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    5-Amino-Oxazepine and 5-Amino-Thiazepane Compounds as Beta Secretase Antagonists and Methods of Use
    1.
    发明申请
    5-Amino-Oxazepine and 5-Amino-Thiazepane Compounds as Beta Secretase Antagonists and Methods of Use 有权
    5-氨基 - 氧氮杂和5-氨基 - 噻吖烷化合物作为β-分泌酶拮抗剂和使用方法

    公开(公告)号：US20140031340A1

    公开(公告)日：2014-01-30

    申请号：US13982222

    申请日：2012-02-06

    申请人： Thomas Dineen ,  Matthew Weiss ,  Vinod F. Patel ,  Xiao Mai Zheng ,  Ryan White

    发明人： Thomas Dineen ,  Matthew Weiss ,  Vinod F. Patel ,  Xiao Mai Zheng ,  Ryan White

    IPC分类号： C07D498/20 ,  C07D498/10

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

    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, R2, R7, X 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 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 Formulas (II) and sub-formula embodiments of Formula (I) and (II), intermediates and processes and methods useful for the preparation of compounds of Formulas (I)-(II).

    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。 该化合物具有通式（I）; 其中式（I）的变量A1，A3，A4，A5，A6，A8，R2，R7，X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（I）和（II）的式（II）和亚式实施方案的化合物，可用于制备式（I） - （II）化合物的中间体和方法和方法。

    5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use
    4.
    发明授权
    5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use 有权
    5-氨基 - 氧氮杂和5-氨基 - 噻嗯烷化合物作为β-分泌酶拮抗剂和使用方法

    公开(公告)号：US09346827B2

    公开(公告)日：2016-05-24

    申请号：US13982222

    申请日：2012-02-06

    申请人： Thomas Dineen ,  Matthew Weiss ,  Vinod F. Patel ,  Xiao Mei Zheng ,  Ryan White

    发明人： Thomas Dineen ,  Matthew Weiss ,  Vinod F. Patel ,  Xiao Mei Zheng ,  Ryan White

    IPC分类号： A61K31/553 ,  A61K31/554 ,  C07D498/10 ,  C07D498/20 ,  C07D513/10 ,  C07D513/20

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

    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, R2, R7, X 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 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 Formulas (II) and sub-formula embodiments of Formula (I) and (II), intermediates and processes and methods useful for the preparation of compounds of Formulas (I)-(II).

    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。 该化合物具有通式（I）; 其中式（I）的变量A1，A3，A4，A5，A6，A8，R2，R7，X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（I）和（II）的式（II）和亚式实施方案的化合物，可用于制备式（I） - （II）化合物的中间体和方法和方法。

    Spiro-Amino-Imidazo-Fused Heterocyclic Compounds as Beta-secretase Modulators and Methods of Use
    7.
    发明申请
    Spiro-Amino-Imidazo-Fused Heterocyclic Compounds as Beta-secretase Modulators and Methods of Use 有权
    螺氨基 - 咪唑并 - 杂环化合物作为β-分泌酶调节剂和使用方法

    公开(公告)号：US20140038954A1

    公开(公告)日：2014-02-06

    申请号：US13982096

    申请日：2012-02-13

    申请人： Oleg Epstein ,  Ryan White ,  Vinod F. Patel ,  Jason Human

    发明人： Oleg Epstein ,  Ryan White ,  Vinod F. Patel ,  Jason Human

    IPC分类号： C07D491/20

    CPC分类号： C07D491/20 ,  A61K31/353

    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, R2, R7, X, Y and Z 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 and impairments, schizophrenia and other central nervous system conditions and disorders. The invention further provides compounds of Formulas II and III, and of sub-formulas of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulas 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，R2，R7，X，Y和Z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介导的病症包括例如阿尔茨海默病，认知缺陷和损伤，精神分裂症和其他中枢神经系统病症和障碍。 本发明还提供了式II和III的化合物和式I，II和III的分子式，可用于制备式I-III化合物的中间体和方法和方法。

    Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
    8.
    发明授权
    Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use 有权
    螺氨基 - 咪唑稠合杂环化合物作为β-分泌酶调节剂和使用方法

    公开(公告)号：US08962859B2

    公开(公告)日：2015-02-24

    申请号：US13982096

    申请日：2012-02-13

    申请人： Oleg Epstein ,  Ryan White ,  Vinod F. Patel ,  Jason Brooks Human

    发明人： Oleg Epstein ,  Ryan White ,  Vinod F. Patel ,  Jason Brooks Human

    IPC分类号： C07D487/10 ,  C07D313/00 ,  C07D491/20 ,  A61K31/353

    CPC分类号： C07D491/20 ,  A61K31/353

    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, A5, A6, A8, R2, R7, X, Y and Z 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 and impairments, schizophrenia and other central nervous system conditions and disorders. The invention further provides compounds of Formulas II and III, and of sub-formulas of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulas 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，A5，A6，A8，R2，R7，X，Y和Z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介导的病症包括例如阿尔茨海默病，认知缺陷和损伤，精神分裂症和其他中枢神经系统病症和障碍。 本发明还提供了式II和III的化合物和式I，II和III的分子式，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
    9.
    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
    10.
    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 ）。