Compounds that participate in cooperative binding and uses thereof

US10533016B2 · kind B2 · utility

Assignee

• Revolution Medicines, Inc. · US

Inventors

• Gregory L. Verdine · Boston, US
• Brian Roger Bowman · New Rochelle, US
• Mathew Edward Sowa · Watertown, US
• Joshua Alan Van Dyke Blodgett · Webster Groves, US
• Keith E. Robison · Wilmington, US
• Dylan Talbot Stiles · Cambridge, US
• Jay P. Morgenstern · Boston, US
• Sharon Ann Townson · Somerville, US
• Uddhav Kumar Shigdel · Cambridge, US

Key dates

• Filing date: Jan 8, 2016
• Grant date: Jan 14, 2020
• Expiry date: Jan 8, 2036

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention features compounds (e.g., macrocyclic compounds) capable of modulating biological processes, for example through binding to a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein such as CEP250. These compounds bind endogenous intracellular presenter proteins, such as the FKBPs or cyclophilins, and the resulting binary complexes selectively bind and modulate the activity of the target protein. Formation of a tripartite complex among the presenter protein, the compound, and the target protein is driven by both protein-compound and protein-protein interactions, and both are required for modulation of target protein activity.