SUBSTITUTED ISOXAZOLES, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD OF INFLAMMATION SUPPRESSION Russian patent published in 2003 - IPC

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to novel substituted isoxazoles of the general formulas (I) , (II) , (III) , (IV) , (V) where R¹ is taken among lower alkyl, carboxyalkyl, alkoxycarbonyl, aminocarbonyl, aminocarbonylalkyl and others; R² is taken among alkylsulfonyl, hydroxysulfonyl and aminosulfonyl; R³ is taken among phenyl or 6-membered heterocycle containing one nitrogen atom being phenyl can be optionally substituted with one or more radicals taken independently among alkyl, cyano-group, halogenalkyl, hydroxyalkyl and others under condition that R² means aminosulfonyl in the case if R² as a substituted phenyl radical is at 3- position of isoxazole; R⁴ is taken among lower alkyl, hydroxyl, carboxyl, halogen atom, lower carboxyalkyl and others; R⁵ is taken among methyl, hydroxy-group and amino-group; R⁶ is taken among phenyl or 6-membered heterocycle containing one nitrogen atom being phenyl can be optionally substituted with one or more radicals taken independently among lower alkylsulfinyl, lower alkyl, cyano-group, lower halogen-alkyl and others; R⁷ is taken among lower alkyl, hydroxyl, carboxyl, halogen atom, lower carboxyl and others; R⁸ means one or more radicals taken independently among hydrogen atom, lower alkylsulfinyl, lower alkyl, cyano-group, lower halogen alkyl and others; R⁹ is taken among alkyl, lower carboxyalkyl, lower alkoxycarbonylalkyl and others; R¹⁰ means one or more radicals taken independently among hydrogen atom, lower alkyl, halogen atom, lower alkoxy-group; R¹¹ is taken among methyl and amino-group; R¹² means one or more radicals taken independently among hydrogen atom, lower alkyl, halogen atom, lower halogenalkyl, lower alkoxy-group; R¹³ is taken among lower alkyl, lower carboxyalkyl, lower alkoxycarbonylalkyl, lower aralkyl; R¹⁴ is taken among methyl and amino-group; and their pharmaceutically acceptable salts. Invention relates also to pharmaceutical composition eliciting activity inhibiting cyclooxygenase-2 activity containing compound of the formula (I) or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier. Invention relates also to method of suppression of states associated with enhanced activity of cyclooxygenase-2, inflammations and associated disorders that involves administration of compound of the formula (I) or its pharmaceutically acceptable salt in patient with indicated disorder or susceptible to this disorder in therapeutically effective dose. Invention provides the development of novel substituted isoxazoles. EFFECT: improved method of treatment, valuable medicinal properties of compounds. 23 cl, 2 tbl