1449423-87-3

Upstream product

• 1449424-01-4 (3-(2-((3H-[1,2,3]triazolo[4,5-b]pyridine-3-yl)oxy)-5-oxobenzo[4,5]imidazo[1,2-a]pyrimido[4,5-d]pyrimidine-12(5H)-yl)phenyl)carbamic acid tert-butylester 
• 1449423-81-7 4-((3-((tert-butoxycarbonyl)amino)phenyl)amino)-2-chloropyrimidine-5-carboxylic acid 
• 1429497-82-4 ethyl 4-((3-((tert-butoxycarbonyl)amino)phenyl)amino)-2-chloropyrimidine-5-carboxylate 
• 68621-88-5 (3-aminophenyl)carbamic acid tert-butyl ester 
• 51940-64-8 ethyl 2,4-dichloropyrimidine-5-carboxylate 
• 1449424-02-5 12-(3-aminophenyl)-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)benzo[4,5]imidazo[1,2-a]pyrimido[4,5-d]pyrimidin-5(12H)-one 
• 814-68-6 acryloyl chloride 

Relevant academic research and scientific papers

Pyrimidine and tricyclic or pyrimidine and tetracyclic compound and its medicinal composition and use

The invention discloses pyrimidotricyclic compounds or pyrimidotetracyclic compounds having a structure represented by the formula (I), (II) or (III), pharmaceutically-acceptable salts, stereoisomers, or prodrug molecules. The compounds can inhibit various tumor cells, and especially, the compounds can selectively act on lung cancer cells of EGFR L858R/T790 and EGFR E745 A750/T790M. Compared to wild type cancer cells, the IC50 of the compounds is 10 times, 100 times or even 1000 times higher. The compounds are a novel protein kinase inhibitor, which can overcome the drug resistance of EGFR-TKI and has selectivity.

Pyrimido[4,5-d]pyrimidin-4(1H)-one derivatives as selective inhibitors of EGFR threonine790 to methionine790 (T790M) mutants

Catching the mutants: Pyrimido[4,5-d]pyrimidin-4(1H)-one derivatives (see example) were identified as specific inhibitors of EGFRT790M mutants. The compounds bound with T790M or L858R/T790M mutants with significantly lower Kd values