190906-91-3Relevant academic research and scientific papers
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 HEPATITIS B VIRUS INFECTION
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Page/Page column 42; 43; 44, (2018/05/24)
The present invention provides novel compounds having the general formula: wherein R1, R2 and R3 are as described herein, compositions including the compounds and methods of using the compounds.
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.
A 1 - tert-butoxy carbonyl -2 - methyl -4 - piperidone method for the synthesis of
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Paragraph 0042-0044, (2016/12/07)
The invention discloses a synthesis method of 1-tertbutyloxycarbonyl-2-methyl-4-piperidone. The synthesis method comprises the following steps: step one, synthesis of 1-Cbz-2-methyl-3,4-dihydro-4-piperidone; step two, synthesis of 1-Cbz-2-methyl-4-piperid
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
HEPATITIS B ANTIVIRAL AGENTS
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Page/Page column 208, (2013/07/05)
The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
LACTAMS AS BETA SECRETASE INHIBITORS
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Page/Page column 25, (2013/02/28)
Compound and pharmaceutically acceptable salts of the compound are disclosed, wherein the compound has the structure (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermedia
LACTAMS AS BETA SECRETASE INHIBITORS
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Page/Page column 37, (2010/07/10)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment methods of synthesis,
Stereoselective synthesis of 4-amino-2, 3-unsaturated-N-Cbz-imino-O- glycosides via new diastereoisomeric N-Cbz-imino glycal-derived allyl N-nosyl aziridines
Bussolo, Valeria Di,Fiasella, Annalisa,Favero, Lucilla,Bertolini, Ferruccio,Crotti, Paolo
supporting information; experimental part, p. 2675 - 2678 (2009/10/10)
The glycosylation of alcohols by the new diastereoisomeric D,L-6-deoxy-N-Cbz-imino glycal-derived allyl N-nosyl aziridines 5 and 6 affords, after deprotection of the 4-(N-nosylamino) group, the corresponding 2,3-unsaturated-N-Cbz-imino-O-glycosides bearin
4-Pyridone derivatives as new inhibitors of bacterial enoyl-ACP reductase FabI
Kitagawa, Hideo,Kumura, Ko,Takahata, Sho,Iida, Maiko,Atsumi, Kunio
, p. 1106 - 1116 (2008/02/01)
Bacterial FAS provides essential fatty acids for use in the assembly of key cellular components. Among them, FabI is an enoyl-ACP reductase which catalyzes the final and rate-limiting step of bacterial FAS. It is a potential target for selective antibacterial action, because it shows low overall sequence homology with mammalian enzymes. Until today, various compounds have been reported as inhibitors of bacterial FabI-inhibitory compounds. To discover novel small-molecular FabI inhibitors, we initially screened our compound library for inhibitory activity toward FabI of Escherichia coli. And discovered 4-pyridone derivatives as a lead compound. Structure optimization studies yielded 4-pyridone derivatives 7n having strong FabI-inhibitory and antibacterial activities against Staphylococcus aureus. There have been no reports concerning 4-pyridone derivatives as FabI inhibitor.
