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US 2017/0281709 A1Published application
Peptide conjugates of glp-1 receptor agonists and gastrin and their use
AssigneeZealand Pharma A/S
InventorsTrine Skovlund Ryge NEERUP, Torben ØSTERLUND, Jakob Lind TOLBORG, Keld FOSGERAU, Ulrika MARTENSSON, Marianne BRORSON, Kamilla ROLSTED
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Abstract
The present invention relates, inter alia, to certain peptide conjugates, and to the use of the conjugates in the treatment of a variety of diseases or disorders, including diabetes (type 1 and/or type 2) and diabetes related diseases or disorders.
Claims33
A peptide conjugate or pharmaceutically acceptable salt thereof having the formula I
- R1—Z-L-Y—R2 (I)
- wherein
- R1 is H, C1-4 alkyl, acetyl, formyl, benzoyl or trifluoroacetyl;
- R2 is OH or NH2;
- Z comprises the sequence of Exendin-4(1-39) having the sequence
- 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-Pro-Ser
- or an analogue thereof Za, wherein Za has substitutions in up to 10 positions, and/or comprises a C-terminal truncation of 1 to 12 amino acids, with respect to the sequence of Exendin-4;
- L is an optional linker moiety;
- and
- Y comprises the sequence of Gastrin17 having the sequence
- Gln-Gly-Pro-Trp-Leu-Glu-Glu-Glu-Glu-Glu-Ala-Tyr-Gly-Trp-Y15-Asp-Phe
- wherein Y15 is selected from Leu, Nle, Phe and Thr
- or an analogue thereof Ya, wherein Ya has substitutions in up to 5 positions with respect to the sequence of Gastrin17.
13 more elements
(canceled)
4-6. (canceled)
15-29. (canceled)
Dependencies are inferred from the claim text.