Pyrazolo[3,4-b]pyrazine derivatives as SHP2 phosphatase inhibitors

US11529348B2 · kind B2 · utility

Assignees

• D.E Shaw Research, LLC. · US
• Relay Therapeutics, Inc. · US

Inventors

• Alexander M. Taylor · Cambridge, US
• W. Patrick Walters · Westborough, US
• Mark A. Murcko · Holliston, US
• Fabrizio Giordanetto · New York, US
• Eric Therrien · The Bronx, US
• Sathesh Bhat · Jersey City, US
• Markus Dahlgren · Stratford, US

Key dates

• Filing date: Sep 28, 2018
• Grant date: Dec 20, 2022
• Expiry date: Sep 28, 2038

Classification

• Technology area (CPC —): General

Abstract

Cellular biological activities are tightly controlled by intracellular signaling processes initiated by extracellular signals. Protein tyrosine phosphatases, which remove phosphate groups from tyrosine phosphorylated signaling molecules, play equally important tyrosine roles as protein kinases in signal transduction. SHP-2, a cytoplasmic SH2 domain containing protein tyrosine phosphatase, is involved in the signaling pathways of a variety of growth factors and cytokines. Recent studies have clearly demonstrated that this phosphatase plays an important role in transducing signal relay from the cell surface to the nucleus, and is a critical intracellular regulator in mediating cell proliferation and differentiation.