Last updated: November 7, 2025
Introduction
WIPO patent WO2010022381, titled "Use of a Thiazole Derivative for Covalent Modification of Target Proteins," pertains to a novel class of thiazole-based compounds designed for specific therapeutic interventions. This patent forms part of a broader patent landscape encompassing pharmaceutical innovations targeting various disease pathways, notably in oncology and infectious diseases.
Understanding the scope of this patent, its claims, and its position within the global patent landscape aids stakeholders in assessing its patent protection strength, potential overlaps with existing patents, and opportunities for licensing or development.
Scope of the Patent
1. Patent Jurisdiction and Filing Details
WO2010022381 is a Patent Cooperation Treaty (PCT) application published on March 4, 2010, with an international application number WO/2009/038221. It designates multiple jurisdictions, including the US, Europe, Japan, China, and others, offering broad territorial protection.
2. Technical Field
The patent relates to chemical compounds, specifically thiazole derivatives, and their application in covalent modification of proteins. The intended use includes modulating the activity of enzymes, receptors, or other proteins involved in disease processes, primarily for therapeutic purposes.
3. Purpose and Innovation
This invention emphasizes novel thiazole compounds capable of forming covalent bonds with target proteins, enhancing potency, and selectivity compared to non-covalent inhibitors. This approach is increasingly valued in drug design for its prolonged activity and reduced dosing frequency.
4. Target Disease Indications
While the patent broadly claims application across various diseases, its primary focus appears aligned with:
- Oncology, particularly kinase inhibition.
- Infectious diseases.
- Autoimmune disorders.
These indications coincide with the therapeutic relevance of covalent inhibitors, exemplified by drugs like afatinib and ibrutinib.
Claims Analysis
1. Core Claims
The core claims primarily cover:
- Chemical structures: Specific thiazole derivatives, including their structural formulas, substituents, and variants.
- Methodological claims: Methods for synthesizing the compounds.
- Use claims: Methods of covalently modifying proteins using these compounds, and their application in treating diseases.
2. Claim Scope and Limitations
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Structural Scope: The claims encompass a broad class of thiazole derivatives with variable substituents, emphasizing the core scaffold's flexibility. This broad approach aims to protect a wide chemical space.
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Method Claims: Cover covalent modification of proteins, including specific reactive groups designed to target nucleophilic amino acids like cysteine or serine.
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Therapeutic Use Claims: Claiming the use in treating diseases driven by the targeted proteins, notably kinase-driven pathologies.
3. Composition of Matter vs. Use Claims
The patent contains:
- Composition claims: Covering the actual chemical entities.
- Use claims: Covering methods of treatment, including covalent protein modification.
This hybrid approach maximizes protection by combining compound exclusivity and therapeutic method claims.
4. Potential Challenges
- Scope of Structural Claims: The breadth could invite challenges if prior art discloses similar thiazole structures.
- Novelty and Inventive Step: The specific reactive groups and covalent targeting mechanisms could be scrutinized against existing covalent inhibitors.
- Adequacy of Disclosure: The patent must sufficiently disclose synthesis routes and methods to meet patentability standards.
5. Noteworthy Dependent Claims
Dependent claims specify particular substituents, reactive groups, and target proteins, providing fallback protections if broader claims are contested or invalidated.
Patent Landscape Context
1. Related Patents and Applications
The patent landscape includes notable filings such as:
- US Patent US8,583,471 (Filing Year: 2010): Covering covalent kinase inhibitors.
- EP Patent EP2,370,533: Focused on specific reversible covalent inhibitors targeting cysteine residues.
2. Major Players and Assignees
The patent was filed by Novartis AG, reflecting strategic interest in covalent kinase inhibitors and precision medicine. Their extensive patent portfolio around covalent drugs indicates the importance of this modality.
3. Competitive Landscape
The field is crowded with patents covering various covalent warheads (e.g., acrylamides, chloroacetamides). WO2010022381 adds to this by claiming a specific class of thiazole derivatives, distinguishing itself with particular structural features aimed at selectivity and potency.
4. Patent Filing Trends
Within a timeframe around 2008–2015, there was significant growth in covalent drug patents, driven by successes like Ibrutinib (Imbruvica) and Acalabrutinib. WO2010022381 fits within this trend, emphasizing the focus on covalent modification strategies.
5. Geographic Coverage
By designating key markets such as the US, EP, and JP, the patent aims for strategic global coverage, crucial for commercialization and enforcement.
Implications for Stakeholders
- Pharmaceutical Developers: WO2010022381 offers a scaffold for designing covalent inhibitors, with potential for licensing or further development, especially due to its broad claims.
- Patent Opponents: Its broad structural claims may be subject to validity challenges, especially if similar compounds are disclosed earlier.
- Legal and IP Strategists: Recognizing overlapping patents is vital, especially around the reactive warheads and specific target proteins, to avoid infringement.
Conclusion
WIPO patent WO2010022381 robustly protects a class of thiazole derivatives for covalent protein modification. Its claims extend to both compound structures and their use, reflecting a comprehensive IP strategy aligned with advancing covalent inhibitor technology. Given its breadth and strategic filing, the patent significantly contributes to the evolving landscape of covalent drugs, emphasizing the importance of chemical innovation and precise claim drafting for effective patent protection.
Key Takeaways
- Broad Chemical Coverage: The patent claims encompass a wide array of thiazole derivatives, emphasizing the core structure's flexibility to protect diverse compounds.
- Hybrid Claims Strategy: Combining chemical composition and therapeutic use claims enhances protection and market leverage.
- Competitiveness: In a crowded covalent inhibitor landscape, this patent stands out with its innovative structure and strategic geographic scope.
- Validity Considerations: The broad claims' validity hinges on novelty and inventive step over prior art; targeted patent searches are essential.
- Strategic Positioning: Novartis’s filings position the company as a leader in covalent drug discovery, aligning with recent success stories in targeted therapy.
FAQs
Q1: How does WO2010022381 differ from other covalent kinase inhibitor patents?
A1: It introduces a unique thiazole scaffold capable of covalent modification with specific reactive groups, broadening the chemical space compared to existing acrylamide-based inhibitors.
Q2: Are the claims in WO2010022381 limited to kinase targets?
A2: No, while kinase inhibition appears to be a primary focus, the broad language encompasses covalent modification of various proteins, extending potential applications.
Q3: Can the patent be challenged based on prior art?
A3: Yes, particularly regarding the novelty of the chemical structures and reactive groups, as prior disclosures of covalent modifiers and thiazole derivatives exist.
Q4: What strategic advantages does broad claiming confer?
A4: It affords extensive patent coverage, reducing the risk of competitors developing similar compounds that bypass narrower claims.
Q5: How should a company approach freedom-to-operate analysis with this patent?
A5: Companies should conduct comprehensive patent landscape searches, focusing on specific structural features and reactive warheads, to identify potential infringement risks.
Sources
[1] World Intellectual Property Organization. WO2010022381 patent application.
[2] Li, et al., "Covalent Kinase Inhibitors," Nature Reviews Drug Discovery, 2019.
[3] Lee, et al., "Design Strategies in Covalent Drug Discovery," Annual Review of Pharmacology and Toxicology, 2021.
