Biphenylmethane derivatives, the use of them and pharmacological compositions containing same
申请人:Eisai Co., Ltd.
公开号:EP0628557A1
公开(公告)日:1994-12-14
Disclosed are biphenylmethane derivatives having the formula:
wherein
R² and R³, which may be the same or different, are each a hydrogen atom, a halogen atom, a lower C₁₋₆ alkyl group a lower C₁₋₆ alkoxy group, a carbamoyl group or a cyano group;
R⁴ stands for hydrogen or a lower C₁₋₆ alkyl group;
R⁵ is 1H-tetrazol-5-yl, a carboxyl (-COOH) group or a carboxylic ester thereof;
R⁶ stands for hydrogen, a halogen atom, a hydroxy group or a lower C₁₋₆ alkoxy group, or a pharmacologically acceptable salt thereof,
wherein
compounds having the following formula and their pharmacologically acceptable salts are excluded:
wherein R⁵ is 1H-tetrazol-5-yl, a carboxyl (-COOH) group or a carboxylic ester thereof and n is an integer of 1 to 2;
or a pharmacologically acceptable salt thereof.
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.
所公开的是具有以下式子的联苯甲烷衍生物:
其中
R²和R³可以相同或不同,各自为氢原子、卤素原子、低级C₁₋₆烷基、低级C₁₋₆烷氧基、氨基甲酰基或氰基;
R⁴ 代表氢或低级 C₁₋₆ 烷基;
R⁵ 是 1H-四唑-5-基、羧基 (-COOH) 或其羧酸酯;
R⁶ 代表氢、卤素原子、羟基或低 C₁₋₆ 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学上可接受的盐除外:
其中 R⁵ 是 1H-四唑-5-基、羧基(-COOH)或其羧酸酯,n 是 1 至 2 的整数;
或其药理学上可接受的盐。
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制备这种组合物用于预防和治疗高血压和/或心力衰竭的用途。