| titleOfInvention |
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 |
| abstract |
FIELD: organic chemistry, biochemistry, medicine. n SUBSTANCE: invention relates, in particular, to optionally N-oxidized compounds represented by the formula: wherein R 1 represents hydrogen atom, (C 1 -C 6 )-alkyl group, phenyl group optionally substituted with halogen atom, (C 1 -C 6 )-alkylthio-group or (C 1 -C 6 )-alkylsulfonyl, or amino-group optionally substituted with (i) (C 1 -C 6 )-alkyl group or (ii) acyl group -(C=O)-R 5 wherein R 5 represents (C 1 -C 6 )-alkyl group, phenyl or pyridyl; R 2 represents (C 6 -C 14 )-aryl group optionally substituted with halogen atom or (C 1 -C 6 )-alkoxy-group, or 5- or 6-membered aromatic heterocyclic group comprising one sulfur atom or one nitrogen atom; R 3 represents phenyl group optionally substituted with one or two (C 1 -C 6 )-alkyl groups or (C 1 -C 6 )-alkoxy-group; X represents sulfur atom; Y represents oxygen (O), sulfur (S) atom or NR 4 wherein R 4 represents hydrogen atom or (C 1 -C 6 )-alkyl group; Z represents a bond, (C 1 -C 6 )-alkylene group optionally substituted with oxo-group or (C 1 -C 6 )-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 A 3 -receptor also and therefore they can be useful as prophylactic or medicinal agents used in treatment of diseases mediated by function of adenosine A 3 -receptor, cytokines or p38 MAP kinase. n EFFECT: valuable biological and medicinal properties of compounds. n 38 cl, 8 tbl, 66 ex |