Targeting compounds and methods for their production
AssigneeClarity Pharmaceuticals Ltd
InventorsPaul Stephen Donnelly, Nicholas Alan Zia
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Abstract
The present invention is directed to sarcophagine based compounds of formula (I). The compounds can complex a radioisotope, such as 64-copper and hence are useful in radioimaging and radiotherapy of cancers, e.g. colorectal cancer. The compounds work via a pre-targeting imaging approach in which the tetrazine reacts via click chemistry with a functional group such as a transcyclooctene which is pre-bound to a ligand such as a tumour specific antibody.
Claims16
A compound of Formula (I), or a salt thereof:
- wherein:
- R1 is a linker group;
- and
- R2 is optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl.
A kit comprising a compound of Formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein:
- R1 is a linker group;
- and
- R2 is optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl;
- the kit comprising:
- a container of a compound of Formula (I), or a pharmaceutically acceptable salt thereof;
- a container comprising a solution of a Cu radioisotope;
- and
- instructions for preparing an aqueous formulation of a compound of Formula (I), or a pharmaceutically acceptable salt thereof, complexed with a Cu radioisotope.
A combination comprising a compound of Formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein:
- R1 is a linker group;
- and
- R2 is optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl;
- and a compound that can bind to a tumour or cancer site and that comprises a functional group that reacts with the tetrazine moiety of the compound of Formula (I), wherein the functional group of the compound that can bind to a tumour or cancer site that reacts with a tetrazine moiety further comprises a transcyclooctene group.
A compound comprising
Dependencies are inferred from the claim text.