Amylin and calcitonin receptor agonist

Patent metadata

Field	Value
Publication number	US-9593149-B2
Application number	US-201615151093-A
Country	US
Kind code	B2
Filing date	May 10, 2016
Priority date	Sep 4, 2014
Publication date	Mar 14, 2017
Grant date	Mar 14, 2017

Abstract

The present invention relates to peptides comprising an amino acid sequence SEQ ID NO: 1 (EASELSTAALGRLSAELHELATLPRTETGPESP), analogs and derivatives thereof and pharmaceutical compositions comprising such peptides and derivatives. This invention further regards the use of these peptides according to SEQ ID NO: 1, analogs and derivatives thereof as medicaments.

First claim

The invention claimed is:

1. A peptide comprising the amino acid sequence of EASELSTAALGRLSAELHELATLPRTETGPESP (SEQ ID NO:1).

2. The peptide according to claim 1 , comprising a C-terminal amide group.

3. A derivative of the peptide according to claim 1 , wherein said derivative comprises a side chain covalently attached to the peptide at its N-terminal and wherein said side chain comprises fatty acid or fatty diacid.

4. The derivative according to claim 3 , wherein said fatty acid or fatty diacid comprises between 14 to 20 carbon atoms.

5. The derivative according to claim 3 , wherein said side chain further comprises a linker.

6. The derivative according to claim 5 , wherein said linker is selected from the group consisting of gGlu, gGlu-OEG, gGlu-OEG-OEG, gGlu-OEG-OEG-OEG, gGlu-OEG-OEG-OEG-OEG, and gGlu-OEG-OEG-OEG-OEG-OEG.

7. A derivative of the peptide according to claim 2 , wherein said derivative comprises a side chain covalently attached to the peptide at its N-terminal and wherein said side chain comprises fatty acid or fatty diacid.

8. The derivative according to claim 7 , wherein said fatty acid or fatty diacid comprises between 14 to 20 carbon atoms.

9. The derivative according to claim 7 , wherein said side chain further comprises a linker.

10. The derivative according to claim 9 , wherein said linker is selected from the group consisting of gGlu, gGlu-OEG, gGlu-OEG-OEG, gGlu-OEG-OEG-OEG, gGlu-OEG-OEG-OEG-OEG, and gGlu-OEG-OEG-OEG-OEG-OEG.

11. A compound which is

12. A pharmaceutical composition comprising the compound of claim 11 and a pharmaceutically acceptable excipient.

13. A method of reducing food intake comprising administering a pharmaceutically effective amount of the compound of claim 11 to a subject in need thereof.

14. A method of treating overweight comprising administering a pharmaceutically effective amount of the compound of claim 11 to a subject in need thereof.

15. A method of treating obesity comprising administering a pharmaceutically effective amount of the compound of claim 11 to a subject in need thereof.

Assignees

• Novo Nordisk As

Inventors

• Kruse Thomas
• Schaeffer Lauge
• Dahl Kirsten
• Raun Kirsten

Classifications

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P3/04

  Anorexiants; Antiobesity agents · CPC title

• A61P25/02

  for peripheral neuropathies · 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