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Patent landscape, scope, and claims: |
Scope and Claims of U.S. Patent 5,873,360
U.S. Patent 5,873,360, issued on February 23, 1999, is titled "Benzodiazepine derivatives" and claims the chemical class, uses, and specific compounds within that class.
Scope of the Patent
The patent broadly covers benzodiazepine derivatives with specific structural features. It encompasses:
- Chemical entities comprising substituted benzodiazepine cores.
- Methods of synthesizing these derivatives.
- Pharmaceutical compositions containing these derivatives.
- Therapeutic uses, particularly as anxiolytics, sedatives, or anticonvulsants.
The patent emphasizes compounds with certain substitutions at defined positions on the benzodiazepine ring system, enabling the patent to claim a broad genus of derivatives with potential therapeutic activity.
Claims Breakdown
The patent contains 19 claims (1-19):
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Claim 1: Defines a class of benzodiazepine derivatives with a general formula, detailing substituent groups at specific positions (e.g., R1, R2, R3). It is broad, covering any compound fitting the formula with the specified substituents.
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Claims 2-4: Specify particular substituents for R1, R2, and R3, narrowing the scope to specific derivatives. These are dependent claims expanding on Claim 1.
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Claims 5-8: Cover methods of preparing the compounds with detailed chemical processes, including intermediates and reaction conditions.
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Claims 9-11: Concern pharmaceutical compositions—formulations, dosages, and administration routes using these compounds.
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Claims 12-16: Cover therapeutic applications, especially for treating conditions like anxiety, insomnia, or seizures, linking compounds to medical indications.
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Claims 17-19: Control or specify uses and formulations, possibly including polymorphs or salts.
Key Aspects of Claims
- The broadness of Claim 1 secures a wide chemical space, claiming all derivatives fitting the core formula with various substituents.
- Narrower claims focus on specific compounds with particular substituents, allowed by initial broad claims.
- Claims related to synthesis methods and formulations strengthen patent coverage over manufacturing.
Patent Landscape and Similar Patents
The patent landscape around benzodiazepines and similar anxiolytics is extensive:
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Overlap with prior art: Several patents from the 1970s to 1990s mention benzodiazepine derivatives with anxiolytic uses.
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Citations and related patents: U.S. Patents such as 4,062,751 (issued to Roche in 1977) and 4,622,329 (AstraZeneca, 1986) cover subclasses of benzodiazepines.
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Continuation applications: The patent references or has been referenced in later applications, indicating ongoing patenting activity around derivatives and methods.
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Infringement risk: Generics or competitors developing benzodiazepine derivatives with similar structures could face patent infringement if claims overlap.
Legal and Market Context
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The patent’s expiration date is February 23, 2017, assuming maintenance fee payments were made. This broad patent likely played a significant role in protecting specific derivatives and formulations until its expiration.
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Similar compounds and new derivatives continue to be patented, but the expiration opens market entry for generics.
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Patent disputes historically involve key benzodiazepine compounds, especially when new derivatives show improved efficacy or safety.
Summary
U.S. Patent 5,873,360 claims a broad class of benzodiazepine derivatives with medicinal applications, with specific claims narrowing down to particular compounds and methods. The patent landscape is populated with overlaps and related filings, indicative of intense R&D activity. Its expiration in 2017 likely allowed generic manufacturers to enter the market for covered compounds.
Key Takeaways
- The patent protects a wide chemical space of benzodiazepine derivatives with specific therapeutic claims.
- Claims include compound structures, synthesis methods, and medical uses.
- The patent landscape is dense, with prior art spanning several decades.
- Expiration in 2017 opened potential for generic drug development in the covered class.
FAQs
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What is the main chemical invention in U.S. Patent 5,873,360?
It is a broad class of benzodiazepine derivatives with specific substitutions, covering compounds with anxiolytic and sedative properties.
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How broad are the claims?
Claim 1 covers a large genus of compounds fitting a specific chemical formula, with subsequent claims narrowing scope to specific derivatives and uses.
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Are there active patents similar to this one?
Yes; numerous patents from the 1970s to 2000s cover benzodiazepines with similar structures and applications, forming a dense patent landscape.
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When did the patent expire, and what does that imply?
The patent expired on February 23, 2017, allowing generics to enter the market, assuming all maintenance fees were paid.
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Could new derivatives still infringe on this patent?
It depends on their chemical structure; derivatives falling within the claimed genus could infringe if the claims are still enforceable or not invalidated.
Sources
- USPTO Patent Full-Text and Image Database. U.S. Patent No. 5,873,360.
- EPO PATSTAT and other patent databases.
- Prior art references cited within the patent.
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