Theravance, Inc.

Theravance Biopharma R&d Ip, LLC

Paul Allegretti

Robert Murray McKinnell

Paul Ross Fatheree

Seok-Ki Choi

Roland Gendron

Darren J McMurtrie

Keith Jendza

Brooke Olson

Ryan Hudson

Christina Owens

Adam D Hughes

Cameron Smith

Erik Fenster

Jennifer Kozak

Steven D E Sullivan

Mandy Loo

Svitlana Kulyk

Tom M Lam

Gabrielle Elaine Dolgonos

Philip Gerken

Robert Murray Mckinnell

Darren Mcmurtrie

Provided herein are compounds of formula (I): and pharmaceutically-acceptable salts thereof, where A, W, X, Y and Z are defined in the specification. The compounds of formula (I) and pharmaceutically-acceptable salts thereof are Janus kinase (JAK) inhibitors. Also provided herein are pharmaceutical compositions comprising such compounds; and methods of using such compounds to treat, e.g., inflammatory and fibrotic diseases, including respiratory diseases.

Imidazolo indazole compounds as JAK inhibitors

The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.

Substituted pyridines and methods of use

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: Q, W, Y, Z, r, and Ar are 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.

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.

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.

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Fort Collins, CO, United States of America

Paul Allegretti