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895 results

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Page 1
Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of betaII tryptase.
Levell J, Astles P, Eastwood P, Cairns J, Houille O, Aldous S, Merriman G, Whiteley B, Pribish J, Czekaj M, Liang G, Maignan S, Guilloteau JP, Dupuy A, Davidson J, Harrison T, Morley A, Watson S, Fenton G, McCarthy C, Romano J, Mathew R, Engers D, Gardyan M, Sides K, Kwong J, Tsay J, Rebello S, Shen L, Wang J, Luo Y, Giardino O, Lim HK, Smith K, Pauls H. Levell J, et al. Among authors: romano j. Bioorg Med Chem. 2005 Apr 15;13(8):2859-72. doi: 10.1016/j.bmc.2005.02.014. Bioorg Med Chem. 2005. PMID: 15781396
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: romano jj. 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: romano jj. 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
Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists.
McIntyre CJ, McCauley JA, Bednar B, Bednar RA, Butcher JW, Claremon DA, Cunningham ME, Freidinger RM, Gaul SL, Homnick CF, Koblan KS, Mosser SD, Romano JJ, Liverton NJ. McIntyre CJ, et al. Among authors: romano jj. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5132-5. doi: 10.1016/j.bmcl.2009.07.028. Epub 2009 Jul 10. Bioorg Med Chem Lett. 2009. PMID: 19648007
NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
McCauley JA, Theberge CR, Romano JJ, Billings SB, Anderson KD, Claremon DA, Freidinger RM, Bednar RA, Mosser SD, Gaul SL, Connolly TM, Condra CL, Xia M, Cunningham ME, Bednar B, Stump GL, Lynch JJ, Macaulay A, Wafford KA, Koblan KS, Liverton NJ. McCauley JA, et al. Among authors: romano jj. J Med Chem. 2004 Apr 8;47(8):2089-96. doi: 10.1021/jm030483s. J Med Chem. 2004. PMID: 15056006
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: romano jj. 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
Molecular modeling based approach to potent P2-P4 macrocyclic inhibitors of hepatitis C NS3/4A protease.
Liverton NJ, Holloway MK, McCauley JA, Rudd MT, Butcher JW, Carroll SS, DiMuzio J, Fandozzi C, Gilbert KF, Mao SS, McIntyre CJ, Nguyen KT, Romano JJ, Stahlhut M, Wan BL, Olsen DB, Vacca JP. Liverton NJ, et al. Among authors: romano jj. J Am Chem Soc. 2008 Apr 9;130(14):4607-9. doi: 10.1021/ja711120r. Epub 2008 Mar 14. J Am Chem Soc. 2008. PMID: 18338894
Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases.
Haile PA, Casillas LN, Votta BJ, Wang GZ, Charnley AK, Dong X, Bury MJ, Romano JJ, Mehlmann JF, King BW, Erhard KF, Hanning CR, Lipshutz DB, Desai BM, Capriotti CA, Schaeffer MC, Berger SB, Mahajan MK, Reilly MA, Nagilla R, Rivera EJ, Sun HH, Kenna JK, Beal AM, Ouellette MT, Kelly M, Stemp G, Convery MA, Vossenkämper A, MacDonald TT, Gough PJ, Bertin J, Marquis RW. Haile PA, et al. Among authors: romano jj. J Med Chem. 2019 Jul 25;62(14):6482-6494. doi: 10.1021/acs.jmedchem.9b00575. Epub 2019 Jul 2. J Med Chem. 2019. PMID: 31265286
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: romano jj. 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.
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: romano jj. 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.
895 results