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    • 1. 发明申请
    • TETRAHYDROBENZINDOLE COMPOUNDS
    • 四氢化萘化合物
    • WO1998000400A1
    • 1998-01-08
    • PCT/JP1997002226
    • 1997-06-27
    • MEIJI SEIKA KAISHA, LTD.KOYAMA, MasaoKIKUCHI, ChikaUSHIRODA, OsamuANDO, TakashiNAGASO, HiroshiFUJI, KazuyukiOKUNO, MasayoHIRANUMA, Toyokazu
    • MEIJI SEIKA KAISHA, LTD.
    • C07D209/92
    • C07D401/06C07D209/92C07D401/12C07D403/12
    • Compounds represented by general formula (I) and pharmaceutically acceptable salts thereof which strongly inhibit [ H]-serotonin and [ H]-5-CT binding to the human serotonin 5-HT7 receptor subtype expressed in a cultured cell line and can provide medicinal compositions for treating or preventing mental diseases. In said formula (I) A represents N, CH, C having a double bond or CR ; B and Z independently represent each N, CH or CR , provided that A is N when B and/or Z is N; R represents hydrogen, halogeno, lower alkyl, cyano, trihalomethyl, hydroxy, alkoxy, alkylthio, alkylsulfenyl, alkylsulfonyl, alkoxycarbonyl, sulfamoyl, optionally substituted amino, optionally alkylated carbamoyl, acyl or carboxy; R represents hydrogen or lower alkyl; R represents hydrogen, lower alkyl or aralkyl; R represents hydrogen, halogeno, lower alkyl, hydroxyl, alkoxy, acyl, alkoxycarbonyl, nitro, optionally substituted amino, optionally alkylated carbamoyl or acyloxy; R represents lower alkyl, cyano, carbamoyl, carboxy, acyl, acyloxy, alkoxy, alkoxycarbonyl, trihalomethyl or hydroxy; and n is an integer of from 2 to 6.
    • 由通式(I)表示的化合物及其药学上可接受的盐,其强力抑制在培养细胞中表达的人5-羟色胺5-HT7受体亚型的[3 H] - 血清素和[3 H] -5-CT结合 可以提供用于治疗或预防精神疾病的药物组合物。 在所述式(I)中,A表示具有双键或CR 5的N,CH,C; B和Z独立地表示每个N,CH或CR 1,条件是当B和/或Z为N时A为N; R 1表示氢,卤代,低级烷基,氰基,三卤代甲基,羟基,烷氧基,烷硫基,烷基亚磺酰基,烷基磺酰基,烷氧基羰基,氨磺酰基,任选取代的氨基,任选烷基化的氨基甲酰基,酰基或羧基; R 2表示氢或低级烷基; R 3表示氢,低级烷基或芳烷基; R 4表示氢,卤代,低级烷基,羟基,烷氧基,酰基,烷氧基羰基,硝基,任选取代的氨基,任选烷基化的氨基甲酰基或酰氧基; R 5代表低级烷基,氰基,氨基甲酰基,羧基,酰基,酰氧基,烷氧基,烷氧基羰基,三卤代甲基或羟基; n为2〜6的整数。