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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: zhang bb. J Med Chem. 2005 Jan 13;48(1):141-51. doi: 10.1021/jm0493156. J Med Chem. 2005. PMID: 15634008
(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. 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
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. 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
Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: Profile of clinical candidate (2R,3S,5R)-2- (2,5-difluorophenyl)-5-(4,6-dihydropyrrolo [3,4-c]pyrazol-5-(1H)-yl)tetrahydro-2H-pyran-3-amine (23) [corrected].
Biftu T, Qian X, Chen P, Feng D, Scapin G, Gao YD, Cox J, Roy RS, Eiermann G, He H, Lyons K, Salituro G, Patel S, Petrov A, Xu F, Xu SS, Zhang B, Caldwell C, Wu JK, Lyons K, Weber AE. Biftu T, et al. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5361-6. doi: 10.1016/j.bmcl.2013.07.061. Epub 2013 Aug 5. Bioorg Med Chem Lett. 2013. PMID: 23972441
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. 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 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: zhang x, zhang bb. J Med Chem. 2008 Feb 14;51(3):589-602. doi: 10.1021/jm070330v. Epub 2008 Jan 18. J Med Chem. 2008. PMID: 18201067
Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus.
Xu J, Lin S, Myers RW, Addona G, Berger JP, Campbell B, Chen HS, Chen Z, Eiermann GJ, Elowe NH, Farrer BT, Feng W, Fu Q, Kats-Kagan R, Kavana M, Malkani S, McMasters DR, Mitra K, Pachanski MJ, Tong X, Trujillo ME, Xu L, Zhang B, Zhang F, Zhang R, Parmee ER. Xu J, et al. Bioorg Med Chem Lett. 2017 May 1;27(9):2069-2073. doi: 10.1016/j.bmcl.2016.10.085. Epub 2016 Oct 31. Bioorg Med Chem Lett. 2017. PMID: 28284804
Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus.
Xu J, Lin S, Myers RW, Trujillo ME, Pachanski MJ, Malkani S, Chen HS, Chen Z, Campbell B, Eiermann GJ, Elowe N, Farrer BT, Feng W, Fu Q, Kats-Kagan R, Kavana M, McMasters DR, Mitra K, Tong X, Xu L, Zhang F, Zhang R, Addona GH, Berger JP, Zhang B, Parmee ER. Xu J, et al. Bioorg Med Chem Lett. 2017 May 1;27(9):2063-2068. doi: 10.1016/j.bmcl.2016.10.088. Epub 2016 Oct 31. Bioorg Med Chem Lett. 2017. PMID: 28284809
465 results