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    • 50. 发明授权
    • [1,2,4]-Triazole bicyclic adenosine A2a receptor antagonists
    • [1,2,4] - 三唑双环腺苷A2a受体拮抗剂
    • US07078408B2
    • 2006-07-18
    • US10973642
    • 2004-10-26
    • Bernard R. NeustadtHong Liu
    • Bernard R. NeustadtHong Liu
    • C07D487/04A61K31/519A61P25/24A61P25/16
    • C07D471/04C07D487/04
    • 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
    • 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