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Generated: August 18, 2017

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Title: Peptide agonists of GLP-1 activity
Abstract:The present invention relates to novel peptide conjugates which have increased stability and are useful in the treatment of excess levels of blood glucose.
Inventor(s): Larsen; Bjarne Due (Br.o slashed.nsh.o slashed.j, DK), Mikkelsen; Jens Damsgaard (Lyngby, DK), Neve; S.o slashed.ren (Lyngby, DK)
Assignee: Zealand Pharma A/S (Glostrup, DK)
Filing Date:Jul 12, 2000
Application Number:09/614,847
Claims:1. A peptide consisting of any one of the following sequences: a) H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala- Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro -Ser-(Lys).sub.6 -NH.sub.2 (des-Pro.sup.36 -exendin-4(1-39)-Lys.sub.6 -NH.sub.2) (SEQ ID NO:93), b) H-Lys.sub.6 -His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-V al-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro- Ser-(Lys).sub.6 -NH.sub.2 (H-Lys.sub.6 -des Pro.sup.36 exendin-4(1-39)-Lys.sub.6 -NH.sub.2) (SEQ ID NO: 149), c) H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala- Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala -Ser-NH.sub.2 (H-des Pro.sup.36,Pro.sup.37,Pro.sup.38 exendin-4(1-39)-NH.sub.2) (SEQ ID NO: 132), d) H-Lys-Lys-Lys-Lys-Lys-Lys-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys- Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro -Ser-Ser-Gly-Ala-Ser-NH.sub.2 (H-(Lys).sub.6 -des Pro.sup.36,Pro.sup.37,Pro.sup.38 exendin-4(1-39)-NH.sub.2), (SEQ ID NO: 134), e) H-Asn-Glu-Glu-Glu-Glu-Glu-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys- Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro -Ser-Ser-Gly-Ala-Ser-NH.sub.2 (H-Asn-(Glu).sub.5 -des Pro.sup.36,Pro.sup.37, Pro.sup.38 exendin-4(1-39)-NH.sup.2) (SEQ ID NO: 137), f) H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala- Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Ser-(Ly s).sub.6 -NH.sub.2 (des Pro.sup.36, Pro.sup.37,Pro.sup.38 exendin-4(1-39)-(Lys).sub.6 -NH.sub.2) (SEQ ID NO: 133), g) H-(Lys).sub.6 -His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-V al-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Ser-(Lys ).sub.6 -NH.sub.2 (H-(Lys).sub.6 -des Pro.sup.36,Pro.sup.37,Pro.sup.38 exendin-4(1-39)-(Lys).sub.6 -NH.sub.2) (SEQ ID NO: 135), h) H-Asp-Glu-Glu-Glu-Glu-Glu-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys- Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro -Ser-Ser-Gly-Ala-Ser-(Lys).sub.6 -NH.sub.2 (H-Asn-(Glu).sub.5 -des Pro.sup.36,Pro.sup.37,Pro.sup.38 exendin-4(1-39)-(Lys).sub.6 -NH.sub.2) (SEQ ID NO: 136); or a pharmaceutically acceptable salt thereof.

2. A composition comprising the peptide of claim 1 and a physiologically acceptable carrier.
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