1256591-41-9

Upstream product

• 1256591-29-3 ethyl 2,6-bis(4-cyanophenoxy)isonicotinate 
• 1256591-30-6 2,6-bis(4-cyanophenoxy)isonicotinic acid 
• 160687-48-9 tert-butyl (3-(4-aminopiperidin-1-yl)propyl)carbamate 
• 767-00-0 4-cyanophenol 
• 1604-14-4 2,6-dichloroisonicotinic acid ethyl ester 

Downstream Products

• 1256591-44-2 tert-butyl (3-(4-(2,6-bis(4-carbamimidoylphenoxy)isonicotinamido)piperidin-1-yl)propyl)carbamate 

Relevant academic research and scientific papers

Discovery of pyridyl bis(oxy)dibenzimidamide derivatives as selective matriptase inhibitors

Matriptase belongs to trypsin-like serine proteases involved in matrix remodeling/degradation, growth regulation, survival, motility, and cell morphogenesis. Herein, we report a structure-based approach, which led to the discovery of sulfonamide and amide derivatives of pyridyl bis(oxy)benzamidine as potent and selective matriptase inhibitors. Co-crystal structures of selected compounds in complex with matriptase supported compound designing. Additionally, WaterMap analyses indicated the possibility of occupying a distinct pocket within the catalytic domain, exploration of which resulted in >100-fold improvement in potency. Co-crystal structure of 10 with matriptase revealed critical interactions leading to potent target inhibition and selectivity against other serine proteases.

PROTEASE INHIBITORS

A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility