HBED-Bisphosphonates, Radiometal Conjugates and Their Use as Theranostic Agents

摘要

The present invention relates to compounds according to Formula I or Formula II, which are potential bone imaging agents. Certain compounds labeled with 68Ga displayed excellent bone uptake and retention. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I or Formula II or a pharmaceutically acceptable salt thereof.;

主权项

1. A compound according to Formula I: or a pharmaceutically acceptable salt thereof, wherein
A is a divalent linking moiety comprising 1 to 10 carbon atoms in a chain, a ring, or a combination thereof, wherein at least one carbon atom is optionally replaced with O, —NR9—, or —C(O)—;B is CR3R4;X is selected from the group consisting of: n is from 1 to 8;Y is independently CH or N;R1 is hydrogen or a (C1-C6) alkyl group;R2, R5, and R8 are independently hydrogen or a carboxylic acid protecting group;R3 and R4 are independently hydrogen, a (C1-C10) alkyl group, an ethylene glycolyl group, or a propylene glycolyl group;R6 is hydrogen or a (C1-C6) acyl group; andR7 is the α-position substituent of an amino acid, andR8 is independently selected from the group consisting of H, alkyl, cycloalkyl, heterocycloalkyl, aryl, alkylaryl, arylalkyl and heteroaryl.