1430097-79-2

Upstream product

• 53554-29-3 ethyl 4-hydroxy-2-(methylthio)pyrimidine-5-carboxylate 
• 24690-19-5 methanesulfonic acid 4-aminophenyl ester 
• 100-02-7 4-nitro-phenol 
• 20455-07-6 p-nitrophenyl methanesulfonate 

Downstream Products

• 1430097-80-5 ethyl 4-chloro-2-((4-((methylsulfonyl)oxy)phenyl)amino)pyrimidine-5-carboxylate 
• 1430096-59-5 4-((5-carbamoyl-4-(cyclopropylamino)pyrimidin-2-yl)amino)phenyl methanesulfonate 
• 1430096-73-3 4-((5-carbamoyl-4-(cyclobutylamino)pyrimidin-2-yl)amino)phenyl methanesulfonate 
• 1430096-74-4 4-((5-carbamoyl-4-(cyclopentylamino)pyrimidin-2-yl)amino)phenyl methanesulfonate 
• 1430096-85-7 4-((5-carbamoyl-4-((cyclopentylmethyl)amino)pyrimidin-2-yl)amino)phenyl methanesulfonate 
• 1430096-39-1 4-((5-carbamoyl-4-(isobutylamino)pyrimidin-2-yl)amino)phenyl methanesulfonate 
• 1430095-32-1 4-((5-carbamoyl-4-((3-methylbutan-2-yl)amino)pyrimidin-2-yl)amino)phenyl methanesulfonate 
• 1430095-30-9 (R)-4-((5-carbamoyl-4-((3-methylbutan-2-yl)amino)pyrimidin-2-yl)amino) phenyl methanesulfonate 
• 1430095-82-1 (R)-4-((5-carbamoyl-4-((1-phenylethyl)amino)pyrimidin-2-yl)amino)phenyl methanesulfonate 
• 1430095-72-9 4-((5-carbamoyl-4-((3-fluorobenzyl)amino)pyrimidin-2-yl)amino)phenyl methanesulfonate 
• 1430095-73-0 4-((5-carbamoyl-4-((4-fluorobenzyl)amino)pyrimidin-2-yl)amino)phenyl methanesulfonate 
• 1430095-71-8 4-((5-carbamoyl-4-((2-fluorobenzyl)amino)pyrimidin-2-yl)amino)phenyl methanesulfonate 

Relevant academic research and scientific papers

Discovery of diaminopyrimidine-carboxamide derivatives as JAK3 inhibitors

Selective inhibition of janus kinase (JAK) has been identified as an important strategy for the treatment of autoimmune disorders. Optimization at the C2 and C4-positions of pyrimidine ring of Cerdulatinib led to the discovery of a potent and orally bioavailable 2,4-diaminopyrimidine-5-carboxamide based JAK3 selective inhibitor (11i). A cellular selectivity study further confirmed that 11i preferentially inhibits JAK3 over JAK1, in JAK/STAT signaling pathway. Compound 11i showed good anti-arthritic activity, which could be correlated with its improved oral bioavailability. In the repeat dose acute toxicity study, 11i showed no adverse changes related to gross pathology and clinical signs, indicating that the new class JAK3 selective inhibitor could be viable therapeutic option for the treatment of rheumatoid arthritis.

HETEROCYCLIC COMPOUNDS

The present invention relates to novel pyrimidine class of compounds, their pharmaceutically acceptable salts, and pharmaceutically acceptable compositions containing them and their use in medicine.