Method of modulating stress-activated protein kinase system

摘要

Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.

主权项

1. A compound of Genus 1a: wherein R2 is selected from the group consisting of C2-C10 alkenyl, C1-C10 haloalkyl, C1-C10 nitroalkyl, C1-C10 thioalkyl, C1-C10 hydroxyalkyl, hydroxyl, C1-C10 alkoxyalkyl, C1-C10 carboxy, CO-uronide, CO-monosaccharide, CO-oligosaccharide, and CO-polysaccharide; R3 is selected from the group consisting of hydrogen, C1-C10 alkyl, substituted C1-C10 alkyl, C2-C10 alkenyl, C1-C10 haloalkyl, C1-C10 nitroalkyl, C1-C10 thioalkyl, C1-C10 hydroxyalkyl, C1-C10 alkoxy, phenyl, substituted phenyl, halogen, hydroxyl, C1-C10 alkoxyalkyl, C1-C10 carboxy, C1-C10 alkoxycarbonyl, CO-uronide, CO-monosaccharide, CO-oligosaccharide, and CO-polysaccharide; R1 is hydrogen; R4 is hydrogen; and X1 X2, X3, X4 and X5 are independently selected from the group consisting of hydrogen, halogen, and hydroxyl, provided that at least one of X1 X2, X3, X4 and X5 is not H.