Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)

Christopher Burns; David G Bourke; Laura Andrau; Xianyong Bu; Susan Ann Charman; Andrew C Donohue; Emmanuelle Fantino; Michelle Farrugia; John T Feutrill; Max Joffe; R Marcel Kling; Margarita Kurek; Tracy L Nero; Thao Nguyen; James T Palmer; Ian D Phillips; David Shackleford; Harrison Sikanyika; Michelle Styles; Stephen Su; H R Treutlein; Jun Zeng; Andrew Frederick Wilks

Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)

Christopher Burns, David G Bourke, Laura Andrau, Xianyong Bu, Susan Ann Charman, Andrew C Donohue, Emmanuelle Fantino, Michelle Farrugia, John T Feutrill, Max Joffe, R Marcel Kling, Margarita Kurek, Tracy L Nero, Thao Nguyen, James T Palmer, Ian D Phillips, David Shackleford, Harrison Sikanyika, Michelle Styles, Stephen SuH R Treutlein, Jun Zeng, Andrew Frederick Wilks

Research output: Contribution to journal › Article › Research › peer-review

68 Citations (Scopus)

Abstract

The 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.

Original language	English
Pages (from-to)	5887 - 5892
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	20
Publication status	Published - 2009

Cite this

Burns, C., Bourke, D. G., Andrau, L., Bu, X., Charman, S. A., Donohue, A. C., Fantino, E., Farrugia, M., Feutrill, J. T., Joffe, M., Kling, R. M., Kurek, M., Nero, T. L., Nguyen, T., Palmer, J. T., Phillips, I. D., Shackleford, D., Sikanyika, H., Styles, M., ... Wilks, A. F. (2009). Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). Bioorganic and Medicinal Chemistry Letters, 19(20), 5887 - 5892.

@article{9d8ab9f0266c4832a2acd1aa0b812892,

title = "Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)",

abstract = "The 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.",

author = "Christopher Burns and Bourke, \{David G\} and Laura Andrau and Xianyong Bu and Charman, \{Susan Ann\} and Donohue, \{Andrew C\} and Emmanuelle Fantino and Michelle Farrugia and Feutrill, \{John T\} and Max Joffe and Kling, \{R Marcel\} and Margarita Kurek and Nero, \{Tracy L\} and Thao Nguyen and Palmer, \{James T\} and Phillips, \{Ian D\} and David Shackleford and Harrison Sikanyika and Michelle Styles and Stephen Su and Treutlein, \{H R\} and Jun Zeng and Wilks, \{Andrew Frederick\}",

year = "2009",

language = "English",

volume = "19",

pages = "5887 -- 5892",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier",

number = "20",

}

Burns, C, Bourke, DG, Andrau, L, Bu, X, Charman, SA, Donohue, AC, Fantino, E, Farrugia, M, Feutrill, JT, Joffe, M, Kling, RM, Kurek, M, Nero, TL, Nguyen, T, Palmer, JT, Phillips, ID, Shackleford, D, Sikanyika, H, Styles, M, Su, S, Treutlein, HR, Zeng, J & Wilks, AF 2009, 'Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)', Bioorganic and Medicinal Chemistry Letters, vol. 19, no. 20, pp. 5887 - 5892.

TY - JOUR

T1 - Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)

AU - Burns, Christopher

AU - Bourke, David G

AU - Andrau, Laura

AU - Bu, Xianyong

AU - Charman, Susan Ann

AU - Donohue, Andrew C

AU - Fantino, Emmanuelle

AU - Farrugia, Michelle

AU - Feutrill, John T

AU - Joffe, Max

AU - Kling, R Marcel

AU - Kurek, Margarita

AU - Nero, Tracy L

AU - Nguyen, Thao

AU - Palmer, James T

AU - Phillips, Ian D

AU - Shackleford, David

AU - Sikanyika, Harrison

AU - Styles, Michelle

AU - Su, Stephen

AU - Treutlein, H R

AU - Zeng, Jun

AU - Wilks, Andrew Frederick

PY - 2009

Y1 - 2009

N2 - The 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.

AB - The 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.

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UR - https://www.scopus.com/pages/publications/70349200694

M3 - Article

SN - 0960-894X

VL - 19

SP - 5887

EP - 5892

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 20

ER -

Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)

Abstract

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