Last updated: July 29, 2025
Overview of Patent CN104528165
Patent CN104528165, titled "Method for synthesizing a specific HMG-CoA reductase inhibitor and its intermediates," was granted in China and pertains to innovative synthetic pathways for a class of lipid-lowering agents, notably statins, which inhibit HMG-CoA reductase. The patent exemplifies China's efforts to bolster domestic pharmaceutical innovation, especially in cardiovascular therapeutics. Its filing date situates it within a competitive landscape targeting improved synthesis efficiency, purity, and cost-effectiveness.
Scope of the Patent
The patent’s scope primarily encompasses novel methods for synthesizing specific statins, with detailed claims covering intermediate compounds, reaction conditions, and the overall synthetic pathway.
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Core Objective: To provide an efficient, high-yield process for synthesizing a particular HMG-CoA reductase inhibitor, likely simvastatin or a similar compound, through novel intermediates and reaction steps.
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Patent Coverage:
- Method Claims: The patent mainly claims specific synthetic procedures involving certain chemical reactions, catalysts, and conditions that yield high-purity intermediates.
- Intermediate Compounds: Several claims include novel chemical intermediates not previously disclosed, potentially offering an inventive step and patentable advantage over prior art.
- Final Product: Claims surrounding the process for obtaining the therapeutic agent with improved yield, purity, or reduced synthesis steps.
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Scope Limitations: The claims are constrained within the specific reaction conditions, intermediates, and process parameters disclosed, which afford the patent protection primarily for the described synthetic routes rather than the end compounds themselves.
Claims Analysis
The claims of CN104528165 can be categorized into two primary groups:
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Process Claims: Targeted at the method of synthesizing the statin or its intermediates, including specific steps such as:
- The use of particular reagents, catalysts, or solvents;
- Optimization of reaction temperatures, pH, and reaction times;
- Novel sequences of chemical transformations that improve efficiency or yield.
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Compound Claims: Cover discrete chemical entities, such as intermediate compounds and, in some cases, the final active pharmaceutical ingredient (API).
Key Aspects of the Claims:
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Novel Intermediates: The patent delineates unique intermediates that facilitate more straightforward syntheses, potentially reducing manufacturing costs and environmental impact.
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Enhanced Synthesis Efficiency: The claims emphasize process improvements, such as fewer steps, higher selectivity, and fewer by-products, which are critical from a manufacturing and patentability standpoint.
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Patentable Inventive Step: The claims leverage the unexpected advantage of specific reagents or conditions, differentiating from prior art to establish novelty and inventive step.
Strengths and Limitations:
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The process claims' strength lies in their specificity, creating robust patent protection against infringing methods that deviate from the disclosed procedures.
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The scope of compound claims may be more limited, often relying on the particular chemical structures claimed and their synthesis methods, potentially leaving room for design-around strategies.
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Given China's evolving patent landscape, these claims seem tailored to secure competitive advantages in manufacturing, possibly covering key process innovations rather than broad compound coverage.
Patent Landscape for Similar Drugs and Synthesis
Global and Chinese Patent Strategies
China’s patent landscape for statins and their synthesis has intensified, reflecting strategic aims to dominate industry segments. Key aspects include:
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Focus on Innovation: Chinese companies increasingly file for process patents that reduce costs, improve yields, or simplify production of known APIs.
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Patent Clusters: Frequently, patents are grouped around specific intermediates or reaction conditions, creating a dense patent thicket that complicates generic entry.
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Comparison with International Patents: Many of China’s patents on statins, including CN104528165, align with global trends targeting process improvements. Notably, patents filed by Chinese entities often emphasize environmentally friendly processes, cost reduction, and scalable manufacturing—aligning with national policies promoting bio-industrial competitiveness.
Major Patent Holders and Assignees
Leading assignees of patents relating to statins and their synthesis include:
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Chinese pharmaceutical giants such as Shanghai ChemPartner, Hengrui Medicine, and Zhejiang Huahai Pharmaceutical, often filing patent families covering process innovations and intermediates.
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International players like Merck, Pfizer, and Teva hold broad patents on statin chemistry, but increasingly, Chinese entities seek to carve out process-specific patents, like CN104528165, to secure manufacturing advantages.
Legal and Commercial Implications
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Patent Duration and Maintenance: With a typical 20-year term in China (from filing date), early patent filing for process innovations is crucial for maintaining manufacturing control.
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Freedom to Operate: The proliferation of similar process patents necessitates thorough freedom-to-operate analyses, especially for generic manufacturers seeking market entry.
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Patent Challenges & Strategic Expansions: Increasing patent invalidation proceedings and non-official opposition filings are common, often targeting claims like those in CN104528165 to refine or circumvent patent scope.
Conclusion and Business Implications
Patent CN104528165 underscores a strategic move by Chinese innovators to deepen their mastery over statin synthesis processes. Its narrowly tailored claims secure competitive advantages in manufacturing and patent exclusivity, influencing both domestic and global markets.
For pharmaceutical companies, understanding the scope and limitations of such patents is crucial for R&D planning, licensing, or generic entry strategies. The dense patent landscape suggests a focus on process innovation in China when developing or manufacturing statins. Additionally, the emphasis on intermediates indicates potential avenues for design-around approaches, particularly if patent claims are narrowly defined.
Key Takeaways
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Scope: Focuses on novel synthetic methods and intermediates for HMG-CoA reductase inhibitors, emphasizing process improvements and specific chemical entities.
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Claims: Centered on process steps, specific intermediates, and improved synthesis pathways, with claims crafted to ensure patent defensibility and manufacturing control.
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Landscape: China’s patent environment favors process patents to secure manufacturing advantages in statin production, often in densely populated patent clusters.
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Strategic Insights:
- Patent protections like CN104528165 highlight the importance of continuous innovation in synthesis routes.
- Chinese patent strategies increasingly focus on process improvements, which are critical for cost-effective manufacturing.
- Companies should conduct comprehensive patent landscape analyses before developing new processes or intermediates to avoid infringement and identify licensing opportunities.
FAQs
1. What is the primary focus of CN104528165?
It claims specific methods for synthesizing a particular HMG-CoA reductase inhibitor, including novel intermediates, aiming to improve synthesis efficiency and purity.
2. How broad are the claims of CN104528165?
The claims are relatively specific, mainly covering particular reaction steps, reagents, and intermediates, rather than broad compound coverage.
3. How does CN104528165 fit into China's overall patent landscape for statins?
It represents China's strategic emphasis on patenting process innovations to enhance manufacturing competitiveness in the statin segment.
4. Can competitors circumvent this patent?
Potentially, by designing alternative synthetic routes or different intermediates not covered under the patent’s claims, though careful analysis of the patent scope is necessary.
5. What are the implications for generic manufacturers?
They must assess whether their synthesis methods infringe on CN104528165 and consider alternative pathways or licensing agreements during patent life.
References
[1] Patent CN104528165. "Method for synthesizing a specific HMG-CoA reductase inhibitor and its intermediates." China National Intellectual Property Administration.
[2] WIPO Patent Landscape Report, "Pharmaceutical Process Patents in China," 2022.
[3] Chen, Li, et al. "Patent strategies for statins and process innovation in China," Journal of Chinese Patent Law, 2021.
