Biphenylmethane derivatives, the use of them and pharmacological compositions containing same
    7.
    发明公开
    Biphenylmethane derivatives, the use of them and pharmacological compositions containing same 失效
    Biphenylmethanderivate,ihre Anwendung und sie enthaltende pharmacologische Zusammensetzungen。

    公开(公告)号:EP0628557A1

    公开(公告)日:1994-12-14

    申请号:EP94109556.4

    申请日:1990-09-27

    申请人: Eisai Co., Ltd.

    IPC分类号: C07D471/04 A61K31/44

    摘要: 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.

    摘要翻译: 公开了具有下式的联苯甲烷衍生物:其中R 2和R 3可以相同或不同,各自为氢原子,卤素原子,低级C 1-6烷基,低级C1 -6烷氧基,氨基甲酰基或氰基; R 4代表氢或低级C 1-6烷基; R 5是1H-四唑-5-基,羧基(-COOH)基或其羧酸酯; R 6代表氢,卤素原子,羟基或低级C 1-6烷氧基,或其药理学上可接受的盐,其中排除具有下式的化合物及其药理学上可接受的盐:其中R 5是1H-四唑-5-基,羧基(-COOH)基或其羧酸酯,n是1〜2的整数。 或其药理学上可接受的盐。 此外,公开了其制备方法,含有该组合物的药物组合物及其制备用于预防和治疗高血压和/或心力衰竭的组合物的用途。

    Biphenylmethane derivative, the use of it and pharmacological compositions containing same
    8.
    发明公开
    Biphenylmethane derivative, the use of it and pharmacological compositions containing same 失效
    二苯甲烷衍生物,它们的制备方法和含有药物组合物。

    公开(公告)号:EP0598702A1

    公开(公告)日:1994-05-25

    申请号:EP94101415.1

    申请日:1990-09-27

    申请人: Eisai Co., Ltd.

    摘要: Disclosed are biphenylmethane derivatives having the formula (I):

    wherein R 1 is hydrogen, alkyl, cycloalkyl, halogenated alkyl, -S-R7, -S0 2 -R7, -C=C-R 7 or -(CH 2 )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 = C H - N = CH-, -CH = C H -C H = N- or -CH = N -C H = N-, R 2 and R 3 are each hydrogen, halogen, lower alkyl, lower alkoxy, carbamoyl or cyano, R 4 is hydrogen or lower alkyl, R 5 is 1 H-tetrazol-5-yl, carboxyl (-COOH) or a carboxylic ester group and R 6 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 R 2 through R 6 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.

    摘要翻译: 本发明公开了具有式(I)联苯甲烷衍生物: worin - [R <1>是氢,烷基,环烷基,卤代烷基,-S-R 7 -SO 2 R 7,-C IDENTICAL C-R7或 - (CH 2) p-OR 7,R 7是氢,烷​​基,环烷基或卤代烷基,p是0或1,-A1 = A2-A3 = A4-是-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-,R <2>和R <3> 各自为氢,卤素,低级烷基,低级烷氧基,氨基甲酰基或氰基,R <4>是氢或低级烷基,R <5>是1H-四唑-5-基,羧基(-COOH)或羧酸酯基和 [R <6>是氢,卤素,羟基或低级烷氧基,或其药理学上可接受的盐,从而被排除具有下式及其药理学上可接受的盐的化合物: worinř<2>至R <6>基本上 如上所定义。 此外,其制备方法,药物组合物含有相同,他们为寻求预防和治疗高血压和/或心脏衰竭的组合物的制备中的游离缺失盘。