Analysis of Technological Developments in the Treatment of Alzheimer’s Disease through Patent Documents

Carvalho, Karinne Marieta; Winter, Eduardo; Antunes, Adelaide Maria de Souza

doi:10.4236/iim.2015.75022

Cited by 7 publications

(4 citation statements)

References 59 publications

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“…The first of the current drugs approved for the treatment of Alzheimer's disease (AD) was donepezil in 1996, followed in subsequent years by rivastigmine (2000) and galantamine (2001), all having the same mechanism of action by inhibiting acetylcholinesterase [1]. In particular, the pharmacophore of rivastigmine is its carbamate structure, which has a unique dual pseudo-irreversible inhibitor action both on acetylcholinesterase and butyrylcholinesterase, affording a more robust, transient increase in the levels of acetylcholine.…”

Section: Introductionmentioning

confidence: 99%

HMTM-Mediated Enhancement of Brain Bioenergetics in a Mouse Tauopathy Model Is Blocked by Chronic Administration of Rivastigmine

et al. 2022

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The tau protein aggregation inhibitor hydromethylthionine mesylate (HMTM) was shown recently to have concentration-dependent pharmacological activity in delaying cognitive decline and brain atrophy in phase 3 Alzheimer’s disease (AD) clinical trials; the activity was reduced in patients receiving symptomatic therapies. The methylthionine (MT) moiety has been reported to increase the clearance of pathological tau and to enhance mitochondrial activity, which is impaired in AD patients. In line 1 (L1) mice (a model of AD), HMTM (5/15 mg/kg) was administered either as a monotherapy or as an add-on to a chronic administration with the cholinesterase inhibitor rivastigmine (0.1/0.5 mg/kg) to explore mitochondrial function and energy substrate utilization as potential targets of drug interference. Compared with wild-type NMRI mice, the L1 mice accumulated greater levels of l-lactate and of the LDH-A subunit responsible for the conversion of pyruvate into l-lactate. In contrast, the levels of LDH-B and mitochondrial ETC subunits and the activity of complexes I and IV was not altered in the L1 mice. The activity of complex I and complex IV tended to increase with the HMTM dosing, in turn decreasing l-lactate accumulation in the brains of the L1 mice, despite increasing the levels of LDH-A. The chronic pre-dosing of the L1 mice with rivastigmine partially prevented the enhancement of the activity of complexes I and IV by HMTM and the increase in the levels of LDH-A while further reducing the levels of l-lactate. Thus, HMTM in combination with rivastigmine leads to a depletion in the energy substrate l-lactate, despite bioenergetic production not being favoured. In this study, the changes in l-lactate appear to be regulated by LDH-A, since neither of the experimental conditions affected the levels of LDH-B. The data show that HMTM monotherapy facilitates the use of substrates for energy production, particularly l-lactate, which is provided by astrocytes, additionally demonstrating that a chronic pre-treatment with rivastigmine averted most of the HMTM-associated effects.

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Section: Introductionmentioning

confidence: 99%

HMTM-Mediated Enhancement of Brain Bioenergetics in a Mouse Tauopathy Model Is Blocked by Chronic Administration of Rivastigmine

et al. 2022

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“…Tech mining examinations mostly occur based on patents and scientific articles using text mining, scientometrics, social network analysis and bibliometrics [1][2][3][4][5]. The findings of studies that use these data sources provide useful information only for the current key technologies because the related estimation techniques require historical citation data of the related patent documents [66,67].…”

Section: Research Aim Objectives and The Conceptual Frameworkmentioning

confidence: 99%

“…Using these techniques to follow the newest technological advancements aids the improvement of business operations. The most common data sources tech mining is applied to include patents [2,3], scientific publications [4,5], and recently, social media data [6,7] and website data [8].…”

Section: Introductionmentioning

confidence: 99%

Human Resources Mining for Examination of R&D Progress and Requirements

Ozcan

Şakar

Suloglu

2021

IEEE Trans. Eng. Manage.

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The amount of job advertisement data is rapidly growing, and this rich dataset is expected to have implications for the employment market, sector trajectories and the education sector. Most significantly, human resources (HR) data has never previously been examined with the lens of tech mining for science and technology analyses. Our study is the first to examine job advertisement data considering research and development (R&D) progress and requirements, and hereafter we refer to this as HR mining. The aim of this study is to use HR mining with the purpose of R&D and human capital intelligence using the job advertisement data of Turkey for the 2015-2017 period. The method of this study follows classification as part of the pre-processing step to determine R&D, engineering and high-tech industry-related job advertisements. Afterwards, we use clustering methods to identify areas where key human capital is required, and investments are made by R&D-oriented companies. The results show that it is possible to identify sector-oriented skill requirements and that the significance of the R&D skills varies. For the case of Turkey, we can clearly show the national human capital and R&D by identifying nine key clusters that indicate R&D progress and directions.

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“…Memantine was the first NMDA receptor antagonist approved in the United States and is prescribed to improve cognition, attention, reasoning, language and the ability to perform simple tasks in moderate‐to‐severe AD. In 2005, the FDA declined to expand the scope of memantine to mild AD, due to side effects such as headache, constipation, confusion and dizziness …”

Section: Introductionmentioning

confidence: 99%

Advancements in nanotherapeutics for Alzheimer’s disease: current perspectives

Harilal

Jose

Parambi

et al. 2019

Journal of Pharmacy and Pharmacology

123

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Objectives Considerable progress has been made in the treatment of Alzheimer's disease (AD), but all available strategies focus on alleviating symptoms rather than curing, which means that AD is viewed as an unresolvable neurodegenerative disease. Nanotechnological applications offer an alternative platform for the treatment of neurodegenerative diseases. This review aims to summarize the recent nanomedicine and nanotechnology developments for the treatment of AD. Key findings A plethora of nanocarriers and nanoparticle prodrugs have been reported to have negligible cytotoxicity in animal models, and these developments have revealed new opportunities for development of new classes of potent drug formulations for AD. Different nanotechnology-based approaches such as polymers, emulsions, lipo-carriers, solid lipid carriers, carbon nanotubes and metal-based carriers have been developed over the past decade, and they have been focusing on both neuroprotective and neurogenerative techniques to treat AD. Studies also reveal that nanotechnological approaches can aid in early diagnosis of AD and enhance therapeutic efficacy and bioavailability. Summary Notably, the drugs used conventionally to target the central nervous system have limitations that include an inability to cross the 'blood-brain barrier' or the 'blood-cerebrospinal fluid barrier' effectively and high drug efflux due to the activity of P-glycoprotein, but these limitations can be successfully overcome when nanocarriers are used for targeted drug delivery in AD.

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Analysis of Technological Developments in the Treatment of Alzheimer’s Disease through Patent Documents

Cited by 7 publications

References 59 publications

HMTM-Mediated Enhancement of Brain Bioenergetics in a Mouse Tauopathy Model Is Blocked by Chronic Administration of Rivastigmine

HMTM-Mediated Enhancement of Brain Bioenergetics in a Mouse Tauopathy Model Is Blocked by Chronic Administration of Rivastigmine

Human Resources Mining for Examination of R&D Progress and Requirements

Advancements in nanotherapeutics for Alzheimer’s disease: current perspectives

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