Inhibitors of tryptophan-2,3-dioxygenase or indoleamine-2,3-dioxygenase

Abstract

Provided is a compound for use in medicine for inhibiting tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO), which compound comprises formula (I) wherein X.sup.1, X.sup.2, and X.sup.7, may be the same or different and each is independently selected from C and N; X.sup.3, X.sup.4, X.sup.5, and X.sup.6 may be the same or different and each is independently selected from C, N, O and S wherein when X.sup.3 is N it has a double bond and wherein when X.sup.6 is N it has a double bond; the dotted line is a bond which may be present or absent; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that at least one of R.sup.2, R.sup.3, R.sup.4 and R.sup.6 comprises a group Y; and provided that the number of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 groups present is such that the respective valencies of X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, X.sup.6, and X.sup.7 are maintained; and wherein Y is a group having a formula selected from (II), (III), (IV), (V) wherein L may be present or absent, and may be a substituted or unsubstituted organic linking group, and R.sup.31 and R.sup.32 may be the same or different and are selected from H and a substituted or unsubstituted organic group, X.sup.8 is selected from C and N, and each R.sup.313 may be the same or different and is selected from H and a substituted or unsubstituted organic group. ##STR00001##

Claims

1. A compound having one of the following formulae, or a pharmaceutically acceptable salt thereof: ##STR00066## R.sup.311 is selected from: a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group selected from Me, Et, Pr, i-Pr, n-Bu, i-Bu, t-Bu, pentyl and hexyl; a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph; a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group selected from CH.sub.2F, CF.sub.3, CH.sub.2CF.sub.3; an NH.sub.2 or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group selected from NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt; a substituted or unsubstituted amino-aryl group selected from NH-Ph, NH-(2,3 or 4)F-Ph, NH-(2,3 or 4)Cl-Ph, NH-(2,3 or 4)Br-Ph, NH-(2,3 or 4)I-Ph, NH-(2,3 or 4)Me-Ph, NH-(2,3 or 4)Et-Ph, NH-(2,3 or 4)Pr-Ph, NH-(2,3 or 4)Bu-Ph, NH-(2,3 or 4)OMe-Ph, NH-(2,3 or 4)OEt-Ph, NH-(2,3 or 4)OPr-Ph, NH-(2,3 or 4)OBu-Ph, NH-2,(3,4,5 or 6)F.sub.2-Ph, NH-2,(3,4,5 or 6)Cl.sub.2-Ph, NH-2,(3,4,5 or 6)Br.sub.2-Ph, NH-2,(3,4,5 or 6)I.sub.2-Ph, NH-2,(3,4,5 or 6)Me.sub.2-Ph, NH-2,(3,4,5 or 6)Et.sub.2-Ph, NH-2,(3,4,5, or 6)Pr.sub.2-Ph, and NH-2,(3,4,5 or 6)Bu.sub.2-Ph; a substituted or unsubstituted cyclic amine or amido group selected from pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, and 4-keto-piperidinyl; a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group selected from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl; a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group selected from CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH; a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 amino carbonyl group selected from NHCO-Me, NHCO-Et, NHCO-Pr, NHCO-Bu, NHCO-pentyl, NHCO-hexyl, NHCO-Ph, NMe-CO-Me, NMe-CO-Et, NMe-CO-Pr, NMe-CO-Bu, NMe-CO-pentyl, NMe-CO-hexyl, and NMe-CO-Ph; a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy or aryloxy group selected from OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, O-Ph, OCH.sub.2-Ph, OCH.sub.2-(2,3 or 4)-F-Ph, OCH.sub.2-(2,3 or 4)-Cl-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe; a substituted or unsubstituted linear or branched aminoalkoxy group selected from OCH.sub.2CH.sub.2NH.sub.2, OCH.sub.2CH.sub.2NHMe, OCH.sub.2CH.sub.2NMe.sub.2, OCH.sub.2CH.sub.2NREt, and OCH.sub.2CH.sub.2NEt.sub.2; a substituted or unsubstituted aminosulphonyl group selected from NHSO.sub.2Me, NHSO.sub.2Et, NHSO.sub.2Pr, NHSO.sub.2iPr, NHSO.sub.2Ph, NHSO.sub.2-(2,3 or 4)-F-Ph, NHSO.sub.2-cyclopropyl, and NHSO.sub.2CH.sub.2CH.sub.2OCH.sub.3; a substituted or unsubstituted aromatic group selected from Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-; and 4-CF.sub.3O-Ph-; and a saturated or unsaturated, substituted or unsubstituted, heterocyclic group selected from pyrrole-2-yl, pyrrole-3-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidine-2-yl, pyrimidine-4-yl, pyrimidine-5-yl, pyrazine-2-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-5-yl; and R.sup.312 is selected from: a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group selected from Me, Et, Pr, i-Pr, n-Bu, i-Bu, t-Bu, pentyl and hexyl; a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group selected from CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph; a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group selected from CH.sub.2F, CF.sub.3, CH.sub.2CF.sub.3; an NH.sub.2 or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group selected from NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt; a substituted or unsubstituted amino-aryl group selected from NH-Ph, NH-(2,3 or 4)F-Ph, NH-(2,3 or 4)Cl-Ph, NH-(2,3 or 4)Br-Ph, NH-(2,3 or 4)I-Ph, NH-(2,3 or 4)Me-Ph, NH-(2,3 or 4)Et-Ph, NH-(2,3 or 4)Pr-Ph, NH-(2,3 or 4)Bu-Ph, NH-(2,3 or 4)OMe-Ph, NH-(2,3 or 4)OEt-Ph, NH-(2,3 or 4)OPr-Ph, NH-(2,3 or 4)OBu-Ph, NH-2,(3,4,5 or 6)F.sub.2-Ph, NH-2,(3,4,5 or 6)Cl.sub.2-Ph, NH-2,(3,4,5 or 6)Br.sub.2-Ph, NH-2,(3,4,5 or 6)I.sub.2-Ph, NH-2,(3,4,5 or 6)Me.sub.2-Ph, NH-2,(3,4,5 or 6)Et.sub.2-Ph, NH-2,(3,4,5, or 6)Pr.sub.2-Ph, and NH-2,(3,4,5 or 6)Bu.sub.2-Ph; a substituted or unsubstituted cyclic amine or amido group selected from pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, and 4-keto-piperidinyl; a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group selected from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl; a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group selected from CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH; a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 amino carbonyl group selected from NHCO-Me, NHCO-Et, NHCO-Pr, NHCO-Bu, NHCO-pentyl, NHCO-hexyl, NHCO-Ph, NMe-CO-Me, NMe-CO-Et, NMe-CO-Pr, NMe-CO-Bu, NMe-CO-pentyl, NMe-CO-hexyl, and NMe-CO-Ph; a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy or aryloxy group selected from OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, O-Ph, OCH.sub.2-Ph, OCH.sub.2-(2,3 or 4)-F-Ph, OCH.sub.2-(2,3 or 4)-Cl-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe; a substituted or unsubstituted linear or branched aminoalkoxy group selected from OCH.sub.2CH.sub.2NH.sub.2, OCH.sub.2CH.sub.2NHMe, OCH.sub.2CH.sub.2NMe.sub.2, OCH.sub.2CH.sub.2NHEt, and OCH.sub.2CH.sub.2NEt.sub.2; a substituted or unsubstituted aminosulphonyl group selected from NHSO.sub.2Me, NHSO.sub.2Et, NHSO.sub.2Pr, NHSO.sub.2iPr, NHSO.sub.2Ph, NHSO.sub.2-(2,3 or 4)-F-Ph, NHSO.sub.2-cyclopropyl, NHSO.sub.2CH.sub.2CH.sub.2OCH.sub.3; a substituted or unsubstituted 6 membered carbocyclic or heterocyclic aromatic group selected from Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-, pyridin-2-yl, pyridine-3-yl, pyridin-4-yl, pyrimidin-2-yl, pyrimidin-5-yl, pyrimidin-4-yl, pyridazin-3-yl, pyridazine-4-yl; and a substituted or unsubstituted saturated heterocyclic group selected from piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, tetrahydrofuran-2-yl, and tetrahydrofuran-3-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, and tetrahydropyran-4-yl.

2. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein R.sup.312 is selected from: a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group selected from CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph; a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl; a substituted or unsubstituted 6 membered carbocyclic or heterocyclic aromatic group selected from Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-, pyridin-2-yl, pyridine-3-yl, pyridin-4-yl, pyrimidin-2-yl, pyrimidin-5-yl, pyrimidin-4-yl, pyridazin-3-yl, and pyridazine-4-yl; and a substituted or unsubstituted saturated heterocyclic group selected from piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, tetrahydrofuran-2-yl, and tetrahydrofuran-3-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, and tetrahydropyran-4-yl.

3. The compound according to claim 2, or a pharmaceutically acceptable salt thereof, wherein R.sup.311 is selected from: a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group selected from Me, Et, Pr, i-Pr, n-Bu, i-Bu, t-Bu, pentyl and hexyl; a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group selected from CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph; a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group selected from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl; a substituted or unsubstituted aromatic group selected from Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-; and a saturated or unsaturated, substituted or unsubstituted, heterocyclic group selected from pyrrole-2-yl, pyrrole-3-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidine-2-yl, pyrimidine-4-yl, pyrimidine-5-yl, pyrazine-2-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-5-yl.

4. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, selected from one of the following: ##STR00067## ##STR00068## ##STR00069## ##STR00070## ##STR00071## ##STR00072## ##STR00073## ##STR00074## ##STR00075##

5. The compound of claim 1, selected from the following formulae, or a pharmaceutically acceptable salt thereof: ##STR00076## ##STR00077## ##STR00078## ##STR00079## ##STR00080## ##STR00081## ##STR00082## ##STR00083## ##STR00084##

6. A pharmaceutical composition comprising a compound as defined in claim 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable additive and/or excipient.

Description

(1) The invention will now be explained in more detail, by way of example only, with reference to the following Figures.

(2) FIG. 1 shows a schematic diagram of tryptophan catabolism along the KP (from The Kynurenine Pathway in Brain Tumour Pathogenesis, Adam et al., 2012, Cancer Res 72:5649-57).

(3) FIG. 2 shows a schematic summary of the involvement of kynurenine in CNS disorders (from The kynurenine pathway as a therapeutic target in cognitive and neurodegenerative disorders, Stone and Darlington. Br. J. Pharmacol. 2013 169(6):1211-27.

(4) The invention will now be described in more detail. Firstly a number of typical general structures of the compounds of the invention will be described.

(5) As has been described, the invention relates to a compound for use in medicine for inhibiting tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO), which compound comprises the following formula:

(6) ##STR00005##
wherein X.sup.1, X.sup.2, and X.sup.7, may be the same or different and each is independently selected from C and N; X.sup.3, X.sup.4, X.sup.5, and X.sup.6 may be the same or different and each is independently selected from C, N, O and S wherein when X.sup.3 is N it has a double bond and wherein when X.sup.6 is N it has a double bond; the dotted line is a bond which may be present or absent; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that at least one of R.sup.2, R.sup.3, R.sup.4 and R.sup.6 comprises a group Y; and provided that the number of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 groups present is such that the respective valencies of X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, X.sup.6, and X.sup.7 are maintained; and wherein Y is a group having a formula selected from the following:

(7) ##STR00006##
wherein L may be present or absent, and may be a substituted or unsubstituted organic linking group, and R.sup.31 and R.sup.32 may be the same or different and are selected from H and a substituted or unsubstituted organic group, X.sup.8 is selected from C and N, and each R.sup.313 may be the same or different and is selected from H and a substituted or unsubstituted organic group.

(8) The fused bicyclic ring system is preferably aromatic. All tautomeric forms of the ring system (including the tautomeric form of each of the two 6-membered rings) are included. Alternatively, the right hand ring may be non-aromatic if it is unsaturated. In this latter case one or both of the bonds represented by the dotted lines are absent.

(9) The group L is a linking group and is not especially limited provided that it does not impair the IDO or TDO inhibitory activity of the compounds. It may be present or absent. When absent, the N group (or CO, or SO.sub.2, or X.sup.8) of group Y is directly attached to the ring system. When present, L may be divalent, such that it may simply link the N atom of group Y to the ring system. Alternatively L may be trivalent if in addition it forms a ring with R.sup.31 or R.sup.32, and further alternatively L may be quadravalent if it forms a ring with both R.sup.31 and R.sup.32.

(10) In typical embodiments, X.sup.3, X.sup.4, X.sup.5 and X.sup.6 are all C atoms. In other typical embodiments, one of X.sup.3, X.sup.4, X.sup.5 and X.sup.6 is N.

(11) In typical embodiments both above and below herein, X.sup.3 and/or X.sup.6 is a C atom.

(12) In typical embodiments, X.sup.1, X.sup.2, and X.sup.7 are all C atoms. In other typical embodiments, one of X.sup.1, X.sup.2, and X.sup.7 is N.

(13) In typical embodiments both above and below herein, X.sup.7 is a C atom. In other typical embodiments X.sup.7 is an N atom.

(14) In typical embodiments both above and below herein, Y comprises an aminocarbonyl group, a carbonylamino group, an aminosulphonyl group, a sulphonylamino group, a piperidinyl group and/or a piperazinyl group.

(15) In typical embodiments both above and below herein, L is absent. In alternative typical embodiments L may comprise a substituted or unsubstituted C.sub.1-C.sub.6 alkylene group (such as CH.sub.2, CH.sub.2CH.sub.2, CH.sub.2CH.sub.2CH.sub.2, CH.sub.2CH.sub.2CH.sub.2CH.sub.2, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2).

(16) Thus, in view of the typical compounds already described, in more typical embodiments the compound used in the invention may comprise one of the following formulae:

(17) ##STR00007##
wherein, in each case, the substituents R and X are as defined in any of the above and below embodiments described herein.

(18) Furthermore, in view of the typical compounds already described, in more typical embodiments the compound used in the invention may comprise one of the following formulae:

(19) ##STR00008## ##STR00009##
wherein, in each case, the substituents Y and R are as defined in any of the above or below embodiments described herein.

(20) Furthermore, in view of the typical compounds already described, in more typical embodiments the compound used in the invention may comprise one of the following formulae:

(21) ##STR00010## ##STR00011##
wherein, in each case, the substituents Y and R are as defined in any of the above or below embodiments described herein.

(22) Furthermore, in view of the typical compounds already described, in more typical embodiments the compound used in the invention may comprise one of the following formulae:

(23) ##STR00012## ##STR00013##
wherein, in each case, the substituents Y and R are as defined in any of the above or below embodiments described herein.

(24) Furthermore, in view of the typical compounds already described, in more typical embodiments the compound used in the invention may comprise one of the following formulae:

(25) ##STR00014##
wherein, in each case, the substituent Y is as defined in any of the above or below embodiments described herein.

(26) In the compounds of the formula:

(27) ##STR00015##
typically Y may be any of the Y groups described herein, but is preferably not a group of the following formula:

(28) ##STR00016##
wherein R.sup.311 comprises a phenyl group which itself has a substituent comprising a substituted or unsubstituted 2-oxodihydroquinoline group.

(29) The Y, R and X groups in all of the compounds and structures both above and below herein will now be described in more detail.

(30) As has been mentioned, the number of R substituents on an X or a ring atom will depend on its valency. Thus, it will be apparent in all of the embodiments of the invention, both above and below, that an X will have no substituents if it is O or S, no substituents or 1 substituent if it is N and 1 substituent or 2 substituents if it is C. The substituents are selected from H and an organic group as defined herein.

(31) As has been mentioned, in all of the embodiments of this invention (both above and below herein), the substituent is not especially limited, provided that it does not prevent the TDO or IDO inhibitory function from occurring. However, in typical embodiments, the substituents may be selected independently as follows.

(32) R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.313 are typically each independently selected from H and a group selected from the following groups: a halogen (such as F, Cl, Br and I); a nitrile group; a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as Me, Et, Pr, i-Pr, n-Bu, i-Bu, t-Bu, pentyl and hexyl); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3); an NH.sub.2 or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt); a substituted or unsubstituted amino-aryl group (such as NH-Ph, NH-(2,3 or 4)F-Ph, NH-(2,3 or 4)Cl-Ph, NH-(2,3 or 4)Br-Ph, NH-(2,3 or 4)I-Ph, NH-(2,3 or 4)Me-Ph, NH-(2,3 or 4)Et-Ph, NH-(2,3 or 4)Pr-Ph, NH-(2,3 or 4)Bu-Ph, NH-(2,3 or 4)OMe-Ph, NH-(2,3 or 4)OEt-Ph, NH-(2,3 or 4)OPr-Ph, NH-(2,3 or 4)OBu-Ph, NH-2,(3,4,5 or 6)F.sub.2-Ph, NH-2,(3,4,5 or 6)Cl.sub.2-Ph, NH-2,(3,4,5 or 6)Br.sub.2-Ph, NH-2,(3,4,5 or 6)I.sub.2-Ph, NH-2,(3,4,5 or 6)Me.sub.2-Ph, NH-2,(3,4,5 or 6)Et.sub.2-Ph, NH-2,(3,4,5, or 6)Pr.sub.2-Ph, NH-2,(3,4,5 or 6)Bu.sub.2-Ph, a substituted or unsubstituted cyclic amine or amido group (such as pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, and 4-keto-piperidinyl); a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl); an OH group, or a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group (such as CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid group (such as COOH, CH.sub.2COOH, CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH); a substituted or unsubstituted linear or branched carbonyl group (such as (CO)Me, (CO)Et, (CO)Pr, (CO)iPr, (CO)nBu, (CO)iBu, (CO)tBu, (CO)Ph, (CO)CH.sub.2Ph, (CO)CH.sub.2OH, (CO)CH.sub.2OCH.sub.3, (CO)CH.sub.2NH.sub.2, (CO)CH.sub.2NHMe, (CO)CH.sub.2NMe.sub.2, (CO)-cyclopropyl, (CO)-1,3-epoxypropan-2-yl; (CO)NH.sub.2, (CO)NHMe, (CO)NMe.sub.2, (CO)NHEt, (CO)NEt.sub.2, (CO)-pyrollidine-N-yl, (CO)-morpholine-N-yl, (CO)-piperazine-N-yl, (CO)N-methyl-piperazine-N-yl, (CO)NHCH.sub.2CH.sub.2OH, (CO)NHCH.sub.2CH.sub.2OMe, (CO)NHCH.sub.2CH.sub.2NH.sub.2, (CO)NHCH.sub.2CH.sub.2NHMe, and (CO)NHCH.sub.2CH.sub.2NMe.sub.2; a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid ester group (such as COOMe, COOEt, COOPr, COO-i-Pr, COO-n-Bu, COO-i-Bu, COO-t-Bu, CH.sub.2COOMe, CH.sub.2CH.sub.2COOMe, CH.sub.2CH.sub.2CH.sub.2COOMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOMe); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 amide group (such as CONH.sub.2, CONMeH, CONMe.sub.2, CONEtH, CONEtMe, CONEt.sub.2, CONPrH, CONPrMe, and CONPrEt); a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 amino carbonyl group (such as NHCO-Me, NHCO-Et, NHCO-Pr, NHCO-Bu, NHCO-pentyl, NHCO-hexyl, NHCO-Ph, NMe-CO-Me, NMe-CO-Et, NMe-CO-Pr, NMe-CO-Bu, NMe-CO-pentyl, NMe-CO-hexyl, NMe-CO-Ph; a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy or aryloxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, O-Ph, OCH.sub.2-Ph, OCH.sub.2-(2,3 or 4)-F-Ph, OCH.sub.2-(2,3 or 4)-Cl-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe); a substituted or unsubstituted linear or branched aminoalkoxy group (such as OCH.sub.2CH.sub.2NH.sub.2, OCH.sub.2CH.sub.2NHMe, OCH.sub.2CH.sub.2NMe.sub.2, OCH.sub.2CH.sub.2NHEt, and OCH.sub.2CH.sub.2NEt.sub.2; a substituted or unsubstituted sulphonyl group (such as SO.sub.2Me, SO.sub.2Et, SO.sub.2Pr, SO.sub.2iPr, SO.sub.2Ph, SO.sub.2-(2,3 or 4)-F-Ph, SO.sub.2 cyclopropyl, SO.sub.2CH.sub.2CH.sub.2OCH.sub.3), SO.sub.2NH.sub.2, SO.sub.2NHMe, SO.sub.2NMe.sub.2, SO.sub.2NHEt, SO.sub.2NEt.sub.2, SO.sub.2-pyrrolidine-N-yl, SO.sub.2-morpholine-N-yl, SO.sub.2NHCH.sub.2OMe, and SO.sub.2NHCH.sub.2CH.sub.2OMe; an substituted or unsubstituted aminosulphonyl group (such as NHSO.sub.2Me, NHSO.sub.2Et, NHSO.sub.2Pr, NHSO.sub.2iPr, NHSO.sub.2Ph, NHSO.sub.2-(2,3 or 4)-F-Ph, NHSO.sub.2-cyclopropyl, NHSO.sub.2CH.sub.2CH.sub.2OCH.sub.3); a substituted or unsubstituted aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-); a substituted or unsubstituted saturated or unsaturated heterocyclic group including an aromatic heterocyclic group and/or a non-aromatic heterocyclic group (such as pyrrole-1-yl, pyrrole-2-yl, pyrrole-3-yl, pyrazole-1-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-1-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-1-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-1-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyrimidin-6-yl, pyrazine-2-yl, pyrrolidine-1-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-1-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-1-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-1-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-1-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-2-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-4-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-4-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-2-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-3-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-2-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-3-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, morpholine-4-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-2-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-4-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-1-yl, tetrazole-2-yl, tetrazole-5-yl); and where there are two R.sup.313 groups attached to the same atom, they may together form a group which is double bonded to that atom, (such as a carbonyl group (O) or an alkene group (C(R).sub.2) wherein each R group is the same or different and is H or an organic group, preferably H or a straight or branched C.sub.1-C.sub.6 alkyl group), or the two R.sup.313 groups on the same atom may form a ring, preferably a substituted or unsubstituted C.sub.3-C.sub.6 saturated carbocyclic ring together with the atom to which they are attached (such as a substituted or unsubstituted cyclopropyl ring or a substituted or unsubstituted cyclobutyl ring), this being more preferable when the two R.sup.313 groups are on an atom adjacent to the NR.sup.31, and/or adjacent to the X.sup.8.

(33) More typically, where present, R.sup.1 and R.sup.7 are independently selected from H, a substituted or unsubstituted C.sub.1-C.sub.6 alkyl group, an NH.sub.2 group and a substituted or unsubstituted C.sub.1-C.sub.6 amino group, and a substituted or unsubstituted C.sub.1-C.sub.6 alkoxy group. More typically, where present R.sup.2, R.sup.3, R.sup.4, and R.sup.6 are independently selected from H, a halogen (such as F, Cl and Br) a substituted or unsubstituted C.sub.1-C.sub.6 alkyl group, an NH.sub.2 group and a substituted or unsubstituted C.sub.1-C.sub.6 amino group, a substituted or unsubstituted C.sub.1-C.sub.6 alkoxy group, a nitrile group, and a substituted or unsubstituted phenyl group. More typically, where present, R.sup.5 is selected from H, a halogen (such as F, Cl and Br) a substituted or unsubstituted C.sub.1-C.sub.6 alkyl group, an group and a substituted or unsubstituted C.sub.1-C.sub.6 amino group, a substituted or unsubstituted C.sub.1-C.sub.6 alkoxy group, a nitrile group, a substituted or unsubstituted aromatic or aliphatic cyclic group (such as a carbocyclic group or a heterocyclic group, such as a substituted or unsubstituted phenyl group). More typically each R.sup.313 is selected from H, a halogen (such as F and Cl) a substituted or unsubstituted C.sub.1-C.sub.6 alkyl group, an NH, group and a substituted or unsubstituted C.sub.1-C.sub.6 amino group, a substituted or unsubstituted C.sub.1-C.sub.6 alkoxy group, a nitrile group, a substituted or unsubstituted aromatic or aliphatic cyclic group (such as a carbocyclic group or a heterocyclic group, such as a substituted or unsubstituted phenyl group). Most typically each R.sup.313 is selected from H and a substituted or unsubstituted C.sub.1-C.sub.6 alkyl group. In certain embodiments, where present all of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.313 are H, or one of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 is not H and all of R.sup.313 are H.

(34) As has been mentioned at least one of R.sup.2, R.sup.3, R.sup.4 and R.sup.6 comprises a group Y having the following formula:

(35) ##STR00017##
wherein L may be present or absent, and may be any substituted or unsubstituted organic linking group; R.sup.31 and R.sup.32 may be the same or different and are selected from H and a substituted or unsubstituted organic group; X.sup.8 is selected from C and N; and each R.sup.313 may be the same or different and is selected from H and a substituted or unsubstituted organic group. In the present context, any group may be a linking group provided that it is capable of joining the ring system to the rest of the Y group. Typically the linking group is divalent, but may be trivalent or tetravalent in some embodiments. In some typical embodiments, R.sup.32 is H:

(36) ##STR00018##
or R.sup.31 is H:

(37) ##STR00019##

(38) As has been mentioned, in typical embodiments, the group L may be present or absent. When present L is a linker group attaching Y to the ring system. L is not especially limited, provided that the function of the molecule is not impaired. Accordingly, any known linking groups in organic chemistry may be employed. Typically L is a divalent group, suitable for linking the ring system to the group Y. In such embodiments L may, for example, comprise a substituted or unsubstituted C.sub.1-C.sub.6 alkylene group (such as CH.sub.2, CH.sub.2CH.sub.2, CH.sub.2CH.sub.2CH.sub.2, CH.sub.2CH.sub.2CH.sub.2CH.sub.2, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2).

(39) The group Y typically comprises an aminocarbonyl group, a carbonylamino group, an aminosulphonyl group, a sulphonylamino group, a piperidinyl group and/or a piperazinyl group. Typically the N atom in the above formula for Y forms the amino part of these groups, although it is not excluded that the N atom is not the amino part of these groups.

(40) In some typical such embodiments L is absent, and Y may be selected from the following groups:

(41) ##STR00020##

(42) Alternatively, an aminocarbonyl group or an aminosulphonyl group may be present when R.sup.31 (or R.sup.32) comprises a carbonyl group or a sulphonyl group. In such cases, typically the carbonyl group or the sulphonyl group is attached to the N atom of Y. For example, in certain embodiments, R.sup.31 (or R.sup.32) may comprise one of the following groups:

(43) ##STR00021##
wherein R.sup.311 is selected from H and a substituted or unsubstituted organic group. In such cases, the Y group is typically selected from the following:

(44) ##STR00022##
where L is present and L, R.sup.32, R.sup.311 and R.sup.313 have the same meaning as anywhere above or below herein. In typical embodiments, R.sup.311 is selected from the following: a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as Me, Et, Pr, i-Pr, n-Bu, i-Bu, t-Bu, pentyl and hexyl); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CF.sub.3, CH.sub.2CF.sub.3); an NH.sub.2 or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt); a substituted or unsubstituted amino-aryl group (such as NH-Ph, NH-(2,3 or 4)F-Ph, NH-(2,3 or 4)Cl-Ph, NH-(2,3 or 4)Br-Ph, NH-(2,3 or 4)I-Ph, NH-(2,3 or 4)Me-Ph, NH-(2,3 or 4)Et-Ph, NH-(2,3 or 4)Pr-Ph, NH-(2,3 or 4)Bu-Ph, NH-(2,3 or 4)OMe-Ph, NH-(2,3 or 4)OEt-Ph, NH-(2,3 or 4)OPr-Ph, NH-(2,3 or 4)OBu-Ph, NH-2,(3,4,5 or 6)F.sub.2-Ph, NH-2,(3,4,5 or 6)Cl.sub.2-Ph, NH-2,(3,4,5 or 6)Br.sub.2-Ph, NH-2,(3,4,5 or 6)I.sub.2-Ph, NH-2,(3,4,5 or 6)Me.sub.2-Ph, NH-2,(3,4,5 or 6)Et.sub.2-Ph, NH-2,(3,4,5, or 6)Pr.sub.2-Ph, NH-2,(3,4,5 or 6)Bu.sub.2-Ph, a substituted or unsubstituted cyclic amine or amido group (such as pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, and 4-keto-piperidinyl); a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group (such as CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH); a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 amino carbonyl group (such as NHCO-Me, NHCO-Et, NHCO-Pr, NHCO-Bu, NHCO-pentyl, NHCO-hexyl, NHCO-Ph, NMe-CO-Me, NMe-CO-Et, NMe-CO-Pr, NMe-CO-Bu, NMe-CO-pentyl, NMe-CO-hexyl, NMe-CO-Ph; a substituted or unsubstituted linear or branched C alkoxy or aryloxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, O-Ph, OCH.sub.2-Ph, OCH.sub.2-(2,3 or 4)-F-Ph, OCH.sub.2-(2,3 or 4)-Cl-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe); a substituted or unsubstituted linear or branched aminoalkoxy group (such as OCH.sub.2CH.sub.2NH.sub.2, OCH.sub.2CH.sub.2NHMe, OCH.sub.2CH.sub.2NMe.sub.2, OCH.sub.2CH.sub.2NHEt, and OCH.sub.2CH.sub.2NEt.sub.2; a substituted or unsubstituted aminosulphonyl group (such as NHSO.sub.2Me, NHSO.sub.2Et, NHSO.sub.2Pr, NHSO.sub.2iPr, NHSO.sub.2Ph, NHSO.sub.2-(2,3 or 4)-F-Ph, NHSO.sub.2-cyclopropyl, NHSO.sub.2CH.sub.2CH.sub.2OCH.sub.3); a substituted or unsubstituted aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-h-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-); a saturated or unsaturated, substituted or unsubstituted, heterocyclic group including an aromatic heterocyclic group and/or a non-aromatic heterocyclic group (such as pyrrole-2-yl, pyrrole-3-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidine-2-yl, pyrimidine-4-yl, pyrimidine-5-yl, pyrazine-2-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-5-yl).

(45) In more preferred embodiments, R.sup.311 is selected from the following: a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as Me, Et, Pr, i-Pr, n-Bu, i-Bu, t-Bu, pentyl and hexyl); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph); a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl); a substituted or unsubstituted aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-); a saturated or unsaturated, substituted or unsubstituted, heterocyclic group including an aromatic heterocyclic group and/or a non-aromatic heterocyclic group (such as pyrrole-2-yl, pyrrole-3-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidine-2-yl, pyrimidine-4-yl, pyrimidine-5-yl, pyrazine-2-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-5-yl).

(46) In these cases, typically L does not comprise a carbonyl or a sulphonyl, although this is not excluded.

(47) In typical embodiments, the linker L is absent. In such cases, Y may be selected from any of the following:

(48) ##STR00023##
wherein R.sup.32 is selected from a substituted or unsubstituted organic group (in these cases R.sup.32 is not H) and R.sup.311 and R.sup.313 are as defined anywhere herein.

(49) In the present context R.sup.312 is selected from the following: a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as Me, Et, Pr, i-Pr, n-Bu, i-Bu, t-Bu, pentyl and hexyl); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CF.sub.3, CH.sub.2CF.sub.3); an NH.sub.2 or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt); a substituted or unsubstituted amino-aryl group (such as NH-Ph, NH-(2,3 or 4)F-Ph, NH-(2,3 or 4)Cl-Ph, NH-(2,3 or 4)Br-Ph, NH-(2,3 or 4)I-Ph, NH-(2,3 or 4)Me-Ph, NH-(2,3 or 4)Et-Ph, NH-(2,3 or 4)Pr-Ph, NH-(2,3 or 4)Bu-Ph, NH-(2,3 or 4)OMe-Ph, NH-(2,3 or 4)OEt-Ph, NH-(2,3 or 4)OPr-Ph, NH-(2,3 or 4)OBu-Ph, NH-2,(3,4,5 or 6)F.sub.2-Ph, NH-2,(3,4,5 or 6)Cl.sub.2-Ph, NH-2,(3,4,5 or 6)Br.sub.2-Ph, NH-2,(3,4,5 or 6)I.sub.2-Ph, NH-2,(3,4,5 or 6)Me.sub.2-Ph, NH-2,(3,4,5 or 6)Et.sub.2-Ph, NH-2,(3,4,5, or 6)Pr.sub.2-Ph, NH-2,(3,4,5 or 6)Bu.sub.2-Ph, a substituted or unsubstituted cyclic amine or amido group (such as pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, and 4-keto-piperidinyl); a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group (such as CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH); a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 amino carbonyl group (such as NHCO-Me, NHCO-Et, NHCO-Pr, NHCO-Bu, NHCO-pentyl, NHCO-hexyl, NHCO-Ph, NMe-CO-Me, NMe-CO-Et, NMe-CO-Pr, NMe-CO-Bu, NMe-CO-pentyl, NMe-CO-hexyl, NMe-CO-Ph; a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy or aryloxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, O-Ph, OCH.sub.2-Ph, OCH.sub.2-(2,3 or 4)-F-Ph, OCH.sub.2-(2,3 or 4)-Cl-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe); a substituted or unsubstituted linear or branched aminoalkoxy group (such as OCH.sub.2CH.sub.2NH.sub.2, OCH.sub.2CH.sub.2NHMe, OCH.sub.2CH.sub.2NMe.sub.2, OCH.sub.2CH.sub.2NHEt, and OCH.sub.2CH.sub.2NEt.sub.2; a substituted or unsubstituted aminosulphonyl group (such as NHSO.sub.2Me, NHSO.sub.2Et, NHSO.sub.2Pr, NHSO.sub.2iPr, NHSO.sub.2Ph, NHSO.sub.2-(2,3 or 4)-F-Ph, NHSO.sub.2-cyclopropyl, NHSO.sub.2CH.sub.2CH.sub.2OCH.sub.3); a substituted or unsubstituted 6 membered carbocyclic or heterocyclic aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-, pyridin-2-yl, pyridine-3-yl, pyridin-4-yl, pyrimidin-2-yl, pyrimidin-5-yl, pyrimidin-4-yl, pyridazin-3-yl, pyridazine-4-yl); and a substituted or unsubstituted saturated heterocyclic group (such as piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, tetrahydrofuran-2-yl, and tetrahydrofuran-3-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl).

(50) In more typical embodiments R.sup.312 is selected from: a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph); a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl); a substituted or unsubstituted 6 membered carbocyclic or heterocyclic aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-b-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-, pyridin-2-yl, pyridine-3-yl, pyridin-4-yl, pyrimidin-2-yl, pyrimidin-5-yl, pyrimidin-4-yl, pyridazin-3-yl, pyridazine-4-yl); and a substituted or unsubstituted saturated heterocyclic group (such as piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, tetrahydrofuran-2-yl, and tetrahydrofuran-3-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl).

(51) In other typical embodiments, the piperidine and piperazine substituents that comprise Y may be selected from any of the following:

(52) ##STR00024##
wherein in each case L may be present or absent.

(53) As has been mentioned, in some cases L may form a ring with R.sup.31 or R.sup.32, and/or R.sup.31 and R.sup.32 may form a ring with each other. In some such embodiments, the Y group may be selected from the following structures:

(54) ##STR00025##

(55) In these groups, L, R.sup.31 and R.sup.32 may have the meaning as defined anywhere herein. In each case L may be present or absent. The curved line represents any organic group joining R.sup.31 and L, or R.sup.31 and R.sup.32, to form a ring. Typically, but not exclusively the curved line may be a substituted or unsubstituted alkylene group having from 1 to 6 C atoms, such as CH.sub.2, CH.sub.2CH.sub.2CH.sub.2, CH.sub.2CH.sub.2CH.sub.2CH.sub.2, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2.

(56) In typical embodiments, the atom of L which forms the ring with R.sup.31 or R.sup.32 is an atom directly bonded to the N of Y. Further typically, the atom of L which forms the ring with R.sup.31 is a C atom, which may be doubly bonded to the rest of L, or singly bonded to the rest of L. Thus, in such cases, Y may be selected from the following groups:

(57) ##STR00026##
where R.sup.33 may be selected from H and a substituted or unsubstituted organic group. In the case where L is double bonded at one end, such as to C in the above, then the valency of L is maintained. In such cases, L is trivalent rather than divalent, and may comprise a substituted or unsubstituted C.sub.1-C.sub.6 alkenyl group (such as CH, CHCH.sub.2, CHCH.sub.2CH.sub.2, CHCH.sub.2CH.sub.2CH.sub.2, CHCH.sub.2CH.sub.2CH.sub.2CH.sub.2, and CHCH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2).

(58) In some cases, the rest of the linker, L, is absent (in these cases the linker comprises only the C atom which forms the ring with R.sup.31, or comprises only CR.sup.33 when R.sup.33 is present):

(59) ##STR00027##

(60) In typical embodiments of the invention, both above and below herein, R.sup.31 and R.sup.32 are each independently selected from H and the following groups: a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as Me, Et, Pr, i-Pr, n-Bu, i-Bu, t-Bu, pentyl and hexyl); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CF.sub.3, and CH.sub.2CF.sub.3); a substituted or unsubstituted cyclic amine or amido group (such as pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, and 4-keto-piperidinyl); a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl); a substituted or unsubstituted linear or branched C.sub.2-C.sub.6 alcohol group (such as CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH); a substituted or unsubstituted linear or branched C alkoxy or aryloxy group linked through O via at least two further C atoms (such as CH.sub.2CH.sub.2OPh CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2OEt, CH.sub.2CH.sub.2OPr, CH.sub.2CH.sub.2OBu, CH.sub.2CH.sub.2CH.sub.2OPh, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe); a substituted or unsubstituted linear or branched C.sub.2-C.sub.6 carboxylic acid group (such as CH.sub.2COOH, CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH); a substituted or unsubstituted linear or branched carbonyl group (such as (CO)Me, (CO)Et, (CO)Pr, (CO)iPr, (CO)nBu, (CO)iBu, (CO)tBu, (CO)Ph, (CO)CH.sub.2Ph, (CO)CH.sub.2OH, (CO)CH.sub.2OCH.sub.3, (CO)CH.sub.2NH.sub.2, (CO)CH.sub.2NHMe, (CO)CH.sub.2NMe.sub.2, (CO)-cyclopropyl, (CO)-1,3-epoxypropan-2-yl; (CO)NH.sub.2, (CO)NHMe, (CO)NMe.sub.2, (CO)NHEt, (CO)NEt.sub.2, (CO)-pyrollidine-N-yl, (CO)-morpholine-N-yl, (CO)-piperazine-N-yl, (CO)N-methyl-piperazine-N-yl, (CO)NHCH.sub.2CH.sub.2OH, (CO)NHCH.sub.2CH.sub.2OMe, (CO)NHCH.sub.2CH.sub.2NH.sub.2, (CO)NHCH.sub.2CH.sub.2NHMe, and (CO)NHCH.sub.2CH.sub.2NMe.sub.2; a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid ester group (such as COOMe, COOEt, COOPr, COO-i-Pr, COO-n-Bu, COO-i-Bu, COO-t-Bu, CH.sub.2COOMe, CH.sub.2CH.sub.2COOMe, CH.sub.2CH.sub.2CH.sub.2COOMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOMe); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 amide group (such as CONH.sub.2, CONMeH, CONMe.sub.2, CONEtH, CONEtMe, CONEt.sub.2, CONPrH, CONPrMe, and CONPrEt); a substituted or unsubstituted sulphonyl group (such as SO.sub.2Me, SO.sub.2Et, SO.sub.2Pr, SO.sub.2iPr, SO.sub.2Ph, SO.sub.2-(2,3 or 4)-F-Ph, SO.sub.2-cyclopropyl, SO.sub.2CH.sub.2CH.sub.2OCH.sub.3), SO.sub.2NH.sub.2, SO.sub.2NHMe, SO.sub.2NMe.sub.2, SO.sub.2NHEt, SO.sub.2NEt.sub.2, SO2-pyrrolidine-N-yl, SO.sub.2-morpholine-N-yl, SO.sub.2NHCH.sub.2OMe, and SO.sub.2NHCH.sub.2CH.sub.2OMe; a substituted or unsubstituted aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-); and a saturated or unsaturated, substituted or unsubstituted, heterocyclic group including an aromatic heterocyclic group and/or a non-aromatic heterocyclic group (such as pyrrole-2-yl, pyrrole-3-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidine-2-yl, pyrimidine-4-yl, pyrimidine-5-yl, pyrazine-2-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-5-yl).

(61) Independently, in typical embodiments of the invention, R.sup.33 is selected from H and the following groups: a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as Me, Et, Pr, r, n-Bu, i-Bu, t-Bu, pentyl and hexyl); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3); an NH.sub.2 or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt); a substituted or unsubstituted amino-aryl group (such as NH-Ph, NH-(2,3 or 4)F-Ph, NH-(2,3 or 4)Cl-Ph, NH-(2,3 or 4)Br-Ph, NH-(2,3 or 4)I-Ph, NH-(2,3 or 4)Me-Ph, NH-(2,3 or 4)Et-Ph, NH-(2,3 or 4)Pr-Ph, NH-(2,3 or 4)Bu-Ph, NH-(2,3 or 4)OMe-Ph, NH-(2,3 or 4)OEt-Ph, NH-(2,3 or 4)OPr-Ph, NH-(2,3 or 4)OBu-Ph, NH-2,(3,4,5 or 6)F.sub.2-Ph, NH-2,(3,4,5 or 6)Cl.sub.2-Ph, NH-2,(3,4,5 or 6)Br.sub.2-Ph, NH-2,(3,4,5 or 6)I.sub.2-Ph, NH-2,(3,4,5 or 6)Me.sub.2-Ph, NH-2,(3,4,5 or 6)Et.sub.2-Ph, NH-2,(3,4,5, or 6)Pr.sub.2-Ph, NH-2,(3,4,5 or 6)Bu.sub.2-Ph, a substituted or unsubstituted cyclic amine or amino group (such as pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, and 4-keto-piperidinyl); a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group (such as CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid group (such as COOH, CH.sub.2COOH, CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH); a substituted or unsubstituted linear or branched carbonyl group (such as (CO)Me, (CO)Et, (CO)Pr, (CO)iPr, (CO)nBu, (CO)iBu, (CO)tBu, (CO)Ph, (CO)CH.sub.2Ph, (CO)CH.sub.2OH, (CO)CH.sub.2OCH.sub.3, (CO)CH.sub.2NH.sub.2, (CO)CH.sub.2NHMe, (CO)CH.sub.2NMe.sub.2, (CO)-cyclopropyl, (CO)-1,3-epoxypropan-2-yl; (CO)NH.sub.2, (CO)NHMe, (CO)NMe.sub.2, (CO)NHEt, (CO)NEt.sub.2, (CO)-pyrollidine-N-yl, (CO)-morpholine-N-yl, (CO)-piperazine-N-yl, (CO)N-methyl-piperazine-N-yl, (CO)NHCH.sub.2CH.sub.2OH, (CO)NHCH.sub.2CH.sub.2OMe, (CO)NHCH.sub.2CH.sub.2NH.sub.2, (CO)NHCH.sub.2CH.sub.2NHMe, and (CO)NHCH.sub.2CH.sub.2NMe.sub.2; a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid ester group (such as COOMe, COOEt, COOPr, COO-i-Pr, COO-n-Bu, COO-i-Bu, COO-t-Bu, CH.sub.2COOMe, CH.sub.2CH.sub.2COOMe, CH.sub.2CH.sub.2CH.sub.2COOMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOMe); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 amide group (such as CONH.sub.2, CONMeH, CONMe.sub.2, CONEtH, CONEtMe, CONEt.sub.2, CONPrH, CONPrMe, and CONPrEt); a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 amino carbonyl group (such as NHCO-Me, NHCO-Et, NHCO-Pr, NHCO-Bu, NHCO-pentyl, NHCO-hexyl, NHCO-Ph, NMe-CO-Me, NMe-CO-Et, NMe-CO-Pr, NMe-CO-Bu, NMe-CO-pentyl, NMe-CO-hexyl, NMe-CO-Ph; a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy or aryloxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, O-Ph, OCH.sub.2-Ph, OCH.sub.2-(2,3 or 4)-F-Ph, OCH.sub.2-(2,3 or 4)-Cl-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe); a substituted or unsubstituted linear or branched aminoalkoxy group (such as OCH.sub.2CH.sub.2NH.sub.2, OCH.sub.2CH.sub.2NHMe, OCH.sub.2CH.sub.2NMe.sub.2, OCH.sub.2CF.sub.2NHEt, and OCH.sub.2CH.sub.2NEt.sub.2; a substituted or unsubstituted sulphonyl group (such as SO.sub.2Me, SO.sub.2Et, SO.sub.2Pr, SO.sub.2iPr, SO.sub.2Ph, SO.sub.2-(2,3 or 4)-F-Ph, SO.sub.2 cyclopropyl, SO.sub.2CH.sub.2CH.sub.2OCH.sub.3), SO.sub.2NH.sub.2, SO.sub.2NHMe, SO.sub.2NMe.sub.2, SO.sub.2NHEt, SO.sub.2NEt.sub.2, SO2-pyrrolidine-N-yl, SO.sub.2-morpholine-N-yl, SO.sub.2NHCH.sub.2OMe, and SO.sub.2NHCH.sub.2CH.sub.2OMe; a substituted or unsubstituted aminosulphonyl group (such as NHSO.sub.2Me, NHSO.sub.2Et, NHSO.sub.2Pr, NHSO.sub.2iPr, NHSO.sub.2Ph, NHSO.sub.2-(2,3 or 4)-F-Ph, NHSO.sub.2-cyclopropyl, NHSO.sub.2CH.sub.2CH.sub.2OCH.sub.3); a substituted or unsubstituted aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-); and a substituted or unsubstituted saturated or unsaturated heterocyclic group including an aromatic heterocyclic group and/or a non-aromatic heterocyclic group (such as pyrrole-1-yl, pyrrole-2-yl, pyrrole-3-yl, pyrazole-1-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-1-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-1-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-1-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyrimidin-6-yl, pyrazine-2-yl, pyrrolidine-1-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-1-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-1-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-1-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-1-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-2-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-4-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-4-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-2-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-3-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-2-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-3-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, morpholine-4-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-2-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-4-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-1-yl, tetrazole-2-yl, tetrazole-5-yl).

(62) In more typical embodiments, R.sup.31 (and/or R.sup.32) is selected from a carbocyclic or heterocyclic group, which may be saturated or unsaturated, or aromatic or aliphatic, such as a substituted or unsubstituted phenyl group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-b-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-); or such as an aromatic heterocyclic group (such as pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, thiophen-2-yl, thiophen-3-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyrimidin-6-yl, tetrazole-1 yl, tetrazole-2-yl, tetrazole-3-yl, tetrazole-4-yl, tetrazole-5-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,3-thiazol)-2-yl, (1,3-thiazol)-4-yl, (1,3-thiazol)-5-yl, furan-2-yl, and furan-3-yl) or such as a substituted or unsubstituted saturated heterocyclic group (such as piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, tetrahydrofuran-2-yl, and tetrahydrofuran-3-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl).

(63) Typically, when the Y group comprises one of the following groups:

(64) ##STR00028##
then R.sup.31 (and/or R.sup.32) is preferably selected from the following: a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as Me, Et, Pr, n-Bu, i-Bu, t-Bu, pentyl and hexyl); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2P and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CF.sub.3, and CH.sub.2CF.sub.3); a substituted or unsubstituted cyclic amine or amido group (such as pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, and 4-keto-piperidinyl); a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl); a substituted or unsubstituted linear or branched C.sub.2-C.sub.6 alcohol group (such as CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH); a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy or aryloxy group linked through O via at least two further C atoms (such as CH.sub.2CH.sub.2OPh CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2OEt, CH.sub.2CH.sub.2OPr, CH.sub.2CH.sub.2OBu, CH.sub.2CH.sub.2CH.sub.2OPh, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe); a substituted or unsubstituted linear or branched C.sub.2-C.sub.6 carboxylic acid group (such as CH.sub.2COOH, CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH); a substituted or unsubstituted linear or branched carbonyl group (such as (CO)Me, (CO)Et, (CO)Pr, (CO)iPr, (CO)nBu, (CO)iBu, (CO)tBu, (CO)Ph, (CO)CH.sub.2Ph, (CO)CH.sub.2OH, (CO)CH.sub.2OCH.sub.3, (CO)CH.sub.2NH.sub.2, (CO)CH.sub.2NHMe, (CO)CH.sub.2NMe.sub.2, (CO)-cyclopropyl, (CO)-1,3-epoxypropan-2-yl; (CO)NH.sub.2, (CO)NHMe, (CO)NMe.sub.2, (CO)NHEt, (CO)NEt.sub.2, (CO)-pyrollidine-N-yl, (CO)-morpholine-N-yl, (CO)-piperazine-N-yl, (CO)N-methyl-piperazine-N-yl, (CO)NHCH.sub.2CH.sub.2OH, (CO)NHCH.sub.2CH.sub.2OMe, (CO)NHCH.sub.2CH.sub.2NH.sub.2, (CO)NHCH.sub.2CH.sub.2NHMe, and (CO)NHCH.sub.2CH.sub.2NMe.sub.2; a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid ester group (such as COOMe, COOEt, COOPr, COO-i-Pr, COO-n-Bu, COO-i-Bu, COO-t-Bu, CH.sub.2COOMe, CH.sub.2CH.sub.2COOMe, CH.sub.2CH.sub.2CH.sub.2COOMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOMe); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 amide group (such as CONH.sub.2, CONMeH, CONMe.sub.2, CONEtH, CONEtMe, CONEt.sub.2, CONPrH, CONPrMe, and CONPrEt); a substituted or unsubstituted sulphonyl group (such as SO.sub.2Me, SO.sub.2Et, SO.sub.2Pr, SO.sub.2iPr, SO.sub.2Ph, SO.sub.2-(2,3 or 4)-F-Ph, SO.sub.2 cyclopropyl, SO.sub.2CH.sub.2CH.sub.2OCH.sub.3), SO.sub.2NH.sub.2, SO.sub.2NHMe, SO.sub.2NMe.sub.2, SO.sub.2NHEt, SO.sub.2NEt.sub.2, SO2-pyrrolidine-N-yl, SO.sub.2-morpholine-N-yl, SO.sub.2NHCH.sub.2OMe, and SO.sub.2NHCH.sub.2CH.sub.2OMe; a substituted or unsubstituted aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 34-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-); and a saturated or unsaturated, substituted or unsubstituted, heterocyclic group including an aromatic heterocyclic group and/or a non-aromatic heterocyclic group (such as pyrrole-2-yl, pyrrole-3-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidine-2-yl, pyrimidine-4-yl, pyrimidine-5-yl, pyrazine-2-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-5-yl).

(65) More preferably, when the Y group comprises one of the following groups:

(66) ##STR00029##
then R.sup.31 (and/or R.sup.32) is preferably selected from a carbocyclic or heterocyclic group, which may be saturated or unsaturated, or aromatic or aliphatic, such as a substituted or unsubstituted phenyl group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-b-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-); or such as an aromatic heterocyclic group (such as pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, thiophen-2-yl, thiophen-3-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyrimidin-6-yl, tetrazole-1 yl, tetrazole-2-yl, tetrazole-3-yl, tetrazole-4-yl, tetrazole-5-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,3-thiazol)-2-yl, (1,3-thiazol)-4-yl, (1,3-thiazol)-5-yl, furan-2-yl, and furan-3-yl) or such as a substituted or unsubstituted saturated heterocyclic group (such as piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, tetrahydrofuran-2-yl, and tetrahydrofuran-3-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl).

(67) Typically, when the Y group comprises the following group:

(68) ##STR00030##
then R.sup.31 is typically a COR.sup.311 group or an SO.sub.2R.sup.311 group:

(69) ##STR00031##
wherein R.sup.311 is selected from: a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as Me, Et, Pr, i-Pr, n-Bu, i-Bu, t-Bu, pentyl and hexyl); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CF.sub.3, CH.sub.2CF.sub.3); an NH.sub.2 or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt); a substituted or unsubstituted amino-aryl group (such as NH-Ph, NH-(2,3 or 4)F-Ph, NH-(2,3 or 4)Cl-Ph, NH-(2,3 or 4)Br-Ph, NH-(2,3 or 4)I-Ph, NH-(2,3 or 4)Me-Ph, NH-(2,3 or 4)Et-Ph, NH-(2,3 or 4)Pr-Ph, NH-(2,3 or 4)Bu-Ph, NH-(2,3 or 4)OMe-Ph, NH-(2,3 or 4)OEt-Ph, NH-(2,3 or 4)OPr-Ph, NH-(2,3 or 4)OBu-Ph, NH-2,(3,4,5 or 6)F.sub.2-Ph, NH-2,(3,4,5 or 6)Cl.sub.2-Ph, NH-2,(3,4,5 or 6)Br.sub.2-Ph, NH-2,(3,4,5 or 6)I.sub.2-Ph, NH-2,(3,4,5 or 6)Me.sub.2-Ph, NH-2,(3,4,5 or 6)Et.sub.2-Ph, NH-2,(3,4,5, or 6)Pr.sub.2-Ph, NH-2,(3,4,5 or 6)Bu.sub.2-Ph, a substituted or unsubstituted cyclic amine or amido group (such as pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, and 4-keto-piperidinyl); a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group (such as CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH); a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 amino carbonyl group (such as NHCO-Me, NHCO-Et, NHCO-Pr, NHCO-Bu, NHCO-pentyl, NHCO-hexyl, NHCO-Ph, NMe-CO-Me, NMe-CO-Et, NMe-CO-Pr, NMe-CO-Bu, NMe-CO-pentyl, NMe-CO-hexyl, NMe-CO-Ph; a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy or aryloxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, O-Ph, OCH.sub.2-Ph, OCH.sub.2-(2,3 or 4)-F-Ph, OCH.sub.2-(2,3 or 4)-Cl-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe); a substituted or unsubstituted linear or branched aminoalkoxy group (such as OCH.sub.2CH.sub.2NH.sub.2, OCH.sub.2CH.sub.2NHMe, OCH.sub.2CH.sub.2NMe.sub.2, OCH.sub.2CH.sub.2NHEt, and OCH.sub.2CH.sub.2NEt.sub.2; a substituted or unsubstituted aminosulphonyl group (such as NHSO.sub.2Me, NHSO.sub.2Et, NHSO.sub.2Pr, NHSO.sub.2iPr, NHSO.sub.2Ph, NHSO.sub.2-(2,3 or 4)-F-Ph, NHSO.sub.2-cyclopropyl, NHSO.sub.2CH.sub.2CH.sub.2OCH.sub.3); a substituted or unsubstituted aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-); a saturated or unsaturated, substituted or unsubstituted, heterocyclic group including an aromatic heterocyclic group and/or a non-aromatic heterocyclic group (such as pyrrole-2-yl, pyrrole-3-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidine-2-yl, pyrimidine-4-yl, pyrimidine-5-yl, pyrazine-2-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-5-yl);
preferably wherein R.sup.311 is selected from the following: a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as Me, Et, Pr, i-Pr, n-Bu, i-Bu, t-Bu, pentyl and hexyl); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph); a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl); a substituted or unsubstituted aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-); a saturated or unsaturated, substituted or unsubstituted, heterocyclic group including an aromatic heterocyclic group and/or a non-aromatic heterocyclic group (such as pyrrole-2-yl, pyrrole-3-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidine-2-yl, pyrimidine-4-yl, pyrimidine-5-yl, pyrazine-2-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-5-yl).

(70) In more typical embodiments, R.sup.32 is selected from H or a C.sub.1-C.sub.6 alkyl group (such as Me, Et, Pr, i-Pr, n-Bu, i-Bu, t-Bu, pentyl and hexyl).

(71) In more typical embodiments, R.sup.33 is selected from H, a substituted or unsubstituted C.sub.1-C.sub.6 alkyl group, an NH.sub.2 group or a substituted or unsubstituted C.sub.1-C.sub.6 amino group, a substituted or unsubstituted C.sub.1-C.sub.6 alkoxy group, and a nitrile group.

(72) In some typical embodiments, the present invention provides a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula:

(73) ##STR00032##
wherein X.sup.1, X.sup.2, and X.sup.7, may be the same or different and each is independently selected from C and N; X.sup.3, X.sup.4, X.sup.5, and X.sup.6 may be the same or different and each is independently selected from C, N, O and S wherein when X.sup.3 is N it has a double bond and wherein when X.sup.6 is N it has a double bond; the dotted line is a bond which may be present or absent; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that at least one of R.sup.2, R.sup.3, R.sup.4 and R.sup.6 comprises a group Y; and provided that the number of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 groups present is such that the respective valencies of X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.6, and X.sup.7 are maintained; and wherein Y is a group having a formula selected from the following:

(74) ##STR00033##
wherein L may be present or absent, and may be a substituted or unsubstituted organic linking group, and R.sup.31 and R.sup.32 may be the same or different and are selected from H and a substituted or unsubstituted organic group, X.sup.8 is selected from C and N, and each R.sup.313 may be the same or different and is selected from H and a substituted or unsubstituted organic group,
and wherein if Y is a group of the following formula:

(75) ##STR00034##
in which L is absent, R.sup.32 is H, and R.sup.31 comprises a carbonyl group directly bonded to the N, (or R.sup.31 is H, and R.sup.32 comprises a carbonyl group directly bonded to the N) then Y is a group having the following formula:

(76) ##STR00035##
wherein R.sup.312 is selected from any of the following: a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as Me, Et, Pr, r, n-Bu, i-Bu, t-Bu, pentyl and hexyl); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CF.sub.3, CH.sub.2CF.sub.3); an NH.sub.2 or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt); a substituted or unsubstituted amino-aryl group (such as NH-Ph, NH-(2,3 or 4)F-Ph, NH-(2,3 or 4)Cl-Ph, NH-(2,3 or 4)Br-Ph, NH-(2,3 or 4)I-Ph, NH-(2,3 or 4)Me-Ph, NH-(2,3 or 4)Et-Ph, NH-(2,3 or 4)Pr-Ph, NH-(2,3 or 4)Bu-Ph, NH-(2,3 or 4)OMe-Ph, NH-(2,3 or 4)OEt-Ph, NH-(2,3 or 4)OPr-Ph, NH-(2,3 or 4)OBu-Ph, NH-2,(3,4,5 or 6)F.sub.2-Ph, NH-2,(3,4,5 or 6)Cl.sub.2-Ph, NH-2,(3,4,5 or 6)Br.sub.2-Ph, NH-2,(3,4,5 or 6)I.sub.2-Ph, NH-2,(3,4,5 or 6)Me.sub.2-Ph, NH-2,(3,4,5 or 6)Et.sub.2-Ph, NH-2,(3,4,5, or 6)Pr.sub.2-Ph, NH-2,(3,4,5 or 6)Bu.sub.2-Ph, a substituted or unsubstituted cyclic amine or amido group (such as pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, and 4-keto-piperidinyl); a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl); a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group (such as CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH); a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 amino carbonyl group (such as NHCO-Me, NHCO-Et, NHCO-Pr, NHCO-Bu, NHCO-pentyl, NHCO-hexyl, NHCO-Ph, NMe-CO-Me, NMe-CO-Et, NMe-CO-Pr, NMe-CO-Bu, NMe-CO-pentyl, NMe-CO-hexyl, NMe-CO-Ph; a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy or aryloxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, O-Ph, OCH.sub.2-Ph, OCH.sub.2-(2,3 or 4)-F-Ph, OCH.sub.2-(2,3 or 4)-Cl-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe); a substituted or unsubstituted linear or branched aminoalkoxy group (such as OCH.sub.2CH.sub.2NH.sub.2, OCH.sub.2CH.sub.2NHMe, OCH.sub.2CH.sub.2NMe.sub.2, OCH.sub.2CH.sub.2NHEt, and OCH.sub.2CH.sub.2NEt.sub.2; a substituted or unsubstituted aminosulphonyl group (such as NHSO.sub.2Me, NHSO.sub.2Et, NHSO.sub.2Pr, NHSO.sub.2iPr, NHSO.sub.2Ph, NHSO.sub.2-(2,3 or 4)-F-Ph, NHSO.sub.2-cyclopropyl, NHSO.sub.2CH.sub.2CH.sub.2OCH.sub.3); a substituted or unsubstituted 6 membered carbocyclic or heterocyclic aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2-00)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-, pyridin-2-yl, pyridine-3-yl, pyridin-4-yl, pyrimidin-2-yl, pyrimidin-5-yl, pyrimidin-4-yl, pyridazin-3-yl, pyridazine-4-yl); a substituted or unsubstituted saturated heterocyclic group (such as piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, tetrahydrofuran-2-yl, and tetrahydrofuran-3-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl);
preferably wherein R.sup.312 is selected from the following: a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph); a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl); a substituted or unsubstituted 6 membered carbocyclic or heterocyclic aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-, pyridin-2-yl, pyridine-3-yl, pyridin-4-yl, pyrimidin-2-yl, pyrimidin-5-yl, pyrimidin-4-yl, pyridazin-3-yl, pyridazine-4-yl); a substituted or unsubstituted saturated heterocyclic group (such as piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, tetrahydropyran-2-yl, and tetrahydrofuran-3-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl).

(77) Thus, the present invention provides a TDO or IDO inhibitor compound for use in medicine, which compound comprises a formula selected from one of the following:

(78) ##STR00036## ##STR00037## ##STR00038## ##STR00039## ##STR00040## ##STR00041## ##STR00042## ##STR00043## ##STR00044## ##STR00045## ##STR00046## ##STR00047##

(79) Typically, the above formulae (and all formulae herein) are shown in non-stereoisomeric form. For the avoidance of doubt, throughout the present disclosure a single formula is intended to represent all possible stereoisomers of a particular structure, including all possible isolated enantiomers corresponding to the formula, all possible mixtures of enantiomers corresponding to the formula, all possible mixtures of diastereomers corresponding to the formula, all possible mixtures of epimers corresponding to the formula and all possible racemic mixtures corresponding to the formula. In addition to this, the above formulae (and all formulae herein) are intended to represent all tautomeric forms equivalent to the corresponding formula.

(80) In the context of the present invention, the medicinal use is not especially limited, provided that it is a use which is facilitated by the TDO and/or the IDO inhibitory effect of the compound. Thus, the compounds of the invention may be for use in any disease, condition or disorder that may be prevented, ameliorated or treated using a TDO and/or IDO inhibitor. Typically this comprises a disease condition and/or a disorder selected from: a cancer, an inflammatory condition, an infectious disease, a central nervous system disease or disorder, coronary heart disease, chronic renal failure, post anaesthesia cognitive dysfunction, a disease condition and/or a disorder relating to female reproductive health including contraception or abortion, and cataracts.

(81) When the disease, condition or disorder is an inflammatory disease, condition or disorder, it is not especially limited, provided that the disease, condition or disorder is one which may be treated, prevented or ameliorated by using a TDO and/or IDO inhibitor. However, typically the inflammatory condition is a condition relating to immune B cell, T cell, dendritic cell, natural killer cell, macrophage, and/or neutrophil dysregulation.

(82) When the disease, condition or disorder is a cancer, it is not especially limited, provided that the cancer is one which may be treated, prevented or ameliorated by using a TDO and/or IDO inhibitor. Thus the cancer may be a cancer selected from: a solid or liquid tumour including cancer of the eye, brain (such as gliomas, glioblastomas, medullablastomas, craniopharyngioma, ependymoma, and astrocytoma), spinal cord, kidney, mouth, lip, throat, oral cavity, nasal cavity, small intestine, colon, parathyroid gland, gall bladder, head and neck, breast, bone, bile duct, cervix, heart, hypopharyngeal gland, lung, bronchus, liver, skin, ureter, urethra, testicles, vagina, anus, laryngeal gland, ovary, thyroid, oesophagus, nasopharyngeal gland, pituitary gland, salivary gland, prostate, pancreas, adrenal glands; an endometrial cancer, oral cancer, melanoma, neuroblastoma, gastric cancer, an angiomatosis, a hemangioblastoma, a pheochromocytoma, a pancreatic cyst, a renal cell carcinoma, Wilms' tumour, squamous cell carcinoma, sarcoma, osteosarcoma, Kaposi sarcoma, rhabdomyosarcoma, hepatocellular carcinoma, PTEN Hamartoma-Tumor Syndromes (PHTS) (such as Lhermitte-Duclos disease, Cowden syndrome, Proteus syndrome, and Proteus-like syndrome), leukaemias and lymphomas (such as acute lymphoblastic leukaemia, chronic lymphocytic leukaemia, acute myelogenous leukaemia, chronic myelogenous leukaemia, hairy cell leukaemia, T-cell prolymphocytic leukemia (T-PLL), large granular lymphocytic leukemia, adult T-cell leukemia, juvenile myelomonocytic leukaemia, Hodgkin lymphoma, non-Hodgkin lymphoma, mantle lymphoma, follicular lymphoma, primary effusion lymphoma, AIDS-related lymphoma, Hodgkin lymphoma, diffuse B cell lymphoma, Burkitt lymphoma, and cutaneous T-cell lymphoma). However, when the compound is an IDO inhibitor, typically (but not exclusively) the cancer is a cancer selected from acute myeloid leukemia (AML), a small-cell lung cancer, a melanoma, an ovarian cancer, a colorectal cancer, a pancreatic cancer, an endometrial cancer, and a skin papilloma. When the compound is a TDO inhibitor, typically (but not exclusively) the cancer is a cancer selected from a glioma, and a hepatocellular carcinoma.

(83) When the disease is an infectious disease, it is not especially limited, provided that the disease is one which may be treated, prevented or ameliorated by using a TDO and/or IDO inhibitor. However, typically the infectious disease is selected from a bacterial infection and a viral infection, preferably a gut infection, sepsis, and sepsis induced hypotension.

(84) When the disease, condition or disorder is a central nervous system disease, condition or disorder, it is not especially limited, provided that the disease, condition or disorder is one which may be treated, prevented or ameliorated by using a TDO and/or IDO inhibitor. However, the central nervous system disease, condition or disorder is typically selected from amyotrophic lateral sclerosis (AML), Huntington's disease, Alzheimer's disease, pain, a psychiatric disorder, multiple sclerosis, Parkinson's disease, and HIV related neurocognitive decline.

(85) When the disease, condition or disorder is one relating to female reproductive health, it is not especially limited provided that the disease, condition or disorder is one which may be treated, prevented or ameliorated by using a TDO and/or IDO inhibitor. In typical embodiments the disease, condition or disorder is selected from gynaecological disorders such as endometriosis. Conditions relating to female reproductive health that are included in the invention include contraception and abortion such that the compounds of the invention may be used as a contraceptive and/or abortive agent.

(86) The present invention also provides a pharmaceutical composition comprising a compound as defined above. Whilst the pharmaceutical composition is not especially limited, typically the composition further comprises a pharmaceutically acceptable additive and/or excipient. In the pharmaceutical composition, the compound as defined above may be present in the form described above, but may alternatively be in a form suitable for improving bioavailability, solubility, and/or activity, and/or may be in a form suitable for improving formulation. Thus, the compound may be in the form of a pharmaceutically acceptable salt, hydrate, acid, ester, or other alternative suitable form. Typically, the composition is for treating a disease, condition or disorder as defined above.

(87) In some embodiments the pharmaceutical composition is a composition for treating a cancer, further comprising a further agent for treating cancer. The further agent for treating cancer is not especially limited, provided that it affords some utility for cancer treatment. However, typically the further agent for treating cancer is selected from anti-microtubule agents, platinum coordination complexes, alkylating agents, antibiotic agents, topoisomerase II inhibitors, antimetabolites, topoisomerase I inhibitors, hormones and hormone analogues, signal transduction pathway inhibitors, non-receptor tyrosine kinase angiogenesis inhibitors, immunotherapeutic agents, proapoptotic agents and cell cycle signalling inhibitors. An immunotherapeutic agent may consist of but is not limited to an anti-tumour vaccine, an oncolytic virus, an immune stimulatory antibody such as anti-CTLA4, anti-PD1, anti-PDL-1, anti-OX40, anti-41BB, anti-CD27, anti-CD40, anti-LAGS, anti-TIM3, and anti-GITR, a novel adjuvant, a peptide, a cytokine, a chimeric antigen receptor T cell therapy (CAR-T), a small molecule immune modulator, tumour microenvironment modulators, and anti-angiogenic agents.

(88) In still further embodiments the invention provides a pharmaceutical kit for treating a cancer, which pharmaceutical kit comprises: (a) a compound as defined above; and (b) a further agent for treating cancer; preferably wherein the further agent for treating cancer is selected from anti-microtubule agents, platinum coordination complexes, alkylating agents, antibiotic agents, topoisomerase II inhibitors, antimetabolites, topoisomerase I inhibitors, hormones and hormone analogues, signal transduction pathway inhibitors, non-receptor tyrosine kinase angiogenesis inhibitors, immunotherapeutic agents, proapoptotic agents and cell cycle signalling inhibitors;
wherein the compound and the further agent are suitable for administration simultaneously, sequentially or separately.

(89) Further provided by the invention is a method of treating a disease and/or a condition and/or a disorder, which method comprises administering to a patient (or subject) a compound, or a composition, or a kit as defined above. The method is typically a method for treating any disease condition or disorder mentioned herein. In typical embodiments, the method is a method for treating a cancer. Preferably such a method comprises administering to a patient (or subject) a compound or a composition as defined above and a further agent for treating cancer as defined above. The compound or composition and the further agent may administered simultaneously, sequentially or separately, depending upon the agents and patients involved, and the type of cancer indicated.

(90) Typically, in all embodiments of the invention, both above and below, the patient (or subject) is an animal, typically a mammal, and more typically a human.

(91) In addition to compounds for use in medicine, the present invention, and in particular the synthetic method, provides compounds that were not previously known, such compounds comprising a formula selected from one of the following:

(92) ##STR00048## ##STR00049## ##STR00050## ##STR00051## ##STR00052## ##STR00053## ##STR00054## ##STR00055## ##STR00056## ##STR00057## ##STR00058## ##STR00059##

(93) Typically, the above formulae (and all formulae herein) are shown in non-stereoisomeric form. For the avoidance of doubt, throughout the present disclosure a single formula is intended to represent all possible stereoisomers of a particular structure, including all possible isolated enantiomers corresponding to the formula, all possible mixtures of enantiomers corresponding to the formula, all possible mixtures of diastereomers corresponding to the formula, all possible mixtures of epimers corresponding to the formula and all possible racemic mixtures corresponding to the formula. In addition to this, the above formulae (and all formulae herein) are intended to represent all tautomeric forms equivalent to the corresponding formula.

(94) Further provided by the invention is a method of synthesis of novel compounds, as defined above, which method comprises a step of reacting a compound having one of the following formulae:

(95) ##STR00060##
wherein the groups R and X are as defined anywhere herein; the dotted lines are bonds which may be present or absent; and wherein P is a precursor group to group Y, in order to form the group Y from P and produce a compound having one of the following formulae:

(96) ##STR00061##

(97) The skilled person may select the type of reagents, and the reaction conditions, with reference to known synthesis techniques. In some embodiments, the method comprises one or more additional substitution steps. Exemplary syntheses are shown in the Examples.

(98) The invention will now be described in more detail, by way of example only, with reference to the following specific embodiments.

EXAMPLES

Example 1

Methods of Synthesis

(99) The following three syntheses are representative exemplary methods by which the compounds of the present invention may be synthesised:

(100) ##STR00062##

(101) All three syntheses may be performed using reagents and reaction conditions suitable for similar reactions known in the field. All the compounds of the present invention may be produced by employing analogous syntheses.

(102) Some specific syntheses of compounds of the present invention are set out in the following.

Synthesis of Compound 45

(103) ##STR00063##

(104) Reagents were purchased from the commercial sources and were used as received. .sup.1H NMR spectra were obtained on a Bruker AVANCE 300 spectrometer at 300 MHz and a Bruker AVANCE 400 spectrometer at 400 MHz with tetramethylsilane used as an internal reference. Thin-layer chromatography (TLC) was performed using Whatman No. 4500-101 (Diamond No. MK6F silica-gel 60 ) plates. Visualization of TLC plates was performed using UV light (254 nm). The mass spectra were obtained on a Finnigan LCQ-DUO spectrometer using electrospray ionization. HPLC analyses were performed on an Agilent 1100 Series instrument. Impurities are expressed as % AUC by HPLC and are non-validated.

Preparation of 5-(4-(methylsulfonyl)piperazin-1-yl)isoquinoline (45)

(105) A stirred solution of 1001 (100 mg, 0.48 mmol) in toluene (1.0 mL) was charged with 1002 (78 mg, 0.48 mmol), t-BuOK (107 mg, 0.96 mmol) and the mixture was purged with argon for 20 min. Pd.sub.2(dba).sub.3 (21 mg, 0.02 mmol) and BINAP (22 mg, 0.03 mmol) were added into this mixture and refluxed at 110 C. for 16 h. The mixture was cooled to room temperature and concentrated under reduced pressure. The resultant dark brown slurry was filtered through Celite pad and pad was washed with ethyl acetate (30 mL). The solvent was concentrated in vacuo to give a dark brown residue. This residue was further purified by Combiflash column chromatography using 12 g Redisep column (hexane/EtOAc, 1:1) to afford 45 (20 mg, 14%) as an off-white solid.

(106) MS (MM) m/z 292 [M+H].sup.+;

(107) HPLC: 95.9%, Eclipse XDB C-18, 220 nm;

(108) .sup.1H NMR (300 MHz, DMSO-d.sub.6): 9.29 (s, 1H), 8.52 (d, J=5.1 Hz, 1H), 7.92 (d, J=4.8 Hz, 1H), 7.82 (d, J=7.5 Hz, 1H), 7.62 (t, J=7.2 Hz, 1H), 7.40 (d, J=6.9 Hz, 1H), 3.42 (bs, 4H), 3.14 (bs, 4H), 2.99 (s, 3H).

Synthesis of Compound 28

(109) ##STR00064##

(110) A solution 1003 (75 mg, 0.29 mmol) in CH.sub.2Cl.sub.2 (5 mL) was treated with pyridine (0.1 mL) followed by 1004 (42 mg, 0.29 mmol) at 0 C. After being stirred at room temperature for 1 h, the reaction mixture was diluted with CH.sub.2Cl.sub.7 (15 mL), washed with water (5 mL) and brine (5 mL). The organic phase was separated, dried over anhydrous Na.sub.2SO.sub.4, filtered and concentrated in vacuo to give a brown solid residue. This residue was further purified by Combiflash column chromatography using 4 g Redisep column (hexane/EtOAc, 1:1) to afford 28 (35 mg, 33%) as an off-white solid.

(111) MS (MM) m/z 356 [M+H].sup.+;

(112) HPLC: 99%, Symmetry C-18 column, 220 nm;

(113) .sup.1H NMR (300 MHz, DMSO-d.sub.6): 10.3 (s, 1H), 9.48 (s, 1H), 8.50 (d, J=6.3 Hz, 1H), 8.09 (t, J=9.0 Hz, 2H), 7.72 (t, J=8.1 Hz, 1H), 7.58 (d, J=7.5 Hz, 1H), 6.86-6.84 (m, J=2H), 6.69 (d, J=8.4 Hz, 1H), 4.23 (t, J=3.9 Hz, 2H), 3.21 (t, J=3.9 Hz, 2H), 2.69 (s, 3H)

Synthesis of Compound 52

(114) ##STR00065##

(115) A solution of 1005 (100 mg, 0.45 mmol) in CH.sub.2Cl.sub.2 (5 mL) was treated with Et.sub.3N (0.25 mL, 1.8 mmol) followed by 1006 (106 mg, 0.45 mmol) at 0 C. After being stirred at room temperature for 4 h, the reaction mixture was diluted with CH.sub.2Cl.sub.2 (15 mL), washed with water (5 mL) and brine (5 mL). The organic phase was separated, dried over anhydrous Na.sub.2SO.sub.4, filtered and concentrated in vacuo to give a yellow color solid. This residue was further purified by preparative TLC (hexanes/EtOAc, 1:1) to afford 52 (20 mg, 13%) as a light yellow solid.

(116) MS (MM) m/z 347 [M+H].sup.+;

(117) HPLC: 97.5%, Eclipse XBD C18, 254 nm;

(118) .sup.1H NMR (400 MHz, DMSO-d.sub.6): 8.28 (s, 1 H), 8.27 (d, J=3.6 Hz, 1H), 8.02 (d, J=8.8 Hz, 1H), 7.78 (d, J=8.8 Hz, 2H), 7.11-7.09 (m, 3 H), 4.78-4.72 (m, 1 H), 4.28 (q, J=8.4 Hz, 1 H), 2.66-2.62 (m, 2 H), 1.79-1.76 (m, 1 H), 1.63-1.59 (m, 2 H), 1.54-1.49 (m, 1 H), 1.30 (d, J=6.0 Hz, 6 H)

Example 2

Assays

(119) Exemplary compounds of the invention were prepared, and tested to determine their effect as TDO and/or IDO inhibitors. Two different assays were employed: 1. a cell-based assay for detecting the effect of test compounds on kynurenine production in two different cancer cell types. This assay utilised cancer cells which expressed either TDO or IDO and as such was used as a means of testing compound activity at these two enzymes in a cell-based context. 2. a TDO and IDO biochemical coupled assay which utilised recombinantly produced and purified TDO and IDO enzymes in combination with the enzyme formamidase. This coupled enzyme system allowed conversion of N-formylkynurenine produced by TDO or IDO activity to kynurenine which was then quantified by fluorescence following addition of Erhlich's Reagent The protocols for these are set out below.

(120) Cell Based Assay for Detection of Kynurenine Produced by TDO and/or IDO

(121) A172 (human glioblastoma) and SKOV3 (human ovarian adenocarcinoma) cells were seeded in a 96 well plate at 30,000 or 40,000 cells per well respectively in phenol red-free RPMI supplemented with 10% FCS, 2 mM L-glutamine and 500 M L-tryptophan. IDO expression was induced in the SKOV3 cells by the addition of 500 ng/ml IFN-. Cells were incubated at 37 C. with or without the addition of test compound. After 48 hours, the cells were removed by centrifugation and Erhlich's reagent was added to the supernatant. The Erhlich's reagent was incubated for 5 minutes before the absorbance was read at 490 nM.

(122) TDO and IDO Biochemical Coupled Assay

(123) Recombinant human IDO or TDO was incubated in 50 mM KPO4 (pH 7.0), 0.5 mM EGTA, 0.5 mM EDTA, 0.05% Triton X100, 20 mM ascorbate, 10 M methylene blue, 500 U/ml catalase, 50 g/ml KynB (kynurenine formamidase). TDO assays were carried out in the presence of 330 M L-tryptophan, while IDO assays had the addition of 45 M L-tryptophan. After incubation for 17 minutes at room temperature the reactions were stopped by the addition of Erhlich's reagent and incubated at room temperature for 5 minutes before the fluorescence was read (Ex475, Em530).

(124) The pIC50 values for a variety of test compounds are shown in Table 1 and Table 2.

(125) TABLE-US-00001 TABLE 1 pIC50 values for Kynurenine cell-based assays determined for test compounds A172 Kynurenine SKOV3 Kynurenine cell based cell based assay Compound assay pIC50 pIC50 1 + + 2 + + 3 + +/ 4 + +/ 5 +/ + 6 + ++ 7 +/ + 8 ++ ++ 9 +++ ++ 10 +/ ++ 11 ++ ++ 12 ++ ++ 13 ++ ++ 14 +++ ++ 15 ++ +/ 16 ++ ++ 17 +++ ++ 18 +/ + 19 +++ +++ 20 +++ +++ 21 ++ ++ 22 +++ + 23 +/ + 24 +/ ++ 25 +++ +++ 26 +++ ++ 27 +++ ++ 28 +++ ++ 29 ++ ++ 30 +/ + 31 +/ +++ 32 +/ + 33 +/ + 34 +/ + 35 +++ ++ 36 +/ + 37 + +/ 38 + + 39 +/ + 40 + + 41 +/ + 42 + + 43 +/ + 44 + ++ 45 +/ + 46 + ++ 47 ++ ++ 48 +/ + 49 +/ + 50 +/ +++ 51 +/ ++ 52 +/ +++ 53 + + 54 + + 55 + ++ 56 +/ + 57 +/ ++ 58 +/ ++ Key: +++ = pIC.sub.50 5.50 ++ = pIC.sub.50 4.50-5.49 + = pIC.sub.50 4.00-4.49 +/ = pIC.sub.50 <4.00

(126) TABLE-US-00002 TABLE 2 pIC50 values for IDO and TDO inhibition determined for test compounds hIDO hTDO biochemical biochemical Compound assay pIC50 assay pIC50 1 ++ ++ 2 +/ ++ 3 +/ + 4 ++ +++ 6 +++ +++ 9 ++ ++ 14 ++ + 16 ++ + 56 + +/ 57 + +/ 58 + +/ Key: +++ = pIC.sub.50 5.50 ++ = pIC.sub.50 4.50-5.49 + = pIC.sub.50 4.00-4.49 +/ = pIC.sub.50 <4.00

(127) The Table shows that a large number of the test compounds show strong TDO and IDO inhibitory function.