(R)-2-ARYLPROPIONIC ACID OMEGA-AMINOALKYLAMIDES AS INHIBITORS OF POLYMORPHONUCLEAR AND MONONUCLEAR CELL HEMOTAXIS, METHOD FOR THEIR PREPARING AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2006 - IPC C07C233/40 C07C233/51 C07C235/54 C07C279/12 C07C231/02 C07D211/06 C07D233/48 C07D239/14 C07D295/13 A61K31/165 A61K31/4164 A61K31/4409 A61K31/506 A61K31/5375 A61K31/54 

Abstract RU 2272024 C2

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to compounds of the formula (I): wherein Ar represents phenyl substituted with a group taken among isobutyl, benzoyl, isopropyl, styryl, pentyl, (2,6-dichlorophenyl)-amino-group, α-hydroxyethyl, α-hydroxybenzyl, α-methylbenzyl and α-hydroxy-α-methylbenzyl; R represents hydrogen atom; X means linear (C1-C6)-alkylene, (C4-C6)-alkenylene, (C4-C6)-alkynylene optionally substituted with group -CO2R3 wherein R3 means hydrogen atom, group (CH2)m-B-(CH2)n wherein B means oxygen atom; m = 0; n means a whole number 2; or B means group -CONH; m means a whole number 1; n means a whole number 2 and so on; R1 and R2 are taken independently among group comprising hydrogen atom, linear (C1-C4)-alkyl, hydroxy-(C2-C3)-alkyl and so on. Invention proposes a method for preparing compounds of the formula (I). Invention proposes inhibitors of C5-induced hemotaxis of polymorphonuclear leukocytes and monocytes representing (R)-2-arylpropionic acid omega-aminoalkylamides of the formula (I). Also, invention relates to a pharmaceutical composition possessing inhibitory activity with respect to hemotaxis of polymorphonuclear leukocytes and monocytes and comprising compounds of the formula (I) in mixture with suitable carrier. Proposes (R)-2-arylpropionic acid omega-alkylamides are useful for inhibition of hemotaxic activation induced C5a and other hemotaxic proteins.

EFFECT: improved preparing method, valuable medicinal properties of compounds and composition.

18 cl, 3 tbl, 23 ex

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RU 2 272 024 C2

Authors

Allegretti Marchello

Bertini Rikkardo

Berdini Valerio

Bitstsarri Chintsija

Chesta Marija Kandida

Di Chochcho Vito

Kazelli Dzhanfranko

Kolotta Franchesko

Gandol'Fi Karmelo

Dates

2006-03-20Published

2002-02-25Filed