HALOGENATED COMPOUNDS FOR CANCER IMAGING AND TREATMENT AND METHODS FOR THEIR USE

摘要

Compounds having a structure of Formula I:;;or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R4, R5, X1, X2, X3 and X4 are as defined herein, and wherein the compound comprises at least one F, Cl, Br, I or 123I moiety, are provided. Uses of such compounds for imaging diagnostics in cancer and therapeutics methods for treatment of subjects in need thereof, including prostate cancer as well as methods and intermediates for preparing such compounds are also provided.

主权项

1. A compound having a structure of Formula I:or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein:
R1 and R2 are each independently H or C1-C10 alkyl, or R1 and R2, together with the carbon atom to which they are bound, are taken together to form a carbocyclic or heterocyclic ring; R3, R4 and R5 are each independently H, C1-C10 alkyl or C1-C10 alkylcarbonyl; and X1, X2, X3 and X4 are each independently H, F, Cl, Br, I or 123I, wherein at least one of X1, X2, X3 or X4 is F, Cl, Br, I or 123I.