High purity copper radiopharmaceutical compositions and diagnostic and therapeutic uses thereof
AssigneesNuclidium AG, University of Basel
InventorsLeila JAAFAR-THIEL, Melpomeni FANI, Jacopo MILLUL, Francesco DE ROSE
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Abstract
The present disclosure relates to the field of nuclear imaging and therapy, and more specifically to high purity copper radiotracer compositions useful in imaging, such as positron emission tomography (PET) and single-photon emission computerized tomography (SPECT), and therapy. More specifically, the present disclosure relates to novel compositions useful in imaging and treatment of conditions such as prostate cancer, somatostatin receptor-expressing tumors, like neuroendocrine tumor, epithelial tumors, as well as to methods wherein such compositions are prepared.
Claims31
1-74. (canceled)
A pharmaceutical composition comprising a compound and a pharmaceutically acceptable excipient, wherein the compound is of Formula 30:
- wherein:
- R1 is Ra;
- R2 and R3 are each Ra or together form a C2-9 heterocycle with the nitrogen atoms to which they are attached;
- Ra, independently for each occurrence, is selected from H, C1-10 alkyl, C2-10 alkenyl, C3-10 alkynyl, C3-10 cycloalkyl, C6-10 aryl, C2-9 heterocyclyl, or C5-9 heteroaryl, optionally substituted by one or more substituents selected from —OH, —OR′, ═O, ═S, —SH, —SR′, —NH2, —NHR′, —N(R′)2, —NHCOR′, —NR′COR′, halogen, —CN, —CO2H, —CO2R′, —CHO, —COR′, —CONH2, —CONHR′, —CON(R′)2, —NO2, —OP(O)(OH)2, —SO3H, —SO3R′, —SOR′, and —SO2R′, wherein R′, independently for each occurrence, is C1-10 alkyl or C3-10 cycloalkyl;
- n is an integer from 1 to 20;
- m is an integer from 1 to 20;
- and
- *Cu is a copper radionuclide selected from 61Cu, 62Cu, 64 Cu, and 67Cu;
- or is a pharmaceutically acceptable salt thereof;
- and
- wherein the composition is characterized by one or more of:
- molar activity of ≥3 MBq/nmol;
- radiochemical purity of ≥91%;
- activity concentration of ≥8 MBq/mL;
- and
- radionuclidic purity of the compound at end of synthesis (EoB plus 2 hours) of ≥95%.
Dependencies are inferred from the claim text.