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公开(公告)号：US20150329552A1
公开(公告)日：2015-11-19
申请号：US14812559
申请日：2015-07-29
IPC分类号： C07D487/14 , C07D207/34 , C07D471/14
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。
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公开(公告)号：US12018023B2
公开(公告)日：2024-06-25
申请号：US17056450
申请日：2019-05-16
发明人： Elena Casale , Francesco Casuscelli , Teresa Disingrini , Paola Magnaghi , Beatrice Malgesini , Ilaria Motto , Stefano Nuvoloni
IPC分类号： C07D471/04 , A61K31/519 , A61K45/06
CPC分类号： C07D471/04 , A61K31/519 , A61K45/06
摘要： The present invention relates to certain substituted heterocondensed pyridone analogues of formula (I) which modulate the activity of Isocitrate Dehydrogenase (IDH). The compounds of this invention are therefore useful in treating diseases caused by mutated IDH1 and/or mutated IDH2 enzyme and/or IDH1 wild type enzyme, in particular cancer, cell proliferative disorders and immune-related disorders. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
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公开(公告)号：US09701686B2
公开(公告)日：2017-07-11
申请号：US14812559
申请日：2015-07-29
IPC分类号： A61K31/55 , C07D487/04 , C07D487/14 , C07D471/14 , C07D207/34
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.
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![Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones as protein kinase inhibitors](/abs-image/US/2015/11/10/US09181258B2/abs.jpg.150x150.jpg)
4.发明授权Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones as protein kinase inhibitors 有权取代的3,4-二氢吡咯并[1,2-a]吡嗪-1（2H） - 酮作为蛋白激酶抑制剂公开(公告)号：US09181258B2
公开(公告)日：2015-11-10
申请号：US14349536
申请日：2012-10-04
发明人： Francesco Casuscelli , Alessandra Badari , Sten Christian Orrenius , Claudia Piutti , Teresa Disingrini
IPC分类号： A61K31/4985 , C07D241/38 , C07D487/04 , A61K31/5377 , A61K45/06
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： The present invention relates to 4-alkyl substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives, of formula (I) which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. 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式（I）的4-烷基取代的3,4-二氢吡咯并[1,2-a]吡嗪-1（2H） - 酮衍生物，因此可用于治疗疾病 由失调的蛋白激酶活性引起。 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。
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![4-ALKYL SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS](/abs-image/US/2014/09/04/US20140249146A1/abs.jpg.150x150.jpg)
5.发明申请4-ALKYL SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS 有权4-烷基取代的3,4-二羟基吡咯并[1,2-a]吡嗪-1（2H） - 酮衍生物作为激动剂抑制剂公开(公告)号：US20140249146A1
公开(公告)日：2014-09-04
申请号：US14349536
申请日：2012-10-04
发明人： Francesco Casuscelli , Alessandra Badari , Sten Christian Orrenius , Claudia Piutti , Teresa Disingrini
IPC分类号： C07D487/04 , A61K31/5377 , A61K45/06 , A61K31/4985
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： The present invention relates to 4-alkyl substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. 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4-烷基取代的3,4-二氢吡咯并[1,2-a]吡嗪-1（2H） - 酮衍生物，因此可用于治疗由失调蛋白激酶活性引起的疾病 。 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。
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