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Page 1
Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).
Pinto DJP, Orwat MJ, Smith LM 2nd, Quan ML, Lam PYS, Rossi KA, Apedo A, Bozarth JM, Wu Y, Zheng JJ, Xin B, Toussaint N, Stetsko P, Gudmundsson O, Maxwell B, Crain EJ, Wong PC, Lou Z, Harper TW, Chacko SA, Myers JE Jr, Sheriff S, Zhang H, Hou X, Mathur A, Seiffert DA, Wexler RR, Luettgen JM, Ewing WR. Pinto DJP, et al. Among authors: ewing wr. J Med Chem. 2017 Dec 14;60(23):9703-9723. doi: 10.1021/acs.jmedchem.7b01171. Epub 2017 Nov 17. J Med Chem. 2017. PMID: 29077405
Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.
Ewing WR, Becker MR, Manetta VE, Davis RS, Pauls HW, Mason H, Choi-Sledeski YM, Green D, Cha D, Spada AP, Cheney DL, Mason JS, Maignan S, Guilloteau JP, Brown K, Colussi D, Bentley R, Bostwick J, Kasiewski CJ, Morgan SR, Leadley RJ, Dunwiddie CT, Perrone MH, Chu V. Ewing WR, et al. J Med Chem. 1999 Sep 9;42(18):3557-71. doi: 10.1021/jm990040h. J Med Chem. 1999. PMID: 10479288
Discovery of a potent and novel motilin agonist.
Li JJ, Chao HG, Wang H, Tino JA, Lawrence RM, Ewing WR, Ma Z, Yan M, Slusarchyk D, Seethala R, Sun H, Li D, Burford NT, Stoffel RH, Salyan ME, Li CY, Witkus M, Zhao N, Rich A, Gordon DA. Li JJ, et al. Among authors: ewing wr. J Med Chem. 2004 Mar 25;47(7):1704-8. doi: 10.1021/jm0304865. J Med Chem. 2004. PMID: 15027861
Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics.
Murugesan N, Gu Z, Fadnis L, Tellew JE, Baska RA, Yang Y, Beyer SM, Monshizadegan H, Dickinson KE, Valentine MT, Humphreys WG, Lan SJ, Ewing WR, Carlson KE, Kowala MC, Zahler R, Macor JE. Murugesan N, et al. Among authors: ewing wr. J Med Chem. 2005 Jan 13;48(1):171-9. doi: 10.1021/jm049548x. J Med Chem. 2005. PMID: 15634011
Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).
Sulsky R, Magnin DR, Huang Y, Simpkins L, Taunk P, Patel M, Zhu Y, Stouch TR, Bassolino-Klimas D, Parker R, Harrity T, Stoffel R, Taylor DS, Lavoie TB, Kish K, Jacobson BL, Sheriff S, Adam LP, Ewing WR, Robl JA. Sulsky R, et al. Among authors: ewing wr. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3511-5. doi: 10.1016/j.bmcl.2006.12.044. Epub 2006 Dec 21. Bioorg Med Chem Lett. 2007. PMID: 17502136
Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180).
Li J, Chen SY, Li JJ, Wang H, Hernandez AS, Tao S, Musial CM, Qu F, Swartz S, Chao ST, Flynn N, Murphy BJ, Slusarchyk DA, Seethala R, Yan M, Sleph P, Grover G, Smith MA, Beehler B, Giupponi L, Dickinson KE, Zhang H, Humphreys WG, Patel BP, Schwinden M, Stouch T, Cheng PT, Biller SA, Ewing WR, Gordon D, Robl JA, Tino JA. Li J, et al. Among authors: ewing wr. J Med Chem. 2007 Nov 29;50(24):5890-3. doi: 10.1021/jm7010595. Epub 2007 Oct 31. J Med Chem. 2007. PMID: 17973363
Eleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity.
Mapelli C, Natarajan SI, Meyer JP, Bastos MM, Bernatowicz MS, Lee VG, Pluscec J, Riexinger DJ, Sieber-McMaster ES, Constantine KL, Smith-Monroy CA, Golla R, Ma Z, Longhi DA, Shi D, Xin L, Taylor JR, Koplowitz B, Chi CL, Khanna A, Robinson GW, Seethala R, Antal-Zimanyi IA, Stoffel RH, Han S, Whaley JM, Huang CS, Krupinski J, Ewing WR. Mapelli C, et al. Among authors: ewing wr. J Med Chem. 2009 Dec 10;52(23):7788-99. doi: 10.1021/jm900752a. J Med Chem. 2009. PMID: 19702274
Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties.
Ellsworth BA, Sher PM, Wu X, Wu G, Sulsky RB, Gu Z, Murugesan N, Zhu Y, Yu G, Sitkoff DF, Carlson KE, Kang L, Yang Y, Lee N, Baska RA, Keim WJ, Cullen MJ, Azzara AV, Zuvich E, Thomas MA, Rohrbach KW, Devenny JJ, Godonis HE, Harvey SJ, Murphy BJ, Everlof GG, Stetsko PI, Gudmundsson O, Johnghar S, Ranasinghe A, Behnia K, Pelleymounter MA, Ewing WR. Ellsworth BA, et al. Among authors: ewing wr. J Med Chem. 2013 Dec 12;56(23):9586-600. doi: 10.1021/jm4010835. Epub 2013 Nov 20. J Med Chem. 2013. PMID: 24182233
60 results