3-amino-1,2-dihydropyrid-1-yl(and 5-amino-1,6-dihydro-6-oxo(and 5,6-dioxo)pyrimidin-1-yl)-acetyl-argininal derivatives, useful for the treatment of blood coagulation and thrombosis

摘要

The compound of formula (I), wherein: X is -S(O)2-, -N(R')-S(O)2-, -(C=O)-, -OC(=O)-, -NH-C(=O)-, -P(O)(R")- and a direct link, wherein R' is H, alkyl, aryl or aralkyl, and R" is NR', OR', R', or SR', with the proviso that R" is not NH, OH, H, or SH, and; R1 is: alkyl, alkyl substituted with optionally substituted cyclic alkyl, or is optionally substituted 4-10 membered heterocycloalkyl, 4-10 membered heterocyclo, alkenyl, aryl, cyclic alkyl, heteroaryl, aralkyl, heteroaralkyl, aralkenyl or heteroaralkenyl, or a group of formula 13-16, or is difluoromethyl, perfluoroalkyl, perfluoroaryl, perfluoroaralkyl or hydrogen provided that if X is not a direct link, then R1 is not H; i is 0, 1 or 2; the heteroatoms are O, N, or S(O)i R2 is H, alkyl or alkenyl R3 is a group of formula II, wherein W is nitrogen or carbon; Het is a group of formula III, wherein R4, R5, R6, and R7 are as defined in the specification. The compounds of formula I are useful in treating thrombosis or for inhibiting blood coagulation.