Purdue Pharma L.p.

Other

Jae Hyun Park

Laykea Tafesse

Jiangchao Yao

Mark Andrew Youngman

Jeffrey Lockman

Bin Shao

Chiyou Ni

Donald Kyle

Stephen Matthew Lynch

Minnie Park

Jianming Yu

Xiaoming Zhou

David Rosen

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

Azamorphinan derivatives and 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 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 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 present invention relates to C-terminal modified Protoxin II peptides that selectively inhibit the Nav1.7 sodium channel; the present invention also relates to pharmaceutical compositions useful for prophylactic or therapeutic treatment of a disorder responsive to the blockade of sodium ion channels, especially Nav1.7 sodium ion channels; the present invention further provides methods of treating a disorder responsive to the blockade of sodium channels, and particularly Nav1.7 sodium channels, in a mammal suffering from excess activity of said channels.

Sodium channel blocking peptides 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 present disclosure provides substituted piperidines or pyrrolidines having Formula IA: and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, A, X, m and n are defined as set forth in the specification. In certain embodiments, Compounds of the present disclosure are useful for treating pain. The present disclosure is also directed to the use of Compounds of the present disclosure to treat a disorder responsive to blockade of one or more sodium channels.

Substituted piperidines as sodium channel blockers

The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: or pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein R, R, X, G, n, p, W, W, W, W, and the E ring are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II-XIII 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.

Pyridine and piperidine derivatives as novel sodium channel blockers

The present invention relates to a peptide and its analogs that selectively inhibit the Na1.7 sodium channel. The present invention also relates to pharmaceutical compositions useful for treating or preventing a disorder responsive to the blockade of sodium ion channels, especially Na1.7 sodium ion channels. The present invention further provides methods of treating a disorder responsive to the blockade of sodium channels, and particularly Na1.7 sodium channels, in a mammal suffering from excess activity of the channels, compositions and methods for providing analgesia by administering a peptide of the invention.

Growing community of inventors

Princeton, NJ, United States of America

Jae Hyun Park