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PHARMACEUTICAL PREPARATIONS CONTAINING NK1 RECEPTORS ANTAGONISTS AND SODIUM CHANNEL BLOCKING COMPOUNDS

机译:包含NK1受体拮抗剂和钠通道阻滞剂的药物制剂

摘要

The present invention relates to pharmaceutical compositions comprising an NK1 receptor antagonist and a sodium channel blocker compound of formula (I) wherein R1 and R2 are independently hydrogen, C1-6alkyl or C3-6cycloalkylC1-6alkyl; or R1 and R2, together with the nitrogen to which they are attached, may form an unsubstituted 3-, 4-, 5- or 6-membered saturated ring; q is 1 or 2; R3 and R4 are hydrogen; or when q is 1, R3 and R4, together with the interconnecting atoms, may form a cyclopropane ring; X is carbon or nitrogen; n is 0, 1 or 2, wherein when present each R5 is independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; and either R6 or R7 is -O-R8 or -OCH2R8, wherein the other R6 or R7 is hydrogen or R5; and wherein R8 is either a phenyl ring or a 5- or 6-membered aromatic heterocyclic ring (independently containing one or more nitrogen, sulphur or oxygen atoms) wherein either the phenyl ring or the heterocyclic ring is optionally substituted by one or more groups independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; or a pharmaceutically acceptable salt or solvate thereof; as a combined preparation for simultaneous or sequential administration, and to the use of such compositions in the treatment of certain disorders, including epilepsy and mood disorders.
机译:本发明涉及包含NK1受体拮抗剂和式(I)的钠通道阻断剂化合物的药物组合物,其中R1和R2独立地是氢,C1-6烷基或C3-6环烷基C1-6烷基; R 1和R 2与它们所连接的氮一起可以形成未取代的3-,4-,5-或6-元饱和环; q是1或2; R3和R4是氢;或者当q为1时,R 3和R 4与相互连接的原子一起可以形成环丙烷环。 X是碳或氮; n为0、1或2,其中当存在时,每个R 5独立地选自C 1-3烷基,卤素,氰基,卤代C 1-3烷基,羟基,C 1-3烷氧基和C 1-3卤代烷氧基。 R6或R7为-O-R8或-OCH2R8,其中另一个R6或R7为氢或R5;其中R8是苯环或5-或6-元芳族杂环(独立地含有一个或多个氮,硫或氧原子),其中苯环或杂环任选地被一个或多个基团独立地取代选自C 1-3烷基,卤素,氰基,卤代C 1-3烷基,羟基,C 1-3烷氧基和C 1-3卤代烷氧基;或其药学上可接受的盐或溶剂化物;作为同时或顺序给药的组合制剂,以及这种组合物在某些疾病包括癫痫和情绪障碍的治疗中的用途。

著录项

  • 公开/公告号AT530182T

    专利类型

  • 公开/公告日2011-11-15

    原文格式PDF

  • 申请/专利权人 GLAXO GROUP LIMITED;

    申请/专利号AT20080708027T

  • 发明设计人 ALVARO GIUSEPPE;LARGE CHARLES;

    申请日2008-01-21

  • 分类号A61K31/401;A61P25/08;

  • 国家 AT

  • 入库时间 2022-08-21 17:21:55

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