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Page 1
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: wexler rr. 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.
Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants.
Lam PY, Clark CG, Li R, Pinto DJ, Orwat MJ, Galemmo RA, Fevig JM, Teleha CA, Alexander RS, Smallwood AM, Rossi KA, Wright MR, Bai SA, He K, Luettgen JM, Wong PC, Knabb RM, Wexler RR. Lam PY, et al. Among authors: wexler rr. J Med Chem. 2003 Oct 9;46(21):4405-18. doi: 10.1021/jm020578e. J Med Chem. 2003. PMID: 14521405
5-Amidinoindoles as dual inhibitors of coagulation factors IXa and Xa.
Batt DG, Qiao JX, Modi DP, Houghton GC, Pierson DA, Rossi KA, Luettgen JM, Knabb RM, Jadhav PK, Wexler RR. Batt DG, et al. Among authors: wexler rr. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5269-73. doi: 10.1016/j.bmcl.2004.08.037. Bioorg Med Chem Lett. 2004. PMID: 15454209
5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa.
Qiao JX, Cheng X, Modi DP, Rossi KA, Luettgen JM, Knabb RM, Jadhav PK, Wexler RR. Qiao JX, et al. Among authors: wexler rr. Bioorg Med Chem Lett. 2005 Jan 3;15(1):29-35. doi: 10.1016/j.bmcl.2004.10.045. Bioorg Med Chem Lett. 2005. PMID: 15582405
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: wexler rr. 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: wexler rr. 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
Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
Pinto DJ, Orwat MJ, Koch S, Rossi KA, Alexander RS, Smallwood A, Wong PC, Rendina AR, Luettgen JM, Knabb RM, He K, Xin B, Wexler RR, Lam PY. Pinto DJ, et al. Among authors: wexler rr. J Med Chem. 2007 Nov 1;50(22):5339-56. doi: 10.1021/jm070245n. Epub 2007 Oct 3. J Med Chem. 2007. PMID: 17914785
195 results