DERIVATIVE OF 2-(3H)-OXAZOLONE, METHODS OF ITS SYNTHESIS, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD OF INHIBITION OF COX-2 ACTIVITY Russian patent published in 2002 - IPC

Abstract RU 2194043 C2

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

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RU 2 194 043 C2

Authors

Pujg Duran Karles

Pukhol' Nogera Ferran

Fernandes Forner Dolors

Dates

2002-12-10Published

1997-03-19Filed