1036242-16-6Relevant articles and documents
TRICYCLIC HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF JANUS KINASE
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Page/Page column 34-35, (2010/04/25)
The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in
A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors
Wang, Tiansheng,Ledeboer, Mark W.,Duffy, John P.,Pierce, Albert C.,Zuccola, Harmon J.,Block, Eric,Shlyakter, Dina,Hogan, James K.,Bennani, Youssef L.
scheme or table, p. 153 - 156 (2010/04/02)
Pictet-Spengler condensation of aldehydes or alpha-keto-esters with 4-(2-anilinophenyl)-7-azaindole (11) or deazapurine (12) gave high yields of the 3,4-fused cyclic compounds. SAR studies, by varying the substituted benzaldehyde components, lead to the discovery of a series of potent JAK2 kinase inhibitors.
Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole
Wang, Tiansheng,Duffy, John P.,Wang, Jian,Halas, Summer,Salituro, Francesco G.,Pierce, Albert C.,Zuccola, Harmon J.,Black, James R.,Hogan, James K.,Jepson, Scott,Shlyakter, Dina,Mahajan, Sudipta,Gu, Yong,Hoock, Thomas,Wood, Mark,Furey, Brinley F.,Frantz, J. Daniel,Dauffenbach, Lisa M.,Germann, Ursula A.,Fan, Bin,Namchuk, Mark,Bennani, Youssef L.,Ledeboer, Mark W.
supporting information; experimental part, p. 7938 - 7941 (2010/06/20)
The synthesis and characterization of a novel polycyclic azaindole based derivative is disclosed, and its binding to JAK2 is described. The compound is further evaluated for its ability to block the EPO/JAK2 signaling cascade in vitro and in vivo.
