FIELD: organic chemistry. SUBSTANCE: invention describes derivatives of pyridine of the formula (I) where X is (C2-C4)-alkynylene group linked by adjacent unsaturated carbon atoms; R1 is (C1-C4)-alkyl, (C1-C4)-alkoxyethynyl, (C1-C4)-alkoxycarbonyl, di-(C1-C4)-alkylamino-group; R2 means hydrogen atom, (C1-C4)-alkyl, hydroxy-(C1-C4)-alkyl, di- (C1-C4)-alkylaminomethyl-group, 4-(4-fluorobenzoyl)piperidin-1-ylcarbonyl, 1-tert. -butyloxycarbonylpiperazin- 1-ylcarbonyl, 4-(4-azido-2-hydroxybenzoyl)-piperazin-1-ylcarbonyl; R3 means hydrogen atom, (C1-C4)-alkyl, carboxy-group, (C1-C4)-alkoxycarbonyl, hydroxy-(C1-C4)-alkyl, di-(C1-C4)-alkylaminomethyl-group, morpholinocarbonyl-group, 4-(4-fluorobenzoyl)-piperidin-1-ylcarbonyl; R4 means hydrogen atom, (C1-C4)- alkoxy-group, carboxy-group, (C2-C5)-alkanoyloxy-group, (C1-C4)-alkoxycarbonyl, amino-(C1-C4)-alkoxy-group, di- (C1-C4)-alkylamino-group-(C1-C4)-alkoxy-group, di-(C1-C4)-alkylamino-(C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl-(C1-C4)-alkoxy- group, di-(C1-C4)-alkylamino-(C1-C4)-alkoxy-group, m-hydroxy-p-azidophenylcarbonylamino-(C1-C4)-alkoxy-group; R5 means substituted phenyl or pyridyl as free form or pharmaceutically acceptable salt. Invention describes also pharmaceutical composition based on indicated compounds. Compounds can be used for treatment of patients with disorders that are completely or partially mediated by mGluR5. EFFECT: valuable medicinal properties of compounds. 6 cl, 1 tbl, 8 ex
Authors
Dates
2003-05-10—Published
1998-07-09—Filed