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
Title | Year | Author | Number |
---|---|---|---|
BISAMIDES DERIVATIVE OF DICARBOXYLIC ACIDS, USE THEREOF, PHARMACEUTICAL COMPOSITION BASED THEREON, METHODS FOR PRODUCTION THEREOF | 2018 |
|
RU2725881C2 |
BICAMIDES DERIVATIVE OF DICARBOXYLIC ACIDS, USE THEREOF, A PHARMACEUTICAL COMPOSITION BASED THEREON, METHODS FOR PRODUCTION THEREOF | 2018 |
|
RU2721421C2 |
DERIVATIVES OF BISAMIDES OF DICARBOXYLIC ACIDS, USE THEREOF, PHARMACEUTICAL COMPOSITION BASED THEREON, METHODS FOR PRODUCTION THEREOF | 2018 |
|
RU2709529C1 |
BISAMIDE DERIVATIVE OF DICARBOXYLIC ACIDS, ITS USE, PHARMACEUTICAL COMPOSITION BASED ON IT, METHODS FOR ITS OBTAINING | 2020 |
|
RU2815401C2 |
DERIVATIVE OF BISAMIDES OF DICARBOXYLIC ACIDS, ITS USE, PHARMACEUTICAL COMPOSITION BASED ON IT, METHODS FOR ITS PRODUCTION | 2018 |
|
RU2719464C2 |
NITROXYCOMPOUNDS AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF SHOWING ANTI-INFLAMMATORY, ANALGETIC AND ANTITHROMBOCYTIC ACTIVITY | 1995 |
|
RU2145595C1 |
DICARBOXYLIC ACID BISAMIDE DERIVATIVES, THEIR APPLICATION, THE PHARMACEUTICAL COMPOSITION ON THEIR BASIS, METHODS FOR THEIR PRODUCTION | 2013 |
|
RU2665688C2 |
THROMBIN INHIBITORS AND INTERMEDIATE COMPOUNDS FOR THEIR SYNTHESIS | 1995 |
|
RU2172741C2 |
TETRAHYDROCARBAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITION BASED ON SAID DERIVATIVES | 2005 |
|
RU2430088C2 |
HYDROXYBENZAMIDE DERIVATIVES AND USE THEREOF AS Hsp90 INHIBITORS | 2006 |
|
RU2458919C2 |
Authors
Dates
2007-10-27—Published
2005-03-25—Filed