Contrast agents
AssigneeGe Healthcare Limited
InventorsHelge Tolleshaug, Alan Cuthbertson, Hege Karlsen
Life of this patent
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Abstract
The present invention provides novel compounds and pharmaceutical compositions containing such compounds, wherein the compounds have affinity for proteoglycans. The compounds comprise an amino acid based core unit linked to positively charged moieties. The compounds further comprise at least one imaging moiety detectable in in vivo imaging making the compounds useful as diagnostic contrast agents for imaging of proteoglycans, such as heparan sulphate proteoglycans.
Claims14
A compound of formula I having affinity for proteoglycans, and pharmaceutically acceptable salts thereof
- R—Sp—C-(L-P)n (I)
- wherein
- C represents a core unit linked to the L units and to the S unit when S is present or to the R moiety when S is not present, and which comprises amino acid residues selected from the group consisting of lysine, ornithine, and diaminopropionic acid, and optionally an amine;
- L is the same or different and represents a bifunctional linker unit comprising a PEG linker, wherein said PEG linker is of formula (II)
- wherein q equals an integer from 1 to 10 and which binds to the carboxy and the amino entities of amino acids;
- or said PEG linker is of formula:
- P is the same or different and represents a positively charged peptide unit comprising 2 to 8 positive charges and 2 to 20 amino acids, wherein at least one amino acid contains a guanidine group;
- S represents a spacer unit;
- R represents an imaging moiety comprising an imaging entity selected from the group consisting of:
- (i) a radioactive metal ion;
- (ii) a paramagnetic metal ion;
- (iii) a gamma-emitting radioactive halogen;
- (iv) a positron-emitting radioactive non-metal;
- (v) a hyperpolarised NMR-active nucleus;
- (vi) a reporter suitable for in vivo optical imaging;
- and
- (vii) a β-emitter suitable for intravascular detection;
- p represents an integer of 0 or 1;
- and
- n represents an integer from 1 to 16.
A compound of formula (I) selected from the group consisting of:
- chelated with a radioactive metal entity;
- and
- chelated with a radioactive metal entity.
A compound of formula (I) suitable for optical imaging selected from the group consisting of:
Dependencies are inferred from the claim text.