发明授权
US06936617B2 Heteroaryl substituted fused bicyclic heteroaryl compound as GABAA receptor ligands
失效
杂芳基取代的稠合双环杂芳基化合物作为GABA A受体配体
- 专利标题： Heteroaryl substituted fused bicyclic heteroaryl compound as GABAA receptor ligands
- 专利标题（中）： 杂芳基取代的稠合双环杂芳基化合物作为GABA A受体配体
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申请号： US10194852申请日： 2002-07-12
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公开(公告)号： US06936617B2公开(公告)日： 2005-08-30
- 发明人: Alan Hutchison , George Maynard , Pamela Albaugh , Linghong Xie , Jun Yuan , Scott Mitchell , Vinod Singh , Manuka Ghosh , Guiying Li , Nian Liu
- 申请人： Alan Hutchison , George Maynard , Pamela Albaugh , Linghong Xie , Jun Yuan , Scott Mitchell , Vinod Singh , Manuka Ghosh , Guiying Li , Nian Liu
- 申请人地址： US CT Branford
- 专利权人： Neurogen Corporation
- 当前专利权人： Neurogen Corporation
- 当前专利权人地址： US CT Branford
- 代理机构： McDonnell Boehnen Hulbert & Berghoff LLP
- 主分类号： G01N33/48
- IPC分类号： G01N33/48 ; A61K31/4355 ; A61K31/4439 ; A61K31/444 ; A61K31/4985 ; A61K31/5025 ; A61K31/506 ; A61K31/519 ; A61P25/00 ; A61P25/14 ; A61P25/18 ; A61P25/20 ; A61P25/22 ; A61P25/24 ; A61P25/28 ; A61P43/00 ; C07D471/04 ; C07D487/04 ; C07D513/04 ; C12N15/09 ; C12Q1/02 ; G01N33/58 ; G01N33/60 ; A61K31/437
摘要：
This invention relates to heteroaryl substituted fused bicyclic heteroaryl compounds, such as heteroaryl substituted imidazopyridines, imidazopyrazines, imidazopyridizines, imidazopyrimidines, and imidazothiazoles, which may be described by Formula I or Formula II: The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Processes for preparing compounds of Formula I and Formula II are disclosed.This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I or Formula II in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.