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    • 4. 发明授权
    • Narcotic antagonist
    • 麻醉拮抗剂
    • US6100280A
    • 2000-08-08
    • US85463
    • 1998-05-28
    • Masato InazuMariko HaradaTomoko Masuda
    • Masato InazuMariko HaradaTomoko Masuda
    • C07D295/12A61K31/495A61P25/30
    • A61K31/495
    • A narcotic antagonist comprising, as its active component, a compound represented by the following formula (1) or a physiologically acceptable salt thereof: wherein each of R.sup.1 and R.sup.2, which may be identical to or different from each other, represents a hydrogen atom or a halogen atom; R.sup.3 represents a hydrogen atom, an alkyl group, or an acyl group; R.sup.4 represents a hydrogen atom, an alkyl group, an acyl group, an alkylsulfonyl group, or a carboxyl group which may be esterified; Ar represents a phenyl group which may have 1 to 3 substituents selected from the group consisting of a halogen atom, an alkyl group, an alkoxyl group, a nitro group, an amino group, an alkylamino group, and a hydroxyl group or Ar represents a monocyclic aromatic heterocyclic ring having a nitrogen atom; m represents a number of 1 to 5 inclusive; and n represents a number of 0 to 5 inclusive. Also, a medicament for the prevention and treatment of narcotic dependence is provided. The medicament is effective in the prevention and treatment of narcosic dependence due to cocaine, etc.
    • 作为其活性成分的麻醉性拮抗剂含有下述式(1)所示的化合物或其生理学上可接受的盐,其中R1和R2各自可以相同或不同,表示氢原子或 卤素原子; R3表示氢原子,烷基或酰基; R4表示可被酯化的氢原子,烷基,酰基,烷基磺酰基或羧基; Ar表示可以具有1〜3个选自卤素原子,烷基,烷氧基,硝基,氨基,烷基氨基和羟基的取代基的苯基,或者Ar表示 具有氮原子的单环芳族杂环; m表示1〜5的数; n表示0〜5的数。 此外,提供了用于预防和治疗麻醉依赖性的药物。 该药物有效预防和治疗可卡因等引起的麻醉依赖。