Chelating polymers as contrast agents for medical imaging

C - Chemistry – Metallurgy – 08 – G

Patent

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C08G 69/48 (2006.01) A61K 31/16 (2006.01) A61K 31/21 (2006.01) A61K 31/395 (2006.01) A61K 31/785 (2006.01) A61K 49/00 (2006.01) A61K 49/08 (2006.01) A61K 51/06 (2006.01) C08G 63/91 (2006.01)

Patent

CA 2223456

The invention provides polymeric polychelants containing polymer repeat units of the formula [L-Ch-L-B] (where Ch is a polydentate chelant moiety; L is an amide or ester linkage; B is a hydrophobic group providing a carbon chain of at least 4 carbon atoms between the L linkages it interconnects) or a salt or chelate thereof, with the proviso that where Ch is 2,5-biscarboxymethyl-2,5- diazahex-1,6-diyl, the polychelant is metallated with lanthanide or manganese ions or B provides a carbon chain of at least 10 carbon atoms between the L linkages it interconnects and their salts and chelates. The paramagnetic polychelates of the polychelants of the invention have remarkably high R1 relaxivities.

On décrit de nouveaux polychélateurs polymères contenant des motifs récurrents polymères de formule [L-Ch-L-B]; (où Ch représente une fraction chélatrice polydentée; L représente une liaison amide ou ester; B représente un goupe hydrophobe fournissant une chaîne carbonée d'au moins 4 atomes de carbone entre les liaisons L qu'il relie), ou bien l'un de ses sels ou chélates, à condition que, quand Ch représente 2,5-biscarboxyméthyl-2,5-diazahex-1,6-diyle, le polychélateur subisse une métallation avec des ions lanthanide ou manganèse ou que B fournisse une chaîne carbonée d'au moins 10 atomes de carbone entre les liaisons L qu'il relie et leurs sels et chélates. Les polychélates paramagnétiques des polychélateurs décrits présentent des relaxivités R¿1? remarquablement élevées.

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