Bifunctional do2pa derivatives, chelates with metallic cations and use thereof
AssigneesCentre National de la Recherche Scientifique (CNRS), Universite De Bretagne Occidentale
InventorsFatima Oukhatar, Maryline Beyler, Raphaël Tripier
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Abstract
Disclosed are chelates resulting from the complexation of bifunctional do2pa derivatives ligands of formula (I), wherein the substituents R1, R1′, R2, R2′, R3, R3′, L1, L1′, L2 and L2′ are defined as in the claims, with metallic cations, especially Pb(II) and Bi(III). Also disclosed are bifunctional do2pa derivatives ligands of formula (I), as well as the use of chelates in nuclear medicine and the use of ligands in cations detection or epuration of effluents.
Claims15
A chelate resulting from the complexation of a ligand of formula (Ia)
- or a basic salt thereof;
- wherein
- R1 and R1′ each independently represents:
- a hydrogen atom;
- a coupling function, wherein the coupling function is selected from the group consisting of amine;
- isothiocyanate;
- isocyanate;
- N-hydroxysuccinimide ester, N-hydroxyglutarimide ester, maleimide ester;
- carboxylic acid;
- acid anhydride, acid halide;
- alcohol;
- alkyne;
- halide;
- azide;
- siloxy;
- phosphonic acid;
- thiol;
- tetrazine;
- norbornen;
- oxoamine;
- aminooxy;
- thioether;
- haloacetamide;
- glutamate;
- glutaric anhydride, succinic anhydride, maleic anhydride;
- aldehyde;
- ketone;
- hydrazide;
- chloroformate;
- and maleimide;
- or
- a bioactive group, wherein the bioactive group is a peptide;
- L1 and L1′ each independently represents:
- a single bond;
- or
- a linker selected from the group consisting of alkyl, aryl, arylalkyl, alkylaryl, heteroaryl, heteroarylalkyl, alkylheteroaryl, alkenyl, and alkynyl;
- wherein alkyl moieties are optionally interrupted by one or more heteroatoms selected from the group consisting of O, N, and S;
- optionally additionally comprising a residue of a coupling function through which R1 and R1′ are bounded to L1, and L1′ respectively;
- provided that at least one of -L1-R1 and-L1′-R1′ represents a linker with a coupling function or a linker with a bioactive group;
- with a metallic cation selected from the group consisting of bismuth (III), lead (II), copper (II), copper (I), gallium (III), zirconium (IV), technetium (III), indium (III), rhenium (VI), astatine (III), yttrium (III), samarium (III), actinium (III), lutetium (III), terbium (III), holmium (III), gadolinium (III), europium (III), and 212Bi(212Pb).
Dependencies are inferred from the claim text.