Brain penetrant amylin receptor based peptides for Alzheimer's disease

Patent metadata

Field	Value
Publication number	US-10766940-B2
Application number	US-201715705789-A
Country	US
Kind code	B2
Filing date	Sep 15, 2017
Priority date	Sep 19, 2016
Publication date	Sep 8, 2020
Grant date	Sep 8, 2020

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.

First claim

What is claimed is:

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.

2. 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.

3. 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.

4. 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.

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

Assignees

• Univ Alberta

Inventors

• Jhamandas Jack
• Soudy Rania
• Kaur Kamaljit
• Fu Wen
• Mactavish David
• Patel Aarti

Classifications

• A61P25/28 Primary

  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 · CPC title

• C07K14/585

  Calcitonins · CPC title

• A61K38/00

  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) · CPC title

• C07K14/575 Primary

  Hormones (derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin C07K14/665, e.g. corticotropin C07K14/695) · CPC title