Theravance Biopharma R&d Ip, LLC

Glenn D Crater

Paul Ross Fatheree

Robert Murray McKinnell

Lan Jiang

Melanie A Kleinschek

Cameron Smith

Gary E L Brandt

Lori Jean Van Orden

Steven D E Sullivan

Edmund J Moran

Christopher Noel Barnes

Srikanth Pendyala

Venkat R Thalladi

Marta Dabros

Jerry Nzerem

Hao Zhang

Gary EL Brandt

Steven DE Sullivan

Methods for treating chronic obstructive pulmonary disease (COPD) in a patient are disclosed. In the methods, a patient having COPD is selected for treatment based on the patient's peak inspiratory flow rate (PIFR) and percent predicted force expiratory volume in one second (FEV); and a bronchodilator is administered to the selected patient using a nebulizer. Administration of a bronchodilator to patients having low PIFR and a percent predicted FEVless than 50 percent using a nebulizer as the inhalation delivery device provides significantly greater improvements in trough FEVand trough forced vital capacity (FVC) compared to administration of a bronchodilator to such patients using a dry powder inhaler.

Methods for treating chronic obstructive pulmonary disease

The invention provides compounds of formula (I): which contain a 4-membered heterocyclic amide, where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.

JAK inhibitors containing a 4-membered heterocyclic amide

The invention relates to methods of treating ocular diseases and certain respiratory diseases using the compound 5-ethyl-2-fluoro-4-(3-(5-(1-methylpiperidin-4-yl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-2-yl)-1H-indazol-6-yl)phenol or a pharmaceutically-acceptable salt thereof.

Methods of treatment using a JAK inhibitor compound

The invention provides compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.

Fused imidazo-piperidine JAK inhibitors

The present invention provides crystalline hydrates of the oxalate and succinate salts of 5-ethyl-2-fluoro-4-(3-(5-(1-methylpiperidin-4-yl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-2-yl)-1H-indazol-6-yl)phenol. The invention also provides pharmaceutical compositions comprising such crystalline hydrates, methods of using such crystalline hydrates to treat respiratory and other diseases, and processes useful for preparing such crystalline oxalate and succinate hydrates.

Crystalline forms of a JAK inhibitor compound

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Raleigh, NC, United States of America

Glenn D Crater