Glaxosmithkline Intellectual Property (no.2) Limited

Glaxosmithkline LLC

Charles William Blackledge, Jr

William Henry Miller

Stuart Paul Romeril

Kenneth Allen Newlander

Steven David Knight

Juan I Luengo

Neil W Johnson

Joelle Lorraine Burgess

Xinrong Tian

Jiri Kasparec

Mark James Schulz

Dai-Shi Su

Louis V LaFrance, Iii

Jeffrey Michael Axten

Seth Wilson Grant

Yanhong Feng

Jesus Raul Medina

Gerald Patrick Brady, Jr

Yanhoug G Feng

Jesus Rahul Medina

This invention relates to novel compounds according to Formula (III)(a) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), and to pharmaceutical compositions containing them. 

Enhancer of zeste homolog 2 inhibitors

This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers. 

The invention is directed to 6-(4-pyrimidinyl)-1H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R-Rare defined herein. The compounds of the invention axe inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. 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 PDK1 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

Growing community of inventors

Collegeville, PA, United States of America

Charles William Blackledge, Jr