Theravance, Inc.

Theravance Biopharma R&d Ip, LLC

Brooke Olson

Paul Ross Fatheree

Seok-Ki Choi

Robert Murray McKinnell

Roland Gendron

Darren J McMurtrie

Keith Jendza

Paul Allegretti

Ryan Hudson

Robert Murray Mckinnell

Darren Mcmurtrie

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

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

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.

The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, 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.

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Williamstown, MA, United States of America

Brooke Olson