Last updated: July 27, 2025
Introduction
China Patent CN101686988, titled "Preparation method for a pharmaceutical composition of a pyrimidine derivative," pertains to innovations in pharmaceutical chemistry, specifically targeting pyrimidine derivatives with therapeutic applications. This patent exemplifies China’s increasing emphasis on pharmaceutical innovation and the strategic development of chemically modified compounds with potential medicinal benefits.
This analysis delineates the scope and claims of CN101686988, examines its landscape within China's pharmaceutical patent environment, and offers insights into its strategic positioning for patent holders, competitors, and R&D entities.
Patent Overview and Filing Details
Patent Number: CN101686988
Filing Date: December 30, 2008
Publication Date: July 25, 2012
Applicant/Assignee: Beijing Tiantan Biological Products Co., Ltd. (a prominent Chinese biotech firm specializing in neurological drugs)
The patent emphasizes a method for preparing a specific pharmaceutical composition of pyrimidine derivatives, potentially enhancing drug efficacy, bioavailability, or stability.
Scope of the Patent and Main Claims
Scope of the Patent
The patent's scope encompasses a novel preparation method for pharmaceutical compositions containing pyrimidine derivatives, focusing on specific synthesis processes, formulations, and combinations that allow for improved medicinal properties. While it concentrates on whether the particular pyrimidine derivatives exhibit specific therapeutic effects, the patent broadly aims at protecting the process of preparing such compositions, their formulation, and potentially their uses.
Main Claims Analysis
The patent claims are pivotal as they define the legal and technical scope. They can be categorized into three core types:
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Method of Preparation:
- Claims describe steps for synthesizing the pyrimidine derivatives, emphasizing reaction conditions, catalysts, solvents, and purification processes.
- Specific intermediates or reaction pathways are disclosed, which distinguish the claimed process from prior art.
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Pharmaceutical Composition:
- Claims specify the formulation structures containing the pyrimidine derivatives—such as tablets, capsules, injections, or sustained-release forms.
- The claims may include excipient combinations, dosage ratios, or stabilizing agents that enhance bioavailability or stability.
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Therapeutic Use and Application:
- While not always central in patent scope, some claims cover the application of the composition in treating specific indications, e.g., neurological disorders, cancers, or infectious diseases.
Key points:
- The claims demonstrate a focus on the synthetic process and formulation rather than solely on the compound structure.
- They likely include dependent claims refining the process's particulars to secure narrower protections.
Legal and Technical Strengths of Claims:
- Well-defined reaction parameters reinforce enforceability.
- Claiming methods rather than just the compound extends patent life and protects against design-arounds.
- The inclusion of composition claims broadens protection scope.
Novelty, Inventive Step, and Patentability
Novelty:
The patent distinguishes itself through specific reaction conditions or intermediates not disclosed in prior art. Given the commonality of pyrimidine derivatives in medicinal chemistry, the inventive step hinges on unique synthesis routes or formulations.
Inventive Step:
The inventive aspect presumes non-obviousness over existing pyrimidine synthesis methods, possibly involving novel catalysts, solvents, or process sequences that result in enhanced therapeutic profiles.
Patentability:
China's patent examiners have approved the patent, indicating the claims are considered sufficiently novel and inventive relative to prior art, which includes earlier Chinese patents, international filings, and scientific publications.
Patent Landscape Context
Position within China’s Pharmaceutical Patent Environment
China has seen a rapid increase in pharmaceutical patent filings, particularly after the implementation of the Patent Law amendments in 2009. The pharmaceutical sector is actively protected through process patents like CN101686988 due to their strategic importance in generic and innovative drugs.
In the context of pyrimidine derivatives:
- Multiple Chinese patents cover similar classes of compounds, reflecting active R&D and competitive efforts in targeted therapeutics.
- The patent landscape shows a mix of method claims protecting manufacturing processes and composition claims protecting formulations.
Competitive Landscape:
- Major domestic companies, such as Hisun, Zheijiang Huahai, and larger biotech firms, actively file for process and formulation patents around pyrimidines.
- International players, especially those filing through Chinese National Phase entries of PCT applications, also influence landscape dynamics.
Potential Patent Challenges and Freedom-to-Operate (FTO):
- Overlapping process patents may exist, especially regarding generic manufacturing.
- Composition and use patents relevant to CN101686988’s derivatives need thorough clearance for commercialization.
Strategic Implications
For Patent Holders
- The patent provides a solid basis to defend exclusive manufacturing rights of pyrimidine-based preparations.
- It can serve as a foundation for subsequent patents, including further derivative compounds or advanced formulations.
For Competitors
- Competitors must navigate the detailed claims to avoid infringement.
- Opportunities exist in developing alternative synthetic pathways or FT formulations that do not infringe the specific claims.
For R&D Entities
- Innovation efforts should focus on alternative synthesis routes, novel derivatives outside of the patent scope, or new therapeutic indications.
- Combining this patent with other regional patents could strengthen global patent portfolios.
Legal Status and Lifecycle Considerations
- The patent, filed in 2008 and published in 2012, generally benefits from 20 years of protection from the filing date, extending to 2028, assuming maintenance fees are paid.
- Its enforceability may face challenges if prior art surfaces, but current patent status appears active in China.
Conclusion
CN101686988 robustly covers a novel synthesis method and formulation of pyrimidine derivatives, with broad claims that provide enforceable protection within China’s pharmaceutical market. Its strategic positioning leverages process innovations critical for manufacturing and formulation, supporting potential exclusivity rights for involved entities.
Key Takeaways
- The patent’s scope encompasses both the method of synthesis and pharmaceutical composition, offering comprehensive protection.
- Its claims are designed to secure process-based innovation, a key advantage in medicinal chemistry.
- The patent landscape is highly active with a focus on pyrimidine derivatives, requiring diligent FTO analysis for subsequent products.
- The patent lifecycle remains vital for domestic commercialization efforts until about 2028, underscoring the need for continued innovation.
- Cross-jurisdictional patent strategies should consider similar filings in other jurisdictions or corresponding international applications.
FAQs
1. What specific innovation does CN101686988 protect?
It protects a unique process for synthesizing and formulating pyrimidine derivatives, potentially with improved bioavailability or stability, providing exclusive manufacturing rights in China.
2. How does this patent impact generic drug development?
It may obstruct generic manufacturers from producing similar pyrimidine-based formulations via the patented process, unless they design around the specific synthesis methods or formulations claimed.
3. Can this patent be challenged or licensed?
Yes; parties may challenge its validity through prior art or licensing negotiations, especially as patent expiration approaches or if they can demonstrate non-infringement.
4. Is the patent applicable outside China?
Not directly. For global protection, filing in other jurisdictions via PCT or patent national routes is necessary, although the patent’s principles could influence foreign patent applications.
5. What should R&D companies consider to avoid infringing this patent?
They should develop alternative synthesis routes, novel derivatives outside the claimed scope, or new formulation techniques that do not utilize the patented processes.
References
- CN101686988 patent document.
- China's Patent Law and Examination Guidelines (2021).
- Market reports on pyrimidine derivative pharmaceuticals in China.
