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Discovery and preclinical characterization of the cyclopropylindolobenzazepine BMS-791325, a potent allosteric inhibitor of the hepatitis C virus NS5B polymerase.
Gentles RG, Ding M, Bender JA, Bergstrom CP, Grant-Young K, Hewawasam P, Hudyma T, Martin S, Nickel A, Regueiro-Ren A, Tu Y, Yang Z, Yeung KS, Zheng X, Chao S, Sun JH, Beno BR, Camac DM, Chang CH, Gao M, Morin PE, Sheriff S, Tredup J, Wan J, Witmer MR, Xie D, Hanumegowda U, Knipe J, Mosure K, Santone KS, Parker DD, Zhuo X, Lemm J, Liu M, Pelosi L, Rigat K, Voss S, Wang Y, Wang YK, Colonno RJ, Gao M, Roberts SB, Gao Q, Ng A, Meanwell NA, Kadow JF. Gentles RG, et al. J Med Chem. 2014 Mar 13;57(5):1855-79. doi: 10.1021/jm4016894. Epub 2014 Jan 7. J Med Chem. 2014. PMID: 24397558
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. 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. 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.
Potent Inhibitors of Hepatitis C Virus NS3 Protease: Employment of a Difluoromethyl Group as a Hydrogen-Bond Donor.
Zheng B, D'Andrea SV, Sun LQ, Wang AX, Chen Y, Hrnciar P, Friborg J, Falk P, Hernandez D, Yu F, Sheaffer AK, Knipe JO, Mosure K, Rajamani R, Good AC, Kish K, Tredup J, Klei HE, Paruchuri M, Ng A, Gao Q, Rampulla RA, Mathur A, Meanwell NA, McPhee F, Scola PM. Zheng B, et al. ACS Med Chem Lett. 2018 Jan 19;9(2):143-148. doi: 10.1021/acsmedchemlett.7b00503. eCollection 2018 Feb 8. ACS Med Chem Lett. 2018. PMID: 29456803 Free PMC article.
Discovery of non-zwitterionic aryl sulfonamides as Nav1.7 inhibitors with efficacy in preclinical behavioral models and translational measures of nociceptive neuron activation.
Wu YJ, Guernon J, McClure A, Luo G, Rajamani R, Ng A, Easton A, Newton A, Bourin C, Parker D, Mosure K, Barnaby O, Soars MG, Knox RJ, Matchett M, Pieschl R, Herrington J, Chen P, Sivarao DV, Bristow LJ, Meanwell NA, Bronson J, Olson R, Thompson LA, Dzierba C. Wu YJ, et al. Bioorg Med Chem. 2017 Oct 15;25(20):5490-5505. doi: 10.1016/j.bmc.2017.08.012. Epub 2017 Aug 9. Bioorg Med Chem. 2017. PMID: 28818462
Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition.
Swidorski JJ, Jenkins S, Hanumegowda U, Parker DD, Beno BR, Protack T, Ng A, Gupta A, Shanmugam Y, Dicker IB, Krystal M, Meanwell NA, Regueiro-Ren A. Swidorski JJ, et al. Bioorg Med Chem Lett. 2021 Mar 15;36:127823. doi: 10.1016/j.bmcl.2021.127823. Epub 2021 Jan 26. Bioorg Med Chem Lett. 2021. PMID: 33508465
Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aβ Reduction in Rodents.
Wu YJ, Guernon J, Yang F, Snyder L, Shi J, Mcclure A, Rajamani R, Park H, Ng A, Lewis H, Chang C, Camac D, Toyn JH, Ahlijanian MK, Albright CF, Macor JE, Thompson LA. Wu YJ, et al. ACS Med Chem Lett. 2016 Jan 11;7(3):271-6. doi: 10.1021/acsmedchemlett.5b00432. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985314 Free PMC article.
82 results