Prochelator for the preparation of radiometal labeled molecules having improved biological properties

摘要

Chelating compounds for labeling bioactive molecules with a radiometal, having general formula (I) in which: both Y groups may be positioned either trans as shown or cis; A is an effector molecule, such as a peptide, in particular octreotide, CCK, substance P, gastrine, a protein, in particular an antibody or enzyme, sugars or radiosensitizing agents, like doxorubicin; R is a hydrogen, a C₁-C₃ alkyl or a alcohol; X is a spacer, in particular (CH₂)_n—X′, in which n is 1-10 and X′ is COOH, NH₂, SH, OH or O-halogen, in which halogen is in particular Br, I or Cl, or a molecule of the formula (a) or of the formula (b), Y is COO—, CH₂CONH₂, CH₂CH₂OH, optionally complexed with a radiometal.