(R)-2-ARYLPROPIONAMIDES USEFUL IN INHIBITION OF IL-8-INDUCED CHEMOTAXIS OF NEUTROPHILES, METHOD AND INTERMEDIATE COMPOUNDS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION INHIBITING INTERLEUKIN-8-INDUCED CHEMOTAXIS OF NEUTROPHILES

摘要

FIELD: organic chemistry, biochemistry, medicine, pharmacy.;SUBSTANCE: invention relates to (R)-enantiomers of 2-arylpropionamides of the formula (Ia): and their pharmaceutically acceptable salts wherein Aryl represents phenyl group substituted with a group chosen from isopropyl, acetyl, (2'',6''-dichlorophenyl)amino-group, -hydroxyisopropyl, (R,S)--hydroxybenzyl and its individual R-isomers, (R,S)-(-methylbenzyl) and its individual R-isomer and (R,S)--hydroxy--methylbenzyl and its individual R-isomer; R represents hydrogen atom (H) or (C₁-C₄)-alkyl; R' represents the following groups: -amino acid residue consisting of linear or branched (C₁-C₆)-alkyl substituted with carboxy-group -CO₂H; -residue of the formula: -CH₂-CH₂X-(CH₂-CH₂O)nR wherein R has abovementioned values; n means a whole number from 0 to 1 while X represents oxygen atom; -heteroaryl chosen from the group consisting of 2-pyrimidinyl or 4-pyrimidinyl. Also, invention proposes a pharmaceutical composition inhibiting of interleukin-8-induced chemotaxis of neutrophiles and comprising as an active components (R)-enantiomers of 2-arylpropionamides of the formula (I) and their pharmaceutically acceptable salts in mixture with a suitable carrier. Also, invention proposes a method for preparing compounds of the formula (Ia). Also, invention proposes (R)-enantiomers of 2-arylpropionic acids of the formula (Va) given in the invention description and their pharmaceutically acceptable salts. Proposed (R)-2-arylpropionamides are useful in prophylaxis and treatment of tissue damage caused by enhanced accumulation of polymorphonuclear neutrophiles in the inflammation sites.;EFFECT: improved preparing method, valuable medicinal properties of compounds and composition.;13 cl, 6 tbl, 24 ex