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    AMINO-OXAZINES AND AMINO-DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
    1.
    发明申请
    AMINO-OXAZINES AND AMINO-DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 有权
    氨基氧化合物和氨基二氢化合物作为β-分泌酶调节剂和使用方法

    公开(公告)号：US20140045828A1

    公开(公告)日：2014-02-13

    申请号：US13929483

    申请日：2013-06-27

    申请人： AMGEN INC.

    发明人： Jian CHEN ,  Wenge ZHONG ,  Bryant YANG ,  Wenyuan QIAN ,  Patricia LOPEZ ,  Ryan WHITE ,  Matthew WEISS ,  Tedd JUDD ,  Timothy POWERS ,  Yuan CHENG ,  Thomas DINEEN ,  Oleg EPSTEIN ,  Jason HUMAN ,  Jonathan D. LOW ,  Isaac E. MARX ,  Ana Elena MINATTI ,  Michele POTASHMAN ,  Nick A. PARAS ,  Qingyian LIU

    IPC分类号： C07D513/10 ,  C07D498/20

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

    OXAZINE DERIVATIVES AS BETA-SECRETASE INHIBITORS AND METHODS OF USE
    2.
    发明申请
    OXAZINE DERIVATIVES AS BETA-SECRETASE INHIBITORS AND METHODS OF USE 审中-公开

    公开(公告)号：US20200207747A1

    公开(公告)日：2020-07-02

    申请号：US16466211

    申请日：2017-12-13

    申请人： AMGEN INC.

    发明人： Jennifer R. ALLEN ,  Matthew P. BOURBEAU ,  Ning CHEN ,  Michael J. FROHN ,  Paul E. HARRINGTON ,  Qingyian LIU ,  Corey REEVES

    IPC分类号： C07D413/10 ,  C07D413/14 ,  A61P25/28

    摘要： The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: (insert Formula I structure) wherein variables W, X, Y, R2, R2′, R3, R4, R5, R6, and R7 of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to beta amyloid (Aβ) 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, and other central nervous system conditions.

    THIAZINE DERIVATIVES AS BETA-SECRETASE INHIBITORS AND METHODS OF USE
    9.
    发明申请
    THIAZINE DERIVATIVES AS BETA-SECRETASE INHIBITORS AND METHODS OF USE 审中-公开

    公开(公告)号：US20200062743A1

    公开(公告)日：2020-02-27

    申请号：US16466209

    申请日：2017-12-13

    申请人： AMGEN INC.

    发明人： Matthew P. BOURBEAU ,  Paul E. HARRINGTON ,  Qingyian LIU

    IPC分类号： C07D417/10 ,  A61P25/28

    摘要： The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: (see Formula I structure) wherein variables R1, R1′, R2, R2′, R3, R4, R5, R6, R7, and b of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ 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, and other central nervous system conditions.