2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2
Constitutive activation of the EPO/JAK2 signaling cascade has recently been implicated in a variety of myeloproliferative disorders including polycythemia vera, essential thrombocythemia and myelofibrosis. In an effort to uncover therapeutic potential of blocking the EPO/JAK2 signaling cascade, we sought to discover selective inhibitors that block the kinase activity of JAK2. Herein, we describe the discovery and structure based optimization of a novel series of 2-amino-pyrazolo[1,5-a]pyrimidines that exhibit potent inhibition of JAK2.
Ledeboer, Mark W.,Pierce, Albert C.,Duffy, John P.,Gao, Huai,Messersmith, David,Salituro, Francesco G.,Nanthakumar, Suganthini,Come, Jon,Zuccola, Harmon J.,Swenson, Lora,Shlyakter, Dina,Mahajan, Sudipta,Hoock, Thomas,Fan, Bin,Tsai, Wan-Jung,Kolaczkowski, Elaine,Carrier, Scott,Hogan, James K.,Zessis, Richard,Pazhanisamy,Bennani, Youssef L.
scheme or table
p. 6529 - 6533
(2010/05/18)
PYRAZOLO [1,5-a] PYRIMIDINES USEFUL AS JAK2 INHIBITORS
The present invention relates to compounds of formula (I) useful as selective inhibitors of JAK2 kinase. The invention also provides pharmaceutical acceptable compositions comprising said compounds and methods of using the compositions in the treatment of
-
Page/Page column 80
(2009/08/14)
More Articles about upstream products of 1169687-29-9