US 12,115,232 B2
Preparation for magnetic resonance diagnostics for oncological diseases, comprising deuterated 3-O-methylglucose, and diagnostic method using said preparation
Aleksei Valerievich Lesiv, Dolgoprudny (RU); Pavel Evgenievich Ivashkin, Moscow (RU); Mikhail Vladimirovich Gulyaev, Moscow (RU); Evgeniya Olegovna Dorofeeva, Moscow (RU); Aleksei Viktorovich Kosenkov, Moscow (RU); Mikhail Valentinovich Kiselevsky, Moscow (RU); and Vladimir Ivanovich Polshakov, Moscow (RU)
Assigned to SOLVEX LIMITED LIABILITY COMPANY, Moscow (RU)
Appl. No. 16/765,934
Filed by SOLVEX LIMITED LIABILITY COMPANY, Moscow (RU)
PCT Filed Nov. 21, 2017, PCT No. PCT/RU2017/000869
§ 371(c)(1), (2) Date May 21, 2020,
PCT Pub. No. WO2019/103635, PCT Pub. Date May 31, 2019.
Prior Publication US 2020/0330618 A1, Oct. 22, 2020
Int. Cl. A61K 49/10 (2006.01); A61K 9/00 (2006.01); C07H 3/02 (2006.01)
CPC A61K 49/10 (2013.01) [C07H 3/02 (2013.01); A61K 9/0053 (2013.01)] 15 Claims
 
1. A method for diagnosing an oncological disease in a subject, the method comprising:
a) administering to the subject a diagnostic agent comprising:
a deuterated derivative of 3-O-methylglucose or a mixture of at least two different deuterated derivatives of 3-O-methylglucose,
wherein the deuterated derivative of 3-O-methylglucose or the mixture of the at least two different deuterated derivatives of 3-O-methylglucose is formulated to accumulate in tumor cells in a concentration detectable in vivo by 2H magnetic resonance imaging, and/or magnetic resonance spectroscopy at a frequency of deuterium nuclei, in the diagnosis of the oncological disease, and
wherein “deuterated” and “deuterated derivative” refer to a compound containing deuterium associated with carbon in excess of its natural content, at least in one position, and wherein “mixture of at least two different deuterated derivatives” refers to a mixture of compounds containing deuterium in different positions of the molecule, or containing different amounts of deuterium in the same position wherein the deuterated derivative of 3-O-methylglucose is a 3-O-CD3-glucose, 3-O-CD2H-glucose, 3-O-CDH2-glucose, 6,6-dideuterio-3-O-CD3-glucose, 6,6-dideuterio-3-O-CD2H-glucose, 6,6-dideuterio-3-O-CDH2-glucose or 6,6-dideuterio-3-O—CH3-glucose or at least two different deuterated derivatives of 3-O-methylglucose, selected from 3-O-CD3-glucose and/or 3-O-CD2H-glucose and/or 3-O-CDH2-glucose and/or 6,6-dideuterio-3-O-CD3-glucose and/or 6,6-dideuterio-3-O-CD2H-glucose and/or 6,6-dideuterio-3-O-CDH2-glucose and/or 6,6-dideuterio-3-O—CH3-glucose and/or any other deuterated derivatives of 3-O-methyl glucose;
b) conducting magnetic resonance imaging and/or magnetic resonance spectroscopy at the frequency of deuterium nuclei after administration of the diagnostic agent after a period of time sufficient for accumulation of said diagnostic agent in a tumor, for obtaining, respectively, a MR image and/or NMR spectrum; and
c) diagnosing presence or absence of the oncological disease based on an observed signal intensity of deuterium nuclei, reflecting a level of accumulation of the diagnostic agent.