CAS: 677297-51-7; 3,3'-(2,4-Diaminopteridine-6,7-Diyl)Diphenol

上下游产品

(1,2-bis(3-hydroxyphenyl)ethane-1,2-dione) 2,4,5,6-tetraaminopyrimidine sulfate 2,4,5,6-tetraaminopyrimidine

2,4,5,6-四氨基嘧啶,3,3-二羟基苄基 以 水 作为反应溶剂,化学反应 3.0H,以93.3%的收率获得产物3,3'-(2,4-二氨基-6,7-蝶啶二基)二苯酚
参考文献:Discovery Of 3,3'-(2,4-Diaminopteridine-6,7-Diyl)Diphenol As An Isozyme-Selective Inhibitor Of Pi3K For The Treatment Of Ischemia Reperfusion Injury Associated With Myocardial Infarction
标题:Discovery Of 3,3'-(2,4-Diaminopteridine-6,7-Diyl)Diphenol As An Isozyme-Selective Inhibitor Of Pi3K For The Treatment Of Ischemia Reperfusion Injury Associated With Myocardial Infarction
摘要:In Studies Aimed Toward Identifying Effective And Safe Inhibitors Of Kinase Signaling Cascades That Underlie Ischemia/reperfusion (I/r) Injury,We Synthesized A Series Of Pteridines And Pyridopyrazines. The Design Strategy Was Inspired By The Examination Of Naturally occurring Pi3K Inhibitors Such As Wortmannin And Quercetin,And Building A Pharmacophore-Based Model Used For Optimization. Structural Modifications Led To Hybrid Molecules Which Incorporated Aminopyrimidine And Aminopyridine Moieties With Atp Mimetic Characteristics Into The Pharmacophore Motifs To Modulate Kinase Affinity And Selectivity. Elaborations Involving Substitutions Of The 2 And 4 Positions Of The Pyrimidine Or Pyridine Ring And The 6 And 7 Positions Of The Central Pyrazine Ring Resulted In In Vivo Activity Profiles Which Identified Potent Inhibitors Of Vascular Endothelial Growth Factor (Vegf) Induced Vascular Leakage. Pathway Analysis Identified A Diaminopteridine-Diphenol As A Potent And Selective Phosphatidylinositol-3-Kinase (Pi3K) Inhibitor. The Structure-Activity Relationship Studies Of Various Analogues Of Diaminopteridine-Diphenol-Based On Biochemical Assays Resulted In Potent Inhibitors Of Pi3K.
DOI:10.1021/jm051056C

专利信息

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

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-2023192681-A1
优先权日:2019-11-14
标 题 :Improved synthesis of kras g12c inhibitor compound

专利号:US-11299491-B2
优先权日:2018-11-16
标 题:Synthesis of key intermediate of KRAS G12C inhibitor compound

专利号:US-2025206735-A1
优先权日:2018-11-16
标题:Synthesis of key intermediate of kras g12c inhibitor compound