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    • 2. 发明申请
    • TETRAHYDROCARBAZOLE DERIVATIVES AS 5-HT1-LIKE AGONISTS
    • 四氢叶酸衍生物作为5-HT1样激动剂
    • WO1994014773A1
    • 1994-07-07
    • PCT/EP1993003628
    • 1993-12-16
    • SMITHKLINE BEECHAM PLCPORTER, Roderick, AlanVIMAL, Mythily
    • SMITHKLINE BEECHAM PLC
    • C07D209/88
    • C07D209/88
    • Compounds of formula (I), wherein R represents halogen, C1-4alkyl, C1-4alkoxy, hydroxy, NO2, -NR R , R R NCO(CH2)m-, R R NSO2(CH2)m-, R CONH(CH2)-m or R SO2NH(CH2)m-; R and R each independently hydrogen or C1-4alkyl or NR<>4 represents a 5- to 7-membered heterocyclic ring; R represents hydrogen or C1-4alkyl; R represents C1-4alkyl; m is zero, 1 or 2; n is zero or 1 to 5; R and R each independently represent hydrogen, C1-6alkyl or benzyl or -NR R represents a pyrrolidino, piperidino or hexahydroazepino ring; and A represents a bond, a C1-5alkylene chain or a C3-5alkenyle chain wherein the double bond is not adjacent the nitrogen atom; and salts thereof have affinity for the 5-HT1-like receptor and are useful e.g. in the treatment of migraine.
    • 式(I)化合物,其中R 1表示卤素,C 1-4烷基,C 1-4烷氧基,羟基,NO 2,-NR 4 R 5,R 4 R 5 NCO(CH 2)m - ,R 4 R 5 NSO 2(CH 2)m - ,R 6 CONH(CH 2)m或R 7 SO 2 NH(CH 2)m - ; R 4和R 5各自独立地为氢或C 1-4烷基或NR <4 表示5-至7-元杂环; R 6表示氢或C 1-4烷基; R 7表示C 1-4烷基; m为零,1或2; n为0或1〜5; R 2和R 3各自独立地表示氢,C 1-6烷基或苄基或-NR 2 R 3表示吡咯烷子基,哌啶子基或六氢氮杂环环。 A表示键,C1-5亚烷基链或C3-5链烯基链,其中双键不与氮原子相邻; 其盐对5-HT1样受体具有亲和力,并且可用于例如 在治疗偏头痛。