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Page 1
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. Among authors: hungate rw. J Med Chem. 2008 Dec 25;51(24):7953-67. doi: 10.1021/jm801073z. J Med Chem. 2008. PMID: 19053753
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
Véniant MM, Hale C, Hungate RW, Gahm K, Emery MG, Jona J, Joseph S, Adams J, Hague A, Moniz G, Zhang J, Bartberger MD, Li V, Syed R, Jordan S, Komorowski R, Chen MM, Cupples R, Kim KW, St Jean DJ Jr, Johansson L, Henriksson MA, Williams M, Vallgårda J, Fotsch C, Wang M. Véniant MM, et al. Among authors: hungate rw. J Med Chem. 2010 Jun 10;53(11):4481-7. doi: 10.1021/jm100242d. J Med Chem. 2010. PMID: 20465278
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. Among authors: hungate rw. 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. Among authors: hungate rw. 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
Identification of a nonpeptidic and conformationally restricted bradykinin B1 receptor antagonist with anti-inflammatory activity.
D'Amico DC, Aya T, Human J, Fotsch C, Chen JJ, Biswas K, Riahi B, Norman MH, Willoughby CA, Hungate R, Reider PJ, Biddlecome G, Lester-Zeiner D, Staden CV, Johnson E, Kamassah A, Arik L, Wang J, Viswanadhan VN, Groneberg RD, Zhan J, Suzuki H, Toro A, Mareska DA, Clarke DE, Harvey DM, Burgess LE, Laird ER, Askew B, Ng G. D'Amico DC, et al. J Med Chem. 2007 Feb 22;50(4):607-10. doi: 10.1021/jm061224g. Epub 2007 Jan 23. J Med Chem. 2007. PMID: 17243660
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. 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
3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation.
Chen JJ, Nguyen T, D'Amico DC, Qian W, Human J, Aya T, Biswas K, Fotsch C, Han N, Liu Q, Nishimura N, Peterkin TA, Yang K, Zhu J, Riahi BB, Hungate RW, Andersen NG, Colyer JT, Faul MM, Kamassah A, Wang J, Jona J, Kumar G, Johnson E, Askew BC. Chen JJ, et al. Among authors: hungate rw. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3384-9. doi: 10.1016/j.bmcl.2011.03.115. Epub 2011 Apr 7. Bioorg Med Chem Lett. 2011. PMID: 21514825
57 results