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    • 2. 发明授权
    • Heterocyclic derivative and medicine
    • 杂环衍生物和药物
    • US06191149B1
    • 2001-02-20
    • US09334253
    • 1999-06-16
    • Shoichi ChokaiYojiro UkaiTomiyoshi AokiKyoichi Ideguchi
    • Shoichi ChokaiYojiro UkaiTomiyoshi AokiKyoichi Ideguchi
    • A61K31444
    • C07D213/64C07D239/34C07D239/38C07D239/52C07D239/56C07D251/22C07D401/04C07D401/12C07D409/04
    • A pharmaceutical composition comprising a compound of the following general formula [I] or its salt. wherein R1 represents aryl or a heteroaromatic group. R2 represents hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, haloalkyl, alkoxy, alkylthio, amino, monoalkylamino, dialkylamino, or phenyl. R3 and R4 independently represent hydrogen or alkyl or R3 and R4 taken together with the adjacent N atom represent a 5- through 7-membered cyclic amino group. A represents a single bond C2-10 alkylene. W represents O, S, or (CH2)n (where CH may be substituted by alkyl; n is an integer of 1 or 2). X, Y, and Z may be the same or different and each represents CH (which may be substituted by alkyl), or N. Provided, however, that the case in which X, Y, and Z concurrently represent CH is excluded. The compound of the invention has excellent neuronal death inhibitory activity and is useful as a therapeutic drug for cerebrovascular diseases.
    • 包含下列通式[Ⅰ]化合物或其盐的药物组合物,其中R 1表示芳基或杂芳基.R 2表示氢,烷基,烯基,环烷基,环烷基烷基,羟基烷基,卤代烷基,烷氧基,烷硫基,氨基,单烷基氨基 ,二烷基氨基或苯基。 R3和R4独立地表示氢或烷基,R3和R4与相邻的N原子一起表示5-至7-元环氨基。 A表示单键C2-10亚烷基。 W表示O,S或(CH 2)n(其中CH可以被烷基取代; n是1或2的整数)。 X,Y和Z可以相同或不同,各自表示CH(可以被烷基取代)或N.可以排除X,Y和Z同时表示CH的情况。 本发明化合物具有优异的神经元死亡抑制活性,可用作脑血管疾病的治疗药物。