CAS: 1268454-23-4; (6-(2-Aminobenzo[d]Oxazol-5-yl)Imidazo[1,2-A]Pyridin-3-yl)(Morpholino)Methanone

上下游产品

(6-Bromoimidazo[1,2-A]Pyridin-3-yl)(Morpholino)Methanone 1434089-03-8

📜6-溴咪唑并[1,2-A]吡啶-3-羧酸乙酯置于n-甲基咪唑,四(三苯基膦)钯,Lithium Hydroxide Monohydrate,N,N,N',N'-Tetramethylchloroformamidinium Hexafluorophosphate,Sodium Carbonate体系中,用 四氢呋喃,1,4-二氧六环,甲醇,水,乙腈 用作溶剂,化学反应 26.0H,反应生成[6-(2-氨基-5-苯并噁唑基)咪唑并[1,2-A]吡啶-3-基]-4-吗啉-甲酮
参考文献:作为潜在结直肠癌药物的 Pi3Kα 选择性抑制剂的设计,合成和生物评价
标题:作为潜在结直肠癌药物的 Pi3Kα 选择性抑制剂的设计,合成和生物评价
摘要:磷酸肌醇 3 激酶 (Pi3K)/雷帕霉素信号通路哺乳动物靶标的失调与多种人类癌症有关,近年来针对 Pi3Kα 的异构体选择性抑制剂引起了人们的极大兴趣.在本研究中,我们基于临床候选tak-117(8A)设计并合成了三个系列的取代苯并恶唑衍生物.详细的构效关系 (Sar) 研究确定了带有喹喔啉支架的最佳化合物18A .与对照8A相比,18A对 Pi3Kα 的抑制活性高出 4.4 倍(ic 50:2.5 Vs 11 Nm),并且比其他 Pi3K 具有更好的异构体选择性.此外,18A对 Hct-116 细胞系的抗增殖作用强于 1.5 倍(ic 50: 3.79 Vs 5.80 μm),并且比正常组织细胞具有更好的选择性.还研究了18A的潜在抗肿瘤机制和体外代谢稳定性.值得注意的是,药代动力学测定表明,与8A相比,18A具有更高的血浆暴露量,更高的最大浓度和更短的消除时间.
Doi:10.1016/j.Ejmech.2023.115754

专利信息

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-2023192681-A1
优先权日:2019-11-14
标 题 :Improved synthesis of kras g12c inhibitor compound

专利号:US-11299491-B2
优先权日:2018-11-16
标 题:Synthesis of key intermediate of KRAS G12C inhibitor compound

专利号:US-2025206735-A1
优先权日:2018-11-16
标题:Synthesis of key intermediate of kras g12c inhibitor compound