Wisconsin Alumni Research Foundation

Theravance Biopharma R&d Ip, LLC

Luke Boralsky

Jennifer Marie Schomaker

Jared Rigoli

Christopher S Adams

John Hershberger

Robert Murray McKinnell

Erik Fenster

Tom M Lam

Breena Gloriana Fraga

Anthony Francesco Palermo

Diana Jin Wang

The disclosure 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 disclosure also provides pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat gastrointestinal inflammatory diseases.

Fused pyrimidine pyridinone compounds as JAK inhibitors

The oxidative functionalization of olefins is a common method for the formation of vicinal carbon-heteroatom bonds. However, oxidative methods to transform allenes into synthetic motifs containing three contiguous carbon-heteroatom bonds are much less developed. The use of bicyclic methylene aziridines (MAs), prepared via intramolecular allene aziridination, as scaffolds for functionalization of all three allene carbons, among other reactions, is described herein.

Bicyclic methylene aziridines and reactions thereof

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San Francisco, CA, United States of America

Luke Boralsky