公开(公告)号：US08957083B2

公开(公告)日：2015-02-17

申请号：US13988745

申请日：2011-11-18

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

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

IPC: C07D491/107 ,  C07D491/20

CPC classification number: C07D491/107 ,  C07D491/20

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 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.

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。

公开(公告)号：US20130338177A1

公开(公告)日：2013-12-19

申请号：US13988745

申请日：2011-11-18

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

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

IPC: C07D491/107 ,  C07D491/20

CPC classification number: C07D491/107 ,  C07D491/20

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 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).

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 ）。