| abstract |
Prodrugs of thrombin inhibitors of the formula 1 R1 is R3 or A1C(O)N(R4)(R5) or A1C(O)OR4 A1 is C1-5 alkylene R2 (which replaces one of the hydrogen atoms in the amidino unit of Pab-H ) is OH, OC(O)R6, C(O)R7 or C(O))CH(R8)OC(O)R9 R3 is H, C1-10 alkyl, C1-3 alkylphenyl optionally substituted with alkyl, nitro or halogen R4, R5, R6, R7, R8, and R9 are disclosed in the specification. Further claimed is the use of these compounds in the treatment of thrombosis, hypercoagulability in blood and tissues. |