Angiotensin converting enzyme inhibitors and their production and use as pharmaceuticals
    133.
    发明公开
    Angiotensin converting enzyme inhibitors and their production and use as pharmaceuticals 失效
    血管紧张素转换酶,它们的制备和用作药物的抑制剂。

    公开(公告)号:EP0183398A1

    公开(公告)日:1986-06-04

    申请号:EP85307931.7

    申请日:1985-11-01

    申请人: FISONS plc

    摘要: There are described compounds of formula I,

    in which Z is R 2 CH(COOH)NH-, R 1 SCH 2 - or Ph(CH 2 ) P PO(OH)-,

    Ph is phenyl,
    p is an integer from 1 to 6,
    R, is hydrogen or R B CO-,
    R 8 is alkyl C1 to 10 or phenyl,
    R is hydrogen or alkyl C1 to 10,
    R2 is alkyl C1 to 10 or phenylalkyl C7 to 12,
    R 4 andR 5 , which may be the same or different, are each hydrogen, phenyl, naphthyl; a 5 or 6 membered alicyclic or heterocyclic ring each of which is optionally fused to a benzene ring; cycloalkyl containing 3 to 7 carbon atoms; or alkyl C1 to 10 optionally substituted by phenyl, napthyl or a 5 or 6 membered heterocyclic ring which latter is optionally fused to a benzene ring,

    the phenyl, naphthyl or 5 or 6 membered alicyclic or heterocyclic ring (which latter two are optionally fused to a benzene ring (are all optionally substituted by one or more alkyl C1 to 10, alkoxy C1 to 10, halogen, phenylalkyl C7 to 12, phenylalkoxy C7 to 12, phenyl, hydroxy, =0, fluoroalkyl C1 to 10, cyano, nitro, phenylsulphonamido, dialkyl (C1 to 10) -amino-alkoxy (C1 to 10), alkylthio C1 to 10, or dialkyl (C1 to 10)-amino,
    or R 4 and R 5 together form a - (CH 2 ) 4 -, -(CH 2 ) 5 -,
    chain

    R 6 is hydrogen or alkyl C1 to 10,
    q is 2 or 3,
    n is 0 or 1,
    Y is hydroxy or -NHS0 2 R 9 , and
    R 9 is alkyl C1 to 10,

    and pharmaceutically acceptable salts, esters and amides thereof.
    There are also described methods for making the compounds, formulations containing them and their use, eg as antihypertensives.