Novel γ-secretase modulators for the treatment of Alzheimer's disease: a review focusing on patents from 2010 to 2012. (Q38123209)

29 August 2017

Novel γ-secretase modulators for the treatment of Alzheimer's disease: a review focusing on patents from 2010 to 2012. (English)

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29 August 2017

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Martin Pettersson

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29 August 2017

Antonia F Stepan

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2

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29 August 2017

Gregory W Kauffman

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3

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29 August 2017

Douglas S Johnson

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4

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29 August 2017

language of work or name

English

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publication date

23 July 2013

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Expert Opinion on Therapeutic Patents

29 August 2017

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29 August 2017

23

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29 August 2017

1349-1366

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29 August 2017

10

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Presenilins and γ-secretase: structure, function, and role in Alzheimer Disease

29 August 2017

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https://api.crossref.org/works/10.1517%2F13543776.2013.821465

The amyloid cascade hypothesis for Alzheimer's disease: an appraisal for the development of therapeutics

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Therapeutic intervention for Alzheimer's disease with γ-secretase inhibitors: still a viable option?

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Targets for AD treatment: conflicting messages from γ-secretase inhibitors

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.821465

What the halted phase III γ-secretase inhibitor trial may (or may not) be telling us.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Safety and tolerability of the γ-secretase inhibitor avagacestat in a phase 2 study of mild to moderate Alzheimer disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

BMS-708,163 targets presenilin and lacks notch-sparing activity

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.821465

The mechanism of γ-Secretase dysfunction in familial Alzheimer disease

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.821465

An improved cell-based method for determining the γ-secretase enzyme activity against both Notch and APP substrates

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Pharmacodynamics of selective inhibition of γ-secretase by avagacestat.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

A subset of NSAIDs lower amyloidogenic Abeta42 independently of cyclooxygenase activity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

NSAIDs and enantiomers of flurbiprofen target gamma-secretase and lower Abeta 42 in vivo

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Abeta42-lowering nonsteroidal anti-inflammatory drugs preserve intramembrane cleavage of the amyloid precursor protein (APP) and ErbB-4 receptor and signaling through the APP intracellular domain.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Sulindac sulfide is a noncompetitive gamma-secretase inhibitor that preferentially reduces Abeta 42 generation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Novel γ-secretase modulators: a review of patents from 2008 to 2010.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

γ-Secretase modulators as potential disease modifying anti-Alzheimer's drugs

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Possible mechanisms of action of NSAIDs and related compounds that modulate gamma-secretase cleavage.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Effect of tarenflurbil on cognitive decline and activities of daily living in patients with mild Alzheimer disease: a randomized controlled trial

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

1-(3',4'-Dichloro-2-fluoro[1,1'-biphenyl]-4-yl)-cyclopropanecarboxylic acid (CHF5074), a novel gamma-secretase modulator, reduces brain beta-amyloid pathology in a transgenic mouse model of Alzheimer's disease without causing peripheral toxicity.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Generation of Abeta38 and Abeta42 is independently and differentially affected by familial Alzheimer disease-associated presenilin mutations and gamma-secretase modulation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Phenylpiperidine-type γ-secretase modulators target the transmembrane domain 1 of presenilin 1

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Piperidine acetic acid based γ-secretase modulators directly bind to Presenilin-1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Modulation of gamma-secretase reduces beta-amyloid deposition in a transgenic mouse model of Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Acute effect on the Aβ isoform pattern in CSF in response to γ-secretase modulator and inhibitor treatment in dogs

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Discovery of a novel pharmacological and structural class of gamma secretase modulators derived from the extract of Actaea racemosa

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Development and mechanism of γ-secretase modulators for Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Fast Calculation of Molecular Polar Surface Area as a Sum of Fragment-Based Contributions and Its Application to the Prediction of Drug Transport Properties

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Piperidine-derived gamma-secretase modulators

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Dynamics of Aβ42 reduction in plasma, CSF and brain of rats treated with the γ-secretase modulator, GSM-10h.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Γ-secretase modulators do not induce Aβ-rebound and accumulation of β-C-terminal fragment

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

TASTPM mice expressing amyloid precursor protein and presenilin-1 mutant transgenes are sensitive to γ-secretase modulation and amyloid-β₄₂ lowering by GSM-10h.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Differential effects between γ-secretase inhibitors and modulators on cognitive function in amyloid precursor protein-transgenic and nontransgenic mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Amelioration of cognitive deficits in plaque-bearing Alzheimer's disease model mice through selective reduction of nascent soluble Aβ42 without affecting other Aβ pools

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Modulation of γ-secretase by EVP-0015962 reduces amyloid deposition and behavioral deficits in Tg2576 mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Chronic treatment with a novel γ-secretase modulator, JNJ-40418677, inhibits amyloid plaque formation in a mouse model of Alzheimer's disease.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Discovery of 4-aminomethylphenylacetic acids as γ-secretase modulators via a scaffold design approach

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Discovery of BIIB042, a Potent, Selective, and Orally Bioavailable γ-Secretase Modulator

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Chemical Biology, Molecular Mechanism and Clinical Perspective of γ-Secretase Modulators in Alzheimer's Disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Therapeutic potential of gamma-secretase inhibitors and modulators

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Synthesis and SAR Studies of Fused Oxadiazines as γ-Secretase Modulators for Treatment of Alzheimer's Disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Design and synthesis of a novel series of bicyclic heterocycles as potent γ-secretase modulators.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Initial Optimization of a New Series of γ-Secretase Modulators Derived from a Triterpene Glycoside

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Optimization of a natural product-based class of γ-secretase modulators.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Escape from flatland: increasing saturation as an approach to improving clinical success.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Physiochemical drug properties associated with in vivo toxicological outcomes

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

Structure of a presenilin family intramembrane aspartate protease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

γ-Secretase modulator (GSM) photoaffinity probes reveal distinct allosteric binding sites on presenilin

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.821465

10.1517/13543776.2013.821465

21 January 2018

Identifiers

DOI

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29 August 2017

1 reference