# US 9,517,225 B2 · Low dose lipoic acid pharmaceutical compositions and methods

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- Number: US 9,517,225 B2
- Document ID: US9517225B2
- Status: Granted
- Kind: B2
- Application number: 14/697,205
- Filed: 2015-04-27
- Published: 2015-10-22
- Granted: 2016-12-13
- Earliest claimed: 2008-03-05
- Assignees: Encore Health, LLC
- Applicants: Encore Health, LLC
- Inventors: William Garner; Margaret Garner
- Web page: https://patentgrep.com/patent/US9517225B2

## CPC

- A61K 31/385: having two or more sulfur atoms in the same ring
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 31/19: Carboxylic acids, e.g. valproic acid (salicylic acid A61K31/60)
- A61K 31/20: having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
- A61P 27/02: Ophthalmic agents
- A61P 39/06: Free radical scavengers or antioxidants
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Compositions containing low doses of lipoic acid-based active agents and methods for using the same are provided. In particular, compositions containing low dose lipoic acid, lipoic acid derivatives, said lipoic acid seleno-derivatives and are provided to prevent and/or treat ocular diseases.

## Claims

### Claim 1

A pharmaceutical composition for ocular use comprising an active agent or a salt or ester thereof, in an amount of about 5 μM to about 250 μM and at least one pharmaceutically acceptable carrier, wherein the active agent is 5-(1,2thiaselenolan-5-yl)pentanoic acid; 5-)1,2-thiaselenolan-3-yl)pentanoic acid; or a salt or ester thereof.

### Claim 2

A method of treating presbyopia, comprising administering to a human in need thereof a pharmaceutical composition for ocular use comprising an active agent that is:
5-(1,2-dithiolan-3-yl)pentanoic acid;
6,8-dimercaptooctanoic acid;
dihydrolipoate;
5-(1,2-thiaselenolan-5-yl)pentanoic acid,
5-(1,2-thiaselenolan-3-yl)pentanoic acid;
or a salt or ester thereof, in an amount of about 5 μM to about 250 μM and at least one pharmaceutically acceptable carrier.

### Claim 3 (depends on 2)

The method of claim 2, further comprising administering to the human a chemical energy source simultaneously or consecutively with the active agent.

### Claim 4 (depends on 3)

The method of claim 3, wherein the chemical energy source is administered simultaneously with the active agent.

### Claim 5 (depends on 3)

The method of claim 3, wherein the chemical energy source is glucose or NADPH.

### Claim 6 (depends on 2)

The method of claim 2, further comprising applying energy to the lens of the human to facilitate breaking disulfide bonds.

### Claim 7 (depends on 6)

The method of claim 6, wherein the energy is applied to a localized region of the lens of the human.

### Claim 8 (depends on 2)

The method of claim 2, wherein the active agent is administered via a topical ocular, subtenons, subconjunctival, intracameral, intravitreal, or iontophoresis route.

### Claim 9 (depends on 2)

The method of claim 2, wherein the method increases accommodative amplitude of the lens of the human to, or maintains an accommodative amplitude of the lens of the human, at least 2% greater than the accommodative amplitude expected in an untreated lens of about the same age as measured in diopters.

### Claim 10 (depends on 2)

The method of claim 2, wherein the method increases accommodative amplitude by at least 0.25 diopters.

### Claim 11 (depends on 2)

The method of claim 2, wherein the method increases lens elasticity of the lens of the human to, or maintains a lens elasticity of the lens of the human, at least 2% greater than the elasticity expected in an untreated lens of about the same age as measured by E.

### Claim 12 (depends on 2)

The method of claim 2, wherein the method decreases lens opacity of the lens of the human to, or maintains lens opacity of the lens of the human at, at least 2% less than the opacity expected in an untreated lens of about the same age.