Merck Sharp + Dohme Corp.

Merck + Co., Inc.

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

Msd International Gmbh

Merck Sharp & Dohme LLC

Msd R&d Co., Ltd.

David L Sloman

David James Witter

Matthew G Stanton

Yongxin Han

Phieng Siliphaivanh

Xianhai Huang

Hongjun Zhang

Derun Li

Hua Zhou

Thomas Allen Miller

Joey Lee Methot

Michelle R Machacek

Nunzio Sciammetta

Anandan Palani

Jongwon Lim

Kevin J Wilson

Solomon D Kattar

Umar Faruk Mansoor

Joseph A Kozlowski

Stephane L Bogen

Christopher W Boyce

Joshua Close

Ryan D Otte

Michael D Altman

Kun Liu

Wensheng Yu

Feroze Ujjainwalla

Thomas H Graham

Raman Kumar Bakshi

Wei Liu

Tesfaye Biftu

Jared N Cumming

Alexander Pasternak

Zhicai Wu

David Joseph Guerin

Purakkattle J Biju

Milana M Maletic

Jianmin Fu

Yimin Qian

Sung-Sau So

Benito Munoz

Yu Wang

Lei Chen

Craig R Gibeau

Christian Fischer

Abdelghani Achab

Michael Hale Reutershan

Xavier Fradera

Indu T Bharathan

Timothy J Henderson

Catherine M White

Matthew Lloyd Childers

Paul A Tempest

Danielle Falcone

Yongqi Deng

Matthew H Daniels

John W Lampe

Wei Zhou

Meredeth Ann McGowan

Min Lu

Pengcheng Patrick Shao

Dann LeRoy Parker, Jr

Francesc Xavier Fradera Llinas

Salem Fevrier

Christopher Hamblett

Liangqin Guo

Wanying Sun

Charles A Lesburg

Richard Wayne Heidebrecht, Jr

Qinglin Pu

Hakan Gunaydin

Min K Park

David Jonathan Bennett

Scott C Berk

Ling Tong

Alan B Northrup

Shuwen He

Guoqing Li

Jason David Katz

Li Xiao

Bing Li

Paul E Harrington

Alessia Petrocchi

James Patrick Jewell

Peter H Fuller

Jonathan B Grimm

Paul Tempest

Dane James Clausen

Sandra Lee Knowles

Brandon Mitsuo Taoka

Ron Ferguson

Jean-Laurent Paparin

Corey E Bienstock

Luis E Torres

Yingchun Ye

Houcine Rahali

Elizabeth Helen Kelley

Kake Zhao

Jed Hubbs

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

The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W, W, Y, Z, M, L, C, C, R, R, R, R, R, R, R, and the subscripts m, n, q, and r are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

Small molecule inhibitors of KRAS G12C mutant

Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

Substituted tetrahydroquinolin compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors

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

Arginase inhibitors and methods of use

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.

Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

Substituted pyrazole compounds as indoleamine 2,3-dioxygenase inhibitors

Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: Formula (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

Substituted tricyclic compounds as indoleamine 2,3-dioxygenase inhibitors

The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W, W, Y, Z, M, L, C, C, R, R, R, R, R, R, Rand the subscripts m, n, q, and r are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

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

Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (I) Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder. 

Substituted phenyl compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors

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

Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

Substituted biaryl compounds as indoleamine 2,3-dioxygenase (IDO) 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 herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof:  Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

Growing community of inventors

Brookline, MA, United States of America

David L Sloman