Theravance Biopharma R&d Ip, LLC

Gene Timothy Fass

Melissa Fleury

Miroslav Rapta

Venkat R Thalladi

Adam D Hughes

Pierre-Jean Colson

Michael Simeone

Paul Ross Fatheree

Lan Jiang

John R Jacobsen

Cameron Smith

Anne-Marie Beausoleil

Gary E L Brandt

Lori Jean Van Orden

Weijiang Zhang

Steven D E Sullivan

Marta Dabros

Noah M Benjamin

David L Bourdet

R Michael Baldwin

Steven De Sullivan

Gary El Brandt

Provided herein is a crystalline hydrate of the compound of formula 1: Also provides herein are pharmaceutical compositions comprising such crystalline hydrate, methods of using such crystalline hydrate to treat respiratory diseases, and processes useful for preparing such crystalline hydrate.

Crystalline hydrate of a JAK inhibitor compound

In one aspect, the invention relates to a crystalline form of the structure: or a pharmaceutically acceptable salt thereof, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this crystalline form; methods of using this crystalline form and its soluble form (I); and processes for preparing soluble (I) and crystalline (I') forms.

Crystalline (2S,4R)-5-(5'-chloro-2&#x2032;-fluoro-[1,1&#x2032;-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2- methylpentanoic acid and uses thereof

The invention provides compounds of formula (I): wherein X is and 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 kinase inhibitor compounds for treatment of respiratory disease

The invention is directed to a process for preparing compounds which are useful as intermediates for the preparation of medicinal agents having inhibitory activity for JAK.

Process for preparing JAK inhibitors and intermediates thereof

Crystalline (2S,4R)-5-(5'-chloro-2&#x2032;-fluoro-[1,1&#x2032;-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof

Crystalline(2S,4R)-5-(5'-chloro-2&#x2032;-fluoro-[1,1&#x2032;-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof

The invention provides processes for preparing intermediates useful for preparing compounds of the formula: or a salt thereof, where Rare as defined in the specification.

Process for preparing biphenyl imidazole compounds

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San Francisco, CA, United States of America

Gene Timothy Fass