NOVEL TUMOR ANTIGEN BINDING AGENTS AND USE THEREOF Russian patent published in 2024 - IPC C07D257/02 A61K51/04 A61P35/00 G01N33/60 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a compound of general formula (1a) relating to PSMA-targeting agents, where D denotes a chelating moiety selected from DOTA, HBED-CC, NOTA, NODAGA, DOTAGA, TRAP, NOPO, PCTA, DFO, DTPA, DO3AP, DO3AP^PrA, DO3AP^ABn or derivatives thereof, Tbm denotes a prostate-specific membrane antigen (PSMA)-binding residue of general formula (3), where X is O, Y is NH, Z is CH₂, R¹, R² and R³ are each independently selected from -CO₂H, and f denotes a number selected from 1, 2, 3, 4, or 5, linker denotes structural formula (4a), spacer denotes structural formula (2)(d)', where A denotes an amino acid residue or—[A]n is absent, and n denotes an integer selected from 0 or 1, where the amino acid residue is selected from aspartate, asparagine, diaminobutyric acid, and k denotes an integer selected from 1, 2, 3, 4, 5 or 6, and a denotes a number selected from 0, or a pharmaceutically acceptable salt thereof. Invention also relates to the use of a compound of formula (1a) for the preparation of a radioactively labeled complex; a radioactively labeled complex comprising a radionuclide and a compound of formula (1a); a pharmaceutical composition based on a compound of formula (1a) or a radioactively labeled complex; a kit comprising a compound of formula (1a), or a radioactively labeled complex, or a pharmaceutical composition; and a method for in vitro detection of the presence of cells and/or tissues expressing a prostate-specific membrane antigen (PSMA).

EFFECT: development of new PSMA-targeting agents carrying therapeutic or diagnostic fragments that bind to albumin.

39 cl, 24 dwg, 8 tbl, 12 ex