Last updated: August 2, 2025
Introduction
Canada Patent CA2543353, titled “Compound and pharmaceutical compositions,” was granted to Pfizer Inc. on May 16, 2014. It covers a novel class of chemical compounds, purportedly with therapeutic applications, particularly in the field of inflammatory and neurodegenerative disorders. This analysis aims to dissect the patent's scope, claims, and its position within the broader patent landscape, providing insights valuable to stakeholders involved in drug development, licensing, or legal strategy.
Patent Overview
Publication Details:
- Patent Number: CA2543353
- Filing Date: June 24, 2008
- Issue Date: May 16, 2014
- Applicants: Pfizer Inc.
- Priority Data: U.S. application 12/119,308 (filed May 9, 2008)
Abstract Summary:
The patent describes unique heterocyclic compounds, their pharmaceutical compositions, and methods of use, primarily targeting inflammatory pathways, including modulation of cytokine production.
Scope of the Patent
Core Focus:
CA2543353 encompasses a class of heterocyclic molecules characterized by a central pyrazoline or related core, having specific substituents designed to optimize biological activity. The patent also covers pharmaceutical compositions containing these compounds and their use in treating inflammatory, neurodegenerative, or autoimmune diseases.
Legal Scope:
The claims are crafted to broadly cover the chemical structures of the compounds, their derivatives, pharmaceutical compositions, and methods of treatment, with a focus on inhibiting cytokine activity (notably TNF-alpha, IL-6). This broad language ensures comprehensive coverage of the targeted chemical space and potential therapeutic applications.
Claims Analysis
Independent Claims:
The patent features multiple independent claims, primarily:
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Chemical Composition Claims: Covering the classes of heterocyclic compounds with specific structural features, such as certain substituents attached to the core heterocycle. These claims establish a broad chemical space.
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Method of Use Claims: Cover methods of treating inflammatory and autoimmune diseases using the compounds, including administration routes and dosages.
Dependent Claims:
These specify particular compounds within the claimed chemical classes, specific substituents, or combination therapies, narrowing the scope for certain embodiments.
Key Features of the Claims:
- Structural Breadth: The claims generally encompass a wide range of substituents, allowing for multiple structural variations within the claimed chemical space.
- Therapeutic Indications: Claims extend to methods for modulating cytokine levels, indicating the patent’s emphasis on anti-inflammatory and immunomodulatory applications.
- Formulations and Administration: The patent also claims pharmaceutical formulations, including oral, injectable, or topical forms.
Strengths and Limitations:
While the broad claim language enables extensive protection, it also subjects the patent to potential challenges based on prior art that discloses similar heterocyclic scaffolds. The specificity of dependent claims helps augment enforceability in case of infringement disputes.
Patent Landscape and Competition
Related Patents:
The patent exists within a crowded landscape of anti-inflammatory compounds. Notably:
- Other heterocyclic compounds: Several compounds with similar scaffolds, such as pyrazolines or imidazoles, have been disclosed in prior art (e.g., WO2007017151, US patent applications by other entities).
- Biologics and Small Molecule Inhibitors: The field includes monoclonal antibodies like adalimumab and small molecule inhibitors targeting cytokines or kinases.
Patent Family and Continuations:
Pfizer maintains a robust portfolio of similar compounds and method patents. Continuous filings and continuation applications aim to extend patent life and territory coverage, aligning with strategic exclusivity goals.
Limitations and Challenges:
Patent validity may be challenged on grounds of obviousness, particularly given the prevalence of heterocycle-based anti-inflammatory agents. The scope’s reliance on a broad chemical class must be supported by detailed experimental data to withstand such challenges.
Implications for Stakeholders
For Innovators:
Recognition of the broad chemical scope and therapeutic claims suggests an opportunity to develop or improve upon similar heterocyclic compounds within this intellectual property framework. Careful analysis of prior art is necessary to identify carve-outs or gaps.
For Patent Holders:
Maintaining patent strength depends on continuously expanding claims through continuations and covering emerging therapeutic targets or formulations.
For Competitors:
The patent delineates a protected chemical space centered on specific heterocycles. Designing compounds outside the scope, or challenging the patent’s validity, requires in-depth prior art review, especially related to heterocyclic chemistry.
Regulatory and Clinical Impacts:
Claims covering methods of treating inflammatory conditions position the patent as a strategic asset for commercializing anti-inflammatory drugs based on these compounds, potentially affecting pipeline development and licensing negotiations.
Legal Status and Market Relevance
Legal Status:
As of recent records, the patent’s maintenance status appears intact, with no publicly documented challenges or oppositions. It remains a strong patent in Pfizer’s portfolio for anti-inflammatory compounds.
Market Relevance:
While Pfizer has no approved drugs directly linked to this patent, the protected compounds inform ongoing research and development activities. Their utility in immune modulation signals potential future therapeutic products, especially given the global emphasis on treating inflammatory and autoimmune disorders.
Key Takeaways
- Broad Chemical Scope: CA2543353’s claims encompass a wide array of heterocyclic compounds with anti-inflammatory potential, maximizing market exclusivity.
- Strategic Patent Position: Pfizer’s extensive patent coverage within this space supports downstream drug development, licensing, and potential litigation.
- Challenges and Caveats: The broad claims face potential invalidity challenges from prior art, necessitating robust supporting data and precise claim drafting.
- Market and Therapeutic Impact: The patent’s claims could underpin future drugs targeting cytokine pathways, fitting into a high-growth segment of personalized immunotherapy.
- Continued Portfolio Development: Ongoing patent filings and patent family expansion are essential to uphold competitive advantage.
FAQs
1. What is the primary therapeutic target of the compounds claimed in CA2543353?
The compounds primarily target cytokines like TNF-alpha, IL-6, and other mediators involved in inflammatory and autoimmune responses.
2. How broad are the chemical claims in this patent?
The claims encompass a wide structural class of heterocyclic compounds with various substituents, making them highly inclusive but potentially vulnerable to prior art challenges.
3. Are any of the compounds disclosed in this patent currently marketed drugs?
No; while the compounds are promising therapeutics, no directly marketed drugs are based solely on this patent’s claims. They serve more as a strategic patent covering potential future products.
4. How does this patent fit into Pfizer’s broader anti-inflammatory portfolio?
It forms part of Pfizer’s intellectual property estate targeting novel anti-inflammatory agents, complementing biologics and small molecule inhibitors to secure a competitive edge.
5. Can competitors develop similar compounds without infringing CA2543353?
Yes; by designing chemical structures outside the patent’s scope—either structurally or functionally—competitors can pursue alternative avenues, though they must ensure novelty and non-infringement.
References
- World Intellectual Property Organization. Patent WO2007017151 – "Heterocyclic Compounds" (prior art related to heterocycle-based anti-inflammatory agents).
- Patent CA2543353, Public Record.
- Pfizer Inc. Official patent filings and publication records.
- Industry reports on cytokine-targeting therapies and heterocyclic compound development.
In conclusion, Canada patent CA2543353 exemplifies a strategic, broad-spectrum patent in the anti-inflammatory drug space, offering extensive protection for heterocyclic compounds with potential therapeutic applications. Its position within Pfizer’s portfolio underscores the importance of such patents in shaping future drug development and competitive dynamics in immunomodulatory therapies.
