# US 10,501,511 B2 · Low molecular polypeptide for preventing and treating inflammation and use thereof

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- Number: US 10,501,511 B2
- Document ID: US10501511B2
- Status: Granted
- Kind: B2
- Application number: 15/024,229
- Filed: 2014-08-13
- Published: 2017-02-09
- Granted: 2019-12-10
- Earliest claimed: 2013-08-15
- Assignees: Shanghai First People's Hospital
- Applicants: Shanghai First People's Hospital
- Inventors: Xun Xu; Lili Wang; Yi Xu
- Web page: https://patentgrep.com/patent/US10501511B2

## CPC

- C07K 14/4753: {Hepatocyte growth factor; Scatter factor; Tumor cytotoxic factor II}
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 17/00: Drugs for dermatological disorders
- A61P 19/00: Drugs for skeletal disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 27/02: Ophthalmic agents
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/0048: {Eye, e.g. artificial tears}
- 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)
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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

Disclosed are a low molecular polypeptide for preventing and treating inflammation, a preparation method and the use thereof and a pharmaceutical composition containing the polypeptide, wherein the polypeptide can penetrate the eye tissue barrier, can maintain a high concentration in neutral tears, aqueous humour and vitreous humour, and can be used to treat inflammation.

## Claims

### Claim 1

A method for treating an ocular inflammatory disease, comprising administering a polypeptide or a pharmaceutically acceptable salt thereof at a concentration of at least 10 μM, to a subject having an ocular inflammatory disease, wherein the polypeptide is selected from the group consisting of peptide SEQ ID NOS: 2-8, wherein the polypeptide exhibits an activity of inhibiting inflammation, and wherein the ocular inflammatory disease is selected from the group consisting of blepharitis, conjunctivitis, scleritis, and optic neuritis.

### Claim 2 (depends on 1)

The method of claim 1, wherein the polypeptide is one or more polypeptides selected from the group consisting of: SEQ ID NO.3, SEQ ID NO.4, SEQ ID NO.5, SEQ ID NO.6, SEQ ID NO.7, and SEQ ID NO.8.

### Claim 3 (depends on 1)

The method of claim 1, wherein the polypeptide is administered as a pharmaceutical composition comprising:
(a) the polypeptide or a pharmaceutically acceptable salt thereof; and
(b) a pharmaceutically acceptable carrier or excipient.

### Claim 4 (depends on 3)

The method of claim 3, wherein the pharmaceutical composition is in a dosage form of eyedrop, injection, eye gel, or eye ointment.

### Claim 5 (depends on 3)

The method of claim 3, wherein the pharmaceutical composition further comprises a corticosteroid, an immunosuppressant, or a non-steroidal anti-inflammatory drug.