NOVEL BETA-LACTAMASE INHIBITOR AND METHOD FOR PRODUCTION THEREOF Russian patent published in 2019 - IPC C07D471/08 C07D211/60 A61K31/439 A61K31/444 A61K31/4545 A61K31/5377 A61P31/04 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a heterocyclic compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is Ra(Rb)N- or RcO-; B is NH; C is SO₃M, where M is H or sodium; Ra and Rb, each independently of the other, are C_1-6 alkyl, formyl, benzoyl, phenylacetyl, C_1-6 alkylcarbonyl, heterocyclylcarbonyl (where heterocyclyl is selected from tetrahydropyran, piperidine, pyrrolidine, morpholine) or heteroarylcarbonyl (where heteroaryl is selected from furan, pyrrole and pyridine), or Ra and Rb can be closed by bonding to obtain 5–6-member heterocyclyl, having at least one nitrogen atom or nitrogen atom and an oxygen atom; A is optionally substituted with 1–2 substitutes Fn1, and Fn1, which modifies A, can be further modified with Fn1; Rc is C_1-6 alkyl or 4–6-member heterocyclyl containing one or two nitrogen atoms; Rc and B can be closed by bonding to obtain 1,2-oxazolidinyl or 1,2-oxazininyl; Fn1 is C_1-6 alkyl, O =, C_3-6 cycloalkyl or Rg- (CH₂)_0-3-; Rg is 4–6-membered heterocyclyl containing 1 to 2 heteroatoms selected from a nitrogen atom, 5-member heteroaryl containing 1 to 2 heteroatoms selected from a nitrogen atom, RdO₂S-, Re(Rf)N-, Re(Rf)NCO-, ReO- or tert-butoxycarbonyl; Rd is MO^-, where M is sodium; Re and Rf, each independently of one another, are H or C_1-6 alkyl, or Re and Rf can be closed by bonding to obtain 5–7-member heterocyclyl containing 2 heteroatoms selected from a nitrogen atom and / or an oxygen atom. Invention also relates to a heterocyclic compound of formula (II) and (III), values of radicals are given in the claim; to a pharmaceutical composition and an inhibitor of β-lactamase based on the compound of formula (I), a method of treating a bacterial infection, a method of producing a compound of formula (III) and intermediate compounds, to specific intermediate compounds.

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EFFECT: technical result is obtaining a novel heterocyclic compound effective in treating bacterial infections.

23 cl, 5 dwg, 9 tbl, 122 ex