# US 7,745,575 B1 · OsK1 derivatives

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- Number: US 7,745,575 B1
- Document ID: US7745575B1
- Status: Granted
- Kind: B1
- Application number: 11/571,005
- Filed: 2005-06-27
- Granted: 2010-06-29
- Earliest claimed: 2004-06-25
- Assignees: Cellpep Pharma Inc.
- Inventors: Stephanie Mouhat; Jean-Marc Sabatier; Bonabes Olivier de Rouge
- Web page: https://patentgrep.com/patent/US7745575B1

## CPC

- C07K 14/43522: {from scorpions}
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 37/02: Immunomodulators
- 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

OsK1 is a 38-residue peptide with 3 disulphide bridges and is found in the venom of the scorpion Orthochirus scrobiculosus. It is potently active on voltage-gated K+ channels Kv1.1, Kv1.2 and Kv1.3, and moderately active on the type 1 intermediate-conductance Cat2+-activated channel KCa3.1. Derivatives of OsK1, particularly involving truncation or point mutations, have been developed to enhance the activity against and selectivity for the Kv1.3 channel. This renders the derivatives likely candidates for the treatment of autoimmune diseases, including multiple sclerosis. Such use may be alone or in combination therapy with maurotoxin, another scorpion toxin.

## Claims

### Claim 1

An OsK1 derivative selected from the group consisting of the following OsK1 derivatives:
[Δ1]-OsK1,
[A34]-OsK1,
[K16]-OsK1,
[D20]-OsK1,
[K16,D20]-OsK1,
[Δ1,K16,D20]-OsK1,
[Δ1,T2,K16,D20]-OsK1,
[Δ1-4,K16,D20]-OsK1,
[Δ1-6,K16,D20]-OsK1,
[Δ1-7,K16,D20]-OsK1,
[K3,K16,D20]-OsK1,
[P12,K16,D20]-OsK1,
[K16,D20,N25]-OsK1,
[K16,D20,R31]-OsK1,
[K16,D20,Y36]-OsK1, and
[K12, K16,R19,D20]-OsK1.

### Claim 2 (depends on 1)

An OsK1 derivative according to claim 1, which is terminated at the N-terminal with an acetyl group or which is amidated at the C-terminal.

### Claim 3 (depends on 1)

An OsK1 derivative according to claim 1, which is terminated with an ω-amino-fatty acid having from 4 to 10 carbon atoms and from 0 to 2 carbon-carbon double bonds.

### Claim 4 (depends on 1)

A pharmaceutical composition comprising an OsK1 derivative according to claim 1 in admixture with a pharmaceutically acceptable diluent or carrier.

### Claim 5 (depends on 1)

An OsK1 derivative according to claim 1, wherein said derivative is [Δ1-7,K16,D20]-OsK1 (SEQ ID NO: 19).

### Claim 6 (depends on 1)

An OsK1 derivative according to claim 1, wherein said derivative is [K16,D20]-OsK1 (SEQ ID NO: 14).