Abstract: New chelators such as H3L1, H3L2, H3L3, H3L26 and derivatives were synthesized for the complexation of {Al18F}2+. These new chelators are able to complex {AI18F}2+ with good radiochemical yields using a labeling temperature of 37° C. The stability of the new Al18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum. AI18F-L3 and AI18F-L26 showed a stability comparable to that of the previously reported Al18F-NODA. Moreover, the biodistribution of Al18F-L3 and AI18F-L26 showed absence of in vivo demetallation since only very limited bone uptake was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestine due to hepatobiliary clearance of the radiolabeled ligand. The chelators H3L3 and Al18F-L26 demonstrated to be a good lead candidates for the labeling of heat sensitive biomolecules with 18F-fluorine and derivatives have been synthesized.

Abstract: New chelators such as H3L1, H3L2, H3L3, H3L26 and derivatives were synthesized for the complexation of {Al18F}2+. These new chelators are able to complex {AI18F}2+ with good radiochemical yields using a labeling temperature of 37° C. The stability of the new Al18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum. AI18F-L3 and AI18F-L26 showed a stability comparable to that of the previously reported Al18F-NODA. Moreover, the biodistribution of Al18F-L3 and Al18F-L26 showed absence of in vivo demetallation since only very limited bone uptake was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestine due to hepatobiliary clearance of the radiolabeled ligand. The chelators H3L3 and Al18F-L26 demonstrated to be a good lead candidates for the labeling of heat sensitive biomolecules with 18F-fluorine and derivatives have been synthesized.

Abstract: The present invention relates to the compound of formula (I), in which R1 represents Sn(R)3, B(OH)2, B(OR)2, a halogen atom, NO2, a radionuclide or a —N+(R)3 group, where R is a (C1-C6) alkyl group, R2 represents a hydrogen atom or a (C1-C6)alkyl group, R3 represents: a —(CH2CH2O)n2—(CH2)n3—X group, or a —(CH2CH2O)n4—(CH2)n5—Y group with Y representing a —C?C—H, a —N3 or a —Ar—(CH2)n6—(OCH2CH2)n7—X group, and X represents a halogen atom, a radionuclide or a —OSO2R? group, where R? is a CF3, CH3, t-Bu, Ph, p-NO2Ph, p-BrPh or p-CH3Ph group, and their addition salts with pharmaceutically acceptable acids, The present invention also relates to pharmaceutical compositions comprising them and to their use in diagnosis, in particular with SPECT or PET imaging and in therapy of melanoma, via targeted radionuclide therapy.