Purdue Pharma L.p.

Venatorx Pharmaceuticals, Inc.

Shionogi Company Limited

Other

Jiangchao Yao

Laykea Tafesse

Bin Shao

Naoki Tsuno

Chiyou Ni

Xiaoming Zhou

Christopher J Burns

Steven Armen Boyd

Jianming Yu

R Richard Goehring

Bin Liu

Mark Andrew Youngman

Jae Hyun Park

Minnie Park

Kouki Fuchino

Donald Kyle

Stephen M Condon

Jeffrey Lockman

Glen Coburn

Christopher Benetatos

Yoshiyuki Taoda

Zhengming Chen

Denis Daigle

John W F Whitehead

John William Frank Whitehead

Thomas Haimowitz

Stephen Matthew Lynch

Kenji Yamawaki

Akira Matsumura

Nobuyuki Tanaka

Donald J Kyle

Khondaker Islam

Hidenori Mikamiyama

Eugen F Mesaros

Guo-Hua Chu

Randy W Jackson

Jodie Hamrick

Richard R Goehring

Matthew Lucas

Mark Youngman

Mark A Youngman

The Invention provides indole derivatives of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R, R, A, X, Y, Z, and Ware defined as set forth in the specification. The Invention also provides the use of compounds of Formula I and the pharmaceutically acceptable salts and solvates thereof to treat pain. In certain embodiments, the Compounds of the Invention are effective in treating a disorder responsive to blockade of one or more sodium channels.

Indole derivatives and use thereof

Described herein are hepatitis B capsid assembly modulators and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of hepatitis B.

Hepatitis B capsid assembly modulators

Described herein are certain boron-containing compounds, compositions, preparations and their use as modulators of the transpeptidase function of bacterial penicillin-binding proteins and as antibacterial agents. In some embodiments, the compounds described herein inhibit penicillin-binding proteins. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Penicillin-binding protein inhibitors

The invention relates to Substituted-Quinoxaline-Type Bridged-Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound.

Pharmaceutical salts of substituted-quinoxaline-type bridged-piperidine compounds

Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Beta-lactamase inhibitors

The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A, X, A, W, W, W, E, Z, and Rare defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain. 

Pyrimidines as sodium channel blockers

Compounds of Formula (I): where R, R, R, a, and b are disclosed herein, and pharmaceutically acceptable derivatives thereof, compositions thereof, and methods to treat or prevent a condition (such as pain) thereof. The disclosure also provides compounds of formula QB or O2 and their utility in manufacture processes in obtaining compounds of Formula (I).

9'-Aza[3,9&#x2032;-bi(bicyclo[3.3.1]nonan)]-3&#x2032;-one and preparation thereof

The invention relates to aryl and heteroaryl substituted compounds of Formula (I), and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, R, and Z-Zare defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain. 

Aryl substituted indoles and the use thereof

The present disclosure provides substituted pyrimidine carboxamides of Formula (I) and the pharmaceutically acceptable salts and solvates thereof wherein A, X, A, W, W, W, E, Z, and Rare defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain. 

Pyrimidine carboxamides as sodium channel blockers

The present invention is directed to Benzomorphan Analog compounds of the Formula I&#x2033;, Formula IA&#x2033;, Formula IB&#x2033;, Formula IC&#x2033;, or Formula ID&#x2033; as shown below; and related Formula I', Formula IA&#x2032;, Formula IB&#x2032;, Formula IC&#x2032;, or Formula ID&#x2032;; Formula I, Formula IA, Formula IB, Formula IC, or Formula ID; wherein R, R, R, Rand Rare as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.

Benzomorphan analogs and the use thereof

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Princeton, NJ, United States of America

Jiangchao Yao