132 articles for thisTarget
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Synthesis of (3S,4S)-4-aminopyrrolidine-3-ol derivatives and biological evaluation for their BACE1 inhibitory activities.
Korea University of Science and Technology
Peptidomimeticß-Secretase Inhibitors Comprising a Sequence of Amyloid-ß Peptide for Alzheimer's Disease.
Instituto De Biologia Experimental E Tecnol£Gica
Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.
Eli Lilly
trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker.
Novartis Pharma
trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.
Novartis Pharma
Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.
Merck Research Laboratories
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.
Novartis Institutes For Biomedical Research
Structure-based design, synthesis and biological evaluation of novelß-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand.
Purdue University
Inhibitors ofß-site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine (AMG-8718).
Amgen
ß-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.
F. Hoffmann-La Roche
The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.
Novartis Pharma
Discovery of biphenylacetamide-derived inhibitors of BACE1 using de novo structure-based molecular design.
University of Leeds
A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.
Novartis Pharma
New aminoimidazoles asß-secretase (BACE-1) inhibitors showing amyloid-ß (Aß) lowering in brain.
Astrazeneca
Structure-based design of highly selectiveß-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure.
Purdue University
Design and synthesis ofß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction ofß-amyloid peptides.
Astrazeneca
Design and synthesis of potent hydroxyethylamine (HEA) BACE-1 inhibitors carrying prime side 4,5,6,7-tetrahydrobenzazole and 4,5,6,7-tetrahydropyridinoazole templates.
Medivir
Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS Aß Reduction.
TBA
Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor.
Merck Research Laboratories
BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.
Glaxosmithkline
Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors.
Wyeth Research
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor.
Schering-Plough Research Institute
BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs).
Glaxosmithkline
Potent pyrrolidine- and piperidine-based BACE-1 inhibitors.
Schering-Plough Research Institute
Discovery of pyrrolidine-basedß-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.
Merck Research Laboratories
Design, synthesis, and qualitative structure-activity evaluations of novelß-secretase inhibitors as potential Alzheimer's drug leads.
University of Sharjah
New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region.
Pfizer
Design and synthesis of aminohydantoins as potent and selective humanß-secretase (BACE1) inhibitors with enhanced brain permeability.
Pfizer
Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.
Merck Research Laboratories
Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors.
Wyeth
Structure-based design and synthesis of novel P2/P3 modified, non-peptidic beta-secretase (BACE-1) inhibitors.
University of Montreal
Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors.
Wyeth Research
Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.
Wyeth Research
Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors.
Wyeth Research
Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.
Purdue University
Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitors.
University of Illinois At Chicago
Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.
Schering-Plough Research Institute
BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character.
Glaxosmithkline
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.
Wyeth Research
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Merck Research Laboratories
Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1).
Technische UniversitäT MüNchen
Synthesis of the Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor NB-360.
TBA
Discovery of Umibecestat (CNP520): A Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor for the Prevention of Alzheimer's Disease.
Novartis Pharma
A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo.
Janssen Research & Development
Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor.
Lilly Research Laboratories
Discovery of Extremely Selective Fused Pyridine-Derived β-Site Amyloid Precursor Protein-Cleaving Enzyme (BACE1) Inhibitors with High In Vivo Efficacy through 10s Loop Interactions.
Shionogi
JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.
Janssen Research & Development
Structure-Based Approaches to Improving Selectivity through Utilizing Explicit Water Molecules: Discovery of Selective β-Secretase (BACE1) Inhibitors over BACE2.
Shionogi
Discovery of Atabecestat (JNJ-54861911): A Thiazine-Based β-Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor Advanced to the Phase 2b/3 EARLY Clinical Trial.
Janssen Research & Development
The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement.
Amgen
Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.
Novartis Institutes For Biomedical Research
3,3-Difluoro-3,4,5,6-tetrahydropyridin-2-amines: Potent and permeable BACE-1 inhibitors.
Janssen Research & Development
Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.
Eli Lilly
Tricyclic Inhibitors of β-Secretase and Their Methods of Use for the Treatment of Alzheimer's Disease.
Temple University
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
New evolutions in the BACE1 inhibitor field from 2014 to 2018.
Janssen Research & Development
Discovery of an Extremely Potent Thiazine-Based β-Secretase Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose.
TBA
Evaluation of a Series of β-Secretase 1 Inhibitors Containing Novel Heteroaryl-Fused-Piperazine Amidine Warheads.
Janssen Research & Development
Structure-Based Design of Selective β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors: Targeting the Flap to Gain Selectivity over BACE2.
TBA
Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine β-Secretase (BACE1) Inhibitors via Active Conformation Stabilization.
TBA
Rational Design of Novel 1,3-Oxazine Based β-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust Aβ Reduction in the Brain.
TBA
Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.
Pfizer
Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality.
The Scripps Research Institute
Design, synthesis, and X-ray structural studies of BACE-1 inhibitors containing substituted 2-oxopiperazines as P1'-P2' ligands.
Purdue University
Compounds that interact with the Ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
Shy Therapeutics
Phenylate derivative, preparation method therefor, and pharmaceutical composition and uses thereof
Institute of Materia Medica, Chinese Academy of Medical Sciences
Condensed [1,4] diazepine compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors
Hoffmann-La Roche
Substituted bicyclic pyrazole compounds as RORgammaT inhibitors and uses thereof
Merck Sharp & Dohme
N-substituted pyrazolo [3,4-D] pyrimidine ketone compound, and preparation process and use thereof
Sun Yat-Sen University
Rho kinase inhibitors and methods of use
H. Lee Moffitt Cancer Center and Research Institute
Bifunctional phenolic-choline conjugates as anti-oxidants and acetylcholinesterase inhibitors.
Instituto Superior Técnico
Inhibitory effects of thioethers on fatty acid synthase and 3T3-L1 cells.
Graduate University of Chinese Academy of Sciences
Discovery of 3,3-di(indolyl)indolin-2-one as a novel scaffold for a-glucosidase inhibitors: In silico studies and SAR predictions
Jishou University
Transition state analogues of Plasmodium falciparum and human orotate phosphoribosyltransferases.
Albert Einstein College of Medicine
Molecular basis of cannabinoid CB1 receptor coupling to the G protein heterotrimer Gaiß¿: identification of key CB1 contacts with the C-terminal helix a5 of Gai.
North Carolina Central University
Key mutations alter the cytochrome P450 BM3 conformational landscape and remove inherent substrate bias.
University of Manchester
Evaluation of Natural and Synthetic 1,4-naphthoquinones as Inhibitors of Monoamine Oxidase.
North-West University
Synthesis and biological evaluation of kojic acid derivatives containing 1,2,4-triazole as potent tyrosinase inhibitors.
Hunan University of Science and Technology
Modulators of calcium release-activated calcium channel and methods for treatment of non-small cell lung cancer
Rhizen Pharmaceuticals
Tricyclic compounds as modulators of TNF-α synthesis and as PDE4 inhibitors
High Point Pharmaceuticals
Pyrazolylbenzothiazole derivatives and their use as therapeutic agents
Dermira (Canada)
Solid phase synthesis of novel pyrrolidinedione analogs as potent HIV-1 integrase inhibitors.
Bristol-Myers Squibb
Indolequinone inhibitors of NRH:quinone oxidoreductase 2. Characterization of the mechanism of inhibition in both cell-free and cellular systems.
University of Colorado Denver
2-thioxanthines are mechanism-based inactivators of myeloperoxidase that block oxidative stress during inflammation.
Astrazeneca R&D
Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors.
University of Michigan
Elucidation of the vasoactive intestinal peptide pharmacophore for VPAC(2) receptors in human and rat and comparison to the pharmacophore for VPAC(1) receptors.
Nih
Venlafaxine: discrepancy between in vivo 5-HT and NE reuptake blockade and affinity for reuptake sites.
Mcgill University
Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors.
University of Toronto
Identification and characterization of the leech CNS cannabinoid receptor: coupling to nitric oxide release.
State University of New York At Old Westbury
Characterization of somatostatin receptor subtypes controlling rat gastric acid and pancreatic amylase release.
Tulane University
Antidepressant biochemical profile of the novel bicyclic compound Wy-45,030, an ethyl cyclohexanol derivative.
Wyeth Laboratories
Thermal denaturation: a method to rank slow binding, high-affinity P38alpha MAP kinase inhibitors.
Boehringer Ingelheim Pharmaceuticals
Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Bristol-Myers Squibb Pharmaceutical Research Institute