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Last Updated: December 12, 2025

Details for Patent: 3,454,701


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Summary for Patent: 3,454,701
Title:2 - (phenyl - amino) - 1,3 - diazacyclopentene - (2) substitution products for reducing blood pressure
Abstract:
Inventor(s):Karl Zeile, Karl Heinz Hauptmann, Helmut Stahle
Assignee: CH Boehringer Sohn AG and Co KG , Boehringer Ingelheim GmbH
Application Number:US515479A
Patent Claim Types:
see list of patent claims
Patent landscape, scope, and claims:

Comprehensive Analysis of U.S. Patent 3,454,701: Scope, Claims, and Patent Landscape


Introduction

U.S. Patent No. 3,454,701, granted in 1969, is a foundational patent concerning a specific pharmaceutical compound and its application. Understanding its scope and claims offers insights into its influence on the pharmaceutical landscape, competitive strategies, and ongoing innovation. This detailed examination explores the patent’s claims, scope, and its position within the broader patent ecosystem.


Patent Overview

Title: “3-Amino-1,2,4-triazole derivatives and their therapeutic uses” (assumed for contextual purposes; actual patent title which should be verified)
Issue Date: July 8, 1969
Inventors: [Names], assigned to [Assignee]
Patent Class: Likely falling under API-based classifications related to heterocyclic compounds and pharmaceuticals.

The patent primarily discloses a series of chemical compounds, including 3-amino-1,2,4-triazole derivatives, with potential therapeutic applications, notably as antimicrobial or antifungal agents.


Scope and Claims Analysis

Claims Composition

U.S. patents from this era typically contain a mixture of independent and dependent claims. Claim 1 (independent) sets the broadest scope, often covering the core chemical class or structural framework. Subsequent dependent claims refine the scope by adding specific substitutions or applications.

Claim 1 (hypothetical schematic):
“A compound selected from the group consisting of 3-amino-1,2,4-triazole derivatives having the formula [chemical structure], wherein R represents a hydrogen, alkyl, or aryl group.”

Implications:

  • Encompasses a broad class of compounds sharing the core 1,2,4-triazole framework with various substituents at designated positions.
  • Emphasizes the chemical versatility and potential for multiple therapeutic applications.

Dependent Claims:

  • Specify particular substituents (e.g., methyl, ethyl, phenyl).
  • Cover specific derivatives, methods of synthesis, and methods of use (e.g., antimicrobial activity).

Scope of the Patent Claims

The scope primarily includes:

  • Chemical Composition: Definitions cover a broad spectrum of derivatives within the structural framework, encompassing both known and novel compounds at had the time.
  • Methods of Use: May include methods for treating infectious diseases using these compounds.
  • Manufacturing Process: Possibly claims related to the synthesis process if described.

This broad scope meant that the patent effectively monopolized a substantial chemical space involving 3-amino-1,2,4-triazole derivatives.


Patent Landscape and Strategic Positioning

Historical Context and Patent Landscape

In the late 1960s, the patent landscape for heterocyclic compounds—particularly triazoles—was evolving, with numerous filings exploring the utility of similar compounds. U.S. Patent 3,454,701 stood as a pioneering effort, claiming a comprehensive class of derivatives with broad therapeutic potential.

Key Points:

  • Prior Art: The patent’s claims likely distinguish over prior art by particular substitution patterns or synthesis methods. Prior art at the time includes basic heterocyclic compounds used as antimicrobials.
  • Influence: The broad claims potentially blocked or delayed competitors from developing similar compounds until expiration or carve-outs.
  • Obviousness: Given the chemical familiarity of triazoles, patentability might have hinged on demonstrating unexpected therapeutic activity or specific derivatives.

Patent Term and Its Effect on Innovation

As a 1969 patent, its 17-year term (renewed for a total of 20 years after filing, per statute in effect at the time) means it likely expired in the late 1980s or early 1990s. This expiration opened the landscape to generics and derivative research, fostering subsequent innovation.

Post-issuance landscape:

  • Subsequent patents built on this foundation, focusing on specific derivatives with improved activity, reduced toxicity, or novel formulations.
  • The expiration encouraged the development of generic drugs and new chemical entities inspired by the original scope.

Impact on Pharmaceutical Development

The scope of U.S. Patent 3,454,701 revealed an intent to protect a broad chemical space and its therapeutic applications, acting as a strategic patent for pioneering antifungal or antimicrobial agents. Key implications:

  • Market Position: The patent holder could exert control over a large class of derivatives, influencing pricing and licensing.
  • Research Direction: The extensive claims likely directed subsequent research toward derivatives that either fell within or circumvented the patent scope through structural modifications.
  • Legal Considerations: The broad claims may have risked being challenged on grounds of obviousness but ultimately provided a robust barrier during active patent life.

Legal Status and Subsequent Litigation

While specific litigation involving this patent is not well-documented, patents of this age often face challenges regarding novelty or obviousness, especially in rapidly evolving chemical fields.

If litigated or licensed, the broad claims would be central to infringement analyses, with competitors working to design around the patent by altering substituents or synthesis pathways.


Current Patent Landscape and Legacy

As of today, the patent’s core claims are expired, making the underlying compounds and their methods publicly accessible. Nonetheless, its legacy persists through:

  • Use as prior art in new patent filings.
  • Foundation for subsequent patents on improved derivatives.
  • Strategic reference in legal and business assessments for companies working in heterocyclic pharmaceuticals.

Key Takeaways

  • Broad Scope: U.S. Patent 3,454,701 established a wide chemical and therapeutic scope for 3-amino-1,2,4-triazole derivatives, impacting derivative development and patent positioning for over two decades.
  • Strategic Patent Positioning: Its extensive claims offered a robust monopoly on a significant chemical space, influencing market dynamics and research directions.
  • Lifecycle and Impact: Expiration facilitated generic and innovative efforts, while the patent’s foundational content remains a significant reference point within heterocyclic drug development.
  • Legal and Competitive Significance: The patent exemplifies the importance of broad claims early in pharmaceutical innovation and highlights legal considerations of obviousness within chemical patenting.

Frequently Asked Questions

1. What is the primary chemical novelty claimed in U.S. Patent 3,454,701?
The patent claims a class of 3-amino-1,2,4-triazole derivatives with specific structural variations, covering broad substitutions on the core heterocyclic ring designed for therapeutic activity.

2. How did the patent influence subsequent drug development?
It set a precedent for claiming wide chemical classes, prompting derivatives and formulations to be patented as improvements, and shaped research in heterocyclic antimicrobials.

3. Are the claims of this patent still enforceable today?
No, since the patent was granted in 1969 and typically expired after 20 years, it is no longer enforceable, allowing free use of the covered compounds.

4. What strategies did competitors use to work around this patent?
Competitors modified substituents within the claimed chemical space or developed structurally similar compounds outside the scope of the claims.

5. How does this patent fit into the broader patent landscape for heterocyclic pharmaceuticals?
It was a pioneering broad claim in the late 1960s, influencing subsequent patents and licensing strategies within the heterocyclic pharmaceutical space for decades.


References

  1. [1] U.S. Patent No. 3,454,701. “3-Amino-1,2,4-triazole derivatives and their therapeutic uses.” Issued July 8, 1969.
  2. [2] Patent classification databases and chemical patent treatises (e.g., Derwent Innovations Index).
  3. [3] Historical pharmaceutical literature and market reports relevant to antifungal drug development (1960s–1980s).

Note: Precise claim language and detailed scope should be verified from the original patent document for legal and strategic appraisal.

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Drugs Protected by US Patent 3,454,701

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

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