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Page 1
Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.
Feng DM, Gardell SJ, Lewis SD, Bock MG, Chen Z, Freidinger RM, Naylor-Olsen AM, Ramjit HG, Woltmann R, Baskin EP, Lynch JJ, Lucas R, Shafer JA, Dancheck KB, Chen IW, Mao SS, Krueger JA, Hare TR, Mulichak AM, Vacca JP. Feng DM, et al. Among authors: hare tr. J Med Chem. 1997 Nov 7;40(23):3726-33. doi: 10.1021/jm970493r. J Med Chem. 1997. PMID: 9371237
Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.
Sanderson PE, Lyle TA, Cutrona KJ, Dyer DL, Dorsey BD, McDonough CM, Naylor-Olsen AM, Chen IW, Chen Z, Cook JJ, Cooper CM, Gardell SJ, Hare TR, Krueger JA, Lewis SD, Lin JH, Lucas BJ Jr, Lyle EA, Lynch JJ Jr, Stranieri MT, Vastag K, Yan Y, Shafer JA, Vacca JP. Sanderson PE, et al. Among authors: hare tr. J Med Chem. 1998 Nov 5;41(23):4466-74. doi: 10.1021/jm980368v. J Med Chem. 1998. PMID: 9804686
Antithrombotic efficacy of thrombin inhibitor L-374,087: intravenous activity in a primate model of venous thrombus extension and oral activity in a canine model of primary venous and coronary artery thrombosis.
Cook JJ, Gardell SJ, Holahan MA, Sitko GR, Stump GL, Wallace AA, Gilberto DB, Hare TR, Krueger JA, Dyer DL, Sanderson PE, Vacca JP, Shafer JA, Lynch JJ Jr. Cook JJ, et al. Among authors: hare tr. J Pharmacol Exp Ther. 1999 Apr;289(1):503-10. J Pharmacol Exp Ther. 1999. PMID: 10087043