发明申请
- 专利标题: MODULATORS FOR AMYLOID BETA
- 专利标题(中): AMYLOID BETA的调节剂
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申请号: PCT/EP2009/050036申请日: 2009-01-05
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公开(公告)号: WO2009087127A1公开(公告)日: 2009-07-16
- 发明人: BAUMANN, Karlheinz , FLOHR, Alexander , GOETSCHI, Erwin , JACOBSEN, Helmut , JOLIDON, Synese , LUEBBERS, Thomas
- 申请人: F. HOFFMANN-LA ROCHE AG , BAUMANN, Karlheinz , FLOHR, Alexander , GOETSCHI, Erwin , JACOBSEN, Helmut , JOLIDON, Synese , LUEBBERS, Thomas
- 申请人地址: Grenzacherstrasse 124 CH-4070 Basel CH
- 专利权人: F. HOFFMANN-LA ROCHE AG,BAUMANN, Karlheinz,FLOHR, Alexander,GOETSCHI, Erwin,JACOBSEN, Helmut,JOLIDON, Synese,LUEBBERS, Thomas
- 当前专利权人: F. HOFFMANN-LA ROCHE AG,BAUMANN, Karlheinz,FLOHR, Alexander,GOETSCHI, Erwin,JACOBSEN, Helmut,JOLIDON, Synese,LUEBBERS, Thomas
- 当前专利权人地址: Grenzacherstrasse 124 CH-4070 Basel CH
- 代理机构: POPPE, Regina
- 优先权: EP08150173.6 20080111
- 主分类号: C07D277/60
- IPC分类号: C07D277/60 ; C07D401/14 ; C07D403/12 ; C07D413/14 ; C07D417/12 ; C07D417/14 ; C07D471/04 ; C07D491/052 ; C07D513/04 ; C07D491/113 ; A61P25/28 ; A61K31/428 ; A61K31/517 ; A61K31/519 ; A61K31/527
摘要:
The invention relates to compounds of formula (I) R 1 is -C(O)O-lower alkyl, cyano or is hetaryl; hetaryl is a five-or six membered heteraryl group, optionally substituted by R'; R' is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or lower alkoxy substituted by halogen; R 2 is hydrogen, lower alkoxy, lower alkyl, halogen or cyano; R 3 is -(CH 2 ) n -C(O)O-lower alkyl, lower alkyl, lower alkoxy, hydroxy, -O-Si(CH 3 ) 2 -lower alkyl, -C(O)-N(lower alkyl) 2 , -O-S(O) 2 -lower alkyl, C 3-7 -cycloalkyl, S(O) 2 -aryl, heterocyclyl, -C(O)-heterocyclyl, or is aryl or hetaryl, which aryl or hetaryl rings are optionally substituted by one or more R'; R 4 is hydrogen, lower alkyl, hydroxy or CH 2 CN; X is S or -N=C(R 5 )-; R 5 is hydrogen, lower alkyl or hydroxy, is a bond, -O-, -CH 2 -, -CH 2 -CH 2 -, formula (II) or or -N(R)-; R is hydrogen, lower alkyl, C(O)O-lower alkyl, C(O)-lower alkyl, S(O) 2 -lower alkyl, or benzyl; n is 0 or 1 or to pharmaceutically active acid addition salts. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.