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

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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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-03, Vol.20 (5), p.1724-1727
Main Authors: Gerspacher, Marc, Furet, Pascal, Pissot-Soldermann, Carole, Gaul, Christoph, Holzer, Philipp, Vangrevelinghe, Eric, Lang, Marc, Erdmann, Dirk, Radimerski, Thomas, Regnier, Catherine H., Chene, Patrick, Pover, Alain De, Hofmann, Francesco, Baffert, Fabienne, Buhl, Thomas, Aichholz, Reiner, Blasco, Francesca, Endres, Ralf, Trappe, Jörg, Drueckes, Peter
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Benzoxazoles - chemical synthesis
Benzoxazoles - chemistry
Benzoxazoles - pharmacokinetics
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
JAK1
JAK2
JAK2 inhibitor
JAK3
Janus kinase
Janus Kinase 2 - antagonists & inhibitors
Janus Kinase 2 - metabolism
Kinase inhibitors
Medical sciences
Pharmacology. Drug treatments
Protein Kinase Inhibitors - chemical synthesis
Protein Kinase Inhibitors - chemistry
Protein Kinase Inhibitors - pharmacokinetics
Rats
Structure-Activity Relationship
Tyk2
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Description
Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.01.069