USES OF ION CHANNEL MODULATING COMPOUNDS
    31.
    发明申请
    USES OF ION CHANNEL MODULATING COMPOUNDS 有权
    离子通道调节化合物的使用

    公开(公告)号:US20080188547A1

    公开(公告)日:2008-08-07

    申请号:US11947679

    申请日:2007-11-29

    IPC分类号: A61K31/402 A61P9/06

    摘要: Methods, formulations, dosing regimes, and routes of administration for the treatment or prevention of arrhythmias, including the treatment or prevention of atrial fibrillation. In these methods, the disease or condition is treated or prevented by administering one or more ion channel modulating compounds to a subject, where the ion channel modulating compound or compounds produce specific plasma levels in the subject. The ion channel modulating compounds may be cycloalkylamine ether compounds, particularly cyclohexylamine ether compounds.

    摘要翻译: 用于治疗或预防心律失常的方法,制剂,给药方案和给药途径,包括治疗或预防心房颤动。 在这些方法中,通过向受试者施用一种或多种离子通道调节化合物来治疗或预防疾病或病症,其中离子通道调节化合物或化合物在受试者中产生特异性血浆水平。 离子通道调节化合物可以是环烷基胺醚化合物,特别是环己胺醚化合物。

    Methods for producing novel conjugates of thrombin inhibitors
    32.
    发明授权
    Methods for producing novel conjugates of thrombin inhibitors 失效
    生产凝血酶抑制剂新型缀合物的方法

    公开(公告)号:US5942620A

    公开(公告)日:1999-08-24

    申请号:US108534

    申请日:1998-07-01

    摘要: Novel compounds comprising chemically reactive intermediates which can react with available reactive functionalities on blood components to form covalent linkages, where the resulting covalently-bound conjugates are found to have thrombin inhibition activity are provided. Specifically, the thrombin inhibitor compounds of the present invention are derivatives of the known thrombin inhibitor argatroban, which can be covalently linked to chemically reactive functionalities on various blood components. The conjugated thrombin inhibitors thereby have extended lifetimes in the bloodstream, as compared to the unconjugated parent drug, and are, therefore, capable of maintaining thrombin inhibitory activity for extended periods of time as compared to the unconjugated parent drug. Also provided herein are methods for inhibiting thrombin activity in vivo comprising administering to the bloodstream of a mammalian host the novel compounds of the present invention.

    摘要翻译: 提供了包含化学反应中间体的新型化合物,其可与血液成分上的可用反应性官能团反应以形成共价键,其中发现所得的共价结合的缀合物具有凝血酶抑制活性。 具体地,本发明的凝血酶抑制剂化合物是已知的凝血酶抑制剂阿加曲班的衍生物,其可以与各种血液成分上的化学反应性官能团共价连接。 与未缀合的母体药物相比,缀合的凝血酶抑制剂在血液中的寿命延长,因此与未缀合的母体药物相比,能够延长凝血酶抑制活性。 本文还提供用于抑制体内凝血酶活性的方法,包括向哺乳动物宿主的血流施用本发明的新化合物。