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2002 1
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22 results

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Page 1
Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa.
Fang T, Corte JR, Gilligan PJ, Jeon Y, Osuna H, Rossi KA, Myers JE Jr, Sheriff S, Lou Z, Zheng JJ, Harper TW, Bozarth JM, Wu Y, Luettgen JM, Seiffert DA, Wexler RR, Lam PYS. Fang T, et al. Among authors: zheng jj. Bioorg Med Chem Lett. 2020 Feb 15;30(4):126949. doi: 10.1016/j.bmcl.2020.126949. Epub 2020 Jan 7. Bioorg Med Chem Lett. 2020. PMID: 31932224
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: zheng j. 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
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: zheng jj. 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
Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).
Pinto DJP, Orwat MJ, Smith LM 2nd, Quan ML, Lam PYS, Rossi KA, Apedo A, Bozarth JM, Wu Y, Zheng JJ, Xin B, Toussaint N, Stetsko P, Gudmundsson O, Maxwell B, Crain EJ, Wong PC, Lou Z, Harper TW, Chacko SA, Myers JE Jr, Sheriff S, Zhang H, Hou X, Mathur A, Seiffert DA, Wexler RR, Luettgen JM, Ewing WR. Pinto DJP, et al. Among authors: zheng jj. J Med Chem. 2017 Dec 14;60(23):9703-9723. doi: 10.1021/acs.jmedchem.7b01171. Epub 2017 Nov 17. J Med Chem. 2017. PMID: 29077405
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: zheng jj. 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
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: zheng j. 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
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: zheng jj. 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
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. Among authors: zheng jj. 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
Conformationally constrained ortho-anilino diaryl ureas: discovery of 1-(2-(1'-neopentylspiro[indoline-3,4'-piperidine]-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a potent, selective, and bioavailable P2Y1 antagonist.
Qiao JX, Wang TC, Ruel R, Thibeault C, L'Heureux A, Schumacher WA, Spronk SA, Hiebert S, Bouthillier G, Lloyd J, Pi Z, Schnur DM, Abell LM, Hua J, Price LA, Liu E, Wu Q, Steinbacher TE, Bostwick JS, Chang M, Zheng J, Gao Q, Ma B, McDonnell PA, Huang CS, Rehfuss R, Wexler RR, Lam PY. Qiao JX, et al. Among authors: zheng j. J Med Chem. 2013 Nov 27;56(22):9275-95. doi: 10.1021/jm4013906. Epub 2013 Nov 12. J Med Chem. 2013. PMID: 24164581
22 results