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327 results

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Page 1
9-hydroxyazafluorenes and their use in thrombin inhibitors.
Stauffer KJ, Williams PD, Selnick HG, Nantermet PG, Newton CL, Homnick CF, Zrada MM, Lewis SD, Lucas BJ, Krueger JA, Pietrak BL, Lyle EA, Singh R, Miller-Stein C, White RB, Wong B, Wallace AA, Sitko GR, Cook JJ, Holahan MA, Stranieri-Michener M, Leonard YM, Lynch JJ Jr, McMasters DR, Yan Y. Stauffer KJ, et al. Among authors: williams pd. J Med Chem. 2005 Apr 7;48(7):2282-93. doi: 10.1021/jm049423s. J Med Chem. 2005. PMID: 15801822
Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.
Burgey CS, Robinson KA, Lyle TA, Sanderson PE, Lewis SD, Lucas BJ, Krueger JA, Singh R, Miller-Stein C, White RB, Wong B, Lyle EA, Williams PD, Coburn CA, Dorsey BD, Barrow JC, Stranieri MT, Holahan MA, Sitko GR, Cook JJ, McMasters DR, McDonough CM, Sanders WM, Wallace AA, Clayton FC, Bohn D, Leonard YM, Detwiler TJ Jr, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP. Burgey CS, et al. Among authors: williams pd. J Med Chem. 2003 Feb 13;46(4):461-73. doi: 10.1021/jm020311f. J Med Chem. 2003. PMID: 12570369
Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors.
Young MB, Barrow JC, Glass KL, Lundell GF, Newton CL, Pellicore JM, Rittle KE, Selnick HG, Stauffer KJ, Vacca JP, Williams PD, Bohn D, Clayton FC, Cook JJ, Krueger JA, Kuo LC, Lewis SD, Lucas BJ, McMasters DR, Miller-Stein C, Pietrak BL, Wallace AA, White RB, Wong B, Yan Y, Nantermet PG. Young MB, et al. Among authors: williams pd. J Med Chem. 2004 Jun 3;47(12):2995-3008. doi: 10.1021/jm030303e. J Med Chem. 2004. PMID: 15163182
Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability.
Morrissette MM, Stauffer KJ, Williams PD, Lyle TA, Vacca JP, Krueger JA, Lewis SD, Lucas BJ, Wong BK, White RB, Miller-Stein C, Lyle EA, Wallace AA, Leonard YM, Welsh DC, Lynch JJ, McMasters DR. Morrissette MM, et al. Among authors: williams pd. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4161-4. doi: 10.1016/j.bmcl.2004.06.030. Bioorg Med Chem Lett. 2004. PMID: 15261262
Discovery of potent, selective 4-fluoroproline-based thrombin inhibitors with improved metabolic stability.
Staas DD, Savage KL, Sherman VL, Shimp HL, Lyle TA, Tran LO, Wiscount CM, McMasters DR, Sanderson PE, Williams PD, Lucas BJ Jr, Krueger JA, Lewis SD, White RB, Yu S, Wong BK, Kochansky CJ, Anari MR, Yan Y, Vacca JP. Staas DD, et al. Among authors: williams pd. Bioorg Med Chem. 2006 Oct 15;14(20):6900-16. doi: 10.1016/j.bmc.2006.06.040. Epub 2006 Jul 25. Bioorg Med Chem. 2006. PMID: 16870455
Design, synthesis and SAR of a series of 1,3,5-trisubstituted benzenes as thrombin inhibitors.
Isaacs RC, Newton CL, Cutrona KJ, Mercer SP, Payne LS, Stauffer KJ, Williams PD, Cook JJ, Krueger JA, Lewis SD, Lucas BJ, Lyle EA, Lynch JJ, McMasters DR, Naylor-Olsen AM, Michener MT, Wallace AA. Isaacs RC, et al. Among authors: williams pd. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1536-40. doi: 10.1016/j.bmcl.2010.12.105. Epub 2010 Dec 28. Bioorg Med Chem Lett. 2011. PMID: 21295467
Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors.
Coburn CA, Rush DM, Williams PD, Homnick C, Lyle EA, Lewis SD, Lucas BJ Jr, Di Muzio-Mower JM, Juliano M, Krueger JA, Vastag K, Chen IW, Vacca JP. Coburn CA, et al. Among authors: williams pd. Bioorg Med Chem Lett. 2000 May 15;10(10):1069-72. doi: 10.1016/s0960-894x(00)00170-0. Bioorg Med Chem Lett. 2000. PMID: 10843219
10-Hydroxy-7,8-dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-diones: potent, orally bioavailable HIV-1 integrase strand-transfer inhibitors with activity against integrase mutants.
Wiscount CM, Williams PD, Tran LO, Embrey MW, Fisher TE, Sherman V, Homnick CF, Donnette Staas D, Lyle TA, Wai JS, Vacca JP, Wang Z, Felock PJ, Stillmock KA, Witmer MV, Miller MD, Hazuda DJ, Day AM, Gabryelski LJ, Ecto LT, Schleif WA, DiStefano DJ, Kochansky CJ, Anari MR. Wiscount CM, et al. Among authors: williams pd. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4581-3. doi: 10.1016/j.bmcl.2008.07.037. Epub 2008 Jul 15. Bioorg Med Chem Lett. 2008. PMID: 18657970
327 results