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Page 1
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: he j. 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
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: he 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
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. Among authors: he h, he j. 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. Among authors: he h, he j. J Med Chem. 2006 Jun 15;49(12):3614-27. doi: 10.1021/jm060015t. J Med Chem. 2006. PMID: 16759103
3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists.
Walsh SP, Severino A, Zhou C, He J, Liang GB, Tan CP, Cao J, Eiermann GJ, Xu L, Salituro G, Howard AD, Mills SG, Yang L. Walsh SP, et al. Among authors: he j. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3390-4. doi: 10.1016/j.bmcl.2011.03.114. Epub 2011 Apr 8. Bioorg Med Chem Lett. 2011. PMID: 21514824
Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.
Edmondson SD, Mastracchio A, He J, Chung CC, Forrest MJ, Hofsess S, MacIntyre E, Metzger J, O'Connor N, Patel K, Tong X, Tota MR, Van der Ploeg LH, Varnerin JP, Fisher MH, Wyvratt MJ, Weber AE, Parmee ER. Edmondson SD, et al. Among authors: he j. Bioorg Med Chem Lett. 2003 Nov 17;13(22):3983-7. doi: 10.1016/j.bmcl.2003.08.056. Bioorg Med Chem Lett. 2003. PMID: 14592490
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.
Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D, Bak A, Eiermann G, He J, Cox J, Hicks J, Lyons K, He H, Salituro G, Tong S, Patel S, Doss G, Petrov A, Wu J, Xu SS, Sewall C, Zhang X, Zhang B, Thornberry NA, Weber AE. Biftu T, et al. Among authors: he h, he j. J Med Chem. 2014 Apr 24;57(8):3205-12. doi: 10.1021/jm401992e. Epub 2014 Apr 2. J Med Chem. 2014. PMID: 24660890
Discovery and Pharmacology of a Novel Somatostatin Subtype 5 (SSTR5) Antagonist: Synergy with DPP-4 Inhibition.
Liu W, Shao PP, Liang GB, Bawiec J, He J, Aster SD, Wu M, Chicchi G, Wang J, Tsao KL, Shang J, Salituro G, Zhou YP, Li C, Akiyama TE, Metzger DE, Murphy BA, Howard AD, Weber AE, Duffy JL. Liu W, et al. Among authors: he j. ACS Med Chem Lett. 2018 Sep 12;9(11):1082-1087. doi: 10.1021/acsmedchemlett.8b00305. eCollection 2018 Nov 8. ACS Med Chem Lett. 2018. PMID: 30429949 Free PMC article.
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