Water-soluble prodrugs of chloramphenicol, thiamphenicol, and analogs thereof
AssigneeIntervet Inc.
InventorTomasz W. Glinka
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Abstract
The present invention discloses certain novel prodrugs of chloramphenicol or thiamphenicol, or of an analog of either, including prodrugs of pharmaceutically acceptable salts of chloramphenicol or thiamphenicol or of their analogs, including nitrogen-containing esters of both alcohol groups of such compounds. In certain embodiments these novel prodrugs are sufficiently water-soluble to serve the functions needed of a prodrug of chloramphenicol or thiamphenicol or of an analog of either. In one embodiment, a certain subclass of the compounds also possesses the hydrolytic stability needed to maintain the prodrug in solution in the subject's system until appropriate conditions exist when the prodrug can hydrolyze, releasing the active compound in question.
Claims6
A compound having the Formula (I)
- in which:
- R is selected from the group consisting of
- R3 is selected from the group consisting of dichloromethyl, difluoromethyl, chlorofluoromethyl, chloromethyl, methyl, cyanomethyl, azidomethyl, and aminomethyl;
- and
- —O—C(═O)-Aa-Ll-Mm-Xx—Y is selected from the group consisting of:
- wherein n is an integer from 2-6 and R′ is H, Me or Et;
- and
- wherein n is an integer from 1 to 6 and R′ is Me or Et;
- and pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.