SULFAMIDO- AND SULFAMIDO-CARBONYLPYRIDINE-2-CARBOXYLIC ACID AMIDES, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION Russian patent published in 1999 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to sulfamido- and sulfamido-carbonylpyridine- -2-carboxylic acid amides of the formula (I) where A is R³ and B is -X-NR⁶R⁷; or B is R³ and A is -X-NR⁶R⁷; X - a simple bond or -CO-; R¹,R²,R³ are similar or distinct and mean hydrogen atom, unsubstituted C₁-C₄-alkyl, (C₁-C₆)-alkoxy-group, fluorine, bromine atoms; R⁴,R⁵ - H independently each of other, C₁-C₈-alkyl, C₆-C₁₀-aryl, C₇-C₁₁-ar-C₁-C₆-alkyl, C₁-C₈-alkyloxy-group possibly once substituted with hydroxy-, carboxy-, C₁-C₆-alkyloxycarbonyl, C₁-C₆-alkoxy-group; R⁶ - H, C₁-C₆-alkyl, monovalent physiologically acceptable cation - Na⁺,K⁺; R⁷ - residue of the formula (II) (for exception SO₂H), Y-[C-V]_r-D-W where Y is SO₂; C - a bond, C₁-C₈-aliphatic alkanediyl; V - bond, -O-; D - bond; W is H, thienyl, C₆-C₁₀-aryl being V means -O- if C does not mean a bond and W is substituted preferably with, for example, a group -O-(CH₂)_xC_fH_(2f+1-q)F_q; f = 1-8; q = 0.1-(2f + 1); z = 1, 2; X = 0-8. Synthesized compounds are used in a pharmaceutical composition showing an antifibrous activity. Compound where X - a simple bond is synthesized from aminopyridine-2-carboxylate and derivative of sulfonic acid followed by interaction of obtained compound with amine. Compound (I) where X means -CO- is synthesized from pyridine-2-carboxylic acid carboxylate ester. EFFECT: improved method of synthesis, antifibrous activity of compounds synthesized. 7 cl, 1 tbl, 2 dwg