Peptide conjugates of GLP-1 receptor agonists and gastrin and their use

Patent metadata

Field	Value
Publication number	US-10406207-B2
Application number	US-201615381993-A
Country	US
Kind code	B2
Filing date	Dec 16, 2016
Priority date	Apr 27, 2010
Publication date	Sep 10, 2019
Grant date	Sep 10, 2019

Abstract

The present invention relates, inter alia, to certain peptide conjugates, and to the use of the conjugates in the treatment of a variety of diseases or disorders, including diabetes (type 1 and/or type 2) and diabetes related diseases or disorders.

First claim

The invention claimed is:

1. A peptide conjugate or pharmaceutically acceptable salt thereof, wherein the peptide conjugate has the sequence:
Exendin-4(1-39)-Peg3-Peg3-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 1)
Exendin-4(1-39)-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 2)
Exendin-4(1-39)-K-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 3)
Exendin-4(1-39)-AAA-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 4)
Exendin-4(1-39)-SKK-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 5)
Exendin-4(1-39)-Peg3-SKK-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 6)
Exendin-4(1-39)-8Aoc-SKK-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 7)
Exendin-4(1-39)-DBF-SKK-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 8)
Exendin-4(1-39)-8Aoc-8Aoc-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 9)
Exendin-4(1-28-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 19)
Exendin-4(1-28)-K-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 20)
Exendin-4(1-28)-AAA-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 21)
Exendin-4(1-28)-SKK-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 22)
Exendin-4(1-28)-Peg3-SKK-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 23)
Exendin-4(1-28)-Peg3-Peg3-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 24)
Exendin-4(1-28)-8Aoc-SKK-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 25)
Exendin-4(1-28)-DBF-SKK-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 26)
Exendin-4(1-28)-8Aoc-8Aoc-[Gln1,Leu15]Gastrin17, (SEQ ID NO: 27).

2. A pharmaceutical composition comprising a peptide conjugate, or pharmaceutically acceptable salt thereof, according to claim 1 , in combination with one or more peptide conjugates or pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable carrier, excipient or vehicle.

3. A device comprising at least one peptide conjugate, or pharmaceutically acceptable salt thereof, according to claim 1 , for delivery of the peptide conjugate to a subject.

4. A kit comprising at least one peptide conjugate, or pharmaceutically acceptable salt thereof, according to claim 1 , further comprising packaging or instructions for use.

Assignees

• Zealand Pharma As

Inventors

• Neerup Trine Skovlund Ryge
• Østerlund Torben
• Tolborg Jakob Lind
• Fosgerau Keld
• Martensson Ulrika
• Brorson Marianne
• Rolsted Kamilla

Classifications

• A61P43/00

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

• A61P9/14

  Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers · CPC title

• A61P9/12

  Antihypertensives · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title