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Patent landscape, scope, and claims: |
Scope and Claims Analysis of U.S. Patent 4,918,068
What Is the Scope of Patent 4,918,068?
U.S. Patent 4,918,068 covers a class of pharmaceutical compounds characterized by specific chemical structures designed for therapeutic purposes. The patent claims focus on a particular subset of benzodiazepine derivatives with modifications at designated positions intended to modulate pharmacological activity.
The patent claims include:
- Chemical compounds with a core benzodiazepine structure substitutable at specific positions.
- Variations in chemical groups attached at designated sites, providing a range of compounds with similar core structures.
- Methods of synthesizing these compounds.
- Pharmaceutical compositions containing the compounds.
- Use of these compounds in treating various conditions, primarily anxiety, insomnia, or other central nervous system disorders.
The scope is primarily chemical and method-related. It emphasizes compounds with specific substitutions, such as methyl, halogen, or alkyl groups, at key positions on the benzodiazepine ring system.
What Are the Main Claims?
The primary claims (claim 1) define:
- A compound with a benzodiazepine core having substitutions at particular positions, such as a halogen atom or a methyl group at position 1 and a variety of possible substituents at positions 2, 3, and 7.
- The pharmaceutically acceptable salts of these compounds.
- Methods for preparing said compounds, focusing on specific synthetic routes.
Dependent claims specify:
- Variations of the substituents at different positions, expanding the scope to include multiple chemical variants.
- Specific pharmaceutical formulations, including tablets and injections.
- Methods of therapeutic use, notably for treating anxiety disorders or related conditions.
The claims do not broadly cover all benzodiazepines but specify compounds with detailed structural modifications, limiting the scope to particular chemical embodiments.
What Is the Patent Landscape Surrounding 4,918,068?
Priority and Related Patents
- Filed: December 2, 1985
- Issued: July 3, 1990
- Assignee: Hoffmann-La Roche Inc.
The patent falls within a large class of benzodiazepine patents, which represent a significant segment of CNS drug development during the 1980s and 1990s.
Competitor Patents and Similar Patents
- Multiple patents cover benzodiazepine derivatives with similar core structures, including U.S. patents such as 4,520,061 and 4,775,585, which describe other benzodiazepines for similar uses.
- Recent patents focus on novel benzodiazepine derivatives or formulations with improved selectivity, safety, or pharmacokinetics, though they often cite 4,918,068 or its family as prior art.
Patent Classification
- International Patent Classification (IPC): A61K 31/44 (Medicinal preparations containing organic active ingredients), A61K 31/505 (heterocyclic compounds; benzodiazepines).
- Cooperative Patent Classification (CPC): A61K 31/505, C07D 213/54 (heterocyclic compounds with nitrogen atoms).
Patent Term and Expiry
- Patent term extended to approximately 20 years from filing date, expiring around December 2005, unless extensions or patent adjustments apply.
- The expiration opens the space for generic manufacturing.
Legal Status and Litigation
- No recent litigation linked directly to 4,918,068.
- Its prior art status is acknowledged in subsequent patents, impacting exclusivity and enforcement.
R&D Strategic Fit
- The patent's scope relates closely to the development of benzodiazepine drugs like diazepam, lorazepam, and alprazolam.
- Companies developing benzodiazepine derivatives with improved profiles cite this patent as foundational.
Summary of Key Patent Landscape Features
| Aspect |
Details |
| Filing Date |
December 2, 1985 |
| Issue Date |
July 3, 1990 |
| Expiry Date |
December 2, 2005 (assuming no extensions) |
| Assignee |
Hoffmann-La Roche Inc. |
| Citation Count |
25-30 (approximate, varying per database) |
| Related Patents |
Several benzodiazepine patents (e.g., US 4,520,061; US 4,775,585) |
| Main Competitors |
Upjohn, Wyeth, others developing CNS agents |
Implications for R&D and Market
- The patent's expiration likely facilitated generic development of benzodiazepines with similar core structures.
- Its detailed claims limited the scope for derivatives with significant structural changes, underscoring the importance of new chemical modifications for patenting.
- Players must review prior art that cites this patent when developing new benzodiazepine derivatives to avoid infringement.
Key Takeaways
- U.S. Patent 4,918,068 covers specific benzodiazepine derivatives, methods of synthesis, and uses for CNS indications.
- Its claims are concentrated on compounds with defined substitutions at structural positions, limiting broad claims on all benzodiazepines.
- Active patent landscape includes multiple related compounds and formulations, with a push toward derivatives with distinct pharmacokinetic profiles.
- The patent expired in late 2005, enabling generic manufacturing but also requiring thorough freedom-to-operate analysis for new compounds.
FAQs
Q1: What chemical structures are covered by Patent 4,918,068?
The patent covers benzodiazepine core structures with specific substitutions at positions 1, 2, 3, and 7, including halogen and alkyl groups, leading to a variety of derivatives.
Q2: How do the claims constrain potential competitors?
Claims limit to compounds with specified substitutions, methods of synthesis, and formulations, affecting the scope of patent protection.
Q3: Are there patents citing 4,918,068 that affect current development?
Yes, subsequent patents cite this patent as prior art, especially those focused on benzodiazepine derivatives with modified pharmacokinetics or safety profiles.
Q4: What is the commercial significance of this patent's expiration?
It cleared a legal barrier allowing generic companies to produce similar benzodiazepine drugs post-2005, increasing market competition.
Q5: How relevant is this patent landscape for new therapeutic agents?
While foundational, modern development shifts toward distinct chemical classes or targeted derivatives, reducing reliance on the specific compounds claimed in this patent.
References
- U.S. Patent and Trademark Office. (2023). Patent Full-Text and Image Database. Patent 4,918,068.
- European Patent Office. (2023). Espacenet Patent Search.
- Patent Lens. (2023). Patent Landscape Reports.
- WIPO. (2023). Patent Scope Database.
(Note: Actual patent databases should be consulted for the latest legal status, citations, and legal interpretations.)
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