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    • 8. 发明申请
    • SULPHONAMIDOANILINE DERIVATIVES BEING JANUS KINASES INHIBITORS
    • 磺酰胺衍生物是JANUS KINASES抑制剂
    • WO2007071393A2
    • 2007-06-28
    • PCT/EP2006/012311
    • 2006-12-20
    • NOVARTIS AGNOVARTIS PHARMA GMBHCAPRARO, Hans-GeorgCOUPEZ, BernardFURET, PascalMANLEY, Paul, W.PISSOT SOLDERMANN, Carole
    • CAPRARO, Hans-GeorgCOUPEZ, BernardFURET, PascalMANLEY, Paul, W.PISSOT SOLDERMANN, Carole
    • C07D473/16C07D473/18C07D487/04C07D519/00A61K31/5377
    • C07D473/16C07D473/18C07D487/04C07D519/00
    • The invention relates to sulphonamidoanilines of formula (I) wherein A is N or CH, W, X, Y and Z are N or CH under the proviso that at least one of the three symbols W, X and Y represent CH, R 1 represents NR 4 R 5 or OR 4 , wherein R 4 represents optionally substituted alkyl, optionally substituted cycloalkyl optionally comprising one or two nitrogen or oxygen atoms, or substituted aryl, and R 5 represents hydrogen or unsubstituted or substituted alkyl, or R 4 and R 5 together with the nitrogen to which they are attached represent an optionally substituted five- or six-membered nitrogen containing monocyclic ring, an optionally substituted nitrogen containing fully saturated bicyclic ring, or an spirocyclic fully saturated ring system containing one or two nitrogen atoms, R 2 is hydrogen, lower alkenyl or alkyl, R 3 is alkyl which is unsubstituted or mono-, di- or trisubstituted by halogen; alkenyl or aryl, and their salts; processes for their preparation, their application in the treatment of the human or animal body, the use thereof - alone or in combination with one or more other pharmaceutically active compounds - for the treatment of diseases, a method for the treatment of such a disease and the use of such a compound - alone or in combination with one or more other pharmaceutically active compounds - for the manufacture of a pharmaceutical preparation for the treatment of a proliferative disease.
    • 本发明涉及式(I)其中A是N或CH,W,X,Y和Z的sulphonamidoanilines是N或CH,条件下,所述三个符号W,X中的至少一个 Y代表CH,R 1代表NR 4 R 5或OR 4,其中R 4 表示任选取代的烷基,任选包含一个或两个氮或氧原子的任选取代的环烷基或取代的芳基,并且R5表示氢或未取代或取代的烷基,或R 4 R 5和它们所连接的氮一起代表任选取代的五元或六元含氮单环,任选取代的含氮完全饱和双环或 含有一个或两个氮原子的螺环全饱和环体系,R 2是氢,低级链烯基或烷基,R 3是未取代的或者单 - ,二 - 或三 - trisubstit 被卤素所阻挡; 烯基或芳基,及其盐; 它们的制备方法,它们在人体或动物体的治疗中的应用,单独或与一种或多种其它药物活性化合物组合用于治疗疾病的方法,治疗这种疾病的方法和 单独或与一种或多种其它药物活性化合物组合使用这样的化合物用于制备用于治疗增殖性疾病的药物制剂。