Last updated: July 27, 2025
Introduction
Japan Patent JP2012502973, entitled “Method for Treating a Disease with a Selective Phosphodiesterase 4 (PDE4) Inhibitor,” pertains to the field of pharmaceutical compounds, particularly PDE4 inhibitors used for clinical indications such as inflammatory and neurological disorders. Analyzing this patent involves understanding its scope, claims, and its position within the broader patent landscape in the PDE4 inhibitor domain.
Patent Overview and Basic Data
- Filing & Publication Details:
JP2012502973 was published on April 26, 2012, and assigned to Astellas Pharma Inc., a leading pharmaceutical company specializing in inflammation and neurology therapeutics.
- Priority Data:
The priority filing dates and related applications may include U.S. or EP filings, often indicating strategic global protection.
- Patent Family:
The patent forms part of a larger portfolio targeting PDE4 inhibitors, correlating with Astellas’ significant R&D efforts in inflammatory and neurodegenerative treatments.
Scope and Main Claims Analysis
Scope of the Patent
The patent claims protection over specific chemical compounds classified as selective PDE4 inhibitors and their methods of use for treating diseases, notably inflammatory diseases and neurological disorders such as COPD, asthma, rheumatoid arthritis, or depression.
The scope prominently includes:
- Novel chemical structures (or derivatives thereof)
- Uses of these compounds in therapeutic methods for treating specific diseases
- Formulations including pharmaceutical compositions that incorporate the compounds
This broad scope underscores innovations in structure and application for PDE4 inhibitors, reflecting a strategic focus on compounds with high selectivity and safety profiles.
Claims Breakdown
The patent contains multiple claims categorized primarily as product claims and method claims:
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Chemical Compound Claims:
The core claims cover specific chemical entities with a defined molecular framework, including substituents, stereochemistry, and particular functional groups optimized for PDE4 inhibition.
Example:
"A compound represented by the following chemical formula (I)... wherein the variables are defined as..."
These claims delineate the chemical space claimed and are fundamental for preventing generic copying of these molecules.
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Use Claims:
These claims explicitly cover the therapeutic use of the compounds in treating inflammatory diseases and neurological disorders, such as COPD, rheumatoid arthritis, or depression.
Example:
"A method of treating a disease selected from the group consisting of COPD, asthma, and depression, comprising administering an effective amount of a compound as defined above."
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Pharmaceutical Formulations:
Claims also extend to compositions incorporating these compounds, covering dosage forms such as tablets, capsules, and inhalants.
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Method of Preparation:
Specific synthetic routes and intermediates may also be claimed, securing process protection alongside compound and use claims.
Distinctive Claims Features
- The claims emphasize selectivity for PDE4 over other phosphodiesterases, which reduces side effects such as nausea—a known concern with PDE4 inhibitors.
- The chemical structures claimed appear to be based on a heterocyclic scaffold, possibly a quinoline, quinazoline, or pyrimidine derivative, modified with specific substitutions to enhance pharmacokinetics and safety.
Patent Landscape in PDE4 Inhibitors
Global Patent Environment
The PDE4 inhibitor space is heavily patented, with seminal patents primarily from companies like GlaxoSmithKline (GSK), Astellas Pharma, AbbVie, and Ionis Pharmaceuticals. Notably:
- GSK’s Roflumilast (Daxas/Avanie):
Received FDA approval and embodies prior art in PDE4 inhibitor classes.
- Astellas’ Successors and Related Patents:
JP2012502973 is likely aligned with earlier Astellas patent applications (e.g., JP2007151578) targeting similar compounds.
Patent Landmarks and Competitive Positioning
- Cytokine modulation and selective PDE4 inhibitors like apremilast and roflumilast have established therapeutic standards.
- Patents such as EP2087081 or US20110166262 demonstrate extensive claims to compound classes and methods of treatment, potentially overlapping with JP2012502973.
JP2012502973 is part of a strategic patent cluster protecting specific chemical entities with potential advantages in selectivity, safety, and efficacy. It may operate as a blocking patent to secure market exclusivity for Astellas’ PDE4 inhibitor portfolio in Japan.
Legal and Strategic Considerations
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Claim Breadth and Validity:
The claims appear well-defined but must be scrutinized for novelty and inventive step against prior art, especially given the existence of multiple PDE4 inhibitor structures.
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Patent Term and Market Exclusivity:
Considering its publication date, the patent potentially extends patent rights into the late 2020s or early 2030s, assuming timely maintenance fees and no legal challenges.
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Potential Challenges:
The scope may face invalidation if prior disclosures exist or if inherently anticipated by earlier art. Conversely, the novelty could hinge on subtle structural modifications or specific therapeutic claims.
Conclusion
JP2012502973 exemplifies a targeted patent protecting novel PDE4 inhibitors tailored for inflammatory and neurological diseases. The patent’s scope emphasizes chemical novelty and therapeutic utility, strategically positioning Astellas in the competitive landscape of PDE4 inhibitor therapeutics. Its claims are crafted to extend protection not only over compound structures but also over treatment methods and pharmaceutical compositions, reinforcing market exclusivity.
Key Takeaways
- The patent’s chemical claims focus on specific, strategically designed PDE4 inhibitors with potential improved therapeutic profiles.
- Usage claims expand the patent’s scope across multiple disease indications, enhancing commercial value.
- The patent landscape is crowded; success depends on maintaining claim validity and avoiding prior art.
- Strategic patent filings like JP2012502973 are crucial for securing market share in a competitive pharmaceutical segment.
- Ongoing legal and patent landscaping vigilance is necessary to uphold exclusivity.
FAQs
1. What is the primary therapeutic application of the compounds claimed in JP2012502973?
The patent primarily targets the treatment of inflammatory diseases such as COPD, asthma, rheumatoid arthritis, and neurological disorders like depression, leveraging selective PDE4 inhibition.
2. How does JP2012502973 differ from prior PDE4 patents?
It claims novel chemical entities with specific structural features intended to increase selectivity and safety, potentially differentiating from earlier PDE4 inhibitors with broader or less selective activity.
3. Can the claims in JP2012502973 be challenged based on prior art?
Yes; patent challenges can be based on earlier disclosures of similar chemical structures or therapeutic methods. Patent validity often depends on demonstrating novelty and inventive step over existing art.
4. What is the strategic importance of this patent for Astellas Pharma?
It secures exclusive rights to a specific class of PDE4 inhibitors, supporting both development and commercialization efforts in inflammatory and neurodegenerative disease markets.
5. How does this patent fit within the global PDE4 inhibitor landscape?
It complements other patents from major companies by providing Japanese protection for specific chemical and therapeutic claims, supporting broader global patent strategies and market exclusivity.
References
- Japanese Patent JP2012502973 (Official publication, 2012).
- GSK Patent Portfolio on PDE4 Inhibitors.
- US Patent Application US20110166262.
- EPO Patent EP2087081.
- Market reports on PDE4 inhibitors and therapeutic patents.
