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    1H-furo[3,2-C]pyrazole compounds useful as kinase inhibitors
    2.
    发明授权
    1H-furo[3,2-C]pyrazole compounds useful as kinase inhibitors 有权
    可用作激酶抑制剂的1H-呋喃并[3,2-C]吡唑化合物

    公开(公告)号：US08119641B2

    公开(公告)日：2012-02-21

    申请号：US12302569

    申请日：2007-05-25

    申请人： Daniele Fancelli ,  Maurizio Pulici ,  Jürgen Moll ,  Tiziano Bandiera

    发明人： Daniele Fancelli ,  Maurizio Pulici ,  Jürgen Moll ,  Tiziano Bandiera

    IPC分类号： A61K31/4162 ,  A61K31/427 ,  A61K31/496 ,  C07D491/048 ,  C07D277/44 ,  C07D295/135 ,  C07D417/10 ,  C07D403/14

    CPC分类号： C07D491/048

    摘要： Furo[3,2-c]pyrazole derivatives of formula (I) as defined in the description, and pharmaceutically acceptable salts thereof, wherein A is an aryl or heteroaryl ring, —NHZR5 is at the ortho position to the CONH linker; —R1 and R2 are the same or different and, independently from each other, represent a hydrogen atom, or an organic residue; R3 is a hydrogen or halogen atom or an organic group; R4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C═O, or —C(═O)NH—; —R5 is hydrogen or an optionally substituted organic group or isomers, tautomers, carriers, metabolites, prodrugs, and pharmaceutically acceptable salts thereof. A process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Aurora kinases activity or IGF-1R activity, like cancer.

    摘要翻译： 如描述中定义的式（I）的呋喃并[3,2-c]吡唑衍生物及其药学上可接受的盐，其中A是芳基或杂芳基环，-NHZR5位于与CONH接头的邻位; -R 1和R 2相同或不同，彼此独立地表示氢原子或有机残基; R3是氢或卤素原子或有机基团; R4是氢或卤素原子或有机基团; Z是直接键合，> C = O或-C（= O）NH-; -R5是氢或任选取代的有机基团或其异构体，互变异构体，载体，代谢物，前药及其药学上可接受的盐。 公开了其制备方法和包含它们的药物组合物; 本发明的化合物在治疗中可用于治疗与失调的蛋白激酶活性，特别是Aurora激酶活性或IGF-1R活性相关的疾病，如癌症。

    Bicyclic pyrazoles as protein kinase inhibitors
    10.
    发明授权
    Bicyclic pyrazoles as protein kinase inhibitors 有权
    双环吡唑作为蛋白激酶抑制剂

    公开(公告)号：US08524707B2

    公开(公告)日：2013-09-03

    申请号：US13140915

    申请日：2009-12-17

    申请人： Maurizio Pulici ,  Chiara Marchionni ,  Claudia Piutti ,  Fabio Gasparri

    发明人： Maurizio Pulici ,  Chiara Marchionni ,  Claudia Piutti ,  Fabio Gasparri

    IPC分类号： C07D513/04 ,  A61K31/429

    CPC分类号： C07D513/04

    摘要： 3,4-diaryl-bicyclicpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

    摘要翻译： 公开了本说明书中定义的式（I）的3,4-二芳基 - 双环吡唑衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物在治疗中可用于治疗与失调的蛋白激酶活性相关的疾病，如癌症。