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Page 1
Discovery of Potent and Selective Quinoxaline-Based Protease-Activated Receptor 4 (PAR4) Antagonists for the Prevention of Arterial Thrombosis.
Zhang X, Jiang W, Richter JM, Bates JA, Reznik SK, Stachura S, Rampulla R, Doddalingappa D, Ulaganathan S, Hua J, Bostwick JS, Sum C, Posy S, Malmstrom S, Dickey J, Harden D, Lawrence RM, Guarino VR, Schumacher WA, Wong P, Yang J, Gordon DA, Wexler RR, Priestley ES. Zhang X, et al. Among authors: hua j. J Med Chem. 2024 Mar 14;67(5):3571-3589. doi: 10.1021/acs.jmedchem.3c01986. Epub 2024 Feb 22. J Med Chem. 2024. PMID: 38385264
Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y1 antagonists.
Chao H, Turdi H, Herpin TF, Roberge JY, Liu Y, Schnur DM, Poss MA, Rehfuss R, Hua J, Wu Q, Price LA, Abell LM, Schumacher WA, Bostwick JS, Steinbacher TE, Stewart AB, Ogletree ML, Huang CS, Chang M, Cacace AM, Arcuri MJ, Celani D, Wexler RR, Lawrence RM. Chao H, et al. Among authors: hua j. J Med Chem. 2013 Feb 28;56(4):1704-14. doi: 10.1021/jm301708u. Epub 2013 Feb 18. J Med Chem. 2013. PMID: 23368907
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: hua 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
Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4.
Priestley ES, Banville J, Deon D, Dubé L, Gagnon M, Guy J, Lapointe P, Lavallée JF, Martel A, Plamondon S, Rémillard R, Ruediger E, Tremblay F, Posy SL, Guarino VR, Richter JM, Li J, Gupta A, Vetrichelvan M, Balapragalathan TJ, Mathur A, Hua J, Callejo M, Guay J, Sum CS, Cvijic ME, Watson C, Wong P, Yang J, Bouvier M, Gordon DA, Wexler RR, Marinier A. Priestley ES, et al. Among authors: hua j. J Med Chem. 2022 Jul 14;65(13):8843-8854. doi: 10.1021/acs.jmedchem.2c00359. Epub 2022 Jun 21. J Med Chem. 2022. PMID: 35729784
New azole antagonists with high affinity for the P2Y(1) receptor.
Ruel R, L'Heureux A, Thibeault C, Daris JP, Martel A, Price LA, Wu Q, Hua J, Wexler RR, Rehfuss R, Lam PY. Ruel R, et al. Among authors: hua j. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3519-22. doi: 10.1016/j.bmcl.2013.04.041. Epub 2013 Apr 25. Bioorg Med Chem Lett. 2013. PMID: 23668989
Identification of 1-{2-[4-chloro-1'-(2,2-dimethylpropyl)-7-hydroxy-1,2-dihydrospiro[indole-3,4'-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y(1) antagonist as an antiplatelet agent.
Jeon YT, Yang W, Qiao JX, Li L, Ruel R, Thibeault C, Hiebert S, Wang TC, Wang Y, Liu Y, Clark CG, Wong HS, Zhu J, Wu DR, Sun D, Chen BC, Mathur A, Chacko SA, Malley M, Chen XQ, Shen H, Huang CS, Schumacher WA, Bostwick JS, Stewart AB, Price LA, Hua J, Li D, Levesque PC, Seiffert DA, Rehfuss R, Wexler RR, Lam PY. Jeon YT, et al. Among authors: hua j. Bioorg Med Chem Lett. 2014 Mar 1;24(5):1294-8. doi: 10.1016/j.bmcl.2014.01.066. Epub 2014 Jan 31. Bioorg Med Chem Lett. 2014. PMID: 24513044
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: hua j. Sci Transl Med. 2017 Jan 4;9(371):eaaf5294. doi: 10.1126/scitranslmed.aaf5294. Sci Transl Med. 2017. PMID: 28053157
2,547 results