# US 12,600,757 B2 · Peptides inhibiting gamma-c-cytokine activity and methods of use

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- Number: US 12,600,757 B2
- Document ID: US12600757B2
- Status: Granted
- Kind: B2
- Application number: 16/603,040
- Filed: 2018-04-04
- Published: 2021-10-21
- Granted: 2026-04-14
- Earliest claimed: 2017-04-07
- Assignees: Bioniz Therapeutics, Inc.
- Applicants: Bioniz, LLC
- Inventors: Nicholas Doerr; Laith Q. Al-Mawsawi; Nazli Azimi
- Web page: https://patentgrep.com/patent/US12600757B2

## CPC

- C07K 14/55: IL-2
- A61K 8/64: Proteins; Peptides; Derivatives or degradation products thereof
- A61K 47/646: {the entire peptide or protein drug conjugate elicits an immune response, e.g. conjugate vaccines}
- A61K 47/65: Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/06: Antipsoriatics
- A61P 17/14: for baldness or alopecia
- A61P 19/00: Drugs for skeletal disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61Q 3/00: Manicure or pedicure preparations
- A61Q 19/00: Preparations for care of the skin
- A61Q 19/08: Anti-ageing preparations
- C07K 14/54: Interleukins [IL]
- C07K 14/5443: {IL-15}
- 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 2319/02: containing a signal sequence
- C07K 2319/30: Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto
- 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
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS

## Abstract

Disclosed herein are stable peptide antagonists based on the consensus yc-subunit binding site to inhibit the activity of yc-cytokines. Such peptide antagonists are capable of inhibiting the activity of multiple yc-cytokine family members. The yc-family cytokines are associated with important human diseases, such as leukemia, autoimmune diseases, collagen diseases, diabetes mellitus, skin diseases, degenerative neuronal diseases and graft-versus-host disease (GvHD). Thus, inhibitors of yc-cytokine activity are valuable therapeutic and cosmetic agents as well as research tools.

## Claims

### Claim 1

A composite peptide comprising the amino acid sequence of SEQ ID NO: 83, wherein the composite peptide comprises at least one hydrocarbon linker element, and inhibits signaling activity of one or more γc-cytokines selected from the group consisting of IL-15 and IL-21.

### Claim 2 (depends on 1)

The composite peptide of claim 1, wherein the composite peptide has enhanced gastric stability as compared to the corresponding composite peptide without a hydrocarbon linker element.

### Claim 3 (depends on 1)

The composite peptide of claim 1, wherein the hydrocarbon linker element is an intra-peptide linker element.

### Claim 4 (depends on 1)

The composite peptide of claim 1, wherein the at least one hydrocarbon linker element is covalently attached to one or more chemical groups or molecules selected from the group consisting of alkyl, alkaryl, aryl, aralkyl, alkoxy, thioalkoxy, aryloxy, haloalkyl, halo, oxo, nitro, hydroxy, mercapto, carboxy, alkylcarbonyl, alkoxycarbonyl, alkanesulfonyl, amino, amido, azido, cyano, PEG, affinity labels, targeting moiety, fatty-acid derived acyl group, biotin, radioisotopes, non-protein fluorescent chemical groups, and protein fluorescent molecules.

### Claim 5 (depends on 1)

A pharmaceutical composition comprising:
the composite peptide of claim 1; and
a pharmaceutically acceptable carrier, diluent, excipient or combination thereof.

### Claim 6 (depends on 5)

A kit comprising the pharmaceutical composition of claim 5.

### Claim 7 (depends on 5)

A method of treating an IL-15 or IL-21-mediated disease, the method comprising administering the pharmaceutical composition of claim 5.

### Claim 8 (depends on 7)

The method of claim 7, wherein the IL-15 or IL-21-mediated disease is celiac disease or refractory celiac disease.

### Claim 9

A composite peptide comprising an amino acid sequence selected from the group consisting of SEQ ID NOS: 12 and 24, wherein the composite peptide comprises at least one hydrocarbon linker element, and inhibits signaling activity of one or more γc-cytokines selected from the group consisting of IL-15 and IL-21.

### Claim 10 (depends on 9)

The composite peptide of claim 9, wherein the composite peptide has enhanced gastric stability as compared to the corresponding composite peptide without a hydrocarbon linker element.

### Claim 11 (depends on 9)

The composite peptide of claim 9, wherein the hydrocarbon linker element is an intra-peptide linker element.

### Claim 12 (depends on 9)

The composite peptide of claim 9, wherein the at least one hydrocarbon linker element is covalently attached to one or more chemical groups or molecules selected from the group consisting of alkyl, alkaryl, aryl, aralkyl, alkoxy, thioalkoxy, aryloxy, haloalkyl, halo, oxo, nitro, hydroxy, mercapto, carboxy, alkylcarbonyl, alkoxycarbonyl, alkanesulfonyl, amino, amido, azido, cyano, PEG, affinity labels, targeting moiety, fatty-acid derived acyl group, biotin, radioisotopes, non-protein fluorescent chemical groups, and protein fluorescent molecules.

### Claim 13 (depends on 9)

A pharmaceutical composition comprising:
the composite peptide of claim 9; and
a pharmaceutically acceptable carrier, diluent, excipient or combination thereof.

### Claim 14 (depends on 13)

A kit comprising the pharmaceutical composition of claim 13.

### Claim 15 (depends on 13)

A method of treating an IL-15 or IL-21-mediated disease, the method comprising administering the pharmaceutical composition of claim 13.

### Claim 16 (depends on 15)

The method of claim 15, wherein the IL-15 or IL-21-mediated disease is celiac disease or refractory celiac disease.