MODIFIED CYCLOSPORIN THAT CAN BE USED AS PRODRUG AND ITS USING Russian patent published in 2006 - IPC A61K38/13 A61K47/48 A61P27/02 A61P37/00 

FIELD: medicine, pharmacology, pharmacy, antibiotics.

SUBSTANCE: invention relates to a prodrug representing a cyclic undecapeptide wherein its peptide chain comprises at least one amino acid residue of the general formula (I) given in the invention description wherein carbon atom C^a form one bond among bonds in the undecapeptide ring; each substitute among Y substitutes represents hydrogen atom, or they form a bond in common; substitutes R¹ and R³ represent independently of one another hydrogen atom, the group aralkyl, alkaryl, heteroalkyl, heterocycle, alkylheterocycle, heterocycloalkyl or direct or branched alkyl comprising 1-6 carbon atoms wherein indicated groups are substituted optionally with at least one group chosen from: -COOH, -CONHR⁸, -NHC=NH(NH₂), - NHC=NR⁸(NH₂), -NH₂, -NHR⁸, -NR⁸ ₂, -N⁺R⁸ ₃, -OH, -OPO(OR)₂, -OPO(OH)(OR⁸), -OPO(OH)₂, -OSO(OR⁸)₂, -0SO(OH)(OR⁸), -OSO(OH)₂ and different saline forms of these groups wherein each group among substitutes R⁸ independently of one another represents a direct or branched alkyl comprising 1-6 carbon atoms; substitutes R² and R⁴ represent independently of one another hydrogen atom, alkaryl group or direct or branched alkyl comprising 1-6 carbon atoms; substitutes R and R⁶ represent independently of one another hydrogen atom, aralkyl group or direct or branched alkyl comprising 1-6 carbon atoms; substitute R⁷ represents the group aralkyl, alkaryl, heteroalkyl, heterocycle, alkylheterocycle, heterocycloalkyl, or direct or branched alkyl. Also, invention relates to using the indicated prodrug for preparing a medicinal agent used in treatment of pathological states of mucous membranes. Invention provides enhancing availability of the drug in its using.

EFFECT: valuable medicinal properties of drug.

17 cl, 5 tbl, 3 dwg, 5 ex