74389-73-4Relevant academic research and scientific papers
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.
BROMODOMAIN INHIBITORS AND USES THEREOF
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, (2012/11/14)
The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
Synthesis of substituted 5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1,5] benzodiazepines
Kosychova,Stumbreviciute,Pleckaitiene,Janciene,Puodziunaite
, p. 811 - 815 (2007/10/03)
A one-pot synthetic approach to the novel 5,6-dihydro-4H-[1,2,4]triazolo[4, 3-a][1,5]benzodiazepines by thermal cyclization of 4-acylhydrazino-2,3-dihydro- 1H-1,5-benzodiazepines is described.
