Theravance Biopharma R&d Ip, LLC

Jerry Nzerem

Venkat R Thalladi

Marta Dabros

Miroslav Rapta

Robert Murray McKinnell

Erik Fenster

Adam D Hughes

Melissa Fleury

Ryan Hudson

Anne-Marie Beausoleil

Jennifer Kozak

Tom M Lam

Paul Ross Fatheree

Lan Jiang

Gary E L Brandt

Weijiang Zhang

Glenn D Crater

Mandy Loo

Melanie A Kleinschek

Xiaojun Huang

Hao Zhang

Breena Gloriana Fraga

Noah M Benjamin

Anthony Francesco Palermo

Diana Jin Wang

Gary EL Brandt

The invention provides a compound of formula (I): or a pharmaceutically-acceptable salt thereof, that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such compound, a crystalline form, methods of using such compound to treat inflammatory skin diseases and other diseases, and processes and intermediates useful for preparing such compound.

Pyrimidine compound as JAK kinase inhibitor

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 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

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

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.

(2S,4R)-5-(5'-chloro-2&#x2032;-fluorobiphenyl-4-yl)-4-(ethoxyoxalylamino)-2-hydroxymethyl-2-methylpentanoic acid

(2S,4R)-5-(5'-chloro-2&#x2032;-fluorobiphenyl-4-yl)-4-(ethoxyoxalylamino)-2-hydroxmethyl-2-methylpentanoic acid

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The invention provides crystalline forms of (R)-3-[N-(3'-chlorobiphenyl-4-ylmethyl)-N&#x2032;-(3-hydroxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic acid isopropyl ester. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases.

Crystalline forms of (R)-3-[N-(3'-chlorobiphenyl-4-ylmethyl)-N'-(3-hydroxyisoxazole-5-carbonyl)hydrazino]-2-hydroxyproprionic acid isopropyl ester

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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South San Francisco, CA, United States of America

Jerry Nzerem