COMPLEX COMPOUNDS CONTAINING RADIONUCLIDE Th, AS WELL AS BISPHOSPHONATE FRAGMENT, METHODS FOR THEIR PRODUCTION, AS WELL AS POTENTIAL USE AS ACTIVE SUBSTANCE IN COMPOSITION OF OSTEOTROPIC RADIOPHARMACEUTICAL DRUG Russian patent published in 2022 - IPC A61K51/04 A61K103/00 C07F5/00 A61P35/00 

FIELD: nuclear medicine.

SUBSTANCE: invention relates to nuclear medicine, namely to the development of a potential osteotropic therapeutic radiopharmaceutical drug, active substance of which is a complex compound of the structure Y: ²²⁷Th-Chel-Zoledron, where Zoledron is a fragment corresponding to the structure:

Chel is a fragment corresponding to bifunctional chelating agents: 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (-DOTA); 2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecane-1-yl)pentanedioic acid (-DOTAGA); 1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetraacetic acid (-TETA); 1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetrapropionic acid (-TETPA); 1,4,7,10,13,16-hexaazacycloctadecane-1,4,7,10,13,16-hexaacetic acid (-HEHA); 1,4,7,10,13-pentaazacyclopentadecane-1,4,7,10,13-pentacetic acid (-PEPA); diethylenetriamine pentacetic acid (-DTPA); trans-cyclohexyl-diethylenetriamine pentaacetic acid (-CHX-DTPA); S-2-(4-isothiocyanatobenzyl)-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (p-SCN-Bn-DOTA); [(R)-2-amino-3-(4-isothiocyanatophenyl)propyl]-diamine-pentacetic acid (p-SCN-Bn-DTPA); [(R)-2-amino-3-(4-isothiocyanatophenyl)propyl]-trans-(S,S)-cyclohexane-1,2-diamine-pentacetic acid (p-SCN-Bn-CHX-A-DTPA); S-2-(4-isothiocyanatobenzyl)-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetamide (p-SCN-Bn-TCMC); S-2-(4-isothiocyanatobenzyl)-1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetraacetic acid (p-SCN-Bn-TETA); S-2-(4-isothiocyanatobenzyl)-1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetrapropionic acid (p-SCN-Bn-TETPA); S-2-(4-isothiocyanatobenzyl)-1,4,7,10,13,16-hexaazacycloctadecane-1,4,7,10,13,16-hexacetic acid (p-SCN-Bn-HEHA); S-2-(4-isothiocyanatobenzyl)-1,4,7,10,13-pentaazacyclopentadecane-1,4,7,10,13-pentacetic acid (p-SCN-Bn-PEPA), and in which radionuclide ²²⁷Th is part of the compound Y due to the formation of stable coordination bonds with the Chel fragment.

EFFECT: proposed complex compound of the structure Y as part of a potential osteotropic radiopharmaceutical drug, in addition to its therapeutic properties, such as reducing bone resorption due to the bisphosphonate fragment, and cytotoxic effect due to the formation of α-particles in the immediate vicinity of the pathological focus due to α-decay of radionuclide ²²⁷Th, is a potential in vivo generator of radionuclide ²²³Ra.

7 cl, 5 tbl