Contrast agents endowed with high relaxivity for use in...

Drug – bio-affecting and body treating compositions – In vivo diagnosis or in vivo testing – Magnetic imaging agent

Reexamination Certificate

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Details

C514S102000, C514S107000, C514S492000, C514S502000

Reexamination Certificate

active

07988950

ABSTRACT:
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)vwherein: A is a linear or cyclic chelating backbone moiety; R is, independently, H or a C2-C70aminopolyol 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.

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PCT Search Report for PCT/EP2005/006958, mail date Oct. 7, 2005.
PCT Written Opinion of the ISA for PCT/EP2005/006958, mail date Oct. 7, 2005.
Kotek et al., “Lanthanide(III) complexes of novel mixed carboxylic-phosphorus acid derivatives of diethylentriamine; A step towards more efficient MRI contrast agents”, Chemistry-A European Journal, vol. 9, No. 23, Dec. 2003, pp. 5899-5915, XP002346487.

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