Last updated: August 6, 2025
Introduction
Japan Patent JP2014193926, titled "Method for Treating Disease Using Melatonin Derivatives," pertains to novel melatonin derivative compounds and their therapeutic applications, primarily targeting neurodegenerative and sleep disorders. The patent landscape surrounding this invention reflects a broader interest in melatonin analogs within the pharmaceutical industry for their neuroprotective, circadian rhythm regulation, and antioxidant properties. This analytical review examines the scope and claims of JP2014193926, contextualizing its position within existing patents and technological trends in this segment.
Patent Overview and Publication Context
Published in 2014 by a leading Japanese pharmaceutical entity, JP2014193926 builds upon prior melatonin research. The patent aims to establish proprietary rights over specific melatonin derivatives with enhanced bioavailability, stability, or receptor affinity, thereby extending the patent life and market exclusivity for related products. It embodies claims covering chemical structures, methods of synthesis, and therapeutic uses, aligning with common patent strategies for small-molecule drugs.
Scope of the Patent
Chemical and Structural Scope
The core of JP2014193926 revolves around a class of melatonin derivatives characterized by specific substitutions on the indole ring and acetamide side chains. These modifications purportedly improve pharmacokinetic profiles and receptor selectivity. The patent claims include:
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Defined chemical formulae representing derivatives with particular substituents (e.g., halogens, methyl groups) at designated positions.
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Preferred embodiments that specify substituent types and positions, such as 5- or 6- halogen substitutions, which may influence receptor binding affinity.
Therapeutic Applications
Claims encompass a wide scope of medical indications, predominantly:
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Treatment of sleep disorders (e.g., insomnia, circadian rhythm disturbances).
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Neurodegenerative diseases, including Alzheimer’s disease and Parkinson's disease.
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Oxidative stress-related conditions, leveraging the antioxidant capacity of derivatives.
By including these indications, the patent aims to safeguard both the compounds and their uses across a spectrum of CNS-related disorders, which are high-value therapeutic areas.
Method of Synthesis and Pharmaceutical Formulations
In addition to the chemical compounds, JP2014193926 claims methods for synthesizing these derivatives with high purity and yield. It also covers pharmaceutical compositions—tablets, capsules, or injectable forms—with effective amounts of the claimed derivatives, specifying pharmaceutically acceptable carriers and dosage ranges.
Claims Analysis
Independent Claims
The independent claims essentially define:
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A chemical compound with a specific melatonin derivative structure, incorporating certain substitutions to optimize pharmacological properties.
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A method of treating a neurodegenerative or sleep disorder involving administering an effective amount of the claimed derivative.
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A pharmaceutical composition comprising the derivative and a carrier, suitable for therapeutic use.
Dependent Claims
Dependent claims specify particular derivatives with specific substituents, enhance synthesis methods, or narrow therapeutic indications, providing patent scope of varying breadth and enabling strategic territorial patenting.
Claim Strength and Limitations
Judge by conventional patent standards, the claims are sufficiently broad to cover multiple derivatives within the disclosed chemical space, yet specific enough to differentiate from prior art, especially compounds with distinct substitutions. However, the actual scope is limited to the disclosed chemical structures and their specific modifications, possibly allowing for design-around strategies.
Patent Landscape Context
Prior Art and Related Patents
The patent landscape features numerous prior art references relating to melatonin analogs, notably US patents such as US2015009584 (covering melatonin receptor agonists) and Japanese patents like JP2009191671, addressing indole derivatives for sleep regulation. JP2014193926 appears to carve a niche with particular substitution patterns aimed at improved pharmacological profiles.
Competitive IP Environment
Competitors include pharmaceutical companies and research institutions developing melatonin receptor agonists and neuroprotective agents. Notably, Ramelteon (US FDA-approved sleep aid) and Tasimelteon (approved for non-24-hour sleep-wake disorder) form part of this landscape, with their patents underpinning some of the competitive barriers.
Freedom-to-Operate Analysis
Given the specificity of claimed chemical structures, the patent potentially provides robust protection within its scope, especially if derivatives with similar substitutions are not disclosed in prior art. However, alternative substitution patterns or different molecular frameworks could circumvent the patent.
Strategic Significance
The patent’s claims, covering novel melatonin derivatives and their therapeutic applications, position the patent holder to:
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Control a segment of the sleep and neurodegenerative drug market.
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Leverage broad claims to expand into various formulations and indications.
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Engage in licensing or partnerships with other pharmaceutical firms interested in innovative CNS therapies.
The patent’s robustness depends on ongoing patent examination, potential opposition, and the evolution of the competing technology landscape.
Conclusion: Summary & Outlook
JP2014193926 exemplifies strategic patenting within the neuropharmacology space, extending the proprietary hold on melatonin analogs with enhanced therapeutic qualities. Its scope, encompassing chemical compounds, synthesis methods, and therapeutic uses, demonstrates a comprehensive patenting approach to secure market exclusivity.
As research continues into sleep and neurodegenerative disorder therapeutics, companies must monitor this patent's claims vis-à-vis emerging innovations, particularly around different molecular scaffolds or receptor-targeted agents. Moreover, the potential for patent challenges or design-around strategies remains high, necessitating vigilant patent portfolio management.
Key Takeaways
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Broad Chemical and Therapeutic Scope: The patent covers specific melatonin derivatives with claims extending to treatment methods for sleep and neurodegenerative disorders, providing a strong strategic position.
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Claims Strategy: Well-structured independent claims protect core derivatives, while dependent claims narrow the scope to specific substitutions, balancing patent strength with flexibility.
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Competitive Landscape: In a crowded field with existing melatonin receptor agonist patents, JP2014193926’s specificity provides a competitive edge, but continued innovation and patent monitoring are essential.
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Future Outlook: As neurotherapeutics evolve, this patent can serve as a foundational asset for developing next-generation melatonin-based drugs and suggests areas for alternative innovation to avoid infringement.
FAQs
Q1: What are the main chemical features of the derivatives claimed in JP2014193926?
A1: The derivatives primarily feature specific substitutions on the indole ring and side chains to enhance pharmacokinetic and receptor-binding properties, notably halogen or methyl groups at particular positions.
Q2: Which therapeutic areas are primarily protected by this patent?
A2: The patent explicitly aims to cover treatments for sleep disorders, neurodegenerative diseases like Alzheimer’s and Parkinson’s, and conditions related to oxidative stress.
Q3: How does this patent compare with existing melatonin-related patents?
A3: JP2014193926 claims specific novel derivatives with targeted substitutions, potentially providing narrower yet more defensible protection compared to broader prior art covering general melatonin analogs.
Q4: Can the patent be circumvented?
A4: Yes, by designing derivatives with different substitution patterns or alternative molecular frameworks not covered by the claims, competitors can avoid infringement.
Q5: What is the commercial significance of this patent?
A5: It offers potential exclusivity over a class of melatonin derivatives that can be developed into therapeutics for sleep aids and neuroprotective drugs, representing valuable intellectual property in the CNS treatment market.
References:
[1] Japan Patent JP2014193926. Legal Status and Specification.
[2] US Patent US2015009584. Melatonin receptor agonists.
[3] JP2009191671. Indole derivatives for use in sleep regulation.
[4] FDA Approvals and Pharmacology Data on Ramelteon and Tasimelteon.
