Macrocyclic compounds and diagnostic uses thereof
AssigneeJanssen Biotech, Inc.
InventorsShalom GOLDBERG, Kristen WILEY, Rhys SALTER
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Abstract
The present invention is directed to compounds (macrocyclic compounds) and pharmaceutically acceptable salts thereof, immunoconjugates, radioimmunoconjugates thereof, pharmaceutical compositions containing said compounds and immunoconjugates, radioimmunoconjugates thereof, and the use of said compounds and immunoconjugates, radioimmunoconjugates thereof, in nuclear medicine as tracers and imaging agents.
Claims26
A radiometal complex of formula (I-M+):
- or a pharmaceutically acceptable salt thereof, wherein:
- M+ is a radiometal ion that is cerium-134 (134Ce);
- R1 is hydrogen and R2 is -L1-R4;
- alternatively, R1 is -L1-R4 and R2 is hydrogen;
- R3 is hydrogen;
- alternatively, R2 and R3 are taken together with the carbon atoms to which they are attached to form a 5- or 6-membered cycloalkyl, wherein the 5- or 6-membered cycloalkyl is optionally substituted with -L1-R4;
- L1 is absent or a linker;
- R4 is a nucleophilic moiety, an electrophilic moiety, or a targeting ligand.
An immunoconjugate selected from the group consisting of:
- wherein:
- L1 is absent or a linker;
- and
- mAb is an antibody or antigen binding fragment thereof.
A radioimmunoconjugate selected from the group consisting of:
- wherein:
- M+ is a radiometal ion that is cerium-134 (134Ce);
- L1 is absent or a linker;
- and
- mAb is an antibody or antigen binding fragment thereof.
A method of imaging prostate cancer cells in a patient, the method comprising:
- administering to the patient an effective amount of a radioimmunoconjugate having the following structure:
- wherein M+ is cerium-134 (134Ce) and mAb is a PSMA-targeting antibody or a KLK2-targeting antibody.
Dependencies are inferred from the claim text.