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1. 发明授权

US06262103B1 Thienycyclohexanone derivatives as ligands of the GABAA &agr;5 receptor subtype 失效
标题翻译：噻吩环己酮衍生物作为GABAAα5受体亚型的配体
公开(公告)号：US06262103B1
公开(公告)日：2001-07-17
申请号：US09284591
申请日：1999-04-16
申请人： Howard Barff Broughton , Mark Stewart Chambers , Sarah Christine Hobbs , Angus Murray MacLeod , Austin John Reeve
发明人： Howard Barff Broughton , Mark Stewart Chambers , Sarah Christine Hobbs , Angus Murray MacLeod , Austin John Reeve
IPC分类号： A61K314155
CPC分类号： C07D417/14 , A61K31/381 , A61K31/4025 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/4436 , A61K31/4439 , A61K31/496 , A61K31/497 , A61K31/506 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04
摘要： A pharamceutical composition comprises a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is C1-6alkyl, C2-6alkenyl, C2-6-alkynyl, C3-6-cycloalkyl, arylC1-6alkyl, aryl, S(O)pR1.
摘要翻译：药用组合物包含式（I）化合物或其药学上可接受的盐，其中A为C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基，芳基C 1-6烷基，芳基，S（O ）pR1。

2. 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。

3. 发明授权

US06355638B1 Pyrazolo[1,5-d][1,2,4] triazines for enhancing cognition 有权
标题翻译：吡唑并[1,5-d] [1,2,4]三嗪用于增强认知
公开(公告)号：US06355638B1
公开(公告)日：2002-03-12
申请号：US09717423
申请日：2000-11-21
申请人： Helen Jane Bryant , William Robert Carling , Mark Stuart Chambers , Sarah Christine Hobbs , Philip Jones , Angus Murray MacLeod
发明人： Helen Jane Bryant , William Robert Carling , Mark Stuart Chambers , Sarah Christine Hobbs , Philip Jones , Angus Murray MacLeod
IPC分类号： C07D48714
CPC分类号： C07D487/04
摘要： Compounds according to Formula (I) or a salt thereof are GABA-A Alpha 5 ligands useful for enhancing cognition:
摘要翻译：根据式（I）的化合物或其盐是可用于增强认知的GABA-Aα5配体：

4. 发明授权

US5973156A Piperidine and tetrahydropyridine derivatives 失效
标题翻译：哌啶和四氢吡啶衍生物
公开(公告)号：US5973156A
公开(公告)日：1999-10-26
申请号：US68723
申请日：1998-05-13
申请人： Mark Stuart Chambers , Sarah Christine Hobbs , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant
发明人： Mark Stuart Chambers , Sarah Christine Hobbs , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant
IPC分类号： C07D401/06 , C07D413/14 , C07D521/00 , C07D401/14 , A61K31/445 , C07D409/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D413/14
摘要： A class of substituted piperidine and tetrahydropyridine derivatives, linked through the 4-position thereof via an alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 1-position by an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl-alkyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.spsb..alpha. receptor subtype whilst processing at least a 10-fold selective affinity for the 5-HT.sub.1D.spsb..alpha. receptor subtype relative to the 5-HT.sub.1D.spsb..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 / 02795 Sec。 371日期1998年5月13日 102（e）日期1998年5月13日PCT 1996年11月14日PCT PCT。公开号WO97 / 19073 日期1997年5月29日一类取代的哌啶和四氢吡啶衍生物，其通过其4-位通过亚烷基链连接到稠合的双环杂芳族部分如吲哚基，并且在1位被进一步被任选取代的烷基，烯基，炔基，环烷基 - 烷基，芳基 - 烷基或杂芳基 - 烷基部分是5-HT1样受体的选择性激动剂，其是人类5-HT1Dα受体亚型的有效激动剂，同时处理至少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。

5. 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。

6. 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。

7. 发明授权

US06946461B2 Imidazolophthalazine derivatives as ligands for GABAA receptors 失效
标题翻译：咪唑并恶嗪衍生物作为GABA A受体的配体
公开(公告)号：US06946461B2
公开(公告)日：2005-09-20
申请号：US10333153
申请日：2001-07-13
申请人： William Robert Carling , Tamara Ladduwahetty , Angus Murray MacLeod , Austin John Reeve , Francine Sternfeld
发明人： William Robert Carling , Tamara Ladduwahetty , Angus Murray MacLeod , Austin John Reeve , Francine Sternfeld
IPC分类号： A61P25/28 , C07D487/04 , A61K31/5025 , A61K31/5377
CPC分类号： C07D487/04
摘要： A class of substituted imadazolo[2,1-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[2,1-a]酞嗪衍生物作为式I的GABA A A受体的配体：它们是α5受体亚单位的部分或完全反向激动剂，同时相对没有活性本文描述了α1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。

8. 发明授权

US07482457B2 Substituted quinoline-4-carboxylic hydrazides as NK-2/NK-3 receptor ligands 失效
标题翻译：取代的喹啉-4-羧酸酰肼作为NK-2 / NK-3受体配体
公开(公告)号：US07482457B2
公开(公告)日：2009-01-27
申请号：US10544440
申请日：2004-02-03
申请人： Mark Stuart Chambers , Philip Jones , Angus Murray MacLeod
发明人： Mark Stuart Chambers , Philip Jones , Angus Murray MacLeod
IPC分类号： C07D215/38
CPC分类号： C07D215/52
摘要： The present invention discloses a compound of formula (I): wherein: R1 is an aryl or heteroaryl ring; R2 is hydroxy, C1-6 alkoxy, C1-6 alkyl, amino, NR′R″ or C1-6 alkyl-NR′R″ where R′ and R″ are independently chosen from hydrogen and C1-4 alkyl and where R′ and R″, together with the nitrogen atom to which they are attached, form a saturated nitrogen-containing 3-7 membered heterocycle optionally containing a further nitrogen atom and optionally substituted by NR′R″ as defined above or R2 is C1-6 alkoxy substituted by NR′R″ as defined above; R3 is hydrogen or C1-6 alkyl; R4 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl or aryl C1-6 alkyl; R5 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl, aryl C1-6 alkyl or C1-6 alkoxycarbonyl; or R4 and R5, together with the nitrogen atom to which they are attached, form a C3-C10 mono- or bicyclic saturated ring; X and Y are independently chosen from hydrogen, hydroxy, nitro, amino, cyano, CF3, halogen and C1-4 alkyl; or a pharmaceutically acceptable salt thereof; as NK-2/NK-3 ligands for treating schizophrenia, COPD, asthma or irritable bowel syndrome.
摘要翻译：本发明公开了式（I）的化合物：其中：R1是芳基或杂芳基环; R 2是羟基，C 1-6烷氧基，C 1-6烷基，氨基，NR'R“或C 1-6烷基-NR'R”，其中R'和R“独立地选自氢和C 1-4烷基，其中R'和R“与它们所连接的氮原子一起形成任选含有另外的氮原子并且任选地被如上所定义的NR'R”取代的饱和含氮3-7元杂环或R2 是由如上定义的NR'R“取代的C 1-6烷氧基; R3是氢或C1-6烷基; R4是氢，C1-8烷基，C2-8烯基，C2-8炔基，C3-8环烷基，芳基或芳基C1-6烷基; R5是氢，C1-8烷基，C2-8烯基，C2-8炔基，C3-8环烷基，芳基，芳基C1-6烷基或C1-6烷氧基羰基; 或R 4和R 5与它们所连接的氮原子一起形成C 3 -C 10单环或双环饱和环; X和Y独立地选自氢，羟基，硝基，氨基，氰基，CF 3，卤素和C 1-4烷基; 或其药学上可接受的盐; 作为用于治疗精神分裂症，COPD，哮喘或肠易激综合征的NK-2 / NK-3配体。

9. 发明授权

US07060710B2 Isoxazole pyrazoloindane derivatives as cognition enhancing GABAA α5 subtype ligands 失效
标题翻译：异恶唑吡唑并林衍生物作为增强GABAAα5亚型配体的认知
公开(公告)号：US07060710B2
公开(公告)日：2006-06-13
申请号：US10301901
申请日：2002-11-22
申请人： Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Francine Sternfeld
发明人： Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Francine Sternfeld
IPC分类号： C07D261/08 , C07D413/14 , C07D471/04 , A61K31/422 , A61K31/4418
CPC分类号： C07D413/14 , C07D413/04
摘要： The present invention provides compounds of formula I: in which: one of X and Y is a nitrogen atom substituted by a group R6′ and the other is a carbon atom substituted by an isoxazole group substituted on its carbon atoms by groups R3 and R4;one of R6 and R6′ is hydrogen;either all of W1, W2, W3 and W4 are carbon or one of W1, W2, W3 and W4 is nitrogen and the rest are carbon;and R1 and R2 are, independently, a small group, heteroaromatic ring or a 4–7 membered cyclic amine ring; processes for making them; pharmaceutical composition containing them; their use in therapy, particularly for enhancing cognition in conditions such as Alzheimer's Disease; and methods of treatment using them.
摘要翻译：本发明提供式I化合物：其中：X和Y之一是被基团R 6'取代的氮原子，另一个是被其上取代的异恶唑基团取代的碳原子通过R 3和R 4基团的碳原子; R 6和R 6之一是氢; W 1，W 2，W 3和W 4中的全部是碳或W SUP中的一个 W 1，W 2，W 3和W 4是氮，其余是碳; R 1和R 2独立地是小组杂芳族环或4-7元环胺环; 制作过程; 含有它们的药物组合物; 它们在治疗中的用途，特别是用于增强诸如阿尔茨海默氏病等疾病的认知; 和使用它们的治疗方法。

10. 发明授权

US6127388A Azetidine, pyrrolidine and piperidine derivatives as 5-HT.sub.1D receptor agonists 失效
标题翻译：氮杂环丁烷，吡咯烷和哌啶衍生物作为5-HT1D受体激动剂
公开(公告)号：US6127388A
公开(公告)日：2000-10-03
申请号：US171929
申请日：1998-10-26
申请人： Sylvie Bourrain , Angus Murray MacLeod , Graham Andrew Showell , Leslie Joseph Street
发明人： Sylvie Bourrain , Angus Murray MacLeod , Graham Andrew Showell , Leslie Joseph Street
IPC分类号： A61P25/06 , C07D405/14 , A61K31/443
CPC分类号： C07D405/14
摘要： A class of substituted azetidine, pyrrolidine and piperidine derivatives of Formula I 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. ##STR1##
摘要翻译： PCT No.PCT / GB97 / 01330 Sec。 371日期：1998年10月26日 102（e）日期1998年10月26日PCT提交1997年5月15日PCT公布。公开号WO97 / 45426 PCT 日期1997年12月4日一类式I的取代的氮杂环丁烷，吡咯烷和哌啶衍生物是5-HT1样受体的选择性激动剂，是人类5-HT1Dα受体亚型的有效激动剂，同时具有至少10倍的选择性相对于5-HT1Dβ亚型的5-HT1Dα受体亚型的亲和力; 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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