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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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2.
公开(公告)号:US5889008A
公开(公告)日:1999-03-30
申请号:US11308
申请日:1998-02-05
申请人: Richard Alexander Jelley , Angus Murray MacLeod , Austin John Reeve , Francine Sternfeld , Leslie Joseph Street
发明人: Richard Alexander Jelley , Angus Murray MacLeod , Austin John Reeve , Francine Sternfeld , Leslie Joseph Street
IPC分类号: C07D403/04 , A61K31/00 , A61K31/495 , A61K31/496 , A61P25/06 , A61P43/00 , C07D413/14 , C07D521/00 , C07D403/14 , C07D471/04
CPC分类号: C07D249/08 , C07D231/12 , C07D233/56
摘要: A class of 1-�3-(1H-indol-3-yl)propyl!-4-(2-phenylethyl) piperazine derivatives, substituted at the 5-position of the indole nucleus by a five-membered heteroaromatic moiety, and on the phenyl ring of the phenethyl moiety by fluoro, chloro, trifluoromethyl, alkoxy or an oxazolidinone group and optionally by one or two further substituents, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D .alpha. receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT.sub.1D .alpha. receptor subtype relative to the 5-HT.sub.1D .alpha. subtype; they are therefore usefull 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, while 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 / GB96 / 01806 Sec。 371日期:1998年2月5日 102(e)1998年2月5日PCT PCT 1996年7月29日PCT公布。 公开号WO97 / 06159 日期1997年2月20日一类1- [3-(1H-吲哚-3-基)丙基] -4-(2-苯基乙基)哌嗪衍生物,其在吲哚核的5位被五元 氟代,氯代,三氟甲基,烷氧基或恶唑烷酮基以及任选地被一个或两个另外的取代基组成的苯乙基部分的苯环是5-HT1样受体的选择性激动剂,是人类的有效激动剂 5-HT1Dα受体亚型,同时相对于5-HT1Dα亚型对5-HT1Dα受体亚型具有至少10倍的选择性亲和力; 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,同时引起更少的副作用,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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3.
公开(公告)号:US06949549B2
公开(公告)日:2005-09-27
申请号:US10333151
申请日:2001-07-13
申请人: Richard Alexander Jelley , Tamara Ladduwahetty , Angus Murray MacLeod , Andrew Madin , Francine Sternfeld
发明人: Richard Alexander Jelley , Tamara Ladduwahetty , Angus Murray MacLeod , Andrew Madin , Francine Sternfeld
IPC分类号: A61P25/28 , C07D487/04 , A61K31/5025
CPC分类号: C07D487/04
摘要: A class of substituted imidazolo[5,1-a]phthalazine derivatives as ligands for GABAA receptors of formula I which are partial or full inverse agonists of an α5 receptor subunit while being relatively free of activity at α1 and/or α2 and/or α3 receptor subunit binding sites are described herein; they are therefore of benefit as a medicament for enhancing cognition but with the reduction or elimination of proconvulsant activity.
摘要翻译: 一类取代的咪唑并[5,1-a]酞嗪衍生物作为式I的GABA A A受体的配体,其是α5受体亚基的部分或完全反向激动剂,而在α1相对没有活性 和/或α2和/或α3受体亚单位结合位点; 因此,它们作为增强认知但减少或消除促凝血活性的药物是有益的。
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公开(公告)号:US07393858B2
公开(公告)日:2008-07-01
申请号:US10548678
申请日:2004-03-04
申请人: Olivier Dirat , Jason Matthew Elliott , Ian Thomas Huscroft , Richard Alexander Jelley , Janusz Jozef Kulagowski , Piotr Antoni Raubo , Duncan Edward Shaw , Francine Sternfeld , Christopher John Swain
发明人: Olivier Dirat , Jason Matthew Elliott , Ian Thomas Huscroft , Richard Alexander Jelley , Janusz Jozef Kulagowski , Piotr Antoni Raubo , Duncan Edward Shaw , Francine Sternfeld , Christopher John Swain
IPC分类号: A61K31/438 , C07D491/10
CPC分类号: C07D405/04 , C07D405/06 , C07D407/12 , C07D417/04 , C07D491/10
摘要: The present invention relates to compounds of formula (Ia) wherein A, B, n, m, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are defined herein, and pharmaceutically acceptable salts thereof; the compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
摘要翻译: 本发明涉及式(Ia)化合物,其中A,B,n,m,R 1,R 2,R 3, R 4,R 5,R 6,R 7,R 8, 本文定义R 9,R 10和R 11和其药学上可接受的盐; 该化合物特别用于治疗或预防抑郁,焦虑,疼痛,炎症,偏头痛,呕吐或带状疱疹后神经痛。
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公开(公告)号:US07410964B2
公开(公告)日:2008-08-12
申请号:US10555034
申请日:2004-05-07
申请人: Kevin Dinnell , Karl Richard Gibson , Timothy Harrison , Richard Alexander Jelley , Alan John Nadin , Paul Joseph Oakley , Andrew Pate Owens , Duncan Edward Shaw , Brian John Williams
发明人: Kevin Dinnell , Karl Richard Gibson , Timothy Harrison , Richard Alexander Jelley , Alan John Nadin , Paul Joseph Oakley , Andrew Pate Owens , Duncan Edward Shaw , Brian John Williams
IPC分类号: C07D285/22 , A61K31/5415
CPC分类号: C07D279/02
摘要: Compounds of formula I: inhibit gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
摘要翻译: 式I化合物:抑制γ-分泌酶,因此可用于治疗或预防阿尔茨海默氏病。
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