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Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
Robinson RP, Bartlett JA, Bertinato P, Bessire AJ, Cosgrove J, Foley PM, Manion TB, Minich ML, Ramos B, Reese MR, Schmahai TJ, Swick AG, Tess DA, Vaz A, Wolford A. Robinson RP, et al. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4150-4. doi: 10.1016/j.bmcl.2011.05.099. Epub 2011 Jun 2. Bioorg Med Chem Lett. 2011. PMID: 21684740
C-Aryl glycoside inhibitors of SGLT2: Exploration of sugar modifications including C-5 spirocyclization.
Robinson RP, Mascitti V, Boustany-Kari CM, Carr CL, Foley PM, Kimoto E, Leininger MT, Lowe A, Klenotic MK, Macdonald JI, Maguire RJ, Masterson VM, Maurer TS, Miao Z, Patel JD, Préville C, Reese MR, She L, Steppan CM, Thuma BA, Zhu T. Robinson RP, et al. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1569-72. doi: 10.1016/j.bmcl.2010.01.075. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20149653
Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119.
Darout E, Robinson RP, McClure KF, Corbett M, Li B, Shavnya A, Andrews MP, Jones CS, Li Q, Minich ML, Mascitti V, Guimarães CR, Munchhof MJ, Bahnck KB, Cai C, Price DA, Liras S, Bonin PD, Cornelius P, Wang R, Bagdasarian V, Sobota CP, Hornby S, Masterson VM, Joseph RM, Kalgutkar AS, Chen Y. Darout E, et al. Among authors: robinson rp. J Med Chem. 2013 Jan 10;56(1):301-19. doi: 10.1021/jm301626p. Epub 2012 Dec 31. J Med Chem. 2013. PMID: 23234271
Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1.
Reiter LA, Robinson RP, McClure KF, Jones CS, Reese MR, Mitchell PG, Otterness IG, Bliven ML, Liras J, Cortina SR, Donahue KM, Eskra JD, Griffiths RJ, Lame ME, Lopez-Anaya A, Martinelli GJ, McGahee SM, Yocum SA, Lopresti-Morrow LL, Tobiassen LM, Vaughn-Bowser ML. Reiter LA, et al. Among authors: robinson rp. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3389-95. doi: 10.1016/j.bmcl.2004.04.083. Bioorg Med Chem Lett. 2004. PMID: 15177439
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
Mascitti V, Maurer TS, Robinson RP, Bian J, Boustany-Kari CM, Brandt T, Collman BM, Kalgutkar AS, Klenotic MK, Leininger MT, Lowe A, Maguire RJ, Masterson VM, Miao Z, Mukaiyama E, Patel JD, Pettersen JC, Préville C, Samas B, She L, Sobol Z, Steppan CM, Stevens BD, Thuma BA, Tugnait M, Zeng D, Zhu T. Mascitti V, et al. Among authors: robinson rp. J Med Chem. 2011 Apr 28;54(8):2952-60. doi: 10.1021/jm200049r. Epub 2011 Mar 30. J Med Chem. 2011. PMID: 21449606
Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14.
Blagg JA, Noe MC, Wolf-Gouveia LA, Reiter LA, Laird ER, Chang SP, Danley DE, Downs JT, Elliott NC, Eskra JD, Griffiths RJ, Hardink JR, Haugeto AI, Jones CS, Liras JL, Lopresti-Morrow LL, Mitchell PG, Pandit J, Robinson RP, Subramanyam C, Vaughn-Bowser ML, Yocum SA. Blagg JA, et al. Among authors: robinson rp. Bioorg Med Chem Lett. 2005 Apr 1;15(7):1807-10. doi: 10.1016/j.bmcl.2005.02.038. Bioorg Med Chem Lett. 2005. PMID: 15780611
From partial to full agonism: identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor.
Futatsugi K, Mascitti V, Guimarães CR, Morishita N, Cai C, DeNinno MP, Gao H, Hamilton MD, Hank R, Harris AR, Kung DW, Lavergne SY, Lefker BA, Lopaze MG, McClure KF, Munchhof MJ, Preville C, Robinson RP, Wright SW, Bonin PD, Cornelius P, Chen Y, Kalgutkar AS. Futatsugi K, et al. Among authors: robinson rp. Bioorg Med Chem Lett. 2013 Jan 1;23(1):194-7. doi: 10.1016/j.bmcl.2012.10.119. Epub 2012 Nov 5. Bioorg Med Chem Lett. 2013. PMID: 23177788
70 results