Biphenylmethane derivative, the use of it and pharmacological compositions containing same
申请人:Eisai Co., Ltd.
公开号:EP0598702A1
公开(公告)日:1994-05-25
Disclosed are biphenylmethane derivatives having the formula (I):
wherein R1 is hydrogen, alkyl, cycloalkyl, halogenated alkyl, -S-R7, -S02-R7, -C=C-R7 or -(CH2)p-OR7, R7 being hydrogen, alkyl, cycloalkyl or halogenated alkyl, p being zero or 1, -A1 =A2-A3 = A4- is -CH = CH-CH = CH- , -N = CH-CH = CH-, -CH = N-CH = CH-, -CH = CH-N = CH-, -CH = CH-CH = N- or -CH = N-CH = N-, R2 and R3 are each hydrogen, halogen, lower alkyl, lower alkoxy, carbamoyl or cyano, R4 is hydrogen or lower alkyl, R5 is 1 H-tetrazol-5-yl, carboxyl (-COOH) or a carboxylic ester group and R6 is hydrogen, halogen, hydroxyl or lower alkoxy, or a pharmacologically acceptable salt thereof,
whereby compounds having the following formula and their pharmacologically acceptable salts are excluded:
wherein R2 through R6 are essentially as defined above. Further, a process for their preparation, pharmaceutical compositions containing same and their use for the preparation of such compositions for preventing and treating hypertension and/or cardiac failure are disclosed.
所公开的是具有式 (I) 的
联苯甲烷衍
生物:
其中R1为氢、烷基、环烷基、卤代烷基、-S-R7、-S02-R7、-C=C-R7或-(
CH2)p-OR7,R7为氢、烷基、环烷基或卤代烷基,p为0或1,-A1 =A2-A3 = A4-为-CH = CH-CH = CH-、-N = CH-CH = CH-、-CH = N-CH = CH-、-CH = CH-N = CH-、-CH = CH-CH = N-或-CH = N-CH = N-、R2 和 R3 分别是氢、卤素、低级烷基、低级烷氧基、
氨基甲酰基或
氰基,R4 是氢或低级烷基,R5 是 1 H-
四唑-5-基、羧基(-COOH)或
羧酸酯基,R6 是氢、卤素、羟基或低级烷氧基,或其药理学上可接受的盐、
其中具有下式的化合物及其药理上可接受的盐除外:
其中 R2 至 R6 基本如上定义。此外,还公开了它们的制备工艺、含有它们的药物组合物以及它们在制备这种组合物中用于预防和治疗高血压和/或心力衰竭的用途。