Imaging agents and methods of imaging NAALADase or PSMA
AssigneeThe Johns Hopkins University
InventorsMartin Gilbert Pomper, Jiazhong Zhang, Alan P. Kozikowski, John L. Musachio
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Abstract
The present invention relates to compounds particularly asymmetric urea compounds which are labeled with one or more radioisotopes and which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors which express NAALADase and/or PSMA. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled compounds of the invention, particularly tissues, organs, or tumors which express NAALADase and/or PSMA to which the compounds of the invention have an affinity.
Claims28
A compound according to Formula I
- wherein
- R is selected from the group consisting of fluoroalkyl, aryl, and benzyl, each of which is optionally substituted with an optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted alkanoyl, or optionally substituted aralkyl, optionally substituted alkoxy, optionally substituted aralkyloxy, or optionally substituted phenoxy, and wherein the R group comprises one or more positron emitting radioactive isotopes;
- Q is hydrogen, optionally substituted alkyl, optionally substituted benzyl or optionally substituted phenyl;
- and
- Z is H, CO2H;
- or a pharmaceutically acceptable salt thereof.
A compound according to Formula II
- wherein R1 is selected from methyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted fluoroalkyl, optionally substituted aryl, and optionally substituted aralkyl, and the R1 group comprises at least one radioactive isotope or fluorescent dye selected from 11C, 18F, 99Tc, 123I, or any combination thereof;
- or a pharmaceutically acceptable salt thereof.
A compound which is 2-[3-(1-Carboxy-2-11C-methylsulfanyl-ethyl)-ureido]-pentanedioic acid.
A compound according to Formula VII:
- wherein
- L is a chelating ligand suitable for coordination to Tc;
- p is 0, or 1;
- and
- n is an integer of from 1 to 6;
- or a pharmaceutically acceptable salt thereof.
A package comprising:
- (i) a compound of the following Formula I:
- wherein
- R is selected from the group consisting of fluoroalkyl, aryl, and benzyl, each of which is optionally substituted with an optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted alkanoyl, or optionally substituted aralkyl, optionally substituted alkoxy, optionally substituted aralkyloxy, or optionally substituted phenoxy, and wherein R comprises one or more positron emitting radioactive isotopes;
- Q is hydrogen, optionally substituted alkyl, optionally substituted benzyl or optionally substituted phenyl;
- and
- Z is H, CO2H;
- or a pharmaceutically acceptable salt thereof;
- and
- (ii) indicia comprising at least one of:
- instructions for using the composition to image cells or tissues expressing at least one of NAALADase or PSMA, or
- instructions for using the composition to image glutamatergic neurotransmission in a patient suffering from a stress-related disorder, or
- instructions for using the composition to image prostate cancer.
Dependencies are inferred from the claim text.