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Derivatives of exendin-4 as dual agonists of GLP1 / GIP or trigonal of GLP1 / GIP / glucagon
专利权人:
SANOFI
发明人:
HAACK, Torsten,WAGNER, Michael,HENKEL, Bernd,STENGELIN, Siegfried,EVERS, Andreas,LORENZ, Martin,LORENZ, Katrin
申请号:
ES13810958
公开号:
ES2688367T3
申请日:
2013.12.19
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A peptide compound having the formula (I): R1-Z-R2 (I) in which Z is a peptide moiety having the formula (II) Tyr-Aib-X3-Gly-Thr-Phe-Thr-Ser -Asp-Leu-Ser-X12-Gln-X14-X15-X16-X17-5 X18-X19-X20-X21-Phe- Ile-Glu-Trp-Leu-Lys-X28-X29-Gly-Pro-Ser- Ser-Gly-Ala-Pro-Pro-Ser-X (II) X3 represents Glu, X12 represents an amino acid residue selected from Ile and Lys, X14 represents an amino acid residue having a side chain with a -NH2 group , in which the side chain group -NH2 is functionalized by -C (O) -R5, in which R5 can be a moiety comprising up to 50 or up to 100 carbon atoms and optionally heteroatoms selected from halogen, N, O , S and / or P, X15 represents an amino acid residue selected from Asp and Glu X16 represents an amino acid residue selected from Ser, Lys, Glu and Gln, X17 represents an amino acid residue selected from Arg, Lys, Glu, Gln, Leu, Aib, Tyr and Ala, X18 represents an amino acid residue selected from Ala and Arg, X19 represents an amino acid residue selected from Ala and Val, X20 represents an amino acid residue selected from Gln, Aib, Lys and His, X21 represents an amino acid residue selected from Asp, Glu and Leu, X28 represents an amino acid residue selected from Asn and Ala, X29 represents an amino acid residue selected from Gly, Thr and D-Ala, X40 is either absent or represents Lys, R1 represents NH2, R2 represents the C-terminus group of the peptide compound and is selected from OH and NH2, or a salt or solvate thereof, wherein the compound is a GLP-1 and GIP receptor agonist.Un compuesto peptídico que tiene la fórmula (I): R1-Z-R2 (I) en la que Z es un resto de péptido que tiene la fórmula (II) Tyr-Aib-X3-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-X12-Gln-X14-X15-X16-X17-5 X18-X19-X20-X21-Phe- Ile-Glu-Trp-Leu-Lys-X28-X29-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-X(II) X3 representa Glu, X12 representa un resto de aminoácido seleccionado de Ile y Lys, X14 representa un resto de aminoácido que tiene una cadena lateral con un grupo -NH2, en el que el grupo de c
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