|
Patent landscape, scope, and claims: |
Summary:
Patent 5,750,561, granted to Eli Lilly and Company in 1998, covers a class of benzodiazepine derivatives characterized by specific chemical structures and their potential therapeutic applications, primarily in central nervous system disorders. The patent claims focus on the compound's chemical composition, synthesis methods, and therapeutic utility. The patent landscape reveals a dense network of related patents targeting benzodiazepines, anxiolytics, and sedatives, with numerous filings across the globe, especially in the US, Europe, and Japan. The patent's scope broadly covers derivatives with similar core structures, potentially impacting generic entry and biosimilar development.
What is the scope of Patent 5,750,561?
Core Chemical Structures and Claims
Patent 5,750,561 claims a family of benzodiazepine derivatives with specific substitutions on the benzodiazepine core. The key structural features include:
- A benzodiazepine ring fused with various substituents at defined positions.
- Substituents on the phenyl rings, such as methyl, chloro, or methoxy groups differentiating compounds.
- A methylene linker connecting the core to diverse side chains.
The claims specify compounds where the substituents influence receptor affinity, primarily for GABA_A receptors, conferring anxiolytic, sedative, or anticonvulsant activities.
Independent Claims:
- Cover a genus of compounds with a core benzodiazepine skeleton substituted with particular groups.
- Cover methods for preparing these compounds, emphasizing synthesis pathways involving conventional organic reactions.
- Cover pharmaceutical compositions comprising these compounds along with carriers or excipients.
Dependent Claims:
Describe specific derivatives with particular substituent patterns, such as:
- 1,4-benzodiazepine compounds substituted with methyl or chloro groups at specific positions.
- Variations in side chains attached to the core via methylene or ethylene bridges.
Scope Limitations
- Chemical scope limited to compounds with specified substitutions, but broad enough to encompass multiple derivatives within the structural framework.
- Claim language explicitly indicates coverage of both the compounds themselves and processes for their synthesis.
How does the patent landscape for US benzodiazepines look?
Related Patents and Patent Families
Numerous patents address benzodiazepines and their derivatives. Major players include:
- Eli Lilly: Multiple filings related to benzodiazepine derivatives, including blocking patents on specific compounds and formulations.
- Roche, Pfizer, Schering-Plough: Filed patents covering specific benzodiazepine compounds, methods of use, and formulations.
- International filings: Similar patents exist in Europe, Japan, and China, reflecting global research efforts.
Key Patent Clusters
- Structure-based patents: Cover modifications of the core benzodiazepine skeleton.
- Use patents: Cover methods for treating anxiety, insomnia, or seizures with specific derivatives.
- Method-of-synthesis patents: Focus on efficient synthetic pathways for benzodiazepine derivatives.
Expiration and Freedom-To-Operate (FTO)
- Patent 5,750,561 expires on 2018, prior to the current date, and thus no longer blocks generic manufacturing of the claimed compounds.
- Remaining patents related to specific derivatives or formulation patents may extend exclusivity until 2025–2030 depending on the jurisdiction.
What are the claims' specific innovations?
- Structural specificity: The patent claims compounds with particular substitution patterns on the benzodiazepine core, aiming for specific receptor activity profiles.
- Broad coverage: The claims do not limit to a single compound but cover a class, enabling coverage of many derivatives within the defined structural boundaries.
- Synthesis methods: Patent claims include specific synthetic routes, potentially offering a competitive advantage for manufacturing compounds.
Implications for current and future R&D
- The patent landscape indicates a navigable path for development of new benzodiazepine derivatives that avoid claim overlap.
- Existing patents on specific derivatives or formulations may block certain markets until expiration.
- The broad structural claims suggest that any new derivatives sharing key features could infringe, unless designed outside the scope.
Key Takeaways
- Patent 5,750,561 claims a broad class of benzodiazepine derivatives with therapeutic applications for CNS disorders.
- The patent covers both specific compounds and methods of synthesis, with claims spanning multiple structural variants.
- The patent expired in 2018, removing barriers for generic development based on this specific patent.
- The current patent landscape remains active with multiple filings, particularly patents covering formulations, method of use, and derivatives with similar core structures.
- Understanding specific claim language and structure is critical for designing non-infringing compounds or assessing freedom to operate.
FAQs
1. What are the main structural features claimed in Patent 5,750,561?
A fused benzodiazepine ring with specific substitutions at defined positions, including methyl, chloro, and methoxy groups, attached via methylene or ethylene linkers.
2. Does the patent cover all benzodiazepine derivatives?
No. It specifically claims derivatives with particular substitutions on the benzodiazepine core, not every benzodiazepine.
3. How does the expiration date affect patent rights?
Since the patent expired in 2018, it no longer provides exclusivity, allowing generic or biosimilar development based on the claimed compounds.
4. Are there similar active patents in other jurisdictions?
Yes. Similar patents exist in Europe, Japan, and other markets, with varying expiration dates and claim scopes.
5. Would developing a new benzodiazepine derivative infringe this patent today?
Potentially not, if the derivative does not fall within the patent's specific structural claims, especially after patent expiration.
References
- U.S. Patent 5,750,561.
- Patent landscape reports on benzodiazepines, IP.com.
- WHO. Benzodiazepines: Pharmacology and Use.
- FDA Orange Book – Approved Drug Products.
- European Patent Office database.
More… ↓
⤷ Start Trial
|
