PYRIMIDINE DERIVATIVES Russian patent published in 2008 - IPC C07D413/14 C07D405/14 C07D407/14 C07D417/14 A61K31/506 A61K31/295 A61P29/00 

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to compound of the formula (I) possessing inhibitory effect on production of interleukin-12 (IL-12) wherein R₁ represents group of the formula , aryl or heteroaryl; each among R₂ and R₄ represents independently hydrogen atom, (C₁-C₆)-alkyl or (C₁-C₆)-alkoxy group; R₃ represents R^c, alkenyl, -OR^c, -OC(O)R^c, -SR^c, -NR^cCOR^d, -NR^cC(O)OR^d, -NR^cC(O)NR^cR^d, -NR^cSO₂R^d, -COR^c, -C(O)OR^c or -C(O)NR^cR^d; R₅ represents hydrogen atom (H); n = 0, 1, 2, 3, 4, 5 or 6; X represents oxygen atom (O) or -NR^c; Y represents a covalent bond. -CH₂, O or -NR^c; Z represents nitrogen atom (N); one of values U and V represents N and another represents -CR^c; W represents O, sulfur atom (S) or -S(O)₂ wherein each radical among R^a and R^b represents independently H, (C₁-C₆)-alkyl, aryl or heteroaryl; each radical among R^c and R^d represents independently H, (C₁-C₆)-alkyl, phenyl, heteroaryl, cyclyl, heterocyclyl or (C₁-C₆)-alkylcarbonyl wherein term "aryl" relates to hydrocarbon cyclic system (monocyclic or bicyclic) comprising at least one aromatic ring; term "heteroaryl" relates to hydrocarbon cyclic system (monocyclic or bicyclic) comprising at least one aromatic ring that comprises at least one heteroatom, such as O, N or S as a part of cyclic system and wherein other atoms mean carbon; term "cyclyl" and "heterocyclyl" relate to partially or completely saturated monocyclic or bicyclic system comprising from 4 to 14 carbons in rings wherein heterocyclic ring comprises one or some heteroatoms (for example, O, N or S) as part of cyclic system and wherein other atoms mean carbon, and under condition that when X represents -NH, Y represents a covalent bond, n = 0, and R₃ represents H or CH₃ then R₁ doesn't mean thiazolyl or pyrimidinyl. Also, invention relates to a pharmaceutical composition and a method for treatment of disorder associated with hyperproduction of interleukin-12.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

49 cl, 43 ex