1-(substituted phenyl)-4-biphenylmethyl-imidazol-2-one derivatives, their preparation and their use as angiotensin II antagonists
申请人:G.D. SEARLE & CO.
公开号:EP0978515A2
公开(公告)日:2000-02-09
A class of 1-phenyl imidazol-2-one biphenylmethyl compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula
wherein each of R1, R2 and R3 is independently selected from hydrogen, alkyl, alkoxy, cyano, halo, hydroxy, nitro, amino, alkylamino,carboxyl, alkoxycarbonyl, formyl, alkylcarbonyl and haloalkylcarbonyl; with the proviso that at least one of R1, R2 and R3 must be a substituent other than hydrogen, and with the further proviso that when each of R1 and R3 is hydrogen, then R2 cannot be chloro; wherein R4 is selected from hydrogen, alkyl, halo, haloalkyl, formyl, carboxyl and alkoxyalkyl; wherein R5 is selected from alkyl, phenyl, phenylalkyl, cycloalkyl and cycloalkylalkyl; and wherein R6 is an acidic group selected from COOH and
or a stereoisomer or a tautomer thereof or a pharmaceutically-acceptable salt thereof.
These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
描述了一类用于治疗循环系统疾病的 1-苯基咪唑-2-酮联苯甲基化合物。特别感兴趣的化合物是式中的血管紧张素 II 拮抗剂
其中 R1、R2 和 R3 各自独立地选自氢、烷基、烷氧基、氰基、卤代、羟基、硝基、氨基、烷基氨基、羧基、烷氧羰基、甲酰基、烷基羰基和卤代烷基羰基;但 R1、R2 和 R3 中至少有一个必须是除氢以外的取代基,而且当 R1 和 R3 都是氢时,R2 不能是氯;其中 R4 选自氢、烷基、卤代、卤代烷基、甲酰基、羧基和烷氧基烷基; 其中 R5 选自烷基、苯基、苯基烷基、环烷基和环烷基烷基;以及其中 R6 是选自 COOH 和
或其立体异构体或同系物或其药学上可接受的盐。
这些化合物尤其适用于治疗或控制高血压和充血性心力衰竭。