Devasthale P, Wang Y, Wang W, Fevig J, Feng J, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei HE, Kish K, Weigelt C, Sun L, Levesque P, Moulin F, Li YX, Zahler R, Kirby MS, Hamann LG (2013)
Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (Sa)-2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]py ridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778)
Journal of Medicinal Chemistry 56: 7343
Zhao G, Kwon C, Wang A, Robertson JG, Marcinkeviciene J, Parker RA, Kirby MS, Hamann LG (2013)
Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Lett 23: 1622
Wang W, Devasthale P, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei HE, Kish K, Weigelt C, Sun L, Levesque P, Li YX, Zahler R, Kirby MS, Hamann LG (2011)
7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site
Bioorganic & Medicinal Chemistry Lett 21: 6646
Brigance RP, Meng W, Fura A, Harrity T, Wang A, Zahler R, Kirby MS, Hamann LG (2010)
Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes
Bioorganic & Medicinal Chemistry Lett 20: 4395
Meng W, Brigance RP, Chao HJ, Fura A, Harrity T, Marcinkeviciene J, O'Connor SP, Tamura JK, Xie D, Zhang Y, Klei HE, Kish K, Weigelt CA, Turdi H, Wang A, Zahler R, Kirby MS, Hamann LG (2010)
Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxa mides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors
Journal of Medicinal Chemistry 53: 5620
O'Connor SP, Wang Y, Simpkins LM, Brigance RP, Meng W, Wang A, Kirby MS, Weigelt CA, Hamann LG (2010)
Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors
Bioorganic & Medicinal Chemistry Lett 20: 6273
Fura A, Khanna A, Vyas V, Koplowitz B, Chang SY, Caporuscio C, Boulton DW, Christopher LJ, Chadwick KD, Hamann LG, Humphreys WG, Kirby M (2009)
Pharmacokinetics of the dipeptidyl peptidase 4 inhibitor saxagliptin in rats, dogs, and monkeys and clinical projections
Drug Metabolism & Disposition: The Biological Fate of Chemicals 37: 1164
Metzler WJ, Yanchunas J, Weigelt C, Kish K, Klei HE, Xie D, Zhang Y, Corbett M, Tamura JK, He B, Hamann LG, Kirby MS, Marcinkeviciene J (2008)
Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation
Protein Science 17: 240
Simpkins LM, Bolton S, Pi Z, Sutton JC, Kwon C, Zhao G, Magnin DR, Augeri DJ, Gungor T, Rotella DP, Sun Z, Liu Y, Slusarchyk WS, Marcinkeviciene J, Robertson JG, Wang A, Robl JA, Atwal KS, Zahler RL, Parker RA, Kirby MS, Hamann LG (2007)
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Lett 17: 6476
Magnin DR, Taunk PC, Robertson JG, Wang A, Marcinkeviciene J, Kirby MS, Hamann LG (2006)
Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1
Bioorganic & Medicinal Chemistry Lett 16: 1731
Augeri DJ, Robl JA, Betebenner DA, Magnin DR, Khanna A, Robertson JG, Wang A, Simpkins LM, Taunk P, Huang Q, Han SP, Abboa-Offei B, Cap M, Xin L, Tao L, Tozzo E, Welzel GE, Egan DM, Marcinkeviciene J, Chang SY, Biller SA, Kirby MS, Parker RA, Hamann LG (2005)
Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Journal of Medicinal Chemistry 48: 5025
Zhao G, Taunk PC, Magnin DR, Simpkins LM, Robl JA, Wang A, Robertson JG, Marcinkeviciene J, Sitkoff DF, Parker RA, Kirby MS, Hamann LG (2005)
Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Lett 15: 3992
Magnin DR, Robl JA, Sulsky RB, Augeri DJ, Huang Y, Simpkins LM, Taunk PC, Betebenner DA, Robertson JG, Abboa-Offei BE, Wang A, Cap M, Xin L, Tao L, Sitkoff DF, Malley MF, Gougoutas JZ, Khanna A, Huang Q, Han SP, Parker RA, Hamann LG (2004)
Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability: interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of alpha-aminoacyl-l-cis-4,5-methanoprolinenitrile-based inhibitors
Journal of Medicinal Chemistry 47: 2587