Pfizer Corporation

Jeffrey Michael Casavant

Chakrapani Subramanyam

Andreas Maderna

Zecheng Chen

Christopher John O'Donnell

Lawrence Nathan Tumey

Matthew David Doroski

Hud Lawrence Risley

Alexander M Porte

Christopher John O'donnell

Mark Edward Flanagan

Adam Matthew Gilbert

Russell Dushin

Ye Che

Lee Richard Roberts

Daniel Paul Uccello

Jeremy Tyson Starr

Gary Frederick Filzen

Joseph Alan Abramite

Ludivine Moine

Jennifer Young

Joseph A Abramite

Jeremy Starr

Daniel P Uccello

The present invention is directed to novel heteroaryl sulfone-based conjugation handles of the formula: (wherein R, R, 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.

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

The present invention is directed to novel bifunctional CTI-CTI and CBI-CTI dimers of the formula:F-L-T-L-Fwhere F, L, T, Land Fare as defined herein, useful for the treatment for proliferative diseases, where the inventive dimers can function as stand-alone drugs, payloads in antibody-drug-conjugates (ADCs), and linker-payload compounds useful in connection with the production or administration of such ADCs; and to compositions including the aforementioned dimers, linker-payloads and ADCs, and methods for using these dimers, linker-payloads and ADCs, to treat pathological conditions including cancer.

Bifunctional cytotoxic agents containing the CTI pharmacophore

Cytotoxic dimers comprising CBI-based and/or CPI-based sub-units, antibody drug conjugates comprising such dimers, and to methods for using the same to treat cancer and other conditions.

Bifunctional cytotoxic agents

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Franklin, CT, United States of America

Jeffrey Michael Casavant