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    Tetrahydroindolone derivatives as gabaaalpha5 ligands for enhancing cognition
    3.
    发明授权
    Tetrahydroindolone derivatives as gabaaalpha5 ligands for enhancing cognition 失效
    四氢吲哚酮衍生物作为增加认知的gabaaalpha5配体

    公开(公告)号：US06395766B1

    公开(公告)日：2002-05-28

    申请号：US09674740

    申请日：2000-11-06

    申请人： Howard Barff Broughton ,  Helen Jane Bryant ,  Mark Stuart Chambers ,  Neil Roy Curtis

    发明人： Howard Barff Broughton ,  Helen Jane Bryant ,  Mark Stuart Chambers ,  Neil Roy Curtis

    IPC分类号： A61K31404

    CPC分类号： C07D401/04 ,  A61K31/40 ,  C07D209/08 ,  C07D401/14 ,  C07D403/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

    摘要： Compounds according to Formula (I) or a pharmaceutically acceptable salt thereof are GABA-A Alpha 5 ligands useful for enhancing cognition: where A is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, arylC1-6alkyl, or aryl wherein the aryl group is optionally substituted by halogen, C1-6alkyl, CF3, CN, NO2 or NH2, NR1R10, S(O)pR1, heteroarylC1-6alkyl or heteroaryl where heteroaryl is a 5- or 6-membered heteroaromatic ring as defined for B; and B is phenyl or a 5-membered ring having one or two unsaturations containing 1, 2, 3, or 4 heteroatoms chosen from O, N and S provided that not more than one heteroatom is other than N, a 6-membered heteroaromatic ring containing 1, 2, 3 or 4 nitrogen atoms, each of which rings is optionally substituted by one or more substituents.

    摘要翻译： 根据式（I）的化合物或其药学上可接受的盐是可用于增强认知的GABA-Aα5配体：其中A是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烷基或芳基 其中芳基任选被卤素，C 1-6烷基，CF 3，CN，NO 2或NH 2，NR 1 R 10，S（O）p R 1，杂芳基C 1-6烷基或杂芳基取代，其中杂芳基是5-或6-元杂芳环， B; 并且B是苯基或具有1或2个不饱和基团的5元环，其含有1,2,3或4个选自O，N和S的杂原子，条件是不超过一个杂原子不是N，6元杂芳环 含有1,2,3或4个氮原子，其中每个环任选被一个或多个取代基取代。

    Pyrrolo-pyridine derivatives
    6.
    发明授权
    Pyrrolo-pyridine derivatives 失效
    吡咯并吡啶衍生物

    公开(公告)号：US5712285A

    公开(公告)日：1998-01-27

    申请号：US626099

    申请日：1996-04-03

    申请人： Neil Roy Curtis ,  Janusz Jozef Kulagowski ,  Paul David Leeson ,  Mark Peter Ridgill

    发明人： Neil Roy Curtis ,  Janusz Jozef Kulagowski ,  Paul David Leeson ,  Mark Peter Ridgill

    IPC分类号： C07D471/04 ,  A61K31/435

    CPC分类号： C07D471/04

    摘要： A class of pyrrolo�2,3 -b!pyridine derivatives, linked via the 3-position thereof by a methylene group to a tetrahydropyridinyl moiety, the latter moiety being substituted in turn by an aryl- or heteroaryl-substituted divalent monocyclic radical, are ligands for dopamine receptorsubtypes within the body, in particular the D.sub.4 subtype, and are accordingly of use in the treatment and/or prevention of disorders of the dopamine system, including schizophrenia and depression.

    摘要翻译： 通过其3-位通过亚甲基连接到四氢吡啶基部分的一类吡咯并[2,3-b]吡啶衍生物，后一部分依次被芳基或杂芳基取代的二价单环基取代， 体内多巴胺受体亚型的配体，特别是D4亚型，因此用于治疗和/或预防多巴胺系统疾病，包括精神分裂症和抑郁症。

    Azabicyclic ether derivatives and their use as therapeutic agents
    7.
    发明授权
    Azabicyclic ether derivatives and their use as therapeutic agents 失效
    偶氮二环醚衍生物及其作为治疗剂的用途

    公开(公告)号：US06727249B2

    公开(公告)日：2004-04-27

    申请号：US10113117

    申请日：2002-04-01

    申请人： Neil Roy Curtis ,  Ian Thomas Huscroft ,  Janusz Jozef Kulagowski ,  Piotr Antoni Raubo

    发明人： Neil Roy Curtis ,  Ian Thomas Huscroft ,  Janusz Jozef Kulagowski ,  Piotr Antoni Raubo

    IPC分类号： A61K31535

    CPC分类号： C07D451/02

    摘要： The present invention relates compounds of the formula (I): wherein X represents hydrogen, C1-4alkyl optionally substituted by a hydroxy, methoxy or benzyloxy group, or CO2(C1-2alkyl); Z is —CR9R10CH2— or —CH2CR9R10—; and R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.

    摘要翻译： 本发明涉及式（I）化合物：其中X代表氢，任选被羟基，甲氧基或苄氧基取代的C 1-4烷基或CO 2（C 1-2烷基）; Z是-CR 9 R 10 CH - 或-CH 2 CR 9 R 10 - ，R 1，R 2，R 3，R 4，R 5和R 6如本文所定义。化合物 特别用于治疗或预防抑郁，焦虑，疼痛，炎症，迁移物，呕吐或带状疱疹后神经痛。