NEW CYANOPYRIMIDINE DERIVATIVE Russian patent published in 2014 - IPC C07D401/12 C07D401/14 A61K31/506 A61P27/06 

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new N-(4-(6-amino-5-cyano-2-((6-(3-oxo-3-(4-(piperidin-4-ylmethyl)piperazin-1-yl)propyl)pyridin-2-yl)methylthio)pyrimidin-4-yl)phenyl)acetamide of formula

or its pharmaceutically acceptable salt. The invention also refers to a pharmaceutical composition containing a compound of formula (1) or its pharmaceutically acceptable salt and a pharmaceutically acceptable carrier, as well as to a method of treating an ophthalmic disease, and to an aqueous preparation for producing eye drops. The aqueous liquid preparation contains the above pharmaceutical composition and optionally additionally contains one or more additives specified in a pharmaceutically acceptable buffer, an isotonic agent, a preserving agent, a solubilising agent and a pH regulator. The buffer is usually specified in succinic acid, boric acid, phosphoric acid, amino acid and its pharmaceutically acceptable salt. Succinic acid shall be preferred. The isotonic solution represents one or more isotonic agents specified in glucose, sorbitol, mannitol, sodium chloride, potassium chloride, propylene glycol and glycerol. The preserving agent is specified in benzalkonium chloride, benzethonium chloride, benzododecinium bromide, chlorhexidine gluconate, methyl-para-oxybenzoate, propyl-para-oxybenzoate, chlorobutanol and benzyl alcohol. The pH value makes approximately 5.0 to 9.0.

EFFECT: compounds have a safe and potent agonist effect on the adenosine A2a receptor and can find application for treating or preventing an ophthalmic disease, particularly glaucoma.

13 cl, 3 dwg, 2 tbl, 15 ex