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Discovery of MK-1220: A Macrocyclic Inhibitor of Hepatitis C Virus NS3/4A Protease with Improved Preclinical Plasma Exposure.
Rudd MT, McCauley JA, Butcher JW, Romano JJ, McIntyre CJ, Nguyen KT, Gilbert KF, Bush KJ, Holloway MK, Swestock J, Wan BL, Carroll SS, DiMuzio JM, Graham DJ, Ludmerer SW, Stahlhut MW, Fandozzi CM, Trainor N, Olsen DB, Vacca JP, Liverton NJ. Rudd MT, et al. Among authors: ludmerer sw. ACS Med Chem Lett. 2011 Jan 12;2(3):207-12. doi: 10.1021/ml1002426. eCollection 2011 Mar 10. ACS Med Chem Lett. 2011. PMID: 24900304 Free PMC article.
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
Liverton NJ, Carroll SS, Dimuzio J, Fandozzi C, Graham DJ, Hazuda D, Holloway MK, Ludmerer SW, McCauley JA, McIntyre CJ, Olsen DB, Rudd MT, Stahlhut M, Vacca JP. Liverton NJ, et al. Among authors: ludmerer sw. Antimicrob Agents Chemother. 2010 Jan;54(1):305-11. doi: 10.1128/AAC.00677-09. Epub 2009 Oct 19. Antimicrob Agents Chemother. 2010. PMID: 19841155 Free PMC article.
Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
McCauley JA, McIntyre CJ, Rudd MT, Nguyen KT, Romano JJ, Butcher JW, Gilbert KF, Bush KJ, Holloway MK, Swestock J, Wan BL, Carroll SS, DiMuzio JM, Graham DJ, Ludmerer SW, Mao SS, Stahlhut MW, Fandozzi CM, Trainor N, Olsen DB, Vacca JP, Liverton NJ. McCauley JA, et al. Among authors: ludmerer sw. J Med Chem. 2010 Mar 25;53(6):2443-63. doi: 10.1021/jm9015526. J Med Chem. 2010. PMID: 20163176
Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease.
Rudd MT, McCauley JA, Romano JJ, Butcher JW, Bush K, McIntyre CJ, Nguyen KT, Gilbert KF, Lyle TA, Holloway MK, Wan BL, Vacca JP, Summa V, Harper S, Rowley M, Carroll SS, Burlein C, DiMuzio JM, Gates A, Graham DJ, Huang Q, Ludmerer SW, McClain S, McHale C, Stahlhut M, Fandozzi C, Taylor A, Trainor N, Olsen DB, Liverton NJ. Rudd MT, et al. Among authors: ludmerer sw. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7201-6. doi: 10.1016/j.bmcl.2012.08.106. Epub 2012 Sep 7. Bioorg Med Chem Lett. 2012. PMID: 23021993
Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers.
Rudd MT, McIntyre CJ, Romano JJ, Butcher JW, Holloway MK, Bush K, Nguyen KT, Gilbert KF, Lyle TA, Liverton NJ, Wan BL, Summa V, Harper S, Rowley M, Vacca JP, Carroll SS, Burlein C, DiMuzio JM, Gates A, Graham DJ, Huang Q, Ludmerer SW, McClain S, McHale C, Stahlhut M, Fandozzi C, Taylor A, Trainor N, Olsen DB, McCauley JA. Rudd MT, et al. Among authors: ludmerer sw. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7207-13. doi: 10.1016/j.bmcl.2012.09.061. Epub 2012 Oct 2. Bioorg Med Chem Lett. 2012. PMID: 23084906
Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.
Harper S, McCauley JA, Rudd MT, Ferrara M, DiFilippo M, Crescenzi B, Koch U, Petrocchi A, Holloway MK, Butcher JW, Romano JJ, Bush KJ, Gilbert KF, McIntyre CJ, Nguyen KT, Nizi E, Carroll SS, Ludmerer SW, Burlein C, DiMuzio JM, Graham DJ, McHale CM, Stahlhut MW, Olsen DB, Monteagudo E, Cianetti S, Giuliano C, Pucci V, Trainor N, Fandozzi CM, Rowley M, Coleman PJ, Vacca JP, Summa V, Liverton NJ. Harper S, et al. Among authors: ludmerer sw. ACS Med Chem Lett. 2012 Mar 2;3(4):332-6. doi: 10.1021/ml300017p. eCollection 2012 Apr 12. ACS Med Chem Lett. 2012. PMID: 24900473 Free PMC article.
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.
Rudd MT, Butcher JW, Nguyen KT, McIntyre CJ, Romano JJ, Gilbert KF, Bush KJ, Liverton NJ, Holloway MK, Harper S, Ferrara M, DiFilippo M, Summa V, Swestock J, Fritzen J, Carroll SS, Burlein C, DiMuzio JM, Gates A, Graham DJ, Huang Q, McClain S, McHale C, Stahlhut MW, Black S, Chase R, Soriano A, Fandozzi CM, Taylor A, Trainor N, Olsen DB, Coleman PJ, Ludmerer SW, McCauley JA. Rudd MT, et al. Among authors: ludmerer sw. ChemMedChem. 2015 Apr;10(4):727-35. doi: 10.1002/cmdc.201402558. Epub 2015 Mar 10. ChemMedChem. 2015. PMID: 25759009
44 results