Purdue Pharma L.p.

Other

Jeffrey Lockman

Laykea Tafesse

Jiangchao Yao

Mark Andrew Youngman

Jae Hyun Park

Jianming Yu

Bin Shao

Chiyou Ni

Minnie Park

Andrew Kassick

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 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

The application is directed to compounds of Formula (I) or (IA) and pharmaceutically acceptable salts and solvates thereof, wherein RR, Rand G are defined as set forth in the specification. The invention is also directed to use of compounds of Formula (I) or (IA), 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. Certain compounds of the present invention are especially useful for treating pain. 

Ring-contracted morphinans 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. 

The application is directed to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein, R-R, R, Y and Zare defined as set forth in the specification. The invention is also directed to use of 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.

Pyridonemorphinan analogs and biological activity on opioid receptors

The application is directed to compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein 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 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.

Substituted morphinans and the use thereof

The application is directed to compounds of Formula I and pharmaceutically acceptable salts and solvates thereof, wherein R-Rare defined as set forth in the specification. The invention is also directed to use of 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. Certain compounds of the present invention are especially useful for treating pain.

Propellane-based compounds and the use thereof

The present invention is directed to Benzomorphan Analog compounds of the Formula I-ID as shown below, 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.

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Princeton Junction, NJ, United States of America

Jeffrey Lockman