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Page 1
Discovery of novel pyridinones as MGAT2 inhibitors for the treatment of metabolic disorders.
Moore F, Wang W, Zhao G, Mignone J, Meng W, Chu CH, Ma Z, Azzara A, Cullen MJ, Pelleymounter MA, Appiah K, Cvijic ME, Dierks E, Chang S, Foster K, Kopcho L, O'Malley K, Li YX, Khandelwal P, Whaley JM, Mathur A, Hou X, Wu DR, Robl JA, Cheng D, Devasthale P. Moore F, et al. Among authors: robl ja. Bioorg Med Chem Lett. 2023 Jul 15;91:129362. doi: 10.1016/j.bmcl.2023.129362. Epub 2023 Jun 8. Bioorg Med Chem Lett. 2023. PMID: 37295614
Microsomal triglyceride transfer protein inhibitors: discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents.
Magnin DR, Biller SA, Wetterau J, Robl JA, Dickson JK Jr, Taunk P, Harrity TW, Lawrence RM, Sun CQ, Wang T, Logan J, Fryszman O, Connolly F, Jolibois K, Kunselman L. Magnin DR, et al. Among authors: robl ja. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1337-40. doi: 10.1016/s0960-894x(03)00116-1. Bioorg Med Chem Lett. 2003. PMID: 12657277
5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP.
Sulsky R, Robl JA, Biller SA, Harrity TW, Wetterau J, Connolly F, Jolibois K, Kunselman L. Sulsky R, et al. Among authors: robl ja. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70. doi: 10.1016/j.bmcl.2004.07.069. Bioorg Med Chem Lett. 2004. PMID: 15380200
Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Augeri DJ, Robl JA, Betebenner DA, Magnin DR, Khanna A, Robertson JG, Wang A, Simpkins LM, Taunk P, Huang Q, Han SP, Abboa-Offei B, Cap M, Xin L, Tao L, Tozzo E, Welzel GE, Egan DM, Marcinkeviciene J, Chang SY, Biller SA, Kirby MS, Parker RA, Hamann LG. Augeri DJ, et al. Among authors: robl ja. J Med Chem. 2005 Jul 28;48(15):5025-37. doi: 10.1021/jm050261p. J Med Chem. 2005. PMID: 16033281
Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors.
Zhao G, Taunk PC, Magnin DR, Simpkins LM, Robl JA, Wang A, Robertson JG, Marcinkeviciene J, Sitkoff DF, Parker RA, Kirby MS, Hamann LG. Zhao G, et al. Among authors: robl ja. Bioorg Med Chem Lett. 2005 Sep 15;15(18):3992-5. doi: 10.1016/j.bmcl.2005.06.043. Bioorg Med Chem Lett. 2005. PMID: 16046120
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. Among authors: robl ja. J Med Chem. 2007 Mar 22;50(6):1365-79. doi: 10.1021/jm0612968. Epub 2007 Feb 23. J Med Chem. 2007. PMID: 17315987
2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.
Li JJ, Wang H, Tino JA, Robl JA, Herpin TF, Lawrence RM, Biller S, Jamil H, Ponticiello R, Chen L, Chu CH, Flynn N, Cheng D, Zhao R, Chen B, Schnur D, Obermeier MT, Sasseville V, Padmanabha R, Pike K, Harrity T. Li JJ, et al. Among authors: robl ja. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3208-11. doi: 10.1016/j.bmcl.2007.03.017. Epub 2007 Mar 12. Bioorg Med Chem Lett. 2007. PMID: 17383874
Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419).
Watterson SH, Chen P, Zhao Y, Gu HH, Dhar TG, Xiao Z, Ballentine SK, Shen Z, Fleener CA, Rouleau KA, Obermeier M, Yang Z, McIntyre KW, Shuster DJ, Witmer M, Dambach D, Chao S, Mathur A, Chen BC, Barrish JC, Robl JA, Townsend R, Iwanowicz EJ. Watterson SH, et al. Among authors: robl ja. J Med Chem. 2007 Jul 26;50(15):3730-42. doi: 10.1021/jm070299x. Epub 2007 Jun 22. J Med Chem. 2007. PMID: 17585753
70 results