Dual GLP-1/glucagon receptor agonists derived from exendin-4
First Claim
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1. A peptidic compound having the formula (I):
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H2N-His-X2-X3-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-X14-X15-Glu-Glu-Ala-X19-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Aib-X28-X29-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-R1
(I)or a salt or solvate thereof,whereinX2 is an amino acid residue selected from the group consisting of D-Ser and Ser,X3 is an amino acid residue selected from the group consisting of Gin and His,X14 is an amino acid residue with a functionalized —
NH2 side chain group selected from the group consisting of Lys, Orn, Dab, and Dap, wherein the —
NH2 side chain group is functionalized by —
Z—
C(O)—
R5, whereinZ is a linker comprising 1-5 amino acid linker groups selected from the group consisting of γ
-glutamate (γ
E) and AEEAc and combinations thereof in all stereoisomeric forms,R5 is a moiety comprising up to 50 carbon atoms and heteroatoms selected from the group consisting of N and O,X15 is an amino acid residue selected from the group consisting of Glu and Asp,X19 is an amino acid residue selected from the group consisting of Ala and Val,X28 is an amino acid residue selected from the group consisting of Ala, Lys, and Ser,X29 is an amino acid residue selected from the group consisting of Thr, D-Ala, and Gly, andR1 is NH2 or OH.
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Abstract
The present invention relates to dual GLP-1/glucagon receptor agonists and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as for reduction of excess food intake.
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Citations
34 Claims
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1. A peptidic compound having the formula (I):
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H2N-His-X2-X3-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-X14-X15-Glu-Glu-Ala-X19-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Aib-X28-X29-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-R1
(I)or a salt or solvate thereof, wherein X2 is an amino acid residue selected from the group consisting of D-Ser and Ser, X3 is an amino acid residue selected from the group consisting of Gin and His, X14 is an amino acid residue with a functionalized —
NH2 side chain group selected from the group consisting of Lys, Orn, Dab, and Dap, wherein the —
NH2 side chain group is functionalized by —
Z—
C(O)—
R5, whereinZ is a linker comprising 1-5 amino acid linker groups selected from the group consisting of γ
-glutamate (γ
E) and AEEAc and combinations thereof in all stereoisomeric forms,R5 is a moiety comprising up to 50 carbon atoms and heteroatoms selected from the group consisting of N and O, X15 is an amino acid residue selected from the group consisting of Glu and Asp, X19 is an amino acid residue selected from the group consisting of Ala and Val, X28 is an amino acid residue selected from the group consisting of Ala, Lys, and Ser, X29 is an amino acid residue selected from the group consisting of Thr, D-Ala, and Gly, and R1 is NH2 or OH. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34)
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Specification