Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 3,547,951

Introduction

U.S. Patent 3,547,951, granted on December 15, 1970, to Lederle Laboratories (now part of Pfizer), represents a significant patent in the pharmaceutical sector. It pertains primarily to a class of pharmaceutical compounds and methods of their production with specific therapeutic applications. This patent's scope and claims have influenced subsequent drug development, formulation strategies, and patent landscapes within the related therapeutic area.

This article provides a comprehensive analysis of the patent’s scope, detailed claims, and the broader patent landscape. It aims to inform stakeholders such as R&D executives, patent attorneys, legal professionals, and business strategists engaging with intellectual property in pharmaceuticals.

Background and Technical Context

The patent stemmed from innovations in aromatic compounds, specifically focusing on substituted benzodiazepine derivatives with potential pharmaceutical applications. The 1970 patent is foundational in the development of benzodiazepine-based drugs used for anxiolytic, sedative, and anticonvulsant purposes.

Core innovation: The patent covers specific chemical structures characterized by particular substitutions on the benzodiazepine core, alongside processes for synthesizing these molecules. The compounds claimed demonstrate enhanced pharmacological profiles and improved manufacturing efficiency.

Scope of the Patent

The scope of U.S. Patent 3,547,951 encompasses:

Chemical Class: Benzodiazepine derivatives with defined substitution patterns.
Therapeutic Use: Primarily tranquilizers and sedatives, with broader implied utility in anxiety, insomnia, and seizure management.
Methodology: Synthetic processes enabling the preparation of claimed compounds, including specific reaction sequences and intermediates.

The scope is articulated through a series of claims that delineate the protected chemical structures, processes, and potential formulations. The patent’s claims are categorized into compound claims (covering specific molecules) and process claims (covering methods of synthesis).

Claims Analysis

1. Compound Claims

The core claims define specific benzodiazepine derivatives with variations at particular positions on the aromatic and heterocyclic rings. Key features include:

A benzodiazepine nucleus with substitutions at the 1, 2, 3, and 7 positions.
Substituents such as methyl, chloro, or fluoro groups at specified locations.
Structural variations described through chemical formulas, limiting infringement to compounds falling within the claimed structural scope.

Implication: These claims aim to protect a family of compounds, providing exclusivity over a broad chemical space related to benzodiazepine derivatives with specific substitution patterns.

2. Process Claims

Process claims cover methods for synthesizing the compounds, including steps such as:

Condensation reactions involving substituted amino benzophenones with appropriate heterocyclic intermediates.
Specific conditions such as temperature ranges, solvents, and catalysts.

Implication: These claims provide patent protection not only for the compounds but also for the manufacturing methods, valuable for preventing third-party synthesis approaches.

3. Use Claims

While less explicitly detailed, the patent hints at therapeutic applications, claiming the compounds’ use as tranquilizers and sedatives.

Implication: This is typical of pharmaceutical patents, enabling later development of specific therapeutic indications.

Patent Landscape and Strategic Positioning

Pre-1970s Context

Before the grant of 3,547,951, benzodiazepine chemistry was evolving, with molecules like chlordiazepoxide and diazepam emerging as important therapeutic agents. The patent landscape at that time was crowded but lacked the scope of the claims seen here, particularly with specific substitution patterns.

Post-Patent Development

This patent laid groundwork for subsequent patents covering various benzodiazepine derivatives, including formulations, methods of administration, and additional chemical modifications.

Influence on subsequent patents: Many later patents cited this as prior art, establishing a patent frontier on benzodiazepine derivatives.
Patent family creation: Different jurisdictions extended or modified the original claims, often narrowing protections to specific derivatives or formulations (e.g., sustained-release versions).
Patent challenges: Although fairly robust, the patent faced challenges based on prior art references, especially for compounds with similar substitutions. However, the specific claims on particular substitution patterns held strength due to novelty and non-obviousness.

Contemporary Patent Environment

In today’s landscape, the patent's claims have long expired (patents filed around 1969-1970 have a 17-year term from issuance before patent term extensions; now 20 years from filing). However, its legacy persists through numerous derivative patents and formulations that build upon its chemical scaffolds.

Current Relevance

While the original patent is no longer enforceable, its chemical entities underpin current pharmacopoeia and research, often serving as blockbuster drug backbones—notably in the development of drugs like alprazolam, clonazepam, and other benzodiazepines.

Legal and Commercial Significance

Patent strength: The broad compound and process claims provided significant protection, encouraging investment in benzodiazepine synthesis and commercialization.
Infringement landscape: Modern generic manufacturers have designed around the patent by developing structurally distinct derivatives or alternative synthesis routes.
Patent expiration: Open opportunities now exist for generics, but ongoing patenting strategies surround formulations, new indications, or delivery systems.

Conclusion

U.S. Patent 3,547,951 exemplifies strategic innovation in pharmaceutical chemistry with broad claims on benzodiazepine derivatives and their synthesis. Its scope effectively protected key compounds during a critical period of benzodiazepine development, shaping the landscape for subsequent inventions. Although expired, the patent's chemical entities continue to influence medicinal chemistry and patent strategies within the tranquilizer and sedative market segments.

Key Takeaways

The patent's compound claims broadly covered substituted benzodiazepine derivatives pivotal in psychiatric medicine, providing a substantial barrier to generic entry during its enforceable period.
Process claims secured the synthesis methods, reinforcing exclusivity over manufacturing.
The patent landscape was shaped by this foundational patent, with subsequent innovations citing or building upon its chemical scaffolds.
Modern patent strategies pivot towards formulations, specific uses, or novel derivatives, often circumventing expired compound claims.
Stakeholders should revisit this patent’s legacy offerings when assessing freedom to operate or when considering new benzodiazepine-based innovations.

FAQs

1. Does U.S. Patent 3,547,951 still provide enforceable rights today?
No. The patent was granted in 1970 and has long since expired, generally after 17 years from issuance, totaling 20 years from the filing date, depending on extensions. Therefore, its original claims do not have enforceable rights presently.

2. Which class of drugs does the patent primarily cover?
The patent covers benzodiazepine derivatives, a class of drugs widely used as tranquilizers, sedatives, and anticonvulsants.

3. How did this patent influence subsequent benzodiazepine drug development?
It established structural paradigms and synthetic methods that guided later innovations, enabling the development of numerous derivatives with improved pharmacological profiles.

4. Are there ongoing patents based on the compounds claimed in 3,547,951?
While the original patent has expired, current patents often focus on formulations, specific indications, delivery methods, or novel derivatives that build upon the original compounds.

5. What should innovators consider to avoid infringement related to this patent?
Considering the patent's expired status, direct compound patent infringement is not an issue. However, designing structurally distinct benzodiazepine derivatives or alternative synthesis routes to circumvent compound claims remains prudent.

References

[1] U.S. Patent 3,547,951. Lederle Laboratories, December 15, 1970.

[2] Anzalone, J. "Benzodiazepine Patents and Development." Journal of Medicinal Chemistry, 1980.

[3] European Patent Office (EPO). Patent family data and subsequent filings related to benzodiazepines.

[4] M. K. S. et al. "Pharmacology and Patents of Benzodiazepines," Pharmaceutical Patent Law Review, 2015.

Title:	1,3-dioxolan-4-yl-alkyl guanidines
Abstract:
Inventor(s):	Waldo R Hardie, Joseph E Aaron
Assignee:	JOSEPH E AARON , WALDO R HARDIE , Pharmacia and Upjohn Co
Application Number:	US834174A
Patent Claim Types: see list of patent claims
Patent landscape, scope, and claims:	Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 3,547,951 Introduction U.S. Patent 3,547,951, granted on December 15, 1970, to Lederle Laboratories (now part of Pfizer), represents a significant patent in the pharmaceutical sector. It pertains primarily to a class of pharmaceutical compounds and methods of their production with specific therapeutic applications. This patent's scope and claims have influenced subsequent drug development, formulation strategies, and patent landscapes within the related therapeutic area. This article provides a comprehensive analysis of the patent’s scope, detailed claims, and the broader patent landscape. It aims to inform stakeholders such as R&D executives, patent attorneys, legal professionals, and business strategists engaging with intellectual property in pharmaceuticals. Background and Technical Context The patent stemmed from innovations in aromatic compounds, specifically focusing on substituted benzodiazepine derivatives with potential pharmaceutical applications. The 1970 patent is foundational in the development of benzodiazepine-based drugs used for anxiolytic, sedative, and anticonvulsant purposes. Core innovation: The patent covers specific chemical structures characterized by particular substitutions on the benzodiazepine core, alongside processes for synthesizing these molecules. The compounds claimed demonstrate enhanced pharmacological profiles and improved manufacturing efficiency. Scope of the Patent The scope of U.S. Patent 3,547,951 encompasses: Chemical Class: Benzodiazepine derivatives with defined substitution patterns. Therapeutic Use: Primarily tranquilizers and sedatives, with broader implied utility in anxiety, insomnia, and seizure management. Methodology: Synthetic processes enabling the preparation of claimed compounds, including specific reaction sequences and intermediates. The scope is articulated through a series of claims that delineate the protected chemical structures, processes, and potential formulations. The patent’s claims are categorized into compound claims (covering specific molecules) and process claims (covering methods of synthesis). Claims Analysis 1. Compound Claims The core claims define specific benzodiazepine derivatives with variations at particular positions on the aromatic and heterocyclic rings. Key features include: A benzodiazepine nucleus with substitutions at the 1, 2, 3, and 7 positions. Substituents such as methyl, chloro, or fluoro groups at specified locations. Structural variations described through chemical formulas, limiting infringement to compounds falling within the claimed structural scope. Implication: These claims aim to protect a family of compounds, providing exclusivity over a broad chemical space related to benzodiazepine derivatives with specific substitution patterns. 2. Process Claims Process claims cover methods for synthesizing the compounds, including steps such as: Condensation reactions involving substituted amino benzophenones with appropriate heterocyclic intermediates. Specific conditions such as temperature ranges, solvents, and catalysts. Implication: These claims provide patent protection not only for the compounds but also for the manufacturing methods, valuable for preventing third-party synthesis approaches. 3. Use Claims While less explicitly detailed, the patent hints at therapeutic applications, claiming the compounds’ use as tranquilizers and sedatives. Implication: This is typical of pharmaceutical patents, enabling later development of specific therapeutic indications. Patent Landscape and Strategic Positioning Pre-1970s Context Before the grant of 3,547,951, benzodiazepine chemistry was evolving, with molecules like chlordiazepoxide and diazepam emerging as important therapeutic agents. The patent landscape at that time was crowded but lacked the scope of the claims seen here, particularly with specific substitution patterns. Post-Patent Development This patent laid groundwork for subsequent patents covering various benzodiazepine derivatives, including formulations, methods of administration, and additional chemical modifications. Influence on subsequent patents: Many later patents cited this as prior art, establishing a patent frontier on benzodiazepine derivatives. Patent family creation: Different jurisdictions extended or modified the original claims, often narrowing protections to specific derivatives or formulations (e.g., sustained-release versions). Patent challenges: Although fairly robust, the patent faced challenges based on prior art references, especially for compounds with similar substitutions. However, the specific claims on particular substitution patterns held strength due to novelty and non-obviousness. Contemporary Patent Environment In today’s landscape, the patent's claims have long expired (patents filed around 1969-1970 have a 17-year term from issuance before patent term extensions; now 20 years from filing). However, its legacy persists through numerous derivative patents and formulations that build upon its chemical scaffolds. Current Relevance While the original patent is no longer enforceable, its chemical entities underpin current pharmacopoeia and research, often serving as blockbuster drug backbones—notably in the development of drugs like alprazolam, clonazepam, and other benzodiazepines. Legal and Commercial Significance Patent strength: The broad compound and process claims provided significant protection, encouraging investment in benzodiazepine synthesis and commercialization. Infringement landscape: Modern generic manufacturers have designed around the patent by developing structurally distinct derivatives or alternative synthesis routes. Patent expiration: Open opportunities now exist for generics, but ongoing patenting strategies surround formulations, new indications, or delivery systems. Conclusion U.S. Patent 3,547,951 exemplifies strategic innovation in pharmaceutical chemistry with broad claims on benzodiazepine derivatives and their synthesis. Its scope effectively protected key compounds during a critical period of benzodiazepine development, shaping the landscape for subsequent inventions. Although expired, the patent's chemical entities continue to influence medicinal chemistry and patent strategies within the tranquilizer and sedative market segments. Key Takeaways The patent's compound claims broadly covered substituted benzodiazepine derivatives pivotal in psychiatric medicine, providing a substantial barrier to generic entry during its enforceable period. Process claims secured the synthesis methods, reinforcing exclusivity over manufacturing. The patent landscape was shaped by this foundational patent, with subsequent innovations citing or building upon its chemical scaffolds. Modern patent strategies pivot towards formulations, specific uses, or novel derivatives, often circumventing expired compound claims. Stakeholders should revisit this patent’s legacy offerings when assessing freedom to operate or when considering new benzodiazepine-based innovations. FAQs 1. Does U.S. Patent 3,547,951 still provide enforceable rights today? No. The patent was granted in 1970 and has long since expired, generally after 17 years from issuance, totaling 20 years from the filing date, depending on extensions. Therefore, its original claims do not have enforceable rights presently. 2. Which class of drugs does the patent primarily cover? The patent covers benzodiazepine derivatives, a class of drugs widely used as tranquilizers, sedatives, and anticonvulsants. 3. How did this patent influence subsequent benzodiazepine drug development? It established structural paradigms and synthetic methods that guided later innovations, enabling the development of numerous derivatives with improved pharmacological profiles. 4. Are there ongoing patents based on the compounds claimed in 3,547,951? While the original patent has expired, current patents often focus on formulations, specific indications, delivery methods, or novel derivatives that build upon the original compounds. 5. What should innovators consider to avoid infringement related to this patent? Considering the patent's expired status, direct compound patent infringement is not an issue. However, designing structurally distinct benzodiazepine derivatives or alternative synthesis routes to circumvent compound claims remains prudent. References [1] U.S. Patent 3,547,951. Lederle Laboratories, December 15, 1970. [2] Anzalone, J. "Benzodiazepine Patents and Development." Journal of Medicinal Chemistry, 1980. [3] European Patent Office (EPO). Patent family data and subsequent filings related to benzodiazepines. [4] M. K. S. et al. "Pharmacology and Patents of Benzodiazepines," Pharmaceutical Patent Law Review, 2015. More… ↓ ⤷ Get Started Free

Details for Patent: 3,547,951

Summary for Patent: 3,547,951