title: Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).
abstract: 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.
authors.affiliation: Cytopia Research Pty Ltd, 576 Swan St, Richmond, VIC 3121, Australia.
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Burns
authors.forename: David G
authors.initials: DG
authors.lastname: Bourke
authors.forename: Laura
authors.initials: L
authors.lastname: Andrau
authors.forename: Xianyong
authors.initials: X
authors.lastname: Bu
authors.forename: Susan A
authors.initials: SA
authors.lastname: Charman
authors.forename: Andrew C
authors.initials: AC
authors.lastname: Donohue
authors.forename: Emmanuelle
authors.initials: E
authors.lastname: Fantino
authors.forename: Michelle
authors.initials: M
authors.lastname: Farrugia
authors.forename: John T
authors.initials: JT
authors.lastname: Feutrill
authors.forename: Max
authors.initials: M
authors.lastname: Joffe
authors.forename: Marcel R
authors.initials: MR
authors.lastname: Kling
authors.forename: Margarita
authors.initials: M
authors.lastname: Kurek
authors.forename: Tracy L
authors.initials: TL
authors.lastname: Nero
authors.forename: Thao
authors.initials: T
authors.lastname: Nguyen
authors.forename: James T
authors.initials: JT
authors.lastname: Palmer
authors.forename: Ian
authors.initials: I
authors.lastname: Phillips
authors.forename: David M
authors.initials: DM
authors.lastname: Shackleford
authors.forename: Harrison
authors.initials: H
authors.lastname: Sikanyika
authors.forename: Michelle
authors.initials: M
authors.lastname: Styles
authors.forename: Stephen
authors.initials: S
authors.lastname: Su
authors.forename: Herbert
authors.initials: H
authors.lastname: Treutlein
authors.forename: Jun
authors.initials: J
authors.lastname: Zeng
authors.forename: Andrew F
authors.initials: AF
authors.lastname: Wilks
mesh_terms: 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
chemical_list: 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