Modified glp-1 peptides with increased biological potency

Details Modified glp-1 peptides with increased biological potency Modified glp-1 peptides with increased biological potency

C - Chemistry, Metallurgy

07

K

C07K 14/605 (2006.01) A61K 38/26 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2500021

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-IIe-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.

La présente invention concerne un peptide GLP-1 représenté par la formule (I) ou un sel pharmaceutiquement acceptable de ce dernier. Formule (I) : X-His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-IIe-Ala-Trp-Leu-val-Lys-Gly-Arg-Y (SEQ ID NO.1) Dans la formule, X représente une fraction hydrophobe rigidifiante et Y est sélectionné dans le groupe formé de OH, NH¿2? et Gly-OH. La présente invention se rapporte également à des compositions pharmaceutiques renfermant une quantité thérapeutiquement efficace d'un peptide selon la présente invention ou d'un sel pharmaceutiquement acceptable de ce dernier, en association avec au moins un constituant sélectionné entre un support pharmaceutiquement acceptable, un diluant et un excipient.

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