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：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。