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Page 1
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: disalvo j. 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 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. 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
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. 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 benzamides as potent human β3 adrenergic receptor agonists.
Zhu C, Kar NF, Li B, Costa M, Dingley KH, Di Salvo J, Ha SN, Hurley AL, Li X, Miller RR, Salituro GM, Struthers M, Weber AE, Hale JJ, Edmondson SD. Zhu C, et al. Bioorg Med Chem Lett. 2016 Jan 1;26(1):55-9. doi: 10.1016/j.bmcl.2015.11.030. Epub 2015 Nov 11. Bioorg Med Chem Lett. 2016. PMID: 26590100
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. 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
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.
Parmee ER, He J, Mastracchio A, Edmondson SD, Colwell L, Eiermann G, Feeney WP, Habulihaz B, He H, Kilburn R, Leiting B, Lyons K, Marsilio F, Patel RA, Petrov A, Di Salvo J, Wu JK, Thornberry NA, Weber AE. Parmee ER, et al. Bioorg Med Chem Lett. 2004 Jan 5;14(1):43-6. doi: 10.1016/j.bmcl.2003.10.016. Bioorg Med Chem Lett. 2004. PMID: 14684294
(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. J Med Chem. 2006 Jun 15;49(12):3614-27. doi: 10.1021/jm060015t. J Med Chem. 2006. PMID: 16759103
Pharmacological Characterization of a Novel Beta 3 Adrenergic Agonist, Vibegron: Evaluation of Antimuscarinic Receptor Selectivity for Combination Therapy for Overactive Bladder.
Di Salvo J, Nagabukuro H, Wickham LA, Abbadie C, DeMartino JA, Fitzmaurice A, Gichuru L, Kulick A, Donnelly MJ, Jochnowitz N, Hurley AL, Pereira A, Sanfiz A, Veronin G, Villa K, Woods J, Zamlynny B, Zycband E, Salituro GM, Frenkl T, Weber AE, Edmondson SD, Struthers M. Di Salvo J, et al. J Pharmacol Exp Ther. 2017 Feb;360(2):346-355. doi: 10.1124/jpet.116.237313. Epub 2016 Dec 13. J Pharmacol Exp Ther. 2017. PMID: 27965369
133 results