Succinic acid compounds
    1.
    发明公开
    Succinic acid compounds 失效
    Bernsteinsäurederivaten。

    公开(公告)号:EP0507534A1

    公开(公告)日:1992-10-07

    申请号:EP92302786.6

    申请日:1992-03-30

    摘要: Succinic acid compounds of the formula:

    wherein A represents a heterocyclic group, a 3 to 8-membered cycloalkyl group or a phenyl group which may have one or more substituents selected from the group of a halogen atom, a lower alkyl group having 1 to 6 carbon atoms and a lower alkoxy group having 1 to 6 carbon atoms; B represents a bicyclic amino group which may have 1 or 2 unsaturated bonds, with the proviso that B bonds to the carbon atom of the carbonyl group at the nitrogen atom; R represents a hydrogen atom or combines each other to form a chemical bond; R 1 represents a hydrogen atom, a lower alkyl group having 1 to 6 carbon atoms or an aralkyl group having 7 to 10 carbon atoms; when there is an asymmetric carbon atom, enantiomers thereof and racemic mixtures thereof; when there are geometrical isomers, each geometrical isomer, E-isomers thereof, Z-isomers thereof, cis-isomers thereof and trans-isomers thereof; and pharmaceutically acceptable salts thereof, enhance insulin secretion and possess a hypoglycemic activity, and are thus useful for the treatment of diabetes.

    摘要翻译: 具有下式的琥珀酸化合物:其中A表示杂环基,3至8元环烷基或苯基,其可以具有一个或多个选自以下的取代基:卤素原子,具有 1至6个碳原子和1至6个碳原子的低级烷氧基; B表示可以具有1或2个不饱和键的双环氨基,条件是B与氮原子上的羰基的碳原子键合; R表示氢原子或彼此结合形成化学键; R 1表示氢原子,碳原子数1〜6的低级烷基或碳原子数7〜10的芳烷基。 当存在不对称碳原子时,其对映异构体和其外消旋混合物; 当存在几何异构体时,每种几何异构体,其异构体,其Z-异构体,其顺式异构体和其反式异构体; 和其药学上可接受的盐,增强胰岛素分泌并具有降血糖活性,因此可用于治疗糖尿病。

    Histidine derivatives as renin inhibitors
    8.
    发明公开
    Histidine derivatives as renin inhibitors 失效
    Histidinderivate ALS Renininhibitoren。

    公开(公告)号:EP0181110A2

    公开(公告)日:1986-05-14

    申请号:EP85307555.4

    申请日:1985-10-18

    摘要: @ Dipeptides are described which are represented by the formula

    wherein His represents an L-histidyl group, Ar, represents a phenyl group, a naphthyl group or an indolyl group, Ar 2 represents a phenyl group or a naphthyl group, X represents a chemical bond, -NHCO-, -CONH-, -CO-, -CH 2 -, -NH-, -O- or -(CH=CH) P -wherein p is 1 or 2, Z represents an oxygen atom or
    in which R 2 represents a hydrogen atom or combines with R, to form a chemical bond, m and n, which may be the same or different, each represents an integer of from 0 to 3, provided that when X is a chemical bond, the sum of n plus m is from 1 to 6 and when X is not a chemical bond, the sum of n plus m is from 1 to 4, Y represents a chemical bond when X is not a chemical bond, or, when X is a chemical bond, an alkylene group having 1 to 3 carbon atoms, R 1 represents a hydrogen atom or combines with R 2 to form a chemical bond, R 3 represents a formyl group or a hydroxymethyl group, R 4 represents an isobutyl group or a benzyl group, and C represents an L-configurational carbon atom; or the pharmaceutically acceptable salt thereof.
    These compounds have a strong inhibitory effect on human renin, and are useful as a therapeutically active agent for the treatment of hypertension, especially renin - associated hypertension.

    Histidine derivatives as renin inhibitors
    10.
    发明公开
    Histidine derivatives as renin inhibitors 失效
    作为RENIN抑制剂的HISTIDINE DERIVATIVES

    公开(公告)号:EP0181110A3

    公开(公告)日:1988-05-11

    申请号:EP85307555

    申请日:1985-10-18

    摘要: @ Dipeptides are described which are represented by the formula

    wherein His represents an L-histidyl group, Ar, represents a phenyl group, a naphthyl group or an indolyl group, Ar 2 represents a phenyl group or a naphthyl group, X represents a chemical bond, -NHCO-, -CONH-, -CO-, -CH 2 -, -NH-, -O- or -(CH=CH) P -wherein p is 1 or 2, Z represents an oxygen atom or
    in which R 2 represents a hydrogen atom or combines with R, to form a chemical bond, m and n, which may be the same or different, each represents an integer of from 0 to 3, provided that when X is a chemical bond, the sum of n plus m is from 1 to 6 and when X is not a chemical bond, the sum of n plus m is from 1 to 4, Y represents a chemical bond when X is not a chemical bond, or, when X is a chemical bond, an alkylene group having 1 to 3 carbon atoms, R 1 represents a hydrogen atom or combines with R 2 to form a chemical bond, R 3 represents a formyl group or a hydroxymethyl group, R 4 represents an isobutyl group or a benzyl group, and C represents an L-configurational carbon atom; or the pharmaceutically acceptable salt thereof. These compounds have a strong inhibitory effect on human renin, and are useful as a therapeutically active agent for the treatment of hypertension, especially renin - associated hypertension.