Advanced Accelerator Applications Sa

Advanced Accelerator Applications

Cedric Bouteiller

Anthony Romieu

Pierre-Yves Renard

Thomas Priem

Davide Camporese

Nucleophile-reactive sulfonated compounds used as precursors to (radio)labelled (bio)molecules are produced by pre-introduction of a nucleophilic compound R* through an unusual nucleophile-induced ring-opening reaction of the sultone moiety of the precursor. The precursors and compounds conform to respective formulae (Ip) and (I): Also disclosed are methods for producing these precursors and compounds, as well as for conjugation of these compounds with (bio)molecules, and to the drugs obtained by this method.

Nucleophile-reactive sulfonated compounds for the (radio)labelling of (bio)molecules; precursors and conjugates thereof

Nucleophile-reactive sulfonated compounds for the (radio)labelling of (bio) molecules; precursors and conjugates thereof

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 Rwhich may be a radionucleide R* for one of the sultone rings and an active radical peptide Rfor 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.

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

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Vulbens, France

Cedric Bouteiller