ACYL GUANIDINE AND AMIDINE PRODRUGS

摘要

Acyl guanidine, thioguanidine and amidine compounds are provided which have the structure <IMG> wherein z is a substructure which when linked to <IMG> forms a prodrug of compounds with pharmaceutically active properties. In preferred embodiments, Z is a thrombin inhibitor substructure containing residues binding at the distal and proximal sites with the proviso that Z does not contain boron or a boron-containing moiety. Ax and A1x may be the same or different and are independently selected from Acyl, H or alkyl, at least one of Ax and A1x being Acyl; and including all stereoisomers thereof, and pharmaceutically acceptable salts thereof.