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Page 1
The discovery of asunaprevir (BMS-650032), an orally efficacious NS3 protease inhibitor for the treatment of hepatitis C virus infection.
Scola PM, Sun LQ, Wang AX, Chen J, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea SV, Zheng B, Hewawasam P, Tu Y, Friborg J, Falk P, Hernandez D, Levine S, Chen C, Yu F, Sheaffer AK, Zhai G, Barry D, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Good AC, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Mueller L, Colonno RJ, Grasela DM, Adams SP, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Meanwell NA, McPhee F. Scola PM, et al. Among authors: grasela dm. J Med Chem. 2014 Mar 13;57(5):1730-52. doi: 10.1021/jm500297k. Epub 2014 Mar 5. J Med Chem. 2014. PMID: 24564672
Single- and multiple-ascending-dose studies of the NS3 protease inhibitor asunaprevir in subjects with or without chronic hepatitis C.
Pasquinelli C, McPhee F, Eley T, Villegas C, Sandy K, Sheridan P, Persson A, Huang SP, Hernandez D, Sheaffer AK, Scola P, Marbury T, Lawitz E, Goldwater R, Rodriguez-Torres M, Demicco M, Wright D, Charlton M, Kraft WK, Lopez-Talavera JC, Grasela DM. Pasquinelli C, et al. Among authors: grasela dm. Antimicrob Agents Chemother. 2012 Apr;56(4):1838-44. doi: 10.1128/AAC.05854-11. Epub 2012 Jan 30. Antimicrob Agents Chemother. 2012. PMID: 22290978 Free PMC article. Clinical Trial.
Discovery and early clinical evaluation of BMS-605339, a potent and orally efficacious tripeptidic acylsulfonamide NS3 protease inhibitor for the treatment of hepatitis C virus infection.
Scola PM, Wang AX, Good AC, Sun LQ, Combrink KD, Campbell JA, Chen J, Tu Y, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea S, Zheng B, Hewawasam P, Ding M, Thuring J, Li J, Hernandez D, Yu F, Falk P, Zhai G, Sheaffer AK, Chen C, Lee MS, Barry D, Knipe JO, Li W, Han YH, Jenkins S, Gesenberg C, Gao Q, Sinz MW, Santone KS, Zvyaga T, Rajamani R, Klei HE, Colonno RJ, Grasela DM, Hughes E, Chien C, Adams S, Levesque PC, Li D, Zhu J, Meanwell NA, McPhee F. Scola PM, et al. Among authors: grasela dm. J Med Chem. 2014 Mar 13;57(5):1708-29. doi: 10.1021/jm401840s. Epub 2014 Feb 20. J Med Chem. 2014. PMID: 24555570
Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing.
Sun LQ, Mull E, Zheng B, D'Andrea S, Zhao Q, Wang AX, Sin N, Venables BL, Sit SY, Chen Y, Chen J, Cocuzza A, Bilder DM, Mathur A, Rampulla R, Chen BC, Palani T, Ganesan S, Arunachalam PN, Falk P, Levine S, Chen C, Friborg J, Yu F, Hernandez D, Sheaffer AK, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Ng A, Mueller L, Grasela DM, Adams S, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Wang YK, Fang H, Cockett MI, Meanwell NA, McPhee F, Scola PM. Sun LQ, et al. Among authors: grasela dm. J Med Chem. 2016 Sep 8;59(17):8042-60. doi: 10.1021/acs.jmedchem.6b00821. Epub 2016 Aug 26. J Med Chem. 2016. PMID: 27564532
Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies.
Yeung KS, Beno BR, Parcella K, Bender JA, Grant-Young KA, Nickel A, Gunaga P, Anjanappa P, Bora RO, Selvakumar K, Rigat K, Wang YK, Liu M, Lemm J, Mosure K, Sheriff S, Wan C, Witmer M, Kish K, Hanumegowda U, Zhuo X, Shu YZ, Parker D, Haskell R, Ng A, Gao Q, Colston E, Raybon J, Grasela DM, Santone K, Gao M, Meanwell NA, Sinz M, Soars MG, Knipe JO, Roberts SB, Kadow JF. Yeung KS, et al. Among authors: grasela dm. J Med Chem. 2017 May 25;60(10):4369-4385. doi: 10.1021/acs.jmedchem.7b00328. Epub 2017 May 4. J Med Chem. 2017. PMID: 28430437 Clinical Trial.
Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)-2-oxoethanone (BMS-488043).
Kadow JF, Ueda Y, Meanwell NA, Connolly TP, Wang T, Chen CP, Yeung KS, Zhu J, Bender JA, Yang Z, Parker D, Lin PF, Colonno RJ, Mathew M, Morgan D, Zheng M, Chien C, Grasela D. Kadow JF, et al. J Med Chem. 2012 Mar 8;55(5):2048-56. doi: 10.1021/jm201218m. Epub 2012 Feb 22. J Med Chem. 2012. PMID: 22356441 Clinical Trial.
Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-585248).
Regueiro-Ren A, Xue QM, Swidorski JJ, Gong YF, Mathew M, Parker DD, Yang Z, Eggers B, D'Arienzo C, Sun Y, Malinowski J, Gao Q, Wu D, Langley DR, Colonno RJ, Chien C, Grasela DM, Zheng M, Lin PF, Meanwell NA, Kadow JF. Regueiro-Ren A, et al. Among authors: grasela dm. J Med Chem. 2013 Feb 28;56(4):1656-69. doi: 10.1021/jm3016377. Epub 2013 Feb 7. J Med Chem. 2013. PMID: 23360431
Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect.
Gao M, Nettles RE, Belema M, Snyder LB, Nguyen VN, Fridell RA, Serrano-Wu MH, Langley DR, Sun JH, O'Boyle DR 2nd, Lemm JA, Wang C, Knipe JO, Chien C, Colonno RJ, Grasela DM, Meanwell NA, Hamann LG. Gao M, et al. Among authors: grasela dm. Nature. 2010 May 6;465(7294):96-100. doi: 10.1038/nature08960. Epub 2010 Apr 21. Nature. 2010. PMID: 20410884 Free PMC article. Clinical Trial.
Randomized trial of daclatasvir and asunaprevir with or without PegIFN/RBV for hepatitis C virus genotype 1 null responders.
Lok AS, Gardiner DF, Hézode C, Lawitz EJ, Bourlière M, Everson GT, Marcellin P, Rodriguez-Torres M, Pol S, Serfaty L, Eley T, Huang SP, Li J, Wind-Rotolo M, Yu F, McPhee F, Grasela DM, Pasquinelli C. Lok AS, et al. Among authors: grasela dm. J Hepatol. 2014 Mar;60(3):490-9. doi: 10.1016/j.jhep.2013.10.019. Epub 2013 Oct 26. J Hepatol. 2014. PMID: 24444658 Clinical Trial.
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