THIAZOL DERIVATIVE AND USING IT AS VAP-1 INHIBITOR Russian patent published in 2013 - IPC C07D277/46 C07D417/06 A61K31/426 A61K31/427 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of general formula R¹-NH-X-Y-Z (I), wherein R¹ represents alkylcarbonyl; X represents a bivalent residue of thiazol; Z is described by formula A-B-D-E (II), wherein A represents a bivalent residue of benzene optionally substituted by 1 or 2 halogen atoms, or a bivalent residue of thiophen optionally substituted by a lower alkyl; B represents -(CH₂)_l-NR²-CO-, wherein R² represents hydrogen, l is equal to an integer from 1 to 6, -(CH₂)_m-O-CO- or -(CH₂)_m-S-CO- (wherein m is equal to an integer from 0 to 6); D represents -NR³-, wherein R³ represents hydrogen; E represents amino; Y is described by formula J-L-M (III), wherein J represents a bond, a lower alkylene, -(CH₂)_n-O0-, -(CH₂)_n-CO- (wherein n is equal to an integer from 0 to 6); L represents a bond, -O-, -NH-; M represents a bond, a lower alkylene. Also, the invention refers to a pharmaceutical composition containing the above compounds and possessing vascular adhesive protein 1 (VAP-1) inhibitory activity, a VAP-1 inhibitor, a pharmaceutical agent, to using the compounds of formula (I) and pharmaceutical agent for preventing and treating a VAP-1 related disease, to a method of inhibiting VAP-1, and to a method of preventing or treating the VAP-1 related disease.

EFFECT: compounds of formula (I) as the VAP-1 inhibitors.

14 cl, 2 ex, 2 tbl, 38 ex