29632-74-4 + 1597407-59-4 = 934660-93-2 反应条件:1.1 Reagents: Lithium Bis(Trimethylsilyl)Amide Solvents: Tetrahydrofuran; 88 Min,20 °C -> 30 °C; 2 H,30 °C1.2 Reagents: Sulfuric Acid Solvents: Water; 25 Min,Rt; 1 H,Rt 标题:Preparation Of Phenylaminophenylhydroxypiperidinylazetidinylmethanone Derivatives For Use As Mek Inhibitors 参考文献:World Intellectual Property Organization]
934664-19-4 + 934666-39-4 = 934660-93-2 反应条件:1.1 Reagents: Diisopropylethylamine Solvents: Tetrahydrofuran; Overnight,Rt1.2 Reagents: Hydrochloric Acid Solvents: Methanol,1,4-Dioxane; 2 H,55 °C 标题:Novel Carboxamide-Based Allosteric Mek Inhibitors: Discovery And Optimization Efforts Toward Xl518 (Gdc-0973) 作者:Rice,Kenneth D.; Aay,Naing; Anand,Neel K.; Blazey,Charles M.; Bowles,Owen J.; Et Al 参考文献:Acs Medicinal Chemistry Letters 日期:2012 卷标:3(5) 页码:416-421]
934663-52-2 = 934660-93-2 反应条件:1.1 Reagents: Trifluoroacetic Acid,Triethylsilane Solvents: Dichloromethane; 0 °C; 3 H,0 °C 标题:Strain-Release-Driven Homologation Of Boronic Esters: Application To The Modular Synthesis Of Azetidines 作者:Fawcett,Alexander; Murtaza,Amna; Gregson,Charlotte H. U.; Aggarwal,Varinder K. 参考文献:Journal Of The American Chemical Society 日期:2019 卷标:141(11) 页码:4573-4578]
2035072-28-5 + 29632-74-4 = 934660-93-2 反应条件:1.1 Reagents: Diisopropylethylamine Solvents: Tetrahydrofuran; 8 H,50 °C 标题:Method For Synthesizing Cobimetinib 参考文献:China]
391211-97-5 + 934666-39-4 = 934660-93-2 反应条件:1.1 Catalysts: Pybop Solvents: Dimethylformamide; 30 Min1.2 Reagents: Diisopropylethylamine; Rt -> 50 °C; 34 H,45 - 50 °C 标题:Process For The Preparation Of Cobimetinib 参考文献:World Intellectual Property Organization]
= 934660-93-2 [标题:Reaction Conditions 标题:Preparation Of The Prodrug Compound And Their Medical Applications 参考文献:World Intellectual Property Organization]
= 934660-93-2 [标题:Reaction Conditions 标题:Process For The Production Of Cobimetinib 参考文献:World Intellectual Property Organization
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-2022233673-A1 优先权日:2019-06-04 标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF 发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M 权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND 摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.
专利号:US-11612610-B2 优先权日:2018-12-14 标题:Mito-magnolol compounds and methods of synthesis and use thereof 发明人:KALYANARAMAN BALARAMAN; ZIELONKA JACEK MICHAL; CHENG GANG; HARDY MICAEL JOËL; OUARI OLIVIER 权利人:MEDICAL COLLEGE WISCONSIN INC; AIX MARSEILLE UNIV; MEDICAL COLLEGE OF WISCONSIN INC 摘要:The present invention provides mito-magnolol compounds, pharmaceutical compositions thereof, and methods of using the mito-magnolol compounds in the treatment of cancer, especially anti-cancer therapy or kinase resistant cancers.
专利号:US-2022118094-A1 优先权日:2019-02-21 标题:Synthesis of biomimetic cell wall structure 发明人:WANG YONG; SHI PENG 权利人:PENN STATE RES FOUND 摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.
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.
1: Krens S, van der Meulen E, Jansman FGA, Burger DM, van Erp NP. Quantification of cobimetinib, cabozantinib, dabrafenib, niraparib, olaparib, vemurafenib, regorafenib and its metabolite regorafenib M2 in human plasma by UPLC-MS/MS. Biomed Chromatogr. 2019 Nov 22:e4758. doi: 10.1002/bmc.4758. [Epub ahead of print] doi: 10.4103/ijo.IJO_2025_18. Available from http://www.ncbi.nlm.nih.gov/books/NBK548657/ doi: 10.1002/ccr3.2297. eCollection 2019 Oct. 8: Sorich MJ, Rowland A, Hopkins AM. Validation of dabrafenib-trametinib prognostic groups in patients treated with vemurafenib and cobimetinib for advanced BRAF-mutated melanoma. Melanoma Res. 2019 Aug 14. doi: 10.1097/CMR.0000000000000634. [Epub ahead of print] doi: 10.1038/s41416-019-0546-y. Epub 2019 Aug 16. doi: 10.1111/exd.14010. Epub 2019 Aug 19. doi: 10.1177/2050313X19847358. eCollection 2019.
合成参考文献
摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355