191543-36-9Relevant articles and documents
BET INHIBITORS FOR MODULATING DUX4 EXPRESSION IN FSHD
-
Page/Page column 100-101, (2020/07/14)
The present disclosure provides BET inhibitors of the formula: wherein the variables are defined herein, as well as pharmaceutical compositions thereof. The present disclosure also provides methods of treating a patient comprising administering a bromo- and extra-terminal (BET) domain inhibitor for the treatment of FSHD which modulates DUX4 expression. In some embodiments, the present methods comprise using one or more BET inhibitors as a therapeutic agent for the treatment of FSHD patients including patients who are being treated with one or more palliative treatments such as therapy and/or agents which lead to increased muscle mass.
Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153)
Bradbury, Robert H.,Callis, Rowena,Carr, Gregory R.,Chen, Huawei,Clark, Edwin,Feron, Lyman,Glossop, Steve,Graham, Mark A.,Hattersley, Maureen,Jones, Chris,Lamont, Scott G.,Ouvry, Gilles,Patel, Anil,Patel, Joe,Rabow, Alfred A.,Roberts, Craig A.,Stokes, Stephen,Stratton, Natalie,Walker, Graeme E.,Ward, Lara,Whalley, David,Whittaker, David,Wrigley, Gail,Waring, Michael J.
, p. 7801 - 7817 (2016/10/22)
Here we report the discovery and optimization of a series of bivalent bromodomain and extraterminal inhibitors. Starting with the observation of BRD4 activity of compounds from a previous program, the compounds were optimized for BRD4 potency and physical
[1,2,4]TRIAZOLO[4,3-B]PYRIDAZINES FOR USE IN THE TREATMENT OF PROLIFERATIVE DISEASES
-
Page/Page column 59, (2016/04/06)
The invention concerns compounds of Formula (I) (Formula (I)) or pharmaceutically-acceptable salts thereof, wherein R1, R2 and n have any of the meanings defined herein before in the description; processes for their preparation, pharmaceutical compositions containing them and their use as anti-proliferative and/or cell-killing agents.
The ortho-substituted N,N-diacetylaniline as a selective acetylating reagent
Murakami, Yasuoki,Kondo, Kazuhiro,Miki, Kazuki,Akiyama, Yoko,Watanabe, Toshiko,Yokoyama, Yuusaku
, p. 3751 - 3754 (2007/10/03)
Selective acetylation of the less hindered amino group in the presence of the more hindered amino group with the use of 2-trifluoromethyl-N,N-diacetylaniline 2c is described. This acetylation with 2c yielded the corresponding less hindered monoacetamide exclusively, simply, conveniently, and in good yields.
