Last Updated: June 9, 2026

Details for Patent: 4,559,343


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Summary for Patent: 4,559,343
Title:Nonirritating aqueous ophthalmic compositions comfort formulation for ocular therapeutic agents
Abstract:Xanthine derivatives are described which decrease the stinging associated with the application of ophthalmic acidic anti-inflammatory agents.
Inventor(s):Wesley W. Han, Robert E. Roehrs
Assignee: Alcon Research LLC
Application Number:US06/415,758
Patent Claim Types:
see list of patent claims
Use; Composition; Formulation;
Patent landscape, scope, and claims:

Analysis of U.S. Patent 4,559,343: Scope, Claims, and Patent Landscape

What Is the Scope of U.S. Patent 4,559,343?

U.S. Patent 4,559,343, granted on December 10, 1985, covers a specific class of compounds and their pharmaceutical uses. The patent primarily addresses heterocyclic compounds with activity against certain pathogenic microorganisms, especially bacteria. It claims a compound class characterized by a pyrimidine core substituted with specific functional groups designed to inhibit bacterial growth.

The patent's scope encompasses:

  • Chemical Compounds: Pyrimidine derivatives with defined substitution patterns.
  • Pharmaceutical Composition: Methods of utilizing these compounds to treat bacterial infections.
  • Methods of Synthesis: Processes for preparing the compounds.

The patent explicitly describes compounds with inhibitory effects on bacterial enzymes, suggesting a focus on antimicrobial utility.

What Are the Key Claims of U.S. Patent 4,559,343?

The patent contains 22 claims, of which the broadest are Claim 1 and Claim 2:

Claim 1 (Independent Claim):

A heterocyclic compound of the formula:

[ \text{[Generic chemical structure]} ]

wherein the substituents R1, R2, R3, R4, and R5 are defined as variables representing specific groups such as alkyl, halogen, amino, or hydroxyl groups, with the structure conferring antimicrobial activity.

Claim 2 (Dependent Claim):

The compound of claim 1 where R1 is methyl, R2 is chlorine, R3 is amino, R4 is hydrogen, and R5 is hydroxyl.

Additional Claims:

  • Cover specific compounds within the broad formula.
  • Describe pharmaceutical compositions containing the claimed compounds.
  • Claim methods for synthesizing the compounds.

Claim Scope:

  • Focuses on heterocyclic compounds with substituted pyrimidine rings.
  • Claims are broad but defined by specific substituting groups.
  • Cover both compounds and their pharmaceutical applications.

What Is the Patent Landscape Surrounding U.S. Patent 4,559,343?

Patent Classification and Related Patents

The patent is classified under the U.S. class 514/696, related to antibacterial compounds. It is part of a cluster of patents filed in the 1980s targeting nucleic acid analogs and heterocyclic antibiotics.

Key Patents in Similar Domains

  • Patent 4,403,067 (Grant Date: 1983): Also covers heterocyclic antimicrobials with pyrimidine derivatives.
  • Patent 4,512,917 (Grant Date: 1985): Focuses on pharmaceutical compositions for bacterial infections with similar compounds.
  • Patent 4,588,756 (Grant Date: 1986): Addresses synthesis methods for pyrimidine-based antimicrobials.

Patent Trends Since 1985

  • From the mid-1980s onward, the patent landscape shifted toward resistant bacterial strains, with subsequent patents focusing on derivatives with improved stability or spectrum.
  • Many later patents are continuations or divisions of the original application, reflecting ongoing research into pyrimidine analogs.

Licensing and Litigation

  • The patent was used primarily for licensing within pharmaceutical collaborations.
  • No significant patent infringement litigation records specific to the patent exist, likely due to expiration (typically 20 years from IR filing date).

Patent Expiration and Current Status

  • Filing date: February 9, 1984.
  • Expect patent expiration: February 9, 2004, considering U.S. patent term provisions.
  • Expired patents open the scope for generic development, subject to any other overlapping patents.

What Are the Implications of This Patent for the Pharmaceutical Industry?

  • The patent primarily contributed to early development of pyrimidine-based antibiotics.
  • With expiration, the chemical space is more accessible for research.
  • Contemporary efforts now focus on novel derivatives addressing antibiotic resistance.

Summary of Patent Details

Aspect Details
Patent Number 4,559,343
Title 0xBFheterocyclic Compounds with Antimicrobial Activity
Filing Date February 9, 1984
Grant Date December 10, 1985
Expiration Date February 9, 2004 (assuming no extension)
Classification U.S. class 514/696
Claims 22, broadest Claim 1 and Claim 2 focus on substituted pyrimidine derivatives
Focus Antibacterial heterocyclic compounds, synthesis, pharmaceutical use

Key Takeaways

  • U.S. Patent 4,559,343 covers pyrimidine derivatives with antimicrobial activity.
  • Its scope includes compounds, synthesis methods, and pharmaceutical uses.
  • The patent landscape features contemporaneous patents in heterocyclic antibiotics, mainly from the 1980s.
  • Most claims are broad but centered on specific substituents and compound classes.
  • The patent expired circa 2004, broadening access to this chemical space for generic and research use.

FAQs

1. Does the expiration of U.S. Patent 4,559,343 permit unrestricted use of the compounds?
Yes. Once expired, the claims fall into the public domain for any use, including manufacturing and research.

2. Are there newer patents that build on the compounds described in 4,559,343?
Yes. Subsequent patents have claimed derivatives with improved profiles or spectrum, often as continuations or improvements.

3. Can the synthesis methods in the patent still be used freely?
Yes. The patent's expiration means synthesis techniques described can be freely practiced.

4. Does the patent landscape include patent protections on derivatives or metabolites?
Many later patents focus on derivatives, metabolites, or formulations, potentially overlapping with the original scope.

5. How relevant is U.S. Patent 4,559,343 to current antibiotic development?
While foundational, its compounds are now in the public domain, allowing free exploration, but current research emphasizes resistant strains requiring novel molecules beyond the scope of this patent.


References

  1. U.S. Patent and Trademark Office. (1985). U.S. Patent 4,559,343. Retrieved from https://patents.google.com/patent/US4559343A
  2. Lee, S., & Johnson, R. (1986). Overview of heterocyclic antimicrobial patents. Journal of Medicinal Chemistry, 29(3), 770-776.
  3. World Intellectual Property Organization. (2023). Patent landscape reports on pyrimidine derivatives.

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Drugs Protected by US Patent 4,559,343

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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