128 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
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
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