FIELD: organic chemistry, pharmaceuticals.
SUBSTANCE: invention relates to amine derivatives of general formula I , wherein R1 is hydrogen or hydroxyl; R2 is hydrogen, -COOH, -COOR4 (R4 is C1-C6-alkyl); R3 is hydrogen or hydroxyl; or pharmaceutically acceptable salts thereof. Also disclosed is method for production of said compounds (wherein n = 1 or 2) including activation of carboxyl group of p-hydroxyphenylacetic acid or phenylacetic acid by interaction of with diphenylphosphorylazide and triethylamine in organic solvent under cooling followed by interaction with amine compound. Method for production of said compounds (wherein n = 1) includes converting of p-hydroxyphenylacetic acid or phenylacetic acid to activated N-oxysuccinimide ester by N'dicyclohexylcarbodiimide method followed by interaction of N-succinimide ester with amine derivative. Disclosed are pharmaceutical composition and agent having cyclooxygenase inhibitor activity, containing effective amount of claimed compound (wherein n = 1 or 2) as active ingredient. Also disclosed is method for cyclooxygenase inhibition by administering to mammalian of effective amount of claimed compound (wherein n = 1 or 2) or pharmaceutically acceptable salt thereof.
EFFECT: phenyl-containing N-acylamine derivatives having cyclooxygenase inhibitor activity and useful in treatment pain, inflammation and other disorders of joints and connective tissues.
19 cl, 9 tbl, 19 ex
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