Smithkline Beecham Corporation

Glaxosmithkline LLC

Other

Glaxosmithkline Intellectual Property (no.2) Limited

Glaxo Group Limited

Cancer Research Technology Limited

Glaxosmithkline Intellectual Property Development Limited

Ligand Pharmaceuticals, Inc.

Nps Pharmaceuticals, Inc.

Juan I Luengo

Kevin J Duffy

John Duncan Elliott

Julian Jenkins

Connie L Erickson-Miller

Antony N Shaw

Sophie Visonneau

Jia-Ning Xiang

William Henry Miller

Dennis Alan Holt

Stuart Paul Romeril

Ralph A Rivero

Stephen F Miller

Kenneth Wiggall

Mark James Schulz

Alan T Price

John G Gleason

Kenneth Allen Newlander

Steven David Knight

Neil W Johnson

Joelle Lorraine Burgess

Xinrong Tian

Jiri Kasparec

Dennis Shinji Yamashita

Allan Michael Jordan

Manuel F Balandrin

Leonard Walter Rozamus, Jr

Rosanna Tedesco

Hong Lin

Charles William Blackledge, Jr

Dai-Shi Su

Louis V LaFrance, Iii

Nicholas D Adams

Bryan Wayne King

Junya Qu

Bohdan Waszkowycz

Stanley J Schmidt

Andrew B Benowitz

James A Chan

Alexander Joseph Reif

David T Fosbenner

Mei Li

Irina V Shcherbakova

Michael Lee Moore

Stephen G Miller

Karen Anderson Evans

Hongyi Yu

Ann L Breen

Guangfei Huang

Peter I Lamb

Nannan Liu

Wenyong Wang

Ali Raoof

Christopher S Kershaw

Kristin M Goldberg

Roger J Butlin

María Lourdes Rueda Benede

Ren Xie

Jin Zeng

Manuel F Balanddrin

Otto Geoffroy

John Fox

Robert Marquis

Lihua Zhang

Daniel F Eppley

Jr Charles William Blackledge

Louis V Lafrance Iii

The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): wherein Y, X, X, R, R, R, Rand Rare as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. 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 DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Substituted pyridines as inhibitors of DNMT1

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. 

PI3K&#x3b2; selective compounds having the structure 

Pyrazolopyrimidine derivatives as PI3 kinase inhibitors

This invention relates to the use of benzimidazole boronic acid derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3' OH kinase family (hereinafter PI3 kinases), suitably, PI3K&#x3b1;, PI3K&#x3b4;, PI3K&#x3b2;, and/or PI3K&#x3b3;. Suitably, the present invention relates to the use of benzimidazole boronic acids in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K&#x3b2; selective benzimidazole boronic acid compounds for treating cancer.

Benzimidazole boronic acid derivatives as PI3 kinase inhibitors

This invention relates to novel compounds of formula (I): and derivatives thereof useful for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3' OH kinase family (hereinafter PI3 kinases), suitably, PI3K&#x3b1;, PI3K&#x3b4;, PI3K&#x3b2;, and/or PI3K&#x3b3;.

Thiazolopyrimidinone derivatives as PI3 kinase inhibitors

Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.

Thrombopoietin mimetics

The pyrimidinone compounds are disclosed. Methods of preparing the pyrimidinone compounds are also disclosed.

Pyrimidinone compounds as calcilytics

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Audubon, PA, United States of America

Juan I Luengo