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31 条记录 (耗时 0.055 秒)

    Triazol[4,5-d] pyramidine derivatives and their use as purinergic receptor antagonists
    1.
    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。

    Pyrimidine compounds as purine receptor antagonist
    8.
    发明授权
    Pyrimidine compounds as purine receptor antagonist 失效
    嘧啶化合物作为嘌呤受体拮抗剂

    公开(公告)号：US07875600B2

    公开(公告)日：2011-01-25

    申请号：US10588757

    申请日：2005-02-11

    申请人： Roger John Gillespie ,  Richard Simon Todd ,  Gemma Caroline Stratton ,  Allan Michael Jordan

    发明人： Roger John Gillespie ,  Richard Simon Todd ,  Gemma Caroline Stratton ,  Allan Michael Jordan

    IPC分类号： A61K31/33 ,  C07D239/00

    CPC分类号： C07D409/14 ,  C07D401/12 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

    摘要： Compounds of formula (I); wherein R1 is H or NHZ; R2 is optionally substituted aryl or heteroaryl attached via a carbon atom; R3 is H; optionally substituted C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, or C3 C7 cycloalkyl, halogen; OH or OR, or R4 is H, optionally substituted C1-C6alkyl, C3 C6alkenyl, C3-C6alkynyl, C3-C7 cycloalkyl, aryl or heteroaryl, R5 is H or optionally substituted C1-C6alkyl, C3-C6alkenyl, C3-C6alkynyl, or C3-C7 cycloalkyl; or R4 and R5 together form a 5 or 6-membered heterocyclic ring; and R10 is optionally substituted C1-C6alkyl; are purine receptor, particularly adenosine receptor antagonists, useful for treatment of, inter alia, movement disorders such as Parkinsons disease.

    摘要翻译： 式（I）化合物; 其中R1是H或NHZ; R2是通过碳原子连接的任选取代的芳基或杂芳基; R3为H; 任选取代的C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或C 3 C7环烷基，卤素; OH或OR，或R 4是H，任选取代的C 1 -C 6烷基，C 3 -C 6烯基，C 3 -C 6炔基，C 3 -C 7环烷基，芳基或杂芳基，R 5是H或任选取代的C 1 -C 6烷基，C 3 -C 6烯基，C 3 -C 6炔基或 C3-C7环烷基; 或R4和R5一起形成5或6元杂环; 并且R 10是任选取代的C 1 -C 6烷基; 是嘌呤受体，特别是腺苷受体拮抗剂，可用于治疗尤其是运动障碍如帕金森病。

    Pyrazolo [3,4-d] pyrimidine derivatives and their use as purinergic receptor antagonists
    9.
    发明授权
    Pyrazolo [3,4-d] pyrimidine derivatives and their use as purinergic receptor antagonists 失效
    吡唑并[3,4-d]嘧啶衍生物及其作为嘌呤能受体拮抗剂的用途

    公开(公告)号：US07629349B2

    公开(公告)日：2009-12-08

    申请号：US11275525

    申请日：2006-01-12

    申请人： Roger John Gillespie ,  Joanne Lerpiniere ,  Suneel Gaur

    发明人： Roger John Gillespie ,  Joanne Lerpiniere ,  Suneel Gaur

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/16 ,  A61P25/24

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

    摘要： Pharmaceutical compositions and their uses comprising compounds of formula (I): wherein: R1 is selected from: alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR6R7, NR5COR6, NR5CONR6R7, NR5CO2R8, and NR5SO2R8; R2 is a heteroaryl attached via an unsaturated ring carbon of said heteroaryl group; R3 is selected from: H, alkyl, halogen, OR5, SR5, and NR6R7; R4 is selected from: H, acyclic alkyl, CONR6R7, CONR5NR6R7, COR6, CO2R8, and SO2R8; R5, R6, and R7 are independently selected from: H, alkyl, and aryl, or where R6 and R7 are in an NR6R7 group, R6 and R7 may be linked to form a hetero cyclic group, or where R5, R6 and R7 are in a (CONR5NR6R7) group, R5 and R6 may be linked to form a heterocyclic group; and R8 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof.

    摘要翻译： 药物组合物及其用途，包括式（I）化合物：其中：R 1选自烷基，烷氧基，芳氧基，烷硫基，芳硫基，芳基，卤素，CN，NR 6 R 7，NR 5 COR 6，NR 5 CONR 6 R 7，NR 5 CO 2 R 8和NR 5 SO 2 R 8; R2是通过所述杂芳基的不饱和环碳连接的杂芳基; R 3选自：H，烷基，卤素，OR 5，SR 5和NR 6 R 7; R 4选自：H，无环烷基，CONR 6 R 7，CONR 5 NR 6 R 7，COR 6，CO 2 R 8和SO 2 R 8; R5，R6和R7独立地选自：H，烷基和芳基，或其中R6和R7在NR6R7基团中，R6和R7可以连接形成杂环基，或其中R5，R6和R7是 在（CONR5NR6R7）基团中，R5和R6可以连接形成杂环基; 并且R 8选自烷基和芳基，或其药学上可接受的盐。

    Thieno(3,2-d)pyrimidines and furano(3,2-d)pyramidines and their use as purinergic receptor antagonists
    10.
    发明申请
    Thieno(3,2-d)pyrimidines and furano(3,2-d)pyramidines and their use as purinergic receptor antagonists 审中-公开

    公开(公告)号：US20080153820A1

    公开(公告)日：2008-06-26

    申请号：US12071577

    申请日：2008-02-22

    申请人： Roger John Gillespie ,  Joanne Lerpiniere ,  Claire Elizabeth Dawson ,  Suneel Gaur ,  Robert Mark Pratt

    发明人： Roger John Gillespie ,  Joanne Lerpiniere ,  Claire Elizabeth Dawson ,  Suneel Gaur ,  Robert Mark Pratt

    IPC分类号： A61K31/5377 ,  A61K31/519 ,  A61K31/497 ,  A61K31/496 ,  A61P25/00

    CPC分类号： C07D491/04 ,  C07D495/04

    摘要： A compound of formula (I), wherein X is S or O; R1 is selected from H, alkyl, aryl, hydroxy, alkoxy, aryloxy, thioalkyl, thioaryl, halogen, CN, COR5, CO2R5, CONR5R7, CONR5NR6R7, NR6R7, NR5CONR6R7, NR5COR6, NR5CO2R8, and NR5SO2R8; R2 is selected from aryl attached via an unsaturated carbon atom; R3 is selected from H, alkyl, hydroxy, alkoxy, halogen, CN and NO2; R3 is selected from H, alkyl, aryl, hydroxy, alkoxy, aryloxy, thioalkyl, thioaryl, halogen, CN, NO2, COR5, CO2R5, CONR6R7, CONR5NR6R7, NR6R7, NR5CONR6R7, NR5COR6, NR5CO2R8 and NR5SO2R8; R5, R6 and R7 are independently selected from H, alkyl and aryl or where R6 and R7 are in an (NR6R7) group, R6 and R7 may be linked to form a heterocyclic group, or where R5, R6 and R7 are in a (CONR5NR6R7) group, R5 and R6 may be linked to form a heterocyclic group; and R8 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, and the use thereof in therapy and 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 a Parkinson's disease or said disorder is depression, cognitive or memory impairment, acute or chronic pain, ADHD or narcolepsy, or wherein said medicament is for neuroprotection in a subject.