Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Merck Canada Inc.

Msd K.k.

James Patrick Jewell

Michael D Altman

Ryan D Otte

Andrew M Haidle

Jared N Cumming

Benjamin Wesley Trotter

Jongwon Lim

Min Lu

Alan B Northrup

Tony Siu

Timothy J Henderson

Wonsuk Chang

William K Hagmann

Linus S Lin

Matthew Lloyd Childers

Matthew A Larsen

Brandon D Cash

Shrenik K Shah

Ping Liu

Rui Liang

Jason David Katz

Quang T Truong

Solomon D Kattar

Ravindra N Guthikonda

Brian M Andresen

Linda L Chang

John Michael Ellis

Christian Fischer

Sandra Lee Knowles

Brandon Mitsuo Taoka

Thomas J Lanza, Jr

Anthony Donofrio

Sriram Tyagarajan

Hongbo Qi

Helen M Armstrong

Mark T Goulet

Maria Emilia Di Francesco

Duane E DeMong

Shawn P Walsh

Corey E Bienstock

Graham Frank Smith

Kake Zhao

Adam J Schell

Scott Peterson

Denis Deschenes

Hua Zhou

Matthew G Stanton

Amjad Ali

Christopher J Dinsmore

Qun Dang

John S Wai

David L Sloman

Michelle R Machacek

Jonathan R Young

Hong Liu

David Joseph Guerin

Joon Jung

Michael Hale Reutershan

Charles A Lesburg

John W Butcher

Matthew Christopher

Satoru Ito

Jason Burch

David Jonathan Bennett

Marc Blouin

Kaleen Konrad Childers

Kerrie Spencer

Joel S Robichaud

Rachel Nicola MacCoss

H Donald Burns

Raymond E Gibson

Terence G Hamill

Alex Minhua Chen

Njamkou Noucti

Andrey V Peresypkin

Ana Esther Gabarda Ortega

Brandon M Taoka

Yongquan Hou

Andrew Marc Haidle

Sandra L Knowles

Corey Bienstock

Kerrie B Spencer

Alan B Northhrup

Core E Bienstock

Scott L Peterson

Ana Esther Ortega Gabarda

Thomas J Lanza

Compounds of general formula (I), and their pharmaceutically acceptable salts, wherein R, R, R, R, R, R, R, A, X, X, and Xare defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.

Aza-benzothiophene compounds as STING agonists

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

Oxo-tetrahydro-isoquinoline carboxylic acids as STING inhibitors

Compounds of general formula (I), of general formula (II), of general formula (III), of general formula (IV), of general formula (V), of general formula (VI), and their pharmaceutically acceptable salts, wherein all variables are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer. 

Sting agonist compounds

A class of polycyclic compounds of general formula (I), of general formula (I'), or of general formula (I&#x2033;), wherein Base, Base, Y, Y, X, X, X, X, X, X, X, X, R, R, R, R, R, R, R, R, R, R, R, R, R, and Rare defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds. 

Cyclic di-nucleotide compounds as sting agonists

Cyclic di-nucleotide compounds as STING agonists

A class of polycyclic compounds of general formula (II), of general formula (II'), or of general formula (II&#x2033;), wherein Base, Base, Y, Y, X, X, X, X, X, X, X, X, R, R, R, R, R, R, R, R, R, R, R, R, R, and Rare defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds. 

Compounds of general formula (Ia), compounds of general formula (Ia'), compounds of general formula (Ib), compounds of general formula (Ib&#x2032;), compounds of general formula (I), compounds of general formula (I&#x2032;), and their pharmaceutically acceptable salts, wherein R, R, R, R, R, R, R, R, X, X, and Xare defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds of the disclosure.

Benzo[b]thiophene compounds as STING agonists

Benzo[b]thiophene compounds as sting agonists

The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R, R, R, R, R, C, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase. 

Substituted pyridine spleen tyrosine kinase (SYK) inhibitors

The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase. 

2-Pyridyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors

The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer.

Bipyridylaminopyridines as Syk inhibitors

The invention encompasses pyrazolo[1,5-a]pyridine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.

Pyrazolo[1,5-a]pyridines as MARK inhibitors

The present invention relates to pyrazolopyridines and imidazopyridines which are inhibitors of the kinase PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. The compounds are also useful as inhibitors of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. Furthermore, the present compounds also selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease.

Therapeutic compounds

The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-]pyridine compounds, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Benzocycloheptapyridines as inhibitors of the receptor tyrosine kinase MET

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Newton, MA, United States of America

James Patrick Jewell