PHENYL-CONTAINING N-ACYLAMINE DERIVATIVES, METHOD FOR PRODUCTION THEREOF, PHARMACEUTICAL COMPOSITION AND USES THEREOF AS ANTI-INFLAMMATORY AND ANALGESIC AGENTS Russian patent published in 2007 - IPC C07C233/51 A61K31/165 A61P29/00 A61P25/16 

Abstract RU 2309144 C2

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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RU 2 309 144 C2

Authors

Nebol'Sin Vladimir Evgen'Evich

Kromova Tat'Jana Aleksandrovna

Zheltukhina Galina Aleksandrovna

Kovaleva Violetta Leonidovna

Dates

2007-10-27Published

2005-03-25Filed