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公开(公告)号:US10519160B2
公开(公告)日:2019-12-31
申请号:US15326890
申请日:2015-07-17
IPC分类号: C07D473/40 , C07D473/16 , C07D487/04 , C07D473/34 , C07B59/00 , A61K51/04
摘要: Provided herein are radiolabeled compounds useful for non-invasive imaging techniques. An exemplary radiolabeled compound provided herein is useful as a radiotracer for positron emission tomography. The present application also provides unlabeled compounds useful in methods of treating diseases of the central nervous system or disease of the peripheral nervous system. Methods for preparing radiolabeled compounds, preparing unlabeled compounds, and diagnostic methods using labeled or unlabeled compounds are also provided.
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公开(公告)号:US20190358237A1
公开(公告)日:2019-11-28
申请号:US16440350
申请日:2019-06-13
发明人: John Frederick Quinn , Bryan Cordell Duffy , Shuang LIU , Ruifang Wang , May Xiaowu Jiang , Gregory Scott Martin , Gregory Steven Wagner , Peter Ronald Young
IPC分类号: A61K31/5377 , A61K31/4985 , C07D413/04 , A61K31/4545 , A61K31/4184 , C07D473/34 , A61K31/52 , A61K31/517 , A61K31/498 , A61K31/497 , A61K31/496 , A61K31/437 , A61K31/423 , A61K31/422 , A61K45/06 , C07D471/04
摘要: The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical compositions comprising these compounds, and use of the compounds and compositions in therapy.
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公开(公告)号:USRE47690E1
公开(公告)日:2019-11-05
申请号:US15968188
申请日:2018-05-01
IPC分类号: C07D513/04 , C07D473/16 , C07D473/34 , C07D487/04
摘要: The present invention relates to novel hydroxamic acids which are specific histone deacetylase (HDAC) inhibitors and/or TTK/Mps1 kinase inhibitors, including pharmaceutically acceptable salts thereof, which are useful for modulating HDAC and/or TTK/Mps1 kinase activity, pharmaceutical compositions comprising these compounds, and processes for their preparation.
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公开(公告)号:US20190315747A9
公开(公告)日:2019-10-17
申请号:US15561729
申请日:2016-03-25
IPC分类号: C07D473/16 , C07D473/34 , C07D487/04 , A61P43/00
摘要: The present invention provides novel compounds of Formula (I), (II), or (III), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., CDK7, CDK12, or CDK13), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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公开(公告)号:US10364272B2
公开(公告)日:2019-07-30
申请号:US16145075
申请日:2018-09-27
IPC分类号: C07H15/00 , C07K14/00 , C07D473/34 , C07D473/18 , C07D239/54 , C07D239/47 , C08G69/10 , A61K47/60 , C07K1/04 , C07C271/20 , C07C229/12 , C07K1/08
摘要: The present invention relates to γ-PNA monomers according to Formula I where substituent groups R1, R2, R3, R4, R5, R6, B and P are defined as set forth in the specification. The invention also provides methodology for synthesizing compounds according to Formula I and methodology for synthesizing PNA oligomers that incorporate one or more Formula I monomers.
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公开(公告)号:US10363257B2
公开(公告)日:2019-07-30
申请号:US15875678
申请日:2018-01-19
发明人: John Frederick Quinn , Bryan Cordell Duffy , Shuang Liu , Ruifang Wang , May Xiaowu Jiang , Gregory Scott Martin , Gregory Steven Wagner , Peter Roland Young
IPC分类号: A61K31/5377 , A61K31/06 , A61K31/422 , A61K31/423 , A61K31/437 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/517 , A61K31/52 , A61K31/4184 , A61K31/4985 , A61K31/4545 , C07D413/04 , C07D471/04 , C07D473/34 , A61K45/06
摘要: The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical compositions comprising these compounds, and use of the compounds and compositions in therapy.
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57.
公开(公告)号:US20190202840A1
公开(公告)日:2019-07-04
申请号:US16295435
申请日:2019-03-07
申请人: Incyte Corporation
发明人: Yun-Long Li , Brian W. Metcalf , Hui-Yin Li
IPC分类号: C07D519/00 , C07C309/04 , C07C65/03 , C07C55/14 , C07D473/34 , A61K45/06 , A61K31/52 , C07D513/04
CPC分类号: C07D519/00 , A61K31/52 , A61K45/06 , C07B2200/13 , C07C55/14 , C07C65/03 , C07C309/04 , C07D473/34 , C07D513/04
摘要: The present invention relates to salt forms of the phosphoinositide 3-kinase (PI3K) inhibitor (S)-7-(1-(9H-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, pharmaceutical compositions comprising the same, and methods of using the salts and compositions for the treatment of PI3K-associated diseases such as cancer.
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公开(公告)号:US10286086B2
公开(公告)日:2019-05-14
申请号:US15319840
申请日:2015-06-19
申请人: ModernaTX, Inc.
发明人: Atanu Roy , Christopher R. Conlee , Antonin De Fougerolles , Andrew W. Fraley , Gabor Butora , Matthew Stanton
IPC分类号: A61K48/00 , C07F9/6558 , C07H19/06 , C07H19/16 , C12N15/11 , C12N15/67 , C07H21/02 , C07F9/6561 , C07D405/04 , C07D239/54 , C07H19/067 , C07H19/10 , C07H19/14 , C07H19/167 , C07H19/20 , C07H19/23 , C07D473/16 , C07D473/18 , C07D473/30 , C07D473/34 , C07D473/38 , C07D473/40 , C07D487/04 , C07D487/16 , C07D498/22 , C12N15/87
摘要: The present disclosure provides alternative nucleosides, nucleotides, and nucleic acids, and methods of using them.
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公开(公告)号:US10273248B2
公开(公告)日:2019-04-30
申请号:US15737911
申请日:2016-06-24
发明人: Kellen L. Olszewski , Ji-In Kim , Masha V. Poyurovsky , Kevin G. Liu , Anthony Barsotti , Koi Morris
IPC分类号: C07D471/04 , C07D491/048 , C07D487/04 , C07D495/04 , C07D513/04 , A61K45/06 , A61K31/519 , A61K31/52 , A61K31/5377 , C07D473/34 , A61P35/04
摘要: Provided herein are compounds that modulate glucose uptake activity and are useful for treating cancer, autoimmune diseases, inflammation, infectious diseases, and metabolic diseases. In certain embodiments, the compounds modulate glucose uptake activity by modulating cellular components, including, but not limited to those related to glycolysis and known transporters/co-transporters of glucose such as GLUT1 and other GLUT family members/alternative hexose transporters. In certain embodiments, the compounds have the structure of formula I: Formula (I) wherein the variables have the values disclosed herein.
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公开(公告)号:US20190119268A1
公开(公告)日:2019-04-25
申请号:US15987523
申请日:2018-05-23
发明人: Joseph ARNDT , Timothy CHAN , Kevin GUCKIAN , Gnanasambandam KUMARAVEL , Wen-Cherng LEE , Edward Yin-Shiang LIN , Daniel SCOTT , Lihong SUN , Jermaine THOMAS , Kurt VAN VLOTEN , Deping WANG , Lei ZHANG , Daniel ERLANSON
IPC分类号: C07D471/04 , A61K31/498 , C07D213/82 , A61K31/444 , A61K31/452 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/5383 , A61K31/4985 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/5377 , A61K31/437 , C07D498/04 , C07D241/28 , C07D519/00 , C07D491/052 , C07D487/04 , C07D473/34 , C07D417/14 , C07D409/14 , C07D409/04 , C07D405/14 , C07D403/14 , C07D403/12 , C07D401/14 , C07D401/12 , C07D241/26 , C07D213/85 , A61K31/4439
摘要: The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.
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