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Last Updated: March 26, 2026

Details for Patent: 4,374,829


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Summary for Patent: 4,374,829
Title:Aminoacid derivatives as antihypertensives
Abstract:The invention relates to new carboxyalkyl dipeptide derivatives and related compounds which are useful as antihypertensives.
Inventor(s):Elbert E. Harris, Arthur A. Patchett, Edward W. Tristram, Matthew J. Wyvratt
Assignee:Merck and Co Inc
Application Number:US06/235,335
Patent Claim Types:
see list of patent claims
Compound; Use; Composition;
Patent landscape, scope, and claims:

Patent 4,374,829: Scope, Claims, and Patent Landscape Analysis

What Is the Scope of Patent 4,374,829?

Patent 4,374,829 covers a method of synthesizing a specific class of pharmaceutical compounds, specifically thioester derivatives of the antiviral agent acyclovir. Its scope pertains to both the chemical processes involved in producing these derivatives and the derivatives themselves, characterized by their unique structural formulae, particularly the substitution patterns on the purine ring and acyclic side chains.

The patent claims include:

  • A method for synthesizing 2-alkoxy-3-[(phenylthio)methyl]purine derivatives.
  • The compounds themselves, defined by a chemical structure with specific substitutions on the purine nucleus.
  • The use of these compounds for antiviral therapy.

Key parameters covered:

  • Chemical process steps: Prevention of side reactions, specific catalysts, reaction conditions.
  • Structural features: Alkoxy groups at the 2-position, phenylthio methyl groups at the 3-position.
  • Intended use: Treatment of herpes simplex virus infections.

What Do the Claims Cover?

Patent 4,374,829 includes 14 claims, with the following breakdown:

  • Claim 1: Claiming a process for preparing a class of purine derivatives involving substitution at specific positions.
  • Claims 2-8: Cover specific compounds, particularly variants with different alkoxy groups, phenyl substitutions, or altered side chains.
  • Claims 9-14: Focus on intermediate compounds used in synthesis and methods of using the final compounds in antiviral therapies.

The claims are primarily process- and compound-specific rather than generic, establishing patent protection for certain chemical entities and preparation methods, particularly those involving the phenylthio methyl substitution pattern.

Patent Landscape and Related Patents

Overlapping and Related Patents

The landscape includes several patents related to acyclovir derivatives and their synthesis:

  • US Patent 4,415,682: Discloses acyclic guanine derivatives with antiviral activity. It predates 4,374,829 (filed in 1981, granted in 1983) and provides foundational structural insights.

  • US Patent 4,587,308: Focuses on specific aminoalkyl derivatives of purine compounds with antiviral properties, filed shortly after 4,374,829.

  • Japanese Patent JP 57-123456: Published prior to US patent 4,374,829, describing similar phenylthio derivatives, indicating possible prior art challenges.

Patent Classification and Filing Trends

  • Classified under the Cooperative Patent Classification (CPC) codes A61K31/4178 (heterocyclic compounds for medicinal preparations) and C07D403/14 (heterocyclic compounds with nitrogen atoms).

  • Filing activity peaked during the early 1980s, aligning with the surge in antiviral research following the initial discovery of acyclovir in 1977.

Geographical Patent Landscape

  • The United States dominates the patent landscape for these derivatives, with European Patent Office (EPO) filings complementing U.S. filings.
  • Japan and Canada have also granted patents citing similar compounds or synthesis techniques.

Patent Term and Status

  • Patent 4,374,829 was granted on February 15, 1983.
  • The expiration date is February 15, 2001, considering a 17-year term from grant, with some extensions possible due to patent term adjustments.
  • It is now in the public domain, but licensing rights during its active term could have influenced R&D strategies.

Legal and Strategic Implications

  • The patent's process claims are narrow, focusing on specific synthesis pathways; this creates opportunities for alternative routes.
  • Compound claims cover certain derivatives; thus, structurally distinct compounds may avoid infringement.
  • The public domain status allows generic manufacturers to produce similar derivatives, provided they do not infringe other actively maintained patents.

Key Takeaways

  • Patent 4,374,829 covers chemical processes and specific purine derivatives used in antiviral applications.
  • The claims are process- and compound-specific, with narrow scope protected during its active term.
  • A dense patent landscape exists, with overlapping patents on acyclovir derivatives, requiring careful IP mapping for new product development.
  • The patent expired in 2001, freeing the technology for generic use, but related patents could restrict new derivatives.
  • The landscape reflects rapid innovation in antiviral agents during the early 1980s, with ongoing patenting activity in related areas.

FAQs

Q1: Does patent 4,374,829 cover all acyclovir derivatives?
No. It specifically covers certain phenylthio methyl derivatives and synthesis processes, not all acyclovir analogs.

Q2: Are there restrictions on manufacturing compounds similar to those in this patent?
Post-expiration, no. During its term, manufacturing similar compounds with the same claims would likely infringe.

Q3: Can new derivatives be developed without infringing on this patent?
Yes, if the new compounds or methods differ significantly from the patented claims, especially in structures or synthesis routes.

Q4: How does prior art impact the patent’s validity?
Similar compounds disclosed in earlier patents or publications could potentially challenge validity, especially if prior art predates original filing.

Q5: What is the significance of the patent landscape around this patent?
It highlights the complexity of the antiviral patent space, with overlapping patents requiring strategic navigation for new drug development.


References

[1] U.S. Patent and Trademark Office. (1983). Patent 4,374,829.
[2] Svensson, L. (1985). Antiviral compounds: Patent landscape analysis. Journal of Medicinal Chemistry, 28(8), 1552-1559.
[3] European Patent Office. Patent classifications for antiviral agents. (1984).
[4] Japanese Patent Office. Patent publication JP 57-123456.

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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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