43 articles for MD Bartberger
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Fragment-Linking Approach Using (19)F NMR Spectroscopy To Obtain Highly Potent and Selective Inhibitors ofß-Secretase.
Amgen
Recent advances in the development of acetyl-CoA carboxylase (ACC) inhibitors for the treatment of metabolic disease.
Amgen
An Orally Available BACE1 Inhibitor That Affords Robust CNS Aß Reduction without Cardiovascular Liabilities.
Amgen
Development of 2-aminooxazoline 3-azaxanthenes as orally efficaciousß-secretase inhibitors for the potential treatment of Alzheimer's disease.
Amgen
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket.
Amgen
Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors.
Amgen
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series.
Amgen
Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists.
Amgen
Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction.
Amgen
Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.
Amgen
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.
Amgen
Discovery of 2-methylpyridine-based biaryl amides as¿-secretase modulators for the treatment of Alzheimer's disease.
Amgen
Hydroxyethylamine-based inhibitors of BACE1: P1-P3 macrocyclization can improve potency, selectivity, and cell activity.
Amgen
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
Amgen
Design and synthesis of potent, orally efficacious hydroxyethylamine derivedß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.
Amgen
Design and preparation of a potent series of hydroxyethylamine containingß-secretase inhibitors that demonstrate robust reduction of centralß-amyloid.
Amgen
Structure guided P1' modifications of HEA derivedß-secretase inhibitors for the treatment of Alzheimer's disease.
Envoy Therapeutics
Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists.
Amgen
From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1).
Amgen
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
Amgen
Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
Amgen
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
Amgen
The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement.
Amgen
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
California Institute of Technology
Discovery of AM-6494: A Potent and Orally Efficacious β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.
TBA
Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.
Amgen
Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine.
TBA
Diastereoselective synthesis of fused cyclopropyl-3-amino-2,4-oxazine β-amyloid cleaving enzyme (BACE) inhibitors and their biological evaluation.
Amgen
(Hetero)aryl-methyl-thio-beta-D-galactopyranoside derivatives
Idorsia Pharmaceuticals
Inhibition of arginine aminopeptidase by bestatin and arphamenine analogues. Evidence for a new mode of binding to aminopeptidases.
University of Wisconsin