190906-91-3Relevant articles and documents
A PROCESS FOR THE PREPARATION OF TETRAHYDROPYRIDOPYRIMIDINES
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Page/Page column 12-13, (2020/07/31)
The present invention relates to a process for synthesizing a compound of formula (I), or a pharmaceutically acceptable salt thereof, which is useful for prophylaxis and treatment of a viral disease in a patient relating to hepatitis B infection or a disease caused by hepatitis B infection.
NOVEL TETRAHYDROPYRIDOPYRIMIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HBV INFECTION
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Page/Page column 36; 37, (2018/09/25)
The present invention provides novel compounds having general formula (I), wherein R1 to R4, A, W, Q and Y are as described herein, compositions including the compounds and methods of using the compounds.
Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency
Egbertson, Melissa,McGaughey, Georgia B.,Pitzenberger, Steven M.,Stauffer, Shaun R.,Coburn, Craig A.,Stachel, Shawn J.,Yang, Wenjin,Barrow, James C.,Neilson, Lou Anne,McWherter, Melody,Perlow, Debra,Fahr, Bruce,Munshi, Sanjeev,Allison, Timothy J.,Holloway, Katharine,Selnick, Harold G.,Yang, Zhiqiang,Swestock, John,Simon, Adam J.,Sankaranarayanan, Sethu,Colussi, Dennis,Tugusheva, Katherine,Lai, Ming-Tain,Pietrak, Beth,Haugabook, Shari,Jin, Lixia,Chen,Holahan, Marie,Stranieri-Michener, Maria,Cook, Jacquelynn J.,Vacca, Joseph,Graham, Samuel L.
supporting information, p. 4812 - 4819 (2015/10/28)
The IC50 of a beta-secretase (BACE-1) lead compound was improved ~200-fold from 11 μM to 55 nM through the addition of a single methyl group. Computational chemistry, small molecule NMR, and protein crystallography capabilities were used to com