# US 10,500,176 B2 · Method for enhancing energy production and metabolism in cells

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- Number: US 10,500,176 B2
- Document ID: US10500176B2
- Status: Granted
- Kind: B2
- Application number: 14/917,764
- Filed: 2014-09-12
- Published: 2016-07-28
- Granted: 2019-12-10
- Earliest claimed: 2013-09-13
- Assignees: Replicon Health Oy
- Applicants: Replicon Health Oy
- Inventors: Petteri Hirvonen; Peter Eriksson; Risto Kaksonen
- Web page: https://patentgrep.com/patent/US10500176B2

## CPC

- A61K 31/191: having two or more hydroxy groups, e.g. gluconic acid
- A23L 2/52: Adding ingredients (adding preservatives A23B70/10)
- A23L 33/10: using additives (addition of substantially indigestible substances A23L33/21)
- A61K 31/19: Carboxylic acids, e.g. valproic acid (salicylic acid A61K31/60)
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 21/06: Anabolic agents (androgens A61P5/26)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A23V 2002/00: Food compositions, function of food ingredients or processes for food or foodstuffs
- A23V 2200/316: having an effect on regeneration or building of ligaments or muscles
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A23V: INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION

## Abstract

The present invention relates to use of a composition comprising D-glyceric acid (DGA), DL-glyceric acid, L-glyceric acid, or hydroxypyruvatic acid and/or their salts or esters. Further, the invention relates to the use of said composition for enhancing direct and indirect mitochondrial metabolism, e.g. the ATP producing electron transport system (ETS), citric acid cycle or tricarboxylic acid cycle, (TCA), and beta oxidation, and also enhancing the shuttling of reducing equivalents from mitochondrial matrix into the cytosol and protein synthesis in the endoplasmic reticulum. Directly related to the above the use of DGA relates also to reducing the formation of reactive oxygen species (ROS). Alleviating, preventing and even healing effects towards extremely wide range of non-communicable diseases materializes.

## Claims

### Claim 1

A method of treating a non-communicable disease or disorder the method comprising administering a composition comprising one or more compounds selected from the group consisting of D-glyceric acid, DL-glyceric acid, L-glyceric acid, a salt of D-glyceric acid, a salt of DL-glyceric acid, an ester of D-glyceric acid, and an ester of DL-glyceric acid, as the only active substance or substances, to a subject in need thereof, wherein the composition enhances mitochondrial ATP production and simultaneously reduces excessive radical oxygen species formation from oxidative phosphorylation (OXPHOS), and wherein the non-communicable disease or disorder is selected from the group consisting of: a cardiovascular disease or disorder, mitochondrial DNA depletion, mitochondrial diseases, cerebrovascular accident, damage from acute head injury, acute or chronic renal failure, acute or chronic liver failure, splenomegaly, acute or chronic pancreatic failure, hemorrhagic shock, pre-eclampsia, thyroid disease, chronic fatigue, fibromyalgia, multi-organ dysfunction syndrome, epilepsy, bipolar disorder, psychiatric and mood disorders, obesity, high blood pressure, an age-related degeneration disease or disorder, rheumatoid arthritis, gout, and chronic obstructive pulmonary disease.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the composition regulates an inducible heme oxygenase pathway to enhance endogenous antioxidant and anti-inflammatory activity in the subject.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the composition increases endogenous pyruvate concentration to provide substrates for aerobic ATP production and anabolic reactions, and enhances endogenous antioxidant and anti-inflammatory activity in the subject.

### Claim 4 (depends on 1)

The method according to claim 1, wherein the cardiovascular disease or disorder is selected from the group consisting of: atherosclerosis, myocardial infarction, cardiomyopathy or congestive heart failure, and vascular thrombosis and embolism, or wherein the age-related degeneration disease or disorder is selected from the group consisting of: age related hearing loss, age related macular degeneration, glaucoma, optic neuropathy, retinitis pigmentosa, sarcopenia, osteoporosis, chronic neurodegeneration, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, and multiple sclerosis.

### Claim 5 (depends on 1)

The method according to claim 1, wherein the composition further comprises a pharmaceutically acceptable excipient.

### Claim 6 (depends on 1)

The method according to claim 1, wherein the composition is in a form of a solution, syrup, powder, ointment, mixture, capsule, tablet, or an inhalable preparation.

### Claim 7 (depends on 1)

The method according to claim 1, wherein the composition is in a form suitable for parenteral, oral, topical or inhalable administration.

### Claim 8 (depends on 1)

The method according to claim 1, wherein the composition is part of a beverage, a food product, a functional food, a dietary supplement, or a nutritive substance.

### Claim 9 (depends on 1)

The method according to claim 1, wherein the composition is a pharmaceutical composition.

### Claim 10 (depends on 1)

The method of claim 1, wherein the composition comprises one or more of D-glyceric acid, DL-glyceric acid, a salt of D-glyceric acid, a salt of DL-glyceric acid, an ester of D-glyceric acid, and an ester of DL-glyceric acid.

### Claim 11 (depends on 10)

The method of claim 10, wherein the composition comprises one or more of D-glyceric acid, a salt of D-glyceric acid, and an ester of D-glyceric acid.

### Claim 12

A method of treating a non-communicable disease or disorder the method comprising administering a composition comprising one or more compounds selected from the group consisting of D-glyceric acid, DL-glyceric acid, L-glyceric acid, a salt of D-glyceric acid, a salt of DL-glyceric acid, an ester of D-glyceric acid, and an ester of DL-glyceric acid, wherein the salts of D-glyceric acid and DL-glyceric acid are calcium salts, as the only active substance or substances, to a subject in need thereof, wherein the composition enhances mitochondrial ATP production and simultaneously reduces excessive radical oxygen species formation from oxidative phosphorylation (OXPHOS), and wherein the non-communicable disease or disorder is selected from the group consisting of: a cardiovascular disease or disorder, mitochondrial DNA depletion, mitochondrial diseases, cerebrovascular accident, damage from acute head injury, acute or chronic renal failure, acute or chronic liver failure, splenomegaly, acute or chronic pancreatic failure, hemorrhagic shock, pre-eclampsia, thyroid disease, chronic fatigue, fibromyalgia, multi-organ dysfunction syndrome, epilepsy, bipolar disorder, psychiatric and mood disorders, cancer, obesity, high blood pressure, an age-related degeneration disease or disorder, rheumatoid arthritis, gout, and chronic obstructive pulmonary disease.

### Claim 13

A method of treating a non-communicable disease or disorder the method comprising administering a composition comprising one or more compounds selected from the group consisting of D-glyceric acid, DL-glyceric acid, L-glyceric acid, and salts and esters thereof, as the only active substance or substances, to a subject in need thereof, wherein the composition enhances mitochondrial ATP production and simultaneously reduces excessive radical oxygen species formation from oxidative phosphorylation (OXPHOS), and wherein the non-communicable disease or disorder is selected from the group consisting of: a cardiovascular disease or disorder, mitochondrial DNA depletion, mitochondrial diseases, cerebrovascular accident, damage from acute head injury, acute or chronic renal failure, acute or chronic liver failure, splenomegaly, acute or chronic pancreatic failure, hemorrhagic shock, pre-eclampsia, thyroid disease, chronic fatigue, fibromyalgia, multi-organ dysfunction syndrome, bipolar disorder, psychiatric and mood disorders, obesity, high blood pressure, an age-related degeneration disease or disorder, rheumatoid arthritis, gout, and chronic obstructive pulmonary disease.
