MK-5172, a Selective Inhibitor of Hepatitis C Virus NS3/4a Protease with Broad Activity across Genotypes and Resistant Variants
SUMMA, Vincenzo, LUDMERER, Steven W, GATES, Adam T, GRAHAM, Donald J, HARPER, Steven, HAZUDA, Daria J, MCHALE, Carolyn, MONTEAGUDO, Edith, PUCCI, Vincenzo, ROWLEY, Michael, RUDD, Michael T, SORIANO, Aileen, MCCAULEY, John A, STAHLHUT, Mark W, VACCA, Joseph P, OLSEN, David B, LIVERTON, Nigel J, CARROLL, Steven S, FANDOZZI, Christine, BURLEIN, Christine, CLAUDIO, Giuliano, COLEMAN, Paul J, DIMUZIO, Jillian M, FERRARA, Marco, DI FILIPPO, Marcello
Published in Antimicrobial Agents and Chemotherapy (01.08.2012)
Published in Antimicrobial Agents and Chemotherapy (01.08.2012)
Get full text
Journal Article
MK-7009, a Potent and Selective Inhibitor of Hepatitis C Virus NS3/4A Protease
LIVERTON, Nigel J, CARROLL, Steven S, OLSEN, David B, RUDD, Michael T, STAHLHUT, Mark, VACCA, Joseph P, DIMUZIO, Jillian, FANDOZZI, Christine, GRAHAM, Donald J, HAZUDA, Daria, KATHERINE HOLLOWAY, M, LUDMERER, Steven W, MCCAULEY, John A, MCINTYRE, Charles J
Published in Antimicrobial Agents and Chemotherapy (01.01.2010)
Published in Antimicrobial Agents and Chemotherapy (01.01.2010)
Get full text
Journal Article
Discovery of Vaniprevir (MK-7009), a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor
McCauley, John A, McIntyre, Charles J, Rudd, Michael T, Nguyen, Kevin T, Romano, Joseph J, Butcher, John W, Gilbert, Kevin F, Bush, Kimberly J, Holloway, M. Katharine, Swestock, John, Wan, Bang-Lin, Carroll, Steven S, DiMuzio, Jillian M, Graham, Donald J, Ludmerer, Steven W, Mao, Shi-Shan, Stahlhut, Mark W, Fandozzi, Christine M, Trainor, Nicole, Olsen, David B, Vacca, Joseph P, Liverton, Nigel J
Published in Journal of medicinal chemistry (25.03.2010)
Published in Journal of medicinal chemistry (25.03.2010)
Get full text
Journal Article
Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor
Harper, Steven, McCauley, John A, Rudd, Michael T, Ferrara, Marco, DiFilippo, Marcello, Crescenzi, Benedetta, Koch, Uwe, Petrocchi, Alessia, Holloway, M. Katharine, Butcher, John W, Romano, Joseph J, Bush, Kimberly J, Gilbert, Kevin F, McIntyre, Charles J, Nguyen, Kevin T, Nizi, Emanuela, Carroll, Steven S, Ludmerer, Steven W, Burlein, Christine, DiMuzio, Jillian M, Graham, Donald J, McHale, Carolyn M, Stahlhut, Mark W, Olsen, David B, Monteagudo, Edith, Cianetti, Simona, Giuliano, Claudio, Pucci, Vincenzo, Trainor, Nicole, Fandozzi, Christine M, Rowley, Michael, Coleman, Paul J, Vacca, Joseph P, Summa, Vincenzo, Liverton, Nigel J
Published in ACS medicinal chemistry letters (12.04.2012)
Published in ACS medicinal chemistry letters (12.04.2012)
Get full text
Journal Article
Pharmacological Characterization of MK-0974 [N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a Potent and Orally Active Calcitonin Gene-Related Peptide Receptor Antagonist for the Treatment of Migraine
Salvatore, Christopher A, Hershey, James C, Corcoran, Halea A, Fay, John F, Johnston, Victor K, Moore, Eric L, Mosser, Scott D, Burgey, Christopher S, Paone, Daniel V, Shaw, Anthony W, Graham, Samuel L, Vacca, Joseph P, Williams, Theresa M, Koblan, Kenneth S, Kane, Stefanie A
Published in The Journal of pharmacology and experimental therapeutics (01.02.2008)
Published in The Journal of pharmacology and experimental therapeutics (01.02.2008)
Get full text
Journal Article
Molecular Modeling Based Approach to Potent P2−P4 Macrocyclic Inhibitors of Hepatitis C NS3/4A Protease
Liverton, Nigel J, Holloway, M. Katharine, McCauley, John A, Rudd, Michael T, Butcher, John W, Carroll, Steven S, DiMuzio, Jillian, Fandozzi, Christine, Gilbert, Kevin F, Mao, Shi-Shan, McIntyre, Charles J, Nguyen, Kevin T, Romano, Joseph J, Stahlhut, Mark, Wan, Bang-Lin, Olsen, David B, Vacca, Joseph P
Published in Journal of the American Chemical Society (09.04.2008)
Published in Journal of the American Chemical Society (09.04.2008)
Get full text
Journal Article
Potent, Orally Bioavailable Calcitonin Gene-Related Peptide Receptor Antagonists for the Treatment of Migraine: Discovery of N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974)
Paone, Daniel V, Shaw, Anthony W, Nguyen, Diem N, Burgey, Christopher S, Deng, James Z, Kane, Stefanie A, Koblan, Kenneth S, Salvatore, Christopher A, Mosser, Scott D, Johnston, Victor K, Wong, Bradley K, Miller-Stein, Cynthia M, Hershey, James C, Graham, Samuel L, Vacca, Joseph P, Williams, Theresa M
Published in Journal of medicinal chemistry (15.11.2007)
Published in Journal of medicinal chemistry (15.11.2007)
Get full text
Journal Article
Integrase Inhibitors and Cellular Immunity Suppress Retroviral Replication in Rhesus Macaques
Hazuda, Daria J., Young, Steven D., Guare, James P., Anthony, Neville J., Gomez, Robert P., Wai, John S., Vacca, Joseph P., Handt, Larry, Motzel, Sherri L., Klein, Hilton J., Dornadula, Geethanjali, Danovich, Robert M., Witmer, Marc V., Keith A. A. Wilson, Tussey, Lynda, Schleif, William A., Gabryelski, Lori S., Jin, Lixia, Miller, Michael D., Casimiro, Danilo R., Emini, Emilio A., Shiver, John W.
Published in Science (American Association for the Advancement of Science) (23.07.2004)
Published in Science (American Association for the Advancement of Science) (23.07.2004)
Get full text
Journal Article
Design and Synthesis of 8-Hydroxy-[1,6]Naphthyridines as Novel Inhibitors of HIV-1 Integrase in Vitro and in Infected Cells
Zhuang, Linghang, Wai, John S, Embrey, Mark W, Fisher, Thorsten E, Egbertson, Melissa S, Payne, Linda S, Guare, James P, Vacca, Joseph P, Hazuda, Daria J, Felock, Peter J, Wolfe, Abigail L, Stillmock, Kara A, Witmer, Marc V, Moyer, Gregory, Schleif, William A, Gabryelski, Lori J, Leonard, Yvonne M, Lynch, Joseph J, Michelson, Stuart R, Young, Steven D
Published in Journal of medicinal chemistry (13.02.2003)
Published in Journal of medicinal chemistry (13.02.2003)
Get full text
Journal Article
Raltegravir: the first HIV-1 integrase strand transfer inhibitor in the HIV armamentarium
Nguyen, Bach-Yen T., Isaacs, Robin D., Teppler, Hedy, Leavitt, Randi Y., Sklar, Peter, Iwamoto, Marian, Wenning, Larissa A., Miller, Michael D., Chen, Joshua, Kemp, Ramon, Xu, Wei, Fromtling, Robert A., Vacca, Joseph P., Young, Steven D., Rowley, Michael, Lower, Michael W., Gottesdiener, Keith M., Hazuda, Daria J.
Published in Annals of the New York Academy of Sciences (01.03.2011)
Published in Annals of the New York Academy of Sciences (01.03.2011)
Get full text
Journal Article
New advances in the discovery of thrombin and factor Xa inhibitors
Get full text
Book Review
Journal Article
Bismacrocyclic Inhibitors of Hepatitis C NS3/4a Protease
McCauley, John A, Rudd, Michael T, Nguyen, Kevin T, McIntyre, Charles J, Romano, Joseph J, Bush, Kimberly J, Varga, Sandor L, Ross, Charles W. III, Carroll, Steven S, DiMuzio, Jillian, Stahlhut, Mark W, Olsen, David B, Lyle, Terry A, Vacca, Joseph P, Liverton, Nigel J
Published in Angewandte Chemie (International ed.) (01.01.2008)
Published in Angewandte Chemie (International ed.) (01.01.2008)
Get full text
Journal Article
Discovery and Evaluation of Potent P1 Aryl Heterocycle-Based Thrombin Inhibitors
Young, Mary Beth, Barrow, James C, Glass, Kristen L, Lundell, George F, Newton, Christina L, Pellicore, Janetta M, Rittle, Kenneth E, Selnick, Harold G, Stauffer, Kenneth J, Vacca, Joseph P, Williams, Peter D, Bohn, Dennis, Clayton, Franklin C, Cook, Jacquelynn J, Krueger, Julie A, Kuo, Lawrence C, Lewis, S. Dale, Lucas, Bobby J, McMasters, Daniel R, Miller-Stein, Cynthia, Pietrak, Beth L, Wallace, Audrey A, White, Rebecca B, Wong, Bradley, Yan, Youwei, Nantermet, Philippe G
Published in Journal of medicinal chemistry (03.06.2004)
Published in Journal of medicinal chemistry (03.06.2004)
Get full text
Journal Article
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors
Lindsley, Stacey R., Moore, Keith P., Rajapakse, Hemaka A., Selnick, Harold G., Young, Mary Beth, Zhu, Hong, Munshi, Sanjeev, Kuo, Lawrence, McGaughey, Georgia B., Colussi, Dennis, Crouthamel, Ming-Chih, Lai, Ming-Tain, Pietrak, Beth, Price, Eric A., Sankaranarayanan, Sethu, Simon, Adam J., Seabrook, Guy R., Hazuda, Daria J., Pudvah, Nicole T., Hochman, Jerome H., Graham, Samuel L., Vacca, Joseph P., Nantermet, Philippe G.
Published in Bioorganic & medicinal chemistry letters (15.07.2007)
Published in Bioorganic & medicinal chemistry letters (15.07.2007)
Get full text
Journal Article
Discovery of MK-8742: An HCV NS5A Inhibitor with Broad Genotype Activity
Coburn, Craig A., Meinke, Peter T., Chang, Wei, Fandozzi, Christine M., Graham, Donald J., Hu, Bin, Huang, Qian, Kargman, Stacia, Kozlowski, Joseph, Liu, Rong, McCauley, John A., Nomeir, Amin A., Soll, Richard M., Vacca, Joseph P., Wang, Dahai, Wu, Hao, Zhong, Bin, Olsen, David B., Ludmerer, Steven W.
Published in ChemMedChem (01.12.2013)
Published in ChemMedChem (01.12.2013)
Get full text
Journal Article
Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors
Zhu, Hong, Young, Mary B., Nantermet, Philippe G., Graham, Samuel L., Colussi, Dennis, Lai, Ming-Tain, Pietrak, Beth, Price, Eric A., Sankaranarayanan, Sethu, Shi, Xiao-ping, Tugusheva, Katherine, Holahan, Marie A., Michener, Maria S., Cook, Jacquelynn J., Simon, Adam, Hazuda, Daria J., Vacca, Joseph P., Rajapakse, Hemaka A.
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Get full text
Journal Article
Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers
Freeman, David B., Hopkins, Tamara D., Mikochik, Peter J., Vacca, Joseph P., Gao, Hua, Naylor-Olsen, Adel, Rudra, Sonali, Li, Huixu, Pop, Marius S., Villagomez, Rosa A., Lee, Christina, Li, Heng, Zhou, Minyun, Saffran, Douglas C., Rioux, Nathalie, Hood, Tressa R., Day, Melinda A. L., McKeown, Michael R., Lin, Charles Y., Bischofberger, Norbert, Trotter, B. Wesley
Published in Journal of medicinal chemistry (14.12.2023)
Published in Journal of medicinal chemistry (14.12.2023)
Get full text
Journal Article
Design and Synthesis of 2,3,5-Substituted Imidazolidin-4-one Inhibitors of BACE-1
Barrow, James C., Rittle, Kenneth E., Ngo, Phung L., Selnick, Harold G., Graham, Samuel L., Pitzenberger, Steven M., McGaughey, Georgia B., Colussi, Dennis, Lai, Ming-Tain, Huang, Qian, Tugusheva, Katherine, Espeseth, Amy S., Simon, Adam J., Munshi, Sanjeev K., Vacca, Joseph P.
Published in ChemMedChem (09.07.2007)
Published in ChemMedChem (09.07.2007)
Get full text
Journal Article
A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells
Embrey, Mark W., Wai, John S., Funk, Timothy W., Homnick, Carl F., Perlow, Debbie S., Young, Steven D., Vacca, Joseph P., Hazuda, Daria J., Felock, Peter J., Stillmock, Kara A., Witmer, Marc V., Moyer, Gregory, Schleif, William A., Gabryelski, Lori J., Jin, Lixia, Chen, I-Wu, Ellis, Joan D., Wong, Bradley K., Lin, Jiunn H., Leonard, Yvonne M., Tsou, Nancy N., Zhuang, Linghang
Published in Bioorganic & medicinal chemistry letters (15.10.2005)
Published in Bioorganic & medicinal chemistry letters (15.10.2005)
Get full text
Journal Article
Biochemical and cell-based assays for characterization of BACE-1 inhibitors
Pietrak, Beth L., Crouthamel, Ming-Chih, Tugusheva, Katherine, Lineberger, Janet E., Xu, Min, DiMuzio, Jillian M., Steele, Thomas, Espeseth, Amy S., Stachel, Shawn J., Coburn, Craig A., Graham, Samuel L., Vacca, Joseph P., Shi, Xiao-Ping, Simon, Adam J., Hazuda, Daria J., Lai, Ming-Tain
Published in Analytical biochemistry (01.07.2005)
Published in Analytical biochemistry (01.07.2005)
Get full text
Journal Article