Sultone compound derivatives substituted by nucleophiles, in particular radionuclides, and use thereof for marking macromolecules

摘要

The invention relates to polysultone derivatives used as precursors to radiolabelled macromolecules usable for medicine and in nuclear imaging. The aim of the invention is to provide novel prosthetic compounds or groupings, the synthesis of which is straightforward, easy and automatable, enabling access to economical and effective radiolabelled macromolecules. The aim is achieved by the invention, which involves compounds of formula 10 or 11. Said double-sultone derivatives are produced by opening the sultone rings using a nucleophile radical Ri which may be a radionucleide R* for one of the sultone rings and an active radical peptide Ra for the other sultone ring. The invention also relates to the method for producing the abovementioned compounds, as well as to the drugs or diagnosis products that the latter are capable of forming.

主权项

1. A method of radiolabelling a macromolecule, comprising:
a. providing a compound of general formula 2 in which
R1 to R6 groups, identical or different, correspond to hydrogen or an alkyl, an aryl, an arylalkyl, an alkylaryl, an acyl, or a cycloalkyl;n, m is an integer,the spacer is a divalent structure;Nu1 is a nucleophilic radionuclide R*; and,M1 is a counter-ion; b. opening the sultone moiety of compound 2 with a nucleophilic macromolecule Ra, thereby yielding a radiolabelled macromolecule of the following general formula 3: wherein
Nu1 is the radionuclide;Nu2 is the macromolecule; and,M2 is a counter-ion identical to or different from M1.