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US 2025/0177580 A1Published application
Psma targeted radiohalogenated urea-polyaminocarboxylates for cancer radiotherapy
AssigneesThe Johns Hopkins University, Duke University
InventorsMartin G. Pomper, Ronnie C. Mease, Vivek Kumar, Sangeeta Ray, Michael Zalutsky, Ganesan Vaidyanathan
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Abstract
Small molecule radiohalogenated PSMA inhibitors and metal complexes thereof and their use in radioimaging and radiotherapy for treating PSMA-related diseases, including prostate cancer, are disclosed. The combination of small molecule radiohalogenated PSMA inhibitors with a competitive PSMA ligand for reducing off-target accumulation of the radiohalogenated PSMA inhibitor also is disclosed.
Claims27
A compound of formula (I):
- wherein:
- Z is CO2Q;
- Q is H;
- m is;
- R is CH2—R1;
- wherein R1 is:
- wherein X1 is —CR3 or —C—X, wherein R3 is H;
- wherein X is selected from the group consisting of a radioisotope of iodine, a radioisotope of bromine, and a radioisotope of astatine;
- L is a linker selected from the group consisting of C1, C2, C3, C4, C5, and C6 alkylene;
- W is —(C═O)—NR2—;
- wherein each occurrence of L and W can be the same or different;
- R2 is H;
- n is an integer selected from the group consisting of 1 and 2;
- Ch is a chelating agent that can comprise a metal;
- and
- pharmaceutically acceptable salts thereof.
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Dependencies are inferred from the claim text.