Glaxosmithkline LLC

Seth Wilson Grant

Stuart Paul Romeril

William Henry Miller

Kenneth Allen Newlander

Steven David Knight

Neil W Johnson

Joelle Lorraine Burgess

Meagan B Rouse

Jeffrey Michael Axten

Xinrong Tian

Sharad Kumar Verma

James Brackley, Iii

Dirk Andries Heerding

Jun Tang

Louis Lafrance

Yanhong Feng

Charles William Blackledge, Jr

Louis Vincent Lafrance, Iii

Jesus Raul Medina

Jesus Rual Medina

Gerald Patrick Brady, Jr

Yanhoug G Feng

Jesus Rahul Medina

Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.

Indoles

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

The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R, R, and Rare defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, 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 PERK 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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Collegeville, PA, United States of America

Seth Wilson Grant