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US 9,694,091 B2Granted
Labeled inhibitors of prostate specific membrane antigen (PSMA) biological evaluation, and use of imaging agents
AssigneeThe Johns Hopkins University
InventorsMartin G. Pomper, Sangeeta Ray, Ronnie C. Mease, Catherine Anne Foss
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Abstract
The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+PC3 PIP tumors.
Claims19
A compound of formula II:
- wherein
- AA1 and AA2 each independently a natural or unnatural amino acid;
- R′ is —CO—NRxRy—, or —CS—NRxRy—, —CORx, or —CSRx;
- R″ is H;
- Rx is optionally substituted aryl or optionally substituted alkyl;
- Ry is H;
- X and Z are each independently C1-C8 alkylene, each of which may be substituted with 0-5 RA;
- W is —C(═O)—;
- Y is —NH—CO—;
- RA, for each occurrence, is CO2H.
7 more elements
Dependencies are inferred from the claim text.