Last updated: July 30, 2025
Overview of EP2416779
European Patent No. EP2416779, titled "Substituted piperazine derivatives for the treatment of diseases, particularly neurological disorders," was granted by the European Patent Office (EPO) in 2012. The patent is assigned to Glaxo Group Limited, a prominent pharmaceutical innovator. It relates broadly to novel substituted piperazine compounds with therapeutic applications, especially targeting neurological conditions such as depression, schizophrenia, and anxiety disorders.
Scope of the Patent
1. Patent Coverage and Geographical Extent
EP2416779 grants exclusive rights within the European Patent Convention (EPC) territory—comprising over 38 member states—preventing third-party manufacturing, selling, or using of the claimed inventions without authorization for the patent’s validity duration, typically 20 years from the filing date (which was March 2, 2010).
2. Claims Overview
The core of the patent resides in its claims, which define the scope of protection. The claims of EP2416779 are structured into:
- Main (independent) claims covering the chemical compounds themselves,
- Dependent claims detailing specific embodiments, substituents, synthesis methods, or therapeutic applications.
Detailed Analysis of the Claims
A. Chemical Compound Claims
The patent claims a class of substituted piperazine derivatives characterized by specific chemical formulas. The general structure, a core piperazine ring with various substituents (e.g., aryl groups, alkyl chains, heteroatoms), is defined with broad parameters. For example, independent claim 1 typically includes:
- A piperazine core structure substituted with at least one aromatic or heteroaromatic group,
- Variations in side-chain lengths,
- Different halogen or alkyl substitutions.
The claims aim to encompass a broad chemical space to preempt generic compounds with similar structures.
B. Pharmacological and Therapeutic Claims
Beyond the chemical compounds, the patent claims their use in treating neurological or psychiatric conditions (e.g., depression, schizophrenia), possibly through mechanisms like serotonin or dopamine receptor modulation. Claims also specify methods of preparing these compounds and their pharmaceutical compositions.
C. Claim Scope and Breadth
The claims are deliberately broad, covering multiple structural variants to secure comprehensive protection. However, they are constrained by the requirement to meet novelty, inventive step, and industrial applicability criteria. The breadth aims to deter third-party generic competitors from developing similar compounds without infringing.
Patent Landscape and Prior Art Considerations
1. Similar Patents and Patent Families
EP2416779 is part of a patent family involving filings in the US, Japan, and other jurisdictions. It aligns with GlaxoSmithKline’s broader R&D programs on CNS-active agents. Patent landscapes reveal a proliferation of patents on piperazine derivatives, with several related to antipsychotics and antidepressants.
2. Prior Art and Novelty
The patent navigates the complex landscape of prior art, including:
- Earlier piperazine derivatives disclosed in patents such as US 2005/0247813, which describe similar compounds for CNS disorders.
- Scientific literature prior to 2010 detailing substituted piperazines and their pharmacological properties.
To establish novelty, the patent emphasizes specific substituents and their unexpected pharmacological effects, which allegedly differ from prior compounds.
3. Inventive Step Analysis
The patent claims an unexpected therapeutic advantage—improved efficacy or reduced side effects—over existing drugs like risperidone or olanzapine, which underpins its inventive step argument.
4. Patent Litigation and Challenges
While no major litigations against EP2416779 are publicly documented, the broad claims may invite challenges under Article 100 EPC grounds (lack of novelty or inventive step). Competitors may contest if they demonstrate prior art disclosing similar compounds or effects.
Implications for Stakeholders
Pharmaceutical Developers:
The patent provides a substantial exclusivity window for developing novel CNS drugs based on the claimed compounds, incentivizing investment in clinical trials.
Generic Manufacturers:
The broad scope and related prior art landscape suggest potential for patent workarounds or invalidation challenges, especially if future prior art emerges that predates the patent’s priority date or claims.
Legal and Patent Strategists:
Understanding the scope helps in designing around strategies, such as designing compounds outside the scope of claims or challenging the patent’s validity based on prior art.
Conclusion and Outlook
EP2416779 secures robust protection over a broad class of substituted piperazine derivatives aimed at neurological disorders. Its claims leverage structural diversity and pharmacological utility to defend its scope, with a landscape characterized by competing prior art and ongoing patent applications. Continued scrutiny and potential challenges could influence its enforceability, emphasizing the importance of strategic patent prosecution and vigilant patent landscaping.
Key Takeaways
- The patent covers a wide range of substituted piperazine derivatives for CNS therapeutic use, providing a strong IP position for GlaxoSmithKline until around 2030.
- Its broad claims require careful navigation around prior art, which includes prior scientific disclosures and patents on similar compounds.
- Competitive advantage lies in the claimed compounds’ enhanced efficacy and reduced side effects, justifying the patent’s inventive step.
- Patent enforcement and potential challenges depend heavily on the evolving landscape of prior art and patent invalidation proceedings.
- Ongoing research and new patent filings could shape the future patent landscape, affecting the scope and value of EP2416779.
FAQs
Q1: How broad are the chemical scope and claims within EP2416779?
A1: The claims cover a wide array of substituted piperazine derivatives with various substituents, significantly broadening the scope to encompass numerous potential compounds for neurological applications.
Q2: What are the main therapeutic claims associated with this patent?
A2: The patent claims the use of the compounds for treating neurological and psychiatric disorders such as depression, schizophrenia, and anxiety, by modulating neurotransmitter receptors.
Q3: Can competitors develop similar drugs without infringing on this patent?
A3: Yes, if they design compounds that fall outside the scope of the claims—either through structural modifications or by targeting different mechanisms—although this requires careful patent landscape analysis.
Q4: How does prior art impact the validity of EP2416779?
A4: Prior art disclosures of similar compounds or uses could challenge the novelty or inventive step of the patent, potentially leading to its invalidation, especially if new disclosures emerge.
Q5: What strategic considerations should patent owners and licensees have regarding this patent?
A5: They should monitor ongoing patent filings, defend against potential challenges, and consider patent-expiry strategies to maximize market exclusivity and avoid infringement issues.
References
- European Patent EP2416779 B1. (2012). Substituted piperazine derivatives for CNS disorders.
- Prior art references detailing piperazine derivatives (e.g., US 2005/0247813).
- Scientific literature on piperazine compounds and their pharmacological effects.
