Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Lycera Corporation

Foghorn Therapeutics Inc.

Enko Chem, Inc.

Revolution Medicines, Inc.

Warp Drive Bio, Inc.

Merck Canada Inc.

Neville J Anthony

Kenneth Jay Barr

John S Wai

Samuel L Graham

Gerald E Stokker

Steven D Young

Nunzio Sciammetta

S Jane deSolms

Theresa M Williams

Christopher J Dinsmore

Hongjun Zhang

Richard Thomas Beresis

Gregory Lawrence Verdine

Michael D Altman

Thomas Daniel Aicher

Kun Liu

Michael R Wood

Hua Zhou

William L Thomas

Scott D Kuduk

John Howard Hutchinson

Mark G Bock

Ian M Bell

Thomas Allen Miller

Shawn E R Schiller

Solomon D Kattar

Jason David Katz

Philip Jones

Melissa S Egbertson

Robert L Smith

Alan B Northrup

Thomas Joseph Tucker

Joey Lee Methot

Michelle R Machacek

Rong Zhang

George D Hartman

Lihu Yang

Linghang Zhuang

Timothy J Guzi

William C Lumma, Jr

Wasyl Halczenko

Scott D Edmondson

Dong-Ming Shen

Jason D Brubaker

Daniel Guay

Douglas C Beshore

Anthony W Shaw

David Joseph Guerin

Cheng Zhu

Gregori J Morriello

Robert P Gomez

Blair T Lapointe

John K MacLean

Brian M Andresen

Corey E Bienstock

Yuan Liu

Dai-Shi Su

Matthew H Daniels

Catherine M White

Chad A VanHuis

Vladimir Simov

Rishi G Vaswani

Mark E Scott

Mark W Embrey

Meredeth Ann McGowan

Terrence M Ciccarone

Kin Chiu Fong

Thorsten E Fisher

Yuan Tian

Joon Jung

Abdelghani Achab

Yongqi Deng

Christopher Francis Thompson

Jeffrey M Bergman

Feng Shi

Dong-Mei Feng

Matthew Christopher

Ta-Jyh Lee

John T Sisko

Francesc Xavier Fradera Llinas

Lekhanh O Tran

Raman Kumar Bakshi

Jianmin Fu

Alessia Petrocchi

John Michael Ellis

Qiaolin Deng

Jonathan B Grimm

Benjamin Wesley Trotter

Liping Wang

Brandon Mitsuo Taoka

Lehua Chang

Wei Xu

Anthony Donofrio

Kaleen Konrad Childers

James P Guare

Kerrie Spencer

Liping Yang

Catherine M Wiscount

Nam Fung Kar

Michelle Martinez

The compounds disclosed herein may be inhibitors of BRG1 (Brahma-related gene-1) and/or BRM (Brahma). The compounds or pharmaceutically acceptable salts thereof are useful for the treatment of disorders associated with an alteration in a BAF complex, e.g., a disorder associated with an alteration in one or both of the BRG1 and BRM proteins. Also disclosed are pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and methods of their preparation and use.

BRM/BRG1 inhibitors and uses thereof

The present disclosure features compounds useful for the treatment of BAF complex-related disorders.

Compounds and uses thereof

The present invention relates to protoporphyrinogen IX oxidase (PPO) inhibitors of the general formula (I) where the variables are defined herein. The invention features processes and intermediates for preparing the compounds of formula (I), compositions comprising them, and their use as herbicides—e.g., for controlling harmful plants. The invention also features methods for controlling unwanted vegetation comprising allowing an herbicidal effective amount of at least one PPO inhibitor of formula (I) to act on plants, their seed, and/or their habitat.

Protoporphyrinogen oxidase inhibitors

The present invention relates to protoporphyrinogen oxidase inhibitors of the general formula (I) where the variables are defined herein. The invention features processes and intermediates for preparing the benzoxazinones of formula (I), compositions comprising them, and their use as herbicides&#x2014;i.e. for controlling harmful plants. The invention also features methods for controlling unwanted vegetation comprising allowing an herbicidal effective amount of at least one benzoxazinone of formula (I) to act on plants, their seed, and/or their habitat.

The present disclosure provides methods and reagents useful for analyzing protein-protein interfaces such as interfaces between a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein. In some embodiments, the target and/or presenter proteins are intracellular proteins. In some embodiments, the target and/or presenter proteins are mammalian proteins.

Methods and reagents for analyzing protein-protein interfaces

The invention provides certain bicylic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X, X, R, R, R, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT. 

Tetrahydronaphthyridine, benzoxazine, aza-benzoxazine and related bicyclic compounds for inhibition of RORgamma activity and the treatment of disease

The invention provides certain bicyclic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X, X, R, R, R, R, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT. 

The present invention relates to compounds according to Formula I (Formula I), and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions. 

4-heteroaryl substituted benzoic acid compounds as RORgammaT inhibitors and uses thereof

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. 

Purine inhibitors of human phosphatidylinositol 3-kinase delta

The invention relates to macrocyclic compounds capable of modulating biological processes through binding to a presenter protein and a target protein. These compounds bind endogenous intracellular presenter proteins, such as the FKBPs or cyclophilins, and the resulting binary complexes selectively bind and modulate the activity of intracellular target proteins. Formation of a tripartite complex among the presenter protein, the compound, and the target protein is driven by both protein-compound and protein-protein interactions, and both are required for modulation of the targeted protein's activity. In some embodiment, the compounds of the invention 're-program' the binding of the presenter proteins to protein targets that either do not normally bind to the presenter protein.

Compounds that participate in cooperative binding and uses thereof

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. 

Growing community of inventors

Hatfield, PA, United States of America

Neville J Anthony