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    Pharmaceutically active benzsulfonamide derivatives as inhibitors of protein junkinases
    5.
    发明授权
    Pharmaceutically active benzsulfonamide derivatives as inhibitors of protein junkinases 失效
    药物活性苯并磺酰胺衍生物作为蛋白质垃圾酶的抑制剂

    公开(公告)号：US07417058B2

    公开(公告)日：2008-08-26

    申请号：US10381197

    申请日：2001-09-27

    申请人： Serge Halazy ,  Dennis Church ,  Stephen J. Arkinstall ,  Marco Biamonte ,  Montserrat Camps ,  Jean-Pierre Gotteland ,  Thomas Rueckle

    发明人： Serge Halazy ,  Dennis Church ,  Stephen J. Arkinstall ,  Marco Biamonte ,  Montserrat Camps ,  Jean-Pierre Gotteland ,  Thomas Rueckle

    IPC分类号： A61K31/445 ,  A61P25/00 ,  A61P37/00 ,  C07D211/96

    CPC分类号： C07D211/96

    摘要： The present invention is related to benzsulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzsulfonamide derivatives. Said benzsulfonamide derivatives are ef-ficient modulators of the JNK pathway, they are in particular efficient and selective in-hibitors of JNK 2 and 3. The present invention is furthermore related to novel benzsul-fonamide derivatives as well as to methods of their preparation (I). The compounds of formula I according to the present invention being suitable pharma-ceutical agents are those wherein Ar1 is a substituted or unsubstituted aryl or heteroaryl group. X is O or S, preferably O.R1 is hydrogen or a C1-C6-alkyl group, preferably H.R2 is hydrogen, —COOR3, —CONR3R3′, OH, a C1-C4 alkyl substituted with an OH group, a hydrazido carbonyl group, a sulfate, a sulfonate, an amine or an ammonium salt; n is either 0 or 1, preferably 1.

    摘要翻译： 本发明涉及式I的苯并磺酰胺衍生物，其特别用作药物活性化合物，以及含有该苯磺酰胺衍生物的药物制剂。 所述苯磺酰胺衍生物是JNK途径的有效调节剂，它们特别是JNK 2和3的有效和选择性的抑制剂。本发明还涉及新型苯磺酰脲衍生物及其制备方法（ 一世）。 根据本发明的式I化合物是合适的制药剂，其中Ar 1是取代或未取代的芳基或杂芳基。 X是O或S，优选O.R1是氢或C1-C6-烷基，优选H.R2是氢，-COOR3，-CONR3R3'，OH，被OH基取代的C1-C4烷基，肼基 羰基，硫酸酯，磺酸酯，胺或铵盐; n为0或1，优选为1。