89283-49-8

Upstream product

• 74-89-5 methylamine 
• 49845-33-2 2,4-Dichloro-5-nitropyrimidine 

Downstream Products

• 904913-82-2 N²-(2,4-difluoro-phenyl)-N⁴-methyl-5-nitro-pyrimidine-2,4-diamine 
• 904913-75-3 N²-(2,6-difluoro-phenyl)-N⁴-methyl-5-nitro-pyrimidine-2,4-diamine 
• 515824-85-8 N²-(4-fluoro-phenyl)-N⁴-methyl-5-nitro-pyrimidine-2,4-diamine 
• 5177-26-4 2,4-Bis(methylamino)-5-nitropyrimidin 
• 515824-68-7 2-(3.4-dichlorophenylamino)-4-methylamino-5-nitro-pyrimidine 
• 330550-94-2 4-(Methylamino)-2-[[4-(morpholin-4-yl)phenyl]amino]-5-nitropyrimidine 
• 1273388-39-8 2-(3-methoxypropyl)-9-methyl-7-({3-[4-(trifluoromethyl)phenyl]azetidin-1-yl}carbonyl)-7,9-dihydro-8H-purine-8-one 
• 1273307-62-2 2-(2-methoxyethyl)-9-methyl-7-({3-[4-(trifluoromethyl)phenyl]azetidin-1-yl}carbonyl)-7,9-dihydro-8H-purine-8-one hydrochloric acid salt 
• 13784-17-3 5-amino-4-methylaminopyrimidine 
• 1350544-88-5 8-phenylamino-9-methyl-2-(4-(4-methylpiperazin-1-yl)phenylamino)-9H-purine 
• 1350545-61-7 4-methylamino-2-(4-(4-methylpiperazin-1-yl)phenylamino)-5-aminopyrimidine 
• 1273315-68-6 2-cyclohexyl-9-methyl-7-{[2-(trimethylsilyl)ethoxy]methyl}-7,9-dihydro-8H-purine-8-one 
• 1273315-70-0 2-cyclohexyl-9-methyl-7,9-dihydro-8H-purine-8-one 
• 1273315-37-9 9-methyl-2-(2-phenylethyl)-7,9-dihydro-8H-purine-8-one 

Relevant academic research and scientific papers

Synthesis and biological evaluation of pyrimidine derivatives as novel human Pin1 inhibitors

Pin1 (Protein interacting with NIMA1) is a cis–trans isomerase and promotes the amide bond rotation of phosphoSer/Thr-Pro motifs in its substrates. Inhibition of Pin1 might be a novel strategy for developing anticancer agents. Herein, a series of pyrimidi

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.

FUSED-BICYCLIC ARYL QUINOLINONE DERIVATIVES AS MUTANT-ISOCITRATE DEHYDROGENASE INHIBITORS

The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula (I) where A, B, U, V, Z, W1, W2, W3, and R1-R6 are described herein.

Substituted purine derivative and preparation method and application thereof

The invention discloses a substituted purine derivative with the structure as shown in a general formula I and a preparation method and application of the derivative. The invention further provides N-oxide or a stereisomer form or a stereisomer mixture or pharmaceutically acceptable salts of the substituted purine derivative. The invention further provides the preparation method of the substituted purine derivative and the application of a composition containing one or more compounds in preparing drugs for resisting hepatitis B. Please see the formula in the description.

INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR

Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.

NOVEL CEPHALOSPORIN DERIVATIVE AND PHARMACEUTICAL COMPOSITION THEREOF

The present invention relates to novel cephalosporin derivatives represented by Chemical Formula 1. Wherein, X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. According to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for the broad spectrum of antibiotic resistant, low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.

HETEROARYL COMPOUNDS AND USES THEREOF

The present invention relates to compounds useful as inhibitors of protein kinases, containing a cysteine residue in the ATP binding site. The invention further provides for pharmaceutically acceptable compositions comprising therapeutically effective amounts of one or more of the protein kinase inhibitor compounds and methods of using said compositions in the treatment of cancers and carcinomas.

ARYLAMINO PURINE DERIVATIVES, PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF

Arylamino purine derivatives represented by formula I and their preparation method are disclosed, wherein each substituent is defined as in the description. The derivatives have an inhibitory effect on non-small cell lung cancer with deletion mutation of exon 19 or L858R point mutation of exon 21 in epidermal growth factor receptor (EGFR).

Structural optimization and structure-activity relationships of N 2-(4-(4-methylpiperazin-1-yl)phenyl)- N 8-phenyl-9 H -purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations

This paper describe the structural optimization of a hit compound, N 2-(4-(4-methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine- 2,8-diamine (1), which is a reversible kinase inhibitor targeting both EGFR-activating and drug-resistance (T790M) mutations but has poor binding affinity. Structure-activity relationship studies led to the identification of 9-cyclopentyl-N2-(4-(4-methylpiperazin-1-yl)phenyl)-N 8-phenyl-9H-purine-2,8-diamine (9e) that exhibits significant in vitro antitumor potency against the non-small-cell lung cancer (NSCLC) cell lines HCC827 and H1975, which harbor EGFR-activating and drug-resistance mutations, respectively. Compound 9e was further assessed for potency and selectivity in enzymatic assays and in vivo anti-NSCLC studies. The results indicated that compound 9e is a highly potent kinase inhibitor against both EGFR-activating and resistance mutations and has good kinase spectrum selectivity across the kinome. In vivo, oral administration of compound 9e at a dose of 5 mg/kg caused rapid and complete tumor regression in a HCC827 xenograft model, and an oral dose of 50 mg/kg initiated a considerable antitumor effect in an H1975 xenograft model.

NOVEL CEPHALOSPORIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF

The present invention relates to novel cephalosporin derivatives represented by Chemical Formula 1. Wherein, X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. According to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for the broad spectrum of antibiotic resistant, low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.