BET bromodomain protein degraders with cleavable linkers

US11267822B2 · kind B2 · utility

Assignee

• THE REGENTS OF THE UNIVERSITY OF MICHIGAN · US

Inventors

• Shaomeng Wang · Saline, US
• Weiguo Xiang · Ypsilanti, US
• Fuming Xu · Ypsilanti, US
• Longchuan Bai · Ann Arbor, US
• Ester Fernandez-Salas · San Mateo, US
• Donna McEachern · Ann Arbor, US

Key dates

• Filing date: Sep 12, 2018
• Grant date: Mar 8, 2022
• Expiry date: Oct 18, 2038

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D495/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present disclosure provides compounds represented by Formula (I): Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, Y, ═, Ar, W, L, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I)I for use to treat a condition or disorder responsive to inhibition and/or degradation of BET bromodomains such as cancer.