Theravance, Inc.

Advanced Medicine, Inc.

Theravance Biopharma R&d Ip, LLC

Yu-Hua Ji

Mathai Mammen

YongQi Mu

Li Li

Craig Husfeld

Adam D Hughes

Thomas E Jenkins

Eric L Stangeland

Viengkham Malathong

Sarah Dunham

Trevor Mischki

John R Jacobsen

John H Griffin

Timothy J Church

Sabine Axt

Weijiang Zhang

Huiwei Wu

J Kevin Judice

Yan Chen

Edmund J Moran

Jonathan W Wray

Richard D Wilson

Ioanna Stergiades

Aaron Kushner

Witold Hruzewicz

Rick Andrew Lee

David A Oare

Christopher W Lange

Cameron Smith

Johnny Uy

Yongqi Mu

Jennifer Bolton

Maya Natarajan

Robert S Chao

Leticia Maria Preza

Witold N Hruzewicz

Robert P Numerof

Davar Khossravi

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

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

The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-[2-({3-[2-(4-hydroxybenzylamino)ethylcarbamoyl]benzoyl}methylamino)ethyl]piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase (Form I or II), a salt such as a hemiedisylate salt or a heminapadisylate salt, or a solvate of a salt such as a heminapadisylate methanolate or a heminapadisylate ethanolate. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.

Crystalline forms of a biphenyl compound

This invention provides compounds of formula I: wherein a, b, c, m, p, s, t, W, Ar, X, R, R, R, R, R, and Rareas 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.

This invention provides compounds of formula I: wherein a, b, c, m, p, r, R, R, R, R, R, R, W and Xare 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.

This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, r, R, R, R, R, R, R, R, and W are 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.

This invention provides compounds of formula I: wherein a, b, c, m, p, s, t, W, Ar, X, 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.

This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, Ar, R, R, R, R, R, R, R, and W are 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.

The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, 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.

The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z, Ar, Z, Y, 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.

The invention provides compounds of formula I: wherein a, b, c, d, f, W, Q, Y, 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.

The invention provides compounds of formula I: wherein a, b, c, p, W, A, X, 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.

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Redwood City, CA, United States of America

Yu-Hua Ji