# US 12,215,173 B2 · Kappa opioid receptor peptide amide ligands

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- Number: US 12,215,173 B2
- Document ID: US12215173B2
- Status: Granted
- Kind: B2
- Application number: 16/988,229
- Filed: 2020-08-07
- Published: 2021-02-11
- Granted: 2025-02-04
- Earliest claimed: 2019-08-07
- Assignees: Humanwell Pharmaceutical US; Yichang Humanwell Pharmaceuticals Co. Ltd.
- Applicants: Humanwell Pharmaceutical US
- Inventors: Subo Liao; Jun Yang; Jinliang Lv; Zongquan Liao; Hao Zhou; Jueyuan Gao; Tianpeng Xie; Quanli Yang; Lei Wang; Zejian Ding
- Web page: https://patentgrep.com/patent/US12215173B2

## CPC

- C07K 5/1016: {and aromatic or cycloaliphatic}
- C07K 7/02: Linear peptides containing at least one abnormal peptide link
- 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)
- 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

The present invention provides kappa opioid receptor peptide agonists, methods for preparing these compounds, compositions comprising these kappa opioid receptor peptide agonists, and methods of using the kappa opioid receptor peptide agonists to treat pain or other conditions.

## Claims

### Claim 1

A kappa opioid receptor peptide ligand of Formula (I) or a salt thereof:
A1-A2-A3-A4-B Formula (I),
wherein A1 is D-phenylalanine, A2 is D-phenylalanine, A3 is D-leucine, A4 is D-lysine, and B is selected from the group consisting of:
wherein represents the connection to A4.

### Claim 2 (depends on 1)

A composition comprising: the kappa opioid receptor peptide ligand of claim 1 and at least one pharmaceutically acceptable excipient.