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    • 2. 发明公开
    • TRICYCLIC COMPOUNDS
    • 三环化合物
    • EP0979821A1
    • 2000-02-16
    • EP98914022.3
    • 1998-04-15
    • KYOWA HAKKO KOGYO CO., LTD.
    • YOSHIDA, MakotoSEISHI, TakashiAONO, ShigeruTAKAI, HarukiSUZUKI, KojiYAMAGATA, TsuyoshiATSUKI, KaoruKARASAWA, AkiraKUMAZAWA, Toshiaki
    • C07D313/12C07D333/06C07D333/12C07D495/04A61K31/335A61K31/38A61K31/435
    • C07D495/04C07D313/12C07D337/12
    • The present invention provides tricyclic compounds which are useful for the treatment of pollakiuria and urinary incontinence and which are represented by general formula (I):
      (wherein R 1 represents hydrogen, substituted or unsubstituted lower alkyl, etc.; X 1 -X 2 -X 3 represents CR 5 =CR 6 -CR 7 =CR 8 (wherein R 5 , R 6 , R 7 and R 8 , which may be the same or different, each represents hydrogen, substituted or unsubstituted lower alkyl, hydroxy, substituted or unsubstituted lower alkoxy, etc.), N(O)m=CR 5 -CR 6 -CR 7 (wherein R 5 , R 6 and R 7 have the same significances as defined above, and m represents 0 or 1), S-CR 7 =CR 8 (wherein R 7 and R 8 have the same significances as defined above), etc.;
      and when R 2 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, a substituted or unsubstituted N-substituted heterocyclic group,
      (wherein n is 0 or 1; R 3 and R 4 , which may be the same or different, each represents hydrogen, substituted or unsubstituted lower alkyl, trifluoromethyl, etc., or R 3 and R 4 may be combined together to form cyclic alkyl; and Q represents hydroxy, halogen, etc.), etc., Y represents -CH 2 SO 2 -, -SCH 2 -, -SOCH 2 -, -SO 2 CH 2 -, etc.) and pharmaceutically acceptable salts thereof.
    • 本发明提供了可用于治疗尿频和尿失禁的三环化合物,其由通式(I)表示:(其中R 1表示氢,取代或未取代的低级烷基等; X 1 -X 2 -X 3表示CR 5 (其中R5,R6,R7和R8可以相同或不同,各自代表氢,取代的或未取代的低级烷基,羟基,取代的或未取代的低级烷氧基等),N(O)= CR6- m = CR 5 -CR 6 -CR 7(其中R 5,R 6和R 7具有与上述定义相同的含义,并且m表示0或1),S-CR 7 = CR 8(其中R 7和R 8具有与上述定义相同的含义)等 ;当R2代表氢时,取代或未取代的低级烷基,取代或未取代的低级烷氧基,取代或未取代的N-取代的杂环基,(其中n是0或1; R3和R4可以相同或不同, 各自代表氢,取代或未取代的低级烷基,t 三氟甲基等,或者R3和R4可以结合在一起形成环烷基; Q表示羟基,卤素等)等,Y表示-CH 2 SO 2 - , - SCH 2 - , - SOCH 2 - ,-SO 2 CH 2 - 等)及其药学上可接受的盐。