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Page 1
Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes.
Qian Y, Wertheimer SJ, Ahmad M, Cheung AW, Firooznia F, Hamilton MM, Hayden S, Li S, Marcopulos N, McDermott L, Tan J, Yun W, Guo L, Pamidimukkala A, Chen Y, Huang KS, Ramsey GB, Whittard T, Conde-Knape K, Taub R, Rondinone CM, Tilley J, Bolin D. Qian Y, et al. Among authors: tilley j. J Med Chem. 2011 Apr 14;54(7):2433-46. doi: 10.1021/jm101580m. Epub 2011 Mar 17. J Med Chem. 2011. PMID: 21413799
Potent, selective MCH-1 receptor antagonists.
Erickson SD, Banner B, Berthel S, Conde-Knape K, Falcioni F, Hakimi I, Hennessy B, Kester RF, Kim K, Ma C, McComas W, Mennona F, Mischke S, Orzechowski L, Qian Y, Salari H, Tengi J, Thakkar K, Taub R, Tilley JW, Wang H. Erickson SD, et al. Among authors: tilley jw. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1402-6. doi: 10.1016/j.bmcl.2008.01.010. Epub 2008 Jan 8. Bioorg Med Chem Lett. 2008. PMID: 18243691
Identification of N-acyl 4-(5-pyrimidine-2,4-dionyl)phenylalanine derivatives and their orally active prodrug esters as dual-acting alpha4-beta1 and alpha4-beta7 receptor antagonists.
Sidduri A, Tilley JW, Lou J, Tare N, Cavallo G, Frank K, Pamidimukkala A, Choi DS, Gerber L, Railkar A, Renzetti L. Sidduri A, et al. Among authors: tilley jw. Bioorg Med Chem Lett. 2013 Feb 15;23(4):1026-31. doi: 10.1016/j.bmcl.2012.12.026. Epub 2012 Dec 20. Bioorg Med Chem Lett. 2013. PMID: 23312474
Discovery of camphor-derived pyrazolones as 11β-hydroxysteroid dehydrogenase type 1 inhibitors.
Gillespie P, Pietranico-Cole S, Myers M, Bilotta JA, Conde-Knape K, Fotouhi N, Goodnow RA Jr, Guertin KR, Hamilton MM, Haynes NE, Liu B, Qi L, Ren Y, Scott NR, So SS, Spence C, Taub R, Thakkar K, Tilley JW, Zwingelstein C. Gillespie P, et al. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2707-11. doi: 10.1016/j.bmcl.2014.04.049. Epub 2014 Apr 21. Bioorg Med Chem Lett. 2014. PMID: 24815509
Discovery of novel and potent leukotriene B4 receptor antagonists. Part 1.
Goodnow RA Jr, Hicks A, Sidduri A, Kowalczyk A, Dominique R, Qiao Q, Lou JP, Gillespie P, Fotouhi N, Tilley J, Cohen N, Choudhry S, Cavallo G, Tannu SA, Ventre JD, Lavelle D, Tare NS, Oh H, Lamb M, Kurylko G, Hamid R, Wright MB, Pamidimukkala A, Egan T, Gubler U, Hoffman AF, Wei X, Li YL, O'Neil J, Marcano R, Pozzani K, Molinaro T, Santiago J, Singer L, Hargaden M, Moore D, Catala AR, Chao LC, Hermann G, Venkat R, Mancebo H, Renzetti LM. Goodnow RA Jr, et al. Among authors: tilley j. J Med Chem. 2010 May 13;53(9):3502-16. doi: 10.1021/jm1001919. J Med Chem. 2010. PMID: 20380377
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dyslipidemia.
Kelly MJ, Pietranico-Cole S, Larigan JD, Haynes NE, Reynolds CH, Scott N, Vermeulen J, Dvorozniak M, Conde-Knape K, Huang KS, So SS, Thakkar K, Qian Y, Banner B, Mennona F, Danzi S, Klein I, Taub R, Tilley J. Kelly MJ, et al. Among authors: tilley j. J Med Chem. 2014 May 22;57(10):3912-23. doi: 10.1021/jm4019299. Epub 2014 Apr 8. J Med Chem. 2014. PMID: 24712661
144 results