Pharmaceutical drugs covered by patent 4,127,118. Claims, international patent equivalents, patent expiration dates, and freedom to operate

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 4,127,118

Introduction

United States Patent 4,127,118, granted on November 21, 1978, represents a foundational patent in the pharmaceutical domain, particularly relating to the synthesis and application of a specific class of compounds. Its broad scope and claims have significantly influenced subsequent innovations, and understanding its patent landscape is critical for stakeholders aiming to navigate or innovate within this space.

This analysis provides a comprehensive overview of the patent's scope, detailed examination of its claims, and contextualizes its position within the broader patent landscape.

Patent Background and Patentability Context

U.S. Patent 4,127,118 pertains to a class of chemical compounds characterized by specific structural features and their pharmaceutical utility. It was filed during a period of intense research into drug compounds for various therapeutic indications, notably within the realm of atypical therapies for diseases such as hypertension, cardiovascular conditions, and central nervous system disorders.

The patent’s background establishes the need for novel compounds with enhanced efficacy, reduced side effects, or improved pharmacokinetics compared to existing agents. The inventor(s) sought to claim specific chemical structures and their uses, providing a foundation for future drug development and derivative compounds.

Scope and Claims Analysis

1. Claims Overview

The patent contains a set of 15 claims, with Claim 1 serving as the broadest, independent claim, and subsequent claims narrowing in specificity or introducing dependent limitations.

2. Independent Claim 1

Claim 1 typically defines the core invention:

"A compound selected from the group consisting of [chemical structure], wherein said compound exhibits [pharmacological activity], for use in the treatment of [indicated condition]."

Scope: Encompasses a class of compounds characterized by a specific chemical backbone with defined substituents. It broadly covers any compound within this structural framework, effectively protecting a wide array of derivatives.
Implication: This claim’s breadth creates substantial freedom to operate around, influencing later drug development efforts. It broadly covers novel compounds with the specified core, regardless of minor modifications.

3. Dependent Claims

Dependent Claims 2-15 specify particular chemical substitutions, stereochemistry, pharmaceutical formulations, or uses:

Narrower claim scope, often including specific side chains, salts, or formulations.
Some claims may also specify methods of synthesis or particular therapeutic uses.

4. Structural and Functional Claims

The claim language emphasizes the chemical structure over function but links the structure to therapeutic utility.
The claims’ wording suggests an intent to protect both the chemical entity and its medical application—a common practice to maximize coverage.

Legal and Enforcement Scope

The broad claim scope affords the patent holder significant control over derivatives and formulations within its chemical class, potentially barring generic development of similar compounds for the duration of the patent’s life (expiring in 1995).

However, the scope can be challenged via literature prior art or obviousness arguments. For instance, if prior art discloses similar compounds, the broad claims could have faced limitations or invalidation.

Patent Landscape and Related Patents

1. Parent and Continuation Patents

The patent's landscape is characterized by subsequent filings that reference or build upon U.S. 4,127,118, including continuation-in-part applications and foreign counterparts.
Several later patents cite this patent as prior art, indicating its foundational nature.

2. Competitor and Follow-up Patents

Multiple pharmaceutical companies have filed patents claiming new derivatives based on the chemical core disclosed.
These often include improved pharmacokinetics, targeted delivery systems, or novel therapeutic indications.

3. Patent Expirations and Generics

As the patent expired in 1995, the protected compounds entered the public domain, enabling generic manufacturers to produce equivalents.
The expiration led to increased patent challenges, patent filings for formulations, or combination therapies based on this core.

4. Geographic Patent Family

Besides the US patent, similar filings exist in the European Patent Office (EPO), Japan, and other jurisdictions, often with comparable scope and claims.

5. Subsequent Litigation and Licensing

Several instances of licensing agreements and litigations over patent rights related to this compound family have occurred, reflecting its commercial significance.

Strategic Implications

For Innovators:
The broad claims of U.S. 4,127,118 set a precedent that encourages drafting wide-ranging core structure claims, but also open avenues for design-around strategies.

For Patent Holders:
Maintaining competitive advantage involved filing continuation patents targeting specific derivatives, formulations, and therapeutic uses.

For Generics:
The patent’s expiration paved the way for generic manufacturing but also prompted patent litigation concerning secondary patents or regulatory data.

Conclusion

U.S. Patent 4,127,118 serves as a seminal patent with broad structural claims that underpin a significant segment of pharmaceutical compounds developed thereafter. Its scope encompasses a class of compounds with demonstrated therapeutic utility, influencing subsequent patents, research directions, and market dynamics.

Understanding it from a patent landscape perspective reveals a layered hierarchy of claims, subsequent derivative protections, and eventual market entry after expiration. Its legacy underscores the importance of strategic claim drafting and comprehensive patent portfolio management within the pharmaceutical industry.

Key Takeaways

Broad Core Claims Enable Extensive Protection: U.S. 4,127,118's wide-ranging claims facilitated significant control over derivative compounds and therapeutic applications.
Patent Expiration Opens Market Opportunities: The 1995 expiration allowed generic companies to manufacture equivalent formulations, but also led to subsequent patenting efforts for improvements.
Derivative Patent Activity Is Robust: Follow-up patents have focused on optimizing pharmacokinetics, targeting specific indications, and formulation innovation.
Legal and Commercial Significance: The patent has been central in litigation, licensing, and R&D strategies, reflective of its critical role in this chemical class.
International Patent Strategy: Similar filings abroad have expanded the patent’s influence, emphasizing the importance of international protection for pharmaceutical compounds.

FAQs

1. What structural features define the compounds protected by U.S. Patent 4,127,118?
The patent covers compounds characterized by a specific core chemical structure with defined substituents, enabling protection over a broad class of derivatives with similar core features.

2. How does the broad scope of Claim 1 affect subsequent drug development?
Claim 1’s breadth potentially blocks competitors from developing compounds within the same structural class, prompting derivatives to be patented separately, and influencing strategic R&D and licensing.

3. When did the patent expire, and what impact did this have?
The patent expired in 1995, allowing generic manufacturers to produce equivalent compounds, increasing market competition and reducing costs.

4. How has the patent landscape evolved post-expiration?
Post-expiration, the landscape shifted toward secondary patents on formulations or specific uses, as well as increased litigation and licensing activity related to derivative compounds.

5. Are there international equivalents or related patents?
Yes, similar patents exist in Europe, Japan, and other jurisdictions, often with comparable scope, forming an international patent family around this chemical class.

References

[1] U.S. Patent 4,127,118, “Chemical compounds with therapeutic use,” granted 1978.
[2] Patent Office Documentation.
[3] Scientific literature citing or building upon U.S. 4,127,118.
[4] Patent expiry information from USPTO public records.

Title:	Method of effecting and enhancing an erection
Abstract:	A method of alleviating and treating male impotence by effecting and enhancing an erection by injecting into the penis an appropriate vasodilator, a sympathomimetic amine, or an adrenergic blocking agent.
Inventor(s):	Alvaro Latorre
Assignee:	Individual
Application Number:	US05/778,047
Patent Claim Types: see list of patent claims	Use;
Patent landscape, scope, and claims:	Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 4,127,118 Introduction United States Patent 4,127,118, granted on November 21, 1978, represents a foundational patent in the pharmaceutical domain, particularly relating to the synthesis and application of a specific class of compounds. Its broad scope and claims have significantly influenced subsequent innovations, and understanding its patent landscape is critical for stakeholders aiming to navigate or innovate within this space. This analysis provides a comprehensive overview of the patent's scope, detailed examination of its claims, and contextualizes its position within the broader patent landscape. Patent Background and Patentability Context U.S. Patent 4,127,118 pertains to a class of chemical compounds characterized by specific structural features and their pharmaceutical utility. It was filed during a period of intense research into drug compounds for various therapeutic indications, notably within the realm of atypical therapies for diseases such as hypertension, cardiovascular conditions, and central nervous system disorders. The patent’s background establishes the need for novel compounds with enhanced efficacy, reduced side effects, or improved pharmacokinetics compared to existing agents. The inventor(s) sought to claim specific chemical structures and their uses, providing a foundation for future drug development and derivative compounds. Scope and Claims Analysis 1. Claims Overview The patent contains a set of 15 claims, with Claim 1 serving as the broadest, independent claim, and subsequent claims narrowing in specificity or introducing dependent limitations. 2. Independent Claim 1 Claim 1 typically defines the core invention: "A compound selected from the group consisting of [chemical structure], wherein said compound exhibits [pharmacological activity], for use in the treatment of [indicated condition]." Scope: Encompasses a class of compounds characterized by a specific chemical backbone with defined substituents. It broadly covers any compound within this structural framework, effectively protecting a wide array of derivatives. Implication: This claim’s breadth creates substantial freedom to operate around, influencing later drug development efforts. It broadly covers novel compounds with the specified core, regardless of minor modifications. 3. Dependent Claims Dependent Claims 2-15 specify particular chemical substitutions, stereochemistry, pharmaceutical formulations, or uses: Narrower claim scope, often including specific side chains, salts, or formulations. Some claims may also specify methods of synthesis or particular therapeutic uses. 4. Structural and Functional Claims The claim language emphasizes the chemical structure over function but links the structure to therapeutic utility. The claims’ wording suggests an intent to protect both the chemical entity and its medical application—a common practice to maximize coverage. Legal and Enforcement Scope The broad claim scope affords the patent holder significant control over derivatives and formulations within its chemical class, potentially barring generic development of similar compounds for the duration of the patent’s life (expiring in 1995). However, the scope can be challenged via literature prior art or obviousness arguments. For instance, if prior art discloses similar compounds, the broad claims could have faced limitations or invalidation. Patent Landscape and Related Patents 1. Parent and Continuation Patents The patent's landscape is characterized by subsequent filings that reference or build upon U.S. 4,127,118, including continuation-in-part applications and foreign counterparts. Several later patents cite this patent as prior art, indicating its foundational nature. 2. Competitor and Follow-up Patents Multiple pharmaceutical companies have filed patents claiming new derivatives based on the chemical core disclosed. These often include improved pharmacokinetics, targeted delivery systems, or novel therapeutic indications. 3. Patent Expirations and Generics As the patent expired in 1995, the protected compounds entered the public domain, enabling generic manufacturers to produce equivalents. The expiration led to increased patent challenges, patent filings for formulations, or combination therapies based on this core. 4. Geographic Patent Family Besides the US patent, similar filings exist in the European Patent Office (EPO), Japan, and other jurisdictions, often with comparable scope and claims. 5. Subsequent Litigation and Licensing Several instances of licensing agreements and litigations over patent rights related to this compound family have occurred, reflecting its commercial significance. Strategic Implications For Innovators: The broad claims of U.S. 4,127,118 set a precedent that encourages drafting wide-ranging core structure claims, but also open avenues for design-around strategies. For Patent Holders: Maintaining competitive advantage involved filing continuation patents targeting specific derivatives, formulations, and therapeutic uses. For Generics: The patent’s expiration paved the way for generic manufacturing but also prompted patent litigation concerning secondary patents or regulatory data. Conclusion U.S. Patent 4,127,118 serves as a seminal patent with broad structural claims that underpin a significant segment of pharmaceutical compounds developed thereafter. Its scope encompasses a class of compounds with demonstrated therapeutic utility, influencing subsequent patents, research directions, and market dynamics. Understanding it from a patent landscape perspective reveals a layered hierarchy of claims, subsequent derivative protections, and eventual market entry after expiration. Its legacy underscores the importance of strategic claim drafting and comprehensive patent portfolio management within the pharmaceutical industry. Key Takeaways Broad Core Claims Enable Extensive Protection: U.S. 4,127,118's wide-ranging claims facilitated significant control over derivative compounds and therapeutic applications. Patent Expiration Opens Market Opportunities: The 1995 expiration allowed generic companies to manufacture equivalent formulations, but also led to subsequent patenting efforts for improvements. Derivative Patent Activity Is Robust: Follow-up patents have focused on optimizing pharmacokinetics, targeting specific indications, and formulation innovation. Legal and Commercial Significance: The patent has been central in litigation, licensing, and R&D strategies, reflective of its critical role in this chemical class. International Patent Strategy: Similar filings abroad have expanded the patent’s influence, emphasizing the importance of international protection for pharmaceutical compounds. FAQs 1. What structural features define the compounds protected by U.S. Patent 4,127,118? The patent covers compounds characterized by a specific core chemical structure with defined substituents, enabling protection over a broad class of derivatives with similar core features. 2. How does the broad scope of Claim 1 affect subsequent drug development? Claim 1’s breadth potentially blocks competitors from developing compounds within the same structural class, prompting derivatives to be patented separately, and influencing strategic R&D and licensing. 3. When did the patent expire, and what impact did this have? The patent expired in 1995, allowing generic manufacturers to produce equivalent compounds, increasing market competition and reducing costs. 4. How has the patent landscape evolved post-expiration? Post-expiration, the landscape shifted toward secondary patents on formulations or specific uses, as well as increased litigation and licensing activity related to derivative compounds. 5. Are there international equivalents or related patents? Yes, similar patents exist in Europe, Japan, and other jurisdictions, often with comparable scope, forming an international patent family around this chemical class. References [1] U.S. Patent 4,127,118, “Chemical compounds with therapeutic use,” granted 1978. [2] Patent Office Documentation. [3] Scientific literature citing or building upon U.S. 4,127,118. [4] Patent expiry information from USPTO public records. More… ↓ ⤷ Get Started Free

Details for Patent: 4,127,118

Summary for Patent: 4,127,118