Theravance, Inc.

Theravance Biopharma R&d IP, LLC

Priscilla M Van Dyke

Daisuke Roland Saito

Daniel D Long

Lan Jiang

John R Jacobsen

Timothy J Church

Lori Jean Patterson

Eric L Stangeland

Michael Robert Leadbetter

Sean Gary Trapp

Ioanna Stergiades

Bryan A Frieman

Adam D Hughes

Miroslav Rapta

Pierre-Jean Colson

Sean Dalziel

Jane F Schmidt

Leticia Maria Preza

Ying Yu

Eric Strangeland

Tmothy J Church

Daniel Long

Leticia Preza

The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R, R, R, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists

In one aspect, the invention relates to compounds of formula I: where Rare as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

3-phenoxymethylpyrrolidine compounds

In one aspect, the invention relates to compounds of formula I: where a and Rare as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

3-(phenoxyphenylmethyl)pyrrolidine compounds

The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): wherein R, R, R, R, R, and Rare defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

3-carboxypropyl-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula wherein R, R, R, and a are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Amidoalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists

The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R, R, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds as mu opioid receptor antagonists

8-azabicyclo[3.2.1]octane compounds as MU opioid receptor antagonists

The invention provides heteroarylene substituted 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R, R, A, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Heteroarylalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists

The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R, R, and m are defined in the specification, or a pharmaceutically -acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R, R, R, and a are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

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San Francisco, CA, United States of America

Priscilla M Van Dyke