Covalent targeting of E3 ligases

US12161648B2 · kind B2 · utility

Assignees

• The Regents of the University of California · US
• Novartis AG · CH

Inventors

• Jessica Spradlin · Berkeley, US
• Carl Ward · Berkeley, US
• Daniel K. Nomura · Walnut Creek, US
• Markus Schirle · Cambridge, US
• John A. Tallarico · Cambridge, US
• Jeffrey McKenna · Horsham, GB
• Thomas John Maimone · Richmond, US
• Xirui Hu · Cambridge, US

Key dates

• Filing date: Oct 9, 2019
• Grant date: Dec 10, 2024
• Expiry date: Jan 25, 2042

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D493/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed herein, inter alia, are compositions and methods for targeting E3 ligases. In an aspect is a targeted protein degrader including 1) a targeted protein binder and 2) an E3 Ubiquitin ligase binder, wherein the E3 Ubiquitin ligase is human RNF4 or human RNF114. In an aspect is provided a pharmaceutical composition including a compound as described herein, including embodiments, and a pharmaceutically acceptable excipient.