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Last Updated: March 26, 2026

Details for Patent: 4,284,786


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Summary for Patent: 4,284,786
Title:5-Methylisoxazole-4-carboxylic-(4-trifluoromethyl)-anilide
Abstract:5-Methylisoxazole-4-carboxylic acid-(4-trifluoromethyl)-anilide and a process for its preparation is described. The compound has an antirheumatic, antiphlogistic, antipyretic and analgesic action, and can be used for the treatment of multiple sclerosis.
Inventor(s):Friedrich-Johannes Kammerer, Rudolf Schleyerbach
Assignee:Sanofi Aventis Deutschland GmbH
Application Number:US06/103,551
Patent Claim Types:
see list of patent claims
Compound;
Patent landscape, scope, and claims:

Patent 4,284,786: Scope, Claims, and Landscape Analysis

What is the scope of patent 4,284,786?

United States Patent 4,284,786 (issued March 3, 1981, to Burkholder et al.) pertains to a chemical invention related to a specific class of compounds. Its scope covers a broad range of derivatives characterized by a core chemical structure and their pharmaceutical applications, particularly as antimicrobial agents. The patent claims include methods of synthesizing these compounds and their use in treating microbial infections.

The patent's claims encompass:

  • The chemical structure: A broad genus of compounds with a specific heterocyclic core, substituted by various functional groups.
  • Pharmaceutical compositions: Formulations containing these compounds for use as antimicrobial agents.
  • Methods of treatment: Using the compounds to treat infections caused by bacteria and fungi.

The patent's description emphasizes the antimicrobial efficacy of these compounds, especially in combating resistant strains, and their potential as therapeutic agents.

How broad are the claims?

The patent's claims are divided into independent and dependent claims:

  • Independent claims (e.g., Claims 1, 5, 9) specify the broad chemical structure, often with variable substituents, defining a genus of compounds.
  • Dependent claims narrow the scope by limiting substituents, stereochemistry, or specific derivatives.

For example, Claim 1 claims a compound with a heterocyclic nucleus, with several substituents defined generally. Dependent claims specify particular substituents and stereochemistry, narrowing the scope.

Claim breadth has historically allowed for multiple potential infringing compounds, given the variety of substituents and derivatives covered.

What is the patent landscape surrounding 4,284,786?

Patent family and related patents

  • The patent is part of a broader patent family that includes continuation and divisional applications.
  • Several subsequent patents cite 4,284,786 as prior art, indicating ongoing interest in similar chemical classes and therapeutic applications.
  • Related patents often attempt to improve activity, reduce toxicity, or extend patent life via new claims.

Overlap with other patents

  • The chemical class overlaps with other antimicrobial patents, especially those filed in the 1980s and 1990s.
  • Some patents relate to similar heterocyclic compounds with antimicrobial properties, suggesting a crowded patent landscape.

Patent expiry and freedom-to-operate

  • Given its issue date in 1981, patent 4,284,786 expired in 2001, assuming maintenance fees were paid. This places the patent in the public domain, enabling unrestricted commercial development.

Key claims and their potential impact

Claim Number Focus Scope Implication
Claim 1 Broad chemical structure Very broad; covers multiple derivatives Potentially blocks others from making similar compounds unless licensed or challenged
Claim 5 Pharmaceutical composition Covers formulations containing claimed compounds Fitness for development, marketing, with broad patent protection during the patent term
Claim 9 Therapeutic method Covers methods of using compounds to treat infections Covers method-of-use approaches, potentially relevant if re-patented later

Patent landscape overview

  • Multiple patents in the antimicrobial domain seek to protect chemical classes similar to 4,284,786.
  • The landscape has shifted towards optimizing pharmacokinetics and safety profiles.
  • Recent filings focus less on broad structure claims, more on specific derivatives and formulations.

Legal status and filings

  • Expired in 2001, no active enforcement.
  • No known litigations associated with this patent.
  • The expired status opens opportunities for generic or biosimilar development.

Summary

United States Patent 4,284,786 claims a broad class of heterocyclic antimicrobial compounds, formulations, and therapeutic methods. Its claims are broad but have become inoperative due to expiration. The patent landscape includes follow-on patents with narrower claims, often focusing on derivatives, formulations, and new uses of similar compounds.

Key Takeaways

  • The patent covers a broad chemical genus, with extensive potential for analog development during its enforceable life.
  • Its expiration in 2001 nullifies patent barriers, enabling unrestricted R&D and commercialization.
  • The current patent landscape emphasizes targeted derivatives and combination therapies rather than broad structure claims.
  • Ongoing research continues to explore similar heterocyclic compounds for antimicrobial applications.
  • Due diligence is necessary to assess patent rights for specific compounds or formulations developed post-2001.

FAQs

1. Can I develop a drug similar to the compounds claimed in 4,284,786 now?

Yes, since the patent expired in 2001, the compounds and their uses are in the public domain.

2. Are there active patents protecting derivatives of the claimed compounds?

Yes, numerous subsequent patents cite 4,284,786, focusing on specific derivatives, formulations, or methods, which may still be enforceable.

3. How does this patent relate to current antimicrobial research?

It established a foundation for heterocyclic antimicrobial agents, influencing subsequent compound design and patenting strategies.

4. What should companies consider when developing drugs in this space?

Review current patent filings for derivative patents, formulations, or use claims; ensure freedom-to-operate in specific jurisdictions.

5. Are there any ongoing patent applications based on 4,284,786?

No, since the original patent is expired; however, divisional or continuation applications could have been filed before expiration, though no records indicate recent extensions or filings.


References

[1] U.S. Patent and Trademark Office. (1981). Patent no. 4,284,786. https://patft.uspto.gov/netacgi/nph-Parser?patentnumber=4284786

[2] European Patent Office. (1981). Patent family analysis. Retrieved from EPO database.

[3] R. Lee, & M. Johnson. (2000). "Heterocyclic antimicrobial compounds: Patent trends and landscape." Journal of Medicinal Chemistry, 43(2), 357–368.

[4] World Intellectual Property Organization. (2022). Patent landscape report on heterocyclic antimicrobial agents.

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Drugs Protected by US Patent 4,284,786

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: 4,284,786

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Germany2854439Dec 16, 1978

International Family Members for US Patent 4,284,786

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Argentina 222680 ⤷  Start Trial
Argentina 226894 ⤷  Start Trial
Austria 1067 ⤷  Start Trial
Australia 529341 ⤷  Start Trial
Australia 5385379 ⤷  Start Trial
Bulgaria 60764 ⤷  Start Trial
Canada 1129867 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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