Lipopeptides for use in treating liver diseases and cardiovascular diseases

Patent metadata

Field	Value
Publication number	US-10967044-B2
Application number	US-201916270293-A
Country	US
Kind code	B2
Filing date	Feb 7, 2019
Priority date	Nov 12, 2012
Publication date	Apr 6, 2021
Grant date	Apr 6, 2021

Abstract

The present invention relates to lipopeptide-based compounds for use in the diagnosis, prevention and/or treatment of a liver disease or condition, preferably liver involved metabolic diseases, as well as in the control or modification of the cholesterol level or cholesterol uptake and, thus, diagnosis, prevention and/or treatment of a cardiovascular disease. The present invention furthermore relates to an in vitro or in vivo assay or method for testing or measuring the NTCP-mediated transport of test compound(s). The present invention furthermore relates to a method for the diagnosis, prevention and/or treatment of a liver disease or condition, comprising administering a therapeutically effective amount of a lipopeptide-based compound to a patient. The present invention furthermore relates to a method for the diagnosis, prevention and/or treatment of a cardiovascular disease.

First claim

The invention claimed is:

1. A method for the treatment of a cardiovascular disease (CVD) in a patient comprising administering a therapeutically effective amount of a lipopeptide to the patient, wherein the lipopeptide comprises a peptide of the general formula
X−P−Y−R 0
wherein
P is the amino acid sequence NPLGFXaaP (SEQ. ID NO: 1),
wherein Xaa is an arbitrary amino acid;

X is an amino acid sequence having a length of m amino acids,
wherein m is at least 4;

Y is an amino sequence having a length of n amino acids,
wherein n is 0 or at least 1;

and wherein m+n>11;
R is a C-terminal modification of said hydrophobic modified peptide, and
o is 0 or at least 1.

2. The method of claim 1 , comprising control or modification of cholesterol level or cholesterol uptake,
wherein the cholesterol level or uptake is controlled or modified by decreasing or blocking the NCTP-mediated bile salt transport by the lipopetide.

3. The method of claim 1 , wherein the route of administration is selected from subcutaneous, intravenous, oral, nasal, intramuscular, transdermal, inhalative, and by suppository.

4. The method of claim 1 , wherein the lipopeptide comprises an N-terminal hydrophobic modification.

5. The method of claim 1 , wherein the lipopetide comprises an amino acid sequence selected from SEQ ID NOs: 2 to 14 and 18 to 20.

Assignees

• Univ Heidelberg Ruprecht Karls
• Cleeves Volker

Inventors

• Cleeves Volker
• Urban Stephan
• Kubitz Ralf

Classifications

• G01N2800/085

  Liver diseases, e.g. portal hypertension, fibrosis, cirrhosis, bilirubin · CPC title

• A61K38/162 Primary

  from virus · CPC title

• G01N33/5067

  Liver cells · CPC title

• G01N33/92

  involving lipids, e.g. cholesterol {, lipoproteins, or their receptors (steroid hormones G01N33/743)} · CPC title

• G01N33/6893

  related to diseases not provided for elsewhere · CPC title