FURO- AND THIENO[2,3-b]-QUINOLINE-2-CARBOXAMIDES, METHOD OF PRODUCTION AND ANTITUBERCULOUS ACTIVITY Russian patent published in 2009 - IPC C07D495/04 C07D491/48 A61K31/4355 A61K31/46 A61K31/4523 A61K31/501 A61K31/4725 A61K31/438 A61P31/06 

FIELD: chemistry.

SUBSTANCE: in formula compounds, each of R¹, R², R³, R⁴ is a substitute for a cyclic system, chosen from hydrogen, halogen, C₁-C₆-alkyl; C₁-C₆-alkoxy group; X is a heteroatom, chosen from oxygen or sulphur; R⁵ and R⁶ independently represent amino group substitutes, chosen from hydrogen, possibly substituted C₁-C₆-alkyl; possibly substituted C₃-C₆-cycloalkyl, which can be annealed with a benzene ring; possibly substituted phenyl, which can be annealed with dioxole, dioxine, -(CH₂)_n group, where n=4 to 6, or with a 5 or 6-member possibly substituted and possibly condensed azaheterocyclyl; possibly substituted saturated or unsaturated 5-6-member heterocyclyl, containing 1-2 heteroatoms, chosen form nitrogen, oxygen, sulphur and possibly condensed with a benzene ring, or R⁵ and R⁶ together with the nitrogen atom to which they are bonded, form an optionally substituted 5 or 6-member azahetero ring, possibly containing an additional heteroatom, chosen from nitrogen, and possibly annealed with a benzene ring or spiro-condensed with dioxole, where substitutes in the said alkyl, cycloalkyl, phenyl and heterocyclyl are chosen from halogen atoms, possibly substituted C₁-C₆-alkyl, CF₃, possibly substituted C₃-C₆-cycloalkyl, possibly substituted phenyl, 5 or 6-member heterocyclyl, nitro group, substituted amino group, alkyloxycarbonyl, substituted carbonyl, aminocarbonyl, alkylsulphanyl.

EFFECT: design of an efficient method of producing new substituted furo[2,3-b]quinoline-2-carboxamides and substituted thieno[2,3-b]quinoline-2-carboxamides or their racemates, or their optical isomers, as well as their pharmaceutically acceptable salts and/or hydrates of general formula (I), which have antituberculous activity.

9 cl, 1 dwg, 7 tbl, 5 ex