# US 2019/0169256 A1 · Antagonists of fish reproduction

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- Number: US 2019/0169256 A1
- Document ID: US20190169256A1
- Status: Published application
- Kind: A1
- Application number: 16/175,012
- Filed: 2018-10-30
- Published: 2019-06-06
- Earliest claimed: 2014-07-17
- Assignees: Yissum Research Development Company of the Hebrew University of Jerusalem
- Applicants: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.
- Inventors: Berta LEVAVI-SIVAN; Chaim GILON
- Web page: https://patentgrep.com/patent/US20190169256A1

## CPC

- C07K 14/57545: {Neuropeptide Y}
- A23K 10/00: Animal feeding-stuffs
- A23K 20/147: Polymeric derivatives, e.g. peptides or proteins
- A23K 50/80: for aquatic animals, e.g. fish, crustaceans or molluscs
- A61K 9/0029: {Parenteral nutrition; Parenteral nutrition compositions as drug carriers}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- C07K 7/22: {Tachykinins, e.g.} Eledoisins {, Substance P}; Related peptides
- 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)
- A23K: FODDER
- 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

Peptide-based neurokinin antagonists of fish reproduction are disclosed. Compositions comprising antagonists of fish neurokinin and methods of inhibiting or delaying puberty, fish maturation or reproduction processes using these compounds are also provided.

## Claims

### Claim 1

A peptidomimetic of 6-10 amino acid residues comprising the sequence X1-NMeVal-βAla-Leu-Met-Z (SEQ ID NO: 7), wherein X1 consists of 2 or 3 amino acid residues comprising an aromatic residue, a negatively charged (acidic) residue, and optionally an N-terminal capping moiety or modification; and Z represents the C-terminus of the peptide which may be amidated, acylated, reduced or esterified.

### Claim 2 (depends on 1)

The peptidomimetic of claim 1, wherein X comprises an N-terminal capping moiety.

### Claim 3 (depends on 1)

The peptidomimetic of claim 1, wherein X1 consists of 2 or 3 amino acids and an N-terminal capping moiety.

### Claim 4 (depends on 3)

The peptidomimetic of claim 3, wherein the N-terminal capping moiety is selected from the group consisting of: succinyl, oxalyl, malonyl, glutaryl, adipoyl, pimaloyl, suberoyl, and acetyl.

### Claim 5 (depends on 1)

The peptidomimetic of claim 1, comprising an amidated C-terminus.

### Claim 6 (depends on 1)

The peptidomimetic co claim 1, comprising an amidated C-terminus and an N-terminal capping moiety.

### Claim 7 (depends on 1)

The peptidomimetic of claim 1, consisting of 6-7 amino acid residues and an N-terminal capping moiety.

### Claim 8 (depends on 1)

The peptidomimetic of claim 1, wherein X1 is selected from the group consisting of: Succ-Asp-Phe; Succ-Asp-Ser-Phe; and Succ-Asp-Ser-DTrp.

### Claim 9 (depends on 8)

The peptidomimetic of claim 8 selected from the group consisting of:
(SEQ ID NO: 2)
Succ-Asp-Phe-N(Me)Val-βAla-Leu-Met-NH2;
(SEQ ID NO: 3)
Succ-Asp-Ser-Phe-N(Me)Val-βAla-Leu-Met-NH2;
(SEQ ID NO: 6)
Succ-Asp-Ser-DTrp-N(Me)Val-βAla-Leu-Met-NH2;
wherein Succ denotes a succinyl.

### Claim 10 (depends on 1)

A food composition comprising at least one peptidomimetic according to claim 1.

### Claim 11 (depends on 10)

The food composition of claim 10, wherein the at least one peptidomimetic is selected from the group consisting of SEQ ID NO: 2, SEQ ID NO: 3 and SEQ ID NO: 6.

### Claim 12 (depends on 10)

The food composition of claim 10, comprising at least one nutrient.

### Claim 13 (depends on 10)

The food composition of claim 10, comprising at least one food additive.

### Claim 14 (depends on 10)

The food composition of claim 10, formulated for administration to fish as part of regular food or water consumption.

### Claim 15 (depends on 1)

A pharmaceutical composition comprising at least one peptidomimetic according to claim 1 and at least one acceptable carrier, diluent, salt or excipient.

### Claim 16 (depends on 15)

The pharmaceutical composition of claim 15 formulated for administration to fish by a route selected from the group consisting of: intraparietal administration, oral administration and administration by immersion.

### Claim 17 (depends on 1)

A method of inhibiting at least one parameter of fish reproduction or maturation, the method comprising administering to fish a food or a pharmaceutical composition comprising at least one peptidomimetic according to claim 1.

### Claim 18 (depends on 17)

The method of claim 17 wherein inhibition of fish reproduction or maturation results in increased weight of the treated fish.

### Claim 19 (depends on 17)

The method of claim 17, wherein fish is selected from the group consisting of: tilapia, carp, salmon, bass, catfish and mullet.

### Claim 20 (depends on 17)

The method of claim 17, wherein the composition is administered to fish by a route selected from the group consisting of: parenteral, oral and administration by immersion.