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公开(公告)号：US5854268A
公开(公告)日：1998-12-29
申请号：US776024
申请日：1997-01-22
申请人： Raymond Baker , Sylvie Bourrain , Jose Luis Castro Pineiro , Mark Stuart Chambers , Alexander Richard Guiblin , Sarah Christine Hobbs , Richard Alexander Jelley , Andrew Madin , Victor Giulio Matassa , Austin John Reeve , Michael Geoffrey Russell , Graham Andrew Showell , Francine Sternfeld , Leslie Joseph Street , Monique Bodil Van Niel
发明人： Raymond Baker , Sylvie Bourrain , Jose Luis Castro Pineiro , Mark Stuart Chambers , Alexander Richard Guiblin , Sarah Christine Hobbs , Richard Alexander Jelley , Andrew Madin , Victor Giulio Matassa , Austin John Reeve , Michael Geoffrey Russell , Graham Andrew Showell , Francine Sternfeld , Leslie Joseph Street , Monique Bodil Van Niel
IPC分类号： C07D401/14 , A61K31/41 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/475 , A61P9/00 , A61P25/04 , A61P43/00 , C07D403/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D521/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： A class of substituted azetidine, pyrrolidine and piperidine derivatives are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
摘要翻译： PCT No.PCT / GB95 / 01819 Sec。 371日期1997年1月22日 102（e）1997年1月22日PCT PCT 1995年8月1日PCT公布。 公开号WO96 / 04274 日期1996年2月15日一类取代的氮杂环丁烷，吡咯烷和哌啶衍生物是5-HT1样受体的选择性激动剂，它是人类5-HT1Dα受体亚型的有效激动剂，同时具有至少10倍的选择性亲和力 5-HT1Dα受体亚型相对于5-HT1Dβ亚型; 因此，它们可用于治疗和/或预防临床状况，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比 与非亚型选择性5-HT1D受体激动剂相关的那些。
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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。
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3.发明授权公开(公告)号：US06255305B1
公开(公告)日：2001-07-03
申请号：US09155587
申请日：1998-11-10
申请人： Howard Barff Broughton , William Robert Carling , Jose Luis Castro Pineiro , Alexander Richard Guiblin , Andrew Madin , Kevin William Moore , Michael Geoffrey Russell , Leslie Joseph Street
发明人： Howard Barff Broughton , William Robert Carling , Jose Luis Castro Pineiro , Alexander Richard Guiblin , Andrew Madin , Kevin William Moore , Michael Geoffrey Russell , Leslie Joseph Street
IPC分类号： A61K375025
CPC分类号： C07D487/04 , C07D487/08
摘要： Substituted triazolo-pyridazine derivative compounds represented by wherein the variables are disclosed herein are selective ligands for GABA-A receptors, particularly for the &agr;2 and/or &agr;3 subunits.
摘要翻译： 由本文公开的变量中所表示的取代的三唑并 - 哒嗪衍生物化合物是GABA-A受体的选择性配体，特别是对于α2和/或α3亚基。
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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。
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公开(公告)号：US6150391A
公开(公告)日：2000-11-21
申请号：US117328
申请日：1998-07-21
IPC分类号： A61P25/06 , C07D521/00 , A61K31/4178 , C07D403/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： Compounds having formula I, or pharmaceutically acceptable salts or prodrugs thereof: ##STR1## are selective agonists of the 5-HT.sub.1D.alpha. receptor and are useful in the treatment of migraine and associated conditions.
摘要翻译： PCT No.PCT / GB97 / 00181 Sec。 371日期：1998年9月28日 102（e）日期1998年9月28日PCT 1997年1月21日PCT PCT。 公开号WO97 / 28162 日期：1997年8月7日具有式I化合物或其药学上可接受的盐或前体药物：是5-HT1Dα受体的选择性激动剂，可用于治疗偏头痛和相关病症。
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6.发明授权(1,8) naphthyridines as gaba ligands, their pharmaceutical compositions and uses 失效（1,8）萘啶作为加巴配体，其药物组合物和用途公开(公告)号：US06960598B2
公开(公告)日：2005-11-01
申请号：US10483242
申请日：2002-07-03
IPC分类号： A61P25/22 , C07D471/04 , A61K31/44 , C07D265/30
CPC分类号： C07D471/04
摘要： A class of [1,8] naphthyridine analogues which are substituted in the 4-position by a substituted phenyl ring. These compounds are ligands for GABAA receptors and useful in the therapy of deleterious mental states such as anxiety.
摘要翻译： 一类通过取代的苯环在4-位取代的[1,8]萘啶类似物。 这些化合物是GABA A A受体的配体，可用于治疗有害精神状态如焦虑症。
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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 。
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公开(公告)号：US06872720B2
公开(公告)日：2005-03-29
申请号：US10240971
申请日：2001-04-04
IPC分类号： A61K31/53 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07B61/00 , C07D487/04
CPC分类号： C07D487/04
摘要： A class of substituted pyrazolo[1,5-d][1,2,4]triazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 7-position, an alkyl group at the 4-position, and a substituted alkoxy moiety at the 2-position, are selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 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： 一类取代的吡唑并[1,5-d] [1,2,4]三嗪衍生物，其在7-位具有任选取代的环烷基，苯基或杂芳基取代基，4-位的烷基和取代的 2-位的烷氧基部分是GABA A受体的选择性配体，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。
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