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Page 1
Beta 3 agonists. Part 1: evolution from inception to BMS-194449.
Washburn WN, Sher PM, Poss KM, Girotra RN, McCann PJ, Gavai AV, Mikkilineni AB, Mathur A, Cheng P, Dejneka TC, Sun CQ, Wang TC, Harper TW, Russell AD, Slusarchyk DA, Skwish S, Allen GT, Hillyer DE, Frohlich BH, Abboa-Offei BE, Cap M, Waldron TL, George RJ, Tesfamariam B, Ciosek CP Jr, Ryono D, Young DA, Dickinson KE, Seymour AA, Arbeeny CM, Gregg RE. Washburn WN, et al. Bioorg Med Chem Lett. 2001 Dec 3;11(23):3035-9. doi: 10.1016/s0960-894x(01)00628-x. Bioorg Med Chem Lett. 2001. PMID: 11714605
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
BMS-201620: a selective beta 3 agonist.
Washburn WN, Sun CQ, Bisacchi G, Wu G, Cheng PT, Sher PM, Ryono D, Gavai AV, Poss K, Girotra RN, McCann PJ, Mikkilineni AB, Dejneka TC, Wang TC, Merchant Z, Morella M, Arbeeny CM, Harper TW, Slusarchyk DA, Skwish S, Russell AD, Allen GT, Tesfamariam B, Frohlich BH, Abboa-Offei BE, Cap M, Waldron TL, George RJ, Young D, Dickinson KE, Seymour AA. Washburn WN, et al. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3525-9. doi: 10.1016/j.bmcl.2004.04.074. Bioorg Med Chem Lett. 2004. PMID: 15177466
Addition of benzylic and allylic organozinc and Grignard reagents to resin-bound imines to provide alpha-branched secondary amines bearing a wide variety of functional groups. Utility in the synthesis of beta-3 adrenergic receptor agonists.
Wu G, Cai ZW, Bednarz MS, Kocy OR, Gavai AV, Godfrey JD Jr, Washburn WN, Poss MA, Sher PM. Wu G, et al. Among authors: washburn wn. J Comb Chem. 2005 Jan-Feb;7(1):99-108. doi: 10.1021/cc0498682. J Comb Chem. 2005. PMID: 15638488
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
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
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
Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2.
Ellsworth BA, Meng W, Patel M, Girotra RN, Wu G, Sher PM, Hagan DL, Obermeier MT, Humphreys WG, Robertson JG, Wang A, Han S, Waldron TL, Morgan NN, Whaley JM, Washburn WN. Ellsworth BA, et al. Among authors: washburn wn. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4770-3. doi: 10.1016/j.bmcl.2008.07.109. Epub 2008 Jul 31. Bioorg Med Chem Lett. 2008. PMID: 18707880
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
28 results