1092499-06-3Relevant academic research and scientific papers
Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors
Pissot-Soldermann, Carole,Gerspacher, Marc,Furet, Pascal,Gaul, Christoph,Holzer, Philipp,McCarthy, Clive,Radimerski, Thomas,Regnier, Catherine H.,Baffert, Fabienne,Drueckes, Peter,Tavares, Gisele A.,Vangrevelinghe, Eric,Blasco, Francesca,Ottaviani, Giorgio,Ossola, Flavio,Scesa, Julien,Reetz, Janitha
scheme or table, p. 2609 - 2613 (2010/07/05)
We have designed and synthesized a novel series of 2,8-diaryl-quinoxalines as Janus kinase 2 inhibitors. Many of the inhibitors show low nanomolar activity against JAK2 and potently suppress proliferation of SET-2 cells in vitro. In addition, compounds from this series have favorable rat pharmacokinetic properties suitable for in vivo efficacy evaluation.
QUINOXALINE DERIVATIVES AS INHIBITORS OF THE TYROSINE KINASE ACTIVITY OF JANUS KINASES
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Page/Page column 77, (2009/01/24)
The present invention relates to quinoxaline compound of the formula (I): wherein R1 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R7; R2 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R8; R3, R4, R5 and R6 are each independently hydrogen or R9; and R7, R8 and R9 are each independently selected from organic and inorganic substituents, their use in therapy of diseases, in particular diseases mediated by the tyrosine kinase activity of Janus kinases, including JAK-2 and JAK-3 kinases
