# US 11,306,130 B2 · PAR3 mimetic peptides and uses thereof

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- Number: US 11,306,130 B2
- Document ID: US11306130B2
- Status: Granted
- Kind: B2
- Application number: 16/090,526
- Filed: 2017-03-31
- Published: 2019-04-25
- Granted: 2022-04-19
- Earliest claimed: 2016-04-01
- Assignees: Arizona Board of Regents on Behalf of the University of Arizona; Board of Regents, The University of Texas System
- Applicants: Arizona Board of Regents On Behalf of the University of Arizona; Board of Regents, the University of Texas System
- Inventors: Josef Vagner; Scott A. Boitano; Theodore J. Price; Gregory O. Dussor
- Web page: https://patentgrep.com/patent/US11306130B2

## CPC

- C07K 14/705: Receptors; Cell surface antigens; Cell surface determinants {(tumour specific antigens C07K14/4748)}
- A61K 47/542: {Carboxylic acids, e.g. a fatty acid or an amino acid}
- A61K 47/543: {Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine}
- A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
- A61K 47/61: the organic macromolecular compound being a polysaccharide or a derivative thereof
- A61K 47/62: the modifying agent being a protein, peptide or polyamino acid
- A61P 25/00: Drugs for disorders of the nervous system
- C07K 5/081: {the side chain containing O or S as heteroatoms, e.g. Cys, Ser}
- C07K 7/06: having 5 to 11 amino acids
- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- C07K 2319/03: containing a transmembrane segment
- 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

This invention is in the field of medicinal pharmacology. In particular, the invention relates to protease activated receptor type 3 (PAR3) modulating compounds (e.g., mimetic peptides), compositions comprising such modulating compounds, and their use as therapeutics for the treatment of conditions involving PAR3 activity.

## Claims

### Claim 1

A composition comprising a protease activator receptor type-3 (PAR3) mimetic peptide consisting of Formula I: [activating peptide sequence]-[linker moiety]-[cell-membrane anchoring moiety] (Formula I), or pharmaceutically acceptable salts, lipidated analogs, pegylated analogs, and/or prodrugs thereof;
wherein the activating peptide sequence consists of the amino acid sequence selected from TFRGAPPNSFEEF (SEQ ID NO:1) and GAPPNSFEEF (SEQ ID NO:2);
wherein the linker moiety consists of a polyethylene glycol (PEG) moiety and/or multimers of 3,19-dioxo-2,8,11,14,21-pentaoxa-4,18-diazatricosan-23-oic acid;
wherein the cell-membrane anchoring moiety comprises a hydrophobic chemical moiety or a synthetic structure that forms a non-covalent binding interaction with a cell membrane; and
wherein the PAR3 mimetic peptide is configured to activate PAR3 biological activity.

### Claim 2 (depends on 1)

The composition of claim 1, wherein the cell-membrane anchoring moiety comprises at least one of a lipid moiety, multimers of 3,19-dioxo-2,8,11,14,21-pentaoxa-4,18-diazatricosan-23-oic acid, a saturated and unsaturated C12-C20 residues, hexadecyl, a cell-membrane homing structure, a cell-penetrating moiety, or a transmembrane domain.

### Claim 3 (depends on 1)

A method for increasing the activity of PARS in a subject in need thereof, comprising administering to the subject a composition as recited in claim 1.

### Claim 4 (depends on 3)

The method of claim 3, wherein the subject is a human subject.

### Claim 5 (depends on 3)

The method of claim 3, wherein the subject has or is at risk for developing chronic pain related to PARS activity.

### Claim 6 (depends on 5)

The method of claim 5, further comprising administering to the subject one or more pain relieving agents.

### Claim 7 (depends on 1)

A pharmaceutical composition comprising a composition as recited in claim 1 and a pharmaceutically acceptable carrier.

### Claim 8 (depends on 7)

A kit comprising (1) a pharmaceutical composition as recited in claim 7, (2) a container, pack, or dispenser, and (3) instructions for administration.