1-IMIDAZOLGEMETHYL BENZOFURAN DERIVATIVES AS INHIBITORS OF ANGIOTENSIN II ACTIVITY

摘要

The invention provides compounds of general formula (I) or a physiologically acceptable salt, solvate or metabolically labile ester thereof wherein: R1 représents a hydrogen atom or a halogen atom or a group selected from C¿1-6?alkyl, C2-6alkenyl, fluoroC1-6alkyl, C1-6alkoxy, -CHO, -CO2H or -COR?2¿; Ar represents the group (II), R2 represents a group selected from C¿1-6?alkyl, C2-6alkenyl, C1-6alkoxy or the group -NR?12R13; R3¿ represents a group selected from -CO¿2?H, -NHSO2CF3 or a C-linked tetrazolyl group; R?4 and R5¿ which may be the same or different each independently represent a hydrogen atom or a halogen atom or a C¿1-6?alkyl group; Het represents the group (III), R?6¿ represents a hydrogen atom or a group selected from C¿1-6?alkyl, C2-6alkenyl, C1-6alkylthio, C1-6alkoxy, C3-7cycloalkyl or C3-7cycloalkylC1-4alkyl; R?7¿ represents a hydrogen atom or a halogen atom or a group selected from C¿1-6?alkyl, C2-6alkenyl or fluoroC1-6alkyl; R?8¿ represents a hydrogen atom or a C¿1-6?alkyl group; R?9¿ represents a hydrogen atom or a group selected from phenyl or C¿1-6?alkyl, optionally substituted by a phenyl, hydroxyphenyl, hydroxyl, amino, guanidino, imidazolyl, indolyl, mercapto, C1-6alkylthio, carboxyl or amido group; or R?8 and R9¿, when taken together, form an alkylene bridge of 2, 3 or 4 carbon atoms; R10 represents a hydrogen atom or a C¿1-6?alkyl group; R?11¿ represents a group selected from hydroxyl, C¿1-6?alkoxy, C2-6alkenoxy or -NR?12R13; R12 and R13¿, which may be the same of different, each independently represent a hydrogen atom or a C¿1-4?alkyl group or -NR?12R13¿ forms a saturated heterocyclic ring which has 5 or 6 ring members and may optionally contain in the ring one oxygen atom; m represents zero or an integer from 1 to 4; and n represents zero or an integer from 1 to 3; with the proviso that when n represents an integer from 1 to 3, R?9 and R10¿ both represent hydrogen atoms. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.