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Page 1
Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues.
Qiao JX, Cheng X, Smallheer JM, Galemmo RA, Drummond S, Pinto DJ, Cheney DL, He K, Wong PC, Luettgen JM, Knabb RM, Wexler RR, Lam PY. Qiao JX, et al. Among authors: smallheer jm. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1432-7. doi: 10.1016/j.bmcl.2006.11.071. Epub 2006 Dec 1. Bioorg Med Chem Lett. 2007. PMID: 17174550
SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.
Smallheer JM, Alexander RS, Wang J, Wang S, Nakajima S, Rossi KA, Smallwood A, Barbera F, Burdick D, Luettgen JM, Knabb RM, Wexler RR, Jadhav PK. Smallheer JM, et al. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5263-7. doi: 10.1016/j.bmcl.2004.08.034. Bioorg Med Chem Lett. 2004. PMID: 15454208
Sulfonamidolactam inhibitors of coagulation factor Xa.
Smallheer JM, Wang S, Laws ML, Nakajima S, Hu Z, Han W, Jacobson I, Luettgen JM, Rossi KA, Rendina AR, Knabb RM, Wexler RR, Lam PY, Quan ML. Smallheer JM, et al. Bioorg Med Chem Lett. 2008 Apr 1;18(7):2428-33. doi: 10.1016/j.bmcl.2008.02.054. Epub 2008 Feb 26. Bioorg Med Chem Lett. 2008. PMID: 18329876
Factor Xa inhibitors: next-generation antithrombotic agents.
Pinto DJ, Smallheer JM, Cheney DL, Knabb RM, Wexler RR. Pinto DJ, et al. Among authors: smallheer jm. J Med Chem. 2010 Sep 9;53(17):6243-74. doi: 10.1021/jm100146h. J Med Chem. 2010. PMID: 20503967 Review. No abstract available.
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. Among authors: smallheer jm. J Med Chem. 2014 Feb 13;57(3):955-69. doi: 10.1021/jm401670x. Epub 2014 Jan 17. J Med Chem. 2014. PMID: 24405333
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: smallheer jm. J Med Chem. 2014 Dec 11;57(23):9915-32. doi: 10.1021/jm5010607. Epub 2014 Dec 2. J Med Chem. 2014. PMID: 25405503
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: smallheer jm. 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
Factor XIa Inhibitors as New Anticoagulants.
Quan ML, Pinto DJP, Smallheer JM, Ewing WR, Rossi KA, Luettgen JM, Seiffert DA, Wexler RR. Quan ML, et al. Among authors: smallheer jm. J Med Chem. 2018 Sep 13;61(17):7425-7447. doi: 10.1021/acs.jmedchem.8b00173. Epub 2018 May 18. J Med Chem. 2018. PMID: 29775297 Review.
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.
Clark CG, Rossi KA, Corte JR, Fang T, Smallheer JM, De Lucca I, Nirschl DS, Orwat MJ, Pinto DJP, Hu Z, Wang Y, Yang W, Jeon Y, Ewing WR, Myers JE Jr, Sheriff S, Lou Z, Bozarth JM, Wu Y, Rendina A, Harper T, Zheng J, Xin B, Xiang Q, Luettgen JM, Seiffert DA, Wexler RR, Lam PYS. Clark CG, et al. Among authors: smallheer jm. Bioorg Med Chem Lett. 2019 Oct 1;29(19):126604. doi: 10.1016/j.bmcl.2019.08.008. Epub 2019 Aug 16. Bioorg Med Chem Lett. 2019. PMID: 31445854
Small molecule and macrocyclic pyrazole derived inhibitors of myeloperoxidase (MPO).
Hu CH, Neissel Valente MW, Halpern OS, Jusuf S, Khan JA, Locke GA, Duke GJ, Liu X, Duclos FJ, Wexler RR, Kick EK, Smallheer JM. Hu CH, et al. Among authors: smallheer jm. Bioorg Med Chem Lett. 2021 Jun 15;42:128010. doi: 10.1016/j.bmcl.2021.128010. Epub 2021 Apr 1. Bioorg Med Chem Lett. 2021. PMID: 33811992
17 results