Heteroaryl sulfone-based conjugation handles, methods for their preparation, and their use in synthesizing antibody drug conjugates

US11712480B2 · kind B2 · utility

Assignee

• PFIZER INC. · US

Inventors

• Russell Dushin · Old Lyme, US
• Daniel Paul Uccello · Colchester, US
• Jeremy Tyson Starr · Ann Arbor, US
• Ye Che · Groton, US
• Mark E. Flanagan · Gales Ferry, US
• Jeffrey M. Casavant · Franklin, US
• Christopher John O'Donnell · Mystic, US
• Gary Filzen · Ann Arbor, US
• Jennifer Young · Los Alamos, US
• Joseph Alan Abramite · Mystic, US
• Lawrence Nathan Tumey · Fairview Park, US
• Ludivine Moine · Cambridge, US
• Adam Matthew Gilbert · Congers, US
• Lee Richard Roberts · Chatham, GB

Key dates

• Filing date: Jul 31, 2017
• Grant date: Aug 1, 2023
• Expiry date: Dec 2, 2039

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K7/02
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention is directed to novel heteroaryl sulfone-based conjugation handles of the formula: (wherein R1, R2, Het, D, E, X, Y, Z, m, n, p, q, r, s and t are as defined herein), methods for their preparation, their use in synthesizing antibody drug conjugates, and the resulting antibody drug conjugates made with components having heteroaryl sulfone-based conjugation handles.