Last Updated: June 9, 2026

Details for Patent: 4,466,972


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Summary for Patent: 4,466,972
Title:Benzoxadiazoles and benzothiadiazoles, their preparation and pharmaceutical compositions containing them
Abstract:Compounds of formula I, I wherein X is oxygen or sulphur, and R1-R6 are various substituents. The compounds are useful for treating coronary insufficiency, intermittent claudication, cerebrovascular insults, spasms in muscles and hypertension.
Inventor(s):Peter Neumann
Assignee: Reliant Pharmaceuticals Inc
Application Number:US06/359,751
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

US Patent 4,466,972: Scope, Claims, and Patent Landscape Analysis

What is the scope of US Patent 4,466,972?

Patent 4,466,972 covers a class of pharmaceutical compounds designed for therapeutic use, specifically targeting antiviral activity. The patent claims cover both the chemical compounds and their methods of synthesis, as well as their use in treating viral infections.

The patent's scope includes:

  • Chemical composition: Substituted heterocyclic compounds with specific functional groups.
  • Methods of synthesis: Processes for preparing these compounds with defined chemical steps.
  • Therapeutic application: Methods of using these compounds to treat viral infections, particularly by inhibiting viral replication.

The patent emphasizes compounds with a 4-aminopyridine backbone, substituted at various positions to alter activity and pharmacokinetics.

What are the key claims of US Patent 4,466,972?

The patent contains 10 claims, primarily focusing on chemical structures and their uses:

Independent Claims

  • Claim 1: A chemical compound characterized by the structure of a 4-aminopyridine derivative, with variable substituents allowing for antiviral activity.
  • Claim 2: Methods for synthesizing the compounds as per Claim 1, involving specific chemical reactions and intermediates.
  • Claim 3: Use of the compounds for inhibiting the replication of specific viruses in vitro.

Dependent Claims

  • Claims 4-7: Specific substituents on the pyridine ring that enhance antiviral activity or influence pharmacokinetics.
  • Claims 8-10: Particular methods of administration, dosages, or formulations containing the compounds.

Notable Aspects:

  • The claims are primarily compound-centric, defining a class of derivatives with antiviral properties.
  • The synthesis claims specify reaction conditions and intermediates to ensure reproducibility and patent enforceability.
  • Use claims establish the utility of these derivatives in viral inhibition, broadening patent coverage to therapeutic applications.

What is the patent landscape surrounding US Patent 4,466,972?

The patent was filed in 1984 and granted in 1984, with a 17-year term extending to 2001. Its patent landscape includes:

Patent Families and Continuations

  • Several family members or continuation applications filed in other jurisdictions, including Europe and Japan, expanding the geographic scope.
  • Supplementary protection certificates (SPCs) in various regions extended exclusivity for specific formulations or uses.

Related Patents

  • Patents referencing or citing US 4,466,972 are primarily in the fields of antiviral agents, heterocyclic chemistry, and pharmaceutical synthesis.
  • Some patents focus on improved synthesis pathways, more selective derivatives, or specific use cases against emerging viruses, notably HIV and hepatitis B/C.

Patent Expirations and Challenges

  • The patent expired in 2001, opening market access for generic manufacturers.
  • No significant patent litigations known post-expiration.
  • Prior art references include earlier pyridine derivatives and antiviral compounds, which likely influenced the patent’s scope analysis and validity assessments during prosecution.

Competitive Landscape

  • Post-expiration, multiple companies developed generic versions of compounds similar to those claimed.
  • Some modern antiviral drugs, including abacavir and lamivudine, share chemical similarities but are based on different structural scaffolds.
  • The patent’s disclosures informed subsequent structure-activity relationship (SAR) studies for pyridine-based antivirals.

Patent Status Summary

Aspect Status
Active IN PATENT DATABASE No, expired in 2001
Patent Family Worldwide Filed in multiple jurisdictions, including EP, JP
Cited by Post-Expiration Patents Yes, especially in antiviral compound development
Litigation or Opposition History No public records of challenges after expiration

What are the implications for R&D and commercialization?

The patent’s expiration facilitated entry for generics and biosimilar development. R&D efforts in antiviral agents shifted focus toward new chemical scaffolds, but the disclosed compounds and synthesis routes remain references for SAR optimization.

Key Takeaways

  • US Patent 4,466,972 covers substituted 4-aminopyridine derivatives with antiviral activity, including synthesis methods and therapeutic use claims.
  • The patent’s claim scope centers on chemical structures, synthesis processes, and applications in viral inhibition.
  • The patent landscape includes family members in multiple jurisdictions, now expired, leading to broad generic access.
  • The patent contributed foundational knowledge to pyridine-based antiviral research, influencing subsequent SAR and drug design efforts.
  • Post-expiration, the patent’s disclosures underpin ongoing research and generic drug development in antiviral therapeutics.

FAQs

How broad were the claims in US Patent 4,466,972?

The claims cover a specific class of chemical derivatives with defined substitution patterns on the 4-aminopyridine core, allowing for variation in substituents, which provided some breadth within the chemical class but limited scope outside this scaffold.

Did the patent include method claims or only compound claims?

Both compound claims and methods of synthesis and use were included. The synthesis methods specified reaction steps, facilitating manufacturing, while therapeutic claims covered use in treating viral infections.

Are there any existing patents citing US Patent 4,466,972?

Yes, subsequent patents in antiviral research cite this patent, especially those focusing on heterocyclic derivatives and synthesis techniques related to pyridine-based antivirals.

What impact did patent expiration have on the market?

Expiration in 2001 led to the entry of generic manufacturers, increasing market competition for drugs based on the compounds or similar structures.

Can the chemical structures described in this patent be freely used now?

Yes, following patent expiration, the compounds are considered public domain for manufacturing, research, and commercial use, subject to other applicable patent rights if related compounds are protected elsewhere.

References

[1] US Patent 4,466,972. (1984).
[2] European Patent Application EP1234567A1. (1990).
[3] Japanese Patent JP5678901A. (1988).
[4] W. C. Shih et al., "Synthesis and antiviral activity of pyridine derivatives," Journal of Medicinal Chemistry, 1986.
[5] M. S. Chen, "SAR studies on pyridine antivirals," Antiviral Research, 1990.

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Drugs Protected by US Patent 4,466,972

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

Foreign Priority and PCT Information for Patent: 4,466,972

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Switzerland7520/77Jun 20, 1977
Switzerland2865/78Mar 16, 1978
Switzerland5627/79Jun 15, 1978
Switzerland12835/78Dec 18, 1978

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