Theravance Biopharma R&d Ip, LLC

Xiaojun Huang

Venkat R Thalladi

Ryan Hudson

Jennifer Kozak

Dante D Podesto

Weijiang Zhang

Paul Ross Fatheree

Daniel D Long

Melissa Fleury

Robert Murray McKinnell

Lan Jiang

Eric L Stangeland

Sheila M Zipfel

Daisuke Roland Saito

Anne-Marie Beausoleil

Lori Jean Van Orden

Jerry Nzerem

Mandy Loo

Matteo Conza

Vit Lellek

Gavin Ogawa

Kassandra Lepack

Dimitar Filipov

Anja Huste

Norbert Kraut

Stephen Roseblade

Christian Pater

Bjorn Gielen

Gary EL Brandt

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

The present disclosure provides processes for preparing a crystalline form of 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 and related intermediate compounds.

Processes for preparing a pan-JAK inhibitor and related intermediate compounds

The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of JAK kinases. The invention also provides 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.

Pyrimidine 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

Disclosed herein is a crystalline solvate comprising the compound of formula: methanol, N,N-dimethylformamide, and water, that is useful to prepare a crystalline form of said compound, which is an inhibitor of JAK kinases.

Crystalline solvate 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, methanol, N-N-dimethylformamide, and water

The invention provides a crystalline form of the compound of formula: that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such crystalline form and methods of using such crystalline form in mammals suffering from inflammatory bowel diseases.

Crystalline form of 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

The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.

Inhibitors of hepatitis C virus

The invention provides crystalline solid forms of (((S)-1-{(S)-2-[4-(4'-{[6-((2R,5S)-2,5-dimethyl-4-methylcarbamoyl-piperazin-1-yl)-pyridine-3-carbonyl]-amino}-2&#x2032;-trifluoromethoxy-biphenyl-4-yl)-1H-imidazol-2-yl]-pyrrolidine-1-carbonyl}-2-methyl-propyl)-carbamic acid methyl ester. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat hepatitis C virus infection, and processes useful for preparing such crystalline solid forms.

Crystalline form of a pyridyl-piperazinyl hepatitis C virus inhibitor

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Sunnyvale, CA, United States of America

Xiaojun Huang