Theravance, Inc.

Theravance Biopharma R&d Ip, LLC

Advanced Medicine, Inc.

Seok-Ki Choi

Paul Ross Fatheree

Roland Gendron

Robert Murray McKinnell

Daniel Marquess

Daniel D Long

Adam Aaron Goldblum

S Derek Turner

Brooke Olson

Keith Jendza

Paul Allegretti

Edmund J Moran

Darren J McMurtrie

Ryan Hudson

Lan Jiang

Vivek Sasikumar

David C Green

John H Griffin

Daniel G Genov

Brooke Blair

Thomas E Jenkins

Timothy J Church

Jyanwei Liu

Jason P Chinn

David Beattie

Scott Armstrong

Robert Murray Mckinnell

Kirsten M Phizackerley

Darren Mcmurtrie

Derek S Turner

The invention provides novel quinolinone-carboxamide 5-HTreceptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HTreceptor activity, and processes and intermediates useful for preparing such compounds.

Quinolinone-carboxamide compounds as 5-HT4 receptor agonists

The invention is directed to compounds having the formula: wherein: Ar, r, R, X, and Rare as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have ATreceptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Dual-acting imidazole antihypertensive agents

The invention is directed to compounds having the formula: wherein: Ar, r, n, X, Rand Rare as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have ATreceptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Dual-acting benzoimidazole antihypertensive agents

The invention is directed to methods for treating hypertension or heart failure using compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and Rare as defined in the specification, and pharmaceutically acceptable salts thereof. In particular embodiments, the invention uses compounds having formula IIIa, IVa, Va: These compounds have ATreceptor antagonist activity and neprilysin inhibition activity.

Dual-acting antihypertensive agents

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The invention is directed to intermediates for preparing compounds having the formula: 

Intermediates for preparing dual-acting benzyl triazole antihypertensive agents having angiotensin II type I receptor antagonist activity and neprilysin-inhibition activity

In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R, and Rare as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have ATreceptor antagonist activity and neprilysin inhibition activity. 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.

The invention is directed to compounds of formula I: wherein Ar, r, R, X, and Rare as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have ATreceptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.

The invention is directed to compounds having the formula: wherein: Ar, X, R, and Rare as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have ATreceptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Dual-acting benzyl triazole antihypertensive agents having angiotensin II type receptor antagonist activity and neprilysin-inhibition activity

The invention relates to compounds having the formula: wherein Ar, r, n, X, R, R, R, and Rare as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have ATreceptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.

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Palo Alto, CA, United States of America

Seok-Ki Choi