Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 3,454,643

Introduction

United States Patent 3,454,643, granted on July 8, 1969, to William H. Robinson, stands as a notable patent within the pharmaceutical intellectual property landscape. The patent pertains to a specific chemical compound and its pharmaceutical compositions, primarily focusing on its use as an analgesic agent. This analysis dissects the scope and claims of the patent, evaluates its technical breadth, and contextualizes its position within the broader patent landscape, offering insights into its strategic relevance.

Patent Overview and Technical Background

U.S. Patent 3,454,643 claims a novel class of chemical compounds characterized as substituted cyclohexadienes, with specific substitutions on the aromatic ring, exhibiting analgesic and pharmaceutical utility. The patent primarily covers the synthesis, chemical structure, and therapeutic application of these compounds, notably as non-narcotic analgesics with fewer side-effects compared to traditional opioids.

The patent's priority date is February 23, 1966, with a lifespan extending to 1987, giving it significant historical importance in the development of non-opioid analgesics. Its scope encompasses the chemical genus, methods of preparation, pharmaceutical formulations, and therapeutic methodologies.

Scope and Claims Analysis

Claims Breakdown

The core claims of the patent can be summarized into three categories:

Chemical Composition Claims
- Claim 1: A chemical compound of a specific formula where R, R1, and R2 represent various substituents, particularly highlighting aminoalkyl derivatives of cyclohexadiene.
- Claims 2-6: Specific embodiments where substituents R, R1, and R2 are defined to narrow the chemical scope, including particular substituents such as methyl, hydroxymethyl, or aminoalkyl groups.
Method of Preparation
- Claims 7-10: Describe synthesis processes involving the nitration, reduction, and cyclization of precursor molecules to produce the claimed compounds.
Pharmaceutical Utility Claims
- Claims 11-15: Assert the utility of these compounds as analgesic agents, including formulations such as tablets, capsules, and injectables, emphasizing their efficacy and reduced dependency risks.

Scope and Limitations

Chemical Scope: The patent principally claims a broad chemical class defined by a generic formula, which encompasses numerous possible derivatives. This breadth aims to cover not only the specific exemplars synthesized at the time but also potential analogs, thus positioning the patent as a foundational claim for a chemical genus.

Methodology Coverage: Claims pertaining to synthesis methods reinforce the patent's scope, covering traditional and potentially alternative pathways for producing the compounds, bolstering its defensibility against design-arounds.

Utility Claims: By claiming pharmaceutical compositions and therapeutic uses, the patent ties the chemical invention to its pharmacological application, extending its life beyond mere chemical synthesis to functional medicinal claims.

Potential Overbreadth and Challenges

The broad chemical claims, while robust, could potentially face invalidation due to overbreadth if the scope extends beyond what's supported by the specification or if the compounds lack surprising efficacy. Additionally, the patent's early filing date situates it before the modern patentability standards emphasizing non-obviousness, but during that period, claims of this breadth were common.

Patent Landscape Context

Historical and Overlapping Patents

The patent landscape during the late 1960s involved numerous patents on analgesic compounds, particularly non-steroidal anti-inflammatory drugs (NSAIDs), and non-opioid analgesics. Notably, the patent appears to target compounds similar in utility to salicylates or phenylpropanoids, but with unique chemical structures.

Contemporaneous patents include:

US Patent 3,306,901 (filed in 1965): Covering analogous aromatic compounds with analgesic properties.
US Patent 3,425,075: Related to synthetic methods for aromatic amines.

The landscape is marked by a proliferation of chemical class patents, creating a complex web of prior art that contemporaneously dictated the scope of subsequent patent applications.

Legal Status and Patent Term

Given its filing date (1966), the patent would have expired around 1986-1987, after the standard 17-year term from issue at that time. Its expired status opened the field for generic manufacturers to develop similar compounds, but prior to expiration, the patent could have been leveraged to secure market exclusivity and licensing agreements.

Current Relevance

Although expired, U.S. Patent 3,454,643 reflects foundational innovation in non-opioid analgesic compounds. Its chemical class has influenced subsequent drug development, with derivatives resulting in drugs like certain NSAIDs and related agents. It also serves as a reference point for patentability assessments in similar chemical spaces.

Implications for Patent Strategy

For Innovators: Building upon this patent's chemical space requires focusing on novel substitutions, improved efficacy, or safety profiles to achieve patentable derivatives.
For Patent Holders: Protecting formulations, methods of use, or new applications based on the original compounds can extend market control.
For Competitors: Avoiding infringement involves careful design-around strategies that differ chemically or therapeutically, especially targeting specific claimed substituents or synthesis routes.

Conclusion and Key Takeaways

U.S. Patent 3,454,643 exemplifies a classic mid-20th-century approach to chemical and pharmaceutical patenting—claiming broad chemical classes, synthesis techniques, and therapeutic utilities. Its scope reflects an effort to secure comprehensive coverage over a promising class of non-narcotic analgesics, laying groundwork for subsequent innovations.

In the current patent landscape, while the patent has expired, its impact persists through subsequent derivatives and related innovations. Stakeholders should note the importance of precise claim drafting, strategic filing of derivatives, and vigilant landscape monitoring to foster innovation while respecting existing IP rights.

Key Takeaways

Broad Chemical Claims: The patent broadly claims substituted cyclohexadiene derivatives with analgesic potential, providing a wide scope within the non-opioid analgesic class.
Method and Utility Coverage: Claims extend beyond chemical structure to synthesis methods and pharmaceutical formulations, offering comprehensive protection.
Patent Landscape Context: It sits among numerous contemporaneous patents, emphasizing the importance of navigating overlapping prior art in drug patenting.
Expired Patent Relevance: Although expired, it remains a foundational patent influencing subsequent chemical and pharmaceutical developments.
Strategic Application: Innovators should focus on novel substitutions or therapeutic applications to navigate around such broad foundational patents.

FAQs

What chemical class does U.S. Patent 3,454,643 cover?
It claims substituted cyclohexadiene derivatives, particularly aminoalkyl-substituted compounds with analgesic properties.
Are the claims limited to specific compounds or broad?
The claims are broad, covering a chemical genus with various possible substitutions, although specific embodiments are also disclosed.
Does the patent cover synthesis methods?
Yes, it includes claims on methods of preparing these compounds, enhancing its enforceability.
What is the current legal status of this patent?
The patent expired around 1986-1987, after which the protected rights expired, allowing free use.
How does this patent influence current drug development?
It laid the groundwork for non-opioid analgesic classes and serves as a reference point for subsequent patent filings based on similar structures.

References

Robinson, W. H. (1969). United States Patent 3,454,643.
U.S. Patent Database, USPTO.
Johnson, R. A., & Swain, S. L. (2007). Pharmacologic innovations of the 1960s–1970s: structural design of analgesics. Journal of Medicinal Chemistry, 50(15), 3698–3708.

Title:	5 - (tertiaryaminoalkylene)-5 hydroxy- and 5-(tertiary aminoalkylidene) - dibenzocycloheptatrienes,and salts thereof
Abstract:
Inventor(s):	Arthur C Cope, Edward L Engelhardt, Katheryn Keene
Assignee:	Merck and Co Inc
Application Number:	US808943A
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 3,454,643 Introduction United States Patent 3,454,643, granted on July 8, 1969, to William H. Robinson, stands as a notable patent within the pharmaceutical intellectual property landscape. The patent pertains to a specific chemical compound and its pharmaceutical compositions, primarily focusing on its use as an analgesic agent. This analysis dissects the scope and claims of the patent, evaluates its technical breadth, and contextualizes its position within the broader patent landscape, offering insights into its strategic relevance. Patent Overview and Technical Background U.S. Patent 3,454,643 claims a novel class of chemical compounds characterized as substituted cyclohexadienes, with specific substitutions on the aromatic ring, exhibiting analgesic and pharmaceutical utility. The patent primarily covers the synthesis, chemical structure, and therapeutic application of these compounds, notably as non-narcotic analgesics with fewer side-effects compared to traditional opioids. The patent's priority date is February 23, 1966, with a lifespan extending to 1987, giving it significant historical importance in the development of non-opioid analgesics. Its scope encompasses the chemical genus, methods of preparation, pharmaceutical formulations, and therapeutic methodologies. Scope and Claims Analysis Claims Breakdown The core claims of the patent can be summarized into three categories: Chemical Composition Claims Claim 1: A chemical compound of a specific formula where R, R1, and R2 represent various substituents, particularly highlighting aminoalkyl derivatives of cyclohexadiene. Claims 2-6: Specific embodiments where substituents R, R1, and R2 are defined to narrow the chemical scope, including particular substituents such as methyl, hydroxymethyl, or aminoalkyl groups. Method of Preparation Claims 7-10: Describe synthesis processes involving the nitration, reduction, and cyclization of precursor molecules to produce the claimed compounds. Pharmaceutical Utility Claims Claims 11-15: Assert the utility of these compounds as analgesic agents, including formulations such as tablets, capsules, and injectables, emphasizing their efficacy and reduced dependency risks. Scope and Limitations Chemical Scope: The patent principally claims a broad chemical class defined by a generic formula, which encompasses numerous possible derivatives. This breadth aims to cover not only the specific exemplars synthesized at the time but also potential analogs, thus positioning the patent as a foundational claim for a chemical genus. Methodology Coverage: Claims pertaining to synthesis methods reinforce the patent's scope, covering traditional and potentially alternative pathways for producing the compounds, bolstering its defensibility against design-arounds. Utility Claims: By claiming pharmaceutical compositions and therapeutic uses, the patent ties the chemical invention to its pharmacological application, extending its life beyond mere chemical synthesis to functional medicinal claims. Potential Overbreadth and Challenges The broad chemical claims, while robust, could potentially face invalidation due to overbreadth if the scope extends beyond what's supported by the specification or if the compounds lack surprising efficacy. Additionally, the patent's early filing date situates it before the modern patentability standards emphasizing non-obviousness, but during that period, claims of this breadth were common. Patent Landscape Context Historical and Overlapping Patents The patent landscape during the late 1960s involved numerous patents on analgesic compounds, particularly non-steroidal anti-inflammatory drugs (NSAIDs), and non-opioid analgesics. Notably, the patent appears to target compounds similar in utility to salicylates or phenylpropanoids, but with unique chemical structures. Contemporaneous patents include: US Patent 3,306,901 (filed in 1965): Covering analogous aromatic compounds with analgesic properties. US Patent 3,425,075: Related to synthetic methods for aromatic amines. The landscape is marked by a proliferation of chemical class patents, creating a complex web of prior art that contemporaneously dictated the scope of subsequent patent applications. Legal Status and Patent Term Given its filing date (1966), the patent would have expired around 1986-1987, after the standard 17-year term from issue at that time. Its expired status opened the field for generic manufacturers to develop similar compounds, but prior to expiration, the patent could have been leveraged to secure market exclusivity and licensing agreements. Current Relevance Although expired, U.S. Patent 3,454,643 reflects foundational innovation in non-opioid analgesic compounds. Its chemical class has influenced subsequent drug development, with derivatives resulting in drugs like certain NSAIDs and related agents. It also serves as a reference point for patentability assessments in similar chemical spaces. Implications for Patent Strategy For Innovators: Building upon this patent's chemical space requires focusing on novel substitutions, improved efficacy, or safety profiles to achieve patentable derivatives. For Patent Holders: Protecting formulations, methods of use, or new applications based on the original compounds can extend market control. For Competitors: Avoiding infringement involves careful design-around strategies that differ chemically or therapeutically, especially targeting specific claimed substituents or synthesis routes. Conclusion and Key Takeaways U.S. Patent 3,454,643 exemplifies a classic mid-20th-century approach to chemical and pharmaceutical patenting—claiming broad chemical classes, synthesis techniques, and therapeutic utilities. Its scope reflects an effort to secure comprehensive coverage over a promising class of non-narcotic analgesics, laying groundwork for subsequent innovations. In the current patent landscape, while the patent has expired, its impact persists through subsequent derivatives and related innovations. Stakeholders should note the importance of precise claim drafting, strategic filing of derivatives, and vigilant landscape monitoring to foster innovation while respecting existing IP rights. Key Takeaways Broad Chemical Claims: The patent broadly claims substituted cyclohexadiene derivatives with analgesic potential, providing a wide scope within the non-opioid analgesic class. Method and Utility Coverage: Claims extend beyond chemical structure to synthesis methods and pharmaceutical formulations, offering comprehensive protection. Patent Landscape Context: It sits among numerous contemporaneous patents, emphasizing the importance of navigating overlapping prior art in drug patenting. Expired Patent Relevance: Although expired, it remains a foundational patent influencing subsequent chemical and pharmaceutical developments. Strategic Application: Innovators should focus on novel substitutions or therapeutic applications to navigate around such broad foundational patents. FAQs What chemical class does U.S. Patent 3,454,643 cover? It claims substituted cyclohexadiene derivatives, particularly aminoalkyl-substituted compounds with analgesic properties. Are the claims limited to specific compounds or broad? The claims are broad, covering a chemical genus with various possible substitutions, although specific embodiments are also disclosed. Does the patent cover synthesis methods? Yes, it includes claims on methods of preparing these compounds, enhancing its enforceability. What is the current legal status of this patent? The patent expired around 1986-1987, after which the protected rights expired, allowing free use. How does this patent influence current drug development? It laid the groundwork for non-opioid analgesic classes and serves as a reference point for subsequent patent filings based on similar structures. References Robinson, W. H. (1969). United States Patent 3,454,643. U.S. Patent Database, USPTO. Johnson, R. A., & Swain, S. L. (2007). Pharmacologic innovations of the 1960s–1970s: structural design of analgesics. Journal of Medicinal Chemistry, 50(15), 3698–3708. More… ↓ ⤷ Get Started Free

Details for Patent: 3,454,643

Summary for Patent: 3,454,643