# US 2019/0169117 A1 · Topical compositions for the treatment of dermatological disorders

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- Number: US 2019/0169117 A1
- Document ID: US20190169117A1
- Status: Published application
- Kind: A1
- Application number: 16/269,318
- Filed: 2019-02-06
- Published: 2019-06-06
- Earliest claimed: 2011-06-21
- Assignees: Evologie LLC
- Applicants: Evologie LLC
- Inventors: Gary I. Weinberger; H. Robert Nagel; Richard A. Brown
- Web page: https://patentgrep.com/patent/US20190169117A1

## CPC

- C07C 279/14: being further substituted by carboxyl groups
- A61K 9/107: Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)}
- A61K 31/194: having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
- A61K 31/198: Alpha-amino acids, e.g. alanine or edetic acid [EDTA] (betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00)
- A61K 31/223: of alpha-aminoacids
- A61K 31/60: Salicylic acid; Derivatives thereof
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/06: Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- 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)

## Abstract

The present invention relates to pharmaceutical compositions and methods useful for the treatment of dermatological disorders, and in particular acne vulgaris and skin pigmentation disorders. Pharmaceutical compositions comprising one or more arginine, salicylic acid and/or azelaic acid that are useful for the treatment of dermatological diseases and the symptoms and underlying causes of such dermatological diseases are also disclosed.

## Claims

### Claim 1

A pharmaceutical composition comprising a tripartite complex and an anti-melanogenic compound, wherein the tripartite complex consists of L-arginine, azelaic acid, and salicylic acid.

### Claim 2 (depends on 1)

The pharmaceutical composition of claim 1, wherein the anti-melanogenic compound is selected from the group consisting of glabridin, licorice, glycyrrhiza glabra root extract, hesperidin, kojic acid, kojic dipalmitate, azelaic acid, niacin, melanowhite, and leukocyte extract.

### Claim 3 (depends on 1)

The pharmaceutical composition of claim 1, wherein the anti-melanogenic compound comprises glabridin.

### Claim 4 (depends on 1)

The pharmaceutical composition of claim 1,
wherein the composition is in the form of an emulsion, and
wherein the emulsion comprising an aqueous phase and an oil phase.

### Claim 5 (depends on 4)

The pharmaceutical composition of claim 4,
wherein the emulsion further comprises one or more salts dispersed therein,
wherein the salts are selected from the group consisting of a micronized L-arginate salt of salicylic acid, and a micronized L-arginate salt of azelaic acid, and
wherein the salts stabilize the emulsion by preventing the oil phase and the aqueous phase from coalescing.

### Claim 6 (depends on 5)

The pharmaceutical composition of claim 5, wherein the one or more salts are unsolubilized.

### Claim 7 (depends on 5)

The pharmaceutical composition of claim 5, wherein the aqueous phase comprises the micronized L-arginate salt of salicylic acid and the micronized L-arginate salt of azelaic acid.

### Claim 8 (depends on 1)

The pharmaceutical composition of claim 1, wherein the L-arginine that comprises the tripartite complex is an L-arginine alkyl ester.

### Claim 9 (depends on 1)

The pharmaceutical composition of claim 1, wherein the composition remains stable for at least 2 years upon storage at 37° C.

### Claim 10 (depends on 1)

The pharmaceutical composition of claim 1, wherein the composition is in the form of an oil, serum, ointment, cream, lotion, gel, shampoo, a saturated pad, a spray or a cleanser.

### Claim 11 (depends on 1)

A method of treating a subject with a dermatological disorder,
wherein the method comprises topically administering to the subject the pharmaceutical composition of claim 1, and
wherein the dermatological disorder is selected from the group consisting of post-inflammatory hyperpigmentation (PIH), low skin hydration, excess sebum production, and acne vulgaris.

### Claim 12

A method of treating a dermatological disorder,
wherein the method comprises topically administering to a subject affected with the dermatological disorder a pharmaceutical composition comprising a tripartite complex and an anti-melanogenic compound, and
wherein the tripartite complex consists of L-arginine, azelaic acid, and salicylic acid.

### Claim 13 (depends on 12)

The method of claim 12, wherein the anti-melanogenic compound is selected from the group consisting of glabridin, licorice, glycyrrhiza glabra root extract, hesperidin, kojic acid, kojic dipalmitate, azelaic acid, niacin, melanowhite, and leukocyte extract.

### Claim 14 (depends on 12)

The method of claim 12, wherein the anti-melanogenic compound comprises glabridin.

### Claim 15 (depends on 12)

The method of claim 12,
wherein the composition is in the form of an emulsion, and
wherein the emulsion comprises an aqueous phase and an oil phase.

### Claim 16 (depends on 15)

The method of claim 15,
wherein the emulsion further comprises one or more salts dispersed therein,
wherein the salts are selected from the group consisting of a micronized L-arginate salt of salicylic acid, and a micronized L-arginate salt of azelaic acid, and
wherein the salts stabilize the emulsion by preventing the oil phase and the aqueous phase from coalescing.

### Claim 17 (depends on 16)

The method of claim 16, wherein the one or more salts are unsolubilized.

### Claim 18 (depends on 15)

The method of claim 15, wherein the composition remains stable for at least 2 years upon storage at 37° C.

### Claim 19 (depends on 12)

The method of claim 12, wherein the dermatological disorder is selected from the group consisting of acne vulgaris and post-inflammatory hyperpigmentation (PIH), low skin hydration, excess sebum production and acne vulgaris.

### Claim 20 (depends on 12)

The pharmaceutical composition of claim 12, wherein the composition is in the form of an oil, serum, ointment, cream, lotion, gel, shampoo, a saturated pad, a spray or a cleanser.

### Claim 21

A pharmaceutical composition comprising a tripartite complex and an anti-melanogenic compound,
wherein the tripartite complex has a structure of formula (I):
wherein x, y and z are each any positive integer.

### Claim 22 (depends on 21)

The pharmaceutical composition of claim 21, wherein the composition is in the form of an emulsion,
wherein the emulsion comprises an aqueous phase and an oil phase,
wherein the emulsion further comprises one or more salts dispersed therein and selected from the group consisting of a micronized L-arginate salt of salicylic acid, and a micronized L-arginate salt of azelaic acid, and
wherein the salts stabilize the emulsion by preventing the oil phase and the aqueous phase from coalescing.

### Claim 23 (depends on 22)

The pharmaceutical composition of claim 22, wherein the one or more salts are unsolubilized.

### Claim 24 (depends on 22)

The pharmaceutical composition of claim 22, wherein the anti-melanogenic compound is selected from the group consisting of glabridin, licorice, glycyrrhiza glabra root extract, hesperidin, kojic acid, kojic dipalmitate, azelaic acid, niacin, melanowhite, and leukocyte extract.

### Claim 25 (depends on 22)

The pharmaceutical composition of claim 22, wherein the anti-melanogenic compound comprises glabradin.

### Claim 26 (depends on 22)

The pharmaceutical composition of claim 22, wherein the composition is in the form of an oil, serum, ointment, cream, lotion, gel, shampoo, a saturated pad, a spray or a cleanser.

### Claim 27 (depends on 22)

A method of treating a dermatological disorder,
wherein the method comprises topically administering to a subject affected with the dermatological disorder the pharmaceutical composition of claim 22, and
wherein the dermatological disorder is selected from the group consisting of acne vulgaris and post-inflammatory hyperpigmentation (PIH), low skin hydration, excess sebum production and acne vulgaris.
