PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITION ELICITING ANTAGONISTIC EFFECT TO HUMAN mGluR Russian patent published in 2003 - IPC

Abstract RU 2203889 C2

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

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RU 2 203 889 C2

Authors

Allgajer Khans

Oberson Iv

B'Olaz Mishel'

Kosford Nikolas Dejvid

Gasparini Fabritsio

Khekkendorn Roland

Dzhonson Ehduin Karl

Kun Rajner

Varni Mark Ehndrju

Veliselebi Gehnjul

Dates

2003-05-10Published

1998-07-09Filed