Theravance Biopharma R&d IP, LLC

Donna A A Wilton

Daniel D Long

Adam D Hughes

Melissa Fleury

Ryan Hudson

Mandy Loo

Anne-Marie Beausoliel

Patrick J Brassil

Anne-Marie Beausoleil

The invention provides compounds which are prodrugs of a JAK inhibitor agent for the targeted delivery of the JAK inhibitor to the gastrointestinal tract of a mammal. The invention also provides pharmaceutical compositions comprising the compounds, methods of using the compounds to treat gastrointestinal inflammatory diseases, and processes and intermediates useful for preparing the compounds.

Prodrugs of a JAK inhibitor compound for treatment of gastrointestinal inflammatory disease

The invention relates to glucuronide prodrug compounds of Janus kinase (JAK) inhibitors having formula I: where W, Rand Aare as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.

Glucuronide prodrugs of Janus kinase inhibitors

In one aspect, the invention relates to compounds having the formula I: where R-Rare as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

Neprilysin inhibitors

In one aspect, the invention relates to compounds having the formula I: where R, R, R, and R-Rare as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

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San Francisco, CA, United States of America

Donna A A Wilton