Patent ID: 6417218
Filing Date: 2002-07-09
Classification: A61P,C07D

Abstract:
A compound of formula I wherein the carbocyclic ring does or does not contain one or two double bonds;n represents 1 or 2; R1 is hydrogen or a functional group which can be converted to hydrogen in vivo; R2 is hydrogen, C1-6-alkyl, cyano or halogen; R3 is hydrogen, hydroxy or halogen; R4 is hydrogen, hydroxy or cyano; R5 is hydrogen; aryl unsubstituted or substituted with halogen, C1-6alkoxy, C1-6-alkyl, trifluoromethyl, C3-8-cycloalkyl, aryl or heteroaryl; C1-6-alkyl unsubstituted or substituted with C3-8-cycloalkyl unsubstituted or substituted with halogen, C1-6-alkoxy, C1-6-alkyl, trifluoromethyl, C3-8-cycloalkyl, aryl or heteroaryl; aryl unsubstituted or substituted with halogen, C1-6-alkoxy, C1-6-alkyl, trifluoromethyl, C3-8-cycloalkyl, aryl or heteroaryl; or heteroaryl unsubstituted or substituted with halogen, C1-6-alkoxy, C1-6-alkyl, trifluoromethyl, C3-8-cycloalkyl, aryl or heteroaryl; â€”Xâ€”R6 wherein X is â€”Oâ€” or â€”Sâ€”; and R6 is hydrogen; C1-6-alkyl unsubstituted or substituted with halogen, C1-6-alkoxy, trifluoromethyl, C3-8-cycloalkyl, aryl or heteroaryl where the C3-8-cycloalkyl, aryl and heteroaryl groups are unsubstituted or substituted with halogen, C1-6-alkoxy, C1-6-alkyl, trifluoromethyl, cyano, C3-8-cycloalkyl, aryl or heteroaryl; C3-8-cycloalkyl unsubstituted or substituted with halogen, C1-6-alkoxy, C1-6-alkyl, trifluoromethyl, C3-8-cycloalkyl, aryl or heteroaryl; aryl unsubstituted or substituted with halogen, C1-6-alkoxy, C1-6-alkyl, trifluoromethyl, cyano, C3-8-cycloalkyl, aryl or heteroaryl; heteroaryl unsubstituted or substituted with halogen, C1-6-alkoxy, C1-6-alkyl, trifluoromethyl, C3-8-cycloalkyl, aryl or heteroaryl; â€”CONR7R8 wherein R7 and R8 independently are hydrogen; C1-6-alkyl unsubstituted or substituted with halogen, C1-6-alkoxy, trifluoromethyl, C3-8-cycloalkyl, aryl or heteroaryl where the C3-8-cycloalkyl, aryl and heteroaryl groups are unsubstituted or substituted with halogen, C1-6-alkoxy, C1-6-alkyl, trifluoromethyl, cyano, C3-8-cycloalkyl, aryl or heteroaryl; C3-8-cycloalkyl unsubstituted or substituted with halogen, C1-6-alkoxy, C1-6-alkyl, trifluoromethyl, C3-8-cycloalkyl, aryl or heteroaryl; aryl unsubstituted or substituted with halogen, C1-6-alkoxy, C1-6-alkyl, trifluoromethyl, cyano, C3-8-cycloalkyl, aryl or heteroaryl; or heteroaryl unsubstituted or substituted with halogen, C1-6-alkoxy, C1-6-alkyl, trifluoromethyl, C3-8-cycloalkyl, aryl or heteroaryl; or R7 and R8 together form a 3 to 8 membered, saturated or unsaturated carbocyclic or heterocyclic ring which is unsubstituted or substituted with halogen, C1-6-alkoxy, C1-6-alkyl, trifluoromethyl, C3-8-cycloalkyl, aryl or heteroaryl; or â€”SO2R7; provided that when X is â€”Sâ€”, R6 must not be hydrogen, â€”CONR7R8 or â€”SO2R7; or â€”CONR7R8; or R4 and R5 taken together represent &boxH;O; â€ƒprovided that when R2 is hydrogen, then R3, R4 or R5 must not be methyl or ethyl in the 1 position; when n is 2, R1 is â€”CPh3, R2 and R3 are hydrogen and R4 is cyano in the 1 position, then R5 must not be hydrogen; when n is 2 and R1, R2, R3 and R4 are hydrogen, then R5 must not be hydrogen; and when n is 1 or 2, and R1, R2, R3 and R4 are hydrogen, then R5 must not be hydroxy; or any optical or geometric isomer or tautomeric form thereof or a pharmaceutically acceptable salt thereof.