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15 条记录 (耗时 0.021 秒)

    POLYCYCLIC GUANINE DERIVATIVES
    3.
    发明授权
    POLYCYCLIC GUANINE DERIVATIVES 失效
    多环芳烃GUANINDERIVATE

    公开(公告)号：EP0538332B1

    公开(公告)日：1997-07-23

    申请号：EP91912779.5

    申请日：1991-06-20

    申请人： SCHERING CORPORATION

    发明人： NEUSTADT, Bernard, R. ,  LINDO, Neil, A. ,  MCKITTRICK, Brian, A.

    IPC分类号： C07D487/14

    CPC分类号： C07D487/14

    摘要： Novel polycyclic guanine derivatives of formula (I) and (I'), wherein J is oxygen or sulfur, R1 is hydrogen, alkyl or alkyl substituted with aryl or hydroxy; R2 is hydrogen, aryl, heteroaryl, cycloalkyl, alkyl or alkyl substituted with aryl, heteroaryl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino, or -(CH¿2?)mTCOR?20¿ wherein m is an integer from 1 to 6, T is oxygen or -NH- and R20 is hydrogen, aryl, heteroaryl, alkyl or alkyl substituted with aryl or heteroaryl; R3 is hydrogen, halo, trifluoromethyl, alkoxy, alkylthio, alkyl, cycloalkyl, aryl, aminosulfonyl, amino, monoalkylamino, dialkylamino, hydroxyalkylamino, aminoalkylamino, carboxy, alkoxycarbonyl or aminocarbonyl or alkyl substituted with aryl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino; R?a, Rb, Rc and Rd¿ independently represent hydrogen, alkyl, cycloalkyl or aryl; or (R?a and Rb) or (Rc and Rd) or (Rb and Rc¿) can complete a saturated ring of 5- to 7- carbon atoms, or (R?a and Rb¿) taken together and (R?b and Rc¿) taken together, each complete a saturated ring of 5- to 7- carbon atoms, wherein each ring optionally can contain a sulfur or oxygen atom and whose carbon atoms may be optionally substituted with one or more of the following: alkenyl, alkynyl, hydroxy, carboxy, alkoxycarbonyl, alkyl or alkyl substituted with hydroxy, carboxy or alkoxycarbonyl; or such saturated ring can have two adjacent carbon atoms which are shared with an adjoining aryl ring; and n is zero or one. The compounds of formulas (I) and (I') are useful as antihypertensive, muscle relaxant and bronchodilating agents.

    PHOSPHINIC ACID DERIVATIVES
    8.
    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.

    MUSCARINIC ANTAGONISTS
    10.
    发明授权
    MUSCARINIC ANTAGONISTS 有权
    毒蕈碱受体拮抗剂

    公开(公告)号：EP1343760B1

    公开(公告)日：2009-08-12

    申请号：EP01985584.0

    申请日：2001-12-17

    申请人： Schering Corporation

    发明人： MCKITTRICK, Brian, A. ,  GUO, Guihua ,  ZHU, Zhaoning ,  YE, Yuanzan

    IPC分类号： C07D211/34 ,  C07D405/04 ,  A61K31/445 ,  A61K31/453 ,  A61P25/28

    CPC分类号： C07D451/04 ,  C07D211/34 ,  C07D405/04

    摘要： Amide derivatives of 1,4 di-substituted piperidine compounds of the formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof, wherein R1 is optionally substituted cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or heteroaryl; R2 is H, alkyl, or optionally substituted cycloalkyl, cycloalkylalkyl, heterocycloalkyl, bridged cycloalkyl, or bridged heterocycloalkyl; R3 is alkyl or -CH¿2?OH; and R4 is H or alkyl; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed.