FUNCTIONAL PLG COPOLYMERS, THEIR NANOPARTICLES, THEIR PREPARATION AND APPLICATION FOR TARGETED DRUG DELIVERY AND IMAGE OBTAINING Russian patent published in 2017 - IPC C08G63/08 C08L67/04 C07D249/04 A61K47/34 A61K9/51 

FIELD: pharmacology.

SUBSTANCE: compound of formula (A)

is described, where: PLA is a polylactide residue of the formula:

where: (3) is the bond attachment to the PEG group; and m is the number of units and is from 1 to 500; PEG is a polyethylene glycol residue of the formula:

where: (4) is the bond attachment to -PLA; (5) is the bond attachment to the nitrogen atom

and n is the number of units and is from 1 to 300; PEG'linker is a polyethylene glycol residue of the formula:

where: n' is the number of units and is from 1 to 10, (1) is the bond attachment to -(CH₂)-triazole group; (2) is the bond attachment to a ligand; and Ligand is a functional ligand residue selected from ligands, membrane recognition, diagnostic/imaging agents. Also nanoparticles having an average diameter of 10 nm to 900 nm, containing one or more of the same or different above compounds of formula (A) are described. A method for preparation of the above compound of formula (A), comprising the combination of a compound of formula (I)

with a compound of the formula (XI)

where PLA, PEG, PEG' and Ligand are as defined above by the click-chemistry method. A method for preparation of the above-mentioned nanoparticles is also described. A drug for targeted drug delivery and imaging which comprises at least one of the above compound of formula (A), optionally in the form of nanoparticles, is described. A pharmaceutical composition for targeted drug delivery and imaging which contains the above compound of formula (A), optionally in the form of nanoparticles, as the active ingredient, and at least one pharmaceutically acceptable excipient is described.

EFFECT: improved compounds properties.

19 cl, 4 dwg, 12 tbl, 11 ex