14678-48-9Relevant articles and documents
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Beckett,A.H. et al.
, p. 1386 - 1388 (1962)
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Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains
Taylor, Alexander M.,Vaswani, Rishi G.,Gehling, Victor S.,Hewitt, Michael C.,Leblanc, Yves,Audia, James E.,Bellon, Steve,Cummings, Richard T.,Co?té, Alexandre,Harmange, Jean-Christophe,Jayaram, Hari,Joshi, Shivangi,Lora, Jose M.,Mertz, Jennifer A.,Neiss, Adrianne,Pardo, Eneida,Nasveschuk, Christopher G.,Poy, Florence,Sandy, Peter,Setser, Jeremy W.,Sims, Robert J.,Tang, Yong,Albrecht, Brian K.
, p. 145 - 150 (2016/03/01)
Inhibition of the bromodomains of the BET family, of which BRD4 is a member, has been shown to decrease myc and interleukin (IL) 6 in vivo, markers that are of therapeutic relevance to cancer and inflammatory disease, respectively. Herein we report substituted benzo[b]isoxazolo[4,5-d]azepines and benzotriazolo[4,3-d][1,4]diazepines as fragment-derived novel inhibitors of the bromodomain of BRD4. Compounds from these series were potent and selective in cells, and subsequent optimization of microsomal stability yielded representatives that demonstrated dose- and time-dependent reduction of plasma IL-6 in mice.
MODULATORS OF HISTONE METHYLTRANSFERASE, AND METHODS OF USE THEREOF
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Page/Page column 156, (2012/06/30)
Disclosed are compounds, pharmaceutical compositions containing the compounds, and the uses of the compounds and compositions as modulators of histone methyltransferases, and for treating diseases influenced by modulation of histone methyltransferase activity.