1093871-74-9Relevant academic research and scientific papers
Thiophene carboxamide inhibitors of JAK2 as potential treatments for myleoproliferative neoplasms
Haidle, Andrew M.,Zabierek, Anna A.,Childers, Kaleen K.,Rosenstein, Craig,Mathur, Anjili,Altman, Michael D.,Chan, Grace,Xu, Lin,Bachman, Eric,Mo, Jan-Rung,Bouthillette, Melaney,Rush, Thomas,Tempest, Paul,Marshall, C. Gary,Young, Jonathan R.
, p. 1968 - 1973 (2014/04/17)
A series of carboxamide-substituted thiophenes demonstrating inhibition of JAK2 is described. Development of this chemical series began with the bioisosteric replacement of a urea substituent by a pyridyl ring. Issues of chemical and metabolic stability were solved using the results of both in vitro and in vivo studies, ultimately delivering compounds such as 24 and 25 that performed well in an acute PK/PD model measuring p-STAT5 inhibition.
INHIBITORS OF JANUS KINASES
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Page/Page column 113, (2009/01/23)
The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
