Search Results - "Butcher, John W"

Discovery of Vaniprevir (MK-7009), a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor by 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

“…A new class of HCV NS3/4a protease inhibitors which contain a P2 to P4 macrocyclic constraint was designed using a molecular-modeling derived strategy…”
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Molecular Modeling Based Approach to Potent P2−P4 Macrocyclic Inhibitors of Hepatitis C NS3/4A Protease by 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

“…Molecular modeling of inhibitor bound full length HCV NS3/4A protease structures proved to be a valuable tool in the design of a new series of potent NS3…”
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Overcoming Mutagenicity and Ion Channel Activity: Optimization of Selective Spleen Tyrosine Kinase Inhibitors by Ellis, J. Michael, Altman, Michael D, Bass, Alan, Butcher, John W, Byford, Alan J, Donofrio, Anthony, Galloway, Sheila, Haidle, Andrew M, Jewell, James, Kelly, Nancy, Leccese, Erica K, Lee, Sandra, Maddess, Matthew, Miller, J. Richard, Moy, Lily Y, Osimboni, Ekundayo, Otte, Ryan D, Reddy, M. Vijay, Spencer, Kerrie, Sun, Binyuan, Vincent, Stella H, Ward, Gwendolyn J, Woo, Grace H. C, Yang, Chiming, Houshyar, Hani, Northrup, Alan B

“…Development of a series of highly kinome-selective spleen tyrosine kinase (Syk) inhibitors with favorable druglike properties is described. Early leads were…”
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Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma by Huang, Xianhai, Brubaker, Jason, Zhou, Wei, Biju, Purakkattle J., Xiao, Li, Shao, Ning, Huang, Ying, Dong, Li, Liu, Zhidan, Bitar, Rema, Buevich, Alexei, Jung, Joon, Peterson, Scott L., Butcher, John W., Close, Joshua, Martinez, Michelle, MacCoss, Rachel N., Zhang, Hongjun, Crawford, Scott, McCormick, Kevin D., Aslanian, Robert, Nargund, Ravi, Correll, Craig, Gervais, Francois, Qiu, Hongchen, Yang, Xiaoxin, Garlisi, Charles, Rindgen, Diane, Maloney, Kevin M., Siliphaivanh, Phieng, Palani, Anandan

“…A novel series of tricyclic tetrahydroquinolines were identified as potent and selective CRTh2 receptor antagonists. The agonism and antagonism switch was…”
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P2-Quinazolinones and Bis-Macrocycles as New Templates for Next-Generation Hepatitis C Virus NS3/4a Protease Inhibitors: Discovery of MK-2748 and MK-6325 by Rudd, Michael T., Butcher, John W., Nguyen, Kevin T., McIntyre, Charles J., Romano, Joseph J., Gilbert, Kevin F., Bush, Kimberly J., Liverton, Nigel J., Holloway, M. Katharine, Harper, Steven, Ferrara, Marco, DiFilippo, Marcello, Summa, Vincenzo, Swestock, John, Fritzen, Jeff, Carroll, Steven S., Burlein, Christine, DiMuzio, Jillian M., Gates, Adam, Graham, Donald J., Huang, Qian, McClain, Stephanie, McHale, Carolyn, Stahlhut, Mark W., Black, Stuart, Chase, Robert, Soriano, Aileen, Fandozzi, Christine M., Taylor, Anne, Trainor, Nicole, Olsen, David B., Coleman, Paul J., Ludmerer, Steven W., McCauley, John A.

“…With the goal of identifying inhibitors of hepatitis C virus (HCV) NS3/4a protease that are potent against a wide range of genotypes and clinically relevant…”
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Identification and Characterization of 4-Methylbenzyl 4-[(Pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an Orally Bioavailable, Brain Penetrant NR2B Selective N-Methyl-d-Aspartate Receptor Antagonist by Liverton, Nigel J, Bednar, Rodney A, Bednar, Bohumil, Butcher, John W, Claiborne, Christopher F, Claremon, David A, Cunningham, Michael, DiLella, Anthony G, Gaul, Stanley L, Libby, Brian E, Lyle, Elizabeth A, Lynch, Joseph J, McCauley, John A, Mosser, Scott D, Nguyen, Kevin T, Stump, Gary L, Sun, Hong, Wang, Hao, Yergey, James, Koblan, Kenneth S

“…The discovery of a novel series of NR2B subtype selective N-methyl-d-aspartate (NMDA) antagonists is reported. Initial optimization of a high-throughput…”
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Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2–P4 linkers by Rudd, Michael T., McIntyre, Charles J., Romano, Joseph J., Butcher, John W., Holloway, M. Katharine, Bush, Kimberly, Nguyen, Kevin T., Gilbert, Kevin F., Lyle, Terry A., Liverton, Nigel J., Wan, Bang-Lin, Summa, Vincenzo, Harper, Steven, Rowley, Michael, Vacca, Joseph P., Carroll, Steven S., Burlein, Christine, DiMuzio, Jillian M., Gates, Adam, Graham, Donald J., Huang, Qian, Ludmerer, Steven W., McClain, Stephanie, McHale, Carolyn, Stahlhut, Mark, Fandozzi, Christine, Taylor, Anne, Trainor, Nicole, Olsen, David B., McCauley, John A.

“…A series of macrocyclic compounds containing a cyclic constraint in the P2–P4 linker region have been discovered and shown to exhibit excellent HCV NS3/4a…”
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Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease by Rudd, Michael T., McCauley, John A., Romano, Joseph J., Butcher, John W., Bush, Kimberly, McIntyre, Charles J., Nguyen, Kevin T., Gilbert, Kevin F., Lyle, Terry A., Holloway, M. Katharine, Wan, Bang-Lin, Vacca, Joseph P., Summa, Vincenzo, Harper, Steven, Rowley, Michael, Carroll, Steven S., Burlein, Christine, DiMuzio, Jillian M., Gates, Adam, Graham, Donald J., Huang, Qian, Ludmerer, Steven W., McClain, Stephanie, McHale, Carolyn, Stahlhut, Mark, Fandozzi, Christine, Taylor, Anne, Trainor, Nicole, Olsen, David B., Liverton, Nigel J.

“…A series of macrocyclic compounds containing 2-substituted-quinoline moieties have been discovered and shown to exhibit excellent HCV NS3/4a genotype 3a and…”
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Discovery of MK-1220: A Macrocyclic Inhibitor of Hepatitis C Virus NS3/4A Protease with Improved Preclinical Plasma Exposure by Rudd, Michael T, McCauley, John A, Butcher, John W, Romano, Joseph J, McIntyre, Charles J, Nguyen, Kevin T, 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, Stahlhut, Mark W, Fandozzi, Christine M, Trainor, Nicole, Olsen, David B, Vacca, Joseph P, Liverton, Nigel J

“…The discovery of MK-1220 is reported along with the development of a series of HCV NS3/4A protease inhibitors containing a P2 to P4 macrocyclic constraint with…”
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P2-Quinazolinones and Bis-Macrocycles as New Templates for Next-Generation HepatitisC Virus NS3/4a Protease Inhibitors: Discovery of MK-2748 and MK-6325 by Rudd, Michael T, Butcher, John W, Nguyen, Kevin T, McIntyre, Charles J, Romano, Joseph J, Gilbert, Kevin F, Bush, Kimberly J, Liverton, Nigel J, Holloway, M Katharine, Harper, Steven, Ferrara, Marco, DiFilippo, Marcello, Summa, Vincenzo, Swestock, John, Fritzen, Jeff, Carroll, Steven S, Burlein, Christine, DiMuzio, Jillian M, Gates, Adam, Graham, Donald J, Huang, Qian, McClain, Stephanie, McHale, Carolyn, Stahlhut, Mark W, Black, Stuart, Chase, Robert, Soriano, Aileen, Fandozzi, Christine M, Taylor, Anne, Trainor, Nicole, Olsen, David B, Coleman, Paul J, Ludmerer, Steven W, McCauley, John A

“…With the goal of identifying inhibitors of hepatitisC virus (HCV) NS3/4a protease that are potent against a wide range of genotypes and clinically relevant…”
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Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists by McIntyre, Charles J., McCauley, John A., Bednar, Bohumil, Bednar, Rodney A., Butcher, John W., Claremon, David A., Cunningham, Michael E., Freidinger, Roger M., Gaul, Stanley L., Homnick, Carl F., Koblan, Ken S., Mosser, Scott D., Romano, Joseph J., Liverton, Nigel J.

“…A novel series of annulated tricyclic compounds was synthesized and evaluated as NMDA/NR2B antagonists. Compound (−)23b was identified as one which showed good…”
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A new series of potent benzodiazepine γ-secretase inhibitors by Churcher, Ian, Ashton, Kate, Butcher, John W., Clarke, Earl E., Harrison, Timothy, Lewis, Huw D., Owens, Andrew P., Teall, Martin R., Williams, Susie, Wrigley, Jonathan D.J.

“…A new series of benzodiazepine-containing γ-secretase inhibitors with potential use in the treatment of Alzheimer's disease is disclosed. Structure–activity…”
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Synthesis of the first sulfur-35-labeled hERG radioligand by Raab, Conrad E., Butcher, John W., Connolly, Thomas M., Karczewski, Jerzy, Yu, Nathan X., Staskiewicz, Steven J., Liverton, Nigel, Dean, Dennis C., Melillo, David G.

“…The synthesis of hERG radioligand [35S]MK-0499 for use in an HTS assay for IKr activity is reported The synthesis of the first high specific activity…”
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Class III Antiarrhythmic Activity in Vivo by Selective Blockade of the Slowly Activating Cardiac Delayed Rectifier Potassium Current I Ks by (R)-2-(2,4- Trifluoromethyl)-N-[2-oxo-5-phenyl- 1-(2,2,2-trifluoroethyl)-2,3-dihydro- 1H-benzo[e][1,4]diazepin-3-yl]acetamide by Selnick, Harold G, Liverton, Nigel J, Baldwin, John J, Butcher, John W, Claremon, David A, Elliott, Jason M, Freidinger, Roger M, King, Stella A, Libby, Brian E, McIntyre, Charles J, Pribush, David A, Remy, David C, Smith, Garry R, Tebben, Andrew J, Jurkiewicz, Nancy K, Lynch, Joseph J, Salata, Joseph J, Sanguinetti, Michael C, Siegl, Peter K. S, Slaughter, Donald E, Vyas, Kamlesh

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A versatile synthesis of 1,1-dioxo 7-substituted cephems: preparation of the human leukocyte elastase (HLE) inhibitor 1,1-dioxo-trans-7-methoxycephalosporanic acid tert-butyl ester by Blacklock, Thomas J, Butcher, John W, Sohar, Paul, Lamanec, Theresa Rothauser, Grabowski, Edward J. J

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Novel 5-cyclopropyl-1,4-benzodiazepin-2-ones as potent and selective Iks-blocking class III antiarrhythmic agents by BUTCHER, John W, LIVERTON, Nigel J, VYAS, Kamlesh, CLAREMON, David A, FREIDINGER, Roger M, JURKIEWICZ, Nancy K, LYNCH, Joseph J, SALATA, Joseph J, JIXIN WANG, DIECKHAUS, Christine M, SLAUGHTER, Donald E

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Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor by 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

“…A new class of HCV NS3/4a protease inhibitors containing a P2 to P4 macrocyclic constraint was designed using a molecular modeling-derived strategy. Building…”
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Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters by Doherty, James B, Ashe, Bonnie M, Barker, Peter L, Blacklock, Thomas J, Butcher, John W, Chandler, Gilbert O, Dahlgren, M. Ellen, Davies, Philip, Dorn, Conrad P

“…Time-dependent inhibitors of the enzyme human leukocyte elastase have been developed based on the cephem nucleus. A series of cephalosporin tert-butyl esters…”
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4-Oxospiro[benzopyran-2,4'-piperidines] as class III antiarrhythmic agents. Pharmacological studies on 3,4-dihydro-1'-[2-(benzofurazan-5-yl)ethyl]-6-methanesulfonamidospiro[(2H)-1-benzopyran-2,4'-piperidin]-4-one (L-691,121) by Elliott, Jason M, Selnick, Harold G, Claremon, David A, Baldwin, John J, Buhrow, Susan A, Butcher, John W, Habecker, Charles N, King, Stella W, Lynch, Joseph J

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Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2aP4 linkers by Rudd, Michael T, McIntyre, Charles J, Romano, Joseph J, Butcher, John W, Holloway, MKatharine, Bush, Kimberly, Nguyen, Kevin T, Gilbert, Kevin F, Lyle, Terry A, Liverton, Nigel J, Wan, Bang-Lin, Summa, Vincenzo, Harper, Steven, Rowley, Michael, Vacca, Joseph P, Carroll, Steven S, Burlein, Christine, DiMuzio, Jillian M, Gates, Adam, Graham, Donald J, Huang, Qian, Ludmerer, Steven W, McClain, Stephanie, McHale, Carolyn, Stahlhut, Mark, Fandozzi, Christine, Taylor, Anne, Trainor, Nicole, Olsen, David B, McCauley, John A

“…A series of macrocyclic compounds containing a cyclic constraint in the P2aP4 linker region have been discovered and shown to exhibit excellent HCV NS3/4a…”
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