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(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Kim D, Wang L, Beconi M, Eiermann GJ, Fisher MH, He H, Hickey GJ, Kowalchick JE, Leiting B, Lyons K, Marsilio F, McCann ME, Patel RA, Petrov A, Scapin G, Patel SB, Roy RS, Wu JK, Wyvratt MJ, Zhang BB, Zhu L, Thornberry NA, Weber AE. Kim D, et al. Among authors: scapin g. J Med Chem. 2005 Jan 13;48(1):141-51. doi: 10.1021/jm0493156. J Med Chem. 2005. PMID: 15634008
(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: scapin g. J Med Chem. 2006 Jun 15;49(12):3614-27. doi: 10.1021/jm060015t. J Med Chem. 2006. PMID: 16759103
Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.
Xu J, Wei L, Mathvink RJ, Edmondson SD, Eiermann GJ, He H, Leone JF, Leiting B, Lyons KA, Marsilio F, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE. Xu J, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5373-7. doi: 10.1016/j.bmcl.2006.07.061. Epub 2006 Aug 17. Bioorg Med Chem Lett. 2006. PMID: 16919457
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Biftu T, Feng D, Qian X, Liang GB, Kieczykowski G, Eiermann G, He H, Leiting B, Lyons K, Petrov A, Sinha-Roy R, Zhang B, Scapin G, Patel S, Gao YD, Singh S, Wu J, Zhang X, Thornberry NA, Weber AE. Biftu T, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2007 Jan 1;17(1):49-52. doi: 10.1016/j.bmcl.2006.09.099. Epub 2006 Oct 5. Bioorg Med Chem Lett. 2007. PMID: 17055272
4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV.
Duffy JL, Kirk BA, Wang L, Eiermann GJ, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE. Duffy JL, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2007 May 15;17(10):2879-85. doi: 10.1016/j.bmcl.2007.02.066. Epub 2007 Feb 25. Bioorg Med Chem Lett. 2007. PMID: 17350841
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin.
Biftu T, Scapin G, Singh S, Feng D, Becker JW, Eiermann G, He H, Lyons K, Patel S, Petrov A, Sinha-Roy R, Zhang B, Wu J, Zhang X, Doss GA, Thornberry NA, Weber AE. Biftu T, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3384-7. doi: 10.1016/j.bmcl.2007.03.095. Epub 2007 Apr 2. Bioorg Med Chem Lett. 2007. PMID: 17433672
Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.
Kowalchick JE, Leiting B, Pryor KD, Marsilio F, Wu JK, He H, Lyons KA, Eiermann GJ, Petrov A, Scapin G, Patel RA, Thornberry NA, Weber AE, Kim D. Kowalchick JE, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5934-9. doi: 10.1016/j.bmcl.2007.07.100. Epub 2007 Aug 23. Bioorg Med Chem Lett. 2007. PMID: 17827003
Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines.
Kim D, Kowalchick JE, Brockunier LL, Parmee ER, Eiermann GJ, Fisher MH, He H, Leiting B, Lyons K, Scapin G, Patel SB, Petrov A, Pryor KD, Roy RS, Wu JK, Zhang X, Wyvratt MJ, Zhang BB, Zhu L, Thornberry NA, Weber AE. Kim D, et al. Among authors: scapin g. J Med Chem. 2008 Feb 14;51(3):589-602. doi: 10.1021/jm070330v. Epub 2008 Jan 18. J Med Chem. 2008. PMID: 18201067
105 results