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Page 1
Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.
Wang TC, Qiao JX, Clark CG, Jua J, Price LA, Wu Q, Chang M, Zheng J, Huang CS, Everlof G, Schumacher WA, Wong PC, Seiffert DA, Stewart AB, Bostwick JS, Crain EJ, Watson CA, Rehfuss R, Wexler RR, Lam PY. Wang TC, et al. Among authors: lam py. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3239-43. doi: 10.1016/j.bmcl.2013.03.125. Epub 2013 Apr 6. Bioorg Med Chem Lett. 2013. PMID: 23602442
Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
Quan ML, Lam PY, Han Q, Pinto DJ, He MY, Li R, Ellis CD, Clark CG, Teleha CA, Sun JH, Alexander RS, Bai S, Luettgen JM, Knabb RM, Wong PC, Wexler RR. Quan ML, et al. Among authors: lam py. J Med Chem. 2005 Mar 24;48(6):1729-44. doi: 10.1021/jm0497949. J Med Chem. 2005. PMID: 15771420
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: lam py. 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
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: lam py. 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
2-Aminothiazole based P2Y(1) antagonists as novel antiplatelet agents.
Pi Z, Sutton J, Lloyd J, Hua J, Price L, Wu Q, Chang M, Zheng J, Rehfuss R, Huang CS, Wexler RR, Lam PY. Pi Z, et al. Among authors: lam py. Bioorg Med Chem Lett. 2013 Jul 15;23(14):4206-9. doi: 10.1016/j.bmcl.2013.05.025. Epub 2013 May 17. Bioorg Med Chem Lett. 2013. PMID: 23743287
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: lam py. J Med Chem. 2013 Nov 27;56(22):9275-95. doi: 10.1021/jm4013906. Epub 2013 Nov 12. J Med Chem. 2013. PMID: 24164581
Potent P2Y1 urea antagonists bearing various cyclic amine scaffolds.
Ruel R, L'Heureux A, Thibeault C, Lapointe P, Martel A, Qiao JX, Hua J, Price LA, Wu Q, Chang M, Zheng J, Huang CS, Wexler RR, Rehfuss R, Lam PY. Ruel R, et al. Among authors: lam py. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6825-8. doi: 10.1016/j.bmcl.2013.10.009. Epub 2013 Oct 11. Bioorg Med Chem Lett. 2013. PMID: 24269480
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: lam py. 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
272 results