1049686-36-3Relevant academic research and scientific papers
Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)-A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer's Disease
Scott, Jack D.,Li, Sarah W.,Brunskill, Andrew P. J.,Chen, Xia,Cox, Kathleen,Cumming, Jared N.,Forman, Mark,Gilbert, Eric J.,Hodgson, Robert A.,Hyde, Lynn A.,Jiang, Qin,Iserloh, Ulrich,Kazakevich, Irina,Kuvelkar, Reshma,Mei, Hong,Meredith, John,Misiaszek, Jeffrey,Orth, Peter,Rossiter, Lana M.,Slater, Meagan,Stone, Julie,Strickland, Corey O.,Voigt, Johannes H.,Wang, Ganfeng,Wang, Hongwu,Wu, Yusheng,Greenlee, William J.,Parker, Eric M.,Kennedy, Matthew E.,Stamford, Andrew W.
, p. 10435 - 10450 (2016/12/16)
Verubecestat 3 (MK-8931), a diaryl amide-substituted 3-imino-1,2,4-thiadiazinane 1,1-dioxide derivative, is a high-affinity β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor currently undergoing Phase 3 clinical evaluation for the treat
Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor
Cumming, Jared N.,Smith, Elizabeth M.,Wang, Lingyan,Misiaszek, Jeffrey,Durkin, James,Pan, Jianping,Iserloh, Ulrich,Wu, Yusheng,Zhu, Zhaoning,Strickland, Corey,Voigt, Johannes,Chen, Xia,Kennedy, Matthew E.,Kuvelkar, Reshma,Hyde, Lynn A.,Cox, Kathleen,Favreau, Leonard,Czarniecki, Michael F.,Greenlee, William J.,McKittrick, Brian A.,Parker, Eric M.,Stamford, Andrew W.
, p. 2444 - 2449 (2012/05/19)
From an initial lead 1, a structure-based design approach led to identification of a novel, high-affinity iminohydantoin BACE1 inhibitor that lowers CNS-derived Aβ following oral administration to rats. Herein we report SAR development in the S3 and F′ subsites of BACE1 for this series, the synthetic approaches employed in this effort, and in vivo data for the optimized compound.
