发明申请
US20060128691A1 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: US11297691申请日: 2005-12-08
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公开(公告)号: US20060128691A1公开(公告)日: 2006-06-15
- 发明人: Bernd Buettelmann , Henner Knust , Andrew Thomas
- 申请人: Bernd Buettelmann , Henner Knust , Andrew Thomas
- 优先权: EP04106556.6 20041214
- 主分类号: A61K31/551
- IPC分类号: A61K31/551 ; C07D487/14
摘要:
The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, nitro, cycloalkyl, —O(CH2)mO(CH2)mOH or —C≡C—R′; R2 is hydrogen or methyl; R3 is lower alkyl, lower alkyl substituted by halogen, lower alkenyl, lower alkenyl substituted by halogen, lower alkynyl, —(CH2)n-cycloalkyl, —(CR′R″)m—CH3, phenyl that is unsubstituted or substituted by halogen, pyridinyl or thienyl each of which is unsubstituted or substituted by lower alkyl, —(CH2)n—NH-cycloalkyl, lower alkenyl-cycloalkyl, lower alkynyl-(CR′R″)mOH, or lower alkynyl-phenyl wherein the phenyl ring is unsubstituited or substituted by halogen, CF3, lower alkyl or lower alkoxy; R′ is hydrogen or lower alkyl; R″ is hydrogen, hydroxy or lower alkyl; n is 0, 1 or 2; m is 1, 2 or 3; and o is 1 or 2; and pharmaceutically acceptable acid addition salts thereof. This class of compounds have high affinity and selectivity for GABA A α5 receptor binding sites. Thus, the invention also relates to methods of enhancing cognition and treating cognitive disorders like Alzheimer's disease.
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