CARBAMYLOXY-COMPOUNDS INHIBITING VLA-4-MEDIATED ADHESION OF LEUKOCYTES Russian patent published in 2004 - IPC

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to carbamyloxy-compounds of the formula (I): wherein R¹ is taken among group including alkyl, substituted alkyl, aryl, substituted aryl, heterocyclyl, substituted heterocyclyl, heteroaryl and substituted heteroaryl; R² represents alkyl; R¹ and R² in common with nitrogen atom bound with R². and SO₂-- -group bound with R¹ can form heterocyclic or substituted heterocyclic group; R³ represents hydrogen atom being when R² doesn't form heterocyclic group with R¹ then R² and R³ in common with nitrogen atom bound with R² and carbon atom bound with R³ can form heterocyclic or substituted heterocyclic group; R⁵ represents wherein is taken among group including O-Z- and O-Z-R¹² wherein R⁸ and are taken independently among group including hydrogen atom, alkyl, substituted alkyl, heterocyclic and wherein R⁸ and are combined to form heterocycle or substituted heterocycle; R¹² is taken among group including heterocycle and substituted heterocycle and Z represents C(O)-; Ar represents aryl, heteroaryl, substituted aryl or substituted heteroaryl; x is a whole number from 1 to 4; Q represents -C(X)NR⁷- wherein R⁷ represents hydrogen atom; X represents oxygen atom; and to its pharmaceutically acceptable salts; to compounds of the formula IA wherein radical R⁶, representing alkoxy-group, substituted alkoxy-group, cycloalkoxy-group or NH-adamantyl are taken instead hydroxyl group by C-end. Invention relates also to two pharmaceutical compositions showing ability to block or inhibit cellular adhesion and comprising compound of the formula (I) or compound of the formula IA as an active component and to method for binding VLA-4 in biological sample and to method for treatment of inflammatory states in mammalian patient. EFFECT: valuable biological and medicinal properties of compounds. 30 cl, 3 tbl, 348 ex