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.
Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4002 Basel, Switzerland. marc.gerspacher@novartis.com
Marc
M
Gerspacher
Pascal
P
Furet
Carole
C
Pissot-Soldermann
Christoph
C
Gaul
Philipp
P
Holzer
Eric
E
Vangrevelinghe
Marc
M
Lang
Dirk
D
Erdmann
Thomas
T
Radimerski
Catherine H
CH
Regnier
Patrick
P
Chene
Alain
A
De Pover
Francesco
F
Hofmann
Fabienne
F
Baffert
Thomas
T
Buhl
Reiner
R
Aichholz
Francesca
F
Blasco
Ralf
R
Endres
Jörg
J
Trappe
Peter
P
Drueckes
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