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公开(公告)号：US20220144813A1
公开(公告)日：2022-05-12
申请号：US17352585
申请日：2021-06-21
发明人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
IPC分类号： C07D405/14 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/04 , C07D405/12 , A61K31/496 , A61K45/06 , C07D403/12
摘要： Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
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2.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：US10081622B2
公开(公告)日：2018-09-25
申请号：US15438872
申请日：2017-02-22
发明人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
IPC分类号： C07D405/14 , C07D231/56 , C07D405/12 , C07D403/12 , C07D403/14 , C07D401/12 , C07D401/14
CPC分类号： C07D405/14 , A61K31/496 , A61K45/06 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12
摘要： Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
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公开(公告)号：US09102662B2
公开(公告)日：2015-08-11
申请号：US14534648
申请日：2014-11-06
发明人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
IPC分类号： A61K31/497 , A61K31/496 , C07D405/12 , C07D403/12 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/04 , C07D405/14
CPC分类号： C07D405/14 , A61K31/496 , A61K45/06 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12
摘要： Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
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公开(公告)号：US20140228351A1
公开(公告)日：2014-08-14
申请号：US14212256
申请日：2014-03-14
发明人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
IPC分类号： C07D231/56 , C07D401/14 , C07D401/12 , C07D403/14 , C07D405/04 , C07D405/14
CPC分类号： C07D405/14 , A61K31/496 , A61K45/06 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12
摘要： Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
摘要翻译： 式（I）的取代的吲唑衍生物及其药学上可接受的盐，如说明书中所定义; 本发明的化合物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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公开(公告)号：US09616059B2
公开(公告)日：2017-04-11
申请号：US14971372
申请日：2015-12-16
发明人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
IPC分类号： A61K31/496 , A61K45/06 , C07D405/12 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/04 , C07D405/14
CPC分类号： C07D405/14 , A61K31/496 , A61K45/06 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12
摘要： Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
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8.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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公开(公告)号：US20150065520A1
公开(公告)日：2015-03-05
申请号：US14534617
申请日：2014-11-06
发明人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
IPC分类号： C07D405/12
CPC分类号： C07D405/14 , A61K31/496 , A61K45/06 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12
摘要： Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
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公开(公告)号：US20150051154A1
公开(公告)日：2015-02-19
申请号：US14390644
申请日：2013-03-28
发明人： Italo Beria , Michele Caruso , Vittoria Lupi , Paolo Orsini , Matteo Salsa , Achille Panzeri
IPC分类号： C07D495/04 , A61K45/06 , A61K31/496 , A61K47/48 , A61K38/05 , C07K5/083 , A61K38/06 , A61K31/407 , C07K5/062
CPC分类号： A61K31/407 , A61K31/496 , A61K38/05 , A61K38/06 , A61K45/06 , A61K47/545 , C07D495/04 , C07K5/06017 , C07K5/0804
摘要： The present invention relates to a novel class of alkylating agents comprising a thieno-indole moiety linked to a DNA-binding moiety, which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them. The invention also relates to the use of this novel class of alkylating agents in the preparation of conjugates.
摘要翻译： 本发明涉及一类新颖的烷化剂，其包含与DNA结合部分连接的噻吩并吲哚部分，其具有细胞毒活性，并且可用于治疗疾病如癌症，细胞增殖病症和病毒感染。 本发明还提供了制备这些化合物的方法，包含它们的药物组合物和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。 本发明还涉及这种新型烷基化剂在制备缀合物中的用途。
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