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：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：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：EP1224187A2

公开(公告)日：2002-07-24

申请号：EP00967133.0

申请日：2000-09-29

申请人： NEUROGEN CORPORATION ,  PFIZER INC.

发明人： HORVATH, Raymond, F. ,  TRAN, Jennifer ,  DE LOMBAERT, Stephane ,  HODGETTS, Kevin, Julian ,  CARPINO, Philip, A. ,  GRIFFITH, David, A.

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/437 ,  A61K31/4365 ,  A61K31/47 ,  A61K31/44 ,  A61P9/00 ,  A61P25/00 ,  C07D471/04 ,  C07D473/34 ,  C07D215/46 ,  C07D213/73 ,  C07D239/48 ,  C07D471/14 ,  C07D495/04 ,  C07D475/08 ,  G01N33/566

CPC分类号： C07D213/73 ,  C07D215/46 ,  C07D239/48 ,  C07D471/04 ,  C07D471/14 ,  C07D473/34 ,  C07D475/08 ,  C07D487/04 ,  C07D495/04 ,  G01N2333/5755 ,  G01N2333/70571

摘要： The present invention also provides a general method to whereby mono-, bi-, or tri-cyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula (I-XV).

公开(公告)号：EP1224187B1

公开(公告)日：2006-02-22

申请号：EP00967133.0

申请日：2000-09-29

申请人： NEUROGEN CORPORATION ,  PFIZER INC.

发明人： HORVATH, Raymond, F. ,  TRAN, Jennifer ,  DE LOMBAERT, Stephane ,  HODGETTS, Kevin, Julian ,  CARPINO, Philip, A. ,  GRIFFITH, David, A.

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/437 ,  A61K31/4365 ,  A61K31/47 ,  A61K31/44 ,  A61P9/00 ,  A61P25/00 ,  C07D471/04 ,  C07D473/34 ,  C07D215/46 ,  C07D213/73 ,  C07D239/48 ,  C07D471/14 ,  C07D495/04 ,  C07D475/08 ,  G01N33/566 ,  C07D239/00 ,  C07D209/00 ,  C07D235/00 ,  C07D221/00

CPC分类号： C07D213/73 ,  C07D215/46 ,  C07D239/48 ,  C07D471/04 ,  C07D471/14 ,  C07D473/34 ,  C07D475/08 ,  C07D487/04 ,  C07D495/04 ,  G01N2333/5755 ,  G01N2333/70571

摘要： The present invention also provides a general method to whereby mono-, bi-, or tri-cyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula (I-XV).

公开(公告)号：EP1322620A1

公开(公告)日：2003-07-02

申请号：EP01977701.0

申请日：2001-10-05

申请人： Neurogen Corporation

发明人： DE LOMBAERT, Stephane ,  GE, Ping ,  HORVATH, Raymond, F. ,  YOON, Taeyoung

IPC分类号： C07D235/14 ,  C07D209/14 ,  C07D401/14 ,  C07D401/04 ,  C07D403/04 ,  C07D403/06 ,  C07D401/06 ,  A61K31/4184 ,  A61K31/454 ,  A61K31/4439 ,  A61P25/00 ,  G01N33/50

CPC分类号： C07D231/12 ,  C07D209/14 ,  C07D233/56 ,  C07D235/14 ,  C07D249/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  G01N2333/726

摘要： Benzimidazole and indole derivatives of the formula (I) that act as selective modulators of CRF 1 receptors are provided. These compounds 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 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.