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    Sulphonamidoaniline Derivatives Being Janus Kinase Inhibitors
    6.
    发明申请
    Sulphonamidoaniline Derivatives Being Janus Kinase Inhibitors 审中-公开
    磺酰胺苯胺衍生物作为Janus激酶抑制剂

    公开(公告)号：US20080261973A1

    公开(公告)日：2008-10-23

    申请号：US12158764

    申请日：2006-12-20

    申请人： Hans-Georg Capraro ,  Bernard Coupez ,  Pascal Furet ,  Paul W. Manley ,  Carole Pissot Soldermann

    发明人： Hans-Georg Capraro ,  Bernard Coupez ,  Pascal Furet ,  Paul W. Manley ,  Carole Pissot Soldermann

    IPC分类号： C07D473/32 ,  C07D487/04 ,  A61K31/52 ,  A61K31/5377

    CPC分类号： C07D473/16 ,  C07D473/18 ,  C07D487/04 ,  C07D519/00

    摘要： 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, R1 represents NR4R5 or OR4, wherein R4 represents optionally substituted alkyl, optionally substituted cycloalkyl optionally comprising one or two nitrogen or oxygen atoms, or substituted aryl, and R5 represents hydrogen or unsubstituted or substituted alky, or R4 and R5 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, R2 is hydrogen, lower alkenyl or alkyl, R3 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.

    摘要翻译： 本发明涉及式I的磺酰氨基苯胺，其中A是N或CH，W，X，Y和Z是N或CH，条件是三个符号W，X和Y中的至少一个表示CH， 1表示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原子或氧原子的任选取代的环烷基或取代的芳基，R 5表示氢或未取代或取代的烷基，或R 4和R 3， 与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，R 2是氢，低级烯基或烷基，R 3是未被取代的或被卤素单 - ，二 - 或三取代的烷基; 烯基或芳基，及其盐; 其制备方法，它们在人体或动物体内的治疗中的应用，单独使用或与一种或多种其它药学活性化合物组合用于治疗疾病，治疗这种疾病的方法和 使用这种化合物单独或与一种或多种其它药学活性化合物组合，用于制备用于治疗增殖性疾病的药物制剂。

    Use of Pyrimidylaminobenzamide Derivatives for the Treatment of Fibrosis
    10.
    发明申请
    Use of Pyrimidylaminobenzamide Derivatives for the Treatment of Fibrosis 审中-公开
    使用嘧啶基氨基苯甲酰胺衍生物治疗纤维化

    公开(公告)号：US20110124670A1

    公开(公告)日：2011-05-26

    申请号：US13054011

    申请日：2009-07-14

    申请人： Elisabeth Buchdunger ,  Paul W. Manley

    发明人： Elisabeth Buchdunger ,  Paul W. Manley

    IPC分类号： A61K31/506 ,  A61P11/00 ,  A61P1/16

    CPC分类号： A61K31/506 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/4184 ,  A61K45/06 ,  A61K2300/00

    摘要： The invention relates to the use of a pyrimidylaminobenzamides of formula I wherein the radicals have the meanings as defined herein, or of a pharmaceutically acceptable salt thereof for the manufacture of pharmaceutical compositions for use in the treatment of fibrosis, to the use of a pyrimidylaminobenzamides of formula I or pharmaceutically acceptable salt thereof in the treatment of fibrosis, to a method of treating warm-blooded animals including humans suffering from fibrosis by administering to a said animal in need of such treatment an effective dose of a pyrimidylaminobenzamide of formula I or a pharmaceutically acceptable salt thereof, and to combinations comprising (a) at least one pyrimidylaminobenzamides of formula I as and (b) at least one compound selected form AT1-receptor antagonists and ACE inhibitors and the use of such combinations in the treatment of fibrosis, in particular hepatic fibrosis.

    摘要翻译： 本发明涉及式I的嘧啶基氨基苯甲酰胺的用途，其中基团具有如本文所定义的含义或其药学上可接受的盐在制备用于治疗纤维化的药物组合物中的用途，使用嘧啶基氨基苯甲酰胺 式I或其药学上可接受的盐在治疗纤维化中的用途，涉及一种通过向需要这种治疗的所述动物施用有效剂量的式I的嘧啶基氨基苯甲酰胺或其药学上可接受的方法来治疗包括患有纤维化的人的温血动物 和（a）至少一种式I的嘧啶基氨基苯甲酰胺和（b）至少一种选自AT1受体拮抗剂和ACE抑制剂的化合物，以及这些组合在治疗纤维化中的用途，特别是 肝纤维化。