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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: lawrence rm. 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: lawrence rm. 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 Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy.
Miller MM, Banville J, Friends TJ, Gagnon M, Hangeland JJ, Lavallée JF, Martel A, O'Grady H, Rémillard R, Ruediger E, Tremblay F, Posy SL, Allegretto NJ, Guarino VR, Harden DG, Harper TW, Hartl K, Josephs J, Malmstrom S, Watson C, Yang Y, Zhang G, Wong P, Yang J, Bouvier M, Seiffert DA, Wexler RR, Lawrence RM, Priestley ES, Marinier A. Miller MM, et al. Among authors: lawrence rm. J Med Chem. 2019 Aug 22;62(16):7400-7416. doi: 10.1021/acs.jmedchem.9b00186. Epub 2019 Aug 5. J Med Chem. 2019. PMID: 31246024
Discovery of a potent and novel motilin agonist.
Li JJ, Chao HG, Wang H, Tino JA, Lawrence RM, Ewing WR, Ma Z, Yan M, Slusarchyk D, Seethala R, Sun H, Li D, Burford NT, Stoffel RH, Salyan ME, Li CY, Witkus M, Zhao N, Rich A, Gordon DA. Li JJ, et al. Among authors: lawrence rm. J Med Chem. 2004 Mar 25;47(7):1704-8. doi: 10.1021/jm0304865. J Med Chem. 2004. PMID: 15027861
Triphenylethanamine Derivatives as Cholesteryl Ester Transfer Protein Inhibitors: Discovery of N-[(1R)-1-(3-Cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide (BMS-795311).
Qiao JX, Wang TC, Adam LP, Chen AY, Taylor DS, Yang RZ, Zhuang S, Sleph PG, Li JP, Li D, Yin X, Chang M, Chen XQ, Shen H, Li J, Smith D, Wu DR, Leith L, Harikrishnan LS, Kamau MG, Miller MM, Bilder D, Rampulla R, Li YX, Xu C, Lawrence RM, Poss MA, Levesque P, Gordon DA, Huang CS, Finlay HJ, Wexler RR, Salvati ME. Qiao JX, et al. Among authors: lawrence rm. J Med Chem. 2015 Nov 25;58(22):9010-26. doi: 10.1021/acs.jmedchem.5b01363. Epub 2015 Nov 17. J Med Chem. 2015. PMID: 26524347
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: lawrence rm. Sci Transl Med. 2017 Jan 4;9(371):eaaf5294. doi: 10.1126/scitranslmed.aaf5294. Sci Transl Med. 2017. PMID: 28053157
PK/PD Disconnect Observed with a Reversible Endothelial Lipase Inhibitor.
Hangeland JJ, Abell LM, Adam LP, Jiang J, Friends TJ, Haque LE, Neels J, Onorato JM, Chen AYA, Taylor DS, Yin X, Harrity TW, Basso MD, Yang R, Sleph PG, Gordon DA, Huang CS, Wexler RR, Finlay HJ, Lawrence RM. Hangeland JJ, et al. Among authors: lawrence rm. ACS Med Chem Lett. 2018 Jun 15;9(7):673-678. doi: 10.1021/acsmedchemlett.8b00138. eCollection 2018 Jul 12. ACS Med Chem Lett. 2018. PMID: 30034599 Free PMC article.
Discovery of a Lead Triphenylethanamine Cholesterol Ester Transfer Protein (CETP) Inhibitor.
Finlay HJ, Jiang J, Rampulla R, Salvati ME, Qiao JX, Wang TC, Lawrence RM, Harikrishnan LS, Kamau MG, Taylor DS, Chen AYA, Yin X, Huang CS, Chang M, Chen XQ, Sleph PG, Xu C, Li J, Levesque P, Adam LP, Wexler RR. Finlay HJ, et al. Among authors: lawrence rm. ACS Med Chem Lett. 2019 May 6;10(6):911-916. doi: 10.1021/acsmedchemlett.9b00086. eCollection 2019 Jun 13. ACS Med Chem Lett. 2019. PMID: 31223447 Free PMC article.
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. Among authors: lawrence rm. 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 and SAR of aryl hydroxy pyrimidinones as potent small molecule agonists of the GPCR APJ.
Myers MC, Bilder DM, Cavallaro CL, Chao HJ, Su S, Burford NT, Nayeem A, Wang T, Yan M, Langish RA, Dabros M, Li YX, Rose AV, Behnia K, Onorato JM, Gargalovic PS, Wexler RR, Lawrence RM. Myers MC, et al. Among authors: lawrence rm. Bioorg Med Chem Lett. 2020 Apr 1;30(7):126955. doi: 10.1016/j.bmcl.2020.126955. Epub 2020 Jan 22. Bioorg Med Chem Lett. 2020. PMID: 32035698
151 results