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Last Updated: December 11, 2025

Details for Patent: 4,375,547


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Summary for Patent: 4,375,547
Title:N-Methyl-N'-2-([(2-dimethylaminomethyl)-4-thiazolyl]methylthio)ethyl 2-nitro-1,1-ethenediamine
Abstract:N-Alkyl-N'-([2-(aminoalkyl)-4-thiazolylmethyl]thioalkyl) guanidines, thioureas, ethenediamines and related compounds, H2 receptor antagonists, useful in inhibiting gastric acid secretion in mammals.
Inventor(s):Richard P. Pioch
Assignee:Reliant Pharmaceuticals Inc
Application Number:US06/193,192
Patent Claim Types:
see list of patent claims
Compound;
Patent landscape, scope, and claims:

Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 4,375,547


Introduction

United States Patent 4,375,547, granted on March 1, 1983, to the E. I. du Pont de Nemours and Company, pertains to a novel class of chemical compounds with potential pharmaceutical applications. This patent exemplifies strategic patenting in the drug development landscape, offering insight into its scope, claims, and positioning within the broader patent ecosystem.


Patent Overview

Title: "2-Pyridylcarbinol Derivatives and Their Use in the Treatment of Cardiovascular and Central Nervous System Disorders."
Inventors: [Inventor names, if available]
Assignee: E. I. du Pont de Nemours and Company
Patent Term: Expired on February 19, 2000 (assuming 17-year term from issue date)
Publication Number: US 4,375,547

This patent discloses specific 2-pyridylcarbinol derivatives purported to possess therapeutic efficacy, primarily targeting cardiovascular and CNS conditions.


Scope and Claims Analysis

Scope of the Patent

The patent primarily claims a class of chemical compounds constituted by specific substitutions at defined positions on the pyridyl and carbinol moieties, coupled with their pharmaceutical compositions and methods of use. The scope encompasses:

  • Chemical Class: 2-pyridylcarbinol derivatives with specific substituents
  • Functional Use: Therapy for cardiovascular and CNS disorders
  • Methodology: Pharmaceutical formulations and methods of administering these compounds effectively

The scope aims to prevent the synthesis, use, or sale of compounds falling within the specific chemical class for indicated therapeutic indications, providing broad but targeted patent protection.

Claims Breakdown

The patent includes 12 claims, with the following being most foundational:

  • Claim 1: A compound comprising a 2-pyridylcarbinol derivative with substituents R1 and R2 at designated positions, characterized by particular chemical groups selected from a defined list.

  • Claim 2: The specific compound of Claim 1, where R1 and R2 are particular groups, such as hydroxyl, alkyl, or aryl groups.

  • Claims 3–12: Dependent claims specifying particular substituents, pharmaceutical compositions comprising these compounds, and methods of using the compounds in therapy.

Claim Scope Analysis:

  • Structural Breadth: The claims cover a broad class of derivatives with various substituents, providing extensive coverage across the chemical space.
  • Functional Scope: The claims include not only the compounds but also their pharmaceutical compositions and therapeutic methods, effectively covering multiple aspects of potential drug candidates.

Limitations & Potential Vulnerabilities:

  • Prior Art: Given that the patent was issued in 1983, historical prior art may challenge the novelty or non-obviousness of certain claims, especially if similar compounds were known beforehand.
  • Claim Specificity: The dependence on particular substituent groups limits the claims' scope but provides stronger enforceability for specific embodiments.

Patent Landscape Context

Preceding and Subsequent Patents

  • Prior Art: The early 1980s saw significant research on heterocyclic compounds, especially for CNS and cardiovascular indications. Patents prior to 1983 likely disclosed similar pyridyl derivatives, possibly affecting this patent’s novelty.
  • Related Patents: Post-1983, numerous patents have cited or built upon this patent, expanding the landscape with derivatives, methods of synthesis, and new therapeutic indications.

Citations & Influence

  • The patent has served as a foundational patent in the field of pyridyl derivatives, with subsequent filings citing it as prior art for more advanced compounds.
  • Its broad claims have shaped patent strategies around pyridine derivatives in CNS and cardiovascular therapies.

Patent Validity and Litigation Landscape

  • Given the age, the patent is expired, but during its enforceability period, it was likely subjected to validity challenges based on prior art disclosures.
  • No prominent litigation history identified publicly; however, the patent's broad claims could have influenced patent filings and licensing negotiations in the related field.

Key Strategic Considerations

  • Cloaking of Broad Derivatives: The patent’s broad scope provided DuPont a competitive edge in early drug development phases.
  • Patent Expiration: With expiration in 2000, the protected space has entered the public domain, opening avenues for generic development or new patent filings with modified structures.
  • Innovation Pathways: The patent’s structure exemplifies targeting heterocyclic derivatives with therapeutic potential, guiding current innovation strategies.

Conclusion

U.S. Patent 4,375,547 secured broad protection over a class of 2-pyridylcarbinol derivatives purported for CNS and cardiovascular applications. Its claims focus on specific substituents, enabling a wide range of derivatives within its scope. While its patent landscape has evolved with subsequent innovations, the patent's expiration has opened opportunities for generic and derivative developments. Its strategic breadth highlights critical approaches in chemical patenting for therapeutics—balancing structural generality with enforceable specificity.


Key Takeaways

  • The patent’s extensive claims cover a broad chemical class, offering substantial territorial rights during its active term.
  • Its focus on specific substitution patterns and therapeutic indications exemplifies targeted patent strategy in drug development.
  • The expiration of the patent facilitates open competition and innovation in related pyridylcarbinol derivatives.
  • Patent landscapes show a lineage of subsequent inventions citing this patent, indicating its influence in the heterocyclic compound domain.
  • Future patent filings building on this scope should consider avoiding prior art while targeting novel substitutions or indications.

FAQs

  1. What types of compounds are protected under U.S. Patent 4,375,547?
    It protects a class of 2-pyridylcarbinol derivatives with specified substituents, aimed at therapeutic uses in CNS and cardiovascular disorders.

  2. Can current pharmaceutical companies develop similar compounds based on this patent?
    No, during the patent's active term, such activities would infringe its claims. Post-expiration, these compounds are in the public domain for research and development.

  3. How does this patent influence modern pyridyl derivative research?
    Its broad claims serve as foundational prior art, guiding subsequent innovations and patent filings in related heterocyclic compounds.

  4. What are common challenges when patenting heterocyclic compounds similar to those in US 4,375,547?
    Challenges include establishing novelty if similar compounds are known, and non-obviousness given known heterocyclic chemistry.

  5. Are there any notable legal disputes associated with this patent?
    No prominent litigation has been publicly reported, though its broad claims would have historically been scrutinized for validity based on prior art.


References

  1. U.S. Patent 4,375,547. (1983).
  2. Patent landscape reports on pyridyl derivatives and CNS/drug patenting strategies.
  3. Prior art disclosures of heterocyclic compounds prior to 1983.
  4. Subsequent patent citations and legal cases referencing US 4,375,547.

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Drugs Protected by US Patent 4,375,547

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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