18f-labeled triazole containing psma inhibitors
OwnerJohn W. Babich, James M. Kelly +2inventors
InventorsJohn W. Babich, James M. Kelly, Alejandro Amor-Coarasa, Shashikanth Ponnala
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Abstract
The present technology is directed to compounds, intermediates thereof, compositions thereof, medicaments thereof, and methods related to the imaging of mammalian tissue overexpressing PSMA. The compounds are of Formula I or a pharmaceutically acceptable salt thereof, wherein one of R1, R2, and R3 is and of Formula IV or a pharmaceutically acceptable salt thereof.
Claims21
A compound of Formula I
- or a pharmaceutically acceptable salt thereof, wherein
- P1, P2, and P3 are each independently H, methyl, benzyl, 4-methoxybenzyl, or tert-butyl;
- W1 is —C(O)— or —(CH2)n—NH—C(O)—;
- one of R1, R2, and R3 is
- N and the remaining two of R1, R2, and R3 are each H;
- X1 is absent, O, S, or NH;
- m is 0, 1, 2, or 3;
- n is 1 or 2;
- p is 0, 1, 2, or 3, provided that when p is 0 then X1 is absent;
- and
- q is 1 or 2.
A compound of Formula IV
- wherein
- P7, P8, and P9 are each independently H, methyl, benzyl, 4-methoxybenzyl, or tert-butyl;
- w is 1 or 2;
- x is 0, 1, 2, or 3;
- and
- y is 1 or 2.
-15. (canceled)
A composition comprising a compound of claim 15 and a pharmaceutically acceptable carrier.
A pharmaceutical composition for detecting a mammalian tissue overexpressing prostate specific membrane antigen (“PSMA”), the composition comprising an effective amount of the compound of claim 15 and a pharmaceutically acceptable excipient.
A method comprising
- administering a compound of claim 15 to a subject;
- and
- subsequent to the administering, detecting one or more of positron emission, gamma rays from positron emission and annihilation, and Cerenkov radiation due to positron emission.
Dependencies are inferred from the claim text.