# US 10,766,940 B2 · Brain penetrant amylin receptor based peptides for Alzheimer's disease

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- Number: US 10,766,940 B2
- Document ID: US10766940B2
- Status: Granted
- Kind: B2
- Application number: 15/705,789
- Filed: 2017-09-15
- Published: 2018-05-17
- Granted: 2020-09-08
- Earliest claimed: 2016-09-19
- Assignees: The Governors of the University of Alberta
- Applicants: The Governors of the University of Alberta
- Inventors: Jack Jhamandas; Rania Soudy; Kamaljit Kaur; Wen Fu; David MacTavish; Aarti Patel
- Web page: https://patentgrep.com/patent/US10766940B2

## CPC

- C07K 14/575: Hormones (derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin C07K14/665, e.g. corticotropin C07K14/695)
- 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
- C07K 14/585: Calcitonins
- 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)
- 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)

## Abstract

Amylin receptor antagonists capable of binding to the amylin receptor and inhibiting activity of amylin or amyloid-beta protein are provided. The amylin receptor antagonists can be administered in the form of pharmaceutical compositions or the like. Methods for preparing and using the amylin receptor antagonists for treating, preventing, or ameliorating Alzheimer's disease are also provided.

## Claims

### Claim 1

An amylin receptor antagonist selected from the group consisting of cyclic AC253 having the amino acid sequence of SEQ ID NO: 2 and a peptide fragment of AC253 consisting of an amino acid sequence selected from the group consisting of SEQ ID NO: 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16, wherein the amylin receptor antagonist is brain penetrant and capable of binding to an amylin receptor and inhibiting activity of amylin, amyloid-beta protein, or both.

### Claim 2 (depends on 1)

The amylin receptor antagonist of claim 1, wherein the amylin receptor antagonist is the peptide fragment and the amino acid sequence is SEQ ID NO: 7, and wherein the amylin receptor antagonist is capable of binding to amylin subtype 1 (AMY1) and amylin subtype 3 (AMY3) receptors.

### Claim 3 (depends on 1)

The amylin receptor antagonist of claim 1, wherein the amylin receptor antagonist is the peptide fragment and the amino acid sequence is SEQ ID NO: 12, and wherein the amylin receptor antagonist is capable of binding to AMY1 receptor.

### Claim 4 (depends on 1)

The amylin receptor antagonist of claim 1, wherein the amylin receptor antagonist is the peptide fragment and the amino acid sequence is SEQ ID NO: 16, and wherein the amylin receptor antagonist is capable of binding to AMY1 and AMY3 receptors.

### Claim 5 (depends on 1)

A composition or pharmaceutical composition comprising the amylin receptor antagonist of claim 1, and a pharmaceutically acceptable carrier.