1201186-05-1Relevant articles and documents
Structure activity optimization of 6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazines as Jak1 kinase inhibitors
Friedman, Michael,Frank, Kristine E.,Aguirre, Ana,Argiriadi, Maria A.,Davis, Heather,Edmunds, Jeremy J.,George, Dawn M.,George, Jonathan S.,Goedken, Eric,Fiamengo, Bryan,Hyland, Deborah,Li, Bin,Murtaza, Anwar,Morytko, Michael,Somal, Gagandeep,Stewart, Kent,Tarcsa, Edit,Van Epps, Stacy,Voss, Jeffrey,Wang, Lu,Woller, Kevin,Wishart, Neil
, p. 4399 - 4404 (2015/10/12)
Previous work investigating tricyclic pyrrolopyrazines as kinase cores led to the discovery that 1-cyclohexyl-6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazine (12) had Jak inhibitory activity. Herein we describe our initial efforts to develop orally bioavailable analogs of 12 with improved selectivity of Jak1 over Jak2.
TRICYCLIC INHIBITORS OF JAK
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, (2011/02/18)
The present invention relates to the use of novel compounds of Formulae I-II, wherein the variables R, X1, X2, X3, Y1, Y2, Y3, Z1, and Z2 are defined as described here