Threonate compounds and methods of use thereof

Inventors

Liu, Guosong • Mao, Fei • Sun, Qifeng

Assignees

Neurocentria Inc

Abstract

Provided herein is a method of using threonate to alter cellular physiology, such as neuronal physiology. A method of the present disclosure may include providing to a medium comprising a cell, a threonate-containing compound, or a precursor thereof, to increase the concentration of threonate in the medium, where the increased concentration of threonate is sufficient to increase the concentration of magnesium in the cell. Also provided is a method that includes administering a threonate-containing compound, or a precursor thereof, to an individual, to increase synaptic density in the brain and/or to treat a neurological disorder, e.g., cognitive impairment. The threonate-containing compound of the present disclosure does not include magnesium threonate.

Core Innovation

The patent discloses threonate-containing compounds that are not magnesium salts, including threonate precursors, and describes their use to alter cellular and neuronal physiology. The disclosed approach increases extracellular threonate and thereby elevates intracellular Mg2+. The change in intracellular Mg2+ is linked to neuronal and synaptic effects in one or more regions of the brain.

The invention addresses using threonate to promote magnesium- and synaptic-related outcomes without administering magnesium threonate and without co-administering a magnesium-containing compound with the threonate-containing dosage form. The patent describes dosage-form and compound selections in which the threonate-containing compound or precursor is a monovalent, divalent or trivalent cation salt, and the first dosage form is not co-administered with a second dosage form comprising a magnesium-containing compound.

The patent further provides a method framework for increasing intracellular magnesium concentration by providing cells with a threonate-containing compound or precursor to increase threonate concentration in the medium. The increase in threonate concentration is described as sufficient to increase intracellular magnesium concentration compared to the cell state before providing, while not providing magnesium-containing compounds. The document also describes experimental findings showing extracellular threonate elevation and downstream changes associated with synaptic density and neuronal markers, including evidence implicating GLUTs.

Claims Coverage

The partial content contains two independent claims. Each independent claim centers on threonate-containing compounds and precursors that are not magnesium salts, with explicit exclusion of magnesium-containing co-administration or magnesium-containing compounds.

Across the independent claims, the core inventive coverage is directed to threonate-containing compounds and precursors that are not magnesium salts, with explicit exclusion of magnesium-containing co-administration for brain synaptic density and explicit exclusion of magnesium-containing compounds for increasing intracellular magnesium.

Stated Advantages

Documented Applications