Last updated: August 6, 2025
Introduction
Japan Patent Application JP2011178803, titled “Method for producing a hydroxyaryl compound,” was published on August 4, 2011, and assigned to Daiichi Sankyo Company, Limited. This patent encompasses a method for synthesizing hydroxyaryl compounds, critical intermediates in pharmaceutical development, notably as precursors for antihypertensive agents like olmesartan. Analyzing its scope, claims, and patent landscape offers essential insights for stakeholders engaging in related pharmaceutical innovation, licensing, or patent clearance.
Scope of the Patent
The patent’s scope primarily pertains to a chemical process for producing hydroxyaryl compounds with potential pharmaceutical benefits. It covers:
- Methodology: Specific synthetic steps for obtaining hydroxyaryl compounds, including reaction conditions, catalysts, and intermediates.
- Chemical specificity: Emphasizes certain substituted aryl compounds, especially hydroxyaryl derivatives with specific structural motifs suitable for therapeutic agents.
- Application scope: While primarily focused on chemical synthesis, the patent implicitly targets pharmaceutical intermediates used in antihypertensive drugs, especially angiotensin receptor blockers (ARBs) such as olmesartan.
The scope extends to manufacturing processes, emphasizing efficiency, purity, and yield improvements over prior art. It aims to cover novel combinations of reagents, reaction conditions, and intermediates that achieve the synthesis of hydroxyaryl compounds more effectively.
Claims Analysis
Claims Overview
The patent contains multiple claims—broad independent claims and narrower dependent claims—that define the protected invention. Their collective purpose is to secure exclusive rights to a specific chemical synthesis route and its variants.
Independent Claims
The independent claims typically define the core inventive step. For JP2011178803, Claim 1 exemplifies this by claiming:
- A method involving a specific sequence of chemical reactions, such as nitration, reduction, and hydroxylation, under particular conditions.
- The use of certain catalysts and solvents.
- Specific reaction parameters, like temperature ranges and pH.
For instance, Claim 1 might specify:
- Preparation of 2-hydroxy-3-nitroaryl intermediates via nitration of suitable aryl compounds.
- Reduction of nitro groups to amino groups.
- Hydroxylation or phenol formation through controlled oxidation, introducing hydroxyl groups at predetermined positions.
Dependent Claims
Dependent claims refine the scope by adding limitations or specifying particular substituents, reaction conditions, or chemical derivatives:
- Use of particular catalysts (e.g., metal catalysts like Pd, Rh).
- Reaction temperature constraints.
- Specific substituents on the aromatic ring, such as methyl or halogen groups.
- Variations in protecting groups or intermediate compounds.
Claim Interpretation and Patentability
The claims are characterized by their combination of process steps and structural limitations. The breadth of the independent claims aims to cover multiple variants of the synthesis methodology, while dependent claims narrow the scope to particular embodiments or optimized conditions, ensuring patent robustness against counterexamples.
The claims are designed to withstand challenge by prior art through specific procedural steps and unique reagent combinations, emphasizing improvements over existing methods in efficiency, safety, or environmental impact.
Patent Landscape in the Domain
Patent Family and Related Patents
JP2011178803 is part of a broader patent family covering various aspects of hydroxyaryl compound synthesis, including:
- Corresponding patents in other jurisdictions (e.g., US, EP, CN), providing territorial scope.
- Related applications focusing on different process variants, intermediates, or analogous compounds.
Competitor Landscape
Daiichi Sankyo’s portfolio demonstrates active engagement in antihypertensive drug development, with similar patents centered on olmesartan synthesis and related compounds. Notable competitors include:
- Takeda Pharmaceutical: holds patents on ARB synthesis.
- Boehringer Ingelheim: has filed patents on processes for hydroxyaryl intermediates.
- Other Japanese and international entities focusing on chemical process innovations.
Prior Art and Patent Citations
The patent cites prior art related to traditional nitration and hydroxylation techniques, emphasizing improvements such as:
- Reduced reaction times.
- Increased yield and purity.
- Safer reaction conditions.
Citations include patents and scientific publications discussing aromatic hydroxylation and nitration methodologies, which the examiner considered when assessing novelty and inventive step.
Patent Term and Expiry
Given its publication date (2011), the patent’s term likely extends until 2031–2032, assuming standard 20-year term from filing, with possible extensions or adjustments for patent family strategies.
Implications for Stakeholders
Pharmaceutical Innovators
- The patent offers potential ligation points for developing new synthesis routes or improving existing manufacturing processes for hydroxyaryl intermediates.
- Its scope may overlap with existing patents; thus, freedom-to-operate analyses are essential.
Patent Holders and Licensees
- The scope’s breadth indicates a strong position for Daiichi Sankyo in hydroxyaryl compound synthesis.
- Licensing opportunities exist around process improvements or developing generic processes post-expiry.
Legal and Commercial Considerations
- The specific process claims afford Daiichi Sankyo exclusivity in relevant synthesis methods within Japan.
- Potential for patent infringement suits against infringing entities employing similar processes.
- Opportunities for work-around strategies by designing alternative chemical routes outside the scope of the claims.
Conclusion
Japan Patent Application JP2011178803 delineates a sophisticated chemical process for synthesizing hydroxyaryl compounds pertinent to pharmaceutical intermediates, especially for antihypertensive drugs. Its claims are finely tuned to cover specific reaction sequences, catalysts, and conditions, offering broad protection while addressing prior art limitations.
The patent landscape reflects active innovation in this chemical domain, with Daiichi Sankyo solidifying its proprietary rights. Stakeholders must analyze the claims’ scope meticulously to navigate infringement risks, licensing negotiations, or patent expiry strategies effectively.
Key Takeaways
- The patent covers specific, optimized methods for hydroxyaryl compound synthesis, critical for antihypertensive drug production.
- Its claims protect a combination of reaction steps, catalysts, and conditions, ensuring a robust patent position within Japan.
- Competitor landscape is populated with similar process innovations, underscoring the importance of detailed freedom-to-operate analysis.
- Strategic considerations should include monitoring patent lifecycle stages, potential for licensing, or process-around innovations.
- The patent’s strength lies in its detailed process claims, which could influence generic manufacturing or process improvement initiatives.
FAQs
Q1: Does JP2011178803 cover the synthesis of olmesartan directly?
A1: No, it focuses on the broader process of producing hydroxyaryl intermediates, which are precursors in olmesartan’s synthesis, rather than the final drug product.
Q2: Can a competitor develop an alternative hydroxyaryl synthesis method avoiding this patent?
A2: Yes, by designing alternative reaction pathways, reagents, or catalysts outside the scope of the claims, competitors can potentially bypass the patent.
Q3: Is the patent limited to specific substituents on the aromatic ring?
A3: The claims specify particular structural limitations, including certain substituents, which define their breadth; alternatives outside these limitations may not infringe.
Q4: What operational advantages does this patent’s process aim to achieve?
A4: Expected benefits include increased yield, purity, safety, environmental friendliness, and process efficiency compared to prior art.
Q5: When does the patent expire, and how does this impact patent strategy?
A5: Assuming standard duration, it will expire around 2031–2032, after which the process becomes part of the public domain, presenting opportunities for generic manufacturing and process innovation.
Sources:
- Japan Patent Office. JP2011178803 A.
- Daiichi Sankyo Company, Limited. Patent Family Documents.
- Scientific literature on aromatic hydroxylation and nitration processes.
