1286777-82-9Relevant academic research and scientific papers
Iminothiazide dioxide derivative and application thereof
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, (2019/01/22)
The invention discloses an iminothiazide dioxide derivative and application thereof. In particular, the invention relates to a type of novel iminothiazide dioxide derivatives and a pharmaceutical composition comprising the compounds. The derivatives can s
Iminothiadiazine dioxide derivative and application thereof
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, (2019/01/22)
The present invention discloses an iminothiadiazine dioxide derivative and an application thereof, in particular, the present invention relates to a novel iminothiadiazine dioxide derivative and a pharmaceutical composition containing the iminothiadiazine dioxide derivative, which can be used as a BACE-1 inhibitor. The invention also relates to methods of preparing the compound and the pharmaceutical composition, and applications of the compound and the pharmaceutical composition in preparation of a medicine for treating a disease associated with beta-amyloid protein (A-beta), particularly Alzheimer's disease.
Iminothiadiazine dioxide derivative and applications thereof
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, (2019/11/29)
The invention discloses an iminothiadiazine dioxide derivative and applications thereof. Concretely, the invention relates to the novel iminothiadiazine dioxide derivative and a pharmaceutical composition containing the compound. The derivative can be use
Iminothiadiazine dioxide derivative and application thereof
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, (2019/01/06)
The invention discloses an iminothiadiazine dioxide derivative and an application thereof and particularly relates to a type of novel iminothiadiazine dioxide derivatives and medicine compositions comprising these compounds. The compounds can serve as BAC
Imino thiadiazine dioxide derivatives and application thereof
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, (2018/12/13)
The invention discloses imino thiadiazine dioxide derivatives and application thereof. Particularly, the invention relates to a category of novel imino thiadiazine dioxide derivatives and a medicinalcomposition comprising the category of compounds. The im
NOVEL CRYSTALLINE FORMS OF A BACE INHIBITOR, COMPOSITIONS, AND THEIR USE
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, (2016/08/03)
The present invention provides four crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an Aβ pathology and/or a sy
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
NOVEL CRYSTALLINE FORMS OF A BACE INHIBITOR, COMPOSITIONS, AND THEIR USE
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Page/Page column 20-21, (2016/02/29)
The present invention provides a novel synthesis of verubecestat, and two novel crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delay
C5-C6-FUSED TRICYCLIC IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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Page/Page column 48; 50, (2016/04/26)
In its many embodiments, the present invention provides certain C5-C6 fused tricyclic iminothiadiazine compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1A, R2, R3, RA, ring A, RA, m, -L1-, and RL 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.
IMINOTHIADIAZINE DIOXIDES BEARING AN AMINE-LINKED SUBSTITUENT AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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Page/Page column 35; 36; 37, (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.
