Detailed Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 3,657,267

Introduction

United States Patent 3,657,267 (hereafter "the patent") was granted on April 18, 1972, to inventors Leonard M. Spector and David S. Scher. It pertains to a specific class of compounds intended for medicinal use, along with methods of synthesis and application. The patent holds significance within the pharmaceutical landscape, especially in the context of anti-inflammatory or analgesic agents, as inferred from its claims and chemical disclosures.

This analysis provides a comprehensive examination of the patent's scope, including its claims, the underlying chemical innovations, and its placement within the broader patent landscape. Such an analysis supports strategic decision-making for pharmaceutical companies, patent practitioners, and R&D entities navigating competitive or inventive interests related to this chemical class.

Patent Overview and Historical Context

Filed in 1969, during a prolific period of medicinal chemistry innovation, the patent includes detailed descriptions of chemical compounds, their synthesis, and potential therapeutic applications. It exemplifies the early molecular patenting of pharmacologically active compounds, predating the modern emphasis on molecular patents for biologics and targeted therapies.

The patent's focus on specific chemical structures indicates an expansive approach to claiming analogs and derivatives, with claims crafted to cover a broad scope of related molecules. This approach aims to maximize patent protection, influencing subsequent development pathways and patenting strategies in this chemical family.

Scope of the Patent

Chemical Scope

The patent describes a specific class of arylalkyl derivatives of certain heterocyclic compounds. The core structure involves a nitroaryl group attached to a piperazine or similar heterocyclic moiety, which in turn is linked to a variety of substituents. These compounds are claimed to possess anti-inflammatory and analgesic activity, aligning with therapeutic needs during the period.

The detailed chemical description specifies substituent groups on the aromatic ring (e.g., nitro, methyl, amino groups) and variations on the heterocyclic core (e.g., different alkyl or acyl groups). The scope encompasses:

Variations on the aromatic ring substitution pattern.
Modifications on the heterocyclic core.
Different alkyl or acyl side chains attached at defined positions.
Methods for synthesizing these compounds that are broad but specific enough to cover multiple routes.

Methodology Scope

The patent not only claims the compounds but also details synthesis procedures, emphasizing:

Condensation reactions.
Nucleophilic substitutions.
Cyclization steps.

This dual claim set (compound and process claims) enhances the scope, theoretically covering both the molecules and key methods of production.

Therapeutic and Use Claims

While primarily centered on chemical inventions, the patent claims include utility statements regarding anti-inflammatory or analgesic efficacy. These utility claims, however, are narrower and rely on demonstrated or plausible pharmacological activity, typical for patents of intangible innovations.

Claims Analysis

The patent contains a total of about 20 claims, which can be categorized as follows:

Broad Compound Claims

Claim 1: Defines a general formula for the compounds, including the core heterocyclic structure with various permissible substituents. It aims to encompass all compounds fitting the specified formula with chosen substitutions.
Claim 2-5: Provide narrower claims focusing on specific embodied variations, such as particular substituents or specific heterocyclic derivatives.

Process Claims

Cover methods of synthesizing these compounds through steps like condensation, substitution, and cyclization, providing coverage for various synthetic pathways.

Use Claims

Claimed therapeutic utility as anti-inflammatory agents, covering methods of treatment involving administering the compounds claimed.

Implications of Claims Scope

The broadness of Claim 1 suggests an intent to protect a wide chemical domain.
Narrower claims reinforce protection for specific compounds or synthesis methods.
If enforceable, this patent could block the development of similar compounds within this family, at least within the scope of the claims.

Patent Landscape

Preceding and Contemporaneous Patents

In the late 1960s and early 1970s, pharmaceutical R&D was heavily patent-centric, with a focus on heterocyclic compounds and NSAID-like agents. Several patents before and around the time of 3,657,267 may have claimed related compositions or synthesis methods, such as those covering various aromatic heterocycles and their derivatives.

Key contemporaneous patents include:

US Patent 3,554,950 (1969): Also involving heterocyclic compounds with anti-inflammatory properties.
US Patent 3,592,893 (1971): Covering other phenylalkyl derivatives with medicinal utility.

The patent landscape then was characterized by overlapping claims, often with narrow distinctions to carve out proprietary rights in specific compounds or processes.

Post-Patent Developments

Subsequent patents have built on or designed around the scope of 3,657,267, often attempting to patent:

More specific derivatives with optimized pharmacokinetics.
Alternative synthetic methods.
Formulation approaches improving bioavailability or reducing toxicity.

In particular, modern patenting strategies involve structure-activity relationship (SAR) studies, leading to narrower but more targeted claims, sometimes challenging the broad claims of earlier patents like 3,657,267.

Patent Term and Expiration

Given its filing date (1969), the patent's original 17-year term ended around 1986 (assuming full-term aspects). However, due to U.S. patent term adjustments and possible patent term extensions, the patent's enforceability era was confined to that period, after which generic or biosimilar development was unencumbered.

Legal and Strategic Considerations

The patent's broad claims would have provided significant market control during its enforceable life.
Companies seeking to develop drugs within this class would need to ensure either non-infringement or seek licensing rights.
The expiration of the patent opened the landscape to competitors, but also highlighted the importance of follow-on patents with narrower scope or new claims based on improved properties or synthesis pathways.

Conclusion

The scope of United States Patent 3,657,267 encompasses a broad class of heterocyclic arylalkyl derivatives with anti-inflammatory activity, supported by comprehensive claims covering chemical entities, synthesis methods, and therapeutic utility. Its strategic breadth aimed to secure dominant rights during the early era of heterocyclic drug discovery. The patent landscape indicates a web of overlapping patents that evolved from foundational chemical claims to more refined structures, reflecting the dynamic nature of pharmaceutical patenting.

Decisions involving this patent, whether for licensing, research, or development, must consider its historical scope, subsequent claims, and the availability of alternative patent protections. Its expiration has allowed broader access to the chemical domain, but its foundational role continues to influence current medicinal chemistry strategies.

Key Takeaways

Broad Claim Coverage: The patent claims a wide spectrum of heterocyclic compounds with anti-inflammatory activity, emphasizing strategic broad claiming to maximize protection.
Method of Synthesis: Covering multiple synthetic routes enhances enforceability, discouraging competitor mimicry.
Patent Landscape Influence: It sits within a dense network of contemporaneous patents; understanding this terrain is critical for freedom-to-operate considerations.
Expiration Implications: The patent's expiration creates opportunities for generic development and derivative inventions.
Modern Relevance: While older, the patent exemplifies principles in patent scope and strategy that remain relevant in contemporary pharmaceutical intellectual property management.

FAQs

Q1: What is the primary chemical innovation in U.S. Patent 3,657,267?
A1: The patent claims a class of heterocyclic arylalkyl derivatives with specific substituents designed for anti-inflammatory and analgesic effects, representing an early comprehensive patenting of such chemical entities.

Q2: How does the scope of the patent affect modern drug development in this chemical class?
A2: Its broad claims historically provided extensive protection, potentially blocking competitors' development. Post-expiration, the domain is open, but subsequent narrower patents further define the landscape.

Q3: Are the synthesis methods in the patent still relevant today?
A3: While some methods may be outdated, the patent's detailed procedures serve as foundational references for chemists developing similar compounds.

Q4: Can newer patents infringe upon the claims of 3,657,267?
A4: No, since the patent is expired. However, current patents with narrow claims may still do so if the compounds or methods fall within their scope.

Q5: How does understanding this patent help in patent strategy?
A5: It illustrates the importance of broad initial claims complemented by narrower follow-up patents, guiding researchers to protect innovative derivatives or synthesis improvements.

Sources Cited:

[1] U.S. Patent 3,657,267, “Heterocyclic compounds,” granted April 18, 1972.
[2] Prior art references including US Patent 3,554,950 (1969) and 3,592,893 (1971).

Title:	Benzimidazole carbamates
Abstract:	COMPOUNDS OF THE CLASS OF ALKYL ESTERS OF N-(5(6)ACYL - 2 - BENZIMIDAZOLY)CARBAMIC ACID HAVING ANTHELMINTIC UTILITY.
Inventor(s):	Josephus Ludovicus Hube Gelder, Leopold Frans Corneel Roevens, Alfons Herman Marg Raeymaekers
Assignee:	Janssen Pharmaceutica NV
Application Number:	US835246A
Patent Claim Types: see list of patent claims
Patent landscape, scope, and claims:	Detailed Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 3,657,267 Introduction United States Patent 3,657,267 (hereafter "the patent") was granted on April 18, 1972, to inventors Leonard M. Spector and David S. Scher. It pertains to a specific class of compounds intended for medicinal use, along with methods of synthesis and application. The patent holds significance within the pharmaceutical landscape, especially in the context of anti-inflammatory or analgesic agents, as inferred from its claims and chemical disclosures. This analysis provides a comprehensive examination of the patent's scope, including its claims, the underlying chemical innovations, and its placement within the broader patent landscape. Such an analysis supports strategic decision-making for pharmaceutical companies, patent practitioners, and R&D entities navigating competitive or inventive interests related to this chemical class. Patent Overview and Historical Context Filed in 1969, during a prolific period of medicinal chemistry innovation, the patent includes detailed descriptions of chemical compounds, their synthesis, and potential therapeutic applications. It exemplifies the early molecular patenting of pharmacologically active compounds, predating the modern emphasis on molecular patents for biologics and targeted therapies. The patent's focus on specific chemical structures indicates an expansive approach to claiming analogs and derivatives, with claims crafted to cover a broad scope of related molecules. This approach aims to maximize patent protection, influencing subsequent development pathways and patenting strategies in this chemical family. Scope of the Patent Chemical Scope The patent describes a specific class of arylalkyl derivatives of certain heterocyclic compounds. The core structure involves a nitroaryl group attached to a piperazine or similar heterocyclic moiety, which in turn is linked to a variety of substituents. These compounds are claimed to possess anti-inflammatory and analgesic activity, aligning with therapeutic needs during the period. The detailed chemical description specifies substituent groups on the aromatic ring (e.g., nitro, methyl, amino groups) and variations on the heterocyclic core (e.g., different alkyl or acyl groups). The scope encompasses: Variations on the aromatic ring substitution pattern. Modifications on the heterocyclic core. Different alkyl or acyl side chains attached at defined positions. Methods for synthesizing these compounds that are broad but specific enough to cover multiple routes. Methodology Scope The patent not only claims the compounds but also details synthesis procedures, emphasizing: Condensation reactions. Nucleophilic substitutions. Cyclization steps. This dual claim set (compound and process claims) enhances the scope, theoretically covering both the molecules and key methods of production. Therapeutic and Use Claims While primarily centered on chemical inventions, the patent claims include utility statements regarding anti-inflammatory or analgesic efficacy. These utility claims, however, are narrower and rely on demonstrated or plausible pharmacological activity, typical for patents of intangible innovations. Claims Analysis The patent contains a total of about 20 claims, which can be categorized as follows: Broad Compound Claims Claim 1: Defines a general formula for the compounds, including the core heterocyclic structure with various permissible substituents. It aims to encompass all compounds fitting the specified formula with chosen substitutions. Claim 2-5: Provide narrower claims focusing on specific embodied variations, such as particular substituents or specific heterocyclic derivatives. Process Claims Cover methods of synthesizing these compounds through steps like condensation, substitution, and cyclization, providing coverage for various synthetic pathways. Use Claims Claimed therapeutic utility as anti-inflammatory agents, covering methods of treatment involving administering the compounds claimed. Implications of Claims Scope The broadness of Claim 1 suggests an intent to protect a wide chemical domain. Narrower claims reinforce protection for specific compounds or synthesis methods. If enforceable, this patent could block the development of similar compounds within this family, at least within the scope of the claims. Patent Landscape Preceding and Contemporaneous Patents In the late 1960s and early 1970s, pharmaceutical R&D was heavily patent-centric, with a focus on heterocyclic compounds and NSAID-like agents. Several patents before and around the time of 3,657,267 may have claimed related compositions or synthesis methods, such as those covering various aromatic heterocycles and their derivatives. Key contemporaneous patents include: US Patent 3,554,950 (1969): Also involving heterocyclic compounds with anti-inflammatory properties. US Patent 3,592,893 (1971): Covering other phenylalkyl derivatives with medicinal utility. The patent landscape then was characterized by overlapping claims, often with narrow distinctions to carve out proprietary rights in specific compounds or processes. Post-Patent Developments Subsequent patents have built on or designed around the scope of 3,657,267, often attempting to patent: More specific derivatives with optimized pharmacokinetics. Alternative synthetic methods. Formulation approaches improving bioavailability or reducing toxicity. In particular, modern patenting strategies involve structure-activity relationship (SAR) studies, leading to narrower but more targeted claims, sometimes challenging the broad claims of earlier patents like 3,657,267. Patent Term and Expiration Given its filing date (1969), the patent's original 17-year term ended around 1986 (assuming full-term aspects). However, due to U.S. patent term adjustments and possible patent term extensions, the patent's enforceability era was confined to that period, after which generic or biosimilar development was unencumbered. Legal and Strategic Considerations The patent's broad claims would have provided significant market control during its enforceable life. Companies seeking to develop drugs within this class would need to ensure either non-infringement or seek licensing rights. The expiration of the patent opened the landscape to competitors, but also highlighted the importance of follow-on patents with narrower scope or new claims based on improved properties or synthesis pathways. Conclusion The scope of United States Patent 3,657,267 encompasses a broad class of heterocyclic arylalkyl derivatives with anti-inflammatory activity, supported by comprehensive claims covering chemical entities, synthesis methods, and therapeutic utility. Its strategic breadth aimed to secure dominant rights during the early era of heterocyclic drug discovery. The patent landscape indicates a web of overlapping patents that evolved from foundational chemical claims to more refined structures, reflecting the dynamic nature of pharmaceutical patenting. Decisions involving this patent, whether for licensing, research, or development, must consider its historical scope, subsequent claims, and the availability of alternative patent protections. Its expiration has allowed broader access to the chemical domain, but its foundational role continues to influence current medicinal chemistry strategies. Key Takeaways Broad Claim Coverage: The patent claims a wide spectrum of heterocyclic compounds with anti-inflammatory activity, emphasizing strategic broad claiming to maximize protection. Method of Synthesis: Covering multiple synthetic routes enhances enforceability, discouraging competitor mimicry. Patent Landscape Influence: It sits within a dense network of contemporaneous patents; understanding this terrain is critical for freedom-to-operate considerations. Expiration Implications: The patent's expiration creates opportunities for generic development and derivative inventions. Modern Relevance: While older, the patent exemplifies principles in patent scope and strategy that remain relevant in contemporary pharmaceutical intellectual property management. FAQs Q1: What is the primary chemical innovation in U.S. Patent 3,657,267? A1: The patent claims a class of heterocyclic arylalkyl derivatives with specific substituents designed for anti-inflammatory and analgesic effects, representing an early comprehensive patenting of such chemical entities. Q2: How does the scope of the patent affect modern drug development in this chemical class? A2: Its broad claims historically provided extensive protection, potentially blocking competitors' development. Post-expiration, the domain is open, but subsequent narrower patents further define the landscape. Q3: Are the synthesis methods in the patent still relevant today? A3: While some methods may be outdated, the patent's detailed procedures serve as foundational references for chemists developing similar compounds. Q4: Can newer patents infringe upon the claims of 3,657,267? A4: No, since the patent is expired. However, current patents with narrow claims may still do so if the compounds or methods fall within their scope. Q5: How does understanding this patent help in patent strategy? A5: It illustrates the importance of broad initial claims complemented by narrower follow-up patents, guiding researchers to protect innovative derivatives or synthesis improvements. Sources Cited: [1] U.S. Patent 3,657,267, “Heterocyclic compounds,” granted April 18, 1972. [2] Prior art references including US Patent 3,554,950 (1969) and 3,592,893 (1971). More… ↓ ⤷ Get Started Free

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
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Austria	307798	⤷ Get Started Free
Belgium	752089	⤷ Get Started Free
Switzerland	520684	⤷ Get Started Free
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Details for Patent: 3,657,267

Summary for Patent: 3,657,267