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公开(公告)号：US20180339978A1
公开(公告)日：2018-11-29
申请号：US16055396
申请日：2018-08-06
发明人： Maria Gabriella Brasca , Simona Bindi , Marina Caldarelli , Marcella Nesi , Sten Christian Orrenius , Achille Panzeri
IPC分类号： C07D403/04 , C07F7/08 , C07F5/04 , C07D487/04 , C07D473/00 , A61K31/506 , A61K45/06 , A61K31/53 , A61K31/52 , A61K31/519 , C07D401/04
摘要： The present invention relates to substituted pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak family kinases. 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.
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2.发明申请TRICYCLIC PYRROLO DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS 审中-公开三聚吡咯衍生物，其制备方法及其作为激酶抑制剂的用途公开(公告)号：US20150141408A1
公开(公告)日：2015-05-21
申请号：US14609534
申请日：2015-01-30
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 , C07C67/00 , C12N9/99 , C07D209/42 , C07D401/04 , A61K45/06 , A61K31/519 , C07D207/34
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 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三环吡咯衍生物，因此可用于治疗由调节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.发明授权公开(公告)号：US10280176B2
公开(公告)日：2019-05-07
申请号：US15467323
申请日：2017-03-23
发明人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
IPC分类号： C07D487/14 , C07D487/04 , C07D401/10 , C07D403/14 , C07D413/14 , C07D231/56 , C07D239/72 , A61K31/519 , A61K31/551 , A61K31/5377
摘要： Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) 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.
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公开(公告)号：US10071986B2
公开(公告)日：2018-09-11
申请号：US15598976
申请日：2017-05-18
发明人： Maria Gabriella Brasca , Simona Bindi , Marina Caldarelli , Marcella Nesi , Sten Christian Orrenius , Achille Panzeri
IPC分类号： C07D471/04 , C07D487/04 , C07D401/04 , C07D403/04 , C07D473/00 , A61K45/06 , A61K31/52 , A61K31/519 , A61K31/506 , C07F5/04 , A61K31/53 , C07F7/08
CPC分类号： C07D403/04 , A61K31/506 , A61K31/519 , A61K31/52 , A61K31/53 , A61K45/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/00 , A61P37/06 , C07D401/04 , C07D471/04 , C07D473/00 , C07D487/04 , C07F5/04 , C07F7/083
摘要： The present invention relates to substituted pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak family kinases. 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.
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5.发明授权公开(公告)号：US09464090B2
公开(公告)日：2016-10-11
申请号：US14625093
申请日：2015-02-18
发明人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
IPC分类号： A61K31/519 , C07D487/04 , C07D403/14 , C07D487/14 , A61K31/5377 , A61K31/551 , C07D231/56 , C07D401/10 , C07D239/72 , C07D413/14
CPC分类号： C07D487/14 , A61K31/519 , A61K31/5377 , A61K31/551 , C07D231/56 , C07D239/72 , C07D401/10 , C07D403/14 , C07D413/14 , C07D487/04
摘要： Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) 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.
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公开(公告)号：US20150166512A1
公开(公告)日：2015-06-18
申请号：US14418555
申请日：2013-07-24
发明人： Maria Gabriella Brasca , Simona Bindi , Marina Caldarelli , Marcella Nesi , Sten Christian Orrenius , Achille Panzeri
IPC分类号： C07D403/04 , C07F5/04 , C07F7/08 , A61K45/06 , A61K31/519 , C07D473/00 , A61K31/52 , A61K31/53 , A61K31/506 , C07D487/04
CPC分类号： C07D403/04 , A61K31/506 , A61K31/519 , A61K31/52 , A61K31/53 , A61K45/06 , C07D401/04 , C07D473/00 , C07D487/04 , C07F5/04 , C07F7/083
摘要： The present invention relates to substituted pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak family kinases. 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取代吡咯化合物，因此可用于治疗由失调的蛋白激酶活性引起的疾病，特别是Jak家族激酶。 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。
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7.发明申请PYRAZOLO-QUINAZOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS 有权吡唑并喹啉衍生物，其制备方法及其作为激酶抑制剂的用途公开(公告)号：US20150158876A1
公开(公告)日：2015-06-11
申请号：US14625093
申请日：2015-02-18
发明人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
IPC分类号： C07D487/04 , C07D231/56
CPC分类号： C07D487/14 , A61K31/519 , A61K31/5377 , A61K31/551 , C07D231/56 , C07D239/72 , C07D401/10 , C07D403/14 , C07D413/14 , C07D487/04
摘要： Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) 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（Ia）或（Ib）的吡唑并喹唑啉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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公开(公告)号：US20170253578A1
公开(公告)日：2017-09-07
申请号：US15598976
申请日：2017-05-18
发明人： Maria Gabriella Brasca , Simona Bindi , Marina Caldarelli , Marcella Nesi , Sten Christian Orrenius , Achille Panzeri
IPC分类号： C07D403/04 , C07D473/00 , C07D487/04 , A61K45/06 , A61K31/53 , A61K31/52 , A61K31/519 , A61K31/506 , C07F5/04 , C07D401/04 , C07F7/08
CPC分类号： C07D403/04 , A61K31/506 , A61K31/519 , A61K31/52 , A61K31/53 , A61K45/06 , C07D401/04 , C07D473/00 , C07D487/04 , C07F5/04 , C07F7/083
摘要： The present invention relates to substituted pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak family kinases. 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.
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9.发明申请PYRAZOLO-QUINAZOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS 有权吡唑并喹啉衍生物，其制备方法及其作为激酶抑制剂的用途公开(公告)号：US20170050972A1
公开(公告)日：2017-02-23
申请号：US15256916
申请日：2016-09-06
发明人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
IPC分类号： C07D487/14
CPC分类号： C07D487/14 , A61K31/519 , A61K31/5377 , A61K31/551 , C07D231/56 , C07D239/72 , C07D401/10 , C07D403/14 , C07D413/14 , C07D487/04
摘要： Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) 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（Ia）或（Ib）的吡唑并喹唑啉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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10.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：US09309253B2
公开(公告)日：2016-04-12
申请号：US14609534
申请日：2015-01-30
发明人： Marina Caldarelli , Mauro Angiolini , Italo Beria , Maria Gabriella Brasca , Francesco Casuscelli , Roberto D'Alessio , Andrea Lombardi Borgia
IPC分类号： A61K31/55 , A61K45/06 , C07D487/04 , A61K31/519 , C07C67/00 , C07D207/34 , C07D209/42 , C07D401/04 , C12N9/99
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 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三环吡咯衍生物，因此可用于治疗由调节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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