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    • 6. 发明公开
    • Use of serotonin antagonists in the treatment of drug addiction
    • Verwendung von Serotonin-Antagonisten bei der Behandlung vonDrogenabhängigkeit。
    • EP0357416A2
    • 1990-03-07
    • EP89308806.2
    • 1989-08-31
    • GLAXO GROUP LIMITED
    • Coates, Ian HaroldOxford, Alexander WilliamNorth, Peter CharlesTyers, Michael Brian
    • A61K31/00A61K31/445A61K31/55
    • A61K31/00A61K31/445A61K31/55
    • The invention relates to the use of compounds of formula (I)
      wherein Im represents an imidazolyl group of formula:
      and R¹ represents a hydrogen atom or a group selected from C₁₋₆alkyl, C₃₋₆alkenyl, C₃₋₁₀alkynyl, C₃₋₇cycloalkyl, C₃₋₇cycloalkylC₁₋₄alkyl, phenyl, phenylC₁₋₃alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, -CO₂R⁵, -COR⁵, -CONR⁵R⁶ or -SO₂R⁵ (wherein R⁵ and R⁶, which may be the same or different, each represents a hydrogen atom, a C₁₋₆alkyl or C₃₋₇cycloalkyl group, or a phenyl or phenylC₁₋₄alkyl group, in which the phenyl group is optionally substituted by one or more C₁₋₄alkyl, C₁₋₄alkoxy or hydroxy groups or halogen atoms, with the proviso that R⁵ does not represent a hydrogen atom when R¹ represents a group -CO₂R⁵ or -SO₂R⁵);
      one of the groups represented by R², R³ and R⁴ is a hydrogen atom or a C₁₋₆alkyl, C₃₋₇cycloalkyl, C₃₋₆alkenyl, phenyl or phenyl C₁₋₃alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C₁₋₆ alkyl group;
      and n represents 2 or 3,
      and physiologically acceptable salts and solvates thereof for the manufacture of a medicament for the relief or prevention of a withdrawal syndrome resulting from addiction to a drug of substance of abuse and/or for the suppression of dependence on drugs or substances of abuse.
    • 本发明涉及式(I)化合物的用途,其中Im表示下式的咪唑基:&lt; CHEM&gt; R 1表示氢原子或选自C 1-6烷基,C 3-6烯基, C 3-10炔基,C 3-7环烷基,C 3-7环烷基C 1-4烷基,苯基,苯基C 1-3烷基,苯基甲氧基甲基,苯氧基乙基,苯氧基甲基,-CO 2 R 5,-COR 5,-CONR 5 R 6或-SO 2 R <5>(其中R 5和R 6可以相同或不同,各自表示氢原子,C 1-6烷基或C 3-7环烷基或苯基或苯基C 1-4烷基,其中 苯基任选被一个或多个C 1-4烷基,C 1-4烷氧基或羟基或卤素原子取代,条件是当R 1表示-CO 2 R 5基团时,R 5不表示氢原子 >或-SO 2 R 5); 由R 2,R 3和R 4表示的基团之一是氢原子或C 1-6烷基,C 3-7环烷基,C 3-6烯基,苯基或苯基C 1-3烷基, 可以相同或不同的其它两个基团表示氢原子或C1-6烷基; 和n表示2或3,以及其生理上可接受的盐和溶剂合物,用于制备用于缓解或预防由于滥用物质的药物成瘾引起的戒断综合征和/或抑制对药物的依赖或 滥用物质