CAGE AMINE LIGANDS FOR METALLO-RADIOPHARMACEUTICALS

摘要

The present invention relates to compounds that are useful as metal ligands and which can be bound to a biological entity such as a molecular recognition moiety and methods of making these compounds. Once the compounds that are bound to a biological entity are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.

主权项

1. A method of functionalising a compound of the formula (1) or a metal complex thereof: wherein Lig is a nitrogen containing macrocyclic metal ligand; L is a bond or a linking moiety; to modify its ability to bind to a biological entity the method comprising;(a) converting the compound of formula (1) or a metal complex thereof to a compound of formula (II) or a metal complex thereof wherein L1 is a spacer group;(b) converting the compound of formula (2) or a metal complex thereof to a compound of formula (3) or a metal complex thereof wherein R is a moiety capable of binding to a biological entity or a protected form thereof or a synthon thereof.