Conjugates of PSMA-binding moieties with cytotoxic agents

Abstract

A conjugate of Formula I or a pharmaceutically acceptable salt thereof, wherein: PB is a PSMA binding moiety which has a molecular weight of below 1000 Da; L1 is a linker covalently attaching PB to Gly-Pro, said linker being a saturated or a partially or fully unsaturated framework comprising C and H atoms and at least one heteroatom, wherein said framework has end points of attachment ‘a’ and ‘b’ and a length between 6 and 30 atoms (via the shortest path between PB and Gly-Pro) between ‘a’ and ‘b’; wherein said framework may include one or more straight and/or branched chains and/or rings and is optionally substituted on any available C atom(s) by one or more F; L2 is a either a single bond or a self-immolative linker; and Drug is a cytotoxic agent linked to Gly-Pro.

CPC Classifications