BORON-CONTAINING COMPOUND Russian patent published in 2020 - IPC C07F5/05 C07H23/00 A61K31/69 A61K41/00 A61P35/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a novel boron-containing compound, specifically to a compound corresponding to following formula 1, or a pharmaceutically acceptable salt thereof, selected from an alkali metal salt, ammonium salts, tetraalkylammonium salts (NR⁴⁺) or tetraphenylphosphonium salts:

[Formula 1]

In formula 1: black circle denotes atom B, white circle denotes BH; -R¹ denotes -(CH₂)-n-X¹-R³ (n denotes integer from 0 to 6; X¹ denotes O-CO, or absent; R³ denotes C₆-C₂₀ alkyl, hydroxy C₆-C₂₀ alkyl, amino C₆-C₂₀ alkyl, azido C₆-C₂₀ alkyl, hydroxycarbonyl C₆-C₂₀ alkyl, substituted, where the substitutes are nitro, hydroxyl, B(OH)₂, or unsubstituted phenoxy C₆-C₂₀ alkyl, substituted, wherein the substituent is dioxyfenylxanten, phenylthiourea or unsubstituted C₆-C₂₀ alkyl or unsubstituted benzyl group) or a group having a repeating sequence -(CH₂)₂-O- 3 times or more and 10 times or less and having a methyl group or an ethyl group on the end from the oxygen atom side; -R² denotes -(CH₂)m-X²-R⁴ (m denotes integer from 0 to 8; X 2 denotes O, NH, NHCO or absent; R⁴ denotes a tumor-recognizing portion selected from a group consisting of an amino acid, amino acid amide, 5-aminolevulinic acid, kojic acid, hydroquinone, resveratrol, ligand TSPO (translocating protein) of DPA type (acetyl amide of dimethyl pyrazolopyrimidine), caffeic acid or its salts, monosaccharides, and nucleic acids or their salts). Also disclosed are methods of producing boron-containing compounds and a pharmaceutical composition.

EFFECT: disclosed boron-containing compound can be used for treating a malignant tumor using a boron neutron capture technique (BNCT).

13 cl, 7 tbl, 4 ex, 3 dwg