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    Benzoxazoles and oxazolopyridines being useful as janus kinases inhibitors
    46.
    发明授权
    Benzoxazoles and oxazolopyridines being useful as janus kinases inhibitors 失效
    苯并恶唑和恶唑啉吡啶可用作甘油激酶抑制剂

    公开(公告)号：US08629168B2

    公开(公告)日：2014-01-14

    申请号：US12440298

    申请日：2007-09-13

    申请人： Marc Gerspacher ,  Pascal Furet ,  Eric Vangrevelinghe

    发明人： Marc Gerspacher ,  Pascal Furet ,  Eric Vangrevelinghe

    IPC分类号： C07D263/58 ,  C07D263/60 ,  C07D413/00 ,  C07D498/00 ,  A01N43/76 ,  A61K31/42

    CPC分类号： C07D263/58 ,  C07D413/04

    摘要： The invention relates to 2,7-disubstituted benzoxazole and 2,4-disubstituted oxazolo[5,4-c]pyridine compounds of the formula I given below, as well as salts thereof, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, these compounds for use in the treatment (including prophylaxis) of the animal, especially human, body (especially with regard to a proliferative disease), the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a protein tyrosine kinase mediated disease (such as a tumor disease) or for the manufacture of a pharmaceutical preparation for use in the treatment of such a disease, a method for the treatment of such a disease and a pharmaceutical preparation for the treatment of a disease as mentioned. The compounds are of the formula I, wherein the symbols are as defined in the description. The compounds inhibit, for example, JAK2 and JAK3.

    摘要翻译： 本发明涉及以下给出的式I的2,7-二取代苯并恶唑和2,4-二取代的恶唑并[5,4-c]吡啶化合物及其盐，其制备方法及其在 用于治疗人或动物体的方法，这些化合物用于动物，特别是人体（特别是关于增殖性疾病）的治疗（包括预防）中，单独使用或与一种 或更多其它药物活性化合物 - 用于治疗特别是蛋白质酪氨酸激酶介导的疾病（例如肿瘤疾病）或用于制备用于治疗这种疾病的药物制剂的治疗方法 用于治疗所述疾病的疾病和药物制剂。 所述化合物具有式I，其中符号如说明书中所定义。 该化合物抑制例如JAK2和JAK3。

    Inhibitors of tyrosine kinases
    48.
    发明授权
    Inhibitors of tyrosine kinases 有权
    酪氨酸激酶抑制剂

    公开(公告)号：US07956053B2

    公开(公告)日：2011-06-07

    申请号：US12489049

    申请日：2009-06-22

    申请人： Werner Breitenstein ,  Pascal Furet ,  Sandra Jacob ,  Paul W Manley

    发明人： Werner Breitenstein ,  Pascal Furet ,  Sandra Jacob ,  Paul W Manley

    IPC分类号： C07D401/04 ,  A61K31/506

    CPC分类号： C07D401/14 ,  C07D405/14

    摘要： The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such a disease.

    摘要翻译： 本发明涉及下式的化合物，其中取代基R 1，R 2和R 4具有本发明说明书中阐述和解释的含义，制备这些化合物的方法，含有它们的药物组合物，其任选组合的用途 与一种或多种用于治疗对蛋白激酶活性，特别是肿瘤性疾病，特别是白血病的抑制作出反应的疾病的其它药学活性化合物，以及治疗这种疾病的方法。