Peptide-Based Compounds
AssigneeGe Healthcare Limited
InventorsAlan Cuthbertson, Bard Indrevoll
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Abstract
The invention relates to new peptide-based compounds for use as diagnostic imaging agents or as therapeutic agents wherein the agents comprise a targeting vector which binds to receptors associated with integrin receptors.
Claims10
1-20. (canceled)
A compound of formula I representing a vector (V)
- wherein
- G represents glycine, and
- D represents aspartic acid, and
- R1 represents —(CH2)n— or —(CH2)n—C6H4— wherein
- n represents a positive integer 1 to 10, and
- h represents a positive integer 1 or 2, and
- X1 represents a bond or 1 to 5 amino acid residues wherein each amino acid residue independently optionally can be derivatized with a functional side-chain suitable for modifying the pharmacokinetics or blood clearance rates of the said agents, and
- X2 and X4 represent independently an amino acid residue capable of forming a disulfide bond,
- X3 represents arginine, N-methylarginine or an arginine mimetic,
- X5 represents a hydrophobic amino acid or derivatives thereof, and
- X6 represents a thiol-containing amino acid residue,
- and k represents a positive integer 1 to 10, and
- X7 represents 1 to 10 amino acid residues or is absent,
- and X8 is absent.
A pharmaceutical composition comprising an effective amount of a compound of general formula (I) or a salt thereof, together with one or more pharmaceutically acceptable adjuvants, excipients or diluents for use in enhancing image contrast in in vivo imaging or for treatment of a disease.
A process for the preparation of a contrast agent comprising the moieties vector (V), linker (L) and reporter (R), said process comprising the conjugation of the vector V, optionally via the linker (L) to a compound detectable in a diagnostic imaging procedure or to a chelating agent and if necessary metallating the chelant groups in the resultant conjugate with a metal ion detectable in a diagnostic imaging procedure.
Dependencies are inferred from the claim text.