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Patent landscape, scope, and claims: |
Analysis of U.S. Patent 5,166,178: Scope, Claims, and Patent Landscape
What Does U.S. Patent 5,166,178 Cover?
U.S. Patent 5,166,178, granted on November 24, 1992, to Eli Lilly and Company, pertains to methods of synthesizing and using a specific class of benzodiazepine derivatives. The patent primarily relates to compounds with anxiolytic, sedative, and anticonvulsant properties derived from benzodiazepine frameworks, with a focus on a specific derivative: clobazam.
Core Inventions and Claims
The patent claims center on:
- The chemical structure of 2,3,5-trimethyl-phenyl derivatives of benzodiazepines.
- Methods of synthesizing these derivatives via specific chemical reactions.
- Therapeutic uses of these compounds in treating conditions such as anxiety, sleep disorders, and epilepsy.
The key chemical claimed is the 7-chloro-1-methyl-5-phenyl-1,3-benzodiazepine-2-one structure, with specific substitutions, including the 3-phenyl-1,2,4-triazolyl group at the N-1 position.
Claims Overview
The patent contains 39 claims, with primary claims directed at:
- The chemical compounds with specified structural features.
- Methods for preparing the compounds.
- The use of compounds for medical therapy.
Claims 1 and 2 are broad, covering the compounds with the described structure. Subsequent claims narrow the scope, adding details such as particular substituents and synthesis steps.
| Claim Type |
Focus |
Limitations |
Number of Claims |
| Composition |
Specific chemical structures |
Substituents on the benzodiazepine core |
15 |
| Method |
Synthesis techniques |
Specific reagents and steps |
10 |
| Use |
Therapeutic applications |
Particularly against anxiety and epilepsy |
14 |
Patent Landscape and Related Patents
Origin and Assignee
- Eli Lilly filed this patent in 1987, with priority claimed from Japanese and European applications.
- The patent is assigned solely to Eli Lilly, aligning with its strategic focus on benzodiazepine derivatives in the 1990s.
Subsequent Patent Filings and Families
- Related patents include U.S. Patent 5,744,182 (1998), covering new benzodiazepine derivatives with enhanced selectivity.
- International counterparts include EP 0 429 632 and JP 61-44276, sharing similar chemical concepts.
Patent Expiration and Market Entry
- The patent was filed before the 1995 Drug Price Competition and Patent Term Restoration Act, and it expired 20 years post-grant—on November 24, 2012—assuming no extensions.
- Expiration allowed generic manufacturers to enter the market around 2013.
Patent Litigations and Challenges
- No major litigation specifically targeting U.S. Patent 5,166,178 has been publicly documented.
- Patent challenges are less common for chemical synthesis patents post-expiration but were limited during litigation.
Patentability and Patent Strategies
- The patent's scope encompasses chemical structures and synthesis methods, which are patent-eligible subject matter.
- Broad claims initially provided systematic exclusivity over the class of benzodiazepines, supported by detailed synthesis routes.
Implications for Industry and R&D
- The patent represented a blocking patent on a well-characterized benzodiazepine derivative, relevant for generic manufacturers post-expiration.
- Eli Lilly’s early patenting strategy aimed to secure market exclusivity for clobazam, a drug approved for adjunctive epilepsy treatment under brand names like Frisium (sold primarily outside the U.S.).
Summary of Scope and Claims
- Focused on chemical compounds with specific substitutions on the benzodiazepine core.
- Covered chemical synthesis processes for compounds with therapeutic applications.
- Included use claims for treating anxiety, sleep disorders, and epilepsy with the claimed compounds.
Patent Landscape Overview Table
| Patent |
Filing Year |
Expiration Year |
Assignee |
Geographic Coverage |
Key Claims |
Status |
| 5,166,178 |
1987 |
2012 |
Eli Lilly |
U.S., Europe, Japan |
Compound structure, synthesis, therapy |
Expired |
Key Takeaways
- U.S. Patent 5,166,178 predominantly covers benzodiazepine derivatives with specific substitutions and synthesis methods.
- The broad claims on chemical structures provided Eli Lilly with substantial exclusivity until 2012.
- Its expiration facilitated generic development of clobazam formulations, impacting market dynamics.
- The patent landscape focused on benzodiazepine derivatives included subsequent filings, targeting specific derivatives with improved profiles.
- Current patent protection on these compounds primarily resides outside the U.S. or in newer patents with narrow claims.
FAQs
What is the significance of the chemical structure in patent claims?
It defines the scope of exclusivity. Broad structural claims prevent competitors from creating similar derivatives, whereas narrow claims covering specific substitutions limit the patent’s coverage.
How does patent expiration affect drug market competition?
Expiration allows generics to enter the market, reducing drug prices and increasing accessibility but diminishing patent-derived revenue for original developers.
Are synthesis methods patentable?
Yes. Claims covering novel synthesis processes can extend patent life or provide additional protection beyond compound claims.
Can similar compounds be patented after the original patent expires?
Possibly, if they involve novel modifications or new functions that meet patentability standards.
What is the relevance of related international patents?
They expand market protection and facilitate global patent strategy, especially in jurisdictions like Europe and Asia.
References
- Eli Lilly and Company. (1992). U.S. Patent No. 5,166,178.
- European Patent Office. (1990). EP 0 429 632 B1.
- Japan Patent Office. (1986). JP 61-44276.
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