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    3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one derivatives for the modulation of the activity of protein kinases
    6.
    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。

    6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one derivatives as protein kinase modulators
    8.
    发明授权
    6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one derivatives as protein kinase modulators 有权
    6,7-二氢咪唑并[1,5-a]吡嗪-8（5H） - 酮衍生物作为蛋白激酶调节剂

    公开(公告)号：US08772279B2

    公开(公告)日：2014-07-08

    申请号：US13575181

    申请日：2011-01-21

    申请人： Danilo Mirizzi ,  Sten Christian Orrenius ,  Paolo Trifirò

    发明人： Danilo Mirizzi ,  Sten Christian Orrenius ,  Paolo Trifirò

    IPC分类号： A61K31/55 ,  A61K31/541 ,  A61K31/4985 ,  A61K31/5377 ,  A61P31/00 ,  A61P35/00 ,  C07D487/04 ,  C40B40/04

    CPC分类号： C07D487/04

    摘要： There are provided 3,5-disubstituted derivatives of 6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one compounds of formula (I) or a pharmaceutically acceptable salt thereof as defined in the present specification, which modulate the activity of protein kinases. The compounds are therefore useful in treating diseases caused by dysregulated protein kinase activity. In particular, such diseases to be treated with a compound of formula (I) of the present invention is one caused by and/or associated with disregulated protein kinase activity selected from the group consisting of cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders. The present invention also relates to processes for preparing the compounds of formula (I), combinatorial libraries thereof, pharmaceutical compositions comprising them, and methods of treating diseases utilizing pharmaceutical compositions comprising a compound of formula (I).

    摘要翻译： 提供了本说明书中定义的式（I）的6,7-二氢咪唑并[1,5-a]吡嗪-8（5H） - 酮化合物或其药学上可接受的盐的3,5-二取代衍生物，其中 调节蛋白激酶的活性。 因此，这些化合物可用于治疗由失调的蛋白激酶活性引起的疾病。 特别地，用本发明的式（I）化合物治疗的这些疾病是由选自下组的失调的蛋白激酶活性引起的和/或与其相关的，所述蛋白激酶活性选自癌症，病毒感染，HIV预防艾滋病发展 感染的个体，细胞增殖性疾病，自身免疫和神经变性疾病。 本发明还涉及制备式（I）化合物的方法，其组合文库，包含它们的药物组合物，以及使用包含式（I）化合物的药物组合物治疗疾病的方法。

    6,7-DIHYDROIMIDAZO[1,5-A]PYRAZIN-8(5H)-ONE DERIVATIVES AS PROTEIN KINASE MODULATORS
    9.
    发明申请
    6,7-DIHYDROIMIDAZO[1,5-A]PYRAZIN-8(5H)-ONE DERIVATIVES AS PROTEIN KINASE MODULATORS 有权
    6,7-DIHYDROIMIDAZO [1,5-A]吡嗪-8（5H） - 酮衍生物作为蛋白激酶调节剂

    公开(公告)号：US20130029974A1

    公开(公告)日：2013-01-31

    申请号：US13575181

    申请日：2011-01-21

    申请人： Danilo Mirizzi ,  Sten Christian Orrenius ,  Paolo Trifirò

    发明人： Danilo Mirizzi ,  Sten Christian Orrenius ,  Paolo Trifirò

    IPC分类号： A61K31/4985 ,  A61K31/55 ,  C40B40/04 ,  A61K31/5377 ,  A61P35/00 ,  A61P31/00 ,  C07D487/04 ,  A61K31/541

    CPC分类号： C07D487/04

    摘要： There are provided 3,5-disubstituted derivatives of 6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one compounds of formula (I) or a pharmaceutically acceptable salt thereof as defined in the present specification, which modulate the activity of protein kinases. The compounds are therefore useful in treating diseases caused by dysregulated protein kinase activity. In particular, such diseases to be treated with a compound of formula (I) of the present invention is one caused by and/or associated with disregulated protein kinase activity selected from the group consisting of cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders. The present invention also relates to processes for preparing the compounds of formula (I), combinatorial libraries thereof, pharmaceutical compositions comprising them, and methods of treating diseases utilizing pharmaceutical compositions comprising a compound of formula (I).

    摘要翻译： 提供了本说明书中定义的式（I）的6,7-二氢咪唑并[1,5-a]吡嗪-8（5H） - 酮化合物或其药学上可接受的盐的3,5-二取代衍生物，其中 调节蛋白激酶的活性。 因此，这些化合物可用于治疗由失调的蛋白激酶活性引起的疾病。 特别地，用本发明的式（I）化合物治疗的这些疾病是由选自下组的失调的蛋白激酶活性引起的和/或与其相关的，所述蛋白激酶活性选自癌症，病毒感染，HIV预防艾滋病发展 感染的个体，细胞增殖性疾病，自身免疫和神经变性疾病。 本发明还涉及制备式（I）化合物的方法，其组合文库，包含它们的药物组合物，以及使用包含式（I）化合物的药物组合物治疗疾病的方法。