Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).
A series of phenylaminopyrimidines has been identified as inhibitors of Janus kinases (JAKs). Development of this initial series led to the potent JAK2/JAK1 inhibitor CYT387 (N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-benzamide). Details of synthesis and SAR studies of these compounds are reported.
Burns
Christopher J
CJ
Cytopia Research Pty Ltd, 576 Swan St, Richmond, VIC 3121, Australia.
Bourke
David G
DG
Andrau
Laura
L
Bu
Xianyong
X
Charman
Susan A
SA
Donohue
Andrew C
AC
Fantino
Emmanuelle
E
Farrugia
Michelle
M
Feutrill
John T
JT
Joffe
Max
M
Kling
Marcel R
MR
Kurek
Margarita
M
Nero
Tracy L
TL
Nguyen
Thao
T
Palmer
James T
JT
Phillips
Ian
I
Shackleford
David M
DM
Sikanyika
Harrison
H
Styles
Michelle
M
Su
Stephen
S
Treutlein
Herbert
H
Zeng
Jun
J
Wilks
Andrew F
AF
D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001665:Binding Sites; D018938:Caco-2 Cells; D045744:Cell Line, Tumor; D003198:Computer Simulation; D006801:Humans; D053614:Janus Kinase 2 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008297:Male; D020033:Protein Isoforms / Q000037:antagonists & inhibitors / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
D001549:Benzamides; D020033:Protein Isoforms; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; C546012:N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide; D053614:Janus Kinase 2