CAS: 1173900-33-8; (R)-2-((1-(7-Methyl-2-Morpholino-4-Oxo-4H-Pyrido[1,2-A]Pyrimidin-9-yl)Ethyl)Amino)Benzoic Acid

上下游产品

2-[[(1R)-1-[7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]benzoic acid methyl ester 2-bromobenzoic-acid 2-chloro-3-acetyl-5-methylpyridine

📜2-Amino-3-Acetyl-5-Methylpyridine置于titanium(Iv) Tetraethanolate,Copper(L) Iodide,水,Potassium Carbonate,对甲苯磺酸,L-脯氨酸,Sodium Hydroxide,S-叔丁基亚磺酰胺体系中,用 四氢呋喃,甲醇,二甲基亚砜,甲苯 用作溶剂,化学反应 106.0H,反应生成2-[[(1R)-1-[7-甲基-2-(4-吗啉基)-4-氧代-4H-吡啶并[1,2-A]嘧啶-9-基]乙基]氨基]苯甲酸
参考文献:抗血小板药物azd6482的制备方法
标题:抗血小板药物azd6482的制备方法
摘要:本发明揭示了一种抗血小板药物azd6482(I)的制备方法,其制备步骤包括:以丙醛和乙酰基乙酰胺等常见化工原料制备得到重要中间体3‑乙酰基‑5‑甲基‑2‑吡啶酮(II),该中间体经过氯化,取代,环合,手性胺化还原以及缩合,水解等步骤制得azd6482(I).该制备方法原料易得,工艺简洁,经济环保,适合工业化生产.

专利信息

专利号:WO-2024259491-A1
优先权日:2023-06-23
标 题:New synthesis method
发明人：FORD DANIEL; POZNAKS VIKTORS; FOTINS JURIS; ÄŒERÅ…AKS DMITRIJS
权利人:THE HEART RES INSTITUTE LTD
摘要:The present disclosure generally relates to a process for the synthesis of AZD6482. In particular, the present disclosure also relates to a process for the synthesis of enantiomerically pure AZD6482. The present disclosure also relates to a process for the synthesis of enantiomerically pure intermediates. The present disclosure also relates to compounds prepared by the processes and the use of such compounds to prepare compositions and to treat disorders.

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.

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.