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11 条记录 (耗时 0.035 秒)

    Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
    2.
    发明授权
    Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use 有权
    氨基 - 恶嗪和氨基 - 二氢噻嗪化合物作为β-分泌酶调节剂和使用方法

    公开(公告)号：US09296759B2

    公开(公告)日：2016-03-29

    申请号：US14346252

    申请日：2012-09-21

    申请人： AMGEN INC.

    发明人： Ryan White ,  Yuan Cheng ,  Ana Elena Minatti ,  Bryant Yang ,  Xiao Mei Zheng ,  Patricia Lopez ,  Jason B. Human ,  Oleg Epstein ,  Ted Judd ,  Kelvin Sham ,  Qiufen Xue

    IPC分类号： C07D498/20 ,  C07D513/20 ,  A61K31/537 ,  A61K31/547 ,  C07D513/10 ,  C07D498/10

    CPC分类号： C07D498/10 ,  C07D498/20 ,  C07D513/10 ,  C07D513/20

    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 A1, A2, A3, A4, A5, A6, L, R2, R7, X, Y and Z of Formula I 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, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.

    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，其中式I中的A1，A2，A3，A4，A5，A6，L，R2，R7，X，Y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。 这种病症包括例如阿尔茨海默氏病，认知缺陷，认知障碍，精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。 本发明还包括式I的其它实施方案，可用于制备式I化合物的中间体和方法。

    Amino-Oxazine and Amino-Dihydrothiazine Compounds as Beta-Secretase Modulators and Methods of Use
    7.
    发明申请
    Amino-Oxazine and Amino-Dihydrothiazine Compounds as Beta-Secretase Modulators and Methods of Use 有权
    氨基 - 恶嗪和氨基 - 二氢噻嗪化合物作为β-分泌酶调节剂和使用方法

    公开(公告)号：US20140296226A1

    公开(公告)日：2014-10-02

    申请号：US14346252

    申请日：2012-09-21

    申请人： AMGEN INC

    发明人： Ryan White ,  Yuan Cheng ,  Ana Elena Minatti ,  Bryant Yang ,  Xiao Mei Zheng ,  Patricia Lopez ,  Jason B. Human ,  Oleg Epstein ,  Ted Judd ,  Kelvin Sham ,  Qiufen Xue

    IPC分类号： C07D513/10 ,  C07D498/20 ,  C07D513/20 ,  C07D498/10

    CPC分类号： C07D498/10 ,  C07D498/20 ,  C07D513/10 ,  C07D513/20

    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 A1, A2, A3, A4, A5, A6, L, R2, R7, X, Y and Z of Formula I 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, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.

    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，其中式I中的A1，A2，A3，A4，A5，A6，L，R2，R7，X，Y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。 这种病症包括例如阿尔茨海默氏病，认知缺陷，认知障碍，精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。 本发明还包括式I的其它实施方案，可用于制备式I化合物的中间体和方法。

    Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta-secretase and methods of use thereof
    10.
    发明授权
    Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta-secretase and methods of use thereof 有权
    作为β-分泌酶抑制剂的桥连双环氨基噻嗪二氧化物化合物及其使用方法

    公开(公告)号：US09096615B2

    公开(公告)日：2015-08-04

    申请号：US14445498

    申请日：2014-07-29

    申请人： AMGEN INC.

    发明人： Richard T. Lewis ,  Jennifer R. Allen ,  James Brown ,  Angel Guzman-Perez ,  Zihao Hua ,  Ted Judd ,  Qingyian Liu ,  Philip R. Olivieri ,  Karina Romero ,  Laurie Schenkel ,  John Stellwagen ,  Ryan White

    IPC分类号： C07D513/06 ,  C07D513/08 ,  C07D519/00

    CPC分类号： C07D513/08 ,  C07D513/06 ,  C07D519/00

    摘要： The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.

    摘要翻译： 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 化合物具有通式I：其中式I的变量A4，A5，A6，A8，R1，R2，R3，R7和n独立地在本文中定义。 本发明还提供包含该化合物的药物组合物，以及用于治疗由BACE的生物学活性产生的A-β斑块形成和沉积相关的病症和/或病症的化合物和组合物的相应用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明还提供式II化合物及其次级实施方案，式III化合物，可用于制备式I-III化合物的中间体和方法和方法及其分式。