140700-64-7Relevant articles and documents
Discovery of novel triazolobenzazepinones as γ-secretase modulators with central Aβ42 lowering in rodents and rhesus monkeys
Fischer, Christian,Zultanski, Susan L.,Zhou, Hua,Methot, Joey L.,Shah, Sanjiv,Hayashi, Ikuo,Hughes, Bethany L.,Moxham, Christopher M.,Bays, Nathan W.,Smotrov, Nadya,Hill, Armetta D.,Pan, Bo-Sheng,Wu, Zhenhua,Moy, Lily Y.,Tanga, Flobert,Kenific, Candia,Cruz, Jonathan C.,Walker, Deborah,Bouthillette, Melanie,Nikov, George N.,Deshmukh, Sujal V.,Jeliazkova-Mecheva, Valentina V.,Diaz, Damaris,Michener, Maria S.,Cook, Jacquelynn J.,Munoz, Benito,Shearman, Mark S.
, p. 3488 - 3494 (2015/08/06)
Abstract Synthesis and SAR studies of novel triazolobenzazepinones as gamma secretase modulators (GSMs) are presented in this communication. Starting from our azepinone leads, optimization studies toward improving central lowering of Aβ42 led to the discovery of novel benzo-fused azepinones. Several benzazepinones were profiled in vivo and found to lower brain Aβ42 levels in Sprague Dawley rats and transgenic APP-YAC mice in a dose-dependent manner after a single oral dose. Compound 34 was further progressed into a pilot study in our cisterna-magna-ported rhesus monkey model, where we observed robust lowering of CSF Aβ42 levels.
A convergent asymmetric synthesis of a growth hormone secretagogue
Zheng, Nan,Armstrong III, Joseph D.,Eng, Kan K.,Keller, Jennifer,Liu, Tom,Purick, Robert,Lynch, Joseph,Hartner, Frederick W.,Volante
, p. 3435 - 3446 (2007/10/03)
Described herein is a convergent asymmetric synthesis of growth hormone secretagogue (GHS) suitable for large-scale preparations. Key features include: (1) an improved method for α-iodination of a lactam; (2) a novel synthesis of a disubstituted urea usin
Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives: A novel series of mixed dopamine D2/D4 receptor antagonists
Zhao, He,Thurkauf, Andrew,Braun, Julia,Brodbeck, Robin,Kieltyka, Andrzej
, p. 2119 - 2122 (2007/10/03)
3-Piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives (δ-lactams) were designed, synthesized, and identified as a new series of mixed dopamine D2/D4 receptor antagonists. To further the structure-activity relationship (SAR) study, 3-piperazinylindolin-2-ones (γ-lactams) and 3-piperazinyl-3H,4H,5H-benzo[f]azepin-2-ones (ε-lactams) were also prepared and examined. (C) 2000 Elsevier Science Ltd.