Benzoxazoles and oxazolopyridines being useful as janus kinases inhibitors
    52.
    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

    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
    54.
    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

    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。

    Phenylacetamides being FLT3 Inhibitors
    56.
    发明申请
    Phenylacetamides being FLT3 Inhibitors 失效
    苯乙酰胺是FLT3抑制剂

    公开(公告)号:US20100075980A1

    公开(公告)日:2010-03-25

    申请号:US12445545

    申请日:2007-10-15

    CPC分类号: C07D471/04 C07D235/06

    摘要: Compounds of formula wherein the residues R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, salts thereof; their use, methods of their use, processes for their production, pharmaceutical compositions comprising them, their combinations with second drug substances and the use thereof and the like. The compounds are protein kinase inhibitors and can be used for the treatment of diseases mediated by protein kinase inhibitors, e.g. for the treatment of various proliferative diseases.

    摘要翻译: 其中残基R 1,R 2,R 3,R 9,R 10和Q和X,Y和Z如说明书中所定义,其盐; 其用途,使用方法,其制备方法,包含它们的药物组合物,其与第二药物物质的组合及其用途等。 这些化合物是蛋白激酶抑制剂,可用于治疗由蛋白激酶抑制剂介导的疾病,例如, 用于治疗各种增殖性疾病。

    DISUBSTITUTED UREAS AS KINASE INHIBITORS
    60.
    发明申请
    DISUBSTITUTED UREAS AS KINASE INHIBITORS 审中-公开
    作为激酶抑制剂的消除性尿路炎

    公开(公告)号:US20090131437A1

    公开(公告)日:2009-05-21

    申请号:US11813067

    申请日:2006-01-03

    IPC分类号: A61K31/5377 C07D413/14

    摘要: The invention relates to compounds of the formula (I), their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.

    摘要翻译: 本发明涉及式(I)化合物,其作为激酶抑制剂的用途,包含所述化合物的新药物制剂,用于诊断或治疗温血动物,特别是人的所述化合物,其用于治疗 疾病或用于制造可用于治疗对激酶活性调节作出反应的疾病的药物制剂,包括将所述化合物施用于温血动物,特别是人的治疗方法,以及所述化合物的制备方法。