2-(2-氟-4-碘苯胺)-3,4-二氟苯甲酸置于盐酸体系中,用 水,甲苯,乙腈 作为反应溶剂,化学反应生成 N-[(2R)-2,3-二羟基丙氧基]-3,4-二氟-2-[(2-氟-4-碘苯)氨基]苯甲酰胺 参考文献:Compositions Of Essentially Pure Form Iv Of N-((R)-2,3-Dihydroxypropoxy)-3,4-Difluoro-2-(2-Fluoro-4-Iodo-Phenylamino)-Benzamide And Uses Thereof 标题:Compositions Of Essentially Pure Form Iv Of N-((R)-2,3-Dihydroxypropoxy)-3,4-Difluoro-2-(2-Fluoro-4-Iodo-Phenylamino)-Benzamide And Uses Thereof 摘要:本公开涉及:A)基本纯度的n-((R)-2,3-二羟基丙氧基)-3,4-二氟-2-(2-氟-4-碘苯胺基)-苯甲酰的iv型晶体组合物;b)包含基本纯度的n-((R)-2,3-二羟基丙氧基)-3,4-二氟-2-(2-氟-4-碘苯胺基)-苯甲酰的iv型晶体组合物的药物组合物,以及可选的药用载体;和c)通过将基本纯度的n-((R)-2,3-二羟基丙氧基)-3,4-二氟-2-(2-氟-4-碘苯胺基)-苯甲酰的iv型晶体组合物给予需要的受试者来治疗肿瘤,癌症或rasopathy障碍的方法.
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-12391691-B2 优先权日:2018-11-16 标题:Synthesis of key intermediate of KRAS G12C inhibitor compound 发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY 权利人:AMGEN INC 摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:US-2025206736-A1 优先权日:2019-11-14 标题 :Synthesis of kras g12c inhibitor compound 发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN 权利人:AMGEN INC 摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
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-9650407-B2 优先权日:2011-11-02 标 题 :Reprogramming of cellular adhesion 发明人:GARTNER ZEV JORDAN; SELDEN NICHOLAS SCOTT; TODHUNTER MICHAEL E; LIANG SAMANTHA ISABEL; WEBER ROBERT JOSEPH; JEE NOEL YOUNGHO; LIU JENNIFER S 权利人:UNIV CALIFORNIA 摘要:Disclosed are membrane-anchored polynucleotides, and compositions comprising the membrane-anchored polynucleotides. Also disclosed are the processes for the synthesis of these compounds, compositions comprising such compounds, and the use of such compounds and compositions in research and therapeutic applications.
专利号:US-2024400576-A1 优先权日:2021-09-03 标 题:Nitrogen-containing derivatives of salinomycin, synthesis and uses thereof 发明人:RODRIGUEZ RAPHAËL; CZERWONKA DOMINIKA; ANTOSZCZAK MICHAL; HUCZYNSKI ADAM 权利人:CENTRE NAT RECH SCIENT; INST CURIE; INST NAT SANTE RECH MED; ADAM MICKIEWICZ UNIV 摘要:The present invention relates to nitrogen-containing derivatives of salinomycin having the formula (I), as well as pharmaceutically acceptable salt thereof, and synthesis and uses thereof, in particular for the treatment and/or prevention of cancer including for preventing cancer metastasis and/or for preventing cancer recurrence and/or for decreasing resistance to a chemotherapy in a subject.
1: Paulo JA, McAllister FE, Everley RA, Beausoleil SA, Banks AS, Gygi SP. Effects of MEK inhibitors GSK1120212 and PD0325901 in vivo using 10-plex quantitative proteomics and phosphoproteomics. Proteomics. 2014 Sep 5. doi: 10.1002/pmic.201400154. [Epub ahead of print] [Epub ahead of print] doi: 10.1016/j.bone.2013.11.013. Epub 2013 Nov 20. doi: 10.1021/bi200542r. Epub 2011 Aug 26. doi: 10.1158/1535-7163.MCT-10-0062. Epub 2010 Jun 29. 6: Hennig M, Yip-Schneider MT, Wentz S, Wu H, Hekmatyar SK, Klein P, Bansal N, Schmidt CM. Targeting mitogen-activated protein kinase kinase with the inhibitor PD0325901 decreases hepatocellular carcinoma growth in vitro and in mouse model systems. Hepatology. 2010 Apr;51(4):1218-25. doi: 10.1002/hep.23470. doi: 10.1089/jop.2009.0060. 9: Leyton J, Smith G, Lees M, Perumal M, Nguyen QD, Aigbirhio FI, Golovko O, He Q, Workman P, Aboagye EO. Noninvasive imaging of cell proliferation following mitogenic extracellular kinase inhibition by PD0325901. Mol Cancer Ther. 2008 Sep;7(9):3112-21. doi: 10.1158/1535-7163.MCT-08-0264. doi: 10.1089/thy.2007.0357.
合成参考文献
参考文献:10.2165/11591380-000000000-00000 摘要:Natarajan N, Telang S, Miller D, Chesney J. Novel immunotherapeutic agents and small molecule antagonists of signalling kinases for the treatment of metastatic melanoma. Drugs. 2011 Jul 09;71(10):1233–50. doi: 10.2165/11591380-000000000-00000.