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    Therapeutic substituted indole compounds and compositions thereof
    2.
    发明授权
    Therapeutic substituted indole compounds and compositions thereof 失效
    治疗性取代的吲哚化合物及其组合物

    公开(公告)号：US5225431A

    公开(公告)日：1993-07-06

    申请号：US660966

    申请日：1991-02-26

    申请人： Alan D. Robertson ,  Graeme R. Martin ,  Janet S. Buckingham

    发明人： Alan D. Robertson ,  Graeme R. Martin ,  Janet S. Buckingham

    IPC分类号： C07D209/16 ,  C07D403/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06

    CPC分类号： C07D403/06 ,  C07D209/16 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06

    摘要： The present invention is concerned with compounds of formula (I) ##STR1## wherein R, R.sup.1 and R.sup.2 are independently selected from hydrogen and C.sub.1-4 alkyl;R.sup.3 and R.sup.4 are independently selected from hydrogen, C.sub.1-6 alkyl (including cycloalkyl) and aryl (wherein the alkyl or aryl group, which latter includes benzyl, is optionally substituted by one or more atoms or groups independently selected from halogen, C.sub.1-4 alkyl and aryl), provided R.sup.3 benzyl or substituted benzyl when R.sup.4 =H;m is an integer of from 0 to 2;n is an integer of from 0 to 3;(W) is a group of formula (i), (ii), (iii), or (iv) ##STR2## wherein Y is selected from oxygen, methylene and >N--R.sup.5, where R.sup.5 is hydrogen, C.sub.1-4 alkyl, or benzyl, Z and Z' are independently selected from >C.dbd.O, >C.dbd.S and methylene, and the chiral center * in formula (i) or (ii) is in its (S) or (R) form or is a mixture thereof in any proportions;X is a group selected fromaryl (including heteroaryl)xanthenyldibenzofuranyl which group is optionally substituted;and salts and solvates thereof, the preparation of these compounds, pharmaceutical formulations containing them and their use in medicine, particularly in the treatment of migraine.

    摘要翻译： 本发明涉及式（I）化合物：其中R 1，R 2和R 2独立地选自氢和C 1-4烷基; R 3和R 4独立地选自氢，C 1-6烷基（包括环烷基）和芳基（其中后者包括苄基的烷基或芳基任选被一个或多个独立地选自卤素，C 1-4的一个或多个原子或基团取代 烷基和芳基），当R 4 = H时提供R 3苄基或取代的苄基; m为0〜2的整数; n为0〜3的整数， （ⅰ）Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y 选自氧，亚甲基和> N-R5，其中R5是氢，C1-4烷基或苄基，Z和Z'独立地选自C = O，> C = S和亚甲基，手性中心* 在式（ⅰ）或（ⅱ）中为其（S）或（R）形式或其任何比例的混合物; X是选自基团任选取代的芳基（包括杂芳基）呫吨基二苯并呋喃基的基团; 其盐和溶剂合物，这些化合物的制备，含有它们的药物制剂及其在医药中的用途，特别是用于治疗偏头痛。