发明授权
US07671048B2 Substituted imidazo [1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives
失效
取代的咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂衍生物
- 专利标题: Substituted imidazo [1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives
- 专利标题(中): 取代的咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂衍生物
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申请号: US11245736申请日: 2005-10-07
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公开(公告)号: US07671048B2公开(公告)日: 2010-03-02
- 发明人: Henner Knust , Heinz Stadler , Andrew William Thomas
- 申请人: Henner Knust , Heinz Stadler , Andrew William Thomas
- 申请人地址: US NJ Nutley
- 专利权人: Hoffmann-La Roche Inc.
- 当前专利权人: Hoffmann-La Roche Inc.
- 当前专利权人地址: US NJ Nutley
- 代理商 George W. Johnston; Patricia S. Rocha-Tramaloni; Kimberly J. Prior
- 优先权: EP04105000 20041012
- 主分类号: A61P25/28
- IPC分类号: A61P25/28 ; A61K31/5517 ; C07D487/12
摘要:
The present invention is concerned with a method of treating a disease selected from the group consisting of cognitive disorders, anxiety, Alzheimer's disease, and schizophrenia comprising administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the following formula wherein R1 is halogen, lower alkyl, lower alkynyl, cycloalkyl, lower alkoxy, OCF3, —NHR, —NHC(O)R or —NHSO2R; R2 is hydrogen, methyl or aryl which is unsubstituted or substituted by one or two substituents selected from the group consisting of halogen and lower alkoxy; R3 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, lower alkoxy, —O(CH2)n+1—O-lower alkyl, —(CH2)n-aryl which is optionally substituted by lower alkyl or halogen, heteroaryl, —NHR, —N(R)2, wherein each R can be the same or different, —NHCH2C≡CH, or pyrrolidin-1-one; R is hydrogen, lower alkyl, lower alkyl substituted by halogen, heteroaryl, —(CH2)nO-lower alkyl, —NH-lower alkyl, cycloalkyl or aryl, and n is 0, 1, 2 or 3; and with their pharmaceutically acceptable acid addition salts. The invention also provides novel compounds of formula I-A and pharmaceutical compositions containing them. The most preferred indication is Alzheimer's disease.