COMPOUNDS FOR TARGETED DRUG DELIVERY AND ENHANCING siRNA ACTIVITY Russian patent published in 2022 - IPC C07C237/08 C07C237/22 C07C323/60 C07C333/04 A61K9/127 A61K31/16 A61P1/16 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a compound consisting of the structure (retinoid)_m-linker-(retinoid)_n, which can be used to deliver therapeutic agents. In the structure (retinoid)_m-linker-(retinoid)_n m and n are independently 1, 2 or 3, the retinoid is selected from the group, consisting of vitamin A, retinoic acid, tretinoin, adapalene, 4-hydroxy(phenyl)retinamide (4-HPR), retinyl palmitate, retinal, saturated retinoic acid and saturated demethylated retinoic acid, and the linker is selected from the group consisting of polyethylene glycol (PEG), bis-amido-PEG, tris-amido-PEG, tetra-amido-PEG, Lys-bis-amido-PEG-Lys, Lys-tris-amido-PEG-Lys , Lys-tetra-amido-PEG-Lys, Lys-PEG-Lys, PEG2000, PEG1250, PEG1000, PEG750, PEG550 and PEG-Glu. Invention also relates to specific compounds and a carrier for a drug for treating fibrous disease or cancer, comprising a retinoid molecule, consisting of a structure (retinoid)_m-linker-(retinoid)_n, and a liposomal composition containing a compound of formula I. In formula I R₁ and R₂ are independently selected from a group, consisting of C₁₂-C₁₈ alkyl, C₁₂-C₁₈ alkenyl and oleyl groups; R₃ and R₄ are independently selected from the group consisting of C₁-C₆ alkyl and C₂-C₆ alkanol; X is selected from the group consisting of -CH₂- and -S-, or is absent; Y is selected from -(CH₂)_n and -S (CH₂)_n, n=1–4; a=1–4; b=1–4; c=1–4; Z is a counterion.

EFFECT: disclosed are compounds for targeted drug delivery and enhancing siRNA activity.

15 cl, 16 dwg, 14 tbl, 43 ex