CONTRAST AGENTS ENDOWED WITH HIGH RELAXIVITY FOR USE IN MAGNETIC RESONANCE IMAGING (MRI) WHICH CONTAIN A CHELATING MOIETY WITH POLYHYDROXYLATED SUBSTITUENTS

摘要

The present invention relates to a novel class of paramagnetic ion-based contrast i agents of formula (I), wherein a chelating backbone moiety is highly functionalized by the presence of one or more polyhdroxylated chain, that show a pharmacokinetic i profile analogous to that of the commonly used T1-general extravascular agents (NSA) but are further characterized by a higher relaxivity. Formula (I): A(LR)<SUB>V </SUB>wherein: A is a linear or cyclic chelating backbone moiety; R is, independently, H or a C<SUB>2-</SUB>C<SUB>70 </SUB>aminopolyol moiety comprising a 'straight or branched alkyl chain substituted by from 2 to 30 hydroxyl groups, the said chain being optionally interrupted by one or more groups selected from -0-, -NH-, -N<, -CO-, -CONH-, -NHCO-, -CON< or >NCO-; and optionally substituted by one or more C4-C10 cyclic units; L is, independently, a direct bond or "a divalent straight or branched linker moiety between A and R, at most comprising 20 carbon atoms; V is a positive integer from 1 to 7; with the proviso that at least one of the R groups is other than H; or a physiologically acceptable salt of such ligand.