Tolero Pharmaceuticals, Inc.

Glaxosmithkline Intellectual Property (no.2) Limited

Sumitomo Dainippon Pharma Oncology, Inc.

Kevin Bret Wright

Koc-Kan Ho

Michael David Saunders

Yong Xu

Jihua Liu

Xiaohui Liu

Kenneth Mark Parnell

Jason Marc Foulks

Steven Brian Kanner

David Lee Vollmer

Scott Albert Pearce

Thomas Francis Hendrickson

Krzysztof Swierczek

Brian John Stevens

Micheal David Saunders

Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R, R, R, R, Rand Rare as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

PKM2 modulators and methods for their use

Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

The invention is directed to substituted heteroaryl derivatives. Specifically, the invention is directed to compounds according to Formula Q: wherein D, L, M, W, X, Y, and Z are defined herein. The compounds of the invention are inhibitors of DNA methyltransferase (DNMT) activity&#x2014;including DNMT1, DNMT3a, or DNMT3b&#x2014;and are useful in the treatment of cancer and hyperproliferative diseases. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Chemical compounds

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Cottonwood Heights, UT, United States of America

Kevin Bret Wright