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    • 3. 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
    • 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
    • US20130172343A1
    • 2013-07-04
    • US13814232
    • 2011-08-04
    • Ana Elena MinattiYuan ChengWenge Zhong
    • Ana Elena MinattiYuan ChengWenge Zhong
    • C07D491/20C07D498/20C07D498/22C07D491/22
    • C07D491/20A61K31/436A61K31/437A61K31/537C07D491/22C07D498/20C07D498/22
    • 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.
    • 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。