CAS: 1197160-78-3; 1-(4-(4-(Dimethylamino)Piperidine-1-Carbonyl)Phenyl)-3-(4-(4,6-Dimorpholino-1,3,5-Triazin-2-yl)Phenyl)Urea

上下游产品

CAS号50533-97-6 4-二甲氨基哌啶

📜6-(4-硝基苯基)-1,3,5-三嗪-2,4-二胺置于吡啶,氢气,Sodium Hydride体系中,用 四氢呋喃,二氯甲烷,二甲基亚砜,N,N-二甲基甲酰胺,Mineral Oil 用作溶剂,化学反应 17.0H,反应生成N-[4-[[4-(二甲基氨基)-1-哌啶基]羰基]苯基]-N'-[4-[4,6-二(4-吗啉基)-1,3,5-三嗪-2-基]苯基]脲
参考文献:格达列西的新的实用合成
标题:格达列西的新的实用合成
摘要:以百克级规模开发了一种新的,实用且聚合的抗肿瘤药gedatolisib合成路线,该路线避免了pd偶联方法.关键步骤是采用6-(4-硝基苯基)-1,3,5-三嗪-2,4-二胺和2,2'-二氯二乙醚制备关键的4,4'-(6-(4-硝基苯基) )-1,3,5-三嗪-2,4-二基)二吗啉的收率为77%,纯度为98.8%.在五个简单的步骤中以98.6%的纯度(HPLC)获得了gedatolisib的收率为48.6%.给出了该路线涉及的中间体和最终产物的纯化方法.
Doi:10.1021/acs.Oprd.7B00298

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.

专利号:US-2022047711-A1
优先权日:2018-12-10
标题 :Photocrosslinking peptides for site specific conjugation to fc-containing proteins
发明人：SADOWSKY JACK; ZACHARIAS NEELIE TYANA
权利人:GENENTECH INC
摘要:Provided herein are peptides having a photocrosslinking moiety useful for the synthesis of antibody-drug conjugates as well as methods of making and using such conjugates.

专利号:US-2022400732-A1
优先权日:2019-03-21
标题:Anti-fructose therapy for colorectal and small intestine cancers
发明人：GONCALVES MARCUS; CANTLEY LEWIS C; YUN JIHYE
权利人:UNIV CORNELL
摘要:As described herein ingestion of high amounts of sugar, especially fructose, can increase the growth of intestinal tumors. Such cancer growth can be inhibited or prevented by limiting the amounts of sugar and amino acids ingested, by inhibiting ketohexokinase (KHK), fructose transport (via GLUT5), fatty acid synthesis (via FASN), phosphoinositide 3-kinases (PI3K), or by limiting amounts of sugar and amino acids ingested while also receiving KHK inhibitors, GLUT5 inhibitors, FASN inhibitors, PI3K inhibitors, or a combination of such inhibitors.

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.