2,6-二氯苯乙腈置于peppsitm-Ipr 硫酸,Potassium Tert-Butylate,Sodium T-Butanolate体系中,用 甲苯 用作溶剂,化学反应 23.0H,反应生成5-(2,6-二氯苯基)-2-((2,4-二氟苯基)硫基)-6H-嘧啶并[1,6-B]哒嗪-6-酮 参考文献:Rapid Synthesis Of Vx-745: P38 Map Kinase Inhibition In Werner Syndrome Cells 标题:Rapid Synthesis Of Vx-745: P38 Map Kinase Inhibition In Werner Syndrome Cells 摘要:The P38 Mitogen-Activated Protein Kinase Inhibitor Vx-745 Is Prepared Rapidly And Efficiently In A Four-Step Sequence Using A Combination Of Conductive Heating And Microwave-Niediated Steps. Its Inhibitory Activity Was Confirmed In Htert Immortalized Hca2 And Ws Dermal Fibroblasts At 0.5-1.0 Mu M Concentration By Elisa And Immunoblot Assay,And Displays Excellent Kinase Selectivity Over The Related Stress-Activated Kinase Jnk. (C) 2007 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2007.07.016
专利号:US-12383499-B2 优先权日:2018-01-01 标题:Scale up synthesis of silicasome nanocarriers 发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG 权利人:UNIV CALIFORNIA 摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).
专利号:US-12006337-B2 优先权日:2018-05-30 标题:Mitogen-activated protein kinase inhibitors, methods of making, and methods of use thereof 发明人:HOLTZMAN MICHAEL J; ROMERO ARTHUR G; GEROVAC BENJAMIN J; HAN ZHENFU; KEELER SHAMUS P; WU KANGYUN; ZHANG YONG 权利人:WASHINGTON UNIVERSITY ST LOUIS 摘要:Compounds that inhibit mitogen-activated protein kinases (MAPKs) are disclosed. Some inhibitor compounds specifically target a single MAPK such as MAPK13, while others target multiple MAPKs such as MAPK13 and MAPK12. The compounds can be used therapeutically for a variety of diseases, including cancer and respiratory diseases. Methods of synthesis of the compounds are also disclosed.
专利号:US-2025289827-A1 优先权日:2022-12-02 标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof 发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN 权利人:C4 THERAPEUTICS INC 摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.
专利号:US-2022143183-A1 优先权日:2019-02-23 标题:Photoswitchable protacs and synthesis and uses thereof 发明人:TRAUNER DIRK; REYNDERS MARTIN; MATSUURA BRYAN; BEROUTI MARLEEN; PAGANO MICHELE 权利人:UNIV NEW YORK 摘要:Provided are compounds, which may be referred to as PHOTACs (photoswitchable proteolysis targeting chimeras), and compositions, kits, and methods of making and using PHOTACs. PHOTACs have one or more E3 ligase ligand(s), one or more photoswitchable group(s), optionally, one or more linker(s), and one or more ligand(s) for a target protein. PHOTACs may be suitable for use in methods to treat diseases, such as, for example, cancer. PHOTACs may also be suitable for use in methods to induce selective degradation of a target protein.
专利号:CN-108821968-A 优先权日:2018-06-28 标题:Preparation method of in-situ acid resin catalyzed synthesis of higher carbon alkyl acrylate