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    Indole derivatives
    8.
    发明授权
    Indole derivatives 失效
    吲哚衍生物

    公开(公告)号：US5457115A

    公开(公告)日：1995-10-10

    申请号：US208529

    申请日：1994-03-09

    申请人： Jens K. Perregaard ,  Kim Andersen ,  Klaus P. Boegesoe ,  Henrik Pedersen

    发明人： Jens K. Perregaard ,  Kim Andersen ,  Klaus P. Boegesoe ,  Henrik Pedersen

    IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  A61K31/445 ,  C07D403/04 ,  C07D403/14

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

    摘要： A substituted indole compound having the formula I: ##STR1## where Ar is one of a phenyl group, a phenyl group substituted with at least one substituent selected from halogen, lower alkyl, lower alkoxy, hydroxy, trifluoromethyl, and cyano, and a hetero aromatic group selected from 2-thienyl, 3-thienyl, 2-furanyl, 3-furanyl, 2-oxazolyl, 2-imidazolyl, 2-pyridyl, 3-pyridyl, and 4-pyridyl; each dotted line is an optional double bond; X and X' are independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, lower alkylthio, lower alkylsulfonyl, lower alkylamino, lower dialkylamino, cyano, trifluoromethyl, and trifluoromethylthio; or X and X' are taken together to form a 5 to 7 membered carbocyclic ring; R.sup.1 is selected from the group consisting of hydrogen, lower alkyl and lower alkyl substituted with one or two hydroxy groups; with the proviso that when X is hydrogen or fluoro then R.sup.1 cannot be hydrogen; R is a substituent having the formula Ib: ##STR2## wherein n is an integer from 2-6 inclusive; W is oxygen or sulfur; V.sup.1 is selected from OR.sup.4, SR.sup.5, CHR.sup.6 R.sup.7, and NR.sup.8 R.sup.9 ;wherein R.sup.3 to R.sup.9 are independently selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, cycloalkyl, lower alkyl substituted with one or two hydroxyl groups, and lower alkenyl substituted with one or two hydroxyl groups; and pharmaceutically acceptable acid addition salts or prodrugs thereof for the therapeutic treatment of CNS disorders.

    摘要翻译： 具有式I的取代的吲哚化合物：其中Ar是苯基，被至少一个选自卤素，低级烷基，低级烷氧基，羟基，三氟甲基和氰基的取代基取代的苯基，和 杂芳基选自2-噻吩基，3-噻吩基，2-呋喃基，3-呋喃基，2-恶唑基，2-咪唑基，2-吡啶基，3-吡啶基和4-吡啶基; 每个虚线是可选的双键; X和X'独立地选自氢，卤素，低级烷基，低级烷氧基，羟基，低级烷硫基，低级烷基磺酰基，低级烷基氨基，低级二烷基氨基，氰基，三氟甲基和三氟甲硫基。 或X和X'一起形成5至7元碳环; R1选自氢，低级烷基和被一个或两个羟基取代的低级烷基; 条件是当X是氢或氟时，则R1不能是氢; R是具有式Ib的取代基：其中n是2-6的整数; W是氧或硫; V1选自OR4，SR5，CHR6R7和NR8R9; 其中R3至R9独立地选自氢，低级烷基，低级烯基，环烷基，被一个或两个羟基取代的低级烷基和被一个或两个羟基取代的低级烯基; 和其药学上可接受的酸加成盐或前药用于治疗CNS疾病。