LIGANDS, TROPIC TO PROSTATIC SPECIFIC MEMBRANE ANTIGEN AND USE THEREOF FOR OBTAINING DOUBLE CONJUGATES WITH THERAPEUTIC AGENTS BASED THEREON FOR COMBINED THERAPY OF PSMA EXPRESSING TUMOURS Russian patent published in 2025 - IPC A61K49/10 A61K51/00 A61K47/64 A61P35/00 

Abstract RU 2841078 C1

FIELD: chemistry; biotechnology.

SUBSTANCE: invention relates to the field of organic and medical chemistry, as well as molecular biology and concerns a new class of compounds, which are candidates for means of delivering diagnostic compounds (agents) for diagnostics, including radio diagnostics or fluorescent diagnostics, or therapy of oncological diseases, including chemotherapy or radiotherapy. Disclosed is a compound of general formula (I), which is intended for preparing a conjugate with a drug or diagnostic agent for diagnosing or treating diseases caused by cells expressing PSMA, for example, such as prostate cancer cells. Disclosed means of delivering diagnostic or therapeutic agents, which include a PSMA ligand with a linker, have high affinity and selectivity for cells expressing PSMA. This property makes it possible to use them for treating diseases associated with high expression of PSMA, with a lower dosage with selective action on cancer cells, without affecting healthy cells.

EFFECT: disclosed delivery devices enable to combine active substances of different nature and mechanism of their action or use, including these delivery devices enable to perform combined chemotherapy of tumours expressing a prostatic specific membrane antigen, due to creation of bimodal conjugates on their basis.

14 cl, 25 dwg, 9 tbl, 67 ex

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RU 2 841 078 C1

Authors

Machulkin Aleksej Eduardovich

Zyk Nikolaj Yurevich

Petrov Stanislav Aleksandrovich

Uspenskaya Anastasiya Alekseevna

Garanina Anastasiya Sergeevna

Skvortsov Dmitrij Aleksandrovich

Shafikov Radik Radikovich

Larenkov Anton Alekseevich

Beloglazkina Elena Kimovna

Mazhuga Aleksandr Georgievich

Dates

2025-06-02Published

2023-12-19Filed