Harvard College

Pfizer Corporation

Other

Daniel Jonathan Smaltz

Andrew G Myers

Kentaro Futatsugi

Kevin James Filipski

David James Edmonds

Michelle Renee Garnsey

Jakub Svenda

Nicholas E Hill

Robert T Yu

Jack Chang Hung Lee

Thomas Magauer

Andreas Schumacher

Thomas Maguer

Described herein are compounds of Formula (I) wherein R, R, R, R, R, R, R, Rand Rare defined herein, their use as diacylglycerol acyltransferase 2 (DGAT2) inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, NASH.

Diacylglycerol acyl transferase 2 inhibitor

Provided herein are trioxacarcin-antibody drug conjugates of Formula (A): and pharmaceutically acceptable salts thereof, comprising at least one instance of the group -L-(A-L)-B attached thereto, wherein a is an integer between 1 and 10, inclusive, Lis absent or is a linking group, A is a moiety formed from the reaction of two complimentary groups (X and Y), Lis absent or is another linking group, and B is an antibody or antibody fragment. Also provided are methods of preparing these antibody-drug conjugates, pharmaceutically acceptable compositions thereof, and methods of their use and treatment. Further provided are precursors to the trioxacarcin-antibody drug conjugates, novel trioxacarcins without an antibody conjugated thereto, pharmaceutical compositions thereof, and methods of their use and treatment.

Trioxacarcins, trioxacarcin#antibody conjugates, and uses thereof

Provided herein are trioxacarcin-antibody drug conjugates of Formula (A): and pharmaceutically acceptable salts thereof, comprising at least one instance of the group -L-(A-L)a-B attached thereto, wherein a is an integer between 1 and 10, inclusive, Lis absent or is a linking group, A is a moiety formed from the reaction of two complimentary groups (X and Y), Lis absent or is another linking group, and B is an antibody or antibody fragment. Also provided are methods of preparing these antibody-drug conjugates, pharmaceutically acceptable compositions thereof, and methods of their use and treatment. Further provided are precursors to the trioxacarcin-antibody drug conjugates, novel trioxacarcins without an antibody conjugated thereto, pharmaceutical compositions thereof, and methods of their use and treatment. 

Trioxacarcins, trioxacarcin-antibody conjugates, and uses thereof

The present invention relates to trioxacarcin compounds of the formula: or pharmaceutically acceptable forms thereof; wherein R, R, R, R, R, R, R, R, and Rare as defined herein. The present invention also provides processes for preparing such compounds and intermediates thereto; pharmaceutical compositions comprising such compounds; and methods of use and treatment.

Trioxacarcins and uses thereof

The present invention relates to trioxacarcin compounds of the formula: (I) or pharmaceutically acceptable forms thereof; wherein R, R, R, R, R, R, R, R, and Rare as defined herein. The present invention also provides processes for preparing such compounds and intermediates thereto; pharmaceutical compositions comprising such compounds; and methods of use and treatment. 

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Cambridge, MA, United States of America

Daniel Jonathan Smaltz