发明公开
- 专利标题: AROMATIC ACETYLCHOLINESTERASE INHIBITORS
- 专利标题(中): 芳香乙酰胆碱酯酶抑制剂
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申请号: EP94917916.0申请日: 1994-05-05
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公开(公告)号: EP0701546A1公开(公告)日: 1996-03-20
- 发明人: COLLARD, Jean-Noel , HORNSPERGER, Jean-Marie , SCHIRLIN, Daniel
- 申请人: MERRELL PHARMACEUTICALS INC.
- 申请人地址: 2110 East Galbraith Road Cincinnati Ohio 45215 US
- 专利权人: MERRELL PHARMACEUTICALS INC.
- 当前专利权人: MERRELL PHARMACEUTICALS INC.
- 当前专利权人地址: 2110 East Galbraith Road Cincinnati Ohio 45215 US
- 代理机构: Gillard, Marie-Louise, et al
- 优先权: EP19930401431 19930604
- 国际公布: WO1994029255 19941222
- 主分类号: A61K31
- IPC分类号: A61K31 ; A61P25 ; A61P43 ; C07C17 ; C07C33 ; C07C39 ; C07C43 ; C07C45 ; C07C49 ; C07C69 ; C07C211 ; C07C225 ; C07C247 ; C07C255 ; C07C309
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.
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