Radiolabelling methods
AssigneeHammersmith Imanet Limited
InventorsERIK ARSTAD, MATTHIAS EBERHARD GLASER
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Abstract
The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I) with a compound of formula (II): or, a compound of formula (III) with a compound of formula (IV) in the presence of a Cu (I) catalyst. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy.
Claims14
1-8. (canceled)
A compound of formula (II) or formula (IV):
- wherein L2 and L4 are each independently a C1-60 hydrocarbyl group optionally including 1 to 30 heteroatoms, alkyl, alkenyl, alkynyl chains, aromatic, polyaromatic, and heteroaromatic rings any of which may be optionally substituted with one or more ether, thiooether, sulphonamide, amide functional groups, amino acid, carbohydrate, or monomers and polymers comprising ethyleneglycol and R* is a reporter moiety selected from the group consisting of radionuclides and radionuclides incorporated into a chelating agent wherein said chelating agent is a chelating agent of Formula X:
- where:
- each R1A, R2A, R3A and R4A is independently an RA group;
- each RA group is independently H or C1-10 alkyl, C3-10 alkylaryl, C2-10 alkoxyalkyl, C1-10 hydroxyalkyl, C1-10 alkylamine, C1-10 fluoroalkyl, or 2 or more RA groups, together with the atoms to which they are attached form a carbocyclic, heterocyclic, saturated or unsaturated ring.
A compound of formula (V) or (VI):
- wherein L1, L2, L3, and L4 are each independently a C1-60 hydrocarbyl group optionally including 1 to 30 heteroatoms, alkyl, alkenyl, alkynyl chains, aromatic, polyaromatic, and heteroaromatic rings any of which may be optionally substituted with one or more ether, thiooether, sulphonamide, amide functional groups, amino acid, carbohydrate, or monomers and polymers comprising ethyleneglycol;
- R* is a reporter moiety selected from the group consisting of radionuclides and radionuclides incorporated into a chelating agent wherein said chelating agent is a chelating agent of Formula X:
- where:
- each R1A, R2A, R3A, R4A is independently an RA group;
- each RA group is independently H or C1-10 alkyl, C3-10 alkylaryl, C2-10 alkoxyalkyl, C1-10 hydroxyalkyl, C1-10 alkylamine, C1-10 fluoroalkyl, or 2 or more RA groups, together with the atoms to which they are attached form a carbocyclic, heterocyclic, saturated or unsaturated ring;
- and
- vector is a peptide, protein, hormone, cell, bacterium, or virus.
A compound of formula (I) or (III):
- wherein L1 and L3 are each independently a C1-60 hydrocarbyl group optionally including 1 to 30 heteroatoms, alkyl, alkenyl, alkynyl chains, aromatic, polyaromatic, and heteroaromatic rings any of which may be optionally substituted with one or more ether, thiooether, sulphonamide, amide functional groups, amino acid, carbohydrate, or monomers and polymers comprising ethyleneglycol and the vector is a peptide, protein, hormone, cell, bacterium, or virus.
15-16. (canceled)
Dependencies are inferred from the claim text.