Last updated: July 31, 2025
Introduction
European Patent EP2376080, titled "Substituted pyrazolopyridazines and their use," exemplifies innovation in the realm of heterocyclic compounds with medicinal applications. Filed by Boehringer Ingelheim International GmbH, this patent encompasses compositions and methods aimed at therapeutic interventions, likely targeting diseases such as cancer, infectious diseases, or inflammatory conditions, consistent with the company's focus.
This analysis provides an in-depth review of the patent’s scope, claims, and its position within the patent landscape, with critical insights relevant for patent practitioners, R&D strategists, and stakeholders evaluating life sciences IP.
Scope of Patent EP2376080
Subject Matter and Technical Field
EP2376080 primarily protects substituted pyrazolopyridazines, a class of heterocyclic compounds with potential kinase inhibitory or other pharmacological activities. The patent broadens the scope to include:
- Chemical Compounds: Specific substituted pyrazolopyridazines, including various derivatives and their chemical structures.
- Pharmaceutical Compositions: Formulations comprising these compounds.
- Therapeutic Uses: Methods for treating diseases, especially where these compounds exhibit biological activity, notably kinase inhibition pathways.
Scope Boundaries
The patent’s scope encapsulates both compound claims—detailing specific molecular structures—and method claims for their use, including methods of treatment and manufacture. It specifies:
- Core Structures: Base pyrazolopyridazine skeletons with varied substituents.
- Substitutions and Derivatives: Functional groups permissible at specific positions, expanding the chemical space.
- Salts, Isomers, and Prodrugs: Inclusion of derivatives and pharmaceutically acceptable salts.
- Therapeutic Indications: Primarily targeting diseases where kinase activity plays a role, such as oncology, inflammation, or infectious diseases.
Legal Scope
The patent’s claims are designed to be broad yet sufficiently specific to withstand potential validity challenges. They reflect a balance between generality—covering a wide chemical space—and specificity—detailing the chemical structures essential for patentability.
Claims Analysis
Types of Claims
EP2376080 contains a structured hierarchy of claims:
- Independent Claims: Central claims defining core compounds and uses.
- Dependent Claims: Narrower claims adding specific substitutions, pharmaceutical formulations, or methods of use.
Key Claim Features
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Chemical Structure Claims:
- Cover basic pyrazolopyridazine scaffolds with substituents R1-R4, where each is defined broadly to encompass a wide chemical variant.
- Example: A claim might specify a pyrazolopyridazine core with at least one phenyl ring substituent, with further optional substituents.
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Pharmaceutically Acceptable Salts and Isomers:
- Claims extend protection to salts, stereoisomers, and prodrugs, ensuring comprehensive coverage.
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Methods of Treatment:
- Claims include administering these compounds for treatment of specific diseases, particularly those responsive to kinase inhibition.
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Use Claims:
- Claims covering the use of the compounds for manufacturing medicaments targeting particular conditions.
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Formulation Claims:
- Claims may also include pharmaceutical compositions, such as tablets, capsules, or injectable forms, involving the claimed compounds.
Claim Scope and Limitations
While broad, the claims are supported by a detailed description of the chemical structures, synthesis methods, and potential uses. The breadth aims to preempt infringements across a wide chemical and application spectrum but may be challenged if the scope is perceived excessively broad without sufficient inventive step or clarity.
Patent Landscape Context
Prior Art and Novelty
The patent’s novelty hinges on specific substituents and therapeutic applications not previously claimed. Prior art includes:
- Other pyrazolopyridazine-based compounds disclosed in patent databases and scientific literature (e.g., WO2010/094894, US7,712,987).
- Known kinase inhibitors with similar core structures.
Boehringer Ingelheim’s claims likely differentiate from prior art through specific substitutions, novel synthesis routes, or particular therapeutic claims.
Related Patents and Applications
The patent landscape showcases a robust cluster of filings covering heterocyclic kinase inhibitors, with various players such as Pfizer, Novartis, and Merck filing analogous patents. EP2376080 distinguishes itself through its particular compound claims and therapeutic scope.
Patent Families and Geographical Coverage
EP2376080 is part of a broader patent family, with counterparts filed in the US, China, and other jurisdictions. This global coverage indicates strategic protection, especially considering the high value of kinase inhibitor markets.
Freedom-to-Operate and Expiry Considerations
The patent is expected to have a standard 20-year term from the priority date (~2011), with potential adjustments for term extensions. It may face freedom-to-operate issues arising from overlapping claims in the field, especially if similar compounds are claimed elsewhere.
Conclusion
European Patent EP2376080 exemplifies a strategic patent combining broad claims on substituted pyrazolopyridazines with specific therapeutic applications, reflecting a typical approach in medicinal chemistry patenting. Its scope aims to foster robust protection for Boehringer Ingelheim’s innovations in kinase inhibitor therapies.
For stakeholders, understanding the nuances of these claims, the pathogen landscape, and the jurisdictional scope is essential for R&D pipelines, licensing strategies, and patent valuation.
Key Takeaways
- EP2376080’s claims encompass a wide array of substituted pyrazolopyridazines, including derivatives and pharmaceutical formulations, with specific therapeutic uses.
- The claim language balances broad chemical coverage with detailed structural limitations to withstand validity challenges.
- The patent landscape features intense competition among pharma giants, with prior art focusing on heterocyclic kinase inhibitors.
- Strategic patent family expansion across key jurisdictions enhances market position and licensing leverage.
- Continuous monitoring of overlapping claims and subsequent innovations is vital to safeguard freedom to operate.
FAQs
1. What distinguishes EP2376080 from previous patents on kinase inhibitors?
EP2376080 claims specific substituted pyrazolopyridazines with defined structural features and particular therapeutic uses, differentiating from prior art through unique substitution patterns and claimed indications.
2. How broad are the chemical claims in EP2376080?
The claims cover a wide chemical space, including various substituents on the pyrazolopyridazine core, salts, isomers, and derivatives, providing extensive protection.
3. Can the patent be challenged for obviousness?
Yes, if prior art discloses similar compounds with minor modifications, the patent could face validity challenges based on inventive step or obviousness.
4. How does this patent fit into Boehringer Ingelheim’s overall patent portfolio?
It adds a strategic layer for kinase inhibitor development, complementing other patents covering related compounds, formulations, and therapeutic methods.
5. What are the main risks for infringement based on this patent?
Potential infringement arises from manufacturing or using compounds falling within the claim scope, especially if derivatives or salts are employed in clinical or commercial settings without license.
Sources:
[1] European Patent EP2376080: "Substituted pyrazolopyridazines and their use."
[2] Patent family filings and priority documents.
[3] Scientific literature on heterocyclic kinase inhibitors.
[4] Patent landscape reports on kinase inhibitor compounds.
