CHOLECYSTOKININ B RECEPTOR TARGETING FOR IMAGING AND THERAPY

摘要

Conjugates are described herein where CCK2R targeting ligands are attached to an active moiety, such as therapeutic agent or an imaging agent, through a linker. The conjugates can be used in the detection, diagnosis, imaging and treatment of cancer.

主权项

1. A conjugate of the following formula
B-[L-D]n wherein B is a targeting ligand of Formula I wherein: the bond between X and Y is a single bond or a double bond, R1=H, CH3 or heterocycle with R2; R2=heterocycle with R1, CH3, CH2CON(Et)2, CH2COC(CH3)3, CH2CONHC(CH3)3, X=CR3 or NR4; R3=phenyl, cyclohexyl, CH3, CH2—CH3, R4=phenyl, cyclohexyl, Y=CH2, N (dashed=double bond), C═O; z= R5=absent, phenyl, C1, CO2H, CH3, OCH3, NHCH3, F, SCH2CO2H, SCH2CO2Et, and analogs, derivatives, salts and esters thereof,L is a bivalent or polyvalent linker,D is an active moiety, wherein each active moiety is individually selected from therapeutic agents and imaging agents, andn is an integer of between 1 and 5.