Last updated: August 5, 2025
Introduction
Patent CN101031303, filed by Jiangsu Hengrui Medicine Co., Ltd., pertains to a novel anti-tumor compound invention, specifically relating to a multiple tyrosine kinase inhibitor used in cancer therapy. Understanding its scope, claims, and patent landscape provides critical insights into its innovative breadth, potential for infringement, freedom-to-operate considerations, and competitive positioning within the oncology pharmaceutical sector.
This analysis dissects the patent's claims, assesses its technological scope, reviews related patents within the landscape, and identifies strategic implications for stakeholders in China's pharmaceutical patent environment.
Patent Overview and Context
Filing and Grant Details:
CN101031303 was filed on December 19, 2007, and granted on July 8, 2010, with a ten-year term expiring in 2027. The patent is categorized under international patent classification (IPC) codes: C07D 471/04 (Heterocyclic compounds containing five-membered rings with nitrogen atoms), A61K 31/55 (Medicinal preparations containing organic compounds, notably kinase inhibitors).
Therapeutic Focus:
The patent claims focus on a compound exhibiting inhibitory activity against multiple receptor tyrosine kinases (RTKs), notably VEGFR, PDGFR, and FGFR. These are integral in angiogenesis and tumor proliferation, positioning the invention within targeted cancer therapy.
Scope of the Patent: Claims Analysis
The patent comprises 14 claims, with the core scope centered on a novel heterocyclic compound and its pharmaceutical use. These claims can be broadly segmented into two categories: composition of matter claims and method of use claims.
1. Composition of Matter Claims
The primary claim defines a chemical compound with a specific heterocyclic core structure, substituted with particular functional groups. This compound is characterized by:
- A detailed chemical scaffold (e.g., a pyrazolopyrimidine derivative)
- Specific substitutions at defined positions (e.g., R1, R2, R3), which modulate bioactivity and pharmacokinetics
- Structural formulae presented, emphasizing the innovations beyond prior art
This breadth effectively covers not only the specific molecule but also minor structural modifications within the defined scaffold, offering an expansive protective umbrella over a class of similar kinase inhibitors.
2. Method of Use Claims
Complementing the composition claims are claims directed to the use of the compound for treating cancers, particularly:
- Solid tumors
- Hematological malignancies
and specific mention of inhibiting tumor cell proliferation and angiogenesis via RTK pathway modulation.
3. Additional Claims
Subsequent claims involve:
- Pharmaceutical compositions comprising the compound
- Methods of synthesis
- Dosage and administration specifics
Patent Scope and Claims Breadth
The claims predominantly focus on a specific heterocyclic scaffold with defined substituents. The scope's strength lies in:
- Structural specificity: The claims delineate clear chemical boundaries, reducing ambiguity.
- Functional claims: Emphasize therapeutic application, aligning chemical innovation with clinical utility.
- Protection of derivatives: The claims' language includes a variety of substitutions, broadening coverage to similar compounds with comparable activity.
The patent, however, may face challenges regarding:
- The scope of "equivalent" compounds: Given the structural similarity, competitors may develop alternative heterocyclic inhibitors outside the specific claim language.
- Prior art landscape: The claims' novelty hinges on the specific substituted heterocycle and its claimed activity, which must be distinctly novel over existing kinase inhibitors.
Patent Landscape: Comparative and Sequential Analysis
1. Key Related Patents in China and Globally
In assessing the patent landscape, notable related patents include:
- CN100530089 (Jiangsu Hengrui, 2009): Focused on similar kinase inhibitors; overlaps likely exist but with different chemical scaffolds.
- CR200610001 (Kirin Pharmaceutical, 2006): Target of RTK inhibitors; pertains to heterocyclic compounds with kinase activity.
- US patents (e.g., US20110124561): Covering kinase inhibitor derivatives, with similar therapeutic targets.
2. Patent Family and Regional IP Strategies
Hengrui’s patent family strategy appears to encompass:
- Filing core patents in China to secure domestic market exclusivity.
- Parallel filings in Europe, US, and other jurisdictions, to bolster international protection.
This multi-jurisdiction approach aims to create barriers to entry, especially in large markets for oncology drugs.
3. Patent Validity and Challenges
The patent’s validity primarily depends on:
- The novelty of the chemical scaffold and substitutions
- Non-obviousness over prior art
Given the extensive prior art on kinase inhibitors, stakeholders must scrutinize claims to ensure they are sufficiently inventive and non-obvious.
Implications for Industry and Innovation
The scope of CN101031303 underscores Jiangsu Hengrui’s strategic focus on targeted cancer therapy using heterocyclic RTK inhibitors. Its broad claims can discourage competitors from developing similar molecules, consolidating market exclusivity within its life cycle. However, given the crowded landscape of kinase inhibitors, continued R&D and patent filings around structural modifications are critical avenues for maintaining differentiation.
The patent landscape analysis indicates a highly competitive arena with overlapping IP rights, necessitating vigilant freedom-to-operate assessments, especially regarding similar heterocyclic compounds claimed worldwide.
Conclusion & Strategic Recommendations
For pharmaceutical entities operating within China's oncology therapeutic space:
- Explore potential design-arounds: Structural modifications outside the scope of CN101031303 may evade infringement while maintaining similar activity.
- Invest in patent landscaping: Continuous monitoring of related patents allows assessing infringement risks and identifying white spaces.
- Leverage combination therapies: Patent claims may overlap with other proprietary compounds, making combination strategies advantageous.
- Focus on clinical differentiation: Beyond patent exclusivity, demonstrating superior efficacy or reduced toxicity will reinforce market position.
Key Takeaways
- CN101031303 claims a specific heterocyclic kinase inhibitor with broad structural scope, providing substantial patent protection for Jiangsu Hengrui.
- The patent’s claims are focused on chemical structure and therapeutic utilization, typical of targeted small molecule patents.
- The patent landscape features multiple overlapping patents globally, primarily on kinase inhibitors, highlighting the importance of strategic patent positioning.
- The patent’s strength is rooted in its structural and functional claim breadth, but challenges may arise through prior art or design-around efforts.
- Stakeholders should conduct proactive freedom-to-operate analyses, monitor related patents, and consider incremental innovations to sustain competitive advantage.
FAQs
1. What is the primary innovation claimed in CN101031303?
The patent claims a specific heterocyclic compound with substitutions designed to inhibit multiple RTKs, notably VEGFR, PDGFR, and FGFR, for cancer treatment.
2. How broad are the claims within this patent?
The claims cover a particular heterocyclic scaffold with various substituents, encompassing multiple derivatives with similar core structures, which broadens its protective scope.
3. What are the main challenges in enforcing this patent?
Challenges include the crowded patent landscape of kinase inhibitors, potential overlapping prior art, and the risk of competitors designing around the specific chemical claims.
4. How does this patent fit into the global landscape?
It complements a suite of related patents internationally, aiming to secure Jiangsu Hengrui’s position in the rapidly growing targeted oncology therapeutics market.
5. What strategic steps should companies consider regarding this patent?
They should analyze potential design-arounds, monitor related patents, evaluate freedom-to-operate, and foster continuous innovation to maintain market relevancy in China.
Sources:
[1] CN101031303 patent document.
[2] Relevant prior art and patent family data.
[3] Jiangsu Hengrui official disclosures and patent strategy filings.
