(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 Russian patent published in 2006 - IPC C07C233/51 C07C233/17 C07C233/11 C07C235/34 C07D213/75 C07D239/26 A61K31/165 A61K31/44 A61K31/505 

Abstract RU 2273630 C2

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, α-hydroxyisopropyl, (R,S)-α-hydroxybenzyl and its individual R-isomers, (R,S)-(α-methylbenzyl) and its individual R-isomer and (R,S)-α-hydroxy-α-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

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Authors

Allegretti Marchello

Bertini Rikkardo

Bitstsarri Chintsija

Sabbatini Vil'Ma

Kazelli Dzhanfranko

Chesta Marija Kandida

Gandol'Fi Karmelo

Kolotta Franchesko

Dates

2006-04-10Published

2001-02-06Filed