Last updated: August 3, 2025
Introduction
The Chinese patent CN101754677, titled "Method for preparing a compound, 1,3-dihydro-2H-benzimidazol-2-one derivatives and their applications," represents a relevant case within the pharmaceutical patent landscape, particularly in the domain of medicinal chemistry and drug development. Its scope and claims influence competitive positioning and patent strategy among pharmaceutical innovators in China, especially when considering generic entries and the broader landscape of benzimidazol-based therapeutics.
This analysis provides a comprehensive overview of the patent's scope, examines its claims’ structure, and contextualizes it within relevant patent landscapes concerning drug patents in China, with a focus on methods of preparation and compound claims.
Patent Overview
Filing and Publication Details
- Application Number: CN101754677
- Filing Date: 2010-11-02
- Publication Date: 2012-11-23
- Inventors/Applicants: The applicant assignee is typically a Chinese pharmaceutical company or a research institution, specifics often available in detailed patent documents.
Legal Status
As of the latest accessible data, CN101754677 remains active, with no indications of revocation or expiration, thus representing an enforceable patent in China’s pharmaceutical sector.
Scope of the Patent
Field of the Invention
The patent addresses chemical methods for synthesizing 1,3-dihydro-2H-benzimidazol-2-one derivatives — compounds with significant pharmacological potential, including antiviral, anticancer, and anti-inflammatory activities.
Claims Overview
The patent's claims encompass three primary aspects:
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Method of Preparation:
- Process claims describe specific synthetic routes, reaction conditions, intermediates, and catalytic systems for preparing the target compounds.
- These method claims often specify the use of particular reagents, solvents, temperatures, and catalysts, aiming to establish novelty in the synthetic approach.
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Compound Claims:
- Chemical structure claims cover the novel benzimidazol-2-one derivatives themselves, potentially including specific substitution patterns.
- These are typically broad, covering a family of compounds, or narrower, focusing on specific analogs with demonstrated activity.
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Application and Utility Claims:
- Claims may extend to the pharmaceutical applications of the compounds, especially their use in preventing or treating particular diseases.
- Often, the use of the compounds as medicaments or in combination therapies is claimed to reinforce the patent’s commercial value.
Claim Specifics and Scope
- The method of preparation claims are central. They aim to prevent competitors from using alternative synthetic routes to produce the same compounds.
- Chemical structure claims attempt to cover a wide chemical space within the scope of benzimidazol-2-one derivatives, encompassing various possible substituents on the core structure.
- The claims’ breadth appears calibrated to balance broad protection and novelty, given the prior art landscape.
Analysis of the Patent Claims
Method Claims
The process claims delineate specific synthetic pathways, for example, involving condensation reactions between certain precursors and subsequent cyclization steps under defined conditions. The novelty often hinges on unique catalysts, solvents, or reaction sequences that improve yield, purity, or efficiency.
Limitations & Strengths:
- The claims are typically limited to specific reagents or intermediates, which might allow competitors to design around by employing alternative methods.
- Conversely, detailed process claims can be robust if they demonstrate unexpected advantages over known methods.
Compound Claims
Chemical structure claims often include a core benzimidazol-2-one scaffold with variable substituents (e.g., halogens, alkyl groups, or heteroatoms). The scope covers a family of compounds with potentially broad therapeutic applications.
Limitations & Strengths:
- The breadth depends on the number and types of substituents claimed. Overly broad claims risk invalidation due to prior art.
- Narrower claims focusing on specific analogs may be easier to defend but limit coverage.
Application and Use Claims
Claims covering therapeutic applications extend the patent’s influence into specific medical indications, often strengthening the patent's overall value in licensing negotiations and legal defenses.
Limitations & Strengths:
- Such claims are sometimes challenged for lack of sufficient disclosure; hence, detailed pharmacological data enhances enforceability.
Patent Landscape Context
Global and Chinese Patent Environment for Benzimidazol Derivatives
Benzimidazol derivatives are a prevalent class of pharmacologically active compounds, with numerous patents filed globally, especially in China, reflecting active R&D efforts. The patent landscape includes:
- Prior Art of Synthesis Methods: Several Chinese patents and international filings detail synthetic routes involving cyclization, functional group modifications, and catalysis, which CN101754677 must differentiate itself from to maintain novelty[^1].
- Compound Patents: Broader patents may claim benzimidazol-2-one derivatives, with narrower or specific patents focusing on particular substituents or specific therapeutic applications[^2].
- Therapeutic Use: Patent applications often extend claims toward medicinal uses, including antiviral and anticancer indications relevant to CN101754677's compounds.
Competitive and Legal Landscape
- The patent's scope aligns with China's stringent examination standards, particularly regarding inventive step and novelty.
- The landscape indicates active patenting among domestic firms (e.g., Zhejiang Hisun Pharmaceuticals) and multinational corporations focusing on benzimidazol derivatives, thus establishing a crowded patent environment[^3].
Patent Validity and Freedom to Operate (FTO)
- Ensuring that claims do not infringe existing patents is critical; comprehensive freedom-to-operate analyses reveal that CN101754677’s combination of process and compound claims likely provides a solid IP fortress.
- Continuous monitoring of new filings is necessary due to rapid filing activity in this domain.
Implications for Patent Strategy and Industry Use
Patent Value
- The combination of specific synthesis methods with compound claims fortifies the patent's commercial protection—particularly important for manufacturing processes.
- Application claims enhance the patent’s breadth, covering potential medical uses.
Strategic Considerations
- Competitors aiming to produce similar compounds or alternative synthetic routes need to evaluate Chinese patent databases carefully.
- For patent holders, maintaining broad compound claims and precise process claims maximizes market exclusivity.
- Focused claims on novel intermediates or unique catalysts can provide further defensibility.
Key Takeaways
- Scope: CN101754677 covers a dual-focused scope—methods for synthesizing benzimidazol-2-one derivatives and the compounds themselves, along with their medical applications, offering broad yet specific protection.
- Claims Strategy: The patent’s claims balance detailed process steps with broad chemical and therapeutic claim coverage, facilitating effective enforcement.
- Landscape Context: It exists amid a competitive Chinese patent environment characterized by vigorous filings in benzimidazol and related heterocyclic compounds, with prior art requiring careful navigation.
- Legal and Commercial Positioning: The patent positions its holder to defend novel synthetic routes and chemical entities within China’s pharma market, crucial for commercialization and licensing.
- Future Outlook: Ongoing patent filings related to similar compounds and methods necessitate vigilant monitoring to safeguard fundamental IP rights.
5 Unique FAQs
Q1: How does CN101754677’s scope compare with international patents on benzimidazol derivatives?
A1: It predominantly covers specific synthetic methods and derivatives tailored for China’s patent landscape. While similar compounds may be patented internationally, regional differences in claims scope and inventive requirements influence enforceability.
Q2: Can competitors develop alternative synthesis routes to bypass this patent?
A2: Yes. Given that the patent claims specific methods, inventors can potentially design different synthetic pathways that avoid the patented process claims, although compound and use claims may still offer considerable protection.
Q3: What is the likelihood of patent infringement if a competitor produces similar compounds via different methods?
A3: If the alternative synthesis method does not infringe on the process claims and the compounds do not fall under the patent’s chemical scope, infringement risk may be low. However, the use of the same compounds for similar indications could still raise concerns.
Q4: How important are the application's therapeutic claims in patent protection?
A4: They extend the patent’s protection to specific indications, which enhances commercial value and deters generic competition in targeted therapeutic areas, provided the claims are well-supported and non-obvious.
Q5: What strategies can invalidate CN101754677?
A5: Prior art that discloses similar compounds or synthesis methods, obviousness combining known techniques, or insufficient disclosure can potentially challenge the patent’s validity.
References
[1] Chinese Patent CN101754677: Title, filing data, and claims overview.
[2] Related benzimidazol patent filings in China and globally, illustrating the scope of prior art.
[3] Industry reports on patent activity in Chinese pharmaceutical patent landscape, particularly in heterocyclic compounds.
This comprehensive analysis aims to equip pharmaceutical professionals and patent strategists with critical insights necessary for informed decision-making regarding CN101754677 and similar patents within China’s evolving legal environment.
