📜3-二甲基氨基苯甲酰氯置于palladium On Activated Charcoal 氢气,三乙胺体系中,用 甲醇,二氯甲烷 用作溶剂,化学反应生成3-(二甲基氨基)-N-[3-[(4-羟基苯甲酰基)氨基]-4-甲基苯基]苯甲酰胺 参考文献:A Novel Series Of P38 Map Kinase Inhibitors For The Potential Treatment Of Rheumatoid Arthritis 标题:A Novel Series Of P38 Map Kinase Inhibitors For The Potential Treatment Of Rheumatoid Arthritis 摘要:A Novel P38 Map Kinase Inhibitor Structural Class Was Discovered Through Selectivity Screening. The Rational Analogue Design,Synthesis And Structure-Activity Relationship Of This Series Of Bisamide Inhibitors Is Reported. The Inhibition In Vitro Of Human P38Alpha Enzyme Activity And Lipopolysaccharide-Induced Tumour Necrosis Factor-Alpha Release Is Described For The Series. The Activity In Vivo And Pharmacokinetic Properties Are Exemplified For The More Potent Analogues. (C) 2004 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2004.08.006
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-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:WO-2022191130-A1 优先权日:2021-03-08 标 题:Method for proliferating cardiomyocytes, method for producing cardiomyocytes, and cardiomyocyte proliferating agent 发明人:YAMASHITA JUN; YOSHIOKA MIKI 权利人:UNIV KYOTO 摘要:Provided are a method for proliferating cardiomyocytes, a method for producing cardiomyocytes, and a cardiomyocyte proliferating agent capable of contributing to cardiac regenerative medicine, that make it possible to induce proliferation of human cardiomyocytes by a drug. The method for proliferating cardiomyocytes, method for producing cardiomyocytes, and cardiomyocyte proliferating agent, including a step for culturing cardiomyocytes in the presence of one or more compounds selected from the group consisting of ALK inhibitors, cytochrome P450 omega hydroxylase inhibitors, and fatty acid synthesis inhibitors