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公开(公告)号：US11161848B2
公开(公告)日：2021-11-02
申请号：US16540327
申请日：2019-08-14
发明人： Alexandre Joseph Buckmelter , Stephanos Ioannidis , Bruce Follows , Gary Gustafson , Minghua Wang , Justin A. Caravella , Zhongguo Wang , Edward L. Fritzen , Jian Lin
IPC分类号： C07D473/00 , A61K31/522
摘要： The application relates to inhibitors of USP1 useful in the treatment of cancers, and other USP1 associated diseases and disorders, having the Formula: where R1, R2, R3, R3′, R4, R5, X1, X2, X3, X4, and n are described herein.
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公开(公告)号：US20210252011A1
公开(公告)日：2021-08-19
申请号：US15733029
申请日：2018-10-25
发明人： Wei LU , Matthew W. MARTIN , Erik WILKER , Howard FINE
IPC分类号： A61K31/55 , A61K31/496 , A61K9/00 , A61P35/00
摘要： The present disclosure relates to methods of treating glioblastoma by administering to a patient in need thereof a FASN inhibitor.
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公开(公告)号：US20210221816A1
公开(公告)日：2021-07-22
申请号：US17223783
申请日：2021-04-06
发明人： David R. Lancia, JR. , Gary Gustafson , Neal Green , Lorna Mitchell , Anna Ericsson , David Richard
IPC分类号： C07D487/04 , A61K9/00
摘要： The disclosure provides chemical compounds useful as activators of PKR. PKR activating compounds are useful in the treatment of disease and disorders associated with modulation of PKR and/or PKM2, such as pyruvate kinase deficiency (PKD).
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公开(公告)号：US10995078B2
公开(公告)日：2021-05-04
申请号：US15929751
申请日：2020-05-20
发明人： Kenneth W. Bair , David R. Lancia, Jr. , Hongbin Li , James Loch , Wei Lu , Matthew W. Martin , David S. Millan , Shawn E. R. Schiller , Mark J. Tebbe
IPC分类号： C07D295/192 , C07D401/04 , C07D403/04 , C07D405/12 , C07D413/12 , A61K31/4965 , A61P35/00 , A61K45/06 , C07D215/14 , C07D231/56 , C07D417/12 , C07D471/04 , C07D257/04 , C07D487/04 , C07D263/57 , C07D491/048 , C07D271/12 , C07D495/04 , C07D209/18 , C07D277/62 , C07D277/66 , C07D513/04 , C07D213/56 , C07D305/08 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/4985 , A61K31/5025 , A61K31/506 , C07D209/08 , C07D213/65 , C07D213/69 , C07D217/16 , C07D231/12 , C07D235/08 , C07D417/04
摘要： The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
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公开(公告)号：US10959994B2
公开(公告)日：2021-03-30
申请号：US16693642
申请日：2019-11-25
发明人： George P. Luke , Pratik Sheth
IPC分类号： A61K31/4709 , A61K9/00 , A61K47/12 , A61K47/38
摘要： The present disclosure reports solid forms of ((S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile.
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公开(公告)号：US20210078973A1
公开(公告)日：2021-03-18
申请号：US17101018
申请日：2020-11-23
发明人： Jian Lin , Anna Ericsson , Ann-Marie Campbell , Gary Gustafson , Zhongguo Wang , R. Bruce Diebold , Susan Ashwell , David R. Lancia, JR. , Justin Andrew Caravella , Wei Lu
IPC分类号： C07D401/12 , C07D401/14 , C07D471/04 , A61P35/00
摘要： The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, U, W1, W2, W3, R1-R6, and R9 are described herein.
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公开(公告)号：US20210017184A1
公开(公告)日：2021-01-21
申请号：US17062059
申请日：2020-10-02
发明人： Xiaozhang Zheng , Neal Green , Gary Gustafson , David R. Lancia, JR. , Lorna Mitchell , Tatiana Shelekhin
IPC分类号： C07D487/04 , C07D519/00 , A61P7/00 , A61K9/00 , A61K31/407
摘要： Compositions for the activation of PKR are provided, as well as therapeutic administration of the compositions for the treatment of pyruvate kinase-related medical conditions, such as pyruvate kinase deficiency (PKD).
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公开(公告)号：US10555935B2
公开(公告)日：2020-02-11
申请号：US16309980
申请日：2017-06-16
IPC分类号： A61K31/438 , C07D401/04 , C07D221/20 , C07D401/06 , C07D209/54 , A61P25/14 , A61P25/28 , A61P35/00 , A61K31/407
摘要： The present invention is directed to inhibitors of histone deacetylases (HDACs) such as HDAC6, and their use in the treatment of diseases such as cell proliferative diseases (e.g., cancer), neurological (e.g., neurodegenerative disease or neurodevelopmental disease), inflammatory or autoimmune disease, infection, metabolic disease, hematologic disease, or cardiovascular disease.
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公开(公告)号：US10550099B2
公开(公告)日：2020-02-04
申请号：US16290328
申请日：2019-03-01
发明人： Jian Lin , Anna Ericsson , Ann-Marie Campbell , Gary Gustafson , Zhongguo Wang , R. Bruce Diebold , Susan Ashwell , David R. Lancia, Jr. , Justin Andrew Caravella , Wei Lu
IPC分类号： A61K31/506 , C07D401/12 , C07D405/14 , C07D401/14 , C07D417/14 , C07D413/14 , C07D471/04 , C07D409/14 , C07D403/12
摘要： The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, B, W1, W2, W3, and R1-R6 are described herein.
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公开(公告)号：US10519129B2
公开(公告)日：2019-12-31
申请号：US16179117
申请日：2018-11-02
发明人： Stephanos Ioannidis , Adam Charles Talbot , Bruce Follows , Alexandre Joseph Buckmelter , Minghua Wang , Ann-Marie Campbell , David R. Lancia, Jr.
IPC分类号： C07D401/06 , C07D239/88 , C07D487/04 , C07D471/04
摘要： The present disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R4, R4′, X1, Y1, Y2, Y3, Y4, n, and m are described herein.
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