BRM/BRG1 inhibitors and uses thereof
AssigneeFoghorn Therapeutics Inc.
InventorsRishi G. Vaswani, Neville John Anthony, David Simon Millan, Shawn E.R. Schiller, Kevin J. Wilson, David S. Huang
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Abstract
The compounds disclosed herein may be inhibitors of BRG1 (Brahma-related gene-1) and/or BRM (Brahma). The compounds or pharmaceutically acceptable salts thereof are useful for the treatment of disorders associated with an alteration in a BAF complex, e.g., a disorder associated with an alteration in one or both of the BRG1 and BRM proteins. Also disclosed are pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and methods of their preparation and use.
Claims16
A compound having the structure:
- wherein
- R1 is H, optionally substituted C1-C6 acyl, optionally substituted C1-C6 alkyl, optionally substituted C3-C8 cycloalkyl, optionally substituted C1-C6 heteroalkyl, optionally substituted C2-C9 heterocyclyl, or —SO2R6;
- each of R2 and R5 is, independently, H or optionally substituted C1-C6 alkyl;
- R3 is H and R4 is H
- R6 is optionally substituted C1-C6 alkyl or —NR7R8;
- R7 and R8 are, independently, optionally substituted C1-C6 alkyl;
- Het is optionally substituted 5-membered heteroarylene, optionally substituted 6-membered heteroarylene, or
- A is optionally substituted C6-C10 arylene, optionally substituted C2-C9 heterocyclylene, or optionally substituted C2-C9 heteroarylene;
- L is absent, —O—, optionally substituted C1-C6 alkylene, optionally substituted C1-C6 heteroalkylene, optionally substituted C2-C6 alkenylene, optionally substituted C2-C6 heteroalkenylene, optionally substituted C2-C6 alkynylene, optionally substituted C2-C6 heteroalkynylene, optionally substituted C2-C9 heterocyclylene, optionally substituted C2-C9 heteroarylene, or optionally substituted C2-C9 heteroaryl C1-C6 alkylene;
- and
- B is H, halogen, cyano, optionally substituted C6-C10 aryl, optionally substituted C3-C10 cycloalkyl, optionally substituted C2-C9 heterocyclyl, or optionally substituted C2-C9 heteroaryl;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.