ASH1L degraders and methods of treatment therewith

US11110177B2 · kind B2 · utility

Assignee

• THE REGENTS OF THE UNIVERSITY OF MICHIGAN · US

Inventors

• Jolanta Grembecka · Ann Arbor, US
• Szymon Klossowski · Ann Arbor, US
• Jing Deng · Ann Arbor, US
• Tomasz Cierpicki · Ann Arbor, US
• Hao Li · Brookline, US
• Hongzhi Miao · Ann Arbor, US
• Trupta Purohit · Ann Arbor, US
• EunGi Kim · Ann Arbor, US
• Dong Chen · Ann Arbor, US

Key dates

• Filing date: Nov 9, 2018
• Grant date: Sep 7, 2021
• Expiry date: Jan 5, 2039

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C12Y203/02
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Provided herein are small molecules comprising a first domain that binds to ASH1L and a second domain that facilitates ASH1L degradation. In particular, ASH1L-targeting proteolysis targeting chimeras (PROTACs) and methods of use thereof for the treatment of disease (e.g., acute leukemia, solid cancers and other diseases dependent on activity of ASH1L) are provided.