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(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Edmondson SD, Mastracchio A, Mathvink RJ, He J, Harper B, Park YJ, Beconi M, Di Salvo J, Eiermann GJ, He H, Leiting B, Leone JF, Levorse DA, Lyons K, Patel RA, Patel SB, Petrov A, Scapin G, Shang J, Roy RS, Smith A, Wu JK, Xu S, Zhu B, Thornberry NA, Weber AE. Edmondson SD, et al. Among authors: harper b. J Med Chem. 2006 Jun 15;49(12):3614-27. doi: 10.1021/jm060015t. J Med Chem. 2006. PMID: 16759103
2-Substituted piperazine-derived imidazole carboxamides as potent and selective CCK1R agonists for the treatment of obesity.
Berger R, Zhu C, Hansen AR, Harper B, Chen Z, Holt TG, Hubert J, Lee SJ, Pan J, Qian S, Reitman ML, Strack AM, Weingarth DT, Wolff M, Macneil DJ, Weber AE, Edmondson SD. Berger R, et al. Among authors: harper b. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4833-7. doi: 10.1016/j.bmcl.2008.07.083. Epub 2008 Jul 24. Bioorg Med Chem Lett. 2008. PMID: 18684621
Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles.
Goble SD, Wang L, Howell KL, Bansal A, Berger R, Brockunier L, DiSalvo J, Feighner S, Harper B, He J, Hurley A, Hreniuk D, Parmee E, Robbins M, Salituro G, Sanfiz A, Streckfuss E, Watkins E, Weber AE, Struthers M, Edmondson SD. Goble SD, et al. Among authors: harper b. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1895-9. doi: 10.1016/j.bmcl.2010.01.130. Epub 2010 Feb 4. Bioorg Med Chem Lett. 2010. PMID: 20181479
Design, synthesis, and evaluation of conformationally restricted acetanilides as potent and selective β3 adrenergic receptor agonists for the treatment of overactive bladder.
Moyes CR, Berger R, Goble SD, Harper B, Shen DM, Wang L, Bansal A, Brown PN, Chen AS, Dingley KH, Di Salvo J, Fitzmaurice A, Gichuru LN, Hurley AL, Jochnowitz N, Miller RR, Mistry S, Nagabukuro H, Salituro GM, Sanfiz A, Stevenson AS, Villa K, Zamlynny B, Struthers M, Weber AE, Edmondson SD. Moyes CR, et al. Among authors: harper b. J Med Chem. 2014 Feb 27;57(4):1437-53. doi: 10.1021/jm4017224. Epub 2014 Feb 5. J Med Chem. 2014. PMID: 24437735
Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
Edmondson SD, Zhu C, Kar NF, Di Salvo J, Nagabukuro H, Sacre-Salem B, Dingley K, Berger R, Goble SD, Morriello G, Harper B, Moyes CR, Shen DM, Wang L, Ball R, Fitzmaurice A, Frenkl T, Gichuru LN, Ha S, Hurley AL, Jochnowitz N, Levorse D, Mistry S, Miller RR, Ormes J, Salituro GM, Sanfiz A, Stevenson AS, Villa K, Zamlynny B, Green S, Struthers M, Weber AE. Edmondson SD, et al. Among authors: harper b. J Med Chem. 2016 Jan 28;59(2):609-23. doi: 10.1021/acs.jmedchem.5b01372. Epub 2016 Jan 8. J Med Chem. 2016. PMID: 26709102
Investigation of piperazine benzamides as human β3 adrenergic receptor agonists for the treatment of overactive bladder.
Harper BH, Wang L, Zhu C, Kar NF, Li B, Moyes CR, Goble SD, Costa M, Dingley K, Di Salvo J, Ha SN, Hurley A, Li X, Miller RR, Nagabukuro H, Salituro GM, Smith S, Struthers M, Hale JJ, Edmondson SD, Berger R. Harper BH, et al. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1094-1098. doi: 10.1016/j.bmcl.2016.12.033. Epub 2016 Dec 11. Bioorg Med Chem Lett. 2017. PMID: 28089699
Rapid development of two factor IXa inhibitors from hit to lead.
Parker DL Jr, Walsh S, Li B, Kim E, Sharipour A, Smith C, Chen YH, Berger R, Harper B, Zhang T, Park M, Shu M, Wu J, Xu J, Dewnani S, Sherer EC, Hruza A, Reichert P, Geissler W, Sonatore L, Ellsworth K, Balkovec J, Greenlee W, Wood HB. Parker DL Jr, et al. Among authors: harper b. Bioorg Med Chem Lett. 2015 Jun 1;25(11):2321-5. doi: 10.1016/j.bmcl.2015.04.025. Epub 2015 Apr 13. Bioorg Med Chem Lett. 2015. PMID: 25937013
295 results