公开(公告)号：US10364272B2

公开(公告)日：2019-07-30

申请号：US16145075

申请日：2018-09-27

申请人： CARNEGIE MELLON UNIVERSITY

发明人： Danith H. Ly ,  Srinivas Rapireddy ,  Bichismita Sahu

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.

公开(公告)号：US10363257B2

公开(公告)日：2019-07-30

申请号：US15875678

申请日：2018-01-19

申请人： ZENITH EPIGENETICS LTD.

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.

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.

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.

公开(公告)号：US10273248B2

公开(公告)日：2019-04-30

申请号：US15737911

申请日：2016-06-24

申请人： Kadmon Corporation LLC

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.

公开(公告)号：US20190119268A1

公开(公告)日：2019-04-25

申请号：US15987523

申请日：2018-05-23

申请人： Sunesis Pharmaceuticals, Inc. ,  Millennium Pharmaceuticals, Inc.

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.

公开(公告)号：US10201559B2

公开(公告)日：2019-02-12

申请号：US15121412

申请日：2014-03-14

申请人： Alltech, Inc.

发明人： Ronan Power ,  Zi-Jian Lan ,  Alexandros Yiannikouris

IPC分类号： A01N43/04 ,  A61K31/70 ,  A61K31/7135 ,  A61K31/7076 ,  C07D473/34 ,  A61K31/28 ,  A61K38/05 ,  A61K38/28 ,  A61K31/706 ,  A61K31/7064

摘要： The present application relates to compositions comprising selenium compounds, such as 5′-Methylselenoadenosine, Se-Adenosyl-L-homocysteine, Gamma-glutamyl-methylseleno-cysteine, a compound of formula (I), formula (II), a compound of formula (III) and combinations thereof, and methods of using the same in enhancing mitochondrial function, or treating mitochondrial dysfunction.

公开(公告)号：US20190031626A1

公开(公告)日：2019-01-31

申请号：US16025862

申请日：2018-07-02

申请人： GILEAD CALISTOGA LLC

发明人： Stacy BREMNER ,  Jerry B. EVARTS ,  Keiko SUJINO ,  Duong TRAN ,  Dragos VIZITIU

IPC分类号： C07D265/22 ,  C07D239/91 ,  C07C233/90 ,  C07D263/58 ,  C07D487/04 ,  C07D265/10 ,  C07D473/34

CPC分类号： C07D265/22 ,  C07C233/90 ,  C07D239/91 ,  C07D263/58 ,  C07D265/10 ,  C07D473/34 ,  C07D487/04

摘要： A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.

公开(公告)号：US10167285B2

公开(公告)日：2019-01-01

申请号：US15620865

申请日：2017-06-13

申请人： Memorial Sloan Kettering Cancer Center

发明人： Gabriela Chiosis ,  Huazhong He ,  Laura Llauger-Bufi ,  Joungnam Kim ,  Steven M. Larson ,  Peter Smith-Jones

IPC分类号： C07D473/34 ,  A61K51/04 ,  C07D491/056 ,  G01N33/60

摘要： Hsp90 inhibitors havin are provided havin the formula: (I) with a 2′,4′,5′-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4′ and 5′ positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C═SR2 NSO2X5, C═OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula —O—(CH2)n—O—, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5′-position and the other at the 4′-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.

公开(公告)号：US20180346465A1

公开(公告)日：2018-12-06

申请号：US16055560

申请日：2018-08-06

申请人： Elanco Tiergesundheit AG

发明人： Noelle Gauvry ,  Chouaib Tahtaoui ,  Pascal Furet ,  Pierre Ducray

IPC分类号： C07D471/14 ,  C07D239/48 ,  C07D471/04 ,  C07D473/34 ,  C07D487/04 ,  C07D495/04 ,  C07D239/42 ,  C07D239/46

CPC分类号： C07D471/14 ,  C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D471/04 ,  C07D473/34 ,  C07D487/04 ,  C07D495/04

摘要： The invention relates to a compound of formula (I) wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful as therapeutic agent for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis. Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, inflammatory bowel diseases, Crohn's disease, Alzheimer's disease, leukemia, osteoarthritis, control of pruritus, chronic respiratory disease or keratoconjunctivitis in mammals.