Purdue Pharma L.p.

Janssen Pharmaceutica Nv

Ortho-mcneil Pharmaceutical Corp.

Other

Janssen Pharmaceutica

Johnson & Johnson Pharmaceutical Research & Development, LLC

Mark Andrew Youngman

Scott L Dax

Laykea Tafesse

James J McNally

Michele C Jetter

Christopher M Flores

Raymond W Colburn

Donald William Ludovici

Jay M Matthews

Bin Shao

Chiyou Ni

Minnie Park

Christopher A Teleha

Ning Qin

Mark E McDonnell

Jiangchao Yao

Jae Hyun Park

Bin Benjamin Zhu

Ellen Codd

Mingde Xia

Kenneth M Wells

Jeffrey Lockman

Xiaoqing Xu

Mark J Macielag

John R Carson

R Richard Goehring

Timothy W Lovenberg

Ronald K Russell

Shawn T Branum

Yi Liu

Scott C Youells

Jung S Lee

Laura M Reaney

Laura Reany

Jiangcho Yao

Allen B Reitz

William H Parsons

William V Murray

Jianming Yu

Mark R Player

Nicholas I Carruthers

Wenying Chai

Xiaoming Zhou

Dale A Rudolph

Xiaobing Li

Jill A Jablonowski

Ellen W Baxter

Mark Seierstad

Raul R Calvo

Wenxi Pan

Sharmila Patel

Wing S Cheung

Yu-Kai Lee

Jian Liu

Michael Richard Brandt

Derek A Beauchamp

Laura M Andraka

Laura W Andraka

Mark Mcdonell

Raul L Calvo

Michael Brandt

Mark Mcdonnell

Xiaoging Xu

Jay M Mathews

James J Mcnally

Laura M Reany

Michele Jetter

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 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 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 application is directed to compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, and Z are defined as set forth in the specification. In certain embodiments, the invention is also directed to compounds of Formula II-VII and the pharmaceutically acceptable salts and solvates thereof. The invention is also directed to use of compounds of Formula I to VII, 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 invention are especially useful for treating pain. 

Heterocyclic morphinan derivatives and use thereof

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 application is directed to Pyridone-sulfone morphinan analogs compounds of Formula I: or pharmaceutically acceptable salts and solvates thereof, wherein ==, R1, R2, R3, R4 and Z are as defined as set forth in the specification. The invention is also directed to use of the compounds of Formula I or the pharmaceutically acceptable salts and solvates thereof to treat disorders responsive to the odulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain. 

Pyridone-sulfone morphinan analogs as opioid receptor ligands

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, 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 application is directed to compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein R, R, Y, Z, and G are defined as set forth in the specification. The invention is also directed to use of compounds of Formula (I), and 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. 

Opioid receptor modulating oxabicyclo[2.2.2]octane morphinans

The present disclosure provides cyclic sulfonamides of Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, and n are 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. For example, compounds of the present disclosure are useful for treating pain. 

Cyclic sulfonamides as sodium channel blockers

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 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. 

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R, R, R, and Rare defined herein.

Sulfonamides as TRPM8 modulators

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North Wales, PA, United States of America

Mark Andrew Youngman