GLP-1 derivatives

Patent metadata

Field	Value
Publication number	US-9758560-B2
Application number	US-201214343152-A
Country	US
Kind code	B2
Filing date	Sep 6, 2012
Priority date	Sep 6, 2011
Publication date	Sep 12, 2017
Grant date	Sep 12, 2017

Abstract

The invention relates to a derivative of a GLP-1 peptide, which peptide has two Lys residues, namely a first and a second Lys residue, and a maximum of eight amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 3), which derivative comprises two protracting moieties attached to the epsilon amino group of said first and second Lys residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 15: HOOC—(CH2)x-CO—*, and Chem. 16: HOOC—C6H4-O—(CH2)y-CO—*, in which x is an integer in the range of 10-16, and y is an integer in the range of 8-12; and the linker comprises a first linker element *—NH—CH(CH2OH)—CO—*. A preferred linker is g Glu-Ser-Ser-Gly-Ser-Ser-Gly (SEQ ID NO: 2). The derivative of the invention has a very good potency, and a very good binding to the GLP-1 receptor. The invention also relates to the pharmaceutical use of the derivative, for example in the treatment and/or prevention of all forms of diabetes and related diseases.

First claim

The invention claimed is:

1. A compound selected from the following:

or a pharmaceutically acceptable salt, amide, or ester of any of the foregoing compounds.

2. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable excipient.

3. A method for treating diabetes, obesity, binge eating, bulimia nervosa, cardiovascular diseases, gastrointestinal diseases, diabetic complications, critical illness poly-nephropathy (CIPNP), systemic inflammatory response syndrome (SIRS), bacteraemia, septicaemia, septic shock and/or polycystic ovary syndrome; and/or for improving lipid parameters, improving P-cell function, and/or for delaying or preventing diabetic disease progression in a subject in need of such treatment, said method comprising administering to said subject a pharmaceutically active amount of a compound according to claim 1 .

Assignees

• Lau Jesper
• Bloch Paw
• Garibay Patrick William
• Novo Nordisk As

Inventors

• Lau Jesper
• Bloch Paw
• Garibay Patrick William

Classifications

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P5/48

  of the pancreatic hormones · CPC title

• A61P7/00

  Drugs for disorders of the blood or the extracellular fluid · CPC title

• A61P3/06

  Antihyperlipidemics · CPC title