Smithkline Beecham Corporation

Glaxosmithkline LLC

Glaxo Group Limited

Affinium Pharmaceuticals, Inc.

Glaxosmithkline Intellectual Property (no.2) Limited

The Dupont Merck Pharmaceutical Company

Glaxosmithkline Intellectual Property Development Limited

Cancer Research Technology Limited

Dupont Pharmaceuticals Company

Vitae Pharmaceuticals, Inc.

Syndax Pharmaceuticals, Inc.

William Henry Miller

Mark Andrew Seefeld

Kenneth Allen Newlander

Irene Nijole Uzinskas

Meagan B Rouse

Xinrong Tian

Steven David Knight

Stuart Paul Romeril

Neil W Johnson

Dalia R Jakas

Sharad Kumar Verma

William Edward Bondinell

Joelle Lorraine Burgess

Jeffrey Michael Axten

William F Huffman

Neil David Pearson

Richard McCulloch Keenan

Israil Pendrak

Walter E Dewolf, Jr

Chet Kwon

Robert A Daines

Louis Lafrance

Walter J Burgess

Timothy Francis Gallagher

Juan I Luengo

Peter J Manley

Graham Elgin Jones

David Thomas Davies

Fadia E Ali

Patricia C Weber

James Martin Samanen

Jiri Kasparec

Ryan Michael Fox

Eugene Cruz Amparo

Gregory James Pacofsky

Seth Wilson Grant

Charles William Blackledge, Jr

Dominic Suarez

Pui Yee Ng

Robert B Perni

John Wityak

Charles A Blum

John J Duncia

Kevin J Duffy

Richard Dana Caldwell

Thomas Wen-Fu Ku

Jeremy S Disch

Bruce G Szczepankiewicz

Antony N Shaw

Russell Donovan Cousins

Brian H White

Christopher Oalmann

Karsten Koppetsch

Rebecca L Casaubon

Mark James Schulz

James Brackley, Iii

Dai-Shi Su

Louis Vincent Lafrance, Iii

Andrea K Myers

Michael N Zimmerman

Karen Anderson Evans

Louis V LaFrance, Iii

Celine Duquenne

James Francis Callahan

Santosh Shripad Kulkarni

Joseph B Santella

John Matthew Fevig

Salvacion Cacatian

Julie Nicole Hamblin

Roger Edward Markwell

Robert A Galemmo, Jr

Allan Michael Jordan

Dirk Andries Heerding

Matthew M Abelman

Nicholas D Adams

Joseph Cacciola

Bryan Wayne King

Matthew Campbell

Bohdan Waszkowycz

Kenneth David Down

Joseph W Venslavsky

Andrew B Benowitz

Stanley J Schmidt

Alan T Price

Thomas The Nguyen

Mei Li

David T Fosbenner

Alexander Joseph Reif

Robert M Knabb

Tobias Oregon Yellin

M Amparo Lago

Yanhong Feng

Sophie Marie Bertrand

Carla A Donatelli

Raul Rolando Calvo

Thomas Wen Fu Ku

Jesus Raul Medina

Roger J Butlin

Kristin M Goldberg

The present disclosure is directed to inhibitors of Formula (0), or a stereoisomer thereof, or pharmaceutically acceptable salt thereof, of the interaction of menin with MLL and MLL fusion proteins, pharmaceutical compositions containing the same, and their use in the treatment of cancer and other diseases mediated by the menin-MLL interaction,

Inhibitors of the menin-MLL interaction

The invention is directed to compounds of formula (I), and salts thereof. The compounds are inhibitors of kinase activity, in particular PI3-kinase activity. 

Oxepinopyrazole derivatives as inhibitors of P13-kinase activity

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

The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

Substituted bridged urea analogs as sirtuin modulators

The present invention relates to novel substituted bridged urea analog compounds of Formula (I) or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, processes for making and use of such compounds, alone or in combination with other therapeutic agents, as Sirtuin Modulators useful for increasing lifespan of a cell, and in treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity.

The present invention relates to novel substituted bridged urea compounds of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

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

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

Indoles

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. 

Enhancer of Zeste Homolog 2 inhibitors

This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.

Cyclopropylamines as LSD1 inhibitors

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

Azaindazoles

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

Indazoles

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Collegeville, PA, United States of America

William Henry Miller