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：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：EP1745024A1

公开(公告)日：2007-01-24

申请号：EP05747952.9

申请日：2005-05-06

申请人： NEUROGEN CORPORATION

发明人： LEE, Kyungae ,  YUAN, Jun ,  MAYNARD, George, D. ,  HUTCHISON, Alan ,  MITCHELL, Scott

IPC分类号： C07D217/02 ,  A61K31/47

CPC分类号： C07D405/12 ,  A61K31/47 ,  C07D217/14 ,  C07D217/16 ,  C07D217/22 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D413/14

摘要： 1-Aryl-4-substituted isoquinolines analogues of Formula (I) and Formula (II) are provided, as follows : wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula (I) and (II) bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 1-aryl-4-substituted isoquinolines, which are useful as probes for the localization of C5a receptors.

公开(公告)号：EP1745039A2

公开(公告)日：2007-01-24

申请号：EP05783074.7

申请日：2005-05-06

申请人： NEUROGEN CORPORATION

发明人： YOON, Taeyoung ,  YUAN, Jun ,  LEE, Kyungae ,  MAYNARD, George, D. ,  LIU, Nian

IPC分类号： C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  A61K31/501 ,  A61K31/502 ,  A61K31/5377 ,  A61K31/55

CPC分类号： C07D237/20 ,  C07D237/34 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D413/04

摘要： The present invention provides compounds of Formula (I) or (II) salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions.

公开(公告)号：EP1565452A2

公开(公告)日：2005-08-24

申请号：EP03768799.3

申请日：2003-11-07

申请人： NEUROGEN CORPORATION

发明人： HUTCHISON, Alan ,  YUAN, Jun ,  LEE, Kyungae ,  MAYNARD, George ,  CHENARD, Bertrand, L. ,  LIU, Nian ,  GUO, Qin ,  GUO, Zihong ,  HRNCIAR, Peter

IPC分类号： C07D401/04

CPC分类号： C07D213/30 ,  C07B2200/05 ,  C07D213/38 ,  C07D213/42 ,  C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/71 ,  C07D213/74 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C40B40/00

摘要： 3-substituted-6-aryl pyridines of Formula (I) are provided: Formula (I) wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula (I) bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.

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：EP1487798A1

公开(公告)日：2004-12-22

申请号：EP03714371.6

申请日：2003-03-25

申请人： Neurogen Corporation

发明人： MITCHELL, Scott ,  OHLIGER, Robert ,  ZHANG, LuYan ,  ZHAO, He ,  CURRIE, Kevin ,  LEE, Kyungae

IPC分类号： C07D217/04 ,  A61K31/47

CPC分类号： C07D221/20 ,  A61K31/47 ,  C07D211/14 ,  C07D211/70 ,  C07D217/04 ,  C07D217/14 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D417/12 ,  C07D495/04

摘要： Substituted tetrahydroisoquinolines of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.