CAS: 1159824-67-5; 5-(2-Amino-8-Fluoro-[1,2,4]Triazolo[1,5-A]Pyridin-6-yl)-N-(Tert-Butyl)Pyridine-3-Sulfonamide

在 盐酸体系中,用 1,4-二氧六环,水 用作溶剂,化学反应 18.0H,反应生成5-(2-氨基-8-氟[1,2,4]三唑并[1,5-A]吡啶-6-基)-N-(叔丁基)-3-吡啶磺酰胺
参考文献:Sar Studies Around A Series Of Triazolopyridines As Potent And Selective Pi3Kγ Inhibitors
标题:Sar Studies Around A Series Of Triazolopyridines As Potent And Selective Pi3Kγ Inhibitors
摘要:Herein We Describe The Sar Of A Novel Series Of 6-Aryl-2-Amino-Triazolopyridines As Potent And Selective Pi3K Gamma Inhibitors. The 6-Aryl-Triazolopyridine Core Was Identified By Chemoproteomic Screening Of A Kinase Focused Library. Rapid Chemical Expansion Around A Bi-Functional Core Identified The Key Features Required For Pi3K Gamma Activity And Selectivity. The Series Was Optimized To Afford 43 (Czc19945),A Potent Pi3K Gamma Inhibitor With High Oral Bioavailability And Selectivity Over Pi3K Alpha And Pi3K Delta. Modification To The Core Afforded 53 (Czc24832) Which Showed Increased Selectivity Over The Entire Kinome In Particular Over Pi3K Beta. (C) 2012 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2012.06.049

专利信息

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.