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    • 1. 发明授权
    • Blockade of sodium channels by phenol derivatives
    • 苯酚衍生物阻断钠通道
    • US07485669B2
    • 2009-02-03
    • US10416632
    • 2001-11-13
    • Gertrud HaeselerMartin Leuwer
    • Gertrud HaeselerMartin Leuwer
    • A01N31/00A01M31/08A61K31/045A61K31/05
    • A61K8/498A61K8/347A61K8/4973A61K31/05A61K31/055A61K31/35A61K31/352A61K2800/28A61Q19/00
    • The invention relates to a pharmaceutical composition comprising at least one phenol derivative represented by formula (I) wherein R1 represents a hydrogen atom, a halogen atom or a hydrocarbon group containing up to 12 carbon atoms; R2 represents a hydrogen atom or a C1-C7 alkyl group; wherein R1 and R2 may optionally form a carbocyclic 5- or 6-membered ring; R3 represents a hydrogen atom, a halogen atom or a C1-C7alkyl group; R4 represents a hydrogen atom, a C1-C7 alkyl group or a halogen atom; R5 represents hydrogen atom, a halogen atom or a C1-C7 alkyl group; and R6 represents a hydrogen atom, a C1-C7 alkyl group or a C2 or C3 alkenyl group, under the proviso that R2 and R4 can only both represent a hydrogen atom if both R1 and R5 represent a C1-C7 alkyl group and R3 represents a halogen atom. The composition is particularly useful for the blockage of sodium channels and/or influencing the kinetics of sodium channels and thus can be used as local anesthetic, antidysrhythmic, anticonvulsant/antiepilepticand spasmolytic.
    • 本发明涉及包含至少一种由式(I)表示的苯酚衍生物的药物组合物,其中R 1表示氢原子,卤素原子或含有至多12个碳原子的烃基; R2表示氢原子或C1-C7烷基; 其中R1和R2可以任选地形成碳环5或6元环; R3表示氢原子,卤素原子或C1-C7烷基; R4表示氢原子,C1-C7烷基或卤素原子; R5代表氢原子,卤素原子或C1-C7烷基; 并且R 6表示氢原子,C 1 -C 7烷基或C 2或C 3烯基,条件是如果R 1和R 5均表示C 1 -C 7烷基,则R 2和R 4只能表示氢原子,并且R 3表示 卤素原子。 该组合物特别可用于阻断钠通道和/或影响钠通道的动力学,因此可用作局部麻醉剂,抗心律失常药,抗惊厥药/抗癫痫药和解痉药。