| abstract |
A serine protease inhibitor having the formula (I), comprising: A is H, D, L alpha-hydroxyacetyl optionally substituted, R1, R1-OC (O) -. R1-C (O) -, R1- SO2-, R2OOC- (CHR2) m-SO2-, R2OOC- (CHR2) m-, H2NCO- (CHR2) m-, or an N-protecting group, where R1 is selected from (1-12C), (2 -12C) alkenyl, (2-12C) -alkynyl and (3-8C) cycloalkyl, groups that can be optionally substituted with (3-8C) cycloalkyl, (1-6C) -alkoxy, oxo, OH, COOH, CF3 or halogen, and of (6-14C) aryl, (7-15 C) aralkyl and (8-1) aralkyl and (8-16) aralkenyl, the aryl groups of which may be optionally substituted with (1-6C) alkyl, (3- 8C) -cycloalkyl, (1-6C) alkoxy, OH, COOH, CF3 or halogen; each R2 group is independently H or has the same meaning as R1; m is 1, 2 or 3; B is a bond, an amino acid of the formula -NH-CH [(CH2) pC (O) OH] -C (O) - or an ester derivative thereof and being pigual to 0, 1, 2 or 3, -N ((1-12C) alkyl-CH2-CO-, -N ((2-12C) -alkenyl-CH2-CO -, - N ((2-12C) alkynyl) -CH2-CO-, -N (benzyl ) -CH2-CO-, D-1-Tiq, D-3Tiq, D-Atc, Aic, D-1-Piq, D-3-Piq, or an L- or D-amino acid having a hydrophobic, basic side chain or neutral, amino acid that can be optionally substituted with N- (1-6C) alkyl; or A and B together are the residue R3R4N-CHR5-C (O) - where R3 and R4 independently are R1, ROC (O) -, R1-C (O) -, R1-SO2-, R2OOC- (CHR2) m-SO2-, R2OOC- (CHR2) m-, H2NCO- (CHR2) m-, or an N-protecting group, or one of R3 and R4 is connected with R5 to form a 5- or 6-membered ring together with NC to which they are attached, which ring can be fused with an aliphatic or aromatic 6-membered ring; and R5 is a neutral, basic or hydrophobic side chain; X is an L -amino acid with a hydrophobic side chain ba, serine, threonine, a cyclic amino acid containing |