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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: beno dw. 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: beno dw. J Med Chem. 2006 Jun 15;49(12):3520-35. doi: 10.1021/jm051283e. J Med Chem. 2006. PMID: 16759095
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: beno dw. 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: beno dw. 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: beno dw. J Med Chem. 2007 Apr 19;50(8):1983-7. doi: 10.1021/jm061436d. Epub 2007 Mar 17. J Med Chem. 2007. PMID: 17367123
2,4-diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists.
Serby MD, Zhao H, Szczepankiewicz BG, Kosogof C, Xin Z, Liu B, Liu M, Nelson LT, Kaszubska W, Falls HD, Schaefer V, Bush EN, Shapiro R, Droz BA, Knourek-Segel VE, Fey TA, Brune ME, Beno DW, Turner TM, Collins CA, Jacobson PB, Sham HL, Liu G. Serby MD, et al. Among authors: beno dw. J Med Chem. 2006 Apr 20;49(8):2568-78. doi: 10.1021/jm0510934. J Med Chem. 2006. PMID: 16610800
Discovery and pharmacological evaluation of growth hormone secretagogue receptor antagonists.
Xin Z, Serby MD, Zhao H, Kosogof C, Szczepankiewicz BG, Liu M, Liu B, Hutchins CW, Sarris KA, Hoff ED, Falls HD, Lin CW, Ogiela CA, Collins CA, Brune ME, Bush EN, Droz BA, Fey TA, Knourek-Segel VE, Shapiro R, Jacobson PB, Beno DW, Turner TM, Sham HL, Liu G. Xin Z, et al. Among authors: beno dw. J Med Chem. 2006 Jul 27;49(15):4459-69. doi: 10.1021/jm060461g. J Med Chem. 2006. PMID: 16854051
Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation.
Patel JR, Shuai Q, Dinges J, Winn M, Pliushchev M, Fung S, Monzon K, Chiou W, Wang J, Pan L, Wagaw S, Engstrom K, Kerdesky FA, Longenecker K, Judge R, Qin W, Imade HM, Stolarik D, Beno DW, Brune M, Chovan LE, Sham HL, Jacobson P, Link JT. Patel JR, et al. Among authors: beno dw. Bioorg Med Chem Lett. 2007 Feb 1;17(3):750-5. doi: 10.1016/j.bmcl.2006.10.074. Epub 2006 Oct 28. Bioorg Med Chem Lett. 2007. PMID: 17110106
Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.
Rohde JJ, Pliushchev MA, Sorensen BK, Wodka D, Shuai Q, Wang J, Fung S, Monzon KM, Chiou WJ, Pan L, Deng X, Chovan LE, Ramaiya A, Mullally M, Henry RF, Stolarik DF, Imade HM, Marsh KC, Beno DW, Fey TA, Droz BA, Brune ME, Camp HS, Sham HL, Frevert EU, Jacobson PB, Link JT. Rohde JJ, et al. Among authors: beno dw. J Med Chem. 2007 Jan 11;50(1):149-64. doi: 10.1021/jm0609364. J Med Chem. 2007. PMID: 17201418
63 results