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.
Gerspacher
Marc
M
Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4002 Basel, Switzerland. marc.gerspacher@novartis.com
Furet
Pascal
P
Pissot-Soldermann
Carole
C
Gaul
Christoph
C
Holzer
Philipp
P
Vangrevelinghe
Eric
E
Lang
Marc
M
Erdmann
Dirk
D
Radimerski
Thomas
T
Regnier
Catherine H
CH
Chene
Patrick
P
De Pover
Alain
A
Hofmann
Francesco
F
Baffert
Fabienne
F
Buhl
Thomas
T
Aichholz
Reiner
R
Blasco
Francesca
F
Endres
Ralf
R
Trappe
Jörg
J
Drueckes
Peter
P
D000284:Administration, Oral; D000818:Animals; D001583:Benzoxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D053614:Janus Kinase 2 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D013329:Structure-Activity Relationship
D001583:Benzoxazoles; D047428:Protein Kinase Inhibitors; D053614:Janus Kinase 2