ASPARTYL PROTEASE INHIBITORS
    4.
    发明公开
    ASPARTYL PROTEASE INHIBITORS 审中-公开
    ASPARTYL蛋白酶抑制剂

    公开(公告)号:EP1891021A1

    公开(公告)日:2008-02-27

    申请号:EP06772934.3

    申请日:2006-06-12

    摘要: Disclosed are certain substituted spiro iminopyrimidinones and other compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein U, W, A, R, R1, R2, R6a and R7, are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of using such compounds and compositions to inhibit aspartyl protease, and to treat a variety of disease and indications including (but not limited) to cardiovascular disease and cognitive and neurodegenerative disease. The compounds of the present invention are disclosed for use alone or in combination with one or more additional active ingredients such as cholinesterase inhibitors and a muscarinic m1 agonist and/or m2 antagonists.

    摘要翻译: 本文公开了式I化合物或其立体异构体,互变异构体或药学上可接受的盐或溶剂合物,其中U,W,A,R,R1,R2,R6a和R7如说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法,特别是治疗心血管疾病,认知和神经退行性疾病的方法。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m2拮抗剂组合治疗认知或神经退行性疾病的方法。

    ASPARTYL PROTEASE INHIBITORS
    5.
    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

    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
    8.
    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

    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.