Acyl guanidine and amidine prodrugs

Details Acyl guanidine and amidine prodrugs Acyl guanidine and amidine prodrugs

C - Chemistry, Metallurgy

07

K

C07K 5/065 (2006.01) A61K 38/05 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2176414

Acyl guanidine, thioguanidine and amidine compounds are provided which have the structure Image wherein z is a substructure which when linked to Image 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.

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