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US 2013/0157935 A1Published application
Glucagon analogues
AssigneeZealand Pharma A/S
InventorsEddi Meier, Ditte Riber, Jens Rosengren Daugaard, Marie Skovgaard
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Abstract
The invention provides materials and methods for promoting weight loss or preventing weight gain without affecting glycemic control. In particular, the invention provides novel glucagon analogue peptides effective in such methods. The peptides may mediate their effect by having increased selectivity for the GLP-1 receptor as compared to human glucagon.
Claims27
A compound having the formula
- R1—X—Z—R2.
- wherein
- R1 is H, C1-4 alkyl, acetyl, formyl, benzoyl or trifluoroacetyl;
- R2 is OH or NH2;
- X is a peptide which has the formula I:
- (SEQ ID NO:
- 11)
- His-X2-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Lys-
- Tyr-Leu-Asp-X16-X17-Arg-Ala-X20-Asp-Phe-Ile-Glu-
- Trp-Leu-X27-X28-X29 (I)
- wherein
- X2 is selected from Ser and Aib;
- X16 is selected from Glu and Y;
- X17 is selected from Arg and Y;
- X20 is selected from Lys and Y;
- X27 is selected from Leu and Y;
- X28 is selected from Ser and Y or absent;
- X29 is Ala or absent;
- wherein at least one of X16, X17, X20, X27 and X28 is Y;
- wherein each residue Y is independently selected from Lys, Cys and Orn;
- wherein the side chain of at least one amino acid residue Y of X is conjugated to a lipophilic substituent having the formula:
- (i) Z1, wherein Z1 is a lipophilic moiety conjugated directly to the side chain of Y;
- or
- (ii) Z1Z2, wherein Z1 is a lipophilic moiety, Z2 is a spacer, and Z1 is conjugated to the side chain of Y via Z2;
- and Z is absent or is a sequence of 1-20 amino acid units independently selected from the group consisting of Ala, Leu, Ser, Thr, Tyr, Cys, Glu, Lys, Arg, Dbu, Dpr and Orn;
- or a pharmaceutically acceptable salt thereof.
23 more elements
(canceled)
Dependencies are inferred from the claim text.