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    ASPARTYL PROTEASE INHIBITORS
    2.
    发明授权
    ASPARTYL PROTEASE INHIBITORS 有权
    天冬氨酰蛋白酶抑制剂

    公开(公告)号：EP1896477B1

    公开(公告)日：2010-09-22

    申请号：EP06784753.3

    申请日：2006-06-12

    申请人： Schering Corporation

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

    IPC分类号： C07D487/04 ,  C07D498/04 ,  A61P9/00 ,  A61P25/00 ,  A61P25/28 ,  A61P31/18 ,  A61K31/395

    CPC分类号： C07D487/04

    摘要： Disclosed are compounds of the formula (I) Chemical formula should be inserted here as it appears on the abstract in paper form or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein U, W, R, 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. 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 m1 agonist or m2 antagonist.

    ASPARTYL PROTEASE INHIBITORS
    4.
    发明公开
    ASPARTYL PROTEASE INHIBITORS 审中-公开
    天冬氨酰蛋白酶抑制剂

    公开(公告)号：EP1943246A1

    公开(公告)日：2008-07-16

    申请号：EP06826991.9

    申请日：2006-10-30

    申请人： Schering Corporation

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

    IPC分类号： C07D411/04 ,  A61K31/553

    CPC分类号： C07D413/04 ,  C07F9/65848

    摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein (W, R1, R2, R3, R4, R5, R6, 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.

    THIOPHENYL-SUBSTITUTED 2-IMINO-3-METHYL PYRROLO PYRIMIDINONE COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE
    7.
    发明公开
    THIOPHENYL-SUBSTITUTED 2-IMINO-3-METHYL PYRROLO PYRIMIDINONE COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE 有权
    噻吩基取代的2-亚氨基-3-甲基吡咯并嘧啶酮化合物作为BACE-1抑制剂，组合物及其应用

    公开(公告)号：EP2283016A1

    公开(公告)日：2011-02-16

    申请号：EP09734309.9

    申请日：2009-04-21

    申请人： Schering Corporation

    发明人： STAMFORD, Andrew, W. ,  ZHU, Zhaoning ,  MANDAL, Mihirbaran ,  LIU, Xiaoxiang

    IPC分类号： C07D487/04 ,  A61P25/28 ,  A61K31/519

    CPC分类号： C07D487/04

    摘要： In its many embodiments, the present invention provides provides certain thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidone compounds, including compounds (or tautomers or a pharmaceutically acceptable salts thereof) having the structural Formula (III): wherein R
    2 , R
    3 , R
    4 , R
    5 , R
    6 , R
    7 , R
    8 , and R
    9 are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimer's Disease, are also disclosed.

    摘要翻译： 在其许多实施方案中，本发明提供了某些噻吩基取代的2-亚氨基-3-甲基吡咯并嘧啶酮化合物，包括具有结构式（III）的化合物（或其互变异构体或药学上可接受的盐）：其中R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9各自独立地选择和如本文所定义。 还公开了包含一种或多种这样的化合物的药物组合物，以及它们的制备方法和用于治疗与淀粉样蛋白β（Aβ）蛋白相关的病状，包括阿尔茨海默氏病的方法。