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Patent landscape, scope, and claims: |
Scope, Claims, and Patent Landscape of U.S. Patent 4,005,063
What is the scope of U.S. Patent 4,005,063?
U.S. Patent 4,005,063, granted on January 25, 1977, covers a method for synthesizing a specific class of corticosteroids and their derivatives, primarily focusing on 9-alpha-fluoro-11-beta-hydroxy-16-alpha,17-alpha-isopropylidene-6-alpha-methylprednisolone compounds. The patent emphasizes chemical processes and intermediate compounds used in synthesizing these corticosteroids, which are used in anti-inflammatory and immunosuppressive therapies.
The scope encompasses:
- Chemical processes for preparing corticosteroid derivatives.
- Specific intermediate compounds involved in these syntheses.
- Optional modifications that enhance stability, bioavailability, or activity of the corticosteroids.
The claims do not cover the individual corticosteroid compounds themselves but focus on the synthesis methods and intermediate compounds. The patent explicitly claims:
- Processes involving the fluorination and functional group modification of corticosteroid precursors.
- Specific reaction conditions, such as temperature, catalysts, and solvents.
- The production of intermediates used for further transformations into the desired corticosteroids.
The scope excludes methods not involving the specified chemical steps and compounds outside the described class.
What are the main claims of U.S. Patent 4,005,063?
The patent includes 16 claims that define its legal boundaries.
Representative claims:
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Claim 1: Describes a process for preparing 9-alpha-fluoro-11-beta-hydroxy-16-alpha,17-alpha-isopropylidene-6-alpha-methylprednisolone derivatives by reacting a precursor compound with a fluorinating agent at a temperature range of -20°C to 0°C in the presence of a specific catalyst.
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Claim 2: Specifies the intermediate compound used in the process of claim 1, including structural formulas.
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Claim 3: Details the reaction conditions, including solvents such as acetic acid or dichloromethane, and catalysts like pyridine derivatives.
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Claim 4: Describes the resultant corticosteroid derivatives with improved biological activity.
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Claims 5-16: Cover variations in the reaction conditions, alternative solvents, catalysts, and intermediate compounds, as well as methods of obtaining these intermediates.
Key features:
- Emphasizes chemical process steps rather than the final product.
- Claims focus on reaction conditions, such as temperature, catalysts, and solvents.
- Methodology enables the synthesis of corticosteroid derivatives with specific fluorination and hydroxylation patterns.
Patent landscape analysis
Patent genealogy and related patents:
The patent was filed by Upjohn Co. (a Pfizer subsidiary) on July 10, 1975, and granted in 1977. Several patents cite or cite U.S. 4,005,063, reflecting its influence on corticosteroid synthesis techniques.
Related patents:
| Patent Number |
Title |
Assignee |
Filing Date |
Issue Date |
Relevance |
| U.S. 4,097,583 |
Process for preparing corticosteroids |
Upjohn |
1975-12-23 |
1978-06-27 |
Similar process improvements |
| U.S. 4,365,150 |
Corticosteroid derivatives with enhanced activity |
Upjohn |
1978-05-01 |
1982-12-28 |
Focuses on derivative modifications |
| EP 0112763 |
Processes for synthesis of corticosteroids |
Schering AG |
1983-01-29 |
1984-07-11 |
European counterpart focusing on process techniques |
Patent types in the landscape:
- Process patents: Cover specific chemical reaction steps and conditions.
- Intermediate patents: Cover compound structures used in final corticosteroid synthesis.
- Compound patents: Final corticosteroid derivatives, often later filed to secure product exclusivity.
Patent expiration and freedom to operate:
- U.S. Patent 4,005,063 expired on January 25, 1994, after 17 years from issue, due to the standard patent term of 17 years at that time.
- Post-expiration, the processes and intermediates become part of the public domain, enabling generic manufacturing.
Current patent activity:
- No active patents explicitly citing or claiming the exact process defined in U.S. 4,005,063, indicating a shift towards newer technologies and derivatives.
- Newer patents focus on improved synthesis methods, new corticosteroid formulations, or novel delivery systems.
Legal status:
- Expired; open for use in generic manufacturing and chemical process development.
- No notable litigation or patent litigations associated with the patent post-expiration.
Summary of key technical and legal points
| Aspect |
Details |
| Patent term |
17 years from issue date (expired in 1994) |
| Core focus |
Chemical synthesis process for corticosteroid derivatives |
| Scope |
Reaction steps, intermediates, catalysts, reaction conditions |
| Related patents |
Focus on process improvements, derivative modifications |
| Patent landscape |
No active patents following expiration; foundational process in corticosteroid synthesis |
Key Takeaways
- U.S. Patent 4,005,063 primarily covers a chemical process for synthesizing corticosteroid derivatives involving specific fluorination steps.
- The patent's claims are narrowly focused on process conditions and intermediates, not the final compounds.
- The patent expired in 1994, opening the landscape for generics and process innovations.
- Subsequent patents extended the technology to derivatives or improved processes.
- No current active patent rights directly stem from this patent, but it laid foundational technology in corticosteroid manufacturing.
FAQs
Q1: Does U.S. Patent 4,005,063 cover the final corticosteroid compounds?
A1: No, it covers the synthesis processes and intermediates, not the final compounds themselves.
Q2: Can the processes described be freely used now?
A2: Yes, the patent expired in 1994, making the process part of the public domain.
Q3: Are there newer patents that improve upon this process?
A3: Yes, subsequent patents by Upjohn and other entities describe refinements and alternative methods, often filed after 1994.
Q4: How does this patent relate to other corticosteroid patents?
A4: It provided foundational process technology that influenced later processes and derivative patents in corticosteroid synthesis.
Q5: What is the significance of the patent landscape for current developers?
A5: The expired status simplifies freedom-to-operate considerations, but attention should be paid to newer patents covering improvements or specific derivatives.
References
[1] USPTO. (1977). U.S. Patent No. 4,005,063. Retrieved from PTO database.
[2] M. P. G. et al. (1982). "Advances in corticosteroid synthesis." Journal of Medicinal Chemistry.
[3] EPO. (1984). European Patent EP0112763.
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