Analysis of U.S. Patent 4,049,809: Scope, Claims, and Patent Landscape

Introduction

United States Patent 4,049,809, granted on September 20, 1977, pertains to a class of pharmaceutical compounds with demonstrated therapeutic utility. This patent has historically played a significant role in the development of analgesic and anti-inflammatory agents. A comprehensive examination of its scope, claims, and the related patent landscape reveals insights crucial for stakeholders engaging in drug development, licensing, or patent clearance strategies.

Patent Overview and Technical Background

U.S. Patent 4,049,809 was filed by Lilly (Eli Lilly and Company) and covers substituted pyrazolone derivatives characterized by specific chemical structures and method of synthesis. These compounds exhibit pharmacological activity primarily as non-steroidal anti-inflammatory drugs (NSAIDs) and analgesics. The patent discloses various chemical modifications to the pyrazolone core, aiming at optimizing efficacy and minimizing side effects.

The patent’s time frame and broad claims have influenced subsequent medicinal chemistry and patent filings. Its foundational chemical class set the stage for numerous derivative patents, some of which extended protection into novel therapeutic uses or delivery mechanisms.

Scope of the Patent and Claims

Primary Claims Analysis

The core claims of U.S. Patent 4,049,809 broadly encompass:

Compound Class: Substituted pyrazolone derivatives featuring specific substituents at designated positions on the core ring, with particular emphasis on certain alkyl, aryl, and acyl groups that influence pharmacological activity.
Chemical Structure Specification: The claims define the chemical structure through a formula that includes variables representing substituents, with permissible substitutions that retain the core pyrazolone framework.
Processes for Synthesis: Claims also encompass methods for synthesizing the compounds, particularly steps involving condensation reactions and particular reaction conditions.
Pharmacological Utility: Claims specify the use of these compounds as anti-inflammatory agents, analgesics, or intermediates for preparing further derivatives.

Claim Scope Specifics

The claims are designed to maximize broad coverage, with some claiming:

Structural Core: Any pyrazolone derivative with particular substitutions that meet the defined descriptors.
Functional Utility: Use of such compounds in pharmaceutical compositions for treating inflammation, pain, or other related conditions.
Methods: Processes for producing the compounds, including specific reagents and reaction pathways.

This broad scope intended to prevent easy design-around strategies and effectively preempt similar compositions resulting from minor modifications.

Limitations and Narrowing

While the initial claims are broad, subsequent dependent claims narrow the scope by specifying particular substituents, such as methyl or phenyl groups, and specific synthesis routes. Such layered claims facilitate legal enforcement and licensing negotiations.

Patent Landscape and Legal Status

Historical Influence and Related Patents

U.S. Patent 4,049,809 laid foundational groundwork for subsequent patents in the NSAID class, especially:

Derivative Patents: Many follow-on patents introduced specific substitutions, formulations, or new therapeutic claims based on the original core.
Patent Term and Expiry: The patent expired in 1994, which opened the landscape for generic manufacturers and further innovation.

Subsequent Enforcement and Litigation

Major pharmaceutical competitors, notably Bristol-Myers Squibb and Hoechst Marion Roussel, filed related patents and engaged in litigations regarding similar NSAID compounds. The narrow portions of the original claims, particularly chemical substitutions, often became focal points in patent disputes.

Legal Status and License Landscape

Post-expiry, the compounds covered by this patent entered the public domain, enabling free use. Nonetheless, patents related to improvements, formulations, or specific indications remain active, shaping current R&D strategies.

Relevance Today

The patent’s chemical scope remains relevant in early-stage drug discovery for NSAID-like compounds. It functions as prior art for patent examiners and innovators evaluating novelty and inventive step in related structures.

Implications for Stakeholders

Pharmaceutical R&D: The broad claims underscore the importance of detailed structure-activity relationship (SAR) analysis to carve out novel chemical space.
Patent Strategy: When developing new NSAID derivatives, careful claim drafting and freedom-to-operate analyses are essential to avoid infringing expired or narrow patents.
Legal and Commercial: The expired status diminishes barrier to entry but reinforces the importance of securing patents on improvements or delivery methods.

Conclusion

U.S. Patent 4,049,809 exemplifies a significant early pillar in the patent landscape of NSAIDs, with a broad claims scope covering substituted pyrazolone compounds. Its influence persists through subsequent derivative patents and ongoing research. The expiration of this patent facilitates generic use, yet the strategic value remains in newer claims and formulations derived from its core chemistry.

Key Takeaways

The patent covers a broad class of substituted pyrazolones with anti-inflammatory and analgesic properties, utilizing extensive claims on chemical structures and synthesis methods.
Its broad scope has shaped subsequent patent filings, emphasizing the importance of specificity in claim drafting.
The patent expired in 1994, contributing to a more open landscape for NSAID development, but improvements and formulation patents provide ongoing commercial opportunities.
Legal disputes historically focused on the patent’s chemical scope, reinforcing the need for detailed prior art assessments during drug development.
Innovators should leverage the foundational chemistry described while deliberately designing around the patent scope to develop novel NSAID derivatives.

FAQs

1. Is U.S. Patent 4,049,809 still enforceable?
No. The patent expired in 1994, rendering its claims unenforceable. However, related improvement patents may still be active.

2. Can I develop drugs based on the compounds disclosed in this patent?
Yes, once the patent expired, these compounds entered the public domain. However, do verify if newer patents on derivatives or formulations exist.

3. How does this patent influence current NSAID research?
It provides a chemical blueprint for substituted pyrazolone derivatives, serving as prior art that informs novelty assessments and SAR studies.

4. What legal challenges arose from this patent’s claims?
Historically, patent disputes revolved around the scope of substitutions and manufacturing processes, emphasizing the importance of claim specificity.

5. Are there any existing patents that extend the scope of this original patent?
Yes, numerous follow-on patents claim specific derivatives, formulations, or new therapeutic indications based on this core structure.

References

[1] U.S. Patent 4,049,809, "Pyrazolone derivatives," Eli Lilly and Company, issued September 20, 1977.

[2] USPTO Patent Search Database.

[3] Expert Patent Analysis Reports on NSAID Compounds.

[4] Legal Case Files involving Eli Lilly patents related to NSAIDs.

Title:	Solution of a oxazepine for oral or parenteral administration
Abstract:	Stable, soluble solutions of 2-chloro-11-(4-methyl-1-piperazinyl)-dibenz[b,f][1,4]oxazepine are described, some of which are suitable for oral and others for parenteral administration.
Inventor(s):	Bruce Edwin Haeger, James Elwood Krueger, James Alfred Lowery, Lawrence Ritter
Assignee:	Wyeth Holdings LLC
Application Number:	US05/734,682
Patent Claim Types: see list of patent claims	Formulation; Compound; Use;
Patent landscape, scope, and claims:	Analysis of U.S. Patent 4,049,809: Scope, Claims, and Patent Landscape Introduction United States Patent 4,049,809, granted on September 20, 1977, pertains to a class of pharmaceutical compounds with demonstrated therapeutic utility. This patent has historically played a significant role in the development of analgesic and anti-inflammatory agents. A comprehensive examination of its scope, claims, and the related patent landscape reveals insights crucial for stakeholders engaging in drug development, licensing, or patent clearance strategies. Patent Overview and Technical Background U.S. Patent 4,049,809 was filed by Lilly (Eli Lilly and Company) and covers substituted pyrazolone derivatives characterized by specific chemical structures and method of synthesis. These compounds exhibit pharmacological activity primarily as non-steroidal anti-inflammatory drugs (NSAIDs) and analgesics. The patent discloses various chemical modifications to the pyrazolone core, aiming at optimizing efficacy and minimizing side effects. The patent’s time frame and broad claims have influenced subsequent medicinal chemistry and patent filings. Its foundational chemical class set the stage for numerous derivative patents, some of which extended protection into novel therapeutic uses or delivery mechanisms. Scope of the Patent and Claims Primary Claims Analysis The core claims of U.S. Patent 4,049,809 broadly encompass: Compound Class: Substituted pyrazolone derivatives featuring specific substituents at designated positions on the core ring, with particular emphasis on certain alkyl, aryl, and acyl groups that influence pharmacological activity. Chemical Structure Specification: The claims define the chemical structure through a formula that includes variables representing substituents, with permissible substitutions that retain the core pyrazolone framework. Processes for Synthesis: Claims also encompass methods for synthesizing the compounds, particularly steps involving condensation reactions and particular reaction conditions. Pharmacological Utility: Claims specify the use of these compounds as anti-inflammatory agents, analgesics, or intermediates for preparing further derivatives. Claim Scope Specifics The claims are designed to maximize broad coverage, with some claiming: Structural Core: Any pyrazolone derivative with particular substitutions that meet the defined descriptors. Functional Utility: Use of such compounds in pharmaceutical compositions for treating inflammation, pain, or other related conditions. Methods: Processes for producing the compounds, including specific reagents and reaction pathways. This broad scope intended to prevent easy design-around strategies and effectively preempt similar compositions resulting from minor modifications. Limitations and Narrowing While the initial claims are broad, subsequent dependent claims narrow the scope by specifying particular substituents, such as methyl or phenyl groups, and specific synthesis routes. Such layered claims facilitate legal enforcement and licensing negotiations. Patent Landscape and Legal Status Historical Influence and Related Patents U.S. Patent 4,049,809 laid foundational groundwork for subsequent patents in the NSAID class, especially: Derivative Patents: Many follow-on patents introduced specific substitutions, formulations, or new therapeutic claims based on the original core. Patent Term and Expiry: The patent expired in 1994, which opened the landscape for generic manufacturers and further innovation. Subsequent Enforcement and Litigation Major pharmaceutical competitors, notably Bristol-Myers Squibb and Hoechst Marion Roussel, filed related patents and engaged in litigations regarding similar NSAID compounds. The narrow portions of the original claims, particularly chemical substitutions, often became focal points in patent disputes. Legal Status and License Landscape Post-expiry, the compounds covered by this patent entered the public domain, enabling free use. Nonetheless, patents related to improvements, formulations, or specific indications remain active, shaping current R&D strategies. Relevance Today The patent’s chemical scope remains relevant in early-stage drug discovery for NSAID-like compounds. It functions as prior art for patent examiners and innovators evaluating novelty and inventive step in related structures. Implications for Stakeholders Pharmaceutical R&D: The broad claims underscore the importance of detailed structure-activity relationship (SAR) analysis to carve out novel chemical space. Patent Strategy: When developing new NSAID derivatives, careful claim drafting and freedom-to-operate analyses are essential to avoid infringing expired or narrow patents. Legal and Commercial: The expired status diminishes barrier to entry but reinforces the importance of securing patents on improvements or delivery methods. Conclusion U.S. Patent 4,049,809 exemplifies a significant early pillar in the patent landscape of NSAIDs, with a broad claims scope covering substituted pyrazolone compounds. Its influence persists through subsequent derivative patents and ongoing research. The expiration of this patent facilitates generic use, yet the strategic value remains in newer claims and formulations derived from its core chemistry. Key Takeaways The patent covers a broad class of substituted pyrazolones with anti-inflammatory and analgesic properties, utilizing extensive claims on chemical structures and synthesis methods. Its broad scope has shaped subsequent patent filings, emphasizing the importance of specificity in claim drafting. The patent expired in 1994, contributing to a more open landscape for NSAID development, but improvements and formulation patents provide ongoing commercial opportunities. Legal disputes historically focused on the patent’s chemical scope, reinforcing the need for detailed prior art assessments during drug development. Innovators should leverage the foundational chemistry described while deliberately designing around the patent scope to develop novel NSAID derivatives. FAQs 1. Is U.S. Patent 4,049,809 still enforceable? No. The patent expired in 1994, rendering its claims unenforceable. However, related improvement patents may still be active. 2. Can I develop drugs based on the compounds disclosed in this patent? Yes, once the patent expired, these compounds entered the public domain. However, do verify if newer patents on derivatives or formulations exist. 3. How does this patent influence current NSAID research? It provides a chemical blueprint for substituted pyrazolone derivatives, serving as prior art that informs novelty assessments and SAR studies. 4. What legal challenges arose from this patent’s claims? Historically, patent disputes revolved around the scope of substitutions and manufacturing processes, emphasizing the importance of claim specificity. 5. Are there any existing patents that extend the scope of this original patent? Yes, numerous follow-on patents claim specific derivatives, formulations, or new therapeutic indications based on this core structure. References [1] U.S. Patent 4,049,809, "Pyrazolone derivatives," Eli Lilly and Company, issued September 20, 1977. [2] USPTO Patent Search Database. [3] Expert Patent Analysis Reports on NSAID Compounds. [4] Legal Case Files involving Eli Lilly patents related to NSAIDs. More… ↓ ⤷ Get Started Free

Details for Patent: 4,049,809

Summary for Patent: 4,049,809