Theravance Biopharma R&d IP, LLC

Theravance, Inc.

Xenoport, Inc.

Venkat R Thalladi

Miroslav Rapta

Melissa Fleury

Adam D Hughes

Erik Fenster

Jerry Nzerem

Anne-Marie Beausoleil

Marta Dabros

Paul Ross Fatheree

Xiaojun Huang

Manshiu Leung

Hao Zhang

Robert Murray McKinnell

Gene Timothy Fass

Lan Jiang

Pierre-Jean Colson

Tom M Lam

Noah M Benjamin

Shaoling Li

David L Bourdet

Michael Simeone

Yun Mo

R Michael Baldwin

John R Jacobsen

Ryan Hudson

Sami Karaborni

Gary E L Brandt

Jennifer Kozak

Chen Mao

Dante D Podesto

Timothy Fass

Cameron Smith

Robert S Chao

Lori Jean Van Orden

Weijiang Zhang

Steven D E Sullivan

Glenn D Crater

Mandy Loo

Melanie A Kleinschek

Breena Gloriana Fraga

Ai Ling Ching

Anthony Francesco Palermo

Diana Jin Wang

Nathan Schulpen

Guido Verniest

Marian E Van Der Veen

Bernardus Joseph Nitert

Jens Maes

Yvonne Rosiaux

Gary EL Brandt

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'-fluoro-[1,1'-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof

The present disclosure relates to pharmaceutical compositions comprising (3-((1R,3s,5S)-3-((7-((5-methyl-1H-pyrazol-3-yl)amino)-1,6-naphthyridin-5-yl)amino)-8-azabicyclo[3.2.1]octan-8-yl)propanenitrile), methods of use thereof, and methods of preparation.

Formulation of a pan-JAK inhibitor

Disclosed are methods for treating Crohn's disease using a compound of the formula: or a pharmaceutically-acceptable salt thereof.

Methods for treating Crohn's disease using 3-((1R,3s,5S)-3-((7-((5-methyl-1H-pyrazol-3-yl)amino)-1,6-naphthyridin-5-yl)amino)-8-azabicyclo[3.2.1]octan-8-yl)propanenitrile

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

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

(2R,4R)-5-(5'-chloro-2&#x2032;-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid

The invention provides a solid composition of the peripheral mu opioid antagonist axelopran and a combination dosage form of the mu opioid antagonist axelopran sulfate in an immediate release form and an opioid analgesic agent which may be in an extended release, sustained release, modified release, or controlled release form and methods of preparing such a combination dosage form.

Combination dosage form of a mu opioid receptor antagonist and an opioid agent

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 a compound of formula 1 or a pharmaceutically-acceptable salt thereof, that is useful as a JAK inhibitor. The invention also provides crystalline forms of the compound, pharmaceutical compositions comprising the compound, methods of using the compound to treat diseases amenable to a JAK inhibitor, and processes and intermediates useful for preparing the compound.

Fused imidazo-piperidine JAK inhibitor compound

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): or a pharmaceutically-acceptable salt thereof, wherein the variables are defined in the specification, that are inhibitors of JAK kinases, particularly JAK3. The invention also provides crystalline forms, pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.

Pyrazolo and triazolo bicyclic compounds as JAK kinase inhibitors

Disclosed are methods for treating ulcerative colitis using a compound of the formula: or a pharmaceutically-acceptable salt thereof.

Methods for treating ulcerative colitis using 3-((1R,3s,5S)-3-((7-((5-methyl-1H-pyrazol-3-yl)amino)-1,6-naphthyridin-5-yl)amino)-8-azabicyclo[3.2.1]octan-8-yl)propanenitrile

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Foster City, CA, United States of America

Venkat R Thalladi