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Page 1
Identification of 6-Hydroxypyrimidin-4(1H)-one-3-carboxamides as Potent and Orally Active APJ Receptor Agonists.
Pi Z, Johnson JA, Meng W, Phillips M, Schumacher WA, Bostwick JS, Gargalovic PS, Onorato JM, Generaux CN, Wang T, He Y, Gordon DA, Wexler RR, Finlay HJ. Pi Z, et al. Among authors: wexler rr. ACS Med Chem Lett. 2021 Oct 22;12(11):1766-1772. doi: 10.1021/acsmedchemlett.1c00385. eCollection 2021 Nov 11. ACS Med Chem Lett. 2021. PMID: 34795866 Free PMC article.
Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1).
Pruitt JR, Pinto DJ, Galemmo RA Jr, Alexander RS, Rossi KA, Wells BL, Drummond S, Bostrom LL, Burdick D, Bruckner R, Chen H, Smallwood A, Wong PC, Wright MR, Bai S, Luettgen JM, Knabb RM, Lam PY, Wexler RR. Pruitt JR, et al. Among authors: wexler rr. J Med Chem. 2003 Dec 4;46(25):5298-315. doi: 10.1021/jm030212h. J Med Chem. 2003. PMID: 14640539
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
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
Pinto DJ, Orwat MJ, Quan ML, Han Q, Galemmo RA Jr, Amparo E, Wells B, Ellis C, He MY, Alexander RS, Rossi KA, Smallwood A, Wong PC, Luettgen JM, Rendina AR, Knabb RM, Mersinger L, Kettner C, Bai S, He K, Wexler RR, Lam PY. Pinto DJ, et al. Among authors: wexler rr. Bioorg Med Chem Lett. 2006 Aug 1;16(15):4141-7. doi: 10.1016/j.bmcl.2006.02.069. Epub 2006 May 30. Bioorg Med Chem Lett. 2006. PMID: 16730984
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
Discovery of ((S)-5-(methoxymethyl)-7-(1-methyl-1H-indol-2-yl)-2-(trifluoromethyl)-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl)((S)-2-(3-methylisoxazol-5-yl)pyrrolidin-1-yl)methanone as a potent and selective I(Kur) inhibitor.
Finlay HJ, Lloyd J, Vaccaro W, Kover A, Yan L, Bhave G, Prol J, Huynh T, Bhandaru R, Caringal Y, DiMarco J, Gan J, Harper T, Huang C, Conder ML, Sun H, Levesque P, Blanar M, Atwal K, Wexler R. Finlay HJ, et al. J Med Chem. 2012 Apr 12;55(7):3036-48. doi: 10.1021/jm201386u. Epub 2012 Mar 21. J Med Chem. 2012. PMID: 22409629
Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors.
Harikrishnan LS, Finlay HJ, Qiao JX, Kamau MG, Jiang J, Wang TC, Li J, Cooper CB, Poss MA, Adam LP, Taylor DS, Chen AY, Yin X, Sleph PG, Yang RZ, Sitkoff DF, Galella MA, Nirschl DS, Van Kirk K, Miller AV, Huang CS, Chang M, Chen XQ, Salvati ME, Wexler RR, Lawrence RM. Harikrishnan LS, et al. Among authors: wexler rr. J Med Chem. 2012 Jul 12;55(13):6162-75. doi: 10.1021/jm300611v. Epub 2012 Jun 22. J Med Chem. 2012. PMID: 22650305
Identification of a potent and metabolically stable series of fluorinated diphenylpyridylethanamine-based cholesteryl ester transfer protein inhibitors.
Miller MM, Liu Y, Jiang J, Johnson JA, Kamau M, Nirschl DS, Wang Y, Harikrishnan L, Taylor DS, Chen AY, Yin X, Seethala R, Peterson TL, Zvyaga T, Zhang J, Huang CS, Wexler RR, Poss MA, Lawrence RM, Adam LP, Salvati ME. Miller MM, et al. Among authors: wexler rr. Bioorg Med Chem Lett. 2012 Oct 15;22(20):6503-8. doi: 10.1016/j.bmcl.2012.08.011. Epub 2012 Aug 9. Bioorg Med Chem Lett. 2012. PMID: 22995620
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: wexler rr. J Med Chem. 2013 Feb 28;56(4):1704-14. doi: 10.1021/jm301708u. Epub 2013 Feb 18. J Med Chem. 2013. PMID: 23368907
195 results