首页> 外国专利> RUFINAMIDE AND DERIVATIVES AND THEIR USE IN MODULATING THE GATING PROCESS OF HUMAN VOLTAGE-GATED SODIUM CHANNELS

RUFINAMIDE AND DERIVATIVES AND THEIR USE IN MODULATING THE GATING PROCESS OF HUMAN VOLTAGE-GATED SODIUM CHANNELS

机译:葡糖酰胺和衍生物及其在调节人为电压门控钠离子通道的过程中的用途

摘要

The present invention provides compounds of formula I or a salt, solvate, or stereoisomer thereof, wherein X is H, or an electron withdrawing group such as a halogen, NH2, NO2, SO2, CN, or a C1-C6 alkyl group; Alk is C1-C3 alkyl; R1 is H, C1-C6 alkyl, which may be substituted with OH, NH2, acyl, sulfonyl, and cyano groups; and R2, is C1-C6 alkyl, which may be substituted with OH, NH2, acyl, sulfonyl, and cyano groups. Pharmaceutical compositions comprising these compounds and/or rufinamide are also provided. Methods for prevention and treatment of epilepsy disorders such as Lennox-Gastaut Syndrome (LGS), and modulation of voltage-gated sodium (Nav) channels are Nav1.1 channels by administration of these compounds and/or rufinamide are also provided.
机译:本发明提供式I化合物或其盐,溶剂化物或立体异构体,其中X为H或吸电子基团如卤素,NH 2 ,NO 2 ,SO 2 ,CN或C 1 -C 6 烷基;烷基是C 1 -C 3 烷基; R 1 是H,C 1 -C 6 烷基,可被OH,NH 2 取代,酰基,磺酰基和氰基;和R 2 是C 1 -C 6 烷基,可以被OH,NH 2 取代,酰基,磺酰基和氰基。还提供了包含这些化合物和/或芦丁酰胺的药物组合物。还提供了预防和治疗癫痫病例如伦诺克斯-盖斯特综合征(LGS)的方法,以及通过施用这些化合物和/或rufinamide调节电压门控钠(Nav)通道为Nav1.1通道。

著录项

  • 公开/公告号US2018050994A1

    专利类型

  • 公开/公告日2018-02-22

    原文格式PDF

  • 申请/专利权人 THE JOHNS HOPKINS UNIVERSITY;

    申请/专利号US201715796146

  • 发明设计人 FRANK BOSMANS;

    申请日2017-10-27

  • 分类号C07D249/04;A61K45/06;A61K31/20;A61K31/27;A61K31/53;A61K31/4192;A61K31/7048;A61K31/357;A61K31/19;A61K31/5513;A61K31/551;

  • 国家 US

  • 入库时间 2022-08-21 13:02:45

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