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    Compounds which potentiate glutamate receptor and uses thereof in medicine
    12.
    发明授权
    Compounds which potentiate glutamate receptor and uses thereof in medicine 失效

    公开(公告)号：US07618969B2

    公开(公告)日：2009-11-17

    申请号：US11573370

    申请日：2005-08-05

    申请人： Daniel Marcus Bradley ,  Kevin Michael Thewlis ,  Simon Edward Ward

    发明人： Daniel Marcus Bradley ,  Kevin Michael Thewlis ,  Simon Edward Ward

    IPC分类号： A61K31/44 ,  C07D213/02

    CPC分类号： C07D213/64 ,  C07D213/42 ,  C07D213/50 ,  C07D213/61 ,  C07D213/84 ,  C07D213/85 ,  C07D231/12 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D333/20

    摘要： Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; R2 and R3, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; each R4, which may be the same or different, is C1-6alkyl, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro, amino, monoC1-4alkylamino or diC1-4alkylamino; p is 0, 1 or 2; n is 1 or 2; R5 and R6, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; and Het is thienyl, pyridyl, pyrimidinyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazolyl, pyrazolyl, pyrrolyl, quinolyl, thiazolyl or furyl, each of which may be substituted by one or more groups independently selected from the list consisting of C1-6alkyl, C1-6alkoxy, acetyl, halogen, haloC1-6alkyl, cyano, nitro, amino, monoC1-4alkylamino and diC1-4alkylamino. Methods of preparation of the compounds, and uses thereof in medicine, for example treatment of schizophrenia, are also disclosed.

    COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE
    13.
    发明申请
    COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
    潜在的谷氨酸受体的化合物及其在医药中的应用

    公开(公告)号：US20090170902A1

    公开(公告)日：2009-07-02

    申请号：US12278604

    申请日：2007-02-06

    申请人： Daniele Andreotti ,  Simon Edward Ward

    发明人： Daniele Andreotti ,  Simon Edward Ward

    IPC分类号： A61K31/443 ,  C07D307/02 ,  C07D405/00 ,  A61K31/34

    CPC分类号： C07D401/10 ,  C07D307/22 ,  C07D409/10

    摘要： Compounds of formula (I), salts and solvates thereof are provided: wherein Ar is selected from phenyl, pyridyl, furanyl and thienyl, each optionally substituted with one or more groups Y; and each Y group is independently selected from the group consisting of: halo, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, cyano, C(O)C1-4alkyl, NHSO2C1-4alkyl, NMeSO2C1-4alkyl, NHCOC1-4alkyl, NMeCOC1-4alkyl, SOC1-4alkyl, SO2C1-4alkyl, and CO2C1-4alkyl, or two Y groups together form a cyclic group —O(CH2)O—. Processes for preparation, and uses thereof in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.

    摘要翻译： 提供式（I）化合物，其盐和溶剂化物：其中Ar选自苯基，吡啶基，呋喃基和噻吩基，各自任选被一个或多个Y基团取代; 并且每个Y基团独立地选自：卤素，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，氰基，C（O）C 1-4烷基，NHSO 2 C 1-4烷基，NMeSO 2 C 1-4烷基，NHCOC 1-4烷基，NMeCOC 1 - 烷基，SO1-4烷基，SO2C1-4烷基和CO2C1-4烷基，或两个Y基团一起形成环状基团-O（CH 2）O-。 还公开了制备方法及其用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症的用途。

    4-Quinolinemethanol derivatives as purine receptor antagonists (1)
    16.
    发明授权
    4-Quinolinemethanol derivatives as purine receptor antagonists (1) 失效
    嘌呤受体拮抗剂4-喹啉甲醇衍生物（1）

    公开(公告)号：US06583156B1

    公开(公告)日：2003-06-24

    申请号：US09786471

    申请日：2001-05-16

    申请人： Roger John Gillespie ,  Joanne Lerpiniere ,  Suneel Gaur ,  David Reginald Adoms ,  Lars Jacob Stray Knutsen ,  Simon Edward Ward

    发明人： Roger John Gillespie ,  Joanne Lerpiniere ,  Suneel Gaur ,  David Reginald Adoms ,  Lars Jacob Stray Knutsen ,  Simon Edward Ward

    IPC分类号： A61K3147

    CPC分类号： C07D215/38 ,  A61K31/47 ,  A61K31/4709 ,  C07D215/14 ,  C07D215/18 ,  C07D215/22 ,  C07D215/26 ,  C07D215/36 ,  C07D215/48 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06

    摘要： Use a compound of formula (I) wherein: R1 is hydrogen or alkyl; R2 and R3 are independently selected from hydrogen, alkyl, aryl and heterocyclyle or together may form a ring or R1 and R2 or R3 together may form an oxygen-containing, optionally fused ring pharmaceutically acceptable salts or prodrugs thereof, with the proviso that where R1 and R4 to R9 are hydrogen, R2 or R3 is not 3-methoxy-4-benzyloxyphenyl or 2-dimethylaminoethoxymethyl, in the manufacture of a medicament for the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial. Said disorders are neurodegenerative disorders or movement disorders selected from Parkinson's disease or progressive supernuclear palsy, Huntington's disease, multiple system atrophy, corticobasal degeneration, Wilson's disease, Hallerrorden-Spatz disease, progressive pallidal atrophy, Dopa-responsive dystonia-Parkinsonism, spasticity, Alzheimer's disease or other disorders of the basal ganglia which result in dyskinesias.

    摘要翻译： 使用式（I）的化合物，其中：R 1是氢或烷基; R2和R3独立地选自氢，烷基，芳基和杂环基，或一起可以形成环，或者R 1和R 2或R 3一起可以形成含氧的，任选稠合的药学上可接受的盐或前药，条件是其中R 1 并且R 4至R 9为氢，R 2或R 3不为3-甲氧基-4-苄氧基苯基或2-二甲基氨基乙氧基甲基，用于制备用于治疗或预防其中阻断嘌呤受体，特别是腺苷受体和 更具体地，A2A受体可能是有益的。 所述病症是选自帕金森氏病或进行性无核麻痹，亨廷顿氏病，多发性系统萎缩，皮质基底变性，威尔逊氏病，哈勒德 - 斯坦茨病，进行性苍白萎缩症，多巴反应性肌张力障碍 - 帕金森综合征，痉挛状态，阿尔茨海默病的神经变性疾病或运动障碍 或导致运动障碍的基底节神经节的其他疾病。