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40 条记录 (耗时 0.019 秒)

    PHOSPHINIC ACID DERIVATIVES
    12.
    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.

    SUBSTITUTED AMIDE BETA SECRETASE INHIBITORS
    18.
    发明授权
    SUBSTITUTED AMIDE BETA SECRETASE INHIBITORS 有权
    取代酰胺作为抑制剂β-分泌

    公开(公告)号：EP1781625B1

    公开(公告)日：2010-12-15

    申请号：EP05773473.3

    申请日：2005-07-20

    申请人： Schering Corporation

    发明人： HUANG, Ying ,  LI, Guoqing ,  STAMFORD, Andrew, W.

    IPC分类号： C07D241/08 ,  A61K31/495

    CPC分类号： C07D401/12 ,  C07D241/04 ,  C07D241/08 ,  C07D401/10 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    摘要： Disclosed are novel compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula (I). Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula (I) and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula (I), HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.