THIAZOLINO-2-PYRIDONES WITH CONDENSED RINGS IN COMBINATION WITH A DRUG AGAINST TUBERCULOSIS Russian patent published in 2023 - IPC A61K31/4365 A61K31/4545 A61K31/496 A61P31/06 

FIELD: pharmaceuticals.

SUBSTANCE: group of inventions includes a combination for the treatment and/or prevention of tuberculosis and its use for the preparation of a drug for the treatment and/or prevention of tuberculosis caused by Mycobacterium tuberculosis. This combination includes: (i) an antibiotic which is 6-chloro-2-ethyl-N-[(4-{4-[4-(trifluoromethoxy)phenyl]piperidin-1-yl}phenyl)methyl]imidazo[1, 2-a]pyridine-3-carboxamide or a pharmaceutically acceptable salt thereof, and (ii) compound II or a pharmaceutically acceptable salt thereof, wherein (i) and (ii) are present in a therapeutically effective amount. In formula II, R₁ is selected from: C(O)OH и C(O)NHSO₂R₇; R₂ is selected from: H, Cl, F, Br, I and CH₂OH; R₃ is selected from the group consisting of: a) 1-naphthyl, 2-naphthyl or 1-naphthyloxy each independently substituted with 0, 1, 2 or 3 substituents selected from the group consisting of methyl, fluorine, chlorine, bromine, cyano and methoxy, b) phenyl substituted with 0, 1, 2 or 3 substituents independently selected from the group consisting of methyl, fluorine, chlorine, cyano and trifluoromethyl, c) 2-(3-methyl)phenylmethylene, d) benzothiophen-2-yl, e) isoxazol-5-yl optionally substituted with methyl, 1-naphthyl, 2-naphthyl, 1-anthryl, m-trifluoromethylphenyl, 3,5-ditrifluoromethylphenyl, 3,4-methylenedioxyphenyl, thiophene or phenyl, f) isoxazole-3-yl substituted with m-trifluoromethylphenyl or 1-naphthyl, g) benzoxazol-2-yl and h) a group as defined in the claims; R₄ is selected from the group consisting of: C₁-C₄ alkyl substituted with 0, 1, 2, 3 or 4 fluorine atoms, C₃ cycloalkyl, C₁-C₄ alkoxy, C₃-C₆ cycloalkoxy, 5-membered heterocycle substituted with 0 or 1 substituent selected from the group consisting of phenyl and 1-naphthyl, N-methyl 3-indolyl; R₅ is selected from the group consisting of: H, phenyl substituted with 0, 1, 2 or 3 methyl groups, benzyl, thienyl, C₁-C ₄ alkoxy and a 5-membered heterocycle.

EFFECT: combination comprising 6-chloro-2-ethyl-N-[(4-{4-[4-(trifluoromethoxy)phenyl]piperidin-1-yl}phenyl)methyl]imidazo[1,2-a]pyridine -3-carboxamide and a compound of formula II, to increase the effectiveness of a drug against tuberculosis.

10 cl, 4 dwg, 2 tbl, 65 ex

Formula II