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Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119.
Wacker DA, Wang Y, Broekema M, Rossi K, O'Connor S, Hong Z, Wu G, Malmstrom SE, Hung CP, LaMarre L, Chimalakonda A, Zhang L, Xin L, Cai H, Chu C, Boehm S, Zalaznick J, Ponticiello R, Sereda L, Han SP, Zebo R, Zinker B, Luk CE, Wong R, Everlof G, Li YX, Wu CK, Lee M, Griffen S, Miller KJ, Krupinski J, Robl JA. Wacker DA, et al. Among authors: miller kj. J Med Chem. 2014 Sep 25;57(18):7499-508. doi: 10.1021/jm501175v. Epub 2014 Sep 10. J Med Chem. 2014. PMID: 25208139
Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT(2C) receptor.
Wacker DA, Varnes JG, Malmstrom SE, Cao X, Hung CP, Ung T, Wu G, Zhang G, Zuvich E, Thomas MA, Keim WJ, Cullen MJ, Rohrbach KW, Qu Q, Narayanan R, Rossi K, Janovitz E, Lehman-McKeeman L, Malley MF, Devenny J, Pelleymounter MA, Miller KJ, Robl JA. Wacker DA, et al. Among authors: miller kj. J Med Chem. 2007 Mar 22;50(6):1365-79. doi: 10.1021/jm0612968. Epub 2007 Feb 23. J Med Chem. 2007. PMID: 17315987
Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT2C Receptor Agonists.
Carpenter J, Wang Y, Wu G, Feng J, Ye XY, Morales CL, Broekema M, Rossi KA, Miller KJ, Murphy BJ, Wu G, Malmstrom SE, Azzara AV, Sher PM, Fevig JM, Alt A, Bertekap RL Jr, Cullen MJ, Harper TM, Foster K, Luk E, Xiang Q, Grubb MF, Robl JA, Wacker DA. Carpenter J, et al. Among authors: miller kj. J Med Chem. 2017 Jul 27;60(14):6166-6190. doi: 10.1021/acs.jmedchem.7b00385. Epub 2017 Jul 7. J Med Chem. 2017. PMID: 28635286
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.
Ahmad S, Ngu K, Miller KJ, Wu G, Hung CP, Malmstrom S, Zhang G, O'Tanyi E, Keim WJ, Cullen MJ, Rohrbach KW, Thomas M, Ung T, Qu Q, Gan J, Narayanan R, Pelleymounter MA, Robl JA. Ahmad S, et al. Among authors: miller kj. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1128-33. doi: 10.1016/j.bmcl.2009.12.014. Epub 2009 Dec 6. Bioorg Med Chem Lett. 2010. PMID: 20022752
Synthesis and SAR of potent and selective tetrahydropyrazinoisoquinolinone 5-HT(2C) receptor agonists.
Zhao G, Kwon C, Bisaha SN, Stein PD, Rossi KA, Cao X, Ung T, Wu G, Hung CP, Malmstrom SE, Zhang G, Qu Q, Gan J, Keim WJ, Cullen MJ, Rohrbach KW, Devenny J, Pelleymounter MA, Miller KJ, Robl JA. Zhao G, et al. Among authors: miller kj. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3914-9. doi: 10.1016/j.bmcl.2013.04.061. Epub 2013 Apr 29. Bioorg Med Chem Lett. 2013. PMID: 23683593
Position 5.46 of the serotonin 5-HT2A receptor contributes to a species-dependent variation for the 5-HT2C agonist (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol-6(2H)-one: impact on selectivity and toxicological evaluation.
Miller KJ, Wu GY, Varnes JG, Levesque P, Li J, Li D, Robl JA, Rossi KA, Wacker DA. Miller KJ, et al. Mol Pharmacol. 2009 Dec;76(6):1211-9. doi: 10.1124/mol.109.059204. Epub 2009 Sep 18. Mol Pharmacol. 2009. PMID: 19767451
485 results