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Patent landscape, scope, and claims: |
Scope and Claims of US Patent 3,882,246
US Patent 3,882,246, issued June 27, 1975, is titled "Corticosteroid compounds" and assigned to Schering Corporation. It covers specific corticosteroid derivatives with anti-inflammatory properties, focusing on fluorinated corticosteroids. The patent's primary claims delineate novel compounds, methods for their synthesis, and their pharmaceutical applications.
Claims Overview
Main Claims (1-15):
- Claim 1 defines a class of corticosteroid derivatives characterized by specific substitutions at positions C-6 and C-9, notably 9α-fluoro and 6α-hydroxy groups.
- Claims 2-4 specify particular compounds within the class, such as fluocinolone acetonide.
- Claims 5-9 describe processes for preparing these compounds, emphasizing steps like fluorination and acetonide formation.
- Claims 10-12 cover pharmaceutical compositions containing these compounds.
- Claims 13-15 detail methods of using the compounds to treat inflammatory conditions.
Scope:
The patent claims focus on corticosteroids with a fluorine atom at the 9α-position, enhancing potency and reducing mineralocorticoid activity. These compounds have particular stereochemistry and substitution patterns that distinguish them from prior art.
Key Elements of Claims
- The structure involves a corticosteroid nucleus with modifications at C-6, C-9, and C-16.
- Introduction of fluorine at the 9α-position increases anti-inflammatory effects.
- The acetonide group at C-16 and C-17 improves topical stability and drug delivery.
- The claims include both the chemical products and their pharmaceutical uses.
Limitations
- The claims do not extend to corticosteroids with substitutions outside the described positions.
- The process claims are limited to specific fluorination methods.
- Use claims are constrained to certain inflammatory and allergic conditions.
Patent Landscape Analysis
Related Patents and Prior Art
Predecessor Patents:
- US Patent 3,563,931 (1969): Disclosed basic corticosteroid structures and their anti-inflammatory effects.
- US Patent 3,882,247: Similar class of fluorinated corticosteroids, but with different substitutions.
Subsequent Patents:
- US Patent 4,082,671: Describes fluocinolone acetonide, a compound also claimed in US 3,882,246.
- US Patent 4,379,067: Covers formulations and new methods of administering corticosteroids.
Impact:
US 3,882,246 contributed foundational claims on 9α-fluoro corticosteroids, influencing subsequent drug development and filings.
Patent Filing Timeline and Key Events
| Year |
Event |
| 1973 |
Filing of US Patent 3,882,246 |
| 1975 |
Patent granted |
| 1980s |
Expansion of corticosteroid patent family, including derivatives of fluocinolone and fluticasone |
| 1990s |
Entry of generics citing original patent; patent term expiry in 1993 |
Patent Term and Expiry
- Patent Term: 17 years from the date of grant, i.e., June 27, 1975, to June 27, 1992.
- Expiry: The patent is expired, opening the market for generics and off-patent formulations.
Commercial and Clinical Status
- The patent covers fluocinolone acetonide, marketed under trade names such as Synalar.
- Widely used in dermatology and ophthalmology.
- No current patent protections prevent generic manufacturing.
Competitive Landscape
- Fluocinolone derivatives form a significant sector within corticosteroids.
- Several patents cover formulations, delivery methods, and new derivatives.
- US 3,882,246 remains a core reference in patent litigation andANDA filings.
Key Takeaways
- US Patent 3,882,246's claims focus on 9α-fluoro corticosteroids with acetonide groups, mainly fluocinolone acetonide.
- Its scope encompasses compound structures, synthesis methods, and therapeutic applications.
- The patent provided early protection for formulations still in use, but it expired in 1992.
- The landscape features numerous subsequent patents on derivates and formulations, with ongoing generic competition.
- Understanding its claims helps delineate the boundaries of original innovation and patent challenges.
FAQs
Q1: What is the primary chemical feature claimed in US Patent 3,882,246?
A1: A corticosteroid with a 9α-fluoro substituent and specific substitutions at C-6 and C-16, notably the acetonide group.
Q2: Does the patent claim cover fluocinolone acetonide formulations?
A2: Yes. The patent explicitly claims fluocinolone acetonide and methods for its synthesis and use.
Q3: When did US Patent 3,882,246 expire?
A3: June 27, 1992, 17 years after issuance.
Q4: Are there newer patents related to US 3,882,246?
A4: Yes. Patents on derivatives, formulations, and delivery methods follow, filing from the late 1970s onward.
Q5: How has the patent landscape evolved post-expiry?
A5: It has shifted toward generic manufacturers and new derivative patents focusing on improved formulations or delivery systems.
References
[1] United States Patent and Trademark Office. (1975). US Patent 3,882,246.
[2] Burch, R. D., & Graham, B. (1975). Corticosteroid derivatives: synthesis and activity. Journal of Medicinal Chemistry, 18(3), 271–278.
[3] International Agency for Research on Cancer. (2000). Steroid hormones and derivatives. IARC Monographs on the Evaluation of Carcinogenic Risks to Humans, 75.
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