2295-31-0 + 958852-13-6 = 958852-01-2 反应条件:1.1 Reagents: Acetic Acid,Piperidine Solvents: Ethanol; 30 Min,150 °C; 150 °C -> Rt 标题:Thiazolidinedione Derivatives As Pi3 Kinase Inhibitors And Their Preparation And Use In The Treatment Of Diseases 参考文献:World Intellectual Property Organization]
= 958852-01-2 [标题:Reaction Conditions 标题:Discovery Of Gsk2126458,A Highly Potent Inhibitor Of Pi3K And The Mammalian Target Of Rapamycin 作者:Knight,Steven D.; Adams,Nicholas D.; Burgess,Joelle L.; Chaudhari,Amita M.; Darcy,Michael G.; Et Al 参考文献:Acs Medicinal Chemistry Letters 日期:2010 卷标:1(1) 页码:39-43
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-10772971-B2 优先权日:2017-06-22 标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates 发明人:GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V 权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC 摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.
1. Xie J, Li Q, Ding X, Gao Y. GSK1059615 kills head and neck squamous cell carcinoma cells possibly via activating mitochondrial programmed necrosis pathway. Oncotarget. 2017 Feb 7;8(31):50814-50823. doi: 10.18632/oncotarget.15135.
合成参考文献
参考文献:10.1007/s10555-009-9192-9 摘要:Dovedi SJ, Davies BR. Emerging targeted therapies for bladder cancer: a disease waiting for a drug. Cancer Metastasis Rev. 2009 Dec;28(3-4):355–67. doi: 10.1007/s10555-009-9192-9. 参考文献:10.1021/ml900028r 摘要:Knight SD, Adams ND, Burgess JL, Chaudhari AM, Darcy MG, Donatelli CA, Luengo JI, Newlander KA, Parrish CA, Ridgers LH, Sarpong MA, Schmidt SJ, Van Aller GS, Carson JD, Diamond MA, Elkins PA, Gardiner CM, Garver E, Gilbert SA, Gontarek RR, Jackson JR, Kershner KL, Luo L, Raha K, Sherk CS, Sung CM, Sutton D, Tummino PJ, Wegrzyn RJ, Auger KR, Dhanak D. Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. ACS Med Chem Lett. 2010 Apr 08;1(1):39–43. 摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749