abstract |
A compound of formula A-L-B wherein A is an E3 ubiquitin ligase protein binding ligand of formula I: I wherein L is a group which is bonded to the compound of formula I and L is a bond or a linker; wherein X is C or N; R1 is a bond or a linker to L; R2a is OH, -CHF2, -CF3, NH2 or F; R2b is H or a substituent; Rx is H, OH, -CHF2, -CF3, NH2 or F; R3 and R4 are H, a C-linked, O-linked, or C(O)-linked bond to L; R5 is a (C1-C3) alkyl group or a C-linked bond to L; Y is a linker; B is an optional ligand which binds to a target protein or polypeptide which is to be degraded by ubiquitin ligase, or a pharmaceutically acceptable, salt, enantiomer, stereoisomer, hydrate, solvate, or polymorph thereof. The compounds find use in PROteolysis Targeted Chimeras (PROTACs). |