公开(公告)号：EP1368342B1

公开(公告)日：2005-09-07

申请号：EP01992307.7

申请日：2001-12-21

申请人： NEUROGEN CORPORATION ,  PFIZER INC.

发明人： LI, Guiying ,  PETERSON, John, M. ,  ALBAUGH, Pamela ,  CURRIE, Kevin, S. ,  CAI, Guolin ,  GUSTAVSON, Linda, M. ,  LEE, Kyungae ,  HUTCHISON, Alan ,  SINGH, Vinod ,  MAYNARD, George, D. ,  YUAN, Jun ,  LING HONG, Xie ,  GHOSH, Manuka ,  LIU, Nian ,  LUKE, George, P. ,  MITCHELL, Scott ,  ALLEN, Martin, Patrick ,  LIRAS, Spiros

IPC分类号： C07D401/14 ,  C07D403/06 ,  C07D413/14 ,  C07D403/14 ,  C07D471/04 ,  C07D417/04 ,  C07D403/04 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14 ,  A61K31/415 ,  A61P25/00

CPC分类号： C07D401/04 ,  C07D233/20 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D491/08 ,  C07D491/10

摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula (I). 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. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I 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.

公开(公告)号：EP1368342A2

公开(公告)日：2003-12-10

申请号：EP01992307.7

申请日：2001-12-21

申请人： NEUROGEN CORPORATION ,  PFIZER INC.

发明人： LI, Guiying ,  PETERSON, John, M. ,  ALBAUGH, Pamela ,  CURRIE, Kevin, S. ,  CAI, Guolin ,  GUSTAVSON, Linda, M. ,  LEE, Kyungae ,  HUTCHISON, Alan ,  SINGH, Vinod ,  MAYNARD, George, D. ,  YUAN, Jun ,  LING HONG, Xie ,  GHOSH, Manuka ,  LIU, Nian ,  LUKE, George, P. ,  MITCHELL, Scott ,  ALLEN, Martin, Patrick ,  LIRAS, Spiros

IPC分类号： C07D401/14 ,  C07D403/06 ,  C07D413/14 ,  C07D403/14 ,  C07D471/04 ,  C07D417/04 ,  C07D403/04 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14 ,  A61K31/415 ,  A61P25/00

CPC分类号： C07D401/04 ,  C07D233/20 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D491/08 ,  C07D491/10

摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula (I). 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. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I 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.

公开(公告)号：EP1368342B3

公开(公告)日：2010-12-01

申请号：EP01992307.7

申请日：2001-12-21

申请人： NEUROGEN CORPORATION ,  Pfizer Inc.

发明人： LI, Guiying ,  PETERSON, John, M. ,  ALBAUGH, Pamela ,  CURRIE, Kevin, S. ,  CAI, Guolin ,  GUSTAVSON, Linda, M. ,  LEE, Kyungae ,  HUTCHISON, Alan ,  SINGH, Vinod ,  MAYNARD, George, D. ,  YUAN, Jun ,  LING HONG, Xie ,  GHOSH, Manuka ,  LIU, Nian ,  LUKE, George, P. ,  MITCHELL, Scott ,  ALLEN, Martin, Patrick ,  LIRAS, Spiros

IPC分类号： C07D401/14 ,  C07D403/06 ,  C07D413/14 ,  C07D403/14 ,  C07D471/04 ,  C07D417/04 ,  C07D403/04 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14 ,  A61K31/415 ,  A61P25/00

CPC分类号： C07D401/04 ,  C07D233/20 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D491/08 ,  C07D491/10

摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula (I). 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. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I 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.

公开(公告)号：EP1406906A1

公开(公告)日：2004-04-14

申请号：EP02749983.9

申请日：2002-07-12

申请人： NEUROGEN CORPORATION

发明人： HUTCHISON, Alan ,  MAYNARD, George ,  ALBAUGH, Pamela ,  XIE, Linghong ,  YUAN, Jun ,  MITCHELL, Scott ,  SINGH, Vinod ,  GHOSH, Manuka ,  LI, Guiying ,  LIU, Nian

IPC分类号： C07D513/04 ,  C07D471/04 ,  C07D487/04 ,  A61K31/437 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/4985 ,  A61P25/00

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D513/04

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 relates 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.