Use of tetrahydrocarbazone derivatives as 5HT.sub.1 receptor agonists
    12.
    发明授权
    Use of tetrahydrocarbazone derivatives as 5HT.sub.1 receptor agonists 失效
    四氢咔唑衍生物作为5HT1受体激动剂的用途

    公开(公告)号:US5464864A

    公开(公告)日:1995-11-07

    申请号:US167846

    申请日:1993-12-23

    CPC分类号: C07D209/88

    摘要: ##STR1## Use of a compound of general formula (I), wherein R
    1 represents hydrogen, halogen, trifluoromethyl, nitro, hydroxy, C
    1-6 alkyl, C
    1-6 alkoxy, arylC
    1-6 alkoxy, --CO
    2 R
    4 , --(CH
    2 )
    n CN, --(CH
    2 )
    n CONR
    5 R
    6 , --(CH
    2 )
    n SO
    2 NR
    5 R
    6 , C
    1-6 alkanoylamino(CH
    2 )
    n , or C
    1-6 alkylsulphonylamino(CH
    2 )
    n ; R
    4 represents hydrogen, C
    1-6 alkyl or arylC
    1-6 alkyl; R
    5 and R
    6 each independently represent hydrogen or C
    1-6 alkyl, or R
    5 and R
    6 together with the nitrogen atom to which they are attached form a ring; n represents 0, 1 or 2; and R
    2 and R
    3 each independently represent hydrogen, C
    1-6 alkyl; or benzyl or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or hexahydroazepino ring; or a physiologically acceptable salt thereof, in the manufacture of a medicament for the treatment of a condition where a 5-HT
    1 -like agonist is indicated, for example migraine. Novel compounds of formula (I), processes for preparing them and pharmaceutical compositions containing them are also described.

    摘要翻译: PCT No.PCT / GB92 / 01082 Sec。 371日期:1993年12月23日 102(e)日期1993年12月23日PCT提交1992年6月17日PCT公布。 第WO93 / 00086号公报 (I)通式(I)的化合物的用途,其中R 1表示氢,卤素,三氟甲基,硝基,羟基,C 1-6烷基,C 1-6烷氧基,芳基C 1-6烷氧基, (CH2)nCN, - (CH2)nCONR5R6, - (CH2)nSO2NR5R6,C1-6烷酰基氨基(CH2)n或C1-6烷基磺酰基氨基(CH2)n; R 4表示氢,C 1-6烷基或芳基C 1-6烷基; R 5和R 6各自独立地表示氢或C 1-6烷基,或者R 5和R 6与它们所连接的氮原子一起形成环; n表示0,1或2; 并且R 2和R 3各自独立地表示氢,C 1-6烷基; 或苄基或与它们所连接的氮原子一起形成吡咯烷子基,哌啶子基或六氢氮杂环; 或其生理上可接受的盐在制备用于治疗其中指示5-HT1样激动剂的病症的药物中,例如偏头痛。 还描述了新的式(I)化合物,其制备方法和含有它们的药物组合物。