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Page 1
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds.
Shen DM, Shu M, Willoughby CA, Shah S, Lynch CL, Hale JJ, Mills SG, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Lyons K, Pivnichny JV, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA. Shen DM, et al. Among authors: lyons k. Bioorg Med Chem Lett. 2004 Feb 23;14(4):941-5. doi: 10.1016/j.bmcl.2003.12.005. Bioorg Med Chem Lett. 2004. PMID: 15012998
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.
Shu M, Loebach JL, Parker KA, Mills SG, Chapman KT, Shen DM, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Salvo JD, Lyons K, Pivnichny JV, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA. Shu M, et al. Among authors: lyons k. Bioorg Med Chem Lett. 2004 Feb 23;14(4):947-52. doi: 10.1016/j.bmcl.2003.12.006. Bioorg Med Chem Lett. 2004. PMID: 15012999
The discovery of sulfonylated dipeptides as potent VLA-4 antagonists.
Hagmann WK, Durette PL, Lanza T, Kevin NJ, de Laszlo SE, Kopka IE, Young D, Magriotis PA, Li B, Lin LS, Yang G, Kamenecka T, Chang LL, Wilson J, MacCoss M, Mills SG, Van Riper G, McCauley E, Egger LA, Kidambi U, Lyons K, Vincent S, Stearns R, Colletti A, Teffera J, Tong S, Fenyk-Melody J, Owens K, Levorse D, Kim P, Schmidt JA, Mumford RA. Hagmann WK, et al. Among authors: lyons k. Bioorg Med Chem Lett. 2001 Oct 22;11(20):2709-13. doi: 10.1016/s0960-894x(01)00544-3. Bioorg Med Chem Lett. 2001. PMID: 11591507
Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity.
Ashton WT, Sisco RM, Kieczykowski GR, Yang YT, Yudkovitz JB, Cui J, Mount GR, Ren RN, Wu TJ, Shen X, Lyons KA, Mao AH, Carlin JR, Karanam BV, Vincent SH, Cheng K, Goulet MT. Ashton WT, et al. Among authors: lyons ka. Bioorg Med Chem Lett. 2001 Oct 8;11(19):2597-602. doi: 10.1016/s0960-894x(01)00512-1. Bioorg Med Chem Lett. 2001. PMID: 11551758
Use of a small molecule CCR5 inhibitor in macaques to treat simian immunodeficiency virus infection or prevent simian-human immunodeficiency virus infection.
Veazey RS, Klasse PJ, Ketas TJ, Reeves JD, Piatak M Jr, Kunstman K, Kuhmann SE, Marx PA, Lifson JD, Dufour J, Mefford M, Pandrea I, Wolinsky SM, Doms RW, DeMartino JA, Siciliano SJ, Lyons K, Springer MS, Moore JP. Veazey RS, et al. Among authors: lyons k. J Exp Med. 2003 Nov 17;198(10):1551-62. doi: 10.1084/jem.20031266. J Exp Med. 2003. PMID: 14623909 Free PMC article.
CCR5 blockade modulates inflammation and alloimmunity in primates.
Schröder C, Pierson RN 3rd, Nguyen BN, Kawka DW, Peterson LB, Wu G, Zhang T, Springer MS, Siciliano SJ, Iliff S, Ayala JM, Lu M, Mudgett JS, Lyons K, Mills SG, Miller GG, Singer II, Azimzadeh AM, DeMartino JA. Schröder C, et al. Among authors: lyons k. J Immunol. 2007 Aug 15;179(4):2289-99. doi: 10.4049/jimmunol.179.4.2289. J Immunol. 2007. PMID: 17675490
Substituted biaryl pyrazoles as sodium channel blockers.
Tyagarajan S, Chakravarty PK, Zhou B, Taylor B, Fisher MH, Wyvratt MJ, Lyons K, Klatt T, Li X, Kumar S, Williams B, Felix J, Priest BT, Brochu RM, Warren V, Smith M, Garcia M, Kaczorowski GJ, Martin WJ, Abbadie C, McGowan E, Jochnowitz N, Parsons WH. Tyagarajan S, et al. Among authors: lyons k. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5480-3. doi: 10.1016/j.bmcl.2010.07.080. Epub 2010 Jul 24. Bioorg Med Chem Lett. 2010. PMID: 20709545
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin.
Biftu T, Scapin G, Singh S, Feng D, Becker JW, Eiermann G, He H, Lyons K, Patel S, Petrov A, Sinha-Roy R, Zhang B, Wu J, Zhang X, Doss GA, Thornberry NA, Weber AE. Biftu T, et al. Among authors: lyons k. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3384-7. doi: 10.1016/j.bmcl.2007.03.095. Epub 2007 Apr 2. Bioorg Med Chem Lett. 2007. PMID: 17433672
Bicyclo[2.2.2]octyltriazole inhibitors of 11β-hydoxysteroid dehydrogenase type 1. Pharmacological agents for the treatment of metabolic syndrome.
Maletic M, Leeman A, Szymonifka M, Mundt SS, Zokian HJ, Shah K, Dragovic J, Lyons K, Thieringer R, Vosatka AH, Balkovec J, Waddell ST. Maletic M, et al. Among authors: lyons k. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2568-72. doi: 10.1016/j.bmcl.2011.01.018. Epub 2011 Jan 11. Bioorg Med Chem Lett. 2011. PMID: 21421311
Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: Profile of clinical candidate (2R,3S,5R)-2- (2,5-difluorophenyl)-5-(4,6-dihydropyrrolo [3,4-c]pyrazol-5-(1H)-yl)tetrahydro-2H-pyran-3-amine (23) [corrected].
Biftu T, Qian X, Chen P, Feng D, Scapin G, Gao YD, Cox J, Roy RS, Eiermann G, He H, Lyons K, Salituro G, Patel S, Petrov A, Xu F, Xu SS, Zhang B, Caldwell C, Wu JK, Lyons K, Weber AE. Biftu T, et al. Among authors: lyons k. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5361-6. doi: 10.1016/j.bmcl.2013.07.061. Epub 2013 Aug 5. Bioorg Med Chem Lett. 2013. PMID: 23972441
1,246 results