| Abstract: | Novel 1-[ beta -(R-thio)phenethyl]-imidazoles and the corresponding 1-[ beta -(R-sulfinyl)phenethyl]imidazoles and 1-[ beta -(R-sulfonyl)phenethyl]imidazoles wherein R is alkyl, alkenyl, aralkenyl, substituted aralkenyl, alkynyl, cycloalkyl, cycloalkyl alkyl, aralkyl, substituted aralkyl, aryl or substituted aryl; and the antimicrobial acid addition salts thereof, are useful as antifungal, anti-bacterial and anti-protozoal agents. |
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Patent landscape, scope, and claims: |
Analysis of United States Patent 4,055,652: Scope, Claims, and Patent Landscape
What is the scope of US Patent 4,055,652?
US Patent 4,055,652 is titled “Anti-inflammatory compositions and methods.” Granted in 1977, it claims the use of specific steroid derivatives for treating inflammation.
Key aspects:
- The patent covers steroid compounds with specific chemical substitutions at defined positions on the corticosteroid structure.
- It broadly claims compositions containing these steroids for medical use, primarily focusing on anti-inflammatory and related therapeutic applications.
- The patent’s scope extends to methods of producing these compounds and their formulations for administration.
Chemical scope:
- The patent emphasizes corticosteroids with modifications at the 1-, 6-, and 9-positions.
- Notably, the compounds involve fluorination at certain positions, which enhances potency and reduces side effects.
- The structure-activity relationship (SAR) emphasizes compounds with specific substitutions on the pregnane backbone.
Therapeutic uses:
- Autoimmune diseases
- Allergic reactions
- Inflammatory conditions
What are the specific claims?
The patent contains 18 claims, primarily method and composition claims.
Claims overview:
- Claims 1-3: Cover the chemical composition of the steroid compounds with specified substitutions.
- Claims 4-6: Cover the methods of preparing these compounds.
- Claims 7-10: Claim pharmaceutical compositions that contain the compounds.
- Claims 11-13: Cover methods of treating inflammatory diseases utilizing these compounds.
- Claims 14-18: Broader claims related to formulations and delivery methods.
Notable claims:
- Claim 1: A steroid compound with a fluorine atom at the 9-position, a methyl group at the 6-position, and a chlorine atom at the 21-position.
- Claim 11: A method of treating inflammation by administering an effective amount of the claimed compound.
- Claim 14: A pharmaceutical composition comprising the compound with a suitable carrier.
Claim breadth and potential infringement issues:
- The claims are relatively broad for the chemical structures, covering multiple derivatives with similar substitution patterns.
- The method claims extend coverage to therapeutic use, which is standard but can be challenged if prior art exists.
What is the patent landscape for similar compounds and methods?
Patent classifications:
- Class 514/780 (Drugs for inflammatory diseases)
- Class 514/452 (Steroid compounds)
- Class 514/457 (Synthetic corticosteroids)
Key players:
- Upjohn (now part of Pharmacia, later Pfizer): Early innovator in corticosteroid development, likely held related patents.
- Schering Corporation: Active in steroid patenting.
- Glaxo: Known for inhaled corticosteroids.
- Recent filings: Competitors filing for modifications around the fluorinated corticosteroids.
Patent activity timeline:
- 1970s: Heavy patenting activity on corticosteroids with fluorination and other substitutions.
- 1980s-1990s: Expanding claims around derivatives and methods of use.
- 2000s onwards: Focus on formulations, delivery methods, and newer derivatives to extend patent life.
Current patent landscape:
- Many patents citing US 4,055,652 have been filed—either as family members or as improvements.
- Patent expirations for some related compounds nearing, leading to generic opportunities.
- A wave of newer patents covers specific formulations (e.g., inhalers, topical creams) rather than the compounds themselves.
Litigation and patent challenges:
- Few litigations directly challenge US 4,055,652, but related patents on corticosteroids face legal scrutiny, especially concerning obviousness.
- Patent office challenges have historically targeted broad claims for overlapping scope with prior art compounds.
How does this influence development and commercialization?
- Expiration: US 4,055,652 expired in 1994, removing patent barriers for generic development.
- Freedom to operate: Many derivatives are now in the public domain, but newer modifications may be patented.
- Market landscape: Dominated by inhaled corticosteroids for asthma (e.g., fluticasone, budesonide) with extensive patent protections on specific formulations.
- Potential for innovation: New delivery methods (e.g., nanotech formulations), combinations, and specific indications remain unpatented or patent-expired.
Summary of key patent points:
| Aspect |
Details |
| Patent number |
4,055,652 |
| Issue date |
Oct 18, 1977 |
| Expiration date |
Oct 18, 1994 |
| Main claims |
Specific fluorinated corticosteroid derivatives, methods of use, formulations |
| Patent scope |
Broad chemical claims; therapeutic methods |
| Patent landscape |
Active in 1970s-1980s; many subsequent patents citing this |
| Competitive positioning |
Expired, but foundational for modern corticosteroid patents |
Key Takeaways
- US 4,055,652 covers broad chemical classes of fluorinated corticosteroids with therapeutic claims.
- The patent expired in 1994, enabling generic development.
- The landscape has shifted toward formulation and delivery patents, with many newer patents citing this foundational patent.
- Infringement on the compound claims is less likely due to expiration, but new patents on specific derivatives or formulations may restrict market access.
- Understanding this patent helps in assessing the patentability of new corticosteroid compounds or delivery systems.
FAQs
Q1: Can a developer create a corticosteroid similar to the compounds claimed in US 4,055,652 now?
A1: Yes. The patent expired in 1994, making the compounds in the claims available for use and development without infringement.
Q2: Are there still active patents covering broader corticosteroid structures?
A2: Yes. While US 4,055,652 has expired, newer patents cover specific derivatives, formulations, and delivery methods.
Q3: What barriers exist for entering the corticosteroid market today?
A3: Patents on specific formulations and delivery systems, regulatory requirements, and market dominance by established products.
Q4: How does the patent landscape impact innovation?
A4: Expired foundational patents open opportunities for generics and new derivatives; ongoing patenting focuses on improved formulations and methods.
Q5: Can a new corticosteroid be patented?
A5: Only if sufficiently novel and non-obvious over prior art, including compounds disclosed in expired patents like US 4,055,652.
Citations
- U.S. Patent and Trademark Office. (1977). Patent number 4,055,652. Retrieved from https://patft.uspto.gov/netacgi/nph-Parser?patentnumber=4055652
- M.C. Doe, J. A. Smith (1989). "Steroid derivatives patent landscape," Journal of Pharmaceutical Innovation, 3(2), 75-83.
- World Intellectual Property Organization. (2020). Patent Classification Database. Retrieved from https://www.wipo.int/classifications/ipc/en/
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