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Page 1
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: rossi ka. 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
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. J Med Chem. 2007 Mar 22;50(6):1365-79. doi: 10.1021/jm0612968. Epub 2007 Feb 23. J Med Chem. 2007. PMID: 17315987
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. J Med Chem. 2014 Sep 25;57(18):7499-508. doi: 10.1021/jm501175v. Epub 2014 Sep 10. J Med Chem. 2014. PMID: 25208139
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: rossi ka. 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
Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants.
Lam PY, Clark CG, Li R, Pinto DJ, Orwat MJ, Galemmo RA, Fevig JM, Teleha CA, Alexander RS, Smallwood AM, Rossi KA, Wright MR, Bai SA, He K, Luettgen JM, Wong PC, Knabb RM, Wexler RR. Lam PY, et al. Among authors: rossi ka. J Med Chem. 2003 Oct 9;46(21):4405-18. doi: 10.1021/jm020578e. J Med Chem. 2003. PMID: 14521405
Preparation of 1-(3-aminobenzo[d]isoxazol-5-yl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa.
Li YL, Fevig JM, Cacciola J, Buriak J Jr, Rossi KA, Jona J, Knabb RM, Luettgen JM, Wong PC, Bai SA, Wexler RR, Lam PY. Li YL, et al. Among authors: rossi ka. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5176-82. doi: 10.1016/j.bmcl.2006.07.002. Epub 2006 Jul 25. Bioorg Med Chem Lett. 2006. PMID: 16870435
58 results