公开(公告)号：EP1569925A1

公开(公告)日：2005-09-07

申请号：EP03813410.2

申请日：2003-12-12

申请人： NEUROGEN CORPORATION

发明人： BAKTHAVATCHALAM, Rajagopal ,  BLUM, Charles, A. ,  BRIELMANN, Harry ,  CALDWELL, Timothy, M. ,  DE LOMBAERT, Stephane ,  HODGETTS, Kevin, J. ,  ZHENG, Xiaozhang

IPC分类号： C07D401/04 ,  C07D471/04

CPC分类号： C07D417/14 ,  C07D239/94 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  C07D491/10 ,  C07F9/65128 ,  C07F9/65583 ,  C07F9/6561

摘要： Certain 2-substituted quinazolin-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.

公开(公告)号：EP1347982A2

公开(公告)日：2003-10-01

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

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：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：EP1218381B1

公开(公告)日：2006-12-06

申请号：EP00967132.2

申请日：2000-09-29

申请人： NEUROGEN CORPORATION ,  PFIZER INC.

发明人： DARROW, James W. ,  DE LOMBAERT, Stephane ,  BLUM, Charles ,  TRAN, Jennifer ,  GIANGIORDANO, Mark ,  GRIFFITH, David Andrew ,  CARPINO, Philip Albert

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/53 ,  A61P9/00 ,  A61P25/00 ,  G01N33/566

CPC分类号： C07D487/04 ,  G01N2333/5755 ,  G01N2333/70571

摘要： Disclosed are compounds of the formula: (I), where R?1, R2, R3, R4, R5, R6¿, and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. 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 NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.

摘要翻译： 公开了下式的化合物：其中R 1，R 2，R 3，R 4，R 5，R 6和X如本文所定义。 这些化合物是NPY1受体的选择性调节剂。 这些化合物可用于治疗许多CNS障碍，代谢障碍和外周障碍，特别是进食障碍和高血压。 还提供了治疗此类病症的方法以及包装的药物组合物。 本发明化合物还可用作NPY1受体定位的探针，并作为NPY1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：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：EP1569926A1

公开(公告)日：2005-09-07

申请号：EP03813411.0

申请日：2003-12-12

申请人： NEUROGEN CORPORATION

发明人： BAKTHAVATCHALAM, Rajagopal ,  BLUM, Charles, A. ,  BRIELMANN, Harry ,  CALDWELL, Timothy, M. ,  DE LOMBAERT, Stephane ,  HODGETTS, Kevin, J. ,  ZHENG, Xiaozhang

IPC分类号： C07D401/04 ,  C07D471/04 ,  C07F9/09 ,  C07F9/38

CPC分类号： C07D417/14 ,  C07D239/94 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  C07D491/10 ,  C07F9/65128 ,  C07F9/65583 ,  C07F9/6561

摘要： Acid-substituted quinazolin-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： 提供了酸取代的喹唑啉-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：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：EP1218379A2

公开(公告)日：2002-07-03

申请号：EP00967134.8

申请日：2000-09-29

申请人： NEUROGEN CORPORATION ,  PFIZER INC.

发明人： DARROW, James, W. ,  DE LOMBAERT, Stephane ,  BLUM, Charles ,  TRAN, Jennifer ,  GIANGIORDANO, Mark ,  GRIFFITH, David, Andrew ,  CARPINO, Philip, Albert

IPC分类号： C07D487/00 ,  A61K31/53 ,  A61K31/519 ,  A61P9/00 ,  A61P25/00 ,  G01N33/566

CPC分类号： C07D487/04 ,  G01N2333/5755 ,  G01N2333/70571

摘要： Disclosed are compounds of formula (I), where R?1, R2, R3, R4, R5, R6¿, and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. 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 NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.

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：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.