Merck Sharp + Dohme Corp.

Scynexis, Inc.

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

Msd International Gmbh

Merch Sharp & Dohme Ltd

Msd R&d Co., Ltd.

Phieng Siliphaivanh

David James Witter

Kevin J Wilson

Xianhai Huang

Joey Lee Methot

Christopher W Boyce

David L Sloman

Jongwon Lim

Wei Zhou

Thomas Allen Miller

Joseph A Kozlowski

Umar Faruk Mansoor

Milana M Maletic

Anandan Palani

Matthew G Stanton

Yongxin Han

Robert G Aslanian

Kevin D McCormick

Hongjun Zhang

Hua Zhou

Michelle R Machacek

Solomon D Kattar

Joshua Close

Raman Kumar Bakshi

Purakkattle J Biju

Wei Liu

Jianmin Fu

Yimin Qian

Brian Alexander McKittrick

Michael D Altman

Benito Munoz

Yu Wang

Lei Chen

Salem Fevrier

Christian Fischer

Matthew H Daniels

Kerrie Spencer

Jason D Brubaker

Michael Hale Reutershan

Jonathan B Grimm

Dong Xiao

Younong Yu

David Joseph Guerin

Robert D Mazzola, Jr

Joon Jung

Paul E Harrington

Craig R Gibeau

Ashwin Umesh Rao

Catherine M White

Richard Wayne Heidebrecht, Jr

Qin Jiang

Corey E Bienstock

Yingchun Ye

Jun Qin

Luis E Torres

James M Balkovec

Alan B Cooper

Joseph Michael Kelly

Ying Huang

Ling Tong

Peter D Williams

Gerald Wayne Shipps, Jr

Ping Liu

Jonathan R Young

Andrew M Haidle

Jason David Katz

Jing Su

Thomas S Reger

Abdelghani Achab

Alessia Petrocchi

Yongqi Deng

Tony Siu

Xiaolei Gao

Timothy J Henderson

Xiao Chen

Charles A Lesburg

John W Butcher

Matthew Lloyd Childers

John P Caldwell

Xavier Fradera

Matthew Christopher

Frances A Bouffard

Jayaram R Tagat

Paul Tempest

Binyuan Sun

Haiqun Tang

Qinglin Pu

Erin F DiMauro

Hakan Gunaydin

Ron Ferguson

Paul A Tempest

Jean-Laurent Paparin

Sobhana Babu Boga

Catherine M Wiscount

Hugh Y Zhu

Matthew A Larsen

Brandon D Cash

Liang Zhu

Xiaohua Huang

Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as IL4I1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for IL4I1-related diseases.

IL4I1 inhibitors and methods of use

The present invention provides a compound of Formula (I) (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

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene Breceptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene Breceptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Nonalcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.

Aryl sulfonamides as BLT1 antagonists

Described herein are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein A, R, R, R, W, X, Y, Z, m, n and p are as defined herein. The compounds of Formula I act as RIPK1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for RIPK1-related diseases.

Spirotricycle RIPK1 inhibitors and methods of uses thereof

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.

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

The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors. 

KDM5 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

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene Breceptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene Breceptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer. 

Aryl acylsulfonamides as BLT1 antagonists

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene Breceptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene Breceptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatoepatitis, metabolic syndrome, atherosclerosis, and cancer. 

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). 

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Newton, MA, United States of America

Phieng Siliphaivanh