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    Condensed purine derivatives
    2.
    发明授权
    Condensed purine derivatives 失效
    凝血嘌呤衍生物

    公开(公告)号：US06306847B1

    公开(公告)日：2001-10-23

    申请号：US09090936

    申请日：1998-06-05

    申请人： Hiroshi Tsumuki ,  Mayumi Saki ,  Hiromi Nonaka ,  Michio Ichimura ,  Junichi Shimada ,  Fumio Suzuki ,  Shunji Ichikawa ,  Nobuo Kosaka

    发明人： Hiroshi Tsumuki ,  Mayumi Saki ,  Hiromi Nonaka ,  Michio Ichimura ,  Junichi Shimada ,  Fumio Suzuki ,  Shunji Ichikawa ,  Nobuo Kosaka

    IPC分类号： C07D48714

    CPC分类号： C07D487/14

    摘要： The present invention provides condensed purine derivatives or pharmacologically acceptable salts thereof exhibiting adenosine A3 acceptor antagonising activity, and having an antiasthmatic action, a bronchodilator action, an antiantiitching action, etc., and represented by the following formula (I): (wherein R1 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; R2 represents hydrogen, lower alkyl, alicyclic alkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted aromatic heterocyclic group; R3 represents hydrogen, lower alkyl, or substituted or unsubstituted aralkyl; X1 and X2 are the same or different and each represents hydrogen, lower alkyl, substituted or unsubstituted aralkyl, or substituted or unsubstituted aryl; and n represents an integer of 0 to 3).

    摘要翻译： 本发明提供具有腺苷A3受体拮抗活性的缩合嘌呤衍生物或其药理学上可接受的盐，并具有抗哮喘作用，支气管扩张剂作用，抗脱除作用等，并由下式（I）表示:(其中R1表示 取代或未取代的芳基或取代或未取代的芳族杂环基; R 2表示氢，低级烷基，脂环族烷基，取代或未取代的芳烷基，取代或未取代的芳基或取代或未取代的芳族杂环基; R 3表示氢，低级烷基或 取代或未取代的芳烷基; X 1和X 2相同或不同，各自表示氢，低级烷基，取代或未取代的芳烷基或取代或未取代的芳基; n表示0〜3的整数。

    [1,2,4] triazolo [1,5-C] pyrimidine derivatives
    3.
    发明授权
    [1,2,4] triazolo [1,5-C] pyrimidine derivatives 失效
    [1,2,4]三唑并[1,5-C]嘧啶衍生物

    公开(公告)号：US06222035B1

    公开(公告)日：2001-04-24

    申请号：US09401984

    申请日：1999-09-23

    申请人： Hiroshi Tsumuki ,  Junichi Shimada ,  Hironori Imma ,  Akiko Nakamura ,  Hiromi Nonaka ,  Shizuo Shiozaki ,  Shunji Ichikawa ,  Tomoyuki Kanda ,  Yoshihisa Kuwana ,  Michio Ichimura ,  Fumio Suzuki

    发明人： Hiroshi Tsumuki ,  Junichi Shimada ,  Hironori Imma ,  Akiko Nakamura ,  Hiromi Nonaka ,  Shizuo Shiozaki ,  Shunji Ichikawa ,  Tomoyuki Kanda ,  Yoshihisa Kuwana ,  Michio Ichimura ,  Fumio Suzuki

    IPC分类号： C07D48700

    CPC分类号： C07D487/04

    摘要： [1,2,4]Triazolo[1,5-c]pyrimidine derivatives represented by formula (I) or pharmaceutically acceptable salts thereof are provided, which have adenosine A2A receptor antagonism and are useful for the treatment or prevention of various diseases induced by hyperactivity of adenosine A2A receptors (for example, Parkinson's disease or senile dementia): wherein R1 represents substituted or unsubstituted aryl, or the like; R2 represents hydrogen, halogen, lower alkyl, substituted or unsubstituted aryl, or the like; R3 represents hydrogen, halogen, XR10 (wherein X represents O or S; and R10 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic ring, substituted or unsubstituted aralkyl, lower alkyl, or hydroxy lower alkyl), or the like; and Q represents hydrogen or 3,4-dimethoxybenzyl.

    摘要翻译： [1,2,4]具有式（I）表示的三唑并[1,5-c]嘧啶衍生物或其药学上可接受的盐，其具有腺苷A2A受体拮抗作用，可用于治疗或预防由 腺苷A2A受体（例如帕金森病或老年性痴呆）的多动症：其中R1表示取代或未取代的芳基等; R 2表示氢，卤素，低级烷基，取代或未取代的芳基等; R3表示氢，卤素，XR10（其中X表示O或S; R10表示取代或未取代的芳基，取代或未取代的芳族杂环，取代或未取代的芳烷基，低级烷基或羟基低级烷基）等; Q表示氢或3,4-二甲氧基苄基。