BORONIC ACID DERIVATIVES Russian patent published in 2020 - IPC C07F5/02 A61K31/69 A61P37/00 

FIELD: chemistry; pharmaceutics.

SUBSTANCE: invention relates to a compound of formula (I) or stereoisomers thereof, which inhibit immunoproteasome activity (LMP7) and can be used to prevent and/or treat medical conditions caused by inhibiting LMP7. In formula (I) LX is (CH_2)n; LY is (CH_2)m; X denotes an α, β-unsaturated amide or sulphonamide group of formula xa), xb) or xd); Q is C=O or SO₂; Y stands for Sus; R¹, R² mean, independently from each other, H or R¹ and R² together form residue in accordance with formula (CE); R^3a denotes a linear or branched C1-C6-alkyl, where 1–5 of the H atoms can be replaced by Hal; R^4a, R^4b mean, independently from each other, R^3a; R^5a, R^5b mean, independently from each other, H or A1; R⁶ denotes H, Ar1 or A1; R⁷, R⁸, R⁹, R¹⁰ mean, independently from each other, H, Hal, (CH₂)_p-A1, (CH₂)_p-NR^4aR^4b, (CH₂)_p-COOR^4a or (CH₂)_p-CONR^4aR^4b; A1 is a linear or branched C1-C6-alkyl or C3-C6-cycloalkyl, each independently unsubstituted or mono-, di- or trisubstituted by Hal or CN; Ar1 denotes phenyl which is unsubstituted, mono-, di- or trisubstituted by Hal, R^3a, OR^4a and/or CONR^4aR^4b; Sus means mono- or bicyclic 4-, 5-, 6-, 7-, 8-, 9- or 10-member hydrocarbon or heterocycle, where monocyclic hydrocarbon system is aromatic and at least one ring of bicyclic hydrocarbon or heterocycle is aromatic and where the heterocyclic system contains 1 O or S atom; n is 0; m is 1, 2, 3, or 4; p is 0, 1, or 2; Hal is F, Cl, Br, or I. Invention also relates to a method of producing said compounds, containing them pharmaceutical composition and medicinal agents.

EFFECT: boronic acid derivatives are disclosed.

25 cl, 1 tbl, 106 ex