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Page 1
Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.
Quan ML, Wong PC, Wang C, Woerner F, Smallheer JM, Barbera FA, Bozarth JM, Brown RL, Harpel MR, Luettgen JM, Morin PE, Peterson T, Ramamurthy V, Rendina AR, Rossi KA, Watson CA, Wei A, Zhang G, Seiffert D, Wexler RR. Quan ML, et al. J Med Chem. 2014 Feb 13;57(3):955-69. doi: 10.1021/jm401670x. Epub 2014 Jan 17. J Med Chem. 2014. PMID: 24405333
Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.
Zhang X, Glunz PW, Johnson JA, Jiang W, Jacutin-Porte S, Ladziata V, Zou Y, Phillips MS, Wurtz NR, Parkhurst B, Rendina AR, Harper TM, Cheney DL, Luettgen JM, Wong PC, Seiffert D, Wexler RR, Priestley ES. Zhang X, et al. J Med Chem. 2016 Aug 11;59(15):7125-37. doi: 10.1021/acs.jmedchem.6b00469. Epub 2016 Aug 2. J Med Chem. 2016. PMID: 27455395
Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding.
Wong PC, Seiffert D, Bird JE, Watson CA, Bostwick JS, Giancarli M, Allegretto N, Hua J, Harden D, Guay J, Callejo M, Miller MM, Lawrence RM, Banville J, Guy J, Maxwell BD, Priestley ES, Marinier A, Wexler RR, Bouvier M, Gordon DA, Schumacher WA, Yang J. Wong PC, et al. Among authors: seiffert d. Sci Transl Med. 2017 Jan 4;9(371):eaaf5294. doi: 10.1126/scitranslmed.aaf5294. Sci Transl Med. 2017. PMID: 28053157
Inhibition of factor XIa as a new approach to anticoagulation.
Schumacher WA, Luettgen JM, Quan ML, Seiffert DA. Schumacher WA, et al. Among authors: seiffert da. Arterioscler Thromb Vasc Biol. 2010 Mar;30(3):388-92. doi: 10.1161/ATVBAHA.109.197178. Epub 2010 Feb 5. Arterioscler Thromb Vasc Biol. 2010. PMID: 20139363 Review.
Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.
Hangeland JJ, Friends TJ, Rossi KA, Smallheer JM, Wang C, Sun Z, Corte JR, Fang T, Wong PC, Rendina AR, Barbera FA, Bozarth JM, Luettgen JM, Watson CA, Zhang G, Wei A, Ramamurthy V, Morin PE, Bisacchi GS, Subramaniam S, Arunachalam P, Mathur A, Seiffert DA, Wexler RR, Quan ML. Hangeland JJ, et al. Among authors: seiffert da. J Med Chem. 2014 Dec 11;57(23):9915-32. doi: 10.1021/jm5010607. Epub 2014 Dec 2. J Med Chem. 2014. PMID: 25405503
Pyridine and pyridinone-based factor XIa inhibitors.
Corte JR, Fang T, Hangeland JJ, Friends TJ, Rendina AR, Luettgen JM, Bozarth JM, Barbera FA, Rossi KA, Wei A, Ramamurthy V, Morin PE, Seiffert DA, Wexler RR, Quan ML. Corte JR, et al. Among authors: seiffert da. Bioorg Med Chem Lett. 2015 Feb 15;25(4):925-30. doi: 10.1016/j.bmcl.2014.12.050. Epub 2014 Dec 31. Bioorg Med Chem Lett. 2015. PMID: 25592713
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.
Pinto DJ, Smallheer JM, Corte JR, Austin EJ, Wang C, Fang T, Smith LM 2nd, Rossi KA, Rendina AR, Bozarth JM, Zhang G, Wei A, Ramamurthy V, Sheriff S, Myers JE Jr, Morin PE, Luettgen JM, Seiffert DA, Quan ML, Wexler RR. Pinto DJ, et al. Among authors: seiffert da. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1635-42. doi: 10.1016/j.bmcl.2015.01.028. Epub 2015 Feb 4. Bioorg Med Chem Lett. 2015. PMID: 25728130
Novel phenylalanine derived diamides as Factor XIa inhibitors.
Smith LM 2nd, Orwat MJ, Hu Z, Han W, Wang C, Rossi KA, Gilligan PJ, Pabbisetty KB, Osuna H, Corte JR, Rendina AR, Luettgen JM, Wong PC, Narayanan R, Harper TW, Bozarth JM, Crain EJ, Wei A, Ramamurthy V, Morin PE, Xin B, Zheng J, Seiffert DA, Quan ML, Lam PYS, Wexler RR, Pinto DJP. Smith LM 2nd, et al. Among authors: seiffert da. Bioorg Med Chem Lett. 2016 Jan 15;26(2):472-478. doi: 10.1016/j.bmcl.2015.11.089. Epub 2015 Nov 26. Bioorg Med Chem Lett. 2016. PMID: 26704266
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.
Corte JR, Fang T, Pinto DJ, Orwat MJ, Rendina AR, Luettgen JM, Rossi KA, Wei A, Ramamurthy V, Myers JE Jr, Sheriff S, Narayanan R, Harper TW, Zheng JJ, Li YX, Seiffert DA, Wexler RR, Quan ML. Corte JR, et al. Among authors: seiffert da. Bioorg Med Chem. 2016 May 15;24(10):2257-72. doi: 10.1016/j.bmc.2016.03.062. Epub 2016 Apr 1. Bioorg Med Chem. 2016. PMID: 27073051
136 results