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    Compounds and methods for the treatment of inflammatory and immune disorders
    2.
    发明授权
    Compounds and methods for the treatment of inflammatory and immune disorders 失效
    用于治疗炎症和免疫疾病的化合物和方法

    公开(公告)号：US06294574B1

    公开(公告)日：2001-09-25

    申请号：US08469073

    申请日：1995-06-06

    申请人： Xiong Cai ,  Sajjat Hussoin ,  San-Bao Hwang ,  David Killian ,  T. Y. Shen

    发明人： Xiong Cai ,  Sajjat Hussoin ,  San-Bao Hwang ,  David Killian ,  T. Y. Shen

    IPC分类号： A01N4308

    CPC分类号： C07D405/12 ,  C07D207/09 ,  C07D307/12 ,  C07D307/14 ,  C07D333/16 ,  C07D333/18 ,  C07D333/20 ,  C07D405/04 ,  C07D407/12 ,  C07D409/12

    摘要： 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

    摘要翻译： 2,5-二芳基四氢呋喃，2,5-二芳基四氢噻吩，2,4-二芳基四氢呋喃，2,4-二芳基四氢噻吩，1,3-二芳基环戊烷，2,4-二芳基吡咯烷和2,5-二芳基吡咯烷 公开了减少趋化性和呼吸道爆发，导致在炎症或免疫反应期间形成多形核白细胞的有害氧自由基。 通过作为PAF受体拮抗剂，通过抑制酶5-脂氧合酶，或通过显示双重活性，化合物表现出这种生物学活性， 还公开了治疗由PAF或白细胞三烯介导的病症的方法，其包括施用有效量的一种或多种上述化合物或 其药学上可接受的盐，任选地在药学上可接受的载体中。

    Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
    6.
    发明授权
    Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders 失效
    用于治疗心血管，炎症和免疫疾病的化合物和方法

    公开(公告)号：US06420392B1

    公开(公告)日：2002-07-16

    申请号：US08669371

    申请日：1996-10-09

    申请人： Tesfaye Biftu ,  Xiong Cai ,  Sajjat Hussoin ,  Gurmit Grewal ,  T Y Shen

    发明人： Tesfaye Biftu ,  Xiong Cai ,  Sajjat Hussoin ,  Gurmit Grewal ,  T Y Shen

    IPC分类号： A01N4306

    CPC分类号： C07D405/04 ,  C07D207/09 ,  C07D307/12 ,  C07D307/14 ,  C07D333/16 ,  C07D333/18 ,  C07D333/20 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  Y10S514/825 ,  Y10S514/826 ,  Y10S514/863 ,  Y10S514/912 ,  Y10S514/914 ,  Y10S514/921 ,  Y10S514/925

    摘要： 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.

    摘要翻译： 公开了2,5-二芳基四氢呋喃，2,5-二芳基四氢噻吩，1,3-二芳基环戊烷，其减少趋化性和呼吸道爆发，导致在炎性或免疫反应期间形成多形核白细胞的有害氧自由基。 该化合物通过作为PAF受体拮抗剂，通过抑制酶5-脂氧合酶，或通过显示双重活性，即作为PAF受体拮抗剂和5-脂肪氧合酶抑制剂两者而表现出该生物学活性。 还公开了一种治疗由PAF和/或白三烯介导的病症的方法，其包括向有需要的患者施用有效量的一种或多种上述化合物或其药学上可接受的盐，任选地在药学上可接受的载体中 的这种疗法。