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Page 1
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. 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
Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.
Corte JR, Fang T, Pinto DJ, Han W, Hu Z, Jiang XJ, Li YL, Gauuan JF, Hadden M, Orton D, Rendina AR, Luettgen JM, Wong PC, He K, Morin PE, Chang CH, Cheney DL, Knabb RM, Wexler RR, Lam PY. Corte JR, et al. Bioorg Med Chem Lett. 2008 May 1;18(9):2845-9. doi: 10.1016/j.bmcl.2008.03.092. Epub 2008 Apr 8. Bioorg Med Chem Lett. 2008. PMID: 18424044
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: corte jr. 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. 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: corte jr. 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: corte jr. 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
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.
Corte JR, Pinto DJP, Fang T, Osuna H, Yang W, Wang Y, Lai A, Clark CG, Sun JH, Rampulla R, Mathur A, Kaspady M, Neithnadka PR, Li YC, Rossi KA, Myers JE Jr, Sheriff S, Lou Z, Harper TW, Huang C, Zheng JJ, Bozarth JM, Wu Y, Wong PC, Crain EJ, Seiffert DA, Luettgen JM, Lam PYS, Wexler RR, Ewing WR. Corte JR, et al. J Med Chem. 2020 Jan 23;63(2):784-803. doi: 10.1021/acs.jmedchem.9b01768. Epub 2020 Jan 2. J Med Chem. 2020. PMID: 31833761
Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.
Yang W, Wang Y, Lai A, Clark CG, Corte JR, Fang T, Gilligan PJ, Jeon Y, Pabbisetty KB, Rampulla RA, Mathur A, Kaspady M, Neithnadka PR, Arumugam A, Raju S, Rossi KA, Myers JE Jr, Sheriff S, Lou Z, Zheng JJ, Chacko SA, Bozarth JM, Wu Y, Crain EJ, Wong PC, Seiffert DA, Luettgen JM, Lam PYS, Wexler RR, Ewing WR. Yang W, et al. Among authors: corte jr. J Med Chem. 2020 Jul 9;63(13):7226-7242. doi: 10.1021/acs.jmedchem.0c00464. Epub 2020 Jun 17. J Med Chem. 2020. PMID: 32456431
Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.
Dilger AK, Pabbisetty KB, Corte JR, De Lucca I, Fang T, Yang W, Pinto DJP, Wang Y, Zhu Y, Mathur A, Li J, Hou X, Smith D, Sun D, Zhang H, Krishnananthan S, Wu DR, Myers JE Jr, Sheriff S, Rossi KA, Chacko S, Zheng JJ, Galella MA, Ziemba T, Dierks EA, Bozarth JM, Wu Y, Crain E, Wong PC, Luettgen JM, Wexler RR, Ewing WR. Dilger AK, et al. Among authors: corte jr. J Med Chem. 2022 Feb 10;65(3):1770-1785. doi: 10.1021/acs.jmedchem.1c00613. Epub 2021 Sep 8. J Med Chem. 2022. PMID: 34494428
27 results