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Page 1
Discovery of Insulin Receptor Partial Agonists MK-5160 and MK-1092 as Novel Basal Insulins with Potential to Improve Therapeutic Index.
Pissarnitski DA, Kekec A, Yan L, Zhu Y, Feng DD, Huo P, Madsen-Duggan C, Moyes CR, Nargund RP, Kelly T, Zhang X, Carballo-Jane E, Gorski J, Zafian P, Qatanani M, Kaarsholm N, Meng F, Jia X, Lee KJ, Wang W, Xu S, Hohn MJ, Iammarino MJ, McCoy MA, Okoh GA, Liang Y, Hollingsworth SA, Erion MD, Kelley DE, Garbaccio RM, Zhang A, Mu J, Lin S. Pissarnitski DA, et al. Among authors: garbaccio rm. J Med Chem. 2022 Apr 14;65(7):5593-5605. doi: 10.1021/acs.jmedchem.1c02073. Epub 2022 Mar 17. J Med Chem. 2022. PMID: 35298158
Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer.
Cox CD, Coleman PJ, Breslin MJ, Whitman DB, Garbaccio RM, Fraley ME, Buser CA, Walsh ES, Hamilton K, Schaber MD, Lobell RB, Tao W, Davide JP, Diehl RE, Abrams MT, South VJ, Huber HE, Torrent M, Prueksaritanont T, Li C, Slaughter DE, Mahan E, Fernandez-Metzler C, Yan Y, Kuo LC, Kohl NE, Hartman GD. Cox CD, et al. Among authors: garbaccio rm. J Med Chem. 2008 Jul 24;51(14):4239-52. doi: 10.1021/jm800386y. Epub 2008 Jun 25. J Med Chem. 2008. PMID: 18578472
Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase.
Converso A, Hartingh T, Fraley ME, Garbaccio RM, Hartman GD, Huang SY, Majercak JM, McCampbell A, Na SJ, Ray WJ, Savage MJ, Wolffe C, Yeh S, Yu Y, White R, Zhang R. Converso A, et al. Among authors: garbaccio rm. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2737-40. doi: 10.1016/j.bmcl.2014.04.034. Epub 2014 Apr 18. Bioorg Med Chem Lett. 2014. PMID: 24813734
Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis.
Layton ME, Reif AJ, Hartingh TJ, Rodzinak K, Dudkin V, Wang C, Arrington K, Kelly MJ 3rd, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Jacobson MA. Layton ME, et al. Among authors: garbaccio rm. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1260-4. doi: 10.1016/j.bmcl.2016.01.021. Epub 2016 Jan 11. Bioorg Med Chem Lett. 2016. PMID: 26810316
Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI.
Pero JE, Rossi MA, Kelly MJ 3rd, Lehman HD, Layton ME, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Joyce LA, Sherer EC, Jacobson MA. Pero JE, et al. Among authors: garbaccio rm. ACS Med Chem Lett. 2016 Jan 10;7(3):312-7. doi: 10.1021/acsmedchemlett.5b00459. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985321 Free PMC article.
Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.
Garbaccio RM, Fraley ME, Tasber ES, Olson CM, Hoffman WF, Arrington KL, Torrent M, Buser CA, Walsh ES, Hamilton K, Schaber MD, Fernandes C, Lobell RB, Tao W, South VJ, Yan Y, Kuo LC, Prueksaritanont T, Slaughter DE, Shu C, Heimbrook DC, Kohl NE, Huber HE, Hartman GD. Garbaccio RM, et al. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1780-3. doi: 10.1016/j.bmcl.2005.12.094. Epub 2006 Jan 24. Bioorg Med Chem Lett. 2006. PMID: 16439122
Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP.
Garbaccio RM, Tasber ES, Neilson LA, Coleman PJ, Fraley ME, Olson C, Bergman J, Torrent M, Buser CA, Rickert K, Walsh ES, Hamilton K, Lobell RB, Tao W, South VJ, Diehl RE, Davide JP, Yan Y, Kuo LC, Li C, Prueksaritanont T, Fernandez-Metzler C, Mahan EA, Slaughter DE, Salata JJ, Kohl NE, Huber HE, Hartman GD. Garbaccio RM, et al. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5671-6. doi: 10.1016/j.bmcl.2007.07.067. Epub 2007 Aug 21. Bioorg Med Chem Lett. 2007. PMID: 17804233
Development of thioquinazolinones, allosteric Chk1 kinase inhibitors.
Converso A, Hartingh T, Garbaccio RM, Tasber E, Rickert K, Fraley ME, Yan Y, Kreatsoulas C, Stirdivant S, Drakas B, Walsh ES, Hamilton K, Buser CA, Mao X, Abrams MT, Beck SC, Tao W, Lobell R, Sepp-Lorenzino L, Zugay-Murphy J, Sardana V, Munshi SK, Jezequel-Sur SM, Zuck PD, Hartman GD. Converso A, et al. Among authors: garbaccio rm. Bioorg Med Chem Lett. 2009 Feb 15;19(4):1240-4. doi: 10.1016/j.bmcl.2008.12.076. Epub 2008 Dec 24. Bioorg Med Chem Lett. 2009. PMID: 19155174
Preface.
Garbaccio RM, Johnson DS, Hong J, Disney MD. Garbaccio RM, et al. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4714. doi: 10.1016/j.bmcl.2015.08.083. Epub 2015 Sep 1. Bioorg Med Chem Lett. 2015. PMID: 26358161 No abstract available.
42 results