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99 results

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Page 1
Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.
Shen HC, Ding FX, Raghavan S, Deng Q, Luell S, Forrest MJ, Carballo-Jane E, Wilsie LC, Krsmanovic ML, Taggart AK, Wu KK, Wu TJ, Cheng K, Ren N, Cai TQ, Chen Q, Wang J, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. Among authors: hammond ml. J Med Chem. 2010 Mar 25;53(6):2666-70. doi: 10.1021/jm100022r. J Med Chem. 2010. PMID: 20184326
(1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (MK-1903): a potent GPR109a agonist that lowers free fatty acids in humans.
Boatman PD, Lauring B, Schrader TO, Kasem M, Johnson BR, Skinner P, Jung JK, Xu J, Cherrier MC, Webb PJ, Semple G, Sage CR, Knudsen J, Chen R, Luo WL, Caro L, Cote J, Lai E, Wagner J, Taggart AK, Carballo-Jane E, Hammond M, Colletti SL, Tata JR, Connolly DT, Waters MG, Richman JG. Boatman PD, et al. J Med Chem. 2012 Apr 26;55(8):3644-66. doi: 10.1021/jm2010964. Epub 2012 Apr 9. J Med Chem. 2012. PMID: 22435740 Clinical Trial.
Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.
Shen HC, Ding FX, Luell S, Forrest MJ, Carballo-Jane E, Wu KK, Wu TJ, Cheng K, Wilsie LC, Krsmanovic ML, Taggart AK, Ren N, Cai TQ, Deng Q, Chen Q, Wang J, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. Among authors: hammond ml. J Med Chem. 2007 Dec 13;50(25):6303-6. doi: 10.1021/jm700942d. Epub 2007 Nov 10. J Med Chem. 2007. PMID: 17994679
Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.
Shen HC, Szymonifka MJ, Kharbanda D, Deng Q, Carballo-Jane E, Wu KK, Wu TJ, Cheng K, Ren N, Cai TQ, Taggart AK, Wang J, Tong X, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. Among authors: hammond ml. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6723-8. doi: 10.1016/j.bmcl.2007.10.055. Epub 2007 Oct 18. Bioorg Med Chem Lett. 2007. PMID: 18029181
Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists.
Raghavan S, Tria GS, Shen HC, Ding FX, Taggart AK, Ren N, Wilsie LC, Krsmanovic ML, Holt TG, Wolff MS, Waters MG, Hammond ML, Tata JR, Colletti SL. Raghavan S, et al. Among authors: hammond ml. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3163-7. doi: 10.1016/j.bmcl.2008.04.071. Epub 2008 May 1. Bioorg Med Chem Lett. 2008. PMID: 18477506
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.
Shen HC, Ding FX, Deng Q, Wilsie LC, Krsmanovic ML, Taggart AK, Carballo-Jane E, Ren N, Cai TQ, Wu TJ, Wu KK, Cheng K, Chen Q, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. Among authors: hammond ml. J Med Chem. 2009 Apr 23;52(8):2587-602. doi: 10.1021/jm900151e. J Med Chem. 2009. PMID: 19309152
Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.
Ding FX, Shen HC, Wilsie LC, Krsmanovic ML, Taggart AK, Ren N, Cai TQ, Wang J, Tong X, Holt TG, Chen Q, Waters MG, Hammond ML, Tata JR, Colletti SL. Ding FX, et al. Among authors: hammond ml. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3372-5. doi: 10.1016/j.bmcl.2010.04.013. Epub 2010 Apr 11. Bioorg Med Chem Lett. 2010. PMID: 20452209
Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity.
Ali A, Thompson CF, Balkovec JM, Graham DW, Hammond ML, Quraishi N, Tata JR, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Thompson CM, Zaller DM, Forrest MJ, Carballo-Jane E, Luell S. Ali A, et al. Among authors: hammond ml. J Med Chem. 2004 May 6;47(10):2441-52. doi: 10.1021/jm030585i. J Med Chem. 2004. PMID: 15115388
Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.
Thompson CF, Quraishi N, Ali A, Tata JR, Hammond ML, Balkovec JM, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Yamin TT, Thompson CM, O'Neill EA, Zaller D, Forrest MJ, Carballo-Jane E, Luell S. Thompson CF, et al. Among authors: hammond ml. Bioorg Med Chem Lett. 2005 Apr 15;15(8):2163-7. doi: 10.1016/j.bmcl.2005.02.009. Bioorg Med Chem Lett. 2005. PMID: 15808489
99 results