4 SO 3-CF.sub.3-Phenyl 548 1 SO.sub.2 4-CF.sub.3-Phenyl 549 2 SO.sub.2 4-CF.sub.3-Phenyl 550 3 SO.sub.2 4-CF.sub.3-Phenyl 551 4 SO.sub.2 4-CF.sub.3-Phenyl 552 1 O 3-iPr-Phenyl 553 2 O 3-iPr-Phenyl 554 3 O 3-iPr-Phenyl 555 4 O 3-iPr-Phenyl 556 1 S 3-iPr-Phenyl 557 2 S 3-iPr-Phenyl 558 3 S 3-iPr-Phenyl 559 4 S 3-iPr-Phenyl 560 1 SO 3-iPr-Phenyl 561 2 SO 3-iPr-Phenyl 562 3 SO 3-iPr-Phenyl 563 4 SO 3-iPr-Phenyl 564 1 SO.sub.2 3-iPr-Phenyl 565 2 SO.sub.2 3-iPr-Phenyl 566 3 SO.sub.2 3-iPr-Phenyl 567 4 SO.sub.2 3-iPr-Phenyl 568 1 O 4-NH.sub.2-Phenyl 569 2 O 4-NH.sub.2-Phenyl 570 3 O 4-NH.sub.2-Phenyl 571 4 O 4-NH.sub.2-Phenyl 572 1 S 4-NH.sub.2-Phenyl 573 2 S 4-NH.sub.2-Phenyl 574 3 S 4-NH.sub.2-Phenyl 575 4 S 4-NH.sub.2-Phenyl 576 1 SO 4-NH.sub.2-Phenyl 577 2 SO 4-NH.sub.2-Phenyl 578 3 SO 4-NH.sub.2-Phenyl 579 4 SO 4-NH.sub.2-Phenyl 580 1 SO.sub.2 4-NH.sub.2-Phenyl 581 2 SO.sub.2 4-NH.sub.2-Phenyl 582 3 SO.sub.2 4-NH.sub.2-Phenyl 583 4 SO.sub.2 4-NH.sub.2-Phenyl 584 1 O 2-NH.sub.2-Phenyl 585 2 O 2-NH.sub.2-Phenyl 586 3 O 2-NH.sub.2-Phenyl 587 4 O 2-NH.sub.2-Phenyl 588 1 S 2-NH.sub.2-Phenyl 589 2 S 2-NH.sub.2-Phenyl 590 3 S 2-NH.sub.2-Phenyl 591 1 S 2-NH.sub.2-Phenyl 592 2 SO 2-NH.sub.2-Phenyl 593 3 SO 2-NH.sub.2-Phenyl 594 4 SO 2-NH.sub.2-Phenyl 595 1 SO 2-NH.sub.2-Phenyl 596 2 SO.sub.2 2-NH.sub.2-Phenyl 597 3 SO.sub.2 2-NH.sub.2-Phenyl 598 4 SO.sub.2 2-NH.sub.2-Phenyl 599 1 O 2,6-di-Me-Phenyl 600 2 O 2,6-di-Me-Phenyl 601 3 O 2,6-di-Me-Phenyl 602 4 O 2,6-di-Me-Phenyl 603 1 S 2,6-di-Me-Phenyl 604 2 S 2,6-di-Me-Phenyl 605 3 S 2,6-di-Me-Phenyl 606 4 S 2,6-di-Me-Phenyl 607 1 SO 2,6-di-Me-Phenyl 608 2 SO 2,6-di-Me-Phenyl 609 3 SO 2,6-di-Me-Phenyl 610 4 SO 2,6-di-Me-Phenyl 611 1 SO.sub.2 2,6-di-Me-Phenyl 612 2 SO.sub.2 2,6-di-Me-Phenyl 613 3 SO.sub.2 2,6-di-Me-Phenyl 614 4 SO.sub.2 2,6-di-Me-Phenyl 615 1 O 2-Ph-Phenyl 616 2 O 2-Ph-Phenyl 617 3 O 2-Ph-Phenyl 618 4 O 2-Ph-Phenyl 619 1 S 2-Ph-Phenyl 620 2 S 2-Ph-Phenyl 621 3 S 2-Ph-Phenyl 622 4 S 2-Ph-Phenyl 623 1 SO 2-Ph-Phenyl 624 2 SO 2-Ph-Phenyl 625 3 SO 2-Ph-Phenyl 626 4 SO 2-Ph-Phenyl 627 1 SO.sub.2 2-Ph-Phenyl 628 2 SO.sub.2 2-Ph-Phenyl 629 3 SO.sub.2 2-Ph-Phenyl 630 4 SO.sub.2 2-Ph-Phenyl 631 1 O 4-Ph-Phenyl 632 2 O 4-Ph-Phenyl 633 3 O 4-Ph-Phenyl 634 4 O 4-Ph-Phenyl 635 1 S 4-Ph-Phenyl 636 2 S 4-Ph-Phenyl 637 3 S 4-Ph-Phenyl 638 4 S 4-Ph-Phenyl 639 1 SO 4-Ph-Phenyl 640 2 SO 4-Ph-Phenyl 641 3 SO 4-Ph-Phenyl 642 4 SO 4-Ph-Phenyl 643 1 SO.sub.2 4-Ph-Phenyl 644 2 SO.sub.2 4-Ph-Phenyl 645 3 SO.sub.2 4-Ph-Phenyl 646 4 SO.sub.2 4-Ph-Phenyl 647 1 O 3-morpholino-phenyl 648 2 O 3-morpholino-phenyl 649 3 O 3-morpholino-phenyl 650 4 O 3-morpholino-phenyl 651 1 S 3-morpholino-phenyl 652 2 S 3-morpholino-phenyl 653 3 S 3-morpholino-phenyl 654 4 S 3-morpholino-phenyl 655 1 SO 3-morpholino-phenyl 656 2 SO 3-morpholino-phenyl 657 3 SO 3-morpholino-phenyl 658 4 SO 3-morpholino-phenyl 659 1 SO.sub.2 3-morpholino-phenyl 660 2 SO.sub.2 3-morpholino-phenyl 661 3 SO.sub.2 3-morpholino-phenyl 662 4 SO.sub.2 3-morpholino-phenyl 663 1 S 4-morpholino-phenyl 664 2 S 4-morpholino-phenyl 665 3 S 4-morpholino-phenyl 667 4 S 4-morpholino-phenyl 668 1 SO.sub.2 4-morpholino-phenyl 669 2 SO.sub.2 4-morpholino-phenyl 670 3 SO.sub.2 4-morpholino-phenyl 671 4 SO.sub.2 4-morpholino-phenyl 672 1 O naphthylen-2-yl 673 2 O naphthylen-2-yl 674 3 O naphthylen-2-yl 675 4 O naphthylen-2-yl 676 1 S naphthylen-2-yl 678 2 S naphthylen-2-yl 679 3 S naphthylen-2-yl 680 4 S naphthylen-2-yl 681 1 SO naphthylen-2-yl 682 2 SO naphthylen-2-yl 683 3 SO naphthylen-2-yl 684 4 SO naphthylen-2-yl 685 1 SO.sub.2 naphthylen-2-yl 686 2 SO.sub.2 naphthylen-2-yl 687 3 SO.sub.2 naphthylen-2-yl 688 4 SO.sub.2 naphthylen-2-yl

    [2052] Exemplary embodiments include compounds having the formula (XXXVII)

    ##STR00451##

    [2053] or a pharmaceutically acceptable salt form thereof defined herein below in Table 30.

    TABLE-US-00030 TABLE 30 Entry n X R.sup.3 1 1 O Phenyl 2 2 O Phenyl 3 3 O Phenyl 4 4 O Phenyl 5 1 S Phenyl 6 2 S Phenyl 7 3 S Phenyl 8 4 S Phenyl 9 1 SO Phenyl 10 2 SO Phenyl 11 3 SO Phenyl 12 4 SO Phenyl 13 1 SO.sub.2 Phenyl 14 2 SO.sub.2 Phenyl 15 3 SO.sub.2 Phenyl 16 4 SO.sub.2 Phenyl 17 1 O 3-OH-Phenyl 18 2 O 3-OH-Phenyl 19 3 O 3-OH-Phenyl 20 4 O 3-OH-Phenyl 21 1 S 3-OH-Phenyl 22 2 S 3-OH-Phenyl 23 3 S 3-OH-Phenyl 24 4 S 3-OH-Phenyl 25 1 SO 3-OH-Phenyl 26 2 SO 3-OH-Phenyl 27 3 SO 3-OH-Phenyl 28 4 SO 3-OH-Phenyl 29 1 SO.sub.2 3-OH-Phenyl 30 2 SO.sub.2 3-OH-Phenyl 31 3 SO.sub.2 3-OH-Phenyl 32 4 SO.sub.2 3-OH-Phenyl 33 1 O 4-NO.sub.2-Phenyl 34 2 O 4-NO.sub.2-Phenyl 35 3 O 4-NO.sub.2-Phenyl 36 4 O 4-NO.sub.2-Phenyl 37 1 S 4-NO.sub.2-Phenyl 38 2 S 4-NO.sub.2-Phenyl 39 3 S 4-NO.sub.2-Phenyl 40 4 S 4-NO.sub.2-Phenyl 41 1 SO 4-NO.sub.2-Phenyl 42 2 SO 4-NO.sub.2-Phenyl 43 3 SO 4-NO.sub.2-Phenyl 44 4 SO 4-NO.sub.2-Phenyl 45 1 SO.sub.2 4-NO.sub.2-Phenyl 46 2 SO.sub.2 4-NO.sub.2-Phenyl 47 3 SO.sub.2 4-NO.sub.2-Phenyl 48 4 SO.sub.2 4-NO.sub.2-Phenyl 49 1 O 3-OMe-Phenyl 50 2 O 3-OMe-Phenyl 51 3 O 3-OMe-Phenyl 52 4 O 3-OMe-Phenyl 53 1 S 3-OMe-Phenyl 54 2 S 3-OMe-Phenyl 55 3 S 3-OMe-Phenyl 56 4 S 3-OMe-Phenyl 57 1 SO 3-OMe-Phenyl 58 2 SO 3-OMe-Phenyl 59 3 SO 3-OMe-Phenyl 60 4 SO 3-OMe-Phenyl 61 1 SO.sub.2 3-OMe-Phenyl 62 2 SO.sub.2 3-OMe-Phenyl 63 3 SO.sub.2 3-OMe-Phenyl 64 4 SO.sub.2 3-OMe-Phenyl 65 1 O 4-CN-Phenyl 66 2 O 4-CN-Phenyl 67 3 O 4-CN-Phenyl 68 4 O 4-CN-Phenyl 69 1 S 4-CN-Phenyl 70 2 S 4-CN-Phenyl 71 3 S 4-CN-Phenyl 72 4 S 4-CN-Phenyl 73 1 SO 4-CN-Phenyl 74 2 SO 4-CN-Phenyl 75 3 SO 4-CN-Phenyl 76 4 SO 4-CN-Phenyl 77 1 SO.sub.2 4-CN-Phenyl 78 2 SO.sub.2 4-CN-Phenyl 79 3 SO.sub.2 4-CN-Phenyl 80 4 SO.sub.2 4-CN-Phenyl 81 1 O 2-CN-Phenyl 82 2 O 2-CN-Phenyl 83 3 O 2-CN-Phenyl 84 4 O 2-CN-Phenyl 85 1 S 2-CN-Phenyl 86 2 S 2-CN-Phenyl 87 3 S 2-CN-Phenyl 88 4 S 2-CN-Phenyl 89 1 SO 2-CN-Phenyl 90 2 SO 2-CN-Phenyl 91 3 SO 2-CN-Phenyl 92 4 SO 2-CN-Phenyl 93 1 SO.sub.2 2-CN-Phenyl 94 2 SO.sub.2 2-CN-Phenyl 95 3 SO.sub.2 2-CN-Phenyl 96 4 SO.sub.2 2-CN-Phenyl 97 1 O 3-Me-Phenyl 98 2 O 3-Me-Phenyl 99 3 O 3-Me-Phenyl 100 4 O 3-Me-Phenyl 101 1 S 3-Me-Phenyl 102 2 S 3-Me-Phenyl 103 3 S 3-Me-Phenyl 104 4 S 3-Me-Phenyl 105 1 SO 3-Me-Phenyl 106 2 SO 3-Me-Phenyl 107 3 SO 3-Me-Phenyl 108 4 SO 3-Me-Phenyl 109 1 SO.sub.2 3-Me-Phenyl 110 2 SO.sub.2 3-Me-Phenyl 111 3 SO.sub.2 3-Me-Phenyl 112 4 SO.sub.2 3-Me-Phenyl 113 1 O 2-F-Phenyl 114 2 O 2-F-Phenyl 115 3 O 2-F-Phenyl 116 4 O 2-F-Phenyl 117 1 S 2-F-Phenyl 118 2 S 2-F-Phenyl 119 3 S 2-F-Phenyl 120 4 S 2-F-Phenyl 121 1 SO 2-F-Phenyl 122 2 SO 2-F-Phenyl 123 3 SO 2-F-Phenyl 124 4 SO 2-F-Phenyl 125 1 SO.sub.2 2-F-Phenyl 126 2 SO.sub.2 2-F-Phenyl 127 3 SO.sub.2 2-F-Phenyl 128 4 SO.sub.2 2-F-Phenyl 129 1 O 4-F-Phenyl 130 2 O 4-F-Phenyl 131 3 O 4-F-Phenyl 132 4 O 4-F-Phenyl 133 1 O 4-F-Phenyl 134 2 S 4-F-Phenyl 135 3 S 4-F-Phenyl 136 4 S 4-F-Phenyl 137 1 S 4-F-Phenyl 138 2 SO 4-F-Phenyl 139 3 SO 4-F-Phenyl 140 4 SO 4-F-Phenyl 141 1 SO 4-F-Phenyl 142 2 SO.sub.2 4-F-Phenyl 143 3 SO.sub.2 4-F-Phenyl 144 4 SO.sub.2 4-F-Phenyl 145 1 O 3-Cl-Phenyl 146 2 O 3-Cl-Phenyl 147 3 O 3-Cl-Phenyl 148 4 O 3-Cl-Phenyl 149 1 S 3-Cl-Phenyl 150 2 S 3-Cl-Phenyl 151 3 S 3-Cl-Phenyl 152 4 S 3-Cl-Phenyl 153 1 SO 3-Cl-Phenyl 154 2 SO 3-Cl-Phenyl 155 3 SO 3-Cl-Phenyl 156 4 SO 3-Cl-Phenyl 157 1 SO.sub.2 3-Cl-Phenyl 158 2 SO.sub.2 3-Cl-Phenyl 159 3 SO.sub.2 3-Cl-Phenyl 160 4 SO.sub.2 3-Cl-Phenyl 161 1 O 2-Br-Phenyl 162 2 O 2-Br-Phenyl 163 3 O 2-Br-Phenyl 164 4 O 2-Br-Phenyl 165 1 S 2-Br-Phenyl 166 2 S 2-Br-Phenyl 167 3 S 2-Br-Phenyl 168 4 S 2-Br-Phenyl 169 1 SO 2-Br-Phenyl 170 2 SO 2-Br-Phenyl 171 3 SO 2-Br-Phenyl 172 4 SO 2-Br-Phenyl 173 1 SO.sub.2 2-Br-Phenyl 174 2 SO.sub.2 2-Br-Phenyl 175 3 SO.sub.2 2-Br-Phenyl 176 4 SO.sub.2 2-Br-Phenyl 177 1 O 4-Br-Phenyl 178 2 O 4-Br-Phenyl 179 3 O 4-Br-Phenyl 180 4 O 4-Br-Phenyl 181 1 S 4-Br-Phenyl 182 2 S 4-Br-Phenyl 183 3 S 4-Br-Phenyl 184 4 S 4-Br-Phenyl 185 1 SO 4-Br-Phenyl 186 2 SO 4-Br-Phenyl 187 3 SO 4-Br-Phenyl 188 4 SO 4-Br-Phenyl 189 1 SO.sub.2 4-Br-Phenyl 190 2 SO.sub.2 4-Br-Phenyl 191 3 SO.sub.2 4-Br-Phenyl 192 4 SO.sub.2 4-Br-Phenyl 193 1 O 3-CF.sub.3-Phenyl 194 2 O 3-CF.sub.3-Phenyl 195 3 O 3-CF.sub.3-Phenyl 196 4 O 3-CF.sub.3-Phenyl 197 1 S 3-CF.sub.3-Phenyl 198 2 S 3-CF.sub.3-Phenyl 199 3 S 3-CF.sub.3-Phenyl 200 4 S 3-CF.sub.3-Phenyl 201 1 SO 3-CF.sub.3-Phenyl 202 2 SO 3-CF.sub.3-Phenyl 203 3 SO 3-CF.sub.3-Phenyl 204 4 SO 3-CF.sub.3-Phenyl 205 1 SO.sub.2 3-CF.sub.3-Phenyl 206 2 SO.sub.2 3-CF.sub.3-Phenyl 207 3 SO.sub.2 3-CF.sub.3-Phenyl 208 4 SO.sub.2 3-CF.sub.3-Phenyl 209 1 O 2-iPr-Phenyl 210 2 O 2-iPr-Phenyl 211 3 O 2-iPr-Phenyl 212 4 O 2-iPr-Phenyl 213 1 S 2-iPr-Phenyl 214 2 S 2-iPr-Phenyl 215 3 S 2-iPr-Phenyl 216 4 S 2-iPr-Phenyl 217 1 SO 2-iPr-Phenyl 218 2 SO 2-iPr-Phenyl 219 3 SO 2-iPr-Phenyl 220 4 SO 2-iPr-Phenyl 221 1 SO.sub.2 2-iPr-Phenyl 222 2 SO.sub.2 2-iPr-Phenyl 223 3 SO.sub.2 2-iPr-Phenyl 224 4 SO.sub.2 2-iPr-Phenyl 225 1 O 4-iPr-Phenyl 226 2 O 4-iPr-Phenyl 227 3 O 4-iPr-Phenyl 228 4 O 4-iPr-Phenyl 229 1 S 4-iPr-Phenyl 230 2 S 4-iPr-Phenyl 231 3 S 4-iPr-Phenyl 232 4 S 4-iPr-Phenyl 233 1 SO 4-iPr-Phenyl 234 2 SO 4-iPr-Phenyl 235 3 SO 4-iPr-Phenyl 236 4 SO 4-iPr-Phenyl 237 1 SO.sub.2 4-iPr-Phenyl 238 2 SO.sub.2 4-iPr-Phenyl 239 3 SO.sub.2 4-iPr-Phenyl 240 4 SO.sub.2 4-iPr-Phenyl 241 1 O 3-NH.sub.2-Phenyl 242 2 O 3-NH.sub.2-Phenyl 243 3 O 3-NH.sub.2-Phenyl 244 4 O 3-NH.sub.2-Phenyl 245 1 S 3-NH.sub.2-Phenyl 246 2 S 3-NH.sub.2-Phenyl 247 3 S 3-NH.sub.2-Phenyl 248 1 S 3-NH.sub.2-Phenyl 249 2 SO 3-NH.sub.2-Phenyl 250 3 SO 3-NH.sub.2-Phenyl 251 4 SO 3-NH.sub.2-Phenyl 252 1 SO 3-NH.sub.2-Phenyl 253 2 SO.sub.2 3-NH.sub.2-Phenyl 254 3 SO.sub.2 3-NH.sub.2-Phenyl 255 4 SO.sub.2 3-NH.sub.2-Phenyl 256 1 O 2,4-di-Me-Phenyl 257 2 O 2,4-di-Me-Phenyl 258 3 O 2,4-di-Me-Phenyl 259 4 O 2,4-di-Me-Phenyl 260 1 S 2,4-di-Me-Phenyl 261 2 S 2,4-di-Me-Phenyl 262 3 S 2,4-di-Me-Phenyl 263 4 S 2,4-di-Me-Phenyl 264 1 SO 2,4-di-Me-Phenyl 265 2 SO 2,4-di-Me-Phenyl 266 3 SO 2,4-di-Me-Phenyl 267 4 SO 2,4-di-Me-Phenyl 268 1 SO.sub.2 2,4-di-Me-Phenyl 269 2 SO.sub.2 2,4-di-Me-Phenyl 270 3 SO.sub.2 2,4-di-Me-Phenyl 271 4 SO.sub.2 2,4-di-Me-Phenyl 272 1 O 2,6-di-iPr-Phenyl 273 2 O 2,6-di-iPr-Phenyl 274 3 O 2,6-di-iPr-Phenyl 275 4 O 2,6-di-iPr-Phenyl 276 1 S 2,6-di-iPr-Phenyl 277 2 S 2,6-di-iPr-Phenyl 278 3 S 2,6-di-iPr-Phenyl 279 4 S 2,6-di-iPr-Phenyl 280 1 SO 2,6-di-iPr-Phenyl 281 2 SO 2,6-di-iPr-Phenyl 282 3 SO 2,6-di-iPr-Phenyl 283 4 SO 2,6-di-iPr-Phenyl 284 1 SO.sub.2 2,6-di-iPr-Phenyl 285 2 SO.sub.2 2,6-di-iPr-Phenyl 286 3 SO.sub.2 2,6-di-iPr-Phenyl 287 4 SO.sub.2 2,6-di-iPr-Phenyl 288 1 O 3-Ph-Phenyl 289 2 O 3-Ph-Phenyl 290 3 O 3-Ph-Phenyl 291 4 O 3-Ph-Phenyl 292 1 S 3-Ph-Phenyl 293 2 S 3-Ph-Phenyl 294 3 S 3-Ph-Phenyl 295 4 S 3-Ph-Phenyl 296 1 SO 3-Ph-Phenyl 297 2 SO 3-Ph-Phenyl 298 3 SO 3-Ph-Phenyl 299 4 SO 3-Ph-Phenyl 300 1 SO.sub.2 3-Ph-Phenyl 301 2 SO.sub.2 3-Ph-Phenyl 302 3 SO.sub.2 3-Ph-Phenyl 303 4 SO.sub.2 3-Ph-Phenyl 304 1 O 2-morpholino-phenyl 305 2 O 2-morpholino-phenyl 306 3 O 2-morpholino-phenyl 307 4 O 2-morpholino-phenyl 308 1 S 2-morpholino-phenyl 309 2 S 2-morpholino-phenyl 310 3 S 2-morpholino-phenyl 311 4 S 2-morpholino-phenyl 312 1 SO 2-morpholino-phenyl 313 2 SO 2-morpholino-phenyl 314 3 SO 2-morpholino-phenyl 315 4 SO 2-morpholino-phenyl 316 1 SO.sub.2 2-morpholino-phenyl 317 2 SO.sub.2 2-morpholino-phenyl 318 3 SO.sub.2 2-morpholino-phenyl 319 4 SO.sub.2 2-morpholino-phenyl 320 1 O 4-morpholino-phenyl 321 2 O 4-morpholino-phenyl 322 3 O 4-morpholino-phenyl 323 4 O 4-morpholino-phenyl 324 1 SO 4-morpholino-phenyl 325 2 SO 4-morpholino-phenyl 326 3 SO 4-morpholino-phenyl 327 4 SO 4-morpholino-phenyl 328 1 O naphthylen-1-yl 329 2 O naphthylen-1-yl 330 3 O naphthylen-1-yl 331 4 O naphthylen-1-yl 332 1 S naphthylen-1-yl 333 2 S naphthylen-1-yl 334 3 S naphthylen-1-yl 335 4 S naphthylen-1-yl 336 1 SO naphthylen-1-yl 337 2 SO naphthylen-1-yl 338 3 SO naphthylen-1-yl 339 4 SO naphthylen-1-yl 340 1 SO.sub.2 naphthylen-1-yl 341 2 SO.sub.2 naphthylen-1-yl 342 3 SO.sub.2 naphthylen-1-yl 343 4 SO.sub.2 naphthylen-1-yl 344 1 O 4-OH-Phenyl 345 2 O 4-OH-Phenyl 346 3 O 4-OH-Phenyl 347 4 O 4-OH-Phenyl 348 1 S 4-OH-Phenyl 349 2 S 4-OH-Phenyl 350 3 S 4-OH-Phenyl 351 4 S 4-OH-Phenyl 352 1 SO 4-OH-Phenyl 353 2 SO 4-OH-Phenyl 354 3 SO 4-OH-Phenyl 355 4 SO 4-OH-Phenyl 356 1 SO.sub.2 4-OH-Phenyl 357 2 SO.sub.2 4-OH-Phenyl 358 3 SO.sub.2 4-OH-Phenyl 359 4 SO.sub.2 4-OH-Phenyl 360 1 O 2-OH-Phenyl 361 2 O 2-OH-Phenyl 362 3 O 2-OH-Phenyl 363 4 O 2-OH-Phenyl 364 1 S 2-OH-Phenyl 365 2 S 2-OH-Phenyl 366 3 S 2-OH-Phenyl 367 4 S 2-OH-Phenyl 368 1 SO 2-OH-Phenyl 369 2 SO 2-OH-Phenyl 370 3 SO 2-OH-Phenyl 371 4 SO 2-OH-Phenyl 372 1 SO.sub.2 2-OH-Phenyl 373 2 SO.sub.2 2-OH-Phenyl 374 3 SO.sub.2 2-OH-Phenyl 375 4 SO.sub.2 2-OH-Phenyl 376 1 O 4-OMe-Phenyl 377 2 O 4-OMe-Phenyl 378 3 O 4-OMe-Phenyl 379 4 O 4-OMe-Phenyl 380 1 S 4-OMe-Phenyl 381 2 S 4-OMe-Phenyl 382 3 S 4-OMe-Phenyl 383 4 S 4-OMe-Phenyl 384 1 SO 4-OMe-Phenyl 385 2 SO 4-OMe-Phenyl 386 3 SO 4-OMe-Phenyl 387 4 SO 4-OMe-Phenyl 388 1 SO.sub.2 4-OMe-Phenyl 389 2 SO.sub.2 4-OMe-Phenyl 390 3 SO.sub.2 4-OMe-Phenyl 391 4 SO.sub.2 4-OMe-Phenyl 392 1 O 2-OMe-Phenyl 393 2 O 2-OMe-Phenyl 394 3 O 2-OMe-Phenyl 395 4 O 2-OMe-Phenyl 396 1 S 2-OMe-Phenyl 397 2 S 2-OMe-Phenyl 398 3 S 2-OMe-Phenyl 399 4 S 2-OMe-Phenyl 400 1 SO 2-OMe-Phenyl 401 2 SO 2-OMe-Phenyl 402 3 SO 2-OMe-Phenyl 403 4 SO 2-OMe-Phenyl 404 1 SO.sub.2 2-OMe-Phenyl 405 2 SO.sub.2 2-OMe-Phenyl 406 3 SO.sub.2 2-OMe-Phenyl 407 4 SO.sub.2 2-OMe-Phenyl 408 1 O 3-CN-Phenyl 409 2 O 3-CN-Phenyl 410 3 O 3-CN-Phenyl 411 4 O 3-CN-Phenyl 412 1 S 3-CN-Phenyl 413 2 S 3-CN-Phenyl 414 3 S 3-CN-Phenyl 415 4 S 3-CN-Phenyl 416 1 SO 3-CN-Phenyl 417 2 SO 3-CN-Phenyl 418 3 SO 3-CN-Phenyl 419 4 SO 3-CN-Phenyl 420 1 SO.sub.2 3-CN-Phenyl 421 2 SO.sub.2 3-CN-Phenyl 422 3 SO.sub.2 3-CN-Phenyl 423 4 SO.sub.2 3-CN-Phenyl 424 1 O 2-Me-Phenyl 425 2 O 2-Me-Phenyl 426 3 O 2-Me-Phenyl 427 4 O 2-Me-Phenyl 428 1 S 2-Me-Phenyl 429 2 S 2-Me-Phenyl 430 3 S 2-Me-Phenyl 431 4 S 2-Me-Phenyl 432 1 SO 2-Me-Phenyl 433 2 SO 2-Me-Phenyl 434 3 SO 2-Me-Phenyl 435 4 SO 2-Me-Phenyl 436 1 SO.sub.2 2-Me-Phenyl 437 2 SO.sub.2 2-Me-Phenyl 438 3 SO.sub.2 2-Me-Phenyl 439 4 SO.sub.2 2-Me-Phenyl 440 1 O 4-Me-Phenyl 441 2 O 4-Me-Phenyl 442 3 O 4-Me-Phenyl 443 4 O 4-Me-Phenyl 444 1 S 4-Me-Phenyl 445 2 S 4-Me-Phenyl 446 3 S 4-Me-Phenyl 447 4 S 4-Me-Phenyl 448 1 SO 4-Me-Phenyl 449 2 SO 4-Me-Phenyl 450 3 SO 4-Me-Phenyl 451 4 SO 4-Me-Phenyl 452 1 SO.sub.2 4-Me-Phenyl 453 2 SO.sub.2 4-Me-Phenyl 454 3 SO.sub.2 4-Me-Phenyl 455 4 SO.sub.2 4-Me-Phenyl 456 1 O 3-F-Phenyl 457 2 O 3-F-Phenyl 458 3 O 3-F-Phenyl 459 4 O 3-F-Phenyl 460 1 S 3-F-Phenyl 461 2 S 3-F-Phenyl 462 3 S 3-F-Phenyl 463 4 S 3-F-Phenyl 464 1 SO 3-F-Phenyl 465 2 SO 3-F-Phenyl 466 3 SO 3-F-Phenyl 467 4 SO 3-F-Phenyl 468 1 SO.sub.2 3-F-Phenyl 469 2 SO.sub.2 3-F-Phenyl 470 3 SO.sub.2 3-F-Phenyl 471 4 SO.sub.2 3-F-Phenyl 472 1 O 2-Cl-Phenyl 473 2 O 2-Cl-Phenyl 474 3 O 2-Cl-Phenyl 475 4 O 2-Cl-Phenyl 476 1 S 2-Cl-Phenyl 477 2 S 2-Cl-Phenyl 478 3 S 2-Cl-Phenyl 479 4 S 2-Cl-Phenyl 480 1 SO 2-Cl-Phenyl 481 2 SO 2-Cl-Phenyl 482 3 SO 2-Cl-Phenyl 483 4 SO 2-Cl-Phenyl 484 1 SO.sub.2 2-Cl-Phenyl 485 2 SO.sub.2 2-Cl-Phenyl 486 3 SO.sub.2 2-Cl-Phenyl 487 4 SO.sub.2 2-Cl-Phenyl 488 1 O 4-Cl-Phenyl 489 2 O 4-Cl-Phenyl 490 3 O 4-Cl-Phenyl 491 4 O 4-Cl-Phenyl 492 1 S 4-Cl-Phenyl 493 2 S 4-Cl-Phenyl 494 3 S 4-Cl-Phenyl 495 4 S 4-Cl-Phenyl 496 1 SO 4-Cl-Phenyl 497 2 SO 4-Cl-Phenyl 498 3 SO 4-Cl-Phenyl 499 4 SO 4-Cl-Phenyl 500 1 SO.sub.2 4-Cl-Phenyl 501 2 SO.sub.2 4-Cl-Phenyl 502 3 SO.sub.2 4-Cl-Phenyl 503 4 SO.sub.2 4-Cl-Phenyl 504 1 O 3-Br-Phenyl 505 2 O 3-Br-Phenyl 506 3 O 3-Br-Phenyl 507 4 O 3-Br-Phenyl 508 1 S 3-Br-Phenyl 509 2 S 3-Br-Phenyl 510 3 S 3-Br-Phenyl 511 4 S 3-Br-Phenyl 512 1 SO 3-Br-Phenyl 513 2 SO 3-Br-Phenyl 514 3 SO 3-Br-Phenyl 515 4 SO 3-Br-Phenyl 516 1 SO.sub.2 3-Br-Phenyl 517 2 SO.sub.2 3-Br-Phenyl 518 3 SO.sub.2 3-Br-Phenyl 519 4 SO.sub.2 3-Br-Phenyl 520 1 O 2-CF.sub.3-Phenyl 521 2 O 2-CF.sub.3-Phenyl 522 3 O 2-CF.sub.3-Phenyl 523 4 O 2-CF.sub.3-Phenyl 524 1 S 2-CF.sub.3-Phenyl 525 2 S 2-CF.sub.3-Phenyl 526 3 S 2-CF.sub.3-Phenyl 527 4 S 2-CF.sub.3-Phenyl 528 1 SO 2-CF.sub.3-Phenyl 529 2 SO 2-CF.sub.3-Phenyl 530 3 SO 2-CF.sub.3-Phenyl 531 4 SO 2-CF.sub.3-Phenyl 532 1 SO.sub.2 2-CF.sub.3-Phenyl 533 2 SO.sub.2 2-CF.sub.3-Phenyl 534 3 SO.sub.2 2-CF.sub.3-Phenyl 535 4 SO.sub.2 2-CF.sub.3-Phenyl 536 1 O 4-CF.sub.3-Phenyl 537 2 O 4-CF.sub.3-Phenyl 538 3 O 4-CF.sub.3-Phenyl 539 4 O 4-CF.sub.3-Phenyl 540 1 S 4-CF.sub.3-Phenyl 541 2 S 4-CF.sub.3-Phenyl 542 3 S 4-CF.sub.3-Phenyl 543 4 S 4-CF.sub.3-Phenyl 544 1 SO 4-CF.sub.3-Phenyl 545 2 SO 4-CF.sub.3-Phenyl 546 3 SO 4-CF.sub.3-Phenyl 547 4 SO 3-CF.sub.3-Phenyl 548 1 SO.sub.2 4-CF.sub.3-Phenyl 549 2 SO.sub.2 4-CF.sub.3-Phenyl 550 3 SO.sub.2 4-CF.sub.3-Phenyl 551 4 SO.sub.2 4-CF.sub.3-Phenyl 552 1 O 3-iPr-Phenyl 553 2 O 3-iPr-Phenyl 554 3 O 3-iPr-Phenyl 555 4 O 3-iPr-Phenyl 556 1 S 3-iPr-Phenyl 557 2 S 3-iPr-Phenyl 558 3 S 3-iPr-Phenyl 559 4 S 3-iPr-Phenyl 560 1 SO 3-iPr-Phenyl 561 2 SO 3-iPr-Phenyl 562 3 SO 3-iPr-Phenyl 563 4 SO 3-iPr-Phenyl 564 1 SO.sub.2 3-iPr-Phenyl 565 2 SO.sub.2 3-iPr-Phenyl 566 3 SO.sub.2 3-iPr-Phenyl 567 4 SO.sub.2 3-iPr-Phenyl 568 1 O 4-NH.sub.2-Phenyl 569 2 O 4-NH.sub.2-Phenyl 570 3 O 4-NH.sub.2-Phenyl 571 4 O 4-NH.sub.2-Phenyl 572 1 S 4-NH.sub.2-Phenyl 573 2 S 4-NH.sub.2-Phenyl 574 3 S 4-NH.sub.2-Phenyl 575 4 S 4-NH.sub.2-Phenyl 576 1 SO 4-NH.sub.2-Phenyl 577 2 SO 4-NH.sub.2-Phenyl 578 3 SO 4-NH.sub.2-Phenyl 579 4 SO 4-NH.sub.2-Phenyl 580 1 SO.sub.2 4-NH.sub.2-Phenyl 581 2 SO.sub.2 4-NH.sub.2-Phenyl 582 3 SO.sub.2 4-NH.sub.2-Phenyl 583 4 SO.sub.2 4-NH.sub.2-Phenyl 584 1 O 2-NH.sub.2-Phenyl 585 2 O 2-NH.sub.2-Phenyl 586 3 O 2-NH.sub.2-Phenyl 587 4 O 2-NH.sub.2-Phenyl 588 1 S 2-NH.sub.2-Phenyl 589 2 S 2-NH.sub.2-Phenyl 590 3 S 2-NH.sub.2-Phenyl 591 1 S 2-NH.sub.2-Phenyl 592 2 SO 2-NH.sub.2-Phenyl 593 3 SO 2-NH.sub.2-Phenyl 594 4 SO 2-NH.sub.2-Phenyl 595 1 SO 2-NH.sub.2-Phenyl 596 2 SO.sub.2 2-NH.sub.2-Phenyl 597 3 SO.sub.2 2-NH.sub.2-Phenyl 598 4 SO.sub.2 2-NH.sub.2-Phenyl 599 1 O 2,6-di-Me-Phenyl 600 2 O 2,6-di-Me-Phenyl 601 3 O 2,6-di-Me-Phenyl 602 4 O 2,6-di-Me-Phenyl 603 1 S 2,6-di-Me-Phenyl 604 2 S 2,6-di-Me-Phenyl 605 3 S 2,6-di-Me-Phenyl 606 4 S 2,6-di-Me-Phenyl 607 1 SO 2,6-di-Me-Phenyl 608 2 SO 2,6-di-Me-Phenyl 609 3 SO 2,6-di-Me-Phenyl 610 4 SO 2,6-di-Me-Phenyl 611 1 SO.sub.2 2,6-di-Me-Phenyl 612 2 SO.sub.2 2,6-di-Me-Phenyl 613 3 SO.sub.2 2,6-di-Me-Phenyl 614 4 SO.sub.2 2,6-di-Me-Phenyl 615 1 O 2-Ph-Phenyl 616 2 O 2-Ph-Phenyl 617 3 O 2-Ph-Phenyl 618 4 O 2-Ph-Phenyl 619 1 S 2-Ph-Phenyl 620 2 S 2-Ph-Phenyl 621 3 S 2-Ph-Phenyl 622 4 S 2-Ph-Phenyl 623 1 SO 2-Ph-Phenyl 624 2 SO 2-Ph-Phenyl 625 3 SO 2-Ph-Phenyl 626 4 SO 2-Ph-Phenyl 627 1 SO.sub.2 2-Ph-Phenyl 628 2 SO.sub.2 2-Ph-Phenyl 629 3 SO.sub.2 2-Ph-Phenyl 630 4 SO.sub.2 2-Ph-Phenyl 631 1 O 4-Ph-Phenyl 632 2 O 4-Ph-Phenyl 633 3 O 4-Ph-Phenyl 634 4 O 4-Ph-Phenyl 635 1 S 4-Ph-Phenyl 636 2 S 4-Ph-Phenyl 637 3 S 4-Ph-Phenyl 638 4 S 4-Ph-Phenyl 639 1 SO 4-Ph-Phenyl 640 2 SO 4-Ph-Phenyl 641 3 SO 4-Ph-Phenyl 642 4 SO 4-Ph-Phenyl 643 1 SO.sub.2 4-Ph-Phenyl 644 2 SO.sub.2 4-Ph-Phenyl 645 3 SO.sub.2 4-Ph-Phenyl 646 4 SO.sub.2 4-Ph-Phenyl 647 1 O 3-morpholino-phenyl 648 2 O 3-morpholino-phenyl 649 3 O 3-morpholino-phenyl 650 4 O 3-morpholino-phenyl 651 1 S 3-morpholino-phenyl 652 2 S 3-morpholino-phenyl 653 3 S 3-morpholino-phenyl 654 4 S 3-morpholino-phenyl 655 1 SO 3-morpholino-phenyl 656 2 SO 3-morpholino-phenyl 657 3 SO 3-morpholino-phenyl 658 4 SO 3-morpholino-phenyl 659 1 SO.sub.2 3-morpholino-phenyl 660 2 SO.sub.2 3-morpholino-phenyl 661 3 SO.sub.2 3-morpholino-phenyl 662 4 SO.sub.2 3-morpholino-phenyl 663 1 S 4-morpholino-phenyl 664 2 S 4-morpholino-phenyl 665 3 S 4-morpholino-phenyl 667 4 S 4-morpholino-phenyl 668 1 SO.sub.2 4-morpholino-phenyl 669 2 SO.sub.2 4-morpholino-phenyl 670 3 SO.sub.2 4-morpholino-phenyl 671 4 SO.sub.2 4-morpholino-phenyl 672 1 O naphthylen-2-yl 673 2 O naphthylen-2-yl 674 3 O naphthylen-2-yl 675 4 O naphthylen-2-yl 676 1 S naphthylen-2-yl 678 2 S naphthylen-2-yl 679 3 S naphthylen-2-yl 680 4 S naphthylen-2-yl 681 1 SO naphthylen-2-yl 682 2 SO naphthylen-2-yl 683 3 SO naphthylen-2-yl 684 4 SO naphthylen-2-yl 685 1 SO.sub.2 naphthylen-2-yl 686 2 SO.sub.2 naphthylen-2-yl 687 3 SO.sub.2 naphthylen-2-yl 688 4 SO.sub.2 naphthylen-2-yl

    [2054] Exemplary embodiments include compounds having the formula (XXXVIII)

    ##STR00452##

    [2055] or a pharmaceutically acceptable salt form thereof defined herein below in Table 31

    TABLE-US-00031 TABLE 31 Entry n R.sup.3 R.sup.10c 1 1 4-CH.sub.3-phenyl Ethyl 2 1 4-CH.sub.3-phenyl n-propyl 3 1 4-CH.sub.3-phenyl Isopropyl 4 1 4-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 5 1 4-CH.sub.3-phenyl CF.sub.3 6 1 4-CH.sub.3-phenyl —CH.sub.2CF.sub.3 7 1 4-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 8 1 4-CH.sub.3-phenyl Cyclopropyl 9 1 4-CH.sub.3-phenyl Cyclobutyl 10 1 4-CH.sub.3-phenyl Cyclopentyl 11 1 4-CH.sub.3-phenyl Cyclohexyl 12 1 4-CH.sub.3-phenyl 3-pyridyl 13 1 4-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 14 1 4-CH.sub.3-phenyl 1H-imidazol-4-yl 15 1 4-CH.sub.3-phenyl 2-furanyl 16 1 4-CH.sub.3-phenyl Ethyl 17 1 4-CH.sub.3-phenyl n-propyl 18 1 4-CH.sub.3-phenyl Isopropyl 19 1 4-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 20 1 4-CH.sub.3-phenyl CF.sub.3 21 1 4-CH.sub.3-phenyl —CH.sub.2CF.sub.3 22 1 4-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 23 1 4-CH.sub.3-phenyl Cyclopropyl 24 1 4-CH.sub.3-phenyl Cyclobutyl 25 1 4-CH.sub.3-phenyl Cyclopentyl 26 1 4-CH.sub.3-phenyl Cyclohexyl 27 1 4-CH.sub.3-phenyl 3-pyridyl 28 1 4-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 29 1 4-CH.sub.3-phenyl 1H-imidazol-4-yl 30 1 4-CH.sub.3-phenyl 2-furanyl 31 1 3-OH-Phenyl Ethyl 32 1 3-OH-Phenyl n-propyl 33 1 3-OH-Phenyl Isopropyl 34 1 3-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 35 1 3-OH-Phenyl CF.sub.3 36 1 3-OH-Phenyl —CH.sub.2CF.sub.3 37 1 3-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 38 1 3-OH-Phenyl Cyclopropyl 39 1 3-OH-Phenyl Cyclobutyl 40 1 3-OH-Phenyl Cyclopentyl 41 1 3-OH-Phenyl Cyclohexyl 42 1 3-OH-Phenyl 3-pyridyl 43 1 3-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 44 1 3-OH-Phenyl 1H-imidazol-4-yl 45 1 3-OH-Phenyl 2-furanyl 46 1 4-OMe-Phenyl Ethyl 47 1 4-OMe-Phenyl n-propyl 48 1 4-OMe-Phenyl Isopropyl 49 1 4-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 50 1 4-OMe-Phenyl CF.sub.3 51 1 4-OMe-Phenyl —CH.sub.2CF.sub.3 52 1 4-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 53 1 4-OMe-Phenyl Cyclopropyl 54 1 4-OMe-Phenyl Cyclobutyl 55 1 4-OMe-Phenyl Cyclopentyl 56 1 4-OMe-Phenyl Cyclohexyl 57 1 4-OMe-Phenyl 3-pyridyl 58 1 4-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 59 1 4-OMe-Phenyl 1H-imidazol-4-yl 60 1 4-OMe-Phenyl 2-furanyl 61 1 2-OMe-Phenyl Ethyl 62 1 2-OMe-Phenyl n-propyl 63 1 2-OMe-Phenyl Isopropyl 64 1 2-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 65 1 2-OMe-Phenyl CF.sub.3 66 1 2-OMe-Phenyl —CH.sub.2CF.sub.3 67 1 2-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 68 1 2-OMe-Phenyl Cyclopropyl 69 1 2-OMe-Phenyl Cyclobutyl 70 1 2-OMe-Phenyl Cyclopentyl 71 1 2-OMe-Phenyl Cyclohexyl 72 1 2-OMe-Phenyl 3-pyridyl 73 1 2-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 74 1 2-OMe-Phenyl 1H-imidazol-4-yl 75 1 2-OMe-Phenyl 2-furanyl 76 1 3-CN-Phenyl Ethyl 77 1 3-CN-Phenyl n-propyl 78 1 3-CN-Phenyl Isopropyl 79 1 3-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 80 1 3-CN-Phenyl CF.sub.3 81 1 3-CN-Phenyl —CH.sub.2CF.sub.3 82 1 3-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 83 1 3-CN-Phenyl Cyclopropyl 84 1 3-CN-Phenyl Cyclobutyl 85 1 3-CN-Phenyl Cyclopentyl 86 1 3-CN-Phenyl Cyclohexyl 87 1 3-CN-Phenyl 3-pyridyl 88 1 3-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 89 1 3-CN-Phenyl 1H-imidazol-4-yl 90 1 3-CN-Phenyl 2-furanyl 91 1 2-F-Phenyl Ethyl 92 1 2-F-Phenyl n-propyl 93 1 2-F-Phenyl Isopropyl 94 1 2-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 95 1 2-F-Phenyl CF.sub.3 96 1 2-F-Phenyl —CH.sub.2CF.sub.3 97 1 2-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 98 1 2-F-Phenyl Cyclopropyl 99 1 2-F-Phenyl Cyclobutyl 100 1 2-F-Phenyl Cyclopentyl 101 1 2-F-Phenyl Cyclohexyl 102 1 2-F-Phenyl 3-pyridyl 103 1 2-F-Phenyl 1-methyl-1H-pyrazol-4-yl 104 1 2-F-Phenyl 1H-imidazol-4-yl 105 1 2-F-Phenyl 2-furanyl 106 1 4-F-Phenyl Ethyl 107 1 4-F-Phenyl n-propyl 108 1 4-F-Phenyl Isopropyl 109 1 4-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 110 1 4-F-Phenyl CF.sub.3 111 1 4-F-Phenyl —CH.sub.2CF.sub.3 112 1 4-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 113 1 4-F-Phenyl Cyclopropyl 114 1 4-F-Phenyl Cyclobutyl 115 1 4-F-Phenyl Cyclopentyl 116 1 4-F-Phenyl Cyclohexyl 117 1 4-F-Phenyl 3-pyridyl 118 1 4-F-Phenyl 1-methyl-1H-pyrazol-4-yl 119 1 4-F-Phenyl 1H-imidazol-4-yl 120 1 4-F-Phenyl 2-furanyl 121 1 3-Cl-Phenyl Ethyl 122 1 3-Cl-Phenyl n-propyl 123 1 3-Cl-Phenyl Isopropyl 124 1 3-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 125 1 3-Cl-Phenyl CF.sub.3 126 1 3-Cl-Phenyl —CH.sub.2CF.sub.3 127 1 3-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 128 1 3-Cl-Phenyl Cyclopropyl 129 1 3-Cl-Phenyl Cyclobutyl 130 1 3-Cl-Phenyl Cyclopentyl 131 1 3-Cl-Phenyl Cyclohexyl 132 1 3-Cl-Phenyl 3-pyridyl 133 1 3-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 134 1 3-Cl-Phenyl 1H-imidazol-4-yl 135 1 3-Cl-Phenyl 2-furanyl 136 1 2-Br-Phenyl ethyl 137 1 2-Br-Phenyl n-propyl 138 1 2-Br-Phenyl isopropyl 139 1 2-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 140 1 2-Br-Phenyl CF.sub.3 141 1 2-Br-Phenyl —CH.sub.2CF.sub.3 142 1 2-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 143 1 2-Br-Phenyl cyclopropyl 144 1 2-Br-Phenyl Cyclobutyl 145 1 2-Br-Phenyl cyclopentyl 146 1 2-Br-Phenyl cyclohexyl 147 1 2-Br-Phenyl 3-pyridyl 148 1 2-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 149 1 2-Br-Phenyl 1H-imidazol-4-yl 150 1 2-Br-Phenyl 2-furanyl 151 1 4-Br-Phenyl ethyl 152 1 4-Br-Phenyl n-propyl 153 1 4-Br-Phenyl isopropyl 154 1 4-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 155 1 4-Br-Phenyl CF.sub.3 156 1 4-Br-Phenyl —CH.sub.2CF.sub.3 157 1 4-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 158 1 4-Br-Phenyl cyclopropyl 159 1 4-Br-Phenyl Cyclobutyl 160 1 4-Br-Phenyl cyclopentyl 161 1 4-Br-Phenyl cyclohexyl 162 1 4-Br-Phenyl 3-pyridyl 163 1 4-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 164 1 4-Br-Phenyl 1H-imidazol-4-yl 165 1 4-Br-Phenyl 2-furanyl 166 1 3-CF.sub.3-Phenyl ethyl 167 1 3-CF.sub.3-Phenyl n-propyl 168 1 3-CF.sub.3-Phenyl isopropyl 169 1 3-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 170 1 3-CF.sub.3-Phenyl CF.sub.3 171 1 3-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 172 1 3-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 173 1 3-CF.sub.3-Phenyl cyclopropyl 174 1 3-CF.sub.3-Phenyl Cyclobutyl 175 1 3-CF.sub.3-Phenyl cyclopentyl 176 1 3-CF.sub.3-Phenyl cyclohexyl 177 1 3-CF.sub.3-Phenyl 3-pyridyl 178 1 3-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 179 1 3-CF.sub.3-Phenyl 1H-imidazol-4-yl 180 1 3-CF.sub.3-Phenyl 2-furanyl 181 1 2-iPr-Phenyl ethyl 182 1 2-iPr-Phenyl n-propyl 183 1 2-iPr-Phenyl isopropyl 184 1 2-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 185 1 2-iPr-Phenyl CF.sub.3 186 1 2-iPr-Phenyl —CH.sub.2CF.sub.3 187 1 2-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 188 1 2-iPr-Phenyl cyclopropyl 189 1 2-iPr-Phenyl Cyclobutyl 190 1 2-iPr-Phenyl cyclopentyl 191 1 2-iPr-Phenyl cyclohexyl 192 1 2-iPr-Phenyl 3-pyridyl 193 1 2-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 194 1 2-iPr-Phenyl 1H-imidazol-4-yl 195 1 2-iPr-Phenyl 2-furanyl 196 1 4-iPr-Phenyl ethyl 197 1 4-iPr-Phenyl n-propyl 198 1 4-iPr-Phenyl isopropyl 199 1 4-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 200 1 4-iPr-Phenyl CF.sub.3 201 1 4-iPr-Phenyl —CH.sub.2CF.sub.3 202 1 4-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 203 1 4-iPr-Phenyl cyclopropyl 204 1 4-iPr-Phenyl Cyclobutyl 205 1 4-iPr-Phenyl cyclopentyl 206 1 4-iPr-Phenyl cyclohexyl 207 1 4-iPr-Phenyl 3-pyridyl 208 1 4-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 209 1 4-iPr-Phenyl 1H-imidazol-4-yl 210 1 4-iPr-Phenyl 2-furanyl 211 1 3-morpholino-phenyl ethyl 212 1 3-morpholino-phenyl n-propyl 213 1 3-morpholino-phenyl isopropyl 214 1 3-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 215 1 3-morpholino-phenyl CF.sub.3 216 1 3-morpholino-phenyl —CH.sub.2CF.sub.3 217 1 3-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 218 1 3-morpholino-phenyl cyclopropyl 219 1 3-morpholino-phenyl Cyclobutyl 220 1 3-morpholino-phenyl cyclopentyl 221 1 3-morpholino-phenyl cyclohexyl 222 1 3-morpholino-phenyl 3-pyridyl 223 1 3-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 224 1 3-morpholino-phenyl 1H-imidazol-4-yl 225 1 3-morpholino-phenyl 2-furanyl 226 1 4-cyano-2-morpholino-phenyl ethyl 227 1 4-cyano-2-morpholino-phenyl n-propyl 228 1 4-cyano-2-morpholino-phenyl isopropyl 229 1 4-cyano-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 230 1 4-cyano-2-morpholino-phenyl CF.sub.3 231 1 4-cyano-2-morpholino-phenyl —CH.sub.2CF.sub.3 232 1 4-cyano-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 233 1 4-cyano-2-morpholino-phenyl cyclopropyl 234 1 4-cyano-2-morpholino-phenyl Cyclobutyl 235 1 4-cyano-2-morpholino-phenyl cyclopentyl 236 1 4-cyano-2-morpholino-phenyl cyclohexyl 237 1 4-cyano-2-morpholino-phenyl 3-pyridyl 238 1 4-cyano-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 239 1 4-cyano-2-morpholino-phenyl 1H-imidazol-4-yl 240 1 4-cyano-2-morpholino-phenyl 2-furanyl 241 1 4-hydroxy-2-morpholino-phenyl ethyl 242 1 4-hydroxy-2-morpholino-phenyl n-propyl 243 1 4-hydroxy-2-morpholino-phenyl isopropyl 244 1 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 245 1 4-hydroxy-2-morpholino-phenyl CF.sub.3 246 1 4-hydroxy-2-morpholino-phenyl —CH.sub.2CF.sub.3 247 1 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 248 1 4-hydroxy-2-morpholino-phenyl cyclopropyl 249 1 4-hydroxy-2-morpholino-phenyl Cyclobutyl 250 1 4-hydroxy-2-morpholino-phenyl cyclopentyl 251 1 4-hydroxy-2-morpholino-phenyl cyclohexyl 252 1 4-hydroxy-2-morpholino-phenyl 3-pyridyl 253 1 4-hydroxy-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 254 1 4-hydroxy-2-morpholino-phenyl 1H-imidazol-4-yl 255 1 4-hydroxy-2-morpholino-phenyl 2-furanyl 256 1 2-CH.sub.3-phenyl Ethyl 257 1 2-CH.sub.3-phenyl n-propyl 258 1 2-CH.sub.3-phenyl Isopropyl 259 1 2-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 260 1 2-CH.sub.3-phenyl CF.sub.3 261 1 2-CH.sub.3-phenyl —CH.sub.2CF.sub.3 262 1 2-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 263 1 2-CH.sub.3-phenyl cyclopropyl 264 1 2-CH.sub.3-phenyl Cyclobutyl 265 1 2-CH.sub.3-phenyl cyclopentyl 266 1 2-CH.sub.3-phenyl cyclohexyl 267 1 2-CH.sub.3-phenyl 3-pyridyl 268 1 2-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 269 1 2-CH.sub.3-phenyl 1H-imidazol-4-yl 270 1 2-CH.sub.3-phenyl 2-furanyl 271 1 4-OH-Phenyl Ethyl 272 1 4-OH-Phenyl n-propyl 273 1 4-OH-Phenyl Isopropyl 274 1 4-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 275 1 4-OH-Phenyl CF.sub.3 276 1 4-OH-Phenyl —CH.sub.2CF.sub.3 277 1 4-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 278 1 4-OH-Phenyl cyclopropyl 279 1 4-OH-Phenyl Cyclobutyl 280 1 4-OH-Phenyl cyclopentyl 281 1 4-OH-Phenyl cyclohexyl 282 1 4-OH-Phenyl 3-pyridyl 283 1 4-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 284 1 4-OH-Phenyl 1H-imidazol-4-yl 285 1 4-OH-Phenyl 2-furanyl 286 1 2-OH-Phenyl Ethyl 287 1 2-OH-Phenyl n-propyl 288 1 2-OH-Phenyl Isopropyl 289 1 2-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 290 1 2-OH-Phenyl CF.sub.3 291 1 2-OH-Phenyl —CH.sub.2CF.sub.3 292 1 2-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 293 1 2-OH-Phenyl cyclopropyl 294 1 2-OH-Phenyl Cyclobutyl 295 1 2-OH-Phenyl cyclopentyl 296 1 2-OH-Phenyl cyclohexyl 297 1 2-OH-Phenyl 3-pyridyl 298 1 2-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 299 1 2-OH-Phenyl 1H-imidazol-4-yl 300 1 2-OH-Phenyl 2-furanyl 301 1 3-OMe-Phenyl Ethyl 302 1 3-OMe-Phenyl n-propyl 303 1 3-OMe-Phenyl Isopropyl 304 1 3-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 305 1 3-OMe-Phenyl CF.sub.3 306 1 3-OMe-Phenyl —CH.sub.2CF.sub.3 307 1 3-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 308 1 3-OMe-Phenyl cyclopropyl 309 1 3-OMe-Phenyl Cyclobutyl 310 1 3-OMe-Phenyl cyclopentyl 311 1 3-OMe-Phenyl cyclohexyl 312 1 3-OMe-Phenyl 3-pyridyl 313 1 3-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 314 1 3-OMe-Phenyl 1H-imidazol-4-yl 315 1 3-OMe-Phenyl 2-furanyl 316 1 4-CN-Phenyl Ethyl 317 1 4-CN-Phenyl n-propyl 318 1 4-CN-Phenyl Isopropyl 319 1 4-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 320 1 4-CN-Phenyl CF.sub.3 321 1 4-CN-Phenyl —CH.sub.2CF.sub.3 322 1 4-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 323 1 4-CN-Phenyl cyclopropyl 324 1 4-CN-Phenyl Cyclobutyl 325 1 4-CN-Phenyl cyclopentyl 326 1 4-CN-Phenyl cyclohexyl 327 1 4-CN-Phenyl 3-pyridyl 328 1 4-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 329 1 4-CN-Phenyl 1H-imidazol-4-yl 330 1 4-CN-Phenyl 2-furanyl 331 1 2-CN-Phenyl Ethyl 332 1 2-CN-Phenyl n-propyl 333 1 2-CN-Phenyl Isopropyl 334 1 2-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 335 1 2-CN-Phenyl CF.sub.3 336 1 2-CN-Phenyl —CH.sub.2CF.sub.3 337 1 2-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 338 1 2-CN-Phenyl cyclopropyl 339 1 2-CN-Phenyl Cyclobutyl 340 1 2-CN-Phenyl cyclopentyl 341 1 2-CN-Phenyl cyclohexyl 342 1 2-CN-Phenyl 3-pyridyl 343 1 2-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 344 1 2-CN-Phenyl 1H-imidazol-4-yl 345 1 2-CN-Phenyl 2-furanyl 346 1 3-F-Phenyl Ethyl 347 1 3-F-Phenyl n-propyl 348 1 3-F-Phenyl Isopropyl 349 1 3-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 350 1 3-F-Phenyl CF.sub.3 351 1 3-F-Phenyl —CH.sub.2CF.sub.3 352 1 3-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 353 1 3-F-Phenyl cyclopropyl 354 1 3-F-Phenyl Cyclobutyl 355 1 3-F-Phenyl cyclopentyl 356 1 3-F-Phenyl cyclohexyl 357 1 3-F-Phenyl 3-pyridyl 358 1 3-F-Phenyl 1-methyl-1H-pyrazol-4-yl 359 1 3-F-Phenyl 1H-imidazol-4-yl 360 1 3-F-Phenyl 2-furanyl 361 1 2-Cl-Phenyl Ethyl 362 1 2-Cl-Phenyl n-propyl 363 1 2-Cl-Phenyl Isopropyl 364 1 2-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 365 1 2-Cl-Phenyl CF.sub.3 366 1 2-Cl-Phenyl —CH.sub.2CF.sub.3 367 1 2-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 368 1 2-Cl-Phenyl cyclopropyl 369 1 2-Cl-Phenyl Cyclobutyl 370 1 2-Cl-Phenyl cyclopentyl 371 1 2-Cl-Phenyl cyclohexyl 372 1 2-Cl-Phenyl 3-pyridyl 373 1 2-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 374 1 2-Cl-Phenyl 1H-imidazol-4-yl 375 1 2-Cl-Phenyl 2-furanyl 376 1 4-Cl-Phenyl Ethyl 377 1 4-Cl-Phenyl n-propyl 378 1 4-Cl-Phenyl Isopropyl 379 1 4-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 380 1 4-Cl-Phenyl CF.sub.3 381 1 4-Cl-Phenyl —CH.sub.2CF.sub.3 382 1 4-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 383 1 4-Cl-Phenyl cyclopropyl 384 1 4-Cl-Phenyl Cyclobutyl 385 1 4-Cl-Phenyl cyclopentyl 386 1 4-Cl-Phenyl cyclohexyl 387 1 4-Cl-Phenyl 3-pyridyl 388 1 4-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 389 1 4-Cl-Phenyl 1H-imidazol-4-yl 390 1 4-Cl-Phenyl 2-furanyl 391 1 3-Br-Phenyl Ethyl 392 1 3-Br-Phenyl n-propyl 393 1 3-Br-Phenyl Isopropyl 394 1 3-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 395 1 3-Br-Phenyl CF.sub.3 396 1 3-Br-Phenyl —CH.sub.2CF.sub.3 397 1 3-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 398 1 3-Br-Phenyl cyclopropyl 399 1 3-Br-Phenyl Cyclobutyl 400 1 3-Br-Phenyl cyclopentyl 401 1 3-Br-Phenyl cyclohexyl 402 1 3-Br-Phenyl 3-pyridyl 403 1 3-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 404 1 3-Br-Phenyl 1H-imidazol-4-yl 405 1 3-Br-Phenyl 2-furanyl 406 1 2-CF.sub.3-Phenyl Ethyl 407 1 2-CF.sub.3-Phenyl n-propyl 408 1 2-CF.sub.3-Phenyl Isopropyl 409 1 2-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 410 1 2-CF.sub.3-Phenyl CF.sub.3 411 1 2-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 412 1 2-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 413 1 2-CF.sub.3-Phenyl cyclopropyl 414 1 2-CF.sub.3-Phenyl Cyclobutyl 415 1 2-CF.sub.3-Phenyl cyclopentyl 416 1 2-CF.sub.3-Phenyl cyclohexyl 417 1 2-CF.sub.3-Phenyl 3-pyridyl 418 1 2-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 419 1 2-CF.sub.3-Phenyl 1H-imidazol-4-yl 420 1 2-CF.sub.3-Phenyl 2-furanyl 421 1 4-CF.sub.3-Phenyl Ethyl 422 1 4-CF.sub.3-Phenyl n-propyl 423 1 4-CF.sub.3-Phenyl Isopropyl 424 1 4-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 425 1 4-CF.sub.3-Phenyl CF.sub.3 426 1 4-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 427 1 4-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 428 1 4-CF.sub.3-Phenyl cyclopropyl 429 1 4-CF.sub.3-Phenyl Cyclobutyl 430 1 4-CF.sub.3-Phenyl cyclopentyl 431 1 4-CF.sub.3-Phenyl cyclohexyl 432 1 4-CF.sub.3-Phenyl 3-pyridyl 433 1 4-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 434 1 4-CF.sub.3-Phenyl 1H-imidazol-4-yl 435 1 4-CF.sub.3-Phenyl 2-furanyl 436 1 3-iPr-Phenyl Ethyl 437 1 3-iPr-Phenyl n-propyl 438 1 3-iPr-Phenyl Isopropyl 439 1 3-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 440 1 3-iPr-Phenyl CF.sub.3 441 1 3-iPr-Phenyl —CH.sub.2CF.sub.3 442 1 3-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 443 1 3-iPr-Phenyl cyclopropyl 444 1 3-iPr-Phenyl Cyclobutyl 445 1 3-iPr-Phenyl cyclopentyl 446 1 3-iPr-Phenyl cyclohexyl 447 1 3-iPr-Phenyl 3-pyridyl 448 1 3-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 449 1 3-iPr-Phenyl 1H-imidazol-4-yl 450 1 3-iPr-Phenyl 2-furanyl 451 1 2-morpholino-phenyl Ethyl 452 1 2-morpholino-phenyl n-propyl 453 1 2-morpholino-phenyl isopropyl 454 1 2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 455 1 2-morpholino-phenyl CF.sub.3 456 1 2-morpholino-phenyl —CH.sub.2CF.sub.3 457 1 2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 458 1 2-morpholino-phenyl cyclopropyl 459 1 2-morpholino-phenyl Cyclobutyl 460 1 2-morpholino-phenyl cyclopentyl 461 1 2-morpholino-phenyl cyclohexyl 462 1 2-morpholino-phenyl 3-pyridyl 463 1 2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 464 1 2-morpholino-phenyl 1H-imidazol-4-yl 465 1 2-morpholino-phenyl 2-furanyl 466 1 4-morpholino-phenyl ethyl 467 1 4-morpholino-phenyl n-propyl 468 1 4-morpholino-phenyl isopropyl 469 1 4-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 470 1 4-morpholino-phenyl CF.sub.3 471 1 4-morpholino-phenyl —CH.sub.2CF.sub.3 472 1 4-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 473 1 4-morpholino-phenyl cyclopropyl 474 1 4-morpholino-phenyl Cyclobutyl 475 1 4-morpholino-phenyl cyclopentyl 476 1 4-morpholino-phenyl cyclohexyl 477 1 4-morpholino-phenyl 3-pyridyl 478 1 4-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 479 1 4-morpholino-phenyl 1H-imidazol-4-yl 480 1 4-morpholino-phenyl 2-furanyl 481 1 4-methyl-2-morpholino-phenyl ethyl 482 1 4-methyl-2-morpholino-phenyl n-propyl 483 1 4-methyl-2-morpholino-phenyl isopropyl 484 1 4-methyl-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 485 1 4-methyl-2-morpholino-phenyl CF.sub.3 486 1 4-methyl-2-morpholino-phenyl —CH.sub.2CF.sub.3 487 1 4-methyl-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 488 1 4-methyl-2-morpholino-phenyl cyclopropyl 489 1 4-methyl-2-morpholino-phenyl Cyclobutyl 490 1 4-methyl-2-morpholino-phenyl cyclopentyl 491 1 4-methyl-2-morpholino-phenyl cyclohexyl 492 1 4-methyl-2-morpholino-phenyl 3-pyridyl 493 1 4-methyl-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 494 1 4-methyl-2-morpholino-phenyl 1H-imidazol-4-yl 495 1 4-methyl-2-morpholino-phenyl 2-furanyl 496 2 4-CH.sub.3-phenyl ethyl 497 2 4-CH.sub.3-phenyl n-propyl 498 2 4-CH.sub.3-phenyl isopropyl 499 2 4-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 500 2 4-CH.sub.3-phenyl CF.sub.3 501 2 4-CH.sub.3-phenyl —CH.sub.2CF.sub.3 502 2 4-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 503 2 4-CH.sub.3-phenyl cyclopropyl 504 2 4-CH.sub.3-phenyl Cyclobutyl 505 2 4-CH.sub.3-phenyl cyclopentyl 506 2 4-CH.sub.3-phenyl cyclohexyl 507 2 4-CH.sub.3-phenyl 3-pyridyl 508 2 4-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 509 2 4-CH.sub.3-phenyl 1H-imidazol-4-yl 510 2 4-CH.sub.3-phenyl 2-furanyl 511 2 3-CH.sub.3-phenyl ethyl 512 2 3-CH.sub.3-phenyl n-propyl 513 2 3-CH.sub.3-phenyl isopropyl 514 2 3-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 515 2 3-CH.sub.3-phenyl CF.sub.3 516 2 3-CH.sub.3-phenyl —CH.sub.2CF.sub.3 517 2 3-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 518 2 3-CHs-phenyl cyclopropyl 519 2 3-CH.sub.3-phenyl Cyclobutyl 520 2 3-CH.sub.3-phenyl cyclopentyl 521 2 3-CH.sub.3-phenyl cyclohexyl 522 2 3-CH.sub.3-phenyl 3-pyridyl 523 2 3-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 524 2 3-CH.sub.3-phenyl 1H-imidazol-4-yl 525 2 3-CH.sub.3-phenyl 2-furanyl 526 2 3-OH-Phenyl ethyl 527 2 3-OH-Phenyl n-propyl 528 2 3-OH-Phenyl isopropyl 529 2 3-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 530 2 3-OH-Phenyl CF.sub.3 531 2 3-OH-Phenyl —CH.sub.2CF.sub.3 532 2 3-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 533 2 3-OH-Phenyl cyclopropyl 534 2 3-OH-Phenyl Cyclobutyl 535 2 3-OH-Phenyl cyclopentyl 536 2 3-OH-Phenyl cyclohexyl 537 2 3-OH-Phenyl 3-pyridyl 538 2 3-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 539 2 3-OH-Phenyl 1H-imidazol-4-yl 540 2 3-OH-Phenyl 2-furanyl 541 2 4-OMe-Phenyl ethyl 542 2 4-OMe-Phenyl n-propyl 543 2 4-OMe-Phenyl isopropyl 544 2 4-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 545 2 4-OMe-Phenyl CF.sub.3 546 2 4-OMe-Phenyl —CH.sub.2CF.sub.3 547 2 4-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 548 2 4-OMe-Phenyl cyclopropyl 549 2 4-OMe-Phenyl Cyclobutyl 550 2 4-OMe-Phenyl cyclopentyl 551 2 4-OMe-Phenyl cyclohexyl 552 2 4-OMe-Phenyl 3-pyridyl 553 2 4-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 554 2 4-OMe-Phenyl 1H-imidazol-4-yl 555 2 4-OMe-Phenyl 2-furanyl 556 2 2-OMe-Phenyl ethyl 557 2 2-OMe-Phenyl n-propyl 558 2 2-OMe-Phenyl isopropyl 559 2 2-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 560 2 2-OMe-Phenyl CF.sub.3 561 2 2-OMe-Phenyl —CH.sub.2CF.sub.3 562 2 2-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 563 2 2-OMe-Phenyl cyclopropyl 564 2 2-OMe-Phenyl Cyclobutyl 565 2 2-OMe-Phenyl cyclopentyl 566 2 2-OMe-Phenyl cyclohexyl 567 2 2-OMe-Phenyl 3-pyridyl 568 2 2-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 569 2 2-OMe-Phenyl 1H-imidazol-4-yl 570 2 2-OMe-Phenyl 2-furanyl 571 2 3-CN-Phenyl ethyl 572 2 3-CN-Phenyl n-propyl 573 2 3-CN-Phenyl isopropyl 574 2 3-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 575 2 3-CN-Phenyl CF.sub.3 576 2 3-CN-Phenyl —CH.sub.2CF.sub.3 577 2 3-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 578 2 3-CN-Phenyl cyclopropyl 579 2 3-CN-Phenyl Cyclobutyl 580 2 3-CN-Phenyl cyclopentyl 581 2 3-CN-Phenyl cyclohexyl 582 2 3-CN-Phenyl 3-pyridyl 583 2 3-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 584 2 3-CN-Phenyl 1H-imidazol-4-yl 585 2 3-CN-Phenyl 2-furanyl 586 2 2-F-Phenyl ethyl 587 2 2-F-Phenyl n-propyl 588 2 2-F-Phenyl isopropyl 589 2 2-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 590 2 2-F-Phenyl CF.sub.3 591 2 2-F-Phenyl —CH.sub.2CF.sub.3 592 2 2-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 593 2 2-F-Phenyl cyclopropyl 594 2 2-F-Phenyl Cyclobutyl 595 2 2-F-Phenyl cyclopentyl 596 2 2-F-Phenyl cyclohexyl 597 2 2-F-Phenyl 3-pyridyl 598 2 2-F-Phenyl 1-methyl-1H-pyrazol-4-yl 599 2 2-F-Phenyl 1H-imidazol-4-yl 600 2 2-F-Phenyl 2-furanyl 601 2 4-F-Phenyl ethyl 602 2 4-F-Phenyl n-propyl 603 2 4-F-Phenyl isopropyl 604 2 4-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 605 2 4-F-Phenyl CF.sub.3 606 2 4-F-Phenyl —CH.sub.2CF.sub.3 607 2 4-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 608 2 4-F-Phenyl cyclopropyl 609 2 4-F-Phenyl Cyclobutyl 610 2 4-F-Phenyl cyclopentyl 611 2 4-F-Phenyl cyclohexyl 612 2 4-F-Phenyl 3-pyridyl 613 2 4-F-Phenyl 1-methyl-1H-pyrazol-4-yl 614 2 4-F-Phenyl 1H-imidazol-4-yl 615 2 4-F-Phenyl 2-furanyl 616 2 3-Cl-Phenyl ethyl 617 2 3-Cl-Phenyl n-propyl 618 2 3-Cl-Phenyl isopropyl 619 2 3-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 620 2 3-Cl-Phenyl CF.sub.3 621 2 3-Cl-Phenyl —CH.sub.2CF.sub.3 622 2 3-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 623 2 3-Cl-Phenyl cyclopropyl 624 2 3-Cl-Phenyl Cyclobutyl 625 2 3-Cl-Phenyl cyclopentyl 626 2 3-Cl-Phenyl cyclohexyl 627 2 3-Cl-Phenyl 3-pyridyl 628 2 3-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 629 2 3-Cl-Phenyl 1H-imidazol-4-yl 630 2 3-Cl-Phenyl 2-furanyl 631 2 2-Br-Phenyl ethyl 632 2 2-Br-Phenyl n-propyl 633 2 2-Br-Phenyl isopropyl 634 2 2-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 635 2 2-Br-Phenyl CF.sub.3 636 2 2-Br-Phenyl —CH.sub.2CF.sub.3 637 2 2-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 638 2 2-Br-Phenyl cyclopropyl 639 2 2-Br-Phenyl Cyclobutyl 640 2 2-Br-Phenyl cyclopentyl 641 2 2-Br-Phenyl cyclohexyl 642 2 2-Br-Phenyl 3-pyridyl 643 2 2-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 644 2 2-Br-Phenyl 1H-imidazol-4-yl 645 2 2-Br-Phenyl 2-furanyl 646 2 4-Br-Phenyl ethyl 647 2 4-Br-Phenyl n-propyl 648 2 4-Br-Phenyl isopropyl 649 2 4-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 650 2 4-Br-Phenyl CF.sub.3 651 2 4-Br-Phenyl —CH.sub.2CF.sub.3 652 2 4-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 653 2 4-Br-Phenyl cyclopropyl 654 2 4-Br-Phenyl Cyclobutyl 655 2 4-Br-Phenyl cyclopentyl 656 2 4-Br-Phenyl cyclohexyl 657 2 4-Br-Phenyl 3-pyridyl 658 2 4-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 659 2 4-Br-Phenyl 1H-imidazol-4-yl 660 2 4-Br-Phenyl 2-furanyl 661 2 3-CF.sub.3-Phenyl ethyl 662 2 3-CF.sub.3-Phenyl n-propyl 663 2 3-CF.sub.3-Phenyl isopropyl 664 2 3-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 665 2 3-CF.sub.3-Phenyl CF.sub.3 666 2 3-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 667 2 3-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 668 2 3-CF.sub.3-Phenyl cyclopropyl 669 2 3-CF.sub.3-Phenyl Cyclobutyl 670 2 3-CF.sub.3-Phenyl cyclopentyl 671 2 3-CF.sub.3-Phenyl cyclohexyl 672 2 3-CF.sub.3-Phenyl 3-pyridyl 673 2 3-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 674 2 3-CF.sub.3-Phenyl 1H-imidazol-4-yl 675 2 3-CF.sub.3-Phenyl 2-furanyl 676 2 2-iPr-Phenyl ethyl 677 2 2-iPr-Phenyl n-propyl 678 2 2-iPr-Phenyl isopropyl 679 2 2-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 680 2 2-iPr-Phenyl CF.sub.3 681 2 2-iPr-Phenyl —CH.sub.2CF.sub.3 682 2 2-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 683 2 2-iPr-Phenyl cyclopropyl 684 2 2-iPr-Phenyl Cyclobutyl 685 2 2-iPr-Phenyl cyclopentyl 686 2 2-iPr-Phenyl cyclohexyl 687 2 2-iPr-Phenyl 3-pyridyl 688 2 2-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 689 2 2-iPr-Phenyl 1H-imidazol-4-yl 690 2 2-iPr-Phenyl 2-furanyl 691 2 4-iPr-Phenyl ethyl 692 2 4-iPr-Phenyl n-propyl 693 2 4-iPr-Phenyl isopropyl 694 2 4-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 695 2 4-iPr-Phenyl CF.sub.3 696 2 4-iPr-Phenyl —CH.sub.2CF.sub.3 697 2 4-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 698 2 4-iPr-Phenyl cyclopropyl 699 2 4-iPr-Phenyl Cyclobutyl 700 2 4-iPr-Phenyl cyclopentyl 701 2 4-iPr-Phenyl cyclohexyl 702 2 4-iPr-Phenyl 3-pyridyl 703 2 4-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 704 2 4-iPr-Phenyl 1H-imidazol-4-yl 705 2 4-iPr-Phenyl 2-furanyl 706 2 3-morpholino-phenyl ethyl 707 2 3-morpholino-phenyl n-propyl 708 2 3-morpholino-phenyl isopropyl 709 2 3-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 710 2 3-morpholino-phenyl CF.sub.3 711 2 3-morpholino-phenyl —CH.sub.2CF.sub.3 712 2 3-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 713 2 3-morpholino-phenyl cyclopropyl 714 2 3-morpholino-phenyl Cyclobutyl 715 2 3-morpholino-phenyl cyclopentyl 716 2 3-morpholino-phenyl cyclohexyl 717 2 3-morpholino-phenyl 3-pyridyl 718 2 3-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 719 2 3-morpholino-phenyl 1H-imidazol-4-yl 720 2 3-morpholino-phenyl 2-furanyl 721 2 4-cyano-2-morpholino-phenyl ethyl 722 2 4-cyano-2-morpholino-phenyl n-propyl 723 2 4-cyano-2-morpholino-phenyl isopropyl 724 2 4-cyano-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 725 2 4-cyano-2-morpholino-phenyl CF.sub.3 726 2 4-cyano-2-morpholino-phenyl —CH.sub.2CF.sub.3 727 2 4-cyano-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 728 2 4-cyano-2-morpholino-phenyl cyclopropyl 729 2 4-cyano-2-morpholino-phenyl Cyclobutyl 730 2 4-cyano-2-morpholino-phenyl cyclopentyl 731 2 4-cyano-2-morpholino-phenyl cyclohexyl 732 2 4-cyano-2-morpholino-phenyl 3-pyridyl 733 2 4-cyano-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 734 2 4-cyano-2-morpholino-phenyl 1H-imidazol-4-yl 735 2 4-cyano-2-morpholino-phenyl 2-furanyl 736 2 4-hydroxy-2-morpholino-phenyl ethyl 737 2 4-hydroxy-2-morpholino-phenyl n-propyl 738 2 4-hydroxy-2-morpholino-phenyl isopropyl 739 2 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 740 2 4-hydroxy-2-morpholino-phenyl CF.sub.3 741 2 4-hydroxy-2-morpholino-phenyl —CH.sub.2CF.sub.3 742 2 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 743 2 4-hydroxy-2-morpholino-phenyl cyclopropyl 744 2 4-hydroxy-2-morpholino-phenyl Cyclobutyl 745 2 4-hydroxy-2-morpholino-phenyl cyclopentyl 746 2 4-hydroxy-2-morpholino-phenyl cyclohexyl 747 2 4-hydroxy-2-morpholino-phenyl 3-pyridyl 748 2 4-hydroxy-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 749 2 4-hydroxy-2-morpholino-phenyl 1H-imidazol-4-yl 750 2 4-hydroxy-2-morpholino-phenyl 2-furanyl 751 2 2-CH.sub.3-phenyl Ethyl 752 2 2-CH.sub.3-phenyl n-propyl 753 2 2-CH.sub.3-phenyl Isopropyl 754 2 2-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 755 2 2-CH.sub.3-phenyl CF.sub.3 756 2 2-CH.sub.3-phenyl —CH.sub.2CF.sub.3 757 2 2-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 758 2 2-CH.sub.3-phenyl cyclopropyl 759 2 2-CH.sub.3-phenyl Cyclobutyl 760 2 2-CH.sub.3-phenyl cyclopentyl 761 2 2-CH.sub.3-phenyl cyclohexyl 762 2 2-CH.sub.3-phenyl 3-pyridyl 763 2 2-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 764 2 2-CH.sub.3-phenyl 1H-imidazol-4-yl 765 2 2-CH.sub.3-phenyl 2-furanyl 766 2 4-OH-Phenyl Ethyl 767 2 4-OH-Phenyl n-propyl 768 2 4-OH-Phenyl Isopropyl 769 2 4-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 770 2 4-OH-Phenyl CF.sub.3 771 2 4-OH-Phenyl —CH.sub.2CF.sub.3 772 2 4-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 773 2 4-OH-Phenyl cyclopropyl 774 2 4-OH-Phenyl Cyclobutyl 775 2 4-OH-Phenyl cyclopentyl 776 2 4-OH-Phenyl cyclohexyl 777 2 4-OH-Phenyl 3-pyridyl 778 2 4-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 779 2 4-OH-Phenyl 1H-imidazol-4-yl 780 2 4-OH-Phenyl 2-furanyl 781 2 2-OH-Phenyl Ethyl 782 2 2-OH-Phenyl n-propyl 783 2 2-OH-Phenyl Isopropyl 784 2 2-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 785 2 2-OH-Phenyl CF.sub.3 786 2 2-OH-Phenyl —CH.sub.2CF.sub.3 787 2 2-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 788 2 2-OH-Phenyl cyclopropyl 789 2 2-OH-Phenyl Cyclobutyl 790 2 2-OH-Phenyl cyclopentyl 791 2 2-OH-Phenyl cyclohexyl 792 2 2-OH-Phenyl 3-pyridyl 793 2 2-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 794 2 2-OH-Phenyl 1H-imidazol-4-yl 795 2 2-OH-Phenyl 2-furanyl 796 2 3-OMe-Phenyl Ethyl 797 2 3-OMe-Phenyl n-propyl 798 2 3-OMe-Phenyl Isopropyl 799 2 3-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 800 2 3-OMe-Phenyl CF.sub.3 801 2 3-OMe-Phenyl —CH.sub.2CF.sub.3 802 2 3-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 803 2 3-OMe-Phenyl cyclopropyl 804 2 3-OMe-Phenyl Cyclobutyl 805 2 3-OMe-Phenyl cyclopentyl 806 2 3-OMe-Phenyl cyclohexyl 807 2 3-OMe-Phenyl 3-pyridyl 808 2 3-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 809 2 3-OMe-Phenyl 1H-imidazol-4-yl 810 2 3-OMe-Phenyl 2-furanyl 811 2 4-CN-Phenyl Ethyl 812 2 4-CN-Phenyl n-propyl 813 2 4-CN-Phenyl Isopropyl 814 2 4-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 815 2 4-CN-Phenyl CF.sub.3 816 2 4-CN-Phenyl —CH.sub.2CF.sub.3 817 2 4-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 818 2 4-CN-Phenyl cyclopropyl 819 2 4-CN-Phenyl Cyclobutyl 820 2 4-CN-Phenyl cyclopentyl 821 2 4-CN-Phenyl cyclohexyl 822 2 4-CN-Phenyl 3-pyridyl 823 2 4-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 824 2 4-CN-Phenyl 1H-imidazol-4-yl 825 2 4-CN-Phenyl 2-furanyl 826 2 2-CN-Phenyl Ethyl 827 2 2-CN-Phenyl n-propyl 828 2 2-CN-Phenyl Isopropyl 829 2 2-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 830 2 2-CN-Phenyl CF.sub.3 831 2 2-CN-Phenyl —CH.sub.2CF.sub.3 832 2 2-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 833 2 2-CN-Phenyl cyclopropyl 834 2 2-CN-Phenyl Cyclobutyl 835 2 2-CN-Phenyl cyclopentyl 836 2 2-CN-Phenyl cyclohexyl 837 2 2-CN-Phenyl 3-pyridyl 838 2 2-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 839 2 2-CN-Phenyl 1H-imidazol-4-yl 840 2 2-CN-Phenyl 2-furanyl 841 2 3-F-Phenyl Ethyl 842 2 3-F-Phenyl n-propyl 843 2 3-F-Phenyl Isopropyl 844 2 3-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 845 2 3-F-Phenyl CF.sub.3 846 2 3-F-Phenyl —CH.sub.2CF.sub.3 847 2 3-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 848 2 3-F-Phenyl cyclopropyl 849 2 3-F-Phenyl Cyclobutyl 850 2 3-F-Phenyl cyclopentyl 851 2 3-F-Phenyl cyclohexyl 852 2 3-F-Phenyl 3-pyridyl 853 2 3-F-Phenyl 1-methyl-1H-pyrazol-4-yl 854 2 3-F-Phenyl 1H-imidazol-4-yl 855 2 3-F-Phenyl 2-furanyl 856 2 2-Cl-Phenyl Ethyl 857 2 2-Cl-Phenyl n-propyl 858 2 2-Cl-Phenyl Isopropyl 859 2 2-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 860 2 2-Cl-Phenyl CF.sub.3 861 2 2-Cl-Phenyl —CH.sub.2CF.sub.3 862 2 2-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 863 2 2-Cl-Phenyl cyclopropyl 864 2 2-Cl-Phenyl Cyclobutyl 865 2 2-Cl-Phenyl cyclopentyl 866 2 2-Cl-Phenyl cyclohexyl 867 2 2-Cl-Phenyl 3-pyridyl 868 2 2-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 869 2 2-Cl-Phenyl 1H-imidazol-4-yl 870 2 2-Cl-Phenyl 2-furanyl 871 2 4-Cl-Phenyl Ethyl 872 2 4-Cl-Phenyl n-propyl 873 2 4-Cl-Phenyl Isopropyl 874 2 4-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 875 2 4-Cl-Phenyl CF.sub.3 876 2 4-Cl-Phenyl —CH.sub.2CF.sub.3 877 2 4-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 878 2 4-Cl-Phenyl cyclopropyl 879 2 4-Cl-Phenyl Cyclobutyl 880 2 4-Cl-Phenyl cyclopentyl 881 2 4-Cl-Phenyl cyclohexyl 882 2 4-Cl-Phenyl 3-pyridyl 883 2 4-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 884 2 4-Cl-Phenyl 1H-imidazol-4-yl 885 2 4-Cl-Phenyl 2-furanyl 886 2 3-Br-Phenyl Ethyl 887 2 3-Br-Phenyl n-propyl 888 2 3-Br-Phenyl Isopropyl 889 2 3-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 890 2 3-Br-Phenyl CF.sub.3 891 2 3-Br-Phenyl —CH.sub.2CF.sub.3 892 2 3-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 893 2 3-Br-Phenyl cyclopropyl 894 2 3-Br-Phenyl Cyclobutyl 895 2 3-Br-Phenyl cyclopentyl 896 2 3-Br-Phenyl cyclohexyl 897 2 3-Br-Phenyl 3-pyridyl 898 2 3-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 899 2 3-Br-Phenyl 1H-imidazol-4-yl 900 2 3-Br-Phenyl 2-furanyl 901 2 2-CF.sub.3-Phenyl Ethyl 902 2 2-CF.sub.3-Phenyl n-propyl 903 2 2-CF.sub.3-Phenyl Isopropyl 904 2 2-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 905 2 2-CF.sub.3-Phenyl CF.sub.3 906 2 2-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 907 2 2-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 908 2 2-CF.sub.3-Phenyl cyclopropyl 909 2 2-CF.sub.3-Phenyl Cyclobutyl 910 2 2-CF.sub.3-Phenyl cyclopentyl 911 2 2-CF.sub.3-Phenyl cyclohexyl 912 2 2-CF.sub.3-Phenyl 3-pyridyl 913 2 2-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 914 2 2-CF.sub.3-Phenyl 1H-imidazol-4-yl 915 2 2-CF.sub.3-Phenyl 2-furanyl 916 2 4-CF.sub.3-Phenyl Ethyl 917 2 4-CF.sub.3-Phenyl n-propyl 918 2 4-CF.sub.3-Phenyl Isopropyl 919 2 4-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 920 2 4-CF.sub.3-Phenyl CF.sub.3 921 2 4-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 922 2 4-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 923 2 4-CF.sub.3-Phenyl cyclopropyl 924 2 4-CF.sub.3-Phenyl Cyclobutyl 925 2 4-CF.sub.3-Phenyl cyclopentyl 926 2 4-CF.sub.3-Phenyl cyclohexyl 927 2 4-CF.sub.3-Phenyl 3-pyridyl 928 2 4-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 929 2 4-CF.sub.3-Phenyl 1H-imidazol-4-yl 930 2 4-CF.sub.3-Phenyl 2-furanyl 931 2 3-iPr-Phenyl Ethyl 932 2 3-iPr-Phenyl n-propyl 933 2 3-iPr-Phenyl Isopropyl 934 2 3-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 935 2 3-iPr-Phenyl CF.sub.3 936 2 3-iPr-Phenyl —CH.sub.2CF.sub.3 937 2 3-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 938 2 3-iPr-Phenyl cyclopropyl 939 2 3-iPr-Phenyl Cyclobutyl 940 2 3-iPr-Phenyl cyclopentyl 941 2 3-iPr-Phenyl cyclohexyl 942 2 3-iPr-Phenyl 3-pyridyl 943 2 3-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 944 2 3-iPr-Phenyl 1H-imidazol-4-yl 945 2 3-iPr-Phenyl 2-furanyl 946 2 2-morpholino-phenyl Ethyl 947 2 2-morpholino-phenyl n-propyl 948 2 2-morpholino-phenyl isopropyl 949 2 2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 950 2 2-morpholino-phenyl CF.sub.3 951 2 2-morpholino-phenyl —CH.sub.2CF.sub.3 952 2 2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 953 2 2-morpholino-phenyl cyclopropyl 954 2 2-morpholino-phenyl Cyclobutyl 955 2 2-morpholino-phenyl cyclopentyl 956 2 2-morpholino-phenyl cyclohexyl 957 2 2-morpholino-phenyl 3-pyridyl 958 2 2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 959 2 2-morpholino-phenyl 1H-imidazol-4-yl 960 2 2-morpholino-phenyl 2-furanyl 961 2 4-morpholino-phenyl ethyl 962 2 4-morpholino-phenyl n-propyl 963 2 4-morpholino-phenyl isopropyl 964 2 4-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 965 2 4-morpholino-phenyl CF.sub.3 966 2 4-morpholino-phenyl —CH.sub.2CF.sub.3 967 2 4-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 968 2 4-morpholino-phenyl cyclopropyl 969 2 4-morpholino-phenyl Cyclobutyl 970 2 4-morpholino-phenyl cyclopentyl 971 2 4-morpholino-phenyl cyclohexyl 972 2 4-morpholino-phenyl 3-pyridyl 973 2 4-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 974 2 4-morpholino-phenyl 1H-imidazol-4-yl 975 2 4-morpholino-phenyl 2-furanyl 976 2 4-methyl-2-morpholino-phenyl ethyl 977 2 4-methyl-2-morpholino-phenyl n-propyl 978 2 4-methyl-2-morpholino-phenyl isopropyl 979 2 4-methyl-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 980 2 4-methyl-2-morpholino-phenyl CF.sub.3 981 2 4-methyl-2-morpholino-phenyl —CH.sub.2CF.sub.3 982 2 4-methyl-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 983 2 4-methyl-2-morpholino-phenyl cyclopropyl 984 2 4-methyl-2-morpholino-phenyl Cyclobutyl 985 2 4-methyl-2-morpholino-phenyl cyclopentyl 986 2 4-methyl-2-morpholino-phenyl cyclohexyl 987 2 4-methyl-2-morpholino-phenyl 3-pyridyl 988 2 4-methyl-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 989 2 4-methyl-2-morpholino-phenyl 1H-imidazol-4-yl 990 2 4-methyl-2-morpholino-phenyl 2-furanyl 991 3 4-CH.sub.3-phenyl ethyl 992 3 4-CH.sub.3-phenyl n-propyl 993 3 4-CH.sub.3-phenyl isopropyl 994 3 4-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 995 3 4-CH.sub.3-phenyl CF.sub.3 996 3 4-CH.sub.3-phenyl —CH.sub.2CF.sub.3 997 3 4-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 998 3 4-CH.sub.3-phenyl cyclopropyl 999 3 4-CH.sub.3-phenyl Cyclobutyl 1000 3 4-CH.sub.3-phenyl cyclopentyl 1001 3 4-CH.sub.3-phenyl cyclohexyl 1002 3 4-CH.sub.3-phenyl 3-pyridyl 1003 3 4-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1004 3 4-CH.sub.3-phenyl 1H-imidazol-4-yl 1005 3 4-CH.sub.3-phenyl 2-furanyl 1006 3 3-CH.sub.3-phenyl ethyl 1007 3 3-CH.sub.3-phenyl n-propyl 1008 3 3-CH.sub.3-phenyl isopropyl 1009 3 3-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1010 3 3-CH.sub.3-phenyl CF.sub.3 1011 3 3-CH.sub.3-phenyl —CH.sub.2CF.sub.3 1012 3 3-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 1013 3 3-CH.sub.3-phenyl cyclopropyl 1014 3 3-CHs-phenyl Cyclobutyl 1015 3 3-CH.sub.3-phenyl cyclopentyl 1016 3 3-CH.sub.3-phenyl cyclohexyl 1017 3 3-CH.sub.3-phenyl 3-pyridyl 1018 3 3-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1019 3 3-CH.sub.3-phenyl 1H-imidazol-4-yl 1020 3 3-CH.sub.3-phenyl 2-furanyl 1021 3 3-OH-Phenyl ethyl 1022 3 3-OH-Phenyl n-propyl 1023 3 3-OH-Phenyl isopropyl 1024 3 3-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1025 3 3-OH-Phenyl CF.sub.3 1026 3 3-OH-Phenyl —CH.sub.2CF.sub.3 1027 3 3-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1028 3 3-OH-Phenyl cyclopropyl 1029 3 3-OH-Phenyl Cyclobutyl 1030 3 3-OH-Phenyl cyclopentyl 1031 3 3-OH-Phenyl cyclohexyl 1032 3 3-OH-Phenyl 3-pyridyl 1033 3 3-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1034 3 3-OH-Phenyl 1H-imidazol-4-yl 1035 3 3-OH-Phenyl 2-furanyl 1036 3 4-OMe-Phenyl ethyl 1037 3 4-OMe-Phenyl n-propyl 1038 3 4-OMe-Phenyl isopropyl 1039 3 4-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1040 3 4-OMe-Phenyl CF.sub.3 1041 3 4-OMe-Phenyl —CH.sub.2CF.sub.3 1042 3 4-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1043 3 4-OMe-Phenyl cyclopropyl 1044 3 4-OMe-Phenyl Cyclobutyl 1045 3 4-OMe-Phenyl cyclopentyl 1046 3 4-OMe-Phenyl cyclohexyl 1047 3 4-OMe-Phenyl 3-pyridyl 1048 3 4-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1049 3 4-OMe-Phenyl 1H-imidazol-4-yl 1050 3 4-OMe-Phenyl 2-furanyl 1051 3 2-OMe-Phenyl ethyl 1052 3 2-OMe-Phenyl n-propyl 1053 3 2-OMe-Phenyl isopropyl 1054 3 2-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1055 3 2-OMe-Phenyl CF.sub.3 1056 3 2-OMe-Phenyl —CH.sub.2CF.sub.3 1057 3 2-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1058 3 2-OMe-Phenyl cyclopropyl 1059 3 2-OMe-Phenyl Cyclobutyl 1060 3 2-OMe-Phenyl cyclopentyl 1061 3 2-OMe-Phenyl cyclohexyl 1062 3 2-OMe-Phenyl 3-pyridyl 1063 3 2-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1064 3 2-OMe-Phenyl 1H-imidazol-4-yl 1065 3 2-OMe-Phenyl 2-furanyl 1066 3 3-CN-Phenyl ethyl 1067 3 3-CN-Phenyl n-propyl 1068 3 3-CN-Phenyl isopropyl 1069 3 3-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1070 3 3-CN-Phenyl CF.sub.3 1071 3 3-CN-Phenyl —CH.sub.2CF.sub.3 1072 3 3-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1073 3 3-CN-Phenyl cyclopropyl 1074 3 3-CN-Phenyl Cyclobutyl 1075 3 3-CN-Phenyl cyclopentyl 1076 3 3-CN-Phenyl cyclohexyl 1077 3 3-CN-Phenyl 3-pyridyl 1078 3 3-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1079 3 3-CN-Phenyl 1H-imidazol-4-yl 1080 3 3-CN-Phenyl 2-furanyl 1081 3 2-F-Phenyl ethyl 1082 3 2-F-Phenyl n-propyl 1083 3 2-F-Phenyl isopropyl 1084 3 2-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1085 3 2-F-Phenyl CF.sub.3 1086 3 2-F-Phenyl —CH.sub.2CF.sub.3 1087 3 2-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1088 3 2-F-Phenyl cyclopropyl 1089 3 2-F-Phenyl Cyclobutyl 1090 3 2-F-Phenyl cyclopentyl 1091 3 2-F-Phenyl cyclohexyl 1092 3 2-F-Phenyl 3-pyridyl 1093 3 2-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1094 3 2-F-Phenyl 1H-imidazol-4-yl 1095 3 2-F-Phenyl 2-furanyl 1096 3 4-F-Phenyl ethyl 1097 3 4-F-Phenyl n-propyl 1098 3 4-F-Phenyl isopropyl 1099 3 4-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1100 3 4-F-Phenyl CF.sub.3 1101 3 4-F-Phenyl —CH.sub.2CF.sub.3 1102 3 4-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1103 3 4-F-Phenyl cyclopropyl 1104 3 4-F-Phenyl Cyclobutyl 1105 3 4-F-Phenyl cyclopentyl 1106 3 4-F-Phenyl cyclohexyl 1107 3 4-F-Phenyl 3-pyridyl 1108 3 4-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1109 3 4-F-Phenyl 1H-imidazol-4-yl 1110 3 4-F-Phenyl 2-furanyl 1111 3 3-Cl-Phenyl ethyl 1112 3 3-Cl-Phenyl n-propyl 1113 3 3-Cl-Phenyl isopropyl 1114 3 3-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1115 3 3-Cl-Phenyl CF.sub.3 1116 3 3-Cl-Phenyl —CH.sub.2CF.sub.3 1117 3 3-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1118 3 3-Cl-Phenyl cyclopropyl 1119 3 3-Cl-Phenyl Cyclobutyl 1120 3 3-Cl-Phenyl cyclopentyl 1121 3 3-Cl-Phenyl cyclohexyl 1122 3 3-Cl-Phenyl 3-pyridyl 1123 3 3-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1124 3 3-Cl-Phenyl 1H-imidazol-4-yl 1125 3 3-Cl-Phenyl 2-furanyl 1126 3 2-Br-Phenyl ethyl 1127 3 2-Br-Phenyl n-propyl 1128 3 2-Br-Phenyl isopropyl 1129 3 2-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1130 3 2-Br-Phenyl CF.sub.3 1131 3 2-Br-Phenyl —CH.sub.2CF.sub.3 1132 3 2-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1133 3 2-Br-Phenyl cyclopropyl 1134 3 2-Br-Phenyl Cyclobutyl 1135 3 2-Br-Phenyl cyclopentyl 1136 3 2-Br-Phenyl cyclohexyl 1137 3 2-Br-Phenyl 3-pyridyl 1138 3 2-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1139 3 2-Br-Phenyl 1H-imidazol-4-yl 1140 3 2-Br-Phenyl 2-furanyl 1141 3 4-Br-Phenyl ethyl 1142 3 4-Br-Phenyl n-propyl 1143 3 4-Br-Phenyl isopropyl 1144 3 4-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1145 3 4-Br-Phenyl CF.sub.3 1146 3 4-Br-Phenyl —CH.sub.2CF.sub.3 1147 3 4-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1148 3 4-Br-Phenyl cyclopropyl 1149 3 4-Br-Phenyl Cyclobutyl 1150 3 4-Br-Phenyl cyclopentyl 1151 3 4-Br-Phenyl cyclohexyl 1152 3 4-Br-Phenyl 3-pyridyl 1153 3 4-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1154 3 4-Br-Phenyl 1H-imidazol-4-yl 1155 3 4-Br-Phenyl 2-furanyl 1156 3 3-CF.sub.3-Phenyl ethyl 1157 3 3-CF.sub.3-Phenyl n-propyl 1158 3 3-CF.sub.3-Phenyl isopropyl 1159 3 3-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1160 3 3-CF.sub.3-Phenyl CF.sub.3 1161 3 3-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1162 3 3-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1163 3 3-CF.sub.3-Phenyl cyclopropyl 1164 3 3-CF.sub.3-Phenyl Cyclobutyl 1165 3 3-CF.sub.3-Phenyl cyclopentyl 1166 3 3-CF.sub.3-Phenyl cyclohexyl 1167 3 3-CF.sub.3-Phenyl 3-pyridyl 1168 3 3-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1169 3 3-CF.sub.3-Phenyl 1H-imidazol-4-yl 1170 3 3-CF.sub.3-Phenyl 2-furanyl 1171 3 2-iPr-Phenyl ethyl 1172 3 2-iPr-Phenyl n-propyl 1173 3 2-iPr-Phenyl isopropyl 1174 3 2-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1175 3 2-iPr-Phenyl CF.sub.3 1176 3 2-iPr-Phenyl —CH.sub.2CF.sub.3 1177 3 2-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1178 3 2-iPr-Phenyl cyclopropyl 1179 3 2-iPr-Phenyl Cyclobutyl 1180 3 2-iPr-Phenyl cyclopentyl 1181 3 2-iPr-Phenyl cyclohexyl 1182 3 2-iPr-Phenyl 3-pyridyl 1183 3 2-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1184 3 2-iPr-Phenyl 1H-imidazol-4-yl 1185 3 2-iPr-Phenyl 2-furanyl 1186 3 4-iPr-Phenyl ethyl 1187 3 4-iPr-Phenyl n-propyl 1188 3 4-iPr-Phenyl isopropyl 1189 3 4-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1190 3 4-iPr-Phenyl CF.sub.3 1191 3 4-iPr-Phenyl —CH.sub.2CF.sub.3 1192 3 4-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1193 3 4-iPr-Phenyl cyclopropyl 1194 3 4-iPr-Phenyl Cyclobutyl 1195 3 4-iPr-Phenyl cyclopentyl 1196 3 4-iPr-Phenyl cyclohexyl 1197 3 4-iPr-Phenyl 3-pyridyl 1198 3 4-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1199 3 4-iPr-Phenyl 1H-imidazol-4-yl 1200 3 4-iPr-Phenyl 2-furanyl 1201 3 3-morpholino-phenyl ethyl 1202 3 3-morpholino-phenyl n-propyl 1203 3 3-morpholino-phenyl isopropyl 1204 3 3-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1205 3 3-morpholino-phenyl CF.sub.3 1206 3 3-morpholino-phenyl —CH.sub.2CF.sub.3 1207 3 3-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1208 3 3-morpholino-phenyl cyclopropyl 1209 3 3-morpholino-phenyl Cyclobutyl 1210 3 3-morpholino-phenyl cyclopentyl 1211 3 3-morpholino-phenyl cyclohexyl 1212 3 3-morpholino-phenyl 3-pyridyl 1213 3 3-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1214 3 3-morpholino-phenyl 1H-imidazol-4-yl 1215 3 3-morpholino-phenyl 2-furanyl 1216 3 4-cyano-2-morpholino-phenyl ethyl 1217 3 4-cyano-2-morpholino-phenyl n-propyl 1218 3 4-cyano-2-morpholino-phenyl isopropyl 1219 3 4-cyano-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1220 3 4-cyano-2-morpholino-phenyl CF.sub.3 1221 3 4-cyano-2-morpholino-phenyl —CH.sub.2CF.sub.3 1222 3 4-cyano-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1223 3 4-cyano-2-morpholino-phenyl cyclopropyl 1224 3 4-cyano-2-morpholino-phenyl Cyclobutyl 1225 3 4-cyano-2-morpholino-phenyl cyclopentyl 1226 3 4-cyano-2-morpholino-phenyl cyclohexyl 1227 3 4-cyano-2-morpholino-phenyl 3-pyridyl 1228 3 4-cyano-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1229 3 4-cyano-2-morpholino-phenyl 1H-imidazol-4-yl 1230 3 4-cyano-2-morpholino-phenyl 2-furanyl 1231 3 4-hydroxy-2-morpholino-phenyl ethyl 1232 3 4-hydroxy-2-morpholino-phenyl n-propyl 1233 3 4-hydroxy-2-morpholino-phenyl isopropyl 1234 3 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1235 3 4-hydroxy-2-morpholino-phenyl CF.sub.3 1236 3 4-hydroxy-2-morpholino-phenyl —CH.sub.2CF.sub.3 1237 3 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1238 3 4-hydroxy-2-morpholino-phenyl cyclopropyl 1239 3 4-hydroxy-2-morpholino-phenyl Cyclobutyl 1240 3 4-hydroxy-2-morpholino-phenyl cyclopentyl 1241 3 4-hydroxy-2-morpholino-phenyl cyclohexyl 1242 3 4-hydroxy-2-morpholino-phenyl 3-pyridyl 1243 3 4-hydroxy-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1244 3 4-hydroxy-2-morpholino-phenyl 1H-imidazol-4-yl 1245 3 4-hydroxy-2-morpholino-phenyl 2-furanyl 1246 3 2-CH.sub.3-phenyl Ethyl 1247 3 2-CH.sub.3-phenyl n-propyl 1248 3 2-CH.sub.3-phenyl Isopropyl 1249 3 2-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1250 3 2-CH.sub.3-phenyl CF.sub.3 1251 3 2-CH.sub.3-phenyl —CH.sub.2CF.sub.3 1252 3 2-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 1253 3 2-CH.sub.3-phenyl cyclopropyl 1254 3 2-CH.sub.3-phenyl Cyclobutyl 1255 3 2-CH.sub.3-phenyl cyclopentyl 1256 3 2-CH.sub.3-phenyl cyclohexyl 1257 3 2-CH.sub.3-phenyl 3-pyridyl 1258 3 2-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1259 3 2-CH.sub.3-phenyl 1H-imidazol-4-yl 1260 3 2-CH.sub.3-phenyl 2-furanyl 1261 3 4-OH-Phenyl Ethyl 1262 3 4-OH-Phenyl n-propyl 1263 3 4-OH-Phenyl Isopropyl 1264 3 4-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1265 3 4-OH-Phenyl CF.sub.3 1266 3 4-OH-Phenyl —CH.sub.2CF.sub.3 1267 3 4-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1268 3 4-OH-Phenyl cyclopropyl 1269 3 4-OH-Phenyl Cyclobutyl 1270 3 4-OH-Phenyl cyclopentyl 1271 3 4-OH-Phenyl cyclohexyl 1272 3 4-OH-Phenyl 3-pyridyl 1273 3 4-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1274 3 4-OH-Phenyl 1H-imidazol-4-yl 1275 3 4-OH-Phenyl 2-furanyl 1276 3 2-OH-Phenyl Ethyl 1277 3 2-OH-Phenyl n-propyl 1278 3 2-OH-Phenyl Isopropyl 1279 3 2-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1280 3 2-OH-Phenyl CF.sub.3 1281 3 2-OH-Phenyl —CH.sub.2CF.sub.3 1282 3 2-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1283 3 2-OH-Phenyl cyclopropyl 1284 3 2-OH-Phenyl Cyclobutyl 1285 3 2-OH-Phenyl cyclopentyl 1286 3 2-OH-Phenyl cyclohexyl 1287 3 2-OH-Phenyl 3-pyridyl 1288 3 2-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1289 3 2-OH-Phenyl 1H-imidazol-4-yl 1290 3 2-OH-Phenyl 2-furanyl 1291 3 3-OMe-Phenyl Ethyl 1292 3 3-OMe-Phenyl n-propyl 1293 3 3-OMe-Phenyl Isopropyl 1294 3 3-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1295 3 3-OMe-Phenyl CF.sub.3 1296 3 3-OMe-Phenyl —CH.sub.2CF.sub.3 1297 3 3-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1298 3 3-OMe-Phenyl cyclopropyl 1299 3 3-OMe-Phenyl Cyclobutyl 1300 3 3-OMe-Phenyl cyclopentyl 1301 3 3-OMe-Phenyl cyclohexyl 1302 3 3-OMe-Phenyl 3-pyridyl 1303 3 3-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1304 3 3-OMe-Phenyl 1H-imidazol-4-yl 1305 3 3-OMe-Phenyl 2-furanyl 1306 3 4-CN-Phenyl Ethyl 1307 3 4-CN-Phenyl n-propyl 1308 3 4-CN-Phenyl Isopropyl 1309 3 4-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1310 3 4-CN-Phenyl CF.sub.3 1311 3 4-CN-Phenyl —CH.sub.2CF.sub.3 1312 3 4-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1313 3 4-CN-Phenyl cyclopropyl 1314 3 4-CN-Phenyl Cyclobutyl 1315 3 4-CN-Phenyl cyclopentyl 1316 3 4-CN-Phenyl cyclohexyl 1317 3 4-CN-Phenyl 3-pyridyl 1318 3 4-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1319 3 4-CN-Phenyl 1H-imidazol-4-yl 1320 3 4-CN-Phenyl 2-furanyl 1321 3 2-CN-Phenyl Ethyl 1322 3 2-CN-Phenyl n-propyl 1323 3 2-CN-Phenyl Isopropyl 1324 3 2-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1325 3 2-CN-Phenyl CF.sub.3 1326 3 2-CN-Phenyl —CH.sub.2CF.sub.3 1327 3 2-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1328 3 2-CN-Phenyl cyclopropyl 1329 3 2-CN-Phenyl Cyclobutyl 1330 3 2-CN-Phenyl cyclopentyl 1331 3 2-CN-Phenyl cyclohexyl 1332 3 2-CN-Phenyl 3-pyridyl 1333 3 2-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1334 3 2-CN-Phenyl 1H-imidazol-4-yl 1335 3 2-CN-Phenyl 2-furanyl 1336 3 3-F-Phenyl Ethyl 1337 3 3-F-Phenyl n-propyl 1338 3 3-F-Phenyl Isopropyl 1339 3 3-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1340 3 3-F-Phenyl CF.sub.3 1341 3 3-F-Phenyl —CH.sub.2CF.sub.3 1342 3 3-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1343 3 3-F-Phenyl cyclopropyl 1344 3 3-F-Phenyl Cyclobutyl 1345 3 3-F-Phenyl cyclopentyl 1346 3 3-F-Phenyl cyclohexyl 1347 3 3-F-Phenyl 3-pyridyl 1348 3 3-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1349 3 3-F-Phenyl 1H-imidazol-4-yl 1350 3 3-F-Phenyl 2-furanyl 1351 3 2-Cl-Phenyl Ethyl 1352 3 2-Cl-Phenyl n-propyl 1353 3 2-Cl-Phenyl Isopropyl 1354 3 2-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1355 3 2-Cl-Phenyl CF.sub.3 1356 3 2-Cl-Phenyl —CH.sub.2CF.sub.3 1357 3 2-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1358 3 2-Cl-Phenyl cyclopropyl 1359 3 2-Cl-Phenyl Cyclobutyl 1360 3 2-Cl-Phenyl cyclopentyl 1361 3 2-Cl-Phenyl cyclohexyl 1362 3 2-Cl-Phenyl 3-pyridyl 1363 3 2-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1364 3 2-Cl-Phenyl 1H-imidazol-4-yl 1365 3 2-Cl-Phenyl 2-furanyl 1366 3 4-Cl-Phenyl Ethyl 1367 3 4-Cl-Phenyl n-propyl 1368 3 4-Cl-Phenyl Isopropyl 1369 3 4-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1370 3 4-Cl-Phenyl CF.sub.3 1371 3 4-Cl-Phenyl —CH.sub.2CF.sub.3 1372 3 4-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1373 3 4-Cl-Phenyl cyclopropyl 1374 3 4-Cl-Phenyl Cyclobutyl 1375 3 4-Cl-Phenyl cyclopentyl 1376 3 4-Cl-Phenyl cyclohexyl 1377 3 4-Cl-Phenyl 3-pyridyl 1378 3 4-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1379 3 4-Cl-Phenyl 1H-imidazol-4-yl 1380 3 4-Cl-Phenyl 2-furanyl 1381 3 3-Br-Phenyl Ethyl 1382 3 3-Br-Phenyl n-propyl 1383 3 3-Br-Phenyl Isopropyl 1384 3 3-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1385 3 3-Br-Phenyl CF.sub.3 1386 3 3-Br-Phenyl —CH.sub.2CF.sub.3 1387 3 3-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1388 3 3-Br-Phenyl cyclopropyl 1389 3 3-Br-Phenyl Cyclobutyl 1390 3 3-Br-Phenyl cyclopentyl 1391 3 3-Br-Phenyl cyclohexyl 1392 3 3-Br-Phenyl 3-pyridyl 1393 3 3-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1394 3 3-Br-Phenyl 1H-imidazol-4-yl 1395 3 3-Br-Phenyl 2-furanyl 1396 3 2-CF.sub.3-Phenyl Ethyl 1397 3 2-CF.sub.3-Phenyl n-propyl 1398 3 2-CF.sub.3-Phenyl Isopropyl 1399 3 2-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1400 3 2-CF.sub.3-Phenyl CF.sub.3 1401 3 2-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1402 3 2-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1403 3 2-CF.sub.3-Phenyl cyclopropyl 1404 3 2-CF.sub.3-Phenyl Cyclobutyl 1405 3 2-CF.sub.3-Phenyl cyclopentyl 1406 3 2-CF.sub.3-Phenyl cyclohexyl 1407 3 2-CF.sub.3-Phenyl 3-pyridyl 1408 3 2-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1409 3 2-CF.sub.3-Phenyl 1H-imidazol-4-yl 1410 3 2-CF.sub.3-Phenyl 2-furanyl 1411 3 4-CF.sub.3-Phenyl Ethyl 1412 3 4-CF.sub.3-Phenyl n-propyl 1413 3 4-CF.sub.3-Phenyl Isopropyl 1414 3 4-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1415 3 4-CF.sub.3-Phenyl CF.sub.3 1416 3 4-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1417 3 4-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1418 3 4-CF.sub.3-Phenyl cyclopropyl 1419 3 4-CF.sub.3-Phenyl Cyclobutyl 1420 3 4-CF.sub.3-Phenyl cyclopentyl 1421 3 4-CF.sub.3-Phenyl cyclohexyl 1422 3 4-CF.sub.3-Phenyl 3-pyridyl 1423 3 4-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1424 3 4-CF.sub.3-Phenyl 1H-imidazol-4-yl 1425 3 4-CF.sub.3-Phenyl 2-furanyl 1426 3 3-iPr-Phenyl Ethyl 1427 3 3-iPr-Phenyl n-propyl 1428 3 3-iPr-Phenyl Isopropyl 1429 3 3-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1430 3 3-iPr-Phenyl CF.sub.3 1431 3 3-iPr-Phenyl —CH.sub.2CF.sub.3 1432 3 3-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1433 3 3-iPr-Phenyl cyclopropyl 1434 3 3-iPr-Phenyl Cyclobutyl 1435 3 3-iPr-Phenyl cyclopentyl 1436 3 3-iPr-Phenyl cyclohexyl 1437 3 3-iPr-Phenyl 3-pyridyl 1438 3 3-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1439 3 3-iPr-Phenyl 1H-imidazol-4-yl 1440 3 3-iPr-Phenyl 2-furanyl 1441 3 2-morpholino-phenyl Ethyl 1442 3 2-morpholino-phenyl n-propyl 1443 3 2-morpholino-phenyl isopropyl 1444 3 2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1445 3 2-morpholino-phenyl CF.sub.3 1446 3 2-morpholino-phenyl —CH.sub.2CF.sub.3 1447 3 2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1448 3 2-morpholino-phenyl cyclopropyl 1449 3 2-morpholino-phenyl Cyclobutyl 1450 3 2-morpholino-phenyl cyclopentyl 1451 3 2-morpholino-phenyl cyclohexyl 1452 3 2-morpholino-phenyl 3-pyridyl 1453 3 2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1454 3 2-morpholino-phenyl 1H-imidazol-4-yl 1455 3 2-morpholino-phenyl 2-furanyl 1456 3 4-morpholino-phenyl ethyl 1457 3 4-morpholino-phenyl n-propyl 1458 3 4-morpholino-phenyl isopropyl 1459 3 4-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1460 3 4-morpholino-phenyl CF.sub.3 1461 3 4-morpholino-phenyl —CH.sub.2CF.sub.3 1462 3 4-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1463 3 4-morpholino-phenyl cyclopropyl 1464 3 4-morpholino-phenyl Cyclobutyl 1465 3 4-morpholino-phenyl cyclopentyl 1466 3 4-morpholino-phenyl cyclohexyl 1467 3 4-morpholino-phenyl 3-pyridyl 1468 3 4-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1469 3 4-morpholino-phenyl 1H-imidazol-4-yl 1470 3 4-morpholino-phenyl 2-furanyl 1471 3 4-methyl-2-morpholino-phenyl ethyl 1472 3 4-methyl-2-morpholino-phenyl n-propyl 1473 3 4-methyl-2-morpholino-phenyl isopropyl 1474 3 4-methyl-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1475 3 4-methyl-2-morpholino-phenyl CF.sub.3 1476 3 4-methyl-2-morpholino-phenyl —CH.sub.2CF.sub.3 1477 3 4-methyl-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1478 3 4-methyl-2-morpholino-phenyl cyclopropyl 1479 3 4-methyl-2-morpholino-phenyl Cyclobutyl 1480 3 4-methyl-2-morpholino-phenyl cyclopentyl 1481 3 4-methyl-2-morpholino-phenyl cyclohexyl 1482 3 4-methyl-2-morpholino-phenyl 3-pyridyl 1483 3 4-methyl-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1484 3 4-methyl-2-morpholino-phenyl 1H-imidazol-4-yl 1485 3 4-methyl-2-morpholino-phenyl 2-furanyl 1486 4 4-CH.sub.3-phenyl ethyl 1487 4 4-CH.sub.3-phenyl n-propyl 1488 4 4-CH.sub.3-phenyl isopropyl 1489 4 4-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1490 4 4-CH.sub.3-phenyl CF.sub.3 1491 4 4-CH.sub.3-phenyl —CH.sub.2CF.sub.3 1492 4 4-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 1493 4 4-CH.sub.3-phenyl cyclopropyl 1494 4 4-CH.sub.3-phenyl Cyclobutyl 1495 4 4-CH.sub.3-phenyl cyclopentyl 1496 4 4-CH.sub.3-phenyl cyclohexyl 1497 4 4-CH.sub.3-phenyl 3-pyridyl 1498 4 4-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1499 4 4-CH.sub.3-phenyl 1H-imidazol-4-yl 1500 4 4-CH.sub.3-phenyl 2-furanyl 1501 4 3-CH.sub.3-phenyl ethyl 1502 4 3-CH.sub.3-phenyl n-propyl 1503 4 3-CH.sub.3-phenyl isopropyl 1504 4 3-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1505 4 3-CH.sub.3-phenyl CF.sub.3 1506 4 3-CH.sub.3-phenyl —CH.sub.2CF.sub.3 1507 4 3-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 1508 4 3-CH.sub.3-phenyl cyclopropyl 1509 4 3-CH.sub.3-phenyl Cyclobutyl 1510 4 3-CHs-phenyl cyclopentyl 1511 4 3-CH.sub.3-phenyl cyclohexyl 1512 4 3-CH.sub.3-phenyl 3-pyridyl 1513 4 3-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1514 4 3-CH.sub.3-phenyl 1H-imidazol-4-yl 1515 4 3-CH.sub.3-phenyl 2-furanyl 1516 4 3-OH-Phenyl ethyl 1517 4 3-OH-Phenyl n-propyl 1518 4 3-OH-Phenyl isopropyl 1519 4 3-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1520 4 3-OH-Phenyl CF.sub.3 1521 4 3-OH-Phenyl —CH.sub.2CF.sub.3 1522 4 3-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1523 4 3-OH-Phenyl cyclopropyl 1524 4 3-OH-Phenyl Cyclobutyl 1525 4 3-OH-Phenyl cyclopentyl 1526 4 3-OH-Phenyl cyclohexyl 1527 4 3-OH-Phenyl 3-pyridyl 1528 4 3-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1529 4 3-OH-Phenyl 1H-imidazol-4-yl 1530 4 3-OH-Phenyl 2-furanyl 1531 4 4-OMe-Phenyl ethyl 1532 4 4-OMe-Phenyl n-propyl 1533 4 4-OMe-Phenyl isopropyl 1534 4 4-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1535 4 4-OMe-Phenyl CF.sub.3 1536 4 4-OMe-Phenyl —CH.sub.2CF.sub.3 1537 4 4-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1538 4 4-OMe-Phenyl cyclopropyl 1539 4 4-OMe-Phenyl Cyclobutyl 1540 4 4-OMe-Phenyl cyclopentyl 1541 4 4-OMe-Phenyl cyclohexyl 1542 4 4-OMe-Phenyl 3-pyridyl 1543 4 4-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1544 4 4-OMe-Phenyl 1H-imidazol-4-yl 1545 4 4-OMe-Phenyl 2-furanyl 1546 4 2-OMe-Phenyl ethyl 1547 4 2-OMe-Phenyl n-propyl 1548 4 2-OMe-Phenyl isopropyl 1549 4 2-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1550 4 2-OMe-Phenyl CF.sub.3 1551 4 2-OMe-Phenyl —CH.sub.2CF.sub.3 1552 4 2-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1553 4 2-OMe-Phenyl cyclopropyl 1554 4 2-OMe-Phenyl Cyclobutyl 1555 4 2-OMe-Phenyl cyclopentyl 1556 4 2-OMe-Phenyl cyclohexyl 1557 4 2-OMe-Phenyl 3-pyridyl 1558 4 2-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1559 4 2-OMe-Phenyl 1H-imidazol-4-yl 1560 4 2-OMe-Phenyl 2-furanyl 1561 4 3-CN-Phenyl ethyl 1562 4 3-CN-Phenyl n-propyl 1563 4 3-CN-Phenyl isopropyl 1564 4 3-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1565 4 3-CN-Phenyl CF.sub.3 1566 4 3-CN-Phenyl —CH.sub.2CF.sub.3 1567 4 3-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1568 4 3-CN-Phenyl cyclopropyl 1569 4 3-CN-Phenyl Cyclobutyl 1570 4 3-CN-Phenyl cyclopentyl 1571 4 3-CN-Phenyl cyclohexyl 1572 4 3-CN-Phenyl 3-pyridyl 1573 4 3-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1574 4 3-CN-Phenyl 1H-imidazol-4-yl 1575 4 3-CN-Phenyl 2-furanyl 1576 4 2-F-Phenyl ethyl 1577 4 2-F-Phenyl n-propyl 1578 4 2-F-Phenyl isopropyl 1579 4 2-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1580 4 2-F-Phenyl CF.sub.3 1581 4 2-F-Phenyl —CH.sub.2CF.sub.3 1582 4 2-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1583 4 2-F-Phenyl cyclopropyl 1584 4 2-F-Phenyl Cyclobutyl 1585 4 2-F-Phenyl cyclopentyl 1586 4 2-F-Phenyl cyclohexyl 1587 4 2-F-Phenyl 3-pyridyl 1588 4 2-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1589 4 2-F-Phenyl 1H-imidazol-4-yl 1590 4 2-F-Phenyl 2-furanyl 1591 4 4-F-Phenyl ethyl 1592 4 4-F-Phenyl n-propyl 1593 4 4-F-Phenyl isopropyl 1594 4 4-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1595 4 4-F-Phenyl CF.sub.3 1596 4 4-F-Phenyl —CH.sub.2CF.sub.3 1597 4 4-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1598 4 4-F-Phenyl cyclopropyl 1599 4 4-F-Phenyl Cyclobutyl 1600 4 4-F-Phenyl cyclopentyl 1601 4 4-F-Phenyl cyclohexyl 1602 4 4-F-Phenyl 3-pyridyl 1603 4 4-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1604 4 4-F-Phenyl 1H-imidazol-4-yl 1605 4 4-F-Phenyl 2-furanyl 1606 4 3-Cl-Phenyl ethyl 1607 4 3-Cl-Phenyl n-propyl 1608 4 3-Cl-Phenyl isopropyl 1609 4 3-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1610 4 3-Cl-Phenyl CF.sub.3 1611 4 3-Cl-Phenyl —CH.sub.2CF.sub.3 1612 4 3-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1613 4 3-Cl-Phenyl cyclopropyl 1614 4 3-Cl-Phenyl Cyclobutyl 1615 4 3-Cl-Phenyl cyclopentyl 1616 4 3-Cl-Phenyl cyclohexyl 1617 4 3-Cl-Phenyl 3-pyridyl 1618 4 3-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1619 4 3-Cl-Phenyl 1H-imidazol-4-yl 1620 4 3-Cl-Phenyl 2-furanyl 1621 4 2-Br-Phenyl ethyl 1622 4 2-Br-Phenyl n-propyl 1623 4 2-Br-Phenyl isopropyl 1624 4 2-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1625 4 2-Br-Phenyl CF.sub.3 1626 4 2-Br-Phenyl —CH.sub.2CF.sub.3 1627 4 2-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1628 4 2-Br-Phenyl cyclopropyl 1629 4 2-Br-Phenyl Cyclobutyl 1630 4 2-Br-Phenyl cyclopentyl 1631 4 2-Br-Phenyl cyclohexyl 1632 4 2-Br-Phenyl 3-pyridyl 1633 4 2-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1634 4 2-Br-Phenyl 1H-imidazol-4-yl 1635 4 2-Br-Phenyl 2-furanyl 1636 4 4-Br-Phenyl ethyl 1637 4 4-Br-Phenyl n-propyl 1638 4 4-Br-Phenyl isopropyl 1639 4 4-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1640 4 4-Br-Phenyl CF.sub.3 1641 4 4-Br-Phenyl —CH.sub.2CF.sub.3 1642 4 4-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1643 4 4-Br-Phenyl cyclopropyl 1644 4 4-Br-Phenyl Cyclobutyl 1645 4 4-Br-Phenyl cyclopentyl 1646 4 4-Br-Phenyl cyclohexyl 1647 4 4-Br-Phenyl 3-pyridyl 1648 4 4-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1649 4 4-Br-Phenyl 1H-imidazol-4-yl 1650 4 4-Br-Phenyl 2-furanyl 1651 4 3-CF.sub.3-Phenyl ethyl 1652 4 3-CF.sub.3-Phenyl n-propyl 1653 4 3-CF.sub.3-Phenyl isopropyl 1654 4 3-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1655 4 3-CF.sub.3-Phenyl CF.sub.3 1656 4 3-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1657 4 3-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1658 4 3-CF.sub.3-Phenyl cyclopropyl 1659 4 3-CF.sub.3-Phenyl Cyclobutyl 1660 4 3-CF.sub.3-Phenyl cyclopentyl 1661 4 3-CF.sub.3-Phenyl cyclohexyl 1662 4 3-CF.sub.3-Phenyl 3-pyridyl 1663 4 3-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1664 4 3-CF.sub.3-Phenyl 1H-imidazol-4-yl 1665 4 3-CF.sub.3-Phenyl 2-furanyl 1666 4 2-iPr-Phenyl ethyl 1667 4 2-iPr-Phenyl n-propyl 1668 4 2-iPr-Phenyl isopropyl 1669 4 2-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1670 4 2-iPr-Phenyl CF.sub.3 1671 4 2-iPr-Phenyl —CH.sub.2CF.sub.3 1672 4 2-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1673 4 2-iPr-Phenyl cyclopropyl 1674 4 2-iPr-Phenyl Cyclobutyl 1675 4 2-iPr-Phenyl cyclopentyl 1676 4 2-iPr-Phenyl cyclohexyl 1677 4 2-iPr-Phenyl 3-pyridyl 1678 4 2-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1679 4 2-iPr-Phenyl 1H-imidazol-4-yl 1680 4 2-iPr-Phenyl 2-furanyl 1681 4 4-iPr-Phenyl ethyl 1682 4 4-iPr-Phenyl n-propyl 1683 4 4-iPr-Phenyl isopropyl 1684 4 4-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1685 4 4-iPr-Phenyl CF.sub.3 1686 4 4-iPr-Phenyl —CH.sub.2CF.sub.3 1687 4 4-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1688 4 4-iPr-Phenyl cyclopropyl 1689 4 4-iPr-Phenyl Cyclobutyl 1690 4 4-iPr-Phenyl cyclopentyl 1691 4 4-iPr-Phenyl cyclohexyl 1692 4 4-iPr-Phenyl 3-pyridyl 1693 4 4-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1694 4 4-iPr-Phenyl 1H-imidazol-4-yl 1695 4 4-iPr-Phenyl 2-furanyl 1696 4 3-morpholino-phenyl ethyl 1697 4 3-morpholino-phenyl n-propyl 1698 4 3-morpholino-phenyl isopropyl 1699 4 3-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1700 4 3-morpholino-phenyl CF.sub.3 1701 4 3-morpholino-phenyl —CH.sub.2CF.sub.3 1702 4 3-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1703 4 3-morpholino-phenyl cyclopropyl 1704 4 3-morpholino-phenyl Cyclobutyl 1705 4 3-morpholino-phenyl cyclopentyl 1706 4 3-morpholino-phenyl cyclohexyl 1707 4 3-morpholino-phenyl 3-pyridyl 1708 4 3-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1709 4 3-morpholino-phenyl 1H-imidazol-4-yl 1710 4 3-morpholino-phenyl 2-furanyl 1711 4 4-cyano-2-morpholino-phenyl ethyl 1712 4 4-cyano-2-morpholino-phenyl n-propyl 1713 4 4-cyano-2-morpholino-phenyl isopropyl 1714 4 4-cyano-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1715 4 4-cyano-2-morpholino-phenyl CF.sub.3 1716 4 4-cyano-2-morpholino-phenyl —CH.sub.2CF.sub.3 1717 4 4-cyano-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1718 4 4-cyano-2-morpholino-phenyl cyclopropyl 1719 4 4-cyano-2-morpholino-phenyl Cyclobutyl 1720 4 4-cyano-2-morpholino-phenyl cyclopentyl 1721 4 4-cyano-2-morpholino-phenyl cyclohexyl 1722 4 4-cyano-2-morpholino-phenyl 3-pyridyl 1723 4 4-cyano-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1724 4 4-cyano-2-morpholino-phenyl 1H-imidazol-4-yl 1725 4 4-cyano-2-morpholino-phenyl 2-furanyl 1726 4 4-hydroxy-2-morpholino-phenyl ethyl 1727 4 4-hydroxy-2-morpholino-phenyl n-propyl 1728 4 4-hydroxy-2-morpholino-phenyl isopropyl 1729 4 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1730 4 4-hydroxy-2-morpholino-phenyl CF.sub.3 1731 4 4-hydroxy-2-morpholino-phenyl —CH.sub.2CF.sub.3 1732 4 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1733 4 4-hydroxy-2-morpholino-phenyl cyclopropyl 1734 4 4-hydroxy-2-morpholino-phenyl Cyclobutyl 1735 4 4-hydroxy-2-morpholino-phenyl cyclopentyl 1736 4 4-hydroxy-2-morpholino-phenyl cyclohexyl 1737 4 4-hydroxy-2-morpholino-phenyl 3-pyridyl 1738 4 4-hydroxy-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1739 4 4-hydroxy-2-morpholino-phenyl 1H-imidazol-4-yl 1740 4 4-hydroxy-2-morpholino-phenyl 2-furanyl 1741 4 2-CH.sub.3-phenyl Ethyl 1742 4 2-CH.sub.3-phenyl n-propyl 1743 4 2-CH.sub.3-phenyl Isopropyl 1744 4 2-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1745 4 2-CH.sub.3-phenyl CF.sub.3 1746 4 2-CH.sub.3-phenyl —CH.sub.2CF.sub.3 1747 4 2-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 1748 4 2-CH.sub.3-phenyl cyclopropyl 1749 4 2-CH.sub.3-phenyl Cyclobutyl 1750 4 2-CH.sub.3-phenyl cyclopentyl 1751 4 2-CH.sub.3-phenyl cyclohexyl 1752 4 2-CH.sub.3-phenyl 3-pyridyl 1753 4 2-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1754 4 2-CH.sub.3-phenyl 1H-imidazol-4-yl 1755 4 2-CH.sub.3-phenyl 2-furanyl 1756 4 4-OH-Phenyl Ethyl 1757 4 4-OH-Phenyl n-propyl 1758 4 4-OH-Phenyl Isopropyl 1759 4 4-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1760 4 4-OH-Phenyl CF.sub.3 1761 4 4-OH-Phenyl —CH.sub.2CF.sub.3 1762 4 4-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1763 4 4-OH-Phenyl cyclopropyl 1764 4 4-OH-Phenyl Cyclobutyl 1765 4 4-OH-Phenyl cyclopentyl 1766 4 4-OH-Phenyl cyclohexyl 1767 4 4-OH-Phenyl 3-pyridyl 1768 4 4-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1769 4 4-OH-Phenyl 1H-imidazol-4-yl 1770 4 4-OH-Phenyl 2-furanyl 1771 4 2-OH-Phenyl Ethyl 1772 4 2-OH-Phenyl n-propyl 1773 4 2-OH-Phenyl Isopropyl 1774 4 2-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1775 4 2-OH-Phenyl CF.sub.3 1776 4 2-OH-Phenyl —CH.sub.2CF.sub.3 1777 4 2-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1778 4 2-OH-Phenyl cyclopropyl 1779 4 2-OH-Phenyl Cyclobutyl 1780 4 2-OH-Phenyl cyclopentyl 1781 4 2-OH-Phenyl cyclohexyl 1782 4 2-OH-Phenyl 3-pyridyl 1783 4 2-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1784 4 2-OH-Phenyl 1H-imidazol-4-yl 1785 4 2-OH-Phenyl 2-furanyl 1786 4 3-OMe-Phenyl Ethyl 1787 4 3-OMe-Phenyl n-propyl 1788 4 3-OMe-Phenyl Isopropyl 1789 4 3-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1790 4 3-OMe-Phenyl CF.sub.3 1791 4 3-OMe-Phenyl —CH.sub.2CF.sub.3 1792 4 3-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1793 4 3-OMe-Phenyl cyclopropyl 1794 4 3-OMe-Phenyl Cyclobutyl 1795 4 3-OMe-Phenyl cyclopentyl 1796 4 3-OMe-Phenyl cyclohexyl 1797 4 3-OMe-Phenyl 3-pyridyl 1798 4 3-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1799 4 3-OMe-Phenyl 1H-imidazol-4-yl 1800 4 3-OMe-Phenyl 2-furanyl 1801 4 4-CN-Phenyl Ethyl 1802 4 4-CN-Phenyl n-propyl 1803 4 4-CN-Phenyl Isopropyl 1804 4 4-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1805 4 4-CN-Phenyl CF.sub.3 1806 4 4-CN-Phenyl —CH.sub.2CF.sub.3 1807 4 4-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1808 4 4-CN-Phenyl cyclopropyl 1809 4 4-CN-Phenyl Cyclobutyl 1810 4 4-CN-Phenyl cyclopentyl 1811 4 4-CN-Phenyl cyclohexyl 1812 4 4-CN-Phenyl 3-pyridyl 1813 4 4-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1814 4 4-CN-Phenyl 1H-imidazol-4-yl 1815 4 4-CN-Phenyl 2-furanyl 1816 4 2-CN-Phenyl Ethyl 1817 4 2-CN-Phenyl n-propyl 1818 4 2-CN-Phenyl Isopropyl 1819 4 2-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1820 4 2-CN-Phenyl CF.sub.3 1821 4 2-CN-Phenyl —CH.sub.2CF.sub.3 1822 4 2-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1823 4 2-CN-Phenyl cyclopropyl 1824 4 2-CN-Phenyl Cyclobutyl 1825 4 2-CN-Phenyl cyclopentyl 1826 4 2-CN-Phenyl cyclohexyl 1827 4 2-CN-Phenyl 3-pyridyl 1828 4 2-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1829 4 2-CN-Phenyl 1H-imidazol-4-yl 1830 4 2-CN-Phenyl 2-furanyl 1831 4 3-F-Phenyl Ethyl 1832 4 3-F-Phenyl n-propyl 1833 4 3-F-Phenyl Isopropyl 1834 4 3-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1835 4 3-F-Phenyl CF.sub.3 1836 4 3-F-Phenyl —CH.sub.2CF.sub.3 1837 4 3-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1838 4 3-F-Phenyl cyclopropyl 1839 4 3-F-Phenyl Cyclobutyl 1840 4 3-F-Phenyl cyclopentyl 1841 4 3-F-Phenyl cyclohexyl 1842 4 3-F-Phenyl 3-pyridyl 1843 4 3-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1844 4 3-F-Phenyl 1H-imidazol-4-yl 1845 4 3-F-Phenyl 2-furanyl 1846 4 2-Cl-Phenyl Ethyl 1847 4 2-Cl-Phenyl n-propyl 1848 4 2-Cl-Phenyl Isopropyl 1849 4 2-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1850 4 2-Cl-Phenyl CF.sub.3 1851 4 2-Cl-Phenyl —CH.sub.2CF.sub.3 1852 4 2-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1853 4 2-Cl-Phenyl cyclopropyl 1854 4 2-Cl-Phenyl Cyclobutyl 1855 4 2-Cl-Phenyl cyclopentyl 1856 4 2-Cl-Phenyl cyclohexyl 1857 4 2-Cl-Phenyl 3-pyridyl 1858 4 2-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1859 4 2-Cl-Phenyl 1H-imidazol-4-yl 1860 4 2-Cl-Phenyl 2-furanyl 1861 4 4-Cl-Phenyl Ethyl 1862 4 4-Cl-Phenyl n-propyl 1863 4 4-Cl-Phenyl Isopropyl 1864 4 4-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1865 4 4-Cl-Phenyl CF.sub.3 1866 4 4-Cl-Phenyl —CH.sub.2CF.sub.3 1867 4 4-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1868 4 4-Cl-Phenyl cyclopropyl 1869 4 4-Cl-Phenyl Cyclobutyl 1870 4 4-Cl-Phenyl cyclopentyl 1871 4 4-Cl-Phenyl cyclohexyl 1872 4 4-Cl-Phenyl 3-pyridyl 1873 4 4-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1874 4 4-Cl-Phenyl 1H-imidazol-4-yl 1875 4 4-Cl-Phenyl 2-furanyl 1876 4 3-Br-Phenyl Ethyl 1877 4 3-Br-Phenyl n-propyl 1878 4 3-Br-Phenyl Isopropyl 1879 4 3-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1880 4 3-Br-Phenyl CF.sub.3 1881 4 3-Br-Phenyl —CH.sub.2CF.sub.3 1882 4 3-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1883 4 3-Br-Phenyl cyclopropyl 1884 4 3-Br-Phenyl Cyclobutyl 1885 4 3-Br-Phenyl cyclopentyl 1886 4 3-Br-Phenyl cyclohexyl 1887 4 3-Br-Phenyl 3-pyridyl 1888 4 3-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1889 4 3-Br-Phenyl 1H-imidazol-4-yl 1890 4 3-Br-Phenyl 2-furanyl 1891 4 2-CF.sub.3-Phenyl Ethyl 1892 4 2-CF.sub.3-Phenyl n-propyl 1893 4 2-CF.sub.3-Phenyl Isopropyl 1894 4 2-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1895 4 2-CF.sub.3-Phenyl CF.sub.3 1896 4 2-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1897 4 2-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1898 4 2-CF.sub.3-Phenyl cyclopropyl 1899 4 2-CF.sub.3-Phenyl Cyclobutyl 1900 4 2-CF.sub.3-Phenyl cyclopentyl 1901 4 2-CF.sub.3-Phenyl cyclohexyl 1902 4 2-CF.sub.3-Phenyl 3-pyridyl 1903 4 2-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1904 4 2-CF.sub.3-Phenyl 1H-imidazol-4-yl 1905 4 2-CF.sub.3-Phenyl 2-furanyl 1906 4 4-CF.sub.3-Phenyl Ethyl 1907 4 4-CF.sub.3-Phenyl n-propyl 1908 4 4-CF.sub.3-Phenyl Isopropyl 1909 4 4-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1910 4 4-CF.sub.3-Phenyl CF.sub.3 1911 4 4-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1912 4 4-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1913 4 4-CF.sub.3-Phenyl cyclopropyl 1914 4 4-CF.sub.3-Phenyl Cyclobutyl 1915 4 4-CF.sub.3-Phenyl cyclopentyl 1916 4 4-CF.sub.3-Phenyl cyclohexyl 1917 4 4-CF.sub.3-Phenyl 3-pyridyl 1918 4 4-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1919 4 4-CF.sub.3-Phenyl 1H-imidazol-4-yl 1920 4 4-CF.sub.3-Phenyl 2-furanyl 1921 4 3-iPr-Phenyl Ethyl 1922 4 3-iPr-Phenyl n-propyl 1923 4 3-iPr-Phenyl Isopropyl 1924 4 3-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1925 4 3-iPr-Phenyl CF.sub.3 1926 4 3-iPr-Phenyl —CH.sub.2CF.sub.3 1927 4 3-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1928 4 3-iPr-Phenyl cyclopropyl 1929 4 3-iPr-Phenyl Cyclobutyl 1930 4 3-iPr-Phenyl cyclopentyl 1931 4 3-iPr-Phenyl cyclohexyl 1932 4 3-iPr-Phenyl 3-pyridyl 1933 4 3-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1934 4 3-iPr-Phenyl 1H-imidazol-4-yl 1935 4 3-iPr-Phenyl 2-furanyl 1936 4 2-morpholino-phenyl Ethyl 1937 4 2-morpholino-phenyl n-propyl 1938 4 2-morpholino-phenyl isopropyl 1939 4 2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1940 4 2-morpholino-phenyl CF.sub.3 1941 4 2-morpholino-phenyl —CH.sub.2CF.sub.3 1942 4 2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1943 4 2-morpholino-phenyl cyclopropyl 1944 4 2-morpholino-phenyl Cyclobutyl 1945 4 2-morpholino-phenyl cyclopentyl 1946 4 2-morpholino-phenyl cyclohexyl 1947 4 2-morpholino-phenyl 3-pyridyl 1948 4 2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1949 4 2-morpholino-phenyl 1H-imidazol-4-yl 1950 4 2-morpholino-phenyl 2-furanyl 1951 4 4-morpholino-phenyl ethyl 1952 4 4-morpholino-phenyl n-propyl 1953 4 4-morpholino-phenyl isopropyl 1954 4 4-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1955 4 4-morpholino-phenyl CF.sub.3 1956 4 4-morpholino-phenyl —CH.sub.2CF.sub.3 1957 4 4-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1958 4 4-morpholino-phenyl cyclopropyl 1959 4 4-morpholino-phenyl Cyclobutyl 1960 4 4-morpholino-phenyl cyclopentyl 1961 4 4-morpholino-phenyl cyclohexyl 1962 4 4-morpholino-phenyl 3-pyridyl 1963 4 4-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1964 4 4-morpholino-phenyl 1H-imidazol-4-yl 1965 4 4-morpholino-phenyl 2-furanyl 1966 4 4-methyl-2-morpholino-phenyl ethyl 1967 4 4-methyl-2-morpholino-phenyl n-propyl 1968 4 4-methyl-2-morpholino-phenyl isopropyl 1969 4 4-methyl-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1970 4 4-methyl-2-morpholino-phenyl CF.sub.3 1971 4 4-methyl-2-morpholino-phenyl —CH.sub.2CF.sub.3 1972 4 4-methyl-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1973 4 4-methyl-2-morpholino-phenyl cyclopropyl 1974 4 4-methyl-2-morpholino-phenyl Cyclobutyl 1975 4 4-methyl-2-morpholino-phenyl cyclopentyl 1976 4 4-methyl-2-morpholino-phenyl cyclohexyl 1977 4 4-methyl-2-morpholino-phenyl 3-pyridyl 1978 4 4-methyl-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1979 4 4-methyl-2-morpholino-phenyl 1H-imidazol-4-yl 1980 4 4-methyl-2-morpholino-phenyl 2-furanyl 1981 1 naphthylen-1-yl Ethyl 1982 1 naphthylen-1-yl n-propyl 1983 1 naphthylen-1-yl Isopropyl 1984 1 naphthylen-1-yl —CH.sub.2CH(CH.sub.3).sub.2 1985 1 naphthylen-1-yl CF.sub.3 1986 1 naphthylen-1-yl —CH.sub.2CF.sub.3 1987 1 naphthylen-1-yl —CH.sub.2CH.sub.2CF.sub.3 1988 1 naphthylen-1-yl Cyclopropyl 1989 1 naphthylen-1-yl Cyclobutyl 1990 1 naphthylen-1-yl Cyclopentyl 1991 1 naphthylen-1-yl Cyclohexyl 1992 1 naphthylen-1-yl 3-pyridyl 1993 1 naphthylen-1-yl 1-methyl-1H-pyrazol-4-yl 1994 1 naphthylen-1-yl 1H-imidazol-4-yl 1995 1 naphthylen-1-yl 2-furanyl 1996 1 naphthylen-2-yl Ethyl 1997 1 naphthylen-2-yl n-propyl 1998 1 naphthylen-2-yl Isopropyl 1999 1 naphthylen-2-yl —CH.sub.2CH(CH.sub.3).sub.2 2000 1 naphthylen-2-yl CF.sub.3 2001 1 naphthylen-2-yl —CH.sub.2CF.sub.3 2002 1 naphthylen-2-yl —CH.sub.2CH.sub.2CF.sub.3 2003 1 naphthylen-2-yl Cyclopropyl 2004 1 naphthylen-2-yl Cyclobutyl 2005 1 naphthylen-2-yl Cyclopentyl 2006 1 naphthylen-2-yl Cyclohexyl 2007 1 naphthylen-2-yl 3-pyridyl 2008 1 naphthylen-2-yl 1-methyl-1H-pyrazol-4-yl 2009 1 naphthylen-2-yl 1H-imidazol-4-yl 2010 1 naphthylen-2-yl 2-furanyl 2011 2 naphthylen-1-yl Ethyl 2012 2 naphthylen-1-yl n-propyl 2013 2 naphthylen-1-yl Isopropyl 2014 2 naphthylen-1-yl —CH.sub.2CH(CH.sub.3).sub.2 2015 2 naphthylen-1-yl CF.sub.3 2016 2 naphthylen-1-yl —CH.sub.2CF.sub.3 2017 2 naphthylen-1-yl —CH.sub.2CH.sub.2CF.sub.3 2018 2 naphthylen-1-yl Cyclopropyl 2019 2 naphthylen-1-yl Cyclobutyl 2020 2 naphthylen-1-yl Cyclopentyl 2021 2 naphthylen-1-yl Cyclohexyl 2022 2 naphthylen-1-yl 3-pyridyl 2023 2 naphthylen-1-yl 1-methyl-1H-pyrazol-4-yl 2024 2 naphthylen-1-yl 1H-imidazol-4-yl 2025 2 naphthylen-1-yl 2-furanyl 2026 2 naphthylen-2-yl Ethyl 2027 2 naphthylen-2-yl n-propyl 2028 2 naphthylen-2-yl Isopropyl 2029 2 naphthylen-2-yl —CH.sub.2CH(CH.sub.3).sub.2 2030 2 naphthylen-2-yl CF.sub.3 2031 2 naphthylen-2-yl —CH.sub.2CF.sub.3 2032 2 naphthylen-2-yl —CH.sub.2CH.sub.2CF.sub.3 2033 2 naphthylen-2-yl Cyclopropyl 2034 2 naphthylen-2-yl Cyclobutyl 2035 2 naphthylen-2-yl Cyclopentyl 2036 2 naphthylen-2-yl Cyclohexyl 2037 2 naphthylen-2-yl 3-pyridyl 2038 2 naphthylen-2-yl 1-methyl-1H-pyrazol-4-yl 2039 2 naphthylen-2-yl 1H-imidazol-4-yl 2040 2 naphthylen-2-yl 2-furanyl 2041 3 naphthylen-1-yl Ethyl 2042 3 naphthylen-1-yl n-propyl 2043 3 naphthylen-1-yl Isopropyl 2044 3 naphthylen-1-yl —CH.sub.2CH(CH.sub.3).sub.2 2045 3 naphthylen-1-yl CF.sub.3 2046 3 naphthylen-1-yl —CH.sub.2CF.sub.3 2047 3 naphthylen-1-yl —CH.sub.2CH.sub.2CF.sub.3 2048 3 naphthylen-1-yl Cyclopropyl 2049 3 naphthylen-1-yl Cyclobutyl 2050 3 naphthylen-1-yl Cyclopentyl 2051 3 naphthylen-1-yl Cyclohexyl 2052 3 naphthylen-1-yl 3-pyridyl 2053 3 naphthylen-1-yl 1-methyl-1H-pyrazol-4-yl 2054 3 naphthylen-1-yl 1H-imidazol-4-yl 2055 3 naphthylen-1-yl 2-furanyl 2056 3 naphthylen-2-yl Ethyl 2057 3 naphthylen-2-yl n-propyl 2058 3 naphthylen-2-yl Isopropyl 2059 3 naphthylen-2-yl —CH.sub.2CH(CH.sub.3).sub.2 2060 3 naphthylen-2-yl CF.sub.3 2061 3 naphthylen-2-yl —CH.sub.2CF.sub.3 2062 3 naphthylen-2-yl —CH.sub.2CH.sub.2CF.sub.3 2063 3 naphthylen-2-yl Cyclopropyl 2064 3 naphthylen-2-yl Cyclobutyl 2065 3 naphthylen-2-yl Cyclopentyl 2066 3 naphthylen-2-yl Cyclohexyl 2067 3 naphthylen-2-yl 3-pyridyl 2068 3 naphthylen-2-yl 1-methyl-1H-pyrazol-4-yl 2069 3 naphthylen-2-yl 1H-imidazol-4-yl 2070 3 naphthylen-2-yl 2-furanyl 2071 4 naphthylen-1-yl Ethyl 2072 4 naphthylen-1-yl n-propyl 2073 4 naphthylen-1-yl Isopropyl 2074 4 naphthylen-1-yl —CH.sub.2CH(CH.sub.3).sub.2 2075 4 naphthylen-1-yl CF.sub.3 2076 4 naphthylen-1-yl —CH.sub.2CF.sub.3 2077 4 naphthylen-1-yl —CH.sub.2CH.sub.2CF.sub.3 2078 4 naphthylen-1-yl Cyclopropyl 2079 4 naphthylen-1-yl Cyclobutyl 2080 4 naphthylen-1-yl Cyclopentyl 2081 4 naphthylen-1-yl Cyclohexyl 2082 4 naphthylen-1-yl 3-pyridyl 2083 4 naphthylen-1-yl 1-methyl-1H-pyrazol-4-yl 2084 4 naphthylen-1-yl 1H-imidazol-4-yl 2085 4 naphthylen-1-yl 2-furanyl 2086 4 naphthylen-2-yl Ethyl 2087 4 naphthylen-2-yl n-propyl 2088 4 naphthylen-2-yl Isopropyl 2089 4 naphthylen-2-yl —CH.sub.2CH(CH.sub.3).sub.2 2090 4 naphthylen-2-yl CF.sub.3 2091 4 naphthylen-2-yl —CH.sub.2CF.sub.3 2092 4 naphthylen-2-yl —CH.sub.2CH.sub.2CF.sub.3 2093 4 naphthylen-2-yl Cyclopropyl 2094 4 naphthylen-2-yl Cyclobutyl 2095 4 naphthylen-2-yl Cyclopentyl 2096 4 naphthylen-2-yl Cyclohexyl 2097 4 naphthylen-2-yl 3-pyridyl 2098 4 naphthylen-2-yl 1-methyl-1H-pyrazol-4-yl 2099 4 naphthylen-2-yl 1H-imidazol-4-yl 2100 4 naphthylen-2-yl 2-furanyl

    [2056] Exemplary embodiments include compounds having the formula (XXXIX)

    ##STR00453##

    [2057] or a pharmaceutically acceptable salt form thereof defined herein below in Table 32.

    TABLE-US-00032 TABLE 32 Entry n R.sup.4 R.sup.10c 1 1 4-CH.sub.3-phenyl Ethyl 2 1 4-CH.sub.3-phenyl n-propyl 3 1 4-CH.sub.3-phenyl Isopropyl 4 1 4-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 5 1 4-CH.sub.3-phenyl CF.sub.3 6 1 4-CH.sub.3-phenyl —CH.sub.2CF.sub.3 7 1 4-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 8 1 4-CH.sub.3-phenyl Cyclopropyl 9 1 4-CH.sub.3-phenyl Cyclobutyl 10 1 4-CH.sub.3-phenyl Cyclopentyl 11 1 4-CH.sub.3-phenyl cyclohexyl 12 1 4-CH.sub.3-phenyl 3-pyridyl 13 1 4-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 14 1 4-CH.sub.3-phenyl 1H-imidazol-4-yl 15 1 4-CH.sub.3-phenyl 2-furanyl 16 1 3-CH.sub.3-phenyl ethyl 17 1 3-CH.sub.3-phenyl n-propyl 18 1 3-CH.sub.3-phenyl isopropyl 19 1 3-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 20 1 3-CH.sub.3-phenyl CF.sub.3 21 1 3-CH.sub.3-phenyl —CH.sub.2CF.sub.3 22 1 3-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 23 1 3-CH.sub.3-phenyl cyclopropyl 24 1 3-CH.sub.3-phenyl Cyclobutyl 25 1 3-CH.sub.3-phenyl cyclopentyl 26 1 3-CH.sub.3-phenyl cyclohexyl 27 1 3-CH.sub.3-phenyl 3-pyridyl 28 1 3-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 29 1 3-CH.sub.3-phenyl 1H-imidazol-4-yl 30 1 3-CH.sub.3-phenyl 2-furanyl 31 1 3-OH-Phenyl ethyl 32 1 3-OH-Phenyl n-propyl 33 1 3-OH-Phenyl isopropyl 34 1 3-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 35 1 3-OH-Phenyl CF.sub.3 36 1 3-OH-Phenyl —CH.sub.2CF.sub.3 37 1 3-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 38 1 3-OH-Phenyl cyclopropyl 39 1 3-OH-Phenyl Cyclobutyl 40 1 3-OH-Phenyl cyclopentyl 41 1 3-OH-Phenyl cyclohexyl 42 1 3-OH-Phenyl 3-pyridyl 43 1 3-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 44 1 3-OH-Phenyl 1H-imidazol-4-yl 45 1 3-OH-Phenyl 2-furanyl 46 1 4-OMe-Phenyl ethyl 47 1 4-OMe-Phenyl n-propyl 48 1 4-OMe-Phenyl isopropyl 49 1 4-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 50 1 4-OMe-Phenyl CF.sub.3 51 1 4-OMe-Phenyl —CH.sub.2CF.sub.3 52 1 4-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 53 1 4-OMe-Phenyl cyclopropyl 54 1 4-OMe-Phenyl Cyclobutyl 55 1 4-OMe-Phenyl cyclopentyl 56 1 4-OMe-Phenyl cyclohexyl 57 1 4-OMe-Phenyl 3-pyridyl 58 1 4-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 59 1 4-OMe-Phenyl 1H-imidazol-4-yl 60 1 4-OMe-Phenyl 2-furanyl 61 1 2-OMe-Phenyl ethyl 62 1 2-OMe-Phenyl n-propyl 63 1 2-OMe-Phenyl isopropyl 64 1 2-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 65 1 2-OMe-Phenyl CF.sub.3 66 1 2-OMe-Phenyl —CH.sub.2CF.sub.3 67 1 2-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 68 1 2-OMe-Phenyl cyclopropyl 69 1 2-OMe-Phenyl Cyclobutyl 70 1 2-OMe-Phenyl cyclopentyl 71 1 2-OMe-Phenyl cyclohexyl 72 1 2-OMe-Phenyl 3-pyridyl 73 1 2-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 74 1 2-OMe-Phenyl 1H-imidazol-4-yl 75 1 2-OMe-Phenyl 2-furanyl 76 1 3-CN-Phenyl ethyl 77 1 3-CN-Phenyl n-propyl 78 1 3-CN-Phenyl isopropyl 79 1 3-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 80 1 3-CN-Phenyl CF.sub.3 81 1 3-CN-Phenyl —CH.sub.2CF.sub.3 82 1 3-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 83 1 3-CN-Phenyl cyclopropyl 84 1 3-CN-Phenyl Cyclobutyl 85 1 3-CN-Phenyl cyclopentyl 86 1 3-CN-Phenyl cyclohexyl 87 1 3-CN-Phenyl 3-pyridyl 88 1 3-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 89 1 3-CN-Phenyl 1H-imidazol-4-yl 90 1 3-CN-Phenyl 2-furanyl 91 1 2-F-Phenyl ethyl 92 1 2-F-Phenyl n-propyl 93 1 2-F-Phenyl isopropyl 94 1 2-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 95 1 2-F-Phenyl CF.sub.3 96 1 2-F-Phenyl —CH.sub.2CF.sub.3 97 1 2-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 98 1 2-F-Phenyl cyclopropyl 99 1 2-F-Phenyl Cyclobutyl 100 1 2-F-Phenyl cyclopentyl 101 1 2-F-Phenyl cyclohexyl 102 1 2-F-Phenyl 3-pyridyl 103 1 2-F-Phenyl 1-methyl-1H-pyrazol-4-yl 104 1 2-F-Phenyl 1H-imidazol-4-yl 105 1 2-F-Phenyl 2-furanyl 106 1 4-F-Phenyl ethyl 107 1 4-F-Phenyl n-propyl 108 1 4-F-Phenyl isopropyl 109 1 4-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 110 1 4-F-Phenyl CF.sub.3 111 1 4-F-Phenyl —CH.sub.2CF.sub.3 112 1 4-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 113 1 4-F-Phenyl cyclopropyl 114 1 4-F-Phenyl Cyclobutyl 115 1 4-F-Phenyl cyclopentyl 116 1 4-F-Phenyl cyclohexyl 117 1 4-F-Phenyl 3-pyridyl 118 1 4-F-Phenyl 1-methyl-1H-pyrazol-4-yl 119 1 4-F-Phenyl 1H-imidazol-4-yl 120 1 4-F-Phenyl 2-furanyl 121 1 3-Cl-Phenyl ethyl 122 1 3-Cl-Phenyl n-propyl 123 1 3-Cl-Phenyl isopropyl 124 1 3-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 125 1 3-Cl-Phenyl CF.sub.3 126 1 3-Cl-Phenyl —CH.sub.2CF.sub.3 127 1 3-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 128 1 3-Cl-Phenyl cyclopropyl 129 1 3-Cl-Phenyl Cyclobutyl 130 1 3-Cl-Phenyl cyclopentyl 131 1 3-Cl-Phenyl cyclohexyl 132 1 3-Cl-Phenyl 3-pyridyl 133 1 3-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 134 1 3-Cl-Phenyl 1H-imidazol-4-yl 135 1 3-Cl-Phenyl 2-furanyl 136 1 2-Br-Phenyl ethyl 137 1 2-Br-Phenyl n-propyl 138 1 2-Br-Phenyl isopropyl 139 1 2-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 140 1 2-Br-Phenyl CF.sub.3 141 1 2-Br-Phenyl —CH.sub.2CF.sub.3 142 1 2-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 143 1 2-Br-Phenyl cyclopropyl 144 1 2-Br-Phenyl Cyclobutyl 145 1 2-Br-Phenyl cyclopentyl 146 1 2-Br-Phenyl cyclohexyl 147 1 2-Br-Phenyl 3-pyridyl 148 1 2-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 149 1 2-Br-Phenyl 1H-imidazol-4-yl 150 1 2-Br-Phenyl 2-furanyl 151 1 4-Br-Phenyl ethyl 152 1 4-Br-Phenyl n-propyl 153 1 4-Br-Phenyl isopropyl 154 1 4-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 155 1 4-Br-Phenyl CF.sub.3 156 1 4-Br-Phenyl —CH.sub.2CF.sub.3 157 1 4-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 158 1 4-Br-Phenyl cyclopropyl 159 1 4-Br-Phenyl Cyclobutyl 160 1 4-Br-Phenyl cyclopentyl 161 1 4-Br-Phenyl cyclohexyl 162 1 4-Br-Phenyl 3-pyridyl 163 1 4-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 164 1 4-Br-Phenyl 1H-imidazol-4-yl 165 1 4-Br-Phenyl 2-furanyl 166 1 3-CF.sub.3-Phenyl ethyl 167 1 3-CF.sub.3-Phenyl n-propyl 168 1 3-CF.sub.3-Phenyl isopropyl 169 1 3-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 170 1 3-CF.sub.3-Phenyl CF.sub.3 171 1 3-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 172 1 3-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 173 1 3-CF.sub.3-Phenyl cyclopropyl 174 1 3-CF.sub.3-Phenyl Cyclobutyl 175 1 3-CF.sub.3-Phenyl cyclopentyl 176 1 3-CF.sub.3-Phenyl cyclohexyl 177 1 3-CF.sub.3-Phenyl 3-pyridyl 178 1 3-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 179 1 3-CF.sub.3-Phenyl 1H-imidazol-4-yl 180 1 3-CF.sub.3-Phenyl 2-furanyl 181 1 2-iPr-Phenyl ethyl 182 1 2-iPr-Phenyl n-propyl 183 1 2-iPr-Phenyl isopropyl 184 1 2-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 185 1 2-iPr-Phenyl CF.sub.3 186 1 2-iPr-Phenyl —CH.sub.2CF.sub.3 187 1 2-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 188 1 2-iPr-Phenyl cyclopropyl 189 1 2-iPr-Phenyl Cyclobutyl 190 1 2-iPr-Phenyl cyclopentyl 191 1 2-iPr-Phenyl cyclohexyl 192 1 2-iPr-Phenyl 3-pyridyl 193 1 2-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 194 1 2-iPr-Phenyl 1H-imidazol-4-yl 195 1 2-iPr-Phenyl 2-furanyl 196 1 4-iPr-Phenyl ethyl 197 1 4-iPr-Phenyl n-propyl 198 1 4-iPr-Phenyl isopropyl 199 1 4-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 200 1 4-iPr-Phenyl CF.sub.3 201 1 4-iPr-Phenyl —CH.sub.2CF.sub.3 202 1 4-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 203 1 4-iPr-Phenyl cyclopropyl 204 1 4-iPr-Phenyl Cyclobutyl 205 1 4-iPr-Phenyl cyclopentyl 206 1 4-iPr-Phenyl cyclohexyl 207 1 4-iPr-Phenyl 3-pyridyl 208 1 4-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 209 1 4-iPr-Phenyl 1H-imidazol-4-yl 210 1 4-iPr-Phenyl 2-furanyl 211 1 3-morpholino-phenyl ethyl 212 1 3-morpholino-phenyl n-propyl 213 1 3-morpholino-phenyl isopropyl 214 1 3-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 215 1 3-morpholino-phenyl CF.sub.3 216 1 3-morpholino-phenyl —CH.sub.2CF.sub.3 217 1 3-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 218 1 3-morpholino-phenyl cyclopropyl 219 1 3-morpholino-phenyl Cyclobutyl 220 1 3-morpholino-phenyl cyclopentyl 221 1 3-morpholino-phenyl cyclohexyl 222 1 3-morpholino-phenyl 3-pyridyl 223 1 3-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 224 1 3-morpholino-phenyl 1H-imidazol-4-yl 225 1 3-morpholino-phenyl 2-furanyl 226 1 4-cyano-2-morpholino-phenyl ethyl 227 1 4-cyano-2-morpholino-phenyl n-propyl 228 1 4-cyano-2-morpholino-phenyl isopropyl 229 1 4-cyano-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 230 1 4-cyano-2-morpholino-phenyl CF.sub.3 231 1 4-cyano-2-morpholino-phenyl —CH.sub.2CF.sub.3 232 1 4-cyano-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 233 1 4-cyano-2-morpholino-phenyl cyclopropyl 234 1 4-cyano-2-morpholino-phenyl Cyclobutyl 235 1 4-cyano-2-morpholino-phenyl cyclopentyl 236 1 4-cyano-2-morpholino-phenyl cyclohexyl 237 1 4-cyano-2-morpholino-phenyl 3-pyridyl 238 1 4-cyano-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 239 1 4-cyano-2-morpholino-phenyl 1H-imidazol-4-yl 240 1 4-cyano-2-morpholino-phenyl 2-furanyl 241 1 4-hydroxy-2-morpholino-phenyl ethyl 242 1 4-hydroxy-2-morpholino-phenyl n-propyl 243 1 4-hydroxy-2-morpholino-phenyl isopropyl 244 1 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 245 1 4-hydroxy-2-morpholino-phenyl CF.sub.3 246 1 4-hydroxy-2-morpholino-phenyl —CH.sub.2CF.sub.3 247 1 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 248 1 4-hydroxy-2-morpholino-phenyl cyclopropyl 249 1 4-hydroxy-2-morpholino-phenyl Cyclobutyl 250 1 4-hydroxy-2-morpholino-phenyl cyclopentyl 251 1 4-hydroxy-2-morpholino-phenyl cyclohexyl 252 1 4-hydroxy-2-morpholino-phenyl 3-pyridyl 253 1 4-hydroxy-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 254 1 4-hydroxy-2-morpholino-phenyl 1H-imidazol-4-yl 255 1 4-hydroxy-2-morpholino-phenyl 2-furanyl 256 1 2-CH.sub.3-phenyl Ethyl 257 1 2-CH.sub.3-phenyl n-propyl 258 1 2-CH.sub.3-phenyl Isopropyl 259 1 2-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 260 1 2-CH.sub.3-phenyl CF.sub.3 261 1 2-CH.sub.3-phenyl —CH.sub.2CF.sub.3 262 1 2-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 263 1 2-CH.sub.3-phenyl cyclopropyl 264 1 2-CH.sub.3-phenyl Cyclobutyl 265 1 2-CH.sub.3-phenyl cyclopentyl 266 1 2-CH.sub.3-phenyl cyclohexyl 267 1 2-CH.sub.3-phenyl 3-pyridyl 268 1 2-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 269 1 2-CH.sub.3-phenyl 1H-imidazol-4-yl 270 1 2-CH.sub.3-phenyl 2-furanyl 271 1 4-OH-Phenyl Ethyl 272 1 4-OH-Phenyl n-propyl 273 1 4-OH-Phenyl Isopropyl 274 1 4-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 275 1 4-OH-Phenyl CF.sub.3 276 1 4-OH-Phenyl —CH.sub.2CF.sub.3 277 1 4-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 278 1 4-OH-Phenyl cyclopropyl 279 1 4-OH-Phenyl Cyclobutyl 280 1 4-OH-Phenyl cyclopentyl 281 1 4-OH-Phenyl cyclohexyl 282 1 4-OH-Phenyl 3-pyridyl 283 1 4-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 284 1 4-OH-Phenyl 1H-imidazol-4-yl 285 1 4-OH-Phenyl 2-furanyl 286 1 2-OH-Phenyl Ethyl 287 1 2-OH-Phenyl n-propyl 288 1 2-OH-Phenyl Isopropyl 289 1 2-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 290 1 2-OH-Phenyl CF.sub.3 291 1 2-OH-Phenyl —CH.sub.2CF.sub.3 292 1 2-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 293 1 2-OH-Phenyl cyclopropyl 294 1 2-OH-Phenyl Cyclobutyl 295 1 2-OH-Phenyl cyclopentyl 296 1 2-OH-Phenyl cyclohexyl 297 1 2-OH-Phenyl 3-pyridyl 298 1 2-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 299 1 2-OH-Phenyl 1H-imidazol-4-yl 300 1 2-OH-Phenyl 2-furanyl 301 1 3-OMe-Phenyl Ethyl 302 1 3-OMe-Phenyl n-propyl 303 1 3-OMe-Phenyl Isopropyl 304 1 3-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 305 1 3-OMe-Phenyl CF.sub.3 306 1 3-OMe-Phenyl —CH.sub.2CF.sub.3 307 1 3-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 308 1 3-OMe-Phenyl cyclopropyl 309 1 3-OMe-Phenyl Cyclobutyl 310 1 3-OMe-Phenyl cyclopentyl 311 1 3-OMe-Phenyl cyclohexyl 312 1 3-OMe-Phenyl 3-pyridyl 313 1 3-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 314 1 3-OMe-Phenyl 1H-imidazol-4-yl 315 1 3-OMe-Phenyl 2-furanyl 316 1 4-CN-Phenyl Ethyl 317 1 4-CN-Phenyl n-propyl 318 1 4-CN-Phenyl Isopropyl 319 1 4-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 320 1 4-CN-Phenyl CF.sub.3 321 1 4-CN-Phenyl —CH.sub.2CF.sub.3 322 1 4-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 323 1 4-CN-Phenyl cyclopropyl 324 1 4-CN-Phenyl Cyclobutyl 325 1 4-CN-Phenyl cyclopentyl 326 1 4-CN-Phenyl cyclohexyl 327 1 4-CN-Phenyl 3-pyridyl 328 1 4-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 329 1 4-CN-Phenyl 1H-imidazol-4-yl 330 1 4-CN-Phenyl 2-furanyl 331 1 2-CN-Phenyl Ethyl 332 1 2-CN-Phenyl n-propyl 333 1 2-CN-Phenyl Isopropyl 334 1 2-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 335 1 2-CN-Phenyl CF.sub.3 336 1 2-CN-Phenyl —CH.sub.2CF.sub.3 337 1 2-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 338 1 2-CN-Phenyl cyclopropyl 339 1 2-CN-Phenyl Cyclobutyl 340 1 2-CN-Phenyl cyclopentyl 341 1 2-CN-Phenyl cyclohexyl 342 1 2-CN-Phenyl 3-pyridyl 343 1 2-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 344 1 2-CN-Phenyl 1H-imidazol-4-yl 345 1 2-CN-Phenyl 2-furanyl 346 1 3-F-Phenyl Ethyl 347 1 3-F-Phenyl n-propyl 348 1 3-F-Phenyl Isopropyl 349 1 3-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 350 1 3-F-Phenyl CF.sub.3 351 1 3-F-Phenyl —CH.sub.2CF.sub.3 352 1 3-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 353 1 3-F-Phenyl cyclopropyl 354 1 3-F-Phenyl Cyclobutyl 355 1 3-F-Phenyl cyclopentyl 356 1 3-F-Phenyl cyclohexyl 357 1 3-F-Phenyl 3-pyridyl 358 1 3-F-Phenyl 1-methyl-1H-pyrazol-4-yl 359 1 3-F-Phenyl 1H-imidazol-4-yl 360 1 3-F-Phenyl 2-furanyl 361 1 2-Cl-Phenyl Ethyl 362 1 2-Cl-Phenyl n-propyl 363 1 2-Cl-Phenyl Isopropyl 364 1 2-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 365 1 2-Cl-Phenyl CF.sub.3 366 1 2-Cl-Phenyl —CH.sub.2CF.sub.3 367 1 2-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 368 1 2-Cl-Phenyl cyclopropyl 369 1 2-Cl-Phenyl Cyclobutyl 370 1 2-Cl-Phenyl cyclopentyl 371 1 2-Cl-Phenyl cyclohexyl 372 1 2-Cl-Phenyl 3-pyridyl 373 1 2-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 374 1 2-Cl-Phenyl 1H-imidazol-4-yl 375 1 2-Cl-Phenyl 2-furanyl 376 1 4-Cl-Phenyl Ethyl 377 1 4-Cl-Phenyl n-propyl 378 1 4-Cl-Phenyl Isopropyl 379 1 4-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 380 1 4-Cl-Phenyl CF.sub.3 381 1 4-Cl-Phenyl —CH.sub.2CF.sub.3 382 1 4-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 383 1 4-Cl-Phenyl cyclopropyl 384 1 4-Cl-Phenyl Cyclobutyl 385 1 4-Cl-Phenyl cyclopentyl 386 1 4-Cl-Phenyl cyclohexyl 387 1 4-Cl-Phenyl 3-pyridyl 388 1 4-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 389 1 4-Cl-Phenyl 1H-imidazol-4-yl 390 1 4-Cl-Phenyl 2-furanyl 391 1 3-Br-Phenyl Ethyl 392 1 3-Br-Phenyl n-propyl 393 1 3-Br-Phenyl Isopropyl 394 1 3-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 395 1 3-Br-Phenyl CF.sub.3 396 1 3-Br-Phenyl —CH.sub.2CF.sub.3 397 1 3-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 398 1 3-Br-Phenyl cyclopropyl 399 1 3-Br-Phenyl Cyclobutyl 400 1 3-Br-Phenyl cyclopentyl 401 1 3-Br-Phenyl cyclohexyl 402 1 3-Br-Phenyl 3-pyridyl 403 1 3-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 404 1 3-Br-Phenyl 1H-imidazol-4-yl 405 1 3-Br-Phenyl 2-furanyl 406 1 2-CF.sub.3-Phenyl Ethyl 407 1 2-CF.sub.3-Phenyl n-propyl 408 1 2-CF.sub.3-Phenyl Isopropyl 409 1 2-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 410 1 2-CF.sub.3-Phenyl CF.sub.3 411 1 2-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 412 1 2-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 413 1 2-CF.sub.3-Phenyl cyclopropyl 414 1 2-CF.sub.3-Phenyl Cyclobutyl 415 1 2-CF.sub.3-Phenyl cyclopentyl 416 1 2-CF.sub.3-Phenyl cyclohexyl 417 1 2-CF.sub.3-Phenyl 3-pyridyl 418 1 2-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 419 1 2-CF.sub.3-Phenyl 1H-imidazol-4-yl 420 1 2-CF.sub.3-Phenyl 2-furanyl 421 1 4-CF.sub.3-Phenyl Ethyl 422 1 4-CF.sub.3-Phenyl n-propyl 423 1 4-CF.sub.3-Phenyl Isopropyl 424 1 4-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 425 1 4-CF.sub.3-Phenyl CF.sub.3 426 1 4-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 427 1 4-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 428 1 4-CF.sub.3-Phenyl cyclopropyl 429 1 4-CF.sub.3-Phenyl Cyclobutyl 430 1 4-CF.sub.3-Phenyl cyclopentyl 431 1 4-CF.sub.3-Phenyl cyclohexyl 432 1 4-CF.sub.3-Phenyl 3-pyridyl 433 1 4-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 434 1 4-CF.sub.3-Phenyl 1H-imidazol-4-yl 435 1 4-CF.sub.3-Phenyl 2-furanyl 436 1 3-iPr-Phenyl Ethyl 437 1 3-iPr-Phenyl n-propyl 438 1 3-iPr-Phenyl Isopropyl 439 1 3-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 440 1 3-iPr-Phenyl CF.sub.3 441 1 3-iPr-Phenyl —CH.sub.2CF.sub.3 442 1 3-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 443 1 3-iPr-Phenyl cyclopropyl 444 1 3-iPr-Phenyl Cyclobutyl 445 1 3-iPr-Phenyl cyclopentyl 446 1 3-iPr-Phenyl cyclohexyl 447 1 3-iPr-Phenyl 3-pyridyl 448 1 3-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 449 1 3-iPr-Phenyl 1H-imidazol-4-yl 450 1 3-iPr-Phenyl 2-furanyl 451 1 2-morpholino-phenyl Ethyl 452 1 2-morpholino-phenyl n-propyl 453 1 2-morpholino-phenyl isopropyl 454 1 2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 455 1 2-morpholino-phenyl CF.sub.3 456 1 2-morpholino-phenyl —CH.sub.2CF.sub.3 457 1 2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 458 1 2-morpholino-phenyl cyclopropyl 459 1 2-morpholino-phenyl Cyclobutyl 460 1 2-morpholino-phenyl cyclopentyl 461 1 2-morpholino-phenyl cyclohexyl 462 1 2-morpholino-phenyl 3-pyridyl 463 1 2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 464 1 2-morpholino-phenyl 1H-imidazol-4-yl 465 1 2-morpholino-phenyl 2-furanyl 466 1 4-morpholino-phenyl ethyl 467 1 4-morpholino-phenyl n-propyl 468 1 4-morpholino-phenyl isopropyl 469 1 4-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 470 1 4-morpholino-phenyl CF.sub.3 471 1 4-morpholino-phenyl —CH.sub.2CF.sub.3 472 1 4-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 473 1 4-morpholino-phenyl cyclopropyl 474 1 4-morpholino-phenyl Cyclobutyl 475 1 4-morpholino-phenyl cyclopentyl 476 1 4-morpholino-phenyl cyclohexyl 477 1 4-morpholino-phenyl 3-pyridyl 478 1 4-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 479 1 4-morpholino-phenyl 1H-imidazol-4-yl 480 1 4-morpholino-phenyl 2-furanyl 481 1 4-methyl-2-morpholino-phenyl ethyl 482 1 4-methyl-2-morpholino-phenyl n-propyl 483 1 4-methyl-2-morpholino-phenyl isopropyl 484 1 4-methyl-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 485 1 4-methyl-2-morpholino-phenyl CF.sub.3 486 1 4-methyl-2-morpholino-phenyl —CH.sub.2CF.sub.3 487 1 4-methyl-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 488 1 4-methyl-2-morpholino-phenyl cyclopropyl 489 1 4-methyl-2-morpholino-phenyl Cyclobutyl 490 1 4-methyl-2-morpholino-phenyl cyclopentyl 491 1 4-methyl-2-morpholino-phenyl cyclohexyl 492 1 4-methyl-2-morpholino-phenyl 3-pyridyl 493 1 4-methyl-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 494 1 4-methyl-2-morpholino-phenyl 1H-imidazol-4-yl 495 1 4-methyl-2-morpholino-phenyl 2-furanyl 496 2 4-CH.sub.3-phenyl ethyl 497 2 4-CH.sub.3-phenyl n-propyl 498 2 4-CH.sub.3-phenyl isopropyl 499 2 4-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 500 2 4-CH.sub.3-phenyl CF.sub.3 501 2 4-CH.sub.3-phenyl —CH.sub.2CF.sub.3 502 2 4-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 503 2 4-CH.sub.3-phenyl cyclopropyl 504 2 4-CH.sub.3-phenyl Cyclobutyl 505 2 4-CH.sub.3-phenyl cyclopentyl 506 2 4-CH.sub.3-phenyl cyclohexyl 507 2 4-CH.sub.3-phenyl 3-pyridyl 508 2 4-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 509 2 4-CH.sub.3-phenyl 1H-imidazol-4-yl 510 2 4-CH.sub.3-phenyl 2-furanyl 511 2 3-CH.sub.3-phenyl ethyl 512 2 3-CH.sub.3-phenyl n-propyl 513 2 3-CH.sub.3-phenyl isopropyl 514 2 3-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 515 2 3-CH.sub.3-phenyl CF.sub.3 516 2 3-CH.sub.3-phenyl —CH.sub.2CF.sub.3 517 2 3-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 518 2 3-CH.sub.3-phenyl cyclopropyl 519 2 3-CH.sub.3-phenyl Cyclobutyl 520 2 3-CH.sub.3-phenyl cyclopentyl 521 2 3-CH.sub.3-phenyl cyclohexyl 522 2 3-CH.sub.3-phenyl 3-pyridyl 523 2 3-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 524 2 3-CH.sub.3-phenyl 1H-imidazol-4-yl 525 2 3-CH.sub.3-phenyl 2-furanyl 526 2 3-OH-Phenyl ethyl 527 2 3-OH-Phenyl n-propyl 528 2 3-OH-Phenyl isopropyl 529 2 3-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 530 2 3-OH-Phenyl CF.sub.3 531 2 3-OH-Phenyl —CH.sub.2CF.sub.3 532 2 3-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 533 2 3-OH-Phenyl cyclopropyl 534 2 3-OH-Phenyl Cyclobutyl 535 2 3-OH-Phenyl cyclopentyl 536 2 3-OH-Phenyl cyclohexyl 537 2 3-OH-Phenyl 3-pyridyl 538 2 3-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 539 2 3-OH-Phenyl 1H-imidazol-4-yl 540 2 3-OH-Phenyl 2-furanyl 541 2 4-OMe-Phenyl ethyl 542 2 4-OMe-Phenyl n-propyl 543 2 4-OMe-Phenyl isopropyl 544 2 4-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 545 2 4-OMe-Phenyl CF.sub.3 546 2 4-OMe-Phenyl —CH.sub.2CF.sub.3 547 2 4-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 548 2 4-OMe-Phenyl cyclopropyl 549 2 4-OMe-Phenyl Cyclobutyl 550 2 4-OMe-Phenyl cyclopentyl 551 2 4-OMe-Phenyl cyclohexyl 552 2 4-OMe-Phenyl 3-pyridyl 553 2 4-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 554 2 4-OMe-Phenyl 1H-imidazol-4-yl 555 2 4-OMe-Phenyl 2-furanyl 556 2 2-OMe-Phenyl ethyl 557 2 2-OMe-Phenyl n-propyl 558 2 2-OMe-Phenyl isopropyl 559 2 2-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 560 2 2-OMe-Phenyl CF.sub.3 561 2 2-OMe-Phenyl —CH.sub.2CF.sub.3 562 2 2-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 563 2 2-OMe-Phenyl cyclopropyl 564 2 2-OMe-Phenyl Cyclobutyl 565 2 2-OMe-Phenyl cyclopentyl 566 2 2-OMe-Phenyl cyclohexyl 567 2 2-OMe-Phenyl 3-pyridyl 568 2 2-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 569 2 2-OMe-Phenyl 1H-imidazol-4-yl 570 2 2-OMe-Phenyl 2-furanyl 571 2 3-CN-Phenyl ethyl 572 2 3-CN-Phenyl n-propyl 573 2 3-CN-Phenyl isopropyl 574 2 3-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 575 2 3-CN-Phenyl CF.sub.3 576 2 3-CN-Phenyl —CH.sub.2CF.sub.3 577 2 3-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 578 2 3-CN-Phenyl cyclopropyl 579 2 3-CN-Phenyl Cyclobutyl 580 2 3-CN-Phenyl cyclopentyl 581 2 3-CN-Phenyl cyclohexyl 582 2 3-CN-Phenyl 3-pyridyl 583 2 3-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 584 2 3-CN-Phenyl 1H-imidazol-4-yl 585 2 3-CN-Phenyl 2-furanyl 586 2 2-F-Phenyl ethyl 587 2 2-F-Phenyl n-propyl 588 2 2-F-Phenyl isopropyl 589 2 2-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 590 2 2-F-Phenyl CF.sub.3 591 2 2-F-Phenyl —CH.sub.2CF.sub.3 592 2 2-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 593 2 2-F-Phenyl cyclopropyl 594 2 2-F-Phenyl Cyclobutyl 595 2 2-F-Phenyl cyclopentyl 596 2 2-F-Phenyl cyclohexyl 597 2 2-F-Phenyl 3-pyridyl 598 2 2-F-Phenyl 1-methyl-1H-pyrazol-4-yl 599 2 2-F-Phenyl 1H-imidazol-4-yl 600 2 2-F-Phenyl 2-furanyl 601 2 4-F-Phenyl ethyl 602 2 4-F-Phenyl n-propyl 603 2 4-F-Phenyl isopropyl 604 2 4-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 605 2 4-F-Phenyl CF.sub.3 606 2 4-F-Phenyl —CH.sub.2CF.sub.3 607 2 4-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 608 2 4-F-Phenyl cyclopropyl 609 2 4-F-Phenyl Cyclobutyl 610 2 4-F-Phenyl cyclopentyl 611 2 4-F-Phenyl cyclohexyl 612 2 4-F-Phenyl 3-pyridyl 613 2 4-F-Phenyl 1-methyl-1H-pyrazol-4-yl 614 2 4-F-Phenyl 1H-imidazol-4-yl 615 2 4-F-Phenyl 2-furanyl 616 2 3-Cl-Phenyl ethyl 617 2 3-Cl-Phenyl n-propyl 618 2 3-Cl-Phenyl isopropyl 619 2 3-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 620 2 3-Cl-Phenyl CF.sub.3 621 2 3-Cl-Phenyl —CH.sub.2CF.sub.3 622 2 3-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 623 2 3-Cl-Phenyl cyclopropyl 624 2 3-Cl-Phenyl Cyclobutyl 625 2 3-Cl-Phenyl cyclopentyl 626 2 3-Cl-Phenyl cyclohexyl 627 2 3-Cl-Phenyl 3-pyridyl 628 2 3-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 629 2 3-Cl-Phenyl 1H-imidazol-4-yl 630 2 3-Cl-Phenyl 2-furanyl 631 2 2-Br-Phenyl ethyl 632 2 2-Br-Phenyl n-propyl 633 2 2-Br-Phenyl isopropyl 634 2 2-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 635 2 2-Br-Phenyl CF.sub.3 636 2 2-Br-Phenyl —CH.sub.2CF.sub.3 637 2 2-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 638 2 2-Br-Phenyl cyclopropyl 639 2 2-Br-Phenyl Cyclobutyl 640 2 2-Br-Phenyl cyclopentyl 641 2 2-Br-Phenyl cyclohexyl 642 2 2-Br-Phenyl 3-pyridyl 643 2 2-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 644 2 2-Br-Phenyl 1H-imidazol-4-yl 645 2 2-Br-Phenyl 2-furanyl 646 2 4-Br-Phenyl ethyl 647 2 4-Br-Phenyl n-propyl 648 2 4-Br-Phenyl isopropyl 649 2 4-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 650 2 4-Br-Phenyl CF.sub.3 651 2 4-Br-Phenyl —CH.sub.2CF.sub.3 652 2 4-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 653 2 4-Br-Phenyl cyclopropyl 654 2 4-Br-Phenyl Cyclobutyl 655 2 4-Br-Phenyl cyclopentyl 656 2 4-Br-Phenyl cyclohexyl 657 2 4-Br-Phenyl 3-pyridyl 658 2 4-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 659 2 4-Br-Phenyl 1H-imidazol-4-yl 660 2 4-Br-Phenyl 2-furanyl 661 2 3-CF.sub.3-Phenyl ethyl 662 2 3-CF.sub.3-Phenyl n-propyl 663 2 3-CF.sub.3-Phenyl isopropyl 664 2 3-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 665 2 3-CF.sub.3-Phenyl CF.sub.3 666 2 3-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 667 2 3-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 668 2 3-CF.sub.3-Phenyl cyclopropyl 669 2 3-CF.sub.3-Phenyl Cyclobutyl 670 2 3-CF.sub.3-Phenyl cyclopentyl 671 2 3-CF.sub.3-Phenyl cyclohexyl 672 2 3-CF.sub.3-Phenyl 3-pyridyl 673 2 3-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 674 2 3-CF.sub.3-Phenyl 1H-imidazol-4-yl 675 2 3-CF.sub.3-Phenyl 2-furanyl 676 2 2-iPr-Phenyl ethyl 677 2 2-iPr-Phenyl n-propyl 678 2 2-iPr-Phenyl isopropyl 679 2 2-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 680 2 2-iPr-Phenyl CF.sub.3 681 2 2-iPr-Phenyl —CH.sub.2CF.sub.3 682 2 2-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 683 2 2-iPr-Phenyl cyclopropyl 684 2 2-iPr-Phenyl Cyclobutyl 685 2 2-iPr-Phenyl cyclopentyl 686 2 2-iPr-Phenyl cyclohexyl 687 2 2-iPr-Phenyl 3-pyridyl 688 2 2-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 689 2 2-iPr-Phenyl 1H-imidazol-4-yl 690 2 2-iPr-Phenyl 2-furanyl 691 2 4-iPr-Phenyl ethyl 692 2 4-iPr-Phenyl n-propyl 693 2 4-iPr-Phenyl isopropyl 694 2 4-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 695 2 4-iPr-Phenyl CF.sub.3 696 2 4-iPr-Phenyl —CH.sub.2CF.sub.3 697 2 4-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 698 2 4-iPr-Phenyl cyclopropyl 699 2 4-iPr-Phenyl Cyclobutyl 700 2 4-iPr-Phenyl cyclopentyl 701 2 4-iPr-Phenyl cyclohexyl 702 2 4-iPr-Phenyl 3-pyridyl 703 2 4-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 704 2 4-iPr-Phenyl 1H-imidazol-4-yl 705 2 4-iPr-Phenyl 2-furanyl 706 2 3-morpholino-phenyl ethyl 707 2 3-morpholino-phenyl n-propyl 708 2 3-morpholino-phenyl isopropyl 709 2 3-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 710 2 3-morpholino-phenyl CF.sub.3 711 2 3-morpholino-phenyl —CH.sub.2CF.sub.3 712 2 3-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 713 2 3-morpholino-phenyl cyclopropyl 714 2 3-morpholino-phenyl Cyclobutyl 715 2 3-morpholino-phenyl cyclopentyl 716 2 3-morpholino-phenyl cyclohexyl 717 2 3-morpholino-phenyl 3-pyridyl 718 2 3-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 719 2 3-morpholino-phenyl 1H-imidazol-4-yl 720 2 3-morpholino-phenyl 2-furanyl 721 2 4-cyano-2-morpholino-phenyl ethyl 722 2 4-cyano-2-morpholino-phenyl n-propyl 723 2 4-cyano-2-morpholino-phenyl isopropyl 724 2 4-cyano-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 725 2 4-cyano-2-morpholino-phenyl CF.sub.3 726 2 4-cyano-2-morpholino-phenyl —CH.sub.2CF.sub.3 727 2 4-cyano-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 728 2 4-cyano-2-morpholino-phenyl cyclopropyl 729 2 4-cyano-2-morpholino-phenyl Cyclobutyl 730 2 4-cyano-2-morpholino-phenyl cyclopentyl 731 2 4-cyano-2-morpholino-phenyl cyclohexyl 732 2 4-cyano-2-morpholino-phenyl 3-pyridyl 733 2 4-cyano-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 734 2 4-cyano-2-morpholino-phenyl 1H-imidazol-4-yl 735 2 4-cyano-2-morpholino-phenyl 2-furanyl 736 2 4-hydroxy-2-morpholino-phenyl ethyl 737 2 4-hydroxy-2-morpholino-phenyl n-propyl 738 2 4-hydroxy-2-morpholino-phenyl isopropyl 739 2 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 740 2 4-hydroxy-2-morpholino-phenyl CF.sub.3 741 2 4-hydroxy-2-morpholino-phenyl —CH.sub.2CF.sub.3 742 2 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 743 2 4-hydroxy-2-morpholino-phenyl cyclopropyl 744 2 4-hydroxy-2-morpholino-phenyl Cyclobutyl 745 2 4-hydroxy-2-morpholino-phenyl cyclopentyl 746 2 4-hydroxy-2-morpholino-phenyl cyclohexyl 747 2 4-hydroxy-2-morpholino-phenyl 3-pyridyl 748 2 4-hydroxy-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 749 2 4-hydroxy-2-morpholino-phenyl 1H-imidazol-4-yl 750 2 4-hydroxy-2-morpholino-phenyl 2-furanyl 751 2 2-CH.sub.3-phenyl Ethyl 752 2 2-CH.sub.3-phenyl n-propyl 753 2 2-CH.sub.3-phenyl Isopropyl 754 2 2-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 755 2 2-CH.sub.3-phenyl CF.sub.3 756 2 2-CH.sub.3-phenyl —CH.sub.2CF.sub.3 757 2 2-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 758 2 2-CH.sub.3-phenyl cyclopropyl 759 2 2-CH.sub.3-phenyl Cyclobutyl 760 2 2-CH.sub.3-phenyl cyclopentyl 761 2 2-CH.sub.3-phenyl cyclohexyl 762 2 2-CH.sub.3-phenyl 3-pyridyl 763 2 2-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 764 2 2-CH.sub.3-phenyl 1H-imidazol-4-yl 765 2 2-CH.sub.3-phenyl 2-furanyl 766 2 4-OH-Phenyl Ethyl 767 2 4-OH-Phenyl n-propyl 768 2 4-OH-Phenyl Isopropyl 769 2 4-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 770 2 4-OH-Phenyl CF.sub.3 771 2 4-OH-Phenyl —CH.sub.2CF.sub.3 772 2 4-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 773 2 4-OH-Phenyl cyclopropyl 774 2 4-OH-Phenyl Cyclobutyl 775 2 4-OH-Phenyl cyclopentyl 776 2 4-OH-Phenyl cyclohexyl 777 2 4-OH-Phenyl 3-pyridyl 778 2 4-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 779 2 4-OH-Phenyl 1H-imidazol-4-yl 780 2 4-OH-Phenyl 2-furanyl 781 2 2-OH-Phenyl Ethyl 782 2 2-OH-Phenyl n-propyl 783 2 2-OH-Phenyl Isopropyl 784 2 2-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 785 2 2-OH-Phenyl CF.sub.3 786 2 2-OH-Phenyl —CH.sub.2CF.sub.3 787 2 2-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 788 2 2-OH-Phenyl cyclopropyl 789 2 2-OH-Phenyl Cyclobutyl 790 2 2-OH-Phenyl cyclopentyl 791 2 2-OH-Phenyl cyclohexyl 792 2 2-OH-Phenyl 3-pyridyl 793 2 2-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 794 2 2-OH-Phenyl 1H-imidazol-4-yl 795 2 2-OH-Phenyl 2-furanyl 796 2 3-OMe-Phenyl Ethyl 797 2 3-OMe-Phenyl n-propyl 798 2 3-OMe-Phenyl Isopropyl 799 2 3-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 800 2 3-OMe-Phenyl CF.sub.3 801 2 3-OMe-Phenyl —CH.sub.2CF.sub.3 802 2 3-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 803 2 3-OMe-Phenyl cyclopropyl 804 2 3-OMe-Phenyl Cyclobutyl 805 2 3-OMe-Phenyl cyclopentyl 806 2 3-OMe-Phenyl cyclohexyl 807 2 3-OMe-Phenyl 3-pyridyl 808 2 3-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 809 2 3-OMe-Phenyl 1H-imidazol-4-yl 810 2 3-OMe-Phenyl 2-furanyl 811 2 4-CN-Phenyl Ethyl 812 2 4-CN-Phenyl n-propyl 813 2 4-CN-Phenyl Isopropyl 814 2 4-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 815 2 4-CN-Phenyl CF.sub.3 816 2 4-CN-Phenyl —CH.sub.2CF.sub.3 817 2 4-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 818 2 4-CN-Phenyl cyclopropyl 819 2 4-CN-Phenyl Cyclobutyl 820 2 4-CN-Phenyl cyclopentyl 821 2 4-CN-Phenyl cyclohexyl 822 2 4-CN-Phenyl 3-pyridyl 823 2 4-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 824 2 4-CN-Phenyl 1H-imidazol-4-yl 825 2 4-CN-Phenyl 2-furanyl 826 2 2-CN-Phenyl Ethyl 827 2 2-CN-Phenyl n-propyl 828 2 2-CN-Phenyl Isopropyl 829 2 2-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 830 2 2-CN-Phenyl CF.sub.3 831 2 2-CN-Phenyl —CH.sub.2CF.sub.3 832 2 2-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 833 2 2-CN-Phenyl cyclopropyl 834 2 2-CN-Phenyl Cyclobutyl 835 2 2-CN-Phenyl cyclopentyl 836 2 2-CN-Phenyl cyclohexyl 837 2 2-CN-Phenyl 3-pyridyl 838 2 2-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 839 2 2-CN-Phenyl 1H-imidazol-4-yl 840 2 2-CN-Phenyl 2-furanyl 841 2 3-F-Phenyl Ethyl 842 2 3-F-Phenyl n-propyl 843 2 3-F-Phenyl Isopropyl 844 2 3-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 845 2 3-F-Phenyl CF.sub.3 846 2 3-F-Phenyl —CH.sub.2CF.sub.3 847 2 3-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 848 2 3-F-Phenyl cyclopropyl 849 2 3-F-Phenyl Cyclobutyl 850 2 3-F-Phenyl cyclopentyl 851 2 3-F-Phenyl cyclohexyl 852 2 3-F-Phenyl 3-pyridyl 853 2 3-F-Phenyl 1-methyl-1H-pyrazol-4-yl 854 2 3-F-Phenyl 1H-imidazol-4-yl 855 2 3-F-Phenyl 2-furanyl 856 2 2-Cl-Phenyl Ethyl 857 2 2-Cl-Phenyl n-propyl 858 2 2-Cl-Phenyl Isopropyl 859 2 2-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 860 2 2-Cl-Phenyl CF.sub.3 861 2 2-Cl-Phenyl —CH.sub.2CF.sub.3 862 2 2-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 863 2 2-Cl-Phenyl cyclopropyl 864 2 2-Cl-Phenyl Cyclobutyl 865 2 2-Cl-Phenyl cyclopentyl 866 2 2-Cl-Phenyl cyclohexyl 867 2 2-Cl-Phenyl 3-pyridyl 868 2 2-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 869 2 2-Cl-Phenyl 1H-imidazol-4-yl 870 2 2-Cl-Phenyl 2-furanyl 871 2 4-Cl-Phenyl Ethyl 872 2 4-Cl-Phenyl n-propyl 873 2 4-Cl-Phenyl Isopropyl 874 2 4-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 875 2 4-Cl-Phenyl CF.sub.3 876 2 4-Cl-Phenyl —CH.sub.2CF.sub.3 877 2 4-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 878 2 4-Cl-Phenyl cyclopropyl 879 2 4-Cl-Phenyl Cyclobutyl 880 2 4-Cl-Phenyl cyclopentyl 881 2 4-Cl-Phenyl cyclohexyl 882 2 4-Cl-Phenyl 3-pyridyl 883 2 4-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 884 2 4-Cl-Phenyl 1H-imidazol-4-yl 885 2 4-Cl-Phenyl 2-furanyl 886 2 3-Br-Phenyl Ethyl 887 2 3-Br-Phenyl n-propyl 888 2 3-Br-Phenyl Isopropyl 889 2 3-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 890 2 3-Br-Phenyl CF.sub.3 891 2 3-Br-Phenyl —CH.sub.2CF.sub.3 892 2 3-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 893 2 3-Br-Phenyl cyclopropyl 894 2 3-Br-Phenyl Cyclobutyl 895 2 3-Br-Phenyl cyclopentyl 896 2 3-Br-Phenyl cyclohexyl 897 2 3-Br-Phenyl 3-pyridyl 898 2 3-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 899 2 3-Br-Phenyl 1H-imidazol-4-yl 900 2 3-Br-Phenyl 2-furanyl 901 2 2-CF.sub.3-Phenyl Ethyl 902 2 2-CF.sub.3-Phenyl n-propyl 903 2 2-CF.sub.3-Phenyl Isopropyl 904 2 2-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 905 2 2-CF.sub.3-Phenyl CF.sub.3 906 2 2-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 907 2 2-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 908 2 2-CF.sub.3-Phenyl cyclopropyl 909 2 2-CF.sub.3-Phenyl Cyclobutyl 910 2 2-CF.sub.3-Phenyl cyclopentyl 911 2 2-CF.sub.3-Phenyl cyclohexyl 912 2 2-CF.sub.3-Phenyl 3-pyridyl 913 2 2-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 914 2 2-CF.sub.3-Phenyl 1H-imidazol-4-yl 915 2 2-CF.sub.3-Phenyl 2-furanyl 916 2 4-CF.sub.3-Phenyl Ethyl 917 2 4-CF.sub.3-Phenyl n-propyl 918 2 4-CF.sub.3-Phenyl Isopropyl 919 2 4-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 920 2 4-CF.sub.3-Phenyl CF.sub.3 921 2 4-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 922 2 4-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 923 2 4-CF.sub.3-Phenyl cyclopropyl 924 2 4-CF.sub.3-Phenyl Cyclobutyl 925 2 4-CF.sub.3-Phenyl cyclopentyl 926 2 4-CF.sub.3-Phenyl cyclohexyl 927 2 4-CF.sub.3-Phenyl 3-pyridyl 928 2 4-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 929 2 4-CF.sub.3-Phenyl 1H-imidazol-4-yl 930 2 4-CF.sub.3-Phenyl 2-furanyl 931 2 3-iPr-Phenyl Ethyl 932 2 3-iPr-Phenyl n-propyl 933 2 3-iPr-Phenyl Isopropyl 934 2 3-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 935 2 3-iPr-Phenyl CF.sub.3 936 2 3-iPr-Phenyl —CH.sub.2CF.sub.3 937 2 3-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 938 2 3-iPr-Phenyl cyclopropyl 939 2 3-iPr-Phenyl Cyclobutyl 940 2 3-iPr-Phenyl cyclopentyl 941 2 3-iPr-Phenyl cyclohexyl 942 2 3-iPr-Phenyl 3-pyridyl 943 2 3-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 944 2 3-iPr-Phenyl 1H-imidazol-4-yl 945 2 3-iPr-Phenyl 2-furanyl 946 2 2-morpholino-phenyl Ethyl 947 2 2-morpholino-phenyl n-propyl 948 2 2-morpholino-phenyl isopropyl 949 2 2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 950 2 2-morpholino-phenyl CF.sub.3 951 2 2-morpholino-phenyl —CH.sub.2CF.sub.3 952 2 2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 953 2 2-morpholino-phenyl cyclopropyl 954 2 2-morpholino-phenyl Cyclobutyl 955 2 2-morpholino-phenyl cyclopentyl 956 2 2-morpholino-phenyl cyclohexyl 957 2 2-morpholino-phenyl 3-pyridyl 958 2 2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 959 2 2-morpholino-phenyl 1H-imidazol-4-yl 960 2 2-morpholino-phenyl 2-furanyl 961 2 4-morpholino-phenyl ethyl 962 2 4-morpholino-phenyl n-propyl 963 2 4-morpholino-phenyl isopropyl 964 2 4-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 965 2 4-morpholino-phenyl CF.sub.3 966 2 4-morpholino-phenyl —CH.sub.2CF.sub.3 967 2 4-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 968 2 4-morpholino-phenyl cyclopropyl 969 2 4-morpholino-phenyl Cyclobutyl 970 2 4-morpholino-phenyl cyclopentyl 971 2 4-morpholino-phenyl cyclohexyl 972 2 4-morpholino-phenyl 3-pyridyl 973 2 4-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 974 2 4-morpholino-phenyl 1H-imidazol-4-yl 975 2 4-morpholino-phenyl 2-furanyl 976 2 4-methyl-2-morpholino-phenyl ethyl 977 2 4-methyl-2-morpholino-phenyl n-propyl 978 2 4-methyl-2-morpholino-phenyl isopropyl 979 2 4-methyl-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 980 2 4-methyl-2-morpholino-phenyl CF.sub.3 981 2 4-methyl-2-morpholino-phenyl —CH.sub.2CF.sub.3 982 2 4-methyl-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 983 2 4-methyl-2-morpholino-phenyl cyclopropyl 984 2 4-methyl-2-morpholino-phenyl Cyclobutyl 985 2 4-methyl-2-morpholino-phenyl cyclopentyl 986 2 4-methyl-2-morpholino-phenyl cyclohexyl 987 2 4-methyl-2-morpholino-phenyl 3-pyridyl 988 2 4-methyl-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 989 2 4-methyl-2-morpholino-phenyl 1H-imidazol-4-yl 990 2 4-methyl-2-morpholino-phenyl 2-furanyl 991 3 4-CH.sub.3-phenyl ethyl 992 3 4-CH.sub.3-phenyl n-propyl 993 3 4-CH.sub.3-phenyl isopropyl 994 3 4-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 995 3 4-CH.sub.3-phenyl CF.sub.3 996 3 4-CH.sub.3-phenyl —CH.sub.2CF.sub.3 997 3 4-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 998 3 4-CH.sub.3-phenyl cyclopropyl 999 3 4-CH.sub.3-phenyl Cyclobutyl 1000 3 4-CH.sub.3-phenyl cyclopentyl 1001 3 4-CH.sub.3-phenyl cyclohexyl 1002 3 4-CH.sub.3-phenyl 3-pyridyl 1003 3 4-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1004 3 4-CH.sub.3-phenyl 1H-imidazol-4-yl 1005 3 4-CH.sub.3-phenyl 2-furanyl 1006 3 3-CH.sub.3-phenyl ethyl 1007 3 3-CH.sub.3-phenyl n-propyl 1008 3 3-CH.sub.3-phenyl isopropyl 1009 3 3-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1010 3 3-CH.sub.3-phenyl CF.sub.3 1011 3 3-CH.sub.3-phenyl —CH.sub.2CF.sub.3 1012 3 3-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 1013 3 3-CH.sub.3-phenyl cyclopropyl 1014 3 3-CH.sub.3-phenyl Cyclobutyl 1015 3 3-CH.sub.3-phenyl cyclopentyl 1016 3 3-CH.sub.3-phenyl cyclohexyl 1017 3 3-CH.sub.3-phenyl 3-pyridyl 1018 3 3-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1019 3 3-CH.sub.3-phenyl 1H-imidazol-4-yl 1020 3 3-CH.sub.3-phenyl 2-furanyl 1021 3 3-OH-Phenyl ethyl 1022 3 3-OH-Phenyl n-propyl 1023 3 3-OH-Phenyl isopropyl 1024 3 3-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1025 3 3-OH-Phenyl CF.sub.3 1026 3 3-OH-Phenyl —CH.sub.2CF.sub.3 1027 3 3-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1028 3 3-OH-Phenyl cyclopropyl 1029 3 3-OH-Phenyl Cyclobutyl 1030 3 3-OH-Phenyl cyclopentyl 1031 3 3-OH-Phenyl cyclohexyl 1032 3 3-OH-Phenyl 3-pyridyl 1033 3 3-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1034 3 3-OH-Phenyl 1H-imidazol-4-yl 1035 3 3-OH-Phenyl 2-furanyl 1036 3 4-OMe-Phenyl ethyl 1037 3 4-OMe-Phenyl n-propyl 1038 3 4-OMe-Phenyl isopropyl 1039 3 4-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1040 3 4-OMe-Phenyl CF.sub.3 1041 3 4-OMe-Phenyl —CH.sub.2CF.sub.3 1042 3 4-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1043 3 4-OMe-Phenyl cyclopropyl 1044 3 4-OMe-Phenyl Cyclobutyl 1045 3 4-OMe-Phenyl cyclopentyl 1046 3 4-OMe-Phenyl cyclohexyl 1047 3 4-OMe-Phenyl 3-pyridyl 1048 3 4-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1049 3 4-OMe-Phenyl 1H-imidazol-4-yl 1050 3 4-OMe-Phenyl 2-furanyl 1051 3 2-OMe-Phenyl ethyl 1052 3 2-OMe-Phenyl n-propyl 1053 3 2-OMe-Phenyl isopropyl 1054 3 2-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1055 3 2-OMe-Phenyl CF.sub.3 1056 3 2-OMe-Phenyl —CH.sub.2CF.sub.3 1057 3 2-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1058 3 2-OMe-Phenyl cyclopropyl 1059 3 2-OMe-Phenyl Cyclobutyl 1060 3 2-OMe-Phenyl cyclopentyl 1061 3 2-OMe-Phenyl cyclohexyl 1062 3 2-OMe-Phenyl 3-pyridyl 1063 3 2-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1064 3 2-OMe-Phenyl 1H-imidazol-4-yl 1065 3 2-OMe-Phenyl 2-furanyl 1066 3 3-CN-Phenyl ethyl 1067 3 3-CN-Phenyl n-propyl 1068 3 3-CN-Phenyl isopropyl 1069 3 3-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1070 3 3-CN-Phenyl CF.sub.3 1071 3 3-CN-Phenyl —CH.sub.2CF.sub.3 1072 3 3-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1073 3 3-CN-Phenyl cyclopropyl 1074 3 3-CN-Phenyl Cyclobutyl 1075 3 3-CN-Phenyl cyclopentyl 1076 3 3-CN-Phenyl cyclohexyl 1077 3 3-CN-Phenyl 3-pyridyl 1078 3 3-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1079 3 3-CN-Phenyl 1H-imidazol-4-yl 1080 3 3-CN-Phenyl 2-furanyl 1081 3 2-F-Phenyl ethyl 1082 3 2-F-Phenyl n-propyl 1083 3 2-F-Phenyl isopropyl 1084 3 2-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1085 3 2-F-Phenyl CF.sub.3 1086 3 2-F-Phenyl —CH.sub.2CF.sub.3 1087 3 2-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1088 3 2-F-Phenyl cyclopropyl 1089 3 2-F-Phenyl Cyclobutyl 1090 3 2-F-Phenyl cyclopentyl 1091 3 2-F-Phenyl cyclohexyl 1092 3 2-F-Phenyl 3-pyridyl 1093 3 2-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1094 3 2-F-Phenyl 1H-imidazol-4-yl 1095 3 2-F-Phenyl 2-furanyl 1096 3 4-F-Phenyl ethyl 1097 3 4-F-Phenyl n-propyl 1098 3 4-F-Phenyl isopropyl 1099 3 4-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1100 3 4-F-Phenyl CF.sub.3 1101 3 4-F-Phenyl —CH.sub.2CF.sub.3 1102 3 4-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1103 3 4-F-Phenyl cyclopropyl 1104 3 4-F-Phenyl Cyclobutyl 1105 3 4-F-Phenyl cyclopentyl 1106 3 4-F-Phenyl cyclohexyl 1107 3 4-F-Phenyl 3-pyridyl 1108 3 4-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1109 3 4-F-Phenyl 1H-imidazol-4-yl 1110 3 4-F-Phenyl 2-furanyl 1111 3 3-Cl-Phenyl ethyl 1112 3 3-Cl-Phenyl n-propyl 1113 3 3-Cl-Phenyl isopropyl 1114 3 3-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1115 3 3-Cl-Phenyl CF.sub.3 1116 3 3-Cl-Phenyl —CH.sub.2CF.sub.3 1117 3 3-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1118 3 3-Cl-Phenyl cyclopropyl 1119 3 3-Cl-Phenyl Cyclobutyl 1120 3 3-Cl-Phenyl cyclopentyl 1121 3 3-Cl-Phenyl cyclohexyl 1122 3 3-Cl-Phenyl 3-pyridyl 1123 3 3-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1124 3 3-Cl-Phenyl 1H-imidazol-4-yl 1125 3 3-Cl-Phenyl 2-furanyl 1126 3 2-Br-Phenyl ethyl 1127 3 2-Br-Phenyl n-propyl 1128 3 2-Br-Phenyl isopropyl 1129 3 2-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1130 3 2-Br-Phenyl CF.sub.3 1131 3 2-Br-Phenyl —CH.sub.2CF.sub.3 1132 3 2-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1133 3 2-Br-Phenyl cyclopropyl 1134 3 2-Br-Phenyl Cyclobutyl 1135 3 2-Br-Phenyl cyclopentyl 1136 3 2-Br-Phenyl cyclohexyl 1137 3 2-Br-Phenyl 3-pyridyl 1138 3 2-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1139 3 2-Br-Phenyl 1H-imidazol-4-yl 1140 3 2-Br-Phenyl 2-furanyl 1141 3 4-Br-Phenyl ethyl 1142 3 4-Br-Phenyl n-propyl 1143 3 4-Br-Phenyl isopropyl 1144 3 4-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1145 3 4-Br-Phenyl CF.sub.3 1146 3 4-Br-Phenyl —CH.sub.2CF.sub.3 1147 3 4-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1148 3 4-Br-Phenyl cyclopropyl 1149 3 4-Br-Phenyl Cyclobutyl 1150 3 4-Br-Phenyl cyclopentyl 1151 3 4-Br-Phenyl cyclohexyl 1152 3 4-Br-Phenyl 3-pyridyl 1153 3 4-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1154 3 4-Br-Phenyl 1H-imidazol-4-yl 1155 3 4-Br-Phenyl 2-furanyl 1156 3 3-CF.sub.3-Phenyl ethyl 1157 3 3-CF.sub.3-Phenyl n-propyl 1158 3 3-CF.sub.3-Phenyl isopropyl 1159 3 3-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1160 3 3-CF.sub.3-Phenyl CF.sub.3 1161 3 3-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1162 3 3-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1163 3 3-CF.sub.3-Phenyl cyclopropyl 1164 3 3-CF.sub.3-Phenyl Cyclobutyl 1165 3 3-CF.sub.3-Phenyl cyclopentyl 1166 3 3-CF.sub.3-Phenyl cyclohexyl 1167 3 3-CF.sub.3-Phenyl 3-pyridyl 1168 3 3-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1169 3 3-CF.sub.3-Phenyl 1H-imidazol-4-yl 1170 3 3-CF.sub.3-Phenyl 2-furanyl 1171 3 2-iPr-Phenyl ethyl 1172 3 2-iPr-Phenyl n-propyl 1173 3 2-iPr-Phenyl isopropyl 1174 3 2-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1175 3 2-iPr-Phenyl CF.sub.3 1176 3 2-iPr-Phenyl —CH.sub.2CF.sub.3 1177 3 2-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1178 3 2-iPr-Phenyl cyclopropyl 1179 3 2-iPr-Phenyl Cyclobutyl 1180 3 2-iPr-Phenyl cyclopentyl 1181 3 2-iPr-Phenyl cyclohexyl 1182 3 2-iPr-Phenyl 3-pyridyl 1183 3 2-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1184 3 2-iPr-Phenyl 1H-imidazol-4-yl 1185 3 2-iPr-Phenyl 2-furanyl 1186 3 4-iPr-Phenyl ethyl 1187 3 4-iPr-Phenyl n-propyl 1188 3 4-iPr-Phenyl isopropyl 1189 3 4-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1190 3 4-iPr-Phenyl CF.sub.3 1191 3 4-iPr-Phenyl —CH.sub.2CF.sub.3 1192 3 4-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1193 3 4-iPr-Phenyl cyclopropyl 1194 3 4-iPr-Phenyl Cyclobutyl 1195 3 4-iPr-Phenyl cyclopentyl 1196 3 4-iPr-Phenyl cyclohexyl 1197 3 4-iPr-Phenyl 3-pyridyl 1198 3 4-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1199 3 4-iPr-Phenyl 1H-imidazol-4-yl 1200 3 4-iPr-Phenyl 2-furanyl 1201 3 3-morpholino-phenyl ethyl 1202 3 3-morpholino-phenyl n-propyl 1203 3 3-morpholino-phenyl isopropyl 1204 3 3-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1205 3 3-morpholino-phenyl CF.sub.3 1206 3 3-morpholino-phenyl —CH.sub.2CF.sub.3 1207 3 3-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1208 3 3-morpholino-phenyl cyclopropyl 1209 3 3-morpholino-phenyl Cyclobutyl 1210 3 3-morpholino-phenyl cyclopentyl 1211 3 3-morpholino-phenyl cyclohexyl 1212 3 3-morpholino-phenyl 3-pyridyl 1213 3 3-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1214 3 3-morpholino-phenyl 1H-imidazol-4-yl 1215 3 3-morpholino-phenyl 2-furanyl 1216 3 4-cyano-2-morpholino-phenyl ethyl 1217 3 4-cyano-2-morpholino-phenyl n-propyl 1218 3 4-cyano-2-morpholino-phenyl isopropyl 1219 3 4-cyano-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1220 3 4-cyano-2-morpholino-phenyl CF.sub.3 1221 3 4-cyano-2-morpholino-phenyl —CH.sub.2CF.sub.3 1222 3 4-cyano-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1223 3 4-cyano-2-morpholino-phenyl cyclopropyl 1224 3 4-cyano-2-morpholino-phenyl Cyclobutyl 1225 3 4-cyano-2-morpholino-phenyl cyclopentyl 1226 3 4-cyano-2-morpholino-phenyl cyclohexyl 1227 3 4-cyano-2-morpholino-phenyl 3-pyridyl 1228 3 4-cyano-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1229 3 4-cyano-2-morpholino-phenyl 1H-imidazol-4-yl 1230 3 4-cyano-2-morpholino-phenyl 2-furanyl 1231 3 4-hydroxy-2-morpholino-phenyl ethyl 1232 3 4-hydroxy-2-morpholino-phenyl n-propyl 1233 3 4-hydroxy-2-morpholino-phenyl isopropyl 1234 3 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1235 3 4-hydroxy-2-morpholino-phenyl CF.sub.3 1236 3 4-hydroxy-2-morpholino-phenyl —CH.sub.2CF.sub.3 1237 3 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1238 3 4-hydroxy-2-morpholino-phenyl cyclopropyl 1239 3 4-hydroxy-2-morpholino-phenyl Cyclobutyl 1240 3 4-hydroxy-2-morpholino-phenyl cyclopentyl 1241 3 4-hydroxy-2-morpholino-phenyl cyclohexyl 1242 3 4-hydroxy-2-morpholino-phenyl 3-pyridyl 1243 3 4-hydroxy-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1244 3 4-hydroxy-2-morpholino-phenyl 1H-imidazol-4-yl 1245 3 4-hydroxy-2-morpholino-phenyl 2-furanyl 1246 3 2-CH.sub.3-phenyl Ethyl 1247 3 2-CH.sub.3-phenyl n-propyl 1248 3 2-CH.sub.3-phenyl Isopropyl 1249 3 2-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1250 3 2-CH.sub.3-phenyl CF.sub.3 1251 3 2-CH.sub.3-phenyl —CH.sub.2CF.sub.3 1252 3 2-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 1253 3 2-CH.sub.3-phenyl cyclopropyl 1254 3 2-CH.sub.3-phenyl Cyclobutyl 1255 3 2-CH.sub.3-phenyl cyclopentyl 1256 3 2-CH.sub.3-phenyl cyclohexyl 1257 3 2-CH.sub.3-phenyl 3-pyridyl 1258 3 2-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1259 3 2-CH.sub.3-phenyl 1H-imidazol-4-yl 1260 3 2-CH.sub.3-phenyl 2-furanyl 1261 3 4-OH-Phenyl Ethyl 1262 3 4-OH-Phenyl n-propyl 1263 3 4-OH-Phenyl Isopropyl 1264 3 4-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1265 3 4-OH-Phenyl CF.sub.3 1266 3 4-OH-Phenyl —CH.sub.2CF.sub.3 1267 3 4-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1268 3 4-OH-Phenyl cyclopropyl 1269 3 4-OH-Phenyl Cyclobutyl 1270 3 4-OH-Phenyl cyclopentyl 1271 3 4-OH-Phenyl cyclohexyl 1272 3 4-OH-Phenyl 3-pyridyl 1273 3 4-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1274 3 4-OH-Phenyl 1H-imidazol-4-yl 1275 3 4-OH-Phenyl 2-furanyl 1276 3 2-OH-Phenyl Ethyl 1277 3 2-OH-Phenyl n-propyl 1278 3 2-OH-Phenyl Isopropyl 1279 3 2-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1280 3 2-OH-Phenyl CF.sub.3 1281 3 2-OH-Phenyl —CH.sub.2CF.sub.3 1282 3 2-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1283 3 2-OH-Phenyl cyclopropyl 1284 3 2-OH-Phenyl Cyclobutyl 1285 3 2-OH-Phenyl cyclopentyl 1286 3 2-OH-Phenyl cyclohexyl 1287 3 2-OH-Phenyl 3-pyridyl 1288 3 2-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1289 3 2-OH-Phenyl 1H-imidazol-4-yl 1290 3 2-OH-Phenyl 2-furanyl 1291 3 3-OMe-Phenyl Ethyl 1292 3 3-OMe-Phenyl n-propyl 1293 3 3-OMe-Phenyl Isopropyl 1294 3 3-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1295 3 3-OMe-Phenyl CF.sub.3 1296 3 3-OMe-Phenyl —CH.sub.2CF.sub.3 1297 3 3-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1298 3 3-OMe-Phenyl cyclopropyl 1299 3 3-OMe-Phenyl Cyclobutyl 1300 3 3-OMe-Phenyl cyclopentyl 1301 3 3-OMe-Phenyl cyclohexyl 1302 3 3-OMe-Phenyl 3-pyridyl 1303 3 3-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1304 3 3-OMe-Phenyl 1H-imidazol-4-yl 1305 3 3-OMe-Phenyl 2-furanyl 1306 3 4-CN-Phenyl Ethyl 1307 3 4-CN-Phenyl n-propyl 1308 3 4-CN-Phenyl Isopropyl 1309 3 4-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1310 3 4-CN-Phenyl CF.sub.3 1311 3 4-CN-Phenyl —CH.sub.2CF.sub.3 1312 3 4-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1313 3 4-CN-Phenyl cyclopropyl 1314 3 4-CN-Phenyl Cyclobutyl 1315 3 4-CN-Phenyl cyclopentyl 1316 3 4-CN-Phenyl cyclohexyl 1317 3 4-CN-Phenyl 3-pyridyl 1318 3 4-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1319 3 4-CN-Phenyl 1H-imidazol-4-yl 1320 3 4-CN-Phenyl 2-furanyl 1321 3 2-CN-Phenyl Ethyl 1322 3 2-CN-Phenyl n-propyl 1323 3 2-CN-Phenyl Isopropyl 1324 3 2-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1325 3 2-CN-Phenyl CF.sub.3 1326 3 2-CN-Phenyl —CH.sub.2CF.sub.3 1327 3 2-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1328 3 2-CN-Phenyl cyclopropyl 1329 3 2-CN-Phenyl Cyclobutyl 1330 3 2-CN-Phenyl cyclopentyl 1331 3 2-CN-Phenyl cyclohexyl 1332 3 2-CN-Phenyl 3-pyridyl 1333 3 2-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1334 3 2-CN-Phenyl 1H-imidazol-4-yl 1335 3 2-CN-Phenyl 2-furanyl 1336 3 3-F-Phenyl Ethyl 1337 3 3-F-Phenyl n-propyl 1338 3 3-F-Phenyl Isopropyl 1339 3 3-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1340 3 3-F-Phenyl CF.sub.3 1341 3 3-F-Phenyl —CH.sub.2CF.sub.3 1342 3 3-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1343 3 3-F-Phenyl cyclopropyl 1344 3 3-F-Phenyl Cyclobutyl 1345 3 3-F-Phenyl cyclopentyl 1346 3 3-F-Phenyl cyclohexyl 1347 3 3-F-Phenyl 3-pyridyl 1348 3 3-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1349 3 3-F-Phenyl 1H-imidazol-4-yl 1350 3 3-F-Phenyl 2-furanyl 1351 3 2-Cl-Phenyl Ethyl 1352 3 2-Cl-Phenyl n-propyl 1353 3 2-Cl-Phenyl Isopropyl 1354 3 2-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1355 3 2-Cl-Phenyl CF.sub.3 1356 3 2-Cl-Phenyl —CH.sub.2CF.sub.3 1357 3 2-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1358 3 2-Cl-Phenyl cyclopropyl 1359 3 2-Cl-Phenyl Cyclobutyl 1360 3 2-Cl-Phenyl cyclopentyl 1361 3 2-Cl-Phenyl cyclohexyl 1362 3 2-Cl-Phenyl 3-pyridyl 1363 3 2-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1364 3 2-Cl-Phenyl 1H-imidazol-4-yl 1365 3 2-Cl-Phenyl 2-furanyl 1366 3 4-Cl-Phenyl Ethyl 1367 3 4-Cl-Phenyl n-propyl 1368 3 4-Cl-Phenyl Isopropyl 1369 3 4-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1370 3 4-Cl-Phenyl CF.sub.3 1371 3 4-Cl-Phenyl —CH.sub.2CF.sub.3 1372 3 4-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1373 3 4-Cl-Phenyl cyclopropyl 1374 3 4-Cl-Phenyl Cyclobutyl 1375 3 4-Cl-Phenyl cyclopentyl 1376 3 4-Cl-Phenyl cyclohexyl 1377 3 4-Cl-Phenyl 3-pyridyl 1378 3 4-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1379 3 4-Cl-Phenyl 1H-imidazol-4-yl 1380 3 4-Cl-Phenyl 2-furanyl 1381 3 3-Br-Phenyl Ethyl 1382 3 3-Br-Phenyl n-propyl 1383 3 3-Br-Phenyl Isopropyl 1384 3 3-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1385 3 3-Br-Phenyl CF.sub.3 1386 3 3-Br-Phenyl —CH.sub.2CF.sub.3 1387 3 3-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1388 3 3-Br-Phenyl cyclopropyl 1389 3 3-Br-Phenyl Cyclobutyl 1390 3 3-Br-Phenyl cyclopentyl 1391 3 3-Br-Phenyl cyclohexyl 1392 3 3-Br-Phenyl 3-pyridyl 1393 3 3-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1394 3 3-Br-Phenyl 1H-imidazol-4-yl 1395 3 3-Br-Phenyl 2-furanyl 1396 3 2-CF.sub.3-Phenyl Ethyl 1397 3 2-CF.sub.3-Phenyl n-propyl 1398 3 2-CF.sub.3-Phenyl Isopropyl 1399 3 2-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1400 3 2-CF.sub.3-Phenyl CF.sub.3 1401 3 2-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1402 3 2-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1403 3 2-CF.sub.3-Phenyl cyclopropyl 1404 3 2-CF.sub.3-Phenyl Cyclobutyl 1405 3 2-CF.sub.3-Phenyl cyclopentyl 1406 3 2-CF.sub.3-Phenyl cyclohexyl 1407 3 2-CF.sub.3-Phenyl 3-pyridyl 1408 3 2-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1409 3 2-CF.sub.3-Phenyl 1H-imidazol-4-yl 1410 3 2-CF.sub.3-Phenyl 2-furanyl 1411 3 4-CF.sub.3-Phenyl Ethyl 1412 3 4-CF.sub.3-Phenyl n-propyl 1413 3 4-CF.sub.3-Phenyl Isopropyl 1414 3 4-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1415 3 4-CF.sub.3-Phenyl CF.sub.3 1416 3 4-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1417 3 4-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1418 3 4-CF.sub.3-Phenyl cyclopropyl 1419 3 4-CF.sub.3-Phenyl Cyclobutyl 1420 3 4-CF.sub.3-Phenyl cyclopentyl 1421 3 4-CF.sub.3-Phenyl cyclohexyl 1422 3 4-CF.sub.3-Phenyl 3-pyridyl 1423 3 4-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1424 3 4-CF.sub.3-Phenyl 1H-imidazol-4-yl 1425 3 4-CF.sub.3-Phenyl 2-furanyl 1426 3 3-iPr-Phenyl Ethyl 1427 3 3-iPr-Phenyl n-propyl 1428 3 3-iPr-Phenyl Isopropyl 1429 3 3-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1430 3 3-iPr-Phenyl CF.sub.3 1431 3 3-iPr-Phenyl —CH.sub.2CF.sub.3 1432 3 3-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1433 3 3-iPr-Phenyl cyclopropyl 1434 3 3-iPr-Phenyl Cyclobutyl 1435 3 3-iPr-Phenyl cyclopentyl 1436 3 3-iPr-Phenyl cyclohexyl 1437 3 3-iPr-Phenyl 3-pyridyl 1438 3 3-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1439 3 3-iPr-Phenyl 1H-imidazol-4-yl 1440 3 3-iPr-Phenyl 2-furanyl 1441 3 2-morpholino-phenyl Ethyl 1442 3 2-morpholino-phenyl n-propyl 1443 3 2-morpholino-phenyl isopropyl 1444 3 2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1445 3 2-morpholino-phenyl CF.sub.3 1446 3 2-morpholino-phenyl —CH.sub.2CF.sub.3 1447 3 2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1448 3 2-morpholino-phenyl cyclopropyl 1449 3 2-morpholino-phenyl Cyclobutyl 1450 3 2-morpholino-phenyl cyclopentyl 1451 3 2-morpholino-phenyl cyclohexyl 1452 3 2-morpholino-phenyl 3-pyridyl 1453 3 2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1454 3 2-morpholino-phenyl 1H-imidazol-4-yl 1455 3 2-morpholino-phenyl 2-furanyl 1456 3 4-morpholino-phenyl ethyl 1457 3 4-morpholino-phenyl n-propyl 1458 3 4-morpholino-phenyl isopropyl 1459 3 4-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1460 3 4-morpholino-phenyl CF.sub.3 1461 3 4-morpholino-phenyl —CH.sub.2CF.sub.3 1462 3 4-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1463 3 4-morpholino-phenyl cyclopropyl 1464 3 4-morpholino-phenyl Cyclobutyl 1465 3 4-morpholino-phenyl cyclopentyl 1466 3 4-morpholino-phenyl cyclohexyl 1467 3 4-morpholino-phenyl 3-pyridyl 1468 3 4-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1469 3 4-morpholino-phenyl 1H-imidazol-4-yl 1470 3 4-morpholino-phenyl 2-furanyl 1471 3 4-methyl-2-morpholino-phenyl ethyl 1472 3 4-methyl-2-morpholino-phenyl n-propyl 1473 3 4-methyl-2-morpholino-phenyl isopropyl 1474 3 4-methyl-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1475 3 4-methyl-2-morpholino-phenyl CF.sub.3 1476 3 4-methyl-2-morpholino-phenyl —CH.sub.2CF.sub.3 1477 3 4-methyl-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1478 3 4-methyl-2-morpholino-phenyl cyclopropyl 1479 3 4-methyl-2-morpholino-phenyl Cyclobutyl 1480 3 4-methyl-2-morpholino-phenyl cyclopentyl 1481 3 4-methyl-2-morpholino-phenyl cyclohexyl 1482 3 4-methyl-2-morpholino-phenyl 3-pyridyl 1483 3 4-methyl-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1484 3 4-methyl-2-morpholino-phenyl 1H-imidazol-4-yl 1485 3 4-methyl-2-morpholino-phenyl 2-furanyl 1486 4 4-CH.sub.3-phenyl ethyl 1487 4 4-CH.sub.3-phenyl n-propyl 1488 4 4-CH.sub.3-phenyl isopropyl 1489 4 4-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1490 4 4-CH.sub.3-phenyl CF.sub.3 1491 4 4-CH.sub.3-phenyl —CH.sub.2CF.sub.3 1492 4 4-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 1493 4 4-CH.sub.3-phenyl cyclopropyl 1494 4 4-CH.sub.3-phenyl Cyclobutyl 1495 4 4-CH.sub.3-phenyl cyclopentyl 1496 4 4-CH.sub.3-phenyl cyclohexyl 1497 4 4-CH.sub.3-phenyl 3-pyridyl 1498 4 4-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1499 4 4-CH.sub.3-phenyl 1H-imidazol-4-yl 1500 4 4-CH.sub.3-phenyl 2-furanyl 1501 4 3-CH.sub.3-phenyl ethyl 1502 4 3-CH.sub.3-phenyl n-propyl 1503 4 3-CH.sub.3-phenyl isopropyl 1504 4 3-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1505 4 3-CH.sub.3-phenyl CF.sub.3 1506 4 3-CH.sub.3-phenyl —CH.sub.2CF.sub.3 1507 4 3-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 1508 4 3-CH.sub.3-phenyl cyclopropyl 1509 4 3-CH.sub.3-phenyl Cyclobutyl 1510 4 3-CH.sub.3-phenyl cyclopentyl 1511 4 3-CH.sub.3-phenyl cyclohexyl 1512 4 3-CH.sub.3-phenyl 3-pyridyl 1513 4 3-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1514 4 3-CH.sub.3-phenyl 1H-imidazol-4-yl 1515 4 3-CH.sub.3-phenyl 2-furanyl 1516 4 3-OH-Phenyl ethyl 1517 4 3-OH-Phenyl n-propyl 1518 4 3-OH-Phenyl isopropyl 1519 4 3-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1520 4 3-OH-Phenyl CF.sub.3 1521 4 3-OH-Phenyl —CH.sub.2CF.sub.3 1522 4 3-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1523 4 3-OH-Phenyl cyclopropyl 1524 4 3-OH-Phenyl Cyclobutyl 1525 4 3-OH-Phenyl cyclopentyl 1526 4 3-OH-Phenyl cyclohexyl 1527 4 3-OH-Phenyl 3-pyridyl 1528 4 3-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1529 4 3-OH-Phenyl 1H-imidazol-4-yl 1530 4 3-OH-Phenyl 2-furanyl 1531 4 4-OMe-Phenyl ethyl 1532 4 4-OMe-Phenyl n-propyl 1533 4 4-OMe-Phenyl isopropyl 1534 4 4-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1535 4 4-OMe-Phenyl CF.sub.3 1536 4 4-OMe-Phenyl —CH.sub.2CF.sub.3 1537 4 4-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1538 4 4-OMe-Phenyl cyclopropyl 1539 4 4-OMe-Phenyl Cyclobutyl 1540 4 4-OMe-Phenyl cyclopentyl 1541 4 4-OMe-Phenyl cyclohexyl 1542 4 4-OMe-Phenyl 3-pyridyl 1543 4 4-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1544 4 4-OMe-Phenyl 1H-imidazol-4-yl 1545 4 4-OMe-Phenyl 2-furanyl 1546 4 2-OMe-Phenyl ethyl 1547 4 2-OMe-Phenyl n-propyl 1548 4 2-OMe-Phenyl isopropyl 1549 4 2-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1550 4 2-OMe-Phenyl CF.sub.3 1551 4 2-OMe-Phenyl —CH.sub.2CF.sub.3 1552 4 2-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1553 4 2-OMe-Phenyl cyclopropyl 1554 4 2-OMe-Phenyl Cyclobutyl 1555 4 2-OMe-Phenyl cyclopentyl 1556 4 2-OMe-Phenyl cyclohexyl 1557 4 2-OMe-Phenyl 3-pyridyl 1558 4 2-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1559 4 2-OMe-Phenyl 1H-imidazol-4-yl 1560 4 2-OMe-Phenyl 2-furanyl 1561 4 3-CN-Phenyl ethyl 1562 4 3-CN-Phenyl n-propyl 1563 4 3-CN-Phenyl isopropyl 1564 4 3-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1565 4 3-CN-Phenyl CF.sub.3 1566 4 3-CN-Phenyl —CH.sub.2CF.sub.3 1567 4 3-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1568 4 3-CN-Phenyl cyclopropyl 1569 4 3-CN-Phenyl Cyclobutyl 1570 4 3-CN-Phenyl cyclopentyl 1571 4 3-CN-Phenyl cyclohexyl 1572 4 3-CN-Phenyl 3-pyridyl 1573 4 3-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1574 4 3-CN-Phenyl 1H-imidazol-4-yl 1575 4 3-CN-Phenyl 2-furanyl 1576 4 2-F-Phenyl ethyl 1577 4 2-F-Phenyl n-propyl 1578 4 2-F-Phenyl isopropyl 1579 4 2-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1580 4 2-F-Phenyl CF.sub.3 1581 4 2-F-Phenyl —CH.sub.2CF.sub.3 1582 4 2-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1583 4 2-F-Phenyl cyclopropyl 1584 4 2-F-Phenyl Cyclobutyl 1585 4 2-F-Phenyl cyclopentyl 1586 4 2-F-Phenyl cyclohexyl 1587 4 2-F-Phenyl 3-pyridyl 1588 4 2-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1589 4 2-F-Phenyl 1H-imidazol-4-yl 1590 4 2-F-Phenyl 2-furanyl 1591 4 4-F-Phenyl ethyl 1592 4 4-F-Phenyl n-propyl 1593 4 4-F-Phenyl isopropyl 1594 4 4-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1595 4 4-F-Phenyl CF.sub.3 1596 4 4-F-Phenyl —CH.sub.2CF.sub.3 1597 4 4-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1598 4 4-F-Phenyl cyclopropyl 1599 4 4-F-Phenyl Cyclobutyl 1600 4 4-F-Phenyl cyclopentyl 1601 4 4-F-Phenyl cyclohexyl 1602 4 4-F-Phenyl 3-pyridyl 1603 4 4-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1604 4 4-F-Phenyl 1H-imidazol-4-yl 1605 4 4-F-Phenyl 2-furanyl 1606 4 3-Cl-Phenyl ethyl 1607 4 3-Cl-Phenyl n-propyl 1608 4 3-Cl-Phenyl isopropyl 1609 4 3-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1610 4 3-Cl-Phenyl CF.sub.3 1611 4 3-Cl-Phenyl —CH.sub.2CF.sub.3 1612 4 3-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1613 4 3-Cl-Phenyl cyclopropyl 1614 4 3-Cl-Phenyl Cyclobutyl 1615 4 3-Cl-Phenyl cyclopentyl 1616 4 3-Cl-Phenyl cyclohexyl 1617 4 3-Cl-Phenyl 3-pyridyl 1618 4 3-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1619 4 3-Cl-Phenyl 1H-imidazol-4-yl 1620 4 3-Cl-Phenyl 2-furanyl 1621 4 2-Br-Phenyl ethyl 1622 4 2-Br-Phenyl n-propyl 1623 4 2-Br-Phenyl isopropyl 1624 4 2-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1625 4 2-Br-Phenyl CF.sub.3 1626 4 2-Br-Phenyl —CH.sub.2CF.sub.3 1627 4 2-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1628 4 2-Br-Phenyl cyclopropyl 1629 4 2-Br-Phenyl Cyclobutyl 1630 4 2-Br-Phenyl cyclopentyl 1631 4 2-Br-Phenyl cyclohexyl 1632 4 2-Br-Phenyl 3-pyridyl 1633 4 2-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1634 4 2-Br-Phenyl 1H-imidazol-4-yl 1635 4 2-Br-Phenyl 2-furanyl 1636 4 4-Br-Phenyl ethyl 1637 4 4-Br-Phenyl n-propyl 1638 4 4-Br-Phenyl isopropyl 1639 4 4-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1640 4 4-Br-Phenyl CF.sub.3 1641 4 4-Br-Phenyl —CH.sub.2CF.sub.3 1642 4 4-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1643 4 4-Br-Phenyl cyclopropyl 1644 4 4-Br-Phenyl Cyclobutyl 1645 4 4-Br-Phenyl cyclopentyl 1646 4 4-Br-Phenyl cyclohexyl 1647 4 4-Br-Phenyl 3-pyridyl 1648 4 4-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1649 4 4-Br-Phenyl 1H-imidazol-4-yl 1650 4 4-Br-Phenyl 2-furanyl 1651 4 3-CF.sub.3-Phenyl ethyl 1652 4 3-CF.sub.3-Phenyl n-propyl 1653 4 3-CF.sub.3-Phenyl isopropyl 1654 4 3-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1655 4 3-CF.sub.3-Phenyl CF.sub.3 1656 4 3-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1657 4 3-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1658 4 3-CF.sub.3-Phenyl cyclopropyl 1659 4 3-CF.sub.3-Phenyl Cyclobutyl 1660 4 3-CF.sub.3-Phenyl cyclopentyl 1661 4 3-CF.sub.3-Phenyl cyclohexyl 1662 4 3-CF.sub.3-Phenyl 3-pyridyl 1663 4 3-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1664 4 3-CF.sub.3-Phenyl 1H-imidazol-4-yl 1665 4 3-CF.sub.3-Phenyl 2-furanyl 1666 4 2-iPr-Phenyl ethyl 1667 4 2-iPr-Phenyl n-propyl 1668 4 2-iPr-Phenyl isopropyl 1669 4 2-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1670 4 2-iPr-Phenyl CF.sub.3 1671 4 2-iPr-Phenyl —CH.sub.2CF.sub.3 1672 4 2-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1673 4 2-iPr-Phenyl cyclopropyl 1674 4 2-iPr-Phenyl Cyclobutyl 1675 4 2-iPr-Phenyl cyclopentyl 1676 4 2-iPr-Phenyl cyclohexyl 1677 4 2-iPr-Phenyl 3-pyridyl 1678 4 2-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1679 4 2-iPr-Phenyl 1H-imidazol-4-yl 1680 4 2-iPr-Phenyl 2-furanyl 1681 4 4-iPr-Phenyl ethyl 1682 4 4-iPr-Phenyl n-propyl 1683 4 4-iPr-Phenyl isopropyl 1684 4 4-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1685 4 4-iPr-Phenyl CF.sub.3 1686 4 4-iPr-Phenyl —CH.sub.2CF.sub.3 1687 4 4-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1688 4 4-iPr-Phenyl cyclopropyl 1689 4 4-iPr-Phenyl Cyclobutyl 1690 4 4-iPr-Phenyl cyclopentyl 1691 4 4-iPr-Phenyl cyclohexyl 1692 4 4-iPr-Phenyl 3-pyridyl 1693 4 4-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1694 4 4-iPr-Phenyl 1H-imidazol-4-yl 1695 4 4-iPr-Phenyl 2-furanyl 1696 4 3-morpholino-phenyl ethyl 1697 4 3-morpholino-phenyl n-propyl 1698 4 3-morpholino-phenyl isopropyl 1699 4 3-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1700 4 3-morpholino-phenyl CF.sub.3 1701 4 3-morpholino-phenyl —CH.sub.2CF.sub.3 1702 4 3-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1703 4 3-morpholino-phenyl cyclopropyl 1704 4 3-morpholino-phenyl Cyclobutyl 1705 4 3-morpholino-phenyl cyclopentyl 1706 4 3-morpholino-phenyl cyclohexyl 1707 4 3-morpholino-phenyl 3-pyridyl 1708 4 3-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1709 4 3-morpholino-phenyl 1H-imidazol-4-yl 1710 4 3-morpholino-phenyl 2-furanyl 1711 4 4-cyano-2-morpholino-phenyl ethyl 1712 4 4-cyano-2-morpholino-phenyl n-propyl 1713 4 4-cyano-2-morpholino-phenyl isopropyl 1714 4 4-cyano-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1715 4 4-cyano-2-morpholino-phenyl CF.sub.3 1716 4 4-cyano-2-morpholino-phenyl —CH.sub.2CF.sub.3 1717 4 4-cyano-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1718 4 4-cyano-2-morpholino-phenyl cyclopropyl 1719 4 4-cyano-2-morpholino-phenyl Cyclobutyl 1720 4 4-cyano-2-morpholino-phenyl cyclopentyl 1721 4 4-cyano-2-morpholino-phenyl cyclohexyl 1722 4 4-cyano-2-morpholino-phenyl 3-pyridyl 1723 4 4-cyano-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1724 4 4-cyano-2-morpholino-phenyl 1H-imidazol-4-yl 1725 4 4-cyano-2-morpholino-phenyl 2-furanyl 1726 4 4-hydroxy-2-morpholino-phenyl ethyl 1727 4 4-hydroxy-2-morpholino-phenyl n-propyl 1728 4 4-hydroxy-2-morpholino-phenyl isopropyl 1729 4 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1730 4 4-hydroxy-2-morpholino-phenyl CF.sub.3 1731 4 4-hydroxy-2-morpholino-phenyl —CH.sub.2CF.sub.3 1732 4 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1733 4 4-hydroxy-2-morpholino-phenyl cyclopropyl 1734 4 4-hydroxy-2-morpholino-phenyl Cyclobutyl 1735 4 4-hydroxy-2-morpholino-phenyl cyclopentyl 1736 4 4-hydroxy-2-morpholino-phenyl cyclohexyl 1737 4 4-hydroxy-2-morpholino-phenyl 3-pyridyl 1738 4 4-hydroxy-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1739 4 4-hydroxy-2-morpholino-phenyl 1H-imidazol-4-yl 1740 4 4-hydroxy-2-morpholino-phenyl 2-furanyl 1741 4 2-CH.sub.3-phenyl Ethyl 1742 4 2-CH.sub.3-phenyl n-propyl 1743 4 2-CH.sub.3-phenyl Isopropyl 1744 4 2-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1745 4 2-CH.sub.3-phenyl CF.sub.3 1746 4 2-CH.sub.3-phenyl —CH.sub.2CF.sub.3 1747 4 2-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 1748 4 2-CH.sub.3-phenyl cyclopropyl 1749 4 2-CH.sub.3-phenyl Cyclobutyl 1750 4 2-CH.sub.3-phenyl cyclopentyl 1751 4 2-CH.sub.3-phenyl cyclohexyl 1752 4 2-CH.sub.3-phenyl 3-pyridyl 1753 4 2-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1754 4 2-CH.sub.3-phenyl 1H-imidazol-4-yl 1755 4 2-CH.sub.3-phenyl 2-furanyl 1756 4 4-OH-Phenyl Ethyl 1757 4 4-OH-Phenyl n-propyl 1758 4 4-OH-Phenyl Isopropyl 1759 4 4-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1760 4 4-OH-Phenyl CF.sub.3 1761 4 4-OH-Phenyl —CH.sub.2CF.sub.3 1762 4 4-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1763 4 4-OH-Phenyl cyclopropyl 1764 4 4-OH-Phenyl Cyclobutyl 1765 4 4-OH-Phenyl cyclopentyl 1766 4 4-OH-Phenyl cyclohexyl 1767 4 4-OH-Phenyl 3-pyridyl 1768 4 4-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1769 4 4-OH-Phenyl 1H-imidazol-4-yl 1770 4 4-OH-Phenyl 2-furanyl 1771 4 2-OH-Phenyl Ethyl 1772 4 2-OH-Phenyl n-propyl 1773 4 2-OH-Phenyl Isopropyl 1774 4 2-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1775 4 2-OH-Phenyl CF.sub.3 1776 4 2-OH-Phenyl —CH.sub.2CF.sub.3 1777 4 2-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1778 4 2-OH-Phenyl cyclopropyl 1779 4 2-OH-Phenyl Cyclobutyl 1780 4 2-OH-Phenyl cyclopentyl 1781 4 2-OH-Phenyl cyclohexyl 1782 4 2-OH-Phenyl 3-pyridyl 1783 4 2-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1784 4 2-OH-Phenyl 1H-imidazol-4-yl 1785 4 2-OH-Phenyl 2-furanyl 1786 4 3-OMe-Phenyl Ethyl 1787 4 3-OMe-Phenyl n-propyl 1788 4 3-OMe-Phenyl Isopropyl 1789 4 3-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1790 4 3-OMe-Phenyl CF.sub.3 1791 4 3-OMe-Phenyl —CH.sub.2CF.sub.3 1792 4 3-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1793 4 3-OMe-Phenyl cyclopropyl 1794 4 3-OMe-Phenyl Cyclobutyl 1795 4 3-OMe-Phenyl cyclopentyl 1796 4 3-OMe-Phenyl cyclohexyl 1797 4 3-OMe-Phenyl 3-pyridyl 1798 4 3-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1799 4 3-OMe-Phenyl 1H-imidazol-4-yl 1800 4 3-OMe-Phenyl 2-furanyl 1801 4 4-CN-Phenyl Ethyl 1802 4 4-CN-Phenyl n-propyl 1803 4 4-CN-Phenyl Isopropyl 1804 4 4-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1805 4 4-CN-Phenyl CF.sub.3 1806 4 4-CN-Phenyl —CH.sub.2CF.sub.3 1807 4 4-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1808 4 4-CN-Phenyl cyclopropyl 1809 4 4-CN-Phenyl Cyclobutyl 1810 4 4-CN-Phenyl cyclopentyl 1811 4 4-CN-Phenyl cyclohexyl 1812 4 4-CN-Phenyl 3-pyridyl 1813 4 4-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1814 4 4-CN-Phenyl 1H-imidazol-4-yl 1815 4 4-CN-Phenyl 2-furanyl 1816 4 2-CN-Phenyl Ethyl 1817 4 2-CN-Phenyl n-propyl 1818 4 2-CN-Phenyl Isopropyl 1819 4 2-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1820 4 2-CN-Phenyl CF.sub.3 1821 4 2-CN-Phenyl —CH.sub.2CF.sub.3 1822 4 2-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1823 4 2-CN-Phenyl cyclopropyl 1824 4 2-CN-Phenyl Cyclobutyl 1825 4 2-CN-Phenyl cyclopentyl 1826 4 2-CN-Phenyl cyclohexyl 1827 4 2-CN-Phenyl 3-pyridyl 1828 4 2-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1829 4 2-CN-Phenyl 1H-imidazol-4-yl 1830 4 2-CN-Phenyl 2-furanyl 1831 4 3-F-Phenyl Ethyl 1832 4 3-F-Phenyl n-propyl 1833 4 3-F-Phenyl Isopropyl 1834 4 3-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1835 4 3-F-Phenyl CF.sub.3 1836 4 3-F-Phenyl —CH.sub.2CF.sub.3 1837 4 3-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1838 4 3-F-Phenyl cyclopropyl 1839 4 3-F-Phenyl Cyclobutyl 1840 4 3-F-Phenyl cyclopentyl 1841 4 3-F-Phenyl cyclohexyl 1842 4 3-F-Phenyl 3-pyridyl 1843 4 3-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1844 4 3-F-Phenyl 1H-imidazol-4-yl 1845 4 3-F-Phenyl 2-furanyl 1846 4 2-Cl-Phenyl Ethyl 1847 4 2-Cl-Phenyl n-propyl 1848 4 2-Cl-Phenyl Isopropyl 1849 4 2-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1850 4 2-Cl-Phenyl CF.sub.3 1851 4 2-Cl-Phenyl —CH.sub.2CF.sub.3 1852 4 2-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1853 4 2-Cl-Phenyl cyclopropyl 1854 4 2-Cl-Phenyl Cyclobutyl 1855 4 2-Cl-Phenyl cyclopentyl 1856 4 2-Cl-Phenyl cyclohexyl 1857 4 2-Cl-Phenyl 3-pyridyl 1858 4 2-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1859 4 2-Cl-Phenyl 1H-imidazol-4-yl 1860 4 2-Cl-Phenyl 2-furanyl 1861 4 4-Cl-Phenyl Ethyl 1862 4 4-Cl-Phenyl n-propyl 1863 4 4-Cl-Phenyl Isopropyl 1864 4 4-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1865 4 4-Cl-Phenyl CF.sub.3 1866 4 4-Cl-Phenyl —CH.sub.2CF.sub.3 1867 4 4-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1868 4 4-Cl-Phenyl cyclopropyl 1869 4 4-Cl-Phenyl Cyclobutyl 1870 4 4-Cl-Phenyl cyclopentyl 1871 4 4-Cl-Phenyl cyclohexyl 1872 4 4-Cl-Phenyl 3-pyridyl 1873 4 4-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1874 4 4-Cl-Phenyl 1H-imidazol-4-yl 1875 4 4-Cl-Phenyl 2-furanyl 1876 4 3-Br-Phenyl Ethyl 1877 4 3-Br-Phenyl n-propyl 1878 4 3-Br-Phenyl Isopropyl 1879 4 3-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1880 4 3-Br-Phenyl CF.sub.3 1881 4 3-Br-Phenyl —CH.sub.2CF.sub.3 1882 4 3-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1883 4 3-Br-Phenyl cyclopropyl 1884 4 3-Br-Phenyl Cyclobutyl 1885 4 3-Br-Phenyl cyclopentyl 1886 4 3-Br-Phenyl cyclohexyl 1887 4 3-Br-Phenyl 3-pyridyl 1888 4 3-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1889 4 3-Br-Phenyl 1H-imidazol-4-yl 1890 4 3-Br-Phenyl 2-furanyl 1891 4 2-CF.sub.3-Phenyl Ethyl 1892 4 2-CF.sub.3-Phenyl n-propyl 1893 4 2-CF.sub.3-Phenyl Isopropyl 1894 4 2-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1895 4 2-CF.sub.3-Phenyl CF.sub.3 1896 4 2-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1897 4 2-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1898 4 2-CF.sub.3-Phenyl cyclopropyl 1899 4 2-CF.sub.3-Phenyl Cyclobutyl 1900 4 2-CF.sub.3-Phenyl cyclopentyl 1901 4 2-CF.sub.3-Phenyl cyclohexyl 1902 4 2-CF.sub.3-Phenyl 3-pyridyl 1903 4 2-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1904 4 2-CF.sub.3-Phenyl 1H-imidazol-4-yl 1905 4 2-CF.sub.3-Phenyl 2-furanyl 1906 4 4-CF.sub.3-Phenyl Ethyl 1907 4 4-CF.sub.3-Phenyl n-propyl 1908 4 4-CF.sub.3-Phenyl Isopropyl 1909 4 4-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1910 4 4-CF.sub.3-Phenyl CF.sub.3 1911 4 4-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1912 4 4-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1913 4 4-CF.sub.3-Phenyl cyclopropyl 1914 4 4-CF.sub.3-Phenyl Cyclobutyl 1915 4 4-CF.sub.3-Phenyl cyclopentyl 1916 4 4-CF.sub.3-Phenyl cyclohexyl 1917 4 4-CF.sub.3-Phenyl 3-pyridyl 1918 4 4-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1919 4 4-CF.sub.3-Phenyl 1H-imidazol-4-yl 1920 4 4-CF.sub.3-Phenyl 2-furanyl 1921 4 3-iPr-Phenyl Ethyl 1922 4 3-iPr-Phenyl n-propyl 1923 4 3-iPr-Phenyl Isopropyl 1924 4 3-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1925 4 3-iPr-Phenyl CF.sub.3 1926 4 3-iPr-Phenyl —CH.sub.2CF.sub.3 1927 4 3-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1928 4 3-iPr-Phenyl cyclopropyl 1929 4 3-iPr-Phenyl Cyclobutyl 1930 4 3-iPr-Phenyl cyclopentyl 1931 4 3-iPr-Phenyl cyclohexyl 1932 4 3-iPr-Phenyl 3-pyridyl 1933 4 3-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1934 4 3-iPr-Phenyl 1H-imidazol-4-yl 1935 4 3-iPr-Phenyl 2-furanyl 1936 4 2-morpholino-phenyl Ethyl 1937 4 2-morpholino-phenyl n-propyl 1938 4 2-morpholino-phenyl isopropyl 1939 4 2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1940 4 2-morpholino-phenyl CF.sub.3 1941 4 2-morpholino-phenyl —CH.sub.2CF.sub.3 1942 4 2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1943 4 2-morpholino-phenyl cyclopropyl 1944 4 2-morpholino-phenyl Cyclobutyl 1945 4 2-morpholino-phenyl cyclopentyl 1946 4 2-morpholino-phenyl cyclohexyl 1947 4 2-morpholino-phenyl 3-pyridyl 1948 4 2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1949 4 2-morpholino-phenyl 1H-imidazol-4-yl 1950 4 2-morpholino-phenyl 2-furanyl 1951 4 4-morpholino-phenyl ethyl 1952 4 4-morpholino-phenyl n-propyl 1953 4 4-morpholino-phenyl isopropyl 1954 4 4-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1955 4 4-morpholino-phenyl CF.sub.3 1956 4 4-morpholino-phenyl —CH.sub.2CF.sub.3 1957 4 4-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1958 4 4-morpholino-phenyl cyclopropyl 1959 4 4-morpholino-phenyl Cyclobutyl 1960 4 4-morpholino-phenyl cyclopentyl 1961 4 4-morpholino-phenyl cyclohexyl 1962 4 4-morpholino-phenyl 3-pyridyl 1963 4 4-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1964 4 4-morpholino-phenyl 1H-imidazol-4-yl 1965 4 4-morpholino-phenyl 2-furanyl 1966 4 4-methyl-2-morpholino-phenyl ethyl 1967 4 4-methyl-2-morpholino-phenyl n-propyl 1968 4 4-methyl-2-morpholino-phenyl isopropyl 1969 4 4-methyl-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1970 4 4-methyl-2-morpholino-phenyl CF.sub.3 1971 4 4-methyl-2-morpholino-phenyl —CH.sub.2CF.sub.3 1972 4 4-methyl-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1973 4 4-methyl-2-morpholino-phenyl cyclopropyl 1974 4 4-methyl-2-morpholino-phenyl Cyclobutyl 1975 4 4-methyl-2-morpholino-phenyl cyclopentyl 1976 4 4-methyl-2-morpholino-phenyl cyclohexyl 1977 4 4-methyl-2-morpholino-phenyl 3-pyridyl 1978 4 4-methyl-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1979 4 4-methyl-2-morpholino-phenyl 1H-imidazol-4-yl 1980 4 4-methyl-2-morpholino-phenyl 2-furanyl 1981 1 naphthylen-1-yl Ethyl 1982 1 naphthylen-1-yl n-propyl 1983 1 naphthylen-1-yl Isopropyl 1984 1 naphthylen-1-yl —CH.sub.2CH(CH.sub.3).sub.2 1985 1 naphthylen-1-yl CF.sub.3 1986 1 naphthylen-1-yl —CH.sub.2CF.sub.3 1987 1 naphthylen-1-yl —CH.sub.2CH.sub.2CF.sub.3 1988 1 naphthylen-1-yl Cyclopropyl 1989 1 naphthylen-1-yl Cyclobutyl 1990 1 naphthylen-1-yl Cyclopentyl 1991 1 naphthylen-1-yl Cyclohexyl 1992 1 naphthylen-1-yl 3-pyridyl 1993 1 naphthylen-1-yl 1-methyl-1H-pyrazol-4-yl 1994 1 naphthylen-1-yl 1H-imidazol-4-yl 1995 1 naphthylen-1-yl 2-furanyl 1996 1 naphthylen-2-yl Ethyl 1997 1 naphthylen-2-yl n-propyl 1998 1 naphthylen-2-yl Isopropyl 1999 1 naphthylen-2-yl —CH.sub.2CH(CH.sub.3).sub.2 2000 1 naphthylen-2-yl CF.sub.3 2001 1 naphthylen-2-yl —CH.sub.2CF.sub.3 2002 1 naphthylen-2-yl —CH.sub.2CH.sub.2CF.sub.3 2003 1 naphthylen-2-yl Cyclopropyl 2004 1 naphthylen-2-yl Cyclobutyl 2005 1 naphthylen-2-yl Cyclopentyl 2006 1 naphthylen-2-yl Cyclohexyl 2007 1 naphthylen-2-yl 3-pyridyl 2008 1 naphthylen-2-yl 1-methyl-1H-pyrazol-4-yl 2009 1 naphthylen-2-yl 1H-imidazol-4-yl 2010 1 naphthylen-2-yl 2-furanyl 2011 2 naphthylen-1-yl Ethyl 2012 2 naphthylen-1-yl n-propyl 2013 2 naphthylen-1-yl Isopropyl 2014 2 naphthylen-1-yl —CH.sub.2CH(CH.sub.3).sub.2 2015 2 naphthylen-1-yl CF.sub.3 2016 2 naphthylen-1-yl —CH.sub.2CF.sub.3 2017 2 naphthylen-1-yl —CH.sub.2CH.sub.2CF.sub.3 2018 2 naphthylen-1-yl Cyclopropyl 2019 2 naphthylen-1-yl Cyclobutyl 2020 2 naphthylen-1-yl Cyclopentyl 2021 2 naphthylen-1-yl Cyclohexyl 2022 2 naphthylen-1-yl 3-pyridyl 2023 2 naphthylen-1-yl 1-methyl-1H-pyrazol-4-yl 2024 2 naphthylen-1-yl 1H-imidazol-4-yl 2025 2 naphthylen-1-yl 2-furanyl 2026 2 naphthylen-2-yl Ethyl 2027 2 naphthylen-2-yl n-propyl 2028 2 naphthylen-2-yl Isopropyl 2029 2 naphthylen-2-yl —CH.sub.2CH(CH.sub.3).sub.2 2030 2 naphthylen-2-yl CF.sub.3 2031 2 naphthylen-2-yl —CH.sub.2CF.sub.3 2032 2 naphthylen-2-yl —CH.sub.2CH.sub.2CF.sub.3 2033 2 naphthylen-2-yl Cyclopropyl 2034 2 naphthylen-2-yl Cyclobutyl 2035 2 naphthylen-2-yl Cyclopentyl 2036 2 naphthylen-2-yl Cyclohexyl 2037 2 naphthylen-2-yl 3-pyridyl 2038 2 naphthylen-2-yl 1-methyl-1H-pyrazol-4-yl 2039 2 naphthylen-2-yl 1H-imidazol-4-yl 2040 2 naphthylen-2-yl 2-furanyl 2041 3 naphthylen-1-yl Ethyl 2042 3 naphthylen-1-yl n-propyl 2043 3 naphthylen-1-yl Isopropyl 2044 3 naphthylen-1-yl —CH.sub.2CH(CH.sub.3).sub.2 2045 3 naphthylen-1-yl CF.sub.3 2046 3 naphthylen-1-yl —CH.sub.2CF.sub.3 2047 3 naphthylen-1-yl —CH.sub.2CH.sub.2CF.sub.3 2048 3 naphthylen-1-yl Cyclopropyl 2049 3 naphthylen-1-yl Cyclobutyl 2050 3 naphthylen-1-yl Cyclopentyl 2051 3 naphthylen-1-yl Cyclohexyl 2052 3 naphthylen-1-yl 3-pyridyl 2053 3 naphthylen-1-yl 1-methyl-1H-pyrazol-4-yl 2054 3 naphthylen-1-yl 1H-imidazol-4-yl 2055 3 naphthylen-1-yl 2-furanyl 2056 3 naphthylen-2-yl Ethyl 2057 3 naphthylen-2-yl n-propyl 2058 3 naphthylen-2-yl Isopropyl 2059 3 naphthylen-2-yl —CH.sub.2CH(CH.sub.3).sub.2 2060 3 naphthylen-2-yl CF.sub.3 2061 3 naphthylen-2-yl —CH.sub.2CF.sub.3 2062 3 naphthylen-2-yl —CH.sub.2CH.sub.2CF.sub.3 2063 3 naphthylen-2-yl Cyclopropyl 2064 3 naphthylen-2-yl Cyclobutyl 2065 3 naphthylen-2-yl Cyclopentyl 2066 3 naphthylen-2-yl Cyclohexyl 2067 3 naphthylen-2-yl 3-pyridyl 2068 3 naphthylen-2-yl 1-methyl-1H-pyrazol-4-yl 2069 3 naphthylen-2-yl 1H-imidazol-4-yl 2070 3 naphthylen-2-yl 2-furanyl 2071 4 naphthylen-1-yl Ethyl 2072 4 naphthylen-1-yl n-propyl 2073 4 naphthylen-1-yl Isopropyl 2074 4 naphthylen-1-yl —CH.sub.2CH(CH.sub.3).sub.2 2075 4 naphthylen-1-yl CF.sub.3 2076 4 naphthylen-1-yl —CH.sub.2CF.sub.3 2077 4 naphthylen-1-yl —CH.sub.2CH.sub.2CF.sub.3 2078 4 naphthylen-1-yl Cyclopropyl 2079 4 naphthylen-1-yl Cyclobutyl 2080 4 naphthylen-1-yl Cyclopentyl 2081 4 naphthylen-1-yl Cyclohexyl 2082 4 naphthylen-1-yl 3-pyridyl 2083 4 naphthylen-1-yl 1-methyl-1H-pyrazol-4-yl 2084 4 naphthylen-1-yl 1H-imidazol-4-yl 2085 4 naphthylen-1-yl 2-furanyl 2086 4 naphthylen-2-yl Ethyl 2087 4 naphthylen-2-yl n-propyl 2088 4 naphthylen-2-yl Isopropyl 2089 4 naphthylen-2-yl —CH.sub.2CH(CH.sub.3).sub.2 2090 4 naphthylen-2-yl CF.sub.3 2091 4 naphthylen-2-yl —CH.sub.2CF.sub.3 2092 4 naphthylen-2-yl —CH.sub.2CH.sub.2CF.sub.3 2093 4 naphthylen-2-yl Cyclopropyl 2094 4 naphthylen-2-yl Cyclobutyl 2095 4 naphthylen-2-yl Cyclopentyl 2096 4 naphthylen-2-yl Cyclohexyl 2097 4 naphthylen-2-yl 3-pyridyl 2098 4 naphthylen-2-yl 1-methyl-1H-pyrazol-4-yl 2099 4 naphthylen-2-yl 1H-imidazol-4-yl 2100 4 naphthylen-2-yl 2-furanyl

    [2058] Exemplary embodiments include compounds having the formula (XXXX)

    ##STR00454##

    [2059] or a pharmaceutically acceptable salt form thereof defined herein below in Table 33.

    TABLE-US-00033 TABLE 33 Entry n R.sup.5 R.sup.10C 1 1 4-CH.sub.3-phenyl Ethyl 2 1 4-CH.sub.3-phenyl n-propyl 3 1 4-CH.sub.3-phenyl Isopropyl 4 1 4-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 5 1 4-CH.sub.3-phenyl CF.sub.3 6 1 4-CH.sub.3-phenyl —CH.sub.2CF.sub.3 7 1 4-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 8 1 4-CH.sub.3-phenyl Cyclopropyl 9 1 4-CH.sub.3-phenyl Cyclobutyl 10 1 4-CH.sub.3-phenyl Cyclopentyl 11 1 4-CH.sub.3-phenyl Cyclohexyl 12 1 4-CH.sub.3-phenyl 3-pyridyl 13 1 4-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 14 1 4-CH.sub.3-phenyl 1H-imidazol-4-yl 15 1 4-CH.sub.3-phenyl 2-furanyl 16 1 3-CH.sub.3-phenyl Ethyl 17 1 3-CH.sub.3-phenyl n-propyl 18 1 3-CH.sub.3-phenyl Isopropyl 19 1 3-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 20 1 3-CH.sub.3-phenyl CF.sub.3 21 1 3-CH.sub.3-phenyl —CH.sub.2CF.sub.3 22 1 3-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 23 1 3-CH.sub.3-phenyl Cyclopropyl 24 1 3-CH.sub.3-phenyl Cyclobutyl 25 1 3-CH.sub.3-phenyl Cyclopentyl 26 1 3-CH.sub.3-phenyl cyclohexyl 27 1 3-CH.sub.3-phenyl 3-pyridyl 28 1 3-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 29 1 3-CH.sub.3-phenyl 1H-imidazol-4-yl 30 1 3-CH.sub.3-phenyl 2-furanyl 31 1 3-OH-Phenyl ethyl 32 1 3-OH-Phenyl n-propyl 33 1 3-OH-Phenyl isopropyl 34 1 3-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 35 1 3-OH-Phenyl CF.sub.3 36 1 3-OH-Phenyl —CH.sub.2CF.sub.3 37 1 3-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 38 1 3-OH-Phenyl cyclopropyl 39 1 3-OH-Phenyl Cyclobutyl 40 1 3-OH-Phenyl cyclopentyl 41 1 3-OH-Phenyl cyclohexyl 42 1 3-OH-Phenyl 3-pyridyl 43 1 3-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 44 1 3-OH-Phenyl 1H-imidazol-4-yl 45 1 3-OH-Phenyl 2-furanyl 46 1 4-OMe-Phenyl ethyl 47 1 4-OMe-Phenyl n-propyl 48 1 4-OMe-Phenyl isopropyl 49 1 4-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 50 1 4-OMe-Phenyl CF.sub.3 51 1 4-OMe-Phenyl —CH.sub.2CF.sub.3 52 1 4-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 53 1 4-OMe-Phenyl cyclopropyl 54 1 4-OMe-Phenyl Cyclobutyl 55 1 4-OMe-Phenyl cyclopentyl 56 1 4-OMe-Phenyl cyclohexyl 57 1 4-OMe-Phenyl 3-pyridyl 58 1 4-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 59 1 4-OMe-Phenyl 1H-imidazol-4-yl 60 1 4-OMe-Phenyl 2-furanyl 61 1 2-OMe-Phenyl ethyl 62 1 2-OMe-Phenyl n-propyl 63 1 2-OMe-Phenyl isopropyl 64 1 2-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 65 1 2-OMe-Phenyl CF.sub.3 66 1 2-OMe-Phenyl —CH.sub.2CF.sub.3 67 1 2-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 68 1 2-OMe-Phenyl cyclopropyl 69 1 2-OMe-Phenyl Cyclobutyl 70 1 2-OMe-Phenyl cyclopentyl 71 1 2-OMe-Phenyl cyclohexyl 72 1 2-OMe-Phenyl 3-pyridyl 73 1 2-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 74 1 2-OMe-Phenyl 1H-imidazol-4-yl 75 1 2-OMe-Phenyl 2-furanyl 76 1 3-CN-Phenyl ethyl 77 1 3-CN-Phenyl n-propyl 78 1 3-CN-Phenyl isopropyl 79 1 3-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 80 1 3-CN-Phenyl CF.sub.3 81 1 3-CN-Phenyl —CH.sub.2CF.sub.3 82 1 3-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 83 1 3-CN-Phenyl cyclopropyl 84 1 3-CN-Phenyl Cyclobutyl 85 1 3-CN-Phenyl cyclopentyl 86 1 3-CN-Phenyl cyclohexyl 87 1 3-CN-Phenyl 3-pyridyl 88 1 3-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 89 1 3-CN-Phenyl 1H-imidazol-4-yl 90 1 3-CN-Phenyl 2-furanyl 91 1 2-F-Phenyl ethyl 92 1 2-F-Phenyl n-propyl 93 1 2-F-Phenyl isopropyl 94 1 2-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 95 1 2-F-Phenyl CF.sub.3 96 1 2-F-Phenyl —CH.sub.2CF.sub.3 97 1 2-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 98 1 2-F-Phenyl cyclopropyl 99 1 2-F-Phenyl Cyclobutyl 100 1 2-F-Phenyl cyclopentyl 101 1 2-F-Phenyl cyclohexyl 102 1 2-F-Phenyl 3-pyridyl 103 1 2-F-Phenyl 1-methyl-1H-pyrazol-4-yl 104 1 2-F-Phenyl 1H-imidazol-4-yl 105 1 2-F-Phenyl 2-furanyl 106 1 4-F-Phenyl ethyl 107 1 4-F-Phenyl n-propyl 108 1 4-F-Phenyl isopropyl 109 1 4-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 110 1 4-F-Phenyl CF.sub.3 111 1 4-F-Phenyl —CH.sub.2CF.sub.3 112 1 4-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 113 1 4-F-Phenyl cyclopropyl 114 1 4-F-Phenyl Cyclobutyl 115 1 4-F-Phenyl cyclopentyl 116 1 4-F-Phenyl cyclohexyl 117 1 4-F-Phenyl 3-pyridyl 118 1 4-F-Phenyl 1-methyl-1H-pyrazol-4-yl 119 1 4-F-Phenyl 1H-imidazol-4-yl 120 1 4-F-Phenyl 2-furanyl 121 1 3-Cl-Phenyl ethyl 122 1 3-Cl-Phenyl n-propyl 123 1 3-Cl-Phenyl isopropyl 124 1 3-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 125 1 3-Cl-Phenyl CF.sub.3 126 1 3-Cl-Phenyl —CH.sub.2CF.sub.3 127 1 3-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 128 1 3-Cl-Phenyl cyclopropyl 129 1 3-Cl-Phenyl Cyclobutyl 130 1 3-Cl-Phenyl cyclopentyl 131 1 3-Cl-Phenyl cyclohexyl 132 1 3-Cl-Phenyl 3-pyridyl 133 1 3-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 134 1 3-Cl-Phenyl 1H-imidazol-4-yl 135 1 3-Cl-Phenyl 2-furanyl 136 1 2-Br-Phenyl ethyl 137 1 2-Br-Phenyl n-propyl 138 1 2-Br-Phenyl isopropyl 139 1 2-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 140 1 2-Br-Phenyl CF.sub.3 141 1 2-Br-Phenyl —CH.sub.2CF.sub.3 142 1 2-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 143 1 2-Br-Phenyl cyclopropyl 144 1 2-Br-Phenyl Cyclobutyl 145 1 2-Br-Phenyl cyclopentyl 146 1 2-Br-Phenyl cyclohexyl 147 1 2-Br-Phenyl 3-pyridyl 148 1 2-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 149 1 2-Br-Phenyl 1H-imidazol-4-yl 150 1 2-Br-Phenyl 2-furanyl 151 1 4-Br-Phenyl ethyl 152 1 4-Br-Phenyl n-propyl 153 1 4-Br-Phenyl isopropyl 154 1 4-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 155 1 4-Br-Phenyl CF.sub.3 156 1 4-Br-Phenyl —CH.sub.2CF.sub.3 157 1 4-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 158 1 4-Br-Phenyl cyclopropyl 159 1 4-Br-Phenyl Cyclobutyl 160 1 4-Br-Phenyl cyclopentyl 161 1 4-Br-Phenyl cyclohexyl 162 1 4-Br-Phenyl 3-pyridyl 163 1 4-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 164 1 4-Br-Phenyl 1H-imidazol-4-yl 165 1 4-Br-Phenyl 2-furanyl 166 1 3-CF.sub.3-Phenyl ethyl 167 1 3-CF.sub.3-Phenyl n-propyl 168 1 3-CF.sub.3-Phenyl isopropyl 169 1 3-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 170 1 3-CF.sub.3-Phenyl CF.sub.3 171 1 3-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 172 1 3-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 173 1 3-CF.sub.3-Phenyl cyclopropyl 174 1 3-CF.sub.3-Phenyl Cyclobutyl 175 1 3-CF.sub.3-Phenyl cyclopentyl 176 1 3-CF.sub.3-Phenyl cyclohexyl 177 1 3-CF.sub.3-Phenyl 3-pyridyl 178 1 3-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 179 1 3-CF.sub.3-Phenyl 1H-imidazol-4-yl 180 1 3-CF.sub.3-Phenyl 2-furanyl 181 1 2-iPr-Phenyl ethyl 182 1 2-iPr-Phenyl n-propyl 183 1 2-iPr-Phenyl isopropyl 184 1 2-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 185 1 2-iPr-Phenyl CF.sub.3 186 1 2-iPr-Phenyl —CH.sub.2CF.sub.3 187 1 2-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 188 1 2-iPr-Phenyl cyclopropyl 189 1 2-iPr-Phenyl Cyclobutyl 190 1 2-iPr-Phenyl cyclopentyl 191 1 2-iPr-Phenyl cyclohexyl 192 1 2-iPr-Phenyl 3-pyridyl 193 1 2-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 194 1 2-iPr-Phenyl 1H-imidazol-4-yl 195 1 2-iPr-Phenyl 2-furanyl 196 1 4-iPr-Phenyl ethyl 197 1 4-iPr-Phenyl n-propyl 198 1 4-iPr-Phenyl isopropyl 199 1 4-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 200 1 4-iPr-Phenyl CF.sub.3 201 1 4-iPr-Phenyl —CH.sub.2CF.sub.3 202 1 4-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 203 1 4-iPr-Phenyl cyclopropyl 204 1 4-iPr-Phenyl Cyclobutyl 205 1 4-iPr-Phenyl cyclopentyl 206 1 4-iPr-Phenyl cyclohexyl 207 1 4-iPr-Phenyl 3-pyridyl 208 1 4-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 209 1 4-iPr-Phenyl 1H-imidazol-4-yl 210 1 4-iPr-Phenyl 2-furanyl 211 1 3-morpholino-phenyl ethyl 212 1 3-morpholino-phenyl n-propyl 213 1 3-morpholino-phenyl isopropyl 214 1 3-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 215 1 3-morpholino-phenyl CF.sub.3 216 1 3-morpholino-phenyl —CH.sub.2CF.sub.3 217 1 3-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 218 1 3-morpholino-phenyl cyclopropyl 219 1 3-morpholino-phenyl Cyclobutyl 220 1 3-morpholino-phenyl cyclopentyl 221 1 3-morpholino-phenyl cyclohexyl 222 1 3-morpholino-phenyl 3-pyridyl 223 1 3-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 224 1 3-morpholino-phenyl 1H-imidazol-4-yl 225 1 3-morpholino-phenyl 2-furanyl 226 1 4-cyano-2-morpholino-phenyl ethyl 227 1 4-cyano-2-morpholino-phenyl n-propyl 228 1 4-cyano-2-morpholino-phenyl isopropyl 229 1 4-cyano-2-morpholino-phenyl —CH2CH(CH.sub.3).sub.2 230 1 4-cyano-2-morpholino-phenyl CF.sub.3 231 1 4-cyano-2-morpholino-phenyl —CH.sub.2CF.sub.3 232 1 4-cyano-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 233 1 4-cyano-2-morpholino-phenyl cyclopropyl 234 1 4-cyano-2-morpholino-phenyl Cyclobutyl 235 1 4-cyano-2-morpholino-phenyl cyclopentyl 236 1 4-cyano-2-morpholino-phenyl cyclohexyl 237 1 4-cyano-2-morpholino-phenyl 3-pyridyl 238 1 4-cyano-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 239 1 4-cyano-2-morpholino-phenyl 1H-imidazol-4-yl 240 1 4-cyano-2-morpholino-phenyl 2-furanyl 241 1 4-hydroxy-2-morpholino-phenyl ethyl 242 1 4-hydroxy-2-morpholino-phenyl n-propyl 243 1 4-hydroxy-2-morpholino-phenyl isopropyl 244 1 4-hydroxy-2-morpholino-phenyl —CH2CH(CH.sub.3).sub.2 245 1 4-hydroxy-2-morpholino-phenyl CF.sub.3 246 1 4-hydroxy-2-morpholino-phenyl —CH.sub.2CF.sub.3 247 1 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 248 1 4-hydroxy-2-morpholino-phenyl cyclopropyl 249 1 4-hydroxy-2-morpholino-phenyl Cyclobutyl 250 1 4-hydroxy-2-morpholino-phenyl cyclopentyl 251 1 4-hydroxy-2-morpholino-phenyl cyclohexyl 252 1 4-hydroxy-2-morpholino-phenyl 3-pyridyl 253 1 4-hydroxy-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 254 1 4-hydroxy-2-morpholino-phenyl 1H-imidazol-4-yl 255 1 4-hydroxy-2-morpholino-phenyl 2-furanyl 256 1 2-CH.sub.3-phenyl Ethyl 257 1 2-CH.sub.3-phenyl n-propyl 258 1 2-CH.sub.3-phenyl Isopropyl 259 1 2-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 260 1 2-CH.sub.3-phenyl CF.sub.3 261 1 2-CH.sub.3-phenyl —CH.sub.2CF.sub.3 262 1 2-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 263 1 2-CH.sub.3-phenyl cyclopropyl 264 1 2-CH.sub.3-phenyl Cyclobutyl 265 1 2-CH.sub.3-phenyl cyclopentyl 266 1 2-CH.sub.3-phenyl cyclohexyl 267 1 2-CH.sub.3-phenyl 3-pyridyl 268 1 2-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 269 1 2-CH.sub.3-phenyl 1H-imidazol-4-yl 270 1 2-CH.sub.3-phenyl 2-furanyl 271 1 4-OH-Phenyl Ethyl 272 1 4-OH-Phenyl n-propyl 273 1 4-OH-Phenyl Isopropyl 274 1 4-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 275 1 4-OH-Phenyl CF.sub.3 276 1 4-OH-Phenyl —CH.sub.2CF.sub.3 277 1 4-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 278 1 4-OH-Phenyl cyclopropyl 279 1 4-OH-Phenyl Cyclobutyl 280 1 4-OH-Phenyl cyclopentyl 281 1 4-OH-Phenyl cyclohexyl 282 1 4-OH-Phenyl 3-pyridyl 283 1 4-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 284 1 4-OH-Phenyl 1H-imidazol-4-yl 285 1 4-OH-Phenyl 2-furanyl 286 1 2-OH-Phenyl Ethyl 287 1 2-OH-Phenyl n-propyl 288 1 2-OH-Phenyl Isopropyl 289 1 2-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 290 1 2-OH-Phenyl CF3 291 1 2-OH-Phenyl —CH.sub.2CF.sub.3 292 1 2-OH-Phenyl —CH2CH2CF3 293 1 2-OH-Phenyl cyclopropyl 294 1 2-OH-Phenyl Cyclobutyl 295 1 2-OH-Phenyl cyclopentyl 296 1 2-OH-Phenyl cyclohexyl 297 1 2-OH-Phenyl 3-pyridyl 298 1 2-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 299 1 2-OH-Phenyl 1H-imidazol-4-yl 300 1 2-OH-Phenyl 2-furanyl 301 1 3-OMe-Phenyl Ethyl 302 1 3-OMe-Phenyl n-propyl 303 1 3-OMe-Phenyl Isopropyl 304 1 3-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 305 1 3-OMe-Phenyl CF.sub.3 306 1 3-OMe-Phenyl —CH.sub.2CF.sub.3 307 1 3-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 308 1 3-OMe-Phenyl cyclopropyl 309 1 3-OMe-Phenyl Cyclobutyl 310 1 3-OMe-Phenyl cyclopentyl 311 1 3-OMe-Phenyl cyclohexyl 312 1 3-OMe-Phenyl 3-pyridyl 313 1 3-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 314 1 3-OMe-Phenyl 1H-imidazol-4-yl 315 1 3-OMe-Phenyl 2-furanyl 316 1 4-CN-Phenyl Ethyl 317 1 4-CN-Phenyl n-propyl 318 1 4-CN-Phenyl Isopropyl 319 1 4-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 320 1 4-CN-Phenyl CF.sub.3 321 1 4-CN-Phenyl —CH.sub.2CF.sub.3 322 1 4-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 323 1 4-CN-Phenyl cyclopropyl 324 1 4-CN-Phenyl Cyclobutyl 325 1 4-CN-Phenyl cyclopentyl 326 1 4-CN-Phenyl cyclohexyl 327 1 4-CN-Phenyl 3-pyridyl 328 1 4-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 329 1 4-CN-Phenyl 1H-imidazol-4-yl 330 1 4-CN-Phenyl 2-furanyl 331 1 2-CN-Phenyl Ethyl 332 1 2-CN-Phenyl n-propyl 333 1 2-CN-Phenyl Isopropyl 334 1 2-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 335 1 2-CN-Phenyl CF.sub.3 336 1 2-CN-Phenyl —CH.sub.2CF.sub.2 337 1 2-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.2 338 1 2-CN-Phenyl cyclopropyl 339 1 2-CN-Phenyl Cyclobutyl 340 1 2-CN-Phenyl cyclopentyl 341 1 2-CN-Phenyl cyclohexyl 342 1 2-CN-Phenyl 3-pyridyl 343 1 2-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 344 1 2-CN-Phenyl 1H-imidazol-4-yl 345 1 2-CN-Phenyl 2-furanyl 346 1 3-F-Phenyl Ethyl 347 1 3-F-Phenyl n-propyl 348 1 3-F-Phenyl Isopropyl 349 1 3-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 350 1 3-F-Phenyl CF.sub.3 351 1 3-F-Phenyl —CH.sub.2CF.sub.2 352 1 3-F-Phenyl —CH.sub.2CH.sub.2CF.sub.2 353 1 3-F-Phenyl cyclopropyl 354 1 3-F-Phenyl Cyclobutyl 355 1 3-F-Phenyl cyclopentyl 356 1 3-F-Phenyl cyclohexyl 357 1 3-F-Phenyl 3-pyridyl 358 1 3-F-Phenyl 1-methyl-1H-pyrazol-4-yl 359 1 3-F-Phenyl 1H-imidazol-4-yl 360 1 3-F-Phenyl 2-furanyl 361 1 2-Cl-Phenyl Ethyl 362 1 2-Cl-Phenyl n-propyl 363 1 2-Cl-Phenyl Isopropyl 364 1 2-Cl-Phenyl —CH.sub.2CH(CH.sub.2).sub.2 365 1 2-Cl-Phenyl CF.sub.3 366 1 2-Cl-Phenyl —CH.sub.2CF.sub.3 367 1 2-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 368 1 2-Cl-Phenyl cyclopropyl 369 1 2-Cl-Phenyl Cyclobutyl 370 1 2-Cl-Phenyl cyclopentyl 371 1 2-Cl-Phenyl cyclohexyl 372 1 2-Cl-Phenyl 3-pyridyl 373 1 2-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 374 1 2-Cl-Phenyl 1H-imidazol-4-yl 375 1 2-Cl-Phenyl 2-furanyl 376 1 4-Cl-Phenyl Ethyl 377 1 4-Cl-Phenyl n-propyl 378 1 4-Cl-Phenyl Isopropyl 379 1 4-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 380 1 4-Cl-Phenyl CF.sub.3 381 1 4-Cl-Phenyl —CH.sub.2CF.sub.3 382 1 4-Cl-Phenyl —CH.sub.2CH.sub.2CF3.sub.3 383 1 4-Cl-Phenyl cyclopropyl 384 1 4-Cl-Phenyl Cyclobutyl 385 1 4-Cl-Phenyl cyclopentyl 386 1 4-Cl-Phenyl cyclohexyl 387 1 4-Cl-Phenyl 3-pyridyl 388 1 4-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 389 1 4-Cl-Phenyl 1H-imidazol-4-yl 390 1 4-Cl-Phenyl 2-furanyl 391 1 3-Br-Phenyl Ethyl 392 1 3-Br-Phenyl n-propyl 393 1 3-Br-Phenyl Isopropyl 394 1 3-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 395 1 3-Br-Phenyl CF.sub.3 396 1 3-Br-Phenyl —CH.sub.2CF.sub.3 397 1 3-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 398 1 3-Br-Phenyl cyclopropyl 399 1 3-Br-Phenyl Cyclobutyl 400 1 3-Br-Phenyl cyclopentyl 401 1 3-Br-Phenyl cyclohexyl 402 1 3-Br-Phenyl 3-pyridyl 403 1 3-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 404 1 3-Br-Phenyl 1H-imidazol-4-yl 405 1 3-BrPhenyl 2-furanyl 406 1 2-CF.sub.3-Phenyl Ethyl 407 1 2-CF.sub.3-Phenyl n-propyl 408 1 2-CF.sub.3-Phenyl Isopropyl 409 1 2-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 410 1 2-CF.sub.3-Phenyl CF.sub.3 411 1 2-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 412 1 2-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 413 1 2-CF.sub.3-Phenyl cyclopropyl 414 1 2-CF.sub.3-Phenyl Cyclobutyl 415 1 2-CF.sub.3-Phenyl cyclopentyl 416 1 2-CF.sub.3-Phenyl cyclohexyl 417 1 2-CF.sub.3-Phenyl 3-pyridyl 418 1 2-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 419 1 2-CF.sub.3-Phenyl 1H-imidazol-4-yl 420 1 2-CF.sub.3-Phenyl 2-furanyl 421 1 4-CF.sub.3-Phenyl Ethyl 422 1 4-CF.sub.3-Phenyl n-propyl 423 1 4-CF.sub.3-Phenyl Isopropyl 424 1 4-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 425 1 4-CF.sub.3-Phenyl CF.sub.3 426 1 4-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 427 1 4-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 428 1 4-CF.sub.3-Phenyl cyclopropyl 429 1 4-CF.sub.3-Phenyl Cyclobutyl 430 1 4-CF.sub.3-Phenyl cyclopentyl 431 1 4-CF.sub.3-Phenyl cyclohexyl 432 1 4-CF.sub.3-Phenyl 3-pyridyl 433 1 4-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 434 1 4-CF.sub.3-Phenyl 1H-imidazol-4-yl 435 1 4-CF.sub.3-Phenyl 2-furanyl 436 1 3-iPr-Phenyl Ethyl 437 1 3-iPr-Phenyl n-propyl 438 1 3-iPr-Phenyl Isopropyl 439 1 3-iPr-Phenyl —CH2CH(CH.sub.3).sub.2 440 1 3-iPr-Phenyl CF.sub.3 441 1 3-iPr-Phenyl —CH.sub.2CF.sub.3 442 1 3-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 443 1 3-iPr-Phenyl cyclopropyl 444 1 3-iPr-Phenyl Cyclobutyl 445 1 3-iPr-Phenyl cyclopentyl 446 1 3-iPr-Phenyl cyclohexyl 447 1 3-iPr-Phenyl 3-pyridyl 448 1 3-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 449 1 3-iPr-Phenyl 1H-imidazol-4-yl 450 1 3-iPr-Phenyl 2-furanyl 451 1 2-morpholino-phenyl Ethyl 452 1 2-morpholino-phenyl n-propyl 453 1 2-morpholino-phenyl isopropyl 454 1 2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 455 1 2-morpholino-phenyl CF.sub.3 456 1 2-morpholino-phenyl —CH.sub.2CF.sub.3 457 1 2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 458 1 2-morpholino-phenyl cyclopropyl 459 1 2-morpholino-phenyl Cyclobutyl 460 1 2-morpholino-phenyl cyclopentyl 461 1 2-morpholino-phenyl cyclohexyl 462 1 2-morpholino-phenyl 3-pyridyl 463 1 2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 464 1 2-morpholino-phenyl 1H-imidazol-4-yl 465 1 2-morpholino-phenyl 2-furanyl 466 1 4-morpholino-phenyl ethyl 467 1 4-morpholino-phenyl n-propyl 468 1 4-morpholino-phenyl isopropyl 469 1 4-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 470 1 4-morpholino-phenyl CF.sub.3 471 1 4-morpholino-phenyl —CH.sub.2CF.sub.3 472 1 4-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 473 1 4-morpholino-phenyl cyclopropyl 474 1 4-morpholino-phenyl Cyclobutyl 475 1 4-morpholino-phenyl cyclopentyl 476 1 4-morpholino-phenyl cyclohexyl 477 1 4-morpholino-phenyl 3-pyridyl 478 1 4-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 479 1 4-morpholino-phenyl 1H-imidazol-4-yl 480 1 4-morpholino-phenyl 2-furanyl 481 1 4-methyl-2-morpholino-phenyl ethyl 482 1 4-methyl-2-morpholino-phenyl n-propyl 483 1 4-methyl-2-morpholino-phenyl isopropyl 484 1 4-methyl-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 485 1 4-methyl-2-morpholino-phenyl CF.sub.3 486 1 4-methyl-2-morpholino-phenyl —CH.sub.2CF.sub.3 487 1 4-methyl-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 488 1 4-methyl-2-morpholino-phenyl cyclopropyl 489 1 4-methyl-2-morpholino-phenyl Cyclobutyl 490 1 4-methyl-2-morpholino-phenyl cyclopentyl 491 1 4-methyl-2-morpholino-phenyl cyclohexyl 492 1 4-methyl-2-morpholino-phenyl 3-pyridyl 493 1 4-methyl-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 494 1 4-methyl-2-morpholino-phenyl 1H-imidazol-4-yl 495 1 4-methyl-2-morpholino-phenyl 2-furanyl 496 2 4-CH.sub.3-phenyl ethyl 497 2 4-CH.sub.3-phenyl n-propyl 498 2 4-CH.sub.3-phenyl isopropyl 499 2 4-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 500 2 4-CH.sub.3-phenyl CF.sub.3 501 2 4-CH.sub.3-phenyl —CH.sub.2CF.sub.3 502 2 4-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 503 2 4-CH.sub.3-phenyl cyclopropyl 504 2 4-CH.sub.3-phenyl Cyclobutyl 505 2 4-CH.sub.3-phenyl cyclopentyl 506 2 4-CH.sub.3-phenyl cyclohexyl 507 2 4-CH.sub.3-phenyl 3-pyridyl 508 2 4-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 509 2 4-CH.sub.3-phenyl 1H-imidazol-4-yl 510 2 4-CH.sub.3-phenyl 2-furanyl 511 2 3-CH.sub.3-phenyl ethyl 512 2 3-CH.sub.3-phenyl n-propyl 513 2 3-CH.sub.3-phenyl isopropyl 514 2 3-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 515 2 3-CH.sub.3-phenyl CF.sub.3 516 2 3-CH.sub.3-phenyl —CH.sub.2CF.sub.3 517 2 3-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 518 2 3-CH.sub.3-phenyl cyclopropyl 519 2 3-CH.sub.3-phenyl Cyclobutyl 520 2 3-CH.sub.3-phenyl cyclopentyl 521 2 3-CH.sub.3-phenyl cyclohexyl 522 2 3-CH.sub.3-phenyl 3-pyridyl 523 2 3-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 524 2 3-CH.sub.3-phenyl 1H-imidazol-4-yl 525 2 3-CH.sub.3-phenyl 2-furanyl 526 2 3-OH-Phenyl ethyl 527 2 3-OH-Phenyl n-propyl 528 2 3-OH-Phenyl isopropyl 529 2 3-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 530 2 3-OH-Phenyl CF.sub.3 531 2 3-OH-Phenyl —CH.sub.2CF.sub.3 532 2 3-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 533 2 3-OH-Phenyl cyclopropyl 534 2 3-OH-Phenyl Cyclobutyl 535 2 3-OH-Phenyl cyclopentyl 536 2 3-OH-Phenyl cyclohexyl 537 2 3-OH-Phenyl 3-pyridyl 538 2 3-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 539 2 3-OH-Phenyl 1H-imidazol-4-yl 540 2 3-OH-Phenyl 2-furanyl 541 2 4-OMe-Phenyl ethyl 542 2 4-OMe-Phenyl n-propyl 543 2 4-OMe-Phenyl isopropyl 544 2 4-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 545 2 4-OMe-Phenyl CF.sub.3 546 2 4-OMe-Phenyl —CH.sub.2CF.sub.3 547 2 4-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 548 2 4-OMe-Phenvl cyclopropyl 549 2 4-OMe-Phenyl Cyclobutyl 550 2 4-OMe-Phenyl cyclopentyl 551 2 4-OMe-Phenyl cyclohexyl 552 2 4-OMe-Phenyl 3-pyridyl 553 2 4-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 554 2 4-OMe-Phenyl 1H-imidazol-4-yl 555 2 4-OMe-Phenyl 2-furanyl 556 2 2-OMe-Phenyl ethyl 557 2 2-OMe-Phenyl n-propyl 558 2 2-OMe-Phenyl isopropyl 559 2 2-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 560 2 2-OMe-Phenyl CF.sub.3 561 2 2-OMe-Phenyl —CH.sub.2CF.sub.3 562 2 2-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 563 2 2-OMe-Phenyl cyclopropyl 564 2 2-OMe-Phenyl Cyclobutyl 565 2 2-OMe-Phenyl cyclopentyl 566 2 2-OMe-Phenyl cyclohexyl 567 2 2-OMe-Phenyl 3-pyridyl 568 2 2-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 569 2 2-OMe-Phenyl 1H-imidazol-4-yl 570 2 2-OMe-Phenyl 2-furanyl 571 2 3-CN-Phenyl ethyl 572 2 3-CN-Phenyl n-propyl 573 2 3-CN-Phenyl isopropyl 574 2 3-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 575 2 3-CN-Phenyl CF.sub.3 576 2 3-CN-Phenyl —CH.sub.2CF.sub.3 577 2 3-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 578 2 3-CN-Phenyl cyclopropyl 579 2 3-CN-Phenyl Cyclobutyl 580 2 3-CN-Phenyl cyclopentyl 581 2 3-CN-Phenyl cyclohexyl 582 2 3-CN-Phenyl 3-pyridyl 583 2 3-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 584 2 3-CN-Phenyl 1H-imidazol-4-yl 585 2 3-CN-Phenyl 2-furanyl 586 2 2-F-Phenyl ethyl 587 2 2-F-Phenyl n-propyl 588 2 2-F-Phenyl isopropyl 589 2 2-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 590 2 2-F-Phenyl CF.sub.3 591 2 2-F-Phenyl —CH.sub.2CF.sub.3 592 2 2-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 593 2 2-F-Phenyl cyclopropyl 594 2 2-F-Phenyl Cyclobutyl 595 2 2-F-Phenyl cyclopentyl 596 2 2-F-Phenyl cyclohexyl 597 2 2-F-Phenyl 3-pyridyl 598 2 2-F-Phenyl 1-methyl-1H-pyrazol-4-yl 599 2 2-F-Phenyl 1H-imidazol-4-yl 600 2 2-F-Phenyl 2-furanyl 601 2 4-F-Phenyl ethyl 602 2 4-F-Phenyl n-propyl 603 2 4-F-Phenyl isopropyl 604 2 4-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 605 2 4-F-Phenyl CF.sub.3 606 2 4-F-Phenyl —CH.sub.2CF.sub.3 607 2 4-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 608 2 4-F-Phenyl cyclopropyl 609 2 4-F-Phenyl Cyclobutyl 610 2 4-F-Phenyl cyclopentyl 611 2 4-F-Phenyl cyclohexyl 612 2 4-F-Phenyl 3-pyridyl 613 2 4-F-Phenyl 1-methyl-1H-pyrazol-4-yl 614 2 4-F-Phenyl 1H-imidazol-4-yl 615 2 4-F-Phenyl 2-furanyl 616 2 3-Cl-Phenyl ethyl 617 2 3-Cl-Phenyl n-propyl 618 2 3-Cl-Phenyl isopropyl 619 2 3-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 620 2 3-Cl-Phenyl CF.sub.3 621 2 3-Cl-Phenyl —CH.sub.2CF.sub.3 622 2 3-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 623 2 3-Cl-Phenyl cyclopropyl 624 2 3-Cl-Phenyl Cyclobutyl 625 2 3-Cl-Phenyl cyclopentyl 626 2 3-Cl-Phenyl cyclohexyl 627 2 3-Cl-Phenyl 3-pyridyl 628 2 3-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 629 2 3-Cl-Phenyl 1H-imidazol-4-yl 630 2 3-Cl-Phenyl 2-furanyl 631 2 2-Br-Phenyl ethyl 632 2 2-Br-Phenyl n-propyl 633 2 2-Br-Phenyl isopropyl 634 2 2-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 635 2 2-Br-Phenyl CF.sub.3 636 2 2-Br-Phenyl —CH.sub.2CF.sub.3 637 2 2-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 638 2 2-Br-Phenyl cyclopropyl 639 2 2-Br-Phenyl Cyclobutyl 640 2 2-Br-Phenyl cyclopentyl 641 2 2-Br-Phenyl cyclohexyl 642 2 2-Br-Phenyl 3-pyridyl 643 2 2-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 644 2 2-Br-Phenyl 1H-imidazol-4-yl 645 2 2-Br-Phenyl 2-furanyl 646 2 4-Br-Phenyl ethyl 647 2 4-Br-Phenyl n-propyl 648 2 4-Br-Phenyl isopropyl 649 2 4-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 650 2 4-Br-Phenyl CF.sub.3 651 2 4-Br-Phenyl —CH.sub.2CF.sub.3 652 2 4-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 653 2 4-Br-Phenyl cyclopropyl 654 2 4-Br-Phenyl Cyclobutyl 655 2 4-Br-Phenyl cyclopentyl 656 2 4-Br-Phenyl cyclohexyl 657 2 4-Br-Phenyl 3-pyridyl 658 2 4-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 659 2 4-Br-Phenyl 1H-imidazol-4-yl 660 2 4-Br-Phenyl 2-furanyl 661 2 3-CF.sub.3-Phenyl ethyl 662 2 3-CF.sub.3-Phenyl n-propyl 663 2 3-CF.sub.3-Phenyl isopropyl 664 2 3-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 665 2 3-CF.sub.3-Phenyl CF.sub.3 666 2 3-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 667 2 3-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 668 2 3-CF.sub.3-Phenyl cyclopropyl 669 2 3-CF.sub.3-Phenyl Cyclobutyl 670 2 3-CF.sub.3-Phenyl cyclopentyl 671 2 3-CF.sub.3-Phenyl cyclohexyl 672 2 3-CF.sub.3-Phenyl 3-pyridyl 673 2 3-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 674 2 3-CF.sub.3-Phenyl 1H-imidazol-4-yl 675 2 3-CF.sub.3-Phenyl 2-furanyl 676 2 2-iPr-Phenyl ethyl 677 2 2-iPr-Phenyl n-propyl 678 2 2-iPr-Phenyl isopropyl 679 2 2-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 680 2 2-iPr-Phenyl CF.sub.3 681 2 2-iPr-Phenyl —CH.sub.2CF.sub.3 682 2 2-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 683 2 2-iPr-Phenyl cyclopropyl 684 2 2-iPr-Phenyl Cyclobutyl 685 2 2-iPr-Phenyl cyclopentyl 686 2 2-iPr-Phenyl cyclohexyl 687 2 2-iPr-Phenyl 3-pyridyl 688 2 2-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 689 2 2-iPr-Phenyl 1H-imidazol-4-yl 690 2 2-iPr-Phenyl 2-furanyl 691 2 4-iPr-Phenyl ethyl 692 2 4-iPr-Phenyl n-propyl 693 2 4-iPr-Phenyl isopropyl 694 2 4-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 695 2 4-iPr-Phenyl CF.sub.3 696 2 4-iPr-Phenyl —CH.sub.2CF.sub.3 697 2 4-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 698 2 4-iPr-Phenyl cyclopropyl 699 2 4-iPr-Phenyl Cyclobutyl 700 2 4-iPr-Phenyl cyclopentyl 701 2 4-iPr-Phenyl cyclohexyl 702 2 4-iPr-Phenyl 3-pyridyl 703 2 4-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 704 2 4-iPr-Phenyl 1H-imidazol-4-yl 705 2 4-iPr-Phenyl 2-furanyl 706 2 3-morpholino-phenyl ethyl 707 2 3-morpholino-phenyl n-propyl 708 2 3-morpholino-phenyl isopropyl 709 2 3-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 710 2 3-morpholino-phenyl CF.sub.3 711 2 3-morpholino-phenyl —CH.sub.2CF.sub.3 712 2 3-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 713 2 3-morpholino-phenyl cyclopropyl 714 2 3-morpholino-phenyl Cyclobutyl 715 2 3-morpholino-phenyl cyclopentyl 716 2 3-morpholino-phenyl cyclohexyl 717 2 3-morpholino-phenyl 3-pyridyl 718 2 3-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 719 2 3-morpholino-phenyl 1H-imidazol-4-yl 720 2 3-morpholino-phenyl 2-furanyl 721 2 4-cyano-2-morpholino-phenyl ethyl 722 2 4-cyano-2-morpholino-phenyl n-propyl 723 2 4-cyano-2-morpholino-phenyl isopropyl 724 2 4-cyano-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 725 2 4-cyano-2-morpholino-phenyl CF.sub.3 726 2 4-cyano-2-morpholino-phenyl —CH.sub.2CF.sub.3 727 2 4-cyano-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 728 2 4-cyano-2-morpholino-phenyl cyclopropyl 729 2 4-cyano-2-morpholino-phenyl Cyclobutyl 730 2 4-cyano-2-morpholino-phenyl cyclopentyl 731 2 4-cyano-2-morpholino-phenyl cyclohexyl 732 2 4-cyano-2-morpholino-phenyl 3-pyridyl 733 2 4-cyano-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 734 2 4-cyano-2-morpholino-phenyl 1H-imidazol-4-yl 735 2 4-cyano-2-morpholino-phenyl 2-furanyl 736 2 4-hydroxy-2-morpholino-phenyl ethyl 737 2 4-hydroxy-2-morpholino-phenyl n-propyl 738 2 4-hydroxy-2-morpholino-phenyl isopropyl 739 2 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 740 2 4-hydroxy-2-morpholino-phenyl CF.sub.3 741 2 4-hydroxy-2-morpholino-phenyl —CH.sub.2CF.sub.3 742 2 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 743 2 4-hydroxy-2-morpholino-phenyl cyclopropyl 744 2 4-hydroxy-2-morpholino-phenyl Cyclobutyl 745 2 4-hydroxy-2-morpholino-phenyl cyclopentyl 746 2 4-hydroxy-2-morpholino-phenyl cyclohexyl 747 2 4-hydroxy-2-morpholino-phenyl 3-pyridyl 748 2 4-hydroxy-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 749 2 4-hydroxy-2-morpholino-phenyl 1H-imidazol-4-yl 750 2 4-hydroxy-2-morpholino-phenyl 2-furanyl 751 2 2-CH.sub.3-phenyl Ethyl 752 2 2-CH.sub.3-phenyl n-propyl 753 2 2-CH.sub.3-phenyl Isopropyl 754 2 2-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 755 2 2-CH.sub.3-phenyl CF.sub.3 756 2 2-CH.sub.3-phenyl —CH.sub.2CF.sub.3 757 2 2-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 758 2 2-CH.sub.3-phenyl cyclopropyl 759 2 2-CH.sub.3-phenyl Cyclobutyl 760 2 2-CH.sub.3-phenyl cyclopentyl 761 2 2-CH.sub.3-phenyl cyclohexyl 762 2 2-CH.sub.3-phenyl 3-pyridyl 763 2 2-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 764 2 2-CH.sub.3-phenyl 1H-imidazol-4-yl 765 2 2-CH.sub.3-phenyl 2-furanyl 766 2 4-OH-Phenyl Ethyl 767 2 4-OH-Phenyl n-propyl 768 2 4-OH-Phenyl Isopropyl 769 2 4-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 770 2 4-OH-Phenyl CF.sub.3 771 2 4-OH-Phenyl —CH.sub.2CF.sub.3 772 2 4-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 773 2 4-OH-Phenyl cyclopropyl 774 2 4-OH-Phenyl Cyclobutyl 775 2 4-OH-Phenyl cyclopentyl 776 2 4-OH-Phenyl cyclohexyl 777 2 4-OH-Phenyl 3-pyridyl 778 2 4-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 779 2 4-OH-Phenyl 1H-imidazol-4-yl 780 2 4-OH-Phenyl 2-furanyl 781 2 2-OH-Phenyl Ethyl 782 2 2-OH-Phenyl n-propyl 783 2 2-OH-Phenyl Isopropyl 784 2 2-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 785 2 2-OH-Phenyl CF.sub.3 786 2 2-OH-Phenyl —CH.sub.2CF.sub.3 787 2 2-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 788 2 2-OH-Phenyl cyclopropyl 789 2 2-OH-Phenyl Cyclobutyl 790 2 2-OH-Phenyl cyclopentyl 791 2 2-OH-Phenyl cyclohexyl 792 2 2-OH-Phenyl 3-pyridyl 793 2 2-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 794 2 2-OH-Phenyl 1H-imidazol-4-yl 795 2 2-OH-Phenyl 2-furanyl 796 2 3-OMe-Phenyl Ethyl 797 2 3-OMe-Phenyl n-propyl 798 2 3-OMe-Phenyl Isopropyl 799 2 3-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 800 2 3-OMe-Phenyl CF.sub.3 801 2 3-OMe-Phenyl —CH.sub.2CF.sub.3 802 2 3-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 803 2 3-OMe-Phenyl cyclopropyl 804 2 3-OMe-Phenyl Cyclobutyl 805 2 3-OMe-Phenyl cyclopentyl 806 2 3-OMe-Phenyl cyclohexyl 807 2 3-OMe-Phenyl 3-pyridyl 808 2 3-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 809 2 3-OMe-Phenyl 1H-imidazol-4-yl 810 2 3-OMe-Phenyl 2-furanyl 811 2 4-CN-Phenyl Ethyl 812 2 4-CN-Phenyl n-propyl 813 2 4-CN-Phenyl Isopropyl 814 2 4-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 815 2 4-CN-Phenyl CF.sub.3 816 2 4-CN-Phenyl —CH.sub.2CF.sub.3 817 2 4-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 818 2 4-CN-Phenyl cyclopropyl 819 2 4-CN-Phenyl Cyclobutyl 820 2 4-CN-Phenyl cyclopentyl 821 2 4-CN-Phenyl cyclohexyl 822 2 4-CN-Phenyl 3-pyridyl 823 2 4-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 824 2 4-CN-Phenyl 1H-imidazol-4-yl 825 2 4-CN-Phenyl 2-furanyl 826 2 2-CN-Phenyl Ethyl 827 2 2-CN-Phenyl n-propyl 828 2 2-CN-Phenyl Isopropyl 829 2 2-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 830 2 2-CN-Phenyl CF.sub.3 831 2 2-CN-Phenyl —CH.sub.2CF.sub.3 832 2 2-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 833 2 2-CN-Phenyl cyclopropyl 834 2 2-CN-Phenyl Cyclobutyl 835 2 2-CN-Phenyl cyclopentyl 836 2 2-CN-Phenyl cyclohexyl 837 2 2-CN-Phenyl 3-pyridyl 838 2 2-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 839 2 2-CN-Phenyl 1H-imidazol-4-yl 840 2 2-CN-Phenyl 2-furanyl 841 2 3-F-Phenyl Ethyl 842 2 3-F-Phenyl n-propyl 843 2 3-F-Phenyl Isopropyl 844 2 3-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 845 2 3-F-Phenyl CF.sub.3 846 2 3-F-Phenyl —CH.sub.2CF.sub.3 847 2 3-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 848 2 3-F-Phenyl cyclopropyl 849 2 3-F-Phenyl Cyclobutyl 850 2 3-F-Phenyl cyclopentyl 851 2 3-F-Phenyl cvclohexyl 852 2 3-F-Phenyl 3-pyridyl 853 2 3-F-Phenyl 1-methyl-1H-pyrazol-4-yl 854 2 3-F-Phenyl 1H-imidazol-4-yl 855 2 3-F-Phenyl 2-furanyl 856 2 2-Cl-Phenyl Ethyl 857 2 2-Cl-Phenyl n-propyl 858 2 2-Cl-Phenyl Isopropyl 859 2 2-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 860 2 2-Cl-Phenyl CF.sub.3 861 2 2-Cl-Phenyl —CH.sub.2CF.sub.3 862 2 2-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 863 2 2-Cl-Phenyl cyclopropyl 864 2 2-Cl-Phenyl Cyclobutyl 865 2 2-Cl-Phenyl cyclopentyl 866 2 2-Cl-Phenyl cyclohexyl 867 2 2-Cl-Phenyl 3-pyridyl 868 2 2-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 869 2 2-Cl-Phenyl 1H-imidazol-4-yl 870 2 2-Cl-Phenyl 2-furanyl 871 2 4-Cl-Phenyl Ethyl 872 2 4-Cl-Phenyl n-propyl 873 2 4-Cl-Phenyl Isopropyl 874 2 4-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 875 2 4-Cl-Phenyl CF.sub.3 876 2 4-Cl-Phenyl —CH.sub.2CF.sub.3 877 2 4-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 878 2 4-Cl-Phenyl cyclopropyl 879 2 4-Cl-Phenyl Cyclobutyl 880 2 4-Cl-Phenyl cyclopentyl 881 2 4-Cl-Phenyl cyclohexyl 882 2 4-Cl-Phenyl 3-pyridyl 883 2 4-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 884 2 4-Cl-Phenyl 1H-imidazol-4-yl 885 2 4-Cl-Phenyl 2-furanyl 886 2 3-Br-Phenyl Ethyl 887 2 3-Br-Phenyl n-propyl 888 2 3-Br-Phenyl Isopropyl 889 2 3-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 890 2 3-Br-Phenyl CF.sub.3 891 2 3-Br-Phenyl —CH.sub.2CF.sub.3 892 2 3-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 893 2 3-Br-Phenyl cyclopropyl 894 2 3-Br-Phenyl Cyclobutyl 895 2 3-Br-Phenyl cyclopentyl 896 2 3-Br-Phenyl cyclohexyl 897 2 3-Br-Phenyl 3-pyridyl 898 2 3-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 899 2 3-Br-Phenyl 1H-imidazol-4-yl 900 2 3-Br-Phenyl 2-furanyl 901 2 2-CF.sub.3-Phenyl Ethyl 902 2 2-CF.sub.3-Phenyl n-propyl 903 2 2-CF.sub.3-Phenyl Isopropyl 904 2 2-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 905 2 2-CF.sub.3-Phenyl CF.sub.3 906 2 2-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 907 2 2-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 908 2 2-CF.sub.3-Phenyl cyclopropyl 909 2 2-CF.sub.3-Phenyl Cyclobutyl 910 2 2-CF.sub.3-Phenyl cyclopentyl 911 2 2-CF.sub.3-Phenyl cyclohexyl 912 2 2-CF.sub.3-Phenyl 3-pyridyl 913 2 2-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 914 2 2-CF.sub.3-Phenyl 1H-imidazol-4-yl 915 2 2-CF.sub.3-Phenyl 2-furanyl 916 2 4-CF.sub.3-Phenyl Ethyl 917 2 4-CF.sub.3-Phenyl n-propyl 918 2 4-CF.sub.3-Phenyl Isopropyl 919 2 4-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 920 2 4-CF.sub.3-Phenyl CF.sub.3 921 2 4-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 922 2 4-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 923 2 4-CF.sub.3-Phenyl cyclopropyl 924 2 4-CF.sub.3-Phenyl Cyclobutyl 925 2 4-CF.sub.3-Phenyl cyclopentyl 926 2 4-CF.sub.3-Phenyl cyclohexyl 927 2 4-CF.sub.3-Phenyl 3-pyridyl 928 2 4-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 929 2 4-CF.sub.3-Phenyl 1H-imidazol-4-yl 930 2 4-CF.sub.3-Phenyl 2-furanyl 931 2 3-iPr-Phenyl Ethyl 932 2 3-iPr-Phenyl n-propyl 933 2 3-iPr-Phenyl Isopropyl 934 2 3-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 935 2 3-iPr-Phenyl CF.sub.3 936 2 3-iPr-Phenyl —CH.sub.2CF.sub.3 937 2 3-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 938 2 3-iPr-Phenyl cyclopropyl 939 2 3-iPr-Phenyl Cyclobutyl 940 2 3-iPr-Phenyl cyclopentyl 941 2 3-iPr-Phenyl cyclohexyl 942 2 3-iPr-Phenyl 3-pyridyl 943 2 3-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 944 2 3-iPr-Phenyl 1H-imidazol-4-yl 945 2 3-iPr-Phenyl 2-furanyl 946 2 2-morpholino-phenyl Ethyl 947 2 2-morpholino-phenyl n-propyl 948 2 2-morpholino-phenyl isopropyl 949 2 2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 950 2 2-morpholino-phenyl CF.sub.3 951 2 2-morpholino-phenyl —CH.sub.2CF.sub.3 952 2 2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 953 2 2-morpholino-phenyl cyclopropyl 954 2 2-morpholino-phenyl Cyclobutyl 955 2 2-morpholino-phenyl cyclopentyl 956 2 2-morpholino-phenyl cyclohexyl 957 2 2-morpholino-phenyl 3-pyridyl 958 2 2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 959 2 2-morpholino-phenyl 1H-imidazol-4-yl 960 2 2-morpholino-phenyl 2-furanyl 961 2 4-morpholino-phenyl ethyl 962 2 4-morpholino-phenyl n-propyl 963 2 4-morpholino-phenyl isopropyl 964 2 4-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 965 2 4-morpholino-phenyl CF.sub.3 966 2 4-morpholino-phenyl —CH.sub.2CF.sub.3 967 2 4-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 968 2 4-morpholino-phenyl cyclopropyl 969 2 4-morpholino-phenyl Cyclobutyl 970 2 4-morpholino-phenyl cyclopentyl 971 2 4-morpholino-phenyl cyclohexyl 972 2 4-morpholino-phenyl 3-pyridyl 973 2 4-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 974 2 4-morpholino-phenyl 1H-imidazol-4-yl 975 2 4-morpholino-phenyl 2-furanyl 976 2 4-methyl-2-morpholino-phenyl ethyl 977 2 4-methyl-2-morpholino-phenyl n-propyl 978 2 4-methyl-2-morpholino-phenyl isopropyl 979 2 4-methyl-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 980 2 4-methyl-2-morpholino-phenyl CF.sub.3 981 2 4-methyl-2-morpholino-phenyl —CH.sub.2CF.sub.3 982 2 4-methyl-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 983 2 4-methyl-2-morpholino-phenyl cyclopropyl 984 2 4-methyl-2-morpholino-phenyl Cyclobutyl 985 2 4-methyl-2-morpholino-phenyl cyclopentyl 986 2 4-methyl-2-morpholino-phenyl cyclohexyl 987 2 4-methyl-2-morpholino-phenyl 3-pyridyl 988 2 4-methyl-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 989 2 4-methyl-2-morpholino-phenyl 1H-imidazol-4-yl 990 2 4-methyl-2-morpholino-phenyl 2-furanyl 991 3 4-CH.sub.3-phenyl ethyl 992 3 4-CH.sub.3-phenyl n-propyl 993 3 4-CH.sub.3-phenyl isopropyl 994 3 4-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 995 3 4-CH.sub.3-phenyl CF.sub.3 996 3 4-CH.sub.3-phenyl —CH.sub.2CF.sub.3 997 3 4-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 998 3 4-CH.sub.3-phenyl cyclopropyl 999 3 4-CH.sub.3-phenyl Cyclobutyl 1000 3 4-CH.sub.3-phenyl cyclopentyl 1001 3 4-CH.sub.3-phenyl cyclohexyl 1002 3 4-CH.sub.3-phenyl 3-pyridyl 1003 3 4-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1004 3 4-CH.sub.3-phenyl 1H-imidazol-4-yl 1005 3 4-CH.sub.3-phenyl 2-furanyl 1006 3 3-CH.sub.3-phenyl ethyl 1007 3 3-CH.sub.3-phenyl n-propyl 1008 3 3-CH.sub.3-phenyl isopropyl 1009 3 3-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1010 3 3-CH.sub.3-phenyl CF.sub.3 1011 3 3-CH.sub.3-phenyl —CH.sub.2CF.sub.3 1012 3 3-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 1013 3 3-CH.sub.3-phenyl cyclopropyl 1014 3 3-CH.sub.3-phenyl Cyclobutyl 1015 3 3-CH.sub.3-phenyl cyclopentyl 1016 3 3-CH.sub.3-phenyl cyclohexyl 1017 3 3-CH.sub.3-phenyl 3-pyridyl 1018 3 3-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1019 3 3-CH.sub.3-phenyl 1H-imidazol-4-yl 1020 3 3-CH.sub.3-phenyl 2-furanyl 1021 3 3-OH-Phenyl ethyl 1022 3 3-OH-Phenyl n-propyl 1023 3 3-OH-Phenyl isopropyl 1024 3 3-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1025 3 3-OH-Phenyl CF.sub.3 1026 3 3-OH-Phenyl —CH.sub.2CF.sub.3 1027 3 3-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1028 3 3-OH-Phenyl cyclopropyl 1029 3 3-OH-Phenyl Cyclobutyl 1030 3 3-OH-Phenyl cyclopentyl 1031 3 3-OH-Phenyl cyclohexyl 1032 3 3-OH-Phenyl 3-pyridyl 1033 3 3-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1034 3 3-OH-Phenyl 1H-imidazol-4-yl 1035 3 3-OH-Phenyl 2-furanyl 1036 3 4-OMe-Phenyl ethyl 1037 3 4-OMe-Phenyl n-propyl 1038 3 4-OMe-Phenyl isopropyl 1039 3 4-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1040 3 4-OMe-Phenyl CF.sub.3 1041 3 4-OMe-Phenyl —CH.sub.2CF.sub.3 1042 3 4-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1043 3 4-OMe-Phenyl cyclopropyl 1044 3 4-OMe-Phenyl Cyclobutyl 1045 3 4-OMe-Phenyl cyclopentyl 1046 3 4-OMe-Phenyl cyclohexyl 1047 3 4-OMe-Phenyl 3-pyridyl 1048 3 4-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1049 3 4-OMe-Phenyl 1H-imidazol-4-yl 1050 3 4-OMe-Phenyl 2-furanyl 1051 3 2-OMe-Phenyl ethyl 1052 3 2-OMe-Phenyl n-propyl 1053 3 2-OMe-Phenyl isopropyl 1054 3 2-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1055 3 2-OMe-Phenyl CF.sub.3 1056 3 2-OMe-Phenyl —CH.sub.2CF.sub.3 1057 3 2-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1058 3 2-OMe-Phenyl cyclopropyl 1059 3 2-OMe-Phenyl Cyclobutyl 1060 3 2-OMe-Phenyl cyclopentyl 1061 3 2-OMe-Phenyl cyclohexyl 1062 3 2-OMe-Phenyl 3-pyridyl 1063 3 2-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1064 3 2-OMe-Phenyl 1H-imidazol-4-yl 1065 3 2-OMe-Phenyl 2-furanyl 1066 3 3-CN-Phenyl ethyl 1067 3 3-CN-Phenyl n-propyl 1068 3 3-CN-Phenyl isopropyl 1069 3 3-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1070 3 3-CN-Phenyl CF.sub.3 1071 3 3-CN-Phenyl —CH.sub.2CF.sub.3 1072 3 3-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1073 3 3-CN-Phenyl cyclopropyl 1074 3 3-CN-Phenyl Cyclobutyl 1075 3 3-CN-Phenyl cyclopentyl 1076 3 3-CN-Phenyl cyclohexyl 1077 3 3-CN-Phenyl 3-pyridyl 1078 3 3-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1079 3 3-CN-Phenyl 1H-imidazol-4-yl 1080 3 3-CN-Phenyl 2-furanyl 1081 3 2-F-Phenyl ethyl 1082 3 2-F-Phenyl n-propyl 1083 3 2-F-Phenyl isopropyl 1084 3 2-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1085 3 2-F-Phenyl CF.sub.3 1086 3 2-F-Phenyl —CH.sub.2CF.sub.3 1087 3 2-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1088 3 2-F-Phenyl cyclopropyl 1089 3 2-F-Phenyl Cyclobutyl 1090 3 2-F-Phenyl cyclopentyl 1091 3 2-F-Phenyl cyclohexyl 1092 3 2-F-Phenyl 3-pyridyl 1093 3 2-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1094 3 2-F-Phenyl 1H-imidazol-4-yl 1095 3 2-F-Phenyl 2-furanyl 1096 3 4-F-Phenyl ethyl 1097 3 4-F-Phenyl n-propyl 1098 3 4-F-Phenyl isopropyl 1099 3 4-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1100 3 4-F-Phenyl CF.sub.3 1101 3 4-F-Phenyl —CH.sub.2CF.sub.3 1102 3 4-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1103 3 4-F-Phenyl cyclopropyl 1104 3 4-F-Phenyl Cyclobutyl 1105 3 4-F-Phenyl cyclopentyl 1106 3 4-F-Phenyl cyclohexyl 1107 3 4-F-Phenyl 3-pyridyl 1108 3 4-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1109 3 4-F-Phenyl 1H-imidazol-4-yl 1110 3 4-F-Phenyl 2-furanyl 1111 3 3-Cl-Phenyl ethyl 1112 3 3-Cl-Phenyl n-propyl 1113 3 3-Cl-Phenyl isopropyl 1114 3 3-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1115 3 3-Cl-Phenyl CF.sub.3 1116 3 3-Cl-Phenyl —CH.sub.2CF.sub.3 1117 3 3-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1118 3 3-Cl-Phenyl cyclopropyl 1119 3 3-Cl-Phenyl Cyclobutyl 1120 3 3-Cl-Phenyl cyclopentyl 1121 3 3-Cl-Phenyl cyclohexyl 1122 3 3-Cl-Phenyl 3-pyridyl 1123 3 3-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1124 3 3-Cl-Phenyl 1H-imidazol-4-yl 1125 3 3-Cl-Phenyl 2-furanyl 1126 3 2-Br-Phenyl ethyl 1127 3 2-Br-Phenyl n-propyl 1128 3 2-Br-Phenyl isopropyl 1129 3 2-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1130 3 2-Br-Phenyl CF.sub.3 1131 3 2-Br-Phenyl —CH.sub.2CF.sub.3 1132 3 2-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1133 3 2-Br-Phenyl cyclopropyl 1134 3 2-Br-Phenyl Cyclobutyl 1135 3 2-Br-Phenyl cyclopentyl 1136 3 2-Br-Phenyl cyclohexyl 1137 3 2-Br-Phenyl 3-pyridyl 1138 3 2-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1139 3 2-Br-Phenyl 1H-imidazol-4-yl 1140 3 2-Br-Phenyl 2-furanyl 1141 3 4-Br-Phenyl ethyl 1142 3 4-Br-Phenyl n-propyl 1143 3 4-Br-Phenyl isopropyl 1144 3 4-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1145 3 4-Br-Phenyl CF.sub.3 1146 3 4-Br-Phenyl —CH.sub.2CF.sub.3 1147 3 4-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1148 3 4-Br-Phenyl cyclopropyl 1149 3 4-Br-Phenyl Cyclobutyl 1150 3 4-Br-Phenyl cyclopentyl 1151 3 4-Br-Phenyl cyclohexyl 1152 3 4-Br-Phenyl 3-pyridyl 1153 3 4-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1154 3 4-Br-Phenyl 1H-imidazol-4-yl 1155 3 4-Br-Phenyl 2-furanyl 1156 3 3-CF.sub.3-Phenyl ethyl 1157 3 3-CF.sub.3-Phenyl n-propyl 1158 3 3-CF.sub.3-Phenyl isopropyl 1159 3 3-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1160 3 3-CF.sub.3-Phenyl CF.sub.3 1161 3 3-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1162 3 3-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1163 3 3-CF.sub.3-Phenyl cyclopropyl 1164 3 3-CF.sub.3-Phenyl Cyclobutyl 1165 3 3-CF.sub.3-Phenyl cyclopentyl 1166 3 3-CF.sub.3-Phenyl cyclohexyl 1167 3 3-CF.sub.3-Phenyl 3-pyridyl 1168 3 3-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1169 3 3-CF.sub.3-Phenyl 1H-imidazol-4-yl 1170 3 3-CF.sub.3-Phenyl 2-furanyl 1171 3 2-iPr-Phenyl ethyl 1172 3 2-iPr-Phenyl n-propyl 1173 3 2-iPr-Phenyl isopropyl 1174 3 2-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1175 3 2-iPr-Phenyl CF.sub.3 1176 3 2-iPr-Phenyl —CH.sub.2CF.sub.3 1177 3 2-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1178 3 2-iPr-Phenyl cyclopropyl 1179 3 2-iPr-Phenyl Cyclobutyl 1180 3 2-iPr-Phenyl cyclopentyl 1181 3 2-iPr-Phenyl cyclohexyl 1182 3 2-iPr-Phenyl 3-pyridyl 1183 3 2-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1184 3 2-iPr-Phenyl 1H-imidazol-4-yl 1185 3 2-iPr-Phenyl 2-furanyl 1186 3 4-iPr-Phenyl ethyl 1187 3 4-iPr-Phenyl n-propyl 1188 3 4-iPr-Phenyl isopropyl 1189 3 4-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1190 3 4-iPr-Phenyl CF.sub.3 1191 3 4-iPr-Phenyl —CH.sub.2CF.sub.3 1192 3 4-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1193 3 4-iPr-Phenyl cyclopropyl 1194 3 4-iPr-Phenyl Cyclobutyl 1195 3 4-iPr-Phenyl cyclopentyl 1196 3 4-iPr-Phenyl cyclohexyl 1197 3 4-iPr-Phenyl 3-pyridyl 1198 3 4-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1199 3 4-iPr-Phenyl 1H-imidazol-4-yl 1200 3 4-iPr-Phenyl 2-furanyl 1201 3 3-morpholino-phenyl ethyl 1202 3 3-morpholino-phenyl n-propyl 1203 3 3-morpholino-phenyl isopropyl 1204 3 3-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1205 3 3-morpholino-phenyl CF.sub.3 1206 3 3-morpholino-phenyl —CH.sub.2CF.sub.3 1207 3 3-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1208 3 3-morpholino-phenyl cyclopropyl 1209 3 3-morpholino-phenyl Cyclobutyl 1210 3 3-morpholino-phenyl cyclopentyl 1211 3 3-morpholino-phenyl cyclohexyl 1212 3 3-morpholino-phenyl 3-pyridyl 1213 3 3-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1214 3 3-morpholino-phenyl 1H-imidazol-4-yl 1215 3 3-morpholino-phenyl 2-furanyl 1216 3 4-cyano-2-morpholino-phenyl ethyl 1217 3 4-cyano-2-morpholino-phenyl n-propyl 1218 3 4-cyano-2-morpholino-phenyl isopropyl 1219 3 4-cyano-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1220 3 4-cyano-2-morpholino-phenyl CF.sub.3 1221 3 4-cyano-2-morpholino-phenyl —CH.sub.2CF.sub.3 1222 3 4-cyano-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1223 3 4-cyano-2-morpholino-phenyl cyclopropyl 1224 3 4-cyano-2-morpholino-phenyl Cyclobutyl 1225 3 4-cyano-2-morpholino-phenyl cyclopentyl 1226 3 4-cyano-2-morpholino-phenyl cyclohexyl 1227 3 4-cyano-2-morpholino-phenyl 3-pyridyl 1228 3 4-cyano-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1229 3 4-cyano-2-morpholino-phenyl 1H-imidazol-4-yl 1230 3 4-cyano-2-morpholino-phenyl 2-furanyl 1231 3 4-hydroxy-2-morpholino-phenyl ethyl 1232 3 4-hydroxy-2-morpholino-phenyl n-propyl 1233 3 4-hydroxy-2-morpholino-phenyl isopropyl 1234 3 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1235 3 4-hydroxy-2-morpholino-phenyl CF.sub.3 1236 3 4-hydroxy-2-morpholino-phenyl —CH.sub.2CF.sub.3 1237 3 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1238 3 4-hydroxy-2-morpholino-phenyl cyclopropyl 1239 3 4-hydroxy-2-morpholino-phenyl Cyclobutyl 1240 3 4-hydroxy-2-morpholino-phenyl cyclopentyl 1241 3 4-hydroxy-2-morpholino-phenyl cyclohexyl 1242 3 4-hydroxy-2-morpholino-phenyl 3-pyridyl 1243 3 4-hydroxy-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1244 3 4-hydroxy-2-morpholino-phenyl 1H-imidazol-4-yl 1245 3 4-hydroxy-2-morpholino-phenyl 2-furanyl 1246 3 2-CH.sub.3-phenyl Ethyl 1247 3 2-CH.sub.3-phenyl n-propyl 1248 3 2-CH.sub.3-phenyl Isopropyl 1249 3 2-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1250 3 2-CH.sub.3-phenyl CF.sub.3 1251 3 2-CH.sub.3-phenyl —CH.sub.2CF.sub.3 1252 3 2-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 1253 3 2-CH.sub.3-phenyl cyclopropyl 1254 3 2-CH.sub.3-phenyl Cyclobutyl 1255 3 2-CH.sub.3-phenyl cyclopentyl 1256 3 2-CH.sub.3-phenyl cyclohexyl 1257 3 2-CH.sub.3-phenyl 3-pyridyl 1258 3 2-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1259 3 2-CH.sub.3-phenyl 1H-imidazol-4-yl 1260 3 2-CH.sub.3-phenyl 2-furanyl 1261 3 4-OH-Phenyl Ethyl 1262 3 4-OH-Phenyl n-propyl 1263 3 4-OH-Phenyl Isopropyl 1264 3 4-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1265 3 4-OH-Phenyl CF.sub.3 1266 3 4-OH-Phenyl —CH.sub.2CF.sub.3 1267 3 4-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1268 3 4-OH-Phenyl cyclopropyl 1269 3 4-OH-Phenyl Cyclobutyl 1270 3 4-OH-Phenyl cyclopentyl 1271 3 4-OH-Phenyl cyclohexyl 1272 3 4-OH-Phenyl 3-pyridyl 1273 3 4-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1274 3 4-OH-Phenyl 1H-imidazol-4-yl 1275 3 4-OH-Phenyl 2-furanyl 1276 3 2-OH-Phenyl Ethyl 1277 3 2-OH-Phenyl n-propyl 1278 3 2-OH-Phenyl Isopropyl 1279 3 2-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1280 3 2-OH-Phenyl CF.sub.3 1281 3 2-OH-Phenyl —CH.sub.2CF.sub.3 1282 3 2-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1283 3 2-OH-Phenyl cyclopropyl 1284 3 2-OH-Phenyl Cyclobutyl 1285 3 2-OH-Phenyl cyclopentyl 1286 3 2-OH-Phenyl cyclohexyl 1287 3 2-OH-Phenyl 3-pyridyl 1288 3 2-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1289 3 2-OH-Phenyl 1H-imidazol-4-yl 1290 3 2-OH-Phenyl 2-furanyl 1291 3 3-OMe-Phenyl Ethyl 1292 3 3-OMe-Phenyl n-propyl 1293 3 3-OMe-Phenyl Isopropyl 1294 3 3-OMe-Phenyl —CH.sub.2CH(CH3).sub.2 1295 3 3-OMe-Phenyl CF.sub.3 1296 3 3-OMe-Phenyl —CH.sub.2CF.sub.3 1297 3 3-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1298 3 3-OMe-Phenyl cyclopropyl 1299 3 3-OMe-Phenyl Cyclobutyl 1300 3 3-OMe-Phenyl cyclopentyl 1301 3 3-OMe-Phenyl cyclohexyl 1302 3 3-OMe-Phenyl 3-pyridyl 1303 3 3-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1304 3 3-OMe-Phenyl 1H-imidazol-4-yl 1305 3 3-OMe-Phenyl 2-furanyl 1306 3 4-CN-Phenyl Ethyl 1307 3 4-CN-Phenyl n-propyl 1308 3 4-CN-Phenyl Isopropyl 1309 3 4-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1310 3 4-CN-Phenyl CF.sub.3 1311 3 4-CN-Phenyl —CH.sub.2CF.sub.3 1312 3 4-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1313 3 4-CN-Phenyl cyclopropyl 1314 3 4-CN-Phenyl Cyclobutyl 1315 3 4-CN-Phenyl cyclopentyl 1316 3 4-CN-Phenyl cyclohexyl 1317 3 4-CN-Phenyl 3-pyridyl 1318 3 4-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1319 3 4-CN-Phenyl 1H-imidazol-4-yl 1320 3 4-CN-Phenyl 2-furanyl 1321 3 2-CN-Phenyl Ethyl 1322 3 2-CN-Phenyl n-propyl 1323 3 2-CN-Phenyl Isopropyl 1324 3 2-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1325 3 2-CN-Phenyl CF.sub.3 1326 3 2-CN-Phenyl —CH.sub.2CF.sub.3 1327 3 2-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1328 3 2-CN-Phenyl cyclopropyl 1329 3 2-CN-Phenyl Cyclobutyl 1330 3 2-CN-Phenyl cyclopentyl 1331 3 2-CN-Phenyl cyclohexyl 1332 3 2-CN-Phenyl 3-pyridyl 1333 3 2-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1334 3 2-CN-Phenyl 1H-imidazol-4-yl 1335 3 2-CN-Phenyl 2-furanyl 1336 3 3-F-Phenyl Ethyl 1337 3 3-F-Phenyl n-propyl 1338 3 3-F-Phenyl Isopropyl 1339 3 3-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1340 3 3-F-Phenyl CF.sub.3 1341 3 3-F-Phenyl —CH.sub.2CF.sub.3 1342 3 3-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1343 3 3-F-Phenyl cyclopropyl 1344 3 3-F-Phenyl Cyclobutyl 1345 3 3-F-Phenyl cyclopentyl 1346 3 3-F-Phenyl cyclohexyl 1347 3 3-F-Phenyl 3-pyridyl 1348 3 3-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1349 3 3-F-Phenyl 1H-imidazol-4-yl 1350 3 3-F-Phenyl 2-furanyl 1351 3 2-Cl-Phenyl Ethyl 1352 3 2-Cl-Phenyl n-propyl 1353 3 2-Cl-Phenyl Isopropyl 1354 3 2-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1355 3 2-Cl-Phenyl CF.sub.3 1356 3 2-Cl-Phenyl —CH.sub.2CF.sub.3 1357 3 2-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1358 3 2-Cl-Phenyl cyclopropyl 1359 3 2-Cl-Phenyl Cyclobutyl 1360 3 2-Cl-Phenyl cyclopentyl 1361 3 2-Cl-Phenyl cyclohexyl 1362 3 2-Cl-Phenyl 3-pyridyl 1363 3 2-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1364 3 2-Cl-Phenyl 1H-imidazol-4-yl 1365 3 2-Cl-Phenyl 2-furanyl 1366 3 4-Cl-Phenyl Ethyl 1367 3 4-Cl-Phenyl n-propyl 1368 3 4-Cl-Phenyl Isopropyl 1369 3 4-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1370 3 4-Cl-Phenyl CF.sub.3 1371 3 4-Cl-Phenyl —CH.sub.2CF.sub.3 1372 3 4-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1373 3 4-Cl-Phenyl cyclopropyl 1374 3 4-Cl-Phenyl Cyclobutyl 1375 3 4-Cl-Phenyl cyclopentyl 1376 3 4-Cl-Phenyl cyclohexyl 1377 3 4-Cl-Phenyl 3-pyridyl 1378 3 4-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1379 3 4-Cl-Phenyl 1H-imidazol-4-yl 1380 3 4-Cl-Phenyl 2-furanyl 1381 3 3-Br-Phenyl Ethyl 1382 3 3-Br-Phenyl n-propyl 1383 3 3-Br-Phenyl Isopropyl 1384 3 3-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1385 3 3-Br-Phenyl CF.sub.3 1386 3 3-Br-Phenyl —CH.sub.2CF.sub.3 1387 3 3-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1388 3 3-Br-Phenyl cyclopropyl 1389 3 3-Br-Phenyl Cyclobutyl 1390 3 3-Br-Phenyl cyclopentyl 1391 3 3-Br-Phenyl cyclohexyl 1392 3 3-Br-Phenyl 3-pyridyl 1393 3 3-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1394 3 3-Br-Phenyl 1H-imidazol-4-yl 1395 3 3-Br-Phenyl 2-furanyl 1396 3 2-CF.sub.3-Phenyl Ethyl 1397 3 2-CF.sub.3-Phenyl n-propyl 1398 3 2-CF.sub.3-Phenyl Isopropyl 1399 3 2-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1400 3 2-CF.sub.3-Phenyl CF.sub.3 1401 3 2-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1402 3 2-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1403 3 2-CF.sub.3-Phenyl cyclopropyl 1404 3 2-CF.sub.3-Phenyl Cyclobutyl 1405 3 2-CF.sub.3-Phenyl cyclopentyl 1406 3 2-CF.sub.3-Phenyl cyclohexyl 1407 3 2-CF.sub.3-Phenyl 3-pyridyl 1408 3 2-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1409 3 2-CF.sub.3-Phenyl 1H-imidazol-4-yl 1410 3 2-CF.sub.3-Phenyl 2-furanyl 1411 3 4-CF.sub.3-Phenyl Ethyl 1412 3 4-CF.sub.3-Phenyl n-propyl 1413 3 4-CF.sub.3-Phenyl Isopropyl 1414 3 4-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1415 3 4-CF.sub.3-Phenyl CF.sub.3 1416 3 4-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1417 3 4-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1418 3 4-CF.sub.3-Phenyl cyclopropyl 1419 3 4-CF.sub.3-Phenyl Cyclobutyl 1420 3 4-CF.sub.3-Phenyl cyclopentyl 1421 3 4-CF.sub.3-Phenyl cyclohexyl 1422 3 4-CF.sub.3-Phenyl 3-pyridyl 1423 3 4-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1424 3 4-CF.sub.3-Phenyl 1H-imidazol-4-yl 1425 3 4-CF.sub.3-Phenyl 2-furanyl 1426 3 3-iPr-Phenyl Ethyl 1427 3 3-iPr-Phenyl n-propyl 1428 3 3-iPr-Phenyl Isopropyl 1429 3 3-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1430 3 3-iPr-Phenyl CF.sub.3 1431 3 3-iPr-Phenyl —CH.sub.2CF.sub.3 1432 3 3-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1433 3 3-iPr-Phenyl cyclopropyl 1434 3 3-iPr-Phenyl Cyclobutyl 1435 3 3-iPr-Phenyl cyclopentyl 1436 3 3-iPr-Phenyl cyclohexyl 1437 3 3-iPr-Phenyl 3-pyridyl 1438 3 3-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1439 3 3-iPr-Phenyl 1H-imidazol-4-yl 1440 3 3-iPr-Phenyl 2-furanyl 1441 3 2-morpholino-phenyl Ethyl 1442 3 2-morpholino-phenyl n-propyl 1443 3 2-morpholino-phenyl isopropyl 1444 3 2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1445 3 2-morpholino-phenyl CF.sub.3 1446 3 2-morpholino-phenyl —CH.sub.2CF.sub.3 1447 3 2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1448 3 2-morpholino-phenyl cyclopropyl 1449 3 2-morpholino-phenyl Cyclobutyl 1450 3 2-morpholino-phenyl cyclopentyl 1451 3 2-morpholino-phenyl cyclohexyl 1452 3 2-morpholino-phenyl 3-pyridyl 1453 3 2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1454 3 2-morpholino-phenyl 1H-imidazol-4-yl 1455 3 2-morpholino-phenyl 2-furanyl 1456 3 4-morpholino-phenyl ethyl 1457 3 4-morpholino-phenyl n-propyl 1458 3 4-morpholino-phenyl isopropyl 1459 3 4-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1460 3 4-morpholino-phenyl CF.sub.3 1461 3 4-morpholino-phenyl —CH.sub.2CF.sub.3 1462 3 4-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1463 3 4-morpholino-phenyl cyclopropyl 1464 3 4-morpholino-phenyl Cyclobutyl 1465 3 4-morpholino-phenyl cyclopentyl 1466 3 4-morpholino-phenyl cyclohexyl 1467 3 4-morpholino-phenyl 3-pyridyl 1468 3 4-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1469 3 4-morpholino-phenyl 1H-imidazol-4-yl 1470 3 4-morpholino-phenyl 2-furanyl 1471 3 4-methyl-2-morpholino-phenyl ethyl 1472 3 4-methyl-2-morpholino-phenyl n-propyl 1473 3 4-methyl-2-morpholino-phenyl isopropyl 1474 3 4-methyl-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1475 3 4-methyl-2-morpholino-phenyl CF.sub.3 1476 3 4-methyl-2-morpholino-phenyl —CH.sub.2CF.sub.3 1477 3 4-methyl-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1478 3 4-methyl-2-morpholino-phenyl cyclopropyl 1479 3 4-methyl-2-morpholino-phenyl Cyclobutyl 1480 3 4-methyl-2-morpholino-phenyl cyclopentyl 1481 3 4-methyl-2-morpholino-phenyl cyclohexyl 1482 3 4-methyl-2-morpholino-phenyl 3-pyridyl 1483 3 4-methyl-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1484 3 4-methyl-2-morpholino-phenyl 1H-imidazol-4-yl 1485 3 4-methyl-2-morpholino-phenyl 2-furanyl 1486 4 4-CH.sub.3-phenyl ethyl 1487 4 4-CH.sub.3-phenyl n-propyl 1488 4 4-CH.sub.3-phenyl isopropyl 1489 4 4-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1490 4 4-CH.sub.3-phenyl CF.sub.3 1491 4 4-CH.sub.3-phenyl —CH.sub.2CF.sub.3 1492 4 4-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 1493 4 4-CH.sub.3-phenyl cyclopropyl 1494 4 4-CH.sub.3-phenyl Cyclobutyl 1495 4 4-CH.sub.3-phenyl cyclopentyl 1496 4 4-CH.sub.3-phenyl cyclohexyl 1497 4 4-CH.sub.3-phenyl 3-pyridyl 1498 4 4-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1499 4 4-CH.sub.3-phenyl 1H-imidazol-4-yl 1500 4 4-CH.sub.3-phenyl 2-furanyl 1501 4 3-CH.sub.3-phenyl ethyl 1502 4 3-CH.sub.3-phenyl n-propyl 1503 4 3-CH.sub.3-phenyl isopropyl 1504 4 3-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1505 4 3-CH.sub.3-phenyl CF.sub.3 1506 4 3-CH.sub.3-phenyl —CH.sub.2CF.sub.3 1507 4 3-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 1508 4 3-CH.sub.3-phenyl cyclopropyl 1509 4 3-CH.sub.3-phenyl Cyclobutyl 1510 4 3-CH.sub.3-phenyl cyclopentyl 1511 4 3-CH.sub.3-phenyl cyclohexyl 1512 4 3-CH.sub.3-phenyl 3-pyridyl 1513 4 3-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1514 4 3-CH.sub.3-phenyl 1H-imidazol-4-yl 1515 4 3-CH.sub.3-phenyl 2-furanyl 1516 4 3-OH-Phenyl ethyl 1517 4 3-OH-Phenyl n-propyl 1518 4 3-OH-Phenyl isopropyl 1519 4 3-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1520 4 3-OH-Phenyl CF.sub.3 1521 4 3-OH-Phenyl —CH.sub.2CF.sub.3 1522 4 3-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1523 4 3-OH-Phenyl cyclopropyl 1524 4 3-OH-Phenyl Cyclobutyl 1525 4 3-OH-Phenyl cyclopentyl 1526 4 3-OH-Phenyl cyclohexyl 1527 4 3-OH-Phenyl 3-pyridyl 1528 4 3-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1529 4 3-OH-Phenyl 1H-imidazol-4-yl 1530 4 3-OH-Phenyl 2-furanyl 1531 4 4-OMe-Phenyl ethyl 1532 4 4-OMe-Phenyl n-propyl 1533 4 4-OMe-Phenyl isopropyl 1534 4 4-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1535 4 4-OMe-Phenyl CF.sub.3 1536 4 4-OMe-Phenyl —CH.sub.2CF.sub.3 1537 4 4-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1538 4 4-OMe-Phenyl cyclopropyl 1539 4 4-OMe-Phenyl Cyclobutyl 1540 4 4-OMe-Phenyl cyclopentyl 1541 4 4-OMe-Phenyl cyclohexyl 1542 4 4-OMe-Phenyl 3-pyridyl 1543 4 4-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1544 4 4-OMe-Phenyl 1H-imidazol-4-yl 1545 4 4-OMe-Phenyl 2-furanyl 1546 4 2-OMe-Phenyl ethyl 1547 4 2-OMe-Phenyl n-propyl 1548 4 2-OMe-Phenyl isopropyl 1549 4 2-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1550 4 2-OMe-Phenyl CF.sub.3 1551 4 2-OMe-Phenyl —CH.sub.2CF.sub.3 1552 4 2-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1553 4 2-OMe-Phenyl cyclopropyl 1554 4 2-OMe-Phenyl Cyclobutyl 1555 4 2-OMe-Phenyl cyclopentyl 1556 4 2-OMe-Phenyl cyclohexyl 1557 4 2-OMe-Phenyl 3-pyridyl 1558 4 2-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1559 4 2-OMe-Phenyl 1H-imidazol-4-yl 1560 4 2-OMe-Phenyl 2-furanyl 1561 4 3-CN-Phenyl ethyl 1562 4 3-CN-Phenyl n-propyl 1563 4 3-CN-Phenyl isopropyl 1564 4 3-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1565 4 3-CN-Phenyl CF.sub.3 1566 4 3-CN-Phenyl —CH.sub.2CF.sub.3 1567 4 3-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1568 4 3-CN-Phenyl cyclopropyl 1569 4 3-CN-Phenyl Cyclobutyl 1570 4 3-CN-Phenyl cyclopentyl 1571 4 3-CN-Phenyl cyclohexyl 1572 4 3-CN-Phenyl 3-pyridyl 1573 4 3-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1574 4 3-CN-Phenyl 1H-imidazol-4-yl 1575 4 3-CN-Phenyl 2-furanyl 1576 4 2-F-Phenyl ethyl 1577 4 2-F-Phenyl n-propyl 1578 4 2-F-Phenyl isopropyl 1579 4 2-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1580 4 2-F-Phenyl CF.sub.3 1581 4 2-F-Phenyl —CH.sub.2CF.sub.3 1582 4 2-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1583 4 2-F-Phenyl cyclopropyl 1584 4 2-F-Phenyl Cyclobutyl 1585 4 2-F-Phenyl cyclopentyl 1586 4 2-F-Phenyl cyclohexyl 1587 4 2-F-Phenyl 3-pyridyl 1588 4 2-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1589 4 2-F-Phenyl 1H-imidazol-4-yl 1590 4 2-F-Phenyl 2-furanyl 1591 4 4-F-Phenyl ethyl 1592 4 4-F-Phenyl n-propyl 1593 4 4-F-Phenyl isopropyl 1594 4 4-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1595 4 4-F-Phenyl CF.sub.3 1596 4 4-F-Phenyl —CH.sub.2CF.sub.3 1597 4 4-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1598 4 4-F-Phenyl cyclopropyl 1599 4 4-F-Phenyl Cyclobutyl 1600 4 4-F-Phenyl cyclopentyl 1601 4 4-F-Phenyl cyclohexyl 1602 4 4-F-Phenyl 3-pyridyl 1603 4 4-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1604 4 4-F-Phenyl 1H-imidazol-4-yl 1605 4 4-F-Phenyl 2-furanyl 1606 4 3-Cl-Phenyl ethyl 1607 4 3-Cl-Phenyl n-propyl 1608 4 3-Cl-Phenyl isopropyl 1609 4 3-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1610 4 3-Cl-Phenyl CF.sub.3 1611 4 3-Cl-Phenyl —CH.sub.2CF.sub.3 1612 4 3-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1613 4 3-Cl-Phenyl cyclopropyl 1614 4 3-Cl-Phenyl Cyclobutyl 1615 4 3-Cl-Phenyl cyclopentyl 1616 4 3-Cl-Phenyl cyclohexyl 1617 4 3-Cl-Phenyl 3-pyridyl 1618 4 3-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1619 4 3-Cl-Phenyl 1H-imidazol-4-yl 1620 4 3-Cl-Phenyl 2-furanyl 1621 4 2-Br-Phenyl ethyl 1622 4 2-Br-Phenyl n-propyl 1623 4 2-Br-Phenyl isopropyl 1624 4 2-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1625 4 2-Br-Phenyl CF.sub.3 1626 4 2-Br-Phenyl —CH.sub.2CF.sub.3 1627 4 2-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1628 4 2-Br-Phenyl cyclopropyl 1629 4 2-Br-Phenyl Cyclobutyl 1630 4 2-Br-Phenyl cyclopentyl 1631 4 2-Br-Phenyl cyclohexyl 1632 4 2-Br-Phenyl 3-pyridyl 1633 4 2-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1634 4 2-Br-Phenyl 1H-imidazol-4-yl 1635 4 2-Br-Phenyl 2-furanyl 1636 4 4-Br-Phenyl ethyl 1637 4 4-Br-Phenyl n-propyl 1638 4 4-Br-Phenyl isopropyl 1639 4 4-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1640 4 4-Br-Phenyl CF.sub.3 1641 4 4-Br-Phenyl —CH.sub.2CF.sub.3 1642 4 4-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1643 4 4-Br-Phenyl cyclopropyl 1644 4 4-Br-Phenyl Cyclobutyl 1645 4 4-Br-Phenyl cyclopentyl 1646 4 4-Br-Phenyl cyclohexyl 1647 4 4-Br-Phenyl 3-pyridyl 1648 4 4-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1649 4 4-Br-Phenyl 1H-imidazol-4-yl 1650 4 4-Br-Phenyl 2-furanyl 1651 4 3-CF.sub.3-Phenyl ethyl 1652 4 3-CF.sub.3-Phenyl n-propyl 1653 4 3-CF.sub.3-Phenyl isopropyl 1654 4 3-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1655 4 3-CF.sub.3-Phenyl CF.sub.3 1656 4 3-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1657 4 3-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1658 4 3-CF.sub.3-Phenyl cyclopropyl 1659 4 3-CF.sub.3-Phenyl Cyclobutyl 1660 4 3-CF.sub.3-Phenyl cyclopentyl 1661 4 3-CF.sub.3-Phenyl cyclohexyl 1662 4 3-CF.sub.3-Phenyl 3-pyridyl 1663 4 3-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1664 4 3-CF.sub.3-Phenyl 1H-imidazol-4-yl 1665 4 3-CF.sub.3-Phenyl 2-furanyl 1666 4 2-iPr-Phenyl ethyl 1667 4 2-iPr-Phenyl n-propyl 1668 4 2-iPr-Phenyl isopropyl 1669 4 2-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1670 4 2-iPr-Phenyl CF.sub.3 1671 4 2-iPr-Phenyl —CH.sub.2CF.sub.3 1672 4 2-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1673 4 2-iPr-Phenyl cyclopropyl 1674 4 2-iPr-Phenyl Cyclobutyl 1675 4 2-iPr-Phenyl cyclopentyl 1676 4 2-iPr-Phenyl cyclohexyl 1677 4 2-iPr-Phenyl 3-pyridyl 1678 4 2-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1679 4 2-iPr-Phenyl 1H-imidazol-4-yl 1680 4 2-iPr-Phenyl 2-furanyl 1681 4 4-iPr-Phenyl ethyl 1682 4 4-iPr-Phenyl n-propyl 1683 4 4-iPr-Phenyl isopropyl 1684 4 4-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1685 4 4-iPr-Phenyl CF.sub.3 1686 4 4-iPr-Phenyl —CH.sub.2CF.sub.3 1687 4 4-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1688 4 4-iPr-Phenyl cyclopropyl 1689 4 4-iPr-Phenyl Cyclobutyl 1690 4 4-iPr-Phenyl cyclopentyl 1691 4 4-iPr-Phenyl cyclohexyl 1692 4 4-iPr-Phenyl 3-pyridyl 1693 4 4-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1694 4 4-iPr-Phenyl 1H-imidazol-4-yl 1695 4 4-iPr-Phenyl 2-furanyl 1696 4 3-morpholino-phenyl ethyl 1697 4 3-morpholino-phenyl n-propyl 1698 4 3-morpholino-phenyl isopropyl 1699 4 3-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1700 4 3-morpholino-phenyl CF.sub.3 1701 4 3-morpholino-phenyl —CH.sub.2CF.sub.3 1702 4 3-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1703 4 3-morpholino-phenyl cyclopropyl 1704 4 3-morpholino-phenyl Cyclobutyl 1705 4 3-morpholino-phenyl cyclopentyl 1706 4 3-morpholino-phenyl cyclohexyl 1707 4 3-morpholino-phenyl 3-pyridyl 1708 4 3-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1709 4 3-morpholino-phenyl 1H-imidazol-4-yl 1710 4 3-morpholino-phenyl 2-furanyl 1711 4 4-cyano-2-morpholino-phenyl ethyl 1712 4 4-cyano-2-morpholino-phenyl n-propyl 1713 4 4-cyano-2-morpholino-phenyl isopropyl 1714 4 4-cyano-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1715 4 4-cyano-2-morpholino-phenyl CF.sub.3 1716 4 4-cyano-2-morpholino-phenyl —CH.sub.2CF.sub.3 1717 4 4-cyano-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1718 4 4-cyano-2-morpholino-phenyl cyclopropyl 1719 4 4-cyano-2-morpholino-phenyl Cyclobutyl 1720 4 4-cyano-2-morpholino-phenyl cyclopentyl 1721 4 4-cyano-2-morpholino-phenyl cyclohexyl 1722 4 4-cyano-2-morpholino-phenyl 3-pyridyl 1723 4 4-cyano-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1724 4 4-cyano-2-morpholino-phenyl 1H-imidazol-4-yl 1725 4 4-cyano-2-morpholino-phenyl 2-furanyl 1726 4 4-hydroxy-2-morpholino-phenyl ethyl 1727 4 4-hydroxy-2-morpholino-phenyl n-propyl 1728 4 4-hydroxy-2-morpholino-phenyl isopropyl 1729 4 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1730 4 4-hydroxy-2-morpholino-phenyl CF.sub.3 1731 4 4-hydroxy-2-morpholino-phenyl —CH.sub.2CF.sub.3 1732 4 4-hydroxy-2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1733 4 4-hydroxy-2-morpholino-phenyl cyclopropyl 1734 4 4-hydroxy-2-morpholino-phenyl Cyclobutyl 1735 4 4-hydroxy-2-morpholino-phenyl cyclopentyl 1736 4 4-hydroxy-2-morpholino-phenyl cyclohexyl 1737 4 4-hydroxy-2-morpholino-phenyl 3-pyridyl 1738 4 4-hydroxy-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1739 4 4-hydroxy-2-morpholino-phenyl 1H-imidazol-4-yl 1740 4 4-hydroxy-2-morpholino-phenyl 2-furanyl 1741 4 2-CH.sub.3-phenyl Ethyl 1742 4 2-CH.sub.3-phenyl n-propyl 1743 4 2-CH.sub.3-phenyl Isopropyl 1744 4 2-CH.sub.3-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1745 4 2-CH.sub.3-phenyl CF.sub.3 1746 4 2-CH.sub.3-phenyl —CH.sub.2CF.sub.3 1747 4 2-CH.sub.3-phenyl —CH.sub.2CH.sub.2CF.sub.3 1748 4 2-CH.sub.3-phenyl cyclopropyl 1749 4 2-CH.sub.3-phenyl Cyclobutyl 1750 4 2-CH.sub.3-phenyl cyclopentyl 1751 4 2-CH.sub.3-phenyl cyclohexyl 1752 4 2-CH.sub.3-phenyl 3-pyridyl 1753 4 2-CH.sub.3-phenyl 1-methyl-1H-pyrazol-4-yl 1754 4 2-CH.sub.3-phenyl 1H-imidazol-4-yl 1755 4 2-CH.sub.3-phenyl 2-furanyl 1756 4 4-OH-Phenyl Ethyl 1757 4 4-OH-Phenyl n-propyl 1758 4 4-OH-Phenyl Isopropyl 1759 4 4-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1760 4 4-OH-Phenyl CF.sub.3 1761 4 4-OH-Phenyl —CH.sub.2CF.sub.3 1762 4 4-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1763 4 4-OH-Phenyl cyclopropyl 1764 4 4-OH-Phenyl Cyclobutyl 1765 4 4-OH-Phenyl cyclopentyl 1766 4 4-OH-Phenyl cyclohexyl 1767 4 4-OH-Phenyl 3-pyridyl 1768 4 4-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1769 4 4-OH-Phenyl 1H-imidazol-4-yl 1770 4 4-OH-Phenyl 2-furanyl 1771 4 2-OH-Phenyl Ethyl 1772 4 2-OH-Phenyl n-propyl 1773 4 2-OH-Phenyl Isopropyl 1774 4 2-OH-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1775 4 2-OH-Phenyl CF.sub.3 1776 4 2-OH-Phenyl —CH.sub.2CF.sub.3 1777 4 2-OH-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1778 4 2-OH-Phenyl cyclopropyl 1779 4 2-OH-Phenyl Cyclobutyl 1780 4 2-OH-Phenyl cyclopentyl 1781 4 2-OH-Phenyl cyclohexyl 1782 4 2-OH-Phenyl 3-pyridyl 1783 4 2-OH-Phenyl 1-methyl-1H-pyrazol-4-yl 1784 4 2-OH-Phenyl 1H-imidazol-4-yl 1785 4 2-OH-Phenyl 2-furanyl 1786 4 3-OMe-Phenyl Ethyl 1787 4 3-OMe-Phenyl n-propyl 1788 4 3-OMe-Phenyl Isopropyl 1789 4 3-OMe-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1790 4 3-OMe-Phenyl CF.sub.3 1791 4 3-OMe-Phenyl —CH.sub.2CF.sub.3 1792 4 3-OMe-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1793 4 3-OMe-Phenyl cyclopropyl 1794 4 3-OMe-Phenyl Cyclobutyl 1795 4 3-OMe-Phenyl cyclopentyl 1796 4 3-OMe-Phenyl cyclohexyl 1797 4 3-OMe-Phenyl 3-pyridyl 1798 4 3-OMe-Phenyl 1-methyl-1H-pyrazol-4-yl 1799 4 3-OMe-Phenyl 1H-imidazol-4-yl 1800 4 3-OMe-Phenyl 2-furanyl 1801 4 4-CN-Phenyl Ethyl 1802 4 4-CN-Phenyl n-propyl 1803 4 4-CN-Phenyl Isopropyl 1804 4 4-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1805 4 4-CN-Phenyl CF.sub.3 1806 4 4-CN-Phenyl —CH.sub.2CF.sub.3 1807 4 4-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1808 4 4-CN-Phenyl cyclopropyl 1809 4 4-CN-Phenyl Cyclobutyl 1810 4 4-CN-Phenyl cyclopentyl 1811 4 4-CN-Phenyl cyclohexyl 1812 4 4-CN-Phenyl 3-pyridyl 1813 4 4-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1814 4 4-CN-Phenyl 1H-imidazol-4-yl 1815 4 4-CN-Phenyl 2-furanyl 1816 4 2-CN-Phenyl Ethyl 1817 4 2-CN-Phenyl n-propyl 1818 4 2-CN-Phenyl Isopropyl 1819 4 2-CN-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1820 4 2-CN-Phenyl CF.sub.3 1821 4 2-CN-Phenyl —CH.sub.2CF.sub.3 1822 4 2-CN-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1823 4 2-CN-Phenyl cyclopropyl 1824 4 2-CN-Phenyl Cyclobutyl 1825 4 2-CN-Phenyl cyclopentyl 1826 4 2-CN-Phenyl cyclohexyl 1827 4 2-CN-Phenyl 3-pyridyl 1828 4 2-CN-Phenyl 1-methyl-1H-pyrazol-4-yl 1829 4 2-CN-Phenyl 1H-imidazol-4-yl 1830 4 2-CN-Phenyl 2-furanyl 1831 4 3-F-Phenyl Ethyl 1832 4 3-F-Phenyl n-propyl 1833 4 3-F-Phenyl Isopropyl 1834 4 3-F-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1835 4 3-F-Phenyl CF.sub.3 1836 4 3-F-Phenyl —CH.sub.2CF.sub.3 1837 4 3-F-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1838 4 3-F-Phenyl cyclopropyl 1839 4 3-F-Phenyl Cyclobutyl 1840 4 3-F-Phenyl cyclopentyl 1841 4 3-F-Phenyl cyclohexyl 1842 4 3-F-Phenyl 3-pyridyl 1843 4 3-F-Phenyl 1-methyl-1H-pyrazol-4-yl 1844 4 3-F-Phenyl 1H-imidazol-4-yl 1845 4 3-F-Phenyl 2-furanyl 1846 4 2-Cl-Phenyl Ethyl 1847 4 2-Cl-Phenyl n-propyl 1848 4 2-Cl-Phenyl Isopropyl 1849 4 2-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1850 4 2-Cl-Phenyl CF.sub.3 1851 4 2-Cl-Phenyl —CH2CF.sub.3 1852 4 2-Cl-Phenyl —CH2CH.sub.2CF.sub.3 1853 4 2-Cl-Phenyl cyclopropyl 1854 4 2-Cl-Phenyl Cyclobutyl 1855 4 2-Cl-Phenyl cyclopentyl 1856 4 2-Cl-Phenyl cyclohexyl 1857 4 2-Cl-Phenyl 3-pyridyl 1858 4 2-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1859 4 2-Cl-Phenyl 1H-imidazol-4-yl 1860 4 2-Cl-Phenyl 2-furanyl 1861 4 4-Cl-Phenyl Ethyl 1862 4 4-Cl-Phenyl n-propyl 1863 4 4-Cl-Phenyl Isopropyl 1864 4 4-Cl-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1865 4 4-Cl-Phenyl CF.sub.3 1866 4 4-Cl-Phenyl —CH.sub.2CF.sub.3 1867 4 4-Cl-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1868 4 4-Cl-Phenyl cyclopropyl 1869 4 4-Cl-Phenyl Cyclobutyl 1870 4 4-Cl-Phenyl cyclopentyl 1871 4 4-Cl-Phenyl cyclohexyl 1872 4 4-Cl-Phenyl 3-pyridyl 1873 4 4-Cl-Phenyl 1-methyl-1H-pyrazol-4-yl 1874 4 4-Cl-Phenyl 1H-imidazol-4-yl 1875 4 4-Cl-Phenyl 2-furanyl 1876 4 3-Br-Phenyl Ethyl 1877 4 3-Br-Phenyl n-propyl 1878 4 3-Br-Phenyl Isopropyl 1879 4 3-Br-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1880 4 3-Br-Phenyl CF.sub.3 1881 4 3-Br-Phenyl —CH.sub.2CF.sub.3 1882 4 3-Br-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1883 4 3-Br-Phenyl cyclopropyl 1884 4 3-Br-Phenyl Cyclobutyl 1885 4 3-Br-Phenyl cyclopentyl 1886 4 3-Br-Phenyl cyclohexyl 1887 4 3-Br-Phenyl 3-pyridyl 1888 4 3-Br-Phenyl 1-methyl-1H-pyrazol-4-yl 1889 4 3-Br-Phenyl 1H-imidazol-4-yl 1890 4 3-Br-Phenyl 2-furanyl 1891 4 2-CF.sub.3-Phenyl Ethyl 1892 4 2-CF.sub.3-Phenyl n-propyl 1893 4 2-CF.sub.3-Phenyl Isopropyl 1894 4 2-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1895 4 2-CF.sub.3-Phenyl CF.sub.3 1896 4 2-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1897 4 2-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1898 4 2-CF.sub.3-Phenyl cyclopropyl 1899 4 2-CF.sub.3-Phenyl Cyclobutyl 1900 4 2-CF.sub.3-Phenyl cyclopentyl 1901 4 2-CF.sub.3-Phenyl cyclohexyl 1902 4 2-CF.sub.3-Phenyl 3-pyridyl 1903 4 2-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1904 4 2-CF.sub.3-Phenyl 1H-imidazol-4-yl 1905 4 2-CF.sub.3-Phenyl 2-furanyl 1906 4 4-CF.sub.3-Phenyl Ethyl 1907 4 4-CF.sub.3-Phenyl n-propyl 1908 4 4-CF.sub.3-Phenyl Isopropyl 1909 4 4-CF.sub.3-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1910 4 4-CF.sub.3-Phenyl CF.sub.3 1911 4 4-CF.sub.3-Phenyl —CH.sub.2CF.sub.3 1912 4 4-CF.sub.3-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1913 4 4-CF.sub.3-Phenyl cyclopropyl 1914 4 4-CF.sub.3-Phenyl Cyclobutyl 1915 4 4-CF.sub.3-Phenyl cyclopentyl 1916 4 4-CF.sub.3-Phenyl cyclohexyl 1917 4 4-CF.sub.3-Phenyl 3-pyridyl 1918 4 4-CF.sub.3-Phenyl 1-methyl-1H-pyrazol-4-yl 1919 4 4-CF.sub.3-Phenyl 1H-imidazol-4-yl 1920 4 4-CF.sub.3-Phenyl 2-furanyl 1921 4 3-iPr-Phenyl Ethyl 1922 4 3-iPr-Phenyl n-propyl 1923 4 3-iPr-Phenyl Isopropyl 1924 4 3-iPr-Phenyl —CH.sub.2CH(CH.sub.3).sub.2 1925 4 3-iPr-Phenyl CF.sub.3 1926 4 3-iPr-Phenyl —CH.sub.2CF.sub.3 1927 4 3-iPr-Phenyl —CH.sub.2CH.sub.2CF.sub.3 1928 4 3-iPr-Phenyl cyclopropyl 1929 4 3-iPr-Phenyl Cyclobutyl 1930 4 3-iPr-Phenyl cyclopentyl 1931 4 3-iPr-Phenyl cyclohexyl 1932 4 3-iPr-Phenyl 3-pyridyl 1933 4 3-iPr-Phenyl 1-methyl-1H-pyrazol-4-yl 1934 4 3-iPr-Phenyl 1H-imidazol-4-yl 1935 4 3-iPr-Phenyl 2-furanyl 1936 4 2-morpholino-phenyl Ethyl 1937 4 2-morpholino-phenyl n-propyl 1938 4 2-morpholino-phenyl isopropyl 1939 4 2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1940 4 2-morpholino-phenyl CF.sub.3 1941 4 2-morpholino-phenyl —CH.sub.2CF.sub.3 1942 4 2-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1943 4 2-morpholino-phenyl cyclopropyl 1944 4 2-morpholino-phenyl Cyclobutyl 1945 4 2-morpholino-phenyl cyclopentyl 1946 4 2-morpholino-phenyl cyclohexyl 1947 4 2-morpholino-phenyl 3-pyridyl 1948 4 2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1949 4 2-morpholino-phenyl 1H-imidazol-4-yl 1950 4 2-morpholino-phenyl 2-furanyl 1951 4 4-morpholino-phenyl ethyl 1952 4 4-morpholino-phenyl n-propyl 1953 4 4-morpholino-phenyl isopropyl 1954 4 4-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1955 4 4-morpholino-phenyl CF.sub.3 1956 4 4-morpholino-phenyl —CH.sub.2CF.sub.3 1957 4 4-morpholino-phenyl —CH.sub.2CH.sub.2CF.sub.3 1958 4 4-morpholino-phenyl cyclopropyl 1959 4 4-morpholino-phenyl Cyclobutyl 1960 4 4-morpholino-phenyl cyclopentyl 1961 4 4-morpholino-phenyl cyclohexyl 1962 4 4-morpholino-phenyl 3-pyridyl 1963 4 4-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1964 4 4-morpholino-phenyl 1H-imidazol-4-yl 1965 4 4-morpholino-phenyl 2-furanyl 1966 4 4-methyl-2-morpholino-phenyl ethyl 1967 4 4-methyl-2-morpholino-phenyl n-propyl 1968 4 4-methyl-2-morpholino-phenyl isopropyl 1969 4 4-methyl-2-morpholino-phenyl —CH.sub.2CH(CH.sub.3).sub.2 1970 4 4-methyl-2-morpholino-phenyl CF.sub.3 1971 4 4-methyl-2-morpholino-phenyl —CH2CF3 1972 4 4-methyl-2-morpholino-phenyl —CH2CH2CF3 1973 4 4-methyl-2-morpholino-phenyl Cyclopropyl 1974 4 4-methyl-2-morpholino-phenyl Cyclobutyl 1975 4 4-methyl-2-morpholino-phenyl Cyclopentyl 1976 4 4-methyl-2-morpholino-phenyl Cyclohexyl 1977 4 4-methyl-2-morpholino-phenyl 3-pyridyl 1978 4 4-methyl-2-morpholino-phenyl 1-methyl-1H-pyrazol-4-yl 1979 4 4-methyl-2-morpholino-phenyl 1H-imidazol-4-yl 1980 4 4-methyl-2-morpholino-phenyl 2-furanyl 1981 1 naphthylen-1-yl Ethyl 1982 1 naphthylen-1-yl n-propyl 1983 1 naphthylen-1-yl Isopropyl 1984 1 naphthylen-1-yl —CH.sub.2CH(CH.sub.3).sub.2 1985 1 naphthylen-1-yl CF.sub.3 1986 1 naphthylen-1-yl —CH.sub.2CF.sub.3 1987 1 naphthylen-1-yl —CH.sub.2CH.sub.2CF.sub.3 1988 1 naphthylen-1-yl Cyclopropyl 1989 1 naphthylen-1-yl Cyclobutyl 1990 1 naphthylen-1-yl Cyclopentyl 1991 1 naphthylen-1-yl Cyclohexyl 1992 1 naphthylen-1-yl 3-pyridyl 1993 1 naphthylen-1-yl 1-methyl-1H-pyrazol-4-yl 1994 1 naphthylen-1-yl 1H-imidazol-4-yl 1995 1 naphthylen-1-yl 2-furanyl 1996 1 naphthylen-2-yl Ethyl 1997 1 naphthylen-2-yl n-propyl 1998 1 naphthylen-2-yl Isopropyl 1999 1 naphthylen-2-yl —CH.sub.2CH(CH.sub.3).sub.2 2000 1 naphthylen-2-yl CF.sub.3 2001 1 naphthylen-2-yl —CH.sub.2CF.sub.3 2002 1 naphthylen-2-yl —CH.sub.2CH.sub.2CF.sub.3 2003 1 naphthylen-2-yl Cyclopropyl 2004 1 naphthylen-2-yl Cyclobutyl 2005 1 naphthylen-2-yl Cyclopentyl 2006 1 naphthylen-2-yl Cyclohexyl 2007 1 naphthylen-2-yl 3-pyridyl 2008 1 naphthylen-2-yl 1-methyl-1H-pyrazol-4-yl 2009 1 naphthylen-2-yl 1H-imidazol-4-yl 2010 1 naphthylen-2-yl 2-furanyl 2011 2 naphthylen-1-yl Ethyl 2012 2 naphthylen-1-yl n-propyl 2013 2 naphthylen-1-yl Isopropyl 2014 2 naphthylen-1-yl —CH.sub.2CH(CH.sub.3).sub.2 2015 2 naphthylen-1-yl CF.sub.3 2016 2 naphthylen-1-yl —CH.sub.2CF.sub.3 2017 2 naphthylen-1-yl —CH.sub.2CH.sub.2CF.sub.3 2018 2 naphthylen-1-yl Cyclopropyl 2019 2 naphthylen-1-yl Cyclobutyl 2020 2 naphthylen-1-yl Cyclopentyl 2021 2 naphthylen-1-yl Cyclohexyl 2022 2 naphthylen-1-yl 3-pyridyl 2023 2 naphthylen-1-yl 1-methyl-1H-pyrazol-4-yl 2024 2 naphthylen-1-yl 1H-imidazol-4-yl 2025 2 naphthylen-1-yl 2-furanyl 2026 2 naphthylen-2-yl Ethyl 2027 2 naphthylen-2-yl n-propyl 2028 2 naphthylen-2-yl Isopropyl 2029 2 naphthylen-2-yl —CH.sub.2CH(CH.sub.3).sub.2 2030 2 naphthylen-2-yl CF.sub.3 2031 2 naphthylen-2-yl —CH.sub.2CF.sub.3 2032 2 naphthylen-2-yl —CH.sub.2CH.sub.2CF.sub.3 2033 2 naphthylen-2-yl Cyclopropyl 2034 2 naphthylen-2-yl Cyclobutyl 2035 2 naphthylen-2-yl Cyclopentyl 2036 2 naphthylen-2-yl Cyclohexyl 2037 2 naphthylen-2-yl 3-pyridyl 2038 2 naphthylen-2-yl 1-methyl-1H-pyrazol-4-yl 2039 2 naphthylen-2-yl 1H-imidazol-4-yl 2040 2 naphthylen-2-yl 2-furanyl 2041 3 naphthylen-1-yl Ethyl 2042 3 naphthylen-1-yl n-propyl 2043 3 naphthylen-1-yl Isopropyl 2044 3 naphthylen-1-yl —CH.sub.2CH(CH.sub.3).sub.2 2045 3 naphthylen-1-yl CF.sub.3 2046 3 naphthylen-1-yl —CH.sub.2CF.sub.3 2047 3 naphthylen-1-yl —CH.sub.2CH.sub.2CF.sub.3 2048 3 naphthylen-1-yl Cyclopropyl 2049 3 naphthylen-1-yl Cyclobutyl 2050 3 naphthylen-1-yl Cyclopentyl 2051 3 naphthylen-1-yl Cyclohexyl 2052 3 naphthylen-1-yl 3-pyridyl 2053 3 naphthylen-1-yl 1-methyl-1H-pyrazol-4-yl 2054 3 naphthylen-1-yl 1H-imidazol-4-yl 2055 3 naphthylen-1-yl 2-furanyl 2056 3 naphthylen-2-yl Ethyl 2057 3 naphthylen-2-yl n-propyl 2058 3 naphthylen-2-yl Isopropyl 2059 3 naphthylen-2-yl —CH.sub.2CH(CH.sub.3).sub.2 2060 3 naphthylen-2-yl CF.sub.3 2061 3 naphthylen-2-yl —CH.sub.2CF.sub.3 2062 3 naphthylen-2-yl —CH.sub.2CH.sub.2CF.sub.3 2063 3 naphthylen-2-yl Cyclopropyl 2064 3 naphthylen-2-yl Cyclobutyl 2065 3 naphthylen-2-yl Cyclopentyl 2066 3 naphthylen-2-yl Cyclohexyl 2067 3 naphthylen-2-yl 3-pyridyl 2068 3 naphthylen-2-yl 1-methyl-1H-pyrazol-4-yl 2069 3 naphthylen-2-yl 1H-imidazol-4-yl 2070 3 naphthylen-2-yl 2-furanyl 2071 4 naphthylen-1-yl Ethyl 2072 4 naphthylen-1-yl n-propyl 2073 4 naphthylen-1-yl Isopropyl 2074 4 naphthylen-1-yl —CH.sub.2CH(CH.sub.3).sub.2 2075 4 naphthylen-1-yl CF.sub.3 2076 4 naphthylen-1-yl —CH.sub.2CF.sub.3 2077 4 naphthylen-1-yl —CH.sub.2CH.sub.2CF.sub.3 2078 4 naphthylen-1-yl Cyclopropyl 2079 4 naphthylen-1-yl Cyclobutyl 2080 4 naphthylen-1-yl Cyclopentyl 2081 4 naphthylen-1-yl Cyclohexyl 2082 4 naphthylen-1-yl 3-pyridyl 2083 4 naphthylen-1-yl 1-methyl-1H-pyrazol-4-yl 2084 4 naphthylen-1-yl 1H-imidazol-4-yl 2085 4 naphthylen-1-yl 2-furanyl 2086 4 naphthylen-2-yl Ethyl 2087 4 naphthylen-2-yl n-propyl 2088 4 naphthylen-2-yl Isopropyl 2089 4 naphthylen-2-yl —CH.sub.2CH(CH.sub.3).sub.2 2090 4 naphthylen-2-yl CF.sub.3 2091 4 naphthylen-2-yl —CH.sub.2CF.sub.3 2092 4 naphthylen-2-yl —CH.sub.2CH.sub.2CF.sub.3 2093 4 naphthylen-2-yl Cyclopropyl 2094 4 naphthylen-2-yl Cyclobutyl 2095 4 naphthylen-2-yl Cyclopentyl 2096 4 naphthylen-2-yl Cyclohexyl 2097 4 naphthylen-2-yl 3-pyridyl 2098 4 naphthylen-2-yl 1-methyl-1H-pyrazol-4-yl 2099 4 naphthylen-2-yl 1H-imidazol-4-yl 2100 4 naphthylen-2-yl 2-furanyl

    [2060] For the purposes of demonstrating the manner in which the compounds of the present invention are named and referred to herein, the compound having the formula:

    ##STR00455##

    [2061] has the chemical name 8-(methylsulfonyl)-3-(2-(4-phenylpiperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one.

    [2062] For the purposes of demonstrating the manner in which the compounds of the present invention are named and referred to herein, the compound having the formula:

    ##STR00456##

    [2063] has the chemical name 8-(methylsulfonyl)-3-(2-(5-phenylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one.

    [2064] For the purposes of demonstrating the manner in which the compounds of the present invention are named and referred to herein, the compound having the formula:

    ##STR00457##

    [2065] has the chemical name 8-(methylsulfonyl)-3-(2-(4-phenylpiperidin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one

    [2066] For the purposes of the present invention, a compound depicted by the racemic formula, for example:

    ##STR00458##

    [2067] will stand equally well for either of the two enantiomers having the formula:

    ##STR00459##

    [2068] or the formula:

    ##STR00460##

    [2069] or mixtures thereof, or in the case where a second chiral center is present, all diastereomers.

    [2070] In all of the embodiments provided herein, examples of suitable optional substituents are not intended to limit the scope of the claimed invention. The compounds of the invention may contain any of the substituents, or combinations of substituents, provided herein.

    [2071] Process for preparing the 5-hydroxytryptamine receptor 7 activity modulators of the invention

    [2072] The present invention further relates to a process for preparing the 5-hydroxytryptamine receptor 7 activity modulators of the present invention.

    [2073] Compounds of the present teachings can be prepared in accordance with the procedures outlined herein, from commercially available starting materials, compounds known in the literature, or readily prepared intermediates, by employing standard synthetic methods and procedures known to those skilled in the art. Standard synthetic methods and procedures for the preparation of organic molecules and functional group transformations and manipulations can be readily obtained from the relevant scientific literature or from standard textbooks in the field. It will be appreciated that where typical or preferred process conditions (i.e., reaction temperatures, times, mole ratios of reactants, solvents, pressures, etc.) are given, other process conditions can also be used unless otherwise stated. Optimum reaction conditions can vary with the particular reactants or solvent used, but such conditions can be determined by one skilled in the art by routine optimization procedures. Those skilled in the art of organic synthesis will recognize that the nature and order of the synthetic steps presented can be varied for the purpose of optimizing the formation of the compounds described herein.

    [2074] The processes described herein can be monitored according to any suitable method known in the art. For example, product formation can be monitored by spectroscopic means, such as nuclear magnetic resonance spectroscopy (e.g., .sup.1H or .sup.13C), infrared spectroscopy, spectrophotometry (e.g., UV-visible), mass spectrometry, or by chromatography such as high pressure liquid chromatograpy (HPLC), gas chromatography (GC), gel-permeation chromatography (GPC), or thin layer chromatography (TLC).

    [2075] Preparation of the compounds can involve protection and deprotection of various chemical groups. The need for protection and deprotection and the selection of appropriate protecting groups can be readily determined by one skilled in the art. The chemistry of protecting groups can be found, for example, in Greene et al., Protective Groups in Organic Synthesis, 2d. Ed. (Wiley & Sons, 1991), the entire disclosure of which is incorporated by reference herein for all purposes.

    [2076] The reactions or the processes described herein can be carried out in suitable solvents which can be readily selected by one skilled in the art of organic synthesis. Suitable solvents typically are substantially nonreactive with the reactants, intermediates, and/or products at the temperatures at which the reactions are carried out, i.e., temperatures that can range from the solvent's freezing temperature to the solvent's boiling temperature. A given reaction can be carried out in one solvent or a mixture of more than one solvent. Depending on the particular reaction step, suitable solvents for a particular reaction step can be selected.

    [2077] The compounds of these teachings can be prepared by methods known in the art of organic chemistry. The reagents used in the preparation of the compounds of these teachings can be either commercially obtained or can be prepared by standard procedures described in the literature. For example, compounds of the present invention can be prepared according to the method illustrated in the General Synthetic Schemes:

    General Synthetic Schemes for Preparation of Compounds

    [2078] The reagents used in the preparation of the compounds of this invention can be either commercially obtained or can be prepared by standard procedures described in the literature. In accordance with this invention, compounds in the genus may be produced by one of the following reaction schemes. Accordingly, the invention further features any of the synthetic intermediates or processes as described herein.

    [2079] Compounds of the disclosure may be prepared according to the process outlined in Scheme 1—

    ##STR00461##

    [2080] A suitably substituted compound of formula (1), a known compound or a compound prepared by known methods wherein PG is a protecting selected from the group consisting of benzyl, tert-butyl carbonate, benzyl carbonate, and tert-butyldimethylsilyl, is reacted with a compound of the formula (2), a known compound or a compound prepared by known methods, in the presence of BnNEt.sub.3Cl, in the presence of a base such as potassium carbonate, sodium carbonate, cesium carbonate, lithium carbonate, sodium hydroxide, potassium hydroxide, cesium hydroxide, lithium hydroxide, and the like, in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, acetonitrile, methanol, ethanol, isopropanol, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation, to provide a compounds of the formula (3). A compounds of the formula (3) is reacted with a compounds of the formula (4) a known compound or compound prepared by known methods in which Z.sup.1 is selected from the group consisting of methyl, trifluoromethyl, para-tolyl, and para-NO.sub.2-phenyl, in the presence of a base such as pyridine, 2,6-dimethyl pyridine, 2,6-di-tert-butyl pyridine, triethylamine, diisopropylethyl amine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (5). A compound of the formula (5) is reacted with a base such as potassium carbonate, sodium carbonate, cesium carbonate, lithium carbonate, and the like, in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (6)

    ##STR00462##

    [2081] A compound of formula (6) is reacted with a compound of the formula (7), a known compound or a compound prepared by known methods, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (8). A compound of the formula (8) is reacted with an acid such as hydrochloric acid, hydrobromic acid, sulfuric acid, para-toluenesulfonic acid, acetic acid, trifluoracetic acid, and the like, in a solvent such as benzene, toluene, para-xylene, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (9). A compound of the formula (9) is reacted with a compound of the formula (10), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (11).

    ##STR00463##

    [2082] A compound of formula (11) is reacted with sodium in the presence of naphthalene in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (12). A compound of the formula (12) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (13). Alternatively, a compound of the formula (12) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (13). Alternatively, a compound of the formula (12) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (13). A compound of the (13) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (14). A compound of the formula (14) is reacted with a compound of the formula (15), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (16).

    ##STR00464##

    [2083] A compound of formula (6) is reacted with a compound of the formula (17), a known compound or a compound prepared by known methods, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (18). A compound of the formula (18) is reacted with an acid such as hydrochloric acid, hydrobromic acid, sulfuric acid, para-toluenesulfonic acid, acetic acid, trifluoracetic acid, and the like, in a solvent such as benzene, toluene, para-xylene, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (19). A compound of the formula (19) is reacted with a compound of the formula (20), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (21). A compound of the formula (21) is reacted with a compound of the formula (22), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (11).

    ##STR00465##

    [2084] A compound of the formula (19) is reacted with a compound of the formula (23), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate and wherein Q.sup.1 is selected from the group consisting of 1 and 2, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (24). A compound of the formula (24) is reacted with a compound of the formula (25), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate and wherein Q.sup.2 is selected from the group consisting of 1 and 2, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (26). A compound of the formula (26) is reacted with a ruthenium catalyst such as benzylidene-bis(tricyclohexylphosphine)dichlororuthenium, (1,3-Bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene)dichloro(phenylmethylene)(tricyclohexyl phosphine)ruthenium, (1,3-bis-(2,4,6-trime thylphenyl)-2-imidazolidinylidene)dichloro(o-isopropoxy phenylmethylene)ruthenium, dichloro(2-isopropoxyphenylme thylene)(tricyclohexylphosphine) ruthenium(II), [1,3-bis(2-methylphenyl)-2-imidazolidinylidene]dichloro(phenylme thylene) (tricyclohexyl phosphine) ruthenium(II), dichloro[1,3-bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene](benzylidene) bis(3-bromopyridine)ruthenium(II), dichloro[1,3-bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene](3-methyl-2-butenylidene) (tricyclohexylphosphine)ruthenium(II), dichloro[1,3-bis(2-methylphenyl)-2-imidazolidinylidene] (2-isopropoxyphenylmethylene)ruthenium(II), [1,3-dimesityl-2-imidazolidinylidene]dichloro [3-(2-pyridinyl)propylidene]ruthenium(II), dichloro[1,3-bis(2,6-isopropylphenyl)-2-imidazolidinylidene] (2-isopropoxyphenylmethylene)ruthenium(II), dichloro(tricyclohexylphosphine) [(tricyclohexylphosphoranyl)methylidene]ruthenium tetrafluoroborate, dichloro[1,3-bis(2,4,6-trimethyl phenyl)-2-imidazolidinylidene][(tricyclohexylphosphoranyl)methylidene]ruthenium(II) tetrafluoroborate, [2-(1-methylethoxy-O)phenylme thyl-C](nitrato-O,O′){rel-(2R,5R,7R)-adamanlane-2,1-diyl[3-(2,4,6-trimethylphenyl)-1-imidazolidinyl-2-ylidene]}ruthenium, dichloro[1,3-bis(2,6-isopropylphenyl)-2-imidazolidinylidene] (benzylidene)(tricyclohexylphosphine)ruthenium(II), [1,3-bis(2-methylphenyl)-2-imidazolidinylidene]dichloro(phenylmethylene)(tricyclohexylphosphine)ruthenium(II), dichloro[1,3-bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene][3-(2-pyridinyl)propylidene]ruthenium(II), and the like in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (27).

    ##STR00466##

    [2085] A compound of the formula (27) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (28). A compound of the formula (28) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (29). Alternatively, a compound of the formula (28) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (29). Alternatively, a compound of the formula (28) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (29). A compound of formula (29) is reacted with sodium in the presence of naphthalene in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (30).

    ##STR00467##

    [2086] Alternatively, a compound of formula (27) is reacted with sodium in the presence of naphthalene in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (31). A compound of the formula (31) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (32). A compound of the formula (32) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (30). Alternatively, a compound of the formula (32) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (30). Alternatively, a compound of the formula (32) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (30).

    ##STR00468##

    [2087] A compound of the (30) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (33). A compound of the formula (33) is reacted with a compound of the formula (34), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (35).

    ##STR00469##

    [2088] A compound of the formula (31) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (36). Alternatively, a compound of the formula (31) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (36). Alternatively, a compound of the formula (31) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (36). A compound of the (36) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (37). A compound of the formula (37) is reacted with a compound of the formula (38), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (39).

    ##STR00470##

    [2089] A compound of the formula (26) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with triphenyl phosphine in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (40). Alternatively, a compound of the formula (26) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with dimethyl sulfide in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxye thane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (40). Alternatively, a compound of the formula (26) is reacted with ruthenium chloride in the presence of sodium periodate in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (40). Alternatively, a compound of the formula (26) is reacted with potassium osmate dehydrate in the presence of potassium ferricyanide, optionally in the presence of potassium carbonate, optionally in the presence of a base such as potassium hydroxide, sodium hydroxide, lithium hydroxide, and the like, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (40). Alternatively, a compound of the formula (26) is reacted with osmium tetraoxide in the presence of sodium periodate, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of a base such as pyridine, 2,6-lutidine, 2,6-di-tert-butylpyridine, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (40). Alternatively, a compound of the formula (26) is reacted with osmium tetraoxide in the presence of N-methylmorpholine N-oxide, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (40). A compound of the formula (40) is reacted with benzyl amine in the presence of a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (41). A compound of the formula (41) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, to provide a compound of the formula (42).

    ##STR00471##

    [2090] A compound of the formula (42) is reacted with Di-tert-butyl dicarbonate in the presence of a base such as such as pyridine, 2,6-lutidine, triethylamine, diisopropylethylamine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (43). A compound of formula (43) is reacted with sodium in the presence of naphthalene in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (44). A compound of the formula (44) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (45). Alternatively, a compound of the formula (44) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (45). Alternatively, a compound of the formula (44) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (45).

    ##STR00472##

    [2091] A compound of the (45) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (46). A compound of the formula (46) is reacted with a compound of the formula (47), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (48). A compound of the formula (48) is reacted with an acid such as trifluoroacetic acid, formic acid, acetic acid, hydrochloric acid, sulfuric acid, and the like, optionally in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (49).

    ##STR00473##

    [2092] A compound of the formula (49) is reacted with a compound of the formula (50), a known compound or a compound prepared by known methods, in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dime thoxyethane, N,N-dimethylformamide, N,N-dime thylacetamide, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (51).

    ##STR00474##

    [2093] A compound of the formula (49) is reacted with a compound of the formula (52), a known compound or a compound prepared by known methods, in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dime thoxyethane, N,N-dimethylformamide, N,N-dime thylacetamide, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (53).

    ##STR00475##

    [2094] A compound of the formula (49) is reacted with a compound of the formula (54), a known compound or a compound prepared by known methods, in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dime thoxyethane, N,N-dimethylformamide, N,N-dime thylacetamide, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (55).

    ##STR00476##

    [2095] A compound of the formula (49) is reacted with a compound of the formula (56), a known compound or a compound prepared by known methods, in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dime thoxyethane, N,N-dimethylformamide, N,N-dime thylacetamide, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (57).

    ##STR00477##

    [2096] A compound of the formula (49) is reacted with a compound of the formula (58), a known compound or a compound prepared by known methods, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dime thoxyethane, N,N-dimethylformamide, N,N-dime thylacetamide, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (59).

    ##STR00478##

    [2097] A compound of the formula (49) is reacted with a compound of the formula (60), a known compound or a compound prepared by known methods, in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dime thoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (61).

    ##STR00479##

    [2098] A compound of the formula (62) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with triphenyl phosphine in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (63). Alternatively, a compound of the formula (62) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with dimethyl sulfide in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (63). Alternatively, a compound of the formula (62) is reacted with ruthenium chloride in the presence of sodium periodate in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (63). Alternatively, a compound of the formula (62) is reacted with potassium osmate dehydrate in the presence of potassium ferricyanide, optionally in the presence of potassium carbonate, optionally in the presence of a base such as potassium hydroxide, sodium hydroxide, lithium hydroxide, and the like, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (63). Alternatively, a compound of the formula (62) is reacted with osmium tetraoxide in the presence of sodium periodate, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of a base such as pyridine, 2,6-lutidine, 2,6-di-tert-butylpyridine, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (63). Alternatively, a compound of the formula (62) is reacted with osmium tetraoxide in the presence of N-methylmorpholine N-oxide, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (63).

    ##STR00480##

    [2099] A compound of the formula (64) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with triphenyl phosphine in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (65). Alternatively, a compound of the formula (64) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with dimethyl sulfide in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (65). Alternatively, a compound of the formula (64) is reacted with ruthenium chloride in the presence of sodium periodate in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (65). Alternatively, a compound of the formula (64) is reacted with potassium osmate dehydrate in the presence of potassium ferricyanide, optionally in the presence of potassium carbonate, optionally in the presence of a base such as potassium hydroxide, sodium hydroxide, lithium hydroxide, and the like, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (65). Alternatively, a compound of the formula (64) is reacted with osmium tetraoxide in the presence of sodium periodate, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of a base such as pyridine, 2,6-lutidine, 2,6-di-tert-butylpyridine, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (65). Alternatively, a compound of the formula (64) is reacted with osmium tetraoxide in the presence of N-methylmorpholine N-oxide, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (65). A compound of the formula (65) is reacted with benzyl amine in the presence of a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (66). A compound of the formula (66) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, to provide a compound of the formula (67).

    ##STR00481##

    [2100] A compound of the formula (68) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (69). Alternatively, a compound of the formula (68) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with dimethyl sulfide in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (68a). Alternatively, a compound of the formula (68) is reacted with ruthenium chloride in the presence of sodium periodate in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (68a). Alternatively, a compound of the formula (68) is reacted with potassium osmate dehydrate in the presence of potassium ferricyanide, optionally in the presence of potassium carbonate, optionally in the presence of a base such as potassium hydroxide, sodium hydroxide, lithium hydroxide, and the like, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (68a). Alternatively, a compound of the formula (68) is reacted with osmium tetraoxide in the presence of sodium periodate, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of a base such as pyridine, 2,6-lutidine, 2,6-di-tert-butylpyridine, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (68a). Alternatively, a compound of the formula (68) is reacted with osmium tetraoxide in the presence of N-methylmorpholine N-oxide, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (68a). A compound of the formula (68a) is reacted with a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (69). A compound of the (69) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (70). Alternatively, a compound of the formula (69) is reacted with bromine in the presence of triphenylphosphine, in the presence of a base such as pyridine 2,6-dimethyl pyridine, 2,6-di-tert-butyl pyridine, triethylamine, diisopropylethyl amine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (70). Alternatively, a compound of the formula (69) is reacted with dibromotriphenylphosphorane, optionally in the presence of a base such as pyridine 2,6-dimethyl pyridine, 2,6-di-tert-butyl pyridine, triethylamine, diisopropylethyl amine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (70). A compound of the formula (70) is reacted with sodium sulfide in the presence of a solvent such as ethanol, methanol, isopropanol, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (71).

    ##STR00482##

    [2101] A compound of the formula (71) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (72). Alternatively, a compound of the formula (71) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (72). Alternatively, a compound of the formula (71) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (72). A compound of the (72) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (73). A compound of the formula (73) is reacted with a compound of the formula (74), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (75).

    ##STR00483##

    [2102] A compound of the formula (75) is reacted with an oxidizing agent such as m-chloroperoxybenzoic acid, monoperphthalic acid, peracetic acid, perpropionic acid, pertrifluoroacetic acid, potassium periodate, sodium metaperiodate, sodium perborate, potassium peroxymonosulfate (Oxon®), potassium peroxydisulfate, dimethyldioxirane, and the like, in the presence of a solvent such as tetrahydrofuran, ether, 1,4-dioxane, acetone, acetonitrile, methanol, ethanol, isopropanol, water, and the like, optionally with heating, optionally with microwave irradiation to provide compounds of the formula (76) and (77). Alternatively, a formula of the compound (75) is reacted with a sulfoxide such as diphenyl sulfoxide, dimethyl sulfoxide, and the like, in the presence of a rhenium catalyst such as ReOCl.sub.3(PPh3).sub.2, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, chloroform, tetrahydrofuran, ether, 1,4-dioxane, acetone, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide compounds of the formula (76) and (77). Alternatively, a formula of the compound (75) is reacted with a urea hydrogen peroxide complex in the presence of a rhenium catalyst such as ReOCl.sub.3(PPh3).sub.2, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, chloroform, tetrahydrofuran, ether, 1,4-dioxane, acetone, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide compounds of the formula (76) and (77). Alternatively, a compound of the formula (75) is reacted with hydrogen peroxide in the presence titanium (IV) isopropoxide-diethyltartarate, optionally in the presence of an amino alcohol such as 2-amino-3-phenylpropan-1-ol, 2-amino-4-methylpentan-1-ol, 2-amino-4-(methylthio)butan-1-ol, 2-aminopropan-1-ol, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, chloroform, tetrahydrofuran, ether, 1,4-dioxane, acetone, acetonitrile, N,N-dimethylformamide, and the like optionally with heating, optionally with microwave irradiation to provide compounds of the formula (76) and (77). It is understood that one skilled in the art would readily understand that the ratio of products (76) and (77) will be controlled by the amount of oxidant added and would adjust the amount of oxidant accordingly to produce the desired ration of products.

    ##STR00484##

    [2103] A suitably substituted compound of the formula (78), a known compound or a compound prepared by known methods wherein PG is a protecting selected from the group consisting of benzyl, tert-butyl carbonate, benzyl carbonate, and tert-butyldimethylsilyl, is reacted with a compound of the formula (79), a known compound or a compound prepared by known methods in which PG.sup.1 is a protecting group selected from the group consisting of benzyl, tert-butyl carbonate, benzyl carbonate, and tert-butyldimethylsilyl, and wherein the LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (80). A compound of the formula (80) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (81). Alternatively, a compound of the formula (80) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (81). Alternatively, a compound of the formula (80) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (81). A compound of the formula (81) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (82). Alternatively, a compound of the formula (81) is reacted with bromine in the presence of triphenylphosphine, in the presence of a base such as pyridine 2,6-dimethyl pyridine, 2,6-di-tert-butyl pyridine, triethylamine, diisopropylethyl amine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (82). Alternatively, a compound of the formula (81) is reacted with dibromotriphenylphosphorane, optionally in the presence of a base such as pyridine 2,6-dimethyl pyridine, 2,6-di-tert-butyl pyridine, triethylamine, diisopropylethyl amine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (82).

    ##STR00485##

    [2104] A compound of the formula (82), is reacted with a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (83). A compound of formula (83) is reacted with sodium in the presence of naphthalene in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (84). A compound of the formula (84) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (85). Alternatively, a compound of the formula (84) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (85). Alternatively, a compound of the formula (84) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (85).

    ##STR00486##

    [2105] A compound of the formula (85) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (86). Alternatively, a compound of the formula (85) is reacted with bromine in the presence of triphenylphosphine, in the presence of a base such as pyridine 2,6-dimethyl pyridine, 2,6-di-tert-butyl pyridine, triethylamine, diisopropylethyl amine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (86). Alternatively, a compound of the formula (85) is reacted with dibromotriphenylphosphorane, optionally in the presence of a base such as pyridine 2,6-dimethyl pyridine, 2,6-di-tert-butyl pyridine, triethylamine, diisopropylethyl amine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (86). A compound of the formula (86) is reacted with a compound of the formula (87), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (88).

    ##STR00487##

    [2106] Diethanolamine (89) is reacted with 4-nitrobenzenesulfonyl chloride (NosCl) in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, 2,6-lutidine, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride and the like to provide a compound of the formula (90). A compound of the formula (90) is then reacted with a compound of the formula (91), a known compound or one prepared by known methods, in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, 2,6-lutidine, and the like, in a solvent such as acetonitrile, methanol, ethanol, dimethyl formamide, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (92). A compound of the formula (92) is reacted with a thiophenol in the presence of a base such as sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, sodium carbonate, potassium carbonate, lithium bicarbonate, sodium hydroxide, potassium hydroxide, lithium hydroxide, and the like, in the presence of a solvent such as tetrahydrofuran, ethyl ether, 1,4-dioxane, acetonitrile and the like, optionally in the presence of dimethylsulfoxide, optionally with heating, optionally with microwave irradiation, to provide a compound of the formula (93).

    ##STR00488##

    [2107] A compound of the formula (94), a known compound or a compound prepared by known methods, is reacted with a compound of the formula (95), a known compound or a compound prepared by known methods in which X.sup.3 is selected from the group consisting of chlorine, bromine, iodine, and methanetrifluorosulfonate, in the presence of a base such as sodium tert-butoxide, lithium tert-butoxide, potassium tert-butoxide, and the like, optionally in the presence of a base such as triethylamine, diisopropylethyl amine, pyridine, 2,6-lutidine, and the like, in the presence of a palladium catalyst such as palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), tris(dibenzylideneacetone)dipalladium(0), and the like, in the presence of a solvent such as toluene, benzene, methylene chloride, 1,2-dichloroethae, tetrahydrofuran, 1,4-dioxane, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation, to provide a compound of the formula (96). A compound of the formula (96) is reacted with an acid such as trifluoroacetic acid, formic acid, acetic acid, hydrochloric acid, sulfuric acid, and the like, optionally in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (97).

    ##STR00489##

    [2108] A compound of the formula (98), a known compound or a compound prepared by known methods, is reacted with a compound of the formula (99), a known compound or a compound prepared by known methods in which X.sup.3 is selected from the group consisting of chlorine, bromine, iodine, and methanetrifluorosulfonate, in the presence of a base such as sodium tert-butoxide, lithium tert-butoxide, potassium tert-butoxide, and the like, optionally in the presence of a base such as triethylamine, diisopropylethyl amine, pyridine, 2,6-lutidine, and the like, in the presence of a palladium catalyst such as palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), tris(dibenzylideneacetone)dipalladium(0), and the like, in the presence of a solvent such as toluene, benzene, methylene chloride, 1,2-dichloroethae, tetrahydrofuran, 1,4-dioxane, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation, to provide a compound of the formula (100). A compound of the formula (100) is reacted with an acid such as trifluoroacetic acid, formic acid, acetic acid, hydrochloric acid, sulfuric acid, and the like, optionally in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (101).

    ##STR00490##

    [2109] A compound of the formula (102), a known compound or a compound prepared by known methods, is reacted with tert-butylchlorodimethylsilane in the presence of a base such as imidazole, 4-dimethylaminopyridine, potassium carbonate, sodium carbonate, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (103). A compound of the formula (103) is reacted with di-tert-butyl dicarbonate in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (104). A compound of the formula (104) is reacted with a compound of the formula (105), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (106). A compound of the formula (106) is reacted with a compound of the formula (107), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (108).

    ##STR00491##

    [2110] A compound of the formula (108) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (109). A compound of the formula (109) is reacted with 4-methylbenzenesulfonyl chloride in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (110). A compound of the formula (110) is reacted with a compound of the formula (111), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (112).

    ##STR00492##

    [2111] A compound of the formula (113), a known compound or a compound prepared by known methods, is reacted with 4-methylbenzenesulfonyl chloride in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (114). A compound of the formula (114) is reacted with a source of cyanide such as potassium cyanide, sodium cyanide, lithium cyanide, tetrabutylammonium cyanide, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (115). A compound of the formula (115) is reacted with an acid such as as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (116) where R.sup.z is H. Alternatively, a compound of the formula of the formula (115) can be treated with acid and a suitable alcoholic solvent to provide the compound of the formula (116) that is a carboxylic acid ester (e.g., where R.sup.z is a C.sub.1-6 alkyl): suitable conditions include using 6M HCl in methanol to provide ester compounds of the formula (116) where Rz is methyl. A compound of the formula (116) is reacted with a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (117). A compound of the formula (117) is reacted with tert-butylchlorodimethylsilane in the presence of a base such as imidazole, 4-dimethylaminopyridine, potassium carbonate, sodium carbonate, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (118). A compound of the formula (118) is reacted with di-tert-butyl dicarbonate in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (119).

    ##STR00493##

    [2112] A compound of the formula (119) is reacted with a compound of the formula (120), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate and wherein Q.sup.1 is selected from the group consisting of 1 and 2, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (121). A compound of the formula (121) is reacted with a compound of the formula (122), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate and wherein Q.sup.2 is selected from the group consisting of 1 and 2, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (123). A compound of the formula (123) is reacted with a ruthenium catalyst such as benzylidene-bis(tricyclohexylphosphine)dichlororuthenium, (1,3-Bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene)dichloro(phenylme thylene)(tricyclohexyl phosphine)ruthenium, (1,3-bis-(2,4,6-trime thylphenyl)-2-imidazolidinylidene)dichloro(o-isopropoxy phenylme thylene)ruthenium, dichloro(2-isopropoxyphenylme thylene)(tricyclohexylphosphine) ruthenium(II), [1,3-bis(2-me thylphenyl)-2-imidazolidinylidene] dichloro(phenylme thylene) (tricyclohexyl phosphine) ruthenium(II), dichloro[1,3-bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene](benzylidene) bis(3-bromopyridine)ruthenium(II), dichloro[1,3-bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene](3-methyl-2-butenylidene) (tricyclohexylphosphine)ruthenium(II), dichloro [1,3-bis(2-methylphenyl)-2-imidazolidinylidene](2-isopropoxyphenylmethylene)ruthenium(II), [1,3-dime sityl-2-imidazolidinylidene] dichloro [3-(2-pyridinyl)propylidene]ruthenium(II), dichloro[1,3-bis(2,6-isopropylphenyl)-2-imidazolidinylidene](2-isopropoxyphenylmethylene)ruthenium(II), dichloro(tricyclohexylphosphine) [(tricyclohexylphosphoranyl)methylidene]ruthenium tetrafluoroborate, dichloro[1,3-bis(2,4,6-trimethyl phenyl)-2-imidazolidinylidene][(tricyclohexylphosphoranyl)methylidene]ruthenium(II) tetrafluoroborate, [2-(1-me thylethoxy-O)phenylme thyl-C](nitrato-O,O′){rel-(2R,5 R,7R)-adamanlane -2,1-diyl[3-(2,4,6-trimethylphenyl)-1-imidazolidinyl-2-ylidene]}ruthenium, dichloro[1,3-bis(2,6-isopropylphenyl)-2-imidazolidinylidene](benzylidene)(tricyclohexylphosphine)ruthenium(II), [1,3-bis(2-methylphenyl)-2-imidazolidinylidene]dichloro(phenylmethylene)(tricyclohexylphosphine)ruthenium(II), dichloro[1,3-bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene][3-(2-pyridinyl)propylidene]ruthenium(II), and the like in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (124).

    ##STR00494##

    [2113] A compound of the formula (124) is reacted with ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with triphenyl phosphine in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (125). Alternatively, a compound of the formula (124) is reacted with a ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with dimethyl sulfide in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (125). Alternatively, a compound of the formula (124) is reacted with ruthenium chloride in the presence of sodium periodate in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (125). Alternatively, a compound of the formula (124) is reacted with potassium osmate dehydrate in the presence of potassium ferricyanide, optionally in the presence of potassium carbonate, optionally in the presence of a base such as potassium hydroxide, sodium hydroxide, lithium hydroxide, and the like, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (125). Alternatively, a compound of the formula (124) is reacted with osmium tetraoxide in the presence of sodium periodate, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of a base such as pyridine, 2,6-lutidine, 2,6-di-tert-butylpyridine, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (125). Alternatively, a compound of the formula (124) is reacted with osmium tetraoxide in the presence of N-methylmorpholine N-oxide, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (125). A compound of the formula (125) is reacted with benzyl amine in the presence of a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (126). A compound of the formula (126) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, to provide a compound of the formula (127).

    ##STR00495##

    [2114] A compound of the formula (127) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (128). A compound of the formula (128) is reacted with di-tert-butyl dicarbonate in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (129). A compound of the formula (129) is reacted with 4-methylbenzenesulfonyl chloride in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (130).

    ##STR00496##

    [2115] A compound of the formula (130) is reacted with a compound of the formula (131), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (132). A compound of the formula (132) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (133).

    ##STR00497##

    [2116] A compound of the formula (134) wherein n is selected from the group consisting 1 and 2, a known compound or a compound prepared by known methods, is reacted with 4-methylbenzenesulfonyl chloride in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (135). A compound of the formula (135) is reacted with di-tert-butyl malonate in the presence of a base such as potassium tert-butoxide, sodium tert-butoxide, lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (136). A compound of the formula (136) an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (137). A compound of the formula (137) is reacted with methanol in the presence of an acid such as hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, 1,2-dime thoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (138). Alternatively, a compound of the formula (137) is reacted with methanol in the presence of a coupling agent such as 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, N,N′-dicyclohexylcarbodiimide, O-benzotriazole-N,N,N ,N′-tetramethyl-uronium-hexafluoro-phosphate, O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate, benzotriazole-1-yl-oxy-tris-(dimethylamino)-phosphonium hexafluorophosphate, benzotriazol-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate, and the like, optionally in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, 2,6-lutidine, and the like, optionally in the presence of 4-N,N-dimethylaminopyridine, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (138). Alternatively, a compound of the formula (137) is reacted with (diazomethyl)trimethylsilane in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (138).

    ##STR00498##

    [2117] A compound of the formula (138) is reacted with a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (139). A compound of the formula (139) is reacted with tert-butylchlorodimethylsilane in the presence of a base such as imidazole, 4-dimethylaminopyridine, potassium carbonate, sodium carbonate, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (140). A compound of the formula (140) is reacted with di-tert-butyl dicarbonate in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (141). A compound of the formula (141) is reacted with a compound of the formula (142), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (143). A compound of the formula (143) is reacted with a compound of the formula (144), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (145).

    ##STR00499##

    [2118] A compound of the formula (145) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (146). A compound of the formula (146) is reacted with 4-methylbenzenesulfonyl chloride in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (147). A compound of the formula (147) is reacted with a compound of the formula (148), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (149).

    ##STR00500## ##STR00501##

    [2119] Intermediate (130) of Scheme 34 can also be used in methods that allow the further homologation of the alkylene linker group. An exemplary method is shown in Scheme 39.

    [2120] A compound of the formula (130) is reacted with a source of cyanide such as potassium cyanide, sodium cyanide, lithium cyanide, tetrabutylammonium cyanide, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (150).

    [2121] A compound of the formula (150) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (151).

    [2122] A group corresponding to R.sup.7 as described herein can be introduced according to methods known in the art (e.g., as described in Scheme 13). For example, a compound of the formula (151) can be reacted with a compound of the formula (50), a known compound or a compound prepared by known methods, in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (152), where R.sup.7 is SO.sub.2R.sup.10c. Alternatively, a compound of the formula (151) can be used as a starting material in the exemplary methods of Schemes 14 and 15 to provide respectively a compound of the formula (152), where R.sup.7 is COR.sup.8 or CO2R.sup.9.

    [2123] A compound of the formula (152) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (153) where R.sup.z is H. Alternatively, a compound of the formula of the formula (152) can be treated with acid and a suitable alcoholic solvent to provide the compound of the formula (153) that is a carboxylic acid ester (e.g., where R.sup.z is a C.sub.1-6 alkyl): suitable conditions include using 6M HCl in methanol to provide ester compounds of the formula (153) where R.sup.z is methyl.

    [2124] A compound of the formula (153) is reacted with a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (154).

    [2125] A compound of the formula (154) is reacted with 4-methylbenzenesulfonyl chloride in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (155).

    [2126] A compound of the formula (155) is reacted with a compound of the formula (131), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (156).

    [2127] The Examples provided below provide representative methods for preparing exemplary compounds of the present invention. The skilled practitioner will know how to substitute the appropriate reagents, starting materials and purification methods known to those skilled in the art, in order to prepare the compounds of the present invention.

    EXAMPLES

    [2128] The practice of the invention is illustrated by the following non-limiting examples. The Examples provided below provide representative methods for preparing exemplary compounds of the present invention. The skilled practitioner will know how to substitute the appropriate reagents, starting materials and purification methods known to those skilled in the art, in order to prepare the compounds of the present invention.

    [2129] In the examples that follow, .sup.1H-NMR spectra were obtained on a Varian Mercury 300-MHz NMR. Purity (%) and mass spectral data were determined with a Waters Alliance 2695 HPLC/MS (Waters Symmetry C18, 4.6×75 mm, 3.5 μm) with a 2996 diode array detector from 210-400 nm.

    Example 1

    Compound Synthesis

    [2130] ##STR00502##

    [2131] Preparation of tert-butyl (R)-2-(((tert-butyldimethylsilyl)oxy)methyl)-5-oxopyrrolidine-1-carboxylate: To a stirred solution of (R)-(+5-(hydroxymethyl)-2-pyrrolidinone (1.0 g, 8.68 mmol, 1.0 equiv) and tert-butyldimethylsilyl chloride (1.44 g, 9.54 mmol, 1.1 equiv.) in dichloromethane (17.3 mL) was added imidazole (0.650 g, 9.54 mmol, 1.1 equiv.). The resulting mixture was then allowed to stirred at 23° C. for 2 hours before being diluted with deionized H.sub.2O (25 mL) and extracted with diethyl ether (3×25 mL). The combined organic layers were dried over Na.sub.2SO.sub.4 and concentrated in vacuum to give a crude intermediate which was then dissolved in acetonitrile (43 mL). To the resulting solution was added triethylamine (1.75 g, 17.3 mmol, 2 equiv.), 4-dimethylaminopyridine (0.212 g, 1.73 mmol, 0.2 equiv.) and di-tert-butyl dicarbonate (2.6 g, 16.5 mmol, 1.9 equiv.). The reaction solution was then allowed to stir at 23° C. for 2 hours before being diluted with saturated aqueous NH.sub.4Cl (25 mL) and extracted with ethyl acetate (3×25 mL). The combined organic layers were dried over Na.sub.2SO.sub.4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 20%-30%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 4.13 (m, 1H), 3.88 (dd, J=4.0, 10.3 Hz, 1H), 3.65 (dd, J=2.2, 10.3 Hz, 1H), 2.66 (m, 1H), 2.33 (m, 1H), 2.13-1.92 (m, 2H), 1.49 (s, 9H), 0.84 (s, 9H), 0.00 (d, J=5.3 Hz, 6H).

    ##STR00503##

    [2132] Preparation of tert-butyl (R)-5-(((tert-butyldimethylsilyl)oxy)methyl)-3,3-diethyl-2-oxopyrrolidine-1-carboxylate: To a dry round bottom flask under N.sub.2 atmosphere was added tert-butyl (R)-2-(((tert-butyldimethylsilyl)oxy)methyl)-5-oxopyrrolidine-1-carboxylate (2.63 g, 7.98 mmol, 1.0 equiv.) and then dissolved in dry tetrahydrofuran (11.5 mL). The resulting solution was then cooled to −78° C. and 1 M Lithium bis(trimethylsilyl)amide solution (tetrahydrofuran, 16.8 mL, 16.8 mmol, 2.1 equiv.) was added dropwise. The resulting solution was allowed to gradually warm to −20° C. before being cooled back to −78° C. and followed by dropwise addition of iodoethane (3.12 g, 20 mmol, 2.5 equiv.). The reaction solution was then allowed to gradually warm to 0° C. and stir at that temperature for 2 hours before being warmed to 23° C. and allowed to stir for an additional 2 hours. The resulting solution was diluted with saturated aq. NH.sub.4Cl (25 mL) and extracted with ethyl acetate (3×25 mL). The combined organic layers were dried over Na.sub.2SO.sub.4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 0%-10%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 3.94 (m, 1H), 3.83 (dd, J=5.2, 10.0 Hz, 1H), 3.67 (dd, J=2.5, 10.0 Hz, 1H), 1.95 (dd, J=6.3, 13.4 Hz, 1H), 1.79 (dd, J=9.0, 13.4 Hz, 1H), 1.65-1.40 (m, 13H), 0.90-0.75 (m, 15H), 0.00 (d, J=3.3 Hz, 6H).

    ##STR00504##

    [2133] Preparation of (R)-3,3-diethyl-5-(hydroxymethyl)pyrrolidin-2-one: A 6M HCl in methanol solution was prepared via the addition of acetyl chloride (4.8 mL) to methanol (12 mL). To a small round bottom flask was added tert-butyl (R)-5-(((tert-butyldimethylsilyl)oxy)methyl)-3,3-diethyl-2-oxopyrrolidine-1-carboxylate (0.875 g, 2.65 mmol, 1.0 equiv.) and 1 mL of methanol. The prepared methanolic HCl solution was then added dropwise (12 mL) and the resulting mixture was allowed to stir at 23° C. for 30 min before being diluted with methanol and concentrated in vacuum to produce a crude product that was used in the next step without further purification. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.61 (b, 1H), 4.96 (b, 1H), 3.69-3.48 (m, 2H), 3.33 (dd, J=8.1, 11.2 Hz, 1H), 1.84 (dd, J=7.8, 13.3 Hz, 1H), 1.58-1.31 (m, 5H), 0.80 (dt, J=7.5, 21.9 Hz, 6H).

    ##STR00505##

    [2134] Preparation of (R)-(4,4-diethyl-5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate: To a stirred solution of (R)-3,3-diethyl-5-(hydroxymethyl)pyrrolidin-2-one (0.367 g, 2.14 mmol, 1.0 equiv) and triethylamine (0.240 g, 2.36 mmol, 1.1 equiv) in dichloromethane (3.3 mL), 4-methylbenzenesulfonyl chloride (0.450 g, 2.36 mmol, 1.1 equiv) and 4-dimethylaminopyridine (0.053 g, 0.428 mmol, 0.2 equiv.) were subsequently added at 0° C. The resulting mixture was stirred at 0° C. for 10 minutes and allowed to stir overnight at 23° C. Then, the reaction mixture was diluted with dichloromethane (25 mL), washed with 1N HCl (1×5 mL) and deionized H.sub.2O (2×5 mL), dried over Na.sub.2SO.sub.4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 0%-100%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.71 (d, J=8.3 Hz, 2H), 7.28 (d, J=8.1 Hz, 2H), 6.57 (b, 1H), 3.96 (dd, J=4.0, 9.6 Hz, 1H), 3.82-3.67 (m, 2H), 2.37 (s, 3H), 1.90 (dd, J=7.9, 13.5 Hz, 1H), 1.52 (dd, J=7.1, 13.6 Hz, 1H) 1.49-1.31 (m, 4H), 0.75 (dt, J=7.4, 26.5 Hz, 6H).

    ##STR00506##

    [2135] Preparation of (R)-3,3-diethyl-5-((4-phenylpiperazin-1-yl)methyl)pyrrolidin-2-one formate: To a small vial was added (R)-(4,4-diethyl-5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate (75 mg, 0.23 mmol, 1 equiv.) and 1-phenylpiperazine (79 mg, 0.48 mmol, 2.1 equiv.) then both were dissolved in acetonitrile (2.3 mL). Then K.sub.2CO.sub.3 (80 mg, 0.57 mmol, 2.5 equiv.) was added, the reaction mixture was allowed to stir at 80° C. for 3 days, and then cooled to 23° C. The mixture was filtered, washed with acetonitrile, and the filtrate was concentrated in vacuum to give a crude product which was further purified by HPLC (CH.sub.3CN/H.sub.2O, 0.1% Formic acid), 0%˜100%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.19 (m, 2H), 6.85 (d, J=8.3 Hz, 2H), 6.79 (t, J=7.0 Hz, 1H), 6.42 (b, 1H), 3.70 (m, 1H), 3.12 (m, 4H), 2.70 (m, 2H), 2.50 (m, 2H), 2.41 (dd, J=3.6, 12.4 Hz, 1H), 2.29 (dd, J=9.8, 12.4 Hz, 1H), 1.93 (dd, J=7.6, 13.5 Hz, 1H), 1.57-1.37 (m, 5H), 0.84 (dt, J=7.4, 19.6 Hz, 6H). LC/MS [M+H]=m/z 316.2.

    ##STR00507##

    [2136] Preparation of (R)-3,3-diethyl-5-((4-(p-tolyppiperazin-1-yl)methyl)pyrrolidin-2-one formate: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-((4-phenylpiperazin-1-yl)methyl)pyrrolidin-2-one formate, except 1-(4-methylphenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.09 (d, J=8.2 Hz, 2H), 6.85 (d, J=8.5 Hz, 2H), 6.47 (b, 1H), 3.78 (m, 1H), 3.15 (m, 4H), 2.78 (m, 2H), 2.59 (m, 2H), 2.49 (dd, J=3.6, 12.4 Hz, 1H), 2.38 (dd, J=9.9, 12.4 Hz, 1H), 2.28 (s, 3H), 2.01 (dd, J=7.6, 13.1 Hz, 1H), 1.67-1.45 (m, 5H), 0.93 (dt, J=7.4, 19.6 Hz, 6H). LC/MS [M+H]=m/z 330.2.

    ##STR00508##

    [2137] Preparation of (R)-5-((4-(3-chlorophenyl)piperazin-1-yl)methyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-((4-phenylpiperazin-1-yl)methyl)pyrrolidin-2-one formate, except 1-(3-chlorophenyl)piperazine hydrochloride was substituted for 1-phenylpiperazine and 5 equiv. of K.sub.2CO.sub.3 used instead of 2.5 equiv. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.09 (t, J=8.1 Hz, 1H), 6.79 (t, J=2.0 Hz, 1H), 6.74 (dd, J=1.8, 7.7 Hz, 1H), 6.70 (dd, J=2.3, 8.3 Hz, 1H), 6.36 (b, 1H), 3.69 (m, 1H), 3.11 (m, 4H), 2.67 (m, 2H), 2.47 (m, 2H), 2.39 (dd, J=3.5, 12.3 Hz, 1H), 2.28 (dd, J=10.0, 12.4 Hz, 1H), 1.92 (dd, J=7.8, 13.2 Hz, 1H), 1.58-1.38 (m, 5H), 0.84 (dt, J=7.5, 20.2 Hz, 6H). LC/MS [M+H]=m/z 350.2.

    ##STR00509##

    [2138] Preparation of (R)-3,3-diethyl-5-((4-(4-fluorophenyl)piperazin-1-yl)methyl)pyrrolidin-2-one formate: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-((4-phenylpiperazin-1-yl)methyl)pyrrolidin-2-one formate, except 1-(4-fluorophenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 6.97 (m, 2H), 6.92-6.77 (m, 3H), 3.81 (m, 1H), 3.15 (m, 4H), 2.82 (m, 2H), 2.65 (m, 2H), 2.53 (dd, J=3.5, 12.4 Hz, 1H), 2.44 (dd, J=9.6, 12.4 Hz, 1H), 2.03 (dd, J=7.6, 13.3 Hz, 1H), 1.68-1.44 (m, 5H), 0.92 (dt, J=7.5, 18.9 Hz, 6H). LC/MS [M+H]=m/z 334.2.

    ##STR00510##

    [2139] Preparation of (R)-3,3-diethyl-5-(pyridin-2-yl)piperazin-1-yl)methyl)pyrrolidin-2-one formate: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-((4-phenylpiperazin-1-yl)methyl)pyrrolidin-2-one formate, except 1-(2-pyridyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 8.19 (m, 1H), 7.50 (m, 1H), 6.86 (b, 1H) 6.65 (m, 2H), 3.81 (m, 1H), 3.57 (m, 4H), 2.77 (m, 2H), 2.59 (m, 2H), 2.51 (dd, J=3.8, 12.6 Hz, 1H), 2.43 (dd, J=9.4, 12.5 Hz, 1H), 2.02 (dd, J=7.7, 13.2 Hz, 1H), 1.66-1.44 (m, 5H), 0.90 (dt, J=7.4, 20.0 Hz, 6H). LC/MS [M+H]=m/z 317.2.

    ##STR00511##

    [2140] Preparation of (R)-3,3-diethyl-5-((4-(2-isopropylphenyl)piperazin-1-yl)methyl)pyrrolidin-2-one formate: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-((4-phenylpiperazin-1-yl)methyl)pyrrolidin-2-one formate, except 1-(2-isopropylphenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.18 (m, 1H), 7.12-6.99 (m, 3H), 6.34 (b, 1H), 3.71 (m, 1H), 3.40 (sept, J=6.8 Hz, 1H), 2.83 (m, 4H), 2.71 (b, 2H), 2.60-2.39 (b, 3H), 2.32 (m, 1H), 1.94 (dd, J=7.5, 13.2 Hz, 1H), 1.60-1.36 (m, 5H), 1.12 (d, J=6.9 Hz, 6H), 0.84 (dt, J=7.4, 18.3 Hz, 6H). LC/MS [M+H]=m/z 358.2.

    ##STR00512##

    [2141] Preparation of (R)-3,3-diethyl-5-((4-(4-methyl-2-morpholinophenyl)piperazin-1-yl)methyl)pyrrolidin-2-one formate: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-((4-phenylpiperazin-1-yl)methyl)pyrrolidin-2-one formate, except 1-(4-methyl-2-morpholinophenyl)piperazine was substituted for 1-phenylpiperazine. NMR (400 MHz, CDCl.sub.3) δ 6.73 (m, 2H), 6.63 (b, 1H), 6.45 (b, 1H) 3.82-3.64 (m, 5H), 3.31-2.84 (b, 8H), 2.68 (b, 2H), 2.57-2.38 (b, 3H), 2.32 (m, 1H), 2.21 (s, 3H), 1.94 (dd, J=7.4, 13.0 Hz, 1H), 1.59-1.38 (m, 5H), 0.84 (dt, J=7.4, 18.8 Hz, 6H). LC/MS [M+H]=m/z 415.2.

    ##STR00513##

    [2142] Preparation of (S)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide: To a stirred solution of (S)-2-(2-(benzyloxy)ethyl)oxirane (0.5 g, 2.8 mmo, 1.0 equiv.) in 1,4-dioxane (11.25 mL) was added p-toluenesulfonamide (0.96 g, 5.6 mmol, 2.0 equiv.), benzyltriethylammonium chloride (0.064 g, 0.28 mmol, 0.1 equiv.) and Cs.sub.2CO.sub.3 (0.092 g, 0.28 mmol, 0.1 equiv.). The resulting mixture was then stirred at 90° C. for 48 hours. The reaction was then allowed to cool to 23° C. and concentrated in vacuum to give a crude product which was further purified by HPLC (CH.sub.3CN/H.sub.2O, 0.1% Formic acid), 0%˜100%). Desired fractions were further purified by column chromatography (Ethyl acetate/Hexanes, 10%˜100%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.73 (d, J=8.2 Hz, 2H), 7.44-7.22 (m, 7H), 5.00 (t, J=6.2 Hz, 1H), 4.50 (s, 2H), 3.93 (m, 1H), 3.66 (m, 2H), 3.07 (m, 1H), 2.87 (m, 1H), 2.43 (s, 3H), 1.83 (m, 1H), 1.70 (m, 1H).

    ##STR00514##

    [2143] Preparation of (R)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide: The title compound was prepared according to the procedure for (S)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide, except (R)-2-(2-(benzyloxy)ethyl)oxirane was substituted for (S)-2-(2-(benzyloxy)ethyl)oxirane. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.64 (d, J=8.2 Hz, 2H), 7.31-7.16 (m, 7H), 4.90 (t, J=6.1 Hz, 1H), 4.41 (s, 2H), 3.84 (m, 1H), 3.57 (m, 2H), 2.98 (m, 1H), 2.78 (m, 1H), 2.34 (s, 3H), 1.74 (m, 1H), 1.60 (m, 1H).

    ##STR00515##

    [2144] Preparation of N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide: The title compound was prepared according to the procedure for (S)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide, except (rac)-2-(2-(benzyloxy)ethyl)oxirane was substituted for (S)-2-(2-(benzyloxy)ethyl)oxirane. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.66 (d, J=8.2 Hz, 2H), 7.35-7.18 (m, 7H), 4.92 (t, J=6.1 Hz, 1H), 4.43 (s, 2H), 3.89 (m, 1H), 3.60 (m, 2H), 3.02 (m, 1H), 2.80 (m, 1H), 2.38 (s, 3H), 1.77 (m, 1H), 1.63 (m, 1H).

    ##STR00516##

    [2145] Preparation of (R)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine: This reaction was performed in oven-dried glassware under a nitrogen atmosphere. To a stirred solution of pyridine (1.57 g, 19.9 mmol, 5.0 equiv.) and methanesulfonyl chloride (2.28 g, 19.9 mmol, 5.0 equiv.) in dry dichloromethane (22.5 mL) at 0° C. was added a solution of (S)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide (1.4 g, 3.99 mmol, 1.0 equiv.) in dry dichloromethane (22.5 mL). The resulting solution was stirred at reflux overnight, cooled to 23° C., and washed with brine (50 mL). The organic layer was dried over Na.sub.2SO.sub.4 and concentrated in vacuo to give crude mesylate which was further purified by column chromatography (Ethyl acetate/Hexanes, 10%˜50%).

    [2146] The purified mesylate was then dissolved in acetonitrile (45 mL) and K.sub.2CO.sub.3 (2.22 g, 16.0 mmol, 4.0 equiv.) was added. The resulting mixture was allowed to stir at 45° C. overnight before being cooled to 23° C. and filtered. The filtrate was concentrated in vacuo to give crude product which was purified by column chromatography (Ethyl acetate/Hexanes, 10% 20%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.84 (d, J=8.2 Hz, 2H), 7.45-7.19 (m, 7H), 4.39 (s, 2H), 3.46 (dt, J=3.7, 9.2 Hz, 1H), 3.35 (m, 1H), 2.93 (m, 1H), 2.70 (d, J=7.1 Hz, 1H), 2.45 (s, 3H), 2.15 (d, J=4.6 Hz, 1H), 1.94 (m, 1H), 1.58 (m, 1H).

    ##STR00517##

    [2147] Preparation of (S)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine: The title compound was prepared according to the procedure for (R)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine, except (R)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide was substituted for (S)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.84 (d, J=8.3 Hz, 2H), 7.43-7.23 (m, 7H), 4.39 (s, 2H), 3.46 (dt, J=3.8, 9.3 Hz, 1H), 3.35 (m, 1H), 2.93 (m, 1H), 2.69 (d, J=7.0 Hz, 1H), 2.45 (s, 3H), 2.15 (d, J=4.5 Hz, 1H), 1.94 (m, 1H), 1.59 (m, 1H).

    ##STR00518##

    [2148] Preparation of 2-(2-(benzyloxy)ethyl)-1-tosylaziridine: The title compound was prepared according to the procedure for (R)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine, except (rac)-N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide was substituted for (S)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.84 (d, J=8.3 Hz, 2H), 7.41-7.26 (m, 7H), 4.39 (s, 2H), 3.46 (dt, J=3.8, 9.3 Hz, 1H), 3.35 (m, 1H), 2.93 (m, 1H), 2.69 (d, J=7.0 Hz, 1H), 2.45 (s, 3H), 2.15 (d, J=4.6 Hz, 1H), 1.93 (m, 1H), 1.59 (m, 1H).

    ##STR00519##

    [2149] Preparation of (S)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido) hexanamide: This reaction was performed in oven-dried glassware under a nitrogen atmosphere. To a cooled solution of dry N,N-dimethylacetamide (0.527 g, 6.05 mmol, 1.1 equiv.) and dry tetrahydrofuran (18 mL) at −78° C. was added dropwise a 1M Lithium diisopropylamide solution (tetrahydrofuran/Hexanes, 7.26 mL, 7.26 mmol, 1.3 equiv.). The resulting solution was then stirred at −78° C. for 30 minutes before being allowed to warm to 0° C. At 0° C., a solution of (R)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine (1.82 g, 5.5 mmol, 1.0 equiv.) in dry tetrahydrofuran (18 mL) was added to the solution. The reaction was stirred at 0° C. for 20 minutes and then allowed to warm to 23° C. and stir overnight. The reaction was quenched with sat. NH.sub.4Cl (40 mL) and extracted with ethyl acetate (3×30 mL). The combined organic layers were dried over Na.sub.2SO.sub.4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 40%˜100%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.72 (d, J=8.2 Hz, 2H), 7.41-7.19 (m, 7H), 5.91 (d, J=7.5 Hz, 1H), 4.40 (q, J=9.3 Hz, 2H), 3.56 (m, 1H), 3.40 (m, 2H), 2.93 (s, 3H), 2.90 (s, 3H), 2.48-2.35 (m, 4H), 2.21 (dt, J=6.6, 16.6 Hz, 1H), 1.88-1.69 (m, 2H), 1.68-1.55 (m, 2H).

    ##STR00520##

    [2150] Preparation of (R)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido) hexanamide: The title compound was prepared according to the procedure for (S)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyOsulfonamido)hexanamide, except (S)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine was substituted for (R)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.71 (d, J=8.2 Hz, 2H), 7.41-7.18 (m, 7H), 5.91 (d, J=7.5 Hz, 1H), 4.40 (q, J=8.9 Hz, 2H), 3.54 (m, 1H), 3.40 (m, 2H), 2.94 (s, 3H), 2.91 (s, 3H), 2.47-2.35 (m, 4H), 2.21 (dt, J=6.6, 16.6 Hz, 1H), 1.87-1.68 (m, 2H), 1.67-1.52 (m, 2H).

    ##STR00521##

    [2151] Preparation of 6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido) hexanamide: The title compound was prepared according to the procedure for (S)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyOsulfonamido)hexanamide, except (rac)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine was substituted for (R)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.72 (d, J=8.2 Hz, 2H), 7.42-7.21 (m, 7H), 5.90 (d, J=7.5 Hz, 1H), 4.41 (q, J=9.3 Hz, 2H), 3.57 (m, 1H), 3.40 (m, 2H), 2.95 (s, 3H), 2.93 (s, 3H), 2.50-2.36 (m, 4H), 2.23 (dt, J=6.6, 16.6 Hz, 1H), 1.88-1.70 (m, 2H), 1.69-1.57 (m, 2H).

    ##STR00522##

    [2152] Preparation of (S)-5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one: (S)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido)hexanamide (0.565g, 1.35 mmol, 1.0 equiv.) was mixed with p-toluenesulfonic acid monohydrate (0.282g, 1.48 mmol, 1.1 equiv.) and toluene (5.65 mL) in a microwave vial. The mixture was then heated in a microwave reactor at 190° C. for 2 hours. The mixture was then neutralized with sat. NaHCO.sub.3 and extracted with ethyl acetate (3×15 mL). The combined organic phase was dried over Na.sub.2SO.sub.4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 0%˜40%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.96 (d, J=8.2 Hz, 2H), 7.42-7.26 (m, 7H), 4.59-4.42 (m, 3H), 3.65-3.54 (m, 2H), 2.62-2.50 (m, 1H), 2.45 (s, 3H), 2.42-2.27 (m, 2H), 2.25-2.12 (m, 1H), 2.11-1.89 (m, 2H).

    ##STR00523##

    [2153] Preparation of (R)-5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one: The title compound was prepared according to the procedure for (S)-5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one, except (R)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido)hexanamide was substituted for (S)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido)hexanamide. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.95 (d, J=8.4 Hz, 2H), 7.39-7.25 (m, 7H), 4.59-4.42 (m, 3H), 3.67-3.53 (m, 2H), 2.61-2.47 (m, 1H), 2.42 (s, 3H), 2.40-2.23 (m, 2H), 2.22-2.09 (m, 1H), 2.07-1.89 (m, 2H).

    ##STR00524##

    [2154] Preparation of 5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one: The title compound was prepared according to the procedure for (S)-5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one, except (rac)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido)hexanamide was substituted for (S)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido)hexanamide. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.96 (d, J=8.3 Hz, 2H), 7.41-7.25 (m, 7H), 4.60-4.42 (m, 3H), 3.64-3.54 (m, 2H), 2.62-2.49 (m, 1H), 2.44 (s, 3H), 2.42-2.26 (m, 2H), 2.24-2.11 (m, 1H), 2.10-1.88 (m, 2H).

    ##STR00525##

    [2155] Preparation of (R)-(5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate: To a cooled mixture of (R)-(−)-5-(hydroxymethyl)-2-pyrrolidinone (10.0 g, 87 mmol, 1.0 equiv.) and triethylamine (9.68 g, 95.7 mmol, 1.1 equiv.) in methylene chloride (134 mL) at 0° C. was added 4-toluenesulfonyl chloride (18.25 g, 95.7 mmol, 1.1 equiv.) followed by 4-dimethylaminopyridine (2.12 g, 17.3 mmol, 0.2 equiv.). The resulting reaction mixture was stirred at 0° C. for 5 minutes before being warmed to 23° C. and allowed to stir overnight. Then, the reaction mixture was diluted with dichloromethane (200 mL), washed with 1N HCl (1×200 mL) and deionized H.sub.2O (2×150 mL), dried over Na.sub.2SO.sub.4 and concentrated in vacuum to give a crude product which used in the next step without further purification. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.77 (d, J=8.2 Hz, 2H), 7.35 (d, J=8.2 Hz, 2H), 6.76 (b, 1H), 4.01 (dd, J=3.6, 9.7 Hz, 1H), 3.86 (m, 1H), 3.80 (dd, J=7.4, 9.6 Hz, 1H), 2.44 (s, 3H), 2.37-2.12 (m, 3H), 1.77 (m, 1H)

    ##STR00526##

    [2156] Preparation of (S)-(5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate: The title compound was prepared according to the procedure for (R)-(5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate, except L-pyroglutaminol was substituted for (R)-(−)-5-(hydroxymethyl)-2-pyrrolidinone. .sup.1HNMR (400 MHz, CDCl.sub.3) δ 7.71 (d, J=8.3 Hz, 2H), 7.30 (d, J=8.2 Hz, 2H), 5.77 (b, 1H), 3.99 (dd, J=3.5, 9.7 Hz, 1H), 3.86 (m, 1H), 3.79 (dd, J=7.4, 9.6 Hz, 1H), 2.39 (s, 3H), 2.29-2.11 (m, 3H), 1.69 (m, 1H).

    ##STR00527##

    [2157] Preparation of (R)-2-(5-oxopyrrolidin-2-yl)acetonitrile: To a solution of (R)-(5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate (21.25 g, 79 mmol, 1.0 equiv.) in acetonitrile (335 mL) was added potassium cyanide (12.86 g, 197 mmol, 2.5 equiv.). The resulting reaction mixture was then heated to reflux and allowed to reflux overnight. After cooling to 23° C., the reaction mixture was filtered thru a plug of Celite and concentrated in vacuum to give a crude product which was further purified by column chromatography (MeOH/Ethyl acetate, 10%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.23 (b, 1H), 3.93 (m, 1H), 2.54 (d, J=5.7 Hz, 2H), 2.48-2.24 (m, 3H), 1.88 (m, 1H).

    ##STR00528##

    [2158] Preparation of (S)-2-(5-oxopyrrolidin-2-yl)acetonitrile: The title compound was prepared according to the procedure for (R)-2-(5-oxopyrrolidin-2-yl)acetonitrile, except (S)-(5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate was substituted for (R)-(5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.47 (b, 1H), 3.92 (m, 1H), 2.55 (d, J=5.6 Hz, 2H), 2.47-2.24 (m, 3H), 1.86 (m, 1H).

    ##STR00529##

    [2159] Preparation of methyl (R)-2-(5-oxopyrrolidin-2-yl)acetate: A 6 M HCl in methanol solution was prepared via the addition of acetyl chloride (33 mL) to methanol (77 mL). (R)-2-(5-oxopyrrolidin-2-yl)acetonitrile (4.73 g, 38 mmol, 1.0 equiv.) was dissolved in the prepared 6 M methanolic HCl solution (77 mL) and stirred at 23° C. overnight. The reaction mixture was diluted with deionized H.sub.2O (100 mL) and methylene chloride (100 mL) and layers were seperated. The aqueous layer was backwashed with methylene chloride (8×100 mL). The combined organic phase was dried over Na.sub.2SO.sub.4 and concentrated in vacuum to give a crude product that was used in the next step without further purification. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 6.40 (b, 1H), 3.94 (m, 1H), 3.64 (s, 3H), 2.52 (dd, J=4.5, 16.5 Hz, 1H), 2.43 (dd, J=9.0, 16.5 Hz, 1H), 2.35-2.19 (m, 3H), 1.68 (m, 1H).

    ##STR00530##

    [2160] Preparation of methyl (S)-2-(5-oxopyrrolidin-2-yl)acetate: The title compound was prepared according to the procedure for methyl (R)-2-(5-oxopyrrolidin-2-yl)acetate, except (S)-2-(5-oxopyrrolidin-2-yl)acetonitrile was substituted for (R)-2-(5-oxopyrrolidin-2-yl)acetonitrile. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 6.25 (b, 1H), 3.94 (m, 1H), 3.64 (s, 3H), 2.52 (dd, J=4.3, 16.4 Hz, 1H), 2.42 (dd, J=9.2, 16.5 Hz, 1H), 2.32-2.23 (m, 3H), 1.68 (m, 1H).

    ##STR00531##

    [2161] Preparation of (R)-5-(2-hydroxyethyl)pyrrolidin-2-one: To a stirred solution of methyl (R)-2-(5-oxopyrrolidin-2-yl)acetate (0.525 g, 3.3 mmol, 1.0 equiv.) in ethanol (13.4 mL) was added NaBH4 (0.380 g, 10 mmol, 3.0 equiv.) and the resulting mixture was stirred at 23° C. for 5 minutes then at reflux for 1 hour. After cooling to 23° C., the reaction mixture was quenched with 1 mL of acetic acid and the filtered while washing with methanol. The filtrate was concentrated in vacuum to give a crude product which was further purified by column chromatography (MeOH/methanol, 10%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.36 (b, 1H), 4.86-4.09 (b, 1H), 3.82-3.54 (m, 3H), 2.32-2.14 (m, 3H), 1.74-1.53 (m, 3H).

    ##STR00532##

    [2162] Preparation of (S)-5-(2-hydroxyethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-5-(2-hydroxyethyl)pyrrolidin-2-one, except methyl (S)-2-(5-oxopyrrolidin-2-yl)acetate was substituted for methyl (R)-2-(5-oxopyrrolidin-2-yl)acetate. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.04 (b, 1H), 3.81-3.59 (m, 3H), 3.35-2.88 (b, 1H), 2.31-2.14 (m, 3H), 1.75-1.57 (m, 3H).

    ##STR00533##

    [2163] Preparation of tert-butyl (R)-2-(2-(ftert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate: To a stirred solution of (R)-5-(2-hydroxyethyl)pyrrolidin-2-one (3.41 g, 26.4 mmol, 1.0 equiv.) in methylene chloride (50 mL) was added tert-butylchlorodimethylsilane (4.37 g, 29 mmol, 1.1 equiv.) followed by imidazole (1.98 g, 29 mmol, 1.1 equiv.). The resulting mixture was then stirred at 23° C. for 2 hr before being diluted with diethyl ether (100 mL) and washed with deionized H.sub.2O (50 mL). The aqueous layer was backwashed with diethyl ether (2×20 mL). The combined organic phase was dried over Na.sub.2SO.sub.4 and concentrated in vacuum to give a crude intermediate that was dissolved in acetonitrile (132 mL). Triethylamine (5.34 g, 52.8 mmol, 2.0 equiv.), di-tert-butyl dicarbonate (10.95 g, 50.2 mmol, 1.9 equiv.) and 4-dimethylaminopyridine (0.645 g, 5.28 mmol, 0.2 equiv.) were then added and the resulting solution was stirred at 23° C. for 2 hrs. The reaction was diluted with ethyl acetate (200 mL) and washed with sat. NH.sub.4Cl (100 mL). The aqueous layer was backwashed with ethyl acetate (2×20 mL) and the combined organic phase was dried over Na.sub.2SO.sub.4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 20-30%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 4.18 (m, 1H), 3.66 (t, J=6.2 Hz, 2H), 2.54 (ddd, J=9.2, 11.3, 17.6 Hz, 1H), 2.36 (ddd, J=2.4, 9.2, 17.6 Hz, 1H), 2.13-1.82 (m, 3H), 1.66 (m, 1H), 1.47 (s, 9H), 0.83 (s, 9H), 0.00 (s, 6H).

    ##STR00534##

    [2164] Preparation of tert-butyl (S)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate: The title compound was prepared according to the procedure for tert-butyl (R)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate, except (S)-5-(2-hydroxyethyl)pyrrolidin-2-one was substituted for (R)-5-(2-hydroxyethyl)pyrrolidin-2-one. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 4.18 (m, 1H), 3.66 (t, J=6.3 Hz, 2H), 2.54 (ddd, J=9.1, 11.3, 17.6 Hz, 1H), 2.36 (ddd, J=2.4, 9.2, 17.6 Hz, 1H), 2.12-1.85 (m, 3H), 1.66 (m, 1H), 1.47 (s, 9H), 0.83 (s, 9H), 0.00 (s, 6H).

    ##STR00535##

    [2165] Preparation of tert-butyl (R)-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-3,3-diethyl-2-oxopyrrolidine-1-carboxylate: This reaction was performed in oven-dried glassware under a nitrogen atmosphere. A stirred solution of tert-butyl (R)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate (8.0 g, 23.2 mmol, 1.0 equiv.) in dry tetrahydrofuran (35 mL) was cooled to −78° C. and 1M lithium bis(trimethylsilyl)amide solution (tetrahydrofuran, 51 mL, 51 mmol, 2.2 equiv.) was added dropwise while maintaining the reaction temperature below −70° C. The resulting solution was allowed to slowly warm to −30° C. before being cooled back to −78° C. at which iodoethane (8.48 g, 50.5 mmol, 2.15 equiv.) was slowly added dropwise. The resulting solution was slowly warmed to −15° C. and allowed to stir at this temperature for 2 hr before being warmed to 23° C. and allowed to stir for an additional 2.5 hr. The reaction was quenched with sat. NH.sub.4Cl (40 mL) and extracted with ethyl acetate (3×50 mL). The combined organic layers were dried over Na.sub.2SO.sub.4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 0%˜10%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 3.97 (m, 1H), 3.65 (t, J=5.9 Hz, 2H), 2.23 (m, 1H), 1.95 (dd, J=8.6, 13.5 Hz, 1H), 1.66 (dd, J=6.1, 13.5 Hz, 1H), 1.58-1.39 (m, 14H), 0.90-0.74 (m, 15H), 0.00 (s, 3H).

    ##STR00536##

    [2166] Preparation of (R)-5-(2-(benzyloxy)ethyl)-3,3-diethyl-1-tosylpyrrolidin-2-one: The title compound was prepared according to the procedure for tert-butyl (R)-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-3,3-diethyl-2-oxopyrrolidine-1-carboxylate, except (R)-5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one was substituted for tert-butyl (R)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.84 (d, J=8.4 Hz, 2H), 7.33-7.16 (m, 7H), 4.44 (dd, J=12.0, 32.0 Hz, 2H), 4.21 (m, 1H), 3.54 (t, J=5.5 Hz, 2H), 2.69 (m, 1H), 2.34 (s, 3H), 1.95 (dd, J=8.1, 13.5 Hz, 1H), 1.81-1.64 (m, 2H), 1.41 (q, J=7.5 Hz, 2H), 1.33-1.13 (m, 2H), 0.71 (t, J=7.5 Hz, 3H), 0.48 (t, J=7.5 Hz, 3H).

    ##STR00537##

    [2167] Preparation of (S)-5-(2-(benzyloxy)ethyl)-3,3-diethyl-1-tosylpyrrolidin-2-one: The title compound was prepared according to the procedure for tert-butyl (R)-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-3,3-diethyl-2-oxopyrrolidine-1-carboxylate, except (S)-5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one was substituted for tert-butyl (R)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.93 (d, J=8.2 Hz, 2H), 7.40-7.24 (m, 7H), 4.53 (dd, J=11.9, 32.6 Hz, 2H), 4.31 (m, 1H), 3.63 (t, J=5.8 Hz, 2H), 2.78 (m, 1H), 2.42 (s, 3H), 2.04 (dd, J=8.6, 13.5 Hz, 1H), 1.90-1.74 (m, 2H), 1.50 (q, J=7.7 Hz, 2H), 1.44-1.23 (m, 2H), 0.80 (t, J=7.4 Hz, 3H), 0.57 (t, J=7.4 Hz, 3H).

    ##STR00538##

    [2168] Preparation of 5-(2-(benzyloxy)ethyl)-3 ,3-diethyl-1-tosylpyrrolidin-2-one: The title compound was prepared according to the procedure for tert-butyl (R)-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-3,3-diethyl-2-oxopyrrolidine-1-carboxylate, except (rac)-5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one was substituted for tert-butyl (R)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.93 (d, J=8.3 Hz, 2H), 7.41-7.24 (m, 7H), 4.52 (dd, J=12.0, 32.4 Hz, 2H), 4.30 (m, 1H), 3.62 (t, J=5.7 Hz, 2H), 2.78 (m, 1H), 2.41 (s, 3H), 2.04 (dd, J=8.6, 13.5 Hz, 1H), 1.89-1.72 (m, 2H), 1.49 (q, J=7.6 Hz, 2H), 1.43-1.19 (m, 2H), 0.80 (t, J=7.4 Hz, 3H), 0.56 (t, J=7.4 Hz, 3H).

    ##STR00539##

    [2169] Preparation of (R)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one: This reaction was performed in oven-dried glassware under a nitrogen atmosphere. A mixture of Na metal (800 mg) and dry tetrahydrofuran (100 mL) was stirred at 23° C. for 45 minutes. The reaction mixture was cooled to −78° C. followed by the addition of a solution of (R)-5-(2-(benzyloxy)ethyl)-3,3-diethyl-1-tosylpyrrolidin-2-one (1.48 g, 3.45 mmol, 1.0 equiv.) in dry tetrahydrofuran (51 mL). The resulting mixture was allowed to stir at −78° C. for 1.5 hours before being quenched with sat. NH.sub.4Cl (50 mL) and extracted with ethyl acetate (3×40 mL). The combined organic layers were dried over Na.sub.2SO.sub.4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 0% 100%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.31-7.14 (m, 5H), 6.59 (b, 1H), 4.40 (s, 2H), 3.60-3.37 (m, 3H), 1.93 (dd, J=7.5, 13.3 Hz, 1H), 1.75-1.58 (m, 2H), 1.57-1.32 (m, 5H), 0.80 (dt, J=7.6, 18.3 Hz, 6H).

    ##STR00540##

    [2170] Preparation of (S)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one, except (S)-5-(2-(benzyloxy)ethyl)-3,3-diethyl-1-tosylpyrrolidin-2-one was substituted for (R)-5-(2-(benzyloxy)ethyl)-3,3-diethyl-1-tosylpyrrolidin-2-one. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.35-7.13 (m, 5H), 6.06 (b, 1H), 4.42 (s, 2H), 3.62-3.36 (m, 3H), 1.95 (dd, J=7.5, 13.3 Hz, 1H), 1.75-1.59 (m, 2H), 1.57-1.36 (m, 5H), 0.80 (dt, J=7.6, 18.3 Hz, 6H)

    ##STR00541##

    [2171] Preparation of 5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one, except (rac)-5-(2-(benzyloxy)ethyl)-3 ,3-diethyl-1-tosylpyrrolidin-2-one was substituted for (R)-5-(2-(benzyloxy)ethyl)-3,3-diethyl-1-tosylpyrrolidin-2-one. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.28-7.10 (m, 5H), 6.17 (b, 1H), 4.36 (s, 2H), 3.58-3.32 (m, 3H), 1.89 (dd, J=7.3, 13.3 Hz, 1H), 1.68-1.53 (m, 2H), 1.52-1.28 (m, 5H), 0.76 (dt, J=7.4, 19.8 Hz, 6H)

    ##STR00542##

    [2172] Preparation of (R)-5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one: To a round bottom flask was added 10% Pd/C (175 mg, 20% wt) followed by a solution of (R)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one (876 mg, 3.19 mmol, 1 equiv.) in ethanol (17 mL). The system was put under H.sub.2 (1 atm) using a balloon and allowed to stir at 23° C. under a H.sub.2 atmosphere overnight. The reaction was filtered through a plug of Celite and concentrated under reduced pressure. The crude alcohol was dissolved in tetrahydrofuran (12.8 mL) and then triphenylphosphine (1.35 g, 5.13 mmol, 1.6 equiv.) and carbon tetrabromide (1.70 g, 5.13 mmol, 1.6 equiv.) were sequentially added and the reaction was allowed to stir at 23° C. for —3 hours. The resulting mixture was filtered and concentrated in vacuum to give a crude product which was further purified by column chromatography (100% Hexanes then Ethyl acetate/Hexanes, 30%˜50%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.31 (b, 1H), 3.65 (p, J=6.8 Hz, 1H), 3.38 (t, J=6.7 Hz, 2H), 2.12-1.85 (m, 3H), 1.62-1.32 (m, 5H), 0.82 (dt, J=7.5, 17.8 Hz, 6H).

    ##STR00543##

    [2173] Preparation of (S)-5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one, except (S)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one was substituted for (R)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.16 (b, 1H), 3.66 (p, J=6.8 Hz, 1H), 3.38 (t, J=6.8 Hz, 2H), 2.08-1.88 (m, 3H), 1.59-1.35 (m, 5H), 0.82 (dt, J=7.5, 17.8 Hz, 6H).

    ##STR00544##

    [2174] Preparation of 5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one, except 5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one was substituted for (R)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 8.06 (b, 1H), 3.64 (p, J=6.5 Hz, 1H), 3.40 (t, J=6.8 Hz, 2H), 2.06-1.86 (m, 3H), 1.58-1.34 (m, 5H), 0.81 (dt, J=7.5 16.8 Hz 6H).

    ##STR00545##

    [2175] Preparation of (R)-3,3-diethyl-5-(2-hydroxyethyl)pyrrolidin-2-one: A 6M HCl in methanol solution was prepared via the addition of acetyl chloride (18 mL) to methanol (45 mL). tert-Butyl (R)-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-3,3-diethyl-2-oxopyrrolidine-1-carboxylate (3.98 g, 10 mmol, 1.0 equiv.) was dissolved in the prepared 6M methanolic HCl solution (45 mL) and stirred at 23° C. for 30 minutes. The resulting reaction solution was diluted with methanol and then concentrated in vacuo to give a crude product which used in the next step without further purification. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.28 (b, 1H), 3.82 (m, 2H), 3.68 (m, 1H), 2.07 (dd, J=7.7, 13.4 Hz, 1H), 1.70 (m, 2H), 1.61 (dd, J=7.7, 13.3 Hz, 1H), 1.57-1.39 (m, 4H), 0.84 (dt, J=7.5, 18.0 Hz, 6H).

    ##STR00546##

    [2176] Preparation of (R)-2-(4,4-diethyl-5-oxopyrrolidin-2-yl)ethyl 4-methylbenzenesulfonate: To a cooled solution of (R)-3,3-diethyl-5-(2-hydroxyethyl)pyrrolidin-2-one (1.85 g, 10 mmol, 1.0 equiv.) and triethylamine (2.02 g, 20 mmol, 2.0 equiv.) in tetrahydrofuran/methylene chloride (50 mL:50 mL) at 0° C. was added 4-toluenesulfonyl chloride (2.85 g, 15 mmol, 1.5 equiv.) followed by 4-dimethylaminopyridine (0.122 g, 1 mmol, 0.2 equiv.). The resulting reaction mixture was stirred at 0° C. for 5 minutes before being warmed to 23° C. and allowed to stir for 72 hours. Then, the reaction mixture was diluted with dichloromethane (50 mL), washed with 1N HCl (1×50 mL) and deionized H.sub.2O (2×50 mL), dried over Na.sub.2SO.sub.4 and concentrated in vacuo to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 20%˜75%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.22 (d, J=8.2 Hz, 2H), 7.29 (d, J=7.9 Hz, 2H), 6.05 (b, 1H), 4.04 (t, J=5.8 Hz, 2H), 3.53 (p, J=6.8 Hz, 1H), 2.38 (s, 3H), 1.94 (dd, J=7.6, 13.2 Hz, 1H), 1.75 (q, J=6.0 Hz, 2H), 1.53-1.32 (m, 5H), 0.78 (dt, J=7.5, 21.5 Hz, 6H).

    ##STR00547##

    [2177] Preparation of 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one: To a small vial was added 5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one (50 mg, 0.201 mmol, 1 equiv.), 1-phenylpiperazine (69 mg, 0.422 mmol, 2.1 eq.) and tetrahydrofuran (3.5 mL). The reaction mixture was allowed to reflux overnight was then cooled to 23° C. The mixture was filtered, washed with tetrahydrofuran, and the filtrate was concentrated in vacuo to give a crude product which was further purified by column chromatography (MeOH/DCM, 0%˜10%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.26 (m, 2H), 6.93 (d, J=8.1 Hz, 2H), 6.86 (t, J=7.2 Hz, 1H), 6.76 (b, 1H), 3.58 (m, 1H), 3.22 (t, J=5.0 Hz, 4H), 2.69 (m, 2H), 2.60-2.40 (m, 4H), 2.06 (dd, J=7.2, 13.1 Hz, 1H), 1.78-1.43 (m, 7H), 0.91 (dt, J=7.5, 13.5 Hz, 6H). LC/MS [M+H]=m/z 330.2

    ##STR00548##

    [2178] Preparation of 3,3-diethyl-5-(2-(4-(p-tolyppiperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 1-(4-methylphenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.07 (d, J=8.1 Hz, 2H), 6.84 (d, J=8.6 Hz, 2H), 6.74 (b, 1H), 3.58 (m, 1H), 3.16 (t, J=5.0 Hz, 4H), 2.69 (m, 2H), 2.56-2.40 (m, 4H), 2.27 (s, 3H), 2.05 (dd, J=7.3, 13.3 Hz, 1H), 1.78-1.43 (m, 7H), 0.91 (dt, J=7.4, 13.8 Hz, 6H). LC/MS [M+H]=m/z 344.2

    ##STR00549##

    [2179] Preparation of 3,3-diethyl-5-(2-(4-(4-hydroxyphenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(4-hydroxyphenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.23 (b, 1H), 6.73 (d, J=9.1 Hz, 2H), 6.68 (d, J=9.0 Hz, 2H), 3.59 (m, 1H), 3.04-2.87 (b, 4H), 2.69 (m, 2H), 2.57 (m, 1H), 2.45 (m, 3H), 2.06 (dd, J=7.4, 13.2 Hz, 1H), 1.75-1.43 (m, 7H), 0.91 (dt, J=7.5, 14.3 Hz, 6H). LC/MS [M+H]=m/z 346.2

    ##STR00550##

    [2180] Preparation of 3 ,3-diethyl-5-(2-(4-(2-isopropylphenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(2-isopropylphenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.26 (d, J=7.5 Hz, 1H), 7.20-7.04 (m, 3H), 6.79 (b, 1H), 3.59 (m, 1H), 3.49 (sept. J=6.8 Hz, 1H), 2.93 (t, J=4.6 Hz, 4H), 2.83-2.60 (b, 2H), 2.60-2.42 (m, 4H), 2.07 (dd, J=7.4, 13.1 Hz, 1H), 1.78-1.45 (m, 7H), 1.23 (dd, J=2.4, 6.9 Hz, 6H), 0.92 (dt, J=7.4, 18.3 Hz, 6H). LC/MS [M+H]=m/z 372.2

    ##STR00551##

    [2181] Preparation of 5-(2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(4-chlorophenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1HNMR (400 MHz, CDCl.sub.3) δ 7.19 (d, J=9.0 Hz, 2H), 6.83 (d, J=9.0 Hz, 2H), 6.73 (b, 1H), 3.57 (m, 1H), 3.17 (t, J=5.0 Hz, 4H), 2.68 (m, 2H), 2.58-2.40 (m, 4H), 2.05 (dd, J=7.4, 13.2 Hz, 1H), 1.76-1.42 (m, 7H), 0.90 (dt, J=7.4, 13.7 Hz, 6H). LC/MS [M+H]=m/z 364.2

    ##STR00552##

    [2182] Preparation of 3,3-diethyl-5-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 1-(4-fluorophenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 6.99-6.90 (m, 2H), 6.89-6.83 (m, 2H), 6.79 (b, 1H), 3.56 (m, 1H), 3.12 (t, J=4.9 Hz, 4H), 2.68 (m, 2H), 2.58-2.39 (m, 4H), 2.04 (dd, J=7.5, 13.2 Hz, 1H), 1.74-1.42 (m, 7H), 0.89 (dt, J=7.4, 13.9 Hz, 6H). LC/MS [M+H]=m/z 348.2

    ##STR00553##

    [2183] Preparation of 3,3-diethyl-5-(2-(4-(2-morpholinophenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 4-(2-(piperazin-1-yl)phenyl)morpholine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 6.91-6.84 (m, 2H), 6.84-6.74 (m, 2H), 6.51 (b, 1H), 3.71 (t, J=4.8 Hz, 4H), 3.46 (m, 1H), 3.36-2.77 (b, 8H), 2.74-2.07 (b, 6H), 1.94 (dd, J=7.5, 13.2 Hz, 1H), 1.65-1.31 (m, 7H), 0.79 (dt, J=7.3, 15.9 Hz, 6H). LC/MS [M+H]=m/z 415.2

    ##STR00554##

    [2184] Preparation of 3,3-diethyl-5-(2-(4-(4-methyl-2-morpholinophenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 4-(5-methyl-2-(piperazin-1-yl)phenyl)morpholine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 6.88-6.78 (m, 2H), 6.77-6.67 (m, 2H), 3.84 (t, J=4.6 Hz, 4H), 3.59 (m, 1H), 3.42-2.86 (b, 8H), 2.80-2.32 (b, 6H), 2.29 (s, 3H), 2.06 (dd, J=7.5, 13.3 Hz, 1H), 1.78-1.44 (m, 7H), 0.92 (dt, J=7.4, 15.6 Hz, 6H). LC/MS [M+H]=m/z 429.2

    ##STR00555##

    [2185] Preparation of (R)-3 ,3-diethyl-5-(2-(4-(p-tolyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except (R)-5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one was substituted 5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one and 1-(4-methylphenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.07 (d, J=8.2 Hz, 2H), 6.84 (d, J=8.5 Hz, 2H), 6.41 (b, 1H), 3.57 (m, 1H), 3.16 (t, J=4.9 Hz, 4H), 2.69 (m, 2H), 2.58-2.40 (m, 4H), 2.27 (s, 3H), 2.05 (dd, J=7.3, 13.1 Hz, 1H), 1.77-1.43 (m, 7H), 0.91 (dt, J=7.4, 13.7 Hz, 6H). LC/MS [M+H]=m/z 344.2

    ##STR00556##

    [2186] Preparation of (S)-3 ,3-diethyl-5-(2-(4-(p-tolyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except (S)-5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one was substituted 5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one and 1-(4-methylphenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.00 (d, J=8.5 Hz, 2H), 6.76 (d, J=8.5 Hz, 2H), 6.41 (b, 1H), 3.50 (m, 1H), 3.09 (t, J=5.1 Hz, 4H), 2.64 (m, 2H), 2.54-2.32 (m, 4H), 2.19 (s, 3H), 1.98 (dd, J=7.3, 13.1 Hz, 1H), 1.69-1.69 (m, 7H), 0.83 (dt, J=7.4, 14.5 Hz, 6H). LC/MS [M+H]=m/z 344.2

    ##STR00557##

    [2187] Preparation of (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one: To a small vial was added (R)-2-(4,4-diethyl-5-oxopyrrolidin-2-yl)ethyl 4-methylbenzenesulfonate (75 mg, 0.22 mmol, 1 equiv.) and 1-phenylpiperazine (76 mg, 0.46 mmol, 2.1 equiv.) then both were dissolved in acetonitrile (2.2 mL). Then K.sub.2CO.sub.3 (77 mg, 0.55 mmol, 2.5 equiv.) was added, the reaction was allowed to stir at 80° C. overnight, and then cooled to 23° C. The mixture was filtered, washed with acetonitrile and the filtrate was concentrated in vacuo to give a crude product which was by further purified by column chromatography (MeOH/DCM, 0%˜10%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.27 (m, 2H), 6.94 (d, J=8.1 Hz, 2H), 6.87 (t, J=7.2 Hz, 1H), 6.65 (b, 1H), 3.59 (m, 1H), 3.23 (t, J=5.0 Hz, 4H), 2.71 (m, 2H), 2.61-2.41 (m, 4H), 2.07 (dd, J=7.4, 13.1 Hz, 1H), 1.77-1.45 (m, 7H), 0.92 (dt, J=7.4, 14.0 Hz, 6H). LC/MS [M+H]=m/z 330.2.

    ##STR00558##

    [2188] Preparation of (R)-3,3-diethyl-5-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(4-fluorophenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.00-6.91 (m, 2H), 6.91-6.82 (m, 2H), 6.74 (b, 1H), 3.57 (m, 1H), 3.13 (t, J=5.0 Hz, 4H), 2.70 (m, 2H), 2.60-2.41 (m, 4H), 2.05 (dd, J=7.3, 13.1 Hz, 1H), 1.76-1.44 (m, 7H), 0.90 (dt, J=7.5, 14.1 Hz, 6H). LC/MS [M+H]=m/z 348.2

    ##STR00559##

    [2189] Preparation of (R)-5-(2-(4-(3,4-dichlorophenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(3,4-dichlorophenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1HNMR (400 MHz, CDCl.sub.3) δ 7.26 (d, J=9.0 Hz, 1H), 6.95 (d, J=2.9 Hz, 1H), 6.79-2.67 (b, 2H), 3.58 (m, 1H), 3.18 (t, J=5.0 Hz, 4H), 2.67 (m, 2H), 2.59-2.39 (m, 4H), 2.05 (dd, J=7.4, 13.1 Hz, 1H), 1.75-1.42 (m, 7H), 0.90 (dt, J=7.4, 13.7 Hz, 6H). LC/MS [M+H]=m/z 398.2.

    ##STR00560##

    [2190] Preparation of (R)-5-(2-(4-(3-chloro-4-fluorophenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(3-chloro-4-fluorophenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1HNMR (400 MHz, CDCl.sub.3) δ 7.01 (t, J=8.8 Hz, 1H), 6.91 (dd, J=2.9, 6.2 Hz, 1H), 6.79-6.66 (b, 2H), 3.57 (m, 1H), 3.14 (t, J=5.0 Hz, 4H), 2.68 (m, 2H), 2.60-2.40 (m, 4H), 2.05 (dd, J=7.5, 13.2 Hz, 1H), 1.75-1.43 (m, 7H), 0.90 (dt, J=7.3, 13.9 Hz, 6H). LC/MS [M+H]=m/z 382.2.

    ##STR00561##

    [2191] Preparation of (R)-5-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(3-chlorophenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.16 (t, J=8.1 Hz, 1H), 6.87 (t, J=2.1 Hz, 1H), 6.83-6.75 (m, 2H), 6.71 (b, 1H), 3.58 (m, 1H), 3.21 (t, J=5.0 Hz, 4H), 2.68 (m, 2H), 2.60-2.40 (m, 4H), 2.06 (dd, J=7.2, 13.1 Hz, 1H), 1.76-1.44 (m, 7H), 0.91 (dt, J=7.4, 13.8 Hz, 6H). LC/MS [M+H]=m/z 364.2

    ##STR00562##

    [2192] Preparation of (R)-5-(2-(4-(2-chlorophenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(2-chlorophenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.27 (dd, J=1.5, 7.9 Hz, 1H), 7.14 (td, J=1.5, 7.7 Hz, 1H), 6.98 (dd, J=1.5, 8.0 Hz, 1H), 6.89 (td, J=1.5, 7.7 Hz, 1H), 6.63 (b, 1H), 3.50 (m, 1H), 3.18-2.83 (b, 4H), 2.77-2.56 (b, 2H), 2.55-2.31 (m, 4H), 1.98 (dd, J=7.4, 13.1 Hz, 1H), 1.69-1.36 (m, 7H), 0.83 (dt, J=7.4, 16.9 Hz, 6H). LC/MS [M+H]=m/z 364.2

    ##STR00563##

    [2193] Preparation of (R)-5-(2-(4-(3-fluorophenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(3-fluorophenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.10 (m, 1H), 6.64-6.54 (b, 2H), 6.50 (dt, J=2.4, 12.4 Hz, 1H), 6.45 (td, J=2.3, 8.2 Hz, 1H), 3.50 (m, 1H), 3.14 (t, J=5.0 Hz, 4H), 2.60 (m, 2H), 2.51-2.30 (m, 4H), 1.98 (dd, J=7.3, 13.2 Hz, 1H), 1.67-1.36 (m, 7H), 0.83 (dt, J=7.3, 14.0 Hz, 6H). LC/MS [M+H]=m/z 348.2

    ##STR00564##

    [2194] Preparation of (R)-5-(2-(4-(2-methylphenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(2-methylphenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.17 (m, 2H), 7.04 (dd, J=1.2, 8.5 Hz, 1H), 6.99 (td, J=1.2, 7.4 Hz, 1H), 6.73 (b, 1H), 3.59 (m, 1H), 3.03-2.89 (b, 4H), 2.83-2.62 (b, 2H), 2.62-2.38 (m, 4H), 2.31 (s, 3H), 2.07 (dd, J=7.5, 13.1 Hz, 1H), 1.77-1.45 (m, 7H), 0.92 (dt, J=7.5, 17.5 Hz, 6H). LC/MS [M+H]=m/z 344.2

    ##STR00565##

    [2195] Preparation of (R)-5-(2-(4-(3-methylphenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 1-(3-methylphenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1HNMR (400 MHz, CDCl.sub.3) δ 7.16 (t, J=7.8 Hz, 1H), 6.80-6.68 (m, 3H), 6.63 (b, 1H), 3.59 (m, 1H), 3.22 (t, J=5.0 Hz, 4H), 2.71 (m, 2H), 2.61-2.41 (m, 4H), 2.33 (s, 3H), 2.07 (dd, J=7.4, 13.2 Hz, 1H), 1.78-1.45 (m, 7H), 0.92 (dt, J=7.4, 14.0 Hz, 6H). LC/MS [M+H]=m/z 344.2

    ##STR00566##

    [2196] Preparation of tert-butyl (R)-3,3-diallyl-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-2-oxopyrrolidine-1-carboxylate: This reaction was performed in oven-dried glassware under a nitrogen atmosphere. A stirred solution of tert-butyl (R)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate (10.0 g, 29.0 mmol, 1.0 equiv.) in dry tetrahydrofuran (43 mL) was cooled to −78° C. and 1M lithium bis(trimethylsilyl)amide solution (tetrahydrofuran, 63.8 mL, 63.8 mmol, 2.2 equiv.) was added dropwise while maintaining the reaction temperature below −70° C. The resulting solution was allowed to slowly warm to −30° C. before being cooled back to −78° C. at which time allyl iodide (10.71 g, 63.8 mmol, 2.2 equiv.) was slowly added dropwise. The resulting solution was slowly warmed to −20° C. and then quenched with sat. NH.sub.4Cl (75 mL) and extracted with ethyl acetate (3×75 mL). The combined organic layers were dried over Na.sub.2SO.sub.4 and concentrated in vacuo to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 0% 10%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 5.77-5.58 (m, 2H), 5.12-4.99 (m, 4H), 3.96 (m, 1H), 3.63 (t, J=6.2 Hz, 2H), 2.40-2.09 (m, 5H), 2.01 (dd, J=8.6, 13.6 Hz, 1H), 1.70 (dd, J=6.4, 13.6 Hz, 1H), 1.57-1.42 (m, 10H), 0.84 (s, 9H), 0.00 (s, 6H).

    ##STR00567##

    [2197] Preparation of tert-butyl (S)-3,3-diallyl-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-2-oxopyrrolidine-1-carboxylate: The title compound was prepared according to the procedure for tert-butyl (R)-3,3-diallyl-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-2-oxopyrrolidine-1-carboxylate, except tert-butyl (S)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate was substituted for tert-butyl (R)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 5.79-5.60 (m, 2H), 5.13-4.98 (m, 4H), 3.96 (m, 1H), 3.62 (t, J=6.2 Hz, 2H), 2.40-2.10 (m, 5H), 2.00 (dd, J=8.6, 13.6 Hz, 1H), 1.69 (dd, J=6.3, 13.6 Hz, 1H), 1.58-1.42 (m, 10H), 0.83 (s, 9H), 0.00 (s, 6H).

    ##STR00568##

    [2198] Preparation of tert-butyl (R)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspiro[4.4]non-7-ene-2-carboxylate: To a stirred solution of tert-butyl (R)-3,3-diallyl-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-2-oxopyrrolidine-1-carboxylate (10.03 g, 23.6 mmol, 1.0 equiv.) in methylene chloride (200 mL) was added benzylidene-bis(tricyclohexyl(phophine) dichlororuthenium (0.388 g, 0.472 mmol, 2 mol %). The resulting solution was allowed to stir at 23° C. for 4 hours before being concentrated in vacuo to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 0%˜20%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 5.56 (m, 2H), 4.08 (m, 1H), 3.66 (t, J=6.1 Hz, 2H), 2.86 (m, 2H), 2.36 (m, 1H), 2.29-2.14 (m, 2H), 2.09 (dd, J=8.0, 13.0 Hz, 1H), 1.98 (dd, J=3.9, 13.0 Hz, 1H), 1.60 (m, 1H), 1.48 (s, 9H), 0.83 (s, 9H), 0.00 (s, 6H).

    ##STR00569##

    [2199] Preparation of tert-butyl (S)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspiro[4.4]non-7-ene-2-carboxylate: The title compound was prepared according to the procedure for tert-butyl (R)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspiro[4.4]non-7-ene-2-carboxylate, except tert-butyl (S)-3,3-diallyl-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-2-oxopyrrolidine-1-carboxylate was substituted for tert-butyl (R)-3,3-diallyl-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-2-oxopyrrolidine-1-carboxylate. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 5.56 (m, 2H), 4.08 (m, 1H), 3.66 (t, J=6.1 Hz, 2H), 2.87 (m, 2H), 2.36 (m, 1H), 2.30-2.14 (m, 2H), 2.09 (dd, J=8.0, 13.1 Hz, 1H), 1.98 (dd, J=3.9, 13.1 Hz, 1H), 1.60 (m, 1H), 1.48 (s, 9H), 0.83 (s, 9H), 0.00 (s, 6H).

    ##STR00570##

    [2200] Preparation of tert-butyl (R)-8-benzyl-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-2-carboxylate: A stirred solution of tert-butyl (R)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspirop.41non-7-ene-2-carboxylate (9.04 g, 22.8 mmol, 1.0 equiv.) in methylene chloride (235 mL) and methanol (7.7 mL) was cooled to −78° C. and a gaseous stream of O.sub.3/O.sub.2 was bubbled through the solution until the color developed a purple tint (45 minutes). Residual O.sub.3 was removed by bubbling O.sub.2 through the solution for 10 minutes. At −78° C., NaBH(OAc).sub.3 (4.93 g, 23.2 mmol, 1.02 equiv.) was added and the reaction mixture was allowed to warm to 23° C. and stir for 45 minutes. Next, BnNH.sub.2 (2.70 g, 25.2 mmol, 1.1 equiv.) and NaBH(OAc).sub.3 (9.72 g, 45.8 mmol, 2.0 equiv.) were sequentially added and the reaction was stirred at 23° C. overnight. The resulting mixture was filtered and concentrated in vacuo to give a crude product which was further purified by column chromatography (2M Ammonia in MeOH/methylene chloride, 0%˜2%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.34-7.19 (m, 5H), 4.03 (m, 1H), 3.65 (t, J=5.9 Hz, 2H) 3.54 (b, 2H), 2.94 (b, 2H), 2.41 (b, 2H), 2.19 (m, 1H), 2.08-1.86 (m, 3H), 1.79 (dd, J=4.7, 13.5 Hz, 1H), 1.60-1.40 (m, 12H), 0.84 (s, 9H), 0.00 (s, 6H).

    ##STR00571##

    [2201] Preparation of tert-butyl (S)-8-benzyl-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-2-carboxylate: The title compound was prepared according to the procedure for tert-butyl (R)-8-benzyl-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-2-carboxylate, except tert-butyl (S)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspirop.41non-7-ene-2-carboxylate was substituted for tert-butyl (R)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspiro[4.4]non-7-ene-2-carboxylate. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.32-7.14 (m, 5H), 4.02 (m, 1H), 3.65 (t, J=5.9 Hz, 2H) 3.54 (b, 2H), 2.84 (b, 2H), 2.41 (b, 2H), 2.19 (m, 1H), 2.05-1.86 (m, 3H), 1.80 (dd, J=4.7, 13.3 Hz, 1H), 1.60-1.39 (m, 12H), 0.84 (s, 9H), 0.00 (s, 6H).

    ##STR00572##

    [2202] Preparation of (R)-3-(2-hydroxyethyl)-2,8-diazaspiro[4.5]decan-1-one: To a round bottom flask was added 10% Pd/C (1.27 g, 20% by weight) followed by a solution of tert-butyl (R)-8-benzyl-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2,8-diazaspiro [4 .5]decane-2-carboxylate (6.32 g, 12.5 mmol, 1 equiv.) in methanol (83 mL). The reaction was put under H.sub.2 (1 atm) using a balloon and stirred at 23° C. overnight. The reaction was filtered through a plug of Celite and concentrated filtrate under reduced pressure to give a crude intermediate.

    [2203] A 6M HCl in methanol solution was prepared via the addition of acetyl chloride (60 mL) to methanol (160 mL). The crude intermediate was dissolved in the prepared 6M methanolic HCl solution (160 mL) and stirred at 23° C. for 30 minutes before being diluted with methanol and concentrated in vacuo to produce a crude product as an HCl salt. The product was free based by stirring with Amberlite IRN-78 base resin in methanol (˜150 mL) for 15 minutes followed by filtration and concentrated in vacuo to produce a crude product that was used in the next step without further purification. .sup.1H NMR (400 MHz, MeOD) δ 3.82-3.61 (m, 3H), 3.02 (m, 2H), 2.76 (td, J=2.9, 12.9 Hz, 1H), 2.64 (td, J=2.9, 12.9 Hz, 1H), 2.46 (dd, J=7.0, 13.0 Hz, 1H), 1.93 (td, J=4.4, 12.7 Hz, 1H), 1.86-1.74 (m, 1H), 1.74-1.64 (m, 2H), 1.60 (dd, J=8.2, 12.9 Hz, 1H), 1.49 (d, J=13.2 Hz, 1H), 1.36 (d, J=13.6 Hz, 1H).

    ##STR00573##

    [2204] Preparation of (S)-3-(2-hydroxyethyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-3-(2-hydroxyethyl)-2,8-diazaspiro[4 .5]decan-1-one, except tert-butyl (R)-8-benzyl-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2,8-diazaspiro [4 .5] decane-2-carboxylate was substituted for tert-butyl (S)-8-benzyl-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-2-carboxylate .sup.1H NMR (400 MHz, MeOD) δ 3.82-3.60 (m, 3H), 3.02 (m, 2H), 2.76 (td, J=2.9, 12.9 Hz, 1H), 2.64 (td, J=2.9, 12.9 Hz, 1H), 2.46 (dd, J=7.1, 13.2 Hz, 1H), 1.93 (td, J=3.7, 12.3 Hz, 1H), 1.86-1.75 (m, 1H), 1.75-1.64 (m, 2H), 1.60 (dd, J=8.0, 12.7 Hz, 1H), 1.49 (d, J=13.1 Hz, 1H), 1.37 (d, J=13.0 Hz, 1H).

    ##STR00574##

    [2205] Preparation of tert-butyl (R)-3-(2-hydroxyethyl)-1-oxo-2,8-diazaspiro [4.5]decane-8-carboxylate: To a solution of (R)-3-(2-hydroxyethyl)-2,8-diazaspiro[4.5]decan-1-one (2.2 g, 11.0 mmol, 1.0 equiv.) and triethylamine (1.12 g, 11.0 mmol, 1.0 equiv.) in methylene chloride (113 mL) and methanol (3 mL) was added di-tert-butyl dicarbonate (2.4 g, 11.0 mmol, 1.0 equiv.). The resulting solution was allowed to stir at 23° C. overnight before being concentrated in vacuo to produce a crude product that was used in the next step without further purification. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 6.93 (b, 1H), 4.15-3.55 (b, 6H), 3.15-2.74 (m, 2H), 2.29 (dd, J=6.7, 12.5 H, 1H), 2.00-1.82 (m, 1H), 1.80-1.60 (m, 3H), 1.58-1.29 (m, 12).

    ##STR00575##

    [2206] Preparation of tert-butyl (S)-3-(2-hydroxyethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate: The title compound was prepared according to the procedure for (tert-butyl (R)-3-(2-hydroxyethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate, except (S)-3-(2-hydroxyethyl)-2,8-diazaspiro[4 .5]decan-1-one was substituted for (R)-3-(2-hydroxyethyl)-2,8-diazaspiro[4.5]decan-1-one. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 6.53 (b, 1H), 4.06-3.56 (b, 6H), 3.05-2.77 (m, 2H), 2.25 (dd, J=6.7, 12.9 H, 1H), 1.93-1.80 (m, 1H), 1.74-1.56 (m, 3H), 1.52-1.24 (m, 12).

    ##STR00576##

    [2207] Preparation of (S)-3-(2-hydroxyethyl)-2-azaspiro[4.4]nonan-1-one: To a round bottom flask was added 10% Pd/C (0.60 g, 20% by wieght) followed by a solution of tert-butyl (S)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspiro[4.4]non-7-ene-2-carboxylate (0.30 g, 0.758 mmol, 1 equiv.) in methanol (7.5 mL). The reaction was put under H.sub.2 (1 atm) using a balloon and stirred at 23° C. for 4 hrs. The reaction was filtered through a plug of Celite and concentrated filtrate under reduced pressure to give a crude intermediate.

    [2208] A 6M HCl in methanol solution was prepared via the addition of acetyl chloride (3 mL) to methanol (7.5 mL). The crude intermediate was dissolved in the prepared 6M methanolic HCl solution (7.5 mL) and stirred at 23° C. for 30 minutes before being diluted with methanol and concentrated in vacuo to produce a crude product was used in the next step without further purification. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 6.95 (b, 1H), 3.99 (b, 1H), 3.76 (m, 1H), 3.64 (m, 2H), 2.09 (dd, J=6.6, 12.6 Hz, 1H), 2.01 (m, 1H), 1.81-1.45 (m, 9H), 1.37 (m, 1H).

    ##STR00577##

    [2209] Preparation of (S)-3-(2-hydroxyethyl)-2-azaspiro[4.4]non-7-en-1-one: A 6M HCl in methanol solution was prepared via the addition of acetyl chloride (3 mL) to methanol (7.5 mL). tert-Butyl (S)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspiro[4.4]non-7-ene-2-carboxylate (0.30 g, 0.758 mmol, 1 equiv.) was dissolved in the prepared 6M methanolic HCl solution (7.5 mL) and stirred at 23° C. for —30 minutes before being diluted with methanol and concentrated in vacuo to produce a crude product was used in the next step without further purification. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.04 (b, 1H), 5.62 (m, 1H), 5.52 (m, 1H), 3.83-3.71 (m, 2H), 3.70-3.57 (m, 2H), 2.90 (dp, J=2.4, 16.6 Hz, 1H), 2.58 (dp, J=2.4, 16.3 Hz, 1H), 2.33 (d, J=16.4 Hz, 1H), 2.22 (dd, J=6.2, 12.4 Hz, 1H), 2.14 (d, J=16.2 Hz, 1H), 1.71-1.54 (m, 3H).

    ##STR00578##

    [2210] Preparation of tert-butyl (R)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate: To a cooled solution of tert-butyl (R)-3-(2-hydroxyethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate (3.2 g, 10.7 mmol, 1.0 equiv.) and triethylamine (2.16 g, 21.4 mmol, 2.0 equiv.) in tetrahydrofuran/methylene chloride (46 mL:46 mL) at 0° C. was added 4-toluenesulfonyl chloride (3.06 g, 16 mmol, 1.5 equiv.) followed by 4-dimethylaminopyridine (0.131 g, 1.07 mmol, 0.2 equiv.). The resulting reaction mixture was stirred at 0° C. for 5 minutes before being warmed to 23° C. and allowed to stir overnight. Then, the reaction mixture was diluted with dichloromethane (50 mL) and washed with deionized H.sub.2O (1×50 mL). The aqueous layer was backwashed with methylene chloride (2×50 mL). The combined organic phase was dried over Na.sub.2SO.sub.4 and concentrated in vacuo to give a crude product which was further purified by HPLC (CH.sub.3CN/H.sub.2O, 0.1% Formic acid), 0%˜100%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.81 (d, J=8.3 Hz, 2H), 7.38 (d, J=8.2 Hz, 2H), 6.11 (b, 1H), 4.14 (m, 2H), 4.07-3.89 (b, 2H), 3.72 (p, J=6.8 Hz, 1H), 2.97 (m, 2H), 2.48 (s, 3H), 2.28 (dd, J=6.9, 12.8 Hz, 1H), 1.97-1.83 (m, 3H), 1.75 (m, 1H), 1.56-1.30 (m, 12H).

    ##STR00579##

    [2211] Preparation of tert-butyl (S)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate: The title compound was prepared according to the procedure for tert-butyl (R)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate, except tert-butyl (S)-3-(2-hydroxyethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate was substituted for tert-butyl (R)-3-(2-hydroxyethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.77 (d, J=8.3 Hz, 2H), 7.34 (d, J=8.2 Hz, 2H), 7.05 (b, 1H), 4.11 (m, 2H), 4.05-3.78 (b, 2H), 3.68 (p, J=6.8 Hz, 1H), 2.92 (m, 2H), 2.43 (s, 3H), 2.22 (dd, J=6.8, 12.9 Hz, 1H), 1.93-1.76 (m, 3H), 1.68 (m, 1H), 1.53-1.24 (m 12H).

    ##STR00580##

    [2212] Preparation of (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate: To a cooled solution of (S)-3-(2-hydroxyethyl)-2-azaspiro[4.4]non-7-en-1-one (0.140 g, 0.758 mmol, 1.0 equiv.) and N-methylimidazole (0.312 g, 3.8 mmol, 5.0 equiv.) in methylene chloride (2.5 mL) at 0° C. was added a solution of 4-toluenesulfonyl chloride (0.217 g, 1.14 mmol, 1.5 equiv.) in methylene chloride (3.5 mL). The resulting reaction mixture was stirred at 0° C. for 5 min utesbefore being warmed to 23° C. and allowed to stir overnight. Then, the reaction mixture was quenched with 1N HCl (1×5 mL) and extracted with methylene chloride (3×15 mL). The combined organic phase was dried over Na.sub.2SO.sub.4 and concentrated in vacuo to give a crude product which was further by column chromatography (Ethyl acetate/Hexanes, 40%˜100%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.71 (d, J=8.3 Hz, 2H), 7.27 (d, J=8.1 Hz, 2H), 6.97 (b, 1H), 5.58 (m, 1H), 5.51 (m, 1H), 4.04 (m, 2H), 3.58 (p, J=6.8 Hz, 1H), 2.86 (dp, J=2.3, 16.5 Hz, 1H), 2.58 (dp, J=2.3, 16.3 Hz, 1H), 2.37 (s, 3H), 2.25 (d, J=16.1 Hz, 1H), 2.19-2.04 (m, 2H), 1.86-1.67 (m, 2H), 1.54 (dd, J=7.7, 12.5 Hz, 1H).

    ##STR00581##

    [2213] Preparation of (S)-2-(1-oxo-2-azaspiro[4.4]nonan-3-yl)ethyl 4-methylbenzenesulfonate: The title compound was prepared according to the procedure for (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate, except (S)-3-(2-hydroxyethyl)-2-azaspiro[4.4]nonan-1-one was substituted for (S)-3-(2-hydroxyethyl)-2-azaspiro[4.4]non-7-en-1-one. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.78 (d, J=8.2 Hz, 2H), 7.34 (d, J=8.1 Hz, 2H), 6.87 (b, 1H), 4.10 (m, 2H), 3.60 (p, J=6.7 Hz, 1H), 2.44 (s, 3H), 2.12-1.97 (m, 2H), 1.94-1.68 (m, 5H), 1.66-1.45 (m, 4H), 1.40 (m, 1H).

    ##STR00582##

    [2214] Preparation of (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl ethyl)-2-azaspiro[4.4]non-7-en-1-one: To a small vial was added (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate (50 mg, 0.15 mmol, 1 equiv.) and 1-(4-fluorophenyl)piperazine (57 mg, 0.31 mmol, 2.1 equiv.) then both were dissolved in acetonitrile (1.5 mL). Then K2CO3 (52 mg, 0.37 mmol, 2.5 equiv.) was added, the reaction was allowed to stir at 80° C. overnight, and then cooled to 23° C. The mixture was filtered, washed with acetonitrile and filtrate was concentrated in vacuo to give a crude product which was by further purified by column chromatography (MeOH/methylene chloride, 0%˜10%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.00-6.82 (m, 5H), 5.70 (m, 1H), 5.59 (m, 1H), 3.63 (m, 1H), 3.13 (t, J=4.9 Hz, 4H), 3.02 (dp, J=2.5, 16.5 Hz, 1H), 2.76-2.62 (m, 3H), 2.61-2.43 (m, 4H), 2.39 (d, J=16.6 Hz, 1H), 2.29 (dd, J=6.1, 12.4 Hz, 1H), 2.20 (d, J=16.4 Hz, 1H), 1.80-1.57 (m, 3H). LC/MS [M+H]=m/z 344.2

    ##STR00583##

    [2215] Preparation of (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl ethyl)-2-azaspiro[4.4]non-7-en-1-one: The title compound was prepared according to the procedure for (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2-azaspiro[4 .4]non-7-en-1-one, except 1-(3-chlorophenyl)piperazine was substituted for 1-(4-fluorophenyl)piperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.08 (t, J=8.0 Hz, 1H), 6.79 (t, J=2.1 Hz, 1H), 6.77-6.65 (m, 3H). 5.60 (m, 1H), 5.51 (m, 1H), 3.56 (m, 1H), 3.13 (t, J=5.1 Hz, 4H), 2.95 (dp, J=2.4, 16.6 Hz, 1H), 2.68-2.54 (m, 3H), 2.54-2.35 (m, 4H), 2.31 (d, J=16.0 Hz, 1H), 2.22 (dd, J=6.1, 12.3 Hz, 1H), 2.13 (d, J=16.5 Hz, 1H), 1.72-1.49 (m, 3H). LC/MS [M+H]=m/z 360.2.

    ##STR00584##

    [2216] Preparation of (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl ethyl)-2-azaspiro[4.4]nonan-1-one: The title compound was prepared according to the procedure for (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2-azaspiro[4.4]non-7-en-1-one, except (S)-2-(1-oxo-2-azaspiro[4.4]nonan-3-yl)ethyl 4-methylbenzenesulfonate was substituted for (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.00-6.91 (m, 2H), 6.90-6.74 (m, 3H), 3.59 (m, 1H), 3.12 (t, J=4.9 Hz, 4H), 2.69 (m, 2H), 2.60-2.44 (m, 4H), 2.19-2.06 (m, 2H), 1.86-1.51 (m, 9H), 1.44 (m, 1H). LC/MS [M+H]=m/z 346.2.

    ##STR00585##

    [2217] Preparation of (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl ethyl)-2-azaspiro[4.4]nonan-1-one: The title compound was prepared according to the procedure for (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2-azaspiro[4.4]non-7-en-1-one, except (S)-2-(1-oxo-2-azaspiro[4.4]nonan-3-yl)ethyl 4-methylbenzenesulfonate was substituted for (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate and 1-(3-chlorophenyl)piperazine was substituted for 1-(4-fluorophenyl)piperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.16 (t, J=8.0 Hz, 1H), 6.88 (t, J=2.1 Hz, 1H), 6.81 (dd, J=1.7, 7.8 Hz, 1H), 6.78 (dd, J=2.3, 8.3 Hz, 1H), 6.69 (b, 1H), 3.60 (m, 1H), 3.22 (t, J=5.0 Hz, 4H), 2.69 (m, 2H), 2.61-2.39 (m, 4H), 2.23-2.08 (m, 2H), 1.87-1.55 (m, 9H), 1.46 (m, 1H). LC/MS [M+H]=m/z 362.2.

    ##STR00586##

    [2218] Preparation of tert-butyl (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspirop.51decane-8-carboxylate: The title compound was prepared according to the procedure for (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2-azaspiro[4.4]non-7-en-1-one, except tert-butyl (R)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate was substituted for (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate and 1-(3-chlorophenyl)piperazine was substituted for 1-(4-fluorophenyl)piperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.15 (t, J=7.9 Hz, 1H), 7.06 (b, 1H), 6.84 (t, J=2.0 Hz, 1H), 6.79 (dd, J=1.6, 7.6 Hz, 1H), 6.74 (dd, J=2.1, 8.3 Hz, 1H), 4.13-3.82 (b, 2H), 3.63 (p, J=7.0 Hz, 1H), 3.20 (t, J=4.8 Hz, 4H), 3.10-2.83 (m, 2H), 2.67 (m, 2H), 2.60-2.40 (m, 4H), 2.29 (dd, J=6.7, 12.8 Hz, 1H), 1.96 (m, 1H), 1.80-1.62 (m, 3H), 1.58-1.30 (m, 12H). LC/MS [M+H]=m/z 478.2.

    ##STR00587##

    [2219] Preparation of tert-butyl (R)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspirop.51decane-8-carboxylate: The title compound was prepared according to the procedure for (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2-azaspirop.41non-7-en-1-one, except tert-butyl (R)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate was substituted for (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.02 (b, 1H), 6.97-6.90 (m, 2H), 6.90-6.80 (m, 2H), 4.23-3.78 (b, 2H), 3.63 (p, J=6.5 Hz, 1H), 3.12 (t, J=4.7 Hz, 4H), 3.07-2.82 (m, 2H), 2.68 (m, 2H), 2.60-2.40 (m, 4H), 2.28 (dd, J=6.7, 12.7 Hz, 1H), 1.95 (m, 1H), 1.80-1.61 (m, 3H), 1.58-1.29 (m, 12H). LC/MS [M+H]=m/z 461.2.

    ##STR00588##

    [2220] Preparation of tert-butyl (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspirop.51decane-8-carboxylate: The title compound was prepared according to the procedure for (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2-azaspirop.41non-7-en-1-one, except tert-butyl (S)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate was substituted for (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate and 1-(3-chlorophenyl)piperazine was substituted for 1-(4-fluorophenyl)piperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.14 (t, J=8.0 Hz, 1H), 7.04 (b, 1H), 6.85 (t, J=2.0 Hz, 1H), 6.79 (dd, J=1.6, 7.7 Hz, 1H), 6.76 (dd, J=2.1, 8.3 Hz, 1H), 4.13-3.83 (b, 2H), 3.63 (p, J=7.0 Hz, 1H), 3.19 (t, J=4.8 Hz, 4H), 3.09-2.80 (m, 2H), 2.67 (m, 2H), 2.60-2.39 (m, 4H), 2.29 (dd, J=6.6, 12.8 Hz, 1H), 1.95 (m, 1H), 1.80-1.63 (m, 3H), 1.57-1.30 (m, 12H). LC/MS [M+H]=m/z 478.2

    ##STR00589##

    [2221] Preparation of tert-butyl (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspirop.51decane-8-carboxylate: The title compound was prepared according to the procedure for (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2-azaspiro[4.4]non-7-en-1-one, except tert-butyl (S)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate was substituted for (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate. NMR (400 MHz, CDCl.sub.3) δ 7.01 (b, 1H), 6.97-6.89 (m, 2H), 6.89-6.80 (m, 2H), 4.21-3.76 (b, 2H), 3.63 (p, J=6.5 Hz, 1H), 3.11 (t, J=4.7 Hz, 4H), 3.06-2.82 (m, 2H), 2.69 (m, 2H), 2.61-2.41 (m, 4H), 2.29 (dd, J=6.7, 12.8 Hz, 1H), 1.94 (m, 1H), 1.80-1.60 (m, 3H), 1.57-1.28 (m, 12H). LC/MS [M+H]=m/z 461.

    ##STR00590##

    [2222] Preparation of (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: A 6M HCl in methanol solution was prepared via the addition of acetyl chloride (1.2 mL) to methanol (3 mL). tert-Butyl (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate (0.127 g, 0.266 mmol, 1.0 equiv.) was dissolved in the prepared 6M methanolic HCl solution (3 mL) and let stir at 23° C. for 30 minutes before being diluted with methanol and concentrated in vacuo to produce a crude product as an HCl salt. The product was free based by stirring with Amberlite IRN-78 base resin in methanol (˜10 mL) for 15 minutes followed by filtration and concentrated in vacuo to produce a crude product that was used in the next step without further purification. .sup.1H NMR (400 MHz, MeOD) δ 7.21 (t, J=8.3 Hz, 1H), 6.95 (s, 1H), 6.88 (d, J=8.5 Hz, 1H), 6.81 (d, J=7.7 Hz, 1H), 3.68 (m, 1H), 3.29-3.13 (m, 4H), 3.01 (m, 2H), 2.81-2.38 (m, 9H), 1.93 (m, 1H), 1.86-1.64 (m, 3H), 1.60 (dd, J=7.6, 12.7 Hz, 1H), 1.49 (d, J=13.2 Hz, 1H), 1.38 (d, J=12.8 Hz, 1H). LC/MS [M+H]=m/z 377.

    ##STR00591##

    [2223] Preparation of (R)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one, except tert-butyl (R)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspiro [4.5]decane-8-carboxylate was substituted for tert-butyl (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate. .sup.1H NMR (400 MHz, MeOD) δ 7.08-6.92 (m, 4H), 3.68 (m, 1H), 3.23-3.09 (m, 4H), 3.01 (m, 2H), 2.81-2.38 (m, 9H), 1.93 (m, 1H), 1.86-1.62 (m, 3H), 1.60 (dd, J=7.6, 12.5 Hz, 1H), 1.48 (d, J=13.5 Hz, 1H), 1.37 (d, J=13.5 Hz, 1H). LC/MS [M+H]=m/z 361.

    ##STR00592##

    [2224] Preparation of (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one, except tert-butyl (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2, 8-diazaspiro[4.5]decan-1-one was substituted for tert-butyl (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate .sup.1H NMR (400 MHz, MeOD) δ 7.20 (t, J=8.2 Hz, 1H), 6.94 (s, 1H), 6.88 (d, J=8.5 Hz, 1H), 6.80 (d, J=7.7 Hz, 1H), 3.68 (m, 1H), 3.28-3.13 (m, 4H), 3.02 (m, 2H), 2.80-2.36 (m, 9H), 1.93 (m, 1H), 1.85-1.64 (m, 3H), 1.59 (dd, J=7.6, 12.7 Hz, 1H), 1.48 (d, J=13.2 Hz, 1H), 1.37 (d, J=12.8 Hz, 1H). LC/MS [M+H]=m/z 377.

    ##STR00593##

    [2225] Preparation of (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one, except tert-butyl (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate was substituted for tert-butyl (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate. .sup.1H NMR (400 MHz, MeOD) δ 7.07-6.91 (m, 4H), 3.68 (m, 1H), 3.22-3.09 (m, 4H), 3.02 (m, 2H), 2.81-2.37 (m, 9H), 1.93 (m, 1H), 1.86-1.63 (m, 3H), 1.59 (dd, J=7.6, 12.5 Hz, 1H), 1.48 (d, J=13.5 Hz, 1H), 1.38 (d, J=13.5 Hz, 1H). LC/MS [M+H]=m/z 361.2.

    ##STR00594##

    [2226] Preparation of (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-8-(methylsulfonyl)-2,8-diazaspirop.51decan-1-one: A solution of (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspirop.51decan-1-one (28 mg, 0.074 mmol, 1 equiv.), dichloromethane (0.85 mL) and triethylamine (15.7 mg, 0.155 mmol, 2.1 eq.) was cooled to 0° C. before methanesulfonyl chloride (12.7 mg. 0.111 mmol, 1.5 equiv.) was added to the solution. The reaction solution was allowed to warm to 23° C. and stir for 15 minutes. The reaction was diluted with methanol (˜2 mL), concentrated in vacuo and further purified by flash column chromatography (methanol/dichloromethane, 0%˜10%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.17 (t, J=8.2 Hz, 1H), 6.88 (t, J=2.1 Hz, 1H), 6.83 (dd, J=1.7, 7.8 Hz, 1H), 6.81-6.72 (m, 2H), 3.81-3.61 (m, 2H), 3.50 (m, 1H), 3.32-3.11 (m, 6H), 2.82 (s, 3H), 2.73 (m, 2H), 2.66-2.42 (m, 4H), 2.20 (dd, J=6.5, 12.7 Hz, 1H), 2.04 (m, 1H), 1.96 (m, 1H), 1.79-1.50 (m, 5H); MS (LC/MS, M+H.sup.+): 456.2.

    ##STR00595##

    [2227] Preparation of (R)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-8-(methylsulfonyl)-2,8-diazaspirop.51decan-1-one: The title compound was prepared according to the procedure for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one, except (R)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one was substituted for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.07-6.93 (m, 2H), 6.92-6.84 (m, 2H), 6.80 (b, 1H), 3.80-3.62 (m, 2H), 3.49 (m, 1H), 3.27 (m, 1H), 3.22-3.08 (m, 5H), 2.82 (s, 3H), 2.75 (m, 2H), 2.66-2.43 (m, 4H), 2.20 (dd, J=6.4, 12.7 Hz, 1H), 2.04 (m, 1H), 1.96 (m, 1H), 1.79-1.48 (m, 5H); MS (LC/MS, M+H.sup.+): 439.2.

    ##STR00596##

    [2228] Preparation of (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one, except (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one was substituted for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.09 (t, J=8.1 Hz, 1H), 6.79 (t, J=2.1 Hz, 1H), 6.74 (dd, J=1.7, 7.7 Hz, 1H), 6.72-6.65 (m, 2H), 3.72-3.53 (m, 2H), 3.41 (m, 1H), 3.23-3.04 (m, 6H), 2.73 (s, 3H), 2.64 (m, 2H), 2.57-2.33 (m, 4H), 2.12 (dd, J=6.4, 12.8 Hz, 1H), 1.95 (m, 1H), 1.88 (m, 1H), 1.70-1.42 (m, 5H); MS (LC/MS, M+H.sup.+): 456.2.

    ##STR00597##

    [2229] Preparation of (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)e thyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one, except (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one was substituted for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 6.94-6.84 (m, 2H), 6.83-6.76 (m, 2H), 6.74 (b, 1H), 3.71-3.54 (m, 2H), 3.41 (m, 1H), 3.17 (m, 1H), 3.13-2.99 (m, 5H), 2.73 (s, 3H), 2.65 (m, 2H), 2.57-2.34 (m, 4H), 2.11 (dd, J=6.4, 12.7 Hz, 1H), 1.95 (m, 1H), 1.87 (m, 1H), 1.70-1.39 (m, 5H); MS (LC/MS, M+H.sup.+): 439.2

    ##STR00598##

    [2230] Preparation of (R)-8-acetyl-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: A solution of (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one (21 mg, 0.056 mmol, 1 equiv.), dichloromethane (0.725 mL) and triethylamine (12 mg, 0.118 mmol, 2.1 eq.) was cooled to 0° C. before acetyl chloride (12.7 mg. 0.057 mmol, 1.01 equiv.) was added to the solution. The reaction solution was allowed to warm to 23° C. and stir for 15 minutes. The reaction was diluted with methanol (˜2 mL), concentrated in vacuo and further purified by flash column chromatography (methanol/methylene chloride, 0%˜10%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.09 (t, J=8.1 Hz, 1H), 6.80 (t, J=2.2 Hz, 1H), 6.77-6.65 (m, 3H), 4.26 (dt, J=4.8, 13.4 Hz, 0.5H), 4.12 (dt, J=5.0, 13.8 Hz, 0.5H), 3.82 (dt, J=4.5, 13.5 Hz, 0.5H), 3.69 (dt, J=4.9, 13.8 Hz, 0.5H), 3.60 (m, 1H), 3.27-3.03 (m, 5.5H), 2.97 (m, 0.5H), 2.63 (m, 2H), 2.57-2.31 (m, 4H), 2.23 (m, 1H), 2.02 (s, 3H), 1.98-1.80 (m, 1H), 1.80-1.56 (m, 3H), 1.55-1.29 (m, 3H); MS (LC/MS, M+H.sup.+): 419.2

    ##STR00599##

    [2231] Preparation of (R)-8-acetyl-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-8-acetyl-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one, except (R)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4 .5]decan-1-one was substituted for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 6.93-6.84 (m, 2H), 6.83-6.70 (m, 3H), 4.26 (dt, J=5.2, 13.5 Hz, 0.5H), 4.12 (dt, J=5.0, 13.5 Hz, 0.5H), 3.82 (dt, J=5.0, 13.7 Hz, 0.5H), 3.69 (dt, J=5.0, 13.7 Hz, 0.5H), 3.59 (m, 1H), 3.27-2.91 (m, 6H), 2.65 (m, 2H), 2.58-2.33 (m, 4H), 2.23 (m, 1H), 2.02 (s, 3H), 1.99-1.82 (m, 1H), 1.80-1.55 (m, 3H), 1.54-1.30 (m, 3H); MS (LC/MS, M+H.sup.+): 403.2

    ##STR00600##

    [2232] Preparation of (S)-8-acetyl-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-8-acetyl-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one, except (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one was substituted for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.09 (t, J=8.1 Hz, 1H), 6.80 (t, J=2.2 Hz, 1H), 6.77-6.66 (m, 3H), 4.26 (dt, J=4.8, 13.4 Hz, 0.5H), 4.12 (dt, J=5.0, 13.8 Hz, 0.5H), 3.82 (dt, J=4.5, 13.5 Hz, 0.5H), 3.69 (dt, J=4.9, 13.8 Hz, 0.5H), 3.60 (m, 1H), 3.25-3.08 (m, 5.5H), 2.98 (m, 0.5H), 2.63 (m, 2H), 2.56-2.34 (m, 4H), 2.23 (m, 1H), 2.02 (s, 3H), 1.98-1.83 (m, 1H), 1.81-1.56 (m, 3H), 1.54-1.30 (m, 3H); MS (LC/MS, M+H.sup.+): 419.2

    ##STR00601##

    [2233] Preparation of (S)-8-acetyl-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-8-acetyl-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one, except (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one was substituted for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)e thyl)-2, 8-diazaspiro[4.5]decan-1-one. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 6.93-6.84 (m, 2H), 6.83-6.73 (m, 3H), 4.26 (dt, J=5.2, 13.5 Hz, 0.5H), 4.12 (dt, J=5.0, 13.5 Hz, 0.5H), 3.82 (dt, J=5.0, 13.7 Hz, 0.5H), 3.69 (dt, J=5.0, 13.7 Hz, 0.5H), 3.59 (m, 1H), 3.26-2.91 (m, 6H), 2.65 (m, 2H), 2.57-2.32 (m, 4H), 2.23 (m, 1H), 2.02 (s, 3H), 1.98-1.82 (m, 1H), 1.81-1.55 (m, 3H), 1.54-1.30 (m, 3H); MS (LC/MS, M+H.sup.+): 403.2

    ##STR00602##

    [2234] Preparation of (R)-3,3-diethyl-5-(2-(4-(pyridin-2-yl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 1-(2-pyridyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 8.18 (dd, J=2.1, 4.8 Hz, 1H), 7.47 (m, 1H), 6.73 (b, 1H), 6.66-6.57 (m, 2H), 3.64-3.47 (m, 5H), 2.63 (m, 2H), 2.58-2.36 (m, 4H), 2.05 (dd, J=7.4, 13.0 Hz, 1H), 1.76-1.43 (m, 7H), 0.90 (dt, J=7.4, 14.5 Hz, 6H). LC/MS [M+H]=m/z 331.2

    ##STR00603##

    [2235] Preparation of (R)-3,3-diethyl-5-(2-(4-(2-me thoxyphenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 1-(2-methoxyphenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.04-6.88 (m, 3H), 6.85 (dd, J=1.1, 8.0 Hz, 1H), 6.72 (b, 1H), 3.86 (s, 3H), 3.58 (m, 1H), 3.28-2.90 (b, 4H), 2.84-2.65 (b, 2H), 2.64-2.41 (m, 4H), 2.05 (dd, J=7.3, 13.1 Hz, 1H), 1.76-1.43 (m, 7H), 0.91 (dt, J=7.5, 16.1 Hz, 6H). LC/MS [M+H]=m/z 360.2

    ##STR00604##

    [2236] Preparation of (R)-4-(4-(2-(4,4-diethyl-5-oxopyrrolidin-2-yl)ethyl)piperazin-1-yl)benzonitrile: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 1-(4-cyanophenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.48 (d, J=9.0 Hz, 2H), 6.85 (d, J=9.0 Hz, 2H), 6.73 (b, 1H), 3.58 (m, 1H), 3.34 (t, J=5.1 Hz, 4H), 2.67 (m, 2H), 2.60-2.38 (m, 4H), 2.06 (dd, J=7.6, 13.2 Hz, 1H), 1.75-1.42 (m, 7H), 0.90 (dt, J=7.4, 14.0 Hz, 6H). LC/MS [M+H]=m/z 355.2

    ##STR00605##

    [2237] Preparation of (R)-3,3-diethyl-5-(2-(4-(4-(trifluoromethyl)phenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 1-(4-(trifluoromethyl)phenyl)piperazine was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.36 (d, J=8.6 Hz, 2H), 6.80 (d, J=8.6 Hz, 2H), 6.58 (b, 1H), 3.47 (m, 1H), 3.18 (t, J=5.0 Hz, 4H), 2.57 (m, 2H), 2.49-2.28 (m, 4H), 1.95 (dd, J=7.4, 13.1 Hz, 1H), 1.64-1.32 (m, 7H), 0.79 (dt, J=7.3, 13.8 Hz, 6H). LC/MS [M+H]=m/z 398.2

    ##STR00606##

    [2238] Preparation of (5R)-3,3-diethyl-5-(2-(5-phenylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 2-phenyloctahydropyrrolo[3,4-c]pyrrole was substituted for 1-phenylpiperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.11 (m, 2H), 6.61 (t, J=7.4 Hz, 1H), 6.56 (d, J=8.6 Hz, 2H), 6.44 (b, 1H), 3.42 (m, 1H), 3.20-3.05 (m, 4H), 2.91 (m, 1H), 2.87-2.70 (m, 3H), 2.51 (m, 1H), 2.34-2.15 (m, 2H), 2.07 (dd, J=4.7, 8.5 Hz, 1H), 1.91 (dd, J=7.4, 13.1 Hz, 1H), 1.58-1.28 (m, 7H), 0.77 (m, 6H). LC/MS [M+H]=m/z 356.2

    ##STR00607##

    [2239] Preparation of tert-butyl (S)-3-(2-cyanoethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate: To a solution of tert-butyl (R)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate (0.2 g, 0.44 mmol, 1.0 equiv.) in acetonitrile (1.9 mL) was added potassium cyanide (0.72 g, 1.1 mmol, 2.5 equiv.). The resulting reaction mixture was then allowed to reflux for 16 hours. After cooling to 23° C., the reaction mixture was filtered thru a plug of Celite and concentrated in vacuo to give a crude product which was further purified by column chromatography (MeOH/dichloromethane, 0%˜10%). iH NMR (400 MHz, CDCl.sub.3) δ 8.08 (b, 1H), 4.11-3.79 (b, 2H), 3.72 (p, J=6.6 Hz, 1H), 3.00 (t, J=11.3 Hz, 1H), 2.91 (t, J=11.3 Hz, 1H), 2.49 (td, J=1.2, 7.4 Hz, 2H), 2.32 (dd, J=7.0, 13.0 Hz, 1H), 1.97-1.78 (m, 3H), 1.72 (m, 1H), 1.52 (dd, J=7.8, 12.9 Hz, 1H), 1.48-1.29 (m, 11H).

    ##STR00608##

    [2240] Preparation of (S)-3-(8-(methylsulfonyl)-1-oxo-2,8-diazaspiro[4.5]decan-3-yl)propanenitrile: To a solution of tert-butyl (S)-3-(2-cyanoethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate (0.1 g, 0.35 mmol, 1.0 equiv.) in dichloromethane (2.75 mL) was added trifluoroacetic acid (0.5 mL). The resulting solution was allowed to stir at 23° C. for 45 minutes before being concentrated in vacuo. The residue was dissolved in MeOH (5 mL) followed by the addition of Amberlite IRN-78 base resin (0.5 g). This mixture was stirred vigorously for 15 minutes, filtered and the filtrate was concentrated in vacuo to give a crude intermediate that was then dissolved in dichloromethane (3.75 mL). The resulting solution was then cooled to 0° C. before the sequential addition of triethylamine (0.72 g, 0.70 mmol, 2.0 eq.) and methanesulfonyl chloride (0.6 g. 0.53 mmol, 1.5 equiv.). The reaction solution was allowed to warm to 23° C. and stir for 15 minutes. The reaction was diluted with MeOH (2 mL), concentrated in vacuo and further purified by flash column chromatography (MeOH w/2M ammonia/dichloromethane, 0% -10%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 6.56 (b, 1H), 3.81 (p, J=6.8 Hz, 1H), 3.72 (m, 1H), 3.53 (m, 1H), 3.32-3.15 (m, 2H), 2.83 (s, 3H), 2.49 (t, J=6.8 Hz, 2H), 2.29 (dd, J=6.9, 12.9 Hz, 1H), 2.09-1.82 (m, 4H), 1.75-1.59 (m, 3H).

    ##STR00609##

    [2241] Preparation of methyl (S)-3-(8-(methylsulfonyl)-1-oxo-2,8-diazaspiro[4.5]decan-3-yl)propanoate: A 6M HCl in methanol solution was prepared via the addition of acetyl chloride (0.48 mL) to MeOH (1 mL). (S)-3-(8-(methylsulfonyl)-1-oxo-2,8-diazaspiro[4.5]decan-3-yl)propanenitrile (91 mg, 0.32 mmol, 1.0 equiv.) was dissolved in the prepared 6M methanolic HCl solution (0.64 mL) and stirred at 23° C. overnight. The reaction mixture was diluted with MeOH (1 mL) and concentrated in vacuo. The resulting residue was suspended in sat. aqueous NaHCO.sub.3 and extracted with dichloromethane (4×15 mL). The combined organic phase was dried over Na.sub.2SO.sub.4 and concentrated in vacuo to give a crude product that was used in the next step without further purification. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.13 (b, 1H), 3.75-3.57 (m, 5H), 3.50 (m, 1H), 3.23-3.02 (m, 2H), 2.79 (s, 3H), 2.40 (td, J=1.7, 7.2 Hz, 2H), 2.18 (dd, J=6.8, 13.0 Hz, 1H), 2.01 (m, 1H), 1.92 (m, 1H), 1.83 (q, J=6.9 Hz, 2H), 1.68-1.45 (m, 3H).

    ##STR00610##

    [2242] Preparation of (S)-3-(3-hydroxypropyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one: This reaction was performed in oven-dried glassware under a nitrogen atmosphere. To a stirred solution of methyl (S)-3-(8-(methylsulfonyl)-1-oxo-2,8-diazaspiro[4.5]decan-3-yl)propanoate (80 mg, 0.25 mmol, 1.0 equiv.) in dry tetrahydrofuran (1.2 mL) at 0° C. was added LiBH.sub.4 (2M in tetrahydrofuran, 0.25 mL, 0.5 mmol, 2.0 equiv.) and the resulting solution was stirred at 23° C. for 6 hours. The reaction was then quenched with 0.5 mL of acetic acid and then filtered while washing with MeOH. The filtrate was concentrated in vacuo to give a crude product which was further purified by column chromatography (MeOH/dichloromethane, 10%). .sup.1H NMR (400 MHz, MeOD) δ 3.74-3.55 (m, 5H), 3.02 (td, J=3.0, 11.2 Hz, 1H), 2.92 (td, J=2.9, 11.5 Hz, 1H), 2.86 (s, 3H), 2.39 (dd, J=7.0, 13.1 Hz, 1H), 2.08-1.97 (m, 1H), 1.89-1.78 (m, 1H), 1.71-1.50 (m, 7H).

    ##STR00611##

    [2243] Preparation of (S)-3-(8-(methylsulfonyl)-1-oxo-2,8-diazaspiro[4.5]decan-3-yl)propyl 4-methylbenzenesulfonate: To a cooled mixture of (S)-3-(3-hydroxypropyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one (55 mg, 0.19 mmol, 1.0 equiv.) and triethylamine (40 mg, 0.38 mmol, 2.0 equiv.) in dichloromethane:dimethylformamide (2.0 mL:0.2 mL) at 0° C. was added 4-toluenesulfonyl chloride (55 mg, 0.28 mmol, 1.5 equiv.) followed by 4-dimethylaminopyridine (3 mg, 0.02 mmol, 0.1 equiv.). The resulting reaction mixture was stirred at 0° C. for 5 minutes before being warmed to 23° C. and allowed to stir for 24 hours. Then, the reaction mixture was diluted with dichloromethane (5 mL), washed with 1N HCl (1×5 mL). The aqueous layer was backwashed with dichloromethane (2×5 mL). The combined organic layers were dried over Na.sub.2SO.sub.4 and concentrated in vacuo to give a crude product which was further purified by HPLC (CH.sub.3CN/H.sub.2O, 0.1% Formic acid), 0%˜100%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.78 (d, J=8.2 Hz, 2H), 7.37 (d, J=8.0 Hz, 2H), 6.84 (b, 1H), 4.04 (t, J=5.9 Hz, 2H), 3.70 (m, 1H), 3.64-3.44 (m, 2H), 3.21-3.00 (m, 2H), 2.80 (s, 3H), 2.46 (s, 3H), 2.17 (dd, J=6.8, 12.8 Hz, 1H), 2.01 (m, 1H), 1.91 (m, 1H), 1.81-1.66 (m, 2H), 1.66-1.44 (m, 5H).

    ##STR00612##

    [2244] Preparation of (S)-3-(3-(4-(4-fluorophenyl)piperazin-1-yl)propyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one: To a small vial was added (S)-3-(8-(methylsulfonyl)-1-oxo-2,8-diazaspiro[4.5]decan-3-yl)propyl 4-methylbenzenesulfonate (16 mg, 0.036 mmol, 1 equiv.) and 1-(4-fluorophenyl)piperazine (13.5 mg, 0.75 mmol, 2.1 equiv.) then both were dissolved in acetonitrile (0.4 mL). Then K.sub.2CO.sub.3 (13 mg, 0.089 mmol, 2.5 equiv.) was added and the reaction mixture was stirred at 80° C. overnight and then cooled to 23° C. The mixture was filtered, washed with acetonitrile and filtrate was concentrated in vacuo to give a crude product which was by further purified by column chromatography (MeOH/dichloromethane, 0%˜10%). .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.02-6.92 (m, 3H), 6.92-6.84 (m, 2H), 3.72 (m, 1H), 3.59 (m, 1H), 3.50 (m, 1H), 3.31-3.09 (m, 6H), 2.81 (s, 3H), 2.74-2.56 (m, 4H), 2.46 (t, J=6.2 Hz, 2H), 2.18 (dd, J=6.6, 12.8 Hz, 1H), 2.09-1.90 (m, 2H), 1.74-1.43 (m, 7H). LC/MS [M+H]=m/z 453.2

    ##STR00613##

    [2245] Preparation of (S)-3-(3-(4-(3-chlorophenyl)piperazin-1-yl)propyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (S)-3-(3-(4-(4-fluorophenyl)piperazin-1-yl)propyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one, except 1-(3-chlorophenyl)piperazine was substituted for 1-(4-fluorophenyl)piperazine. .sup.1H NMR (400 MHz, CDCl.sub.3) δ 7.17 (t, J=8.2 Hz, 1H), 6.92-6.85 (m, 2H), 6.84-6.76 (m, 2H), 3.72 (m, 1H), 3.60 (m, 1H), 3.50 (m, 1H), 3.32-3.13 (m, 6H), 2.81 (s, 3H), 2.71-2.55 (m, 4H), 2.45 (t, J=6.3 Hz, 2H), 2.19 (dd, J=6.7, 12.8 Hz, 1H), 2.09-1.90 (m, 2H), 1.73-1.44 (m, 7H). LC/MS [M+H]=m/z 469.2

    Example 2

    Exemplary Formulations

    [2246] The present invention also relates to compositions or formulations which comprise the 5-hydroxytryptamine receptor 7 activity modulators according to the present invention. In general, the compositions of the present invention comprise an effective amount of one or more compounds of the disclosure and salts thereof according to the present invention which are effective for providing modulation of 5-hydroxytryptamine receptor 7 activity; and one or more excipients.

    [2247] For the purposes of the present invention the term “excipient” and “carrier” are used interchangeably throughout the description of the present invention and said terms are defined herein as, “ingredients which are used in the practice of formulating a safe and effective pharmaceutical composition.”

    [2248] The formulator will understand that excipients are used primarily to serve in delivering a safe, stable, and functional pharmaceutical, serving not only as part of the overall vehicle for delivery but also as a means for achieving effective absorption by the recipient of the active ingredient. An excipient may fill a role as simple and direct as being an inert filler, or an excipient as used herein may be part of a pH stabilizing system or coating to insure delivery of the ingredients safely to the stomach. The formulator can also take advantage of the fact the compounds of the present invention have improved cellular potency, pharmacokinetic properties, as well as improved oral bioavailability.

    [2249] The present teachings also provide pharmaceutical compositions that include at least one compound described herein and one or more pharmaceutically acceptable carriers, excipients, or diluents. Examples of such carriers are well known to those skilled in the art and can be prepared in accordance with acceptable pharmaceutical procedures, such as, for example, those described in Remington's Pharmaceutical Sciences, 17th edition, ed. Alfonoso R. Gennaro, Mack Publishing Company, Easton, Pa. (1985), the entire disclosure of which is incorporated by reference herein for all purposes. As used herein, “pharmaceutically acceptable” refers to a substance that is acceptable for use in pharmaceutical applications from a toxicological perspective and does not adversely interact with the active ingredient. Accordingly, pharmaceutically acceptable carriers are those that are compatible with the other ingredients in the formulation and are biologically acceptable. Supplementary active ingredients can also be incorporated into the pharmaceutical compositions.

    [2250] Compounds of the present teachings can be administered orally or parenterally, neat or in combination with conventional pharmaceutical carriers. Applicable solid carriers can include one or more substances which can also act as flavoring agents, lubricants, solubilizers, suspending agents, fillers, glidants, compression aids, binders or tablet-disintegrating agents, or encapsulating materials. The compounds can be formulated in conventional manner, for example, in a manner similar to that used for known 5-hydroxytryptamine receptor 7 activity modulators. Oral formulations containing a compound disclosed herein can comprise any conventionally used oral form, including tablets, capsules, buccal forms, troches, lozenges and oral liquids, suspensions or solutions. In powders, the carrier can be a finely divided solid, which is an admixture with a finely divided compound. In tablets, a compound disclosed herein can be mixed with a carrier having the necessary compression properties in suitable proportions and compacted in the shape and size desired. The powders and tablets can contain up to 99% of the compound.

    [2251] Capsules can contain mixtures of one or more compound(s) disclosed herein with inert filler(s) and/or diluent(s) such as pharmaceutically acceptable starches (e.g., corn, potato or tapioca starch), sugars, artificial sweetening agents, powdered celluloses (e.g., crystalline and microcrystalline celluloses), flours, gelatins, gums, and the like.

    [2252] Useful tablet formulations can be made by conventional compression, wet granulation or dry granulation methods and utilize pharmaceutically acceptable diluents, binding agents, lubricants, disintegrants, surface modifying agents (including surfactants), suspending or stabilizing agents, including, but not limited to, magnesium stearate, stearic acid, sodium lauryl sulfate, talc, sugars, lactose, dextrin, starch, gelatin, cellulose, methyl cellulose, microcrystalline cellulose, sodium carboxymethyl cellulose, carboxymethylcellulose calcium, polyvinylpyrrolidine, alginic acid, acacia gum, xanthan gum, sodium citrate, complex silicates, calcium carbonate, glycine, sucrose, sorbitol, dicalcium phosphate, calcium sulfate, lactose, kaolin, mannitol, sodium chloride, low melting waxes, and ion exchange resins. Surface modifying agents include nonionic and anionic surface modifying agents. Representative examples of surface modifying agents include, but are not limited to, poloxamer 188, benzalkonium chloride, calcium stearate, cetostearl alcohol, cetomacrogol emulsifying wax, sorbitan esters, colloidal silicon dioxide, phosphates, sodium dodecylsulfate, magnesium aluminum silicate, and triethanolamine. Oral formulations herein can utilize standard delay or time-release formulations to alter the absorption of the compound(s). The oral formulation can also consist of administering a compound disclosed herein in water or fruit juice, containing appropriate solubilizers or emulsifiers as needed.

    [2253] Liquid carriers can be used in preparing solutions, suspensions, emulsions, syrups, elixirs, and for inhaled delivery. A compound of the present teachings can be dissolved or suspended in a pharmaceutically acceptable liquid carrier such as water, an organic solvent, or a mixture of both, or a pharmaceutically acceptable oils or fats. The liquid carrier can contain other suitable pharmaceutical additives such as solubilizers, emulsifiers, buffers, preservatives, sweeteners, flavoring agents, suspending agents, thickening agents, colors, viscosity regulators, stabilizers, and osmo-regulators. Examples of liquid carriers for oral and parenteral administration include, but are not limited to, water (particularly containing additives as described herein, e.g., cellulose derivatives such as a sodium carboxymethyl cellulose solution), alcohols (including monohydric alcohols and polyhydric alcohols, e.g., glycols) and their derivatives, and oils (e.g., fractionated coconut oil and arachis oil). For parenteral administration, the carrier can be an oily ester such as ethyl oleate and isopropyl myristate. Sterile liquid carriers are used in sterile liquid form compositions for parenteral administration. The liquid carrier for pressurized compositions can be halogenated hydrocarbon or other pharmaceutically acceptable propellants.

    [2254] Liquid pharmaceutical compositions, which are sterile solutions or suspensions, can be utilized by, for example, intramuscular, intraperitoneal or subcutaneous injection. Sterile solutions can also be administered intravenously. Compositions for oral administration can be in either liquid or solid form.

    [2255] Preferably the pharmaceutical composition is in unit dosage form, for example, as tablets, capsules, powders, solutions, suspensions, emulsions, granules, or suppositories. In such form, the pharmaceutical composition can be sub-divided in unit dose(s) containing appropriate quantities of the compound. The unit dosage forms can be packaged compositions, for example, packeted powders, vials, ampoules, prefilled syringes or sachets containing liquids. Alternatively, the unit dosage form can be a capsule or tablet itself, or it can be the appropriate number of any such compositions in package form. Such unit dosage form can contain from about 1 mg/kg of compound to about 500 mg/kg of compound, and can be given in a single dose or in two or more doses. Such doses can be administered in any manner useful in directing the compound(s) to the recipient' s bloodstream, including orally, via implants, parenterally (including intravenous, intraperitoneal and subcutaneous injections), rectally, vaginally, and transdermally.

    [2256] When administered for the treatment or inhibition of a particular disease state or disorder, it is understood that an effective dosage can vary depending upon the particular compound utilized, the mode of administration, and severity of the condition being treated, as well as the various physical factors related to the individual being treated. In therapeutic applications, a compound of the present teachings can be provided to a patient already suffering from a disease in an amount sufficient to cure or at least partially ameliorate the symptoms of the disease and its complications. The dosage to be used in the treatment of a specific individual typically must be subjectively determined by the attending physician. The variables involved include the specific condition and its state as well as the size, age and response pattern of the patient.

    [2257] In some cases it may be desirable to administer a compound directly to the airways of the patient, using devices such as, but not limited to, metered dose inhalers, breath-operated inhalers, multidose dry-powder inhalers, pumps, squeeze-actuated nebulized spray dispensers, aerosol dispensers, and aerosol nebulizers. For administration by intranasal or intrabronchial inhalation, the compounds of the present teachings can be formulated into a liquid composition, a solid composition, or an aerosol composition. The liquid composition can include, by way of illustration, one or more compounds of the present teachings dissolved, partially dissolved, or suspended in one or more pharmaceutically acceptable solvents and can be administered by, for example, a pump or a squeeze-actuated nebulized spray dispenser. The solvents can be, for example, isotonic saline or bacteriostatic water. The solid composition can be, by way of illustration, a powder preparation including one or more compounds of the present teachings intermixed with lactose or other inert powders that are acceptable for intrabronchial use, and can be administered by, for example, an aerosol dispenser or a device that breaks or punctures a capsule encasing the solid composition and delivers the solid composition for inhalation. The aerosol composition can include, by way of illustration, one or more compounds of the present teachings, propellants, surfactants, and co-solvents, and can be administered by, for example, a metered device. The propellants can be a chlorofluorocarbon (CFC), a hydrofluoroalkane (HFA), or other propellants that are physiologically and environmentally acceptable.]

    [2258] Compounds described herein can be administered parenterally or intraperitoneally. Solutions or suspensions of these compounds or a pharmaceutically acceptable salts, hydrates, or esters thereof can be prepared in water suitably mixed with a surfactant such as hydroxyl-propylcellulose. Dispersions can also be prepared in glycerol, liquid polyethylene glycols, and mixtures thereof in oils. Under ordinary conditions of storage and use, these preparations typically contain a preservative to inhibit the growth of microorganisms.

    [2259] The pharmaceutical forms suitable for injection can include sterile aqueous solutions or dispersions and sterile powders for the extemporaneous preparation of sterile injectable solutions or dispersions. In some embodiments, the form can sterile and its viscosity permits it to flow through a syringe. The form preferably is stable under the conditions of manufacture and storage and can be preserved against the contaminating action of microorganisms such as bacteria and fungi. The carrier can be a solvent or dispersion medium containing, for example, water, ethanol, polyol (e.g., glycerol, propylene glycol and liquid polyethylene glycol), suitable mixtures thereof, and vegetable oils.

    [2260] Compounds described herein can be administered transdermally, i.e., administered across the surface of the body and the inner linings of bodily passages including epithelial and mucosal tissues. Such administration can be carried out using the compounds of the present teachings including pharmaceutically acceptable salts, hydrates, or esters thereof, in lotions, creams, foams, patches, suspensions, solutions, and suppositories (rectal and vaginal).

    [2261] Transdermal administration can be accomplished through the use of a transdermal patch containing a compound, such as a compound disclosed herein, and a carrier that can be inert to the compound, can be non-toxic to the skin, and can allow delivery of the compound for systemic absorption into the blood stream via the skin. The carrier can take any number of forms such as creams and ointments, pastes, gels, and occlusive devices. The creams and ointments can be viscous liquid or semisolid emulsions of either the oil-in-water or water-in-oil type. Pastes comprised of absorptive powders dispersed in petroleum or hydrophilic petroleum containing the compound can also be suitable. A variety of occlusive devices can be used to release the compound into the blood stream, such as a semi-permeable membrane covering a reservoir containing the compound with or without a carrier, or a matrix containing the compound. Other occlusive devices are known in the literature.

    [2262] Compounds described herein can be administered rectally or vaginally in the form of a conventional suppository. Suppository formulations can be made from traditional materials, including cocoa butter, with or without the addition of waxes to alter the suppository' s melting point, and glycerin. Water-soluble suppository bases, such as polyethylene glycols of various molecular weights, can also be used.

    [2263] Lipid formulations or nanocapsules can be used to introduce compounds of the present teachings into host cells either in vitro or in vivo. Lipid formulations and nanocapsules can be prepared by methods known in the art.

    [2264] To increase the effectiveness of compounds of the present teachings, it can be desirable to combine a compound with other agents effective in the treatment of the target disease. For example, other active compounds (i.e., other active ingredients or agents) effective in treating the target disease can be administered with compounds of the present teachings. The other agents can be administered at the same time or at different times than the compounds disclosed herein.

    [2265] Compounds of the present teachings can be useful for the treatment or inhibition of a pathological condition or disorder in a mammal, for example, a human subject. The present teachings accordingly provide methods of treating or inhibiting a pathological condition or disorder by providing to a mammal a compound of the present teachings including its pharmaceutically acceptable salt) or a pharmaceutical composition that includes one or more compounds of the present teachings in combination or association with pharmaceutically acceptable carriers. Compounds of the present teachings can be administered alone or in combination with other therapeutically effective compounds or therapies for the treatment or inhibition of the pathological condition or disorder.

    [2266] Non-limiting examples of compositions according to the present invention include from about 0.001 mg to about 1000 mg of one or more compounds of the disclosure according to the present invention and one or more excipients; from about 0.01 mg to about 100 mg of one or more compounds of the disclosure according to the present invention and one or more excipients; and from about 0.1 mg to about 10 mg of one or more compounds of the disclosure according to the present invention; and one or more excipients.

    Example 3

    General Biochemical Procedures

    [2267] The following procedures can be utilized in evaluating and selecting compounds as 5-hydroxytryptamine receptor 7 activity modulators.

    [2268] Radiolabel Binding Studies for Serotonin 5HT7 receptors, method 1:

    [2269] A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer or DMSO according to its solubility. A similar stock of the reference compound chlorpromazine is also prepared as a positive control. Eleven dilutions (5× assay concentration) of the compound of the disclosure and chlorpromazine are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 pM to 10 μM.

    [2270] A stock concentration of 5 nM [.sup.3H]LSD (lysergic acid diethyl amide) is prepared in 50 mM Tris-HCl, 10 mM MgCl.sub.2, 1 mM EDTA, pH 7.4 (Assay Buffer). Aliquots (50 μl) of radioligand are dispensed into the wells of a 96-well plate containing 100 μl of Assay Buffer. Duplicate 50-μl aliquots of the compound of the disclosure test and chlorpromazine positive control reference compound serial dilutions are added.

    [2271] Membrane fractions of cells expressing recombinant 5HT.sub.7 receptors (50 μL) are dispensed into each well. The membranes are prepared from stably transfected cell lines expressing 5HT.sub.7 receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000×g, decanting the supernatant and storing at −80° C.; the membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before using in the assay.

    [2272] The 250-μl reactions are incubated at room temperature for 1.5 hours, then harvested by rapid filtration onto 0.3% polyethyleneimine-treated, 96-well filter mats using a 96-well Filtermate harvester. Four rapid 500-μl washes are performed with chilled Assay Buffer to reduce non-specific binding The filter mats are dried, then scintillant is added to the filters and the radioactivity retained on the filters is counted in a Microbeta scintillation counter.

    [2273] Raw data (dpm) representing total radioligand binding (i.e., specific+non-specific binding) are plotted as a function of the logarithm of the molar concentration of the competitor (i.e., test or reference compound). Non-linear regression of the normalized (i.e., percent radioligand binding compared to that observed in the absence of test or reference compound) raw data is performed in Prism 4.0 (GraphPad Software) using the built-in three parameter logistic model describing ligand competition binding to radioligand-labeled sites:


    y=bottom+[(top-bottom)/(1+10×-log IC.sub.50)]

    [2274] where bottom equals the residual radioligand binding measured in the presence of 10 μM reference compound (i.e., non-specific binding) and top equals the total radioligand binding observed in the absence of competitor. The log IC.sub.50 (i.e., the log of the ligand concentration that reduces radioligand binding by 50%) is thus estimated from the data and used to obtain the Ki by applying the Cheng-Prusoff approximation:


    Ki=IC.sub.50/(1+[ligand]/KD)

    [2275] where [ligand] equals the assay radioligand concentration and KD equals the affinity constant of the radioligand for the target receptor.

    [2276] Compounds of the disclosure are also screened at a single concentration of 10 μM using the same method described for the Radiolabel Binding Studies for Serotonin 5HT.sub.7 receptors to determine the percent inhibition of [.sup.3H]LSD binding.

    [2277] Radiolabel Binding Studies for Serotonin 5-HT7 Receptors, Method 2:

    [2278] A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer or DMSO according to its solubility. A similar stock of the reference compound chlorpromazine is also prepared as a positive control. Eleven dilutions (5× assay concentration) of the compound of the disclosure and chlorpromazine are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 μM to 10 μM.

    [2279] A stock concentration of 5 nM [.sup.3H]-5-Hydroxytryptamine ([.sup.3H]-5HT) is prepared in 50 mM Tris-HCl, 10 mM MgCl.sub.2, 1 mM EDTA, pH 7.4 (Assay Buffer). Aliquots (50 μl) of radioligand are dispensed into the wells of a 96-well plate containing 100 μl of Assay Buffer. Duplicate 50-μl aliquots of the compound of the disclosure test and chlorpromazine positive control reference compound serial dilutions are added.

    [2280] Membrane fractions of cells expressing recombinant 5HT.sub.7 receptors (50 μL) are dispensed into each well. The membranes are prepared from stably transfected cell lines expressing 5HT.sub.7 receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000× g, decanting the supernatant and storing at −80° C.; the membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before using in the assay.

    [2281] The 250 μl reactions are incubated at room temperature for 1.5 hours, then harvested by rapid filtration onto 0.3% polyethyleneimine-treated, 96-well filter mats using a 96-well Filtermate harvester. Four rapid 500-μl washes are performed with chilled Assay Buffer to reduce non-specific binding The filter mats are dried, then scintillant is added to the filters and the radioactivity retained on the filters is counted in a Microbeta scintillation counter.

    [2282] Raw data (dpm) representing total radioligand binding (i.e., specific+non-specific binding) are plotted as a function of the logarithm of the molar concentration of the competitor (i.e., test or reference compound). Non-linear regression of the normalized (i.e., percent radioligand binding compared to that observed in the absence of test or reference compound) raw data is performed in Prism 4.0 (GraphPad Software) using the built-in three parameter logistic model describing ligand competition binding to radioligand-labeled sites:


    y=bottom+[(top-bottom)/(1+10×-log IC.sub.50)]

    [2283] where bottom equals the residual radioligand binding measured in the presence of 10 μM reference compound (i.e., non-specific binding) and top equals the total radioligand binding observed in the absence of competitor. The log IC.sub.50 (i.e., the log of the ligand concentration that reduces radioligand binding by 50%) is thus estimated from the data and used to obtain the Ki by applying the Cheng-Prusoff approximation:


    Ki=IC.sub.50/(1+[ligand]/KD)

    [2284] where [ligand] equals the assay radioligand concentration and KD equals the affinity constant of the radioligand for the target receptor.

    [2285] Compounds of the disclosure are also screened at a single concentration of 10 μM using the same method described for the Radiolabel Binding Studies for Serotonin 5HT.sub.7 receptors to determine the percent inhibition of [.sup.3H]-5HT binding.

    [2286] Functional Serotonin 5HT7 Assay, Method 1:

    [2287] Cell lines stably expressing human 5HT.sub.7 receptors are seeded in 96-well, poly-L-lysine-coated plates 48 hours prior to the assay (40,000 cells per well) in Dulbecco's Modified Eagle Medium (DMEM) containing 5% dialyzed serum. Twenty hours prior to the assay, the medium is changed to serum-free DMEM. On the day of the assay, the DMEM is washed and replaced with 30 μl of assay buffer (1× Krebs-Ringer bicarbonate glucose buffer, 0.75 mM IBMX, pH 7.4). A 10-min pre-incubation is performed in a 37-degree centigrade, humidified incubator. Then, the cells are stimulated by addition of 30 μl of 2× dilutions of compounds of the disclosure or chlorpromazine (final concentrations ranging from 0.1 nM to 10 μM, each concentration assayed in triplicate). A positive control (100 μM forskolin) is also included. Accumulation of cAMP is allowed to continue for 15 min, after which the buffer is removed and the cells are lysed with Cell Lysis Buffer (CatchPoint cAMP Assay Kit, Molecular Devices). Next, the lysates are transferred to 96-well, glass-bottom plates coated with goat anti-rabbit IgG and adsorbed with rabbit anti-cAMP (Molecular Devices). Following a 5 minute incubation, horseradish peroxidase-cAMP conjugate is added (Molecular Devices) and a 2-hour incubation is performed at room temperature. Then, after three washes with Wash Buffer (Molecular Devices), Stoplight Red substrate (Molecular Devices), reconstituted in Substrate Buffer (Molecular Devices) containing freshly-added 1 mM H.sub.2O.sub.2, is added and, after a 15-min incubation at room temperature, fluorescence is measured (excitation 510-545 nm, emission 565-625 nm). For each assay, a cAMP calibration curve is generated and controls without lysate and without antibody are included.

    [2288] For agonist tests, raw data (maximum fluorescence, fluorescence units) for each concentration of the compounds of the disclosure or chlorpromazine are normalized to the basal (vehicle-stimulated) fluorescence (reported as fold increase over basal) and plotted as a function of the logarithm of the molar concentration of the drug (i.e., test or reference compound). Non-linear regression of the normalized data is performed in Prism 4.0 (GraphPad Software) using the built-in three parameter logistic model (i.e., sigmoidal concentration-response) describing agonist-stimulated activation of one receptor population:


    y=bottom+[(top-bottom)/(1+10×-log EC.sub.50)]

    [2289] where bottom equals the best-fit basal fluorescence and top equals the best-fit maximal fluorescence stimulated by the compound of the disclosure or chlorpromazine. The log EC.sub.50 (i.e., the log of the drug concentration that increases fluorescence by 50% of the maximum fluorescence observed for the compound of the disclosure or chlorpromazine is thus estimated from the data, and the EC.sub.50 (agonist potency) is obtained. To obtain an estimate of the relative efficacy of the test compound (Rel. Emax), its best-fit top is compared to and expressed as a ratio of that for the chlorpromazine (Rel. Emax of the reference agonist is 1.00).

    [2290] To ascertain whether compounds of the disclosure are antagonists, a double-addition paradigm is employed. First, 30 μl of a compound of the disclosure (20 μM) is added (10 μM final concentration) and a 15 minute incubation is performed. Then, 30 μl of chlorpromazine (3×; EC.sub.90) is added (final concentration of agonist is EC30) and cAMP accumulation is allowed to proceed for 15 minutes. The samples are then processed for cAMP measurements as detailed above. Measurements of chlorpromazine-induced cAMP accumulation are compared to the signals elicited by the chlorpromazine following addition of vehicle instead of test compound and expressed as a ratio. ‘Hits’ (compounds that antagonize chlorpromazine -stimulated increases in baseline-normalized fluorescence by at least 50%) are then characterized by a modified Schild analysis.

    [2291] For modified Schild analysis, a family of chlorpromazine concentration-response isotherms is generated in the absence and presence of graded concentrations of test compound (added 15 min prior to reference agonist). Theoretically, compounds that are competitive antagonists cause a dextral shift of agonist concentration-response isotherms without reducing the maximum response to agonist (i.e., surmountable antagonism). However, on occasion, factors such as non-competitive antagonism, hemiequilibria, and/or receptor reserve cause apparent insurmountable antagonism. To account for such deviations, we apply the modified Lew-Angus method to ascertain antagonist potency (Christopoulos et al., 1999). Briefly, equieffective concentrations of agonist (concentrations of agonist that elicit a response equal to the EC.sub.25% of the agonist control curve) are plotted as a function of the compound of the disclosure concentration present in the wells in which they were measured. Non-linear regression of the baseline-normalized data is performed in Prism 4.0 using the following equation:


    pEC25%=−log([B]+10−pK)−log c

    [2292] where EC25% equals the concentration of agonist that elicits a response equal to 25% of the maximum agonist control curve response and [B] equals the antagonist concentration; K, c, and s are fit parameters. The parameter s is equal to the Schild slope factor. If s is not significantly different from unity, pK equals pKB; otherwise, pA2 is calculated (pA2=pK/s). The parameter c equals the ratio EC.sub.25%/[B].

    [2293] Functional Efficacy Assay for 5-HT.sub.7 Receptors Method 2:

    [2294] Functional efficacy of the compounds of the disclosure on 5-HT.sub.7 serotonin receptors were measured in a cell based cAMP enzyme fragment complementation assay using the HitHunter cAMP assay (DiscoveRx). Cells stably expressing human 5HT7 receptors were plated in 96-well plates at 4000 cells/well, 16-20 hours prior to assay in growth media (Ultraculture medium, 2 mM GlutaMax and G418 1 mg/mL. Serial dilutions of the agonist, 5-Carboxamidotryptamine (5-CT), were prepared in a final concentration range of 10 μM to 10 nM. Compounds of the disclosure were prepared in 3-fold serial dilutions to obtain a final concentration range of 10 μM to 0.1 nM. Compounds of the disclosure are tested for agonist activity in the absence of 5-CT and antagonist activity in the presence of 5-CT. For the cAMP assay, the protocol was followed according to the instructions provided by the supplier. Briefly, cells were incubated with a compound of the disclosure for 30 minutes at 37° C. prior to addition of EC7o concentration of 5-CT. After an additional 30 minutes, cAMP antibody/cell lysis solution was added (20 μL/well) and incubated for 60 minutes at room temperature. cAMP XS+EA reagent is added (20 μL/well) and incubated for 2 hours at room temperature. Luminescence was read on the Envision Multilabel plate reader.

    [2295] The disclosures of each and every patent, patent application, and publication cited herein are hereby incorporated herein by reference in their entirety.

    [2296] While this invention has been disclosed with reference to specific embodiments, it is apparent that other embodiments and variations of this invention may be devised by others skilled in the art without departing from the true spirit and scope of the invention. The appended claims are intended to be construed to include all such embodiments and equivalent variations.

    Example 4

    Biochemical Experiments

    Methods:

    [2297] .sup.1Radiolabeled Binding (IC.sub.50 and K.sub.1)

    [2298] A solution of the compound of the disclosure to be tested was prepared as a 1-mg/ml stock in Assay Buffer or DMSO according to its solubility. A similar stock of the reference compound chlorpromazine was also prepared as a positive control. Eleven dilutions (5 x assay concentration) of the compound of the disclosure and chlorpromazine were prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 pM to 10 μM.

    [2299] A stock concentration of 5 nM [.sup.3H]LSD (lysergic acid diethyl amide) was prepared in 50 mM Tris-HCl, 10 mM MgCl.sub.2, 1 mM EDTA, pH 7.4 (Assay Buffer). Aliquots (50 μl) of radioligand were dispensed into the wells of a 96-well plate containing 100 μl of Assay Buffer. Duplicate 50 μl aliquots of the compound of the disclosure test and chlorpromazine positive control reference compound serial dilutions were added.

    [2300] Membrane fractions of cells expressing recombinant 5HT.sub.7 receptors (50 μL) were dispensed into each well. The membranes were prepared from stably transfected cell lines expressing 5HT.sub.7 receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000×g, decanting the supernatant and storing at −80° C.; the membrane preparations were resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before using in the assay.

    [2301] The 250 μl reactions were incubated at room temperature for 1.5 hours, then harvested by rapid filtration onto 0.3% polyethyleneimine-treated, 96-well filter mats using a 96-well Filtermate harvester. Four rapid 500-μl washes were performed with chilled Assay Buffer to reduce non-specific binding The filter mats were dried, then scintillant is added to the filters and the radioactivity retained on the filters was counted in a Microbeta scintillation counter.

    [2302] Raw data (dpm) representing total radioligand binding (i.e., specific+non-specific binding) was plotted as a function of the logarithm of the molar concentration of the competitor (i.e., test or reference compound). Non-linear regression of the normalized (i.e., percent radioligand binding compared to that observed in the absence of test or reference compound) raw data was performed in Prism 4.0 (GraphPad Software) using the built-in three parameter logistic model describing ligand competition binding to radioligand-labeled sites:


    y=bottom+[(top-bottom)/(1+10×-logIC.sub.50)]

    where bottom equals the residual radioligand binding measured in the presence of 10 μM reference compound (i.e., non-specific binding) and top equals the total radioligand binding observed in the absence of competitor. The log IC.sub.50 (i.e., the log of the ligand concentration that reduces radioligand binding by 50%) was thus estimated from the data and used to obtain the Ki by applying the Cheng-Prusoff approximation:


    Ki =IC.sub.50/(1+[ligand]/KD)

    where [ligand] equals the assay radioligand concentration and KD equals the affinity constant of the radioligand for the target receptor.

    Functional Data (K.SUB.b.)

    [2303] Functional efficacy of the compounds of the disclosure on 5-HT.sub.7 serotonin receptors were measured in a cell based cAMP enzyme fragment complementation assay using the HitHunter cAMP assay (DiscoveRx). Cells stably expressing human 5HT.sub.7 receptors were plated in 96-well plates at 4000 cells/well, 16-20 hours prior to assay in growth media (Ultraculture medium, 2 mM GlutaMax and G418 1 mg/mL. Serial dilutions of the agonist, 5-hydroxytryptamine (5-HT), were prepared in a final concentration range of 10 μM to 10 nM. Compounds of the disclosure were prepared in 3-fold serial dilutions to obtain a final concentration range of 10 μM to 0.1 nM. Compounds of the disclosure are tested for agonist activity in the absence of 5-HT and antagonist activity in the presence of 5-HT. For the cAMP assay, the protocol was followed according to the instructions provided by the supplier. Briefly, cells were incubated with a compound of the disclosure for 30 minutes at 37° C. prior to addition of EC.sub.70 concentration of 5-HT. After an additional 30 minutes, cAMP antibody/cell lysis solution was added (20 μL/well) and incubated for 60 minutes at room temperature. cAMP XS+EA reagent is added (20 μL/well) and incubated for 2 hours at room temperature. Luminescence was read on the Envision Multilabel plate reader.

    Results

    [2304] ##STR00614##

    TABLE-US-00034 TABLE 34 IC.sub.50 K.sub.i K.sub.b n R.sup.1 R.sup.2 R.sup.3 (nM).sup.1 (nM).sup.1 (nM).sup.2 TPSA 2 Ethyl Ethyl 4-F-Phenyl 8.5 8.98 35.6 2 Ethyl Ethyl 4-Cl-Phenyl 13 54.6 35.6 2 Ethyl Ethyl 2-iPr-phenyl 23 163 35.6 2 Ethyl Ethyl 2-morpholino- 24 32.3 48.1 phenyl 2 Ethyl Ethyl 4-Me-Phenyl 28 24.1 35.6 2 Ethyl Ethyl 4-OH-Phenyl 34 50 55.8 2 Ethyl Ethyl Phenyl 68 17.8 35.6 2 Ethyl Ethyl 4-Me-2- 74 59.3 48.1 morpholino-phenyl

    ##STR00615##

    TABLE-US-00035 TABLE 35 IC.sub.50 K.sub.i K.sub.b n R.sup.1 R.sup.2 R.sup.3 (nM).sup.1 (nM).sup.1 (nM).sup.2 TPSA 1 Ethyl Ethyl 2-iPr-phenyl 121 35.6 1 Ethyl Ethyl 4-Me-2- 132 43.8 48.1 morpholino-phenyl 1 Ethyl Ethyl 4-F-Phenyl 243 35.6 1 Ethyl Ethyl 4-Me-Phenyl 249 35.6 1 Ethyl Ethyl 2-pyridyl 669 48.5 1 Ethyl Ethyl Phenyl 819 35.6 1 Ethyl Ethyl 3-Cl-Phenyl 1087 35.6 2 Ethyl Ethyl 4-Me-Phenyl 11 8.43 35.6 2 Ethyl Ethyl 4-F-Phenyl 12.34 0.81 35.6 2 Ethyl Ethyl 3,4-di-Cl-Phenyl 82.8 6.19 35.6 2 Ethyl Ethyl 4-F-3-Cl-Phenyl 8.7 1.92 35.6 2 Ethyl Ethyl 3-Cl-Phenyl 9.9 1.38 35.6 2 Ethyl Ethyl Phenyl 6.59 35.6 2 Ethyl Ethyl 2-Cl-Phenyl 109 35.6 2 Ethyl Ethyl 3-F-Phenyl 9.89 35.6 2 Ethyl Ethyl 2-Me-Phenyl 127 35.6 2 Ethyl Ethyl 3-Me-Phenyl 1.65 35.6 2 Ethyl Ethyl 2-pyridyl 4.91 48.5 2 Ethyl Ethyl 2-OMe-Phenyl 230 44.8 2 Ethyl Ethyl 4-CN-Phenyl 544 59.4 2 Ethyl Ethyl 4-CF.sub.3-Phenyl 137 35.6

    ##STR00616##

    TABLE-US-00036 TABLE 36 IC.sub.50 K.sub.i K.sub.b n R.sup.1 R.sup.2 R.sup.3 (nM).sup.1 (nM).sup.1 (nM).sup.2 TPSA 2 Ethyl Ethyl 4-Me-Phenyl 79 58.1 35.6 2 —CH.sub.2CH═CHCH.sub.2— 4-F-Phenyl 46.2 35.6 2 —CH.sub.2CH═CHCH.sub.2— 3-Cl-Phenyl 36.3 35.6 2 —CH.sub.2CH.sub.2CH.sub.2CH.sub.2— 4-F-Phenyl 52.6 35.6 2 —CH.sub.2CH.sub.2CH.sub.2CH.sub.2— 3-Cl-Phenyl 48.4 35.6

    ##STR00617##

    TABLE-US-00037 TABLE 37 IC.sub.50 K.sub.i K.sub.b n R.sup.3 R.sup.7 (nM).sup.1 (nM).sup.1 (nM).sup.2 TPSA 2 3-Cl-Phenyl Acetyl 63 5.04 55.9 2 4-F-Phenyl Acetyl 76 14.4 55.9 2 4-F-Phenyl MeSO.sub.2 89 30.7 81.3 2 3-Cl-Phenyl MeSO.sub.2 107 13.5 81.3 3 3-Cl-Phenyl MeSO.sub.2 321 81.3 3 4-F-Phenyl MeSO.sub.2 526 81.3

    ##STR00618##

    TABLE-US-00038 TABLE 38 IC.sub.50 K.sub.i K.sub.b n R.sup.3 R.sup.7 (nM).sup.1 (nM).sup.1 (nM).sup.2 TPSA 2 3-Cl-Phenyl MeSO.sub.2 117 81.3 2 4-F-Phenyl MeSO.sub.2 167 74.2 81.3 2 3-Cl-Phenyl Acetyl 214 55.9 2 4-F-Phenyl Acetyl 325 55.9

    ##STR00619##

    TABLE-US-00039 TABLE 39 IC.sub.50 K.sub.i K.sub.b n R.sup.1 R.sup.2 R.sup.3 (nM).sup.1 (nM).sup.1 (nM).sup.2 TPSA 2 Ethyl Ethyl Phenyl 144 35.6

    [2305] From the foregoing description, one skilled in the art can easily ascertain the essential characteristics of this invention, and without departing from the spirit and scope thereof, can make various changes and modifications of the invention to adapt it to various usages and conditions.

    [2306] All references, patents or applications, U.S. or foreign, cited in the application are hereby incorporated by reference as if written herein in their entireties. Where any inconsistencies arise, material literally disclosed herein controls.