CAS: 1007207-67-1; 5-(7-(Methylsulfonyl)-2-Morpholino-6,7-Dihydro-5H-Pyrrolo[2,3-D]Pyrimidin-4-yl)Pyrimidin-2-Amine

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CAS号402960-38-7 2-氨基嘧啶-5-硼酸频哪醇酯 | CAS号1178564-27-6 4-氯-6,7-二氢-7-(甲... | CAS号1007206-27-0 4-(4,6-二氯-5-(2-... | CAS号1178564-17-4 5-(2-羟基乙基)-2-吗啉...

📜4-(4,6-二氯-5-(2-氯乙基)嘧啶-2-基)吗啉置于bis-Triphenylphosphine-Palladium(II) Chloride,Potassium Phosphate,Potassium Carbonate体系中,用 N-甲基吡咯烷酮,N,N-二甲基甲酰胺 用作溶剂,化学反应生成[5-[7-甲磺酰基-2-(吗啉-4-基)-6,7-二氢-5H-吡咯并[2,3-D]嘧啶-4-基]嘧啶-2-基]胺
参考文献:Discovery And Biological Activity Of A Novel Class I Pi3K Inhibitor,Ch5132799
标题:Discovery And Biological Activity Of A Novel Class I Pi3K Inhibitor,Ch5132799
摘要:Phosphatidylinositol 3-Kinase (Pi3K) Is A Lipid Kinase And A Promising Therapeutic Target For Cancer. Using Structure-Based Drug Design (Sbdd),We Have Identified Novel Pi3K Inhibitors With A Dihydropyrrolopyrimidine Skeleton. Metabolic Stability Of The First Lead Series Was Drastically Improved By Replacing Phenol With Aminopyrimidine Moiety. Ch5132799,A Novel Class I Pi3K Inhibitor,Exhibited A Strong Inhibitory Activity Especially Against Pi3K Alpha (Ic(50) = 0.014 Mu M). In Human Tumor Cell Lines With Pi3K Pathway Activation,Ch5132799 Showed Potent Antiproliferative Activity. Ch5132799 Is Orally Available And Showed Significant Antitumor Activity In Pi3K Pathway-Activated Human Cancer Xenograft Models In Mice. (C) 2011 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2011.01.065

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:CN-108379591-B
优先权日:2018-04-03
标 题 :Synthesis of Immune Agonist Targeting Compounds and Their Applications

专利号:US-11285169-B2
优先权日:2013-03-13
标题 :Methods for modulating chemotherapeutic cytotoxicity
发明人：ROBERTS DAVID D; SOTO PANTOJA DAVID R
权利人:US HEALTH
摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.

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.