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Page 1
Synthesis and P1' SAR exploration of potent macrocyclic tissue factor-factor VIIa inhibitors.
Ladziata VU, Glunz PW, Zou Y, Zhang X, Jiang W, Jacutin-Porte S, Cheney DL, Wei A, Luettgen JM, Harper TM, Wong PC, Seiffert D, Wexler RR, Priestley ES. Ladziata VU, et al. Among authors: harper tm. Bioorg Med Chem Lett. 2016 Oct 15;26(20):5051-5057. doi: 10.1016/j.bmcl.2016.08.088. Epub 2016 Aug 28. Bioorg Med Chem Lett. 2016. PMID: 27612545
Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors.
Zhang X, Jiang W, Jacutin-Porte S, Glunz PW, Zou Y, Cheng X, Nirschl AH, Wurtz NR, Luettgen JM, Rendina AR, Luo G, Harper TM, Wei A, Anumula R, Cheney DL, Knabb RM, Wong PC, Wexler RR, Priestley ES. Zhang X, et al. Among authors: harper tm. ACS Med Chem Lett. 2013 Dec 26;5(2):188-92. doi: 10.1021/ml400453z. eCollection 2014 Feb 13. ACS Med Chem Lett. 2013. PMID: 24900796 Free PMC article.
Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.
Zhang X, Glunz PW, Johnson JA, Jiang W, Jacutin-Porte S, Ladziata V, Zou Y, Phillips MS, Wurtz NR, Parkhurst B, Rendina AR, Harper TM, Cheney DL, Luettgen JM, Wong PC, Seiffert D, Wexler RR, Priestley ES. Zhang X, et al. Among authors: harper tm. J Med Chem. 2016 Aug 11;59(15):7125-37. doi: 10.1021/acs.jmedchem.6b00469. Epub 2016 Aug 2. J Med Chem. 2016. PMID: 27455395
Design and Synthesis of Novel Meta-Linked Phenylglycine Macrocyclic FVIIa Inhibitors.
Richter JM, Cheney DL, Bates JA, Wei A, Luettgen JM, Rendina AR, Harper TM, Narayanan R, Wong PC, Seiffert D, Wexler RR, Priestley ES. Richter JM, et al. Among authors: harper tm. ACS Med Chem Lett. 2016 Nov 1;8(1):67-72. doi: 10.1021/acsmedchemlett.6b00375. eCollection 2017 Jan 12. ACS Med Chem Lett. 2016. PMID: 28105277 Free PMC article.
Neutral macrocyclic factor VIIa inhibitors.
Wurtz NR, Parkhurst BL, DeLucca I, Glunz PW, Jiang W, Zhang X, Cheney DL, Bozarth JM, Rendina AR, Wei A, Harper T, Luettgen JM, Wu Y, Wong PC, Seiffert DA, Wexler RR, Priestley ES. Wurtz NR, et al. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2650-2654. doi: 10.1016/j.bmcl.2017.04.008. Epub 2017 Apr 19. Bioorg Med Chem Lett. 2017. PMID: 28460818
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.
Hu Z, Wong PC, Gilligan PJ, Han W, Pabbisetty KB, Bozarth JM, Crain EJ, Harper T, Luettgen JM, Myers JE Jr, Ramamurthy V, Rossi KA, Sheriff S, Watson CA, Wei A, Zheng JJ, Seiffert DA, Wexler RR, Quan ML. Hu Z, et al. ACS Med Chem Lett. 2015 Apr 8;6(5):590-5. doi: 10.1021/acsmedchemlett.5b00066. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005539 Free PMC article.
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.
Clark CG, Rossi KA, Corte JR, Fang T, Smallheer JM, De Lucca I, Nirschl DS, Orwat MJ, Pinto DJP, Hu Z, Wang Y, Yang W, Jeon Y, Ewing WR, Myers JE Jr, Sheriff S, Lou Z, Bozarth JM, Wu Y, Rendina A, Harper T, Zheng J, Xin B, Xiang Q, Luettgen JM, Seiffert DA, Wexler RR, Lam PYS. Clark CG, et al. Bioorg Med Chem Lett. 2019 Oct 1;29(19):126604. doi: 10.1016/j.bmcl.2019.08.008. Epub 2019 Aug 16. Bioorg Med Chem Lett. 2019. PMID: 31445854
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
Triazolo and imidazo dihydropyrazolopyrimidine potassium channel antagonists.
Finlay HJ, Jiang J, Caringal Y, Kover A, Conder ML, Xing D, Levesque P, Harper T, Hsueh MM, Atwal K, Blanar M, Wexler R, Lloyd J. Finlay HJ, et al. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1743-7. doi: 10.1016/j.bmcl.2013.01.064. Epub 2013 Jan 26. Bioorg Med Chem Lett. 2013. PMID: 23414837
21 results