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1.发明授权Tricyclic derivatives, process for their preparation and their use as kinase inhibitors 有权三环衍生物，其制备方法及其作为激酶抑制剂的用途公开(公告)号：US08916577B2
公开(公告)日：2014-12-23
申请号：US13980182
申请日：2012-01-19
申请人： Marina Caldarelli , Francesco Casuscelli , Daniele Donati , Danilo Mirizzi , Francesca Quartieri , Marco Silvagni
发明人： Marina Caldarelli , Francesco Casuscelli , Daniele Donati , Danilo Mirizzi , Francesca Quartieri , Marco Silvagni
IPC分类号： A61K45/06 , A61K31/551 , C07D498/14 , C07D498/04 , C07D487/04 , A61K31/519 , A61K31/5377 , A61K31/5383
CPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , A61K31/5383 , A61K31/551 , A61K45/06 , C07D498/04 , C07D498/14
摘要： New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase.
摘要翻译： 描述了式（I）的新取代的三环化合物，其中R1，R2，X，Y，Z在本文中定义，具有蛋白激酶抑制活性。 本发明包括制备式（I）化合物，含有它们的药物组合物的方法及其在治疗中的用途，特别是用于治疗由蛋白激酶失调的活性引起的和/或与之有关的疾病。
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2.发明申请TRICYCLIC DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS 有权三肽衍生物，其制备方法及其作为激酶抑制剂的用途公开(公告)号：US20130302416A1
公开(公告)日：2013-11-14
申请号：US13980182
申请日：2012-01-19
申请人： Marina Caldarelli , Francesco Casuscelli , Daniele Donati , Danilo Mirizzi , Francesca Quartieri , Marco Silvagni
发明人： Marina Caldarelli , Francesco Casuscelli , Daniele Donati , Danilo Mirizzi , Francesca Quartieri , Marco Silvagni
IPC分类号： C07D487/04 , C07D498/04 , A61K45/06 , A61K31/551 , C07D498/14 , A61K31/5383 , A61K31/519 , A61K31/5377
CPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , A61K31/5383 , A61K31/551 , A61K45/06 , C07D498/04 , C07D498/14
摘要： New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase.
摘要翻译： 描述了式（I）的新取代的三环化合物，其中R1，R2，X，Y，Z在本文中定义，具有蛋白激酶抑制活性。 本发明包括制备式（I）化合物，含有它们的药物组合物的方法及其在治疗中的用途，特别是用于治疗由蛋白激酶失调的活性引起的和/或与之有关的疾病。
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公开(公告)号：US09284298B2
公开(公告)日：2016-03-15
申请号：US14110596
申请日：2012-04-03
申请人： Francesco Casuscelli , Maria Gabriella Brasca , Marina Caldarelli , Giovanni Cervi , Teresa Disingrini , Francesca Quartieri
发明人： Francesco Casuscelli , Maria Gabriella Brasca , Marina Caldarelli , Giovanni Cervi , Teresa Disingrini , Francesca Quartieri
IPC分类号： A61K45/06 , A61K31/506 , C07D403/04 , C07D401/14 , C07D403/14 , C07D413/14
CPC分类号： C07D403/04 , A61K31/506 , A61K45/06 , C07D401/14 , C07D403/14 , C07D413/14
摘要： The present invention relates to pyrazolyl-pyrimidine 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 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吡唑基 - 嘧啶衍生物，因此可用于治疗由失调的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。
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公开(公告)号：US20140051708A1
公开(公告)日：2014-02-20
申请号：US14110596
申请日：2012-04-03
申请人： Francesco Casuscelli , Maria Gabriella Brasca , Marina Caldarelli , Giovanni Cervi , Teresa Disingrini , Francesca Quartieri
发明人： Francesco Casuscelli , Maria Gabriella Brasca , Marina Caldarelli , Giovanni Cervi , Teresa Disingrini , Francesca Quartieri
IPC分类号： C07D403/04 , A61K45/06 , C07D401/14 , A61K31/506
CPC分类号： C07D403/04 , A61K31/506 , A61K45/06 , C07D401/14 , C07D403/14 , C07D413/14
摘要： The present invention relates to pyrazolyl-pyrimidine 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 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吡唑基 - 嘧啶衍生物，因此可用于治疗由失调的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。
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![Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity](/abs-image/US/2015/03/17/US08981092B2/abs.jpg.150x150.jpg)
5.发明授权Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity 有权取代的3,4-二氢-2H-吡咯并[1,2-a]吡嗪-1-酮作为蛋白激酶活性的调节剂公开(公告)号：US08981092B2
公开(公告)日：2015-03-17
申请号：US13747859
申请日：2013-01-23
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： C07D241/38 , A61K31/4985 , C07D487/04 , A61K45/06
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, 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4,7-二取代衍生物或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。 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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6.发明申请TRICYCLIC PYRROLO DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS 有权三聚吡咯衍生物，其制备方法及其作为激酶抑制剂的用途公开(公告)号：US20130296305A1
公开(公告)日：2013-11-07
申请号：US13980168
申请日：2012-01-19
申请人： Marina Caldarelli , Mauro Angiolini , Italo Beria , Maria Gabriella Brasca , Francesco Casuscelli , Roberto D'Alessio , Andrea Lombardi Borgia
发明人： Marina Caldarelli , Mauro Angiolini , Italo Beria , Maria Gabriella Brasca , Francesco Casuscelli , Roberto D'Alessio , Andrea Lombardi Borgia
IPC分类号： C07D487/04 , A61K31/55 , A61K45/06 , A61K31/519
CPC分类号： C07D487/04 , A61K31/519 , A61K31/55 , A61K45/06 , C07C67/00 , C07D207/34 , C07D209/42 , C07D401/04 , C12N9/99
摘要： The present invention relates to tricyclic pyrrolo 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： 本发明涉及式（I）的三环吡咯衍生物，其调节蛋白激酶的活性，因此可用于治疗由失调的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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![3,4-DIHYDRO-2H-PYRROLO[1,2-a]PYRAZIN-1-ONE DERIVATIVES](/abs-image/US/2011/10/13/US20110251179A1/abs.jpg.150x150.jpg)
公开(公告)号：US20110251179A1
公开(公告)日：2011-10-13
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： A61K31/4985 , C40B40/04 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P35/02 , C12N9/99 , A61P35/00 , A61P31/12 , A61P31/18 , A61P37/06 , A61P25/28 , C07D487/04 , A61K31/551
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, 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4,7-二取代衍生物或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。 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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![3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one derivatives for the modulation of the activity of protein kinases](/abs-image/US/2013/03/12/US08394802B2/abs.jpg.150x150.jpg)
8.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。
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9.发明授权Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors 有权三环吡咯衍生物，其制备方法及其作为激酶抑制剂的用途公开(公告)号：US08975267B2
公开(公告)日：2015-03-10
申请号：US13980168
申请日：2012-01-19
申请人： Marina Caldarelli , Mauro Angiolini , Italo Beria , Maria Gabriella Brasca , Francesco Casuscelli , Roberto D'Alessio , Andrea Lombardi Borgia
发明人： Marina Caldarelli , Mauro Angiolini , Italo Beria , Maria Gabriella Brasca , Francesco Casuscelli , Roberto D'Alessio , Andrea Lombardi Borgia
IPC分类号： A61K31/519 , C07D487/04 , A61K31/55 , A61K45/06
CPC分类号： C07D487/04 , A61K31/519 , A61K31/55 , A61K45/06 , C07C67/00 , C07D207/34 , C07D209/42 , C07D401/04 , C12N9/99
摘要： The present invention relates to tricyclic pyrrolo 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： 本发明涉及式（I）的三环吡咯衍生物，其调节蛋白激酶的活性，因此可用于治疗由失调的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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![3,4-DIHYDRO-2H-PYRROLO[1,2-A]PYRAZIN-1-ONE DERIVATIVES FOR THE MODULATION OF THE ACTIVITY OF PROTEIN KINASES](/abs-image/US/2013/05/30/US20130137696A1/abs.jpg.150x150.jpg)
10.发明申请3,4-DIHYDRO-2H-PYRROLO[1,2-A]PYRAZIN-1-ONE DERIVATIVES FOR THE MODULATION OF THE ACTIVITY OF PROTEIN KINASES 审中-公开用于调节蛋白激酶活性的3,4-二氢-2H-吡喃[1,2-A]吡嗪-1-酮衍生物公开(公告)号：US20130137696A1
公开(公告)日：2013-05-30
申请号：US13747859
申请日：2013-01-23
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： A61K31/4985 , A61K45/06 , C07D487/04
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, 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4,7-二取代衍生物或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。 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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