Aminocarboxylate ligands having substituted aromatic amide moieties
AssigneeBracco International B.V.
InventorsRadhakrishna K. Pillai, Sang I. Kang, Edmund R. Marinelli, Ramachandran S. Ranganathan, Michael F. Tweedle
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Abstract
Novel metal-chelate complexes comprising aminocarboxylate ligands including substituted aromatic amide moieties, such as those having the formula 1 wherein R13, A1, R1 and R2 are as defined herein, are disclosed.
Claims50
A diagnostic agent comprising an aminocarboxylate ligand complexed with a paramagnetic metal ion wherein a nitrogen atom within said aminocarboxylate is substituted with a substituted aromatic amide group.
A compound of the formula
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- A1 is —(CH2)m′— or a single bond;
- (CH2)m and (CH2)m′ may independently be substituted with alkyl or hydroxyalkyl;
- R1 and R2 are each independently hydrogen, alkyl, —NO2, —NH2,
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- NCS,
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- and NR3COR9 where R9 is alkyl or hydroxyalkyl, with the proviso that at least one of R1 and R2 must be other than hydrogen;
- R3 and R4 are independently hydrogen, alkyl, arylalkyl, aryl, alkoxy and hydroxyalkyl;
- R12 is hydrogen, alkyl or hydroxyalkyl;
- R13 is hydrogen, alkyl, arylalkyl, aryl, alkoxy or hydroxyalkyl;
- m and m′ are independently 1 to 5;
- and multimeric forms thereof.
A complex, or a pharmaceutically acceptable salt of a complex, of a metal atom and a metal chelating ligand having the formula
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- wherein
- A1 is —(CH2)m′— or a single bond;
- (CH2)m and (CH2)m′ may independently be substituted with alkyl or hydroxyalkyl;
- R1 and R2 are each independently hydrogen, alkyl, —NO2, —NH2,
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- NCS,
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- and NR3COR9 where R9 is alkyl or hydroxyalkyl, with the proviso that at least one of R1 and R2 must be other than hydrogen;
- R3 and R4 are independently hydrogen, alkyl, arylalkyl, aryl, alkoxy and hydroxyalkyl;
- R12 is hydrogen, alkyl or hydroxyalkyl;
- R13 is hydrogen, alkyl, arylalkyl, aryl, alkoxy or hydroxyalkyl;
- m and m′ are independently 1 to 5;
- and multimeric forms thereof.
Dependencies are inferred from the claim text.