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    Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
    4.
    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：US06201016B1

    公开(公告)日：2001-03-13

    申请号：US08390641

    申请日：1995-02-17

    申请人： Xiong Cai ,  Gurmit Grewal ,  Sajjat Hussoin ,  Aberra Fura ,  Ralph Scannell ,  Tesfaye Biftu

    发明人： Xiong Cai ,  Gurmit Grewal ,  Sajjat Hussoin ,  Aberra Fura ,  Ralph Scannell ,  Tesfaye Biftu

    IPC分类号： A61K3134

    CPC分类号： C07D307/14 ,  C07D471/04

    摘要： Enantiomerically enriched disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and 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. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.

    摘要翻译： 公开了对映体富集的二取代的四氢呋喃，四氢噻吩，吡咯烷和环戊烷，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。 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， 例如通过作为PAF受体拮抗剂和5-脂加氧酶抑制剂两者。已经确定5-脂氧合酶活性，口服可利用性和体内稳定性（例如葡糖苷酸化速率）可以在光学异构体 所公开的化合物。

    Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
    5.
    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：US5681966A

    公开(公告)日：1997-10-28

    申请号：US485096

    申请日：1995-06-07

    申请人： Xiong Cai ,  Gurmit Grewal ,  Sajjat Hussoin ,  Aberra Fura ,  Ralph Scannell ,  Tesfaye Biftu

    发明人： Xiong Cai ,  Gurmit Grewal ,  Sajjat Hussoin ,  Aberra Fura ,  Ralph Scannell ,  Tesfaye Biftu

    IPC分类号： C07D307/14 ,  C07D471/04 ,  C07D333/22 ,  A61K31/34 ,  A61K31/38 ,  C07D307/02

    CPC分类号： C07D471/04 ,  C07D307/14

    摘要： Enantiomerically enriched disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and 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. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.

    摘要翻译： 公开了对映体富集的二取代的四氢呋喃，四氢噻吩，吡咯烷和环戊烷，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。 已经确定，所公开的化合物的光学异构体中的5-脂氧合酶活性，口服可利用性和体内稳定性（例如葡糖苷酸化速率）可以显着变化。

    Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
    7.
    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。