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：EP0915859B1

公开(公告)日：2003-01-02

申请号：EP97934217.7

申请日：1997-07-18

申请人： NEUROGEN CORPORATION

发明人： BLUM, Charles, A. ,  HUTCHISON, Alan ,  PETERSON, John, M.

IPC分类号： C07D295/18 ,  C07D491/10 ,  C07D211/86 ,  C07D211/84 ,  A61K31/495

CPC分类号： C07D213/75 ,  C07C2601/14 ,  C07D215/38 ,  C07D233/38 ,  C07D295/135 ,  C07D295/155

公开(公告)号：EP0793653A1

公开(公告)日：1997-09-10

申请号：EP95942473.0

申请日：1995-11-22

申请人： NEUROGEN CORPORATION

发明人： THURKAUF, Andrew ,  HORVATH, Raymond, F. ,  YUAN, Jun ,  PETERSON, John, M.

IPC分类号： C07D233 ,  A61K31 ,  A61P25 ,  A61P43 ,  C07D401 ,  C07D403 ,  C07D487

CPC分类号： C07D233/64 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

摘要： Disclosed are compounds of formula (III), wherein R1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R3 and R4 are organic or inorganic substituents which may together form ring structures; m is zero, one or two; and R5 and R6 are organic or inorganic substituents; and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.

公开(公告)号：EP1678149A2

公开(公告)日：2006-07-12

申请号：EP04796879.7

申请日：2004-10-28

申请人： NEUROGEN CORPORATION

发明人： BAKTHAVATCHALAM, Rajagopal ,  BLUM, Charles, A. ,  BRIELMANN, Harry ,  CALDWELL, Timothy, M. ,  CORTRIGHT, Daniel, N. ,  HODGETTS, Kevin, J. ,  PETERSON, John, M. ,  ZHENG, Xiaozhang

IPC分类号： C07D239/94

CPC分类号： C04B35/632 ,  C07D215/44 ,  C07D239/94 ,  C07D401/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04 ,  C07D475/06

摘要： Capsaicin receptor agonists are provided. Such compounds are ligands that may be used to modulate VRl activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to capsaicin 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.

摘要翻译： 提供了辣椒素受体激动剂。 这样的化合物是可以用于体内或体外调节VR1活性的配体，并且特别可用于治疗对人，家养伴侣动物和家畜动物中辣椒素受体活化有反应的病症。 提供了使用它们治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

公开(公告)号：EP1720542A1

公开(公告)日：2006-11-15

申请号：EP05729370.6

申请日：2005-03-01

申请人： NEUROGEN CORPORATION

发明人： BAKTHAVATCHALAM, Rajagopal ,  CHENARD, Bertrand, L. ,  PETERSON, John, M. ,  STEENSTRA, Cheryl, K.

IPC分类号： A61K31/395 ,  A61K31/505 ,  C07D215/16 ,  C07D239/95

CPC分类号： C07D401/04 ,  C07D239/94 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D491/10

摘要： Arylalkylamino-substituted quinazoline analogues are provided, of the Formula wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

公开(公告)号：EP1392692B1

公开(公告)日：2006-11-15

申请号：EP02728576.6

申请日：2002-03-27

申请人： NEUROGEN CORPORATION

发明人： LI, Guiying ,  PETERSON, John, M. ,  ALBAUGH, Pamela

IPC分类号： C07D487/04 ,  A61K31/437 ,  A61P25/24 ,  A61P25/28

CPC分类号： C07D487/04

摘要： Disclosed are compounds of the formula: (I), and the pharmaceuticallz acceptable salts thereof where the variables R1, R2, A, R4, R5, R6, R6', n, and W are defined herein. These compounds bind to the benzodiazepine site of GABAA receptors are provided and, therefore can 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.

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：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：EP1165518A2

公开(公告)日：2002-01-02

申请号：EP00919946.4

申请日：2000-03-31

申请人： NEUROGEN CORPORATION

发明人： DESIMONE, Robert, W. ,  HUTCHISON, Alan ,  SHAW, Kenneth ,  MAYNARD, George, D. ,  PETERSON, John, M. ,  LEW, Richard ,  BRIELMANN, Harry, L.

IPC分类号： C07D235/14 ,  C07D471/04 ,  C07D403/10 ,  C07D401/06 ,  A61K31/415 ,  A61K31/495 ,  A61K31/535 ,  A61K31/44

CPC分类号： C07D471/04

摘要： Disclosed are compounds of formula (I) or pharmaceutically acceptable salts thereof wherein: R1 is not 3-fluorobenzyl and represents (C2-C6) alkenyl, aryl (C1-C6)alkyl or heteroaryl (C1-C6)alkyl, OR7, O(CH2)nC(O)R7, O(CH2)nNR7R8, O(CH2)nCO2R7, NR7COR8, COR7, CONR7R8 or CO2R7; R2 represents hydrogen, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, amino (C1-C6)alkyl, mono- or di(C1-C6)alkylamino (C1-C6), or mono- or di(C1-C6)alkylamino(C1-C6)alkoxy; or OR7, O(CH2)nC(O)R7, O(CH2)nNR7R8, O(CH2)nCO2R7, NR7COR8, COR7, CONR7R8 or CO2R7; R3 represents (C1-C6)alkyl; R4 represents halogen or trifluoromethyl; R5 and R6 represent hydrogen, trifluoromethyl, triluoromethoxy, cyano, (C1-C6)alkyl, halogen, (C1-C6)alkylamino(C1-C6)alkyl, mono or di(C1-C6)alkylamino(C1-C6), or mono- or di(C1-C6)alkylamino(C1-C6)alkoxy; or together form a 5 or 6 membered aromatic ring which is optionally substituted. X represents a bond or CH2 which is optionally mono- or disubstituted with a (C1-C6)alkyl or (C1-C6)alkoxy; and A, B, C and D are the same or different and represent CRp or N with the proviso that not more than two of A,B, C and D represent N; which compounds are selective modulators of Bradykinin B2 receptors.

公开(公告)号：EP0915860A1

公开(公告)日：1999-05-19

申请号：EP97934218.0

申请日：1997-07-18

申请人： NEUROGEN CORPORATION

发明人： BLUM, Charles, A. ,  HUTCHISON, Alan ,  PETERSON, John, M.

IPC分类号： C07D295 ,  A61K31 ,  A61P3 ,  A61P9 ,  A61P43 ,  C07D211 ,  C07D491

CPC分类号： C07D295/135 ,  C07D211/46 ,  C07D211/74 ,  C07D295/155 ,  C07D491/10

摘要： This invention encompasses compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein X1, X2, X3 represent organic or inorganic susbtituents, n is 1, 2, or 3, R1-R4 are hydrogen or organic substituents, and B is nitrogen, carbon, sulfur or oxygen, useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to human Neuropeptide Y1 receptors.

摘要翻译： 本发明包括式（I）化合物及其药学上可接受的盐，其中X 1，X 2，X 3代表有机或无机的取代基，n是1,2或3，R 1 -R 4是氢或有机取代基，B是氮 ，碳，硫或氧，可用于诊断和治疗喂养障碍，如肥胖和贪食症和心血管疾病，如原发性高血压和由于这些化合物与人神经肽Y1受体结合导致的充血性心力衰竭。