K. J. Filipski

发表

Discovery of Orally Bioavailable Selective Inhibitors of the Sodium-Phosphate Cotransporter NaPi2a (SLC34A1).

P. Loria, M. Boehm, H. Jüppner, 2018, ACS medicinal chemistry letters.

Structural attributes influencing unbound tissue distribution.

Christopher E. Keefer, A. Kalgutkar, D. Scott, 2019, European journal of medicinal chemistry.

A Versatile Copper-Catalyzed Coupling Reaction of Pyridin-2(1H)-ones with Aryl Halides.

A. Casimiro-Garcia, K. J. Filipski, D. Dudley, 2006 .

Progress in the discovery of Factor Xa inhibitors

A. Casimiro-Garcia, C. Bigge, K. J. Filipski, 2006 .

Pyrazole inhibitors of HMG-CoA reductase: an attempt to dramatically reduce synthetic complexity through minimal analog re-design.

B. Tait, M. Kowala, G. Lu, 2007, Bioorganic & medicinal chemistry letters.

Discovery and in Vitro Optimization of 3-Sulfamoylbenzamides as ROMK Inhibitors.

A. Carlo, M. Boehm, K. J. Filipski, 2018, ACS medicinal chemistry letters.

Pyridones as glucokinase activators: identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle.

J. Pfefferkorn, P. Oates, J. Litchfield, 2009, Bioorganic & medicinal chemistry letters.

The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of type 2 diabetes mellitus.

Michael D. Hamilton, J. Pfefferkorn, N. Barucci, 2012, Bioorganic & medicinal chemistry letters.

Designing glucokinase activators with reduced hypoglycemia risk: discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus

M. Ammirati, J. Treadway, S. Liras, 2011 .

Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia.

A. Carlo, J. Pfefferkorn, J. Litchfield, 2013, Bioorganic & medicinal chemistry letters.

Optimizing glucokinase activator binding kinetics to lower in vivo hypoglycemia risk

T. Rolph, J. Pfefferkorn, K. Borzilleri, 2014 .

A patent review of glucokinase activators and disruptors of the glucokinase – glucokinase regulatory protein interaction: 2011 – 2014

J. Pfefferkorn, K. J. Filipski, 2014, Expert opinion on therapeutic patents.

Selective pharmacological inhibition of the sodium-dependent phosphate co-transporter NPT2a promotes phosphate excretion.

Jeonifer M. Garren, H. Jüppner, K. J. Filipski, 2020, The Journal of clinical investigation.

BDK inhibition acts as a catabolic switch to mimic fasting and improve metabolism in mice

A. Hadjipanayis, E. Pashos, C. Steppan, 2022, Molecular metabolism.

The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus.

J. Treadway, J. Pfefferkorn, W. Zavadoski, 2013, Bioorganic & medicinal chemistry letters.

Intrinsic electrophilicity of the 4-methylsulfonyl-2-pyridone scaffold in glucokinase activators: role of glutathione-S-transferases and in vivo quantitation of a glutathione conjugate in rats.

S. Wright, A. Kalgutkar, J. Pfefferkorn, 2010, Bioorganic & medicinal chemistry letters.

Novel and selective spiroindoline-based inhibitors of Sky kinase.

N. Powell, F. Schwende, Amy M. Delaney, 2012, Bioorganic & medicinal chemistry letters.

The discovery of fluoropyridine-based inhibitors of the factor VIIa/TF complex--Part 2.

M. Adler, M. Whitlow, E. Zhang, 2005, Bioorganic & medicinal chemistry letters.

The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex.

M. Adler, M. Whitlow, E. Zhang, 2006, Bioorganic & Medicinal Chemistry Letters.

An efficient synthesis of 2-(3-(4-amidinophenylcarbamoyl)naphthalen-2-yl)-5-((2,2-methylpropyl)carbamoyl)benzoic acid: a factor VIIa inhibitor discovered by the Ono Pharmaceutical Company

K. J. Filipski, W. L. Cody, J. Edmunds, 2000 .

The discovery of glycine and related amino acid-based factor Xa inhibitors.

Mostofa A Hena, V. Sahasrabudhe, E. Zhang, 2006, Bioorganic & medicinal chemistry.

A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity.

S. Wright, J. Pfefferkorn, J. Litchfield, 2012, Bioorganic & medicinal chemistry letters.

Structure‐based Drug Design of Pyrrolidine‐1, 2‐dicarboxamides as a Novel Series of Orally Bioavailable Factor Xa Inhibitors

E. Zhang, Tom McClanahan, A. Casimiro-Garcia, 2007, Chemical biology & drug design.

The Discovery of (2R,4R)‐N‐(4‐chlorophenyl)‐N‐ (2‐fluoro‐4‐(2‐oxopyridin‐1(2H)‐yl)phenyl)‐4‐methoxypyrrolidine‐1,2‐dicarboxamide (PD 0348292), an Orally Efficacious Factor Xa Inhibitor

L. Chi, E. Zhang, Tom McClanahan, 2007, Chemical biology & drug design.

Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action.

Kevin J Filipski, Igor Mochalkin, V. Sahasrabudhe, 2009, Bioorganic & medicinal chemistry.

Intestinal targeting of drugs: rational design approaches and challenges.

T. Goosen, M. Varma, A. El‐Kattan, 2013, Current topics in medicinal chemistry.

Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus.

Jing Chen, David B Duignan, Robert Aiello, 2012, Journal of medicinal chemistry.

Chapter 4:Glucokinase Activators in Development

J. Pfefferkorn, K. J. Filipski, Benjamin D. Stevens, 2012 .

Structural studies identify angiotensin II receptor blocker-like compounds as branched-chain ketoacid dehydrogenase kinase inhibitors

B. L. Kormos, P. Sahasrabudhe, R. Sommese, 2023, The Journal of biological chemistry.

Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif.

K. Gajiwala, M. Hickey, J. Pfefferkorn, 2013, Bioorganic & medicinal chemistry letters.

Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-Activated Protein Kinase (AMPK).

R. Kurumbail, A. Kalgutkar, B. Feng, 2018, Journal of medicinal chemistry.

Teaching a multicultural perspective in software engineering

M.W. Bigrigg, K.J. Filipski, M. Bigrigg, 2007, 2007 37th Annual Frontiers In Education Conference - Global Engineering: Knowledge Without Borders, Opportunities Without Passports.

Identification of a novel conformationally constrained glucagon receptor antagonist.

S. Wright, A. Kalgutkar, J. Pfefferkorn, 2014, Bioorganic & medicinal chemistry letters.

Small molecule glucagon receptor antagonists: a patent review (2011 – 2014)

K. J. Filipski, 2015, Expert opinion on therapeutic patents.

Building structure-activity insights through patent mining.

Kevin J Filipski, Meihua Tu, Jeffrey A Pfefferkorn, 2012, Pharmaceutical patent analyst.

Small molecule branched-chain ketoacid dehydrogenase kinase (BDK) inhibitors with opposing effects on BDK protein levels

Jake E. Delmore, A. Kalgutkar, B. L. Kormos, 2023, Nature communications.