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Page 1
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: salituro gm. 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
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. Among authors: salituro gm. 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
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. Among authors: salituro gm. 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. Among authors: salituro gm. 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. Among authors: salituro gm. 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
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. Among authors: salituro gm. 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
Discovery of phenyl acetamides as potent and selective GPR119 agonists.
Zhu C, Wang L, Zhu Y, Guo ZZ, Liu P, Hu Z, Szewczyk JW, Kang L, Chicchi G, Ehrhardt A, Woods A, Seo T, Woods M, van Heek M, Dingley KH, Pang J, Salituro GM, Powell J, Terebetski JL, Hornak V, Campeau LC, Orr RK, Ujjainwalla F, Miller M, Stamford A, Wood HB, Kowalski T, Nargund RP, Edmondson SD. Zhu C, et al. Among authors: salituro gm. Bioorg Med Chem Lett. 2017 Mar 1;27(5):1124-1128. doi: 10.1016/j.bmcl.2017.01.091. Epub 2017 Feb 1. Bioorg Med Chem Lett. 2017. PMID: 28185720
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. 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 Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes.
Liu P, Hu Z, DuBois BG, Moyes CR, Hunter DN, Zhu C, Kar NF, Zhu Y, Garfunkle J, Kang L, Chicchi G, Ehrhardt A, Woods A, Seo T, Woods M, van Heek M, Dingley KH, Pang J, Salituro GM, Powell J, Terebetski JL, Hornak V, Campeau LC, Lamberson J, Ujjainwalla F, Miller M, Stamford A, Wood HB, Kowalski T, Nargund RP, Edmondson SD. Liu P, et al. Among authors: salituro gm. ACS Med Chem Lett. 2015 Jul 10;6(8):936-41. doi: 10.1021/acsmedchemlett.5b00207. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288697 Free PMC article.
Improved Stability of Proline-Derived Direct Thrombin Inhibitors through Hydroxyl to Heterocycle Replacement.
Chobanian HR, Pio B, Guo Y, Shen H, Huffman MA, Madeira M, Salituro G, Terebetski JL, Ormes J, Jochnowitz N, Hoos L, Zhou Y, Lewis D, Hawes B, Mitnaul L, O'Neill K, Ellsworth K, Wang L, Biftu T, Duffy JL. Chobanian HR, et al. ACS Med Chem Lett. 2015 Mar 13;6(5):553-7. doi: 10.1021/acsmedchemlett.5b00047. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005532 Free PMC article.
52 results