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    Substituted 1-indolylpropyl-4-benzyl-tetrahydropyridine derivatives
    1.
    发明授权
    Substituted 1-indolylpropyl-4-benzyl-tetrahydropyridine derivatives 失效
    取代的1-吲哚基丙基-4-苄基 - 四氢吡啶衍生物

    公开(公告)号：US5994374A

    公开(公告)日：1999-11-30

    申请号：US068631

    申请日：1998-05-08

    申请人： Sylvie Bourrain ,  Angus Murray MacLeod ,  Joseph George Neduvelil ,  Graham Andrew Showell

    发明人： Sylvie Bourrain ,  Angus Murray MacLeod ,  Joseph George Neduvelil ,  Graham Andrew Showell

    IPC分类号： C07D521/00 ,  A61K31/44 ,  C07D401/14

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： A class of 1-[3-(1H-indol-3-yl)propyl]-4-benzyl-1,2,5,6-tetrahydropyridine derivatives, substituted at the 5-position of the indole nucleus by a 1,2,4-triazol-4-yl moiety, and on the methylene linkage of the benzyl moiety by an alkyl, alkoxy, or alkoxy-alkoxy substituent, 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 5HT.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.alpha. receptors is indicated, and are expected to have fewer undesirable cardiovascular and other side effects.

    摘要翻译： PCT No.PCT / GB96 / 02684。 371日期1998年5月8日 102（e）日期1998年5月8日PCT 1996年11月4日PCT PCT。 公开号WO97 / 17337 日期1997年5月15日一类在吲哚核的5-位被取代的1- [3-（1H-吲哚-3-基）丙基] -4-苄基-1,2,5,6-四氢吡啶衍生物 1,2,4-三唑-4-基部分，并且在烷基，烷氧基或烷氧基 - 烷氧基取代基上的苄基部分的亚甲基键是5-HT1样受体的选择性激动剂，其为 人类5-HT1Dα受体亚型，而对5HT1Dα受体亚型相对于5-HT1Dβ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/或预防临床症状，特别是偏头痛和相关疾病，其中指出5-HT1Dα受体的亚型选择性激动剂，并且预期具有较少的不期望的心血管和其它副作用 。

    Azetidine, pyrrolidine and piperidine derivatives as 5-HT.sub.1D receptor agonists
    2.
    发明授权
    Azetidine, pyrrolidine and piperidine derivatives as 5-HT.sub.1D receptor agonists 失效
    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。

    Piperazine, piperidine and tetrahydropyridine derivatives as 5-HT receptor agonists
    4.
    发明授权
    Piperazine, piperidine and tetrahydropyridine derivatives as 5-HT receptor agonists 失效
    哌嗪，哌啶和四氢吡啶衍生物作为5-HT受体激动剂

    公开(公告)号：US5998416A

    公开(公告)日：1999-12-07

    申请号：US171930

    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： C07D405/04 ,  C07D405/14 ,  A61K31/495 ,  A61K31/505

    CPC分类号： C07D405/04 ,  C07D405/14

    摘要： A class of N-substituted piperazine, piperidine, and tetrahydropyridine derivatives, further subltitutedat the 4-position by an optionally substituted alkenyl, alkynyl, 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.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 / GB97 / 01329 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。 出版物WO97 / 45432 PCT 日期1997年12月4日一类N-取代的哌嗪，哌啶和四氢吡啶衍生物，通过任选取代的烯基，炔基，芳基 - 烷基或杂芳基 - 烷基部分进一步在4-位上被取代为5-HT1- 作为人5-HT1Dα受体亚型的有效激动剂，同时相对于5-HT1Dβ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。

    Aminocyclohexane derivatives as 5-HT receptor agonists
    5.
    发明授权
    Aminocyclohexane derivatives as 5-HT receptor agonists 失效
    氨基环己烷衍生物作为5-HT受体激动剂

    公开(公告)号：US06211219B1

    公开(公告)日：2001-04-03

    申请号：US09214343

    申请日：1999-01-04

    申请人： Angus Murray MacLeod ,  Graham Andrew Showell ,  Leslie Joseph Street

    发明人： Angus Murray MacLeod ,  Graham Andrew Showell ,  Leslie Joseph Street

    IPC分类号： C07D40306

    CPC分类号： C07D231/12 ,  C07D209/14 ,  C07D233/56 ,  C07D249/08

    摘要： A class of substituted aminocyclohexane derivatives are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D&agr; receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT1D&agr; receptor subtype relative to the 5-HT1D&bgr; 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： 一类取代的氨基环己烷衍生物是5-HT1样受体的选择性激动剂，它是人类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， 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。

    Substituted quinoline-4-carboxylic hydrazides as NK-2/NK-3 receptor ligands
    7.
    发明授权
    Substituted quinoline-4-carboxylic hydrazides as NK-2/NK-3 receptor ligands 失效
    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。

    Isoxazole pyrazoloindane derivatives as cognition enhancing GABAA α5 subtype ligands
    8.
    发明授权
    Isoxazole pyrazoloindane derivatives as cognition enhancing GABAA α5 subtype ligands 失效
    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。