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1. 发明授权

US5981529A Substituted indolylpropyl-piperazine derivatives as 5-HT.sub.1D .alpha. agonists 失效
标题翻译：取代的吲哚基丙基哌嗪衍生物作为5-HT1Dα激动剂
公开(公告)号：US5981529A
公开(公告)日：1999-11-09
申请号：US043440
申请日：1998-03-18
申请人： Raymond Baker , Mark Stuart Chambers , Sarah Christine Hobbs , Angus Murray MacLeod , Austin John Reeve , Francine Sternfeld , Leslie Joseph Street
发明人： Raymond Baker , Mark Stuart Chambers , Sarah Christine Hobbs , Angus Murray MacLeod , Austin John Reeve , Francine Sternfeld , Leslie Joseph Street
IPC分类号： C07D403/04 , A61K31/00 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4178 , A61K31/4196 , A61P25/06 , A61P43/00 , C07D403/06 , C07D521/00 , A61K31/495 , C07D403/14 , C07D413/14
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, on one or other of the ethylene carbon atoms of the phenethyl moiety by halogen, trifluoromethyl, alkyl, hydroxyalkyl or alkoxyalkyl, and optionally on the phenyl ring of the phenethyl moiety by halogen, 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 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 / GB96 / 02309 Sec。 371日期1998年3月18日 102（e）1998年3月18日PCT PCT 1996年9月19日PCT公布。公开号WO97 / 11695 日期1997年4月3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-位被五元三氟甲基，烷基，羟基烷基或烷氧基烷基，以及任选地在苯乙基部分的苯环上被卤素，三氟甲基，烷氧基或恶唑烷酮基团任选地在苯乙基部分的一个或另外的乙烯碳原子上，一个或两个另外的取代基是5-HT1样受体的选择性激动剂，是人类5-HT1Dα受体亚型的有效激动剂，同时对5-HT1Dα受体亚型具有至少10倍的选择性亲和力 5-HT1D beta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。

2. 发明授权

US5854268A Azetidine, pyrrolidine and piperidine derivatives 失效
标题翻译：氮杂环丁烷，吡咯烷，哌啶衍生物
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。

3. 发明授权

US06465462B1 Substituted triazolo pyridazine derivatives as inverse agonists of the GABAA&agr;5 receptor subtype 失效
标题翻译：取代的三唑并哒嗪衍生物作为GABAAα5受体亚型的反向激动剂
公开(公告)号：US06465462B1
公开(公告)日：2002-10-15
申请号：US09214882
申请日：1999-01-14
申请人： William Robert Carling , Angus Murray MacLeod , Ruth McKernan , Austin John Reeve , Francine Sternfeld , Leslie Joseph Street
发明人： William Robert Carling , Angus Murray MacLeod , Ruth McKernan , Austin John Reeve , Francine Sternfeld , Leslie Joseph Street
IPC分类号： A61K31502
CPC分类号： C07D487/04 , C07D487/08
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof are useful in enhancing cognition.
摘要翻译：式（I）化合物或其药学上可接受的盐可用于增强认知。

4. 发明授权

US5889008A Substituted 1-indolylpropyl-4-phenethylpiperazadine derivatives 失效
标题翻译：取代的1-吲哚丙基-4-苯乙基哌嗪衍生物
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。

5. 发明授权

US5807857A Piperazine, piperidine and tetrahydropyridine derivative of indol-3-alkyl as 5-HT.sub.1D-.alpha. agonists 失效
标题翻译：吲哚-3-烷基的哌嗪，哌啶和四氢吡啶衍生物作为5-HT1D-α激动剂
公开(公告)号：US5807857A
公开(公告)日：1998-09-15
申请号：US737769
申请日：1996-11-15
申请人： Jose Luis Castro Pineiro , Mark Stuart Chambers , Sarah Christine Hobbs , Austin John Reeve , Graham Andrew Showell , Leslie Joseph Street , Victor Giulio Matassa
发明人： Jose Luis Castro Pineiro , Mark Stuart Chambers , Sarah Christine Hobbs , Austin John Reeve , Graham Andrew Showell , Leslie Joseph Street , Victor Giulio Matassa
IPC分类号： C07D401/14 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/495 , A61P9/00 , A61P25/04 , A61P25/06 , A61P43/00 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D471/04
摘要： Compounds of formula (I), or a salt or prodrug thereof, wherein Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; E represents a chemical bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; Q represents a straight or branched alkylene chain containing from 1 to 6 carbon atoms, optionally substituted in any position by a hydroxy group; T represents nitrogen or CH; U represents nitrogen or C--R.sup.2 ; V represents oxygen, sulphur or N--R.sup.3 ; --F--G-- represents --CH2--N--, --CH2--CH-- or --CH.dbd.C--; R.sup.1 represents C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, aryl(C.sub.1-6)alkyl or heteroaryl(C.sub.1-6)alkyl, any of which groups may be optionally substituted; and R.sup.2 and R.sup.3 independently represent hydrogen or C.sub.1-6 alkyl are selective agonists of 5-HT1D receptors, being potent agonists of the human 5-HT1Dalpha receptor subtype, while possessing at least a 10-fold selective affinity for the 5-HT1Dalpha receptor subtype, relative to the 5-HT1Dbeta 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-HT1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.
摘要翻译： PCT No.PCT / GB95 / 01129 Sec。 371日期1996年11月15日 102（e）日期1996年11月15日PCT提交1995年5月18日PCT公布。公开号WO95 / 32196 （I）式（I）化合物或其盐或前药，其中Z表示选自呋喃，噻吩，吡咯，恶唑，噻唑，异恶唑的任选取代的五元杂芳环，异噻唑，咪唑，吡唑，恶二唑，噻二唑，三唑和四唑; E表示化学键或含有1至4个碳原子的直链或支链亚烷基链; Q表示任选被羟基取代的含有1至6个碳原子的直链或支链亚烷基链; T表示氮或CH; U表示氮或C-R2; V表示氧，硫或N-R3; -F-G-表示-CH 2 -N，-CH 2 -CH-或-CH = C-; R 1表示C 3-6烯基，C 3-6炔基，芳基（C 1-6）烷基或杂芳基（C 1-6）烷基，其中任何基团可以任选被取代; 并且R 2和R 3独立地表示氢或C 1-6烷基是5-HT1D受体的选择性激动剂，它是人5-HT1Dalpha受体亚型的有效激动剂，同时对5-HT1Dalpha受体亚型具有至少10倍的选择性亲和力，相对于5-HT1Dbeta亚型; 因此，它们可用于治疗和/或预防临床症状，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。

6. 发明授权

US06448249B1 Substituted 1,2,4-triazolo[3,4-A]phthalazine derivatives as GABA&agr;5 ligands 失效
标题翻译：取代的1,2,4-三唑并[3,4-A]酞嗪衍生物作为GABAalpha5配体
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。

7. 发明授权

US06310203B1 Precursor compounds to substituted 1,2,4-triazolo[3,4,-a]phathalazine GABA alpha 5 ligands 失效
标题翻译：前体化合物与取代的1,2,4-三唑并[3,4，a]哌嗪嗪GABAα5配体
公开(公告)号：US06310203B1
公开(公告)日：2001-10-30
申请号：US09547216
申请日：2000-04-11
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： C07D48704
CPC分类号： C07D487/04
摘要： Substituted 1,2,4-Triazolo[3,4-A]phthalazine derivatives that are GABA Alpha 5 ligands are prepared from compounds represented by the formula: in which R1 is hydrogen, halogen, CF3, OCF3, CN or an optionally substituted C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy group; R2 is hydrogen, halogen, CF3, OCF3, CN or an optionally substituted C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy group; Z is an optionally substituted 5-membered or 6-membered heteroaromatic ring; and G is a leaving group.
摘要翻译：作为GABAα5配体的取代的1,2,4-三唑并[3,4-A]酞嗪衍生物由下式表示的化合物制备：其中R 1是氢，卤素，CF 3，OCF 3，CN或任选取代的C 1 C4烷基，C2-4烯基，C2-4炔基，C1-4烷氧基，C2-4链烯氧基或C2-4炔基氧基; R 2是氢，卤素，CF 3，OCF 3，CN或任选取代的C 1-4烷基，C 2-4烯基，C 2-4炔基，C 1-4烷氧基，C 2-4链烯氧基或C 2-4烷氧基; Z是任选取代的5元或6元杂芳环; G是离职团体。

8. 发明授权

US06200975B1 Substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives as GABA alpha 5 ligands 有权
标题翻译：取代的1,2,4-三唑并[3,4-a]酞嗪衍生物作为GABAα5配体
公开(公告)号：US06200975B1
公开(公告)日：2001-03-13
申请号：US09180623
申请日：1998-11-12
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： Substituted 1,2,4-Triazolo[3,4-A]phthalazine derivatives are GABA Alpha 5 ligands and are represented by the formula
摘要翻译：取代的1,2,4-三唑并[3,4-A]酞嗪衍生物是GABAα5配体，由下式表示

9. 发明授权

US07030128B2 Imidazo-pyrimidine derivatives as ligands for GABA receptors 失效
标题翻译：咪唑并嘧啶衍生物作为GABA受体的配体
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。

10. 发明授权

US5998415A Bicyclic heteroaryl-alkylene-(homo)piperazinones and thione analogues thereof, their preparation, and their use of as selective agonists of 5-HT.sub.1 -like receptors 失效
标题翻译：双环杂芳基 - 亚烷基 - （同）哌嗪酮及其硫酮类似物，其制备及其作为5-HT1样受体选择性激动剂的用途
公开(公告)号：US5998415A
公开(公告)日：1999-12-07
申请号：US065020
申请日：1998-04-17
申请人： Mark Stuart Chambers , Sarah Christine Hobbs , Leslie Joseph Street
发明人： Mark Stuart Chambers , Sarah Christine Hobbs , Leslie Joseph Street
IPC分类号： C07D403/06 , C07D521/00 , A61K31/495 , C07D403/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D403/06
摘要： A class of piperazinones, homopiperazinones and thione analogues thereof, substituted at the 1-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, and linked at the 4-position via an alkylene spacer to a fused bicyclic heteroaromatic moiety, typically indolyl, 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.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, 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 / 02624。 371日期：1998年4月17日 102（e）1998年4月17日PCT PCT 1996年10月28日PCT公布。公开号WO97 / 16446 日期1997年5月9日一类哌嗪酮，高哌嗪酮和其硫酮类似物在1位被任选取代的烯基，炔基，芳基 - 烷基或杂芳基 - 烷基部分取代，并通过亚烷基间隔基在4-位连接至稠合双环杂芳族部分，通常为吲哚基，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，同时对5-HT1Dα受体亚型具有至少10倍的选择性亲和力相对于5-HT1Dβ亚型; 因此，它们可用于治疗和/或预防临床症状，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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