Invention Grant
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
- Patent Title: Substituted imidazo [1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives
- Patent Title (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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Application No.: US11245736Application Date: 2005-10-07
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Publication No.: US07671048B2Publication Date: 2010-03-02
- Inventor: Henner Knust , Heinz Stadler , Andrew William Thomas
- Applicant: Henner Knust , Heinz Stadler , Andrew William Thomas
- Applicant Address: US NJ Nutley
- Assignee: Hoffmann-La Roche Inc.
- Current Assignee: Hoffmann-La Roche Inc.
- Current Assignee Address: US NJ Nutley
- Agent George W. Johnston; Patricia S. Rocha-Tramaloni; Kimberly J. Prior
- Priority: EP04105000 20041012
- Main IPC: A61P25/28
- IPC: A61P25/28 ; A61K31/5517 ; C07D487/12
![Substituted imidazo [1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives](/abs-image/US/2010/03/02/US07671048B2/abs.jpg.150x150.jpg)
Abstract:
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.
Public/Granted literature
- US20060079507A1 Substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives Public/Granted day:2006-04-13
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