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    4-quinolinemethanol derivatives as purine receptor antagonists (II)
    2.
    发明授权
    4-quinolinemethanol derivatives as purine receptor antagonists (II) 失效
    4-喹啉甲醇衍生物作为嘌呤受体拮抗剂（II）

    公开(公告)号：US06608085B1

    公开(公告)日：2003-08-19

    申请号：US09786472

    申请日：2001-05-09

    申请人： Roger John Gillespie ,  Joanne Lerpiniere ,  Paul Richard Giles ,  David Reginald Adams ,  Lars Jacob Stray Knutsen ,  Ian Anthony Cliffe

    发明人： Roger John Gillespie ,  Joanne Lerpiniere ,  Paul Richard Giles ,  David Reginald Adams ,  Lars Jacob Stray Knutsen ,  Ian Anthony Cliffe

    IPC分类号： A61K314709

    CPC分类号： A61K31/47

    摘要： Use of a compound of formula (I) as defined herein, 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 supemuclear 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： 本文定义的式（I）化合物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，尤其是腺苷受体的病症的药物中的用途 A2a受体可能是有益的，例如运动障碍，例如帕金森氏病或进行性超核性麻痹，亨廷顿病，多系统萎缩，皮质基底变性，威尔逊病，哈勒勒斯特氏病，进行性苍白萎缩，多巴反应性肌张力障碍 - 帕金森综合征，痉挛性，阿尔茨海默病或基底神经节的其他障碍，导致运动障碍。

    Indole derivatives process for their preparation, pharmaceutical compositions containing them and their medicinal application
    10.
    发明授权
    Indole derivatives process for their preparation, pharmaceutical compositions containing them and their medicinal application 失效
    吲哚衍生物制备方法，含有它们的药物组合物及其药物应用

    公开(公告)号：US06706750B1

    公开(公告)日：2004-03-16

    申请号：US10009568

    申请日：2002-03-11

    申请人： Jonathan Mark Bentley ,  Jonathan Richard Anthony Roffey ,  James Edward Paul Davidson ,  Howard Langham Mansell ,  Richard John Hamlyn ,  Ian Anthony Cliffe ,  David Reginald Adams ,  Nathaniel Julius Monck

    发明人： Jonathan Mark Bentley ,  Jonathan Richard Anthony Roffey ,  James Edward Paul Davidson ,  Howard Langham Mansell ,  Richard John Hamlyn ,  Ian Anthony Cliffe ,  David Reginald Adams ,  Nathaniel Julius Monck

    IPC分类号： A61K3140

    CPC分类号： C07D495/04 ,  C07D209/94

    摘要： A chemical compound of formula (I) wherein: R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4, R6 and R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsufoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; R5 is selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; A is a 5- or 6-membered partially unsaturated or aromatic heterocyclic ring or a 5- or 6-membered partially unsaturated carbocyclic ring, wherein if A is a 6-membered partially unsaturated carbocyclic ring then at least one of R4 to R7 is other than hydrogen, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof, and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinial disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

    摘要翻译： 式（I）的化合物，其中：R 1和R 2独立地选自氢和烷基; R3是烷基; R4，R6和R7独立地选自氢，卤素，羟基，烷基，芳基，氨基，烷基氨基，二烷基氨基，烷氧基，芳氧基，烷硫基，烷基磺酰基，烷基磺酰基，硝基，腈，碳 - 烷氧基，碳 - 芳氧基和羧基; R5选自氢，卤素，羟基，烷基，芳基，氨基，烷基氨基，二烷基氨基，烷氧基，芳氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，硝基，腈，碳 - 烷氧基，碳 - 芳氧基和羧基; A是5或6元部分不饱和或芳族杂环或5或6元部分不饱和碳环，其中如果A是6元部分不饱和的碳环，则R 4至R 7中的至少一个 >不是氢，和其药学上可接受的盐，加成化合物和前药，以及其在治疗中的用途，特别是作为5HT受体，特别是5HT 2C受体的激动剂或拮抗剂，例如用于治疗中枢性疾病 神经系统; 损害中枢神经系统; 心血管疾病; 胃肠疾病; 尿崩症和睡眠呼吸暂停，特别是用于治疗肥胖。