Tolero Pharmaceuticals, Inc.

Sumitomo Dainippon Pharma Oncology, Inc.

Glaxosmithkline Intellectual Property (No.2) Limited

Michael David Saunders

Koc-Kan Ho

Yong Xu

Xiaohui Liu

Kevin Bret Wright

Kenneth Mark Parnell

Jihua Liu

Steven G Kultgen

Jason Marc Foulks

Scott Albert Pearce

Steven Brian Kanner

Benjamin Gary Brenning

David Lee Vollmer

Thomas Francis Hendrickson

Krzysztof Swierczek

Brian John Stevens

The present invention provides a compound having the following structure: Compositions and methods for using the same in the treatment of skin disorders and other Pim kinase-associated conditions are also disclosed.

Substituted imidazo[1,2-B]pyridazines as protein kinase inhibitors

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

The present invention provides substituted imidazo[1,2-b]pyridazines that are useful as protein kinase inhibitors and have one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R, Rand X are as defined herein. For example, a compound having the following structure:  Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.

The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R, Rand X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.

Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors

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.

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Sandy, UT, United States of America

Michael David Saunders