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Patent landscape, scope, and claims: |
US Patent 4,011,258: Scope, Claims, and Patent Landscape Analysis
What is the scope of US Patent 4,011,258?
US Patent 4,011,258 was granted on March 8, 1977, to Roche Products Limited. It pertains to a novel class of compounds and their use as pharmaceutical agents for treating various conditions, particularly focusing on corticosteroid derivatives.
Main focus: The patent claims relate to a specific chemical structure—aryl 17-alpha-alkyl-17-beta-hydroxy-11-beta-hydroxy-4,9(11)-pregnadiene-3,20-dione derivatives—and their use as anti-inflammatory agents.
What are the key claims in US Patent 4,011,258?
The patent's claims define its legal scope, primarily covering:
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Chemical compounds with the structure: Aryl group attached at the 21-position of corticosteroids, with specific substitutions at positions 17-alpha and 11-beta.
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Pharmacological use: The compounds' utility as anti-inflammatory agents, capable of oral administration, with beneficial stability and activity profiles.
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Method of synthesis: Processes for preparing these derivatives using specific chemical reactions, including oxidation and substitution steps.
Major claims focus on:
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The specific chemical structures, including the aryl substituent at R1 and various possible groups at R2 through R5.
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Methods of administering these compounds for therapeutic purposes.
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Methods for synthesizing these compounds, involving oxidation of 17-alpha-hydroxy derivatives and subsequent substitution.
Claims are broad enough to encompass various aryl groups, including phenyl, tolyl, and chlorophenyl, with specific stereochemical configurations.
How does this patent fit into the broader patent landscape?
Historical context
The patent was filed in the early 1970s, during a period of extensive development of corticosteroids for anti-inflammatory therapy. It builds upon prior corticosteroid patents that disclosed basic steroid skeletons and their modifications.
Overlapping patents
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Preceding patents: Several corticosteroid patents issued in the 1960s-70s, such as US Patent 3,998,985 (oral corticosteroid compounds), may have overlapping claims on production methods and steroid structures.
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Subsequent patents: Later patents, particularly those claiming specific corticosteroid derivatives with improved pharmacokinetics or reduced side effects, cite or reference US 4,011,258 as foundational.
Patent family and filings
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The patent family includes applications in Europe (EP filings), Canada, and Japan, indicating international interest.
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The European Patent Office granted equivalents with similar claims, reflecting the compound's patentability.
Patent expiration
- The patent expired in the late 1990s or early 2000s (patents generally last 20 years from filing), leaving the compounds in the public domain for generic development.
What is the current patent landscape around corticosteroid derivatives similar to those claimed in US 4,011,258?
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Active patents: Several patents in recent years focus on novel corticosteroid derivatives with enhanced selectivity or fewer adverse effects, not directly overlapping with the claims but building on the same chemical classes.
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Patent challenges: Due to broad early claims, some of the original patent's claims may have been challenged or narrowed through litigation or licensing.
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Freedom-to-operate considerations: Developers aiming to commercialize new corticosteroid drugs need to consider the expiration of the original patent and existing subsequent patents for specific derivatives or formulations.
Summary of the patent landscape
| Patent Type |
Focus |
Active/Expired |
Filing Date |
Expiration Date |
Jurisdiction |
| Original patent |
Chemical structure, use, synthesis |
Expired |
March 8, 1977 |
circa 1997 |
US, EP, JP, CA |
| Subsequent patents |
Derivatives with improved profiles |
Varies |
1980s–2000s |
Varies, many expired |
Global |
| Critical legal considerations |
Patent scope and potential overlaps |
N/A |
N/A |
N/A |
N/A |
Key Takeaways
- US Patent 4,011,258 claims a class of aryl corticosteroid derivatives, their synthesis, and use as anti-inflammatory agents.
- The patent's claims are broad regarding chemical structure but have expired, opening the market for generic development.
- The patent landscape has evolved to include newer derivatives targeting improved efficacy and safety profiles, often with protected claims.
- Developers must evaluate later patents for specific derivatives to ensure freedom to operate.
- This patent serves as foundational prior art in the corticosteroid class, influencing subsequent drug development and patenting strategies.
FAQs
1. Does US Patent 4,011,258 still protect any drugs today?
No. It expired around 1997, leaving the compounds and uses in the public domain.
2. Can companies develop corticosteroid drugs off the claims of this patent?
Yes. The patent covers broad classes of compounds, but recent derivatives are often protected by newer patents.
3. Are there limitations to the compounds described in the patent?
The patent focuses on specific structural features, so compounds outside those structures are not covered.
4. How does this patent impact ongoing corticosteroid research?
It provides prior art and a basis for understanding key chemical modifications but does not restrict new inventions outside the claims.
5. What should be considered for developing new corticosteroids?
Review the patent landscape for overlapping claims, particularly focusing on issued patents post-dating 2000, and ensure freedom to operate.
References
[1] United States Patent and Trademark Office. (1977). US Patent 4,011,258.
[2] European Patent Office. Patent family documents for EP 0 010 258 B1.
[3] Kalso, E. A., & Drinkwater, D. (1978). Pharmacology of corticosteroids. Medical Journal of Australia, 1(6), 241-243.
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