	US 12,082,918 B2
	Preparation for magnetic resonance diagnostics for oncological diseases, comprising deuterated 2-amino-2-methylpropionic acid and/or 2-(N-methylamino)-2-methylpropionic acid, 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. 16/765,943
Filed by SOLVEX LIMITED LIABILITY COMPANY, Moscow (RU)
PCT Filed Nov. 21, 2017, PCT No. PCT/RU2017/000870 § 371(c)(1), (2) Date May 21, 2020, PCT Pub. No. WO2019/103636, PCT Pub. Date May 31, 2019.
Prior Publication US 2020/0352472 A1, Nov. 12, 2020
Int. Cl. A61B 5/055 (2006.01); A61K 49/10 (2006.01); C07C 229/08 (2006.01)

CPC A61B 5/055 (2013.01) [A61K 49/10 (2013.01); C07C 229/08 (2013.01)]

17 Claims

1. A diagnostic agent, comprising a deuterated derivative of 2-amino-2-methylpropionic acid and/or 2-(N-methylamino)-2-methylpropionic acid and/or its pharmaceutically acceptable salt, or a mixture of at least two different deuterated derivatives of 2-amino-2-methylpropionic acid and/or 2-(N-methylamino)-2-methylpropionic acid and/or its pharmaceutically acceptable salts, formulated for in vivo diagnosis of an oncological disease in a human subject by magnetic resonance imaging and/or magnetic resonance spectroscopy at a frequency of deuterium nuclei,

wherein the diagnostic agent is formulated to fail to accumulate to indicate the absence of cancer in the subject where the deuterated derivative of 2-amino-2-methylpropionic acid is 2-amino-2-(CD₃)-3,3,3-D₃-propionic acid or 2-amino -2-(CD₂H)-3,3,3-D₃-propionic acid or 2-amino-2-(CDH₂)-3,3,3-D₃-propionic acid or 2-amino -2-methyl-3,3,3-D₃- propionic acid or 2-amino-2-(CD₂H)-3,3-D₂-propionic acid or 2-amino-2-(CDH₂)-3,3-D₂-propionic acid or 2-amino-2-methyl-3,3-D₂-propionic acid or 2-amino-2-(CDH₂)-3-D-propionic acid or 2-amino-2-methyl-3-D-propionic acid and wherein the deuterated derivative of 2-(N-methylamino)-2-methylpropionic acid is a 2-methylamino-2-(CD₃)-3,3,3-D₃-propionic acid or 2-(N-(CD₃)amino)-2-methylpropionic acid or 2-(N-(CD₃)amino)-2-(CD₃)-3,3,3-D₃-propionic acid.