THIAZOLINE-2-PYRIDONES WITH CONDENSED RINGS, THEIR PRODUCTION METHODS, AND THEIR USE IN TREATMENT AND/OR PREVENTION OF TUBERCULOSIS Russian patent published in 2022 - IPC C07D513/04 A61K31/4365 A61K31/44 A61K31/4409 A61K31/444 A61K31/69 A61P31/06 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to the field of pharmaceutics, namely to a pharmaceutical composition for the treatment and/or prevention of tuberculosis, including (i) isonicotinylhydrazide or its pharmaceutically acceptable salt and (ii) a compound II or its pharmaceutically acceptable salt, where R₁ is selected from a group including a) C(O)OH, b) tetrazolyl, c) CH₂OH, d) C(O)NR_6aR_6b, e) C(O)NHSO₂R₇, f) C(O)OR₈, g) NH₂, h) H, R₂ is selected from a group including a) H, b) Br, and c) CH₂OH, R₃ is selected from a group including a) 1-naphthyl, 2-naphthyl, 1-naphthyloxy, 4-fluor-1-naphthyl, 4-brom-1-naphthyl, 4-methyl-1-naphthyl, 4-methoxy-1-naphthyl, or 2-methoxy-1-naphthyl, b) 2-fluor-5-methyl-phenyl, 2,3-xylyl, 2,3-dichlorophenyl, para-chlorophenyl, meta-(trifluoromethyl)phenyl, or meta-tolyl, c) 2,3-xylydino, d) 2-(3-methyl)phenylmethylene, e) benzothiophene-2-yl, f) hydrogen, R₄ is selected from a group including methyl, trifluoromethyl, isopropyl, cyclopropyl, ethoxy, isobutoxy, cyclopropylmethoxy, dimethylamino, 2-thienyl, and N-methyl-3-indolyl, R₅ is selected from a group including a) H, b) phenyl or meta-tolyl, c) benzyl, d) 3-thienyl, e) methoxy, and f) 1H-1,2,3-triazole-4-yl; and, in above-mentioned representations, R_6a is selected from a group including H, R_6b is selected from a group including H and isonicotinylamino; R₇ is methyl or phenyl, R₈ is 2-{2-[1-(hydroxymethyl)propylamino]ethylamino}butyl), and X is S, SO, or SO₂. The invention also relates to the use of a pharmaceutical composition for the production of a drug for the treatment and/or prevention of tuberculosis and a specific compound.

EFFECT: effective treatment and/or prevention of tuberculosis, provided by a pharmaceutical composition including isonicotinylhydrazide and a compound of the formula II.

Formula II

14 cl, 22 dwg, 2 tbl, 54 ex