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    Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition
    12.
    发明授权
    Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition 失效
    氮取代的1,2,4-三唑并[3,4-a]酞嗪衍生物用于增强认知

    公开(公告)号：US06900209B2

    公开(公告)日：2005-05-31

    申请号：US10432391

    申请日：2001-11-22

    Applicant: Mark Stuart Chambers ,  Philip Jones ,  Angus Murray MacLeod ,  Robert James Maxey ,  Helen Jane Szekeres

    Inventor： Mark Stuart Chambers ,  Philip Jones ,  Angus Murray MacLeod ,  Robert James Maxey ,  Helen Jane Szekeres

    IPC: C07D487/04 ,  A61K31/5025 ,  A61P25/28

    CPC classification number: C07D487/04

    Abstract: The present invention provides a compound of formula (I) wherein A is an optionally substituted C1-4alkylidene group or a bond, R20 and R21 are hydrogen, alkyl groups or heterocyclic groups, R1 and R2 are small substituents or hydrogen, L is O, S or substituted N, X is a 5- or 6-membered heteroaromatic ring, Y is C1-4alkylidene and Z is a 5- or 6-membered heteroaromatic ring; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; its use in making medicaments for treating neurodegenerative disease and methods of using it to enhance cognition.

    Abstract translation: 本发明提供式（I）的化合物，其中A是任选取代的C 1-4烷基或键，R 20和R 21， / SO 2是氢，烷基或杂环基，R 1和R 2是小取代基或氢，L是O，S或取代的N，X是5 - 或6-元杂芳环，Y是C 1-4 - 亚烷基，Z是5-或6-元杂芳环; 或其药学上可接受的盐; 包含它的药物组合物; 其用于治疗; 其用于制备用于治疗神经退行性疾病的药物和使用其增强认知的方法。

    Substituted indolylpropyl-piperazine derivatives as 5-HT.sub.1D .alpha. agonists
    15.
    发明授权
    Substituted indolylpropyl-piperazine derivatives as 5-HT.sub.1D .alpha. agonists 失效
    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

    Applicant: Raymond Baker ,  Mark Stuart Chambers ,  Sarah Christine Hobbs ,  Angus Murray MacLeod ,  Austin John Reeve ,  Francine Sternfeld ,  Leslie Joseph Street

    Inventor： Raymond Baker ,  Mark Stuart Chambers ,  Sarah Christine Hobbs ,  Angus Murray MacLeod ,  Austin John Reeve ,  Francine Sternfeld ,  Leslie Joseph Street

    IPC: 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 classification number: C07D249/08 ,  C07D231/12 ,  C07D233/56

    Abstract: 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.

    Abstract translation: 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。

    Substituted 1,4-piperazine-heteroaryl derivatives as 5-HT.sub.1D receptor agonists
    17.
    发明授权
    Substituted 1,4-piperazine-heteroaryl derivatives as 5-HT.sub.1D receptor agonists 失效
    取代的1,4-哌嗪 - 杂芳基衍生物作为5-HT1D受体激动剂

    公开(公告)号：US5849746A

    公开(公告)日：1998-12-15

    申请号：US894302

    申请日：1997-07-22

    Applicant: Mark Stuart Chambers ,  Angus Murray MacLeod ,  Victor Giulio Matassa

    Inventor： Mark Stuart Chambers ,  Angus Murray MacLeod ,  Victor Giulio Matassa

    IPC: A61K31/495 ,  A61P9/00 ,  A61P25/04 ,  A61P43/00 ,  C07D403/14 ,  C07D413/14

    CPC classification number: C07D403/14

    Abstract: A class of 1,4-disubstituted piperazine derivatives, further substituted on one of the carbon atoms of the piperazine ring, 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, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.

    Abstract translation: PCT No.PCT / GB96 / 00179 Sec。 371日期1997年7月22日 102（e）日期1997年7月22日PCT提交1996年1月29日PCT公布。 出版物WO96 / 23785 日期1996年8月8日一类在哌嗪环的一个碳原子上进一步取代的1,4-二取代哌嗪衍生物是5-HT1样受体的选择性激动剂，是人5-HT1Dα的有效激动剂 受体亚型，而相对于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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