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107 results

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Page 1
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: wong bk. 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
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. 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. 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
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. J Med Chem. 2004 Jun 3;47(12):2995-3008. doi: 10.1021/jm030303e. J Med Chem. 2004. PMID: 15163182
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. J Med Chem. 2005 Apr 7;48(7):2282-93. doi: 10.1021/jm049423s. J Med Chem. 2005. PMID: 15801822
P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold.
Nantermet PG, Burgey CS, Robinson KA, Pellicore JM, Newton CL, Deng JZ, Selnick HG, Lewis SD, Lucas BJ, Krueger JA, Miller-Stein C, White RB, Wong B, McMasters DR, Wallace AA, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP, Lyle TA. Nantermet PG, et al. Bioorg Med Chem Lett. 2005 Jun 2;15(11):2771-5. doi: 10.1016/j.bmcl.2005.03.110. Bioorg Med Chem Lett. 2005. PMID: 15911253
Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel.
Bilodeau MT, Balitza AE, Koester TJ, Manley PJ, Rodman LD, Buser-Doepner C, Coll KE, Fernandes C, Gibbs JB, Heimbrook DC, Huckle WR, Kohl N, Lynch JJ, Mao X, McFall RC, McLoughlin D, Miller-Stein CM, Rickert KW, Sepp-Lorenzino L, Shipman JM, Subramanian R, Thomas KA, Wong BK, Yu S, Hartman GD. Bilodeau MT, et al. Among authors: wong bk. J Med Chem. 2004 Dec 2;47(25):6363-72. doi: 10.1021/jm049697f. J Med Chem. 2004. PMID: 15566305
A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells.
Embrey MW, Wai JS, Funk TW, Homnick CF, Perlow DS, Young SD, Vacca JP, Hazuda DJ, Felock PJ, Stillmock KA, Witmer MV, Moyer G, Schleif WA, Gabryelski LJ, Jin L, Chen IW, Ellis JD, Wong BK, Lin JH, Leonard YM, Tsou NN, Zhuang L. Embrey MW, et al. Among authors: wong bk. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4550-4. doi: 10.1016/j.bmcl.2005.06.105. Bioorg Med Chem Lett. 2005. PMID: 16102965
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: wong bk. 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
Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists.
Bell IM, Bednar RA, Fay JF, Gallicchio SN, Hochman JH, McMasters DR, Miller-Stein C, Moore EL, Mosser SD, Pudvah NT, Quigley AG, Salvatore CA, Stump CA, Theberge CR, Wong BK, Zartman CB, Zhang XF, Kane SA, Graham SL, Vacca JP, Williams TM. Bell IM, et al. Among authors: wong bk. Bioorg Med Chem Lett. 2006 Dec 15;16(24):6165-9. doi: 10.1016/j.bmcl.2006.09.045. Epub 2006 Oct 5. Bioorg Med Chem Lett. 2006. PMID: 17027263
107 results