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    Pyrazolo [1,5-A]pyrimidine adenosine A2a receptor antagonists
    3.
    发明授权
    Pyrazolo [1,5-A]pyrimidine adenosine A2a receptor antagonists 有权
    吡唑并[1,5-A]嘧啶腺苷A2a受体拮抗剂

    公开(公告)号：US07741318B2

    公开(公告)日：2010-06-22

    申请号：US11311195

    申请日：2005-12-19

    申请人： Martin C. Clasby ,  Samuel Chackalamannil ,  Bernard R. Neustadt ,  Xiaobang Gao

    发明人： Martin C. Clasby ,  Samuel Chackalamannil ,  Bernard R. Neustadt ,  Xiaobang Gao

    IPC分类号： C07D243/08 ,  C07D295/02 ,  C07D295/16 ,  C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/5513 ,  A61P25/16

    CPC分类号： C07D487/04

    摘要： Compounds having the structural formula I are disclosed, wherein A is alkylene, or optionally substituted arylene, cycloalkylene or heteroaryldiyl; X is —C(O)— or —S(O)2—; R1 is alkyl or cycloalkyl; R2 is hydrogen, halo or —CN; R3 is hydrogen or alkyl; R4 is hydrogen, alkyl, alkoxy, hydroxyalkyl, aminoalkyl-, cycloalkyl, heterocycloalkyl, heterocycloalkyl substituted by alkyl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; or R3 and R4, form an optionally substituted 5-7 membered ring, said ring optionally comprising an additional heteroatom ring member; R7 is alkyl, optionally substituted phenyl, optionally substituted heteroaryl, cycloalkyl, halo, morpholinyl, optionally substituted piperazinyl, or optionally substituted azacycloalkyl. Also disclosed is the use of the compounds 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： 公开了具有结构式I的化合物，其中A是亚烷基或任选取代的亚芳基，亚环烷基或杂芳基二基; X是-C（O） - 或-S（O）2 - ; R1是烷基或环烷基; R2是氢，卤素或-CN; R3是氢或烷基; R4是氢，烷基，烷氧基，羟基烷基，氨基烷基 - ，环烷基，杂环烷基，被烷基取代的杂环烷基，任选取代的芳基烷基或任选取代的杂芳基烷基; 或R 3和R 4形成任选取代的5-7元环，所述环任选地包含另外的杂原子环成员; R 7是烷基，任选取代的苯基，任选取代的杂芳基，环烷基，卤素，吗啉基，任选取代的哌嗪基或任选取代的氮杂环烷基。 还公开了化合物在治疗帕金森病中的用途，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组分的试剂盒的用途。

    Pyrazolo [1,5-A] pyrimidine adenosine A2a receptor antagonists
    4.
    发明申请
    Pyrazolo [1,5-A] pyrimidine adenosine A2a receptor antagonists 有权
    吡唑并[1,5-A]嘧啶腺苷A2a受体拮抗剂

    公开(公告)号：US20060135526A1

    公开(公告)日：2006-06-22

    申请号：US11311195

    申请日：2005-12-19

    申请人： Martin Clasby ,  Samuel Chackalamannil ,  Bernard Neustadt ,  Xiaobang Gao

    发明人： Martin Clasby ,  Samuel Chackalamannil ,  Bernard Neustadt ,  Xiaobang Gao

    IPC分类号： A61K31/519 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： Compounds having the structural formula I are disclosed, wherein A is alkylene, or optionally substituted arylene, cycloalkylene or heteroaryldiyl; X is —C(O)— or —S(O)2—; R1 is alkyl or cycloalkyl; R2 is hydrogen, halo or —CN; R3 is hydrogen or alkyl; R4 is hydrogen, alkyl, alkoxy, hydroxyalkyl, aminoalkyl-, cycloalkyl, heterocycloalkyl, heterocycloalkyl substituted by alkyl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; or R3 and R4, form an optionally substituted 5-7 membered ring, said ring optionally comprising an additional heteroatom ring member; R7 is alkyl, optionally substituted phenyl, optionally substituted heteroaryl, cycloalkyl, halo, morpholinyl, optionally substituted piperazinyl, or optionally substituted azacycloalkyl. Also disclosed is the use of the compounds 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： 公开了具有结构式I的化合物，其中A是亚烷基或任选取代的亚芳基，亚环烷基或杂芳基二基; X是-C（O） - 或-S（O）2 - 。 R 1是烷基或环烷基; R 2是氢，卤素或-CN; R 3是氢或烷基; R 4是氢，烷基，烷氧基，羟基烷基，氨基烷基 - ，环烷基，杂环烷基，被烷基，任选取代的芳基烷基或任选取代的杂芳基烷基取代的杂环烷基; 或R 3和R 4，形成任选取代的5-7元环，所述环任选地包含另外的杂原子环成员; R 7是烷基，任选取代的苯基，任选取代的杂芳基，环烷基，卤素，吗啉基，任选取代的哌嗪基或任选取代的氮杂环烷基。 还公开了化合物在治疗帕金森病中的用途，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组分的试剂盒的用途。