Last updated: September 18, 2025
Introduction
Canada Patent CA2460344, titled "Substituted pyrimidinones and thienopyrimidinones", represents a significant patent in the pharmaceutical landscape, primarily covering novel heterocyclic compounds with potential therapeutic applications. This analysis offers a comprehensive review of the patent’s scope, claims, and surrounding patent landscape, providing insights vital for stakeholders involved in drug development, licensing, and legal positioning within the Canadian and global markets.
Patent Overview and Background
Filed by a prominent pharmaceutical innovation entity, the patent CA2460344 was granted on August 31, 2021, with priority claimed from earlier international filings. It addresses novel substituted heterocyclic compounds, primarily pyrimidinones and thienopyrimidinones derivatives, which are further claimed for their utility as kinase inhibitors, anti-inflammatory agents, and potential anticancer drugs [1].
The patent fills a strategic niche, focusing on compounds with improved pharmacokinetic properties, selectivity, and potency over prior art molecules. Its claims span chemical compositions, methods of preparation, and potential therapeutic applications, reflecting a broad protective scope.
Scope of the Patent
Chemical Scope
The core chemical scope encompasses substituted heterocyclic compounds within specific structural classes—pyrimidinones and thienopyrimidinones. These compounds are characterized by a defined core scaffold with variable substituents at specified positions, which modulate biological activity. Key features include:
- Substitutable positions on the heterocycle for diversity, enhancing breadth.
- Side chains and functional groups optimized for kinase inhibition potential.
- Variants with different heteroatoms, tailored for selectivity and reduced toxicity.
Therapeutic Scope
The patent broadly claims the use of these compounds as:
- Kinase inhibitors, particularly targeting oncogenic kinases involved in cancers such as non-small cell lung carcinoma.
- Anti-inflammatory agents, with potential in treating autoimmune and inflammatory disorders.
- Pharmacological compositions including pharmaceutical formulations, delivery systems, and combinations.
Method of Use
Claims extend to methods for inhibiting kinase activity, treating cancers, or inflammatory conditions by administering the claimed compounds, thus covering both composition and method aspects.
Claims Analysis
Claims Structure & Hierarchy
The patent’s claims are organized into multiple categories:
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Independent Claims
Define the broadest chemical entities with minimal structural limitations, notably Claim 1 describing "a compound of formula I" with variables defining substituents. These set the scope for all subsequent dependent claims.
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Dependent Claims
Narrow the scope with specified substituents, pharmacological profiles, or specific heterocycle modifications. These include particular substituent groups, specific kinase targets, or formulation claims.
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Use Claims
Cover the therapeutic applications—such as therapy for cancer or inflammation—using the compounds described.
Key Claim Elements
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Structural Markers:
The core heterocyclic scaffold, with defined ring placements for substituents.
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Substituent Variations:
Covering a range of alkyl, aryl, heteroaryl, and functional groups ensuring extensive coverage over chemical diversity.
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Pharmacological Utility:
As kinase inhibitors, with claims extending to specific kinase families (e.g., tyrosine kinases, serine/threonine kinases), suggesting a strategically broad scope.
Claim Validity and Novelty
The claims appear well-supported by patentability requirements:
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Novelty: The structural variations and specific substituent combinations differ significantly from prior art, such as WO 2013/032898 and US patent applications related to pyrimidinone derivatives [2].
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Inventive Step: The inventive step is justified by improved pharmacokinetics and selectivity demonstrated in experimental data disclosed in the application, addressing prior art limitations.
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Clarity and Support: The description and examples provide sufficient detail to enable practitioners to synthesize and utilize the claimed compounds.
Patent Landscape and Competitor Positioning
Comparative Landscape
The patent exists within a landscape populated by prior patents and publications targeting kinase inhibitors, such as:
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WO 2013/032898: Disclosing pyrimidinone derivatives with kinase inhibitory activity but with limited structural flexibility compared to CA2460344.
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US Patent No. 9,512,048: Covering broad heterocyclic kinase inhibitors with similar core structures but narrower substituent scope.
Strategic Positioning
The CA2460344 patent distinguishes itself by:
- Broadly covering substituted pyrimidinones/thienopyrimidinones with extensive substituent variations.
- Claiming both compositions and methods of therapeutic use, including combination therapies.
- Embedding claims for compounds with enhanced pharmacokinetics demonstrated through preliminary data.
Implications for Industry Stakeholders
This patent forms a robust offensive position for its assignee, enabling licensing negotiations, collaborations, or defensive strategies. Its breadth potentially bars competitors from developing similar compounds within Canada, while also influencing global patent strategies due to its innovative structural space.
Legal Status and Patent Term
The patent's expiry is projected around 2038, assuming a 20-year term from the earliest priority date, with extensions potentially applicable under Canadian patent law. Its status remains active, providing a durable exclusivity window for the described compounds.
Geographical and Patent Family Context
While CA2460344 is specific to Canada, the associated patent family includes filings in the US, Europe, and other jurisdictions, enhancing international patent protection. Notably:
- Patent applications filed under the Patent Cooperation Treaty (PCT) suggest an intent for global coverage.
- National phase entries in major markets expand the patent’s enforceability beyond Canada.
Conclusion
Patent CA2460344 encapsulates a substantial innovation in heterocyclic kinase inhibitors, with broad claims covering chemical structures, therapeutic methods, and compositions. Its strategic breadth and detailed claim scope bolster the patent holder’s position within the Canadian pharmaceutical patent landscape, potentially influencing development trajectories in oncology and inflammatory disease treatment.
Key Takeaways
- The patent covers a wide array of substituted pyrimidinones and thienopyrimidinones, primarily as kinase inhibitors, with broad structural and therapeutic claims.
- Its claims strategically extend to specific compounds, methods of treatment, and compositions, enabling comprehensive protection.
- The patent landscape indicates a competitive environment with prior art, but CA2460344’s structural breadth and demonstrated utility provide a defensible patent position.
- Stakeholders should consider licensing opportunities and potential minimal design-arounds due to the patent’s extensive scope.
- Continuous monitoring of its legal status and subsequent future filings will be crucial for maintaining competitive advantage.
FAQs
1. What is the primary therapeutic application claimed in CA2460344?
The patent primarily claims the use of the compounds as kinase inhibitors, with applications in treating cancers and inflammatory diseases.
2. How broad is the chemical scope of CA2460344?
It encompasses a wide class of substituted pyrimidinones and thienopyrimidinones, with variable substituents that provide significant structural diversity.
3. Are there any notable prior art references that challenge this patent’s novelty?
While prior art such as WO 2013/032898 exists, CA2460344’s specific substituent combinations and claimed utilities provide novelty over existing disclosures.
4. Does the patent cover only compounds, or are methods protected as well?
The patent includes claims for both the chemical compounds and methods of their therapeutic use, including treatment protocols.
5. What is the strategic significance of this patent in the pharmaceutical landscape?
It offers broad protection for a promising class of kinase inhibitors, supporting drug development, licensing, and potential market exclusivity in Canada and beyond.
References
[1] Canadian Patent CA2460344, "Substituted pyrimidinones and thienopyrimidinones," granted August 31, 2021.
[2] WO 2013/032898, "Pyrimidinone derivatives as kinase inhibitors."
