2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors

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

doi:10.1016/j.bmcl.2010.01.069

2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1724-7. doi: 10.1016/j.bmcl.2010.01.069. Epub 2010 Jan 21.

Affiliation

¹ Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4002 Basel, Switzerland. marc.gerspacher@novartis.com

PMID: 20138510
DOI: 10.1016/j.bmcl.2010.01.069

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.

MeSH terms

Administration, Oral
Animals
Benzoxazoles / chemical synthesis
Benzoxazoles / chemistry*
Benzoxazoles / pharmacokinetics
Janus Kinase 2 / antagonists & inhibitors*
Janus Kinase 2 / metabolism
Protein Kinase Inhibitors / chemical synthesis
Protein Kinase Inhibitors / chemistry*
Protein Kinase Inhibitors / pharmacokinetics
Rats
Structure-Activity Relationship

Substances

Benzoxazoles
Protein Kinase Inhibitors
Janus Kinase 2