| abstract |
(57) [Summary] (Modified) [Structure] A ketone derivative represented by the general formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same as an active ingredient. [Wherein n = 0, 1 ; R 1 is R 10 —CO—, R 10 -O-CO-, R 10 -SO 2 -, R 10 -NH- CO- and; R 2, R 4, R 6 is H, a C 1 to 5 alkyl; R 3, R 5 is H, (substituted) aryl group, (substituted) C 1 to 20 alkyl; R 7 is cycloalkyl, hydroxyl group, The C 1 to 5 alkoxy or the like; R 8 represents H, C 1 to 5 alkyl, (substituted) C 7 to 20 aralkyl; or R 2- R 3 , R 4 -R 5 may form a heterocycle, and R 7 -R 8 may form a cycloalkyl or benzylidene. A is O, S (O) n (where n = 0, 1, 2), N (R 11 ); R 9 is 2-furylmethyl, benzyl, methyl, pyridylmethyl and the like; R 10 is cycloalkyl, Aryl or the like; R 11 represents C 1-15 alkyl] [Effect] This ketone derivative shows a strong inhibitory activity against thiol proteases such as papain, cathepsin B, cathepsin H, cathepsin L, calpain, etc. It is also excellent in absorbability, tissue migration and cell membrane permeability. |