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    2-alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
    2.
    发明申请
    2-alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists 有权
    2-炔基 - 和2-烯基 - 吡唑并[4,3-e] -1,2,4-三唑并 - [1,5-c] - 嘧啶腺苷A2a受体拮抗剂

    公开(公告)号：US20050222164A1

    公开(公告)日：2005-10-06

    申请号：US11135261

    申请日：2005-05-23

    申请人： Bernard Neustadt ,  Jinsong Hao ,  Hong Liu ,  Craig Boyle ,  Samuel Chackalamannil ,  Unmesh Shah ,  Andrew Stamford

    发明人： Bernard Neustadt ,  Jinsong Hao ,  Hong Liu ,  Craig Boyle ,  Samuel Chackalamannil ,  Unmesh Shah ,  Andrew Stamford

    IPC分类号： A61P25/16 ,  C07D487/14 ,  A61K31/519

    CPC分类号： C07D487/14

    摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; R6 is H, alkyl, hydroxyalkyl or —CH2F; R7, R8 and R9 are H, alkyl, alkoxy, alkylthio, alkoxyalkyl, halo or —CF3; and Z is optionally substituted aryl, heteroaryl or heteroaryl-alkyl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.

    摘要翻译： 具有结构式I的化合物或其药学上可接受的盐，其中R是R 1，R 2，R 3，R 3， 4和R 5是H，烷基或烷氧基烷基; R 6是H，烷基，羟基烷基或-CH 2 F; R 7，R 8和R 9是H，烷基，烷氧基，烷硫基，烷氧基烷基，卤素或-CF 3， SUB>; 和Z是任选取代的芳基，杂芳基或杂芳基 - 烷基。 还公开了式I化合物在治疗中枢神经系统疾病，特别是帕金森病中单独使用或与用于治疗帕金森病的其它药物组合的用途，以及包含它们的药物组合物的用途。

    2-alkynyl- and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
    8.
    发明授权
    2-alkynyl- and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists 有权
    2-炔基 - 和2-烯基 - 吡唑并[4,3-e] -1,2,4-三唑并 - [1,5-c] - 嘧啶腺苷A2a受体拮抗剂

    公开(公告)号：US07368449B2

    公开(公告)日：2008-05-06

    申请号：US11135261

    申请日：2005-05-23

    申请人： Bernard R. Neustadt ,  Jinsong Hao ,  Hong Liu ,  Craig D. Boyle ,  Samuel Chackalamannil ,  Unmesh G. Shah ,  Andrew Stamford

    发明人： Bernard R. Neustadt ,  Jinsong Hao ,  Hong Liu ,  Craig D. Boyle ,  Samuel Chackalamannil ,  Unmesh G. Shah ,  Andrew Stamford

    IPC分类号： A61K31/497

    CPC分类号： C07D487/14

    摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; R6 is H, alkyl, hydroxyalkyl or —CH2F; R7, R8 and R9 are H, alkyl, alkoxy, alkylthio, alkoxyalkyl, halo or —CF3; and Z is optionally substituted aryl, heteroaryl or heteroaryl-alkyl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.

    摘要翻译： 具有结构式I的化合物或其药学上可接受的盐，其中R是R 1，R 2，R 3，R 3， 4和R 5是H，烷基或烷氧基烷基; R 6是H，烷基，羟基烷基或-CH 2 F; R 7，R 8和R 9是H，烷基，烷氧基，烷硫基，烷氧基烷基，卤素或-CF 3， SUB>; 和Z是任选取代的芳基，杂芳基或杂芳基 - 烷基。 还公开了式I化合物在治疗中枢神经系统疾病，特别是帕金森病中单独使用或与用于治疗帕金森病的其它药物组合的用途，以及包含它们的药物组合物的用途。

    Topical and/or transdermal bioactive compound delivery system
    9.
    发明申请
    Topical and/or transdermal bioactive compound delivery system 审中-公开
    局部和/或透皮生物活性化合物递送系统

    公开(公告)号：US20060067995A1

    公开(公告)日：2006-03-30

    申请号：US11173536

    申请日：2005-07-01

    申请人： Wan Sia Heng ,  Jinsong Hao ,  Lai Chan ,  Ma Nyunt ,  Gil Yosipovitch ,  Yolande Anthony

    发明人： Wan Sia Heng ,  Jinsong Hao ,  Lai Chan ,  Ma Nyunt ,  Gil Yosipovitch ,  Yolande Anthony

    IPC分类号： A61K9/70

    CPC分类号： A61K9/7061 ,  A61K47/34

    摘要： Topical and/or transdermal bioactive compound delivery system The present invention provides a topical and/or transdermal bioactive compound delivery system comprising a non-aqueous matrix, the matrix comprising a water-sensitive bioactive compound. In particular, the matrix comprises a three-dimensional polymeric network comprising at least a co-polymer, at least a cross-linking agent, and at least a non-aqueous and/or non-volatile solvent and wherein the water-sensitive bioactive compound is housed by the three-dimensional network. Even more in particular, the matrix comprises a co-polymer of N-vinylacetamide and sodium acrylate aluminium chloride; N-methyl-2-pyrrolidone; propylene glycol; glycerine; and at least a water-sensitive bioactive compound.

    摘要翻译： 局部和/或透皮生物活性化合物递送系统本发明提供了包含非水性基质的局部和/或透皮生物活性化合物递送系统，所述基质包含水敏感的生物活性化合物。 特别地，基质包括三维聚合物网络，其包含至少共聚物，至少交联剂和至少非水和/或非挥发性溶剂，并且其中所述水敏生物活性化合物 由三维网络容纳。 更特别地，基质包括N-乙烯基乙酰胺和丙烯酸钠氯化铝的共聚物; N-甲基-2-吡咯烷酮; 丙二醇 甘油; 和至少一种水敏感的生物活性化合物。