公开(公告)号：EP1756107A2

公开(公告)日：2007-02-28

申请号：EP05760258.3

申请日：2005-06-16

申请人： NEUROGEN CORPORATION

发明人： HUTCHISON, Alan, J. ,  CHENARD, Bertrand, L. ,  LI, Guiying ,  GHOSH, Manuka ,  TARRANT, James, G. ,  YOON, Taeyoung ,  LUKE, George, P. ,  LEE, Kyungae ,  O'DONNELL, Mary-Margaret, E. ,  PRINGLE, Wallace, C. ,  PETERSON, John, M. ,  HODGETTS, Kevin, J. ,  STEENSTRA, Cheryl, K. ,  DOLLER, Dario

IPC分类号： C07D471/04 ,  C07D487/08 ,  C07D487/04 ,  C07D211/74 ,  C07D207/26 ,  C07D207/08 ,  C07D307/79 ,  C07D295/08 ,  C07D295/06 ,  C07D211/34 ,  A61P3/00

CPC分类号： C07D295/073 ,  C07D207/08 ,  C07D207/12 ,  C07D207/26 ,  C07D207/38 ,  C07D211/18 ,  C07D211/34 ,  C07D211/38 ,  C07D211/42 ,  C07D211/46 ,  C07D211/52 ,  C07D211/74 ,  C07D213/64 ,  C07D213/74 ,  C07D213/82 ,  C07D231/12 ,  C07D233/54 ,  C07D233/56 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D261/08 ,  C07D275/02 ,  C07D295/088 ,  C07D295/096 ,  C07D295/192 ,  C07D307/20 ,  C07D307/79 ,  C07D307/82 ,  C07D309/06 ,  C07D309/12 ,  C07D311/14 ,  C07D401/12 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08

摘要： Aryl-substituted piperazine derivatives are provided. Such compounds may be used to modulate MCH receptor activity in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).

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：EP1325006A2

公开(公告)日：2003-07-09

申请号：EP01964561.3

申请日：2001-08-06

申请人： NEUROGEN CORPORATION ,  PFIZER INC.

发明人： MAYNARD, George ,  YOHANNES, Daniel ,  YUAN, Jun ,  XIE, Linghong ,  GHOSH, Manuka ,  LUKE, George, P. ,  LIU, Xiaojun ,  NAGEL, Art ,  VINCENT, Lawrence, Albert ,  CURRIE, Kevin, S. ,  WANG, Zhe-Qing ,  LEE, Kyungae

IPC分类号： C07D471/14

CPC分类号： C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D487/14 ,  C07D513/04

摘要： Disclosed are heterocyclic compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables A, V, Y, J, E, X, G, Q, W, Z, b, n and m are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptor.

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：EP1506194A1

公开(公告)日：2005-02-16

申请号：EP03736638.2

申请日：2003-05-15

申请人： NEUROGEN CORPORATION

发明人： MAYNARD, George, D. ,  YUAN, Jun ,  LUKE, George, P. ,  CURRIE, Kevin

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P25/00

CPC分类号： C07D471/04

摘要： (Formula I). Substituted ring-fused imidazole derivatives that bind to GABAA receptors are provided. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent (s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).

公开(公告)号：EP1506194B1

公开(公告)日：2006-07-19

申请号：EP03736638.2

申请日：2003-05-15

申请人： NEUROGEN CORPORATION

发明人： MAYNARD, George, D. ,  YUAN, Jun ,  LUKE, George, P. ,  CURRIE, Kevin

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P25/00 ,  G01N33/566

CPC分类号： C07D471/04

摘要： (Formula I). Substituted ring-fused imidazole derivatives that bind to GABAA receptors are provided. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent (s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).

公开(公告)号：EP1490343A1

公开(公告)日：2004-12-29

申请号：EP03726169.0

申请日：2003-03-28

申请人： Neurogen Corporation

发明人： LUKE, George, P. ,  MAYNARD, George ,  MITCHELL, Scott ,  THURKAUF, Andrew ,  XIE, Linghong ,  ZHANG, LuYan ,  ZHANG, Suoming ,  ZHAO, He ,  CHENARD, Bertrand, L. ,  GAO, Yang ,  HAN, Bingsong ,  HE, Xiao, Shu

IPC分类号： C07D233/54 ,  A61K31/4164

CPC分类号： C07D233/64 ,  A61K31/4164 ,  C07D233/68 ,  C07D235/02 ,  C07D235/30 ,  C07D237/12 ,  C07D401/04 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

摘要： The invention provides Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula (I) where the ring system represented by Formula (A) is a 5 membered heteroaryl ring system, in which x is 0, A is chosen from carbon and heteroatoms nitrogen, oxygen, and sulfur, and E and G are independently carbon or nitrogen, provided that the 5 membered heteroaryl ring system does not contain more than 3 heteroatoms or more than 1 oxygen or sulfur atom, or a 6 membered heteroaryl ring system, in which x is 1, A, B, E, and G are independently chosen from carbon and nitrogen, provided that the 6 membered heteroaryl ring system does not contain more than 3 nitrogen atoms. The remaining variables, Ar1, Ar2, R, R1, R2, R3, R4, R5, R6, y and z are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of the invention act bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders.

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.