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US 6,187,285 B1Granted
Metal chelates of substituted polyaminocarboxylic macrocycles and their use in diagnostic imaging
AssigneeGuerbet
InventorsDominique Meyer, Marc Port, Olivier Rousseaux, Christian Simonot
Life of this patent
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Abstract
Chelates of the compounds of formula I in which R is a hydrophilic group containing 3 or 4 successive phenyl rings and m is 1 or 2, with metal ions, for use in diagnostic imaging.
Claims12
Chelate of a cation of a paramagnetic metal with a compound of formula
- in which
- m is 1 or 2,
- R′ is selected from the group consisting of H, a C1-C4 alkyl or hydroxyalkyl group, a group CH2—COOH and a group CH2—CONZ1Z2, Z1 and Z2 being, independently of each other, H or an optionally hydroxylated C1-C4 alkyl group,
- or R′ is a group
- R is a group
- in which a is 1 or 2
- Z is selected from the group consisting of a bond, CH2,CH2CONH and (CH2)2NHCO
- Z′ is selected from the group consisting of a bond, O, S, NQ, CH2, CO, CO—NQ, NQ—CO, NQ—CO—NQ and CO—NQ—CH2—CONQ
- Z″ is selected from the group consisting of CO—NQ, NQ—CO, CO—NQ—CH2—CO—NQ and NQ—CO—CH2—NQ—CO
- where Q is H or an optionally hydroxylated C1-C4 alkyl group
- R1, R2, R3, R4 and R5, independently of each other, are selected from the group consisting of H, Br, Cl, I, CO—NQ1Q2 and N(Q1)—CO—Q2 and Q1 and Q2 are independently selected from C2-C6 alkyl groups which are optionally interrupted by an oxygen atom, wherein at least one of Q1, Q2 is hydroxylated such that Q1 and Q2 together contain from 4 to 10 OH groups,
- with the proviso that at least 1, and not more than 2, groups R1, R2, R3, R4 and R5 are amido groups,
- and the salts thereof with a pharmacologically acceptable organic base or inorganic base.
10 more elements
Scintigraphy agent containing a radio-labelled chelate of a metal cation with a compound of formula
- in which
- m is selected from the group consisting of 1 and 2,
- R′ is selected from the group consisting of H, a C1-C4 alkyl or hydroxyalkyl group, and a group CH2—COOH or CH2—CONZ1Z2, Z1 and Z2 being, independently of each other, H or an optionally hydroxylated C1-C4 alkyl group,
- or R′ is a group
- R is a group
- in which a is 1 or 2
- Z is selected from the group consisting of a bond, CH2, CH2CONH and (CH2)2NHCO
- Z′ is selected from the group consisting of a bond, O, S, NQ, CH2, CO, CO—NQ, NQ—CO, NQ—CO—NQ and CO—NQ—CH2—CONQ
- Z″ is selected from the group consisting of CO—NQ, NQ—CO, CO—NQ—CH2—CO—NQ and NQ—CO—CH2—NQ—CO
- where Q is H or an optionally hydroxylated C1-C4 alkyl group
- R1, R2, R3, R4 and R5, independently of each other, are selected from the group consisting of H, Br, Cl, I, CO—NQ1Q2 or N(Q1)—CO—Q2 and Q1 and Q2 are independently selected from C2-C6 alkyl groups which are optionally interrupted by an oxygen atom, wherein at least one of Q1, Q2 is hydroxylated such that Q1 and Q2 together contain from 4 to 10 OH groups, with the proviso that at least 1, and not more than 2, groups R1, R2, R3, R4 and R5 are amido groups,
- and the salts thereof with a pharmacologically acceptable organic base or inorganic base.
9 more elements
Dependencies are inferred from the claim text.