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2-Amino-aryl-7-aryl-benzoxazoles as potent,selective and orally available JAK2 inhibitors |
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| Authors: | Marc Gerspacher Pascal Furet Carole Pissot-Soldermann Christoph Gaul Philipp Holzer Eric Vangrevelinghe Marc Lang Dirk Erdmann Thomas Radimerski Catherine H. Regnier Patrick Chene Alain De Pover Francesco Hofmann Fabienne Baffert Thomas Buhl Reiner Aichholz Francesca Blasco Ralf Endres Jörg Trappe Peter Drueckes |
| Affiliation: | Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4002 Basel, Switzerland |
| Abstract: | A series of novel benzoxazole derivatives has been designed and shown to exhibit attractive JAK2 inhibitory profiles in biochemical and cellular assays, capable of delivering compounds with favorable PK properties in rats. Synthesis and structure–activity relationship data are also provided. |
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