Pyrazole derivative and harmful organism-controlling agent
11964957 · 2024-04-23
Assignee
Inventors
- Ryo Ishikawa (Tokyo, JP)
- Akira KINPARA (TOKYO, JP)
- Keiji TORIYABE (Tokyo, JP)
- Akira WATANABE (Tokyo, JP)
- Masao NAKATANI (TOKYO, JP)
- Akira TAKANEZAWA (Tokyo, JP)
- Takeshi Matsuda (Tokyo, JP)
Cpc classification
A01N43/66
HUMAN NECESSITIES
A01N25/04
HUMAN NECESSITIES
A01N43/80
HUMAN NECESSITIES
C07D401/04
CHEMISTRY; METALLURGY
A01N43/707
HUMAN NECESSITIES
International classification
C07D401/04
CHEMISTRY; METALLURGY
A01N25/04
HUMAN NECESSITIES
Abstract
Embodiments provide a pest control agent that is excellent in safety, controlling effect, residual activity, and so on. According to an embodiment, there is provided a pyrazole derivative represented by general formula [I], or an agriculturally acceptable salt thereof, and a pest control agent containing the same as an active ingredient: ##STR00001## wherein, p represents an integer of 0 or 1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 represent a hydrogen atom, halogen atom, C.sub.1-C.sub.6 alkyl group, or the like, A represents an oxygen atom or sulfur atom, Q represents a halogen atom, C.sub.6-C.sub.10 aryl group that is unsubstituted or substituted with (R.sup.8).sub.m, or the like, and R.sup.6 and R.sup.7 represent a hydrogen atom, C.sub.1-C.sub.6 alkyl group, or the like.
Claims
1. A pyrazole derivative represented by general formula [I] or an agriculturally acceptable salt thereof ##STR00028## wherein, p represents an integer of 0, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 each independently represent a hydrogen atom, A represents an oxygen atom, Q represents a C.sub.6-C.sub.10 aryl group that is substituted with (R.sup.8).sub.m, R.sup.6 and R.sup.7 each independently represent a hydrogen atom, R.sup.8 represents a hydrogen atom, halogen atom, hydroxy group, a C.sub.1-C.sub.6 alkyl group, C.sub.1-C.sub.6 haloalkyl group, C.sub.3-C.sub.6 cycloalkyl group, C.sub.2-C.sub.6 alkenyl group C.sub.2-C.sub.6 alkynyl group, C.sub.1-C.sub.6 haloalkoxy group, C.sub.3-C.sub.6 cycloalkoxy group, C.sub.1-C.sub.6 alkylthio group, C.sub.1-C.sub.6 alkylsulfinyl group, C.sub.1-C.sub.6 alkylsulfonyl group, C.sub.1-C.sub.6 haloalkylthio group, C.sub.1-C.sub.6 haloalkylsulfinyl group, C.sub.1-C.sub.6 alkylcarbonyl group, C.sub.1-C.sub.6 alkoxycarbonyl group, aminocarbonyl group, di(C.sub.1-C.sub.6 alkyl)amino C.sub.1-C.sub.6-alkyl group, -hydroxy C.sub.1-C.sub.6 alkyl group, C.sub.1-C.sub.6 alkoxy C.sub.1-C.sub.6 alkyl group, C.sub.1-C.sub.6 alkylcarbonyloxy group, -di(C.sub.1-C.sub.6 alkyl)aminocarbonyloxy group, C.sub.1-C.sub.6 alkylsulfonyloxy group, C.sub.1-C.sub.6 alkylthio C.sub.1-C.sub.6 alkyl group, C.sub.1-C.sub.6 haloalkylthio C.sub.1-C.sub.6 alkyl group, -phenyl group, benzyloxy group, amino group, mono(C.sub.1-C.sub.6 alkyl)amino group, di(C.sub.1-C.sub.6 alkyl)amino group, carboxy group, 1,3-dioxolane-2-yl group, -(methyloxyimino)methyl group, cyano group, or nitro group, and further, neighboring two R.sup.8s may form, together with a carbon atom bound to each R.sup.8, a 4 to 8-membered carbon ring, or a 4 to 8-membered hetero ring having 1 to 4 hetero atoms selected from an oxygen atom, m represents a number of chemically acceptable R.sup.8s and is an integer of 0 to 7, R.sup.8s may be the same or different from each other when m is 2 or more.
2. A agrochemical composition comprising the pyrazole derivative or an agriculturally acceptable salt thereof according to claim 1 as an active ingredient.
3. The agrochemical composition according to claim 2, wherein the agrochemical composition further comprises a surfactant.
4. A pest control agent comprising the pyrazole derivative or an agriculturally acceptable salt thereof according to claim 1 as an active ingredient.
5. The pest control agent according to claim 4 that is an insecticide.
6. The pest control agent according to claim 4 having a control effect on a pest in a dry field or a paddy field where a farming or gardening plant is cultured.
7. The pest control agent according to claim 6, wherein the farming or gardening plant is a plant provided with tolerance by a breeding method or a gene recombination technique.
Description
DESCRIPTION OF THE PREFERRED EMBODIMENTS
(1) Symbols and terms used in this specification are described.
(2) In the present invention, pest control agent means insecticides, miticides, nematocides, and the like in farming and gardening fields, for animals such as domestic animals and pets, for household use or for prevention of epidemics.
(3) In the present invention, halogen atom refers to a fluorine atom, a chlorine atom, a bromine atom, or an iodine atom.
(4) In the present invention, unless otherwise specified, C.sub.6-C.sub.10 aryl group refers to an aromatic hydrocarbon group having 6 to 10 carbon atoms, and examples of the C.sub.6-C.sub.10 aryl group include a phenyl, naphthalene-1-yl, or naphthalene-2-yl group.
(5) In the present invention, unless otherwise specified, heteroaryl group refers to an aromatic heterocyclic or condensed heterocyclic group, and examples of the heteroaryl group include a pyrrolyl, furanyl, thienyl, pyrazolyl, oxazolyl, isoxazolyl, imidazolyl, 1,2,4-oxadiazolyl, 1,2,3-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,4-triazolyl, 1,2,3-triazolyl, thiazolyl, isothiazolyl, 1,2,4-thiadiazolyl, 1,2,3-thiadiazolyl, 1,3,4-thiadiazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, benzofuranyl, benzothienyl, indolyl, benzoxazolyl, benzoimidazolyl, benzotriazolyl, benzothiazolyl, quinolinyl, quinazolinyl, quinoxalinyl, phthalazinyl, or naphthyridinyl group.
(6) In the present invention, unless otherwise specified, C.sub.1-C.sub.3 alkyl group refers to a linear or branched alkyl group having 1 to 3 carbon atoms, and examples of the C.sub.1-C.sub.3 alkyl group include a methyl, ethyl, n-propyl, or isopropyl group.
(7) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 alkyl group refers to a linear or branched alkyl group having 1 to 6 carbon atoms, and examples of the C.sub.1-C.sub.6 alkyl group include, in addition to those exemplified in the C.sub.1-C.sub.3 alkyl group, a n-butyl, s-butyl, isobutyl, tert-butyl, n-pentyl, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl, 1-ethylpropyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, neopentyl, n-hexyl, 1-methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl, 1-ethylbutyl, 2-ethylbutyl, 1,1-dimethylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl, 2,2-dimethylbutyl, 2,3-dimethylbutyl, 3,3-dimethylbutyl, 1,1,2-trimethylpropyl, 1,2,2-trimethylpropyl, 1-ethyl-1-methylpropyl, or 1-ethyl-2-methylpropyl group.
(8) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 haloalkyl group refers to a linear or branched alkyl group having 1 to 6 carbon atoms, substituted with 1 to 13 same or different halogen atoms, and refers to, for example, a haloalkyl group, and examples of the C.sub.1-C.sub.6 haloalkyl group include a fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, bromomethyl, dibromomethyl, tribromomethyl, iodomethyl, chlorodifluoromethyl, dichlorofluoromethyl, 1-fluoroethyl, 2-fluoroethyl, 1,1-difluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, 1,1,2,2-tetrafluoroethyl, pentafluoroethyl, 1-chloroethyl, 2-chloroethyl, 1,1-dichloroethyl, 2,2-dichloroethyl, 2,2,2-trichloroethyl, 1,1,2,2-tetrachloroethyl, pentachloroethyl, 1-bromoethyl, 2-bromoethyl, 2,2,2-tribromoethyl, 1-iodoethyl, 2-iodoethyl, 2-chloro-2,2-difluoroethyl, 2,2-dichloro-2-fluoroethyl, 1-fluoropropyl, 2-fluoropropyl, 3-fluoropropyl, 1,1-difluoropropyl, 2,2-difluoropropyl, 3,3-difluoropropyl, 3,3,3-trifluoropropyl, 2,2,3,3,3-pentafluoropropyl, 1,1,2,3,3,3-hexafluoropropyl, heptafluoropropyl, 1-fluoropropane-2-yl, 2-fluoropropane-2-yl, 1,1-difluoropropane-2-yl, 1,2-difluoropropane-2-yl, 1,3-difluoropropane-2-yl, 1,2,3-trifluoropropane-2-yl, 1,1,3,3-tetrafluoropropane-2-yl, 1,1,1,3,3,3-hexafluoropropane-2-yl, heptafluoropropane-2-yl, 1-chloropropyl, 2-chloropropyl, 3-chloropropyl, 1,1-dichloropropyl, 2,2-dichloropropyl, 3,3-dichloropropyl, 3,3,3-trichloropropyl, 2,2,3,3,3-pentachloropropyl, heptachloropropyl, 1-chloropropane-2-yl, 2-chloropropane-2-yl, 1,1-dichloropropane-2-yl, 1,2-dichloropropane-2-yl, 1,3-dichloropropane-2-yl, 1,2,3-trichloropropane-2-yl, 1,1,3,3-tetrachloropropane-2-yl, 1,1,1,3,3,3-hexachloropropane-2-yl, heptachloropropane-2-yl, 1-bromopropyl, 2-bromopropyl, 3-bromopropyl, 1-bromopropane-2-yl, 2-bromopropane-2-yl, 1-iodopropyl, 2-iodopropyl, 3-iodopropyl, 1-iodopropane-2-yl, 2-iodopropane-2-yl, 1-fluorobutyl, 2-fluorobutyl, 3-fluorobutyl, 4-fluorobutyl, 4,4-difluorobutyl, 4,4,4-trifluorobutyl, 3,3,4,4,4-pentafluorobutyl, 2,2,3,3,4,4,4-heptafluorobutyl, nonafluorobutyl, 1,1,1-trifluorobutane-2-yl, 4,4,4-trifluorobutane-2-yl, 3,3,4,4,4-pentafluorobutane-2-yl, nonafluorobutane-2-yl, 1,1,1,3,3,3-hexafluoro-2-(trifluoromethyl)propane-2-yl, 2,2,3,4,4,4-hexafluorobutyl, 1-chlorobutyl, 2-chlorobutyl, 3-chlorobutyl, 4-chlorobutyl, 4,4-dichlorobutyl, 4,4,4-trichlorobutyl, nonachlorobutyl, 1,1,1-trichlorobutane-2-yl, 4,4,4-trichlorobutane-2-yl, nonachlorobutane-2-yl, 1-bromobutyl, 2-bromobutyl, 3-bromobutyl, 4-bromobutyl, 1-iodobutyl, 2-iodobutyl, 3-iodobutyl, 4-iodobutyl, 4-chloro-1,1,2,2,3,3,4,4-octafluorobutyl, 4-bromo-1,1,2,2,3,3,4,4-octafluorobutyl, 1-fluoropentyl, 2-fluoropentyl, 3-fluoropentyl, 4-fluoropentyl, 5-fluoropentyl, 5,5,5-trifluoropentyl, 4,4,5,5,5-pentafluoropentyl, 3,3,4,4,5,5,5-heptafluoropentyl, 2,2,3,3,4,4,5,5-octafluoropentyl, 2,2,3,3,4,4,5,5,5-nonafluoropentyl, undecafluoropentyl, 4,4,4-trifluoro-3-methylbutyl, 1-chloropentyl, 2-chloropentyl, 3-chloropentyl, 4-chloropentyl, 5-chloropentyl, 5,5,5-trichloropentyl, 4,4,5,5,5-pentachloropentyl, 3,3,4,4,5,5,5-heptachloropentyl, 2,2,3,3,4,4,5,5,5-nonachloropentyl, undecachloropentyl, 1-bromopentyl, 2-bromopentyl, 3-bromopentyl, 4-bromopentyl, 5-bromopentyl, 5-iodopentyl, 1-fluorohexyl, 2-fluorohexyl, 3-fluorohexyl, 4-fluorohexyl, 5-fluorohexyl, 6-fluorohexyl, 6,6,6-trifluorohexyl, 5,5,6,6,6-pentafluorohexyl, 4,4,5,5,6,6,6-heptafluorohexyl, 3,3,4,4,5,5,6,6,6-nonafluorohexyl, 2,2,3,3,4,4,5,5,6,6-decafluorohexyl, 2,2,3,3,4,4,5,5,6,6,6-undecafluorohexyl, tridecafluorohexyl, 1-chlorohexyl, 2-chlorohexyl, 3-chlorohexyl, 4-chlorohexyl, 5-chlorohexyl, 6-chlorohexyl, 5-bromohexyl, 6-bromohexyl, 5-iodohexyl, or 6-iodohexyl group.
(9) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 alkoxy group refers to a (C.sub.1-C.sub.6 alkyl)-O group in which the alkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkoxy group include a methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, isobutoxy, sec-butoxy, tert-butoxy, n-pentoxy, 1-methylbutoxy, 2-methylbutoxy, 3-methylbutoxy, 1-ethylpropoxy, 1,1-dimethylpropoxy, 1,2-dimethylpropoxy, or n-hexyloxy group.
(10) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 haloalkoxy group refers to a (C.sub.1-C.sub.6 haloalkyl)-O group in which the haloalkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 haloalkoxy group include difluoromethoxy, dichloromethoxy, trifluoromethoxy, trichloromethoxy, tribromomethoxy, chlorodifluoromethoxy, bromodifluoromethoxy, 2-fluoroethoxy, 1-chloroethoxy, 2-chloroethoxy, 1-bromoethoxy, 2-bromoethoxy, 2,2-difluoroethoxy, 1,2-dichloroethoxy, 2,2-dichloroethoxy, 2,2,2-trifluoroethoxy, 2,2,2-trichloroethoxy, 1,1,2,2-tetrafluoroethoxy, pentafluoroethoxy, 2-bromo-2-chloroethoxy, 2-chloro-1,1,2,2-tetrafluoroethoxy, 1-chloro-1,2,2,2-tetrafluoroethoxy, 1-chloropropoxy, 2-chloropropoxy, 3-chloropropoxy, 2-bromopropoxy, 3-bromopropoxy, 2-bromo-1-methylethoxy, 3-iodopropoxy, 2,3-dichloropropoxy, 2,3-dibromopropoxy, 3,3,3-trifluoropropoxy, 3,3,3-trifluoro-2-propoxy, 3,3,3-trichloropropoxy, 3-bromo-3,3-difluoropropoxy, 2,2-difluoropropoxy, 3,3-dichloro-3-fluoropropoxy, 2,2,3,3-tetrafluoropropoxy, 1-bromo-3,3,3-trifluoropropoxy, 2,2,3,3,3-pentafluoropropoxy, 2,2,2-trifluoro-1-trifluoromethylethoxy, heptafluoropropoxy, heptafluoro-2-propoxy, 1,2,2,2-tetrafluoro-1-trifluoromethylethoxy, 1,1,2,3,3,3-hexafluoropropoxy, 2-chlorobutoxy, 3-chlorobutoxy, 4-chlorobutoxy, 2-chloro-1,1-dimethylethoxy, 4-bromobutoxy, 3-bromo-2-methylpropoxy, 2-bromo-1,1-dimethylethoxy, 2,2-dichloro-1,1-dimethylethoxy, 2-chloro-1-chloromethyl-2-methylethoxy, 4,4,4-trifluorobutoxy, 3,3,3-trifluoro-1-methylpropoxy, 3,3,3-trifluoro-2-methylpropoxy, 2,3,4-trichlorobutoxy, 2,2,2-trichloro-1,1-dimethylethoxy, 4-chloro-4,4-difluorobutoxy, 4,4-dichloro-4-fluorobutoxy, 4-bromo-4,4-difluorobutoxy, 2,4-dibromo-4,4-difluorobutoxy, 3,4-dichloro-3,4,4-trifluorobutoxy, 3,3-dichloro-4,4,4-trifluorobutoxy, 4-bromo-3,3,4,4-tetrafluorobutoxy, 4-bromo-3-chloro-3,4,4-trifluorobutoxy, 2,2,3,3,4,4-hexafluorobutoxy, 2,2,3,4,4,4-hexafluorobutoxy, 2,2,2-trifluoro-1-methyl-1-trifluoromethylethoxy, 3,3,3-trifluoro-2-trifluoromethylpropoxy, 2,2,3,3,4,4,4-heptafluorobutoxy, 3,3,4,4,4-pentafluoro-2-butoxy, 2,3,3,3-tetrafluoro-2-trifluoromethylpropoxy, 1,1,2,2,3,3,4,4-octafluorobutoxy, nonafluorobutoxy, perfluoro-tert-butoxy, 4-chloro-1,1,2,2,3,3,4,4-octafluorobutoxy, 5,5,5-trifluoropentoxy, 4,4,5,5,5-pentafluoropentoxy, 3,3,4,4,5,5,5-heptafluoropentoxy, 3,3,4,4,5,5,5-heptafluoro-2-pentoxy, 2,2,3,3,4,4,5,5,5-nonafluoropentoxy, 2,2,3,3,4,4,5,5-octafluoropentoxy, perfluoropentoxy, 4,4,5,5,5-pentafluoro-2-butoxy, 2,2-bis(trifluoromethyl)propoxy, 2,2,3,3,4,4,5,5,6,6,6-undecafluorohexyloxy, 3,3,4,4,5,5,6,6,6-nonafluorohexyloxy, 4,4,5,5,6,6,6-heptafluorohexyloxy, 2,2,3,3,4,4,5,5,6,6-decafluorohexyloxy, 4,4,4-trifluoro-3,3-bis(trifluoromethyl)butyloxy, or perfluorohexyloxy group.
(11) In the present invention, unless otherwise specified, C.sub.3-C.sub.6 cycloalkyl group refers to a cycloalkyl group having 3 to 6 carbon atoms, and examples of the C.sub.3-C.sub.6 cycloalkyl group include a cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl group.
(12) In the present invention, unless otherwise specified, C.sub.3-C.sub.6 halocycloalkyl group refers to a cycloalkyl group having 3 to 6 carbon atoms, substituted by the same or different 1 to 11 halogen atoms, and examples of the C.sub.3-C.sub.6 halocycloalkyl group include a 1-fluorocyclopropyl, 2-fluorocyclopropyl, 2,2-difluorocyclopropyl, 2,2,3,3-tetrafluorocyclopropyl, 1-chlorocyclopropyl, 2-chlorocyclopropyl, 2,2-dichlorocyclopropyl, 2,2,3,3-tetrachlorocyclopropyl, 2,2-dibromocyclopropyl, 2,2-diiodocyclopropyl, 1-fluorocyclobutyl, 2-fluorocyclobutyl, 3-fluorocyclobutyl, 3,3-difluorocyclobutyl, heptafluorocyclobutyl, 2-chlorocyclobutyl, 3-chlorocyclobutyl, 3,3-dichlorocyclobutyl, 3,3-dibromocyclobutyl, 3,3-diiodocyclobutyl, 1-fluorocyclopentyl, 2-fluorocyclopentyl, 3-fluorocyclopentyl, 2,2-difluorocyclopentyl, 3,3-difluorocyclopentyl, nonafluorocyclopentyl, 2,2-dichlorocyclopentyl, 3,3-dichlorocyclopentyl, 2,2-dibromocyclopentyl, 3,3-dibromocyclopentyl, 2,2-diiodocyclopentyl, 3,3-diiodocyclopentyl, 1-fluorocyclohexyl, 2-fluorocyclohexyl, 3-fluorocyclohexyl, 4-fluorocyclohexyl, 2,2-difluorocyclohexyl, 3,3-difluorocyclohexyl, 4,4-difluorocyclohexyl, 1-chlorocyclohexyl, 2-chlorocyclohexyl, 3-chlorocyclohexyl, 4-chlorocyclohexyl, 2,2-dichlorocyclohexyl, 3,3-dichlorocyclohexyl, 4,4-dichlorocyclohexyl, 3,3-dibromocyclohexyl, 4,4-dibromocyclohexyl, 3,3-diiodocyclohexyl, or 4,4-diiodocyclohexyl group.
(13) In the present invention, unless otherwise specified, C.sub.3-C.sub.6 cycloalkyl C.sub.1-C.sub.6 alkyl group refers to a (C.sub.3-C.sub.6 cycloalkyl)-(C.sub.1-C.sub.6 alkyl)- group in which the cycloalkyl moiety and the alkyl moiety are as defined above, and examples of the C.sub.3-C.sub.6 cycloalkyl C.sub.1-C.sub.6 alkyl group include a cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, 2-cyclopropylethyl, 2-cyclobutylethyl, or 2-cyclopentylethyl group.
(14) In the present invention, unless otherwise specified, C.sub.3-C.sub.6 halocycloalkyl C.sub.1-C.sub.6 alkyl group refers to a (C.sub.3-C.sub.6 halocycloalkyl)-(C.sub.1-C.sub.6 alkyl)- group in which the halocycloalkyl moiety and the alkyl moiety are as defined above, and examples of the C.sub.3-C.sub.6 halocycloalkyl C.sub.1-C.sub.6 alkyl group include a (1-fluorocyclopropyl)methyl, (2-fluorocyclopropyl)methyl, (2,2-difluorocyclopropyl)methyl, (1-chlorocyclopropyl)methyl, (2-chlorocyclopropyl)methyl, or (2,2-dichlorocyclopropyl)methyl group.
(15) In the present invention, C.sub.1-C.sub.6 alkoxy C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkoxy)-(C.sub.1-C.sub.6 alkyl)- group in which the alkoxy moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkoxy C.sub.1-C.sub.6 alkyl group include a methoxymethyl, 1-methoxyethyl, 2-methoxyethyl, 2-ethoxyethyl, 3-ethoxypropyl, 3-methoxypropyl, 1-methyl-3-methoxybutyl, or 3-butoxybutyl group.
(16) In the present invention, C.sub.1-C.sub.6 alkoxy C.sub.1-C.sub.6 haloalkyl group refers to a (C.sub.1-C.sub.6 alkoxy)-(C.sub.1-C.sub.6 haloalkyl)- group in which the alkoxy moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkoxy C.sub.1-C.sub.6 haloalkyl group include a 2-methoxy-1,1,2-trifluoroethyl or 2-ethoxy-1,1,2-trifluoroethyl group.
(17) In the present invention, C.sub.1-C.sub.6 haloalkoxy C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 haloalkoxy)-(C.sub.1-C.sub.6 alkyl)- group in which the haloalkoxy moiety is as defined above, and examples of the C.sub.1-C.sub.6 haloalkoxy C.sub.1-C.sub.6 alkyl group include a 2-(difluoromethoxy)ethyl, 2-(trifluoromethoxy)ethyl, 2-(2,2-difluoroethoxy)ethyl, or 2-(2,2,2-trifluoroethoxy)ethyl group.
(18) In the present invention, C.sub.1-C.sub.6 haloalkoxy C.sub.1-C.sub.6 haloalkyl group refers to a (C.sub.1-C.sub.6 haloalkoxy)-(C.sub.1-C.sub.6 haloalkyl)- group in which the haloalkoxy moiety is as defined above, and examples of the C.sub.1-C.sub.6 haloalkoxy C.sub.1-C.sub.6 haloalkyl group include a 1,1,2-trifluoro-2-(trifluoromethoxy)ethyl, 1,1,2-trifluoro-2-(pentafluoroethoxy)ethyl, or 1,1,2-trifluoro-2-(heptafluoropropoxy)ethyl group.
(19) In the present invention, unless otherwise specified, C.sub.2-C.sub.6 alkenyl group refers to a linear or branched alkenyl group having 2 to 6 carbon atoms, and examples of the C.sub.2-C.sub.6 alkenyl group include a vinyl, 1-propenyl, isopropenyl, 2-propenyl, 1-butenyl, 1-methyl-1-propenyl, 2-butenyl, 1-methyl-2-propenyl, 3-butenyl, 2-methyl-1-propenyl, 2-methyl-2-propenyl, 1,3-butadienyl, 1-pentenyl, 1-ethyl-2-propenyl, 2-pentenyl, 1-methyl-1-butenyl, 3-pentenyl, 1-methyl-2-butenyl, 4-pentenyl, 1-methyl-3-butenyl, 3-methyl-1-butenyl, 1,2-dimethyl-2-propenyl, 1,1-dimethyl-2-propenyl, 2-methyl-2-butenyl, 3-methyl-2-butenyl, 1,2-dimethyl-1-propenyl, 2-methyl-3-butenyl, 3-methyl-3-butenyl, 1,3-pentadienyl, 1-vinyl-2-propenyl, 1-hexenyl, 1-propyl-2-propenyl, 2-hexenyl, 1-methyl-1-pentenyl, 1-ethyl-2-butenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl, 1-methyl-4-pentenyl, 1-ethyl-3-butenyl, 1-(isobutyl)vinyl, 1-ethyl-1-methyl-2-propenyl, 1-ethyl-2-methyl-2-propenyl, 1-(isopropyl)-2-prop enyl, 2-methyl-2-pentenyl, 3-methyl-3-pentenyl, 4-methyl-3-pentenyl, 1,3-dimethyl-2-butenyl, 1,1-dimethyl-3-butenyl, 3-methyl-4-pentenyl, 4-methyl-4-pentenyl, 1,2-dimethyl-3-butenyl, 1,3-dimethyl-3-butenyl, 1,1,2-trimethyl-2-propenyl, 1,5-hexadienyl, 1-vinyl-3-butenyl, or 2,4-hexadienyl group.
(20) In the present invention, unless otherwise specified, C.sub.2-C.sub.7 alkynyl group refers to a linear or branched alkynyl group having 2 to 7 carbon atoms, and examples of the C.sub.2-C.sub.7 alkynyl group include an ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 1-methyl-2-propynyl, 2-butynyl, 3-butynyl, 1-pentynyl, 1-ethyl-2-propynyl, 2-pentynyl, 3-pentynyl, 1-methyl-2-butynyl, 4-pentynyl, 1-methyl-3-butynyl, 2-methyl-3-butynyl, 1-hexynyl, 1-(n-propyl)-2-propynyl, 2-hexynyl, 1-ethyl-2-butynyl, 3-hexynyl, 1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 4-methyl-1-pentynyl, 3-methyl-1-pentynyl, 5-hexynyl, 1-ethyl-3-butynyl, 1-ethyl-1-methyl-2-propynyl, 1-(isopropyl)-2-propynyl, 1,1-dimethyl-2-butynyl or 2,2-dimethyl-3-butynyl, 1-heptynyl, 1-(n-butyl)-2-propynyl, 1-(s-butyl)-2-propynyl, 1-isobutyl-2-propynyl, 2-heptynyl, 3-heptynyl, 1-methyl-2-hexynyl, 4-methyl-2-hexynyl, 5-methyl-2-hexynyl, 6-heptynyl, 1,1-diethyl-2-propynyl, 1-methyl-1-propyl-2-propynyl, 1-isopropyl-1-methyl-2-propynyl, 1,1-dimethyl-2-pentynyl, 1,4-dimethyl-2-pentynyl, or 4,4-dimethyl-2-pentynyl group.
(21) In the present invention, unless otherwise specified, C.sub.2-C.sub.6 haloalkynyl group refers to a linear or branched alkynyl group having 2 to 6 carbon atoms, substituted with the same or different 1 to 9 halogen atoms, and examples of the C.sub.2-C.sub.6 haloalkynyl group include a fluoroethynyl, chloroethynyl, bromoethynyl, iodoethynyl, 3-fluoro-2-propynyl, 3-chloro-2-propynyl, 3-bromo-2-propynyl, 3-iodo-2-propynyl, 4-fluoro-3-butynyl, 4-chloro-3-butynyl, 4-bromo-3-butynyl, 4-iodo-3-butynyl, 4,4-difluoro-2-butynyl, 4,4-dichloro-2-butynyl, 4,4,4-trifluoro-2-butynyl, 4,4,4-trichloro-2-butynyl, 3-fluoro-1-methyl-2-propynyl, 3-chloro-1-methyl-2-propynyl, 5-fluoro-4-pentynyl, 5-chloro-4-pentynyl, 5,5,5-trifluoro-3-pentynyl, 5,5,5-trichloro-3-pentynyl, 4-fluoro-2-methyl-3-butynyl, 4-chloro-2-methyl-3-butynyl, 6-fluoro-5-hexynyl, 6-chloro-5-hexynyl, 6,6,6-trifluoro-4-hexynyl, 6,6,6-trichloro-4-hexynyl, 5-fluoro-3-methyl-4-pentynyl, or 5-chloro-3-methyl-4-pentynyl group.
(22) In the present invention, unless otherwise specified, C.sub.2-C.sub.6 haloalkenyl group refers to a linear or branched alkenyl group having 2 to 6 carbon atoms, substituted with the same or different 1 to 11 halogen atoms, and examples of the C.sub.2-C.sub.6 haloalkenyl group include a 1-fluorovinyl, 2-fluorovinyl, 1,2-difluorovinyl, 2,2-difluorovinyl, trifluorovinyl, 1-chlorovinyl, 2-chlorovinyl, 1,2-dichlorovinyl, 2,2-dichlorovinyl, trichlorovinyl, 1,2-dibromovinyl, 2,2-dibromovinyl, tribromovinyl, 1,2-diiodovinyl, 2,2-diiodovinyl, triodovinyl, 1-fluoro-2-propenyl, 2-fluoro-2-propenyl, 3-fluoro-2-propenyl, 2,3-difluoro-2-propenyl, 3,3-difluoro-2-propenyl, 3,3-difluoro-1-propenyl, 2,3,3-trifluoro-2-propenyl, 3,3,3-trifluoro-1-propenyl, 2-chloro-3,3,3-trifluoro-1-propenyl, 1,2,3,3,3-pentafluoro-1-propenyl, 1-chloro-2-propenyl, 2-chloro-2-propenyl, 3-chloro-2-propenyl, 2,3-dichloro-2-propenyl, 3,3-dichloro-2-propenyl, 3,3-dichloro-1-propenyl, 2,3,3-trichloro-2-propenyl, 3,3,3-trichloro-1-propenyl, 3-bromo-2-propenyl, 3,3-dibromo-2-propenyl, 3,3-diiodo-2-propenyl, 2,2-difluoro-1-propene-2-yl, 3,3,3-trifluoro-1-propene-2-yl, 3,3,3-trichloro-1-propene-2-yl, 4-fluoro-3-butenyl, 4,4-difluoro-3-butenyl, 4,4-difluoro-3-butene-2-yl, 4,4,4-trifluoro-2-butenyl, 3,4,4-trifluoro-3-butenyl, 2-trifluoromethyl-2-propenyl, 2-trifluoromethyl-3,3-difluoro-2-propenyl, 4,4,4-trifluoro-3-chloro-2-butenyl, 4,4-dichloro-3-butenyl, 4,4,4-trichloro-2-butenyl, 2-trichloromethyl-2-propenyl, 5,5-difluoro-4-pentenyl, 4,5,5-trifluoro-4-pentenyl, 5,5,5-trifluoro-3-pentenyl, 4,4,4-trifluoro-3-methyl-2-butenyl, 4,4,4-trifluoro-3-trifluoromethyl-2-butenyl, 5,5-dichloro-4-pentenyl, 4,4,4-trichloro-3-methyl-2-butenyl, 6,6-difluoro-5-hexenyl, 5,6,6-trifluoro-5-pentenyl, 6,6,6-trifluoro-4-pentenyl, 5,5,5-trifluoro-4-methyl-3-pentenyl, 5,5,5-trifluoro-4-trifluoromethyl-3-pentenyl, 6,6-dichloro-5-hexenyl, or 5,5,5-trichloro-4-methyl-3-pentenyl group.
(23) In the present invention, C.sub.1-C.sub.6 alkylthio group refers to a (C.sub.1-C.sub.6 alkyl)-S group in which the alkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkylthio group include a methylthio, ethylthio, n-propylthio, isopropylthio, n-butylthio, isobutylthio, sec-butylthio, or tert-butylthio group.
(24) In the present invention, C.sub.1-C.sub.6 alkylsulfinyl group refers to a (C.sub.1-C.sub.6 alkyl)-S(?O) group in which the alkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkylsulfinyl group include a methylsulfinyl, ethylsulfinyl, n-propylsulfinyl, isopropylsulfinyl, n-butylsulfinyl, isobutylsulfinyl, sec-butylsulfinyl, or tert-butylsulfinyl group.
(25) In the present invention, C.sub.1-C.sub.6 alkylsulfonyl group refers to a (C.sub.1-C.sub.6 alkyl)-S(?O).sub.2 group in which the alkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkylsulfonyl group include a methylsulfonyl, ethylsulfonyl, n-propylsulfonyl, isopropylsulfonyl, n-butylsulfonyl, isobutylsulfonyl, sec-butylsulfonyl, or tert-butylsulfonyl group.
(26) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 haloalkylthio group refers to a (C.sub.1-C.sub.6 haloalkyl)-S group in which the haloalkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 haloalkylthio group include a fluoromethylthio, difluoromethylthio, trifluoromethylthio, trichloromethylthio, 2,2,2-trifluoroethylthio, pentafluoroethylthio, 2,2,2-trichloroethylthio, 3,3,3-trifluoropropylthio, 1,1,2,3,3,3-hexafluoropropyl, heptafluoropropylthio, 1,1,1,3,3,3-hexafluoropropane-2-ylthio, heptafluoropropane-2-ylthio, or 4,4,4-trifluorobutylthio group.
(27) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 haloalkylsulfinyl group refers to a (C.sub.1-C.sub.6 haloalkyl)-S(?O) group in which the haloalkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 haloalkylsulfinyl group include a difluoromethylsulfinyl, trifluoromethylsulfinyl, trichloromethylsulfinyl, 2,2,2-trifluoroethylsulfinyl, 2,2,2-trichloroethylsulfinyl, pentafluoroethylsulfinyl, 3,3,3-trifluoropropylsulfinyl, heptafluoropropylsulfinyl, or heptafluoro-2-propylsulfinyl group.
(28) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 haloalkylsulfonyl group refers to a (C.sub.1-C.sub.6 haloalkyl)-S(?O).sub.2 group in which the haloalkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 haloalkylsulfonyl group include a difluoromethylsulfonyl, trifluoromethylsulfonyl, trichloromethylsulfonyl, 2,2,2-trifluoroethylsulfonyl, pentafluoroethylsulfonyl, 3,3,3-trifluoropropylsulfonyl, heptafluoropropylsulfonyl, or heptafluoro-2-propylsulfonyl group.
(29) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 alkylthio C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkyl)-S(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkylthio C.sub.1-C.sub.6 alkyl group include a methylthiomethyl, ethylthiomethyl, n-propylthiomethyl, isopropylthiomethyl, 1-(methylthio)ethyl, 2-(methylthio)ethyl, 2-(ethylthio)ethyl, 1-(n-propylthio)ethyl, 2-(n-propylthio)ethyl, 1-(methylthio)propyl, 2-(methylthio)propyl, 3-(methylthio)propyl, 1-(ethylthio)propyl, 2-(ethylthio)propyl, 3-(ethylthio)propyl, 1-(n-propylthio)propyl, 2-(n-propylthio)propyl, 3-(n-propylthio)propyl, 2-(n-butylthio)ethyl, 2-(isobutylthio)ethyl, sec-butylthioethyl, 2-(tert-butylthio)ethyl, pentylthiomethyl, or hexylthiomethyl group.
(30) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 alkylsulfinyl C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkyl)-S(?O)(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkylsulfinyl C.sub.1-C.sub.6 alkyl group include a methylsulfinylmethyl, ethylsulfinylmethyl, n-propylsulfinylmethyl, isopropylsulfinylmethyl, 1-(methylsulfinyl)ethyl, 2-(methylsulfinyl)ethyl, 2-(ethylsulfinyl)ethyl, 1-(n-propylsulfinyl)ethyl, 2-(n-propylsulfinyl)ethyl, 1-(methylsulfinyl)propyl, 2-(methylsulfinyl)propyl, 3-(methylsulfinyl)propyl, 1-(ethylsulfinyl)propyl, 2-(ethylsulfinyl)propyl, 3-(ethylsulfinyl)propyl, 1-(n-propylsulfinyl)propyl, 2-(n-propylsulfinyl)propyl, 3-(n-propylsulfinyl)propyl, 2-(n-butylsulfinyl)ethyl, 2-(isobutylsulfinyl)ethyl, sec-butylsulfinylethyl, 2-(tert-butylsulfinyl)ethyl, pentylsulfinylmethyl, or hexylsulfinylmethyl group.
(31) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 alkylsulfonyl C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkyl)-S(?O).sub.2(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkylsulfonyl C.sub.1-C.sub.6 alkyl group include a methylsulfonylmethyl, ethylsulfonylmethyl, n-propylsulfonylmethyl, isopropylsulfonylmethyl, 1-(methylsulfonyl)ethyl, 2-(methylsulfonyl)ethyl, 2-(ethylsulfonyl)ethyl, 1-(n-propylsulfonyl)ethyl, 2-(n-propylsulfonyl)ethyl, 1-(methylsulfonyl)propyl, 2-(methylsulfonyl)propyl, 3-(methylsulfonyl)propyl, 1-(ethylsulfonyl)propyl, 2-(ethylsulfonyl)propyl, 3-(ethylsulfonyl)propyl, 1-(n-propylsulfonyl)propyl, 2-(n-propylsulfonyl)propyl, 3-(n-propylsulfonyl)propyl, 2-(n-butylsulfonyl)ethyl, 2-(isobutylsulfonyl)ethyl, sec-butylsulfonylethyl, 2-(tert-butylsulfonyl)ethyl, pentylsulfonylmethyl, or hexylsulfonylmethyl group.
(32) In the present invention, C.sub.1-C.sub.6 haloalkylthio C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 haloalkyl)-S(C.sub.1-C.sub.6 alkyl)- group in which the haloalkylthio moiety and the alkyl moiety are as defined above, and examples of the C.sub.1-C.sub.6 haloalkylthio C.sub.1-C.sub.6 alkyl group include a 2-(difluoromethylthio)ethyl, 2-(trifluoromethylthio)ethyl, 2-(2,2-difluoroethylthio)ethyl, 2-(2,2,2-trifluoroethylthio)ethyl, 2-(3,3-difluoropropylthio)ethyl, 2-(3,3,3-trifluoroethylthio)ethyl, 3-(difluoromethylthio)propyl, 3-(trifluoromethylthio)propyl, 3-(2,2-difluoroethylthio)propyl, 3-(2,2,2-trifluoroethylthio)propyl, 3-(3,3-difluoropropylthio)propyl, or 3-(3,3,3-trifluoropropylthio)propyl group.
(33) In the present invention, C.sub.1-C.sub.6 haloalkylsulfinyl C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 haloalkyl)-S(?O)(C.sub.1-C.sub.6 alkyl)- group in which the haloalkylsulfinyl moiety and the alkyl moiety are as defined above, and examples of the C.sub.1-C.sub.6 haloalkylsulfinyl C.sub.1-C.sub.6 alkyl group include a 2-(difluoromethylsulfinyl)ethyl, 2-(trifluoromethylsulfinyl)ethyl, 2-(2,2-difluoroethylsulfinyl)ethyl, 2-(2,2,2-trifluoroethylsulfinyl)ethyl, 2-(3,3-difluoropropylsulfinyl)ethyl, 2-(3,3,3-trifluoroethylsulfinyl)ethyl, 3-(difluoromethylsulfinyl)propyl, 3-(trifluoromethylsulfinyl)propyl, 3-(2,2-difluoroethylsulfinyl)propyl, 3-(2,2,2-trifluoroethylsulfinyl)propyl, 3-(3,3-difluoropropylsulfinyl)propyl, or 3-(3,3,3-trifluoropropylsulfinyl)propyl group.
(34) In the present invention, C.sub.1-C.sub.6 haloalkylsulfonyl C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 haloalkyl)-S(?O).sub.2(C.sub.1-C.sub.6 alkyl)- group in which the haloalkylsulfonyl moiety and the alkyl moiety are as defined above, and examples of the C.sub.1-C.sub.6 haloalkylsulfonyl C.sub.1-C.sub.6 alkyl group include a 2-(difluoromethylsulfonyl)ethyl, 2-(trifluoromethylsulfonyl)ethyl, 2-(2,2-difluoroethylsulfonyl)ethyl, 2-(2,2,2-trifluoroethylsulfonyl)ethyl, 2-(3,3-difluoropropylsulfonyl)ethyl, 2-(3,3,3-trifluoroethylsulfonyl)ethyl, 3-(difluoromethylsulfonyl)propyl, 3-(trifluoromethylsulfonyl)propyl, 3-(2,2-difluoroethylsulfonyl)propyl, 3-(2,2,2-trifluoroethylsulfonyl)propyl, 3-(3,3-difluoropropylsulfonyl)propyl, or 3-(3,3,3-trifluoropropylsulfonyl)propyl group.
(35) In the present invention, mono(C.sub.1-C.sub.6 alkyl)amino group refers to a (C.sub.1-C.sub.6 alkyl)-NH group in which the alkyl moiety is as defined above, and examples of the mono(C.sub.1-C.sub.6 alkyl)amino group include a methylamino, ethylamino, n-propylamino, or isopropyl amino group.
(36) In the present invention, di(C.sub.1-C.sub.6 alkyl)amino group refers to a (C.sub.1-C.sub.6 alkyl).sub.2-N group in which the alkyl moiety is as defined above, and the two alkyl groups may be different from each other, and examples of the di(C.sub.1-C.sub.6 alkyl)amino group include a dimethylamino, diethylamino, or N-ethyl-N-methylamino group.
(37) In the present invention, mono(C.sub.1-C.sub.6 alkyl)aminocarbonyl group refers to a (C.sub.1-C.sub.6 alkyl)-NHC(?O) group in which the alkyl moiety is as defined above, and examples of the mono(C.sub.1-C.sub.6 alkyl)aminocarbonyl group include a methylaminocarbonyl, ethylaminocarbonyl, propylaminocarbonyl, or isopropylaminocarbonyl group.
(38) In the present invention, di(C.sub.1-C.sub.6 alkyl)aminocarbonyl group refers to a (C.sub.1-C.sub.6 alkyl).sub.2-NC(?O) group in which the alkyl moiety is as defined above, and the two alkyl groups may be different from each other, and examples of the di(C.sub.1-C.sub.6 alkyl)aminocarbonyl group include a dimethylaminocarbonyl, diethylaminocarbonyl, di(n-propyl)aminocarbonyl, or N-ethyl-N-methylaminocarbonyl group.
(39) In the present invention, C.sub.1-C.sub.6 alkylcarbonyl C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkyl)-C(?O)(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkylcarbonyl C.sub.1-C.sub.6 alkyl group include an acetonyl, propionylmethyl, 2-methylpropionylmethyl, pivaloylmethyl, 2-acetylethyl, 2-propionylethyl, 2(2-methylpropionyl)ethyl, 2-pivaloylethyl, 3-acetylpropyl, 3-propionylpropyl, 3(2-methylpropionyl)propyl, or 3-pivaloylpropyl group.
(40) In the present invention, C.sub.1-C.sub.6 haloalkylcarbonyl C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 haloalkyl)-C(?O)(C.sub.1-C.sub.6 alkyl)- group in which the haloalkyl moiety and the alkyl moiety are as defined above, and examples of the C.sub.1-C.sub.6 haloalkylcarbonyl C.sub.1-C.sub.6 alkyl group include a 3,3,3-trifluoro-2-oxopropyl group.
(41) In the present invention, C.sub.1-C.sub.6 alkoxycarbonyl C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkoxy)-C(?O)(C.sub.1-C.sub.6 alkyl)- group in which the alkoxy moiety and the alkyl moiety are as defined above, and examples of the C.sub.1-C.sub.6 alkoxycarbonyl C.sub.1-C.sub.6 alkyl group include a methoxycarbonylmethyl, ethoxycarbonylmethyl, n-propoxycarbonylmethyl, isopropoxycarbonylmethyl, tert-butoxycarbonylmethyl, 2-(methoxycarbonyl)ethyl, 2-(ethoxycarbonyl)ethyl, or 2-(tert-butoxycarbonyl)ethyl group.
(42) In the present invention, unless otherwise specified, hydroxy C.sub.1-C.sub.6 alkyl group refers to a (hydroxy)-(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the hydroxy C.sub.1-C.sub.6 alkyl group include a 2-hydroxyethyl, 2-hydroxypropyl, 3-hydroxypropyl, or 4-hydroxybutyl group.
(43) In the present invention, unless otherwise specified, cyano C.sub.1-C.sub.6 alkyl group refers to a (cyano)-(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the cyano C.sub.1-C.sub.6 alkyl group include a cyanomethyl, 1-cyanoethyl, 2-cyanoethyl, 3-cyanopropyl, 2-cyanopropane-2-yl, 1-cyanobutyl, 4-cyanobutyl, 5-cyanopentyl, or 6-cyanohexyl group.
(44) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 alkylsulfonyloxy group refers to a (C.sub.1-C.sub.6 alkyl)-S(?O).sub.2O group in which the alkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkylsulfonyloxy group include a methylsulfonyloxy, ethylsulfonyloxy, or isopropylsulfonyloxy group.
(45) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 haloalkylsulfonyloxy group refers to a (C.sub.1-C.sub.6haloalkyl)-S(?O).sub.2O group in which the haloalkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 haloalkylsulfonyloxy group include a trifluoromethylsulfonyloxy, perfluoroethylsulfonyloxy, perfluoropropylsulfonyloxy, or perfluorobutylsulfonyloxy group.
(46) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 alkylcarbonyl group refers to a (C.sub.1-C.sub.6 alkyl)-C(?O) group in which the alkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkylcarbonyl group include an acetyl or propionyl group.
(47) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 haloalkylcarbonyl group refers to a (C.sub.1-C.sub.6 haloalkyl)-C(?O) group in which the haloalkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 haloalkylcarbonyl group include a 2,2,2-trifluoroacetyl group or 2,2,2-trichloroacetyl group.
(48) In the present invention, C.sub.1-C.sub.6 alkoxycarbonyl group refers to a (C.sub.1-C.sub.6 alkoxy)-C(?O) group in which the alkoxy moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkoxycarbonyl group include a methoxycarbonyl, ethoxycarbonyl, n-propoxycarbonyl, isopropoxycarbonyl, or tert-butoxycarbonyl group.
(49) In the present invention, unless otherwise specified, C.sub.3-C.sub.6 cycloalkoxy group refers to a (C.sub.3-C.sub.6 cycloalkyl)-O group in which the cycloalkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 cycloalkoxy group include a cyclopropoxy, cyclobutoxy, cyclopentyloxy, or cyclohexyloxy group.
(50) In the present invention, unless otherwise specified, C.sub.3-C.sub.6 halocycloalkoxy group refers to a (C.sub.3-C.sub.6 halocycloalkyl)-O group in which the halocycloalkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 halocycloalkoxy group include a 1-fluorocyclopropoxy, 2-fluorocyclopropoxy, 2,2-difluorocyclopropoxy, 2,2,3,3-tetrafluorocyclopropoxy, 1-chlorocyclopropoxy, 2-chlorocyclopropoxy, 2,2-dichlorocyclopropoxy, 2,2,3,3-tetrachlorocyclopropoxy, 1-fluorocyclobutoxy, 2-fluorocyclobutoxy, 3-fluorocyclobutoxy, 3,3-difluorocyclobutoxy, 2-chlorocyclobutoxy, 3-chlorocyclobutoxy, 3,3-dichlorocyclobutoxy, 2-fluorocyclopentyloxy, 3-fluorocyclopentyloxy, 2,2-difluorocyclopentyloxy, 3,3-difluorocyclopentyloxy, 2,2-dichlorocyclopentyloxy, 3,3-dichlorocyclopentyloxy, 1-fluorocyclohexyloxy, 2-fluorocyclohexyloxy, 3-fluorocyclohexyloxy, 4-fluorocyclohexyloxy, 2,2-difluorocyclohexyloxy, 3,3-difluorocyclohexyloxy, 4,4-difluorocyclohexyloxy, 1-chlorocyclohexyloxy, 2-chlorocyclohexyloxy, 3-chlorocyclohexyloxy, 4-chlorocyclohexyloxy, 2,2-dichlorocyclohexyloxy, 3,3-dichlorocyclohexyloxy, or 4,4-dichlorocyclohexyloxy group.
(51) In the present invention, unless otherwise specified, C.sub.3-C.sub.6 cycloalkyl C.sub.1-C.sub.6 alkoxy group refers to a (C.sub.3-C.sub.6 cycloalkyl)-(C.sub.1-C.sub.6 alkyl)-O group in which the cycloalkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 cycloalkyl C.sub.1-C.sub.6 alkoxy group include a cyclopropylmethoxy, cyclobutylmethoxy, cyclopentylmethoxy, 2-cyclopropylethoxy, 2-cyclobutylethoxy, or 2-cyclopentylethoxy group.
(52) In the present invention, unless otherwise specified, C.sub.3-C.sub.6 halocycloalkyl C.sub.1-C.sub.6 alkoxy group refers to a (C.sub.3-C.sub.6 halocycloalkyl)-(C.sub.1-C.sub.6 alkyl)-O group in which the halocycloalkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 halocycloalkyl C.sub.1-C.sub.6 alkoxy group include a (1-fluorocyclopropyl)methoxy, (2-fluorocyclopropyl)methoxy, (2,2-difluorocyclopropyl)methoxy, (2-chlorocyclopropyl)methoxy, or (2,2-dichlorocyclopropyl)methoxy group.
(53) In the present invention, unless otherwise specified, C.sub.3-C.sub.6 cycloalkyl C.sub.1-C.sub.6 alkylthio group refers to a (C.sub.3-C.sub.6 cycloalkyl)-(C.sub.1-C.sub.6 alkyl)-S group in which the cycloalkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 cycloalkyl C.sub.1-C.sub.6 alkylthio group include a (cyclopropylmethyl)thio, (cyclobutylmethyl)thio, (cyclopentylmethyl)thio, (2-cyclopropylethyl)thio, (2-cyclobutylethyl)thio, or (2-cyclopentylethyl)thio group.
(54) In the present invention, unless otherwise specified, C.sub.3-C.sub.6 cycloalkyl C.sub.1-C.sub.6 alkylsulfinyl group refers to a (C.sub.3-C.sub.6 cycloalkyl)-(C.sub.1-C.sub.6 alkyl)-S(?O) group in which the cycloalkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 cycloalkyl C.sub.1-C.sub.6 alkylsulfinyl group include a (cyclopropylmethyl)sulfinyl, (cyclobutylmethyl)sulfinyl, (cyclopentylmethyl)sulfinyl, (2-cyclopropylethyl)sulfinyl, (2-cyclobutylethyl)sulfinyl, or (2-cyclopentylethyl)sulfinyl group.
(55) In the present invention, unless otherwise specified, C.sub.3-C.sub.6 cycloalkyl C.sub.1-C.sub.6 alkylsulfonyl group refers to a (C.sub.3-C.sub.6 cycloalkyl)-(C.sub.1-C.sub.6 alkyl)-S(?O).sub.2 group in which the cycloalkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 cycloalkyl C.sub.1-C.sub.6 alkylsulfonyl group include a (cyclopropylmethyl)sulfonyl, (cyclobutylmethyl)sulfonyl, (cyclopentylmethyl)sulfonyl, (2-cyclopropylethyl)sulfonyl, (2-cyclobutylethyl)sulfonyl, or (2-cyclopentylethyl)sulfonyl group.
(56) In the present invention, unless otherwise specified, C.sub.3-C.sub.6 halocycloalkyl C.sub.1-C.sub.6 alkylthio group refers to a (C.sub.3-C.sub.6 halocycloalkyl)-(C.sub.1-C.sub.6 alkyl)-S group in which the halocycloalkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 halocycloalkyl C.sub.1-C.sub.6 alkylthio group include a (1-fluorocyclopropyl)methylthio, (2-fluorocyclopropyl)methylthio, (2,2-difluorocyclopropyl)methylthio, (2-chlorocyclopropyl)methylthio, or (2,2-dichlorocyclopropyl)methylthio group.
(57) In the present invention, unless otherwise specified, C.sub.3-C.sub.6 halocycloalkyl C.sub.1-C.sub.6 alkylsulfinyl group refers to a (C.sub.3-C.sub.6 halocycloalkyl)-(C.sub.1-C.sub.6 alkyl)-S(?O) group in which the halocycloalkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 halocycloalkyl C.sub.1-C.sub.6 alkylsulfinyl group include a (1-fluorocyclopropyl)methylsulfinyl, (2-fluorocyclopropyl)methylsulfinyl, (2,2-difluorocyclopropyl)methylsulfinyl, (2-chlorocyclopropyl)methylsulfinyl, or (2,2-dichlorocyclopropyl)methylsulfinyl group.
(58) In the present invention, unless otherwise specified, C.sub.3-C.sub.6 halocycloalkyl C.sub.1-C.sub.6 alkylsulfonyl group refers to a (C.sub.3-C.sub.6 halocycloalkyl)-(C.sub.1-C.sub.6 alkyl)-S(?O).sub.2 group in which the cycloalkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 halocycloalkyl C.sub.1-C.sub.6 alkylsulfonyl group include a (1-fluorocyclopropyl)methylsulfonyl, (2-fluorocyclopropyl)methylsulfonyl, (2,2-difluorocyclopropyl)methylsulfonyl, (2-chlorocyclopropyl)methylsulfonyl, or (2,2-dichlorocyclopropyl)methylsulfonyl group.
(59) In the present invention, unless otherwise specified, mono(oxirane-2-yl) C.sub.1-C.sub.3 alkyl group refers to an (oxirane-2-yl)-(C.sub.1-C.sub.3 alkyl)- group in which the alkyl moiety is as defined above, and examples of the mono(oxirane-2-yl) C.sub.1-C.sub.3 alkyl group include an oxirane-2-ylmethyl, 2-(oxirane-2-yl)ethyl, or 3-(oxirane-2-yl)propyl group.
(60) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 alkylcarbonyloxy group refers to a (C.sub.1-C.sub.6 alkyl)-C(?O)O group in which the alkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkylcarbonyloxy group include an acetoxy or propionyloxy group.
(61) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 haloalkylcarbonyloxy group refers to a (C.sub.1-C.sub.6 haloalkyl)-C(?O)O group in which the haloalkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 haloalkylcarbonyloxy group include a 2,2,2-trifluoroacetoxy or 2,2,2-trichloroacetoxy group.
(62) In the present invention, unless otherwise specified, mono(C.sub.1-C.sub.6 alkyl)aminocarbonyloxy group refers to a (C.sub.1-C.sub.6 alkyl)-NHC(?O)O group in which the alkyl moiety is as defined above, and examples of the mono(C.sub.1-C.sub.6 alkyl)aminocarbonyloxy group include a (methylcarbamoyl)oxy or (ethylcarbamoyl)oxy group.
(63) In the present invention, unless otherwise specified, di(C.sub.1-C.sub.6 alkyl)aminocarbonyloxy group refers to a (C.sub.1-C.sub.6 alkyl).sub.2-NC(?O)O group in which the alkyl moiety is as defined above, and examples of the di(C.sub.1-C.sub.6 alkyl)aminocarbonyloxy group include a (dimethylcarbamoyl)oxy or (diethylcarbamoyl)oxy group.
(64) In the present invention, unless otherwise specified, aminocarbonyloxy C.sub.1-C.sub.6 alkyl group refers to an (amino)-C(?O)O(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the aminocarbonyloxy C.sub.1-C.sub.6 alkyl group include a carbamoyloxymethyl or carbamoyloxyethyl group.
(65) In the present invention, unless otherwise specified, mono(C.sub.1-C.sub.6 alkyl)aminocarbonyloxy C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkyl)-NHC(?O)O(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the mono(C.sub.1-C.sub.6 alkyl)aminocarbonyloxy C.sub.1-C.sub.6 alkyl group include a methylcarbamoyloxymethyl or ethylcarbamoyloxymethyl group.
(66) In the present invention, unless otherwise specified, di(C.sub.1-C.sub.6 alkyl)aminocarbonyloxy C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkyl).sub.2-NC(?O)O(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the di(C.sub.1-C.sub.6 alkyl)aminocarbonyloxy C.sub.1-C.sub.6 alkyl group include a dimethylcarbamoyloxymethyl or diethylcarbamoyloxymethyl group.
(67) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 alkoxycarbonyloxy group refers to a (C.sub.1-C.sub.6 alkoxy)-C(?O)O group in which the alkoxy moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkoxycarbonyloxy group include a methoxycarbonyloxy or ethoxycarbonyloxy group.
(68) In the present invention, C.sub.1-C.sub.6 alkoxycarbonyloxy C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkoxy)-C(?O)O(C.sub.1-C.sub.6 alkyl)- group in which the alkoxy moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkoxycarbonyloxy C.sub.1-C.sub.6 alkyl group include a methoxycarbonyloxymethyl or ethoxycarbonyloxymethyl group.
(69) In the present invention, C.sub.3-C.sub.6 cycloalkyl C.sub.2-C.sub.6 alkynyl group refers to a (C.sub.3-C.sub.6 cycloalkyl)-(C.sub.2-C.sub.6 alkynyl)- group in which the cycloalkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 cycloalkyl C.sub.2-C.sub.6 alkynyl group include a cyclopropylethynyl or cyclobutylethynyl group.
(70) In the present invention, C.sub.3-C.sub.6 cycloalkylthio group refers to a (C.sub.3-C.sub.6 cycloalkyl)-S group in which the cycloalkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 cycloalkylthio group include a cyclopropylthio, cyclobutylthio, or cyclopentylthio group.
(71) In the present invention, C.sub.3-C.sub.6 cycloalkylsulfinyl group refers to a (C.sub.3-C.sub.6 cycloalkyl)-S(?O) group in which the cycloalkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 cycloalkylsulfinyl group include a cyclopropylsulfinyl, cyclobutylsulfinyl, or cyclopentylsulfinyl group.
(72) In the present invention, C.sub.3-C.sub.6 cycloalkylsulfonyl group refers to a (C.sub.3-C.sub.6 cycloalkyl)-S(?O).sub.2 group in which the cycloalkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 cycloalkylsulfonyl group include a cyclopropylsulfonyl, cyclobutylsulfonyl, or cyclopentylsulfonyl group.
(73) In the present invention, C.sub.1-C.sub.6 alkylcarbonyloxy C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkyl)-C(?O)O(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkylcarbonyloxy C.sub.1-C.sub.6 alkyl group include an acetoxymethyl, 2-acetoxyethyl, or propionylmethyl group.
(74) In the present invention, di(C.sub.1-C.sub.6 alkyl)sulfamoyloxy group refers to a (C.sub.1-C.sub.6 alkyl).sub.2-NS(?O).sub.2O group in which the alkyl moiety is as defined above, and examples of the di(C.sub.1-C.sub.6 alkyl)sulfamoyloxy group include a dimethylsulfamoyloxy or diethylsulfamoyloxy group.
(75) In the present invention, unless otherwise specified, cyano C.sub.3-C.sub.6 cycloalkyl group refers to a (cyano)-(C.sub.3-C.sub.6 cycloalkyl) group in which the cycloalkyl moiety is as defined above, and examples of the cyano C.sub.3-C.sub.6 cycloalkyl group include a 1-cyanocyclopropyl, 2-cyanocyclopropyl, 1-cyanocyclobutyl, 3-cyanocyclobutyl, or 1-cyanocyclopentyl group.
(76) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 alkoxy C.sub.1-C.sub.6 alkylcarbonyl group refers to a (C.sub.1-C.sub.6 alkyl)-O(C.sub.1-C.sub.6 alkyl)-C(?O) group in which the alkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkoxy C.sub.1-C.sub.6 alkylcarbonyl group include a methoxyacetyl, ethoxyacetyl, propoxyacetyl, isopropoxyacetyl, butoxyacetyl, 2-methoxypropionyl, 3-methoxypropionyl, 2-ethoxypropionyl, 3-ethoxypropionyl, 2-methoxybutanoyl, 4-methoxybutanoyl, 2-methoxypentanoyl, or 5-methoxypentanoyl group.
(77) In the present invention, unless otherwise specified, C.sub.3-C.sub.6 cycloalkylcarbonyl group refers to a (C.sub.3-C.sub.6 cycloalkyl)-C(?O) group in which the cycloalkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 cycloalkylcarbonyl group include a cyclopropanecarbonyl, cyclobutanecarbonyl, cyclopentanecarbonyl, or cyclohexanecarbonyl group.
(78) In the present invention, C.sub.3-C.sub.6 cycloalkyl C.sub.1-C.sub.6 alkylcarbonyl group refers to a (C.sub.3-C.sub.6 cycloalkyl C.sub.1-C.sub.6 alkyl)-C(?O) group in which the cycloalkyl alkyl moiety is as defined above, and examples of the C.sub.3-C.sub.6 cycloalkyl C.sub.1-C.sub.6 alkylcarbonyl group include a 2-cyclopropylacetyl, 2-cyclobutylacetyl, 2-cyclopentylacetyl, 2-cyclohexylacetyl, 2-cyclopropylpropanoyl, or 2-cyclopropylbutanoyl group.
(79) In the present invention, unless otherwise specified, C.sub.7-C.sub.13 aralkylcarbonyl group refers to a (C.sub.7-C.sub.13 aralkyl)-C(?O) group in which the aralkyl moiety is as defined above, and examples of the C.sub.7-C.sub.13 aralkylcarbonyl group include a phenylethanoyl, 1-phenylpropanoyl, or 2-phenylpropanoyl group.
(80) In the present invention, unless otherwise specified, (C.sub.1-C.sub.6 alkyl)thiocarbonyl group refers to a (C.sub.1-C.sub.6 alkyl)-C(?S) group in which the alkyl moiety is as defined above, and examples of the (C.sub.1-C.sub.6 alkyl)thiocarbonyl group include a methylthiocarbonyl, ethylthiocarbonyl, n-propylthiocarbonyl, isopropylthiocarbonyl, n-butylthiocarbonyl, isobutylthiocarbonyl, sec-butylthiocarbonyl, tert-butylthiocarbonyl, or n-pentylthiocarbonyl group.
(81) In the present invention, unless otherwise specified, (C.sub.1-C.sub.6 alkoxy)thiocarbonyl group refers to a (C.sub.1-C.sub.6 alkyl)-OC(?S) group in which the alkyl moiety is as defined above, and examples of the (C.sub.1-C.sub.6 alkoxy)thiocarbonyl group include a methoxythiocarbonyl, ethoxythiocarbonyl, n-propoxythiocarbonyl, isopropoxythiocarbonyl, n-butoxythiocarbonyl, isobutoxythiocarbonyl, sec-butoxythiocarbonyl, tert-butoxythiocarbonyl, n-pentoxythiocarbonyl, 1-methyl butoxythiocarbonyl, 2-methyl butoxythiocarbonyl, 3-methyl butoxythiocarbonyl, 1-ethylpropoxythiocarbonyl, 1,1-dimethylpropoxythiocarbonyl, 1,2-dimethylpropoxythiocarbonyl, or 2,2-dimethylpropoxythiocarbonyl group.
(82) In the present invention, mono(C.sub.1-C.sub.6 alkyl)aminothiocarbonyl group refers to a (C.sub.1-C.sub.6 alkyl)-NHC(?S) group in which the alkyl moiety is as defined above, and examples of the mono(C.sub.1-C.sub.6 alkyl)aminothiocarbonyl group include a methylaminothiocarbonyl, ethylaminothiocarbonyl, n-propylaminothiocarbonyl, isopropylaminothiocarbonyl, n-butylaminothiocarbonyl, isobutylaminothiocarbonyl, sec-butylaminothiocarbonyl, tert-butylaminothiocarbonyl, n-pentylaminothiocarbonyl, 1-methylbutylaminothiocarbonyl, 2-methylbutylaminothiocarbonyl, 3-methylbutylaminothiocarbonyl, 1-ethylpropylaminothiocarbonyl, 1,1-dimethylpropylaminothiocarbonyl, 1,2-dimethylpropylaminothiocarbonyl, 2,2-dimethylpropylaminothiocarbonyl, or n-hexylaminothiocarbonyl group.
(83) In the present invention, di(C.sub.1-C.sub.6 alkyl)aminothiocarbonyl group refers to a (C.sub.1-C.sub.6 alkyl).sub.2-NC(?S) group in which the alkyl moiety is as defined above, and the two alkyl groups may be different from each other, and examples of the di(C.sub.1-C.sub.6 alkyl)aminothiocarbonyl group include a dimethylaminothiocarbonyl, diethylaminothiocarbonyl, di(n-propyl)aminothiocarbonyl, diisopropylaminothiocarbonyl, dibutylaminothiocarbonyl, N-ethyl-N-methylaminothiocarbonyl, N-methyl-N-propylaminothiocarbonyl, N-isopropyl-N-methylaminothiocarbonyl, N-butyl-N-methylaminothiocarbonyl, N-(s-butyl)-N-methylaminothiocarbonyl, N-isobutyl-N-methylaminothiocarbonyl, N-pentyl-N-methylaminothiocarbonyl, N-ethyl-N-propylaminothiocarbonyl, N-ethyl-N-isopropylaminothiocarbonyl, or N-ethyl-N-butylaminothiocarbonyl group.
(84) In the present invention, mono(C.sub.1-C.sub.6 alkyl)aminosulfonyl group refers to a (C.sub.1-C.sub.6 alkyl)-NHS(?O) group in which the alkyl moiety is as defined above, and examples of the mono(C.sub.1-C.sub.6 alkyl)aminosulfonyl group include a methylaminosulfonyl, ethylaminosulfonyl, n-propylaminosulfonyl, isopropylaminosulfonyl, n-butylaminosulfonyl, isobutylaminosulfonyl, sec-butylaminosulfonyl, tert-butylaminosulfonyl, n-pentylaminosulfonyl, 1-methylbutylaminosulfonyl, 2-methylbutylaminosulfonyl, 3-methylbutylaminosulfonyl, 1-ethylpropylaminosulfonyl, 1,1-dimethylpropylaminosulfonyl, 1,2-dimethylpropylaminosulfonyl, 2,2-dimethylpropylaminosulfonyl, or n-hexylaminosulfonyl group.
(85) In the present invention, di(C.sub.1-C.sub.6 alkyl)aminosulfonyl group refers to a (C.sub.1-C.sub.6 alkyl).sub.2-NS(?O).sub.2 group in which the alkyl moiety is as defined above, and the two alkyl groups may be different from each other, and examples of the di(C.sub.1-C.sub.6 alkyl)aminosulfonyl group include a dimethylaminosulfonyl, diethylaminosulfonyl, di(n-propyl)aminosulfonyl, diisopropylaminosulfonyl, dibutylaminosulfonyl, N-ethyl-N-methylaminosulfonyl, N-methyl-N-propylaminosulfonyl, N-isopropyl-N-methylaminosulfonyl, N-butyl-N-methylaminosulfonyl, N-(s-butyl)-N-methylaminosulfonyl, N-isobutyl-N-methylaminosulfonyl, N-pentyl-N-methylaminosulfonyl, N-ethyl-N-propylaminosulfocarbonyl, N-ethyl-N-isopropylaminosulfocarbonyl, or N-ethyl-N-butylaminosulfonyl group.
(86) In the present invention, aminocarbonyl C.sub.1-C.sub.6 alkyl group refers to a H.sub.2NC(?O)(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the aminocarbonyl C.sub.1-C.sub.6 alkyl group include a carbamoylmethyl, 1-carbamoylethyl, or 2-carbamoylethyl group.
(87) In the present invention, mono(C.sub.1-C.sub.6 alkyl)aminocarbonyl C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkyl)-NHC(?O)(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the mono(C.sub.1-C.sub.6 alkyl)aminocarbonyl C.sub.1-C.sub.6 alkyl group include a N-methylcarbamoylmethyl, N-ethylcarbamoylmethyl, or N-(tert-butyl)carbamoylmethyl group.
(88) In the present invention, mono(C.sub.1-C.sub.6 haloalkyl)aminocarbonyl C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 haloalkyl)-NHC(?O)(C.sub.1-C.sub.6 alkyl)- group in which the haloalkyl moiety is as defined above, and examples of the mono(C.sub.1-C.sub.6 haloalkyl)aminocarbonyl C.sub.1-C.sub.6 alkyl group include a N-(2,2-difluoroethyl)carbamoylmethyl, N-(2,2,2-trifluoroethyl)carbamoylmethyl, 1-{N-(2,2-difluoroethyl)carbamoyl}ethyl, 1-{N-(2,2-trifluoroethyl)carbamoyl]}ethyl, 1-{N-(2,2-difluoroethyl)carbamoyl}-1-methylethyl, or 1-{N-(2,2-trifluoroethyl)carbamoyl}-1-methylethyl group.
(89) In the present invention, mono(C.sub.3-C.sub.6 cycloalkyl)aminocarbonyl C.sub.1-C.sub.6 alkyl group refers to a (C.sub.3-C.sub.6 cycloalkyl)-NHC(?O)(C.sub.1-C.sub.6 alkyl)- group in which the cycloalkyl moiety is as defined above, and examples of the mono(C.sub.3-C.sub.6 cycloalkyl)aminocarbonyl C.sub.1-C.sub.6 alkyl group include a N-cyclopropylcarbamoylmethyl, N-cyclobutylcarbamoylmethyl, N-cyclopentylcarbamoylmethyl, or N-cyclohexylcarbamoylmethyl group.
(90) In the present invention, di(C.sub.1-C.sub.6 alkyl)aminocarbonyl C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkyl).sub.2-NC(?O)(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the di(C.sub.1-C.sub.6 alkyl)aminocarbonyl C.sub.1-C.sub.6 alkyl group include a N,N-dimethylcarbamoylmethyl, N,N-diethylcarbamoylmethyl, N,N-dipropylcarbamoylmethyl, N-ethyl-N-methylcarbamoylmethyl, or N-methyl-N-propylcarbamoylmethyl group.
(91) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 alkoxyimino group refers to a (C.sub.1-C.sub.6 alkyl)-ON?C group in which the alkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkoxyimino group include a methoxyimino, ethoxyimino, or isopropoxyimino group.
(92) In the present invention, unless otherwise specified, hydroxyimino C.sub.1-C.sub.6 alkyl group refers to a HON?(C.sub.1-C.sub.6 alkyl) group in which the alkyl moiety is as defined above, and examples of the hydroxyimino C.sub.1-C.sub.6 alkyl group include a 1-(hydroxyimino)ethyl, 2-(hydroxyimino)ethyl, 1-(hydroxyimino)propyl, 2-(hydroxyimino)propyl, or 3-(hydroxyimino)propyl group.
(93) In the present invention, unless otherwise specified, C.sub.1-C.sub.6 alkoxyimino C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkyl)-ON?(C.sub.1-C.sub.6 alkyl) group in which the alkyl moiety is as defined above, and examples of the C.sub.1-C.sub.6 alkoxyimino C.sub.1-C.sub.6 alkyl group include a 1-(methoxyimino)ethyl, 2-(methoxyimino)ethyl, 1-(methoxyimino)propyl, 2-(methoxyimino)propyl, 3-(methoxyimino)propyl, 1-(ethoxyimino)ethyl, 2-(ethoxyimino)ethyl, 1-(ethoxyimino)propyl, 2-(ethoxyimino)propyl, 3-(ethoxyimino)propyl, 1-(isopropoxyimino)ethyl, or 2-(isopropoxyimino)ethyl group.
(94) In the present invention, unless otherwise specified, amino C.sub.1-C.sub.6 alkyl group refers to a H.sub.2N(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the amino C.sub.1-C.sub.6 alkyl group include an aminomethyl, or 2-aminoethyl group.
(95) In the present invention, unless otherwise specified, mono(C.sub.1-C.sub.6 alkyl)amino C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkyl)-NH(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the mono(C.sub.1-C.sub.6 alkyl)amino C.sub.1-C.sub.6 alkyl group include a N-methylaminomethyl, or N-ethylaminomethyl group.
(96) In the present invention, unless otherwise specified, di(C.sub.1-C.sub.6 alkyl)amino C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkyl).sub.2-N(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the di(C.sub.1-C.sub.6 alkyl)amino C.sub.1-C.sub.6 alkyl group include a N,N-dimethylaminomethyl or N,N-diethylaminomethyl group.
(97) In the present invention, unless otherwise specified, tri(C.sub.1-C.sub.6 alkyl)silyloxy C.sub.1-C.sub.6 alkyl group refers to a (C.sub.1-C.sub.6 alkyl).sub.3-SiO(C.sub.1-C.sub.6 alkyl)- group in which the alkyl moiety is as defined above, and examples of the tri(C.sub.1-C.sub.6 alkyl)silyloxy C.sub.1-C.sub.6 alkyl group include a trimethylsilyloxymethyl, trimethylsilyloxyethyl, triethylsilyloxymethyl, triethylsilyloxyethyl, triisopropylsilyloxymethyl, triisopropylsilyloxyethyl, tert-butyldimethylsilyloxymethyl, or tert-butyldimethylsilyloxyethyl group.
(98) In the present invention, the wording agriculturally acceptable salt or salt refers to a salt of a hydroxyl group, a carboxyl group, an amino group or the like when such a group exists in the structure of the present compound represented by general formula [I] or [II], or a nitrogen atom in a pyridine ring, with metal or an organic base, or a salt with a mineral acid or an organic acid, and examples of the metal include alkali metal such as sodium or potassium, and alkali earth metal such as magnesium or calcium, examples of the organic base include triethylamine or diisopropylamine, examples of the mineral acid include phosphoric acid, hydrochloric acid, hydrobromic acid, hydroiodic acid, boric acid, or sulfuric acid, and examples of the organic acid include formic acid, acetic acid, lactic acid, ascorbic acid, succinic acid, fumaric acid, maleic acid, oxalic acid, citric acid, benzoic acid, salicylic acid, tartaric acid, methanesulfonic acid, 4-toluenesulfonic acid, or trifluoromethanesulfonic acid.
(99) Next, representative compound examples of compounds included in the pyrazole derivative of the present invention represented by general formula [I] are shown in Table 1 to Table 194, and representative compound examples of compounds included in the pyrazole derivative of the present invention represented by general formula [II] are shown in Table 195 to Table 314. However, the compounds included in the derivatives of the present invention are not limited to these. The compound numbers in Tables are referred to in the following description.
(100) The compounds included in the pyrazole derivatives of the present invention can have geometrical isomers of E-form and Z-form depending on the kind of the substituent, and the present invention encompasses such E-form, Z-form, or a mixture containing E-form and Z-form in any ratio. The compounds encompassed in the present invention can have optical isomers caused by the existence of one or two or more asymmetric carbon atoms and asymmetric sulfur atoms, and the present invention encompasses any optically active substances, racemic modifications, or diastereomers.
(101) In the present specification, the following signs in tables respectively represent the corresponding groups as shown below. Me: methyl Et: ethyl Pr: n-propyl i-Pr: isopropyl Bu: n-butyl t-Bu: tert-butyl OMe: methoxy O(i-Pr): isopropoxy 2-CF.sub.3: 2-trifluoromethyl 4-Me,2-CF.sub.3: 4-methyl-2-trifluoromethyl 2-CF.sub.3-pyridin-3-yl: 2-trifluoromethylpyridine-3-yl 3,6-Cl.sub.2-pyridin-2-yl: 3,6-dichloropyridine-2-yl CH.sub.2OTBS: tert-butyldimethylsilyloxymethyl C(?O(4-Cl)Ph: 4-chlorobenzoyl
(102) TABLE-US-00001 TABLE 1
(103) TABLE-US-00002 TABLE 2 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8)m p A-0053 H H H H H O H H 2-CF.sub.2Cl 0 A-0054 H H H H H O H H 3-CF.sub.2Cl 0 A-0055 H H H H H O H H 4-CF.sub.2Cl 0 A-0056 H H H H H O H H 2-CF(CF.sub.3).sub.2 0 A-0057 H H H H H O H H 3-CF(CF.sub.3).sub.2 0 A-0058 H H H H H O H H 4-CF(CF.sub.3).sub.2 0 A-0059 H H H H H O H H 2-cyclopropyl 0 A-0060 H H H H H O H H 3-cyclopropyl 0 A-0061 H H H H H O H H 4-cyclopropyl 0 A-0062 H H H H H O H H 2-cyclobutyl 0 A-0063 H H H H H O H H 3-cyclobutyl 0 A-0064 H H H H H O H H 4-cyclobutyl 0 A-0065 H H H H H O H H 2-cyclopentyl 0 A-0066 H H H H H O H H 3-cyclopentyl 0 A-0067 H H H H H O H H 4-cyclopentyl 0 A-0068 H H H H H O H H 2-(cyclopropylmethyl) 0 A-0069 H H H H H O H H 3-(cyclopropylmethyl) 0 A-0070 H H H H H O H H 4-(cyclopropylmethyl) 0 A-0071 H H H H H O H H 2-(cyclobutylmethyl) 0 A-0072 H H H H H O H H 3-(cyclobutylmethyl) 0 A-0073 H H H H H O H H 4-(cyclobutylmethyl) 0 A-0074 H H H H H O H H 2-(cyclopentylmethyl) 0 A-0075 H H H H H O H H 3-(cyclopentylmethyl) 0 A-0076 H H H H H O H H 4-(cyclopentylmethyl) 0 A-0077 H H H H H O H H 2-(cyclopropylethyl) 0 A-0078 H H H H H O H H 3-(cyclopropylethyl) 0 A-0079 H H H H H O H H 4-(cyclopropylethyl) 0 A-0080 H H H H H O H H 2-(2,2-difluorocyclopropyl) 0 A-0081 H H H H H O H H 3-(2,2-difluorocyclopropyl) 0 A-0082 H H H H H O H H 4-(2,2-difluorocyclopropyl) 0 A-0083 H H H H H O H H 2-(2,2-dichlorocyclopropyl) 0 A-0084 H H H H H O H H 3-(2,2-dichlorocyclopropyl) 0 A-0085 H H H H H O H H 4-(2,2-dichlorocyclopropyl) 0 A-0086 H H H H H O H H 2-ethenyl 0 A-0087 H H H H H O H H 3-ethenyl 0 A-0088 H H H H H O H H 4-ethenyl 0 A-0089 H H H H H O H H 2-allyl 0 A-0090 H H H H H O H H 3-allyl 0 A-0091 H H H H H O H H 4-allyl 0 A-0092 H H H H H O H H 2-(prop-1-en-1-yl) 0 A-0093 H H H H H O H H 3-(prop-1-en-1-yl) 0 A-0094 H H H H H O H H 4-(prop-1-en-1-yl) 0 A-0095 H H H H H O H H 2-(trifluoroethenyl) 0 A-0096 H H H H H O H H 3-(trifluoroethenyl) 0 A-0097 H H H H H O H H 4-(trifluoroethenyl) 0 A-0098 H H H H H O H H 2-(2,2-dichloroethenyl) 0 A-0099 H H H H H O H H 3-(2,2-dichloroethenyl) 0 A-0100 H H H H H O H H 4-(2,2-dichloroethenyl) 0 A-0101 H H H H H O H H 2-ethynyl 0 A-0102 H H H H H O H H 3-ethynyl 0 A-0103 H H H H H O H H 4-ethynyl 0 A-0104 H H H H H O H H 2-(1-propyn-1-yl) 0 A-0105 H H H H H O H H 3-(1-propyn-1-yl) 0 A-0106 H H H H H O H H 4-(1-propyn-1-yl) 0 A-0107 H H H H H O H H 2-(2-propyn-1-yl) 0 A-0108 H H H H H O H H 3-(2-propyn-1-yl) 0 A-0109 H H H H H O H H 4-(2-propyn-1-yl) 0
(104) TABLE-US-00003 TABLE 3 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8)m p A-0110 H H H H H O H H 2-(2-cyclopropylethynyl) 0 A-0111 H H H H H O H H 3-(2-cyclopropylethynyl) 0 A-0112 H H H H H O H H 4-(2-cyclopropylethynyl) 0 A-0113 H H H H H O H H 2-(2-chloroethynyl) 0 A-0114 H H H H H O H H 3-(2-chloroethynyl) 0 A-0115 H H H H H O H H 4-(2-chloroethynyl) 0 A-0116 H H H H H O H H 2-(2-bromoethynyl) 0 A-0117 H H H H H O H H 3-(2-bromoethynyl) 0 A-0118 H H H H H O H H 4-(2-bromoethynyl) 0 A-0119 H H H H H O H H 2-OMe 0 A-0120 H H H H H O H H 3-OMe 0 A-0121 H H H H H O H H 4-OMe 0 A-0122 H H H H H O H H 2-OEt 0 A-0123 H H H H H O H H 3-OEt 0 A-0124 H H H H H O H H 4-OEt 0 A-0125 H H H H H O H H 2-OPr 0 A-0126 H H H H H O H H 3-OPr 0 A-0127 H H H H H O H H 4-OPr 0 A-0128 H H H H H O H H 2-O(i-Pr) 0 A-0129 H H H H H O H H 3-O(i-Pr) 0 A-0130 H H H H H O H H 4-O(i-Pr) 0 A-0131 H H H H H O H H 2-OBu 0 A-0132 H H H H H O H H 3-OBu 0 A-0133 H H H H H O H H 4-OBu 0 A-0134 H H H H H O H H 2-O(s-Bu) 0 A-0135 H H H H H O H H 3-O(s-Bu) 0 A-0136 H H H H H O H H 4-O(s-Bu) 0 A-0137 H H H H H O H H 2-O(i-Bu) 0 A-0138 H H H H H O H H 3-O(i-Bu) 0 A-0139 H H H H H O H H 4-O(i-Bu) 0 A-0140 H H H H H O H H 2-O(t-Bu) 0 A-0141 H H H H H O H H 3-O(t-Bu) 0 A-0142 H H H H H O H H 4-O(t-Bu) 0 A-0143 H H H H H O H H 2-OCF.sub.3 0 A-0144 H H H H H O H H 3-OCF.sub.3 0 A-0145 H H H H H O H H 4-OCF.sub.3 0 A-0146 H H H H H O H H 2-OCHF.sub.2 0 A-0147 H H H H H O H H 3-OCHF.sub.2 0 A-0148 H H H H H O H H 4-OCHF.sub.2 0 A-0149 H H H H H O H H 2-OCH.sub.2CF.sub.3 0 A-0150 H H H H H O H H 3-OCH.sub.2CF.sub.3 0 A-0151 H H H H H O H H 4-OCH.sub.2CF.sub.3 0 A-0152 H H H H H O H H 2-(cyclopropyloxy) 0 A-0153 H H H H H O H H 3-(cyclopropyloxy) 0 A-0154 H H H H H O H H 4-(cyclopropyloxy) 0 A-0155 H H H H H O H H 2-(cyclobutyloxy) 0 A-0156 H H H H H O H H 3-(cyclobutyloxy) 0 A-0157 H H H H H O H H 4-(cyclobutyloxy) 0 A-0158 H H H H H O H H 2-(cyclopentyloxy) 0 A-0159 H H H H H O H H 3-(cyclopentyloxy) 0 A-0160 H H H H H O H H 4-(cyclopentyloxy) 0 A-0161 H H H H H O H H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-0162 H H H H H O H H 3-((2,2-dichlorocyclopropyl)oxy) 0 A-0163 H H H H H O H H 4-((2,2-dichlorocyclopropyl)oxy) 0 A-0164 H H H H H O H H 2-(cyclopropylmethoxy) 0 A-0165 H H H H H O H H 3-(cyclopropylmethoxy) 0 A-0166 H H H H H O H H 4-(cyclopropylmethoxy) 0
(105) TABLE-US-00004 TABLE 4 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-0167 H H H H H O H H 2-((2,2-difluorocyclopropyl)methoxy) 0 A-0168 H H H H H O H H 3-((2,2-difluorocyclopropyl)methoxy) 0 A-0169 H H H H H O H H 4-((2,2-difluorocyclopropyl)methoxy) 0 A-0170 H H H H H O H H 2-(oxiran-2-yl) 0 A-0171 H H H H H O H H 3-(oxiran-2-yl) 0 A-0172 H H H H H O H H 4-(oxiran-2-yl) 0 A-0173 H H H H H O H H 2-(oxiran-2-ylmethyl) 0 A-0174 H H H H H O H H 3-(oxiran-2-ylmethyl) 0 A-0175 H H H H H O H H 4-(oxiran-2-ylmethyl) 0 A-0176 H H H H H O H H 2-SMe 0 A-0177 H H H H H O H H 3-SMe 0 A-0178 H H H H H O H H 4-SMe 0 A-0179 H H H H H O H H 2-SEt 0 A-0180 H H H H H O H H 3-SEt 0 A-0181 H H H H H O H H 4-SEt 0 A-0182 H H H H H O H H 2-S(?O)Me 0 A-0183 H H H H H O H H 3-S(?O)Me 0 A-0184 H H H H H O H H 4-S(?O)Me 0 A-0185 H H H H H O H H 2-S(?O).sub.2Me 0 A-0186 H H H H H O H H 3-S(?O).sub.2Me 0 A-0187 H H H H H O H H 4-S(?O).sub.2Me 0 A-0188 H H H H H O H H 2-SCF.sub.3 0 A-0189 H H H H H O H H 3-SCF.sub.3 0 A-0190 H H H H H O H H 4-SCF.sub.3 0 A-0191 H H H H H O H H 2-S(?O)CF.sub.3 0 A-0192 H H H H H O H H 3-S(?O)CF.sub.3 0 A-0193 H H H H H O H H 4-S(?O)CF.sub.3 0 A-0194 H H H H H O H H 2-S(?O).sub.2CF.sub.3 0 A-0195 H H H H H O H H 3-S(?O).sub.2CF.sub.3 0 A-0196 H H H H H O H H 4-S(?O).sub.2CF.sub.3 0 A-0197 H H H H H O H H 2-SCF(CF.sub.3).sub.2 0 A-0198 H H H H H O H H 3-SCF(CF.sub.3).sub.2 0 A-0199 H H H H H O H H 4-SCF(CF.sub.3).sub.2 0 A-0200 H H H H H O H H 2-(cyclopropylthio) 0 A-0201 H H H H H O H H 3-(cyclopropylthio) 0 A-0202 H H H H H O H H 4-(cyclopropylthio) 0 A-0203 H H H H H O H H 2-(cyclopropylsulfinyl) 0 A-0204 H H H H H O H H 3-(cyclopropylsulfinyl) 0 A-0205 H H H H H O H H 4-(cyclopropylsulfinyl) 0 A-0206 H H H H H O H H 2-(cyclopropylsulfonyl) 0 A-0207 H H H H H O H H 3-(cyclopropylsulfonyl) 0 A-0208 H H H H H O H H 4-(cyclopropylsulfonyl) 0 A-0209 H H H H H O H H 2-((cyclopropylmethyl)thio) 0 A-0210 H H H H H O H H 3-((cyclopropylmethyl)thio) 0 A-0211 H H H H H O H H 4-((cyclopropylmethyl)thio) 0 A-0212 H H H H H O H H 2-((cyclopropylmethyl)sulfinyl) 0 A-0213 H H H H H O H H 3-((cyclopropylmethyl)sulfinyl) 0 A-0214 H H H H H O H H 4-((cyclopropylmethyl)sulfinyl) 0 A-0215 H H H H H O H H 2-((cyclopropylmethyl)sulfonyl) 0 A-0216 H H H H H O H H 3-((cyclopropylmethyl)sulfonyl) 0 A-0217 H H H H H O H H 4-((cyclopropylmethyl)sulfonyl) 0 A-0218 H H H H H O H H 2-(((2,2-difluorocyclopropyl)methyl)thio) 0 A-0219 H H H H H O H H 3-(((2,2-difluorocyclopropyl)methyl)thio) 0 A-0220 H H H H H O H H 4-(((2,2-difluorocyclopropyl)methyl)thio) 0 A-0221 H H H H H O H H 2-(((2,2-difluorocyclopropyl)methyl)sulfinyl) 0 A-0222 H H H H H O H H 3-(((2,2-difluorocyclopropyl)methyl)sulfinyl) 0 A-0223 H H H H H O H H 4-(((2,2-difluorocyclopropyl)methyl)sulfinyl) 0
(106) TABLE-US-00005 TABLE 5 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-0224 H H H H H O H H 2-(((2,2-difluorocyclopropyl)methyl)sulfonyl) 0 A-0225 H H H H H O H H 3-(((2,2-difluorocyclopropyl)methyl)sulfonyl) 0 A-0226 H H H H H O H H 4-(((2,2-difluorocyclopropyl)methyl)sulfonyl) 0 A-0227 H H H H H O H H 2-C(?O)Me 0 A-0228 H H H H H O H H 3-C(?O)Me 0 A-0229 H H H H H O H H 4-C(?O)Me 0 A-0230 H H H H H O H H 2-C(?O)Et 0 A-0231 H H H H H O H H 3-C(?O)Et 0 A-0232 H H H H H O H H 4-C(?O)Et 0 A-0233 H H H H H O H H 2-C(?O)CF.sub.3 0 A-0234 H H H H H O H H 3-C(?O)CF.sub.3 0 A-0235 H H H H H O H H 4-C(?O)CF.sub.3 0 A-0236 H H H H H O H H 2-C(?O)OMe 0 A-0237 H H H H H O H H 3-C(?O)OMe 0 A-0238 H H H H H O H H 4-C(?O)OMe 0 A-0239 H H H H H O H H 2-C(?O)OET 0 A-0240 H H H H H O H H 3-C(?O)OET 0 A-0241 H H H H H O H H 4-C(?O)OET 0 A-0242 H H H H H O H H 2-C(?O)NH.sub.2 0 A-0243 H H H H H O H H 3-C(?O)NH.sub.2 0 A-0244 H H H H H O H H 4-C(?O)NH.sub.2 0 A-0245 H H H H H O H H 2-C(?O)NHMe 0 A-0246 H H H H H O H H 3-C(?O)NHMe 0 A-0247 H H H H H O H H 4-C(?O)NHMe 0 A-0248 H H H H H O H H 2-C(?O)NMe.sub.2 0 A-0249 H H H H H O H H 3-C(?O)NMe.sub.2 0 A-0250 H H H H H O H H 4-C(?O)NMe.sub.2 0 A-0251 H H H H H O H H 2-CH.sub.2C(?O)CH.sub.3 0 A-0252 H H H H H O H H 3-CH.sub.2C(?O)CH.sub.3 0 A-0253 H H H H H O H H 4-CH.sub.2C(?O)CH.sub.3 0 A-0254 H H H H H O H H 2-CH.sub.2C(?O)CF.sub.3 0 A-0255 H H H H H O H H 3-CH.sub.2C(?O)CF.sub.3 0 A-0256 H H H H H O H H 4-CH.sub.2C(?O)CF.sub.3 0 A-0257 H H H H H O H H 2-CH.sub.2C(?O)OCH.sub.3 0 A-0258 H H H H H O H H 3-CH.sub.2C(?O)OCH.sub.3 0 A-0259 H H H H H O H H 4-CH.sub.2C(?O)OCH.sub.3 0 A-0260 H H H H H O H H 2-CH.sub.2OH 0 A-0261 H H H H H O H H 3-CH.sub.2OH 0 A-0262 H H H H H O H H 4-CH.sub.2OH 0 A-0263 H H H H H O H H 2-CH.sub.2OCH.sub.3 0 A-0264 H H H H H O H H 3-CH.sub.2OCH.sub.3 0 A-0265 H H H H H O H H 4-CH.sub.2OCH.sub.3 0 A-0266 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-0267 H H H H H O H H 3-CH.sub.2OCH.sub.2CH.sub.3 0 A-0268 H H H H H O H H 4-CH.sub.2OCH.sub.2CH.sub.3 0 A-0269 H H H H H O H H 2-CH(CH.sub.3)OCH.sub.3 0 A-0270 H H H H H O H H 3-CH(CH.sub.3)OCH.sub.3 0 A-0271 H H H H H O H H 4-CH(CH.sub.3)OCH.sub.3 0 A-0272 H H H H H O H H 2-CH.sub.2CH.sub.2OCH.sub.3 0 A-0273 H H H H H O H H 3-CH.sub.2CH.sub.2OCH.sub.3 0 A-0274 H H H H H O H H 4-CH.sub.2CH.sub.2OCH.sub.3 0 A-0275 H H H H H O H H 2-CH.sub.2OCF.sub.3 0 A-0276 H H H H H O H H 3-CH.sub.2OCF.sub.3 0 A-0277 H H H H H O H H 4-CH.sub.2OCF.sub.3 0 A-0278 H H H H H O H H 2-CF.sub.2OCH.sub.3 0 A-0279 H H H H H O H H 3-CF.sub.2OCH.sub.3 0 A-0280 H H H H H O H H 4-CF.sub.2OCH.sub.3 0
(107) TABLE-US-00006 TABLE 6 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-0281 H H H H H O H H 2-CF.sub.2CF.sub.2OCF.sub.3 0 A-0282 H H H H H O H H 3-CF.sub.2CF.sub.2OCF.sub.3 0 A-0283 H H H H H O H H 4-CF.sub.2CF.sub.2OCF.sub.3 0 A-0284 H H H H H O H H 2-OC(?O)CH.sub.3 0 A-0285 H H H H H O H H 3-OC(?O)CH.sub.3 0 A-0286 H H H H H O H H 4-OC(?O)CH.sub.3 0 A-0287 H H H H H O H H 2-OC(?O)CF.sub.3 0 A-0288 H H H H H O H H 3-OC(?O)CF.sub.3 0 A-0289 H H H H H O H H 4-OC(?O)CF.sub.3 0 A-0290 H H H H H O H H 2-OC(?O)NH.sub.2 0 A-0291 H H H H H O H H 3-OC(?O)NH.sub.2 0 A-0292 H H H H H O H H 4-OC(?O)NH.sub.2 0 A-0293 H H H H H O H H 2-OC(?O)NHCH.sub.3 0 A-0294 H H H H H O H H 3-OC(?O)NHCH.sub.3 0 A-0295 H H H H H O H H 4-OC(?O)NHCH.sub.3 0 A-0296 H H H H H O H H 2-OC(?O)N(CH.sub.3).sub.2 0 A-0297 H H H H H O H H 3-OC(?O)N(CH.sub.3).sub.2 0 A-0298 H H H H H O H H 4-OC(?O)N(CH.sub.3).sub.2 0 A-0299 H H H H H O H H 2-CH.sub.2OC(?O)NH.sub.2 0 A-0300 H H H H H O H H 3-CH.sub.2OC(?O)NH.sub.2 0 A-0301 H H H H H O H H 4-CH.sub.2OC(?O)NH.sub.2 0 A-0302 H H H H H O H H 2-CH.sub.2OC(?O)NHCH.sub.3 0 A-0303 H H H H H O H H 3-CH.sub.2OC(?O)NHCH.sub.3 0 A-0304 H H H H H O H H 4-CH.sub.2OC(?O)NHCH.sub.3 0 A-0305 H H H H H O H H 2-CH.sub.2OC(?O)N(CH.sub.3).sub.2 0 A-0306 H H H H H O H H 3-CH.sub.2OC(?O)N(CH.sub.3).sub.2 0 A-0307 H H H H H O H H 4-CH.sub.2OC(?O)N(CH.sub.3).sub.2 0 A-0308 H H H H H O H H 2-OC(?O)OCH.sub.3 0 A-0309 H H H H H O H H 3-OC(?O)OCH.sub.3 0 A-0310 H H H H H O H H 4-OC(?O)OCH.sub.3 0 A-0311 H H H H H O H H 2-CH.sub.2OC(?O)OCH.sub.3 0 A-0312 H H H H H O H H 3-CH.sub.2OC(?O)OCH.sub.3 0 A-0313 H H H H H O H H 4-CH.sub.2OC(?O)OCH.sub.3 0 A-0314 H H H H H O H H 2-CH.sub.2OC(?O)CH.sub.3 0 A-0315 H H H H H O H H 3-CH.sub.2OC(?O)CH.sub.3 0 A-0316 H H H H H O H H 4-CH.sub.2OC(?O)CH.sub.3 0 A-0317 H H H H H O H H 2-OS(?O).sub.2CH.sub.3 0 A-0318 H H H H H O H H 3-OS(?O).sub.2CH.sub.3 0 A-0319 H H H H H O H H 4-OS(?O).sub.2CH.sub.3 0 A-0320 H H H H H O H H 2-CH.sub.2SCH.sub.3 0 A-0321 H H H H H O H H 3-CH.sub.2SCH.sub.3 0 A-0322 H H H H H O H H 4-CH.sub.2SCH.sub.3 0 A-0323 H H H H H O H H 2-CH.sub.2S(?O)CH.sub.3 0 A-0324 H H H H H O H H 3-CH.sub.2S(?O)CH.sub.3 0 A-0325 H H H H H O H H 4-CH.sub.2S(?O)CH.sub.3 0 A-0326 H H H H H O H H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-0327 H H H H H O H H 3-CH.sub.2S(?O).sub.2CH.sub.3 0 A-0328 H H H H H O H H 4-CH.sub.2S(?O).sub.2CH.sub.3 0 A-0329 H H H H H O H H 2-CH.sub.2SCF.sub.3 0 A-0330 H H H H H O H H 3-CH.sub.2SCF.sub.3 0 A-0331 H H H H H O H H 4-CH.sub.2SCF.sub.3 0 A-0332 H H H H H O H H 2-CH.sub.2S(?O)CF.sub.3 0 A-0333 H H H H H O H H 3-CH.sub.2S(?O)CF.sub.3 0 A-0334 H H H H H O H H 4-CH.sub.2S(?O)CF.sub.3 0 A-0335 H H H H H O H H 2-CH.sub.2S(?O).sub.2CF.sub.3 0 A-0336 H H H H H O H H 3-CH.sub.2S(?O).sub.2CF.sub.3 0 A-0337 H H H H H O H H 4-CH.sub.2S(?O).sub.2CF.sub.3 0
(108) TABLE-US-00007 TABLE 7 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-0338 H H H H H O H H 2-phenyl 0 A-0339 H H H H H O H H 3-phenyl 0 A-0340 H H H H H O H H 4-phenyl 0 A-0341 H H H H H O H H 2-(phenyl)oxy) 0 A-0342 H H H H H O H H 3-(phenyl)oxy) 0 A-0343 H H H H H O H H 4-(phenyl)oxy) 0 A-0344 H H H H H O H H 2-benzyl 0 A-0345 H H H H H O H H 3-benzyl 0 A-0346 H H H H H O H H 4-benzyl 0 A-0347 H H H H H O H H 2-(benzyl)oxy) 0 A-0348 H H H H H O H H 3-(benzyl)oxy) 0 A-0349 H H H H H O H H 4-(benzyl)oxy) 0 A-0350 H H H H H O H H 2-((2-fluorobenzyl)oxy) 0 A-0351 H H H H H O H H 3-((2-fluorobenzyl)oxy) 0 A-0352 H H H H H O H H 4-((2-fluorobenzyl)oxy) 0 A-0353 H H H H H O H H 2-((3-fluorobenzyl)oxy) 0 A-0354 H H H H H O H H 3-((3-fluorobenzyl)oxy) 0 A-0355 H H H H H O H H 4-((3-fluorobenzyl)oxy) 0 A-0356 H H H H H O H H 2-((4-fluorobenzyl)oxy) 0 A-0357 H H H H H O H H 3-((4-fluorobenzyl)oxy) 0 A-0358 H H H H H O H H 4-((4-fluorobenzyl)oxy) 0 A-0359 H H H H H O H H 2-((2-chlorobenzyl)oxy) 0 A-0360 H H H H H O H H 3-((2-chlorobenzyl)oxy) 0 A-0361 H H H H H O H H 4-((2-chlorobenzyl)oxy) 0 A-0362 H H H H H O H H 2-((3-chlorobenzyl)oxy) 0 A-0363 H H H H H O H H 3-((3-chlorobenzyl)oxy) 0 A-0364 H H H H H O H H 4-((3-chlorobenzyl)oxy) 0 A-0365 H H H H H O H H 2-((4-chlorobenzyl)oxy) 0 A-0366 H H H H H O H H 3-((4-chlorobenzyl)oxy) 0 A-0367 H H H H H O H H 4-((4-chlorobenzyl)oxy) 0 A-0368 H H H H H O H H 2-((2-methybenzyl)oxy) 0 A-0369 H H H H H O H H 3-((2-methybenzyl)oxy) 0 A-0370 H H H H H O H H 4-((2-methybenzyl)oxy) 0 A-0371 H H H H H O H H 2-((3-methybenzyl)oxy) 0 A-0372 H H H H H O H H 3-((3-methybenzyl)oxy) 0 A-0373 H H H H H O H H 4-((3-methybenzyl)oxy) 0 A-0374 H H H H H O H H 2-((4-methybenzyl)oxy) 0 A-0375 H H H H H O H H 3-((4-methybenzyl)oxy) 0 A-0376 H H H H H O H H 4-((4-methybenzyl)oxy) 0 A-0377 H H H H H O H H 2-((2-(trifluoromethyl)benzyl)oxy) 0 A-0378 H H H H H O H H 3-((2-(trifluoromethyl)benzyl)oxy) 0 A-0379 H H H H H O H H 4-((2-(trifluoromethyl)benzyl)oxy) 0 A-0380 H H H H H O H H 2-((3-(trifluoromethyl)benzyl)oxy) 0 A-0381 H H H H H O H H 3-((3-(trifluoromethyl)benzyl)oxy) 0 A-0382 H H H H H O H H 4-((3-(trifluoromethyl)benzyl)oxy) 0 A-0383 H H H H H O H H 2-((4-(trifluoromethyl)benzyl)oxy) 0 A-0384 H H H H H O H H 3-((4-(trifluoromethyl)benzyl)oxy) 0 A-0385 H H H H H O H H 4-((4-(trifluoromethyl)benzyl)oxy) 0 A-0386 H H H H H O H H 2-((2-methoxybenzyl)oxy) 0 A-0387 H H H H H O H H 3-((2-methoxybenzyl)oxy) 0 A-0388 H H H H H O H H 4-((2-methoxybenzyl)oxy) 0 A-0389 H H H H H O H H 2-((3-methoxybenzyl)oxy) 0 A-0390 H H H H H O H H 3-((3-methoxybenzyl)oxy) 0 A-0391 H H H H H O H H 4-((3-methoxybenzyl)oxy) 0 A-0392 H H H H H O H H 2-((4-methoxybenzyl)oxy) 0 A-0393 H H H H H O H H 3-((4-methoxybenzyl)oxy) 0 A-0394 H H H H H O H H 4-((4-methoxybenzyl)oxy) 0
(109) TABLE-US-00008 TABLE 8 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-0395 H H H H H O H H 2-((2-(trifluoromethoxy)benzyl)oxy) 0 A-0396 H H H H H O H H 3-((2-(trifluoromethoxy)benzyl)oxy) 0 A-0397 H H H H H O H H 4-((2-(trifluoromethoxy)benzyl)oxy) 0 A-0398 H H H H H O H H 2-((3-(trifluoromethoxy)benzyl)oxy) 0 A-0399 H H H H H O H H 3-((3-(trifluoromethoxy)benzyl)oxy) 0 A-0400 H H H H H O H H 4-((3-(trifluoromethoxy)benzyl)oxy) 0 A-0401 H H H H H O H H 2-((4-(trifluoromethoxy)benzyl)oxy) 0 A-0402 H H H H H O H H 3-((4-(trifluoromethoxy)benzyl)oxy) 0 A-0403 H H H H H O H H 4-((4-(trifluoromethoxy)benzyl)oxy) 0 A-0404 H H H H H O H H 2-((2-(methylthio)benzyl)oxy) 0 A-0405 H H H H H O H H 3-((2-(methylthio)benzyl)oxy) 0 A-0406 H H H H H O H H 4-((2-(methylthio)benzyl)oxy) 0 A-0407 H H H H H O H H 2-((3-(methylthio)benzyl)oxy) 0 A-0408 H H H H H O H H 3-((3-(methylthio)benzyl)oxy) 0 A-0409 H H H H H O H H 4-((3-(methylthio)benzyl)oxy) 0 A-0410 H H H H H O H H 2-((4-(methylthio)benzyl)oxy) 0 A-0411 H H H H H O H H 3-((4-(methylthio)benzyl)oxy) 0 A-0412 H H H H H O H H 4-((4-(methylthio)benzyl)oxy) 0 A-0413 H H H H H O H H 2-((2-(methylsulfinyl)benzyl)oxy) 0 A-0414 H H H H H O H H 3-((2-(methylsulfinyl)benzyl)oxy) 0 A-0415 H H H H H O H H 4-((2-(methylsulfinyl)benzyl)oxy) 0 A-0416 H H H H H O H H 2-((3-(methylsulfinyl)benzyl)oxy) 0 A-0417 H H H H H O H H 3-((3-(methylsulfinyl)benzyl)oxy) 0 A-0418 H H H H H O H H 4-((3-(methylsulfinyl)benzyl)oxy) 0 A-0419 H H H H H O H H 2-((4-(methylsulfinyl)benzyl)oxy) 0 A-0420 H H H H H O H H 3-((4-(methylsulfinyl)benzyl)oxy) 0 A-0421 H H H H H O H H 4-((4-(methylsulfinyl)benzyl)oxy) 0 A-0422 H H H H H O H H 2-((2-(methylsulfonyl)benzyl)oxy) 0 A-0423 H H H H H O H H 3-((2-(methylsulfonyl)benzyl)oxy) 0 A-0424 H H H H H O H H 4-((2-(methylsulfonyl)benzyl)oxy) 0 A-0425 H H H H H O H H 2-((3-(methylsulfonyl)benzyl)oxy) 0 A-0426 H H H H H O H H 3-((3-(methylsulfonyl)benzyl)oxy) 0 A-0427 H H H H H O H H 4-((3-(methylsulfonyl)benzyl)oxy) 0 A-0428 H H H H H O H H 2-((4-(methylsulfonyl)benzyl)oxy) 0 A-0429 H H H H H O H H 3-((4-(methylsulfonyl)benzyl)oxy) 0 A-0430 H H H H H O H H 4-((4-(methylsulfonyl)benzyl)oxy) 0 A-0431 H H H H H O H H 2-((2-(trifluoromethylthio)benzyl)oxy) 0 A-0432 H H H H H O H H 3-((2-(trifluoromethylthio)benzyl)oxy) 0 A-0433 H H H H H O H H 4-((2-(trifluoromethylthio)benzyl)oxy) 0 A-0434 H H H H H O H H 2-((3-(trifluoromethylthio)benzyl)oxy) 0 A-0435 H H H H H O H H 3-((3-(trifluoromethylthio)benzyl)oxy) 0 A-0436 H H H H H O H H 4-((3-(trifluoromethylthio)benzyl)oxy) 0 A-0437 H H H H H O H H 2-((4-(trifluoromethylthio)benzyl)oxy) 0 A-0438 H H H H H O H H 3-((4-(trifluoromethylthio)benzyl)oxy) 0 A-0439 H H H H H O H H 4-((4-(trifluoromethylthio)benzyl)oxy) 0 A-0440 H H H H H O H H 2-((2-(trifluoromethylsulfinyl)benzyl)oxy) 0 A-0441 H H H H H O H H 3-((2-(trifluoromethylsulfinyl)benzyl)oxy) 0 A-0442 H H H H H O H H 4-((2-(trifluoromethylsulfinyl)benzyl)oxy) 0 A-0443 H H H H H O H H 2-((3-(trifluoromethylsulfinyl)benzyl)oxy) 0 A-0444 H H H H H O H H 3-((3-(trifluoromethylsulfinyl)benzyl)oxy) 0 A-0445 H H H H H O H H 4-((3-(trifluoromethylsulfinyl)benzyl)oxy) 0 A-0446 H H H H H O H H 2-((4-(trifluoromethylsulfinyl)benzyl)oxy) 0 A-0447 H H H H H O H H 3-((4-(trifluoromethylsulfinyl)benzyl)oxy) 0 A-0448 H H H H H O H H 4-((4-(trifluoromethylsulfinyl)benzyl)oxy) 0 A-0449 H H H H H O H H 2-((2-(trifluoromethylsulfonyl)benzyl)oxy) 0 A-0450 H H H H H O H H 3-((2-(trifluoromethylsulfonyl)benzyl)oxy) 0 A-0451 H H H H H O H H 4-((2-(trifluoromethylsulfonyl)benzyl)oxy) 0
(110) TABLE-US-00009 TABLE 9 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-0452 H H H H H O H H 2-((3-(trifluoromethylsulfonyl)benzyl)oxy) 0 A-0453 H H H H H O H H 3-((3-(trifluoromethylsulfonyl)benzyl)oxy) 0 A-0454 H H H H H O H H 4-((3-(trifluoromethylsulfonyl)benzyl)oxy) 0 A-0455 H H H H H O H H 2-((4-(trifluoromethylsulfonyl)benzyl)oxy) 0 A-0456 H H H H H O H H 3-((4-(trifluoromethylsulfonyl)benzyl)oxy) 0 A-0457 H H H H H O H H 4-((4-(trifluoromethylsulfonyl)benzyl)oxy) 0 A-0458 H H H H H O H H 2-((2-aminobenzyl)oxy) 0 A-0459 H H H H H O H H 3-((2-aminobenzyl)oxy) 0 A-0460 H H H H H O H H 4-((2-aminobenzyl)oxy) 0 A-0461 H H H H H O H H 2-((3-aminobenzyl)oxy) 0 A-0462 H H H H H O H H 3-((3-aminobenzyl)oxy) 0 A-0463 H H H H H O H H 4-((3-aminobenzyl)oxy) 0 A-0464 H H H H H O H H 2-((4-aminobenzyl)oxy) 0 A-0465 H H H H H O H H 3-((4-aminobenzyl)oxy) 0 A-0466 H H H H H O H H 4-((4-aminobenzyl)oxy) 0 A-0467 H H H H H O H H 2-((2-(methylamino)benzyl)oxy) 0 A-0468 H H H H H O H H 3-((2-(methylamino)benzyl)oxy) 0 A-0469 H H H H H O H H 4-((2-(methylamino)benzyl)oxy) 0 A-0470 H H H H H O H H 2-((3-(methylamino)benzyl)oxy) 0 A-0471 H H H H H O H H 3-((3-(methylamino)benzyl)oxy) 0 A-0472 H H H H H O H H 4-((3-(methylamino)benzyl)oxy) 0 A-0473 H H H H H O H H 2-((4-(methylamino)benzyl)oxy) 0 A-0474 H H H H H O H H 3-((4-(methylamino)benzyl)oxy) 0 A-0475 H H H H H O H H 4-((4-(methylamino)benzyl)oxy) 0 A-0476 H H H H H O H H 2-((2-(dimethylamino)benzyl)oxy) 0 A-0477 H H H H H O H H 3-((2-(dimethylamino)benzyl)oxy) 0 A-0478 H H H H H O H H 4-((2-(dimethylamino)benzyl)oxy) 0 A-0479 H H H H H O H H 2-((3-(dimethylamino)benzyl)oxy) 0 A-0480 H H H H H O H H 3-((3-(dimethylamino)benzyl)oxy) 0 A-0481 H H H H H O H H 4-((3-(dimethylamino)benzyl)oxy) 0 A-0482 H H H H H O H H 2-((4-(dimethylamino)benzyl)oxy) 0 A-0483 H H H H H O H H 3-((4-(dimethylamino)benzyl)oxy) 0 A-0484 H H H H H O H H 4-((4-(dimethylamino)benzyl)oxy) 0 A-0485 H H H H H O H H 2-((2-cyanobenzyl)oxy) 0 A-0486 H H H H H O H H 3-((2-cyanobenzyl)oxy) 0 A-0487 H H H H H O H H 4-((2-cyanobenzyl)oxy) 0 A-0488 H H H H H O H H 2-((3-cyanobenzyl)oxy) 0 A-0489 H H H H H O H H 3-((3-cyanobenzyl)oxy) 0 A-0490 H H H H H O H H 4-((3-cyanobenzyl)oxy) 0 A-0491 H H H H H O H H 2-((4-cyanobenzyl)oxy) 0 A-0492 H H H H H O H H 3-((4-cyanobenzyl)oxy) 0 A-0493 H H H H H O H H 4-((4-cyanobenzyl)oxy) 0 A-0494 H H H H H O H H 2-((2-nitrobenzyl)oxy) 0 A-0495 H H H H H O H H 3-((2-nitrobenzyl)oxy) 0 A-0496 H H H H H O H H 4-((2-nitrobenzyl)oxy) 0 A-0497 H H H H H O H H 2-((3-nitrobenzyl)oxy) 0 A-0498 H H H H H O H H 3-((3-nitrobenzyl)oxy) 0 A-0499 H H H H H O H H 4-((3-nitrobenzyl)oxy) 0 A-0500 H H H H H O H H 2-((4-nitrobenzyl)oxy) 0 A-0501 H H H H H O H H 3-((4-nitrobenzyl)oxy) 0 A-0502 H H H H H O H H 4-((4-nitrobenzyl)oxy) 0 A-0503 H H H H H O H H 2-NH.sub.2 0 A-0504 H H H H H O H H 3-NH.sub.2 0 A-0505 H H H H H O H H 4-NH.sub.2 0 A-0506 H H H H H O H H 2-NHMe 0 A-0507 H H H H H O H H 3-NHMe 0 A-0508 H H H H H O H H 4-NHMe 0
(111) TABLE-US-00010 TABLE 10 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-0509 H H H H H O H H 2-NHEt 0 A-0510 H H H H H O H H 3-NHEt 0 A-0511 H H H H H O H H 4-NHEt 0 A-0512 H H H H H O H H 2-N(Me).sub.2 0 A-0513 H H H H H O H H 3-N(Me).sub.2 0 A-0514 H H H H H O H H 4-N(Me).sub.2 0 A-0515 H H H H H O H H 2-N(Et).sub.2 0 A-0516 H H H H H O H H 3-N(Et).sub.2 0 A-0517 H H H H H O H H 4-N(Et).sub.2 0 A-0518 H H H H H O H H 2-CHO 0 A-0519 H H H H H O H H 3-CHO 0 A-0520 H H H H H O H H 4-CHO 0 A-0521 H H H H H O H H 2-C(?O)OH 0 A-0522 H H H H H O H H 3-C(?O)OH 0 A-0523 H H H H H O H H 4-C(?O)OH 0 A-0524 H H H H H O H H 2-(1,3-dioxolan-2-yl) 0 A-0525 H H H H H O H H 3-(1,3-dioxolan-2-yl) 0 A-0526 H H H H H O H H 4-(1,3-dioxolan-2-yl) 0 A-0527 H H H H H O H H 2-(1,3-dioxan-2-yl) 0 A-0528 H H H H H O H H 3-(1,3-dioxan-2-yl) 0 A-0529 H H H H H O H H 4-(1,3-dioxan-2-yl) 0 A-0530 H H H H H O H H 2-(1H-imidazol-2-yl) 0 A-0531 H H H H H O H H 3-(1H-imidazol-2-yl) 0 A-0532 H H H H H O H H 4-(1H-imidazol-2-yl) 0 A-0533 H H H H H O H H 2-(thiazol-2-yl) 0 A-0534 H H H H H O H H 3-(thiazol-2-yl) 0 A-0535 H H H H H O H H 4-(thiazol-2-yl) 0 A-0536 H H H H H O H H 2-(oxazol-2-yl) 0 A-0537 H H H H H O H H 3-(oxazol-2-yl) 0 A-0538 H H H H H O H H 4-(oxazol-2-yl) 0 A-0539 H H H H H O H H 2-CH?NOH 0 A-0540 H H H H H O H H 3-CH?NOH 0 A-0541 H H H H H O H H 4-CH?NOH 0 A-0542 H H H H H O H H 2-CH?NOMe 0 A-0543 H H H H H O H H 3-CH?NOMe 0 A-0544 H H H H H O H H 4-CH?NOMe 0 A-0545 H H H H H O H H 2-(4,5-dihydro-3-isoxazolyl) 0 A-0546 H H H H H O H H 3-(4,5-dihydro-3-isoxazolyl) 0 A-0547 H H H H H O H H 4-(4,5-dihydro-3-isoxazolyl) 0 A-0548 H H H H H O H H 2-CN 0 A-0549 H H H H H O H H 3-CN 0 A-0550 H H H H H O H H 4-CN 0 A-0551 H H H H H O H H 2-NO.sub.2 0 A-0552 H H H H H O H H 3-NO.sub.2 0 A-0553 H H H H H O H H 4-NO.sub.2 0 A-0554 H H H H H O H H 2,3-F.sub.2 0 A-0555 H H H H H O H H 2,4-F.sub.2 0 A-0556 H H H H H O H H 2,5-F.sub.2 0 A-0557 H H H H H O H H 2,6-F.sub.2 0 A-0558 H H H H H O H H 3,4-F.sub.2 0 A-0559 H H H H H O H H 3,5-F.sub.2 0 A-0560 H H H H H O H H 2-F,3-Cl 0 A-0561 H H H H H O H H 2-F,4-Cl 0 A-0562 H H H H H O H H 2-F,5-Cl 0 A-0563 H H H H H O H H 2-F,6-Cl 0 A-0564 H H H H H O H H 3-F,2-Cl 0 A-0565 H H H H H O H H 3-F,4-Cl 0
(112) TABLE-US-00011 TABLE 11 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-0566 H H H H H O H H 3-F,5-Cl 0 A-0567 H H H H H O H H 3-F,6-Cl 0 A-0568 H H H H H O H H 4-F,2-Cl 0 A-0569 H H H H H O H H 4-F,3-Cl 0 A-0570 H H H H H O H H 2-F,3-Me 0 A-0571 H H H H H O H H 2-F,4-Me 0 A-0572 H H H H H O H H 2-F,5-Me 0 A-0573 H H H H H O H H 2-F,6-Me 0 A-0574 H H H H H O H H 3-F,2-Me 0 A-0575 H H H H H O H H 3-F,4-Me 0 A-0576 H H H H H O H H 3-F,5-Me 0 A-0577 H H H H H O H H 3-F,6-Me 0 A-0578 H H H H H O H H 4-F,2-Me 0 A-0579 H H H H H O H H 4-F,3-Me 0 A-0580 H H H H H O H H 2-F,3-CF.sub.3 0 A-0581 H H H H H O H H 2-F,4-CF.sub.3 0 A-0582 H H H H H O H H 2-F,5-CF.sub.3 0 A-0583 H H H H H O H H 2-F,6-CF.sub.3 0 A-0584 H H H H H O H H 3-F,2-CF.sub.3 0 A-0585 H H H H H O H H 3-F,4-CF.sub.3 0 A-0586 H H H H H O H H 3-F,5-CF.sub.3 0 A-0587 H H H H H O H H 3-F,6-CF.sub.3 0 A-0588 H H H H H O H H 4-F,2-CF.sub.3 0 A-0589 H H H H H O H H 4-F,3-CF.sub.3 0 A-0590 H H H H H O H H 2-F,3-OMe 0 A-0591 H H H H H O H H 2-F,4-OMe 0 A-0592 H H H H H O H H 2-F,5-OMe 0 A-0593 H H H H H O H H 2-F,6-OMe 0 A-0594 H H H H H O H H 3-F,2-OMe 0 A-0595 H H H H H O H H 3-F,4-OMe 0 A-0596 H H H H H O H H 3-F,5-OMe 0 A-0597 H H H H H O H H 3-F,6-OMe 0 A-0598 H H H H H O H H 4-F,2-OMe 0 A-0599 H H H H H O H H 4-F,3-OMe 0 A-0600 H H H H H O H H 2,3-Cl.sub.2 0 A-0601 H H H H H O H H 2,4-Cl.sub.2 0 A-0602 H H H H H O H H 2,5-Cl.sub.2 0 A-0603 H H H H H O H H 2,6-Cl.sub.2 0 A-0604 H H H H H O H H 3,4-Cl.sub.2 0 A-0605 H H H H H O H H 3,5-Cl.sub.2 0 A-0606 H H H H H O H H 2-Cl,3-Me 0 A-0607 H H H H H O H H 2-Cl,4-Me 0 A-0608 H H H H H O H H 2-Cl,5-Me 0 A-0609 H H H H H O H H 2-Cl,6-Me 0 A-0610 H H H H H O H H 3-Cl,2-Me 0 A-0611 H H H H H O H H 3-Cl,4-Me 0 A-0612 H H H H H O H H 3-Cl,5-Me 0 A-0613 H H H H H O H H 3-Cl,6-Me 0 A-0614 H H H H H O H H 4-Cl,2-Me 0 A-0615 H H H H H O H H 4-Cl,3-Me 0 A-0616 H H H H H O H H 2-Cl,3-CF.sub.3 0 A-0617 H H H H H O H H 2-Cl,4-CF.sub.3 0 A-0618 H H H H H O H H 2-Cl,5-CF.sub.3 0 A-0619 H H H H H O H H 2-Cl,6-CF.sub.3 0 A-0620 H H H H H O H H 3-Cl,2-CF.sub.3 0 A-0621 H H H H H O H H 3-Cl,4-CF.sub.3 0 A-0622 H H H H H O H H 3-Cl,5-CF.sub.3 0
(113) TABLE-US-00012 TABLE 12 com- pound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-0623 H H H H H O H H 3-Cl,6-CF.sub.3 0 A-0624 H H H H H O H H 4-Cl,2-CF.sub.3 0 A-0625 H H H H H O H H 4-Cl,3-CF.sub.3 0 A-0626 H H H H H O H H 2-Cl,3-OMe 0 A-0627 H H H H H O H H 2-Cl,4-OMe 0 A-0628 H H H H H O H H 2-Cl,5-OMe 0 A-0629 H H H H H O H H 2-Cl,6-OMe 0 A-0630 H H H H H O H H 3-Cl,2-OMe 0 A-0631 H H H H H O H H 3-Cl,4-OMe 0 A-0632 H H H H H O H H 3-Cl,5-OMe 0 A-0633 H H H H H O H H 3-Cl,6-OMe 0 A-0634 H H H H H O H H 4-Cl,2-OMe 0 A-0635 H H H H H O H H 4-Cl,3-OMe 0 A-0636 H H H H H O H H 2,3-Me.sub.2 0 A-0637 H H H H H O H H 2,4-Me.sub.2 0 A-0638 H H H H H O H H 2,5-Me.sub.2 0 A-0639 H H H H H O H H 2,6-Me.sub.2 0 A-0640 H H H H H O H H 3,4-Me.sub.2 0 A-0641 H H H H H O H H 3,5-Me.sub.2 0 A-0642 H H H H H O H H 2-Me,3-CF.sub.3 0 A-0643 H H H H H O H H 2-Me,4-CF.sub.3 0 A-0644 H H H H H O H H 2-Me,5-CF.sub.3 0 A-0645 H H H H H O H H 2-Me,6-CF.sub.3 0 A-0646 H H H H H O H H 3-Me,2-CF.sub.3 0 A-0647 H H H H H O H H 3-Me,4-CF.sub.3 0 A-0648 H H H H H O H H 3-Me,5-CF.sub.3 0 A-0649 H H H H H O H H 3-Me,6-CF.sub.3 0 A-0650 H H H H H O H H 4-Me,2-CF.sub.3 0 A-0651 H H H H H O H H 4-Me,3-CF.sub.3 0 A-0652 H H H H H O H H 2-Me,3-OMe 0 A-0653 H H H H H O H H 2-Me,4-OMe 0 A-0654 H H H H H O H H 2-Me,5-OMe 0 A-0655 H H H H H O H H 2-Me,6-OMe 0 A-0656 H H H H H O H H 3-Me,2-OMe 0 A-0657 H H H H H O H H 3-Me,4-OMe 0 A-0658 H H H H H O H H 3-Me,5-OMe 0 A-0659 H H H H H O H H 3-Me,6-OMe 0 A-0660 H H H H H O H H 4-Me,2-OMe 0 A-0661 H H H H H O H H 4-Me,3-OMe 0 A-0662 H H H H H O H H 2,3-OMe.sub.2 0 A-0663 H H H H H O H H 2,4-OMe.sub.2 0 A-0664 H H H H H O H H 2,5-OMe.sub.2 0 A-0665 H H H H H O H H 2,6-OMe.sub.2 0 A-0666 H H H H H O H H 3,4-OMe.sub.2 0 A-0667 H H H H H O H H 3,5-OMe.sub.2 0 A-0668 H H H H H O H H 2-OMe,3-CF.sub.3 0 A-0669 H H H H H O H H 2-OMe,4-CF.sub.3 0 A-0670 H H H H H O H H 2-OMe,5-CF.sub.3 0 A-0671 H H H H H O H H 2-OMe,6-CF.sub.3 0 A-0672 H H H H H O H H 3-OMe,2-CF.sub.3 0 A-0673 H H H H H O H H 3-OMe,4-CF.sub.3 0 A-0674 H H H H H O H H 3-OMe,5-CF.sub.3 0 A-0675 H H H H H O H H 3-OMe,6-CF.sub.3 0 A-0676 H H H H H O H H 4-OMe,2-CF.sub.3 0 A-0677 H H H H H O H H 4-OMe,3-CF.sub.3 0 A-0678 H H H H H O H H 2-CHF.sub.2,3-F 0 A-0679 H H H H H O H H 2-CHF.sub.2,4-F 0
(114) TABLE-US-00013 TABLE 13 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-0680 H H H H H O H H 2-CHF.sub.2,5-F 0 A-0681 H H H H H O H H 2-CHF.sub.2,6-F 0 A-0682 H H H H H O H H 2-CHF.sub.2,3-Me 0 A-0683 H H H H H O H H 2-CHF.sub.2,4-Me 0 A-0684 H H H H H O H H 2-CHF.sub.2,5-Me 0 A-0685 H H H H H O H H 2-CHF.sub.2,6-Me 0 A-0686 H H H H H O H H 2-cyclopropyl,3-F 0 A-0687 H H H H H O H H 2-cyclopropyl,4-F 0 A-0688 H H H H H O H H 2-cyclopropyl,5-F 0 A-0689 H H H H H O H H 2-cyclopropyl,6-F 0 A-0690 H H H H H O H H 2-cyclopropyl,3-Me 0 A-0691 H H H H H O H H 2-cyclopropyl,4-Me 0 A-0692 H H H H H O H H 2-cyclopropyl,5-Me 0 A-0693 H H H H H O H H 2-cyclopropyl,6-Me 0 A-0694 H H H H H O H H 2-ethenyl,3-F 0 A-0695 H H H H H O H H 2-ethenyl,4-F 0 A-0696 H H H H H O H H 2-ethenyl,5-F 0 A-0697 H H H H H O H H 2-ethenyl,6-F 0 A-0698 H H H H H O H H 2-ethenyl,3-Me 0 A-0699 H H H H H O H H 2-ethenyl,4-Me 0 A-0700 H H H H H O H H 2-ethenyl,5-Me 0 A-0701 H H H H H O H H 2-ethenyl,6-Me 0 A-0702 H H H H H O H H 2-OET,3-F 0 A-0703 H H H H H O H H 2-OET,4-F 0 A-0704 H H H H H O H H 2-OET,5-F 0 A-0705 H H H H H O H H 2-OET,6-F 0 A-0706 H H H H H O H H 2-OET,3-Cl 0 A-0707 H H H H H O H H 2-OET,4-Cl 0 A-0708 H H H H H O H H 2-OET,5-Cl 0 A-0709 H H H H H O H H 2-OET,6-Cl 0 A-0710 H H H H H O H H 2-OET,3-Me 0 A-0711 H H H H H O H H 2-OET,4-Me 0 A-0712 H H H H H O H H 2-OET,5-Me 0 A-0713 H H H H H O H H 2-OET,6-Me 0 A-0714 H H H H H O H H 2-OPr,3-F 0 A-0715 H H H H H O H H 2-OPr,4-F 0 A-0716 H H H H H O H H 2-OPr,5-F 0 A-0717 H H H H H O H H 2-OPr,6-F 0 A-0718 H H H H H O H H 2-OPr,3-Me 0 A-0719 H H H H H O H H 2-OPr,4-Me 0 A-0720 H H H H H O H H 2-OPr,5-Me 0 A-0721 H H H H H O H H 2-OPr,6-Me 0 A-0722 H H H H H O H H 2-O(i-Pr),3-F 0 A-0723 H H H H H O H H 2-O(i-Pr),4-F 0 A-0724 H H H H H O H H 2-O(i-Pr),5-F 0 A-0725 H H H H H O H H 2-O(i-Pr),6-F 0 A-0726 H H H H H O H H 2-O(i-Pr),3-Me 0 A-0727 H H H H H O H H 2-O(i-Pr),4-Me 0 A-0728 H H H H H O H H 2-O(i-Pr),5-Me 0 A-0729 H H H H H O H H 2-O(i-Pr),6-Me 0 A-0730 H H H H H O H H 2-OCF.sub.3,3-F 0 A-0731 H H H H H O H H 2-OCF.sub.3,4-F 0 A-0732 H H H H H O H H 2-OCF.sub.3,5-F 0 A-0733 H H H H H O H H 2-OCF.sub.3,6-F 0 A-0734 H H H H H O H H 2-OCF.sub.3,3-Me 0 A-0735 H H H H H O H H 2-OCF.sub.3,4-Me 0 A-0736 H H H H H O H H 2-OCF.sub.3,5-Me 0
(115) TABLE-US-00014 TABLE 14 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-0737 H H H H H O H H 2-OCF.sub.3,6-Me 0 A-0738 H H H H H O H H 2-OCHF.sub.2,3-F 0 A-0739 H H H H H O H H 2-OCHF.sub.2,4-F 0 A-0740 H H H H H O H H 2-OCHF.sub.2,5-F 0 A-0741 H H H H H O H H 2-OCHF.sub.2,6-F 0 A-0742 H H H H H O H H 2-OCHF.sub.2,3-Me 0 A-0743 H H H H H O H H 2-OCHF.sub.2,4-Me 0 A-0744 H H H H H O H H 2-OCHF.sub.2,5-Me 0 A-0745 H H H H H O H H 2-OCHF.sub.2,6-Me 0 A-0746 H H H H H O H H 2-(cyclopropyl)oxy),3-F 0 A-0747 H H H H H O H H 2-(cyclopropyl)oxy),4-F 0 A-0748 H H H H H O H H 2-(cyclopropyl)oxy),5-F 0 A-0749 H H H H H O H H 2-(cyclopropyl)oxy),6-F 0 A-0750 H H H H H O H H 2-(cyclopropyl)oxy),3-Me 0 A-0751 H H H H H O H H 2-(cyclopropyl)oxy),4-Me 0 A-0752 H H H H H O H H 2-(cyclopropyl)oxy),5-Me 0 A-0753 H H H H H O H H 2-(cyclopropyl)oxy),6-Me 0 A-0754 H H H H H O H H 2-(oxiran-2-yl),3-F 0 A-0755 H H H H H O H H 2-(oxiran-2-yl),4-F 0 A-0756 H H H H H O H H 2-(oxiran-2-yl),5-F 0 A-0757 H H H H H O H H 2-(oxiran-2-yl),6-F 0 A-0758 H H H H H O H H 2-(oxiran-2-yl),3-Me 0 A-0759 H H H H H O H H 2-(oxiran-2-yl),4-Me 0 A-0760 H H H H H O H H 2-(oxiran-2-yl),5-Me 0 A-0761 H H H H H O H H 2-(oxiran-2-yl),6-Me 0 A-0762 H H H H H O H H 2-(oxiran-2-ylmethyl),3-F 0 A-0763 H H H H H O H H 2-(oxiran-2-ylmethyl),4-F 0 A-0764 H H H H H O H H 2-(oxiran-2-ylmethyl),5-F 0 A-0765 H H H H H O H H 2-(oxiran-2-ylmethyl),6-F 0 A-0766 H H H H H O H H 2-(oxiran-2-ylmethyl),3-Me 0 A-0767 H H H H H O H H 2-(oxiran-2-ylmethyl),4-Me 0 A-0768 H H H H H O H H 2-(oxiran-2-ylmethyl),5-Me 0 A-0769 H H H H H O H H 2-(oxiran-2-ylmethyl),6-Me 0 A-0770 H H H H H O H H 2-SMe,3-F 0 A-0771 H H H H H O H H 2-SMe,4-F 0 A-0772 H H H H H O H H 2-SMe,5-F 0 A-0773 H H H H H O H H 2-SMe,6-F 0 A-0774 H H H H H O H H 2-SMe,3-Me 0 A-0775 H H H H H O H H 2-SMe,4-Me 0 A-0776 H H H H H O H H 2-SMe,5-Me 0 A-0777 H H H H H O H H 2-SMe,6-Me 0 A-0778 H H H H H O H H 2-SEt,3-F 0 A-0779 H H H H H O H H 2-SEt,4-F 0 A-0780 H H H H H O H H 2-SEt,5-F 0 A-0781 H H H H H O H H 2-SEt,6-F 0 A-0782 H H H H H O H H 2-SEt,3-Me 0 A-0783 H H H H H O H H 2-SEt,4-Me 0 A-0784 H H H H H O H H 2-SEt,5-Me 0 A-0785 H H H H H O H H 2-SEt,6-Me 0 A-0786 H H H H H O H H 2-S(?O)Me,3-F 0 A-0787 H H H H H O H H 2-S(?O)Me,4-F 0 A-0788 H H H H H O H H 2-S(?O)Me,5-F 0 A-0789 H H H H H O H H 2-S(?O)Me,6-F 0 A-0790 H H H H H O H H 3-S(?O)Me,2-F 0 A-0791 H H H H H O H H 3-S(?O)Me,4-F 0 A-0792 H H H H H O H H 3-S(?O)Me,5-F 0 A-0793 H H H H H O H H 3-S(?O)Me,6-F 0
(116) TABLE-US-00015 TABLE 15 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-0794 H H H H H O H H 2-S(?O)Me,3-Me 0 A-0795 H H H H H O H H 2-S(?O)Me,4-Me 0 A-0796 H H H H H O H H 2-S(?O)Me,5-Me 0 A-0797 H H H H H O H H 2-S(?O)Me,6-Me 0 A-0798 H H H H H O H H 3-S(?O)Me,2-Me 0 A-0799 H H H H H O H H 3-S(?O)Me,4-Me 0 A-0800 H H H H H O H H 3-S(?O)Me,5-Me 0 A-0801 H H H H H O H H 3-S(?O)Me,6-Me 0 A-0802 H H H H H O H H 2-S(?O).sub.2Me,3-F 0 A-0803 H H H H H O H H 2-S(?O).sub.2Me,4-F 0 A-0804 H H H H H O H H 2-S(?O).sub.2Me,5-F 0 A-0805 H H H H H O H H 2-S(?O).sub.2Me,6-F 0 A-0806 H H H H H O H H 2-S(?O).sub.2Me,3-Me 0 A-0807 H H H H H O H H 2-S(?O).sub.2Me,4-Me 0 A-0808 H H H H H O H H 2-S(?O).sub.2Me,5-Me 0 A-0809 H H H H H O H H 2-S(?O).sub.2Me,6-Me 0 A-0810 H H H H H O H H 2-SCF.sub.3,3-F 0 A-0811 H H H H H O H H 2-SCF.sub.3,4-F 0 A-0812 H H H H H O H H 2-SCF.sub.3,5-F 0 A-0813 H H H H H O H H 2-SCF.sub.3,6-F 0 A-0814 H H H H H O H H 2-SCF.sub.3,3-Me 0 A-0815 H H H H H O H H 2-SCF.sub.3,4-Me 0 A-0816 H H H H H O H H 2-SCF.sub.3,5-Me 0 A-0817 H H H H H O H H 2-SCF.sub.3,6-Me 0 A-0818 H H H H H O H H 2-S(?O)CF.sub.3,3-F 0 A-0819 H H H H H O H H 2-S(?O)CF.sub.3,4-F 0 A-0820 H H H H H O H H 2-S(?O)CF.sub.3,5-F 0 A-0821 H H H H H O H H 2-S(?O)CF.sub.3,6-F 0 A-0822 H H H H H O H H 2-S(?O)CF.sub.3,3-Me 0 A-0823 H H H H H O H H 2-S(?O)CF.sub.3,4-Me 0 A-0824 H H H H H O H H 2-S(?O)CF.sub.3,5-Me 0 A-0825 H H H H H O H H 2-S(?O)CF.sub.3,6-Me 0 A-0826 H H H H H O H H 2-S(?O).sub.2CF.sub.3,3-F 0 A-0827 H H H H H O H H 2-S(?O).sub.2CF.sub.3,4-F 0 A-0828 H H H H H O H H 2-S(?O).sub.2CF.sub.3,5-F 0 A-0829 H H H H H O H H 2-S(?O).sub.2CF.sub.3,6-F 0 A-0830 H H H H H O H H 2-S(?O).sub.2CF.sub.3,3-Me 0 A-0831 H H H H H O H H 2-S(?O).sub.2CF.sub.3,4-Me 0 A-0832 H H H H H O H H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-0833 H H H H H O H H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-0834 H H H H H O H H 2-(cyclopropylthio),3-F 0 A-0835 H H H H H O H H 2-(cyclopropylthio),4-F 0 A-0836 H H H H H O H H 2-(cyclopropylthio),5-F 0 A-0837 H H H H H O H H 2-(cyclopropylthio),6-F 0 A-0838 H H H H H O H H 2-(cyclopropylthio),3-Me 0 A-0839 H H H H H O H H 2-(cyclopropylthio),4-Me 0 A-0840 H H H H H O H H 2-(cyclopropylthio),5-Me 0 A-0841 H H H H H O H H 2-(cyclopropylthio),6-Me 0 A-0842 H H H H H O H H 2-C(?O)Me,3-F 0 A-0843 H H H H H O H H 2-C(?O)Me,4-F 0 A-0844 H H H H H O H H 2-C(?O)Me,5-F 0 A-0845 H H H H H O H H 2-C(?O)Me,6-F 0 A-0846 H H H H H O H H 2-C(?O)Me,3-Me 0 A-0847 H H H H H O H H 2-C(?O)Me,4-Me 0 A-0848 H H H H H O H H 2-C(?O)Me,5-Me 0 A-0849 H H H H H O H H 2-C(?O)Me,6-Me 0 A-0850 H H H H H O H H 3-C(?O)Me,2-F 0
(117) TABLE-US-00016 TABLE 16 com- pound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-0851 H H H H H O H H 3-C(?O)Me,4-F 0 A-0852 H H H H H O H H 3-C(?O)Me,5-F 0 A-0853 H H H H H O H H 3-C(?O)Me,6-F 0 A-0854 H H H H H O H H 3-C(?O)Me,2-Me 0 A-0855 H H H H H O H H 3-C(?O)Me,4-Me 0 A-0856 H H H H H O H H 3-C(?O)Me,5-Me 0 A-0857 H H H H H O H H 3-C(?O)Me,6-Me 0 A-0858 H H H H H O H H 2-C(?O)OMe,3-F 0 A-0859 H H H H H O H H 2-C(?O)OMe,4-F 0 A-0860 H H H H H O H H 2-C(?O)OMe,5-F 0 A-0861 H H H H H O H H 2-C(?O)OMe,6-F 0 A-0862 H H H H H O H H 2-C(?O)OMe,3-Me 0 A-0863 H H H H H O H H 2-C(?O)OMe,4-Me 0 A-0864 H H H H H O H H 2-C(?O)OMe,4-Me 0 A-0865 H H H H H O H H 2-C(?O)OMe,6-Me 0 A-0866 H H H H H O H H 2-C(?O)OET,3-F 0 A-0867 H H H H H O H H 2-C(?O)OET,4-F 0 A-0868 H H H H H O H H 2-C(?O)OET,5-F 0 A-0869 H H H H H O H H 2-C(?O)OET,6-F 0 A-0870 H H H H H O H H 2-C(?O)OET,3-Me 0 A-0871 H H H H H O H H 2-C(?O)OET,4-Me 0 A-0872 H H H H H O H H 2-C(?O)OET,5-Me 0 A-0873 H H H H H O H H 2-C(?O)OET,6-Me 0 A-0874 H H H H H O H H 2-C(?O)NH.sub.2,3-F 0 A-0875 H H H H H O H H 2-C(?O)NH.sub.2,4-F 0 A-0876 H H H H H O H H 2-C(?O)NH.sub.2,5-F 0 A-0877 H H H H H O H H 2-C(?O)NH.sub.2,6-F 0 A-0878 H H H H H O H H 2-C(?O)NH.sub.2,3-Me 0 A-0879 H H H H H O H H 2-C(?O)NH.sub.2,4-Me 0 A-0880 H H H H H O H H 2-C(?O)NH.sub.2,5-Me 0 A-0881 H H H H H O H H 2-C(?O)NH.sub.2,6-Me 0 A-0882 H H H H H O H H 2-C(?O)NHMe,3-F 0 A-0883 H H H H H O H H 2-C(?O)NHMe,4-F 0 A-0884 H H H H H O H H 2-C(?O)NHMe,5-F 0 A-0885 H H H H H O H H 2-C(?O)NHMe,6-F 0 A-0886 H H H H H O H H 2-C(?O)NHMe,3-Me 0 A-0887 H H H H H O H H 2-C(?O)NHMe,4-Me 0 A-0888 H H H H H O H H 2-C(?O)NHMe,5-Me 0 A-0889 H H H H H O H H 2-C(?O)NHMe,6-Me 0 A-0890 H H H H H O H H 2-C(?O)NMe.sub.2,3-F 0 A-0891 H H H H H O H H 2-C(?O)NMe.sub.2,4-F 0 A-0892 H H H H H O H H 2-C(?O)NMe.sub.2,5-F 0 A-0893 H H H H H O H H 2-C(?O)NMe.sub.2,6-F 0 A-0894 H H H H H O H H 2-C(?O)NMe.sub.2,3-Me 0 A-0895 H H H H H O H H 2-C(?O)NMe.sub.2,4-Me 0 A-0896 H H H H H O H H 2-C(?O)NMe.sub.2,5-Me 0 A-0897 H H H H H O H H 2-C(?O)NMe.sub.2,6-Me 0 A-0898 H H H H H O H H 2-CH.sub.2OH,3-F 0 A-0899 H H H H H O H H 2-CH.sub.2OH,4-F 0 A-0900 H H H H H O H H 2-CH.sub.2OH,5-F 0 A-0901 H H H H H O H H 2-CH.sub.2OH,6-F 0 A-0902 H H H H H O H H 2-CH.sub.2OH,3-Me 0 A-0903 H H H H H O H H 2-CH.sub.2OH,4-Me 0 A-0904 H H H H H O H H 2-CH.sub.2OH,5-Me 0 A-0905 H H H H H O H H 2-CH.sub.2OH,6-Me 0 A-0906 H H H H H O H H 2-CH.sub.2OCH.sub.3,3-F 0 A-0907 H H H H H O H H 2-CH.sub.2OCH.sub.3,4-F 0
(118) TABLE-US-00017 TABLE 17 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-0908 H H H H H O H H 2-CH.sub.2OCH.sub.3,5-F 0 A-0909 H H H H H O H H 2-CH.sub.2OCH.sub.3,6-F 0 A-0910 H H H H H O H H 2-CH.sub.2OCH.sub.3,3-Me 0 A-0911 H H H H H O H H 2-CH.sub.2OCH.sub.3,4-Me 0 A-0912 H H H H H O H H 2-CH.sub.2OCH.sub.3,5-Me 0 A-0913 H H H H H O H H 2-CH.sub.2OCH.sub.3,6-Me 0 A-0914 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,3-F 0 A-0915 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,4-F 0 A-0916 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,5-F 0 A-0917 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-F 0 A-0918 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,3-Me 0 A-0919 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,4-Me 0 A-0920 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,5-Me 0 A-0921 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Me 0 A-0922 H H H H H O H H 2-OC(?O)CH.sub.3,3-F 0 A-0923 H H H H H O H H 2-OC(?O)CH.sub.3,4-F 0 A-0924 H H H H H O H H 2-OC(?O)CH.sub.3,5-F 0 A-0925 H H H H H O H H 2-OC(?O)CH.sub.3,6-F 0 A-0926 H H H H H O H H 2-OC(?O)CH.sub.3,3-Me 0 A-0927 H H H H H O H H 2-OC(?O)CH.sub.3,4-Me 0 A-0928 H H H H H O H H 2-OC(?O)CH.sub.3,5-Me 0 A-0929 H H H H H O H H 2-OC(?O)CH.sub.3,6-Me 0 A-0930 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,3-F 0 A-0931 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,4-F 0 A-0932 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-0933 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-0934 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,3-Me 0 A-0935 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,4-Me 0 A-0936 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-0937 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-0938 H H H H H O H H 2-CH.sub.2SCH.sub.3,3-F 0 A-0939 H H H H H O H H 2-CH.sub.2SCH.sub.3,4-F 0 A-0940 H H H H H O H H 2-CH.sub.2SCH.sub.3,5-F 0 A-0941 H H H H H O H H 2-CH.sub.2SCH.sub.3,6-F 0 A-0942 H H H H H O H H 2-CH.sub.2SCH.sub.3,3-Me 0 A-0943 H H H H H O H H 2-CH.sub.2SCH.sub.3,4-Me 0 A-0944 H H H H H O H H 2-CH.sub.2SCH.sub.3,5-Me 0 A-0945 H H H H H O H H 2-CH.sub.2SCH.sub.3,6-Me 0 A-0946 H H H H H O H H 2-CH.sub.2SCF.sub.3,3-F 0 A-0947 H H H H H O H H 2-CH.sub.2SCF.sub.3,4-F 0 A-0948 H H H H H O H H 2-CH.sub.2SCF.sub.3,5-F 0 A-0949 H H H H H O H H 2-CH.sub.2SCF.sub.3,6-F 0 A-0950 H H H H H O H H 2-CH.sub.2SCF.sub.3,3-Me 0 A-0951 H H H H H O H H 2-CH.sub.2SCF.sub.3,4-Me 0 A-0952 H H H H H O H H 2-CH.sub.2SCF.sub.3,5-Me 0 A-0953 H H H H H O H H 2-CH.sub.2SCF.sub.3,6-Me 0 A-0954 H H H H H O H H 2-(benzyloxy),3-F 0 A-0955 H H H H H O H H 2-(benzyloxy),4-F 0 A-0956 H H H H H O H H 2-(benzyloxy),5-F 0 A-0957 H H H H H O H H 2-(benzyloxy),6-F 0 A-0958 H H H H H O H H 2-(benzyloxy),3-Me 0 A-0959 H H H H H O H H 2-(benzyloxy),4-Me 0 A-0960 H H H H H O H H 2-(benzyloxy),5-Me 0 A-0961 H H H H H O H H 2-(benzyloxy),6-Me 0 A-0962 H H H H H O H H 2-NH.sub.2,3-F 0 A-0963 H H H H H O H H 2-NH.sub.2,4-F 0 A-0964 H H H H H O H H 2-NH.sub.2,5-F 0
(119) TABLE-US-00018 TABLE 18 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-0965 H H H H H O H H 2-NH.sub.2,6-F 0 A-0966 H H H H H O H H 2-NH.sub.2,3-Me 0 A-0967 H H H H H O H H 2-NH.sub.2,4-Me 0 A-0968 H H H H H O H H 2-NH.sub.2,5-Me 0 A-0969 H H H H H O H H 2-NH.sub.2,6-Me 0 A-0970 H H H H H O H H 2-NHMe,3-F 0 A-0971 H H H H H O H H 2-NHMe,4-F 0 A-0972 H H H H H O H H 2-NHMe,5-F 0 A-0973 H H H H H O H H 2-NHMe,6-F 0 A-0974 H H H H H O H H 2-NHMe,3-Me 0 A-0975 H H H H H O H H 2-NHMe,4-Me 0 A-0976 H H H H H O H H 2-NHMe,5-Me 0 A-0977 H H H H H O H H 2-NHMe,6-Me 0 A-0978 H H H H H O H H 2-NHEt,3-F 0 A-0979 H H H H H O H H 2-NHEt,4-F 0 A-0980 H H H H H O H H 2-NHEt,5-F 0 A-0981 H H H H H O H H 2-NHEt,6-F 0 A-0982 H H H H H O H H 2-NHEt,3-Me 0 A-0983 H H H H H O H H 2-NHEt,4-Me 0 A-0984 H H H H H O H H 2-NHEt,5-Me 0 A-0985 H H H H H O H H 2-NHEt,6-Me 0 A-0986 H H H H H O H H 2-NMe.sub.2,3-F 0 A-0987 H H H H H O H H 2-NMe.sub.2,4-F 0 A-0988 H H H H H O H H 2-NMe.sub.2,5-F 0 A-0989 H H H H H O H H 2-NMe.sub.2,6-F 0 A-0990 H H H H H O H H 2-NMe.sub.2,3-Me 0 A-0991 H H H H H O H H 2-NMe.sub.2,4-Me 0 A-0992 H H H H H O H H 2-NMe.sub.2,5-Me 0 A-0993 H H H H H O H H 2-NMe.sub.2,6-Me 0 A-0994 H H H H H O H H 2-NEt.sub.2,3-F 0 A-0995 H H H H H O H H 2-NEt.sub.2,4-F 0 A-0996 H H H H H O H H 2-NEt.sub.2,5-F 0 A-0997 H H H H H O H H 2-NEt.sub.2,6-F 0 A-0998 H H H H H O H H 2-NEt.sub.2,3-Me 0 A-0999 H H H H H O H H 2-NEt.sub.2,4-Me 0 A-1000 H H H H H O H H 2-NEt.sub.2,5-Me 0 A-1001 H H H H H O H H 2-NEt.sub.2,6-Me 0 A-1002 H H H H H O H H 2-CHO,3-F 0 A-1003 H H H H H O H H 2-CHO,4-F 0 A-1004 H H H H H O H H 2-CHO,5-F 0 A-1005 H H H H H O H H 2-CHO,6-F 0 A-1006 H H H H H O H H 2-CHO,3-Me 0 A-1007 H H H H H O H H 2-CHO,4-Me 0 A-1008 H H H H H O H H 2-CHO,5-Me 0 A-1009 H H H H H O H H 2-CHO,6-Me 0 A-1010 H H H H H O H H 2-C(?O)OH,3-F 0 A-1011 H H H H H O H H 2-C(?O)OH,4-F 0 A-1012 H H H H H O H H 2-C(?O)OH,5-F 0 A-1013 H H H H H O H H 2-C(?O)OH,6-F 0 A-1014 H H H H H O H H 2-C(?O)OH,3-Me 0 A-1015 H H H H H O H H 2-C(?O)OH,4-Me 0 A-1016 H H H H H O H H 2-C(?O)OH,5-Me 0 A-1017 H H H H H O H H 2-C(?O)OH,6-Me 0 A-1018 H H H H H O H H 2-(1,3-dioxolan-2-yl),3-F 0 A-1019 H H H H H O H H 2-(1,3-dioxolan-2-yl),4-F 0 A-1020 H H H H H O H H 2-(1,3-dioxolan-2-yl),5-F 0 A-1021 H H H H H O H H 2-(1,3-dioxolan-2-yl),6-F 0
(120) TABLE-US-00019 TABLE 19 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1022 H H H H H O H H 2-(1,3-dioxolan-2-yl),3-Me 0 A-1023 H H H H H O H H 2-(1,3-dioxolan-2-yl),4-Me 0 A-1024 H H H H H O H H 2-(1,3-dioxolan-2-yl),5-Me 0 A-1025 H H H H H O H H 2-(1,3-dioxolan-2-yl),6-Me 0 A-1026 H H H H H O H H 2-(1,3-dioxan-2-yl),3-F 0 A-1027 H H H H H O H H 2-(1,3-dioxan-2-yl),4-F 0 A-1028 H H H H H O H H 2-(1,3-dioxan-2-yl),5-F 0 A-1029 H H H H H O H H 2-(1,3-dioxan-2-yl),6-F 0 A-1030 H H H H H O H H 2-(1,3-dioxan-2-yl),3-Me 0 A-1031 H H H H H O H H 2-(1,3-dioxan-2-yl),4-Me 0 A-1032 H H H H H O H H 2-(1,3-dioxan-2-yl),5-Me 0 A-1033 H H H H H O H H 2-(1,3-dioxan-2-yl),6-Me 0 A-1034 H H H H H O H H 2-(thiazol-2-yl),3-F 0 A-1035 H H H H H O H H 2-(thiazol-2-yl),4-F 0 A-1036 H H H H H O H H 2-(thiazol-2-yl),5-F 0 A-1037 H H H H H O H H 2-(thiazol-2-yl),6-F 0 A-1038 H H H H H O H H 2-(thiazol-2-yl),3-Me 0 A-1039 H H H H H O H H 2-(thiazol-2-yl),4-Me 0 A-1040 H H H H H O H H 2-(thiazol-2-yl),5-Me 0 A-1041 H H H H H O H H 2-(thiazol-2-yl),6-Me 0 A-1042 H H H H H O H H 2-(oxazol-2-yl),3-F 0 A-1043 H H H H H O H H 2-(oxazol-2-yl),4-F 0 A-1044 H H H H H O H H 2-(oxazol-2-yl),5-F 0 A-1045 H H H H H O H H 2-(oxazol-2-yl),6-F 0 A-1046 H H H H H O H H 2-(oxazol-2-yl),3-Me 0 A-1047 H H H H H O H H 2-(oxazol-2-yl),4-Me 0 A-1048 H H H H H O H H 2-(oxazol-2-yl),5-Me 0 A-1049 H H H H H O H H 2-(oxazol-2-yl),6-Me 0 A-1050 H H H H H O H H 2-CH?NOH,3-F 0 A-1051 H H H H H O H H 2-CH?NOH,4-F 0 A-1052 H H H H H O H H 2-CH?NOH,5-F 0 A-1053 H H H H H O H H 2-CH?NOH,6-F 0 A-1054 H H H H H O H H 2-CH?NOH,3-Me 0 A-1055 H H H H H O H H 2-CH?NOH,4-Me 0 A-1056 H H H H H O H H 2-CH?NOH,5-Me 0 A-1057 H H H H H O H H 2-CH?NOH,6-Me 0 A-1058 H H H H H O H H 2-CH?NOMe,3-F 0 A-1059 H H H H H O H H 2-CH?NOMe,4-F 0 A-1060 H H H H H O H H 2-CH?NOMe,5-F 0 A-1061 H H H H H O H H 2-CH?NOMe,6-F 0 A-1062 H H H H H O H H 2-CH?NOMe,3-Me 0 A-1063 H H H H H O H H 2-CH?NOMe,4-Me 0 A-1064 H H H H H O H H 2-CH?NOMe,5-Me 0 A-1065 H H H H H O H H 2-CH?NOMe,6-Me 0 A-1066 H H H H H O H H 2-CN,3-F 0 A-1067 H H H H H O H H 2-CN,4-F 0 A-1068 H H H H H O H H 2-CN,5-F 0 A-1069 H H H H H O H H 2-CN,6-F 0 A-1070 H H H H H O H H 2-CN,3-Cl 0 A-1071 H H H H H O H H 2-CN,4-Cl 0 A-1072 H H H H H O H H 2-CN,5-Cl 0 A-1073 H H H H H O H H 2-CN,6-Cl 0 A-1074 H H H H H O H H 2-CN,3-Me 0 A-1075 H H H H H O H H 2-CN,4-Me 0 A-1076 H H H H H O H H 2-CN,5-Me 0 A-1077 H H H H H O H H 2-CN,6-Me 0 A-1078 H H H H H O H H 2-CN,3-OMe 0
(121) TABLE-US-00020 TABLE 20 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1079 H H H H H O H H 2-CN,4-OMe 0 A-1080 H H H H H O H H 2-CN,5-OMe 0 A-1081 H H H H H O H H 2-CN,6-OMe 0 A-1082 H H H H H O H H 3-CN,2-F 0 A-1083 H H H H H O H H 3-CN,4-F 0 A-1084 H H H H H O H H 3-CN,5-F 0 A-1085 H H H H H O H H 3-CN,6-F 0 A-1086 H H H H H O H H 3-CN,2-Cl 0 A-1087 H H H H H O H H 3-CN,4-Cl 0 A-1088 H H H H H O H H 3-CN,5-Cl 0 A-1089 H H H H H O H H 3-CN,6-Cl 0 A-1090 H H H H H O H H 3-CN,2-Me 0 A-1091 H H H H H O H H 3-CN,4-Me 0 A-1092 H H H H H O H H 3-CN,5-Me 0 A-1093 H H H H H O H H 3-CN,6-Me 0 A-1094 H H H H H O H H 3-CN,2-OMe 0 A-1095 H H H H H O H H 3-CN,4-OMe 0 A-1096 H H H H H O H H 3-CN,5-OMe 0 A-1097 H H H H H O H H 3-CN,6-OMe 0 A-1098 H H H H H O H H 4-CN,2-F 0 A-1099 H H H H H O H H 4-CN,3-F 0 A-1100 H H H H H O H H 4-CN,2-Cl 0 A-1101 H H H H H O H H 4-CN,3-Cl 0 A-1102 H H H H H O H H 4-CN,2-Me 0 A-1103 H H H H H O H H 4-CN,3-Me 0 A-1104 H H H H H O H H 4-CN,2-OMe 0 A-1105 H H H H H O H H 4-CN,3-OMe 0 A-1106 H H H H H O H H 2-NO.sub.2,3-F 0 A-1107 H H H H H O H H 2-NO.sub.2,4-F 0 A-1108 H H H H H O H H 2-NO.sub.2,5-F 0 A-1109 H H H H H O H H 2-NO.sub.2,6-F 0 A-1110 H H H H H O H H 2-NO.sub.2,3-Me 0 A-1111 H H H H H O H H 2-NO.sub.2,4-Me 0 A-1112 H H H H H O H H 2-NO.sub.2,5-Me 0 A-1113 H H H H H O H H 2-NO.sub.2,6-Me 0 A-1114 H H H H H O H H 2-Me,3,4-F.sub.2 0 A-1115 H H H H H O H H 2-Me,3,5-F.sub.2 0 A-1116 H H H H H O H H 2-Me,3,6-F.sub.2 0 A-1117 H H H H H O H H 2-Me,4,5-F.sub.2 0 A-1118 H H H H H O H H 2-OMe,3,4-F.sub.2 0 A-1119 H H H H H O H H 2-OMe,3,5-F.sub.2 0 A-1120 H H H H H O H H 2-OMe,3,6-F.sub.2 0 A-1121 H H H H H O H H 2-OMe,4,5-F.sub.2 0 A-1122 H H H H H O H H 2-(CH.sub.2).sub.3-3 0 A-1123 H H H H H O H H 2-(CH.sub.2).sub.4-3 0 A-1124 H H H H H O H H 2-(OCH.sub.2CH.sub.2)-3 0 A-1125 H H H H H O H H 2-(OCH.sub.2CH.sub.2CH.sub.2)-3 0 A-1126 H H H H H O H H 2-(CH.sub.2CH.sub.2O)-3 0 A-1127 H H H H H O H H 2-(CH.sub.2CH.sub.2CH.sub.2O)-3 0 A-1128 H H H H H O H H 3-(CH.sub.2).sub.3-4 0 A-1129 H H H H H O H H 3-(CH.sub.2).sub.4-4 0 A-1130 H H H H H O H H 3-(OCH.sub.2CH.sub.2)-4 0 A-1131 H H H H H O H H 3-(OCH.sub.2CH.sub.2CH.sub.2)-4 0 A-1132 H H H H H O H H 3-(CH.sub.2CH.sub.2O)-4 0 A-1133 H H H H H O H H 3-(CH.sub.2CH.sub.2CH.sub.2O)-4 0 A-1134 H H H H H O H H 2-(OCH.sub.2O)-3 0 A-1135 H H H H H O H H 3-(OCH.sub.2O)-4 0
(122) TABLE-US-00021 TABLE 21 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1136 H H H H H O H H 2-(OCH.sub.2CH.sub.2O)-3 0 A-1137 H H H H H O H H 3-(OCH.sub.2CH.sub.2O)-4 0 A-1138 H H H H H O H H 2-(OCF.sub.2O)-3 0 A-1139 H H H H H O H H 3-(OCF.sub.2O)-4 0 A-1140 H H H H H O H H 2-Me,6-Et 0 A-1141 H H H H H O H H 2-CH.sub.2OTBS 0 A-1142 H H H H H O H H 2-cyclopropyl,3-OMe 0 A-1143 H H H H H O H H 2-cyclopropyl,4-OMe 0 A-1144 H H H H H O H H 2-cyclopropyl,5-OMe 0 A-1145 H H H H H O H H 2-cyclopropyl,6-OMe 0 A-1146 H H H H H O H H 2-Me,3-OMe,6-Me 0 A-1147 H H H H H O H H 2-Me,4-OMe,6-Me 0 A-1148 H H H H H O H H 2-OMe,3-Me,6-Me 0 A-1149 H H H H H O H H 2-OMe,5-Me,6-Me 0 A-1150 H H H H H O H H 2-OMe,3-F,6-Me 0 A-1151 H H H H H O H H 2-OMe,5-F,6-Me 0 A-1152 H H H H H O H H 2-OMe,5-Me,6-F 0 A-1153 H H H H H O H H 2-Cl,3-Me,6-F 0 A-1154 H H H H H O H H 2-Cl,5-Me,6-F 0 A-1155 H H H H H O H H 2-Cl,3-OMe,6-F 0 A-1156 H H H H H O H H 2-Cl,5-OMe,6-F 0 A-1157 H H H H H O H H 2-Me,5-Et 0 A-1158 H H H H H O H H 2,6-Et.sub.2 0 A-1159 H H H H H O H H 2-Et,6-F 0 A-1160 H H H H H O H H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-1161 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-1162 H H H H H O H H 2-OMe,5-CH?NOMe 0 A-1163 H H H H H O H H 2-CH.sub.2NMe.sub.2 0 A-1164 H H H H H O H H 2-CH.sub.2OCH.sub.3,6-CF.sub.3 0 A-1165 H H H H H O H H 2-CHCl.sub.2 0 A-1166 H H H H H O H H 2-Me 0 A-1167 H H H H H O CH.sub.3 H H 0 A-1168 H H H H H O CH.sub.3 H 2-F 0 A-1169 H H H H H O CH.sub.3 H 2-Cl 0 A-1170 H H H H H O CH.sub.3 H 2-Br 0 A-1171 H H H H H O CH.sub.3 H 2-OH 0 A-1172 H H H H H O CH.sub.3 H 2-Me 0 A-1173 H H H H H O CH.sub.3 H 2-Et 0 A-1174 H H H H H O CH.sub.3 H 2-Pr 0 A-1175 H H H H H O CH.sub.3 H 2-CF.sub.3 0 A-1176 H H H H H O CH.sub.3 H 2-CHF.sub.2 0 A-1177 H H H H H O CH.sub.3 H 2-CH.sub.2F 0 A-1178 H H H H H O CH.sub.3 H 2-CF.sub.2Cl 0 A-1179 H H H H H O CH.sub.3 H 2-cyclopropyl 0 A-1180 H H H H H O CH.sub.3 H 2-cyclobutyl 0 A-1181 H H H H H O CH.sub.3 H 2-cyclopentyl 0 A-1182 H H H H H O CH.sub.3 H 2-ethenyl 0 A-1183 H H H H H O CH.sub.3 H 2-allyl 0 A-1184 H H H H H O CH.sub.3 H 2-(prop-1-en-1-yl) 0 A-1185 H H H H H O CH.sub.3 H 2-(trifluoroethenyl) 0 A-1186 H H H H H O CH.sub.3 H 2-OMe 0 A-1187 H H H H H O CH.sub.3 H 2-OEt 0 A-1188 H H H H H O CH.sub.3 H 2-OPr 0 A-1189 H H H H H O CH.sub.3 H 2-O(i-Pr) 0 A-1190 H H H H H O CH.sub.3 H 2-OCF.sub.3 0 A-1191 H H H H H O CH.sub.3 H 2-OCHF.sub.2 0 A-1192 H H H H H O CH.sub.3 H 2-(cyclopropyloxy) 0
(123) TABLE-US-00022 TABLE 22 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1193 H H H H H O CH.sub.3 H 2-(cyclobutyloxy) 0 A-1194 H H H H H O CH.sub.3 H 2-(cyclopentyloxy) 0 A-1195 H H H H H O CH.sub.3 H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-1196 H H H H H O CH.sub.3 H 2-(oxiran-2-yl) 0 A-1197 H H H H H O CH.sub.3 H 2-SMe 0 A-1198 H H H H H O CH.sub.3 H 3-SMe 0 A-1199 H H H H H O CH.sub.3 H 2-S(?O)Me 0 A-1200 H H H H H O CH.sub.3 H 3-S(?O)Me 0 A-1201 H H H H H O CH.sub.3 H 2-S(?O).sub.2Me 0 A-1202 H H H H H O CH.sub.3 H 3-S(?O).sub.2Me 0 A-1203 H H H H H O CH.sub.3 H 2-SCF.sub.3 0 A-1204 H H H H H O CH.sub.3 H 3-SCF.sub.3 0 A-1205 H H H H H O CH.sub.3 H 3-S(O)CF.sub.3 0 A-1206 H H H H H O CH.sub.3 H 3-SCF(CF.sub.3).sub.2 0 A-1207 H H H H H O CH.sub.3 H 2-(cyclopropylthio) 0 A-1208 H H H H H O CH.sub.3 H 2-(cyclopropylsulfinyl) 0 A-1209 H H H H H O CH.sub.3 H 2-(cyclopropylsulfonyl) 0 A-1210 H H H H H O CH.sub.3 H 2-C(?O)Me 0 A-1211 H H H H H O CH.sub.3 H 2-CH.sub.2C(?O)CH.sub.3 0 A-1212 H H H H H O CH.sub.3 H 2-CH.sub.2C(?O)CF.sub.3 0 A-1213 H H H H H O CH.sub.3 H 2-CH.sub.2OH 0 A-1214 H H H H H O CH.sub.3 H 2-CH.sub.2OCH.sub.3 0 A-1215 H H H H H O CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-1216 H H H H H O CH.sub.3 H 2-CH.sub.2SCH.sub.3 0 A-1217 H H H H H O CH.sub.3 H 2-CH.sub.2S(?O)CH.sub.3 0 A-1218 H H H H H O CH.sub.3 H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-1219 H H H H H O CH.sub.3 H 2-(benzyloxy) 0 A-1220 H H H H H O CH.sub.3 H 2-NH.sub.2 0 A-1221 H H H H H O CH.sub.3 H 2-NHMe 0 A-1222 H H H H H O CH.sub.3 H 2-N(Me).sub.2 0 A-1223 H H H H H O CH.sub.3 H 2-(1,3-dioxolan-2-yl) 0 A-1224 H H H H H O CH.sub.3 H 2-(1,3-dioxan-2-yl) 0 A-1225 H H H H H O CH.sub.3 H 2-(1H-imidazol-2-yl) 0 A-1226 H H H H H O CH.sub.3 H 2-(thiazol-2-yl) 0 A-1227 H H H H H O CH.sub.3 H 2-(oxazol-2-yl) 0 A-1228 H H H H H O CH.sub.3 H 2-CH?NOH 0 A-1229 H H H H H O CH.sub.3 H 2-CH?NOMe 0 A-1230 H H H H H O CH.sub.3 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-1231 H H H H H O CH.sub.3 H 2-CN 0 A-1232 H H H H H O CH.sub.3 H 2-NO2 0 A-1233 H H H H H O CH.sub.3 H 2-F,6-Cl 0 A-1234 H H H H H O CH.sub.3 H 2-F,6-Me 0 A-1235 H H H H H O CH.sub.3 H 3-F,6-Me 0 A-1236 H H H H H O CH.sub.3 H 4-F,2-Me 0 A-1237 H H H H H O CH.sub.3 H 2-F,6-OMe 0 A-1238 H H H H H O CH.sub.3 H 3-F,6-OMe 0 A-1239 H H H H H O CH.sub.3 H 2,6-Cl.sub.2 0 A-1240 H H H H H O CH.sub.3 H 2-Cl,6-Me 0 A-1241 H H H H H O CH.sub.3 H 3-Cl,6-Me 0 A-1242 H H H H H O CH.sub.3 H 4-Cl,2-Me 0 A-1243 H H H H H O CH.sub.3 H 2-Cl,5-CF.sub.3 0 A-1244 H H H H H O CH.sub.3 H 2-Cl,6-CF.sub.3 0 A-1245 H H H H H O CH.sub.3 H 2-Cl,6-OMe 0 A-1246 H H H H H O CH.sub.3 H 3-Cl,6-OMe 0 A-1247 H H H H H O CH.sub.3 H 4-Cl,2-OMe 0 A-1248 H H H H H O CH.sub.3 H 2,4-Me.sub.2 0 A-1249 H H H H H O CH.sub.3 H 2,5-Me.sub.2 0
(124) TABLE-US-00023 TABLE 23 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1250 H H H H H O CH.sub.3 H 2,6-Me2 0 A-1251 H H H H H O CH.sub.3 H 2-Me,4-CF.sub.3 0 A-1252 H H H H H O CH.sub.3 H 2-Me,5-CF.sub.3 0 A-1253 H H H H H O CH.sub.3 H 2-Me,6-CF.sub.3 0 A-1254 H H H H H O CH.sub.3 H 2-Me,4-OMe 0 A-1255 H H H H H O CH.sub.3 H 2-Me,5-OMe 0 A-1256 H H H H H O CH.sub.3 H 2-Me,6-OMe 0 A-1257 H H H H H O CH.sub.3 H 3-Me,6-OMe 0 A-1258 H H H H H O CH.sub.3 H 4-Me,2-OMe 0 A-1259 H H H H H O CH.sub.3 H 2,5-OMe.sub.2 0 A-1260 H H H H H O CH.sub.3 H 2,6-OMe.sub.2 0 A-1261 H H H H H O CH.sub.3 H 2-OMe,6-CF.sub.3 0 A-1262 H H H H H O CH.sub.3 H 2-CHF.sub.2,5-F 0 A-1263 H H H H H O CH.sub.3 H 2-CHF.sub.2,6-F 0 A-1264 H H H H H O CH.sub.3 H 2-CHF.sub.2,5-Me 0 A-1265 H H H H H O CH.sub.3 H 2-CHF.sub.2,6-Me 0 A-1266 H H H H H O CH.sub.3 H 2-cyclopropyl,5-F 0 A-1267 H H H H H O CH.sub.3 H 2-cyclopropyl,6-F 0 A-1268 H H H H H O CH.sub.3 H 2-cyclopropyl,5-Me 0 A-1269 H H H H H O CH.sub.3 H 2-cyclopropyl,6-Me 0 A-1270 H H H H H O CH.sub.3 H 2-ethenyl,6-F 0 A-1271 H H H H H O CH.sub.3 H 2-ethenyl,6-Me 0 A-1272 H H H H H O CH.sub.3 H 2-OEt,5-F 0 A-1273 H H H H H O CH.sub.3 H 2-OEt,6-F 0 A-1274 H H H H H O CH.sub.3 H 2-OEt,5-Cl 0 A-1275 H H H H H O CH.sub.3 H 2-OEt,6-Cl 0 A-1276 H H H H H O CH.sub.3 H 2-OEt,5-Me 0 A-1277 H H H H H O CH.sub.3 H 2-OEt,6-Me 0 A-1278 H H H H H O CH.sub.3 H 2-OCHF.sub.2,5-F 0 A-1279 H H H H H O CH.sub.3 H 2-OCHF.sub.2,6-F 0 A-1280 H H H H H O CH.sub.3 H 2-OCHF.sub.2,5-Me 0 A-1281 H H H H H O CH.sub.3 H 2-OCHF.sub.2,6-Me 0 A-1282 H H H H H O CH.sub.3 H 2-(cyclopropyloxy),5-F 0 A-1283 H H H H H O CH.sub.3 H 2-(cyclopropyloxy),6-F 0 A-1284 H H H H H O CH.sub.3 H 2-(cyclopropyloxy),5-Me 0 A-1285 H H H H H O CH.sub.3 H 2-(cyclopropyloxy),6-Me 0 A-1286 H H H H H O CH.sub.3 H 2-SMe,5-F 0 A-1287 H H H H H O CH.sub.3 H 2-SMe,6-F 0 A-1288 H H H H H O CH.sub.3 H 2-SMe,5-Me 0 A-1289 H H H H H O CH.sub.3 H 2-SMe,6-Me 0 A-1290 H H H H H O CH.sub.3 H 2-S(?O)Me,5-F 0 A-1291 H H H H H O CH.sub.3 H 2-S(?O)Me,6-F 0 A-1292 H H H H H O CH.sub.3 H 2-S(?O)Me,5-Me 0 A-1293 H H H H H O CH.sub.3 H 2-S(?O)Me,6-Me 0 A-1294 H H H H H O CH.sub.3 H 2-S(?O).sub.2Me,5-F 0 A-1295 H H H H H O CH.sub.3 H 2-S(?O).sub.2Me,6-F 0 A-1296 H H H H H O CH.sub.3 H 2-S(?O).sub.2Me,5-Me 0 A-1297 H H H H H O CH.sub.3 H 2-S(?O).sub.2Me,6-Me 0 A-1298 H H H H H O CH.sub.3 H 2-SCF.sub.3,5-F 0 A-1299 H H H H H O CH.sub.3 H 2-SCF.sub.3,6-F 0 A-1300 H H H H H O CH.sub.3 H 2-SCF.sub.3,5-Me 0 A-1301 H H H H H O CH.sub.3 H 2-SCF.sub.3,6-Me 0 A-1302 H H H H H O CH.sub.3 H 2-S(?O)CF.sub.3,5-F 0 A-1303 H H H H H O CH.sub.3 H 2-S(?O)CF.sub.3,6-F 0 A-1304 H H H H H O CH.sub.3 H 2-S(?O)CF.sub.3,5-Me 0 A-1305 H H H H H O CH.sub.3 H 2-S(?O)CF.sub.3,6-Me 0 A-1306 H H H H H O CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-F 0
(125) TABLE-US-00024 TABLE 24 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1307 H H H H H O CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-1308 H H H H H O CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-1309 H H H H H O CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-1310 H H H H H O CH.sub.3 H 2-(cyclopropylthio),5-F 0 A-1311 H H H H H O CH.sub.3 H 2-(cyclopropylthio),6-F 0 A-1312 H H H H H O CH.sub.3 H 2-(cyclopropylthio),5-Me 0 A-1313 H H H H H O CH.sub.3 H 2-(cyclopropylthio),6-Me 0 A-1314 H H H H H O CH.sub.3 H 2-C(?O)Me,5-F 0 A-1315 H H H H H O CH.sub.3 H 2-C(?O)Me,6-F 0 A-1316 H H H H H O CH.sub.3 H 2-C(?O)Me,5-Me 0 A-1317 H H H H H O CH.sub.3 H 2-C(?O)Me,6-Me 0 A-1318 H H H H H O CH.sub.3 H 2-CH.sub.2OH,5-F 0 A-1319 H H H H H O CH.sub.3 H 2-CH.sub.2OH,6-F 0 A-1320 H H H H H O CH.sub.3 H 2-CH.sub.2OH,5-Me 0 A-1321 H H H H H O CH.sub.3 H 2-CH.sub.2OH,6-Me 0 A-1322 H H H H H O CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-F 0 A-1323 H H H H H O CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-F 0 A-1324 H H H H H O CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-F 0 A-1325 H H H H H O CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-1326 H H H H H O CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-1327 H H H H H O CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-1328 H H H H H O CH.sub.3 H 2-OC(?O)CH.sub.3,5-F 0 A-1329 H H H H H O CH.sub.3 H 2-OC(?O)CH.sub.3,6-F 0 A-1330 H H H H H O CH.sub.3 H 2-OC(?O)CH.sub.3,5-Me 0 A-1331 H H H H H O CH.sub.3 H 2-OC(?O)CH.sub.3,6-Me 0 A-1332 H H H H H O CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-1333 H H H H H O CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-1334 H H H H H O CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-1335 H H H H H O CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-1336 H H H H H O CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-F 0 A-1337 H H H H H O CH.sub.3 H 2-CH.sub.2SCH.sub.3,6-F 0 A-1338 H H H H H O CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-Me 0 A-1339 H H H H H O CH.sub.3 H 2-CH.sub.2SCH3,6-Me 0 A-1340 H H H H H O CH.sub.3 H 2-NMe.sub.2,5-F 0 A-1341 H H H H H O CH.sub.3 H 2-NMe.sub.2,6-F 0 A-1342 H H H H H O CH.sub.3 H 2-NMe.sub.2,5-Me 0 A-1343 H H H H H O CH.sub.3 H 2-NMe.sub.2,6-Me 0 A-1344 H H H H H O CH.sub.3 H 2-CN,4-F 0 A-1345 H H H H H O CH.sub.3 H 2-CN,5-F 0 A-1346 H H H H H O CH.sub.3 H 2-CN,6-F 0 A-1347 H H H H H O CH.sub.3 H 2-CN,6-Me 0 A-1348 H H H H H O CH.sub.3 H 2-CN,5-OMe 0 A-1349 H H H H H O CH.sub.3 H 2-CN,6-OMe 0 A-1350 H H H H H O CH.sub.3 H 3-CN,6-Me 0 A-1351 H H H H H O CH.sub.3 H 3-CN,6-OMe 0 A-1352 H H H H H O CH.sub.3 H 4-CN,2-Me 0 A-1353 H H H H H O CH.sub.3 H 4-CN,2-OMe 0 A-1354 H H H H H O CH.sub.3 H 2-NO.sub.2,4-F 0 A-1355 H H H H H O CH.sub.3 H 2-NO.sub.2,5-F 0 A-1356 H H H H H O CH.sub.3 H 2-NO.sub.2,6-F 0 A-1357 H H H H H O CH.sub.3 H 2-NO.sub.2,4-Me 0 A-1358 H H H H H O CH.sub.3 H 2-NO.sub.2,5-Me 0 A-1359 H H H H H O CH.sub.3 H 2-NO.sub.2,6-Me 0 A-1360 H H H H H O CH.sub.3 H 2-Me,4,5-F.sub.2 0 A-1361 H H H H H O CH.sub.3 H 2-Me,6-Et 0 A-1362 H H H H H O CH.sub.3 H 2-cyclopropyl,6-OMe 0 A-1363 H H H H H O CH.sub.3 H 2-Me,5-Et 0
(126) TABLE-US-00025 TABLE 25 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1364 H H H H H O CH.sub.3 H 2,6-Et2 0 A-1365 H H H H H O CH.sub.3 H 2-Et,6-F 0 A-1366 H H H H H O CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-1367 H H H H H O CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3,6+-Cl 0 A-1368 H H H H H O CH.sub.3 H 2-CH.sub.2NMe.sub.2 0 A-1369 H H H H H O CH.sub.2CH.sub.3 H H 0 A-1370 H H H H H O CH.sub.2CH.sub.3 H 2-F 0 A-1371 H H H H H O CH.sub.2CH.sub.3 H 2-Cl 0 A-1372 H H H H H O CH.sub.2CH.sub.3 H 2-Br 0 A-1373 H H H H H O CH.sub.2CH.sub.3 H 2-OH 0 A-1374 H H H H H O CH.sub.2CH.sub.3 H 2-Me 0 A-1375 H H H H H O CH.sub.2CH.sub.3 H 2-Et 0 A-1376 H H H H H O CH.sub.2CH.sub.3 H 2-Pr 0 A-1377 H H H H H O CH.sub.2CH.sub.3 H 2-CF.sub.3 0 A-1378 H H H H H O CH.sub.2CH.sub.3 H 2-CHF.sub.2 0 A-1379 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2F 0 A-1380 H H H H H O CH.sub.2CH.sub.3 H 2-CF.sub.2Cl 0 A-1381 H H H H H O CH.sub.2CH.sub.3 H 2-cyclopropyl 0 A-1382 H H H H H O CH.sub.2CH.sub.3 H 2-cyclobutyl 0 A-1383 H H H H H O CH.sub.2CH.sub.3 H 2-cyclopentyl 0 A-1384 H H H H H O CH.sub.2CH.sub.3 H 2-ethenyl 0 A-1385 H H H H H O CH.sub.2CH.sub.3 H 2-allyl 0 A-1386 H H H H H O CH.sub.2CH.sub.3 H 2-(prop-1-en-1-y) 0 A-1387 H H H H H O CH.sub.2CH.sub.3 H 2-(trifluoroethenyl) 0 A-1388 H H H H H O CH.sub.2CH.sub.3 H 2-OMe 0 A-1389 H H H H H O CH.sub.2CH.sub.3 H 2-OEt 0 A-1390 H H H H H O CH.sub.2CH.sub.3 H 2-OPr 0 A-1391 H H H H H O CH.sub.2CH.sub.3 H 2-O(i-Pr) 0 A-1392 H H H H H O CH.sub.2CH.sub.3 H 2-OCF.sub.3 0 A-1393 H H H H H O CH.sub.2CH.sub.3 H 2-OCHF.sub.2 0 A-1394 H H H H H O CH.sub.2CH.sub.3 H 2-(cyclopropyloxy) 0 A-1395 H H H H H O CH.sub.2CH.sub.3 H 2-(cyclobutyloxy) 0 A-1396 H H H H H O CH.sub.2CH.sub.3 H 2-(cyclopentyloxy) 0 A-1397 H H H H H O CH.sub.2CH.sub.3 H 2-((2,2-dichl;orocyclopropyl)oxy) 0 A-1398 H H H H H O CH.sub.2CH.sub.3 H 2-(oxiran-2-yI) 0 A-1399 H H H H H O CH.sub.2CH.sub.3 H 2-SMe 0 A-1400 H H H H H O CH.sub.2CH.sub.3 H 3-SMe 0 A-1401 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O)Me 0 A-1402 H H H H H O CH.sub.2CH.sub.3 H 3-S(?O)Me 0 A-1403 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O).sub.2Me 0 A-1404 H H H H H O CH.sub.2CH.sub.3 H 3-S(?O).sub.2Me 0 A-1405 H H H H H O CH.sub.2CH.sub.3 H 2-SCF.sub.3 0 A-1406 H H H H H O CH.sub.2CH.sub.3 H 3-SCF.sub.3 0 A-1407 H H H H H O CH.sub.2CH.sub.3 H 3-S(?O)CF.sub.3 0 A-1408 H H H H H O CH.sub.2CH.sub.3 H 3-SCF(CF.sub.3).sub.2 0 A-1409 H H H H H O CH.sub.2CH.sub.3 H 2-(cyclopropylthio) 0 A-1410 H H H H H O CH.sub.2CH.sub.3 H 2-(cyclopropylsulfinyl) 0 A-1411 H H H H H O CH.sub.2CH.sub.3 H 2-(cyclopropylsulfonyl) 0 A-1412 H H H H H O CH.sub.2CH.sub.3 H 2-C(?O)Me 0 A-1413 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2C(?O)CH.sub.3 0 A-1414 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2C(?O)CF.sub.3 0 A-1415 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2OH 0 A-1416 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3 0 A-1417 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-1418 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3 0 A-1419 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2S(?O)CH.sub.3 0 A-1420 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2S(?O).sub.2CH.sub.3 0
(127) TABLE-US-00026 TABLE 26 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1421 H H H H H O CH.sub.2CH.sub.3 H 2-(benzyloxy) 0 A-1422 H H H H H O CH.sub.2CH.sub.3 H 2-NH.sub.2 0 A-1423 H H H H H O CH.sub.2CH.sub.3 H 2-NHMe 0 A-1424 H H H H H O CH.sub.2CH.sub.3 H 2-N(Me).sub.2 0 A-1425 H H H H H O CH.sub.2CH.sub.3 H 2-(1,3-dioxolan-2-yl) 0 A-1426 H H H H H O CH.sub.2CH.sub.3 H 2-(1,3-dioxan-2-yl) 0 A-1427 H H H H H O CH.sub.2CH.sub.3 H 2-(1H-imidazol-2-yl) 0 A-1428 H H H H H O CH.sub.2CH.sub.3 H 2-(thiazol-2-yl) 0 A-1429 H H H H H O CH.sub.2CH.sub.3 H 2-(oxazol-2-y) 0 A-1430 H H H H H O CH.sub.2CH.sub.3 H 2-CH?NOH 0 A-1431 H H H H H O CH.sub.2CH.sub.3 H 2-CH?NOMe 0 A-1432 H H H H H O CH.sub.2CH.sub.3 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-1433 H H H H H O CH.sub.2CH.sub.3 H 2-CN 0 A-1434 H H H H H O CH.sub.2CH.sub.3 H 2-NO.sub.2 0 A-1435 H H H H H O CH.sub.2CH.sub.3 H 2-F,6-Cl 0 A-1436 H H H H H O CH.sub.2CH.sub.3 H 2-F,6-Me 0 A-1437 H H H H H O CH.sub.2CH.sub.3 H 3-F,6-Me 0 A-1438 H H H H H O CH.sub.2CH.sub.3 H 4-F,2-Me 0 A-1439 H H H H H O CH.sub.2CH.sub.3 H 2-F,6-OMe 0 A-1440 H H H H H O CH.sub.2CH.sub.3 H 3-F,6-OMe 0 A-1441 H H H H H O CH.sub.2CH.sub.3 H 2,6-Cl.sub.2 0 A-1442 H H H H H O CH.sub.2CH.sub.3 H 2-Cl,6-Me 0 A-1443 H H H H H O CH.sub.2CH.sub.3 H 3-Cl,6-Me 0 A-1444 H H H H H O CH.sub.2CH.sub.3 H 4-Cl,2-Me 0 A-1445 H H H H H O CH.sub.2CH.sub.3 H 2-Cl,5-CF.sub.3 0 A-1446 H H H H H O CH.sub.2CH.sub.3 H 2-Cl,6-CF.sub.3 0 A-1447 H H H H H O CH.sub.2CH.sub.3 H 2-Cl,6-OMe 0 A-1448 H H H H H O CH.sub.2CH.sub.3 H 3-Cl,6-OMe 0 A-1449 H H H H H O CH.sub.2CH.sub.3 H 4-Cl,2-OMe 0 A-1450 H H H H H O CH.sub.2CH.sub.3 H 2,4-Me.sub.2 0 A-1451 H H H H H O CH.sub.2CH.sub.3 H 2,5-Me.sub.2 0 A-1452 H H H H H O CH.sub.2CH.sub.3 H 2,6-Me.sub.2 0 A-1453 H H H H H O CH.sub.2CH.sub.3 H 2-Me,4-CF.sub.3 0 A-1454 H H H H H O CH.sub.2CH.sub.3 H 2-Me,5-CF.sub.3 0 A-1455 H H H H H O CH.sub.2CH.sub.3 H 2-Me,6-CF.sub.3 0 A-1456 H H H H H O CH.sub.2CH.sub.3 H 2-Me,4-OMe 0 A-1457 H H H H H O CH.sub.2CH.sub.3 H 2-Me,5-OMe 0 A-1458 H H H H H O CH.sub.2CH.sub.3 H 2-Me,6-OMe 0 A-1459 H H H H H O CH.sub.2CH.sub.3 H 3-Me,6-OMe 0 A-1460 H H H H H O CH.sub.2CH.sub.3 H 4-Me,2-OMe 0 A-1461 H H H H H O CH.sub.2CH.sub.3 H 2,5-OMe.sub.2 0 A-1462 H H H H H O CH.sub.2CH.sub.3 H 2,6-OMe.sub.2 0 A-1463 H H H H H O CH.sub.2CH.sub.3 H 2-OMe,6-CF.sub.3 0 A-1464 H H H H H O CH.sub.2CH.sub.3 H 2-CHF.sub.2,5-F 0 A-1465 H H H H H O CH.sub.2CH.sub.3 H 2-CHF.sub.2,6-F 0 A-1466 H H H H H O CH.sub.2CH.sub.3 H 2-CHF.sub.2,5-Me 0 A-1467 H H H H H O CH.sub.2CH.sub.3 H 2-CHF.sub.2,6-Me 0 A-1468 H H H H H O CH.sub.2CH.sub.3 H 2-cyclopropyl,5-F 0 A-1469 H H H H H O CH.sub.2CH.sub.3 H 2-cyclopropyl,6-F 0 A-1470 H H H H H O CH.sub.2CH.sub.3 H 2-cyclopropyl,5-Me 0 A-1471 H H H H H O CH.sub.2CH.sub.3 H 2-cyclopropyl,6-Me 0 A-1472 H H H H H O CH.sub.2CH.sub.3 H 2-ethenyl,6-F 0 A-1473 H H H H H O CH.sub.2CH.sub.3 H 2-ethenyl,6-Me 0 A-1474 H H H H H O CH.sub.2CH.sub.3 H 2-OEt,5-F 0 A-1475 H H H H H O CH.sub.2CH.sub.3 H 2-OEt,6-F 0 A-1476 H H H H H O CH.sub.2CH.sub.3 H 2-OEt,5-Cl 0 A-1477 H H H H H O CH.sub.2CH.sub.3 H 2-OEt,6-Cl 0
(128) TABLE-US-00027 TABLE 27 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1478 H H H H H O CH.sub.2CH.sub.3 H 2-OEt,5-Me 0 A-1479 H H H H H O CH.sub.2CH.sub.3 H 2-OEt,6-Me 0 A-1480 H H H H H O CH.sub.2CH.sub.3 H 2-OCHF.sub.2,5-F 0 A-1481 H H H H H O CH.sub.2CH.sub.3 H 2-OCHF.sub.2,6-F 0 A-1482 H H H H H O CH.sub.2CH.sub.3 H 2-OCHF.sub.2,5-Me 0 A-1483 H H H H H O CH.sub.2CH.sub.3 H 2-OCHF.sub.2,6-Me 0 A-1484 H H H H H O CH.sub.2CH.sub.3 H 2-(cyclopropyloxy),5-F 0 A-1485 H H H H H O CH.sub.2CH.sub.3 H 2-(cyclopropyloxy),6-F 0 A-1486 H H H H H O CH.sub.2CH.sub.3 H 2-(cyclopropyloxy),5-Me 0 A-1487 H H H H H O CH.sub.2CH.sub.3 H 2-(cyclopropyloxy),6-Me 0 A-1488 H H H H H O CH.sub.2CH.sub.3 H 2-SMe,5-F 0 A-1489 H H H H H O CH.sub.2CH.sub.3 H 2-SMe,6-F 0 A-1490 H H H H H O CH.sub.2CH.sub.3 H 2-SMe,5-Me 0 A-1491 H H H H H O CH.sub.2CH.sub.3 H 2-SMe,6-Me 0 A-1492 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O)Me,5-F 0 A-1493 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O)Me,6-F 0 A-1494 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O)Me,5-Me 0 A-1495 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O)Me,6-Me 0 A-1496 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,5-F 0 A-1497 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,6-F 0 A-1498 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,5-Me 0 A-1499 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,6-Me 0 A-1500 H H H H H O CH.sub.2CH.sub.3 H 2-SCF.sub.3,5-F 0 A-1501 H H H H H O CH.sub.2CH.sub.3 H 2-SCF.sub.3,6-F 0 A-1502 H H H H H O CH.sub.2CH.sub.3 H 2-SCF.sub.3,5-Me 0 A-1503 H H H H H O CH.sub.2CH.sub.3 H 2-SCF.sub.3,6-Me 0 A-1504 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,5-F 0 A-1505 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,6-F 0 A-1506 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,5-Me 0 A-1507 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,6-Me 0 A-1508 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-1509 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-1510 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-1511 H H H H H O CH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-1512 H H H H H O CH.sub.2CH.sub.3 H 2-(cyclopropylthio),5-F 0 A-1513 H H H H H O CH.sub.2CH.sub.3 H 2-(cyclopropylthio),6-F 0 A-1514 H H H H H O CH.sub.2CH.sub.3 H 2-(cyclopropylthio),5-Me 0 A-1515 H H H H H O CH.sub.2CH.sub.3 H 2-(cyclopropylthio),6-Me 0 A-1516 H H H H H O CH.sub.2CH.sub.3 H 2-C(?O)Me,5-F 0 A-1517 H H H H H O CH.sub.2CH.sub.3 H 2-C(?O)Me,6-F 0 A-1518 H H H H H O CH.sub.2CH.sub.3 H 2-C(?O)Me,5-Me 0 A-1519 H H H H H O CH.sub.2CH.sub.3 H 2-C(?O)Me,6-Me 0 A-1520 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2OH,5-F 0 A-1521 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2OH,6-F 0 A-1522 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2OH,5-Me 0 A-1523 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2OH,6-Me 0 A-1524 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-F 0 A-1525 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-F 0 A-1526 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-F 0 A-1527 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-1528 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-1529 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-1530 H H H H H O CH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,5-F 0 A-1531 H H H H H O CH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,6-F 0 A-1532 H H H H H O CH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,5-Me 0 A-1533 H H H H H O CH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,6-Me 0 A-1534 H H H H H O CH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-F 0
(129) TABLE-US-00028 TABLE 28 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1535 H H H H H O CH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-1536 H H H H H O CH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-1537 H H H H H O CH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-1538 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-F 0 A-1539 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,6-F 0 A-1540 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-Me 0 A-1541 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,6-Me 0 A-1542 H H H H H O CH.sub.2CH.sub.3 H 2-NMe.sub.2,5-F 0 A-1543 H H H H H O CH.sub.2CH.sub.3 H 2-NMe.sub.2,6-F 0 A-1544 H H H H H O CH.sub.2CH.sub.3 H 2-NMe.sub.2,5-Me 0 A-1545 H H H H H O CH.sub.2CH.sub.3 H 2-NMe.sub.2,6-Me 0 A-1546 H H H H H O CH.sub.2CH.sub.3 H 2-CN,4-F 0 A-1547 H H H H H O CH.sub.2CH.sub.3 H 2-CN,5-F 0 A-1548 H H H H H O CH.sub.2CH.sub.3 H 2-CN,6-F 0 A-1549 H H H H H O CH.sub.2CH.sub.3 H 2-CN,6-Me 0 A-1550 H H H H H O CH.sub.2CH.sub.3 H 2-CN,5-OMe 0 A-1551 H H H H H O CH.sub.2CH.sub.3 H 2-CN,6-OMe 0 A-1552 H H H H H O CH.sub.2CH.sub.3 H 3-CN,6-Me 0 A-1553 H H H H H O CH.sub.2CH.sub.3 H 3-CN,6-OMe 0 A-1554 H H H H H O CH.sub.2CH.sub.3 H 4-CN,2-Me 0 A-1555 H H H H H O CH.sub.2CH.sub.3 H 4-CN,2-OMe 0 A-1556 H H H H H O CH.sub.2CH.sub.3 H 2-NO.sub.2,4-F 0 A-1557 H H H H H O CH.sub.2CH.sub.3 H 2-NO.sub.2,5-F 0 A-1558 H H H H H O CH.sub.2CH.sub.3 H 2-NO.sub.2,6-F 0 A-1559 H H H H H O CH.sub.2CH.sub.3 H 2-NO.sub.2,4-Me 0 A-1560 H H H H H O CH.sub.2CH.sub.3 H 2-NO.sub.2,5-Me 0 A-1561 H H H H H O CH.sub.2CH.sub.3 H 2-NO.sub.2,6-Me 0 A-1562 H H H H H O CH.sub.2CH.sub.3 H 2-Me,4,5-F.sub.2 0 A-1563 H H H H H O CH.sub.2CH.sub.3 H 2-Me,6-Et 0 A-1564 H H H H H O CH.sub.2CH.sub.3 H 2-cyclopropyl,6-OMe 0 A-1565 H H H H H O CH.sub.2CH.sub.3 H 2-Me,5-Et 0 A-1566 H H H H H O CH.sub.2CH.sub.3 H 2,6-Et.sub.2 0 A-1567 H H H H H O CH.sub.2CH.sub.3 H 2-Et,6-F 0 A-1568 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-1569 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-1570 H H H H H O CH.sub.2CH.sub.3 H 2-CH.sub.2NMe.sub.2 0 A-1571 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H H 0 A-1572 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-F 0 A-1573 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Cl 0 A-1574 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Br 0 A-1575 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OH 0 A-1576 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Me 0 A-1577 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Et 0 A-1578 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Pr 0 A-1579 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CF.sub.3 0 A-1580 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CHF.sub.2 0 A-1581 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2F 0 A-1582 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CF.sub.2Cl 0 A-1583 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-cyclopropyl 0 A-1584 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-cyclobutyl 0 A-1585 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-cyclopentyl 0 A-1586 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-ethenyl 0 A-1587 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-allyl 0 A-1588 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(prop-1-en-1-yl) 0 A-1589 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(trifluoroethenyl) 0 A-1590 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OMe 0 A-1591 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OEt 0
(130) TABLE-US-00029 TABLE 29 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1592 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OPr 0 A-1593 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-O(i-Pr) 0 A-1594 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OCF.sub.3 0 A-1595 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OCHF.sub.2 0 A-1596 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(cyclopropyloxy) 0 A-1597 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(cyclobutyloxy) 0 A-1598 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(cyclopentyloxy) 0 A-1599 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-1600 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(oxiran-2-yl) 0 A-1601 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-SMe 0 A-1602 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 3-SMe 0 A-1603 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O)Me 0 A-1604 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 3-S(?O)Me 0 A-1605 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O).sub.2Me 0 A-1606 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 3-S(?O).sub.2Me 0 A-1607 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-SCF.sub.3 0 A-1608 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 3-SCF.sub.3 0 A-1609 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 3-S(?O)CF.sub.3 0 A-1610 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 3-SCF(CF.sub.3).sub.2 0 A-1611 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(cyclopropylthio) 0 A-1612 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(cyclopropylsuIfinyl) 0 A-1613 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(cyclopropylsulfonyl) 0 A-1614 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-C(?O)Me 0 A-1615 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2C(?O)CH.sub.3 0 A-1616 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2C(?O)CF.sub.3 0 A-1617 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2OH 0 A-1618 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3 0 A-1619 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-1620 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3 0 A-1621 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2S(?O)CH.sub.3 0 A-1622 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-1623 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(benzyloxy) 0 A-1624 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-NH.sub.2 0 A-1625 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-NHMe 0 A-1626 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-N(Me).sub.2 0 A-1627 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(1,3-dioxolan-2-yl) 0 A-1628 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(1,3-dioxan-2-yl) 0 A-1629 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(1H-imidazol-2-yl) 0 A-1630 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(thiazol-2-yl) 0 A-1631 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(oxazol-2-yl) 0 A-1632 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH?NOH 0 A-1633 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH?NOMe 0 A-1634 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-1635 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CN 0 A-1636 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-NO.sub.2 0 A-1637 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-F,6-Cl 0 A-1638 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-F,6-Me 0 A-1639 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 3-F,6-Me 0 A-1640 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 4-F,2-Me 0 A-1641 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-F,6-OMe 0 A-1642 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 3-F,6-OMe 0 A-1643 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2,6-Cl.sub.2 0 A-1644 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Cl,6-Me 0 A-1645 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 3-Cl,6-Me 0 A-1646 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 4-Cl,2-Me 0 A-1647 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Cl,5-CF.sub.3 0 A-1648 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Cl,6-CF.sub.3 0
(131) TABLE-US-00030 TABLE 30 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1649 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Cl,6-OMe 0 A-1650 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 3-Cl,6-OMe 0 A-1651 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 4-Cl,2-OMe 0 A-1652 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2,4-Me.sub.2 0 A-1653 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2,5-Me.sub.2 0 A-1654 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2,6-Me.sub.2 0 A-1655 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Me,4-CF.sub.3 0 A-1656 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Me,5-CF.sub.3 0 A-1657 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Me,6-CF.sub.3 0 A-1658 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Me,4-OMe 0 A-1659 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Me,5-OMe 0 A-1660 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Me,6-OMe 0 A-1661 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 3-Me,6-OMe 0 A-1662 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 4-Me,2-OMe 0 A-1663 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2,5-OMe.sub.2 0 A-1664 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2,6-OMe.sub.2 0 A-1665 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OMe,6-CF.sub.3 0 A-1666 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CHF.sub.2,5-F 0 A-1667 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CHF.sub.2,6-F 0 A-1668 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CHF.sub.2,5-Me 0 A-1669 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CHF.sub.2,6-Me 0 A-1670 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-cyclopropyl,5-F 0 A-1671 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-cyclopropyl,6-F 0 A-1672 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-cyclopropyl,5-Me 0 A-1673 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-cyclopropyl,6-Me 0 A-1674 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-ethenyl,6-F 0 A-1675 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-ethenyl,6-Me 0 A-1676 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OEt,5-F 0 A-1677 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OEt,6-F 0 A-1678 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OEt,5-Cl 0 A-1679 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OEt,6-Cl 0 A-1680 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OEt,5-Me 0 A-1681 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OEt,6-Me 0 A-1682 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OCHF.sub.2,5-F 0 A-1683 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OCHF.sub.2,6-F 0 A-1684 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OCHF.sub.2,5-Me 0 A-1685 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OCHF.sub.2,6-Me 0 A-1686 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(cyclopropyloxy),5-F 0 A-1687 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(cyclopropyloxy),6-F 0 A-1688 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(cyclopropyloxy),5-Me 0 A-1689 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(cyclopropyloxy),6-Me 0 A-1690 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-SMe,5-F 0 A-1691 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-SMe,6-F 0 A-1692 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-SMe,5-Me 0 A-1693 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-SMe,6-Me 0 A-1694 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O)Me,5-F 0 A-1695 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O)Me,6-F 0 A-1696 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O)Me,5-Me 0 A-1697 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O)Me,6-Me 0 A-1698 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,5-F 0 A-1699 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,6-F 0 A-1700 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,5-Me 0 A-1701 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,6-Me 0 A-1702 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-SCF.sub.3,5-F 0 A-1703 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-SCF.sub.3,6-F 0 A-1704 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-SCF.sub.3,5-Me 0 A-1705 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-SCF.sub.3,6-Me 0
(132) TABLE-US-00031 TABLE 31 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1706 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,5-F 0 A-1707 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,6-F 0 A-1708 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,5-Me 0 A-1709 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,6-Me 0 A-1710 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-1711 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-1712 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-1713 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-1714 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(cyclopropylthio),5-F 0 A-1715 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(cyclopropylthio),6-F 0 A-1716 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(cyclopropylthio),5-Me 0 A-1717 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-(cyclopropylthio),6-Me 0 A-1718 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-C(?O)Me,5-F 0 A-1719 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-C(?O)Me,6-F 0 A-1720 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-C(?O)Me,5-Me 0 A-1721 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-C(?O)Me,6-Me 0 A-1722 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2OH,5-F 0 A-1723 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2OH,6-F 0 A-1724 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2OH,5-Me 0 A-1725 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2OH,6-Me 0 A-1726 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-F 0 A-1727 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-F 0 A-1728 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-F 0 A-1729 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-1730 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-1731 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-1732 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,5-F 0 A-1733 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,6-F 0 A-1734 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,5-Me 0 A-1735 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,6-Me 0 A-1736 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-1737 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-1738 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-1739 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-1740 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-F 0 A-1741 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,6-F 0 A-1742 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-Me 0 A-1743 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,6-Me 0 A-1744 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-NMe.sub.2,5-F 0 A-1745 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-NMe.sub.2,6-F 0 A-1746 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-NMe.sub.2,5-Me 0 A-1747 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-NMe.sub.2,6-Me 0 A-1748 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CN,4-F 0 A-1749 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CN,5-F 0 A-1750 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CN,6-F 0 A-1751 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CN,6-Me 0 A-1752 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CN,5-OMe 0 A-1753 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CN,6-OMe 0 A-1754 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 3-CN,6-Me 0 A-1755 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 3-CN,6-OMe 0 A-1756 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 4-CN,2-Me 0 A-1757 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 4-CN,2-OMe 0 A-1758 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-NO.sub.2,4-F 0 A-1759 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-NO.sub.2,5-F 0 A-1760 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-NO.sub.2,6-F 0 A-1761 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-NO.sub.2,4-Me 0 A-1762 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-NO.sub.2,5-Me 0
(133) TABLE-US-00032 TABLE 32 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1763 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-NO.sub.2,6-Me 0 A-1764 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Me,4,5-F.sub.2 0 A-1765 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Me,6-Et 0 A-1766 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-cyclopropyl,6-OMe 0 A-1767 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Me,5-Et 0 A-1768 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2,6-Et.sub.2 0 A-1769 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-Et,6-F 0 A-1770 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-1771 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-1772 H H H H H O CH.sub.2CH.sub.2CH.sub.3 H 2-CH.sub.2NMe.sub.2 0 A-1773 H H H H H O cyclopropyl H H 0 A-1774 H H H H H O cyclopropyl H 2-F 0 A-1775 H H H H H O cyclopropyl H 2-Cl 0 A-1776 H H H H H O cyclopropyl H 2-Br 0 A-1777 H H H H H O cyclopropyl H 2-OH 0 A-1778 H H H H H O cyclopropyl H 2-Me 0 A-1779 H H H H H O cyclopropyl H 2-Et 0 A-1780 H H H H H O cyclopropyl H 2-Pr 0 A-1781 H H H H H O cyclopropyl H 2-CF.sub.3 0 A-1782 H H H H H O cyclopropyl H 2-CHF.sub.2 0 A-1783 H H H H H O cyclopropyl H 2-CH.sub.2F 0 A-1784 H H H H H O cyclopropyl H 2-CF.sub.2Cl 0 A-1785 H H H H H O cyclopropyl H 2-cyclopropyl 0 A-1786 H H H H H O cyclopropyl H 2-cyclobutyl 0 A-1787 H H H H H O cyclopropyl H 2-cyclopentyl 0 A-1788 H H H H H O cyclopropyl H 2-ethenyl 0 A-1789 H H H H H O cyclopropyl H 2-allyl 0 A-1790 H H H H H O cyclopropyl H 2-(prop-1-en-1-yl) 0 A-1791 H H H H H O cyclopropyl H 2-(trifluoroethenyl) 0 A-1792 H H H H H O cyclopropyl H 2-OMe 0 A-1793 H H H H H O cyclopropyl H 2-OEt 0 A-1794 H H H H H O cyclopropyl H 2-OPr 0 A-1795 H H H H H O cyclopropyl H 2-O(i-Pr) 0 A-1796 H H H H H O cyclopropyl H 2-OCF.sub.3 0 A-1797 H H H H H O cyclopropyl H 2-OCHF.sub.2 0 A-1798 H H H H H O cyclopropyl H 2-(cyclopropyloxy) 0 A-1799 H H H H H O cyclopropyl H 2-(cyclobutyloxy) 0 A-1800 H H H H H O cyclopropyl H 2-(cyclopentyloxy) 0 A-1801 H H H H H O cyclopropyl H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-1802 H H H H H O cyclopropyl H 2-(oxiran-2-yl) 0 A-1803 H H H H H O cyclopropyl H 2-SMe 0 A-1804 H H H H H O cyclopropyl H 3-SMe 0 A-1805 H H H H H O cyclopropyl H 2-S(?O)Me 0 A-1806 H H H H H O cyclopropyl H 3-S(?O)Me 0 A-1807 H H H H H O cyclopropyl H 2-S(?O).sub.2Me 0 A-1808 H H H H H O cyclopropyl H 3-S(?O).sub.2Me 0 A-1809 H H H H H O cyclopropyl H 2-SCF.sub.3 0 A-1810 H H H H H O cyclopropyl H 3-SCF.sub.3 0 A-1811 H H H H H O cyclopropyl H 3-S(?O)CF.sub.3 0 A-1812 H H H H H O cyclopropyl H 3-SCF(CF.sub.3).sub.2 0 A-1813 H H H H H O cyclopropyl H 2-(cyclopropylthio) 0 A-1814 H H H H H O cyclopropyl H 2-(cyclopropylsulfinyl) 0 A-1815 H H H H H O cyclopropyl H 2-(cyclopropylsulfonyl) 0 A-1816 H H H H H O cyclopropyl H 2-C(?O)Me 0 A-1817 H H H H H O cyclopropyl H 2-CH.sub.2C(?O)CH.sub.3 0 A-1818 H H H H H O cyclopropyl H 2-CH.sub.2C(?O)CF.sub.3 0 A-1819 H H H H H O cyclopropyl H 2-CH.sub.2OH 0
(134) TABLE-US-00033 TABLE 33 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1820 H H H H H O cyclopropyl H 2-CH.sub.2OCH.sub.3 0 A-1821 H H H H H O cyclopropyl H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-1822 H H H H H O cyclopropyl H 2-CH.sub.2SCH.sub.3 0 A-1823 H H H H H O cyclopropyl H 2-CH.sub.2S(?O)CH.sub.3 0 A-1824 H H H H H O cyclopropyl H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-1825 H H H H H O cyclopropyl H 2-(benzyloxy) 0 A-1826 H H H H H O cyclopropyl H 2-NH.sub.2 0 A-1827 H H H H H O cyclopropyl H 2-NHMe 0 A-1828 H H H H H O cyclopropyl H 2-N(Me).sub.2 0 A-1829 H H H H H O cyclopropyl H 2-(1,3-dioxolan-2-yl) 0 A-1830 H H H H H O cyclopropyl H 2-(1,3-dioxan-2-yl) 0 A-1831 H H H H H O cyclopropyl H 2-(1-imidazol-2-y-l) 0 A-1832 H H H H H O cyclopropyl H 2-(thiazol-2-yl) 0 A-1833 H H H H H O cyclopropyl H 2-(oxazol2-yl) 0 A-1834 H H H H H O cyclopropyl H 2-CH?NOH 0 A-1835 H H H H H O cyclopropyl H 2-CH?NOMe 0 A-1836 H H H H H O cyclopropyl H 2-(4,5-dihydro-3-isoxazolyl) 0 A-1837 H H H H H O cyclopropyl H 2-CN 0 A-1838 H H H H H O cyclopropyl H 2-NO.sub.2 0 A-1839 H H H H H O cyclopropyl H 2,6-Cl 0 A-1840 H H H H H O cyclopropyl H 2-F,6-Me 0 A-1841 H H H H H O cyclopropyl H 3-F,6-Me 0 A-1842 H H H H H O cyclopropyl H 4-F,2-Me 0 A-1843 H H H H H O cyclopropyl H 2-F,6-OMe 0 A-1844 H H H H H O cyclopropyl H 3-F,6-OMe 0 A-1845 H H H H H O cyclopropyl H 2,6-Cl.sub.2 0 A-1846 H H H H H O cyclopropyl H 2-Cl,6-Me 0 A-1847 H H H H H O cyclopropyl H 3-Cl,6-Me 0 A-1848 H H H H H O cyclopropyl H 4-Cl,2-Me 0 A-1849 H H H H H O cyclopropyl H 2-Cl,5-CF.sub.3 0 A-1850 H H H H H O cyclopropyl H 2-Cl,6-CF.sub.3 0 A-1851 H H H H H O cyclopropyl H 2-Cl,6-OMe 0 A-1852 H H H H H O cyclopropyl H 3-Cl,6-OMe 0 A-1853 H H H H H O cyclopropyl H 4-Cl,2-OMe 0 A-1854 H H H H H O cyclopropyl H 2,4-Me.sub.2 0 A-1855 H H H H H O cyclopropyl H 2,5-Me.sub.2 0 A-1856 H H H H H O cyclopropyl H 2,6-Me.sub.2 0 A-1857 H H H H H O cyclopropyl H 2-Me,4-CF.sub.3 0 A-1858 H H H H H O cyclopropyl H 2-Me,5-CF.sub.3 0 A-1859 H H H H H O cyclopropyl H 2-Me,6-CF.sub.3 0 A-1860 H H H H H O cyclopropyl H 2-Me,4-OMe 0 A-1861 H H H H H O cyclopropyl H 2-Me,5-OMe 0 A-1862 H H H H H O cyclopropyl H 2-Me,6-OMe 0 A-1863 H H H H H O cyclopropyl H 3-Me,6-OMe 0 A-1864 H H H H H O cyclopropyl H 4-Me,2-OMe 0 A-1865 H H H H H O cyclopropyl H 2,5-OMe.sub.2 0 A-1866 H H H H H O cyclopropyl H 2,6-OMe.sub.2 0 A-1867 H H H H H O cyclopropyl H 2-OMe,6-CF.sub.3 0 A-1868 H H H H H O cyclopropyl H 2-CHF.sub.2,5-F 0 A-1869 H H H H H O cyclopropyl H 2-CHF.sub.2,6-F 0 A-1870 H H H H H O cyclopropyl H 2-CHF.sub.2,5-Me 0 A-1871 H H H H H O cyclopropyl H 2-CHF.sub.2,6-Me 0 A-1872 H H H H H O cyclopropyl H 2-cyclopropyl,5-F 0 A-1873 H H H H H O cyclopropyl H 2-cyclopropyl,6-F 0 A-1874 H H H H H O cyclopropyl H 2-cyclopropyl,5-Me 0 A-1875 H H H H H O cyclopropyl H 2-cyclopropyl,6-Me 0 A-1876 H H H H H O cyclopropyl H 2-ethenyl,6-F 0
(135) TABLE-US-00034 TABLE 34 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1877 H H H H H O cyclopropyl H 2-ethenyl,6-Me 0 A-1878 H H H H H O cyclopropyl H 2-OEt,5-F 0 A-1879 H H H H H O cyclopropyl H 2-OEt,6-F 0 A-1880 H H H H H O cyclopropyl H 2-OEt,5-Cl 0 A-1881 H H H H H O cyclopropyl H 2-OEt,6-Cl 0 A-1882 H H H H H O cyclopropyl H 2-OEt,5-Me 0 A-1883 H H H H H O cyclopropyl H 2-OEt,6-Me 0 A-1884 H H H H H O cyclopropyl H 2-OCHF.sub.2,5-F 0 A-1885 H H H H H O cyclopropyl H 2-OCHF.sub.2,6-F 0 A-1886 H H H H H O cyclopropyl H 2-OCHF.sub.2,5-Me 0 A-1887 H H H H H O cyclopropyl H 2-OCHF.sub.2,6-Me 0 A-1888 H H H H H O cyclopropyl H 2-(cyclopropyloxy),5-F 0 A-1889 H H H H H O cyclopropyl H 2-(cyclopropyloxy),6-F 0 A-1890 H H H H H O cyclopropyl H 2-(cyclopropyloxy),5-Me 0 A-1891 H H H H H O cyclopropyl H 2-(cyclopropyloxy),6-Me 0 A-1892 H H H H H O cyclopropyl H 2-SMe,5-F 0 A-1893 H H H H H O cyclopropyl H 2-SMe,6-F 0 A-1894 H H H H H O cyclopropyl H 2-SMe,5-Me 0 A-1895 H H H H H O cyclopropyl H 2-SMe,6-Me 0 A-1896 H H H H H O cyclopropyl H 2-S(?O)Me,5-F 0 A-1897 H H H H H O cyclopropyl H 2-S(?O)Me,6-F 0 A-1898 H H H H H O cyclopropyl H 2-S(?O)Me,5-Me 0 A-1899 H H H H H O cyclopropyl H 2-S(?O)Me,6-Me 0 A-1900 H H H H H O cyclopropyl H 2-S(?O).sub.2Me,5-F 0 A-1901 H H H H H O cyclopropyl H 2-S(?O).sub.2Me,6-F 0 A-1902 H H H H H O cyclopropyl H 2-S(?O).sub.2Me,5-Me 0 A-1903 H H H H H O cyclopropyl H 2-S(?O).sub.2Me,6-Me 0 A-1904 H H H H H O cyclopropyl H 2-SCF.sub.3,5-F 0 A-1905 H H H H H O cyclopropyl H 2-SCF.sub.3,6-F 0 A-1906 H H H H H O cyclopropyl H 2-SCF.sub.3,5-Me 0 A-1907 H H H H H O cyclopropyl H 2-SCF.sub.3,6-Me 0 A-1908 H H H H H O cyclopropyl H 2-S(?O)CF.sub.3,5-F 0 A-1909 H H H H H O cyclopropyl H 2-S(?O)CF.sub.3,6-F 0 A-1910 H H H H H O cyclopropyl H 2-S(?O)CF.sub.3,5-Me 0 A-1911 H H H H H O cyclopropyl H 2-S(?O)CF.sub.3,6-Me 0 A-1912 H H H H H O cyclopropyl H 2-S(?O).sub.2CF.sub.3,5-F 0 A-1913 H H H H H O cyclopropyl H 2-S(?O).sub.2CF.sub.3,6-F 0 A-1914 H H H H H O cyclopropyl H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-1915 H H H H H O cyclopropyl H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-1916 H H H H H O cyclopropyl H 2-(cyclopropylthio),5-F 0 A-1917 H H H H H O cyclopropyl H 2-(cyclopropylthio),6-F 0 A-1918 H H H H H O cyclopropyl H 2-(cyclopropylthio),5-Me 0 A-1919 H H H H H O cyclopropyl H 2-(cyclopropylthio),6-Me 0 A-1920 H H H H H O cyclopropyl H 2-C(?O)Me,5-F 0 A-1921 H H H H H O cyclopropyl H 2-C(?O)Me,6-F 0 A-1922 H H H H H O cyclopropyl H 2-C(?O)Me,5-Me 0 A-1923 H H H H H O cyclopropyl H 2-C(?O)Me,6-Me 0 A-1924 H H H H H O cyclopropyl H 2-CH.sub.2OH,5-F 0 A-1925 H H H H H O cyclopropyl H 2-CH.sub.2OH,6-F 0 A-1926 H H H H H O cyclopropyl H 2-CH.sub.2OH,5-Me 0 A-1927 H H H H H O cyclopropyl H 2-CH.sub.2OH,6-Me 0 A-1928 H H H H H O cyclopropyl H 2-CH.sub.2OCH.sub.3,4-F 0 A-1929 H H H H H O cyclopropyl H 2-CH.sub.2OCH.sub.3,5-F 0 A-1930 H H H H H O cyclopropyl H 2-CH.sub.2OCH.sub.3,6-F 0 A-1931 H H H H H O cyclopropyl H 2-CH.sub.2OCH.sub.3,4-Me 0 A-1932 H H H H H O cyclopropyl H 2-CH.sub.2OCH.sub.3,5-Me 0 A-1933 H H H H H O cyclopropyl H 2-CH.sub.2OCH.sub.3,6-Me 0
(136) TABLE-US-00035 TABLE 35 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1934 H H H H H O cyclopropyl H 2-OC(?O)CH.sub.3,5-F 0 A-1935 H H H H H O cyclopropyl H 2-OC(?O)CH.sub.3,6-F 0 A-1936 H H H H H O cyclopropyl H 2-OC(?O)CH.sub.3,5-Me 0 A-1937 H H H H H O cyclopropyl H 2-OC(?O)CH.sub.3,6-Me 0 A-1938 H H H H H O cyclopropyl H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-1939 H H H H H O cyclopropyl H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-1940 H H H H H O cyclopropyl H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-1941 H H H H H O cyclopropyl H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-1942 H H H H H O cyclopropyl H 2-CH.sub.2SCH.sub.3,5-F 0 A-1943 H H H H H O cyclopropyl H 2-CH.sub.2SCH.sub.3,6-F 0 A-1944 H H H H H O cyclopropyl H 2-CH.sub.2SCH.sub.3,5-Me 0 A-1945 H H H H H O cyclopropyl H 2-CH.sub.2SCH.sub.3,6-Me 0 A-1946 H H H H H O cyclopropyl H 2-NMe.sub.2,5-F 0 A-1947 H H H H H O cyclopropyl H 2-NMe.sub.2,6-F 0 A-1948 H H H H H O cyclopropyl H 2-NMe.sub.2,5-Me 0 A-1949 H H H H H O cyclopropyl H 2-NMe.sub.2,6-Me 0 A-1950 H H H H H O cyclopropyl H 2-CN,4-F 0 A-1951 H H H H H O cyclopropyl H 2-CN,5-F 0 A-1952 H H H H H O cyclopropyl H 2-CN,6-F 0 A-1953 H H H H H O cyclopropyl H 2-CN,6-Me 0 A-1954 H H H H H O cyclopropyl H 2-CN,5-OMe 0 A-1955 H H H H H O cyclopropyl H 2-CN,6-OMe 0 A-1956 H H H H H O cyclopropyl H 3-CN,6-Me 0 A-1957 H H H H H O cyclopropyl H 3-CN,6-OMe 0 A-1958 H H H H H O cyclopropyl H 4-CN,2-Me 0 A-1959 H H H H H O cyclopropyl H 4-CN,2-OMe 0 A-1960 H H H H H O cyclopropyl H 2-NO.sub.2,4-F 0 A-1961 H H H H H O cyclopropyl H 2-NO.sub.2,5-F 0 A-1962 H H H H H O cyclopropyl H 2-NO.sub.2,6-F 0 A-1963 H H H H H O cyclopropyl H 2-NO.sub.2,4-Me 0 A-1964 H H H H H O cyclopropyl H 2-NO.sub.2,5-Me 0 A-1965 H H H H H O cyclopropyl H 2-NO.sub.2,6-Me 0 A-1966 H H H H H O cyclopropyl H 2-Me,4,5-F.sub.2 0 A-1967 H H H H H O cyclopropyl H 2-Me,6-Et 0 A-1968 H H H H H O cyclopropyl H 2-cyclopropyl,6-OMe 0 A-1969 H H H H H O cyclopropyl H 2-Me,5-Et 0 A-1970 H H H H H O cyclopropyl H 2,6-Et.sub.2 0 A-1971 H H H H H O cyclopropyl H 2-Et,6-F 0 A-1972 H H H H H O cyclopropyl H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-1973 H H H H H O cyclopropyl H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-1974 H H H H H O cyclopropyl H 2-CH.sub.2NMe.sub.2 0 A-1975 H H H H H O cyclohexyl H H 0 A-1976 H H H H H O cyclohexyl H 2-F 0 A-1977 H H H H H O cyclohexyl H 2-Cl 0 A-1978 H H H H H O cyclohexyl H 2-Br 0 A-1979 H H H H H O cyclohexyl H 2-OH 0 A-1980 H H H H H O cyclohexyl H 2-Me 0 A-1981 H H H H H O cyclohexyl H 2-Et 0 A-1982 H H H H H O cyclohexyl H 2-Pr 0 A-1983 H H H H H O cyclohexyl H 2-CF.sub.3 0 A-1984 H H H H H O cyclohexyl H 2-CHF.sub.2 0 A-1985 H H H H H O cyclohexyl H 2-CH.sub.2F 0 A-1986 H H H H H O cyclohexyl H 2-CF.sub.2Cl 0 A-1987 H H H H H O cyclohexyl H 2-cyclopropyl 0 A-1988 H H H H H O cyclohexyl H 2-cyclobutyl 0 A-1989 H H H H H O cyclohexyl H 2-cyclopentyl 0 A-1990 H H H H H O cyclohexyl H 2-ethenyl 0
(137) TABLE-US-00036 TABLE 36 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-1991 H H H H H O cyclohexyl H 2-allyl 0 A-1992 H H H H H O cyclohexyl H 2-(prop-1-en-1-yl) 0 A-1993 H H H H H O cyclohexyl H 2-(trifluoroethenyl) 0 A-1994 H H H H H O cyclohexyl H 2-OMe 0 A-1995 H H H H H O cyclohexyl H 2-OEt 0 A-1996 H H H H H O cyclohexyl H 2-OPr 0 A-1997 H H H H H O cyclohexyl H 2-O(i-Pr) 0 A-1998 H H H H H O cyclohexyl H 2-OCF.sub.3 0 A-1999 H H H H H O cyclohexyl H 2-OCHF.sub.2 0 A-2000 H H H H H O cyclohexyl H 2-(cyclopropyloxy) 0 A-2001 H H H H H O cyclohexyl H 2-(cyclobutyloxy) 0 A-2002 H H H H H O cyclohexyl H 2-(cyclopentyloxy) 0 A-2003 H H H H H O cyclohexyl H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-2004 H H H H H O cyclohexyl H 2-(oxiran-2-yl) 0 A-2005 H H H H H O cyclohexyl H 2-SMe 0 A-2006 H H H H H O cyclohexyl H 3-SMe 0 A-2007 H H H H H O cyclohexyl H 2-S(?O)Me 0 A-2008 H H H H H O cyclohexyl H 3-S(?O)Me 0 A-2009 H H H H H O cyclohexyl H 2-S(?O).sub.2Me 0 A-2010 H H H H H O cyclohexyl H 3-S(?O).sub.2Me 0 A-2011 H H H H H O cyclohexyl H 2-SCF.sub.3 0 A-2012 H H H H H O cyclohexyl H 3-SCF.sub.3 0 A-2013 H H H H H O cyclohexyl H 3-S(?O)CF.sub.3 0 A-2014 H H H H H O cyclohexyl H 3-SCF(CF.sub.3).sub.2 0 A-2015 H H H H H O cyclohexyl H 2-(cyclopropylthio) 0 A-2016 H H H H H O cyclohexyl H 2-(cyclopropylsulfinyl) 0 A-2017 H H H H H O cyclohexyl H 2-(cyclopropylsulfonyl) 0 A-2018 H H H H H O cyclohexyl H 2-C(?O)Me 0 A-2019 H H H H H O cyclohexyl H 2-CH.sub.2C(?O)CH.sub.3 0 A-2020 H H H H H O cyclohexyl H 2-CH.sub.2C(?O)CF.sub.3 0 A-2021 H H H H H O cyclohexyl H 2-CH.sub.2OH 0 A-2022 H H H H H O cyclohexyl H 2-CH.sub.2OCH.sub.3 0 A-2023 H H H H H O cyclohexyl H 2-CH.sub.2OCH .sub.2CH.sub.3 0 A-2024 H H H H H O cyclohexyl H 2-CH.sub.2SCH.sub.3 0 A-2025 H H H H H O cyclohexyl H 2-CH.sub.2S(?O)CH.sub.3 0 A-2026 H H H H H O cyclohexyl H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-2027 H H H H H O cyclohexyl H 2-(benzyloxy) 0 A-2028 H H H H H O cyclohexyl H 2-NH.sub.2 0 A-2029 H H H H H O cyclohexyl H 2-NHMe 0 A-2030 H H H H H O cyclohexyl H 2-N(Me).sub.2 0 A-2031 H H H H H O cyclohexyl H 2-(1,3-dioxolan-2-yl) 0 A-2032 H H H H H O cyclohexyl H 2-(1,3-dioxan-2-yl) 0 A-2033 H H H H H O cyclohexyl H 2-(1H-imidazol-2-yl) 0 A-2034 H H H H H O cyclohexyl H 2-(thiazol-2-yl) 0 A-2035 H H H H H O cyclohexyl H 2-(oxazol-2-yl) 0 A-2036 H H H H H O cyclohexyl H 2-CH?NOH 0 A-2037 H H H H H O cyclohexyl H 2-CH?NOMe 0 A-2038 H H H H H O cyclohexyl H 2-(4,5-dihydro-3-isoxazolyl) 0 A-2039 H H H H H O cyclohexyl H 2-CN 0 A-2040 H H H H H O cyclohexyl H 2-NO.sub.2 0 A-2041 H H H H H O cyclohexyl H 2-F,6-Cl 0 A-2042 H H H H H O cyclohexyl H 2-F,6-Me 0 A-2043 H H H H H O cyclohexyl H 3-F,6-Me 0 A-2044 H H H H H O cyclohexyl H 4-F,2-Me 0 A-2045 H H H H H O cyclohexyl H 2-F,6-OMe 0 A-2046 H H H H H O cyclohexyl H 3-F,6-OMe 0 A-2047 H H H H H O cyclohexyl H 2,6-Cl.sub.2 0
(138) TABLE-US-00037 TABLE 37 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2048 H H H H H O cyclohexyl H 2-Cl,6-Me 0 A-2049 H H H H H O cyclohexyl H 3-Cl,6-Me 0 A-2050 H H H H H O cyclohexyl H 4-Cl,2-Me 0 A-2051 H H H H H O cyclohexyl H 2-Cl,5-CF.sub.3 0 A-2052 H H H H H O cyclohexy| H 2-Cl,6-CF.sub.3 0 A-2053 H H H H H O cyclohexyl H 2-Cl,6-OMe 0 A-2054 H H H H H O cyclohexyl H 3-Cl,6-OMe 0 A-2055 H H H H H O cyclohexyl H 4-Cl,2-OMe 0 A-2056 H H H H H O cyclohexyl H 2,4-Me.sub.2 0 A-2057 H H H H H O cyclohexyl H 2,5-Me.sub.2 0 A-2058 H H H H H O cyclohexy| H 2,6-Me.sub.2 0 A-2059 H H H H H O cyclohexyl H 2-Me,4-CF.sub.3 0 A-2060 H H H H H O cyclohexyl H 2-Me,5-CF.sub.3 0 A-2061 H H H H H O cyclohexyl H 2-Me,6-CF.sub.3 0 A-2062 H H H H H O cyclohexyl H 2-Me,4-OMe 0 A-2063 H H H H H O cyclohexyl H 2-Me,5-OMe 0 A-2064 H H H H H O cyclohexyl H 2-Me,6-OMe 0 A-2065 H H H H H O cyclohexyl H 3-Me,6-OMe 0 A-2066 H H H H H O cyclohexyl H 4-Me,2-OMe 0 A-2067 H H H H H O cyclohexyl H 2,5-OMe.sub.2 0 A-2068 H H H H H O cyclohexyl H 2,6-OMe.sub.2 0 A-2069 H H H H H O cyclohexyl H 2-OMe,6-CF.sub.3 0 A-2070 H H H H H O cyclohexyl H 2-CHF.sub.2,5-F 0 A-2071 H H H H H O cyclohexyl H 2-CHF.sub.2,6-F 0 A-2072 H H H H H O cyclohexyl H 2-CHF.sub.2,5-Me 0 A-2073 H H H H H O cyclohexyl H 2-CHF.sub.2,6-Me 0 A-2074 H H H H H O cyclohexyl H 2-cyclopropyl,5-F 0 A-2075 H H H H H O cyclohexyl H 2-cyclopropyl,6-F 0 A-2076 H H H H H O cyclohexyl H 2-cyclopropyl,5-Me 0 A-2077 H H H H H O cyclohexyl H 2-cyclopropyl,6-Me 0 A-2078 H H H H H O cyclohexyl H 2-ethenyl,6-F 0 A-2079 H H H H H O cyclohexyl H 2-ethenyl,6-Me 0 A-2080 H H H H H O cyclohexyl H 2-OEt,5-F 0 A-2081 H H H H H O cyclohexyl H 2-OEt,6-F 0 A-2082 H H H H H O cyclohexyl H 2-OEt,5-Cl 0 A-2083 H H H H H O cyclohexyl H 2-OEt,6-Cl 0 A-2084 H H H H H O cyclohexyl H 2-OEt,5-Me 0 A-2085 H H H H H O cyclohexyl H 2-OEt,6-Me 0 A-2086 H H H H H O cyclohexyl H 2-OCHF.sub.2,5-F 0 A-2087 H H H H H O cyclohexyl H 2-OCHF.sub.2,6-F 0 A-2088 H H H H H O cyclohexyl H 2-OCHF.sub.2,5-Me 0 A-2089 H H H H H O cyclohexyl H 2-OCHF.sub.2,6-Me 0 A-2090 H H H H H O cyclohexyl H 2-(cyclopropyloxy),5-F 0 A-2091 H H H H H O cyclohexyl H 2-(cyclopropyloxy),6-F 0 A-2092 H H H H H O cyclohexyl H 2-(cyclopropyloxy),5-Me 0 A-2093 H H H H H O cyclohexyl H 2-(cyclopropyloxy),6-Me 0 A-2094 H H H H H O cyclohexyl H 2-SMe,5-F 0 A-2095 H H H H H O cyclohexyl H 2-SMe,6-F 0 A-2096 H H H H H O cyclohexyl H 2-SMe,5-Me 0 A-2097 H H H H H O cyclohexyl H 2-SMe,6-Me 0 A-2098 H H H H H O cyclohexyl H 2-S(?O)Me,5-F 0 A-2099 H H H H H O cyclohexyl H 2-S(?O)Me,6-F 0 A-2100 H H H H H O cyclohexyl H 2-S(?O)Me,5-Me 0 A-2101 H H H H H O cyclohexyl H 2-S(?O)Me,6-Me 0 A-2102 H H H H H O cyclohexyl H 2-S(?O).sub.2Me,5-F 0 A-2103 H H H H H O cyclohexyl H 2-S(?O).sub.2Me,6-F 0 A-2104 H H H H H O cyclohexyl H 2-S(?O).sub.2Me,5-Me 0
(139) TABLE-US-00038 TABLE 38 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2105 H H H H H O cyclohexyl H 2-S(?O).sub.2Me,6-Me 0 A-2106 H H H H H O cyclohexyl H 2-SCF.sub.3,5-F 0 A-2107 H H H H H O cyclohexyl H 2-SCF.sub.3,6-F 0 A-2108 H H H H H O cyclohexyl H 2-SCF.sub.3,5-Me 0 A-2109 H H H H H O cyclohexyl H 2-SCF.sub.3,6-Me 0 A-2110 H H H H H O cyclohexyl H 2-S(?O)CF.sub.3,5-F 0 A-2111 H H H H H O cyclohexyl H 2-S(?O)CF.sub.3,6-F 0 A-2112 H H H H H O cyclohexyl H 2-S(?O)CF.sub.3,5-Me 0 A-2113 H H H H H O cyclohexyl H 2-S(?O)CF.sub.3,6-Me 0 A-2114 H H H H H O cyclohexyl H 2-S(?O).sub.2CF.sub.3,5-F 0 A-2115 H H H H H O cyclohexyl H 2-S(?O).sub.2CF.sub.3,6-F 0 A-2116 H H H H H O cyclohexyl H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-2117 H H H H H O cyclohexyl H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-2118 H H H H H O cyclohexyl H 2-(cyclopropylthio),5-F 0 A-2119 H H H H H O cyclohexyl H 2-(cyclopropylthio),6-F 0 A-2120 H H H H H O cyclohexyl H 2-(cyclopropylthio),5-Me 0 A-2121 H H H H H O cyclohexyl H 2-(cyclopropylthio),6-Me 0 A-2122 H H H H H O cyclohexyl H 2-C(?O)Me,5-F 0 A-2123 H H H H H O cyclohexyl H 2-C(?O)Me,6-F 0 A-2124 H H H H H O cyclohexyl H 2-C(?O)Me,5-Me 0 A-2125 H H H H H O cyclohexyl H 2-C(?O)Me,6-Me 0 A-2126 H H H H H O cyclohexyl H 2-CH.sub.2OH,5-F 0 A-2127 H H H H H O cyclohexyl H 2-CH.sub.2OH,6-F 0 A-2128 H H H H H O cyclohexyl H 2-CH.sub.2OH,5-Me 0 A-2129 H H H H H O cyclohexyl H 2-CH.sub.2OH,6-Me 0 A-2130 H H H H H O cyclohexyl H 2-CH.sub.2OCH.sub.3,4-F 0 A-2131 H H H H H O cyclohexyl H 2-CH.sub.2OCH.sub.3,5-F 0 A-2132 H H H H H O cyclohexyl H 2-CH.sub.2OCH.sub.3,6-F 0 A-2133 H H H H H O cyclohexyl H 2-CH.sub.2OCH.sub.3,4-Me 0 A-2134 H H H H H O cyclohexyl H 2-CH.sub.2OCH.sub.3,5-Me 0 A-2135 H H H H H O cyclohexyl H 2-CH.sub.2OCH.sub.3,6-Me 0 A-2136 H H H H H O cyclohexyl H 2-OC(?O)CH.sub.3,5-F 0 A-2137 H H H H H O cyclohexyl H 2-OC(?O)CH.sub.3,6-F 0 A-2138 H H H H H O cyclohexyl H 2-OC(?O)CH.sub.3,5-Me 0 A-2139 H H H H H O cyclohexyl H 2-OC(?O)CH.sub.3,6-Me 0 A-2140 H H H H H O cyclohexyl H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-2141 H H H H H O cyclohexyl H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-2142 H H H H H O cyclohexyl H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-2143 H H H H H O cyclohexyl H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-2144 H H H H H O cyclohexyl H 2-CH.sub.2SCH.sub.3,5-F 0 A-2145 H H H H H O cyclohexyl H 2-CH.sub.2SCH.sub.3,6-F 0 A-2146 H H H H H O cyclohexyl H 2-CH.sub.2SCH.sub.3,5-Me 0 A-2147 H H H H H O cyclohexyl H 2-CH.sub.2SCH.sub.3,6-Me 0 A-2148 H H H H H O cyclohexyl H 2-NMe.sub.2,5-F 0 A-2149 H H H H H O cyclohexyl H 2-NMe.sub.2,6-F 0 A-2150 H H H H H O cyclohexyl H 2-NMe.sub.2,5-Me 0 A-2151 H H H H H O cyclohexyl H 2-NMe.sub.2,6-Me 0 A-2152 H H H H H O cyclohexyl H 2-CN,4-F 0 A-2153 H H H H H O cyclohexyl H 2-CN,5-F 0 A-2154 H H H H H O cyclohexyl H 2-CN,6-F 0 A-2155 H H H H H O cyclohexyl H 2-CN,6-Me 0 A-2156 H H H H H O cyclohexyl H 2-CN,5-OMe 0 A-2157 H H H H H O cyclohexyl H 2-CN,6-OMe 0 A-2158 H H H H H O cyclohexyl H 3-CN,6-Me 0 A-2159 H H H H H O cyclohexyl H 3-CN,6-OMe 0 A-2160 H H H H H O cyclohexyl H 4-CN,2-Me 0 A-2161 H H H H H O cyclohexyl H 4-CN,2-OMe 0
(140) TABLE-US-00039 TABLE 39 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2162 H H H H H O cyclohexyl H 2-NO.sub.2,4-F 0 A-2163 H H H H H O cyclohexyl H 2-NO.sub.2,5-F 0 A-2164 H H H H H O cyclohexyl H 2-NO.sub.2,6-F 0 A-2165 H H H H H O cyclohexyl H 2-NO.sub.2,4-Me 0 A-2166 H H H H H O cyclohexyl H 2-NO.sub.2,5-Me 0 A-2167 H H H H H O cyclohexyl H 2-NO.sub.2,6-Me 0 A-2168 H H H H H O cyclohexyl H 2-Me,4,5-F.sub.2 0 A-2169 H H H H H O cyclohexyl H 2-Me,6-Et 0 A-2170 H H H H H O cyclohexyl H 2-cyclopropyl,6-OMe 0 A-2171 H H H H H O cyclohexyl H 2-Me,5-Et 0 A-2172 H H H H H O cyclohexyl H 2,6-Et.sub.2 0 A-2173 H H H H H O cyclohexyl H 2-Et,6-F 0 A-2174 H H H H H O cyclohexyl H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-2175 H H H H H O cyclohexyl H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-2176 H H H H H O cyclohexyl H 2-CH.sub.2NMe.sub.2 0 A-2177 H H H H H O allyl H H 0 A-2178 H H H H H O allyl H 2-F 0 A-2179 H H H H H O allyl H 2-C 0 A-2180 H H H H H O allyl H 2-Br 0 A-2181 H H H H H O allyl H 2-OH 0 A-2182 H H H H H O allyl H 2-Me 0 A-2183 H H H H H O allyl H 2-Et 0 A-2184 H H H H H O allyl H 2-Pr 0 A-2185 H H H H H O allyl H 2-CF.sub.3 0 A-2186 H H H H H O allyl H 2-CHF.sub.2 0 A-2187 H H H H H O allyl H 2-CH.sub.2F 0 A-2188 H H H H H O allyl H 2-CF.sub.2Cl 0 A-2189 H H H H H O allyl H 2-cyclopropyl 0 A-2190 H H H H H O allyl H 2-cyclobutyl 0 A-2191 H H H H H O allyl H 2-cyclopentyl 0 A-2192 H H H H H O allyl H 2-ethenyl 0 A-2193 H H H H H O allyl H 2-allyl 0 A-2194 H H H H H O allyl H 2-(prop-1-en-1-yl) 0 A-2195 H H H H H O allyl H 2-(trifluorothenyl) 0 A-2196 H H H H H O allyl H 2-OMe 0 A-2197 H H H H H O allyl H 2-OEt 0 A-2198 H H H H H O allyl H 2-OPr 0 A-2199 H H H H H O allyl H 2-O(i-Pr) 0 A-2200 H H H H H O allyl H 2-OCF.sub.3 0 A-2201 H H H H H O allyl H 2-OCHF.sub.2 0 A-2202 H H H H H O allyl H 2-(cyclopropyloxy) 0 A-2203 H H H H H O allyl H 2-(cyclobutyloxy) 0 A-2204 H H H H H O allyl H 2-(cyclopentyloxy) 0 A-2205 H H H H H O allyl H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-2206 H H H H H O allyl H 2-(oxiran-2-yl) 0 A-2207 H H H H H O allyl H 2-SMe 0 A-2208 H H H H H O allyl H 3-SMe 0 A-2209 H H H H H O allyl H 2-S(?O)Me 0 A-2210 H H H H H O allyl H 3-S(?O)Me 0 A-2211 H H H H H O allyl H 2-S(?O).sub.2Me 0 A-2212 H H H H H O allyl H 3-S(?O).sub.2Me 0 A-2213 H H H H H O allyl H 2-SCF.sub.3 0 A-2214 H H H H H O allyl H 3-SCF.sub.3 0 A-2215 H H H H H O allyl H 3-S(?O)CF.sub.3 0 A-2216 H H H H H O allyl H 3-SCF(CF.sub.3).sub.2 0 A-2217 H H H H H O allyl H 2-(cyclopropylthio) 0 A-2218 H H H H H O allyl H 2-(cyclopropylsulfinyl) 0
(141) TABLE-US-00040 TABLE 40 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2219 H H H H H O allyl H 2-(cyclopropylsulfonyl) 0 A-2220 H H H H H O allyl H 2-C(?O)Me 0 A-2221 H H H H H O allyl H 2-CH.sub.2C(?O)CH.sub.3 0 A-2222 H H H H H O allyl H 2-CH.sub.2C(?O)CF.sub.3 0 A-2223 H H H H H O allyl H 2-CH.sub.2OH 0 A-2224 H H H H H O allyl H 2-CH.sub.2OCH.sub.3 0 A-2225 H H H H H O allyl H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-2226 H H H H H O allyl H 2-CH.sub.2SCH.sub.3 0 A-2227 H H H H H O allyl H 2-CH.sub.2S(?O)CH.sub.3 0 A-2228 H H H H H O allyl H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-2229 H H H H H O allyl H 2-(benzyloxy) 0 A-2230 H H H H H O allyl H 2-NH.sub.2 0 A-2231 H H H H H O allyl H 2-NHMe 0 A-2232 H H H H H O allyl H 2-N(Me).sub.2 0 A-2233 H H H H H O allyl H 2-(1,3-ioxolan-2-yl) 0 A-2234 H H H H H O allyl H 2-(1,3-dioxan-2-yl) 0 A-2235 H H H H H O allyl H 2-(1H-imidazol-2-yl) 0 A-2236 H H H H H O allyl H 2-(thizol-2-yl) 0 A-2237 H H H H H O allyl H 2-(oxazol-2-yl) 0 A-2238 H H H H H O allyl H 2-CH?NOH 0 A-2239 H H H H H O allyl H 2-CH?NOMe 0 A-2240 H H H H H O allyl H 2-(4,5-dihydro-3-isoxazolyl) 0 A-2241 H H H H H O allyl H 2-CN 0 A-2242 H H H H H O allyl H 2-NO.sub.2 0 A-2243 H H H H H O allyl H 2-F,6-Cl 0 A-2244 H H H H H O allyl H 2-F,6-Me 0 A-2245 H H H H H O allyl H 3-F,6-Me 0 A-2246 H H H H H O allyl H 4-F,2-Me 0 A-2247 H H H H H O allyl H 2-F,6-OMe 0 A-2248 H H H H H O allyl H 3-F,6-OMe 0 A-2249 H H H H H O allyl H 2,6-Cl 0 A-2250 H H H H H O allyl H 2-Cl,6-Me 0 A-2251 H H H H H O allyl H 3-Cl,6-Me 0 A-2252 H H H H H O allyl H 4-Cl,2-Me 0 A-2253 H H H H H O allyl H 2-Cl,5-CF.sub.3 0 A-2254 H H H H H O allyl H 2-Cl,6-CF.sub.3 0 A-2255 H H H H H O allyl H 2-Cl,6-OMe 0 A-2256 H H H H H O allyl H 3-Cl,6-OMe 0 A-2257 H H H H H O allyl H 4-Cl,2-OMe 0 A-2258 H H H H H O allyl H 2,4-Me.sub.2 0 A-2259 H H H H H O allyl H 2,5-Me.sub.2 0 A-2260 H H H H H O allyl H 2,6-Me.sub.2 0 A-2261 H H H H H O allyl H 2-Me,4-CF.sub.3 0 A-2262 H H H H H O allyl H 2-Me,5-CF.sub.3 0 A-2263 H H H H H O allyl H 2-Me,6-CF.sub.3 0 A-2264 H H H H H O allyl H 2-Me,4-OMe 0 A-2265 H H H H H O allyl H 2-Me,5-OMe 0 A-2266 H H H H H O allyl H 2-Me,6-OMe 0 A-2267 H H H H H O allyl H 3-Me,6-OMe 0 A-2268 H H H H H O allyl H 4-Me,2-OMe 0 A-2269 H H H H H O allyl H 2,5-OMe.sub.2 0 A-2270 H H H H H O allyl H 2,6-OMe.sub.2 0 A-2271 H H H H H O allyl H 2-OMe,6-CF.sub.3 0 A-2272 H H H H H O allyl H 2-CHF.sub.2,5-F 0 A-2273 H H H H H O allyl H 2-CHF.sub.2,6-F 0 A-2274 H H H H H O allyl H 2-CHF.sub.2,5-Me 0 A-2275 H H H H H O allyl H 2-CHF.sub.2,6-Me 0
(142) TABLE-US-00041 TABLE 41 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2276 H H H H H O allyl H 2-cyclopropyl,5-F 0 A-2277 H H H H H O allyl H 2-cyclopropyl,6-F 0 A-2278 H H H H H O allyl H 2-cyclopropyl,5-Me 0 A-2279 H H H H H O allyl H 2-cyclopropyl,6-Me 0 A-2280 H H H H H O allyl H 2-ethenyl,6-F 0 A-2281 H H H H H O allyl H 2-ethenyl,6-Me 0 A-2282 H H H H H O allyl H 2-OEt,5-F 0 A-2283 H H H H H O allyl H 2-OEt,6-F 0 A-2284 H H H H H O allyl H 2-OEt,5-Cl 0 A-2285 H H H H H O allyl H 2-OEt,6-Cl 0 A-2286 H H H H H O allyl H 2-OEt,5-Me 0 A-2287 H H H H H O allyl H 2-OEt,6-Me 0 A-2288 H H H H H O allyl H 2-OCHF.sub.2,5-F 0 A-2289 H H H H H O allyl H 2-OCHF.sub.2,6-F 0 A-2290 H H H H H O allyl H 2-OCHF.sub.2,5-Me 0 A-2291 H H H H H O allyl H 2-OCHF.sub.2,6-Me 0 A-2292 H H H H H O allyl H 2-(cyclopropyloxy),5-F 0 A-2293 H H H H H O allyl H 2-(cyclopropyloxy),6-F 0 A-2294 H H H H H O allyl H 2-(cyclopropyloxy),5-Me 0 A-2295 H H H H H O allyl H 2-(cyclopropyloxy),6-Me 0 A-2296 H H H H H O allyl H 2-SMe,5-F 0 A-2297 H H H H H O allyl H 2-SMe,6-F 0 A-2298 H H H H H O allyl H 2-SMe,5-Me 0 A-2299 H H H H H O allyl H 2-SMe,6-Me 0 A-2300 H H H H H O allyl H 2-S(?O)Me,5-F 0 A-2301 H H H H H O allyl H 2-S(?O)Me,6-F 0 A-2302 H H H H H O allyl H 2-S(?O)Me,5-Me 0 A-2303 H H H H H O allyl H 2-S(?O)Me,6-Me 0 A-2304 H H H H H O allyl H 2-S(?O).sub.2Me,5-F 0 A-2305 H H H H H O allyl H 2-S(?O).sub.2Me,6-F 0 A-2306 H H H H H O allyl H 2-S(?O).sub.2Me,5-Me 0 A-2307 H H H H H O allyl H 2-S(?O).sub.2Me,6-Me 0 A-2308 H H H H H O allyl H 2-SCF.sub.3,5-F 0 A-2309 H H H H H O allyl H 2-SCF.sub.3,6-F 0 A-2310 H H H H H O allyl H 2-SCF.sub.3,5-Me 0 A-2311 H H H H H O allyl H 2-SCF.sub.3,6-Me 0 A-2312 H H H H H O allyl H 2-S(?O)CF.sub.3,5-F 0 A-2313 H H H H H O allyl H 2-S(?O)CF.sub.3,6-F 0 A-2314 H H H H H O allyl H 2-S(?O)CF.sub.3,5-Me 0 A-2315 H H H H H O allyl H 2-S(?O)CF.sub.3,6-Me 0 A-2316 H H H H H O allyl H 2-S(?O).sub.2CF.sub.3,5-F 0 A-2317 H H H H H O allyl H 2-S(?O).sub.2CF.sub.3,6-F 0 A-2318 H H H H H O allyl H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-2319 H H H H H O allyl H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-2320 H H H H H O allyl H 2-(cyclopropylthio),5-F 0 A-2321 H H H H H O allyl H 2-(cyclopropylthio),6-F 0 A-2322 H H H H H O allyl H 2-(cyclopropylthio),5-Me 0 A-2323 H H H H H O allyl H 2-(cyclopropylthio),6-Me 0 A-2324 H H H H H O allyl H 2-C(?O)Me,5-F 0 A-2325 H H H H H O allyl H 2-C(?O)Me,6-F 0 A-2326 H H H H H O allyl H 2-C(?O)Me,5-Me 0 A-2327 H H H H H O allyl H 2-C(?O)Me,6-Me 0 A-2328 H H H H H O allyl H 2-CH.sub.2OH,5-F 0 A-2329 H H H H H O allyl H 2-CH.sub.2OH,6-F 0 A-2330 H H H H H O allyl H 2-CH.sub.2OH,5-Me 0 A-2331 H H H H H O allyl H 2-CH.sub.2OH,6-Me 0 A-2332 H H H H H O allyl H 2-CH.sub.2OCH.sub.3,4-F 0
(143) TABLE-US-00042 TABLE 42 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2333 H H H H H O allyl H 2-CH.sub.2OCH.sub.3,5-F 0 A-2334 H H H H H O allyl H 2-CH.sub.2OCH.sub.3,6-F 0 A-2335 H H H H H O allyl H 2-CH.sub.2OCH.sub.3,4-Me 0 A-2336 H H H H H O allyl H 2-CH.sub.2OCH.sub.3,5-Me 0 A-2337 H H H H H O allyl H 2-CH.sub.2OCH.sub.3,6-Me 0 A-2338 H H H H H O allyl H 2-OC(?O)CH.sub.3,5-F 0 A-2339 H H H H H O allyl H 2-OC(?O)CH.sub.3,6-F 0 A-2340 H H H H H O allyl H 2-OC(?O)CH.sub.3,5-Me 0 A-2341 H H H H H O allyl H 2-OC(?O)CH.sub.3,6-Me 0 A-2342 H H H H H O allyl H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-2343 H H H H H O allyl H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-2344 H H H H H O allyl H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-2345 H H H H H O allyl H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-2346 H H H H H O allyl H 2-CH.sub.2SCH.sub.3,5-F 0 A-2347 H H H H H O allyl H 2-CH.sub.2SCH.sub.3,6-F 0 A-2348 H H H H H O allyl H 2-CH.sub.2SCH.sub.3,5-Me 0 A-2349 H H H H H O allyl H 2-CH.sub.2SCH.sub.3,6-Me 0 A-2350 H H H H H O allyl H 2-NMe.sub.2,5-F 0 A-2351 H H H H H O allyl H 2-NMe.sub.2,6-F 0 A-2352 H H H H H O allyl H 2-NMe.sub.2,5-Me 0 A-2353 H H H H H O allyl H 2-NMe.sub.2,6-Me 0 A-2354 H H H H H O allyl H 2-CN,4-F 0 A-2355 H H H H H O allyl H 2-CN,5-F 0 A-2356 H H H H H O allyl H 2-CN,6-F 0 A-2357 H H H H H O allyl H 2-CN,6-Me 0 A-2358 H H H H H O allyl H 2-CN,5-OMe 0 A-2359 H H H H H O allyl H 2-CN,6-OMe 0 A-2360 H H H H H O allyl H 3-CN,6-Me 0 A-2361 H H H H H O allyl H 3-CN,6-OMe 0 A-2362 H H H H H O allyl H 4-CN,2-Me 0 A-2363 H H H H H O allyl H 4-CN,2-OMe 0 A-2364 H H H H H O allyl H 2-NO.sub.2,4-F 0 A-2365 H H H H H O allyl H 2-NO.sub.2,5-F 0 A-2366 H H H H H O allyl H 2-NO.sub.2,6-F 0 A-2367 H H H H H O allyl H 2-NO.sub.2,4-Me 0 A-2368 H H H H H O allyl H 2-NO.sub.2,5-Me 0 A-2369 H H H H H O allyl H 2-NO.sub.2,6-Me 0 A-2370 H H H H H O allyl H 2-Me,4,5-F.sub.2 0 A-2371 H H H H H O allyl H 2-Me,6-Et 0 A-2372 H H H H H O allyl H 2-cyclopropyl,6-OMe 0 A-2373 H H H H H O allyl H 2-Me,5-Et 0 A-2374 H H H H H O allyl H 2,6-Et.sub.2 0 A-2375 H H H H H O allyl H 2-Et,6-F 0 A-2376 H H H H H O allyl H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-2377 H H H H H O allyl H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-2378 H H H H H O allyl H 2-CH.sub.2NMe.sub.2 0 A-2379 H H H H H O 1-cyclohexylethyl H H 0 A-2380 H H H H H O 1-cyclohexylethyl H 2-F 0 A-2381 H H H H H O 1-cyclohexylethyl H 2-Cl 0 A-2382 H H H H H O 1-cyclohexylethyl H 2-Br 0 A-2383 H H H H H O 1-cyclohexylethyl H 2-OH 0 A-2384 H H H H H O 1-cyclohexylethyl H 2-Me 0 A-2385 H H H H H O 1-cyclohexylethyl H 2-Et 0 A-2386 H H H H H O 1-cyclohexylethyl H 2-Pr 0 A-2387 H H H H H O 1-cyclohexylethyl H 2-CF.sub.3 0 A-2388 H H H H H O 1-cyclohexylethyl H 2-CHF.sub.2 0 A-2389 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2F 0
(144) TABLE-US-00043 TABLE 43 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2390 H H H H H O 1-cyclohexylethyl H 2-CF.sub.2Cl 0 A-2391 H H H H H O 1-cyclohexylethyl H 2-cyclopropyl 0 A-2392 H H H H H O 1-cyclohexylethyl H 2-cyclobutyl 0 A-2393 H H H H H O 1-cyclohexylethyl H 2-cyclopentyl 0 A-2394 H H H H H O 1-cyclohexylethyl H 2-ethenyl 0 A-2395 H H H H H O 1-cyclohexylethyl H 2-allyl 0 A-2396 H H H H H O 1-cyclohexylethyl H 2-(prop-1-en-1-yl) 0 A-2397 H H H H H O 1-cyclohexylethyl H 2-(trifluoroethenyl) 0 A-2398 H H H H H O 1-cyclohexylethyl H 2-OMe 0 A-2399 H H H H H O 1-cyclohexylethyl H 2-OEt 0 A-2400 H H H H H O 1-cyclohexylethyl H 2-OPr 0 A-2401 H H H H H O 1-cyclohexylethyl H 2-O(i-Pr) 0 A-2402 H H H H H O 1-cyclohexylethyl H 2-OCF.sub.3 0 A-2403 H H H H H O 1-cyclohexylethyl H 2-OCHF.sub.2 0 A-2404 H H H H H O 1-cyclohexylethyl H 2-(cyclopropyloxy) 0 A-2405 H H H H H O 1-cyclohexylethyl H 2-(cyclobutyloxy) 0 A-2406 H H H H H O 1-cyclohexylethyl H 2-(cyclopentyloxy) 0 A-2407 H H H H H O 1-cyclohexylethyl H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-2408 H H H H H O 1-cyclohexylethyl H 2-(oxiran-2-yl) 0 A-2409 H H H H H O 1-cyclohexylethyl H 2-SMe 0 A-2410 H H H H H O 1-cyclohexylethyl H 3-SMe 0 A-2411 H H H H H O 1-cyclohexylethyl H 2-S(?O)Me 0 A-2412 H H H H H O 1-cyclohexylethyl H 3-S(?O)Me 0 A-2413 H H H H H O 1-cyclohexylethyl H 2-S(?O).sub.2Me 0 A-2414 H H H H H O 1-cyclohexylethyl H 3-S(?O).sub.2Me 0 A-2415 H H H H H O 1-cyclohexylethyl H 2-SCF.sub.3 0 A-2416 H H H H H O 1-cyclohexylethyl H 3-SCF.sub.3 0 A-2417 H H H H H O 1-cyclohexylethyl H 3-S(?O)CF.sub.3 0 A-2418 H H H H H O 1-cyclohexylethyl H 3-SCF(CF.sub.3).sub.2 0 A-2419 H H H H H O 1-cyclohexylethyl H 2-(cyclopropylthio) 0 A-2420 H H H H H O 1-cyclohexylethyl H 2-(cyclopropylsulfinyl) 0 A-2421 H H H H H O 1-cyclohexylethyl H 2-(cyclopropylsulfonyl) 0 A-2422 H H H H H O 1-cyclohexylethyl H 2-C(?O)Me 0 A-2423 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2C(?O)CH.sub.3 0 A-2424 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2C(?O)CF.sub.3 0 A-2425 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2OH 0 A-2426 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2OCH.sub.3 0 A-2427 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-2428 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2SCH.sub.3 0 A-2429 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2S(?O)CH.sub.3 0 A-2430 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-2431 H H H H H O 1-cyclohexylethyl H 2-(benzyloxy) 0 A-2432 H H H H H O 1-cyclohexylethyl H 2-NH.sub.2 0 A-2433 H H H H H O 1-cyclohexylethyl H 2-NHMe 0 A-2434 H H H H H O 1-cyclohexylethyl H 2-N(Me).sub.2 0 A-2435 H H H H H O 1-cyclohexylethyl H 2-(1,3-dioxolan-2-yl) 0 A-2436 H H H H H O 1-cyclohexylethyl H 2-(1,3-dioxan-2-yl) 0 A-2437 H H H H H O 1-cyclohexylethyl H 2-(1H-imidazol-2-yl) 0 A-2438 H H H H H O 1-cyclohexylethyl H 2-(thiazol-2-yl) 0 A-2439 H H H H H O 1-cyclohexylethyl H 2-(oxazol-2-yl) 0 A-2440 H H H H H O 1-cyclohexylethyl H 2-CH?NOH 0 A-2441 H H H H H O 1-cyclohexylethyl H 2-CH?NOMe 0 A-2442 H H H H H O 1-cyclohexylethyl H 2-(4,5-dihydro-3-isoxazolyl) 0 A-2443 H H H H H O 1-cyclohexylethyl H 2-CN 0 A-2444 H H H H H O 1-cyclohexylethyl H 2-NO.sub.2 0 A-2445 H H H H H O 1-cyclohexylethyl H 2-F,6-Cl 0 A-2446 H H H H H O 1-cyclohexylethyl H 2-F,6-Me 0
(145) TABLE-US-00044 TABLE 44 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2447 H H H H H O 1-cyclohexylethyl H 3-F,6-Me 0 A-2448 H H H H H O 1-cyclohexylethyl H 4-F,2-Me 0 A-2449 H H H H H O 1-cyclohexylethyl H 2-F,6-OMe 0 A-2450 H H H H H O 1-cyclohexylethyl H 3-F,6-OMe 0 A-2451 H H H H H O 1-cyclohexylethyl H 2,6-Cl.sub.2 0 A-2452 H H H H H O 1-cyclohexylethyl H 2-Cl,6-Me 0 A-2453 H H H H H O 1-cyclohexylethyl H 3-Cl,6-Me 0 A-2454 H H H H H O 1-cyclohexylethyl H 4-Cl,2-Me 0 A-2455 H H H H H O 1-cyclohexylethyl H 2-Cl,5-CF.sub.3 0 A-2456 H H H H H O 1-cyclohexylethyl H 2-Cl,6-CF.sub.3 0 A-2457 H H H H H O 1-cyclohexylethyl H 2-Cl,6-OMe 0 A-2458 H H H H H O 1-cyclohexylethyl H 3-Cl,6-OMe 0 A-2459 H H H H H O 1-cyclohexylethyl H 4-Cl,2-OMe 0 A-2460 H H H H H O 1-cyclohexylethyl H 2,4-Me.sub.2 0 A-2461 H H H H H O 1-cyclohexylethyl H 2,5-Me.sub.2 0 A-2462 H H H H H O 1-cyclohexylethyl H 2,6-Me.sub.2 0 A-2463 H H H H H O 1-cyclohexylethyl H 2-Me,4-CF.sub.3 0 A-2464 H H H H H O 1-cyclohexylethyl H 2-Me,5-CF.sub.3 0 A-2465 H H H H H O 1-cyclohexylethyl H 2-Me,6-CF.sub.3 0 A-2466 H H H H H O 1-cyclohexylethyl H 2-Me,4-OMe 0 A-2467 H H H H H O 1-cyclohexylethyl H 2-Me,5-OMe 0 A-2468 H H H H H O 1-cyclohexylethyl H 2-Me,6-OMe 0 A-2469 H H H H H O 1-cyclohexylethyl H 3-Me,6-OMe 0 A-2470 H H H H H O 1-cyclohexylethyl H 4-Me,2-OMe 0 A-2471 H H H H H O 1-cyclohexylethyl H 2,5-OMe.sub.2 0 A-2472 H H H H H O 1-cyclohexylethyl H 2,6-OMe.sub.2 0 A-2473 H H H H H O 1-cyclohexylethyl H 2-OMe,6-CF.sub.3 0 A-2474 H H H H H O 1-cyclohexylethyl H 2-CHF.sub.2,5-F 0 A-2475 H H H H H O 1-cyclohexylethyl H 2-CHF.sub.2,6-F 0 A-2476 H H H H H O 1-cyclohexylethyl H 2-CHF.sub.2,5-Me 0 A-2477 H H H H H O 1-cyclohexylethyl H 2-CHF.sub.2,6-Me 0 A-2478 H H H H H O 1-cyclohexylethyl H 2-cyclopropyl,5-F 0 A-2479 H H H H H O 1-cyclohexylethyl H 2-cyclopropyl,6-F 0 A-2480 H H H H H O 1-cyclohexylethyl H 2-cyclopropyl,5-Me 0 A-2481 H H H H H O 1-cyclohexylethyl H 2-cyclopropyl,6-Me 0 A-2482 H H H H H O 1-cyclohexylethyl H 2-ethenyl,6-F 0 A-2483 H H H H H O 1-cyclohexylethyl H 2-ethenyl,6-Me 0 A-2484 H H H H H O 1-cyclohexylethyl H 2-OEt,5-F 0 A-2485 H H H H H O 1-cyclohexylethyl H 2-OEt,6-F 0 A-2486 H H H H H O 1-cyclohexylethyl H 2-OEt,5-Cl 0 A-2487 H H H H H O 1-cyclohexylethyl H 2-OEt,6-Cl 0 A-2488 H H H H H O 1-cyclohexylethyl H 2-OEt,5-Me 0 A-2489 H H H H H O 1-cyclohexylethyl H 2-OEt,6-Me 0 A-2490 H H H H H O 1-cyclohexylethyl H 2-OCHF.sub.2,5-F 0 A-2491 H H H H H O 1-cyclohexylethyl H 2-OCHF.sub.2,6-F 0 A-2492 H H H H H O 1-cyclohexylethyl H 2-OCHF.sub.2,5-Me 0 A-2493 H H H H H O 1-cyclohexylethyl H 2-OCHF.sub.2,6-Me 0 A-2494 H H H H H O 1-cyclohexylethyl H 2-(cyclopropyloxy),5-F 0 A-2495 H H H H H O 1-cyclohexylethyl H 2-(cyclopropyloxy),6-F 0 A-2496 H H H H H O 1-cyclohexylethyl H 2-(cyclopropyloxy),5-Me 0 A-2497 H H H H H O 1-cyclohexylethyl H 2-(cyclopropyloxy),6-Me 0 A-2498 H H H H H O 1-cyclohexylethyl H 2-SMe,5-F 0 A-2499 H H H H H O 1-cyclohexylethyl H 2-SMe,6-F 0 A-2500 H H H H H O 1-cyclohexylethyl H 2-SMe,5-Me 0 A-2501 H H H H H O 1-cyclohexylethyl H 2-SMe,6-Me 0 A-2502 H H H H H O 1-cyclohexylethyl H 2-S(?O)Me,5-F 0 A-2503 H H H H H O 1-cyclohexylethyl H 2-S(?O)Me,6-F 0
(146) TABLE-US-00045 TABLE 45 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2504 H H H H H O 1-cyclohexylethyl H 2-S(?O)Me,5-Me 0 A-2505 H H H H H O 1-cyclohexylethyl H 2-S(?O)Me,6-Me 0 A-2506 H H H H H O 1-cyclohexylethyl H 2-S(?O).sub.2Me,5-F 0 A-2507 H H H H H O 1-cyclohexylethyl H 2-S(?O).sub.2Me,6-F 0 A-2508 H H H H H O 1-cyclohexylethyl H 2-S(?O).sub.2Me,5-Me 0 A-2509 H H H H H O 1-cyclohexylethyl H 2-S(?O).sub.2Me,6-Me 0 A-2510 H H H H H O 1-cyclohexylethyl H 2-SCF.sub.3,5-F 0 A-2511 H H H H H O 1-cyclohexylethyl H 2-SCF.sub.3,6-F 0 A-2512 H H H H H O 1-cyclohexylethyl H 2-SCF.sub.3,5-Me 0 A-2513 H H H H H O 1-cyclohexylethyl H 2-SCF.sub.3,6-Me 0 A-2514 H H H H H O 1-cyclohexylethyl H 2-S(?O)CF.sub.3,5-F 0 A-2515 H H H H H O 1-cyclohexylethyl H 2-S(?O)CF.sub.3,6-F 0 A-2516 H H H H H O 1-cyclohexylethyl H 2-S(?O)CF.sub.3,5-Me 0 A-2517 H H H H H O 1-cyclohexylethyl H 2-S(?O)CF.sub.3,6-Me 0 A-2518 H H H H H O 1-cyclohexylethyl H 2-S(?O).sub.2CF.sub.3,5-F 0 A-2519 H H H H H O 1-cyclohexylethyl H 2-S(?O).sub.2CF.sub.3,6-F 0 A-2520 H H H H H O 1-cyclohexylethyl H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-2521 H H H H H O 1-cyclohexylethyl H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-2522 H H H H H O 1-cyclohexylethyl H 2-(cyclopropylthio),5-F 0 A-2523 H H H H H O 1-cyclohexylethyl H 2-(cyclopropylthio),6-F 0 A-2524 H H H H H O 1-cyclohexylethyl H 2-(cyclopropylthio),5-Me 0 A-2525 H H H H H O 1-cyclohexylethyl H 2-(cyclopropylthio),6-Me 0 A-2526 H H H H H O 1-cyclohexylethyl H 2-C(?O)Me,5-F 0 A-2527 H H H H H O 1-cyclohexylethyl H 2-C(?O)Me,6-F 0 A-2528 H H H H H O 1-cyclohexylethyl H 2-C(?O)Me,5-Me 0 A-2529 H H H H H O 1-cyclohexylethyl H 2-C(?O)Me,6-Me 0 A-2530 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2OH,5-F 0 A-2531 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2OH,6-F 0 A-2532 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2OH,5-Me 0 A-2533 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2OH,6-Me 0 A-2534 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2OCH.sub.3,4-F 0 A-2535 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2OCH.sub.3,5-F 0 A-2536 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2OCH.sub.3,6-F 0 A-2537 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2OCH.sub.3,4-Me 0 A-2538 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2OCH.sub.3,5-Me 0 A-2539 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2OCH.sub.3,6-Me 0 A-2540 H H H H H O 1-cyclohexylethyl H 2-OC(?O)CH.sub.3,5-F 0 A-2541 H H H H H O 1-cyclohexylethyl H 2-OC(?O)CH.sub.3,6-F 0 A-2542 H H H H H O 1-cyclohexylethyl H 2-OC(?O)CH.sub.3,5-Me 0 A-2543 H H H H H O 1-cyclohexylethyl H 2-OC(?O)CH.sub.3,6-Me 0 A-2544 H H H H H O 1-cyclohexylethyl H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-2545 H H H H H O 1-cyclohexylethyl H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-2546 H H H H H O 1-cyclohexylethyl H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-2547 H H H H H O 1-cyclohexylethyl H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-2548 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2SCH.sub.3,5-F 0 A-2549 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2SCH.sub.3,6-F 0 A-2550 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2SCH.sub.3,5-Me 0 A-2551 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2SCH.sub.3,6-Me 0 A-2552 H H H H H O 1-cyclohexylethyl H 2-NMe.sub.2,5-F 0 A-2553 H H H H H O 1-cyclohexylethyl H 2-NMe.sub.2,6-F 0 A-2554 H H H H H O 1-cyclohexylethyl H 2-NMe.sub.2,5-Me 0 A-2555 H H H H H O 1-cyclohexylethyl H 2-NMe.sub.2,6-Me 0 A-2556 H H H H H O 1-cyclohexylethyl H 2-CN,4-F 0 A-2557 H H H H H O 1-cyclohexylethyl H 2-CN,5-F 0 A-2558 H H H H H O 1-cyclohexylethyl H 2-CN,6-F 0 A-2559 H H H H H O 1-cyclohexylethyl H 2-CN,6-Me 0 A-2560 H H H H H O 1-cyclohexylethyl H 2-CN,5-OMe 0
(147) TABLE-US-00046 TABLE 46 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2561 H H H H H O 1-cyclohexylethyl H 2-CN,6-Me 0 A-2562 H H H H H O 1-cyclohexylethyl H 3-CN,6-Me 0 A-2563 H H H H H O 1-cyclohexylethyl H 3-CN,6-OMe 0 A-2564 H H H H H O 1-cyclohexylethyl H 4-CN,2-Me 0 A-2565 H H H H H O 1-cyclohexylethyl H 4-CN,2-OMe 0 A-2566 H H H H H O 1-cyclohexylethyl H 2-NO.sub.2,4-F 0 A-2567 H H H H H O 1-cyclohexylethyl H 2-NO.sub.2,5-F 0 A-2568 H H H H H O 1-cyclohexylethyl H 2-NO.sub.2,6-F 0 A-2569 H H H H H O 1-cyclohexylethyl H 2-NO.sub.2,4-Me 0 A-2570 H H H H H O 1-cyclohexylethyl H 2-NO.sub.2,5-Me 0 A-2571 H H H H H O 1-cyclohexylethyl H 2-NO.sub.2,6-Me 0 A-2572 H H H H H O 1-cyclohexylethyl H 2-Me,4,5-F.sub.2 0 A-2573 H H H H H O 1-cyclohexylethyl H 2-Me,6-Et 0 A-2574 H H H H H O 1-cyclohexylethyl H 2-cyclopropyl,6-OMe 0 A-2575 H H H H H O 1-cyclohexylethyl H 2-Me,5-Et 0 A-2576 H H H H H O 1-cyclohexylethyl H 2,6-Et.sub.2 0 A-2577 H H H H H O 1-cyclohexylethyl H 2-Et,6-F 0 A-2578 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-2579 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-2580 H H H H H O 1-cyclohexylethyl H 2-CH.sub.2NMe.sub.2 0 A-2581 H H H H H O CH.sub.2C?CH H H 0 A-2582 H H H H H O CH.sub.2C?CH H 2-F 0 A-2583 H H H H H O CH.sub.2C?CH H 2-Cl 0 A-2584 H H H H H O CH.sub.2C?CH H 2-Br 0 A-2585 H H H H H O CH.sub.2C?CH H 2-OH 0 A-2586 H H H H H O CH.sub.2C?CH H 2-Me 0 A-2587 H H H H H O CH.sub.2C?CH H 2-Et 0 A-2588 H H H H H O CH.sub.2C?CH H 2-Pr 0 A-2589 H H H H H O CH.sub.2C?CH H 2-CF.sub.3 0 A-2590 H H H H H O CH.sub.2C?CH H 2-CHF.sub.2 0 A-2591 H H H H H O CH.sub.2C?CH H 2-CH.sub.2F 0 A-2592 H H H H H O CH.sub.2C?CH H 2-CF.sub.2Cl 0 A-2593 H H H H H O CH.sub.2C?CH H 2-cyclopropyl 0 A-2594 H H H H H O CH.sub.2C?CH H 2-cyclobutyl 0 A-2595 H H H H H O CH.sub.2C?CH H 2-cyclopentyl 0 A-2596 H H H H H O CH.sub.2C?CH H 2-ethenyl 0 A-2597 H H H H H O CH.sub.2C?CH H 2-allyl 0 A-2598 H H H H H O CH.sub.2C?CH H 2-(prop-1-en-1-yl) 0 A-2599 H H H H H O CH.sub.2C?CH H 2-(trifluoroethenyl) 0 A-2600 H H H H H O CH.sub.2C?CH H 2-OMe 0 A-2601 H H H H H O CH.sub.2C?CH H 2-OEt 0 A-2602 H H H H H O CH.sub.2C?CH H 2-OPr 0 A-2603 H H H H H O CH.sub.2C?CH H 2-O(i-Pr) 0 A-2604 H H H H H O CH.sub.2C?CH H 2-OCF.sub.3 0 A-2605 H H H H H O CH.sub.2C?CH H 2-OCHF.sub.2 0 A-2606 H H H H H O CH.sub.2C?CH H 2-(cyclopropyloxy) 0 A-2607 H H H H H O CH.sub.2C?CH H 2-(cyclobutyloxy) 0 A-2608 H H H H H O CH.sub.2C?CH H 2-(cyclopentyloxy) 0 A-2609 H H H H H O CH.sub.2C?CH H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-2610 H H H H H O CH.sub.2C?CH H 2-(oxiran-2-yl) 0 A-2611 H H H H H O CH.sub.2C?CH H 2-SMe 0 A-2612 H H H H H O CH.sub.2C?CH H 3-SMe 0 A-2613 H H H H H O CH.sub.2C?CH H 2-S(?O)Me 0 A-2614 H H H H H O CH.sub.2C?CH H 3-S(?O)Me 0 A-2615 H H H H H O CH.sub.2C?CH H 2-S(?O).sub.2Me 0 A-2616 H H H H H O CH.sub.2C?CH H 3-S(?O).sub.2Me 0 A-2617 H H H H H O CH.sub.2C?CH H 2-SCF.sub.3 0
(148) TABLE-US-00047 TABLE 47 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2618 H H H H H O CH.sub.2C?CH H 3-SCF.sub.3 0 A-2619 H H H H H O CH.sub.2C?CH H 3-S(?O)CF.sub.3 0 A-2620 H H H H H O CH.sub.2C?CH H 3-SCF(CF.sub.3).sub.2 0 A-2621 H H H H H O CH.sub.2C?CH H 2-(cyclopropylthio) 0 A-2622 H H H H H O CH.sub.2C?CH H 2-(cyclopropylsulfinyl) 0 A-2623 H H H H H O CH.sub.2C?CH H 2-(cyclopropylsulfonyl) 0 A-2624 H H H H H O CH.sub.2C?CH H 2-C(?O)Me 0 A-2625 H H H H H O CH.sub.2C?CH H 2-CH.sub.2C(?O)CH.sub.3 0 A-2626 H H H H H O CH.sub.2C?CH H 2-CH.sub.2C(?O)CF.sub.3 0 A-2627 H H H H H O CH.sub.2C?CH H 2-CH.sub.2OH 0 A-2628 H H H H H O CH.sub.2C?CH H 2-CH.sub.2OCH.sub.3 0 A-2629 H H H H H O CH.sub.2C?CH H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-2630 H H H H H O CH.sub.2C?CH H 2-CH.sub.2SCH.sub.3 0 A-2631 H H H H H O CH.sub.2C?CH H 2-CH.sub.2S(?O)CH.sub.3 0 A-2632 H H H H H O CH.sub.2C?CH H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-2633 H H H H H O CH.sub.2C?CH H 2-(benzyloxy) 0 A-2634 H H H H H O CH.sub.2C?CH H 2-NH.sub.2 0 A-2635 H H H H H O CH.sub.2C?CH H 2-NHMe 0 A-2636 H H H H H O CH.sub.2C?CH H 2-N(Me).sub.2 0 A-2637 H H H H H O CH.sub.2C?CH H 2-(1,3-dioxolan-2-yl) 0 A-2638 H H H H H O CH.sub.2C?CH H 2-(1,3-dioxan-2-yl) 0 A-2639 H H H H H O CH.sub.2C?CH H 2-(1H-imidazol-2-yl) 0 A-2640 H H H H H O CH.sub.2C?CH H 2-(thiazol-2-yl) 0 A-2641 H H H H H O CH.sub.2C?CH H 2-(oxazol-2-yl) 0 A-2642 H H H H H O CH.sub.2C?CH H 2-CH?NOH 0 A-2643 H H H H H O CH.sub.2C?CH H 2-CH?NOMe 0 A-2644 H H H H H O CH.sub.2C?CH H 2-(4,5-dihydro-3-isoxazolyl) 0 A-2645 H H H H H O CH.sub.2C?CH H 2-CN 0 A-2646 H H H H H O CH.sub.2C?CH H 2-NO.sub.2 0 A-2647 H H H H H O CH.sub.2C?CH H 2-F,6-Cl 0 A-2648 H H H H H O CH.sub.2C?CH H 2-F,6-Me 0 A-2649 H H H H H O CH.sub.2C?CH H 3-F,6-Me 0 A-2650 H H H H H O CH.sub.2C?CH H 4-F,2-Me 0 A-2651 H H H H H O CH.sub.2C?CH H 2-F,6-OMe 0 A-2652 H H H H H O CH.sub.2C?CH H 3-F,6-OMe 0 A-2653 H H H H H O CH.sub.2C?CH H 2,6-Cl.sub.2 0 A-2654 H H H H H O CH.sub.2C?CH H 2-Cl,6-Me 0 A-2655 H H H H H O CH.sub.2C?CH H 3-Cl,6-Me 0 A-2656 H H H H H O CH.sub.2C?CH H 4-Cl,2-Me 0 A-2657 H H H H H O CH.sub.2C?CH H 2-Cl,5-CF.sub.3 0 A-2658 H H H H H O CH.sub.2C?CH H 2-Cl,6-CF.sub.3 0 A-2659 H H H H H O CH.sub.2C?CH H 2-Cl,6-OMe 0 A-2660 H H H H H O CH.sub.2C?CH H 3-Cl,6-OMe 0 A-2661 H H H H H O CH.sub.2C?CH H 4-Cl,2-OMe 0 A-2662 H H H H H O CH.sub.2C?CH H 2,4-Me.sub.2 0 A-2663 H H H H H O CH.sub.2C?CH H 2,5-Me.sub.2 0 A-2664 H H H H H O CH.sub.2C?CH H 2,6-Me.sub.2 0 A-2665 H H H H H O CH.sub.2C?CH H 2-Me,4-CF.sub.3 0 A-2666 H H H H H O CH.sub.2C?CH H 2-Me,5-CF.sub.3 0 A-2667 H H H H H O CH.sub.2C?CH H 2-Me,6-CF.sub.3 0 A-2668 H H H H H O CH.sub.2C?CH H 2-Me,4-OMe 0 A-2669 H H H H H O CH.sub.2C?CH H 2-Me,5-OMe 0 A-2670 H H H H H O CH.sub.2C?CH H 2-Me,6-OMe 0 A-2671 H H H H H O CH.sub.2C?CH H 3-Me,6-OMe 0 A-2672 H H H H H O CH.sub.2C?CH H 4-Me,2-OMe 0 A-2673 H H H H H O CH.sub.2C?CH H 2,5-OMe.sub.2 0 A-2674 H H H H H O CH.sub.2C?CH H 2,6-OMe.sub.2 0
(149) TABLE-US-00048 TABLE 48 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2675 H H H H H O CH.sub.2C?CH H 2-OMe,6-CF.sub.3 0 A-2676 H H H H H O CH.sub.2C?CH H 2-CHF.sub.2,5-F 0 A-2677 H H H H H O CH.sub.2C?CH H 2-CHF.sub.2,6-F 0 A-2678 H H H H H O CH.sub.2C?CH H 2-CHF.sub.2,5-Me 0 A-2679 H H H H H O CH.sub.2C?CH H 2-CHF.sub.2,6-Me 0 A-2680 H H H H H O CH.sub.2C?CH H 2-cyclopropyl,5-F 0 A-2681 H H H H H O CH.sub.2C?CH H 2-cyclopropyl,6-F 0 A-2682 H H H H H O CH.sub.2C?CH H 2-cyclopropyl,5-Me 0 A-2683 H H H H H O CH.sub.2C?CH H 2-cyclopropyl,6-Me 0 A-2684 H H H H H O CH.sub.2C?CH H 2-ethenyl,6-F 0 A-2685 H H H H H O CH.sub.2C?CH H 2-ethenyl,6-Me 0 A-2686 H H H H H O CH.sub.2C?CH H 2-OEt,5-F 0 A-2687 H H H H H O CH.sub.2C?CH H 2-OEt,6-F 0 A-2688 H H H H H O CH.sub.2C?CH H 2-OEt,5-Cl 0 A-2689 H H H H H O CH.sub.2C?CH H 2-OEt,6-Cl 0 A-2690 H H H H H O CH.sub.2C?CH H 2-OEt,5-Me 0 A-2691 H H H H H O CH.sub.2C?CH H 2-OEt,6-Me 0 A-2692 H H H H H O CH.sub.2C?CH H 2-OCHF.sub.2,5-F 0 A-2693 H H H H H O CH.sub.2C?CH H 2-OCHF.sub.2,6-F 0 A-2694 H H H H H O CH.sub.2C?CH H 2-OCHF.sub.2,5-Me 0 A-2695 H H H H H O CH.sub.2C?CH H 2-OCHF.sub.2,6-Me 0 A-2696 H H H H H O CH.sub.2C?CH H 2-(cyclopropyloxy),5-F 0 A-2697 H H H H H O CH.sub.2C?CH H 2-(cyclopropyloxy),6-F 0 A-2698 H H H H H O CH.sub.2C?CH H 2-(cyclopropyloxy),5-Me 0 A-2699 H H H H H O CH.sub.2C?CH H 2-(cyclopropyloxy),6-Me 0 A-2700 H H H H H O CH.sub.2C?CH H 2-SMe,5-F 0 A-2701 H H H H H O CH.sub.2C?CH H 2-SMe,6-F 0 A-2702 H H H H H O CH.sub.2C?CH H 2-SMe,5-Me 0 A-2703 H H H H H O CH.sub.2C?CH H 2-SMe,6-Me 0 A-2704 H H H H H O CH.sub.2C?CH H 2-S(?O)Me,5-F 0 A-2705 H H H H H O CH.sub.2C?CH H 2-S(?O)Me,6-F 0 A-2706 H H H H H O CH.sub.2C?CH H 2-S(?O)Me,5-Me 0 A-2707 H H H H H O CH.sub.2C?CH H 2-S(?O)Me,6-Me 0 A-2708 H H H H H O CH.sub.2C?CH H 2-S(?O).sub.2Me,5-F 0 A-2709 H H H H H O CH.sub.2C?CH H 2-S(?O).sub.2Me,6-F 0 A-2710 H H H H H O CH.sub.2C?CH H 2-S(?O).sub.2Me,5-Me 0 A-2711 H H H H H O CH.sub.2C?CH H 2-S(?O).sub.2Me,6-Me 0 A-2712 H H H H H O CH.sub.2C?CH H 2-SCF.sub.3,5-F 0 A-2713 H H H H H O CH.sub.2C?CH H 2-SCF.sub.3,6-F 0 A-2714 H H H H H O CH.sub.2C?CH H 2-SCF.sub.3,5-Me 0 A-2715 H H H H H O CH.sub.2C?CH H 2-SCF.sub.3,6-Me 0 A-2716 H H H H H O CH.sub.2C?CH H 2-S(?O)CF.sub.3,5-F 0 A-2717 H H H H H O CH.sub.2C?CH H 2-S(?O)CF.sub.3,6-F 0 A-2718 H H H H H O CH.sub.2C?CH H 2-S(?O)CF.sub.3,5-Me 0 A-2719 H H H H H O CH.sub.2C?CH H 2-S(?O)CF.sub.3,6-Me 0 A-2720 H H H H H O CH.sub.2C?CH H 2-S(?O).sub.2CF.sub.3,5-F 0 A-2721 H H H H H O CH.sub.2C?CH H 2-S(?O).sub.2CF.sub.3,6-F 0 A-2722 H H H H H O CH.sub.2C?CH H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-2723 H H H H H O CH.sub.2C?CH H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-2724 H H H H H O CH.sub.2C?CH H 2-(cyclopropylthio),5-F 0 A-2725 H H H H H O CH.sub.2C?CH H 2-(cyclopropylthio),6-F 0 A-2726 H H H H H O CH.sub.2C?CH H 2-(cyclopropylthio),5-Me 0 A-2727 H H H H H O CH.sub.2C?CH H 2-(cyclopropylthio),6-Me 0 A-2728 H H H H H O CH.sub.2C?CH H 2-C(?O)Me,5-F 0 A-2729 H H H H H O CH.sub.2C?CH H 2-C(?O)Me,6-F 0 A-2730 H H H H H O CH.sub.2C?CH H 2-C(?O)Me,5-Me 0 A-2731 H H H H H O CH.sub.2C?CH H 2-C(?O)Me,6-Me 0
(150) TABLE-US-00049 TABLE 49 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2732 H H H H H O CH.sub.2C?CH H 2-CH.sub.2OH,5-F 0 A-2733 H H H H H O CH.sub.2C?CH H 2-CH.sub.2OH,6-F 0 A-2734 H H H H H O CH.sub.2C?CH H 2-CH.sub.2OH,5-Me 0 A-2735 H H H H H O CH.sub.2C?CH H 2-CH.sub.2OH,6-Me 0 A-2736 H H H H H O CH.sub.2C?CH H 2-CH.sub.2OCH.sub.3,4-F 0 A-2737 H H H H H O CH.sub.2C?CH H 2-CH.sub.2OCH.sub.3,5-F 0 A-2738 H H H H H O CH.sub.2C?CH H 2-CH.sub.2OCH.sub.3,6-F 0 A-2739 H H H H H O CH.sub.2C?CH H 2-CH.sub.2OCH.sub.3,4-Me 0 A-2740 H H H H H O CH.sub.2C?CH H 2-CH.sub.2OCH.sub.3,5-Me 0 A-2741 H H H H H O CH.sub.2C?CH H 2-CH.sub.2OCH.sub.3,6-Me 0 A-2742 H H H H H O CH.sub.2C?CH H 2-OC(?O)CH.sub.3,5-F 0 A-2743 H H H H H O CH.sub.2C?CH H 2-OC(?O)CH.sub.3,6-F 0 A-2744 H H H H H O CH.sub.2C?CH H 2-OC(?O)CH.sub.3,5-Me 0 A-2745 H H H H H O CH.sub.2C?CH H 2-OC(?O)CH.sub.3,6-Me 0 A-2746 H H H H H O CH.sub.2C?CH H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-2747 H H H H H O CH.sub.2C?CH H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-2748 H H H H H O CH.sub.2C?CH H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-2749 H H H H H O CH.sub.2C?CH H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-2750 H H H H H O CH.sub.2C?CH H 2-CH.sub.2SCH.sub.3,5-F 0 A-2751 H H H H H O CH.sub.2C?CH H 2-CH.sub.2SCH.sub.3,6-F 0 A-2752 H H H H H O CH.sub.2C?CH H 2-CH.sub.2SCH.sub.3,5-Me 0 A-2753 H H H H H O CH.sub.2C?CH H 2-CH.sub.2SCH.sub.3,6-Me 0 A-2754 H H H H H O CH.sub.2C?CH H 2-NMe.sub.2,5-F 0 A-2755 H H H H H O CH.sub.2C?CH H 2-NMe.sub.2,6-F 0 A-2756 H H H H H O CH.sub.2C?CH H 2-NMe.sub.2,5-Me 0 A-2757 H H H H H O CH.sub.2C?CH H 2-NMe.sub.2,6-Me 0 A-2758 H H H H H O CH.sub.2C?CH H 2-CN,4-F 0 A-2759 H H H H H O CH.sub.2C?CH H 2-CN,5-F 0 A-2760 H H H H H O CH.sub.2C?CH H 2-CN,6-F 0 A-2761 H H H H H O CH.sub.2C?CH H 2-CN,6-Me 0 A-2762 H H H H H O CH.sub.2C?CH H 2-CN,5-OMe 0 A-2763 H H H H H O CH.sub.2C?CH H 2-CN,6-OMe 0 A-2764 H H H H H O CH.sub.2C?CH H 3-CN,6-Me 0 A-2765 H H H H H O CH.sub.2C?CH H 3-CN,6-OMe 0 A-2766 H H H H H O CH.sub.2C?CH H 4-CN,2-Me 0 A-2767 H H H H H O CH.sub.2C?CH H 4-CN,2-OMe 0 A-2768 H H H H H O CH.sub.2C?CH H 2-NO.sub.2,4-F 0 A-2769 H H H H H O CH.sub.2C?CH H 2-NO.sub.2,5-F 0 A-2770 H H H H H O CH.sub.2C?CH H 2-NO.sub.2,6-F 0 A-2771 H H H H H O CH.sub.2C?CH H 2-NO.sub.2,4-Me 0 A-2772 H H H H H O CH.sub.2C?CH H 2-NO.sub.2,5-Me 0 A-2773 H H H H H O CH.sub.2C?CH H 2-NO.sub.2,6-Me 0 A-2774 H H H H H O CH.sub.2C?CH H 2-Me,4,5-F.sub.2 0 A-2775 H H H H H O CH.sub.2C?CH H 2-Me,6-Et 0 A-2776 H H H H H O CH.sub.2C?CH H 2-cyclopropyl,6-OMe 0 A-2777 H H H H H O CH.sub.2C?CH H 2-Me,5-Et 0 A-2778 H H H H H O CH.sub.2C?CH H 2,6-Et.sub.2 0 A-2779 H H H H H O CH.sub.2C?CH H 2-Et,6-F 0 A-2780 H H H H H O CH.sub.2C?CH H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-2781 H H H H H O CH.sub.2C?CH H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-2782 H H H H H O CH.sub.2C?CH H 2-CH.sub.2NMe.sub.2 0 A-2783 H H H H H O OH H H 0 A-2784 H H H H H O OH H 2-F 0 A-2785 H H H H H O OH H 2-Cl 0 A-2786 H H H H H O OH H 2-Br 0 A-2787 H H H H H O OH H 2-OH 0 A-2788 H H H H H O OH H 2-Me 0
(151) TABLE-US-00050 TABLE 50 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2789 H H H H H O OH H 2-Et 0 A-2790 H H H H H O OH H 2-Pr 0 A-2791 H H H H H O OH H 2-CF.sub.3 0 A-2792 H H H H H O OH H 2-CHF.sub.2 0 A-2793 H H H H H O OH H 2-CH.sub.2F 0 A-2794 H H H H H O OH H 2-CF.sub.2Cl 0 A-2795 H H H H H O OH H 2-cyclopropyl 0 A-2796 H H H H H O OH H 2-cyclobutyl 0 A-2797 H H H H H O OH H 2-cyclopentyl 0 A-2798 H H H H H O OH H 2-ethenyl 0 A-2799 H H H H H O OH H 2-allyl 0 A-2800 H H H H H O OH H 2-(prop-1-en-1-yl) 0 A-2801 H H H H H O OH H 2-(trifluoroethenyl) 0 A-2802 H H H H H O OH H 2-OMe 0 A-2803 H H H H H O OH H 2-OEt 0 A-2804 H H H H H O OH H 2-OPr 0 A-2805 H H H H H O OH H 2-O(i-Pr) 0 A-2806 H H H H H O OH H 2-OCF.sub.3 0 A-2807 H H H H H O OH H 2-OCHF.sub.2 0 A-2808 H H H H H O OH H 2-(cyclopropyloxy) 0 A-2809 H H H H H O OH H 2-(cyclobutyloxy) 0 A-2810 H H H H H O OH H 2-(cyclopentyloxy) 0 A-2811 H H H H H O OH H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-2812 H H H H H O OH H 2-(oxiran-2-yl) 0 A-2813 H H H H H O OH H 2-SMe 0 A-2814 H H H H H O OH H 3-SMe 0 A-2815 H H H H H O OH H 2-S(?O)Me 0 A-2816 H H H H H O OH H 3-S(?O)Me 0 A-2817 H H H H H O OH H 2-S(?O).sub.2Me 0 A-2818 H H H H H O OH H 3-S(?O).sub.2Me 0 A-2819 H H H H H O OH H 2-SCF.sub.3 0 A-2820 H H H H H O OH H 3-SCF.sub.3 0 A-2821 H H H H H O OH H 3-S(?O)CF.sub.3 0 A-2822 H H H H H O OH H 3-SCF(CF.sub.3).sub.2 0 A-2823 H H H H H O OH H 2-(cyclopropylthio) 0 A-2824 H H H H H O OH H 2-(cyclopropylsulfinyl) 0 A-2825 H H H H H O OH H 2-(cyclopropylsulfonyl) 0 A-2826 H H H H H O OH H 2-C(?O)Me 0 A-2827 H H H H H O OH H 2-CH.sub.2C(?O)CH.sub.3 0 A-2828 H H H H H O OH H 2-CH.sub.2C(?O)CF.sub.3 0 A-2829 H H H H H O OH H 2-CH.sub.2OH 0 A-2830 H H H H H O OH H 2-CH.sub.2OCH.sub.3 0 A-2831 H H H H H O OH H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-2832 H H H H H O OH H 2-CH.sub.2SCH.sub.3 0 A-2833 H H H H H O OH H 2-CH.sub.2S(?O)CH.sub.3 0 A-2834 H H H H H O OH H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-2835 H H H H H O OH H 2-(benzyloxy) 0 A-2836 H H H H H O OH H 2-NH.sub.2 0 A-2837 H H H H H O OH H 2-NHMe 0 A-2838 H H H H H O OH H 2-N(Me).sub.2 0 A-2839 H H H H H O OH H 2-(1,3-dioxolan-2-yl) 0 A-2840 H H H H H O OH H 2-(1,3-dioxan-2-yl) 0 A-2841 H H H H H O OH H 2-(1H-imidazol-2-yl) 0 A-2842 H H H H H O OH H 2-(thiazol-2-yl) 0 A-2843 H H H H H O OH H 2-(oxazol-2-yl) 0 A-2844 H H H H H O OH H 2-CH?NOH 0 A-2845 H H H H H O OH H 2-CH?NOMe 0
(152) TABLE-US-00051 TABLE 51 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2846 H H H H H O OH H 2-(4,5-dihydro-3-isoxazolyl) 0 A-2847 H H H H H O OH H 2-CN 0 A-2848 H H H H H O OH H 2-NO.sub.2 0 A-2849 H H H H H O OH H 2-F,6-Cl 0 A-2850 H H H H H O OH H 2-F,6-Me 0 A-2851 H H H H H O OH H 3-F,6-Me 0 A-2852 H H H H H O OH H 4-F,2-Me 0 A-2853 H H H H H O OH H 2-F,6-OMe 0 A-2854 H H H H H O OH H 3-F,6-OMe 0 A-2855 H H H H H O OH H 2,6-Cl.sub.2 0 A-2856 H H H H H O OH H 2-Cl,6-Me 0 A-2857 H H H H H O OH H 3-Cl,6-Me 0 A-2858 H H H H H O OH H 4-Cl,2-Me 0 A-2859 H H H H H O OH H 2-Cl,5-CF.sub.3 0 A-2860 H H H H H O OH H 2-Cl,6-CF.sub.3 0 A-2861 H H H H H O OH H 2-Cl,6-OMe 0 A-2862 H H H H H O OH H 3-Cl,6-OMe 0 A-2863 H H H H H O OH H 4-Cl,2-OMe 0 A-2864 H H H H H O OH H 2,4-Me.sub.2 0 A-2865 H H H H H O OH H 2,5-Me.sub.2 0 A-2866 H H H H H O OH H 2,6-Me.sub.2 0 A-2867 H H H H H O OH H 2-Me,4-CF.sub.3 0 A-2868 H H H H H O OH H 2-Me,5-CF.sub.3 0 A-2869 H H H H H O OH H 2-Me,6-CF.sub.3 0 A-2870 H H H H H O OH H 2-Me,4-OMe 0 A-2871 H H H H H O OH H 2-Me,5-OMe 0 A-2872 H H H H H O OH H 2-Me,6-OMe 0 A-2873 H H H H H O OH H 3-Me,6-OMe 0 A-2874 H H H H H O OH H 4-Me,2-OMe 0 A-2875 H H H H H O OH H 2,5-OMe.sub.2 0 A-2876 H H H H H O OH H 2,6-OMe.sub.2 0 A-2877 H H H H H O OH H 2-OMe,6-CF.sub.3 0 A-2878 H H H H H O OH H 2-CHF.sub.2,5-F 0 A-2879 H H H H H O OH H 2-CHF.sub.2,6-F 0 A-2880 H H H H H O OH H 2-CHF.sub.2,5-Me 0 A-2881 H H H H H O OH H 2-CHF.sub.2,6-Me 0 A-2882 H H H H H O OH H 2-cyclopropyl,5-F 0 A-2883 H H H H H O OH H 2-cyclopropyl,6-F 0 A-2884 H H H H H O OH H 2-cyclopropyl,5-Me 0 A-2885 H H H H H O OH H 2-cyclopropyl,6-Me 0 A-2886 H H H H H O OH H 2-ethenyl,6-F 0 A-2887 H H H H H O OH H 2-ethenyl,6-Me 0 A-2888 H H H H H O OH H 2-OEt,5-F 0 A-2889 H H H H H O OH H 2-OEt,6-F 0 A-2890 H H H H H O OH H 2-OEt,5-Cl 0 A-2891 H H H H H O OH H 2-OEt,6-Cl 0 A-2892 H H H H H O OH H 2-OEt,5-Me 0 A-2893 H H H H H O OH H 2-OEt,6-Me 0 A-2894 H H H H H O OH H 2-OCHF.sub.2,5-F 0 A-2895 H H H H H O OH H 2-OCHF.sub.2,6-F 0 A-2896 H H H H H O OH H 2-OCHF.sub.2,5-Me 0 A-2897 H H H H H O OH H 2-OCHF.sub.2,6-Me 0 A-2898 H H H H H O OH H 2-(cyclopropyloxy),5-F 0 A-2899 H H H H H O OH H 2-(cyclopropyloxy),6-F 0 A-2900 H H H H H O OH H 2-(cyclopropyloxy),5-Me 0 A-2901 H H H H H O OH H 2-(cyclopropyloxy),6-Me 0 A-2902 H H H H H O OH H 2-SMe,5-F 0
(153) TABLE-US-00052 TABLE 52 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2903 H H H H H O OH H 2-SMe,6-F 0 A-2904 H H H H H O OH H 2-SMe,5-Me 0 A-2905 H H H H H O OH H 2-SMe,6-Me 0 A-2906 H H H H H O OH H 2-S(?O)Me,5-F 0 A-2907 H H H H H O OH H 2-S(?O)Me,6-F 0 A-2908 H H H H H O OH H 2-S(?O)Me,5-Me 0 A-2909 H H H H H O OH H 2-S(?O)Me,6-Me 0 A-2910 H H H H H O OH H 2-S(?O).sub.2Me,5-F 0 A-2911 H H H H H O OH H 2-S(?O).sub.2Me,6-F 0 A-2912 H H H H H O OH H 2-S(?O).sub.2Me,5-Me 0 A-2913 H H H H H O OH H 2-S(?O).sub.2Me,6-Me 0 A-2914 H H H H H O OH H 2-SCF.sub.3,5-F 0 A-2915 H H H H H O OH H 2-SCF.sub.3,6-F 0 A-2916 H H H H H O OH H 2-SCF.sub.3,5-Me 0 A-2917 H H H H H O OH H 2-SCF.sub.3,6-Me 0 A-2918 H H H H H O OH H 2-S(?O)CF.sub.3,5-F 0 A-2919 H H H H H O OH H 2-S(?O)CF.sub.3,6-F 0 A-2920 H H H H H O OH H 2-S(?O)CF.sub.3,5-Me 0 A-2921 H H H H H O OH H 2-S(?O)CF.sub.3,6-Me 0 A-2922 H H H H H O OH H 2-S(?O).sub.2CF.sub.3,5-F 0 A-2923 H H H H H O OH H 2-S(?O).sub.2CF.sub.3,6-F 0 A-2924 H H H H H O OH H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-2925 H H H H H O OH H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-2926 H H H H H O OH H 2-(cyclopropylthio),5-F 0 A-2927 H H H H H O OH H 2-(cyclopropylthio),6-F 0 A-2928 H H H H H O OH H 2-(cyclopropylthio),5-Me 0 A-2929 H H H H H O OH H 2-(cyclopropylthio),6-Me 0 A-2930 H H H H H O OH H 2-C(?O)Me,5-F 0 A-2931 H H H H H O OH H 2-C(?O)Me,6-F 0 A-2932 H H H H H O OH H 2-C(?O)Me,5-Me 0 A-2933 H H H H H O OH H 2-C(?O)Me,6-Me 0 A-2934 H H H H H O OH H 2-CH.sub.2OH,5-F 0 A-2935 H H H H H O OH H 2-CH.sub.2OH,6-F 0 A-2936 H H H H H O OH H 2-CH.sub.2OH,5-Me 0 A-2937 H H H H H O OH H 2-CH.sub.2OH,6-Me 0 A-2938 H H H H H O OH H 2-CH.sub.2OCH.sub.3,4-F 0 A-2939 H H H H H O OH H 2-CH.sub.2OCH.sub.3,5-F 0 A-2940 H H H H H O OH H 2-CH.sub.2OCH.sub.3,6-F 0 A-2941 H H H H H O OH H 2-CH.sub.2OCH.sub.3,4-Me 0 A-2942 H H H H H O OH H 2-CH.sub.2OCH.sub.3,5-Me 0 A-2943 H H H H H O OH H 2-CH.sub.2OCH.sub.3,6-Me 0 A-2944 H H H H H O OH H 2-OC(?O)CH.sub.3,5-F 0 A-2945 H H H H H O OH H 2-OC(?O)CH.sub.3,6-F 0 A-2946 H H H H H O OH H 2-OC(?O)CH.sub.3,5-Me 0 A-2947 H H H H H O OH H 2-OC(?O)CH.sub.3,6-Me 0 A-2948 H H H H H O OH H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-2949 H H H H H O OH H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-2950 H H H H H O OH H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-2951 H H H H H O OH H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-2952 H H H H H O OH H 2-CH.sub.2SCH.sub.3,5-F 0 A-2953 H H H H H O OH H 2-CH.sub.2SCH.sub.3,6-F 0 A-2954 H H H H H O OH H 2-CH.sub.2SCH.sub.3,5-Me 0 A-2955 H H H H H O OH H 2-CH.sub.2SCH.sub.3,6-Me 0 A-2956 H H H H H O OH H 2-NMe.sub.2,5-F 0 A-2957 H H H H H O OH H 2-NMe.sub.2,6-F 0 A-2958 H H H H H O OH H 2-NMe.sub.2,5-Me 0 A-2959 H H H H H O OH H 2-NMe.sub.2,6-Me 0
(154) TABLE-US-00053 TABLE 53 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-2960 H H H H H O OH H 2-CN,4-F 0 A-2961 H H H H H O OH H 2-CN,5-F 0 A-2962 H H H H H O OH H 2-CN,6-F 0 A-2963 H H H H H O OH H 2-CN,6-Me 0 A-2964 H H H H H O OH H 2-CN,5-OMe 0 A-2965 H H H H H O OH H 2-CN,6-OMe 0 A-2966 H H H H H O OH H 3-CN,6-Me 0 A-2967 H H H H H O OH H 3-CN,6-OMe 0 A-2968 H H H H H O OH H 4-CN,2-Me 0 A-2969 H H H H H O OH H 4-CN,2-OMe 0 A-2970 H H H H H O OH H 2-NO.sub.2,4-F 0 A-2971 H H H H H O OH H 2-NO.sub.2,5-F 0 A-2972 H H H H H O OH H 2-NO.sub.2,6-F 0 A-2973 H H H H H O OH H 2-NO.sub.2,4-Me 0 A-2974 H H H H H O OH H 2-NO.sub.2,5-Me 0 A-2975 H H H H H O OH H 2-NO.sub.2,6-Me 0 A-2976 H H H H H O OH H 2-Me,4,5-F.sub.2 0 A-2977 H H H H H O OH H 2-Me,6-Et 0 A-2978 H H H H H O OH H 2-cyclopropyl,6-OMe 0 A-2979 H H H H H O OH H 2-Me,5-Et 0 A-2980 H H H H H O OH H 2,6-Et.sub.2 0 A-2981 H H H H H O OH H 2-Et,6-F 0 A-2982 H H H H H O OH H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-2983 H H H H H O OH H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-2984 H H H H H O OH H 2-CH.sub.2NMe.sub.2 0 A-2985 H H H H H O OCH.sub.2CH.sub.3 H H 0 A-2986 H H H H H O OCH.sub.2CH.sub.3 H 2-F 0 A-2987 H H H H H O OCH.sub.2CH.sub.3 H 2-Cl 0 A-2988 H H H H H O OCH.sub.2CH.sub.3 H 2-Br 0 A-2989 H H H H H O OCH.sub.2CH.sub.3 H 2-OH 0 A-2990 H H H H H O OCH.sub.2CH.sub.3 H 2-Me 0 A-2991 H H H H H O OCH.sub.2CH.sub.3 H 2-Et 0 A-2992 H H H H H O OCH.sub.2CH.sub.3 H 2-Pr 0 A-2993 H H H H H O OCH.sub.2CH.sub.3 H 2-CF.sub.3 0 A-2994 H H H H H O OCH.sub.2CH.sub.3 H 2-CHF.sub.2 0 A-2995 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2F 0 A-2996 H H H H H O OCH.sub.2CH.sub.3 H 2-CF.sub.2Cl 0 A-2997 H H H H H O OCH.sub.2CH.sub.3 H 2-cyclopropyl 0 A-2998 H H H H H O OCH.sub.2CH.sub.3 H 2-cyclobutyl 0 A-2999 H H H H H O OCH.sub.2CH.sub.3 H 2-cyclopentyl 0 A-3000 H H H H H O OCH.sub.2CH.sub.3 H 2-ethenyl 0 A-3001 H H H H H O OCH.sub.2CH.sub.3 H 2-allyl 0 A-3002 H H H H H O OCH.sub.2CH.sub.3 H 2-(prop-1-en-1-yl) 0 A-3003 H H H H H O OCH.sub.2CH.sub.3 H 2-(trifluoroethenyl) 0 A-3004 H H H H H O OCH.sub.2CH.sub.3 H 2-OMe 0 A-3005 H H H H H O OCH.sub.2CH.sub.3 H 2-OEt 0 A-3006 H H H H H O OCH.sub.2CH.sub.3 H 2-OPr 0 A-3007 H H H H H O OCH.sub.2CH.sub.3 H 2-O(i-Pr) 0 A-3008 H H H H H O OCH.sub.2CH.sub.3 H 2-OCF.sub.3 0 A-3009 H H H H H O OCH.sub.2CH.sub.3 H 2-OCHF.sub.2 0 A-3010 H H H H H O OCH.sub.2CH.sub.3 H 2-(cyclopropyloxy) 0 A-3011 H H H H H O OCH.sub.2CH.sub.3 H 2-(cyclobutyloxy) 0 A-3012 H H H H H O OCH.sub.2CH.sub.3 H 2-(cyclopentyloxy) 0 A-3013 H H H H H O OCH.sub.2CH.sub.3 H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-3014 H H H H H O OCH.sub.2CH.sub.3 H 2-(oxiran-2-yl) 0 A-3015 H H H H H O OCH.sub.2CH.sub.3 H 2-SMe 0 A-3016 H H H H H O OCH.sub.2CH.sub.3 H 3-SMe 0
(155) TABLE-US-00054 TABLE 54 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3017 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O)Me 0 A-3018 H H H H H O OCH.sub.2CH.sub.3 H 3-S(?O)Me 0 A-3019 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O).sub.2Me 0 A-3020 H H H H H O OCH.sub.2CH.sub.3 H 3-S(?O).sub.2Me 0 A-3021 H H H H H O OCH.sub.2CH.sub.3 H 2-SCF.sub.3 0 A-3022 H H H H H O OCH.sub.2CH.sub.3 H 3-SCF.sub.3 0 A-3023 H H H H H O OCH.sub.2CH.sub.3 H 3-S(?O)CF.sub.3 0 A-3024 H H H H H O OCH.sub.2CH.sub.3 H 3-SCF(CF.sub.3).sub.2 0 A-3025 H H H H H O OCH.sub.2CH.sub.3 H 2-(cyclopropylthio) 0 A-3026 H H H H H O OCH.sub.2CH.sub.3 H 2-(cyclopropylsulfinyl) 0 A-3027 H H H H H O OCH.sub.2CH.sub.3 H 2-(cyclopropylsulfonyl) 0 A-3028 H H H H H O OCH.sub.2CH.sub.3 H 2-C(?O)Me 0 A-3029 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2C(?O)CH.sub.3 0 A-3030 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2C(?O)CF.sub.3 0 A-3031 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2OH 0 A-3032 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3 0 A-3033 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-3034 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3 0 A-3035 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2S(?O)CH.sub.3 0 A-3036 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-3037 H H H H H O OCH.sub.2CH.sub.3 H 2-(benzyloxy) 0 A-3038 H H H H H O OCH.sub.2CH.sub.3 H 2-NH.sub.2 0 A-3039 H H H H H O OCH.sub.2CH.sub.3 H 2-NHMe 0 A-3040 H H H H H O OCH.sub.2CH.sub.3 H 2-N(Me).sub.2 0 A-3041 H H H H H O OCH.sub.2CH.sub.3 H 2-(1,3-dioxolan-2-yl) 0 A-3042 H H H H H O OCH.sub.2CH.sub.3 H 2-(1,3-dioxan-2-yl) 0 A-3043 H H H H H O OCH.sub.2CH.sub.3 H 2-(1H-imidazol-2-yl) 0 A-3044 H H H H H O OCH.sub.2CH.sub.3 H 2-(thiazol-2-yl) 0 A-3045 H H H H H O OCH.sub.2CH.sub.3 H 2-(oxazol-2-yl) 0 A-3046 H H H H H O OCH.sub.2CH.sub.3 H 2-CH?NOH 0 A-3047 H H H H H O OCH.sub.2CH.sub.3 H 2-CH?NOMe 0 A-3048 H H H H H O OCH.sub.2CH.sub.3 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-3049 H H H H H O OCH.sub.2CH.sub.3 H 2-CN 0 A-3050 H H H H H O OCH.sub.2CH.sub.3 H 2-NO.sub.2 0 A-3051 H H H H H O OCH.sub.2CH.sub.3 H 2-F,6-Cl 0 A-3052 H H H H H O OCH.sub.2CH.sub.3 H 2-F,6-Me 0 A-3053 H H H H H O OCH.sub.2CH.sub.3 H 3-F,6-Me 0 A-3054 H H H H H O OCH.sub.2CH.sub.3 H 4-F,2-Me 0 A-3055 H H H H H O OCH.sub.2CH.sub.3 H 2-F,6-OMe 0 A-3056 H H H H H O OCH.sub.2CH.sub.3 H 3-F,6-OMe 0 A-3057 H H H H H O OCH.sub.2CH.sub.3 H 2,6-Cl.sub.2 0 A-3058 H H H H H O OCH.sub.2CH.sub.3 H 2-Cl,6-Me 0 A-3059 H H H H H O OCH.sub.2CH.sub.3 H 3-Cl,6-Me 0 A-3060 H H H H H O OCH.sub.2CH.sub.3 H 4-Cl,2-Me 0 A-3061 H H H H H O OCH.sub.2CH.sub.3 H 2-Cl,5-CF.sub.3 0 A-3062 H H H H H O OCH.sub.2CH.sub.3 H 2-Cl,6-CF.sub.3 0 A-3063 H H H H H O OCH.sub.2CH.sub.3 H 2-Cl,6-OMe 0 A-3064 H H H H H O OCH.sub.2CH.sub.3 H 3-Cl,6-OMe 0 A-3065 H H H H H O OCH.sub.2CH.sub.3 H 4-Cl,2-OMe 0 A-3066 H H H H H O OCH.sub.2CH.sub.3 H 2,4-Me.sub.2 0 A-3067 H H H H H O OCH.sub.2CH.sub.3 H 2,5-Me.sub.2 0 A-3068 H H H H H O OCH.sub.2CH.sub.3 H 2,6-Me.sub.2 0 A-3069 H H H H H O OCH.sub.2CH.sub.3 H 2-Me,4-CF.sub.3 0 A-3070 H H H H H O OCH.sub.2CH.sub.3 H 2-Me,5-CF.sub.3 0 A-3071 H H H H H O OCH.sub.2CH.sub.3 H 2-Me,6-CF.sub.3 0 A-3072 H H H H H O OCH.sub.2CH.sub.3 H 2-Me,4-OMe 0 A-3073 H H H H H O OCH.sub.2CH.sub.3 H 2-Me,5-OMe 0
(156) TABLE-US-00055 TABLE 55 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3074 H H H H H O OCH.sub.2CH.sub.3 H 2-Me,6-OMe 0 A-3075 H H H H H O OCH.sub.2CH.sub.3 H 3-Me,6-OMe 0 A-3076 H H H H H O OCH.sub.2CH.sub.3 H 4-Me,2-OMe 0 A-3077 H H H H H O OCH.sub.2CH.sub.3 H 2,5-OMe.sub.2 0 A-3078 H H H H H O OCH.sub.2CH.sub.3 H 2,6-OMe.sub.2 0 A-3079 H H H H H O OCH.sub.2CH.sub.3 H 2-OMe,6-CF.sub.3 0 A-3080 H H H H H O OCH.sub.2CH.sub.3 H 2-CHF.sub.2,5-F 0 A-3081 H H H H H O OCH.sub.2CH.sub.3 H 2-CHF.sub.2,6-F 0 A-3082 H H H H H O OCH.sub.2CH.sub.3 H 2-CHF.sub.2,5-Me 0 A-3083 H H H H H O OCH.sub.2CH.sub.3 H 2-CHF.sub.2,6-Me 0 A-3084 H H H H H O OCH.sub.2CH.sub.3 H 2-cyclopropyl,5-F 0 A-3085 H H H H H O OCH.sub.2CH.sub.3 H 2-cyclopropyl,6-F 0 A-3086 H H H H H O OCH.sub.2CH.sub.3 H 2-cyclopropyl,5-Me 0 A-3087 H H H H H O OCH.sub.2CH.sub.3 H 2-cyclopropyl,6-Me 0 A-3088 H H H H H O OCH.sub.2CH.sub.3 H 2-ethenyl,6-F 0 A-3089 H H H H H O OCH.sub.2CH.sub.3 H 2-ethenyl,6-Me 0 A-3090 H H H H H O OCH.sub.2CH.sub.3 H 2-OEt,5-F 0 A-3091 H H H H H O OCH.sub.2CH.sub.3 H 2-OEt,6-F 0 A-3092 H H H H H O OCH.sub.2CH.sub.3 H 2-OEt,5-Cl 0 A-3093 H H H H H O OCH.sub.2CH.sub.3 H 2-OEt,6-Cl 0 A-3094 H H H H H O OCH.sub.2CH.sub.3 H 2-OEt,5-Me 0 A-3095 H H H H H O OCH.sub.2CH.sub.3 H 2-OEt,6-Me 0 A-3096 H H H H H O OCH.sub.2CH.sub.3 H 2-OCHF.sub.2,5-F 0 A-3097 H H H H H O OCH.sub.2CH.sub.3 H 2-OCHF.sub.2,6-F 0 A-3098 H H H H H O OCH.sub.2CH.sub.3 H 2-OCHF.sub.2,5-Me 0 A-3099 H H H H H O OCH.sub.2CH.sub.3 H 2-OCHF.sub.2,6-Me 0 A-3100 H H H H H O OCH.sub.2CH.sub.3 H 2-(cyclopropyloxy),5-F 0 A-3101 H H H H H O OCH.sub.2CH.sub.3 H 2-(cyclopropyloxy),6-F 0 A-3102 H H H H H O OCH.sub.2CH.sub.3 H 2-(cyclopropyloxy),5-Me 0 A-3103 H H H H H O OCH.sub.2CH.sub.3 H 2-(cyclopropyloxy),6-Me 0 A-3104 H H H H H O OCH.sub.2CH.sub.3 H 2-SMe,5-F 0 A-3105 H H H H H O OCH.sub.2CH.sub.3 H 2-SMe,6-F 0 A-3106 H H H H H O OCH.sub.2CH.sub.3 H 2-SMe,5-Me 0 A-3107 H H H H H O OCH.sub.2CH.sub.3 H 2-SMe,6-Me 0 A-3108 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O)Me,5-F 0 A-3109 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O)Me,6-F 0 A-3110 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O)Me,5-Me 0 A-3111 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O)Me,6-Me 0 A-3112 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,5-F 0 A-3113 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,6-F 0 A-3114 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,5-Me 0 A-3115 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,6-Me 0 A-3116 H H H H H O OCH.sub.2CH.sub.3 H 2-SCF.sub.3,5-F 0 A-3117 H H H H H O OCH.sub.2CH.sub.3 H 2-SCF.sub.3,6-F 0 A-3118 H H H H H O OCH.sub.2CH.sub.3 H 2-SCF.sub.3,5-Me 0 A-3119 H H H H H O OCH.sub.2CH.sub.3 H 2-SCF.sub.3,6-Me 0 A-3120 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,5-F 0 A-3121 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,6-F 0 A-3122 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,5-Me 0 A-3123 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,6-Me 0 A-3124 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-3125 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-3126 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-3127 H H H H H O OCH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-3128 H H H H H O OCH.sub.2CH.sub.3 H 2-(cyclopropylthio),5-F 0 A-3129 H H H H H O OCH.sub.2CH.sub.3 H 2-(cyclopropylthio),6-F 0 A-3130 H H H H H O OCH.sub.2CH.sub.3 H 2-(cyclopropylthio),5-Me 0
(157) TABLE-US-00056 TABLE 56 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3131 H H H H H O OCH.sub.2CH.sub.3 H 2-(cyclopropylthio),6-Me 0 A-3132 H H H H H O OCH.sub.2CH.sub.3 H 2-C(?O)Me,5-F 0 A-3133 H H H H H O OCH.sub.2CH.sub.3 H 2-C(?O)Me,6-F 0 A-3134 H H H H H O OCH.sub.2CH.sub.3 H 2-C(?O)Me,5-Me 0 A-3135 H H H H H O OCH.sub.2CH.sub.3 H 2-C(?O)Me,6-Me 0 A-3136 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2OH,5-F 0 A-3137 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2OH,6-F 0 A-3138 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2OH,5-Me 0 A-3139 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2OH,6-Me 0 A-3140 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-F 0 A-3141 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-F 0 A-3142 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-F 0 A-3143 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-3144 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-3145 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-3146 H H H H H O OCH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,5-F 0 A-3147 H H H H H O OCH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,6-F 0 A-3148 H H H H H O OCH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,5-Me 0 A-3149 H H H H H O OCH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,6-Me 0 A-3150 H H H H H O OCH.sub.2CH.sub.3 H 2-OS(?O).sub.2-CH.sub.3,5-F 0 A-3151 H H H H H O OCH.sub.2CH.sub.3 H 2-OS(?O).sub.2-CH.sub.3,6-F 0 A-3152 H H H H H O OCH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-3153 H H H H H O OCH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-3154 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-F 0 A-3155 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,6-F 0 A-3156 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-Me 0 A-3157 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,6-Me 0 A-3158 H H H H H O OCH.sub.2CH.sub.3 H 2-NMe.sub.2,5-F 0 A-3159 H H H H H O OCH.sub.2CH.sub.3 H 2-NMe.sub.2,6-F 0 A-3160 H H H H H O OCH.sub.2CH.sub.3 H 2-NMe.sub.2,5-Me 0 A-3161 H H H H H O OCH.sub.2CH.sub.3 H 2-NMe.sub.2,6-Me 0 A-3162 H H H H H O OCH.sub.2CH.sub.3 H 2-CN,4-F 0 A-3163 H H H H H O OCH.sub.2CH.sub.3 H 2-CN,5-F 0 A-3164 H H H H H O OCH.sub.2CH.sub.3 H 2-CN,6-F 0 A-3165 H H H H H O OCH.sub.2CH.sub.3 H 2-CN,6-Me 0 A-3166 H H H H H O OCH.sub.2CH.sub.3 H 2-CN,5-OMe 0 A-3167 H H H H H O OCH.sub.2CH.sub.3 H 2-CN,6-OMe 0 A-3168 H H H H H O OCH.sub.2CH.sub.3 H 3-CN,6-Me 0 A-3169 H H H H H O OCH.sub.2CH.sub.3 H 3-CN,6-OMe 0 A-3170 H H H H H O OCH.sub.2CH.sub.3 H 4-CN,2-Me 0 A-3171 H H H H H O OCH.sub.2CH.sub.3 H 4-CN,2-OMe 0 A-3172 H H H H H O OCH.sub.2CH.sub.3 H 2-NO.sub.2,4-F 0 A-3173 H H H H H O OCH.sub.2CH.sub.3 H 2-NO.sub.2,5-F 0 A-3174 H H H H H O OCH.sub.2CH.sub.3 H 2-NO.sub.2,6-F 0 A-3175 H H H H H O OCH.sub.2CH.sub.3 H 2-NO.sub.2,4-Me 0 A-3176 H H H H H O OCH.sub.2CH.sub.3 H 2-NO.sub.2,5-Me 0 A-3177 H H H H H O OCH.sub.2CH.sub.3 H 2-NO.sub.2,6-Me 0 A-3178 H H H H H O OCH.sub.2CH.sub.3 H 2-Me,4,5-F.sub.2 0 A-3179 H H H H H O OCH.sub.2CH.sub.3 H 2-Me,6-Et 0 A-3180 H H H H H O OCH.sub.2CH.sub.3 H 2-cyclopropyl,6-OMe 0 A-3181 H H H H H O OCH.sub.2CH.sub.3 H 2-Me,5-Et 0 A-3182 H H H H H O OCH.sub.2CH.sub.3 H 2,6-Et.sub.2 0 A-3183 H H H H H O OCH.sub.2CH.sub.3 H 2-Et,6-F 0 A-3184 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-3185 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-3186 H H H H H O OCH.sub.2CH.sub.3 H 2-CH.sub.2NMe.sub.2 0 A-3187 H H H H H O CH.sub.2CF.sub.3 H H 0
(158) TABLE-US-00057 TABLE 57 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3188 H H H H H O CH.sub.2CF.sub.3 H 2-F 0 A-3189 H H H H H O CH.sub.2CF.sub.3 H 2-Cl 0 A-3190 H H H H H O CH.sub.2CF.sub.3 H 2-Br 0 A-3191 H H H H H O CH.sub.2CF.sub.3 H 2-OH 0 A-3192 H H H H H O CH.sub.2CF.sub.3 H 2-Me 0 A-3193 H H H H H O CH.sub.2CF.sub.3 H 2-Et 0 A-3194 H H H H H O CH.sub.2CF.sub.3 H 2-Pr 0 A-3195 H H H H H O CH.sub.2CF.sub.3 H 2-CF.sub.3 0 A-3196 H H H H H O CH.sub.2CF.sub.3 H 2-CHF.sub.2 0 A-3197 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2F 0 A-3198 H H H H H O CH.sub.2CF.sub.3 H 2-CF.sub.2Cl 0 A-3199 H H H H H O CH.sub.2CF.sub.3 H 2-cyclopropyl 0 A-3200 H H H H H O CH.sub.2CF.sub.3 H 2-cyclobutyl 0 A-3201 H H H H H O CH.sub.2CF.sub.3 H 2-cyclopentyl 0 A-3202 H H H H H O CH.sub.2CF.sub.3 H 2-ethenyl 0 A-3203 H H H H H O CH.sub.2CF.sub.3 H 2-allyl 0 A-3204 H H H H H O CH.sub.2CF.sub.3 H 2-(prop-1-en-1-yl) 0 A-3205 H H H H H O CH.sub.2CF.sub.3 H 2-(trifluoroethenyl) 0 A-3206 H H H H H O CH.sub.2CF.sub.3 H 2-OMe 0 A-3207 H H H H H O CH.sub.2CF.sub.3 H 2-OEt 0 A-3208 H H H H H O CH.sub.2CF.sub.3 H 2-OPr 0 A-3209 H H H H H O CH.sub.2CF.sub.3 H 2-O(i-Pr) 0 A-3210 H H H H H O CH.sub.2CF.sub.3 H 2-OCF.sub.3 0 A-3211 H H H H H O CH.sub.2CF.sub.3 H 2-OCHF.sub.2 0 A-3212 H H H H H O CH.sub.2CF.sub.3 H 2-(cyclopropyloxy) 0 A-3213 H H H H H O CH.sub.2CF.sub.3 H 2-(cyclobutyloxy) 0 A-3214 H H H H H O CH.sub.2CF.sub.3 H 2-(cyclopentyloxy) 0 A-3215 H H H H H O CH.sub.2CF.sub.3 H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-3216 H H H H H O CH.sub.2CF.sub.3 H 2-(oxiran-2-yl) 0 A-3217 H H H H H O CH.sub.2CF.sub.3 H 2-SMe 0 A-3218 H H H H H O CH.sub.2CF.sub.3 H 3-SMe 0 A-3219 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O)Me 0 A-3220 H H H H H O CH.sub.2CF.sub.3 H 3-S(?O)Me 0 A-3221 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O).sub.2Me 0 A-3222 H H H H H O CH.sub.2CF.sub.3 H 3-S(?O).sub.2Me 0 A-3223 H H H H H O CH.sub.2CF.sub.3 H 2-SCF.sub.3 0 A-3224 H H H H H O CH.sub.2CF.sub.3 H 3-SCF.sub.3 0 A-3225 H H H H H O CH.sub.2CF.sub.3 H 3-S(?O)CF.sub.3 0 A-3226 H H H H H O CH.sub.2CF.sub.3 H 3-SCF(CF.sub.3).sub.2 0 A-3227 H H H H H O CH.sub.2CF.sub.3 H 2-(cyclopropylthio) 0 A-3228 H H H H H O CH.sub.2CF.sub.3 H 2-(cyclopropylsulfinyl) 0 A-3229 H H H H H O CH.sub.2CF.sub.3 H 2-(cyclopropylsulfonyl) 0 A-3230 H H H H H O CH.sub.2CF.sub.3 H 2-C(?O)Me 0 A-3231 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2C(?O)CH.sub.3 0 A-3232 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2C(?O)CF.sub.3 0 A-3233 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2OH 0 A-3234 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2OCH.sub.3 0 A-3235 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-3236 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2SCH.sub.3 0 A-3237 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2S(?O)CH.sub.3 0 A-3238 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-3239 H H H H H O CH.sub.2CF.sub.3 H 2-(benzyloxy) 0 A-3240 H H H H H O CH.sub.2CF.sub.3 H 2-NH.sub.2 0 A-3241 H H H H H O CH.sub.2CF.sub.3 H 2-NHMe 0 A-3242 H H H H H O CH.sub.2CF.sub.3 H 2-N(Me).sub.2 0 A-3243 H H H H H O CH.sub.2CF.sub.3 H 2-(1,3-dioxolan-2-yl) 0 A-3244 H H H H H O CH.sub.2CF.sub.3 H 2-(1,3-dioxan-2-yl) 0
(159) TABLE-US-00058 TABLE 58 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3245 H H H H H O CH.sub.2CF.sub.3 H 2-(1H-imidazol-2-yl) 0 A-3246 H H H H H O CH.sub.2CF.sub.3 H 2-(thiazol-2-yl) 0 A-3247 H H H H H O CH.sub.2CF.sub.3 H 2-(oxazol-2-yl) 0 A-3248 H H H H H O CH.sub.2CF.sub.3 H 2-CH?NOH 0 A-3249 H H H H H O CH.sub.2CF.sub.3 H 2-CH?NOMe 0 A-3250 H H H H H O CH.sub.2CF.sub.3 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-3251 H H H H H O CH.sub.2CF.sub.3 H 2-CN 0 A-3252 H H H H H O CH.sub.2CF.sub.3 H 2-NO.sub.2 0 A-3253 H H H H H O CH.sub.2CF.sub.3 H 2-F,6-Cl 0 A-3254 H H H H H O CH.sub.2CF.sub.3 H 2-F,6-Me 0 A-3255 H H H H H O CH.sub.2CF.sub.3 H 3-F,6-Me 0 A-3256 H H H H H O CH.sub.2CF.sub.3 H 4-F,2-Me 0 A-3257 H H H H H O CH.sub.2CF.sub.3 H 2-F,6-OMe 0 A-3258 H H H H H O CH.sub.2CF.sub.3 H 3-F,6-OMe 0 A-3259 H H H H H O CH.sub.2CF.sub.3 H 2,6-Cl.sub.2 0 A-3260 H H H H H O CH.sub.2CF.sub.3 H 2-Cl,6-Me 0 A-3261 H H H H H O CH.sub.2CF.sub.3 H 3-Cl,6-Me 0 A-3262 H H H H H O CH.sub.2CF.sub.3 H 4-Cl,2-Me 0 A-3263 H H H H H O CH.sub.2CF.sub.3 H 2-Cl,5-CF.sub.3 0 A-3264 H H H H H O CH.sub.2CF.sub.3 H 2-Cl,6-CF.sub.3 0 A-3265 H H H H H O CH.sub.2CF.sub.3 H 2-Cl,6-OMe 0 A-3266 H H H H H O CH.sub.2CF.sub.3 H 3-Cl,6-OMe 0 A-3267 H H H H H O CH.sub.2CF.sub.3 H 4-Cl,2-OMe 0 A-3268 H H H H H O CH.sub.2CF.sub.3 H 2,4-Me.sub.2 0 A-3269 H H H H H O CH.sub.2CF.sub.3 H 2,5-Me.sub.2 0 A-3270 H H H H H O CH.sub.2CF.sub.3 H 2,6-Me.sub.2 0 A-3271 H H H H H O CH.sub.2CF.sub.3 H 2-Me,4-CF.sub.3 0 A-3272 H H H H H O CH.sub.2CF.sub.3 H 2-Me,5-CF.sub.3 0 A-3273 H H H H H O CH.sub.2CF.sub.3 H 2-Me,6-CF.sub.3 0 A-3274 H H H H H O CH.sub.2CF.sub.3 H 2-Me,4-OMe 0 A-3275 H H H H H O CH.sub.2CF.sub.3 H 2-Me,5-OMe 0 A-3276 H H H H H O CH.sub.2CF.sub.3 H 2-Me,6-OMe 0 A-3277 H H H H H O CH.sub.2CF.sub.3 H 3-Me,6-OMe 0 A-3278 H H H H H O CH.sub.2CF.sub.3 H 4-Me,2-OMe 0 A-3279 H H H H H O CH.sub.2CF.sub.3 H 2,5-OMe.sub.2 0 A-3280 H H H H H O CH.sub.2CF.sub.3 H 2,6-OMe.sub.2 0 A-3281 H H H H H O CH.sub.2CF.sub.3 H 2-OMe,6-CF.sub.3 0 A-3282 H H H H H O CH.sub.2CF.sub.3 H 2-CHF.sub.2,5-F 0 A-3283 H H H H H O CH.sub.2CF.sub.3 H 2-CHF.sub.2,6-F 0 A-3284 H H H H H O CH.sub.2CF.sub.3 H 2-CHF.sub.2,5-Me 0 A-3285 H H H H H O CH.sub.2CF.sub.3 H 2-CHF.sub.2,6-Me 0 A-3286 H H H H H O CH.sub.2CF.sub.3 H 2-cyclopropyl,5-F 0 A-3287 H H H H H O CH.sub.2CF.sub.3 H 2-cyclopropyl,6-F 0 A-3288 H H H H H O CH.sub.2CF.sub.3 H 2-cyclopropyl,5-Me 0 A-3289 H H H H H O CH.sub.2CF.sub.3 H 2-cyclopropyl,6-Me 0 A-3290 H H H H H O CH.sub.2CF.sub.3 H 2-ethenyl,6-F 0 A-3291 H H H H H O CH.sub.2CF.sub.3 H 2-ethenyl,6-Me 0 A-3292 H H H H H O CH.sub.2CF.sub.3 H 2-OEt,5-F 0 A-3293 H H H H H O CH.sub.2CF.sub.3 H 2-OEt,6-F 0 A-3294 H H H H H O CH.sub.2CF.sub.3 H 2-OEt,5-Cl 0 A-3295 H H H H H O CH.sub.2CF.sub.3 H 2-OEt,6-Cl 0 A-3296 H H H H H O CH.sub.2CF.sub.3 H 2-OEt,5-Me 0 A-3297 H H H H H O CH.sub.2CF.sub.3 H 2-OEt,6-Me 0 A-3298 H H H H H O CH.sub.2CF.sub.3 H 2-OCHF.sub.2,5-F 0 A-3299 H H H H H O CH.sub.2CF.sub.3 H 2-OCHF.sub.2,6-F 0 A-3300 H H H H H O CH.sub.2CF.sub.3 H 2-OCHF.sub.2,5-Me 0 A-3301 H H H H H O CH.sub.2CF.sub.3 H 2-OCHF.sub.2,6-Me 0
(160) TABLE-US-00059 TABLE 59 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3302 H H H H H O CH.sub.2CF.sub.3 H 2-(cyclopropyloxy),5-F 0 A-3303 H H H H H O CH.sub.2CF.sub.3 H 2-(cyclopropyloxy),6-F 0 A-3304 H H H H H O CH.sub.2CF.sub.3 H 2-(cyclopropyloxy),5-Me 0 A-3305 H H H H H O CH.sub.2CF.sub.3 H 2-(cyclopropyloxy),6-Me 0 A-3306 H H H H H O CH.sub.2CF.sub.3 H 2-SMe,5-F 0 A-3307 H H H H H O CH.sub.2CF.sub.3 H 2-SMe,6-F 0 A-3308 H H H H H O CH.sub.2CF.sub.3 H 2-SMe,5-Me 0 A-3309 H H H H H O CH.sub.2CF.sub.3 H 2-SMe,6-Me 0 A-3310 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O)Me,5-F 0 A-3311 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O)Me,6-F 0 A-3312 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O)Me,5-Me 0 A-3313 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O)Me,6-Me 0 A-3314 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O).sub.2Me,5-F 0 A-3315 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O).sub.2Me,6-F 0 A-3316 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O).sub.2Me,5-Me 0 A-3317 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O).sub.2Me,6-Me 0 A-3318 H H H H H O CH.sub.2CF.sub.3 H 2-SCF.sub.3,5-F 0 A-3319 H H H H H O CH.sub.2CF.sub.3 H 2-SCF.sub.3,6-F 0 A-3320 H H H H H O CH.sub.2CF.sub.3 H 2-SCF.sub.3,5-Me 0 A-3321 H H H H H O CH.sub.2CF.sub.3 H 2-SCF.sub.3,6-Me 0 A-3322 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O)CF.sub.3,5-F 0 A-3323 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O)CF.sub.3,6-F 0 A-3324 H H H H H O CH2CF.sub.3 H 2-S(?O)CF.sub.3,5-Me 0 A-3325 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O)CF.sub.3,6-Me 0 A-3326 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-3327 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-3328 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-3329 H H H H H O CH.sub.2CF.sub.3 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-3330 H H H H H O CH.sub.2CF.sub.3 H 2-(cyclopropylthio),5-F 0 A-3331 H H H H H O CH.sub.2CF.sub.3 H 2-(cyclopropylthio),6-F 0 A-3332 H H H H H O CH.sub.2CF.sub.3 H 2-(cyclopropylthio),5-Me 0 A-3333 H H H H H O CH.sub.2CF.sub.3 H 2-(cyclopropylthio),6-Me 0 A-3334 H H H H H O CH.sub.2CF.sub.3 H 2-C(?O)Me,5-F 0 A-3335 H H H H H O CH.sub.2CF.sub.3 H 2-C(?O)Me,6-F 0 A-3336 H H H H H O CH.sub.2CF.sub.3 H 2-C(?O)Me,5-Me 0 A-3337 H H H H H O CH.sub.2CF.sub.3 H 2-C(?O)Me,6-Me 0 A-3338 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2OH,5-F 0 A-3339 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2OH,6-F 0 A-3340 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2OH,5-Me 0 A-3341 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2OH,6-Me 0 A-3342 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2OCH.sub.3,4-F 0 A-3343 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2OCH.sub.3,5-F 0 A-3344 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2OCH.sub.3,6-F 0 A-3345 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-3346 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-3347 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-3348 H H H H H O CH.sub.2CF.sub.3 H 2-OC(?O)CH.sub.3,5-F 0 A-3349 H H H H H O CH.sub.2CF.sub.3 H 2-OC(?O)CH.sub.3,6-F 0 A-3350 H H H H H O CH.sub.2CF.sub.3 H 2-OC(?O)CH.sub.3,5-Me 0 A-3351 H H H H H O CH.sub.2CF.sub.3 H 2-OC(?O)CH.sub.3,6-Me 0 A-3352 H H H H H O CH.sub.2CF.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-3353 H H H H H O CH.sub.2CF.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-3354 H H H H H O CH.sub.2CF.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-3355 H H H H H O CH.sub.2CF.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-3356 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2SCH.sub.3,5-F 0 A-3357 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2SCH.sub.3,6-F 0 A-3358 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2SCH.sub.3,5-Me 0
(161) TABLE-US-00060 TABLE 60 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3359 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2SCH.sub.3,6-Me 0 A-3360 H H H H H O CH.sub.2CF.sub.3 H 2-NMe.sub.2,5-F 0 A-3361 H H H H H O CH.sub.2CF.sub.3 H 2-NMe.sub.2,6-F 0 A-3362 H H H H H O CH.sub.2CF.sub.3 H 2-NMe.sub.2,5-Me 0 A-3363 H H H H H O CH.sub.2CF.sub.3 H 2-NMe.sub.2,6-Me 0 A-3364 H H H H H O CH.sub.2CF.sub.3 H 2-CN,4-F 0 A-3365 H H H H H O CH.sub.2CF.sub.3 H 2-CN,5-F 0 A-3366 H H H H H O CH.sub.2CF.sub.3 H 2-CN,6-F 0 A-3367 H H H H H O CH.sub.2CF.sub.3 H 2-CN,6-Me 0 A-3368 H H H H H O CH.sub.2CF.sub.3 H 2-CN,5-OMe 0 A-3369 H H H H H O CH.sub.2CF.sub.3 H 2-CN,6-OMe 0 A-3370 H H H H H O CH.sub.2CF.sub.3 H 3-CN,6-Me 0 A-3371 H H H H H O CH.sub.2CF.sub.3 H 3-CN,6-OMe 0 A-3372 H H H H H O CH.sub.2CF.sub.3 H 4-CN,2-Me 0 A-3373 H H H H H O CH.sub.2CF.sub.3 H 4-CN,2-OMe 0 A-3374 H H H H H O CH.sub.2CF.sub.3 H 2-NO.sub.2,4-F 0 A-3375 H H H H H O CH.sub.2CF.sub.3 H 2-NO.sub.2,5-F 0 A-3376 H H H H H O CH.sub.2CF.sub.3 H 2-NO.sub.2,6-F 0 A-3377 H H H H H O CH.sub.2CF.sub.3 H 2-NO.sub.2,4-Me 0 A-3378 H H H H H O CH.sub.2CF.sub.3 H 2-NO.sub.2,5-Me 0 A-3379 H H H H H O CH.sub.2CF.sub.3 H 2-NO.sub.2,6-Me 0 A-3380 H H H H H O CH.sub.2CF.sub.3 H 2-Me,4,5-F.sub.2 0 A-3381 H H H H H O CH.sub.2CF.sub.3 H 2-Me,6-Et 0 A-3382 H H H H H O CH.sub.2CF.sub.3 H 2-cyclopropyl,6-OMe 0 A-3383 H H H H H O CH.sub.2CF.sub.3 H 2-Me,5-Et 0 A-3384 H H H H H O CH.sub.2CF.sub.3 H 2,6-Et.sub.2 0 A-3385 H H H H H O CH.sub.2CF.sub.3 H 2-Et,6-F 0 A-3386 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-3387 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-3388 H H H H H O CH.sub.2CF.sub.3 H 2-CH.sub.2NMe.sub.2 0 A-3389 H H H H H O tetrahydrofuran-3-yl H H 0 A-3390 H H H H H O tetrahydrofuran-3-yl H 2-F 0 A-3391 H H H H H O tetrahydrofuran-3-yl H 2-Cl 0 A-3392 H H H H H O tetrahydrofuran-3-yl H 2-Br 0 A-3393 H H H H H O tetrahydrofuran-3-yl H 2-OH 0 A-3394 H H H H H O tetrahydrofuran-3-yl H 2-Me 0 A-3395 H H H H H O tetrahydrofuran-3-yl H 2-Et 0 A-3396 H H H H H O tetrahydrofuran-3-yl H 2-Pr 0 A-3397 H H H H H O tetrahydrofuran-3-yl H 2-CF.sub.3 0 A-3398 H H H H H O tetrahydrofuran-3-yl H 2-CHF.sub.2 0 A-3399 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2F 0 A-3400 H H H H H O tetrahydrofuran-3-yl H 2-CF.sub.2Cl 0 A-3401 H H H H H O tetrahydrofuran-3-yl H 2-cyclopropyl 0 A-3402 H H H H H O tetrahydrofuran-3-yl H 2-cyclobutyl 0 A-3403 H H H H H O tetrahydrofuran-3-yl H 2-cyclopentyl 0 A-3404 H H H H H O tetrahydrofuran-3-yl H 2-ethenyl 0 A-3405 H H H H H O tetrahydrofuran-3-yl H 2-allyl 0 A-3406 H H H H H O tetrahydrofuran-3-yl H 2-(prop-1-en-1-yl) 0 A-3407 H H H H H O tetrahydrofuran-3-yl H 2-(trifluoroethenyl) 0 A-3408 H H H H H O tetrahydrofuran-3-yl H 2-OMe 0 A-3409 H H H H H O tetrahydrofuran-3-yl H 2-OEt 0 A-3410 H H H H H O tetrahydrofuran-3-yl H 2-OPr 0 A-3411 H H H H H O tetrahydrofuran-3-yl H 2-O(i-Pr) 0 A-3412 H H H H H O tetrahydrofuran-3-yl H 2-OCF.sub.3 0 A-3413 H H H H H O tetrahydrofuran-3-yl H 2-OCHF.sub.2 0 A-3414 H H H H H O tetrahydrofuran-3-yl H 2-(cyclopropyloxy) 0 A-3415 H H H H H O tetrahydrofuran-3-yl H 2-(cyclobutyloxy) 0
(162) TABLE-US-00061 TABLE 61 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3416 H H H H H O tetrahydrofuran-3-yl H 2-(cyclopentyloxy) 0 A-3417 H H H H H O tetrahydrofuran-3-yl H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-3418 H H H H H O tetrahydrofuran-3-yl H 2-(oxiran-2-yl) 0 A-3419 H H H H H O tetrahydrofuran-3-yl H 2-SMe 0 A-3420 H H H H H O tetrahydrofuran-3-yl H 3-SMe 0 A-3421 H H H H H O tetrahydrofuran-3-yl H 2-S(?O)Me 0 A-3422 H H H H H O tetrahydrofuran-3-yl H 3-S(?O)Me 0 A-3423 H H H H H O tetrahydrofuran-3-yl H 2-S(?O).sub.2Me 0 A-3424 H H H H H O tetrahydrofuran-3-yl H 3-S(?O).sub.2Me 0 A-3425 H H H H H O tetrahydrofuran-3-yl H 2-SCF.sub.3 0 A-3426 H H H H H O tetrahydrofuran-3-yl H 3-SCF.sub.3 0 A-3427 H H H H H O tetrahydrofuran-3-yl H 3-S(?O)CF.sub.3 0 A-3428 H H H H H O tetrahydrofuran-3-yl H 3-SCF(CF.sub.3).sub.2 0 A-3429 H H H H H O tetrahydrofuran-3-yl H 2-(cyclopropylthio) 0 A-3430 H H H H H O tetrahydrofuran-3-yl H 2-(cyclopropylsulfinyl) 0 A-3431 H H H H H O tetrahydrofuran-3-yl H 2-(cyclopropylsulfonyl) 0 A-3432 H H H H H O tetrahydrofuran-3-yl H 2-C(?O)Me 0 A-3433 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2C(?O)CH.sub.3 0 A-3434 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2C(?O)CF.sub.3 0 A-3435 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2OH 0 A-3436 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2OCH.sub.3 0 A-3437 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-3438 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2SCH.sub.3 0 A-3439 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2S(?O)CH.sub.3 0 A-3440 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-3441 H H H H H O tetrahydrofuran-3-yl H 2-(benzyloxy) 0 A-3442 H H H H H O tetrahydrofuran-3-yl H 2-NH.sub.2 0 A-3443 H H H H H O tetrahydrofuran-3-yl H 2-NHMe 0 A-3444 H H H H H O tetrahydrofuran-3-yl H 2-N(Me).sub.2 0 A-3445 H H H H H O tetrahydrofuran-3-yl H 2-(1,3-dioxolan-2-yl) 0 A-3446 H H H H H O tetrahydrofuran-3-yl H 2-(1,3-dioxan-2-yl) 0 A-3447 H H H H H O tetrahydrofuran-3-yl H 2-(1H-imidazol-2-yl) 0 A-3448 H H H H H O tetrahydrofuran-3-yl H 2-(thiazol-2-yl) 0 A-3449 H H H H H O tetrahydrofuran-3-yl H 2-(oxazol-2-yl) 0 A-3450 H H H H H O tetrahydrofuran-3-yl H 2-CH?NOH 0 A-3451 H H H H H O tetrahydrofuran-3-yl H 2-CH?NOMe 0 A-3452 H H H H H O tetrahydrofuran-3-yl H 2-(4,5-dihydro-3-isoxazolyl) 0 A-3453 H H H H H O tetrahydrofuran-3-yl H 2-CN 0 A-3454 H H H H H O tetrahydrofuran-3-yl H 2-NO.sub.2 0 A-3455 H H H H H O tetrahydrofuran-3-yl H 2-F,6-Cl 0 A-3456 H H H H H O tetrahydrofuran-3-yl H 2-F,6-Me 0 A-3457 H H H H H O tetrahydrofuran-3-yl H 3-F,6-Me 0 A-3458 H H H H H O tetrahydrofuran-3-yl H 4-F,2-Me 0 A-3459 H H H H H O tetrahydrofuran-3-yl H 2-F,6-OMe 0 A-3460 H H H H H O tetrahydrofuran-3-yl H 3-F,6-OMe 0 A-3461 H H H H H O tetrahydrofuran-3-yl H 2,6-Cl.sub.2 0 A-3462 H H H H H O tetrahydrofuran-3-yl H 2-Cl,6-Me 0 A-3463 H H H H H O tetrahydrofuran-3-yl H 3-Cl,6-Me 0 A-3464 H H H H H O tetrahydrofuran-3-yl H 4-Cl,2-Me 0 A-3465 H H H H H O tetrahydrofuran-3-yl H 2-Cl,5-CF.sub.3 0 A-3466 H H H H H O tetrahydrofuran-3-yl H 2-Cl,6-CF.sub.3 0 A-3467 H H H H H O tetrahydrofuran-3-yl H 2-Cl,6-OMe 0 A-3468 H H H H H O tetrahydrofuran-3-yl H 3-Cl,6-OMe 0 A-3469 H H H H H O tetrahydrofuran-3-yl H 4-Cl,2-OMe 0 A-3470 H H H H H O tetrahydrofuran-3-yl H 2,4-Me.sub.2 0 A-3471 H H H H H O tetrahydrofuran-3-yl H 2,5-Me.sub.2 0 A-3472 H H H H H O tetrahydrofuran-3-yl H 2,6-Me.sub.2 0
(163) TABLE-US-00062 TABLE 62 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3473 H H H H H O tetrahydrofuran-3-yl H 2-Me,4-CF.sub.3 0 A-3474 H H H H H O tetrahydrofuran-3-yl H 2-Me,5-CF.sub.3 0 A-3475 H H H H H O tetrahydrofuran-3-yl H 2-Me,6-CF.sub.3 0 A-3476 H H H H H O tetrahydrofuran-3-yl H 2-Me,4-OMe 0 A-3477 H H H H H O tetrahydrofuran-3-yl H 2-Me,5-OMe 0 A-3478 H H H H H O tetrahydrofuran-3-yl H 2-Me,6-OMe 0 A-3479 H H H H H O tetrahydrofuran-3-yl H 3-Me,6-OMe 0 A-3480 H H H H H O tetrahydrofuran-3-yl H 4-Me,2-OMe 0 A-3481 H H H H H O tetrahydrofuran-3-yl H 2,5-OMe.sub.2 0 A-3482 H H H H H O tetrahydrofuran-3-yl H 2,6-OMe.sub.2 0 A-3483 H H H H H O tetrahydrofuran-3-yl H 2-OMe,6-CF.sub.3 0 A-3484 H H H H H O tetrahydrofuran-3-yl H 2-CHF.sub.2,5-F 0 A-3485 H H H H H O tetrahydrofuran-3-yl H 2-CHF.sub.2,6-F 0 A-3486 H H H H H O tetrahydrofuran-3-yl H 2-CHF.sub.2,5-Me 0 A-3487 H H H H H O tetrahydrofuran-3-yl H 2-CHF.sub.2,6-Me 0 A-3488 H H H H H O tetrahydrofuran-3-yl H 2-cyclopropyl,5-F 0 A-3489 H H H H H O tetrahydrofuran-3-yl H 2-cyclopropyl,6-F 0 A-3490 H H H H H O tetrahydrofuran-3-yl H 2-cyclopropyl,5-Me 0 A-3491 H H H H H O tetrahydrofuran-3-yl H 2-cyclopropyl,6-Me 0 A-3492 H H H H H O tetrahydrofuran-3-yl H 2-ethenyl,6-F 0 A-3493 H H H H H O tetrahydrofuran-3-yl H 2-ethenyl,6-Me 0 A-3494 H H H H H O tetrahydrofuran-3-yl H 2-OEt,5-F 0 A-3495 H H H H H O tetrahydrofuran-3-yl H 2-OEt,6-F 0 A-3496 H H H H H O tetrahydrofuran-3-yl H 2-OEt,5-Cl 0 A-3497 H H H H H O tetrahydrofuran-3-yl H 2-OEt,6-Cl 0 A-3498 H H H H H O tetrahydrofuran-3-yl H 2-OEt,5-Me 0 A-3499 H H H H H O tetrahydrofuran-3-yl H 2-OEt,6-Me 0 A-3500 H H H H H O tetrahydrofuran-3-yl H 2-OCHF.sub.2,5-F 0 A-3501 H H H H H O tetrahydrofuran-3-yl H 2-OCHF.sub.2,6-F 0 A-3502 H H H H H O tetrahydrofuran-3-yl H 2-OCHF.sub.2,5-Me 0 A-3503 H H H H H O tetrahydrofuran-3-yl H 2-OCHF.sub.2,6-Me 0 A-3504 H H H H H O tetrahydrofuran-3-yl H 2-(cyclopropyloxy),5-F 0 A-3505 H H H H H O tetrahydrofuran-3-yl H 2-(cyclopropyloxy),6-F 0 A-3506 H H H H H O tetrahydrofuran-3-yl H 2-(cyclopropyloxy),5-Me 0 A-3507 H H H H H O tetrahydrofuran-3-yl H 2-(cyclopropyloxy),6-Me 0 A-3508 H H H H H O tetrahydrofuran-3-yl H 2-SMe,5-F 0 A-3509 H H H H H O tetrahydrofuran-3-yl H 2-SMe,6-F 0 A-3510 H H H H H O tetrahydrofuran-3-yl H 2-SMe,5-Me 0 A-3511 H H H H H O tetrahydrofuran-3-yl H 2-SMe,6-Me 0 A-3512 H H H H H O tetrahydrofuran-3-yl H 2-S(?O)Me,5-F 0 A-3513 H H H H H O tetrahydrofuran-3-yl H 2-S(?O)Me,6-F 0 A-3514 H H H H H O tetrahydrofuran-3-yl H 2-S(?O)Me,5-Me 0 A-3515 H H H H H O tetrahydrofuran-3-yl H 2-S(?O)Me,6-Me 0 A-3516 H H H H H O tetrahydrofuran-3-yl H 2-S(?O).sub.2Me,5-F 0 A-3517 H H H H H O tetrahydrofuran-3-yl H 2-S(?O).sub.2Me,6-F 0 A-3518 H H H H H O tetrahydrofuran-3-yl H 2-S(?O).sub.2Me,5-Me 0 A-3519 H H H H H O tetrahydrofuran-3-yl H 2-S(?O).sub.2Me,6-Me 0 A-3520 H H H H H O tetrahydrofuran-3-yl H 2-SCF.sub.3,5-F 0 A-3521 H H H H H O tetrahydrofuran-3-yl H 2-SCF.sub.3,6-F 0 A-3522 H H H H H O tetrahydrofuran-3-yl H 2-SCF.sub.3,5-Me 0 A-3523 H H H H H O tetrahydrofuran-3-yl H 2-SCF.sub.3,6-Me 0 A-3524 H H H H H O tetrahydrofuran-3-yl H 2-S(?O)CF.sub.3,5-F 0 A-3525 H H H H H O tetrahydrofuran-3-yl H 2-S(?O)CF.sub.3,6-F 0 A-3526 H H H H H O tetrahydrofuran-3-yl H 2-S(?O)CF.sub.3,5-Me 0 A-3527 H H H H H O tetrahydrofuran-3-yl H 2-S(?O)CF.sub.3,6-Me 0 A-3528 H H H H H O tetrahydrofuran-3-yl H 2-S(?O).sub.2CF.sub.3,5-F 0 A-3529 H H H H H O tetrahydrofuran-3-yl H 2-S(?O).sub.2CF.sub.3,6-F 0
(164) TABLE-US-00063 TABLE 63 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3530 H H H H H O tetrahydrofuran-3-yl H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-3531 H H H H H O tetrahydrofuran-3-yl H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-3532 H H H H H O tetrahydrofuran-3-yl H 2-(cyclopropylthio),5-F 0 A-3533 H H H H H O tetrahydrofuran-3-yl H 2-(cyclopropylthio),6-F 0 A-3534 H H H H H O tetrahydrofuran-3-yl H 2-(cyclopropylthio),5-Me 0 A-3535 H H H H H O tetrahydrofuran-3-yl H 2-(cyclopropylthio),6-Me 0 A-3536 H H H H H O tetrahydrofuran-3-yl H 2-C(?O)Me,5-F 0 A-3537 H H H H H O tetrahydrofuran-3-yl H 2-C(?O)Me,6-F 0 A-3538 H H H H H O tetrahydrofuran-3-yl H 2-C(?O)Me,5-Me 0 A-3539 H H H H H O tetrahydrofuran-3-yl H 2-C(?O)Me,6-Me 0 A-3540 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2OH,5-F 0 A-3541 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2OH,6-F 0 A-3542 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2OH,5-Me 0 A-3543 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2OH,6-Me 0 A-3544 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2OCH.sub.3,4-F 0 A-3545 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2OCH.sub.3,5-F 0 A-3546 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2OCH.sub.3,6-F 0 A-3547 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2OCH.sub.3,4-Me 0 A-3548 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2OCH.sub.3,5-Me 0 A-3549 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2OCH.sub.3,6-Me 0 A-3550 H H H H H O tetrahydrofuran-3-yl H 2-OC(?O)CH.sub.3,5-F 0 A-3551 H H H H H O tetrahydrofuran-3-yl H 2-OC(?O)CH.sub.3,6-F 0 A-3552 H H H H H O tetrahydrofuran-3-yl H 2-OC(?O)CH.sub.3,5-Me 0 A-3553 H H H H H O tetrahydrofuran-3-yl H 2-OC(?O)CH.sub.3,6-Me 0 A-3554 H H H H H O tetrahydrofuran-3-yl H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-3555 H H H H H O tetrahydrofuran-3-yl H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-3556 H H H H H O tetrahydrofuran-3-yl H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-3557 H H H H H O tetrahydrofuran-3-yl H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-3558 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2SCH.sub.3,5-F 0 A-3559 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2SCH.sub.3,6-F 0 A-3560 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2SCH.sub.3,5-Me 0 A-3561 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2SCH.sub.3,6-Me 0 A-3562 H H H H H O tetrahydrofuran-3-yl H 2-NMe.sub.2,5-F 0 A-3563 H H H H H O tetrahydrofuran-3-yl H 2-NMe.sub.2,6-F 0 A-3564 H H H H H O tetrahydrofuran-3-yl H 2-NMe.sub.2,5-Me 0 A-3565 H H H H H O tetrahydrofuran-3-yl H 2-NMe.sub.2,6-Me 0 A-3566 H H H H H O tetrahydrofuran-3-yl H 2-CN,4-F 0 A-3567 H H H H H O tetrahydrofuran-3-yl H 2-CN,5-F 0 A-3568 H H H H H O tetrahydrofuran-3-yl H 2-CN,6-F 0 A-3569 H H H H H O tetrahydrofuran-3-yl H 2-CN,6-Me 0 A-3570 H H H H H O tetrahydrofuran-3-yl H 2-CN,5-OMe 0 A-3571 H H H H H O tetrahydrofuran-3-yl H 2-CN,6-OMe 0 A-3572 H H H H H O tetrahydrofuran-3-yl H 3-CN,6-Me 0 A-3573 H H H H H O tetrahydrofuran-3-yl H 3-CN,6-OMe 0 A-3574 H H H H H O tetrahydrofuran-3-yl H 4-CN,2-Me 0 A-3575 H H H H H O tetrahydrofuran-3-yl H 4-CN,2-OMe 0 A-3576 H H H H H O tetrahydrofuran-3-yl H 2-NO.sub.2,4-F 0 A-3577 H H H H H O tetrahydrofuran-3-yl H 2-NO.sub.2,5-F 0 A-3578 H H H H H O tetrahydrofuran-3-yl H 2-NO.sub.2,6-F 0 A-3579 H H H H H O tetrahydrofuran-3-yl H 2-NO.sub.2,4-Me 0 A-3580 H H H H H O tetrahydrofuran-3-yl H 2-NO.sub.2,5-Me 0 A-3581 H H H H H O tetrahydrofuran-3-yl H 2-NO.sub.2,6-Me 0 A-3582 H H H H H O tetrahydrofuran-3-yl H 2-Me,4,5-F.sub.2 0 A-3583 H H H H H O tetrahydrofuran-3-yl H 2-Me,6-Et 0 A-3584 H H H H H O tetrahydrofuran-3-yl H 2-cyclopropyl,6-OMe 0 A-3585 H H H H H O tetrahydrofuran-3-yl H 2-Me,5-Et 0 A-3586 H H H H H O tetrahydrofuran-3-yl H 2,6-Et.sub.2 0
(165) TABLE-US-00064 TABLE 64 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3587 H H H H H O tetrahydrofuran-3-yl H 2-Et,6-F 0 A-3588 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-3589 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-3590 H H H H H O tetrahydrofuran-3-yl H 2-CH.sub.2NMe.sub.2 0 A-3591 H H H H H O tetrahydropyran-4-yl H H 0 A-3592 H H H H H O tetrahydropyran-4-yl H 2-F 0 A-3593 H H H H H O tetrahydropyran-4-yl H 2-Cl 0 A-3594 H H H H H O tetrahydropyran-4-yl H 2-Br 0 A-3595 H H H H H O tetrahydropyran-4-yl H 2-OH 0 A-3596 H H H H H O tetrahydropyran-4-yl H 2-Me 0 A-3597 H H H H H O tetrahydropyran-4-yl H 2-Et 0 A-3598 H H H H H O tetrahydropyran-4-yl H 2-Pr 0 A-3599 H H H H H O tetrahydropyran-4-yl H 2-CF.sub.3 0 A-3600 H H H H H O tetrahydropyran-4-yl H 2-CHF.sub.2 0 A-3601 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2F 0 A-3602 H H H H H O tetrahydropyran-4-yl H 2-CF.sub.2Cl 0 A-3603 H H H H H O tetrahydropyran-4-yl H 2-cyclopropyl 0 A-3604 H H H H H O tetrahydropyran-4-yl H 2-cyclobutyl 0 A-3605 H H H H H O tetrahydropyran-4-yl H 2-cyclopentyl 0 A-3606 H H H H H O tetrahydropyran-4-yl H 2-ethenyl 0 A-3607 H H H H H O tetrahydropyran-4-yl H 2-allyl 0 A-3608 H H H H H O tetrahydropyran-4-yl H 2-(prop-1-en-1-y) 0 A-3609 H H H H H O tetrahydropyran-4-yl H 2-(trifluoroethenyl) 0 A-3610 H H H H H O tetrahydropyran-4-yl H 2-OMe 0 A-3611 H H H H H O tetrahydropyran-4-yl H 2-OEt 0 A-3612 H H H H H O tetrahydropyran-4-yl H 2-OPr 0 A-3613 H H H H H O tetrahydropyran-4-yl H 2-O(i-Pr) 0 A-3614 H H H H H O tetrahydropyran-4-yl H 2-OCF.sub.3 0 A-3615 H H H H H O tetrahydropyran-4-yl H 2-OCHF.sub.2 0 A-3616 H H H H H O tetrahydropyran-4-yl H 2-(cyclopropyloxy) 0 A-3617 H H H H H O tetrahydropyran-4-yl H 2-(cyclobutyloxy) 0 A-3618 H H H H H O tetrahydropyran-4-yl H 2-(cyclopentyloxy) 0 A-3619 H H H H H O tetrahydropyran-4-yl H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-3620 H H H H H O tetrahydropyran-4-yl H 2-(oxiran-2-yl) 0 A-3621 H H H H H O tetrahydropyran-4-yl H 2-SMe 0 A-3622 H H H H H O tetrahydropyran-4-yl H 3-SMe 0 A-3623 H H H H H O tetrahydropyran-4-yl H 2-S(?O)Me 0 A-3624 H H H H H O tetrahydropyran-4-yl H 3-S(?O)Me 0 A-3625 H H H H H O tetrahydropyran-4-yl H 2-S(?O).sub.2Me 0 A-3626 H H H H H O tetrahydropyran-4-yl H 3-S(?O).sub.2Me 0 A-3627 H H H H H O tetrahydropyran-4-yl H 2-SCF.sub.3 0 A-3628 H H H H H O tetrahydropyran-4-yl H 3-SCF.sub.3 0 A-3629 H H H H H O tetrahydropyran-4-yl H 3-S(?O)CF.sub.3 0 A-3630 H H H H H O tetrahydropyran-4-yl H 3-SCF(CF.sub.3).sub.2 0 A-3631 H H H H H O tetrahydropyran-4-yl H 2-(cyclopropylthio) 0 A-3632 H H H H H O tetrahydropyran-4-yl H 2-(cyclopropylsulfinyl) 0 A-3633 H H H H H O tetrahydropyran-4-yl H 2-(cyclopropylsulfonyl) 0 A-3634 H H H H H O tetrahydropyran-4-yl H 2-C(?O)Me 0 A-3635 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2C(?O)CH.sub.3 0 A-3636 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2C(?O)CF.sub.3 0 A-3637 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2OH 0 A-3638 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2OCH.sub.3 0 A-3639 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-3640 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2SCH.sub.3 0 A-3641 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2S(?O)CH.sub.3 0 A-3642 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-3643 H H H H H O tetrahydropyran-4-yl H 2-(benzyloxy) 0
(166) TABLE-US-00065 TABLE 65 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3644 H H H H H O tetrahydropyran-4-yl H 2-NH.sub.2 0 A-3645 H H H H H O tetrahydropyran-4-yl H 2-NHMe 0 A-3646 H H H H H O tetrahydropyran-4-yl H 2-N(Me).sub.2 0 A-3647 H H H H H O tetrahydropyran-4-yl H 2-(1,3-dioxolan-2-yl) 0 A-3648 H H H H H O tetrahydropyran-4-yl H 2-(1,3-dioxan-2-yl) 0 A-3649 H H H H H O tetrahydropyran-4-yl H 2-(1H-imidazol-2-yl) 0 A-3650 H H H H H O tetrahydropyran-4-yl H 2-(thiazol-2-yl) 0 A-3651 H H H H H O tetrahydropyran-4-yl H 2-(oxazol-2-yl) 0 A-3652 H H H H H O tetrahydropyran-4-yl H 2-CH?NOH 0 A-3653 H H H H H O tetrahydropyran-4-yl H 2-CH?NOMe 0 A-3654 H H H H H O tetrahydropyran-4-yl H 2-(4,5-dihydro-3-isoxazolyl) 0 A-3655 H H H H H O tetrahydropyran-4-yl H 2-CN 0 A-3656 H H H H H O tetrahydropyran-4-yl H 2-NO.sub.2 0 A-3657 H H H H H O tetrahydropyran-4-yl H 2-F,6-Cl 0 A-3658 H H H H H O tetrahydropyran-4-yl H 2-F,6-Me 0 A-3659 H H H H H O tetrahydropyran-4-yl H 3-F,6-Me 0 A-3660 H H H H H O tetrahydropyran-4-yl H 4-F,2-Me 0 A-3661 H H H H H O tetrahydropyran-4-yl H 2-F,6-OMe 0 A-3662 H H H H H O tetrahydropyran-4-yl H 3-F,6-OMe 0 A-3663 H H H H H O tetrahydropyran-4-yl H 2,6-Cl.sub.2 0 A-3664 H H H H H O tetrahydropyran-4-yl H 2-Cl,6-Me 0 A-3665 H H H H H O tetrahydropyran-4-yl H 3-Cl,6-Me 0 A-3666 H H H H H O tetrahydropyran-4-yl H 4-Cl,2-Me 0 A-3667 H H H H H O tetrahydropyran-4-yl H 2-Cl,5-CF.sub.3 0 A-3668 H H H H H O tetrahydropyran-4-yl H 2-Cl,6-CF.sub.3 0 A-3669 H H H H H O tetrahydropyran-4-yl H 2-Cl,6-OMe 0 A-3670 H H H H H O tetrahydropyran-4-yl H 3-Cl,6-OMe 0 A-3671 H H H H H O tetrahydropyran-4-yl H 4-Cl,2-OMe 0 A-3672 H H H H H O tetrahydropyran-4-yl H 2,4-Me.sub.2 0 A-3673 H H H H H O tetrahydropyran-4-yl H 2,5-Me.sub.2 0 A-3674 H H H H H O tetrahydropyran-4-yl H 2,6-Me.sub.2 0 A-3675 H H H H H O tetrahydropyran-4-yl H 2-Me,4-CF.sub.3 0 A-3676 H H H H H O tetrahydropyran-4-yl H 2-Me,5-CF.sub.3 0 A-3677 H H H H H O tetrahydropyran-4-yl H 2-Me,6-CF.sub.3 0 A-3678 H H H H H O tetrahydropyran-4-yl H 2-Me,4-OMe 0 A-3679 H H H H H O tetrahydropyran-4-yl H 2-Me,5-OMe 0 A-3680 H H H H H O tetrahydropyran-4-yl H 2-Me,6-OMe 0 A-3681 H H H H H O tetrahydropyran-4-yl H 3-Me,6-OMe 0 A-3682 H H H H H O tetrahydropyran-4-yl H 4-Me,2-OMe 0 A-3683 H H H H H O tetrahydropyran-4-yl H 2,5-OMe.sub.2 0 A-3684 H H H H H O tetrahydropyran-4-yl H 2,6-OMe.sub.2 0 A-3685 H H H H H O tetrahydropyran-4-yl H 2-OMe,6-CF.sub.3 0 A-3686 H H H H H O tetrahydropyran-4-yl H 2-CHF.sub.2,5-F 0 A-3687 H H H H H O tetrahydropyran-4-yl H 2-CHF.sub.2,6-F 0 A-3688 H H H H H O tetrahydropyran-4-yl H 2-CHF.sub.2,5-Me 0 A-3689 H H H H H O tetrahydropyran-4-yl H 2-CHF.sub.2,6-Me 0 A-3690 H H H H H O tetrahydropyran-4-yl H 2-cyclopropyl,5-F 0 A-3691 H H H H H O tetrahydropyran-4-yl H 2-cyclopropyl,6-F 0 A-3692 H H H H H O tetrahydropyran-4-yl H 2-cyclopropyl,5-Me 0 A-3693 H H H H H O tetrahydropyran-4-yl H 2-cyclopropyl,6-Me 0 A-3694 H H H H H O tetrahydropyran-4-yl H 2-ethenyl,6-F 0 A-3695 H H H H H O tetrahydropyran-4-yl H 2-ethenyl,6-Me 0 A-3696 H H H H H O tetrahydropyran-4-yl H 2-OEt,5-F 0 A-3697 H H H H H O tetrahydropyran-4-yl H 2-OEt,6-F 0 A-3698 H H H H H O tetrahydropyran-4-yl H 2-OEt,5-Cl 0 A-3699 H H H H H O tetrahydropyran-4-yl H 2-OEt,6-Cl 0 A-3700 H H H H H O tetrahydropyran-4-yl H 2-OEt,5-Me 0
(167) TABLE-US-00066 TABLE 66 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3701 H H H H H O tetrahydropyran-4-yl H 2-OEt,6-Me 0 A-3702 H H H H H O tetrahydropyran-4-yl H 2-OCHF.sub.2,5-F 0 A-3703 H H H H H O tetrahydropyran-4-yl H 2-OCHF.sub.2,6-F 0 A-3704 H H H H H O tetrahydropyran-4-yl H 2-OCHF.sub.2,5-Me 0 A-3705 H H H H H O tetrahydropyran-4-yl H 2-OCHF.sub.2,6-Me 0 A-3706 H H H H H O tetrahydropyran-4-yl H 2-(cyclopropyloxy),5-F 0 A-3707 H H H H H O tetrahydropyran-4-yl H 2-(cyclopropyloxy),6-F 0 A-3708 H H H H H O tetrahydropyran-4-yl H 2-(cyclopropyloxy),5-Me 0 A-3709 H H H H H O tetrahydropyran-4-yl H 2-(cyclopropyloxy),6-Me 0 A-3710 H H H H H O tetrahydropyran-4-yl H 2-SMe,5-F 0 A-3711 H H H H H O tetrahydropyran-4-yl H 2-SMe,6-F 0 A-3712 H H H H H O tetrahydropyran-4-yl H 2-SMe,5-Me 0 A-3713 H H H H H O tetrahydropyran-4-yl H 2-SMe,6-Me 0 A-3714 H H H H H O tetrahydropyran-4-yl H 2-S(?O)Me,5-F 0 A-3715 H H H H H O tetrahydropyran-4-yl H 2-S(?O)Me,6-F 0 A-3716 H H H H H O tetrahydropyran-4-yl H 2-S(?O)Me,5-Me 0 A-3717 H H H H H O tetrahydropyran-4-yl H 2-S(?O)Me,6-Me 0 A-3718 H H H H H O tetrahydropyran-4-yl H 2-S(?O).sub.2Me,5-F 0 A-3719 H H H H H O tetrahydropyran-4-yl H 2-S(?O).sub.2Me,6-F 0 A-3720 H H H H H O tetrahydropyran-4-yl H 2-S(?O).sub.2Me,5-Me 0 A-3721 H H H H H O tetrahydropyran-4-yl H 2-S(?O).sub.2Me,6-Me 0 A-3722 H H H H H O tetrahydropyran-4-yl H 2-SCF.sub.3,5-F 0 A-3723 H H H H H O tetrahydropyran-4-yl H 2-SCF.sub.3,6-F 0 A-3724 H H H H H O tetrahydropyran-4-yl H 2-SCF.sub.3,5-Me 0 A-3725 H H H H H O tetrahydropyran-4-yl H 2-SCF.sub.3,6-Me 0 A-3726 H H H H H O tetrahydropyran-4-yl H 2-S(?O)CF.sub.3,5-F 0 A-3727 H H H H H O tetrahydropyran-4-yl H 2-S(?O)CF.sub.3,6-F 0 A-3728 H H H H H O tetrahydropyran-4-yl H 2-S(?O)CF.sub.3,5-Me 0 A-3729 H H H H H O tetrahydropyran-4-yl H 2-S(?O)CF.sub.3,6-Me 0 A-3730 H H H H H O tetrahydropyran-4-yl H 2-S(?O).sub.2CF.sub.3,5-F 0 A-3731 H H H H H O tetrahydropyran-4-yl H 2-S(?O).sub.2CF.sub.3,6-F 0 A-3732 H H H H H O tetrahydropyran-4-yl H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-3733 H H H H H O tetrahydropyran-4-yl H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-3734 H H H H H O tetrahydropyran-4-yl H 2-(cyclopropylthio),5-F 0 A-3735 H H H H H O tetrahydropyran-4-yl H 2-(cyclopropylthio),6-F 0 A-3736 H H H H H O tetrahydropyran-4-yl H 2-(cyclopropylthio),5-Me 0 A-3737 H H H H H O tetrahydropyran-4-yl H 2-(cyclopropylthio),6-Me 0 A-3738 H H H H H O tetrahydropyran-4-yl H 2-C(?O)Me,5-F 0 A-3739 H H H H H O tetrahydropyran-4-yl H 2-C(?O)Me,6-F 0 A-3740 H H H H H O tetrahydropyran-4-yl H 2-C(?O)Me,5-Me 0 A-3741 H H H H H O tetrahydropyran-4-yl H 2-C(?O)Me,6-Me 0 A-3742 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2OH,5-F 0 A-3743 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2OH,6-F 0 A-3744 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2OH,5-Me 0 A-3745 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2OH,6-Me 0 A-3746 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2OCH.sub.3,4-F 0 A-3747 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2OCH.sub.3,5-F 0 A-3748 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2OCH.sub.3,6-F 0 A-3749 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2OCH.sub.3,4-Me 0 A-3750 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2OCH.sub.3,5-Me 0 A-3751 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2OCH.sub.3,6-Me 0 A-3752 H H H H H O tetrahydropyran-4-yl H 2-OC(?O)CH.sub.3,5-F 0 A-3753 H H H H H O tetrahydropyran-4-yl H 2-OC(?O)CH.sub.3,6-F 0 A-3754 H H H H H O tetrahydropyran-4-yl H 2-OC(?O)CH.sub.3,5-Me 0 A-3755 H H H H H O tetrahydropyran-4-yl H 2-OC(?O)CH.sub.3,6-Me 0 A-3756 H H H H H O tetrahydropyran-4-yl H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-3757 H H H H H O tetrahydropyran-4-yl H 2-OS(?O).sub.2CH.sub.3,6-F 0
(168) TABLE-US-00067 TABLE 67 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3758 H H H H H O tetrahydropyran-4-yl H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-3759 H H H H H O tetrahydropyran-4-yl H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-3760 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2SCH.sub.3,5-F 0 A-3761 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2SCH.sub.3,6-F 0 A-3762 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2SCH.sub.3,5-Me 0 A-3763 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2SCH.sub.3,6-Me 0 A-3764 H H H H H O tetrahydropyran-4-yl H 2-NMe.sub.2,5-F 0 A-3765 H H H H H O tetrahydropyran-4-yl H 2-NMe.sub.2,6-F 0 A-3766 H H H H H O tetrahydropyran-4-yl H 2-NMe.sub.2,5-Me 0 A-3767 H H H H H O tetrahydropyran-4-yl H 2-NMe.sub.2,6-Me 0 A-3768 H H H H H O tetrahydropyran-4-yl H 2-CN,4-F 0 A-3769 H H H H H O tetrahydropyran-4-yl H 2-CN,5-F 0 A-3770 H H H H H O tetrahydropyran-4-yl H 2-CN,6-F 0 A-3771 H H H H H O tetrahydropyran-4-yl H 2-CN,6-Me 0 A-3772 H H H H H O tetrahydropyran-4-yl H 2-CN,5-OMe 0 A-3773 H H H H H O tetrahydropyran-4-yl H 2-CN,6-OMe 0 A-3774 H H H H H O tetrahydropyran-4-yl H 3-CN,6-Me 0 A-3775 H H H H H O tetrahydropyran-4-yl H 3-CN,6-OMe 0 A-3776 H H H H H O tetrahydropyran-4-yl H 4-CN,2-Me 0 A-3777 H H H H H O tetrahydropyran-4-yl H 4-CN,2-OMe 0 A-3778 H H H H H O tetrahydropyran-4-yl H 2-NO.sub.2,4-F 0 A-3779 H H H H H O tetrahydropyran-4-yl H 2-NO.sub.2,5-F 0 A-3780 H H H H H O tetrahydropyran-4-yl H 2-NO.sub.2,6-F 0 A-3781 H H H H H O tetrahydropyran-4-yl H 2-NO.sub.2,4-Me 0 A-3782 H H H H H O tetrahydropyran-4-yl H 2-NO.sub.2,5-Me 0 A-3783 H H H H H O tetrahydropyran-4-yl H 2-NO.sub.2,6-Me 0 A-3784 H H H H H O tetrahydropyran-4-yl H 2-Me,4,5-F.sub.2 0 A-3785 H H H H H O tetrahydropyran-4-yl H 2-Me,6-Et 0 A-3786 H H H H H O tetrahydropyran-4-yl H 2-cyclopropyl,6-OMe 0 A-3787 H H H H H O tetrahydropyran-4-yl H 2-Me,5-Et 0 A-3788 H H H H H O tetrahydropyran-4-yl H 2,6-Et.sub.2 0 A-3789 H H H H H O tetrahydropyran-4-yl H 2-Et,6-F 0 A-3790 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-3791 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-3792 H H H H H O tetrahydropyran-4-yl H 2-CH.sub.2NMe.sub.2 0 A-3793 H H H H H O CH.sub.2CN H H 0 A-3794 H H H H H O CH.sub.2CN H 2-F 0 A-3795 H H H H H O CH.sub.2CN H 2-Cl 0 A-3796 H H H H H O CH.sub.2CN H 2-Br 0 A-3797 H H H H H O CH.sub.2CN H 2-OH 0 A-3798 H H H H H O CH.sub.2CN H 2-Me 0 A-3799 H H H H H O CH.sub.2CN H 2-Et 0 A-3800 H H H H H O CH.sub.2CN H 2-Pr 0 A-3801 H H H H H O CH.sub.2CN H 2-CF.sub.3 0 A-3802 H H H H H O CH.sub.2CN H 2-CHF.sub.2 0 A-3803 H H H H H O CH.sub.2CN H 2-CH.sub.2F 0 A-3804 H H H H H O CH.sub.2CN H 2-CF.sub.2Cl 0 A-3805 H H H H H O CH.sub.2CN H 2-cyclopropyl 0 A-3806 H H H H H O CH.sub.2CN H 2-cyclobutyl 0 A-3807 H H H H H O CH.sub.2CN H 2-cyclopentyl 0 A-3808 H H H H H O CH.sub.2CN H 2-ethenyl 0 A-3809 H H H H H O CH.sub.2CN H 2-allyl 0 A-3810 H H H H H O CH.sub.2CN H 2-(prop-1-en-1-yl) 0 A-3811 H H H H H O CH.sub.2CN H 2-(trifluoroethenyl) 0 A-3812 H H H H H O CH.sub.2CN H 2-OMe 0 A-3813 H H H H H O CH.sub.2CN H 2-OEt 0 A-3814 H H H H H O CH.sub.2CN H 2-OPr 0
(169) TABLE-US-00068 TABLE 68 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3815 H H H H H O CH.sub.2CN H 2-O(i-Pr) 0 A-3816 H H H H H O CH.sub.2CN H 2-OCF.sub.3 0 A-3817 H H H H H O CH.sub.2CN H 2-OCHF.sub.2 0 A-3818 H H H H H O CH.sub.2CN H 2-(cyclopropyloxy) 0 A-3819 H H H H H O CH.sub.2CN H 2-(cyclobutyloxy) 0 A-3820 H H H H H O CH.sub.2CN H 2-(cyclopentyloxy) 0 A-3821 H H H H H O CH.sub.2CN H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-3822 H H H H H O CH.sub.2CN H 2-(oxiran-2-yl) 0 A-3823 H H H H H O CH.sub.2CN H 2-SMe 0 A-3824 H H H H H O CH.sub.2CN H 3-SMe 0 A-3825 H H H H H O CH.sub.2CN H 2-S(?O)Me 0 A-3826 H H H H H O CH.sub.2CN H 3-S(?O)Me 0 A-3827 H H H H H O CH.sub.2CN H 2-S(?O).sub.2Me 0 A-3828 H H H H H O CH.sub.2CN H 3-S(?O).sub.2Me 0 A-3829 H H H H H O CH.sub.2CN H 2-SCF.sub.3 0 A-3830 H H H H H O CH.sub.2CN H 3-SCF.sub.3 0 A-3831 H H H H H O CH.sub.2CN H 3-S(?O)CF.sub.3 0 A-3832 H H H H H O CH.sub.2CN H 3-SCF(CF.sub.3).sub.2 0 A-3833 H H H H H O CH.sub.2CN H 2-(cyclopropylthio) 0 A-3834 H H H H H O CH.sub.2CN H 2-(cyclopropylsulfinyl) 0 A-3835 H H H H H O CH.sub.2CN H 2-(cyclopropylsulfonyl) 0 A-3836 H H H H H O CH.sub.2CN H 2-C(?O)Me 0 A-3837 H H H H H O CH.sub.2CN H 2-CH.sub.2C(?O)CH.sub.3 0 A-3838 H H H H H O CH.sub.2CN H 2-CH.sub.2C(?O)CF.sub.3 0 A-3839 H H H H H O CH.sub.2CN H 2-CH.sub.2OH 0 A-3840 H H H H H O CH.sub.2CN H 2-CH.sub.2OCH.sub.3 0 A-3841 H H H H H O CH.sub.2CN H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-3842 H H H H H O CH.sub.2CN H 2-CH.sub.2SCH.sub.3 0 A-3843 H H H H H O CH.sub.2CN H 2-CH.sub.2S(?O)CH.sub.3 0 A-3844 H H H H H O CH.sub.2CN H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-3845 H H H H H O CH.sub.2CN H 2-(benzyloxy) 0 A-3846 H H H H H O CH.sub.2CN H 2-NH.sub.2 0 A-3847 H H H H H O CH.sub.2CN H 2-NHMe 0 A-3848 H H H H H O CH.sub.2CN H 2-N(Me).sub.2 0 A-3849 H H H H H O CH.sub.2CN H 2-(1,3-dioxolan-2-yl) 0 A-3850 H H H H H O CH.sub.2CN H 2-(1,3-dioxan-2-yl) 0 A-3851 H H H H H O CH.sub.2CN H 2-(1H-imidazol-2-yl) 0 A-3852 H H H H H O CH.sub.2CN H 2-(thiazol-2-yl) 0 A-3853 H H H H H O CH.sub.2CN H 2-(oxazol-2-yl) 0 A-3854 H H H H H O CH.sub.2CN H 2-CH?NOH 0 A-3855 H H H H H O CH.sub.2CN H 2-CH?NOMe 0 A-3856 H H H H H O CH.sub.2CN H 2-(4,5-dihydro-3-isoxazolyl) 0 A-3857 H H H H H O CH.sub.2CN H 2-CN 0 A-3858 H H H H H O CH.sub.2CN H 2-NO.sub.2 0 A-3859 H H H H H O CH.sub.2CN H 2-F,6-Cl 0 A-3860 H H H H H O CH.sub.2CN H 2-F,6-Me 0 A-3861 H H H H H O CH.sub.2CN H 3-F,6-Me 0 A-3862 H H H H H O CH.sub.2CN H 4-F,2-Me 0 A-3863 H H H H H O CH.sub.2CN H 2-F,6-OMe 0 A-3864 H H H H H O CH.sub.2CN H 3-F,6-OMe 0 A-3865 H H H H H O CH.sub.2CN H 2,6-Cl.sub.2 0 A-3866 H H H H H O CH.sub.2CN H 2-Cl,6-Me 0 A-3867 H H H H H O CH.sub.2CN H 3-Cl,6-Me 0 A-3868 H H H H H O CH.sub.2CN H 4-Cl,2-Me 0 A-3869 H H H H H O CH.sub.2CN H 2-Cl,5-CF.sub.3 0 A-3870 H H H H H O CH.sub.2CN H 2-Cl,6-CF.sub.3 0 A-3871 H H H H H O CH.sub.2CN H 2-Cl,6-OMe 0
(170) TABLE-US-00069 TABLE 69 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3872 H H H H H O CH.sub.2CN H 3-Cl,6-OMe 0 A-3873 H H H H H O CH.sub.2CN H 4-Cl,2-OMe 0 A-3874 H H H H H O CH.sub.2CN H 2,4-Me.sub.2 0 A-3875 H H H H H O CH.sub.2CN H 2,5-Me.sub.2 0 A-3876 H H H H H O CH.sub.2CN H 2,6-Me.sub.2 0 A-3877 H H H H H O CH.sub.2CN H 2-Me,4-CF.sub.3 0 A-3878 H H H H H O CH.sub.2CN H 2-Me,5-CF.sub.3 0 A-3879 H H H H H O CH.sub.2CN H 2-Me,6-CF.sub.3 0 A-3880 H H H H H O CH.sub.2CN H 2-Me,4-OMe 0 A-3881 H H H H H O CH.sub.2CN H 2-Me,5-OMe 0 A-3882 H H H H H O CH.sub.2CN H 2-Me,6-OMe 0 A-3883 H H H H H O CH.sub.2CN H 3-Me,6-OMe 0 A-3884 H H H H H O CH.sub.2CN H 4-Me,2-OMe 0 A-3885 H H H H H O CH.sub.2CN H 2,5-OMe.sub.2 0 A-3886 H H H H H O CH.sub.2CN H 2,6-OMe.sub.2 0 A-3887 H H H H H O CH.sub.2CN H 2-OMe,6-CF.sub.3 0 A-3888 H H H H H O CH.sub.2CN H 2-CHF.sub.2,5-F 0 A-3889 H H H H H O CH.sub.2CN H 2-CHF.sub.2,6-F 0 A-3890 H H H H H O CH.sub.2CN H 2-CHF.sub.2,5-Me 0 A-3891 H H H H H O CH.sub.2CN H 2-CHF.sub.2,6-Me 0 A-3892 H H H H H O CH.sub.2CN H 2-cyclopropyl,5-F 0 A-3893 H H H H H O CH.sub.2CN H 2-cyclopropyl,6-F 0 A-3894 H H H H H O CH.sub.2CN H 2-cyclopropyl,5-Me 0 A-3895 H H H H H O CH.sub.2CN H 2-cyclopropyl,6-Me 0 A-3896 H H H H H O CH.sub.2CN H 2-ethenyl,6-F 0 A-3897 H H H H H O CH.sub.2CN H 2-ethenyl,6-Me 0 A-3898 H H H H H O CH.sub.2CN H 2-OEt,5-F 0 A-3899 H H H H H O CH.sub.2CN H 2-OEt,6-F 0 A-3900 H H H H H O CH.sub.2CN H 2-OEt,5-Cl 0 A-3901 H H H H H O CH.sub.2CN H 2-OEt,6-Cl 0 A-3902 H H H H H O CH.sub.2CN H 2-OEt,5-Me 0 A-3903 H H H H H O CH.sub.2CN H 2-OEt,6-Me 0 A-3904 H H H H H O CH.sub.2CN H 2-OCHF.sub.2,5-F 0 A-3905 H H H H H O CH.sub.2CN H 2-OCHF.sub.2,6-F 0 A-3906 H H H H H O CH.sub.2CN H 2-OCHF.sub.2,5-Me 0 A-3907 H H H H H O CH.sub.2CN H 2-OCHF.sub.2,6-Me 0 A-3908 H H H H H O CH.sub.2CN H 2-(cyclopropyloxy),5-F 0 A-3909 H H H H H O CH.sub.2CN H 2-(cyclopropyloxy),6-F 0 A-3910 H H H H H O CH.sub.2CN H 2-(cyclopropyloxy),5-Me 0 A-3911 H H H H H O CH.sub.2CN H 2-(cyclopropyloxy),6-Me 0 A-3912 H H H H H O CH.sub.2CN H 2-SMe,5-F 0 A-3913 H H H H H O CH.sub.2CN H 2-SMe,6-F 0 A-3914 H H H H H O CH.sub.2CN H 2-SMe,5-Me 0 A-3915 H H H H H O CH.sub.2CN H 2-SMe,6-Me 0 A-3916 H H H H H O CH.sub.2CN H 2-S(?O)Me,5-F 0 A-3917 H H H H H O CH.sub.2CN H 2-S(?O)Me,6-F 0 A-3918 H H H H H O CH.sub.2CN H 2-S(?O)Me,5-Me 0 A-3919 H H H H H O CH.sub.2CN H 2-S(?O)Me,6-Me 0 A-3920 H H H H H O CH.sub.2CN H 2-S(?O).sub.2Me,5-F 0 A-3921 H H H H H O CH.sub.2CN H 2-S(?O).sub.2Me,6-F 0 A-3922 H H H H H O CH.sub.2CN H 2-S(?O).sub.2Me,5-Me 0 A-3923 H H H H H O CH.sub.2CN H 2-S(?O).sub.2Me,6-Me 0 A-3924 H H H H H O CH.sub.2CN H 2-SCF.sub.3,5-F 0 A-3925 H H H H H O CH.sub.2CN H 2-SCF.sub.3,6-F 0 A-3926 H H H H H O CH.sub.2CN H 2-SCF.sub.3,5-Me 0 A-3927 H H H H H O CH.sub.2CN H 2-SCF.sub.3,6-Me 0 A-3928 H H H H H O CH.sub.2CN H 2-S(?O)CF.sub.3,5-F 0
(171) TABLE-US-00070 TABLE 70 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3929 H H H H H O CH.sub.2CN H 2-S(?O)CF.sub.3,6-F 0 A-3930 H H H H H O CH.sub.2CN H 2-S(?O)CF.sub.3,5-Me 0 A-3931 H H H H H O CH.sub.2CN H 2-S(?O)CF.sub.3,6-Me 0 A-3932 H H H H H O CH.sub.2CN H 2-S(?O).sub.2CF.sub.3,5-F 0 A-3933 H H H H H O CH.sub.2CN H 2-S(?O).sub.2CF.sub.3,6-F 0 A-3934 H H H H H O CH.sub.2CN H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-3935 H H H H H O CH.sub.2CN H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-3936 H H H H H O CH.sub.2CN H 2-(cyclopropylthio),5-F 0 A-3937 H H H H H O CH.sub.2CN H 2-(cyclopropylthio),6-F 0 A-3938 H H H H H O CH.sub.2CN H 2-(cyclopropylthio),5-Me 0 A-3939 H H H H H O CH.sub.2CN H 2-(cyclopropylthio),6-Me 0 A-3940 H H H H H O CH.sub.2CN H 2-C(?O)Me,5-F 0 A-3941 H H H H H O CH.sub.2CN H 2-C(?O)Me,6-F 0 A-3942 H H H H H O CH.sub.2CN H 2-C(?O)Me,5-Me 0 A-3943 H H H H H O CH.sub.2CN H 2-C(?O)Me,6-Me 0 A-3944 H H H H H O CH.sub.2CN H 2-CH.sub.2OH,5-F 0 A-3945 H H H H H O CH.sub.2CN H 2-CH.sub.2OH,6-F 0 A-3946 H H H H H O CH.sub.2CN H 2-CH.sub.2OH,5-Me 0 A-3947 H H H H H O CH.sub.2CN H 2-CH.sub.2OH,6-Me 0 A-3948 H H H H H O CH.sub.2CN H 2-CH.sub.2OCH.sub.3,4-F 0 A-3949 H H H H H O CH.sub.2CN H 2-CH.sub.2OCH.sub.3,5-F 0 A-3950 H H H H H O CH.sub.2CN H 2-CH.sub.2OCH.sub.3,6-F 0 A-3951 H H H H H O CH.sub.2CN H 2-CH.sub.2OCH.sub.3,4-Me 0 A-3952 H H H H H O CH.sub.2CN H 2-CH.sub.2OCH.sub.3,5-Me 0 A-3953 H H H H H O CH.sub.2CN H 2-CH.sub.2OCH.sub.3,6-Me 0 A-3954 H H H H H O CH.sub.2CN H 2-OC(?O)CH.sub.3,5-F 0 A-3955 H H H H H O CH.sub.2CN H 2-OC(?O)CH.sub.3,6-F 0 A-3956 H H H H H O CH.sub.2CN H 2-OC(?O)CH.sub.3,5-Me 0 A-3957 H H H H H O CH.sub.2CN H 2-OC(?O)CH.sub.3,6-Me 0 A-3958 H H H H H O CH.sub.2CN H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-3959 H H H H H O CH.sub.2CN H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-3960 H H H H H O CH.sub.2CN H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-3961 H H H H H O CH.sub.2CN H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-3962 H H H H H O CH.sub.2CN H 2-CH.sub.2SCH.sub.3,5-F 0 A-3963 H H H H H O CH.sub.2CN H 2-CH.sub.2SCH.sub.3,6-F 0 A-3964 H H H H H O CH.sub.2CN H 2-CH.sub.2SCH.sub.3,5-Me 0 A-3965 H H H H H O CH.sub.2CN H 2-CH.sub.2SCH.sub.3,6-Me 0 A-3966 H H H H H O CH.sub.2CN H 2-NMe.sub.2,5-F 0 A-3967 H H H H H O CH.sub.2CN H 2-NMe.sub.2,6-F 0 A-3968 H H H H H O CH.sub.2CN H 2-NMe.sub.2,5-Me 0 A-3969 H H H H H O CH.sub.2CN H 2-NMe.sub.2,6-Me 0 A-3970 H H H H H O CH.sub.2CN H 2-CN,4-F 0 A-3971 H H H H H O CH.sub.2CN H 2-CN,5-F 0 A-3972 H H H H H O CH.sub.2CN H 2-CN,6-F 0 A-3973 H H H H H O CH.sub.2CN H 2-CN,6-Me 0 A-3974 H H H H H O CH.sub.2CN H 2-CN,5-OMe 0 A-3975 H H H H H O CH.sub.2CN H 2-CN,6-OMe 0 A-3976 H H H H H O CH.sub.2CN H 3-CN,6-Me 0 A-3977 H H H H H O CH.sub.2CN H 3-CN,6-OMe 0 A-3978 H H H H H O CH.sub.2CN H 4-CN,2-Me 0 A-3979 H H H H H O CH.sub.2CN H 4-CN,2-OMe 0 A-3980 H H H H H O CH.sub.2CN H 2-NO.sub.2,4-F 0 A-3981 H H H H H O CH.sub.2CN H 2-NO.sub.2,5-F 0 A-3982 H H H H H O CH.sub.2CN H 2-NO.sub.2,6-F 0 A-3983 H H H H H O CH.sub.2CN H 2-NO.sub.2,4-Me 0 A-3984 H H H H H O CH.sub.2CN H 2-NO.sub.2,5-Me 0 A-3985 H H H H H O CH.sub.2CN H 2-NO.sub.2,6-Me 0
(172) TABLE-US-00071 TABLE 71 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-3986 H H H H H O CH.sub.2CN H 2-Me,4,5-F.sub.2 0 A-3987 H H H H H O CH.sub.2CN H 2-Me,6-Et 0 A-3988 H H H H H O CH.sub.2CN H 2-cyclopropyl,6-OMe 0 A-3989 H H H H H O CH.sub.2CN H 2-Me,5-Et 0 A-3990 H H H H H O CH.sub.2CN H 2,6-Et.sub.2 0 A-3991 H H H H H O CH.sub.2CN H 2-Et,6F 0 A-3992 H H H H H O CH.sub.2CN H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-3993 H H H H H O CH.sub.2CN H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-3994 H H H H H O CH.sub.2CN H 2-CH.sub.2NMe.sub.2 0 A-3995 H H H H H O 1-CN-cyclopropyl H H 0 A-3996 H H H H H O 1-CN-cyclopropyl H 2-F 0 A-3997 H H H H H O 1-CN-cyclopropyl H 2-Cl 0 A-3998 H H H H H O 1-CN-cyclopropyl H 2-Br 0 A-3999 H H H H H O 1-CN-cyclopropyl H 2-OH 0 A-4000 H H H H H O 1-CN-cyclopropyl H 2-Me 0 A-4001 H H H H H O 1-CN-cyclopropyl H 2-Et 0 A-4002 H H H H H O 1-CN-cyclopropyl H 2-Pr 0 A-4003 H H H H H O 1-CN-cyclopropyl H 2-CF.sub.3 0 A-4004 H H H H H O 1-CN-cyclopropyl H 2-CHF.sub.2 0 A-4005 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2F 0 A-4006 H H H H H O 1-CN-cyclopropyl H 2-CF.sub.2Cl 0 A-4007 H H H H H O 1-CN-cyclopropyl H 2-cyclopropyl 0 A-4008 H H H H H O 1-CN-cyclopropyl H 2-cyclobutyl 0 A-4009 H H H H H O 1-CN-cyclopropyl H 2-cyclopentyl 0 A-4010 H H H H H O 1-CN-cyclopropyl H 2-ethenyl 0 A-4011 H H H H H O 1-CN-cyclopropyl H 2-allyl 0 A-4012 H H H H H O 1-CN-cyclopropyl H 2-(prop-1-en-1-yl) 0 A-4013 H H H H H O 1-CN-cyclopropyl H 2-(trifluoroethenyl) 0 A-4014 H H H H H O 1-CN-cyclopropyl H 2-OMe 0 A-4015 H H H H H O 1-CN-cyclopropyl H 2-OEt 0 A-4016 H H H H H O 1-CN-cyclopropyl H 2-OPr 0 A-4017 H H H H H O 1-CN-cyclopropyl H 2-O(i-Pr) 0 A-4018 H H H H H O 1-CN-cyclopropyl H 2-OCF.sub.3 0 A-4019 H H H H H O 1-CN-cyclopropyl H 2-OCHF.sub.2 0 A-4020 H H H H H O 1-CN-cyclopropyl H 2-(cyclopropyloxy) 0 A-4021 H H H H H O 1-CN-cyclopropyl H 2-(cyclobutyloxy) 0 A-4022 H H H H H O 1-CN-cyclopropyl H 2-(cyclopentyloxy) 0 A-4023 H H H H H O 1-CN-cyclopropyl H 2-((2,2-dichbrocyclopropyl)oxy) 0 A-4024 H H H H H O 1-CN-cyclopropyl H 2-(oxiran-2-yl) 0 A-4025 H H H H H O 1-CN-cyclopropyl H 2-SMe 0 A-4026 H H H H H O 1-CN-cyclopropyl H 3-SMe 0 A-4027 H H H H H O 1-CN-cyclopropyl H 2-S(?O)Me 0 A-4028 H H H H H O 1-CN-cyclopropyl H 3-S(?O)Me 0 A-4029 H H H H H O 1-CN-cyclopropyl H 2-S(?O).sub.2Me 0 A-4030 H H H H H O 1-CN-cyclopropyl H 3-S(?O).sub.2Me 0 A-4031 H H H H H O 1-CN-cyclopropyl H 2-SCF.sub.3 0 A-4032 H H H H H O 1-CN-cyclopropyl H 3-SCF.sub.3 0 A-4033 H H H H H O 1-CN-cyclopropyl H 3-S(?O)CF.sub.3 0 A-4034 H H H H H O 1-CN-cyclopropyl H 3-SCF(CF.sub.3).sub.2 0 A-4035 H H H H H O 1-CN-cyclopropyl H 2-(cyclopropylthio) 0 A-4036 H H H H H O 1-CN-cyclopropyl H 2-(cyclopropylsulfinyl) 0 A-4037 H H H H H O 1-CN-cyclopropyl H 2-(cyclopropylsulfonyl) 0 A-4038 H H H H H O 1-CN-cyclopropyl H 2-C(?O)Me 0 A-4039 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2C(?O)CH.sub.3 0 A-4040 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2C(?O)CF.sub.3 0 A-4041 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2OH 0 A-4042 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2OCH.sub.3 0
(173) TABLE-US-00072 TABLE 72 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4043 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-4044 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2SCH 0 A-4045 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2S(?O)CH.sub.3 0 A-4046 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-4047 H H H H H O 1-CN-cyclopropyl H 2-(benzylboxy) 0 A-4048 H H H H H O 1-CN-cyclopropyl H 2-NH.sub.2 0 A-4049 H H H H H O 1-CN-cyclopropyl H 2-NHMe 0 A-4050 H H H H H O 1-CN-cyclopropyl H 2-N(Me).sub.2 0 A-4051 H H H H H O 1-CN-cyclopropyl H 2-(1,3-dioxolan-2-yl) 0 A-4052 H H H H H O 1-CN-cyclopropyl H 2-(1,3-dioxan-2-yl) 0 A-4053 H H H H H O 1-CN-cyclopropyl H 2-(1H-imidazo-2-yl) 0 A-4054 H H H H H O 1-CN-cyclopropyl H 2-(thiazol-2-yl) 0 A-4055 H H H H H O 1-CN-cyclopropyl H 2-(oxazol-2-yl) 0 A-4056 H H H H H O 1-CN-cyclopropyl H 2-CH?NOH 0 A-4057 H H H H H O 1-CN-cyclopropyl H 2-CH?NOMe 0 A-4058 H H H H H O 1-CN-cyclopropyl H 2-(4,5-dihydro-3-isoxazolyl) 0 A-4059 H H H H H O 1-CN-cyclopropyl H 2-CN 0 A-4060 H H H H H O 1-CN-cyclopropyl H 2-NO.sub.2 0 A-4061 H H H H H O 1-CN-cyclopropyl H 2-F,6-Cl 0 A-4062 H H H H H O 1-CN-cyclopropyl H 2-F,6-Me 0 A-4063 H H H H H O 1-CN-cyclopropyl H 3-F,6-Me 0 A-4064 H H H H H O 1-CN-cyclopropyl H 4-F,2-Me 0 A-4065 H H H H H O 1-CN-cyclopropyl H 2-F,6-OMe 0 A-4066 H H H H H O 1-CN-cyclopropyl H 3-F,6-OMe 0 A-4067 H H H H H O 1-CN-cyclopropyl H 2,6-Cl.sub.2 0 A-4068 H H H H H O 1-CN-cyclopropyl H 2-Cl,6-Me 0 A-4069 H H H H H O 1-CN-cyclopropyl H 3-Cl,6-Me 0 A-4070 H H H H H O 1-CN-cyclopropyl H 4-Cl,2-Me 0 A-4071 H H H H H O 1-CN-cyclopropyl H 2-Cl,5-CF.sub.3 0 A-4072 H H H H H O 1-CN-cyclopropyl H 2-Cl,6-CF.sub.3 0 A-4073 H H H H H O 1-CN-cyclopropyl H 2-Cl,6-OMe 0 A-4074 H H H H H O 1-CN-cyclopropyl H 3-Cl,6-OMe 0 A-4075 H H H H H O 1-CN-cyclopropyl H 4-Cl,2-OMe 0 A-4076 H H H H H O 1-CN-cyclopropyl H 2,4-Me.sub.2 0 A-4077 H H H H H O 1-CN-cyclopropyl H 2,5-Me.sub.2 0 A-4078 H H H H H O 1-CN-cyclopropyl H 2,6-Me.sub.2 0 A-4079 H H H H H O 1-CN-cyclopropyl H 2-Me,4-CF.sub.3 0 A-4080 H H H H H O 1-CN-cyclopropyl H 2-Me,5-CF.sub.3 0 A-4081 H H H H H O 1-CN-cyclopropyl H 2-Me,6-CF.sub.3 0 A-4082 H H H H H O 1-CN-cyclopropyl H 2-Me,4-OMe 0 A-4083 H H H H H O 1-CN-cyclopropyl H 2-Me,5-OMe 0 A-4084 H H H H H O 1-CN-cyclopropyl H 2-Me,6-OMe 0 A-4085 H H H H H O 1-CN-cyclopropyl H 3-Me,6-OMe 0 A-4086 H H H H H O 1-CN-cyclopropyl H 4-Me,2-OMe 0 A-4087 H H H H H O 1-CN-cyclopropyl H 2,5-OMe.sub.2 0 A-4088 H H H H H O 1-CN-cyclopropyl H 2,6-OMe.sub.2 0 A-4089 H H H H H O 1-CN-cyclopropyl H 2-OMe,6-CF.sub.3 0 A-4090 H H H H H O 1-CN-cyclopropyl H 2-CHF.sub.2,5-F 0 A-4091 H H H H H O 1-CN-cyclopropyl H 2-CHF.sub.2,6-F 0 A-4092 H H H H H O 1-CN-cyclopropyl H 2-CHF.sub.2,5-Me 0 A-4093 H H H H H O 1-CN-cyclopropyl H 2-CHF.sub.2,6-Me 0 A-4094 H H H H H O 1-CN-cyclopropyl H 2-cyclopropyl,5-F 0 A-4095 H H H H H O 1-CN-cyclopropyl H 2-cyclopropyl,6-F 0 A-4096 H H H H H O 1-CN-cyclopropyl H 2-cyclopropyl,5-Me 0 A-4097 H H H H H O 1-CN-cyclopropyl H 2-cyclopropyl,6-Me 0 A-4098 H H H H H O 1-CN-cyclopropyl H 2-ethenyl,6-F 0 A-4099 H H H H H O 1-CN-cyclopropyl H 2-ethenyl,6-Me 0
(174) TABLE-US-00073 TABLE 73 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4100 H H H H H O 1-CN-cyclopropyl H 2-OEt,5-F 0 A-4101 H H H H H O 1-CN-cyclopropyl H 2-OEt,6-F 0 A-4102 H H H H H O 1-CN-cyclopropyl H 2-OEt,5-Cl 0 A-4103 H H H H H O 1-CN-cyclopropyl H 2-OEt,6-Cl 0 A-4104 H H H H H O 1-CN-cyclopropyl H 2-OEt,5-Me 0 A-4105 H H H H H O 1-CN-cyclopropyl H 2-OEt,6-Me 0 A-4106 H H H H H O 1-CN-cyclopropyl H 2-OCHF.sub.2,5-F 0 A-4107 H H H H H O 1-CN-cyclopropyl H 2-OCHF.sub.2,6-F 0 A-4108 H H H H H O 1-CN-cyclopropyl H 2-OCHF.sub.2,5-Me 0 A-4109 H H H H H O 1-CN-cyclopropyl H 2-OCHF.sub.2,6-Me 0 A-4110 H H H H H O 1-CN-cyclopropyl H 2-(cyclopropyloxy),5-F 0 A-4111 H H H H H O 1-CN-cyclopropyl H 2-(cyclopropyloxy),6-F 0 A-4112 H H H H H O 1-CN-cyclopropyl H 2-(cyclopropyloxy),5-Me 0 A-4113 H H H H H O 1-CN-cyclopropyl H 2-(cyclopropyloxy),6-Me 0 A-4114 H H H H H O 1-CN-cyclopropyl H 2-SMe,5-F 0 A-4115 H H H H H O 1-CN-cyclopropyl H 2-SMe,6-F 0 A-4116 H H H H H O 1-CN-cyclopropyl H 2-SMe,5-Me 0 A-4117 H H H H H O 1-CN-cyclopropyl H 2-SMe,6-Me 0 A-4118 H H H H H O 1-CN-cyclopropyl H 2-S(?O)Me,5-F 0 A-4119 H H H H H O 1-CN-cyclopropyl H 2-S(?O)Me,6-F 0 A-4120 H H H H H O 1-CN-cyclopropyl H 2-S(?O)Me,5-Me 0 A-4121 H H H H H O 1-CN-cyclopropyl H 2-S(?O)Me,6-Me 0 A-4122 H H H H H O 1-CN-cyclopropyl H 2-S(?O).sub.2Me,5-F 0 A-4123 H H H H H O 1-CN-cyclopropyl H 2-S(?O).sub.2Me,6-F 0 A-4124 H H H H H O 1-CN-cyclopropyl H 2-S(?O).sub.2Me,5-Me 0 A-4125 H H H H H O 1-CN-cyclopropyl H 2-S(?O).sub.2Me,6-Me 0 A-4126 H H H H H O 1-CN-cyclopropyl H 2-SCF.sub.3,5-F 0 A-4127 H H H H H O 1-CN-cyclopropyl H 2-SCF.sub.3,6-F 0 A-4128 H H H H H O 1-CN-cyclopropyl H 2-SCF.sub.3,5-Me 0 A-4129 H H H H H O 1-CN-cyclopropyl H 2-SCF.sub.3,6-Me 0 A-4130 H H H H H O 1-CN-cyclopropyl H 2-S(?O)CF.sub.3,5-F 0 A-4131 H H H H H O 1-CN-cyclopropyl H 2-S(?O)CF.sub.3,6-F 0 A-4132 H H H H H O 1-CN-cyclopropyl H 2-S(?O)CF.sub.3,5-Me 0 A-4133 H H H H H O 1-CN-cyclopropyl H 2-S(?O)CF.sub.3,6-Me 0 A-4134 H H H H H O 1-CN-cyclopropyl H 2-S(?O).sub.2CF.sub.3,5-F 0 A-4135 H H H H H O 1-CN-cyclopropyl H 2-S(?O).sub.2CF.sub.3,6-F 0 A-4136 H H H H H O 1-CN-cyclopropyl H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-4137 H H H H H O 1-CN-cyclopropyl H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-4138 H H H H H O 1-CN-cyclopropyl H 2-(cyclopropylthio),5-F 0 A-4139 H H H H H O 1-CN-cyclopropyl H 2-(cyclopropylthio),6-F 0 A-4140 H H H H H O 1-CN-cyclopropyl H 2-(cyclopropylthio),5-Me 0 A-4141 H H H H H O 1-CN-cyclopropyl H 2-(cyclopropylthio),6-Me 0 A-4142 H H H H H O 1-CN-cyclopropyl H 2-C(?O)Me,5-F 0 A-4143 H H H H H O 1-CN-cyclopropyl H 2-C(?O)Me,6-F 0 A-4144 H H H H H O 1-CN-cyclopropyl H 2-C(?O)Me,5-Me 0 A-4145 H H H H H O 1-CN-cyclopropyl H 2-C(?O)Me,6-Me 0 A-4146 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2OH,5-F 0 A-4147 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2OH,6-F 0 A-4148 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2OH,5-Me 0 A-4149 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2OH,6-Me 0 A-4150 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2OCH.sub.3,4-F 0 A-4151 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2OCH.sub.3,5-F 0 A-4152 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2OCH.sub.3,6-F 0 A-4153 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2OCH.sub.3,4-Me 0 A-4154 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2OCH.sub.3,5-Me 0 A-4155 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2OCH.sub.3,6-Me 0 A-4156 H H H H H O 1-CN-cyclopropyl H 2-OC(?O)CH.sub.3,5-F 0
(175) TABLE-US-00074 TABLE 74 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4157 H H H H H O 1-CN-cyclopropyl H 2-OC(?O)CH.sub.3,6-F 0 A-4158 H H H H H O 1-CN-cyclopropyl H 2-OC(?O)CH.sub.3,5-Me 0 A-4159 H H H H H O 1-CN-cyclopropyl H 2-OC(?O)CH.sub.3,6-Me 0 A-4160 H H H H H O 1-CN-cyclopropyl H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-4161 H H H H H O 1-CN-cyclopropyl H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-4162 H H H H H O 1-CN-cyclopropyl H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-4163 H H H H H O 1-CN-cyclopropyl H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-4164 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2SCH.sub.3,5-F 0 A-4165 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2SCH.sub.3,6-F 0 A-4166 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2SCH.sub.3,5-Me 0 A-4167 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2SCH.sub.3,6-Me 0 A-4168 H H H H H O 1-CN-cyclopropyl H 2-NMe.sub.2,5-F 0 A-4169 H H H H H O 1-CN-cyclopropyl H 2-NMe.sub.2,6-F 0 A-4170 H H H H H O 1-CN-cyclopropyl H 2-NMe.sub.2,5-Me 0 A-4171 H H H H H O 1-CN-cyclopropyl H 2-NMe.sub.2,6-Me 0 A-4172 H H H H H O 1-CN-cyclopropyl H 2-CN,4-F 0 A-4173 H H H H H O 1-CN-cyclopropyl H 2-CN,5-F 0 A-4174 H H H H H O 1-CN-cyclopropyl H 2-CN,6-F 0 A-4175 H H H H H O 1-CN-cyclopropyl H 2-CN,6-Me 0 A-4176 H H H H H O 1-CN-cyclopropyl H 2-CN,5-OMe 0 A-4177 H H H H H O 1-CN-cyclopropyl H 2-CN,6-OMe 0 A-4178 H H H H H O 1-CN-cyclopropyl H 3-CN,6-Me 0 A-4179 H H H H H O 1-CN-cyclopropyl H 3-CN,6-OMe 0 A-4180 H H H H H O 1-CN-cyclopropyl H 4-CN,2-Me 0 A-4181 H H H H H O 1-CN-cyclopropyl H 4-CN,2-OMe 0 A-4182 H H H H H O 1-CN-cyclopropyl H 2-NO.sub.2,4-F 0 A-4183 H H H H H O 1-CN-cyclopropyl H 2-NO.sub.2,5-F 0 A-4184 H H H H H O 1-CN-cyclopropyl H 2-NO.sub.2,6-F 0 A-4185 H H H H H O 1-CN-cyclopropyl H 2-NO.sub.2,4-Me 0 A-4186 H H H H H O 1-CN-cyclopropyl H 2-NO.sub.2,5-Me 0 A-4187 H H H H H O 1-CN-cyclopropyl H 2-NO.sub.2,6-Me 0 A-4188 H H H H H O 1-CN-cyclopropyl H 2-Me,4,5-F.sub.2 0 A-4189 H H H H H O 1-CN-cyclopropyl H 2-Me,6-Et 0 A-4190 H H H H H O 1-CN-cyclopropyl H 2-cyclopropyl,6-OMe 0 A-4191 H H H H H O 1-CN-cyclopropyl H 2-Me,5-Et 0 A-4192 H H H H H O 1-CN-cyclopropyl H 2,6-Et.sub.2 0 A-4193 H H H H H O 1-CN-cyclopropyl H 2-Et,6-F 0 A-4194 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-4195 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-4196 H H H H H O 1-CN-cyclopropyl H 2-CH.sub.2NMe.sub.2 0 A-4197 H H H H H O CH.sub.2OH H H 0 A-4198 H H H H H O CH.sub.2OH H 2-F 0 A-4199 H H H H H O CH.sub.2OH H 2-Cl 0 A-4200 H H H H H O CH.sub.2OH H 2-Br 0 A-4201 H H H H H O CH.sub.2OH H 2-OH 0 A-4202 H H H H H O CH.sub.2OH H 2-Me 0 A-4203 H H H H H O CH.sub.2OH H 2-Et 0 A-4204 H H H H H O CH.sub.2OH H 2-Pr 0 A-4205 H H H H H O CH.sub.2OH H 2-CF.sub.3 0 A-4206 H H H H H O CH.sub.2OH H 2-CHF.sub.2 0 A-4207 H H H H H O CH.sub.2OH H 2-CH.sub.2F 0 A-4208 H H H H H O CH.sub.2OH H 2-CF.sub.2Cl 0 A-4209 H H H H H O CH.sub.2OH H 2-cyclopropyl 0 A-4210 H H H H H O CH.sub.2OH H 2-cyclobutyl 0 A-4211 H H H H H O CH.sub.2OH H 2-cyclopentyl 0 A-4212 H H H H H O CH.sub.2OH H 2-ethenyl 0 A-4213 H H H H H O CH.sub.2OH H 2-allyl 0
(176) TABLE-US-00075 TABLE 75 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4214 H H H H H O CH.sub.2OH H 2-(prop-1-en-1-yl) 0 A-4215 H H H H H O CH.sub.2OH H 2-(trifluoroephenyl) 0 A-4216 H H H H H O CH.sub.2OH H 2-OMe 0 A-4217 H H H H H O CH.sub.2OH H 2-OEt 0 A-4218 H H H H H O CH.sub.2OH H 2-OPr 0 A-4219 H H H H H O CH.sub.2OH H 2-O(i-Pr) 0 A-4220 H H H H H O CH.sub.2OH H 2-OCF.sub.3 0 A-4221 H H H H H O CH.sub.2OH H 2-OCHF.sub.2 0 A-4222 H H H H H O CH.sub.2OH H 2-(cyclopropyloxy) 0 A-4223 H H H H H O CH.sub.2OH H 2-(cyclobutyloxy) 0 A-4224 H H H H H O CH.sub.2OH H 2-(cyclopentyloxy) 0 A-4225 H H H H H O CH.sub.2OH H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-4226 H H H H H O CH.sub.2OH H 2-(oxiran-2-yl) 0 A-4227 H H H H H O CH.sub.2OH H 2-SMe 0 A-4228 H H H H H O CH.sub.2OH H 3-SMe 0 A-4229 H H H H H O CH.sub.2OH H 2-S(?O)Me 0 A-4230 H H H H H O CH.sub.2OH H 3-S(?O)Me 0 A-4231 H H H H H O CH.sub.2OH H 2-S(?O).sub.2Me 0 A-4232 H H H H H O CH.sub.2OH H 3-S(?O).sub.2Me 0 A-4233 H H H H H O CH.sub.2OH H 2-SCF.sub.3 0 A-4234 H H H H H O CH.sub.2OH H 3-SCF.sub.3 0 A-4235 H H H H H O CH.sub.2OH H 3-S(?O)CF.sub.3 0 A-4236 H H H H H O CH.sub.2OH H 3-SCF(CF.sub.3).sub.2 0 A-4237 H H H H H O CH.sub.2OH H 2-(cyclopropylthio) 0 A-4238 H H H H H O CH.sub.2OH H 2-(cyclopropylsulfinyl) 0 A-4239 H H H H H O CH.sub.2OH H 2-(cyclopropylsulfonyl) 0 A-4240 H H H H H O CH.sub.2OH H 2-C(?O)Me 0 A-4241 H H H H H O CH.sub.2OH H 2-CH.sub.2C(?O)CH.sub.3 0 A-4242 H H H H H O CH.sub.2OH H 2-CH.sub.2C(?O)CF.sub.3 0 A-4243 H H H H H O CH.sub.2OH H 2-CH.sub.2OH 0 A-4244 H H H H H O CH.sub.2OH H 2-CH.sub.2OCH.sub.3 0 A-4245 H H H H H O CH.sub.2OH H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-4246 H H H H H O CH.sub.2OH H 2-CH.sub.2SCH.sub.3 0 A-4247 H H H H H O CH.sub.2OH H 2-CH.sub.2S(?O)CH.sub.3 0 A-4248 H H H H H O CH.sub.2OH H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-4249 H H H H H O CH.sub.2OH H 2-(benzyloxy) 0 A-4250 H H H H H O CH.sub.2OH H 2-NH.sub.2 0 A-4251 H H H H H O CH.sub.2OH H 2-NHMe 0 A-4252 H H H H H O CH.sub.2OH H 2-N(Me).sub.2 0 A-4253 H H H H H O CH.sub.2OH H 2-(1,3-dioxolan-2-yl) 0 A-4254 H H H H H O CH.sub.2OH H 2-(1,3-dioxan-2-yl) 0 A-4255 H H H H H O CH.sub.2OH H 2-(1H-imidazol-2-yl) 0 A-4256 H H H H H O CH.sub.2OH H 2-(thiazol-2-yl) 0 A-4257 H H H H H O CH.sub.2OH H 2-(oxazol-2-yl) 0 A-4258 H H H H H O CH.sub.2OH H 2-CH?NOH 0 A-4259 H H H H H O CH.sub.2OH H 2-CH?NOMe 0 A-4260 H H H H H O CH.sub.2OH H 2-(4,5-dihydro-3-isoxazolyl) 0 A-4261 H H H H H O CH.sub.2OH H 2-CN 0 A-4262 H H H H H O CH.sub.2OH H 2-NO.sub.2 0 A-4263 H H H H H O CH.sub.2OH H 2-F,6-Cl 0 A-4264 H H H H H O CH.sub.2OH H 2-F,6-Me 0 A-4265 H H H H H O CH.sub.2OH H 3-F,6-Me 0 A-4266 H H H H H O CH.sub.2OH H 4-F,2-Me 0 A-4267 H H H H H O CH.sub.2OH H 2-F,6-OMe 0 A-4268 H H H H H O CH.sub.2OH H 3-F,6-OMe 0 A-4269 H H H H H O CH.sub.2OH H 2,6-Cl.sub.2 0 A-4270 H H H H H O CH.sub.2OH H 2-Cl,6-Me 0
(177) TABLE-US-00076 TABLE 76 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4271 H H H H H O CH.sub.2OH H 3-Cl,6-Me 0 A-4272 H H H H H O CH.sub.2OH H 4-Cl,2-Me 0 A-4273 H H H H H O CH.sub.2OH H 2-Cl,5-CF.sub.3 0 A-4274 H H H H H O CH.sub.2OH H 2-Cl,6-CF.sub.3 0 A-4275 H H H H H O CH.sub.2OH H 2-Cl,6-OMe 0 A-4276 H H H H H O CH.sub.2OH H 3-Cl,6-OMe 0 A-4277 H H H H H O CH.sub.2OH H 4-Cl,2-OMe 0 A-4278 H H H H H O CH.sub.2OH H 2,4-Me.sub.2 0 A-4279 H H H H H O CH.sub.2OH H 2,5-Me.sub.2 0 A-4280 H H H H H O CH.sub.2OH H 2,6-Me.sub.2 0 A-4281 H H H H H O CH.sub.2OH H 2-Me,4-CF.sub.3 0 A-4282 H H H H H O CH.sub.2OH H 2-Me,5-CF.sub.3 0 A-4283 H H H H H O CH.sub.2OH H 2-Me,6-CF.sub.3 0 A-4284 H H H H H O CH.sub.2OH H 2-Me,4-OMe 0 A-4285 H H H H H O CH.sub.2OH H 2-Me,5-OMe 0 A-4286 H H H H H O CH.sub.2OH H 2-Me,6-OMe 0 A-4287 H H H H H O CH.sub.2OH H 3-Me,6-OMe 0 A-4288 H H H H H O CH.sub.2OH H 4-Me,2-OMe 0 A-4289 H H H H H O CH.sub.2OH H 2,5-OMe.sub.2 0 A-4290 H H H H H O CH.sub.2OH H 2,6-OMe.sub.2 0 A-4291 H H H H H O CH.sub.2OH H 2-OMe,6-CF.sub.3 0 A-4292 H H H H H O CH.sub.2OH H 2-CHF.sub.2,5-F 0 A-4293 H H H H H O CH.sub.2OH H 2-CHF.sub.2,6-F 0 A-4294 H H H H H O CH.sub.2OH H 2-CHF.sub.2,5-Me 0 A-4295 H H H H H O CH.sub.2OH H 2-CHF.sub.2,6-Me 0 A-4296 H H H H H O CH.sub.2OH H 2-cyclopropyl,5-F 0 A-4297 H H H H H O CH.sub.2OH H 2-cyclopropyl,6-F 0 A-4298 H H H H H O CH.sub.2OH H 2-cyclopropyl,5-Me 0 A-4299 H H H H H O CH.sub.2OH H 2-cyclopropyl,6-Me 0 A-4300 H H H H H O CH.sub.2OH H 2-ethenyl,6-F 0 A-4301 H H H H H O CH.sub.2OH H 2-ethenyl,6-Me 0 A-4302 H H H H H O CH.sub.2OH H 2-OEt,5-F 0 A-4303 H H H H H O CH.sub.2OH H 2-OEt,6-F 0 A-4304 H H H H H O CH.sub.2OH H 2-OEt,5-Cl 0 A-4305 H H H H H O CH.sub.2OH H 2-OEt,6-Cl 0 A-4306 H H H H H O CH.sub.2OH H 2-OEt,5-Me 0 A-4307 H H H H H O CH.sub.2OH H 2-OEt,6-Me 0 A-4308 H H H H H O CH.sub.2OH H 2-OCHF.sub.2,5-F 0 A-4309 H H H H H O CH.sub.2OH H 2-OCHF.sub.2,6-F 0 A-4310 H H H H H O CH.sub.2OH H 2-OCHF.sub.2,5-Me 0 A-4311 H H H H H O CH.sub.2OH H 2-OCHF.sub.2,6-Me 0 A-4312 H H H H H O CH.sub.2OH H 2-(cyclopropyloxy),5-F 0 A-4313 H H H H H O CH.sub.2OH H 2-(cyclopropyloxy),6-F 0 A-4314 H H H H H O CH.sub.2OH H 2-(cyclopropyloxy),5-Me 0 A-4315 H H H H H O CH.sub.2OH H 2-(cyclopropyloxy),6-Me 0 A-4316 H H H H H O CH.sub.2OH H 2-SMe,5-F 0 A-4317 H H H H H O CH.sub.2OH H 2-SMe,6-F 0 A-4318 H H H H H O CH.sub.2OH H 2-SMe,5-Me 0 A-4319 H H H H H O CH.sub.2OH H 2-SMe,6-Me 0 A-4320 H H H H H O CH.sub.2OH H 2-S(?O)Me,5-F 0 A-4321 H H H H H O CH.sub.2OH H 2-S(?O)Me,6-F 0 A-4322 H H H H H O CH.sub.2OH H 2-S(?O)Me,5-Me 0 A-4323 H H H H H O CH.sub.2OH H 2-S(?O)Me,6-Me 0 A-4324 H H H H H O CH.sub.2OH H 2-S(?O).sub.2Me,5-F 0 A-4325 H H H H H O CH.sub.2OH H 2-S(?O).sub.2Me,6-F 0 A-4326 H H H H H O CH.sub.2OH H 2-S(?O).sub.2Me,5-Me 0 A-4327 H H H H H O CH.sub.2OH H 2-S(?O).sub.2Me,6-Me 0
(178) TABLE-US-00077 TABLE 77 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4328 H H H H H O CH.sub.2OH H 2-SCF.sub.3,5-F 0 A-4329 H H H H H O CH.sub.2OH H 2-SCF.sub.3,6-F 0 A-4330 H H H H H O CH.sub.2OH H 2-SCF.sub.3,5-Me 0 A-4331 H H H H H O CH.sub.2OH H 2-SCF.sub.3,6-Me 0 A-4332 H H H H H O CH.sub.2OH H 2-S(?O)CF.sub.3,5-F 0 A-4333 H H H H H O CH.sub.2OH H 2-S(?O)CF.sub.3,6-F 0 A-4334 H H H H H O CH.sub.2OH H 2-S(?O)CF.sub.3,5-Me 0 A-4335 H H H H H O CH.sub.2OH H 2-S(?O)CF.sub.3,6-Me 0 A-4336 H H H H H O CH.sub.2OH H 2-S(?O).sub.2CF.sub.3,5-F 0 A-4337 H H H H H O CH.sub.2OH H 2-S(?O).sub.2CF.sub.3,6-F 0 A-4338 H H H H H O CH.sub.2OH H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-4339 H H H H H O CH.sub.2OH H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-4340 H H H H H O CH.sub.2OH H 2-(cyclopropylthio),5-F 0 A-4341 H H H H H O CH.sub.2OH H 2-(cyclopropylthio),6-F 0 A-4342 H H H H H O CH.sub.2OH H 2-(cyclopropylthio),5-Me 0 A-4343 H H H H H O CH.sub.2OH H 2-(cyclopropylthio),6-Me 0 A-4344 H H H H H O CH.sub.2OH H 2-C(?O)Me,5-F 0 A-4345 H H H H H O CH.sub.2OH H 2-C(?O)Me,6-F 0 A-4346 H H H H H O CH.sub.2OH H 2-C(?O)Me,5-Me 0 A-4347 H H H H H O CH.sub.2OH H 2-C(?O)Me,6-Me 0 A-4348 H H H H H O CH.sub.2OH H 2-CH.sub.2OH,5-F 0 A-4349 H H H H H O CH.sub.2OH H 2-CH.sub.2OH,6-F 0 A-4350 H H H H H O CH.sub.2OH H 2-CH.sub.2OH,5-Me 0 A-4351 H H H H H O CH.sub.2OH H 2-CH.sub.2OH,6-Me 0 A-4352 H H H H H O CH.sub.2OH H 2-CH.sub.2OCH.sub.3,4-F 0 A-4353 H H H H H O CH.sub.2OH H 2-CH.sub.2OCH.sub.3,5-F 0 A-4354 H H H H H O CH.sub.2OH H 2-CH.sub.2OCH.sub.3,6-F 0 A-4355 H H H H H O CH.sub.2OH H 2-CH.sub.2OCH.sub.3,4-Me 0 A-4356 H H H H H O CH.sub.2OH H 2-CH.sub.2OCH.sub.3,5-Me 0 A-4357 H H H H H O CH.sub.2OH H 2-CH.sub.2OCH.sub.3,6-Me 0 A-4358 H H H H H O CH.sub.2OH H 2-OC(?O)CH.sub.3,5-F 0 A-4359 H H H H H O CH.sub.2OH H 2-OC(?O)CH.sub.3,6-F 0 A-4360 H H H H H O CH.sub.2OH H 2-OC(?O)CH.sub.3,5-Me 0 A-4361 H H H H H O CH.sub.2OH H 2-OC(?O)CH.sub.3,6-Me 0 A-4362 H H H H H O CH.sub.2OH H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-4363 H H H H H O CH.sub.2OH H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-4364 H H H H H O CH.sub.2OH H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-4365 H H H H H O CH.sub.2OH H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-4366 H H H H H O CH.sub.2OH H 2-CH.sub.2SCH.sub.3,5-F 0 A-4367 H H H H H O CH.sub.2OH H 2-CH.sub.2SCH.sub.3,6-F 0 A-4368 H H H H H O CH.sub.2OH H 2-CH2SCH.sub.3,5-Me 0 A-4369 H H H H H O CH.sub.2OH H 2-CH.sub.2SCH.sub.3,6-Me 0 A-4370 H H H H H O CH.sub.2OH H 2-NMe.sub.2,5-F 0 A-4371 H H H H H O CH.sub.2OH H 2-NMe.sub.2,6-F 0 A-4372 H H H H H O CH.sub.2OH H 2-NMe.sub.2,5-Me 0 A-4373 H H H H H O CH.sub.2OH H 2-NMe.sub.2,6-Me 0 A-4374 H H H H H O CH.sub.2OH H 2-CN,4-F 0 A-4375 H H H H H O CH.sub.2OH H 2-CN,5-F 0 A-4376 H H H H H O CH.sub.2OH H 2-CN,6-F 0 A-4377 H H H H H O CH.sub.2OH H 2-CN,6-Me 0 A-4378 H H H H H O CH.sub.2OH H 2-CN,5-OMe 0 A-4379 H H H H H O CH.sub.2OH H 2-CN,6-OMe 0 A-4380 H H H H H O CH.sub.2OH H 3-CN,6-Me 0 A-4381 H H H H H O CH.sub.2OH H 3-CN,6-OMe 0 A-4382 H H H H H O CH.sub.2OH H 4-CN,2-Me 0 A-4383 H H H H H O CH.sub.2OH H 4-CN,2-OMe 0 A-4384 H H H H H O CH.sub.2OH H 2-NO.sub.2,4-F 0
(179) TABLE-US-00078 TABLE 78 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4385 H H H H H O CH.sub.2OH H 2-NO.sub.2,5-F 0 A-4386 H H H H H O CH.sub.2OH H 2-NO.sub.2,6-F 0 A-4387 H H H H H O CH.sub.2OH H 2-NO.sub.2,4-Me 0 A-4388 H H H H H O CH.sub.2OH H 2-NO.sub.2,5-Me 0 A-4389 H H H H H O CH.sub.2OH H 2-NO.sub.2,6-Me 0 A-4390 H H H H H O CH.sub.2OH H 2-Me,4,5-F2 0 A-4391 H H H H H O CH.sub.2OH H 2-Me,6-Et 0 A-4392 H H H H H O CH.sub.2OH H 2-cyclopropyl,6-OMe 0 A-4393 H H H H H O CH.sub.2OH H 2-Me,5-Et 0 A-4394 H H H H H O CH.sub.2OH H 2,6-Et.sub.2 0 A-4395 H H H H H O CH.sub.2OH H 2-Et,6-F 0 A-4396 H H H H H O CH.sub.2OH H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-4397 H H H H H O CH.sub.2OH H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-4398 H H H H H O CH.sub.2OH H 2-CH.sub.2NMe.sub.2 0 A-4399 H H H H H O NH.sub.2 H H 0 A-4400 H H H H H O NH.sub.2 H 2-F 0 A-4401 H H H H H O NH.sub.2 H 2-Cl 0 A-4402 H H H H H O NH.sub.2 H 2-Br 0 A-4403 H H H H H O NH.sub.2 H 2-OH 0 A-4404 H H H H H O NH.sub.2 H 2-Me 0 A-4405 H H H H H O NH.sub.2 H 2-Et 0 A-4406 H H H H H O NH.sub.2 H 2-Pr 0 A-4407 H H H H H O NH.sub.2 H 2-CF.sub.3 0 A-4408 H H H H H O NH.sub.2 H 2-CHF.sub.2 0 A-4409 H H H H H O NH.sub.2 H 2-CH.sub.2F 0 A-4410 H H H H H O NH.sub.2 H 2-CF.sub.2Cl 0 A-4411 H H H H H O NH.sub.2 H 2-cyclopropyl 0 A-4412 H H H H H O NH.sub.2 H 2-cyclobutyl 0 A-4413 H H H H H O NH.sub.2 H 2-cyclopentyl 0 A-4414 H H H H H O NH.sub.2 H 2-ethenyl 0 A-4415 H H H H H O NH.sub.2 H 2-allyl 0 A-4416 H H H H H O NH.sub.2 H 2-(prop-1-en-1-yl) 0 A-4417 H H H H H O NH.sub.2 H 2-(trifluoroethenyl) 0 A-4418 H H H H H O NH.sub.2 H 2-OMe 0 A-4419 H H H H H O NH.sub.2 H 2-OEt 0 A-4420 H H H H H O NH.sub.2 H 2-OPr 0 A-4421 H H H H H O NH.sub.2 H 2-O(i-Pr) 0 A-4422 H H H H H O NH.sub.2 H 2-OCF.sub.3 0 A-4423 H H H H H O NH.sub.2 H 2-OCHF.sub.2 0 A-4424 H H H H H O NH.sub.2 H 2-(cyclopropyloxyl) 0 A-4425 H H H H H O NH.sub.2 H 2-(cycbbutyloxyl) 0 A-4426 H H H H H O NH.sub.2 H 2-(cyclopentyloxyl) 0 A-4427 H H H H H O NH.sub.2 H 2-((2,2-dichborocyclopropyl)oxy) 0 A-4428 H H H H H O NH.sub.2 H 2-(oxiran-2-yl) 0 A-4429 H H H H H O NH.sub.2 H 2-SMe 0 A-4430 H H H H H O NH.sub.2 H 3-SMe 0 A-4431 H H H H H O NH.sub.2 H 2-S(?O)Me 0 A-4432 H H H H H O NH.sub.2 H 3-S(?O)Me 0 A-4433 H H H H H O NH.sub.2 H 2-S(?O).sub.2Me 0 A-4434 H H H H H O NH.sub.2 H 3-S(?O).sub.2Me 0 A-4435 H H H H H O NH.sub.2 H 2-SCF.sub.3 0 A-4436 H H H H H O NH.sub.2 H 3-SCF.sub.3 0 A-4437 H H H H H O NH.sub.2 H 3-S(?O)CF.sub.3 0 A-4438 H H H H H O NH.sub.2 H 3-SCF(CF.sub.3).sub.2 0 A-4439 H H H H H O NH.sub.2 H 2-(cyclopropylthio) 0 A-4440 H H H H H O NH.sub.2 H 2-(cyclopropylsulfinyl) 0 A-4441 H H H H H O NH.sub.2 H 2-(cyclopropylsulfonyl) 0
(180) TABLE-US-00079 TABLE 79 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4442 H H H H H O NH.sub.2 H 2-C(?O)Me 0 A-4443 H H H H H O NH.sub.2 H 2-CH.sub.2C(?O)CH.sub.3 0 A-4444 H H H H H O NH.sub.2 H 2-CH.sub.2C(?O)CF.sub.3 0 A-4445 H H H H H O NH.sub.2 H 2-CH.sub.2OH 0 A-4446 H H H H H O NH.sub.2 H 2-CH.sub.2OCH.sub.3 0 A-4447 H H H H H O NH.sub.2 H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-4448 H H H H H O NH.sub.2 H 2-CH.sub.2SCH.sub.3 0 A-4449 H H H H H O NH.sub.2 H 2-CH.sub.2S(?O)CH.sub.3 0 A-4450 H H H H H O NH.sub.2 H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-4451 H H H H H O NH.sub.2 H 2-(benzyloxy) 0 A-4452 H H H H H O NH.sub.2 H 2-NH.sub.2 0 A-4453 H H H H H O NH.sub.2 H 2-NHMe 0 A-4454 H H H H H O NH.sub.2 H 2-N(Me).sub.2 0 A-4455 H H H H H O NH.sub.2 H 2-(1,3-dioxolan-2-yl) 0 A-4456 H H H H H O NH.sub.2 H 2-(1,3-dioxan-2-yl) 0 A-4457 H H H H H O NH.sub.2 H 2-(1H-imidazol-2-yl) 0 A-4458 H H H H H O NH.sub.2 H 2-(thiazol-2-yl) 0 A-4459 H H H H H O NH.sub.2 H 2-(oxazol-2-yl) 0 A-4460 H H H H H O NH.sub.2 H 2-CH?NOH 0 A-4461 H H H H H O NH.sub.2 H 2-CH?NOMe 0 A-4462 H H H H H O NH.sub.2 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-4463 H H H H H O NH.sub.2 H 2-CN 0 A-4464 H H H H H O NH.sub.2 H 2-NO.sub.2 0 A-4465 H H H H H O NH.sub.2 H 2-F,6-Cl 0 A-4466 H H H H H O NH.sub.2 H 2-F,6-Me 0 A-4467 H H H H H O NH.sub.2 H 3-F,6-Me 0 A-4468 H H H H H O NH.sub.2 H 4-F,2-Me 0 A-4469 H H H H H O NH.sub.2 H 2-F,6-OMe 0 A-4470 H H H H H O NH.sub.2 H 3-F,6-OMe 0 A-4471 H H H H H O NH.sub.2 H 2,6-Cl.sub.2 0 A-4472 H H H H H O NH.sub.2 H 2-Cl,6-Me 0 A-4473 H H H H H O NH.sub.2 H 3-Cl,6-Me 0 A-4474 H H H H H O NH.sub.2 H 4-Cl,2-Me 0 A-4475 H H H H H O NH.sub.2 H 2-Cl,5-CF.sub.3 0 A-4476 H H H H H O NH.sub.2 H 2-Cl,6-CF.sub.3 0 A-4477 H H H H H O NH.sub.2 H 2-Cl,6-OMe 0 A-4478 H H H H H O NH.sub.2 H 3-Cl,6-OMe 0 A-4479 H H H H H O NH.sub.2 H 4-Cl,2-OMe 0 A-4480 H H H H H O NH.sub.2 H 2,4-Me.sub.2 0 A-4481 H H H H H O NH.sub.2 H 2,5-Me.sub.2 0 A-4482 H H H H H O NH.sub.2 H 2,6-Me.sub.2 0 A-4483 H H H H H O NH.sub.2 H 2-Me,4-CF.sub.3 0 A-4484 H H H H H O NH.sub.2 H 2-Me,5-CF.sub.3 0 A-4485 H H H H H O NH.sub.2 H 2-Me,6-CF.sub.3 0 A-4486 H H H H H O NH.sub.2 H 2-Me,4-OMe 0 A-4487 H H H H H O NH.sub.2 H 2-Me,5-OMe 0 A-4488 H H H H H O NH.sub.2 H 2-Me,6-OMe 0 A-4489 H H H H H O NH.sub.2 H 3-Me,6-OMe 0 A-4490 H H H H H O NH.sub.2 H 4-Me,2-OMe 0 A-4491 H H H H H O NH.sub.2 H 2,5-OMe.sub.2 0 A-4492 H H H H H O NH.sub.2 H 2,6-OMe.sub.2 0 A-4493 H H H H H O NH.sub.2 H 2-OMe,6-CF.sub.3 0 A-4494 H H H H H O NH.sub.2 H 2-CHF.sub.2,5-F 0 A-4495 H H H H H O NH.sub.2 H 2-CHF.sub.2,6-F 0 A-4496 H H H H H O NH.sub.2 H 2-CHF.sub.2,5-Me 0 A-4497 H H H H H O NH.sub.2 H 2-CHF.sub.2,6-Me 0 A-4498 H H H H H O NH.sub.2 H 2-cyclopropyl,5-F 0
(181) TABLE-US-00080 TABLE 80 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4499 H H H H H O NH.sub.2 H 2-cyclopropyl,6-F 0 A-4500 H H H H H O NH.sub.2 H 2-cyclopropyl,5-Me 0 A-4501 H H H H H O NH.sub.2 H 2-cyclopropyl,6-Me 0 A-4502 H H H H H O NH.sub.2 H 2-ethenyl,6-F 0 A-4503 H H H H H O NH.sub.2 H 2-ethenyl,6-Me 0 A-4504 H H H H H O NH.sub.2 H 2-OEt,5-F 0 A-4505 H H H H H O NH.sub.2 H 2-OEt,6-F 0 A-4506 H H H H H O NH.sub.2 H 2-OEt,5-Cl 0 A-4507 H H H H H O NH.sub.2 H 2-OEt,6-Cl 0 A-4508 H H H H H O NH.sub.2 H 2-OEt,5-Me 0 A-4509 H H H H H O NH.sub.2 H 2-OEt,6-Me 0 A-4510 H H H H H O NH.sub.2 H 2-OCHF.sub.2,5-F 0 A-4511 H H H H H O NH.sub.2 H 2-OCHF.sub.2,6-F 0 A-4512 H H H H H O NH.sub.2 H 2-OCHF.sub.2,5-Me 0 A-4513 H H H H H O NH.sub.2 H 2-OCHF.sub.2,6-Me 0 A-4514 H H H H H O NH.sub.2 H 2-(cyclopropyloxy),5-F 0 A-4515 H H H H H O NH.sub.2 H 2-(cyclopropyloxy),6-F 0 A-4516 H H H H H O NH.sub.2 H 2-(cyclopropyloxy),5-Me 0 A-4517 H H H H H O NH.sub.2 H 2-(cyclopropyloxy),6-Me 0 A-4518 H H H H H O NH.sub.2 H 2-SMe,5-F 0 A-4519 H H H H H O NH.sub.2 H 2-SMe,6-F 0 A-4520 H H H H H O NH.sub.2 H 2-SMe,5-Me 0 A-4521 H H H H H O NH.sub.2 H 2-SMe,6-Me 0 A-4522 H H H H H O NH.sub.2 H 2-S(?O)Me,5-F 0 A-4523 H H H H H O NH.sub.2 H 2-S(?O)Me,6-F 0 A-4524 H H H H H O NH.sub.2 H 2-S(?O)Me,5-Me 0 A-4525 H H H H H O NH.sub.2 H 2-S(?O)Me,6-Me 0 A-4526 H H H H H O NH.sub.2 H 2-S(?O).sub.2Me,5-F 0 A-4527 H H H H H O NH.sub.2 H 2-S(?O).sub.2Me,6-F 0 A-4528 H H H H H O NH.sub.2 H 2-S(?O).sub.2Me,5-Me 0 A-4529 H H H H H O NH.sub.2 H 2-S(?O).sub.2Me,6-Me 0 A-4530 H H H H H O NH.sub.2 H 2-SCF.sub.3,5-F 0 A-4531 H H H H H O NH.sub.2 H 2-SCF.sub.3,6-F 0 A-4532 H H H H H O NH.sub.2 H 2-SCF.sub.3,5-Me 0 A-4533 H H H H H O NH.sub.2 H 2-SCF.sub.3,6-Me 0 A-4534 H H H H H O NH.sub.2 H 2-S(?O)CF.sub.3,5-F 0 A-4535 H H H H H O NH.sub.2 H 2-S(?O)CF.sub.3,6-F 0 A-4536 H H H H H O NH.sub.2 H 2-S(?O)CF.sub.3,5-Me 0 A-4537 H H H H H O NH.sub.2 H 2-S(?O)CF.sub.3,6-Me 0 A-4538 H H H H H O NH.sub.2 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-4539 H H H H H O NH.sub.2 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-4540 H H H H H O NH.sub.2 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-4541 H H H H H O NH.sub.2 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-4542 H H H H H O NH.sub.2 H 2-(cyclopropylthio),5-F 0 A-4543 H H H H H O NH.sub.2 H 2-(cyclopropylthio),6-F 0 A-4544 H H H H H O NH.sub.2 H 2-(cyclopropylthio),5-Me 0 A-4545 H H H H H O NH.sub.2 H 2-(cyclopropylthio),6-Me 0 A-4546 H H H H H O NH.sub.2 H 2-C(?O)Me,5-F 0 A-4547 H H H H H O NH.sub.2 H 2-C(?O)Me,6-F 0 A-4548 H H H H H O NH.sub.2 H 2-C(?O)Me,5-Me 0 A-4549 H H H H H O NH.sub.2 H 2-C(?O)Me,6-Me 0 A-4550 H H H H H O NH.sub.2 H 2-CH.sub.2OH,5-F 0 A-4551 H H H H H O NH.sub.2 H 2-CH.sub.2OH,6-F 0 A-4552 H H H H H O NH.sub.2 H 2-CH.sub.2OH,5-Me 0 A-4553 H H H H H O NH.sub.2 H 2-CH.sub.2OH,6-Me 0 A-4554 H H H H H O NH.sub.2 H 2-CH.sub.2OCH.sub.3,4-F 0 A-4555 H H H H H O NH.sub.2 H 2-CH.sub.2OCH.sub.3,5-F 0
(182) TABLE-US-00081 TABLE 81 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4556 H H H H H O NH.sub.2 H 2-CH.sub.2OCH.sub.3,6-F 0 A-4557 H H H H H O NH.sub.2 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-4558 H H H H H O NH.sub.2 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-4559 H H H H H O NH.sub.2 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-4560 H H H H H O NH.sub.2 H 2-OC(?O)CH.sub.3,5-F 0 A-4561 H H H H H O NH.sub.2 H 2-OC(?O)CH.sub.3,6-F 0 A-4562 H H H H H O NH.sub.2 H 2-OC(?O)CH.sub.3,5-Me 0 A-4563 H H H H H O NH.sub.2 H 2-OC(?O)CH.sub.3,6-Me 0 A-4564 H H H H H O NH.sub.2 H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-4565 H H H H H O NH.sub.2 H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-4566 H H H H H O NH.sub.2 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-4567 H H H H H O NH.sub.2 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-4568 H H H H H O NH.sub.2 H 2-CH.sub.2SCH.sub.3,5-F 0 A-4569 H H H H H O NH.sub.2 H 2-CH.sub.2SCH.sub.3,6-F 0 A-4570 H H H H H O NH.sub.2 H 2-CH.sub.2SCH.sub.3,5-Me 0 A-4571 H H H H H O NH.sub.2 H 2-CH.sub.2SCH.sub.3,6-Me 0 A-4572 H H H H H O NH.sub.2 H 2-NMe.sub.2,5-F 0 A-4573 H H H H H O NH.sub.2 H 2-NMe.sub.2,6-F 0 A-4574 H H H H H O NH.sub.2 H 2-NMe.sub.2,5-Me 0 A-4575 H H H H H O NH.sub.2 H 2-NMe.sub.2,6-Me 0 A-4576 H H H H H O NH.sub.2 H 2-CN,4-F 0 A-4577 H H H H H O NH.sub.2 H 2-CN,5-F 0 A-4578 H H H H H O NH.sub.2 H 2-CN,6-F 0 A-4579 H H H H H O NH.sub.2 H 2-CN,6-Me 0 A-4580 H H H H H O NH.sub.2 H 2-CN,5-OMe 0 A-4581 H H H H H O NH.sub.2 H 2-CN,6-OMe 0 A-4582 H H H H H O NH.sub.2 H 3-CN,6-Me 0 A-4583 H H H H H O NH.sub.2 H 3-CN,6-OMe 0 A-4584 H H H H H O NH.sub.2 H 4-CN,2-Me 0 A-4585 H H H H H O NH.sub.2 H 4-CN,2-OMe 0 A-4586 H H H H H O NH.sub.2 H 2-NO.sub.2,4-F 0 A-4587 H H H H H O NH.sub.2 H 2-NO.sub.2,5-F 0 A-4588 H H H H H O NH.sub.2 H 2-NO.sub.2,6-F 0 A-4589 H H H H H O NH.sub.2 H 2-NO.sub.2,4-Me 0 A-4590 H H H H H O NH.sub.2 H 2-NO.sub.2,5-Me 0 A-4591 H H H H H O NH.sub.2 H 2-NO.sub.2,6-Me 0 A-4592 H H H H H O NH.sub.2 H 2-Me,4,5-F.sub.2 0 A-4593 H H H H H O NH.sub.2 H 2-Me,6-Et 0 A-4594 H H H H H O NH.sub.2 H 2-cyclopropyl,6-OMe 0 A-4595 H H H H H O NH.sub.2 H 2-Me,5-Et 0 A-4596 H H H H H O NH.sub.2 H 2,6-Et.sub.2 0 A-4597 H H H H H O NH.sub.2 H 2-Et,6-F 0 A-4598 H H H H H O NH.sub.2 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-4599 H H H H H O NH.sub.2 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-4600 H H H H H O NH.sub.2 H 2-CH.sub.2NMe.sub.2 0 A-4601 H H H H H O C(?O)CH.sub.3 H H 0 A-4602 H H H H H O C(?O)CH.sub.3 H 2-F 0 A-4603 H H H H H O C(?O)CH.sub.3 H 2-Cl 0 A-4604 H H H H H O C(?O)CH.sub.3 H 2-Br 0 A-4605 H H H H H O C(?O)CH.sub.3 H 2-OH 0 A-4606 H H H H H O C(?O)CH.sub.3 H 2-Me 0 A-4607 H H H H H O C(?O)CH.sub.3 H 2-Et 0 A-4608 H H H H H O C(?O)CH.sub.3 H 2-Pr 0 A-4609 H H H H H O C(?O)CH.sub.3 H 2-CF.sub.3 0 A-4610 H H H H H O C(?O)CH.sub.3 H 2-CHF.sub.2 0 A-4611 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2F 0 A-4612 H H H H H O C(?O)CH.sub.3 H 2-CF.sub.2Cl 0
(183) TABLE-US-00082 TABLE 82 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4613 H H H H H O C(?O)CH.sub.3 H 2-cyclopropyl 0 A-4614 H H H H H O C(?O)CH.sub.3 H 2-cyclobutyl 0 A-4615 H H H H H O C(?O)CH.sub.3 H 2-cyclopentyl 0 A-4616 H H H H H O C(?O)CH.sub.3 H 2-ethenyl 0 A-4617 H H H H H O C(?O)CH.sub.3 H 2-allyl 0 A-4618 H H H H H O C(?O)CH.sub.3 H 2-(prop-1-en-1-yl) 0 A-4619 H H H H H O C(?O)CH.sub.3 H 2-(trifluoroethenyl) 0 A-4620 H H H H H O C(?O)CH.sub.3 H 2-OMe 0 A-4621 H H H H H O C(?O)CH.sub.3 H 2-OEt 0 A-4622 H H H H H O C(?O)CH.sub.3 H 2-OPr 0 A-4623 H H H H H O C(?O)CH.sub.3 H 2-O(i-Pr) 0 A-4624 H H H H H O C(?O)CH.sub.3 H 2-OCF.sub.3 0 A-4625 H H H H H O C(?O)CH.sub.3 H 2-OCHF.sub.2 0 A-4626 H H H H H O C(?O)CH.sub.3 H 2-(cyclopropyloxy) 0 A-4627 H H H H H O C(?O)CH.sub.3 H 2-(cyclobutyloxy) 0 A-4628 H H H H H O C(?O)CH.sub.3 H 2-(cyclopentyloxy) 0 A-4629 H H H H H O C(?O)CH.sub.3 H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-4630 H H H H H O C(?O)CH.sub.3 H 2-(oxiran-2-yl) 0 A-4631 H H H H H O C(?O)CH.sub.3 H 2-SMe 0 A-4632 H H H H H O C(?O)CH.sub.3 H 3-SMe 0 A-4633 H H H H H O C(?O)CH.sub.3 H 2-S(?O)Me 0 A-4634 H H H H H O C(?O)CH.sub.3 H 3-S(?O)Me 0 A-4635 H H H H H O C(?O)CH.sub.3 H 2-S(?O).sub.2Me 0 A-4636 H H H H H O C(?O)CH.sub.3 H 3-S(?O).sub.2Me 0 A-4637 H H H H H O C(?O)CH.sub.3 H 2-SCF.sub.3 0 A-4638 H H H H H O C(?O)CH.sub.3 H 3-SCF.sub.3 0 A-4639 H H H H H O C(?O)CH.sub.3 H 3-S(?O)CF.sub.3 0 A-4640 H H H H H O C(?O)CH.sub.3 H 3-SCF(CF.sub.3).sub.2 0 A-4641 H H H H H O C(?O)CH.sub.3 H 2-(cyclopropylthio) 0 A-4642 H H H H H O C(?O)CH.sub.3 H 2-(cyclopropylsulfinyl) 0 A-4643 H H H H H O C(?O)CH.sub.3 H 2-(cyclopropylsulfonyl) 0 A-4644 H H H H H O C(?O)CH.sub.3 H 2-C(?O)Me 0 A-4645 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2C(?O)CH.sub.3 0 A-4646 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2C(?O)CF.sub.3 0 A-4647 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2OH 0 A-4648 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2OCH.sub.3 0 A-4649 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-4650 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2SCH.sub.3 0 A-4651 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2S(?O)CH.sub.3 0 A-4652 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-4653 H H H H H O C(?O)CH.sub.3 H 2-(benzyloxy) 0 A-4654 H H H H H O C(?O)CH.sub.3 H 2-NH.sub.2 0 A-4655 H H H H H O C(?O)CH.sub.3 H 2-NHMe 0 A-4656 H H H H H O C(?O)CH.sub.3 H 2-N(Me).sub.2 0 A-4657 H H H H H O C(?O)CH.sub.3 H 2-(1,3-dioxolan-2-yl) 0 A-4658 H H H H H O C(?O)CH.sub.3 H 2-(1,3-dioxan-2-yl) 0 A-4659 H H H H H O C(?O)CH.sub.3 H 2-(1H-imidazol-2-yl) 0 A-4660 H H H H H O C(?O)CH.sub.3 H 2-(thiazol-2-yl) 0 A-4661 H H H H H O C(?O)CH.sub.3 H 2-(oxazol-2-yl) 0 A-4662 H H H H H O C(?O)CH.sub.3 H 2-CH?NOH 0 A-4663 H H H H H O C(?O)CH.sub.3 H 2-CH?NOMe 0 A-4664 H H H H H O C(?O)CH.sub.3 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-4665 H H H H H O C(?O)CH.sub.3 H 2-CN 0 A-4666 H H H H H O C(?O)CH.sub.3 H 2-NO.sub.2 0 A-4667 H H H H H O C(?O)CH.sub.3 H 2-F,6-Cl 0 A-4668 H H H H H O C(?O)CH.sub.3 H 2-F,6-Me 0 A-4669 H H H H H O C(?O)CH.sub.3 H 3-F,6-Me 0
(184) TABLE-US-00083 TABLE 83 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4670 H H H H H O C(?O)CH.sub.3 H 4-F,2-Me 0 A-4671 H H H H H O C(?O)CH.sub.3 H 2-F,6-OMe 0 A-4672 H H H H H O C(?O)CH.sub.3 H 3-F,6-OMe 0 A-4673 H H H H H O C(?O)CH.sub.3 H 2,6-Cl.sub.2 0 A-4674 H H H H H O C(?O)CH.sub.3 H 2-Cl,6-Me 0 A-4675 H H H H H O C(?O)CH.sub.3 H 3-Cl,6-Me 0 A-4676 H H H H H O C(?O)CH.sub.3 H 4-Cl,2-Me 0 A-4677 H H H H H O C(?O)CH.sub.3 H 2-Cl,5-CF.sub.3 0 A-4678 H H H H H O C(?O)CH.sub.3 H 2-Cl,6-CF.sub.3 0 A-4679 H H H H H O C(?O)CH.sub.3 H 2-Cl,6-OMe 0 A-4680 H H H H H O C(?O)CH.sub.3 H 3-Cl,6-OMe 0 A-4681 H H H H H O C(?O)CH.sub.3 H 4-Cl,2-OMe 0 A-4682 H H H H H O C(?O)CH.sub.3 H 2,4-Me.sub.2 0 A-4683 H H H H H O C(?O)CH.sub.3 H 2,5-Me.sub.2 0 A-4684 H H H H H O C(?O)CH.sub.3 H 2,6-Me.sub.2 0 A-4685 H H H H H O C(?O)CH.sub.3 H 2-Me,4-CF.sub.3 0 A-4686 H H H H H O C(?O)CH.sub.3 H 2-Me,5-CF.sub.3 0 A-4687 H H H H H O C(?O)CH.sub.3 H 2-Me,6-CF.sub.3 0 A-4688 H H H H H O C(?O)CH.sub.3 H 2-Me,4-OMe 0 A-4689 H H H H H O C(?O)CH.sub.3 H 2-Me,5-OMe 0 A-4690 H H H H H O C(?O)CH.sub.3 H 2-Me,6-OMe 0 A-4691 H H H H H O C(?O)CH.sub.3 H 3-Me,6-OMe 0 A-4692 H H H H H O C(?O)CH.sub.3 H 4-Me,2-OMe 0 A-4693 H H H H H O C(?O)CH.sub.3 H 2,5-OMe.sub.2 0 A-4694 H H H H H O C(?O)CH.sub.3 H 2,6-OMe.sub.2 0 A-4695 H H H H H O C(?O)CH.sub.3 H 2-OMe,6-CF.sub.3 0 A-4696 H H H H H O C(?O)CH.sub.3 H 2-CHF.sub.2,5-F 0 A-4697 H H H H H O C(?O)CH.sub.3 H 2-CHF.sub.2,6-F 0 A-4698 H H H H H O C(?O)CH.sub.3 H 2-CHF.sub.2,5-Me 0 A-4699 H H H H H O C(?O)CH.sub.3 H 2-CHF.sub.2,6-Me 0 A-4700 H H H H H O C(?O)CH.sub.3 H 2-cyclopropyl,5-F 0 A-4701 H H H H H O C(?O)CH.sub.3 H 2-cyclopropyl,6-F 0 A-4702 H H H H H O C(?O)CH.sub.3 H 2-cyclopropyl,5-Me 0 A-4703 H H H H H O C(?O)CH.sub.3 H 2-cyclopropyl,6-Me 0 A-4704 H H H H H O C(?O)CH.sub.3 H 2-ethenyl,6-F 0 A-4705 H H H H H O C(?O)CH.sub.3 H 2-ethenyl,6-Me 0 A-4706 H H H H H O C(?O)CH.sub.3 H 2-OEt,5-F 0 A-4707 H H H H H O C(?O)CH.sub.3 H 2-OEt,6-F 0 A-4708 H H H H H O C(?O)CH.sub.3 H 2-OEt,5-Cl 0 A-4709 H H H H H O C(?O)CH.sub.3 H 2-OEt,6-Cl 0 A-4710 H H H H H O C(?O)CH.sub.3 H 2-OEt,5-Me 0 A-4711 H H H H H O C(?O)CH.sub.3 H 2-OEt,6-Me 0 A-4712 H H H H H O C(?O)CH.sub.3 H 2-OCHF.sub.2,5-F 0 A-4713 H H H H H O C(?O)CH.sub.3 H 2-OCHF.sub.2,6-F 0 A-4714 H H H H H O C(?O)CH.sub.3 H 2-OCHF.sub.2,5-Me 0 A-4715 H H H H H O C(?O)CH.sub.3 H 2-OCHF.sub.2,6-Me 0 A-4716 H H H H H O C(?O)CH.sub.3 H 2-(cyclopropyloxy),5-F 0 A-4717 H H H H H O C(?O)CH.sub.3 H 2-(cyclopropyloxy),6-F 0 A-4718 H H H H H O C(?O)CH.sub.3 H 2-(cyclopropyloxy),5-Me 0 A-4719 H H H H H O C(?O)CH.sub.3 H 2-(cyclopropyloxy),6-Me 0 A-4720 H H H H H O C(?O)CH.sub.3 H 2-SMe,5-F 0 A-4721 H H H H H O C(?O)CH.sub.3 H 2-SMe,6-F 0 A-4722 H H H H H O C(?O)CH.sub.3 H 2-SMe,5-Me 0 A-4723 H H H H H O C(?O)CH.sub.3 H 2-SMe,6-Me 0 A-4724 H H H H H O C(?O)CH.sub.3 H 2-S(?O)Me,5-F 0 A-4725 H H H H H O C(?O)CH.sub.3 H 2-S(?O)Me,6-F 0 A-4726 H H H H H O C(?O)CH.sub.3 H 2-S(?O)Me,5-Me 0
(185) TABLE-US-00084 TABLE 84 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4727 H H H H H O C(?O)CH.sub.3 H 2-S(?O)Me,6-Me 0 A-4728 H H H H H O C(?O)CH.sub.3 H 2-S(?O).sub.2Me,5-F 0 A-4729 H H H H H O C(?O)CH.sub.3 H 2-S(?O).sub.2Me,6-F 0 A-4730 H H H H H O C(?O)CH.sub.3 H 2-S(?O).sub.2Me,5-Me 0 A-4731 H H H H H O C(?O)CH.sub.3 H 2-S(?O).sub.2Me,6-Me 0 A-4732 H H H H H O C(?O)CH.sub.3 H 2-SCF.sub.3,5-F 0 A-4733 H H H H H O C(?O)CH.sub.3 H 2-SCF.sub.3,6-F 0 A-4734 H H H H H O C(?O)CH.sub.3 H 2-SCF.sub.3,5-Me 0 A-4735 H H H H H O C(?O)CH.sub.3 H 2-SCF.sub.3,6-Me 0 A-4736 H H H H H O C(?O)CH.sub.3 H 2-S(?O)CF.sub.3,5-F 0 A-4737 H H H H H O C(?O)CH.sub.3 H 2-S(?O)CF.sub.3,6-F 0 A-4738 H H H H H O C(?O)CH.sub.3 H 2-S(?O)CF.sub.3,5-Me 0 A-4739 H H H H H O C(?O)CH.sub.3 H 2-S(?O)CF.sub.3,6-Me 0 A-4740 H H H H H O C(?O)CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-4741 H H H H H O C(?O)CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-4742 H H H H H O C(?O)CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-4743 H H H H H O C(?O)CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-4744 H H H H H O C(?O)CH.sub.3 H 2-(cyclopropylthio),5-F 0 A-4745 H H H H H O C(?O)CH.sub.3 H 2-(cyclopropylthio),6-F 0 A-4746 H H H H H O C(?O)CH.sub.3 H 2-(cyclopropylthio),5-Me 0 A-4747 H H H H H O C(?O)CH.sub.3 H 2-(cyclopropylthio),6-Me 0 A-4748 H H H H H O C(?O)CH.sub.3 H 2-C(?O)Me,5-F 0 A-4749 H H H H H O C(?O)CH.sub.3 H 2-C(?O)Me,6-F 0 A-4750 H H H H H O C(?O)CH.sub.3 H 2-C(?O)Me,5-Me 0 A-4751 H H H H H O C(?O)CH.sub.3 H 2-C(?O)Me,6-Me 0 A-4752 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2OH,5-F 0 A-4753 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2OH,6-F 0 A-4754 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2OH,5-Me 0 A-4755 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2OH,6-Me 0 A-4756 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-F 0 A-4757 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-F 0 A-4758 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-F 0 A-4759 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-4760 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-4761 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-4762 H H H H H O C(?O)CH.sub.3 H 2-OC(?O)CH.sub.3,5-F 0 A-4763 H H H H H O C(?O)CH.sub.3 H 2-OC(?O)CH.sub.3,6-F 0 A-4764 H H H H H O C(?O)CH.sub.3 H 2-OC(?O)CH.sub.3,5-Me 0 A-4765 H H H H H O C(?O)CH.sub.3 H 2-OC(?O)CH.sub.3,6-Me 0 A-4766 H H H H H O C(?O)CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-4767 H H H H H O C(?O)CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-4768 H H H H H O C(?O)CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-4769 H H H H H O C(?O)CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-4770 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-F 0 A-4771 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2SCH.sub.3,6-F 0 A-4772 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-Me 0 A-4773 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2SCH.sub.3,6-Me 0 A-4774 H H H H H O C(?O)CH.sub.3 H 2-NMe.sub.2,5-F 0 A-4775 H H H H H O C(?O)CH.sub.3 H 2-NMe.sub.2,6-F 0 A-4776 H H H H H O C(?O)CH.sub.3 H 2-NMe.sub.2,5-Me 0 A-4777 H H H H H O C(?O)CH.sub.3 H 2-NMe.sub.2,6-Me 0 A-4778 H H H H H O C(?O)CH.sub.3 H 2-CN,4-F 0 A-4779 H H H H H O C(?O)CH.sub.3 H 2-CN,5-F 0 A-4780 H H H H H O C(?O)CH.sub.3 H 2-CN,6-F 0 A-4781 H H H H H O C(?O)CH.sub.3 H 2-CN,6-Me 0 A-4782 H H H H H O C(?O)CH.sub.3 H 2-CN,5-OMe 0 A-4783 H H H H H O C(?O)CH.sub.3 H 2-CN,6-OMe 0
(186) TABLE-US-00085 TABLE 85 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4784 H H H H H O C(?O)CH.sub.3 H 3-CN,6-Me 0 A-4785 H H H H H O C(?O)CH.sub.3 H 3-CN,6-OMe 0 A-4786 H H H H H O C(?O)CH.sub.3 H 4-CN,2-Me 0 A-4787 H H H H H O C(?O)CH.sub.3 H 4-CN,2-OMe 0 A-4788 H H H H H O C(?O)CH.sub.3 H 2-NO.sub.2,4-F 0 A-4789 H H H H H O C(?O)CH.sub.3 H 2-NO.sub.2,5-F 0 A-4790 H H H H H O C(?O)CH.sub.3 H 2-NO.sub.2,6-F 0 A-4791 H H H H H O C(?O)CH.sub.3 H 2-NO.sub.2,4-Me 0 A-4792 H H H H H O C(?O)CH.sub.3 H 2-NO.sub.2,5-Me 0 A-4793 H H H H H O C(?O)CH.sub.3 H 2-NO.sub.2,6-Me 0 A-4794 H H H H H O C(?O)CH.sub.3 H 2-Me,4,5F.sub.2 0 A-4795 H H H H H O C(?O)CH.sub.3 H 2-Me,6-Et 0 A-4796 H H H H H O C(?O)CH.sub.3 H 2-cyclopropyl,6-OMe 0 A-4797 H H H H H O C(?O)CH.sub.3 H 2-Me,5-Et 0 A-4798 H H H H H O C(?O)CH.sub.3 H 2,6-Et2 0 A-4799 H H H H H O C(?O)CH.sub.3 H 2-Et,6-F 0 A-4800 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-4801 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-4802 H H H H H O C(?O)CH.sub.3 H 2-CH.sub.2NMe.sub.2 0 A-4803 H H H H H O C(?O)CH.sub.2OCH.sub.3 H H 0 A-4804 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-F 0 A-4805 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Cl 0 A-4806 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Br 0 A-4807 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OH 0 A-4808 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Me 0 A-4809 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Et 0 A-4810 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Pr 0 A-4811 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CF.sub.3 0 A-4812 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CHF.sub.2 0 A-4813 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2F 0 A-4814 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CF.sub.2Cl 0 A-4815 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-cyclopropyl 0 A-4816 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-cyclobutyl 0 A-4817 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-cyclopentyl 0 A-4818 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-ethenyl 0 A-4819 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-allyl 0 A-4820 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(prop-1-en-1-yl) 0 A-4821 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(trifluoroethenyl) 0 A-4822 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OMe 0 A-4823 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OEt 0 A-4824 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OPr 0 A-4825 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-O(i-Pr) 0 A-4826 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OCF.sub.3 0 A-4827 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OCHF.sub.2 0 A-4828 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(cyclopropyloxy) 0 A-4829 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(cyclobutyloxy) 0 A-4830 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(cyclopentyloxy) 0 A-4831 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-4832 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(oxiran-2-yl) 0 A-4833 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-SMe 0 A-4834 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 3-SMe 0 A-4835 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O)Me 0 A-4836 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 3-S(?O)Me 0 A-4837 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O).sub.2Me 0 A-4838 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 3-S(?O).sub.2Me 0 A-4839 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-SCF.sub.3 0 A-4840 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 3-SCF.sub.3 0
(187) TABLE-US-00086 TABLE 86 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4841 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 3-S(?O)CF.sub.3 0 A-4842 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 3-SCF(CF.sub.3).sub.2 0 A-4843 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(cyclopropylthio) 0 A-4844 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(cyclopropylsulfinyl) 0 A-4845 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(cyclopropylsulfonyl) 0 A-4846 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-C(?O)Me 0 A-4847 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2C(?O)CH.sub.3 0 A-4848 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2C(?O)CF.sub.3 0 A-4849 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2OH 0 A-4850 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2OCH.sub.3 0 A-4851 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-4852 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2SCH.sub.3 0 A-4853 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2S(?O)CH.sub.3 0 A-4854 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-4855 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(benzyloxy) 0 A-4856 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-NH.sub.2 0 A-4857 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-NHMe 0 A-4858 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-N(Me).sub.2 0 A-4859 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(1,3-dioxolan-2-yl) 0 A-4860 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(1,3-dioxan-2-yl) 0 A-4861 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(1H-imidazol-2-yl) 0 A-4862 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(thiazol-2-yl) 0 A-4863 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(oxazol-2-yl) 0 A-4864 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH?NOH 0 A-4865 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH?NOMe 0 A-4866 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-4867 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CN 0 A-4868 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-NO.sub.2 0 A-4869 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2F,6-Cl 0 A-4870 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-F,6-Me 0 A-4871 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 3-F,6-Me 0 A-4872 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 4-F,2-Me 0 A-4873 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-F,6-OMe 0 A-4874 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 3-F,6-OMe 0 A-4875 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2,6-Cl.sub.2 0 A-4876 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Cl,6-Me 0 A-4877 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 3-Cl,6-Me 0 A-4878 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 4-Cl,2-Me 0 A-4879 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Cl,5-CF.sub.3 0 A-4880 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Cl,6-CF.sub.3 0 A-4881 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Cl,6-OMe 0 A-4882 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 3-Cl,6-OMe 0 A-4883 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 4-Cl,2-OMe 0 A-4884 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2,4-Me.sub.2 0 A-4885 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2,5-Me.sub.2 0 A-4886 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2,6-Me.sub.2 0 A-4887 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Me,4-CF.sub.3 0 A-4888 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Me,5-CF.sub.3 0 A-4889 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Me,6-CF.sub.3 0 A-4890 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Me,4-OMe 0 A-4891 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Me,5-OMe 0 A-4892 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Me,6-OMe 0 A-4893 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 3-Me,6-OMe 0 A-4894 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 4-Me,2-OMe 0 A-4895 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2,5-OMe.sub.2 0 A-4896 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2,6-OMe.sub.2 0 A-4897 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OMe,6-CF.sub.3 0
(188) TABLE-US-00087 TABLE 87 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4898 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CHF.sub.2,5-F 0 A-4899 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CHF.sub.2,6-F 0 A-4900 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CHF.sub.2,5-Me 0 A-4901 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CHF.sub.2,6-Me 0 A-4902 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-cyclopropyl,5-F 0 A-4903 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-cyclopropyl,6-F 0 A-4904 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-cyclopropyl,5-Me 0 A-4905 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-cyclopropyl,6-Me 0 A-4906 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-ethenyl,6-F 0 A-4907 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-ethenyl,6-Me 0 A-4908 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OEt,5-F 0 A-4909 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OEt,6-F 0 A-4910 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OEt,5-Cl 0 A-4911 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OEt,6-Cl 0 A-4912 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OEt,5-Me 0 A-4913 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OEt,6-Me 0 A-4914 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OCHF.sub.2,5-F 0 A-4915 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OCHF.sub.2,6-F 0 A-4916 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OCHF.sub.2,5-Me 0 A-4917 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OCHF.sub.2,6-Me 0 A-4918 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(cyclopropyloxy),5-F 0 A-4919 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(cyclopropyloxy),6-F 0 A-4920 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(cyclopropyloxy),5-Me 0 A-4921 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(cyclopropyloxy),6-Me 0 A-4922 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-SMe,5-F 0 A-4923 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-SMe,6-F 0 A-4924 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-SMe,5-Me 0 A-4925 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-SMe,6-Me 0 A-4926 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O)Me,5-F 0 A-4927 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O)Me,6-F 0 A-4928 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O)Me,5-Me 0 A-4929 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O)Me,6-Me 0 A-4930 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O).sub.2Me,5-F 0 A-4931 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O).sub.2Me,6-F 0 A-4932 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O).sub.2Me,5-Me 0 A-4933 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O).sub.2Me,6-Me 0 A-4934 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-SCF.sub.3,5-F 0 A-4935 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-SCF.sub.3,6-F 0 A-4936 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-SCF.sub.3,5-Me 0 A-4937 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-SCF.sub.3,6-Me 0 A-4938 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O)CF.sub.3,5-F 0 A-4939 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O)CF.sub.3,6-F 0 A-4940 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O)CF.sub.3,5-Me 0 A-4941 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O)CF.sub.3,6-Me 0 A-4942 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-4943 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-4944 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-4945 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-4946 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(cyclopropylthio),5-F 0 A-4947 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(cyclopropylthio),6-F 0 A-4948 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(cyclopropylthio),5-Me 0 A-4949 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-(cyclopropylthio),6-Me 0 A-4950 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-C(?O)Me,5-F 0 A-4951 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-C(?O)Me,6-F 0 A-4952 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-C(?O)Me,5-Me 0 A-4953 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-C(?O)Me,6-Me 0 A-4954 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2OH,5-F 0
(189) TABLE-US-00088 TABLE 88 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-4955 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2OH,6-F 0 A-4956 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2OH,5-Me 0 A-4957 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2OH,6-Me 0 A-4958 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2OCH.sub.3,4-F 0 A-4959 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2OCH.sub.3,5-F 0 A-4960 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2OCH.sub.3,6-F 0 A-4961 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-4962 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-4963 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-4964 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OC(?O)CH.sub.3,5-F 0 A-4965 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OC(?O)CH.sub.3,6-F 0 A-4966 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OC(?O)CH.sub.3,5-Me 0 A-4967 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OC(?O)CH.sub.3,6-Me 0 A-4968 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-4969 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-4970 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-4971 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-4972 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2SCH.sub.3,5-F 0 A-4973 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2SCH.sub.3,6-F 0 A-4974 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2SCH.sub.3,5-Me 0 A-4975 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2SCH.sub.3,6-Me 0 A-4976 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-NMe.sub.2,5-F 0 A-4977 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-NMe.sub.2,6-F 0 A-4978 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-NMe.sub.2,5-Me 0 A-4979 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-NMe.sub.2,6-Me 0 A-4980 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CN,4-F 0 A-4981 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CN,5-F 0 A-4982 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CN,6-F 0 A-4983 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CN,6-Me 0 A-4984 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CN,5-OMe 0 A-4985 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CN,6-OMe 0 A-4986 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 3-CN,6-Me 0 A-4987 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 3-CN,6-OMe 0 A-4988 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 4-CN,2-Me 0 A-4989 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 4-CN,2-OMe 0 A-4990 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-NO.sub.2,4-F 0 A-4991 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-NO.sub.2,5-F 0 A-4992 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-NO.sub.2,6-F 0 A-4993 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-NO.sub.2,4-Me 0 A-4994 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-NO.sub.2,5-Me 0 A-4995 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-NO.sub.2,6-Me 0 A-4996 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Me,4,5-F.sub.2 0 A-4997 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Me,6-Et 0 A-4998 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-cyclopropyl,6-OMe 0 A-4999 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Me,5-Et 0 A-5000 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2,6-Et.sub.2 0 A-5001 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-Et,6-F 0 A-5002 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-5003 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-5004 H H H H H O C(?O)CH.sub.2OCH.sub.3 H 2-CH.sub.2NMe.sub.2 0 A-5005 H H H H H O C(?O)cyclopropyl H H 0 A-5006 H H H H H O C(?O)cyclopropyl H 2-F 0 A-5007 H H H H H O C(?O)cyclopropyl H 2-Cl 0 A-5008 H H H H H O C(?O)cyclopropyl H 2-Br 0 A-5009 H H H H H O C(?O)cyclopropyl H 2-OH 0 A-5010 H H H H H O C(?O)cyclopropyl H 2-Me 0 A-5011 H H H H H O C(?O)cyclopropyl H 2-Et 0
(190) TABLE-US-00089 TABLE 89 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5012 H H H H H O C(?O)cyclopropyl H 2-Pr 0 A-5013 H H H H H O C(?O)cyclopropyl H 2-CF.sub.3 0 A-5014 H H H H H O C(?O)cyclopropyl H 2-CHF.sub.2 0 A-5015 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2F 0 A-5016 H H H H H O C(?O)cyclopropyl H 2-CF.sub.2Cl 0 A-5017 H H H H H O C(?O)cyclopropyl H 2-cyclopropyl 0 A-5018 H H H H H O C(?O)cyclopropyl H 2-cyclobutyl 0 A-5019 H H H H H O C(?O)cyclopropyl H 2-cyclopentyl 0 A-5020 H H H H H O C(?O)cyclopropyl H 2-ethenyl 0 A-5021 H H H H H O C(?O)cyclopropyl H 2-allyl 0 A-5022 H H H H H O C(?O)cyclopropyl H 2-(prop-1-en-1-yl) 0 A-5023 H H H H H O C(?O)cyclopropyl H 2-(trifluoroethenyl) 0 A-5024 H H H H H O C(?O)cyclopropyl H 2-OMe 0 A-5025 H H H H H O C(?O)cyclopropyl H 2-OEt 0 A-5026 H H H H H O C(?O)cyclopropyl H 2-OPr 0 A-5027 H H H H H O C(?O)cyclopropyl H 2-O(i-Pr) 0 A-5028 H H H H H O C(?O)cyclopropyl H 2-OCF.sub.3 0 A-5029 H H H H H O C(?O)cyclopropyl H 2-OCHF.sub.2 0 A-5030 H H H H H O C(?O)cyclopropyl H 2-(cyclopropyloxy) 0 A-5031 H H H H H O C(?O)cyclopropyl H 2-(cyclobutyloxy) 0 A-5032 H H H H H O C(?O)cyclopropyl H 2-(cyclopentyloxy) 0 A-5033 H H H H H O C(?O)cyclopropyl H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-5034 H H H H H O C(?O)cyclopropyl H 2-(oxiran-2-yl) 0 A-5035 H H H H H O C(?O)cyclopropyl H 2-SMe 0 A-5036 H H H H H O C(?O)cyclopropyl H 3-SMe 0 A-5037 H H H H H O C(?O)cyclopropyl H 2-S(?O)Me 0 A-5038 H H H H H O C(?O)cyclopropyl H 3-S(?O)Me 0 A-5039 H H H H H O C(?O)cyclopropyl H 2-S(?O).sub.2Me 0 A-5040 H H H H H O C(?O)cyclopropyl H 3-S(?O).sub.2Me 0 A-5041 H H H H H O C(?O)cyclopropyl H 2-SCF.sub.3 0 A-5042 H H H H H O C(?O)cyclopropyl H 3-SCF.sub.3 0 A-5043 H H H H H O C(?O)cyclopropyl H 3-S(?O)CF.sub.3 0 A-5044 H H H H H O C(?O)cyclopropyl H 3-SCF(CF.sub.3).sub.2 0 A-5045 H H H H H O C(?O)cyclopropyl H 2-(cyclopropylthio) 0 A-5046 H H H H H O C(?O)cyclopropyl H 2-(cyclopropylsulfinyl) 0 A-5047 H H H H H O C(?O)cyclopropyl H 2-(cyclopropylsulfonyl) 0 A-5048 H H H H H O C(?O)cyclopropyl H 2-C(?O)Me 0 A-5049 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2C(?O)CH.sub.3 0 A-5050 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2C(?O)CF.sub.3 0 A-5051 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2OH 0 A 5052 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2OCH.sub.3 0 A-5053 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-5054 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2SCH.sub.3 0 A-5055 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2S(?O)CH.sub.3 0 A-5056 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2S(?O)2CH.sub.3 0 A-5057 H H H H H O C(?O)cyclopropyl H 2-(benzyloxy) 0 A-5058 H H H H H O C(?O)cyclopropyl H 2-NH.sub.2 0 A-5059 H H H H H O C(?O)cyclopropyl H 2-NHMe 0 A-5060 H H H H H O C(?O)cyclopropyl H 2-N(Me).sub.2 0 A-5061 H H H H H O C(?O)cyclopropyl H 2-(1,3-dioxolan-2-yl) 0 A-5062 H H H H H O C(?O)cyclopropyl H 2-(1,3-dioxan-2-yl) 0 A-5063 H H H H H O C(?O)cyclopropyl H 2-(1H-imidazol-2-yl) 0 A 5064 H H H H H O C(?O)cyclopropyl H 2-(thiazol-2-yl) 0 A-5065 H H H H H O C(?O)cyclopropyl H 2-(oxazol-2-yl) 0 A-5066 H H H H H O C(?O)cyclopropyl H 2-CH?NOH 0 A-5067 H H H H H O C(?O)cyclopropyl H 2-CH?NOMe 0 A-5068 H H H H H O C(?O)cyclopropyl H 2-(4,5-dihydro-3-isoxazolyl) 0
(191) TABLE-US-00090 TABLE 90 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5069 H H H H H O C(?O)cyclopropyl H 2-CN 0 A-5070 H H H H H O C(?O)cyclopropyl H 2-NO.sub.2 0 A-5071 H H H H H O C(?O)cyclopropyl H 2-F,6-Cl 0 A-5072 H H H H H O C(?O)cyclopropyl H 2-F,6-Me 0 A-5073 H H H H H O C(?O)cyclopropyl H 3-F,6-Me 0 A-5074 H H H H H O C(?O)cyclopropyl H 4-F,2-Me 0 A-5075 H H H H H O C(?O)cyclopropyl H 2-F,6-OMe 0 A-5076 H H H H H O C(?O)cyclopropyl H 3-F,6-OMe 0 A-5077 H H H H H O C(?O)cyclopropyl H 2,6-Cl.sub.2 0 A-5078 H H H H H O C(?O)cyclopropyl H 2-Cl,6-Me 0 A-5079 H H H H H O C(?O)cyclopropyl H 3-Cl,6-Me 0 A-5080 H H H H H O C(?O)cyclopropyl H 4-Cl,2-Me 0 A-5081 H H H H H O C(?O)cyclopropyl H 2-Cl,5-CF.sub.3 0 A-5082 H H H H H O C(?O)cyclopropyl H 2-Cl,6-CF.sub.3 0 A-5083 H H H H H O C(?O)cyclopropyl H 2-Cl,6 OMe 0 A-5084 H H H H H O C(?O)cyclopropyl H 3-Cl,6-OMe 0 A-5085 H H H H H O C(?O)cyclopropyl H 4-Cl,2-OMe 0 A-5086 H H H H H O C(?O)cyclopropyl H 2,4-Me.sub.2 0 A-5087 H H H H H O C(?O)cyclopropyl H 2,5-Me.sub.2 0 A-5088 H H H H H O C(?O)cyclopropyl H 2,6-Me.sub.2 0 A-5089 H H H H H O C(?O)cyclopropyl H 2-Me,4-CF.sub.3 0 A-5090 H H H H H O C(?O)cyclopropyl H 2-Me,5-CF.sub.3 0 A-5091 H H H H H O C(?O)cyclopropyl H 2-Me,6-CF.sub.3 0 A-5092 H H H H H O C(?O)cyclopropyl H 2-Me,4-OMe 0 A-5093 H H H H H O C(?O)cyclopropyl H 2-Me,5-OMe 0 A-5094 H H H H H O C(?O)cyclopropyl H 2-Me,6-OMe 0 A-5095 H H H H H O C(?O)cyclopropyl H 3-Me,6-OMe 0 A-5096 H H H H H O C(?O)cyclopropyl H 4-Me,2-OMe 0 A-5097 H H H H H O C(?O)cyclopropyl H 2,5-OMe.sub.2 0 A-5098 H H H H H O C(?O)cyclopropyl H 2,6-OMe.sub.2 0 A-5099 H H H H H O C(?O)cyclopropyl H 2-OMe,6-CF.sub.3 0 A-5100 H H H H H O C(?O)cyclopropyl H 2-CHF.sub.2,5-F 0 A-5101 H H H H H O C(?O)cyclopropyl H 2-CHF.sub.2,6-F 0 A-5102 H H H H H O C(?O)cyclopropyl H 2-CHF.sub.2,5-Me 0 A-5103 H H H H H O C(?O)cyclopropyl H 2-CHF.sub.2,6-Me 0 A-5104 H H H H H O C(?O)cyclopropyl H 2-cyclopropyl,5-F 0 A-5105 H H H H H O C(?O)cyclopropyl H 2-cyclopropyl,6-F 0 A-5106 H H H H H O C(?O)cyclopropyl H 2-cyclopropyl,5-Me 0 A-5107 H H H H H O C(?O)cyclopropyl H 2-cyclopropyl,6-Me 0 A-5108 H H H H H O C(?O)cyclopropyl H 2-ethenyl,6-F 0 A-5109 H H H H H O C(?O)cyclopropyl H 2-ethenyl,6-Me 0 A-5110 H H H H H O C(?O)cyclopropyl H 2-OEt,5-F 0 A-5111 H H H H H O C(?O)cyclopropyl H 2-OEt,6-F 0 A-5112 H H H H H O C(?O)cyclopropyl H 2-OEt,5-Cl 0 A-5113 H H H H H O C(?O)cyclopropyl H 2-OEt,6-Cl 0 A-5114 H H H H H O C(?O)cyclopropyl H 2-OEt,5-Me 0 A-5115 H H H H H O C(?O)cyclopropyl H 2-OEt,6-Me 0 A-5116 H H H H H O C(?O)cyclopropyl H 2-OCHF.sub.2,5-F 0 A-5117 H H H H H O C(?O)cyclopropyl H 2-OCHF.sub.2,6-F 0 A-5118 H H H H H O C(?O)cyclopropyl H 2-OCHF.sub.2,5-Me 0 A-5119 H H H H H O C(?O)cyclopropyl H 2-OCHF.sub.2,6-Me 0 A-5120 H H H H H O C(?O)cyclopropyl H 2-(cyclopropyloxy),5-F 0 A-5121 H H H H H O C(?O)cyclopropyl H 2-(cyclopropyloxy),6-F 0 A-5122 H H H H H O C(?O)cyclopropyl H 2-(cyclopropyloxy),5-Me 0 A-5123 H H H H H O C(?O)cyclopropyl H 2-(cyclopropyloxy) ,6-Me 0 A-5124 H H H H H O C(?O)cyclopropyl H 2-SMe,5-F 0 A-5125 H H H H H O C(?O)cyclopropyl H 2-SMe,6-F 0
(192) TABLE-US-00091 TABLE 91 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5126 H H H H H O C(?O)cyclopropyl H 2-SMe,5-Me 0 A-5127 H H H H H O C(?O)cyclopropyl H 2-SMe,6-Me 0 A-5128 H H H H H O C(?O)cyclopropyl H 2-S(?O)Me,5-F 0 A-5129 H H H H H O C(?O)cyclopropyl H 2-S(?O)Me,6-F 0 A-5130 H H H H H O C(?O)cyclopropyl H 2-S(?O)Me,5-Me 0 A-5131 H H H H H O C(?O)cyclopropyl H 2-S(?O)Me,6-Me 0 A-5132 H H H H H O C(?O)cyclopropyl H 2-S(?O).sub.2Me,5-F 0 A-5133 H H H H H O C(?O)cyclopropyl H 2-S(?O).sub.2Me,6-F 0 A-5134 H H H H H O C(?O)cyclopropyl H 2-S ?O).sub.2Me,5-Me 0 A-5135 H H H H H O C(?O)cyclopropyl H 2-S(?O).sub.2Me,6-Me 0 A-5136 H H H H H O C(?O)cyclopropyl H 2-SCF.sub.3,5-F 0 A 5137 H H H H H O C(?O)cyclopropyl H 2-SCF.sub.3,6-F 0 A-5138 H H H H H O C(?O)cyclopropyl H 2-SCF.sub.3,5-Me 0 A-5139 H H H H H O C(?O)cyclopropyl H 2-SCF.sub.3,6-Me 0 A-5140 H H H H H O C(?O)cyclopropyl H 2-S(?O)CF.sub.3,5-F 0 A-5141 H H H H H O C(?O)cyclopropyl H 2-S(?O)CF.sub.3,6-F 0 A-5142 H H H H H O C(?O)cyclopropyl H 2-S(?O)CF.sub.3,5-Me 0 A-5143 H H H H H O C(?O)cyclopropyl H 2-S(?O)CF.sub.3,6-Me 0 A-5144 H H H H H O C(?O)cyclopropyl H 2-S(?O).sub.2CF.sub.3,5-F 0 A-5145 H H H H H O C(?O)cyclopropyl H 2-S(?O).sub.2CF.sub.3,6-F 0 A-5146 H H H H H O C(?O)cyclopropyl H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-5147 H H H H H O C(?O)cyclopropyl H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-5148 H H H H H O C(?O)cyclopropyl H 2-(cyclopropylthio),5-F 0 A-5149 H H H H H O C(?O)cyclopropyl H 2-(cyclopropylthio),6-F 0 A-5150 H H H H H O C(?O)cyclopropyl H 2-(cyclopropylthio),5-Me 0 A-5151 H H H H H O C(?O)cyclopropyl H 2-(cyclopropylthio),6-Me 0 A-5152 H H H H H O C(?O)cyclopropyl H 2-C(?O)Me,5-F 0 A-5153 H H H H H O C(?O)cyclopropyl H 2-C(?O)Me,6-F 0 A-5154 H H H H H O C(?O)cyclopropyl H 2-C(?O)Me,5-Me 0 A-5155 H H H H H O C(?O)cyclopropyl H 2-C(?O)Me,6-Me 0 A-5156 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2OH,5-F 0 A-5157 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2OH,6-F 0 A-5158 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2OH,5-Me 0 A 5159 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2OH,6-Me 0 A-5160 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2OCH.sub.3,4-F 0 A-5161 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2OCH.sub.3,5-F 0 A-5162 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2OCH.sub.3,6-F 0 A-5163 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2OCH.sub.3,4-Me 0 A-5164 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2OCH.sub.3,5-Me 0 A-5165 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2OCH.sub.3,6-Me 0 A-5166 H H H H H O C(?O)cyclopropyl H 2-OC(?O)CH.sub.3,5-F 0 A-5167 H H H H H O C(?O)cyclopropyl H 2-OC(?O)CH.sub.3,6-F 0 A-5168 H H H H H O C(?O)cyclopropyl H 2-OC(?O)CH.sub.3,5-Me 0 A-5169 H H H H H O C(?O)cyclopropyl H 2-OC(?O)CH.sub.3,6-Me 0 A-5170 H H H H H O C(?O)cyclopropyl H 2-OS(?O)CH.sub.3,5-F 0 A-5171 H H H H H O C(?O)cyclopropyl H 2-OS(?O)CH.sub.3,6-F 0 A-5172 H H H H H O C(?O)cyclopropyl H 2-OS(?O)CH.sub.3,5-Me 0 A-5173 H H H H H O C(?O)cyclopropyl H 2-OS(?O)CH.sub.3,6-Me 0 A-5174 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2SCH.sub.3,5-F 0 A-5175 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2SCH.sub.3,6-F 0 A-5176 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2SCH.sub.3,5-Me 0 A-5177 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2SCH.sub.3,6-Me 0 A-5178 H H H H H O C(?O)cyclopropyl H 2-NMe.sub.2,5-F 0 A-5179 H H H H H O C(?O)cyclopropyl H 2-NMe.sub.2,6-F 0 A-5180 H H H H H O C(?O)cyclopropyl H 2-NMe.sub.2,5-Me 0 A-5181 H H H H H O C(?O)cyclopropyl H 2-NMe.sub.2,6-Me 0 A-5182 H H H H H O C(?O)cyclopropyl H 2-CN,4-F 0
(193) TABLE-US-00092 TABLE 92 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5183 H H H H H O C(?O)cyclopropyl H 2-CN,5-F 0 A-5184 H H H H H O C(?O)cyclopropyl H 2-CN,6-F 0 A-5185 H H H H H O C(?O)cyclopropyl H 2-CN,6-Me 0 A-5186 H H H H H O C(?O)cyclopropyl H 2-CN,5-OMe 0 A-5187 H H H H H O C(?O)cyclopropyl H 2-CN,6-OMe 0 A-5188 H H H H H O C(?O)cyclopropyl H 3-CN,6-Me 0 A-5189 H H H H H O C(?O)cyclopropyl H 3-CN,6-OMe 0 A-5190 H H H H H O C(?O)cyclopropyl H 4-CN,2-Me 0 A-5191 H H H H H O C(?O)cyclopropyl H 4-CN,2-OMe 0 A-5192 H H H H H O C(?O)cyclopropyl H 2-NO.sub.2,4-F 0 A-5193 H H H H H O C(?O)cyclopropyl H 2-NO.sub.2,5-F 0 A-5194 H H H H H O C(?O)cyclopropyl H 2-NO.sub.2,6-F 0 A-5195 H H H H H O C(?O)cyclopropyl H 2-NO.sub.2,4-Me 0 A-5196 H H H H H O C(?O)cyclopropyl H 2-NO.sub.2,5-Me 0 A-5197 H H H H H O C(?O)cyclopropyl H 2-NO.sub.2,6-Me 0 A-5198 H H H H H O C(?O)cyclopropyl H 2-Me,4,5 F.sub.2 0 A-5199 H H H H H O C(?O)cyclopropyl H 2-Me,6-Et 0 A-5200 H H H H H O C(?O)cyclopropyl H 2-cyclopropyl,6-OMe 0 A-5201 H H H H H O C(?O)cyclopropyl H 2-Me,5-Et 0 A-5202 H H H H H O C(?O)cyclopropyl H 2,6-Et.sub.2 0 A-5203 H H H H H O C(?O)cyclopropyl H 2-Et,6-F 0 A-5204 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-5205 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-5206 H H H H H O C(?O)cyclopropyl H 2-CH.sub.2NMe.sub.2 0 A-5207 H H H H H O C(?O)OCH.sub.3 H H 0 A-5208 H H H H H O C(?O)OCH.sub.3 H 2-F 0 A-5209 H H H H H O C(?O)OCH.sub.3 H 2-C 0 A-5210 H H H H H O C(?O)OCH.sub.3 H 2-Br 0 A-5211 H H H H H O C(?O)OCH.sub.3 H 2-OH 0 A-5212 H H H H H O C(?O)OCH.sub.3 H 2-Me 0 A-5213 H H H H H O C(?O)OCH.sub.3 H 2-Et 0 A-5214 H H H H H O C(?O)OCH.sub.3 H 2-Pr 0 A-5215 H H H H H O C(?O)OCH.sub.3 H 2-CF 0 A-5216 H H H H H O C(?O)OCH.sub.3 H 2-CHF.sub.2 0 A-5217 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2F 0 A-5218 H H H H H O C(?O)OCH.sub.3 H 2-CF.sub.2Cl 0 A-5219 H H H H H O C(?O)OCH.sub.3 H 2-cyclopropyl 0 A-5220 H H H H H O C(?O)OCH.sub.3 H 2-cyclobutyl 0 A-5221 H H H H H O C(?O)OCH.sub.3 H 2-cyclopentyl 0 A-5222 H H H H H O C(?O)OCH.sub.3 H 2-ethenyl 0 A-5223 H H H H H O C(?O)OCH.sub.3 H 2-allyl 0 A-5224 H H H H H O C(?O)OCH.sub.3 H 2-(prop-1en-1-yl) 0 A-5225 H H H H H O C(?O)OCH.sub.3 H 2-(trifluoroethenyl) 0 A-5226 H H H H H O C(?O)OCH.sub.3 H 2-OMe 0 A-5227 H H H H H O C(?O)OCH.sub.3 H 2-OEt 0 A-5228 H H H H H O C(?O)OCH.sub.3 H 2-OPr 0 A-5229 H H H H H O C(?O)OCH.sub.3 H 2-O(i-Pr) 0 A 5230 H H H H H O C(?O)OCH.sub.3 H 2-OCF.sub.3 0 A-5231 H H H H H O C(?O)OCH.sub.3 H 2-OCHF.sub.2 0 A-5232 H H H H H O C(?O)OCH.sub.3 H 2-(cyclopropyloxy) 0 A-5233 H H H H H O C(?O)OCH.sub.3 H 2-(cyclobutyloxy) 0 A-5234 H H H H H O C(?O)OCH.sub.3 H 2-(cyclopentyloxy) 0 A-5235 H H H H H O C(?O)OCH.sub.3 H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-5236 H H H H H O C(?O)OCH.sub.3 H 2-(oxiran-2-yl) 0 A-5237 H H H H H O C(?O)OCH.sub.3 H 2-SMe 0 A-5238 H H H H H O C(?O)OCH.sub.3 H 3-SMe 0 A-5239 H H H H H O C(?O)OCH.sub.3 H 2-S(?O)Me 0
(194) TABLE-US-00093 TABLE 93 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5240 H H H H H O C(?O)OCH.sub.3 H 3-S(?O)Me 0 A-5241 H H H H H O C(?O)OCH.sub.3 H 2-S(?O).sub.2Me 0 A-5242 H H H H H O C(?O)OCH.sub.3 H 3-S(?O).sub.2Me 0 A 5243 H H H H H O C(?O)OCH.sub.3 H 2-SCF.sub.3 0 A-5244 H H H H H O C(?O)OCH.sub.3 H 3-SCF.sub.3 0 A-5245 H H H H H O C(?O)OCH.sub.3 H 3-S(?O)CF.sub.3 0 A-5246 H H H H H O C(?O)OCH.sub.3 H 3-SCF(CF.sub.3).sub.2 0 A-5247 H H H H H O C(?O)OCH.sub.3 H 2-(cyclopropylthio) 0 A-5248 H H H H H O C(?O)OCH.sub.3 H 2-(cyclopropylsulfinyl) 0 A-5249 H H H H H O C(?O)OCH.sub.3 H 2-(cyclopropylsulfonyl) 0 A-5250 H H H H H O C(?O)OCH.sub.3 H 2-C(?O)Me 0 A-5251 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2C(?O)CH.sub.3 0 A-5252 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2C(?O)CF.sub.3 0 A-5253 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2OH 0 A-5254 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3 0 A-5255 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-5256 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2SCH.sub.3 0 A-5257 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2S(?O)CH.sub.3 0 A-5258 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-5259 H H H H H O C(?O)OCH.sub.3 H 2-(benzyloxy) 0 A-5260 H H H H H O C(?O)OCH.sub.3 H 2-NH.sub.2 0 A-5261 H H H H H O C(?O)OCH.sub.3 H 2-NHMe 0 A-5262 H H H H H O C(?O)OCH.sub.3 H 2-N(Me).sub.2 0 A-5263 H H H H H O C(?O)OCH.sub.3 H 2-(1,3-dioxolan-2-yl) 0 A-5264 H H H H H O C(?O)OCH.sub.3 H 2-(1,3-dioxan-2-yl) 0 A-5265 H H H H H O C(?O)OCH.sub.3 H 2-(1H-imidazol-2-yl) 0 A-5266 H H H H H O C(?O)OCH.sub.3 H 2-(thiazol-2-yl) 0 A-5267 H H H H H O C(?O)OCH.sub.3 H 2-(oxazol-2-yl) 0 A-5268 H H H H H O C(?O)OCH.sub.3 H 2-CH?NOH 0 A-5269 H H H H H O C(?O)OCH.sub.3 H 2-CH?NOMe 0 A-5270 H H H H H O C(?O)OCH.sub.3 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-5271 H H H H H O C(?O)OCH.sub.3 H 2-CN 0 A-5272 H H H H H O C(?O)OCH.sub.3 H 2-NO.sub.2 0 A-5273 H H H H H O C(?O)OCH.sub.3 H 2-F,6-Cl 0 A-5274 H H H H H O C(?O)OCH.sub.3 H 2-F,6-Me 0 A-5275 H H H H H O C(?O)OCH.sub.3 H 3-F,6-Me 0 A-5276 H H H H H O C(?O)OCH.sub.3 H 4-F,2-Me 0 A-5277 H H H H H O C(?O)OCH.sub.3 H 2-F,6-OMe 0 A-5278 H H H H H O C(?O)OCH.sub.3 H 3-F,6-OMe 0 A-5279 H H H H H O C(?O)OCH.sub.3 H 2,6-Cl.sub.2 0 A-5280 H H H H H O C(?O)OCH.sub.3 H 2-Cl,6-Me 0 A-5281 H H H H H O C(?O)OCH.sub.3 H 3-Cl,6-Me 0 A-5282 H H H H H O C(?O)OCH.sub.3 H 4-Cl,2-Me 0 A-5283 H H H H H O C(?O)OCH.sub.3 H 2-Cl,5-CF.sub.3 0 A-5284 H H H H H O C(?O)OCH.sub.3 H 2-Cl,6-CF.sub.3 0 A-5285 H H H H H O C(?O)OCH.sub.3 H 2-Cl,6-OMe 0 A-5286 H H H H H O C(?O)OCH.sub.3 H 3-Cl,6 OMe 0 A-5287 H H H H H O C(?O)OCH.sub.3 H 4-Cl,2-OMe 0 A-5288 H H H H H O C(?O)OCH.sub.3 H 2,4-Me.sub.2 0 A-5289 H H H H H O C(?O)OCH.sub.3 H 2,5-Me.sub.2 0 A-5290 H H H H H O C(?O)OCH.sub.3 H 2,6-Me.sub.2 0 A-5291 H H H H H O C(?O)OCH.sub.3 H 2-Me,4-CF.sub.3 0 A-5292 H H H H H O C(?O)OCH.sub.3 H 2-Me,5-CF.sub.3 0 A-5293 H H H H H O C(?O)OCH.sub.3 H 2-Me,6-CF.sub.3 0 A-5294 H H H H H O C(?O)OCH.sub.3 H 2-Me,4-OMe 0 A-5295 H H H H H O C(?O)OCH.sub.3 H 2-Me,5-OMe 0 A-5296 H H H H H O C(?O)OCH.sub.3 H 2-Me,6-OMe 0
(195) TABLE-US-00094 TABLE 94 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5297 H H H H H O C(?O)OCH.sub.3 H 3-Me,6-OMe 0 A-5298 H H H H H O C(?O)OCH.sub.3 H 4-Me,2-OMe 0 A-5299 H H H H H O C(?O)OCH.sub.3 H 2,5-OMe.sub.2 0 A-5300 H H H H H O C(?O)OCH.sub.3 H 2,6-OMe.sub.2 0 A-5301 H H H H H O C(?O)OCH.sub.3 H 2-OMe,6-CF.sub.3 0 A-5302 H H H H H O C(?O)OCH.sub.3 H 2-CHF.sub.2,5-F 0 A-5303 H H H H H O C(?O)OCH.sub.3 H 2-CHF.sub.2,6-F 0 A-5304 H H H H H O C(?O)OCH.sub.3 H 2-CHF.sub.2,5-Me 0 A-5305 H H H H H O C(?O)OCH.sub.3 H 2-CHF.sub.2,6-Me 0 A-5306 H H H H H O C(?O)OCH.sub.3 H 2-cyclopropyl,5-F 0 A-5307 H H H H H O C(?O)OCH.sub.3 H 2-cyclopropyl,6-F 0 A-5308 H H H H H O C(?O)OCH.sub.3 H 2-cyclopropyl,5-Me 0 A-5309 H H H H H O C(?O)OCH.sub.3 H 2-cyclopropyl,6-Me 0 A-5310 H H H H H O C(?O)OCH.sub.3 H 2-ethenyl,6-F 0 A-5311 H H H H H O C(?O)OCH.sub.3 H 2-ethenyl,6-Me 0 A-5312 H H H H H O C(?O)OCH.sub.3 H 2-OEt,5-F 0 A-5313 H H H H H O C(?O)OCH.sub.3 H 2-OEt,6-F 0 A-5314 H H H H H O C(?O)OCH.sub.3 H 2-OEt,5-Cl 0 A-5315 H H H H H O C(?O)OCH.sub.3 H 2-OEt,6-Cl 0 A-5316 H H H H H O C(?O)OCH.sub.3 H 2-OEt,5-Me 0 A-5317 H H H H H O C(?O)OCH.sub.3 H 2-OEt,6-Me 0 A-5318 H H H H H O C(?O)OCH.sub.3 H 2-OCHF.sub.2,5-F 0 A-5319 H H H H H O C(?O)OCH.sub.3 H 2-OCHF.sub.2,6-F 0 A-5320 H H H H H O C(?O)OCH.sub.3 H 2-OCHF.sub.2,5-Me 0 A-5321 H H H H H O C(?O)OCH.sub.3 H 2-OCHF.sub.2,6-Me 0 A-5322 H H H H H O C(?O)OCH.sub.3 H 2-(cyclopropyloxy),5-F 0 A-5323 H H H H H O C(?O)OCH.sub.3 H 2-(cyclopropyloxy),6-F 0 A-5324 H H H H H O C(?O)OCH.sub.3 H 2-(cyclopropyloxy),5-Me 0 A-5325 H H H H H O C(?O)OCH.sub.3 H 2-(cyclopropyloxy),6-Me 0 A-5326 H H H H H O C(?O)OCH.sub.3 H 2-SMe,5-F 0 A-5327 H H H H H O C(?O)OCH.sub.3 H 2-SMe,6-F 0 A-5328 H H H H H O C(?O)OCH.sub.3 H 2-SMe,5-Me 0 A-5329 H H H H H O C(?O)OCH.sub.3 H 2-SMe,6-Me 0 A-5330 H H H H H O C(?O)OCH.sub.3 H 2-S(?O)Me,5-F 0 A-5331 H H H H H O C(?O)OCH.sub.3 H 2-S(?O)Me,6-F 0 A-5332 H H H H H O C(?O)OCH.sub.3 H 2-S(?O)Me,5-Me 0 A-5333 H H H H H O C(?O)OCH.sub.3 H 2-S(?O)Me,6-Me 0 A-5334 H H H H H O C(?O)OCH.sub.3 H 2-S(?O)2Me,5-F 0 A-5335 H H H H H O C(?O)OCH.sub.3 H 2-S(?O)2Me,6-F 0 A-5336 H H H H H O C(?O)OCH.sub.3 H 2-S ?O)2Me,5-Me 0 A-5337 H H H H H O C(?O)OCH.sub.3 H 2-S(?O)2Me,6-Me 0 A-5338 H H H H H O C(?O)OCH.sub.3 H 2-SCF.sub.3,5-F 0 A-5339 H H H H H O C(?O)OCH.sub.3 H 2-SCF.sub.3,6-F 0 A-5340 H H H H H O C(?O)OCH.sub.3 H 2-SCF.sub.3,5-Me 0 A-5341 H H H H H O C(?O)OCH.sub.3 H 2-SCF.sub.3,6-Me 0 A-5342 H H H H H O C(?O)OCH.sub.3 H 2-S(?O)CF.sub.3,5-F 0 A-5343 H H H H H O C(?O)OCH.sub.3 H 2-S(?O)CF.sub.3,6-F 0 A-5344 H H H H H O C(?O)OCH.sub.3 H 2-S(?O)CF.sub.3,5-Me 0 A-5345 H H H H H O C(?O)OCH.sub.3 H 2-S(?O)CF.sub.3,6-Me 0 A-5346 H H H H H O C(?O)OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-5347 H H H H H O C(?O)OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-5348 H H H H H O C(?O)OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-5349 H H H H H O C(?O)OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-5350 H H H H H O C(?O)OCH.sub.3 H 2-(cyclopropylthio),5-F 0 A-5351 H H H H H O C(?O)OCH.sub.3 H 2-(cyclopropylthio),6-F 0 A-5352 H H H H H O C(?O)OCH.sub.3 H 2-(cyclopropylthio),5-Me 0 A-5353 H H H H H O C(?O)OCH.sub.3 H 2-(cyclopropylthio),6-Me 0
(196) TABLE-US-00095 TABLE 95 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5354 H H H H H O C(?O)OCH.sub.3 H 2-C(?O)Me,5-F O A-5355 H H H H H O C(?O)OCH.sub.3 H 2-C(?O)Me,6-F O A-5356 H H H H H O C(?O)OCH.sub.3 H 2-C(?O)Me,5-Me O A-5357 H H H H H O C(?O)OCH.sub.3 H 2-C(?O)Me,6-Me O A-5358 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2OH,5-F O A-5359 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2OH,6-F O A-5360 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2OH,5-Me O A-5361 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2OH,6-Me O A-5362 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,4-F O A-5363 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,5-F O A-5364 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,6-F O A-5365 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,4-Me O A-5366 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,5-Me O A-5367 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Me O A-5368 H H H H H O C(?O)OCH.sub.3 H 2-OC(?O)CH.sub.3,5-F O A-5369 H H H H H O C(?O)OCH.sub.3 H 2-OC(?O)CH.sub.3,6-F O A-5370 H H H H H O C(?O)OCH.sub.3 H 2-OC(?O)CH.sub.3,5-Me O A-5371 H H H H H O C(?O)OCH.sub.3 H 2-OC(?O)CH.sub.3,6-Me O A-5372 H H H H H O C(?O)OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-F O A-5373 H H H H H O C(?O)OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-F O A-5374 H H H H H O C(?O)OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-Me O A-5375 H H H H H O C(?O)OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-Me O A-5376 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2SCH.sub.3,5-F O A-5377 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2SCH.sub.3,6-F O A-5378 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2SCH.sub.3,5-Me O A-5379 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2SCH.sub.3,6-Me O A-5380 H H H H H O C(?O)OCH.sub.3 H 2-NMe.sub.2,5-F O A-5381 H H H H H O C(?O)OCH.sub.3 H 2-NMe.sub.2,6-F O A-5382 H H H H H O C(?O)OCH.sub.3 H 2-NMe.sub.2,5-Me O A-5383 H H H H H O C(?O)OCH.sub.3 H 2-NMe.sub.2,6-Me O A-5384 H H H H H O C(?O)OCH.sub.3 H 2-CN,4-F O A-5385 H H H H H O C(?O)OCH.sub.3 H 2-CN,5F O A-5386 H H H H H O C(?O)OCH.sub.3 H 2-CN,6-F O A-5387 H H H H H O C(?O)OCH.sub.3 H 2-CN,6-Me O A-5388 H H H H H O C(?O)OCH.sub.3 H 2-CN,5-OMe O A-5389 H H H H H O C(?O)OCH.sub.3 H 2-CN,6-OMe O A-5390 H H H H H O C(?O)OCH.sub.3 H 3-CN,6-Me O A-5391 H H H H H O C(?O)OCH.sub.3 H 3-CN,6-OMe O A-5392 H H H H H O C(?O)OCH.sub.3 H 4-CN,2-Me O A-5393 H H H H H O C(?O)OCH.sub.3 H 4-CN,2-OMe O A-5394 H H H H H O C(?O)OCH.sub.3 H 2-NO.sub.2,4-F O A-5395 H H H H H O C(?O)OCH.sub.3 H 2-NO.sub.2,5-F O A-5396 H H H H H O C(?O)OCH.sub.3 H 2-NO.sub.2,6-F O A-5397 H H H H H O C(?O)OCH.sub.3 H 2-NO.sub.2,4-Me O A-5398 H H H H H O C(?O)OCH.sub.3 H 2-NO.sub.2,5-Me O A-5399 H H H H H O C(?O)OCH.sub.3 H 2-NO.sub.2,6-Me O A-5400 H H H H H O C(?O)OCH.sub.3 H 2-Me,4,5-F.sub.2 O A-5401 H H H H H O C(?O)OCH.sub.3 H 2-Me,6-Et O A-5402 H H H H H O C(?O)OCH.sub.3 H 2-cyclopropyl,6-OMe O A-5403 H H H H H O C(?O)OCH.sub.3 H 2-Me,5-Et O A-5404 H H H H H O C(?O)OCH.sub.3 H 2,6-Et.sub.2 O A-5405 H H H H H O C(?O)OCH.sub.3 H 2-Et,6-F O A-5406 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Cl O A-5407 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl O A-5408 H H H H H O C(?O)OCH.sub.3 H 2-CH.sub.2NMe.sub.2 O A-5409 H H H H H O C(?O)OCH.sub.3 H H O A-5410 H H H H H O C(?O)OCH.sub.3 H 2F O
(197) TABLE-US-00096 TABLE 96 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5411 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Cl O A-5412 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Br O A-5413 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OH O A-5414 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Me O A-5415 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Et O A-5416 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Pr O A-5417 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CF.sub.3 O A-5418 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CHF.sub.2 O A-5419 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2F O A-5420 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CF.sub.2Cl O A-5421 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-cyclopropyl O A-5422 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-cyclobutyl O A-5423 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-cyclopentyl O A-5424 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-ethenyl O A-5425 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-allyl O A-5426 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(prop-1-en-1-yl) O A-5427 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(trifluoroethenyl) O A-5428 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OMe O A-5429 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OEt O A-5430 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OPr O A-5431 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-O(i-Pr) O A-5432 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OCF.sub.3 O A-5433 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OCHF.sub.2 O A-5434 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropyloxy) O A-5435 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclobutyloxy) O A-5436 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopentyloxy) O A-5437 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-((2,2-dichlorocyclopropyl)oxy) O A-5438 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(oxiran-2-yl) O A-5439 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-SMe O A-5440 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-SMe O A-5441 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O)Me O A-5442 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-S(?O)Me O A-5443 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O).sub.2Me O A-5444 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-S(?O).sub.2Me O A-5445 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-SCF.sub.3 O A-5446 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-SCF.sub.3 O A-5447 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-S(?O)CF.sub.3 O A-5448 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-SCF(CF.sub.3).sub.2 O A-5449 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropylthio) O A-5450 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropylsulfinyl) O A-5451 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropylsulfonyl) O A-5452 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-C(?O)Me O A-5453 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2C(?O)CH.sub.3 O A-5454 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2C(?O)CF.sub.3 O A-5455 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OH O A-5456 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3 O A-5457 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3 O A-5458 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3 O A-5459 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2S(?O)CH.sub.3 O A-5460 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2S(?O).sub.2CH.sub.3 O A-5461 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(benzyloxy) O A-5462 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NH.sub.2 O A-5463 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NHMe O A-5464 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-N(Me).sub.2 O A-5465 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(1,3-dioxolan-2-yl) O A-5466 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(1,3-dioxan-2-yl) O A-5467 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(1H-midazo-2-yl) O
(198) TABLE-US-00097 TABLE 97 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5468 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(thiazol-2-yl) O A-5469 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(oxazol-2-yl) O A-5470 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH?NOH O A-5471 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH?NOMe O A-5472 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(4,5-dihydro-3-isoxazolyl) O A-5473 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CN O A-5474 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NO.sub.2 O A-5475 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-F,6-Cl O A-5476 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-F,6-Me O A-5477 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-F,6-Me O A-5478 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 4-F,2-Me O A-5479 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-F,6-OMe O A-5480 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-F,6-OMe O A-5481 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2,6-Cl.sub.2 O A-5482 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Cl,6-Me O A-5483 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-Cl,6-Me O A-5484 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 4-Cl,2-Me O A-5485 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Cl,5-CF.sub.3 O A-5486 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Cl,6-CF.sub.3 O A-5487 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Cl,6-OMe O A-5488 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-Cl,6-OMe O A-5489 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 4-Cl,2-OMe O A-5490 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2,4-Me.sub.2 O A-5491 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2,5-Me.sub.2 O A-5492 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2,6-Me.sub.2 O A-5493 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Me,4-CF.sub.3 O A-5494 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Me,5-CF.sub.3 O A-5495 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Me,6-CF.sub.3 O A-5496 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Me,4-OMe O A-5497 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Me,5-OMe O A-5498 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Me,6-OMe O A-5499 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-Me,6-OMe O A-5500 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 4-Me,2-OMe O A-5501 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2,5-OMe.sub.2 O A-5502 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2,6-OMe.sub.2 O A-5503 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OMe,6-CF.sub.3 O A-5504 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CHF.sub.2,5-F O A-5505 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CHF.sub.2,6-F O A-5506 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CHF.sub.2,5-Me O A-5507 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CHF.sub.2,6-Me O A-5508 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-cyclopropyl,5-F O A-5509 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-cyclopropyl,6-F O A-5510 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-cyclopropyl,5-Me O A-5511 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-cyclopropyl,6-Me O A-5512 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-ethenyl,6-F O A-5513 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-ethenyl,6-Me O A-5514 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OEt,5-F O A-5515 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OEt,6-F O A-5516 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OEt,5-Cl O A-5517 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OEt,6-Cl O A-5518 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OEt,5-Me O A-5519 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OEt,6-Me O A-5520 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OCHF.sub.2,5-F O A-5521 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OCHF.sub.2,6-F O A-5522 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OCHF.sub.2,5-Me O A-5523 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OCHF.sub.2,6-Me O A-5524 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropyloxy),5-F O
(199) TABLE-US-00098 TABLE 98 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5525 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropyloxy),6-F O A-5526 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropyloxy),5-Me O A-5527 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropyloxy),6-Me O A-5528 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-SMe,5-F O A-5529 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-SMe,6-F O A-5530 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-SMe,5-Me O A-5531 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-SMe,6-Me O A-5532 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O)Me,5-F O A-5533 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O)Me,6-F O A-5534 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O)Me,5-Me O A-5535 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O)Me,6-Me O A-5536 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O)2Me,5-F O A-5537 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,6-F O A-5538 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,5-Me O A-5539 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,6-Me O A-5540 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-SCF.sub.3,5-F O A-5541 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-SCF.sub.3,6-F O A-5542 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-SCF.sub.3,5-Me O A-5543 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-SCF.sub.3,6-Me O A-5544 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,5-F O A-5545 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,6-F O A-5546 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,5-Me O A-5547 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,6-Me O A-5548 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-F O A-5549 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-F O A-5550 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-Me O A-5551 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-Me O A-5552 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropylthio),5-F O A-5553 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropylthio),6-F O A-5554 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropylthio),5-Me O A-5555 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropylthio),6-Me O A-5556 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-C(?O)Me,5-F O A-5557 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-C(?O)Me,6-F O A-5558 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-C(?O)Me,5-Me O A-5559 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-C(?O)Me,6-Me O A-5560 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OH,5-F O A-5561 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OH,6-F O A-5562 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OH,5-Me O A-5563 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OH,6-Me O A-5564 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-F O A-5565 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-F O A-5566 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-F O A-5567 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-Me O A-5568 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-Me O A-5569 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Me O A-5570 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,5-F O A-5571 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,6-F O A-5572 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,5-Me O A-5573 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,6-Me O A-5574 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-F O A-5575 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OC(?O).sub.2CH.sub.3,6-F O A-5576 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-Me O A-5577 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-Me O A-5578 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-F O A-5579 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,6-F O A-5580 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-Me O A-5581 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,6-Me O
(200) TABLE-US-00099 TABLE 99 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5582 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NMe.sub.2,5-F O A-5583 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NMe.sub.2,6-F O A-5584 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NMe.sub.2,5-Me O A-5585 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NMe.sub.2,6-Me O A-5586 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CN,4-F O A-5587 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CN,5-F O A-5588 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CN,6-F O A-5589 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CN,6-Me O A-5590 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CN,5-OMe O A-5591 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CN,6-OMe O A-5592 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-CN,6-Me O A-5593 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-CN,6-OMe O A-5594 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 4-CN,2-Me O A-5595 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 4-CN,2-OMe O A-5596 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NO.sub.2,4-F O A-5597 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NO.sub.2,5-F O A-5598 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NO.sub.2,6-F O A-5599 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NO.sub.2,4-Me O A-5600 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NO.sub.2,5-Me O A-5601 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NO.sub.2,6-Me O A-5602 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Me,4,5-F.sub.2 O A-5603 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Me,6-Et O A-5604 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-cyclopropyl,6-OMe O A-5605 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Me,5-Et O A-5606 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2,6-Et.sub.2 O A-5607 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Et,6-F O A-5608 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Cl O A-5609 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl O A-5610 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2NMe.sub.2 O A-5611 H H H H H O C(?O)OCH.sub.2CH.sub.3 H H O A-5612 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-F O A-5613 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Cl O A-5614 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Br O A-5615 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OH O A-5616 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Me O A-5617 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Et O A-5618 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Pr O A-5619 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CF.sub.3 O A-5620 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CHF.sub.2 O A-5621 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2F O A-5622 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CF.sub.2Cl O A-5623 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-cyclopropyl O A-5624 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-cyclobutyl O A-5625 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-cyclopentyl O A-5626 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-ethenyl O A-5627 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-allyl O A-5628 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(prop-1-en-1-yl) O A-5629 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(trifluoroethenyl) O A-5630 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OMe O A-5631 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OEt O A-5632 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OPr O A-5633 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-O(i-Pr) O A-5634 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OCF.sub.3 O A-5635 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-OCHF.sub.2 O A-5636 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropyloxy) O A-5637 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclobutyloxy) O A-5638 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopentyloxy) O
(201) TABLE-US-00100 TABLE 100 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5639 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-((2,2-dichbrocyclopropyl)oxy) O A-5640 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(oxiran-2-yl) O A-5641 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-SMe O A-5642 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-SMe O A-5643 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O)Me O A-5644 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-S(?O)Me O A-5645 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-S(?O).sub.2Me O A-5646 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-S(?O).sub.2Me O A-5647 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-SCF.sub.3 O A-5648 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-SCF.sub.3 O A-5649 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-S(?O)CF.sub.3 O A-5650 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-SCF(CF.sub.3).sub.2 O A-5651 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropylthio) O A-5652 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropylsulfinyl) O A-5653 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(cyclopropylsulfonyl) O A-5654 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-C(?O)Me O A-5655 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2C(?O)CH.sub.3 O A-5656 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2C(?O)CF.sub.3 O A-5657 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OH O A-5658 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3 O A-5659 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3 O A-5660 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3 O A-5661 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2S(?O)CH.sub.3 O A-5662 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH.sub.2S(?O).sub.2CH.sub.3 O A-5663 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(benzyloxy) O A-5664 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NH.sub.2 O A-5665 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NHMe O A-5666 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-N(Me).sub.2 O A-5667 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(1,3-dioxolan-2-yl) O A-5668 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(1,3-dioxan-2-yl) O A-5669 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(1H-midazol-2-yl) O A-5670 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(thiazol-2-yl) O A-5671 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(oxazol-2-yl) O A-5672 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH?NOH O A-5673 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CH?NOMe O A-5674 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-(4,5-dihydro-3-isoxazolyl) O A-5675 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-CN O A-5676 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-NO.sub.2 O A-5677 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-F,6-Cl O A-5678 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-F,6-Me O A-5679 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-F,6-Me O A-5680 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 4-F,2-Me O A-5681 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-F,6-OMe O A-5682 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-F,6-OMe O A-5683 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2,6-Cl.sub.2 O A-5684 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Cl,6-Me O A-5685 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-Cl,6-Me O A-5686 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 4-Cl,2-Me O A-5687 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Cl,5-CF.sub.3 O A-5688 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Cl,6-CF.sub.3 O A-5689 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Cl,6-OMe O A-5690 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 3-Cl,6-OMe O A-5691 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 4-Cl,2-OMe O A-5692 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2,4-Me.sub.2 O A-5693 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2,5-Me.sub.2 O A-5694 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2,6-Me.sub.2 O A-5695 H H H H H O C(?O)OCH.sub.2CH.sub.3 H 2-Me,4-CF.sub.3 O
(202) TABLE-US-00101 TABLE 101 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5696 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-Me,5-CF.sub.3 O A-5697 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-Me,6-CF.sub.3 O A-5698 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-Me,4-OMe O A-5699 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-Me,5-OMe O A-5700 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-Me,6-OMe O A-5701 H H H H H O C(?O)N(CH.sub.3).sub.2 H 3-Me,6-OMe O A-5702 H H H H H O C(?O)N(CH.sub.3).sub.2 H 4-Me,2-OMe O A-5703 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2,5-OMe.sub.2 O A-5704 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2,6-OMe.sub.2 O A-5705 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OMe,6-CF.sub.3 O A-5706 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CHF.sub.2,5-F O A-5707 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CHF.sub.2,6-F O A-5708 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CHF.sub.2,5-Me O A-5709 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CHF.sub.2,6-Me O A-5710 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-cyclopropyl,5-F O A-5711 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-cyclopropyl,6-F O A-5712 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-cyclopropyl,5-Me O A-5713 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-cyclopropyl,6-Me O A-5714 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-ethenyl,6-F O A-5715 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-ethenyl,6-Me O A-5716 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OEt,5-F O A-5717 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OEt,6-F O A-5718 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OEt,5-Cl O A-5719 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OEt,6-Cl O A-5720 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OEt,5-Me O A-5721 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OEt,6-Me O A-5722 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OCHF.sub.2,5-F O A-5723 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OCHF.sub.2,6-F O A-5724 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OCHF.sub.2,5-Me O A-5725 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OCHF.sub.2,6-Me O A-5726 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),5-F O A-5727 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),6-F O A-5728 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),5-Me O A-5729 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),6-Me O A-5730 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-SMe,5-F O A-5731 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-SMe,6-F O A-5732 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-SMe,5-Me O A-5733 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-SMe,6-Me O A-5734 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O)Me,5-F O A-5735 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O)Me,6-F O A-5736 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O)Me,5-Me O A-5737 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O)Me,6-Me O A-5738 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,5-F O A-5739 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,6-F O A-5740 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,5-Me O A-5741 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,6-Me O A-5742 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-SCF.sub.3,5-F O A-5743 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-SCF.sub.3,6-F O A-5744 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-SCF.sub.3,5-Me O A-5745 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-SCF.sub.3,6-Me O A-5746 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,5F O A-5747 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,6-F O A-5748 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,5-Me O A-5749 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,6-Me O A-5750 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O).sub.2CF3,5-F O A-5751 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O).sub.2CF3,6-F O A-5752 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O).sub.2CF.sub.3,5-Me O
(203) TABLE-US-00102 TABLE 102 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5753 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-S(?O)2CF3,6-Me O A-5754 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-(cyclopropylthio),5-F O A-5755 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-(cyclopropylthio),6-F O A-5756 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-(cyclopropylthio),5-Me O A-5757 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-(cyclopropylthio),6-Me O A-5758 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-C(?O)Me,5-F O A-5759 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-C(?O)Me,6-F O A-5760 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-C(?O)Me,5-Me O A-5761 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-C(?O)Me,6-Me O A-5762 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2OH,5-F O A-5763 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2OH,6-F O A-5764 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2OH,5-Me O A-5765 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2OH,6-Me O A-5766 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,4-F O A-5767 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,5-F O A-5768 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,6-F O A-5769 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,4-Me O A-5770 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,5-Me O A-5771 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,6-Me O A-5772 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,5-F O A-5773 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,6-F O A-5774 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,5-Me O A-5775 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,6-Me O A-5776 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH.sub.3,5-F O A-5777 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH.sub.3,6-F O A-5778 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH.sub.3,5-Me O A-5779 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH.sub.3,6-Me O A-5780 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,5-F O A-5781 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,6-F O A-5782 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,5-Me O A-5783 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,6-Me O A-5784 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-NMe.sub.2,5-F O A-5785 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-NMe.sub.2,6-F O A-5786 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-NMe.sub.2,5-Me O A-5787 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-NMe.sub.2,6-Me O A-5788 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CN,4-F O A-5789 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CN,5-F O A-5790 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CN,6-F O A-5791 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CN,6-Me O A-5792 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CN,5-OMe O A-5793 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CN,6-OMe O A-5794 H H H H H O C(?O)N(CH.sub.3).sub.2 H 3-CN,6-Me O A-5795 H H H H H O C(?O)N(CH.sub.3).sub.2 H 3-CN,6-OMe O A-5796 H H H H H O C(?O)N(CH.sub.3).sub.2 H 4-CN,2-Me O A-5797 H H H H H O C(?O)N(CH.sub.3).sub.2 H 4-CN,2-OMe O A-5798 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-NO.sub.2,4-F O A-5799 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-NO.sub.2,5-F O A-5800 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-NO.sub.2,6-F O A-5801 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-NO.sub.2,4-Me O A-5802 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-NO.sub.2,5-Me O A-5803 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-NO.sub.2,6-Me O A-5804 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-Me,4,5-F.sub.2 O A-5805 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-Me,6-Et O A-5806 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-cyclopropyl,6-OMe O A-5807 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-Me,5-Et O A-5808 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2,6-Et.sub.2 O A-5809 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-Et,6-F O
(204) TABLE-US-00103 TABLE 103 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5810 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,6-Cl O A-5811 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl O A-5812 H H H H H O C(?O)N(CH.sub.3).sub.2 H 2-CH.sub.2NMe.sub.2 O A-5813 H H H H H O C(?O)(4-Cl)Ph H H O A-5814 H H H H H O C(?O)(4-Cl)Ph H 2-F O A-5815 H H H H H O C(?O)(4-Cl)Ph H 2-Cl O A-5816 H H H H H O C(?O)(4-Cl)Ph H 2-Br O A-5817 H H H H H O C(?O)(4-Cl)Ph H 2-OH O A-5818 H H H H H O C(?O)(4-Cl)Ph H 2-Me O A-5819 H H H H H O C(?O)(4-Cl)Ph H 2-Et O A-5820 H H H H H O C(?O)(4-Cl)Ph H 2-Pr O A-5821 H H H H H O C(?O)(4-Cl)Ph H 2-CF.sub.3 O A-5822 H H H H H O C(?O)(4-Cl)Ph H 2-CHF.sub.2 O A-5823 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2F O A-5824 H H H H H O C(?O)(4-Cl)Ph H 2-CF.sub.2Cl O A-5825 H H H H H O C(?O)(4-Cl)Ph H 2-cyclopropyl O A-5826 H H H H H O C(?O)(4-Cl)Ph H 2-cyclobutyl O A-5827 H H H H H O C(?O)(4-Cl)Ph H 2-cyclopentyl O A-5828 H H H H H O C(?O)(4-Cl)Ph H 2-ethenyl O A-5829 H H H H H O C(?O)(4-Cl)Ph H 2-allyl O A-5830 H H H H H O C(?O)(4-Cl)Ph H 2-(prop-1-en-1-yl) O A-5831 H H H H H O C(?O)(4-Cl)Ph H 2-(trifluoroethenyl) O A-5832 H H H H H O C(?O)(4-Cl)Ph H 2-OMe O A-5833 H H H H H O C(?O)(4-Cl)Ph H 2-OEt O A-5834 H H H H H O C(?O)(4-Cl)Ph H 2-OPr O A-5835 H H H H H O C(?O)(4-Cl)Ph H 2-O(i-Pr) O A-5836 H H H H H O C(?O)(4-Cl)Ph H 2-OCF.sub.3 O A-5837 H H H H H O C(?O)(4-Cl)Ph H 2-OCHF.sub.2 O A-5838 H H H H H O C(?O)(4-Cl)Ph H 2-(cyclopropyloxy) O A-5839 H H H H H O C(?O)(4-Cl)Ph H 2-(cyclobutyloxy) O A-5840 H H H H H O C(?O)(4-Cl)Ph H 2-(cyclopentyloxy) O A-5841 H H H H H O C(?O)(4-Cl)Ph H 2-((2,2-dichlorocyclopropyl)oxy) O A-5842 H H H H H O C(?O)(4-Cl)Ph H 2-(oxiran-2-yl) O A-5843 H H H H H O C(?O)(4-Cl)Ph H 2-SMe O A-5844 H H H H H O C(?O)(4-Cl)Ph H 3-SMe O A-5845 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O)Me O A-5846 H H H H H O C(?O)(4-Cl)Ph H 3-S(?O)Me O A-5847 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O).sub.2Me O A-5848 H H H H H O C(?O)(4-Cl)Ph H 3-S(?O).sub.2Me O A-5849 H H H H H O C(?O)(4-Cl)Ph H 2-SCF.sub.3 O A-5850 H H H H H O C(?O)(4-Cl)Ph H 3-SCF.sub.3 O A-5851 H H H H H O C(?O)(4-Cl)Ph H 3-S(?O)CF.sub.3 O A-5852 H H H H H O C(?O)(4-Cl)Ph H 3-SCF(CF.sub.3).sub.2 O A-5853 H H H H H O C(?O)(4-Cl)Ph H 2-(cyclopropylthio) O A-5854 H H H H H O C(?O)(4-Cl)Ph H 2-(cyclopropylsulfinyl) O A-5855 H H H H H O C(?O)(4-Cl)Ph H 2-(cyclopropylsulfonyl) O A-5856 H H H H H O C(?O)(4-Cl)Ph H 2-C(?O)Me O A-5857 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2C(?O)CH.sub.3 O A-5858 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2C(?O)CF.sub.3 O A-5859 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2OH O A-5860 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2OCH.sub.3 O A-5861 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2OCH.sub.2CH.sub.3 O A-5862 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2SCH.sub.3 O A-5863 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2S(?O)CH.sub.3 O A-5864 H H H H H O C(?O)(4-Cl)Ph H 2-CH2S(?O).sub.2CH.sub.3 O A-5865 H H H H H O C(?O)(4-Cl)Ph H 2-(benzyloxy) O A-5866 H H H H H O C(?O)(4-Cl)Ph H 2-NH.sub.2 O
(205) TABLE-US-00104 TABLE 104 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5867 H H H H H O C(?O)(4-Cl)Ph H 2-NHMe O A-5868 H H H H H O C(?O)(4-Cl)Ph H 2-N(Me).sub.2 O A-5869 H H H H H O C(?O)(4-Cl)Ph H 2-(1,3-dioxolan-2-yl) O A-5870 H H H H H O C(?O)(4-Cl)Ph H 2-(1,3-dioxan-2-yl) O A-5871 H H H H H O C(?O)(4-Cl)Ph H 2-(1H-imidazo1-2-yl) O A-5872 H H H H H O C(?O)(4-Cl)Ph H 2-(thiazol-2-yl) O A-5873 H H H H H O C(?O)(4-Cl)Ph H 2-(oxazol-2-yl) O A-5874 H H H H H O C(?O)(4-Cl)Ph H 2-CH?NOH O A-5875 H H H H H O C(?O)(4-Cl)Ph H 2-CH?NOMe O A-5876 H H H H H O C(?O)(4-Cl)Ph H 2-(4,5-dihydro-3-isoxazol)yl) O A-5877 H H H H H O C(?O)(4-Cl)Ph H 2-CN O A-5878 H H H H H O C(?O)(4-Cl)Ph H 2-NO.sub.2 O A-5879 H H H H H O C(?O)(4-Cl)Ph H 2-F,6-Cl O A-5880 H H H H H O C(?O)(4-Cl)Ph H 2-F,6-Me O A-5881 H H H H H O C(?O)(4-Cl)Ph H 3-F,6-Me O A-5882 H H H H H O C(?O)(4-Cl)Ph H 4-F,2-Me O A-5883 H H H H H O C(?O)(4-Cl)Ph H 2-F,6-OMe O A-5884 H H H H H O C(?O)(4-Cl)Ph H 3-F,6-OMe O A-5885 H H H H H O C(?O)(4-Cl)Ph H 2,6-Cl.sub.2 O A-5886 H H H H H O C(?O)(4-Cl)Ph H 2-Cl,6-Me O A-5887 H H H H H O C(?O)(4-Cl)Ph H 3-Cl,6-Me O A-5888 H H H H H O C(?O)(4-Cl)Ph H 4-Cl,2-Me O A-5889 H H H H H O C(?O)(4-Cl)Ph H 2-Cl,5-CF.sub.3 O A-5890 H H H H H O C(?O)(4-Cl)Ph H 2-Cl,6-CF.sub.3 O A-5891 H H H H H O C(?O)(4-Cl)Ph H 2-Cl,6-OMe O A-5892 H H H H H O C(?O)(4-Cl)Ph H 3-Cl,6-OMe O A-5893 H H H H H O C(?O)(4-Cl)Ph H 4-Cl,2-OMe O A-5894 H H H H H O C(?O)(4-Cl)Ph H 2,4-Me.sub.2 O A-5895 H H H H H O C(?O)(4-Cl)Ph H 2,5-Me.sub.2 O A-5896 H H H H H O C(?O)(4-Cl)Ph H 2,6-Me.sub.2 O A-5897 H H H H H O C(?O)(4-Cl)Ph H 2-Me,4-CF.sub.3 O A-5898 H H H H H O C(?O)(4-Cl)Ph H 2-Me,5-CF.sub.3 O A-5899 H H H H H O C(?O)(4-Cl)Ph H 2-Me,6-CF.sub.3 O A-5900 H H H H H O C(?O)(4-Cl)Ph H 2-Me,4-OMe O A-5901 H H H H H O C(?O)(4-Cl)Ph H 2-Me,5-OMe O A-5902 H H H H H O C(?O)(4-Cl)Ph H 2-Me,6-OMe O A-5903 H H H H H O C(?O)(4-Cl)Ph H 3-Me,6-OMe O A-5904 H H H H H O C(?O)(4-Cl)Ph H 4-Me,2-OMe O A-5905 H H H H H O C(?O)(4-Cl)Ph H 2,5-OMe.sub.2 O A-5906 H H H H H O C(?O)(4-Cl)Ph H 2,6-OMe.sub.2 O A-5907 H H H H H O C(?O)(4-Cl)Ph H 2-OMe,6-CF.sub.3 O A-5908 H H H H H O C(?O)(4-Cl)Ph H 2-CHF.sub.2,5-F O A-5909 H H H H H O C(?O)(4-Cl)Ph H 2-CHF.sub.2,6-F O A-5910 H H H H H O C(?O)(4-Cl)Ph H 2-CHF.sub.2,5-Me O A-5911 H H H H H O C(?O)(4-Cl)Ph H 2-CHF.sub.2,6-Me O A-5912 H H H H H O C(?O)(4-Cl)Ph H 2-cyclopropyl,5-F O A-5913 H H H H H O C(?O)(4-Cl)Ph H 2-cyclopropyl,6-F O A-5914 H H H H H O C(?O)(4-Cl)Ph H 2-cyclopropyl,5-Me O A-5915 H H H H H O C(?O)(4-Cl)Ph H 2-cyclopropyl,6-Me O A-5916 H H H H H O C(?O)(4-Cl)Ph H 2-ethenyl,6-F O A-5917 H H H H H O C(?O)(4-Cl)Ph H 2-ethenyl,6-Me O A-5918 H H H H H O C(?O)(4-Cl)Ph H 2-OEt,5-F O A-5919 H H H H H O C(?O)(4-Cl)Ph H 2-OEt,6-F O A-5920 H H H H H O C(?O)(4-Cl)Ph H 2-OEt,5-Cl O A-5921 H H H H H O C(?O)(4-Cl)Ph H 2-OEt,6-Cl O A-5922 H H H H H O C(?O)(4-Cl)Ph H 2-OEt,5-Me O A-5923 H H H H H O C(?O)(4-Cl)Ph H 2-OEt,6-Me O
(206) TABLE-US-00105 TABLE 105 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5924 H H H H H O C(?O)(4-Cl)Ph H 2-OCHF.sub.2,5-F O A-5925 H H H H H O C(?O)(4-Cl)Ph H 2-OCHF.sub.2,6-F O A-5926 H H H H H O C(?O)(4-Cl)Ph H 2-OCHF.sub.2,5-Me O A-5927 H H H H H O C(?O)(4-Cl)Ph H 2-OCHF.sub.2,6-Me O A-5928 H H H H H O C(?O)(4-Cl)Ph H 2-(cyclopropyloxy),5-F O A-5929 H H H H H O C(?O)(4-Cl)Ph H 2-(cyclopropyloxy),6-F O A-5930 H H H H H O C(?O)(4-Cl)Ph H 2-(cyclopropyloxy),5-Me O A-5931 H H H H H O C(?O)(4-Cl)Ph H 2-(cyclopropyloxy),6-Me O A-5932 H H H H H O C(?O)(4-Cl)Ph H 2-SMe,5-F O A-5933 H H H H H O C(?O)(4-Cl)Ph H 2-SMe,6-F O A-5934 H H H H H O C(?O)(4-Cl)Ph H 2-SMe,5-Me O A-5935 H H H H H O C(?O)(4-Cl)Ph H 2-SMe,6-Me O A-5936 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O)Me,5-F O A-5937 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O)Me,6-F O A-5938 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O)Me,5-Me O A-5939 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O)Me,6-Me O A-5940 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O).sub.2Me,5-F O A-5941 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O).sub.2Me,6-F O A-5942 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O).sub.2Me,5-Me O A-5943 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O).sub.2Me,6-Me O A-5944 H H H H H O C(?O)(4-Cl)Ph H 2-SCF.sub.3,5-F O A-5945 H H H H H O C(?O)(4-Cl)Ph H 2-SCF.sub.3,6-F O A-5946 H H H H H O C(?O)(4-Cl)Ph H 2-SCF.sub.3,5-Me O A-5947 H H H H H O C(?O)(4-Cl)Ph H 2-SCF.sub.3,6-Me O A-5948 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O)CF.sub.3,5-F O A-5949 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O)CF.sub.3,6-F O A-5950 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O)CF.sub.3,5-Me O A-5951 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O)CF3,6-Me O A-5952 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O).sub.2CF.sub.3,5-F O A-5953 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O).sub.2CF.sub.3,6-F O A-5954 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O).sub.2CF.sub.3,5-Me O A-5955 H H H H H O C(?O)(4-Cl)Ph H 2-S(?O).sub.2CF.sub.3,6-Me O A-5956 H H H H H O C(?O)(4-Cl)Ph H 2-(cyclopropylthio),5-F O A-5957 H H H H H O C(?O)(4-Cl)Ph H 2-(cyclopropylthio),6-F O A-5958 H H H H H O C(?O)(4-Cl)Ph H 2-(cyclopropylthio),5-Me O A-5959 H H H H H O C(?O)(4-Cl)Ph H 2-(cyclopropylthio),6-Me O A-5960 H H H H H O C(?O)(4-Cl)Ph H 2-C(?O)Me,5-F O A-5961 H H H H H O C(?O)(4-Cl)Ph H 2-C(?O)Me,6-F O A-5962 H H H H H O C(?O)(4-Cl)Ph H 2-C(?O)Me,5-Me O A-5963 H H H H H O C(?O)(4-Cl)Ph H 2-C(?O)Me,6-Me O A-5964 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2OH,5-F O A-5965 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2OH,6-F O A-5966 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2OH,5-Me O A-5967 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2OH,6-Me O A-5968 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2OCH.sub.3,4-F O A-5969 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2OCH.sub.3,5-F O A-5970 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2OCH.sub.3,6-F O A-5971 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2OCH.sub.3,4-Me O A-5972 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2OCH.sub.3,5-Me O A-5973 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2OCH.sub.3,6-Me O A-5974 H H H H H O C(?O)(4-Cl)Ph H 2-OC(?O)CH.sub.3,5-F O A-5975 H H H H H O C(?O)(4-Cl)Ph H 2-OC(?O)CH.sub.3,6-F O A-5976 H H H H H O C(?O)(4-Cl)Ph H 2-OC(?O)CH.sub.3,5-Me O A-5977 H H H H H O C(?O)(4-Cl)Ph H 2-OC(?O)CH.sub.3,6-Me O A-5978 H H H H H O C(?O)(4-Cl)Ph H 2-OS(?O).sub.2CH.sub.3,5-F O A-5979 H H H H H O C(?O)(4-Cl)Ph H 2-OS(?O).sub.2CH.sub.3,6-F O A-5980 H H H H H O C(?O)(4-Cl)Ph H 2-OS(?O).sub.2CH.sub.3,5-Me O
(207) TABLE-US-00106 TABLE 106 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-5981 H H H H H O C(?O)(4-Cl)Ph H 2-OS(?O)2CH.sub.3,6-Me O A-5982 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2SCH.sub.3,5-F O A-5983 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2SCH.sub.3,6-F O A-5984 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2SCH O A-5985 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2SCH.sub.3,6-Me O A-5986 H H H H H O C(?O)(4-Cl)Ph H 2-NMe.sub.2,5-F O A-5987 H H H H H O C(?O)(4-Cl)Ph H 2-NMe.sub.2,6-F O A-5988 H H H H H O C(?O)(4-Cl)Ph H 2-NMe.sub.2,5-Me O A-5989 H H H H H O C(?O)(4-Cl)Ph H 2-NMe.sub.2,6-Me O A-5990 H H H H H O C(?O)(4-Cl)Ph H 2-CN,4-F O A-5991 H H H H H O C(?O)(4-Cl)Ph H 2-CN,5-F O A-5992 H H H H H O C(?O)(4-Cl)Ph H 2-CN,6-F O A-5993 H H H H H O C(?O)(4-Cl)Ph H 2-CN,6-Me O A-5994 H H H H H O C(?O)(4-Cl)Ph H 2-CN,5-OMe O A-5995 H H H H H O C(?O)(4-Cl)Ph H 2-CN,6-OMe O A-5996 H H H H H O C(?O)(4-Cl)Ph H 3-CN,6-Me O A-5997 H H H H H O C(?O)(4-Cl)Ph H 3-CN,6-OMe O A-5998 H H H H H O C(?O)(4-Cl)Ph H 4-CN,2-Me O A-5999 H H H H H O C(?O)(4-Cl)Ph H 4-CN,2-OMe O A-6000 H H H H H O C(?O)(4-Cl)Ph H 2-NO.sub.2,4-F O A-6001 H H H H H O C(?O)(4-Cl)Ph H 2-NO.sub.2,5-F O A-6002 H H H H H O C(?O)(4-Cl)Ph H 2-NO.sub.2,6-F O A-6003 H H H H H O C(?O)(4-Cl)Ph H 2-NO.sub.2,4-Me O A-6004 H H H H H O C(?O)(4-Cl)Ph H 2-NO.sub.2,5-Me O A-6005 H H H H H O C(?O)(4-Cl)Ph H 2-NO.sub.2,6-Me O A-6006 H H H H H O C(?O)(4-Cl)Ph H 2-Me,4,5-F.sub.2 O A-6007 H H H H H O C(?O)(4-Cl)Ph H 2-Me,6-Et O A-6008 H H H H H O C(?O)(4-Cl)Ph H 2-cyclopropyl,6-OMe O A-6009 H H H H H O C(?O)(4-Cl)Ph H 2-Me,5-Et O A-6010 H H H H H O C(?O)(4-Cl)Ph H 2,6-Et.sub.2 O A-6011 H H H H H O C(?O)(4-Cl)Ph H 2-Et,6-F O A-6012 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2OCH.sub.3,6-Cl O A-6013 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl O A-6014 H H H H H O C(?O)(4-Cl)Ph H 2-CH.sub.2NMe.sub.2 O A-6015 H H H H H O C(?S)OCH.sub.3 H H O A-6016 H H H H H O C(?S)OCH.sub.3 H 2-F O A-6017 H H H H H O C(?S)OCH.sub.3 H 2-Cl O A-6018 H H H H H O C(?S)OCH.sub.3 H 2-Br O A-6019 H H H H H O C(?S)OCH.sub.3 H 2-OH O A-6020 H H H H H O C(?S)OCH.sub.3 H 2-Me O A-6021 H H H H H O C(?S)OCH.sub.3 H 2-Et O A-6022 H H H H H O C(?S)OCH.sub.3 H 2-Pr O A-6023 H H H H H O C(?S)OCH.sub.3 H 2-CF.sub.3 O A-6024 H H H H H O C(?S)OCH.sub.3 H 2-CHF.sub.2 O A-6025 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2F O A-6026 H H H H H O C(?S)OCH.sub.3 H 2-CF.sub.2Cl O A-6027 H H H H H O C(?S)OCH.sub.3 H 2-cyclopropyl O A-6028 H H H H H O C(?S)OCH.sub.3 H 2-cyclobutyl O A-6029 H H H H H O C(?S)OCH.sub.3 H 2-cyclopentyl O A-6030 H H H H H O C(?S)OCH.sub.3 H 2-ethenyl O A-6031 H H H H H O C(?S)OCH.sub.3 H 2-allyl O A-6032 H H H H H O C(?S)OCH.sub.3 H 2-(prop-1-en-1-yl) O A-6033 H H H H H O C(?S)OCH.sub.3 H 2-(trifluoroethenyl) O A-6034 H H H H H O C(?S)OCH.sub.3 H 2-OMe O A-6035 H H H H H O C(?S)OCH.sub.3 H 2-OEt O A-6036 H H H H H O C(?S)OCH.sub.3 H 2-OPr O A-6037 H H H H H O C(?S)OCH.sub.3 H 2-O(i-Pr) O
(208) TABLE-US-00107 TABLE 107 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6038 H H H H H O C(?S)OCH.sub.3 H 2-OCF.sub.3 O A-6039 H H H H H O C(?S)OCH.sub.3 H 2-OCHF.sub.2 O A-6040 H H H H H O C(?S)OCH.sub.3 H 2-(cyclopropyloxy) O A-6041 H H H H H O C(?S)OCH.sub.3 H 2-(cyclobutyloxy) O A-6042 H H H H H O C(?S)OCH.sub.3 H 2-(cyclopentyloxy) O A-6043 H H H H H O C(?S)OCH.sub.3 H 2-((2,2-dichlorocyclopropyl)oxy) O A-6044 H H H H H O C(?S)OCH.sub.3 H 2-(oxiran-2-yl) O A-6045 H H H H H O C(?S)OCH.sub.3 H 2-SMe O A-6046 H H H H H O C(?S)OCH.sub.3 H 3-SMe O A-6047 H H H H H O C(?S)OCH.sub.3 H 2-S(?O)Me O A-6048 H H H H H O C(?S)OCH.sub.3 H 3-S(?O)Me O A-6049 H H H H H O C(?S)OCH.sub.3 H 2-S(?O).sub.2Me O A-6050 H H H H H O C(?S)OCH.sub.3 H 3-S(?O).sub.2Me O A-6051 H H H H H O C(?S)OCH.sub.3 H 2-SCF.sub.3 O A-6052 H H H H H O C(?S)OCH.sub.3 H 3-SCF.sub.3 O A-6053 H H H H H O C(?S)OCH.sub.3 H 3-S(?O)CF.sub.3 O A-6054 H H H H H O C(?S)OCH.sub.3 H 3-SCF(CF.sub.3).sub.2 O A-6055 H H H H H O C(?S)OCH.sub.3 H 2-(cyclopropylthio) O A-6056 H H H H H O C(?S)OCH.sub.3 H 2-(cyclopropylsulfinyl) O A-6057 H H H H H O C(?S)OCH.sub.3 H 2-(cyclopropylsulfonyl) O A-6058 H H H H H O C(?S)OCH.sub.3 H 2-C(?O)Me O A-6059 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2C(?O)CH.sub.3 O A-6060 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2C(?O)CF.sub.3 O A-6061 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2OH O A-6062 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2OCH.sub.3 O A-6063 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3 O A-6064 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2SCH.sub.3 O A-6065 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2S(?O)CH.sub.3 O A-6066 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2S(?O).sub.2CH.sub.3 O A-6067 H H H H H O C(?S)OCH.sub.3 H 2-(benzyloxy) O A-6068 H H H H H O C(?S)OCH.sub.3 H 2-NH.sub.2 O A-6069 H H H H H O C(?S)OCH.sub.3 H 2-NHMe O A-6070 H H H H H O C(?S)OCH.sub.3 H 2-N(Me).sub.2 O A-6071 H H H H H O C(?S)OCH.sub.3 H 2-(1,3-dioxolan-2-yl) O A-6072 H H H H H O C(?S)OCH.sub.3 H 2-(1,3-dioxan-2-yl) O A-6073 H H H H H O C(?S)OCH.sub.3 H 2-(1H-imidazol-2-yl) O A-6074 H H H H H O C(?S)OCH.sub.3 H 2-(thiazol-2-yl) O A-6075 H H H H H O C(?S)OCH.sub.3 H 2-(oxazol-2-yl) O A-6076 H H H H H O C(?S)OCH.sub.3 H 2-CH?NOH O A-6077 H H H H H O C(?S)OCH.sub.3 H 2-CH?NOMe O A-6078 H H H H H O C(?S)OCH.sub.3 H 2-(4,5-dihydro-3-isoxazolyl) O A-6079 H H H H H O C(?S)OCH.sub.3 H 2-CN O A-6080 H H H H H O C(?S)OCH.sub.3 H 2-NO.sub.2 O A-6081 H H H H H O C(?S)OCH.sub.3 H 2-F,6-Cl O A-6082 H H H H H O C(?S)OCH.sub.3 H 2-F,6-Me O A-6083 H H H H H O C(?S)OCH.sub.3 H 3-F,6-Me O A-6084 H H H H H O C(?S)OCH.sub.3 H 4-F,2-Me O A-6085 H H H H H O C(?S)OCH.sub.3 H 2-F,6-OMe O A-6086 H H H H H O C(?S)OCH.sub.3 H 3-F,6-OMe O A-6087 H H H H H O C(?S)OCH.sub.3 H 2,6-Cl.sub.2 O A-6088 H H H H H O C(?S)OCH.sub.3 H 2-Cl,6-Me O A-6089 H H H H H O C(?S)OCH.sub.3 H 3-Cl,6-Me O A-6090 H H H H H O C(?S)OCH.sub.3 H 4-Cl,2-Me O A-6091 H H H H H O C(?S)OCH.sub.3 H 2-Cl,5-CF.sub.3 O A-6092 H H H H H O C(?S)OCH.sub.3 H 2-Cl,6-CF.sub.3 O A-6093 H H H H H O C(?S)OCH.sub.3 H 2-Cl,6-OMe O A-6094 H H H H H O C(?S)OCH.sub.3 H 3-Cl,6-OMe O
(209) TABLE-US-00108 TABLE 108 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6095 H H H H H O C(?S)OCH.sub.3 H 4-Cl,2-OMe 0 A-6096 H H H H H O C(?S)OCH.sub.3 H 2,4-Me.sub.2 0 A-6097 H H H H H O C(?S)OCH.sub.3 H 2,5-Me.sub.2 0 A-6098 H H H H H O C(?S)OCH.sub.3 H 2,6-Me.sub.2 0 A-6099 H H H H H O C(?S)OCH.sub.3 H 2-Me,4-CF.sub.3 0 A-6100 H H H H H O C(?S)OCH.sub.3 H 2-Me,5-CF.sub.3 0 A-6101 H H H H H O C(?S)OCH.sub.3 H 2-Me,6-CF.sub.3 0 A-6102 H H H H H O C(?S)OCH.sub.3 H 2-Me,4-OMe 0 A-6103 H H H H H O C(?S)OCH.sub.3 H 2-Me,5-OMe 0 A-6104 H H H H H O C(?S)OCH.sub.3 H 2-Me,6-OMe 0 A-6105 H H H H H O C(?S)OCH.sub.3 H 3-Me,6-OMe 0 A-6106 H H H H H O C(?S)OCH.sub.3 H 4-Me,2-OMe 0 A-6107 H H H H H O C(?S)OCH.sub.3 H 2,5-OMe.sub.2 0 A-6108 H H H H H O C(?S)OCH.sub.3 H 2,6-OMe.sub.2 0 A-6109 H H H H H O C(?S)OCH.sub.3 H 2-OMe,6-CF.sub.3 0 A-6110 H H H H H O C(?S)OCH.sub.3 H 2-CHF.sub.2,5-F 0 A-6111 H H H H H O C(?S)OCH.sub.3 H 2-CHF.sub.2,6-F 0 A-6112 H H H H H O C(?S)OCH.sub.3 H 2-CHF.sub.2,5-Me 0 A-6113 H H H H H O C(?S)OCH.sub.3 H 2-CHF.sub.2,6-Me 0 A-6114 H H H H H O C(?S)OCH.sub.3 H 2-cyclopropyl,5-F 0 A-6115 H H H H H O C(?S)OCH.sub.3 H 2-cyclopropyl,6-F 0 A-6116 H H H H H O C(?S)OCH.sub.3 H 2-cyclopropyl,5-Me 0 A-6117 H H H H H O C(?S)OCH.sub.3 H 2-cyclopropyl,6-Me 0 A-6118 H H H H H O C(?S)OCH.sub.3 H 2-ethenyl,6-F 0 A-6119 H H H H H O C(?S)OCH.sub.3 H 2-ethenyl,6-Me 0 A-6120 H H H H H O C(?S)OCH.sub.3 H 2-OEt,5-F 0 A-6121 H H H H H O C(?S)OCH.sub.3 H 2-OEt,6-F 0 A-6122 H H H H H O C(?S)OCH.sub.3 H 2-OEt,5-Cl 0 A-6123 H H H H H O C(?S)OCH.sub.3 H 2-OEt,6-Cl 0 A-6124 H H H H H O C(?S)OCH.sub.3 H 2-OEt,5-Me 0 A-6125 H H H H H O C(?S)OCH.sub.3 H 2-OEt,6-Me 0 A-6126 H H H H H O C(?S)OCH.sub.3 H 2-OCHF.sub.2,5-F 0 A-6127 H H H H H O C(?S)OCH.sub.3 H 2-OCHF.sub.2,6-F 0 A-6128 H H H H H O C(?S)OCH.sub.3 H 2-OCHF.sub.2,5-Me 0 A-6129 H H H H H O C(?S)OCH.sub.3 H 2-OCHF.sub.2,6-Me 0 A-6130 H H H H H O C(?S)OCH.sub.3 H 2-(cyclopropyloxy),5-F 0 A-6131 H H H H H O C(?S)OCH.sub.3 H 2-(cyclopropyloxy),6-F 0 A-6132 H H H H H O C(?S)OCH.sub.3 H 2-(cyclopropyloxy),5-Me 0 A-6133 H H H H H O C(?S)OCH.sub.3 H 2-(cyclopropyloxy),6-Me 0 A-6134 H H H H H O C(?S)OCH.sub.3 H 2-SMe,5-F 0 A-6135 H H H H H O C(?S)OCH.sub.3 H 2-SMe,6-F 0 A-6136 H H H H H O C(?S)OCH.sub.3 H 2-SMe,5-Me 0 A-6137 H H H H H O C(?S)OCH.sub.3 H 2-SMe,6-Me 0 A-6138 H H H H H O C(?S)OCH.sub.3 H 2-S(?O)Me,5-F 0 A-6139 H H H H H O C(?S)OCH.sub.3 H 2-S(?O)Me,6-F 0 A-6140 H H H H H O C(?S)OCH.sub.3 H 2-S(?O)Me,5-Me 0 A-6141 H H H H H O C(?S)OCH.sub.3 H 2-S(?O)Me,6-Me 0 A-6142 H H H H H O C(?S)OCH.sub.3 H 2-S(?O).sub.2Me,5-F 0 A-6143 H H H H H O C(?S)OCH.sub.3 H 2-S(?O).sub.2Me,6-F 0 A-6144 H H H H H O C(?S)OCH.sub.3 H 2-S(?O).sub.2Me,5-Me 0 A-6145 H H H H H O C(?S)OCH.sub.3 H 2-S(?O).sub.2Me,6-Me 0 A-6146 H H H H H O C(?S)OCH.sub.3 H 2-SCF.sub.3,5-F 0 A-6147 H H H H H O C(?S)OCH.sub.3 H 2-SCF.sub.3,6-F 0 A-6148 H H H H H O C(?S)OCH.sub.3 H 2-SCF.sub.3,5-Me 0 A-6149 H H H H H O C(?S)OCH.sub.3 H 2-SCF.sub.3,6-Me 0 A-6150 H H H H H O C(?S)OCH.sub.3 H 2-S(?O)CF.sub.3,5-F 0 A-6151 H H H H H O C(?S)OCH.sub.3 H 2-S(?O)CF.sub.3,6-F 0
(210) TABLE-US-00109 TABLE 109 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6152 H H H H H O C(?S)OCH.sub.3 H 2-S(?O)CF.sub.3,5-Me 0 A-6153 H H H H H O C(?S)OCH.sub.3 H 2-S(?O)CF.sub.3,6-Me 0 A-6154 H H H H H O C(?S)OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-6155 H H H H H O C(?S)OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-6156 H H H H H O C(?S)OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-6157 H H H H H O C(?S)OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-6158 H H H H H O C(?S)OCH.sub.3 H 2-(cyclopropylthio),5-F 0 A-6159 H H H H H O C(?S)OCH.sub.3 H 2-(cyclopropylthio),6-F 0 A-6160 H H H H H O C(?S)OCH.sub.3 H 2-(cyclopropylthio),5-Me 0 A-6161 H H H H H O C(?S)OCH.sub.3 H 2-(cyclopropylthio),6-Me 0 A-6162 H H H H H O C(?S)OCH.sub.3 H 2-C(?O)Me,5-F 0 A-6163 H H H H H O C(?S)OCH.sub.3 H 2-C(?O)Me,6-F 0 A-6164 H H H H H O C(?S)OCH.sub.3 H 2-C(?O)Me,5-Me 0 A-6165 H H H H H O C(?S)OCH.sub.3 H 2-C(?O)Me,6-Me 0 A-6166 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2OH,5-F 0 A-6167 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2OH,6-F 0 A-6168 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2OH,5-Me 0 A-6169 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2OH,6-Me 0 A-6170 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,4-F 0 A-6171 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,5-F 0 A-6172 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,6-F 0 A-6173 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-6174 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-6175 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-6176 H H H H H O C(?S)OCH.sub.3 H 2-OC(?O)CH.sub.3,5-F 0 A-6177 H H H H H O C(?S)OCH.sub.3 H 2-OC(?O)CH.sub.3,6-F 0 A-6178 H H H H H O C(?S)OCH.sub.3 H 2-OC(?O)CH.sub.3,5-Me 0 A-6179 H H H H H O C(?S)OCH.sub.3 H 2-OC(?O)CH.sub.3,6-Me 0 A-6180 H H H H H O C(?S)OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-6181 H H H H H O C(?S)OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-6182 H H H H H O C(?S)OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-6183 H H H H H O C(?S)OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-6184 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2SCH.sub.3,5-F 0 A-6185 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2SCH.sub.3,6-F 0 A-6186 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2SCH.sub.3,5-Me 0 A-6187 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2SCH.sub.3,6-Me 0 A-6188 H H H H H O C(?S)OCH.sub.3 H 2-NMe.sub.2,5-F 0 A-6189 H H H H H O C(?S)OCH.sub.3 H 2-NMe.sub.2,6-F 0 A-6190 H H H H H O C(?S)OCH.sub.3 H 2-NMe.sub.2,5-Me 0 A-6191 H H H H H O C(?S)OCH.sub.3 H 2-NMe.sub.2,6-Me 0 A-6192 H H H H H O C(?S)OCH.sub.3 H 2-CN,4-F 0 A-6193 H H H H H O C(?S)OCH.sub.3 H 2-CN,5-F 0 A-6194 H H H H H O C(?S)OCH.sub.3 H 2-CN,6-F 0 A-6195 H H H H H O C(?S)OCH.sub.3 H 2-CN,6-Me 0 A-6196 H H H H H O C(?S)OCH.sub.3 H 2-CN,5-OMe 0 A-6197 H H H H H O C(?S)OCH.sub.3 H 2-CN,6-OMe 0 A-6198 H H H H H O C(?S)OCH.sub.3 H 3-CN,6-Me 0 A-6199 H H H H H O C(?S)OCH.sub.3 H 3-CN,6-OMe 0 A-6200 H H H H H O C(?S)OCH.sub.3 H 4-CN,2-Me 0 A-6201 H H H H H O C(?S)OCH.sub.3 H 4-CN,2-OMe 0 A-6202 H H H H H O C(?S)OCH.sub.3 H 2-NO.sub.2,4-F 0 A-6203 H H H H H O C(?S)OCH.sub.3 H 2-NO.sub.2,5-F 0 A-6204 H H H H H O C(?S)OCH.sub.3 H 2-NO.sub.2,6-F 0 A-6205 H H H H H O C(?S)OCH.sub.3 H 2-NO.sub.2,4-Me 0 A-6206 H H H H H O C(?S)OCH.sub.3 H 2-NO.sub.2,5-Me 0 A-6207 H H H H H O C(?S)OCH.sub.3 H 2-NO.sub.2,6-Me 0 A-6208 H H H H H O C(?S)OCH.sub.3 H 2-Me,4,5-F.sub.2 0
(211) TABLE-US-00110 TABLE 110 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6209 H H H H H O C(?S)OCH.sub.3 H 2-Me,6-Et 0 A-6210 H H H H H O C(?S)OCH.sub.3 H 2-cyclopropyl,6-OMe 0 A-6211 H H H H H O C(?S)OCH.sub.3 H 2-Me,5-Et 0 A-6212 H H H H H O C(?S)OCH.sub.3 H 2,6-Et.sub.2 0 A-6213 H H H H H O C(?S)OCH.sub.3 H 2-Et,6-F 0 A-6214 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-6215 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-6216 H H H H H O C(?S)OCH.sub.3 H 2-CH.sub.2NMe.sub.2 0 A-6217 H H H H H O C(?S)N(CH.sub.3).sub.2 H H 0 A-6218 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-F 0 A-6219 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Cl 0 A-6220 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Br 0 A-6221 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OH 0 A-6222 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Me 0 A-6223 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Et 0 A-6224 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Pr 0 A-6225 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CF.sub.3 0 A-6226 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CHF.sub.2 0 A-6227 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2F 0 A-6228 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CF.sub.2Cl 0 A-6229 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-cyclopropyl 0 A-6230 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-cyclobutyl 0 A-6231 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-cyclopentyl 0 A-6232 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-ethenyl 0 A-6233 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-allyl 0 A-6234 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(prop-1-en-1-y) 0 A-6235 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(trifluoroethenyl) 0 A-6236 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OMe 0 A-6237 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OEt 0 A-6238 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OPr 0 A-6239 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-O(i-Pr) 0 A-6240 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OCF.sub.3 0 A-6241 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OCHF.sub.2 0 A-6242 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(cyclopropyloxy) 0 A-6243 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(cyclobutyloxy) 0 A-6244 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(cyclopentyloxy) 0 A-6245 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-6246 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(oxiran-2-yl) 0 A-6247 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-SMe 0 A-6248 H H H H H O C(?S)N(CH.sub.3).sub.2 H 3-SMe 0 A-6249 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O)Me 0 A-6250 H H H H H O C(?S)N(CH.sub.3).sub.2 H 3-S(?O)Me 0 A-6251 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me 0 A-6252 H H H H H O C(?S)N(CH.sub.3).sub.2 H 3-S(?O).sub.2Me 0 A-6253 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-SCF.sub.3 0 A-6254 H H H H H O C(?S)N(CH.sub.3).sub.2 H 3-SCF.sub.3 0 A-6255 H H H H H O C(?S)N(CH.sub.3).sub.2 H 3-S(?O)CF.sub.3 0 A-6256 H H H H H O C(?S)N(CH.sub.3).sub.2 H 3-SCF(CF.sub.3).sub.2 0 A-6257 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(cyclopropylthio) 0 A-6258 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(cyclopropylsulfinyl) 0 A-6259 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(cyclopropylsulfonyl) 0 A-6260 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-C(?O)Me 0 A-6261 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2C(?O)CH.sub.3 0 A-6262 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2C(?O)CF.sub.3 0 A-6263 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2OH 0 A-6264 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3 0 A-6265 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.2CH.sub.3 0
(212) TABLE-US-00111 TABLE 111 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6266 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3 0 A-6267 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2S(?0)CH.sub.3 0 A-6268 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2S(?0).sub.2CH.sub.3 0 A-6269 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(benzyloxy) 0 A-6270 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-NH.sub.2 0 A-6271 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-NHMe 0 A-6272 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-N(Me).sub.2 0 A-6273 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(1,3-dioxolan-2-yl) 0 A-6274 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(1,3-dioxan-2-yl) 0 A-6275 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(1H-imidazol-2-yl) 0 A-6276 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(thiazol-2-yl) 0 A-6277 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(oxazol-2-yl) 0 A-6278 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH?NOH 0 A-6279 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH?NOMe 0 A-6280 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-6281 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CN 0 A-6282 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-NO.sub.2 0 A-6283 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-F,6-Cl 0 A-6284 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-F,6-Me 0 A-6285 H H H H H O C(?S)N(CH.sub.3).sub.2 H 3-F,6-Me 0 A-6286 H H H H H O C(?S)N(CH.sub.3).sub.2 H 4-F,2-Me 0 A-6287 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-F,6-OMe 0 A-6288 H H H H H O C(?S)N(CH.sub.3).sub.2 H 3-F,6-OMe 0 A-6289 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2,6-Cl.sub.2 0 A-6290 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Cl,6-Me 0 A-6291 H H H H H O C(?S)N(CH.sub.3).sub.2 H 3-Cl,6-Me 0 A-6292 H H H H H O C(?S)N(CH.sub.3).sub.2 H 4-Cl,2-Me 0 A-6293 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Cl,5-CF.sub.3 0 A-6294 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Cl,6-CF.sub.3 0 A-6295 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Cl,6-OMe 0 A-6296 H H H H H O C(?S)N(CH.sub.3).sub.2 H 3-Cl,6-OMe 0 A-6297 H H H H H O C(?S)N(CH.sub.3).sub.2 H 4-Cl,2-OMe 0 A-6298 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2,4-Me.sub.2 0 A-6299 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2,5-Me.sub.2 0 A-6300 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2,6-Me.sub.2 0 A-6301 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Me,4-CF.sub.3 0 A-6302 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Me,5-CF.sub.3 0 A-6303 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Me,6-CF.sub.3 0 A-6304 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Me,4-OMe 0 A-6305 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Me,5-OMe 0 A-6306 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Me,6-OMe 0 A-6307 H H H H H O C(?S)N(CH.sub.3).sub.2 H 3-Me,6-OMe 0 A-6308 H H H H H O C(?S)N(CH.sub.3).sub.2 H 4-Me,2-OMe 0 A-6309 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2,5-OMe.sub.2 0 A-6310 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2,6-OMe.sub.2 0 A-6311 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OMe,6-CF.sub.3 0 A-6312 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CHF.sub.2,5-F 0 A-6313 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CHF.sub.2,6-F 0 A-6314 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CHF.sub.2,5-Me 0 A-6315 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CHF.sub.2,6-Me 0 A-6316 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-cyclopropyl,5-F 0 A-6317 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-cyclopropyl,6-F 0 A-6318 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-cyclopropyl,5-Me 0 A-6319 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-cyclopropyl,6-Me 0 A-6320 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-ethenyl,6-F 0 A-6321 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-ethenyl,6-Me 0 A-6322 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OEt,5-F 0
(213) TABLE-US-00112 TABLE 112 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6323 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OEt,6-F 0 A-6324 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OEt,5-Cl 0 A-6325 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OEt,6-Cl 0 A-6326 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OEt,5-Me 0 A-6327 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OEt,6-Me 0 A-6328 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OCHF.sub.2,5-F 0 A-6329 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OCHF.sub.2,6-F 0 A-6330 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OCHF.sub.2,5-Me 0 A-6331 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OCHF.sub.2,6-Me 0 A-6332 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),5-F 0 A-6333 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),6-F 0 A-6334 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),5-Me 0 A-6335 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),6-Me 0 A-6336 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-SMe,5-F 0 A-6337 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-SMe,6-F 0 A-6338 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-SMe,5-Me 0 A-6339 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-SMe,6-Me 0 A-6340 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O)Me,5-F 0 A-6341 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O)Me,6-F 0 A-6342 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O)Me,5-Me 0 A-6343 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O)Me,6-Me 0 A-6344 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,5-F 0 A-6345 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,6-F 0 A-6346 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,5-Me 0 A-6347 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,6-Me 0 A-6348 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-SCF.sub.3,5-F 0 A-6349 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-SCF.sub.3,6-F 0 A-6350 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-SCF.sub.3,5-Me 0 A-6351 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-SCF.sub.3,6-Me 0 A-6352 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,5-F 0 A-6353 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,6-F 0 A-6354 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,5-Me 0 A-6355 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,6-Me 0 A-6356 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-6357 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-6358 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-6359 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-6360 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(cyclopropylthio),5-F 0 A-6361 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(cyclopropylthio),6-F 0 A-6362 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(cyclopropylthio),5-Me 0 A-6363 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-(cyclopropylthio),6-Me 0 A-6364 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-C(?O)Me,5-F 0 A-6365 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-C(?O)Me,6-F 0 A-6366 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-C(?O)Me,5-Me 0 A-6367 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-C(?O)Me,6-Me 0 A-6368 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2OH,5-F 0 A-6369 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2OH,6-F 0 A-6370 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2OH,5-Me 0 A-6371 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2OH,6-Me 0 A-6372 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,4-F 0 A-6373 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,5-F 0 A-6374 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,6-F 0 A-6375 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-6376 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-6377 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-6378 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,5-F 0 A-6379 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,6-F 0
(214) TABLE-US-00113 TABLE 113 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6380 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,5-Me 0 A-6381 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,6-Me 0 A-6382 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-6383 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-6384 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-6385 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-6386 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,5-F 0 A-6387 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,6-F 0 A-6388 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,5-Me 0 A-6389 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,6-Me 0 A-6390 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-NMe.sub.2,5-F 0 A-6391 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-NMe.sub.2,6-F 0 A-6392 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-NMe.sub.2,5-Me 0 A-6393 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-NMe.sub.2,6-Me 0 A-6394 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CN,4-F 0 A-6395 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CN,5-F 0 A-6396 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CN,6-F 0 A-6397 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CN,6-Me 0 A-6398 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CN,5-OMe 0 A-6399 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CN,6-OMe 0 A-6400 H H H H H O C(?S)N(CH.sub.3).sub.2 H 3-CN,6-Me 0 A-6401 H H H H H O C(?S)N(CH.sub.3).sub.2 H 3-CN,6-OMe 0 A-6402 H H H H H O C(?S)N(CH.sub.3).sub.2 H 4-CN,2-Me 0 A-6403 H H H H H O C(?S)N(CH.sub.3).sub.2 H 4-CN,2-OMe 0 A-6404 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-NO.sub.2,4-F 0 A-6405 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-NO.sub.2,5-F 0 A-6406 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-NO.sub.2,6-F 0 A-6407 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-NO.sub.2,4-Me 0 A-6408 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-NO.sub.2,5-Me 0 A-6409 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-NO.sub.2,6-Me 0 A-6410 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Me,4,5-F.sub.2 0 A-6411 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Me,6-Et 0 A-6412 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-cyclopropyl,6-OMe 0 A-6413 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Me,5-Et 0 A-6414 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2,6-Et.sub.2 0 A-6415 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-Et,6-F 0 A-6416 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-6417 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-6418 H H H H H O C(?S)N(CH.sub.3).sub.2 H 2-CH.sub.2NMe.sub.2 0 A-6419 H H H H H O S(?O).sub.2CH.sub.3 H H 0 A-6420 H H H H H O S(?O).sub.2CH.sub.3 H 2-F 0 A-6421 H H H H H O S(?O).sub.2CH.sub.3 H 2-Cl 0 A-6422 H H H H H O S(?O).sub.2CH.sub.3 H 2-Br 0 A-6423 H H H H H O S(?O).sub.2CH.sub.3 H 2-OH 0 A-6424 H H H H H O S(?O).sub.2CH.sub.3 H 2-Me 0 A-6425 H H H H H O S(?O).sub.2CH.sub.3 H 2-Et 0 A-6426 H H H H H O S(?O).sub.2CH.sub.3 H 2-Pr 0 A-6427 H H H H H O S(?O).sub.2CH.sub.3 H 2-CF.sub.3 0 A-6428 H H H H H O S(?O).sub.2CH.sub.3 H 2-CHF.sub.2 0 A-6429 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2F 0 A-6430 H H H H H O S(?O).sub.2CH.sub.3 H 2-CF.sub.2C 0 A-6431 H H H H H O S(?O).sub.2CH.sub.3 H 2-cyclopropyl 0 A-6432 H H H H H O S(?O).sub.2CH.sub.3 H 2-cyclobutyl 0 A-6433 H H H H H O S(?O).sub.2CH.sub.3 H 2-cyclopentyl 0 A-6434 H H H H H O S(?O).sub.2CH.sub.3 H 2-ethenyl 0 A-6435 H H H H H O S(?O).sub.2CH.sub.3 H 2-allyl 0 A-6436 H H H H H O S(?O).sub.2CH.sub.3 H 2-(prop-1-en-1-yl) 0
(215) TABLE-US-00114 TABLE 114 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6437 H H H H H O S(?O).sub.2CH.sub.3 H 2-(trifluoroethenyl) 0 A-6438 H H H H H O S(?O).sub.2CH.sub.3 H 2-OMe 0 A-6439 H H H H H O S(?O).sub.2CH.sub.3 H 2-OEt 0 A-6440 H H H H H O S(?O).sub.2CH.sub.3 H 2-OPr 0 A-6441 H H H H H O S(?O).sub.2CH.sub.3 H 2-O(i-Pr) 0 A-6442 H H H H H O S(?O).sub.2CH.sub.3 H 2-OCF.sub.3 0 A-6443 H H H H H O S(?O).sub.2CH.sub.3 H 2-OCHF.sub.2 0 A-6444 H H H H H O S(?O).sub.2CH.sub.3 H 2-(cyclopropyloxy) 0 A-6445 H H H H H O S(?O).sub.2CH.sub.3 H 2-(cyclobutyloxy) 0 A-6446 H H H H H O S(?O).sub.2CH.sub.3 H 2-(cyclopentyloxy) 0 A-6447 H H H H H O S(?O).sub.2CH.sub.3 H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-6448 H H H H H O S(?O).sub.2CH.sub.3 H 2-(oxiran-2-yl) 0 A-6449 H H H H H O S(?O).sub.2CH.sub.3 H 2-SMe 0 A-6450 H H H H H O S(?O).sub.2CH.sub.3 H 3-SMe 0 A-6451 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O)Me 0 A-6452 H H H H H O S(?O).sub.2CH.sub.3 H 3-S(?O)Me 0 A-6453 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O).sub.2Me 0 A-6454 H H H H H O S(?O).sub.2CH.sub.3 H 3-S(?O).sub.2Me 0 A-6455 H H H H H O S(?O).sub.2CH.sub.3 H 2-SCF.sub.3 0 A-6456 H H H H H O S(?O).sub.2CH.sub.3 H 3-SCF.sub.3 0 A-6457 H H H H H O S(?O).sub.2CH.sub.3 H 3-S(?O)CF.sub.3 0 A-6458 H H H H H O S(?O).sub.2CH.sub.3 H 3-SCF(CF.sub.3).sub.2 0 A-6459 H H H H H O S(?O).sub.2CH.sub.3 H 2-(cyclopropylthio) 0 A-6460 H H H H H O S(?O).sub.2CH.sub.3 H 2-(cyclopropylsulfinyl) 0 A-6461 H H H H H O S(?O).sub.2CH.sub.3 H 2-(cyclopropylsulfonyl) 0 A-6462 H H H H H O S(?O).sub.2CH.sub.3 H 2-C(?O)Me 0 A-6463 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2C(?O)CH.sub.3 0 A-6464 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2C(?O)CF.sub.3 0 A-6465 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2OH 0 A-6466 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3 0 A-6467 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-6468 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3 0 A-6469 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2S(?O)CH.sub.3 0 A-6470 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-6471 H H H H H O S(?O).sub.2CH.sub.3 H 2-(benzyloxy) 0 A-6472 H H H H H O S(?O).sub.2CH.sub.3 H 2-NH.sub.2 0 A-6473 H H H H H O S(?O).sub.2CH.sub.3 H 2-NHMe 0 A-6474 H H H H H O S(?O).sub.2CH.sub.3 H 2-N(Me).sub.2 0 A-6475 H H H H H O S(?O).sub.2CH.sub.3 H 2-(1,3-dioxolan-2-yl) 0 A-6476 H H H H H O S(?O).sub.2CH.sub.3 H 2-(1,3-dioxan-2-yl) 0 A-6477 H H H H H O S(?O).sub.2CH.sub.3 H 2-(1,3-imidazol-2-yl) 0 A-6478 H H H H H O S(?O).sub.2CH.sub.3 H 2-(thiazol-2-yl) 0 A-6479 H H H H H O S(?O).sub.2CH.sub.3 H 2-(oxazol-2-yl) 0 A-6480 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH?NOH 0 A-6481 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH?NOMe 0 A-6482 H H H H H O S(?O).sub.2CH.sub.3 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-6483 H H H H H O S(?O).sub.2CH.sub.3 H 2-CN 0 A-6484 H H H H H O S(?O).sub.2CH.sub.3 H 2-NO.sub.2 0 A-6485 H H H H H O S(?O).sub.2CH.sub.3 H 2-F,6-Cl 0 A-6486 H H H H H O S(?O).sub.2CH.sub.3 H 2-F,6-Me 0 A-6487 H H H H H O S(?O).sub.2CH.sub.3 H 3-F,6-Me 0 A-6488 H H H H H O S(?O).sub.2CH.sub.3 H 4-F,2-Me 0 A-6489 H H H H H O S(?O).sub.2CH.sub.3 H 2-F,6-OMe 0 A-6490 H H H H H O S(?O).sub.2CH.sub.3 H 3-F,6-OMe 0 A-6491 H H H H H O S(?O).sub.2CH.sub.3 H 2,6-Cl.sub.2 0 A-6492 H H H H H O S(?O).sub.2CH.sub.3 H 2-Cl,6-Me 0 A-6493 H H H H H O S(?O).sub.2CH.sub.3 H 3-Cl,6-Me 0
(216) TABLE-US-00115 TABLE 115 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6494 H H H H H O S(?O).sub.2CH.sub.3 H 4-Cl,2-Me 0 A-6495 H H H H H O S(?O).sub.2CH.sub.3 H 2-Cl,5-CF.sub.3 0 A-6496 H H H H H O S(?O).sub.2CH.sub.3 H 2-Cl,6-CF.sub.3 0 A-6497 H H H H H O S(?O).sub.2CH.sub.3 H 2-Cl,6-OMe 0 A-6498 H H H H H O S(?O).sub.2CH.sub.3 H 3-Cl,6-OMe 0 A-6499 H H H H H O S(?O).sub.2CH.sub.3 H 4-Cl,2-OMe 0 A-6500 H H H H H O S(?O).sub.2CH.sub.3 H 2,4-Me.sub.2 0 A-6501 H H H H H O S(?O).sub.2CH.sub.3 H 2,5-Me.sub.2 0 A-6502 H H H H H O S(?O).sub.2CH.sub.3 H 2,6-Me.sub.2 0 A-6503 H H H H H O S(?O).sub.2CH.sub.3 H 2-Me,4-CF.sub.3 0 A-6504 H H H H H O S(?O).sub.2CH.sub.3 H 2-Me,5-CF.sub.3 0 A-6505 H H H H H O S(?O).sub.2CH.sub.3 H 2-Me,6-CF.sub.3 0 A-6506 H H H H H O S(?O).sub.2CH.sub.3 H 2-Me,4-OMe 0 A-6507 H H H H H O S(?O).sub.2CH.sub.3 H 2-Me,5-OMe 0 A-6508 H H H H H O S(?O).sub.2CH.sub.3 H 2-Me,6-OMe 0 A-6509 H H H H H O S(?O).sub.2CH.sub.3 H 3-Me,6-OMe 0 A-6510 H H H H H O S(?O).sub.2CH.sub.3 H 4-Me,2-OMe 0 A-6511 H H H H H O S(?O).sub.2CH.sub.3 H 2,5-OMe.sub.2 0 A-6512 H H H H H O S(?O).sub.2CH.sub.3 H 2,6-OMe.sub.2 0 A-6513 H H H H H O S(?O).sub.2CH.sub.3 H 2-OMe,6-CF.sub.3 0 A-6514 H H H H H O S(?O).sub.2CH.sub.3 H 2-CHF.sub.2,5-F 0 A-6515 H H H H H O S(?O).sub.2CH.sub.3 H 2-CHF.sub.2,6-F 0 A-6516 H H H H H O S(?O).sub.2CH.sub.3 H 2-CHF.sub.2,5-Me 0 A-6517 H H H H H O S(?O).sub.2CH.sub.3 H 2-CHF.sub.2,6-Me 0 A-6518 H H H H H O S(?O).sub.2CH.sub.3 H 2-cyclopropyl,5-F 0 A-6519 H H H H H O S(?O).sub.2CH.sub.3 H 2-cyclopropyl,6-F 0 A-6520 H H H H H O S(?O).sub.2CH.sub.3 H 2-cyclopropyl,5-Me 0 A-6521 H H H H H O S(?O).sub.2CH.sub.3 H 2-cyclopropyl,6-Me 0 A-6522 H H H H H O S(?O).sub.2CH.sub.3 H 2-ethenyl,6-F 0 A-6523 H H H H H O S(?O).sub.2CH.sub.3 H 2-ethenyl,6-Me 0 A-6524 H H H H H O S(?O).sub.2CH.sub.3 H 2-OEt,5-F 0 A-6525 H H H H H O S(?O).sub.2CH.sub.3 H 2-OEt,6-F 0 A-6526 H H H H H O S(?O).sub.2CH.sub.3 H 2-OEt,5-Cl 0 A-6527 H H H H H O S(?O).sub.2CH.sub.3 H 2-OEt,6-Cl 0 A-6528 H H H H H O S(?O).sub.2CH.sub.3 H 2-OEt,5-Me 0 A-6529 H H H H H O S(?O).sub.2CH.sub.3 H 2-OEt,6-Me 0 A-6530 H H H H H O S(?O).sub.2CH.sub.3 H 2-OCHF.sub.2,5-F 0 A-6531 H H H H H O S(?O).sub.2CH.sub.3 H 2-OCHF.sub.2,6-F 0 A-6532 H H H H H O S(?O).sub.2CH.sub.3 H 2-OCHF.sub.2,5-Me 0 A-6533 H H H H H O S(?O).sub.2CH.sub.3 H 2-OCHF.sub.2,6-Me 0 A-6534 H H H H H O S(?O).sub.2CH.sub.3 H 2-(cyclopropyloxy),5-F 0 A-6535 H H H H H O S(?O).sub.2CH.sub.3 H 2-(cyclopropyloxy),6-F 0 A-6536 H H H H H O S(?O).sub.2CH.sub.3 H 2-(cyclopropyloxy),5-Me 0 A-6537 H H H H H O S(?O).sub.2CH.sub.3 H 2-(cyclopropyloxy),6-Me 0 A-6538 H H H H H O S(?O).sub.2CH.sub.3 H 2-SMe,5-F 0 A-6539 H H H H H O S(?O).sub.2CH.sub.3 H 2-SMe,6-F 0 A-6540 H H H H H O S(?O).sub.2CH.sub.3 H 2-SMe,5-Me 0 A-6541 H H H H H O S(?O).sub.2CH.sub.3 H 2-SMe,6-Me 0 A-6542 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O)Me,5-F 0 A-6543 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O)Me,6-F 0 A-6544 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O)Me,5-Me 0 A-6545 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O)Me,6-Me 0 A-6546 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O).sub.2Me,5-F 0 A-6547 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O).sub.2Me,6-F 0 A-6548 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O).sub.2Me,5-Me 0 A-6549 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O).sub.2Me,6-Me 0 A-6550 H H H H H O S(?O).sub.2CH.sub.3 H 2-SCF.sub.3,5-F 0
(217) TABLE-US-00116 TABLE 116 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6551 H H H H H O S(?O).sub.2CH.sub.3 H 2-SCF.sub.3,6-F 0 A-6552 H H H H H O S(?O).sub.2CH.sub.3 H 2-SCF.sub.3,5-Me 0 A-6553 H H H H H O S(?O).sub.2CH.sub.3 H 2-SCF.sub.3,6-Me 0 A-6554 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O)CF.sub.3,5-F 0 A-6555 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O)CF.sub.3,6-F 0 A-6556 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O)CF.sub.3,5-Me 0 A-6557 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O)CF.sub.3,6-Me 0 A-6558 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-6559 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-6560 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-6561 H H H H H O S(?O).sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-6562 H H H H H O S(?O).sub.2CH.sub.3 H 2-(cyclopropylthio),5-F 0 A-6563 H H H H H O S(?O).sub.2CH.sub.3 H 2-(cyclopropylthio),6-F 0 A-6564 H H H H H O S(?O).sub.2CH.sub.3 H 2-(cyclopropylthio),5-Me 0 A-6565 H H H H H O S(?O).sub.2CH.sub.3 H 2-(cyclopropylthio),6-Me 0 A-6566 H H H H H O S(?O).sub.2CH.sub.3 H 2-C(?O)Me,5-F 0 A-6567 H H H H H O S(?O).sub.2CH.sub.3 H 2-C(?O)Me,6-F 0 A-6568 H H H H H O S(?O).sub.2CH.sub.3 H 2-C(?O)Me,5-Me 0 A-6569 H H H H H O S(?O).sub.2CH.sub.3 H 2-C(?O)Me,6-Me 0 A-6570 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2OH,5-F 0 A-6571 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2OH,6-F 0 A-6572 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2OH,5-Me 0 A-6573 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2OH,6-Me 0 A-6574 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-F 0 A-6575 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-F 0 A-6576 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-F 0 A-6577 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-6578 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-6579 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-6580 H H H H H O S(?O).sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,5-F 0 A-6581 H H H H H O S(?O).sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,6-F 0 A-6582 H H H H H O S(?O).sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,5-Me 0 A-6583 H H H H H O S(?O).sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,6-Me 0 A-6584 H H H H H O S(?O).sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-6585 H H H H H O S(?O).sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-6586 H H H H H O S(?O).sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-6587 H H H H H O S(?O).sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-6588 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-F 0 A-6589 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,6-F 0 A-6590 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-Me 0 A-6591 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,6-Me 0 A-6592 H H H H H O S(?O).sub.2CH.sub.3 H 2-NMe.sub.2,5-F 0 A-6593 H H H H H O S(?O).sub.2CH.sub.3 H 2-NMe.sub.2,6-F 0 A-6594 H H H H H O S(?O).sub.2CH.sub.3 H 2-NMe.sub.2,5-Me 0 A-6595 H H H H H O S(?O).sub.2CH.sub.3 H 2-NMe.sub.2,6-Me 0 A-6596 H H H H H O S(?O).sub.2CH.sub.3 H 2-CN,4-F 0 A-6597 H H H H H O S(?O).sub.2CH.sub.3 H 2-CN,5-F 0 A-6598 H H H H H O S(?O).sub.2CH.sub.3 H 2-CN,6-F 0 A-6599 H H H H H O S(?O).sub.2CH.sub.3 H 2-CN,6-Me 0 A-6600 H H H H H O S(?O).sub.2CH.sub.3 H 2-CN,5-OMe 0 A-6601 H H H H H O S(?O).sub.2CH.sub.3 H 2-CN,6-OMe 0 A-6602 H H H H H O S(?O).sub.2CH.sub.3 H 3-CN,6-Me 0 A-6603 H H H H H O S(?O).sub.2CH.sub.3 H 3-CN,6-OMe 0 A-6604 H H H H H O S(?O).sub.2CH.sub.3 H 4-CN,2-Me 0 A-6605 H H H H H O S(?O).sub.2CH.sub.3 H 4-CN,2-OMe 0 A-6606 H H H H H O S(?O).sub.2CH.sub.3 H 2-NO.sub.2,4-F 0 A-6607 H H H H H O S(?O).sub.2CH.sub.3 H 2-NO.sub.2,5-F 0
(218) TABLE-US-00117 TABLE 117 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6608 H H H H H O S(?O).sub.2CH.sub.3 H 2NO.sub.2,6-F 0 A-6609 H H H H H O S(?O).sub.2CH.sub.3 H 2-NO.sub.2,4-Me 0 A-6610 H H H H H O S(?O).sub.2CH.sub.3 H 2-NO.sub.2,5-Me 0 A-6611 H H H H H O S(?O).sub.2CH.sub.3 H 2-NO.sub.2,6-Me 0 A-6612 H H H H H O S(?O).sub.2CH.sub.3 H 2-Me,4,5-F.sub.2 0 A-6613 H H H H H O S(?O).sub.2CH.sub.3 H 2-Me,6-Et 0 A-6614 H H H H H O S(?O).sub.2CH.sub.3 H 2-cyclopropyl,6-OMe 0 A-6615 H H H H H O S(?O).sub.2CH.sub.3 H 2-Me,5-Et 0 A-6616 H H H H H O S(?O).sub.2CH.sub.3 H 2,6-Et.sub.2 0 A-6617 H H H H H O S(?O).sub.2CH.sub.3 H 2-Et,6-F 0 A-6618 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-6619 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-6620 H H H H H O S(?O).sub.2CH.sub.3 H 2-CH.sub.2NMe.sub.2 0 A-6621 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H H 0 A-6622 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-F 0 A-6623 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Cl 0 A-6624 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Br 0 A-6625 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OH 0 A-6626 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Me 0 A-6627 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Et 0 A-6628 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Pr 0 A-6629 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CF.sub.3 0 A-6630 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CHF.sub.2 0 A-6631 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2F 0 A-6632 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CF.sub.2Cl 0 A-6633 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-cyclopropyl 0 A-6634 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-cyclobutyl 0 A-6635 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-cyclopentyl 0 A-6636 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-ethenyl 0 A-6637 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-allyl 0 A-6638 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(prop-1-en-1-yl) 0 A-6639 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(trifluoroethenyl) 0 A-6640 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OMe 0 A-6641 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OEt 0 A-6642 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OPr 0 A-6643 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-O(i-Pr) 0 A-6644 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OCF.sub.3 0 A-6645 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OCHF.sub.2 0 A-6646 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(cyclopropyloxy) 0 A-6647 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(cyclobutyloxy) 0 A-6648 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(cyclopentyloxy) 0 A-6649 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-6650 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(oxiran-2-yl) 0 A-6651 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-SMe 0 A-6652 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 3-SMe 0 A-6653 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O)Me 0 A-6654 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 3-S(?O)Me 0 A-6655 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me 0 A-6656 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 3-S(?O).sub.2Me 0 A-6657 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-SCF.sub.3 0 A-6658 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 3-SCF.sub.3 0 A-6659 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 3-S(?O)CF.sub.3 0 A-6660 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 3-SCF(CF.sub.3).sub.2 0 A-6661 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(cyclopropylthio) 0 A-6662 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(cyclopropylsulfinyl) 0 A-6663 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(cyclopropylsulfonyl) 0 A-6664 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-C(?O)Me 0
(219) TABLE-US-00118 TABLE 118 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6665 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2C(?O)CH.sub.3 0 A-6666 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2C(?O)CF.sub.3 0 A-6667 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OH 0 A-6668 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3 0 A-6669 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-6670 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3 0 A-6671 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2S(?O)CH.sub.3 0 A-6672 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-6673 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(benzyboxy) 0 A-6674 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-NH.sub.2 0 A-6675 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-NHMe 0 A-6676 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-N(Me).sub.2 0 A-6677 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(1,3-dioxolan-2-yl) 0 A-6678 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(1,3-dioxan-2-yl) 0 A-6679 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(1H-imidazol-2-yl) 0 A-6680 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(thiazol-2-yl) 0 A-6681 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(oxazol-2-yl) 0 A-6682 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH?NOH 0 A-6683 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH?NOMe 0 A-6684 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-6685 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CN 0 A-6686 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-NO.sub.2 0 A-6687 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2F,6-Cl 0 A-6688 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-F,6-Me 0 A-6689 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 3-F,6-Me 0 A-6690 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 4-F,2-Me 0 A-6691 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-F,6-OMe 0 A-6692 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 3-F,6-OMe 0 A-6693 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2,6-Cl.sub.2 0 A-6694 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Cl,6-Me 0 A-6695 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 3-Cl,6-Me 0 A-6696 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 4-Cl,2-Me 0 A-6697 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Cl,5-CF.sub.3 0 A-6698 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Cl,6-CF.sub.3 0 A-6699 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Cl,6-OMe 0 A-6700 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 3-Cl,6-OMe 0 A-6701 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 4-Cl,2-OMe 0 A-6702 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2,4-Me.sub.2 0 A-6703 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2,5-Me.sub.2 0 A-6704 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2,6-Me.sub.2 0 A-6705 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Me,4-CF.sub.3 0 A-6706 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Me,5-CF.sub.3 0 A-6707 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Me,6-CF.sub.3 0 A-6708 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Me,4-OMe 0 A-6709 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Me,5-OMe 0 A-6710 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Me,6-OMe 0 A-6711 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 3-Me,6-OMe 0 A-6712 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 4-Me,2-OMe 0 A-6713 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2,5-OMe.sub.2 0 A-6714 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2,6-OMe.sub.2 0 A-6715 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OMe,6-CF.sub.3 0 A-6716 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CHF.sub.2,5-F 0 A-6717 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CHF.sub.2,6-F 0 A-6718 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CHF.sub.2,5-Me 0 A-6719 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CHF.sub.2,6-Me 0 A-6720 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-cyclopropyl,5-F 0 A-6721 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-cyclopropyl,6-F 0
(220) TABLE-US-00119 TABLE 119 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6722 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-cyclopropyl,5-Me 0 A-6723 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-cyclopropyl,6-Me 0 A-6724 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-ethenyl,6-F 0 A-6725 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-ethenyl,6-Me 0 A-6726 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OEt,5-F 0 A-6727 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OEt,6-F 0 A-6728 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OEt,5-Cl 0 A-6729 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OEt,6-Cl 0 A-6730 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OEt,5-Me 0 A-6731 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OEt,6-Me 0 A-6732 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OCHF.sub.2,5-F 0 A-6733 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OCHF.sub.2,6-F 0 A-6734 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OCHF.sub.2,5-Me 0 A-6735 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OCHF.sub.2,6-Me 0 A-6736 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),5-F 0 A-6737 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),6-F 0 A-6738 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),5-Me 0 A-6739 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),6-Me 0 A-6740 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-SMe,5-F 0 A-6741 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-SMe,6-F 0 A-6742 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-SMe,5-Me 0 A-6743 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-SMe,6-Me 0 A-6744 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O)Me,5-F 0 A-6745 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O)Me,6-F 0 A-6746 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O)Me,5-Me 0 A-6747 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O)Me,6-Me 0 A-6748 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,5-F 0 A-6749 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,6-F 0 A-6750 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,5-Me 0 A-6751 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,6-Me 0 A-6752 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-SCF.sub.3,5-F 0 A-6753 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-SCF.sub.3,6-F 0 A-6754 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-SCF.sub.3,5-Me 0 A-6755 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-SCF.sub.3,6-Me 0 A-6756 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,5-F 0 A-6757 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,6-F 0 A-6758 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,5-Me 0 A-6759 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,6-Me 0 A-6760 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-6761 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-6762 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-6763 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-6764 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(cyclopropylthio),5-F 0 A-6765 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(cyclopropylthio),6-F 0 A-6766 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(cyclopropylthio),5-Me 0 A-6767 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-(cyclopropylthio),6-Me 0 A-6768 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-C(?O)Me,5-F 0 A-6769 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-C(?O)Me,6-F 0 A-6770 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-C(?O)Me,5-Me 0 A-6771 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-C(?O)Me,6-Me 0 A-6772 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OH,5-F 0 A-6773 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OH,6-F 0 A-6774 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OH,5-Me 0 A-6775 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OH,6-Me 0 A-6776 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,4-F 0 A-6777 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,5-F 0 A-6778 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,6-F 0
(221) TABLE-US-00120 TABLE 120 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6779 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-6780 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-6781 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-6782 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,5-F 0 A-6783 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,6-F 0 A-6784 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,5-Me 0 A-6785 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,6-Me 0 A-6786 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH3,5-F 0 A-6787 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-6788 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-6789 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-6790 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,5-F 0 A-6791 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,6-F 0 A-6792 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,5-Me 0 A-6793 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,6-Me 0 A-6794 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-NMe.sub.2,5-F 0 A-6795 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-NMe.sub.2,6-F 0 A-6796 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-NMe.sub.2,5-Me 0 A-6797 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-NMe.sub.2,6-Me 0 A-6798 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CN,4-F 0 A-6799 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CN,5-F 0 A-6800 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CN,6-F 0 A-6801 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CN,6-Me 0 A-6802 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CN,5-OMe 0 A-6803 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CN,6-OMe 0 A-6804 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 3-CN,6-Me 0 A-6805 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 3-CN,6-OMe 0 A-6806 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 4-CN,2-Me 0 A-6807 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 4-CN,2-OMe 0 A-6808 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-NO.sub.2,4-F 0 A-6809 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-NO.sub.2,5-F 0 A-6810 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-NO.sub.2,6-F 0 A-6811 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-NO.sub.2,4-Me 0 A-6812 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-NO.sub.2,5-Me 0 A-6813 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-NO.sub.2,6-Me 0 A-6814 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Me,4,5-F.sub.2 0 A-6815 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Me,6-Et 0 A-6816 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-cyclopropyl,6-OMe 0 A-6817 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Me,5-Et 0 A-6818 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2,6-Et.sub.2 0 A-6819 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-Et,6-F 0 A-6820 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-6821 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.2CH.sub.3,6Cl 0 A-6822 H H H H H O S(?O).sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2NMe.sub.2 0 A-6823 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H H 0 A-6824 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-F 0 A-6825 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Cl 0 A-6826 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Br 0 A-6827 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OH 0 A-6828 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Me 0 A-6829 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Et 0 A-6830 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Pr 0 A-6831 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CF.sub.3 0 A-6832 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CHF.sub.2 0 A-6833 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2F 0 A-6834 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CF.sub.2Cl 0 A-6835 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-cyclopropyl 0
(222) TABLE-US-00121 TABLE 121 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6836 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-cyclobutyl 0 A-6837 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-cyclopentyl 0 A-6838 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-ethenyl 0 A-6839 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-allyl 0 A-6840 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(prop-1-en-1-yl) 0 A-6841 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(trifluoroethenyl) 0 A-6842 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OMe 0 A-6843 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OEt 0 A-6844 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OPr 0 A-6845 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-O(i-Pr) 0 A-6846 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OCF.sub.3 0 A-6847 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OCHF.sub.2 0 A-6848 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(cyclopropyloxy) 0 A-6849 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(cyclobutyloxy) 0 A-6850 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(cyclopentyloxy) 0 A-6851 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-6852 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(oxiran-2-yl) 0 A-6853 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-SMe 0 A-6854 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 3-SMe 0 A-6855 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O)Me 0 A-6856 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 3-S(?O)Me 0 A-6857 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me 0 A-6858 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 3-S(?O).sub.2Me 0 A-6859 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-SCF.sub.3 0 A-6860 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 3-SCF.sub.3 0 A-6861 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 3-S(?O)CF.sub.3 0 A-6862 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 3-SCF(CF.sub.3).sub.2 0 A-6863 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(cyclopropylthio) 0 A-6864 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(cyclopropylsulfinyl) 0 A-6865 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(cyclopropylsuIfonyl) 0 A-6866 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-C(?O)Me 0 A-6867 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2C(?O)CH.sub.3 0 A-6868 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2C(?O)CF.sub.3 0 A-6869 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OH 0 A-6870 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3 0 A-6871 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-6872 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3 0 A-6873 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2S(?O)CH.sub.3 0 A-6874 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-6875 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(benzyloxy) 0 A-6876 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-NH.sub.2 0 A-6877 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-NHMe 0 A-6878 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-N(Me).sub.2 0 A-6879 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(1,3-dioxolan-2-yl) 0 A-6880 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(1,3-dioxan-2-yl) 0 A-6881 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(1H-imidazol-2-yl) 0 A-6882 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(thiazol-2-yl) 0 A-6883 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(oxazol-2-yl) 0 A-6884 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH?NOH 0 A-6885 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH?NOMe 0 A-6886 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-6887 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CN 0 A-6888 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-NO.sub.2 0 A-6889 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-F,6-Cl 0 A-6890 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-F,6-Me 0 A-6891 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 3-F,6-Me 0 A-6892 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 4-F,2-Me 0
(223) TABLE-US-00122 TABLE 122 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6893 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-F,6-OMe 0 A-6894 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 3-F,6-OMe 0 A-6895 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2,6-Cl.sub.2 0 A-6896 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Cl,6-Me 0 A-6897 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 3-Cl,6-Me 0 A-6898 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 4-Cl,2-Me 0 A-6899 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Cl,5-CF.sub.3 0 A-6900 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Cl,6-CF.sub.3 0 A-6901 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Cl,6-OMe 0 A-6902 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 3-Cl,6-OMe 0 A-6903 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 4-Cl,2-OMe 0 A-6904 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2,4-Me.sub.2 0 A-6905 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2,5-Me.sub.2 0 A-6906 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2,6-Me.sub.2 0 A-6907 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Me,4-CF.sub.3 0 A-6908 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Me,5-CF.sub.3 0 A-6909 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Me,6-CF.sub.3 0 A-6910 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Me,4-OMe 0 A-6911 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Me,5-OMe 0 A-6912 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Me,6-OMe 0 A-6913 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 3-Me,6-OMe 0 A-6914 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 4-Me,2-OMe 0 A-6915 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2,5-OMe.sub.2 0 A-6916 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2,6-OMe.sub.2 0 A-6917 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OMe,6-CF.sub.3 0 A-6918 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CHF.sub.2,5-F 0 A-6919 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CHF.sub.2,6-F 0 A-6920 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CHF.sub.2,5-Me 0 A-6921 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CHF.sub.2,6-Me 0 A-6922 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-cyclopropyl,5-F 0 A-6923 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-cyclopropyl,6-F 0 A-6924 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-cyclopropyl,5-Me 0 A-6925 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-cyclopropyl,6-Me 0 A-6926 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-ethenyl,6-F 0 A-6927 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-ethenyl,6-Me 0 A-6928 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OEt,5-F 0 A-6929 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OEt,6-F 0 A-6930 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OEt,5-Cl 0 A-6931 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OEt,6-Cl 0 A-6932 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OEt,5-Me 0 A-6933 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OEt,6-Me 0 A-6934 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OCHF.sub.2,5-F 0 A-6935 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OCHF.sub.2,6-F 0 A-6936 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OCHF.sub.2,5-Me 0 A-6937 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OCHF.sub.2,6-Me 0 A-6938 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),5-F 0 A-6939 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),6-F 0 A-6940 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),5-Me 0 A-6941 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(cyclopropyloxy),6-Me 0 A-6942 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-SMe,5-F 0 A-6943 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-SMe,6-F 0 A-6944 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-SMe,5-Me 0 A-6945 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-SMe,6-Me 0 A-6946 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O)Me,5-F 0 A-6947 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O)Me,6-F 0 A-6948 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O)Me,5-Me 0 A-6949 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O)Me,6-Me 0
(224) TABLE-US-00123 TABLE 123 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-6950 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,5-f 0 A-6951 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,6-F 0 A-6952 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,5-Me 0 A-6953 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2Me,6-Me 0 A-6954 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-SCF.sub.3,5-F 0 A-6955 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-SCF.sub.3,6-F 0 A-6956 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-SCF.sub.3,5-Me 0 A-6957 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-SCF.sub.3,6-Me 0 A-6958 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,5-F 0 A-6959 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,6-F 0 A-6960 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,5-Me 0 A-6961 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O)CF.sub.3,6-Me 0 A-6962 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-6963 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-6964 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-6965 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-6966 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(cyclopropylthio),5-F 0 A-6967 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(cyclopropylthio),6-F 0 A-6968 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(cyclopropylthio),5-Me 0 A-6969 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-(cyclopropylthio),6-Me 0 A-6970 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-C(?O)Me,5-F 0 A-6971 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-C(?O)Me,6-F 0 A-6972 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-C(?O)Me,5-Me 0 A-6973 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-C(?O)Me,6-Me 0 A-6974 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OH,5-F 0 A-6975 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OH,6-F 0 A-6976 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OH,5-Me 0 A-6977 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OH,6-Me 0 A-6978 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,4-F 0 A-6979 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,5-F 0 A-6980 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,6-F 0 A-6981 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-6982 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-6983 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-6984 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,5-F 0 A-6985 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,6-F 0 A-6986 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,5-Me 0 A-6987 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OC(?O)CH.sub.3,6-Me 0 A-6988 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-6989 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-6990 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-6991 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-6992 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,5-F 0 A-6993 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,6-F 0 A-6994 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,5-Me 0 A-6995 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2SCH.sub.3,6-Me 0 A-6996 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-NMe.sub.2,5-F 0 A-6997 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-NMe.sub.2,6-F 0 A-6998 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-NMe.sub.2,5-Me 0 A-6999 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-NMe.sub.2,6-Me 0 A-7000 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CN,4-F 0 A-7001 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CN,5-F 0 A-7002 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CN,6-F 0 A-7003 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CN,6-Me 0 A-7004 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CN,5-OMe 0 A-7005 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CN,6-OMe 0 A-7006 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 3-CN,6-Me 0
(225) TABLE-US-00124 TABLE 124 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7007 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 3-CN,6-OMe 0 A-7008 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 4-CN,2-Me 0 A-7009 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 4-CN,2-OMe 0 A-7010 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-NO.sub.2,4-F 0 A-7011 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-NO.sub.2,5-F 0 A-7012 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-NO.sub.2,6-F 0 A-7013 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-NO.sub.2,4-Me 0 A-7014 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-NO.sub.2,5-Me 0 A-7015 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-NO.sub.2,6-Me 0 A-7016 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Me,4,5-F.sub.2 0 A-7017 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Me,6-Et 0 A-7018 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-cyclopropyl,6-OMe 0 A-7019 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Me,5-Et 0 A-7020 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2,6-Et.sub.2 0 A-7021 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-Et,6-F 0 A-7022 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-7023 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-7024 H H H H H O CH.sub.2N(CH.sub.3).sub.2 H 2-CH.sub.2NMe.sub.2 0 A-7025 H H H H H O CH.sub.2C(?O)OCH.sub.3 H H 0 A-7026 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-F 0 A-7027 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-Cl 0 A-7028 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-Br 0 A-7029 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-OH 0 A-7030 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-Me 0 A-7031 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-Et 0 A-7032 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-Pr 0 A-7033 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CF.sub.3 0 A-7034 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CHF.sub.2 0 A-7035 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2F 0 A-7036 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CF.sub.2Cl 0 A-7037 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-cyclopropyl 0 A-7038 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-cyclobutyl 0 A-7039 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-cyclopentyl 0 A-7040 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-ethenyl 0 A-7041 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-allyl 0 A-7042 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-(prop-1-en-1-yl) 0 A-7043 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-(trifluoroethenyl) 0 A-7044 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-OMe 0 A-7045 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-OEt 0 A-7046 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-OPr 0 A-7047 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-O(i-Pr) 0 A-7048 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-OCF.sub.3 0 A-7049 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-OCHF.sub.2 0 A-7050 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-(cyclopropyloxy) 0 A-7051 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-(cycbbutyloxy) 0 A-7052 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-(cyclopentyloxy) 0 A-7053 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-7054 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-(oxiran-2-yl) 0 A-7055 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-SMe 0 A-7056 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 3-SMe 0 A-7057 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-S(=O)Me 0 A-7058 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 3-S(=O)Me 0 A-7059 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-S(=O).sub.2Me 0 A-7060 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 3-S(=O).sub.2Me 0 A-7061 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-SCF.sub.3 0 A-7062 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 3-SCF.sub.3 0 A-7063 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 3-S(=O)CF.sub.3 0
(226) TABLE-US-00125 TABLE 125 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7064 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 3-SCF(CF.sub.3).sub.2 0 A-7065 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(cyclopropylthio) 0 A-7066 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(cyclopropylsulfinyl) 0 A-7067 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(cyclopropylsulfonyl) 0 A-7068 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-C(?O)Me 0 A-7069 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2C(?O)CH.sub.3 0 A-7070 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2C(?O)CF.sub.3 0 A-7071 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2O 0 A-7072 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3 0 A-7073 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-7074 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2SCH.sub.3 0 A-7075 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2S(?O)CH.sub.3 0 A-7076 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-7077 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(benzyloxy) 0 A-7078 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-NH.sub.2 0 A-7079 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-NHMe 0 A-7080 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-N(Me).sub.2 0 A-7081 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(1,3-dioxolan-2-yl) 0 A-7082 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(1,3-dioxan-2-yl) 0 A-7083 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(1H-imidazol-2-yl) 0 A-7084 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(thiazol-2-yl) 0 A-7085 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(oxazol-2-yl) 0 A-7086 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CH?NOH 0 A-7087 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CH?NOMe 0 A-7088 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-7089 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CN 0 A-7090 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-NO.sub.2 0 A-7091 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-F,6-Cl 0 A-7092 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-F,6-Me 0 A-7093 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 3-F,6-Me 0 A-7094 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 4-F,2-Me 0 A-7095 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-F,6-OMe 0 A-7096 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 3-F,6-OMe 0 A-7097 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2,6-Cl.sub.2 0 A-7098 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-Cl,6-Me 0 A-7099 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 3-Cl,6-Me 0 A-7100 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 4-Cl,2-Me 0 A-7101 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-Cl,5-CF.sub.3 0 A-7102 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-Cl,6-CF.sub.3 0 A-7103 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-Cl,6-OMe 0 A-7104 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 3-Cl,6-OMe 0 A-7105 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 4-Cl,2-OMe 0 A-7106 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2,4-Me.sub.2 0 A-7107 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2,5-Me.sub.2 0 A-7108 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2,6-Me.sub.2 0 A-7109 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-Me,4-CF.sub.3 0 A-7110 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-Me,5-CF.sub.3 0 A-7111 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-Me,6-CF.sub.3 0 A-7112 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-Me,4-OMe 0 A-7113 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-Me,5-OMe 0 A-7114 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-Me,6-OMe 0 A-7115 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 3-Me,6-OMe 0 A-7116 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 4-Me,2-OMe 0 A-7117 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2,5-OMe.sub.2 0 A-7118 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2,6-OMe.sub.2 0 A-7119 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-OMe,6-CF.sub.3 0 A-7120 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CHF.sub.2,5-F 0
(227) TABLE-US-00126 TABLE 126 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7121 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CHF.sub.2,6-F 0 A-7122 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CHF.sub.2,5-Me 0 A-7123 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CHF.sub.2,6-Me 0 A-7124 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-cyclopropyl,5-F 0 A-7125 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-cyclopropyl,6-F 0 A-7126 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-cyclopropyl,5-Me 0 A-7127 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-cyclopropyl,6-Me 0 A-7128 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-ethenyl,6-F 0 A-7129 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-ethenyl,6-Me 0 A-7130 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-OEt,5-F 0 A-7131 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-OEt,6-F 0 A-7132 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-OEt,5-Cl 0 A-7133 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-OEt,6-Cl 0 A-7134 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-OEt,5-Me 0 A-7135 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-OEt,6-Me 0 A-7136 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-OCHF.sub.2,5-F 0 A-7137 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-OCHF.sub.2,6-F 0 A-7138 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-OCHF.sub.2,5-Me 0 A-7139 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-OCHF.sub.2,6-Me 0 A-7140 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(cyclopropyloxy),5-F 0 A-7141 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(cyclopropyloxy),6-F 0 A-7142 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(cyclopropyloxy),5-Me 0 A-7143 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(cyclopropyloxy),6-Me 0 A-7144 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-SMe,5-F 0 A-7145 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-SMe,6-F 0 A-7146 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-SMe,5-Me 0 A-7147 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-SMe,6-Me 0 A-7148 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O)Me,5-F 0 A-7149 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O)Me,6-F 0 A-7150 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O)Me,5-Me 0 A-7151 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O)Me,6-Me 0 A-7152 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O).sub.2Me,5-F 0 A-7153 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O).sub.2Me,6-F 0 A-7154 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O).sub.2Me,5-Me 0 A-7155 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O).sub.2Me,6-Me 0 A-7156 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-SCF.sub.3,5-F 0 A-7157 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-SCF.sub.3,6-F 0 A-7158 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-SCF.sub.3,5-Me 0 A-7159 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-SCF.sub.3,6-Me 0 A-7160 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O)CF.sub.3,5-F 0 A-7161 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O)CF.sub.3,6-F 0 A-7162 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O)CF.sub.3,5-Me 0 A-7163 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O)CF.sub.3,6-Me 0 A-7164 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-7165 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-7166 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-7167 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-7168 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(cyclopropylthio),5-F 0 A-7169 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(cyclopropylthio),6-F 0 A-7170 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(cyclopropylthio),5-Me 0 A-7171 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-(cyclopropylthio),6-Me 0 A-7172 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-C(?O)Me,5-F 0 A-7173 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-C(?O)Me,6-F 0 A-7174 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-C(?O)Me,5-Me 0 A-7175 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-C(?O)Me,6-Me 0 A-7176 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2OH,5-F 0 A-7177 H H H H H 0 CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2OH,6-F 0
(228) TABLE-US-00127 TABLE 127 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7178 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2OH,5-Me 0 A-7179 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2OH,6-Me 0 A-7180 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,4-F 0 A-7181 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,5-F 0 A-7182 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,6-F 0 A-7183 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-7184 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-7185 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-7186 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-OC(?O)CH.sub.3,5-F 0 A-7187 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-OC(?O)CH.sub.3,6-F 0 A-7188 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-OC(?O)CH.sub.3,5-Me 0 A-7189 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-OC(?O)CH.sub.3,6-Me 0 A-7190 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-7191 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-7192 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-7193 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-7194 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2SCH.sub.3,5-F 0 A-7195 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2SCH.sub.3,6-F 0 A-7196 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2SCH.sub.3,5-Me 0 A-7197 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2SCH.sub.3,6-Me 0 A-7198 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-NMe.sub.2,5-F 0 A-7199 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-NMe.sub.2,6-F 0 A-7200 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-NMe.sub.2,5-Me 0 A-7201 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-NMe.sub.2,6-Me 0 A-7202 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CN,4-F 0 A-7203 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CN,5-F 0 A-7204 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CN,6-F 0 A-7205 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CN,6-Me 0 A-7206 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CN,5-OMe 0 A-7207 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CN,6-OMe 0 A-7208 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 3-CN,6-Me 0 A-7209 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 3-CN,6-OMe 0 A-7210 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 4-CN,2-Me 0 A-7211 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 4-CN,2-OMe 0 A-7212 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-NO.sub.2,4-F 0 A-7213 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-NO.sub.2,5-F 0 A-7214 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-NO.sub.2,6-F 0 A-7215 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-NO.sub.2,4-Me 0 A-7216 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-NO.sub.2,5-Me 0 A-7217 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-NO.sub.2,6-Me 0 A-7218 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-Me,4,5-F.sub.2 0 A-7219 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-Me,6-Et 0 A-7220 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-cyclopropyl,6-OMe 0 A-7221 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-Me,5-Et 0 A-7222 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2,6-Et.sub.2 0 A-7223 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-Et,6-F 0 A-7224 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-7225 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-7226 H H H H H O CH.sub.2C(?O)OCH.sub.3 H 2-CH.sub.2NMe.sub.2 0 A-7227 H H H H H O CH.sub.2C(?O)NH.sub.2 H H 0 A-7228 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-F 0 A-7229 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Cl 0 A-7230 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Br 0 A-7231 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OH 0 A-7232 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Me 0 A-7233 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Et 0 A-7234 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Pr 0
(229) TABLE-US-00128 TABLE 128 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7235 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CF.sub.3 0 A-7236 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CHF.sub.2 0 A-7237 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2F 0 A-7238 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CF.sub.2Cl 0 A-7239 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-cyclopropyl 0 A-7240 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-cyclobutyl 0 A-7241 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-cyclopentyl 0 A-7242 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-ethenyl 0 A-7243 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-allyl 0 A-7244 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(prop-1-en-1-yl) 0 A-7245 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(trifluoroethenyl) 0 A-7246 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OMe 0 A-7247 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OEt 0 A-7248 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OPr 0 A-7249 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-O(i-Pr) 0 A-7250 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OCF.sub.3 0 A-7251 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OCHF.sub.2 0 A-7252 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(cyclopropyloxy) 0 A-7253 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(cyclobutyloxy) 0 A-7254 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(cyclopentyloxy) 0 A-7255 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-7256 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(oxiran-2-yl) 0 A-7257 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-SMe 0 A-7258 H H H H H O CH.sub.2C(?O)NH.sub.2 H 3-SMe 0 A-7259 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O)Me 0 A-7260 H H H H H O CH.sub.2C(?O)NH.sub.2 H 3-S(?O)Me 0 A-7261 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O).sub.2Me 0 A-7262 H H H H H O CH.sub.2C(?O)NH.sub.2 H 3-S(?O).sub.2Me 0 A-7263 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-SCF.sub.3 0 A-7264 H H H H H O CH.sub.2C(?O)NH.sub.2 H 3-SCF.sub.3 0 A-7265 H H H H H O CH.sub.2C(?O)NH.sub.2 H 3-S(?O)CF.sub.3 0 A-7266 H H H H H O CH.sub.2C(?O)NH.sub.2 H 3-SCF(CF.sub.3).sub.2 0 A-7267 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(cyclopropylthio) 0 A-7268 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(cyclopropylsulfinyl) 0 A-7269 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(cyclopropylsulfonyl) 0 A-7270 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-C(?O)Me 0 A-7271 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2C(?O)CH.sub.3 0 A-7272 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2C(?O)CF.sub.3 0 A-7273 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2OH 0 A-7274 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2OCH.sub.3 0 A-7275 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-7276 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2SCH.sub.3 0 A-7277 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2S(?O)CH.sub.3 0 A-7278 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-7279 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(benzyloxy) 0 A-7280 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-NH.sub.2 0 A-7281 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-NHMe 0 A-7282 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-N(Me).sub.2 0 A-7283 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(1,3-dioxolan-2-yl) 0 A-7284 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(1,3-dioxan-2-yl) 0 A-7285 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(1H-imidazol-2-yl) 0 A-7286 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(thiazol-2-yl) 0 A-7287 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(oxazol-2-yl) 0 A-7288 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH?NOH 0 A-7289 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH?NOMe 0 A-7290 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-7291 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CN 0
(230) TABLE-US-00129 TABLE 129 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7292 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-NO.sub.2 0 A-7293 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-F,6-Cl 0 A-7294 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-F,6-Me 0 A-7295 H H H H H O CH.sub.2C(?O)NH.sub.2 H 3-F,6-Me 0 A-7296 H H H H H O CH.sub.2C(?O)NH.sub.2 H 4-F,2-Me 0 A-7297 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-F,6-OMe 0 A-7298 H H H H H O CH.sub.2C(?O)NH.sub.2 H 3-F,6-OMe 0 A-7299 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2,6-Cl.sub.2 0 A-7300 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Cl,6-Me 0 A-7301 H H H H H O CH.sub.2C(?O)NH.sub.2 H 3-Cl,6-Me 0 A-7302 H H H H H O CH.sub.2C(?O)NH.sub.2 H 4-Cl,2-Me 0 A-7303 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Cl,5-CF.sub.3 0 A-7304 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Cl,6-CF.sub.3 0 A-7305 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Cl,6-OMe 0 A-7306 H H H H H O CH.sub.2C(?O)NH.sub.2 H 3-Cl,6-OMe 0 A-7307 H H H H H O CH.sub.2C(?O)NH.sub.2 H 4-Cl,2-OMe 0 A-7308 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2,4-Me.sub.2 0 A-7309 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2,5-Me.sub.2 0 A-7310 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2,6-Me.sub.2 0 A-7311 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Me,4-CF.sub.3 0 A-7312 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Me,5-CF.sub.3 0 A-7313 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Me,6-CF.sub.3 0 A-7314 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Me,4-OMe 0 A-7315 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Me,5-OMe 0 A-7316 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Me,6-OMe 0 A-7317 H H H H H O CH.sub.2C(?O)NH.sub.2 H 3-Me,6-OMe 0 A-7318 H H H H H O CH.sub.2C(?O)NH.sub.2 H 4-Me,2-OMe 0 A-7319 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2,5-OMe.sub.2 0 A-7320 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2,6-OMe.sub.2 0 A-7321 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OMe,6-CF.sub.3 0 A-7322 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CHF.sub.2,5-F 0 A-7323 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CHF.sub.2,6-F 0 A-7324 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CHF.sub.2,5-Me 0 A-7325 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CHF.sub.2,6-Me 0 A-7326 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-cyclopropyl,5-F 0 A-7327 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-cyclopropyl,6-F 0 A-7328 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-cyclopropyl,5-Me 0 A-7329 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-cyclopropyl,6-Me 0 A-7330 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-ethenyl,6-F 0 A-7331 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-ethenyl,6-Me 0 A-7332 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OEt,5-F 0 A-7333 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OEt,6-F 0 A-7334 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OEt,5-Cl 0 A-7335 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OEt,6-Cl 0 A-7336 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OEt,5-Me 0 A-7337 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OEt,6-Me 0 A-7338 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OCHF.sub.2,5-F 0 A-7339 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OCHF.sub.2,6-F 0 A-7340 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OCHF.sub.2,5-Me 0 A-7341 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OCHF.sub.2,6-Me 0 A-7342 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(cyclopropyloxy),5-F 0 A-7343 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(cyclopropyloxy),6-F 0 A-7344 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(cyclopropyloxy),5-Me 0 A-7345 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(cyclopropyloxy),6-Me 0 A-7346 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-SMe,5-F 0 A-7347 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-SMe,6-F 0 A-7348 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-SMe,5-Me 0
(231) TABLE-US-00130 TABLE 130 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7349 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-SMe,6-Me 0 A-7350 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O)Me,5-F 0 A-7351 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O)Me,6-F 0 A-7352 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O)Me,5-Me 0 A-7353 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O)Me,6-Me 0 A-7354 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O).sub.2Me,5-F 0 A-7355 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O).sub.2Me,6-F 0 A-7356 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O).sub.2Me,5-Me 0 A-7357 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O).sub.2Me,6-Me 0 A-7358 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-SCF.sub.3,5-F 0 A-7359 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-SCF.sub.3,6-F 0 A-7360 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-SCF.sub.3,5-Me 0 A-7361 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-SCF.sub.3,6-Me 0 A-7362 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O)CF.sub.3,5-F 0 A-7363 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O)CF.sub.3,6-F 0 A-7364 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O)CF.sub.3,5-Me 0 A-7365 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O)CF.sub.3,6-Me 0 A-7366 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-7367 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-7368 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-7369 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-7370 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(cyclopropylthio),5-F 0 A-7371 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(cyclopropylthio),6-F 0 A-7372 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(cyclopropylthio),5-Me 0 A-7373 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-(cyclopropylthio),6-Me 0 A-7374 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-C(?O)Me,5-F 0 A-7375 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-C(?O)Me,6-F 0 A-7376 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-C(?O)Me,5-Me 0 A-7377 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-C(?O)Me,6-Me 0 A-7378 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2OH,5-F 0 A-7379 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2OH,6-F 0 A-7380 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2OH,5-Me 0 A-7381 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2OH,6-Me 0 A-7382 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2OCH.sub.3,4-F 0 A-7383 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2OCH.sub.3,5-F 0 A-7384 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2OCH.sub.3,6-F 0 A-7385 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-7386 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-7387 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-7388 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OC(?O)CH.sub.3,5-F 0 A-7389 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OC(?O)CH.sub.3,6-F 0 A-7390 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OC(?O)CH.sub.3,5-Me 0 A-7391 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OC(?O)CH.sub.3,6-Me 0 A-7392 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-7393 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-7394 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-7395 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-7396 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2SCH.sub.3,5-F 0 A-7397 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2SCH.sub.3,6-F 0 A-7398 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2SCH.sub.3,5-Me 0 A-7399 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2SCH.sub.3,6-Me 0 A-7400 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-NMe.sub.2,5-F 0 A-7401 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-NMe.sub.2,6-F 0 A-7402 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-NMe.sub.2,5-Me 0 A-7403 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-NMe.sub.2,6-Me 0 A-7404 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CN,4-F 0 A-7405 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CN,5-F 0
(232) TABLE-US-00131 TABLE 131 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7406 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CN,6-F 0 A-7407 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CN,6-Me 0 A-7408 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CN,5-OMe 0 A-7409 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CN,6-OMe 0 A-7410 H H H H H O CH.sub.2C(?O)NH.sub.2 H 3-CN,6-Me 0 A-7411 H H H H H O CH.sub.2C(?O)NH.sub.2 H 3-CN,6-OMe 0 A-7412 H H H H H O CH.sub.2C(?O)NH.sub.2 H 4-CN,2-Me 0 A-7413 H H H H H O CH.sub.2C(?O)NH.sub.2 H 4-CN,2-OMe 0 A-7414 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-NO.sub.2,4-F 0 A-7415 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-NO.sub.2,5-F 0 A-7416 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-NO.sub.2,6-F 0 A-7417 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-NO.sub.2,4-Me 0 A-7418 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-NO.sub.2,5-Me 0 A-7419 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-NO.sub.2,6-Me 0 A-7420 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Me,4,5-F.sub.2 0 A-7421 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Me,6-Et 0 A-7422 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-cyclopropyl,6-OMe 0 A-7423 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Me,5-Et 0 A-7424 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2,6-Et.sub.2 0 A-7425 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-Et,6-F 0 A-7426 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-7427 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-7428 H H H H H O CH.sub.2C(?O)NH.sub.2 H 2-CH.sub.2NMe.sub.2 0 A-7429 H H H H H O CH?NOH H H 0 A-7430 H H H H H O CH?NOH H 2-F 0 A-7431 H H H H H O CH?NOH H 2-Cl 0 A-7432 H H H H H O CH?NOH H 2-Br 0 A-7433 H H H H H O CH?NOH H 2-OH 0 A-7434 H H H H H O CH?NOH H 2-Me 0 A-7435 H H H H H O CH?NOH H 2-Et 0 A-7436 H H H H H O CH?NOH H 2-Pr 0 A-7437 H H H H H O CH?NOH H 2-CF.sub.3 0 A-7438 H H H H H O CH?NOH H 2-CHF.sub.2 0 A-7439 H H H H H O CH?NOH H 2-CH.sub.2F 0 A-7440 H H H H H O CH?NOH H 2-CF.sub.2Cl 0 A-7441 H H H H H O CH?NOH H 2-cyclopropyl 0 A-7442 H H H H H O CH?NOH H 2-cyclobutyl 0 A-7443 H H H H H O CH?NOH H 2-cyclopentyl 0 A-7444 H H H H H O CH?NOH H 2-ethenyl 0 A-7445 H H H H H O CH?NOH H 2-allyl 0 A-7446 H H H H H O CH?NOH H 2-(prop-1-en-1-yl) 0 A-7447 H H H H H O CH?NOH H 2-(trifluoroethenyl) 0 A-7448 H H H H H O CH?NOH H 2-OMe 0 A-7449 H H H H H O CH?NOH H 2-OEt 0 A-7450 H H H H H O CH?NOH H 2-OPr 0 A-7451 H H H H H O CH?NOH H 2-O(i-Pr) 0 A-7452 H H H H H O CH?NOH H 2-OCF.sub.3 0 A-7453 H H H H H O CH?NOH H 2-OCHF.sub.2 0 A-7454 H H H H H O CH?NOH H 2-(cyclopropyloxy) 0 A-7455 H H H H H O CH?NOH H 2-(cyclobutyloxy) 0 A-7456 H H H H H O CH?NOH H 2-(cyclopentyloxy) 0 A-7457 H H H H H O CH?NOH H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-7458 H H H H H O CH?NOH H 2-(oxiran-2-yl) 0 A-7459 H H H H H O CH?NOH H 2-SMe 0 A-7460 H H H H H O CH?NOH H 3-SMe 0 A-7461 H H H H H O CH?NOH H 2-S(?O)Me 0 A-7462 H H H H H O CH?NOH H 3-S(?O)Me 0
(233) TABLE-US-00132 TABLE 132 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7463 H H H H H O CH?NOH H 2-S(?O).sub.2Me 0 A-7464 H H H H H O CH?NOH H 3-S(?O).sub.2Me 0 A-7465 H H H H H O CH?NOH H 2-SCF.sub.3 0 A-7466 H H H H H O CH?NOH H 3-SCF.sub.3 0 A-7467 H H H H H O CH?NOH H 3-S(?O)CF.sub.3 0 A-7468 H H H H H O CH?NOH H 3-SCF(CF.sub.3).sub.2 0 A-7469 H H H H H O CH?NOH H 2-(cyclopropylthio) 0 A-7470 H H H H H O CH?NOH H 2-(cyclopropylsulfinyl) 0 A-7471 H H H H H O CH?NOH H 2-(cyclopropylsulfonyl) 0 A-7472 H H H H H O CH?NOH H 2-C(?O)Me 0 A-7473 H H H H H O CH?NOH H 2-CH.sub.2C(?O)CH.sub.3 0 A-7474 H H H H H O CH?NOH H 2-CH.sub.2C(?O)CF.sub.3 0 A-7475 H H H H H O CH?NOH H 2-CH.sub.2OH 0 A-7476 H H H H H O CH?NOH H 2-CH.sub.2OCH.sub.3 0 A-7477 H H H H H O CH?NOH H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-7478 H H H H H O CH?NOH H 2-CH.sub.2SCH.sub.3 0 A-7479 H H H H H O CH?NOH H 2-CH.sub.2S(?O)CH.sub.3 0 A-7480 H H H H H O CH?NOH H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-7481 H H H H H O CH?NOH H 2-(benzyloxy) 0 A-7482 H H H H H O CH?NOH H 2-NH.sub.2 0 A-7483 H H H H H O CH?NOH H 2-NHMe 0 A-7484 H H H H H O CH?NOH H 2-N(Me).sub.2 0 A-7485 H H H H H O CH?NOH H 2-(1,3-dioxolan-2-yl) 0 A-7486 H H H H H O CH?NOH H 2-(1,3-dioxan-2-yl) 0 A-7487 H H H H H O CH?NOH H 2-(1H-imidazol-2-yl) 0 A-7488 H H H H H O CH?NOH H 2-(thiazol-2-yl) 0 A-7489 H H H H H O CH?NOH H 2-(oxazol-2-yl) 0 A-7490 H H H H H O CH?NOH H 2-CH?NOH 0 A-7491 H H H H H O CH?NOH H 2-CH?NOMe 0 A-7492 H H H H H O CH?NOH H 2-(4,5-dihydro-3-isoxazolyl) 0 A-7493 H H H H H O CH?NOH H 2-CN 0 A-7494 H H H H H O CH?NOH H 2-NO.sub.2 0 A-7495 H H H H H O CH?NOH H 2-F,6-Cl 0 A-7496 H H H H H O CH?NOH H 2-F,6-Me 0 A-7497 H H H H H O CH?NOH H 3-F,6-Me 0 A-7498 H H H H H O CH?NOH H 4-F,2-Me 0 A-7499 H H H H H O CH?NOH H 2-F,6-OMe 0 A-7500 H H H H H O CH?NOH H 3-F,6-OMe 0 A-7501 H H H H H O CH?NOH H 2,6-Cl.sub.2 0 A-7502 H H H H H O CH?NOH H 2-Cl,6-Me 0 A-7503 H H H H H O CH?NOH H 3-Cl,6-Me 0 A-7504 H H H H H O CH?NOH H 4-Cl,2-Me 0 A-7505 H H H H H O CH?NOH H 2-Cl,5-CF.sub.3 0 A-7506 H H H H H O CH?NOH H 2-Cl,6-CF.sub.3 0 A-7507 H H H H H O CH?NOH H 2-Cl,6-OMe 0 A-7508 H H H H H O CH?NOH H 3-Cl,6-OMe 0 A-7509 H H H H H O CH?NOH H 4-Cl,2-OMe 0 A-7510 H H H H H O CH?NOH H 2,4-Me.sub.2 0 A-7511 H H H H H O CH?NOH H 2,5-Me.sub.2 0 A-7512 H H H H H O CH?NOH H 2,6-Me.sub.2 0 A-7513 H H H H H O CH?NOH H 2-Me,4-CF.sub.3 0 A-7514 H H H H H O CH?NOH H 2-Me,5-CF.sub.3 0 A-7515 H H H H H O CH?NOH H 2-Me,6-CF.sub.3 0 A-7516 H H H H H O CH?NOH H 2-Me,4-OMe 0 A-7517 H H H H H O CH?NOH H 2-Me,5-OMe 0 A-7518 H H H H H O CH?NOH H 2-Me,6-OMe 0 A-7519 H H H H H O CH?NOH H 3-Me,6-OMe 0
(234) TABLE-US-00133 TABLE 133 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7520 H H H H H O CH?NOH H 4-Me,2-OMe 0 A-7521 H H H H H O CH?NOH H 2,5-OMe.sub.2 0 A-7522 H H H H H O CH?NOH H 2,6-OMe.sub.2 0 A-7523 H H H H H O CH?NOH H 2-OMe,6-CF.sub.3 0 A-7524 H H H H H O CH?NOH H 2-CHF.sub.2,5-F 0 A-7525 H H H H H O CH?NOH H 2-CHF.sub.2,6-F 0 A-7526 H H H H H O CH?NOH H 2-CHF.sub.2,5-Me 0 A-7527 H H H H H O CH?NOH H 2-CHF.sub.2,6-Me 0 A-7528 H H H H H O CH?NOH H 2-cyclopropyl,5-F 0 A-7529 H H H H H O CH?NOH H 2-cyclopropyl,6-F 0 A-7530 H H H H H O CH?NOH H 2-cyclopropyl,5-Me 0 A-7531 H H H H H O CH?NOH H 2-cyclopropyl,6-Me 0 A-7532 H H H H H O CH?NOH H 2-ethenyl,6-F 0 A-7533 H H H H H O CH?NOH H 2-ethenyl,6-Me 0 A-7534 H H H H H O CH?NOH H 2-OEt,5-F 0 A-7535 H H H H H O CH?NOH H 2-OEt,6-F 0 A-7536 H H H H H O CH?NOH H 2-OEt,5-Cl 0 A-7537 H H H H H O CH?NOH H 2-OEt,6-Cl 0 A-7538 H H H H H O CH?NOH H 2-OEt,5-Me 0 A-7539 H H H H H O CH?NOH H 2-OEt,6-Me 0 A-7540 H H H H H O CH?NOH H 2-OCHF.sub.2,5-F 0 A-7541 H H H H H O CH?NOH H 2-OCHF.sub.2,6-F 0 A-7542 H H H H H O CH?NOH H 2-OCHF.sub.2,5-Me 0 A-7543 H H H H H O CH?NOH H 2-OCHF.sub.2,6-Me 0 A-7544 H H H H H O CH?NOH H 2-(cyclopropyloxy),5-F 0 A-7545 H H H H H O CH?NOH H 2-(cyclopropyloxy),6-F 0 A-7546 H H H H H O CH?NOH H 2-(cyclopropyloxy),5-Me 0 A-7547 H H H H H O CH?NOH H 2-(cyclopropyloxy),6-Me 0 A-7548 H H H H H O CH?NOH H 2-SMe,5-F 0 A-7549 H H H H H O CH?NOH H 2-SMe,6-F 0 A-7550 H H H H H O CH?NOH H 2-SMe,5-Me 0 A-7551 H H H H H O CH?NOH H 2-SMe,6-Me 0 A-7552 H H H H H O CH?NOH H 2-S(?O)Me,5-F 0 A-7553 H H H H H O CH?NOH H 2-S(?O)Me,6-F 0 A-7554 H H H H H O CH?NOH H 2-S(?O)Me,5-Me 0 A-7555 H H H H H O CH?NOH H 2-S(?O)Me,6-Me 0 A-7556 H H H H H O CH?NOH H 2-S(?O).sub.2Me,5-F 0 A-7557 H H H H H O CH?NOH H 2-S(?O).sub.2Me,6-F 0 A-7558 H H H H H O CH?NOH H 2-S(?O).sub.2Me,5-Me 0 A-7559 H H H H H O CH?NOH H 2-S(?O).sub.2Me,6-Me 0 A-7560 H H H H H O CH?NOH H 2-SCF.sub.3,5-F 0 A-7561 H H H H H O CH?NOH H 2-SCF.sub.3,6-F 0 A-7562 H H H H H O CH?NOH H 2-SCF.sub.3,5-Me 0 A-7563 H H H H H O CH?NOH H 2-SCF.sub.3,6-Me 0 A-7564 H H H H H O CH?NOH H 2-S(?O)CF.sub.3,5-F 0 A-7565 H H H H H O CH?NOH H 2-S(?O)CF.sub.3,6-F 0 A-7566 H H H H H O CH?NOH H 2-S(?O)CF.sub.3,5-Me 0 A-7567 H H H H H O CH?NOH H 2-S(?O)CF.sub.3,6-Me 0 A-7568 H H H H H O CH?NOH H 2-S(?O).sub.2CF.sub.3,5-F 0 A-7569 H H H H H O CH?NOH H 2-S(?O).sub.2CF.sub.3,6-F 0 A-7570 H H H H H O CH?NOH H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-7571 H H H H H O CH?NOH H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-7572 H H H H H O CH?NOH H 2-(cyclopropylthio),5-F 0 A-7573 H H H H H O CH?NOH H 2-(cyclopropylthio),6-F 0 A-7574 H H H H H O CH?NOH H 2-(cyclopropylthio),5-Me 0 A-7575 H H H H H O CH?NOH H 2-(cyclopropylthio),6-Me 0 A-7576 H H H H H O CH?NOH H 2-C(?O)Me,5-F 0
(235) TABLE-US-00134 TABLE 134 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7577 H H H H H O CH?NOH H 2-C(?O)Me,6-F 0 A-7578 H H H H H O CH?NOH H 2-C(?O)Me,5-Me 0 A-7579 H H H H H O CH?NOH H 2-C(?O)Me,6-Me 0 A-7580 H H H H H O CH?NOH H 2-CH.sub.2OH,5-F 0 A-7581 H H H H H O CH?NOH H 2-CH.sub.2OH,6-F 0 A-7582 H H H H H O CH?NOH H 2-CH.sub.2OH,5-Me 0 A-7583 H H H H H O CH?NOH H 2-CH.sub.2OH,6-Me 0 A-7584 H H H H H O CH?NOH H 2-CH.sub.2OCH.sub.3,4-F 0 A-7585 H H H H H O CH?NOH H 2-CH.sub.2OCH.sub.3,5-F 0 A-7586 H H H H H O CH?NOH H 2-CH.sub.2OCH.sub.3,6-F 0 A-7587 H H H H H O CH?NOH H 2-CH.sub.2OCH.sub.3,4-Me 0 A-7588 H H H H H O CH?NOH H 2-CH.sub.2OCH.sub.3,5-Me 0 A-7589 H H H H H O CH?NOH H 2-CH.sub.2OCH.sub.3,6-Me 0 A-7590 H H H H H O CH?NOH H 2-OC(?O)CH.sub.3,5-F 0 A-7591 H H H H H O CH?NOH H 2-OC(?O)CH.sub.3,6-F 0 A-7592 H H H H H O CH?NOH H 2-OC(?O)CH.sub.3,5-Me 0 A-7593 H H H H H O CH?NOH H 2-OC(?O)CH.sub.3,6-Me 0 A-7594 H H H H H O CH?NOH H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-7595 H H H H H O CH?NOH H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-7596 H H H H H O CH?NOH H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-7597 H H H H H O CH?NOH H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-7598 H H H H H O CH?NOH H 2-CH.sub.2SCH.sub.3,5-F 0 A-7599 H H H H H O CH?NOH H 2-CH.sub.2SCH.sub.3,6-F 0 A-7600 H H H H H O CH?NOH H 2-CH.sub.2SCH.sub.3,5-Me 0 A-7601 H H H H H O CH?NOH H 2-CH.sub.2SCH.sub.3,6-Me 0 A-7602 H H H H H O CH?NOH H 2-NMe.sub.2,5-F 0 A-7603 H H H H H O CH?NOH H 2-NMe.sub.2,6-F 0 A-7604 H H H H H O CH?NOH H 2-NMe.sub.2,5-Me 0 A-7605 H H H H H O CH?NOH H 2-NMe.sub.2,6-Me 0 A-7606 H H H H H O CH?NOH H 2-CN,4-F 0 A-7607 H H H H H O CH?NOH H 2-CN,5-F 0 A-7608 H H H H H O CH?NOH H 2-CN,6-F 0 A-7609 H H H H H O CH?NOH H 2-CN,6-Me 0 A-7610 H H H H H O CH?NOH H 2-CN,5-OMe 0 A-7611 H H H H H O CH?NOH H 2-CN,6-OMe 0 A-7612 H H H H H O CH?NOH H 3-CN,6-Me 0 A-7613 H H H H H O CH?NOH H 3-CN,6-OMe 0 A-7614 H H H H H O CH?NOH H 4-CN,2-Me 0 A-7615 H H H H H O CH?NOH H 4-CN,2-OMe 0 A-7616 H H H H H O CH?NOH H 2-NO.sub.2,4-F 0 A-7617 H H H H H O CH?NOH H 2-NO.sub.2,5-F 0 A-7618 H H H H H O CH?NOH H 2-NO.sub.2,6-F 0 A-7619 H H H H H O CH?NOH H 2-NO.sub.2,4-Me 0 A-7620 H H H H H O CH?NOH H 2-NO.sub.2,5-Me 0 A-7621 H H H H H O CH?NOH H 2-NO.sub.2,6-Me 0 A-7622 H H H H H O CH?NOH H 2-Me,4,5-F.sub.2 0 A-7623 H H H H H O CH?NOH H 2-Me,6-Et 0 A-7624 H H H H H O CH?NOH H 2-cyclopropyl,6-OMe 0 A-7625 H H H H H O CH?NOH H 2-Me,5-Et 0 A-7626 H H H H H O CH?NOH H 2,6-Et.sub.2 0 A-7627 H H H H H O CH?NOH H 2-Et,6-F 0 A-7628 H H H H H O CH?NOH H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-7629 H H H H H O CH?NOH H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-7630 H H H H H O CH?NOH H 2-CH.sub.2NMe.sub.2 0 A-7631 H H H H H O CH?NOCH.sub.2CH.sub.3 H H 0 A-7632 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-F 0 A-7633 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Cl 0
(236) TABLE-US-00135 TABLE 135 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7634 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Br 0 A-7635 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OH 0 A-7636 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Me 0 A-7637 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Et 0 A-7638 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Pr 0 A-7639 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CF.sub.3 0 A-7640 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CHF.sub.2 0 A-7641 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2F 0 A-7642 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CF.sub.2Cl 0 A-7643 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-cyclopropyl 0 A-7644 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-cyclobutyl 0 A-7645 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-cyclopentyl 0 A-7646 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-ethenyl 0 A-7647 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-allyl 0 A-7648 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(prop-1-en-1-yl) 0 A-7649 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(trifluoroethenyl) 0 A-7650 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OMe 0 A-7651 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OEt 0 A-7652 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OPr 0 A-7653 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-O(i-Pr) 0 A-7654 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OCF.sub.3 0 A-7655 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OCHF.sub.2 0 A-7656 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(cyclopropyloxy) 0 A-7657 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(cyclobutyloxy) 0 A-7658 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(cyclopentyloxy) 0 A-7659 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-((2,2-dichlrocyclopropyl)oxy) 0 A-7660 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(oxiran-2-yl) 0 A-7661 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-SMe 0 A-7662 H H H H H O CH?NOCH.sub.2CH.sub.3 H 3-SMe 0 A-7663 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O)Me 0 A-7664 H H H H H O CH?NOCH.sub.2CH.sub.3 H 3-S(?O)Me 0 A-7665 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O).sub.2Me 0 A-7666 H H H H H O CH?NOCH.sub.2CH.sub.3 H 3-S(?O).sub.2Me 0 A-7667 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-SCF.sub.3 0 A-7668 H H H H H O CH?NOCH.sub.2CH.sub.3 H 3-SCF.sub.3 0 A-7669 H H H H H O CH?NOCH.sub.2CH.sub.3 H 3-S(?O)CF.sub.3 0 A-7670 H H H H H O CH?NOCH.sub.2CH.sub.3 H 3-SCF(CF.sub.3).sub.2 0 A-7671 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(cyclopropylthio) 0 A-7672 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(cyclopropylsulfinyl) 0 A-7673 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(cyclopropylsulfonyl) 0 A-7674 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-C(?O)Me 0 A-7675 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2C(?O)CH.sub.3 0 A-7676 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2C(?O)CF.sub.3 0 A-7677 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2OH 0 A-7678 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3 0 A-7679 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3 0 A-7680 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3 0 A-7681 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2S(?O)CH.sub.3 0 A-7682 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-7683 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(benzyloxy) 0 A-7684 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-NH.sub.2 0 A-7685 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-NHMe 0 A-7686 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-N(Me).sub.2 0 A-7687 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(1,3-dioxolan-2-yl) 0 A-7688 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(1,3-dioxan-2-yl) 0 A-7689 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(1H-imidazol-2-yl) 0 A-7690 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(thiazol-2-yl) 0
(237) TABLE-US-00136 TABLE 136 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7691 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(oxazol-2-yl) 0 A-7692 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH?NOH 0 A-7693 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH?NOMe 0 A-7694 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(4,5-dihydro-3-isoxazolyl) 0 A-7695 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CN 0 A-7696 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-NO.sub.2 0 A-7697 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-F,6-Cl 0 A-7698 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-F,6-Me 0 A-7699 H H H H H O CH?NOCH.sub.2CH.sub.3 H 3-F,6-Me 0 A-7700 H H H H H O CH?NOCH.sub.2CH.sub.3 H 4-F,2-Me 0 A-7701 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-F,6-OMe 0 A-7702 H H H H H O CH?NOCH.sub.2CH.sub.3 H 3-F,6-OMe 0 A-7703 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2,6-Cl.sub.2 0 A-7704 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Cl,6-Me 0 A-7705 H H H H H O CH?NOCH.sub.2CH.sub.3 H 3-Cl,6-Me 0 A-7706 H H H H H O CH?NOCH.sub.2CH.sub.3 H 4-Cl,2-Me 0 A-7707 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Cl,5-CF.sub.3 0 A-7708 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Cl,6-CF.sub.3 0 A-7709 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Cl,6-OMe 0 A-7710 H H H H H O CH?NOCH.sub.2CH.sub.3 H 3-Cl,6-OMe 0 A-7711 H H H H H O CH?NOCH.sub.2CH.sub.3 H 4-Cl,2-OMe 0 A-7712 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2,4-Me.sub.2 0 A-7713 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2,5-Me.sub.2 0 A-7714 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2,6-Me.sub.2 0 A-7715 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Me,4-CF.sub.3 0 A-7716 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Me,5-CF.sub.3 0 A-7717 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Me,6-CF.sub.3 0 A-7718 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Me,4-OMe 0 A-7719 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Me,5-OMe 0 A-7720 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Me,6-OMe 0 A-7721 H H H H H O CH?NOCH.sub.2CH.sub.3 H 3-Me,6-OMe 0 A-7722 H H H H H O CH?NOCH.sub.2CH.sub.3 H 4-Me,2-OMe 0 A-7723 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2,5-OMe.sub.2 0 A-7724 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2,6-OMe.sub.2 0 A-7725 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OMe,6-CF.sub.3 0 A-7726 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CHF.sub.2,5-F 0 A-7727 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CHF.sub.2,6-F 0 A-7728 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CHF.sub.2,5-Me 0 A-7729 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CHF.sub.2,6-Me 0 A-7730 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-cyclopropyl,5-F 0 A-7731 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-cyclopropyl,6-F 0 A-7732 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-cyclopropyl,5-Me 0 A-7733 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-cyclopropyl,6-Me 0 A-7734 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-ethenyl,6-F 0 A-7735 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-ethenyl,6-Me 0 A-7736 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OEt,5-F 0 A-7737 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OEt,6-F 0 A-7738 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OEt,5-Cl 0 A-7739 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OEt,6-Cl 0 A-7740 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OEt,5-Me 0 A-7741 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OEt,6-Me 0 A-7742 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OCHF.sub.2,5-F 0 A-7743 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OCHF.sub.2,6-F 0 A-7744 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OCHF.sub.2,5-Me 0 A-7745 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OCHF.sub.2,6-Me 0 A-7746 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(cyclopropyloxy),5-F 0 A-7747 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(cyclopropyloxy),6-F 0
(238) TABLE-US-00137 TABLE 137 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7748 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(cyclopropyloxy),5-Me 0 A-7749 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(cyclopropyloxy),6-Me 0 A-7750 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-SMe,5-F 0 A-7751 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-SMe,6-F 0 A-7752 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-SMe,5-Me 0 A-7753 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-SMe,6-Me 0 A-7754 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O)Me,5-F 0 A-7755 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O)Me,6-F 0 A-7756 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O)Me,5-Me 0 A-7757 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O)Me,6-Me 0 A-7758 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,5-F 0 A-7759 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,6-F 0 A-7760 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,5-Me 0 A-7761 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O).sub.2Me,6-Me 0 A-7762 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-SCF.sub.3,5-F 0 A-7763 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-SCF.sub.3,6-F 0 A-7764 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-SCF.sub.3,5-Me 0 A-7765 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-SCF.sub.3,6-Me 0 A-7766 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,5-F 0 A-7767 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,6-F 0 A-7768 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,5-Me 0 A-7769 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O)CF.sub.3,6-Me 0 A-7770 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-F 0 A-7771 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-F 0 A-7772 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-7773 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-7774 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(cyclopropylthio),5-F 0 A-7775 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(cyclopropylthio),6-F 0 A-7776 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(cyclopropylthio),5-Me 0 A-7777 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-(cyclopropylthio),6-Me 0 A-7778 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-C(?O)Me,5-F 0 A-7779 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-C(?O)Me,6-F 0 A-7780 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-C(?O)Me,5-Me 0 A-7781 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-C(?O)Me,6-Me 0 A-7782 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2OH,5-F 0 A-7783 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2OH,6-F 0 A-7784 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2OH,5-Me 0 A-7785 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2OH,6-Me 0 A-7786 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-F 0 A-7787 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-F 0 A-7788 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-F 0 A-7789 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,4-Me 0 A-7790 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,5-Me 0 A-7791 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Me 0 A-7792 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,5-F 0 A-7793 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,6-F 0 A-7794 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,5-Me 0 A-7795 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OC(?O)CH.sub.3,6-Me 0 A-7796 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-7797 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-7798 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-7799 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-7800 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-F 0 A-7801 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,6-F 0 A-7802 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,5-Me 0 A-7803 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2SCH.sub.3,6-Me 0 A-7804 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-NMe.sub.2,5-F 0
(239) TABLE-US-00138 TABLE 138 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7805 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-NMe.sub.2,6-F 0 A-7806 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-NMe.sub.2,5-Me 0 A-7807 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-NMe.sub.2,6-Me 0 A-7808 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CN,4-F 0 A-7809 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CN,5-F 0 A-7810 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CN,6-F 0 A-7811 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CN,6-Me 0 A-7812 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CN,5-OMe 0 A-7813 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CN,6-OMe 0 A-7814 H H H H H O CH?NOCH.sub.2CH.sub.3 H 3-CN,6-Me 0 A-7815 H H H H H O CH?NOCH.sub.2CH.sub.3 H 3-CN,6-OMe 0 A-7816 H H H H H O CH?NOCH.sub.2CH.sub.3 H 4-CN,2-Me 0 A-7817 H H H H H O CH?NOCH.sub.2CH.sub.3 H 4-CN,2-OMe 0 A-7818 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-NO.sub.2,4-F 0 A-7819 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-NO.sub.2,5-F 0 A-7820 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-NO.sub.2,6-F 0 A-7821 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-NO.sub.2,4-Me 0 A-7822 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-NO.sub.2,5-Me 0 A-7823 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-NO.sub.2,6-Me 0 A-7824 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Me,4,5-F.sub.2 0 A-7825 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Me,6-Et 0 A-7826 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-cyclopropyl,6-OMe 0 A-7827 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Me,5-Et 0 A-7828 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2,6-Et.sub.2 0 A-7829 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-Et,6-F 0 A-7830 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-7831 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-7832 H H H H H O CH?NOCH.sub.2CH.sub.3 H 2-CH.sub.2NMe.sub.2 0 A-7833 H H H H H O ?CHN(CH.sub.3).sub.2 H 0 A-7834 H H H H H O ?CHN(CH.sub.3).sub.2 2-F 0 A-7835 H H H H H O ?CHN(CH.sub.3).sub.2 2-Cl 0 A-7836 H H H H H O ?CHN(CH.sub.3).sub.2 2-Br 0 A-7837 H H H H H O ?CHN(CH.sub.3).sub.2 2-OH 0 A-7838 H H H H H O ?CHN(CH.sub.3).sub.2 2-Me 0 A-7839 H H H H H O ?CHN(CH.sub.3).sub.2 2-Et 0 A-7840 H H H H H O ?CHN(CH.sub.3).sub.2 2-Pr 0 A-7841 H H H H H O ?CHN(CH.sub.3).sub.2 2-CF.sub.3 0 A-7842 H H H H H O ?CHN(CH.sub.3).sub.2 2-CHF.sub.2 0 A-7843 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2F 0 A-7844 H H H H H O ?CHN(CH.sub.3).sub.2 2-CF.sub.2Cl 0 A-7845 H H H H H O ?CHN(CH.sub.3).sub.2 2-cyclopropyl 0 A-7846 H H H H H O ?CHN(CH.sub.3).sub.2 2-cyclobutyl 0 A-7847 H H H H H O ?CHN(CH.sub.3).sub.2 2-cyclopentyl 0 A-7848 H H H H H O ?CHN(CH.sub.3).sub.2 2-ethenyl 0 A-7849 H H H H H O ?CHN(CH.sub.3).sub.2 2-allyl 0 A-7850 H H H H H O ?CHN(CH.sub.3).sub.2 2-(prop-1-en-1-yl) 0 A-7851 H H H H H O ?CHN(CH.sub.3).sub.2 2-(trifluoroethenyl) 0 A-7852 H H H H H O ?CHN(CH.sub.3).sub.2 2-OMe 0 A-7853 H H H H H O ?CHN(CH.sub.3).sub.2 2-OEt 0 A-7854 H H H H H O ?CHN(CH.sub.3).sub.2 2-OPr 0 A-7855 H H H H H O ?CHN(CH.sub.3).sub.2 2-O(i-Pr) 0 A-7856 H H H H H O ?CHN(CH.sub.3).sub.2 2-OCF.sub.3 0 A-7857 H H H H H O ?CHN(CH.sub.3).sub.2 2-OCHF.sub.2 0 A-7858 H H H H H O ?CHN(CH.sub.3).sub.2 2-(cyclopropyloxy) 0 A-7859 H H H H H O ?CHN(CH.sub.3).sub.2 2-(cyclobutyloxy) 0 A-7860 H H H H H O ?CHN(CH.sub.3).sub.2 2-(cyclopentyloxy) 0 A-7861 H H H H H O ?CHN(CH.sub.3).sub.2 2-((2,2-dichlorocyclopropyl)oxy) 0
(240) TABLE-US-00139 TABLE 139 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7862 H H H H H O ?CHN(CH.sub.3).sub.2 2-(oxiran-2-yl) 0 A-7863 H H H H H O ?CHN(CH.sub.3).sub.2 2-SMe 0 A-7864 H H H H H O ?CHN(CH.sub.3).sub.2 3-SMe 0 A-7865 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O)Me 0 A-7866 H H H H H O ?CHN(CH.sub.3).sub.2 3-S(?O)Me 0 A-7867 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O).sub.2Me 0 A-7868 H H H H H O ?CHN(CH.sub.3).sub.2 3-S(?O).sub.2Me 0 A-7869 H H H H H O ?CHN(CH.sub.3).sub.2 2-SCF.sub.3 0 A-7870 H H H H H O ?CHN(CH.sub.3).sub.2 3-SCF.sub.3 0 A-7871 H H H H H O ?CHN(CH.sub.3).sub.2 3-S(?O)CF.sub.3 0 A-7872 H H H H H O ?CHN(CH.sub.3).sub.2 3-SCF(CF.sub.3).sub.2 0 A-7873 H H H H H O ?CHN(CH.sub.3).sub.2 2-(cyclopropylthio) 0 A-7874 H H H H H O ?CHN(CH.sub.3).sub.2 2-(cyclopropylsulfinyl) 0 A-7875 H H H H H O ?CHN(CH.sub.3).sub.2 2-(cyclopropylsulfonyl) 0 A-7876 H H H H H O ?CHN(CH.sub.3).sub.2 2-C(?O)Me 0 A-7877 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2C(?O)CH.sub.3 0 A-7878 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2C(?O)CF.sub.3 0 A-7879 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2OH 0 A-7880 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2OCH.sub.3 0 A-7881 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-7882 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2SCH.sub.3 0 A-7883 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2S(?O)CH.sub.3 0 A-7884 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-7885 H H H H H O ?CHN(CH.sub.3).sub.2 2-(benzyloxy) 0 A-7886 H H H H H O ?CHN(CH.sub.3).sub.2 2-NH.sub.2 0 A-7887 H H H H H O ?CHN(CH.sub.3).sub.2 2-NHMe 0 A-7888 H H H H H O ?CHN(CH.sub.3).sub.2 2-N(Me).sub.2 0 A-7889 H H H H H O ?CHN(CH.sub.3).sub.2 2-(1,3-dioxolan-2-yl) 0 A-7890 H H H H H O ?CHN(CH.sub.3).sub.2 2-(1,3-dioxan-2-yl) 0 A-7891 H H H H H O ?CHN(CH.sub.3).sub.2 2-(1H-imidazol-2-yl) 0 A-7892 H H H H H H ?CHN(CH.sub.3).sub.2 2-(thiazol-2-yl) 0 A-7893 H H H H H H ?CHN(CH.sub.3).sub.2 2-(oxazol-2-yl) 0 A-7894 H H H H H H ?CHN(CH.sub.3).sub.2 2-CH?NOH 0 A-7895 H H H H H H ?CHN(CH.sub.3).sub.2 2-CH?NOMe 0 A-7896 H H H H H H ?CHN(CH.sub.3).sub.2 2-(4,5-dihydro-3-isoxazolyl) 0 A-7897 H H H H H H ?CHN(CH.sub.3).sub.2 2-CN 0 A-7898 H H H H H H ?CHN(CH.sub.3).sub.2 2-NO.sub.2 0 A-7899 H H H H H H ?CHN(CH.sub.3).sub.2 2-F,6-Cl 0 A-7900 H H H H H H ?CHN(CH.sub.3).sub.2 2-F,6-Me 0 A-7901 H H H H H H ?CHN(CH.sub.3).sub.2 3-F,6-Me 0 A-7902 H H H H H H ?CHN(CH.sub.3).sub.2 4-F,2-Me 0 A-7903 H H H H H H ?CHN(CH.sub.3).sub.2 2-F,6-OMe 0 A-7904 H H H H H H ?CHN(CH.sub.3).sub.2 3-F,6-OMe 0 A-7905 H H H H H H ?CHN(CH.sub.3).sub.2 2,6-Cl.sub.2 0 A-7906 H H H H H H ?CHN(CH.sub.3).sub.2 2-Cl,6-Me 0 A-7907 H H H H H H ?CHN(CH.sub.3).sub.2 3-Cl,6-Me 0 A-7908 H H H H H H ?CHN(CH.sub.3).sub.2 4-Cl,2-Me 0 A-7909 H H H H H H ?CHN(CH.sub.3).sub.2 2-Cl,5-CF.sub.3 0 A-7910 H H H H H H ?CHN(CH.sub.3).sub.2 2-Cl,6-CF.sub.3 0 A-7911 H H H H H H ?CHN(CH.sub.3).sub.2 2-Cl,6-OMe 0 A-7912 H H H H H H ?CHN(CH.sub.3).sub.2 3-Cl,6-OMe 0 A-7913 H H H H H H ?CHN(CH.sub.3).sub.2 4-Cl,2-OMe 0 A-7914 H H H H H H ?CHN(CH.sub.3).sub.2 2,4-Me.sub.2 0 A-7915 H H H H H H ?CHN(CH.sub.3).sub.2 2,5-Me.sub.2 0 A-7916 H H H H H H ?CHN(CH.sub.3).sub.2 2,6-Me.sub.2 0 A-7917 H H H H H H ?CHN(CH.sub.3).sub.2 2-Me,4-CF.sub.3 0 A-7918 H H H H H H ?CHN(CH.sub.3).sub.2 2-Me,5-CF.sub.3 0
(241) TABLE-US-00140 TABLE 140 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7919 H H H H H O ?CHN(CH.sub.3).sub.2 2-Me, 6-CF.sub.3 O A-7920 H H H H H O ?CHN(CH.sub.3).sub.2 2-Me, 4-OMe O A-7921 H H H H H O ?CHN(CH.sub.3).sub.2 2-Me, 5-Me O A-7922 H H H H H O ?CHN(CH.sub.3).sub.2 2-Me, 6-Me O A-7923 H H H H H O ?CHN(CH.sub.3).sub.2 3-Me, 6-OMe O A-7924 H H H H H O ?CHN(CH.sub.3).sub.2 4-Me, 2-OMe O A-7925 H H H H H O ?CHN(CH.sub.3).sub.2 2,5-OMe.sub.2 O A-7926 H H H H H O ?CHN(CH.sub.3).sub.2 2,6-OMe.sub.2 O A-7927 H H H H H O ?CHN(CH.sub.3).sub.2 2-OMe, 6-CF.sub.3 O A-7928 H H H H H O ?CHN(CH.sub.3).sub.2 2-CHF.sub.2, 5-F O A-7929 H H H H H O ?CHN(CH.sub.3).sub.2 2-CHF.sub.2, 6-F O A-7930 H H H H H O ?CHN(CH.sub.3).sub.2 2-CHF.sub.2, 5-Me O A-7931 H H H H H O ?CHN(CH.sub.3).sub.2 2-CHF.sub.2, 6-Me O A-7932 H H H H H O ?CHN(CH.sub.3).sub.2 2-cyclopropyl, 5-F O A-7933 H H H H H O ?CHN(CH.sub.3).sub.2 2-cyclopropyl, 6-+F O A-7934 H H H H H O ?CHN(CH.sub.3).sub.2 2-cyclopropyl, 5-Me O A-7935 H H H H H O ?CHN(CH.sub.3).sub.2 2-cyclopropyl, 6-Me O A-7936 H H H H H O ?CHN(CH.sub.3).sub.2 2-ethenyl, 6-F O A-7937 H H H H H O ?CHN(CH.sub.3).sub.2 2-ethenyl, 6-Me O A-7938 H H H H H O ?CHN(CH.sub.3).sub.2 2-OEt, 5-F O A-7939 H H H H H O ?CHN(CH.sub.3).sub.2 2-OEt, 6-F O A-7940 H H H H H O ?CHN(CH.sub.3).sub.2 2-OEt, 5-Cl O A-7941 H H H H H O ?CHN(CH.sub.3).sub.2 2-OEt, 6-Cl O A-7942 H H H H H O ?CHN(CH.sub.3).sub.2 2-OEt, 5-Me O A-7943 H H H H H O ?CHN(CH.sub.3).sub.2 2-OEt, 6-Me O A-7944 H H H H H O ?CHN(CH.sub.3).sub.2 2-OCHF.sub.2, 5-F O A-7945 H H H H H O ?CHN(CH.sub.3).sub.2 2-OCHF.sub.2, 6-F O A-7946 H H H H H O ?CHN(CH.sub.3).sub.2 2-OCHF.sub.2, 5-Me O A-7947 H H H H H O ?CHN(CH.sub.3).sub.2 2-OCHF.sub.2, 6-Me O A-7948 H H H H H O ?CHN(CH.sub.3).sub.2 2-(cyclopropyloxy), 5-F O A-7949 H H H H H O ?CHN(CH.sub.3).sub.2 2-(cyclopropyloxy), 6-F O A-7950 H H H H H O ?CHN(CH.sub.3).sub.2 2-(cyclopropyloxy), 5-Me O A-7951 H H H H H O ?CHN(CH.sub.3).sub.2 2-(cyclopropyloxy), 6-Me O A-7952 H H H H H O ?CHN(CH.sub.3).sub.2 2-SMe, 5-F O A-7953 H H H H H O ?CHN(CH.sub.3).sub.2 2-SMe, 6-F O A-7954 H H H H H O ?CHN(CH.sub.3).sub.2 2-SMe, 5-Me O A-7955 H H H H H O ?CHN(CH.sub.3).sub.2 2-SMe, 6-Me O A-7956 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O)Me, 5-F O A-7957 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O)Me, 6-F O A-7958 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O)Me, 5-Me O A-7959 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O)Me, 6-Me O A-7960 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O).sub.2Me, 5-F O A-7961 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O).sub.2Me, 6-F O A-7962 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O).sub.2Me, 5-Me O A-7963 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O).sub.2Me, 6-Me O A-7964 H H H H H O ?CHN(CH.sub.3).sub.2 2-SCF.sub.3, 5-F O A-7965 H H H H H O ?CHN(CH.sub.3).sub.2 2-SCF.sub.3, 6-F O A-7966 H H H H H O ?CHN(CH.sub.3).sub.2 2-SCF.sub.3, 5-Me O A-7967 H H H H H O ?CHN(CH.sub.3).sub.2 2-SCF.sub.3, 6-Me O A-7968 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O)CF.sub.3, 5-F O A-7969 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O)CF.sub.3, 6-F O A-7970 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O)CF.sub.3, 5-Me O A-7971 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O)CF.sub.3, 6-Me O A-7972 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O).sub.2CF.sub.3, 5-F O A-7973 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O).sub.2CF.sub.3, 6-F O A-7974 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O).sub.2CF.sub.3, 5-Me O A-7975 H H H H H O ?CHN(CH.sub.3).sub.2 2-S(?O).sub.2CF.sub.3, 6-Me O
(242) TABLE-US-00141 TABLE 141 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-7976 H H H H H O ?CHN(CH.sub.3).sub.2 2-(cyclopropylthio), 5-F O A-7977 H H H H H O ?CHN(CH.sub.3).sub.2 2-(cyclopropylthio), 6-F O A-7978 H H H H H O ?CHN(CH.sub.3).sub.2 2-(cyclopropylthio), 5-Me O A-7979 H H H H H O ?CHN(CH.sub.3).sub.2 2-(cyclopropylthio), 6-Me O A-7980 H H H H H O ?CHN(CH.sub.3).sub.2 2-C(?O)Me, 5-F O A-7981 H H H H H O ?CHN(CH.sub.3).sub.2 2-C(?O)Me, 6-F O A-7982 H H H H H O ?CHN(CH.sub.3).sub.2 2-C(?O)Me, 5-Me O A-7983 H H H H H O ?CHN(CH.sub.3).sub.2 2-C(?O)Me, 6-Me O A-7984 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2OH, 5-F O A-7985 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2OH, 6-F O A-7986 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2OH, 5-Me O A-7987 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2OH, 6-Me O A-7988 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2OCH.sub.3, 4-F O A-7989 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2OCH.sub.3, 5-F O A-7990 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2OCH.sub.3, 6-F O A-7991 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2OCH.sub.3, 4-Me O A-7992 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2OCH.sub.3, 5-Me O A-7993 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2OCH.sub.3, 6-Me O A-7994 H H H H H O ?CHN(CH.sub.3).sub.2 2-OC(?O)CH.sub.3, 5-F O A-7995 H H H H H O ?CHN(CH.sub.3).sub.2 2-OC(?O)CH.sub.3, 6-F O A-7996 H H H H H O ?CHN(CH.sub.3).sub.2 2-OC(?O)CH.sub.3, 5-Me O A-7997 H H H H H O ?CHN(CH.sub.3).sub.2 2-OC(?O)CH.sub.3, 6-Me O A-7998 H H H H H O ?CHN(CH.sub.3).sub.2 2-OS(?O).sub.2CH.sub.3, 5-F O A-7999 H H H H H O ?CHN(CH.sub.3).sub.2 2-OS(?O).sub.2CH.sub.3, 6-F O A-8000 H H H H H O ?CHN(CH.sub.3).sub.2 2-OS(?O).sub.2CH.sub.3, 5-Me O A-8001 H H H H H O ?CHN(CH.sub.3).sub.2 2-OS(?O).sub.2CH.sub.3, 6-Me O A-8002 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2SCH.sub.3, 5-F O A-8003 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2SCH.sub.3, 6-F O A-8004 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2SCH.sub.3, 5-Me O A-8005 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2SCH.sub.3, 6-Me O A-8006 H H H H H O ?CHN(CH.sub.3).sub.2 2-NMe.sub.2, 5-F O A -8007 H H H H H O ?CHN(CH.sub.3).sub.2 2-NMe.sub.2, 6-F O A-8008 H H H H H O ?CHN(CH.sub.3).sub.2 2-NMe.sub.2, 5-Me O A-8009 H H H H H O ?CHN(CH.sub.3).sub.2 2-NMe.sub.2, 6-Me O A-8010 H H H H H O ?CHN(CH.sub.3).sub.2 2-CN, 4-F O A-8011 H H H H H O ?CHN(CH.sub.3).sub.2 2-CN, 5-F O A-8012 H H H H H O ?CHN(CH.sub.3).sub.2 2-CN, 6-F O A-8013 H H H H H O ?CHN(CH.sub.3).sub.2 2-CN, 6-Me O A-8014 H H H H H O ?CHN(CH.sub.3).sub.2 2-CN, 5-OMe O A-8015 H H H H H O ?CHN(CH.sub.3).sub.2 2-CN, 6-OMe O A-8016 H H H H H O ?CHN(CH.sub.3).sub.2 3-CN, 6-Me O A-8017 H H H H H O ?CHN(CH.sub.3).sub.2 3-CN, 6-OMe O A-8018 H H H H H O ?CHN(CH.sub.3).sub.2 4-CN, 2-Me O A-8019 H H H H H O ?CHN(CH.sub.3).sub.2 4-CN, 2-OMe O A-8020 H H H H H O ?CHN(CH.sub.3).sub.2 2-NO.sub.2, 4-F O A-8021 H H H H H O ?CHN(CH.sub.3).sub.2 2-NO.sub.2, 5-F O A-8022 H H H H H O ?CHN(CH.sub.3).sub.2 2-NO.sub.2, 6-F O A-8023 H H H H H O ?CHN(CH.sub.3).sub.2 2-NO.sub.2, 4-Me O A-8024 H H H H H O ?CHN(CH.sub.3).sub.2 2-NO.sub.2, 5-Me O A-8025 H H H H H O ?CHN(CH.sub.3).sub.2 2-NO.sub.2, 6-Me O A-8026 H H H H H O ?CHN(CH.sub.3).sub.2 2-Me, 4,5-F.sub.2 O A-8027 H H H H H O ?CHN(CH.sub.3).sub.2 2-Me, 6-Et O A-8028 H H H H H O ?CHN(CH.sub.3).sub.2 2-cyclopropyl, 6-OMe O A-8029 H H H H H O ?CHN(CH.sub.3).sub.2 2-Me, 5-Et O A-8030 H H H H H O ?CHN(CH.sub.3).sub.2 2,6-Et.sub.2 O A-8031 H H H H H O ?CHN(CH.sub.3).sub.2 2-Et, 6-F O A-8032 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2OCH.sub.3, 6-Cl O
(243) TABLE-US-00142 TABLE 142 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8033 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2OCH.sub.2CH.sub.3, 6-Cl O A-8034 H H H H H O ?CHN(CH.sub.3).sub.2 2-CH.sub.2NMe.sub.2 O A-8035 H H H H H O CH.sub.3 CH.sub.3 H O A-8036 H H H H H O CH.sub.3 CH.sub.3 2-F O A-8037 H H H H H O CH.sub.3 CH.sub.3 2-Cl O A-8038 H H H H H O CH.sub.3 CH.sub.3 2-Br O A-8039 H H H H H O CH.sub.3 CH.sub.3 2-OH O A-8040 H H H H H O CH.sub.3 CH.sub.3 2-Me O A-8041 H H H H H O CH.sub.3 CH.sub.3 2-Et O A-8042 H H H H H O CH.sub.3 CH.sub.3 2-Pr O A-8043 H H H H H O CH.sub.3 CH.sub.3 2-CF.sub.3 O A-8044 H H H H H O CH.sub.3 CH.sub.3 2-CHF.sub.2 O A-8045 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2F O A-8046 H H H H H O CH.sub.3 CH.sub.3 2-CF.sub.2Cl O A-8047 H H H H H O CH.sub.3 CH.sub.3 2-cyclopropyl O A-8048 H H H H H O CH.sub.3 CH.sub.3 2-cyclobutyl O A-8049 H H H H H O CH.sub.3 CH.sub.3 2-cyclopentyl O A-8050 H H H H H O CH.sub.3 CH.sub.3 2-ethenyl O A-8051 H H H H H O CH.sub.3 CH.sub.3 2-allyl O A-8052 H H H H H O CH.sub.3 CH.sub.3 2-(prop-1-en-1-yl) O A-8053 H H H H H O CH.sub.3 CH.sub.3 2-(trifluoroethenyl) O A-8054 H H H H H O CH.sub.3 CH.sub.3 2-OMe O A-8055 H H H H H O CH.sub.3 CH.sub.3 2-OEt O A-8056 H H H H H O CH.sub.3 CH.sub.3 2-OPr O A-8057 H H H H H O CH.sub.3 CH.sub.3 2-O(i-Pr) O A-8058 H H H H H O CH.sub.3 CH.sub.3 2-OCF.sub.3 O A-8059 H H H H H O CH.sub.3 CH.sub.3 2-OCHF.sub.2 O A-8060 H H H H H O CH.sub.3 CH.sub.3 2-(cyclopropyloxy) O A-8061 H H H H H O CH.sub.3 CH.sub.3 2-(cyclobutyloxy) O A-8062 H H H H H O CH.sub.3 CH.sub.3 2-(cyclopentyloxy) O A-8063 H H H H H O CH.sub.3 CH.sub.3 2-((2,2-dichlorocyclopropyl)oxy) O A-8064 H H H H H O CH.sub.3 CH.sub.3 2-(oxiran-2-yl) O A-8065 H H H H H O CH.sub.3 CH.sub.3 2-SMe O A-8066 H H H H H O CH.sub.3 CH.sub.3 3-SMe O A-8067 H H H H H O CH.sub.3 CH.sub.3 2-S(?O)Me O A-8068 H H H H H O CH.sub.3 CH.sub.3 3-S(?O)Me O A-8069 H H H H H O CH.sub.3 CH.sub.3 2-S(?O ).sub.2Me O A-8070 H H H H H O CH.sub.3 CH.sub.3 3-S(?O).sub.2Me O A-8071 H H H H H O CH.sub.3 CH.sub.3 2-SCF.sub.3 O A-8072 H H H H H O CH.sub.3 CH.sub.3 3-SCF.sub.3 O A-8073 H H H H H O CH.sub.3 CH.sub.3 3-S(?O)CF.sub.3 O A-8074 H H H H H O CH.sub.3 CH.sub.3 3-SCF(CF.sub.3).sub.2 O A-8075 H H H H H O CH.sub.3 CH.sub.3 2-(cyclopropylthio) O A-8076 H H H H H O CH.sub.3 CH.sub.3 2-(cyclopropylsulfinyl) O A-8077 H H H H H O CH.sub.3 CH.sub.3 2-(cyclopropylsulfonyl) O A-8078 H H H H H O CH.sub.3 CH.sub.3 2-C(?O)Me O A-8079 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2C(?O)CH.sub.3 O A-8080 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2C(?O )CF.sub.3 O A-8081 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2OH O A-8082 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2OCH.sub.3 O A-8083 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2OCH.sub.2CH.sub.3 O A-8084 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2SCH.sub.3 O A-8085 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2S(?O)CH.sub.3 O A-8086 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2S(?O).sub.2CH.sub.3 O A-8087 H H H H H O CH.sub.3 CH.sub.3 2-(benzyloxy) O A-8088 H H H H H O CH.sub.3 CH.sub.3 2-NH.sub.2 O A-8089 H H H H H O CH.sub.3 CH.sub.3 2-NHMe O
(244) TABLE-US-00143 TABLE 143 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8090 H H H H H O CH.sub.3 CH.sub.3 2-N(Me).sub.2 O A-8091 H H H H H O CH.sub.3 CH.sub.3 2-(1,3-dioxolan-2-yl) O A-8092 H H H H H O CH.sub.3 CH.sub.3 2-(1,3-dioxan-2-yl) O A-8093 H H H H H O CH.sub.3 CH.sub.3 2-(1H-midazol-2-yl) O A-8094 H H H H H O CH.sub.3 CH.sub.3 2-(thiazol-2-yl) O A-8095 H H H H H O CH.sub.3 CH.sub.3 2-(oxazol-2-yl) O A-8096 H H H H H O CH.sub.3 CH.sub.3 2-CH?NOH O A-8097 H H H H H O CH.sub.3 CH.sub.3 2-CH?NOMe O A-8098 H H H H H O CH.sub.3 CH.sub.3 2-(4,5-dihydro-3-isoxazolyl) O A-8099 H H H H H O CH.sub.3 CH.sub.3 2-CN O A-8100 H H H H H O CH.sub.3 CH.sub.3 2-NO.sub.2 O A-8101 H H H H H O CH.sub.3 CH.sub.3 2-F, 6-Cl O A-8102 H H H H H O CH.sub.3 CH.sub.3 2-F, 6-Me O A-8103 H H H H H O CH.sub.3 CH.sub.3 3-F, 6-Me O A-8104 H H H H H O CH.sub.3 CH.sub.3 4-F, 2-Me O A-8105 H H H H H O CH.sub.3 CH.sub.3 2-F, 6-OMe O A-8106 H H H H H O CH.sub.3 CH.sub.3 3-F, 6-OMe O A-8107 H H H H H O CH.sub.3 CH.sub.3 2,6-Cl.sub.2 O A-8108 H H H H H O CH.sub.3 CH.sub.3 2-Cl, 6-Me O A-8109 H H H H H O CH.sub.3 CH.sub.3 3-Cl, 6-Me O A-8110 H H H H H O CH.sub.3 CH.sub.3 4-Cl, 2-Me O A-8111 H H H H H O CH.sub.3 CH.sub.3 2-Cl, 5-CF.sub.3 O A-8112 H H H H H O CH.sub.3 CH.sub.3 2-Cl, 6-CF.sub.3 O A-8113 H H H H H O CH.sub.3 CH.sub.3 2-Cl, 6-OMe O A-8114 H H H H H O CH.sub.3 CH.sub.3 3-Cl, 6-OMe O A-8115 H H H H H O CH.sub.3 CH.sub.3 4-Cl, 2-OMe O A-8116 H H H H H O CH.sub.3 CH.sub.3 2,4-Me.sub.2 O A-8117 H H H H H O CH.sub.3 CH.sub.3 2,5-Me.sub.2 O A-8118 H H H H H O CH.sub.3 CH.sub.3 2,6-Me.sub.2 O A-8119 H H H H H O CH.sub.3 CH.sub.3 2-Me, 4-CF.sub.3 O A-8120 H H H H H O CH.sub.3 CH.sub.3 2-Me, 5-CF.sub.3 O A-8121 H H H H H O CH.sub.3 CH.sub.3 2-Me, 6-CF.sub.3 O A-8122 H H H H H O CH.sub.3 CH.sub.3 2-Me, 4-OMe O A-8123 H H H H H O CH.sub.3 CH.sub.3 2-Me, 5-OMe O A-8124 H H H H H O CH.sub.3 CH.sub.3 2-Me, 6-OMe O A-8125 H H H H H O CH.sub.3 CH.sub.3 3-Me, 6-OMe O A-8126 H H H H H O CH.sub.3 CH.sub.3 4-Me, 2-OMe O A-8127 H H H H H O CH.sub.3 CH.sub.3 2,5-OMe.sub.2 O A-8128 H H H H H O CH.sub.3 CH.sub.3 2,6-OMe.sub.2 O A-8129 H H H H H O CH.sub.3 CH.sub.3 2-OMe, 6-CF.sub.3 O A-8130 H H H H H O CH.sub.3 CH.sub.3 2-CHF.sub.2, 5-F O A-8131 H H H H H O CH.sub.3 CH.sub.3 2-CHF.sub.2, 6-F O A-8132 H H H H H O CH.sub.3 CH.sub.3 2-CHF.sub.2, 5-Me O A-8133 H H H H H O CH.sub.3 CH.sub.3 2-CHF.sub.2, 6-Me O A-8134 H H H H H O CH.sub.3 CH.sub.3 2-cyclopropyl, 5-F O A-8135 H H H H H O CH.sub.3 CH.sub.3 2-cyclopropyl, 6-F O A-8136 H H H H H O CH.sub.3 CH.sub.3 2-cyclopropyl, 5-Me O A-8137 H H H H H O CH.sub.3 CH.sub.3 2-cyclopropyl, 6-Me O A-8138 H H H H H O CH.sub.3 CH.sub.3 2-ethenyl, 6 F O A-8139 H H H H H O CH.sub.3 CH.sub.3 2-ethenyl, 6-Me O A-8140 H H H H H O CH.sub.3 CH.sub.3 2-OEt, 5-F O A-8141 H H H H H O CH.sub.3 CH.sub.3 2-OEt, 6-F O A-8142 H H H H H O CH.sub.3 CH.sub.3 2-OEt, 5-Cl O A-8143 H H H H H O CH.sub.3 CH.sub.3 2-OEt, 6-Cl O A-8144 H H H H H O CH.sub.3 CH.sub.3 2-OEt, 5-Me O A-8145 H H H H H O CH.sub.3 CH.sub.3 2-OEt, 6-Me O A-8146 H H H H H O CH.sub.3 CH.sub.3 2-OCHF.sub.2, 5-F O
(245) TABLE-US-00144 TABLE 144 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8147 H H H H H O CH.sub.3 CH.sub.3 2-OCHF.sub.2, 6-F O A-8148 H H H H H O CH.sub.3 CH.sub.3 2-OCHF.sub.2, 5-Me O A-8149 H H H H H O CH.sub.3 CH.sub.3 2-OCHF.sub.2, 6-Me O A-8150 H H H H H O CH.sub.3 CH.sub.3 2-(cyclopropyloxy), 5-F O A-8151 H H H H H O CH.sub.3 CH.sub.3 2-(cyclopropyloxy), 6-F O A-8152 H H H H H O CH.sub.3 CH.sub.3 2-(cyclopropyloxy), 5-Me O A-8153 H H H H H O CH.sub.3 CH.sub.3 2-(cyclopropyloxy), 6-Me O A-8154 H H H H H O CH.sub.3 CH.sub.3 2-SMe, 5-F O A-8155 H H H H H O CH.sub.3 CH.sub.3 2-SMe, 6-F O A-8156 H H H H H O CH.sub.3 CH.sub.3 2-SMe, 5-Me O A-8157 H H H H H O CH.sub.3 CH.sub.3 2-SMe, 6-Me O A-8158 H H H H H O CH.sub.3 CH.sub.3 2-S(?O)Me,5-F O A-8159 H H H H H O CH.sub.3 CH.sub.3 2-S(?O)Me, 6-F O A-8160 H H H H H O CH.sub.3 CH.sub.3 2-S(?O)Me, 5-Me O A-8161 H H H H H O CH.sub.3 CH.sub.3 2-S(?O)Me, 6-Me O A-8162 H H H H H O CH.sub.3 CH.sub.3 2-S(?O).sub.2Me, 5-F O A-8163 H H H H H O CH.sub.3 CH.sub.3 2-S(?O).sub.2Me, 6-F O A-8164 H H H H H O CH.sub.3 CH.sub.3 2-S(?O).sub.2Me, 5-Me O A -8165 H H H H H O CH.sub.3 CH.sub.3 2-S(?O).sub.2Me, 6-Me O A-8166 H H H H H O CH.sub.3 CH.sub.3 2-SCF.sub.3, 5-F O A-8167 H H H H H O CH.sub.3 CH.sub.3 2-SCF.sub.3, 6-F O A 8168 H H H H H O CH.sub.3 CH.sub.3 2-SCF.sub.3, 5-Me O A-8169 H H H H H O CH.sub.3 CH.sub.3 2-SCF.sub.3, 6-Me O A-8170 H H H H H O CH.sub.3 CH.sub.3 2-S(?O)CF.sub.3, 5-F O A-8171 H H H H H O CH.sub.3 CH.sub.3 2-S(?O)CF.sub.3, 6-F O A-8172 H H H H H O CH.sub.3 CH.sub.3 2-S(?O)CF.sub.3, 5-Me O A-8173 H H H H H O CH.sub.3 CH.sub.3 2-S(?O)CF.sub.3, 6-Me O A-8174 H H H H H O CH.sub.3 CH.sub.3 2-S(?O).sub.2CF.sub.3, 5-F O A-8175 H H H H H O CH.sub.3 CH.sub.3 2-S(?O).sub.2CF.sub.3, 6-F O A-8176 H H H H H O CH.sub.3 CH.sub.3 2-S(?O).sub.2CF.sub.3, 5-Me O A-8177 H H H H H O CH.sub.3 CH.sub.3 2-S(?O).sub.2CF.sub.3, 6-Me O A-8178 H H H H H O CH.sub.3 CH.sub.3 2-(cyclopropylthio), 5-F O A-8179 H H H H H O CH.sub.3 CH.sub.3 2-(cyclopropylthio), 6-F O A 8180 H H H H H O CH.sub.3 CH.sub.3 2-(cyclopropylthio), 5-Me O A-8181 H H H H H O CH.sub.3 CH.sub.3 2-(cyclopropylthio), 6-Me O A-8182 H H H H H O CH.sub.3 CH.sub.3 2-C(?O)Me, 5-F O A-8183 H H H H H O CH.sub.3 CH.sub.3 2-C(?O)Me, 6-F O A-8184 H H H H H O CH.sub.3 CH.sub.3 2-C(?O)Me, 5-Me O A-8185 H H H H H O CH.sub.3 CH.sub.3 2-C(?O)Me, 6-Me O A-8186 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2OH, 5-F O A-8187 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2OH, 6-F O A-8188 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2OH, 5-Me O A-8189 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2OH, 6-Me O A-8190 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2OCH.sub.3, 4-F O A-8191 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2OCH.sub.3, 5-F O A-8192 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2OCH.sub.3, 6-F O A-8193 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2OCH.sub.3, 4-Me O A-8194 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2OCH.sub.3, 5-Me O A-8195 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2OCH.sub.3, 6-Me O A-8196 H H H H H O CH.sub.3 CH.sub.3 2-OC(?O)CH.sub.3, 5-F O A-8197 H H H H H O CH.sub.3 CH.sub.3 2-OC(?O)CH.sub.3, 6-F O A-8198 H H H H H O CH.sub.3 CH.sub.3 2-OC(?O)CH.sub.3, 5-Me O A-8199 H H H H H O CH.sub.3 CH.sub.3 2-OC(?O)CH.sub.3, 6-Me O A-8200 H H H H H O CH.sub.3 CH.sub.3 2-OS(?O).sub.2CH.sub.3, 5-F O A-8201 H H H H H O CH.sub.3 CH.sub.3 2-OS(?O).sub.2CH.sub.3, 6-F O A-8202 H H H H H O CH.sub.3 CH.sub.3 2-OS(?O).sub.2CH.sub.3, 5-Me O A-8203 H H H H H O CH.sub.3 CH.sub.3 2-OS(?O)2CH.sub.3, 6-Me O
(246) TABLE-US-00145 TABLE 145 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8204 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2SCH.sub.3, 5-F O A-8205 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2SCH.sub.3, 6-F O A-8206 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2SCH.sub.3, 5-Me O A-8207 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2SCH.sub.3, 6-Me O A-8208 H H H H H O CH.sub.3 CH.sub.3 2-NMe.sub.2, 5-F O A-8209 H H H H H O CH.sub.3 CH.sub.3 2-NMe.sub.2, 6-F O A-8210 H H H H H O CH.sub.3 CH.sub.3 2-NMe.sub.2, 5-Me O A-8211 H H H H H O CH.sub.3 CH.sub.3 2-NMe.sub.2, 6-Me O A-8212 H H H H H O CH.sub.3 CH.sub.3 2-CN, 4-F O A-8213 H H H H H O CH.sub.3 CH.sub.3 2-CN, 5-F O A 8214 H H H H H O CH.sub.3 CH.sub.3 2-CN, 6-F O A-8215 H H H H H O CH.sub.3 CH.sub.3 2-CN,6-Me O A-8216 H H H H H O CH.sub.3 CH.sub.3 2-CN, 5-OMe O A-8217 H H H H H O CH.sub.3 CH.sub.3 2-CN, 6-OMe O A-8218 H H H H H O CH.sub.3 CH.sub.3 3-CN, 6-Me O A-8219 H H H H H O CH.sub.3 CH.sub.3 3-CN, 6-OMe O A-8220 H H H H H O CH.sub.3 CH.sub.3 4-CN, 2-Me O A-8221 H H H H H O CH.sub.3 CH.sub.3 4-CN, 2-OMe O A-8222 H H H H H O CH.sub.3 CH.sub.3 2-NO.sub.2, 4-F O A-8223 H H H H H O CH.sub.3 CH.sub.3 2-NO.sub.2, 5-F O A-8224 H H H H H O CH.sub.3 CH.sub.3 2-NO.sub.2, 6-F O A-8225 H H H H H O CH.sub.3 CH.sub.3 2-NO.sub.2, 4-Me O A-8226 H H H H H O CH.sub.3 CH.sub.3 2-NO.sub.2, 5-Me O A-8227 H H H H H O CH.sub.3 CH.sub.3 2-NO.sub.2, 6-Me O A-8228 H H H H H O CH.sub.3 CH.sub.3 2-Me, 4,5-F.sub.2 O A-8229 H H H H H O CH.sub.3 CH.sub.3 2-Me, 6-Et O A-8230 H H H H H O CH.sub.3 CH.sub.3 2-cyclopropyl, 6-OMe O A-8231 H H H H H O CH.sub.3 CH.sub.3 2-Me, 5-Et O A-8232 H H H H H O CH.sub.3 CH.sub.3 2,6-Et.sub.2 O A-8233 H H H H H O CH.sub.3 CH.sub.3 2-Et, 6-F O A-8234 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2OCH.sub.3, 6-Cl O A-8235 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2OCH.sub.2CH.sub.3, 6-Cl O A-8236 H H H H H O CH.sub.3 CH.sub.3 2-CH.sub.2NMe.sub.2 O A-8237 H H H H H O CH.sub.2CN CH.sub.2CN H O A-8238 H H H H H O CH.sub.2CN CH.sub.2CN 2-F O A-8239 H H H H H O CH.sub.2CN CH.sub.2CN 2-Cl O A-8240 H H H H H O CH.sub.2CN CH.sub.2CN 2-Br O A-8241 H H H H H O CH.sub.2CN CH.sub.2CN 2-OH O A-8242 H H H H H O CH.sub.2CN CH.sub.2CN 2-Me O A-8243 H H H H H O CH.sub.2CN CH.sub.2CN 2-Et O A-8244 H H H H H O CH.sub.2CN CH.sub.2CN 2-Pr O A-8245 H H H H H O CH.sub.2CN CH.sub.2CN 2-CF.sub.3 O A-8246 H H H H H O CH.sub.2CN CH.sub.2CN 2-CHF.sub.2 O A-8247 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2F O A-8248 H H H H H O CH.sub.2CN CH.sub.2CN 2-CF.sub.2Cl O A-8249 H H H H H O CH.sub.2CN CH.sub.2CN 2-cyclopropyl O A-8250 H H H H H O CH.sub.2CN CH.sub.2CN 2 -cyclobutyl O A-8251 H H H H H O CH.sub.2CN CH.sub.2CN 2-cyclopentyl O A-8252 H H H H H O CH.sub.2CN CH.sub.2CN 2-ethenyl O A-8253 H H H H H O CH.sub.2CN CH.sub.2CN 2-allyl O A-8254 H H H H H O CH.sub.2CN CH.sub.2CN 2-(prop-1-en-1-yl) O A-8255 H H H H H O CH.sub.2CN CH.sub.2CN 2-(trifluoroethenyl) O A-8256 H H H H H O CH.sub.2CN CH.sub.2CN 2-OMe O A-8257 H H H H H O CH.sub.2CN CH.sub.2CN 2-OEt O A-8258 H H H H H O CH.sub.2CN CH.sub.2CN 2-OPr O A-8259 H H H H H O CH.sub.2CN CH.sub.2CN 2-O(i-Pr) O A-8260 H H H H H O CH.sub.2CN CH.sub.2CN 2-OCF.sub.3 O
(247) TABLE-US-00146 TABLE 146 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8261 H H H H H O CH.sub.2CN CH.sub.2CN 2-OCHF.sub.2 O A-8262 H H H H H O CH.sub.2CN CH.sub.2CN 2-(cyclopropyboxy) O A-8263 H H H H H O CH.sub.2CN CH.sub.2CN 2-(cyclobutyloxy) O A-8264 H H H H H O CH.sub.2CN CH.sub.2CN 2-(cyclopentyloxy) O A-8265 H H H H H O CH.sub.2CN CH.sub.2CN 2-((2,2-dichlorocyclopropyl)oxy) O A 8266 H H H H H O CH.sub.2CN CH.sub.2CN 2-(oxiran-2-yl) O A-8267 H H H H H O CH.sub.2CN CH.sub.2CN 2-SMe O A-8268 H H H H H O CH.sub.2CN CH.sub.2CN 3-SMe O A-8269 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O)Me O A-8270 H H H H H O CH.sub.2CN CH.sub.2CN 3-S(?O)Me O A-8271 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O).sub.2Me O A-8272 H H H H H O CH.sub.2CN CH.sub.2CN 3-S(?O).sub.2Me O A-8273 H H H H H O CH.sub.2CN CH.sub.2CN 2-SCF.sub.3 O A-8274 H H H H H O CH.sub.2CN CH.sub.2CN 3-SCF.sub.3 O A-8275 H H H H H O CH.sub.2CN CH.sub.2CN 3-S(?O)CF.sub.3 O A-8276 H H H H H O CH.sub.2CN CH.sub.2CN 3-SCF(CF.sub.3).sub.2 O A-8277 H H H H H O CH.sub.2CN CH.sub.2CN 2-(cyclopropylthio) O A-8278 H H H H H O CH.sub.2CN CH.sub.2CN 2-(cyclopropylsulfinyl) O A-8279 H H H H H O CH.sub.2CN CH.sub.2CN 2-(cyclopropylsulfonyl) O A-8280 H H H H H O CH.sub.2CN CH.sub.2CN 2-C(?O)Me O A-8281 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2C(?O)CH.sub.3 O A-8282 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2C(?O)CF.sub.3 O A-8283 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2OH O A-8284 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2OCH.sub.3 O A-8285 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2OCH.sub.2CH.sub.3 O A-8286 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2SCH.sub.3 O A-8287 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2S(?O)CH.sub.3 O A-8288 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2S(?O).sub.2CH.sub.3 O A-8289 H H H H H O CH.sub.2CN CH.sub.2CN 2-(benzyloxy) O A-8290 H H H H H O CH.sub.2CN CH.sub.2CN 2-NH.sub.2 O A-8291 H H H H H O CH.sub.2CN CH.sub.2CN 2-NHMe O A-8292 H H H H H O CH.sub.2CN CH.sub.2CN 2-N(Me).sub.2 O A-8293 H H H H H O CH.sub.2CN CH.sub.2CN 2-(1,3-dioxolan-2-yl) O A-8294 H H H H H O CH.sub.2CN CH.sub.2CN 2-(1,3-dioxan-2-yl) O A-8295 H H H H H O CH.sub.2CN CH.sub.2CN 2-(1H-midazol-2-yl) O A-8296 H H H H H O CH.sub.2CN CH.sub.2CN 2-(thiazol-2-yl) O A-8297 H H H H H O CH.sub.2CN CH.sub.2CN 2-(oxazol-2-yl) O A-8298 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH?NOH O A-8299 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH?NOMe O A-8300 H H H H H O CH.sub.2CN CH.sub.2CN 2-(4,5-dihydro-3-isoxazolyl) O A-8301 H H H H H O CH.sub.2CN CH.sub.2CN 2-CN O A-8302 H H H H H O CH.sub.2CN CH.sub.2CN 2-NO.sub.2 O A-8303 H H H H H O CH.sub.2CN CH.sub.2CN 2-F, 6-Cl O A-8304 H H H H H O CH.sub.2CN CH.sub.2CN 2-F, 6-Me O A-8305 H H H H H O CH.sub.2CN CH.sub.2CN 3-F, 6-Me O A-8306 H H H H H O CH.sub.2CN CH.sub.2CN 4-F, 2-Me O A-8307 H H H H H O CH.sub.2CN CH.sub.2CN 2-F, 6-OMe O A-8308 H H H H H O CH.sub.2CN CH.sub.2CN 3-F, 6-OMe O A-8309 H H H H H O CH.sub.2CN CH.sub.2CN 2,6-Cl.sub.2 O A-8310 H H H H H O CH.sub.2CN CH.sub.2CN 2-Cl, 6-Me O A-8311 H H H H H O CH.sub.2CN CH.sub.2CN 3-Cl, 6-Me O A-8312 H H H H H O CH.sub.2CN CH.sub.2CN 4-Cl, 2-Me O A-8313 H H H H H O CH.sub.2CN CH.sub.2CN 2-Cl, 5-CF.sub.3 O A-8314 H H H H H O CH.sub.2CN CH.sub.2CN 2-Cl, 6-CF.sub.3 O A-8315 H H H H H O CH.sub.2CN CH.sub.2CN 2-Cl, 6-OMe O A-8316 H H H H H O CH.sub.2CN CH.sub.2CN 3-Cl, 6-OMe O A-8317 H H H H H O CH.sub.2CN CH.sub.2CN 4-Cl, 2-OMe O
(248) TABLE-US-00147 TABLE 147 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8318 H H H H H O CH.sub.2CN CH.sub.2CN 2,4-Me.sub.2 O A-8319 H H H H H O CH.sub.2CN CH.sub.2CN 2,5-Me.sub.2 O A-8320 H H H H H O CH.sub.2CN CH.sub.2CN 2,6-Me.sub.2 O A-8321 H H H H H O CH.sub.2CN CH.sub.2CN 2-Me, 4-CF.sub.3 O A-8322 H H H H H O CH.sub.2CN CH.sub.2CN 2-Me, 5 CF.sub.3 O A-8323 H H H H H O CH.sub.2CN CH.sub.2CN 2-Me, 6-CF.sub.3 O A-8324 H H H H H O CH.sub.2CN CH.sub.2CN 2-Me, 4-OMe O A-8325 H H H H H O CH.sub.2CN CH.sub.2CN 2-Me, 5-OMe O A-8326 H H H H H O CH.sub.2CN CH.sub.2CN 2-Me, 6-OMe O A-8327 H H H H H O CH.sub.2CN CH.sub.2CN 3-Me, 6-OMe O A-8328 H H H H H O CH.sub.2CN CH.sub.2CN 4-Me, 2-OMe O A-8329 H H H H H O CH.sub.2CN CH.sub.2CN 2,5-OMe.sub.2 O A-8330 H H H H H O CH.sub.2CN CH.sub.2CN 2,6-OMe.sub.2 O A-8331 H H H H H O CH.sub.2CN CH.sub.2CN 2-OMe, 6-CF.sub.3 O A-8332 H H H H H O CH.sub.2CN CH.sub.2CN 2-CHF.sub.2, 5-F O A-8333 H H H H H O CH.sub.2CN CH.sub.2CN 2-CHF.sub.2, 6-F O A-8334 H H H H H O CH.sub.2CN CH.sub.2CN 2-CHF.sub.2, 5-Me O A-8335 H H H H H O CH.sub.2CN CH.sub.2CN 2-CHF.sub.2, 6-Me O A-8336 H H H H H O CH.sub.2CN CH.sub.2CN 2-cyclopropyl, 5-F O A-8337 H H H H H O CH.sub.2CN CH.sub.2CN 2-cyclopropyl, 6-F O A-8338 H H H H H O CH.sub.2CN CH.sub.2CN 2-cyclopropyl, 5-Me O A-8339 H H H H H O CH.sub.2CN CH.sub.2CN 2-cyclopropyl, 6-Me O A-8340 H H H H H O CH.sub.2CN CH.sub.2CN 2-ethenyl, 6-F O A-8341 H H H H H O CH.sub.2CN CH.sub.2CN 2-ethenyl, 6-Me O A-8342 H H H H H O CH.sub.2CN CH.sub.2CN 2-OEt, 5-F O A-8343 H H H H H O CH.sub.2CN CH.sub.2CN 2-OEt, 6-F O A-8344 H H H H H O CH.sub.2CN CH.sub.2CN 2-OEt, 5-Cl O A-8345 H H H H H O CH.sub.2CN CH.sub.2CN 2-OEt, 6-Cl O A-8346 H H H H H O CH.sub.2CN CH.sub.2CN 2-OEt, 5-Me O A-8347 H H H H H O CH.sub.2CN CH.sub.2CN 2-OEt, 6-Me O A-8348 H H H H H O CH.sub.2CN CH.sub.2CN 2-OCHF.sub.2, 5-F O A-8349 H H H H H O CH.sub.2CN CH.sub.2CN 2-OCHF.sub.2, 6-F O A-8350 H H H H H O CH.sub.2CN CH.sub.2CN 2-OCHF.sub.2, 5-Me O A-8351 H H H H H O CH.sub.2CN CH.sub.2CN 2-OCHF.sub.2, 6-Me O A-8352 H H H H H O CH.sub.2CN CH.sub.2CN 2-(cyclopropyloxy), 5-F O A-8353 H H H H H O CH.sub.2CN CH.sub.2CN 2-(cyclopropyloxy), 6-F O A-8354 H H H H H O CH.sub.2CN CH.sub.2CN 2-(cyclopropyloxy), 5-Me O A-8355 H H H H H O CH.sub.2CN CH.sub.2CN 2-(cyclopropyloxy), 6-Me O A-8356 H H H H H O CH.sub.2CN CH.sub.2CN 2-SMe, 5-F O A-8357 H H H H H O CH.sub.2CN CH.sub.2CN 2-SMe, 6-F O A-8358 H H H H H O CH.sub.2CN CH.sub.2CN 2-SMe, 5-Me O A-8359 H H H H H O CH.sub.2CN CH.sub.2CN 2-SMe, 6-Me O A-8360 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O)Me, 5-F O A-8361 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O)Me, 6-F O A-8362 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O)Me, 5-Me O A-8363 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O)Me, 6-Me O A-8364 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O).sub.2Me, 5-F O A-8365 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O).sub.2Me, 6-F O A-8366 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O).sub.2Me, 5-Me O A-8367 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O).sub.2Me, 6-Me O A-8368 H H H H H O CH.sub.2CN CH.sub.2CN 2-SCF.sub.3, 5-F O A-8369 H H H H H O CH.sub.2CN CH.sub.2CN 2-SCF.sub.3, 6-F O A-8370 H H H H H O CH.sub.2CN CH.sub.2CN 2-SCF.sub.3, 5-Me O A-8371 H H H H H O CH.sub.2CN CH.sub.2CN 2-SCF.sub.3, 6-Me O A-8372 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O)CF.sub.3, 5-F O A-8373 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O)CF.sub.3, 6-F O A-8374 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O)CF.sub.3, 5-Me O
(249) TABLE-US-00148 TABLE 148 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8375 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O)CF.sub.3, 6-Me O A-8376 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O).sub.2CF.sub.3, 5-F O A-8377 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O).sub.2CF.sub.3, 6-F O A-8378 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O).sub.2CF.sub.3, 5-Me O A-8379 H H H H H O CH.sub.2CN CH.sub.2CN 2-S(?O).sub.2CF.sub.3, 6-Me O A-8380 H H H H H O CH.sub.2CN CH.sub.2CN 2-(cyclopropylthio), 5-F O A-8381 H H H H H O CH.sub.2CN CH.sub.2CN 2-(cyclopropylthio), 6-F O A-8382 H H H H H O CH.sub.2CN CH.sub.2CN 2-(cyclopropylthio), 5-Me O A-8383 H H H H H O CH.sub.2CN CH.sub.2CN 2-(cyclopropylthio), 6-Me O A-8384 H H H H H O CH.sub.2CN CH.sub.2CN 2-C(?O)Me, 5-F O A-8385 H H H H H O CH.sub.2CN CH.sub.2CN 2-C(?O)Me, 6-F O A-8386 H H H H H O CH.sub.2CN CH.sub.2CN 2-C(?O)Me, 5-Me O A-8387 H H H H H O CH.sub.2CN CH.sub.2CN 2-C(?O)Me, 6-Me O A-8388 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2OH, 5-F O A-8389 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2OH, 6-F O A-8390 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2OH, 5-Me O A-8391 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2OH, 6-Me O A-8392 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2OCH.sub.3, 4-F O A-8393 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2OCH.sub.3, 5-F O A-8394 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2OCH.sub.3, 6-F O A-8395 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2OCH.sub.3, 4-Me O A-8396 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2OCH.sub.3, 5-Me O A-8397 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2OCH.sub.3, 6-Me O A-8398 H H H H H O CH.sub.2CN CH.sub.2CN 2-OC(?O)CH.sub.3, 5-F O A-8399 H H H H H O CH.sub.2CN CH.sub.2CN 2-OC(?O)CH.sub.3, 6-F O A-8400 H H H H H O CH.sub.2CN CH.sub.2CN 2-OC(?O)CH.sub.3, 5 Me O A-8401 H H H H H O CH.sub.2CN CH.sub.2CN 2-OC(?O)CH.sub.3, 6-Me O A-8402 H H H H H O CH.sub.2CN CH.sub.2CN 2-OS(?O).sub.2CH.sub.3, 5-F O A-8403 H H H H H O CH.sub.2CN CH.sub.2CN 2-OS(?O).sub.2CH.sub.3, 6-F O A-8404 H H H H H O CH.sub.2CN CH.sub.2CN 2-OS(?O).sub.2CH.sub.3,5-Me O A-8405 H H H H H O CH.sub.2CN CH.sub.2CN 2-OS(?O).sub.2CH.sub.3, 6-Me O A-8406 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2SCH.sub.3, 5-F O A-8407 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2SCH.sub.3, 6-F O A-8408 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2SCH.sub.3, 5-Me O A-8409 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2SCH.sub.3, 6-Me O A-8410 H H H H H O CH.sub.2CN CH.sub.2CN 2-NMe.sub.2, 5-F O A-8411 H H H H H O CH.sub.2CN CH.sub.2CN 2-NMe.sub.2, 6-F O A-8412 H H H H H O CH.sub.2CN CH.sub.2CN 2-NMe.sub.2, 5-Me O A-8413 H H H H H O CH.sub.2CN CH.sub.2CN 2-NMe.sub.2, 6-Me O A-8414 H H H H H O CH.sub.2CN CH.sub.2CN 2-CN, 4-F O A-8415 H H H H H O CH.sub.2CN CH.sub.2CN 2-CN, 5-F O A-8416 H H H H H O CH.sub.2CN CH.sub.2CN 2-CN, 6-F O A-8417 H H H H H O CH.sub.2CN CH.sub.2CN 2-CN, 6-Me O A-8418 H H H H H O CH.sub.2CN CH.sub.2CN 2-CN, 5-OMe O A-8419 H H H H H O CH.sub.2CN CH.sub.2CN 2-CN, 6-OMe O A-8420 H H H H H O CH.sub.2CN CH.sub.2CN 3-CN, 6-Me O A-8421 H H H H H O CH.sub.2CN CH.sub.2CN 3-CN, 6-OMe O A-8422 H H H H H O CH.sub.2CN CH.sub.2CN 4-CN, 2-Me O A-8423 H H H H H O CH.sub.2CN CH.sub.2CN 4-CN, 2-OMe O A-8424 H H H H H O CH.sub.2CN CH.sub.2CN 2-NO.sub.2, 4-F O A-8425 H H H H H O CH.sub.2CN CH.sub.2CN 2-NO.sub.2, 5-F O A-8426 H H H H H O CH.sub.2CN CH.sub.2CN 2-NO.sub.2, 6-F O A-8427 H H H H H O CH.sub.2CN CH.sub.2CN 2-NO.sub.2, 4-Me O A-8428 H H H H H O CH.sub.2CN CH.sub.2CN 2-NO.sub.2, 5-Me O A-8429 H H H H H O CH.sub.2CN CH.sub.2CN 2-NO.sub.2, 6-Me O A-8430 H H H H H O CH.sub.2CN CH.sub.2CN 2-Me, 4,5-F.sub.2 O A-8431 H H H H H O CH.sub.2CN CH.sub.2CN 2-Me, 6-Et O
(250) TABLE-US-00149 TABLE 149 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8432 H H H H H O CH.sub.2CN CH.sub.2CN 2-cyclopropyl, 6-OMe O A-8433 H H H H H O CH.sub.2CN CH.sub.2CN 2-Me, 5-Et O A-8434 H H H H H O CH.sub.2CN CH.sub.2CN 2,6-Et.sub.2 O A-8435 H H H H H O CH.sub.2CN CH.sub.2CN 2-Et, 6-F O A-8436 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2OCH.sub.3, 6-Cl O A-8437 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2OCH.sub.2CH.sub.3, 6-Cl O A-8438 H H H H H O CH.sub.2CN CH.sub.2CN 2-CH.sub.2NMe.sub.2 O A-8439 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 H O A-8440 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-F O A-8441 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Cl O A-8442 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Br O A-8443 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OH O A-8444 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Me O A-8445 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Et O A-8446 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Pr O A-8447 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CF.sub.3 O A-8448 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CHF.sub.2 O A-8449 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2F O A-8450 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CF.sub.2Cl O A-8451 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-cyclopropyl O A-8452 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2 -cyclobutyl O A-8453 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2 -cyclopentyl O A-8454 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-ethenyl O A-8455 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-allyl O A-8456 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(prop-1-en-1-yl) O A-8457 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(trifluoroethenyl) O A-8458 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OMe O A-8459 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OEt O A-8460 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OPr O A-8461 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-O(i-Pr) O A-8462 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OCF.sub.3 O A-8463 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OCHF.sub.2 O A-8464 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(cyclopropyloxy) O A-8465 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(cyclobutyloxy) O A-8466 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(cyclopentyloxy) O A-8467 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-((2,2-dichlorocyclopropyl)oxy) O A-8468 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(oxiran-2-yl) O A-8469 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-SMe O A-8470 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 3-SMe O A-8471 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O)Me O A-8472 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 3-S(?O)Me O A-8473 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O).sub.2Me O A-8474 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 3-S(?O).sub.2Me O A-8475 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-SCF.sub.3 O A-8476 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 3-SCF.sub.3 O A-8477 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 3-S(?O)CF.sub.3 O A-8478 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 3-SCF(CF.sub.3).sub.2 O A-8479 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(cyclopropylthio) O A-8480 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(cyclopropylsulfinyl) O A-8481 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(cyclopropylsulfonyl) O A-8482 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-C(?O)Me O A-8483 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2C(?O)CH.sub.3 O A-8484 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2C(?O)CF.sub.3 O A-8485 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2OH O A-8486 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2OCH.sub.3 O A-8487 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2OCH.sub.2CH.sub.3 O A-8488 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2SCH.sub.3 O
(251) TABLE-US-00150 TABLE 150 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8489 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2S(?O)CH.sub.3 0 A-8490 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-8491 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(benzyloxy) 0 A-8492 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-NH.sub.2 0 A-8493 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-NHMe 0 A-8494 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-N(Me).sub.2 0 A-8495 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(1,3-dioxolan-2-yl) 0 A-8496 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(1,3-dioxan-2-yl) 0 A-8497 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(1,3-imidazol-2-yl) 0 A-8498 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(thiazol-2-yl) 0 A-8499 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(oxazol-2-yl) 0 A-8500 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH?NOH 0 A-8501 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH?NOMe 0 A-8502 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(4,5-dihydro-3-isoxazolyl) 0 A-8503 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CN 0 A-8504 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-NO.sub.2 0 A-8505 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-F,6-Cl 0 A-8506 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2,6-Me 0 A-8507 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 3-F,6-Me 0 A-8508 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 4-F,2-Me 0 A-8509 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-F,6-OMe 0 A-8510 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 3-F,6-OMe 0 A-8511 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2,6-Cl.sub.2 0 A-8512 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Cl,6-Me 0 A-8513 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 3-Cl,6-Me 0 A-8514 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 4-Cl,2-Me 0 A-8515 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Cl,5-CF.sub.3 0 A-8516 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Cl,6-CF.sub.3 0 A-8517 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Cl,6-OMe 0 A-8518 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 3-Cl,6-OMe 0 A-8519 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 4-Cl,2-OMe 0 A-8520 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2,4-Me.sub.2 0 A-8521 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2,5-Me.sub.2 0 A-8522 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2,6-Me.sub.2 0 A-8523 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Me,4-CF.sub.3 0 A-8524 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Me,5-CF.sub.3 0 A-8525 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Me,6-CF.sub.3 0 A-8526 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Me,4-OMe 0 A-8527 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Me,5-OMe 0 A-8528 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Me,6-OMe 0 A-8529 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 3-Me,6-OMe 0 A-8530 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 4-Me,2-OMe 0 A-8531 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2,5-OMe.sub.2 0 A-8532 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2,6-OMe.sub.2 0 A-8533 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OMe,6-CF.sub.3 0 A-8534 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CHF.sub.2,5-F 0 A-8535 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CHF.sub.2,6-F 0 A-8536 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CHF.sub.2,5-Me 0 A-8537 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CHF.sub.2,6-Me 0 A-8538 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-cyclopropyl,5-F 0 A-8539 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-cyclopropyl,6-F 0 A-8540 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-cyclopropyl,5-Me 0 A-8541 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-cyclopropyl,6-Me 0 A-8542 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-ethenyl,6-F 0 A-8543 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-ethenyl,6-Me 0 A-8544 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OEt,5-F 0 A-8545 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OEt,6-F 0
(252) TABLE-US-00151 TABLE 151 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8546 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OEt, 5-Cl O A-8547 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OEt, 6-Cl O A-8548 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OEt, 5-Me O A-8549 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OEt, 6-Me O A-8550 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OCHF.sub.2, 5-F O A-8551 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OCHF.sub.2, 6-F O A-8552 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OCHF.sub.2, 5-Me O A-8553 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OCHF.sub.2, 6-Me O A-8554 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(cyclopropyloxy), 5-F O A-8555 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(cyclopropyloxy), 6 F O A-8556 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(cyclopropyloxy), 5-Me O A-8557 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(cyclopropyloxy), 6-Me O A-8558 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-SMe, 5-F O A-8559 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-SMe, 6-F O A-8560 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-SMe, 5-Me O A-8561 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-SMe, 6-Me O A-8562 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O)Me, 5-F O A-8563 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O)Me, 6-F O A-8564 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O)Me, 5-Me O A-8565 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O)Me, 6-Me O A-8566 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O).sub.2Me, 5-F O A-8567 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O).sub.2Me, 6-F O A-8568 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O).sub.2Me, 5-Me O A-8569 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O).sub.2Me, 6-Me O A-8570 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-SCF.sub.3, 5-F O A-8571 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-SCF.sub.3, 6-F O A-8572 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-SCF.sub.3, 5-Me O A-8573 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-SCF.sub.3, 6-Me O A-8574 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O)CF.sub.3, 5-F O A-8575 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O)CF.sub.3, 6-F O A-8576 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O)CF.sub.3, 5-Me O A-8577 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O)CF.sub.3, 6-Me O A-8578 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O)2CF.sub.3, 5-F O A-8579 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O)2CF.sub.3, 6-F O A-8580 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O)2CF.sub.3, 5-Me O A-8581 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-S(?O).sub.2CF.sub.3, 6-Me O A-8582 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(cyclopropylthio), 5-F O A-8583 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(cyclopropylthio), 6-F O A-8584 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(cyclopropylthio), 5-Me O A-8585 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-(cyclopropylthio), 6-Me O A-8586 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-C(?O)Me, 5-F O A-8587 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-C(?O)Me, 6-F O A-8588 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-C(?O)Me, 5-Me O A-8589 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-C(?O)Me, 6-Me O A-8590 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2OH, 5-F O A-8591 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2OH, 6-F O A-8592 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2OH, 5-Me O A-8593 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2OH, 6-Me O A-8594 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2OCH.sub.3, 4-F O A-8595 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2OCH.sub.3, 5-F O A-8596 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2OCH.sub.3, 6-F O A-8597 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2OCH.sub.3, 4-Me O A-8598 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2OCH.sub.3, 5-Me O A-8599 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2OCH.sub.3, 6-Me O A-8600 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OC(?O)CH.sub.3, 5-F O A-8601 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OC(?O)CH.sub.3, 6-F O A-8602 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OC(?O)CH.sub.3, 5-Me O
(253) TABLE-US-00152 TABLE 152 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8) p A-8603 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OC(?O)CH.sub.3, 6-Me O A-8604 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OS(?O).sub.2CH.sub.3, 5-F O A-8605 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OS(?O).sub.2CH.sub.3, 6-F O A-8606 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OS(?O).sub.2CH.sub.3, 5-Me O A-8607 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-OS(?O).sub.2CH.sub.3, 6-Me O A-8608 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH2SCH.sub.3, 5-F O A-8609 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH2SCH.sub.3, 6-F O A-8610 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH2SCH.sub.3, 5-Me O A-8611 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH2SCH.sub.3, 6-F O A-8612 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-NMe.sub.2, 5-F O A-8613 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-NMe.sub.2, 6-F O A-8614 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-NMe.sub.2, 5-Me O A-8615 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-NMe.sub.2, 6-Me O A-8616 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CN, 4-F O A-8617 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CN, 5-F O A-8618 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CN, 6-F O A-8619 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CN, 6-Me O A-8620 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CN, 5-OMe O A-8621 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CN, 6-OMe O A-8622 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 3-CN, 6-Me O A-8623 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 3-CN, 6-OMe O A-8624 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 4-CN, 2-Me O A-8625 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 4-CN, 2-OMe O A-8626 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-NO.sub.2, 4-F O A-8627 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-NO.sub.2, 5-F O A-8628 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-NO.sub.2, 6-F O A-8629 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-NO.sub.2, 4-Me O A-8630 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-NO.sub.2, 5-Me O A-8631 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-NO.sub.2, 6-Me O A-8632 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Me, 4,5-F.sub.2 O A-8633 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Me, 6-Et O A-8634 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-cyclopropyl, 6-OMe O A-8635 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Me ,5-Et O A-8636 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2,6-Et.sub.2 O A-8637 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-Et, 6-F O A-8638 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2OCH.sub.3, 6-Cl O A-8639 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2OCH.sub.2CH.sub.3, 6-Cl O A-8640 H H H H H O CH.sub.2CH.sub.2OCH.sub.2CH.sub.2 2-CH.sub.2NMe.sub.2 O A-8641 H H H H H S H H H O A-8642 H H H H H S H H 2-F O A-8643 H H H H H S H H 2-Cl O A-8644 H H H H H S H H 2-Br O A-8645 H H H H H S H H 2-OH O A-8646 H H H H H S H H 2-Me O A-8647 H H H H H S H H 2-Et O A-8648 H H H H H S H H 2-Pr O A-8649 H H H H H S H H 2-CF.sub.3 O A-8650 H H H H H S H H 2-CHF.sub.2 O A-8651 H H H H H S H H 2-CH.sub.2F O A-8652 H H H H H S H H 2-CF.sub.2Cl O A-8653 H H H H H S H H 2-cyclopropyl O A-8654 H H H H H S H H 2-cyclobutyl O A-8655 H H H H H S H H 2-cyclopentyl O A-8656 H H H H H S H H 2-ethenyl O A-8657 H H H H H S H H H 2-allyl O A-8658 H H H H H S H H 2-(prop-1-en-1-yl) O A-8659 H H H H H S H H 2-(trifluoroethenyl) O
(254) TABLE-US-00153 TABLE 153 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8660 H H H H H S H H 2-OMe 0 A-8661 H H H H H S H H 2-OEt 0 A-8662 H H H H H S H H 2-OPr 0 A-8663 H H H H H S H H 2-O(i-Pr) 0 A-8664 H H H H H S H H 2-OCF.sub.3 0 A-8665 H H H H H S H H 2-OCHF.sub.2 0 A-8666 H H H H H S H H 2-(cyclopropyloxy) 0 A-8667 H H H H H S H H 2-(cyclobutyloxy) 0 A-8668 H H H H H S H H 2-(cyclopentyloxy) 0 A-8669 H H H H H S H H 2-((2,2-dichlorocyclopropyl)oxy) 0 A-8670 H H H H H S H H 2-(oxiran-2-yl) 0 A-8671 H H H H H S H H 2-SMe 0 A-8672 H H H H H S H H 3-SMe 0 A-8673 H H H H H S H H 2-S(?O)Me 0 A-8674 H H H H H S H H 3-S(?O)Me 0 A-8675 H H H H H S H H 2-S(?O).sub.2Me 0 A-8676 H H H H H S H H 3-S(?O).sub.2Me 0 A-8677 H H H H H S H H 2-SCF.sub.3 0 A-8678 H H H H H S H H 3-SCF.sub.3 0 A-8679 H H H H H S H H 3-S(?O)CF.sub.3 0 A-8680 H H H H H S H H 3-SCF(CF.sub.3).sub.2 0 A-8681 H H H H H S H H 2-(cyclopropylthio) 0 A-8682 H H H H H S H H 2-(cyclopropylsulfinyl) 0 A-8683 H H H H H S H H 2-(cyclopropylsulfonyl) 0 A-8684 H H H H H S H H 2-C(?O)Me 0 A-8685 H H H H H S H H 2-CH.sub.2C(?O)CH.sub.3 0 A-8686 H H H H H S H H 2-CH.sub.2C(?O)CF.sub.3 0 A-8687 H H H H H S H H 2-CH.sub.2OH 0 A-8688 H H H H H S H H 2-CH.sub.2OCH.sub.3 0 A-8689 H H H H H S H H 2-CH.sub.2OCH.sub.2CH.sub.3 0 A-8690 H H H H H S H H 2-CH.sub.2SCH.sub.3 0 A-8691 H H H H H S H H 2-CH.sub.2S(?O)CH.sub.3 0 A-8692 H H H H H S H H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 A-8693 H H H H H S H H 2-(benzyboxy) 0 A-8694 H H H H H S H H 2-NH.sub.2 0 A-8695 H H H H H S H H 2-NHMe 0 A-8696 H H H H H S H H 2-N(Me).sub.2 0 A-8697 H H H H H S H H 2-(1,3-dioxolan-2-yl) 0 A-8698 H H H H H S H H 2-(1,3-dioxan-2-yl) 0 A-8699 H H H H H S H H 2-(1H-imidazol-2-yl) 0 A-8700 H H H H H S H H 2-(thiazol-2-yl) 0 A-8701 H H H H H S H H 2-(oxazol-2-yl) 0 A-8702 H H H H H S H H 2-CH?NOH 0 A-8703 H H H H H S H H 2-CH?NOMe 0 A-8704 H H H H H S H H 2-(4,5-dihydro-3-isoxazolyl) 0 A-8705 H H H H H S H H 2-CN 0 A-8706 H H H H H S H H 2-NO.sub.2 0 A-8707 H H H H H S H H 2-F,6-Cl 0 A-8708 H H H H H S H H 2-F,6-Me 0 A-8709 H H H H H S H H 3-F,6-Me 0 A-8710 H H H H H S H H 4-F,2-Me 0 A-8711 H H H H H S H H 2-F,6-OMe 0 A-8712 H H H H H S H H 2-F,6-OMe 0 A-8713 H H H H H S H H 2,6-Cl.sub.2 0 A-8714 H H H H H S H H 2-Cl,6-Me 0 A-8715 H H H H H S H H 3-Cl,6-Me 0 A-8716 H H H H H S H H 4-Cl,2-Me 0
(255) TABLE-US-00154 TABLE 154 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8717 H H H H H S H H 2-Cl,5-CF.sub.3 0 A-8718 H H H H H S H H 2-Cl,6-CF.sub.3 0 A-8719 H H H H H S H H 2-Cl,6-OMe 0 A-8720 H H H H H S H H 3-Cl,6-OMe 0 A-8721 H H H H H S H H 4-Cl,2-OMe 0 A-8722 H H H H H S H H 2,4-Me.sub.2 0 A-8723 H H H H H S H H 2,5-Me.sub.2 0 A-8724 H H H H H S H H 2,6-Me.sub.2 0 A-8725 H H H H H S H H 2-Me,4-CF.sub.3 0 A-8726 H H H H H S H H 2-Me,5CF.sub.3 0 A-8727 H H H H H S H H 2-Me, 0 A-8728 H H H H H S H H 2-Me,4-OMe 0 A-8729 H H H H H S H H 2-Me,5-OMe 0 A-8730 H H H H H S H H 2-Me,6-OMe 0 A-8731 H H H H H S H H 3-Me,6-OMe 0 A-8732 H H H H H S H H 4-Me,2-OMe 0 A-8733 H H H H H S H H 2,5-OMe.sub.2 0 A-8734 H H H H H S H H 2,6-OMe.sub.2 0 A-8735 H H H H H S H H 2-OMe,6-CF.sub.3 0 A-8736 H H H H H S H H 2-CHF.sub.2,5-F 0 A-8737 H H H H H S H H 2-CHF.sub.2,6-F 0 A-8738 H H H H H S H H 2-CHF.sub.2,5-Me 0 A-8739 H H H H H S H H 2-CHF.sub.2,6-Me 0 A-8740 H H H H H S H H 2-cyclopropyl,5-F 0 A-8741 H H H H H S H H 2-cyclopropyl,6-F 0 A-8742 H H H H H S H H 2-cyclopropyl,5-Me 0 A-8743 H H H H H S H H 2-cyclopropyl,6-Me 0 A-8744 H H H H H S H H 2-ethenyl,6-F 0 A-8745 H H H H H S H H 2-ethenyl,6-Me 0 A-8746 H H H H H S H H 2-OEt,5-F 0 A-8747 H H H H H S H H 2-OEt,6-F 0 A-8748 H H H H H S H H 2-OEt,5-Cl 0 A-8749 H H H H H S H H 2-OEt,6-Cl 0 A-8750 H H H H H S H H 2-OEt,5-Me 0 A-8751 H H H H H S H H 2-OEt,6-Me 0 A-8752 H H H H H S H H 2-OCHF.sub.2,5-F 0 A-8753 H H H H H S H H 2-OCHF.sub.2,6-F 0 A-8754 H H H H H S H H 2-OCHF.sub.2,5-Me 0 A-8755 H H H H H S H H 2-OCHF.sub.2,6-Me 0 A-8756 H H H H H S H H 2-(cyclopropyloxy),5-F 0 A-8757 H H H H H S H H 2-(cyclopropyloxy),6-F 0 A-8758 H H H H H S H H 2-(cyclopropyloxy),5-Me 0 A-8759 H H H H H S H H 2-(cyclopropyloxy),6-Me 0 A-8760 H H H H H S H H 2-SMe,5-F 0 A-8761 H H H H H S H H 2-SMe,6-F 0 A-8762 H H H H H S H H 2-SMe,5-Me 0 A-8763 H H H H H S H H 2-SMe,6-Me 0 A-8764 H H H H H S H H 2-S(?O)Me,5-F 0 A-8765 H H H H H S H H 2-S(?O)Me,6-F 0 A-8766 H H H H H S H H 2-S(?O)Me,5-Me 0 A-8767 H H H H H S H H 2-S(?O)Me,6-Me 0 A-8768 H H H H H S H H 2-S(?O).sub.2Me,5-F 0 A-8769 H H H H H S H H 2-S(?O).sub.2Me,6-F 0 A-8770 H H H H H S H H 2-S(?O).sub.2Me,5-Me 0 A-8771 H H H H H S H H 2-S(?O).sub.2Me,6-Me 0 A-8772 H H H H H S H H 2-SCF.sub.3,5-F 0 A-8773 H H H H H S H H 2-SCF.sub.3,6-F 0
(256) TABLE-US-00155 TABLE 155 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8774 H H H H H S H H 2-SCF.sub.3,5-Me 0 A-8775 H H H H H S H H 2-SCF.sub.3,6-Me 0 A-8776 H H H H H S H H 2-S(?O)CF.sub.3,5-F 0 A-8777 H H H H H S H H 2-S(?O)CF.sub.3,6-F 0 A-8778 H H H H H S H H 2-S(?O)CF.sub.3,5-Me 0 A-8779 H H H H H S H H 2-S(?O)CF.sub.3,6-Me 0 A-8780 H H H H H S H H 2-S(?O).sub.2CF.sub.3,5-F 0 A-8781 H H H H H S H H 2-S(?O).sub.2CF.sub.3,6-F 0 A-8782 H H H H H S H H 2-S(?O).sub.2CF.sub.3,5-Me 0 A-8783 H H H H H S H H 2-S(?O).sub.2CF.sub.3,6-Me 0 A-8784 H H H H H S H H 2-(cyclopropylthio),5-F 0 A-8785 H H H H H S H H 2-(cyclopropylthio),6-F 0 A-8786 H H H H H S H H 2-(cyclopropylthio),5-Me 0 A-8787 H H H H H S H H 2-(cyclopropylthio),6-Me 0 A-8788 H H H H H S H H 2-C(?O)Me,5-F 0 A-8789 H H H H H S H H 2-C(?O)Me,6-F 0 A-8790 H H H H H S H H 2-C(?O)Me,5-Me 0 A-8791 H H H H H S H H 2-C(?O)Me,6-Me 0 A-8792 H H H H H S H H 2-CH.sub.2OH,5-F 0 A-8793 H H H H H S H H 2-CH.sub.2OH,6-F 0 A-8794 H H H H H S H H 2-CH.sub.2OH,5-Me 0 A-8795 H H H H H S H H 2-CH.sub.2OH,6-Me 0 A-8796 H H H H H S H H 2-CH.sub.2OCH.sub.3,4-F 0 A-8797 H H H H H S H H 2-CH.sub.2OCH.sub.3,5-F 0 A-8798 H H H H H S H H 2-CH.sub.2OCH.sub.3,6-F 0 A-8799 H H H H H S H H 2-CH.sub.2OCH.sub.3,4-Me 0 A-8800 H H H H H S H H 2-CH.sub.2OCH.sub.3,5-Me 0 A-8801 H H H H H S H H 2-CH.sub.2OCH.sub.3,6-Me 0 A-8802 H H H H H S H H 2-OC(?O)CH.sub.3,5-F 0 A-8803 H H H H H S H H 2-OC(?O)CH.sub.3,6-F 0 A-8804 H H H H H S H H 2-OC(?O)CH.sub.3,5-Me 0 A-8805 H H H H H S H H 2-OC(?O)CH.sub.3,6-Me 0 A-8806 H H H H H S H H 2-OS(?O).sub.2CH.sub.3,5-F 0 A-8807 H H H H H S H H 2-OS(?O).sub.2CH.sub.3,6-F 0 A-8808 H H H H H S H H 2-OS(?O).sub.2CH.sub.3,5-Me 0 A-8809 H H H H H S H H 2-OS(?O).sub.2CH.sub.3,6-Me 0 A-8810 H H H H H S H H 2-CH.sub.2SCH.sub.3,5-F 0 A-8811 H H H H H S H H 2-CH.sub.2SCH.sub.3,6-F 0 A-8812 H H H H H S H H 2-CH.sub.2SCH.sub.3,5-Me 0 A-8813 H H H H H S H H 2-CH.sub.2SCH.sub.3,6-Me 0 A-8814 H H H H H S H H 2-NMe.sub.2,5-F 0 A-8815 H H H H H S H H 2-NMe.sub.2,6-F 0 A-8816 H H H H H S H H 2-NMe.sub.2,5-Me 0 A-8817 H H H H H S H H 2-NMe.sub.2,6-Me 0 A-8818 H H H H H S H H 2-CN,4-F 0 A-8819 H H H H H S H H 2-CN,5-F 0 A-8820 H H H H H S H H 2-CN,6-F 0 A-8821 H H H H H S H H 2-CN,6-Me 0 A-8822 H H H H H S H H 2-CN,5-OMe 0 A-8823 H H H H H S H H 2-CN,6-OMe 0 A-8824 H H H H H S H H 3-CN,6-Me 0 A-8825 H H H H H S H H 3-CN,6-OMe 0 A-8826 H H H H H S H H 4-CN,2-Me 0 A-8827 H H H H H S H H 4-CN,2-OMe 0 A-8828 H H H H H S H H 2-NO.sub.2,4-F 0 A-8829 H H H H H S H H 2-NO.sub.2,5-F 0 A-8830 H H H H H S H H 2-NO.sub.2,6-F 0
(257) TABLE-US-00156 TABLE 156 com- pound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8831 H H H H H S H H 2-NO.sub.2,4-Me 0 A-8832 H H H H H S H H 2-NO.sub.2,5-Me 0 A-8833 H H H H H S H H 2-NO.sub.2,6-Me 0 A-8834 H H H H H S H H 2-Me,4,5-F.sub.2 0 A-8835 H H H H H S H H 2-Me,6-Et 0 A-8836 H H H H H S H H 2-cyclopropyl,6-OMe 0 A-8837 H H H H H S H H 2-Me,5-Et 0 A-8838 H H H H H S H H 2,6-Et.sub.2 0 A-8839 H H H H H S H H 2-Et,6-F 0 A-8840 H H H H H S H H 2-CH.sub.2OCH.sub.3,6-Cl 0 A-8841 H H H H H S H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 A-8842 H H H H H S H H 2-CH.sub.2NMe.sub.2 0 A-8843 H H H H H O H H H 1 A-8844 H H H H H O H H 2-F 1 A-8845 H H H H H O H H 3-F 1 A-8846 H H H H H O H H 4-F 1 A-8847 H H H H H O H H 2-Cl 1 A-8848 H H H H H O H H 3-Cl 1 A-8849 H H H H H O H H 4-Cl 1 A-8850 H H H H H O H H 2-Br 1 A-8851 H H H H H O H H 3-Br 1 A-8852 H H H H H O H H 4-Br 1 A-8853 H H H H H O H H 2-I 1 A-8854 H H H H H O H H 3-I 1 A-8855 H H H H H O H H 4-I 1 A-8856 H H H H H O H H 2-OH 1 A-8857 H H H H H O H H 3-OH 1 A-8858 H H H H H O H H 4-OH 1 A-8859 H H H H H O H H 2-SH 1 A-8860 H H H H H O H H 3-SH 1 A-8861 H H H H H O H H 4-SH 1 A-8862 H H H H H O H H 2-Me 1 A-8863 H H H H H O H H 3-Me 1 A-8864 H H H H H O H H 4-Me 1 A-8865 H H H H H O H H 2-Et 1 A-8866 H H H H H O H H 3-Et 1 A-8867 H H H H H O H H 4-Et 1 A-8868 H H H H H O H H 2-Pr 1 A-8869 H H H H H O H H 3-Pr 1 A-8870 H H H H H O H H 4-Pr 1 A-8871 H H H H H O H H 2-i-Pr 1 A-8872 H H H H H O H H 3-i-Pr 1 A-8873 H H H H H O H H 4-i-Pr 1 A-8874 H H H H H O H H 2-Bu 1 A-8875 H H H H H O H H 3-Bu 1 A-8876 H H H H H O H H 4-Bu 1 A-8877 H H H H H O H H 2-s-Bu 1 A-8878 H H H H H O H H 3-s-Bu 1 A-8879 H H H H H O H H 4-s-Bu 1 A-8880 H H H H H O H H 2-i-Bu 1 A-8881 H H H H H O H H 3-i-Bu 1 A-8882 H H H H H O H H 4-i-Bu 1 A-8883 H H H H H O H H 2-t-Bu 1 A-8884 H H H H H O H H 3-t-Bu 1 A-8885 H H H H H O H H 4-t-Bu 1 A-8886 H H H H H O H H 2-CF.sub.3 1 A-8887 H H H H H O H H 3-CF.sub.3 1
(258) TABLE-US-00157 TABLE 157 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8888 H H H H H O H H 4-CF.sub.3 1 A-8889 H H H H H O H H 2-CHF.sub.2 1 A-8890 H H H H H O H H 3CHF.sub.2 1 A-8891 H H H H H O H H 4-CHF.sub.2 1 A-8892 H H H H H O H H 2-CH.sub.2F 1 A-8893 H H H H H O H H 3-CH.sub.2F 1 A-8894 H H H H H O H H 4-CH.sub.2F 1 A-8895 H H H H H O H H 2-CF.sub.2Cl 1 A-8896 H H H H H O H H 3-CF.sub.2Cl 1 A-8897 H H H H H O H H 4-CF.sub.2Cl 1 A-8898 H H H H H O H H 2-CF(CF.sub.3).sub.2 1 A-8899 H H H H H O H H 3-CF(CF.sub.3).sub.2 1 A-8900 H H H H H O H H 4-CF(CF.sub.3).sub.2 1 A-8901 H H H H H O H H 2-cyclopropyl 1 A-8902 H H H H H O H H 3-cyclopropyl 1 A-8903 H H H H H O H H 4-cyclopropyl 1 A-8904 H H H H H O H H 2-cyclobutyl 1 A-8905 H H H H H O H H 3-cyclobutyl 1 A-8906 H H H H H O H H 4-cyclobutyl 1 A-8907 H H H H H O H H 2-cyclopentyl 1 A-8908 H H H H H O H H 3-cyclopentyl 1 A-8909 H H H H H O H H 4-cyclopentyl 1 A-8910 H H H H H O H H 2-(cyclopropylmethyl) 1 A-8911 H H H H H O H H 3-(cyclopropylmethyl) 1 A-8912 H H H H H O H H 4-(cyclopropylmethyl) 1 A-8913 H H H H H O H H 2-(cyclobutylmethyl) 1 A-8914 H H H H H O H H 3-(cyclobutylmethyl) 1 A-8915 H H H H H O H H 4-(cyclobutylmethyl) 1 A-8916 H H H H H O H H 2-(cyclopentylmethyl) 1 A-8917 H H H H H O H H 3-(cyclopentylmethyl) 1 A-8918 H H H H H O H H 4-(cyclopentylmethyl) 1 A-8919 H H H H H O H H 2-(cyclopropylethyl) 1 A-8920 H H H H H O H H 3-(cyclopropylethyl) 1 A-8921 H H H H H O H H 4-(cyclopropylethyl) 1 A-8922 H H H H H O H H 2-(2,2-difluorocyclopropyl) 1 A-8923 H H H H H O H H 3-(2,2-difluorocyclopropyl) 1 A-8924 H H H H H O H H 4-(2,2-difluorocyclopropyl) 1 A-8925 H H H H H O H H 2-(2,2-dichlorocyclopropyl) 1 A-8926 H H H H H O H H 3-(2,2-dichlorocyclopropyl) 1 A-8927 H H H H H O H H 4-(2,2-dichlorocyclopropyl) 1 A-8928 H H H H H O H H 2-ethenyl 1 A-8929 H H H H H O H H 3-ethenyl 1 A-8930 H H H H H O H H 4-ethenyl 1 A-8931 H H H H H O H H 2-allyl 1 A-8932 H H H H H O H H 3-allyl 1 A-8933 H H H H H O H H 4-allyl 1 A-8934 H H H H H O H H 2-(prop-1-en-1-yl) 1 A-8935 H H H H H O H H 3-(prop-1-en-1-yl) 1 A-8936 H H H H H O H H 4-(prop-1-en-1-yl) 1 A-8937 H H H H H O H H 2-(trifluoroethenyl) 1 A-8938 H H H H H O H H 3-(trifluoroethenyl) 1 A-8939 H H H H H O H H 4-(trifluoroethenyl) 1 A-8940 H H H H H O H H 2-(2,2-dichloroethenyl) 1 A-8941 H H H H H O H H 3-(2,2-dichloroethenyl) 1 A-8942 H H H H H O H H 4-(2,2-dichloroethenyl) 1 A-8943 H H H H H O H H 2-ethynyl 1 A-8944 H H H H H O H H 3-ethynyl 1
(259) TABLE-US-00158 TABLE 158 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-8945 H H H H H O H H 4-ethynyl 1 A-8946 H H H H H O H H 2-(1-propyn-1-yl) 1 A-8947 H H H H H O H H 3-(1-propyn-1-yl) 1 A-8948 H H H H H O H H 4-(1-propyn-1-yl) 1 A-8949 H H H H H O H H 2-(2-propyn-1-yl) 1 A-8950 H H H H H O H H 3-(2-propyn-1-yl) 1 A-8951 H H H H H O H H 4-(2-propyn-1-yl) 1 A-8952 H H H H H O H H 2-(2-cyclopropylethynyl) 1 A-8953 H H H H H O H H 3-(2-cyclopropylethynyl) 1 A-8954 H H H H H O H H 4-(2-cyclopropylethynyl) 1 A-8955 H H H H H O H H 2-(2-chloroethynyl) 1 A-8956 H H H H H O H H 3-(2-chloroethynyl) 1 A-8957 H H H H H O H H 4-(2-chloroethynyl) 1 A-8958 H H H H H O H H 2-(2-bromoethynyl) 1 A-8959 H H H H H O H H 3-(2-bromoethynyl) 1 A-8960 H H H H H O H H 4-(2-bromoethynyl) 1 A-8961 H H H H H O H H 2-OMe 1 A-8962 H H H H H O H H 3-OMe 1 A-8963 H H H H H O H H 4-OMe 1 A-8964 H H H H H O H H 2-OEt 1 A-8965 H H H H H O H H 3-OEt 1 A-8966 H H H H H O H H 4-OEt 1 A-8967 H H H H H O H H 2-OPr 1 A-8968 H H H H H O H H 3-OPr 1 A-8969 H H H H H O H H 4-OPr 1 A-8970 H H H H H O H H 2-O(i-Pr) 1 A-8971 H H H H H O H H 3-O(i-Pr) 1 A-8972 H H H H H O H H 4-O(i-Pr) 1 A-8973 H H H H H O H H 2-OBu 1 A-8974 H H H H H O H H 3-OBu 1 A-8975 H H H H H O H H 4-OBu 1 A-8976 H H H H H O H H 2-O(s-Bu) 1 A-8977 H H H H H O H H 3-O(s-Bu) 1 A-8978 H H H H H O H H 4-O(s-Bu) 1 A-8979 H H H H H O H H 2-O(i-Bu) 1 A-8980 H H H H H O H H 3-O(i-Bu) 1 A-8981 H H H H H O H H 4-O(i-Bu) 1 A-8982 H H H H H O H H 2-O(t-Bu) 1 A-8983 H H H H H O H H 3-O(t-Bu) 1 A-8984 H H H H H O H H 4-O(t-Bu) 1 A-8985 H H H H H O H H 2-OCF.sub.3 1 A-8986 H H H H H O H H 3-OCF.sub.3 1 A-8987 H H H H H O H H 4-OCF.sub.3 1 A-8988 H H H H H O H H 2-OCHF.sub.2 1 A-8989 H H H H H O H H 3-OCHF.sub.2 1 A-8990 H H H H H O H H 4-OCHF.sub.2 1 A-8991 H H H H H O H H 2-OCH.sub.2CF.sub.3 1 A-8992 H H H H H O H H 3-OCH.sub.2CF.sub.3 1 A-8993 H H H H H O H H 4-OCH.sub.2CF.sub.3 1 A-8994 H H H H H O H H 2-(cyclopropyloxy) 1 A-8995 H H H H H O H H 3-(cyclopropyloxy) 1 A-8996 H H H H H O H H 4-(cyclopropyloxy) 1 A-8997 H H H H H O H H 2-(cyclobutyloxy) 1 A-8998 H H H H H O H H 3-(cyclobutyloxy) 1 A-8999 H H H H H O H H 4-(cyclobutyloxy) 1 A-9000 H H H H H O H H 2-(cyclopentyloxy) 1 A-9001 H H H H H O H H 3-(cyclopentyloxy) 1
(260) TABLE-US-00159 TABLE 159 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9002 H H H H H O H H 4-(cyclopentyloxy) 1 A-9003 H H H H H O H H 2-((2,2-dichlorocyclopropyl)oxy) 1 A-9004 H H H H H O H H 3-((2,2-dichlorocyclopropyl)oxy) 1 A-9005 H H H H H O H H 4-((2,2-dichlorocyclopropyl)oxy) 1 A-9006 H H H H H O H H 2-(cyclopropylmethoxy) 1 A-9007 H H H H H O H H 3-(cyclopropylmethoxy) 1 A-9008 H H H H H O H H 4-(cyclopropylmethoxy) 1 A-9009 H H H H H O H H 2-((2,2-difluorocyclopropyl)methoxy) 1 A-9010 H H H H H O H H 3-((2,2-difluorocyclopropyl)methoxy) 1 A-9011 H H H H H O H H 4-((2,2-difluorocyclopropyl)methoxy) 1 A-9012 H H H H H O H H 2-(oxiran-2-yl) 1 A-9013 H H H H H O H H 3-(oxiran-2-yl) 1 A-9014 H H H H H O H H 4-(oxiran-2-yl) 1 A-9015 H H H H H O H H 2-(oxiran-2-ylmethyl) 1 A-9016 H H H H H O H H 3-(oxiran-2-ylmethyl) 1 A-9017 H H H H H O H H 4-(oxiran-2-ylmethyl) 1 A-9018 H H H H H O H H 2-SMe 1 A-9019 H H H H H O H H 3-SMe 1 A-9020 H H H H H O H H 4-SMe 1 A-9021 H H H H H O H H 2-SEt 1 A-9022 H H H H H O H H 3-SEt 1 A-9023 H H H H H O H H 4-SEt 1 A-9024 H H H H H O H H 2-S(?O)Me 1 A-9025 H H H H H O H H 3-S(?O)Me 1 A-9026 H H H H H O H H 4-S(?O)Me 1 A-9027 H H H H H O H H 2-S(?O).sub.2Me 1 A-9028 H H H H H O H H 3-S(?O).sub.2Me 1 A-9029 H H H H H O H H 4-S(?O).sub.2Me 1 A-9030 H H H H H O H H 2-SCF.sub.3 1 A-9031 H H H H H O H H 3-SCF.sub.3 1 A-9032 H H H H H O H H 4-SCF.sub.3 1 A-9033 H H H H H O H H 2-S(?O)CF.sub.3 1 A-9034 H H H H H O H H 3-S(?O)CF.sub.3 1 A-9035 H H H H H O H H 4-S(?O)CF.sub.3 1 A-9036 H H H H H O H H 2-S(?O).sub.2CF.sub.3 1 A-9037 H H H H H O H H 3-S(?O).sub.2CF.sub.3 1 A-9038 H H H H H O H H 4-S(?O).sub.2CF.sub.3 1 A-9039 H H H H H O H H 2-SCF(CF.sub.3).sub.2 1 A-9040 H H H H H O H H 3-SCF(CF.sub.3).sub.2 1 A-9041 H H H H H O H H 4-SCF(CF.sub.3).sub.2 1 A-9042 H H H H H O H H 2-(cyclopropylthio) 1 A-9043 H H H H H O H H 3-(cyclopropylthio) 1 A-9044 H H H H H O H H 4-(cyclopropylthio) 1 A-9045 H H H H H O H H 2-(cyclopropylsulfinyl) 1 A-9046 H H H H H O H H 3-(cyclopropylsulfinyl) 1 A-9047 H H H H H O H H 4-(cyclopropylsulfinyl) 1 A-9048 H H H H H O H H 2-(cyclopropylsulfonyl) 1 A-9049 H H H H H O H H 3-(cyclopropylsulfonyl) 1 A-9050 H H H H H O H H 4-(cyclopropylsulfonyl) 1 A-9051 H H H H H O H H 2-((cyclopropylmethyl)thio) 1 A-9052 H H H H H O H H 3-((cyclopropylmethyl)thio) 1 A-9053 H H H H H O H H 4-((cyclopropylmethyl)thio) 1 A-9054 H H H H H O H H 2-((cyclopropylmethyl)sulfinyl) 1 A-9055 H H H H H O H H 3-((cyclopropylmethyl)sulfinyl) 1 A-9056 H H H H H O H H 4-((cyclopropylmethyl)sulfinyl) 1 A-9057 H H H H H O H H 2-((cyclopropylmethyl)sulfonyl) 1 A-9058 H H H H H O H H 3-((cyclopropylmethyl)sulfonyl) 1
(261) TABLE-US-00160 TABLE 160 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9059 H H H H H O H H 4-((cyclopropymethyl)sulfonyl) 1 A-9060 H H H H H O H H 2-(((2,2-difluorocyclopropyl)methyl)thio) 1 A-9061 H H H H H O H H 3-(((2,2-difluorocyclopropyl)methyl)thio) 1 A-9062 H H H H H O H H 4-(((2,2-difluorocyclopropyl)methyl)thio) 1 A-9063 H H H H H O H H 2-(((2,2-difluorocyclopropyl)methyl)sulfinyl) 1 A-9064 H H H H H O H H 3-(((2,2-difluorocyclopropyl)methyl)sulfinyl) 1 A-9065 H H H H H O H H 4-(((2,2-difluorocyclopropyl)methyl)sulfinyl) 1 A-9066 H H H H H O H H 2-(((2,2-difluorocyclopropyl)methyl)sulfonyl) 1 A-9067 H H H H H O H H 3-(((2,2-difluorocyclopropyl)methyl)sulfonyl) 1 A-9068 H H H H H O H H 4-(((2,2-difluorocyclopropyl)methyl)sulfonyl) 1 A-9069 H H H H H O H H 2-C(?O)Me 1 A-9070 H H H H H O H H 3-C(?O)Me 1 A-9071 H H H H H O H H 4-C(?O)Me 1 A-9072 H H H H H O H H 2-C(?O)Et 1 A-9073 H H H H H O H H 3-C(?O)Et 1 A-9074 H H H H H O H H 4-C(?O)Et 1 A-9075 H H H H H O H H 2-C(?O)CF.sub.3 1 A-9076 H H H H H O H H 3-C(?O)CF.sub.3 1 A-9077 H H H H H O H H 4-C(?O)CF.sub.3 1 A-9078 H H H H H O H H 2-C(?O) 1 A-9079 H H H H H O H H 3-C(?O)OMe 1 A-9080 H H H H H O H H 4-C(?O)OMe 1 A-9081 H H H H H O H H 2-C(?O)OEt 1 A-9082 H H H H H O H H 3-C(?O)OEt 1 A-9083 H H H H H O H H 4-C(?O)OEt 1 A-9084 H H H H H O H H 2-C(?O)NH.sub.2 1 A-9085 H H H H H O H H 3-C(?O)NH.sub.2 1 A-9086 H H H H H O H H 4-C(?O)NH.sub.2 1 A-9087 H H H H H O H H 2-C(?O)NHMe 1 A-9088 H H H H H O H H 3-C(?O)NHMe 1 A-9089 H H H H H O H H 4-C(?O)NHMe 1 A-9090 H H H H H O H H 2-C(?O)NMe.sub.2 1 A-9091 H H H H H O H H 3-C(?O)NMe.sub.2 1 A-9092 H H H H H O H H 4-C(?O)NMe.sub.2 1 A-9093 H H H H H O H H 2-CH.sub.2C(?O)CH.sub.3 1 A-9094 H H H H H O H H 3-CH.sub.2C(?O)CH.sub.3 1 A-9095 H H H H H O H H 4-CH.sub.2C(?O)CH.sub.3 1 A-9096 H H H H H O H H 2-CH.sub.2C(?O)CF.sub.3 1 A-9097 H H H H H O H H 3-CH.sub.2C(?O)CF.sub.3 1 A-9098 H H H H H O H H 4-CH.sub.2C(?O)CF.sub.3 1 A-9099 H H H H H O H H 2-CH.sub.2C(?O)OCH.sub.3 1 A-9100 H H H H H O H H 3-CH.sub.2C(?O)OCH.sub.3 1 A-9101 H H H H H O H H 4-CH.sub.2C(?O)OCH.sub.3 1 A-9102 H H H H H O H H 2-CH.sub.2OH 1 A-9103 H H H H H O H H 3-CH.sub.2OH 1 A-9104 H H H H H O H H 4-CH.sub.2OH 1 A-9105 H H H H H O H H 2-CH.sub.2OCH.sub.3 1 A-9106 H H H H H O H H 3-CH.sub.2OCH.sub.3 1 A-9107 H H H H H O H H 4-CH.sub.2OCH.sub.3 1 A-9108 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3 1 A-9109 H H H H H O H H 3-CH.sub.2OCH.sub.2CH.sub.3 1 A-9110 H H H H H O H H 4-CH.sub.2OCH.sub.2CH.sub.3 1 A-9111 H H H H H O H H 2-CH(CH.sub.3)OCH.sub.3 1 A-9112 H H H H H O H H 3-CH(CH.sub.3)OCH.sub.3 1 A-9113 H H H H H O H H 4-CH(CH.sub.3)OCH.sub.3 1 A-9114 H H H H H O H H 2-CH.sub.2CH.sub.2OCH.sub.3 1 A-9115 H H H H H O H H 3-CH.sub.2CH.sub.2OCH.sub.3 1
(262) TABLE-US-00161 TABLE 161 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9116 H H H H H O H H 4-CH.sub.2CH.sub.2OCH.sub.3 1 A-9117 H H H H H O H H 2-CH.sub.2OCF.sub.3 1 A-9118 H H H H H O H H 3-CH.sub.2OCF.sub.3 1 A-9119 H H H H H O H H 4-CH.sub.2OCF.sub.3 1 A-9120 H H H H H O H H 2-CF.sub.2OCH.sub.3 1 A-9121 H H H H H O H H 3-CF.sub.2OCH.sub.3 1 A-9122 H H H H H O H H 4-CF.sub.2OCH.sub.3 1 A-9123 H H H H H O H H 2-CF.sub.2CF.sub.2OCF.sub.3 1 A-9124 H H H H H O H H 3-CF.sub.2CF.sub.2OCF.sub.3 1 A-9125 H H H H H O H H 4-CF.sub.2CF.sub.2OCF.sub.3 1 A-9126 H H H H H O H H 2-OC(?O)CH.sub.3 1 A-9127 H H H H H O H H 3-OC(?O)CH.sub.3 1 A-9128 H H H H H O H H 4-OC(?O)CH.sub.3 1 A-9129 H H H H H O H H 2-OC(?O)CF.sub.3 1 A-9130 H H H H H O H H 3-OC(?O)CF.sub.3 1 A-9131 H H H H H O H H 4-OC(?O)CF.sub.3 1 A-9132 H H H H H O H H 2-OC(?O)NH.sub.2 1 A-9133 H H H H H O H H 3-OC(?O)NH.sub.2 1 A-9134 H H H H H O H H 4-OC(?O)NH.sub.2 1 A-9135 H H H H H O H H 2-OC(?O)NHCH.sub.3 1 A-9136 H H H H H O H H 3-OC(?O)NHCH.sub.3 1 A-9137 H H H H H O H H 4-OC(?O)NHCH.sub.3 1 A-9138 H H H H H O H H 2-OC(?O)N(CH.sub.3).sub.2 1 A-9139 H H H H H O H H 3-OC(?O)N(CH.sub.3).sub.2 1 A-9140 H H H H H O H H 4-OC(?O)N(CH.sub.3).sub.2 1 A-9141 H H H H H O H H 2-CH.sub.2OC(?O)NH.sub.2 1 A-9142 H H H H H O H H 3-CH.sub.2OC(?O)NH.sub.2 1 A-9143 H H H H H O H H 4-CH.sub.2OC(?O)NH.sub.2 1 A-9144 H H H H H O H H 2-CH.sub.2OC(?O)NHCH.sub.3 1 A-9145 H H H H H O H H 3-CH.sub.2OC(?O)NHCH.sub.3 1 A-9146 H H H H H O H H 4-CH.sub.2OC(?O)NHCH.sub.3 1 A-9147 H H H H H O H H 2-CH.sub.2OC(?O)N(CH.sub.3).sub.2 1 A-9148 H H H H H O H H 3-CH.sub.2OC(?O)N(CH.sub.3).sub.2 1 A-9149 H H H H H O H H 4-CH.sub.2OC(?O)N(CH.sub.3).sub.2 1 A-9150 H H H H H O H H 2-OC(?O)OCH.sub.3 1 A-9151 H H H H H O H H 3-OC(?O)OCH.sub.3 1 A-9152 H H H H H O H H 4-OC(?O)OCH.sub.3 1 A-9153 H H H H H O H H 2-CH.sub.2OC(?O)OCH.sub.3 1 A-9154 H H H H H O H H 3-CH.sub.2OC(?O)OCH.sub.3 1 A-9155 H H H H H O H H 4-CH.sub.2OC(?O)OCH.sub.3 1 A-9156 H H H H H O H H 2-CH.sub.2OC(?O)CH.sub.3 1 A-9157 H H H H H O H H 3-CH.sub.2OC(?O)CH.sub.3 1 A-9158 H H H H H O H H 4-CH.sub.2OC(?O)CH.sub.3 1 A-9159 H H H H H O H H 2-OS(?O).sub.2CH.sub.3 1 A-9160 H H H H H O H H 3-OS(?O).sub.2CH.sub.3 1 A-9161 H H H H H O H H 4-OS(?O).sub.2CH.sub.3 1 A-9162 H H H H H O H H 2-CH.sub.2SCH.sub.3 1 A-9163 H H H H H O H H 3-CH.sub.2SCH.sub.3 1 A-9164 H H H H H O H H 4-CH.sub.2SCH.sub.3 1 A-9165 H H H H H O H H 2-CH.sub.2S(?O)CH.sub.3 1 A-9166 H H H H H O H H 3-CH.sub.2S(?O)CH.sub.3 1 A-9167 H H H H H O H H 4-CH.sub.2S(?O)CH.sub.3 1 A-9168 H H H H H O H H 2-CH.sub.2S(?O).sub.2CH.sub.3 1 A-9169 H H H H H O H H 3-CH.sub.2S(?O).sub.2CH.sub.3 1 A-9170 H H H H H O H H 4-CH.sub.2S(?O).sub.2CH.sub.3 1 A-9171 H H H H H O H H 2-CH.sub.2SCF.sub.3 1 A-9172 H H H H H O H H 3-CH.sub.2SCF.sub.3 1
(263) TABLE-US-00162 TABLE 162 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9173 H H H H H O H H 4-CH.sub.2SCF.sub.3 1 A-9174 H H H H H O H H 2-CH.sub.2S(?O)CF.sub.3 1 A-9175 H H H H H O H H 3-CH.sub.2S(?O)CF.sub.3 1 A-9176 H H H H H O H H 4-CH.sub.2S(?O)CF.sub.3 1 A-9177 H H H H H O H H 2-CH.sub.2S(?O).sub.2CF.sub.3 1 A-9178 H H H H H O H H 3-CH.sub.2S(?O).sub.2CF.sub.3 1 A-9179 H H H H H O H H 4-CH.sub.2S(?O).sub.2CF.sub.3 1 A-9180 H H H H H O H H 2-phenyl 1 A-9181 H H H H H O H H 3-phenyl 1 A-9182 H H H H H O H H 4-phenyl 1 A-9183 H H H H H O H H 2-(phenyloxy) 1 A-9184 H H H H H O H H 3-(phenyloxy) 1 A-9185 H H H H H O H H 4-(phenyloxy) 1 A-9186 H H H H H O H H 2-benzyl 1 A-9187 H H H H H O H H 3-benzyl 1 A-9188 H H H H H O H H 4-benzyl 1 A-9189 H H H H H O H H 2-(benzyloxy) 1 A-9190 H H H H H O H H 3-(benzyloxy) 1 A-9191 H H H H H O H H 4-(benzyloxy) 1 A-9192 H H H H H O H H 2-((2-fluorobenzyl)oxy) 1 A-9193 H H H H H O H H 3-((2-fluorobenzyl)oxy) 1 A-9194 H H H H H O H H 4-((2-fluorobenzyl)oxy) 1 A-9195 H H H H H O H H 2-((3-fluorobenzyl)oxy) 1 A-9196 H H H H H O H H 3-((3-fluorobenzyl)oxy) 1 A-9197 H H H H H O H H 4-((3-fluorobenzyl)oxy) 1 A-9198 H H H H H O H H 2-((4-fluorobenzyl)oxy) 1 A-9199 H H H H H O H H 3-((4-fluorobenzyl)oxy) 1 A-9200 H H H H H O H H 4-((4-fluorobenzyl)oxy) 1 A-9201 H H H H H O H H 2-((2-chlorobenzyl)oxy) 1 A-9202 H H H H H O H H 3-((2-chlorobenzyl)oxy) 1 A-9203 H H H H H O H H 4-((2-chlorobenzyl)oxy) 1 A-9204 H H H H H O H H 2-((3-chlorobenzyl)oxy) 1 A-9205 H H H H H O H H 3-((3-chlorobenzyl)oxy) 1 A-9206 H H H H H O H H 4-((3-chlorobenzyl)oxy) 1 A-9207 H H H H H O H H 2-((4-chlorobenzyl)oxy) 1 A-9208 H H H H H O H H 3-((4-chlorobenzyl)oxy) 1 A-9209 H H H H H O H H 4-((4-chlorobenzyl)oxy) 1 A-9210 H H H H H O H H 2-((2-methybenzyl)oxy) 1 A-9211 H H H H H O H H 3-((2-methybenzyl)oxy) 1 A-9212 H H H H H O H H 4-((2-methybenzyl)oxy) 1 A-9213 H H H H H O H H 2-((3-methybenzyl)oxy) 1 A-9214 H H H H H O H H 3-((3-methybenzyl)oxy) 1 A-9215 H H H H H O H H 4-((3-methybenzyl)oxy) 1 A-9216 H H H H H O H H 2-((4-methybenzyl)oxy) 1 A-9217 H H H H H O H H 3-((4-methybenzyl)oxy) 1 A-9218 H H H H H O H H 4-((4-methybenzyl)oxy) 1 A-9219 H H H H H O H H 2-((2-(trifluoromethyl)benzyl)oxy) 1 A-9220 H H H H H O H H 3-((2-(trifluoromethyl)benzyl)oxy) 1 A-9221 H H H H H O H H 4-((2-(trifluoromethyl)benzyl)oxy) 1 A-9222 H H H H H O H H 2-((3-(trifluoromethyl)benzyl)oxy) 1 A-9223 H H H H H O H H 3-((3-(trifluoromethyl)benzyl)oxy) 1 A-9224 H H H H H O H H 4-((3-(trifluoromethyl)benzyl)oxy) 1 A-9225 H H H H H O H H 2-((4-(trifluoromethyl)benzyl)oxy) 1 A-9226 H H H H H O H H 3-((4-(trifluoromethyl)benzyl)oxy) 1 A-9227 H H H H H O H H 4-((4-(trifluoromethyl)benzyl)oxy) 1 A-9228 H H H H H O H H 2-((2-methoxybenzyl)oxy) 1 A-9229 H H H H H O H H 3-((2-methoxybenzyl)oxy) 1
(264) TABLE-US-00163 TABLE 163 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9230 H H H H H O H H 4-((2-methoxybenzyl)oxy) 1 A-9231 H H H H H O H H 2-((3-methoxybenzyl)oxy) 1 A-9232 H H H H H O H H 3-((3-methoxybenzyl)oxy) 1 A-9233 H H H H H O H H 4-((3-methoxybenzyl)oxy) 1 A-9234 H H H H H O H H 2-((4-methoxybenzyl)oxy) 1 A-9235 H H H H H O H H 3-((4-methoxybenzyl)oxy) 1 A-9236 H H H H H O H H 4-((4-methoxybenzyl)oxy) 1 A-9237 H H H H H O H H 2-((2-(trifluoromethoxy)benzyl)oxy) 1 A-9238 H H H H H O H H 3-((2-(trifluoromethoxy)benzyl)oxy) 1 A-9239 H H H H H O H H 4-((2-(trifluoromethoxy)benzyl)oxy) 1 A-9240 H H H H H O H H 2-((3-(trifluoromethoxy)benzyl)oxy) 1 A-9241 H H H H H O H H 3-((3-(trifluoromethoxy)benzyl)oxy) 1 A-9242 H H H H H O H H 4-((3-(trifluoromethoxy)benzyl)oxy) 1 A-9243 H H H H H O H H 2-((4-(trifluoromethoxy)benzyl)oxy) 1 A-9244 H H H H H O H H 3-((4-(trifluoromethoxy)benzyl)oxy) 1 A-9245 H H H H H O H H 4-((4-(trifluoromethoxy)benzyl)oxy) 1 A-9246 H H H H H O H H 2-((2-(methylthio)benzyl)oxy) 1 A-9247 H H H H H O H H 3-((2-(methylthio)benzyl)oxy) 1 A-9248 H H H H H O H H 4-((2-(methylthio)benzyl)oxy) 1 A-9249 H H H H H O H H 2-((3-(methylthio)benzyl)oxy) 1 A-9250 H H H H H O H H 3-((3-(methylthio)benzyl)oxy) 1 A-9251 H H H H H O H H 4-((3-(methylthio)benzyl)oxy) 1 A-9252 H H H H H O H H 2-((4-(methylthio)benzyl)oxy) 1 A-9253 H H H H H O H H 3-((4-(methylthio)benzyl)oxy) 1 A-9254 H H H H H O H H 4-((4-(methylthio)benzyl)oxy) 1 A-9255 H H H H H O H H 2-((2-(methylsulfinyl)benzyl)oxy) 1 A-9256 H H H H H O H H 3-((2-(methylsulfinyl)benzyl)oxy) 1 A-9257 H H H H H O H H 4-((2-(methylsulfinyl)benzyl)oxy) 1 A-9258 H H H H H O H H 2-((3-(methylsulfinyl)benzyl)oxy) 1 A-9259 H H H H H O H H 3-((3-(methylsulfinyl)benzyl)oxy) 1 A-9260 H H H H H O H H 4-((3-(methylsulfinyl)benzyl)oxy) 1 A-9261 H H H H H O H H 2-((4-(methylsulfinyl)benzyl)oxy) 1 A-9262 H H H H H O H H 3-((4-(methylsulfinyl)benzyl)oxy) 1 A-9263 H H H H H O H H 4-((4-(methylsulfinyl)benzyl)oxy) 1 A-9264 H H H H H O H H 2-((2-(methylsulfonyl)benzyl)oxy) 1 A-9265 H H H H H O H H 3-((2-(methylsulfonyl)benzyl)oxy) 1 A-9266 H H H H H O H H 4-((2-(methylsulfonyl)benzyl)oxy) 1 A-9267 H H H H H O H H 2-((3-(methylsulfonyl)benzyl)oxy) 1 A-9268 H H H H H O H H 3-((3-(methylsulfonyl)benzyl)oxy) 1 A-9269 H H H H H O H H 4-((3-(methylsulfonyl)benzyl)oxy) 1 A-9270 H H H H H O H H 2-((4-(methylsulfonyl)benzyl)oxy) 1 A-9271 H H H H H O H H 3-((4-(methylsulfonyl)benzyl)oxy) 1 A-9272 H H H H H O H H 4-((4-(methylsulfonyl)benzyl)oxy) 1 A-9273 H H H H H O H H 2-((2-(trifluoromethylthio)benzyl)oxy) 1 A-9274 H H H H H O H H 3-((2-(trifluoromethylthio)benzyl)oxy) 1 A-9275 H H H H H O H H 4-((2-(trifluoromethylthio)benzyl)oxy) 1 A-9276 H H H H H O H H 2-((3-(trifluoromethylthio)benzyl)oxy) 1 A-9277 H H H H H O H H 3-((3-(trifluoromethylthio)benzyl)oxy) 1 A-9278 H H H H H O H H 4-((3-(trifluoromethylthio)benzyl)oxy) 1 A-9279 H H H H H O H H 2-((4-(trifluoromethylthio)benzyl)oxy) 1 A-9280 H H H H H O H H 3-((4-(trifluoromethylthio)benzyl)oxy) 1 A-9281 H H H H H O H H 4-((4-(trifluoromethylthio)benzyl)oxy) 1 A-9282 H H H H H O H H 2-((2-(trifluoromethylsulfinyl)benzyl)oxy) 1 A-9283 H H H H H O H H 3-((2-(trifluoromethylsulfinyl)benzyl)oxy) 1 A-9284 H H H H H O H H 4-((2-(trifluoromethylsulfinyl)benzyl)oxy) 1 A-9285 H H H H H O H H 2-((3-(trifluoromethylsulfinyl)benzyl)oxy) 1 A-9286 H H H H H O H H 3-((3-(trifluoromethylsulfinyl)benzyl)oxy) 1
(265) TABLE-US-00164 TABLE 164 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9287 H H H H H O H H 4-((3-(trifluoromethylsulfinyl)benzyl)oxy) 1 A-9288 H H H H H O H H 2-((4-(trifluoromethylsuffinyl)benzyl)oxy) 1 A-9289 H H H H H O H H 3-((4-(trifluoromethylsulfinyl)benzyl)oxy) 1 A-9290 H H H H H O H H 4-((4-(trifluoromethylsulfinyl)benzyl)oxy) 1 A-9291 H H H H H O H H 2-((2-(trifluoromethylsulfonyl)benzyl)oxy) 1 A-9292 H H H H H O H H 3-((2-(trifluoromethylsulfonyl)benzyl)oxy) 1 A-9293 H H H H H O H H 4-((2-(trifluoromethylsulfonyl)benzyl)oxy) 1 A-9294 H H H H H O H H 2-((3-(trifluoromethylsulfonyl)benzyl)oxy) 1 A-9295 H H H H H O H H 3-((3-(trifluoromethylsulfonyl)benzyl)oxy) 1 A-9296 H H H H H O H H 4-((3-(trifluoromethylsulfonyl)benzyl)oxy) 1 A-9297 H H H H H O H H 2-((4-(trifluoromethylsulfonyl)benzyl)oxy) 1 A-9298 H H H H H O H H 3-((4-(trifluoromethylsulfonyl)benzyl)oxy) 1 A-9299 H H H H H O H H 4-((4-(trifluoromethylsulfonyl)benzyl)oxy) 1 A-9300 H H H H H O H H 2-((2-aminobenzyl)oxy) 1 A-9301 H H H H H O H H 3-((2-aminobenzyl)oxy) 1 A-9302 H H H H H O H H 4-((2-aminobenzyl)oxy) 1 A-9303 H H H H H O H H 2-((3-aminobenzyl)oxy) 1 A-9304 H H H H H O H H 3-((3-aminobenzyl)oxy) 1 A-9305 H H H H H O H H 4-((3-aminobenzyl)oxy) 1 A-9306 H H H H H O H H 2-((4-aminobenzyl)oxy) 1 A-9307 H H H H H O H H 3-((4-aminobenzyl)oxy) 1 A-9308 H H H H H O H H 4-((4-aminobenzyl)oxy) 1 A-9309 H H H H H O H H 2-((2-(methylamino)benzyl)oxy) 1 A-9310 H H H H H O H H 3-((2-(methylamino)benzyl)oxy) 1 A-9311 H H H H H O H H 4-((2-(methylamino)benzyl)oxy) 1 A-9312 H H H H H O H H 2-((3-(methylamino)benzyl)oxy) 1 A-9313 H H H H H O H H 3-((3-(methylamino)benzyl)oxy) 1 A-9314 H H H H H O H H 4-((3-(methylamino)benzyl)oxy) 1 A-9315 H H H H H O H H 2-((4-(methylamino)benzyl)oxy) 1 A-9316 H H H H H O H H 3-((4-(methylamino)benzyl)oxy) 1 A-9317 H H H H H O H H 4-((4-(methylamino)benzyl)oxy) 1 A-9318 H H H H H O H H 2-((2-(dimethylamino)benzyl)oxy) 1 A-9319 H H H H H O H H 3-((2-(dimethylamino)benzyl)oxy) 1 A-9320 H H H H H O H H 4-((2-(dimethylamino)benzyl)oxy) 1 A-9321 H H H H H O H H 2-((3-(dimethylamino)benzyl)oxy) 1 A-9322 H H H H H O H H 3-((3-(dimethylamino)benzyl)oxy) 1 A-9323 H H H H H O H H 4-((3-(dimethylamino)benzyl)oxy) 1 A-9324 H H H H H O H H 2-((4-(dimethylamino)benzyl)oxy) 1 A-9325 H H H H H O H H 3-((4-(dimethylamino)benzyl)oxy) 1 A-9326 H H H H H O H H 4-((4-(dimethylamino)benzyl)oxy) 1 A-9327 H H H H H O H H 2-((2-cyanobenzyl)oxy) 1 A-9328 H H H H H O H H 3-((2-cyanobenzyl)oxy) 1 A-9329 H H H H H O H H 4-((2-cyanobenzyl)oxy) 1 A-9330 H H H H H O H H 2-((3-cyanobenzyl)oxy) 1 A-9331 H H H H H O H H 3-((3-cyanobenzyl)oxy) 1 A-9332 H H H H H O H H 4-((3-cyanobenzyl)oxy) 1 A-9333 H H H H H O H H 2-((4-cyanobenzyl)oxy) 1 A-9334 H H H H H O H H 3-((4-cyanobenzyl)oxy) 1 A-9335 H H H H H O H H 4-((4-cyanobenzyl)oxy) 1 A-9336 H H H H H O H H 2-((2-nitrobenzyl)oxy) 1 A-9337 H H H H H O H H 3-((2-nitrobenzyl)oxy) 1 A-9338 H H H H H O H H 4-((2-nitrobenzyl)oxy) 1 A-9339 H H H H H O H H 2-((3-nitrobenzyl)oxy) 1 A-9340 H H H H H O H H 3-((3-nitrobenzyl)oxy) 1 A-9341 H H H H H O H H 4-((3-nitrobenzyl)oxy) 1 A-9342 H H H H H O H H 2-((4-nitrobenzyl)oxy) 1 A-9343 H H H H H O H H 3-((4-nitrobenzyl)oxy) 1
(266) TABLE-US-00165 TABLE 165 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9344 H H H H H O H H 4-((4-nitrobenzyl)oxy) 1 A-9345 H H H H H O H H 2-NH.sub.2 1 A-9346 H H H H H O H H 3-NH.sub.2 1 A-9347 H H H H H O H H 4-NH.sub.2 1 A-9348 H H H H H O H H 2-NHMe 1 A-9349 H H H H H O H H 3-NHMe 1 A-9350 H H H H H O H H 4-NHMe 1 A-9351 H H H H H O H H 2-NHEt 1 A-9352 H H H H H O H H 3-NHEt 1 A-9353 H H H H H O H H 4-NHEt 1 A-9354 H H H H H O H H 2-N(Me).sub.2 1 A-9355 H H H H H O H H 3-N(Me).sub.2 1 A-9356 H H H H H O H H 4-N(Me).sub.2 1 A-9357 H H H H H O H H 2-N(Et).sub.2 1 A-9358 H H H H H O H H 3-N(Et).sub.2 1 A-9359 H H H H H O H H 4-N(Et).sub.2 1 A-9360 H H H H H O H H 2-CHO 1 A-9361 H H H H H O H H 3-CHO 1 A-9362 H H H H H O H H 4-CHO 1 A-9363 H H H H H O H H 2-C(?O)OH 1 A-9364 H H H H H O H H 3-C(?O)OH 1 A-9365 H H H H H O H H 4-C(?O)OH 1 A-9366 H H H H H O H H 2-(1,3-dioxolan-2-yl) 1 A-9367 H H H H H O H H 3-(1,3-dioxolan-2-yl) 1 A-9368 H H H H H O H H 4-(1,3-dioxolan-2-yl) 1 A-9369 H H H H H O H H 2-(1,3-dioxan-2-y) 1 A-9370 H H H H H O H H 3-(1,3-dioxan-2-yl) 1 A-9371 H H H H H O H H 4-(1,3-dioxan-2-yl) 1 A-9372 H H H H H O H H 2-(1H-imidazol-2-yl) 1 A-9373 H H H H H O H H 3-(1H-imidazol-2-yl) 1 A-9374 H H H H H O H H 4-(1H-imidazol-2-yl) 1 A-9375 H H H H H O H H 2-(thiazol-2-yl) 1 A-9376 H H H H H O H H 3-(thiazol-2-yl) 1 A-9377 H H H H H O H H 4-(thiazol-2-yl) 1 A-9378 H H H H H O H H 2-(oxazol-2-yl) 1 A-9379 H H H H H O H H 3-(oxazol-2-yl) 1 A-9380 H H H H H O H H 4-(oxazol-2-yl) 1 A-9381 H H H H H O H H 2-CH?NOH 1 A-9382 H H H H H O H H 3-CH?NOH 1 A-9383 H H H H H O H H 4-CH?NOH 1 A-9384 H H H H H O H H 2-CH?NOMe 1 A-9385 H H H H H O H H 3-CH?NOMe 1 A-9386 H H H H H O H H 4-CH?NOMe 1 A-9387 H H H H H O H H 2-(4,5-dihydro-3-isoxazolyl) 1 A-9388 H H H H H O H H 3-(4,5-dihydro-3-isoxazolyl) 1 A-9389 H H H H H O H H 4-(4,5-dihydro-3-isoxazolyl) 1 A-9390 H H H H H O H H 2-CN 1 A-9391 H H H H H O H H 3-CN 1 A-9392 H H H H H O H H 4-CN 1 A-9393 H H H H H O H H 2-NO.sub.2 1 A-9394 H H H H H O H H 3-NO.sub.2 1 A-9395 H H H H H O H H 4-NO.sub.2 1 A-9396 H H H H H O H H 2,3-F.sub.2 1 A-9397 H H H H H O H H 2,4-F.sub.2 1 A-9398 H H H H H O H H 2,5-F.sub.2 1 A-9399 H H H H H O H H 2,6-F.sub.2 1 A-9400 H H H H H O H H 3,4-F.sub.2 1
(267) TABLE-US-00166 TABLE 166 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9401 H H H H H O H H 3,5-F.sub.2 1 A-9402 H H H H H O H H 2-F,3-Cl 1 A-9403 H H H H H O H H 2-F,4-Cl 1 A-9404 H H H H H O H H 2-F,5-Cl 1 A-9405 H H H H H O H H 2-F,6-Cl 1 A-9406 H H H H H O H H 3-F,2-Cl 1 A-9407 H H H H H O H H 3-F,4-Cl 1 A-9408 H H H H H O H H 3-F,5-Cl 1 A-9409 H H H H H O H H 3-F,6-Cl 1 A-9410 H H H H H O H H 4-F,2-Cl 1 A-9411 H H H H H O H H 4-F,3-Cl 1 A-9412 H H H H H O H H 2-F,3-Me 1 A-9413 H H H H H O H H 2-F,4-Me 1 A-9414 H H H H H O H H 2-F,5-Me 1 A-9415 H H H H H O H H 2-F,6-Me 1 A-9416 H H H H H O H H 3-F,2-Me 1 A-9417 H H H H H O H H 3-F,4-Me 1 A-9418 H H H H H O H H 3-F,5-Me 1 A-9419 H H H H H O H H 3-F,6-Me 1 A-9420 H H H H H O H H 4-F,2-Me 1 A-9421 H H H H H O H H 4-F,3-Me 1 A-9422 H H H H H O H H 2-F,3-CF.sub.3 1 A-9423 H H H H H O H H 2-F,4-CF.sub.3 1 A-9424 H H H H H O H H 2-F,5-CF.sub.3 1 A-9425 H H H H H O H H 2-F,6-CF.sub.3 1 A-9426 H H H H H O H H 3-F,2-CF.sub.3 1 A-9427 H H H H H O H H 3-F,4-CF.sub.3 1 A-9428 H H H H H O H H 3-F,5-CF.sub.3 1 A-9429 H H H H H O H H 3-F,6-CF.sub.3 1 A-9430 H H H H H O H H 4-F,2-CF.sub.3 1 A-9431 H H H H H O H H 4-F,3-CF.sub.3 1 A-9432 H H H H H O H H 2-F,3-OMe 1 A-9433 H H H H H O H H 2-F,4-OMe 1 A-9434 H H H H H O H H 2-F,5-OMe 1 A-9435 H H H H H O H H 2-F,6-OMe 1 A-9436 H H H H H O H H 3-F,2-OMe 1 A-9437 H H H H H O H H 3-F,4-OMe 1 A-9438 H H H H H O H H 3-F,5-OMe 1 A-9439 H H H H H O H H 3-F,6-OMe 1 A-9440 H H H H H O H H 4-F,2-OMe 1 A-9441 H H H H H O H H 3-F,3-OMe 1 A-9442 H H H H H O H H 2,3-Cl.sub.2 1 A-9443 H H H H H O H H 2,4-Cl.sub.2 1 A-9444 H H H H H O H H 2,5-Cl.sub.2 1 A-9445 H H H H H O H H 2,6-Cl.sub.2 1 A-9446 H H H H H O H H 3,4-Cl.sub.2 1 A-9447 H H H H H O H H 3,5-Cl.sub.2 1 A-9448 H H H H H O H H 2-Cl,3-Me 1 A-9449 H H H H H O H H 2-Cl,4-Me 1 A-9450 H H H H H O H H 2-Cl,5-Me 1 A-9451 H H H H H O H H 2-Cl,6-Me 1 A-9452 H H H H H O H H 3-Cl,2-Me 1 A-9453 H H H H H O H H 3-Cl,4-Me 1 A-9454 H H H H H O H H 3-Cl,5-Me 1 A-9455 H H H H H O H H 3-Cl,6-Me 1 A-9456 H H H H H O H H 4-Cl,2-Me 1 A-9457 H H H H H O H H 4-Cl,3-Me 1
(268) TABLE-US-00167 TABLE 167 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9458 H H H H H O H H 2-Cl,3-CF.sub.3 1 A-9459 H H H H H O H H 2-Cl,4-CF.sub.3 1 A-9460 H H H H H O H H 2-Cl,5-CF.sub.3 1 A-9461 H H H H H O H H 2-Cl,6-CF.sub.3 1 A-9462 H H H H H O H H 3-C1,2-CF.sub.3 1 A-9463 H H H H H O H H 3-Cl,4-CF.sub.3 1 A-9464 H H H H H O H H 3-Cl,5-CF.sub.3 1 A-9465 H H H H H O H H 3-Cl,6-CF.sub.3 1 A-9466 H H H H H O H H 4-Cl,2-CF.sub.3 1 A-9467 H H H H H O H H 4-Cl,3-CF.sub.3 1 A-9468 H H H H H O H H 2-Cl,3-OMe 1 A-9469 H H H H H O H H 2-Cl,4-OMe 1 A-9470 H H H H H O H H 2-Cl,5-OMe 1 A-9471 H H H H H O H H 2-Cl,6-OMe 1 A-9472 H H H H H O H H 3-Cl,2-OMe 1 A-9473 H H H H H O H H 3-Cl,4-OMe 1 A-9474 H H H H H O H H 3-Cl,5-OMe 1 A-9475 H H H H H O H H 3-Cl,6-OMe 1 A-9476 H H H H H O H H 4-Cl,2-OMe 1 A-9477 H H H H H O H H 4-Cl,3-OMe 1 A-9478 H H H H H O H H 2,3-Me.sub.2 1 A-9479 H H H H H O H H 2,4-Me.sub.2 1 A-9480 H H H H H O H H 2,5-Me.sub.2 1 A-9481 H H H H H O H H 2,6-Me.sub.2 1 A-9482 H H H H H O H H 3,4-Me.sub.2 1 A-9483 H H H H H O H H 3,5-Me.sub.2 1 A-9484 H H H H H O H H 2-Me,3-CF.sub.3 1 A-9485 H H H H H O H H 2-Me,4-CF.sub.3 1 A-9486 H H H H H O H H 2-Me,5-CF.sub.3 1 A-9487 H H H H H O H H 2-Me,6-CF.sub.3 1 A-9488 H H H H H O H H 3-Me,2-CF.sub.3 1 A-9489 H H H H H O H H 3-Me,4-CF.sub.3 1 A-9490 H H H H H O H H 3-Me,5-CF.sub.3 1 A-9491 H H H H H O H H 3-Me,6-CF.sub.3 1 A-9492 H H H H H O H H 4-Me,2-CF.sub.3 1 A-9493 H H H H H O H H 4-Me,3-CF.sub.3 1 A-9494 H H H H H O H H 2-Me,3-OMe 1 A-9495 H H H H H O H H 2-Me,4-OMe 1 A-9496 H H H H H O H H 2-Me,5-OMe 1 A-9497 H H H H H O H H 2-Me,6-OMe 1 A-9498 H H H H H O H H 3-Me,2-OMe 1 A-9499 H H H H H O H H 3-Me,4-OMe 1 A-9500 H H H H H O H H 3-Me,5-OMe 1 A-9501 H H H H H O H H 3-Me,6-OMe 1 A-9502 H H H H H O H H 4-Me,2-OMe 1 A-9503 H H H H H O H H 4-Me,3-OMe 1 A-9504 H H H H H O H H 2,3-OMe.sub.2 1 A-9505 H H H H H O H H 2,4-OMe.sub.2 1 A-9506 H H H H H O H H 2,5-OMe.sub.2 1 A-9507 H H H H H O H H 2,6-OMe.sub.2 1 A-9508 H H H H H O H H 3,4-OMe.sub.2 1 A-9509 H H H H H O H H 3,5-OMe.sub.2 1 A-9510 H H H H H O H H 2-OMe,3-CF.sub.3 1 A-9511 H H H H H O H H 2-OMe,4-CF.sub.3 1 A-9512 H H H H H O H H 2-OMe,5-CF.sub.3 1 A-9513 H H H H H O H H 2-OMe,6-CF.sub.3 1 A-9514 H H H H H O H H 3-OMe,2-CF.sub.3 1
(269) TABLE-US-00168 TABLE 168 com- pound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9515 H H H H H O H H 3-OMe,4-CF.sub.3 1 A-9516 H H H H H O H H 3-OMe,5-CF.sub.3 1 A-9517 H H H H H O H H 3-OMe,6-CF.sub.3 1 A-9518 H H H H H O H H 4-OMe,2-CF.sub.3 1 A-9519 H H H H H O H H 4-OMe,3-CF.sub.3 1 A-9520 H H H H H O H H 2-CHF.sub.2,3-F 1 A-9521 H H H H H O H H 2-CHF.sub.2,4-F 1 A-9522 H H H H H O H H 2-CHF.sub.2,5-F 1 A-9523 H H H H H O H H 2-CHF.sub.2,6-F 1 A-9524 H H H H H O H H 2-CHF.sub.2,3-Me 1 A-9525 H H H H H O H H 2-CHF.sub.2,4-Me 1 A-9526 H H H H H O H H 2-CHF.sub.2,5-Me 1 A-9527 H H H H H O H H 2-CHF.sub.2,6-Me 1 A-9528 H H H H H O H H 2-cyclopropyl,3-F 1 A-9529 H H H H H O H H 2-cyclopropyl,4-F 1 A-9530 H H H H H O H H 2-cyclopropyl,5-F 1 A-9531 H H H H H O H H 2-cyclopropyl,6-F 1 A-9532 H H H H H O H H 2-cyclopropyl,3-Me 1 A-9533 H H H H H O H H 2-cyclopropyl,4-Me 1 A-9534 H H H H H O H H 2-cyclopropyl,5-Me 1 A-9535 H H H H H O H H 2-cyclopropyl,6-Me 1 A-9536 H H H H H O H H 2-ethenyl,3-F 1 A-9537 H H H H H O H H 2-ethenyl,4-F 1 A-9538 H H H H H O H H 2-ethenyl,5-F 1 A-9539 H H H H H O H H 2-ethenyl,6-F 1 A-9540 H H H H H O H H 2-ethenyl,3-Me 1 A-9541 H H H H H O H H 2-ethenyl,4-Me 1 A-9542 H H H H H O H H 2-ethenyl,5-Me 1 A-9543 H H H H H O H H 2-ethenyl,6-Me 1 A-9544 H H H H H O H H 2-OEt,3-F 1 A-9545 H H H H H O H H 2-OEt,4-F 1 A-9546 H H H H H O H H 2-OEt,5-F 1 A-9547 H H H H H O H H 2-OEt,6-F 1 A-9548 H H H H H O H H 2-OEt,3-Cl 1 A-9549 H H H H H O H H 2-OEt,4-Cl 1 A-9550 H H H H H O H H 2-OEt,5-Cl 1 A-9551 H H H H H O H H 2-OEt,6-Cl 1 A-9552 H H H H H O H H 2-OEt,3-Me 1 A-9553 H H H H H O H H 2-OEt,4-Me 1 A-9554 H H H H H O H H 2-OEt,5-Me 1 A-9555 H H H H H O H H 2-OEt,6-Me 1 A-9556 H H H H H O H H 2-OPr,3-F 1 A-9557 H H H H H O H H 2-OPr,4-F 1 A-9558 H H H H H O H H 2-OPr,5-F 1 A-9559 H H H H H O H H 2-OPr,6-F 1 A-9560 H H H H H O H H 2-OPr,3-Me 1 A-9561 H H H H H O H H 2-OPr,4-Me 1 A-9562 H H H H H O H H 2-OPr,5-Me 1 A-9563 H H H H H O H H 2-OPr,6-Me 1 A-9564 H H H H H O H H 2-O(i-Pr),3-F 1 A-9565 H H H H H O H H 2-O(i-Pr),4-F 1 A-9566 H H H H H O H H 2-O(i-Pr),5-F 1 A-9567 H H H H H O H H 2-O(i-Pr),6-F 1 A-9568 H H H H H O H H 2-O(i-Pr),3-Me 1 A-9569 H H H H H O H H 2-O(i-Pr),4-Me 1 A-9570 H H H H H O H H 2-O(i-Pr),5-Me 1 A-9571 H H H H H O H H 2-O(i-Pr),6-Me 1
(270) TABLE-US-00169 TABLE 169 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9572 H H H H H O H H 2-OCF.sub.3,3-F 1 A-9573 H H H H H O H H 2-OCF.sub.3,4-F 1 A-9574 H H H H H O H H 2-OCF.sub.3,5-F 1 A-9575 H H H H H O H H 2-OCF.sub.3,6-F 1 A-9576 H H H H H O H H 2-OCF.sub.3,3-Me 1 A-9577 H H H H H O H H 2-OCF.sub.3,4-Me 1 A-9578 H H H H H O H H 2-OCF.sub.3,5-Me 1 A-9579 H H H H H O H H 2-OCF.sub.3,6-Me 1 A-9580 H H H H H O H H 2-OCHF.sub.2,3-F 1 A-9581 H H H H H O H H 2-OCHF.sub.2,4-F 1 A-9582 H H H H H O H H 2-OCHF.sub.2,5-F 1 A-9583 H H H H H O H H 2-OCHF.sub.2,6-F 1 A-9584 H H H H H O H H 2-OCHF.sub.2,3-Me 1 A-9585 H H H H H O H H 2-OCHF.sub.2,4-Me 1 A-9586 H H H H H O H H 2-OCHF.sub.2,5-Me 1 A-9587 H H H H H O H H 2-OCHF.sub.2,6-Me 1 A-9588 H H H H H O H H 2-(cyclopropyloxy),3-F 1 A-9589 H H H H H O H H 2-(cyclopropyloxy),4-F 1 A-9590 H H H H H O H H 2-(cyclopropyloxy),5-F 1 A-9591 H H H H H O H H 2-(cyclopropyloxy),6-F 1 A-9592 H H H H H O H H 2-(cyclopropyloxy),3-Me 1 A-9593 H H H H H O H H 2-(cyclopropyloxy),4-Me 1 A-9594 H H H H H O H H 2-(cyclopropyloxy),5-Me 1 A-9595 H H H H H O H H 2-(cyclopropyloxy),6-Me 1 A-9596 H H H H H O H H 2-(oxiran-2-yl),3-F 1 A-9597 H H H H H O H H 2-(oxiran-2-yl),4-F 1 A-9598 H H H H H O H H 2-(oxiran-2-yl),5-F 1 A-9599 H H H H H O H H 2-(oxiran-2-yl),6-F 1 A-9600 H H H H H O H H 2-(oxiran-2-yl),3-Me 1 A-9601 H H H H H O H H 2-(oxiran-2-yl),4-Me 1 A-9602 H H H H H O H H 2-(oxiran-2-yl),5-Me 1 A-9603 H H H H H O H H 2-(oxiran-2-yl),6-Me 1 A-9604 H H H H H O H H 2-(oxiran-2-ylmethyl),3-F 1 A-9605 H H H H H O H H 2-(oxiran-2-ylmethyl),4-F 1 A-9606 H H H H H O H H 2-(oxiran-2-ylmethyl),5-F 1 A-9607 H H H H H O H H 2-(oxiran-2-ylmethyl),6-F 1 A-9608 H H H H H O H H 2-(oxiran-2-ylmethyl),3-Me 1 A-9609 H H H H H O H H 2-(oxiran-2-ylmethyl),4-Me 1 A-9610 H H H H H O H H 2-(oxiran-2-ylmethyl),5-Me 1 A-9611 H H H H H O H H 2-(oxiran-2-ylmethyl),6-Me 1 A-9612 H H H H H O H H 2-SMe,3-F 1 A-9613 H H H H H O H H 2-SMe,4-F 1 A-9614 H H H H H O H H 2-SMe,5-F 1 A-9615 H H H H H O H H 2-SMe,6-F 1 A-9616 H H H H H O H H 2-SMe,3-Me 1 A-9617 H H H H H O H H 2-SMe,4-Me 1 A-9618 H H H H H O H H 2-SMe,5-Me 1 A-9619 H H H H H O H H 2-SMe,6-Me 1 A-9620 H H H H H O H H 2-SEt,3-F 1 A-9621 H H H H H O H H 2-SEt,4-F 1 A-9622 H H H H H O H H 2-SEt,5-F 1 A-9623 H H H H H O H H 2-SEt,6-F 1 A-9624 H H H H H O H H 2-SEt,3-Me 1 A-9625 H H H H H O H H 2-SEt,4-Me 1 A-9626 H H H H H O H H 2-SEt,5-Me 1 A-9627 H H H H H O H H 2-SEt,6-Me 1 A-9628 H H H H H O H H 2-S(?O)Me,3-F 1
(271) TABLE-US-00170 TABLE 170 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9629 H H H H H O H H 2-S(?O)Me,4-F 1 A-9630 H H H H H O H H 2-S(?O)Me,5-F 1 A-9631 H H H H H O H H 2-S(?O)Me,6-F 1 A-9632 H H H H H O H H 3-S(?O)Me,2-F 1 A-9633 H H H H H O H H 3-S(?O)Me,4-F 1 A-9634 H H H H H O H H 3-S(?O)Me,5-F 1 A-9635 H H H H H O H H 3-S(?O)Me,6-F 1 A-9636 H H H H H O H H 2-S(?O)Me,3-Me 1 A-9637 H H H H H O H H 2-S(?O)Me,4-Me 1 A-9638 H H H H H O H H 2-S(?O)Me,5-Me 1 A-9639 H H H H H O H H 2-S(?O)Me,6-Me 1 A-9640 H H H H H O H H 3-S(?O)Me,2-Me 1 A-9641 H H H H H O H H 3-S(?O)Me,4-Me 1 A-9642 H H H H H O H H 3-S(?O)Me,5-Me 1 A-9643 H H H H H O H H 3-S(?O)Me,6-Me 1 A-9644 H H H H H O H H 2-S(?O).sub.2Me,3F 1 A-9645 H H H H H O H H 2-S(?O).sub.2Me,4-F 1 A-9646 H H H H H O H H 2-S(?O).sub.2Me,5-F 1 A-9647 H H H H H O H H 2-S(?O).sub.2Me,6-F 1 A-9648 H H H H H O H H 2-S(?O).sub.2Me,3-Me 1 A-9649 H H H H H O H H 2-S(?O).sub.2Me,4-Me 1 A-9650 H H H H H O H H 2-S(?O).sub.2Me,5-Me 1 A-9651 H H H H H O H H 2-S(?O).sub.2Me,6-Me 1 A-9652 H H H H H O H H 2-SCF.sub.3,3-F 1 A-9653 H H H H H O H H 2-SCF.sub.3,4-F 1 A-9654 H H H H H O H H 2-SCF.sub.3,5-F 1 A-9655 H H H H H O H H 2-SCF.sub.3,6-F 1 A-9656 H H H H H O H H 2-SCF.sub.3,3-Me 1 A-9657 H H H H H O H H 2-SCF.sub.3,4-Me 1 A-9658 H H H H H O H H 2-SCF.sub.3,5-Me 1 A-9659 H H H H H O H H 2-SCF.sub.3,6-Me 1 A-9660 H H H H H O H H 2-S(?O)CF.sub.3,3-F 1 A-9661 H H H H H O H H 2-S(?O)CF.sub.3,4-F 1 A-9662 H H H H H O H H 2-S(?O)CF.sub.3,5-F 1 A-9663 H H H H H O H H 2-S(?O)CF.sub.3,6-F 1 A-9664 H H H H H O H H 2-S(?O)CF.sub.3,3-Me 1 A-9665 H H H H H O H H 2-S(?O)CF.sub.3,4-Me 1 A-9666 H H H H H O H H 2-S(?O)CF.sub.3,5-Me 1 A-9667 H H H H H O H H 2-S(?O)CF.sub.3,6-Me 1 A-9668 H H H H H O H H 2-S(?O).sub.2CF.sub.3,3-F 1 A-9669 H H H H H O H H 2-S(?O).sub.2CF.sub.3,4-F 1 A-9670 H H H H H O H H 2-S(?O).sub.2CF.sub.3,5-F 1 A-9671 H H H H H O H H 2-S(?O).sub.2CF.sub.3,6-F 1 A-9672 H H H H H O H H 2-S(?O).sub.2CF.sub.3,3-Me 1 A-9673 H H H H H O H H 2-S(?O).sub.2CF.sub.3,4-Me 1 A-9674 H H H H H O H H 2-S(?O).sub.2CF.sub.3,5-Me 1 A-9675 H H H H H O H H 2-S(?O).sub.2CF.sub.3,6-Me 1 A-9676 H H H H H O H H 2-(cyclopropylthio),3-F 1 A-9677 H H H H H O H H 2-(cyclopropylthio),4-F 1 A-9678 H H H H H O H H 2-(cyclopropylthio),5-F 1 A-9679 H H H H H O H H 2-(cyclopropylthio),6-F 1 A-9680 H H H H H O H H 2-(cyclopropylthio),3-Me 1 A-9681 H H H H H O H H 2-(cyclopropylthio),4-Me 1 A-9682 H H H H H O H H 2-(cyclopropylthio),5-Me 1 A-9683 H H H H H O H H 2-(cyclopropylthio),6-Me 1 A-9684 H H H H H O H H 2-C(?O)Me,3-F 1 A-9685 H H H H H O H H 2-C(?O)Me,4-F 1
(272) TABLE-US-00171 TABLE 171 com- pound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9686 H H H H H O H H 2-C(?O)Me,5-F 1 A-9687 H H H H H O H H 2-C(?O)Me,6-F 1 A-9688 H H H H H O H H 2-C(?O)Me,3-Me 1 A-9689 H H H H H O H H 2-C(?O)Me,4-Me 1 A-9690 H H H H H O H H 2-C(?O)Me,5-Me 1 A-9691 H H H H H O H H 2-C(?O)Me,6-Me 1 A-9692 H H H H H O H H 3-C(?O)Me,2-F 1 A-9693 H H H H H O H H 3-C(?O)Me,4-F 1 A-9694 H H H H H O H H 3-C(?O)Me,5-F 1 A-9695 H H H H H O H H 3-C(?O)Me,6-F 1 A-9696 H H H H H O H H 3-C(?O)Me,2-Me 1 A-9697 H H H H H O H H 3-C(?O)Me,4-Me 1 A-9698 H H H H H O H H 3-C(?O)Me,5-Me 1 A-9699 H H H H H O H H 3-C(?O)Me,6-Me 1 A-9700 H H H H H O H H 2-C(?O)OMe,3-F 1 A-9701 H H H H H O H H 2-C(?O)OMe,4-F 1 A-9702 H H H H H O H H 2-C(?O)OMe,5-F 1 A-9703 H H H H H O H H 2-C(?O)OMe,6-F 1 A-9704 H H H H H O H H 2-C(?O)OMe,3-Me 1 A-9705 H H H H H O H H 2-C(?O)OMe,4-Me 1 A-9706 H H H H H O H H 2-C(?O)OMe,5-Me 1 A-9707 H H H H H O H H 2-C(?O)OMe,6-Me 1 A-9708 H H H H H O H H 2-C(?O)OEt,3-F 1 A-9709 H H H H H O H H 2-C(?O)OEt,4-F 1 A-9710 H H H H H O H H 2-C(?O)OEt,5-F 1 A-9711 H H H H H O H H 2-C(?O)OEt,6-F 1 A-9712 H H H H H O H H 2-C(?O)OEt,3-Me 1 A-9713 H H H H H O H H 2-C(?O)OEt,4-Me 1 A-9714 H H H H H O H H 2-C(?O)OEt,5-Me 1 A-9715 H H H H H O H H 2-C(?O)OEt,6-Me 1 A-9716 H H H H H O H H 2-C(?O)NH.sub.2,3-F 1 A-9717 H H H H H O H H 2-C(?O)NH.sub.2,4-F 1 A-9718 H H H H H O H H 2-C(?O)NH.sub.2,5-F 1 A-9719 H H H H H O H H 2-C(?O)NH.sub.2,6-F 1 A-9720 H H H H H O H H 2-C(?O)NH.sub.2,3-Me 1 A-9721 H H H H H O H H 2-C(?O)NH.sub.2,4-Me 1 A-9722 H H H H H O H H 2-C(?O)NH.sub.2,5-Me 1 A-9723 H H H H H O H H 2-C(?O)NH.sub.2,6-Me 1 A-9724 H H H H H O H H 2-C(?O)NHMe,3-F 1 A-9725 H H H H H O H H 2-C(?O)NHMe,4-F 1 A-9726 H H H H H O H H 2-C(?O)NHMe,5-F 1 A-9727 H H H H H O H H 2-C(?O)NHMe,6-F 1 A-9728 H H H H H O H H 2-C(?O)NHMe,3-Me 1 A-9729 H H H H H O H H 2-C(?O)NHMe,4-Me 1 A-9730 H H H H H O H H 2-C(?O)NHMe,5-Me 1 A-9731 H H H H H O H H 2-C(?O)NHMe,6-Me 1 A-9732 H H H H H O H H 2-C(?O)NMe.sub.2,3-F 1 A-9733 H H H H H O H H 2-C(?O)NMe.sub.2,4-F 1 A-9734 H H H H H O H H 2-C(?O)NMe.sub.2,5-F 1 A-9735 H H H H H O H H 2-C(?O)NMe.sub.2,6-F 1 A-9736 H H H H H O H H 2-C(?O)NMe.sub.2,3-Me 1 A-9737 H H H H H O H H 2-C(?O)NMe.sub.2,4-Me 1 A-9738 H H H H H O H H 2-C(?O)NMe.sub.2,5-Me 1 A-9739 H H H H H O H H 2-C(?O)NMe.sub.2,6-Me 1 A-9740 H H H H H O H H 2-CH.sub.2OH,3-F 1 A-9741 H H H H H O H H 2-CH.sub.2OH,4-F 1 A-9742 H H H H H O H H 2-CH.sub.2OH,5-F 1
(273) TABLE-US-00172 TABLE 172 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9743 H H H H H O H H 2-CH.sub.2OH,6-F 1 A-9744 H H H H H O H H 2-CH.sub.2OH,3-Me 1 A-9745 H H H H H O H H 2-CH.sub.2OH,4-Me 1 A-9746 H H H H H O H H 2-CH.sub.2OH,5-Me 1 A-9747 H H H H H O H H 2-CH.sub.2OH,6-Me 1 A-9748 H H H H H O H H 2-CH.sub.2OCH.sub.3,3F 1 A-9749 H H H H H O H H 2-CH.sub.2OCH.sub.3,4-F 1 A-9750 H H H H H O H H 2-CH.sub.2OCH.sub.3,5-F 1 A-9751 H H H H H O H H 2-CH.sub.2OCH.sub.3,6-F 1 A-9752 H H H H H O H H 2-CH.sub.2OCH.sub.3,3-Me 1 A-9753 H H H H H O H H 2-CH.sub.2OCH.sub.3,4-Me 1 A-9754 H H H H H O H H 2-CH.sub.2OCH.sub.3,5-Me 1 A-9755 H H H H H O H H 2-CH.sub.2OCH.sub.3,6-Me 1 A-9756 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,3-F 1 A-9757 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,4-F 1 A-9758 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,5-F 1 A-9759 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-F 1 A-9760 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,3-Me 1 A-9761 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,4-Me 1 A-9762 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,5-Me 1 A-9763 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Me 1 A-9764 H H H H H O H H 2-OC(?O)CH.sub.3,3-F 1 A-9765 H H H H H O H H 2-OC(?O)CH.sub.3,4-F 1 A-9766 H H H H H O H H 2-OC(?O)CH.sub.3,5-F 1 A-9767 H H H H H O H H 2-OC(?O)CH.sub.3,6-F 1 A-9768 H H H H H O H H 2-OC(?O)CH.sub.3,3-Me 1 A-9769 H H H H H O H H 2-OC(?O)CH.sub.3,4-Me 1 A-9770 H H H H H O H H 2-OC(?O)CH.sub.3,5-Me 1 A-9771 H H H H H O H H 2-OC(?O)CH.sub.3,6-Me 1 A-9772 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,3-F 1 A-9773 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,4-F 1 A-9774 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,5-F 1 A-9775 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,6-F 1 A-9776 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,3-Me 1 A-9777 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,4-Me 1 A-9778 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,5-Me 1 A-9779 H H H H H O H H 2-OS(?O).sub.2CH.sub.3,6-Me 1 A-9780 H H H H H O H H 2-CH.sub.2SCH.sub.3,3-F 1 A-9781 H H H H H O H H 2-CH.sub.2SCH.sub.3,4-F 1 A-9782 H H H H H O H H 2-CH.sub.2SCH.sub.3,5-F 1 A-9783 H H H H H O H H 2-CH.sub.2SCH.sub.3,6-F 1 A-9784 H H H H H O H H 2-CH.sub.2SCH.sub.3,3-Me 1 A-9785 H H H H H O H H 2-CH.sub.2SCH.sub.3,4-Me 1 A-9786 H H H H H O H H 2-CH.sub.2SCH.sub.3,5-Me 1 A-9787 H H H H H O H H 2-CH.sub.2SCH.sub.3,6-Me 1 A-9788 H H H H H O H H 2-CH.sub.2SCF.sub.3,3-F 1 A-9789 H H H H H O H H 2-CH.sub.2SCF.sub.3,4-F 1 A-9790 H H H H H O H H 2-CH.sub.2SCF.sub.3,5-F 1 A-9791 H H H H H O H H 2-CH.sub.2SCF.sub.3,6-F 1 A-9792 H H H H H O H H 2-CH.sub.2SCF.sub.3,3-Me 1 A-9793 H H H H H O H H 2-CH.sub.2SCF.sub.3,4-Me 1 A-9794 H H H H H O H H 2-CH.sub.2SCF.sub.3,5-Me 1 A-9795 H H H H H O H H 2-CH.sub.2SCF.sub.3,6-Me 1 A-9796 H H H H H O H H 2-(benzyloxy),3-F 1 A-9797 H H H H H O H H 2-(benzyloxy),4-F 1 A-9798 H H H H H O H H 2-(benzyloxy),5-F 1 A-9799 H H H H H O H H 2-(benzyloxy),6-F 1
(274) TABLE-US-00173 TABLE 173 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9800 H H H H H O H H 2-(benzyloxy),3-Me 1 A-9801 H H H H H O H H 2-(benzyloxy),4-Me 1 A-9802 H H H H H O H H 2-(benzyloxy),5-Me 1 A-9803 H H H H H O H H 2-(benzyloxy),6-Me 1 A-9804 H H H H H O H H 2-NH.sub.2,3-F 1 A-9805 H H H H H O H H 2-NH.sub.2,4-F 1 A-9806 H H H H H O H H 2-NH.sub.2,5-F 1 A-9807 H H H H H O H H 2-NH.sub.2,6-F 1 A-9808 H H H H H O H H 2-NH.sub.2,3-Me 1 A-9809 H H H H H O H H 2-NH.sub.2,4-Me 1 A-9810 H H H H H O H H 2-NH.sub.2,5-Me 1 A-9811 H H H H H O H H 2-NH.sub.2,6-Me 1 A-9812 H H H H H O H H 2-NHMe,3-F 1 A-9813 H H H H H O H H 2-NHMe,4-F 1 A-9814 H H H H H O H H 2-NHMe,5-F 1 A-9815 H H H H H O H H 2-NHMe,6-F 1 A-9816 H H H H H O H H 2-NHMe,3-Me 1 A-9817 H H H H H O H H 2-NHMe,4-Me 1 A-9818 H H H H H O H H 2-NHMe,5-Me 1 A-9819 H H H H H O H H 2-NHMe,6-Me 1 A-9820 H H H H H O H H 2-NHEt,3-F 1 A-9821 H H H H H O H H 2-NHEt,4-F 1 A-9822 H H H H H O H H 2-NHEt,5-F 1 A-9823 H H H H H O H H 2-NHEt,6-F 1 A-9824 H H H H H O H H 2-NHEt,3-Me 1 A-9825 H H H H H O H H 2-NHEt,4-Me 1 A-9826 H H H H H O H H 2-NHEt,5-Me 1 A-9827 H H H H H O H H 2-NHEt,6-Me 1 A-9828 H H H H H O H H 2-NMe.sub.2,3-F 1 A-9829 H H H H H O H H 2-NMe.sub.2,4-F 1 A-9830 H H H H H O H H 2-NMe.sub.2,5-F 1 A-9831 H H H H H O H H 2-NMe.sub.2,6-F 1 A-9832 H H H H H O H H 2-NMe.sub.2,3-Me 1 A-9833 H H H H H O H H 2-NMe.sub.2,4-Me 1 A-9834 H H H H H O H H 2-NMe.sub.2,5-Me 1 A-9835 H H H H H O H H 2-NMe.sub.2,6-Me 1 A-9836 H H H H H O H H 2-NEt.sub.2,3F 1 A-9837 H H H H H O H H 2-NEt.sub.2,4-F 1 A-9838 H H H H H O H H 2-NEt.sub.2,5-F 1 A-9839 H H H H H O H H 2-NEt.sub.2,6-F 1 A-9840 H H H H H O H H 2-NEt.sub.2,3Me 1 A-9841 H H H H H O H H 2-NEt.sub.2,4-Me 1 A-9842 H H H H H O H H 2-NEt.sub.2,5-Me 1 A-9843 H H H H H O H H 2-NEt.sub.2,6-Me 1 A-9844 H H H H H O H H 2-CHO,3-F 1 A-9845 H H H H H O H H 2-CHO,4-F 1 A-9846 H H H H H O H H 2-CHO,5-F 1 A-9847 H H H H H O H H 2-CHO,6-F 1 A-9848 H H H H H O H H 2-CHO,3-Me 1 A-9849 H H H H H O H H 2-CHO,4-Me 1 A-9850 H H H H H O H H 2-CHO,5-Me 1 A-9851 H H H H H O H H 2-CHO,6-Me 1 A-9852 H H H H H O H H 2-C(?O)OH,3-F 1 A-9853 H H H H H O H H 2-C(?O)OH,4-F 1 A-9854 H H H H H O H H 2-C(?O)OH,5-F 1 A-9855 H H H H H O H H 2-C(?O)OH,6-F 1 A-9856 H H H H H O H H 2-C(?O)OH,3-Me 1
(275) TABLE-US-00174 TABLE 174 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9857 H H H H H O H H 2-C(?O)OH,4-Me 1 A-9858 H H H H H O H H 2-C(?O)OH,5-Me 1 A-9859 H H H H H O H H 2-C(?O)OH,6-Me 1 A-9860 H H H H H O H H 2-(1,3-dioxolan-2-yl),3-F 1 A-9861 H H H H H O H H 2-(1,3-dioxolan-2-yl),4-F 1 A-9862 H H H H H O H H 2-(1,3-dioxolan-2-yl),5-F 1 A-9863 H H H H H O H H 2-(1,3-dioxolan-2-yl),6-F 1 A-9864 H H H H H O H H 2-(1,3-dioxolan-2-yl),3-Me 1 A-9865 H H H H H O H H 2-(1,3-dioxolan-2-yl),4-Me 1 A-9866 H H H H H O H H 2-(1,3-dioxolan-2-yl),5-Me 1 A-9867 H H H H H O H H 2-(1,3-dioxolan-2-yl),6-Me 1 A-9868 H H H H H O H H 2-(1,3-dioxan-2-yl),3-F 1 A-9869 H H H H H O H H 2-(1,3-dioxan-2-yl),4-F 1 A-9870 H H H H H O H H 2-(1,3-dioxan-2-yl),5-F 1 A-9871 H H H H H O H H 2-(1,3-dioxan-2-yl),6-F 1 A-9872 H H H H H O H H 2-(1,3-dioxan-2-yl),3-Me 1 A-9873 H H H H H O H H 2-(1,3-dioxan-2-yl),4-Me 1 A-9874 H H H H H O H H 2-(1,3-dioxan-2-yl),5-Me 1 A-9875 H H H H H O H H 2-(1,3-dioxan-2-yl),6-Me 1 A-9876 H H H H H O H H 2-(thiazol-2-yl),3-F 1 A-9877 H H H H H O H H 2-(thiazol-2-yl),4-F 1 A-9878 H H H H H O H H 2-(thiazol-2-yl),5-F 1 A-9879 H H H H H O H H 2-(thiazol-2-yl),6-F 1 A-9880 H H H H H O H H 2-(thiazol-2-yl),3-Me 1 A-9881 H H H H H O H H 2-(thiazol-2-yl),4-Me 1 A-9882 H H H H H O H H 2-(thiazol-2-yl),5-Me 1 A-9883 H H H H H O H H 2-(thiazol-2-yl),6-Me 1 A-9884 H H H H H O H H 2-(oxazol-2-yl),3-F 1 A-9885 H H H H H O H H 2-(oxazol-2-yl),4-F 1 A-9886 H H H H H O H H 2-(oxazol-2-yl),5-F 1 A-9887 H H H H H O H H 2-(oxazol-2-yl),6-F 1 A-9888 H H H H H O H H 2-(oxazol-2-yl),3-Me 1 A-9889 H H H H H O H H 2-(oxazol-2-yl),4-Me 1 A-9890 H H H H H O H H 2-(oxazol-2-yl),5-Me 1 A-9891 H H H H H O H H 2-(oxazol-2-yl),6-Me 1 A-9892 H H H H H O H H 2-CH?NOH,3F 1 A-9893 H H H H H O H H 2-CH?NOH,4-F 1 A-9894 H H H H H O H H 2-CH?NOH,5-F 1 A-9895 H H H H H O H H 2-CH?NOH,6-F 1 A-9896 H H H H H O H H 2-CH?NOH,3-Me 1 A-9897 H H H H H O H H 2-CH?NOH,4-Me 1 A-9898 H H H H H O H H 2-CH?NOH,5-Me 1 A-9899 H H H H H O H H 2-CH?NOH,6-Me 1 A-9900 H H H H H O H H 2-CH?NOMe,3-F 1 A-9901 H H H H H O H H 2-CH?NOMe,4-F 1 A-9902 H H H H H O H H 2-CH?NOMe,5-F 1 A-9903 H H H H H O H H 2-CH?NOMe,6-F 1 A-9904 H H H H H O H H 2-CH?NOMe,3-Me 1 A-9905 H H H H H O H H 2-CH?NOMe,4-Me 1 A-9906 H H H H H O H H 2-CH?NOMe,5-Me 1 A-9907 H H H H H O H H 2-CH?NOMe,6-Me 1 A-9908 H H H H H O H H 2-CN,3-F 1 A-9909 H H H H H O H H 2-CN,4-F 1 A-9910 H H H H H O H H 2-CN,5-F 1 A-9911 H H H H H O H H 2-CN,6-F 1 A-9912 H H H H H O H H 2-CN,3-Cl 1 A-9913 H H H H H O H H 2-CN,4-Cl 1
(276) TABLE-US-00175 TABLE 175 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9914 H H H H H O H H 2-CN,5-Cl 1 A-9915 H H H H H O H H 2-CN,6-Cl 1 A-9916 H H H H H O H H 2-CN,3-Me 1 A-9917 H H H H H O H H 2-CN,4-Me 1 A-9918 H H H H H O H H 2-CN,5-Me 1 A-9919 H H H H H O H H 2-CN,6-Me 1 A-9920 H H H H H O H H 2-CN,3-OMe 1 A-9921 H H H H H O H H 2-CN,4-OMe 1 A-9922 H H H H H O H H 2-CN,5-OMe 1 A-9923 H H H H H O H H 2-CN,6-OMe 1 A-9924 H H H H H O H H 3-CN,2-F 1 A-9925 H H H H H O H H 3-CN,4-F 1 A-9926 H H H H H O H H 3-CN,5-F 1 A-9927 H H H H H O H H 3-CN,6-F 1 A-9928 H H H H H O H H 3-CN,2-Cl 1 A-9929 H H H H H O H H 3-CN,4-Cl 1 A-9930 H H H H H O H H 3-CN,5-Cl 1 A-9931 H H H H H O H H 3-CN,6-Cl 1 A-9932 H H H H H O H H 3-CN,2-Me 1 A-9933 H H H H H O H H 3-CN,4-Me 1 A-9934 H H H H H O H H 3-CN,5-Me 1 A-9935 H H H H H O H H 3-CN,6-Me 1 A-9936 H H H H H O H H 3-CN,2-OMe 1 A-9937 H H H H H O H H 3-CN,4-OMe 1 A-9938 H H H H H O H H 3-CN,5-OMe 1 A-9939 H H H H H O H H 3-CN,6-OMe 1 A-9940 H H H H H O H H 4-CN,2-F 1 A-9941 H H H H H O H H 4-CN,3-F 1 A-9942 H H H H H O H H 4-CN,2-Cl 1 A-9943 H H H H H O H H 4-CN,3-Cl 1 A-9944 H H H H H O H H 4-CN,2-Me 1 A-9945 H H H H H O H H 4-CN,3-Me 1 A-9946 H H H H H O H H 4-CN,2-OMe 1 A-9947 H H H H H O H H 4-CN,3-OMe 1 A-9948 H H H H H O H H 2-NO.sub.2,3-F 1 A-9949 H H H H H O H H 2-NO.sub.2,4-F 1 A-9950 H H H H H O H H 2-NO.sub.2,5-F 1 A-9951 H H H H H O H H 2-NO.sub.2,6-F 1 A-9952 H H H H H O H H 2-NO.sub.2,3-Me 1 A-9953 H H H H H O H H 2-NO.sub.2,4-Me 1 A-9954 H H H H H O H H 2-NO.sub.2,5-Me 1 A-9955 H H H H H O H H 2-NO.sub.2,6-Me 1 A-9956 H H H H H O H H 2-Me,3,4-F.sub.2 1 A-9957 H H H H H O H H 2-Me,3,5-F.sub.2 1 A-9958 H H H H H O H H 2-Me,3,6-F.sub.2 1 A-9959 H H H H H O H H 2-Me,4,5-F.sub.2 1 A-9960 H H H H H O H H 2-OMe,3,4-F.sub.2 1 A-9961 H H H H H O H H 2-OMe,3,5-F.sub.2 1 A-9962 H H H H H O H H 2-OMe,3,6-F.sub.2 1 A-9963 H H H H H O H H 2-OMe,4,5-F.sub.2 1 A-9964 H H H H H O H H 2-(CH.sub.2).sub.3-3 1 A-9965 H H H H H O H H 2-(CH.sub.2).sub.4-3 1 A-9966 H H H H H O H H 2-(OCH.sub.2CH.sub.2)-3 1 A-9967 H H H H H O H H 2-(OCH.sub.2CH.sub.2CH.sub.2)-3 1 A-9968 H H H H H O H H 2-(CH.sub.2CH.sub.2O)-3 1 A-9969 H H H H H O H H 2-(CH.sub.2CH.sub.2CH.sub.2O)-3 1 A-9970 H H H H H O H H 3-(CH.sub.2).sub.3-4 1
(277) TABLE-US-00176 TABLE 176 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 (R.sup.8).sub.m p A-9971 H H H H H O H H 3-(CH.sub.2).sub.4-4 1 A-9972 H H H H H O H H 3-(OCH.sub.2CH.sub.2)-4 1 A-9973 H H H H H O H H 3-(OCH.sub.2CH.sub.2CH.sub.2)-4 1 A-9974 H H H H H O H H 3-(CH.sub.2CH.sub.2O)-4 1 A-9975 H H H H H O H H 3-(CH.sub.2CH.sub.2CH.sub.2O)-4 1 A-9976 H H H H H O H H 2-(OCH.sub.2O)-3 1 A-9977 H H H H H O H H 3-(OCH.sub.2O)-4 1 A-9978 H H H H H O H H 2-(OCH.sub.2CH.sub.2O)-3 1 A-9979 H H H H H O H H 3-(OCH.sub.2CH.sub.2O)-4 1 A-9980 H H H H H O H H 2-(OCF.sub.2O)-3 1 A-9981 H H H H H O H H 3-(OCF.sub.2O)-4 1 A-9982 H H H H H O H H 2-Me,6-Et 1 A-9983 H H H H H O H H 2-Me,4,5-F.sub.2 1 A-9984 H H H H H O H H 2-cyclopropyl,6-OMe 1 A-9985 H H H H H O H H 2-Me,5-Et 1 A-9986 H H H H H O H H 2,6-Et.sub.2 1 A-9987 H H H H H O H H 2-Et,6-F 1 A-9988 H H H H H O H H 2-CH.sub.2OCH.sub.3,6-Cl 1 A-9989 H H H H H O H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 1 A-9990 H H H H H O H H 2-CH.sub.2NMe.sub.2 1 A-9991 H H H H H O H H 2-CH.sub.2OCH.sub.3,6-OMe 0 A-9992 H H H H H O H H 2-CH.sub.2OCH.sub.3,6-OMe 1 A-9993 H H H H H O pyridin-2-ylmethyl H 2-Me 0 A-9994 H H H H H O pyridin-3-ylmethyl H 2-Me 0
(278) TABLE-US-00177 TABLE 177
(279) TABLE-US-00178 TABLE 178 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-0053 H H H H H O H H 3-F-6-OMe-pyridin-2-yl 0 B-0054 H H H H H O H H 3-Cl-4-F-pyridin-2-yl 0 B-0055 H H H H H O H H 3-Cl-5-F-pyridin-2-yl 0 B-0056 H H H H H O H H 3-Cl-6-F-pyridin-2-yl 0 B-0057 H H H H H O H H 3-Cl-4-Me-pyridin-2-yl 0 B-0058 H H H H H O H H 3-Cl-5-Me-pyridin-2-yl 0 B-0059 H H H H H O H H 3-Cl-6-Me-pyridin-2-yl 0 B-0060 H H H H H O H H 3-Me-4-F-pyridin-2-yl 0 B-0061 H H H H H O H H 3-Me-5-F-pyridin-2-yl 0 B-0062 H H H H H O H H 3-Me-6-F-pyridin-2-yl 0 B-0063 H H H H H O H H 3-Me-4-Cl-pyridin-2-yl 0 B-0064 H H H H H O H H 3-Me-5-Cl-pyridin-2-yl 0 B-0065 H H H H H O H H 3-Me-6-Cl-pyridin-2-yl 0 B-0066 H H H H H O H H 3,4-(Me).sub.2-pyridin-2-yl 0 B-0067 H H H H H O H H 3,5-(Me).sub.2-pyridin-2-yl 0 B-0068 H H H H H O H H 3,6-(Me).sub.2-pyridin-2-yl 0 B-0069 H H H H H O H H 3-Me-4-OMe-pyridin-2-yl 0 B-0070 H H H H H O H H 3-Me-5-OMe-pyridin-2-yl 0 B-0071 H H H H H O H H 3-Me-6-OMe-pyridin-2-yl 0 B-0072 H H H H H O H H 3-CF.sub.3-4-F-pyridin-2-yl 0 B-0073 H H H H H O H H 3-CF.sub.3-5-F-pyridin-2-yl 0 B-0074 H H H H H O H H 3-CF.sub.3-6-F-pyridin-2-yl 0 B-0075 H H H H H O H H 3-CF.sub.3-4-Me-pyridin-2-yl 0 B-0076 H H H H H O H H 3-CF.sub.3-5-Me-pyridin-2-yl 0 B-0077 H H H H H O H H 3-CF.sub.3-6-Me-pyridin-2-yl 0 B-0078 H H H H H O H H 3-OMe-4-F-pyridin-2-yl 0 B-0079 H H H H H O H H 3-OMe-5-F-pyridin-2-yl 0 B-0080 H H H H H O H H 3-OMe-6-F-pyridin-2-yl 0 B-0081 H H H H H O H H 3-OMe-4-Cl-pyridin-2-yl 0 B-0082 H H H H H O H H 3-OMe-5-Cl-pyridin-2-yl 0 B-0083 H H H H H O H H 3-OMe-6-Cl-pyridin-2-yl 0 B-0084 H H H H H O H H 3-OMe-4-Me-pyridin-2-yl 0 B-0085 H H H H H O H H 3-OMe-5-Me-pyridin-2-yl 0 B-0086 H H H H H O H H 3-OMe-6-Me-pyridin-2-yl 0 B-0087 H H H H H O H H 3,4-(OMe)2-pyridin-2-yl 0 B-0088 H H H H H O H H 3,5-(OMe)2-pyridin-2-yl 0 B-0089 H H H H H O H H 3,6-(OMe)2-pyridin-2-yl 0 B-0090 H H H H H O H H pyridin-3-yl 0 B-0091 H H H H H O H H 2-F-pyridin-3-yl 0 B-0092 H H H H H O H H 4-F-pyridin-3-yl 0 B-0093 H H H H H O H H 5-F-pyridin-3-yl 0 B-0094 H H H H H O H H 6-F-pyridin-3-yl 0 B-0095 H H H H H O H H 2-Cl-pyridin-3-yl 0 B-0096 H H H H H O H H 4-Cl-pyridin-3-yl 0 B-0097 H H H H H O H H 5-Cl-pyridin-3-yl 0 B-0098 H H H H H O H H 6-Cl-pyridin-3-yl 0 B-0099 H H H H H O H H 2-Me-pyridin-3-yl 0 B-0100 H H H H H O H H 4-Me-pyridin-3-yl 0 B-0101 H H H H H O H H 5-Me-pyridin-3-yl 0 B-0102 H H H H H O H H 6-Me-pyridin-3-yl 0 B-0103 H H H H H O H H 2-CF.sub.3-pyridin-3-yl 0 B-0104 H H H H H O H H 4-CF.sub.3-pyridin-3-yl 0 B-0105 H H H H H O H H 5-CF.sub.3-pyridin-3-yl 0 B-0106 H H H H H O H H 6-CF.sub.3-pyridin-3-yl 0 B-0107 H H H H H O H H 2-OMe-pyridin-3-yl 0 B-0108 H H H H H O H H 4-OMe-pyridin-3-yl 0 B-0109 H H H H H O H H 5-OMe-pyridin-3-yl 0
(280) TABLE-US-00179 TABLE 179 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-0110 H H H H H O H H 6-OMe-pyridin-3-yl 0 B-0111 H H H H H O H H 2,4-F.sub.2-pyridin-3-yl 0 B-0112 H H H H H O H H 2,5-F.sub.2-pyridin-3-yl 0 B-0113 H H H H H O H H 2,6-F.sub.2-pyridin-3-yl 0 B-0114 H H H H H O H H 4,5-F.sub.2-pyridin-3-yl 0 B-0115 H H H H H O H H 4,6-F.sub.2-pyridin-3-yl 0 B-0116 H H H H H O H H 2,4-Cl.sub.2-pyridin-3-yl 0 B-0117 H H H H H O H H 2,5-Cl.sub.2-pyridin-3-yl 0 B-0118 H H H H H O H H 2,6-Cl.sub.2-pyridin-3-yl 0 B-0119 H H H H H O H H 4,5-Cl.sub.2-pyridin-3-yl 0 B-0120 H H H H H O H H 4,6-Cl.sub.2-pyridin-3-yl 0 B-0121 H H H H H O H H 2-F-4-Cl-pyridin-3-yl 0 B-0122 H H H H H O H H 2-F-5-Cl-pyridin-3-yl 0 B-0123 H H H H H O H H 2-F-6-Cl-pyridin-3-yl 0 B-0124 H H H H H O H H 4-F-2-Cl-pyridin-3-yl 0 B-0125 H H H H H O H H 4-F-5-Cl-pyridin-3-yl 0 B-0126 H H H H H O H H 4-F-6-Cl-pyridin-3-yl 0 B-0127 H H H H H O H H 2-F-4-Me-pyridin-3-yl 0 B-0128 H H H H H O H H 2-F-5-Me-pyridin-3-yl 0 B-0129 H H H H H O H H 2-F-6-Me-pyridin-3-yl 0 B-0130 H H H H H O H H 4-F-2-Me-pyridin-3-yl 0 B-0131 H H H H H O H H 4-F-5-Me-pyridin-3-yl 0 B-0132 H H H H H O H H 4-F-6-Me-pyridin-3-yl 0 B-0133 H H H H H O H H 2-F-4-OMe-pyridin-3-yl 0 B-0134 H H H H H O H H 2-F-5-OMe-pyridin-3-yl 0 B-0135 H H H H H O H H 2-F-6-OMe-pyridin-3-yl 0 B-0136 H H H H H O H H 4-F-2-OMe-pyridin-3-yl 0 B-0137 H H H H H O H H 4-F-5-OMe-pyridin-3-yl 0 B-0138 H H H H H O H H 4-F-6-OMe-pyridin-3-yl 0 B-0139 H H H H H O H H 2-Cl-5-F-pyridin-3-yl 0 B-0140 H H H H H O H H 2-Cl-6-F-pyridin-3-yl 0 B-0141 H H H H H O H H 4-Cl-5-F-pyridin-3-yl 0 B-0142 H H H H H O H H 4-Cl-6-F-pyridin-3-yl 0 B-0143 H H H H H O H H 2-Cl-4-Me-pyridin-3-yl 0 B-0144 H H H H H O H H 2-Cl-5-Me-pyridin-3-yl 0 B-0145 H H H H H O H H 2-Cl-6-Me-pyridin-3-yl 0 B-0146 H H H H H O H H 4-Cl-2-Me-pyridin-3-yl 0 B-0147 H H H H H O H H 4-Cl-5-Me-pyridin-3-yl 0 B-0148 H H H H H O H H 4-Cl-6-Me-pyridin-3-yl 0 B-0149 H H H H H O H H 2-Me-5-F-pyridin-3-yl 0 B-0150 H H H H H O H H 2-Me-6-F-pyridin-3-yl 0 B-0151 H H H H H O H H 4-Me-5-F-pyridin-3-yl 0 B-0152 H H H H H O H H 4-Me-6-F-pyridin-3-yl 0 B-0153 H H H H H O H H 2-Me-5-Cl-pyridin-3-yl 0 B-0154 H H H H H O H H 2-Me-6-Cl-pyridin-3-yl 0 B-0155 H H H H H O H H 4-Me-5-Cl-pyridin-3-yl 0 B-0156 H H H H H O H H 4-Me-6-Cl-pyridin-3-yl 0 B-0157 H H H H H O H H 2,4-(Me).sub.2-pyridin-3-yl 0 B-0158 H H H H H O H H 2,5-(Me).sub.2-pyridin-3-yl 0 B-0159 H H H H H O H H 2,6-(Me).sub.2-pyridin-3-yl 0 B-0160 H H H H H O H H 4,5-(Me).sub.2-pyridin-3-yl 0 B-0161 H H H H H O H H 4,6-(Me).sub.2-pyridin-3-yl 0 B-0162 H H H H H O H H 2-Me-4-OMe-pyridin-3-yl 0 B-0163 H H H H H O H H 2-Me-5-OMe-pyridin-3-yl 0 B-0164 H H H H H O H H 2-Me-6-OMe-pyridin-3-yl 0 B-0165 H H H H H O H H 4-Me-2-OMe-pyridin-3-yl 0 B-0166 H H H H H O H H 4-Me-5-OMe-pyridin-3-yl 0
(281) TABLE-US-00180 TABLE 180 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-0167 H H H H H O H H 4-Me-6-OMe-pyridin-3-yl 0 B-0168 H H H H H O H H 2-CF.sub.3-4-F-pyridin-3-yl 0 B-0169 H H H H H O H H 2-CF.sub.3-5-F-pyridin-3-yl 0 B-0170 H H H H H O H H 2-CF.sub.3-6-F-pyridin-3-yl 0 B-0171 H H H H H O H H 4-CF.sub.3-2-F-pyridin-3-yl 0 B-0172 H H H H H O H H 4-CF.sub.3-5-F-pyridin-3-yl 0 B-0173 H H H H H O H H 4-CF.sub.3-6-F-pyridin-3-yl 0 B-0174 H H H H H O H H 2-CF.sub.3-4-Me-pyridin-3-yl 0 B-0175 H H H H H O H H 2-CF.sub.3-5-Me-pyridin-3-yl 0 B-0176 H H H H H O H H 2-CF.sub.3-6-Me-pyridin-3-yl 0 B-0177 H H H H H O H H 4-CF.sub.3-2-Me-pyridin-3-yl 0 B-0178 H H H H H O H H 4-CF.sub.3-5-Me-pyridin-3-yl 0 B-0179 H H H H H O H H 4-CF.sub.3-6-Me-pyridin-3-yl 0 B-0180 H H H H H O H H 2-OMe-5-F-pyridin-3-yl 0 B-0181 H H H H H O H H 2-OMe-6-F-pyridin-3-yl 0 B-0182 H H H H H O H H 4-OMe-5-F-pyridin-3-yl 0 B-0183 H H H H H O H H 4-OMe-6-F-pyridin-3-yl 0 B-0184 H H H H H O H H 2-OMe-4-Cl-pyridin-3-yl 0 B-0185 H H H H H O H H 2-OMe-5-Cl-pyridin-3-yl 0 B-0186 H H H H H O H H 2-OMe-6-Cl-pyridin-3-yl 0 B-0187 H H H H H O H H 4-OMe-2-Cl-pyridin-3-yl 0 B-0188 H H H H H O H H 4-OMe-5-Cl-pyridin-3-yl 0 B-0189 H H H H H O H H 4-OMe-6-Cl-pyridin-3-yl 0 B-0190 H H H H H O H H 2-OMe-5-Me-pyridin-3-yl 0 B-0191 H H H H H O H H 2-OMe-6-Me-pyridin-3-yl 0 B-0192 H H H H H O H H 4-OMe-5-Me-pyridin-3-yl 0 B-0193 H H H H H O H H 4-OMe-6-Me-pyridin-3-yl 0 B-0194 H H H H H O H H 2,4-(OMe).sub.2-pyridin-3-yl 0 B-0195 H H H H H O H H 2,5-(OMe).sub.2-pyridin-3-yl 0 B-0196 H H H H H O H H 2,6-(OMe).sub.2-pyridin-3-yl 0 B-0197 H H H H H O H H 4,5-(OMe).sub.2-pyridin-3-yl 0 B-0198 H H H H H O H H 4,6-(OMe).sub.2-pyridin-3-yl 0 B-0199 H H H H H O H H pyridin-4-yl 0 B-0200 H H H H H O H H 2-F-pyridin-4-yl 0 B-0201 H H H H H O H H 3-F-pyridin-4-yl 0 B-0202 H H H H H O H H 2-Cl-pyridin-4-yl 0 B-0203 H H H H H O H H 3-Cl-pyridin-4-yl 0 B-0204 H H H H H O H H 2-Me-pyridin-4-yl 0 B-0205 H H H H H O H H 3-Me-pyridin-4-yl 0 B-0206 H H H H H O H H 2-CF.sub.3-pyridin-4-yl 0 B-0207 H H H H H O H H 3-CF.sub.3-pyridin-4-yl 0 B-0208 H H H H H O H H 2-OMe-pyridin-4-yl 0 B-0209 H H H H H O H H 3-OMe-pyridin-4-yl 0 B-0210 H H H H H O H H 2,3-F.sub.2-pyridin-4-yl 0 B-0211 H H H H H O H H 2,5-F.sub.2-pyridin-4-yl 0 B-0212 H H H H H O H H 2,6-F.sub.2-pyridin-4-yl 0 B-0213 H H H H H O H H 3,5-F.sub.2-pyridin-4-y 0 B-0214 H H H H H O H H 2,3-Cl.sub.2-pyridin-4-yl 0 B-0215 H H H H H O H H 2,5-Cl.sub.2-pyridin-4-yl 0 B-0216 H H H H H O H H 2,6-Cl.sub.2-pyridin-4-yl 0 B-0217 H H H H H O H H 3,5-Cl.sub.2-pyridin-4-yl 0 B-0218 H H H H H O H H 3-F-2-Cl-pyridin-4-yl 0 B-0219 H H H H H O H H 3-F-5-Cl-pyridin-4-yl 0 B-0220 H H H H H O H H 3-F-6-Cl-pyridin-4-yl 0 B-0221 H H H H H O H H 3-F-2-Me-pyridin-4-yl 0 B-0222 H H H H H O H H 3-F-5-Me-pyridin-4-yl 0 B-0223 H H H H H O H H 3-F-6-Me-pyridin-4-yl 0
(282) TABLE-US-00181 TABLE 181 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-0224 H H H H H O H H 3-F-2-OMe-pyridin-4-yl 0 B-0225 H H H H H O H H 3-F-5-OMe-pyridin-4-yl 0 B-0226 H H H H H O H H 3-F-6-OMe-pyridin-4-yl 0 B-0227 H H H H H O H H 3-Cl-2-F-pyridin-4-yl 0 B-0228 H H H H H O H H 3-Cl-6-F-pyridin-4-yl 0 B-0229 H H H H H O H H 3-Cl-2-Me-pyridin-4-yl 0 B-0230 H H H H H O H H 3-Cl-5-Me-pyridin-4-yl 0 B-0231 H H H H H O H H 3-Cl-6-Me-pyridin-4-yl 0 B-0232 H H H H H O H H 3-Me-2-F-pyridin-4-yl 0 B-0233 H H H H H O H H 3-Me-6-F-pyridin-4-yl 0 B-0234 H H H H H O H H 3-Me-2-Cl-pyridin-4-y 0 B-0235 H H H H H O H H 3-Me-6-Cl-pyridin-4-y 0 B-0236 H H H H H O H H 2,3-(Me).sub.2-pyridin-4-yl 0 B-0237 H H H H H O H H 3,5-(Me).sub.2-pyridin-4-yl 0 B-0238 H H H H H O H H 3,6-(Me).sub.2-pyridin-4-yl 0 B-0239 H H H H H O H H 3-Me-2-OMe-pyridin-4-yl 0 B-0240 H H H H H O H H 3-Me-5-OMe-pyridin-4-yl 0 B-0241 H H H H H O H H 3-Me-6-OMe-pyridin-4-yl 0 B-0242 H H H H H O H H 3-CF.sub.3-2-F-pyridin-4-yl 0 B-0243 H H H H H O H H 3-CF.sub.3-5-F-pyridin-4-yl 0 B-0244 H H H H H O H H 3-CF.sub.3-6-F-pyridin-4-yl 0 B-0245 H H H H H O H H 3-CF.sub.3-2-Me-pyridin-4-yl 0 B-0246 H H H H H O H H 3-CF.sub.3-5-Me-pyridin-4-yl 0 B-0247 H H H H H O H H 3-CF.sub.3-6-Me-pyridin-4-yl 0 B-0248 H H H H H O H H 3-OMe-2-F-pyridin-4-yl 0 B-0249 H H H H H O H H 3-OMe-6-F-pyridin-4-yl 0 B-0250 H H H H H O H H 3-OMe-2-Cl-pyridin-4-yl 0 B-0251 H H H H H O H H 3-OMe-5-Cl-pyridin-4-yl 0 B-0252 H H H H H O H H 3-OMe-6-Cl-pyridin-4-yl 0 B-0253 H H H H H O H H 3-OMe-2-Me-pyridin-4-yl 0 B-0254 H H H H H O H H 3-OMe-6-Me-pyridin-4-yl 0 B-0255 H H H H H O H H 2,3-(OMe).sub.2-pyridin-4-yl 0 B-0256 H H H H H O H H 3,5-(OMe).sub.2-pyridin-4-yl 0 B-0257 H H H H H O H H 3,6-(OMe).sub.2-pyridin-4-yl 0 B-0258 H H H H H O H H pyrimidin-2-yl 0 B-0259 H H H H H O H H pyrimidin-4-yl 0 B-0260 H H H H H O H H 5-F-pyrmidin-4-yl 0 B-0261 H H H H H O H H 5-Me-pyrimidin-4-yl 0 B-0262 H H H H H O H H 5-CF.sub.3-pyrimidin-4-yl 0 B-0263 H H H H H O H H 5-OMe-pyrimidin-4-yl 0 B-0264 H H H H H O H H pyrimidin-5-yl 0 B-0265 H H H H H O H H 4-F-pyrimidin-5-y 0 B-0266 H H H H H O H H 4-Cl-pyrimidin-5-yl 0 B-0267 H H H H H O H H 4-Me-pyrimidin-5-yl 0 B-0268 H H H H H O H H 4-CF.sub.3-pyrimidin-5-yl 0 B-0269 H H H H H O H H 4-OMe-pyrimidin-5-yl 0 B-0270 H H H H H O H H pyridazin-3-yl 0 B-0271 H H H H H O H H 4-F-pyridazin-3-yl 0 B-0272 H H H H H O H H 4-Cl-pyridazin-3-yl 0 B-0273 H H H H H O H H 4-Me-pyridazin-3-yl 0 B-0274 H H H H H O H H 4-CF.sub.3-pyridazin-3-yl 0 B-0275 H H H H H O H H 4-OMe-pyridazin-3-yl 0 B-0276 H H H H H O H H pyridazin-4-yl 0 B-0277 H H H H H O H H 3-F-pyridazin-4-yl 0 B-0278 H H H H H O H H 3-Cl-pyridazin-4-yl 0 B-0279 H H H H H O H H 3-Me-pyridazin-4-yl 0 B-0280 H H H H H O H H 3-CF.sub.3-pyridazin-4-yl 0
(283) TABLE-US-00182 TABLE 182 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-0281 H H H H H O H H 3-OMe-pyridazin-4-yl 0 B-0282 H H H H H O H H 5-F-pyridazin-4-yl 0 B-0283 H H H H H O H H 5-Cl-pyridazin-4-yl 0 B-0284 H H H H H O H H 5-Me-pyridazin-4-yl 0 B-0285 H H H H H O H H 5-CF.sub.3-pyridazin-4-yl 0 B-0286 H H H H H O H H 5-OMe-pyridazin-4-yl 0 B-0287 H H H H H O H H thiophen-2-yl 0 B-0288 H H H H H O H H 3-F-thiophen-2-yl 0 B-0289 H H H H H O H H 3-Cl-thiophen-2-yl 0 B-0290 H H H H H O H H 3-Me-thiophen-2-yl 0 B-0291 H H H H H O H H 3-CF.sub.3-thiophen-2-yl 0 B-0292 H H H H H O H H 3-OMe-thiophen-2-yl 0 B-0293 H H H H H O H H thiophen-3-yl 0 B-0294 H H H H H O H H 2-F-thiophen-3-yl 0 B-0295 H H H H H O H H 2-Cl-thiophen-3-yl 0 B-0296 H H H H H O H H 2-Me-thiophen-3-yl 0 B-0297 H H H H H O H H 2-CF.sub.3-thiophen-3-yl 0 B-0298 H H H H H O H H 2-OMe-thiophen-3-yl 0 B-0299 H H H H H O H H 4-F-thiophen-3-yl 0 B-0300 H H H H H O H H 4-Cl-thiophen-3-yl 0 B-0301 H H H H H O H H 4-Me-thiophen-3-yl 0 B-0302 H H H H H O H H 4-CF.sub.3-thiophen-3-yl 0 B-0303 H H H H H O H H 4-OMe-thiophen-3-yl 0 B-0304 H H H H H O H H thiazol-2-yl 0 B-0305 H H H H H O H H thiazol-4-yl 0 B-0306 H H H H H O H H 5-F-thiazol-4-yl 0 B-0307 H H H H H O H H 5-Me-thiazol-4-yl 0 B-0308 H H H H H O H H 5-CF.sub.3-thiazol-4-yl 0 B-0309 H H H H H O H H 5-OMe-thiazol-4-yl 0 B-0310 H H H H H O H H thiazol-5-yl 0 B-0311 H H H H H O H H 4-F-thiazol-5-yl 0 B-0312 H H H H H O H H 4-Me-thiazol-5-yl 0 B-0313 H H H H H O H H 4-CF.sub.3-thiazol-5-yl 0 B-0314 H H H H H O H H 4-OMe-thiazol-5-yl 0 B-0315 H H H H H O H H 1H-pyrrol-1-yl 0 B-0316 H H H H H O H H 2-F-1H-pyrrol-1-yl 0 B-0317 H H H H H O H H 2-Me-1H-pyrrol-1-yl 0 B-0318 H H H H H O H H 2-CF.sub.3-1H-pyrrol-1-yl 0 B-0319 H H H H H O H H 2-OMe-1H-pyrrol-1-yl 0 B-0320 H H H H H O H H 1H-pyrrol-2-yl 0 B-0321 H H H H H O H H 1-Me-1H-pyrrol-2-yl 0 B-0322 H H H H H O H H 3-F-1H-pyrrol-2-yl 0 B-0323 H H H H H O H H 3-Me-1H-pyrrol-2-yl 0 B-0324 H H H H H O H H 3-CF.sub.3-1H-pyrrol-2-yl 0 B-0325 H H H H H O H H 3-OMe-1H-pyrrol-2-yl 0 B-0326 H H H H H O H H 1-Me-3-F-1H-pyrrol-2-yl 0 B-0327 H H H H H O H H 1,3-(Me).sub.2-1H-pyrrol-2-yl 0 B-0328 H H H H H O H H 1-Me-3-CF.sub.3-1H-pyrrol-2-yl 0 B-0329 H H H H H O H H 1-Me-3-OMe-1H-pyrrol-2-yl 0 B-0330 H H H H H O H H 1H-pyrrol-3-yl 0 B-0331 H H H H H O H H 1-Me-1H-pyrrol-3-yl 0 B-0332 H H H H H O H H 2-F-1H-pyrrol-3-yl 0 B-0333 H H H H H O H H 2-Me-1H-pyrrol-3-yl 0 B-0334 H H H H H O H H 2-CF.sub.3-1H-pyrrol-1-3-yl 0 B-0335 H H H H H O H H 2-OMe-1H-pyrrol-1-3-yl 0 B-0336 H H H H H O H H 1-Me-2-F-1H-pyrrol-3-yl 0 B-0337 H H H H H O H H 1,2-(Me).sub.2-1H-pyrrol-3-yl 0
(284) TABLE-US-00183 TABLE 183 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-0338 H H H H H O H H 1-Me-2-CF.sub.3-1H-pyrrol-3-yl 0 B-0339 H H H H H O H H 1-Me-2-OMe-1H-pyrrol-3-yl 0 B-0340 H H H H H O H H 4-F-1H-pyrrol-3-yl 0 B-0341 H H H H H O H H 4-Me-1H-pyrrol-3-yl 0 B-0342 H H H H H O H H 4-CF.sub.3-1H-pyrrol-3-yl 0 B-0343 H H H H H O H H 4-OMe-1H-pyrrol-3-yl 0 B-0344 H H H H H O H H 1-Me-4-F-1H-pyrrol-3-yl 0 B-0345 H H H H H O H H 1,4-(Me).sub.2-1H-pyrrol-3-yl 0 B-0346 H H H H H O H H 1-Me-4-CF.sub.3-1H-pyrrol-3-yl 0 B-0347 H H H H H O H H 1-Me-4-OMe-1H-pyrrol-3-yl 0 B-0348 H H H H H O H H 1H-pyrazol-1-yl 0 B-0349 H H H H H O H H 5F-1H-pyrazol-1-yl 0 B-0350 H H H H H O H H 5-Cl-1H-pyrazol-1-yl 0 B-0351 H H H H H O H H 5-Me-1H-pyrazol-1-yl 0 B-0352 H H H H H O H H 5-CF.sub.3-1H-pyrazol-1-yl 0 B-0353 H H H H H O H H 5-OMe-1H-pyrazol-1-yl 0 B-0354 H H H H H O H H 1H-pyrazol-3-yl 0 B-0355 H H H H H O H H 1-Me-1H-pyrazol-3-yl 0 B-0356 H H H H H O H H 4-1H-pyrazol-3-yl 0 B-0357 H H H H H O H H 4-Cl-1H-pyrazol-3-yl 0 B-0358 H H H H H O H H 4-Me-1H-pyrazol-3-yl 0 B-0359 H H H H H O H H 4-CF.sub.3-1H-pyrazol-3-yl 0 B-0360 H H H H H O H H 4-OMe-1H-pyrazol-3-yl 0 B-0361 H H H H H O H H 1-Me-4F-1H-pyrazol-3-yl 0 B-0362 H H H H H O H H 1-Me-4-Cl-1H-pyrazol-3-yl 0 B-0363 H H H H H O H H 1,4-(Me).sub.2-1H-pyrazol-3-yl 0 B-0364 H H H H H O H H 1-Me-4-CF.sub.3-1H-pyrazol-3-yl 0 B-0365 H H H H H O H H 1-Me-4-OMe-1H-pyrazol-3-yl 0 B-0366 H H H H H O H H 1H-pyrazol-4-yl 0 B-0367 H H H H H O H H 1-Me-1H-pyrazol-4-yl 0 B-0368 H H H H H O H H 3-F-1H-pyrazol-4-yl 0 B-0369 H H H H H O H H 3-Cl-1H-pyrazol-4-yl 0 B-0370 H H H H H O H H 3-Me-1H-pyrazol-4-yl 0 B-0371 H H H H H O H H 3-CF.sub.3-1H-pyrazol-4-yl 0 B-0372 H H H H H O H H 3-OMe-1H-pyrazol-4-yl 0 B-0373 H H H H H O H H 1-Me-3-F-1H-pyrazol-4-yl 0 B-0374 H H H H H O H H 1-Me-3-Cl-1H-pyrazol-4-yl 0 B-0375 H H H H H O H H 1,3-(Me).sub.2-1H-pyrazol-4-yl 0 B-0376 H H H H H O H H 1-Me-3-CF.sub.3-1H-pyrazol-4-yl 0 B-0377 H H H H H O H H 1-Me-3-OMe-1H-pyrazol-4-yl 0 B-0378 H H H H H O H H 5-F-1H-pyrazol-4-yl 0 B-0379 H H H H H O H H 5-Cl-1H-pyrazol-4-yl 0 B-0380 H H H H H O H H 5-Me-1H-pyrazol-4-yl 0 B-0381 H H H H H O H H 5-CF.sub.3-1H-pyrazol-4-yl 0 B-0382 H H H H H O H H 5-OMe-1H-pyrazol-4-yl 0 B-0383 H H H H H O H H 1-Me-5-F-1H-pyrazol-4-yl 0 B-0384 H H H H H O H H 1-Me-5-Cl-1H-pyrazol-4-yl 0 B-0385 H H H H H O H H 1,5-(Me).sub.2-1H-pyrazol-4-yl 0 B-0386 H H H H H O H H 1-Me-5-CF.sub.3-1H-pyrazol-4-yl 0 B-0387 H H H H H O H H 1-Me-5-OMe-1H-pyrazol-4-yl 0 B-0388 H H H H H O H H 1H-pyrazol-5-yl 0 B-0389 H H H H H O H H 1-Me-1H-pyrazol-5-yl 0 B-0390 H H H H H O H H 4-F-1H-pyrazol-5-yl 0 B-0391 H H H H H O H H 4-Cl-1H-pyrazol-5-yl 0 B-0392 H H H H H O H H 4-Me-1H-pyrazol-5-yl 0 B-0393 H H H H H O H H 4-CF.sub.3-1H-pyrazol-5-yl 0 B-0394 H H H H H O H H 4-OMe-1H-pyrazol-5-yl 0
(285) TABLE-US-00184 TABLE 184 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-0395 H H H H H O H H 1-Me-4-F-1H-pyrazol-5-yl 0 B-0396 H H H H H O H H 1-Me-4-Cl-1H-pyrazol-5-yl 0 B-0397 H H H H H O H H 1,4-(Me).sub.2-1H-pyrazol-5-yl 0 B-0398 H H H H H O H H 1-Me-4-CF.sub.3-1H-pyrazol-5-yl 0 B-0399 H H H H H O H H 1-Me-4-OMe-1H-pyrazol-5-yl 0 B-0400 H H H H H O H H furan-2-yl 0 B-0401 H H H H H O H H 3-F-furan-2-yl 0 B-0402 H H H H H O H H 3-Me-furan-2-yl 0 B-0403 H H H H H O H H 3-CF.sub.3-furan-2-yl 0 B-0404 H H H H H O H H 3-OMe-furan-2-yl 0 B-0405 H H H H H O H H furan-3-yl 0 B-0406 H H H H H O H H 2-F-furan-3-yl 0 B-0407 H H H H H O H H 2-Me-furan-3-yl 0 B-0408 H H H H H O H H 2-CF.sub.3-furan-3-yl 0 B-0409 H H H H H O H H 2-OMe-furan-3-yl 0 B-0410 H H H H H O H H 4-F-furan-3-yl 0 B-0411 H H H H H O H H 4-Me-furan-3-yl 0 B-0412 H H H H H O H H 4-CF.sub.3-furan-3-yl 0 B-0413 H H H H H O H H 4-OMe-furan-3-yl 0 B-0414 H H H H H O H H isoxazol-3-yl 0 B-0415 H H H H H O H H 4-F-isoxazol-3-yl 0 B-0416 H H H H H O H H 4-Me-isoxazol-3-yl 0 B-0417 H H H H H O H H 4-CF.sub.3-isoxazol-3-yl 0 B-0418 H H H H H O H H 4-OMe-isoxazol-3-yl 0 B-0419 H H H H H O H H isoxazol-4-yl 0 B-0420 H H H H H O H H 5-F-isoxazol-4-yl 0 B-0421 H H H H H O H H 5-Me-isoxazol-4-yl 0 B-0422 H H H H H O H H 5-CF.sub.3-isoxazol-4-y 0 B-0423 H H H H H O H H 5-OMe-isoxazol-4-yl 0 B-0424 H H H H H O H H isoxazol-5-yl 0 B-0425 H H H H H O H H 4-F-isoxazol-5-yl 0 B-0426 H H H H H O H H 4-Me-isoxazol-15-yl 0 B-0427 H H H H H O H H 4-CF.sub.3-isoxazol-5-yl 0 B-0428 H H H H H O H H 4-OMe-isoxazol-5-yl 0 B-0429 H H H H H O H H 1H-1,2,3-triazol-1-yl 0 B-0430 H H H H H O H H 5-F-1H-1,2,3-triazol-1-yl 0 B-0431 H H H H H O H H 5-Me-1H-1,2,3-triazol-1-yl 0 B-0432 H H H H H O H H 5-CF.sub.3-1H-1,2,3-triazol-1-yl 0 B-0433 H H H H H O H H 5-OMe-1H-1,2,3-triazol-1-yl 0 B-0434 H H H H H O H H 1H-1,2,3-triazol-4-yl 0 B-0435 H H H H H O H H 5-F-1H-1,2,3-triazol-4-yl 0 B-0436 H H H H H O H H 5-Me-1H-1,2,3-triazol-4-yl 0 B-0437 H H H H H O H H 5-CF.sub.3-1H-1,2,3-triazol-4-yl 0 B-0438 H H H H H O H H 5-OMe-1H-1,2,3-triazol-4-yl 0 B-0439 H H H H H O H H 1H-1,2,3-triazol-5-yl 0 B-0440 H H H H H O H H 4-F-1H-1,2,3-triazol-5-yl 0 B-0441 H H H H H O H H 4-Me-1H-1,2,3-triazol-5-yl 0 B-0442 H H H H H O H H 4-CF.sub.3-1H-1,2,3-triazol-5-yl 0 B-0443 H H H H H O H H 4-OMe-1H-1,2,3-triazol-5-yl 0 B-0444 H H H H H O H H 1H-1,2,4-triazol-1-yl 0 B-0445 H H H H H O H H 5-Me-1H-1,2,4-triazol-1-yl 0 B-0446 H H H H H O H H 5-F-1H-1,2,4-triazol-1-yl 0 B-0447 H H H H H O H H 5-CF.sub.3-1H-1,2,4-triazol-1-yl 0 B-0448 H H H H H O H H 5-OMe-1H-1,2,4-triazol-1-yl 0 B-0449 H H H H H O H H 1H-1,2,4-triazol-3-yl 0 B-0450 H H H H H O H H 1-Me-1H-1,2,4-triazol-3-yl 0 B-0451 H H H H H O H H 1H-1,2,4-triazol-5-yl 0
(286) TABLE-US-00185 TABLE 185 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-0452 H H H H H O H H 1-Me-1H-1,2,4-triazol-5-yl 0 B-0453 H H H H H O H H 3,5-(Me).sub.2-isoxazol-4-yl 0 B-0454 H H H H H O H H 3,5-(Et).sub.2-isoxazol-4-yl 0 B-0455 H H H H H O H H 1,3,5-(Me).sub.3-1H-pyrazol-4-yl 0 B-0456 H H H H H O H H quinolin-4-yl 0 B-0457 H H H H H O H H isoquinolin-4-yl 0 B-0458 H H H H H O H H 3,6-(OMe).sub.2-pyridazin-4-yl 0 B-0459 H H H H H O H H 2,4-(OMe).sub.2-pyrimidin-5-yl 0
(287) TABLE-US-00186 TABLE 186
(288) TABLE-US-00187 TABLE 187 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-5053 H H H H H O H H 3-F-6-OMe-pyridin-2-yl 1 B-5054 H H H H H O H H 3-Cl-4-F-pyridin-2-yl 1 B-5055 H H H H H O H H 3-Cl-5-F-pyridin-2-yl 1 B-5056 H H H H H O H H 3-Cl-6-F-pyridin-2-yl 1 B-5057 H H H H H O H H 3-Cl-4-Me-pyridin-2-yl 1 B-5058 H H H H H O H H 3-Cl-5-Me-pyridin-2-yl 1 B-5059 H H H H H O H H 3-Cl-6-Me-pyridin-2-yl 1 B-5060 H H H H H O H H 3-Me-4-F-pyridin-2-yl 1 B-5061 H H H H H O H H 3-Me-5-F-pyridin-2-yl 1 B-5062 H H H H H O H H 3-Me-6-F-pyridin-2-yl 1 B-5063 H H H H H O H H 3-Me-4-Cl-pyridin-2-yl 1 B-5064 H H H H H O H H 3-Me-5-Cl-pyridin-2-yl 1 B-5065 H H H H H O H H 3-Me-6-Cl-pyridin-2-yl 1 B-5066 H H H H H O H H 3,4-(Me).sub.2-pyridin-2-yl 1 B-5067 H H H H H O H H 3,5-(Me).sub.2-pyridin-2-y 1 B-5068 H H H H H O H H 3,6-(Me).sub.2-pyridin-2-yl 1 B-5069 H H H H H O H H 3-Me-4-OMe-pyridin-2-yl 1 B-5070 H H H H H O H H 3-Me-5-OMe-pyridin-2-y 1 B-5071 H H H H H O H H 3-Me-6-OMe-pyridin-2-yl 1 B-5072 H H H H H O H H 3-CF.sub.3-4-F-pyridin-2-yl 1 B-5073 H H H H H O H H 3-CF.sub.3-5-F-pyridin-2-yl 1 B-5074 H H H H H O H H 3-CF.sub.3-6-F-pyridin-2-yl 1 B-5075 H H H H H O H H 3-CF.sub.3-4-Me-pyridin-2-yl 1 B-5076 H H H H H O H H 3-CF.sub.3-5-Me-pyridin-2-yl 1 B-5077 H H H H H O H H 3-CF.sub.3-6-Me-pyridin-2-yl 1 B-5078 H H H H H O H H 3-OMe-4-F-pyridin-2-yl 1 B-5079 H H H H H O H H 3-OMe-5-F-pyridin-2-yl 1 B-5080 H H H H H O H H 3-OMe-6-F-pyridin-2-yl 1 B-5081 H H H H H O H H 3-OMe-4-Cl-pyridin-2-yl 1 B-5082 H H H H H O H H 3-OMe-5-Cl-pyridin-2-yl 1 B-5083 H H H H H O H H 3-OMe-6-Cl-pyridin-2-yl 1 B-5084 H H H H H O H H 3-OMe-4-Me-pyridin-2-yl 1 B-5085 H H H H H O H H 3-OMe-5-Me-pyridin-2-yl 1 B-5086 H H H H H O H H 3-OMe-6-Me-pyridin-2-yl 1 B-5087 H H H H H O H H 3,4-(OMe).sub.2-pyridin-2-yl 1 B-5088 H H H H H O H H 3,5-(OMe).sub.2-pyridin-2-yl 1 B-5089 H H H H H O H H 3,6-(OMe).sub.2-pyridin-2-yl 1 B-5090 H H H H H O H H pyridin-3-yl 1 B-5091 H H H H H O H H 2-F-pyridin-3-yl 1 B-5092 H H H H H O H H 4-F-pyridin-3-yl 1 B-5093 H H H H H O H H 5-F-pyridin-3-yl 1 B-5094 H H H H H O H H 6-F-pyridin-3-yl 1 B-5095 H H H H H O H H 2-Cl-pyridin-3-yl 1 B-5096 H H H H H O H H 4-Cl-pyridin-3-yl 1 B-5097 H H H H H O H H 5-Cl-pyridin-3-yl 1 B-5098 H H H H H O H H 6-Cl-pyridin-3-yl 1 B-5099 H H H H H O H H 2-Me-pyridin-3-yl 1 B-5100 H H H H H O H H 4-Me-pyridin-3-yl 1 B-5101 H H H H H O H H 5-Me-pyridin-3-yl 1 B-5102 H H H H H O H H 6-Me-pyridin-3-yl 1 B-5103 H H H H H O H H 2-CF.sub.3-pyridin-3-yl 1 B-5104 H H H H H O H H 4-CF.sub.3-pyridin-3-yl 1 B-5105 H H H H H O H H 5-CF.sub.3-pyridin-3-yl 1 B-5106 H H H H H O H H 6-CF.sub.3-pyridin-3-yl 1 B-5107 H H H H H O H H 2-OMe-pyridin-3-yl 1 B-5108 H H H H H O H H 4-OMe-pyridin-3-yl 1 B-5109 H H H H H O H H 5-OMe-pyridin-3-yl 1
(289) TABLE-US-00188 TABLE 188 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-5110 H H H H H O H H 6-OMe-pyridin-3-yl 1 B-5111 H H H H H O H H 2,4-F.sub.2-pyridin-3-yl 1 B-5112 H H H H H O H H 2,5-F.sub.2-pyridin-3-yl 1 B-5113 H H H H H O H H 2,6-F.sub.2-pyridin-3-yl 1 B-5114 H H H H H O H H 4,5-F.sub.2-pyridin-3-yl 1 B-5115 H H H H H O H H 4,6-F.sub.2-pyridin-3-yl 1 B-5116 H H H H H O H H 2,4-Cl.sub.2-pyridin-3-yl 1 B-5117 H H H H H O H H 2,5-Cl.sub.2-pyridin-3-yl 1 B-5118 H H H H H O H H 2,6-Cl.sub.2-pyridin-3-yl 1 B-5119 H H H H H O H H 4,5-Cl.sub.2-pyridin-3-yl 1 B-5120 H H H H H O H H 4,6-Cl.sub.2-pyridin-3-yl 1 B-5121 H H H H H O H H 2-F-4-Cl-pyridin-3-yl 1 B-5122 H H H H H O H H 2-F-5-Cl-pyridin-3-yl 1 B-5123 H H H H H O H H 2-F-6-Cl-pyridin-3-yl 1 B-5124 H H H H H O H H 4-F-2-Cl-pyridin-3-yl 1 B-5125 H H H H H O H H 4-F-5-Cl-pyridin-3-yl 1 B-5126 H H H H H O H H 4-F-6-Cl-pyridin-3-yl 1 B-5127 H H H H H O H H 2-F-4-Me-pyridin-3-yl 1 B-5128 H H H H H O H H 2-F-5-Me-pyridin-3-yl 1 B-5129 H H H H H O H H 2-F-6-Me-pyridin-3-yl 1 B-5130 H H H H H O H H 4-F-2-Me-pyridin-3-yl 1 B-5131 H H H H H O H H 4-F-5-Me-pyridin-3-yl 1 B-5132 H H H H H O H H 4-F-6-Me-pyridin-3-yl 1 B-5133 H H H H H O H H 2-4-OMe-pyridin-3-yl 1 B-5134 H H H H H O H H 2-F-5-OMe-pyridin-3-yl 1 B-5135 H H H H H O H H 2-F-6-OMe-pyridin-3-yl 1 B-5136 H H H H H O H H 4-F-2-OMe-pyridin-3-yl 1 B-5137 H H H H H O H H 4-F-5-OMe-pyridin-3-yl 1 B-5138 H H H H H O H H 4-F-6-OMe-pyridin-3-yl 1 B-5139 H H H H H O H H 2-Cl-5-F-pyridin-3-yl 1 B-5140 H H H H H O H H 2-Cl-6-F-pyridin-3-yl 1 B-5141 H H H H H O H H 4-Cl-5-F-pyridin-3-yl 1 B-5142 H H H H H O H H 4-Cl-6-F-pyridin-3-yl 1 B-5143 H H H H H O H H 2-Cl-4-Me-pyridin-3-yl 1 B-5144 H H H H H O H H 2-Cl-5-Me-pyridin-3-yl 1 B-5145 H H H H H O H H 2-Cl-6-Me-pyridin-3-yl 1 B-5146 H H H H H O H H 4-Cl-2-Me-pyridin-3-yl 1 B-5147 H H H H H O H H 4-Cl-5-Me-pyridin-3-yl 1 B-5148 H H H H H O H H 4-Cl-6-Me-pyridin-3-yl 1 B-5149 H H H H H O H H 2-Me-5-F-pyridin-3-yl 1 B-5150 H H H H H O H H 2-Me-6-F-pyridin-3-yl 1 B-5151 H H H H H O H H 4-Me-5-F-pyridin-3-yl 1 B-5152 H H H H H O H H 4-Me-6-F-pyridin-3-yl 1 B-5153 H H H H H O H H 2-Me-5-Cl-pyridin-3-yl 1 B-5154 H H H H H O H H 2-Me-6-Cl-pyridin-3-yl 1 B-5155 H H H H H O H H 4-Me-5-Cl-pyridin-3-yl 1 B-5156 H H H H H O H H 4-Me-6-Cl-pyridin-3-yl 1 B-5157 H H H H H O H H 2,4-(Me).sub.2-pyridin-3-yl 1 B-5158 H H H H H O H H 2,5-(Me).sub.2-pyridin-3-yl 1 B-5159 H H H H H O H H 2,6-(Me).sub.2-pyridin-3-yl 1 B-5160 H H H H H O H H 4,5-(Me).sub.2-pyridin-3-yl 1 B-5161 H H H H H O H H 4,6-(Me).sub.2-pyridin-3-yl 1 B-5162 H H H H H O H H 2-Me-4-OMe-pyridin-3-yl 1 B-5163 H H H H H O H H 2-Me-5-OMe-pyridin-3-yl 1 B-5164 H H H H H O H H 2-Me-6-OMe-pyridin-3-yl 1 B-5165 H H H H H O H H 4-Me-2-OMe-pyridin-3-yl 1 B-5166 H H H H H O H H 4-Me-5-OMe-pyridin-3-yl 1
(290) TABLE-US-00189 TABLE 189 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-5167 H H H H H O H H 4-Me-6-OMe-pyridin-3-yl 1 B-5168 H H H H H O H H 2-CF.sub.3-4-F-pyridin-3-yl 1 B-5169 H H H H H O H H 2-CF.sub.3-5-F-pyridin-3-yl 1 B-5170 H H H H H O H H 2-CF.sub.3-6-F-pyridin-3-yl 1 B-5171 H H H H H O H H 4-CF.sub.3-2-F-pyridin-3-yl 1 B-5172 H H H H H O H H 4-CF.sub.3-5-F-pyridin-3-yl 1 B-5173 H H H H H O H H 4-CF.sub.3-6-F-pyridin-3-yl 1 B-5174 H H H H H O H H 2-CF.sub.3-4-Me-pyridin-3-yl 1 B-5175 H H H H H O H H 2-CF.sub.3-5-Me-pyridin-3-yl 1 B-5176 H H H H H O H H 2-CF.sub.3-6-Me-pyridin-3-yl 1 B-5177 H H H H H O H H 4-CF.sub.3-2-Me-pyridin-3-yl 1 B-5178 H H H H H O H H 4-CF.sub.3-5-Me-pyridin-3-yl 1 B-5179 H H H H H O H H 4-CF.sub.3-6-Me-pyridin-3-yl 1 B-5180 H H H H H O H H 2-OMe-5-F-pyridin-3-yl 1 B-5181 H H H H H O H H 2-OMe-6-F-pyridin-3-yl 1 B-5182 H H H H H O H H 4-OMe-5-F-pyridin-3-yl 1 B-5183 H H H H H O H H 4-OMe-6-F-pyridin-3-yl 1 B-5184 H H H H H O H H 2-OMe-4-Cl-pyridin-3-yl 1 B-5185 H H H H H O H H 2-OMe-5-Cl-pyridin-3-yl 1 B-5186 H H H H H O H H 2-OMe-6-Cl-pyridin-3-yl 1 B-5187 H H H H H O H H 4-OMe-2-Cl-pyridin-3-yl 1 B-5188 H H H H H O H H 4-OMe-5-Cl-pyridin-3-yl 1 B-5189 H H H H H O H H 4-OMe-6-Cl-pyridin-3-yl 1 B-5190 H H H H H O H H 2-OMe-5-Me-pyridin-3-yl 1 B-5191 H H H H H O H H 2-OMe-6-Me-pyridin-3-yl 1 B-5192 H H H H H O H H 4-OMe-5-Me-pyridin-3-yl 1 B-5193 H H H H H O H H 4-OMe-6-Me-pyridin-3-yl 1 B-5194 H H H H H O H H 2,4-(OMe).sub.2-pyridin-3-yl 1 B-5195 H H H H H O H H 2,5-(OMe).sub.2-pyridin-3-yl 1 B-5196 H H H H H O H H 2,6-(OMe).sub.2-pyridin-3-yl 1 B-5197 H H H H H O H H 4,5-(OMe).sub.2-pyridin-3-yl 1 B-5198 H H H H H O H H 4,6-(OMe).sub.2-pyridin-3-yl 1 B-5199 H H H H H O H H pyridin-4-yl 1 B-5200 H H H H H O H H 2-F-pyridin-4-yl 1 B-5201 H H H H H O H H 3-F-pyridin-4-yl 1 B-5202 H H H H H O H H 2-Cl-pyridin-4-yl 1 B-5203 H H H H H O H H 3-Cl-pyridin-4-yl 1 B-5204 H H H H H O H H 2-Me-pyridin-4-yl 1 B-5205 H H H H H O H H 3-Me-pyridin-4-yl 1 B-5206 H H H H H O H H 2-CF.sub.3-pyridin-4-yl 1 B-5207 H H H H H O H H 3-CF.sub.3-pyridin-4-yl 1 B-5208 H H H H H O H H 2-OMe-pyridin-4-yl 1 B-5209 H H H H H O H H 3-OMe-pyridin-4-yl 1 B-5210 H H H H H O H H 2,3-F.sub.2-pyridin-4-yl 1 B-5211 H H H H H O H H 2,5-F.sub.2-pyridin-4-yl 1 B-5212 H H H H H O H H 2,6-F.sub.2-pyridin-4-yl 1 B-5213 H H H H H O H H 3,5-F.sub.2-pyridin-4-yl 1 B-5214 H H H H H O H H 2,3-Cl.sub.2-pyridin-4-yl 1 B-5215 H H H H H O H H 2,5-Cl.sub.2-pyridin-4-yl 1 B-5216 H H H H H O H H 2,6-Cl.sub.2-pyridin-4-yl 1 B-5217 H H H H H O H H 3,5-Cl.sub.2-pyridin-4-yl 1 B-5218 H H H H H O H H 3-F-2-Cl-pyridin-4-yl 1 B-5219 H H H H H O H H 3-F-5-Cl-pyridin-4-yl 1 B-5220 H H H H H O H H 3-F-6-Cl-pyridin-4-yl 1 B-5221 H H H H H O H H 3-F-2-Me-pyridin-4-yl 1 B-5222 H H H H H O H H 3-F-5-Me-pyridin-4-yl 1 B-5223 H H H H H O H H 3-F-6-Me-pyridin-4-yl 1
(291) TABLE-US-00190 TABLE 190 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-5224 H H H H H O H H 3-F-2-OMe-pyridin-4-yl 1 B-5225 H H H H H O H H 3-F-5-OMe-pyridin-4-yl 1 B-5226 H H H H H O H H 3-F-6-OMe-pyridin-4-yl 1 B-5227 H H H H H O H H 3-Cl-2-F-pyridin-4-yl 1 B-5228 H H H H H O H H 3-Cl-6-F-pyridin-4-yl 1 B-5229 H H H H H O H H 3-Cl-2-Me-pyridin-4-yl 1 B-5230 H H H H H O H H 3-Cl-5-Me-pyridin-4-yl 1 B-5231 H H H H H O H H 3-Cl-6-Me-pyridin-4-yl 1 B-5232 H H H H H O H H 3-Me-2-F-pyridin-4-yl 1 B-5233 H H H H H O H H 3-Me-6-F-pyridin-4-yl 1 B-5234 H H H H H O H H 3-Me-2-Cl-pyridin-4-yl 1 B-5235 H H H H H O H H 3-Me-6-Cl-pyridin-4-yl 1 B-5236 H H H H H O H H 2,3-(Me).sub.2-pyridin-4-yl 1 B-5237 H H H H H O H H 3,5-(Me).sub.2-pyridin-4-yl 1 B-5238 H H H H H O H H 3,6-(Me).sub.2-pyridin-4-yl 1 B-5239 H H H H H O H H 3-Me-2-OMe-pyridin-4-yl 1 B-5240 H H H H H O H H 3-Me-5-OMe-pyridin-4-yl 1 B-5241 H H H H H O H H 3-Me-6-OMe-pyridin-4-yl 1 B-5242 H H H H H O H H 3-CF.sub.3-2-F-pyridin-4-yl 1 B-5243 H H H H H O H H 3-CF.sub.3-5-F-pyridin-4-yl 1 B-5244 H H H H H O H H 3-CF.sub.3-6-F-pyridin-4-yl 1 B-5245 H H H H H O H H 3-CF.sub.3-2-Me-pyridin-4-yl 1 B-5246 H H H H H O H H 3-CF.sub.3-5-Me-pyridin-4-yl 1 B-5247 H H H H H O H H 3-CF.sub.3-6-Me-pyridin-4-yl 1 B-5248 H H H H H O H H 3-OMe-2-F-pyridin-4-yl 1 B-5249 H H H H H O H H 3-OMe-6-F-pyridin-4-yl 1 B-5250 H H H H H O H H 3-OMe-2-Cl-pyridin-4-yl 1 B-5251 H H H H H O H H 3-OMe-5-Cl-pyridin-4-yl 1 B-5252 H H H H H O H H 3-OMe-6-Cl-pyridin-4-yl 1 B-5253 H H H H H O H H 3-OMe-2-Me-pyridin-4-yl 1 B-5254 H H H H H O H H 3-OMe-6-Me-pyridin-4-yl 1 B-5255 H H H H H O H H 2,3-(OMe).sub.2-pyridin-4-yl 1 B-5256 H H H H H O H H 3,5-(OMe).sub.2-pyridin-4-yl 1 B-5257 H H H H H O H H 3,6-(OMe).sub.2-pyridin-4-yl 1 B-5258 H H H H H O H H pyrmidin-2-yl 1 B-5259 H H H H H O H H pyrimidin-4-yl 1 B-5260 H H H H H O H H 5-F-pyrimidin-4-yl 1 B-5261 H H H H H O H H 5-Me-pyrimidin-4-yl 1 B-5262 H H H H H O H H 5-CF.sub.3-pyrimidin-4-yl 1 B-5263 H H H H H O H H 5-OMe-pyrimidin-4-yl 1 B-5264 H H H H H O H H pyrimidin-5-yl 1 B-5265 H H H H H O H H 4-F-pyrimidin-5-yl 1 B-5266 H H H H H O H H 4-Cl-pyrmidin-5-yl 1 B-5267 H H H H H O H H 4-Me-pyrimidin-5-yl 1 B-5268 H H H H H O H H 4-CF.sub.3-pyrimidin-5-yl 1 B-5269 H H H H H O H H 4-OMe-pyrimidin-5-yl 1 B-5270 H H H H H O H H pyridazin-3-yl 1 B-5271 H H H H H O H H 4-F-pyridazin-3-yl 1 B-5272 H H H H H O H H 4-Cl-pyridazin-3-yl 1 B-5273 H H H H H O H H 4-Me-pyridazin-3-yl 1 B-5274 H H H H H O H H 4-CF.sub.3-pyridazin-3-yl 1 B-5275 H H H H H O H H 4-OMe-pyridazin-3-yl 1 B-5276 H H H H H O H H pyridazin-4-yl 1 B-5277 H H H H H O H H 3-F-pyridazin-4-yl 1 B-5278 H H H H H O H H 3-Cl-pyridazin-4-yl 1 B-5279 H H H H H O H H 3-Me-pyridazin-4-yl 1 B-5280 H H H H H O H H 3-CF.sub.3-pyridazin-4-yl 1
(292) TABLE-US-00191 TABLE 191 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-5281 H H H H H O H H 3-OMe-pyridazin-4-yl 1 B-5282 H H H H H O H H 5-F-pyridazin-4-yl 1 B-5283 H H H H H O H H 5-Cl-pyridazin-4-yl 1 B-5284 H H H H H O H H 5-Me-pyridazin-4-y 1 B-5285 H H H H H O H H 5-CF.sub.3-pyridazin-4-yl 1 B-5286 H H H H H O H H 5-OMe-pyridazin-4-yl 1 B-5287 H H H H H O H H thiophen-2-yl 1 B-5288 H H H H H O H H 3-F-thiopen-2-yl 1 B-5289 H H H H H O H H 3-Cl-thiophen-2-yl 1 B-5290 H H H H H O H H 3-Me-thiophen-2-yl 1 B-5291 H H H H H O H H 3-CF.sub.3-thiophen-2-y 1 B-5292 H H H H H O H H 3-OMe-thiophen-2-yl 1 B-5293 H H H H H O H H thiophen-3-yl 1 B-5294 H H H H H O H H 2-F-thiophen-3-yl 1 B-5295 H H H H H O H H 2-Cl-thiophen-3-yl 1 B-5296 H H H H H O H H 2-Me-thiophen-3-yl 1 B-5297 H H H H H O H H 2-CF.sub.3-thiophen-3-yl 1 B-5298 H H H H H O H H 2-OMe-thiophen-3-y 1 B-5299 H H H H H O H H 4-F-thiophen-3-yl 1 B-5300 H H H H H O H H 4-Cl-thiophen-3-yl 1 B-5301 H H H H H O H H 4-Me-thiophen-3-yl 1 B-5302 H H H H H O H H 4-CF.sub.3-thiophen-3-yl 1 B-5303 H H H H H O H H 4-OMe-thiophen-3-yl 1 B-5304 H H H H H O H H thiazol-2-yl 1 B-5305 H H H H H O H H thiazol-4-yl 1 B-5306 H H H H H O H H 5-F-thiazol-4-yl 1 B-5307 H H H H H O H H 5-Me-thiazol4-yl 1 B-5308 H H H H H O H H 5-CF.sub.3-thiazol-4-yl 1 B-5309 H H H H H O H H 5-OMe-thiazol-4-yl 1 B-5310 H H H H H O H H thiazol-5-yl 1 B-5311 H H H H H O H H 4-F-thiazol-5-y 1 B-5312 H H H H H O H H 4-Me-thiazol-5-yl 1 B-5313 H H H H H O H H 4-CF.sub.3-thiazol-5-yl 1 B-5314 H H H H H O H H 4-OMe-thiazol-5-yl 1 B-5315 H H H H H O H H 1H-pyrrol-1-yl 1 B-5316 H H H H H O H H 2-F-1H-pyrrol-1-yl 1 B-5317 H H H H H O H H 2-Me-1H-pyrrol-1-yl 1 B-5318 H H H H H O H H 2-CF.sub.3-1H-pyrrol-1-yl 1 B-5319 H H H H H O H H 2-OMe-1H-pyrrol-1-yl 1 B-5320 H H H H H O H H 1H-pyrrol-2-yl 1 B-5321 H H H H H O H H 1-Me-1H-pyrrol-2-yl 1 B-5322 H H H H H O H H 3-F-1H-pyrrol-2-yl 1 B-5323 H H H H H O H H 3-Me-1H-pyrrol-2-yl 1 B-5324 H H H H H O H H 3-CF.sub.3-1H-pyrrol-2-yl 1 B-5325 H H H H H O H H 3-OMe-1H-pyrrol-2-yl 1 B-5326 H H H H H O H H 1-Me-3-F-1H-pyrrol-2-yl 1 B-5327 H H H H H O H H 1,3-(Me).sub.2-1H-pyrrol-2-yl 1 B-5328 H H H H H O H H 1-Me-3-CF.sub.3-1H-pyrrol-2-yl 1 B-5329 H H H H H O H H 1-Me-3-OMe-1H-pyrrol-2-yl 1 B-5330 H H H H H O H H 1H-pyrrol-3-yl 1 B-5331 H H H H H O H H 1-Me-1H-pyrrol-3-yl 1 B-5332 H H H H H O H H 2-F-1H-pyrrol-3-yl 1 B-5333 H H H H H O H H 2-Me-1H-pyrrol-3-yl 1 B-5334 H H H H H O H H 2-CF.sub.3-1H-pyrrol-3-yl 1 B-5335 H H H H H O H H 2-OMe-1H-pyrrol-3-yl 1 B-5336 H H H H H O H H 1-Me-2-F-1H-pyrrol-3-yl 1 B-5337 H H H H H O H H 1,2-(Me).sub.2-1H-pyrrol-3-yl 1
(293) TABLE-US-00192 TABLE 192 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-5338 H H H H H O H H 1-Me-2-CF.sub.3-1H-pyrrol-3-yl 1 B-5339 H H H H H O H H 1-Me-2-OMe-1H-pyrrol-3-yl 1 B-5340 H H H H H O H H 4-F-1H-pyrrol-3-yl 1 B-5341 H H H H H O H H 4-Me-1H-pyrrol-3-yl 1 B-5342 H H H H H O H H 4-CF.sub.3-1H-pyrrol-3-yl 1 B-5343 H H H H H O H H 4-OMe-1H-pyrrol-3-yl 1 B-5344 H H H H H O H H 1-Me-4-F-1H-pyrrol-3-yl 1 B-5345 H H H H H O H H 1,4-(Me).sub.2-1H-pyrrol-3-yl 1 B-5346 H H H H H O H H 1-Me-4-CF.sub.3-1H-pyrrol-3-yl 1 B-5347 H H H H H O H H 1-Me-4-OMe-1H-pyrrol-3-yl 1 B-5348 H H H H H O H H 1H-pyrazol-1-yl 1 B-5349 H H H H H O H H 5-F-1H-pyrazol-1-yl 1 B-5350 H H H H H O H H 5-Cl-1H-pyrazol-1-yl 1 B-5351 H H H H H O H H 5-Me-1H-pyrazol-1-yl 1 B-5352 H H H H H O H H 5-CF.sub.3-1H-pyrazol-1-yl 1 B-5353 H H H H H O H H 5-OMe-1H-pyrazol-1-yl 1 B-5354 H H H H H O H H 1H-pyrazol-3-yl 1 B-5355 H H H H H O H H 1-Me-1H-pyrazol-3-yl 1 B-5356 H H H H H O H H 4F-1H-pyrazol-3-yl 1 B-5357 H H H H H O H H 4-Cl-1H-pyrazol-3-yl 1 B-5358 H H H H H O H H 4-Me-1H-pyrazol-3-yl 1 B-5359 H H H H H O H H 4-CF.sub.3-1H-pyrazol-3-yl 1 B-5360 H H H H H O H H 4-OMe-1H-pyrazol-3-yl 1 B-5361 H H H H H O H H 1-Me-4-F-1H-pyrazol-3-yl 1 B-5362 H H H H H O H H 1-Me-4-Cl-1H-pyrazol-3-yl 1 B-5363 H H H H H O H H 1,4-(Me).sub.2-1H-pyrazol-3-yl 1 B-5364 H H H H H O H H 1-Me-4-CF.sub.3-1H-pyrazol-3-yl 1 B-5365 H H H H H O H H 1-Me-4-OMe-1H-pyrazol-3-yl 1 B-5366 H H H H H O H H 1H-pyrazol4-yl 1 B-5367 H H H H H O H H 1-Me-1H-pyrazol-4-yl 1 B-5368 H H H H H O H H 3-F-1H-pyrazol-4-yl 1 B-5369 H H H H H O H H 3-Cl-1H-pyrazol-4-yl 1 B-5370 H H H H H O H H 3-Me-1H-pyrazol-4-yl 1 B-5371 H H H H H O H H 3-CF.sub.3-1H-pyrazol-4-yl 1 B-5372 H H H H H O H H 3-OMe-1H-pyrazol-4-yl 1 B-5373 H H H H H O H H 1-Me-3-F-1H-pyrazol-4-yl 1 B-5374 H H H H H O H H 1-Me-3-Cl-1H-pyrazol-4-yl 1 B-5375 H H H H H O H H 1,3-(Me).sub.2-1H-pyrazol-4-yl 1 B-5376 H H H H H O H H 1-Me-3-CF.sub.3-1H-pyrazol-4-yl 1 B-5377 H H H H H O H H 1-Me-3-OMe-1H-pyrazol-4-yl 1 B-5378 H H H H H O H H 5-F-1H-pyrazol-4-yl 1 B-5379 H H H H H O H H 5-Cl-1H-pyrazol-4-yl 1 B-5380 H H H H H O H H 5-Me-1H-pyrazol-4-yl 1 B-5381 H H H H H O H H 5-CF.sub.3-1H-pyrazol-4-yl 1 B-5382 H H H H H O H H 5-OMe-1H-pyrazol-4-yl 1 B-5383 H H H H H O H H 1-Me-5F-1H-pyrazol-4-yl 1 B-5384 H H H H H O H H 1-Me-5-Cl-1H-pyrazol-4-yl 1 B-5385 H H H H H O H H 1,5-(Me).sub.2-1H-pyrazol-4-yl 1 B-5386 H H H H H O H H 1-Me-5-CF.sub.3-1H-pyrazol-4-yl 1 B-5387 H H H H H O H H 1-Me-5-OMe-1H-pyrazol-4-yl 1 B-5388 H H H H H O H H 1H-pyrazol-5-yl 1 B-5389 H H H H H O H H 1-Me-1H-pyrazol-5-yl 1 B-5390 H H H H H O H H 4-F-1H-pyrazol-5-yl 1 B-5391 H H H H H O H H 4-Cl-H-pyrazol-5-yl 1 B-5392 H H H H H O H H 4-Me-1H-pyrazol-5-yl 1 B-5393 H H H H H O H H 4-CF.sub.3-1H-pyrazol-5-yl 1 B-5394 H H H H H O H H 4-OMe-1H-pyrazol-5-yl 1
(294) TABLE-US-00193 TABLE 193 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-5395 H H H H H O H H 1-Me-4F-1H-pyrazol-5-yl 1 B-5396 H H H H H O H H 1-Me-4-Cl-1H-pyrazol-5-yl 1 B-5397 H H H H H O H H 1,4-(Me).sub.2-1H-pyrazol-5-yl 1 B-5398 H H H H H O H H 1-Me-4-CF.sub.3-1H-pyrazol-5-yl 1 B-5399 H H H H H O H H 1-Me-4-OMe-1H-pyrazol-5-yl 1 B-5400 H H H H H O H H furan-2-yl 1 B-5401 H H H H H O H H 3-F-furan-2-yl 1 B-5402 H H H H H O H H 3-Me-furan-2-yl 1 B-5403 H H H H H O H H 3-CF.sub.3-furan-2-yl 1 B-5404 H H H H H O H H 3-OMe-furan-2-yl 1 B-5405 H H H H H O H H furan-3-yl 1 B-5406 H H H H H O H H 2-F-furan-3-yl 1 B-5407 H H H H H O H H 2-Me-furan-3-yl 1 B-5408 H H H H H O H H 2-CF.sub.3-furan-3-yl 1 B-5409 H H H H H O H H 2-OMe-furan-3-yl 1 B-5410 H H H H H O H H 4-F-furan-3-yl 1 B-5411 H H H H H O H H 4-Me-furan-3-yl 1 B-5412 H H H H H O H H 4-CF.sub.3-furan-3-yl 1 B-5413 H H H H H O H H 4-OMe-furan-3-yl 1 B-5414 H H H H H O H H isoxazol-3-yl 1 B-5415 H H H H H O H H 4-F-isoxazol-3-yl 1 B-5416 H H H H H O H H 4-Me-isoxazol-3-yl 1 B-5417 H H H H H O H H 4-CF.sub.3-isoxazol-3-yl 1 B-5418 H H H H H O H H 4-OMe-isoxazol-3-yl 1 B-5419 H H H H H O H H isoxazol-4-yl 1 B-5420 H H H H H O H H 5-F-isoxazol-4-yl 1 B-5421 H H H H H O H H 5-Me-isoxazol-4-yl 1 B-5422 H H H H H O H H 5-CF.sub.3-isoxazol-4-yl 1 B-5423 H H H H H O H H 5-OMe-isoxazol-4-yl 1 B-5424 H H H H H O H H isoxazol-5-yl 1 B-5425 H H H H H O H H 4-F-isoxazol-5-yl 1 B-5426 H H H H H O H H 4-Me-isoxazol-5-yl 1 B-5427 H H H H H O H H 4-CF.sub.3-isoxazol-5-yl 1 B-5428 H H H H H O H H 4-OMe-isoxazol-5-yl 1 B-5429 H H H H H O H H 1H-1,2,3-triazol-1-yl 1 B-5430 H H H H H O H H 5-F-1H-1,2,3-triazol-1-yl 1 B-5431 H H H H H O H H 5-Me-1H-1,2,3-triazol-1-yl 1 B-5432 H H H H H O H H 5-CF.sub.3-1H-1,2,3-triazol-1-yl 1 B-5433 H H H H H O H H 5-OMe-1H-1,2,3-triazol-1-yl 1 B-5434 H H H H H O H H 1H-1,2,3-triazol-4-yl 1 B-5435 H H H H H O H H 5-F-1H-1,2,3-triazol-4-yl 1 B-5436 H H H H H O H H 5-Me-1H-1,2,3-triazol-4-yl 1 B-5437 H H H H H O H H 5-CF.sub.3-1H-1,2,3-triazol-4-y 1 B-5438 H H H H H O H H 5-OMe-1H-1,2,3-triazol-4-yl 1 B-5439 H H H H H O H H 1H-1,2,3-triazol-5-yl 1 B-5440 H H H H H O H H 4-F-1H-1,2,3-triazol-5-yl 1 B-5441 H H H H H O H H 4-Me-1H-1,2,3-triazol-5-yl 1 B-5442 H H H H H O H H 4-CF.sub.3-1H-1,2,3-triazol-5-yl 1 B-5443 H H H H H O H H 4-OMe-1H-1,2,3-triazol-5-yl 1 B-5444 H H H H H O H H 1H-1,2,4-triazol-1-yl 1 B-5445 H H H H H O H H 5-Me-1H-1,2,4-triazol-1-yl 1 B-5446 H H H H H O H H 5-F-1H-1,2,4-triazol-1-yl 1 B-5447 H H H H H O H H 5-CF.sub.3-1H-1,2,4-triazol-1-yl 1 B-5448 H H H H H O H H 5-OMe-1H-1,2,4-triazol-1-yl 1 B-5449 H H H H H O H H 1H-1,2,4-triazol-3-yl 1 B-5450 H H H H H O H H 1-Me-1H-1,2,4-triazol-3-yl 1 B-5451 H H H H H O H H 1H-1,2,4-triazol-5-yl 1
(295) TABLE-US-00194 TABLE 194 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 A R.sup.6 R.sup.7 Q p B-5452 H H H H H O H H 1-Me-1H-1,2,4-triazol-5-yl 1 B-5453 H H H H H O H H 3,5-(Me).sub.2-isoxazol-4-yl 1 B-5454 H H H H H O H H 3,5-(Me).sub.2-isoxazol-4-yl 1 B-5455 H H H H H O H H 1,3,5-(Me).sub.3-1H-pyrazol-4-yl 1 B-5456 H H H H H O H H quinolin-4-yl 1 B-5457 H H H H H O H H isoquinolin-4-yl 1 B-5458 H H H H H O H H 3,6-(OMe).sub.2-pyridazin-4-yl 1 B-5459 H H H H H O H H 2,4-(OMe).sub.2-pyrmidin-5-yl 1
(296) TABLE-US-00195 TABLE 195
(297) TABLE-US-00196 TABLE 196 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0052 H H H H H 4-CH.sub.2F 0 C-0053 H H H H H 2-CF.sub.2Cl 0 C-0054 H H H H H 3-CF.sub.2Cl 0 C-0055 H H H H H 4-CF.sub.2Cl 0 C-0056 H H H H H 2-CF(CF.sub.3).sub.2 0 C-0057 H H H H H 3-CF(CF.sub.3).sub.2 0 C-0058 H H H H H 4-CF(CF.sub.3).sub.2 0 C-0059 H H H H H 2-cycloprop 0 C-0060 H H H H H 3-cyclopropyl 0 C-0061 H H H H H 4-cyclopropyl 0 C-0062 H H H H H 2-cyclobutyl 0 C-0063 H H H H H 3-cyclobutyl 0 C-0064 H H H H H 4-cyclobutyl 0 C-0065 H H H H H 2-cyclopentyl 0 C-0066 H H H H H 3-cyclopentyl 0 C-0067 H H H H H 4-cyclopentyl 0 C-0068 H H H H H 2-(cyclopropylmethyl) 0 C-0069 H H H H H 3-(cyclopropylmethyl) 0 C-0070 H H H H H 4-(cyclopropylmethyl) 0 C-0071 H H H H H 2-(cyclobutylmethyl) 0 C-0072 H H H H H 3-(cyclobutylmethyl) 0 C-0073 H H H H H 4-(cyclobutylmethyl) 0 C-0074 H H H H H 2-(cyclopentylmethyl) 0 C-0075 H H H H H 3-(cyclopentylmethyl) 0 C-0076 H H H H H 4-(cyclopentylmethyl) 0 C-0077 H H H H H 2-(cyclopropylethyl) 0 C-0078 H H H H H 3-(cyclopropylethyl) 0 C-0079 H H H H H 4-(cyclopropylethyl) 0 C-0080 H H H H H 2-(2,2-difluorocyclopropyl) 0 C-0081 H H H H H 3-(2,2-difluorocyclopropyl) 0 C-0082 H H H H H 4-(2,2-difluorocyclopropyl) 0 C-0083 H H H H H 2-(2,2-dichlorocyclopropyl) 0 C-0084 H H H H H 3-(2,2-dichlorocyclopropyl) 0 C-0085 H H H H H 4-(2,2-dichlorocyclopropyl) 0 C-0086 H H H H H 2-ethenyl 0 C-0087 H H H H H 3-ethenyl 0 C-0088 H H H H H 4-ethenyl 0 C-0089 H H H H H 2-allyl 0 C-0090 H H H H H 3-allyl 0 C-0091 H H H H H 4-allyl 0 C-0092 H H H H H 2-(prop-1-en-1-yl) 0 C-0093 H H H H H 3-(prop-1-en-1-yl) 0 C-0094 H H H H H 4-(prop-1-en-1-yl) 0 C-0095 H H H H H 2-(trifluoroethenyl) 0 C-0096 H H H H H 3-(trifluoroethenyl) 0 C-0097 H H H H H 4-(trifluoroethenyl) 0 C-0098 H H H H H 2-(2,2-dichloroethenyl) 0 C-0099 H H H H H 3-(2,2-dichloroethenyl) 0 C-0100 H H H H H 4-(2,2-dichloroethenyl) 0 C-0101 H H H H H 2-ethynyl 0 C-0102 H H H H H 3-ethynyl 0 C-0103 H H H H H 4-ethynyl 0 C-0104 H H H H H 2-(1-propyn-1-yl) 0 C-0105 H H H H H 3-(1-propyn-1-yl) 0 C-0106 H H H H H 4-(1-propyn-1-yl) 0 C-0107 H H H H H 2-(2-propyn-1-yl) 0
(298) TABLE-US-00197 TABLE 197 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0108 H H H H H 3-(2-propyn-1-yl) 0 C-0109 H H H H H 4-(2-propyn-1-yl) 0 C-0110 H H H H H 2-(2-cyclopropylethynyl) 0 C-0111 H H H H H 3-(2-cyclopropylethynyl) 0 C-0112 H H H H H 4-(2-cyclopropylethynyl) 0 C-0113 H H H H H 2-(2-chloroethynyl) 0 C-0114 H H H H H 3-(2-chloroethynyl) 0 C-0115 H H H H H 4-(2-chloroethynyl) 0 C-0116 H H H H H 2-(2-bromoethynyl) 0 C-0117 H H H H H 3-(2-bromoethynyl) 0 C-0118 H H H H H 4-(2-bromoethynyl) 0 C-0119 H H H H H 2-OMe 0 C-0120 H H H H H 3-OMe 0 C-0121 H H H H H 4-OMe 0 C-0122 H H H H H 2-OEt 0 C-0123 H H H H H 3-OEt 0 C-0124 H H H H H 4-OEt 0 C-0125 H H H H H 2-OPr 0 C-0126 H H H H H 3-OPr 0 C-0127 H H H H H 4-OPr 0 C-0128 H H H H H 2-O(i-Pr) 0 C-0129 H H H H H 3-O(i-Pr) 0 C-0130 H H H H H 4-O(i-Pr) 0 C-0131 H H H H H 2-OBu 0 C-0132 H H H H H 3-OBu 0 C-0133 H H H H H 4-OBu 0 C-0134 H H H H H 2-O(s-Bu) 0 C-0135 H H H H H 3-O(s-Bu) 0 C-0136 H H H H H 4-O(s-Bu) 0 C-0137 H H H H H 2-O(i-Bu) 0 C-0138 H H H H H 3-O(i-Bu) 0 C-0139 H H H H H 4-O(i-Bu) 0 C-0140 H H H H H 2-O(t-Bu) 0 C-0141 H H H H H 3-O(t-Bu) 0 C-0142 H H H H H 4-O(t-Bu) 0 C-0143 H H H H H 2-OCF.sub.3 0 C-0144 H H H H H 3-OCF.sub.3 0 C-0145 H H H H H 4-OCF.sub.3 0 C-0146 H H H H H 2-OCHF.sub.2 0 C-0147 H H H H H 3-OCHF.sub.2 0 C-0148 H H H H H 4-OCHF.sub.2 0 C-0149 H H H H H 2-OCH.sub.2CF.sub.3 0 C-0150 H H H H H 3-OCH.sub.2CF.sub.3 0 C-0151 H H H H H 4-OCH.sub.2CF.sub.3 0 C-0152 H H H H H 2-(cyclopropyloxy) 0 C-0153 H H H H H 3-(cyclopropyloxy) 0 C-0154 H H H H H 4-(cyclopropyloxy) 0 C-0155 H H H H H 2-(cyclobutyloxy) 0 C-0156 H H H H H 3-(cyclobutyloxy) 0 C-0157 H H H H H 4-(cyclobutyloxy) 0 C-0158 H H H H H 2-(cyclopentyloxy) 0 C-0159 H H H H H 3-(cyclopentyloxy) 0 C-0160 H H H H H 4-(cyclopentyloxy) 0 C-0161 H H H H H 2-((2,2-dichlorocyclopropyl)oxy) 0 C-0162 H H H H H 3-((2,2-dichlorocyclopropyl)oxy) 0 C-0163 H H H H H 4-((2,2-dichlorocyclopropyl)oxy) 0
(299) TABLE-US-00198 TABLE 198 com- pound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0164 H H H H H 2-(cyclopropylmethoxy) 0 C-0165 H H H H H 3-(cyclopropylmethoxy) 0 C-0166 H H H H H 4-(cyclopropylmethoxy) 0 C-0167 H H H H H 2-((2,2- 0 difluorocyclopropyl)methoxy) C-0168 H H H H H 3-((2,2- 0 difluorocyclopropyl)methoxy) C-0169 H H H H H 4-((2,2- 0 difluorocyclopropyl)methoxy) C-0170 H H H H H 2-(oxiran-2-yl) 0 C-0171 H H H H H 3-(oxiran-2-yl) 0 C-0172 H H H H H 4-(oxiran-2-yl) 0 C-0173 H H H H H 2-(oxiran-2-ylmethyl) 0 C-0174 H H H H H 3-(oxiran-2-ylmethyl) 0 C-0175 H H H H H 4-(oxiran-2-ylmethyl) 0 C-0176 H H H H H 2-SMe 0 C-0177 H H H H H 3-SMe 0 C-0178 H H H H H 4-SMe 0 C-0179 H H H H H 2-SEt 0 C-0180 H H H H H 3-SEt 0 C-0181 H H H H H 4-SEt 0 C-0182 H H H H H 2-S(?O)Me 0 C-0183 H H H H H 3-S(?O)Me 0 C-0184 H H H H H 4-S(?O)Me 0 C-0185 H H H H H 2-S(?O).sub.2Me 0 C-0186 H H H H H 3-S(?O).sub.2Me 0 C-0187 H H H H H 4-S(?O).sub.2Me 0 C-0188 H H H H H 2-SCF.sub.3 0 C-0189 H H H H H 3-SCF.sub.3 0 C-0190 H H H H H 4-SCF.sub.3 0 C-0191 H H H H H 2-S(?O)CF.sub.3 0 C-0192 H H H H H 3-S(?O)CF.sub.3 0 C-0193 H H H H H 4-S(?O)CF.sub.3 0 C-0194 H H H H H 2-S(?O).sub.2CF.sub.3 0 C-0195 H H H H H 3-S(?O).sub.2CF.sub.3 0 C-0196 H H H H H 4-S(?O).sub.2CF.sub.3 0 C-0197 H H H H H 2-SCF(CF.sub.3).sub.2 0 C-0198 H H H H H 3-SCF(CF.sub.3).sub.2 0 C-0199 H H H H H 4-SCF(CF.sub.3).sub.2 0 C-0200 H H H H H 2-(cyclopropylthio) 0 C-0201 H H H H H 3-(cyclopropylthio) 0 C-0202 H H H H H 4-(cyclopropylthio) 0 C-0203 H H H H H 2-(cyclopropylsulfinyl) 0 C-0204 H H H H H 3-(cyclopropylsulfinyl) 0 C-0205 H H H H H 4-(cyclopropylsulfinyl) 0 C-0206 H H H H H 2-(cyclopropylsulfonyl) 0 C-0207 H H H H H 3-(cyclopropysulfonyl) 0 C-0208 H H H H H 4-(cyclopropylsulfonyl) 0 C-0209 H H H H H 2-((cyclopropylmethyl)thio) 0 C-0210 H H H H H 3-((cyclopropylmethyl)thio) 0 C-0211 H H H H H 4-((cyclopropylmethyl)thio) 0 C-0212 H H H H H 2-((cyclopropylmethyl)sulfinyl) 0 C-0213 H H H H H 3-((cyclopropylmethyl)sulfinyl) 0 C-0214 H H H H H 4-((cyclopropylmethyl)sulfinyl) 0 C-0215 H H H H H 2-((cyclopropylmethyl)sulfonyl) 0 C-0216 H H H H H 3-((cyclopropylmethyl)sulfonyl) 0 C-0217 H H H H H 4-((cyclopropylmethyl)sulfonyl) 0 C-0218 H H H H H 2-(((2,2- 0 difluorocyclopropyl)methyl)thio) C-0219 H H H H H 3-(((2,2- 0 difluorocyclopropyl)methyl)thio)
(300) TABLE-US-00199 TABLE 199 com- pound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0220 H H H H H 4-(((2,2- 0 difluorocyclopropyl)methyl)thio) C-0221 H H H H H 2-(((2,2- 0 difluorocyclopropyl)methyl)sulfinyl) C-0222 H H H H H 3-(((2,2- 0 difluorocyclopropyl)methyl)sulfinyl) C-0223 H H H H H 4-(((2,2- 0 difluorocyclopropyl)methyl)sulfinyl) C-0224 H H H H H 2-(((2,2- 0 difluorocyclopropyl)methyl)sulfonyl) C-0225 H H H H H 3-(((2,2- 0 difluorocyclopropyl)methyl)sulfonyl) C-0226 H H H H H 4-(((2,2- 0 difluorocyclopropyl)methyl)sulfonyl) C-0227 H H H H H 2-C(?O)Me 0 C-0228 H H H H H 3-C(?O)Me 0 C-0229 H H H H H 4-C(?O)Me 0 C-0230 H H H H H 2-C(?O)Et 0 C-0231 H H H H H 3-C(?O)Et 0 C-0232 H H H H H 4-C(?O)Et 0 C-0233 H H H H H 2-C(?O)CF.sub.3 0 C-0234 H H H H H 3-C(?O)CF.sub.3 0 C-0235 H H H H H 4-C(?O)CF.sub.3 0 C-0236 H H H H H 2-C(?O)OMe 0 C-0237 H H H H H 3-C(?O)OMe 0 C-0238 H H H H H 4-C(?O)OMe 0 C-0239 H H H H H 2-C(?O)OEt 0 C-0240 H H H H H 3-C(?O)OEt 0 C-0241 H H H H H 4-C(?O)OEt 0 C-0242 H H H H H 2-C(?O)NH.sub.2 0 C-0243 H H H H H 3-C(?O)NH.sub.2 0 C-0244 H H H H H 4-C(?O)NH.sub.2 0 C-0245 H H H H H 2-C(?O)NHMe 0 C-0246 H H H H H 3-C(?O)NHMe 0 C-0247 H H H H H 4-C(?O)NHMe 0 C-0248 H H H H H 2-C(?O)NMe.sub.2 0 C-0249 H H H H H 3-C(?O)NMe.sub.2 0 C-0250 H H H H H 4-C(?O)NMe.sub.2 0 C-0251 H H H H H 2-CH.sub.2C(?O)CH.sub.3 0 C-0252 H H H H H 3-CH.sub.2C(?O)CH.sub.3 0 C-0253 H H H H H 4-CH.sub.2C(?O)CH.sub.3 0 C-0254 H H H H H 2-CH.sub.2C(?O)CF.sub.3 0 C-0255 H H H H H 3-CH.sub.2C(?O)CF.sub.3 0 C-0256 H H H H H 4-CH.sub.2C(?O)CF.sub.3 0 C-0257 H H H H H 2-CH.sub.2C(?O)OCH.sub.3 0 C-0258 H H H H H 3-CH.sub.2C(?O)OCH.sub.3 0 C-0259 H H H H H 4-CH.sub.2C(?O)OCH.sub.3 0 C-0260 H H H H H 2-CH.sub.2OH 0 C-0261 H H H H H 3-CH.sub.2OH 0 C-0262 H H H H H 4-CH.sub.2OH 0 C-0263 H H H H H 2-CH.sub.2OCH.sub.3 0 C-0264 H H H H H 3-CH.sub.2OCH.sub.3 0 C-0265 H H H H H 4-CH.sub.2OCH.sub.3 0 C-0266 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3 0 C-0267 H H H H H 3-CH.sub.2OCH.sub.2CH.sub.3 0 C-0268 H H H H H 4-CH.sub.2OCH.sub.2CH.sub.3 0 C-0269 H H H H H 2-CH(CH.sub.3)OCH.sub.3 0 C-0270 H H H H H 3-CH(CH.sub.3)OCH.sub.3 0 C-0271 H H H H H 4-CH(CH.sub.3)OCH.sub.3 0 C-0272 H H H H H 2-CH.sub.2CH.sub.2OCH.sub.3 0 C-0273 H H H H H 3-CH.sub.2CH.sub.2OCH.sub.3 0 C-0274 H H H H H 4-CH.sub.2CH.sub.2OCH.sub.3 0 C-0275 H H H H H 2-CH.sub.2OCF.sub.3 0
(301) TABLE-US-00200 TABLE 200 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0276 H H H H H 3-CH.sub.2OCF.sub.3 0 C-0277 H H H H H 4-CH.sub.2OCF.sub.3 0 C-0278 H H H H H 2-CF.sub.2OCH.sub.3 0 C-0279 H H H H H 3-CF.sub.2OCH.sub.3 0 C-0280 H H H H H 4-CF.sub.2OCH.sub.3 0 C-0281 H H H H H 2-CF.sub.2CF.sub.2OCF.sub.3 0 C-0282 H H H H H 3-CF.sub.2CF.sub.2OCF.sub.3 0 C-0283 H H H H H 4-CF.sub.2CF.sub.2OCF.sub.3 0 C-0284 H H H H H 2-OC(?O)CH.sub.3 0 C-0285 H H H H H 3-OC(?O)CH.sub.3 0 C-0286 H H H H H 4-OC(?O)CH.sub.3 0 C-0287 H H H H H 2-OC(?O)CF.sub.3 0 C-0288 H H H H H 3-OC(?O)CF.sub.3 0 C-0289 H H H H H 4-OC(?O)CF.sub.3 0 C-0290 H H H H H 2-OC(?O)NH.sub.2 0 C-0291 H H H H H 3-OC(?O)NH.sub.2 0 C-0292 H H H H H 4-OC(?O)NH.sub.2 0 C-0293 H H H H H 2-OC(?O)NHCH.sub.3 0 C-0294 H H H H H 3-OC(?O)NHCH.sub.3 0 C-0295 H H H H H 4-OC(?O)NHCH.sub.3 0 C-0296 H H H H H 2-OC(?O)N(CH.sub.3).sub.2 0 C-0297 H H H H H 3-OC(?O)N(CH.sub.3).sub.2 0 C-0298 H H H H H 4-OC(?O)N(CH.sub.3).sub.2 0 C-0299 H H H H H 2-CH.sub.2OC(?O)NH.sub.2 0 C-0300 H H H H H 3-CH.sub.2OC(?O)NH.sub.2 0 C-0301 H H H H H 4-CH.sub.2OC(?O)NH.sub.2 0 C-0302 H H H H H 2-CH.sub.2OC(?O)NHCH.sub.3 0 C-0303 H H H H H 3-CH.sub.2OC(?O)NHCH.sub.3 0 C-0304 H H H H H 4-CH.sub.2OC(?O)NHCH.sub.3 0 C-0305 H H H H H 2-CH.sub.2OC(?O)N(CH.sub.3).sub.2 0 C-0306 H H H H H 3-CH.sub.2OC(?O)N(CH.sub.3).sub.2 0 C-0307 H H H H H 4-CH.sub.2OC(?O)N(CH.sub.3).sub.2 0 C-0308 H H H H H 2-OC(?O)OCH.sub.3 0 C-0309 H H H H H 3-OC(?O)OCH.sub.3 0 C-0310 H H H H H 4-OC(?O)OCH.sub.3 0 C-0311 H H H H H 2-CH.sub.2OC(?O)OCH.sub.3 0 C-0312 H H H H H 3-CH.sub.2OC(?O)OCH.sub.3 0 C-0313 H H H H H 4-CH.sub.2OC(?O)OCH.sub.3 0 C-0314 H H H H H 2-CH.sub.2OC(?O)CH.sub.3 0 C-0315 H H H H H 3-CH.sub.2OC(?O)CH.sub.3 0 C-0316 H H H H H 4-CH.sub.2OC(?O)CH.sub.3 0 C-0317 H H H H H 2-OS(?O).sub.2CH.sub.3 0 C-0318 H H H H H 3-OS(?O).sub.2CH.sub.3 0 C-0319 H H H H H 4-OS(?O).sub.2CH.sub.3 0 C-0320 H H H H H 2-CH.sub.2SCH.sub.3 0 C-0321 H H H H H 3-CH.sub.2SCH.sub.3 0 C-0322 H H H H H 4-CH.sub.2SCH.sub.3 0 C-0323 H H H H H 2-CH.sub.2S(?O)CH.sub.3 0 C-0324 H H H H H 3-CH.sub.2S(?O)CH.sub.3 0 C-0325 H H H H H 4-CH.sub.2S(?O)CH.sub.3 0 C-0326 H H H H H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 C-0327 H H H H H 3-CH.sub.2S(?O).sub.2CH.sub.3 0 C-0328 H H H H H 4-CH.sub.2S(?O).sub.2CH.sub.3 0 C-0329 H H H H H 2-CH.sub.2SCF.sub.3 0 C-0330 H H H H H 3-CH.sub.2SCF.sub.3 0 C-0331 H H H H H 4-CH.sub.2SCF.sub.3 0
(302) TABLE-US-00201 TABLE 201 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0332 H H H H H 2-CH.sub.2S(?O)CF.sub.3 0 C-0333 H H H H H 3-CH.sub.2S(?O)CF.sub.3 0 C-0334 H H H H H 4-CH.sub.2S(?O)CF.sub.3 0 C-0335 H H H H H 2-CH.sub.2S(?O).sub.2CF.sub.3 0 C-0336 H H H H H 3-CH.sub.2S(?O).sub.2CF.sub.3 0 C-0337 H H H H H 4-CH.sub.2S(?O).sub.2CF.sub.3 0 C-0338 H H H H H 2-phenyl 0 C-0339 H H H H H 3-phenyl 0 C-0340 H H H H H 4-phenyl 0 C-0341 H H H H H 2-(phenyloxy) 0 C-0342 H H H H H 3-(phenyloxy) 0 C-0343 H H H H H 4-(phenyloxy) 0 C-0344 H H H H H 2-benzyl 0 C-0345 H H H H H 3-benzyl 0 C-0346 H H H H H 4-benzyl 0 C-0347 H H H H H 2-(benzyloxy) 0 C-0348 H H H H H 3-(benzyloxy) 0 C-0349 H H H H H 4-(benzyloxy) 0 C-0350 H H H H H 2-((2-fluorobenzyl)oxy) 0 C-0351 H H H H H 3-((2-fluorobenzyl)oxy) 0 C-0352 H H H H H 4-((2-fluorobenzyl)oxy) 0 C-0353 H H H H H 2-((3-fluorobenzyl)oxy) 0 C-0354 H H H H H 3-((3-fluorobenzyl)oxy) 0 C-0355 H H H H H 4-((3-fluorobenzyl)oxy) 0 C-0356 H H H H H 2-((4-fluorobenzyl)oxy) 0 C-0357 H H H H H 3-((4-fluorobenzyl)oxy) 0 C-0358 H H H H H 4-((4-fluorobenzyl)oxy) 0 C-0359 H H H H H 2-((2-chlorobenzyl)oxy) 0 C-0360 H H H H H 3-((2-chlorobenzyl)oxy) 0 C-0361 H H H H H 4-((2-chlorobenzyl)oxy) 0 C-0362 H H H H H 2-((3-chlorobenzyl)oxy) 0 C-0363 H H H H H 3-((3-chlorobenzyl)oxy) 0 C-0364 H H H H H 4-((3-chlorobenzyl)oxy) 0 C-0365 H H H H H 2-((4-chlorobenzyl)oxy) 0 C-0366 H H H H H 3-((4-chlorobenzyl)oxy) 0 C-0367 H H H H H 4-((4-chlorobenzyl)oxy) 0 C-0368 H H H H H 2-((2-methylbenzyl)oxy) 0 C-0369 H H H H H 3-((2-methylbenzyl)oxy) 0 C-0370 H H H H H 4-((2-methylbenzyl)oxy) 0 C-0371 H H H H H 2-((3-methylbenzyl)oxy) 0 C-0372 H H H H H 3-((3-methylbenzyl)oxy) 0 C-0373 H H H H H 4-((3-methylbenzyl)oxy) 0 C-0374 H H H H H 2-((4-methylbenzyl)oxy) 0 C-0375 H H H H H 3-((4-methylbenzyl)oxy) 0 C-0376 H H H H H 4-((4-methylbenzyl)oxy) 0 C-0377 H H H H H 2-((2-(trifluoromethyl)benzyl)oxy) 0 C-0378 H H H H H 3-((2-(trifluoromethyl)benzyl)oxy) 0 C-0379 H H H H H 4-((2-(trifluoromethyl)benzyl)oxy) 0 C-0380 H H H H H 2-((3-(trifluoromethyl)benzyl)oxy) 0 C-0381 H H H H H 3-((3-(trifluoromethyl)benzyl)oxy) 0 C-0382 H H H H H 4-((3-(trifluoromethyl)benzyl)oxy) 0 C-0383 H H H H H 2-((4-(trifluoromethyl)benzyl)oxy) 0 C-0384 H H H H H 3-((4-(trifluoromethyl)benzyl)oxy) 0 C-0385 H H H H H 4-((4-(trifluoromethyl)benzyl)oxy) 0 C-0386 H H H H H 2-((2-methoxybenzyl)oxy) 0 C-0387 H H H H H 3-((2-methoxybenzyl)oxy) 0
(303) TABLE-US-00202 TABLE 202 com- pound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0388 H H H H H 4-((2-methoxybenzyl)oxy) 0 C-0389 H H H H H 2-((3-methoxybenzyl)oxy) 0 C-0390 H H H H H 3-((3-methoxybenzyl)oxy) 0 C-0391 H H H H H 4-((3-methoxybenzyl)oxy) 0 C-0392 H H H H H 2-((4-methoxybenzyl)oxy) 0 C-0393 H H H H H 3-((4-methoxybenzyl)oxy) 0 C-0394 H H H H H 4-((4-methoxybenzyl)oxy) 0 C-0395 H H H H H 2-((2-(trifluoromethoxy)benzyl)oxy) 0 C-0396 H H H H H 3-((2-(trifluoromethoxy)benzyl)oxy) 0 C-0397 H H H H H 4-((2-(trifluoromethoxy)benzyl)oxy) 0 C-0398 H H H H H 2-((3-(trifluoromethoxy)benzyl)oxy) 0 C-0399 H H H H H 3-((3-(trifluoromethoxy)benzyl)oxy) 0 C-0400 H H H H H 4-((3-(trifluoromethoxy)benzyl)oxy) 0 C-0401 H H H H H 2-((4-(trifluoromethoxy)benzyl)oxy) 0 C-0402 H H H H H 3-((4-(trifluoromethoxy)benzyl)oxy) 0 C-0403 H H H H H 4-((4-(trifluoromethoxy)benzyl)oxy) 0 C-0404 H H H H H 2-((2-(methylthio)benzyl)oxy) 0 C-0405 H H H H H 3-((2-(methylthio)benzyl)oxy) 0 C-0406 H H H H H 4-((2-(methylthio)benzyl)oxy) 0 C-0407 H H H H H 2-((3-(methylthio)benzyl)oxy) 0 C-0408 H H H H H 3-((3-(methylthio)benzyl)oxy) 0 C-0409 H H H H H 4-((3-(methylthio)benzyl)oxy) 0 C-0410 H H H H H 2-((4-(methylthio)benzyl)oxy) 0 C-0411 H H H H H 3-((4-(methylthio)benzyl)oxy) 0 C-0412 H H H H H 4-((4-(methylthio)benzyl)oxy) 0 C-0413 H H H H H 2-((2-(methylsulfinyl)benzyl)oxy) 0 C-0414 H H H H H 3-((2-(methylsulfinyl)benzyl)oxy) 0 C-0415 H H H H H 4-((2-(methylsulfinyl)benzyl)oxy) 0 C-0416 H H H H H 2-((3-(methylsulfinyl)benzyl)oxy) 0 C-0417 H H H H H 3-((3-(methylsulfinyl)benzyl)oxy) 0 C-0418 H H H H H 4-((3-(methylsulfinyl)benzyl)oxy) 0 C-0419 H H H H H 2-((4-(methylsulfinyl)benzyl)oxy) 0 C-0420 H H H H H 3-((4-(methylsulfinyl)benzyl)oxy) 0 C-0421 H H H H H 4-((4-(methylsulfinyl)benzyl)oxy) 0 C-0422 H H H H H 2-((2-(methylsulfonyl)benzyl)oxy) 0 C-0423 H H H H H 3-((2-(methylsulfonyl)benzyl)oxy) 0 C-0424 H H H H H 4-((2-(methylsulfonyl)benzyl)oxy) 0 C-0425 H H H H H 2-((3-(methylsulfonyl)benzyl)oxy) 0 C-0426 H H H H H 3-((3-(methylsulfonyl)benzyl)oxy) 0 C-0427 H H H H H 4-((3-(methylsulfonyl)benzyl)oxy) 0 C-0428 H H H H H 2-((4-(methylsulfonyl)benzyl)oxy) 0 C-0429 H H H H H 3-((4-(methylsulfonyl)benzyl)oxy) 0 C-0430 H H H H H 4-((4-(methylsulfonyl)benzyl)oxy) 0 C-0431 H H H H H 2-((2-(trifluoromethylthio)benzyl)oxy) 0 C-0432 H H H H H 3-((2-(trifluoromethylthio)benzyl)oxy) 0 C-0433 H H H H H 4-((2-(trifluoromethylthio)benzyl)oxy) 0 C-0434 H H H H H 2-((3-(trifluoromethylthio)benzyl)oxy) 0 C-0435 H H H H H 3-((3-(trifluoromethylthio)benzyl)oxy) 0 C-0436 H H H H H 4-((3-(trifluoromethylthio)benzyl)oxy) 0 C-0437 H H H H H 2-((4-(trifluoromethylthio)benzyl)oxy) 0 C-0438 H H H H H 3-((4-(trifluoromethylthio)benzyl)oxy) 0 C-0439 H H H H H 4-((4-(trifluoromethylthio)benzyl)oxy) 0 C-0440 H H H H H 2-((2- 0 (trifluoromethylsulfinyl)benzyl)oxy) C-0441 H H H H H 3-((2- 0 (trifluoromethylsulfinyl)benzyl)oxy) C-0442 H H H H H 4-((2- 0 (trifluoromethylsulfinyl)benzyl)oxy) C-0443 H H H H H 2-((3- 0 (trifluoromethylsulfinyl)benzyl)oxy)
(304) TABLE-US-00203 TABLE 203 com- pound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0444 H H H H H 3-((3- 0 (trifluoromethylsulfinyl)benzyl)oxy) C-0445 H H H H H 4-((3- 0 (trifluoromethylsulfinyl)benzyl)oxy) C-0446 H H H H H 2-((4- 0 (trifluoromethylsulfinyl)benzyl)oxy) C-0447 H H H H H 3-((4- 0 (trifluoromethylsulfinyl)benzyl)oxy) C-0448 H H H H H 4-((4- 0 (trifluoromethylsulfinyl)benzyl)oxy) C-0449 H H H H H 2-((2- 0 (trifluoromethylsulfonyl)benzyl)oxy) C-0450 H H H H H 3-((2- 0 (trifluoromethylsulfonyl)benzyl)oxy) C-0451 H H H H H 4-((2- 0 (trifluoromethylsulfonyl)benzyl)oxy) C-0452 H H H H H 2-((3- 0 (trifluoromethylsulfonyl)benzyl)oxy) C-0453 H H H H H 3-((3- 0 (trifluoromethysulfonyl)benzyl)oxy) C-0454 H H H H H 4-((3- 0 (trifluoromethylsulfonyl)benzyl)oxy) C-0455 H H H H H 2-((4- 0 (trifluoromethylsulfonyl)benzyl)oxy) C-0456 H H H H H 3-((4- 0 (trifluoromethylsulfonyl)benzyl)oxy) C-0457 H H H H H 4-((4- 0 (trifluoromethylsulfonyl)benzyl)oxy) C-0458 H H H H H 2-((2-aminobenzyl)oxy) 0 C-0459 H H H H H 3-((2-aminobenzyl)oxy) 0 C-0460 H H H H H 4-((2-aminobenzyl)oxy) 0 C-0461 H H H H H 2-((3-aminobenzyl)oxy) 0 C-0462 H H H H H 3-((3-aminobenzyl)oxy) 0 C-0463 H H H H H 4-((3-aminobenzyl)oxy) 0 C-0464 H H H H H 2-((4-aminobenzyl)oxy) 0 C-0465 H H H H H 3-((4-aminobenzyl)oxy) 0 C-0466 H H H H H 4-((4-aminobenzyl)oxy) 0 C-0467 H H H H H 2-((2-(methylamino)benzyl)oxy) 0 C-0468 H H H H H 3-((2-(methylamino)benzyl)oxy) 0 C-0469 H H H H H 4-((2-(methylamino)benzyl)oxy) 0 C-0470 H H H H H 2-((3-(methylamino)benzyl)oxy) 0 C-0471 H H H H H 3-((3-(methylamino)benzyl)oxy) 0 C-0472 H H H H H 4-((3-(methylamino)benzyl)oxy) 0 C-0473 H H H H H 2-((4-(methylamino)benzyl)oxy) 0 C-0474 H H H H H 3-((4-(methylamino)benzyl)oxy) 0 C-0475 H H H H H 4-((4-(methylamino)benzyl)oxy) 0 C-0476 H H H H H 2-((2-(dimethylamino)benzyl)oxy) 0 C-0477 H H H H H 3-((2-(dimethylamino)benzyl)oxy) 0 C-0478 H H H H H 4-((2-(dimethylamino)benzyl)oxy) 0 C-0479 H H H H H 2-((3-(dimethylamino)benzyl)oxy) 0 C-0480 H H H H H 3-((3-(dimethylamino)benzyl)oxy) 0 C-0481 H H H H H 4-((3-(dimethylamino)benzyl)oxy) 0 C-0482 H H H H H 2-((4-(dimethylamino)benzyl)oxy) 0 C-0483 H H H H H 3-((4-(dimethylamino)benzyl)oxy) 0 C-0484 H H H H H 4-((4-(dimethylamino)benzyl)oxy) 0 C-0485 H H H H H 2-((2-cyanobenzyl)oxy) 0 C-0486 H H H H H 3-((2-cyanobenzyl)oxy) 0 C-0487 H H H H H 4-((2-cyanobenzyl)oxy) 0 C-0488 H H H H H 2-((3-cyanobenzyl)oxy) 0 C-0489 H H H H H 3-((3-cyanobenzyl)oxy) 0 C-0490 H H H H H 4-((3-cyanobenzyl)oxy) 0 C-0491 H H H H H 2-((4-cyanobenzyl)oxy) 0 C-0492 H H H H H 3-((4-cyanobenzyl)oxy) 0 C-0493 H H H H H 4-((4-cyanobenzyl)oxy) 0 C-0494 H H H H H 2-((2-nitrobenzyl)oxy) 0 C-0495 H H H H H 3-((2-nitrobenzyl)oxy) 0 C-0496 H H H H H 4-((2-nitrobenzyl)oxy) 0 C-0497 H H H H H 2-((3-nitrobenzyl)oxy) 0 C-0498 H H H H H 3-((3-nitrobenzyl)oxy) 0 C-0499 H H H H H 4-((3-nitrobenzyl)oxy) 0
(305) TABLE-US-00204 TABLE 204 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0500 H H H H H 2-((4-nitrobenzyl)oxy) 0 C-0501 H H H H H 3-((4-nitrobenzyl)oxy) 0 C-0502 H H H H H 4-((4-nitrobenzyl)oxy) 0 C-0503 H H H H H 2-NH.sub.2 0 C-0504 H H H H H 3-NH.sub.2 0 C-0505 H H H H H 4-NH.sub.2 0 C-0506 H H H H H 2-NHMe 0 C-0507 H H H H H 3-NHMe 0 C-0508 H H H H H 4-NHMe 0 C-0509 H H H H H 2-NHEt 0 C-0510 H H H H H 3-NHEt 0 C-0511 H H H H H 4-NHEt 0 C-0512 H H H H H 2-N(Me).sub.2 0 C-0513 H H H H H 3-N(Me).sub.2 0 C-0514 H H H H H 4-N(Me).sub.2 0 C-0515 H H H H H 2-N(Et).sub.2 0 C-0516 H H H H H 3-N(Et).sub.2 0 C-0517 H H H H H 4-N(Et).sub.2 0 C-0518 H H H H H 2-CHO 0 C-0519 H H H H H 3-CHO 0 C-0520 H H H H H 4-CHO 0 C-0521 H H H H H 2-C(?O)OH 0 C-0522 H H H H H 3-C(?O)OH 0 C-0523 H H H H H 4-C(?O)OH 0 C-0524 H H H H H 2-(1,3-dioxolan-2-yl) 0 C-0525 H H H H H 3-(1,3-dioxolan-2-yl) 0 C-0526 H H H H H 4-(1,3-dioxolan-2-yl) 0 C-0527 H H H H H 2-(1,3-dioxan-2-yl) 0 C-0528 H H H H H 3-(1,3-dioxan-2-yl) 0 C-0529 H H H H H 4-(1,3-dioxan-2-yl) 0 C-0530 H H H H H 2-(1H-imidazol-2-yl) 0 C-0531 H H H H H 3-(1H-imidazol-2-yl) 0 C-0532 H H H H H 4-(1H-imidazol-2-yl) 0 C-0533 H H H H H 2-(thiazol-2-yl) 0 C-0534 H H H H H 3-(thiazol-2-yl) 0 C-0535 H H H H H 4-(thiazol-2-yl) 0 C-0536 H H H H H 2-(oxazol-2-yl) 0 C-0537 H H H H H 3-(oxazol-2-yl) 0 C-0538 H H H H H 4-(oxazo-2-yl) 0 C-0539 H H H H H 2-CH?NOH 0 C-0540 H H H H H 3-CH?NOH 0 C-0541 H H H H H 4-CH?NOH 0 C-0542 H H H H H 2-CH?NOMe 0 C-0543 H H H H H 3-CH?NOMe 0 C-0544 H H H H H 4-CH?NOMe 0 C-0545 H H H H H 2-(4,5-dihydro-3-isoxazolyl) 0 C-0546 H H H H H 3-(4,5-dihydro-3-isoxazolyl) 0 C-0547 H H H H H 4-(4,5-dihydro-3-isoxazolyl) 0 C-0548 H H H H H 2-CN 0 C-0549 H H H H H 3-CN 0 C-0550 H H H H H 4-CN 0 C-0551 H H H H H 2-NO.sub.2 0 C-0552 H H H H H 3-NO.sub.2 0 C-0553 H H H H H 4-NO.sub.2 0 C-0554 H H H H H 2,3-F.sub.2 0 C-0555 H H H H H 2,4-F.sub.2 0
(306) TABLE-US-00205 TABLE 205 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0556 H H H H H 2,5-F.sub.2 0 C-0557 H H H H H 2,6-F.sub.2 0 C-0558 H H H H H 3,4-F.sub.2 0 C-0559 H H H H H 3,5-F.sub.2 0 C-0560 H H H H H 2-F,3-Cl 0 C-0561 H H H H H 2-F,4-Cl 0 C-0562 H H H H H 2-F,5-Cl 0 C-0563 H H H H H 2-F,6-Cl 0 C-0564 H H H H H 3-F,2-Cl 0 C-0565 H H H H H 3-F,4-Cl 0 C-0566 H H H H H 3-F,5-Cl 0 C-0567 H H H H H 3-F,6-Cl 0 C-0568 H H H H H 4-F,2-Cl 0 C-0569 H H H H H 4-F,3-Cl 0 C-0570 H H H H H 2-F,3-Me 0 C-0571 H H H H H 2-F,4-Me 0 C-0572 H H H H H 2-F,5-Me 0 C-0573 H H H H H 2-F,6-Me 0 C-0574 H H H H H 3-F,2-Me 0 C-0575 H H H H H 3-F,4-Me 0 C-0576 H H H H H 3-F,5-Me 0 C-0577 H H H H H 3-F,6-Me 0 C-0578 H H H H H 4-F,2-Me 0 C-0579 H H H H H 4-F,3-Me 0 C-0580 H H H H H 2-F,3-CF.sub.3 0 C-0581 H H H H H 2-F,4-CF.sub.3 0 C-0582 H H H H H 2-F,5-CF.sub.3 0 C-0583 H H H H H 2-F,6-CF.sub.3 0 C-0584 H H H H H 3-F,2-CF.sub.3 0 C-0585 H H H H H 3-F,4-CF.sub.3 0 C-0586 H H H H H 3-F,5-CF.sub.3 0 C-0587 H H H H H 3-F,6-CF.sub.3 0 C-0588 H H H H H 4-F,2-CF.sub.3 0 C-0589 H H H H H 4-F,3-CF.sub.3 0 C-0590 H H H H H 2-F,3-OMe 0 C-0591 H H H H H 2-F,4-OMe 0 C-0592 H H H H H 2-F,5-OMe 0 C-0593 H H H H H 2-F,6-OMe 0 C-0594 H H H H H 3-F,2-OMe 0 C-0595 H H H H H 3-F,4-OMe 0 C-0596 H H H H H 3-F,5-OMe 0 C-0597 H H H H H 3-F,6-OMe 0 C-0598 H H H H H 4-F,2-OMe 0 C-0599 H H H H H 4-F,3-OMe 0 C-0600 H H H H H 2,3-Cl.sub.2 0 C-0601 H H H H H 2,4-Cl.sub.2 0 C-0602 H H H H H 2,5-Cl.sub.2 0 C-0603 H H H H H 2,6-Cl.sub.2 0 C-0604 H H H H H 3,4-Cl.sub.2 0 C-0605 H H H H H 3,5-Cl.sub.2 0 C-0606 H H H H H 2-Cl,3-Me 0 C-0607 H H H H H 2-Cl,4-Me 0 C-0608 H H H H H 2-Cl,5-Me 0 C-0609 H H H H H 2-Cl,6-Me 0 C-0610 H H H H H 3-Cl,2-Me 0 C-0611 H H H H H 3-Cl,4-Me 0
(307) TABLE-US-00206 TABLE 206 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0612 H H H H H 3-Cl,5-Me 0 C-0613 H H H H H 3-Cl,6-Me 0 C-0614 H H H H H 4-Cl,2-Me 0 C-0615 H H H H H 4-Cl,3-Me 0 C-0616 H H H H H 2-Cl,3-CF.sub.3 0 C-0617 H H H H H 2-Cl,4-CF.sub.3 0 C-0618 H H H H H 2-Cl,5-CF 0 C-0619 H H H H H 2-Cl,6-CF.sub.3 0 C-0620 H H H H H 3-Cl,2-CF.sub.3 0 C-0621 H H H H H 3-Cl,4-CF.sub.3 0 C-0622 H H H H H 3-Cl,5-CF.sub.3 0 C-0623 H H H H H 3-Cl,6-CF.sub.3 0 C-0624 H H H H H 4-Cl,2-CF.sub.3 0 C-0625 H H H H H 4-Cl,3-CF.sub.3 0 C-0626 H H H H H 2-Cl,3-OMe 0 C-0627 H H H H H 2-Cl,4-OMe 0 C-0628 H H H H H 2-Cl,5-OMe 0 C-0629 H H H H H 2-Cl,6-OMe 0 C-0630 H H H H H 3-Cl,2-OMe 0 C-0631 H H H H H 3-Cl,4-OMe 0 C-0632 H H H H H 3-Cl,5-OMe 0 C-0633 H H H H H 3-Cl,6-OMe 0 C-0634 H H H H H 4-Cl,2-OMe 0 C-0635 H H H H H 4-Cl,3-OMe 0 C-0636 H H H H H 2,3-Me.sub.2 0 C-0637 H H H H H 2,4-Me.sub.2 0 C-0638 H H H H H 2,5-Me.sub.2 0 C-0639 H H H H H 2,6-Me.sub.2 0 C-0640 H H H H H 3,4-Me.sub.2 0 C-0641 H H H H H 3,5-Me.sub.2 0 C-0642 H H H H H 2-Me,3-CF.sub.3 0 C-0643 H H H H H 2-Me,4-CF.sub.3 0 C-0644 H H H H H 2-Me,5-CF.sub.3 0 C-0645 H H H H H 2-Me,6-CF.sub.3 0 C-0646 H H H H H 3-Me,2-CF.sub.3 0 C-0647 H H H H H 3-Me,4-CF.sub.3 0 C-0648 H H H H H 3-Me,5-CF.sub.3 0 C-0649 H H H H H 3-Me,6-CF.sub.3 0 C-0650 H H H H H 4-Me,2-CF.sub.3 0 C-0651 H H H H H 4-Me,3-CF.sub.3 0 C-0652 H H H H H 2-Me,3-OMe 0 C-0653 H H H H H 2-Me,4-OMe 0 C-0654 H H H H H 2-Me,5-OMe 0 C-0655 H H H H H 2-Me,6-OMe 0 C-0656 H H H H H 3-Me,2-OMe 0 C-0657 H H H H H 3-Me,4-OMe 0 C-0658 H H H H H 3-Me,5-OMe 0 C-0659 H H H H H 3-Me,6-OMe 0 C-0660 H H H H H 4-Me,2-OMe 0 C-0661 H H H H H 4-Me,3-OMe 0 C-0662 H H H H H 2,3-OMe.sub.2 0 C-0663 H H H H H 2,4-OMe.sub.2 0 C-0664 H H H H H 2,5-OMe.sub.2 0 C-0665 H H H H H 2,6-OMe.sub.2 0 C-0666 H H H H H 3,4-OMe.sub.2 0 C-0667 H H H H H 3,5-OMe.sub.2 0
(308) TABLE-US-00207 TABLE 207 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0668 H H H H H 2-OMe,3-CF.sub.3 0 C-0669 H H H H H 2-OMe,4-CF.sub.3 0 C-0670 H H H H H 2-OMe,5-CF.sub.3 0 C-0671 H H H H H 2-OMe,6-CF.sub.3 0 C-0672 H H H H H 3-OMe,2-CF.sub.3 0 C-0673 H H H H H 3-OMe,4-CF.sub.3 0 C-0674 H H H H H 3-OMe,5-CF.sub.3 0 C-0675 H H H H H 3-OMe,6-CF.sub.3 0 C-0676 H H H H H 4-OMe,2-CF.sub.3 0 C-0677 H H H H H 4-OMe,3-CF.sub.3 0 C-0678 H H H H H 2-CHF.sub.2,3-F 0 C-0679 H H H H H 2-CHF.sub.2,4-F 0 C-0680 H H H H H 2-CHF.sub.2,5-F 0 C-0681 H H H H H 2-CHF.sub.2,6-F 0 C-0682 H H H H H 2-CHF.sub.2,3-Me 0 C-0683 H H H H H 2-CHF.sub.2,4-Me 0 C-0684 H H H H H 2-CHF.sub.2,5-Me 0 C-0685 H H H H H 2-CHF.sub.2,6-Me 0 C-0686 H H H H H 2-cyclopropyl,3-F 0 C-0687 H H H H H 2-cyclopropyl,4-F 0 C-0688 H H H H H 2-cyclopropyl,5-F 0 C-0689 H H H H H 2-cyclopropyl,6-F 0 C-0690 H H H H H 2-cyclopropyl,3-Me 0 C-0691 H H H H H 2-cyclopropyl,4-Me 0 C-0692 H H H H H 2-cyclopropyl,5-Me 0 C-0693 H H H H H 2-cyclopropyl,6-Me 0 C-0694 H H H H H 2-ethenyl,3-F 0 C-0695 H H H H H 2-ethenyl,4-F 0 C-0696 H H H H H 2-ethenyl,5-F 0 C-0697 H H H H H 2-ethenyl,6-F 0 C-0698 H H H H H 2-ethenyl,3-Me 0 C-0699 H H H H H 2-ethenyl,4-Me 0 C-0700 H H H H H 2-ethenyl,5-Me 0 C-0701 H H H H H 2-ethenyl,6-Me 0 C-0702 H H H H H 2-OEt,3-F 0 C-0703 H H H H H 2-OEt,4-F 0 C-0704 H H H H H 2-OEt,5-F 0 C-0705 H H H H H 2-OEt,6-F 0 C-0706 H H H H H 2-OEt,3-Cl 0 C-0707 H H H H H 2-OEt,4-Cl 0 C-0708 H H H H H 2-OEt,5-Cl 0 C-0709 H H H H H 2-OEt,6-Cl 0 C-0710 H H H H H 2-OEt,3-Me 0 C-0711 H H H H H 2-OEt,4-Me 0 C-0712 H H H H H 2-OEt,5-Me 0 C-0713 H H H H H 2-OEt,6-Me 0 C-0714 H H H H H 2-OPr,3-F 0 C-0715 H H H H H 2-OPr,4-F 0 C-0716 H H H H H 2-OPr,5-F 0 C-0717 H H H H H 2-OPr,6-F 0 C-0718 H H H H H 2-OPr,3-Me 0 C-0719 H H H H H 2-OPr,4-Me 0 C-0720 H H H H H 2-OPr,5-Me 0 C-0721 H H H H H 2-OPr,6-Me 0 C-0722 H H H H H 2-O(i-Pr),3-F 0 C-0723 H H H H H 2-O(i-Pr),4-F 0
(309) TABLE-US-00208 TABLE 208 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0724 H H H H H 2-O(i-Pr),5-F 0 C-0725 H H H H H 2-O(i-Pr),6-F 0 C-0726 H H H H H 2-O(i-Pr),3-Me 0 C-0727 H H H H H 2-O(i-Pr),4-Me 0 C-0728 H H H H H 2-O(i-Pr),5-Me 0 C-0729 H H H H H 2-O(i-Pr),6-Me 0 C-0730 H H H H H 2-OCF.sub.3,3-F 0 C-0731 H H H H H 2-OCF.sub.3,4-F 0 C-0732 H H H H H 2-OCF.sub.3,5-F 0 C-0733 H H H H H 2-OCF.sub.3,6-F 0 C-0734 H H H H H 2-OCF.sub.3,3-Me 0 C-0735 H H H H H 2-OCF.sub.3,4-Me 0 C-0736 H H H H H 2-OCF.sub.3,5-Me 0 C-0737 H H H H H 2-OCF.sub.3,6-Me 0 C-0738 H H H H H 2-OCHF.sub.2,3-F 0 C-0739 H H H H H 2-OCHF.sub.2,4-F 0 C-0740 H H H H H 2-OCHF.sub.2,5-F 0 C-0741 H H H H H 2-OCHF.sub.2,6-F 0 C-0742 H H H H H 2-OCHF.sub.2,3-Me 0 C-0743 H H H H H 2-OCHF.sub.2,4-Me 0 C-0744 H H H H H 2-OCHF.sub.2,5-Me 0 C-0745 H H H H H 2-OCHF.sub.2,6-Me 0 C-0746 H H H H H 2-(cyclopropyloxy),3-F 0 C-0747 H H H H H 2-(cyclopropyloxy),4-F 0 C-0748 H H H H H 2-(cyclopropyloxy),5-F 0 C-0749 H H H H H 2-(cyclopropyloxy),6-F 0 C-0750 H H H H H 2-(cyclopropyloxy),3-Me 0 C-0751 H H H H H 2-(cyclopropyloxy),4-Me 0 C-0752 H H H H H 2-(cyclopropyloxy),5-Me 0 C-0753 H H H H H 2-(cyclopropyloxy),6-Me 0 C-0754 H H H H H 2-(oxiran-2-yl),3-F 0 C-0755 H H H H H 2-(oxiran-2-yl),4-F 0 C-0756 H H H H H 2-(oxiran-2-yl),5-F 0 C-0757 H H H H H 2-(oxiran-2-yl),6-F 0 C-0758 H H H H H 2-(oxiran-2-yl),3-Me 0 C-0759 H H H H H 2-(oxiran-2-yl),4-Me 0 C-0760 H H H H H 2-(oxiran-2-yl),5-Me 0 C-0761 H H H H H 2-(oxiran-2-yl),6-Me 0 C-0762 H H H H H 2-(oxiran-2-ylmethyl),3-F 0 C-0763 H H H H H 2-(oxiran-2-ylmethyl),4-F 0 C-0764 H H H H H 2-(oxiran-2-ylmethyl),5-F 0 C-0765 H H H H H 2-(oxiran-2-ylmethyl),6-F 0 C-0766 H H H H H 2-(oxiran-2-ylmethyl),3-Me 0 C-0767 H H H H H 2-(oxiran-2-ylmethyl),4-Me 0 C-0768 H H H H H 2-(oxiran-2-ylmethyl),5-Me 0 C-0769 H H H H H 2-(oxiran-2-ylmethyl),6-Me 0 C-0770 H H H H H 2-SMe,3-F 0 C-0771 H H H H H 2-SMe,4-F 0 C-0772 H H H H H 2-SMe,5-F 0 C-0773 H H H H H 2-SMe,6-F 0 C-0774 H H H H H 2-SMe,3-Me 0 C-0775 H H H H H 2-SMe,4-Me 0 C-0776 H H H H H 2-SMe,5-Me 0 C-0777 H H H H H 2-SMe,6-Me 0 C-0778 H H H H H 2-SEt,3-F 0 C-0779 H H H H H 2-SEt,4-F 0
(310) TABLE-US-00209 TABLE 209 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0780 H H H H H 2-SEt,5-F 0 C-0781 H H H H H 2-SEt,6-F 0 C-0782 H H H H H 2-SEt,3-Me 0 C-0783 H H H H H 2-SEt,4-Me 0 C-0784 H H H H H 2-SEt,5-Me 0 C-0785 H H H H H 2-SEt,6-Me 0 C-0786 H H H H H 2-S(?O)Me,3-F 0 C-0787 H H H H H 2-S(?O)Me,4-F 0 C-0788 H H H H H 2-S(?O)Me,5-F 0 C-0789 H H H H H 2-S(?O)Me,6-F 0 C-0790 H H H H H 3-S(?O)Me,2-F 0 C-0791 H H H H H 3-S(?O)Me,4-F 0 C-0792 H H H H H 3-S(?O)Me,5-F 0 C-0793 H H H H H 3-S(?O)Me,6-F 0 C-0794 H H H H H 2-S(?O)Me,3-Me 0 C-0795 H H H H H 2-S(?O)Me,4-Me 0 C-0796 H H H H H 2-S(?O)Me,5-Me 0 C-0797 H H H H H 2-S(?O)Me,6-Me 0 C-0798 H H H H H 3-S(?O)Me,2-Me 0 C-0799 H H H H H 3-S(?O)Me,4-Me 0 C-0800 H H H H H 3-S(?O)Me,5-Me 0 C-0801 H H H H H 3-S(?O)Me,6-Me 0 C-0802 H H H H H 2-S(?O).sub.2Me,3-F 0 C-0803 H H H H H 2-S(?O).sub.2Me,4-F 0 C-0804 H H H H H 2-S(?O).sub.2Me,5-F 0 C-0805 H H H H H 2-S(?O).sub.2Me,6-F 0 C-0806 H H H H H 2-S(?O).sub.2Me,3-Me 0 C-0807 H H H H H 2-S(?O).sub.2Me,4-Me 0 C-0808 H H H H H 2-S(?O).sub.2Me,5-Me 0 C-0809 H H H H H 2-S(?O).sub.2Me,6-Me 0 C-0810 H H H H H 2-SCF.sub.3,3-F 0 C-0811 H H H H H 2-SCF.sub.3,4-F 0 C-0812 H H H H H 2-SCF.sub.3,5-F 0 C-0813 H H H H H 2-SCF.sub.3,6-F 0 C-0814 H H H H H 2-SCF.sub.3,3-Me 0 C-0815 H H H H H 2-SCF.sub.3,4-Me 0 C-0816 H H H H H 2-SCF.sub.3,5-Me 0 C-0817 H H H H H 2-SCF.sub.3,6-Me 0 C-0818 H H H H H 2-S(?O)CF.sub.3,3-F 0 C-0819 H H H H H 2-S(?O)CF.sub.3,4-F 0 C-0820 H H H H H 2-S(?O)CF.sub.3,5-F 0 C-0821 H H H H H 2-S(?O)CF.sub.3,6-F 0 C-0822 H H H H H 2-S(?O)CF.sub.3,3-Me 0 C-0823 H H H H H 2-S(?O)CF.sub.3,4-Me 0 C-0824 H H H H H 2-S(?O)CF.sub.3,5-Me 0 C-0825 H H H H H 2-S(?O)CF.sub.3,6-Me 0 C-0826 H H H H H 2-S(?O).sub.2CF.sub.3,3-F 0 C-0827 H H H H H 2-S(?O).sub.2CF.sub.3,4-F 0 C-0828 H H H H H 2-S(?O).sub.2CF.sub.3,5-F 0 C-0829 H H H H H 2-S(?O).sub.2CF.sub.3,6-F 0 C-0830 H H H H H 2-S(?O).sub.2CF.sub.3,3-Me 0 C-0831 H H H H H 2-S(?O).sub.2CF.sub.3,4-Me 0 C-0832 H H H H H 2-S(?O).sub.2CF.sub.3,5-Me 0 C-0833 H H H H H 2-S(?O).sub.2CF.sub.3,6-Me 0 C-0834 H H H H H 2-(cyclopropylthio),3-F 0 C-0835 H H H H H 2-(cyclopropylthio),4-F 0
(311) TABLE-US-00210 TABLE 210 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0836 H H H H H 2-(cyclopropylthio),5-F 0 C-0837 H H H H H 2-(cyclopropylthio),6-F 0 C-0838 H H H H H 2-(cyclopropylthio),3-Me 0 C-0839 H H H H H 2-(cyclopropylthio),4-Me 0 C-0840 H H H H H 2-(cyclopropylthio),5-Me 0 C-0841 H H H H H 2-(cyclopropylthio),6-Me 0 C-0842 H H H H H 2-C(?O)Me,3-F 0 C-0843 H H H H H 2-C(?O)Me,4-F 0 C-0844 H H H H H 2-C(?O)Me,5-F 0 C-0845 H H H H H 2-C(?O)Me,6-F 0 C-0846 H H H H H 2-C(?O)Me,3-Me 0 C-0847 H H H H H 2-C(?O)Me,4-Me 0 C-0848 H H H H H 2-C(?O)Me,5-Me 0 C-0849 H H H H H 2-C(?O)Me,6-Me 0 C-0850 H H H H H 3-C(?O)Me,2-F 0 C-0851 H H H H H 3-C(?O)Me,4-F 0 C-0852 H H H H H 3-C(?O)Me,5-F 0 C-0853 H H H H H 3-C(?O)Me,6-F 0 C-0854 H H H H H 3-C(?O)Me,2-Me 0 C-0855 H H H H H 3-C(?O)Me,4-Me 0 C-0856 H H H H H 3-C(?O)Me,5-Me 0 C-0857 H H H H H 3-C(?O)Me,6-Me 0 C-0858 H H H H H 2-C(?O)OMe,3-F 0 C-0859 H H H H H 2-C(?O)OMe,4-F 0 C-0860 H H H H H 2-C(?O)OMe,5-F 0 C-0861 H H H H H 2-C(?O)OMe,6-F 0 C-0862 H H H H H 2-C(?O)OMe,3-Me 0 C-0863 H H H H H 2-C(?O)OMe,4-Me 0 C-0864 H H H H H 2-C(?O)OMe,5-Me 0 C-0865 H H H H H 2-C(?O)OMe,6-Me 0 C-0866 H H H H H 2-C(?O)OEt,3-F 0 C-0867 H H H H H 2-C(?O)OEt,4-F 0 C-0868 H H H H H 2-C(?O)OEt,5-F 0 C-0869 H H H H H 2-C(?O)OEt,6-F 0 C-0870 H H H H H 2-C(?O)OEt,3-Me 0 C-0871 H H H H H 2-C(?O)OEt,4-Me 0 C-0872 H H H H H 2-C(?O)OEt,5-Me 0 C-0873 H H H H H 2-C(?O)OEt,6-Me 0 C-0874 H H H H H 2-C(?O)NH.sub.2,3-F 0 C-0875 H H H H H 2-C(?O)NH.sub.2,4-F 0 C-0876 H H H H H 2-C(?O)NH.sub.2,5-F 0 C-0877 H H H H H 2-C(?O)NH.sub.2,6-F 0 C-0878 H H H H H 2-C(?O)NH.sub.2,3-Me 0 C-0879 H H H H H 2-C(?O)NH.sub.2,4-Me 0 C-0880 H H H H H 2-C(?O)NH.sub.2,5-Me 0 C-0881 H H H H H 2-C(?O)NH.sub.2,6-Me 0 C-0882 H H H H H 2-C(?O)NHMe,3-F 0 C-0883 H H H H H 2-C(?O)NHMe,4-F 0 C-0884 H H H H H 2-C(?O)NHMe,5-F 0 C-0885 H H H H H 2-C(?O)NHMe,6-F 0 C-0886 H H H H H 2-C(?O)NHMe,3-Me 0 C-0887 H H H H H 2-C(?O)NHMe,4-Me 0 C-0888 H H H H H 2-C(?O)NHMe,5-Me 0 C-0889 H H H H H 2-C(?O)NHMe,6-Me 0 C-0890 H H H H H 2-C(?O)NMe.sub.2,3-F 0 C-0891 H H H H H 2-C(?O)NMe.sub.2,4-F 0
(312) TABLE-US-00211 TABLE 211 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0892 H H H H H 2-C(?O)NMe.sub.2,5-F 0 C-0893 H H H H H 2-C(?O)NMe.sub.2,6-F 0 C-0894 H H H H H 2-C(?O)NMe.sub.2,3-Me 0 C-0895 H H H H H 2-C(?O)NMe.sub.2,4-Me 0 C-0896 H H H H H 2-C(?O)NMe.sub.2,5-Me 0 C-0897 H H H H H 2-C(?O)NMe.sub.2,6-Me 0 C-0898 H H H H H 2-CH.sub.2OH,3-F 0 C-0899 H H H H H 2-CH.sub.2OH,4-F 0 C-0900 H H H H H 2-CH.sub.2OH,5-F 0 C-0901 H H H H H 2-CH.sub.2OH,6-F 0 C-0902 H H H H H 2-CH.sub.2OH,3-Me 0 C-0903 H H H H H 2-CH.sub.2OH,4-Me 0 C-0904 H H H H H 2-CH.sub.2OH,5-Me 0 C-0905 H H H H H 2-CH.sub.2OH,6-Me 0 C-0906 H H H H H 2-CH.sub.2OCH.sub.3,3-F 0 C-0907 H H H H H 2-CH.sub.2OCH.sub.3,4-F 0 C-0908 H H H H H 2-CH.sub.2OCH.sub.3,5-F 0 C-0909 H H H H H 2-CH.sub.2OCH.sub.3,6-F 0 C-0910 H H H H H 2-CH.sub.2OCH.sub.3,3-Me 0 C-0911 H H H H H 2-CH.sub.2OCH.sub.3,4-Me 0 C-0912 H H H H H 2-CH.sub.2OCH.sub.3,5-Me 0 C-0913 H H H H H 2-CH.sub.2OCH.sub.3,6-Me 0 C-0914 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,3-F 0 C-0915 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,4-F 0 C-0916 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,5-F 0 C-0917 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-F 0 C-0918 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,3-Me 0 C-0919 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,4-Me 0 C-0920 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,5-Me 0 C-0921 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Me 0 C-0922 H H H H H 2-OC(?O)CH.sub.3,3-F 0 C-0923 H H H H H 2-OC(?O)CH.sub.3,4-F 0 C-0924 H H H H H 2-OC(?O)CH.sub.3,5-F 0 C-0925 H H H H H 2-OC(?O)CH.sub.3,6-F 0 C-0926 H H H H H 2-OC(?O)CH.sub.3,3-Me 0 C-0927 H H H H H 2-OC(?O)CH.sub.3,4-Me 0 C-0928 H H H H H 2-OC(?O)CH.sub.3,5-Me 0 C-0929 H H H H H 2-OC(?O)CH.sub.3,6-Me 0 C-0930 H H H H H 2-OS(?O).sub.2CH.sub.3,3-F 0 C-0931 H H H H H 2-OS(?O).sub.2CH.sub.3,4-F 0 C-0932 H H H H H 2-OS(?O).sub.2CH.sub.3,5-F 0 C-0933 H H H H H 2-OS(?O).sub.2CH.sub.3,6-F 0 C-0934 H H H H H 2-OS(?O).sub.2CH.sub.3,3-Me 0 C-0935 H H H H H 2-OS(?O).sub.2CH.sub.3,4-Me 0 C-0936 H H H H H 2-OS(?O).sub.2CH.sub.3,5-Me 0 C-0937 H H H H H 2-OS(?O).sub.2CH.sub.3,6-Me 0 C-0938 H H H H H 2-CH.sub.2SCH.sub.3,3-F 0 C-0939 H H H H H 2-CH.sub.2SCH.sub.3,4-F 0 C-0940 H H H H H 2-CH.sub.2SCH.sub.3,5-F 0 C-0941 H H H H H 2-CH.sub.2SCH.sub.3,6-F 0 C-0942 H H H H H 2-CH.sub.2SCH.sub.3,3-Me 0 C-0943 H H H H H 2-CH.sub.2SCH.sub.3,4-Me 0 C-0944 H H H H H 2-CH.sub.2SCH.sub.3,5-Me 0 C-0945 H H H H H 2-CH.sub.2SCH.sub.3,6-Me 0 C-0946 H H H H H 2-CH.sub.2SCF.sub.3,3-F 0 C-0947 H H H H H 2-CH.sub.2SCF.sub.3,4-F 0
(313) TABLE-US-00212 TABLE 212 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-0948 H H H H H 2-CH.sub.2SCF.sub.3,5-F 0 C-0949 H H H H H 2-CH.sub.2SCF.sub.3,6-F 0 C-0950 H H H H H 2-CH.sub.2SCF.sub.3,3-Me 0 C-0951 H H H H H 2-CH.sub.2SCF.sub.3,4-Me 0 C-0952 H H H H H 2-CH.sub.2SCF.sub.3,5-Me 0 C-0953 H H H H H 2-CH.sub.2SCF.sub.3,6-Me 0 C-0954 H H H H H 2-(benzyloxy),3-F 0 C-0955 H H H H H 2-(benzyloxy),4-F 0 C-0956 H H H H H 2-(benzyloxy),5-F 0 C-0957 H H H H H 2-(benzyloxy),6-F 0 C-0958 H H H H H 2-(benzyloxy),3-Me 0 C-0959 H H H H H 2-(benzyloxy),4-Me 0 C-0960 H H H H H 2-(benzyloxy),5-Me 0 C-0961 H H H H H 2-(benzyloxy),6-Me 0 C-0962 H H H H H 2-NH.sub.2,3-F 0 C-0963 H H H H H 2-NH.sub.2,4-F 0 C-0964 H H H H H 2-NH.sub.2,5-F 0 C-0965 H H H H H 2-NH.sub.2,6-F 0 C-0966 H H H H H 2-NH.sub.2,3-Me 0 C-0967 H H H H H 2-NH.sub.2,4-Me 0 C-0968 H H H H H 2-NH.sub.2,5-Me 0 C-0969 H H H H H 2-NH.sub.2,6-Me 0 C-0970 H H H H H 2-NHMe,3-F 0 C-0971 H H H H H 2-NHMe,4-F 0 C-0972 H H H H H 2-NHMe,5-F 0 C-0973 H H H H H 2-NHMe,6-F 0 C-0974 H H H H H 2-NHMe,3-Me 0 C-0975 H H H H H 2-NHMe,4-Me 0 C-0976 H H H H H 2-NHMe,5-Me 0 C-0977 H H H H H 2-NHMe,6-Me 0 C-0978 H H H H H 2-NHEt,3-F 0 C-0979 H H H H H 2-NHEt,4-F 0 C-0980 H H H H H 2-NHEt,5-F 0 C-0981 H H H H H 2-NHEt,6-F 0 C-0982 H H H H H 2-NHEt,3-Me 0 C-0983 H H H H H 2-NHEt,4-Me 0 C-0984 H H H H H 2-NHEt,5-Me 0 C-0985 H H H H H 2-NHEt,6-Me 0 C-0986 H H H H H 2-NMe.sub.2,3-F 0 C-0987 H H H H H 2-NMe.sub.2,4-F 0 C-0988 H H H H H 2-NMe.sub.2,5-F 0 C-0989 H H H H H 2-NMe.sub.2,6-F 0 C-0990 H H H H H 2-NMe.sub.2,3-Me 0 C-0991 H H H H H 2-NMe.sub.2,4-Me 0 C-0992 H H H H H 2-NMe.sub.2,5-Me 0 C-0993 H H H H H 2-NMe.sub.2,6-Me 0 C-0994 H H H H H 2-NEt.sub.2,3-F 0 C-0995 H H H H H 2-NEt.sub.2,4-F 0 C-0996 H H H H H 2-NEt.sub.2,5-F 0 C-0997 H H H H H 2-NEt.sub.2,6-F 0 C-0998 H H H H H 2-NEt.sub.2,3-Me 0 C-0999 H H H H H 2-NEt.sub.2,4-Me 0 C-1000 H H H H H 2-NEt.sub.2,5-Me 0 C-1001 H H H H H 2-NEt.sub.2,6-Me 0 C-1002 H H H H H 2-CHO,3-F 0 C-1003 H H H H H 2-CHO,4-F 0
(314) TABLE-US-00213 TABLE 213 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-1004 H H H H H 2-CHO,5-F 0 C-1005 H H H H H 2-CHO,6-F 0 C-1006 H H H H H 2-CHO,3-Me 0 C-1007 H H H H H 2-CHO,4-Me 0 C-1008 H H H H H 2-CHO,5-Me 0 C-1009 H H H H H 2-CHO,6-Me 0 C-1010 H H H H H 2-C(?O)OH,3-F 0 C-1011 H H H H H 2-C(?O)OH,4-F 0 C-1012 H H H H H 2-C(?O)OH,5-F 0 C-1013 H H H H H 2-C(?O)OH,6-F 0 C-1014 H H H H H 2-C(?O)OH,3-Me 0 C-1015 H H H H H 2-C(?O)OH,4-Me 0 C-1016 H H H H H 2-C(?O)OH,5-Me 0 C-1017 H H H H H 2-C(?O)OH,6-Me 0 C-1018 H H H H H 2-(1,3-dioxolan-2-yl),3-F 0 C-1019 H H H H H 2-(1,3-dioxolan-2-yl),4-F 0 C-1020 H H H H H 2-(1,3-dioxolan-2-yl),5-F 0 C-1021 H H H H H 2-(1,3-dioxolan-2-yl),6-F 0 C-1022 H H H H H 2-(1,3-dioxolan-2-yl),3-Me 0 C-1023 H H H H H 2-(1,3-dioxolan-2-yl),4-Me 0 C-1024 H H H H H 2-(1,3-dioxolan-2-yl),5-Me 0 C-1025 H H H H H 2-(1,3-dioxolan-2-yl),6-Me 0 C-1026 H H H H H 2-(1,3-dioxan-2-yl),3-F 0 C-1027 H H H H H 2-(1,3-dioxan-2-yl),4-F 0 C-1028 H H H H H 2-(1,3-dioxan-2-yl),5-F 0 C-1029 H H H H H 2-(1,3-dioxan-2-yl),6-F 0 C-1030 H H H H H 2-(1,3-dioxan-2-yl),3-Me 0 C-1031 H H H H H 2-(1,3-dioxan-2-yl),4-Me 0 C-1032 H H H H H 2-(1,3-dioxan-2-yl),5-Me 0 C-1033 H H H H H 2-(1,3-dioxan-2-yl),6-Me 0 C-1034 H H H H H 2-(thiazol-2-yl),3-F 0 C-1035 H H H H H 2-(thiazol-2-yl),4-F 0 C-1036 H H H H H 2-(thiazol-2-yl),5-F 0 C-1037 H H H H H 2-(thiazol-2-yl),6-F 0 C-1038 H H H H H 2-(thiazol-2-yl),3-Me 0 C-1039 H H H H H 2-(thiazol-2-yl),4-Me 0 C-1040 H H H H H 2-(thiazol-2-yl),5-Me 0 C-1041 H H H H H 2-(thiazol-2-yl),6-Me 0 C-1042 H H H H H 2-(oxazol-2-yl),3-F 0 C-1043 H H H H H 2-(oxazol-2-yl),4-F 0 C-1044 H H H H H 2-(oxazol-2-yl),5-F 0 C-1045 H H H H H 2-(oxazol-2-yl),6-F 0 C-1046 H H H H H 2-(oxazol-2-yl),3-Me 0 C-1047 H H H H H 2-(oxazol-2-yl),4-Me 0 C-1048 H H H H H 2-(oxazol-2-yl),5-Me 0 C-1049 H H H H H 2-(oxazol-2-yl),6-Me 0 C-1050 H H H H H 2-CH?NOH,3-F 0 C-1051 H H H H H 2-CH?NOH,4-F 0 C-1052 H H H H H 2-CH?NOH,5-F 0 C-1053 H H H H H 2-CH?NOH,6-F 0 C-1054 H H H H H 2-CH?NOH,3-Me 0 C-1055 H H H H H 2-CH?NOH,4-Me 0 C-1056 H H H H H 2-CH?NOH,5-Me 0 C-1057 H H H H H 2-CH?NOH,6-Me 0 C-1058 H H H H H 2-CH?NOMe,3-F 0 C-1059 H H H H H 2-CH?NOMe,4-F 0
(315) TABLE-US-00214 TABLE 214 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-1060 H H H H H 2-CH?NOMe,5-F 0 C-1061 H H H H H 2-CH?NOMe,6-F 0 C-1062 H H H H H 2-CH?NOMe,3-Me 0 C-1063 H H H H H 2-CH?NOMe,4-Me 0 C-1064 H H H H H 2-CH?NOMe,5-Me 0 C-1065 H H H H H 2-CH?NOMe,6-Me 0 C-1066 H H H H H 2-CN,3-F 0 C-1067 H H H H H 2-CN,4-F 0 C-1068 H H H H H 2-CN,5-F 0 C-1069 H H H H H 2-CN,6-F 0 C-1070 H H H H H 2-CN,3-Cl 0 C-1071 H H H H H 2-CN,4-Cl 0 C-1072 H H H H H 2-CN,5-Cl 0 C-1073 H H H H H 2-CN,6-Cl 0 C-1074 H H H H H 2-CN,3-Me 0 C-1075 H H H H H 2-CN,4-Me 0 C-1076 H H H H H 2-CN,5-Me 0 C-1077 H H H H H 2-CN,6-Me 0 C-1078 H H H H H 2-CN,3-OMe 0 C-1079 H H H H H 2-CN,4-OMe 0 C-1080 H H H H H 2-CN,5-OMe 0 C-1081 H H H H H 2-CN,6-OMe 0 C-1082 H H H H H 3-CN,2-F 0 C-1083 H H H H H 3-CN,4-F 0 C-1084 H H H H H 3-CN,5-F 0 C-1085 H H H H H 3-CN,6-F 0 C-1086 H H H H H 3-CN,2-Cl 0 C-1087 H H H H H 3-CN,4-Cl 0 C-1088 H H H H H 3-CN,5-Cl 0 C-1089 H H H H H 3-CN,6-Cl 0 C-1090 H H H H H 3-CN,2-Me 0 C-1091 H H H H H 3-CN,4-Me 0 C-1092 H H H H H 3-CN,5-Me 0 C-1093 H H H H H 3-CN,6-Me 0 C-1094 H H H H H 3-CN,2-OMe 0 C-1095 H H H H H 3-CN,4-OMe 0 C-1096 H H H H H 3-CN,5-OMe 0 C-1097 H H H H H 3-CN,6-OMe 0 C-1098 H H H H H 4-CN,2-F 0 C-1099 H H H H H 4-CN,3-F 0 C-1100 H H H H H 4-CN,2-Cl 0 C-1101 H H H H H 4-CN,3-Cl 0 C-1102 H H H H H 4-CN,2-Me 0 C-1103 H H H H H 4-CN,3-Me 0 C-1104 H H H H H 4-CN,2-OMe 0 C-1105 H H H H H 4-CN,3-OMe 0 C-1106 H H H H H 2-NO.sub.2,3-F 0 C-1107 H H H H H 2-NO.sub.2,4-F 0 C-1108 H H H H H 2-NO.sub.2,5-F 0 C-1109 H H H H H 2-NO.sub.2,6-F 0 C-1110 H H H H H 2-NO.sub.2,3-Me 0 C-1111 H H H H H 2-NO.sub.2,4-Me 0 C-1112 H H H H H 2-NO.sub.2,5-Me 0 C-1113 H H H H H 2-NO.sub.2,6-Me 0 C-1114 H H H H H 2-Me,3,4-F.sub.2 0 C-1115 H H H H H 2-Me,3,5-F.sub.2 0
(316) TABLE-US-00215 TABLE 215 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-1116 H H H H H 2-Me,3,6-F.sub.2 0 C-1117 H H H H H 2-Me,4,5-F.sub.2 0 C-1118 H H H H H 2-OMe,3,4-F.sub.2 0 C-1119 H H H H H 2-OMe,3,5-F.sub.2 0 C-1120 H H H H H 2-OMe,3,6-F.sub.2 0 C-1121 H H H H H 2-OMe,4,5-F.sub.2 0 C-1122 H H H H H 2-(CH.sub.2).sub.3-3 0 C-1123 H H H H H 2-(CH.sub.2).sub.4-3 0 C-1124 H H H H H 2-(OCH.sub.2CH.sub.2)-3 0 C-1125 H H H H H 2-(OCH.sub.2CH.sub.2CH.sub.2)-3 0 C-1126 H H H H H 2-(CH.sub.2CH.sub.2O)-3 0 C-1127 H H H H H 2-(CH.sub.2CH.sub.2CH.sub.2O)-3 0 C-1128 H H H H H 3-(CH.sub.2).sub.3-4 0 C-1129 H H H H H 3-(CH.sub.2).sub.4-4 0 C-1130 H H H H H 3-(OCH.sub.2CH.sub.2)-4 0 C-1131 H H H H H 3-(OCH.sub.2CH.sub.2CH.sub.2)-4 0 C-1132 H H H H H 3-(CH.sub.2CH.sub.2O)-4 0 C-1133 H H H H H 3-(CH.sub.2CH.sub.2CH.sub.2O)-4 0 C-1134 H H H H H 2-(OCH.sub.2O)-3 0 C-1135 H H H H H 3-(OCH.sub.2O)-4 0 C-1136 H H H H H 2-(OCH.sub.2CH.sub.2O)-3 0 C-1137 H H H H H 3-(OCH.sub.2CH.sub.2O)-4 0 C-1138 H H H H H 2-(OCF.sub.2O)-3 0 C-1139 H H H H H 3-(OCF.sub.2O)-4 0 C-1140 H H H H H 2-Me,6-Et 0 C-1141 H H H H H 2-CH.sub.2OTBS 0 C-1142 H H H H H 2-cyclopropyl,3-OMe 0 C-1143 H H H H H 2-cyclopropyl,4-OMe 0 C-1144 H H H H H 2-cyclopropyl,5-OMe 0 C-1145 H H H H H 2-cyclopropyl,6-OMe 0 C-1146 H H H H H 2-Me,3-OMe,6-Me 0 C-1147 H H H H H 2-Me,4-OMe,6-Me 0 C-1148 H H H H H 2-OMe,3-Me,6-Me 0 C-1149 H H H H H 2-OMe,5-Me,6-Me 0 C-1150 H H H H H 2-OMe,3-F,6-Me 0 C-1151 H H H H H 2-OMe,5-F,6-Me 0 C-1152 H H H H H 2-OMe,5-Me,6-F 0 C-1153 H H H H H 2-Cl,3-Me,6-F 0 C-1154 H H H H H 2-Cl,5-Me,6-F 0 C-1155 H H H H H 2-Cl,3-OMe,6-F 0 C-1156 H H H H H 2-Cl,5-OMe,6-F 0 C-1157 H H H H H 2-Me,5-Et 0 C-1158 H H H H H 2,6-Et.sub.2 0 C-1159 H H H H H 2-Et,6-F 0 C-1160 H H H H H 2-CH.sub.2OCH.sub.3,6-Cl 0 C-1161 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 C-1162 H H H H H 2-OMe,5-CH?NOMe 0 C-1163 H H H H H 2-CH.sub.2NMe.sub.2 0 C-1164 H H H H H 2-CH.sub.2OCH.sub.3,6-CF.sub.3 0 C-1165 H H F H H 2-Me 0
(317) TABLE-US-00216 TABLE 216
(318) TABLE-US-00217 TABLE 217 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5053 H H H H H 2-CF.sub.2Cl 1 C-5054 H H H H H 3-CF.sub.2Cl 1 C-5055 H H H H H 4-CF.sub.2Cl 1 C-5056 H H H H H 2-CF(CF.sub.3).sub.2 1 C-5057 H H H H H 3-CF(CF.sub.3).sub.2 1 C-5058 H H H H H 4-CF(CF.sub.3).sub.2 1 C-5059 H H H H H 2-cyclopropyl 1 C-5060 H H H H H 3-cyclopropyl 1 C-5061 H H H H H 4-cyclopropyl 1 C-5062 H H H H H 2-cyclobutyl 1 C-5063 H H H H H 3-cyclobutyl 1 C-5064 H H H H H 4-cyclobutyl 1 C-5065 H H H H H 2-cyclopentyl 1 C-5066 H H H H H 3-cyclopentyl 1 C-5067 H H H H H 4-cyclopentyl 1 C-5068 H H H H H 2-(cyclopropylmethyl) 1 C-5069 H H H H H 3-(cyclopropylmethyl) 1 C-5070 H H H H H 4-(cyclopropylmethyl) 1 C-5071 H H H H H 2-(cyclobutylmethyl) 1 C-5072 H H H H H 3-(cyclobutylmethyl) 1 C-5073 H H H H H 4-(cyclobutylmethyl) 1 C-5074 H H H H H 2-(cyclopentylmethyl) 1 C-5075 H H H H H 3-(cyclopentylmethyl) 1 C-5076 H H H H H 4-(cyclopentylmethyl) 1 C-5077 H H H H H 2-(cyclopropylethyl) 1 C-5078 H H H H H 3-(cyclopropylethyl) 1 C-5079 H H H H H 4-(cyclopropylethyl) 1 C-5080 H H H H H 2-(2,2-difluorocyclopropyl) 1 C-5081 H H H H H 3-(2,2-difluorocyclopropyl) 1 C-5082 H H H H H 4-(2,2-difluorocyclopropyl) 1 C-5083 H H H H H 2-(2,2-dichlorocyclopropyl) 1 C-5084 H H H H H 3-(2,2-dichlorocyclopropyl) 1 C-5085 H H H H H 4-(2,2-dichlorocyclopropyl) 1 C-5086 H H H H H 2-ethenyl 1 C-5087 H H H H H 3-ethenyl 1 C-5088 H H H H H 4-ethenyl 1 C-5089 H H H H H 2-allyl 1 C-5090 H H H H H 3-allyl 1 C-5091 H H H H H 4-allyl 1 C-5092 H H H H H 2-(prop-1-en-1-yl) 1 C-5093 H H H H H 3-(prop-1-en-1-yl) 1 C-5094 H H H H H 4-(prop-1-en-1-yl) 1 C-5095 H H H H H 2-(trifluoroethenyl) 1 C-5096 H H H H H 3-(trifluoroethenyl) 1 C-5097 H H H H H 4-(trifluoroethenyl) 1 C-5098 H H H H H 2-(2,2-dichloroethenyl) 1 C-5099 H H H H H 3-(2,2-dichloroethenyl) 1 C-5100 H H H H H 4-(2,2-dichloroethenyl) 1 C-5101 H H H H H 2-ethynyl 1 C-5102 H H H H H 3-ethynyl 1 C-5103 H H H H H 4-ethynyl 1 C-5104 H H H H H 2-(1-propyn-1-yl) 1 C-5105 H H H H H 3-(1-propyn-1-yl) 1 C-5106 H H H H H 4-(1-propyn-1-yl) 1 C-5107 H H H H H 2-(2-propyn-1-yl) 1 C-5108 H H H H H 3-(2-propyn-1-yl) 1 C-5109 H H H H H 4-(2-propyn-1-yl) 1
(319) TABLE-US-00218 TABLE 218 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5110 H H H H H 2-(2-cyclopropylethynyl) 1 C-5111 H H H H H 3-(2-cyclopropylethynyl) 1 C-5112 H H H H H 4-(2-cyclopropylethynyl) 1 C-5113 H H H H H 2-(2-chloroethynyl) 1 C-5114 H H H H H 3-(2-chloroethynyl) 1 C-5115 H H H H H 4-(2-chloroethynyl) 1 C-5116 H H H H H 2-(2-bromoethynyl) 1 C-5117 H H H H H 3-(2-bromoethynyl) 1 C-5118 H H H H H 4-(2-bromoethynyl) 1 C-5119 H H H H H 2-OMe 1 C-5120 H H H H H 3-OMe 1 C-5121 H H H H H 4-OMe 1 C-5122 H H H H H 2-OEt 1 C-5123 H H H H H 3-OEt 1 C-5124 H H H H H 4-OEt 1 C-5125 H H H H H 2-OPr 1 C-5126 H H H H H 3-OPr 1 C-5127 H H H H H 4-OPr 1 C-5128 H H H H H 2-O(i-Pr) 1 C-5129 H H H H H 3-O(i-Pr) 1 C-5130 H H H H H 4-O(i-Pr) 1 C-5131 H H H H H 2-OBu 1 C-5132 H H H H H 3-OBu 1 C-5133 H H H H H 4-OBu 1 C-5134 H H H H H 2-O(s-Bu) 1 C-5135 H H H H H 3-O(s-Bu) 1 C-5136 H H H H H 4-O(s-Bu) 1 C-5137 H H H H H 2-O(i-Bu) 1 C-5138 H H H H H 3-O(i-Bu) 1 C-5139 H H H H H 4-O(i-Bu) 1 C-5140 H H H H H 2-O(t-Bu) 1 C-5141 H H H H H 3-O(t-Bu) 1 C-5142 H H H H H 4-O(t-Bu) 1 C-5143 H H H H H 2-OCF.sub.3 1 C-5144 H H H H H 3-OCF.sub.3 1 C-5145 H H H H H 4-OCF.sub.3 1 C-5146 H H H H H 2-OCHF.sub.2 1 C-5147 H H H H H 3-OCHF.sub.2 1 C-5148 H H H H H 4-OCHF.sub.2 1 C-5149 H H H H H 2-OCH.sub.2CF.sub.3 1 C-5150 H H H H H 3-OCH.sub.2CF.sub.3 1 C-5151 H H H H H 4-OCH.sub.2CF.sub.3 1 C-5152 H H H H H 2-(cyclopropyloxy) 1 C-5153 H H H H H 3-(cyclopropyloxy) 1 C-5154 H H H H H 4-(cyclopropyloxy) 1 C-5155 H H H H H 2-(cyclobutyloxy) 1 C-5156 H H H H H 3-(cyclobutyloxy) 1 C-5157 H H H H H 4-(cyclobutyloxy) 1 C-5158 H H H H H 2-(cyclopentyloxy) 1 C-5159 H H H H H 3-(cyclopentyloxy) 1 C-5160 H H H H H 4-(cyclopentyloxy) 1 C-5161 H H H H H 2-((2,2-dichlorocyclopropyl)oxy) 1 C-5162 H H H H H 3-((2,2-dichlorocyclopropyl)oxy) 1 C-5163 H H H H H 4-((2,2-dichlorocyclopropyl)oxy) 1 C-5164 H H H H H 2-(cyclopropylmethoxy) 1 C-5165 H H H H H 3-(cyclopropylmethoxy) 1 C-5166 H H H H H 4-(cyclopropylmethoxy) 1
(320) TABLE-US-00219 TABLE 219 com- pound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5167 H H H H H 2-((2,2-difluorocyclopropyl)methoxy) 1 C-5168 H H H H H 3-((2,2-difluorocyclopropyl)methoxy) 1 C-5169 H H H H H 4-((2,2-difluorocyclopropyl)methoxy) 1 C-5170 H H H H H 2-(oxiran-2-yl) 1 C-5171 H H H H H 3-(oxiran-2-yl) 1 C-5172 H H H H H 4-(oxiran-2-yl) 1 C-5173 H H H H H 2-(oxiran-2-ylmethyl) 1 C-5174 H H H H H 3-(oxiran-2-ylmethyl) 1 C-5175 H H H H H 4-(oxiran-2-ylmethyl) 1 C-5176 H H H H H 2-SMe 1 C-5177 H H H H H 3-SMe 1 C-5178 H H H H H 4-SMe 1 C-5179 H H H H H 2-SEt 1 C-5180 H H H H H 3-SEt 1 C-5181 H H H H H 4-SEt 1 C-5182 H H H H H 2-S(?O)Me 1 C-5183 H H H H H 3-S(?O)Me 1 C-5184 H H H H H 4-S(?O)Me 1 C-5185 H H H H H 2-S(?O).sub.2Me 1 C-5186 H H H H H 3-S(?O).sub.2Me 1 C-5187 H H H H H 4-S(?O).sub.2Me 1 C-5188 H H H H H 2-SCF.sub.3 1 C-5189 H H H H H 3-SCF.sub.3 1 C-5190 H H H H H 4-SCF.sub.3 1 C-5191 H H H H H 2-S(?O)CF.sub.3 1 C-5192 H H H H H 3-S(?O)CF.sub.3 1 C-5193 H H H H H 4-S(?O)CF.sub.3 1 C-5194 H H H H H 2-S(?O).sub.2CF.sub.3 1 C-5195 H H H H H 3-S(?O).sub.2CF.sub.3 1 C-5196 H H H H H 4-S(?O).sub.2CF.sub.3 1 C-5197 H H H H H 2-SCF(CF.sub.3).sub.2 1 C-5198 H H H H H 3-SCF(CF.sub.3).sub.2 1 C-5199 H H H H H 4-SCF(CF.sub.3).sub.2 1 C-5200 H H H H H 2-(cyclopropylthio) 1 C-5201 H H H H H 3-(cyclopropylthio) 1 C-5202 H H H H H 4-(cyclopropylthio) 1 C-5203 H H H H H 2-(cyclopropylsulfinyl) 1 C-5204 H H H H H 3-(cyclopropylsulfinyl) 1 C-5205 H H H H H 4-(cyclopropylsulfinyl) 1 C-5206 H H H H H 2-(cyclopropylsulfonyl) 1 C-5207 H H H H H 3-(cyclopropylsulfonyl) 1 C-5208 H H H H H 4-(cyclopropylsulfonyl) 1 C-5209 H H H H H 2-((cyclopropylmethyl)thio) 1 C-5210 H H H H H 3-((cyclopropylmethyl)thio) 1 C-5211 H H H H H 4-((cyclopropylmethyl)thio) 1 C-5212 H H H H H 2-((cyclopropylmethyl)sulfinyl) 1 C-5213 H H H H H 3-((cyclopropylmethyl)sulfinyl) 1 C-5214 H H H H H 4-((cyclopropylmethyl)sulfinyl) 1 C-5215 H H H H H 2-((cyclopropylmethyl)sulfonyl) 1 C-5216 H H H H H 3-((cyclopropylmethyl)sulfonyl) 1 C-5217 H H H H H 4-((cyclopropylmethyl)sulfonyl) 1 C-5218 H H H H H 2-(((2,2- 1 difluorocyclopropyl)methyl)thio) C-5219 H H H H H 3-(((2,2- 1 difluorocyclopropyl)methyl)thio) C-5220 H H H H H 4-(((2,2- 1 difluorocyclopropyl)methyl)thio) C-5221 H H H H H 2-(((2,2- 1 difluorocyclopropyl)methyl)sulfinyl) C-5222 H H H H H 3-(((2,2- 1 difluorocyclopropyl)methyl)sulfinyl) C-5223 H H H H H 4-(((2,2- 1 difluorocyclopropyl)methyl)sulfinyl)
(321) TABLE-US-00220 TABLE 220 com- pound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5224 H H H H H 2-(((2,2- 1 difluorocyclopropyl)methyl)sulfonyl) C-5225 H H H H H 3-(((2,2- 1 difluorocyclopropyl)methyl)sulfonyl) C-5226 H H H H H 4-(((2,2- 1 difluorocyclopropyl)methyl)sulfonyl) C-5227 H H H H H 2-C(?O)Me 1 C-5228 H H H H H 3-C(?O)Me 1 C-5229 H H H H H 4-C(?O)Me 1 C-5230 H H H H H 2-C(?O)Et 1 C-5231 H H H H H 3-C(?O)Et 1 C-5232 H H H H H 4-C(?O)Et 1 C-5233 H H H H H 2-C(?O)CF.sub.3 1 C-5234 H H H H H 3-C(?O)CF.sub.3 1 C-5235 H H H H H 4-C(?O)CF.sub.3 1 C-5236 H H H H H 2-C(?O)OMe 1 C-5237 H H H H H 3-C(?O)OMe 1 C-5238 H H H H H 4-C(?O)OMe 1 C-5239 H H H H H 2-C(?O)OEt 1 C-5240 H H H H H 3-C(?O)OEt 1 C-5241 H H H H H 4-C(?O)OEt 1 C-5242 H H H H H 2-C(?O)NH.sub.2 1 C-5243 H H H H H 3-C(?O)NH.sub.2 1 C-5244 H H H H H 4-C(?O)NH.sub.2 1 C-5245 H H H H H 2-C(?O)NHMe 1 C-5246 H H H H H 3-C(?O)NHMe 1 C-5247 H H H H H 4-C(?O)NHMe 1 C-5248 H H H H H 2-C(?O)NMe.sub.2 1 C-5249 H H H H H 3-C(?O)NMe.sub.2 1 C-5250 H H H H H 4-C(?O)NMe.sub.2 1 C-5251 H H H H H 2-CH.sub.2C(?O)CH.sub.3 1 C-5252 H H H H H 3-CH.sub.2C(?O)CH.sub.3 1 C-5253 H H H H H 4-CH.sub.2C(?O)CH.sub.3 1 C-5254 H H H H H 2-CH.sub.2C(?O)CF.sub.3 1 C-5255 H H H H H 3-CH.sub.2C(?O)CF.sub.3 1 C-5256 H H H H H 4-CH.sub.2C(?O)CF.sub.3 1 C-5257 H H H H H 2-CH.sub.2C(?O)OCH.sub.3 1 C-5258 H H H H H 3-CH.sub.2C(?O)OCH.sub.3 1 C-5259 H H H H H 4-CH.sub.2C(?O)OCH.sub.3 1 C-5260 H H H H H 2-CH.sub.2OH 1 C-5261 H H H H H 3-CH.sub.2OH 1 C-5262 H H H H H 4-CH.sub.2OH 1 C-5263 H H H H H 2-CH.sub.2OCH.sub.3 1 C-5264 H H H H H 3-CH.sub.2OCH.sub.3 1 C-5265 H H H H H 4-CH.sub.2OCH.sub.3 1 C-5266 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3 1 C-5267 H H H H H 3-CH.sub.2OCH.sub.2CH.sub.3 1 C-5268 H H H H H 4-CH.sub.2OCH.sub.2CH.sub.3 1 C-5269 H H H H H 2-CH(CH.sub.3)OCH.sub.3 1 C-5270 H H H H H 3-CH(CH.sub.3)OCH.sub.3 1 C-5271 H H H H H 4-CH(CH.sub.3)OCH.sub.3 1 C-5272 H H H H H 2-CH.sub.2CH.sub.2OCH.sub.3 1 C-5273 H H H H H 3-CH.sub.2CH.sub.2OCH.sub.3 1 C-5274 H H H H H 4-CH.sub.2CH.sub.2OCH.sub.3 1 C-5275 H H H H H 2-CH.sub.2OCF.sub.3 1 C-5276 H H H H H 3-CH.sub.2OCF.sub.3 1 C-5277 H H H H H 4-CH.sub.2OCF.sub.3 1 C-5278 H H H H H 2-CF.sub.2OCH.sub.3 1 C-5279 H H H H H 3-CF.sub.2OCH.sub.3 1 C-5280 H H H H H 4-CF.sub.2OCH.sub.3 1
(322) TABLE-US-00221 TABLE 221 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5281 H H H H H 2-CF.sub.2CF.sub.2OCF.sub.3 1 C-5282 H H H H H 3-CF.sub.2CF.sub.2OCF.sub.3 1 C-5283 H H H H H 4-CF.sub.2CF.sub.2OCF.sub.3 1 C-5284 H H H H H 2-OC(?O)CH.sub.3 1 C-5285 H H H H H 3-OC(?O)CH.sub.3 1 C-5286 H H H H H 4-OC(?O)CH.sub.3 1 C-5287 H H H H H 2-OC(?O)CF.sub.3 1 C-5288 H H H H H 3-OC(?O)CF.sub.3 1 C-5289 H H H H H 4-OC(?O)CF.sub.3 1 C-5290 H H H H H 2-OC(?O)NH.sub.2 1 C-5291 H H H H H 3-OC(?O)NH.sub.2 1 C-5292 H H H H H 4-OC(?O)NH.sub.2 1 C-5293 H H H H H 2-OC(?O)NHCH.sub.3 1 C-5294 H H H H H 3-OC(?O)NHCH.sub.3 1 C-5295 H H H H H 4-OC(?O)NHCH.sub.3 1 C-5296 H H H H H 2-OC(?O)N(CH.sub.3).sub.2 1 C-5297 H H H H H 3-OC(?O)N(CH.sub.3).sub.2 1 C-5298 H H H H H 4-OC(?O)N(CH.sub.3).sub.2 1 C-5299 H H H H H 2-CH.sub.2OC(?O)NH.sub.2 1 C-5300 H H H H H 3-CH.sub.2OC(?O)NH.sub.2 1 C-5301 H H H H H 4-CH.sub.2OC(?O)NH.sub.2 1 C-5302 H H H H H 2-CH.sub.2OC(?O)NHCH.sub.3 1 C-5303 H H H H H 3-CH.sub.2OC(?O)NHCH.sub.3 1 C-5304 H H H H H 4-CH.sub.2OC(?O)NHCH.sub.3 1 C-5305 H H H H H 2-CH.sub.2OC(?O)N(CH.sub.3).sub.2 1 C-5306 H H H H H 3-CH.sub.2OC(?O)N(CH.sub.3).sub.2 1 C-5307 H H H H H 4-CH.sub.2OC(?O)N(CH.sub.3).sub.2 1 C-5308 H H H H H 2-OC(?O)OCH.sub.3 1 C-5309 H H H H H 3-OC(?O)OCH.sub.3 1 C-5310 H H H H H 4-OC(?O)OCH.sub.3 1 C-5311 H H H H H 2-CH.sub.2OC(?O)OCH.sub.3 1 C-5312 H H H H H 3-CH.sub.2OC(?O)OCH.sub.3 1 C-5313 H H H H H 4-CH.sub.2OC(?O)OCH.sub.3 1 C-5314 H H H H H 2-CH.sub.2OC(?O)CH.sub.3 1 C-5315 H H H H H 3-CH.sub.2OC(?O)CH.sub.3 1 C-5316 H H H H H 4-CH.sub.2OC(?O)CH.sub.3 1 C-5317 H H H H H 2-OS(?O).sub.2CH.sub.3 1 C-5318 H H H H H 3-OS(?O).sub.2CH.sub.3 1 C-5319 H H H H H 4-OS(?O).sub.2CH.sub.3 1 C-5320 H H H H H 2-CH.sub.2SCH.sub.3 1 C-5321 H H H H H 3-CH.sub.2SCH.sub.3 1 C-5322 H H H H H 4-CH.sub.2SCH.sub.3 1 C-5323 H H H H H 2-CH.sub.2S(?O)CH.sub.3 1 C-5324 H H H H H 3-CH.sub.2S(?O)CH.sub.3 1 C-5325 H H H H H 4-CH.sub.2S(?O)CH.sub.3 1 C-5326 H H H H H 2-CH.sub.2S(?O).sub.2CH.sub.3 1 C-5327 H H H H H 3-CH.sub.2S(?O).sub.2CH.sub.3 1 C-5328 H H H H H 4-CH.sub.2S(?O).sub.2CH.sub.3 1 C-5329 H H H H H 2-CH.sub.2SCF.sub.3 1 C-5330 H H H H H 3-CH.sub.2SCF.sub.3 1 C-5331 H H H H H 4-CH.sub.2SCF.sub.3 1 C-5332 H H H H H 2-CH.sub.2S(?O)CF.sub.3 1 C-5333 H H H H H 3-CH.sub.2S(?O)CF.sub.3 1 C-5334 H H H H H 4-CH.sub.2S(?O)CF.sub.3 1 C-5335 H H H H H 2-CH.sub.2S(?O).sub.2CF.sub.3 1 C-5336 H H H H H 3-CH.sub.2S(?O).sub.2CF.sub.3 1 C-5337 H H H H H 4-CH.sub.2S(?O).sub.2CF.sub.3 1
(323) TABLE-US-00222 TABLE 222 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5338 H H H H H 2-phenyl 1 C-5339 H H H H H 3-phenyl 1 C-5340 H H H H H 4-phenyl 1 C-5341 H H H H H 2-(phenyloxy) 1 C-5342 H H H H H 3-(phenyloxy) 1 C-5343 H H H H H 4-(phenyloxy) 1 C-5344 H H H H H 2-benzyl 1 C-5345 H H H H H 3-benzyl 1 C-5346 H H H H H 4-benzyl 1 C-5347 H H H H H 2-(benzyloxy) 1 C-5348 H H H H H 3-(benzyloxy) 1 C-5349 H H H H H 4-(benzyloxy) 1 C-5350 H H H H H 2-((2-fluorobenzyl)oxy) 1 C-5351 H H H H H 3-((2-fluorobenzyl)oxy) 1 C-5352 H H H H H 4-((2-fluorobenzyl)oxy) 1 C-5353 H H H H H 2-((3-fluorobenzyl)oxy) 1 C-5354 H H H H H 3-((3-fluorobenzyl)oxy) 1 C-5355 H H H H H 4-((3-fluorobenzyl)oxy) 1 C-5356 H H H H H 2-((4-fluorobenzyl)oxy) 1 C-5357 H H H H H 3-((4-fluorobenzyl)oxy) 1 C-5358 H H H H H 4-((4-fluorobenzyl)oxy) 1 C-5359 H H H H H 2-((2-chlorobenzyl)oxy) 1 C-5360 H H H H H 3-((2-chlorobenzyl)oxy) 1 C-5361 H H H H H 4-((2-chlorobenzyl)oxy) 1 C-5362 H H H H H 2-((3-chlorobenzyl)oxy) 1 C-5363 H H H H H 3-((3-chlorobenzyl)oxy) 1 C-5364 H H H H H 4-((3-chlorobenzyl)oxy) 1 C-5365 H H H H H 2-((4-chlorobenzyl)oxy) 1 C-5366 H H H H H 3-((4-chlorobenzyl)oxy) 1 C-5367 H H H H H 4-((4-chlorobenzyl)oxy) 1 C-5368 H H H H H 2-((2-methylbenzyl)oxy) 1 C-5369 H H H H H 3-((2-methylbenzyl)oxy) 1 C-5370 H H H H H 4-((2-methylbenzyl)oxy) 1 C-5371 H H H H H 2-((3-methylbenzyl)oxy) 1 C-5372 H H H H H 3-((3-methylbenzyl)oxy) 1 C-5373 H H H H H 4-((3-methylbenzyl)oxy) 1 C-5374 H H H H H 2-((4-methylbenzyl)oxy) 1 C-5375 H H H H H 3-((4-methylbenzyl)oxy) 1 C-5376 H H H H H 4-((4-methylbenzyl)oxy) 1 C-5377 H H H H H 2-((2-(trifluoromethyl)benzyl)oxy) 1 C-5378 H H H H H 3-((2-(trifluoromethyl)benzyl)oxy) 1 C-5379 H H H H H 4-((2-(trifluoromethyl)benzyl)oxy) 1 C-5380 H H H H H 2-((3-(trifluoromethyl)benzyl)oxy) 1 C-5381 H H H H H 3-((3-(trifluoromethyl)benzyl)oxy) 1 C-5382 H H H H H 4-((3-(trifluoromethyl)benzyl)oxy) 1 C-5383 H H H H H 2-((4-(trifluoromethyl)benzyl)oxy) 1 C-5384 H H H H H 3-((4-(trifluoromethyl)benzyl)oxy) 1 C-5385 H H H H H 4-((4-(trifluoromethyl)benzyl)oxy) 1 C-5386 H H H H H 2-((2-methoxybenzyl)oxy) 1 C-5387 H H H H H 3-((2-methoxybenzyl)oxy) 1 C-5388 H H H H H 4-((2-methoxybenzyl)oxy) 1 C-5389 H H H H H 2-((3-methoxybenzyl)oxy) 1 C-5390 H H H H H 3-((3-methoxybenzyl)oxy) 1 C-5391 H H H H H 4-((3-methoxybenzyl)oxy) 1 C-5392 H H H H H 2-((4-methoxybenzyl)oxy) 1 C-5393 H H H H H 3-((4-methoxybenzyl)oxy) 1 C-5394 H H H H H 4-((4-methoxybenzyl)oxy) 1
(324) TABLE-US-00223 TABLE 223 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5395 H H H H H 2-((2-(trifluoromethoxy)benzyl)oxy) 1 C-5396 H H H H H 3-((2-(trifluoromethoxy)benzyl)oxy) 1 C-5397 H H H H H 4-((2-(trifluoromethoxy)benzyl)oxy) 1 C-5398 H H H H H 2-((3-(trifluoromethoxy)benzyl)oxy) 1 C-5399 H H H H H 3-((3-(trifluoromethoxy)benzyl)oxy) 1 C-5400 H H H H H 4-((3-(trifluoromethoxy)benzyl)oxy) 1 C-5401 H H H H H 2-((4-(trifluoromethoxy)benzyl)oxy) 1 C-5402 H H H H H 3-((4-(trifluoromethoxy)benzyl)oxy) 1 C-5403 H H H H H 4-((4-(trifluoromethoxy)benzyl)oxy) 1 C-5404 H H H H H 2-((2-(methylthio)benzyl)oxy) 1 C-5405 H H H H H 3-((2-(methylthio)benzyl)oxy) 1 C-5406 H H H H H 4-((2-(methylthio)benzyl)oxy) 1 C-5407 H H H H H 2-((3-(methylthio)benzyl)oxy) 1 C-5408 H H H H H 3-((3-(methylthio)benzyl)oxy) 1 C-5409 H H H H H 4-((3-(methylthio)benzyl)oxy) 1 C-5410 H H H H H 2-((4-(methylthio)benzyl)oxy) 1 C-5411 H H H H H 3-((4-(methylthio)benzyl)oxy) 1 C-5412 H H H H H 4-((4-(methylthio)benzyl)oxy) 1 C-5413 H H H H H 2-((2-(methylsulfinyl)benzyl)oxy) 1 C-5414 H H H H H 3-((2-(methylsulfinyl)benzyl)oxy) 1 C-5415 H H H H H 4-((2-(methylsulfinyl)benzyl)oxy) 1 C-5416 H H H H H 2-((3-(methylsulfinyl)benzyl)oxy) 1 C-5417 H H H H H 3-((3-(methylsulfinyl)benzyl)oxy) 1 C-5418 H H H H H 4-((3-(methylsulfinyl)benzyl)oxy) 1 C-5419 H H H H H 2-((4-(methylsulfinyl)benzyl)oxy) 1 C-5420 H H H H H 3-((4-(methylsulfinyl)benzyl)oxy) 1 C-5421 H H H H H 4-((4-(methylsulfinyl)benzyl)oxy) 1 C-5422 H H H H H 2-((2-(methylsulfonyl)benzyl)oxy) 1 C-5423 H H H H H 3-((2-(methylsulfonyl)benzyl)oxy) 1 C-5424 H H H H H 4-((2-(methylsulfonyl)benzyl)oxy) 1 C-5425 H H H H H 2-((3-(methylsulfonyl)benzyl)oxy) 1 C-5426 H H H H H 3-((3-(methylsulfonyl)benzyl)oxy) 1 C-5427 H H H H H 4-((3-(methylsulfonyl)benzyl)oxy) 1 C-5428 H H H H H 2-((4-(methylsulfonyl)benzyl)oxy) 1 C-5429 H H H H H 3-((4-(methylsulfonyl)benzyl)oxy) 1 C-5430 H H H H H 4-((4-(methylsulfonyl)benzyl)oxy) 1 C-5431 H H H H H 2-((2-(trifluoromethylthio)benzyl)oxy) 1 C-5432 H H H H H 3-((2-(trifluoromethylthio)benzyl)oxy) 1 C-5433 H H H H H 4-((2-(trifluoromethylthio)benzyl)oxy) 1 C-5434 H H H H H 2-((3-(trifluoromethylthio)benzyl)oxy) 1 C-5435 H H H H H 3-((3-(trifluoromethylthio)benzyl)oxy) 1 C-5436 H H H H H 4-((3-(trifluoromethylthio)benzyl)oxy) 1 C-5437 H H H H H 2-((4-(trifluoromethylthio)benzyl)oxy) 1 C-5438 H H H H H 3-((4-(trifluoromethylthio)benzyl)oxy) 1 C-5439 H H H H H 4-((4-(trifluoromethylthio)benzyl)oxy) 1 C-5440 H H H H H 2-((2-(trifluoromethylsulfinyl)benzyl)oxy) 1 C-5441 H H H H H 3-((2-(trifluoromethylsulfinyl)benzyl)oxy) 1 C-5442 H H H H H 4-((2-(trifluoromethylsulfinyl)benzyl)oxy) 1 C-5443 H H H H H 2-((3-(trifluoromethylsulfinyl)benzyl)oxy) 1 C-5444 H H H H H 3-((3-(trifluoromethylsulfinyl)benzyl)oxy) 1 C-5445 H H H H H 4-((3-(trifluoromethylsulfinyl)benzyl)oxy) 1 C-5446 H H H H H 2-((4-(trifluoromethylsulfinyl)benzyl)oxy) 1 C-5447 H H H H H 3-((4-(trifluoromethylsulfinyl)benzyl)oxy) 1 C-5448 H H H H H 4-((4-(trifluoromethylsulfinyl)benzyl)oxy) 1 C-5449 H H H H H 2-((2-(trifluoromethylsulfonyl)benzyl)oxy) 1 C-5450 H H H H H 3-((2-(trifluoromethylsulfonyl)benzyl)oxy) 1 C-5451 H H H H H 4-((2-(trifluoromethylsulfonyl)benzyl)oxy) 1
(325) TABLE-US-00224 TABLE 224 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5452 H H H H H 2-((3-(trifluoromethylsulfonyl)benzyl)oxy) 1 C-5453 H H H H H 3-((3-(trifluoromethylsulfonyl)benzyl)oxy) 1 C-5454 H H H H H 4-((3-(trifluoromethylsulfonyl)benzyl)oxy) 1 C-5455 H H H H H 2-((4-(trifluoromethylsulfonyl)benzyl)oxy) 1 C-5456 H H H H H 3-((4-(trifluoromethylsulfonyl)benzyl)oxy) 1 C-5457 H H H H H 4-((4-(trifluoromethylsulfonyl)benzyl)oxy) 1 C-5458 H H H H H 2-((2-aminobenzyl)oxy) 1 C-5459 H H H H H 3-((2-aminobenzyl)oxy) 1 C-5460 H H H H H 4-((2-aminobenzyl)oxy) 1 C-5461 H H H H H 2-((3-aminobenzyl)oxy) 1 C-5462 H H H H H 3-((3-aminobenzyl)oxy) 1 C-5463 H H H H H 4-((3-aminobenzyl)oxy) 1 C-5464 H H H H H 2-((4-aminobenzyl)oxy) 1 C-5465 H H H H H 3-((4-aminobenzyl)oxy) 1 C-5466 H H H H H 4-((4-aminobenzyl)oxy) 1 C-5467 H H H H H 2-((2-(methylamino)benzyl)oxy) 1 C-5468 H H H H H 3-((2-(methylamino)benzyl)oxy) 1 C-5469 H H H H H 4-((2-(methylamino)benzyl)oxy) 1 C-5470 H H H H H 2-((3-(methylamino)benzyl)oxy) 1 C-5471 H H H H H 3-((3-(methylamino)benzyl)oxy) 1 C-5472 H H H H H 4-((3-(methylamino)benzyl)oxy) 1 C-5473 H H H H H 2-((4-(methylamino)benzyl)oxy) 1 C-5474 H H H H H 3-((4-(methylamino)benzyl)oxy) 1 C-5475 H H H H H 4-((4-(methylamino)benzyl)oxy) 1 C-5476 H H H H H 2-((2-(dimethylamino)benzyl)oxy) 1 C-5477 H H H H H 3-((2-(dimethylamino)benzyl)oxy) 1 C-5478 H H H H H 4-((2-(dimethylamino)benzyl)oxy) 1 C-5479 H H H H H 2-((3-(dimethylamino)benzyl)oxy) 1 C-5480 H H H H H 3-((3-(dimethylamino)benzyl)oxy) 1 C-5481 H H H H H 4-((3-(dimethylamino)benzyl)oxy) 1 C-5482 H H H H H 2-((4-(dimethylamino)benzyl)oxy) 1 C-5483 H H H H H 3-((4-(dimethylamino)benzyl)oxy) 1 C-5484 H H H H H 4-((4-(dimethylamino)benzyl)oxy) 1 C-5485 H H H H H 2-((2-cyanobenzyl)oxy) 1 C-5486 H H H H H 3-((2-cyanobenzyl)oxy) 1 C-5487 H H H H H 4-((2-cyanobenzyl)oxy) 1 C-5488 H H H H H 2-((3-cyanobenzyl)oxy) 1 C-5489 H H H H H 3-((3-cyanobenzyl)oxy) 1 C-5490 H H H H H 4-((3-cyanobenzyl)oxy) 1 C-5491 H H H H H 2-((4-cyanobenzyl)oxy) 1 C-5492 H H H H H 3-((4-cyanobenzyl)oxy) 1 C-5493 H H H H H 4-((4-cyanobenzyl)oxy) 1 C-5494 H H H H H 2-((2-nitrobenzyl)oxy) 1 C-5495 H H H H H 3-((2-nitrobenzyl)oxy) 1 C-5496 H H H H H 4-((2-nitrobenzyl)oxy) 1 C-5497 H H H H H 2-((3-nitrobenzyl)oxy) 1 C-5498 H H H H H 3-((3-nitrobenzyl)oxy) 1 C-5499 H H H H H 4-((3-nitrobenzyl)oxy) 1 C-5500 H H H H H 2-((4-nitrobenzyl)oxy) 1 C-5501 H H H H H 3-((4-nitrobenzyl)oxy) 1 C-5502 H H H H H 4-((4-nitrobenzyl)oxy) 1 C-5503 H H H H H 2-NH.sub.2 1 C-5504 H H H H H 3-NH.sub.2 1 C-5505 H H H H H 4-NH.sub.2 1 C-5506 H H H H H 2-NHMe 1 C-5507 H H H H H 3-NHMe 1 C-5508 H H H H H 4-NHMe 1
(326) TABLE-US-00225 TABLE 225 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5509 H H H H H 2-NHEt 1 C-5510 H H H H H 3-NHEt 1 C-5511 H H H H H 4-NHEt 1 C-5512 H H H H H 2-N(Me).sub.2 1 C-5513 H H H H H 3-N(Me).sub.2 1 C-5514 H H H H H 4-N(Me).sub.2 1 C-5515 H H H H H 2-N(Et).sub.2 1 C-5516 H H H H H 3-N(Et).sub.2 1 C-5517 H H H H H 4-N(Et).sub.2 1 C-5518 H H H H H 2-CHO 1 C-5519 H H H H H 3-CHO 1 C-5520 H H H H H 4-CHO 1 C-5521 H H H H H 2-C(?O)OH 1 C-5522 H H H H H 3-C(?O)OH 1 C-5523 H H H H H 4-C(?O)OH 1 C-5524 H H H H H 2-(1,3-dioxolan-2-yl) 1 C-5525 H H H H H 3-(1,3-dioxolan-2-yl) 1 C-5526 H H H H H 4-(1,3-dioxolan-2-yl) 1 C-5527 H H H H H 2-(1,3-dioxan-2-yl) 1 C-5528 H H H H H 3-(1,3-dioxan-2-yl) 1 C-5529 H H H H H 4-(1,3-dioxan-2-yl) 1 C-5530 H H H H H 2-(1H-imidazol-2-yl) 1 C-5531 H H H H H 3-(1H-imidazol-2-yl) 1 C-5532 H H H H H 4-(1H-imidazol-2-yl) 1 C-5533 H H H H H 2-(thiazol-2-yl) 1 C-5534 H H H H H 3-(thiazol-2-yl) 1 C-5535 H H H H H 4-(thiazol-2-yl) 1 C-5536 H H H H H 2-(oxazol-2-yl) 1 C-5537 H H H H H 3-(oxazol-2-yl) 1 C-5538 H H H H H 4-(oxazol-2-yl) 1 C-5539 H H H H H 2-CH?NOH 1 C-5540 H H H H H 3-CH?NOH 1 C-5541 H H H H H 4-CH?NOH 1 C-5542 H H H H H 2-CH?NOMe 1 C-5543 H H H H H 3-CH?NOMe 1 C-5544 H H H H H 4-CH?NOMe 1 C-5545 H H H H H 2-(4,5-dihydro-3-isoxazolyl) 1 C-5546 H H H H H 3-(4,5-dihydro-3-isoxazolyl) 1 C-5547 H H H H H 4-(4,5-dihydro-3-isoxazolyl) 1 C-5548 H H H H H 2-CN 1 C-5549 H H H H H 3-CN 1 C-5550 H H H H H 4-CN 1 C-5551 H H H H H 2-NO.sub.2 1 C-5552 H H H H H 3-NO.sub.2 1 C-5553 H H H H H 4-NO.sub.2 1 C-5554 H H H H H 2,3-F.sub.2 1 C-5555 H H H H H 2,4-F.sub.2 1 C-5556 H H H H H 2,5-F.sub.2 1 C-5557 H H H H H 2,6-F.sub.2 1 C-5558 H H H H H 3,4-F.sub.2 1 C-5559 H H H H H 3,5-F.sub.2 1 C-5560 H H H H H 2-F,3-Cl 1 C-5561 H H H H H 2-F,4-Cl 1 C-5562 H H H H H 2-F,5-Cl 1 C-5563 H H H H H 2-F,6-Cl 1 C-5564 H H H H H 3-F,2-Cl 1 C-5565 H H H H H 3-F,4-Cl 1
(327) TABLE-US-00226 TABLE 226 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5566 H H H H H 3-F,5-Cl 1 C-5567 H H H H H 3-F,6-Cl 1 C-5568 H H H H H 4-F,2-Cl 1 C-5569 H H H H H 4-F,3-Cl 1 C-5570 H H H H H 2-F,3-Me 1 C-5571 H H H H H 2-F,4-Me 1 C-5572 H H H H H 2-F,5-Me 1 C-5573 H H H H H 2-F,6-Me 1 C-5574 H H H H H 3-F,3-Me 1 C-5575 H H H H H 3-F,4-Me 1 C-5576 H H H H H 3-F,5-Me 1 C-5577 H H H H H 3-F,6-Me 1 C-5578 H H H H H 4-F,2-Me 1 C-5579 H H H H H 4-F,3-Me 1 C-5580 H H H H H 2-F,3-CF.sub.3 1 C-5581 H H H H H 2-F,4-CF.sub.3 1 C-5582 H H H H H 2-F,5-CF.sub.3 1 C-5583 H H H H H 2-F,6-CF.sub.3 1 C-5584 H H H H H 3-F,2-CF.sub.3 1 C-5585 H H H H H 3-F,4-CF.sub.3 1 C-5586 H H H H H 3-F,5-CF.sub.3 1 C-5587 H H H H H 3-F,6-CF.sub.3 1 C-5588 H H H H H 4-F,2-CF.sub.3 1 C-5589 H H H H H 4-F,3-CF.sub.3 1 C-5590 H H H H H 2-F,3-OMe 1 C-5591 H H H H H 2-F,4-OMe 1 C-5592 H H H H H 2-F,5-OMe 1 C-5593 H H H H H 2-F,6-OMe 1 C-5594 H H H H H 3-F,2-OMe 1 C-5595 H H H H H 3-F,4-OMe 1 C-5596 H H H H H 3-F,5-OMe 1 C-5597 H H H H H 3-F,6-OMe 1 C-5598 H H H H H 4-F,2-OMe 1 C-5599 H H H H H 4-F,3-OMe 1 C-5600 H H H H H 2,3-Cl.sub.2 1 C-5601 H H H H H 2,4-Cl.sub.2 1 C-5602 H H H H H 2,5-Cl.sub.2 1 C-5603 H H H H H 2,6-Cl.sub.2 1 C-5604 H H H H H 3,4-Cl.sub.2 1 C-5605 H H H H H 3,5-Cl.sub.2 1 C-5606 H H H H H 2-Cl,3-Me 1 C-5607 H H H H H 2-Cl,4-Me 1 C-5608 H H H H H 2-Cl,5-Me 1 C-5609 H H H H H 2-Cl,6-Me 1 C-5610 H H H H H 3-Cl,2-Me 1 C-5611 H H H H H 3-Cl,4-Me 1 C-5612 H H H H H 3-Cl,5 Me 1 C-5613 H H H H H 3-Cl,6 Me 1 C-5614 H H H H H 4-Cl,2 Me 1 C-5615 H H H H H 4-Cl,3-Me 1 C-5616 H H H H H 2-Cl,3-CF.sub.3 1 C-5617 H H H H H 2-Cl,4-CF.sub.3 1 C-5618 H H H H H 2-Cl,5-CF.sub.3 1 C-5619 H H H H H 2-Cl,6-CF.sub.3 1 C-5620 H H H H H 3-Cl,2-CF.sub.3 1 C-5621 H H H H H 3-Cl,4-CF.sub.3 1 C-5622 H H H H H 3-Cl,5-CF.sub.3 1
(328) TABLE-US-00227 TABLE 227 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5623 H H H H H 3-Cl,6-CF.sub.3 1 C-5624 H H H H H 4-Cl,2-CF.sub.3 1 C-5625 H H H H H 4-Cl,3-CF.sub.3 1 C-5626 H H H H H 2-Cl,3-OMe 1 C-5627 H H H H H 2-Cl,4-OMe 1 C-5628 H H H H H 2-Cl,5-OMe 1 C-5629 H H H H H 2-Cl,6-OMe 1 C-5630 H H H H H 3-Cl,2-OMe 1 C-5631 H H H H H 3-Cl,4-OMe 1 C-5632 H H H H H 3-Cl,5-OMe 1 C-5633 H H H H H 3-Cl,6-OMe 1 C-5634 H H H H H 4-Cl,2-OMe 1 C-5635 H H H H H 4-Cl,3-OMe 1 C-5636 H H H H H 2,3-Me.sub.2 1 C-5637 H H H H H 2,4-Me.sub.2 1 C-5638 H H H H H 2,5-Me.sub.2 1 C-5639 H H H H H 2,6-Me.sub.2 1 C-5640 H H H H H 3,4-Me.sub.2 1 C-5641 H H H H H 3,5-Me.sub.2 1 C-5642 H H H H H 2-Me,3-CF.sub.3 1 C-5643 H H H H H 2-Me,4-CF.sub.3 1 C-5644 H H H H H 2-Me,5-CF.sub.3 1 C-5645 H H H H H 2-Me,6-CF.sub.3 1 C-5646 H H H H H 3-Me,2-CF.sub.3 1 C-5647 H H H H H 3-Me,4-CF.sub.3 1 C-5648 H H H H H 3-Me,5-CF.sub.3 1 C-5649 H H H H H 3-Me,6-CF.sub.3 1 C-5650 H H H H H 4-Me,2-CF.sub.3 1 C-5651 H H H H P 4-Me,3-CF.sub.3 1 C-5652 H H H H H 2-Me,3-OMe 1 C-5653 H H H H H 2-Me,4-OMe 1 C-5654 H H H H H 2-Me,5-OMe 1 C-5655 H H H H H 2-Me,6-OMe 1 C-5656 H H H H H 3-Me,2-OMe 1 C-5657 H H H H H 3-Me,4-OMe 1 C-5658 H H H H H 3-Me,5-OMe 1 C-5659 H H H H H 3-Me,6-OMe 1 C-5660 H H H H H 4-Me,2-OMe 1 C-5661 H H H H H 4-Me,3-OMe 1 C-5662 H H H H H 2,3-OMe.sub.2 1 C-5663 H H H H H 2,4-OMe.sub.2 1 C-5664 H H H H H 2,5-OMe.sub.2 1 C-5665 H H H H H 2,6-OMe.sub.2 1 C-5666 H H H H H 3,4-OMe.sub.2 1 C-5667 H H H H H 3,5-OMe.sub.2 1 C-5668 H H H H H 2-OMe,3-CF.sub.3 1 C-5669 H H H H H 2-OMe,4-CF.sub.3 1 C-5670 H H H H H 2-OMe,5-CF.sub.3 1 C-5671 H H H H H 2-OMe,6-CF.sub.3 1 C-5672 H H H H H 3-OMe,2-CF.sub.3 1 C-5673 H H H H H 3-OMe,4-CF.sub.3 1 C-5674 H H H H H 3-OMe,5-CF.sub.3 1 C-5675 H H H H H 3-OMe,6-CF.sub.3 1 C-5676 H H H H H 4-OMe,2-CF.sub.3 1 C-5677 H H H H H 4-OMe,3-CF.sub.3 1 C-5678 H H H H H 2-CHF.sub.2,3-F 1 C-5679 H H H H H 2-CHF.sub.2,4-F 1
(329) TABLE-US-00228 TABLE 228 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5680 H H H H H 2-CHF.sub.2,5-F 1 C-5681 H H H H H 2-CHF.sub.2,6-F 1 C-5682 H H H H H 2-CHF.sub.2,3-Me 1 C-5683 H H H H H 2-CHF.sub.2,4-Me 1 C-5684 H H H H H 2-CHF.sub.2,5-Me 1 C-5685 H H H H H 2-CHF.sub.2,6-Me 1 C-5686 H H H H H 2-cyclopropyl,3-F 1 C-5687 H H H H H 2-cyclopropyl,4-F 1 C-5688 H H H H H 2-cyclopropyl,5-F 1 C-5689 H H H H H 2-cyclopropyl,6-F 1 C-5690 H H H H H 2-cyclopropyl,3-Me 1 C-5691 H H H H H 2-cyclopropyl,4-Me 1 C-5692 H H H H H 2-cyclopropyl,5-Me 1 C-5693 H H H H H 2-cyclopropyl,6-Me 1 C-5694 H H H H H 2-ethenyl,3-F 1 C-5695 H H H H H 2-ethenyl,4-F 1 C-5696 H H H H H 2-ethenyl,5-F 1 C-5697 H H H H H 2-ethenyl,6-F 1 C-5698 H H H H H 2-ethenyl,3-Me 1 C-5699 H H H H H 2-ethenyl,4-Me 1 C-5700 H H H H H 2-ethenyl,5-Me 1 C-5701 H H H H H 2-ethenyl,6-Me 1 C-5702 H H H H H 2-OEt,3-F 1 C-5703 H H H H H 2-OEt,4-F 1 C-5704 H H H H H 2-OEt,5-F 1 C-5705 H H H H H 2-OEt,6-F 1 C-5706 H H H H H 2-OEt,3-Cl 1 C-5707 H H H H H 2-OEt,4-Cl 1 C-5708 H H H H H 2-OEt,5-Cl 1 C-5709 H H H H H 2-OEt,6-Cl 1 C-5710 H H H H H 2-OEt,3-Me 1 C-5711 H H H H H 2-OEt,4-Me 1 C-5712 H H H H H 2-OEt,5-Me 1 C-5713 H H H H H 2-OEt,6-Me 1 C-5714 H H H H H 2-OPr,3-F 1 C-5715 H H H H H 2-OPr,4-F 1 C-5716 H H H H H 2-OPr,5-F 1 C-5717 H H H H H 2-OPr,6-F 1 C-5718 H H H H H 2-OPr,3-Me 1 C-5719 H H H H H 2-OPr,4-Me 1 C-5720 H H H H H 2-OPr,5-Me 1 C-5721 H H H H H 2-OPr,6-Me 1 C-5722 H H H H H 2-O(i-Pr),3-F 1 C-5723 H H H H H 2-O(i-Pr),4-F 1 C-5724 H H H H H 2-O(i-Pr),5-F 1 C-5725 H H H H H 2-O(i-Pr),6-F 1 C-5726 H H H H H 2-O(i-Pr),3-Me 1 C-5727 H H H H H 2-O(i-Pr),4-Me 1 C-5728 H H H H H 2-O(i-Pr),5-Me 1 C-5729 H H H H H 2-O(i-Pr),6-Me 1 C-5730 H H H H H 2-OCF.sub.3,3-F 1 C-5731 H H H H H 2-OCF.sub.3,4-F 1 C-5732 H H H H H 2-OCF.sub.3,5-F 1 C-5733 H H H H H 2-OCF.sub.3,6-F 1 C-5734 H H H H H 2-OCF.sub.3,3-Me 1 C-5735 H H H H H 2-OCF.sub.3,4-Me 1 C-5736 H H H H H 2-OCF.sub.3,5-Me 1
(330) TABLE-US-00229 TABLE 229 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5737 H H H H H 2-OCF.sub.3,6-Me 1 C-5738 H H H H H 2-OCHF.sub.2,3-F 1 C-5739 H H H H H 2-OCHF.sub.2,4-F 1 C-5740 H H H H H 2-OCHF.sub.2,5-F 1 C-5741 H H H H H 2-OCHF.sub.2,6-F 1 C-5742 H H H H H 2-OCHF.sub.2,3-Me 1 C-5743 H H H H H 2-OCHF.sub.2,4-Me 1 C-5744 H H H H H 2-OCHF.sub.2,5-Me 1 C-5745 H H H H H 2-OCHF.sub.2,6-Me 1 C-5746 H H H H H 2-(cyclopropyloxy),3-F 1 C-5747 H H H H H 2-(cyclopropyloxy),4-F 1 C-5748 H H H H H 2-(cyclopropyloxy),5-F 1 C-5749 H H H H H 2-(cyclopropyloxy),6-F 1 C-5750 H H H H H 2-(cyclopropyloxy),3-Me 1 C-5751 H H H H H 2-(cyclopropyloxy),4-Me 1 C-5752 H H H H H 2-(cyclopropyloxy),5-Me 1 C-5753 H H H H H 2-(cyclopropyloxy),6-Me 1 C-5754 H H H H H 2-(oxiran-2-yl),3-F 1 C-5755 H H H H H 2-(oxiran-2-yl),4-F 1 C-5756 H H H H H 2-(oxiran-2-yl),5-F 1 C-5757 H H H H H 2-(oxiran-2-yl),6-F 1 C-5758 H H H H H 2-(oxiran-2-yl),3-Me 1 C-5759 H H H H H 2-(oxiran-2-yl),4-Me 1 C-5760 H H H H H 2-(oxiran-2-yl),5-Me 1 C-5761 H H H H H 2-(oxiran-2-yl),6-Me 1 C-5762 H H H H H 2-(oxiran-2-ylmethyl),3-F 1 C-5763 H H H H H 2-(oxiran-2-ylmethyl),4-F 1 C-5764 H H H H H 2-(oxiran-2-ylmethyl),5-F 1 C-5765 H H H H H 2-(oxiran-2-ylmethyl),6-F 1 C-5766 H H H H H 2-(oxiran-2-ylmethyl),3-Me 1 C-5767 H H H H H 2-(oxiran-2-ylmethyl),4-Me 1 C-5768 H H H H H 2-(oxiran-2-ylmethyl),5-Me 1 C-5769 H H H H H 2-(oxiran-2-ylmethyl),6-Me 1 C-5770 H H H H H 2-SMe,3-F 1 C-5771 H H H H H 2-SMe,4-F 1 C-5772 H H H H H 2-SMe,5-F 1 C-5773 H H H H H 2-SMe,6-F 1 C-5774 H H H H H 2-SMe,3-Me 1 C-5775 H H H H H 2-SMe,4-Me 1 C-5776 H H H H H 2-SMe,5-Me 1 C-5777 H H H H H 2-SMe,6-Me 1 C-5778 H H H H H 2-SEt,3-F 1 C-5779 H H H H H 2-SEt,4-F 1 C-5780 H H H H H 2-SEt,5-F 1 C-5781 H H H H H 2-SEt,6-F 1 C-5782 H H H H H 2-SEt,3-Me 1 C-5783 H H H H H 2-SEt,4-Me 1 C-5784 H H H H H 2-SEt,5-Me 1 C-5785 H H H H H 2-SEt,6-Me 1 C-5786 H H H H H 2-S(?O)Me,3-F 1 C-5787 H H H H H 2-S(?O)Me,4-F 1 C-5788 H H H H H 2-S(?O)Me,5-F 1 C-5789 H H H H H 2-S(?O)Me,6-F 1 C-5790 H H H H H 3-S(?O)Me,2-F 1 C-5791 H H H H H 3-S(?O)Me,4-F 1 C-5792 H H H H H 3-S(?O)Me,5-F 1 C-5793 H H H H H 3-S(?O)Me,6-F 1
(331) TABLE-US-00230 TABLE 230 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5794 H H H H H 2-S(?O)Me,3-Me 1 C-5795 H H H H H 2-S(?O)Me,4-Me 1 C-5796 H H H H H 2-S(?O)Me,5-Me 1 C-5797 H H H H H 2-S(?O)Me,6-Me 1 C-5798 H H H H H 3-S(?O)Me,2-Me 1 C-5799 H H H H H 3-S(?O)Me,4-Me 1 C-5800 H H H H H 3-S(?O)Me,5-Me 1 C-5801 H H H H H 3-S(?O)Me,6-Me 1 C-5802 H H H H H 2-S(?O).sub.2Me,3-F 1 C-5803 H H H H H 2-S(?O).sub.2Me,4-F 1 C-5804 H H H H H 2-S(?O).sub.2Me,5-F 1 C-5805 H H H H H 2-S(?O).sub.2Me,6-F 1 C-5806 H H H H H 2-S(?O).sub.2Me,3-Me 1 C-5807 H H H H H 2-S(?O).sub.2Me,4-Me 1 C-5808 H H H H H 2-S(?O).sub.2Me,5-Me 1 C-5809 H H H H H 2-S(?O).sub.2Me,6-Me 1 C-5810 H H H H H 2-SCF.sub.3,3-F 1 C-5811 H H H H H 2-SCF.sub.3,4-F 1 C-5812 H H H H H 2-SCF.sub.3,5-F 1 C-5813 H H H H H 2-SCF.sub.3,6-F 1 C-5814 H H H H H 2-SCF.sub.3,3-Me 1 C-5815 H H H H H 2-SCF.sub.3,4-Me 1 C-5816 H H H H H 2-SCF.sub.3,5-Me 1 C-5817 H H H H H 2-SCF.sub.3,6-Me 1 C-5818 H H H H H 2-S(?O)CF.sub.3,3-F 1 C-5819 H H H H H 2-S(?O)CF.sub.3,4-F 1 C-5820 H H H H H 2-S(?O)CF.sub.3,5-F 1 C-5821 H H H H H 2-S(?O)CF.sub.3,6-F 1 C-5822 H H H H H 2-S(?O)CF.sub.3,3-Me 1 C-5823 H H H H H 2-S(?O)CF.sub.3,3-Me 1 C-5824 H H H H H 2-S(?O)CF.sub.3,3-Me 1 C-5825 H H H H H 2-S(?O)CF.sub.3,3-Me 1 C-5826 H H H H H 2-S(?O).sub.2CF.sub.3,3-F 1 C-5827 H H H H H 2-S(?O).sub.2CF.sub.3,4-F 1 C-5828 H H H H H 2-S(?O).sub.2CF.sub.3,5-F 1 C-5829 H H H H H 2-S(?O).sub.2CF.sub.3,6-F 1 C-5830 H H H H H 2-S(?O).sub.2CF.sub.3,3-Me 1 C-5831 H H H H H 2-S(?O).sub.2CF.sub.3,4-Me 1 C-5832 H H H H H 2-S(?O).sub.2CF.sub.3,5-Me 1 C-5833 H H H H H 2-S(?O).sub.2CF.sub.3,6-Me 1 C-5834 H H H H H 2-(cyclopropylthio),3-F 1 C-5835 H H H H H 2-(cyclopropylthio),4-F 1 C-5836 H H H H H 2-(cyclopropylthio),5-F 1 C-5837 H H H H H 2-(cyclopropylthio),6-F 1 C-5838 H H H H H 2-(cyclopropylthio),3-Me 1 C-5839 H H H H H 2-(cyclopropylthio),4-Me 1 C-5840 H H H H H 2-(cyclopropylthio),5-Me 1 C-5841 H H H H H 2-(cyclopropylthio),6-Me 1 C-5842 H H H H H 2-C(?O)Me,3-F 1 C-5843 H H H H H 2-C(?O)Me,4-F 1 C-5844 H H H H H 2-C(?O)Me,5-F 1 C-5845 H H H H H 2-C(?O)Me,6-F 1 C-5846 H H H H H 2-C(?O)Me,3-Me 1 C-5847 H H H H H 2-C(?O)Me,4-Me 1 C-5848 H H H H H 2-C(?O)Me,5-Me 1 C-5849 H H H H H 2-C(?O)Me,6-Me 1 C-5850 H H H H H 3-C(?O)Me,2-F 1
(332) TABLE-US-00231 TABLE 231 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5851 H H H H H 3-C(?O)Me,4-F 1 C-5852 H H H H H 3-C(?O)Me,5-F 1 C-5853 H H H H H 3-C(?O)Me,6-F 1 C-5854 H H H H H 3-C(?O)Me,2-Me 1 C-5855 H H H H H 3-C(?O)Me,4-Me 1 C-5856 H H H H H 3-C(?O)Me,5-Me 1 C-5857 H H H H H 3-C(?O)Me,6-Me 1 C-5858 H H H H H 2-C(?O)OMe,3-F 1 C-5859 H H H H H 2-C(?O)OMe,4-F 1 C-5860 H H H H H 2-C(?O)OMe,5-F 1 C-5861 H H H H H 2-C(?O)OMe,6-F 1 C-5862 H H H H H 2-C(?O)OMe,3-Me 1 C-5863 H H H H H 2-C(?O)OMe,4-Me 1 C-5864 H H H H H 2-C(?O)OMe,5-Me 1 C-5865 H H H H H 2-C(?O)OMe,6-Me 1 C-5866 H H H H H 2-C(?O)OEt,3-F 1 C-5867 H H H H H 2-C(?O)OEt,4-F 1 C-5868 H H H H H 2-C(?O)OEt,5-F 1 C-5869 H H H H H 2-C(?O)OEt,6-F 1 C-5870 H H H H H 2-C(?O)OEt,3-Me 1 C-5871 H H H H H 2-C(?O)OEt,4-Me 1 C-5872 H H H H H 2-C(?O)OEt,5-Me 1 C-5873 H H H H H 2-C(?O)OEt,6-Me 1 C-5874 H H H H H 2-C(?O)NH.sub.2,3-F 1 C-5875 H H H H H 2-C(?O)NH.sub.2,4-F 1 C-5876 H H H H H 2-C(?O)NH.sub.2,5-F 1 C-5877 H H H H H 2-C(?O)NH.sub.2,6-F 1 C-5878 H H H H H 2-C(?O)NH.sub.2,3-Me 1 C-5879 H H H H H 2-C(?O)NH.sub.2,4-Me 1 C-5880 H H H H H 2-C(?O)NH.sub.2,5-Me 1 C-5881 H H H H H 2-C(?O)NH.sub.2,6-Me 1 C-5882 H H H H H 2-C(?O)NHMe,3-F 1 C-5883 H H H H H 2-C(?O)NHMe,4-F 1 C-5884 H H H H H 2-C(?O)NHMe,5-F 1 C-5885 H H H H H 2-C(?O)NHMe,6-F 1 C-5886 H H H H H 2-C(?O)NHMe,3-Me 1 C-5887 H H H H H 2-C(?O)NHMe,4-Me 1 C-5888 H H H H H 2-C(?O)NHMe,5-Me 1 C-5889 H H H H H 2-C(?O)NHMe,6-Me 1 C-5890 H H H H H 2-C(?O)NMe.sub.2,3-F 1 C-5891 H H H H H 2-C(?O)NMe.sub.2,4-F 1 C-5892 H H H H H 2-C(?O)NMe.sub.2,5-F 1 C-5893 H H H H H 2-C(?O)NMe.sub.2,6-F 1 C-5894 H H H H H 2-C(?O)NMe.sub.2,3-Me 1 C-5895 H H H H H 2-C(?O)NMe.sub.2,4-Me 1 C-5896 H H H H H 2-C(?O)NMe.sub.2,5-Me 1 C-5897 H H H H H 2-C(?O)NMe.sub.2,6-Me 1 C-5898 H H H H H 2-CH.sub.2OH,3-F 1 C-5899 H H H H H 2-CH.sub.2OH,4-F 1 C-5900 H H H H H 2-CH.sub.2OH,5-F 1 C-5901 H H H H H 2-CH.sub.2OH,6-F 1 C-5902 H H H H H 2-CH.sub.2OH,3-Me 1 C-5903 H H H H H 2-CH.sub.2OH,4-Me 1 C-5904 H H H H H 2-CH.sub.2OH,5-Me 1 C-5905 H H H H H 2-CH.sub.2OH,6-Me 1 C-5906 H H H H H 2-CH.sub.2OCH.sub.3,3-F 1 C-5907 H H H H H 2-CH.sub.2OCH.sub.3,4-F 1
(333) TABLE-US-00232 TABLE 232 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5908 H H H H H 2-CH.sub.2OCH.sub.3,5-F 1 C-5909 H H H H H 2-CH.sub.2OCH.sub.3,6-F 1 C-5910 H H H H H 2-CH.sub.2OCH.sub.3,3-Me 1 C-5911 H H H H H 2-CH.sub.2OCH.sub.3,4-Me 1 C-5912 H H H H H 2-CH.sub.2OCH.sub.3,5-Me 1 C-5913 H H H H H 2-CH.sub.2OCH.sub.3,6-Me 1 C-5914 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,3-F 1 C-5915 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,4-F 1 C-5916 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,5-F 1 C-5917 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-F 1 C-5918 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,3-Me 1 C-5919 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,4-Me 1 C-5920 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,5-Me 1 C-5921 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Me 1 C-5922 H H H H H 2-OC(?O)CH.sub.3,3-F 1 C-5923 H H H H H 2-OC(?O)CH.sub.3,4-F 1 C-5924 H H H H H 2-OC(?O)CH.sub.3,5-F 1 C-5925 H H H H H 2-OC(?O)CH.sub.3,6-F 1 C-5926 H H H H H 2-OC(?O)CH.sub.3,3-Me 1 C-5927 H H H H H 2-OC(?O)CH.sub.3,4-Me 1 C-5928 H H H H H 2-OC(?O)CH.sub.3,5-Me 1 C-5929 H H H H H 2-OC(?O)CH.sub.3,6-Me 1 C-5930 H H H H H 2-OS(?O).sub.2CH.sub.3,3-F 1 C-5931 H H H H H 2-OS(?O).sub.2CH.sub.3,4-F 1 C-5932 H H H H H 2-OS(?O).sub.2CH.sub.3,5-F 1 C-5933 H H H H H 2-OS(?O).sub.2CH.sub.3,6-F 1 C-5934 H H H H H 2-OS(?O).sub.2CH.sub.3,3-Me 1 C-5935 H H H H H 2-OS(?O).sub.2CH.sub.3,4-Me 1 C-5936 H H H H H 2-OS(?O).sub.2CH.sub.3,5-Me 1 C-5937 H H H H H 2-OS(?O).sub.2CH.sub.3,6-Me 1 C-5938 H H H H H 2-CH.sub.2SCH.sub.3,3-F 1 C-5939 H H H H H 2-CH.sub.2SCH.sub.3,4-F 1 C-5940 H H H H H 2-CH.sub.2SCH.sub.3,5-F 1 C-5941 H H H H H 2-CH.sub.2SCH.sub.3,6-F 1 C-5942 H H H H H 2-CH.sub.2SCH.sub.3,3-Me 1 C-5943 H H H H H 2-CH.sub.2SCH.sub.3,4-Me 1 C-5944 H H H H H 2-CH.sub.2SCH.sub.3,5-Me 1 C-5945 H H H H H 2-CH.sub.2SCH.sub.3,6-Me 1 C-5946 H H H H H 2-CH.sub.2SCF.sub.3,3-F 1 C-5947 H H H H H 2-CH.sub.2SCF.sub.3,4-F 1 C-5948 H H H H H 2-CH.sub.2SCF.sub.3,5-F 1 C-5949 H H H H H 2-CH.sub.2SCF.sub.3,6-F 1 C-5950 H H H H H 2-CH.sub.2SCF.sub.3,3-Me 1 C-5951 H H H H H 2-CH.sub.2SCF.sub.3,4-Me 1 C-5952 H H H H H 2-CH.sub.2SCF.sub.3,5-Me 1 C-5953 H H H H H 2-CH.sub.2SCF.sub.3,6-Me 1 C-5954 H H H H H 2-(benzyloxy),3-F 1 C-5955 H H H H H 2-(benzyloxy),4-F 1 C-5956 H H H H H 2-(benzyloxy),5-F 1 C-5957 H H H H H 2-(benzyloxy),6-F 1 C-5958 H H H H H 2-(benzyloxy),3-Me 1 C-5959 H H H H H 2-(benzyloxy),4-Me 1 C-5960 H H H H H 2-(benzyloxy),5-Me 1 C-5961 H H H H H 2-(benzyloxy),6-Me 1 C-5962 H H H H H 2-NH.sub.2,3-F 1 C-5963 H H H H H 2-NH.sub.2,4-F 1 C-5964 H H H H H 2-NH.sub.2,5-F 1
(334) TABLE-US-00233 TABLE 233 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-5965 H H H H H 2-NH.sub.2,6-F 1 C-5966 H H H H H 2-NH.sub.2,3-Me 1 C-5967 H H H H H 2-NH.sub.2,4-Me 1 C-5968 H H H H H 2-NH.sub.2,5-Me 1 C-5969 H H H H H 2-NH.sub.2,6-Me 1 C-5970 H H H H H 2-NHMe,3-F 1 C-5971 H H H H H 2-NHMe,4-F 1 C-5972 H H H H H 2-NHMe,5-F 1 C-5973 H H H H H 2-NHMe,6-F 1 C-5974 H H H H H 2-NHMe,3-Me 1 C-5975 H H H H H 2-NHMe,4-Me 1 C-5976 H H H H H 2-NHMe,5-Me 1 C-5977 H H H H H 2-NHMe,6-Me 1 C-5978 H H H H H 2-NHEt,3-F 1 C-5979 H H H H H 2-NHEt,4-F 1 C-5980 H H H H H 2-NHEt,5-F 1 C-5981 H H H H H 2-NHEt,6-F 1 C-5982 H H H H H 2-NHEt,3-Me 1 C-5983 H H H H H 2-NHEt,4-Me 1 C-5984 H H H H H 2-NHEt,5-Me 1 C-5985 H H H H H 2-NHEt,6-Me 1 C-5986 H H H H H 2-NMe.sub.2,3-F 1 C-5987 H H H H H 2-NMe.sub.2,4-F 1 C-5988 H H H H H 2-NMe.sub.2,5-F 1 C-5989 H H H H H 2-NMe.sub.2,6-F 1 C-5990 H H H H H 2-NMe.sub.2,3-Me 1 C-5991 H H H H H 2-NMe.sub.2,4-Me 1 C-5992 H H H H H 2-NMe.sub.2,5-Me 1 C-5993 H H H H H 2-NMe.sub.2,6-Me 1 C-5994 H H H H H 2-NEt.sub.2,3-F 1 C-5995 H H H H H 2-NEt.sub.2,4-F 1 C-5996 H H H H H 2-NEt.sub.2,5-F 1 C-5997 H H H H H 2-NEt.sub.2,6-F 1 C-5998 H H H H H 2-NEt.sub.2,3-Me 1 C-5999 H H H H H 2-NEt.sub.2,4-Me 1 C-6000 H H H H H 2-NEt.sub.2,5-Me 1 C-6001 H H H H H 2-NEt.sub.2,6-Me 1 C-6002 H H H H H 2-CHO,3-F 1 C-6003 H H H H H 2-CHO,4-F 1 C-6004 H H H H H 2-CHO,5-F 1 C-6005 H H H H H 2-CHO,6-F 1 C-6006 H H H H H 2-CHO,3-Me 1 C-6007 H H H H H 2-CHO,4-Me 1 C-6008 H H H H H 2-CHO,5-Me 1 C-6009 H H H H H 2-CHO,6-Me 1 C-6010 H H H H H 2-C(?O)OH,3-F 1 C-6011 H H H H H 2-C(?O)OH,4-F 1 C-6012 H H H H H 2-C(?O)OH,5-F 1 C-6013 H H H H H 2-C(?O)OH,6-F 1 C-6014 H H H H H 2-C(?O)OH,3-Me 1 C-6015 H H H H H 2-C(?O)OH,4-Me 1 C-6016 H H H H H 2-C(?O)OH,5-Me 1 C-6017 H H H H H 2-C(?O)OH,6-Me 1 C-6018 H H H H H 2-(1,3-dioxolan-2-yl),3-F 1 C-6019 H H H H H 2-(1,3-dioxolan-2-yl),4-F 1 C-6020 H H H H H 2-(1,3-dioxolan-2-yl),5-F 1 C-6021 H H H H H 2-(1,3-dioxolan-2-yl),6-F 1
(335) TABLE-US-00234 TABLE 234 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-6022 H H H H H 2-(1,3-dioxolan-2-yl),3-Me 1 C-6023 H H H H H 2-(1,3-dioxolan-2-yl),4-Me 1 C-6024 H H H H H 2-(1,3-dioxolan-2-yl),5-Me 1 C-6025 H H H H H 2-(1,3-dioxolan-2-yl),6-Me 1 C-6026 H H H H H 2-(1,3-dioxan-2-yl),3-F 1 C-6027 H H H H H 2-(1,3-dioxan-2-yl),4-F 1 C-6028 H H H H H 2-(1,3-dioxan-2-yl),5-F 1 C-6029 H H H H H 2-(1,3-dioxan-2-yl),6-F 1 C-6030 H H H H H 2-(1,3-dioxan-2-yl),3-Me 1 C-6031 H H H H H 2-(1,3-dioxan-2-yl),4-Me 1 C-6032 H H H H H 2-(1,3-dioxan-2-yl),5-Me 1 C-6033 H H H H H 2-(1,3-dioxan-2-yl),6-Me 1 C-6034 H H H H H 2-(thiazol-2-yl),3-F 1 C-6035 H H H H H 2-(thiazol-2-yl),4-F 1 C-6036 H H H H H 2-(thiazol-2-yl),5-F 1 C-6037 H H H H H 2-(thiazol-2-yl),6-F 1 C-6038 H H H H H 2-(thiazol-2-yl),3-Me 1 C-6039 H H H H H 2-(thiazol-2-yl),4-Me 1 C-6040 H H H H H 2-(thiazol-2-yl),5-Me 1 C-6041 H H H H H 2-(thiazol-2-yl),6-Me 1 C-6042 H H H H H 2-(oxazol-2-yl),3-F 1 C-6043 H H H H H 2-(oxazol-2-yl),4-F 1 C-6044 H H H H H 2-(oxazol-2-yl),5-F 1 C-6045 H H H H H 2-(oxazol-2-yl),6-F 1 C-6046 H H H H H 2-(oxazol-2-yl),3-Me 1 C-6047 H H H H H 2-(oxazol-2-yl),4-Me 1 C-6048 H H H H H 2-(oxazol-2-yl),5-Me 1 C-6049 H H H H H 2-(oxazol-2-yl),6-Me 1 C-6050 H H H H H 2-CH?NOH,3-F 1 C-6051 H H H H H 2-CH?NOH,4-F 1 C-6052 H H H H H 2-CH?NOH,5-F 1 C-6053 H H H H H 2-CH?NOH,6-F 1 C-6054 H H H H H 2-CH?NOH,3-Me 1 C-6055 H H H H H 2-CH?NOH,4-Me 1 C-6056 H H H H H 2-CH?NOH,5-Me 1 C-6057 H H H H H 2-CH?NOH,6-Me 1 C-6058 H H H H H 2-CH?NOMe,3-F 1 C-6059 H H H H H 2-CH?NOMe,4-F 1 C-6060 H H H H H 2-CH?NOMe,5-F 1 C-6061 H H H H H 2-CH?NOMe,6-F 1 C-6062 H H H H H 2-CH?NOMe,3-Me 1 C-6063 H H H H H 2-CH?NOMe,4-Me 1 C-6064 H H H H H 2-CH?NOMe,5-Me 1 C-6065 H H H H H 2-CH?NOMe,6-Me 1 C-6066 H H H H H 2-CN,3-F 1 C-6067 H H H H H 2-CN,4-F 1 C-6068 H H H H H 2-CN,5-F 1 C-6069 H H H H H 2-CN,6-F 1 C-6070 H H H H H 2-CN,3-Cl 1 C-6071 H H H H H 2-CN,4-Cl 1 C-6072 H H H H H 2-CN,5-Cl 1 C-6073 H H H H H 2-CN,6-Cl 1 C-6074 H H H H H 2-CN,3-Me 1 C-6075 H H H H H 2-CN,4-Me 1 C-6076 H H H H H 2-CN,5-Me 1 C-6077 H H H H H 2-CN,6-Me 1 C-6078 H H H H H 2-CN,3-OMe 1
(336) TABLE-US-00235 TABLE 235 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-6079 H H H H H 2-CN,4-OMe 1 C-6080 H H H H H 2-CN,5-OMe 1 C-6081 H H H H H 2-CN,6-OMe 1 C-6082 H H H H H 3-CN,2-F 1 C-6083 H H H H H 3-CN,4-F 1 C-6084 H H H H H 3-CN,5-F 1 C-6085 H H H H H 3-CN,6-F 1 C-6086 H H H H H 3-CN,2-Cl 1 C-6087 H H H H H 3-CN,4-Cl 1 C-6088 H H H H H 3-CN,5-Cl 1 C-6089 H H H H H 3-CN,6-Cl 1 C-6090 H H H H H 3-CN,2-Me 1 C-6091 H H H H H 3-CN,4-Me 1 C-6092 H H H H H 3-CN,5-Me 1 C-6093 H H H H H 3-CN,6-Me 1 C-6094 H H H H H 3-CN,2-OMe 1 C-6095 H H H H H 3-CN,4-OMe 1 C-6096 H H H H H 3-CN,5-OMe 1 C-6097 H H H H H 3-CN,6-OMe 1 C-6098 H H H H H 4-CN,2-F 1 C-6099 H H H H H 4-CN,3-F 1 C-6100 H H H H H 4-CN,2-Cl 1 C-6101 H H H H H 4-CN,3-Cl 1 C-6102 H H H H H 4-CN,2-Me 1 C-6103 H H H H H 4-CN,3-Me 1 C-6104 H H H H H 4-CN,2-OMe 1 C-6105 H H H H H 4-CN,3-OMe 1 C-6106 H H H H H 2-NO.sub.2,3-F 1 C-6107 H H H H H 2-NO.sub.2,4-F 1 C-6108 H H H H H 2-NO.sub.2,5-F 1 C-6109 H H H H H 2-NO.sub.2,6-F 1 C-6110 H H H H H 2-NO.sub.2,3-Me 1 C-6111 H H H H H 2-NO.sub.2,4-Me 1 C-6112 H H H H H 2-NO.sub.2,5-Me 1 C-6113 H H H H H 2-NO.sub.2,6-Me 1 C-6114 H H H H H 2-Me,3,4-F.sub.2 1 C-6115 H H H H H 2-Me,3,5-F.sub.2 1 C-6116 H H H H H 2-Me,3,6-F.sub.2 1 C-6117 H H H H H 2-Me,4,5-F.sub.2 1 C-6118 H H H H H 2-OMe,3,4-F.sub.2 1 C-6119 H H H H H 2-OMe,3,5-F.sub.2 1 C-6120 H H H H H 2-OMe,3,6-F.sub.2 1 C-6121 H H H H H 2-OMe,4,5-F.sub.2 1 C-6122 H H H H H 2-(CH.sub.2).sub.3-3 1 C-6123 H H H H H 2-(CH.sub.2).sub.4-3 1 C-6124 H H H H H 2-(OCH.sub.2CH.sub.2)-3 1 C-6125 H H H H H 2-(OCH.sub.2CH.sub.2CH.sub.2)-3 1 C-6126 H H H H H 2-(CH.sub.2CH.sub.2O)-3 1 C-6127 H H H H H 2-(CH.sub.2CH.sub.2CH.sub.2O)-3 1 C-6128 H H H H H 3-(CH.sub.2).sub.3-4 1 C-6129 H H H H H 3-(CH.sub.2).sub.4-4 1 C-6130 H H H H H 3-(OCH.sub.2CH.sub.2)-4 1 C-6131 H H H H H 3-(OCH.sub.2CH.sub.2CH.sub.2)-4 1 C-6132 H H H H H 3-(CH.sub.2CH.sub.2O)-4 1 C-6133 H H H H H 3-(CH.sub.2CH.sub.2CH.sub.2O)-4 1 C-6134 H H H H H 2-(OCH.sub.2O)-3 1 C-6135 H H H H H 3-(OCH.sub.2O)-4 1
(337) TABLE-US-00236 TABLE 236 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p C-6136 H H H H H 2-(OCH.sub.2CH.sub.2O)-3 1 C-6137 H H H H H 3-(OCH.sub.2CH.sub.2O)-4 1 C-6138 H H H H H 2-(OCF.sub.2O)-3 1 C-6139 H H H H H 3-(OCF.sub.2O)-4 1 C-6140 H H H H H 2-Me,6-Et 1 C-6141 H H H H H 2-Me,4,5-F.sub.2 1 C-6142 H H H H H 2-cyclopropyl,6-OMe 1 C-6143 H H H H H 2-Me,5-Et 1 C-6144 H H H H H 2,6-Et.sub.2 1 C-6145 H H H H H 2-Et,6-F 1 C-6146 H H H H H 2-CH.sub.2OCH.sub.3,6-Cl 1 C-6147 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 1 C-6148 H H H H H 2-CH.sub.2NMe.sub.2 1
(338) TABLE-US-00237 TABLE 237
(339) TABLE-US-00238 TABLE 238 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-0053 H H H H H 3-F-4-Cl-pyridin-2-yl 0 D-0054 H H H H H 3-F-5-Cl-pyridin-2-yl 0 D-0055 H H H H H 3-F-6-Cl-pyridin-2-yl 0 D-0056 H H H H H 3-F-4-Me-pyridin-2-yl 0 D-0057 H H H H H 3-F-5-Me-pyridin-2-yl 0 D-0058 H H H H H 3-F-6-Me-pyridin-2-yl 0 D-0059 H H H H H 3-F-4-OMe-pyridin-2-yl 0 D-0060 H H H H H 3-F-5-OMe-pyridin-2-yl 0 D-0061 H H H H H 3-F-6-OMe-pyridin-2-yl 0 D-0062 H H H H H 3-Cl-4-F-pyridin-2-yl 0 D-0063 H H H H H 3-Cl-5-F-pyridin-2-yl 0 D-0064 H H H H H 3-Cl-6-F-pyridin-2-yl 0 D-0065 H H H H H 3-Cl-4-Me-pyridin-2-yl 0 D-0066 H H H H H 3-Cl-5-Me-pyridin-2-yl 0 D-0067 H H H H H 3-Cl-6-Me-pyridin-2-yl 0 D-0068 H H H H H 3-Me-4-F-pyridin-2-yl 0 D-0069 H H H H H 3-Me-5-F-pyridin-2-yl 0 D-0070 H H H H H 3-Me-6-F-pyridin-2-yl 0 D-0071 H H H H H 3-Me-4-Cl-pyridin-2-yl 0 D-0072 H H H H H 3-Me-5-Cl-pyridin-2-yl 0 D-0073 H H H H H 3-Me-6-Cl-pyridin-2-yl 0 D-0074 H H H H H 3,4-(Me).sub.2-pyridin-2-yl 0 D-0075 H H H H H 3,5-(Me).sub.2-pyridin-2-yl 0 D-0076 H H H H H 3,6-(Me).sub.2-pyridin-2-yl 0 D-0077 H H H H H 3-Me-4-OMe-pyridin-2-yl 0 D-0078 H H H H H 3-Me-5-OMe-pyridin-2-yl 0 D-0079 H H H H H 3-Me-6-OMe-pyridin-2-yl 0 D-0080 H H H H H 3-CF.sub.3-4-F-pyridin-2-yl 0 D-0081 H H H H H 3-CF.sub.3-5-F-pyridin-2-yl 0 D-0082 H H H H H 3-CF.sub.3-6-F-pyridin-2-yl 0 D-0083 H H H H H 3-CF.sub.3-4-Me-pyridin-2-yl 0 D-0084 H H H H H 3-CF.sub.3-5-Me-pyridin-2-yl 0 D-0085 H H H H H 3-CF.sub.3-6-Me-pyridin-2-yl 0 D-0086 H H H H H 3-OMe-4-F-pyridin-2-yl 0 D-0087 H H H H H 3-OMe-5-F-pyridin-2-yl 0 D-0088 H H H H H 3-OMe-6-F-pyridin-2-yl 0 D-0089 H H H H H 3-OMe-4-Cl-pyridin-2-yl 0 D-0090 H H H H H 3-OMe-5-Cl-pyridin-2-yl 0 D-0091 H H H H H 3-OMe-6-Cl-pyridin-2-yl 0 D-0092 H H H H H 3-OMe-4-Me-pyridin-2-yl 0 D-0093 H H H H H 3-OMe-5-Me-pyridin-2-yl 0 D-0094 H H H H H 3-OMe-6-Me-pyridin-2-yl 0 D-0095 H H H H H 3,4-(OMe).sub.2-pyridin-2-yl 0 D-0096 H H H H H 3,5-(OMe).sub.2-pyridin-2-yl 0 D-0097 H H H H H 3,6-(OMe).sub.2-pyridin-2-yl 0 D-0098 H H H H H pyridin-3-yl 0 D-0099 H H H H H 2-F-pyridin-3-yl 0 D-0100 H H H H H 4-F-pyridin-3-yl 0 D-0101 H H H H H 5-F-pyridin-3-yl 0 D-0102 H H H H H 6-F-pyridin-3-yl 0 D-0103 H H H H H 2-Cl-pyridin-3-yl 0 D-0104 H H H H H 4-Cl-pyridin-3-yl 0 D-0105 H H H H H 5-Cl-pyridin-3-yl 0 D-0106 H H H H H 6-Cl-pyridin-3-yl 0 D-0107 H H H H H 2-Me-pyridin-3-yl 0 D-0108 H H H H H 4-Me-pyridin-3-yl 0 D-0109 H H H H H 5-Me-pyridin-3-yl 0
(340) TABLE-US-00239 TABLE 239 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-0110 H H H H H 6-Me-pyridin-3-yl 0 D-0111 H H H H H 2-CF.sub.3-pyridin-3-yl 0 D-0112 H H H H H 4-CF.sub.3-pyridin-3-yl 0 D-0113 H H H H H 5-CF.sub.3-pyridin-3-yl 0 D-0114 H H H H H 6-CF.sub.3-pyridin-3-yl 0 D-0115 H H H H H 2-OMe-pyridin-3-yl 0 D-0116 H H H H H 4-OMe-pyridin-3-yl 0 D-0117 H H H H H 5-OMe-pyridin-3-yl 0 D-0118 H H H H H 6-OMe-pyridin-3-yl 0 D-0119 H H H H H 2,4-F.sub.2-pyridin-3-yl 0 D-0120 H H H H H 2,5-F.sub.2-pyridin-3-yl 0 D-0121 H H H H H 2,6-F.sub.2-pyridin-3-yl 0 D-0122 H H H H H 4,5-F.sub.2-pyridin-3-yl 0 D-0123 H H H H H 4,6-F.sub.2-pyridin-3-yl 0 D-0124 H H H H H 2,4-Cl.sub.2-pyridin-3-yl 0 D-0125 H H H H H 2,5-Cl.sub.2-pyridin-3-yl 0 D-0126 H H H H H 2,6-Cl.sub.2-pyridin-3-yl 0 D-0127 H H H H H 4,5-Cl.sub.2-pyridin-3-yl 0 D-0128 H H H H H 4,6-Cl.sub.2-pyridin-3-yl 0 D-0129 H H H H H 2-F-4-Cl-pyridin-3-yl 0 D-0130 H H H H H 2-F-5-Cl-pyridin-3-yl 0 D-0131 H H H H H 2-F-6-Cl-pyridin-3-yl 0 D-0132 H H H H H 4-F-2-Cl-pyridin-3-yl 0 D-0133 H H H H H 4-F-5-Cl-pyridin-3-yl 0 D-0134 H H H H H 4-F-6-Cl-pyridin-3-yl 0 D-0135 H H H H H 2-F-4-Me-pyridin-3-yl 0 D-0136 H H H H H 2-F-5-Me-pyridin-3-yl 0 D-0137 H H H H H 2-F-6-Me-pyridin-3-yl 0 D-0138 H H H H H 4-F-2-Me-pyridin-3-yl 0 D-0139 H H H H H 4-F-5-Me-pyridin-3-yl 0 D-0140 H H H H H 4-F-6-Me-pyridin-3-yl 0 D-0141 H H H H H 2-F-4-OMe-pyridin-3-yl 0 D-0142 H H H H H 2-F-5-OMe-pyridin-3-yl 0 D-0143 H H H H H 2-F-6-OMe-pyridin-3-yl 0 D-0144 H H H H H 4-F-2-OMe-pyridin-3-yl 0 D-0145 H H H H H 4-F-5-OMe-pyridin-3-yl 0 D-0146 H H H H H 4-F-6-OMe-pyridin-3-yl 0 D-0147 H H H H H 2-Cl-5-F-pyridin-3-yl 0 D-0148 H H H H H 2-Cl-6-F-pyridin-3-yl 0 D-0149 H H H H H 4-Cl-5-F-pyridin-3-yl 0 D-0150 H H H H H 4-Cl-6-F-pyridin-3-yl 0 D-0151 H H H H H 2-Cl-4-Me-pyridin-3-yl 0 D-0152 H H H H H 2-Cl-5-Me-pyridin-3-yl 0 D-0153 H H H H H 2-Cl-6-Me-pyridin-3-yl 0 D-0154 H H H H H 4-Cl-2-Me-pyridin-3-yl 0 D-0155 H H H H H 4-Cl-5-Me-pyridin-3-yl 0 D-0156 H H H H H 4-Cl-6-Me-pyridin-3-yl 0 D-0157 H H H H H 2-Me-5-F-pyridin-3-yl 0 D-0158 H H H H H 2-Me-6-F-pyridin-3-yl 0 D-0159 H H H H H 4-Me-5-F-pyridin-3-yl 0 D-0160 H H H H H 4-Me-6-F-pyridin-3-yl 0 D-0161 H H H H H 2-Me-5-Cl-pyridin-3-yl 0 D-0162 H H H H H 2-Me-6-Cl-pyridin-3-yl 0 D-0163 H H H H H 4-Me-5-Cl-pyridin-3-yl 0 D-0164 H H H H H 4-Me-6-Cl-pyridin-3-yl 0 D-0165 H H H H H 2,4-(Me).sub.2-pyridin-3-yl 0 D-0166 H H H H H 2,5-(Me).sub.2-pyridin-3-yl 0
(341) TABLE-US-00240 TABLE 240 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-0167 H H H H H 2,6-(Me).sub.2-pyridin-3-yl 0 D-0168 H H H H H 4,5-(Me).sub.2-pyridin-3-yl 0 D-0169 H H H H H 4,6-(Me).sub.2-pyridin-3-yl 0 D-0170 H H H H H 2-Me-4-OMe-pyridin-3-yl 0 D-0171 H H H H H 2-Me-5-OMe-pyridin-3-yl 0 D-0172 H H H H H 2-Me-6-OMe-pyridin-3-yl 0 D-0173 H H H H H 4-Me-2-OMe-pyridin-3-yl 0 D-0174 H H H H H 4-Me-5-OMe-pyridin-3-yl 0 D-0175 H H H H H 4-Me-6-OMe-pyridin-3-yl 0 D-0176 H H H H H 2-CF.sub.3-4-F-pyridin-3-yl 0 D-0177 H H H H H 2-CF.sub.3-5-F-pyridin-3-yl 0 D-0178 H H H H H 2-CF.sub.3-6-F-pyridin-3-yl 0 D-0179 H H H H H 4-CF.sub.3-2-F-pyridin-3-yl 0 D-0180 H H H H H 4-CF.sub.3-5-F-pyridin-3-yl 0 D-0181 H H H H H 4-CF.sub.3-6-F-pyridin-3-yl 0 D-0182 H H H H H 2-CF.sub.3-4-Me-pyridin-3-yl 0 D-0183 H H H H H 2-CF.sub.3-5-Me-pyridin-3-yl 0 D-0184 H H H H H 2-CF.sub.3-6-Me-pyridin-3-yl 0 D-0185 H H H H H 4-CF.sub.3-2-Me-pyridin-3-yl 0 D-0186 H H H H H 4-CF.sub.3-5-Me-pyridin-3-yl 0 D-0187 H H H H H 4-CF.sub.3-6-Me-pyridin-3-yl 0 D-0188 H H H H H 2-OMe-5-F-pyridin-3-yl 0 D-0189 H H H H H 2-OMe-6-F-pyridin-3-yl 0 D-0190 H H H H H 4-OMe-5-F-pyridin-3-yl 0 D-0191 H H H H H 4-OMe-6-F-pyridin-3-yl 0 D-0192 H H H H H 2-OMe-4-Cl-pyridin-3-yl 0 D-0193 H H H H H 2-OMe-5-Cl-pyridin-3-yl 0 D-0194 H H H H H 2-OMe-6-Cl-pyridin-3-yl 0 D-0195 H H H H H 4-OMe-2-Cl-pyridin-3-yl 0 D-0196 H H H H H 4-OMe-5-Cl-pyridin-3-yl 0 D-0197 H H H H H 4-OMe-6-Cl-pyridin-3-yl 0 D-0198 H H H H H 2-OMe-5-Me-pyridin-3-yl 0 D-0199 H H H H H 2-OMe-6-Me-pyridin-3-yl 0 D-0200 H H H H H 4-OMe-5-Me-pyridin-3-yl 0 D-0201 H H H H H 4-OMe-6-Me-pyridin-3-yl 0 D-0202 H H H H H 2,4-(OMe).sub.2-pyridin-3-yl 0 D-0203 H H H H H 2,5-(OMe).sub.2-pyridin-3-yl 0 D-0204 H H H H H 2,6-(OMe).sub.2-pyridin-3-yl 0 D-0205 H H H H H 4,5-(OMe).sub.2-pyridin-3-yl 0 D-0206 H H H H H 4,6-(OMe).sub.2-pyridin-3-yl 0 D-0207 H H H H H pyridin-4-yl 0 D-0208 H H H H H 2-F-pyridin-4-yl 0 D-0209 H H H H H 3-F-pyridin-4-yl 0 D-0210 H H H H H 2-Cl-pyridin-4-yl 0 D-0211 H H H H H 3-Cl-pyridin-4-yl 0 D-0212 H H H H H 2-Me-pyridin-4-yl 0 D-0213 H H H H H 3-Me-pyridin-4-yl 0 D-0214 H H H H H 2-CF.sub.3-pyridin-4-yl 0 D-0215 H H H H H 3-CF.sub.3-pyridin-4-yl 0 D-0216 H H H H H 2-OMe-pyridin-4-yl 0 D-0217 H H H H H 3-OMe-pyridin-4-yl 0 D-0218 H H H H H 2,3-F.sub.2-pyridin-4-yl 0 D-0219 H H H H H 2,5-F.sub.2-pyridin-4-yl 0 D-0220 H H H H H 2,6-F.sub.2-pyridin-4-yl 0 D-0221 H H H H H 3,5-F.sub.2-pyridin-4-yl 0 D-0222 H H H H H 2,3-Cl.sub.2-pyridin-4-yl 0 D-0223 H H H H H 2,5-Cl.sub.2-pyridin-4-yl 0
(342) TABLE-US-00241 TABLE 241 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-0224 H H H H H 2,6-Cl.sub.2-pyridin-4-yl 0 D-0225 H H H H H 3,5-Cl.sub.2-pyridin-4-yl 0 D-0226 H H H H H 3-F-2-Cl-pyridin-4-yl 0 D-0227 H H H H H 3-F-5-Cl-pyridin-4-yl 0 D-0228 H H H H H 3-F-6-Cl-pyridin-4-yl 0 D-0229 H H H H H 3-F-2-Me-pyridin-4-yl 0 D-0230 H H H H H 3-F-5-Me-pyridin-4-yl 0 D-0231 H H H H H 3-F-6-Me-pyridin-4-yl 0 D-0232 H H H H H 3-F-2-OMe-pyridin-4-yl 0 D-0233 H H H H H 3-F-5-OMe-pyridin-4-yl 0 D-0234 H H H H H 3-F-6-OMe-pyridin-4-yl 0 D-0235 H H H H H 3-Cl-2-F-pyridin-4-yl 0 D-0236 H H H H H 3-Cl-6-F-pyridin-4-yl 0 D-0237 H H H H H 3-Cl-2-Me-pyridin-4-yl 0 D-0238 H H H H H 3-Cl-5-Me-pyridin-4-yl 0 D-0239 H H H H H 3-Cl-6-Me-pyridin-4-yl 0 D-0240 H H H H H 3-Me-2-F-pyridin-4-yl 0 D-0241 H H H H H 3-Me-6-F-pyridin-4-yl 0 D-0242 H H H H H 3-Me-2-Cl-pyridin-4-yl 0 D-0243 H H H H H 3-Me-6-Cl-pyridin-4-yl 0 D-0244 H H H H H 2,3-(Me).sub.2-pyridin-4-yl 0 D-0245 H H H H H 3,5-(Me).sub.2-pyridin-4-yl 0 D-0246 H H H H H 3,6-(Me).sub.2-pyridin-4-yl 0 D-0247 H H H H H 3-Me-2-OMe-pyridin-4-yl 0 D-0248 H H H H H 3-Me-5-OMe-pyridin-4-yl 0 D-0249 H H H H H 3-Me-6-OMe-pyridin-4-yl 0 D-0250 H H H H H 3-CF.sub.3-2-F-pyridin-4-yl 0 D-0251 H H H H H 3-CF.sub.3-5-F-pyridin-4-yl 0 D-0252 H H H H H 3-CF.sub.3-6-F-pyridin-4-yl 0 D-0253 H H H H H 3-CF.sub.3-2-Me-pyridin-4-yl 0 D-0254 H H H H H 3-CF.sub.3-5-Me-pyridin-4-yl 0 D-0255 H H H H H 3-CF.sub.3-6-Me-pyridin-4-yl 0 D-0256 H H H H H 3-OMe-2-F-pyridin-4-yl 0 D-0257 H H H H H 3-OMe-6-F-pyridin-4-yl 0 D-0258 H H H H H 3-OMe-2-Cl-pyridin-4-yl 0 D-0259 H H H H H 3-OMe-5-Cl-pyridin-4-yl 0 D-0260 H H H H H 3-OMe-6-Cl-pyridin-4-yl 0 D-0261 H H H H H 3-OMe-2-Me-pyridin-4-yl 0 D-0262 H H H H H 3-OMe-6-Me-pyridin-4-yl 0 D-0263 H H H H H 2,3-(OMe).sub.2-pyridin-4-yl 0 D-0264 H H H H H 3,5-(OMe).sub.2-pyridin-4-yl 0 D-0265 H H H H H 3,6-(OMe).sub.2-pyridin-4-yl 0 D-0266 H H H H H pyrimidin-2-yl 0 D-0267 H H H H H pyrimidin-4-yl 0 D-0268 H H H H H 5-F-pyrimidin-4-yl 0 D-0269 H H H H H 5-Me-pyrimidin-4-yl 0 D-0270 H H H H H 5-CF.sub.3-pyrimidin-4-yl 0 D-0271 H H H H H 5-OMe-pyrimidin-4-yl 0 D-0272 H H H H H pyrimidin-5-yl 0 D-0273 H H H H H 4-F-pyrimidin-5-yl 0 D-0274 H H H H H 4-Cl-pyrimidin-5-yl 0 D-0275 H H H H H 4-Me-pyrimidin-5-yl 0 D-0276 H H H H H 4-CF.sub.3-pyrimidin-5-yl 0 D-0277 H H H H H 4-OMe-pyrimidin-5-yl 0 D-0278 H H H H H pyridazin-3-yl 0 D-0279 H H H H H 4-F-pyridazin-3-yl 0 D-0280 H H H H H 4-Cl-pyridazin-3-yl 0
(343) TABLE-US-00242 TABLE 242 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-0281 H H H H H 4-Me-pyridazin-3-yl 0 D-0282 H H H H H 4-CF.sub.3-pyridazin-3-yl 0 D-0283 H H H H H 4-OMe-pyridazin-3-yl 0 D-0284 H H H H H pyridazin-4-yl 0 D-0285 H H H H H 3-F-pyridazin-4-yl 0 D-0286 H H H H H 3-Cl-pyridazin-4-yl 0 D-0287 H H H H H 3-Me-pyridazin-4-yl 0 D-0288 H H H H H 3-CF.sub.3-pyridazin-4-yl 0 D-0289 H H H H H 3-OMe-pyridazin-4-yl 0 D-0290 H H H H H 5-F-pyridazin-4-yl 0 D-0291 H H H H H 5-Cl-pyridazin-4-yl 0 D-0292 H H H H H 5-Me-pyridazin-4-yl 0 D-0293 H H H H H 5-CF.sub.3-pyridazin-4-yl 0 D-0294 H H H H H 5-OMe-pyridazin-4-yl 0 D-0295 H H H H H thiophen-2-yl 0 D-0296 H H H H H 3-F-thiophen-2-yl 0 D-0297 H H H H H 3-Cl-thiophen-2-yl 0 D-0298 H H H H H 3-Me-thiophen-2-yl 0 D-0299 H H H H H 3-CF.sub.3-thiophen-2-yl 0 D-0300 H H H H H 3-OMe-thiophen-2-yl 0 D-0301 H H H H H thiophen-3-yl 0 D-0302 H H H H H 2-F-thiophen-3-yl 0 D-0303 H H H H H 2-Cl-thiophen-3-yl 0 D-0304 H H H H H 2-Me-thiophen-3-yl 0 D-0305 H H H H H 2-CF.sub.3-thiophen-3-yl 0 D-0306 H H H H H 2-OMe-thiophen-3-yl 0 D-0307 H H H H H 4-F-thiophen-3-yl 0 D-0308 H H H H H 4-Cl-thiophen-3-yl 0 D-0309 H H H H H 4-Me-thiophen-3-yl 0 D-0310 H H H H H 4-CF.sub.3-thiophen-3-yl 0 D-0311 H H H H H 4-OMe-thiophen-3-yl 0 D-0312 H H H H H thiazol-2-yl 0 D-0313 H H H H H thiazol-4-yl 0 D-0314 H H H H H 5-F-thiazol-4-yl 0 D-0315 H H H H H 5-Me-thiazol-4-yl 0 D-0316 H H H H H 5-CF.sub.3-thiazol-4-yl 0 D-0317 H H H H H 5-OMe-thiazol-4-yl 0 D-0318 H H H H H thiazol-5-yl 0 D-0319 H H H H H 4-F-thiazol-5-yl 0 D-0320 H H H H H 4-Me-thiazol-5-yl 0 D-0321 H H H H H 4-CF.sub.3-thiazol-5-yl 0 D-0322 H H H H H 4-OMe-thiazol-5-yl 0 D-0323 H H H H H 1H-pyrrol-1-yl 0 D-0324 H H H H H 2-F-1H-pyrrol-1-yl 0 D-0325 H H H H H 2-Me-1H-pyrrol-1-yl 0 D-0326 H H H H H 2-CF.sub.3-1H-pyrrol-1-yl 0 D-0327 H H H H H 2-OMe-1H-pyrrol-1-yl 0 D-0328 H H H H H 1H-pyrrol-2-yl 0 D-0329 H H H H H 1-Me-1H-pyrrol-2-yl 0 D-0330 H H H H H 3-F-1H-pyrrol-2-yl 0 D-0331 H H H H H 3-Me-1H-pyrrol-2-yl 0 D-0332 H H H H H 3-CF.sub.3-1H-pyrrol-2-yl 0 D-0333 H H H H H 3-OMe-1H-pyrrol-2-yl 0 D-0334 H H H H H 1-Me-3-F-1H-pyrrol-2-yl 0 D-0335 H H H H H 1,3-(Me).sub.2-1H-pyrrol-2-yl 0 D-0336 H H H H H 1-Me-3-CF.sub.3-1H-pyrrol-2-yl 0 D-0337 H H H H H 1-Me-3-OMe-1H-pyrrol-2-yl 0
(344) TABLE-US-00243 TABLE 243 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-0338 H H H H H 1H-pyrrol-3-yl 0 D-0339 H H H H H 1-Me-1H-pyrrol-3-yl 0 D-0340 H H H H H 2-F-1H-pyrrol-3-yl 0 D-0341 H H H H H 2-Me-1H-pyrrol-3-yl 0 D-0342 H H H H H 2-CF.sub.3-1H-pyrrol-3-yl 0 D-0343 H H H H H 2-OMe-1H-pyrrol-3-yl 0 D-0344 H H H H H 1-Me-2-F-1H-pyrrol-3-yl 0 D-0345 H H H H H 1,2-(Me).sub.2-1H-pyrrol-3-yl 0 D-0346 H H H H H 1-Me-2-CF.sub.3-1H-pyrrol-3-yl 0 D-0347 H H H H H 1-Me-2-OMe-1H-pyrrol-3-yl 0 D-0348 H H H H H 4-F-1H-pyrrol-3-yl 0 D-0349 H H H H H 4-Me-1H-pyrrol-3-yl 0 D-0350 H H H H H 4-CF.sub.3-1H-pyrrol-3-yl 0 D-0351 H H H H H 4-OMe-1H-pyrrol-3-yl 0 D-0352 H H H H H 1-Me-4-F-1H-pyrrol-3-yl 0 D-0353 H H H H H 1,4-(Me).sub.2-1H-pyrrol-3-yl 0 D-0354 H H H H H 1-Me-4-CF.sub.3-1H-pyrrol-3-yl 0 D-0355 H H H H H 1-Me-4-OMe-1H-pyrrol-3-yl 0 D-0356 H H H H H 1H-pyrazol-1-yl 0 D-0357 H H H H H 5-F-1H-pyrazol-1-yl 0 D-0358 H H H H H 5-Cl-1H-pyrazol-1-yl 0 D-0359 H H H H H 5-Me-1H-pyrazol-1-yl 0 D-0360 H H H H H 5-CF.sub.3-1H-pyrazol-1-yl 0 D-0361 H H H H H 5-OMe-1H-pyrazol-1-yl 0 D-0362 H H H H H 1H-pyrazol-3-yl 0 D-0363 H H H H H 1-Me-1H-pyrazol-3-yl 0 D-0364 H H H H H 4-F-1H-pyrazol-3-yl 0 D-0365 H H H H H 4-Cl-1H-pyrazol-3-yl 0 D-0366 H H H H H 4-Me-1H-pyrazol-3-yl 0 D-0367 H H H H H 4-CF.sub.3-1H-pyrazol-3-yl 0 D-0368 H H H H H 4-OMe-1H-pyrazol-3-yl 0 D-0369 H H H H H 1-Me-4-F-1H-pyrazol-3-yl 0 D-0370 H H H H H 1-Me-4-Cl-1H-pyrazol-3-yl 0 D-0371 H H H H H 1,4-(Me).sub.2-1H-pyrazol-3-yl 0 D-0372 H H H H H 1-Me-4-CF.sub.3-1H-pyrazol-3-yl 0 D-0373 H H H H H 1-Me-4-OMe-1H-pyrazol-3-yl 0 D-0374 H H H H H 1H-pyrazol-4-yl 0 D-0375 H H H H H 1-Me-1H-pyrazol-4-yl 0 D-0376 H H H H H 3-F-1H-pyrazol-4-yl 0 D-0377 H H H H H 3-Cl-1H-pyrazol-4-yl 0 D-0378 H H H H H 3-Me-1H-pyrazol-4-yl 0 D-0379 H H H H H 3-CF.sub.3-17-pyrazol-4-yl 0 D-0380 H H H H H 3-OMe-1H-pyrazol-4-yl 0 D-0381 H H H H H 1-Me-3-F-1H-pyrazol-4-yl 0 D-0382 H H H H H 1-Me-3-Cl-1H-pyrazol-4-yl 0 D-0383 H H H H H 1,3-(Me).sub.2-1H-pyrazol-4-yl 0 D-0384 H H H H H 1-Me-3-CF.sub.3-1H-pyrazol-4-yl 0 D-0385 H H H H H 1-Me-3-OMe-1H-pyrazol-4-yl 0 D-0386 H H H H H 5-F-1H-pyrazol-4-yl 0 D-0387 H H H H H 5-Cl-1H-pyrazol-4-yl 0 D-0388 H H H H H 5-Me-1H-pyrazol-4-yl 0 D-0389 H H H H H 5-CF.sub.3-1H-pyrazol-4-yl 0 D-0390 H H H H H 5-OMe-1H-pyrazol-4-yl 0 D-0391 H H H H H 1-Me-5-F-1H-pyrazol-4-yl 0 D-0392 H H H H H 1-Me-5-Cl-1H-pyrazol-4-yl 0 D-0393 H H H H H 1,5-(Me).sub.2-1H-pyrazol-4-yl 0 D-0394 H H H H H 1-Me-5-CF.sub.3-1H-pyrazol-4-yl 0
(345) TABLE-US-00244 TABLE 244 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-0395 H H H H H 1-Me-5-OMe-1H-pyrazol-4-yl 0 D-0396 H H H H H 1H-pyrazol-5-yl 0 D-0397 H H H H H 1-Me-1H-pyrazol-5-yl 0 D-0398 H H H H H 4-F-1H-pyrazol-5-yl 0 D-0399 H H H H H 4-Cl-1H-pyrazol-5-yl 0 D-0400 H H H H H 4-Me-1H-pyrazol-5-yl 0 D-0401 H H H H H 4-CF.sub.3-1H-pyrazol-5-yl 0 D-0402 H H H H H 4-OMe-1H-pyrazol-5-yl 0 D-0403 H H H H H 1-Me-4-F-1H-pyrazol-5-yl 0 D-0404 H H H H H 1-Me-4-Cl-1H-pyrazol-5-yl 0 D-0405 H H H H H 1,4-(Me).sub.2-1H-pyrazol-5-yl 0 D-0406 H H H H H 1-Me-4-CF.sub.3-1H-pyrazol-5-yl 0 D-0407 H H H H H 1-Me-4-OMe-1H-pyrazol-5-yl 0 D-0408 H H H H H furan-2-yl 0 D-0409 H H H H H 3-F-furan-2-yl 0 D-0410 H H H H H 3-Me-furan-2-yl 0 D-0411 H H H H H 3-CF.sub.3-furan-2-yl 0 D-0412 H H H H H 3-OMe-furan-2-yl 0 D-0413 H H H H H furan-3-yl 0 D-0414 H H H H H 2-F-furan-3-yl 0 D-0415 H H H H H 2-Me-furan-3-yl 0 D-0416 H H H H H 2-CF.sub.3-furan-3-yl 0 D-0417 H H H H H 2-OMe-furan-3-yl 0 D-0418 H H H H H 4-F-furan-3-yl 0 D-0419 H H H H H 4-Me-furan-3-yl 0 D-0420 H H H H H 4-CF.sub.3-furan-3-yl 0 D-0421 H H H H H 4-OMe-furan-3-yl 0 D-0422 H H H H H isoxazol-3-yl 0 D-0423 H H H H H 4-F-isoxazol-3-yl 0 D-0424 H H H H H 4-Me-isoxazol-3-yl 0 D-0425 H H H H H 4-CF.sub.3-isoxazol-3-yl 0 D-0426 H H H H H 4-OMe-isoxazol-3-yl 0 D-0427 H H H H H isoxazol-4-yl 0 D-0428 H H H H H 5-F-isoxazol-4-yl 0 D-0429 H H H H H 5-Me-isoxazol-4-yl 0 D-0430 H H H H H 5-CF.sub.3-isoxazol-4-yl 0 D-0431 H H H H H 5-OMe-isoxazol-4-yl 0 D-0432 H H H H H isoxazol-5-yl 0 D-0433 H H H H H 4-F-isoxazol-5-yl 0 D-0434 H H H H H 4-Me-isoxazol-5-yl 0 D-0435 H H H H H 4-CF.sub.3-isoxazol-5-yl 0 D-0436 H H H H H 4-OMe-isoxazol-5-yl 0 D-0437 H H H H H 1H-1,2,3-triazol-1-yl 0 D-0438 H H H H H 5-F-1H-1,2,3-triazol-1-yl 0 D-0439 H H H H H 5-Me-1H-1,2,3-triazol-1-yl 0 D-0440 H H H H H 5-CF.sub.3-1H-1,2,3-triazol-1-yl 0 D-0441 H H H H H 5-OMe-1H-1,2,3-triazol-1-yl 0 D-0442 H H H H H 1H-1,2,3-triazol-4-yl 0 D-0443 H H H H H 5-F-1H-1,2,3-triazol-4-yl 0 D-0444 H H H H H 5-Me-1H-1,2,3-triazol-4-yl 0 D-0445 H H H H H 5-CF.sub.3-1H-1,2,3-triazol-4-yl 0 D-0446 H H H H H 5-OMe-1H-1,2,3-triazol-4-yl 0 D-0447 H H H H H 1H-1,2,3-triazol-5-yl 0 D-0448 H H H H H 4-F-1H-1,2,3-triazol-5-yl 0 D-0449 H H H H H 4-Me-1H-1,2,3-triazol-5-yl 0 D-0450 H H H H H 4-CF.sub.3-1H-1,2,3-triazol-5-yl 0 D-0451 H H H H H 4-OMe-1H-1,2,3-triazol-5-yl 0
(346) TABLE-US-00245 TABLE 245 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-0452 H H H H H 1H-1,2,4-triazol-1-yl 0 D-0453 H H H H H 5-Me-1H-1,2,4-triazol-1-yl 0 D-0454 H H H H H 5-F-1H-1,2,4-triazol-1-yl 0 D-0455 H H H H H 5-CF.sub.3-1H-1,2,4-triazol-1-yl 0 D-0456 H H H H H 5-OMe-1H-1,2,4-triazol-1-yl 0 D-0457 H H H H H 1H-1,2,4-triazol-3-yl 0 D-0458 H H H H H 1-Me-1H-1,2,4-triazol-3-yl 0 D-0459 H H H H H 1H-1,2,4-triazol-5-yl 0 D-0460 H H H H H 1-Me-1H-1,2,4-triazol-5-yl 0 D-0461 H H H H H 3,5-(Me).sub.2-isoxazol-4-yl 0 D-0462 H H H H H 3,5-(Et).sub.2-isoxazol-4-yl 0 D-0463 H H H H H quinolin-4-yl 0 D-0464 H H H H H isoquinolin-4-yl 0 D-0465 H H H H H 3,6-(OMe).sub.2-pyridazin-4-yl 0 D-0466 H H H H H 2,4-(OMe).sub.2-pyrimidin-5-yl 0 D-0467 H H H H Cl OS(?O).sub.2CF.sub.3 0
(347) TABLE-US-00246 TABLE 246
(348) TABLE-US-00247 TABLE 247 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-5053 H H H H H 3-F-4-Cl-pyridin-2-yl 1 D-5054 H H H H H 3-F-5-Cl-pyridin-2-yl 1 D-5055 H H H H H 3-F-6-Cl-pyridin-2-yl 1 D-5056 H H H H H 3-F-4-Me-pyridin-2-yl 1 D-5057 H H H H H 3-F-5-Me-pyridin-2-yl 1 D-5058 H H H H H 3-F-6-Me-pyridin-2-yl 1 D-5059 H H H H H 3-F-4-OMe-pyridin-2-yl 1 D-5060 H H H H H 3-F-5-OMe-pyridin-2-yl 1 D-5061 H H H H H 3-F-6-OMe-pyridin-2-yl 1 D-5062 H H H H H 3-Cl-4-F-pyridin-2-yl 1 D-5063 H H H H H 3-Cl-5-F-pyridin-2-yl 1 D-5064 H H H H H 3-Cl-6-F-pyridin-2-yl 1 D-5065 H H H H H 3-Cl-4-Me-pyridin-2-yl 1 D-5066 H H H H H 3-Cl-5-Me-pyridin-2-yl 1 D-5067 H H H H H 3-Cl-6-Me-pyridin-2-yl 1 D-5068 H H H H H 3-Me-4-F-pyridin-2-yl 1 D-5069 H H H H H 3-Me-5-F-pyridin-2-yl 1 D-5070 H H H H H 3-Me-6-F-pyridin-2-yl 1 D-5071 H H H H H 3-Me-4-Cl-pyridin-2-yl 1 D-5072 H H H H H 3-Me-5-Cl-pyridin-2-yl 1 D-5073 H H H H H 3-Me-6-Cl-pyridin-2-yl 1 D-5074 H H H H H 3,4-(Me).sub.2-pyridin-2-yl 1 D-5075 H H H H H 3,5-(Me).sub.2-pyridin-2-yl 1 D-5076 H H H H H 3,6-(Me).sub.2-pyridin-2-yl 1 D-5077 H H H H H 3-Me-4-OMe-pyridin-2-yl 1 D-5078 H H H H H 3-Me-5-OMe-pyridin-2-yl 1 D-5079 H H H H H 3-Me-6-OMe-pyridin-2-yl 1 D-5080 H H H H H 3-CF.sub.3-4-F-pyridin-2-yl 1 D-5081 H H H H H 3-CF.sub.3-5-F-pyridin-2-yl 1 D-5082 H H H H H 3-CF.sub.3-6-F-pyridin-2-yl 1 D-5083 H H H H H 3-CF.sub.3-4-Me-pyridin-2-yl 1 D-5084 H H H H H 3-CF.sub.3-5-Me-pyridin-2-yl 1 D-5085 H H H H H 3-CF.sub.3-6-Me-pyridin-2-yl 1 D-5086 H H H H H 3-OMe-4-F-pyridin-2-yl 1 D-5087 H H H H H 3-OMe-5-F-pyridin-2-yl 1 D-5088 H H H H H 3-OMe-6-F-pyridin-2-yl 1 D-5089 H H H H H 3-OMe-4-Cl-pyridin-2-yl 1 D-5090 H H H H H 3-OMe-5-Cl-pyridin-2-yl 1 D-5091 H H H H H 3-OMe-6-Cl-pyridin-2-yl 1 D-5092 H H H H H 3-OMe-4-Me-pyridin-2-yl 1 D-5093 H H H H H 3-OMe-5-Me-pyridin-2-yl 1 D-5094 H H H H H 3-OMe-6-Me-pyridin-2-yl 1 D-5095 H H H H H 3,4-(OMe).sub.2-pyridin-2-yl 1 D-5096 H H H H H 3,5-(OMe).sub.2-pyridin-2-yl 1 D-5097 H H H H H 3,6-(OMe).sub.2-pyridin-2-yl 1 D-5098 H H H H H pyridin-3-yl 1 D-5099 H H H H H 2-F-pyridin-3-yl 1 D-5100 H H H H H 4-F-pyridin-3-yl 1 D-5101 H H H H H 5-F-pyridin-3-yl 1 D-5102 H H H H H 6-F-pyridin-3-yl 1 D-5103 H H H H H 2-Cl-pyridin-3-yl 1 D-5104 H H H H H 4-Cl-pyridin-3-yl 1 D-5105 H H H H H 5-Cl-pyridin-3-yl 1 D-5106 H H H H H 6-Cl-pyridin-3-yl 1 D-5107 H H H H H 2-Me-pyridin-3-yl 1 D-5108 H H H H H 4-Me-pyridin-3-yl 1 D-5109 H H H H H 5-Me-pyridin-3-yl 1
(349) TABLE-US-00248 TABLE 248 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-5110 H H H H H 6-Me-pyridin-3-yl 1 D-5111 H H H H H 2-CF.sub.3-pyridin-3-yl 1 D-5112 H H H H H 4-CF.sub.3-pyridin-3-yl 1 D-5113 H H H H H 5-CF.sub.3-pyridin-3-yl 1 D-5114 H H H H H 6-CF.sub.3-pyridin-3-yl 1 D-5115 H H H H H 2-OMe-pyridin-3-yl 1 D-5116 H H H H H 4-OMe-pyridin-3-yl 1 D-5117 H H H H H 5-OMe-pyridin-3-yl 1 D-5118 H H H H H 6-OMe-pyridin-3-yl 1 D-5119 H H H H H 2,4-F.sub.2-pyridin-3-yl 1 D-5120 H H H H H 2,5-F.sub.2-pyridin-3-yl 1 D-5121 H H H H H 2,6-F.sub.2-pyridin-3-yl 1 D-5122 H H H H H 4,5-F.sub.2-pyridin-3-yl 1 D-5123 H H H H H 4,6-F.sub.2-pyridin-3-yl 1 D-5124 H H H H H 2,4-Cl.sub.2-pyridin-3-yl 1 D-5125 H H H H H 2,5-Cl.sub.2-pyridin-3-yl 1 D-5126 H H H H H 2,6-Cl.sub.2-pyridin-3-yl 1 D-5127 H H H H H 4,5-Cl.sub.2-pyridin-3-yl 1 D-5128 H H H H H 4,6-Cl.sub.2-pyridin-3-yl 1 D-5129 H H H H H 2-F-4-Cl-pyridin-3-yl 1 D-5130 H H H H H 2-F-5-Cl-pyridin-3-yl 1 D-5131 H H H H H 2-F-6-Cl-pyridin-3-yl 1 D-5132 H H H H H 4-F-2-Cl-pyridin-3-yl 1 D-5133 H H H H H 4-F-5-Cl-pyridin-3-yl 1 D-5134 H H H H H 4-F-6-Cl-pyridin-3-yl 1 D-5135 H H H H H 2-F-4-Me-pyridin-3-yl 1 D-5136 H H H H H 2-F-5-Me-pyridin-3-yl 1 D-5137 H H H H H 2-F-6-Me-pyridin-3-yl 1 D-5138 H H H H H 4-F-2-Me-pyridin-3-yl 1 D-5139 H H H H H 4-F-5-Me-pyridin-3-yl 1 D-5140 H H H H H 4-F-6-Me-pyridin-3-yl 1 D-5141 H H H H H 2-F-4-OMe-pyridin-3-yl 1 D-5142 H H H H H 2-F-5-OMe-pyridin-3-yl 1 D-5143 H H H H H 2-F-6-OMe-pyridin-3-yl 1 D-5144 H H H H H 4-F-2-OMe-pyridin-3-yl 1 D-5145 H H H H H 4-F-5-OMe-pyridin-3-yl 1 D-5146 H H H H H 4-F-6-OMe-pyridin-3-yl 1 D-5147 H H H H H 2-Cl-5-F-pyridin-3-yl 1 D-5148 H H H H H 2-Cl-6-F-pyridin-3-yl 1 D-5149 H H H H H 4-Cl-5-F-pyridin-3-yl 1 D-5150 H H H H H 4-Cl-6-F-pyridin-3-yl 1 D-5151 H H H H H 2-Cl-4-Me-pyridin-3-yl 1 D-5152 H H H H H 2-Cl-5-Me-pyridin-3-yl 1 D-5153 H H H H H 2-Cl-6-Me-pyridin-3-yl 1 D-5154 H H H H H 4-Cl-2-Me-pyridin-3-yl 1 D-5155 H H H H H 4-Cl-5-Me-pyridin-3-yl 1 D-5156 H H H H H 4-Cl-6-Me-pyridin-3-yl 1 D-5157 H H H H H 2-Me-5-F-pyridin-3-yl 1 D-5158 H H H H H 2-Me-6-F-pyridin-3-yl 1 D-5159 H H H H H 4-Me-5-F-pyridin-3-yl 1 D-5160 H H H H H 4-Me-6-F-pyridin-3-yl 1 D-5161 H H H H H 2-Me-5-Cl-pyridin-3-yl 1 D-5162 H H H H H 2-Me-6-Cl-pyridin-3-yl 1 D-5163 H H H H H 4-Me-5-Cl-pyridin-3-yl 1 D-5164 H H H H H 4-Me-6-Cl-pyridin-3-yl 1 D-5165 H H H H H 2,4-(Me).sub.2-pyridin-3-yl 1 D-5166 H H H H H 2,5-(Me).sub.2-pyridin-3-yl 1
(350) TABLE-US-00249 TABLE 249 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-5167 H H H H H 2,6-(Me).sub.2-pyridin-3-yl 1 D-5168 H H H H H 4,5-(Me).sub.2-pyridin-3-yl 1 D-5169 H H H H H 4,6-(Me).sub.2-pyridin-3-yl 1 D-5170 H H H H H 2-Me-4-OMe-pyridin-3-yl 1 D-5171 H H H H H 2-Me-5-OMe-pyridin-3-yl 1 D-5172 H H H H H 2-Me-6-OMe-pyridin-3-yl 1 D-5173 H H H H H 4-Me-2-OMe-pyridin-3-yl 1 D-5174 H H H H H 4-Me-5-OMe-pyridin-3-yl 1 D-5175 H H H H H 4-Me-6-OMe-pyridin-3-yl 1 D-5176 H H H H H 2-CF.sub.3-4-F-pyridin-3-yl 1 D-5177 H H H H H 2-CF.sub.3-5-F-pyridin-3-yl 1 D-5178 H H H H H 2-CF.sub.3-6-F-pyridin-3-yl 1 D-5179 H H H H H 4-CF.sub.3-2-F-pyridin-3-yl 1 D-5180 H H H H H 4-CF.sub.3-5-F-pyridin-3-yl 1 D-5181 H H H H H 4-CF.sub.3-6-F-pyridin-3-yl 1 D-5182 H H H H H 2-CF.sub.3-4-Me-pyridin-3-yl 1 D-5183 H H H H H 2-CF.sub.3-5-Me-pyridin-3-yl 1 D-5184 H H H H H 2-CF.sub.3-6-Me-pyridin-3-yl 1 D-5185 H H H H H 4-CF.sub.3-2-Me-pyridin-3-yl 1 D-5186 H H H H H 4-CF.sub.3-5-Me-pyridin-3-yl 1 D-5187 H H H H H 4-CF.sub.3-6-Me-pyridin-3-yl 1 D-5188 H H H H H 2-OMe-5-F-pyridin-3-yl 1 D-5189 H H H H H 2-OMe-6-F-pyridin-3-yl 1 D-5190 H H H H H 4-OMe-5-F-pyridin-3-yl 1 D-5191 H H H H H 4-OMe-6-F-pyridin-3-yl 1 D-5192 H H H H H 2-OMe-4-Cl-pyridin-3-yl 1 D-5193 H H H H H 2-OMe-5-Cl-pyridin-3-yl 1 D-5194 H H H H H 2-OMe-6-Cl-pyridin-3-yl 1 D-5195 H H H H H 4-OMe-2-Cl-pyridin-3-yl 1 D-5196 H H H H H 4-OMe-5-Cl-pyridin-3-yl 1 D-5197 H H H H H 4-OMe-6-Cl-pyridin-3-yl 1 D-5198 H H H H H 2-OMe-5-Me-pyridin-3-yl 1 D-5199 H H H H H 2-OMe-6-Me-pyridin-3-yl 1 D-5200 H H H H H 4-OMe-5-Me-pyridin-3-yl 1 D-5201 H H H H H 4-OMe-6-Me-pyridin-3-yl 1 D-5202 H H H H H 2,4-(OMe).sub.2-pyridin-3-yl 1 D-5203 H H H H H 2,5-(OMe).sub.2-pyridin-3-yl 1 D-5204 H H H H H 2,6-(OMe).sub.2-pyridin-3-yl 1 D-5205 H H H H H 4,5-(OMe).sub.2-pyridin-3-yl 1 D-5206 H H H H H 4,6-(OMe).sub.2-pyridin-3-yl 1 D-5207 H H H H H pyridin-4-yl 1 D-5208 H H H H H 2-F-pyridin-4-yl 1 D-5209 H H H H H 3-F-pyridin-4-yl 1 D-5210 H H H H H 2-Cl-pyridin-4-yl 1 D-5211 H H H H H 3-Cl-pyridin-4-yl 1 D-5212 H H H H H 2-Me-pyridin-4-yl 1 D-5213 H H H H H 3-Me-pyridin-4-yl 1 D-5214 H H H H H 2-CF.sub.3-pyridin-4-yl 1 D-5215 H H H H H 3-CF.sub.3-pyridin-4-yl 1 D-5216 H H H H H 2-OMe-pyridin-4-yl 1 D-5217 H H H H H 3-OMe-pyridin-4-yl 1 D-5218 H H H H H 2,3-F.sub.2-pyridin-4-yl 1 D-5219 H H H H H 2,5-F.sub.2-pyridin-4-yl 1 D-5220 H H H H H 2,6-F.sub.2-pyridin-4-yl 1 D-5221 H H H H H 3,5-F.sub.2-pyridin-4-yl 1 D-5222 H H H H H 2,3-Cl.sub.2-pyridin-4-yl 1 D-5223 H H H H H 2,5-Cl.sub.2-pyridin-4-yl 1
(351) TABLE-US-00250 TABLE 250 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-5224 H H H H H 2,6-Cl.sub.2-pyridin-4-yl 1 D-5225 H H H H H 3,5-Cl.sub.2-pyridin-4-yl 1 D-5226 H H H H H 3-F-2-Cl-pyridin-4-yl 1 D-5227 H H H H H 3-F-5-Cl-pyridin-4-yl 1 D-5228 H H H H H 3-F-6-Cl-pyridin-4-yl 1 D-5229 H H H H H 3-F-2-Me-pyridin-4-yl 1 D-5230 H H H H H 3-F-5-Me-pyridin-4-yl 1 D-5231 H H H H H 3-F-6-Me-pyridin-4-yl 1 D-5232 H H H H H 3-F-2-OMe-pyridin-4-yl 1 D-5233 H H H H H 3-F-5-OMe-pyridin-4-yl 1 D-5234 H H H H H 3-F-6-OMe-pyridin-4-yl 1 D-5235 H H H H H 3-Cl-2-F-pyridin-4-yl 1 D-5236 H H H H H 3-Cl-6-F-pyridin-4-yl 1 D-5237 H H H H H 3-Cl-2-Me-pyridin-4-yl 1 D-5238 H H H H H 3-Cl-5-Me-pyridin-4-yl 1 D-5239 H H H H H 3-Cl-6-Me-pyridin-4-yl 1 D-5240 H H H H H 3-Me-2-F-pyridin-4-yl 1 D-5241 H H H H H 3-Me-6-F-pyridin-4-yl 1 D-5242 H H H H H 3-Me-2-Cl-pyridin-4-yl 1 D-5243 H H H H H 3-Me-6-Cl-pyridin-4-yl 1 D-5244 H H H H H 2,3-(Me).sub.2-pyridin-4-yl 1 D-5245 H H H H H 3,5-(Me).sub.2-pyridin-4-yl 1 D-5246 H H H H H 3,6-(Me).sub.2-pyridin-4-yl 1 D-5247 H H H H H 3-Me-2-OMe-pyridin-4-yl 1 D-5248 H H H H H 3-Me-5-OMe-pyridin-4-yl 1 D-5249 H H H H H 3-Me-6-OMe-pyridin-4-yl 1 D-5250 H H H H H 3-CF.sub.3-2-F-pyridin-4-yl 1 D-5251 H H H H H 3-CF.sub.3-5-F-pyridin-4-yl 1 D-5252 H H H H H 3-CF.sub.3-6-F-pyridin-4-yl 1 D-5253 H H H H H 3-CF.sub.3-2-Me-pyridin-4-yl 1 D-5254 H H H H H 3-CF.sub.3-5-Me-pyridin-4-yl 1 D-5255 H H H H H 3-CF.sub.3-6-Me-pyridin-4-yl 1 D-5256 H H H H H 3-OMe-2-F-pyridin-4-yl 1 D-5257 H H H H H 3-OMe-6-F-pyridin-4-yl 1 D-5258 H H H H H 3-OMe-2-Cl-pyridin-4-yl 1 D-5259 H H H H H 3-OMe-5-Cl-pyridin-4-yl 1 D-5260 H H H H H 3-OMe-6-Cl-pyridin-4-yl 1 D-5261 H H H H H 3-OMe-2-Me-pyridin-4-yl 1 D-5262 H H H H H 3-OMe-6-Me-pyridin-4-yl 1 D-5263 H H H H H 2,3-(OMe).sub.2-pyridin-4-yl 1 D-5264 H H H H H 3,5-(OMe).sub.2-pyridin-4-yl 1 D-5265 H H H H H 3,6-(OMe).sub.2-pyridin-4-yl 1 D-5266 H H H H H pyrimidin-2-yl 1 D-5267 H H H H H pyrimidin-4-yl 1 D-5268 H H H H H 5-F-pyrimidin-4-yl 1 D-5269 H H H H H 5-Me-pyrimidin-4-yl 1 D-5270 H H H H H 5-CF.sub.3-pyrimidin-4-yl 1 D-5271 H H H H H 5-OMe-pyrimidin-4-yl 1 D-5272 H H H H H pyrimidin-5-yl 1 D-5273 H H H H H 4-F-pyrimidin-5-yl 1 D-5274 H H H H H 4-Cl-pyrimidin-5-yl 1 D-5275 H H H H H 4-Me-pyrimidin-5-yl 1 D-5276 H H H H H 4-CF.sub.3-pyrimidin-5-yl 1 D-5277 H H H H H 4-OMe-pyrimidin-5-yl 1 D-5278 H H H H H pyridazin-3-yl 1 D-5279 H H H H H 4-F-pyridazin-3-yl 1 D-5280 H H H H H 4-Cl-pyridazin-3-yl 1
(352) TABLE-US-00251 TABLE 251 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-5281 H H H H H 4-Me-pyridazin-3-yl 1 D-5282 H H H H H 4-CF.sub.3-pyridazin-3-yl 1 D-5283 H H H H H 4-OMe-pyridazin-3-yl 1 D-5284 H H H H H pyridazin-4-yl 1 D-5285 H H H H H 3-F-pyridazin-4-yl 1 D-5286 H H H H H 3-Cl-pyridazin-4-yl 1 D-5287 H H H H H 3-Me-pyridazin-4-yl 1 D-5288 H H H H H 3-CF.sub.3-pyridazn-4-yl 1 D-5289 H H H H H 3-OMe-pyridazin-4-yl 1 D-5290 H H H H H 5-F-pyridazin-4-yl 1 D-5291 H H H H H 5-Cl-pyridazin-4-yl 1 D-5292 H H H H H 5-Me-pyridazin-4-yl 1 D-5293 H H H H H 5-CF.sub.3-pyridazn-4-yl 1 D-5294 H H H H H 5-OMe-pyridazin-4-yl 1 D-5295 H H H H H thiophen-2-yl 1 D-5296 H H H H H 3-F-thiophen-2-yl 1 D-5297 H H H H H 3-Cl-thiophen-2-yl 1 D-5298 H H H H H 3-Me-thiophen-2-yl 1 D-5299 H H H H H 3-CF.sub.3-thiophen-2-yl 1 D-5300 H H H H H 3-OMe-thiophen-2-yl 1 D-5301 H H H H H thiophen-3-yl 1 D-5302 H H H H H 2F-thiophen-3-yl 1 D-5303 H H H H H 2-Cl-thiophen-3-yl 1 D-5304 H H H H H 2-Me-thiophen-3-yl 1 D-5305 H H H H H 2-CF.sub.3-thiophen-3-y 1 D-5306 H H H H H 2-OMe-thiophen-3-yl 1 D-5307 H H H H H 4-F-thiophen-3-yl 1 D-5308 H H H H H 4-Cl-thiophen-3-yl 1 D-5309 H H H H H 4-Me-thiophen-3-yl 1 D-5310 H H H H H 4-CF.sub.3-thiophen-3-yl 1 D-5311 H H H H H 4-OMe-thiophen-3-yl 1 D-5312 H H H H H thiazol-2-yl 1 D-5313 H H H H H thiazol-4-yl 1 D-5314 H H H H H 5-F-thiazol-4-yl 1 D-5315 H H H H H 5-Me-thiazol-4-yl 1 D-5316 H H H H H 5-CF.sub.3-thiazol-4-yl 1 D-5317 H H H H H 5-OMe-thiazol-4-yl 1 D-5318 H H H H H thiazol-5-yl 1 D-5319 H H H H H 4-F-thiazol-5-yl 1 D-5320 H H H H H 4-Me-thiazol-5-yl 1 D-5321 H H H H H 4-CF.sub.3-thiazol-5-yl 1 D-5322 H H H H H 4-OMe-thiazol-5-yl 1 D-5323 H H H H H 1H-pyrrol-1-yl 1 D-5324 H H H H H 2-F-1H-pyrrol-1-yl 1 D-5325 H H H H H 2-Me-1H-pyrrol-1-yl 1 D-5326 H H H H H 2-CF.sub.3-1H-pyrrol-1-yl 1 D-5327 H H H H H 2-OMe-1H-pyrrol-1-yl 1 D-5328 H H H H H 1H-pyrrol-2-yl 1 D-5329 H H H H H 1-Me-1H-pyrrol-2-yl 1 D-5330 H H H H H 3-F-1H-pyrrol-2-yl 1 D-5331 H H H H H 3-Me-1H-pyrrol-2-yl 1 D-5332 H H H H H 3-CF.sub.3-1H-pyrrol-2-yl 1 D-5333 H H H H H 3-OMe-1H-pyrrol-2-yl 1 D-5334 H H H H H 1-Me-3-F-1H-pyrrol-2-yl 1 D-5335 H H H H H 1,3-(Me).sub.2-1H-pyrrol-2-yl 1 D-5336 H H H H H 1-Me-3-CF.sub.3-1H-pyrrol-2-yl 1 D-5337 H H H H H 1-Me-3-OMe-1H-pyrrol-2-yl 1
(353) TABLE-US-00252 TABLE 252 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-5338 H H H H H 1H-pyrrol-3-yl 1 D-5339 H H H H H 1-Me-1H-pyrrol-3-yl 1 D-5340 H H H H H 2-F-1H-pyrrol-3-yl 1 D-5341 H H H H H 2-Me-1H-pyrrol-3-yl 1 D-5342 H H H H H 2-CF.sub.3-1H-pyrrol-3-yl 1 D-5343 H H H H H 2-OMe-1H-pyrrol-3-yl 1 D-5344 H H H H H 1-Me-2-F-1H-pyrrol-3-yl 1 D-5345 H H H H H 1,2-(Me).sub.2-1H-pyrrol-3-yl 1 D-5346 H H H H H 1-Me-2-CF.sub.3-1H-pyrrol-3-yl 1 D-5347 H H H H H 1-Me-2-OMe-1H-pyrrol-3-yl 1 D-5348 H H H H H 4-F-1H-pyrrol-3-yl 1 D-5349 H H H H H 4-Me-1H-pyrrol-3-yl 1 D-5350 H H H H H 4-CF.sub.3-1H-pyrrol-3-yl 1 D-5351 H H H H H 4-OMe-1H-pyrrol-3-yl 1 D-5352 H H H H H 1-Me-4-F-1H-pyrrol-3-yl 1 D-5353 H H H H H 1,4-(Me).sub.2-1H-pyrrol-3-yl 1 D-5354 H H H H H 1-Me-4-CF.sub.3-1H-pyrrol-3-yl 1 D-5355 H H H H H 1-Me-4-OMe-1H-pyrrol-3-yl 1 D-5356 H H H H H 1H-pyrazol-1-yl 1 D-5357 H H H H H 5-F-1H-pyrazol-yl 1 D-5358 H H H H H 5-Cl-1H-pyrazol-1-yl 1 D-5359 H H H H H 5-Me-1H-pyrazol-1-yl 1 D-5360 H H H H H 5-CF.sub.3-1H-pyrazol-1-yl 1 D-5361 H H H H H 5-OMe-1H-pyrazol-1-yl 1 D-5362 H H H H H 1H-pyrazol-3-yl 1 D-5363 H H H H H 1-Me-1H-pyrazol-3-yl 1 D-5364 H H H H H 4-F-1H-pyrazol-3-yl 1 D-5365 H H H H H 4-Cl-1H-pyrazol-3-yl 1 D-5366 H H H H H 4-Me-1H-pyrazol-3-yl 1 D-5367 H H H H H 4-CF.sub.3-1H-pyrazol-3-y 1 D-5368 H H H H H 4-OMe-1H-pyrazol-3-yl 1 D-5369 H H H H H 1-Me-4-F-1H-pyrazol-3-yl 1 D-5370 H H H H H 1-Me-4-Cl-1H-pyrazol-3-yl 1 D-5371 H H H H H 1,4-(Me).sub.2-17-pyrazol-3-yl 1 D-5372 H H H H H 1-Me-4-CF.sub.3-1H-pyrazol-3-yl 1 D-5373 H H H H H 1-Me-4-OMe-1H-pyrazol-3-yl 1 D-5374 H H H H H 1H-pyrazol-4-yl 1 D-5375 H H H H H 1-Me-1H-pyrazol-4-yl 1 D-5376 H H H H H 3-F-1H-pyrazol-4-yl 1 D-5377 H H H H H 3-Cl-1H-pyrazol-4-yl 1 D-5378 H H H H H 3-Me-1H-pyrazol-4-yl 1 D-5379 H H H H H 3-CF.sub.3-1H-pyrazol-4-y 1 D-5380 H H H H H 3-OMe-1H-pyrazol-4-yl 1 D-5381 H H H H H 1-Me-3-F-1H-pyrazol-4-yl 1 D-5382 H H H H H 1-Me-3-Cl-1H-pyrazol-4-yl 1 D-5383 H H H H H 1,3-(Me).sub.2-1H-pyrazol-4-yl 1 D-5384 H H H H H 1-Me-3-CF.sub.3-1H-pyrazol-4-yl 1 D-5385 H H H H H 1-Me-3-OMe-1H-pyrazol-4-yl 1 D-5386 H H H H H 5-F-1H-pyrazol-4-yl 1 D-5387 H H H H H 5-Cl-1H-pyrazol-4-yl 1 D-5388 H H H H H 5-Me-1H-pyrazol-4-yl 1 D-5389 H H H H H 5-CF.sub.3-1H-pyrazol-4-yl 1 D-5390 H H H H H 5-OMe-1H-pyrazol-4-yl 1 D-5391 H H H H H 1-Me-5-F-1H-pyrazol-4-yl 1 D-5392 H H H H H 1-Me-5-Cl-1H-pyrazol-4-yl 1 D-5393 H H H H H 1,5-(Me).sub.2-1H-pyrazol-4-yl 1 D-5394 H H H H H 1-Me-5-CF.sub.3-1H-pyrazol-4-yl 1
(354) TABLE-US-00253 TABLE 253 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-5395 H H H H H 1-Me-5-OMe-1H-pyrazol-4-yl 1 D-5396 H H H H H 1H-pyrazol-5-yl 1 D-5397 H H H H H 1-Me-1H-pyrazol-5-yl 1 D-5398 H H H H H 4-F-1H-pyrazol-5-yl 1 D-5399 H H H H H 4-Cl-1H-pyrazol-5-yl 1 D-5400 H H H H H 4-Me-1H-pyrazol-5-yl 1 D-5401 H H H H H 4-CF.sub.3-1H-pyrazol-5-yl 1 D-5402 H H H H H 4-OMe-1H-pyrazol-5-yl 1 D-5403 H H H H H 1-Me-4-F-1H-pyrazol-5-yl 1 D-5404 H H H H H 1-Me-4-Cl-1H-pyrazol-5-yl 1 D-5405 H H H H H 1,4-(Me).sub.2-1H-pyrazol-5-yl 1 D-5406 H H H H H 1-Me-4-CF.sub.3-1H-pyrazol-5-yl 1 D-5407 H H H H H 1-Me-4-OMe-1H-pyrazol-5-yl 1 D-5408 H H H H H furan-2-yl 1 D-5409 H H H H H 3-F-furan-2-yl 1 D-5410 H H H H H 3-Me-furan-2-yl 1 D-5411 H H H H H 3-CF.sub.3-furan-2-yl 1 D-5412 H H H H H 3-OMe-furan-2-yl 1 D-5413 H H H H H furan-3-yl 1 D-5414 H H H H H 2-F-furan-3-yl 1 D-5415 H H H H H 2-Me-furan-3-yl 1 D-5416 H H H H H 2-CF3-furan-3-yl 1 D-5417 H H H H H 2-OMe-furan-3-yl 1 D-5418 H H H H H 4-F-furan-3-yl 1 D-5419 H H H H H 4-Me-furan-3-yl 1 D-5420 H H H H H 4-CF.sub.3-furan-3-yl 1 D-5421 H H H H H 4-OMe-furan-3-yl 1 D-5422 H H H H H isoxazol-3-yl 1 D-5423 H H H H H 4-F-isoxazol3-yl 1 D-5424 H H H H H 4-Me-isoxazol-3-yl 1 D-5425 H H H H H 4-CF.sub.3-isoxazol-3-yl 1 D-5426 H H H H H 4-OMe-isoxazol-3-yl 1 D-5427 H H H H H isoxazol-4-yl 1 D-5428 H H H H H 5-F-isoxazol-4-yl 1 D-5429 H H H H H 5-Me-isoxazol-4-yl 1 D-5430 H H H H H 5-CF.sub.3-isoxazol-4-yl 1 D-5431 H H H H H 5-OMe-isoxazol-4-yl 1 D-5432 H H H H H isoxazo-5-yl 1 D-5433 H H H H H 4-F-isoxazol-5-yl 1 D-5434 H H H H H 4-Me-isoxazol-5-yl 1 D-5435 H H H H H 4-CF.sub.3-isoxazol-5-yl 1 D-5436 H H H H H 4-OMe-isoxazol-5-yl 1 D-5437 H H H H H 1H-1,2,3-triazol-1-yl 1 D-5438 H H H H H 5-F-1H-1,2,3-triazol-1-yl 1 D-5439 H H H H H 5-Me-1H-1,2,3-triazol-1-yl 1 D-5440 H H H H H 5-CF.sub.3-1H-1,2,3-triazol-1-yl 1 D-5441 H H H H H 5-OMe-1H-1,2,3-triazol-1-yl 1 D-5442 H H H H H 1H-1,2,3-triazol-4-yl 1 D-5443 H H H H H 5-F-1H-1,2,3-triazol-4-yl 1 D-5444 H H H H H 5-Me-1H-1,2,3-triazol-4-yl 1 D-5445 H H H H H 5-CF.sub.3-1H-1,2,3-triazol-4-yl 1 D-5446 H H H H H 5-OMe-1H-1,2,3-triazol-4-yl 1 D-5447 H H H H H 1H-1,2,3-triazol-5-yl 1 D-5448 H H H H H 4-F-1H-1,2,3-triazol-5-yl 1 D-5449 H H H H H 4-Me-1H-1,2,3-triazol-5-yl 1 D-5450 H H H H H 4-CF.sub.3-1H-1,2,3-triazol-5-yl 1 D-5451 H H H H H 4-OMe-1H-1,2,3-triazol-5-yl 1
(355) TABLE-US-00254 TABLE 254 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p D-5452 H H H H H 1H-1,2,4-triazol-1-yl 1 D-5453 H H H H H 5-Me-1H-1,2,4-triazol-1-yl 1 D-5454 H H H H H 5-F-1H-1,2,4-triazol-1-yl 1 D-5455 H H H H H 5-CF.sub.3-1H-1,2,4-triazol-1-yl 1 D-5456 H H H H H 5-OMe-1H-1,2,4-triazol-1-yl 1 D-5457 H H H H H 1H-1,2,4-triazol-3-yl 1 D-5458 H H H H H 1-Me-1H-1,2,4-triazol-3-yl 1 D-5459 H H H H H 1H-1,2,4-triazol-5-yl 1 D-5460 H H H H H 1-Me-1H-1,2,4-triazol-5-yl 1 D-5461 H H H H H 3,5-(Me).sub.2-isoxazol-4-yl 1 D-5462 H H H H H 3,5-(Et).sub.2-isoxazol-4-yl 1 D-5463 H H H H H 1,3,5-(Me).sub.3-1H-pyrazol-4-yl 1 D-5464 H H H H H quinolin-4-yl 1 D-5465 H H H H H isoquinolin-4-yl 1 D-5466 H H H H H 3,6-(OMe).sub.2-pyridazin-4-yl 1 D-5467 H H H H H 2,4-(OMe).sub.2-pyrmidin-5-yl 1
(356) TABLE-US-00255 TABLE 255
(357) TABLE-US-00256 TABLE 256 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0053 H H H H H 2-CF.sub.2Cl 0 E-0054 H H H H H 3-CF.sub.2Cl 0 E-0055 H H H H H 4-CF.sub.2Cl 0 E-0056 H H H H H 2-CF(CF.sub.3).sub.2 0 E-0057 H H H H H 3-CF(CF.sub.3).sub.2 0 E-0058 H H H H H 4-CF(CF.sub.3).sub.2 0 E-0059 H H H H H 2-cyclopropyl 0 E-0060 H H H H H 3-cyclopropyl 0 E-0061 H H H H H 4-cyclopropyl 0 E-0062 H H H H H 2-cyclobutyl 0 E-0063 H H H H H 3-cyclobutyl 0 E-0064 H H H H H 4-cyclobutyl 0 E-0065 H H H H H 2-cyclopentyl 0 E-0066 H H H H H 3-cyclopentyl 0 E-0067 H H H H H 4-cyclopentyl 0 E-0068 H H H H H 2-(cyclopropylmethyl) 0 E-0069 H H H H H 3-(cyclopropylmethyl) 0 E-0070 H H H H H 4-(cyclopropylmethyl) 0 E-0071 H H H H H 2-(cyclobutylmethyl) 0 E-0072 H H H H H 3-(cyclobutylmethyl) 0 E-0073 H H H H H 4-(cyclobutylmethyl) 0 E-0074 H H H H H 2-(cyclopentylmethyl) 0 E-0075 H H H H H 3-(cyclopentylmethyl) 0 E-0076 H H H H H 4-(cyclopentylmethyl) 0 E-0077 H H H H H 2-(cyclopropylethyl) 0 E-0078 H H H H H 3-(cyclopropylethyl) 0 E-0079 H H H H H 4-(cyclopropylethyl) 0 E-0080 H H H H H 2-(2,2-difluorocyclopropyl) 0 E-0081 H H H H H 3-(2,2-difluorocyclopropyl) 0 E-0082 H H H H H 4-(2,2-difluorocyclopropyl) 0 E-0083 H H H H H 2-(2,2-dichlorocyclopropyl) 0 E-0084 H H H H H 3-(2,2-dichlorocyclopropyl) 0 E-0085 H H H H H 4-(2,2-dichlorocyclopropyl) 0 E-0086 H H H H H 2-ethenyl 0 E-0087 H H H H H 3-ethenyl 0 E-0088 H H H H H 4-ethenyl 0 E-0089 H H H H H 2-allyl 0 E-0090 H H H H H 3-allyl 0 E-0091 H H H H H 4-allyl 0 E-0092 H H H H H 2-(prop-1-en-1-yl) 0 E-0093 H H H H H 3-(prop-1-en-1-yl) 0 E-0094 H H H H H 4-(prop-1-en-1-yl) 0 E-0095 H H H H H 2-(trifluoroethenyl) 0 E-0096 H H H H H 3-(trifluoroethenyl) 0 E-0097 H H H H H 4-(trifluoroethenyI) 0 E-0098 H H H H H 2-(2,2-dichloroethenyl) 0 E-0099 H H H H H 3-(2,2-dichloroethenyl) 0 E-0100 H H H H H 4-(2,2-dichloroethenyl) 0 E-0101 H H H H H 2-ethynyl 0 E-0102 H H H H H 3-ethynyl 0 E-0103 H H H H H 4-ethynyl 0 E-0104 H H H H H 2-(1-propyn-1-yl) 0 E-0105 H H H H H 3-(1-propyn-1-yl) 0 E-0106 H H H H H 4-(1-propyn-1-yl) 0 E-0107 H H H H H 2-(2-propyn-1-yl) 0 E-0108 H H H H H 3-(2-propyn-1-yl) 0 E-0109 H H H H H 4-(2-propyn-1-yl) 0
(358) TABLE-US-00257 TABLE 257 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0110 H H H H H 2-(2-cyclopropylethynyl) 0 E-0111 H H H H H 3-(2-cyclopropylethynyl) 0 E-0112 H H H H H 4-(2-cyclopropylethynyl) 0 E-0113 H H H H H 2-(2-chloroethynyl) 0 E-0114 H H H H H 3-(2-chloroethynyl) 0 E-0115 H H H H H 4-(2-chloroethynyl) 0 E-0116 H H H H H 2-(2-bromoethynyl) 0 E-0117 H H H H H 3-(2-bromoethynyl) 0 E-0118 H H H H H 4-(2-bromoethynyl) 0 E-0119 H H H H H 2-OMe 0 E-0120 H H H H H 3-OMe 0 E-0121 H H H H H 4-OMe 0 E-0122 H H H H H 2-OEt 0 E-0123 H H H H H 3-OEt 0 E-0124 H H H H H 4-OEt 0 E-0125 H H H H H 2-OPr 0 E-0126 H H H H H 3-OPr 0 E-0127 H H H H H 4-OPr 0 E-0128 H H H H H 2-O(i-Pr) 0 E-0129 H H H H H 3-O(i-Pr) 0 E-0130 H H H H H 4-O(i-Pr) 0 E-0131 H H H H H 2-OBu 0 E-0132 H H H H H 3-OBu 0 E-0133 H H H H H 4-OBu 0 E-0134 H H H H H 2-O(s-Bu) 0 E-0135 H H H H H 3-O(s-Bu) 0 E-0136 H H H H H 4-O(s-Bu) 0 E-0137 H H H H H 2-O(i-Bu) 0 E-0138 H H H H H 3-O(i-Bu) 0 E-0139 H H H H H 4-O(i-Bu) 0 E-0140 H H H H H 2-O(t-Bu) 0 E-0141 H H H H H 3-O(t-Bu) 0 E-0142 H H H H H 4-O(t-Bu) 0 E-0143 H H H H H 2-OCF.sub.3 0 E-0144 H H H H H 3-OCF.sub.3 0 E-0145 H H H H H 4-OCF.sub.3 0 E-0146 H H H H H 2-OCHF.sub.2 0 E-0147 H H H H H 3-OCHF.sub.2 0 E-0148 H H H H H 4-OCHF.sub.2 0 E-0149 H H H H H 2-OCH.sub.2CF.sub.3 0 E-0150 H H H H H 3-OCH.sub.2CF.sub.3 0 E-0151 H H H H H 4-OCH.sub.2CF.sub.3 0 E-0152 H H H H H 2-(cyclopropyloxy) 0 E-0153 H H H H H 3-(cyclopropyloxy) 0 E-0154 H H H H H 4-(cyclopropyloxy) 0 E-0155 H H H H H 2-(cyclobutyloxy) 0 E-0156 H H H H H 3-(cyclobutyloxy) 0 E-0157 H H H H H 4-(cyclobutyloxy) 0 E-0158 H H H H H 2-(cyclopentyloxy) 0 E-0159 H H H H H 3-(cyclopentyloxy) 0 E-0160 H H H H H 4-(cyclopentyloxy) 0 E-0161 H H H H H 2-((2,2-dichlorocyclopropyl)oxy) 0 E-0162 H H H H H 3-((2,2-dichlorocyclopropyl)oxy) 0 E-0163 H H H H H 4-((2,2-dichlorocyclopropyl)oxy) 0 E-0164 H H H H H 2-(cyclopropylmethoxy) 0 E-0165 H H H H H 3-(cyclopropylmethoxy) 0 E-0166 H H H H H 4-(cyclopropylmethoxy) 0
(359) TABLE-US-00258 TABLE 258 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0167 H H H H H 2-((2,2-difluorocyclopropyl)methoxy) 0 E-0168 H H H H H 3-((2,2-difluorocyclopropyl)methoxy) 0 E-0169 H H H H H 4-((2,2-difluorocyclopropyl)methoxy) 0 E-0170 H H H H H 2-(oxiran-2-yl) 0 E-0171 H H H H H 3-(oxiran-2-yl) 0 E-0172 H H H H H 4-(oxiran-2-yl) 0 E-0173 H H H H H 2-(oxiran-2-ylmethyl) 0 E-0174 H H H H H 3-(oxiran-2-ylmethyl) 0 E-0175 H H H H H 4-(oxiran-2-ylmethyl) 0 E-0176 H H H H H 2-SMe 0 E-0177 H H H H H 3-SMe 0 E-0178 H H H H H 4-SMe 0 E-0179 H H H H H 2-SEt 0 E-0180 H H H H H 3-SEt 0 E-0181 H H H H H 4-SEt 0 E-0182 H H H H H 2-S(?O)Me 0 E-0183 H H H H H 3-S(?O)Me 0 E-0184 H H H H H 4-S(?O)Me 0 E-0185 H H H H H 2-S(?O).sub.2Me 0 E-0186 H H H H H 3-S(?O).sub.2Me 0 E-0187 H H H H H 4-S(?O).sub.2Me 0 E-0188 H H H H H 2-SCF.sub.3 0 E-0189 H H H H H 3-SCF.sub.3 0 E-0190 H H H H H 4-SCF.sub.3 0 E-0191 H H H H H 2-S(?O)CF.sub.3 0 E-0192 H H H H H 3-S(?O)CF.sub.3 0 E-0193 H H H H H 4-S(?O)CF.sub.3 0 E-0194 H H H H H 2-S(?O).sub.2CF.sub.3 0 E-0195 H H H H H 3-S(?O).sub.2CF.sub.3 0 E-0196 H H H H H 4-S(?O).sub.2CF.sub.3 0 E-0197 H H H H H 2-SCF(CF.sub.3).sub.2 0 E-0198 H H H H H 3-SCF(CF.sub.3).sub.2 0 E-0199 H H H H H 4-SCF(CF.sub.3).sub.2 0 E-0200 H H H H H 2-(cyclopropylthio) 0 E-0201 H H H H H 3-(cyclopropylthio) 0 E-0202 H H H H H 4-(cyclopropylthio) 0 E-0203 H H H H H 2-(cyclopropylsulfinyl) 0 E-0204 H H H H H 3-(cyclopropylsulfinyl) 0 E-0205 H H H H H 4-(cyclopropylsulfinyl) 0 E-0206 H H H H H 2-(cyclopropylsulfonyl) 0 E-0207 H H H H H 3-(cyclopropylsulfonyl) 0 E-0208 H H H H H 4-(cyclopropylsulfonyl) 0 E-0209 H H H H H 2-((cyclopropylmethyl)thio) 0 E-0210 H H H H H 3-((cyclopropylmethyl)thio) 0 E-0211 H H H H H 4-((cyclopropylmethyl)thio) 0 E-0212 H H H H H 2-((cyclopropylmethyl)sulfinyl) 0 E-0213 H H H H H 3-((cyclopropylmethyl)sulfinyl) 0 E-0214 H H H H H 4-((cyclopropylmethyl)sulfinyl) 0 E-0215 H H H H H 2-((cyclopropylmethyl)sulfonyl) 0 E-0216 H H H H H 3-((cyclopropylmethyl)sulfonyl) 0 E-0217 H H H H H 4-((cyclopropylmethyl)sulfonyl) 0 E-0218 H H H H H 2-(((2,2-difluorocyclopropyl)methyl)thio) 0 E-0219 H H H H H 3-(((2,2-difluorocyclopropyl)methyl)thio) 0 E-0220 H H H H H 4-(((2,2-difluorocyclopropyl)methyl)thio) 0 E-0221 H H H H H 2-(((2,2-difluorocyclopropyl)methyl)sulfinyl) 0 E-0222 H H H H H 3-(((2,2-difluorocyclopropyl)methyl)sulfinyl) 0 E-0223 H H H H H 4-(((2,2-difluorocyclopropyl)methyl)sulfinyl) 0
(360) TABLE-US-00259 TABLE 259 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0224 H H H H H 2-(((2,2-difluorocyclopropyl)methyl)sulfonyl) 0 E-0225 H H H H H 3-(((2,2-difluorocyclopropyl)methyl)sulfonyl) 0 E-0226 H H H H H 4-(((2,2-difluorocyclopropyl)methyl)sulfonyl) 0 E-0227 H H H H H 2-C(?O)Me 0 E-0228 H H H H H 3-C(?O)Me 0 E-0229 H H H H H 4-C(?O)Me 0 E-0230 H H H H H 2-C(?O)Et 0 E-0231 H H H H H 3-C(?O)Et 0 E-0232 H H H H H 4-C(?O)Et 0 E-0233 H H H H H 2-C(?O)CF.sub.3 0 E-0234 H H H H H 3-C(?O)CF.sub.3 0 E-0235 H H H H H 4-C(?O)CF.sub.3 0 E-0236 H H H H H 2-C(?O)OMe 0 E-0237 H H H H H 3-C(?O)OMe 0 E-0238 H H H H H 4-C(?O)OMe 0 E-0239 H H H H H 2-C(?O)OEt 0 E-0240 H H H H H 3-C(?O)OEt 0 E-0241 H H H H H 4-C(?O)OEt 0 E-0242 H H H H H 2-C(?O)NH.sub.2 0 E-0243 H H H H H 3-C(?O)NH.sub.2 0 E-0244 H H H H H 4-C(?O)NH.sub.2 0 E-0245 H H H H H 2-C(?O)NHMe 0 E-0246 H H H H H 3-C(?O)NHMe 0 E-0247 H H H H H 4-C(?O)NHMe 0 E-0248 H H H H H 2-C(?O)NMe.sub.2 0 E-0249 H H H H H 3-C(?O)NMe.sub.2 0 E-0250 H H H H H 4-C(?O)NMe.sub.2 0 E-0251 H H H H H 2-CH.sub.2C(?O)CH.sub.3 0 E-0252 H H H H H 3-CH.sub.2C(?O)CH.sub.3 0 E-0253 H H H H H 4-CH.sub.2C(?O)CH.sub.3 0 E-0254 H H H H H 2-CH.sub.2C(?O)CF.sub.3 0 E-0255 H H H H H 3-CH.sub.2C(?O)CF.sub.3 0 E-0256 H H H H H 4-CH.sub.2C(?O)CF.sub.3 0 E-0257 H H H H H 2-CH.sub.2C(?O)OCH.sub.3 0 E-0258 H H H H H 3-CH.sub.2C(?O)OCH.sub.3 0 E-0259 H H H H H 4-CH.sub.2C(?O)OCH.sub.3 0 E-0260 H H H H H 2-CH.sub.2OH 0 E-0261 H H H H H 3-CH.sub.2OH 0 E-0262 H H H H H 4-CH.sub.2OH 0 E-0263 H H H H H 2-CH.sub.2OCH.sub.3 0 E-0264 H H H H H 3-CH.sub.2OCH.sub.3 0 E-0265 H H H H H 4-CH.sub.2OCH.sub.3 0 E-0266 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3 0 E-0267 H H H H H 3-CH.sub.2OCH.sub.2CH.sub.3 0 E-0268 H H H H H 4-CH.sub.2OCH.sub.2CH.sub.3 0 E-0269 H H H H H 2-CH(CH.sub.3)OCH.sub.3 0 E-0270 H H H H H 3-CH(CH.sub.3)OCH.sub.3 0 E-0271 H H H H H 4-CH(CH.sub.3)OCH.sub.3 0 E-0272 H H H H H 2-CH.sub.2CH.sub.2OCH.sub.3 0 E-0273 H H H H H 3-CH.sub.2CH.sub.2OCH.sub.3 0 E-0274 H H H H H 4-CH.sub.2CH.sub.2OCH.sub.3 0 E-0275 H H H H H 2-CH.sub.2OCF.sub.3 0 E-0276 H H H H H 3-CH.sub.2OCF.sub.3 0 E-0277 H H H H H 4-CH.sub.2OCF.sub.3 0 E-0278 H H H H H 2-CF.sub.2OCH.sub.3 0 E-0279 H H H H H 3-CF.sub.2OCH.sub.3 0 E-0280 H H H H H 4-CF.sub.2OCH.sub.3 0
(361) TABLE-US-00260 TABLE 260 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0281 H H H H H 2-CF.sub.2CF.sub.2OCF.sub.3 0 E-0282 H H H H H 3-CF.sub.2CF.sub.2OCF.sub.3 0 E-0283 H H H H H 4-CF.sub.2CF.sub.2OCF.sub.3 0 E-0284 H H H H H 2-OC(?O)CH.sub.3 0 E-0285 H H H H H 3-OC(?O)CH.sub.3 0 E-0286 H H H H H 4-OC(?O)CH.sub.3 0 E-0287 H H H H H 2-OC(?O)CF.sub.3 0 E-0288 H H H H H 3-OC(?O)CF.sub.3 0 E-0289 H H H H H 4-OC(?O)CF.sub.3 0 E-0290 H H H H H 2-OC(?O)NH.sub.2 0 E-0291 H H H H H 3-OC(?O)NH.sub.2 0 E-0292 H H H H H 4-OC(?O)NH.sub.2 0 E-0293 H H H H H 2-OC(?O)NHCH.sub.3 0 E-0294 H H H H H 3-OC(?O)NHCH.sub.3 0 E-0295 H H H H H 4-OC(?O)NHCH.sub.3 0 E-0296 H H H H H 2-OC(?O)N(CH.sub.3).sub.2 0 E-0297 H H H H H 3-OC(?O)N(CH.sub.3).sub.2 0 E-0298 H H H H H 4-OC(?O)N(CH.sub.3).sub.2 0 E-0299 H H H H H 2-CH.sub.2OC(?O)NH.sub.2 0 E-0300 H H H H H 3-CH.sub.2OC(?O)NH.sub.2 0 E-0301 H H H H H 4-CH.sub.2OC(?O)NH.sub.2 0 E-0302 H H H H H 2-CH.sub.2OC(?O)NHCH.sub.3 0 E-0303 H H H H H 3-CH.sub.2OC(?O)NHCH.sub.3 0 E-0304 H H H H H 4-CH.sub.2OC(?O)NHCH.sub.3 0 E-0305 H H H H H 2-CH.sub.2OC(?O)N(CH.sub.3).sub.2 0 E-0306 H H H H H 3-CH.sub.2OC(?O)N(CH.sub.3).sub.2 0 E-0307 H H H H H 4-CH.sub.2OC(?O)N(CH.sub.3).sub.2 0 E-0308 H H H H H 2-OC(?O)OCH.sub.3 0 E-0309 H H H H H 3-OC(?O)OCH.sub.3 0 E-0310 H H H H H 4-OC(?O)OCH.sub.3 0 E-0311 H H H H H 2-CH.sub.2OC(?O)OCH.sub.3 0 E-0312 H H H H H 3-CH.sub.2OC(?O)OCH.sub.3 0 E-0313 H H H H H 4-CH.sub.2OC(?O)OCH.sub.3 0 E-0314 H H H H H 2-CH.sub.2OC(?O)CH.sub.3 0 E-0315 H H H H H 3-CH.sub.2OC(?O)CH.sub.3 0 E-0316 H H H H H 4-CH.sub.2OC(?O)CH.sub.3 0 E-0317 H H H H H 2-OS(?O).sub.2CH.sub.3 0 E-0318 H H H H H 3-OS(?O).sub.2CH.sub.3 0 E-0319 H H H H H 4-OS(?O).sub.2CH.sub.3 0 E-0320 H H H H H 2-CH.sub.2SCH.sub.3 0 E-0321 H H H H H 3-CH.sub.2SCH.sub.3 0 E-0322 H H H H H 4-CH.sub.2SCH.sub.3 0 E-0323 H H H H H 2-CH.sub.2S(?O)CH.sub.3 0 E-0324 H H H H H 3-CH.sub.2S(?O)CH.sub.3 0 E-0325 H H H H H 4-CH.sub.2S(?O)CH.sub.3 0 E-0326 H H H H H 2-CH.sub.2S(?O).sub.2CH.sub.3 0 E-0327 H H H H H 3-CH.sub.2S(?O).sub.2CH.sub.3 0 E-0328 H H H H H 4-CH.sub.2S(?O).sub.2CH.sub.3 0 E-0329 H H H H H 2-CH.sub.2SCF.sub.3 0 E-0330 H H H H H 3-CH.sub.2SCF.sub.3 0 E-0331 H H H H H 4-CH.sub.2SCF.sub.3 0 E-0332 H H H H H 2-CH.sub.2S(?O)CF.sub.3 0 E-0333 H H H H H 3-CH.sub.2S(?O)CF.sub.3 0 E-0334 H H H H H 4-CH.sub.2S(?O)CF.sub.3 0 E-0335 H H H H H 2-CH.sub.2S(?O).sub.2CF.sub.3 0 E-0336 H H H H H 3-CH.sub.2S(?O).sub.2CF.sub.3 0 E-0337 H H H H H 4-CH.sub.2S(?O).sub.2CF.sub.3 0
(362) TABLE-US-00261 TABLE 261 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0338 H H H H H 2-phenyl 0 E-0339 H H H H H 3-phenyl 0 E-0340 H H H H H 4-phenyl 0 E-0341 H H H H H 2-(phenyloxy) 0 E-0342 H H H H H 3-(phenyloxy) 0 E-0343 H H H H H 4-(phenyloxy) 0 E-0344 H H H H H 2-benzyl 0 E-0345 H H H H H 3-benzyl 0 E-0346 H H H H H 4-benzyl 0 E-0347 H H H H H 2-(benzyloxy) 0 E-0348 H H H H H 3-(benzyloxy) 0 E-0349 H H H H H 4-(benzyloxy) 0 E-0350 H H H H H 2-((2-fluorobenzyl)oxy) 0 E-0351 H H H H H 3-((2-fluorobenzyl)oxy) 0 E-0352 H H H H H 4-((2-fluorobenzyl)oxy) 0 E-0353 H H H H H 2-((3-fluorobenzyl)oxy) 0 E-0354 H H H H H 3-((3-fluorobenzyl)oxy) 0 E-0355 H H H H H 4-((3-fluorobenzyl)oxy) 0 E-0356 H H H H H 2-((4-fluorobenzyl)oxy) 0 E-0357 H H H H H 3-((4-fluorobenzyl)oxy) 0 E-0358 H H H H H 4-((4-fluorobenzyl)oxy) 0 E-0359 H H H H H 2-((2-chlorobenzyl)oxy) 0 E-0360 H H H H H 3-((2-chlorobenzyl)oxy) 0 E-0361 H H H H H 4-((2-chlorobenzyl)oxy) 0 E-0362 H H H H H 2-((3-chlorobenzyl)oxy) 0 E-0363 H H H H H 3-((3-chlorobenzyl)oxy) 0 E-0364 H H H H H 4-((3-chlorobenzyl)oxy) 0 E-0365 H H H H H 2-((4-chlorobenzyl)oxy) 0 E-0366 H H H H H 3-((4-chlorobenzyl)oxy) 0 E-0367 H H H H H 4-((4-chlorobenzyl)oxy) 0 E-0368 H H H H H 2-((2-methybenzyl)oxy) 0 E-0369 H H H H H 3-((2-methybenzyl)oxy) 0 E-0370 H H H H H 4-((2-methybenzyl)oxy) 0 E-0371 H H H H H 2-((3-methybenzyl)oxy) 0 E-0372 H H H H H 3-((3-methybenzyl)oxy) 0 E-0373 H H H H H 4-((3-methybenzyl)oxy) 0 E-0374 H H H H H 2-((4-methybenzyl)oxy) 0 E-0375 H H H H H 3-((4-methybenzyl)oxy) 0 E-0376 H H H H H 4-((4-methybenzyl)oxy) 0 E-0377 H H H H H 2-((2-(trifluoromethyl)benzyl)oxy) 0 E-0378 H H H H H 3-((2-(trifluoromethyl)benzyl)oxy) 0 E-0379 H H H H H 4-((2-(trifluoromethyl)benzyl)oxy) 0 E-0380 H H H H H 2-((3-(trifluoromethyl)benzyl)oxy) 0 E-0381 H H H H H 3-((3-(trifluoromethyl)benzyl)oxy) 0 E-0382 H H H H H 4-((3-(trifluoromethyl)benzyl)oxy) 0 E-0383 H H H H H 2-((4-(trifluoromethyl)benzyl)oxy) 0 E-0384 H H H H H 3-((4-(trifluoromethyl)benzyl)oxy) 0 E-0385 H H H H H 4-((4-(trifluoromethyl)benzyl)oxy) 0 E-0386 H H H H H 2-((2-methoxybenzyl)oxy) 0 E-0387 H H H H H 3-((2-methoxybenzyl)oxy) 0 E-0388 H H H H H 4-((2-methoxybenzyl)oxy) 0 E-0389 H H H H H 2-((3-methoxybenzyl)oxy) 0 E-0390 H H H H H 3-((3-methoxybenzyl)oxy) 0 E-0391 H H H H H 4-((3-methoxybenzyl)oxy) 0 E-0392 H H H H H 2-((4-methoxybenzyl)oxy) 0 E-0393 H H H H H 3-((4-methoxybenzyl)oxy) 0 E-0394 H H H H H 4-((4-methoxybenzyl)oxy) 0
(363) TABLE-US-00262 TABLE 262 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0395 H H H H H 2-((2-(trifluoromethoxy)benzyl)oxy) 0 E-0396 H H H H H 3-((2-(trifluoromethoxy)benzyl)oxy) 0 E-0397 H H H H H 4-((2-(trifluoromethoxy)benzyl)oxy) 0 E-0398 H H H H H 2-((3-(trifluoromethoxy)benzyl)oxy) 0 E-0399 H H H H H 3-((3-(trifluoromethoxy)benzyl)oxy) 0 E-0400 H H H H H 4-((3-(trifluoromethoxy)benzyl)oxy) 0 E-0401 H H H H H 2-((4-(trifluoromethoxy)benzyl)oxy) 0 E-0402 H H H H H 3-((4-(trifluoromethoxy)benzyl)oxy) 0 E-0403 H H H H H 4-((4-(trifluoromethoxy)benzyl)oxy) 0 E-0404 H H H H H 2-((2-(methylthio)benzyl)oxy) 0 E-0405 H H H H H 3-((2-(methylthio)benzyl)oxy) 0 E-0406 H H H H H 4-((2-(methylthio)benzyl)oxy) 0 E-0407 H H H H H 2-((3-(methylthio)benzyl)oxy) 0 E-0408 H H H H H 3-((3-(methylthio)benzyl)oxy) 0 E-0409 H H H H H 4-((3-(methylthio)benzyl)oxy) 0 E-0410 H H H H H 2-((4-(methylthio)benzyl)oxy) 0 E-0411 H H H H H 3-((4-(methylthio)benzyl)oxy) 0 E-0412 H H H H H 4-((4-(methylthio)benzyl)oxy) 0 E-0413 H H H H H 2-((2-(methylsulfinyl)benzyl)oxy) 0 E-0414 H H H H H 3-((2-(methylsulfiny)benzyl)oxy) 0 E-0415 H H H H H 4-((2-(methylsuffiny)benzyl)oxy) 0 E-0416 H H H H H 2-((3-(methylsulfinyl)benzyl)oxy) 0 E-0417 H H H H H 3-((3-(methylsuffinyl)benzyl)oxy) 0 E-0418 H H H H H 4-((3-(methylsulfinyl)benzyl)oxy) 0 E-0419 H H H H H 2-((4-(methylsulfinyl)benzyl)oxy) 0 E-0420 H H H H H 3-((4-(methylsuffinyl)benzyl)oxy) 0 E-0421 H H H H H 4-((4-(methylsulfinyl)benzyl)oxy) 0 E-0422 H H H H H 2-((2-(methylsulfonyl)benzyl)oxy) 0 E-0423 H H H H H 3-((2-(methylsulfonyl)benzyl)oxy) 0 E-0424 H H H H H 4-((2-(methylsulfonyl)benzyl)oxy) 0 E-0425 H H H H H 2-((3-(methylsulfonyl)benzyl)oxy) 0 E-0426 H H H H H 3-((3-(methylsulfonyl)benzyl)oxy) 0 E-0427 H H H H H 4-((3-(methylsulfonyl)benzyl)oxy) 0 E-0428 H H H H H 2-((4-(methylsulfonyl)benzyl)oxy) 0 E-0429 H H H H H 3-((4-(methylsulfonyl)benzyl)oxy) 0 E-0430 H H H H H 4-((4-(methylsulfonyl)benzyl)oxy) 0 E-0431 H H H H H 2-((2-(trifluoromethylthio)benzyl)oxy) 0 E-0432 H H H H H 3-((2-(trifluoromethylthio)benzyl)oxy) 0 E-0433 H H H H H 4-((2-(trifluoromethylthio)benzyl)oxy) 0 E-0434 H H H H H 2-((3-(trifluoromethylthio)benzyl)oxy) 0 E-0435 H H H H H 3-((3-(trifluoromethylthio)benzyl)oxy) 0 E-0436 H H H H H 4-((3-(trifluoromethylthio)benzyl)oxy) 0 E-0437 H H H H H 2-((4-(trifluoromethylthio)benzyl)oxy) 0 E-0438 H H H H H 3-((4-(trifluoromethylthio)benzyl)oxy) 0 E-0439 H H H H H 4-((4-(trifluoromethylthio)benzyl)oxy) 0 E-0440 H H H H H 2-((2-(trifluoromethylsulfinyl)benzyl)oxy) 0 E-0441 H H H H H 3-((2-(trifluoromethylsulfinyl)benzyl)oxy) 0 E-0442 H H H H H 4-((2-(trifluoromethylsulfinyl)benzyl)oxy) 0 E-0443 H H H H H 2-((3-(trifluoromethylsulfinyl)benzyl)oxy) 0 E-0444 H H H H H 3-((3-(trifluoromethylsulfinyl)benzyl)oxy) 0 E-0445 H H H H H 4-((3-(trifluoromethylsulfinyl)benzyl)oxy) 0 E-0446 H H H H H 2-((4-(trifluoromethylsulfinyl)benzyl)oxy) 0 E-0447 H H H H H 3-((4-(trifluoromethylsulfinyl)benzyl)oxy) 0 E-0448 H H H H H 4-((4-(trifluoromethylsulfinyl)benzyl)oxy) 0 E-0449 H H H H H 2-((2-(trifluoromethylsulfinyl)benzyl)oxy) 0 E-0450 H H H H H 3-((2-(trifluoromethylsulfinyl)benzyl)oxy) 0 E-0451 H H H H H 4-((2-(trifluoromethylsulfinyl)benzyl)oxy) 0
(364) TABLE-US-00263 TABLE 263 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0452 H H H H H 2-((3-(trifuoromethylsulfonyl)benzyl)oxy) 0 E-0453 H H H H H 3-((3-(trifuoromethylsulfonyl)benzyl)oxy) 0 E-0454 H H H H H 4-((3-(trifuoromethylsulfonyl)benzyl)oxy) 0 E-0455 H H H H H 2-((4-(trifuoromethylsulfonyl)benzyl)oxy) 0 E-0456 H H H H H 3-((4-(trifuoromethylsulfonyl)benzyl)oxy) 0 E-0457 H H H H H 4 -((4-(trifuoromethylsulfonyl)benzyl)oxy) 0 E-0458 H H H H H 2-((2-aminobenzyl)oxy) 0 E-0459 H H H H H 3-((2-aminobenzyl)oxy) 0 E-0460 H H H H H 4-((2-aminobenzyl)oxy) 0 E-0461 H H H H H 2-((3-aminobenzyl)oxy) 0 E-0462 H H H H H 3-((3-aminobenzyl)oxy) 0 E-0463 H H H H H 4-((3-aminobenzyl)oxy) 0 E-0464 H H H H H 2-((4-aminobenzyl)oxy) 0 E-0465 H H H H H 3-((4-aminobenzyl)oxy) 0 E-0466 H H H H H 4-((4-aminobenzyl)oxy) 0 E-0467 H H H H H 2-((2-(methylamino)benzyl)oxy) 0 E-0468 H H H H H 3-((2-(methylamino)benzyl)oxy) 0 E-0469 H H H H H 4-((2-(methylamino)benzyl)oxy) 0 E-0470 H H H H H 2-((3-(methylamino)benzyl)oxy) 0 E-0471 H H H H H 3-((3-(methylamino)benzyl)oxy) 0 E-0472 H H H H H 4-((3-(methylamino)benzyl)oxy) 0 E-0473 H H H H H 2-((4-(methylamino)benzyl)oxy) 0 E-0474 H H H H H 3-((4-(methylamino)benzyl)oxy) 0 E-0475 H H H H H 4-((4-(methylamino)benzyl)oxy) 0 E-0476 H H H H H 2-((2-(dimethylamino)benzyl)oxy) 0 E-0477 H H H H H 3-((2-(dimethylamino)benzyl)oxy) 0 E-0478 H H H H H 4-((2-(dimethylamino)benzyl)oxy) 0 E-0479 H H H H H 2-((3-(dimethylamino)benzyl)oxy) 0 E-0480 H H H H H 3-((3-(dimethylamino)benzyl)oxy) 0 E-0481 H H H H H 4-((3-(dimethylamino)benzyl)oxy) 0 E-0482 H H H H H 2-((4-(dimethylamino)benzyl)oxy) 0 E-0483 H H H H H 3-((4-(dimethylamino)benzyl)oxy) 0 E-0484 H H H H H 4-((4-(dimethylamino)benzyl)oxy) 0 E-0485 H H H H H 2-((2-cyanobenzyl)oxy) 0 E-0486 H H H H H 3-((2-cyanobenzyl)oxy) 0 E-0487 H H H H H 4-((2-cyanobenzyl)oxy) 0 E-0488 H H H H H 2-((3-cyanobenzyl)oxy) 0 E-0489 H H H H H 3-((3-cyanobenzyl)oxy) 0 E-0490 H H H H H 4-((3-cyanobenzyl)oxy) 0 E-0491 H H H H H 2-((4-cyanobenzyl)oxy) 0 E-0492 H H H H H 3-((4-cyanobenzyl)oxy) 0 E-0493 H H H H H 4-((4-cyanobenzyl)oxy) 0 E-0494 H H H H H 2-((2-nitrobenzyl)oxy) 0 E-0495 H H H H H 3-((2-nitrobenzyl)oxy) 0 E-0496 H H H H H 4-((2-nitrobenzyl)oxy) 0 E-0497 H H H H H 2-((3-nitrobenzyl)oxy) 0 E-0498 H H H H H 3-((3-nitrobenzyl)oxy) 0 E-0499 H H H H H 4-((3-nitrobenzyl)oxy) 0 E-0500 H H H H H 2-((4-nitrobenzyl)oxy) 0 E-0501 H H H H H 3-((4-nitrobenzyl)oxy) 0 E-0502 H H H H H 4-((4-nitrobenzyl)oxy) 0 E-0503 H H H H H 2-NH.sub.2 0 E-0504 H H H H H 3-NH.sub.2 0 E-0505 H H H H H 4-NH.sub.2 0 E-0506 H H H H H 2-NHMe 0 E-0507 H H H H H 3-NHMe 0 E-0508 H H H H H 4-NHMe 0
(365) TABLE-US-00264 TABLE 264 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0509 H H H H H 2-NHEt 0 E-0510 H H H H H 3-NHEt 0 E-0511 H H H H H 4-NHEt 0 E-0512 H H H H H 2-N(Me).sub.2 0 E-0513 H H H H H 3-N(Me).sub.2 0 E-0514 H H H H H 4-N(Me).sub.2 0 E-0515 H H H H H 2-N(Et).sub.2 0 E-0516 H H H H H 3-N(Et).sub.2 0 E-0517 H H H H H 4-N(Et).sub.2 0 E-0518 H H H H H 2-CHO 0 E-0519 H H H H H 3-CHO 0 E-0520 H H H H H 4-CHO 0 E-0521 H H H H H 2-C(?O)OH 0 E-0522 H H H H H 3-C(?O)OH 0 E-0523 H H H H H 4-C(?O)OH 0 E-0524 H H H H H 2-(1,3-dioxolan-2-yl) 0 E-0525 H H H H H 3-(1,3-dioxolan-2-yl) 0 E-0526 H H H H H 4-(1,3-dioxolan-2-yl) 0 E-0527 H H H H H 2-(1,3-dioxolan-2-yl) 0 E-0528 H H H H H 3-(1,3-dioxolan-2-yl) 0 E-0529 H H H H H 4-(1,3-dioxolan-2-yl) 0 E-0530 H H H H H 2-(1H-imidazol-2-yl) 0 E-0531 H H H H H 3-(1H-imidazol-2-yl) 0 E-0532 H H H H H 4-(1H-imidazol-2-yl) 0 E-0533 H H H H H 2-(thiazol-2-yl) 0 E-0534 H H H H H 3-(thiazol-2-yl) 0 E-0535 H H H H H 4-(thiazol-2-yl) 0 E-0536 H H H H H 2-(oxazol-2-yl) 0 E-0537 H H H H H 3-(oxazol-2-yl) 0 E-0538 H H H H H 4-(oxazol-2-yl) 0 E-0539 H H H H H 2-CH?NOH 0 E-0540 H H H H H 3-CH?NOH 0 E-0541 H H H H H 4-CH?NOH 0 E-0542 H H H H H 2-CH?NOMe 0 E-0543 H H H H H 3-CH?NOMe 0 E-0544 H H H H H 4-CH?NOMe 0 E-0545 H H H H H 2-(4,5-d hydro-3-isoxazolyl) 0 E-0546 H H H H H 3-(4,5-d hydro-3-isoxazolyl) 0 E-0547 H H H H H 4-(4,5-d hydro-3-isoxazolyl) 0 E-0548 H H H H H 2-CN 0 E-0549 H H H H H 3-CN 0 E-0550 H H H H H 4-CN 0 E-0551 H H H H H 2-NO.sub.2 0 E-0552 H H H H H 3-NO.sub.2 0 E-0553 H H H H H 4-NO.sub.2 0 E-0554 H H H H H 2,3-F.sub.2 0 E-0555 H H H H H 2,4-F.sub.2 0 E-0556 H H H H H 2,5-F.sub.2 0 E-0557 H H H H H 2,6-F.sub.2 0 E-0558 H H H H H 3,4-F.sub.2 0 E-0559 H H H H H 3,5-F.sub.2 0 E-0560 H H H H H 2-F,3-Cl 0 E-0561 H H H H H 2-F,4-Cl 0 E-0562 H H H H H 2-F,5-Cl 0 E-0563 H H H H H 2-F,6-Cl 0 E-0564 H H H H H 3-F,2-Cl 0 E-0565 H H H H H 3-F,4-Cl 0
(366) TABLE-US-00265 TABLE 265 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0566 H H H H H 3-F,5-Cl 0 E-0567 H H H H H 3-F,6-Cl 0 E-0568 H H H H H 4-F,2-Cl 0 E-0569 H H H H H 4-F,3-Cl 0 E-0570 H H H H H 2-F,3-Me 0 E-0571 H H H H H 2-F,4-Me 0 E-0572 H H H H H 2-F,5-Me 0 E-0573 H H H H H 2-F,6-Me 0 E-0574 H H H H H 3-F,2-Me 0 E-0575 H H H H H 3-F,4-Me 0 E-0576 H H H H H 3-F,5-Me 0 E-0577 H H H H H 3-F,6-Me 0 E-0578 H H H H H 4-F,2-Me 0 E-0579 H H H H H 4-F,3-Me 0 E-0580 H H H H H 2-F,3-CF.sub.3 0 E-0581 H H H H H 2-F,4-CF.sub.3 0 E-0582 H H H H H 2-F,5-CF.sub.3 0 E-0583 H H H H H 2-F,6-CF.sub.3 0 E-0584 H H H H H 3-F,2-CF.sub.3 0 E-0585 H H H H H 3-F,4-CF.sub.3 0 E-0586 H H H H H 3-F,5-CF.sub.3 0 E-0587 H H H H H 3-F,6-CF.sub.3 0 E-0588 H H H H H 4-F,2-CF.sub.3 0 E-0589 H H H H H 4-F,3-CF.sub.3 0 E-0590 H H H H H 2-F,3-OMe 0 E-0591 H H H H H 2-F,4-OMe 0 E-0592 H H H H H 2-F,5-OMe 0 E-0593 H H H H H 2-F,6-OMe 0 E-0594 H H H H H 3-F,2-OMe 0 E-0595 H H H H H 3-F,4-OMe 0 E-0596 H H H H H 3-F,5-OMe 0 E-0597 H H H H H 3-F,6-OMe 0 E-0598 H H H H H 4-F,2-OMe 0 E-0599 H H H H H 4-F,3-OMe 0 E-0600 H H H H H 2,3-Cl.sub.2 0 E-0601 H H H H H 2,4-Cl.sub.2 0 E-0602 H H H H H 2,5-Cl.sub.2 0 E-0603 H H H H H 2,6-Cl.sub.2 0 E-0604 H H H H H 3,4-Cl.sub.2 0 E-0605 H H H H H 3,5-Cl.sub.2 0 E-0606 H H H H H 2-Cl,3-Me 0 E-0607 H H H H H 2-Cl,4-Me 0 E-0608 H H H H H 2-Cl,5-Me 0 E-0609 H H H H H 2-Cl,6-Me 0 E-0610 H H H H H 3-Cl,2-Me 0 E-0611 H H H H H 3-Cl,4-Me 0 E-0612 H H H H H 3-Cl,5-Me 0 E-0613 H H H H H 3-Cl,6-Me 0 E-0614 H H H H H 4-Cl,2-Me 0 E-0615 H H H H H 4-Cl,3-Me 0 E-0616 H H H H H 2-Cl,3-CF.sub.3 0 E-0617 H H H H H 2-Cl,4-CF.sub.3 0 E-0618 H H H H H 2-Cl,5-CF.sub.3 0 E-0619 H H H H H 2-Cl,6-CF.sub.3 0 E-0620 H H H H H 3-Cl,2-CF.sub.3 0 E-0621 H H H H H 3-Cl,4-CF.sub.3 0 E-0622 H H H H H 3-Cl,5-CF.sub.3 0
(367) TABLE-US-00266 TABLE 266 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0623 H H H H H 3-Cl,6-CF.sub.3 0 E-0624 H H H H H 4-Cl,2-CF.sub.3 0 E-0625 H H H H H 4-Cl,3-CF.sub.3 0 E-0626 H H H H H 2-Cl,3-OMe 0 E-0627 H H H H H 2-Cl,4-OMe 0 E-0628 H H H H H 2-Cl,5-OMe 0 E-0629 H H H H H 2-Cl,6-OMe 0 E-0630 H H H H H 3-Cl,2-OMe 0 E-0631 H H H H H 3-Cl,4-OMe 0 E-0632 H H H H H 3-Cl,5-OMe 0 E-0633 H H H H H 3-Cl,6-OMe 0 E-0634 H H H H H 4-Cl,2-OMe 0 E-0635 H H H H H 4-Cl,3-OMe 0 E-0636 H H H H H 2,3-Me.sub.2 0 E-0637 H H H H H 2,4-Me.sub.2 0 E-0638 H H H H H 2,5-Me.sub.2 0 E-0639 H H H H H 2,6-Me.sub.2 0 E-0640 H H H H H 3,4-Me.sub.2 0 E-0641 H H H H H 3,5-Me.sub.2 0 E-0642 H H H H H 2-Me,3-CF.sub.3 0 E-0643 H H H H H 2-Me,4-CF.sub.3 0 E-0644 H H H H H 2-Me,5-CF.sub.3 0 E-0645 H H H H H 2-Me,6-CF.sub.3 0 E-0646 H H H H H 3-Me,2-CF.sub.3 0 E-0647 H H H H H 3-Me,4-CF.sub.3 0 E-0648 H H H H H 3-Me,5-CF.sub.3 0 E-0649 H H H H H 3-Me,6-CF.sub.3 0 E-0650 H H H H H 4-Me,2-CF.sub.3 0 E-0651 H H H H H 4-Me,3-CF.sub.3 0 E-0652 H H H H H 2-Me,3-OMe 0 E-0653 H H H H H 2-Me,4-OMe 0 E-0654 H H H H H 2-Me,5-OMe 0 E-0655 H H H H H 2-Me,6-OMe 0 E-0656 H H H H H 3-Me,2-OMe 0 E-0657 H H H H H 3-Me,4-OMe 0 E-0658 H H H H H 3-Me,5-OMe 0 E-0659 H H H H H 3-Me,6-OMe 0 E-0660 H H H H H 4-Me,2-OMe 0 E-0661 H H H H H 4-Me,3-OMe 0 E-0662 H H H H H 2,3-OMe.sub.2 0 E-0663 H H H H H 2,4-OMe.sub.2 0 E-0664 H H H H H 2,5-OMe.sub.2 0 E-0665 H H H H H 2,6-OMe.sub.2 0 E-0666 H H H H H 3,4-OMe.sub.2 0 E-0667 H H H H H 3,5-OMe.sub.2 0 E-0668 H H H H H 2-OMe,3-CF.sub.3 0 E-0669 H H H H H 2-OMe,4-CF.sub.3 0 E-0670 H H H H H 2-OMe,5-CF.sub.3 0 E-0671 H H H H H 2-OMe,6-CF.sub.3 0 E-0672 H H H H H 3-OMe,2-CF.sub.3 0 E-0673 H H H H H 3-OMe,4-CF.sub.3 0 E-0674 H H H H H 3-OMe,5-CF.sub.3 0 E-0675 H H H H H 3-OMe,6-CF.sub.3 0 E-0676 H H H H H 4-OMe,2-CF.sub.3 0 E-0677 H H H H H 4-OMe,3-CF.sub.3 0 E-0678 H H H H H 2-CHF.sub.2,3-F 0 E-0679 H H H H H 2-CHF.sub.2,4-F 0
(368) TABLE-US-00267 TABLE 267 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0680 H H H H H 2-CHF.sub.2,5-F 0 E-0681 H H H H H 2-CHF.sub.2,6-F 0 E-0682 H H H H H 2-CHF.sub.2,3-Me 0 E-0683 H H H H H 2-CHF.sub.2,4-Me 0 E-0684 H H H H H 2-CHF.sub.2,5-Me 0 E-0685 H H H H H 2-CHF.sub.2,6-Me 0 E-0686 H H H H H 2-cyclopropyl,3-F 0 E-0687 H H H H H 2-cyclopropyl,4-F 0 E-0688 H H H H H 2-cyclopropyl,5-F 0 E-0689 H H H H H 2-cyclopropyl,6-F 0 E-0690 H H H H H 2-cyclopropyl,3-Me 0 E-0691 H H H H H 2-cyclopropyl,4-Me 0 E-0692 H H H H H 2-cyclopropyl,5-Me 0 E-0693 H H H H H 2-cyclopropyl,6-Me 0 E-0694 H H H H H 2-ethenyl,3-F 0 E-0695 H H H H H 2-ethenyl,4-F 0 E-0696 H H H H H 2-ethenyl,5-F 0 E-0697 H H H H H 2-ethenyl,6-F 0 E-0698 H H H H H 2-ethenyl,3-Me 0 E-0699 H H H H H 2-ethenyl,4-Me 0 E-0700 H H H H H 2-ethenyl,5-Me 0 E-0701 H H H H H 2-ethenyl,6-Me 0 E-0702 H H H H H 2-OEt,3-F 0 E-0703 H H H H H 2-OEt,4-F 0 E-0704 H H H H H 2-OEt,5-F 0 E-0705 H H H H H 2-OEt,6-F 0 E-0706 H H H H H 2-OEt,3-Cl 0 E-0707 H H H H H 2-OEt,4-Cl 0 E-0708 H H H H H 2-OEt,5-Cl 0 E-0709 H H H H H 2-OEt,6-Cl 0 E-0710 H H H H H 2-OEt,3-Me 0 E-0711 H H H H H 2-OEt,4-Me 0 E-0712 H H H H H 2-OEt,5-Me 0 E-0713 H H H H H 2-OEt,6-Me 0 E-0714 H H H H H 2-OPr,3-F 0 E-0715 H H H H H 2-OPr,4-F 0 E-0716 H H H H H 2-OPr,5-F 0 E-0717 H H H H H 2-OPr,6-F 0 E-0718 H H H H H 2-OPr,3-Me 0 E-0719 H H H H H 2-OPr,4-Me 0 E-0720 H H H H H 2-OPr,5-Me 0 E-0721 H H H H H 2-OPr,6-Me 0 E-0722 H H H H H 2-O(i-Pr),3-F 0 E-0723 H H H H H 2-O(i-Pr),4-F 0 E-0724 H H H H H 2-O(i-Pr),5-F 0 E-0725 H H H H H 2-O(i-Pr),6-F 0 E-0726 H H H H H 2-O(i-Pr),3-Me 0 E-0727 H H H H H 2-O(i-Pr),4-Me 0 E-0728 H H H H H 2-O(i-Pr),5-Me 0 E-0729 H H H H H 2-O(i-Pr),6-Me 0 E-0730 H H H H H 2-OCF.sub.3,3-F 0 E-0731 H H H H H 2-OCF.sub.3,4-F 0 E-0732 H H H H H 2-OCF.sub.3,5-F 0 E-0733 H H H H H 2-OCF.sub.3,6-F 0 E-0734 H H H H H 2-OCF.sub.3,3-Me 0 E-0735 H H H H H 2-OCF.sub.3,4-Me 0 E-0736 H H H H H 2-OCF.sub.3,5-Me 0
(369) TABLE-US-00268 TABLE 268 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0737 H H H H H 2-OCF.sub.3,6-Me 0 E-0738 H H H H H 2-OCHF.sub.2,3-F 0 E-0739 H H H H H 2-OCHF.sub.2,4-F 0 E-0740 H H H H H 2-OCHF.sub.2,5-F 0 E-0741 H H H H H 2-OCHF.sub.2,6-F 0 E-0742 H H H H H 2-OCHF.sub.2,3-Me 0 E-0743 H H H H H 2-OCHF.sub.2,4-Me 0 E-0744 H H H H H 2-OCHF.sub.2,5-Me 0 E-0745 H H H H H 2-OCHF.sub.2,6-Me 0 E-0746 H H H H H 2-(cyclopropyloxy),3-F 0 E-0747 H H H H H 2-(cyclopropyloxy),4-F 0 E-0748 H H H H H 2-(cyclopropyloxy),5-F 0 E-0749 H H H H H 2-(cyclopropyloxy),6-F 0 E-0750 H H H H H 2-(cyclopropyloxy),3-Me 0 E-0751 H H H H H 2-(cyclopropyloxy),4-Me 0 E-0752 H H H H H 2-(cyclopropyloxy),5-Me 0 E-0753 H H H H H 2-(cyclopropyloxy),6-Me 0 E-0754 H H H H H 2-(oxiran-2-yl),3-F 0 E-0755 H H H H H 2-(oxiran-2-yl),4-F 0 E-0756 H H H H H 2-(oxiran-2-yl),5-F 0 E-0757 H H H H H 2-(oxiran-2-yl),6-F 0 E-0758 H H H H H 2-(oxiran-2-yl),3-Me 0 E-0759 H H H H H 2-(oxiran-2-yl),4-Me 0 E-0760 H H H H H 2-(oxiran-2-yl),5-Me 0 E-0761 H H H H H 2-(oxiran-2-yl),6-Me 0 E-0762 H H H H H 2-(oxiran-2-ylmethyl),3-F 0 E-0763 H H H H H 2-(oxiran-2-ylmethyl),4-F 0 E-0764 H H H H H 2-(oxiran-2-ylmethyl),5-F 0 E-0765 H H H H H 2-(oxiran-2-ylmethyl),6-F 0 E-0766 H H H H H 2-(oxiran-2-ylmethyl),3-Me 0 E-0767 H H H H H 2-(oxiran-2-ylmethyl),4-Me 0 E-0768 H H H H H 2-(oxiran-2-ylmethyl),5-Me 0 E-0769 H H H H H 2-(oxiran-2-ylmethyl),6-Me 0 E-0770 H H H H H 2-SMe,3-F 0 E-0771 H H H H H 2-SMe,4-F 0 E-0772 H H H H H 2-SMe,5-F 0 E-0773 H H H H H 2-SMe,6-F 0 E-0774 H H H H H 2-SMe,3-Me 0 E-0775 H H H H H 2-SMe,4-Me 0 E-0776 H H H H H 2-SMe,5-Me 0 E-0777 H H H H H 2-SMe,6-Me 0 E-0778 H H H H H 2-SEt,3-F 0 E-0779 H H H H H 2-SEt,4-F 0 E-0780 H H H H H 2-SEt,5-F 0 E-0781 H H H H H 2-SEt,6-F 0 E-0782 H H H H H 2-SEt,3-Me 0 E-0783 H H H H H 2-SEt,4-Me 0 E-0784 H H H H H 2-SEt,5-Me 0 E-0785 H H H H H 2-SEt,6-Me 0 E-0786 H H H H H 2-S(?O)Me,3-F 0 E-0787 H H H H H 2-S(?O)Me,4-F 0 E-0788 H H H H H 2-S(?O)Me,5-F 0 E-0789 H H H H H 2-S(?O)Me,6-F 0 E-0790 H H H H H 3-S(?O)Me,2-F 0 E-0791 H H H H H 3-S(?O)Me,4-F 0 E-0792 H H H H H 3-S(?O)Me,5-F 0 E-0793 H H H H H 3-S(?O)Me,6-F 0
(370) TABLE-US-00269 TABLE 269 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0794 H H H H H 2-S(?O)Me,3-Me 0 E-0795 H H H H H 2-S(?O)Me,4-Me 0 E-0796 H H H H H 2-S(?O)Me,5-Me 0 E-0797 H H H H H 2-S(?O)Me,6-Me 0 E-0798 H H H H H 3-S(?O)Me,2-Me 0 E-0799 H H H H H 3-S(?O)Me,4-Me 0 E-0800 H H H H H 3-S(?O)Me,5-Me 0 E-0801 H H H H H 3-S(?O)Me,6-Me 0 E-0802 H H H H H 2-S(?O).sub.2Me,3-F 0 E-0803 H H H H H 2-S(?O).sub.2Me ,4-F 0 E-0804 H H H H H 2-S(?O).sub.2Me,5-F 0 E-0805 H H H H H 2-S(?O).sub.2Me,6-F 0 E-0806 H H H H H 2-S(?O).sub.2Me,3-Me 0 E-0807 H H H H H 2-S(?O).sub.2Me,4-Me 0 E-0808 H H H H H 2-S(?O).sub.2Me,5-Me 0 E-0809 H H H H H 2-S(?O).sub.2Me,6-Me 0 E-0810 H H H H H 2-SCF.sub.3,3-F 0 E-0811 H H H H H 2-SCF.sub.3,4-F 0 E-0812 H H H H H 2-SCF.sub.3,5-F 0 E-0813 H H H H H 2-SCF.sub.3,6-F 0 E-0814 H H H H H 2-SCF.sub.3,3-Me 0 E-0815 H H H H H 2-SCF.sub.3,4-Me 0 E-0816 H H H H H 2-SCF.sub.3,5-Me 0 E-0817 H H H H H 2-SCF.sub.3,6-Me 0 E-0818 H H H H H 2-S(?O)CF.sub.3,3-F 0 E-0819 H H H H H 2-S(?O)CF.sub.3,4-F 0 E-0820 H H H H H 2-S(?O)CF.sub.3,5-F 0 E-0821 H H H H H 2-S(?O)CF.sub.3,6-F 0 E-0822 H H H H H 2-S(?O)CF.sub.3,3-Me 0 E-0823 H H H H H 2-S(?O)CF.sub.3,4-Me 0 E-0824 H H H H H 2-S(?O)CF.sub.3,5-Me 0 E-0825 H H H H H 2-S(?O)CF.sub.3,6-Me 0 E-0826 H H H H H 2-S(?O)CF.sub.3,3-F 0 E-0827 H H H H H 2-S(?O)CF.sub.3,4-F 0 E-0828 H H H H H 2-S(?O)CF.sub.3,5-F 0 E-0829 H H H H H 2-S(?O)CF.sub.3,6-F 0 E-0830 H H H H H 2-S(?O).sub.2CF.sub.3,3-Me 0 E-0831 H H H H H 2-S(?O).sub.2CF.sub.3,4-Me 0 E-0832 H H H H H 2-S(?O).sub.2CF.sub.3,5-Me 0 E-0833 H H H H H 2-S(?O).sub.2CF.sub.3,6-Me 0 E-0834 H H H H H 2-(cyclopropylthio),3-F 0 E-0835 H H H H H 2-(cyclopropylthio),4-F 0 E-0836 H H H H H 2-(cyclopropylthio),5-F 0 E-0837 H H H H H 2-(cyclopropylthio),6-F 0 E-0838 H H H H H 2-(cyclopropylthio),3-Me 0 E-0839 H H H H H 2-(cyclopropylthio),4-Me 0 E-0840 H H H H H 2-(cyclopropylthio),5-Me 0 E-0841 H H H H H 2-(cyclopropylthio),6-Me 0 E-0842 H H H H H 2-C(?O)Me,3-F 0 E-0843 H H H H H 2-C(?O)Me,4-F 0 E-0844 H H H H H 2-C(?O)Me,5-F 0 E-0845 H H H H H 2-C(?O)Me,6-F 0 E-0846 H H H H H 2-C(?O)Me,3-Me 0 E-0847 H H H H H 2-C(?O)Me,4-Me 0 E-0848 H H H H H 2-C(?O)Me,5-Me 0 E-0849 H H H H H 2-C(?O)Me,6-Me 0 E-0850 H H H H H 3-C(?O)Me,2-F 0
(371) TABLE-US-00270 TABLE 270 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0851 H H H H H 3-C(?O)Me,4-F 0 E-0852 H H H H H 3-C(?O)Me,5-F 0 E-0853 H H H H H 3-C(?O)Me,6-F 0 E-0854 H H H H H 3-C(?O)Me,2-Me 0 E-0855 H H H H H 3-C(?O)Me,4-Me 0 E-0856 H H H H H 3-C(?O)Me,5-Me 0 E-0857 H H H H H 3-C(?O)Me,6-Me 0 E-0858 H H H H H 2-C(?O)OMe,3-F 0 E-0859 H H H H H 2-C(?O)OMe,4-F 0 E-0860 H H H H H 2-C(?O)OMe,5-F 0 E-0861 H H H H H 2-C(?O)OMe,6 F 0 E-0862 H H H H H 2-C(?O)OMe,3-Me 0 E-0863 H H H H H 2-C(?O)OMe,4-Me 0 E-0864 H H H H H 2-C(?O)OMe,5-Me 0 E-0865 H H H H H 2-C(?O)OMe,6-Me 0 E-0866 H H H H H 2-C(?O)OEt,3-F 0 E-0867 H H H H H 2-C(?O)OEt,4-F 0 E-0868 H H H H H 2-C(?O)OEt,5-F 0 E-0869 H H H H H 2-C(?O)OEt,6-F 0 E-0870 H H H H H 2-C(?O)OEt,3-Me 0 E-0871 H H H H H 2-C(?O)OEt,4-Me 0 E-0872 H H H H H 2-C(?O)OEt,5-Me 0 E-0873 H H H H H 2-C(?O)OEt,6-Me 0 E-0874 H H H H H 2-C(?O)NH.sub.2,3-F 0 E-0875 H H H H H 2-C(?O)NH.sub.2,4-F 0 E-0876 H H H H H 2-C(?O)NH.sub.2,5-F 0 E-0877 H H H H H 2-C(?O)NH.sub.2,6-F 0 E-0878 H H H H H 2-C(?O)NH.sub.2,3-Me 0 E-0879 H H H H H 2-C(?O)NH.sub.2,4-Me 0 E-0880 H H H H H 2-C(?O)NH.sub.2,5-Me 0 E-0881 H H H H H 2-C(?O)NH.sub.2,6-Me 0 E-0882 H H H H H 2-C(?O)NHMe,3-F 0 E-0883 H H H H H 2-C(?O)NHMe,4-F 0 E-0884 H H H H H 2-C(?O)NHMe,5-F 0 E-0885 H H H H H 2-C(?O)NHMe,6-F 0 E-0886 H H H H H 2-C(?O)NHMe,3-Me 0 E-0887 H H H H H 2-C(?O)NHMe,4-Me 0 E-0888 H H H H H 2-C(?O)NHMe,5-Me 0 E-0889 H H H H H 2-C(?O)NHMe,6-Me 0 E-0890 H H H H H 2-C(?O)NHMe.sub.2,3-F 0 E-0891 H H H H H 2-C(?O)NHMe.sub.2,4-F 0 E-0892 H H H H H 2-C(?O)NHMe.sub.2,5-F 0 E-0893 H H H H H 2-C(?O)NHMe.sub.2,6-F 0 E-0894 H H H H H 2-C(?O)NHMe.sub.2,3-Me 0 E-0895 H H H H H 2-C(?O)NHMe.sub.2,4-Me 0 E-0896 H H H H H 2-C(?O)NHMe.sub.2,5-Me 0 E-0897 H H H H H 2-C(?O)NHMe.sub.2,6-Me 0 E-0898 H H H H H 2-CH.sub.2OH,3-F 0 E-0899 H H H H H 2-CH.sub.2OH,4-F 0 E-0900 H H H H H 2-CH.sub.2OH,5-F 0 E-0901 H H H H H 2-CH.sub.2OH,6-F 0 E-0902 H H H H H 2-CH.sub.2OH,3-Me 0 E-0903 H H H H H 2-CH.sub.2OH,4-Me 0 E-0904 H H H H H 2-CH.sub.2OH,5-Me 0 E-0905 H H H H H 2-CH.sub.2OH,6-Me 0 E-0906 H H H H H 2-CH.sub.2OCH.sub.3,3-F 0 E-0907 H H H H H 2-CH.sub.2OCH.sub.3,4-F 0
(372) TABLE-US-00271 TABLE 271 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0908 H H H H H 2-CH.sub.2OCH.sub.3,5-F 0 E-0909 H H H H H 2-CH.sub.2OCH.sub.3,6-F 0 E-0910 H H H H H 2-CH.sub.2OCH.sub.3,3-Me 0 E-0911 H H H H H 2-CH.sub.2OCH.sub.3,4-Me 0 E-0912 H H H H H 2-CH.sub.2OCH.sub.3,5-Me 0 E-0913 H H H H H 2-CH.sub.2OCH.sub.3,6-Me 0 E-0914 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,3-F 0 E-0915 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,4-F 0 E-0916 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,5-F 0 E-0917 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-F 0 E-0918 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,3-Me 0 E-0919 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,4-Me 0 E-0920 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,5-Me 0 E-0921 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Me 0 E-0922 H H H H H 2-OC(?O)CH.sub.3,3-F 0 E-0923 H H H H H 2-OC(?O)CH.sub.3,4-F 0 E-0924 H H H H H 2-OC(?O)CH.sub.3,5-F 0 E-0925 H H H H H 2-OC(?O)CH.sub.3,6-F 0 E-0926 H H H H H 2-OC(?O)CH.sub.3,3-Me 0 E-0927 H H H H H 2-OC(?O)CH.sub.3,4-Me 0 E-0928 H H H H H 2-OC(?O)CH.sub.3,5-Me 0 E-0929 H H H H H 2-OC(?O)CH.sub.3,6-Me 0 E-0930 H H H H H 2-OS(?O).sub.2CH.sub.3,3-F 0 E-0931 H H H H H 2-OS(?O).sub.2CH.sub.3,4-F 0 E-0932 H H H H H 2-OS(?O).sub.2CH.sub.3,5-F 0 E-0933 H H H H H 2-OS(?O).sub.2CH.sub.3,6-F 0 E-0934 H H H H H 2-OS(?O).sub.2CH.sub.3,3-Me 0 E-0935 H H H H H 2-OS(?O).sub.2CH.sub.3,4-Me 0 E-0936 H H H H H 2-OS(?O).sub.2CH.sub.3,5-Me 0 E-0937 H H H H H 2-OS(?O).sub.2CH.sub.3,6-Me 0 E-0938 H H H H H 2-CH.sub.2SCH.sub.3,3-F 0 E-0939 H H H H H 2-CH.sub.2SCH.sub.3,4-F 0 E-0940 H H H H H 2-CH.sub.2SCH.sub.3,5-F 0 E-0941 H H H H H 2-CH.sub.2SCH.sub.3,6 F 0 E-0942 H H H H H 2-CH.sub.2SCH.sub.3,3-Me 0 E-0943 H H H H H 2-CH.sub.2SCH.sub.3,4-Me 0 E-0944 H H H H H 2-CH.sub.2SCH.sub.3,5-Me 0 E-0945 H H H H H 2-CH.sub.2SCH.sub.3,6-Me 0 E-0946 H H H H H 2-CH.sub.2SCF.sub.3,3-F 0 E-0947 H H H H H 2-CH.sub.2SCF.sub.3,4-F 0 E-0948 H H H H H 2-CH.sub.2SCF.sub.3,5-F 0 E-0949 H H H H H 2-CH.sub.2SCF.sub.3,6-F 0 E-0950 H H H H H 2-CH.sub.2SCF.sub.3,3-Me 0 E-0951 H H H H H 2-CH.sub.2SCF.sub.3,4-Me 0 E-0952 H H H H H 2-CH.sub.2SCF.sub.3,5-Me 0 E-0953 H H H H H 2-CH.sub.2SCF.sub.3,6-Me 0 E-0954 H H H H H 2-(benzyloxy),3-F 0 E-0955 H H H H H 2-(benzyloxy),4-F 0 E-0956 H H H H H 2-(benzyloxy),5-F 0 E-0957 H H H H H 2-(benzyloxy),6-F 0 E-0958 H H H H H 2-(benzyloxy),3-Me 0 E-0959 H H H H H 2-(benzyloxy),4-Me 0 E-0960 H H H H H 2-(benzyloxy),5-Me 0 E-0961 H H H H H 2-(benzyloxy),6-Me 0 E-0962 H H H H H 2-NH.sub.2,3-F 0 E-0963 H H H H H 2-NH.sub.2,4-F 0 E-0964 H H H H H 2-NH.sub.2,5-F 0
(373) TABLE-US-00272 TABLE 272 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-0965 H H H H H 2-NH.sub.2,6-F 0 E-0966 H H H H H 2-NH.sub.2,3-Me 0 E-0967 H H H H H 2-NH.sub.2,4-Me 0 E-0968 H H H H H 2-NH.sub.2,5-Me 0 E-0969 H H H H H 2-NH.sub.2,6-Me 0 E-0970 H H H H H 2-NHMe,3F 0 E-0971 H H H H H 2-NHMe,4-F 0 E-0972 H H H H H 2-NHMe,5-F 0 E-0973 H H H H H 2-NHMe,6-F 0 E-0974 H H H H H 2-NHMe,3-Me 0 E-0975 H H H H H 2-NHMe,4-Me 0 E-0976 H H H H H 2-NHMe,5-Me 0 E-0977 H H H H H 2-NHMe,6-Me 0 E-0978 H H H H H 2-NHEt,3-F 0 E-0979 H H H H H 2-NHEt,4-F 0 E-0980 H H H H H 2-NHEt,5-F 0 E-0981 H H H H H 2-NHEt,6-F 0 E-0982 H H H H H 2-NHEt,3-Me 0 E-0983 H H H H H 2-NHEt,4-Me 0 E-0984 H H H H H 2-NHEt,5-Me 0 E-0985 H H H H H 2-NHEt,6-Me 0 E-0986 H H H H H 2-NMe.sub.2,3-F 0 E-0987 H H H H H 2-NMe.sub.2,4-F 0 E-0988 H H H H H 2-NMe.sub.2,5-F 0 E-0989 H H H H H 2-NMe.sub.2,6-F 0 E-0990 H H H H H 2-NMe.sub.2,3-Me 0 E-0991 H H H H H 2-NMe.sub.2,4-Me 0 E-0992 H H H H H 2-NMe.sub.2,5-Me 0 E-0993 H H H H H 2-NMe.sub.2,6-Me 0 E-0994 H H H H H 2-NEt.sub.2,3-F 0 E-0995 H H H H H 2-NEt.sub.2,4-F 0 E-0996 H H H H H 2-NEt.sub.2,5-F 0 E-0997 H H H H H 2-NEt.sub.2,6-F 0 E-0998 H H H H H 2-NEt.sub.2,3-Me 0 E-0999 H H H H H 2-NEt.sub.2,4-Me 0 E-1000 H H H H H 2-NEt.sub.2,5-Me 0 E-1001 H H H H H 2-NEt.sub.2,6-Me 0 E-1002 H H H H H 2-CHO,3-F 0 E-1003 H H H H H 2-CHO,4-F 0 E-1004 H H H H H 2-CHO,5-F 0 E-1005 H H H H H 2-CHO,6-F 0 E-1006 H H H H H 2-CHO,3-Me 0 E-1007 H H H H H 2-CHO,4-Me 0 E-1008 H H H H H 2-CHO,5-Me 0 E-1009 H H H H H 2-CHO,6-Me 0 E-1010 H H H H H 2-C(?O)OH,3-F 0 E-1011 H H H H H 2-C(?O)OH,4-F 0 E-1012 H H H H H 2-C(?O)OH,5-F 0 E-1013 H H H H H 2-C(?O)OH,6-F 0 E-1014 H H H H H 2-C(?O)OH,3-Me 0 E-1015 H H H H H 2-C(?O)OH,4-Me 0 E-1016 H H H H H 2-C(?O)OH,5-Me 0 E-1017 H H H H H 2-C(?O)OH,6-Me 0 E-1018 H H H H H 2-(1,3-dioxolan-2-yl),3-F 0 E-1019 H H H H H 2-(1,3-dioxolan-2-yl),4-F 0 E-1020 H H H H H 2-(1,3-dioxolan-2-yl),5-F 0 E-1021 H H H H H 2-(1,3-dioxolan-2-yl),6-F 0
(374) TABLE-US-00273 TABLE 273 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-1022 H H H H H 2-(1,3-dioxolan-2-yl),3-Me 0 E-1023 H H H H H 2-(1,3-dioxolan-2-yl),4-Me 0 E-1024 H H H H H 2-(1,3-dioxolan-2-yl),5-Me 0 E-1025 H H H H H 2-(1,3-dioxolan-2-yl),6-Me 0 E-1026 H H H H H 2-(1,3-dioxolan-2-yl),3-F 0 E-1027 H H H H H 2-(1,3-dioxolan-2-yl),4-F 0 E-1028 H H H H H 2-(1,3-dioxolan-2-yl),5 F 0 E-1029 H H H H H 2-(1,3-dioxolan-2-yl),6-F 0 E-1030 H H H H H 2-(1,3-dioxolan-2-yl),3-Me 0 E-1031 H H H H H 2-(1,3-dioxolan-2-yl),4-Me 0 E-1032 H H H H H 2-(1,3-dioxolan-2-yl),5-Me 0 E-1033 H H H H H 2-(1,3-dioxolan-2-yl),6-Me 0 E-1034 H H H H H 2-(thiazol-2-yl),3-F 0 E-1035 H H H H H 2-(thiazol-2-yl),4-F 0 E-1036 H H H H H 2-(thiazol-2-yl),5-F 0 E-1037 H H H H H 2-(thiazol-2-yl),6-F 0 E-1038 H H H H H 2-(thiazol-2-yl),3-Me 0 E-1039 H H H H H 2-(thiazol-2-yl),4-Me 0 E-1040 H H H H H 2-(thiazol-2-yl),5-Me 0 E-1041 H H H H H 2-(thiazol-2-yl),6-Me 0 E-1042 H H H H H 2-(oxazol-2-yl),3-F 0 E-1043 H H H H H 2-(oxazol-2-yl),4-F 0 E-1044 H H H H H 2-(oxazol-2-yl),5-F 0 E-1045 H H H H H 2-(oxazol-2-yl),6-F 0 E-1046 H H H H H 2-(oxazol-2-yl),3-Me 0 E-1047 H H H H H 2-(oxazol-2-yl),4-Me 0 E-1048 H H H H H 2-(oxazol-2-yl),5-Me 0 E-1049 H H H H H 2-(oxazol-2-yl),6-Me 0 E-1050 H H H H H 2-CH?NOH,3-F 0 E-1051 H H H H H 2-CH?NOH,4-F 0 E-1052 H H H H H 2-CH?NOH,5-F 0 E-1053 H H H H H 2-CH?NOH,6-F 0 E-1054 H H H H H 2-CH?NOH,3-Me 0 E-1055 H H H H H 2-CH?NOH,4-Me 0 E-1056 H H H H H 2-CH?NOH,5-Me 0 E-1057 H H H H H 2-CH?NOH,6-Me 0 E-1058 H H H H H 2-CH?NOMe,3-F 0 E-1059 H H H H H 2-CH?NOMe,4-F 0 E-1060 H H H H H 2-CH?NOMe,5-F 0 E-1061 H H H H H 2-CH?NOMe,6-F 0 E-1062 H H H H H 2-CH?NOMe,3-Me 0 E-1063 H H H H H 2-CH?NOMe,4-Me 0 E-1064 H H H H H 2-CH?NOMe,5-Me 0 E-1065 H H H H H 2-CH?NOMe,6-Me 0 E-1066 H H H H H 2-CN,3-F 0 E-1067 H H H H H 2-CN,4-F 0 E-1068 H H H H H 2-CN,5-F 0 E-1069 H H H H H 2-CN,6-F 0 E-1070 H H H H H 2-CN,3-Cl 0 E-1071 H H H H H 2-CN,4-Cl 0 E-1072 H H H H H 2-CN,5-Cl 0 E-1073 H H H H H 2-CN,6-C 0 E-1074 H H H H H 2-CN,3-Me 0 E-1075 H H H H H 2-CN,4-Me 0 E-1076 H H H H H 2-CN,5-Me 0 E-1077 H H H H H 2-CN,6-Me 0 E-1078 H H H H H 2-CN,3-OMe 0
(375) TABLE-US-00274 TABLE 274 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-1079 H H H H H 2-CN,4-OMe 0 E-1080 H H H H H 2-CN,5-OMe 0 E-1081 H H H H H 2-CN,6-OMe 0 E-1082 H H H H H 3-CN,2-F 0 E-1083 H H H H H 3-CN,4-F 0 E-1084 H H H H H 3-CN,5-F 0 E-1085 H H H H H 3-CN,6-F 0 E-1086 H H H H H 3-CN,2-Cl 0 E-1087 H H H H H 3-CN,4-Cl 0 E-1088 H H H H H 3-CN,5-Cl 0 E-1089 H H H H H 3-CN,6-Cl 0 E-1090 H H H H H 3-CN,2-Me 0 E-1091 H H H H H 3-CN,4-Me 0 E-1092 H H H H H 3-CN,5 Me 0 E-1093 H H H H H 3-CN,6-Me 0 E-1094 H H H H H 3-CN,2-OMe 0 E-1095 H H H H H 3-CN,4-OMe 0 E-1096 H H H H H 3-CN,5-OMe 0 E-1097 H H H H H 3-CN,6-OMe 0 E-1098 H H H H H 4-CN,2-F 0 E-1099 H H H H H 4-CN,3-F 0 E-1100 H H H H H 4-CN,2-Cl 0 E-1101 H H H H H 4-CN,3-Cl 0 E-1102 H H H H H 4-CN,2-Me 0 E-1103 H H H H H 4-CN,3-Me 0 E-1104 H H H H H 4-CN,2-OMe 0 E-1105 H H H H H 4-CN,3-OMe 0 E-1106 H H H H H 2-NO.sub.2,3-F 0 E-1107 H H H H H 2-NO.sub.2,4-F 0 E-1108 H H H H H 2-NO.sub.2,5-F 0 E-1109 H H H H H 2-NO.sub.2,6-F 0 E-1110 H H H H H 2-NO.sub.2,3-Me 0 E-1111 H H H H H 2-NO.sub.2,4-Me 0 E-1112 H H H H H 2-NO.sub.2,5-Me 0 E-1113 H H H H H 2-NO.sub.2,6-Me 0 E-1114 H H H H H 2-Me,3,4-F.sub.2 0 E-1115 H H H H H 2-Me,3,5-F.sub.2 0 E-1116 H H H H H 2-Me,3,6-F.sub.2 0 E-1117 H H H H H 2-Me,4,5-F.sub.2 0 E-1118 H H H H H 2-OMe,3,4-F.sub.2 0 E-1119 H H H H H 2-OMe,3,5-F.sub.2 0 E-1120 H H H H H 2-OMe,3,6-F.sub.2 0 E-1121 H H H H H 2-OMe,4,5-F.sub.2 0 E-1122 H H H H H 2-(CH.sub.2).sub.3-3 0 E-1123 H H H H H 2-(CH.sub.2).sub.4-3 0 E-1124 H H H H H 2-(OCH.sub.2CH.sub.2)-3 0 E-1125 H H H H H 2-(OCH.sub.2CH.sub.2CH.sub.2)-3 0 E-1126 H H H H H 2-(CH.sub.2CH.sub.2O)-3 0 E-1127 H H H H H 2-(CH.sub.2CH.sub.2CH.sub.2O)-3 0 E-1128 H H H H H 3-(CH.sub.2).sub.3-4 0 E-1129 H H H H H 3-(CH.sub.2).sub.4-4 0 E-1130 H H H H H 3-(OCH.sub.2CH.sub.2)-4 0 E-1131 H H H H H 3-(OCH.sub.2CH.sub.2CH.sub.2)-4 0 E-1132 H H H H H 3-(CH.sub.2CH.sub.2O)-4 0 E-1133 H H H H H 3-(CH.sub.2CH.sub.2CH.sub.2O)-4 0 E-1134 H H H H H 2-(OCH.sub.2O)-3 0 E-1135 H H H H H 3-OCH.sub.2O)-4 0
(376) TABLE-US-00275 TABLE 275 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-1136 H H H H H 2-(OCH.sub.2CH.sub.2O)-3 0 E-1137 H H H H H 3-(OCH.sub.2CH.sub.2O)-4 0 E-1138 H H H H H 2-(OCF.sub.2O)-3 0 E-1139 H H H H H 3-(OCF.sub.2O)-4 0 E-1140 H H H H H 2-Me,6-Et 0 E-1141 H H H H H 2-CH.sub.2OTBS 0 E-1142 H H H H H 2-cyclopropyl,3-OMe 0 E-1143 H H H H H 2-cyclopropyl,4-OMe 0 E-1144 H H H H H 2-cyclopropyl,5-OMe 0 E-1145 H H H H H 2-cyclopropyl,6-OMe 0 E-1146 H H H H H 2-Me,3-OMe,6 Me 0 E-1147 H H H H H 2-Me,4-OMe,6-Me 0 E-1148 H H H H H 2-OMe,3-Me,6-Me 0 E-1149 H H H H H 2-OMe,5-Me,6-Me 0 E-1150 H H H H H 2-OMe,3-F,6-Me 0 E-1151 H H H H H 2-OMe,5-F,6-Me 0 E-1152 H H H H H 2-OMe,5-Me,6-F 0 E-1153 H H H H H 2-Cl,3-Me,6-F 0 E-1154 H H H H H 2-Cl,5-Me,6-F 0 E-1155 H H H H H 2-Cl,3-OMe,6-F 0 E-1156 H H H H H 2-Cl,5-OMe,6-F 0 E-1157 H H H H H 2-Me,5-Et 0 E-1158 H H H H H 2,6-Et.sub.2 0 E-1159 H H H H H 2-Et,6-F 0 E-1160 H H H H H 2-CH.sub.2OCH.sub.3,6-Cl 0 E-1161 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 0 E-1162 H H H H H 2-OMe,5-CH?NOMe 0 E-1163 H H H H H 2-CH.sub.2NMe.sub.2 0 E-1164 H H H H H 2-CH.sub.2OCH.sub.3,6-CF.sub.3 0 E-1165 H H F H H 2-Me 0
(377) TABLE-US-00276 TABLE 276
(378) TABLE-US-00277 TABLE 277 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5053 H H H H H 2-CF.sub.2Cl 1 E-5054 H H H H H 3-CF.sub.2Cl 1 E-5055 H H H H H 4-CF.sub.2Cl 1 E-5056 H H H H H 2-CF(CF.sub.3).sub.2 1 E-5057 H H H H H 3-CF(CF.sub.3).sub.2 1 E-5058 H H H H H 4-CF(CF.sub.3).sub.2 1 E-5059 H H H H H 2-cyclopropyl 1 E-5060 H H H H H 3-cyclopropyl 1 E-5061 H H H H H 4-cyclopropyl 1 E-5062 H H H H H 2-cyclobutyl 1 E-5063 H H H H H 3-cyclobutyl 1 E-5064 H H H H H 4-cyclobutyl 1 E-5065 H H H H H 2-cyclopentyl 1 E-5066 H H H H H 3-cyclopentyl 1 E-5067 H H H H H 4-cyclopentyl 1 E-5068 H H H H H 2-(cyclopropylmethyl) 1 E-5069 H H H H H 3-(cyclopropylmethyl) 1 E-5070 H H H H H 4-(cyclopropylmethyl) 1 E-5071 H H H H H 2-(cyclobutylmethyl) 1 E-5072 H H H H H 3-(cyclobutylmethyl) 1 E-5073 H H H H H 4-(cyclobutylmethyl) 1 E-5074 H H H H H 2-(cyclopentylmethyl) 1 E-5075 H H H H H 3-(cyclopentylmethyl) 1 E-5076 H H H H H 4-(cyclopentylmethyl) 1 E-5077 H H H H H 2-(cyclopropylethyl) 1 E-5078 H H H H H 3-(cyclopropylethyl) 1 E-5079 H H H H H 4-(cyclopropylethyl) 1 E-5080 H H H H H 2-(2,2-difluorocyclopropyl) 1 E-5081 H H H H H 3-(2,2-difluorocyclopropyl) 1 E-5082 H H H H H 4-(2,2-difluorocyclopropyl) 1 E-5083 H H H H H 2-(2,2-dichlorocyclopropyl) 1 E-5084 H H H H H 3-(2,2-dichlorocyclopropyl) 1 E-5085 H H H H H 4-(2,2-dichlorocyclopropyl) 1 E-5086 H H H H H 2-ethenyl 1 E-5087 H H H H H 3-ethenyl 1 E-5088 H H H H H 4-ethenyl 1 E-5089 H H H H H 2-allyl 1 E-5090 H H H H H 3-allyl 1 E-5091 H H H H H 4-allyl 1 E-5092 H H H H H 2-(prop-1-en-1-yl) 1 E-5093 H H H H H 3-(prop-1-en-1-yl) 1 E-5094 H H H H H 4-(prop-1-en-1-yl) 1 E-5095 H H H H H 2-(trifluoroethenyl) 1 E-5096 H H H H H 3-(trifluoroethenyl) 1 E-5097 H H H H H 4-(trifluoroethenyl) 1 E-5098 H H H H H 2-(2,2-dichloroethenyl) 1 E-5099 H H H H H 3-(2,2-dichloroethenyl) 1 E-5100 H H H H H 4-(2,2-dichloroethenyl) 1 E-5101 H H H H H 2-ethynyl 1 E-5102 H H H H H 3-ethynyl 1 E-5103 H H H H H 4-ethynyl 1 E-5104 H H H H H 2-(1-propyn-1-yl) 1 E-5105 H H H H H 3-(1-propyn-1-yl) 1 E-5106 H H H H H 4-(1-propyn-1-yl) 1 E-5107 H H H H H 2-(2-propyn-1-yl) 1 E-5108 H H H H H 3-(2-propyn-1-yl) 1 E-5109 H H H H H 4-(2-propyn-1-yl) 1
(379) TABLE-US-00278 TABLE 278 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5110 H H H H H 2-(2-cyclopropylethynyl) 1 E-5111 H H H H H 3-(2-cyclopropylethynyl) 1 E-5112 H H H H H 4-(2-cyclopropylethynyl) 1 E-5113 H H H H H 2-(2-chloroethynyl) 1 E-5114 H H H H H 3-(2-chloroethynyl) 1 E-5115 H H H H H 4-(2-chloroethynyl) 1 E-5116 H H H H H 2-(2-bromoethynyl) 1 E-5117 H H H H H 3-(2-bromoethynyl) 1 E-5118 H H H H H 4-(2-bromoethynyl) 1 E-5119 H H H H H 2-OMe 1 E-5120 H H H H H 3-OMe 1 E-5121 H H H H H 4-OMe 1 E-5122 H H H H H 2-OEt 1 E-5123 H H H H H 3-OEt 1 E-5124 H H H H H 4-OEt 1 E-5125 H H H H H 2-OPr 1 E-5126 H H H H H 3-OPr 1 E-5127 H H H H H 4-OPr 1 E-5128 H H H H H 2-O(i-Pr) 1 E-5129 H H H H H 3-O(i-Pr) 1 E-5130 H H H H H 4-O(i-Pr) 1 E-5131 H H H H H 2-OBu 1 E-5132 H H H H H 3-OBu 1 E-5133 H H H H H 4-OBu 1 E-5134 H H H H H 2-O(s-Bu) 1 E-5135 H H H H H 3-O(s-Bu) 1 E-5136 H H H H H 4-O(s-Bu) 1 E-5137 H H H H H 2-O(i-Bu) 1 E-5138 H H H H H 3-O(i-Bu) 1 E-5139 H H H H H 4-O(i-Bu) 1 E-5140 H H H H H 2-O(t-Bu) 1 E-5141 H H H H H 3-O(t-Bu) 1 E-5142 H H H H H 4-O(t-Bu) 1 E-5143 H H H H H 2-OCF.sub.3 1 E-5144 H H H H H 3-OCF.sub.3 1 E-5145 H H H H H 4-OCF.sub.3 1 E-5146 H H H H H 2-OCHF.sub.2 1 E-5147 H H H H H 3-OCHF.sub.2 1 E-5148 H H H H H 4-OCHF.sub.2 1 E-5149 H H H H H 2-OCH.sub.2CF.sub.3 1 E-5150 H H H H H 3-OCH.sub.2CF.sub.3 1 E-5151 H H H H H 4-OCH.sub.2CF.sub.3 1 E-5152 H H H H H 2-(cyclopropyloxy) 1 E-5153 H H H H H 3-(cyclopropyloxy) 1 E-5154 H H H H H 4-(cyclopropyloxy) 1 E-5155 H H H H H 2-(cyclobutyloxy) 1 E-5156 H H H H H 3-(cyclobutyloxy) 1 E-5157 H H H H H 4-(cyclobutyloxy) 1 E-5158 H H H H H 2-(cyclopentyloxy) 1 E-5159 H H H H H 3-(cyclopentyloxy) 1 E-5160 H H H H H 4-(cyclopentyloxy) 1 E-5161 H H H H H 2-((2,2-dichlorocyclopropyl)oxy) 1 E-5162 H H H H H 3-((2,2-dichlorocyclopropyl)oxy) 1 E-5163 H H H H H 4-((2,2-dichlorocyclopropyl)oxy) 1 E-5164 H H H H H 2-(cyclopropylmethoxy) 1 E-5165 H H H H H 3-(cyclopropylmethoxy) 1 E-5166 H H H H H 4-(cyclopropylmethoxy) 1
(380) TABLE-US-00279 TABLE 279 com- pound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5167 H H H H H 2-((2,2-difluorocyclopropyl)methoxy) 1 E-5168 H H H H H 3-((2,2-difluorocyclopropyl)methoxy) 1 E-5169 H H H H H 4-((2,2-difluorocyclopropyl)methoxy) 1 E-5170 H H H H H 2-(oxiran-2-yl) 1 E-5171 H H H H H 3-(oxiran-2-yl) 1 E-5172 H H H H H 4-(oxiran-2-yl) 1 E-5173 H H H H H 2-(oxiran-2-ylmethyl) 1 E-5174 H H H H H 3-(oxiran-2-ylmethyl) 1 E-5175 H H H H H 4-(oxiran-2-ylmethyl) 1 E-5176 H H H H H 2-SMe 1 E-5177 H H H H H 3-SMe 1 E-5178 H H H H H 4-SMe 1 E-5179 H H H H H 2-SEt 1 E-5180 H H H H H 3-SEt 1 E-5181 H H H H H 4-SEt 1 E-5182 H H H H H 2-S(?O)Me 1 E-5183 H H H H H 3-S(?O)Me 1 E-5184 H H H H H 4-S(?O)Me 1 E-5185 H H H H H 2-S(?O).sub.2Me 1 E-5186 H H H H H 3-S(?O).sub.2Me 1 E-5187 H H H H H 4-S(?O).sub.2Me 1 E-5188 H H H H H 2-SCF.sub.3 1 E-5189 H H H H H 3-SCF.sub.3 1 E-5190 H H H H H 4-SCF.sub.3 1 E-5191 H H H H H 2-S(?O)CF.sub.3 1 E-5192 H H H H H 3-S(?O)CF.sub.3 1 E-5193 H H H H H 4-S(?O)CF.sub.3 1 E-5194 H H H H H 2-S(?O).sub.2CF.sub.3 1 E-5195 H H H H H 3-S(?O).sub.2CF.sub.3 1 E-5196 H H H H H 4-S(?O).sub.2CF.sub.3 1 E-5197 H H H H H 2-SCF(CF.sub.3).sub.2 1 E-5198 H H H H H 3-SCF(CF.sub.3).sub.2 1 E-5199 H H H H H 4-SCF(CF.sub.3).sub.2 1 E-5200 H H H H H 2-(cyclopropylthio) 1 E-5201 H H H H H 3-(cyclopropylthio) 1 E-5202 H H H H H 4-(cyclopropylthio) 1 E-5203 H H H H H 2-(cyclopropylsulfinyl) 1 E-5204 H H H H H 3-(cyclopropylsulfinyl) 1 E-5205 H H H H H 4-(cyclopropylsulfinyl) 1 E-5206 H H H H H 2-(cyclopropylsulfonyl) 1 E-5207 H H H H H 3-(cyclopropylsulfonyl) 1 E-5208 H H H H H 4-(cyclopropylsulfonyl) 1 E-5209 H H H H H 2-((cyclopropylmethyl)thio) 1 E-5210 H H H H H 3-((cyclopropylmethyl)thio) 1 E-5211 H H H H H 4-((cyclopropylmethyl)thio) 1 E-5212 H H H H H 2-((cyclopropylmethyl)sulfinyl) 1 E-5213 H H H H H 3-((cyclopropylmethyl)sulfinyl) 1 E-5214 H H H H H 4-((cyclopropylmethyl)sulfinyl) 1 E-5215 H H H H H 2-((cyclopropylmethyl)sulfonyl) 1 E-5216 H H H H H 3-((cyclopropylmethyl)sulfonyl) 1 E-5217 H H H H H 4-((cyclopropylmethyl)sulfonyl) 1 E-5218 H H H H H 2-(((2,2- 1 difluorocyclopropyl)methyl)thio) E-5219 H H H H H 3-(((2,2- 1 difluorocyclopropyl)methyl)thio) E-5220 H H H H H 4-(((2,2- 1 difluorocyclopropyl)methyl)thio) E-5221 H H H H H 2-(((2,2- 1 difluorocyclopropyl)methyl)sulfinyl) E-5222 H H H H H 3-(((2,2- 1 difluorocyclopropyl)methyl)sulfinyl) E-5223 H H H H H 4-(((2,2- 1 difluorocyclopropyl)methyl)sulfinyl)
(381) TABLE-US-00280 TABLE 280 com- pound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5224 H H H H H 2-(((2,2- 1 difluorocyclopropyl)methyl)sulfonyl) E-5225 H H H H H 3-(((2,2- 1 difluorocyclopropyl)methyl)sulfonyl) E-5226 H H H H H 4-(((2,2- 1 difluorocyclopropyl)methyl)sulfonyl) E-5227 H H H H H 2-C(?O)Me 1 E-5228 H H H H H 3-C(?O)Me 1 E-5229 H H H H H 4-C(?O)Me 1 E-5230 H H H H H 2-C(?O)Et 1 E-5231 H H H H H 3-C(?O)Et 1 E-5232 H H H H H 4-C(?O)Et 1 E-5233 H H H H H 2-C(?O)CF.sub.3 1 E-5234 H H H H H 3-C(?O)CF.sub.3 1 E-5235 H H H H H 4-C(?O)CF.sub.3 1 E-5236 H H H H H 2-C(?O)OMe 1 E-5237 H H H H H 3-C(?O)OMe 1 E-5238 H H H H H 4-C(?O)OMe 1 E-5239 H H H H H 2-C(?O)OEt 1 E-5240 H H H H H 3-C(?O)OEt 1 E-5241 H H H H H 4-C(?O)OEt 1 E-5242 H H H H H 2-C(?O)NH.sub.2 1 E-5243 H H H H H 3-C(?O)NH.sub.2 1 E-5244 H H H H H 4-C(?O)NH.sub.2 1 E-5245 H H H H H 2-C(?O)NHMe 1 E-5246 H H H H H 3-C(?O)NHMe 1 E-5247 H H H H H 4-C(?O)NHMe 1 E-5248 H H H H H 2-C(?O)NMe.sub.2 1 E-5249 H H H H H 3-C(?O)NMe.sub.2 1 E-5250 H H H H H 4-C(?O)NMe.sub.2 1 E-5251 H H H H H 2-CH.sub.2C(?O)CH.sub.3 1 E-5252 H H H H H 3-CH.sub.2C(?O)CH.sub.3 1 E-5253 H H H H H 4-CH.sub.2C(?O)CH.sub.3 1 E-5254 H H H H H 2-CH.sub.2C(?O)CF.sub.3 1 E-5255 H H H H H 3-CH.sub.2C(?O)CF.sub.3 1 E-5256 H H H H H 4-CH.sub.2C(?O)CF.sub.3 1 E-5257 H H H H H 2-CH.sub.2C(?O)OCH.sub.3 1 E-5258 H H H H H 3-CH.sub.2C(?O)OCH.sub.3 1 E-5259 H H H H H 4-CH.sub.2C(?O)OCH.sub.3 1 E-5260 H H H H H 2-CH.sub.2OH 1 E-5261 H H H H H 3-CH.sub.2OH 1 E-5262 H H H H H 4-CH.sub.2OH 1 E-5263 H H H H H 2-CH.sub.2OCH.sub.3 1 E-5264 H H H H H 3-CH.sub.2OCH.sub.3 1 E-5265 H H H H H 4-CH.sub.2OCH.sub.3 1 E-5266 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3 1 E-5267 H H H H H 3-CH.sub.2OCH.sub.2CH.sub.3 1 E-5268 H H H H H 4-CH.sub.2OCH.sub.2CH.sub.3 1 E-5269 H H H H H 2-CH(CH.sub.3)OCH.sub.3 1 E-5270 H H H H H 3-CH(CH.sub.3)OCH.sub.3 1 E-5271 H H H H H 4-CH(CH.sub.3)OCH.sub.3 1 E-5272 H H H H H 2-CH.sub.2CH.sub.2OCH.sub.3 1 E-5273 H H H H H 3-CH.sub.2CH.sub.2OCH.sub.3 1 E-5274 H H H H H 4-CH.sub.2CH.sub.2OCH.sub.3 1 E-5275 H H H H H 2-CH.sub.2OCF.sub.3 1 E-5276 H H H H H 3-CH.sub.2OCF.sub.3 1 E-5277 H H H H H 4-CH.sub.2OCF.sub.3 1 E-5278 H H H H H 2-CF.sub.2OCH.sub.3 1 E-5279 H H H H H 3-CF.sub.2OCH.sub.3 1 E-5280 H H H H H 4-CF.sub.2OCH.sub.3 1
(382) TABLE-US-00281 TABLE 281 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5281 H H H H H 2-CF.sub.2CF.sub.2OCF.sub.3 1 E-5282 H H H H H 3-CF.sub.2CF.sub.2OCF.sub.3 1 E-5283 H H H H H 4-CF.sub.2CF.sub.2OCF.sub.3 1 E-5284 H H H H H 2-OC(?O)CH.sub.3 1 E-5285 H H H H H 3-OC(?O)CH.sub.3 1 E-5286 H H H H H 4-OC(?O)CH.sub.3 1 E-5287 H H H H H 2-OC(?O)CF.sub.3 1 E-5288 H H H H H 3-OC(?O)CF.sub.3 1 E-5289 H H H H H 4-OC(?O)CF.sub.3 1 E-5290 H H H H H 2-OC(?O)NH.sub.2 1 E-5291 H H H H H 3-OC(?O)NH.sub.2 1 E-5292 H H H H H 4-OC(?O)NH.sub.2 1 E-5293 H H H H H 2-OC(?O)NHCH.sub.3 1 E-5294 H H H H H 3-OC(?O)NHCH.sub.3 1 E-5295 H H H H H 4-OC(?O)NHCH.sub.3 1 E-5296 H H H H H 2-OC(?O)N(CH.sub.3).sub.2 1 E-5297 H H H H H 3-OC(?O)N(CH.sub.3).sub.2 1 E-5298 H H H H H 4-OC(?O)N(CH.sub.3).sub.2 1 E-5299 H H H H H 2-CH.sub.2OC(?O)NH.sub.2 1 E-5300 H H H H H 3-CH.sub.2OC(?O)NH.sub.2 1 E-5301 H H H H H 4-CH.sub.2OC(?O)NH.sub.2 1 E-5302 H H H H H 2-CH.sub.2OC(?O)NHCH.sub.3 1 E-5303 H H H H H 3-CH.sub.2OC(?O)NHCH.sub.3 1 E-5304 H H H H H 4-CH.sub.2OC(?O)NHCH.sub.3 1 E-5305 H H H H H 2-CH.sub.2OC(?O)N(CH.sub.3).sub.2 1 E-5306 H H H H H 3-CH.sub.2OC(?O)N(CH.sub.3).sub.2 1 E-5307 H H H H H 4-CH.sub.2OC(?O)N(CH.sub.3).sub.2 1 E-5308 H H H H H 2-OC(?O)OCH.sub.3 1 E-5309 H H H H H 3-OC(?O)OCH.sub.3 1 E-5310 H H H H H 4-OC(?O)OCH.sub.3 1 E-5311 H H H H H 2-CH.sub.2OC(?O)OCH.sub.3 1 E-5312 H H H H H 3-CH.sub.2OC(?O)OCH.sub.3 1 E-5313 H H H H H 4-CH.sub.2OC(?O)OCH.sub.3 1 E-5314 H H H H H 2-CH.sub.2OC(?O)CH.sub.3 1 E-5315 H H H H H 3-CH.sub.2OC(?O)CH.sub.3 1 E-5316 H H H H H 4-CH.sub.2OC(?O)CH.sub.3 1 E-5317 H H H H H 2-OS(?O).sub.2CH.sub.3 1 E-5318 H H H H H 3-OS(?O).sub.2CH.sub.3 1 E-5319 H H H H H 4-OS(?O).sub.2CH.sub.3 1 E-5320 H H H H H 2-CH.sub.2SCH.sub.3 1 E-5321 H H H H H 3-CH.sub.2SCH.sub.3 1 E-5322 H H H H H 4-CH.sub.2SCH.sub.3 1 E-5323 H H H H H 2-CH.sub.2S(?O)CH.sub.3 1 E-5324 H H H H H 3-CH.sub.2S(?O)CH.sub.3 1 E-5325 H H H H H 4-CH.sub.2S(?O)CH.sub.3 1 E-5326 H H H H H 2-CH.sub.2S(?O).sub.2CH.sub.3 1 E-5327 H H H H H 3-CH.sub.2S(?O).sub.2CH.sub.3 1 E-5328 H H H H H 4-CH.sub.2S(?O).sub.2CH.sub.3 1 E-5329 H H H H H 2-CH.sub.2SCF.sub.3 1 E-5330 H H H H H 3-CH.sub.2SCF.sub.3 1 E-5331 H H H H H 4-CH.sub.2SCF.sub.3 1 E-5332 H H H H H 2-CH.sub.2S(?O)CF.sub.3 1 E-5333 H H H H H 3-CH.sub.2S(?O)CF.sub.3 1 E-5334 H H H H H 4-CH.sub.2S(?O)CF.sub.3 1 E-5335 H H H H H 2-CH.sub.2S(?O).sub.2CF.sub.3 1 E-5336 H H H H H 3-CH.sub.2S(?O).sub.2CF.sub.3 1 E-5337 H H H H H 4-CH.sub.2S(?O).sub.2CF.sub.3 1
(383) TABLE-US-00282 TABLE 282 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5338 H H H H H 2-phenyl 1 E-5339 H H H H H 3-phenyl 1 E-5340 H H H H H 4-phenyl 1 E-5341 H H H H H 2-(phenyloxy) 1 E-5342 H H H H H 3-(phenyloxy) 1 E-5343 H H H H H 4-(phenyloxy) 1 E-5344 H H H H H 2-benzyl 1 E-5345 H H H H H 3-benzyl 1 E-5346 H H H H H 4-benzyl 1 E-5347 H H H H H 2-(benzyloxy) 1 E-5348 H H H H H 3-(benzyloxy) 1 E-5349 H H H H H 4-(benzyloxy) 1 E-5350 H H H H H 2-((2-fluorobenzyl)oxy) 1 E-5351 H H H H H 3-((2-fluorobenzyl)oxy) 1 E-5352 H H H H H 4-((2-fluorobenzyl)oxy) 1 E-5353 H H H H H 2-((3-fluorobenzyl)oxy) 1 E-5354 H H H H H 3-((3-fluorobenzyl)oxy) 1 E-5355 H H H H H 4-((3-fluorobenzyl)oxy) 1 E-5356 H H H H H 2-((4-fluorobenzyl)oxy) 1 E-5357 H H H H H 3-((4-fluorobenzyl)oxy) 1 E-5358 H H H H H 4-((4-fluorobenzyl)oxy) 1 E-5359 H H H H H 2-((2-chlorobenzyl)oxy) 1 E-5360 H H H H H 3-((2-chlorobenzyl)oxy) 1 E-5361 H H H H H 4-((2-chlorobenzyl)oxy) 1 E-5362 H H H H H 2-((3-chlorobenzyl)oxy) 1 E-5363 H H H H H 3-((3-chlorobenzyl)oxy) 1 E-5364 H H H H H 4-((3-chlorobenzyl)oxy) 1 E-5365 H H H H H 2-((4-chlorobenzyl)oxy) 1 E-5366 H H H H H 3-((4-chlorobenzyl)oxy) 1 E-5367 H H H H H 4-((4-chlorobenzyl)oxy) 1 E-5368 H H H H H 2-((2-methylbenzyl)oxy) 1 E-5369 H H H H H 3-((2-methylbenzyl)oxy) 1 E-5370 H H H H H 4-((2-methylbenzyl)oxy) 1 E-5371 H H H H H 2-((3-methylbenzyl)oxy) 1 E-5372 H H H H H 3-((3-methylbenzyl)oxy) 1 E-5373 H H H H H 4-((3-methylbenzyl)oxy) 1 E-5374 H H H H H 2-((4-methylbenzyl)oxy) 1 E-5375 H H H H H 3-((4-methylbenzyl)oxy) 1 E-5376 H H H H H 4-((4-methylbenzyl)oxy) 1 E-5377 H H H H H 2-((2-(trifluoromethyl)benzyl)oxy) 1 E-5378 H H H H H 3-((2-(trifluoromethyl)benzyl)oxy) 1 E-5379 H H H H H 4-((2-(trifluoromethyl)benzyl)oxy) 1 E-5380 H H H H H 2-((3-(trifluoromethyl)benzyl)oxy) 1 E-5381 H H H H H 3-((3-(trifluoromethyl)benzyl)oxy) 1 E-5382 H H H H H 4-((3-(trifluoromethyl)benzyl)oxy) 1 E-5383 H H H H H 2-((4-(trifluoromethyl)benzyl)oxy) 1 E-5384 H H H H H 3-((4-(trifluoromethyl)benzyl)oxy) 1 E-5385 H H H H H 4-((4-(trifluoromethyl)benzyl)oxy) 1 E-5386 H H H H H 2-((2-methoxybenzyl)oxy) 1 E-5387 H H H H H 3-((2-methoxybenzyl)oxy) 1 E-5388 H H H H H 4-((2-methoxybenzyl)oxy) 1 E-5389 H H H H H 2-((3-methoxybenzyl)oxy) 1 E-5390 H H H H H 3-((3-methoxybenzyl)oxy) 1 E-5391 H H H H H 4-((3-methoxybenzyl)oxy) 1 E-5392 H H H H H 2-((4-methoxybenzyl)oxy) 1 E-5393 H H H H H 3-((4-methoxybenzyl)oxy) 1 E-5394 H H H H H 4-((4-methoxybenzyl)oxy) 1
(384) TABLE-US-00283 TABLE 283 com- pound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5395 H H H H H 2-((2-(trifluoromethoxy)benzyl)oxy) 1 E-5396 H H H H H 3-((2-(trifluoromethoxy)benzyl)oxy) 1 E-5397 H H H H H 4-((2-(trifluoromethoxy)benzyl)oxy) 1 E-5398 H H H H H 2-((3-(trifluoromethoxy)benzyl)oxy) 1 E-5399 H H H H H 3-((3-(trifluoromethoxy)benzyl)oxy) 1 E-5400 H H H H H 4-((3-(trifluoromethoxy)benzyl)oxy) 1 E-5401 H H H H H 2-((4-(trifluoromethoxy)benzyl)oxy) 1 E-5402 H H H H H 3-((4-(trifluoromethoxy)benzyl)oxy) 1 E-5403 H H H H H 4-((4-(trifluoromethoxy)benzyl)oxy) 1 E-5404 H H H H H 2-((2-(methylthio)benzyl)oxy) 1 E-5405 H H H H H 3-((2-(methylthio)benzyl)oxy) 1 E-5406 H H H H H 4-((2-(methylthio)benzyl)oxy) 1 E-5407 H H H H H 2-((3-(methylthio)benzyl)oxy) 1 E-5408 H H H H H 3-((3-(methylthio)benzyl)oxy) 1 E-5409 H H H H H 4-((3-(methylthio)benzyl)oxy) 1 E-5410 H H H H H 2-((4-(methylthio)benzyl)oxy) 1 E-5411 H H H H H 3-((4-(methylthio)benzyl)oxy) 1 E-5412 H H H H H 4-((4-(methylthio)benzyl)oxy) 1 E-5413 H H H H H 2-((2-(methylsulfinyl)benzyl)oxy) 1 E-5414 H H H H H 3-((2-(methylsulfinyl)benzyl)oxy) 1 E-5415 H H H H H 4-((2-(methylsulfinyl)benzyl)oxy) 1 E-5416 H H H H H 2-((3-(methylsulfinyl)benzyl)oxy) 1 E-5417 H H H H H 3-((3-(methylsulfinyl)benzyl)oxy) 1 E-5418 H H H H H 4-((3-(methylsulfinyl)benzyl)oxy) 1 E-5419 H H H H H 2-((4-(methylsulfinyl)benzyl)oxy) 1 E-5420 H H H H H 3-((4-(methylsulfinyl)benzyl)oxy) 1 E-5421 H H H H H 4-((4-(methylsulfinyl)benzyl)oxy) 1 E-5422 H H H H H 2-((2-(methylsulfonyl)benzyl)oxy) 1 E-5423 H H H H H 3-((2-(methylsulfonyl)benzyl)oxy) 1 E-5424 H H H H H 4-((2-(methylsulfonyl)benzyl)oxy) 1 E-5425 H H H H H 2-((3-(methylsulfonyl)benzyl)oxy) 1 E-5426 H H H H H 3-((3-(methylsulfonyl)benzyl)oxy) 1 E-5427 H H H H H 4-((3-(methylsulfonyl)benzyl)oxy) 1 E-5428 H H H H H 2-((4-(methylsulfonyl)benzyl)oxy) 1 E-5429 H H H H H 3-((4-(methylsulfonyl)benzyl)oxy) 1 E-5430 H H H H H 4-((4-(methylsulfonyl)benzyl)oxy) 1 E-5431 H H H H H 2-((2-(trifluoromethylthio)benzyl)oxy) 1 E-5432 H H H H H 3-((2-(trifluoromethylthio)benzyl)oxy) 1 E-5433 H H H H H 4-((2-(trifluoromethylthio)benzyl)oxy) 1 E-5434 H H H H H 2-((3-(trifluoromethylthio)benzyl)oxy) 1 E-5435 H H H H H 3-((3-(trifluoromethylthio)benzyl)oxy) 1 E-5436 H H H H H 4-((3-(trifluoromethylthio)benzyl)oxy) 1 E-5437 H H H H H 2-((4-(trifluoromethylthio)benzyl)oxy) 1 E-5438 H H H H H 3-((4-(trifluoromethylthio)benzyl)oxy) 1 E-5439 H H H H H 4-((4-(trifluoromethylthio)benzyl)oxy) 1 E-5440 H H H H H 2-((2- 1 (trifluoromethylsulfinyl)benzyl)oxy) E-5441 H H H H H 3-((2- 1 (trifluoromethylsulfinyl)benzyl)oxy) E-5442 H H H H H 4-((2- 1 (trifluoromethylsulfinyl)benzyl)oxy) E-5443 H H H H H 2-((3- 1 (trifluoromethylsulfinyl)benzyl)oxy) E-5444 H H H H H 3-((3- 1 (trifluoromethylsulfinyl)benzyl)oxy) E-5445 H H H H H 4-((3- 1 (trifluoromethylsulfinyl)benzyl)oxy) E-5446 H H H H H 2-((4- 1 (trifluoromethylsulfinyl)benzyl)oxy) E-5447 H H H H H 3-((4- 1 (trifluoromethylsulfinyl)benzyl)oxy) E-5448 H H H H H 4-((4- 1 (trifluoromethylsulfinyl)benzyl)oxy) E-5449 H H H H H 2-((2- 1 (trifluoromethylsulfonyl)benzyl)oxy) E-5450 H H H H H 3-((2- 1 (trifluoromethylsulfonyl)benzyl)oxy) E-5451 H H H H H 4-((2- 1 (trifluoromethylsulfonyl)benzyl)oxy)
(385) TABLE-US-00284 TABLE 284 com- pound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5452 H H H H H 2-((3- 1 (trifluoromethylsulfonyl)benzyl)oxy) E-5453 H H H H H 3-((3- 1 (trifluoromethylsulfonyl)benzyl)oxy) E-5454 H H H H H 4-((3- 1 (trifluoromethylsulfonyl)benzyl)oxy) E-5455 H H H H H 2-((4- 1 (trifluoromethylsulfonyl)benzyl)oxy) E-5456 H H H H H 3-((4- 1 (trifluoromethylsulfonyl)benzyl)oxy) E-5457 H H H H H 4-((4- 1 (trifluoromethylsulfonyl)benzyl)oxy) E-5458 H H H H H 2-((2-aminobenzyl)oxy) 1 E-5459 H H H H H 3-((2-aminobenzyl)oxy) 1 E-5460 H H H H H 4-((2-aminobenzyl)oxy) 1 E-5461 H H H H H 2-((3-aminobenzyl)oxy) 1 E-5462 H H H H H 3-((3-aminobenzyl)oxy) 1 E-5463 H H H H H 4-((3-aminobenzyl)oxy) 1 E-5464 H H H H H 2-((4-aminobenzyl)oxy) 1 E-5465 H H H H H 3-((4-aminobenzyl)oxy) 1 E-5466 H H H H H 4-((4-aminobenzyl)oxy) 1 E-5467 H H H H H 2-((2-(methylamino)benzyl)oxy) 1 E-5468 H H H H H 3-((2-(methylamino)benzyl)oxy) 1 E-5469 H H H H H 4-((2-(methylamino)benzyl)oxy) 1 E-5470 H H H H H 2-((3-(methylamino)benzyl)oxy) 1 E-5471 H H H H H 3-((3-(methylamino)benzyl)oxy) 1 E-5472 H H H H H 4-((3-(methylamino)benzyl)oxy) 1 E-5473 H H H H H 2-((4-(methylamino)benzyl)oxy) 1 E-5474 H H H H H 3-((4-(methylamino)benzyl)oxy) 1 E-5475 H H H H H 4-((4-(methylamino)benzyl)oxy) 1 E-5476 H H H H H 2-((2-(dimethylamino)benzyl)oxy) 1 E-5477 H H H H H 3-((2-(dimethylamino)benzyl)oxy) 1 E-5478 H H H H H 4-((2-(dimethylamino)benzyl)oxy) 1 E-5479 H H H H H 2-((3-(dimethylamino)benzyl)oxy) 1 E-5480 H H H H H 3-((3-(dimethylamino)benzyl)oxy) 1 E-5481 H H H H H 4-((3-(dimethylamino)benzyl)oxy) 1 E-5482 H H H H H 2-((4-(dimethylamino)benzyl)oxy) 1 E-5483 H H H H H 3-((4-(dimethylamino)benzyl)oxy) 1 E-5484 H H H H H 4-((4-(dimethylamino)benzyl)oxy) 1 E-5485 H H H H H 2-((2-cyanobenzyl)oxy) 1 E-5486 H H H H H 3-((2-cyanobenzyl)oxy) 1 E-5487 H H H H H 4-((2-cyanobenzyl)oxy) 1 E-5488 H H H H H 2-((3-cyanobenzyl)oxy) 1 E-5489 H H H H H 3-((3-cyanobenzyl)oxy) 1 E-5490 H H H H H 4-((3-cyanobenzyl)oxy) 1 E-5491 H H H H H 2-((4-cyanobenzyl)oxy) 1 E-5492 H H H H H 3-((4-cyanobenzyl)oxy) 1 E-5493 H H H H H 4-((4-cyanobenzyl)oxy) 1 E-5494 H H H H H 2-((2-nitrobenzyl)oxy) 1 E-5495 H H H H H 3-((2-nitrobenzyl)oxy) 1 E-5496 H H H H H 4-((2-nitrobenzyl)oxy) 1 E-5497 H H H H H 2-((3-nitrobenzyl)oxy) 1 E-5498 H H H H H 3-((3-nitrobenzyl)oxy) 1 E-5499 H H H H H 4-((3-nitrobenzyl)oxy) 1 E-5500 H H H H H 2-((4-nitrobenzyl)oxy) 1 E-5501 H H H H H 3-((4-nitrobenzyl)oxy) 1 E-5502 H H H H H 4-((4-nitrobenzyl)oxy) 1 E-5503 H H H H H 2-NH.sub.2 1 E-5504 H H H H H 3-NH.sub.2 1 E-5505 H H H H H 4-NH.sub.2 1 E-5506 H H H H H 2-NHMe 1 E-5507 H H H H H 3-NHMe 1 E-5508 H H H H H 4-NHMe 1
(386) TABLE-US-00285 TABLE 285 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5509 H H H H H 2-NHEt 1 E-5510 H H H H H 3-NHEt 1 E-5511 H H H H H 4-NHEt 1 E-5512 H H H H H 2-N(Me).sub.2 1 E-5513 H H H H H 3-N(Me).sub.2 1 E-5514 H H H H H 4-N(Me).sub.2 1 E-5515 H H H H H 2-N(Et).sub.2 1 E-5516 H H H H H 3-N(Et).sub.2 1 E-5517 H H H H H 4-N(Et).sub.2 1 E-5518 H H H H H 2-CHO 1 E-5519 H H H H H 3-CHO 1 E-5520 H H H H H 4-CHO 1 E-5521 H H H H H 2-C(?O)OH 1 E-5522 H H H H H 3-C(?O)OH 1 E-5523 H H H H H 4-C(?O)OH 1 E-5524 H H H H H 2-(1,3-dioxolan-2-yl) 1 E-5525 H H H H H 3-(1,3-dioxolan-2-yl) 1 E-5526 H H H H H 4-(1,3-dioxolan-2-yl) 1 E-5527 H H H H H 2-(1,3-dioxan-2-yl) 1 E-5528 H H H H H 3-(1,3-dioxan-2-yl) 1 E-5529 H H H H H 4-(1,3-dioxan-2-yl) 1 E-5530 H H H H H 2-(1H-imidazol-2-yl) 1 E-5531 H H H H H 3-(1H-imidazol-2-yl) 1 E-5532 H H H H H 4-(1H-imidazol-2-yl) 1 E-5533 H H H H H 2-(thiazol-2-yl) 1 E-5534 H H H H H 3-(thiazol-2-yl) 1 E-5535 H H H H H 4-(thiazol-2-yl) 1 E-5536 H H H H H 2-(oxazol-2-yl) 1 E-5537 H H H H H 3-(oxazol-2-yl) 1 E-5538 H H H H H 4-(oxazol-2-yl) 1 E-5539 H H H H H 2-CH?NOH 1 E-5540 H H H H H 3-CH?NOH 1 E-5541 H H H H H 4-CH?NOH 1 E-5542 H H H H H 2-CH?NOMe 1 E-5543 H H H H H 3-CH?NOMe 1 E-5544 H H H H H 4-CH?NOMe 1 E-5545 H H H H H 2-(4,5-dihydro-3-isoxazolyl) 1 E-5546 H H H H H 3-(4,5-dihydro-3-isoxazolyl) 1 E-5547 H H H H H 4-(4,5-dihydro-3-isoxazolyl) 1 E-5548 H H H H H 2-CN 1 E-5549 H H H H H 3-CN 1 E-5550 H H H H H 4-CN 1 E-5551 H H H H H 2-NO.sub.2 1 E-5552 H H H H H 3-NO.sub.2 1 E-5553 H H H H H 4-NO.sub.2 1 E-5554 H H H H H 2,3-F.sub.2 1 E-5555 H H H H H 2,4-F.sub.2 1 E-5556 H H H H H 2,5-F.sub.2 1 E-5557 H H H H H 2,6-F.sub.2 1 E-5558 H H H H H 3,4-F.sub.2 1 E-5559 H H H H H 3,5-F.sub.2 1 E-5560 H H H H H 2-F,3-Cl 1 E-5561 H H H H H 2-F,4-Cl 1 E-5562 H H H H H 2-F,5-Cl 1 E-5563 H H H H H 2-F,6-Cl 1 E-5564 H H H H H 3-F,2-Cl 1 E-5565 H H H H H 3-F,4-Cl 1
(387) TABLE-US-00286 TABLE 286 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5566 H H H H H 3-F,5-Cl 1 E-5567 H H H H H 3-F,6-Cl 1 E-5568 H H H H H 4-F,2-Cl 1 E-5569 H H H H H 4-F,3-Cl 1 E-5570 H H H H H 2-F,3-Me 1 E-5571 H H H H H 2-F,4-Me 1 E-5572 H H H H H 2-F,5-Me 1 E-5573 H H H H H 2-F,6-Me 1 E-5574 H H H H H 3-F,2-Me 1 E-5575 H H H H H 3-F,4-Me 1 E-5576 H H H H H 3-F,5-Me 1 E-5577 H H H H H 3-F,6-Me 1 E-5578 H H H H H 4-F,2-Me 1 E-5579 H H H H H 4-F,3-Me 1 E-5580 H H H H H 2-F,3-CF.sub.3 1 E-5581 H H H H H 2-F,4-CF.sub.3 1 E-5582 H H H H H 2-F,5-CF.sub.3 1 E-5583 H H H H H 2-F,6-CF.sub.3 1 E-5584 H H H H H 3-F,2-CF.sub.3 1 E-5585 H H H H H 3-F,4-CF.sub.3 1 E-5586 H H H H H 3-F,5-CF.sub.3 1 E-5587 H H H H H 3-F,6-CF.sub.3 1 E-5588 H H H H H 4-F,2-CF.sub.3 1 E-5589 H H H H H 4-F,3-CF.sub.3 1 E-5590 H H H H H 2-F,3-OMe 1 E-5591 H H H H H 2-F,4-OMe 1 E-5592 H H H H H 2-F,5-OMe 1 E-5593 H H H H H 2-F,6-OMe 1 E-5594 H H H H H 3-F,2-OMe 1 E-5595 H H H H H 3-F,4-OMe 1 E-5596 H H H H H 3-F,5-OMe 1 E-5597 H H H H H 3-F,6-OMe 1 E-5598 H H H H H 4-F,2-OMe 1 E-5599 H H H H H 4-F,3-OMe 1 E-5600 H H H H H 2,3-Cl.sub.2 1 E-5601 H H H H H 2,4-Cl.sub.2 1 E-5602 H H H H H 2,5-Cl.sub.2 1 E-5603 H H H H H 2,6-Cl.sub.2 1 E-5604 H H H H H 3,4-Cl.sub.2 1 E-5605 H H H H H 3,5-Cl.sub.2 1 E-5606 H H H H H 2-Cl,3-Me 1 E-5607 H H H H H 2-Cl,4-Me 1 E-5608 H H H H H 2-Cl,5-Me 1 E-5609 H H H H H 2-Cl,6-Me 1 E-5610 H H H H H 3-Cl,2-Me 1 E-5611 H H H H H 3-Cl,4-Me 1 E-5612 H H H H H 3-Cl,5-Me 1 E-5613 H H H H H 3-Cl,6-Me 1 E-5614 H H H H H 4-Cl,2-Me 1 E-5615 H H H H H 4-Cl,3-Me 1 E-5616 H H H H H 2-Cl,3-CF.sub.3 1 E-5617 H H H H H 2-Cl,4-CF.sub.3 1 E-5618 H H H H H 2-Cl,5-CF.sub.3 1 E-5619 H H H H H 2-Cl,6-CF.sub.3 1 E-5620 H H H H H 3-Cl,2-CF.sub.3 1 E-5621 H H H H H 3-Cl,4-CF.sub.3 1 E-5622 H H H H H 3-Cl,5-CF.sub.3 1
(388) TABLE-US-00287 TABLE 287 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5623 H H H H H 3-Cl,6-CF.sub.3 1 E-5624 H H H H H 4-Cl,2-CF.sub.3 1 E-5625 H H H H H 4-Cl,3-CF.sub.3 1 E-5626 H H H H H 2-Cl,3-OMe 1 E-5627 H H H H H 2-Cl,4-OMe 1 E-5628 H H H H H 2-Cl,5-OMe 1 E-5629 H H H H H 2-Cl,6-OMe 1 E-5630 H H H H H 3-Cl,2-OMe 1 E-5631 H H H H H 3-Cl,4-OMe 1 E-5632 H H H H H 3-Cl,5-OMe 1 E-5633 H H H H H 3-Cl,6-OMe 1 E-5634 H H H H H 4-Cl,2-OMe 1 E-5635 H H H H H 4-Cl,3-OMe 1 E-5636 H H H H H 2,3-Me.sub.2 1 E-5637 H H H H H 2,4-Me.sub.2 1 E-5638 H H H H H 2,5-Me.sub.2 1 E-5639 H H H H H 2,6-Me.sub.2 1 E-5640 H H H H H 3,4-Me.sub.2 1 E-5641 H H H H H 3,5-Me.sub.2 1 E-5642 H H H H H 2-Me,3-CF.sub.3 1 E-5643 H H H H H 2-Me,4-CF.sub.3 1 E-5644 H H H H H 2-Me,5-CF.sub.3 1 E-5645 H H H H H 2-Me,6-CF.sub.3 1 E-5646 H H H H H 3-Me,2-CF.sub.3 1 E-5647 H H H H H 3-Me,4-CF.sub.3 1 E-5648 H H H H H 3-Me,5-CF.sub.3 1 E-5649 H H H H H 3-Me,6-CF.sub.3 1 E-5650 H H H H H 4-Me,2-CF.sub.3 1 E-5651 H H H H H 4-Me,3-CF.sub.3 1 E-5652 H H H H H 2-Me,3-OMe 1 E-5653 H H H H H 2-Me,4-OMe 1 E-5654 H H H H H 2-Me,5-OMe 1 E-5655 H H H H H 2-Me,6-OMe 1 E-5656 H H H H H 3-Me,2-OMe 1 E-5657 H H H H H 3-Me,4-OMe 1 E-5658 H H H H H 3-Me,5-OMe 1 E-5659 H H H H H 3-Me,6-OMe 1 E-5660 H H H H H 4-Me,2-OMe 1 E-5661 H H H H H 4-Me,3-OMe 1 E-5662 H H H H H 2,3-OMe.sub.2 1 E-5663 H H H H H 2,4-OMe.sub.2 1 E-5664 H H H H H 2,5-OMe.sub.2 1 E-5665 H H H H H 2,6-OMe.sub.2 1 E-5666 H H H H H 3,4-OMe.sub.2 1 E-5667 H H H H H 3,5-OMe.sub.2 1 E-5668 H H H H H 2-OMe,3-CF.sub.3 1 E-5669 H H H H H 2-OMe,4-CF.sub.3 1 E-5670 H H H H H 2-OMe,5-CF.sub.3 1 E-5671 H H H H H 2-OMe,6-CF.sub.3 1 E-5672 H H H H H 3-OMe,2-CF.sub.3 1 E-5673 H H H H H 3-OMe,4-CF.sub.3 1 E-5674 H H H H H 3-OMe,5-CF.sub.3 1 E-5675 H H H H H 3-OMe,6-CF.sub.3 1 E-5676 H H H H H 4-OMe,2-CF.sub.3 1 E-5677 H H H H H 4-OMe,3-CF.sub.3 1 E-5678 H H H H H 2-CHF.sub.2,3-F 1 E-5679 H H H H H 2-CHF.sub.2,4-F 1
(389) TABLE-US-00288 TABLE 288 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5680 H H H H H 2-CHF.sub.2,5-F 1 E-5681 H H H H H 2-CHF.sub.2,6-F 1 E-5682 H H H H H 2-CHF.sub.2,3-Me 1 E-5683 H H H H H 2-CHF.sub.2,4-Me 1 E-5684 H H H H H 2-CHF.sub.2,5-Me 1 E-5685 H H H H H 2-CHF.sub.2,6-Me 1 E-5686 H H H H H 2-cyclopropyl,3-F 1 E-5687 H H H H H 2-cyclopropyl,4-F 1 E-5688 H H H H H 2-cyclopropyl,5-F 1 E-5689 H H H H H 2-cyclopropyl,6-F 1 E-5690 H H H H H 2-cyclopropyl,3-Me 1 E-5691 H H H H H 2-cyclopropyl,4-Me 1 E-5692 H H H H H 2-cyclopropyl,5-Me 1 E-5693 H H H H H 2-cyclopropyl,6-Me 1 E-5694 H H H H H 2-ethenyl,3-F 1 E-5695 H H H H H 2-ethenyl,4-F 1 E-5696 H H H H H 2-ethenyl,5-F 1 E-5697 H H H H H 2-ethenyl,6-F 1 E-5698 H H H H H 2-ethenyl,3-Me 1 E-5699 H H H H H 2-ethenyl,4-Me 1 E-5700 H H H H H 2-ethenyl,5-Me 1 E-5701 H H H H H 2-ethenyl,6-Me 1 E-5702 H H H H H 2-OEt,3-F 1 E-5703 H H H H H 2-OEt,4-F 1 E-5704 H H H H H 2-OEt,5-F 1 E-5705 H H H H H 2-OEt,6-F 1 E-5706 H H H H H 2-OEt,3-Cl 1 E-5707 H H H H H 2-OEt,4-Cl 1 E-5708 H H H H H 2-OEt,5-Cl 1 E-5709 H H H H H 2-OEt,6-Cl 1 E-5710 H H H H H 2-OEt,3-Me 1 E-5711 H H H H H 2-OEt,4-Me 1 E-5712 H H H H H 2-OEt,5-Me 1 E-5713 H H H H H 2-OEt,6-Me 1 E-5714 H H H H H 2-OPr,3-F 1 E-5715 H H H H H 2-OPr,4-F 1 E-5716 H H H H H 2-OPr,5-F 1 E-5717 H H H H H 2-OPr,6-F 1 E-5718 H H H H H 2-OPr,3-Me 1 E-5719 H H H H H 2-OPr,4-Me 1 E-5720 H H H H H 2-OPr,5-Me 1 E-5721 H H H H H 2-OPr,6-Me 1 E-5722 H H H H H 2-O(i-Pr),3-F 1 E-5723 H H H H H 2-O(i-Pr),4-F 1 E-5724 H H H H H 2-O(i-Pr),5-F 1 E-5725 H H H H H 2-O(i-Pr),6-F 1 E-5726 H H H H H 2-O(i-Pr),3-Me 1 E-5727 H H H H H 2-O(i-Pr),4-Me 1 E-5728 H H H H H 2-O(i-Pr),5-Me 1 E-5729 H H H H H 2-O(i-Pr),6-Me 1 E-5730 H H H H H 2-OCF.sub.3,3-F 1 E-5731 H H H H H 2-OCF.sub.3,4-F 1 E-5732 H H H H H 2-OCF.sub.3,5-F 1 E-5733 H H H H H 2-OCF.sub.3,6-F 1 E-5734 H H H H H 2-OCF.sub.3,3-Me 1 E-5735 H H H H H 2-OCF.sub.3,4-Me 1 E-5736 H H H H H 2-OCF.sub.3,5-Me 1
(390) TABLE-US-00289 TABLE 289 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5737 H H H H H 2-OCF.sub.3,6-Me 1 E-5738 H H H H H 2-OCHF.sub.2,3-F 1 E-5739 H H H H H 2-OCHF.sub.2,4-F 1 E-5740 H H H H H 2-OCHF.sub.2,5-F 1 E-5741 H H H H H 2-OCHF.sub.2,6-F 1 E-5742 H H H H H 2-OCHF.sub.2,3-Me 1 E-5743 H H H H H 2-OCHF.sub.2,4-Me 1 E-5744 H H H H H 2-OCHF.sub.2,5-Me 1 E-5745 H H H H H 2-OCHF.sub.2,6-Me 1 E-5746 H H H H H 2-(cyclopropyloxy),3-F 1 E-5747 H H H H H 2-(cyclopropyloxy),4-F 1 E-5748 H H H H H 2-(cyclopropyloxy),5-F 1 E-5749 H H H H H 2-(cyclopropyloxy),6-F 1 E-5750 H H H H H 2-(cyclopropyloxy),3-Me 1 E-5751 H H H H H 2-(cyclopropyloxy),4-Me 1 E-5752 H H H H H 2-(cyclopropyloxy),5-Me 1 E-5753 H H H H H 2-(cyclopropyloxy),6-Me 1 E-5754 H H H H H 2-(oxiran-2-yl),3-F 1 E-5755 H H H H H 2-(oxiran-2-yl),4-F 1 E-5756 H H H H H 2-(oxiran-2-yl),5-F 1 E-5757 H H H H H 2-(oxiran-2-yl),6-F 1 E-5758 H H H H H 2-(oxiran-2-yl),3-Me 1 E-5759 H H H H H 2-(oxiran-2-yl),4-Me 1 E-5760 H H H H H 2-(oxiran-2-yl),5-Me 1 E-5761 H H H H H 2-(oxiran-2-yl),6-Me 1 E-5762 H H H H H 2-(oxiran-2-ylmethyl),3-F 1 E-5763 H H H H H 2-(oxiran-2-ylmethyl),4-F 1 E-5764 H H H H H 2-(oxiran-2-ylmethyl),5-F 1 E-5765 H H H H H 2-(oxiran-2-ylmethyl),6-F 1 E-5766 H H H H H 2-(oxiran-2-ylmethyl),3-Me 1 E-5767 H H H H H 2-(oxiran-2-ylmethyl),4-Me 1 E-5768 H H H H H 2-(oxiran-2-ylmethyl),5-Me 1 E-5769 H H H H H 2-(oxiran-2-ylmethyl),6-Me 1 E-5770 H H H H H 2-SMe,3-F 1 E-5771 H H H H H 2-SMe,4-F 1 E-5772 H H H H H 2-SMe,5-F 1 E-5773 H H H H H 2-SMe,6-F 1 E-5774 H H H H H 2-SMe,3-Me 1 E-5775 H H H H H 2-SMe,4-Me 1 E-5776 H H H H H 2-SMe,5-Me 1 E-5777 H H H H H 2-SMe,6-Me 1 E-5778 H H H H H 2-SEt,3-F 1 E-5779 H H H H H 2-SEt,4-F 1 E-5780 H H H H H 2-SEt,5-F 1 E-5781 H H H H H 2-SEt,6-F 1 E-5782 H H H H H 2-SEt,3-Me 1 E-5783 H H H H H 2-SEt,4-Me 1 E-5784 H H H H H 2-SEt,5-Me 1 E-5785 H H H H H 2-SEt,6-Me 1 E-5786 H H H H H 2-S(?O)Me,3-F 1 E-5787 H H H H H 2-S(?O)Me,4-F 1 E-5788 H H H H H 2-S(?O)Me,5-F 1 E-5789 H H H H H 2-S(?O)Me,6-F 1 E-5790 H H H H H 3-S(?O)Me,2-F 1 E-5791 H H H H H 3-S(?O)Me,4-F 1 E-5792 H H H H H 3-S(?O)Me,5-F 1 E-5793 H H H H H 3-S(?O)Me,6-F 1
(391) TABLE-US-00290 TABLE 290 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5794 H H H H H 2-S(?O)Me,3-Me 1 E-5795 H H H H H 2-S(?O)Me,4-Me 1 E-5796 H H H H H 2-S(?O)Me,5-Me 1 E-5797 H H H H H 2-S(?O)Me,6-Me 1 E-5798 H H H H H 2-S(?O)Me,2-Me 1 E-5799 H H H H H 3-S(?O)Me,4-Me 1 E-5800 H H H H H 3-S(?O)Me,5-Me 1 E-5801 H H H H H 3-S(?O)Me,6-Me 1 E-5802 H H H H H 2-S(?O).sub.2Me,3-F 1 E-5803 H H H H H 2-S(?O).sub.2Me,4-F 1 E-5804 H H H H H 2-S(?O).sub.2Me,5-F 1 E-5805 H H H H H 2-S(?O).sub.2Me,6-F 1 E-5806 H H H H H 2-S(?O).sub.2Me,3-Me 1 E-5807 H H H H H 2-S(?O).sub.2Me,4-Me 1 E-5808 H H H H H 2-S(?O).sub.2Me,5-Me 1 E-5809 H H H H H 2-S(?O).sub.2Me,6-Me 1 E-5810 H H H H H 2-SCF.sub.3,3-F 1 E-5811 H H H H H 2-SCF.sub.3,4-F 1 E-5812 H H H H H 2-SCF.sub.3,5-F 1 E-5813 H H H H H 2-SCF.sub.3,6-F 1 E-5814 H H H H H 2-SCF.sub.3,3-Me 1 E-5815 H H H H H 2-SCF.sub.3,4-Me 1 E-5816 H H H H H 2-SCF.sub.3,5-Me 1 E-5817 H H H H H 2-SCF.sub.3,6-Me 1 E-5818 H H H H H 2-S(?O)CF.sub.3,3-F 1 E-5819 H H H H H 2-S(?O)CF.sub.3,4-F 1 E-5820 H H H H H 2-S(?O)CF.sub.3,5-F 1 E-5821 H H H H H 2-S(?O)CF.sub.3,6-F 1 E-5822 H H H H H 2-S(?O)CF.sub.3,3-Me 1 E-5823 H H H H H 2-S(?O)CF.sub.3,4-Me 1 E-5824 H H H H H 2-S(?O)CF.sub.3,5-Me 1 E-5825 H H H H H 2-S(?O)CF.sub.3,6-Me 1 E-5826 H H H H H 2-S(?O).sub.2CF.sub.3,3-F 1 E-5827 H H H H H 2-S(?O).sub.2CF.sub.3,4-F 1 E-5828 H H H H H 2-S(?O).sub.2CF.sub.3,5-F 1 E-5829 H H H H H 2-S(?O).sub.2CF.sub.3,6-F 1 E-5830 H H H H H 2-S(?O).sub.2CF.sub.3,3-Me 1 E-5831 H H H H H 2-S(?O).sub.2CF.sub.3,4-Me 1 E-5832 H H H H H 2-S(?O).sub.2CF.sub.3,5-Me 1 E-5833 H H H H H 2-S(?O).sub.2CF.sub.3,6-Me 1 E-5834 H H H H H 2-(cyclopropylthio),3-F 1 E-5835 H H H H H 2-(cyclopropylthio),4-F 1 E-5836 H H H H H 2-(cyclopropylthio),5-F 1 E-5837 H H H H H 2-(cyclopropylthio),6-F 1 E-5838 H H H H H 2-(cyclopropylthio),3-Me 1 E-5839 H H H H H 2-(cyclopropylthio),4-Me 1 E-5840 H H H H H 2-(cyclopropylthio),5-Me 1 E-5841 H H H H H 2-(cyclopropylthio),6-Me 1 E-5842 H H H H H 2-C(?O)Me,3-F 1 E-5843 H H H H H 2-C(?O)Me,4-F 1 E-5844 H H H H H 2-C(?O)Me,5-F 1 E-5845 H H H H H 2-C(?O)Me,6-F 1 E-5846 H H H H H 2-C(?O)Me,3-Me 1 E-5847 H H H H H 2-C(?O)Me,4-Me 1 E-5848 H H H H H 2-C(?O)Me,5-Me 1 E-5849 H H H H H 2-C(?O)Me,6-Me 1 E-5850 H H H H H 3-C(?O)Me,2-F 1
(392) TABLE-US-00291 TABLE 291 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5851 H H H H H 3-C(?O)Me,4-F 1 E-5852 H H H H H 3-C(?O)Me,5-F 1 E-5853 H H H H H 3-C(?O)Me,6-F 1 E-5854 H H H H H 3-C(?O)Me,2-Me 1 E-5855 H H H H H 3-C(?O)Me,4-Me 1 E-5856 H H H H H 3-C(?O)Me,5-Me 1 E-5857 H H H H H 3-C(?O)Me,6-Me 1 E-5858 H H H H H 2-C(?O)OMe,3-F 1 E-5859 H H H H H 2-C(?O)OMe,4-F 1 E-5860 H H H H H 2-C(?O)OMe,5-F 1 E-5861 H H H H H 2-C(?O)OMe,6-F 1 E-5862 H H H H H 2-C(?O)OMe,3-Me 1 E-5863 H H H H H 2-C(?O)OMe,4-Me 1 E-5864 H H H H H 2-C(?O)OMe,5-Me 1 E-5865 H H H H H 2-C(?O)OMe,6-Me 1 E-5866 H H H H H 2-C(?O)OEt,3-F 1 E-5867 H H H H H 2-C(?O)OEt,4-F 1 E-5868 H H H H H 2-C(?O)OEt,5-F 1 E-5869 H H H H H 2-C(?O)OEt,6-F 1 E-5870 H H H H H 2-C(?O)OEt,3-Me 1 E-5871 H H H H H 2-C(?O)OEt,4-Me 1 E-5872 H H H H H 2-C(?O)OEt,5-Me 1 E-5873 H H H H H 2-C(?O)OEt,6-Me 1 E-5874 H H H H H 2-C(?O)NH.sub.2,3-F 1 E-5875 H H H H H 2-C(?O)NH.sub.2,4-F 1 E-5876 H H H H H 2-C(?O)NH.sub.2,5-F 1 E-5877 H H H H H 2-C(?O)NH.sub.2,6-F 1 E-5878 H H H H H 2-C(?O)NH.sub.2,3-Me 1 E-5879 H H H H H 2-C(?O)NH.sub.2,4-Me 1 E-5880 H H H H H 2-C(?O)NH.sub.2,5-Me 1 E-5881 H H H H H 2-C(?O)NH.sub.2,6-Me 1 E-5882 H H H H H 2-C(?O)NHMe,3-F 1 E-5883 H H H H H 2-C(?O)NHMe,4-F 1 E-5884 H H H H H 2-C(?O)NHMe,5-F 1 E-5885 H H H H H 2-C(?O)NHMe,6-F 1 E-5886 H H H H H 2-C(?O)NHMe,3-Me 1 E-5887 H H H H H 2-C(?O)NHMe,4-Me 1 E-5888 H H H H H 2-C(?O)NHMe,5-Me 1 E-5889 H H H H H 2-C(?O)NHMe,6-Me 1 E-5890 H H H H H 2-C(?O)NMe.sub.2,3-F 1 E-5891 H H H H H 2-C(?O)NMe.sub.2,4-F 1 E-5892 H H H H H 2-C(?O)NMe.sub.2,5-F 1 E-5893 H H H H H 2-C(?O)NMe.sub.2,6-F 1 E-5894 H H H H H 2-C(?O)NMe.sub.2,3-Me 1 E-5895 H H H H H 2-C(?O)NMe.sub.2,4-Me 1 E-5896 H H H H H 2-C(?O)NMe.sub.2,5-Me 1 E-5897 H H H H H 2-C(?O)NMe.sub.2,6-Me 1 E-5898 H H H H H 2-CH.sub.2OH,3-F 1 E-5899 H H H H H 2-CH.sub.2OH,4-F 1 E-5900 H H H H H 2-CH.sub.2OH,5-F 1 E-5901 H H H H H 2-CH.sub.2OH,6-F 1 E-5902 H H H H H 2-CH.sub.2OH,3-Me 1 E-5903 H H H H H 2-CH.sub.2OH,4-Me 1 E-5904 H H H H H 2-CH.sub.2OH,5-Me 1 E-5905 H H H H H 2-CH.sub.2OH,6-Me 1 E-5906 H H H H H 2-CH.sub.2OCH.sub.3,3-F 1 E-5907 H H H H H 2-CH.sub.2OCH.sub.3,4-F 1
(393) TABLE-US-00292 TABLE 292 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5908 H H H H H 2-CH.sub.2OCH.sub.3,5-F 1 E-5909 H H H H H 2-CH.sub.2OCH.sub.3,6-F 1 E-5910 H H H H H 2-CH.sub.2OCH.sub.3,3-Me 1 E-5911 H H H H H 2-CH.sub.2OCH.sub.3,4-Me 1 E-5912 H H H H H 2-CH.sub.2OCH.sub.3,5-Me 1 E-5913 H H H H H 2-CH.sub.2OCH.sub.3,6-Me 1 E-5914 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,3-F 1 E-5915 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,4-F 1 E-5916 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,5-F 1 E-5917 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-F 1 E-5918 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,3-Me 1 E-5919 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,4-Me 1 E-5920 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,5-Me 1 E-5921 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Me 1 E-5922 H H H H H 2-OC(?O)CH.sub.3,3-F 1 E-5923 H H H H H 2-OC(?O)CH.sub.3,4-F 1 E-5924 H H H H H 2-OC(?O)CH.sub.3,5-F 1 E-5925 H H H H H 2-OC(?O)CH.sub.3,6-F 1 E-5926 H H H H H 2-OC(?O)CH.sub.3,3-Me 1 E-5927 H H H H H 2-OC(?O)CH.sub.3,4-Me 1 E-5928 H H H H H 2-OC(?O)CH.sub.3,5-Me 1 E-5929 H H H H H 2-OC(?O)CH.sub.3,6-Me 1 E-5930 H H H H H 2-OS(?O).sub.2CH.sub.3,3-F 1 E-5931 H H H H H 2-OS(?O).sub.2CH.sub.3,4-F 1 E-5932 H H H H H 2-OS(?O).sub.2CH.sub.3,5-F 1 E-5933 H H H H H 2-OS(?O).sub.2CH.sub.3,6-F 1 E-5934 H H H H H 2-OS(?O).sub.2CH.sub.3,3-Me 1 E-5935 H H H H H 2-OS(?O).sub.2CH.sub.3,4-Me 1 E-5936 H H H H H 2-OS(?O).sub.2CH.sub.3,5-Me 1 E-5937 H H H H H 2-OS(?O).sub.2CH.sub.3,6-Me 1 E-5938 H H H H H 2-CH.sub.2SCH.sub.3,3-F 1 E-5939 H H H H H 2-CH.sub.2SCH.sub.3,4-F 1 E-5940 H H H H H 2-CH.sub.2SCH.sub.3,5-F 1 E-5941 H H H H H 2-CH.sub.2SCH.sub.3,6-F 1 E-5942 H H H H H 2-CH.sub.2SCH.sub.3,3-Me 1 E-5943 H H H H H 2-CH.sub.2SCH.sub.3,4-Me 1 E-5944 H H H H H 2-CH.sub.2SCH.sub.3,5-Me 1 E-5945 H H H H H 2-CH.sub.2SCH.sub.3,6-Me 1 E-5946 H H H H H 2-CH.sub.2SCF.sub.3,3-F 1 E-5947 H H H H H 2-CH.sub.2SCF.sub.3,4-F 1 E-5948 H H H H H 2-CH.sub.2SCF.sub.3,5-F 1 E-5949 H H H H H 2-CH.sub.2SCF.sub.3,6-F 1 E-5950 H H H H H 2-CH.sub.2SCF.sub.3,3-Me 1 E-5951 H H H H H 2-CH.sub.2SCF.sub.3,4-Me 1 E-5952 H H H H H 2-CH.sub.2SCF.sub.3,5-Me 1 E-5953 H H H H H 2-CH.sub.2SCF.sub.3,6-Me 1 E-5954 H H H H H 2-(benzyloxy),3-F 1 E-5955 H H H H H 2-(benzyloxy),4-F 1 E-5956 H H H H H 2-(benzyloxy),5-F 1 E-5957 H H H H H 2-(benzyloxy),6-F 1 E-5958 H H H H H 2-(benzyloxy),3-Me 1 E-5959 H H H H H 2-(benzyloxy),4-Me 1 E-5960 H H H H H 2-(benzyloxy),5-Me 1 E-5961 H H H H H 2-(benzyloxy),6-Me 1 E-5962 H H H H H 2-NH.sub.2,3-F 1 E-5963 H H H H H 2-NH.sub.2,4-F 1 E-5964 H H H H H 2-NH.sub.2,5-F 1
(394) TABLE-US-00293 TABLE 293 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-5965 H H H H H 2-NH.sub.2,6-F 1 E-5966 H H H H H 2-NH.sub.2,3-Me 1 E-5967 H H H H H 2-NH.sub.2,4-Me 1 E-5968 H H H H H 2-NH.sub.2,5-Me 1 E-5969 H H H H H 2-NH.sub.2,6-Me 1 E-5970 H H H H H 2-NHMe,3-F 1 E-5971 H H H H H 2-NHMe,4-F 1 E-5972 H H H H H 2-NHMe,5-F 1 E-5973 H H H H H 2-NHMe,6-F 1 E-5974 H H H H H 2-NHMe,3-Me 1 E-5975 H H H H H 2-NHMe,4-Me 1 E-5976 H H H H H 2-NHMe,5-Me 1 E-5977 H H H H H 2-NHMe,6-Me 1 E-5978 H H H H H 2-NHEt,3-F 1 E-5979 H H H H H 2-NHEt,4-F 1 E-5980 H H H H H 2-NHEt,5-F 1 E-5981 H H H H H 2-NHEt,6-F 1 E-5982 H H H H H 2-NHEt,3-Me 1 E-5983 H H H H H 2-NHEt,4-Me 1 E-5984 H H H H H 2-NHEt,5-Me 1 E-5985 H H H H H 2-NHEt,6-Me 1 E-5986 H H H H H 2-NMe.sub.2,3-F 1 E-5987 H H H H H 2-NMe.sub.2,4-F 1 E-5988 H H H H H 2-NMe.sub.2,5-F 1 E-5989 H H H H H 2-NMe.sub.2,6-F 1 E-5990 H H H H H 2-NMe.sub.2,3-Me 1 E-5991 H H H H H 2-NMe.sub.2,4-Me 1 E-5992 H H H H H 2-NMe.sub.2,5-Me 1 E-5993 H H H H H 2-NMe.sub.2,6-Me 1 E-5994 H H H H H 2-NEt.sub.2,3-F 1 E-5995 H H H H H 2-NEt.sub.2,4-F 1 E-5996 H H H H H 2-NEt.sub.2,5-F 1 E-5997 H H H H H 2-NEt.sub.2,6-F 1 E-5998 H H H H H 2-NEt.sub.2,3-Me 1 E-5999 H H H H H 2-NEt.sub.2,4-Me 1 E-6000 H H H H H 2-NEt.sub.2,5-Me 1 E-6001 H H H H H 2-NEt.sub.2,6-Me 1 E-6002 H H H H H 2-CHO,3-F 1 E-6003 H H H H H 2-CHO,4-F 1 E-6004 H H H H H 2-CHO,5-F 1 E-6005 H H H H H 2-CHO,6-F 1 E-6006 H H H H H 2-CHO,3-Me 1 E-6007 H H H H H 2-CHO,4-Me 1 E-6008 H H H H H 2-CHO,5-Me 1 E-6009 H H H H H 2-CHO,6-Me 1 E-6010 H H H H H 2-C(?O)OH,3-F 1 E-6011 H H H H H 2-C(?O)OH,4-F 1 E-6012 H H H H H 2-C(?O)OH,5-F 1 E-6013 H H H H H 2-C(?O)OH,6-F 1 E-6014 H H H H H 2-C(?O)OH,3-Me 1 E-6015 H H H H H 2-C(?O)OH,4-Me 1 E-6016 H H H H H 2-C(?O)OH,5-Me 1 E-6017 H H H H H 2-C(?O)OH,6-Me 1 E-6018 H H H H H 2-(1,3-dioxolan-2-yl),3-F 1 E-6019 H H H H H 2-(1,3-dioxolan-2-yl),4-F 1 E-6020 H H H H H 2-(1,3-dioxolan-2-yl),5-F 1 E-6021 H H H H H 2-(1,3-dioxolan-2-yl),6-F 1
(395) TABLE-US-00294 TABLE 294 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-6022 H H H H H 2-(1,3-dioxolan-2-yl),3-Me 1 E-6023 H H H H H 2-(1,3-dioxolan-2-yl),4-Me 1 E-6024 H H H H H 2-(1,3-dioxolan-2-yl),5-Me 1 E-6025 H H H H H 2-(1,3-dioxolan-2-yl),6-Me 1 E-6026 H H H H H 2-(1,3-dioxan-2-yl),3-F 1 E-6027 H H H H H 2-(1,3-dioxan-2-yl),4-F 1 E-6028 H H H H H 2-(1,3-dioxan-2-yl),5-F 1 E-6029 H H H H H 2-(1,3-dioxan-2-yl),6-F 1 E-6030 H H H H H 2-(1,3-dioxan-2-yl),3-Me 1 E-6031 H H H H H 2-(1,3-dioxan-2-yl),4-Me 1 E-6032 H H H H H 2-(1,3-dioxan-2-yl),5-Me 1 E-6033 H H H H H 2-(1,3-dioxan-2-yl),6-Me 1 E-6034 H H H H H 2-(thiazol-2-yl),3-F 1 E-6035 H H H H H 2-(thiazol-2-yl),4-F 1 E-6036 H H H H H 2-(thiazol-2-yl),5-F 1 E-6037 H H H H H 2-(thiazol-2-yl),6-F 1 E-6038 H H H H H 2-(thiazol-2-yl),3-Me 1 E-6039 H H H H H 2-(thiazol-2-yl),4-Me 1 E-6040 H H H H H 2-(thiazol-2-yl),5-Me 1 E-6041 H H H H H 2-(thiazol-2-yl),6-Me 1 E-6042 H H H H H 2-(oxazol-2-yl),3-F 1 E-6043 H H H H H 2-(oxazol-2-yl),4-F 1 E-6044 H H H H H 2-(oxazol-2-yl),5-F 1 E-6045 H H H H H 2-(oxazol-2-yl),6-F 1 E-6046 H H H H H 2-(oxazol-2-yl),3-Me 1 E-6047 H H H H H 2-(oxazol-2-yl),4-Me 1 E-6048 H H H H H 2-(oxazol-2-yl),5-Me 1 E-6049 H H H H H 2-(oxazol-2-yl),6-Me 1 E-6050 H H H H H 2-CH?NOH,3-F 1 E-6051 H H H H H 2-CH?NOH,4-F 1 E-6052 H H H H H 2-CH?NOH,5-F 1 E-6053 H H H H H 2-CH?NOH,6-F 1 E-6054 H H H H H 2-CH?NOH,3-Me 1 E-6055 H H H H H 2-CH?NOH,4-Me 1 E-6056 H H H H H 2-CH?NOH,5-Me 1 E-6057 H H H H H 2-CH?NOH,6-Me 1 E-6058 H H H H H 2-CH?NOMe,3-F 1 E-6059 H H H H H 2-CH?NOMe,4-F 1 E-6060 H H H H H 2-CH?NOMe,5-F 1 E-6061 H H H H H 2-CH?NOMe,6-F 1 E-6062 H H H H H 2-CH?NOMe,3-Me 1 E-6063 H H H H H 2-CH?NOMe,4-Me 1 E-6064 H H H H H 2-CH?NOMe,5-Me 1 E-6065 H H H H H 2-CH?NOMe,6-Me 1 E-6066 H H H H H 2-CN,3-F 1 E-6067 H H H H H 2-CN,4-F 1 E-6068 H H H H H 2-CN,5-F 1 E-6069 H H H H H 2-CN,6-F 1 E-6070 H H H H H 2-CN,3-Cl 1 E-6071 H H H H H 2-CN,4-Cl 1 E-6072 H H H H H 2-CN,5-Cl 1 E-6073 H H H H H 2-CN,6-Cl 1 E-6074 H H H H H 2-CN,3-Me 1 E-6075 H H H H H 2-CN,4-Me 1 E-6076 H H H H H 2-CN,5-Me 1 E-6077 H H H H H 2-CN,6-Me 1 E-6078 H H H H H 2-CN,3-OMe 1
(396) TABLE-US-00295 TABLE 295 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-6079 H H H H H 2-CN,4-OMe 1 E-6080 H H H H H 2-CN,5-OMe 1 E-6081 H H H H H 2-CN,6-OMe 1 E-6082 H H H H H 3-CN,2-F 1 E-6083 H H H H H 3-CN,4-F 1 E-6084 H H H H H 3-CN,5-F 1 E-6085 H H H H H 3-CN,6-F 1 E-6086 H H H H H 3-CN,2-Cl 1 E-6087 H H H H H 3-CN,4-Cl 1 E-6088 H H H H H 3-CN,5-Cl 1 E-6089 H H H H H 3-CN,6-Cl 1 E-6090 H H H H H 3-CN,2-Me 1 E-6091 H H H H H 3-CN,4-Me 1 E-6092 H H H H H 3-CN,5-Me 1 E-6093 H H H H H 3-CN,6-Me 1 E-6094 H H H H H 3-CN,2-OMe 1 E-6095 H H H H H 3-CN,4-OMe 1 E-6096 H H H H H 3-CN,5-OMe 1 E-6097 H H H H H 3-CN,6-OMe 1 E-6098 H H H H H 4-CN,2-F 1 E-6099 H H H H H 4-CN,3-F 1 E-6100 H H H H H 4-CN,2-Cl 1 E-6101 H H H H H 4-CN,3-Cl 1 E-6102 H H H H H 4-CN,2-Me 1 E-6103 H H H H H 4-CN,3-Me 1 E-6104 H H H H H 4-CN,2-OMe 1 E-6105 H H H H H 4-CN,3-OMe 1 E-6106 H H H H H 2-NO.sub.2,3-F 1 E-6107 H H H H H 2-NO.sub.2,4-F 1 E-6108 H H H H H 2-NO.sub.2,5-F 1 E-6109 H H H H H 2-NO.sub.2,6-F 1 E-6110 H H H H H 2-NO.sub.2,3-Me 1 E-6111 H H H H H 2-NO.sub.2,4-Me 1 E-6112 H H H H H 2-NO.sub.2,5-Me 1 E-6113 H H H H H 2-NO.sub.2,6-Me 1 E-6114 H H H H H 2-Me,3,4-F.sub.2 1 E-6115 H H H H H 2-Me,3,5-F.sub.2 1 E-6116 H H H H H 2-Me,3,6-F.sub.2 1 E-6117 H H H H H 2-Me,4,5-F.sub.2 1 E-6118 H H H H H 2-OMe,3,4-F.sub.2 1 E-6119 H H H H H 2-OMe,3,5-F.sub.2 1 E-6120 H H H H H 2-OMe,3,6-F.sub.2 1 E-6121 H H H H H 2-OMe,4,5-F.sub.2 1 E-6122 H H H H H 2-(CH.sub.2).sub.3-3 1 E-6123 H H H H H 2-(CH.sub.2).sub.4-3 1 E-6124 H H H H H 2-(OCH.sub.2CH.sub.2)-3 1 E-6125 H H H H H 2-(OCH.sub.2CH.sub.2CH.sub.2)-3 1 E-6126 H H H H H 2-(CH.sub.2CH.sub.2O)-3 1 E-6127 H H H H H 2-(CH.sub.2CH.sub.2CH.sub.2O)-3 1 E-6128 H H H H H 3-(CH.sub.2).sub.3-4 1 E-6129 H H H H H 3-(CH.sub.2).sub.4-4 1 E-6130 H H H H H 3-(OCH.sub.2CH.sub.2)-4 1 E-6131 H H H H H 3-(OCH.sub.2CH.sub.2CH.sub.2)-4 1 E-6132 H H H H H 3-(CH.sub.2CH.sub.2O)-4 1 E-6133 H H H H H 3-(CH.sub.2CH.sub.2CH.sub.2O)-4 1 E-6134 H H H H H 2-(OCH.sub.2O)-3 1 E-6135 H H H H H 3-(OCH.sub.2O)-4 1
(397) TABLE-US-00296 TABLE 296 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 (R.sup.8).sub.m p E-6136 H H H H H 2-(OCH.sub.2CH.sub.2O)-3 1 E-6137 H H H H H 3-(OCH.sub.2CH.sub.2O)-4 1 E-6138 H H H H H 2-(OCF.sub.2O)-3 1 E-6139 H H H H H 3-(OCF.sub.2O)-4 1 E-6140 H H H H H 2-Me,6-Et 1 E-6141 H H H H H 2-Me,4,5-F.sub.2 1 E-6142 H H H H H 2-cyclopropyl,6-OMe 1 E-6143 H H H H H 2-Me,5-Et 1 E-6144 H H H H H 2,6-Et.sub.2 1 E-6145 H H H H H 2-Et,6-F 1 E-6146 H H H H H 2-CH.sub.2OCH.sub.3,6-Cl 1 E-6147 H H H H H 2-CH.sub.2OCH.sub.2CH.sub.3,6-Cl 1 E-6148 H H H H H 2-CH.sub.2NMe.sub.2 1
(398) TABLE-US-00297 TABLE 297
(399) TABLE-US-00298 TABLE 298 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-0053 H H H H H 3-F-4-Cl-pyridin-2-yl 0 F-0054 H H H H H 3-F-5-Cl-pyridin-2-yl 0 F-0055 H H H H H 3-F-6-Cl-pyridin-2-yl 0 F-0056 H H H H H 3-F-4-Me-pyridin-2-yl 0 F-0057 H H H H H 3-F-5-Me-pyridin-2-yl 0 F-0058 H H H H H 3-F-6-Me-pyridin-2-yl 0 F-0059 H H H H H 3-F-4-OMe-pyridin-2-yl 0 F-0060 H H H H H 3-F-5-OMe-pyridin-2-yl 0 F-0061 H H H H H 3-F-6-OMe-pyridin-2-yl 0 F-0062 H H H H H 3-Cl-4-F-pyridin-2-yl 0 F-0063 H H H H H 3-Cl-5-F-pyridin-2-yl 0 F-0064 H H H H H 3-Cl-6-F-pyridin-2-yl 0 F-0065 H H H H H 3-Cl-4-Me-pyridin-2-yl 0 F-0066 H H H H H 3-Cl-5-Me-pyridin-2-yl 0 F-0067 H H H H H 3-Cl-6-Me-pyridin-2-yl 0 F-0068 H H H H H 3-Me-4-F-pyridin-2-yl 0 F-0069 H H H H H 3-Me-5-F-pyridin-2-yl 0 F-0070 H H H H H 3-Me-6-F-pyridin-2-yl 0 F-0071 H H H H H 3-Me-4-Cl-pyridin-2-yl 0 F-0072 H H H H H 3-Me-5-Cl-pyridin-2-yl 0 F-0073 H H H H H 3-Me-6-Cl-pyridin-2-yl 0 F-0074 H H H H H 3,4-(Me).sub.2-pyridin-2-yl 0 F-0075 H H H H H 3,5-(Me).sub.2-pyridin-2-yl 0 F-0076 H H H H H 3,6-(Me).sub.2-pyridin-2-yl 0 F-0077 H H H H H 3-Me-4-OMe-pyridin-2-yl 0 F-0078 H H H H H 3-Me-5-OMe-pyridin-2-yl 0 F-0079 H H H H H 3-Me-6-OMe-pyridin-2-yl 0 F-0080 H H H H H 3-CF.sub.3-4-F-pyridin-2-yl 0 F-0081 H H H H H 3-CF.sub.3-5-F-pyridin-2-yl 0 F-0082 H H H H H 3-CF.sub.3-6-F-pyridin-2-yl 0 F-0083 H H H H H 3-CF.sub.3-4-Me-pyridin-2-yl 0 F-0084 H H H H H 3-CF.sub.3-5-Me-pyridin-2-yl 0 F-0085 H H H H H 3-CF.sub.3-6-Me-pyridin-2-yl 0 F-0086 H H H H H 3-OMe-4-F-pyridin-2-yl 0 F-0087 H H H H H 3-OMe-5-F-pyridin-2-yl 0 F-0088 H H H H H 3-OMe-6-F-pyridin-2-yl 0 F-0089 H H H H H 3-OMe-4-Cl-pyridin-2-yl 0 F-0090 H H H H H 3-OMe-5-Cl-pyridin-2-yl 0 F-0091 H H H H H 3-OMe-6-Cl-pyridin-2-yl 0 F-0092 H H H H H 3-OMe-4-Me-pyridin-2-yl 0 F-0093 H H H H H 3-OMe-5-Me-pyridin-2-yl 0 F-0094 H H H H H 3-OMe-6-Me-pyridin-2-yl 0 F-0095 H H H H H 3,4-(OMe).sub.2-pyridin-2-yl 0 F-0096 H H H H H 3,5-(OMe).sub.2-pyridin-2-yl 0 F-0097 H H H H H 3,6-(OMe).sub.2-pyridin-2-yl 0 F-0098 H H H H H pyridin-3-yl 0 F-0099 H H H H H 2-F-pyridin-3-yl 0 F-0100 H H H H H 4-F-pyridin-3-yl 0 F-0101 H H H H H 5-F-pyridin-3-yl 0 F-0102 H H H H H 6-F-pyridin-3-yl 0 F-0103 H H H H H 2-Cl-pyridin-3-yl 0 F-0104 H H H H H 4-Cl-pyridin-3-yl 0 F-0105 H H H H H 5-Cl-pyridin-3-yl 0 F-0106 H H H H H 6-Cl-pyridin-3-yl 0 F-0107 H H H H H 2-Me-pyridin-3-yl 0 F-0108 H H H H H 4-Me-pyridin-3-yl 0 F-0109 H H H H H 5-Me-pyridin-3-yl 0
(400) TABLE-US-00299 TABLE 299 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-0110 H H H H H 6-Me-pyridin-3-yl 0 F-0111 H H H H H 2-CF.sub.3-pyridin-3-yl 0 F-0112 H H H H H 4-CF.sub.3-pyridin-3-yl 0 F-0113 H H H H H 5-CF.sub.3-pyridin-3-yl 0 F-0114 H H H H H 6-CF.sub.3-pyridin-3-yl 0 F-0115 H H H H H 2-OMe-pyridin-3-yl 0 F-0116 H H H H H 4-OMe-pyridin-3-yl 0 F-0117 H H H H H 5-OMe-pyridin-3-yl 0 F-0118 H H H H H 6-OMe-pyridin-3-yl 0 F-0119 H H H H H 2,4-F.sub.2-pyridin-3-yl 0 F-0120 H H H H H 2,5-F.sub.2-pyridin-3-yl 0 F-0121 H H H H H 2,6-F.sub.2-pyridin-3-yl 0 F-0122 H H H H H 4,5-F.sub.2-pyridin-3-yl 0 F-0123 H H H H H 4,6-F.sub.2-pyridin-3-yl 0 F-0124 H H H H H 2,4-Cl.sub.2-pyridin-3-yl 0 F-0125 H H H H H 2,5-Cl.sub.2-pyridin-3-yl 0 F-0126 H H H H H 2,6-Cl.sub.2-pyridin-3-yl 0 F-0127 H H H H H 4,5-Cl.sub.2-pyridin-3-yl 0 F-0128 H H H H H 4,6-Cl.sub.2-pyridin-3-yl 0 F-0129 H H H H H 2-F-4-Cl-pyridin-3-yl 0 F-0130 H H H H H 2-F-5-Cl-pyridin-3-yl 0 F-0131 H H H H H 2-F-6-Cl-pyridin-3-yl 0 F-0132 H H H H H 4-F-2-Cl-pyridin-3-yl 0 F-0133 H H H H H 4-F-5-Cl-pyridin-3-yl 0 F-0134 H H H H H 4-F-6-Cl-pyridin-3-yl 0 F-0135 H H H H H 2-F-4-Me-pyridin-3-yl 0 F-0136 H H H H H 2-F-5-Me-pyridin-3-yl 0 F-0137 H H H H H 2-F-6-Me-pyridin-3-yl 0 F-0138 H H H H H 4-F-2-Me-pyridin-3-yl 0 F-0139 H H H H H 4-F-5-Me-pyridin-3-yl 0 F-0140 H H H H H 4-F-6-Me-pyridin-3-yl 0 F-0141 H H H H H 2-F-4-OMe-pyridin-3-yl 0 F-0142 H H H H H 2-F-5-OMe-pyridin-3-yl 0 F-0143 H H H H H 2-F-6-OMe-pyridin-3-yl 0 F-0144 H H H H H 4-F-2-OMe-pyridin-3-yl 0 F-0145 H H H H H 4-F-5-OMe-pyridin-3-yl 0 F-0146 H H H H H 4-F-6-OMe-pyridin-3-yl 0 F-0147 H H H H H 2-Cl-5-F-pyridin-3-yl 0 F-0148 H H H H H 2-Cl-6-F-pyridin-3-yl 0 F-0149 H H H H H 4-Cl-5-F-pyridin-3-yl 0 F-0150 H H H H H 4-Cl-6-F-pyridin-3-yl 0 F-0151 H H H H H 2-Cl-4-Me-pyridin-3-yl 0 F-0152 H H H H H 2-Cl-5-Me-pyridin-3-yl 0 F-0153 H H H H H 2-Cl-6-Me-pyridin-3-yl 0 F-0154 H H H H H 4-Cl-2-Me-pyridin-3-yl 0 F-0155 H H H H H 4-Cl-5-Me-pyridin-3-yl 0 F-0156 H H H H H 4-Cl-6-Me-pyridin-3-yl 0 F-0157 H H H H H 2-Me-5-F-pyridin-3-yl 0 F-0158 H H H H H 2-Me-6-F-pyridin-3-yl 0 F-0159 H H H H H 4-Me-5-F-pyridin-3-yl 0 F-0160 H H H H H 4-Me-6-F-pyridin-3-yl 0 F-0161 H H H H H 2-Me-5-Cl-pyridin-3-yl 0 F-0162 H H H H H 2-Me-6-Cl-pyridin-3-yl 0 F-0163 H H H H H 4-Me-5-Cl-pyridin-3-yl 0 F-0164 H H H H H 4-Me-6-Cl-pyridin-3-yl 0 F-0165 H H H H H 2,4-(Me).sub.2-pyridin-3-yl 0 F-0166 H H H H H 2,5-(Me).sub.2-pyridin-3-yl 0
(401) TABLE-US-00300 TABLE 300 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-0167 H H H H H 2,6-(Me).sub.2-pyridin-3-yl 0 F-0168 H H H H H 4,5-(Me).sub.2-pyridin-3-yl 0 F-0169 H H H H H 4,6-(Me).sub.2-pyridin-3-yl 0 F-0170 H H H H H 2-Me-4-OMe-pyridin-3-yl 0 F-0171 H H H H H 2-Me-5-OMe-pyridin-3-yl 0 F-0172 H H H H H 2-Me-6-OMe-pyridin-3-yl 0 F-0173 H H H H H 4-Me-2-OMe-pyridin-3-yl 0 F-0174 H H H H H 4-Me-5-OMe-pyridin-3-yl 0 F-0175 H H H H H 4-Me-6-OMe-pyridin-3-yl 0 F-0176 H H H H H 2-CF.sub.3-4-F-pyridin-3-yl 0 F-0177 H H H H H 2-CF.sub.3-5-F-pyridin-3-yl 0 F-0178 H H H H H 2-CF.sub.3-6-F-pyridin-3-yl 0 F-0179 H H H H H 4-CF.sub.3-2-F-pyridin-3-yl 0 F-0180 H H H H H 4-CF.sub.3-5-F-pyridin-3-yl 0 F-0181 H H H H H 4-CF.sub.3-6-F-pyridin-3-yl 0 F-0182 H H H H H 2-CF.sub.3-4-Me-pyridin-3-yl 0 F-0183 H H H H H 2-CF.sub.3-5-Me-pyridin-3-yl 0 F-0184 H H H H H 2-CF.sub.3-6-Me-pyridin-3-yl 0 F-0185 H H H H H 4-CF.sub.3-2-Me-pyridin-3-yl 0 F-0186 H H H H H 4-CF.sub.3-5-Me-pyridin-3-yl 0 F-0187 H H H H H 4-CF.sub.3-6-Me-pyridin-3-yl 0 F-0188 H H H H H 2-OMe-5-F-pyridin-3-yl 0 F-0189 H H H H H 2-OMe-6-F-pyridin-3-yl 0 F-0190 H H H H H 4-OMe-5-F-pyridin-3-yl 0 F-0191 H H H H H 4-OMe-6-F-pyridin-3-yl 0 F-0192 H H H H H 2-OMe-4-Cl-pyridin-3-yl 0 F-0193 H H H H H 2-OMe-5-Cl-pyridin-3-yl 0 F-0194 H H H H H 2-OMe-6-Cl-pyridin-3-yl 0 F-0195 H H H H H 4-OMe-2-Cl-pyridin-3-yl 0 F-0196 H H H H H 4-OMe-5-Cl-pyridin-3-yl 0 F-0197 H H H H H 4-OMe-6-Cl-pyridin-3-yl 0 F-0198 H H H H H 2-OMe-5-Me-pyridin-3-yl 0 F-0199 H H H H H 2-OMe-6-Me-pyridin-3-yl 0 F-0200 H H H H H 4-OMe-5-Me-pyridin-3-yl 0 F-0201 H H H H H 4-OMe-6-Me-pyridin-3-yl 0 F-0202 H H H H H 2,4-(OMe).sub.2-pyridin-3-yl 0 F-0203 H H H H H 2,5-(OMe).sub.2-pyridin-3-yl 0 F-0204 H H H H H 2,6-(OMe).sub.2-pyridin-3-yl 0 F-0205 H H H H H 4,5-(OMe).sub.2-pyridin-3-yl 0 F-0206 H H H H H 4,6-(OMe).sub.2-pyridin-3-yl 0 F-0207 H H H H H pyridin-4-yl 0 F-0208 H H H H H 2-F-pyridin-4-yl 0 F-0209 H H H H H 3-F-pyridin-4-yl 0 F-0210 H H H H H 2-Cl-pyridin-4-yl 0 F-0211 H H H H H 3-Cl-pyridin-4-yl 0 F-0212 H H H H H 2-Me-pyridin-4-yl 0 F-0213 H H H H H 3-Me-pyridin-4-yl 0 F-0214 H H H H H 2-CF.sub.3-pyridin-4-yl 0 F-0215 H H H H H 3-CF.sub.3-pyridin-4-yl 0 F-0216 H H H H H 2-OMe-pyridin-4-yl 0 F-0217 H H H H H 3-OMe-pyridin-4-yl 0 F-0218 H H H H H 2,3-F.sub.2-pyridin-4-yl 0 F-0219 H H H H H 2,5-F.sub.2-pyridin-4-yl 0 F-0220 H H H H H 2,6-F.sub.2-pyridin-4-yl 0 F-0221 H H H H H 3,5-F.sub.2-pyridin-4-yl 0 F-0222 H H H H H 2,3-Cl.sub.2-pyridin-4-yl 0 F-0223 H H H H H 2,5-Cl.sub.2-pyridin-4-yl 0
(402) TABLE-US-00301 TABLE 301 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-0224 H H H H H 2,6-Cl.sub.2-pyridin-4-yl 0 F-0225 H H H H H 3,5-Cl.sub.2-pyridin-4-yl 0 F-0226 H H H H H 3-F-2-Cl-pyridin-4-yl 0 F-0227 H H H H H 3-F-5-Cl-pyridin-4-yl 0 F-0228 H H H H H 3-F-6-Cl-pyridin-4-yl 0 F-0229 H H H H H 3-F-2-Me-pyridin-4-yl 0 F-0230 H H H H H 3-F-5-Me-pyridin-4-yl 0 F-0231 H H H H H 3-F-6-Me-pyridin-4-yl 0 F-0232 H H H H H 3-F-2-OMe-pyridin-4-yl 0 F-0233 H H H H H 3-F-5-OMe-pyridin-4-yl 0 F-0234 H H H H H 3-F-6-OMe-pyridin-4-yl 0 F-0235 H H H H H 3-Cl-2-F-pyridin-4-yl 0 F-0236 H H H H H 3-Cl-6-F-pyridin-4-yl 0 F-0237 H H H H H 3-Cl-2-Me-pyridin-4-yl 0 F-0238 H H H H H 3-Cl-5-Me-pyridin-4-yl 0 F-0239 H H H H H 3-Cl-6-Me-pyridin-4-yl 0 F-0240 H H H H H 3-Me-2-F-pyridin-4-yl 0 F-0241 H H H H H 3-Me-6-F-pyridin-4-yl 0 F-0242 H H H H H 3-Me-2-Cl-pyridin-4-yl 0 F-0243 H H H H H 3-Me-6-Cl-pyridin-4-yl 0 F-0244 H H H H H 2,3-(Me).sub.2-pyridin-4-yl 0 F-0245 H H H H H 3,5-(Me).sub.2-pyridin-4-yl 0 F-0246 H H H H H 3,6-(Me).sub.2-pyridin-4-yl 0 F-0247 H H H H H 3-Me-2-OMe-pyridin-4-yl 0 F-0248 H H H H H 3-Me-5-OMe-pyridin-4-yl 0 F-0249 H H H H H 3-Me-6-OMe-pyridin-4-yl 0 F-0250 H H H H H 3-CF.sub.3-2-F-pyridin-4-yl 0 F-0251 H H H H H 3-CF.sub.3-5-F-pyridin-4-yl 0 F-0252 H H H H H 3-CF.sub.3-6-F-pyridin-4-yl 0 F-0253 H H H H H 3-CF.sub.3-2-Me-pyridin-4-yl 0 F-0254 H H H H H 3-CF.sub.3-5-Me-pyridin-4-yl 0 F-0255 H H H H H 3-CF.sub.3-6-Me-pyridin-4-yl 0 F-0256 H H H H H 3-OMe-2-F-pyridin-4-yl 0 F-0257 H H H H H 3-OMe-6-F-pyridin-4-yl 0 F-0258 H H H H H 3-OMe-2-Cl-pyridin-4-yl 0 F-0259 H H H H H 3-OMe-5-Cl-pyridin-4-yl 0 F-0260 H H H H H 3-OMe-6-Cl-pyridin-4-yl 0 F-0261 H H H H H 3-OMe-2-Me-pyridin-4-yl 0 F-0262 H H H H H 3-OMe-6-Me-pyridin-4-yl 0 F-0263 H H H H H 2,3-(OMe).sub.2-pyridin-4-yl 0 F-0264 H H H H H 3,5-(OMe).sub.2-pyridin-4-yl 0 F-0265 H H H H H 3,6-(OMe).sub.2-pyridin-4-yl 0 F-0266 H H H H H pyrimidin-2-yl 0 F-0267 H H H H H pyrimidin-4-yl 0 F-0268 H H H H H 5-F-pyrimidin-4-yl 0 F-0269 H H H H H 5-Me-pyrimidin-4-yl 0 F-0270 H H H H H 5-CF.sub.3-pyrimidin-4-yl 0 F-0271 H H H H H 5-OMe-pyrimidin-4-yl 0 F-0272 H H H H H pyrimidin-5-yl 0 F-0273 H H H H H 4-F-pyrimidin-5-yl 0 F-0274 H H H H H 4-Cl-pyrimidin-5-yl 0 F-0275 H H H H H 4-Me-pyrimidin-5-yl 0 F-0276 H H H H H 4-CF.sub.3-pyrimidin-5-yl 0 F-0277 H H H H H 4-OMe-pyrimidin-5-yl 0 F-0278 H H H H H pyridazin-3-yl 0 F-0279 H H H H H 4-F-pyridazin-3-yl 0 F-0280 H H H H H 4-Cl-pyridazin-3-yl 0
(403) TABLE-US-00302 TABLE 302 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-0281 H H H H H 4-Me-pyridazin-3-yl 0 F-0282 H H H H H 4-CF.sub.3-pyridazin-3-yl 0 F-0283 H H H H H 4-OMe-pyridazin-3-yl 0 F-0284 H H H H H pyridazin-4-yl 0 F-0285 H H H H H 3-F-pyridazin-4-yl 0 F-0286 H H H H H 3-Cl-pyridazin-4-yl 0 F-0287 H H H H H 3-Me-pyridazin-4-yl 0 F-0288 H H H H H 3-CF.sub.3-pyridazin-4-yl 0 F-0289 H H H H H 3-OMe-pyridazin-4-yl 0 F-0290 H H H H H 5-F-pyridazin-4-yl 0 F-0291 H H H H H 5-Cl-pyridazin-4-yl 0 F-0292 H H H H H 5-Me-pyridazin-4-yl 0 F-0293 H H H H H 5-CF.sub.3-pyridazin-4-yl 0 F-0294 H H H H H 5-OMe-pyridazin-4-yl 0 F-0295 H H H H H thiophen-2-yl 0 F-0296 H H H H H 3-F-thiophen-2-yl 0 F-0297 H H H H H 3-Cl-thiophen-2-yl 0 F-0298 H H H H H 3-Me-thiophen-2-yl 0 F-0299 H H H H H 3-CF.sub.3-thiophen-2-yl 0 F-0300 H H H H H 3-OMe-thiophen-2-yl 0 F-0301 H H H H H thiophen-3-yl 0 F-0302 H H H H H 2-F-thiophen-3-yl 0 F-0303 H H H H H 2-Cl-thiophen-3-yl 0 F-0304 H H H H H 2-Me-thiophen-3-yl 0 F-0305 H H H H H 2-CF.sub.3-thiophen-3-yl 0 F-0306 H H H H H 2-OMe-thiophen-3-yl 0 F-0307 H H H H H 4-F-thiophen-3-yl 0 F-0308 H H H H H 4-Cl-thiophen-3-yl 0 F-0309 H H H H H 4-Me-thiophen-3-yl 0 F-0310 H H H H H 4-CF.sub.3-thiophen-3-yl 0 F-0311 H H H H H 4-OMe-thiophen-3-yl 0 F-0312 H H H H H thiazol-2-yl 0 F-0313 H H H H H thiazol-4-yl 0 F-0314 H H H H H 5-F-thiazol-4-yl 0 F-0315 H H H H H 5-Me-thiazol-4-yl 0 F-0316 H H H H H 5-CF.sub.3-thiazol-4-yl 0 F-0317 H H H H H 5-OMe-thiazol-4-yl 0 F-0318 H H H H H thiazol-5-yl 0 F-0319 H H H H H 4-F-thiazol-5-yl 0 F-0320 H H H H H 4-Me-thiazol-5-yl 0 F-0321 H H H H H 4-CF.sub.3-thiazol-5-y 0 F-0322 H H H H H 4-OMe-thiazol-5-yl 0 F-0323 H H H H H 1H-pyrrol-1-yl 0 F-0324 H H H H H 2-F-1H-pyrrol-1-yl 0 F-0325 H H H H H 2-Me-1H-pyrrol-1-yl 0 F-0326 H H H H H 2-CF.sub.3-1H-pyrrol-1-yl 0 F-0327 H H H H H 2-OMe-1H-pyrrol-1-yl 0 F-0328 H H H H H 1H-pyrrol-2-yl 0 F-0329 H H H H H 1-Me-1H-pyrrol-2-yl 0 F-0330 H H H H H 3-F-1H-pyrrol-2-yl 0 F-0331 H H H H H 3-Me-1H-pyrrol-2-yl 0 F-0332 H H H H H 3-CF.sub.3-1H-pyrrol-2-yl 0 F-0333 H H H H H 3-OMe-1H-pyrrol-2-yl 0 F-0334 H H H H H 1-Me-3-F-1H-pyrrol-2-yl 0 F-0335 H H H H H 1,3-(Me).sub.2-1H-pyrrol-2-yl 0 F-0336 H H H H H 1-Me-3-CF.sub.3-1H-pyrrol-2-yl 0 F-0337 H H H H H 1-Me-3-OMe-1H-pyrrol-2-yl 0
(404) TABLE-US-00303 TABLE 303 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-0338 H H H H H 1H-pyrrol-3-yl 0 F-0339 H H H H H 1-Me-1H-pyrrol-3-yl 0 F-0340 H H H H H 2-F-1H-pyrrol-3-yl 0 F-0341 H H H H H 2-Me-1H-pyrrol-3-yl 0 F-0342 H H H H H 2-CF.sub.3-1H-pyrrol-3-yl 0 F-0343 H H H H H 2-OMe-1H-pyrrol-3-yl 0 F-0344 H H H H H 1-Me-2-F-1H-pyrrol-3-yl 0 F-0345 H H H H H 1,2-(Me).sub.2-1H-pyrrol-3-yl 0 F-0346 H H H H H 1-Me-2-CF.sub.3-1H-pyrrol-3-yl 0 F-0347 H H H H H 1-Me-2-OMe-1H-pyrrol-3-yl 0 F-0348 H H H H H 4-F-1H-pyrrol-3-yl 0 F-0349 H H H H H 4-Me-1H-pyrrol-3-yl 0 F-0350 H H H H H 4-CF.sub.3-1H-pyrrol-3-yl 0 F-0351 H H H H H 4-OMe-1H-pyrrol-3-yl 0 F-0352 H H H H H 1-Me-4-F-1H-pyrrol-3-yl 0 F-0353 H H H H H 1,4-(Me).sub.2-1H-pyrrol-3-yl 0 F-0354 H H H H H 1-Me-4-CF.sub.3-1H-pyrrol-3-yl 0 F-0355 H H H H H 1-Me-4-OMe-1H-pyrrol-3-yl 0 F-0356 H H H H H 1H-pyrazol-1-yl 0 F-0357 H H H H H 5-F-1H-pyrazol-1-yl 0 F-0358 H H H H H 5-Cl-1H-pyrazol-1-yl 0 F-0359 H H H H H 5-Me-1H-pyrazol-1-yl 0 F-0360 H H H H H 5-CF.sub.3-1H-pyrazol-1-yl 0 F-0361 H H H H H 5-OMe-1H-pyrazol-1-yl 0 F-0362 H H H H H 1H-pyrazol-3-yl 0 F-0363 H H H H H 1-Me-1H-pyrazol-3-yl 0 F-0364 H H H H H 4-F-1H-pyrazol-3-yl 0 F-0365 H H H H H 4-Cl-1H-pyrazol-3-yl 0 F-0366 H H H H H 4-Me-1H-pyrazol-3-yl 0 F-0367 H H H H H 4-CF.sub.3-1H-pyrazol-3-yl 0 F-0368 H H H H H 4-OMe-1H-pyrazol-3-yl 0 F-0369 H H H H H 1-Me-4-F-1H-pyrazol-3-yl 0 F-0370 H H H H H 1-Me-4-Cl-1H-pyrazol-3-yl 0 F-0371 H H H H H 1,4-(Me).sub.2-1H-pyrazol-3-yl 0 F-0372 H H H H H 1-Me-4-CF.sub.3-1H-pyrazol-3-yl 0 F-0373 H H H H H 1-Me-4-OMe-1H-pyrazol-3-yl 0 F-0374 H H H H H 1H-pyrazol-4-yl 0 F-0375 H H H H H 1-Me-1H-pyrazol-4-yl 0 F-0376 H H H H H 3-F-1H-pyrazol-4-yl 0 F-0377 H H H H H 3-Cl-1H-pyrazol-4-yl 0 F-0378 H H H H H 3-Me-1H-pyrazol-4-yl 0 F-0379 H H H H H 3-CF.sub.3-1H-pyrazol-4-yl 0 F-0380 H H H H H 3-OMe-1H-pyrazol-4-yl 0 F-0381 H H H H H 1-Me-3-F-1H-pyrazol-4-yl 0 F-0382 H H H H H 1-Me-3-Cl-1H-pyrazol-4-yl 0 F-0383 H H H H H 1,3-(Me).sub.2-1H-pyrazol-4-yl 0 F-0384 H H H H H 1-Me-3-CF.sub.3-1H-pyrazol-4-yl 0 F-0385 H H H H H 1-Me-3-OMe-1H-pyrazol-4-yl 0 F-0386 H H H H H 5-F-1H-pyrazol-4-yl 0 F-0387 H H H H H 5-Cl-1H-pyrazol-4-yl 0 F-0388 H H H H H 5-Me-1H-pyrazol-4-yl 0 F-0389 H H H H H 5-CF.sub.3-1H-pyrazol-4-yl 0 F-0390 H H H H H 5-OMe-1H-pyrazol-4-yl 0 F-0391 H H H H H 1-Me-5-F-1H-pyrazol-4-yl 0 F-0392 H H H H H 1-Me-5-Cl-1H-pyrazol-4-yl 0 F-0393 H H H H H 1,5-(Me).sub.2-1H-pyrazol-4-yl 0 F-0394 H H H H H 1-Me-5-CF.sub.3-1H-pyrazol-4-yl 0
(405) TABLE-US-00304 TABLE 304 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-0395 H H H H H 1-Me-5-OMe-1H-pyrazol-4-yl 0 F-0396 H H H H H 1H-pyrazol-5-yl 0 F-0397 H H H H H 1-Me-1H-pyrazol-5-yl 0 F-0398 H H H H H 4-F-1H-pyrazol-5-yl 0 F-0399 H H H H H 4-Cl-1H-pyrazol-5-yl 0 F-0400 H H H H H 4-Me-1H-pyrazol-5-yl 0 F-0401 H H H H H 4-CF.sub.3-1H-pyrazol-5-yl 0 F-0402 H H H H H 4-OMe-1H-pyrazol-5-yl 0 F-0403 H H H H H 1-Me-4-F-1H-pyrazol-5-yl 0 F-0404 H H H H H 1-Me-4-Cl-1H-pyrazol-5-yl 0 F-0405 H H H H H 1,4-(Me).sub.2-1H-pyrazol-5-yl 0 F-0406 H H H H H 1-Me-4-CF.sub.3-1H-pyrazol-5-yl 0 F-0407 H H H H H 1-Me-4-OMe-1H-pyrazol-5-yl 0 F-0408 H H H H H furan-2-yl 0 F-0409 H H H H H 3-F-furan-2-yl 0 F-0410 H H H H H 3-Me-furan-2-yl 0 F-0411 H H H H H 3-CF.sub.3-furan-2-yl 0 F-0412 H H H H H 3-OMe-furan-2-yl 0 F-0413 H H H H H furan-3-yl 0 F-0414 H H H H H 2-F-furan-3-yl 0 F-0415 H H H H H 2-Me-furan-3-yl 0 F-0416 H H H H H 2-CF.sub.3-furan-3-yl 0 F-0417 H H H H H 2-OMe-furan-3-yl 0 F-0418 H H H H H 4-F-furan-3-yl 0 F-0419 H H H H H 4-Me-furan-3-yl 0 F-0420 H H H H H 4-CF3-furan-3-yl 0 F-0421 H H H H H 4-OMe-furan-3-yl 0 F-0422 H H H H H isoxazol-3-yl 0 F-0423 H H H H H 4-F-isoxazol-3-yl 0 F-0424 H H H H H 4-Me-isoxazol-3-yl 0 F-0425 H H H H H 4-CF.sub.3-isoxazol-3-yl 0 F-0426 H H H H H 4-OMe-isoxazol-3-yl 0 F-0427 H H H H H isoxazol-4-yl 0 F-0428 H H H H H 5-F-isoxazol-4-yl 0 F-0429 H H H H H 5-Me-isoxazol-4-yl 0 F-0430 H H H H H 5-CF.sub.3-isoxazol-4-yl 0 F-0431 H H H H H 5-OMe-isoxazol-4-yl 0 F-0432 H H H H H isoxazol-5-yl 0 F-0433 H H H H H 4-F-isoxazol-5-yl 0 F-0434 H H H H H 4-Me-isoxazol-5-yl 0 F-0435 H H H H H 4-CF.sub.3-isoxazol-5-yl 0 F-0436 H H H H H 4-OMe-isoxazol-5-yl 0 F-0437 H H H H H 1H-1,2,3-triazol-1-yl 0 F-0438 H H H H H 5-F-1H-1,2,3-triazol-1-yl 0 F-0439 H H H H H 5-Me-1H-1,2,3-triazol-1-yl 0 F-0440 H H H H H 5-CF.sub.3-1H-1,2,3-triazol-1-yl 0 F-0441 H H H H H 5-OMe-1H-1,2,3-triazol-1-yl 0 F-0442 H H H H H 1H-1,2,3-triazol-4-yl 0 F-0443 H H H H H 5-F-1H-1,2,3-triazol-4-yl 0 F-0444 H H H H H 5-Me-1H-1,2,3-triazol-4-yl 0 F-0445 H H H H H 5-CF.sub.3-1H-1,2,3-triazol-4-yl 0 F-0446 H H H H H 5-OMe-1H-1,2,3-triazol-4-yl 0 F-0447 H H H H H 1H-1,2,3-triazol-5-yl 0 F-0448 H H H H H 4-F-1H-1,2,3-triazol-5-yl 0 F-0449 H H H H H 4-Me-1H-1,2,3-triazol-5-yl 0 F-0450 H H H H H 4-CF.sub.3-1H-1,2,3-triazol-5-yl 0 F-0451 H H H H H 4-OMe-1H-1,2,3-triazol-5-yl 0
(406) TABLE-US-00305 TABLE 305 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-0452 H H H H H 1H-1,2,4-triazol-1-yl 0 F-0453 H H H H H 5-Me-1H-1,2,4-triazol-1-yl 0 F-0454 H H H H H 5-F-1H-1,2,4-triazol-1-yl 0 F-0455 H H H H H 5-CF.sub.3-1H-1,2,4-triazo-1-y 0 F-0456 H H H H H 5-OMe-1H-1,2,4-triazol-1-yl 0 F-0457 H H H H H 1H-1,2,4-triazol-3-yl 0 F-0458 H H H H H 1-Me-1H-1,2,4-triazol-3-yl 0 F-0459 H H H H H 1H-1,2,4-triazol-5-yl 0 F-0460 H H H H H 1-Me-1H-1,2,4-triazol-5-yl 0 F-0461 H H H H H 3,5-(Me).sub.2-isoxazol-4-yl 0 F-0462 H H H H H 3,5-(Et).sub.2-isoxazol-4-yl 0 F-0463 H H H H H quinolin-4-yl 0 F-0464 H H H H H isoquinolin-4-yl 0 F-0465 H H H H H 3,6-(OMe).sub.2-pyridazin-4-yl 0 F-0466 H H H H H 2,4-(OMe).sub.2-pyrimidin-5-yl 0
(407) TABLE-US-00306 TABLE 306
(408) TABLE-US-00307 TABLE 307 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-5053 H H H H H 3-F-4-Cl-pyridin-2-yl 1 F-5054 H H H H H 3-F-5-Cl-pyridin-2-yl 1 F-5055 H H H H H 3-F-6-Cl-pyridin-2-yl 1 F-5056 H H H H H 3-F-4-Me-pyridin-2-yl 1 F-5057 H H H H H 3-F-5-Me-pyridin-2-yl 1 F-5058 H H H H H 3-F-6-Me-pyridin-2-yl 1 F-5059 H H H H H 3-F-4-OMe-pyridin-2-yl 1 F-5060 H H H H H 3-F-5-OMe-pyridin-2-yl 1 F-5061 H H H H H 3-F-6-OMe-pyridin-2-yl 1 F-5062 H H H H H 3-Cl-4-F-pyridin-2-yl 1 F-5063 H H H H H 3-Cl-5-F-pyridin-2-yl 1 F-5064 H H H H H 3-Cl-6-F-pyridin-2-yl 1 F-5065 H H H H H 3-Cl-4-Me-pyridin-2-yl 1 F-5066 H H H H H 3-Cl-5-Me-pyridin-2-yl 1 F-5067 H H H H H 3-Cl-6-Me-pyridn-2-yl 1 F-5068 H H H H H 3-Me-4-F-pyridin-2-yl 1 F-5069 H H H H H 3-Me-5-F-pyridin-2-yl 1 F-5070 H H H H H 3-Me-6-F-pyridin-2-yl 1 F-5071 H H H H H 3-Me-4-Cl-pyridin-2-yl 1 F-5072 H H H H H 3-Me-5-Cl-pyridin-2-yl 1 F-5073 H H H H H 3-Me-6-Cl-pyridin-2-yl 1 F-5074 H H H H H 3,4-(Me).sub.2-pyridin-2-yl 1 F-5075 H H H H H 3,5-(Me).sub.2-pyridin-2-yl 1 F-5076 H H H H H 3,6-(Me).sub.2-pyridin-2-yl 1 F-5077 H H H H H 3-Me-4-OMe-pyridin-2-yl 1 F-5078 H H H H H 3-Me-5-OMe-pyridin-2-yl 1 F-5079 H H H H H 3-Me-6-OMe-pyridin-2-yl 1 F-5080 H H H H H 3-CF.sub.3-4-F-pyridin-2-yl 1 F-5081 H H H H H 3-CF.sub.3-5-F-pyridin-2-yl 1 F-5082 H H H H H 3-CF.sub.3-6-F-pyridin-2-yl 1 F-5083 H H H H H 3-CF.sub.3-4-Me-pyridin-2-yl 1 F-5084 H H H H H 3-CF.sub.3-5-Me-pyridin-2-yl 1 F-5085 H H H H H 3-CF.sub.3-6-Me-pyridin-2-yl 1 F-5086 H H H H H 3-OMe-4-F-pyridin-2-yl 1 F-5087 H H H H H 3-OMe-5-F-pyridin-2-yl 1 F-5088 H H H H H 3-OMe-6-F-pyridin-2-yl 1 F-5089 H H H H H 3-OMe-4-Cl-pyridin-2-yl 1 F-5090 H H H H H 3-OMe-5-Cl-pyridin-2-yl 1 F-5091 H H H H H 3-OMe-6-Cl-pyridin-2-yl 1 F-5092 H H H H H 3-OMe-4-Me-pyridin-2-yl 1 F-5093 H H H H H 3-OMe-5-Me-pyridin-2-yl 1 F-5094 H H H H H 3-OMe-6-Me-pyridin-2-yl 1 F-5095 H H H H H 3,4-(OMe).sub.2-pyridin-2-yl 1 F-5096 H H H H H 3,5-(OMe).sub.2-pyridin-2-yl 1 F-5097 H H H H H 3,6-(OMe).sub.2-pyridin-2-yl 1 F-5098 H H H H H pyridin-3-yl 1 F-5099 H H H H H 2-F-pyridin-3-yl 1 F-5100 H H H H H 4-F-pyridin-3-yl 1 F-5101 H H H H H 5-F-pyridin-3-yl 1 F-5102 H H H H H 6-F-pyridin-3-yl 1 F-5103 H H H H H 2-Cl-pyridin-3-yl 1 F-5104 H H H H H 4-Cl-pyridin-3-yl 1 F-5105 H H H H H 5-Cl-pyridin-3-yl 1 F-5106 H H H H H 6-Cl-pyridin-3-yl 1 F-5107 H H H H H 2-Me-pyridin-3-yl 1 F-5108 H H H H H 4-Me-pyridin-3-yl 1 F-5109 H H H H H 5-Me-pyridin-3-yl 1
(409) TABLE-US-00308 TABLE 308 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-5110 H H H H H 6-Me-pyridin-3-yl 1 F-5111 H H H H H 2-CF.sub.3-pyridin-3-yl 1 F-5112 H H H H H 4-CF.sub.3-pyridin-3-yl 1 F-5113 H H H H H 5-CF.sub.3-pyridin-3-yl 1 F-5114 H H H H H 6-CF.sub.3-pyridn-3-yl 1 F-5115 H H H H H 2-OMe-pyridin-3-yl 1 F-5116 H H H H H 4-OMe-pyridin-3-yl 1 F-5117 H H H H H 5-OMe-pyridn-3-yl 1 F-5118 H H H H H 6-OMe-pyridn-3-yl 1 F-5119 H H H H H 2,4-F.sub.2-pyridin-3-yl 1 F-5120 H H H H H 2,5-F.sub.2-pyridin-3-yl 1 F-5121 H H H H H 2,6-F.sub.2-pyridin-3-yl 1 F-5122 H H H H H 4,5-F.sub.2-pyridin-3-yl 1 F-5123 H H H H H 4,6-F.sub.2-pyridin-3-yl 1 F-5124 H H H H H 2,4-Cl.sub.2-pyridin-3-yl 1 F-5125 H H H H H 2,5-Cl.sub.2-pyridin-3-yl 1 F-5126 H H H H H 2,6-Cl.sub.2-pyridin-3-yl 1 F-5127 H H H H H 4,5-Cl.sub.2-pyridin-3-yl 1 F-5128 H H H H H 4,6-Cl.sub.2-pyridin-3-yl 1 F-5129 H H H H H 2-F-4-Cl-pyridin-3-yl 1 F-5130 H H H H H 2-F-5-Cl-pyridin-3-yl 1 F-5131 H H H H H 2-F-6-Cl-pyridin-3-yl 1 F-5132 H H H H H 4-F-2-Cl-pyridin-3-yl 1 F-5133 H H H H H 4-F-5-Cl-pyridin-3-yl 1 F-5134 H H H H H 4-F-6-Cl-pyridin-3-yl 1 F-5135 H H H H H 2-F-4-Me-pyridin-3-yl 1 F-5136 H H H H H 2-F-5-Me-pyridin-3-yl 1 F-5137 H H H H H 2-F-6-Me-pyridin-3-yl 1 F-5138 H H H H H 4-F-2-Me-pyridin-3-yl 1 F-5139 H H H H H 4-F-5-Me-pyridin-3-yl 1 F-5140 H H H H H 4-F-6-Me-pyridin-3-yl 1 F-5141 H H H H H 2-F-4-OMe-pyridin-3-yl 1 F-5142 H H H H H 2-F-5-OMe-pyridin-3-yl 1 F-5143 H H H H H 2-F-6-OMe-pyridin-3-yl 1 F-5144 H H H H H 4-F-2-OMe-pyridin-3-yl 1 F-5145 H H H H H 4-F-5-OMe-pyridin-3-yl 1 F-5146 H H H H H 4-F-6-OMe-pyridin-3-yl 1 F-5147 H H H H H 2-Cl-5-F-pyridin-3-yl 1 F-5148 H H H H H 2-Cl-6-F-pyridin-3-yl 1 F-5149 H H H H H 4-Cl-5F-pyridin-3-yl 1 F-5150 H H H H H 4-Cl-6-F-pyridin-3-yl 1 F-5151 H H H H H 2-Cl-4-Me-pyridin-3-yl 1 F-5152 H H H H H 2-Cl-5-Me-pyridin-3-yl 1 F-5153 H H H H H 2-Cl-6-Me-pyridin-3-yl 1 F-5154 H H H H H 4-Cl-2-Me-pyridin-3-yl 1 F-5155 H H H H H 4-Cl-5-Me-pyridin-3-yl 1 F-5156 H H H H H 4-Cl-6-Me-pyridin-3-yl 1 F-5157 H H H H H 2-Me-5-F-pyridin-3-yl 1 F-5158 H H H H H 2-Me-6-F-pyridin-3-yl 1 F-5159 H H H H H 4-Me-5-F-pyridin-3-yl 1 F-5160 H H H H H 4-Me-6-F-pyridin-3-yl 1 F-5161 H H H H H 2-Me-5-Cl-pyridin-3-yl 1 F-5162 H H H H H 2-Me-6-Cl-pyridin-3-yl 1 F-5163 H H H H H 4-Me-5-Cl-pyridn-3-yl 1 F-5164 H H H H H 4-Me-6-Cl-pyridin-3-yl 1 F-5165 H H H H H 2,4-(Me).sub.2-pyridin-3-yl 1 F-5166 H H H H H 2,5-(Me).sub.2-pyridin-3-yl 1
(410) TABLE-US-00309 TABLE 309 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-5167 H H H H H 2,6-(Me).sub.2-pyridin-3-yl 1 F-5168 H H H H H 4,5-(Me).sub.2-pyridin-3-yl 1 F-5169 H H H H H 4,6-(Me).sub.2-pyridin-3-yl 1 F-5170 H H H H H 2-Me-4-OMe-pyridin-3-yl 1 F-5171 H H H H H 2-Me-5-OMe-pyridin-3-yl 1 F-5172 H H H H H 2-Me-6-OMe-pyridin-3-yl 1 F-5173 H H H H H 4-Me-2-OMe-pyridin-3-yl 1 F-5174 H H H H H 4-Me-5-OMe-pyridin-3-yl 1 F-5175 H H H H H 4-Me-6-OMe-pyridin-3-yl 1 F-5176 H H H H H 2-CF.sub.3-4-F-pyridin-3-yl 1 F-5177 H H H H H 2-CF.sub.3-5-F-pyridin-3-yl 1 F-5178 H H H H H 2-CF.sub.3-6-F-pyridin-3-yl 1 F-5179 H H H H H 4-CF.sub.3-2-Fpyridin-3-yl 1 F-5180 H H H H H 4-CF.sub.3-5-F-pyridin-3-yl 1 F-5181 H H H H H 4-CF.sub.3-6-F-pyridin-3-yl 1 F-5182 H H H H H 2-CF.sub.3-4-Me-pyridin-3-yl 1 F-5183 H H H H H 2-CF.sub.3-5-Me-pyridin-3-yl 1 F-5184 H H H H H 2-CF.sub.3-6-Me-pyridin-3-yl 1 F-5185 H H H H H 4-CF.sub.3-2-Me-pyridin-3-yl 1 F-5186 H H H H H 4-CF.sub.3-5-Me-pyridin-3-yl 1 F-5187 H H H H H 4-CF.sub.3-6Me-pyridin-3-yl 1 F-5188 H H H H H 2-OMe-5-F-pyridin-3-yl 1 F-5189 H H H H H 2-OMe-6-F-pyridin-3-yl 1 F-5190 H H H H H 4-OMe-5-F-pyridin-3-yl 1 F-5191 H H H H H 4-OMe-6-F-pyridin-3-yl 1 F-5192 H H H H H 2-OMe-4-Cl-pyridin-3-yl 1 F-5193 H H H H H 2-OMe-5-Cl-pyridin-3-yl 1 F-5194 H H H H H 2-OMe-6-Cl-pyridin-3-yl 1 F-5195 H H H H H 4-OMe-2-Cl-pyridin-3-yl 1 F-5196 H H H H H 4-OMe-5-Cl-pyridin-3-yl 1 F-5197 H H H H H 4-OMe-6-Cl-pyridin-3-yl 1 F-5198 H H H H H 2-OMe-5-Me-pyridin-3-yl 1 F-5199 H H H H H 2-OMe-6-Me-pyridin-3-yl 1 F-5200 H H H H H 4-OMe-5-Me-pyridin-3-yl 1 F-5201 H H H H H 4-OMe-6-Me-pyridin-3-yl 1 F-5202 H H H H H 2,4-(OMe).sub.2-pyridin-3-yl 1 F-5203 H H H H H 2,5-(OMe).sub.2-pyridin-3-yl 1 F-5204 H H H H H 2,6-(OMe).sub.2-pyridin-3-yl 1 F-5205 H H H H H 4,5-(OMe).sub.2-pyridin-3-yl 1 F-5206 H H H H H 4,6-(OMe).sub.2-pyridin-3-yl 1 F-5207 H H H H H pyridin-4-yl 1 F-5208 H H H H H 2-F-pyridin-4-yl 1 F-5209 H H H H H 3-F-pyridin-4-yl 1 F-5210 H H H H H 2-Cl-pyridin-4-yl 1 F-5211 H H H H H 3-Cl-pyridin-4-yl 1 F-5212 H H H H H 2-Me-pyridin-4-yl 1 F-5213 H H H H H 3-Me-pyridn-4-yl 1 F-5214 H H H H H 2-CF.sub.3-pyridin-4-yl 1 F-5215 H H H H H 3-CF.sub.3-pyridin-4-yl 1 F-5216 H H H H H 2-OMe-pyridin-4-yl 1 F-5217 H H H H H 3-OMe-pyridin-4-yl 1 F-5218 H H H H H 2,3-F.sub.2-pyridin-4-yl 1 F-5219 H H H H H 2,5-F.sub.2-pyridin-4-yl 1 F-5220 H H H H H 2,6-F.sub.2-pyridin-4-yl 1 F-5221 H H H H H 3,5-F.sub.2-pyridin-4-yl 1 F-5222 H H H H H 2,3-Cl.sub.2-pyridin-4-yl 1 F-5223 H H H H H 2,5-Cl.sub.2-pyridin-4-yl 1
(411) TABLE-US-00310 TABLE 310 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-5224 H H H H H 2,6-Cl.sub.2-pyridin-4-yl 1 F-5225 H H H H H 3,5-Cl.sub.2-pyridin-4-yl 1 F-5226 H H H H H 3-F-2-Cl-pyridin-4-yl 1 F-5227 H H H H H 3-F-5-Cl-pyridin-4-yl 1 F-5228 H H H H H 3-F-6-Cl-pyridin-4-yl 1 F-5229 H H H H H 3-F-2-Me-pyridin-4-yl 1 F-5230 H H H H H 3-F-5-Me-pyridin-4-yl 1 F-5231 H H H H H 3-F-6-Me-pyridin-4-yl 1 F-5232 H H H H H 3-F-2-OMe-pyridin-4-yl 1 F-5233 H H H H H 3-F-5-OMe-pyridin-4-yl 1 F-5234 H H H H H 3-F-6-OMe-pyridin-4-yl 1 F-5235 H H H H H 3-Cl-2-F-pyridin-4-yl 1 F-5236 H H H H H 3-Cl-6-F-pyridin-4-yl 1 F-5237 H H H H H 3-Cl-2-Me-pyridin-4-y 1 F-5238 H H H H H 3-Cl-5-Me-pyridn-4-yl 1 F-5239 H H H H H 3-Cl-6-Me-pyridin-4-yl 1 F-5240 H H H H H 3-Me-2-F-pyridin-4-yl 1 F-5241 H H H H H 3-Me-6-F-pyridin-4-yl 1 F-5242 H H H H H 3-Me-2-Cl-pyridin-4-yl 1 F-5243 H H H H H 3-Me-6-Cl-pyridn-4-yl 1 F-5244 H H H H H 2,3-(Me).sub.2-pyridin-4-yl 1 F-5245 H H H H H 3,5-(Me).sub.2-pyridin-4-yl 1 F-5246 H H H H H 3,6-(Me).sub.2-pyridin-4-yl 1 F-5247 H H H H H 3-Me-2-OMe-pyridin-4-yl 1 F-5248 H H H H H 3-Me-5-OMe-pyridin-4-yl 1 F-5249 H H H H H 3-Me-6-OMe-pyridin-4-yl 1 F-5250 H H H H H 3-CF.sub.3-2-F-pyridin-4-yl 1 F-5251 H H H H H 3-CF.sub.3-5-F-pyridin-4-yl 1 F-5252 H H H H H 3-CF.sub.3-6-F-pyridin-4-yl 1 F-5253 H H H H H 3-CF.sub.3-2-Me-pyridin-4-yl 1 F-5254 H H H H H 3-CF.sub.3-5-Me-pyridin-4-yl 1 F-5255 H H H H H 3-CF.sub.3-6-Me-pyridin-4-yl 1 F-5256 H H H H H 3-OMe-2-F-pyridin-4-yl 1 F-5257 H H H H H 3-OMe-6-F-pyridin-4-yl 1 F-5258 H H H H H 3-OMe-2-Cl-pyridin-4-yl 1 F-5259 H H H H H 3-OMe-5-Cl-pyridin-4-yl 1 F-5260 H H H H H 3-OMe-6-Cl-pyridin-4-yl 1 F-5261 H H H H H 3-OMe-2-Me-pyridin-4-yl 1 F-5262 H H H H H 3-OMe-6-Me-pyridin-4-yl 1 F-5263 H H H H H 2,3-(OMe).sub.2-pyridin-4-yl 1 F-5264 H H H H H 3,5-(OMe).sub.2-pyridin-4-yl 1 F-5265 H H H H H 3,6-(OMe).sub.2-pyridin-4-yl 1 F-5266 H H H H H pyrimidin-2-yl 1 F-5267 H H H H H pyrimidin-4-yl 1 F-5268 H H H H H 5-F-pyrimidin-4-yl 1 F-5269 H H H H H 5-Me-pyrimidin-4-yl 1 F-5270 H H H H H 5-CF.sub.3-pyrimidin-4-yl 1 F-5271 H H H H H 5-OMe-pyrimidin-4-yl 1 F-5272 H H H H H pyrimidin-5-yl 1 F-5273 H H H H H 4-F-pyrimidin-5-yl 1 F-5274 H H H H H 4-Cl-pyrimidin-5-yl 1 F-5275 H H H H H 4-Me-pyrimidin-5-yl 1 F-5276 H H H H H 4-CF.sub.3-pyrimidin-5-yl 1 F-5277 H H H H H 4-OMe-pyrimidin-5-yl 1 F-5278 H H H H H pyridazin-3-yl 1 F-5279 H H H H H 4-F-pyridazin-3-yl 1 F-5280 H H H H H 4-Cl-pyridazin-3-yl 1
(412) TABLE-US-00311 TABLE 311 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-5281 H H H H H 4-Me-pyridazin-3-yl 1 F-5282 H H H H H 4-CF.sub.3-pyridazin-3-yl 1 F-5283 H H H H H 4-OMe-pyridazin-3-yl 1 F-5284 H H H H H pyridazin-4-yl 1 F-5285 H H H H H 3-F-pyridazin-4-yl 1 F-5286 H H H H H 3-Cl-pyridazin-4-yl 1 F-5287 H H H H H 3-Me-pyridazin-4-yl 1 F-5288 H H H H H 3-CF.sub.3-pyridazin-4-yl 1 F-5289 H H H H H 3-OMe-pyridazin-4-yl 1 F-5290 H H H H H 5-F-pyridazin-4-yl 1 F-5291 H H H H H 5-Cl-pyridazin-4-yl 1 F-5292 H H H H H 5-Me-pyridazin-4-yl 1 F-5293 H H H H H 5-CF.sub.3-pyridazin-4-y 1 F-5294 H H H H H 5-OMe-pyridazin-4-yl 1 F-5295 H H H H H thiophen-2-yl 1 F-5296 H H H H H 3-F-thiophen-2-yl 1 F-5297 H H H H H 3-Cl-thiophen-2-yl 1 F-5298 H H H H H 3-Me-thiophen-2-yl 1 F-5299 H H H H H 3-CF.sub.3-thiophen-2-yl 1 F-5300 H H H H H 3-OMe-thiophen-2-yl 1 F-5301 H H H H H thiophen-3-yl 1 F-5302 H H H H H 2-F-thiophen-3-yl 1 F-5303 H H H H H 2-Cl-thiophen-3-yl 1 F-5304 H H H H H 2-Me-thiophen-3-yl 1 F-5305 H H H H H 2-CF.sub.3-thiophen-3-yl 1 F-5306 H H H H H 2-OMe-thiophen-3-yl 1 F-5307 H H H H H 4-F-thiophen-3-yl 1 F-5308 H H H H H 4-Cl-thiophen-3-yl 1 F-5309 H H H H H 4-Me-thiophen-3-yl 1 F-5310 H H H H H 4-CF.sub.3-thiophen-3-yl 1 F-5311 H H H H H 4-OMe-thiophen-3-yl 1 F-5312 H H H H H thiazol-2-yl 1 F-5313 H H H H H thiazol-4-yl 1 F-5314 H H H H H 5-F-thiazol-4-yl 1 F-5315 H H H H H 5-Me-thiazol-4-yl 1 F-5316 H H H H H 5-CF.sub.3-thiazol-4-yl 1 F-5317 H H H H H 5-OMe-thiazol-4-yl 1 F-5318 H H H H H thiazol-5-yl 1 F-5319 H H H H H 4-F-thiazol-5-yl 1 F-5320 H H H H H 4-Me-thiazol-5-yl 1 F-5321 H H H H H 4-CF.sub.3-thiazol-5-yl 1 F-5322 H H H H H 4-OMe-thiazol-5-yl 1 F-5323 H H H H H 1H-pyrrol-1-yl 1 F-5324 H H H H H 2-F-1H-pyrrol-1-yl 1 F-5325 H H H H H 2-Me-1H-pyrrol-1-yl 1 F-5326 H H H H H 2-CF.sub.3-1H-pyrrol-1-yl 1 F-5327 H H H H H 2-OMe-1H-pyrrol-1-yl 1 F-5328 H H H H H 1H-pyrrol-2-yl 1 F-5329 H H H H H 1-Me-1H-pyrrol-2-yl 1 F-5330 H H H H H 3-F-1H-pyrrol-2-yl 1 F-5331 H H H H H 3-Me-1H-pyrrol-2-yl 1 F-5332 H H H H H 3-CF.sub.3-1H-pyrrol-2-yl 1 F-5333 H H H H H 3-OMe-1H-pyrrol-2-yl 1 F-5334 H H H H H 1-Me-3-F-1H-pyrrol-2-yl 1 F-5335 H H H H H 1,3-(Me).sub.2-1H-pyrro-2-yl 1 F-5336 H H H H H 1-Me-3-CF.sub.3-1H-pyrrol-2-yl 1 F-5337 H H H H H 1-Me-3-OMe-1H-pyrrol-2-yl 1
(413) TABLE-US-00312 TABLE 312 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-5338 H H H H H 1H-pyrrol-3-yl 1 F-5339 H H H H H 1-Me-1H-pyrrol-3-yl 1 F-5340 H H H H H 2-F-1H-pyrrol-3-yl 1 F-5341 H H H H H 2-Me-1H-pyrrol-3-yl 1 F-5342 H H H H H 2-CF.sub.3-1H-pyrrol-3-yl 1 F-5343 H H H H H 2-OMe-1H-pyrrol-3-yl 1 F-5344 H H H H H 1-Me-2-F-1H-pyrrol-3-yl 1 F-5345 H H H H H 1,2-(Me).sub.2-1H-pyrrol-3-yl 1 F-5346 H H H H H 1-Me-2-CF.sub.3-1H-pyrrol-3-yl 1 F-5347 H H H H H 1-Me-2-OMe-1H-pyrrol-3-yl 1 F-5348 H H H H H 4-F-1H-pyrrol-3-yl 1 F-5349 H H H H H 4-Me-1H-pyrrol-3-yl 1 F-5350 H H H H H 4-CF.sub.3-1H-pyrrol-3-yl 1 F-5351 H H H H H 4-OMe-1H-pyrrol-3-yl 1 F-5352 H H H H H 1-Me-4-F-1H-pyrrol-3-yl 1 F-5353 H H H H H 1,4-(Me).sub.2-1H-pyrrol-3-yl 1 F-5354 H H H H H 1-Me-4-CF.sub.3-1H-pyrrol-3-yl 1 F-5355 H H H H H 1-Me-4-OMe-1H-pyrrol-3-yl 1 F-5356 H H H H H 1H-pyrazol-1-yl 1 F-5357 H H H H H 5-F-1H-pyrazol-1-yl 1 F-5358 H H H H H 5-Cl-1H-pyrazol-1-yl 1 F-5359 H H H H H 5-Me-1H-pyrazol-1-yl 1 F-5360 H H H H H 5-CF.sub.3-1H-pyrazol-1-yl 1 F-5361 H H H H H 5-OMe-1H-pyrazol-1-yl 1 F-5362 H H H H H 1H-pyrazol-3-yl 1 F-5363 H H H H H 1-Me-1H-pyrazol-3-yl 1 F-5364 H H H H H 4-F-1H-pyrazol-3-yl 1 F-5365 H H H H H 4-Cl-1H-pyrazol-3-yl 1 F-5366 H H H H H 4-Me-1H-pyrazol-3-yl 1 F-5367 H H H H H 4-CF.sub.3-1H-pyrazol-3-yl 1 F-5368 H H H H H 4-OMe-1H-pyrazol-3-yl 1 F-5369 H H H H H 1-Me-4-F-1H-pyrazol-3-yl 1 F-5370 H H H H H 1-Me-4-Cl-1H-pyrazol-3-yl 1 F-5371 H H H H H 1,4-(Me).sub.2-1H-pyrazol-3-yl 1 F-5372 H H H H H 1-Me-4-CF.sub.3-1H-pyrazol-3-yl 1 F-5373 H H H H H 1-Me-4-OMe-1H-pyrazol-3-yl 1 F-5374 H H H H H 1H-pyrazol-4-yl 1 F-5375 H H H H H 1-Me-1H-pyrazol-4-yl 1 F-5376 H H H H H 3-F-1H-pyrazol-4-yl 1 F-5377 H H H H H 3-Cl-1H-pyrazol-4-yl 1 F-5378 H H H H H 3-Me-1H-pyrazol4-yl 1 F-5379 H H H H H 3-CF.sub.3-1H-pyrazol-4-yl 1 F-5380 H H H H H 3-OMe-1H-pyrazol-4-yl 1 F-5381 H H H H H 1-Me-3-F-1H-pyrazol-4-yl 1 F-5382 H H H H H 1-Me-3-Cl-1H-pyrazol-4-yl 1 F-5383 H H H H H 1,3-(Me).sub.2-1H-pyrazol-4-yl 1 F-5384 H H H H H 1-Me-3-CF.sub.3-1H-pyrazol-4-yl 1 F-5385 H H H H H 1-Me-3-OMe-1H-pyrazol-4-yl 1 F-5386 H H H H H 5-F-1H-pyrazol-4-yl 1 F-5387 H H H H H 5-Cl-1H-pyrazol-4-yl 1 F-5388 H H H H H 5-Me-1H-pyrazol-4-yl 1 F-5389 H H H H H 5-CF.sub.3-1H-pyrazol-4-yl 1 F-5390 H H H H H 5-OMe-1H-pyrazol-4-yl 1 F-5391 H H H H H 1-Me-5-F-1H-pyrazol-4-yl 1 F-5392 H H H H H 1-Me-5-Cl-1H-pyrazol-4-yl 1 F-5393 H H H H H 1,5-(Me).sub.2-1H-pyrazol-4-yl 1 F-5394 H H H H H 1-Me-5-CF.sub.3-1H-pyrazol4-yl 1
(414) TABLE-US-00313 TABLE 313 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-5395 H H H H H 1-Me-5-OMe-1H-pyrazol-4-yl 1 F-5396 H H H H H 1H-pyrazol-5-yl 1 F-5397 H H H H H 1-Me-1H-pyrazol-5-yl 1 F-5398 H H H H H 4-F-1H-pyrazol-5-yl 1 F-5399 H H H H H 4-Cl-1H-pyrazol-5-yl 1 F-5400 H H H H H 4-Me-1H-pyrazol-5-yl 1 F-5401 H H H H H 4-CF.sub.3-1H-pyrazol5-yl 1 F-5402 H H H H H 4-OMe-1H-pyrazol-5-yl 1 F-5403 H H H H H 1-Me-4-F-1H-pyrazol-5-yl 1 F-5404 H H H H H 1-Me-4-Cl-1H-pyrazol-5-yl 1 F-5405 H H H H H 1,4-(Me).sub.2-1H-pyrazol-5-yl 1 F-5406 H H H H H 1-Me-4-CF.sub.3-1H-pyrazol-5-yl 1 F-5407 H H H H H 1-Me-4-OMe-1H-pyrazol-5-yl 1 F-5408 H H H H H furan-2-yl 1 F-5409 H H H H H 3-F-furan-2-yl 1 F-5410 H H H H H 3-Me-furan-2-yl 1 F-5411 H H H H H 3-CF.sub.3-furan-2-yl 1 F-5412 H H H H H 3-OMe-furan-2-yl 1 F-5413 H H H H H furan-3-yl 1 F-5414 H H H H H 2-F-furan-3-yl 1 F-5415 H H H H H 2-Me-furan-3-yl 1 F-5416 H H H H H 2-CF.sub.3-furan-3-yl 1 F-5417 H H H H H 2-OMe-furan-3-yl 1 F-5418 H H H H H 4-F-furan-3-yl 1 F-5419 H H H H H 4-Me-furan-3-yl 1 F-5420 H H H H H 4-CF.sub.3-furan-3-yl 1 F-5421 H H H H H 4-OMe-furan-3-yl 1 F-5422 H H H H H isoxazol-3-yl 1 F-5423 H H H H H 4-F-isoxazol-3-yl 1 F-5424 H H H H H 4-Me-isoxazol-3-yl 1 F-5425 H H H H H 4-CF.sub.3-isoxazol-3-yl 1 F-5426 H H H H H 4-OMe-isoxazol-3-yl 1 F-5427 H H H H H isoxazol-4-yl 1 F-5428 H H H H H 5-F-isoxazol-4-yl 1 F-5429 H H H H H 5-Me-isoxazol-4-yl 1 F-5430 H H H H H 5-CF.sub.3-isoxazol-4-yl 1 F-5431 H H H H H 5-OMe-isoxazol-4-yl 1 F-5432 H H H H H isoxazol-5-yl 1 F-5433 H H H H H 4-F-isoxazol-5-yl 1 F-5434 H H H H H 4-Me-isoxazol-5-yl 1 F-5435 H H H H H 4-CF.sub.3-isoxazol-5-yl 1 F-5436 H H H H H 4-OMe-isoxazol-5-yl 1 F-5437 H H H H H 1H-1,2,3-triazol-1-yl 1 F-5438 H H H H H 5-F-1H-1,2,3-triazol-1-yl 1 F-5439 H H H H H 5-Me-1H-1,2,3-triazol-1-yl 1 F-5440 H H H H H 5-CF.sub.3-1H-1,2,3-triazol-1-yl 1 F-5441 H H H H H 5-OMe-1H-1,2,3-triazol-1-yl 1 F-5442 H H H H H 1H-1,2,3-triazol-4-yl 1 F-5443 H H H H H 5-F-1H-1,2,3-triazol-4-yl 1 F-5444 H H H H H 5-Me-1H-1,2,3-triazol-4-yl 1 F-5445 H H H H H 5-CF.sub.3-1H-1,2,3-triazol-4-yl 1 F-5446 H H H H H 5-OMe-1H-1,2,3-triazol-4-yl 1 F-5447 H H H H H 1H-1,2,3-triazol-5-yl 1 F-5448 H H H H H 4-F-1H-1,2,3-triazol-5-yl 1 F-5449 H H H H H 4-Me-1H-1,2,3-triazol-5-yl 1 F-5450 H H H H H 4-CF.sub.3-1H-1,2,3-triazol-5-yl 1 F-5451 H H H H H 4-OMe-1H-1,2,3-triazol-5-yl 1
(415) TABLE-US-00314 TABLE 314 compound R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 Q p F-5452 H H H H H 1H-1,2,4-triazol-1-yl 1 F-5453 H H H H H 5-Me-1H-1,2,4-triazol-1-yl 1 F-5454 H H H H H 5-F-1H-1,2,4-triazol-1-yl 1 F-5455 H H H H H 5-CF.sub.3-1H-1,2,4-triazol-1-yl 1 F-5456 H H H H H 5-OMe-1H-1,2,4-triazol-1-yl 1 F-5457 H H H H H 1H-1,2,4-triazol-3-yl 1 F-5458 H H H H H 1-Me-1H-1,2,4-triazol-3-yl 1 F-5459 H H H H H 1H-1,2,4-triazol-5-yl 1 F-5460 H H H H H 1-Me-1H-1,2,4-triazol-5-yl 1 F-5461 H H H H H 3,5-(Me).sub.2-isoxazol-4-y 1 F-5462 H H H H H 3,5-(Et).sub.2-isoxazol-4-yl 1 F-5463 H H H H H 1,3,5-(Me).sub.3-1H-pyrazol-4-yl 1 F-5464 H H H H H quinolin-4-yl 1 F-5465 H H H H H isoquinolin-4-yl 1 F-5466 H H H H H 3,6-(OMe).sub.2-pyridazin-4-y 1 F-5467 H H H H H 2,4-(OMe).sub.2-pyrmidin-5-yl 1
(416) On the other hand, the present compound represented by general formula [I] or [II] can be produced in accordance with, but not limited to, the production methods shown below. Hereinafter, for example, compound represented by general formula [I] is synonymous to compound represented by formula [I] and compound [I].
(417) <Production Method 1>
(418) A compound represented by general formula [VI] among the present compounds can be produced, for example, in accordance with the following method.
(419) ##STR00015## (wherein, R.sup.17 represents a C.sub.1-C.sub.6 alkyl group, R.sup.18 represents a C.sub.1-C.sub.6 alkyl group, C.sub.1-C.sub.6 haloalkyl group, di(C.sub.1-C.sub.6 alkyl)amino group, or a phenyl group that is unsubstituted or substituted with (R.sup.9).sub.m, X.sup.1 represents a halogen atom, and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.9 are as defined above.)
(420) That is, the compound represented by general formula [VI] can be produced by reacting compound [III] and compound [IV] or compound [V] in an appropriate solvent in the presence of an appropriate base.
(421) The compound represented by general formula [III] used in the present reaction can be produced by a method described in WO 2012/028332 A, WO 2014/114649 A, WO 2016/027790 A, WO 2016/166250 A, or U.S. Pat. No. 5,055,482, or produced in accordance with such a method.
(422) The use amount of compound [IV] or compound [V] used in the present reaction may be appropriately selected from the range of 1 to 5 mol, and is preferably 1.0 to 2.0 mol, relative to 1 mol of compound [III].
(423) Examples of the solvent that can be used in the present reaction include halogenated hydrocarbons such as dichloromethane, chloroform, 1,2-dichloroethane, or carbon tetrachloride; ethers such as diethylether, tetrahydrofuran, or 1,4-dioxane, 1,2-dimethoxyethane, or methyl tert-butyl ether; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; nitriles such as acetonitrile, or propionitrile; pyridines such as pyridine, or picoline; tertiary amines such as triethylamine, or tributylamine; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 300 liters, preferably 0.3 to 50 liters relative to 1 mol of compound [III].
(424) Examples of the base that can be used in the present reaction include inorganic bases such as hydroxides of alkali metal (e.g. sodium hydroxide or potassium hydroxide); hydroxides of alkali earth metal (e.g. calcium hydroxide or magnesium hydroxide); carbonates of alkali metal (e.g. sodium carbonate or potassium carbonate); bicarbonates of alkali metal (e.g. sodium hydrogen carbonate or potassium hydrogen carbonate); metal hydrides (e.g. sodium hydride or potassium hydride); metal salts of alcohol (e.g. sodium methoxide, sodium ethoxide, or potassium tert-butoxide); or organic bases such as triethylamine, N,N-dimethylaniline, pyridine, 4-N,N-dimethylaminepyridine, 1,8-diazacyclo[5.4.0]-7-undecene, and so on. The use amount of the base may be appropriately selected from the range of 1.0 to 5.0 mol, and is preferably 1.0 to 3.5 mol, relative to 1 mol of compound [III]. The organic bases such as triethylamine or pyridine can also be used as the solvent.
(425) The reaction temperature of the present reaction may be selected from any range of temperature typically from ?70? C. to a reflux temperature in a reaction system, and is preferably in the range of 0? C. to 150? C.
(426) The reaction time of the present reaction is typically 10 minutes to 24 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.
(427) After end of the reaction, water is added to the reaction mixture, and then extraction with an organic solvent is conducted, and then concentration or the like operation is conducted, and thus compound [VI] can be isolated. The isolated compound [VI] can be further purified by column chromatography, recrystallization, or the like as necessary.
(428) <Production Method 2>
(429) A compound represented by general formula [VIII] among the present compounds can be produced, for example, in accordance with the following method.
(430) ##STR00016## (wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.17, and X.sup.1 are as defined above.)
(431) That is, the compound represented by general formula [VIII] can be produced by reacting compound [VII] and a halogenating agent in an appropriate solvent in the presence or absence of an appropriate acid, in the presence or absence of an appropriate oxidizing agent.
(432) The compound represented by general formula [VII] used in the present reaction can be produced by a method described in WO 2008/019357 A or WO 2008/157740 A, or produced in accordance with such a method.
(433) Examples of the halogenating agent used in the present reaction include fluorine, chlorine, bromine, iodine, N-chlorosuccinimide, N-bromosuccinimide, N-iodosuccinimide, sulfuryl chloride, iodine monochloride, tert-butyl hypochlorite, N-fluoro-N-(chloromethyl)-triethylenediaminebis(tetrafluoroborate), 1-fluoro-2,6-dichloropyridinium tetrafluoroborate, or 1,3-dibromo-5,5-dimethylhydantoin. The use amount of the halogenating agent may be appropriately selected from the range of 1.0 to 10 mol, and is preferably 1.0 to 3.0 mol, relative to 1 mol of compound [VII].
(434) Examples of the oxidizing agent that can be used in the present reaction include ammonium hexanitratocerate (IV), hydrogen peroxide, or iodobenzene diacetate. The use amount of the oxidizing agent may be appropriately selected from the range of 0 to 10 mol, and is preferably 0 to 3.0 mol, relative to 1 mol of compound [VII].
(435) Examples of the solvent that can be used in the present reaction include inorganic acids such as sulfuric acid; ethers such as diethylether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or methyl tert-butyl ether; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; halogenated hydrocarbons such as dichloromethane, chloroform, 1,2-dichloroethane, or carbon tetrachloride; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such as methanol, ethanol, 2-propanol, or methyl cellosolve; nitriles such as acetonitrile or propionitrile; carboxylic acids such as acetic acid or trifluoroacetic acid; pyridines such as pyridine or picoline; ketones such as acetone or methyl ethyl ketone; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 100 liters, preferably 0.3 to 10 liters relative to 1 mol of compound [VII].
(436) Examples of the acid that can be used in the present reaction include inorganic acids such as sulfuric acid; or carboxylic acids such as acetic acid or trifluoro acetic acid. The use amount of the acid may be appropriately selected from the range of 1.0 to 10 mol, and is preferably 0 to 3.0 mol, relative to 1 mol of compound [VII]. The acid may be used as the solvent.
(437) The reaction temperature of the present reaction may be selected from any range of temperature from ?60? C. to a reflux temperature in a reaction system, and is preferably in the range of ?20? C. to 100? C.
(438) The reaction time of the present reaction is typically 10 minutes to 24 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.
(439) After end of the reaction, water is added to the reaction mixture, and then extraction with an organic solvent is conducted, and then concentration or the like operation is conducted, and thus compound [VIII] can be isolated. The isolated compound [VIII] can be further purified by column chromatography, recrystallization, or the like as necessary.
(440) <Production Method 3>
(441) A compound represented by general formula [XII] among the compounds of the present invention can be produced, for example, in accordance with the following method.
(442) ##STR00017## (wherein, L represents a halogen atom, C.sub.1-C.sub.6 alkylsulfonyloxy group, C.sub.1-C.sub.6 haloalkylsulfonyloxy group, di(C.sub.1-C.sub.6 alkyl)sulfamoyloxy group, or a phenylsulfonyloxy group that is unsubstituted or substituted with (R.sup.9).sub.m, Q represents a C.sub.6-C.sub.10 aryl group that is unsubstituted or substituted with (R.sup.8).sub.m or a heteroaryl group that is unsubstituted or substituted with (R.sup.8).sub.m, R.sup.19 represents a group OR.sup.16 or a group NR.sup.6R.sup.7, and m, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, and R.sup.16 are as defined above.)
(443) Some of [X] or [XI] used herein are known compounds, part of which are commercially available. The remainder can be easily synthesized according to the method described in literature, for example, in the methods described in Chemical Review, 1995, vol. 95, p. 2457; Journal of Organic Chemistry, 1995, vol. 60, p. 7508; Journal of Organic Chemistry 1997, vol. 62, p. 6458 and so on.
(444) That is, the compound represented by general formula [XII] can be produced by reacting compound [IX] and compound [X] or compound [XI] in an appropriate solvent in the presence of an appropriate catalyst and an appropriate base.
(445) The use amount of compound [X] or compound [XI] used in the present reaction may be appropriately selected from the range of 1.0 to 10 mol, and is preferably 1.0 to 3.0 mol, relative to 1 mol of compound [IX].
(446) Examples of the solvent that can be used in the present reaction include ethers such as diethylether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or methyl tert-butylether; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such as methanol, ethanol, 2-propanol, or methyl cellosolve; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 300 liters, preferably 0.3 to 50 liters relative to 1 mol of compound [IX].
(447) Examples of the catalyst that can be used in the present reaction include palladium catalysts such as palladium-carbon, palladium chloride, palladium acetate, tris(dibenzylideneacetone)dipalladium, bis(dibenzylideneacetone)dipalladium, bis(triphenylphosphine)palladium dichloride, tetrakis(triphenylphosphine)palladium, [1,1-bis(diphenylphosphino)ferrocene]palladium dichloride, or [1,2-bis(diphenylphosphino)ethane]palladium dichloride; or copper catalysts such as metal copper, copper (I) acetate, coper (II) acetate, copper (I) oxide, copper(II) oxide, copper (I) chloride, or copper (I) iodide.
(448) Besides the above, a palladium catalyst prepared from a palladium catalyst and a ligand may be used. Examples of the palladium catalyst include palladium acetate, tris(dibenzylidene acetone)dipalladium, and bis(dibenzylidene acetone)palladium. Examples of the ligand include triphenylphosphine, tri(tert-butyl)phosphine, tricyclohexylphosphine, SPhos, Xantphos, and BINAP.
(449) The use amount of the catalyst may be appropriately selected from the range of 0.001 to 1.0 mol, and is preferably 0.01 to 0.5 mol, relative to 1 mol of compound [IX].
(450) Examples of the base that can be used in the present reaction include organic bases such as pyridine, diisopropylethylamine, or triethylamine; hydroxides of alkali metal such as sodium hydroxide or potassium hydroxide; carbonates of alkali metal such as sodium carbonate, potassium carbonate, or cesium carbonate; bicarbonates of alkali metal such as sodium hydrogen carbonate or potassium hydrogen carbonate; metal salts of alcohol such as sodium methoxide, sodium ethoxide, or potassium tert-butoxide; tripotassium phosphate, potassium fluoride, or cesium fluoride. The use amount of the base may be appropriately selected from the range of 0.1 to 10 mol, and is preferably 1.0 to 5.0 mol, relative to 1 mol of compound [IX].
(451) The reaction temperature of the present reaction may be selected from any range of temperature typically from ?30? C. to a reflux temperature in a reaction system, and is preferably in the range of 0? C. to 150? C.
(452) The reaction time of the present reaction is typically 1 minute to 72 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.
(453) After end of the reaction, water is added to the reaction mixture, and then the precipitated solid is filtered off or extracted with an organic solvent, followed by concentration or the like operation, and thus compound [XII] can be isolated. The isolated compound [XII] can be further purified by column chromatography, recrystallization, or the like as necessary.
(454) <Production Method 4>
(455) A compound represented by general formula [XIV] among the present compounds can be produced, for example, in accordance with the following method.
(456) ##STR00018## (wherein, Q, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.17 are as defined above.)
(457) That is, the compound represented by general formula [XIV] can be produced by hydrolysis of compound [XIII] in an appropriate solvent in the presence of an appropriate base or appropriate acid.
(458) Examples of the base that can be used in the present reaction include inorganic bases such as hydroxides of alkali metal (e.g. sodium hydroxide, potassium hydroxide, lithium hydroxide, or barium hydroxide); carbonates of alkali metal (e.g. sodium carbonate or potassium carbonate); bicarbonates of alkali metal (e.g. sodium hydrogen carbonate or potassium hydrogen carbonate). The use amount of the base may be appropriately selected from the range of 0.1 to 50 mol, and is preferably 0.5 to 20 mol, relative to 1 mol of compound [XIII].
(459) Examples of the acid that can be used in the present reaction include inorganic acids such as hydrochloric acid, hydrobromic acid, or sulfuric acid; or carboxylic acids such as acetic acid or trifluoro acetic acid. The use amount of the acid may be appropriately selected from the range of 1 to 1000 mol, and is preferably 1 to 100 mol, relative to 1 mol of compound [XIII].
(460) Examples of the solvent that can be used in the present reaction include ethers such as diethyl ether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or methyl tert-butyl ether; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such as methanol, ethanol, 2-propanol, or methyl cellosolve; nitriles such as acetonitrile or propionitrile; ketones such as acetone or methylethylketone; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 500 liters, preferably 0.3 to 30 liters relative to 1 mol of compound [XIII].
(461) The reaction temperature of the present reaction may be selected from any range of temperature typically from ?30? C. to a reflux temperature in a reaction system, and is preferably in the range of 0? C. to 150? C.
(462) The reaction time of the present reaction is typically 10 minutes to 72 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.
(463) After end of the reaction, the reaction mixture water is neutralized by adding water, and then the precipitated solid is filtered off or extracted with an organic solvent, followed by concentration or the like operation, and thus compound [XIV] can be isolated. The isolated compound [XIV] can be further purified by column chromatography, recrystallization, or the like as necessary.
(464) <Production Method 5>
(465) A compound represented by general formula [XVII] among the present compounds can also be produced, for example, in accordance with the following method.
(466) ##STR00019## (wherein, Q, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and X.sup.1 are as defined above.)
(467) That is, the compound represented by general formula [XVII] can be produced by (step 1) making compound [XIV] into compound [XV] by using an acid halogenating agent in an appropriate solvent in the presence or absence of an appropriate catalyst, and then (step 2) reacting with compound [XVI] or a salt thereof in an appropriate solvent in the presence or absence of an appropriate base.
(468) (Step 1)
(469) Examples of the acid halogenating agent that can be used in the present reaction include thionyl chloride, oxalyl chloride, or phosphoryl chloride. The use amount of the acid halogenating agent may be appropriately selected from the range of 0.1 to 30 mol, and is preferably 0.5 to 10 mol, relative to 1 mol of compound [XIV].
(470) Examples of the catalyst that can be used in the present reaction include N,N-dimethylformamide. The use amount of the catalyst may be appropriately selected from the range of 0.01 to 1.0 mol, and is preferably 0.01 to 0.1 mol, relative to 1 mol of compound [XIV].
(471) Examples of the solvent that can be used in the present reaction include ethers such as diethylether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or methyl tert-butyl ether; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; halogenated hydrocarbons such as dichloromethane, chloroform, 1,2-dichloroethane, or carbon tetrachloride; nitriles such as acetonitrile or propionitrile; esters such as ethyl acetate, or ethyl propionate; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; or mixed solvents thereof. The use amount of the solvent is 0.1 to 100 liters, preferably 0.3 to 10 liters relative to 1 mol of compound [XIV].
(472) The reaction temperature of the present reaction may be selected from any range of temperature typically from ?30? C. to a reflux temperature in a reaction system, and is preferably in the range of 0? C. to 150? C.
(473) The reaction time of the present reaction is typically 10 minutes to 24 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.
(474) After end of the reaction, compound [XV] can be isolated by conducting concentration or the like operation.
(475) (Step 2)
(476) The use amount of compound [XVI] used in the present reaction may be appropriately selected from the range of typically 1 to 500 mol, and is preferably 1.0 to 300 mol, relative to 1 mol of compound [XV].
(477) Examples of the solvent that can be used in the present reaction include ethers such as diethylether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or methyl tert-butyl ether; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; halogenated hydrocarbons such as dichloromethane, chloroform, 1,2-dichloroethane, or carbon tetrachloride; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such as methanol, ethanol, 2-propanol, or methyl cellosolve; nitriles such as acetonitrile or propionitrile; esters such as ethyl acetate or ethyl propionate; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; pyridines such as pyridine or picoline; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 500 liters, preferably 0.2 to 50 liters relative to 1 mol of compound [XV].
(478) Examples of the base that can be used in the present reaction include inorganic bases such as hydroxides of alkali metal (e.g. sodium hydroxide or potassium hydroxide); hydroxides of alkali earth metal (e.g. calcium hydroxide or magnesium hydroxide); carbonates of alkali metal (e.g. sodium carbonate or potassium carbonate); bicarbonates of alkali metal (e.g. sodium hydrogen carbonate or potassium hydrogen carbonate): metal hydrides (e.g. sodium hydride or potassium hydride); metal salts of alcohol (e.g. sodium methoxide, sodium ethoxide, or potassium tert-butoxide); or organic bases such as triethylamine, N,N-dimethylaniline, pyridine, 4-N,N-dimethylaminepyridine, 1,8-diazacyclo[5.4.0]-7-undecene, and so on. The use amount of the base may be appropriately selected from the range of 0 to 5 mol, and is preferably 0 to 1.2 mol, relative to 1 mol of compound [XV].
(479) The reaction temperature of the present reaction may be selected from any range of temperature typically from ?30? C. to a reflux temperature in a reaction system, and is preferably in the range of 0? C. to 150? C.
(480) The reaction time of the present reaction is typically 10 minutes to 24 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.
(481) After end of the reaction, water is added to the reaction mixture, and then the precipitated solid is filtered off or extracted with an organic solvent, followed by concentration or the like operation, and thus compound [XVII] can be isolated. The isolated compound [XVII] can be further purified by column chromatography, recrystallization, or the like as necessary.
(482) <Production Method 6>
(483) A compound represented by general formula [XVII] among the present compounds can also be produced, for example, in accordance with the following method.
(484) ##STR00020## (wherein, Q, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are as defined above.)
(485) That is, the compound represented by general formula [XVII] can be produced by reacting compound [XIV] and compound [XVI] or a salt thereof in an appropriate solvent in the presence or absence of an appropriate condensing agent and an appropriate base.
(486) The use amount of compound [XVI] or a salt thereof used in the present reaction may be appropriately selected from the range of 1 to 10 mol, and is preferably 1.0 to 3.0 mol, relative to 1 mol of compound [XIV].
(487) Examples of the condensing agent that can be used in the present reaction include 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride, a mixture of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride and 1-hydroxybenzotriazole, 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide, a mixture of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide and 1-hydroxybenzotriazole, N,N-dicyclohexylcarbodiimide, N,N-diisopropylcarbodiimide, N,N-carbonyldiimidazole, 4-(4,6-dimethoxy-1,3,5-triazine-2-yl)-4-methylmorpholinium chloride, 1H-benzotriazole-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate, {{[(1-cyano-2-ethoxy-2-oxoethylidene)amino]oxy}-4-morpholinomethylene}dimethylammonium hexafluorophosphate, or O-(7-azabenzotriazole-1-yl)-N,N,N,N-tetramethyluronium hexafluorophosphate. The use amount of the condensing agent may be appropriately selected from the range of 1.0 to 10 mol, and is preferably 1.0 to 6.0 mol, relative to 1 mol of compound [XIV].
(488) When a base is used in the present reaction, examples of the base that can be used include organic bases such as triethylamine, 4-methylmorpholine, diisopropylethylamine, 1,8-diazabicyclo[5.4.0]-7-undecene, pyridine, or 2,6-lutidine. The use amount of the base may be appropriately selected from the range of 0 to 10 mol, and is preferably 0.1 to 6.0 mol, relative to 1 mol of compound [XIV].
(489) Examples of the solvent that can be used in the present reaction include halogenated hydrocarbons such as dichloromethane, chloroform, or 1,2-dichloroethane, or carbon tetrachloride; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; esters such as ethyl acetate, or ethyl propionate; nitriles such as acetonitrile or propionitrile; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; ethers such as diethylether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or methyl tert-butyl ether; or mixed solvents thereof. The use amount of the solvent is 0.1 to 100 liters, preferably 0.3 to 50 liters relative to 1 mol of compound [XIV].
(490) The present reaction can be conducted in the presence of a catalyst as necessary, and examples of the catalyst include 4-(N,N-dimethyl)aminopyridine. The use amount of the catalyst may be appropriately selected from the range of 0.001 to 10 mol, and is preferably 0.01 to 0.3 mol, relative to 1 mol of compound [XIV].
(491) The reaction temperature of the present reaction may be selected from any range of temperature from ?20? C. to a reflux temperature in a reaction system, and is preferably in the range of 0? C. to 80? C.
(492) The reaction time of the present reaction is typically 1 minute to 48 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.
(493) After end of the reaction, water is added to the reaction mixture, and then the precipitated solid is filtered off or extracted with an organic solvent, followed by concentration or the like operation, and thus compound [XVII] can be isolated. The isolated compound [XVII] can be further purified by column chromatography, recrystallization, or the like as necessary.
(494) <Production Method 7>
(495) A compound represented by general formula [XVII] among the present compounds can be produced, for example, in accordance with the following method.
(496) ##STR00021## (wherein, Q, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.17 are as defined above.)
(497) That is, the compound represented by general formula [XVII] can be produced by reacting the compound represented by general formula [XIII] and the compound represented by general formula [XVI] in an appropriate solvent in the presence or absence of an appropriate base.
(498) The use amount of compound [XVI] used in the present reaction may be appropriately selected from the range of typically 1.0 to 500 mol, and is preferably 1.0 to 300 mol, relative to 1 mol of compound [XIII].
(499) Examples of the solvent that can be used in the present reaction include ethers such as diethylether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or methyl tert-butyl ether; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; halogenated hydrocarbons such as dichloromethane, chloroform, 1,2-dichloroethane, or carbon tetrachloride; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such as methanol, ethanol, 2-propanol, or methyl cellosolve; nitriles such as acetonitrile or propionitrile; esters such as ethyl acetate or ethyl propionate; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; pyridines such as pyridine or picoline; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 500 liters, preferably 0.2 to 50 liters relative to 1 mol of compound [XIII].
(500) Examples of the base that can be used in the present reaction include inorganic bases such as hydroxides of alkali metal (e.g. sodium hydroxide or potassium hydroxide); hydroxides of alkali earth metal (e.g. calcium hydroxide or magnesium hydroxide); carbonates of alkali metal (e.g. sodium carbonate or potassium carbonate); bicarbonates of alkali metal (e.g. sodium hydrogen carbonate or potassium hydrogen carbonate): metal hydrides (e.g. sodium hydride or potassium hydride); metal salts of alcohol (e.g. sodium methoxide, sodium ethoxide, or potassium tert-butoxide); or organic bases such as triethylamine, N,N-dimethylaniline, pyridine, 4-N,N-dimethylaminepyridine, 1,8-diazacyclo[5.4.0]-7-undecene, and so on. The use amount of the base may be appropriately selected from the range of 0 to 5.0 mol, and is preferably 0 to 1.2 mol, relative to 1 mol of compound [XIII].
(501) The reaction temperature of the present reaction may be selected from any range of temperature typically from ?30? C. to a reflux temperature in a reaction system, and is preferably in the range of 0? C. to 150? C.
(502) The reaction time of the present reaction is typically 10 minutes to 1 week although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.
(503) After end of the reaction, water is added to the reaction mixture, and then extraction with an organic solvent is conducted, and then concentration or the like operation is conducted, and thus compound [XVII] can be isolated. The isolated compound [XVII] can be further purified by column chromatography, recrystallization, or the like as necessary.
(504) <Production Method 8>
(505) A compound represented by general formula [XIX] among the present compounds can be produced, for example, in accordance with the following method.
(506) ##STR00022## (wherein, Q, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.19 are as defined above.)
(507) That is, the compound represented by general formula [XIX] can be produced by reacting compound [XVIII] and an appropriate oxidizing agent in an appropriate solvent in the presence or absence of a catalyst.
(508) Examples of the solvent that can be used in the present reaction include halogenated hydrocarbons such as dichloromethane, chloroform, 1,2-dichloroethane, carbon tetrachloride; ethers such as diethylether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or methyl tert-butyl ether; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such as methanol, ethanol, 2-propanol, or methyl cellosolve; ketones such as acetone or methyl ethyl ketone; nitriles such as acetonitrile or propionitrile; acetic acid, water, or mixtures thereof. The use amount of the solvent is 0.1 to 500 liters, preferably 0.3 to 200 liters relative to 1 mol of compound [XVIII].
(509) Examples of the oxidizing agent that can be used in the present reaction include organic peroxides such as m-chloroperbenzoic acid, performic acid, or peracetic acid; and inorganic peroxides such as hydrogen peroxide, potassium permanganate, OXONE (registered tradename available from E. I. du Pont de Nemours and Company, product containing potassium peroxymonosulfate), or sodium periodate. The use amount of the oxidizing agent is 0.5 to 3.0 mol, relative to 1 mol of compound [XVIII].
(510) Examples of the catalyst that can be used in the present reaction include sodium tungstate. The use amount of the catalyst is 0.01 to 0.5 mol, relative to 1 mol of compound [XVIII].
(511) The reaction temperature of the present reaction may be selected from any range of temperature typically from ?30? C. to a reflux temperature in a reaction system, and is preferably in the range of ?10? C. to 100? C.
(512) The reaction time of the present reaction is typically 10 minutes to 48 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.
(513) After end of the reaction, water is added to the reaction mixture, and then extraction with an organic solvent is conducted, and then concentration or the like operation is conducted, and thus compound [XIX] can be isolated. Alternatively, compound [XIX] can also be isolated by concentrating the solvent of the reaction mixture. The isolated compound [XIX] can be further purified by column chromatography, recrystallization, or the like as necessary.
(514) <Production Method 9>
(515) A compound represented by general formula [XX] among the present compounds can be produced, for example, in accordance with the following method.
(516) ##STR00023## (wherein, R.sup.20s, which may be the same or different, each represent a hydrogen atom or C.sub.1-C.sub.6 alkyl, or two R.sup.20s may together form CH.sub.2CH.sub.2 or C(CH.sub.3).sub.2C(CH.sub.3).sub.2, and L, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.19 are as defined above.)
(517) That is, the compound represented by general formula [XX] can be produced by reacting compound [IX] and compound [B(OR.sup.20).sub.2].sub.2 in an appropriate solvent in the presence of an appropriate catalyst and an appropriate base.
(518) The use amount of compound [B(OR.sup.20).sub.2].sub.2 used in the present reaction may be appropriately selected from the range of 1 to 10 mol, and is preferably 1.0 to 3.0 mol, relative to 1 mol of compound [IX].
(519) Examples of the solvent that can be used in the present reaction include ethers such as diethyl ether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or methyl tert-butyl ether; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such as methanol, ethanol, 2-propanol, or methyl cellosolve; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 300 liters, preferably 0.3 to 50 liters relative to 1 mol of compound [IX].
(520) Examples of the catalyst that can be used in the present reaction include palladium catalysts such as palladium-carbon, palladium chloride, palladium acetate, tris(dibenzylideneacetone)dipalladium, bis(dibenzylideneacetone)palladium, bis(triphenylphosphine)palladium dichloride, tetrakis(triphenylphosphine)palladium, [1,1-bis(diphenylphosphino)ferrocene]palladium dichloride, or [1,2-bis(diphenylphosphino)ethane]palladium dichloride; or copper catalysts such as metal copper, copper (I) acetate, coper (II) acetate, copper (I) oxide, copper (II) oxide, copper (I) chloride, or copper (I) iodide.
(521) Besides the above, a palladium catalyst prepared from a palladium catalyst and a ligand may be used. Examples of the palladium catalyst include palladium acetate, tris(dibenzylidene acetone)dipalladium, and bis(dibenzylidene acetone)palladium. Examples of the ligand include triphenylphosphine, tri(tert-butyl)phosphine, tricyclohexylphosphine, SPhos, Xantphos, and BINAP.
(522) The use amount of the catalyst may be appropriately selected from the range of 0.001 to 1.0 mol, and is preferably 0.01 to 0.5 mol, relative to 1 mol of compound [IX].
(523) Examples of the base that can be used in the present reaction include organic bases such as pyridine, diisopropylethylamine, or triethylamine; carbonates of alkali metal such as sodium carbonate, potassium carbonate, or cesium carbonate; bicarbonates of alkali metal such as sodium hydrogen carbonate or potassium hydrogen carbonate; metal salts of alcohol such as sodium methoxide, sodium ethoxide, or potassium tert-butoxide; potassium phosphate, potassium fluoride, cesium fluoride, or potassium acetate. The use amount of the base may be appropriately selected from the range of 0.1 to 10 mol, and is preferably 1.0 to 5.0 mol, relative to 1 mol of compound [IX].
(524) The reaction temperature of the present reaction may be selected from any range of temperature typically from 25? C. to a reflux temperature in a reaction system, and is preferably in the range of 30? C. to 150? C.
(525) The reaction time of the present reaction is typically 1 minute to 72 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.
(526) After end of the reaction, water is added to the reaction mixture, and then the precipitated solid is filtered off or extracted with an organic solvent, followed by concentration or the like operation, and thus compound [XX] can be isolated. The isolated compound [XX] can be further purified by column chromatography, recrystallization, or the like as necessary.
(527) <Production Method 10>
(528) A compound represented by general formula [XII] among the present compounds can be produced, for example, in accordance with the following method.
(529) ##STR00024## (wherein, Q, L, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.19 and R.sup.20 are as defined above.)
(530) That is, the compound represented by general formula [XII] can be produced by reacting compound [XX] and compound [XX] in an appropriate solvent in the presence of an appropriate catalyst and an appropriate base.
(531) The use amount of compound [XX] used in the present reaction may be appropriately selected from the range of 0.3 to 10 mol, and is preferably 0.4 to 3.0 mol, relative to 1 mol of compound [XX].
(532) Examples of the solvent that can be used in the present reaction include ethers such as diethyl ether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or methyltert-butyl ether; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such as methanol, ethanol, 2-propanol, or methyl cellosolve; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 300 liters, preferably 0.3 to 50 liters relative to 1 mol of compound [XX].
(533) Examples of the catalyst that can be used in the present reaction include palladium catalysts such as palladium-carbon, palladium chloride, palladium acetate, tris(dibenzylideneacetone)dipalladium, bis(dibenzylideneacetone)palladium, bis(triphenylphosphine)palladium dichloride, tetrakis(triphenylphosphine)palladium, [1,1-bis(diphenylphosphino)ferrocene]palladium dichloride, or [1,2-bis(diphenylphosphino)ethane]palladium dichloride; or copper catalysts such as metal copper, copper (I) acetate, coper (II) acetate, copper (I) oxide, copper (II) oxide, copper (I) chloride, or copper (I) iodide.
(534) Besides the above, a palladium catalyst prepared from a palladium catalyst and a ligand may be used. Examples of the palladium catalyst include palladium acetate, tris(dibenzylidene acetone)dipalladium, and bis(dibenzylidene acetone)palladium. Examples of the ligand include triphenylphosphine, tri(tert-butyl)phosphine, tricyclohexylphosphine, SPhos, Xantphos, and BINAP.
(535) The use amount of the catalyst may be appropriately selected from the range of 0.001 to 1.0 mol, and is preferably 0.01 to 0.5 mol, relative to 1 mol of compound [XX].
(536) Examples of the base that can be used in the present reaction include organic bases such as pyridine, diisopropylethylamine, or triethylamine; hydroxides of alkali metal such as sodium hydroxide or potassium hydroxide; carbonates of alkali metal such as sodium carbonate, potassium carbonate, or cesium carbonate; bicarbonates of alkali metal such as sodium hydrogen carbonate or potassium hydrogen carbonate; metal salts of alcohol such as sodium methoxide, sodium ethoxide, or potassium tert-butoxide; potassium phosphate, potassium fluoride, or cesium fluoride. The use amount of the base may be appropriately selected from the range of 0.1 to 10 mol, and is preferably 1.0 to 5.0 mol, relative to 1 mol of compound [XX].
(537) The reaction temperature of the present reaction may be selected from any range of temperature typically from ?30? C. to a reflux temperature in a reaction system, and is preferably in the range of 0? C. to 150? C.
(538) The reaction time of the present reaction is typically 1 minute to 72 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.
(539) After end of the reaction, water is added to the reaction mixture, and then the precipitated solid is filtered off or extracted with an organic solvent, followed by concentration or the like operation, and thus compound [XII] can be isolated. The isolated compound [XII] can be further purified by column chromatography, recrystallization, or the like as necessary.
(540) <Production Method 11>
(541) A compound represented by general formula [XXII] among the present compounds can be produced, for example, by using a compound represented by general formula [XVII] in accordance with the following method.
(542) ##STR00025## (wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and Q are as defined above.)
(543) That is, the compound represented by general formula [XXII] can be produced by reacting compound [XVII] with an appropriate sulphidizing agent.
(544) Examples of the solvent that can be used in the present reaction include ethers such as diethyl ether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or methyltert-butyl ether; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; halogenated hydrocarbons such as dichloromethane, chloroform, 1,2-dichloroethane, or carbon tetrachloride; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 300 liters, preferably 0.3 to 50 liters relative to 1 mol of compound [XVII].
(545) Examples of the sulphidizing agent that can be used in the present reaction include phosphorus pentasulfide, or Lawesson's reagent. The use amount of the sulphidizing agent may be appropriately selected from the range of 0.5 to 30 mol, and is preferably 0.5 to 5 mol, relative to 1 mol of compound [XVII].
(546) The reaction temperature of the present reaction may be selected from any range of temperature typically from ?70? C. to a reflux temperature in a reaction system, and is preferably in the range of 0? C. to 150? C.
(547) The reaction time of the present reaction is typically 10 minutes to 24 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.
(548) After end of the reaction, water is added to the reaction mixture, and then extraction with an organic solvent is conducted, and then concentration or the like operation is conducted, and thus compound [XXII] can be isolated. Alternatively, compound [XXII] can also be isolated by concentrating the solvent of the reaction mixture. The isolated compound [XXII] can be further purified by column chromatography, recrystallization, or the like as necessary.
(549) <Production Method 12>
(550) A compound represented by general formula [XXVI] among the present compounds can be produced, for example, by using a compound represented by general formula [XXIII] in accordance with the following method.
(551) ##STR00026## (wherein, R.sup.21 represents a C.sub.1-C.sub.6 alkoxy group, amino group, mono(C.sub.1-C.sub.6 alkyl)amino group, di(C.sub.1-C.sub.6 alkyl)amino group, C.sub.1-C.sub.6 alkylthio group, or C.sub.1-C.sub.6 alkoxy C.sub.1-C.sub.6 alkoxy group, and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Q are as defined above.)
(552) That is, the compound represented by general formula [XXVI] can be produced by (step 1) making compound [XXIII] into compound [XXIV] by using oxalyl chloride in an appropriate solvent or in the absence of a solvent, and then (step 2) reacting with compound [XXV] or a salt thereof in an appropriate solvent or in the absence of a solvent.
(553) (Step 1)
(554) The use amount of oxalyl chloride may be appropriately selected from the range of 1.0 to 1000 mol, and is preferably 1.0 to 300 mol, relative to 1 mol of compound [XXIII].
(555) Examples of the solvent that can be used in the present reaction include ethers such as diethyl ether, tetrahydrofuran, methyltert-butyl ether, or 1,4-dioxane; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; halogenated hydrocarbons such as dichloromethane, chloroform, 1,2-dichloroethane, or carbon tetrachloride; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; nitriles such as acetonitrile or propionitrile; esters such as ethyl acetate or ethyl propionate, or mixed solvents thereof. The use amount of the solvent is 0.1 to 500 liters, preferably 0.2 to 50 liters relative to 1 mol of compound [XXIII].
(556) The reaction temperature of the present reaction may be selected from any range of temperature typically from 0? C. to a reflux temperature in a reaction system, and is preferably in the range of 20? C. to 90? C.
(557) The reaction time of the present reaction is typically 1 minute to 6 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.
(558) After end of the reaction, compound [XXIV] can be isolated by conducting concentration or the like operation.
(559) (Step 2)
(560) The use amount of compound [XXV] used in the present reaction may be appropriately selected from the range of typically 1.0 to 500 mol, and is preferably 1.0 to 300 mol, relative to 1 mol of compound [XXIV].
(561) Examples of the solvent that can be used in the present reaction include ethers such as diethyl ether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or methyl tert-butyl ether; halogenated hydrocarbons such as dichloromethane, chloroform, 1,2-dichloroethane, or carbon tetrachloride; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; nitriles such as acetonitrile or propionitrile; esters such as ethyl acetate or ethyl propionate, or mixed solvents thereof. The use amount of the solvent is 0.1 to 500 liters, preferably 0.2 to 50 liters relative to 1 mol of compound [XXIV].
(562) The reaction temperature of the present reaction may be selected from any range of temperature typically from ?30? C. to a reflux temperature in a reaction system, and is preferably in the range of ?10? C. to 100? C.
(563) The reaction time of the present reaction is typically 5 minutes to 24 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.
(564) After end of the reaction, water is added to the reaction mixture, and then the precipitated solid is filtered off or extracted with an organic solvent, followed by concentration or the like operation, and thus compound [XXVI] can be isolated. The isolated compound [XXVI] can be further purified by column chromatography, recrystallization, or the like as necessary.
(565) <Production Method 13>
(566) A compound represented by general formula [XVII] among the present compounds can be produced, for example, by using a compound represented by general formula [XXVII] in accordance with the following method.
(567) ##STR00027## (wherein, X.sup.2 represents a halogen atom, C.sub.1-C.sub.6 alkylsulfonyloxy group, trifluoromethanesulfonyloxy group, nonafluorobutylsulfonyloxy group, phenylsulfonyloxy group, 4-toluenesulfonyloxy group, C.sub.1-C.sub.6 alkylsulfonyl group, phenylsulfonyl group or 4-toluenesulfonyl group, and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and Q are as defined above.)
(568) That is, the compound represented by general formula [XVII] can be produced by reacting compound [XXVII] and compound [XXVIII] or compound [XXIX] in an appropriate solvent in the presence or absence of an appropriate base.
(569) The use amount of compound [XXVIII] or compound [XXIX] used in the present reaction may be appropriately selected from the range of 1.0 to 10 mol, and is preferably 1.0 to 5.0 mol, relative to 1 mol of compound [XXVII].
(570) Examples of the solvent that can be used in the present reaction include ethers such as diethyl ether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or methyl tert-butyl ether; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; nitriles such as acetonitrile or propionitrile; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; pyridines such as pyridine or picoline; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 300 liters, preferably 0.3 to 50 liters relative to 1 mol of compound [XXVII].
(571) Examples of the base that can be used in the present reaction include inorganic bases such as hydroxides of alkali metal (e.g. sodium hydroxide or potassium hydroxide); hydroxides of alkali earth metal (e.g. calcium hydroxide or magnesium hydroxide); carbonates of alkali metal (e.g. sodium carbonate or potassium carbonate); bicarbonates of alkali metal (e.g. sodium hydrogen carbonate or potassium hydrogen carbonate); metal hydrides (e.g. sodium hydride or potassium hydride); metal salts of alcohol (e.g. sodium methoxide, sodium ethoxide, or potassium tert-butoxide); or organic bases such as triethylamine, N,N-dimethylaniline, pyridine, 4-N,N-dimethylaminepyridine, 1,8-diazacyclo[5.4.0]-7-undecene, and so on. The use amount of the base may be appropriately selected from the range of 1.0 to 10 mol, and is preferably 1.0 to 6.0 mol, relative to 1 mol of compound [XXVII]. The organic bases such as triethylamine or pyridine can also be used as the solvent.
(572) The present reaction can be conducted in the presence of a catalyst as necessary, and examples of the catalyst include pyridine, 4-(N,N-dimethyl)aminopyridine, or 4-pyrrolidinopyridine. The use amount of the catalyst may be appropriately selected from the range of 0.001 to 1.0 mol, and is preferably 0.01 to 0.1 mol, relative to 1 mol of compound [XXVII].
(573) The reaction temperature of the present reaction may be selected from any range of temperature from ?70? C. to a reflux temperature in a reaction system, and is preferably in the range of 0? C. to 150? C.
(574) The reaction time of the present reaction is typically 10 minutes to 24 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.
(575) After end of the reaction, water is added to the reaction mixture, and then extraction with an organic solvent is conducted, and then concentration or the like operation is conducted, and thus compound [XVII] can be isolated. The isolated compound [XVII] can be further purified by column chromatography, recrystallization, or the like as necessary.
(576) An agrochemical composition of the present invention contains the pyrazole derivative or an agriculturally acceptable salt thereof represented by general formula [I] or [II] of the present invention, as an active ingredient.
(577) The agrochemical composition can contain an additive component (carrier) that is typically used in an agrochemical formulation, as necessary.
(578) The present pest control agent contains the pyrazole derivative or an agriculturally acceptable salt thereof represented by general formula [I] or [II] of the present invention, as an active ingredient. The present pest control agent is representatively an insecticide and a miticide.
(579) The present pest control agent can contain an additive component (carrier) that is typically used in an agrochemical formulation, as necessary.
(580) Examples of the additive component include a carrier such as a solid carrier or a liquid carrier, a surfactant, a binder or a tackifier, a thickener, a coloring agent, a spreader, a sticker, an antifreezing agent, an anticaking agent, a disintegrating agent, and a stabilizing agent, and besides the above, an antiseptic, a plant piece, or the like may be added to the additive component as necessary. These additive components may be used singly or in combination of two or more kinds.
(581) Hereinafter, the aforementioned additive components are described.
(582) Examples of the solid carrier include mineral carriers such as pyrophyllite clay, kaolin clay, silica clay, talc, diatomite, zeolite, bentonite, Japanese acid clay, activated clay, attapulgus clay, vermiculite, pearlite, pumice, white carbon (synthetic silicic acid, synthetic silicate, or the like), or titanium dioxide; vegetal carriers such as woody powder, corn haulm, walnut shell, fruit stone, chaff, sawdust, bran, soybean meal, powdered cellulose, starch, dextrin, or saccgarudes; inorganic salt carriers such as calcium carbonate, ammonium sulfate, sodium sulfate, or potassium chloride; and polymeric carriers such as polyethylene, polypropylene, polyvinyl chloride, polyvinyl acetate, ethylene-vinyl acetate copolymer, or urea-aldehyde resin.
(583) Examples of the liquid carrier include monohydric alcohols such as methanol, ethanol, propanol, 2-propanol, butanol, or cyclohexanol; polyhydric alcohols such as ethylene glycol, diethylene glycol, propylene glycol, hexylene glycol, polyethylene glycol, polypropylene glycol, or glycerin; polyhydric alcohol derivatives such as propylene glycol ether; ketones such as acetone, methylethyl ketone, methylisobutyl ketone, diisobutyl ketone, cyclohexanone, or isophoron; ethers such as ethyl ether, 1,4-dioxane, Cellosolve, dipropyl ether, or tetrahydrofuran; aliphatic hydrocarbons such as normal paraffin, naphthene, isoparaffin, kerosene, or mineral oil; aromatic hydrocarbons such as toluene, C.sub.9-C.sub.10 alkylbenzene, xylene, solvent naphtha, alkyl naphthalene, or high boiling point aromatic hydrocarbons; halogenated hydrocarbons such as 1,2-dichloroethane, chloroform, or carbon tetrachloride; esters such as ethyl acetate, diisopropyl phthalate, dibutyl phthalate, dioctyl phthalate, or dimethyl adipate; lactones such as ?-butyrolactone; amides such as N,N-dimethylformamide, N,N-diethylformamide, N,N-dimethylacetamide, or N-methyl-2-pyrrolidone; nitriles such as acetonitrile; sulfur compounds such as dimethyl sulfoxide; vegetable oils such as soybean oil, rapeseed oil, cottonseed oil, coconut oil, or castor oil; and water.
(584) Although not particularly limited, the surfactant preferably gelates or shows swelling property in water, and examples of the surfactant include noionic surfactants such as sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, sucrose fatty acid ester, polyoxyethylene fatty acid ester, polyoxyethylene resin acid ester, polyoxyethylene fatty acid diester, polyoxyethylene alkyl ether, polyoxyethylene alkylphenyl ether, polyoxyethylene dialkylphenyl ether, polyoxyethylene alkylphenyl ether formalin condensate, polyoxyethylene polyoxypropylene block polymer, alkylpolyoxyethylene polypropylene block polymer ether, polyoxyethylene alkyl amine, polyoxyethylene fatty acid amide, polyoxyethylene fatty acid bisphenyl ether, polyalkylene benzyl phenyl ether, polyoxyalkylene styryl phenyl ether, acetylene diol, polyoxyalkylene-added acetylene diol, polyoxyethylene ether silicone, ester silicone, fluorine surfactant, polyoxyethylene castor oil, or polyoxyethylene hardened castor oil; anionic surfactants such as alkyl sulfates, polyoxyethylene alkyl ether sulfates, polyoxyethylene alkyl phenyl ether sulfates, polyoxyethylene styryl phenyl ether sulfate, alkyl benzenesulfonates, lignin sulfonate, alkyl sulfosuccinates, naphthalene sulfonate, alkylnaphthalene sulfonates, salts of formalin condensate of naphthalene sulfonate, salts of formalin condensate of alkylnaphthalene sulfonate, fatty acid salts, polycarboxylates, N-methyl-fatty acid Sarcosinates, resinates, polyoxyethylene alkyl ether phosphates, or polyoxyethylene alkyl pheny ether phosphates; cationic surfactants such as alkyl amine salts such as lauryl amine hydrochloride, stearyl amine hydrochloride, oleyl amine hydrochloride, stearyl amine acetate, stearyl aminopropylamine acetate, alkyl trimethyl ammonium chlorides, or alkyl dimethylbenzarconium chloride; and amphoteric surfactants including a betaine type such as dialkyl diaminoethyl betaine, or alkyl dimethylbenzyl betaine, and an amino acid type such as dialkylaminoethyl glycin, or alkyl dimethylbenzyl glycin.
(585) Examples of the binder or the tackifier include carboxymethylcelullose or a salt thereof, dextrin, soluble starch, xanthan gum, guar gum, sucrose, polyvinylpyrrolidone, gum arabic, polyvinyl alcohol, polyvinyl acetate, sodium polyacrylate, polyethylene glycol having an average molecular weight of 6000 to 20000, polyethylene oxide having an average molecular weight of 100000 to 5000000, and naturally-occurring phospholipid (for example, Cephalin, lecithin, or the like).
(586) Examples of the thickener include water-soluble polymers such as xanthan gum, guar gum, carboxymethylcelullose, polyvinylpyrrolidone, carboxyvinyl polymer, acrylic polymer, starch derivatives, or polysaccharides; and inorganic fine powder such as high purity bentonite or white carbon.
(587) Examples of the coloring agent include inorganic pigments such as iron oxide, titanium oxide, or Prussian blue; and organic dyes such as an alizarin dye, an azo dye, or a metal phthalocyanine dye.
(588) Examples of the spreader include a silicone surfactant, cellulose powder, dextrin, processed starch, a polyaminocarboxylic acid chelete compound, a cross-linked polyvinylpyrrolidone, malic acid and styrenes, methacrylic acid copolymer, a half ester of a polymer of polyhydric alcohol and dicarboxylic acid anhydride, and a water-soluble salt of polystyrene sulfonic acid.
(589) Examples of the sticker include various surfactants such as sodium dialkyl sulfosuccinate, polyoxyethylene alkyl ether, polyoxyethylene alkylphenyl ether, or polyoxyethylene fatty acid ester; paraffin, terpene, polyamide resin, polyacrylate, polyoxyethylene, wax, polyvinylalkyl ether, an alkylphenol formalin condensate, and a synthetic resin emulsion.
(590) Examples of the antifreezing agent include polyhydric alcohols such as ethylene glycol, diethylene glycol, propylene glycol, or glycerin.
(591) Examples of the anticaking agent include polysaccharides such as starch, alginic acid, mannose, or galactose; polyvinylpyrrolidone, white carbon, ester gum, and petroleum resin.
(592) Examples of the disintegrating agent include sodium tripolyphosphate, sodium hexametaphosphate, a stearic metal salt, cellulose powder, dextrin, copolymer of methacrylic ester, polynylpyrrolidone, polyaminocarboxylic chelate compound, styrene sulfonate-isobutylene-maleic anhydride copolymer, and starch-polyacrylonitrile graft copolymer.
(593) Examples of the stabilizing agent include a desiccant such as zeolite, calcined lime, or magnesium oxide; an antioxidant based on phenol, amine, sulfur, phosphoric acid, or the like; an ultraviolet absorber based on salicylic acid, benzophenone, or the like.
(594) In the present pest control agent, when the additive component is contained, the content thereof is selected typically in a range of 5 to 95%, preferably in the range of 20 to 90% on the mass basis in the case of a carrier such as a solid carrier or a liquid carrier, selected typically in a range of 0.1% to 30%, preferably in a range of 0.5 to 10% in the case of a surfactant, and selected typically in a range of 0.1 to 30%, preferably in a range of 0.5 to 10% in the case of other additive.
(595) The present pest control agent is used while it is prepared into any formulation including dusts, dusts and granules, granules, water-dispersible powders, water-soluble powders, water-dispersible granules, tablets, Jumbos, emulsifiable concentrates, oils, solutions, flowable concentrates, emulsions, microemulsions, suspoemulsions, ultra-low volume dusting powders, microcapsules, smoking agents, aerosols, baiting agents, and pastes.
(596) In actual use of the formulation, the formulation can be used per se or after dilution with a diluent such as water in a predetermined concentration. Application of various formulations containing the present compound, and dilution products thereof can be conducted by a method ordinarily used, such as dispersion (e.g., spraying, misting, atomizing, powder dispersion, granule dispersion, on-water-surface dispersion, or inbox dispersion), in-soil application (e.g., mixing or drenching), on-surface application (e.g., coating, dust coating, or covering), seed treatment (e.g., smearing or dressing treatment), immersion, poison bait, smoking, and the like. It is also possible to mix the above-mentioned active ingredient with a livestock feed in order to prevent the infestation and growth of pests, particularly harmful insects in the excreta of the livestock.
(597) A method for controlling a pest of the present invention can be conducted by using an active ingredient amount of the pyrazole derivative represented by general formula [I] or [II] of the present invention or an agriculturally acceptable salt thereof in the above-mentioned application method described above.
(598) The mixing proportion (% by mass) of the active ingredient in the present pest control agent is appropriately selected as needed. For example, the mixing proportion may be appropriately selected in the following ranges: 0.01 to 20%, preferably to 10% for dusts, dusts and granules, microgranules, or the like; 0.1 to 30%, preferably to 20% for granules or the like; 1 to 70%, preferably 5 to 50% for water-dispersible powders, water-dispersible granules, or the like; 1 to 95%, preferably 10 to 80% for water-soluble powders, solutions, or the like; 5 to 90%, preferably 10 to 80% for emulsifiable concentrates or the like; 1 to 50%, preferably 5 to 30% for oils or the like; 5 to 60%, preferably 10 to 50% for flowable concentrates or the like; 5 to 70%, preferably 10 to 60% for emulsions, microemulsions, suspoemulsions, or the like; 1 to 80%, preferably 5 to 50% for tablets, baiting agents, pastes, or the like; 0.1 to 50%, preferably 1 to 30% for smoking agents or the like; and 0.05 to 20%, preferably 0.1 to 10% for aerosols or the like.
(599) The formulation is sprayed after dilution in an appropriate concentration, or applied directly.
(600) When present pest control agent is used after dilution with a diluent, the concentration of the active ingredient is generally 0.1 to 5000 ppm. When the formulation is used per se, the application amount thereof per unit area is 0.1 to 5000 g per 1 ha in terms of the active ingredient compound; however, the application amount is not restricted thereto.
(601) It goes without saying that the present pest control agent is sufficiently effective when the present compound is used alone as an active ingredient. However, the present pest control agent may be mixed or used in combination, as necessary, with other fertilizers and agricultural chemicals such as insecticide, miticide, nematicide, synergist, fungicide, antiviral agent, attractant, herbicide, plant growth-controlling agent, and the like. In this case, a more excellent effect can be exhibited.
(602) Below are shown examples of known insecticides, miticides, nematicides, and synergist compounds, which may be mixed or used in combination.
(603) Insecticide Active Ingredients: acrinathrin, azadirachtin, azamethiphos, acynonapyr, azinphos-ethyl, azinphos-methyl, acequinocyl, acetamiprid, acetoprole, acephate, azocyclotin, abamectin, afidopyropen, afoxolaner, amidoflumet, amitraz, alanycarb, aldicarb, aldoxycarb, allethrin [including d-cis-trans-form, and d-trans-form], isazophos, isamidofos, isocarbophos, isoxathion, isocycloseram, isofenphos-methyl, isoprocarb, epsilon-metofluthrin, epsilon-momfluorothrin, ivermectin, imicyafos, imidacloprid, imiprothrin, indoxacarb, esfenvalerate, ethiofencarb, ethion, ethiprole, ethylene dibromide, etoxazole, etofenprox, ethoprophos, etrimfos, emamectin, emamectin benzoate, endosulfan, empenthrin, oxazosulfyl, oxamyl, oxydemeton-methyl, oxydeprofos, omethoate, cadusafos, kappa-tefluthrin, kappa-bifenthrin, karanjin, cartap, carbaryl, carbosulfan, carbofuran, gamma-BHC, xylylcarb, quinalphos, kinoprene, chinomethionat, coumaphos, cryolite, clothianidin, clofentezine, chromafenozide, chlorantraniliprole, chlorethoxyfos, chlordane, chloropicrin, chlorpyrifos, chlorpyrifos-methyl, chlorfenapyr, chlorfenvinphos, chlorfluazuron, chlormephos, chloroprallethrin, cyazypyr, cyanophos, diafenthiuron, diamidafos, cyantraniliprole, dienochlor, cyenopyrafen, dioxabenzofos, diofenolan, cyclaniliprole, cycloxaprid, dicrotophos, dichlofenthion, cycloprothrin, dichlorvos, dicloromezotiaz, dicofol, dicyclanil, disulfoton, dinotefuran, dinobuton, cyhalodiamide, cyhalothrin [including gamma-form, and lambda-form], cyphenothrin [including (1R)-trans-form], cyfluthrin) [including beta-form], diflubenzuron, cyflumetofen, diflovidazin, cyhexatin, cypermethrin [including alpha-form, beta-form, theta-form, and zeta-form], dimpropyridaz, dimethyl-2,2,2-trichloro-1-hydroxyethyl phosphate (DEP), dimethylvinphos, dimethoate, dimefluthrin, silafluofen, cyromazine, spinetoram, spinosad, spirodiclofen, spirotetramat, spiropidion, spiromesifen, sulcofuron-sodium, sulfluramid, sulfoxaflor, sulfotep, diazinon, thiacloprid, thiamethoxam, tioxazafen, thiodicarb, thiocyclam, thiosultap, thionazin, thiofanox, thiometon, tyclopyrazoflor, tetrachlorantraniliprole, tetrachlorvinphos, tetradifon, tetraniliprole, tetramethylfluthrin, tetramethrin, tebupirimfos, tebufenozide, tebufenpyrad, tefluthrin, teflubenzuron, demeton-S-methyl, temephos, deltamethrin, terbufos, tralomethrin, transfluthrin, triazamate, triazophos, trichlorfon, triflumuron, triflumezopyrim, trimethacarb, tolfenpyrad, naled, nicotine, nitenpyram, nemadectin, novaluron, noviflumuron, Verticillium lecanii, hydroprene, Bacillus sphaericus, Bacillus subtillis, Bacillus thuringiensis, insect toxin produced by Bacillus thuringiensis, Bacillus thuringiensis subsp. aizawai, Bacillus thuringiensis subsp. israelensis, Bacillus thuringiensis subsp. kurstaki, Bacillus thuringiensis subsp. tenebrionis, Bacillus popilliae, Pasteuriapenetrans spore, vamidothion, parathion, parathion-methyl, halfenprox, halofenozide, bioallethrin, bioallethrin S-cyclopentenyl, bioresmethrin, bis-(2-chloro-1-methylethyl)ether (DCIP), bistrifluron, hydramethylnon, bifenazate, bifenthrin, pyflubumide, piperonyl butoxide, pymetrozine, pyraclofos, pyrafluprole, pyridaphenthion, pyridaben, pyridalyl, pyrifluquinazon, pyriprole, pyriproxyfen, pirimicarb, pyrimidifen, pyriminostrobin, pirimiphos-methyl, pyrethrine, famphur, fipronil, fenazaquin, fenamiphos, fenitrothion, fenoxycarb, fenothiocarb, phenothrin [including (1R)-trans-form], fenobucarb, fenthion, phenthoate, fenvalerate, fenpyroximate, fenbutatin oxide, fenpropathrin, fonofos, sulfuryl fluoride, butocarboxim, butoxycarboxim, buprofezin, furathiocarb, prallethrin, fluacrypyrim, fluazaindolizine, fluazuron, fluensulfone, fluopyram, sodium fluoroacetate, fluxametamide, flucycloxuron, flucythrinate, flusulfamide, fluthrin, fluvalinate [including tau-form], flupyradifurone, flupyrazofos, flupyrimin, flufiprole, flufenerim, flufenoxystrobin, flufenoxuron, fluhexafon, flubendiamide, flumethrin, fluralaner, flurimfen, prothiofos, protrifenbute, flonicamid, propaphos, propargite, profenofos, broflanilide, profluthrin, propetamphos, propoxur, flometoquin, bromopropylate, hexythiazox, hexaflumuron, Pacilimyces tenuipes, Paecilomyces fumosoroceus, heptafluthrin, heptenophos, permethrin, benclothiaz, benzpyrimoxan, bensultap, benzoximate, bendiocarb, benfuracarb, Beauveria tenella, Beauveria bassiana, Beauveria brongniartii, phoxim, phosalone, fosthiazate, fosthietan, phosphamidon, phosmet, polynactins, formetanate, phorate, machine oil, malathion, milbemectin, mecarbam, mesulfenfos, methomyl, metaldehyde, metaflumizone, methamidophos, metham, methiocarb, methidathion, methyl isothiocyanate, methyl bromide, methoxychlor, methoxyfenozide, methothrin, metofluthrin, methoprene, metolcarb, mevinphos, meperfluthrin, Monacrosporium phymatophagum, monocrotophos, momfluorothrin, litlure-A, litlure-B, aluminium phosphide, zinc phosphide, phosphine, lufenuron, rescalure, resmethrin, lepimectin, rotenone, nuclear polyhedrosis virus silkworm-embedded form, fenbutatin oxide, calcium cyanide, organotins, nicotine-sulfate, (Z)-11-tetradecenyl=acetate, (Z)-11-hexadecenal, (Z)-11-hexadecenyl=acetate, (Z)-9,12-tetradecadienyl=acetate, (Z)-9-tetradecene-1-ol, (Z,E)-9,11-tetradecadienyl=acetate, (Z,E)-9,12-tetradecadienyl=acetate, 1,1,1-trichloro-2,2-bis(4-chlorophenyl)ethane (DDT), 1,3-dichloropropene(1,3-dichloropropene), 2,4-dichloro-5-{2-[4-(trifluoromethyl)phenyl]ethoxy}phenyl 2,2,2-trifluoroethyl sulfoxide (Chemical name, CAS registry number: 1472050-04-6), 2,4-dichloro-5-12-[4-(trifluoromethyl)phenyl]ethoxylphenyl 2,2,2-trifluoroethyl sulfoxide (Chemical name, CAS registry number: 1472052-11-1), 2,4-dimethyl-5-[6-(trifluoromethylthio)hexyloxy]phenyl-2,2,2-trifluoroethyl sulfoxide (Chemical name, CAS registry number: 1472050-34-2), 2-{2-fluoro-4-methyl-5-[(2,2,2-trifluoroethyl)sulfinyl]phenoxy}-5-(trifluoromethyl)pyridine (Chemical name, CAS registry number: 1448758-62-0), 3-chloro-2-{2-fluoro-4-methyl-5-[(2,2,2-trifluoroethyl)sulfinyl]phenoxy}-5-(trifluoromethyl)pyridine (Chemical name, CAS registry number: 1448761-28-1), 4,6-dinitro-o-cresol (DNOC), 4-fluoro-2-methyl-5-(5,5-dimethylhexyloxy]phenyl-2,2,2-trifluoroethyl sulfoxide (Chemical name, CAS registry number: 1472047-71-4), Bt protein (Cry1Ab, Cry1Ac, Cry1Fa, Cry2Ab, mCry3A, Cry3Ab, Cry3Bb, Cry34/35Ab1), CL900167 (code number), NA-85 (code number), NI-30 (code number), O,O-diethyl-O-[4-(dimethylsulfamoyl)phenyl]-phosphorothioate (DSP), O-ethyl-O-4-(nitrophenyl)phenylphosphonothioate (EPN), RU15525 (code number), XMC(XMC), Z-13-icosen-10-one, ZXI8901 (code number).
(604) Next, examples of known bactericides or disease controller compounds that can be mixed or used in combination are shown below.
(605) Bactericide active Ingredients: azaconazole, acibenzolar-S-methyl, azoxystrobin, anilazine, amisulbrom, aminopyrifen, ametoctradin, aldimorph, isotianil, isopyrazam, isofetamid, isoflucypram, isoprothiolane, ipconazole, ipflufenoquin, ipfentrifluconazole, iprodione, iprovalicarb, iprobenfos, imazalil, iminoctadine-albesilate, iminoctadine-triacetate, imibenconazole, inpyrfluxam, imprimatin A, imprimatin B, edifenphos, etaconazole, ethaboxam, ethirimol, ethoxyquin, etridiazole, enestroburin, enoxastrobin, epoxiconazole, organic oils, oxadixyl, oxazinylazole, oxathiapiprolin, oxycarboxin, oxine-copper, oxytetracycline, oxpoconazole-fumarate, oxolinic acid, copper dioctanoate, octhilinone, ofurace, orysastrobin, o-phenylphenol, kasugamycin, captafol, carpropamid, carbendazim, carboxin, carvone, quinoxyfen, quinofumelin, chinomethionat, captan, quinconazole, quintozene, guazatine, cufraneb, coumethoxystrobin, coumoxystrobin, kresoxim-methyl, clozylacon, chlozolinate, chlorothalonil, chloroneb, cyazofamid, diethofencarb, diclocymet, dichlofluanid, dichlobentiazox, diclomezine, dicloran, dichlorophen, dithianon, diniconazole, diniconazole-M, zineb, dinocap, dipymetitrone, diphenylamine, difenoconazole, cyflufenamid, diflumetorim, cyproconazole, cyprodinil, simeconazole, dimethirimol, dimethyl disulfide, dimethomorph, cymoxanil, dimoxystrobin, Pseudomonas rhodesiae HAI-0804, ziram, silthiofam, streptomycin, spiroxamine, sedaxane, zoxamide, solatenol, dazomet, Talaromyces flavus, tiadinil, thiabendazole, thiram, thiophanate, thiophanate-methyl, thifluzamide, thiram, tecnazene, tecloftalam, tetraconazole, debacarb, tebuconazole, tebufloquin, terbinafine, dodine, dodemorph, triadimenol, triadimefon, triazoxide, trichlamide, triclopyricarb, Trichoderma atroviride, tricyclazole, triticonazole, tridemorph, triflumizole, trifloxystrobin, triforine, tolylfluanid, tolclofos-methyl, tolnifanide, tolprocarb, nabam, natamycin, naftifine, nitrapyrin, nitrothal-isopropyl, nuarimol, copper nonyl phenol sulphonate, Bacillus subtilis)(strain: QST 713, validamycin, valifenalate, picarbutrazox, bixafen, picoxystrobin, pydiflumetofen, bitertanol, binapacryl, hinokitiol, biphenyl, piperalin, hymexazol, pyraoxystrobin, pyraclostrobin, pyraziflumid, pyrazophos, pyrapropoyne, pyrametostrobin, pyriofenone, pyrisoxazole, pyridachlometyl, pyrifenox, pyributicarb, pyribencarb, pyrimethanil, pyroquilon, vinclozolin, ferbam, famoxadone, phenazine oxide, fenamidone, fenaminstrobin, fenarimol, fenoxanil, ferimzone, fenpiclonil, fenpicoxamid, fenpyrazamine, fenbuconazole, fenfuram, fenpropidin, fenpropimorph, fenhexamid, folpet, phthalide, bupirimate, fuberidazole, blasticidin-S, furametpyr, furalaxyl, furancarboxylic acid, fluazinam, fluindapyr, fluoxastrobin, fluoxapiprolin, fluopicolide, fluopimomide, fluopyram, fluoroimide, fluxapyroxad, fluquinconazole, furconazole, furconazole-cis, fludioxonil, flusilazole, flusulfamide, flutianil, flutolanil, flutriafol, flufenoxystrobin, flumetover, flumorph, proquinazid, prochloraz, procymidone, prothiocarb, prothioconazole, bronopol, propamocarb-hydrochloride, propiconazole, propineb, probenazole, bromuconazole, flometoquin, florylpicoxamid, hexaconazole, benalaxyl, benalaxyl-M, benodanil, benomyl, pefurazoate, penconazole, pencycuron, benzovindiflupyr, benthiazole, benthiavalicarb-isopropyl, penthiopyrad, penflufen, boscalid, fosetyl (aluminium, calcium, sodium), polyoxin, polycarbamate, Bordeaux mixture, mancopper, mancozeb, mandipropamid, mandestrobin, maneb, myclobutanil, mineral oils, mildiomycin, methasulfocarb, metam, metalaxyl, metalaxyl-M, metiram, metyltetraprole, metconazole, metominostrobin, metrafenone, mepanipyrim, mefentrifluconazole, meptyldinocap, mepronil, iodocarb, laminarin, Rhizobium vitis, phosphorous acid and salts, copper oxychloride, silver, cuprous oxide, copper hydroxide, potassium bicarbonate, sodium bicarbonate, sulfur, oxyquinoline sulfate, copper sulfate, (3,4-dichloroisothiazole-5-yl)methyl 4-(tert-butyl)benzoic ester (Chemical name, CAS registry number: 1231214-23-5), BAF-045 (code number), BAG-010 (code number), UK-2A (code number), dodecylbenzenesulfonic acid bisethylenediamine copper [II] salt (DBEDC), MIF-1002 (code number), NF-180 (code number), triphenyltin acetate (TPTA), triphenyltin chloride (TPTC), triphenyltin hydroxide (TPTH), avirulent Erwinia carotovora.
(606) Next, examples of known herbicides or plant growth regulator compounds that can be mixed or used in combination are shown below.
(607) Herbicide active Ingredients: ioxynil, aclonifen, acrolein, azafenidin, acifluorfen (including a salt with sodium or the like), azimsulfuron, asulam, acetochlor, atrazine, anilofos, amicarbazone, amidosulfuron, amitrole, aminocyclopyrachlor, aminopyralid, amiprofos-methyl, ametryn, alachlor, alloxydim, ancymidol, isouron, isoxachlortole, isoxaflutole, isoxaben, isodecylalkoholethoxylate, isoproturon, ipfencarbazone, imazaquin, imazapic (including a salt with amine or the like), imazapyr (including a salt of isopropylamine or the like), imazamethabenz-methyl, imazamox, imazethapyr, imazosulfuron, indaziflam, indanofan, eglinazine-ethyl, esprocarb, ethametsulfuron-methyl, ethalfluralin, ethidimuron, ethoxysulfuron, ethoxyfen-ethyl, ethofumesate, etobenzanid, endothal-disodium, oxadiazon, oxadiargyl, oxaziclomefone, oxasulfuron, oxyfluorfen, oryzalin, orthosulfamuron, orbencarb, oleic acid, cafenstrole, carfentrazone-ethyl, karbutilate, carbetamide, quizalofop, quizalofop-ethyl, quizalofop-P-ethyl, quizalofop-P-tefuryl, quinoclamine, quinclorac, quinmerac, cumyluron, clacyfos, glyphosate (including a salt of sodium, potassium, amine, propylamine, isopropylamine, dimethylamine, trimesium, or the like), glufosinate (including a salt of amine, sodium, or the like), glufosinate-P, glufosinate-P-sodium, clethodim, clodinafop-propargyl, clopyralid, clomazone, chlomethoxyfen, clomeprop, cloransulam-methyl, chloramben, chloridazon, chlorimuron-ethyl, chlorsulfuron, chlorthal-dimethyl, chlorthiamid, chlorphthalim, chlorflurenol-methyl, chlorpropham, chlorbromuron, chloroxuron, chlorotoluron, ketospiradox (including a salt of sodium, calcium, ammonia, or the like), saflufenacil, sarmentine, cyanazine, cyanamide, diuron, diethatyl-ethyl, dicamba (including a salt of amine, diethylamine, isopropylamine, diglycolamine, sodium, lithium, or the like), cycloate, cycloxydim, diclosulam, cyclosulfamuron, cyclopyranil, cyclopyrimorate, dichlobenil, diclofop-P-methyl, diclofop-methyl, dichlorprop, dichlorprop-P, diquat, dithiopyr, siduron, dinitramine, cinidon-ethyl, cinosulfuron, dinoseb, dinoterb, cyhalofop-butyl, diphenamid, difenzoquat, diflufenican, diflufenzopyr, simazine, dimethachlor, dimethametryn, dimethenamid, dimethenamid-P, simetryn, dimepiperate, dimefuron, cinmethylin, swep, sulcotrione, sulfentrazone, sulfosate, sulfosulfuron, sulfometuron-methyl, sethoxydim, terbacil, daimuron, thaxtomin A, dalapon, thiazopyr, tiafenacil, thiencarbazone (including sodium salt, methyl ester, or the like), tiocarbazil, thiobencarb, thidiazimin, thidiazuron, thifensulfuron-methyl, desmedipham, desmetryne, tetflupyrolimet, thenylchlor, tebutam, tebuthiuron, tepraloxydim, tefuryltrione, terbuthylazine, terbutryn, terbumeton, tembotrione, topramezone, tralkoxydim, triaziflam, triasulfuron, triafamone, tri-allate, trietazine, triclopyr, triclopyr-butotyl, tritosulfuron, trifludimoxazin, triflusulfuron-methyl, trifluralin, trifloxysulfuron-sodium, tribenuron-methyl, tolpyralate, naptalam (including a salt with sodium or the like), naproanilide, napropamide, napropamide-M, nicosulfuron, neburon, norflurazon, vernolate, paraquat dichloride, halauxifen-benzyl, halauxifen-methyl, haloxyfop, haloxyfop-P, haloxyfop-etotyl, halosafen, halosulfuron-methyl, bixlozone, picloram, picolinafen, bicyclopyrone, bispyribac-sodium, pinoxaden, bifenox, piperophos, pyraclonil, pyrasulfotole, pyrazoxyfen, pyrazosulfuron-ethyl, pyrazolynate, bilanafos, pyraflufen-ethyl, pyridafol, pyrithiobac-sodium, pyridate, pyriftalid, pyributicarb, pyribenzoxim, pyrimisulfan, pyriminobac-methyl, pyroxasulfone, pyroxsulam, phenisopham, fenuron, fenoxasulfone, fenoxaprop (including methyl, ethyl, isopropylester), fenoxaprop-P (including methyl, ethyl, isopropyl ester), fenquinotrione, fenthiaprop-ethyl, fentrazamide, phenmedipham, foramsulfuron, butachlor, butafenacil, butamifos, butylate, butenachlor, butralin, butroxydim, flazasulfuron, flamprop (including methyl, ethyl, isopropyl ester), flamprop-M (including methyl, ethyl, isopropyl ester), primisulfuron-methyl, fluazifop-butyl, fluazifop-P-butyl, fluazolate, fluometuron, fluoroglycofen-ethyl, flucarbazone-sodium, fluchloralin, flucetosulfuron, fluthiacet-methyl, flupyrsulfuron-methyl (including a salt of sodium, calcium, ammonia, or the like), flufenacet, flufenpyr-ethyl, flupropanate, flupoxame, flumioxazin, flumiclorac-pentyl, flumetsulam, fluridone, flurtamone, fluroxypyr (including an ester such as butomethyl or meptyl, a salt of sodium, calcium, ammonia, or the like), flurochloridone, pretilachlor, procarbazone-sodium, prodiamine, prosulfuron, prosulfocarb, propaquizafop, propachlor, propazine, propanil, propyzamide, propisochlor, propyrisulfuron, propham, profluazol, prohexadione-calcium, propoxycarbazone, propoxycarbazone-sodium, profoxydim, bromacil, brompyrazon, prometryn, prometon, bromoxynil (including an ester of butyric acid, octanoic acid, heptanoic acid, or the like), bromofenoxim, bromobutide, florasulam, florpyrauxifen, florpyrauxifen-benzyl, hexazinone, pethoxamid, benazolin, penoxsulam, heptamaloxyloglucan, beflubutamid, beflubutamid-M, pebulate, pelargonic acid, bencarbazone, pendimethalin, benzfendizone, bensulide, bensulfuron-methyl, benzobicyclon, benzofenap, bentazone, pentanochlor, pentoxazone, benfluralin, benfuresate, fosamine, fomesafen, foramsulfuron, forchlorfenuron, mecoprop (including a salt of sodium, potassium, isopropylamine, triethanolamine, dimethylamine, or the like), mecoprop-P-potassium, mesosulfuron (including an ester of methyl or the like), mesotrione, metazachlor, metazosulfuron, methabenzthiazuron, metamitron, metamifop, metam, disodium methanearsonate (DSMA), methiozolin, methyldymuron, metoxuron, metosulam, metsulfuron-methyl, metobromuron, metobenzuron, metolachlor, metribuzin, mepiquat chloride, mefenacet, monosulfuron (including methyl, ethyl, isopropylester), monolinuron, molinate, iodosulfuron, iodosulfulon-methyl-sodium, iofensulfuron, iofensulfuron-sodium, lactofen, lancotrione, linuron, rimsulfuron, lenacil, 2,2,2-trichloroacetic acid (TCA) (including a salt of sodium, calcium, ammonia, or the like), 2,3,6-trichlorobenzoic acid (2,3,6-TBA), 2,4,5-trichlorophenoxyacetic acid (2,4,5-T), 2,4-dichlorophenoxyacetic acid (2,4-D) (including a salt of amine, diethylamine, triethanolamine, isopropylamine, sodium, lithium, or the like), 2-amino-3-chloro-1,4-naphthoquinone (ACN), 2-methyl-4-chlorophenoxyacetic acid (MCPA) (including a sodium salt, ethyl ester, or the like), 2-methyl-4-chlorophenoxyacetic acid (MCPB) (including a sodium salt, ethyl ester, or the like), 4-(2,4-dichlorophenoxy)butyric acid (2,4-DB), 4,6-dinitro-O-cresol (DNOC) (including a salt of amine, sodium, or the like), AE-F-150944 (code number), IR-6396 (code number), MCPA-thioethyl, SYP-298 (code number), SYP-300 (code number), S-ethyldipropylthiocarbamate (EPTC), S-metolachlor, S-9750 (code number), MSMA, HW-02 (code number).
(608) Plant Growth Regulators: 1-naphthylacetamide, 1-methylcyclopropene, 2,6-diisopropylnaphthalene, 4-oxo-4-(2-phenylethyl)aminobutyric acid (Chemical name, CAS registry number: 1083-55-2), 4-chlorophenoxyacetic acid (4-CPA), n-decanol, aviglycine, ancymidol, abscisic acid, inabenfide, indole acetic acid, indole butyric acid, uniconazole, uniconazole-P, Ecolyst, ethychlozate, ethephon, epocholeone, oxine-sulfate, carvone, calcium formate, cloxyfonac, cloxyfonac-potassium, cloprop, chlormequat, choline, cytokinins, cyclanilide, dikegulac, gibberellin acid, dimethipin, sintofen, daminozide, thidiazuron, triacontanol, trinexapac-ethyl, paclobutrazol, paraffin, flumetralin, flurprimidol, flurenol, prohydrojasmon, prohexadione-calcium, heptamaloxyloglucan, benzylaminopurine, forchlorfenuron, maleic hydrazide, mepiquat chloride, mefluidide, calcium peroxide.
(609) Next, examples of known phytotoxicity alleviating compounds that can be mixed or used in combination are shown below.
(610) Isoxadifen, isoxadifen-ethyl, oxabetrinil, cloquintcet-mexyl, dietholate, cyometrinil, dichlormid, dicyclonone, cyprosulfamide, 1,8-Naphthalic Anhydride, fenchlorazole-O-ethyl, fenclorim, furilazole, fluxofenim, flurazole, benoxacor, mephenate, mefenpyr, mefenpyr-ethyl, mefenpyr-diethyl, lower alkyl-substituted benzoic acid, 2,2-dichloro-N-(1,3-dioxane-2-ylmethyl)-N-(2-propenyl)acetamide (PPG-1292), 2-dichloromethyl-2-methyl-1,3-dioxane (MG-191), 3-dichloroacetyl-2,2,5-trimethyl-1,3-oxazolidine (R-29148), 4-dichloroacetyl-1-oxa-4-azaspiro[4.5]decane (AD-67), MON4660 (code number), metcamifen, N1,N2-diallyl-N2-dichloroacetyl glycineamide (DKA-24), TI-35 (code number).
(611) The present pest control agent configured as described above exhibits excellent controlling effect on Orthoptera pests, Thysanoptera pests, Hemiptera pests, Coleoptera pests, Diptera pests, Lepidoptera pests, Hymenoptera pests, Collembola pests, Thysanura pests, Blattodea pests, Isoptera pests, Psocoptera pests, Mallophage pests, Anoplura pests, plant parasitic Acari, plant parasitic nematoda, plant parasitic mollusks, and other pests such as harmful animals, uncomfortable animals, sanitary insects, and parasites. As such pests, the following organism species can be exemplified.
(612) Examples of the Orthopteran pests include Ruspolia lineosa or the like of Tettigoniidae, Teleogryllus emma, Truljalia hibinonis, or the like of Gryllidae, Gryllotalpa orientalis or the like of Gryllotalpidae, Oxya hyla intricate, Locusta migratoria, Melanoplus sanguinipes, Melanoplus differentialis, Melanoplus femurrubrum, or the like of Acrididae, Atractomorpha lata of Pyrgomorphidae, Euscyrtus japonicus of Eneopteridae, and Xya japonicus or the like of Tridactylidae.
(613) Examples of the Thysanoptera pests include Frankliniella intonsa, Frankliniella occidentalis, Scirtothrips dorsalis, Thrips palmi, Thrips tabaci, Thrips setosus, Heliothrips haemorrhoidalis, Stenchaetothrips biformis, or the like of Thripidae, and Ponticulothrips diospyrosi, Liothrips wasabiae, Haplothrips aculeatus, or the like of Phlaeothripidaes.
(614) Examples of the Hemipteran pests include Mogannia minuta or the like of Cicadidae, Aphrophora intermedia or the like of Aphrophoridae, Machaerotypus sibiricus or the like of Membracidae, Arboridia apicalis, Empoasca onukii, Nephotettix cincticeps, Nephotettix malayanus, Nephotettix virescens, Nephotettix nigropictus, Recilia dorsalis, Okura Leafhopper (Amrasca biguttula), Mango Leafhopper (Idioscopus nitidulus, Idioscopus clypealis, Amritodus atkinsoni), Recilia dorsalis, Empoasca fabae, or the like of Cicadellidae, Pentastiridius apicalis or the like of Cixiidae, Laodelphax striatellus, Nilaparvata lugens, Sogatella furcifera, or the like of Delphacidae, Nisia nervosa or the like of Meenoplidae, Kamendaka saccharivora or the like of Derbidae, Achilus flammeus or the like of Cixidia, Orosanga japonicus or the like of Ricaniidae, Mimophantia maritima or the like of Flatidae, Cacopsylla pyrisuga, Diaphorina citri, or the like of Psyllidae, Calophya mangiferae or the like of Calophyidae, Daktulosphaira vitifoliae or the like of Phylloxeridae, Adelges laricis, Adelges tsugae, or the like of Adelgidae, Acyrthosiphon pisum, Aphis gossypii, Aphis spiraecola, Lipaphis erysimi, Brevicoryne brassicae, Myzuspersicae, Schizaphis graminum, Rhopalosiphum padi, Toxoptera aurautii, Aulacorthum solani, Macrosiphum euphorbiae, Nasonovia ribisnigri, Sitobion avenae, Aphis glycines, or the like of Aphydidae, Aleurocanthus camelliae, Aleurocanthus spiniferus, Bemisia tabaci, Bemisia argentifolii, Trialeurodes vaporariorum, or the like of Aleyrodidae, Drosicha corpulenta, Icerya purchasi, or the like of Margarodidae, Dysmicoccus brevipes, Planococcus citri, Pseudococcus comstocki, or the like of Pseudococcidae, Ceroplastes ceriferus, Ceroplastes rubens, or the like of Coccidae, Aclerda takahashii or the like of Aclerdidae, Aonidiella aurantii, Diaspidiotus perniciosus, Pseudaulacaspis pentagoa, Unaspis yanonensis, or the like of Diaspididae, Lygus lineolaris, Trigonotylus caelestialium, Apolygus lucorum, Nesidiocoris tenuis, Halticus bractatus, or the like of Miridae, Stephanitis pyrioides, Stephanitis nashi, or the like of Tingidae, Eurydema rugosum, Eysarcoris lewisi, Eysarcoris aeneus, Lagynotomus elongatus, Nezara viridula, Plautia crossota, Nezara antennata, Eushistus heros, or the like of Pentatomidae, Megacopta cribraria or the like of Plataspidae, Urochela luteovoria or the like of Urostylididae, Cavelerius saccharivorus or the like of Lygaeidae, Malcus japonicus or the like of Malcidae, Dysdercus cingulatus or the like of Pyrrhocoridae, Leptocorisa acuta, Leptocorisa chinensis, or the like of Alydidae, Anacanthocoris striicornis or the like of Coreidae, Rhopalus maculatus or the like of Rhopalidae, and Cimex lectularis or the like of Cimicidae.
(615) Examples of the Coleoptera pests include Anomara cuprea, Anomara rufocuprea, Popillia japonica, Oxycetonia jucunda, Anomala geniculata, Oryctes rhinoceros, Heptophylla picea, or the like of Scarabaeidae, Agriotes ogurae, Agriotes lineatus, Agriotes obscurus, Melanotus okinawensis, Melanotus fortnumi, or the like of Elateridae, Anthrenus verbasci or the like of Dermestidae, Heterobostrychus hamatipennis or the like of Bostrychidae, Stegobium paniceum or the like of Anobiidae, Pitinus clavipes or the like of Ptinidae, Tenebroides mauritanicus or the like of Trogossitidae, Necrobia rufipes of Cleridae, Carpophilus hemipterus, Meligethes aeneus, or the like of Nitidulidae, Ahasverus advena or the like of Silvanidae, Cryptolestes ferrugineus or the like of Laemophloeidae, Epilachna varivestis, Henosepilachna vigintioctopunctata or the like of Coccinellidae, Tenebrio molitor, Tribolium castaneum, or the like of Tenebrionidae, Epicauta gorhami or the like of Meloidae, Anoplophora glabripennis, Xylotrechus pyrrhoderus, Monochamus alternatus, Dectes texanus, or the like of Cerambycidae, Callosobruchus chinensis or the like of Bruchidae, Leptinotarsa decemlineata, Diabrotica virgifera virgifera, Diabrotica barberi, Diabrotica undecimpunctata howardi, Aulacophora femoralis, Phaedon brassicae, Cassida nebulosa, Oulema oryzae, Epilachna varivestis, Phyllotreta striolata, Demotina fasciculata, Psylliodes chrysocephala, Cerotoma trifurcate, Colaspis brunnea, Colaspis crinnicornis, Odontota horni, Chaetocnema pulicaria, or the like of Chrysomelidae, Cylas formicarius or the like of Brentidae, Hypera postica, Listroderes costirostris, Euscepes postfasciatus, Curculio sikkimensis, or the like of Curculionidae, Echinocnemus bipunctatus, Lissorhoptrus oryzophilus, Oryzophagus oryzae, or the like of Erirhinidae, Sitophilus zeamais, Sphenophrus venatus, or the like of Dryophthoridae, Tomicus piniperda or the like of Scolytidae, Crossotarsus niponicus or the like of Platypodidae, and Lyctus brunneus or the like of Lyctidae.
(616) Examples of the Diptera pests include Tipula aino or the like of Tipulidae, Plecia nearctica or the like of Bibionidae, Exechia shiitakevora or the like of Mycetophidae, Pnyxiascabiei, Bradysia agrestis, or the like of Sciaridae, Asphondylia yushimai, Mayetiola destructor, Dasineura oxycoccana, or the like of Cecidomyiidae, Aedes aegypti, Culex pipiens pallens, or the like of Culicidae, Simulium takahashii or the like of Simuliidae, Chironomus oryzae or the like of Chironomidae, Chrysops suavis, Tabanus trigonus, or the like of Tabanidae, Eumerus strigatus or the like of Syrphidae, Bactrocera dorsalis, Euphranta japonica, Ceratitis capitata, or the like of Tephritidae, Liriomyza trifolii, Liriomyza sativae, Agromyza oryzae, Liriomyza bryoniae, Chromatomyia horticola, Liriomyza chinensis, Liriomyza trifolii, or the like of Agromyzidae, Meromyza nigriventris or the like of Chloropidae, Drosophila suzukii, Drosophila melanogaster, or the like of Drosophilidae, Hydrellia griseola or the like of Ephydridae, Hippobosca equina or the like of Hippoboscidae, Parallelpmma sasakawae or the like of Scatophagidae, Delia antiqua, Delia platura, or the like of Anthomyiidae, Fannia canicularis or the like of Fanniidae, Musca domestica, Stomoxys calcitrans or the like of Muscidae, Sarcophaga peregrina or the like of Sarcophagidae, Gasterophilus intestinalis or the like of Gasterophilidae, Hypoderma lineatum or the like of Hypodermatidae, and Oestrus ovis or the like of Oestridae.
(617) Examples of the Lepidoptera pests include Endoclita excrescens or the like of Hepialidae, Antispila ampelopsia or the like of Heliozelidae, Zeuzera leuconotum, Cossus insularis, or the like of Cossidae, Archips fuscocupreanus, Adoxophyes orana fasciata, Grapholita molesta, Homona magnanima, Leguminivora glycinivorella, Cydia pomonella, Lobesia botrana, or the like of Tortricidae, Eupoecilia ambiguella or the like of Cochylidae, Bambalina sp., Eumeta minuscula, or the like of Psychidae, Nemapogon granella, Tinea translucens, or the like of Tineidae, Bucculatrix pyrivorella or the like of Bucculatricidae, Lyonetia clerkella, Lyonetiaprunifoliella malinella, or the like of Lyonetiidae, Caloptilia theivora, Phyllonorycter ringoniella, or the like of Gracilariidae, Phyllocnistis citrella or the like of Phyllocnistidae, Acrolepiopsis sapporensis or the like of Acrolepiidae, Plutella xylostella of Plutellidae, Yponomeuta orientalis, or the like of Yponomeutidae, Argyresthia conjugella or the like of Argyresthidae, Nokona regalis, Synanthedin hector or the like of Sesidae, Phthorimaea operculella, Sitotroga cerealella, Pectinophora gossypiella, Tuta absoluta, or the like of Gelechiidae, Carposina sasakii or the like of Carposinidae, Illiberis pruni or the like of Zygaenidae, Monema flavescens or the like of Limacodidae, Ancylolomia japonica, Chilo suppressalis, Cnaphalocrocis medinalis, Ostrinia furnacalis, Hellulla undalis, Conogethes punctiferlis, Diaphania indica, Parapediasia teterrella, Ostrinia nubilalis, or the like of Crambidae, Diatraea saccharalis, Cadra cautella, Galleria mellonella, or the like of Pyralidae, Nippoptilia vitis or the like of Pterophoridae, Papilio xuthus or the like of Papilionidae, Pieris rapae or the like of Pieridae, Parnara guttata or the like of Hesperiidae, Ascotis selenaria or the like of Geometridae, Dendrolimus spectabilis, Malacosoma neustrium testaceum, or the like of Lasiocampidae, Agrius convolvuli or the like of Sphingidae, Ama pseudoconspersa, Orygia recens approximans, Lymantria dispar, or the like of Lymantriidae, Hyphantria cunea or the like of Arctiidae, and Agrotis ipsilon, Agrotis segetum, Autographa nigrisigna, Helicoverpa armigera, Helicoverpa zea, Heliothis virescens, Spodoptera exigua, Spodoptera litura, Chrysodeix includens, Spodoptera frugiperda, Nephelodes minians, or the like of Noctuidae.
(618) Examples of the Hymenoptera pests include Arge pagana or the like of Argidae, Apethymus kuri, Athalia rosae ruficomis, or the like of Tenthredinidae, Dryocosmus kuriphilus, or the like of Cynipidae, Vespa simillima xanthoptera or the like of Vespidae, Solenopsis invicta, Linepithema humile, or the like of Formicidae, and Megachile nipponica or the like of Megachilidae.
(619) Examples of the Collembola pests include Bourletiellahortensis or the like of Sminthuridae.
(620) Examples of the Thysanura pests include Lepisma saccharina, Ctenolepisma villosa, or the like of Lepismatidae.
(621) Examples of the Blattodea pests include Periplaneta americana of Blattidae, and Blattella germanica or the like of Blattellidae.
(622) Examples of the Isoptera pests include Incisitermes minor or the like of Kalotermitidae, Coptotermes formosanus or the like of Rhinotermitidae, and Odontotermes formosanus or the like of Termitidae.
(623) Examples of the Psocoptera pests include Trogium pulsatorium or the like of Trogiidae, and Liposcelis corrodens or the like of Liposcelididae.
(624) Examples of the Dermaptera pests include Labodura riparia or the like of Labiduridae.
(625) Examples of the Mallophaga pests include Lipeurus caponis or the like of Menoponidae, and Damalinia bovis or the like of Trichodectidae.
(626) Examples of the Anoplura pests include Haematopinus suis or the like of Haematopinidae, Pediculus humanus or the like of Pediculine, Linognathus setosus or the like of Linognathidae, and Pthirus pubis or the like of Pthiridae
(627) Examples of the Acari pests include Penthaleus major or the like of Eupodidae, Phytonemus pallidus, Polyphagotarsonemus latus, or the like of Tarsonemidae, one species of Siteroptes sp. or the like of Pyemotidae, Brevipalpus lewisi or the like of Tenuipalpidae, Tuckerella pavoniformis or the like of Tuckerellidae, Eotetranychusboreus, Panonychus citri, Panonychus ulmi, Tetranychus urticae, Tetranychus kanzawai, or the like of Tetranychidae, Trisetacus pini or the like of Nalepellidae, Aculops pelekassi, Epitrimerus pyri, Phyllocoptruta oleivora, Aculops lycopersici, or the like of Eriophyidae, Diptacus crenatae or the like of Diptilomiopida, Aleuroglyphus ovatus, Tyrophagus putrescentiae, or Rhizoglyphus robini of Acaridae, Varroa jacobsoni or the like of Varroidae, Dermanyssus gallinae or the like of Dermanyssidae, Ornithonyssus sylvialum or the like of Macronyssidae, Boophilus microplus, Rhipicephalus sanguineus, Haemaphysalis longicornis, or the like of Ixodidae, and Sarcoptes scabiei or the like of Sarcoptidae.
(628) Examples of the plant parasitic nematoda, include Xiphinema index or the like of Longidoridae, Paratrichodorus minor or the like of Trichodoridae, one species of Rhabditidae (Rhabditella sp.) or the like, one species of Tylenchidae (Aglenchus sp.) or the like, one species of Tylodoridae (Cephalenchus sp.) or the like, Nothotylenchus acris, Ditylenchus destructor, or the like of Anguinidae, Rotylenchulus reniformis, Helicotylenchus dihystera, or the like of Hoplolaimidae, Paratylenchus curvitatus or the like of Paratylenchidae, Meloidogyne incognita, Meloidogyne hapla, Meloidogyne javanica, Meloidogyne arenaria, Melidogyne chitwoodi, Meloidogyne fallax or the like of Meloidogynidae, Globodera rostochiensis, Globodera pallida, Heterodera glycines or the like of Heteroderidae, Tylenchorhynchus claytoni or the like of Telotylenchidae, one species of Psilenchidae (Psilenchus sp.) or the like, one species of Criconematidae (Criconemoides sp.) or the like, Tylenchulus semipenetrans or the like of Tylenchulidae, Sphaeronema camelliae or the like of Sphaeronematidae, Sphaeronema camelliae, Radopholus citrophilus, Radopholus similis, Nacobbus aberrans, Pratylenchus penetrans, Pratylenchus coffeae, Platylechus zeae, Platylenchus brachyurus or the like of Pratylenchidae, Iotonchium ungulatum or the like of Iotonchiidae, Aphelenchus avenae or the like of Aphelenchidae, Aphelenchoides besseyi, Aphelenchoides fragariae, or the like of Aphelenchoididae, and Bursaphelenchus xylophilus or the like ofPalasitaphelenchidae.
(629) Examples of the plant parasitic mollusks include Pomacea canaliculata or the like of Pilidae, Leavicaulis alte or the like of Veronicellidae, Achatina fulica or the like of Achatinidae, Meghimatium bilineatum or the like of Philomycidae, Succinealauta or the like of Succineidae, Discus pauper or the like of Didcidae, Zonitoides yessoensis or the like of Zonitidae, Limax flavus, Lehmannia valentiana, Deroceras reticulatum, or the like of Limacidae, Parakaliella harimensis or the like of Helicarionidae, and Acusta despecta sieboldiana, Bradybaena similaris, or the like of Bradybaenidae.
(630) Examples of pests such as harmful animals, uncomfortable animals, sanitary insects, livestock insects, and parasites include Procambarus clarkii or the like of Decapoda Astacidae, Porcellio scaber or the like of Isopoda Porcellionidae, Chilopoda pests such as Scutigeromorpha Sutigeridae, Scolopendra subspinipes, or the like, Diplopoda pests such as Oxidus gracilis, Theridiidae hasseltii or the like of Araneae Latrodectus hasseltii, Chiracanthium japonicum, or the like of Clubionidae, Androctonus crassicauda or the like of Scorpiones, roundworm endoparasites such as Ascaris lumbricoides or the like, Syphacia sp. or the like, and Wuchereria bancrofti or the like, and flatworm endoparasites such as Distomum sp., Paragonimus westermanii, Metagonimus yokokawai, Schistosoma japonicum, Taenia solium, Taeniarhynchus saginatus, Echinococcus sp., or Diphyllobothrium latum.
(631) The present pest control agent exhibits a controlling effect also on the pests and the like exemplified above that have acquired the resistance to existing pest control agents. Furthermore, the present pest control agent can be applied to plants that have acquired characteristics such as pest tolerance, disease tolerance, herbicide tolerance, or the like by gene recombination, artificial mating, or the like.
(632) The plant provided with tolerance by a breeding method or a gene recombination technique in the present invention includes plants provided with tolerance by new plant breeding techniques (NBTs) established by combining molecular biological techniques with existing mating techniques, as well as those provided with tolerance by classical mating, or by gene recombinant techniques. The new plant breeding techniques (NBTs) are described in the publication Atarashii syokubutu ikusyu wo rikaishiyo (Kokusai bunken sha, written by Ryo OSAWA, and Hiroshi EZURA), the review Genome Editing Tools in Plants (Genes 2017, 8, 399, written by Tapan Kumar Mohanta, Tufail Bashir, Abeer Hashem, Elsayed Fathi Abd Allah and Hanhong Bae), and so on.
(633) Next, the production methods, formulation methods and applications of the present compound will be described in detail by way of Examples. However, the present invention is in no way restricted by these Examples. The melting point which is a physical property value of the present compound was determined by a MP-500V micro melting point measuring apparatus available from Yanaco. The refractive index was determined by using an Abbe refractometer available from ATAGO CO., LTD. .sup.1H NMR spectrum was determined by using JNM-LA400 (400 MHz), JNM-LA300 (300 MHz) or JNM-ECS300 (300 MHz) available from JEOL Ltd. and tetramethylsilane (TMS) as the internal standard.
(634) Methods for producing production intermediates of the present compound are also described.
EXAMPLES
Example 1
Production of 1-(pyridine-3-yl)-4-[2-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxamide (Present Compound Number: A-0044)
1) Ethyl 4-{[(nonafluorobutyl)sulfonyl]oxy}-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (Present Compound Number: D-0008)
(635) Ethyl 4-hydroxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (15.0 g, 64.3 mmol) synthesized by the method described in Reference examples 1 and 2 of WO 2016/027790 A, triethylamine (13.0 g, 128.5 mmol), and nanofluorobutanesulfonic acid fluoride (27.2 g, 90.0 mmol) were sequentially added into dichloromethane (300 mL) under ice-cooling, and stirred overnight at room temperature. The reaction solution was poured into saturated brine, and extracted with dichloromethane. The obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was washed with diisopropyl ether to give ethyl 4-{[(nonafluorobutyl)sulfonyl]oxy}-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (29.0 g, yield: 88%).
(636) Melting point: 103-104? C.
(637) .sup.1H-NMR data (400 MHz, CDCl.sub.3/TMS ? (ppm)): 1.44 (3H, t), 4.50 (2H, q), 7.48 (1H, dd), 8.08 (1H, s), 8.15 (1H, dd), 8.70 (1H, d), 8.99 (1H, d)
2) Ethyl 1-(pyridine-3-yl)-4-(2-(trifluoromethyl)phenyl)-1H-pyrazole-3-carboxylate (Present Compound Number: C-0044)
(638) Ethyl 4-{[(nonafluorobutyl)sulfonyl]oxy}-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (4.0 g, 7.8 mmol), 2-(trifluoromethyl)phenylboronic acid (2.4 g, 12.6 mmol), sodium carbonate (2.7 g, 25.5 mmol), and tetrakis(triphenylphosphine) palladium (0.45 g, 0.39 mmol) were added to a mixed solvent of tetrahydrofuran (30 mL) and water (6 mL), and refluxed under heating for 5 hours in a nitrogen atmosphere. After end of the reaction, the reaction solution was poured into saturated brine, and extracted with ethyl acetate. The obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography, to give ethyl 1-(pyridine-3-yl)-4-[2-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxylate (2.6 g, yield: 93%).
(639) Melting point: 131-134? C.
(640) .sup.1H-NMR data (400 MHz, CDCl.sub.3/TMS ? (ppm)): 1.13 (3H, t), 4.24 (2H, q), 7.30-7.70 (4H, m), 7.77 (1H, d), 7.98 (1H, s), 8.21 (1H, ddd), 8.65 (1H, dd), 9.04 (1H, d)
3) 1-(pyridine-3-yl)-4-[2-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxamide (Present Compound Number: A-0044)
(641) Ethyl 1-(pyridine-3-yl)-4-[2-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxylate (2.5 g, 6.9 mmol) was dissolved in ethanol (30 mL), and sodium hydroxide (0.84 g, 21.0 mmol) and water (5.0 mL) were added at room temperature, and further, the resultant solution was heated to 40? C. with an oil bath and stirred for 1 hour. The solvent of the reaction solution was distilled off under reduced pressure, and 6 N hydrochloric acid was added to the residue, and the precipitated solid was filtered off, and dried to give crude 1-(pyridine-3-yl)-4-[2-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxylic acid. The obtained 1-(pyridine-3-yl)-4-[2-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxylic acid was dissolved in dichloromethane (50 mL), and oxalyl chloride (5.9 g, 46.5 mmol) and N,N-dimethylformamide (catalytic amount) were added, and allowed to react at room temperature for 1 hour. The solvent was distilled off under reduced pressure, and the residue was dissolved in tetrahydrofuran (10 mL). The solution was then added to a mixed solution of tetrahydrofuran (20 mL) and aqueous ammonia (content: 28%, 10 mL) at 0? C., and then stirred at room temperature for 1 hour. The solvent of the reaction solution was distilled off under reduced pressure. The residue was washed sequentially with water and 2-propanol, and the obtained crude product was recrystallized in chloroform to give 1-(pyridine-3-yl)-4-[2-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxamide (1.1 g, yield: 48%).
(642) Melting point: 178-181? C.
(643) .sup.1H-NMR data (400 MHz, CDCl.sub.3/TMS ? (ppm)): 5.34 (1H, brs), 6.79 (1H, brs), 7.44-7.61 (4H, m), 7.75 (1H, d), 7.96 (1H, s), 8.09 (1H, dd), 8.64 (1H, d), 9.04 (1H, d)
Example 2
Production of 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (Present Compound Number: B-100)
1) Ethyl 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (Present Compound Number: D-0108)
(644) Ethyl 4-{[(nonafluorobutyl)sulfonyl]oxy}-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (3.4 g, 6.6 mmol), 4-(methylpyridine-3-yl)boronic acid (1.0 g, 7.3 mmol), sodium carbonate (1.6 g, 15.1 mmol), and tetrakis(triphenylphosphine) palladium (0.38 g, 0.33 mmol) were added to a mixed solvent of 1,2-dimethoxyethane (30 mL) and water (6 mL), and refluxed under heating for 9 hours in a nitrogen atmosphere. After end of the reaction, the reaction solution was poured into saturated brine, and extracted with ethyl acetate. The obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography, to give ethyl 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (1.3 g, yield: 64%).
(645) Melting point: 120-123? C.
(646) .sup.1H-NMR data (300 MHz, CDCl.sub.3/TMS ? (ppm)): 1.20 (3H, t), 2.24 (3H, s), 4.28 (2H, q), 7.21 (1H, d), 7.47 (1H, dd), 7.96 (1H, s), 8.21 (1H, ddd), 8.41 (1H, s), 8.48 (1H, dd), 8.65 (1H, dd), 9.05 (1H, d)
2) 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylic acid (Present Compound Number: F-0108)
(647) Ethyl 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (1.2 g, 3.9 mmol) was dissolved in ethanol (15 mL), and sodium hydroxide (0.47 g, 11.8 mmol) and water (3.0 mL) were added at room temperature, and stirred for 1 hour. The solvent of the reaction solution was distilled off under reduced pressure, and 6 N hydrochloric acid was added to the residue, and the precipitated solid was filtered off, and washed with water and hexane, and dried to give 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylic acid (0.8 g, yield: 73%).
(648) Melting point: 277-280? C.
(649) .sup.1H-NMR data (300 MHz, DMSO-d.sub.6/TMS ? (ppm)): 2.05 (3H, s), 7.29 (1H, d), 7.58 (1H, dd), 8.30 (1H, dd), 8.34 (1H, s), 8.39 (1H, d), 8.59 (1H, d), 8.80 (1H, s), 9.15 (1H, d)
3) 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (Present Compound Number: B-0100)
(650) 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylic acid (0.20 g, 0.71 mmol) was dissolved in N,N-dimethylformamide (5.0 mL), and ammonium chloride (0.076 g, 1.4 mmol), 1-hydroxybenzotriazole (0.12 g, 0.89 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (0.20 g, 1.0 mol), and triethylamine (0.15 g, 1.5 mmol) were added, and the mixture was allowed to react at room temperature for 2 hours. The reaction solution was poured into a saturated aqueous solution of sodium hydrogen carbonate, and the solid was filtered off, and washed sequentially with water and n-hexane, to give 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (0.16 g, yield: 80%).
(651) Melting point: 264-267? C.
(652) .sup.1H-NMR data (400 MHz, DMSO-d.sub.6/TMS ? (ppm)): 2.22 (3H, s) 7.30 (1H, d), 7.43 (1H, brs), 7.62 (1H, dd), 7.87 (1H, brs), 8.37 (1H, s), 8.38-8.45 (2H, m), 8.61 (1H, d), 8.80 (1H, s), 9.28 (1H, d)
Example 3
Production of 4-(4-chloro-2-methoxyphenyl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (Present Compound Number: A-0634)
1) Ethyl 4-(4-chloro-2-methoxyphenyl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (Present Compound Number: C-0634)
(653) Ethyl 4-{[(nonafluorobutyl)sulfonyl]oxy}-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (0.42 g, 0.82 mmol), 4-chloro-2-methoxyphenylboronic acid (0.20 g, 1.1 mmol), sodium carbonate (0.19 g, 1.8 mmol), and tetrakis(triphenylphosphine) palladium (0.050 g, mmol) were added to a mixed solvent of tetrahydrofuran (5.0 mL) and water (0.50 mL), and refluxed under heating for 3 hours in a nitrogen atmosphere. After end of the reaction, the reaction solution was poured into saturated brine, and extracted with ethyl acetate. The obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography, to give ethyl 4-(4-chloro-2-methoxyphenyl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (0.25 g, yield: 86%).
(654) Melting point: 133-134? C.
(655) .sup.1H-NMR data (300 MHz, CDCl.sub.3/TMS ? (ppm)): 1.27 (3H, t), 3.78 (3H, s), 4.32 (2H, q), 6.94 (1H, d), 7.00 (1H, dd), 7.26 (1H, d), 7.44 (1H, dd), 7.99 (1H, s), 8.17 (1H, ddd), 8.61 (1H, dd), 9.02 (1H, d)
2) 4-(4-chloro-2-methoxyphenyl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (Present Compound Number: A-0634)
(656) Ethyl 4-(4-chloro-2-methoxyphenyl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (0.15 g, 0.42 mmol) was dissolved in a 7 M ammonia solution in methanol (20 mL), and stirred at room temperature for 2 days. Further, a 7 M ammonia solution in methanol (30 mL) was added to the reaction solution, and stirred at room temperature for 3 days. The solvent of the reaction solution was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to give 4-(4-chloro-2-methoxyphenyl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (0.12 g, yield: 87%).
(657) Melting point: 192-194? C.
(658) .sup.1H-NMR data (300 MHz, CDCl.sub.3/TMS ? (ppm)): 3.81 (3H, s), 5.44 (1H, brs), 6.77 (1H, brs), 6.94 (1H, d), 6.99 (1H, dd), 7.40 (1H, d), 7.42-7.48 (1H, m), 8.05 (1H, s), 8.05-8.11 (1H, m), 8.57-8.67 (1H, m), 8.98-9.09 (1H, m)
Example 4
Production of ethyl 4-iodo-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (Present Compound Number: D-0003)
(659) Ethyl 1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (0.92 g, 4.2 mmol) was dissolved in acetonitrile (10 mL), and iodine (1.1 g, 4.3 mmol) and ammonium hexanitratocerate (IV) (2.4 g, 4.3 mmol) were added, and refluxed under heating for 10 hours. After end of the reaction, a saturated aqueous solution of sodium thiosulfate was added to the reaction solution, and extracted with ethyl acetate. The obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to give ethyl 4-iodo-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (0.75 g, yield: 52%).
(660) Melting point 128-130? C.
(661) .sup.1H-NMR data (300 MHz, CDCl.sub.3/TMS ? (ppm)): 1.44 (3H, t), 4.47 (2H, q), 7.45 (1H, dd), 8.07 (1H, s), 8.10 (1H, ddd), 8.64 (1H, dd), 8.97 (1H, d)
Example 5
Production of 3-[3-carbamoyl-4-(2-methylphenyl)-1H-pyrazole-1-yl]pyridine-1-oxide (Present Compound Number: A-8862)
(662) In chloroform (50 mL), 1-(pyridine-3-yl)-4-(2-methylphenyl)-1H-pyrazole-3-carboxamide (present compound number: A-0020; 0.30 g, 1.1 mmol) was dissolved, and m-chloroperbenzoic acid (content: 77%, 0.48 g, 2.1 mmol) was added, and refluxed under heating for 2 hours. After end of the reaction, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to give 3-[3-carbamoyl-4-(2-methylphenyl)-1H-pyrazole-1-yl]pyridine-1-oxide (0.31 g, yield: 98%).
(663) .sup.1H-NMR data (400 MHz, CDCl.sub.3/TMS ? (ppm)): 2.24 (3H, s), 5.39 (1H, brs), 6.63 (1H, brs), 7.23-7.34 (4H, m), 7.40 (1H, dd), 7.62 (1H, d), 7.84 (1H, s), 8.19 (1H, d), 8.81 (1H, s)
Example 6
Production of 4-(3-methylpyridine-2-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (Present Compound Number: B-0027)
1) Ethyl 4-(3-methylpyridine-2-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (Present Compound Number: D-0035)
(664) Ethyl 4-{[(nonafluorobutyl)sulfonyl]oxy}-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (3.1 g, 6.0 mmol), bis(pinacolato)diboron (2.3 g, 9.1 mmol), potassium acetate (1.8 g, 18.3 mmol), and [1,1-bis(diphenylphosphino)ferrocene]palladium dichloride dichloromethane adduct (0.49 g, 0.60 mmol) were dissolved in N,N-dimethylformamide (60 mL), and heated to 90? C. and stirred for 4 hours in a nitrogen atmosphere by using an oil bath. After end of the reaction, the reaction solution was poured into saturated brine, and extracted with ethyl acetate. The obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. Further, silica gel column chromatography was conducted to give crude (3-(ethoxycarbonyl)-1-(pyridine-3-yl)-1H-pyrazole-4-yl)boronic acid. The obtained (3-(ethoxycarbonyl)-1-(pyridine-3-yl)-1H-pyrazole-4-yl)boronic acid was dissolved in a mixed solvent of tetrahydrofuran (15 mL) and water (3 mL), and 2-bromo-3-methylpyridine (0.44 g, 2.6 mmol), sodium carbonate (0.53 g, 5.0 mmol), and tetrakis(triphenylphosphine)palladium (0.25 g, 0.22 mmol) were added, and refluxed under heating for 1 hour in a nitrogen atmosphere. After end of the reaction, the reaction solution was poured into saturated brine, and extracted with ethyl acetate. The obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography, to give ethyl 4-(3-methylpyridine-2-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (0.74 g, yield; 40%).
(665) Melting point: 97-100? C.
(666) .sup.1H-NMR data (400 MHz, DMSO/TMS ? (ppm)): 0.86 (3H, t), 2.25 (3H, s), 4.19 (2H, q), 7.31 (1H, dd), 7.64 (1H, dd), 7.71 (1H, d), 8.30-8.39 (1H, m), 8.40 (1H, d), 8.64 (1H, d), 8.90 (1H, s), 9.19 (1H, d)
2) 4-(3-methylpyridine-2-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (Present Compound Number: B-0027)
(667) Ethyl 4-(3-methylpyridine-2-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (0.69 g, 2.2 mmol) was dissolved in ethanol (15 mL), and sodium hydroxide (0.27 g, 6.8 mmol) and water (3.0 mL) were added at room temperature, and stirred for 2 hours. The solvent of the reaction solution was distilled off under reduced pressure, and the residue was dissolved in water, and 2N hydrochloric acid was added to adjust the pH to 4 to 7. Further, water was distilled off under reduced pressure to give crude 4-(3-methylpyridine-2-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylic acid. The obtained 4-(3-methylpyridine-2-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylic acid was dissolved in N,N-dimethylformamide (10 mL), and ammonium chloride (0.24 g, 4.5 mmol), 1-hydroxybenzotriazole (0.36 g, 2.7 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (0.64 g, 3.3 mol) and triethylamine (1.1 g, 10.9 mmol) were added, and allowed to react at room temperature for 2 hours. The reaction solution was poured into a saturated aqueous solution of sodium hydrogen carbonate, and extracted with ethyl acetate. The obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. Ethyl acetate and hexane were added to the residue, and the precipitated solid was washed with ethyl acetate and hexane, to give 4-(3-methylpyridine-2-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (0.11 g, yield; 18%).
(668) Melting point: 145-148? C.
(669) .sup.1H-NMR data (400 MHz, DMSO/TMS ? (ppm)): 2.22 (3H, s), 7.28 (1H, dd), 7.40 (1H, s), 7.60 (1H, dd), 7.67 (1H, d), 7.90 (1H, s), 8.35-8.43 (2H, m), 8.60 (1H, d), 8.80 (1H, s), 9.27 (1H, d)
Example 7
Production of ethyl 1-(pyridine-3-yl)-4-(2-methylphenyl)-1H-pyrazole-3-carbonyl carbamate (Present Compound Number: A-5414)
(670) In oxalyl chloride (15 g, 118 mmol), 1-(pyridine-3-yl)-4-(2-methylphenyl)-1H-pyrazole-3-carboxamide (present compound number: A-0020; 0.50 g, 1.8 mmol) was dissolved, and the resultant solution was refluxed under heating for 10 minutes. Oxalyl chloride was distilled off under reduced pressure, and the residue was dissolved in ethanol (7.9 g, 171 mmol), and stirred at room temperature for 10 minutes. After end of the reaction, the reaction solution was poured into a saturated aqueous solution of sodium hydrogen carbonate, and extracted with ethyl acetate. The obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography, to give ethyl 1-(pyridine-3-yl)-4-(2-methylphenyl)-1H-pyrazole-3-carbonyl carbamate (0.18 g, yield: 29%).
(671) .sup.1H-NMR data (300 MHz, CDCl.sub.3/TMS ? (ppm)): 1.40 (3H, t), 2.22 (3H, s), 4.41 (2H, q), 7.13-7.37 (4H, m), 7.51 (1H, dd), 7.97 (1H, s), 8.14 (1H, dd), 8.68 (1H, d), 9.07 (1H, d), 10.75 (1H, s)
Example 8
Production of N-(2-methoxyacetyl)-1-(pyridine-3-yl)-4-(2-methylphenyl)-1H-pyrazole-3-carboxamide (Present Compound Number: A-4808)
(672) In toluene (5 mL), 1-(pyridine-3-yl)-4-(2-methylphenyl)-1H-pyrazole-3-carboxamide (present compound number: A-0020; 0.20 g, 0.72 mmol) was dissolved, and 2-methoxyacetyl chloride (0.17 g, 1.6 mmol) was added and refluxed under heating for 2 hours. The reaction solution was poured into water and extraction with ethyl acetate was conducted. The obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography, to give N-(2-methoxyacetyl)-1-(pyridine-3-yl)-4-(2-methylphenyl)-1H-pyrazole-3-carboxamide (0.080 g, yield: 32%).
(673) .sup.1H-NMR data (300 MHz, CDCl.sub.3/TMS ? (ppm)): 2.24 (3H, s), 3.50 (3H, s), 4.42 (2H, s), 7.23-7.37 (4H, m), 7.52 (1H, dd), 8.00 (1H, s), 8.14 (1H, dd), 8.69 (1H, d), 9.06 (1H, d), 9.89 (1H, s)
Example 9
Production of 1-(pyridine-3-yl)-4-(2-methylphenyl)-1H-pyrazole-3-carbothioamide (Present Compound Number: A-8646)
(674) In 1,4-dioxane (10 mL), 1-(pyridine-3-yl)-4-(2-methylphenyl)-1H-pyrazole-3-carboxamide (present compound number: A-0020; 0.70 g, 2.5 mmol) was dissolved, and Lawesson's reagent (1.2 g, 3.0 mmol) was added and stirred at 80? C. for 40 minutes. After end of the reaction, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography, to give 1-(pyridine-3-yl)-4-(2-methylphenyl)-1H-pyrazole-3-carbothioamide (0.66 g, yield: 89%).
(675) .sup.1H-NMR data (400 MHz, CDCl.sub.3/TMS ? (ppm)): 2.24 (3H, s), 7.22-7.38 (5H, m), 7.47 (1H, dd), 7.90 (1H, s), 8.00 (1H, s), 8.12 (1H, dd), 8.64 (1H, d), 9.06 (1H, d)
(676) Physical property values, including those in the above-described examples, of the present compound [I] synthesized in accordance with the above-described examples are shown in the following Table 315 to Table 323, and physical property values of the present compound [II] are similarly shown in the following Table 324 to Table 334. The compound numbers and the signs in Tables are as defined above.
(677) TABLE-US-00315 TABLE 315 compound physical property value A-0001 melting point (? C.) 161-163 A-0002 melting point (? C.) 183-185 A-0003 melting point (? C.) 204-207 A-0004 melting point (? C.) 203-206 A-0005 melting point (? C.) 164-166 A-0006 melting point (? C.) 169-172 A-0007 melting point (? C.) 203-206 A-0008 melting point (? C.) 171-174 A-0014 melting point (? C.) 171-174 A-0020 melting point (? C.) 181-184 A-0021 melting point (? C.) 170-173 A-0022 melting point (? C.) 177-179 A-0023 melting point (? C.) 166-168 A-0025 melting point (? C.) 170-173 A-0029 melting point (? C.) 192-194 A-0041 melting point (? C.) 188-190 A-0044 melting point (? C.) 178-181 A-0045 melting point (? C.) 179-181 A-0046 melting point (? C.) 205-208 A-0047 melting point (? C.) 202-205 A-0059 melting point (? C.) 140-143 A-0086 melting point (? C.) 145-147 A-0101 melting point (? C.) 162-165 A-0103 melting point (? C.) 205-208 A-0119 melting point (? C.) 177-179 A-0120 melting point (? C.) 123-126 A-0121 melting point (? C.) 168-171 A-0122 melting point (? C.) 205-207 A-0123 melting point (? C.) 170-173 A-0124 melting point (? C.) 190-193 A-0125 melting point (? C.) 169-170 A-0128 melting point (? C.) 190-193 A-0134 melting point (? C.) 129-132 A-0137 melting point (? C.) 147-149 A-0143 melting point (? C.) 154-157 A-0144 melting point (? C.) 160-162 A-0145 melting point (? C.) 182-183 A-0146 melting point (? C.) 163-166 A-0147 melting point (? C.) 150-153 A-0148 melting point (? C.) 190-192 A-0152 melting point (? C.) 193-196
(678) TABLE-US-00316 TABLE 316 compound physical property value A-0176 melting point (? C.) 126-128 A-0177 melting point (? C.) 138-141 A-0179 melting point (? C.) 127-130 A-0183 melting point (? C.) 183-185 A-0185 melting point (? C.) 201-202 A-0186 melting point (? C.) 186-188 A-0188 melting point (? C.) 204-206 A-0189 melting point (? C.) 167-170 A-0192 melting point (? C.) 250-253 A-0198 melting point (? C.) 157-160 A-0227 melting point (? C.) 200-202 A-0239 melting point (? C.) 226-229 A-0242 melting point (? C.) 297-300 A-0260 melting point (? C.) 155-157 A-0263 melting point (? C.) 180-182 A-0266 melting point (? C.) 147-150 A-0269 melting point (? C.) 200-203 A-0320 melting point (? C.) 196-199 A-0329 melting point (? C.) 173-175 A-0338 melting point (? C.) 185-188 A-0340 melting point (? C.) 218-221 A-0347 melting point (? C.) 190-193 A-0512 melting point (? C.) 163-166 A-0521 melting point (? C.) 245-248 A-0524 melting point (? C.) 237-240 A-0542 melting point (? C.) 243-245 A-0548 melting point (? C.) 195-198 A-0549 melting point (? C.) 263-266 A-0550 melting point (? C.) 197-200 A-0551 melting point (? C.) 239-242 A-0553 melting point (? C.) 297-300 A-0555 melting point (? C.) 202-205 A-0557 melting point (? C.) 199-202 A-0561 melting point (? C.) 239-242 A-0563 melting point (? C.) 176-178 A-0571 melting point (? C.) 170-173 A-0573 melting point (? C.) 177-178 A-0574 melting point (? C.) 170-173 A-0577 melting point (? C.) 147-150 A-0578 melting point (? C.) 195-198 A-0582 melting point (? C.) 170-173
(679) TABLE-US-00317 TABLE 317 compound physical property value A-0583 melting point (? C.) 186-188 A-0587 melting point (? C.) 203-206 A-0588 melting point (? C.) 213-216 A-0591 melting point (? C.) 196-199 A-0593 melting point (? C.) 127-130 A-0594 melting point (? C.) 90-93 A-0597 melting point (? C.) 170-173 A-0598 melting point (? C.) 202-203 A-0600 melting point (? C.) 214-216 A-0603 melting point (? C.) 216-219 A-0608 melting point (? C.) 167-170 A-0609 melting point (? C.) 215-218 A-0613 melting point (? C.) 167-170 A-0614 melting point (? C.) 197-198 A-0618 melting point (? C.) 195-198 A-0624 melting point (? C.) 209-212 A-0629 melting point (? C.) 203-206 A-0633 melting point (? C.) 200-203 A-0634 melting point (? C.) 192-194 A-0636 melting point (? C.) 163-166 A-0637 melting point (? C.) 179-182 A-0638 melting point (? C.) 113-116 A-0639 melting point (? C.) 220-223 A-0644 melting point (? C.) 171-174 A-0645 melting point (? C.) 194-196 A-0649 melting point (? C.) 156-159 A-0652 melting point (? C.) 175-178 A-0653 melting point (? C.) 213-216 A-0654 melting point (? C.) 145-148 A-0655 melting point (? C.) 154-157 A-0656 melting point (? C.) 144-147 A-0659 melting point (? C.) 141-144 A-0660 melting point (? C.) 210-213 A-0663 melting point (? C.) 213-216 A-0664 melting point (? C.) 143-146 A-0665 melting point (? C.) 253-256 A-0670 melting point (? C.) 192-195 A-0671 melting point (? C.) 206-209 A-0688 melting point (? C.) 144-147 A-0689 melting point (? C.) 161-163 A-0691 melting point (? C.) 165-168
(680) TABLE-US-00318 TABLE 318 compound physical property value A-0692 melting point (? C.) 150-153 A-0693 melting point (? C.) 165-166 A-0697 melting point (? C.) 160-163 A-0701 melting point (? C.) 171-173 A-0705 melting point (? C.) 156-159 A-0709 melting point (? C.) 150-153 A-0712 melting point (? C.) 173-175 A-0713 melting point (? C.) 113-115 A-0733 melting point (? C.) 183-186 A-0875 melting point (? C.) 220-223 A-0906 melting point (? C.) 177-180 A-0907 melting point (? C.) 188-190 A-0908 melting point (? C.) 194-197 A-0909 melting point (? C.) 137-140 A-0910 melting point (? C.) 186-189 A-0911 melting point (? C.) 230-233 A-0912 melting point (? C.) 196-198 A-0913 melting point (? C.) 160-162 A-1067 melting point (? C.) 225-227 A-1076 melting point (? C.) 145-148 A-1077 melting point (? C.) 198-201 A-1097 melting point (? C.) 233-236 A-1102 melting point (? C.) 256-258 A-1117 melting point (? C.) 209-211 A-1134 melting point (? C.) 205-208 A-1136 melting point (? C.) 222-225 A-1140 melting point (? C.) 180-183 A-1141 melting point (? C.) 131-134 A-1145 melting point (? C.) 155-157 A-1146 melting point (? C.) 183-184 A-1147 melting point (? C.) 193-196 A-1148 melting point (? C.) 166-167 A-1151 melting point (? C.) 206-208 A-1152 melting point (? C.) 127-130 A-1153 melting point (? C.) 173-175 A-1154 melting point (? C.) 172-174 A-1155 melting point (? C.) 133-136 A-1156 melting point (? C.) 156-159 A-1157 melting point (? C.) 171-174 A-1158 melting point (? C.) 180-183 A-1159 melting point (? C.) 169-171
(681) TABLE-US-00319 TABLE 319 compound physical property value A-1160 melting point (? C.) 184-187 A-1161 melting point (? C.) 140-143 A-1162 melting point (? C.) 85-88 A-1163 melting point (? C.) 167-170 A-1164 melting point (? C.) 167-170 A-1165 melting point (? C.) 200-203 A-1166 melting point (? C.) 130-133 A-1980 melting point (? C.) 90-93 A-2182 melting point (? C.) 136-139 A-2384 refractive index (n.sub.D.sup.20) 1.5741 A-2586 melting point (? C.) 157-160 A-2600 melting point (? C.) 139-141 A-2788 melting point (? C.) 110-113 A-2990 melting point (? C.) 157-160 A-3192 melting point (? C.) 153-156 A-3596 melting point (? C.) 90-93 A-3798 melting point (? C.) 159-161 A-3812 melting point (? C.) 103-106 A-4000 melting point (? C.) 172-174 A-4202 refractive index (n.sub.D.sup.20) 1.5991 A-4404 melting point (? C.) 140-143 A-4606 melting point (? C.) 166-168 A-5616 melting point (? C.) 97-100 A-6020 refractive index (n.sub.D.sup.20) 1.6006 A-6222 melting point (? C.) 132-134 A-6424 melting point (? C.) 200-203 A-6626 melting point (? C.) 217-219 A-7030 refractive index (n.sub.D.sup.20) 1.5688 A-7232 melting point (? C.) 204-206 A-7434 melting point (? C.) 136-139 A-7636 melting point (? C.) 117-120 A-7838 melting point (? C.) 150-152 A-8040 melting point (? C.) 129-132 A-8242 melting point (? C.) 120-123 A-8444 melting point (? C.) 75-78 A-8646 melting point (? C.) 134-135 A-8862 melting point (? C.) 147-150 A-9435 melting point (? C.) 236-239 A-9480 melting point (? C.) 176-179 A-9993 refractive index (n.sub.D.sup.20) 1.6292 A-9994 melting point (? C.) 72-75
(682) TABLE-US-00320 TABLE 320 compound physical property value hydrochloride of A-0593 melting point (? C.) 147-150
(683) TABLE-US-00321 TABLE 321 com- physical property value pound (.sup.1H-NMR data, in CDCl.sub.3 TMS ?(ppm)) A-0044 400 MHz 5.34 (1H, brs), 6.79 (1H, brs), 7.44-7.61 (4H, m), 7.75 (1H, d), 7.96 (1H, s), 8.09 (1H, dd), 8.64 (1H, d), 9.04 (1H, d) A-0182 300 MHz 2.66 (3H, s), 5.42 (1H, s), 6.90 (1H, s), 7.34 (1H, dd), 7.45-7.57 (2H, m), 7.64 (1H, dt), 8.02 (1H, s), 8.04-8.12 (2H, m), 8.66 (1H, dd), 9.07 (1H, d) A-0634 300 Mhz 3.81 (3H, s), 5.44 (1H, brs), 6.77 (1H, brs), 6.94 (1H, d), 6.99 (1H, dd), 7.40 (1H, d), 7.42-7.48 (1H, m), 8.05 (1H, s), 8.05-8.11 (1H, m), 8.57-8.67 (1H, m), 8.98-9.09 (1H, m)
(684) TABLE-US-00322 TABLE 322 compound physical property value B-0001 melting point (? C.) 194-197 B-0002 melting point (? C.) 193-196 B-0003 melting point (? C.) 210-213 B-0004 melting point (? C.) 214-217 B-0009 melting point (? C.) 175-178 B-0018 melting point (? C.) 245-248 B-0027 melting point (? C.) 145-148 B-0090 melting point (? C.) 254-257 B-0091 melting point (? C.) 262-264 B-0095 melting point (? C.) 241-243 B-0099 melting point (? C.) 188-191 B-0100 melting point (? C.) 264-267 B-0107 melting point (? C.) 235-237 B-0165 melting point (? C.) 217-220 B-0199 melting point (? C.) 244-247 B-0205 melting point (? C.) 224-227 B-0287 melting point (? C.) 178-180 B-0290 melting point (? C.) 137-140 B-0293 melting point (? C.) 185-188 B-0296 melting point (? C.) 140-143 B-0301 melting point (? C.) 166-168 B-0367 melting point (? C.) 233-236 B-0389 melting point (? C.) 242-245 B-0453 melting point (? C.) 201-204 B-0454 melting point (? C.) 180-183 B-0455 melting point (? C.) 167-170 B-0456 melting point (? C.) 197-200 B-0457 melting point (? C.) 230-233 B-0458 melting point (? C.) 270-273 B-0459 melting point (? C.) 253-255
(685) TABLE-US-00323 TABLE 323 com- physical property value pound (.sup.1H-NMR data, in DMSO-d6 TMS ?(ppm)) B-0100 400 MHz 2.22 (3H, s), 7.30 (1H, d), 7.43 (1H, brs), 7.62 (1H, dd), 7.87 (1H, brs), 8.37 (1H, s), 8.38-8.45 (2H, m), 8.61 (1H, d), 8.80 (1H, s), 9.28 (1H, d)
(686) TABLE-US-00324 TABLE 324 compound physical property value C-0001 melting point (? C.) 57-59 C-0003 melting point (? C.) 110-112 C-0004 melting point (? C.) 134-136 C-0005 melting point (? C.) 113-115 C-0006 melting point (? C.) 101-103 C-0007 melting point (? C.) 114-116 C-0008 melting point (? C.) 131-133 C-0020 refractive index (n.sub.D.sup.20) 1.6018 C-0021 refractive index (n.sub.D.sup.20) 1.6099 C-0022 melting point (? C.) 113-116 C-0023 melting point (? C.) 108-110 C-0025 refractive index (n.sub.D.sup.20) 1.6062 C-0029 melting point (? C.) 92-95 C-0041 melting point (? C.) 119-122 C-0044 melting point (? C.) 131-134 C-0045 melting point (? C.) 100-101 C-0046 melting point (? C.) 124-126 C-0047 melting point (? C.) 108-109 C-0086 melting point (? C.) 90-93 C-0119 refractive index (n.sub.D.sup.20) 1.5782 C-0120 melting point (? C.) 110-112 C-0121 melting point (? C.) 97-100 C-0122 refractive index (n.sub.D.sup.20) 1.5981 C-0124 melting point (? C.) 87-90 C-0125 refractive index (n.sub.D.sup.20) 1.5982 C-0128 refractive index (n.sub.D.sup.20) 1.5890 C-0134 refractive index (n.sub.D.sup.20) 1.5873 C-0137 refractive index (n.sub.D.sup.20) 1.5901 C-0143 melting point (? C.) 78-80 C-0144 melting point (? C.) 62-63 C-0145 melting point (? C.) 92-94 C-0147 melting point (? C.) 93-94 C-0152 refractive index (n.sub.D.sup.20) 1.5951 C-0176 melting point (? C.) 87-89 C-0179 melting point (? C.) 88-89 C-0182 melting point (? C.) 160-163 C-0183 melting point (? C.) 137-139 C-0186 melting point (? C.) 190-193 C-0198 melting point (? C.) 111-112 C-0227 melting point (? C.) 105-108 C-0239 melting point (? C.) 110-113
(687) TABLE-US-00325 TABLE 325 compound physical property value C-0263 refractive index (n.sub.D.sup.20) 1.5818 C-0266 refractive index (n.sub.D.sup.20) 1.5869 C-0269 melting point (? C.) 87-90 C-0320 melting point (? C.) 90-92 C-0329 melting point (? C.) 96-98 C-0338 melting point (? C.) 117-119 C-0340 melting point (? C.) 113-116 C-0512 refractive index (n.sub.D.sup.20) 1.6076 C-0518 melting point (? C.) 134-136 C-0520 melting point (? C.) 140-143 C-0549 melting point (? C.) 191-194 C-0550 melting point (? C.) 170-173 C-0553 melting point (? C.) 144-147 C-0555 melting point (? C.) 103-104 C-0557 melting point (? C.) 99-100 C-0561 melting point (? C.) 96-98 C-0563 melting point (? C.) 97-100 C-0571 melting point (? C.) 109-111 C-0573 melting point (? C.) 95-97 C-0574 melting point (? C.) 46-49 C-0577 melting point (? C.) 116-118 C-0578 melting point (? C.) 116-118 C-0587 melting point (? C.) 153-155 C-0588 melting point (? C.) 127-129 C-0591 melting point (? C.) 150-153 C-0593 melting point (? C.) 118-120 C-0594 refractive index (n.sub.D.sup.20) 1.5904 C-0597 melting point (? C.) 142-144 C-0598 melting point (? C.) 92-93 C-0600 melting point (? C.) 123-126 C-0608 refractive index (n.sub.D.sup.20) 1.5777 C-0613 melting point (? C.) 111-113 C-0614 refractive index (n.sub.D.sup.20) 1.6008 C-0624 melting point (? C.) 93-96 C-0629 refractive index (n.sub.D.sup.20) 1.5092 C-0633 melting point (? C.) 151-154 C-0634 melting point (? C.) 133-134 C-0636 melting point (? C.) 89-91 C-0637 melting point (? C.) 75-77 C-0638 refractive index (n.sub.D.sup.20) 1.6013 C-0639 refractive index (n.sub.D.sup.20) 1.5971
(688) TABLE-US-00326 TABLE 326 compound physical property value C-0644 melting point (? C.) 137-140 C-0652 melting point (? C.) 87-90 C-0653 refractive index (n.sub.D.sup.20) 1.6039 C-0655 refractive index (n.sub.D.sup.20) 1.5994 C-0656 melting point (? C.) 85-88 C-0659 melting point (? C.) 124-127 C-0660 melting point (? C.) 110-113 C-0663 refractive index (n.sub.D.sup.20) 1.6038 C-0664 refractive index (n.sub.D.sup.20) 1.6066 C-0670 refractive index (n.sub.D.sup.20) 1.5635 C-0692 refractive index (n.sub.D.sup.20) 1.5928 C-0697 refractive index (n.sub.D.sup.20) 1.5911 C-0705 refractive index (n.sub.D.sup.20) 1.5889 C-0712 melting point (? C.) 131-133 C-0906 melting point (? C.) 92-94 C-0907 refractive index (n.sub.D.sup.20) 1.5875 C-0908 melting point (? C.) 92-95 C-0910 refractive index (n.sub.D.sup.20) 1.5816 C-0911 refractive index (n.sub.D.sup.20) 1.5919 C-0912 refractive index (n.sub.D.sup.20) 1.5881 C-1067 melting point (? C.) 146-148 C-1097 melting point (? C.) 173-175 C-1102 melting point (? C.) 93-96 C-1117 melting point (? C.) 119-120 C-1136 melting point (? C.) 120-123 C-1140 refractive index (n.sub.D.sup.20) 1.5821 C-1141 melting point (? C.) 95-97 C-1145 melting point (? C.) 80-83 C-1148 melting point (? C.) 98-100 C-1152 melting point (? C.) 150-153 C-1155 melting point (? C.) 130-133 C-1156 melting point (? C.) 145-148 C-1162 melting point (? C.) 92-95 C-1163 refractive index (n.sub.D.sup.20) 1.5996 C-1165 melting point (? C.) 84-87
(689) TABLE-US-00327 TABLE 327 compound physical property value D-0002 melting point (? C.) 207-210 D-0003 melting point (? C.) 128-130 D-0004 melting point (? C.) 114-117 D-0005 melting point (? C.) 96-98 D-0008 melting point (? C.) 103-104 D-0012 melting point (? C.) 109-111 D-0035 melting point (? C.) 97-100 D-0098 melting point (? C.) 156-159 D-0099 melting point (? C.) 163-166 D-0103 melting point (? C.) 126-129 D-0107 melting point (? C.) 95-98 D-0108 melting point (? C.) 120-123 D-0115 melting point (? C.) 87-90 D-0207 melting point (? C.) 145-148 D-0213 melting point (? C.) 123-126 D-0295 melting point (? C.) 100-102 D-0301 melting point (? C.) 97-100 D-0309 melting point (? C.) 96-98 D-0375 melting point (? C.) 182-185 D-0464 melting point (? C.) 120-123 D-0466 melting point (? C.) 146-149
(690) TABLE-US-00328 TABLE 328 compound physical property value E-0002 melting point (? C.) 190-193 E-0003 melting point (? C.) 235-237 E-0004 melting point (? C.) 220-223 E-0005 melting point (? C.) 204-207 E-0006 melting point (? C.) 224-227 E-0007 melting point (? C.) 228-231 E-0008 melting point (? C.) 225-227 E-0020 melting point (? C.) 200-203 E-0021 melting point (? C.) 153-156 E-0022 melting point (? C.) 235-238 E-0023 melting point (? C.) 200-203 E-0025 melting point (? C.) 243-246 E-0029 melting point (? C.) 182-185 E-0041 melting point (? C.) 219-222 E-0044 melting point (? C.) 193-196 E-0046 melting point (? C.) 237-240 E-0047 melting point (? C.) 220-223 E-0086 melting point (? C.) 195-198 E-0119 melting point (? C.) 171-174 E-0120 melting point (? C.) 185-188 E-0121 melting point (? C.) 242-245 E-0122 melting point (? C.) 219-222 E-0123 melting point (? C.) 172-175 E-0124 melting point (? C.) 263-263 E-0125 melting point (? C.) 222-225 E-0128 melting point (? C.) 217-220 E-0134 melting point (? C.) 203-206 E-0137 melting point (? C.) 210-213 E-0147 melting point (? C.) 210-212 E-0148 melting point (? C.) 223-226 E-0152 melting point (? C.) 233-236 E-0176 melting point (? C.) 211-214 E-0177 melting point (? C.) 176-178 E-0179 melting point (? C.) 211-214 E-0227 melting point (? C.) 225-228 E-0263 melting point (? C.) 212-214 E-0266 melting point (? C.) 202-205 E-0269 melting point (? C.) 183-186 E-0320 melting point (? C.) 221-224 E-0329 melting point (? C.) 183-186 E-0338 melting point (? C.) 240-243
(691) TABLE-US-00329 TABLE 329 compound physical property value E-0340 melting point (? C.) 223-226 E-0518 melting point (? C.) 260-263 E-0520 melting point (? C.) 247-250 E-0521 melting point (? C.) 155-158 E-0542 melting point (? C.) 203-206 E-0549 melting point (? C.) 204-207 E-0553 melting point (? C.) 275-277 E-0555 melting point (? C.) 239-241 E-0557 melting point (? C.) 221-224 E-0561 melting point (? C.) 238-240 E-0563 melting point (? C.) 200-203 E-0571 melting point (? C.) 246-248 E-0573 melting point (? C.) 234-236 E-0574 melting point (? C.) 197-200 E-0577 melting point (? C.) 240-241 E-0578 melting point (? C.) 199-201 E-0587 melting point (? C.) 231-234 E-0588 melting point (? C.) 245-248 E-0591 melting point (? C.) 217-220 E-0593 melting point (? C.) 224-226 E-0594 melting point (? C.) 223-225 E-0597 melting point (? C.) 239-241 E-0598 melting point (? C.) 248-250 E-0600 melting point (? C.) 219-221 E-0608 melting point (? C.) 247-250 E-0609 melting point (? C.) 217-220 E-0613 melting point (? C.) 251-254 E-0614 melting point (? C.) 236-239 E-0618 melting point (? C.) 250-253 E-0624 melting point (? C.) 234-237 E-0629 melting point (? C.) 197-200 E-0633 melting point (? C.) 235-238 E-0636 melting point (? C.) 199-201 E-0638 melting point (? C.) 232-234 E-0639 melting point (? C.) 220-223 E-0644 melting point (? C.) 197-200 E-0652 melting point (? C.) 227-230 E-0653 melting point (? C.) 221-224 E-0655 melting point (? C.) 221-224 E-0656 melting point (? C.) 264-267 E-0659 melting point (? C.) 233-236
(692) TABLE-US-00330 TABLE 330 compound physical property value E-0660 melting point (? C.) 208-211 E-0663 melting point (? C.) 240-243 E-0664 melting point (? C.) 237-240 E-0665 melting point (? C.) 267-270 E-0670 melting point (? C.) 220-223 E-0688 melting point (? C.) 203-206 E-0689 melting point (? C.) 228-231 E-0691 melting point (? C.) 211-213 E-0692 melting point (? C.) 230-233 E-0693 melting point (? C.) 219-222 E-0697 melting point (? C.) 192-195 E-0701 melting point (? C.) 180-183 E-0705 melting point (? C.) 251-253 E-0712 melting point (? C.) 257-260 E-0733 melting point (? C.) 210-213 E-0906 melting point (? C.) 203-205 E-0907 melting point (? C.) 215-218 E-0908 melting point (? C.) 226-229 E-0910 melting point (? C.) 190-193 E-0911 melting point (? C.) 223-226 E-0912 melting point (? C.) 198-201 E-0913 melting point (? C.) 155-157 E-1067 melting point (? C.) 240-243 E-1076 melting point (? C.) 264-267 E-1077 melting point (? C.) 253-256 E-1102 melting point (? C.) 260-263 E-1117 melting point (? C.) 233-236 E-1136 melting point (? C.) 246-248 E-1140 melting point (? C.) 237-240 E-1148 melting point (? C.) 198-200 E-1152 melting point (? C.) 233-236 E-1153 melting point (? C.) 217-220 E-1155 melting point (? C.) 241-244 E-1156 melting point (? C.) 232-235 E-1160 melting point (? C.) 165-168 E-1163 melting point (? C.) 240-243 E-1165 melting point (? C.) 165-168
(693) TABLE-US-00331 TABLE 331 compound physical property value F-0003 melting point (? C.) 261-264 F-0008 melting point (? C.) 237-240 F-0012 melting point (? C.) 240-243 F-0017 melting point (? C.) 243-246 F-0099 melting point (? C.) 292-295 F-0108 melting point (? C.) 277-280 F-0115 melting point (? C.) 213-216 F-0207 melting point (? C.) 260-263 F-0213 melting point (? C.) 264-267 F-0295 melting point (? C.) 245-248 F-0301 melting point (? C.) 201-204 F-0309 melting point (? C.) 172-174 F-0375 melting point (? C.) 267-270 F-0461 melting point (? C.) 242-245 F-0462 melting point (? C.) 200-202 F-0463 melting point (? C.) 263-266 F-0464 melting point (? C.) 294-297 F-0466 melting point (? C.) 227-230
(694) TABLE-US-00332 TABLE 332 com- physical property value pound (.sup.1H-NMR data, in CDCl.sub.3 TMS ?(ppm)) C-0002 300 MHz 1.29 (3H, t), 4.37 (2H, q), 7.11-7.29 (2H, m), 7.32-7.51 (3H, m), 8.08 (1H, s), 8.20 (1H, ddd), 8.65 (1H, dd), 9.04 (1H, d) C-0044 400 MHz 1.13 (3H, t), 4.24 (2H, q), 7.30-7.70 (4H, m), 7.77 (1H, d), 7.98 (1H, s), 8.21 (1H, ddd), 8.65 (1H, dd), 9.04 (1H, d) C-0123 300 MHz 1.33 (3H, t), 1.43 (3H, t), 4.38 (2H, q), 4.70 (2H, q), 6.86-6.92 (1H, m), 7.03-7.09 (2H, m), 7.28 (1H, dd), 7.44 (1H, dd), 8.00 (1H, s), 8.16 (1H, dd), 8.62 (1H, d), 9.03 (1H, d) C-0177 400 MHz 1.32 (3H, t), 2.52 (3H, s), 4.39 (2H, q), 7.24- 7.37 (3H, m), 7.41 (1H, s), 7.42-7.50 (1H, m), 8.04 (1H, s), 8.16-8.21 (1H, m), 8.63 (1H, d), 9.08 (1H, s) C-0185 400 MHz 1.22 (3H, t), 2.62 (3H, s), 4.28 (2H, q), 7.42 (1H, d), 7.47 (1H, dd), 7.59-7.70 (2H, m), 8.14- 8.26 (3H, m), 8.67 (1H, d), 9.09 (1H, d) C-0189 400 MHz 1.32 (3H, t), 4.38 (2H, q), 7.26-7.35 (1H, m), 7.41-7.62 (3H, m), 7.67 (1H, d), 8.04 (1H, s), 8.20 (1H, d), 8.65 (1H, d), 9.05 (1H, d) C-0634 300 MHz 1.27 (3H, t), 3.78 (3H, s), 4.32 (2H, q), 6.94 (1H, d), 7.00 (1H, dd), 7.26 (1H, d), 7.44 (1H, dd), 7.99 (1H, s), 8.17 (1H, ddd), 8.61 (1H, dd), 9.02 (1H, d) C-0665 300 MHz 1.21 (3H, t), 3.76 (6H, s), 4.29 (2H, q), 6.62 (2H, d), 7.30 (1H, d), 7.43 (1H, dd), 8.03 (1H, s), 8.18 (1H, dd), 8.80 (1H, d), 9.19 (1H, d) C-0689 300 MHz 0.63-0.72 (2H, m), 0.78-0.90 (2H, m), 1.15 (3H, t), 1.66-1.78 (1H, m), 4.27 (2H, q), 6.72 (1H, d), 6.95 (1H, t), 7.25 (1H, dd), 7.47 (1H, dd), 8.03 (1H, s), 8.22 (1H, ddd), 8.63 (1H, dd), 9.05 (1H, d) C-1077 300 MHz 1.21 (3H, t), 2.23 (3H, s), 4.30 (2H, q), 7.30- 7.68 (4H, m), 8.05 (1H, s), 8.23 (1H, dd), 8.67 (1H, d), 9.07 (1H, d) C-1134 300 MHz 1.35 (3H, t), 4.40 (2H, q), 6.00 (2H, s), 6.80- 6.93 (2H, m), 7.09 (1H, d), 7.47 (1H, dd), 8.12- 8.23 (2H, m), 8.63 (1H, d), 9.04 (1H, s)
(695) TABLE-US-00333 TABLE 333 com- physical property value pound (.sup.1H-NMR data, in CDCl.sub.3 TMS ?(ppm)) C-1153 400 MHz 1.21 (3H, t), 2.41 (3H, s), 4.30 (2H, q), 7.01 (1H, t), 7.16-7.30 (1H, m), 7.48 (1H, dd), 8.03 (1H, s), 8.22 (1H, d), 8.63 (1H, d), 9.06 (1H, s) C-1160 400 MHz 1.15 (3H, t), 3.28 (3H, s), 4.21 (2H, s), 4.25 (2H, q), 7.35 (1H, t), 7.39-8.01 (3H, m), 8.01 (1H, s), 8.23 (1H, d), 8.65 (1H, d), 9.07 (1H, s) D-0017 300 MHz 1.31 (3H, t), 4.39 (2H, q), 7.42-7.56 (3H, m), 7.64 (1H, d), 7.82-7.92 (3H, m ), 7.98 (1H, s), 8.11 (1H, s), 8.22 (1H, d), 8.65 (1H, d), 9.09 (1H, s) D-0108 300 MHz 1.20 (3H, t), 2.24 (3H, s), 4.28 (2H, q), 7.21 (1H, d), 7.47 (1H, dd), 7.96 (1H, s), 8.21 (1H, ddd), 8.41 (1H, s), 8.48 (1H, dd), 8.65 (1H, dd), 9.05 (1H, d) D-0461 400 MHz 1.33 (3H, t), 2.18 (3H, s), 2.30 (3H, s) , 4.38 (2H, q), 7.50 (1H, dd), 7.93 (1H, s), 8.19 (1H, dd), 8.67(1H, d), 9.04 (1H, d) D-0462 400 MHz 1.10-1.31 (9H, m), 2.55 (2H, q), 2.63 (2H, q), 4.32 (2H, q), 7.48 (1H, dd), 7.91 (1H, s), 8.18 (1H, dd), 8.63 (1H, d), 9.03 (1H, d) D-0463 300 MHz 0.87 (3H, t), 4.10 (2H, q), 7.39 (1H, d), 7.45-7.57 (2H, m), 7.70-7.80 (2H, m), 8.12 (1H, s), 8.18 (1H, d), 8.25 (1H, d), 8.67 (1H, d), 8.96 (1H, d), 9.09 (1H, d)
(696) TABLE-US-00334 TABLE 334 com- physical property value pound (.sup.1H-NMR data, in CDCl.sub.3 TMS ?(ppm)) F-0103 300 MHz 7.48 (1H, dd), 7.60 (1H, dd), 7.90 (1H, dd), 8.29 (1H, ddd), 8.40 (1H, dd), 8.60 (1H, dd), 8.89 (1H, s), 9.14 (1H, d) F-0108 300 MHz 2.05 (3H, s), 7.29 (1H, d), 7.58 (1H, dd), 8.30 (1H, dd), 8.34 (1H, s), 8.39 (1H, d), 8.59 (1H, d), 8.80 (1H, s), 9.15 (1H, d)
(697) Next, formulation examples of the pest control agent of the present invention using the pyrazole derivative of the present invention produced in the manner as described above, or an agriculturally acceptable salt thereof will be specifically described. It is to be noted that the compound, the kinds and the mixing ratios of additives are not limited to this, but may be changed in a wide range. In the following description, part means a part by mass.
(Formulation Example 1) Emulsifiable Concentrate
(698) Compound described in Table 1 to Table 334 10 parts Cyclohexanone 30 parts Polyoxyethylene alkyl aryl ether 11 parts Calcium alkylbenzene sulfonate 4 parts Methylnaphthalene 45 parts
(699) These ingredients were uniformly dissolved to give an emulsifiable concentrate.
(Formulation Example 2) Water-Dispersible Powder
(700) Compound described in Table 1 to Table 334 10 parts Sodium salt of naphthalene sulfonic acid formalin condensate 0.5 parts Polyoxyethylene alkyl aryl ether 0.5 parts Diatomaceous earth 24 parts Clay 65 parts
(701) These ingredients were uniformly mixed and ground to give a water-dispersible powder.
(Formulation Example 3) Dust
(702) Compound described in Table 1 to Table 334 2 parts Diatomaceous earth 5 parts Clay 93 parts
(703) These ingredients were uniformly mixed and ground to give a dust.
(Formulation Example 4) Granules
(704) Compound described in Table 1 to Table 334 5 parts Sodium salt of lauryl alcohol sulfate ester 2 parts Sodium lignin sulfonate 5 parts Carboxymethylcellulose 2 parts Clay 86 parts
(705) These ingredients were uniformly mixed and ground. To this mixture, water in an amount corresponding to 20 parts was added and kneaded, and processed into 14 to 32 mesh granules by using an extruding granulator, and then dried to give granules.
(Formulation Example 5) Flowable Concentrate
(706) Compound described in Table 1 to Table 334 20 parts Polyoxyethylene styrenated phenyl ether sulfate 4 parts Ethylene glycol 7 parts Silicone AF-118N (available from Asahi Kasei Corporation) 0.02 parts Water 68.98 parts
(707) These ingredients were mixed with a high-speed stirrer for 30 minutes, and then ground with a wet grinder to give a flowable concentrate.
(Formulation Example 6) Water-Dispersible Granule
(708) Compound described in Table 1 to Table 334 10 parts Sodium lignin sulfonate 5 parts Polyoxyethylene alkyl aryl ether 1 part Sodium polycarboxylate 3 parts White carbon 5 parts Pregelatinized starch 1 part Calcium carbonate 65 parts Water 10 parts
(709) These ingredients were mixed and kneaded and extrusion granulated. The obtained granules were dried by a fluidized-bed dryer, to give a water-dispersible granule.
(710) Next, the effect exerted by the pest control agent of the present invention will be described by way of test examples.
(Test Example 1) Plutella xylostella Killing Test
(711) The water-dispersible powder prepared in accordance with Formulation example 2 was diluted in water so that the concentration of the active ingredient was 500 ppm. A cabbage leaf was dipped in this liquid agent, and air-dried, and then put into a plastic cup. Ten second instar larvae of Plutella xylostella were released in the cup, and the cup was lidded. Then, the cup was placed in a thermostatic chamber at 25? C., and the number of dead insects was examined after 6 days, and the insect mortality was determined by the calculation formula of numerical formula 1. The test was conducted singly.
Insect mortality (%)=[1?(number of living insects)/(number of tested insects)]?100[Numerical formula 1]
(712) The compounds showing an insect mortality of 50% or more in this test are as follows.
(713) A-0020, A-0023, A-0025, A-0029, A-0047, A-0059, A-0125, A-0134, A-0144, A-0147, A-0148, A-0152, A-0176, A-0182, A-0183, A-0185, A-0186, A-0192, A-0227, A-0260, A-0263, A-0266, A-0269, A-0329, A-338, A-0340, A-0524, A-0542, A-0551, A-0555, A-0557, A-0571, A-0573, A-0574, A-0577, A-0578, A-0587, A-0588, A-0593, A-0594, A-0597, A-0598, A-0600, A-0613, A-0614, A-0618, A-0624, A-0634, A-0636, A-0637, A-0638, A-0639, A-0645, A-0649, A-0654, A-0655, A-0659, A-0663, A-0670, A-0671, A-0688, A-0692, A-0693, A-0697, A-0701, A-0709, A-0875, A-0906, A-0907, A-0908, A-0909, A-0911, A-1067, A-1077, A-1097, A-1117, A-1136, A-1141, A-1145, A-1151, A-1155, A-1156, A-1162, A-1164, A-1980, A-2182, A-2384, A-2600, A-2990, A-3192, A-3812, A-4404, A-4606, A-5414, A-7030, A-7838, A-8646, A-9993, A-9994, B-0003, B-0018, B-0027, B-0090, B-0095, B-0099, B-0100, B-0107, B-0165, B-0199, B-0205, B-0290, B-0296, B-0367, B-0456, B-0457, B-0458, C-0001, C-0002, C-0008, C-0020, C-0021, C-0023, C-0047, C-0086, C-0134, C-0137, C-0144, C-0145, C-0152, C-0176, C-0179, C-0185, C-0186, C-0189, C-0198, C-0239, C-0263, C-0269, C-0329, C-0340, C-0520, C-0555, C-0557, C-0561, C-0563, C-0571, C-0573, C-0587, C-0588, C-0594, C-0597, C-0598, C-0600, C-0614, C-0624, C-0629, C-0634, C-0637, C-0638, C-0656, C-0663, C-0907, C-0910, C-1067, C-1097, C-1145, C-1153, C-1162, C-1165, D-0035, D-0098, D-0099, D-0103, D-0107, D-0108, D-0207, D-0309, D-0466, E-0002, E-0003, E-0006, E-0008, E-0020, E-0023, E-0041, E-0047, E-0086, E-0119, E-0125, E-0128, E-0134, E-0137, E-0176, E-0177, E-0179, E-0263, E-0329, E-0340, E-0518, E-0557, E-0561, E-0563, E-0571, E-0573, E-0587, E-0588, E-0593, E-0594, E-0597, E-0598, E-0600, E-0609, E-0613, E-0614, E-0618, E-0624, E-0633, E-0644, E-0652, E-0653, E-0663, E-0693, E-0733, E-0907, E-0908, E-1067, E-1076, E-1077, E-1117, E-1148, E-1152, F-0012, F-0108, F-0207, F-0295, F-0301, F-0309, F-0464, F-0466
(Test Example 2) Helicoverpa armigera Killing Test
(714) The water-dispersible powder prepared in accordance with Formulation example 2 was diluted in water so that the concentration of the active ingredient was 500 ppm. A cabbage leaf was dipped in this liquid agent, and air-dried, and then put into a plastic cup. Five newly hatched larvae of Helicoverpa armigera were released in the cup, and the cup was lidded. Then, the cup was placed in a thermostatic chamber at 25? C., and the number of dead insects was examined after 6 days, and the insect mortality was determined by the calculation formula of numerical formula 1. The test was conducted in duplicate.
(715) The compounds showing an insect mortality of 50% or more in this test are as follows.
(716) A-0002, A-0008, A-0014, A-0020, A-0023, A-0029, A-0086, A-0103, A-0128, A-0137, A-0145, A-0148, A-0152, A-0179, A-0183, A-0188, A-0242, A-0263, A-0266, A-0329, A-0338, A-0340, A-0512, A-0524, A-0542, A-0551, A-0553, A-0555, A-0561, A-0574, A-0583, A-0587, A-0588, A-0591, A-0593, A-0594, A-0597, A-0608, A-0614, A-0633, A-0634, A-0638, A-0639, A-0644, A-0645, A-0653, A-0654, A-0655, A-0659, A-0660, A-0671, A-0688, A-0689, A-0691, A-0692, A-0693, A-0705, A-0709, A-0713, A-0906, A-0907, A-0908, A-0909, A-0910, A-0911, A-0912, A-0913, A-1076, A-1117, A-1140, A-1141, A-1145, A-1146, A-1148, A-1151, A-1153, A-1158, A-1162, A-1163, A-1164, A-1165, A-1166, A-2182, A-2384, A-2586, A-2600, A-2990, A-6020, A-7838, A-9480, A-9993, A-9994, B-0004, B-0027, B-0090, B-0091, B-0095, B-0099, B-0100, B-0165, B-0199, B-0287, B-0290, B-0367, B-0454, B-0455, B-0457, C-0004, C-0008, C-0021, C-0022, C-0041, C-0046, C-0086, C-0120, C-0125, C-0134, C-0137, C-0147, C-0179, C-0189, C-0227, C-0239, C-0263, C-0266, C-0269, C-0320, C-0329, C-0340, C-0512, C-0518, C-0553, C-0557, C-0561, C-0563, C-0573, C-0574, C-0577, C-0578, C-0587, C-0588, C-0594, C-0597, C-0598, C-0600, C-0608, C-0614, C-0633, C-0636, C-0637, C-0653, C-0656, C-0659, C-0660, C-0689, C-0692, C-0705, C-0906, C-0907, C-0908, C-0911, C-1117, C-1140, C-1141, C-1162, C-1163, C-1165, D-0003, D-0004, D-0012, D-0035, D-0099, D-0107, D-0108, D-0115, D-0207, D-0295, D-0301, D-0375, D-0464, E-0006, E-0008, E-0047, E-0086, E-0119, E-0121, E-0128, E-0148, E-0177, E-0263, E-0329, E-0521, E-0542, E-0561, E-0563, E-0571, E-0573, E-0587, E-0588, E-0594, E-0597, E-0600, E-0614, E-0633, E-0639, E-0644, E-0659, E-0660, E-0688, E-0692, E-0693, E-0705, E-0733, E-0906, E-0907, E-0908, E-0911, E-0912, E-1076, E-1117, E-1160, F-0003, F-0012, F-0017, F-0099, F-0108, F-0207, F-0301, F-0375, F-0461, F-0466
(Test Example 3) Aphis gossypii Killing Test
(717) The water-dispersible powder prepared in accordance with Formulation example 2 was diluted in water so that the concentration of the active ingredient was 500 ppm. A nursery plant of cucumber preliminarily inoculated with nymphs of Aphis gossypii was dipped in this liquid agent, and air-dried. The nursery plant of cucumber after the treatment was placed in a thermostatic chamber at 25? C., and the number of live insects was counted after 3 days, and the insect mortality was determined by the calculation formula of numerical formula 1. The test was conducted singly.
(718) The compounds showing an insect mortality of 50% or more in this test are as follows.
(719) A-0001, A-0002, A-0004, A-0005, A-0006, A-0007, A-0008, A-0014, A-0020, A-0021, A-0022, A-0023, A-0025, A-0029, A-0044, A-0045, A-0046, A-0047, A-0059, A-0086, A-0101, A-0103, A-0119, A-0120, A-0121, A-0122, A-0123, A-0124, A-0143, A-0144, A-0145, A-0146, A-0147, A-0148, A-0152, A-0176, A-0177, A-0179, A-0182, A-0183, A-0185, A-0186, A-0189, A-0260, A-0263, A-0266, A-0269, A-0320, A-0340, A-0347, A-0512, A-0524, A-0550, A-0555, A-0557, A-0561, A-0563, A-0571, A-0573, A-0574, A-0577, A-0578, A-0582, A-0583, A-0591, A-0593, A-0594, A-0597, A-0598, A-0603, A-0609, A-0613, A-0614, A-0618, A-0634, A-0636, A-0637, A-0639, A-0644, A-0652, A-0653, A-0654, A-0655, A-0656, A-0659, A-0660, A-0663, A-0665, A-0670, A-0688, A-0689, A-0691, A-0692, A-0693, A-0697, A-0701, A-0705, A-0709, A-0712, A-0713, A-0875, A-0906, A-0907, A-0908, A-0909, A-0913, A-1067, A-1077, A-1102, A-1117, A-1134, A-1140, A-1141, A-1145, A-1146, A-1147, A-1152, A-1157, A-1158, A-1160, A-1161, A-1162, A-1163, A-1165, A-1166, A-2182, A-2586, A-2600, A-3596, A-3798, A-3812, A-4202, A-4404, A-4606, A-4808, A-5414, A-5616, A-6020, A-6022, A-7434, A-7636, A-7838, A-8040, A-8862, A-9993, A-9994, B-0001, B-0002, B-0003, B-0004, B-0009, B-0027, B-0091, B-0095, B-0099, B-0107, B-0290, B-0293, B-0301, B-0367, B-0389, B-0453, B-0455, C-0001, C-0002, C-0003, C-0006, C-0007, C-0020, C-0021, C-0025, C-0044, C-0045, C-0047, C-0119, C-0122, C-0125, C-0128, C-0134, C-0137, C-0145, C-0176, C-0177, C-0183, C-0186, C-0189, C-0227, C-0239, C-0320, C-0553, C-0557, C-0561, C-0574, C-0578, C-0594, C-0600, C-0637, C-0638, C-0639, C-0653, C-0655, C-0660, C-0697, C-0907, C-0910, C-0911, C-1077, C-1117, C-1141, C-1162, D-0002, D-0003, D-0005, D-0008, D-0012, D-0035, D-0103, D-0107, D-0108, D-0115, D-0207, D-0213, D-0301, D-0375, D-0463, D-0464, E-0023, E-0121, E-0124, E-0128, E-0269, E-0609, E-0656, E-0693, E-1067, F-0003
(Test Example 4) Nilaparvata lugens Killing Activity Test
(720) The water-dispersible powder prepared in accordance with Formulation example 2 was diluted in water so that the concentration of the active ingredient was 500 ppm. Paddy was dipped in this liquid agent, and then put into a plastic cup. Ten second instar larvae of Nilaparvata lugens were released in the plastic cup, and the cup was lidded, and placed in a thermostatic chamber at 25? C. After 6 days, the number of live insects was counted, and the insect mortality was determined by the calculation formula of numerical formula 1. The test was conducted singly.
(721) The compounds showing an insect mortality of 50% or more in this test are as follows.
(722) A-0002, A-0003, A-0004, A-0005, A-0007, A-0008, A-0014, A-0020, A-0021, A-0022, A-0023, A-0025, A-0041, A-0045, A-0046, A-0047, A-0059, A-0086, A-0101, A-0119, A-0120, A-0121, A-0122, A-0123, A-0124, A-0125, A-0128, A-0134, A-0145, A-0146, A-0147, A-0148, A-0152, A-0176, A-0177, A-0179, A-0182, A-0183, A-0185, A-0186, A-0188, A-0189, A-0198, A-0227, A-0239, A-0242, A-0260, A-0263, A-0266, A-0269, A-0320, A-0329, A-0340, A-0347, A-0548, A-0550, A-0551, A-0555, A-0557, A-0561, A-0563, A-0571, A-0577, A-0578, A-0583, A-0587, A-0588, A-0591, A-0593, A-0594, A-0597, A-0598, A-0600, A-0603, A-0609, A-0613, A-0614, A-0618, A-0624, A-0629, A-0633, A-0634, A-0636, A-0637, A-0638, A-0639, A-0644, A-0645, A-0653, A-0654, A-0655, A-0656, A-0659, A-0660, A-0663, A-0664, A-0665, A-0670, A-0671, A-0688, A-0689, A-0692, A-0693, A-0697, A-0701, A-0705, A-0709, A-0712, A-0713, A-0733, A-0907, A-0910, A-1067, A-1076, A-1077, A-1097, A-1102, A-1117, A-1134, A-1136, A-1140, A-1145, A-1146, A-1147, A-1148, A-1151, A-1153, A-1154, A-1155, A-1156, A-1158, A-1159, A-1161, A-1162, A-1163, A-1164, A-1166, A-1980, A-2182, A-2384, A-2586, A-2600, A-2788, A-2990, A-3192, A-3596, A-3798, A-3812, A-4000, A-4202, A-4404, A-4808, A-5414, A-5616, A-6020, A-6222, A-6424, A-7030, A-7232, A-7434, A-7636, A-7838, A-8040, A-8242, A-8444, A-8646, A-8862, A-9435, A-9993, A-9994, B-0001, B-0004, B-0018, B-0027, B-0090, B-0091, B-0095, B-0099, B-0100, B-0107, B-0165, B-0205, B-0287, B-0290, B-0296, B-0301, B-0389, B-0454, B-0455, B-0456, B-0457, B-0458, B-0459, C-0001, C-0002, C-0021, C-0022, C-0023, C-0025, C-0041, C-0044, C-0047, C-0086, C-0119, C-0120, C-0121, C-0123, C-0124, C-0125, C-0128, C-0134, C-0137, C-0145, C-0147, C-0152, C-0176, C-0177, C-0179, C-0185, C-0186, C-0189, C-0227, C-0239, C-0263, C-0269, C-0320, C-0340, C-0549, C-0557, C-0561, C-0571, C-0574, C-0577, C-0578, C-0587, C-0588, C-0591, C-0593, C-0594, C-0597, C-0598, C-0600, C-0614, C-0624, C-0633, C-0636, C-0637, C-0638, C-0639, C-0653, C-0665, C-0656, C-0660, C-0663, C-0665, C-0689, C-0692, C-0697, C-0705, C-0712, C-0912, C-1067, C-1077, C-1097, C-1102, C-1134, C-1140, C-1141, C-1145, C-1152, C-1153, C-1162, C-1163, C-1165, D-0005, D-0012, D-0017, D-0035, D-0098, D-0099, D-0103, D-0107, D-0213, D-0295, D-0375, D-0462, D-0463, D-0464, D-0466, E-0044, E-0086, E-0125, E-0134, E-0148, E-0152, E-0177, E-0179, E-0227, E-0266, E-0329, E-0521, E-0555, E-0578, E-0587, E-0588, E-0600, E-0614, E-0618, E-0629, E-0633, E-0660, E-0693, E-0908, E-1077, F-0003, F-0012, F-0099, F-0295, F-0462
(723) The present invention provides a novel compound having excellent insecticide activity, and is useful in pesticide fields and agricultural fields, and has industrial applicability.