Synergistic bioactive compositions for enhancing cellular energy

Inventors

Dhamane, Dhiraj • Tongra, Rajendra Prasad

Assignees

Celagenex Research India Pvt Ltd

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Publication Number

US-11491175-B2

Patent

Publication Date

2022-11-08

Expiration Date


Abstract

The present invention relates to synergistic bioactive compositions for enhancing cellular energy in aerobic or anaerobic conditions. Particularly, the invention relates to a synergistic bioactive composition comprising specific combination of purine nucleoside and hydrophilic pyridinecarboxamide compound(s) which are present in the ratio of 1:0.1 to 1:1 along with pharmaceutically acceptable carriers/excipients, wherein ‘purine nucleoside’ is inosine adduct and the hydrophilic pyridinecarboxamide compound is selected from nicotinamide riboside or nicotinamide mononucleotide either alone or in combination thereof. Further, the present cellular energy enhancing bioactive compositions are useful for treating ATP deficiency conditions. Moreover, the composition is useful for treating hepatic dysfunctions.

Core Innovation

The invention relates to a synergistic bioactive composition for enhancing intracellular ATP levels. The composition uses an exogenous blend that combines inosine 5′ monophosphate disodium salt hydrate with hydrophilic pyridinecarboxamide NAD+ precursors comprising nicotinamide riboside chloride and/or β-nicotinamide mononucleotide, together with pharmaceutically acceptable excipients.

The disclosed concept links the combination to increased cellular energy by pairing an inosine/IMP component with NAD+ precursor components that affect intracellular NAD+ and NAD+/NADH balance. The disclosed mechanism is described as supporting ATP generation through purine salvage pathways associated with IMP and as driving mitochondrial ATP production and oxidative phosphorylation via increased NAD+ from the NAD+ precursors.

The patent content describes the formulation as a synergistic energy/ATP-enhancing composition and recites weight-ratio ranges between IMP and NR and/or NMN. The disclosed non-limiting data include in vitro HepG2 results showing increased cellular ATP levels from the combination, including comparison where the combination produces greater ATP enhancement than IMP or NMN alone, including under hydrogen peroxide-induced stress, while also reporting non-cytotoxic concentrations via an MTT assay.

Claims Coverage

The provided independent claims cover a synergistic bioactive composition with three variants: IMP combined with nicotinamide riboside chloride, IMP combined with β-nicotinamide mononucleotide, and IMP combined with NR and/or β-NMN chloride, each formulated with pharmaceutically acceptable excipients. Across the independent claims, the key inventive content is the specified exogenous combination and the weight ratio range between IMP and the NAD+ precursor.

Exogenous IMP and NR blend for intracellular ATP enhancement

A synergistic bioactive composition for enhancing intracellular ATP levels in a subject suffering from liver diseases, comprising an exogenous blend of inosine 5′ monophosphate disodium salt hydrate and nicotinamide riboside chloride along with pharmaceutically acceptable excipients, wherein the inosine 5′ monophosphate disodium salt hydrate and the nicotinamide riboside chloride are present in a weight ratio of 1:0.2 to 1:0.5.

Exogenous IMP and β-NMN blend for intracellular ATP enhancement

A synergistic bioactive composition for enhancing intracellular ATP levels in a subject suffering from liver diseases, comprising an exogenous blend of inosine 5′-monophosphate disodium salt hydrate and β-nicotinamide mononucleotide in a ratio of 1:0.25 to 1:0.5 along with pharmaceutically acceptable excipients.

Exogenous IMP and NR or β-NMN blend with specified weight ratio range

A synergistic bioactive composition for enhancing intracellular ATP levels in a subject suffering from liver diseases, comprising an exogenous blend of inosine 5′ monophosphate disodium salt hydrate and nicotinamide riboside chloride or β-nicotinamide mononucleotide along with pharmaceutically acceptable excipients, wherein the inosine 5′ monophosphate disodium salt hydrate and the nicotinamide riboside chloride or the β-nicotinamide mononucleotide are present in a weight ratio of 1:0.2 to 1:0.5.

Collectively, the independent claims require a synergistic bioactive composition for liver-disease subjects that enhances intracellular ATP levels using an exogenous blend of IMP with a NAD+ precursor plus pharmaceutically acceptable excipients, with the inventive scope defined by specified weight-ratio ranges between the IMP component and the NR/NMN component.

Stated Advantages

Enhances intracellular ATP levels in a subject suffering from liver diseases.

Documented Applications

For a subject suffering from liver diseases, including liver diseases or liver dysfunctions as described by dependent claim context, to increase intracellular ATP levels.

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