# US 2010/0168015 A1 · Peptides with capacity for binding with interleukine 10 (il-10)

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- Number: US 2010/0168015 A1
- Document ID: US20100168015A1
- Status: Published application
- Kind: A1
- Application number: 12/593,321
- Filed: 2008-03-27
- Published: 2010-07-01
- Earliest claimed: 2007-03-27
- Assignees: Proyecto De Biomedicina Cima, S.L.
- Inventors: Lorea Manterola Careaga; Inés Noelia Casares Lagar; Nancy Diaz-Valdés Farray; Javier Dotor De Las Herrerias; Juan José Lasarte Sagastibelza; Pablo Sarobe Ugarriza; Jesús Prieto Valtueña; Francisco Borràs Cuesta
- Web page: https://patentgrep.com/patent/US20100168015A1

## CPC

- C07K 14/5428: {IL-10}
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/04: Antibacterial agents
- A61P 31/06: for tuberculosis
- A61P 31/08: for leprosy
- A61P 31/14: for RNA viruses
- A61P 33/02: Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P 33/06: Antimalarials
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The invention relates to peptides having the capacity to bind to interleukin-10 (IL-10) and their use in the treatment of clinical conditions or pathological disorders associated to IL-10 expression, particularly to a high IL-10 expression, for example, infectious diseases, tumors, cancers and acute damage conditions.

## Claims

### Claim 1

A peptide with the capacity to bind to IL-10 selected from:
a) a peptide the amino acid sequence of which is selected from the group consisting of SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3, SEQ ID NO: 4, SEQ ID NO: 5, SEQ ID NO: 6, SEQ ID NO: 8, SEQ ID NO: 9, SEQ ID NO: 10, SEQ ID NO: 11, SEQ ID NO: 12, SEQ ID NO: 13, SEQ ID NO: 14, SEQ ID NO: 15, SEQ ID NO: 16, SEQ ID NO: 17, SEQ ID NO: 18, SEQ ID NO: 19, SEQ ID NO: 20, SEQ ID NO: 21; SEQ ID NO: 22; SEQ ID NO: 23; SEQ ID NO: 24; SEQ ID NO: 25; SEQ ID NO: 26; SEQ ID NO: 33; SEQ ID NO: 34; SEQ ID NO: 35 and SEQ ID NO: 36,
b) a variant of a peptide defined in a); and
c) a fragment of a peptide defined in a) or of a variant defined in b), comprising between 5 and 15 consecutive amino acids; and
its pharmaceutically acceptable salts.

### Claim 2 (depends on 1)

A peptide according to claim 1, selected from the group consisting of the peptides identified as SEQ ID NO: 45, SEQ ID NO: 46, SEQ ID NO: 47, SEQ ID NO: 48, SEQ ID NO: 49, SEQ ID NO: 50, SEQ ID NO: 51, SEQ ID NO: 52 and SEQ ID NO: 53, and their pharmaceutically acceptable salts.

### Claim 3 (depends on 1)

A peptide according to claim 1, wherein said peptide has the capacity to inhibit the biological activity of IL-10 in vitro and/or in vivo.

### Claim 4 (depends on 3)

A peptide according to claim 3, selected from the group consisting of the peptides identified as SEQ ID NO: 1, SEQ ID NO: 6, SEQ ID NO: 8, SEQ ID NO: 10, SEQ ID NO:
13, SEQ ID NO: 14, SEQ ID NO: 16, SEQ ID NO: 19 and SEQ ID NO: 25, a variant or a fragment thereof, and their pharmaceutically acceptable salts.

### Claim 5 (depends on 1)

A nucleic acid sequence encoding a peptide according to claim 1.

### Claim 6 (depends on 5)

A gene construct comprising a nucleic acid sequence according to claim 5.

### Claim 7 (depends on 5)

A vector comprising a nucleic acid sequence according to claim 5.

### Claim 8 (depends on 5)

A host cell comprising a nucleic acid sequence according to claim 5.

### Claim 9 (depends on 1)

A pharmaceutical composition comprising a therapeutically effective amount of a peptide according to claim 1 together with at least one pharmaceutically acceptable excipient.

### Claim 10 (depends on 9)

A pharmaceutical composition according to claim 9, further comprising one or more different IL-10 inhibitor compounds.

### Claim 11 (depends on 1)

A method of treating a clinical condition or pathological disorder presenting IL-10 expression, said method comprising administering a peptide of claim 1 to a human or animal body to inhibit the biological activity of IL-10 and thus treat the clinical conditions and pathological disorders associated to IL-10 expression.

### Claim 12 (depends on 11)

The method according to claim 11, wherein the treatment of a clinical condition or pathological disorder presenting IL-10 expression comprises clinical conditions or pathological disorders in which Th1 cell response is inhibited.

### Claim 13 (depends on 11)

The method according to claim 11, wherein the treatment of a clinical condition or pathological disorder presenting IL-10 expression is selected from the group consisting of an infectious disease, a tumor, a cancer and an acute damage situation.

### Claim 14 (depends on 13)

The method according to claim 13, wherein the treatment is selected from the group consisting of: an infection caused by Mycobacterium leprae, Mycobacterium tuberculosis, Yersinia pestis, Helicobacter pylori, Candida albicans, Trichophyton rubrum, Aspergillus sp., Plasmodium falciparum, leishmaniasis, and toxoplasmosis; treatment of a Hodgkin's lymphoma; head and neck cancer; melanoma; or basal cell carcinomas and squamous cell carcinomas developed from keratinocytes mutated by UV; and for the treatment of burns and associated sepsis.

### Claim 15 (depends on 1)

A process for producing a peptide according to claim 1, which comprises growing a host cell comprising the nucleic acid sequences of the peptide under conditions allowing the production of said peptide and, if desired, the recovery of said peptide.

### Claim 16 (depends on 5, 6, 7, 8)

A pharmaceutical composition comprising a pharmaceutically acceptable carrier and one of (i) a therapeutically effective amount of a nucleic acid sequence according to claim 5, (ii) a therapeutically effective amount of a gene construct according to claim 6, (iii) a therapeutically effective amount of a vector according to claim 7, or (iv) a therapeutically effective amount of a host cell according to claim 8.

### Claim 17 (depends on 1)

A pharmaceutical composition comprising a therapeutically effective amount of a peptide according to claim 1 together with one or more different IL-10 inhibitor compounds.