Mri image enhancement of bone and related tissue using...

A - Human Necessities – 61 – B

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A61B 5/055 (2006.01) A61K 49/00 (2006.01) A61K 49/06 (2006.01) C07F 9/6524 (2006.01) G01R 33/28 (2006.01)

Patent

CA 2069638

Polyphosphonate ligands containing three or more phosphonate groups, combined with paramagnetic metal cations and adminictered in the form of pharmacologically acceptable salts, are useful as MRI contrast enhancement agents, which tend to localize in bone tissue without being conjugated to bone-specific biomolecules. Triazacyclononanes and tetraazacyclododecanes, with dihydroxyphosphorylmethyl or dihydroxyphosphorylethyl groups, optionally substituted at the methyl or ethyl bridges with alkyl, aryl, hydroxyl or amino groups, are particularly preferred.

Des ligands à base de polyphosphonate contenant au moins trois groupements phosphonates, combinés à des cations de métal paramagnétiques et administrés sous la forme de sels utilisables en pharmacie, sont utiles comme agents d'amélioration du contraste d'une IRM, qui ont tendance à se concentrer dans le tissu osseux sans se conjuguer aux biomolécules osseuses. Les triazacyclononanes et les tétraazacyclododécanes, avec des groupements dihydroxyphosphorylméthyles ou dihydroxyphosphoryléthyles, facultativement substitués aux ponts méthyles ou éthyles par des groupements alkyles, aryles, hydroxyles ou amines, sont particulièrement préférés.

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