Theravance, Inc.

Theravance Biopharma R&d IP, LLC

Ioanna Stergiades

Daniel D Long

Lan Jiang

John R Jacobsen

Daisuke Roland Saito

Adam D Hughes

Mathai Mammen

Craig Husfeld

Yu-Hua Ji

Li Li

Pierre-Jean Colson

Sarah Dunham

Priscilla M Van Dyke

Richard D Wilson

Trevor Mischki

Ying Yu

Timothy J Church

David A Oare

Edward Yost

Yan Chen

Sean Dalziel

Sabine Axt

Weijiang Zhang

Leticia Maria Preza

Cristin Hubbard

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

The invention provides an efficient method for preparing 3-endo-(8-azabicyclo[3.2.1]oct-3-yl)benzamide by hydrogenation, under controlled conditions, of an amino-protected 3-(8-azabicyclo[3.2.1]oct-2-en-3-yl)benzamide intermediate in which the amino-protecting group is removable by catalytic hydrogenation.

Process for preparing an intermediate to mu opioid receptor antagonists

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

This invention provides 4-amino-1-benzylpiperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome, asthma and chronic obstructive pulmonary disease, using such compounds.

Substituted 4-amino-benzylpiperidine compounds

Process for preparing an intermediate to opioid receptor antagonists

The invention provides a novel &#x3b2;adrenergic receptor agonist in crystalline salt form. The invention also provides pharmaceutical compositions comprising the novel &#x3b2;adrenergic receptor agonist in crystalline salt form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt to treat diseases associated with &#x3b2;adrenergic receptor activity, and processes useful for preparing such crystalline compounds.

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Substituted 4-amino-1-benzylpiperidine compounds

This invention provides 4-amino-1-(pyridylmethyl)piperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome and chronic obstructive pulmonary disease, using such compounds.

Substituted 4-amino-1-(pyridylmethyl)piperidine and related compounds

The invention provides crystalline solvate forms of a salt of a novel &#x3b2;adrenergic receptor agonist. The invention also provides pharmaceutical compositions comprising the solvate forms, formulations containing the pharmaceutical compositions, methods of using the solvate forms to treat diseases associated with &#x3b2;adrenergic receptor activity, and processes useful for preparing such solvate forms.

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San Francisco, CA, United States of America

Ioanna Stergiades