G
George J. Eiermann
Researcher at Merck & Co.
Publications - 54
Citations - 4196
George J. Eiermann is an academic researcher from Merck & Co.. The author has contributed to research in topics: Dipeptidyl peptidase & Agonist. The author has an hindex of 28, co-authored 54 publications receiving 3887 citations. Previous affiliations of George J. Eiermann include Protein Sciences.
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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
Dooseop Kim,Liping Wang,Maria G. Beconi,George J. Eiermann,Michael H. Fisher,Huaibing He,Gerard J. Hickey,Jennifer E. Kowalchick,Barbara Leiting,Kathryn A. Lyons,Frank Marsilio,Margaret E. McCann,Reshma A. Patel,Aleksandr Petrov,Giovanna Scapin,Sangita B. Patel,Ranabir Sinha Roy,Joseph K. Wu,Matthew J. Wyvratt,Bei B. Zhang,Lan Zhu,Nancy A. Thornberry,Ann E. Weber +22 more
TL;DR: A novel series of beta-amino amides incorporating fused heterocycles, i.e., triazolopiperazines, were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-IV) for the treatment of type 2 diabetes and MK-0431, the phosphate salt of compound 1, was selected for development.
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Dipeptidyl Peptidase IV Inhibition for the Treatment of Type 2 Diabetes: Potential Importance of Selectivity Over Dipeptidyl Peptidases 8 and 9
George R. Lankas,Barbara Leiting,Ranabir Sinha Roy,George J. Eiermann,Maria G. Beconi,Tesfaye Biftu,Chi-Chung Chan,Scott D. Edmondson,William P. Feeney,Huaibing He,Dawn E. Ippolito,Dooseop Kim,Kathryn A. Lyons,Hyun O. Ok,Reshma A. Patel,Aleksandr Petrov,Kelly Ann Pryor,Xiaoxia Qian,Leah Bitalac Reigle,Andrea Woods,Joseph K. Wu,Dennis M. Zaller,Xiaoping Zhang,Lan Zhu,Ann E. Weber,Nancy A. Thornberry +25 more
TL;DR: Assessment of selectivity of potential clinical candidates may be important to an optimal safety profile for this new class of antihyperglycemic agents, according to the results of toxicity and tolerability studies.
Journal ArticleDOI
Glucagon-Like Peptide 1/Glucagon Receptor Dual Agonism Reverses Obesity in Mice
Alessandro Pocai,Paul E. Carrington,Jennifer R. Adams,Michael Wright,George J. Eiermann,Lan Zhu,Xiaobing Du,Aleksandr Petrov,Michael E. Lassman,Guoqiang Jiang,Franklin Liu,Corey N. Miller,Laurie Tota,Gaochao Zhou,Xiaoping Zhang,Michael M. Sountis,Alessia Santoprete,Elena Capito,Gary G. Chicchi,Nancy A. Thornberry,Elisabetta Bianchi,Antonello Pessi,Donald J. Marsh,Ranabir SinhaRoy +23 more
TL;DR: Sustained GLP1R/GCGR dual agonism reverses obesity in DIO mice and is a novel therapeutic approach to the treatment of obesity.
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Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy
Robert W. Myers,Hong-Ping Guan,Juliann Ehrhart,Aleksandr Petrov,Srinivasa Prahalada,Effie Tozzo,Xiaodong Yang,Marc M. Kurtz,Maria E. Trujillo,Dinko Gonzalez Trotter,Danqing Feng,Shiyao Xu,George J. Eiermann,Marie A. Holahan,Daniel Rubins,Stacey Conarello,Xiaoda Niu,Sandra C. Souza,Corin O. Miller,Jinqi Liu,Ku Lu,Wen Feng,Ying Li,Ronald E. Painter,James A. Milligan,Huaibing He,Franklin Liu,Aimie Ogawa,Douglas Wisniewski,Rory J. Rohm,Liyang Wang,Michelle Bunzel,Ying Qian,Wei Zhu,Hongwu Wang,Bindu Bennet,Lisa LaFranco Scheuch,Guillermo Fernandez,Cai Li,Michael Klimas,Gaochao Zhou,Margaret van Heek,Tesfaye Biftu,Ann E. Weber,David E. Kelley,Nancy A. Thornberry,Mark D. Erion,Daniel M. Kemp,Iyassu K. Sebhat +48 more
TL;DR: MK-8722 is developed, a potent, direct, allosteric activator of all 12 mammalian AMPK complexes that induced robust, durable, insulin-independent glucose uptake and glycogen synthesis, with resultant improvements in glycemia and no evidence of hypoglycemia in rodents and rhesus monkeys.
Journal ArticleDOI
Structural Optimization Affording 2-(R)-(1-(R)-3,5-Bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a Potent, Orally Active, Long-Acting Morpholine Acetal Human NK-1 Receptor Antagonist
J. J. Hale,Sander G. Mills,M. Maccoss,P. E. Finke,Margaret A. Cascieri,Sharon Sadowski,E. Ber,Gary G. Chicchi,Myra B. Kurtz,Joe Metzger,George J. Eiermann,Nancy N. Tsou,F.D. Tattersall,Nadia M.J. Rupniak,Angela Williams,W. Rycroft,Richard Hargreaves,D. E. Macintyre +17 more
TL;DR: The activity of 17 at extended time points in these preclinical animal models sets it apart from earlier morpholine antagonists (such as 4), and the piperidine antagonists 2 and 3 and could prove to be an advantage in the treatment of chronic disorders related to the actions of Substance P.