# US 8,772,241 B2 · Peptide and use thereof

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- Number: US 8,772,241 B2
- Document ID: US8772241B2
- Status: Granted
- Kind: B2
- Application number: 13/701,465
- Filed: 2011-06-22
- Published: 2013-05-02
- Granted: 2014-07-08
- Earliest claimed: 2010-06-30
- Assignees: Ensoltek Co., Ltd.
- Applicants: Hae Jin Kim; Je Wook Lee; Young Joon Kwon; Eun Joung Moon
- Inventors: Hae Jin Kim; Je Wook Lee; Young Joon Kwon; Eun Joung Moon
- Web page: https://patentgrep.com/patent/US8772241B2

## CPC

- C07K 7/06: having 5 to 11 amino acids
- A61K 38/08: Peptides having 5 to 11 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61K 38/1841: {Transforming growth factor [TGF]}
- A61P 19/00: Drugs for skeletal disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention provides a peptide represented by formula (I) of X1-Leu-X2-Leu-X3 wherein X1 represents Glu or Asp, X2 represents His, Lys or Arg, X3 represents Asp or Glu, with Glu, Asp, Leu, His, Lys and Arg being respectively glutamic acid, aspartic acid, leucine, histidine, lysine and arginine; or a pharmaceutically acceptable salt thereof; a composition for the treatment or prevention of at least one selected from cartilage damage and arthritis, containing the same peptide or a pharmaceutically acceptable salt thereof as an active ingredient; and a composition containing the same peptide or a pharmaceutically acceptable salt thereof and TGFβ1. The above-mentioned peptide or a pharmaceutically acceptable salt thereof is effective for the treatment and/or prevention of cartilage damage and/or arthritis and is capable of exhibiting effects of the regeneration of cartilage tissue, the inhibition of the expression of cartilage tissue matrix degrading enzyme and/or the inhibition of cartilage tissue ossification.

## Claims

### Claim 1

An isolated peptide consisting of the amino acid sequence of formula (I)
X1-Leu-X2-Leu-X3 (I)
or pharmaceutically acceptable salt thereof,
wherein X1 is Glu or Asp; X2 is His, Lys or Arg; X3 is Asp or Glu, and Glu, Asp, Leu, His, Lys, and Arg are glutamic acid, aspartic acid, leucine, histidine, lysine, and arginine, respectively.

### Claim 2

An isolated peptide consisting of the amino acid sequence of SEQ ID NO: 1 (Glu-Leu-His-Leu-Asp) or pharmaceutically acceptable salt thereof,
wherein and Glu, Asp, Leu, His, Lys, and Arg are glutamic acid, aspartic acid, leucine, histidine, lysine, and arginine, respectively.

### Claim 3 (depends on 1)

A composition comprising the peptide of claim 1 or a pharmaceutically acceptable salt thereof as an active ingredient.

### Claim 4 (depends on 3)

The composition according to claim 3, wherein the composition is a pharmaceutical composition.

### Claim 5 (depends on 1)

A composition comprising the peptide of claim 1 or a pharmaceutically acceptable salt thereof and transforming growth factor beta 1 (TGFβ1).

### Claim 6 (depends on 2)

A composition comprising the peptide of claim 2 or a pharmaceutically acceptable salt thereof as an active ingredient.

### Claim 7 (depends on 2)

A composition comprising the peptide of claim 2 or a pharmaceutically acceptable salt thereof and transforming growth factor beta 1 (TGFβ1).

### Claim 8 (depends on 3)

The composition of claim 3, wherein administering the composition promotes the production of type II collagen.