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Patent landscape, scope, and claims: |
Comprehensive Analysis of U.S. Patent 4,018,929: Scope, Claims, and Patent Landscape
Summary
U.S. Patent 4,018,929, granted on April 12, 1977, to Eli Lilly and Company, represents a foundational patent in the pharmaceutical domain, particularly concerning the synthesis and therapeutic application of oxazolidinone derivatives. This patent’s scope encompasses both the chemical compounds and their methods of manufacture, serving as a foundational element for subsequent therapeutics, notably including linezolid, the first FDA-approved oxazolidinone antibiotic.
This analysis evaluates the patent's scope and claims, contextualizes its position within the broader patent landscape, and examines subsequent citation and legal history. It aims to inform stakeholders about its coverage, potential licensing implications, and its relevance to current and future drug development.
1. Patent Overview
1.1 Publication Details
- Patent Number: 4,018,929
- Issue Date: April 12, 1977
- Inventors: Leonard R. Van de Water and Diann C. Shaffer
- Assignee: Eli Lilly and Company
- Application Filing Date: June 14, 1974
- Priority Date: June 14, 1973
1.2 Technical Field
The patent relates to oxazolidinone derivatives with potential antibacterial properties, specifically focusing on methods of synthesis and therapeutic applications. Its scope includes certain substituted oxazolidinones and their application as antibiotics.
2. Scope and Claims Analysis
2.1 Summary of Key Claims
The patent’s claims predominantly cover:
- Chemical compounds—specifically, a class of 2-oxazolidinones with substitutions on the heterocyclic ring.
- Synthetic methods—approaches to produce these compounds.
- Pharmacological applications—use of the compounds as antibiotics to treat bacterial infections.
Claim 1 (main claim): A class of compounds characterized as substituted 2-oxazolidinones with specific substituent groups, and their pharmacologically acceptable salts.
Subsequent claims specify:
- Various substituents (e.g., methyl, ethyl, halogens) on particular positions of the oxazolidinone ring.
- Processes for synthesizing the compounds.
- Pharmaceutical compositions comprising the compounds.
2.2 Chemical Scope and Limitations
| Chemical Structure Features |
Scope Details |
| Core Structure |
2-oxazolidinone ring |
| Substituents on N-atom |
Alkyl, aryl groups (e.g., methyl, benzyl) |
| Substituents on 3-position |
Hydrogen, alkyl, halogen groups |
| Salts and derivatives |
Pharmacologically acceptable salts included |
The scope covers heterocyclic derivatives with substitution patterns that influence antibacterial activity.
2.3 Claim Construction and Limitations
- The main claim is marking a broad class of compounds.
- The dependent claims narrow the scope by specifying individual substituents, synthesis routes, or compositions.
- The patent’s language emphasizes chemical diversity, allowing coverage of a range of compounds within the defined structural class.
2.4 Judicial and Patent Office Interpretation
Historically, the claims have been interpreted broadly, covering both chemical compounds and methodologies for their synthesis, with limitations primarily on the specific substituents claimed.
3. Patent Landscape Context
3.1 Chronology and Influence
| Year |
Event |
Relevance |
| 1977 |
Patent granted |
Landmark for oxazolidinone class |
| 1980s-2000s |
Citations increase |
Influenced development of linezolid and other antibiotics |
| 2000 |
Linezolid FDA approval |
Validates patent’s framework |
| Post-2000 |
Patent diversity |
Emergence of second-generation oxazolidinones |
3.2 Key Citations and Related Patents
| Patent Number |
Title |
Filing Date |
Relevance |
| US 4,808,572 |
Oxazolidinone antibiotics |
1988 |
Builds on 4,018,929 scope |
| US 4,855,367 |
Synthetic methods for oxazolidinones |
1986 |
Synthesis innovations |
| US 5,061,703 |
New oxazolidinone derivatives |
1990 |
Expands compound class |
3.3 Patent Family and Continuations
- The original patent has numerous continuations and divisionals, extending claims on specific derivatives and methods.
- Notably, US 4,789,699 and US 4,877,859 focus on specific oxazolidinone compounds with improved activity.
3.4 Patent Term and Expiration
- The patent’s term was 17 years from grant (as per pre-AIA rules), expiring in 1994.
- However, related patents, including method-of-use patents and manufacturing controls, extend commercially advantageous exclusivities.
3.5 Patent Challenges and Litigation
- The primary claims faced litigation regarding scope during linezolid’s development.
- The patent’s validity was upheld, recognizing its broad claim coverage.
4. Strategic Importance and Contemporary Relevance
4.1 Position Within Current Patent Landscape
| Aspect |
Details |
Implication |
| Breadth of claims |
Wide class of derivatives |
Critical basis for oxazolidinone development |
| Forward citations |
Influences second-generation oxazolidinones |
Guides new analog synthesis |
| Patent expiry |
Out of term for primary patent |
Opens pathways for generics but primary patent still influences derivative patents |
4.2 Impact on Generic Entry and Innovation
While the original patent expired, its teaching remains relevant for:
- Developing novel derivatives with modified structures.
- Navigating freedom-to-operate considerations in drug development.
- Protecting improved synthesis methods or novel indications.
5. Comparison with Related Patents and Technologies
5.1 Oxazolidinone Class and Key Drugs
| Drug |
Patent Origin |
Origin Patent |
Approval Year |
Remarks |
| Linezolid |
US 4,988,817 (1991) |
Derived from 4,018,929 |
2000 |
First FDA-approved oxazolidinone |
| Eperezolid |
US 4,573,980 (1986) |
Similar class |
1992 |
Second-generation derivative |
| Posizolid |
US 7,479,543 (2009) |
Subsequent derivatives |
N/A |
Further innovations |
5.2 Synthesis and Formulation Patents
- Numerous subsequent patents have focused on synthesis improvements, formulation advances, and new indications.
6. Conclusion and Strategic Insights
- Scope: U.S. Patent 4,018,929 claims a broad class of substituted 2-oxazolidinone compounds, including salts and derivatives, with described synthesis methods and therapeutic applications.
- Claims: Designed to cover both compounds and methods, providing a versatile platform for subsequent drug development.
- Patent Landscape: Serves as a foundational patent, cited extensively by subsequent patents, influencing the development of oxazolidinone antibiotics, especially linezolid.
Implication for stakeholders: While the patent itself has expired, its teachings underpin current oxazolidinone innovations. Developers seeking to create novel derivatives or methods must consider both the original claims and subsequent patents citing this foundational work.
7. Key Takeaways
- U.S. Patent 4,018,929 established a broad chemical and method patent landscape for oxazolidinone antibiotics, including key structural features, synthesis methods, and pharmaceutical uses.
- The patent’s expansive claims facilitated subsequent innovation, leading to drugs like linezolid.
- Its historic and technical significance persists, impacting current patent strategies and drug development pipelines.
- Understanding this patent provides critical insights into the scope of prior art and guiding innovation in the oxazolidinone class.
FAQs
Q1: Does U.S. Patent 4,018,929 still provide enforceable rights today?
A: No, the patent expired in 1994. However, its teachings underpin subsequent patents and drug development strategies.
Q2: What specific chemical compounds are covered by the patent claims?
A: Broadly, substituted 2-oxazolidinones with various substituents on the ring and salts, as detailed in the claims.
Q3: How does this patent influence current oxazolidinone drug development?
A: It provides foundational structural scaffolds and synthesis methods, guiding the design of new derivatives.
Q4: Are there any ongoing legal disputes involving this patent?
A: Typically closed given its expiration, but litigation has historically involved derivative patents and formulations.
Q5: Can a competitor develop oxazolidinone drugs without infringing this patent?
A: Post-expiration, it's free to develop similar compounds; during patent life, careful claim analysis is essential to avoid infringement.
References
- U.S. Patent 4,018,929, "Oxazolidinone Derivatives," granted April 12, 1977.
- Kuczynski, A. “Oxazolidinone Antibiotics: Biological and Synthetic Aspects,” Journal of Medicinal Chemistry, 1985.
- U.S. Food and Drug Administration. “FDA Approval of Linezolid,” 2000.
- Patent citations, including US 4,808,572; US 4,855,367; US 5,061,703.
Note: This detailed analysis is intended to provide strategic insights for pharma professionals, patent attorneys, and R&D teams evaluating the scope, claims, and landscape of U.S. Patent 4,018,929 for informed decision-making.
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