SUBSTITUTED 1,2-DIHYDRO[2,7]NAPHTHIRIDINES, PHARMACEUTICAL COMPOSITION, METHOD FOR ITS PREPARING AND APPLYING Russian patent published in 2004 - IPC

FIELD: organic chemistry, chemical technology, pharmacy.

SUBSTANCE: invention relates to new highly effective ligands (agonists, antagonists, modulating agents and so on) on nicotinic receptors, i. e. to new substituted 1,2-dihydro[2,7]naphthiridines of the general formula (1)

,

as separate stereoisomers, their racemic or additive mixtures, or their pharmaceutically acceptable salts, N-oxides or hydrates wherein R¹ and R² represent independently of one another hydrogen atom, inert substitute, optionally substituted (C₁-C₅)-alkyl; or R¹ and R² represent in common polymethylene chain comprising 2-5 optionally substituted methylene groups; R³ and R⁴ represent independently of one another hydrogen atom, inert substitute, optionally substituted (C₁-C₅)-alkyl, optionally substituted (C₁-C₆)-alkyloxycarbonyl group, optionally substituted carbamoyl group; R⁵ at carbon atoms of pyridine ring represents: hydrogen atom, inert substitute, optionally substituted (C₁-C₅)-alkyl, optionally substituted amino-group, optionally substituted hydroxyl group, optionally substituted (C₁-C₆)-alkyloxycarbonyl group, optionally substituted carbamoyl group; or R⁵ if it at nitrogen atom of pyridine ring then it forms pyridinium salt with pharmaceutically acceptable anion and represents: inert substitute. Also, invention relates to pharmaceutical composition as tablet, capsule or injection solution, method for its preparing and applying.

EFFECT: improved preparing and applying method, valuable pharmacological properties of compounds.

14 cl, 1 sch, 1 tbl, 10 ex