1235893-75-0

Upstream product

• 371-40-4 4-fluoroaniline 
• 49845-33-2 2,4-Dichloro-5-nitropyrimidine 

Downstream Products

• 1448694-40-3 2-chloro-N⁴-(4-fluoro-phenyl)-pyrimidine-4,5-diamine 
• 1448694-41-4 5-chloro-3-(4-fluoro-phenyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidine 
• 1448692-96-3 [3-(4-fluoro-phenyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl]-[1-(tetrahydro-pyran-4-yl)-1H-pyrazol-4-yl]-amine 

Relevant academic research and scientific papers

Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N-9-Diphenyl-9H-purin-2-amine scaffold

Based upon the modeling binding mode of marketed AZD9291 with T790M, a series of N-9-Diphenyl-9H-purin-2-amine derivatives were designed and synthesized with the purpose to overcome the drug resistance resulted from T790M/L858R double mutations. The most potent compound 23a showed excellent enzyme inhibitory activities and selectivity with nanomolar IC50 values for both the single T790M and double T790M/L858R mutant EGFRs, and was more than 8-fold selective for wild type EGFR. Compound 23a displayed strong antiproliferative activity against the H1975 non-small cell lung cancer (NSCLC) cells bearing T790M/L858R. And it was less potent against A549 (WT EGFR and k-Ras mutation) and HT-29 (non-special gene type) cells, showing a high safety index.

TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES

Compounds of the formula (I) in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.