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(3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1h-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic acid (BMS-644950): a rationally designed orally efficacious 3-hydroxy-3-methylglutaryl coenzyme-a reductase inhibitor with reduced myotoxicity potential.
Ahmad S, Madsen CS, Stein PD, Janovitz E, Huang C, Ngu K, Bisaha S, Kennedy LJ, Chen BC, Zhao R, Sitkoff D, Monshizadegan H, Yin X, Ryan CS, Zhang R, Giancarli M, Bird E, Chang M, Chen X, Setters R, Search D, Zhuang S, Nguyen-Tran V, Cuff CA, Harrity T, Darienzo CJ, Li T, Reeves RA, Blanar MA, Barrish JC, Zahler R, Robl JA. Ahmad S, et al. Among authors: huang c. J Med Chem. 2008 May 8;51(9):2722-33. doi: 10.1021/jm800001n. Epub 2008 Apr 15. J Med Chem. 2008. PMID: 18412317
Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor.
Ahmad S, Washburn WN, Hernandez AS, Bisaha S, Ngu K, Wang W, Pelleymounter MA, Longhi D, Flynn N, Azzara AV, Rohrbach K, Devenny J, Rooney S, Thomas M, Glick S, Godonis H, Harvey S, Zhang H, Gemzik B, Janovitz EB, Huang C, Zhang L, Robl JA, Murphy BJ. Ahmad S, et al. Among authors: huang c. J Med Chem. 2016 Oct 13;59(19):8848-8858. doi: 10.1021/acs.jmedchem.6b00676. Epub 2016 Sep 15. J Med Chem. 2016. PMID: 27564419
The Guinea pig as a preclinical model for demonstrating the efficacy and safety of statins.
Madsen CS, Janovitz E, Zhang R, Nguyen-Tran V, Ryan CS, Yin X, Monshizadegan H, Chang M, D'Arienzo C, Scheer S, Setters R, Search D, Chen X, Zhuang S, Kunselman L, Peters A, Harrity T, Apedo A, Huang C, Cuff CA, Kowala MC, Blanar MA, Sun CQ, Robl JA, Stein PD. Madsen CS, et al. Among authors: huang c. J Pharmacol Exp Ther. 2008 Feb;324(2):576-86. doi: 10.1124/jpet.107.131615. Epub 2007 Nov 6. J Pharmacol Exp Ther. 2008. PMID: 17986646
Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors.
Harikrishnan LS, Finlay HJ, Qiao JX, Kamau MG, Jiang J, Wang TC, Li J, Cooper CB, Poss MA, Adam LP, Taylor DS, Chen AY, Yin X, Sleph PG, Yang RZ, Sitkoff DF, Galella MA, Nirschl DS, Van Kirk K, Miller AV, Huang CS, Chang M, Chen XQ, Salvati ME, Wexler RR, Lawrence RM. Harikrishnan LS, et al. Among authors: huang cs. J Med Chem. 2012 Jul 12;55(13):6162-75. doi: 10.1021/jm300611v. Epub 2012 Jun 22. J Med Chem. 2012. PMID: 22650305
Triphenylethanamine Derivatives as Cholesteryl Ester Transfer Protein Inhibitors: Discovery of N-[(1R)-1-(3-Cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide (BMS-795311).
Qiao JX, Wang TC, Adam LP, Chen AY, Taylor DS, Yang RZ, Zhuang S, Sleph PG, Li JP, Li D, Yin X, Chang M, Chen XQ, Shen H, Li J, Smith D, Wu DR, Leith L, Harikrishnan LS, Kamau MG, Miller MM, Bilder D, Rampulla R, Li YX, Xu C, Lawrence RM, Poss MA, Levesque P, Gordon DA, Huang CS, Finlay HJ, Wexler RR, Salvati ME. Qiao JX, et al. Among authors: huang cs. J Med Chem. 2015 Nov 25;58(22):9010-26. doi: 10.1021/acs.jmedchem.5b01363. Epub 2015 Nov 17. J Med Chem. 2015. PMID: 26524347
Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577.
Shi Y, Li C, O'Connor SP, Zhang J, Shi M, Bisaha SN, Wang Y, Sitkoff D, Pudzianowski AT, Huang C, Klei HE, Kish K, Yanchunas J Jr, Liu EC, Hartl KS, Seiler SM, Steinbacher TE, Schumacher WA, Atwal KS, Stein PD. Shi Y, et al. Among authors: huang c. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9. doi: 10.1016/j.bmcl.2009.10.084. Epub 2009 Oct 23. Bioorg Med Chem Lett. 2009. PMID: 19896847
Discovery of ((S)-5-(methoxymethyl)-7-(1-methyl-1H-indol-2-yl)-2-(trifluoromethyl)-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl)((S)-2-(3-methylisoxazol-5-yl)pyrrolidin-1-yl)methanone as a potent and selective I(Kur) inhibitor.
Finlay HJ, Lloyd J, Vaccaro W, Kover A, Yan L, Bhave G, Prol J, Huynh T, Bhandaru R, Caringal Y, DiMarco J, Gan J, Harper T, Huang C, Conder ML, Sun H, Levesque P, Blanar M, Atwal K, Wexler R. Finlay HJ, et al. Among authors: huang c. J Med Chem. 2012 Apr 12;55(7):3036-48. doi: 10.1021/jm201386u. Epub 2012 Mar 21. J Med Chem. 2012. PMID: 22409629
Identification of a nonbasic melanin hormone receptor 1 antagonist as an antiobesity clinical candidate.
Washburn WN, Manfredi M, Devasthale P, Zhao G, Ahmad S, Hernandez A, Robl JA, Wang W, Mignone J, Wang Z, Ngu K, Pelleymounter MA, Longhi D, Zhao R, Wang B, Huang N, Flynn N, Azzara AV, Barrish JC, Rohrbach K, Devenny JJ, Rooney S, Thomas M, Glick S, Godonis HE, Harvey SJ, Cullen MJ, Zhang H, Caporuscio C, Stetsko P, Grubb M, Maxwell BD, Yang H, Apedo A, Gemzik B, Janovitz EB, Huang C, Zhang L, Freeden C, Murphy BJ. Washburn WN, et al. Among authors: huang n, huang c. J Med Chem. 2014 Sep 25;57(18):7509-22. doi: 10.1021/jm500026w. Epub 2014 Sep 9. J Med Chem. 2014. PMID: 25165888
Design, structure-activity relationships, X-ray crystal structure, and energetic contributions of a critical P1 pharmacophore: 3-chloroindole-7-yl-based factor Xa inhibitors.
Shi Y, Sitkoff D, Zhang J, Klei HE, Kish K, Liu EC, Hartl KS, Seiler SM, Chang M, Huang C, Youssef S, Steinbacher TE, Schumacher WA, Grazier N, Pudzianowski A, Apedo A, Discenza L, Yanchunas J, Stein PD, Atwal KS. Shi Y, et al. Among authors: huang c. J Med Chem. 2008 Dec 11;51(23):7541-51. doi: 10.1021/jm800855x. J Med Chem. 2008. PMID: 18998662
Non-basic azolotriazinone MCHR1 antagonists for the treatment of obesity: An empirical brain-exposures-driven candidate selection for in vivo efficacy studies.
Devasthale P, Wang W, Mignone J, Renduchintala K, Radhakrishnan S, Dhanapal J, Selvaraj J, Kuppusamy R, Pelleymounter MA, Longhi D, Huang N, Flynn N, Azzara AV, Rohrbach K, Devenny J, Rooney S, Thomas M, Glick S, Godonis H, Harvey S, Cullen MJ, Zhang H, Caporuscio C, Stetsko P, Grubb M, Huang C, Zhang L, Freeden C, Murphy BJ, Robl JA, Washburn WN. Devasthale P, et al. Among authors: huang n, huang c. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4412-8. doi: 10.1016/j.bmcl.2015.09.018. Epub 2015 Sep 8. Bioorg Med Chem Lett. 2015. PMID: 26386604
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