公开(公告)号：EP1301484A2

公开(公告)日：2003-04-16

申请号：EP01959075.1

申请日：2001-07-20

申请人： NEUROGEN CORPORATION ,  Hutchison, Alan ,  Desimone, Robert W. ,  Hodgetts, Kevin J. ,  Krause, James E. ,  White, Geoffrey G.

发明人： BAKTHAVATCHALAM, Rajagopal

IPC分类号： C07D213/74 ,  C07D401/04 ,  C07D295/192 ,  C07D295/21 ,  C07D295/215 ,  C07D241/20 ,  C07D403/04 ,  C07D405/12 ,  C07D417/12 ,  C07D217/22 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/444 ,  A61K31/496 ,  A61K31/495 ,  A61K31/4725 ,  A61P19/02 ,  A61P29/00 ,  A61P25/02 ,  A61P25/06

CPC分类号： C07D213/74 ,  C07D213/75 ,  C07D217/22 ,  C07D241/20 ,  C07D405/12 ,  C07D417/12

摘要： Disclosed are diaryl piperazines and related compounds. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.

公开(公告)号：EP1465888A2

公开(公告)日：2004-10-13

申请号：EP03708824.2

申请日：2003-01-09

申请人： NEUROGEN CORPORATION ,  De Simone, Robert ,  Peterson, John ,  Steenstra, Cheryl ,  Shen, Yiping ,  Gustavson, Linda ,  Bakthavatchalam, Rajagopal ,  Hutchison, Alan

发明人： DE SIMONE, Robert ,  PETERSON, John ,  STEENSTRA, Cheryl ,  SHEN, Yiping ,  GUSTAVSON, Linda ,  BAKTHAVATCHALAM, Rajagopal ,  HUTCHISON, Alan

IPC分类号： C07D401/10 ,  C07D401/14 ,  A61K31/454

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D235/14 ,  C07D249/08 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D513/04

摘要： Melanin concentrating hormone receptor ligands (especially substituted benzoimidazole analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors 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：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：EP1651636A1

公开(公告)日：2006-05-03

申请号：EP04778036.6

申请日：2004-07-09

申请人： NEUROGEN CORPORATION

发明人： BAKTHAVATCHALAM, Rajagopal ,  HODGETTS, Kevin, J. ,  HUTCHISON, Alan, J. ,  OHLIGER, Robert ,  YOON, Taeyoung ,  ZHENG, Xiaozhang

IPC分类号： C07D401/12 ,  C07D251/52 ,  C07D251/54 ,  C07D401/14 ,  A61K31/506 ,  A61K31/53 ,  A61P17/02 ,  A61P11/06 ,  A61P19/00 ,  A61P13/02 ,  A61P11/14 ,  A61P3/04

CPC分类号： C07D401/12 ,  A61K31/506 ,  A61K31/53 ,  C07D251/52 ,  C07D251/54 ,  C07D401/14 ,  G01N33/566

摘要： Substituted heterocyclic diarylamine analogues of Formula I are provided: wherein X, Y and Z are independently N or optionally substituted C, and other variables are as described in the specification. 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

公开(公告)号：EP1644372A2

公开(公告)日：2006-04-12

申请号：EP04779026.6

申请日：2004-07-14

申请人： NEUROGEN CORPORATION

发明人： BAKTHAVATCHALAM, Rajagopal ,  CALDWELL, Timothy, M. ,  CHENARD, Bertrand, L. ,  DE LOMBAERT, Stéphane ,  HODGETTS, Kevin, J.

IPC分类号： C07D471/04 ,  C07D401/04 ,  C07D491/04

CPC分类号： C07D401/04 ,  C07D215/44 ,  C07D471/04 ,  C07D491/14

摘要： Substituted quinolin-4-ylamine analogues are provided. 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

摘要翻译： 提供了取代的喹啉-4-基胺类似物。 此类化合物是可用于体内或体外调节特定受体活性的配体，并且特别用于治疗与人，家养伴侣动物和家畜动物中的病理性受体激活相关的病症。 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：EP1347982B1

公开(公告)日：2005-11-16

申请号：EP01270536.4

申请日：2001-12-11

申请人： NEUROGEN CORPORATION ,  PFIZER INC.

发明人： BAKTHAVATCHALAM, Rajagopal ,  BLUM, Charles, A. ,  BRIELMANN, Harry, L. ,  DARROW, James, William ,  DE LOMBAERT, Stephane ,  HUTCHISON, Alan ,  TRAN, Jennifer ,  ZHENG, Xiaozhang ,  ELLIOTT, Richard, Louis ,  HAMMOND, Marlys

IPC分类号： C07D491/10 ,  A61K31/517 ,  A61K31/438

CPC分类号： C07D487/04 ,  C07D491/10

摘要： Substituted spiro [isobenzofuran-1,4'-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4'-piperidines capable of modulating NPY5 receptor activity are provided (1) . Such compounds may be used to modulate ligand binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders(e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and method for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.

公开(公告)号：EP1575918A2

公开(公告)日：2005-09-21

申请号：EP03800070.9

申请日：2003-12-19

申请人： NEUROGEN CORPORATION

发明人： BAKTHAVATCHALAM, Rajagopal ,  BLUM, Charles, A. ,  BRIELMANN, Harry ,  DARROW, James, W. ,  DE LOMBAERT, Stephane ,  YOON, Taeyoung ,  ZHENG, Xiaozhang

IPC分类号： C07D213/61 ,  C07C235/64 ,  C07D213/82 ,  C07D213/26 ,  C07D213/48 ,  C07D405/12 ,  C07D213/73 ,  C07D211/34 ,  C07D213/76 ,  A61K31/44 ,  A61P25/00 ,  C07D417/12 ,  C07D401/12 ,  C07D405/04 ,  C07D405/14

CPC分类号： C07D213/76 ,  C07C233/65 ,  C07C233/66 ,  C07C233/75 ,  C07C235/64 ,  C07D211/34 ,  C07D213/26 ,  C07D213/48 ,  C07D213/61 ,  C07D213/73 ,  C07D213/82 ,  C07D213/85 ,  C07D241/16 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D417/12

摘要： Substituted biphenyl-4-carboxylic acid arylamide analogues of the formula (I) capable of modulating receptor activity, are provided. Such ligands may be used to modulate receptor activity in vivo or in vitro, and are particularly useful in the treatment of pain and other conditions associated with receptor activation 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 receptor localization studies.

公开(公告)号：EP1678173A2

公开(公告)日：2006-07-12

申请号：EP04783712.5

申请日：2004-09-09

申请人： NEUROGEN CORPORATION

发明人： BAKTHAVATCHALAM, Rajagopal ,  BLUM, Charles, A. ,  CHENARD, Bertrand, L.

IPC分类号： C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D401/12

CPC分类号： C07D401/12 ,  C04B35/632 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： Substituted bicyclic quinazolin-4-ylamine derivatives are provided. 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

公开(公告)号：EP1644358A2

公开(公告)日：2006-04-12

申请号：EP04778532.4

申请日：2004-07-16

申请人： NEUROGEN CORPORATION

发明人： BAKTHAVATCHALAM, Rajagopal ,  BLUM, Charles, A. ,  BRIELMANN, Harry ,  CHENARD, Bertrand, L. ,  DE LOMBAERT, Stéphane ,  HODGETTS, Kevin, J. ,  HUTCHISON, Alan ,  YOON, Taeyoung ,  ZHENG, Xiaozhang

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D251/48 ,  C07D403/14 ,  C07D413/14 ,  A61K31/496 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377

CPC分类号： C04B35/632 ,  A61K31/496 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  C07D251/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

摘要： Biaryl piperazinyl -pyri dine analogues are provided, of the Formula (I): 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.

摘要翻译： 提供式（I）的联芳基哌嗪基 - 吡啶类似物：其中变量如本文所述。 此类化合物是可用于体内或体外调节特定受体活性的配体，并且特别用于治疗与人，家养伴侣动物和家畜动物中的病理性受体激活相关的病症。 提供了使用这些化合物治疗这些病症的药物组合物和方法，以及使用这些配体的方法进行受体定位研究。

公开(公告)号：EP1366030A2

公开(公告)日：2003-12-03

申请号：EP01957558.8

申请日：2001-07-06

申请人： Neurogen Corporation

发明人： BAKTHAVATCHALAM, Rajagopal ,  HUTCHISON, Alan ,  THURKAUF, Andrew

IPC分类号： C07D295/096 ,  A61K31/495 ,  A61P3/04 ,  C07D295/08 ,  C07D295/06 ,  C07D295/18 ,  C07D211/22 ,  A61K31/445

CPC分类号： C07D295/096

摘要： Disclosed are compounds of formula (I), and the pharmaceutically acceptable salts thereof wheren Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.