Conjugates for imaging
Inventors
Vlahov, Iontcho R. • Leamon, Christopher P. • Santhapuram, Hari Krishna R.
Assignees
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Publication Number
US-10188759-B2
Publication Date
2019-01-29
Expiration Date
Abstract
The invention described herein relates to conjugates and compositions for imaging, diagnosing, and/or monitoring diseases using radionuclide-based imaging. In particular, the invention described herein relates to conjugates and compositions for imaging, diagnosing, and/or monitoring diseases using positron emission tomography.
Core Innovation
The invention provides conjugates, or pharmaceutically acceptable salts thereof, defined by a specified formula. The content describes PET imaging conjugates that target vitamin receptor-mediated endocytosis, including folate receptor targeting using folic acid and derivatives, and also indicates targeting of PSMA (prostate-specific membrane antigen).
The partial content further describes radionuclide complexation and positron-emitting metal ions for PET imaging, including 89Zr, 68Ga, and 64Cu. It also describes deferoxamine-based conjugates, including EC2419, EC2420, EC2448 and EC2448-derived derivatives, as well as peptide-conjugate EC2448, EC2450, EC2458, EC2460, and EC0652 to EC2460.
The content also includes related pharmaceutical carriers and excipients, kit concepts associated with the conjugates and/or salts, and chemical purification and confirmation, including column purification and LCMS confirmation. Illustrative conjugates such as EC2418, EC2419, EC2420, and related EC compounds are described, together with chemical formulas and analytical reporting such as LCMS (ESI) for illustrative conjugates.
Claims Coverage
The independent claims are directed to formula-defined conjugates, or pharmaceutically acceptable salts thereof. Coverage includes multiple inventive features across the claim sets, including 89Zr complexation, pharmaceutical compositions, and kits.
Formula-defined conjugate and pharmaceutically acceptable salt
A conjugate, or a pharmaceutically acceptable salt thereof, of the formula [formula-defined conjugate].
Conjugate complexed with 89Zr
The conjugate, or its pharmaceutically acceptable salt, is complexed with 89Zr.
Pharmaceutical composition comprising the conjugate or salt
A composition comprising a conjugate, or a pharmaceutically acceptable salt thereof, of claim 1.
Kit comprising the conjugate or salt
A kit comprising a conjugate, or a pharmaceutically acceptable salt thereof, of claim 1.
Overall, the claims focus on formula-defined PET imaging conjugates and pharmaceutically acceptable salts, with dependent coverage adding 89Zr complexation and further expanding the subject matter to compositions and kits containing the conjugate or salt.
Stated Advantages
PET imaging is enabled using conjugates that target folate receptors and PSMA, as described in the partial content.
Documented Applications
PET imaging targeting folate receptor-mediated endocytosis and PSMA (prostate-specific membrane antigen), as described in the partial content.
PET imaging conjugates using deferoxamine conjugates complexed with a positron-emitting metal ion using known PET-imaging conjugate procedures.
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