📜2-(2-氟-4-碘苯基氨基)-1,5-二甲基-6-氧代-N-(2-(乙烯基氧基)乙氧基)-1,6-二氢吡啶-3-甲酰胺置于resultant Solution,Ptfe,Cr13体系中,用 甲醇 作为反应溶剂,化学反应生成 Azd 8330; 2-(2-氟-4-碘苯氨基)-N-(2-羟基乙氧基)-1,5-二甲基-6-氧代-1,6-二氢吡啶-3-甲酰胺 参考文献:Crystalline Forms Of 2-(2-Flouro-4-Iodophenylamino)-N-(2-Hydroxyethoxy)-1,5-Dimethyl-6-Oxo-1,6-Dihydropyridine-3-Carboxamide 标题:Crystalline Forms Of 2-(2-Flouro-4-Iodophenylamino)-N-(2-Hydroxyethoxy)-1,5-Dimethyl-6-Oxo-1,6-Dihydropyridine-3-Carboxamide 摘要:本发明揭示了2-(2-氟-4-碘苯氨基)-N-(2-羟乙氧基)-1,5-二甲基-6-氧代-1,6-二氢吡啶-3-羧酰胺的晶体形式,用于治疗哺乳动物中的高增殖性疾病,如癌症和炎症以及炎症状况.还揭示了使用这种化合物治疗哺乳动物的高增殖性疾病的方法和包含这种化合物的制药组合物.
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.
参考文献:10.1038/s41388-018-0274-4 摘要:Morris SM, Mhyre AJ, Carmack SS, Myers CH, Burns C, Ye W, Ferrer M, Olson JM, Klinghoffer RA. A modified gene trap approach for improved high-throughput cancer drug discovery. Oncogene. 2018 May 02;37(31):4226–38. doi: 10.1038/s41388-018-0274-4. 参考文献:10.1186/1756-8722-3-8 摘要:Frémin C, Meloche S. From basic research to clinical development of MEK1/2 inhibitors for cancer therapy. Journal of Hematology & Oncology. 2010 Feb 11;3(1):8. doi: 10.1186/1756-8722-3-8.