Purdue Pharma L.p.

Shionogi Company Limited

Other

Euro-celtique S.a.

Purdue Pharma, L.p., USA

Laykea Tafesse

Jiangchao Yao

Mark Andrew Youngman

Chiyou Ni

Donald Kyle

Xiaoming Zhou

Jae Hyun Park

Qun Sun

Bin Shao

Jeffrey Lockman

Minnie Park

Jianming Yu

R Richard Goehring

Sam Victory

Stephen Matthew Lynch

Noriyuki Kurose

Zhengming Chen

Andrew Kassick

Khondaker Islam

Jiangcho Yao

Naoki Tsuno

Donald J Kyle

Chongwu Zhang

Shigeru Ando

Samuel F Victory

Hidenori Mikamiyama

Deyou Sha

Kouki Fuchino

Dawit Tadesse

Parviz Gharagozloo

Naoko Yamaguchi

John W F Whitehead

Ji Yang

Paul Blake

Don Kyle

John William Frank Whitehead

Yasuyoshi Iso

Kayoko Hata

Richard R Goehring

John J Engel

Elfrida R Benjamin

Donald James Kyle

Mark Youngman

Mark A Youngman

David Rosen

The application is directed to compounds of formula (I): and pharmaceutically acceptable salts, radiolabeled isomers, solvates, or hydrates thereof, wherein R, R, R, X, and n are defined as set forth in the specification. The application is also directed to compounds of formulae II, I-a, I-a1, I-a2, I-b, and I-b1 and the pharmaceutically acceptable salts, radiolabeled isomers, solvates, and hydrates thereof. The application is also directed to use of Compounds of the present disclosure to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain Compounds of the present disclosure are especially useful for treating pain. In one embodiment, Compounds of the present disclosure exhibit less opioid-induced side effects (such as, euphoria or drug-liking).

Morphinan derivatives and use thereof

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

The Invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, N-oxides, or diastereomers thereof: wherein W, W, W, J, J, A, R, R, R, R, R, a, and b are defined as set forth in the specification. The Invention also provides uses of the compounds of any one of Formulae (I)-(VIII) and the pharmaceutically acceptable salts, solvates, hydrates, N-oxides, or diastereomers thereof. Compounds of the Invention are useful for treating a disorder responsive to blockade of one or more sodium channels. In certain embodiments, Compounds of the Invention are useful for treating pain. 

Isoquinoline derivatives and use thereof

The invention provides azaspiro[4.5]decane derivatives of Formula (A): and pharmaceutically acceptable salts, solvates, hydrates, N-oxides, and diastereomers thereof, wherein A, X, A, Rr, R, W, W, R, R, a, and b are defined in the disclosure. The invention also provides compounds of Formulae I, and B-G, and pharmaceutically acceptable salts, solvates, hydrates, N-oxides, and diastereomers thereof. Further, the invention provides use of the compounds of Formulae A-G and I, and the pharmaceutically acceptable salts, solvates, hydrates, N-oxides, and diastereomers thereof, to treat pain. In certain embodiments, Compounds of the Disclosure are useful for treating a disorder responsive to blockade of one or more sodium channels. 

Azaspiro[4.5]decane derivatives and use thereof

The present disclosure is directed to oxazoline mono- and hetero-pseudodimer compounds, such as compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof: These compounds are useful for treating pain. The present disclosure also relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of Formula (I) or (II) or a pharmaceutically acceptable salt or solvate thereof.

Oxazoline pseudodimers, pharmaceutical compositions and the use thereof

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

The application is directed to compounds of formula (I): and pharmaceutically acceptable salts, radiolabeled isomers, solvates, or hydrates thereof, wherein R, R, R, X, and n are defined as set forth in the specification. The application is also directed to compounds of formulae II, I-a, I-a1, I-a2, I-b, and I-b1 and the pharmaceutically acceptable salts, radiolabeled isomers, solvates, and hydrates thereof. The application is also directed to use of Compounds of the present disclosure to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain Compounds of the present disclosure are especially useful for treating pain. In one embodiment, Compounds of the present disclosure exhibit less opioid-induced side effects (such as, euphoria or drug-liking). 

The invention relates to compounds of formula IA and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA 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 IA or a pharmaceutically acceptable derivative thereof.

TRPV1 antagonists including dihydroxy substituent and uses thereof

The application is directed to compounds of Formula I or II: and pharmaceutically acceptable salts and solvates thereof, wherein R', R&#x2033;, R&#x2032;&#x2033; R, R, R, R, R, and Rare defined as set forth in the specification. The invention is also directed to use of compounds of Formula I or II and the pharmaceutically acceptable salts and solvates thereof to treat disorders responsive to the modulation of one or more opioid receptors. Certain compounds of the invention are especially useful for treating pain. 

6-substituted and 7-substituted morphinan analogs and the use thereof

The disclosure provides processes of preparing compounds of Formula (I) and Formula (IV), their salts, and intermediates thereof, wherein R, R, R, and Rare defined as set forth in the specification. 

Process for preparing substituted 9,10-dioxo-9,10-dihydroanthrecenes and 6H-anthra[1,9-cd]isoxazol-6-ones

The disclosure relates to Compounds of Formula (I) and pharmaceutically acceptable derivatives thereof, where R, R, R, R, and m are as defined herein, 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, pain associated with osteoarthritis, osteoarthritis, 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.

The application provides compounds of Formula I and pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, R, dash line a, dash line b, W, Z, X, and m are defined as set forth in the specification. The invention is also directed to use of the compounds of Formula I and the pharmaceutically acceptable salts and solvates thereof to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. In certain embodiments, the Compounds of the Invention are useful for treating pain. 

6,7-cyclicmorphinan derivatives and use 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

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Robbinsville, NJ, United States of America

Laykea Tafesse