DERIVATIVES OF 5-PYRIDYL-1,3-AZOLE, METHOD FOR THEIR PREPARING, THEIR PRODRUG, PHARMACEUTICAL COMPOSITION, METHOD FOR ANTAGONISM OF ADENOSINE A3-RECEPTOR, METHOD FOR INHIBITION OF P38 MAP KINASE, METHOD FOR INHIBITION PRODUCING TNF-ALPHA AND METHOD FOR PROPHYLAXIS Russian patent published in 2004 - IPC

FIELD: organic chemistry, biochemistry, medicine.

SUBSTANCE: invention relates, in particular, to optionally N-oxidized compounds represented by the formula: wherein R¹ represents hydrogen atom, (C₁-C₆)-alkyl group, phenyl group optionally substituted with halogen atom, (C₁-C₆)-alkylthio-group or (C₁-C₆)-alkylsulfonyl, or amino-group optionally substituted with (i) (C₁-C₆)-alkyl group or (ii) acyl group -(C=O)-R⁵ wherein R⁵ represents (C₁-C₆)-alkyl group, phenyl or pyridyl; R² represents (C₆-C₁₄)-aryl group optionally substituted with halogen atom or (C₁-C₆)-alkoxy-group, or 5- or 6-membered aromatic heterocyclic group comprising one sulfur atom or one nitrogen atom; R³ represents phenyl group optionally substituted with one or two (C₁-C₆)-alkyl groups or (C₁-C₆)-alkoxy-group; X represents sulfur atom; Y represents oxygen (O), sulfur (S) atom or NR⁴ wherein R⁴ represents hydrogen atom or (C₁-C₆)-alkyl group; Z represents a bond, (C₁-C₆)-alkylene group optionally substituted with oxo-group or (C₁-C₆)-alkyl group. Compounds of the formula (I) or their salts elicit high inhibitory effect on p38 MAP kinase and inhibition in producing TNF-α and elicit antagonistic effect with respect to adenosine A₃-receptor also and therefore they can be useful as prophylactic or medicinal agents used in treatment of diseases mediated by function of adenosine A₃-receptor, cytokines or p38 MAP kinase.

EFFECT: valuable biological and medicinal properties of compounds.

38 cl, 8 tbl, 66 ex