MOLECULE OF GENERAL STRUCTURE OF Y-NIC-18F, METHODS OF PREPARATION, PRECURSORS FOR ITS PREPARATION, AS WELL AS USE AS ACTIVE SUBSTANCE IN COMPOSITION OF POTENTIAL RADIOPHARMACEUTICAL DRUG Russian patent published in 2024 - IPC C07D213/82 C07B59/00 A61K51/04 A61P35/00 

Abstract RU 2811181 C2

FIELD: nuclear medicine.

SUBSTANCE: invention relates to a molecule of the general structure Y-Nic-18F of the following formulas, which in its composition contains a diagnostic positron-emitting radionuclide 18F, a fragment Y containing a biologically active motif Glu-urea-Lys, and also Nic fragment — a fragment of nicotinic acid with a substituent of the first kind (Z) in the second (18F-PSMA-1007-2Z) or fourth (18F-PSMA-1007-4Z) position of the pyridine ring, covalently bound to the Y fragment and to radionuclide 18F and responsible for the inclusion of the radionuclide 18F in the composition of the Y-Nic-18F molecule. In the Y-Nic-18F molecule, the substituent of the first kind (Z) is selected from -OCH3, -CH3, -SСH3, -CH2CH3, -CH(CH3)2. The specified molecule Y-Nic-18F can find use as an active substance in the composition of a diagnostic radiopharmaceutical drug for visualizing the localization of PSMA-overexpressing tumor cells. The invention also relates to a precursor molecule of the general structure Y-Nic-(N+Me3)X, its use as a starting reagent for obtaining a molecule of the general structure Y-Nic-18F and the use of a molecule Y-Nic-18F as an active substances in a potential diagnostic radiopharmaceutical for visualizing the localization of PSMA-overexpressing prostate cancer cells.

EFFECT: obtaining a molecule of the general structure of Y-Nic-18F that can be used as an active substance in the composition of a potential radiopharmaceutical drug.

8 cl, 20 dwg, 13 ex

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RU 2 811 181 C2

Authors

Dorovatovskij Stanislav Anatolevich

Dates

2024-01-11Published

2021-12-24Filed