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Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.
Madar DJ, Kopecka H, Pireh D, Yong H, Pei Z, Li X, Wiedeman PE, Djuric SW, Von Geldern TW, Fickes MG, Bhagavatula L, McDermott T, Wittenberger S, Richards SJ, Longenecker KL, Stewart KD, Lubben TH, Ballaron SJ, Stashko MA, Long MA, Wells H, Zinker BA, Mika AK, Beno DW, Kempf-Grote AJ, Polakowski J, Segreti J, Reinhart GA, Fryer RM, Sham HL, Trevillyan JM. Madar DJ, et al. Among authors: von geldern tw. J Med Chem. 2006 Oct 19;49(21):6416-20. doi: 10.1021/jm060777o. J Med Chem. 2006. PMID: 17034148
Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors.
Pei Z, Li X, Longenecker K, von Geldern TW, Wiedeman PE, Lubben TH, Zinker BA, Stewart K, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Long M, Wells H, Kempf-Grote AJ, Madar DJ, McDermott TS, Bhagavatula L, Fickes MG, Pireh D, Solomon LR, Lake MR, Edalji R, Fry EH, Sham HL, Trevillyan JM. Pei Z, et al. Among authors: von geldern tw. J Med Chem. 2006 Jun 15;49(12):3520-35. doi: 10.1021/jm051283e. J Med Chem. 2006. PMID: 16759095
Crystal structures of DPP-IV (CD26) from rat kidney exhibit flexible accommodation of peptidase-selective inhibitors.
Longenecker KL, Stewart KD, Madar DJ, Jakob CG, Fry EH, Wilk S, Lin CW, Ballaron SJ, Stashko MA, Lubben TH, Yong H, Pireh D, Pei Z, Basha F, Wiedeman PE, von Geldern TW, Trevillyan JM, Stoll VS. Longenecker KL, et al. Among authors: von geldern tw. Biochemistry. 2006 Jun 20;45(24):7474-82. doi: 10.1021/bi060184f. Biochemistry. 2006. PMID: 16768443
Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors.
Kurukulasuriya R, Rohde JJ, Szczepankiewicz BG, Basha F, Lai C, Jae HS, Winn M, Stewart KD, Longenecker KL, Lubben TW, Ballaron SJ, Sham HL, von Geldern TW. Kurukulasuriya R, et al. Among authors: von geldern tw. Bioorg Med Chem Lett. 2006 Dec 15;16(24):6226-30. doi: 10.1016/j.bmcl.2006.09.024. Epub 2006 Sep 28. Bioorg Med Chem Lett. 2006. PMID: 17010607
Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Pei Z, Li X, von Geldern TW, Madar DJ, Longenecker K, Yong H, Lubben TH, Stewart KD, Zinker BA, Backes BJ, Judd AS, Mulhern M, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Reinhart GA, Fryer RM, Preusser LC, Kempf-Grote AJ, Sham HL, Trevillyan JM. Pei Z, et al. Among authors: von geldern tw. J Med Chem. 2006 Nov 2;49(22):6439-42. doi: 10.1021/jm060955d. J Med Chem. 2006. PMID: 17064063
Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.
Backes BJ, Longenecker K, Hamilton GL, Stewart K, Lai C, Kopecka H, von Geldern TW, Madar DJ, Pei Z, Lubben TH, Zinker BA, Tian Z, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Kempf-Grote AJ, Black-Schaefer C, Sham HL, Trevillyan JM. Backes BJ, et al. Among authors: von geldern tw. Bioorg Med Chem Lett. 2007 Apr 1;17(7):2005-12. doi: 10.1016/j.bmcl.2007.01.026. Epub 2007 Jan 19. Bioorg Med Chem Lett. 2007. PMID: 17276063
Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors.
Pei Z, Li X, von Geldern TW, Longenecker K, Pireh D, Stewart KD, Backes BJ, Lai C, Lubben TH, Ballaron SJ, Beno DW, Kempf-Grote AJ, Sham HL, Trevillyan JM. Pei Z, et al. Among authors: von geldern tw. J Med Chem. 2007 Apr 19;50(8):1983-7. doi: 10.1021/jm061436d. Epub 2007 Mar 17. J Med Chem. 2007. PMID: 17367123
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
Richards SJ, von Geldern TW, Jacobson P, Wilcox D, Nguyen P, Ohman L, Osterlund M, Gelius B, Grynfarb M, Goos-Nilsson A, Wang J, Fung S, Kalmanovich M. Richards SJ, et al. Among authors: von geldern tw. Bioorg Med Chem Lett. 2006 Dec 1;16(23):6086-90. doi: 10.1016/j.bmcl.2006.08.133. Epub 2006 Sep 20. Bioorg Med Chem Lett. 2006. PMID: 16987661
Effect of bradykinin metabolism inhibitors on evoked hypotension in rats: rank efficacy of enzymes associated with bradykinin-mediated angioedema.
Fryer RM, Segreti J, Banfor PN, Widomski DL, Backes BJ, Lin CW, Ballaron SJ, Cox BF, Trevillyan JM, Reinhart GA, von Geldern TW. Fryer RM, et al. Among authors: von geldern tw. Br J Pharmacol. 2008 Mar;153(5):947-55. doi: 10.1038/sj.bjp.0707641. Epub 2007 Dec 17. Br J Pharmacol. 2008. PMID: 18084312 Free PMC article.
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
von Geldern TW, Tu N, Kym PR, Link JT, Jae HS, Lai C, Apelqvist T, Rhonnstad P, Hagberg L, Koehler K, Grynfarb M, Goos-Nilsson A, Sandberg J, Osterlund M, Barkhem T, Höglund M, Wang J, Fung S, Wilcox D, Nguyen P, Jakob C, Hutchins C, Färnegårdh M, Kauppi B, Ohman L, Jacobson PB. von Geldern TW, et al. J Med Chem. 2004 Aug 12;47(17):4213-30. doi: 10.1021/jm0400045. J Med Chem. 2004. PMID: 15293993
66 results