# US 10,370,413 B2 · Kv1.3 potassium channel antagonists

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- Number: US 10,370,413 B2
- Document ID: US10370413B2
- Status: Granted
- Kind: B2
- Application number: 15/309,781
- Filed: 2015-05-07
- Published: 2017-05-18
- Granted: 2019-08-06
- Earliest claimed: 2014-05-08
- Assignees: cgtx-Peptide Development GmbH
- Applicants: cgtx-Peptide Development GmbH
- Inventors: Andreas Klostermann; Jörg Stockhaus
- Web page: https://patentgrep.com/patent/US10370413B2

## CPC

- C07K 14/00: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61P 1/02: Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/06: Antihyperlipidemics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/14: of the thyroid hormones, e.g. T3, T4
- A61P 5/40: Mineralocorticosteroids, e.g. aldosterone; Drugs increasing or potentiating the activity of mineralocorticosteroids
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 7/06: Antianaemics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/06: Antigout agents, e.g. antihyperuricemic or uricosuric agents
- A61P 21/04: for myasthenia gravis
- A61P 27/02: Ophthalmic agents
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 14/4703: {Inhibitors; Suppressors}
- C07K 14/705: Receptors; Cell surface antigens; Cell surface determinants {(tumour specific antigens C07K14/4748)}
- 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)
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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
- 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)
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

Compounds which selectively bind to and inhibit the activity of the potassium channel Kv1.3 are described. Pharmaceutical compositions comprising such compounds and the use of said compounds and said pharmaceutical compositions for the treatment or prevention of autoimmune diseases, obesity, parodontitis and/or tissue transplant rejection are also described.

## Claims

### Claim 1

A composition comprising a peptide having the amino acid sequence X1-X2-X3-N-V-X4-C-X5-X6-X7-X8-X9C-X10-X11-X12-C-X13-X14-X15-T-G-C-P-X16-X17-K-C-M-N-R-K-C-X18-C-X19-X20-C as set forth in SEQ ID NO: 23:
wherein X1 is selected from the group consisting of T, Q, S, Y and N;
wherein X2 is selected from the group consisting of I, F, V, A, L and W;
wherein X3 is selected from the group consisting of I, T, Y, S, V, A and L;
wherein X4 is selected from the group consisting of K, S, T, Y and R;
wherein X5 is selected from the group consisting of R, T, K, S and Y;
wherein X6 is selected from the group consisting of T, G, S, N, I, K, Q, A, V, L and Y;
wherein X7 is selected from the group consisting of P, S and T;
wherein X8 is selected from the group consisting of R, K and P;
wherein X9 is selected from the group consisting of D, Q, N and E;
wherein X10 is selected from the group consisting of A, Y, I, L, W, S, T, V, L and F;
wherein X11 is selected from the group consisting of D, R, P, K, E, S, T and Y;
wherein X12 is selected from the group consisting of P, H, V, I, L and A;
wherein X13 is selected from the group consisting of R, K, Q and N;
wherein X14 is selected from the group consisting of K, D, A, R, E, V, L and I;
wherein X15 is selected from the group consisting of E, Q, A, L, D, N, V and I;
wherein X16 is selected from the group consisting of Y, N, S, T and Q;
wherein X17 is selected from the group consisting of A, G, V, I and L;
wherein X18 is selected from the group consisting of K and R;
wherein X19 is selected from the group consisting of Y, N, Q, T and S; and
wherein X20 is selected from the group consisting of G, R and K.

### Claim 2 (depends on 1)

The composition of claim 1:
wherein X1 is Thr;
wherein X2 is Ile;
wherein X3 is Ile;
wherein X4 is Lys;
wherein X5 is Thr;
wherein X6 is Ser;
wherein X7 is Pro;
wherein X5 is Lys;
wherein X9 is Gln;
wherein X10 is Leu;
wherein X11 is Pro;
wherein X12 is Pro;
wherein X13 is Lys;
wherein X14 is Ala;
wherein X15 is Gln;
wherein X16 is Tyr;
wherein X17 is Gly;
wherein X18 is Lys;
wherein X19 is Asn; and
wherein X20 is Arg.

### Claim 3 (depends on 1)

A pharmaceutical composition comprising the composition of claim 1 and a pharmaceutically acceptable carrier.

### Claim 4 (depends on 2)

A pharmaceutical composition comprising the composition of claim 2 and a pharmaceutically acceptable carrier.

### Claim 5 (depends on 3)

The composition of claim 3, wherein the composition is formulated for intravenous, subcutaneous, or intramuscular administration.

### Claim 6 (depends on 4)

The composition of claim 4, wherein the composition is formulated for intravenous, subcutaneous, or intramuscular administration.

### Claim 7 (depends on 1)

A method of treating an autoimmune disease in a subject in need thereof, comprising administering the composition of claim 1 to a subject selected as having an autoimmune disease, wherein the autoimmune disease is rheumatoid arthritis, psoriasis, or atopic dermatitis.

### Claim 8 (depends on 2, 7)

The method of claim 7, wherein the composition is the composition of claim 2.

### Claim 9 (depends on 7)

The method of claim 7, wherein administering the composition comprises administering the composition to the subject intravenously, subcutaneously, or intramuscularly.

### Claim 10 (depends on 8)

The method of claim 8, wherein administering the composition comprises administering the composition to the subject intravenously, subcutaneously, or intramuscularly.