公开(公告)号：EP1554258A1

公开(公告)日：2005-07-20

申请号：EP03793200.1

申请日：2003-08-20

申请人： NEUROGEN CORPORATION ,  Aventis Pharmaceuticals Inc.

发明人： YOON, Taeyoung ,  GE, Ping ,  DELOMBAERT, Stephane ,  HORVATH, Raymond ,  YAMAGUCHI, Yasuchika ,  DOLLER, Dario ,  LU, Jingqi ,  HODGETTS, Kevin, J. ,  JOHN, Stanly ,  KAISER, Bernd ,  ZHANG, Xeuchun ,  SHUTSKE, Greg ,  ZHANG, Cunyu ,  DARROW, Jim ,  MOORCROFT, Neil

IPC分类号： C07D241/20 ,  C07D241/18 ,  C07D241/26 ,  C07D401/04 ,  A61K31/497 ,  A61P25/22 ,  A61P25/24

CPC分类号： C07D241/12 ,  C07D241/18 ,  C07D241/20 ,  C07D241/26 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04

摘要： Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators of CRF receptors. The 5-substituted-2-arylpyrazine compounds provided herein are useful in the treatment of a number of CNS and peripheral disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

公开(公告)号：EP1399428A1

公开(公告)日：2004-03-24

申请号：EP02737167.3

申请日：2002-05-22

申请人： Neurogen Corporation

发明人： HUANG, Kianhua ,  HODGETTS, Kevin ,  DOLLER, Dario ,  GE, Ping ,  YAMAGUCHI, Yasuchika

IPC分类号： C07D241/12 ,  C07D401/04 ,  C07D239/34 ,  A61K31/44 ,  A61K31/495 ,  A61K31/505 ,  A61P25/00

CPC分类号： A61K31/00 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0463 ,  C07D213/74 ,  C07D241/12 ,  C07D401/04

摘要： Diarylpyrazine, diarylpyridine, and diarylpyrimidine compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of formula I are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

摘要翻译： 提供了充当CRF1受体的选择性调节剂的二芳基吡嗪，二芳基吡啶和二芳基嘧啶化合物。 这些化合物可用于治疗许多CNS和周围疾病，特别是压力，焦虑，抑郁，心血管疾病和进食障碍。 还提供了治疗此类病症的方法以及包装的药物组合物。 式I化合物也可用作CRF受体定位探针，并作为CRF受体结合测定的标准。 给出了在受体定位研究中使用这些化合物的方法。

公开(公告)号：EP1255740A2

公开(公告)日：2002-11-13

申请号：EP01910939.6

申请日：2001-02-16

申请人： NEUROGEN CORPORATION ,  Yoon, Taeyoung ,  Ge, Ping ,  Horvath, Raymond F. ,  De Lombaert, Stephane ,  Hodgetts, Kevin J.

发明人： YOON, Taeyoung ,  GE, Ping ,  HORVATH, Raymond, F. ,  DE LOMBAERT, Stephane ,  HODGETTS, Kevin, J. ,  DOLLER, Dario ,  ZHANG, Cunyu

IPC分类号： C07D241/18 ,  C07D241/20 ,  C07D241/12 ,  C07D409/04 ,  C07D401/04 ,  C07D403/04 ,  C07D401/12 ,  C07D405/12 ,  A61K31/4965 ,  A61P25/00 ,  C07D241/52

CPC分类号： C07D401/04 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/5355 ,  C07D241/12 ,  C07D241/18 ,  C07D241/20 ,  C07D401/12 ,  C07D403/04 ,  C07D405/12 ,  C07D409/04

摘要： Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affiity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.

摘要翻译： 提供了芳基吡嗪化合物，包括芳基吡嗪，其可以高亲和性和高选择性结合CRF1受体，包括人CRF1受体。 因此，本发明包括用于治疗与CRF1受体相关的病症和疾病的方法，所述CRF1受体包括CNS相关障碍和疾病，特别是情感障碍和疾病以及急性和慢性神经障碍和疾病。

公开(公告)号：EP1809626A2

公开(公告)日：2007-07-25

申请号：EP05812516.2

申请日：2005-10-04

申请人： NEUROGEN CORPORATION

发明人： CHENARD, Bertrand, L ,  GHOSH, Manuka ,  DOLLER, Dario ,  HUTCHISON, Alan, J. ,  LI, Guiying

IPC分类号： C07D451/06 ,  C07D451/02 ,  C07D451/04 ,  A61K31/46 ,  A61P3/04

CPC分类号： C07D451/02 ,  C07D451/04 ,  C07D451/06

摘要： Aryl substituted 8-azabicyclo[3.2.1]octane compounds and analogues thereof, are provided. Such compounds 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, neuropsychiatric, reproductive 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：EP1734820A2

公开(公告)日：2006-12-27

申请号：EP05778777.2

申请日：2005-04-15

申请人： NEUROGEN CORPORATION

发明人： DOLLER, Dario ,  ZHANG, Lu Yan ,  GE, Ping ,  YAMAGUCHI, Yasuchika ,  HORVATH, Raymond, F. ,  ZHANG, Xuechun

IPC分类号： A01N43/04 ,  A01N43/60 ,  A01N43/58 ,  A01N43/42 ,  A61K31/53 ,  A61K31/50 ,  A61K31/44 ,  A61K31/495 ,  C07D487/00 ,  C07D471/00 ,  C07D491/00

CPC分类号： C07D487/04 ,  C07D471/04

摘要： Novel aryl substituted imidazopyrazines, imidazopyrimidines, and imidazopyridines are provided. Such compounds can act as selective modulators of CRF receptors. The 5-substituted-2-arylpyridine compounds provided herein are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

公开(公告)号：EP1729762A2

公开(公告)日：2006-12-13

申请号：EP05743960.6

申请日：2005-03-28

申请人： NEUROGEN CORPORATION

发明人： KRAUSE, James ,  DOLLER, Dario ,  BERETTA, Elena ,  RAJACHANDRAN, Lavanya ,  BRODBECK, Robbin

IPC分类号： A61K31/397 ,  A61K31/40 ,  A61K31/55 ,  A61K31/535 ,  A61K31/4965 ,  A61K31/445 ,  A61K31/415 ,  A61K31/38

CPC分类号： A61K45/06 ,  A61K31/454 ,  A61K31/5377 ,  A61K2300/00

摘要： Compositions and methods are provided for weight management. The compositions generally comprise a MCHR antagonist, either in combination with a CB1 antagonist or formulated for coadministration with a CB1 antagonist. Certain methods involve coadministering a MCHR antagonist and a CB1 antagonist to a patient.

公开(公告)号：EP1301490A2

公开(公告)日：2003-04-16

申请号：EP01958986.0

申请日：2001-07-18

申请人： NEUROGEN CORPORATION

发明人： HODGETTS, Kevin, J. ,  DOLLER, Dario

IPC分类号： C07D239/47 ,  C07D239/52 ,  A61K31/505 ,  A61P25/22 ,  A61P25/24 ,  G01N33/50

CPC分类号： C07D239/36 ,  C07D239/47 ,  C07D239/52

摘要： Arylpyrimidinone compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. 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 CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

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：EP1255740B1

公开(公告)日：2005-10-19

申请号：EP01910939.6

申请日：2001-02-16

申请人： NEUROGEN CORPORATION

发明人： YOON, Taeyoung ,  GE, Ping ,  HORVATH, Raymond, F. ,  DE LOMBAERT, Stephane ,  HODGETTS, Kevin, J. ,  DOLLER, Dario ,  ZHANG, Cunyu

IPC分类号： C07D241/18 ,  C07D241/20 ,  C07D241/12 ,  C07D409/04 ,  C07D401/04 ,  C07D403/04 ,  C07D401/12 ,  C07D405/12 ,  A61K31/4965 ,  A61P25/00 ,  C07D241/52

CPC分类号： C07D401/04 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/5355 ,  C07D241/12 ,  C07D241/18 ,  C07D241/20 ,  C07D401/12 ,  C07D403/04 ,  C07D405/12 ,  C07D409/04

摘要： Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affiity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.

摘要翻译： 提供了芳基吡嗪化合物，包括可以以高亲和力和对CRF 1受体（包括人CRF 1受体）的高选择性结合的芳基吡嗪。 因此，本发明包括治疗与CRF 1受体相关的疾病和疾病的方法，包括CNS相关疾病和疾病，特别是情感障碍和疾病，以及急性和慢性神经障碍和疾病。

公开(公告)号：EP1389189A2

公开(公告)日：2004-02-18

申请号：EP02746423.9

申请日：2002-05-21

申请人： NEUROGEN CORPORATION

发明人： HUTCHISON, Alan ,  PETERSON, John ,  DOLLER, Dario ,  GUSTAVSON, Linda, E. ,  CALDWELL, Timothy ,  YOON, Taeyoung ,  PRINGLE, Wallace ,  BAKTHAVATCHALAM, Rajagopal ,  SHEN, Yiping ,  STEENSTRA, Cheryl ,  YIN, Helen ,  DE SIMONE, Robert ,  HE, Xiao-shu

IPC分类号： C07D213/74 ,  C07D295/08 ,  C07D215/12 ,  C07D471/04 ,  C07D513/04 ,  C07D487/04 ,  C07D295/18 ,  C07D487/08 ,  C07D243/08 ,  C07D401/12 ,  C07D209/86 ,  C07D239/46 ,  C07D211/52 ,  C07D317/58 ,  C07D215/20

CPC分类号： C07D513/04 ,  C07D209/86 ,  C07D211/52 ,  C07D213/64 ,  C07D213/74 ,  C07D215/12 ,  C07D215/20 ,  C07D243/08 ,  C07D295/096 ,  C07D295/108 ,  C07D311/18 ,  C07D317/58 ,  C07D401/12 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08

摘要： Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptir 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).