PHARMACEUTICAL COMPOSITIONS AND METHODS FOR APPLICATION OF 4-PREGNEN-11β-17-21-TRIOL-3,20-DIONE DERIVATIVES Russian patent published in 2019 - IPC A61K31/575 A61K47/00 A61P27/02 

FIELD: medicine.

SUBSTANCE: group of inventions relates to the field of medicine, namely to ophthalmology, and is intended for the treatment of an eye disease selected from acne rosacea, dry eye, blepharitis and dysfunction of the meibomian gland. For the treatment of this ocular disease associated with the modulation of the glucocorticoid and/or mineralocorticoid receptor, is administered locally to a patient in need thereof, pharmaceutical composition comprising a therapeutically effective amount of a compound selected from: (8S,9S,10R,11S,13S,14S,17R)-17-glycoloyl-11-hydroxy-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene-17-yl phenylacetate; (8S,9S,10R,11S,13S,14S,17R)-17-glycoloyl-11-hydroxy-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene-17-yl octanoate; (8S,9S,10R,11S,13S,14S,17R)-17-glycoloyl-11-hydroxy-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene-17-yl hexanoate; (8S,9S,10R,11S,13S,14S,17R)-17-glycoloyl-11-hydroxy-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene-17-yl benzoate; (8S,9S,10R,11S,13S,14S,17R)-17-glycoloyl-11-hydroxy-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene-17-yl heptanoate; (8S,9S,10R,11S,13S,14S,17R)-17-glycoloyl-11-hydroxy-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene-17-yl 2-methylpropanoate; and (8S,9S,10R,11S,13S,14S,17R)-17-glycoloyl-11-hydroxy-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene-17-yl rel-cyclopentanecarboxylate. Ophthalmic composition for local use for the treatment of ocular disease associated with modulating the glucocorticoid and/or mineralocorticoid receptor is also provided, the composition contains a pharmaceutically acceptable carrier and the above compound.

EFFECT: use of the group of inventions allows to increase the effectiveness of treatment of an eye disease selected from rosacea on the eyes, dry eyes, blepharitis and dysfunction of the meibomian gland.

51 cl, 4 tbl, 4 ex