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：EP1392302A1

公开(公告)日：2004-03-03

申请号：EP02741732.8

申请日：2002-05-22

申请人： NEUROGEN CORPORATION

发明人： GE, Ping ,  YOON, Taeyoung ,  ZHANG, Lu, Yan ,  HORVATH, Raymond, F.

IPC分类号： A61K31/4418 ,  C07D213/65 ,  C07D213/74 ,  A61K31/44 ,  C07D213/69 ,  A61P25/24 ,  A61P25/00 ,  A61P9/00

CPC分类号： C07D213/68 ,  C07D213/65 ,  C07D213/69 ,  C07D213/74 ,  C07D213/82 ,  C07D413/04

摘要： Novel 5-substituted-2-arylpyridine compounds 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：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：EP1165517A1

公开(公告)日：2002-01-02

申请号：EP00918516.6

申请日：2000-03-31

申请人： NEUROGEN CORPORATION

发明人： HORVATH, Raymond, F. ,  GE, Ping ,  YOON, Taeyoung ,  HUTCHISON, Alan

IPC分类号： C07D235/14 ,  C07D209/14 ,  A61K31/4184 ,  A61K31/4045 ,  A61P25/00 ,  G01N33/50

CPC分类号： C07D209/14 ,  C07D235/14 ,  G01N2333/726

摘要： Disclosed are compounds of formula (I); or the pharmaceutically acceptable non-toxic salts thereof wherein; A is N or CH; R1 and R2 represents hydrogen or lower alkyl; G, R3, R4, R5, R6, R7 and R8 are variables defined herein. These compounds are modulators of CRF receptors and are therefore useful for treating affective disorders, anxiety, depression, eating disorders, and stress disorders in humans and other animals. Methods of treatment of such disorders as 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：EP1680424A2

公开(公告)日：2006-07-19

申请号：EP04788585.0

申请日：2004-09-03

申请人： NEUROGEN CORPORATION ,  Aventis Pharmaceuticals, Inc.

发明人： GE, Ping ,  HORVATH, Raymond, F. ,  ZHANG, Lu, Yan ,  YAMAGUCHI, Yasuchika ,  KAISER, Bernd ,  ZHANG, Xuechun ,  ZHANG, Suoming ,  ZHAO, He ,  JOHN, Stanly ,  MOORCROFT, Neil ,  SHUTSKE, Greg

IPC分类号： C07D487/04

CPC分类号： C07D471/04 ,  C07D487/04

摘要： Substituted heteroaryl fused pyridine, pyrazine, and pyrimidine 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：EP1675858A2

公开(公告)日：2006-07-05

申请号：EP04788563.7

申请日：2004-09-03

申请人： NEUROGEN CORPORATION ,  Aventis Pharmaceuticals, Inc.

发明人： HODGETTS, Kevin, J. ,  JOHN, Stanly ,  MOORCROFT, Neil ,  SHUTSKE, Greg ,  KAISER, Bernd ,  YAMAGUCHI, Yasuchika ,  GE, Ping ,  HORVATH, Raymond, F.

IPC分类号： C07D487/04 ,  C07D471/04 ,  C07D519/00 ,  A61K31/519 ,  A61K31/437 ,  A61P25/18 ,  A61P25/22

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D519/00

摘要： 5-aryl-Pyrazolo[4,3-d] pyrimidines, 6-aryl-Pyrazolo[3,4-d]pyrimidines and related compounds, as well as other chemically related 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 CRIF receptor binding. Methods of using the compounds in receptor localization studies are given.

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：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：EP1909797A2

公开(公告)日：2008-04-16

申请号：EP06788999.8

申请日：2006-07-28

申请人： NEUROGEN CORPORATION

发明人： XIE, Linghong ,  OCHTERSKI, Joseph W. ,  GAO, Yang ,  HAN, Bingsong ,  CALDWELL, Timothy M. ,  XU, Yuelian ,  PETERSON, John M. ,  GE, Ping ,  OHLIGER, Robert

IPC分类号： A61K31/551 ,  A61K31/55 ,  A61K31/497 ,  A61K31/496 ,  A61K31/4545 ,  A61K31/454 ,  C07D403/02

CPC分类号： C07D403/06 ,  C07D207/09 ,  C07D207/14 ,  C07D211/14 ,  C07D211/34 ,  C07D211/52 ,  C07D211/58 ,  C07D211/64 ,  C07D211/72 ,  C07D213/74 ,  C07D213/82 ,  C07D215/48 ,  C07D217/02 ,  C07D237/20 ,  C07D237/22 ,  C07D237/24 ,  C07D239/47 ,  C07D241/08 ,  C07D241/20 ,  C07D243/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/56 ,  C07D277/82 ,  C07D295/033 ,  C07D295/185 ,  C07D295/192 ,  C07D295/215 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/04 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D491/10 ,  C07D491/107

摘要： Dipiperazinyl ketones and related analogues are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).