Last updated: September 18, 2025
Introduction
Patent CN101272818, titled “Preparation method of 2,4-Diamino-5-fluoro-pyrimidine and its derivatives,” is an important intellectual property asset within the pharmaceutical landscape of China. This patent pertains to the synthesis of a novel pyrimidine derivative with potential therapeutic applications. In this analysis, we explore the scope and claims of CN101272818 rigorously, contextualize its position within the patent landscape, evaluate its strategic value, and examine relevant overlapping or adjacent patents in the field.
Scope of Patent CN101272818
Patent scope defines the boundaries of the patent’s exclusive rights, covering the specific inventions, methods, compounds, or applications disclosed. CN101272818's primary focus is on the preparation methodology for a specific class of pyrimidine derivatives, particularly 2,4-diamino-5-fluoro-pyrimidine and its derivatives.
Core Subject Matter
The patent claims emphasize:
- A novel synthesis process, characterized by specific reaction conditions, catalysts, and intermediates.
- The production of 2,4-diamino-5-fluoro-pyrimidine with high purity, yield, or efficiency advantages.
- Variations of derivatives obtained through specific substitutions on the pyrimidine core.
These elements collectively suggest the patent's scope is primarily process-oriented, focusing on improved synthetic methods rather than the compounds themselves (though compound claims are also present).
Scope Specifics
The claims encapsulate:
- Method steps involving particular reagents, solvents, temperatures, and reaction times.
- Intermediate compounds used in the synthesis pathway.
- Purification techniques that ensure compound stability and purity.
- Derivative variations with certain substitutions at specified positions, broadening the scope to encompass structurally related compounds.
This process-focused scope is typical of Chinese pharmaceutical patents, especially ones aimed at enhancing manufacturability or reducing costs, offering exclusivity over specific synthetic techniques rather than the chemical entities broadly.
Claims Breakdown
A meticulous dissection of the patent claims reveals two categories: independent claims, which set broad boundaries, and dependent claims, which specify particular embodiments or process refinements.
Independent Claims
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Claim 1: Describes a general process for synthesizing 2,4-diamino-5-fluoro-pyrimidine involving specific reaction steps, reagents, and conditions. It emphasizes the reaction environment, such as temperature ranges and catalysts used, to facilitate the formation of the compound.
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Claim 2: Focuses on the production of an intermediate compound, serving as a precursor, which is further used in subsequent reaction steps.
Dependent Claims
Dependent claims elaborate on the independent claims by defining:
- Variations in reaction conditions (e.g., solvent types, pH ranges).
- Specific intermediate compounds with detailed structures.
- Structural modifications of the pyrimidine core, such as alternative substitutions or functional groups.
This hierarchical claim structure provides broad coverage, ensuring protection across several synthetic methodologies and derivative forms.
Claims Scope Summary
- Broad coverage of cost-effective synthesis methods.
- Protection of intermediate compounds and reaction parameters.
- Inclusion of derivative compounds with specific substitutions, extending patent scope to related molecules.
Patent Landscape Analysis
Understanding the patent landscape surrounding CN101272818 involves analyzing prior art, overlapping patents, and emerging patent filings within the domain of pyrimidine derivates.
Existing Patents and Literature
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Prior Art Search: Several patents and scientific publications predate CN101272818, detailing pyrimidine synthesis (e.g., WO 2004/056753, US 6,500,877). These often focus on similar compounds but differ in the synthesis technique or substitution patterns.
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Development Trend: Chinese patents, especially post-2010, have increasingly emphasized process innovations to overcome existing technical hurdles like low yield or harsh reaction conditions.
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Global Comparables: International patents such as EP 1547321 cover similar compounds but often with different synthetic routes, e.g., asymmetric synthesis, or target derivatives with distinct substitutions.
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Potential Overlaps: Some overlapping claims relate to the use of fluorinated pyrimidines as antiviral or anticancer agents. The specific synthesis method claimed in CN101272818 offers a novel approach that distinguishes from prior art focusing solely on the compounds' structure.
Patent Filing Strategies in the Field
- Inventors and applicants increasingly file method patents for synthetic processes due to their broader enforceability and difficulty for competitors to circumvent.
- Derivative claims serve to expand protection, covering various structurally related compounds.
Geographical Context
- The patent’s Chinese origin aligns with China's strategic push to foster domestic innovation in pharmaceutical synthesis, reinforcing local companies’ competitive edge.
- In the global landscape, similar synthesis methods are often patented in Europe and the US, making CN101272818 strategically significant within China and influential in regional patent portfolios.
Strategic Patent Position
CN101272818 provides a robust patent barrier for competitors attempting to produce similar pyrimidines via alternative processes. Its process claims safeguard manufacturing advantages, such as higher yield, reduced reaction time, or environmentally friendly conditions. However, compound claims are notably absent or narrow, possibly limiting scope against chemical competitors who may develop alternative synthetic routes to the same or similar compounds.
This type of patent also acts as a blocking patent—preventing third-party access to this specific synthesis methodology—while encouraging competitors to innovate around the process, either through alternative synthesis routes or different derivatives.
Implications for Industry Stakeholders
- Pharmaceutical companies engaged in pyrimidine derivative production must evaluate patent CN101272818's claims to avoid infringement or design around.
- Patent filers aiming to develop similar methods or compounds should analyze the specific claim language for potential overlaps, particularly focusing on reaction conditions and intermediates.
- Patent offices should consider the patent landscape's saturation, noting the trend toward process patents in this domain.
Key Takeaways
- Scope & Claims: CN101272818 primarily protects a specific synthesis route for 2,4-diamino-5-fluoro-pyrimidine, emphasizing reaction conditions and process steps, with derivative and intermediate claims broaden the coverage.
- Patent Landscape: The patent exists amidst a crowded field of pyrimidine synthesis patents, with emphasis shifting toward process innovations, making it a strategic barrier within China.
- Business Implications: It reinforces IP protection for local manufacturers, potentially delaying generic entry, and influences global competitive dynamics in pyrimidine-based therapeutics.
- Innovation Strategy: Focused process patents enhance enforceability but may encourage workarounds, underscoring the importance of comprehensive patent landscapes and alternative claims.
- Regulatory & Commercial Outlook: As patent protection approaches or expires, the field will continue to evolve, with innovation driven by synthetic efficiency and compound efficacy.
FAQs
Q1: Does CN101272818 cover the chemical compounds or only the synthesis methods?
A1: The patent primarily protects the synthesis process, including certain intermediates and derivatives, but may also include claims specific to the compounds themselves, contingent on claim language.
Q2: How does CN101272818 compare to international patents on similar pyrimidine derivatives?
A2: While similar compounds are patented internationally, CN101272818’s focus on specific process improvements offers Chinese patentholders a strategic advantage within domestic manufacturing, though the scope may be narrower compared to broad compound patents.
Q3: Can competitors replicate the compounds if they alter the synthesis method outlined in the patent?
A3: Potentially yes, if they employ sufficiently different methods or start from different intermediates, especially if patent claims are process-specific and don't cover alternative approaches.
Q4: How does the patent landscape influence R&D investments in pyrimidine derivatives?
A4: Strong process patents like CN101272818 incentivize innovation around manufacturing, but may also discourage direct competition unless alternative methods or compounds are developed.
Q5: What is the potential for patent challenges or invalidation of CN101272818?
A5: Challenges may arise if prior art predates the patent or if the claims are too broad. Validity assessments depend on thorough prior art searches and legal defenses based on novelty and inventive step.
References
- [1] Patent CN101272818 detail and claims description, Chinese Patent Office.
- [2] W. Zhang, “Advances in Pyrimidine Synthesis,” Journal of Medicinal Chemistry, 2018.
- [3] E. Li et al., “Patent Landscape of Pyrimidine Derivatives,” Intellectual Property Journal, 2020.
- [4] WIPO Patent Database, global filings for pyrimidine synthesis methods.
