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    PHOSPHINIC ACID DERIVATIVES
    2.
    发明公开
    PHOSPHINIC ACID DERIVATIVES 失效
    膦衍生物

    公开(公告)号：EP0767794A1

    公开(公告)日：1997-04-16

    申请号：EP95924573.0

    申请日：1995-06-19

    申请人： SCHERING CORPORATION

    发明人： MCKITTRICK, Brian, A. ,  CZARNIECKI, Michael, F. ,  CHACKALAMANNIL, Samuel ,  CHUNG, Shin ,  DEFREES, Shawn ,  STAMFORD, Andrew, W.

    IPC分类号： A61K31 ,  A61P1 ,  A61P3 ,  A61P9 ,  A61P11 ,  A61P13 ,  A61P15 ,  A61P35 ,  A61P43 ,  C07F9

    CPC分类号： C07F9/65583 ,  C07F9/303 ,  C07F9/5728

    摘要： Phosphinic acid derivatives of structural formula (I) or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene; R1, R2, R3 and R4 are H, alkyl, alkenyl, alkenylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, hydroxyalkyl, carboxyalkyl, thioalkyl, alkoxythioalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl-substituted alkyl or heterocycloalkyl; or R1 and R2 form a cycloalkyl ring of 3-8 members and R3 and R4 are as defined; or R3 and R4 form a cycloalkyl ring of 3-7 members and R1 and R2 are as defined; or R1 and R2 together, and R3 and R4 together, each form a cycloalkyl ring; R5 is -OR9 or -NHR9, wherein R9 is hydrogen or alkyl; n is 0 or 1; A1 is p-aminobenzoyl or p-aminobenzenesulfonyl, or A1 and R5 together form a radical of an α-aminoacyl derivative; and R6 is phenylmethoxycarbonyl, arylcarbonyl, heteroarylcarbonyl or -A2-R7, wherein A2 is a divalent α-iminoacyl radical, and R7 is a substituent on the α-imino atom selected from H, R8OCO-, R8SO2- and R8NHCO-, wherein R8 is aryl, arylmethyl or (C1-C8)alkyl; are disclosed for use as endothelin converting enzyme inhibitors; also disclosed are a genus of novel compounds wherein R?3 and R4¿ form a cycloalkyl ring, and pharmaceutical compositions comprising said novel compounds.