Glucose-dependent insulinotropic peptide analogs

摘要

The present invention provides compounds which are analogs of glucose-dependent insulinotropic polypeptide (GIP) and pharmaceutically acceptable salts of such compounds. These compounds have activity as agonists of GIP receptor.

主权项

1. A compound having the formula (I):
(Y)n—R1-Ala-Glu-Gly-Thr-Phe-Ile-Ser-Asp-Tyr-Ser-Ile-Ala-Met-Asp-R2-Ile-His-Gln-Gln-Asp-Phe-Val-Asn-Trp-Leu-Leu-Ala-Gln-R3—NH2  (I) wherein: R1 is selected from the group consisting of: (D)Tyr; DesNH2-Tyr; (D)Phe; DesNH2-Phe; (D)Trp; (D)3Pya; 2-Cl(D)Phe; 3-Cl(D)Phe; 4-Cl(D)Phe; 2-F(D)Phe; 3-F(D)Phe; 3,5 DiF(D)Phe; and 3,4,5TriF(D)Phe; R2 is Lys or Ala; R3 is Lys or PEGylated Lys; Y is acyl; n is 1 when R1 is (D)Tyr; (D)Phe; (D)Trp; (D)3Pya; 2-Cl-(D)Phe; 3-Cl-(D)Phe; 4-Cl-(D)Phe; 2-F-(D)Phe; 3-F-(D)Phe; 3,5-DiF(D)Phe; or 3,4,5-TriF(D)Phe; and n is 0 when R1 is DesNH2-Tyr; (D)Phe or DesNH2-Phe; or a pharmaceutically-acceptable salt thereof.