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
Secretase targets for Alzheimer's disease: identification and therapeutic potential.
Harvard Medical School
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
Discovery of cell-permeable non-peptide inhibitors of beta-secretase by high-throughput docking and continuum electrostatics calculations.
University of ZüRich
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
Applications of combinatorial technologies to drug discovery. 1. Background and peptide combinatorial libraries.
Affymax Research Institute
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
Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity
Shionogi
Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
Amgen
1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
Amgen
C5-C6-oxacyclic fused iminothiazine dioxide compounds bearing an ether linker as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
Amgen
C5-C6-oxacyclic fused iminothiazine dioxide compounds bearing an ether linker as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
Heterocyclic derivatives and their use in the treatment of neurological disorders
Novartis
C5-C6-oxacyclic fused iminothiadiazine dioxide compounds bearing an ether linker as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
C5-C6-carbocyclic fused iminothiadiazine dioxides as BACE inhibitors, compositions, and their use
TBA
Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
Amgen
C5-C6-fused tricyclic iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
TBA
Diazine-fused amidines as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
C-6 spirocarbocyclic iminothiadiazine dioxides as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-A]pyrazine derivatives as inhibitors of beta-secretase (BACE)
Janssen Pharmaceutica
Iminothiadiazepane dioxide compounds as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
C2-carbocyclic iminothiazine dioxides as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
C6-spiro iminothiadiazine dioxides as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
Heterocyclic derivatives and their use in the treatment of neurological disorders
Novartis
Iminothiadiazine dioxides bearing an amine-linked substituent as BACE inhibitors, compositions, and their use
TBA
C5-C6-oxacyclic fused iminopyrimidinone compounds as bace inhibitors, compositions, and their use
Merck Sharp & Dohme
5-substituted iminothiazines and their mono- and dioxides as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
C6-azaspiro iminothiadiazine dioxides as bace inhibitors, compositions, and their use
Merck Sharp & Dohme
C2-azaspiro iminothiazine dioxides as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
Iminothiadiazine dioxides containing a thioamide, amidine, or amide oxime group as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
S-imino-S-oxo-iminothiadiazine compounds as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
Merck Sharp & Dohme
S-imino-S-oxo-iminothiazine compounds as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
Merck Sharp & Dohme
Carbocyclic- and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
Pfizer
C5, C6 oxacyclic-fused thiazine dioxide compounds as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
Merck Sharp & Dohme
Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
Inhibition of memapsin 1 cleavage in the treatment of diabetes
Oklahoma Medical Research Foundation
Iminothiadiazine dioxide compounds as brace inhibitors, compositions, and their use
Merck Sharp & Dohme
Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
Heterocyclic derivatives and their use in the treatment of neurological disorders
Novartis
Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
Second generation of BACE-1 inhibitors part 3: Towards non hydroxyethylamine transition state mimetics.
Gsk
Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side substituent.
Gsk
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
Gsk
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
Gsk
Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability.
Gsk
Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).
Merck Research Laboratories
Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands.
Purdue University