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US 2019/0338009 A1Published application
Glp-1/glp-2 dual agonists
AssigneeZealand Pharma A/S
InventorsBjarne Due LARSEN, Lise GIEHM, Alistair Vincent Gordon EDWARDS
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Abstract
The invention relates to compounds having agonist activity at the GLP-1 (glucagon-like-peptide 1) and GLP-2 (glucagon-like peptide 2) receptors. The compounds find use, inter alia, in the prophylaxis or treatment of intestinal damage and dysfunction, regulation of body weight, and prophylaxis or treatment of metabolic dysfunction.
Claims26
A GLP-1/GLP-2 dual agonist represented by the formula:
- R1—X*—U—R2
- wherein:
- R1 is hydrogen (Hy), C1-4 alkyl, acetyl, formyl, benzoyl or trifluoroacetyl;
- R2 is NH2 or OH;
- X* is a peptide of formula I:
- (I)
- (SEQ ID NO:
- 3)
- H-X2-EG-X5-F-X7-X8-E-X10-X11-TIL-X15-X16-X17-A-X19-
- X20-X21-FI-X24-WL-X27-X28-X29-KIT-X33
- wherein
- X2 is Aib or G;
- X5 is S or T;
- X7 is S or T;
- X8 is S, E or D;
- X10 is L, M or V;
- X11 is A, N or S;
- X15 is D or E
- X16 is E, A or G;
- X17 is Q, E, L or K;
- X19 is A, V or S;
- X20 is R or K;
- X21 is D, L or E;
- X24 is A, N or S;
- X27 is I, Y, Q, H or K;
- X28 is A, E, H, Y, L, K, Q, R or S;
- X29 is H, Y, K or Q;
- X33 is D or E;
- U is absent or a sequence of 1-15 residues, each independently selected from K and k;
- and wherein at least one of X5 and X7 is T;
- or a pharmaceutically acceptable salt thereof.
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Dependencies are inferred from the claim text.