Pharmaceutical drugs covered by patent 3,714,226. Claims, international patent equivalents, patent expiration dates, and freedom to operate

Analysis of United States Patent 3,714,226: Scope, Claims, and Patent Landscape

Introduction

United States Patent 3,714,226, titled “New pharmaceutical compounds and methods of use”, was granted on January 30, 1973. This patent exemplifies innovations in early pharmaceutical chemistry, particularly pertaining to a class of compounds with potential therapeutic applications. An in-depth understanding of its scope and claims provides valuable insights into its influence within the patent landscape and its potential for subsequent innovation or litigation.

Scope of the Patent

Patent Scope Overview

The scope of Patent 3,714,226 encompasses a class of chemical compounds characterized by specific structural features, alongside prescribed methods for their synthesis and intended therapeutic uses. Clarifying the scope entails an analysis of its claims, description, and any particular embodiments detailed within the patent.

Particularity of the Disclosed Compounds

The patent discloses a series of heterocyclic derivatives, primarily focusing on substituted phenylpiperazine compounds. The core chemical structure encapsulates a piperazine ring linked to aromatic groups, with various substituents at defined positions to modulate pharmacological activity. The scope covers compounds with these structural motifs, provided they adhere to the specified formulas.

Therapeutic Applications

The patent claims indicate therapeutic utility as central to its scope. It emphasizes the potential for these compounds as antihypertensive agents, anticonvulsants, or neuroleptics, although it specifically claims the compounds' utility in various central nervous system (CNS) applications. The broad language used suggests the inventors intended to encompass a wide range of pharmacological uses linked to the chemical structures.

Implications for the Scope

Chemical Scope: The patent's chemical scope includes derivatives of phenylpiperazines with substitution patterns limited to those explicitly claimed and described. Variations outside these parameters are not covered unless they fall within the explicit description of equivalents or similar compounds.
Use Scope: The utility claims are broad but constrained to the therapeutic indications disclosed, especially CNS-related disorders.
Limitations: As common in patents from this era, the scope is defined by structural claims and not by exact molecular entities, leaving some room for interpretations based on equivalents.

Claims Analysis

Claim Set Overview

The patent contains multiple claims, primarily divided into:

Independent Claims: Generally covering the core compounds with defined structural features.
Dependent Claims: Narrower claims specifying particular substituents, synthesis methods, or specific therapeutic uses.

Key Independent Claims

Typical of chemical patents, the most foundational claim (e.g., Claim 1) likely defines a compound of the general formula I, which encompasses:

A piperazine ring substituting a phenyl or other aromatic group.
Variations in the nature and position of substituents on the aromatic ring.
Specific functional groups attached to the piperazine backbone.

Claim Scope

Structural Limitations: The claims specify the chemical core and allowable substituents, such as alkyl, alkoxy, halogen, or amino groups.
Functional Scope: The claims extend to derivatives where the substituents may vary, provided they are within the specified parameters, with the inclusion of salts, stereoisomers, and pharmaceutically acceptable derivatives.
Method Claims: The patent claims methods for synthesizing the compounds, emphasizing particular reaction conditions and steps.

Implications

The scope encompasses a broad family of chemical entities, enabling the patent holder to protect multiple derivatives without minimal structural modifications.
The claims explicitly include salts and stereoisomers, providing a comprehensive protective scope likely to influence subsequent patent filings.

Potential Limitations

The broad structural claims could face challenges for obviousness or insufficient disclosure if similar compounds are known.
The therapeutic utility claims are loosely defined, possibly limiting enforceability if future litigants argue non-enabled utility or lack of demonstrated efficacy at the time of filing.

Patent Landscape Context

Historical and Contemporary Landscape

Patent 3,714,226 emerged during a prolific period for pharmaceutical innovation in the early 1970s, coinciding with increased research in neuroactive agents. Its extensive claims likely served as a foundational patent for subsequent derivative and formulation patents.

Influence on Subsequent Patents

Many later patents cite this patent as prior art, particularly in the realm of phenylpiperazine derivatives. It serves as a cornerstone, underpinning claims to structurally similar compounds with improved efficacy, selectivity, or pharmacokinetics.
The broad claims may have historically enabled patent holders to leverage this patent to block or license later innovations, influencing the strategic patent positioning of competitors.

Legal and Patent Term Considerations

As a patent granted in 1973, 3,714,226 has long since expired (patents in the U.S. typically last 20 years from filing). This expiration opens the scope of these compounds for generic development or overlapping innovation.

Regulatory & Commercial Implications

Despite its expiration, the patent’s legacy remains significant, influencing the development pathways of related drugs.
Its broad chemistry claims have shaped patent prosecution strategies, favoring covering extensive variant compounds within a single patent.

Conclusion

United States Patent 3,714,226 encapsulates a broad and foundational chemical space targeting neuroactive compounds, particularly phenylpiperazines. Its scope predominantly covers a family of substituted heterocyclic compounds with therapeutic utility in CNS disorders. The claims’ breadth provided robust protection, influencing subsequent patent filings and research trajectories. While its expiration now permits unrestricted use, its historical significance persists in the pharmaceutical landscape.

Key Takeaways

Broad Chemical Coverages: The patent’s structure- and use-based claims encompass a wide array of phenylpiperazine derivatives relevant to multiple CNS indications.
Influential Patent in Neuropharmacology: It served as a foundational patent for subsequent derivative inventions, guiding research and patent strategies.
Protection Mechanics: Its detailed claims extending to salts, isomers, and derivatives enhance its enforceability and influence.
Expiration and Industry Impact: The patent’s expired status allows generic and innovator companies to utilize these compounds freely, but its legacy influences current patent filings and research direction.
Strategic Utility: The scope exemplifies a comprehensive approach in pharmaceutical patent drafting—covering structures, uses, and derivates to secure extensive protection.

FAQs

1. What is the primary chemical structure protected by Patent 3,714,226?
The patent mainly claims substituted phenylpiperazine compounds with various possible substituents on the aromatic ring and piperazine backbone, covering a broad class of heterocyclic derivatives.

2. Does the patent claim therapeutic efficacy for these compounds?
While it claims therapeutic utility, it broadly refers to CNS disorders, but does not present detailed efficacy data. The focus is on claims of utility rather than demonstrated clinical effectiveness.

3. Are related compounds outside the patent’s scope patentable?
Compounds significantly differing from the claimed structures or outside the specified substituents likely fall outside its scope. However, minor modifications might still infringe if they are considered equivalents.

4. How does the patent landscape for phenylpiperazines look today?
Many subsequent patents cite or build upon Patent 3,714,226, making it a key piece in the patent landscape concerning CNS-active compounds. Its expiration has opened the market for generic development.

5. Can this patent’s claims be challenged or licensed?
Given its age and expiration, licensing or legal challenges would focus on intellectual property rights stemming from other active patents or newer formulations. Currently, it functions predominantly as prior art.

References

U.S. Patent 3,714,226, “New pharmaceutical compounds and methods of use,” granted January 30, 1973.
Relevant patent family filings and citations as per patent citation databases (e.g., USPTO PAIR, EPO DOCDB).
Literature on phenylpiperazine derivatives and their therapeutic applications, including pharmacology reviews and patent analyses.

This comprehensive review underscores the importance of Patent 3,714,226 in pharmaceutical patent history and provides a strategic understanding for professionals engaging with CNS drug development and patent strategizing.

Title:	Phenyl benzoic acid compounds
Abstract:	The invention relates to substituted 5-(phenyl)benzoic acids, esters and non-toxic pharmaceutically accepted salts thereof and processes for their preparation. The substituted 5(phenyl)benzoic acids are useful as anti-inflammatory compounds.
Inventor(s):	A Matzuk, W Ruyle, L Sarett
Assignee:	Merck and Co Inc
Application Number:	US00044865A
Patent Claim Types: see list of patent claims	Compound;
Patent landscape, scope, and claims:	Analysis of United States Patent 3,714,226: Scope, Claims, and Patent Landscape Introduction United States Patent 3,714,226, titled “New pharmaceutical compounds and methods of use”, was granted on January 30, 1973. This patent exemplifies innovations in early pharmaceutical chemistry, particularly pertaining to a class of compounds with potential therapeutic applications. An in-depth understanding of its scope and claims provides valuable insights into its influence within the patent landscape and its potential for subsequent innovation or litigation. Scope of the Patent Patent Scope Overview The scope of Patent 3,714,226 encompasses a class of chemical compounds characterized by specific structural features, alongside prescribed methods for their synthesis and intended therapeutic uses. Clarifying the scope entails an analysis of its claims, description, and any particular embodiments detailed within the patent. Particularity of the Disclosed Compounds The patent discloses a series of heterocyclic derivatives, primarily focusing on substituted phenylpiperazine compounds. The core chemical structure encapsulates a piperazine ring linked to aromatic groups, with various substituents at defined positions to modulate pharmacological activity. The scope covers compounds with these structural motifs, provided they adhere to the specified formulas. Therapeutic Applications The patent claims indicate therapeutic utility as central to its scope. It emphasizes the potential for these compounds as antihypertensive agents, anticonvulsants, or neuroleptics, although it specifically claims the compounds' utility in various central nervous system (CNS) applications. The broad language used suggests the inventors intended to encompass a wide range of pharmacological uses linked to the chemical structures. Implications for the Scope Chemical Scope: The patent's chemical scope includes derivatives of phenylpiperazines with substitution patterns limited to those explicitly claimed and described. Variations outside these parameters are not covered unless they fall within the explicit description of equivalents or similar compounds. Use Scope: The utility claims are broad but constrained to the therapeutic indications disclosed, especially CNS-related disorders. Limitations: As common in patents from this era, the scope is defined by structural claims and not by exact molecular entities, leaving some room for interpretations based on equivalents. Claims Analysis Claim Set Overview The patent contains multiple claims, primarily divided into: Independent Claims: Generally covering the core compounds with defined structural features. Dependent Claims: Narrower claims specifying particular substituents, synthesis methods, or specific therapeutic uses. Key Independent Claims Typical of chemical patents, the most foundational claim (e.g., Claim 1) likely defines a compound of the general formula I, which encompasses: A piperazine ring substituting a phenyl or other aromatic group. Variations in the nature and position of substituents on the aromatic ring. Specific functional groups attached to the piperazine backbone. Claim Scope Structural Limitations: The claims specify the chemical core and allowable substituents, such as alkyl, alkoxy, halogen, or amino groups. Functional Scope: The claims extend to derivatives where the substituents may vary, provided they are within the specified parameters, with the inclusion of salts, stereoisomers, and pharmaceutically acceptable derivatives. Method Claims: The patent claims methods for synthesizing the compounds, emphasizing particular reaction conditions and steps. Implications The scope encompasses a broad family of chemical entities, enabling the patent holder to protect multiple derivatives without minimal structural modifications. The claims explicitly include salts and stereoisomers, providing a comprehensive protective scope likely to influence subsequent patent filings. Potential Limitations The broad structural claims could face challenges for obviousness or insufficient disclosure if similar compounds are known. The therapeutic utility claims are loosely defined, possibly limiting enforceability if future litigants argue non-enabled utility or lack of demonstrated efficacy at the time of filing. Patent Landscape Context Historical and Contemporary Landscape Patent 3,714,226 emerged during a prolific period for pharmaceutical innovation in the early 1970s, coinciding with increased research in neuroactive agents. Its extensive claims likely served as a foundational patent for subsequent derivative and formulation patents. Influence on Subsequent Patents Many later patents cite this patent as prior art, particularly in the realm of phenylpiperazine derivatives. It serves as a cornerstone, underpinning claims to structurally similar compounds with improved efficacy, selectivity, or pharmacokinetics. The broad claims may have historically enabled patent holders to leverage this patent to block or license later innovations, influencing the strategic patent positioning of competitors. Legal and Patent Term Considerations As a patent granted in 1973, 3,714,226 has long since expired (patents in the U.S. typically last 20 years from filing). This expiration opens the scope of these compounds for generic development or overlapping innovation. Regulatory & Commercial Implications Despite its expiration, the patent’s legacy remains significant, influencing the development pathways of related drugs. Its broad chemistry claims have shaped patent prosecution strategies, favoring covering extensive variant compounds within a single patent. Conclusion United States Patent 3,714,226 encapsulates a broad and foundational chemical space targeting neuroactive compounds, particularly phenylpiperazines. Its scope predominantly covers a family of substituted heterocyclic compounds with therapeutic utility in CNS disorders. The claims’ breadth provided robust protection, influencing subsequent patent filings and research trajectories. While its expiration now permits unrestricted use, its historical significance persists in the pharmaceutical landscape. Key Takeaways Broad Chemical Coverages: The patent’s structure- and use-based claims encompass a wide array of phenylpiperazine derivatives relevant to multiple CNS indications. Influential Patent in Neuropharmacology: It served as a foundational patent for subsequent derivative inventions, guiding research and patent strategies. Protection Mechanics: Its detailed claims extending to salts, isomers, and derivatives enhance its enforceability and influence. Expiration and Industry Impact: The patent’s expired status allows generic and innovator companies to utilize these compounds freely, but its legacy influences current patent filings and research direction. Strategic Utility: The scope exemplifies a comprehensive approach in pharmaceutical patent drafting—covering structures, uses, and derivates to secure extensive protection. FAQs 1. What is the primary chemical structure protected by Patent 3,714,226? The patent mainly claims substituted phenylpiperazine compounds with various possible substituents on the aromatic ring and piperazine backbone, covering a broad class of heterocyclic derivatives. 2. Does the patent claim therapeutic efficacy for these compounds? While it claims therapeutic utility, it broadly refers to CNS disorders, but does not present detailed efficacy data. The focus is on claims of utility rather than demonstrated clinical effectiveness. 3. Are related compounds outside the patent’s scope patentable? Compounds significantly differing from the claimed structures or outside the specified substituents likely fall outside its scope. However, minor modifications might still infringe if they are considered equivalents. 4. How does the patent landscape for phenylpiperazines look today? Many subsequent patents cite or build upon Patent 3,714,226, making it a key piece in the patent landscape concerning CNS-active compounds. Its expiration has opened the market for generic development. 5. Can this patent’s claims be challenged or licensed? Given its age and expiration, licensing or legal challenges would focus on intellectual property rights stemming from other active patents or newer formulations. Currently, it functions predominantly as prior art. References U.S. Patent 3,714,226, “New pharmaceutical compounds and methods of use,” granted January 30, 1973. Relevant patent family filings and citations as per patent citation databases (e.g., USPTO PAIR, EPO DOCDB). Literature on phenylpiperazine derivatives and their therapeutic applications, including pharmacology reviews and patent analyses. This comprehensive review underscores the importance of Patent 3,714,226 in pharmaceutical patent history and provides a strategic understanding for professionals engaging with CNS drug development and patent strategizing. More… ↓ ⤷ Get Started Free

Details for Patent: 3,714,226

Summary for Patent: 3,714,226