Bracco Imaging S.p.a.

Matteo Galli

Fulvio Uggeri

Kondareddiar Ramalingam

Luciano Lattuada

Silvio Aime

Pierfrancesco Morosini

The present invention relates to a novel class of paramagnetic ion-based contrast agents of formula (I), wherein a chelating backbone moiety is highly functionalized by the presence of one or more polyhydroxylated chain, that show a pharmacokinetic profile analogous to that of the commonly used T1-general extravascular agents (NSA) but are further characterized by a higher relaxivity.

Contrast agents endowed with high relaxivity

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 polyhydroxylated 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)wherein: A is a linear or cyclic chelating backbone moiety; R is, independently, H or a CCaminopolyol 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-, &#x2014;NH&#x2014;, &#x2014;N&#x3c;, &#x2014;CO&#x2014;, &#x2014;CONH&#x2014;, &#x2014;NHCO&#x2014;, &#x2014;CON&#x3c; or &#x3e;NCO&#x2014;; 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.

Contrast agents endowed with high relaxivity for use in magnetic resonance imaging (MRI) which contain a chelating moiety with polyhydroxylated substituents

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Treviglio, Italy

Matteo Galli