Merck Sharp + Dohme Corp.

Matthew A Larsen

Jared N Cumming

Andrew M Haidle

Brandon D Cash

Michael D Altman

Duane E DeMong

Ryan D Otte

James Patrick Jewell

Benjamin Wesley Trotter

Min Lu

Amjad Ali

Kun Liu

Jongwon Lim

Ping Liu

Thomas H Graham

Umar Faruk Mansoor

Timothy J Henderson

Qiaolin Deng

Yonglian Zhang

Huijun Wang

Rui Liang

Tony Siu

Christopher W Plummer

Wonsuk Chang

Jianping Pan

Sriram Tyagarajan

Elisabeth Hennessy

Uma Swaminathan

Aaron Sather

Andrew J Hoover

Phieng Siliphaivanh

Rongze Kuang

Matthew Lloyd Childers

Charles A Lesburg

Yeon-Hee Lim

Catherine M White

Brandon Mitsuo Taoka

Quang T Truong

Qinglin Pu

Brett A Hopkins

Wenlang Fu

Gioconda V Gallo-Etienne

Sulagna Sanyal

Xin Yan

Zachary G Brill

Brandon A Vara

Meredeth A Mcgowan

Duane Demong

Jesus Moreno

George Madalin Giambasu

James P Jewell

Jared Cumming

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

In its many embodiments, the present invention provides certain substituted amino triazolopyrimidine and amino triazolopyrazine compounds of Formula (IA) and Formula (IB): and, and pharmaceutically acceptable salts thereof, wherein, R, n, R, and Rare as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use

In its many embodiments, the present invention provides certain 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives of Formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A, R1, R2, and R4 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutic agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

7-, 8-, and 10-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use

In its many embodiments, the present invention provides certain 9-substituted amino triazolo quinazoline compounds of the structural Formula (I): and pharmaceutically acceptable salts thereof, wherein, ring A, Rand Rare as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2and/or A2receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2receptor and/or the adenosine A2receptor.

9-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use

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

In its many embodiments, the present invention provides certain 9-substituted amino triazolo quinazoline compounds of the structural Formula (I): and pharmaceutically acceptable salts thereof, wherein, ring A, Rand Rare as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

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

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

Growing community of inventors

Dedham, MA, United States of America

Matthew A Larsen