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    FUSED MULTI-CYCLIC SULFONE COMPOUNDS AS INHIBITORS OF BETA-SECRETASE AND METHODS OF USE THEREOF
    3.
    发明申请
    FUSED MULTI-CYCLIC SULFONE COMPOUNDS AS INHIBITORS OF BETA-SECRETASE AND METHODS OF USE THEREOF 有权
    作为β-分泌酶的抑制剂的熔融多循环磺化合物及其使用方法

    公开(公告)号：US20140213581A1

    公开(公告)日：2014-07-31

    申请号：US14166012

    申请日：2014-01-28

    Applicant: AMGEN INC.

    Inventor： Ryan WHITE ,  Jennifer R. ALLEN ,  Oleg EPSTEIN ,  Fang-Tsao HONG ,  Zihao HUA ,  Jason Brooks HUMAN ,  Patricia LOPEZ ,  Philip R. OLIVIERI ,  Karina ROMERO ,  Laurie SCHENKEL ,  John STELLWAGEN ,  Nuria A. TAMAYO ,  Xiao Mei ZHENG

    IPC: C07D513/04 ,  C07D513/14

    CPC classification number: C07D513/04 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/10 ,  C07D513/14 ,  C07D513/20 ,  C07D519/00

    Abstract: 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 A5, A6, A8, R1, R2, R3, R7, X, Y, n and o 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.

    Abstract translation: 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A5，A6，A8，R1，R2，R3，R7，X，Y，n和o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。 本发明进一步提供式II化合物及其次式实施方案，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。

    BRIDGED BICYCLIC AMINO THIAZINE DIOXIDE COMPOUNDS AS INHIBITORS OF BETA-SECRETASE AND METHODS OF USE THEREOF
    5.
    发明申请
    BRIDGED BICYCLIC AMINO THIAZINE DIOXIDE COMPOUNDS AS INHIBITORS OF BETA-SECRETASE AND METHODS OF USE THEREOF 有权
    作为β-分泌酶的抑制剂的桥联双氨基二氧化二氮化合物及其使用方法

    公开(公告)号：US20150038497A1

    公开(公告)日：2015-02-05

    申请号：US14445498

    申请日：2014-07-29

    Applicant: AMGEN INC.

    Inventor： 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: C07D513/06

    CPC classification number: C07D513/08 ,  C07D513/06 ,  C07D519/00

    Abstract: 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.

    Abstract translation: 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。

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