Minigastrin derivatives, particularly for use in the diagnosis and / or treatment of CCK2 receptor positive tumors

摘要

Accordingly, it is an object of the present invention to provide a minigastrin derivative that further improves accumulation in CCK-2 receptor positive tumors and at the same time has very low accumulation in other organs, such as the kidneys. This object is achieved according to the invention by means of a minigastrin derivative having the formula: XZ-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH ₂ (Y), wherein the amino acids of the sequences Z, Ala, Tyr, Gly, Trp, Met, Asp, Phe and NH ₂ or Y (C- Terminal), at least one of the before or after linking or terminal amide bond is replaced by 1,4-disubstituted or 1,5-disubstituted 1,2,3-triazole, and X is a diagnosis of CCK-2 receptor related disease And / or amides and esters derived from linear or branched alkyl-, alkenyl-, alkynyl-, aromatic- and heterocyclic alcohols, wherein Y represents a chemical group attached to the peptide for therapeutic intervention purposes. C-terminal modifications of non-limiting peptides, such as amides, primary and secondary amides, free carboxylic acids and carboxylic ester derivatives, Z represents a linker or DGlu *, where DGlu * is 1 to 6 Represents a chain of DGlu (-DGlu- to -DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-) with repeats. These minigastrin derivatives have high specific internalization, good IC ₅₀ values and sufficient plasma stability.