91 articles for thisTarget
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Article Title
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Hydroxytriamides as potent gamma-secretase inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Part 3: Notch-sparing¿-secretase inhibitors: SAR studies of 2-substituted aminopyridopyrimidinones.
Harvard Medical School
Part 1: Notch-sparing¿-secretase inhibitors: The identification of novel naphthyl and benzofuranyl amide analogs.
Harvard Medical School
Synthesis of pyrimido[4,5-c]azepine- and pyrimido[4,5-c]oxepine-based¿-secretase modulators.
Bristol-Myers Squibb
Design and optimization of tricyclic gamma-secretase modulators.
Bristol-Myers Squibb Research and Development
SAR-studies of¿-secretase modulators with PPAR¿-agonistic and 5-lipoxygenase-inhibitory activity for Alzheimer's disease.
Goethe-University Frankfurt
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
Membrane anchoring¿-secretase modulators with terpene-derived moieties.
Technische Universit£T Darmstadt
Discovery of SCH 900229, a Potent Presenilin 1 Selective ¿-Secretase Inhibitor for the Treatment of Alzheimer's Disease.
TBA
Insensitivity to Abeta42-lowering nonsteroidal anti-inflammatory drugs and gamma-secretase inhibitors is common among aggressive presenilin-1 mutations.
Emmy Noether Research Group
Small molecules targeting ?-secretase and their potential biological applications.
Shenyang Pharmaceutical University
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
Indian Institute of Technology (B.H.U.)
Discovery of the Oxadiazine FRM-024: A Potent CNS-Penetrant Gamma Secretase Modulator.
Forum Pharmaceuticals
Design of Transmembrane Mimetic Structural Probes to Trap Different Stages of ?-Secretase-Substrate Interaction.
University of Kansas
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
University of Nebraska Medical Center
Phenyl bioisosteres in medicinal chemistry: discovery of novel ?-secretase modulators as a potential treatment for Alzheimer's disease.
Roche Innovation Center Basel
Novel Bicyclic Heteroaryl Compounds as ?-Secretase Modulators for Treating Alzheimer's Disease.
Smith, Gambrell & Russell
Design and synthesis of novel methoxypyridine-derived gamma-secretase modulators.
University of California
Synthesis of functionalized derivatives of the gamma-secretase modulator BMS-932481 and identification of its major metabolite.
Bristol-Myers Squibb
Recent developments of small molecule ?-secretase modulators for Alzheimer's disease.
Memorial Sloan-Kettering Cancer Center
Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.
Novartis Institutes For Biomedical Research
Optimization and biological evaluation of imidazopyridine derivatives as a novel scaffold for ?-secretase modulators with oral efficacy against cognitive deficits in Alzheimer's disease model mice.
Astellas Pharma
Stepwise Design of ?-Secretase Modulators with an Advanced Profile by Judicious Coordinated Structural Replacements and an Unconventional Phenyl Ring Bioisostere.
F. Hoffmann-La Roche
Discovery of RO7185876, a Highly Potent ?-Secretase Modulator (GSM) as a Potential Treatment for Alzheimer's Disease.
F. Hoffmann-La Roche
Discovery of N-ethylpyridine-2-carboxamide derivatives as a novel scaffold for orally active ?-secretase modulators.
Astellas Pharma
Design and synthesis of aminothiazole modulators of the gamma-secretase enzyme.
University of California
Notch Antagonists: Potential Modulators of Cancer and Inflammatory Diseases.
Centre Hospitalier Universitaire Vaudois (Chuv)
Design and synthesis of a novel series of cyanoindole derivatives as potent ?-secretase modulators.
Janssen Research & Development
Bridged Piperidine Derivatives Useful as ?-Secretase Inhibitors for the Treatment of Alzheimer's Disease.
Temple University
Triazolo Pyridines Useful as Inhibitors of ?-Secretase and Their Methods of Use.
Temple University
Part 2. Notch-sparing ?-secretase inhibitors: The study of novel ?-amino naphthyl alcohols.
Harvard Medical School
Discovery of novel triazolobenzazepinones as ?-secretase modulators with central A?42 lowering in rodents and rhesus monkeys.
Merck Research Laboratories Boston
Development of CBAP-BPyne, a probe for ?-secretase and presenilinase.
Memorial Sloan-Kettering Cancer Center
Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious ?-secretase inhibitors.
Elan Pharmaceuticals
Effect of helical conformation and side chain structure on ?-secretase inhibition by ?-peptide foldamers: insight into substrate recognition.
Nagoya City University
A-ring modification of SCH 900229 and related chromene sulfone ?-secretase inhibitors.
Merck Research Laboratories
Structure activity relationship studies of tricyclic bispyran sulfone ?-secretase inhibitors.
Merck Research Laboratories
Synthesis and SAR Studies of Fused Oxadiazines as ?-Secretase Modulators for Treatment of Alzheimer's Disease.
Merck Research Laboratory
2-(N-Benzyl-N-phenylsulfonamido)alkyl amide derivatives as ?-secretase inhibitors.
Bristol-Myers Squibb R&D
Initial Optimization of a New Series of ?-Secretase Modulators Derived from a Triterpene Glycoside.
Satori Pharmaceuticals
Application of the bicyclo[1.1.1]pentane motif as a nonclassical phenyl ring bioisostere in the design of a potent and orally active ?-secretase inhibitor.
Pfizer
Lead optimization of 4,4-biaryl piperidine amides as ?-secretase inhibitors.
Merck Research Laboratories
Development of clickable active site-directed photoaffinity probes for ?-secretase.
Memorial Sloan-Kettering Cancer Center
Metabolism-directed design of oxetane-containing arylsulfonamide derivatives as ?-secretase inhibitors.
Pfizer
Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent ?-secretase inhibitors.
Elan Pharmaceuticals
NSAID-derived ?-secretase modulation requires an acidic moiety on the carbazole scaffold.
Technische Universit£T Darmstadt
Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as ?-secretase inhibitors: discovery of PF-3084014.
Pfizer
Diamide amino-imidazoles: a novel series of ?-secretase inhibitors for the treatment of Alzheimer's disease.
Pfizer
Discovery of fused 5,6-bicyclic heterocycles as ?-secretase modulators.
Merck Research Laboratories
Novel Notch-sparing gamma-secretase inhibitors derived from a peroxisome proliferator-activated receptor agonist library.
Okayama University Graduate School of Medicine
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors (Part II).
Elan Pharmaceuticals
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors.
Elan Pharmaceuticals
NSAID-derived gamma-secretase modulators. Part III: Membrane anchoring.
Technische Universit£T Darmstadt
Piperazinyl pyrimidine derivatives as potent gamma-secretase modulators.
Merck Research Laboratories
Fluorinated piperidine acetic acids as gamma-secretase modulators.
Merck Research Laboratories
Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors.
Elan Pharmaceuticals
Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors.
Wyeth Research
Novel orally bioavailable gamma-secretase inhibitors with excellent in vivo activity.
Merck Sharp & Dohme Research Laboratories
Stereo-controlled synthesis of novel photoreactive gamma-secretase inhibitors.
Memorial Sloan-Kettering Cancer Center
Signal peptide peptidase and gamma-secretase share equivalent inhibitor binding pharmacology.
Bristol-Myers Squibb Research and Development
Substituted 2-oxo-azepane derivatives are potent, orally active gamma-secretase inhibitors.
F. Hoffmann-La Roche
Sulfonamide derivatives of bridgehead substituted bicyclo[4.2.1]nonanes as gamma-secretase inhibitors.
Merck Sharp and Dohme Research Laboratories
Nitrogen-appended N-alkylsulfonamides as inhibitors of gamma-secretase.
Bristol-Myers Squibb
Amino-caprolactam derivatives as gamma-secretase inhibitors.
Bristol-Myers Squibb Research and Development
Conversion of the LXR-agonist TO-901317--from inverse to normal modulation of gamma-secretase by addition of a carboxylic acid and a lipophilic anchor.
Darmstadt University of Technology
Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheimer's disease.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of gamma-secretase inhibitors efficacious in a transgenic animal model of Alzheimer's disease.
Schering-Plough Research Institute
Tetrahydroquinoline sulfonamides as gamma-secretase inhibitors.
Schering-Plough Research Institute
N-Substituted carbazolyloxyacetic acids modulate Alzheimer associated gamma-secretase.
Darmstadt University of Technology
Novel orally active, dibenzazepinone-based gamma-secretase inhibitors.
F. Hoffmann-La Roche
N-(5-chloro-2-(hydroxymethyl)-N-alkyl-arylsulfonamides as gamma-secretase inhibitors.
Bristol-Myers Squibb Research and Development
Design and synthesis of benzoazepinone-derived cyclic malonamides and aminoamides as potent gamma-secretase inhibitors.
Bristol-Myers Squibb
2,6-Disubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.
Schering-Plough Research Institute
Azabicyclic Fused Pyrimidine Derivatives Useful for the Treatment of Alzheimer's Disease.
Temple University
Azabicyclic Fused Pyrimidine Derivatives Useful for the Treatment of Alzheimer's Disease.
Temple University
Secretase inhibitors for the treatment of Alzheimer's disease: Long road ahead.
Banaras Hindu University
Discovery of novel scaffolds for ?-secretase modulators without an arylimidazole moiety.
Astellas Pharma
Discovery of a Tetrahydrobenzisoxazole Series of ?-Secretase Modulators.
Merck Research Laboratories