公开(公告)号：US07030128B2

公开(公告)日：2006-04-18

申请号：US10472680

申请日：2002-03-19

申请人： Wesley Peter Blackaby ,  Jose Luis Castro Pineiro ,  Mark Stuart Chambers ,  Simon Charles Goodacre ,  David James Hallett ,  Philip Jones ,  Richard Thomas Lewis ,  Angus Murray MacLeod ,  Robert James Maxey ,  Kevin William Moore ,  Leslie Joseph Street

发明人： Wesley Peter Blackaby ,  Jose Luis Castro Pineiro ,  Mark Stuart Chambers ,  Simon Charles Goodacre ,  David James Hallett ,  Philip Jones ,  Richard Thomas Lewis ,  Angus Murray MacLeod ,  Robert James Maxey ,  Kevin William Moore ,  Leslie Joseph Street

IPC分类号： A61K31/519 ,  C07D487/04 ,  A61P25/22

CPC分类号： C07D487/04 ,  A61K31/519

摘要： A class of imidazo[1,2-α]pyrimidine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, are selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

摘要翻译： 一类由任选取代的五元或六元杂芳环在3-位上被取代的咪唑并[1,2-α]嘧啶衍生物，是GABA A A受体的选择性配体， 特别是对α2和/或α3和/或α5亚基具有良好的亲和力，因此有益于治疗和/或预防中枢神经系统的不利条件，包括焦虑，抽搐和认知障碍。

公开(公告)号：US06900215B2

公开(公告)日：2005-05-31

申请号：US10100797

申请日：2002-03-19

申请人： Mark Stuart Chambers ,  Simon Charles Goodacre ,  David James Hallett ,  Andrew Jennings ,  Philip Jones ,  Richard Thomas Lewis ,  Kevin William Moore ,  Michael Geoffrey Neil Russell ,  Leslie Joseph Street ,  Helen Jane Szekeres

发明人： Mark Stuart Chambers ,  Simon Charles Goodacre ,  David James Hallett ,  Andrew Jennings ,  Philip Jones ,  Richard Thomas Lewis ,  Kevin William Moore ,  Michael Geoffrey Neil Russell ,  Leslie Joseph Street ,  Helen Jane Szekeres

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/22

CPC分类号： C07D487/04

摘要： A class of 3-phenylimidazo[1,2-α]pyrimidine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, and further substituted on the phenyl ring by alkyl, trifluoromethyl, alkoxy or one or two halogen atoms, especially fluoro, are selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

摘要翻译： 一类3-苯基咪唑并[1,2-a]嘧啶衍生物，其在苯环的间位被被氧原子或-NH-键直接连接或桥连的任选取代的芳基或杂芳基取代， 并且在苯环上被烷基，三氟甲基，烷氧基或一个或两个卤原子，特别是氟取代，是GABA A A受体的选择性配体，特别是对α2和/或α3具有良好的亲和力 和/或其α5亚基，因此有益于治疗和/或预防中枢神经系统的不良状况，包括焦虑，抽搐和认知障碍。

公开(公告)号：US07279580B2

公开(公告)日：2007-10-09

申请号：US10512984

申请日：2003-05-23

申请人： Simon Charles Goodacre ,  David James Hallett ,  Alexander Charles Humphries ,  Philip Jones ,  Sarah Margaret Kelly ,  Kevin John Merchant ,  Kevin William Moore ,  Michael Reader

发明人： Simon Charles Goodacre ,  David James Hallett ,  Alexander Charles Humphries ,  Philip Jones ,  Sarah Margaret Kelly ,  Kevin John Merchant ,  Kevin William Moore ,  Michael Reader

IPC分类号： C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  A01N43/42 ,  A61K31/44

CPC分类号： C07D471/04

摘要： A class of 8-fluoro-3-phenylimidazo[1,2-α]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group, or by a pyrrolidinonyl group, which is directly attached or bridged by an oxygen atom or by a —NH— or —OCH2— linkage, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

摘要翻译： 一类在苯环的间位被任意取代的芳基或杂芳基取代的8-氟-3-苯基咪唑并[1,2-α]吡啶衍生物，或直接连接或桥连的吡咯烷基 由氧原子或-NH-或-OCH 2 - 键组成，是GABA A A受体的选择性配体，特别是对α2和/或 α3和/或α5亚基因此有益于治疗和/或预防中枢神经系统的不利条件，包括焦虑，抽搐和认知障碍。

公开(公告)号：US06500828B1

公开(公告)日：2002-12-31

申请号：US09890000

申请日：2001-07-23

申请人： William Robert Carling ,  Jose Luis Castro Pineiro ,  Richard Thomas Lewis ,  Kevin William Moore ,  Leslie Joseph Street

发明人： William Robert Carling ,  Jose Luis Castro Pineiro ,  Richard Thomas Lewis ,  Kevin William Moore ,  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 difluoro-or tri-fluoro-substituted phenyl ring at the 3-position, a triazolyl moiety at the 6-position, and a tert-butyl group at the 7-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are useful in the treatment of anxiety and convulsions.

摘要翻译： 在3位具有二氟或三氟取代的苯环，6位的三唑基部分和叔丁基的1,2,4-三唑并[4,3-b]哒嗪衍生物 在7位是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，并且可用于治疗焦虑和抽搐。

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：US06448249B1

公开(公告)日：2002-09-10

申请号：US09600988

申请日：2000-07-24

申请人： William Robert Carling ,  Tamara Ladduwahetty ,  Angus Murray MacLeod ,  Kevin John Merchant ,  Kevin William Moore ,  Francine Sternfeld ,  Leslie Joseph Street

发明人： William Robert Carling ,  Tamara Ladduwahetty ,  Angus Murray MacLeod ,  Kevin John Merchant ,  Kevin William Moore ,  Francine Sternfeld ,  Leslie Joseph Street

IPC分类号： A61K315025

CPC分类号： C07D487/04

摘要： A substituted triazolopyridazine derivative, its use in cognition enhancement therapy, compositions containing it and processes for its manufacture.

摘要翻译： 取代的三唑并哒嗪衍生物，其在认知增强疗法中的应用，含有其的组合物及其制备方法。

公开(公告)号：US06303597B1

公开(公告)日：2001-10-16

申请号：US09582444

申请日：2000-06-26

申请人： William Robert Carling ,  Kevin William Moore ,  Leslie Joseph Street

发明人： William Robert Carling ,  Kevin William Moore ,  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 an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position, a substituted alkoxy moiety at the 6-position, and an optionally substituted bicycloalkyl ring system at the 7-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位具有任选取代的环烷基，苯基或杂芳基取代基，6位取代的烷氧基部分和任选取代的双环烷基环系统的1,2,4-三唑并[4,3-b]哒嗪衍生物 在7位是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，可用于治疗焦虑和抽搐。

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。

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 。