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Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308.
Hoekstra WJ, Maryanoff BE, Damiano BP, Andrade-Gordon P, Cohen JH, Costanzo MJ, Haertlein BJ, Hecker LR, Hulshizer BL, Kauffman JA, Keane P, McComsey DF, Mitchell JA, Scott L, Shah RD, Yabut SC. Hoekstra WJ, et al. Among authors: haertlein bj. J Med Chem. 1999 Dec 16;42(25):5254-65. doi: 10.1021/jm990418b. J Med Chem. 1999. PMID: 10602710
In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.
Costanzo MJ, Almond HR Jr, Hecker LR, Schott MR, Yabut SC, Zhang HC, Andrade-Gordon P, Corcoran TW, Giardino EC, Kauffman JA, Lewis JM, de Garavilla L, Haertlein BJ, Maryanoff BE. Costanzo MJ, et al. Among authors: haertlein bj. J Med Chem. 2005 Mar 24;48(6):1984-2008. doi: 10.1021/jm0303857. J Med Chem. 2005. PMID: 15771442
A novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase: molecular mechanisms and anti-inflammatory activity in vivo.
de Garavilla L, Greco MN, Sukumar N, Chen ZW, Pineda AO, Mathews FS, Di Cera E, Giardino EC, Wells GI, Haertlein BJ, Kauffman JA, Corcoran TW, Derian CK, Eckardt AJ, Damiano BP, Andrade-Gordon P, Maryanoff BE. de Garavilla L, et al. Among authors: haertlein bj. J Biol Chem. 2005 May 6;280(18):18001-7. doi: 10.1074/jbc.M501302200. Epub 2005 Feb 28. J Biol Chem. 2005. PMID: 15741158 Free article.
Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif.
Kreutter KD, Lu T, Lee L, Giardino EC, Patel S, Huang H, Xu G, Fitzgerald M, Haertlein BJ, Mohan V, Crysler C, Eisennagel S, Dasgupta M, McMillan M, Spurlino JC, Huebert ND, Maryanoff BE, Tomczuk BE, Damiano BP, Player MR. Kreutter KD, et al. Among authors: haertlein bj. Bioorg Med Chem Lett. 2008 May 1;18(9):2865-70. doi: 10.1016/j.bmcl.2008.03.087. Epub 2008 Apr 8. Bioorg Med Chem Lett. 2008. PMID: 18420408
Administration of a potent antagonist of protease-activated receptor-1 (PAR-1) attenuates vascular restenosis following balloon angioplasty in rats.
Andrade-Gordon P, Derian CK, Maryanoff BE, Zhang HC, Addo MF, Cheung Wm, Damiano BP, D'Andrea MR, Darrow AL, de Garavilla L, Eckardt AJ, Giardino EC, Haertlein BJ, McComsey DF. Andrade-Gordon P, et al. Among authors: haertlein bj. J Pharmacol Exp Ther. 2001 Jul;298(1):34-42. J Pharmacol Exp Ther. 2001. PMID: 11408522
21 results