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19 条记录 (耗时 0.034 秒)

    3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one derivatives for the modulation of the activity of protein kinases
    13.
    发明授权
    3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one derivatives for the modulation of the activity of protein kinases 有权
    3,4-二氢-2H-吡咯并[1,2-a]吡嗪-1-酮衍生物，用于调节蛋白激酶的活性

    公开(公告)号：US08394802B2

    公开(公告)日：2013-03-12

    申请号：US13119849

    申请日：2009-09-17

    申请人： Danilo Mirizzi ,  Giovanni Cervi ,  Matteo D'Anello ,  Gianluca Mariano Enrico Papeo ,  Ron Ferguson ,  Francesco Casuscelli

    发明人： Danilo Mirizzi ,  Giovanni Cervi ,  Matteo D'Anello ,  Gianluca Mariano Enrico Papeo ,  Ron Ferguson ,  Francesco Casuscelli

    IPC分类号： A61K31/495

    CPC分类号： A61K31/4985 ,  A61K45/06 ,  C07D487/04

    摘要： Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds with the formula 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： 具有下式或其药学上可接受的盐的3,4-二氢-2H-吡咯并[1,2-a]吡嗪-1-酮化合物的4,7-二取代衍生物，其制备方法和包含它们的药物组合物是 披露; 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。

    Substituted pyrazolo-quinazoline derivatives as kinase inhibitors
    16.
    发明授权
    Substituted pyrazolo-quinazoline derivatives as kinase inhibitors 有权
    取代的吡唑并喹唑啉衍生物作为激酶抑制剂

    公开(公告)号：US08541576B2

    公开(公告)日：2013-09-24

    申请号：US13327979

    申请日：2011-12-16

    申请人： Francesco Casuscelli ,  Claudia Piutti ,  Antonella Ermoli ,  Daniela Faiardi

    发明人： Francesco Casuscelli ,  Claudia Piutti ,  Antonella Ermoli ,  Daniela Faiardi

    IPC分类号： C07D487/04 ,  A61K31/517

    CPC分类号： C07D487/04

    摘要： The present invention relates to substituted pyrazolo[4,3-h]quinazoline compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular PIM kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.

    摘要翻译： 本发明涉及调节蛋白激酶活性的取代吡唑并[4,3-h]喹唑啉化合物，因此可用于治疗由失调蛋白激酶活性引起的疾病，特别是PIM激酶。 本发明还提供了制备这些化合物的方法，包含这些化合物的药物组合物，以及使用这些化合物治疗疾病的方法或含有它们的药物组合物的方法。

    [1,2,4]TRIAZOLO[1,5-C]PYRIMIDINE DERIVATIVES AS HSP90 MODULATORS
    18.
    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。