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    • 9. 发明公开
    • TRICYCLIC COMPOUNDS
    • TRIZYKLISCHE VERBINDUNGEN
    • EP0979821A4
    • 2002-04-24
    • EP98914022
    • 1998-04-15
    • KYOWA HAKKO KOGYO KK
    • YOSHIDA MAKOTOSEISHI TAKASHIAONO SHIGERUTAKAI HARUKISUZUKI KOJIYAMAGATA TSUYOSHIATSUKI KAORUKARASAWA AKIRAKUMAZAWA TOSHIAKI
    • C07D313/12C07D337/12C07D495/04A61K31/335A61K31/38A61K31/435C07D333/06C07D333/12
    • C07D495/04C07D313/12C07D337/12
    • Tricyclic compounds of general formula (I) and pharmacologically acceptable salts thereof, which are useful for the treatment of pollakiuria and enuresis, wherein R1 is hydrogen, substituted or unsubstituted lower alkyl or the like; X?1-X2-X3 is CR5= CR6-CR7=CR8¿ (wherein R?5, R6, R7 and R8¿ are each independently hydrogen, substituted or unsubstituted lower alkyl, hydroxyl, substituted or unsubstituted lower alkoxy or the like), N(O)¿m?=CR?5-CR6-CR7¿ (wherein R?5, R6 and R7¿ are each the same as defined above; and m is 0 to 1), S-CR7=CR8 (wherein R?7 and R8¿ are each the same as defined above) or the like; R2 is hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, a substituted or unsubstituted N-substituted heterocyclic group or a group of general formula (a); (wherein n is 0 or 1; R?3 and R4¿ are each independently hydrogen, substituted or unsubstituted lower alkyl, trifluoromethyl or the like, or alternatively R?3 and R4¿ may be united to form cyclic alkyl; and Q is hydroxyl, halogeno or the like); and Y is -CH¿2?SO2-, -SCH2-, -SOCH2-, -SO2CH2- or the like.
    • 通式(I)的三环化合物及其药理学上可接受的盐,其可用于治疗尿频和遗尿,其中R 1为氢,取代或未取代的低级烷基等; X 1 -X 2 -X 3是CR 5 = CR 6 -CR 7 = CR 8(其中R 5,R 6,R 7和R 8各自独立地为氢,取代或未取代的低级烷基,羟基,取代或未取代的低级烷氧基等) (式中,R 5,R 6和R 7各自与上述定义相同,m为0〜1),S-CR 7 = CR 8(式中, R 7和R 8各自与上述定义相同)等; R2是氢,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-取代杂环基或通式(a)的基团; (其中n是0或1; R 3和R 4各自独立地是氢,取代或未取代的低级烷基,三氟甲基等,或者R 3和R 4可以结合形成环状烷基; Q是羟基 ,卤代或诸如此类); Y是-CH 2 SO 2 - , - SCH 2 - , - SOCH 2 - ,-SO 2 CH 2 - 等。