公开(公告)号：US20240300948A1

公开(公告)日：2024-09-12

申请号：US18584553

申请日：2024-02-22

申请人： Incyte Corporation

发明人： Charles Cole ,  Yanran Ai ,  Eddy W. Yue

IPC分类号： C07D471/12 ,  A61K31/519 ,  A61K31/5377

CPC分类号： C07D471/12 ,  A61K31/519 ,  A61K31/5377

摘要： The present application provides heterocyclic compounds that modulate the activity of JAK2, which are useful in the treatment of various diseases, including cancer.

公开(公告)号：US11512083B2

公开(公告)日：2022-11-29

申请号：US16905641

申请日：2020-06-18

申请人： Arvinas Operations, Inc. ,  Yale University

发明人： Andrew P. Crew ,  Craig M. Crews ,  Xin Chen ,  Hanqing Dong ,  Caterina Ferraro ,  Yimin Qian ,  Kam Siu ,  Jing Wang ,  Meizhong Jin ,  Michael Berlin ,  Kurt Zimmermann

IPC分类号： C07D521/00 ,  C07D413/14 ,  C07D471/12 ,  C07D417/14 ,  C07D207/16 ,  C07D207/26 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  A61K31/422 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/5377 ,  C07D471/04 ,  A61K45/06 ,  C07D417/12 ,  C07D403/14 ,  C07D401/14 ,  C07D405/14 ,  C07D495/04

摘要： The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.

公开(公告)号：US20220104496A1

公开(公告)日：2022-04-07

申请号：US17551910

申请日：2021-12-15

申请人： SYNGENTA PARTICIPATIONS AG

发明人： Andrew EDMUNDS ,  Michel MUEHLEBACH ,  Andre STOLLER ,  Olivier LOISELEUR ,  Anke BUCHHOLZ ,  Ottmar Franz HUETER ,  Roger Graham HALL ,  Daniel EMERY ,  Pierre Joseph Marcel JUNG ,  Long LU ,  Yaming WU ,  Aurelien BIGOT ,  Ruifang CHEN

IPC分类号： A01N43/90 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D471/12

摘要： Compounds of formula I A-B  (I), wherein A is a radical selected from the group consisting of formulae A1 to A8: wherein the arrow denotes the point of attachment to the radical B; and B is a radical selected from the group consisting of formulae B1 to B11: wherein the arrow denotes the point of attachment to the radical A; and wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as insecticides and can be prepared in a manner known per se.

公开(公告)号：US11229208B2

公开(公告)日：2022-01-25

申请号：US17068334

申请日：2020-10-12

申请人： SYNGENTA PARTICIPATIONS AG

发明人： Andrew Edmunds ,  Michel Muehlebach ,  André Stoller ,  Olivier Loiseleur ,  Anke Buchholz ,  Ottmar Franz Hueter ,  Aurelien Bigot ,  Roger Graham Hall ,  Daniel Emery ,  Pierre Joseph Marcel Jung ,  Long Lu ,  Yaming Wu ,  Ruifang Chen

IPC分类号： A01N43/90 ,  C07D471/04 ,  C07D471/12 ,  C07D487/04 ,  C07D498/04

摘要： Compounds of formula I A-B  (I), wherein A is a radical selected from the group consisting of formulae A1 to A8: wherein the arrow denotes the point of attachment to the radical B; and B is a radical selected from the group consisting of formulae B1 to B11: wherein the arrow denotes the point of attachment to the radical A; and wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as insecticides and can be prepared in a manner known per se.

公开(公告)号：US10829455B2

公开(公告)日：2020-11-10

申请号：US16358460

申请日：2019-03-19

申请人： AMPHASTAR NANJING PHARMACEUTICALS INC.

发明人： Yonggang Xu ,  Hao Wei ,  Song Chen ,  Haoning Zhang

IPC分类号： C07D221/22 ,  C07D471/12

摘要： A method of resolving a racemic mixture of (±)-Huperzine A to (−)-Huperzine A includes: separating the (−)-Huperzine A from the racemic mixture of (±)-Huperzine A by chiral high performance liquid chromatography (HPLC), the chiral HPLC being performed utilizing a mobile phase including a solution including an alcohol and one selected from dichloromethane, trichloromethane, and a mixture thereof, and the chiral HPLC being performed utilizing a chiral stationary phase including a polysaccharide derivative.

公开(公告)号：US10450434B2

公开(公告)日：2019-10-22

申请号：US15796993

申请日：2017-10-30

申请人： Owens Corning Intellectual Capital, LLC

发明人： Matthew Daniel Gawryla

IPC分类号： C08J3/24 ,  C08K3/011 ,  C08J9/14 ,  C08J9/12 ,  C08F8/50 ,  C08J9/00 ,  B01J31/16 ,  C07D471/12 ,  C08K5/00

摘要： Reversibly cross-linkable foam is provided. The reversibly cross-linked foam includes a first polymeric material, at least one reversibly cross-linkable monomer polymerized with the first polymeric material, and at least one blowing agent. The reversibly cross-linkable co-polymeric foam is thermally stable at temperatures of at least 10 degrees higher than otherwise identical polymeric foam that does not include the reversibly cross-linkable agent polymerized with the first polymeric material.

公开(公告)号：US10329297B2

公开(公告)日：2019-06-25

申请号：US15680683

申请日：2017-08-18

申请人： Merck Patent GmbH

发明人： Brian A. Sherer

IPC分类号： C07D471/14 ,  C07D487/04 ,  C07D471/12 ,  A61K31/4188 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/519 ,  A61K45/06 ,  C07D487/14

摘要： The present invention relates to compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of IDO, and for the treatment of IDO-related disorders.

公开(公告)号：US09926318B2

公开(公告)日：2018-03-27

申请号：US15036370

申请日：2014-11-20

申请人： PharmAkea, Inc.

发明人： John Howard Hutchinson ,  David Lonergan ,  Martin Rowbottom ,  Andiliy Gokching Lai

IPC分类号： A61K31/437 ,  A61K31/4985 ,  C07D471/14 ,  C07D471/22 ,  C07D498/14 ,  C07D471/12 ,  A61K45/06 ,  A61K31/4375 ,  A61K31/444 ,  C07D498/22 ,  A61K9/10 ,  A61K9/51

CPC分类号： C07D471/14 ,  A61K9/10 ,  A61K9/5153 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/4985 ,  A61K45/06 ,  C07D471/12 ,  C07D471/22 ,  C07D498/14 ,  C07D498/22 ,  A61K2300/00

摘要： Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity.

公开(公告)号：US20170334920A1

公开(公告)日：2017-11-23

申请号：US15669410

申请日：2017-08-04

申请人： ChemoCentryx, Inc.

发明人： Antoni Krasinski ,  Sreenivas Punna ,  Solomon Ungashe ,  Qiang Wang ,  Yibin Zeng

IPC分类号： C07D487/04 ,  C07D471/12 ,  C07D471/04 ,  C07D213/84 ,  C07D213/81 ,  C07D473/00 ,  C07D213/79

CPC分类号： C07D487/04 ,  C07D213/79 ,  C07D213/81 ,  C07D213/84 ,  C07D471/04 ,  C07D471/12 ,  C07D473/00

摘要： Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the identification of CCR2 antagonists.

公开(公告)号：US09765078B2

公开(公告)日：2017-09-19

申请号：US14810225

申请日：2015-07-27

申请人： Millennium Pharmaceuticals, Inc.

发明人： Christopher F. Claiborne ,  Lloyd J. Payne ,  Richard J. Boyce ,  Todd B. Sells ,  Stephen G. Stroud ,  Stuart Travers ,  Tricia J. Vos ,  Gabriel S. Weatherhead

IPC分类号： A61K31/55 ,  C07D471/12 ,  C07D487/04 ,  C07D487/12 ,  C07D487/14 ,  C07D491/14 ,  C07D495/14 ,  C07D513/14

CPC分类号： C07D487/04 ,  C07D487/14 ,  C07D491/14 ,  C07D495/14 ,  C07D513/14

摘要： This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.