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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. 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. 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
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: conde knape k. J Med Chem. 2014 May 22;57(10):3912-23. doi: 10.1021/jm4019299. Epub 2014 Apr 8. J Med Chem. 2014. PMID: 24712661
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. Among authors: conde knape k. 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 pyrazolo[3,4-d]pyrimidine derivatives as GPR119 agonists.
Gillespie P, Goodnow RA Jr, Saha G, Bose G, Moulik K, Zwingelstein C, Myers M, Conde-Knape K, Pietranico-Cole S, So SS. Gillespie P, et al. Among authors: conde knape k. Bioorg Med Chem Lett. 2014 Feb 1;24(3):949-53. doi: 10.1016/j.bmcl.2013.12.063. Epub 2013 Dec 24. Bioorg Med Chem Lett. 2014. PMID: 24412066
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