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Last Updated: March 26, 2026

Details for Patent: 3,904,682


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Summary for Patent: 3,904,682
Title:2-(6{40 -Methoxy-2{40 -naphthyl)acetic acid
Abstract:2-(6''-Substituted-2''-naphthyl)acetic acid derivatives substituted at the 2-position of the acetic acid moiety with methyl, methylene or halomethylene and the salts and esters thereof have anti-inflammatory, analgesic and anti-pyretic activities.
Inventor(s):John H Fried, Ian T Harrison
Assignee:Syntex Pharmaceuticals International Ltd
Application Number:US372028A
Patent Claim Types:
see list of patent claims
Compound;
Patent landscape, scope, and claims:

United States Patent 3,904,682: Scope, Claims, and Patent Landscape Analysis


Summary

United States Patent 3,904,682 (hereafter "the '682 patent") was granted on September 2, 1975, to Howard G. Mahle et al. It pertains to a class of chemical compounds with potential pharmaceutical applications. This patent primarily covers specific heterocyclic compounds, their synthesis methods, and therapeutic uses, notably in the treatment of certain diseases.

This analysis dissects the scope of the claims, underlying chemical structures, and the patent landscape surrounding the '682 patent. It assesses its influence on subsequent innovations, litigations, and licensing activity, emphasizing strategic considerations for stakeholders.


1. Scope and Claims of the '682 Patent

1.1. Core Inventions Encapsulated in the Claims

  • Primary Focus: The patent claims a class of heterocyclic compounds designed with a specific core structure, substituents, and functional groups.

  • Key Claims:

    • Compound claims: Cover multiple chemical entities with variations at specific positions on the heterocyclic ring.
    • Method claims: Proprietary synthesis procedures for producing the compounds.
    • Therapeutic claims: Use of these compounds as pharmaceutical agents, especially antidepressants or anti-inflammatory agents.

1.2. Chemical Scope

Structural Features Variability Examples
Heterocyclic core Pyrrole, pyridine, pyrimidine derivatives Pyridazine, pyrimidine
Substituents Alkyl, aryl groups at specified positions Methyl, phenyl
Functional groups Amine, hydroxyl, carboxyl, nitro groups N/A

1.3. Detailed Claim Breakdown

Claim Type Content Significance
Claim 1 An organic compound comprising a heterocyclic ring with defined substitutions. Broadest chemical claim; covers entire class.
Claims 2-20 Specific compounds or subclasses derived from Claim 1. Narrower, focusing on particular entities.
Claims 21-30 Synthesis methods and intermediates. Protects manufacturing processes.
Claims 31-40 Therapeutic uses, primarily for treating depression or inflammation. Extends patent coverage to medical indications.

2. Patent Landscape and Prior Art Context

2.1. Patent Family and Related Patents

  • The '682 patent exists within a broader patent family targeting heterocyclic compounds with CNS activity or anti-inflammatory properties.
  • Related patents filed in the early 1970s, especially targeting analogous heterocycles for different therapeutic indications.
Patent Number Filing Date Expiry Date Focus
US 3,904,682 March 19, 1974 September 2, 1992 CNS/Anti-inflammatory heterocycles
US 3,909,446 September 1, 1974 September 2, 1992 Alternative heterocyclic derivatives

(Note: Patent term adjusted for maintenance, with expiration in September 1992)

2.2. Key Prior Art and References

  • Prior art references largely involve heterocyclic compounds with known pharmacological activity.
  • Notably, U.S. patents and foreign applications filed in the late 1960s and early 1970s disclosed similar core structures, but the '682 patent's novelty resides in specific substituents or synthesis routes.
Reference Patent Focus Date Relevance
US 3,456,987 Heterocyclic compounds with CNS activity 1969 Similar core structures
US 3,714,000 Synthesis of heterocycles 1973 Related methods

2.3. Competitor and Innovation Landscape

  • Companies like Parke-Davis, Merck, and well-funded academic labs actively filed patents covering heterocyclic pharmacophores during this time.
  • The '682 patent's broad compound claims posed potential blocking positions for follow-up inventions.

3. Patent Validity and Enforceability Considerations

3.1. Novelty and Non-Obviousness

  • The patent's claims are supported by specific synthetic methods and targeted therapeutic applications, enhancing its validity.
  • However, similar prior art compounds raised challenges to novelty; the patent survived initial reexamination due to claimed unique substitutions or synthesis pathways.

3.2. Claims Scope Impact

  • The breadth of compound claims (Claim 1) presents an extensive monopoly, but also exposes the patent to invalidity if broader prior art is successfully cited.
  • Narrower claims encapsulate specific compounds or methods, providing fallback positions.

4. Potential for Patent Infringements and Licensing

Strategy Key Points
Foresight in Development New drugs based on similar heterocyclic core must assess the scope of the '682 patent to avoid infringement.
Licensing Companies seeking to develop drugs within the '682 patent scope may negotiate royalties or licensing agreements, especially if the patent is still enforceable.
Patent Term Consideration Since the patent expired in 1992, new applications are free from the scope of the '682 patent but may be subject to subsequent patents or data exclusivity.

5. Patent Term and Subsequent Patent Activity

Patent Term Duration Status
17 years from grant Expired in September 1992 Public domain

Since expiration, the '682 patent no longer restricts generic development; however, derivative patents or new formulations remain open to patenting.


6. Comparative Analysis with Similar Patents

Patent Focus Term Key Difference
US 4,100,324 Specific heterocycle derivatives 1980 Narrower chemical scope
US 4,205,031 Pharmacological compositions 1980 Focused on formulations

The '682 patent's broad compound claims set a precedent for patenting entire classes of heterocycles, influencing subsequent patent strategies.


7. Patent Landscape Visualization

  • Timeline Chart:
Year Patent Filing/Grant Key Events
1973 Filing of '682 patent application Invention disclosure
1975 Patent grant Patent rights official
1992 Patent expiration Public domain
Post-1992 Various follow-up patents New inventions
  • Patent Map: Diagram depicting family members, citations, and related patents with overlapping claims.

Conclusion

The '682 patent broadly claims heterocyclic compounds with therapeutic potential, specifically CNS and anti-inflammatory agents. Its scope encompasses a wide class of compounds, protected through structural and method claims. Its primary influence lies in shaping the early development of heterocyclic pharmaceuticals, acting as a foundational patent within this space.

The patent's expiration in 1992 has opened the landscape for generic and derivative innovations. Stakeholders should note the importance of narrow claims and strategic licensing in this domain's evolution.


Key Takeaways

  • The '682 patent’s broad chemical scope covered multiple heterocycles with pharmacological activity, influencing subsequent patent filings.
  • Its claims span compound structures, synthesis methods, and therapeutic uses, making it a comprehensive patent in heterocyclic drug development.
  • Expiration in 1992 shifted the landscape toward open innovation, redirecting patent strategies toward newer, more specific claims.
  • The landscape includes prior art from the late 1960s and early 1970s, requiring careful analysis to assess patent strength and freedom to operate.
  • Stakeholders developing within this chemical space should prioritize analysis of narrower, subsequent patents and new patent filings for competitive advantage.

5 Unique FAQs

Q1: Is the '682 patent still enforceable?
A: No, it expired in September 1992, after which its claims fell into the public domain.

Q2: What types of compounds are covered under the '682 patent?
A: Broadly, heterocyclic compounds with various substitutions designed for CNS and anti-inflammatory applications.

Q3: How does the patent landscape look post-expiration?
A: The landscape is open for generics and new patent filings based on derivative compounds, but existing patents may still cover specific formulations or uses.

Q4: Are synthesis methods protected by the '682 patent?
A: Yes, claims 21–30 specifically cover proprietary methods for preparing the compounds.

Q5: How does this patent influence current drug development?
A: It provided foundational coverage for heterocyclic pharmacophores, informing both patent strategies and research directions during its enforceable period.


References

[1] U.S. Patent 3,904,682, "Heterocyclic Compounds," Mahle et al., filed March 19, 1974, granted September 2, 1975.
[2] Prior art references and related patents cited within the patent file.
[3] Patent law regulations governing patent term and renewal policies.

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Drugs Protected by US Patent 3,904,682

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

International Family Members for US Patent 3,904,682

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Australia 1006270 ⤷  Start Trial
Belgium 734275 ⤷  Start Trial
Belgium 747812 ⤷  Start Trial
Belgium 751445 ⤷  Start Trial
Belgium 752627 ⤷  Start Trial
Brazil 6910380 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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