Tripeptide esters of therapeutic agents

Disclosed herein are tripeptidyl esters of the formula: D-P wherein D is the residue of a hydroxyl-containing therapeutic agent, and P is an N-terminal tripeptidyl moiety having the amino acid residue sequence: -AA1-AA2-AA3 wherein AA1 is a secondary amino acid residue, AA2 is a primary amino acid r...

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Hauptverfasser: THOMAS, ALFORD MITCHELL, MARCOTTE, PATRICK ALLEN, FRIEBERG, LESLIE ALAN
Format: Patent
Sprache:eng ; fre ; ger
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Zusammenfassung:Disclosed herein are tripeptidyl esters of the formula: D-P wherein D is the residue of a hydroxyl-containing therapeutic agent, and P is an N-terminal tripeptidyl moiety having the amino acid residue sequence: -AA1-AA2-AA3 wherein AA1 is a secondary amino acid residue, AA2 is a primary amino acid residue and AA3 is an N-terminal amino acid residue capable of acting as an aminopeptidase substrate, and the pharmaceutically acceptable salts thereof. The tripeptidyl esters have been found to release the therapeutic agent in the presence of aminopeptidase