FIELD: organic chemistry, biochemistry, medicine, pharmacy. SUBSTANCE: invention relates to compounds-inhibitors of dipeptidylpeptidase IV of the general formula A- B-C wherein A means amino acid; B means a chemical bond between A and C, or amino acid; C means the stable inhibitor of dipeptidylpeptidase IV with the truncated C-terminal phosphonate residue that represents aminoacylpyrrolidine, aminoacylthiazolidine or N-dipeptidyl, O-acylhydroxylamine. Such compounds-prodrugs are used for treatment of damaged tolerance to glucose, in glucosuria, hyperlipidemia, metabolic acidosis, diabetes mellitus, diabetic neuropathy and nephropathy and complications caused by diabetes mellitus in mammals. Invention describes also pharmaceutical compositions containing such compounds. Invention provides enhancing activity of inhibitors of dipeptidylpeptidase IV and possibility for regulation of its onset effect. EFFECT: valuable medicinal properties of prodrugs. 16 cl, 4 tbl, 2 dwg
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