US 7,067,488 B2 · Modified GLP-1 peptides with increased biological potency

Abstract

The present invention relates to a GLP-1 peptide having the following formula, or a pharmaceutically acceptable salt thereof: X-His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-lle-Ala-Trp-Leu-val-Lys-Gly-Arg-Y (SEQ ID NO. 1) wherein X is a rigidifying hydrophobic moiety and wherein Y is selected from the group consisting of OH, NH2 and Gly-OH. Moreover, the present invention relates to pharmaceutical compositions comprising a therapeutically effective amount of a peptide of the present invention, or a pharmaceutically acceptable salt thereof, in association with at least one constituent selected from a pharmaceutically acceptable carrier, diluent, and excipient.

Claims23

Dependent claims

A GLP-1 peptide having the following formula, or a pharmaceutically acceptable salt thereof:

X-His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg-Y (SEQ ID NO.1)
wherein:
X is a rigidifying hydrophobic acyl moiety as obtained from the corresponding carboxylic acid of general structure I:
wherein R1 is 2- or 3-lower alkoxy, 2- or 3-hydroxy, 2- or 3- amino, 2-N-phenylamino, 2,6-dihalo or 2,3,4,5,6-pentahalo and n=0 or 1, and Y is selected from the group consisting of OH, NH2 and Gly-OH.

1 more element

Dependencies are inferred from the claim text.

Modified GLP-1 peptides with increased biological potency

Life of this patent

Modified GLP-1 peptides with increased biological potency

Life of this patent

Abstract

Claims23