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    [1,2,4]-Triazole bicyclic adenosine A2a receptor antagonists
    2.
    发明授权
    [1,2,4]-Triazole bicyclic adenosine A2a receptor antagonists 有权
    [1,2,4] - 三唑双环腺苷A2a受体拮抗剂

    公开(公告)号：US07078408B2

    公开(公告)日：2006-07-18

    申请号：US10973642

    申请日：2004-10-26

    申请人： Bernard R. Neustadt ,  Hong Liu

    发明人： Bernard R. Neustadt ,  Hong Liu

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

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Compounds having the structural formula Iwherein: n is 0, 1, 2 or 3; A is C(R1) or N; R1 and R1a are H, (C1–C6)-alkyl, halo, CN or —CF3; X is —C(O)—, —O—, —SO0-2—, or optionally substituted methylene, imino, arylene or heteroaryldiyl; Y is —O—, —SO0-2—, or optionally substituted arylene, heteroaryldiyl, or nitrogen-containing heterocycloalkyl, or with certain provisos, a bond; R is optionally substituted-aryl or heteroaryl; and R2 is optionally substituted-aryl, heteroaryl, arylalkyl or heteroarylalkyl; or R2—Y is a fused piperidinyl, substituted piperazinyl or substituted piperidinyl; their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations

    摘要翻译： 具有结构式I的化合物，其中：n为0,1,2或3; A是C（R 1）或N; R 1和R 2是H，（C 1 -C 6 -C 6） - 烷基，卤素，CN或 -CF 3 N 3; X是-C（O） - ， - O - ， - SO 2 - 或任选取代的亚甲基，亚氨基，亚芳基或杂芳基二基; Y是-O-，-SO 0-2 - 或任选取代的亚芳基，杂芳基二基或含氮杂环烷基，或具有一定条件的键; R是任选取代的 - 芳基或杂芳基; R 2是任选取代的 - 芳基，杂芳基，芳基烷基或杂芳基烷基; 或R 2 -Y是稠合的哌啶基，取代的哌嗪基或取代的哌啶基; 其用于治疗帕金森病，单独或与其他治疗帕金森病的药物组合，包含它们的药物组合物和包含组合的组分的试剂盒

    [1,2,4]-Triazole bicyclic adeonsine A2a receptor antagonists
    3.
    发明授权
    [1,2,4]-Triazole bicyclic adeonsine A2a receptor antagonists 有权
    Ä1,2,4'-三唑双环腺苷A2a受体拮抗剂

    公开(公告)号：US06875772B2

    公开(公告)日：2005-04-05

    申请号：US10304939

    申请日：2002-11-26

    申请人： Bernard R. Neustadt ,  Hong Liu

    发明人： Bernard R. Neustadt ,  Hong Liu

    IPC分类号： A61K31/519 ,  A61P25/00 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  C07D471/04 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Compounds having the structural formula I wherein: n is 0, 1, 2 or 3; A is C(R1) or N; R1 and R1a are H, (C1-C6)-alkyl, halo, CN or —CF3; X is —C(O)—, —O—, —SO0-2—, or optionally substituted methylene, imino, arylene or heteroaryldiyl; Y is —O—, —SO0-2—, or optionally substituted arylene, heteroaryldiyl, or nitrogen-containing heterocycloalkyl, or with certain provisos, a bond; R is optionally substituted-aryl or heteroaryl; and R2 is optionally substituted aryl, heteroaryl, arylalkyl or heteroarylalkyl; or R2—Y is a fused piperidinyl, substituted piperazinyl or substituted piperidinyl; their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations.

    摘要翻译： 具有结构式I的化合物，其中n为0,1,2或3; A为C（R 1）或N; R 1和R 1a为H，（C 1 -C 6） - 烷基，卤代 ，CN或-CF 3; X是-C（O） - ， - O - ， - SO 2 2-或任选取代的亚甲基，亚氨基，亚芳基或杂芳基二; Y是-O-，-SOO- 取代的亚芳基，杂芳基二基或含氮杂环烷基，或具有某些条件的键; R是任选取代的 - 芳基或杂芳基; R 2是任选取代的芳基，杂芳基，芳基烷基或杂芳基烷基; 或R 2 -Y是稠合的哌啶基，取代的哌嗪基或取代的哌啶基;它们用于治疗帕金森病，单独或与其它用于治疗帕金森病的药物组合，其包含它们的药物组合物和包含 组合。