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12 条记录 (耗时 0.013 秒)

    4-QUINOLINEMETHANOL DERIVATIVES AS PURINE RECEPTOR ANTAGONISTS.(II)
    9.
    发明申请
    4-QUINOLINEMETHANOL DERIVATIVES AS PURINE RECEPTOR ANTAGONISTS.(II) 审中-公开
    （II）作为嘌呤受体拮抗剂的4-喹啉甲醇衍生物

    公开(公告)号：WO0013682A3

    公开(公告)日：2000-06-02

    申请号：PCT/GB9902924

    申请日：1999-09-03

    申请人： CEREBRUS PHARM LTD ,  GILLESPIE ROGER JOHN ,  LERPINIERE JOANNE ,  GILES PAUL RICHARD ,  ADAMS DAVID REGINALD ,  KNUTSEN LARS JACOB STRAY ,  CLIFFE IAN ANTHONY

    发明人： GILLESPIE ROGER JOHN ,  LERPINIERE JOANNE ,  GILES PAUL RICHARD ,  ADAMS DAVID REGINALD ,  KNUTSEN LARS JACOB STRAY ,  CLIFFE IAN ANTHONY

    IPC分类号： A61K31/47 ,  A61P25/16 ,  A61P25/24

    CPC分类号： A61K31/47

    摘要： Wherein: R1 is hydrogen or alkyl; R2 is selected from hydrogen, alkyl, aryl and 4,5,6,7 or 8 membered satured and partially unsaturated heterocyclic rings containing one or more heteroatoms selected from O, S and N; R3 and R4 are independently selected from hydrogen, alkyl, aryl, COR13, CO2R13, CONR13R14, CONR13NR14R15, SO2R13, SO2NR13R14, SO2NR13NR14R15 or may form a ring. Or R1 and R4 together may form a heterocyclic ring or R2 and R3 together may form a heterocyclic ring. R5 and R6 are independently selected from hydrogen, alkyl, aryl and heterocyclic with the proviso that where R3 and R5 together form a ring, then R3, and R4 do not also form a ring; or a pharmaceutically acceptable salt or prodrug thereof, 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, such as a movement disorder, for example, Parkinson's Disease or progressive supernuclear palsy, Huntingtons disease, multiple system atrophy, corticobasal degeneration, Wilsons disease, Hallerrorder-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： 其中：R1为氢或烷基; R2选自氢，含有一个或多个选自O，S和N的杂原子的烷基，芳基和4,5,6,7或8元饱和和部分不饱和的杂环; R3和R4独立地选自氢，烷基，芳基，COR13，CO2R13，CONR13R14，CONR13NR14R15，SO2R13，SO2NR13R14，SO2NR13NR14R15或可以形成环。 或者R1和R4一起可以形成杂环，或者R2和R3可以一起形成杂环。 R5和R6独立地选自氢，烷基，芳基和杂环，条件是当R3和R5一起形成环时，则R3和R4也不形成环; 或其药学上可接受的盐或前药在制备用于治疗或预防其中阻断嘌呤受体，特别是腺苷受体，更特别是A 2A受体可能是有益的病症例如运动障碍的药物中的用途， 例如帕金森氏病或进行性超核麻痹，亨廷顿病，多系统萎缩，皮质基底节变性，Wilsons病，Hallerrorder-Spatz病，进行性苍白球性萎缩，多巴反应性肌张力障碍 - 帕金森综合征，痉挛状态，阿尔茨海默病或其他基底节病 导致运动障碍。

    CHEMICAL COMPOUNDS, THEIR PREPARATION AND USE
    10.
    发明申请
    CHEMICAL COMPOUNDS, THEIR PREPARATION AND USE 审中-公开
    化学化合物，其制备和使用

    公开(公告)号：WO1995007921A1

    公开(公告)日：1995-03-23

    申请号：PCT/DK1994000344

    申请日：1994-09-15

    申请人： NOVO NORDISK A/S ,  LAU, Jesper ,  KNUTSEN, Lars, Jacob, Stray

    发明人： NOVO NORDISK A/S

    IPC分类号： C07H19/16

    CPC分类号： C07H19/16

    摘要： A compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein X is halogen, amino, perhalomethyl, cyano, C1-6-alkoxy, C1-6-alkylthio or C1-6-alkylamino; A is methyl, halomethyl, cyanomethyl, aminomethyl, vinyl, methylthiomethyl or methoxymethyl; R is selected from optionally substituted N-bonded heterocyclics. The compounds have been found useful for treating central nervous system ailments.

    摘要翻译： 式（I）化合物或其药学上可接受的盐，其中X为卤素，氨基，全卤代甲基，氰基，C 1-6 - 烷氧基，C 1-6 - 烷硫基或C 1-6 - 烷基氨基; A是甲基，卤代甲基，氰基甲基，氨基甲基，乙烯基，甲硫基甲基或甲氧基甲基; R 1选自任选取代的N-键合杂环。 已经发现这些化合物可用于治疗中枢神经系统疾病。