Search Results - "Engstrom, Kenneth M."

Validation of Diacyl Glycerolacyltransferase I as a Novel Target for the Treatment of Obesity and Dyslipidemia Using a Potent and Selective Small Molecule Inhibitor by Zhao, Gang, Souers, Andrew J, Voorbach, Martin, Falls, H. Doug, Droz, Brian, Brodjian, Sevan, Lau, Yau Yi, Iyengar, Rajesh R, Gao, Ju, Judd, Andrew S, Wagaw, Seble H, Ravn, Matthew M, Engstrom, Kenneth M, Lynch, John K, Mulhern, Mathew M, Freeman, Jennifer, Dayton, Brian D, Wang, Xiaojun, Grihalde, Nelson, Fry, Dennis, Beno, David W. A, Marsh, Kennan C, Su, Zhi, Diaz, Gilbert J, Collins, Christine A, Sham, Hing, Reilly, Regina M, Brune, Michael E, Kym, Philip R

“…A highly potent and selective DGAT-1 inhibitor was identified and used in rodent models of obesity and postprandial chylomicron excursion to validate DGAT-1…”
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Practical Considerations for the Formation of Acyl Imidazolides from Carboxylic Acids and N,N′‑Carbonyldiimidazole: The Role of Acid Catalysis by Engstrom, Kenneth M

“…The conversion of carboxylic acids to acyl imidazolides using N,N′-carbonyldiimidazole (CDI) is hampered by the presence of alkali salts of the carboxylic…”
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Implications of the Conformationally Flexible, Macrocyclic Structure of the First-Generation, Direct-Acting Anti-Viral Paritaprevir on Its Solid Form Complexity and Chameleonic Behavior by Sheikh, Ahmad Y., Mattei, Alessandra, Miglani Bhardwaj, Rajni, Hong, Richard S., Abraham, Nathan S., Schneider-Rauber, Gabriela, Engstrom, Kenneth M., Diwan, Moiz, Henry, Rodger F., Gao, Yi, Juarez, Vivian, Jordan, Erin, DeGoey, David A., Hutchins, Charles W.

“…Direct-acting antiviral regimens have transformed therapeutic management of hepatitis C across all prevalent genotypes. Most of the chemical matter in these…”
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Gram Scale Synthesis of the Glucuronide Metabolite of ABT-724 by Engstrom, Kenneth M, Daanen, Jerome F, Wagaw, Seble, Stewart, Andrew O

“…A gram scale synthesis of the glucuronide metabolite of ABT-724 is reported. Glycosidic coupling between a trichloroacetimidate glucuronyl donor and a…”
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The Stability of N,N -Carbonyldiimidazole Toward Atmospheric Moisture by Engstrom, Kenneth M, Sheikh, Ahmad, Ho, Raimundo, Miller, Robert W

“…N,N -Carbonyldiimidazole (CDI) is known to be sensitive to degradation by atmospheric moisture. This work details some mechanistic aspects of CDI degradation…”
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Development of a Large-Scale Route to Glecaprevir: Synthesis of the Side Chain and Final Assembly by Hill, David R, Abrahamson, Michael J, Lukin, Kirill A, Towne, Timothy B, Engstrom, Kenneth M, Reddy, Rajarathnam E, Kielbus, Angelica B, Pelc, Matthew J, Mei, Jianzhang, Nere, Nandkishor K, Chen, Shuang, Henry, Rodger, Chemburkar, Sanjay, Ding, Chen, Zhang, Hongqiang, Cink, Russell D

“…The preceding article described the development of the large-scale synthetic route to macrocycle 3 of glecaprevir (1), a potent HCV protease inhibitor. This…”
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Development of a Large-Scale Route to Glecaprevir: Synthesis of the Macrocycle via Intramolecular Etherification by Kallemeyn, Jeffrey M, Engstrom, Kenneth M, Pelc, Matthew J, Lukin, Kirill A, Morrill, Westin H, Wei, Haojuan, Towne, Timothy B, Henle, Jeremy, Nere, Nandkishor K, Welch, Dennie S, Shekhar, Shashank, Ravn, Matthew M, Zhao, Gang, Fickes, Michael G, Ding, Chen, Vinci, John C, Marren, James, Cink, Russell D

“…Glecaprevir was identified as a potent hepatitis C virus (HCV) protease inhibitor, and a large-scale synthesis was required to support the late-stage clinical…”
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Risk Assessment of the Leachables’ Profile for Small-Molecule Pharmaceutical Drug Substances by Reddy, Rajarathnam E, Hu, Wenbin, Lowry, Brian R, Fogle, Jace L, Malick, Robert E, Erexson, Greg, Westerberg, John M, Carragher, Adelia L, Robinson, Emily E, Orihuela, Carlos A, Hillier, Michael C, Davis, Steven R, Kruk, Paul E, Ide, Nathan D, Mlinar, Laurie, Mulhern, Mathew M, Engstrom, Kenneth M, Chaaya, Elie, McKee, Laura A, Manning, Patrick E, Tirino, Pasquale, Joudioux, Roberta, Cornelio, Lisa

“…Appropriate control of impurities from all sources is critically important during the development of a pharmaceutical product. One class of impurity that has…”
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Improved Synthesis of 3-Substituted-4-amino-[3,2-c]-thienopyridines by Engstrom, Kenneth M, Baize, Amanda L, Franczyk, Thaddeus S, Kallemeyn, Jeffrey M, Mulhern, Mathew M, Rickert, Robert C, Wagaw, Seble

“…Two syntheses of 3-substituted-4-amino-[3,2-c]thienopyridines have been developed to replace the standard literature route to these compounds, which uses…”
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Development of a Scalable Synthesis of Dipeptidyl Peptidase-4 Inhibitor ABT-279 by McDermott, Todd S, Bhagavatula, Lakshmi, Borchardt, Thomas B, Engstrom, Kenneth M, Gandarilla, Jorge, Kotecki, Brian J, Kruger, Albert W, Rozema, Michael J, Sheikh, Ahmad Y, Wagaw, Seble H, Wittenberger, Steven J

“…A convergent, scalable synthesis of dipeptidyl peptidase-4 inhibitor, ABT-279, has been developed and demonstrated on multikilogram scale. The…”
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Process Development of a Diacyl Glycerolacyltransferase-1 Inhibitor by Ravn, Matthew M, Wagaw, Seble H, Engstrom, Kenneth M, Mei, Jianzhang, Kotecki, Brian, Souers, Andrew J, Kym, Philip R, Judd, Andrew S, Zhao, Gang

“…A synthesis of a selective diacyl glycerolacyltransferase-1 (DGAT-1) inhibitor, 1, is described. The synthesis illustrates a diketone Favorskii reaction on 9…”
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A Convergent Process for the Preparation of Adamantane 11-β-HSD-1 Inhibitors by Becker, Calvin L, Engstrom, Kenneth M, Kerdesky, Francis A, Tolle, John C, Wagaw, Seble H, Wang, Weifeng

“…A convergent, scalable process was developed for the synthesis of adamantane 11-β-hydroxysteroid dehydrogenase-1 inhibitors…”
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Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists by Vasudevan, Anil, Souers, Andrew J., Freeman, Jennifer C., Verzal, Mary K., Gao, Ju, Mulhern, Mathew M., Wodka, Derek, Lynch, John K., Engstrom, Kenneth M., Wagaw, Seble H., Brodjian, Sevan, Dayton, Brian, Falls, Doug H., Bush, Eugene, Brune, Michael, Shapiro, Robin D., Marsh, Kennan C., Hernandez, Lisa E., Collins, Christine A., Kym, Philip R.

“…The synthesis and biological evaluation of novel 3-amino indazole melanin concentrating hormone receptor-1 antagonists are reported, several of which…”
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Chlorination at the 8-Position of a Functionalized Quinolone and the Synthesis of Quinolone Antibiotic ABT-492 by Barnes, David M, Christesen, Alan C, Engstrom, Kenneth M, Haight, Anthony R, Hsu, Margaret C, Lee, Elaine C, Peterson, Matthew J, Plata, Daniel J, Raje, Prasad S, Stoner, Eric J, Tedrow, Jason S, Wagaw, Seble

“…The total synthesis of quinolone antibiotic ABT-492 has been achieved in 67% yield over nine steps from 2,4,5-trifluorobenzoic acid. The highlights of this…”
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Process development of ABT-450 – A first generation NS3/4A protease inhibitor for HCV by Caspi, Daniel D., Cink, Russell D., Clyne, Dean, Diwan, Moiz, Engstrom, Kenneth M., Grieme, Timothy, Mei, Jianzhang, Miller, Robert W., Mitchell, Clifford, Napolitano, José G., Nere, Nandkishor, Ravn, Matthew M., Sheikh, Ahmad, Wagaw, Seble, Zhang, Hongqiang

“…ABT-450 (8), a potent hepatitis C (HCV) NS3/4A protease inhibitor, was approved as part of AbbVie's first generation HCV treatment for the United States in…”
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Total Synthesis of (+)-Pyrenolide D This research was supported by the National Institutes of Health, Glaxo Wellcome Inc., the Alfred P. Sloan Foundation, and the Arnold and Mabel Beckman Foundation by Engstrom, Kenneth M., Mendoza, Mario R., Navarro-Villalobos, Mauricio, Gin, David Y.

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Synthesis of the glucuronide metabolite of ABT-751 by Engstrom, Kenneth M., Henry, Rodger F., Marsden, Ian

“…A linear synthesis of the glucuronide metabolite of ABT-751 was replaced with a convergent synthesis that features direct glycosidic coupling between the…”
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Total Synthesis of (+)-Pyrenolide D by Engstrom, Kenneth M., Mendoza, Mario R., Navarro-Villalobos, Mauricio, Gin, David Y.

“…The direct stereoselective IIII‐mediated oxidative ring contraction of a protected 6‐deoxy‐D‐gulal substrate to form a highly functionalized tetrahydrofurfural…”
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Total Synthesis of (+)-Pyrenolide D by Engstrom, Kenneth M., Mendoza, Mario R., Navarro-Villalobos, Mauricio, Gin, David Y.

“…Die direkte stereoselektive IIII‐vermittelte oxidative Ringverengung eines geschützten 6‐Desoxy‐D‐gulals zu einem hochfunktionalisierten…”
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Total Synthesis of (+)-Pyrenolide D by Engstrom, Kenneth M., Mendoza, Mario R., Navarro-Villalobos, Mauricio, Gin, David Y.

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