| 主权项 |
1. A compound having the formula
R1—X—Z—R2 wherein R1 is H, C1-4 alkyl, acetyl, formyl, benzoyl or trifluoroacetyl; R2 is OH or NH2; X is a peptide which has the formula I:
His-X2-X3-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-X12-Tyr-Leu-Asp-X16-Arg-Arg-Ala-X20-Asp-Phe-Ile-X24-Trp-Leu-X27-X28-X29 (I) wherein X2 is selected from Ser, D-Ser and Aib; X3 is selected from Gln, His and Pro; X12 is selected from Lys and Y X16 is selected from Glu and Y; X20 is selected from Lys and Y; X24 is selected from Glu and Y; X27 is selected from Leu and Y; X28 is selected from Ser and Y or is absent; X29 is Ala or absent; wherein at least one of X12, X16, X17, X20, X27 and X28 is Y; wherein each residue Y is independently selected from Lys, Cys and Orn; wherein the side chain of at least one amino acid residue Y is conjugated to a lipophilic substituent having the formula: (i) Z1, wherein Z1 is a lipophilic moiety conjugated directly to the side chain of Y; or (ii) Z1Z2, wherein Z1 is a lipophilic moiety, Z2 is a spacer, and Z1 is conjugated to the side chain of Y via Z2; and Z is absent or is a sequence of 1-20 amino acid units independently selected from the group consisting of Ala, Leu, Ser, Thr, Tyr, Cys, Glu, Lys, Arg, Dbu, Dpr and Orn; or a pharmaceutically acceptable salt thereof. |
