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1. 发明申请

WO2011092120A1 6,7- DIHYDROIMIDAZO [1,5-A] PYRAZIN-8 (5H) - ONE DERIVATIVES AS PROTEIN KINASE MODULATORS 审中-公开
标题翻译： 6,7-二氢吲哚并[1,5-A]吡嗪-8（5H） - 一种衍生物作为蛋白激酶调节剂
公开(公告)号：WO2011092120A1
公开(公告)日：2011-08-04
申请号：PCT/EP2011/050846
申请日：2011-01-21
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , MIRIZZI, Danilo , ORRENIUS, Sten Christian , TRIFIRO', Paolo
发明人： MIRIZZI, Danilo , ORRENIUS, Sten Christian , TRIFIRO', Paolo
IPC分类号： C07D487/04 , A61K31/4985 , A61P35/00
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。

2. 发明申请

WO2010010154A1 3,4-DIARYLPYRAZOLES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的3,4-二氨基吡唑
公开(公告)号：WO2010010154A1
公开(公告)日：2010-01-28
申请号：PCT/EP2009/059506
申请日：2009-07-23
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , PULICI, Maurizio , ZUCCOTTO, Fabio , BADARI, Alessandra , NUVOLONI, Stefano , CERVI, Giovanni , TRAQUANDI, Gabriella , BIONDARO, Sonia , TRIFIRO', Paolo , MARCHIONNI, Chiara , MODUGNO, Michele
发明人： PULICI, Maurizio , ZUCCOTTO, Fabio , BADARI, Alessandra , NUVOLONI, Stefano , CERVI, Giovanni , TRAQUANDI, Gabriella , BIONDARO, Sonia , TRIFIRO', Paolo , MARCHIONNI, Chiara , MODUGNO, Michele
IPC分类号： C07D401/04 , C07D403/04 , C07D407/14 , C07D409/14 , A61K31/4439 , A61P35/00
CPC分类号： C07D401/04 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/506 , A61K31/635 , A61K45/06 , C07D401/14 , C07D403/04 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D513/14
摘要： 3,4-diarylpyrazole 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：公开了说明书中定义的式（I）的3,4-二芳基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。

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