Cyclopentapeptide derivatives and uses thereof

摘要

The present invention, among others, relates to a compound having a structure according to formula (I) or a pharmaceutically acceptable salt thereof, wherein Xaa1 to Xaa4 are independently of each other, an optionally N-alkylated natural or unnatural amino acid, R is H or methyl, L is a linker moiety, Ar is a spacer comprising an aromatic moiety, and D comprises, preferably is i) a combination of an organic complexation agent and a detectable label; or ii) a detectable label, an organic complexation agent or an active substance, said active substance particularly being selected from cytotoxic agents, lipids, sugars, sugar conjugates, sugar derivatives, proteins and combinations thereof, with the proviso that -L-Ar-D does not comprise a 18F-benzoyl residue.

主权项

1. A compound having a structure according to formula I or a pharmaceutically acceptable salt thereof, wherein Xaa1 is D-tyrosine, Xaa2 is arginine, Xaa3 is naphthylalanine (Nal) and Xaa4 is glycine, R is methyl, L has the formula —(CH2)3—NH—, and Ar is selected from the group consisting of and D is
i) DOTA,ii) a combination of a Ga atom and DOTA, oriii) a combination of a Ga atom and DOTA, with the complexation agent DOTA being covalently bound to Ar.