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Page 1
Discovery of VX-509 (Decernotinib): A Potent and Selective Janus Kinase 3 Inhibitor for the Treatment of Autoimmune Diseases.
Farmer LJ, Ledeboer MW, Hoock T, Arnost MJ, Bethiel RS, Bennani YL, Black JJ, Brummel CL, Chakilam A, Dorsch WA, Fan B, Cochran JE, Halas S, Harrington EM, Hogan JK, Howe D, Huang H, Jacobs DH, Laitinen LM, Liao S, Mahajan S, Marone V, Martinez-Botella G, McCarthy P, Messersmith D, Namchuk M, Oh L, Penney MS, Pierce AC, Raybuck SA, Rugg A, Salituro FG, Saxena K, Shannon D, Shlyakter D, Swenson L, Tian SK, Town C, Wang J, Wang T, Wannamaker MW, Winquist RJ, Zuccola HJ. Farmer LJ, et al. Among authors: bennani yl. J Med Chem. 2015 Sep 24;58(18):7195-216. doi: 10.1021/acs.jmedchem.5b00301. Epub 2015 Sep 10. J Med Chem. 2015. PMID: 26230873
2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.
Ledeboer MW, Pierce AC, Duffy JP, Gao H, Messersmith D, Salituro FG, Nanthakumar S, Come J, Zuccola HJ, Swenson L, Shlyakter D, Mahajan S, Hoock T, Fan B, Tsai WJ, Kolaczkowski E, Carrier S, Hogan JK, Zessis R, Pazhanisamy S, Bennani YL. Ledeboer MW, et al. Among authors: bennani yl. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6529-33. doi: 10.1016/j.bmcl.2009.10.053. Epub 2009 Oct 24. Bioorg Med Chem Lett. 2009. PMID: 19857967
In vitro and in vivo isotope effects with hepatitis C protease inhibitors: enhanced plasma exposure of deuterated telaprevir versus telaprevir in rats.
Maltais F, Jung YC, Chen M, Tanoury J, Perni RB, Mani N, Laitinen L, Huang H, Liao S, Gao H, Tsao H, Block E, Ma C, Shawgo RS, Town C, Brummel CL, Howe D, Pazhanisamy S, Raybuck S, Namchuk M, Bennani YL. Maltais F, et al. Among authors: bennani yl. J Med Chem. 2009 Dec 24;52(24):7993-8001. doi: 10.1021/jm901023f. J Med Chem. 2009. PMID: 19894743
Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.
Wang T, Duffy JP, Wang J, Halas S, Salituro FG, Pierce AC, Zuccola HJ, Black JR, Hogan JK, Jepson S, Shlyakter D, Mahajan S, Gu Y, Hoock T, Wood M, Furey BF, Frantz JD, Dauffenbach LM, Germann UA, Fan B, Namchuk M, Bennani YL, Ledeboer MW. Wang T, et al. Among authors: bennani yl. J Med Chem. 2009 Dec 24;52(24):7938-41. doi: 10.1021/jm901383u. J Med Chem. 2009. PMID: 20014869
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
Clark MP, Ledeboer MW, Davies I, Byrn RA, Jones SM, Perola E, Tsai A, Jacobs M, Nti-Addae K, Bandarage UK, Boyd MJ, Bethiel RS, Court JJ, Deng H, Duffy JP, Dorsch WA, Farmer LJ, Gao H, Gu W, Jackson K, Jacobs DH, Kennedy JM, Ledford B, Liang J, Maltais F, Murcko M, Wang T, Wannamaker MW, Bennett HB, Leeman JR, McNeil C, Taylor WP, Memmott C, Jiang M, Rijnbrand R, Bral C, Germann U, Nezami A, Zhang Y, Salituro FG, Bennani YL, Charifson PS. Clark MP, et al. Among authors: bennani yl. J Med Chem. 2014 Aug 14;57(15):6668-78. doi: 10.1021/jm5007275. Epub 2014 Jul 24. J Med Chem. 2014. PMID: 25019388
Second-generation antibacterial benzimidazole ureas: discovery of a preclinical candidate with reduced metabolic liability.
Grillot AL, Le Tiran A, Shannon D, Krueger E, Liao Y, O'Dowd H, Tang Q, Ronkin S, Wang T, Waal N, Li P, Lauffer D, Sizensky E, Tanoury J, Perola E, Grossman TH, Doyle T, Hanzelka B, Jones S, Dixit V, Ewing N, Liao S, Boucher B, Jacobs M, Bennani Y, Charifson PS. Grillot AL, et al. J Med Chem. 2014 Nov 13;57(21):8792-816. doi: 10.1021/jm500563g. Epub 2014 Oct 28. J Med Chem. 2014. PMID: 25317480
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.
Boyd MJ, Bandarage UK, Bennett H, Byrn RR, Davies I, Gu W, Jacobs M, Ledeboer MW, Ledford B, Leeman JR, Perola E, Wang T, Bennani Y, Clark MP, Charifson PS. Boyd MJ, et al. Bioorg Med Chem Lett. 2015 May 1;25(9):1990-4. doi: 10.1016/j.bmcl.2015.03.013. Epub 2015 Mar 14. Bioorg Med Chem Lett. 2015. PMID: 25827523
Discovery of Novel, Orally Bioavailable β-Amino Acid Azaindole Inhibitors of Influenza PB2.
Farmer LJ, Clark MP, Boyd MJ, Perola E, Jones SM, Tsai A, Jacobs MD, Bandarage UK, Ledeboer MW, Wang T, Deng H, Ledford B, Gu W, Duffy JP, Bethiel RS, Shannon D, Byrn RA, Leeman JR, Rijnbrand R, Bennett HB, O'Brien C, Memmott C, Nti-Addae K, Bennani YL, Charifson PS. Farmer LJ, et al. Among authors: bennani yl. ACS Med Chem Lett. 2017 Jan 20;8(2):256-260. doi: 10.1021/acsmedchemlett.6b00486. eCollection 2017 Feb 9. ACS Med Chem Lett. 2017. PMID: 28197322 Free PMC article.
Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions.
Wang T, Bemis G, Hanzelka B, Zuccola H, Wynn M, Moody CS, Green J, Locher C, Liu A, Gao H, Xu Y, Wang S, Wang J, Bennani YL, Thomson JA, Müh U. Wang T, et al. Among authors: bennani yl. ACS Med Chem Lett. 2017 Nov 28;8(12):1224-1229. doi: 10.1021/acsmedchemlett.7b00239. eCollection 2017 Dec 14. ACS Med Chem Lett. 2017. PMID: 29259738 Free PMC article.
78 results