Theravance, Inc.

Theravance Biopharma R&d Ip, LLC

Signature Therapeutics, Inc.

Concentric Analgesics, Inc.

Elysium Therapeutics, Inc.

Theravance Respiratory Company, LLC

Craig Husfeld

YongQi Mu

Mathai Mammen

Li Li

Yuhua Ji

Yu-Hua Ji

Eric L Stangeland

Rick Andrew Lee

Thomas E Jenkins

Adam D Hughes

YuHua Ji

Sarah Dunham

Trevor Mischki

Aaron Kushner

Jonathan W Wray

Julie D Seroogy

John F Donovan

Yan Chen

Cameron Smith

Christopher W Lange

Johnny Uy

Miroslav Rapta

Pierre-Jean Colson

Richard D Wilson

Ioanna Stergiades

Yongqi Mu

David A Oare

Andrei William Konradi

Tae Weon Lee

This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar, R, R, R, R, R, R, and Rare as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Biphenyl compounds useful as muscarinic receptor antagonists

Described herein are compounds, pharmaceutical compositions and medicaments that include such compounds, and methods of using such compounds to modulate transient receptor potential vanilloid 1 receptor (TRPV1) activity.

Prodrugs of phenolic TRPV1 agonists

Prodrugs of phenolic TRPV1 agonists in combination with local anesthetics and vasoconstrictors for improved local anesthesia

Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an amphetamine prodrug that provides enzymatically-controlled release of amphetamine or an amphetamine analog. The composition can further comprise an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of amphetamine or the amphetamine analog from the amphetamine prodrug so as to attenuate enzymatic cleavage of the amphetamine prodrug.

Compositions comprising enzyme-cleavable amphetamine prodrugs and inhibitors thereof

Pegylated prodrugs of phenolic TRPV1 agonists

The invention provides compositions and methods for the treatment or prevention of pain. Compositions provided are resistant to overdose and abuse. Compositions provided comprise two or more different molecules, where each molecule comprises at least one GI enzyme-labile opioid agonist releasing subunit comprising an opioid agonist that is covalently linked to at least one GI enzyme inhibitor subunit.

Polysubunit opioid prodrugs resistant to overdose and abuse

A method of providing a patient with controlled release of ketone-containing opioid using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing the ketone-containing opioid is disclosed. The disclosure also provides such prodrug compounds and pharmaceutical compositions comprising such compounds. Such pharmaceutical compositions can optionally include an enzyme inhibitor that interacts with the enzyme(s) to mediate the enzymatically-controlled release of the ketone-containing opioid from the prodrug so as to modify enzymatic cleavage of the prodrug. Also included are methods to use such compounds and pharmaceutical compositions.

Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof

Growing community of inventors

Redwood City, CA, United States of America

Craig Husfeld