Manganese chelates and their use as contrast agents in magnetic resonance imaging (MRI)

Patent metadata

Field	Value
Publication number	US-9486544-B2
Application number	US-201013510064-A
Country	US
Kind code	B2
Filing date	Dec 17, 2010
Priority date	Dec 18, 2009
Publication date	Nov 8, 2016
Grant date	Nov 8, 2016

Abstract

The present invention relates to manganese(II). The invention also relates to manganese(II) chelates attached to other molecules and their use as contrast agents in magnetic resonance imaging (MRI).

First claim

What is claimed is:

1. A compound having formula (II)

wherein R L is a hydrogen or a linker whereby the compound of formula (II) can be linked to another molecule,
wherein the linker R L is selected from group consisting of:

 and
wherein n is an integer from 1 to 7 and * denotes the position whereby the linker, if present, is attached to the compound and said another molecule.

2. The compound of claim 1 , wherein said another molecule is an aromatic ring, inositol or carbohydrate, or any derivative thereof.

3. The compound of claim 1 , wherein said another molecule is a natural or synthetic peptide, an amino acid or derivatives thereof, polyamines and derivatives thereof, a peptidomimetic, a polypeptide, a protein, an antibody, a natural or synthetic polymer, a dendrimer, a nanoparticle or a lipophilic compound.

4. The compound of claim 3 , wherein said another molecule is a dendrimer.

5. The compound of claim 1 , wherein the compound is of the following structures:

6. A compound having the formula:

wherein X is alkyl or a linker;
Y is alkyl, —PEG, —COOH, —PO(OH) 2 , —H, or a linker;
R is alkyl, —PEG, —N(alkyl) 2 , —N(PEG) 2 , —O(alkyl), —O(PEG), —NMe 2 , —NH 2 , —OMe, —OH, —H, or a linker;
wherein the compound is attached to another molecule if a linker is present;
wherein the linker moiety is selected from group consisting of:

and wherein n is an integer from 1 to 7 and * denotes the position whereby the linker, if present, is attached to the compound and said another molecule.

7. Compound according to claim 6 , wherein Y is methyl, —COOH, —PO(OH) 2 , —H or a linker.

8. Compound according to claim 6 , wherein Y is —H or a linker.

9. Compound according to claim 6 , wherein R is H, methyl, —NMe 2 , —NH 2 , —OMe, —OH or a linker.

10. Compound according to claim 6 , wherein the compound is attached to another molecule via said linker.

11. Compound according to claim 10 , wherein said another molecule is an aromatic ring, inositol or carbohydrate, or any derivative thereof.

12. Compound according to claim 10 , wherein said another molecule is a natural or synthetic peptide, an amino acid or derivatives thereof, polyamines and derivatives thereof, a peptidomimetic, a polypeptide, a protein, an antibody, a natural or synthetic polymer, a dendrimer, a nanoparticle or a lipophilic compound.

13. Compound according to claim 12 , wherein said another molecule is a dendrimer.

14. Compound according to claim 6 for use as MR contrast agents.

15. Composition comprising a compound according to claim 6 and at least one physiologically tolerable carrier.

16. Composition according to claim 15 for use as MR contrast medium in MRI.

17. Method of MR imaging wherein a composition according to claim 15 is administered to a subject and the subject is subjected to an MR examination wherein MR signals are detected from the subject or parts of the subject into which the composition distributes and optionally MR images and/or MR spectra are generated from the detected signals.

18. Compound according to claim 6 , wherein X is C 1 -C 6 alkyl.

19. A compound of claim 6 , having one of the following structures:

Assignees

• Meijer Andreas
• Ge Healthcare As

Inventors

• Meijer Andreas

Classifications

• C07D471/04 Primary

  Ortho-condensed systems · CPC title

• A61K49/10

  Organic compounds · CPC title

• A61K49/106 Primary

  the complex-forming compound being cyclic, e.g. DOTA · CPC title

• C07D471/08

  Bridged systems · CPC title

• A61K49/12

  Macromolecular compounds · CPC title