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    Derivatives of 1H-isoindol-3-amine, 1H-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as Beta-secretase Inhibitors
    4.
    发明申请
    Derivatives of 1H-isoindol-3-amine, 1H-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as Beta-secretase Inhibitors 有权
    1H-异吲哚-3-胺的衍生物，1H-异氮杂 - 吲哚-3-胺，3,4-二氢异喹啉-1-胺和1,4-二氢异喹啉-3-胺作为β-分泌酶抑制剂

    公开(公告)号：US20130172343A1

    公开(公告)日：2013-07-04

    申请号：US13814232

    申请日：2011-08-04

    申请人： Ana Elena Minatti ,  Yuan Cheng ,  Wenge Zhong

    发明人： Ana Elena Minatti ,  Yuan Cheng ,  Wenge Zhong

    IPC分类号： C07D491/20 ,  C07D498/20 ,  C07D498/22 ,  C07D491/22

    CPC分类号： C07D491/20 ,  A61K31/436 ,  A61K31/437 ,  A61K31/537 ,  C07D491/22 ,  C07D498/20 ,  C07D498/22

    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: (I). In another embodiment, the compounds have a general Formula II: (II). In another embodiment, the compounds have a general Formula III: (III). Variables A1, A2, A3, A4, A5, A6, R2, R7, V, W, X, Y and Z of Formulas I, II and III 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 Formulas I, II and III, intermediates and processes useful for the preparation of compounds of Formulas I, II and III.

    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：（I）。 在另一个实施方案中，化合物具有通式II：（II）。 在另一个实施方案中，化合物具有通式III：（III）。 式I，II和III的变量A1，A2，A3，A4，A5，A6，R2，R7，V，W，X，Y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，II和III的其它实施方案，可用于制备式I，II和III化合物的中间体和方法。

    Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
    5.
    发明授权
    Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use 有权
    螺 - 氨基 - 咪唑啉酮和螺 - 氨基 - 二氢 - 嘧啶酮化合物作为β-分泌酶调节剂和使用方法

    公开(公告)号：US08957083B2

    公开(公告)日：2015-02-17

    申请号：US13988745

    申请日：2011-11-18

    申请人： Ana Elena Minatti ,  Oleg Epstein ,  Ryan White ,  Matthew Weiss ,  Wenge Zhong ,  Jonathan D. Low

    发明人： Ana Elena Minatti ,  Oleg Epstein ,  Ryan White ,  Matthew Weiss ,  Wenge Zhong ,  Jonathan D. Low

    IPC分类号： C07D491/107 ,  C07D491/20

    CPC分类号： C07D491/107 ,  C07D491/20

    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 A1, A3, A4, A5, A6, A8, L, R2, R7, R9, W and Y of Formula I 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 plaque formation and deposition, resulting from the 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 Formulas II and III, sub-Formula embodiments of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulae I-III.

    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A1，A3，A4，A5，A6，A8，L，R2，R7，R9，W和Y在本文中定义。 本发明还提供包含该化合物的药物组合物，以及用于治疗由于BACE的活性而导致的斑块形成和沉积相关疾病和/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和III的化合物，式I，II和III的次级实施方案，可用于制备式I-III化合物的中间体和方法和方法。

    Spiro-Amino-Imidazolone and Spiro-Amino-Dihydro-Pyrimidinone Compounds as Beta-Secretase Modulators and Methods of Use
    6.
    发明申请
    Spiro-Amino-Imidazolone and Spiro-Amino-Dihydro-Pyrimidinone Compounds as Beta-Secretase Modulators and Methods of Use 有权
    螺氨基 - 咪唑啉酮和螺 - 氨基 - 二氢 - 嘧啶酮化合物作为β-分泌酶调节剂和使用方法

    公开(公告)号：US20130338177A1

    公开(公告)日：2013-12-19

    申请号：US13988745

    申请日：2011-11-18

    申请人： Ana Elena Minatti ,  Oleg Epstein ,  Ryan White ,  Matthew Weiss ,  Wenge Zhong ,  Jonathan D. Low

    发明人： Ana Elena Minatti ,  Oleg Epstein ,  Ryan White ,  Matthew Weiss ,  Wenge Zhong ,  Jonathan D. Low

    IPC分类号： C07D491/107 ,  C07D491/20

    CPC分类号： C07D491/107 ,  C07D491/20

    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 A1, A3, A4, A5, A6, A8, L, R2, R7, R9, W and Y of Formula (I) 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 plaque formation and deposition, resulting from the 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 Formulas (II) and (III), sub-Formula embodiments of Formulas (I), (II) and (III), intermediates and processes and methods useful for the preparation of compounds of Formulae (I-III).

    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A1，A3，A4，A5，A6，A8，L，R2，R7，R9，W和Y如本文所定义。 本发明还提供包含该化合物的药物组合物，以及用于治疗由于BACE的活性而导致的斑块形成和沉积相关疾病和/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）和（III）的化合物，式（I），（II）和（III）的分式实施方案，可用于制备式（I-III）化合物的中间体和方法和方法 ）。