1035211-86-9Relevant academic research and scientific papers
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
NOVEL TRIFLUOROMETHYL-OXADIAZOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
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Page/Page column 50, (2013/06/27)
The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical com
N-HYDROXYACRYLAMIDE COMPOUNDS
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Page/Page column 23, (2008/12/06)
A compound having the following formula (I) : wherein - R1is hydrogen, optionally substituted lower alkyl, cyclo (lower) alkyl, cyclo (higher) alkyl, optionally substituted aryl, optionally substituted heterocyclyl, or aryl-fused cyclo (lower) alkyl, R2 is hydrogen or halogen, Z is CH or N, X is formula (II) R3 is lower alkyl which may be substituted with -OH or optionally substituted aryl, or lower alkanoyl, R4 is hydrogen or lower alkyl, Y is optionally substituted lower alkylene, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.
