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    PYRAZOLOTHIAZOLOPYRIMIDINE DERIVATIVE
    2.
    发明公开
    PYRAZOLOTHIAZOLOPYRIMIDINE DERIVATIVE 失效
    吡唑并噻唑并嘧啶衍生物

    公开(公告)号：EP0573659A1

    公开(公告)日：1993-12-15

    申请号：EP92924885.4

    申请日：1992-12-07

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： SUZUKI, Fumio 18-4, Fujimidai ,  NAKASATO, Yoshisuke 1188, Shimotogari ,  OHMORI, Kenji 2-14-6, Fuyodai ,  TAMURA, Tadafumi 3198-3, Ooka ,  SATO, Soichiro 564-5, Nakatogari Nagaizumi-cho ,  TANAKA, Hiroshi 2-31-13, Ishidai

    IPC分类号： C07D513/14 ,  A61K31/505 ,  A61K31/54 ,  A61K31/55

    CPC分类号： C07D513/14

    摘要： A pyrazolothiazolopyrimidine derivative represented by general formula (I), which is useful as anti-inflammatory, analgesic, immunomodulator and antiulcerative, or a pharmacologically acceptable salt thereof, wherein R¹ represents hydrogen, (un)substituted lower alkyl, (un)substituted aryl, (un)substituted aralkyl, halogen or -NR³R⁴ wherein R³ and R⁴ may be the same or different from each other and each represents hydrogen, lower alkyl, lower alkanoyl or aroyl; when R² is substituted at the 1-positiion, then X represents N or CH and R² represents hydrogen, (un)substituted lower alkyl, (un)substituted aryl, (un)substituted aralkyl or lower alkoxycarbonyl; while when R² is substituted at the 2-position, then X represents N and R² represents -CR⁵R⁶R⁷ (wherein R⁵ represents (un)substituted lower alkyl, and R⁶ and R⁷ may be the same or different from each other and each represents hydrogen or lower alkyl), (un)substituted aryl, (un)substituted aralkyl or lower alkoxycarbonyl; Y represents O or S; and Q represents -CR⁸R⁹CR¹⁰R¹¹-(CH₂) n - or -CR⁸=CR⁹-(CH₂)n- wherein R⁸, R⁹, R¹⁰ and R¹¹ may be the same or different from one another and each represents hydrogen, (un)substituted lower alkyl, (un)substituted aryl, (un)substituted aralkyl or lower alkoxycarbonyl, and n represents an integer of 0 to 2.

    摘要翻译： （I）表示的吡唑并噻唑并嘧啶衍生物，其可用作抗炎，镇痛，免疫调节剂和抗溃疡药或其药理学可接受的盐，其中R 1代表氢，（未）取代的低级烷基，（未）取代的芳基， （未）取代的芳烷基，卤素或-NR 3 R 4，其中R 3和R 4可以相同或不同，各自代表氢，低级烷基，低级烷酰基或芳酰基; 当R 2在1-位被取代时，则X代表N或CH，并且R 2代表氢，（未）取代的低级烷基，（未）取代的芳基，（未）取代的芳烷基或低级烷氧基羰基; 而当R 2在2-位被取代时，则X代表N，R 2代表-CR 5 R 6 R 8（其中R 5代表（未）取代的低级烷基，R 6和R 6可以相同或不同，各代表氢或更低 烷基），（未）取代的芳基，（未）取代的芳烷基或低级烷氧基羰基; Y代表O或S; 和Q代表-CR 8 R 9 CR 10 R 11 - （CH 2）n - 或-CR 8 = CR 8 - （CH 2）n - ，其中R 7，R 9，R 10和R 11可以相同或不同，并且各代表氢，（未）取代的低级烷基 （未）取代的芳基，（未）取代的芳烷基或低级烷氧基羰基，并且n表示0至2的整数。