📜(2-(6-(1H-Indol-4-yl)-1-(Tetrahydro-2H-Pyran-2-yl)-1H-Indazol-4-yl)Oxazol-5-yl)(4-Isopropylpiperazin-1-yl)Methanone置于aluminum (III) Chloride,Lithium Aluminium Tetrahydride,甲醇,三甲基氯硅烷,三乙胺体系中,用 四氢呋喃,乙酸乙酯 用作溶剂,化学反应 3.5H,以81%的收率获得奈米利塞 参考文献: Processes To Make Indazole Derivatives[fr] Procédés Pour Fabriquer Des Dérivés D'Indazole 标题: Processes To Make Indazole Derivatives[fr] Procédés Pour Fabriquer Des Dérivés D'Indazole 摘要:本发明提供了制备化合物(iv)及其盐的新工艺,新中间体,以及新的盐和其多晶形式.
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-2022411407-A1 优先权日:2019-11-15 标题:Aryl aminopyrimidines as dual mertk and tyro3 inhibitors and methods thereof 发明人:WANG XIAODONG; ZHOU YUBAI; DING RANSHENG; KONG DEYU; FRYE STEPHEN 权利人:UNIV NORTH CAROLINA CHAPEL HILL 摘要:Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.
1: Begg M, Edwards CD, Hamblin JN, Pifani E, Wilson R, Gilbert J, Vitulli G, Mallett D, Morrell J, Hingle MI, Uddin S, Ehtesham F, Marotti M, Harell A, Newman C, Fernando D, Clark J, Cahn A, Hessel EM. Translation of inhaled drug optimization strategies into clinical pharmacokinetics and pharmacodynamics using GSK2292767A, a novel inhaled PI3Kδ inhibitor. J Pharmacol Exp Ther. 2019 Apr 2. pii: jpet.119.257311. doi: 10.1124/jpet.119.257311. [Epub ahead of print] doi: 10.1002/cpdd.614. Epub 2018 Oct 10. doi: 10.1124/jpet.118.249516. Epub 2018 Sep 14. doi: 10.1016/j.clinthera.2018.06.011. Epub 2018 Jul 25.
合成参考文献
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