1076160-56-9Relevant articles and documents
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.
supporting information, 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
IMINOTHIADIAZINE DIOXIDES BEARING AN AMINE-LINKED SUBSTITUENT AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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Page/Page column 35, (2016/08/17)
In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, ring A, RA, m, ringB, RB, and n are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
C2-CARBOCYCLIC IMINOTHIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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, (2016/01/29)
In its many embodiments, the present invention provides certain C2-carbocyclic iminothiazine dioxide compounds, including compounds Formula (I); or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, ring A, RA, m, ring B, RB, n, ring C, RC and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.