# US 10,865,226 B2 · Peptide showing melanogenesis promoting activity and use thereof

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- Number: US 10,865,226 B2
- Document ID: US10865226B2
- Status: Granted
- Kind: B2
- Application number: 16/615,899
- Filed: 2018-02-21
- Published: 2020-05-14
- Granted: 2020-12-15
- Earliest claimed: 2017-05-23
- Assignees: Caregen Co., Ltd.
- Applicants: Caregen Co., Ltd.
- Inventors: Yong Ji Chung; Eun Mi Kim; Eung-Ji Lee
- Web page: https://patentgrep.com/patent/US10865226B2

## CPC

- A61Q 19/04: for chemically tanning the skin (topical sun or radiation screening or tanning preparations A61Q17/04)
- C07K 7/06: having 5 to 11 amino acids
- A61K 8/64: Proteins; Peptides; Derivatives or degradation products thereof
- A61Q 19/00: Preparations for care of the skin
- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- A61K 2800/10: General cosmetic use
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- 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

Peptides exhibiting melanogenesis promoting activity are described. The peptides increase the activity and expression of tyrosinase and the expression of factors involved in melanogenesis, thereby exhibiting an outstanding effect on melanogenesis. The peptides can be used for the prevention, alleviation, and treatment of hypomelanosis. The outstanding activity and stability stated above allow the peptides to be very favorably applied to medicines, quasi-medicines, and cosmetics.

## Claims

### Claim 1

A peptide consisting of the amino acid sequence SEQ ID NO: 2 or SEQ ID NO: 3, wherein (i) the C-terminal end of the peptide is modified by the presence of an amino group or an azide group, or (ii) the N-terminal end of the peptide comprises a protecting group.

### Claim 2 (depends on 1)

The peptide of claim 1, wherein the C-terminal end of the peptide is modified by the presence of an amino group or an azide group.

### Claim 3 (depends on 1)

The peptide of claim 1, wherein the N-terminal end of the peptide comprises a protecting group.

### Claim 4 (depends on 3)

The peptide of claim 3, wherein the protecting group is selected from the group consisting of an acetyl group, a fluorenyl methoxy carbonyl group, a formyl group, a palmitoyl group, a myristyl group, a stearyl group, and polyethylene glycol (PEG).

### Claim 5

A pharmaceutical composition for the treatment of hypomelanosis, comprising, as an active ingredient, at least one peptide selected from the group consisting of a peptide consisting of the amino acid sequence of SEQ ID NO: 2 and a peptide consisting of the amino acid sequence of SEQ ID NO: 3, optionally wherein (i) the C-terminal end of the peptide is modified by the presence of an amino group or an azide group, or (ii) the N-terminal end of the peptide comprises a protecting group.

### Claim 6 (depends on 5)

The pharmaceutical composition of claim 5, wherein the hypomelanosis is vitiligo, albinism, nevus depigmentosus, pityriasis alba, pityriasis versicolor, post-inflammatory depigmentation, morphea, piebaldism, idiopathic guttate hypomelanosis, or leucoderma punctatum.

### Claim 7 (depends on 5)

The pharmaceutical composition of claim 5, wherein the C-terminal end of the at least one peptide is modified by the presence of an amino group or an azide group.

### Claim 8 (depends on 5)

The pharmaceutical composition of claim 5, wherein the N-terminal end of the at least one peptide comprises a protecting group.

### Claim 9 (depends on 8)

The pharmaceutical composition of claim 8, wherein the protecting group is selected from the group consisting of an acetyl group, a fluorenyl methoxy carbonyl group, a formyl group, a palmitoyl group, a myristyl group, a stearyl group, and polyethylene glycol (PEG).

### Claim 10

A cosmetic composition for the alleviation of hypomelanosis, comprising, as an active ingredient, at least one peptide selected from the group consisting of a peptide consisting of the amino acid sequence of SEQ ID NO: 2 and a peptide consisting of the amino acid sequence of SEQ ID NO: 3, optionally wherein (i) the C-terminal end of the peptide is modified by the presence of an amino group or an azide group, or (ii) the N-terminal end of the peptide comprises a protecting group.

### Claim 11 (depends on 10)

The cosmetic composition of claim 10, wherein the hypomelanosis is vitiligo, albinism, nevus depigmentosus, pityriasis alba, pityriasis versicolor, post-inflammatory depigmentation, morphea, piebaldism, idiopathic guttate hypomelanosis, or leucoderma punctatum.

### Claim 12 (depends on 10)

The cosmetic composition of claim 10, wherein the C-terminal end of the at least one peptide is modified by the presence of an amino group or an azide group.

### Claim 13 (depends on 10)

The cosmetic composition of claim 10, wherein the N-terminal end of the at least one peptide comprises a protecting group.

### Claim 14 (depends on 13)

The cosmetic composition of claim 13, wherein the protecting group is selected from the group consisting of an acetyl group, a fluorenyl methoxy carbonyl group, a formyl group, a palmitoyl group, a myristyl group, a stearyl group, and polyethylene glycol (PEG).

### Claim 15 (depends on 1)

A method for the treatment or alleviation of hypomelanosis in a subject in need thereof, the method comprising administration of a peptide of claim 1 to the subject.

### Claim 16 (depends on 15)

The method of claim 15, wherein the peptide is comprised within a pharmaceutical composition or a cosmetic composition.

### Claim 17 (depends on 15)

The method of claim 15, wherein the C-terminal end of the at least one peptide is modified by the presence of an amino group or an azide group.

### Claim 18 (depends on 15)

The method of claim 15, wherein the N-terminal end of the at least one peptide comprises a protecting group.

### Claim 19 (depends on 18)

The method of claim 18, wherein the protecting group is selected from the group consisting of an acetyl group, a fluorenyl methoxy carbonyl group, a formyl group, a palmitoyl group, a myristyl group, a stearyl group, and polyethylene glycol (PEG).

### Claim 20 (depends on 15)

The method composition of claim 15, wherein the hypomelanosis is vitiligo, albinism, nevus depigmentosus, pityriasis alba, pityriasis versicolor, post-inflammatory depigmentation, morphea, piebaldism, idiopathic guttate hypomelanosis, or leucoderma punctatum.
