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Discovery of ((1S,3R)-1-isopropyl-3-((3S,4S)-3-methoxy-tetrahydro-2H-pyran-4-ylamino)cyclopentyl)(4-(5-(trifluoromethyl)pyridazin-3-yl)piperazin-1-yl)methanone, PF-4254196, a CCR2 antagonist with an improved cardiovascular profile.
Hughes RO, Rogier DJ, Devraj R, Zheng C, Cao G, Feng H, Xia M, Anand R, Xing L, Glenn J, Zhang K, Covington M, Morton PA, Hutzler JM, Davis JW 2nd, Scherle P, Baribaud F, Bahinski A, Mo ZL, Newton R, Metcalf B, Xue CB. Hughes RO, et al. Among authors: newton r. Bioorg Med Chem Lett. 2011 May 1;21(9):2626-30. doi: 10.1016/j.bmcl.2011.01.034. Epub 2011 Jan 15. Bioorg Med Chem Lett. 2011. PMID: 21315584
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
Xue CB, Wang A, Meloni D, Zhang K, Kong L, Feng H, Glenn J, Huang T, Zhang Y, Cao G, Anand R, Zheng C, Xia M, Han Q, Robinson DJ, Storace L, Shao L, Li M, Brodmerkel CM, Covington M, Scherle P, Diamond S, Yeleswaram S, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B. Xue CB, et al. Among authors: newton r. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7473-8. doi: 10.1016/j.bmcl.2010.10.020. Epub 2010 Oct 13. Bioorg Med Chem Lett. 2010. PMID: 21036044
Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist.
Zheng C, Cao G, Xia M, Feng H, Glenn J, Anand R, Zhang K, Huang T, Wang A, Kong L, Li M, Galya L, Hughes RO, Devraj R, Morton PA, Rogier DJ, Covington M, Baribaud F, Shin N, Scherle P, Diamond S, Yeleswaram S, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B, Xue CB. Zheng C, et al. Among authors: newton r. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1442-6. doi: 10.1016/j.bmcl.2011.01.015. Epub 2011 Jan 11. Bioorg Med Chem Lett. 2011. PMID: 21295478
Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.
Xue CB, Wang A, Han Q, Zhang Y, Cao G, Feng H, Huang T, Zheng C, Xia M, Zhang K, Kong L, Glenn J, Anand R, Meloni D, Robinson DJ, Shao L, Storace L, Li M, Hughes RO, Devraj R, Morton PA, Rogier DJ, Covington M, Scherle P, Diamond S, Emm T, Yeleswaram S, Contel N, Vaddi K, Newton R, Hollis G, Metcalf B. Xue CB, et al. Among authors: newton r. ACS Med Chem Lett. 2011 Oct 5;2(12):913-8. doi: 10.1021/ml200199c. eCollection 2011 Dec 8. ACS Med Chem Lett. 2011. PMID: 24900280 Free PMC article.
Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents.
Ott GR, Asakawa N, Lu Z, Anand R, Liu RQ, Covington MB, Vaddi K, Qian M, Newton RC, Christ DD, Trzaskos JM, Duan JJ. Ott GR, et al. Among authors: newton rc. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1577-82. doi: 10.1016/j.bmcl.2008.01.075. Epub 2008 Jan 26. Bioorg Med Chem Lett. 2008. PMID: 18242982
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification.
Xue CB, He X, Roderick J, Corbett RL, Duan JJ, Liu RQ, Covington MB, Newton RC, Trzaskos JM, Magolda RL, Wexler RR, Decicco CP. Xue CB, et al. Among authors: newton rc. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4293-7. doi: 10.1016/j.bmcl.2003.09.056. Bioorg Med Chem Lett. 2003. PMID: 14643312
2,125 results