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1. 发明申请

WO1994029255A1 AROMATIC ACETYLCHOLINESTERASE INHIBITORS 审中-公开
标题翻译：芳香乙酰胆碱酯酶抑制剂
公开(公告)号：WO1994029255A1
公开(公告)日：1994-12-22
申请号：PCT/US1994004957
申请日：1994-05-05
申请人： MERRELL DOW PHARMACEUTICALS INC. , COLLARD, Jean-Noel , HORNSPERGER, Jean-Marie , SCHIRLIN, Daniel
发明人： MERRELL DOW PHARMACEUTICALS INC.
IPC分类号： C07C49/80
CPC分类号： C07C225/22 , C07C17/35 , C07C17/361 , C07C33/46 , C07C45/45 , C07C45/673 , C07C49/80 , C07C49/82 , C07C49/84 , C07C69/63 , C07C25/02 , C07C25/13
摘要： Compounds of general formula (I), stereoisomers and pharmaceutically acceptable salts thereof, wherein each of Z and Z' are independently H or F; Q is (a), CH(OH), (b); X is H, Br, Cl, F or CF3; Y is H, Br, Cl, F, OH, OR5, OC(O)R4, N3, CN, NO2, SO3H, CO2R4, NH2, NHR9, NR9R'9, C(R6)(R7)(V'R8) or C(O)R7, provided that when both Z and Z' are F, then Y is H or F; V and V' are each independently CH2 or O; R1 is H or CH3; R2, R9 and R'9 are each independently (C1-6)alkyl, or R2 and V-R3 taken together with the carbon atom to which they are attached form a 3-6 membered ring; R3, R6, R7 and R8 are each independently H, (C1-6)alkyl, or (C3-6)cycloalkyl; R4 is H, (C1-10)alkyl, (C0-4)alkylene aryl or (C3-8)cycloalkyl; and R5 is (C1-10)alkyl, benzyl, phenethyl or (C3-6)cycloalkyl, possess anticholinesterase activity and may be used in the treatment of Degenerativa Dementias.
摘要翻译：通式（I）的化合物，其立体异构体和药学上可接受的盐，其中Z和Z'各自独立地为H或F; Q是（a），CH（OH），（b）; X是H，Br，Cl，F或CF 3; Y为H，Br，Cl，F，OH，OR5，OC（O）R4，N3，CN，NO2，SO3H，CO2R4，NH2，NHR9，NR9R'9，C（R6）（R7）（V'R8）或C（O）R7，条件是当Z和Z'均为F时，则Y为H或F; V和V'各自独立地为CH 2或O; R1是H或CH3; R2，R9和R'9各自独立地为（C1-6）烷基，或R2和V-R3与它们所连接的碳原子一起形成3-6元环; R 3，R 6，R 7和R 8各自独立地为H，（C 1-6）烷基或（C 3-6）环烷基; R4是H，（C1-10）烷基，（C0-4）亚烷基芳基或（C3-8）环烷基; 并且R 5是（C 1-10）烷基，苄基，苯乙基或（C 3-6）环烷基）具有抗胆碱酯酶活性并可用于治疗退行性痴呆。

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