NEW PSA-BINDING AGENTS AND THEIR USE Russian patent published in 2022 - IPC A61K47/64 A61K51/04 A61K51/08 A61P35/00 C07K5/02 

FIELD: medicine.

SUBSTANCE: invention relates to a compound of the general formula (1a), or its pharmaceutically acceptable salts, or complexes marked with a radioactive mark, which have a capability of selective binding to membrane of a prostate-specific antigen (hereinafter – PSA), and which can be used as radio-pharmaceutical agents, imaging agents, as well as for the treatment of cancer. In the formula (1a), D is a chelating residue selected from a group including 1,4,7,10-tetraazacyclododecan-1,4,7,10-tetraacetic acid (hereinafter – DOTA), 2-(4,7-bis(carboxymethyl)-1,4,7-triazononan-1-yl)pentanedioic acid (hereinafter – NODAGA), 2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)pentanedioic acid (hereinafter – DOTAGA), or their derivatives, X, each independently, is selected from O, R¹ and R², each independently, is H, F, Cl, Br, I, or C₁-C₁₂ alkyl, Y is selected from a group including a direct bond or C₁-C₁₂ alkyl, R³, R⁴, and R⁵, each independently, is selected from -CO₂H, a spacer has the formula (3a), (3b), or (3c), where m is an integer 1 or 2, n is an integer selected from 1, 2, 3, 4, or 5, o is an integer selected from 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, a linker has the structural formula (6), where X, each independently, is O, Q is selected from C₅-C₁₄ cycloalkyl, W is selected from -(CH₂)_c-aryl, where c is an integer selected from 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, and a, b, each independently, is an integer selected from 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10. The invention also relates to the use of the specified compounds for the production of complexes marked with a radioactive mark, to complexes marked with a radioactive mark, pharmaceutical compositions, and kits containing these compounds, options of the use of the specified compounds, complexes, compositions, and kits, including for diagnostics, treatment and/or prevention of prostatic cancer, pancreatic cancer, kidney cancer, or bladder cancer, a method for in vitro determination of the presence of cells and/or tissues expressing PSA.

EFFECT: obtainment of PSA-binding compounds for the treatment of cancer.,

36 cl, 27 dwg, 15 tbl, 6 ex