Janus kinase inhibitor

Sakamoto H, Yasukawa H, Masuhara M, Tanimura S, Sasaki A, Yuge K, Ohtsubo M, Ohtsuka A, Fujita T, Ohta T, Furukawa Y, Iwase S, Yamada H, Yoshimura A A Janus kinase inhibitor, JAB, is an interferon-y-inducible gene and confers resistance to interferons. Blood 1998 92 1668-1676. 

Tasocitinib Tasocitinib (CP-690,550) is an orally active Janus kinase inhibitor in development for prophylaxis of acute rejection after kidney transplantation and for treatment of autoimmune diseases. In a population pharmacokinetic analysis co-administration of tasocitinib did not influence systemic exposure to mycophenolic acid [99. ... 

Krishnaswami S, Kudlacz E, Wang R, Chan G (2011) A supratherapentic dose of the Janus kinase inhibitor tasocitinib (CP-690,550) does not prolong QTc interval in healthy participants. J Clin Pharmacol 51 1256-1263... 

In 2009, Lin et al. reported an enantioselective synthesis of an important Janus kinase inhibitor, INCBO18424, the key step of which was an asymmetric aza-Michael addition of pyrazoles to an a,p-unsaturated aldehyde catalysed by a chiral diarylprolinol silyl ether. The use of benzoic acid or 4-nitrobenzoic acid as an additive was shown to increase the reaction rate. The highest enantioselectivities of up to 93% ee were observed for the reactions using the more sterically hindered organocatalysts (Scheme 1.68). 

Rodgers JD, Shepard S, Arvanitis AG Wang H, Storace L, Folmer B, Shao L, Zhu W, Glenn JP (2010) N-(Hetero)aryl-pyrroUdine derivatives of pyrzol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d] pyrimidines as janus kinase inhibitors. Patent W02010135650 (Al), 25 Nov 2010... 

Changelian PS, Flanagan ME, Ball DJ et al (2003) Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. Science 302 875-878... 

Uckun, F.M., Thoen, J., Chen, H., Sudbeck, E., Mao, C., Malaviya, R., Liu, X.-P. and Chen, C.-L. (2002) CYP1A-mediated metabolism of the janus kinase-3 inhibitor 4-(4 -hydroxyphenyl)-amino-6,7-dimethoxyquinazoline structural basis for inactivation by regioselective o-demethylation. Drug Metabolism and Disposition The Biological Fate of Chemicals, 30 (1), 74—85. 

Li WQ, Dehnade F, Zafarullah M (2001) Oncostatin M-induced matrix metalloproteinase and tissue inhibitor of metalloproteinase-3 genes expression in chondrocytes requires Janus kinase/STAT signaling pathway. J Immunol 166 3491-3498... 

Chen, X., Wilson, L.J., Malaviya, R., Argentieri, R.L., and Yang, S.-M. (2008) Virtual screening to successfully identify novel Janus kinase 3 inhibitors a sequential focused screening approach. Journal of Medicinal Chemistry, 51, 7015-7019. 

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