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Page 1
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: lewis sd. J Med Chem. 2003 Feb 13;46(4):461-73. doi: 10.1021/jm020311f. J Med Chem. 2003. PMID: 12570369
Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides.
Burgey CS, Robinson KA, Lyle TA, Nantermet PG, Selnick HG, Isaacs RC, Lewis SD, Lucas BJ, Krueger JA, Singh R, Miller-Stein C, White RB, Wong B, Lyle EA, Stranieri MT, Cook JJ, McMasters DR, Pellicore JM, Pal S, Wallace AA, Clayton FC, Bohn D, Welsh DC, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP. Burgey CS, et al. Among authors: lewis sd. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1353-7. doi: 10.1016/s0960-894x(03)00099-4. Bioorg Med Chem Lett. 2003. PMID: 12657281
3-amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors.
Sanderson PE, Cutrona KJ, Savage KL, Naylor-Olsen AM, Bickel DJ, Bohn DL, Clayton FC, Krueger JA, Lewis SD, Lucas BJ, Lyle EA, Wallace AA, Welsh DC, Yan Y. Sanderson PE, et al. Among authors: lewis sd. Bioorg Med Chem Lett. 2003 Apr 17;13(8):1441-4. doi: 10.1016/s0960-894x(03)00154-9. Bioorg Med Chem Lett. 2003. PMID: 12668008
Design and synthesis of potent and selective macrocyclic thrombin inhibitors.
Nantermet PG, Barrow JC, Newton CL, Pellicore JM, Young M, Lewis SD, Lucas BJ, Krueger JA, McMasters DR, Yan Y, Kuo LC, Vacca JP, Selnick HG. Nantermet PG, et al. Among authors: lewis sd. Bioorg Med Chem Lett. 2003 Aug 18;13(16):2781-4. doi: 10.1016/s0960-894x(03)00506-7. Bioorg Med Chem Lett. 2003. PMID: 12873514
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: lewis sd. 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: lewis sd. 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
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: lewis sd. J Med Chem. 2005 Apr 7;48(7):2282-93. doi: 10.1021/jm049423s. J Med Chem. 2005. PMID: 15801822
97 results