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    Substituted pyrano [2,3-b] pyridinamine compounds as beta-secretase modulators and methods of use
    8.
    发明授权
    Substituted pyrano [2,3-b] pyridinamine compounds as beta-secretase modulators and methods of use 有权
    取代的吡喃并[2,3-b]吡啶胺化合物作为β-分泌酶调节剂和使用方法

    公开(公告)号：US07803809B2

    公开(公告)日：2010-09-28

    申请号：US12291753

    申请日：2008-11-12

    申请人： Russell Graceffa ,  Matthew Kaller ,  Daniel La ,  Patricia Lopez ,  Vinod F. Patel ,  Wenge Zhong

    发明人： Russell Graceffa ,  Matthew Kaller ,  Daniel La ,  Patricia Lopez ,  Vinod F. Patel ,  Wenge Zhong

    IPC分类号： A61K31/44

    CPC分类号： C07D487/04 ,  C07D311/96 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/052 ,  C07D519/00

    摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.

    摘要翻译： 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式I，其中R 1，R 2，R 3，R 4，R 5，A 1，A 2，A 3，A 4，X和Z在本文中定义。 本发明还包括在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的病症和病症的用途。 这些疾病包括例如阿尔茨海默病（AD），认知缺陷和损伤，精神分裂症和其他类似的中枢神经系统疾病。 本发明还包括式II的其它实施方案，可用于制备式I和II化合物的中间体和方法。

    Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
    10.
    发明授权
    Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use 有权
    取代的羟乙基胺化合物作为β-分泌酶调节剂和使用方法

    公开(公告)号：US08633315B2

    公开(公告)日：2014-01-21

    申请号：US13427802

    申请日：2012-03-22

    申请人： Wenge Zhong ,  Stephen Hitchcock ,  Patel F. Vinod ,  Michael Croghan ,  Bryant Yang

    发明人： Wenge Zhong ,  Stephen Hitchcock ,  Patel F. Vinod ,  Michael Croghan ,  Bryant Yang

    IPC分类号： C07D491/107 ,  C07D311/96 ,  C07D471/10

    CPC分类号： C07D491/107 ,  C07D221/06 ,  C07D311/96 ,  C07D471/10 ,  C07D491/10 ,  C07D493/10 ,  C07D495/10

    摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1a, R1b, R1c, B, W, R3, R4 and R5 are defined herein. In another embodiment, the invention provides compounds of general Formula II wherein A1, A2, A3, A4, R1a, R1b, R1c, R2, R4, R5, W, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.

    摘要翻译： 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式I，其中R 1a，R 1b，R 1c，B，W，R 3，R 4和R 5在本文中定义。 在另一个实施方案中，本发明提供通式II的化合物，其中A1，A2，A3，A4，R1a，R1b，R1c，R2，R4，R5，W，X和Z如本文所定义。 本发明还包括在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的病症和病症的用途。 这些疾病包括例如阿尔茨海默病（AD），认知缺陷和损伤，精神分裂症和其他类似的中枢神经系统疾病。 本发明还包括式II的其它实施方案，可用于制备式I和II化合物的中间体和方法。