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59 条记录 (耗时 0.03 秒)

    MUSCARINIC ANTAGONISTS
    18.
    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.

    THE PREPARATION AND USE OF COMPOUNDS AS ASPARTYL PROTEASE INHIBITORS
    19.
    发明公开
    THE PREPARATION AND USE OF COMPOUNDS AS ASPARTYL PROTEASE INHIBITORS 有权
    生产和化合物的用途，AS天冬氨酰蛋白酶抑制剂

    公开(公告)号：EP1896430A2

    公开(公告)日：2008-03-12

    申请号：EP06784809.3

    申请日：2006-06-12

    申请人： Schering Corporation

    发明人： MCKITTRICK, Brian ,  ZHU, Zhaoning ,  STAMFORD, Andrew ,  SMITH, Elizabeth, M.

    IPC分类号： C07D251/10 ,  A61K31/53 ,  A61P9/00

    CPC分类号： C07D251/72 ,  C07D239/70 ,  C07F9/6584

    摘要： Disclosed are compounds of the formula I (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein A is a bond, -C(O)-, or -C(R3’)(R4’)-; X is -N(R1)- or -C(R6)(R7)-; Y is -S(O)2-, -C(=O)-, -PO(OR9) or -C(R6’R7’)-; is a single or double bond and R, R1, R2, R3, R4, R3’, R4’, R5, R6, R6’, R7 and R7’ are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.

    THE PREPARATION AND USE OF COMPOUNDS AS PROTEASE INHIBITORS
    20.
    发明公开
    THE PREPARATION AND USE OF COMPOUNDS AS PROTEASE INHIBITORS 审中-公开
    生产和化合物的蛋白酶抑制剂的用途

    公开(公告)号：EP1896406A2

    公开(公告)日：2008-03-12

    申请号：EP06772948.3

    申请日：2006-06-12

    申请人： Schering Corporation

    发明人： MCKITTRICK, Brian ,  ZHU, Zhaoning ,  STAMFORD, Andrew

    IPC分类号： C07D205/06

    CPC分类号： C07D487/04 ,  C07D205/06

    摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein, X is -C(R3 R4)-; Y is -N(R5)-; Z is -C(=N-R5’)-; and R1, R2, R3, and R4 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.