发明名称 Exendin-4 Derivatives
摘要 The present invention relates to exendin-4 derivatives and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as reduction of excess food intake.
申请公布号 US2014206608(A1) 申请公布日期 2014.07.24
申请号 US201314135756 申请日期 2013.12.20
申请人 Sanofi 发明人 Haack Torsten;Wagner Michael;Henkel Bernd;Stengelin Siegfried;Evers Andreas;Lorenz Martin;Lorenz Katrin
分类号 C07K14/605;A61K45/06;A61K38/28;A61K38/26 主分类号 C07K14/605
代理机构 代理人
主权项 1. A peptidic compound having the formula (I): R1—Z—R2  (I) wherein 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 X18 X19 X20 X21-Phe-Ile-Glu-Trp-Leu-Lys-X28-X29-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-X40 (II) X3 represents an amino acid residue selected from Gln, Glu and His, X12 represents an amino acid residue selected from Ile and Lys, X14 represents an amino acid residue having a side chain with an —NH2 group, wherein the —NH2 side chain group is functionalized by —C(O)—R5, wherein R5 may 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, Ile, Gln, Leu, Aib, Tyr and Ala, X18 represents an amino acid residue selected from Ala, Arg, Aib, Leu, Lys and Tyr, X19 represents an amino acid residue selected from Ala, Gln, Val and Aib, X20 represents an amino acid residue selected from Gln, Aib, Phe, Arg, Leu, Lys and His, X21 represents an amino acid residue selected from Asp, Glu, Tyr, and Leu, X28 represents an amino acid residue selected from Asn, Ala, Aib, Arg and Lys, X29 represents an amino acid residue selected from Gly, Thr, Aib, D-Ala and Ala, X40 is either absent or represents Lys, R1 represents NH2, R2 represents the C-terminal group of the peptidic compound and is selected from OH and NH2, or a salt or solvate thereof.
地址 Paris FR