公开(公告)号：US06476030B1

公开(公告)日：2002-11-05

申请号：US09806879

申请日：2001-06-08

申请人： William Robert Carling ,  Andrew Mitchinson ,  Kevin William Moore ,  Michael Geoffrey Russell ,  Gayle Scott ,  Leslie Joseph Street

发明人： William Robert Carling ,  Andrew Mitchinson ,  Kevin William Moore ,  Michael Geoffrey Russell ,  Gayle Scott ,  Leslie Joseph Street

IPC分类号： C07D48704

CPC分类号： C07D487/04

摘要： Compounds according to Formula (I): or a salt or prodrug thereof, have good affinity as ligands for the alpha2 and/or alpha3 subunit of the human GABAA receptor and are useful for treatment of disorders of the central nervous system, including anxiety and convulsions.

摘要翻译： 根据式（I）的化合物或其盐或前药与人类GABA A受体的α2和/或α3亚基的配体具有良好的亲和力，并且可用于治疗中枢神经系统疾病，包括焦虑和抽搐 。

公开(公告)号：US06828322B2

公开(公告)日：2004-12-07

申请号：US10463075

申请日：2003-06-17

申请人： William Robert Carling ,  Jose Luis Castro Pineiro ,  Ian James Collins ,  Alexander Richard Guiblin ,  Timothy Harrison ,  Andrew Madin ,  Kevin William Moore ,  Michael Geoffrey Russell ,  Gayle Scott ,  Leslie Joseph Street

发明人： William Robert Carling ,  Jose Luis Castro Pineiro ,  Ian James Collins ,  Alexander Richard Guiblin ,  Timothy Harrison ,  Andrew Madin ,  Kevin William Moore ,  Michael Geoffrey Russell ,  Gayle Scott ,  Leslie Joseph Street

IPC分类号： A61K315025

CPC分类号： C07D487/04

摘要： A class of substituted 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a fluoro-substituted phenyl ring at the 3-position and a heteroaryl-methoxy moiety at the 6-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

摘要翻译： 在3-位上具有氟取代的苯环和6-位上的杂芳基 - 甲氧基部分的一类取代的1,2,4-三唑并[4,3-b]哒嗪衍生物是GABAA的选择性配体 受体，特别是对其α2和/或α3亚基具有高亲和力，因此有益于治疗和/或预防中枢神经系统疾病，包括焦虑和抽搐。

公开(公告)号：US06579875B1

公开(公告)日：2003-06-17

申请号：US09582589

申请日：2000-06-28

申请人： William Robert Carling ,  Jose Luis Castro Pineiro ,  Ian James Collins ,  Alexander Richard Guiblin ,  Timothy Harrison ,  Andrew Madin ,  Kevin William Moore ,  Michael Geoffrey Russell ,  Gayle Scott ,  Leslie Joseph Street

发明人： William Robert Carling ,  Jose Luis Castro Pineiro ,  Ian James Collins ,  Alexander Richard Guiblin ,  Timothy Harrison ,  Andrew Madin ,  Kevin William Moore ,  Michael Geoffrey Russell ,  Gayle Scott ,  Leslie Joseph Street

IPC分类号： A61K315025

CPC分类号： C07D487/04

摘要： 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a fluoro-substituted phenyl ring at the 3-position and a heteroaryl-alkoxy moiety at the 6-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, are useful in the treatment of anxiety and convulsions.

摘要翻译： 在3-位具有氟取代的苯环和6-位的杂芳基 - 烷氧基部分的1,2,4-三唑并[4,3-b]哒嗪衍生物是GABA A受体的选择性配体，特别是 对α2和/或α3亚基具有高亲和力，可用于治疗焦虑和抽搐。