736053-73-9Relevant academic research and scientific papers
Discovery of potent and selective PKC-θ inhibitors
Cywin, Charles L.,Dahmann, Georg,Prokopowicz III, Anthony S.,Young, Erick R.R.,Magolda, Ronald L.,Cardozo, Mario G.,Cogan, Derek A.,DiSalvo, Darren,Ginn, John D.,Kashem, Mohammed A.,Wolak, John P.,Homon, Carol A.,Farrell, Thomas M.,Grbic, Heather,Hu, Hanbo,Kaplita, Paul V.,Liu, Lisa H.,Spero, Denice M.,Jeanfavre, Deborah D.,O'Shea, Kathy M.,White, Della M.,Woska Jr., Joseph R.,Brown, Maryanne L.
, p. 225 - 230 (2007/10/03)
An uHTS campaign was performed to identify selective inhibitors of PKC-θ. Initial triaging of the hit set based on selectivity and historical analysis led to the identification of 2,4-diamino-5-nitropyrimidines as potent and selective PKC-θ inhibitors. A homology model and initial SAR is presented demonstrating that a 2-arylalkylamino substituent in conjunction with suitable 4-diamino substituent are essential for achieving selectivity over many kinases. Additional hit to lead profiling is presented on selected compounds.
Pyrimidine derivatives useful as inhibitors of PKC-theta
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, (2008/06/13)
Disclosed are novel compounds of formula (I): wherein R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
2,4-DIAMINOPYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF PKC-THETA
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Page 80, (2008/06/13)
Disclosed are novel compounds of formula (I) wherein R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders and processes for preparing these compounds.
