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
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...
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Zusammenfassung: | 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-alpha 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 |
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