34825-81-5Relevant academic research and scientific papers
PYRIDYL OR PYRIMIDYL MTOR KINASE INHIBITORS
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Page/Page column 88, (2020/12/30)
The invention relates to compounds or pharmaceutically acceptable salts thereof of formula (I): (I) wherein R1, R2, R3, R4, R4' and R5 are as defined in the description and claims; and comp
1,4-THIAZINE DIOXIDE AND 1,2,4-THIADIAZINE DIOXIDE DERIVATIVES AS BETA-SECRETASE INHIBITORS AND METHODS OF USE
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Page/Page column 90-91, (2018/07/05)
The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A, X, R2, R2', R3, R4, R5, R6, and R7 of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, and other central nervous system conditions.
A Next Generation Synthesis of BACE1 Inhibitor Verubecestat (MK-8931)
Thaisrivongs, David A.,Morris, William J.,Tan, Lushi,Song, Zhiguo J.,Lyons, Thomas W.,Waldman, Jacob H.,Naber, John R.,Chen, Wenyong,Chen, Lu,Zhang, Baoyun,Yang, Jun
, p. 1568 - 1571 (2018/03/23)
The development of a commercial manufacturing route to verubecestat (MK-8931) is described, highlights of which include the application of a continuous processing step to outcompete fast proton transfer in a Mannich-type ketimine addition, a copper-cataly
N-[2-(3-AMINO-2,5-DIMETHYL-1,1-DIOXIDO-5,6-DIHYDRO-2H-1,2,4-THIADIAZIN-5-YL)-1,3-THIAZOL-4-YL] AMIDES USEFUL AS BACE INHIBITORS
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Page/Page column 39; 40; 41, (2017/04/11)
The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, wherein the variables R1, R2 and R3/su
C5-C6-CARBOCYCLIC FUSED IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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Page/Page column 43; 44, (2017/07/29)
In its many embodiments, the present invention provides certain C5-C6-carbocyclic fused iminothiazine dioxide compounds, including compounds Formula (I): and tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, ring A, RA, m, -L1-, ring B, RB, n, q, 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.
PROCESSES FOR THE PREPARATION OF A BACE INHIBITOR
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Page/Page column 33; 34, (2017/09/08)
This invention provides an improved processes for the preparation of verubecestat (Compound of Formula (I)), a potent inhibitor of BACE-1 and BACE-2.
C5-C6-FUSED TRICYCLIC IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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Page/Page column 48; 49, (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.
Synthesis of Verubecestat, a BACE1 Inhibitor for the Treatment of Alzheimer's Disease
Thaisrivongs, David A.,Miller, Steven P.,Molinaro, Carmela,Chen, Qinghao,Song, Zhiguo J.,Tan, Lushi,Chen, Lu,Chen, Wenyong,Lekhal, Azzeddine,Pulicare, Sarah K.,Xu, Yanke
, p. 5780 - 5783 (2016/11/29)
Verubecestat is an inhibitor of β-secretase being evaluated for the treatment of Alzheimer's disease. The first-generation route relies on an amide coupling with a functionalized aniline, the preparation of which introduces synthetic inefficiencies. The s
IMINOTHIADIAZINE DIOXIDES BEARING AN AMINE-LINKED SUBSTITUENT AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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Page/Page column 35; 36, (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.
NOVEL CRYSTALLINE FORMS OF A BACE INHIBITOR, COMPOSITIONS, AND THEIR USE
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Page/Page column 24-25, (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
