Degradation of bromodomain-containing protein 9 (BRD9) by conjugation of BRD9 inhibitors with E3 ligase ligand and methods of use
The present application provides bifunctional compounds of Formula (I): or Targeting Ligand or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for bromodomain-containing protein 9 (BRD9). The present application also provides methods for the targeted degradation of BRD9 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BRD9 which can be utilized in the treatment of disorders modulated by BRD9.
1. A bifunctional compound which is:
or a stereoisomer or pharmaceutically acceptable salt thereof.
2. A pharmaceutical composition comprising a therapeutically effective amount of the bifunctional compound of claim 1 , or a stereoisomer or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
3. A bifunctional compound which is
or pharmaceutically acceptable salt thereof.
4. A bifunctional compound which is
or pharmaceutically acceptable salt thereof.