Glucagon analogues as long-acting glp-1/glucagon receptor agonists in the treatment of fatty liver disease and steatohepatitis
AssigneeBoehringer Ingelheim International GmbH
InventorLeo THOMAS
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Abstract
The present invention relates to the medical use of specific long-acting glucagon analogues having dual GLP-1/glucagon receptor agonist activity in the prevention and/or treatment of metabolic liver disease, particularly non-alcoholic fatty liver disease (NAFLD), non-alcoholic fatty liver (NAFL), non-alcoholic steatohepatitis (NASH), NAFLD-associated liver fibrosis and/or cirrhosis.
Claims13
A method for preventing or treating a metabolic liver disease, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I
- R—H—X2-QGTFTSDYSKYL-X15-X16-X17-X18-AKDFI-X24-WLE-X28-A-NH2 (I)
- wherein
- R is selected from H, C1-4 alkyl and acetyl;
- X2 is selected from Aib and Ac4c;
- X15 is selected from Asp and Glu;
- X16 is selected from Glu and ψ;
- X17 is selected from Arg and ψ;
- X18 is selected from Ala and Arg;
- X24 is selected from Glu and ψ;
- X28 is selected from Ser and ψ;
- wherein the compound contains one and only one ψ and wherein said ψ is a residue of Lys, in which the amino group of the side chain is conjugated to a substituent selected from the group consisting of
- HOOC—(CH2)16—(CO)-isoGlu-Peg3-Peg3-, and
- HOOC—(CH2)16—(CO)-isoGlu-GSGSGG-.
A method of preventing or treating a metabolic liver disease, the method comprising administering to a patient in need thereof a pharmaceutical composition comprising a compound of formula I
- R—H—X2-QGTFTSDYSKYL-X15-X16-X17-X18-AKDFI-X24-WLE-X28-A-NH22 (I)
- wherein
- R is selected from H, C1-4 alkyl and acetyl;
- X2 is selected from Aib and Ac4c;
- X15 is selected from Asp and Glu;
- X16 is selected from Glu and ψ;
- X17 is selected from Arg and ψ;
- X18 is selected from Ala and Arg;
- X24 is selected from Glu and ψ;
- X28 is selected from Ser and ψ;
- wherein the compound contains one and only one ψ and wherein said ψ is a residue of Lys, in which the amino group of the side chain is conjugated to a substituent selected from the group consisting of
- HOOC—(CH2)16—(CO)-isoGlu-Peg3-Peg3-, and
- HOOC—(CH2)16—(CO)-isoGlu-GSGSGG-.
Dependencies are inferred from the claim text.