PEPTIDE AGENT COMPRISING A PSMA-BINDING LIGAND BASED ON A UREA DERIVATIVE, A METHOD FOR PRODUCTION THEREOF AND USE THEREOF FOR PREPARING A CONJUGATE WITH A DRUG AND DIAGNOSTIC AGENT Russian patent published in 2019 - IPC C07C275/16 C07C275/24 C07B41/06 C07B41/12 C07B43/06 A61P35/00 

Abstract RU 2697519 C1

FIELD: chemistry.

SUBSTANCE: present invention relates to a substance of general formula

(I),

where n = 3-5; X, Y, Z independently represent F, Cl, Br, H; R = OH, H; R1 = H, Br. Invention also relates to a method of producing such a substance, to use thereof for producing a conjugate with a drug or diagnostic agent for diagnosing or treating diseases caused by cells expressing a prostatic specific membrane antigen (PSMA), as well as to the conjugate itself.

EFFECT: obtaining novel means of delivering diagnostic or therapeutic agents, including PSMA-ligand with a linker, having low toxicity, high affinity and selectivity of action on cells expressing PSMA, which enables to use them for treating diseases associated with high expression PSMA, with a lower dosage with selective action on cancer cells, without affecting healthy cells.

12 cl, 20 dwg, 1 tbl, 1 ex

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RU 2 697 519 C1

Authors

Machulkin Aleksej Eduardovich

Uspenskaya Anastasiya Alekseevna

Ber Anton Petrovich

Petrov Stanislav Aleksandrovich

Saltykova Irina Vladimirovna

Ivanenkov Yan Andreevich

Skvortsov Dmitrij Aleksandrovich

Erofeev Aleksandr Sergeevich

Gorelkin Petr Vladimirovich

Beloglazkina Elena Kimovna

Belov Evgenij Yurevich

Khazanova Elena Sergeevna

Mazhuga Aleksandr Georgievich

Dates

2019-08-15Published

2018-10-15Filed