Purdue Pharma L.p.

Euro-celtique S.a.

Shionogi Company Limited

Scios Inc.

Purde Pharma L.p.

R Richard Goehring

Donald Kyle

Sam Victory

Bin Shao

Laykea Tafesse

Jiangchao Yao

Zhengming Chen

John Whitehead

Qun Sun

Naoki Tsuno

Mark Andrew Youngman

Yoshiyuki Taoda

Samuel F Victory

Parviz Gharagozloo

Kouki Fuchino

John William Frank Whitehead

David Y Liu

John A Lewicki

Jianming Yu

George Frederic Schreiner

Babu J Mavunkel

Kevin Brown

Sarvajit Chakravarty

Sundeep Dugar

Gary Lee

Gregory R Luedtke

Akira Matsumura

John W F Whitehead

Marian E Fundytus

Yoshiyasu Baba

Sam Vicotry

Gregory Leudtke

Kevin C Brown

Donald J Kyle

In one aspect, the invention provides compounds of Formula I: (I) and pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, R, Y, Zare defined as set forth in the disclosure. The invention also provides compounds of any one of Formulae II to VII, IA to IC, and IIA to IIC, and pharmaceutically acceptable salts and solvates thereof. Other aspects of the invention include the use of compounds of Formulae I to VII, IA to IC, and IIA to IIC, 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. 

Spirocyclic morphinans and use thereof

The invention provides compounds as represented by Formula I or I' and pharmaceutically acceptable salts, solvates, and diastereomers thereof: Wherein R, R, R, R, and Rare defined in the disclosure. The invention also provides compounds of Formulae II, III, and A-H, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. In certain embodiments, Compounds of the Invention are useful for treating pain, constipation, and other conditions as delineated in the disclosure. Without wishing to be bound by any theory, it is believed that Compounds of the Invention are effective in treating conditions that are modulated by activity of opioid and/or ORL-1 receptors. 

Benzomorphan analogs and use thereof

The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a 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 Substituted-Quinoxaline-Type Piperidine Compound.

Substituted-quinoxaline-type piperidine compounds and the uses thereof

The present invention is directed to Buprenorphine Analog compounds of Formula I, II, III, IV or V and including various stereoisomers (such as Formula IA shown below), wherein R, R, R, R, R, G, Q, X, A and Z are as defined herein. Compounds of the Invention may be useful for preparing medicaments useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors. Compounds of the Invention may be useful for treating Conditions such as pain, constipation, and others modulated by activity of opioid and ORL-1 receptors.

Buprenorphine analogs

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

Spirocyclic morphinans and their use

The invention relates to aryl substituted quinazolines of Formula I, and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, A, and R-Rare 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. 

Quinazoline compounds as sodium channel blockers

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

The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted 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 Heterocyclic-Substituted Piperidine Compound.

2,3,4,5-tetrahydro-benzo{B}{1,4}diazepine-comprising compounds of formula(III) for treating pain

The present invention is directed to Buprenorphine Analog compounds of the Formula I, Formula II or Formula III shown below, wherein R, R, R, R, R, R, X, Z and Y are as defined herein. Compounds of the Invention are useful for treating pain and other conditions modulated by activity of opioid and ORL1 receptors.

Buprenophine analogs

A compound of the formula (I), (II), (III) or (IV) 

Nociceptin analogs

Compounds comprising heterocyclic-substituted piperidine for treating pain

This invention relates aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R-Rare set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

Aryl substituted pyridines and the use thereof

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Pipersville, PA, United States of America

R Richard Goehring