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Page 1
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: bostwick js. J Med Chem. 2013 Feb 28;56(4):1704-14. doi: 10.1021/jm301708u. Epub 2013 Feb 18. J Med Chem. 2013. PMID: 23368907
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: bostwick js. 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
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: bostwick js. J Med Chem. 2013 Nov 27;56(22):9275-95. doi: 10.1021/jm4013906. Epub 2013 Nov 12. J Med Chem. 2013. PMID: 24164581
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: bostwick js. 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
4-Benzothiazole-7-hydroxyindolinyl diaryl ureas are potent P2Y1 antagonists with favorable pharmacokinetics: low clearance and small volume of distribution.
Qiao JX, Wang TC, Hiebert S, Hu CH, Schumacher WA, Spronk SA, Clark CG, Han Y, Hua J, Price LA, Shen H, Chacko SA, Everlof G, Bostwick JS, Steinbacher TE, Li YX, Huang CS, Seiffert DA, Rehfuss R, Wexler RR, Lam PY. Qiao JX, et al. Among authors: bostwick js. ChemMedChem. 2014 Oct;9(10):2327-43. doi: 10.1002/cmdc.201402141. Epub 2014 Jul 2. ChemMedChem. 2014. PMID: 24989964
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: bostwick js. Sci Transl Med. 2017 Jan 4;9(371):eaaf5294. doi: 10.1126/scitranslmed.aaf5294. Sci Transl Med. 2017. PMID: 28053157
Linking (Pyr)1apelin-13 pharmacokinetics to efficacy: Stabilization and measurement of a high clearance peptide in rodents.
Onorato JM, Xu C, Chen XQ, Rose AV, Generaux C, Lentz K, Shipkova P, Arthur S, Hennan JK, Haskell R, Myers MC, Lawrence RM, Finlay HJ, Basso M, Bostwick J, Fernando G, Garcia R, Hellings S, Hsu MY, Zhang R, Zhao L, Gargalovic P. Onorato JM, et al. Anal Biochem. 2019 Mar 1;568:41-50. doi: 10.1016/j.ab.2018.12.022. Epub 2018 Dec 31. Anal Biochem. 2019. PMID: 30605634
Biphenyl Acid Derivatives as APJ Receptor Agonists.
Su S, Clarke A, Han Y, Chao HJ, Bostwick J, Schumacher W, Wang T, Yan M, Hsu MY, Simmons E, Luk C, Xu C, Dabros M, Galella M, Onorato J, Gordon D, Wexler R, Gargalovic PS, Lawrence RM. Su S, et al. J Med Chem. 2019 Nov 27;62(22):10456-10465. doi: 10.1021/acs.jmedchem.9b01513. Epub 2019 Nov 14. J Med Chem. 2019. PMID: 31724863
Discovery of a Hydroxypyridinone APJ Receptor Agonist as a Clinical Candidate.
Johnson JA, Kim SH, Jiang J, Phillips M, Schumacher WA, Bostwick JS, Gargalovic PS, Onorato JM, Luk CE, Generaux C, He Y, Chen XQ, Xu C, Galella MA, Wang T, Gordon DA, Wexler RR, Finlay HJ. Johnson JA, et al. Among authors: bostwick js. J Med Chem. 2021 Mar 25;64(6):3086-3099. doi: 10.1021/acs.jmedchem.0c01878. Epub 2021 Mar 9. J Med Chem. 2021. PMID: 33689340
34 results