# US 10,307,456 B2 · Use of short synthetic peptide for the treatment and/or prophylaxis of dry eye disease

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 10,307,456 B2
- Document ID: US10307456B2
- Status: Granted
- Kind: B2
- Application number: 15/552,529
- Filed: 2015-02-25
- Published: 2018-11-29
- Granted: 2019-06-04
- Earliest claimed: 2015-02-25
- Assignees: Mackay Memorial Hospital
- Applicants: Tsung-Chuan Ho; Yeou-Ping Tsao
- Inventors: Tsung-Chuan Ho; Yeou-Ping Tsao
- Web page: https://patentgrep.com/patent/US10307456B2

## CPC

- A61K 38/04: Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof ({enzyme inhibitors A61K38/005;} gastrins {A61K38/2207}, somatostatins A61K38/31, melanotropins A61K38/34 {; protease inhibitors A61K38/55})
- A61K 31/7036: having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
- A61K 31/7048: having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin {, digitoxin or digoxin}
- A61K 31/7052: having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K 38/13: Cyclosporins
- A61K 38/14: Peptides containing saccharide radicals; Derivatives thereof {, e.g. bleomycin, phleomycin, muramylpeptides or vancomycin}
- A61K 38/16: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof {(enzyme inhibitors A61K38/005)}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 27/02: Ophthalmic agents
- C07K 14/00: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K 14/001: {by chemical synthesis}
- A61K 2300/00: Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
- 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
- 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)

## Abstract

Disclosed herein are synthetic peptides and compositions comprising the same for the treatment and/or prophylaxis of an ocular disease, particularly, dry eye disease. Also disclosed herein are methods of treating and/or preventing an ocular disease by administering to a subject in need of such treatment a composition containing a synthetic peptide of the present disclosure.

## Claims

### Claim 1

A synthetic peptide consisting of 7 consecutive amino acid residues set forth as DLYRX1X2S (SEQ ID NO: 1), wherein X1 and X2 are respectively leucine and arginine, valine and arginine, glutamine and arginine, or glutamine and lysine.

### Claim 2 (depends on 1)

The synthetic peptide of claim 1, wherein at least one D-form amino acid residue is present in the amino acid sequence of SEQ ID NO: 1.

### Claim 3 (depends on 2)

The synthetic peptide of claim 2, wherein at least two D-form amino acid residues are present in the amino acid sequence of SEQ ID NO: 1.

### Claim 4

A method of treating a subject suffering from a dry eye disease (DED) comprising administering to the subject an effective amount of a synthetic peptide consisting of 7 consecutive amino acid residues set forth as DLYRX1X2S (SEQ ID NO: 1), wherein X1 and X2 are respectively leucine and arginine, valine and arginine, glutamine and arginine, or glutamine and lysine.

### Claim 5 (depends on 4)

The method of claim 4, wherein at least one D-form amino acid residue is present in the amino acid sequence of SEQ ID NO: 1.

### Claim 6 (depends on 4)

The method of claim 4, further comprising administering to the subject an effective amount of an agent selected from the group consisting of an anti-inflammatory agent, a calcineurin inhibitor, an antibiotic, a nicotinic acetylcholine receptor agonist, and an anti-lymphangiogenic agent for treating the DED.

### Claim 7 (depends on 4)

The method of claim 4, wherein the subject is a human.

### Claim 8 (depends on 5)

The method of claim 5, wherein at least two D-form amino acid residues are present in the amino acid sequence of SEQ ID NO: 1.

### Claim 9 (depends on 6)

The method of claim 6, wherein the anti-inflammatory agent is cyclosporine.

### Claim 10 (depends on 6)

The method of claim 6, wherein the calcineurin inhibitor is voclosporin.

### Claim 11 (depends on 6)

The method of claim 6, wherein the antibiotic is selected from the group consisting of, amikacin, gentamycin, kanamycin, neomycin, netilmicin, streptomycin, tobramycin, teicoplanin, vancomycin, azithromycin, clarithromycin, dirithromycin, erythromycin, roxithromycin, troleandomycin, amoxicillin, ampicillin, azlocillin, carbenicillin, cloxacillin, dicloxacillin, flucloxacillin, mezlocillin, nafcillin, penicillin, piperacillin, ticarcillin, bacitracin, colistin, polymyxin B, ciprofloxacin, enoxacin, gatifloxacin, levofloxacin, lomefloxacin, moxifloxacin, norfloxacin, ofloxacin, trovafloxacin, mafenide, sulfacetamide, sulfamethizole, sulfasalazine, sulfisoxazole, trimethoprim, cotrimoxazole, demeclocycline, doxycycline, minocycline, oxytetracycline, and tetracycline.

### Claim 12 (depends on 6)

The method of claim 6, wherein the nicotinic acetylcholine receptor agonist is selected from the group consisting of, pilocarpine, atropine, nicotine, epibatidine, lobeline, and imidacloprid.

### Claim 13 (depends on 6)

The method of claim 6, wherein the anti-lymphangiogenic agent is a vascular endothelial growth factor C (VEGF-C) antibody, a VEGF-D antibody or a VEGF-3 antibody.