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公开(公告)号：US11078191B2
公开(公告)日：2021-08-03
申请号：US16484183
申请日：2018-02-08
申请人： Novartis AG , Palobiofarma S.L.
发明人： Sanela Bilic , Juan Alberto Camacho Gomez , John Scott Cameron , Julio Cesar Castro-Palomino Laria , Danny Roland Howard, Jr.
IPC分类号： C07D403/14 , C07K16/28 , A61K31/506 , A61P35/00
摘要： This invention relates to an active metabolite of 5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimindin-4-amine that modulates the activity of adenosine A2a receptor. In particular, the present invention relates to pharmaceutical compositions comprising 1-(4-amino-5-bromo-6-(1H-pyrazol-1-yl)-pyrimidin-2-yl)-1H-pyrazol-4-ol, as well as processes for its preparation and its use in the treatment of cancer alone of in combination with one or more immunotherapeutic agents.
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公开(公告)号：US10933064B2
公开(公告)日：2021-03-02
申请号：US16616844
申请日：2018-05-30
申请人： Novartis AG , Palobiofarma S.L.
IPC分类号： A61K31/506 , A61K39/395 , A61K45/06 , C07D403/14 , C07K16/28 , A61K39/00
摘要： This application relates to various crystalline forms of 5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimidin-4-amine and salt thereof, as well as compositions and methods of using the same. In some embodiments the crystalline forms also contain water (“hydrates”). These materials are useful in the treatment of various diseases, including carcinomas, specifically lung cancer and more specifically non-small cell lung cancer.
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公开(公告)号：US11654144B2
公开(公告)日：2023-05-23
申请号：US17156785
申请日：2021-01-25
申请人： Novartis AG , Palobiofarma S.L.
IPC分类号： A61K31/506 , A61K39/395 , A61K45/06 , C07D403/14 , C07K16/28 , A61K39/00
CPC分类号： A61K31/506 , A61K39/3955 , A61K45/06 , C07D403/14 , C07K16/2818 , C07K16/2827 , A61K2039/545 , C07B2200/13 , C07K2317/565
摘要： This application relates to various crystalline forms of 5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimidin-4-amine and salt thereof, as well as compositions and methods of using the same. In some embodiments the crystalline forms also contain water (“hydrates”). These materials are useful in the treatment of various diseases, including carcinomas, specifically lung cancer and more specifically non-small cell lung cancer.
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公开(公告)号：US10561653B2
公开(公告)日：2020-02-18
申请号：US15751140
申请日：2016-08-10
申请人： NOVARTIS AG , PALOBIOFARMA, S.L.
发明人： Sanela Bilic , Juan Alberto Camacho Gomez , John Scott Cameron , Julio Cesar Castro-Palomino Laria , Danny Roland Howard, Jr.
IPC分类号： A61K39/395 , A61K31/506 , A61P35/00 , A61K39/00
摘要： The present invention relates to 5-bromo-2,6-di-(1H-pyrazol-1-yl)pyrimidin-4-amine, its pharmaceutically acceptable salts and co-crystals thereof and to pharmaceutical compositions comprising said compounds for use in the treatment of cancer.
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公开(公告)号：US10253017B2
公开(公告)日：2019-04-09
申请号：US15552039
申请日：2016-02-19
申请人： PALOBIOFARMA, S.L.
IPC分类号： C07D401/14 , A61K45/06 , A61K31/506 , A61K31/444
摘要： The present invention relates to novel pyridine derivatives of formula (I): as A2B adenosine receptor antagonists and ligands of MT3 melatonin receptor, to processes for their preparation, to pharmaceutical compositions comprising said compounds and to the use of said for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by antagonizing the adenosine A2B receptor and by inhibition of MT3 melatonin receptor, such as respiratory disease, metabolic disorders, neurological disorders and cancer.
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