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28 results

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Page 1
Identification of a nonbasic melanin hormone receptor 1 antagonist as an antiobesity clinical candidate.
Washburn WN, Manfredi M, Devasthale P, Zhao G, Ahmad S, Hernandez A, Robl JA, Wang W, Mignone J, Wang Z, Ngu K, Pelleymounter MA, Longhi D, Zhao R, Wang B, Huang N, Flynn N, Azzara AV, Barrish JC, Rohrbach K, Devenny JJ, Rooney S, Thomas M, Glick S, Godonis HE, Harvey SJ, Cullen MJ, Zhang H, Caporuscio C, Stetsko P, Grubb M, Maxwell BD, Yang H, Apedo A, Gemzik B, Janovitz EB, Huang C, Zhang L, Freeden C, Murphy BJ. Washburn WN, et al. J Med Chem. 2014 Sep 25;57(18):7509-22. doi: 10.1021/jm500026w. Epub 2014 Sep 9. J Med Chem. 2014. PMID: 25165888
Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup.
Devasthale P, Wang W, Hernandez AS, Moore F, Renduchintala K, Sridhar R, Pelleymounter MA, Longhi D, Huang N, Flynn N, Azzara AV, Rohrbach K, Devenny J, Rooney S, Thomas M, Glick S, Godonis H, Harvey S, Cullen MJ, Zhang H, Caporuscio C, Stetsko P, Grubb M, Huang C, Zhang L, Freeden C, Li YX, Murphy BJ, Robl JA, Washburn WN. Devasthale P, et al. Among authors: washburn wn. Bioorg Med Chem Lett. 2015 Jul 15;25(14):2793-9. doi: 10.1016/j.bmcl.2015.05.008. Epub 2015 May 15. Bioorg Med Chem Lett. 2015. PMID: 26022839
Non-basic azolotriazinone MCHR1 antagonists for the treatment of obesity: An empirical brain-exposures-driven candidate selection for in vivo efficacy studies.
Devasthale P, Wang W, Mignone J, Renduchintala K, Radhakrishnan S, Dhanapal J, Selvaraj J, Kuppusamy R, Pelleymounter MA, Longhi D, Huang N, Flynn N, Azzara AV, Rohrbach K, Devenny J, Rooney S, Thomas M, Glick S, Godonis H, Harvey S, Cullen MJ, Zhang H, Caporuscio C, Stetsko P, Grubb M, Huang C, Zhang L, Freeden C, Murphy BJ, Robl JA, Washburn WN. Devasthale P, et al. Among authors: washburn wn. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4412-8. doi: 10.1016/j.bmcl.2015.09.018. Epub 2015 Sep 8. Bioorg Med Chem Lett. 2015. PMID: 26386604
Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor.
Ahmad S, Washburn WN, Hernandez AS, Bisaha S, Ngu K, Wang W, Pelleymounter MA, Longhi D, Flynn N, Azzara AV, Rohrbach K, Devenny J, Rooney S, Thomas M, Glick S, Godonis H, Harvey S, Zhang H, Gemzik B, Janovitz EB, Huang C, Zhang L, Robl JA, Murphy BJ. Ahmad S, et al. Among authors: washburn wn. J Med Chem. 2016 Oct 13;59(19):8848-8858. doi: 10.1021/acs.jmedchem.6b00676. Epub 2016 Sep 15. J Med Chem. 2016. PMID: 27564419
Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series.
Ellsworth BA, Wang Y, Zhu Y, Pendri A, Gerritz SW, Sun C, Carlson KE, Kang L, Baska RA, Yang Y, Huang Q, Burford NT, Cullen MJ, Johnghar S, Behnia K, Pelleymounter MA, Washburn WN, Ewing WR. Ellsworth BA, et al. Among authors: washburn wn. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3978-82. doi: 10.1016/j.bmcl.2007.04.087. Epub 2007 Apr 29. Bioorg Med Chem Lett. 2007. PMID: 17513109
Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.
Meng W, Ellsworth BA, Nirschl AA, McCann PJ, Patel M, Girotra RN, Wu G, Sher PM, Morrison EP, Biller SA, Zahler R, Deshpande PP, Pullockaran A, Hagan DL, Morgan N, Taylor JR, Obermeier MT, Humphreys WG, Khanna A, Discenza L, Robertson JG, Wang A, Han S, Wetterau JR, Janovitz EB, Flint OP, Whaley JM, Washburn WN. Meng W, et al. Among authors: washburn wn. J Med Chem. 2008 Mar 13;51(5):1145-9. doi: 10.1021/jm701272q. Epub 2008 Feb 9. J Med Chem. 2008. PMID: 18260618
BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor.
Gavai AV, Sher PM, Mikkilineni AB, Poss KM, McCann PJ, Girotra RN, Fisher LG, Wu G, Bednarz MS, Mathur A, Wang TC, Sun CQ, Slusarchyk DA, Skwish S, Allen GT, Hillyer DE, Frohlich BH, Abboa-Offei BE, Cap M, Waldron TL, George RJ, Tesfamariam B, Harper TW, Ciosek CP Jr, Young DA, Dickinson KE, Seymour AA, Arbeeny CM, Washburn WN. Gavai AV, et al. Among authors: washburn wn. Bioorg Med Chem Lett. 2001 Dec 3;11(23):3041-4. doi: 10.1016/s0960-894x(01)00629-1. Bioorg Med Chem Lett. 2001. PMID: 11714606
Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations.
Washburn WN, Harper TW, Wu G, Godfrey JD, McCann P, Girotra R, Shao C, Zhang H, Gavai A, Mikkilineni A, Dejneka T, Ahmed S, Caringal Y, Hangeland J, Zhang M, Cheng PT, Russell AD, Skwish S, Slusarchyk DA, Allen GT, Frohlich BH, Abboa-Offei BE, Cap M, Waldron TL, George RJ, Tesfamariam B, Dickinson KE, Seymour AA, Sher PM. Washburn WN, et al. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4290-6. doi: 10.1016/j.bmcl.2007.05.030. Epub 2007 May 16. Bioorg Med Chem Lett. 2007. PMID: 17533126
28 results