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Page 1
Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists.
Guo L, Ye Z, Liu J, He S, Bakshi RK, Sebhat IK, Dobbelaar PH, Hong Q, Jian T, Dellureficio JP, Tsou NN, Ball RG, Weinberg DH, MacNeil T, Tang R, Tamvakopoulos C, Peng Q, Chen HY, Chen AS, Martin WJ, MacIntyre DE, Strack AM, Fong TM, Wyvratt MJ, Nargund RP. Guo L, et al. Among authors: ball rg. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4895-900. doi: 10.1016/j.bmcl.2010.06.068. Epub 2010 Jun 17. Bioorg Med Chem Lett. 2010. PMID: 20621473
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine.
Lin P, Chang L, Devita RJ, Young JR, Eid R, Tong X, Zheng S, Ball RG, Tsou NN, Chicchi GG, Kurtz MM, Tsao KL, Wheeldon A, Carlson EJ, Eng W, Burns HD, Hargreaves RJ, Mills SG. Lin P, et al. Among authors: ball rg. Bioorg Med Chem Lett. 2007 Sep 15;17(18):5191-8. doi: 10.1016/j.bmcl.2007.06.085. Epub 2007 Jul 4. Bioorg Med Chem Lett. 2007. PMID: 17637506
1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity.
Vachal P, Fletcher JM, Fong TM, Huang CC, Lao J, Xiao JC, Shen CP, Strack AM, Shearman L, Stribling S, Chen RZ, Frassetto A, Tong X, Wang J, Ball RG, Tsou NN, Hickey GJ, Thompson DF, Faidley TD, Nicolich S, Achanfuo-Yeboah J, Hora DF, Hale JJ, Hagmann WK. Vachal P, et al. Among authors: ball rg. J Med Chem. 2009 Apr 23;52(8):2550-8. doi: 10.1021/jm900063x. J Med Chem. 2009. PMID: 19320488
Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.
He S, Ye Z, Dobbelaar PH, Sebhat IK, Guo L, Liu J, Jian T, Lai Y, Franklin CL, Bakshi RK, Dellureficio JP, Hong Q, Tsou NN, Ball RG, Cashen DE, Martin WJ, Weinberg DH, Macneil T, Tang R, Tamvakopoulos C, Peng Q, Miller RR, Stearns RA, Chen HY, Chen AS, Strack AM, Fong TM, Macintyre DE, Wyvratt MJ Jr, Nargund RP. He S, et al. Among authors: ball rg. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2106-10. doi: 10.1016/j.bmcl.2010.02.058. Epub 2010 Feb 19. Bioorg Med Chem Lett. 2010. PMID: 20207541
Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.
Yan L, Huo P, Debenham JS, Madsen-Duggan CB, Lao J, Chen RZ, Xiao JC, Shen CP, Stribling DS, Shearman LP, Strack AM, Tsou N, Ball RG, Wang J, Tong X, Bateman TJ, Reddy VB, Fong TM, Hale JJ. Yan L, et al. Among authors: ball rg. J Med Chem. 2010 May 27;53(10):4028-37. doi: 10.1021/jm100023j. J Med Chem. 2010. PMID: 20423086
Design of a novel pyrrolidine scaffold utilized in the discovery of potent and selective human β3 adrenergic receptor agonists.
Morriello GJ, Wendt HR, Bansal A, Di Salvo J, Feighner S, He J, Hurley AL, Hreniuk DL, Salituro GM, Reddy MV, Galloway SM, McGettigan KK, Laws G, McKnight C, Doss GA, Tsou NN, Black RM, Morris J, Ball RG, Sanfiz AT, Streckfuss E, Struthers M, Edmondson SD. Morriello GJ, et al. Among authors: ball rg. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1865-70. doi: 10.1016/j.bmcl.2010.12.087. Epub 2010 Dec 25. Bioorg Med Chem Lett. 2011. PMID: 21353541
Discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 agonists and their unusual chirality.
Liu P, Lanza TJ Jr, Chioda M, Jones C, Chobanian HR, Guo Y, Chang L, Kelly TM, Kan Y, Palyha O, Guan XM, Marsh DJ, Metzger JM, Ramsay K, Wang SP, Strack AM, Miller R, Pang J, Lyons K, Dragovic J, Ning JG, Schafer WA, Welch CJ, Gong X, Gao YD, Hornak V, Ball RG, Tsou N, Reitman ML, Wyvratt MJ, Nargund RP, Lin LS. Liu P, et al. Among authors: ball rg. ACS Med Chem Lett. 2011 Oct 3;2(12):933-7. doi: 10.1021/ml200207w. eCollection 2011 Dec 8. ACS Med Chem Lett. 2011. PMID: 24900283 Free PMC article.
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
Meurer LC, Finke PE, Owens KA, Tsou NN, Ball RG, Mills SG, Maccoss M, Sadowski S, Cascieri MA, Tsao KL, Chicchi GG, Egger LA, Luell S, Metzger JM, Macintyre DE, Rupniak NM, Williams AR, Hargreaves RJ. Meurer LC, et al. Among authors: ball rg. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4504-11. doi: 10.1016/j.bmcl.2006.06.044. Epub 2006 Jul 10. Bioorg Med Chem Lett. 2006. PMID: 16831551
Bicyclic amidine inhibitors of nitric oxide synthase: discovery of perhydro-iminopyrindine and perhydro-iminoquinoline as potent, orally active inhibitors of inducible nitric oxide synthase.
Guthikonda RN, Shah SK, Pacholok SG, Humes JL, Mumford RA, Grant SK, Chabin RM, Green BG, Tsou N, Ball R, Fletcher DS, Luell S, Euan MacIntyre D, Maccoss M. Guthikonda RN, et al. Bioorg Med Chem Lett. 2005 Apr 15;15(8):1997-2001. doi: 10.1016/j.bmcl.2005.02.067. Bioorg Med Chem Lett. 2005. PMID: 15808455
69 results