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    Triazol[4,5-d] pyramidine derivatives and their use as purinergic receptor antagonists
    5.
    发明授权
    Triazol[4,5-d] pyramidine derivatives and their use as purinergic receptor antagonists 有权
    三唑[4,5-d]吡啶衍生物及其作为嘌呤能受体拮抗剂的用途

    公开(公告)号：US07589097B2

    公开(公告)日：2009-09-15

    申请号：US12003110

    申请日：2007-12-20

    申请人： Roger John Gillespie ,  Joanne Lerpiniere ,  Suneel Gaur ,  Samantha Jayne Bamford ,  Gemma Caroline Stratton ,  Stefania Leonardi ,  Scott Murray Weiss

    发明人： Roger John Gillespie ,  Joanne Lerpiniere ,  Suneel Gaur ,  Samantha Jayne Bamford ,  Gemma Caroline Stratton ,  Stefania Leonardi ,  Scott Murray Weiss

    IPC分类号： A61K31/519 ,  A61P25/16 ,  A61P9/02 ,  A61P25/02 ,  A61P25/14 ,  A61P25/18 ,  A61P25/28

    CPC分类号： C07D487/04 ,  A61K31/00 ,  A61K31/505 ,  A61K31/519 ,  A61K31/195 ,  A61K2300/00

    摘要： The use of a compound of formula (I): wherein R1 is selected from H, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, halogen, CN, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2R7 and NR4SO2R7; R2 is selected from aryl attached via an unsaturated carbon; R3 is selected from H, alkyl, COR5, CO2R7, CONR5R6, CONR4NR5R6 and SO2R7; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an NR5R6 group, R5 and R6 may be linked to form a heterocyclic group, or where R4, R5 and R6 are in a (CONR4NR5R6) group, R4 and R5 may be linked to form a heterocyclic group; and R7 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in 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, particularly wherein said disorder is a movement disorder such as Parkinson's disease or said disorder is depression, cognitive or memory impairment, acute or chronic pain, ADHD or narcolepsy, or for neuroprotection in a subject; compounds of formula (I) for use in therapy; and novel compounds of formula (I) per se.

    摘要翻译： 使用式（I）化合物：其中R1选自H，烷基，芳基，烷氧基，芳氧基，烷硫基，芳硫基，卤素，CN，NR5R6，NR4COR5，NR4CONR5R6，NR4CO2R7和NR4SO2R7; R2选自经由不饱和碳连接的芳基; R 3选自H，烷基，COR 5，CO 2 R 7，CONR 5 R 6，CONR 4 NR 5 R 6和SO 2 R 7; R 4，R 5和R 6独立地选自H，烷基和芳基或其中R 5和R 6在NR 5 R 6基团中，R 5和R 6可以连接形成杂环基，或其中R 4，R 5和R 6在（CONR 4 NR 5 R 6） 基团，R 4和R 5可以连接形成杂环基; 并且R 7选自烷基和芳基，或其药学上可接受的盐或前药，用于治疗或预防嘌呤受体，特别是腺苷受体，特别是A 2A受体阻断可能是有益的病症，特别是其中 所述障碍是运动障碍，例如帕金森病或所述障碍是抑郁症，认知障碍或记忆障碍，急性或慢性疼痛，ADHD或发作性睡病，或对受试者的神经保护; 用于治疗的式（I）化合物; 和式（I）的新化合物本身。