(Q38003497)

26 August 2017

title

Small-molecule BACE1 inhibitors: a patent literature review (2006 - 2011). (English)

1 reference

26 August 2017

1 reference

Gary Probst

1

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26 August 2017

Ying-zi Xu

series ordinal

2

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26 August 2017

language of work or name

English

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publication date

19 April 2012

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Expert Opinion on Therapeutic Patents

26 August 2017

published in

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26 August 2017

volume

22

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26 August 2017

issue

5

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26 August 2017

page(s)

511-540

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2011 Alzheimer's disease facts and figures

26 August 2017

cites work

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Amyloid deposition as the central event in the aetiology of Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Neurodegenerative tauopathies

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Alzheimer's disease: the amyloid cascade hypothesis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

The molecular pathology of Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Cellular mechanisms of beta-amyloid production and secretion

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

The secretases: enzymes with therapeutic potential in Alzheimer disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Alzheimer's disease: strategies for disease modification

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

γ-secretase substrates and their implications for drug development in Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Activity of gamma-secretase on substrates other than APP.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Chronic treatment with the gamma-secretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Modulation of notch processing by gamma-secretase inhibitors causes intestinal goblet cell metaplasia and induction of genes known to specify gut secretory lineage differentiation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

BACE knockout mice are healthy despite lacking the primary beta-secretase activity in brain: implications for Alzheimer's disease therapeutics

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Mice deficient in BACE1, the Alzheimer's beta-secretase, have normal phenotype and abolished beta-amyloid generation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

BACE1 (beta-secretase) knockout mice do not acquire compensatory gene expression changes or develop neural lesions over time

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Partial reduction of BACE1 has dramatic effects on Alzheimer plaque and synaptic pathology in APP Transgenic Mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

BACE1 deficiency rescues memory deficits and cholinergic dysfunction in a mouse model of Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Cell biology, regulation and inhibition of beta-secretase (BACE-1).

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

The beta-secretase enzyme BACE in health and Alzheimer's disease: regulation, cell biology, function, and therapeutic potential

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Alteration of BACE1-dependent NRG1/ErbB4 signaling and schizophrenia-like phenotypes in BACE1-null mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Neuregulin 1 and schizophrenia

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Genetic deletion of BACE1 in mice affects remyelination of sciatic nerves

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Bace1 modulates myelination in the central and peripheral nervous system.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Control of peripheral nerve myelination by the beta-secretase BACE1

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

BACE1 deficiency causes altered neuronal activity and neurodegeneration

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

BACE1, a major determinant of selective vulnerability of the brain to amyloid-beta amyloidogenesis, is essential for cognitive, emotional, and synaptic functions.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

In vivo beta-secretase 1 inhibition leads to brain Abeta lowering and increased alpha-secretase processing of amyloid precursor protein without effect on neuregulin-1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Human aspartic protease memapsin 2 cleaves the beta-secretase site of beta-amyloid precursor protein

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Beta-secretase cleavage of Alzheimer's amyloid precursor protein by the transmembrane aspartic protease BACE

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Purification and cloning of amyloid precursor protein beta-secretase from human brain

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Membrane-anchored aspartyl protease with Alzheimer's disease beta-secretase activity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Identification of a Novel Aspartic Protease (Asp 2) as β-Secretase

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Specificity of memapsin 1 and its implications on the design of memapsin 2 (beta-secretase) inhibitor selectivity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Elevated beta-secretase expression and enzymatic activity detected in sporadic Alzheimer disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Beta-secretase protein and activity are increased in the neocortex in Alzheimer disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Beta-secretase activity increases with aging in human, monkey, and mouse brain.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Energy inhibition elevates beta-secretase levels and activity and is potentially amyloidogenic in APP transgenic mice: possible early events in Alzheimer's disease pathogenesis.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Amyloid beta peptide load is correlated with increased beta-secretase activity in sporadic Alzheimer's disease patients

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Phosphorylation of the translation initiation factor eIF2alpha increases BACE1 levels and promotes amyloidogenesis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

APP binds DR6 to trigger axon pruning and neuron death via distinct caspases

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Modes of Aβ toxicity in Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Cortical synaptic integration in vivo is disrupted by amyloid-beta plaques.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Fibrillar amyloid deposition leads to local synaptic abnormalities and breakage of neuronal branches.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Beta-amyloid deposition and other measures of neuropathology predict cognitive status in Alzheimer's disease.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Soluble protein oligomers in neurodegeneration: lessons from the Alzheimer's amyloid beta-peptide

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

The role of amyloid-beta derived diffusible ligands (ADDLs) in Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Alzheimer's disease-affected brain: presence of oligomeric A beta ligands (ADDLs) suggests a molecular basis for reversible memory loss

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Diffusible, nonfibrillar ligands derived from Abeta1-42 are potent central nervous system neurotoxins

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

A specific amyloid-beta protein assembly in the brain impairs memory

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Natural oligomers of the amyloid-beta protein specifically disrupt cognitive function

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Accelerating amyloid-beta fibrillization reduces oligomer levels and functional deficits in Alzheimer disease mouse models.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Behavioral changes in transgenic mice expressing both amyloid precursor protein and presenilin-1 mutations: lack of association with amyloid deposits.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Plaque-independent disruption of neural circuits in Alzheimer's disease mouse models

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Correlation between elevated levels of amyloid beta-peptide in the brain and cognitive decline

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Soluble pool of Abeta amyloid as a determinant of severity of neurodegeneration in Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Soluble amyloid beta peptide concentration as a predictor of synaptic change in Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

The levels of soluble versus insoluble brain Abeta distinguish Alzheimer's disease from normal and pathologic aging

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Alzheimer disease amyloid beta protein forms calcium channels in bilayer membranes: blockade by tromethamine and aluminum

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Calcium dysregulation and membrane disruption as a ubiquitous neurotoxic mechanism of soluble amyloid oligomers

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Neuronal calcium mishandling and the pathogenesis of Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Linking calcium to Abeta and Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Alzheimer's disease-type neuronal tau hyperphosphorylation induced by A beta oligomers

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Amyloid-beta42 signals tau hyperphosphorylation and compromises neuronal viability by disrupting alkylacylglycerophosphocholine metabolism.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Soluble amyloid beta-protein dimers isolated from Alzheimer cortex directly induce Tau hyperphosphorylation and neuritic degeneration

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Tau is essential to beta -amyloid-induced neurotoxicity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Amyloid-beta protein dimers isolated directly from Alzheimer's brains impair synaptic plasticity and memory

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Formation of neurofibrillary tangles in P301l tau transgenic mice induced by Abeta 42 fibrils

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

A phase 2 multiple ascending dose trial of bapineuzumab in mild to moderate Alzheimer disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

11C-PiB PET assessment of change in fibrillar amyloid-beta load in patients with Alzheimer's disease treated with bapineuzumab: a phase 2, double-blind, placebo-controlled, ascending-dose study

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Soluble oligomers of amyloid Beta protein facilitate hippocampal long-term depression by disrupting neuronal glutamate uptake

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Naturally secreted oligomers of amyloid beta protein potently inhibit hippocampal long-term potentiation in vivo

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Oral treatment with a gamma-secretase inhibitor improves long-term potentiation in a mouse model of Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Intracellular amyloid-beta in Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

ABAD directly links Abeta to mitochondrial toxicity in Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Mitochondria are a direct site of A beta accumulation in Alzheimer's disease neurons: implications for free radical generation and oxidative damage in disease progression

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Alzheimer's disease: genetic studies and transgenic models

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

The presenilins and Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Amyloid, the presenilins and Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

The role of apolipoprotein E in Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Apolipoprotein E and its receptors in Alzheimer's disease: pathways, pathogenesis and therapy

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Aβ-degrading enzymes: potential for treatment of Alzheimer disease.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Abeta-degrading enzymes in Alzheimer's disease.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Insulin-degrading enzyme regulates the levels of insulin, amyloid beta-protein, and the beta-amyloid precursor protein intracellular domain in vivo

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Age- and region-dependent alterations in Abeta-degrading enzymes: implications for Abeta-induced disorders

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

ApoE promotes the proteolytic degradation of Abeta

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Somatostatin regulates brain amyloid beta peptide Abeta42 through modulation of proteolytic degradation.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Loss of somatostatin-like immunoreactivity in the frontal cortex of Alzheimer patients carrying the apolipoprotein epsilon 4 allele.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Decreased expression and activity of neprilysin in Alzheimer disease are associated with cerebral amyloid angiopathy.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Reduced hippocampal insulin-degrading enzyme in late-onset Alzheimer's disease is associated with the apolipoprotein E-epsilon4 allele

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Cerebral amyloid angiopathy: progressive disruption of the neurovascular unit

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Proteolytic shedding of ST6Gal-I by BACE1 regulates the glycosylation and function of alpha4beta1 integrins

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Second generation of BACE-1 inhibitors part 3: Towards non hydroxyethylamine transition state mimetics

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side substituent

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs)

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Potent pyrrolidine- and piperidine-based BACE-1 inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Design and synthesis of 2,3,5-substituted imidazolidin-4-one inhibitors of BACE-1

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE)

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1)

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Macrocyclic inhibitors of beta-secretase: functional activity in an animal model.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Discovery of pyrrolidine-based β-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

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)

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

2-Amino-3,4-dihydroquinazolines as inhibitors of BACE-1 (beta-site APP cleaving enzyme): Use of structure based design to convert a micromolar hit into a nanomolar lead

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Macrocyclic BACE inhibitors: Optimization of a micromolar hit to nanomolar leads

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Discovery of aminoheterocycles as a novel beta-secretase inhibitor class: pH dependence on binding activity part 1

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Thiophene substituted acylguanidines as BACE1 inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Pyridinyl aminohydantoins as small molecule BACE1 inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Design and synthesis of aminohydantoins as potent and selective human β-secretase (BACE1) inhibitors with enhanced brain permeability

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Aminoimidazoles as BACE-1 inhibitors: the challenge to achieve in vivo brain efficacy

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

Rational design and synthesis of aminopiperazinones as β-secretase (BACE) inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

A therapeutic antibody targeting BACE1 inhibits amyloid-β production in vivo

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.681302

10.1517/13543776.2012.681302

21 January 2018

Identifiers

DOI

1 reference

26 August 2017

1 reference