Merck Sharp + Dohme Corp.

Osi Pharmaceuticals, Inc.

Merck + Co., Inc.

Merck Hdac Research, LLC

Prosidion Limited

Msd R&d (china) Co., Ltd.

Msd International Gmbh

Ctxt Pty Limited

Msd R&d Co., Ltd.

David James Witter

Thomas Allen Miller

Phieng Siliphaivanh

Arlindo Lucas Castelhano

David L Sloman

Kevin J Wilson

Bryan McKibben

Xianhai Huang

Matthew G Stanton

Joey Lee Methot

Christopher W Boyce

Joseph A Kozlowski

Jongwon Lim

Sandro Belvedere

Hua Zhou

Michelle R Machacek

Solomon D Kattar

Milana M Maletic

Michael Hale Reutershan

Umar Faruk Mansoor

Raman Kumar Bakshi

Jianmin Fu

Paul E Harrington

Wei Liu

Tesfaye Biftu

Michael D Altman

Christopher J Dinsmore

Stephane L Bogen

Philip Jones

Yimin Qian

Yu Wang

Lei Chen

Wei Zhou

Kathryn Ann Lipford

Danielle Falcone

Joshua Close

Matthew H Daniels

Jonathan B Grimm

Salem Fevrier

Brendan O'Boyle

Chunhui Huang

Jiaming Yan

David Joseph Guerin

Purakkattle J Biju

Jason David Katz

Joon Jung

Abdelghani Achab

Craig R Gibeau

Xavier Fradera

Catherine M White

Christian Fischer

Paul Tempest

John W Lampe

Matthew Christopher

Meredeth Ann McGowan

Shimin Xu

Min K Park

Yingchun Ye

Alexey A Rivkin

Christopher Hamblett

Jed Hubbs

Chaomin Li

Hongjun Zhang

Feroze Ujjainwalla

Ling Tong

Zhicai Wu

Paul Anthony Stupple

Ryan D Otte

Martin James Procter

Nunzio Sciammetta

Bing Li

Alessia Petrocchi

Timothy J Henderson

Douglas S Werner

Matthew Lloyd Childers

Mark E Scott

John W Butcher

Peter H Fuller

Richard Wayne Heidebrecht, Jr

Paul A Tempest

Qinglin Pu

Matthew Colin Thor Fyfe

Kosuke Yasuda

Ron Ferguson

Jean-Laurent Paparin

Dann LeRoy Parker, Jr

Corey E Bienstock

Pengcheng Patrick Shao

Francesc Xavier Fradera Llinas

Brandon D Cash

Elizabeth Helen Kelley

Houcine Rahali

Kake Zhao

Hyun Chong Woo

Geoffrey Martyn Williams

Scott Peterson

Shuyi Tang

June J Kim

Alexander J Kim

The present invention provides a compound of Formula (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.

PRMT5 inhibitors

The present invention provides a compound of Formula (I) Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.

The instant invention provides compounds of formulas Ia and Ib which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer. 

Purine inhibitors of human phosphatidylinositol 3-kinase delta

The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.

The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors. 

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I).

Compounds that are ERK inhibitors

The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers. 

Tricyclic compounds as inhibitors of mutant IDH enzymes

The present invention is directed to tricyclic compounds of formula (I), (Ia) or (Ib) which are inhibitors of one or more mutant IDH enzymes. The present invention is also directed to uses of these tricyclic compounds in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers. 

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). 

The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a method of inhibiting ERK2 in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of Formula (I). The invention also provides a method for treating cancer in a patient in need of such treatment, said method comprising administering to said patient an effective amount of at least one compound of Formula (I). 

ERK inhibitors

The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. 

Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I). 

Disclosed are the ERK inhibitors of formula (1.0) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0). This invention provides compounds that are ERK inhibitors (i.e., ERK2 inhibitors). This invention also provides a pharmaceutical composition comprising an effective amount of at least one (e.g., 1) compound of formula (1.0) and a pharmaceutically acceptable carrier.

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1). 

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Norfolk, MA, United States of America

David James Witter