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Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine.
Horne DB, Biswas K, Brown J, Bartberger MD, Clarine J, Davis CD, Gore VK, Harried S, Horner M, Kaller MR, Lehto SG, Liu Q, Ma VV, Monenschein H, Nguyen TT, Yuan CC, Youngblood BD, Zhang M, Zhong W, Allen JR, Chen JJ, Gavva NR. Horne DB, et al. Among authors: yuan cc. J Med Chem. 2018 Sep 27;61(18):8186-8201. doi: 10.1021/acs.jmedchem.8b00518. Epub 2018 Sep 10. J Med Chem. 2018. PMID: 30148953
Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer's disease.
Chen JJ, Liu Q, Yuan C, Gore V, Lopez P, Ma V, Amegadzie A, Qian W, Judd TC, Minatti AE, Brown J, Cheng Y, Xue M, Zhong W, Dineen TA, Epstein O, Human J, Kreiman C, Marx I, Weiss MM, Hitchcock SA, Powers TS, Chen K, Wen PH, Whittington DA, Cheng AC, Bartberger MD, Hickman D, Werner JA, Vargas HM, Everds NE, Vonderfecht SL, Dunn RT 2nd, Wood S, Fremeau RT Jr, White RD, Patel VF. Chen JJ, et al. Bioorg Med Chem Lett. 2015 Feb 15;25(4):767-74. doi: 10.1016/j.bmcl.2014.12.092. Epub 2015 Jan 8. Bioorg Med Chem Lett. 2015. PMID: 25613679
Discovery of 2-methylpyridine-based biaryl amides as γ-secretase modulators for the treatment of Alzheimer's disease.
Chen JJ, Qian W, Biswas K, Yuan C, Amegadzie A, Liu Q, Nixey T, Zhu J, Ncube M, Rzasa RM, Chavez F Jr, Chen N, DeMorin F, Rumfelt S, Tegley CM, Allen JR, Hitchcock S, Hungate R, Bartberger MD, Zalameda L, Liu Y, McCarter JD, Zhang J, Zhu L, Babu-Khan S, Luo Y, Bradley J, Wen PH, Reid DL, Koegler F, Dean C Jr, Hickman D, Correll TL, Williamson T, Wood S. Chen JJ, et al. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6447-54. doi: 10.1016/j.bmcl.2013.09.041. Epub 2013 Sep 29. Bioorg Med Chem Lett. 2013. PMID: 24139583
Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides.
Biswas K, Li A, Chen JJ, D'Amico DC, Fotsch C, Han N, Human J, Liu Q, Norman MH, Riahi B, Yuan C, Suzuki H, Mareska DA, Zhan J, Clarke DE, Toro A, Groneberg RD, Burgess LE, Lester-Zeiner D, Biddlecome G, Manning BH, Arik L, Dong H, Huang M, Kamassah A, Loeloff R, Sun H, Hsieh FY, Kumar G, Ng GY, Hungate RW, Askew BC, Johnson E. Biswas K, et al. J Med Chem. 2007 May 3;50(9):2200-12. doi: 10.1021/jm070055c. Epub 2007 Apr 5. J Med Chem. 2007. PMID: 17408249
The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors.
Yuan C, St Jean DJ Jr, Liu Q, Cai L, Li A, Han N, Moniz G, Askew B, Hungate RW, Johansson L, Tedenborg L, Pyring D, Williams M, Hale C, Chen M, Cupples R, Zhang J, Jordan S, Bartberger MD, Sun Y, Emery M, Wang M, Fotsch C. Yuan C, et al. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6056-61. doi: 10.1016/j.bmcl.2007.09.070. Epub 2007 Sep 25. Bioorg Med Chem Lett. 2007. PMID: 17919905
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
Fotsch C, Bartberger MD, Bercot EA, Chen M, Cupples R, Emery M, Fretland J, Guram A, Hale C, Han N, Hickman D, Hungate RW, Hayashi M, Komorowski R, Liu Q, Matsumoto G, St Jean DJ Jr, Ursu S, Véniant M, Xu G, Ye Q, Yuan C, Zhang J, Zhang X, Tu H, Wang M. Fotsch C, et al. J Med Chem. 2008 Dec 25;51(24):7953-67. doi: 10.1021/jm801073z. J Med Chem. 2008. PMID: 19053753
Azole-based inhibitors of AKT/PKB for the treatment of cancer.
Zeng Q, Allen JG, Bourbeau MP, Wang X, Yao G, Tadesse S, Rider JT, Yuan CC, Hong FT, Lee MR, Zhang S, Lofgren JA, Freeman DJ, Yang S, Li C, Tominey E, Huang X, Hoffman D, Yamane HK, Fotsch C, Dominguez C, Hungate R, Zhang X. Zeng Q, et al. Among authors: yuan cc. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1559-64. doi: 10.1016/j.bmcl.2010.01.067. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20137943
305 results