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    4-Quinolinemethanol derivatives as purine receptor antagonists (1)
    1.
    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。

    Compounds which potentiate glutamate receptor and uses thereof in medicine
    4.
    发明授权
    Compounds which potentiate glutamate receptor and uses thereof in medicine 失效
    增强谷氨酸受体的药物及其在药物中的应用

    公开(公告)号：US07741351B2

    公开(公告)日：2010-06-22

    申请号：US11573368

    申请日：2005-08-05

    申请人： Kevin Michael Thewlis ,  Simon Edward Ward

    发明人： Kevin Michael Thewlis ,  Simon Edward Ward

    IPC分类号： A61K31/425 ,  A61K31/40 ,  A61K31/275 ,  A61K31/17

    CPC分类号： C07D207/27 ,  C07C311/07 ,  C07C311/08 ,  C07C311/37 ,  C07C317/28 ,  C07C2602/08 ,  C07D275/02

    摘要： This case discloses compounds of formula (I) 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 or amino; each R4, which may be the same or different, is C1-6alkyl, halogen, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro or amino; p is 0, 1 or 2; each R5, which may be the same or different, is C1-6alkyl, halogen, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro or amino; q is 0, 1 or 2; R6 is —NR6aSO2R6b, —NR6aC(═O)R6b, —NR6a(C═O)N(R6c)2, —(C═O)R6d, —CH2NR6aSO2R6b, —CH2NR6aC(═O)R6b, CH2NR6a(C═O)N(R6c)2 or —CH2(C═O)R6d; where R6a and each R6c, which may be the same or different, is hydrogen or C1-6alkyl; R6b and R6d are C1-6alkyl or haloC1-6alkyl; or R6a and R6b, or R6a and R6c, together with the interconnecting atoms, may form a 5- or 6-membered ring; n is 1 or 2; and R7 and R8, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano or amino. It also discloses methods for preparing the compounds and their use in therapy such as treating schizophrenia.

    摘要翻译： 本例公开了式（I）的化合物，其中R 1是C 1-6烷基，卤代C 1-6烷基，C 2-6烯基，氨基，单C 1-4烷基氨基或二C 1-4烷基氨基; R 2和R 3可以相同或不同，是氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基或氨基; 每个R 4可以相同或不同，为C 1-6烷基，卤素，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基，硝基或氨基; p为0,1或2; 每个R 5可以相同或不同，是C 1-6烷基，卤素，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基，硝基或氨基; q是0,1或2; R6是-NR6aSO2R6b，-NR6aC（= O）R6b，-NR6a（C = O）N（R6c）2， - （C = O）R6d，-CH2NR6aSO2R6b，-CH2NR6aC（= O）R6b，CH2NR6a ）N（R6c）2或-CH2（C = O）R6d; 其中R 6a和R 6c可以相同或不同，是氢或C 1-6烷基; R6b和R6d是C1-6烷基或卤代C 1-6烷基; 或R6a和R6b或R6a和R6c与互连原子一起可以形成5-或6-元环; n为1或2; 和可以相同或不同的R 7和R 8是氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基或氨基。 它还公开了制备化合物的方法及其在诸如治疗精神分裂症的治疗中的用途。

    Compounds which potentiate glutamate receptor and uses thereof in medicine
    5.
    发明授权
    Compounds which potentiate glutamate receptor and uses thereof in medicine 失效
    增强谷氨酸受体的药物及其在药物中的应用

    公开(公告)号：US07572819B2

    公开(公告)日：2009-08-11

    申请号：US11673044

    申请日：2007-02-09

    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： A61K31/445 ,  C07D213/56

    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.

    摘要翻译： 公开了式（I）化合物或其药学上可接受的盐，溶剂合物或前体药物：其中R 1是C 1-6烷基，卤代C 1-6烷基，C 2-6烯基，氨基，单C 1-4烷基氨基或二C 1-4烷基氨基; R 2和R 3可以相同或不同，为氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基，氨基，单C 1-4烷基氨基或二C 1-4烷基氨基; 每个R 4可以相同或不同，为C 1-6烷基，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基，硝基，氨基，单C 1-4烷基氨基或二C 1-4烷基氨基; p为0,1或2; n为1或2; R 5和R 6可以相同或不同，为氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基，氨基，单C 1-4烷基氨基或二C 1-4烷基氨基; 并且Het是噻吩基，吡啶基，嘧啶基，哒嗪基，嘧啶基，吡嗪基，咪唑基，吡唑基，吡咯基，喹啉基，噻唑基或呋喃基，其各自可以被一个或多个独立地选自C 1-6烷基， 1-6烷氧基，乙酰基，卤素，卤代C 1-6烷基，氰基，硝基，氨基，单C 1-4烷基氨基和二C 1-4烷基氨基。 还公开了化合物的制备方法及其在药物中的用途，例如精神分裂症的治疗。