BORONIC ACID DERIVATIVES Russian patent published in 2023 - IPC C07F5/02 A61K31/69 A61K35/00 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to derivatives of α-aminoboronic acid, namely to the compound of formula (I) and its stereoisomers, including their mixtures in all ratios. In formula (I): LY means (CH₂)_m; X means a heterobicycle or heterotricycle of the formula (xa), (xb), (xc), (xd), (xe), (xf), (xg), (xh) or (xi), each, independently of each other friend, unsubstituted or mono-, di- or tri-substituted by R^5a; Y means P² or P³; P² means phenyl, unsubstituted or mono-, di-, tri-, tetra- or penta-substituted by R^3a; P³ means a bicyclic 8-, 9- or 10-membered heterocycle, unsubstituted or mono-, di-, tri-, tetra- or penta-substituted by Hal, R^3a, and where the heterocyclic system contains 1 atom of O; Cy¹, Cy², Cy³, Cy⁴ and Cy⁵ mean, each, independently of each other, Ar¹ or Het¹; R¹, R² mean H; R^3a means linear or branched C₁-C₆-alkyl; R^5a means H, R^3a-; T¹, T², T³, T⁴, T⁵, T⁶, T⁷, T⁸ and T⁹ mean O; Ar¹ is an aromatic 6-membered carbocycle, Het¹ is saturated, unsaturated or aromatic 5- or 6-membered heterocycle containing 1 atom of N; m means 1 or 2; Hal means F, Cl, Br or I. A method for obtaining the compound of formula (I), pharmaceutical composition and application of the compound of formula (I) are also proposed.

EFFECT: proposed compounds are useful for inhibiting the activity of the immunoproteasome (LMP7) and for the treatment and/or prevention of medical conditions caused by the activity of the immunoproteasome, such as inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases and malignant neoplasm.

19 cl, 3 tbl, 11 ex