CAS: 1282512-48-4; 2-(4-(2-(1-Isopropyl-3-Methyl-1H-1,2,4-Triazol-5-yl)-5,6-Dihydrobenzo[f]Imidazo[1,2-D][1,4]Oxazepin-9-yl)-1H-Pyrazol-1-yl)-2-Methylpropanamide

上下游产品

2-(4-(2-(1-异丙基-3-甲基-1H-1,2,4-三唑-5-基)-5,6-二氢苯并[f]咪唑 2-(4-(2-(1-Isopropyl-3-Methyl-1H-1,2,4-Triazol-5-yl)-5,6-Dihydrobenzo[f]Imidazo[1,2-D][1,4]Oxazepin-9-yl)-1H-Pyrazol-1-yl)-2-Methylpropanoic Acid 1282513-03-4
2-(4-(2-(1-异丙基-3-甲基-1H-1,2,4-三唑-5-基)-5,6-二氢苯并[f]咪唑 Ethyl 2-(4-(2-(1-Isopropyl-3-Methyl-1H-1,2,4-Triazol-5-yl)-5,6-Dihydrobenzo[f]Imidazo[1,2-D][1,4]Oxazepin-9-yl)-1H-Pyrazol-1-yl)-2-Methylpropanoate 1282514-64-0
Cdc0032中间体 9-Bromo-2-(1-Isopropyl-3-Methyl-1H-1,2,4-Triazol-5-yl)-5,6-Dihydrobenzo[f]Imidazo[1,2-D][1,4]Oxazepine 1282514-63-9
2-(2-(4-溴-2-氟苯基)-4-(1-异丙基-3-甲基-1H-1,2,4-三唑-5-基)-1H 2-(2-(4-Bromo-2-Fluorophenyl)-4-(1-Isopropyl-3-Methyl-1H-1,2,4-Triazol-5-yl)-1H-Imidazol-1-yl)Ethanol 1282516-77-1
9-Bromo-N-(1-Iminoethyl)-5,6-Dihydrobenzo[f]Imidazo[1,2-D][1,4]Oxazepine-2-Carboxamide
9-Bromo-5,6-Dihydrobenzo[f]Imidazo[1,2-D][1,4]Oxazepine-2-Carboxamide 1282516-65-7
9-Bromo-5,6-Dihydrobenzo[f]Imidazo[1,2-D][1,4]Oxazepine-2-Carboxylic Acid 1282516-74-8
9-Bromo-2,3-Diiodo-5,6-Dihydrobenzo[f]Imidazo[1,2-D][1,4]Oxazepine 1282516-68-0

📜2-(4-(2-(1-异丙基-3-甲基-1H-1,2,4-三唑-5-基)-5,6-二氢苯并[f]咪唑置于n,N'-羰基二咪唑,甲醇,氨体系中,用 四氢呋喃 用作溶剂,化学反应 1.0H,以90%的收率获得pi3K抑制剂(Gdc-0032)
参考文献:保留pi3Kβ的抑制剂taselisib的生产.第2部分:开发高效且区域选择性的后期方法
标题:保留pi3Kβ的抑制剂taselisib的生产.第2部分:开发高效且区域选择性的后期方法
摘要:开发了磷酸肌醇3-激酶β-保留抑制剂taselisib的高效和区域选择性制造途径.合成的亮点包括:(1)镁介导的具有挑战性的环am的形成;(2)通过与溴丙酮酸的烷基化/缩合来构建区域选择性的咪唑;(3)与2-异丙基乙酰胺zone形成三唑,生成关键的溴苯并x氮杂核心中间体.随后高效的一锅钯催化的miyaura硼酸酯化/铃木交叉偶联/皂化反应,然后与氨进行1,1'-羰基二咪唑介导的偶联反应,形成了五环taselisib.与以前的早期向溴代苯并a庚因核心的早期开发路线相比,这种新的合成方法提供了一种更高效的塔塞来昔路线,并且工艺质量强度显着降低.最后,控制结晶的实施为活性药物成分提供了所需的多晶型形式.
Doi:10.1021/acs.Oprd.9B00050

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:EP-3845540-A1
优先权日:2013-03-13
标题 :Intermediates for the synthesis of benzoxazepin compounds

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.

专利号:WO-2023144235-A1
优先权日:2022-01-27
标 题 :Methods for monitoring and treating warburg effect in patients with pi3k-related disorders
发明人：CANAUD GUILLAUME; LADRAA SOPHIA
权利人:INST NAT SANTE RECH MED; ASSIST PUBLIQUE HOPITAUX PARIS APHP; CENTRE NAT RECH SCIENT; UNIV PARIS CITE
摘要:Using a unique tool of PROS, they demonstrate that PIK3CA mutation leads to GLUT4 membrane accumulation with a negative feedback loop on insulin secretion, a burst of liver IGFBP1 synthesis with IGF1 sequestration and low circulating levels. They further show that AKT2 drives a large part of the phenotype. In addition, they demonstrate for the first time that a single PIK3CA mutation induces metabolic reprogramming with the Warburg effect and protein and lipid synthesis—hallmarks of cancer cells—in vitro, in vivo and in patients. They finally show that alpelisib, an approved PIK3CA inhibitor in oncology, is efficient at preventing and improving PIK3CA-adipose tissue overgrowth and reversing metabolomic anomalies in both animal models and patients. Accordingly, the present invention relates to an in vitro method for monitoring the efficiency of a PI3K inhibitor treatment in a subject in need thereof comprising the step of determining the level of at least one metabolite selected in the group consisting of cis-aconitate, succinic acid, 5-methylcytosine, acetyl-carnitine, acetyl-lysine, argininosuccinate, betaine, butyric acid, carnitine, creatine, glucose, glycine, hexanoyl-carnitine, L-fucose, lactate, L-dihydroorotic acid, linolenic acid, nicotinamide N-oxide, palmitoyl-carnitine, panthotenate, pyruvate, quinolinic acid, tryptophan, urate, in a biological sample obtained from the subject.