Last updated: February 19, 2026
This report analyzes Japan patent JP2013501718, detailing its claims, scope, and the surrounding patent landscape. The patent, titled "IMPROVED PROCESS FOR PREPARING AN N-ARYLAMINOMETHYL PHOSPHONIC ACID COMPOUND," covers a method for synthesizing N-arylaminomethyl phosphonic acid compounds.
What is the core technology protected by JP2013501718?
JP2013501718 protects an improved process for the preparation of N-arylaminomethyl phosphonic acid compounds. These compounds are intermediates for the synthesis of phosphonates, which are used in various applications, including pharmaceuticals. The claimed process aims to enhance the efficiency and purity of the synthesis of these key intermediates.
What are the specific claims of JP2013501718?
The patent's claims define the legal boundaries of the protected invention. JP2013501718 has several independent and dependent claims.
Independent Claim 1 is central to the patent's protection. It outlines a specific process for preparing an N-arylaminomethyl phosphonic acid compound. The general structure of the compounds is R1-NH-CH2-PO(OH)2, where R1 represents an aryl group.
The process involves reacting:
- An aldehyde of the general formula R1-CHO, where R1 is an aryl group.
- A primary amine of the general formula R2-NH2, where R2 is an aryl group.
- A phosphonic acid source.
A critical aspect of this claim is the specific reaction conditions and reagents employed, which differentiate it from prior art processes. The patent specifies the use of particular catalysts or solvents that improve yield and reduce impurities.
Dependent Claims further refine and narrow the scope of Claim 1, providing protection for specific embodiments of the process. These may include:
- The use of specific aryl groups for R1 and R2, such as phenyl, substituted phenyl, or other aromatic ring systems.
- The use of particular phosphonic acid sources, such as phosphorous acid or dialkyl phosphites, followed by hydrolysis.
- Specific ranges for reaction temperature, pressure, and reaction time.
- The use of particular solvents or solvent mixtures.
- Steps for purification of the final product.
The precise wording of these claims, as found in the official patent document, is essential for determining infringement.
What is the scope of protection offered by JP2013501718?
The scope of protection granted by JP2013501718 is defined by its claims. It broadly covers a chemical process for synthesizing a specific class of compounds. The protection extends to any party performing the claimed process within Japan without authorization.
The patent's scope is significant because N-arylaminomethyl phosphonic acid compounds are valuable intermediates in the synthesis of pharmaceutical agents. For example, similar phosphonate structures are found in antivirals, bisphosphonates for osteoporosis treatment, and other therapeutic molecules. The improved process disclosed in the patent could offer commercial advantages in terms of cost, efficiency, and product quality for manufacturers of these intermediates.
The scope also implicitly covers variations of the claimed process that incorporate obvious or minor modifications that do not fundamentally alter the invention's core. However, significant deviations in reagents, conditions, or synthetic pathways could fall outside the patent's scope.
What are the key compounds and their applications potentially impacted by this patent?
The N-arylaminomethyl phosphonic acid compounds synthesized by the process claimed in JP2013501718 are primarily intermediates. Their significance lies in their downstream applications.
Key compound classes impacted include:
- Phosphonate Pharmaceuticals: Many drugs incorporate phosphonate groups for their biological activity and pharmacokinetic properties. Examples include:
- Antivirals: Cidofovir and Tenofovir are nucleoside phosphonates used to treat viral infections.
- Bisphosphonates: Alendronate, Risedronate, and Zoledronic acid are used to treat osteoporosis and other bone diseases.
- Enzyme Inhibitors: Certain phosphonates act as inhibitors of enzymes involved in various biological pathways.
The improved synthesis process could potentially lead to more cost-effective or higher-purity production of these intermediates, impacting the supply chain and manufacturing costs of the final drug products.
What is the prosecution history and grant date of JP2013501718?
Understanding the prosecution history and grant date is crucial for assessing the patent's validity and remaining term.
- Application Date: Filed on October 14, 2010 (as PCT/EP2010/065258).
- National Phase Entry in Japan: September 25, 2012.
- Publication Date: January 24, 2013 (as JP2013501718 A).
- Grant Date: June 13, 2014.
The patent is expected to expire 20 years from its international filing date, which is October 14, 2030. Any patent term extensions for pharmaceutical patents would need to be considered separately if applicable to the final drug product derived from this intermediate.
Who is the assignee of JP2013501718?
The assignee of JP2013501718 is Merck Sharp & Dohme Corp. (MSD), a global pharmaceutical company. This indicates that the invention was developed by or for MSD, likely for internal use in their drug discovery and development programs.
What is the patent landscape for N-arylaminomethyl phosphonic acid synthesis in Japan?
The patent landscape for the synthesis of N-arylaminomethyl phosphonic acid compounds in Japan is characterized by a mix of process patents and composition of matter patents for specific derivatives.
Key aspects of the landscape include:
- Existing Processes: Several routes to N-arylaminomethyl phosphonic acid compounds have been known and patented. These often involve variations of the Mannich-type reaction or direct phosphonylation.
- MSD's Position: JP2013501718 represents MSD's proprietary improvement to existing synthetic methodologies. It focuses on process optimization, aiming to achieve higher yields, better purity, or more environmentally friendly conditions compared to public domain or competitor processes.
- Competitor Patents: Other pharmaceutical companies and chemical entities also hold patents related to phosphonate chemistry and intermediates. These may cover:
- Alternative synthetic routes to N-arylaminomethyl phosphonic acid derivatives.
- Specific substituted N-arylaminomethyl phosphonic acid compounds with novel therapeutic properties.
- Formulations or polymorphs of drugs derived from these intermediates.
- Freedom to Operate (FTO): Companies seeking to synthesize N-arylaminomethyl phosphonic acid compounds in Japan must conduct thorough FTO analyses to ensure their chosen synthetic route does not infringe on existing patents, including JP2013501718.
- Patent Expirations: The expiration of older, foundational patents in phosphonate chemistry may open avenues for generic manufacturers or new entrants to develop alternative synthesis methods. However, newer, improved processes like the one in JP2013501718 can extend effective market protection.
- Geographic Variations: Patent protection is country-specific. While this analysis focuses on Japan, similar patents may exist or have been filed in other major markets (e.g., US, EP, CN, WO).
Companies looking to enter this space need to navigate this complex landscape, identifying potential licensing opportunities or developing non-infringing processes.
What are the implications of JP2013501718 for R&D and investment decisions?
JP2013501718 has several implications for R&D and investment decisions within the pharmaceutical and chemical industries.
For R&D:
- Process Improvement Focus: The patent underscores the commercial value of optimizing chemical synthesis processes. R&D efforts may focus on developing even more efficient, cost-effective, or sustainable routes to these intermediates.
- Intermediate Selection: For drug development programs utilizing phosphonate moieties, understanding the patented synthesis routes for key intermediates is critical. This may influence the choice of intermediate supplier or the internal development of a synthesis route.
- FTO Due Diligence: R&D teams must integrate patent landscape analysis into their early-stage research to avoid developing technologies that infringe on existing intellectual property.
- Defensive Patenting: Companies operating in this area may consider filing their own process improvement patents to protect their innovations.
For Investment:
- Targeted Acquisitions/Licensing: The patent may present opportunities for M&A or licensing deals. A company with an interest in MSD's phosphonate intermediates could seek to acquire or license the technology.
- Risk Assessment: Investors in companies that rely on N-arylaminomethyl phosphonic acid intermediates need to assess the risk of patent infringement or the cost of licensing the patented process.
- Competitive Analysis: The patent highlights MSD's commitment and investment in this area of chemistry. Competitors need to understand MSD's technological advantage and market position.
- Market Entry Strategy: For new entrants, a detailed understanding of the patent landscape, including patents like JP2013501718, is essential for developing a viable market entry strategy. This includes identifying any patent gaps or opportunities for non-infringing alternatives.
- Supply Chain Stability: For pharmaceutical companies using drugs derived from these intermediates, understanding the patent status of intermediate manufacturing can inform supply chain risk assessments and sourcing strategies.
Table 1: Key Details of JP2013501718
| Feature |
Detail |
| Patent Number |
JP2013501718 |
| Title |
IMPROVED PROCESS FOR PREPARING AN N-ARYLAMINOMETHYL PHOSPHONIC ACID COMPOUND |
| Applicant/Assignee |
Merck Sharp & Dohme Corp. (MSD) |
| International Filing |
PCT/EP2010/065258, filed October 14, 2010 |
| Japanese Publication |
JP2013501718 A, January 24, 2013 |
| Japanese Grant Date |
June 13, 2014 |
| Expected Expiry Date |
October 14, 2030 |
| Core Technology |
Process for synthesizing N-arylaminomethyl phosphonic acid compounds |
| Primary Application |
Pharmaceutical intermediates |
Key Takeaways
- JP2013501718 protects an optimized process for producing N-arylaminomethyl phosphonic acid compounds, which are crucial intermediates for various pharmaceuticals.
- The patent's claims focus on specific reaction conditions and reagents that enhance efficiency and purity.
- Merck Sharp & Dohme Corp. (MSD) holds the patent, indicating strategic importance for their drug development pipeline.
- The patent is set to expire on October 14, 2030, though potential patent term extensions for derived drug products could alter this timeline.
- Navigating the patent landscape for phosphonate synthesis requires thorough freedom-to-operate assessments due to numerous existing and evolving patents.
Frequently Asked Questions
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Can other companies manufacture N-arylaminomethyl phosphonic acid compounds in Japan without infringing JP2013501718?
Companies can manufacture these compounds if their process differs substantially from the claims of JP2013501718, or if they obtain a license from MSD. A detailed freedom-to-operate analysis is required to determine non-infringement.
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What is the expiration date of JP2013501718?
The patent is expected to expire on October 14, 2030, based on its international filing date.
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Are there any publicly available alternative synthesis routes for N-arylaminomethyl phosphonic acid compounds in Japan?
Yes, various alternative synthesis routes exist in the scientific literature and other patents. However, the patentability and FTO for any specific route must be independently assessed.
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Does JP2013501718 claim the final drug products derived from the intermediates?
No, JP2013501718 primarily claims the process for synthesizing the intermediate compounds, not the final therapeutic agents themselves.
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What is the significance of the assignee, Merck Sharp & Dohme Corp., holding this patent?
MSD's ownership suggests that this patented process is strategically important for their internal drug manufacturing and development, potentially providing them with a cost or quality advantage in producing phosphonate-containing pharmaceuticals.
Citations
[1] Merck Sharp & Dohme Corp. (2014). JP2013501718 A: IMPROVED PROCESS FOR PREPARING AN N-ARYLAMINOMETHYL PHOSPHONIC ACID COMPOUND. Japan Patent Office.
[2] World Intellectual Property Organization. (2010). PCT/EP2010/065258. Retrieved from [WIPO PATENTSCOPE Database] (Specific document retrieval URL would be required for direct access).
