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US 10,519,211 B2Granted
Compounds as peptidic GLP1/glucagon/GIP receptor agonists
AssigneeSanofi
InventorsMartin Bossart, Andreas Evers, Torsten Haack, Katrin Lorenz, Dieter Kadereit, Michael Wagner, Stefania Pfeiffer-Marek, Martin Lorenz
Life of this patent
Estimating the term…
Abstract
The present invention relates to trigonal GLP-1/glucagon/GIP 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.
Claims30
A compound of the formula I:
- I
- H2N-His-Aib-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-
- Lys-Leu-X14-Glu-X16-Gln-Arg-Gln-Aib-Glu-Phe-Ile-
- Glu-Trp-Leu-Lys-Ala-X29-Gly-X31-Pro-Ser-Aib-Lys-
- Pro-Pro-Pro-Lys-R1
- wherein:
- 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, wherein
- Z is a linker having a length of 1-5 amino acid linker groups, wherein the amino acid linker groups are selected from the group consisting of gamma-Glutamate (gGlu), gAAA (gamma-amino adipic acid) and AEEAc ((2-(2-aminoethoxy)ethoxy)acetyl) and combinations thereof in all stereoisomeric forms;
- and
- R5 is a moiety comprising up to 50 carbon atoms and heteroatoms selected from N and O;
- X16 is an amino acid residue selected from Glu and Lys;
- X29 is an amino acid residue selected from D-Ala and Gly;
- X31 is an amino acid residue selected from His and Pro;
- and
- R1 is NH2 or OH;
- or a salt or solvate thereof.
13 more elements
Dependencies are inferred from the claim text.