发明授权
EP1711470B1 MALONAMIDE DERIVATIVES BLOCKING THE ACTIVTIY OF GAMMA-SECRETASE
有权
γ-分泌BLOCKING MALONAMIDDERIVATE的活动
- 专利标题: MALONAMIDE DERIVATIVES BLOCKING THE ACTIVTIY OF GAMMA-SECRETASE
- 专利标题(中): γ-分泌BLOCKING MALONAMIDDERIVATE的活动
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申请号: EP04764665.8申请日: 2004-08-31
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公开(公告)号: EP1711470B1公开(公告)日: 2009-04-15
- 发明人: FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric, Argirios , PETERS, Jens-Uwe , WOSTL, Wolfgang
- 申请人: F. Hoffmann-La Roche AG
- 申请人地址: Grenzacherstrasse 124 4070 Basel CH
- 专利权人: F. Hoffmann-La Roche AG
- 当前专利权人: F. Hoffmann-La Roche AG
- 当前专利权人地址: Grenzacherstrasse 124 4070 Basel CH
- 代理机构: Poppe, Regina
- 优先权: EP03019683 20030909
- 国际公布: WO2005023772 20050317
- 主分类号: C07D223/18
- IPC分类号: C07D223/18 ; C07D223/16 ; C07D243/14 ; C07D313/14 ; A61K31/5513 ; A61K31/55
摘要:
The invention relates to malonamide derivatives of formula (I), wherein: R1 is one of the following groups (Formulae a), b), c), d)); R2 is lower alkyl, lower alkinyl, -(CH2)n-O-lower alkyl, -(CH2)n-S-lower alkyl, -(CH2)n-CN, -(CR'R')n-CF3, -(CR'R')n-CHF2, -(CR'R')n-CH2F, -(CH2)n-C(O)O-lower alkyl, -(CH2)n-halogen, or is -(CH2)n-cycloalkyl, optionally substituted by one or more substituents, selected from the group consisting of phenyl, halogen or CF3; R',R' are independently from n and from each other hydrogen, lower alkyl, lower alkoxy, halogen or hydroxy; R3, R4 are independently from each other hydrogen, lower alkyl, lower alkoxy, phenyl or halogen; R5 is hydrogen, lower alkyl, -(CH2)n-CF3 or -(CH2)n-cycloalkyl; R6 is hydrogen or halogen; R7 is hydrogen or lower alkyl; R8 is hydrogen, lower alkyl, lower alkinyl, -(CH2)n-CF3,-(CH2)n-cycloalkyl or -(CH2)n-phenyl, optionally substituted by halogen; R9 is hydrogen, lower alkyl, -C(O)H, -C(O)-lower alkyl, -C(O)-CF3,-C(O)-CH2F,-C(O)-CHF2,-C(O)-cycloalkyl,-C(O)-(CH2)n-O-lower alkyl,-C(O)O-(CH2)n-cycloalkyl, -C(O)-phenyl, optionally substituted by one or more substituents selected from the group consisting of halogen or -C(O)O-lower alkyl, or is -S(O)2-lower alkyl, -S(O)2-CF3,-(CH2)n-cycloalkyl or is -(CH2)n-phenyl, optionally substituted by halogen; n is 0, 1, 2, 3 or 4; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixture thereof. These compounds may be used for the treatment of Alzheimer's disease.
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