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    Local anesthetic compounds
    5.
    发明授权
    Local anesthetic compounds 有权
    局部麻醉化合物

    公开(公告)号：US06436919B1

    公开(公告)日：2002-08-20

    申请号：US09671630

    申请日：2000-09-28

    申请人： Sabine M. Axt ,  Timothy J. Church ,  John R. Jacobsen ,  Thomas E. Jenkins ,  Yu-Hua Ji ,  Huiwei Wu

    发明人： Sabine M. Axt ,  Timothy J. Church ,  John R. Jacobsen ,  Thomas E. Jenkins ,  Yu-Hua Ji ,  Huiwei Wu

    IPC分类号： C07D41306

    CPC分类号： C07D273/00 ,  C07D239/90 ,  C07D413/06 ,  C07D413/14

    摘要： This invention is directed to novel local anesthetic compounds, pharmaceutical compositions containing these compounds, methods of use and methods of preparing these compounds. In one embodiment, the compounds are of the following formula: wherein: R1 and R2 are independently selected from the group consisting of hydrogen, alkyl, halo, cyano, hydroxy, alkoxy, amino, monosubstituted or disubstituted amino, carboxy, and alkoxycarbonyl; R5 and R6 are independently selected from the group consisting of hydrogen and alkyl; R7 is alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle, or substituted heterocycle; R8 and R9 are independently selected from the group consisting of hydrogen, alkyl, substituted alkyl and NRaRb-where Ra and Rb are alkyl; and Ar is selected from the group consisting of aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle, substituted heterocycle, cycloalkyl and substituted cycloalkyl; or a pharmaceutically acceptable salt thereof. The compounds find use as local anesthetics.

    摘要翻译： 本发明涉及新的局部麻醉剂化合物，含有这些化合物的药物组合物，使用方法和制备这些化合物的方法。 在一个实施方案中，所述化合物具有下式：其中：R 1和R 2独立地选自氢，烷基，卤素，氰基，羟基，烷氧基，氨基，单取代或二取代的氨基，羧基和烷氧基羰基; R5和R6独立地选自氢和烷基; R 7是烷基，取代的烷基，芳基，取代的芳基，杂芳基，取代的杂芳基，杂环或取代的杂环; R 8和R 9独立地选自氢，烷基，取代的烷基和NR a R b，其中R a和R b是烷基; 并且Ar选自芳基，取代的芳基，杂芳基，取代的杂芳基，杂环，取代的杂环，环烷基和取代的环烷基; 或其药学上可接受的盐。 该化合物可用作局部麻醉剂。