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    [1,2,4]TRIAZOLO[1,5-C]PYRIMIDINE DERIVATIVES AS HSP90 MODULATORS
    33.
    发明申请
    [1,2,4]TRIAZOLO[1,5-C]PYRIMIDINE DERIVATIVES AS HSP90 MODULATORS 审中-公开
    [1,2,4]三唑并[1,5-C]嘧啶衍生物作为HSP90调节剂

    公开(公告)号：US20140045836A1

    公开(公告)日：2014-02-13

    申请号：US14055388

    申请日：2013-10-16

    申请人： Elena Casale ,  Francesco Casuscelli ,  Claudio Dalvit ,  Paolo Polucci ,  Fabio Zuccotto

    发明人： Elena Casale ,  Francesco Casuscelli ,  Claudio Dalvit ,  Paolo Polucci ,  Fabio Zuccotto

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04

    摘要： The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives which inhibit the activity of Heat Shock Protein Hsp90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, methods of treating diseases and the pharmaceutical compositions comprising these compounds.

    摘要翻译： 本发明涉及抑制热休克蛋白Hsp90活性的[1,2,4]三唑并[1,5-c]嘧啶衍生物。 因此，本发明的化合物可用于治疗增殖性疾病如癌症和神经变性疾病。 本发明还提供了制备这些化合物的方法，治疗疾病的方法和包含这些化合物的药物组合物。

    TRICYCLOPYRAZOLE DERIVATIVES
    35.
    发明申请
    TRICYCLOPYRAZOLE DERIVATIVES 有权
    三甲基吡唑衍生物

    公开(公告)号：US20120277214A1

    公开(公告)日：2012-11-01

    申请号：US13512904

    申请日：2010-11-24

    申请人： Teresa Disingrini ,  Sergio Mantegani ,  Mario Varasi

    发明人： Teresa Disingrini ,  Sergio Mantegani ,  Mario Varasi

    IPC分类号： C07D487/14 ,  C40B40/04 ,  A61K31/55 ,  A61K31/551 ,  A61K31/437 ,  A61P25/28 ,  A61K31/541 ,  A61P35/00 ,  A61P35/02 ,  A61P31/18 ,  A61P31/12 ,  A61P37/06 ,  C07D471/14 ,  A61K31/496

    CPC分类号： C07D487/14 ,  C07D207/34 ,  C07D471/14

    摘要： Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.

    摘要翻译： 公开了作为三环吡唑衍生物或其药学上可接受的盐的化合物，其制备方法和包含它们的药物组合物; 这些化合物可用于治疗由改变的蛋白激酶活性引起的和/或与其相关的疾病，例如癌症，病毒感染，HIV感染个体中的AIDS发展的预防，细胞增殖性疾病，自身免疫和神经变性疾病; 还公开了用于制备本发明化合物的固相合成条件和包含多个化合物的化学文库的方法。

    1H-furo[3,2-C]pyrazole compounds useful as kinase inhibitors
    40.
    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。