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US 2020/0331893 A9Published application
Dimeric contrast agents
AssigneeBracco Imaging S.P.A.
InventorsValeria BOI, Roberta NAPOLITANO, Luciano LATTUADA
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Abstract
The present invention relates to new class of dimeric macrocycles capable of chelating paramagnetic metal ions, their chelated complexes with metal ions and the use thereof as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.
Claims27
A compound of formula (I)
- where:
- R is —CH(R1)—COOH, where:
- R1 is H or a C1-C3 alkyl chain that is optionally substituted by a C1-C3 alkoxy or C1-C3 hydroxyalkoxy group;
- n is 1 or 2;
- R2 is selected from the group consisting of:
- an aryl ring;
- a cyclohexyl ring;
- a C1-C5 alkyl substituted by one or more C1-C8 hydroxyalkoxy groups, or by a cycloalkyl ring;
- a group of formula —(CH2)sCH(R3)-G;
- and a C5-C12 hydroxyalkyl comprising at least 2 hydroxyl groups;
- in which
- s is 0, 1 or 2;
- R3 is H, or an arylalkylene or cycloalkyl-alkylene having from 1 up to 3 carbon atoms in the alkylene chain;
- G is a group selected from —PO(OR4)2, —PO(R5)(OR4) and —COOH;
- in which
- R4 independently of one another is H or C1-C5 alkyl;
- R5 is an aryl or a cyclohexyl ring, or C1-C5 alkyl which is optionally substituted by an aryl or cyclohexyl ring;
- and
- L is a C1-C6 alkylene, optionally interrupted by one or more —N(R′2)— groups, and optionally substituted by one or more substituent groups selected from hydroxyl, C1-C3 alkoxy and C1-C3 hydroxyalkoxy, where
- R′2 is, independently, as defined for R2,
- as well as individual diastereoisomers and their racemic mixtures, geometric isomers and solved enantiomers of the same, and the physiologically acceptable salt thereof.
18 more elements
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Dependencies are inferred from the claim text.