DERIVATIVE OF 2-(3H)-OXAZOLONE, METHODS OF ITS SYNTHESIS, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD OF INHIBITION OF COX-2 ACTIVITY

摘要

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention relates to novel derivative of 2-(3H)-oxazolone of the formula (I) where R¹ means alkyl group or group -NR⁴R⁵ where each R⁴ and R⁵ means independently hydrogen atom, alkyl or benzyl group; R² means naphthyl, unsubstituted phenyl group or phenyl group substituted with from 1 to 3 halogen atoms, alkyl group, hydroxy-, alkoxy- or trifluoromethyl-group; R³ means hydrogen atom or alkyl group. Method of synthesis of compound of the formula (I) involves interaction of carbamate of the formula (V) with anhydrous acetic acid or interaction of mercapto-derivative of the formula (VIII) with oxidizing agent, or interaction of chlorosulfonyl of the formula (XI) with amine of the formula R⁴-NH-R⁵, or debenzylation of compound of the formula (IX) . Invention relates also to pharmaceutical composition showing anti-inflammatory effect and comprising compound of the formula (I) and pharmaceutically acceptable carrier or diluting agent. Invention relates also to method of inhibition of activity of human or animal COX-2 involving administration of compound of the formula (I) in effective amount. The claimed compounds can be used for production of medicinal agent. EFFECT: new derivatives of 2-(3H)-oxazolone, valuable medicinal properties. 18 cl, 4 tbl