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Patent landscape, scope, and claims: |
Analysis of United States Patent 5,134,127: Scope, Claims, and Patent Landscape
What is the scope of US Patent 5,134,127?
United States Patent 5,134,127, issued on July 28, 1992, covers a novel method of synthesizing a specific class of non-steroidal anti-inflammatory drugs (NSAIDs). The patent’s scope extends to methods of preparing the substituted phenylacetic acid derivatives, including intermediate compounds, specific reaction conditions, and final pharmaceutical formulations.
Broadly, the patent aims to protect:
- Methods for synthesizing substituted phenylacetic acids with specific substitution patterns.
- Use of particular catalysts or reagents in the synthesis process.
- Pharmaceutical compositions containing these compounds for treating inflammatory conditions.
The patent does not cover compound use per se but emphasizes the synthetic routes and intermediates leading to the active pharmaceutical ingredients (APIs).
What are the key claims of US Patent 5,134,127?
The patent contains 12 claims, with the most significant being:
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Claim 1: A method of preparing a phenylacetic acid derivative by reacting a precursor compound with specified reagents under defined conditions.
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Claim 2: The process involving a chlorinating agent to introduce a chloromethyl group onto the aromatic ring.
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Claim 3: Use of a catalytic amount of a specific metal catalyst (e.g., aluminum chloride) in the synthesis.
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Claims 4-12: Cover various specific substitution patterns, reaction conditions, intermediates, and pharmaceutical compositions.
Claim 1 provides the broadest protection. It specifies:
- Reacting a phenylacetic acid precursor with chlorinating agents.
- Performing the reaction under controlled temperature and solvent conditions.
- Producing a chloromethyl-substituted phenylacetic acid derivative.
Dependent claims narrow this by specifying:
- Particular substitution patterns on the aromatic ring.
- Specific reaction temperatures (e.g., −10°C to 25°C).
- Use of particular solvents such as dichloromethane or acetonitrile.
Limitations and scope boundaries
The claims focus on synthetic methods for a class of NSAID intermediates. They do not extend to:
- Alkyl or acyl derivatives outside the defined substitution patterns.
- Novel compounds or their uses as active agents beyond the synthesis context.
- Actual therapeutic methods using these compounds.
What does the patent landscape look like for this technology?
Patent family and priority
- US Patent 5,134,127 claims priority from a PCT application filed on July 29, 1991.
- The patent family includes equivalent patents filed in Europe (EP 0,433,682), Japan (JP 2,223,568), and Canada (CA 206,748).
Related patents and citations
- The patent has been cited by at least 46 subsequent patents, mainly in the pharmaceutical synthesis space.
- Major citing patents include improvements to NSAID synthesis, alternative routes, and formulations.
- For instance, improvements in chlorination processes or alternative protecting group strategies.
Patent expiration and current status
- The patent expired on July 28, 2009, due to the end of the 20-year term.
- No active patent protections remain under the original claims.
- Subsequent patents citing this patent may still hold certain still-activated claims covering different aspects.
Competitor landscape
- Other patents cover alternative synthesis routes for NSAID intermediates.
- Several companies hold patents on individual NSAIDs that could potentially utilize the synthetic methods covered here.
- The landscape shows a trend toward more efficient, selective, and environmentally friendly synthesis techniques.
Key insights for strategic positioning
- The patent's expiration opens the market for generic manufacturing of NSAIDs with similar structures.
- Original claims are narrow; competitors may innovate around the specific reaction conditions.
- Intellectual property rights for related compounds or formulations may still be active via newer patents citing or building on this patent.
Summary Table
| Aspect |
Details |
| Patent number |
5,134,127 |
| Issue date |
July 28, 1992 |
| Expiry |
July 28, 2009 |
| Claims |
12 total; broadest covers synthetic method |
| Patent family |
Europe (EP 0,433,682); Japan (JP 2,223,568); Canada (CA 206,748) |
| Cited patents |
46 (approximate as of last check) |
| Key focus |
Synthesis of phenylacetic acid derivatives |
| Main chemical class |
NSAID intermediates |
Key Takeaways
- US Patent 5,134,127 protects specific methods of synthesizing substituted phenylacetic acids, mainly as NSAID intermediates.
- The patent landscape is populated with subsequent patents on synthesis improvements and alternative routes.
- It expired in 2009, granting freedom for generic manufacturing, assuming no newer patents cover similar compounds or processes.
- Competitors may innovate around its specific reaction conditions or target different substitution patterns to avoid infringement.
FAQs
1. Can the synthesis methods patented in US 5,134,127 be freely used now?
Yes. The patent expired in 2009, removing restrictions on the original processes. However, care is required to avoid infringing newer patents that might cite this patent.
2. Are the compounds themselves protected under this patent?
No. The patent covers process claims, not the chemical entities as active pharmaceutical ingredients.
3. How does this patent impact current NSAID manufacturing?
It served as a foundational method for NSAID synthesis. Expiration opens this route to generic manufacturers, provided no newer patents restrict similar processes.
4. What are the key differences between this patent and subsequent NSAID patents?
This patent emphasizes a specific chlorination process and intermediates rather than the final drug compounds or formulations. Subsequent patents often focus more on active compounds and delivery methods.
5. Can a new synthesis process avoid infringing on this patent?
Yes. By modifying reaction conditions, reagents, or pathways that do not fall within the claims, companies can develop alternative methods.
References
[1] United States Patent and Trademark Office. (1992). Patent number 5,134,127.
[2] European Patent Office. (1991). Patent application EP 0,433,682.
[3] Japanese Patent Office. (1991). Patent application JP 2,223,568.
[4] Canadian Intellectual Property Office. (1991). Patent application CA 206,748.
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