G. Eiermann

发表

(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.

G. Scapin, N. Thornberry, R. S. Roy, 2005, Journal of medicinal chemistry.

Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.

Joseph L Duffy, Aleksandr Petrov, N. Thornberry, 2005, Bioorganic & medicinal chemistry letters.

Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.

Ping Chen, N. Thornberry, B. Leiting, 2004, Bioorganic & medicinal chemistry letters.

4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.

Aleksandr Petrov, N. Thornberry, B. Leiting, 2004, Bioorganic & medicinal chemistry letters.

Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors.

Aleksandr Petrov, N. Thornberry, B. Leiting, 2006, Bioorganic & medicinal chemistry letters.

(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.

G. Scapin, N. Thornberry, R. S. Roy, 2006, Journal of medicinal chemistry.

A PEGylated analog of the gut hormone oxyntomodulin with long-lasting antihyperglycemic, insulinotropic and anorexigenic activity.

A. Pocai, A. Pessi, Alessia Santoprete, 2013, Bioorganic & medicinal chemistry.

Optimization of co‐agonism at GLP‐1 and glucagon receptors to safely maximize weight reduction in DIO‐rodents

M. Erion, M. Tschöp, J. Gidda, 2012, Biopolymers.

Quantifying rates of glucose production in vivo following an intraperitoneal tracer bolus.

M. Erion, D. Kelley, Dan Zhou, 2016, American journal of physiology. Endocrinology and metabolism.

An automated electrophysiology serum shift assay for K(V) channels.

O. McManus, J. Herrington, G. Eiermann, 2008, Assay and drug development technologies.

Glucagon-Like Peptide 1/Glucagon Receptor Dual Agonism Reverses Obesity in Mice

Michael E. Lassman, N. Thornberry, Gaochao Zhou, 2009, Diabetes.

Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus.

Nadine H. Elowe, Brian T. Campbell, J. Berger, 2017, Bioorganic & medicinal chemistry letters.

Selective Small-Molecule Agonists of G Protein–Coupled Receptor 40 Promote Glucose-Dependent Insulin Secretion and Reduce Blood Glucose in Mice

Yun-ping Zhou, J. Berger, N. Thornberry, 2008, Diabetes.

Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst3 Antagonist.

Margaret S. Wu, Yun-ping Zhou, A. Howard, 2012, ACS medicinal chemistry letters.

(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.

G. Scapin, Suresh B. Singh, N. Thornberry, 2007, Bioorganic & medicinal chemistry letters.

Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate).

N. Thornberry, B. Leiting, Dooseop Kim, 2007, Bioorganic & medicinal chemistry letters.

Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes.

N. Thornberry, B. Leiting, G. Eiermann, 2007, Bioorganic & medicinal chemistry letters.

Differential effects of oxyntomodulin and GLP-1 on glucose metabolism.

A. Pocai, Jennifer R. Kosinski, G. Eiermann, 2012, American journal of physiology. Endocrinology and metabolism.

The role of CD 18 in IL‐8 induced dermal and synovial inflammation

D. Macintyre, G. Eiermann, L. Walakovits, 1992, British journal of pharmacology.

Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.

Yun-ping Zhou, J. Berger, N. Thornberry, 2010, Bioorganic & medicinal chemistry letters.

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].

Ping Chen, G. Scapin, R. S. Roy, 2013, Bioorganic & medicinal chemistry letters.

Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists.

Yun-ping Zhou, E. Sherer, A. Howard, 2014, ACS medicinal chemistry letters.

The Role of Voltage-Gated Potassium Channels Kv2.1 and Kv2.2 in the Regulation of Insulin and Somatostatin Release from Pancreatic Islets

M. Jensen, C. Newgard, Yun-ping Zhou, 2013, The Journal of Pharmacology and Experimental Therapeutics.

3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists.

A. Howard, Carina P. Tan, G. Eiermann, 2011, Bioorganic & medicinal chemistry letters.

Leukotrienes and Asthma

R. Dixon, J. Metzger, D. Riendeau, 1992 .

Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.

Youwei Yan, Ping Chen, J. Metzger, 2015, Bioorganic & medicinal chemistry letters.

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. Metzger, M. Maccoss, D. Macintyre, 1998, Journal of medicinal chemistry.

Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.

Ping Chen, N. Thornberry, B. Leiting, 2004, Bioorganic & medicinal chemistry letters.

Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists.

Margaret S. Wu, M. Reibarkh, Yun-ping Zhou, 2014, ACS medicinal chemistry letters.

Recombinant human interleukin-1 beta-induced increase in levels of proteoglycans, stromelysin, and leukocytes in rabbit synovial fluid.

M. Lark, G. Eiermann, I. Singer, 1992, Arthritis and rheumatism.

GLP-1/GCGR dual agonism reverses obesity in mice Short-running title: Dual GLP-1/GCGR agonist for the treatment of obesity

Michael E. Lassman, N. Thornberry, Gaochao Zhou, 2009 .

Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus.

Nadine H. Elowe, Brian T. Campbell, J. Berger, 2017, Bioorganic & medicinal chemistry letters.

Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.

G. Scapin, N. Thornberry, B. Leiting, 2007, Bioorganic & medicinal chemistry letters.

The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes.

Margaret S. Wu, Rebecca T. Ruck, M. Reibarkh, 2012, ACS medicinal chemistry letters.

Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9.

A. Woods, D. Zaller, N. Thornberry, 2005, Diabetes.

Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.

Kathy Lyons, Ping Chen, Dennis Feng, 2014, Journal of medicinal chemistry.

Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy

M. Erion, D. Kemp, S. Prahalada, 2017, Science.

Plasma lipid profiling across species for the identification of optimal animal models of human dyslipidemia[S]

N. Geoghagen, L. Mitnaul, Peggy H. Wong, 2012, Journal of Lipid Research.

Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.

F. Ujjainwalla, E. Sherer, A. Howard, 2016, ACS medicinal chemistry letters.

Inhibition of DPP-4 with sitagliptin improves glycemic control and restores islet cell mass and function in a rodent model of type 2 diabetes.

Yun-ping Zhou, N. Thornberry, J. Mu, 2009, European journal of pharmacology.

Genetic ablation or pharmacological blockade of dipeptidyl peptidase IV does not impact T cell-dependent immune responses

D. Zaller, Yan Cui, K. Vora, 2009, BMC Immunology.

Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines.

G. Scapin, N. Thornberry, R. S. Roy, 2008, Journal of medicinal chemistry.

Extensive laminin and basement membrane accumulation occurs at the onset of bleomycin-induced rodent pulmonary fibrosis.

G. Eiermann, L. Peterson, I. Singer, 1986, The American journal of pathology.

SAR exploration at the C-3 position of tetrahydro-β-carboline sstr3 antagonists.

Margaret S. Wu, M. Reibarkh, Yun-ping Zhou, 2016, Bioorganic & medicinal chemistry letters.

Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes

Margaret S. Wu, Yun-ping Zhou, E. Sherer, 2015, ACS medicinal chemistry letters.

A comparative study of the binding properties, dipeptidyl peptidase‐4 (DPP‐4) inhibitory activity and glucose‐lowering efficacy of the DPP‐4 inhibitors alogliptin, linagliptin, saxagliptin, sitagliptin and vildagliptin in mice

G. Scapin, J. Berger, N. Thornberry, 2017, Endocrinology, diabetes & metabolism.

The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors.

J. Metzger, G. Scapin, S. Xu, 2016, Bioorganic & medicinal chemistry letters.

Polymorphonuclear leukocyte participation in acute oleic-acid-induced lung injury.

R. Thrall, G. Eiermann, B. Dickey, 1983, The American review of respiratory disease.

4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV.

Joseph L Duffy, G. Scapin, N. Thornberry, 2007, Bioorganic & medicinal chemistry letters.

Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.

G. Scapin, N. Thornberry, B. Leiting, 2006, Bioorganic & medicinal chemistry letters.

Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors.

G. Scapin, N. Thornberry, R. S. Roy, 2009, Bioorganic & medicinal chemistry letters.

4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV.