Purdue Pharma L.p.

Euro-celtique S.a.

Shionogi Company Limited

Purdue Pharma, L.p., USA

Xiaoming Zhou

Laykea Tafesse

Qun Sun

Jiangchao Yao

Donald Kyle

Bin Shao

Jianming Yu

Naoki Tsuno

Chiyou Ni

Nobuyuki Tanaka

Tatsuhiko Ueno

Dawit Tadesse

Chongwu Zhang

Mark Andrew Youngman

Zhengming Chen

Jae Hyun Park

Samuel F Victory

Kate Wen

Kenji Yamawaki

Kevin Brown

Noriyuki Kurose

Deyou Sha

Minnie Park

Kouki Fuchino

Parviz Gharagozloo

Naoko Yamaguchi

John W F Whitehead

Ji Yang

John William Frank Whitehead

Yasuyoshi Iso

Khondaker Islam

Kayoko Hata

John J Engel

Jeffrey Michael Marra

Elfrida R Benjamin

Donald James Kyle

In one aspect, the invention provides compounds of Formula (I) or (II): (I) or (II) and pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, R, Z and G are defined as set forth in the disclosure. The invention also provides compounds of Formulae A and B and pharmaceutically acceptable salts and solvates thereof. Other aspects of the invention include the use of compounds of Formulae I, II, A, and B, and pharmaceutically acceptable salts and solvates thereof for the treatment of disorders responsive to modulation of one or more opioid receptors. In certain embodiments, the Compounds of the Invention are useful for treating pain. 

Benzomorphan analogs and the use thereof

The disclosure relates to Substituted Piperidin-4-amino-Type Compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof wherein R, R, R, Q, Q, E, E, A, B, D, W, Z, a, b, n, and x are as defined herein, compositions comprising an effective amount of a Substituted Piperidin-4-amino-Type 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 Piperidin-4-amino-Type Compound. 

Substituted piperidin-4-amino-type compounds and uses thereof

The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: and pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein W, W, W, W, U, G, m, R, and Rare defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II to V as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.

Benzimidazole derivatives and use thereof

The present disclosure provides pyrimidines of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein A, X, A, G, Y, n, R, R, and Rare defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I and the pharmaceutically acceptable salts and solvates thereof to treat a disorder responsive to the blockade of one or more sodium channels. In one embodiment, compounds of the present disclosure are useful for treating pain. 

Pyrimidines and use thereof

The invention relates to substituted pyridine compounds of Formula I: (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R, R, R, R, R, A, A, and X are 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. 

Substituted pyridines as sodium channel blockers

The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R, A, A, E, G, Z, and 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. 

Pyridine compounds and the uses thereof

The disclosure relates to Phosphorus-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein the dashed line, A, B, Q, R, R, R, R, Y, Z, and a are as defined herein, compositions comprising an effective amount of a Phosphorus-Substituted Quinoxaline-Type 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 Phosphorus-Substituted Quinoxaline-Type Piperidine Compound.

Phosphorus-substituted quinoxaline-type piperidine compounds and uses thereof

The disclosure relates to Substituted Benzimidazole-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable salts or solvates thereof, e.g., a pharmaceutically acceptable salt or solvate, wherein R, R, R, Q, W, U, A, B, Z, a, and the dashed lines are as defined herein, compositions comprising an effective amount of a Substituted Benzimidazole-Type 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 Benzimidazole-Type Piperidine Compound.

Substituted benzimidazole-type piperidine compounds and uses thereof

The disclosure relates to Azetidine-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein the R, R, R, Q, Y, Z, A, B, a, and b are as defined herein, compositions comprising an effective amount of an Azetidine-Substituted Quinoxaline-Type 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 an Azetidine-Substituted Quinoxaline-Type Piperidine Compound.

Azetidine-substituted quinoxalines as opioid receptor like-1 modulators

The invention relates to compounds of Formula I: wherein Ar, Ar, Ar, L, L, Y, Z and v are defined in the specification, and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.

Heterocyclic compounds

The disclosure relates to Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein R, R, Q, Y, Z, A, B, Q, E, G, J, M, U, W, and a are as defined herein, compositions comprising an effective amount of a Cyclic Urea- or Lactam-Substituted Quinoxaline-Type 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 Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compound.

Cyclic urea- or lactam-substituted quinoxaline-type piperidines as ORL-1 modulators

Pyridine compounds and the users thereof

The present disclosure relates to Oxime-Substituted Quinoxaline-Type Piperidine Compounds, such as those of Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, R, R, Q, Y, Z, A, B, and a are as defined herein; compositions comprising an effective amount of an Oxime-Substituted Quinoxaline-Type 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 an Oxime-Substituted Quinoxaline-Type Piperidine Compound.

Oxime-substituted-quinoxaline-type piperidine compounds as ORL-1 modulators

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Plainsboro, NJ, United States of America

Xiaoming Zhou