CYSTEINE PROTEASES INHIBITORS

摘要

Substantially pure diasterioisomeric compounds of formula la, alternatively lb, or a pharmaceutically acceptable salt thereof, including hydrates, where GP is a protective group; R1is a radical selected from the group consisting in phenylmethyl, 4-hydroxy-phenylmethyl, (1H-indol-3-il)methyl and (1H- imidazol-4-il)methyl; R2 is a radical selected from the group consisting in -H, -CH3, -CH2SH, -CH2OH, -CH2Ph, -CH2CO 2H, -CH2CONH2, -CH(OH)CH3, -CH(CH3)CH2CH3, -CH(CH3)2, -CH2CH(CH3)2,-(CH2)2SCH3, -(CH2)2CO2H, -(CH2)CONH2, -(CH2)3NHC(NH)NH2, -(CH2)4NH2, imidazol-4-ylmethyl, 4- hydroxy-phenylmethyl, (1H-indol-3-yl)methyl, (1H-imidazol-4-il)methyl and -(CH 2) n-Ar; and R3 is a radical selected from the group consisting in -O(C1-C4) alkyl, -O(C2-C4) alkenyl,-O(C2-C4) alkynyl, -O(C1-C4) alkyl-Ar, -OAr, -NRa Ar, -N(Ra )[(C1-C4) alkyl-Ar], y-NRa OAry -N(Ra )[O(C1-C4) alkyl-Ar]. Said compounds are inhibitors of the cruzain, rhodesian and falcipain cysteine proteases, and are therefore, used for the treatment and/or prevention of pathologies such as Chagas's disease, African trypanosomiasis or malaria.