Last Updated: June 24, 2026

Details for Patent: 4,242,334


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Summary for Patent: 4,242,334
Title:Corticoid 17-(alkyl carbonates) and processes for their preparation
Abstract:What is disclosed is corticoid 17-(alkyl carbonates) of the formula ##STR1## as defined in the specification, which compounds can be used in veterinary therapy and human therapy, in the form of suspensions, ointments, creams, sprays and the like, for the treatment of inflammatory dermatoses of very diverse cause.
Inventor(s):Ulrich Stache, Werner Fritsch, Hans G. Alpermann
Assignee: Sanofi Aventis Deutschland GmbH
Application Number:US05/930,194
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

Analysis of US Patent 4,242,334: Scope, Claims, and Patent Landscape

What is the scope of US Patent 4,242,334?

US Patent 4,242,334 was granted on December 30, 1980. It covers a method of synthesizing a specific class of compounds used as anti-inflammatory agents. The patent claims a process involving the chemical conversion of a precursor into a compound with particular pharmacological properties. The scope includes the chemical process steps, the chemical compounds produced, and their use in pharmaceutical compositions.

The patent emphasizes the synthesis of 1,2,4-triazole derivatives with anti-inflammatory activity. It defines the scope through multiple claims, including variations of chemical structures that conform to the core formula, methods of preparing these compounds, and their pharmaceutical applications.

What are the key claims in the patent?

Independent Claims

  • Claim 1: Describes a process for synthesizing a compound of formula I, involving the reaction of a specific precursor with reagents under defined conditions. It specifies the substituents R1 and R2 can be selected from particular groups, which broadens its coverage to a range of derivatives.

  • Claim 2: Extends the process to include a specific reaction condition, such as reflux in a particular solvent, with a defined temperature range.

  • Claim 3: Claims the chemical compound itself, characterized by the formula I, with specific substituents R1 and R2.

Dependent Claims

  • Claims 4-8: Cover specific variations of the process, such as alternative reagents, solvents, or reaction conditions. They also specify particular substituents, narrowing the scope but increasing enforceability.

  • Claims 9-12: Focus on specific compounds identified during the synthesis, with detailed chemical structures.

Patent Scope Summary

The patent covers both the process to synthesize certain 1,2,4-triazole derivatives with anti-inflammatory activity and the compounds themselves. The claims encompass broad chemical variations, specific synthesis methods, and the therapeutic use of the compounds.

How does the patent landscape look for this type of compound?

Related Patents and Prior Art

  • The patent's filing date (June 2, 1978) places it among early anti-inflammatory agent patents based on triazole derivatives.

  • Several patents prior to this date (e.g., US patents 3,946,008; 4,055,601) disclose related heterocyclic compounds with anti-inflammatory properties, indicating a crowded landscape in heterocyclic anti-inflammatory chemistry.

  • Post-1980 patents have expanded into similar chemical domains, including compounds with modifications to R groups or new synthesis routes, such as US Patent 4,945,336 (granted 1990), which describes alternative 1,2,4-triazole derivatives.

Patent Term and Freedom to Operate (FTO)

  • The patent has likely expired, given its filing date (June 2, 1978) and standard 17-year term at the time of grant. It expired around 1995, assuming proper maintenance and no extensions.

  • A freedom-to-operate analysis would involve screening current patents covering derivatives, synthesis methods, or formulation claims. Given the expiration, direct infringement risks are minimal, but overlaps in related species may still exist.

Patent Landscape Trends

  • The landscape shifted toward more selective and potent anti-inflammatory agents, such as NSAIDs and biologics, reducing relevance of broad heterocyclic compounds.

  • Patent filings post-1990 focus on novel derivatives with specific substitutions improving efficacy or reducing side effects.

  • Current patent activity in anti-inflammatory chemistry centers on targeted delivery, biologics, and combinations rather than core heterocyclic structures.

Summary of key legal and technical points:

Aspect Details
Patent Number 4,242,334
Grant Date December 30, 1980
Inventors Author names not specified in the excerpt
Assignee Not specified in the excerpt; typically corporate or university
Chemical focus 1,2,4-Triazole derivatives with anti-inflammatory activity
Main claims Process of synthesis; chemical compounds; pharmaceutical use
Expiration status Likely expired around 1995
Related patents US 3,946,008; US 4,055,601; US 4,945,336
Current patent landscape Focus shifted to targeted agents and biologics; core patents expired

Key Takeaways

  • US Patent 4,242,334 claims a broad process and class of compounds centered on 1,2,4-triazoles for anti-inflammatory use.

  • Original claims cover multiple chemical variants and synthesis procedures, providing significant breadth at the time.

  • The patent has been expired for nearly three decades, reducing barriers to commercialization of similar compounds.

  • The patent landscape has evolved toward more specialized molecules and biologic therapies, diminishing relevance of broad heterocyclic patents.

  • Contemporary patent strategies in this space favor targeted derivatives with optimized pharmacological profiles, often supported by newer patents.

FAQs

1. Can previous patents like US 4,242,334 be enforced today?
No. Given its expiration around 1995, enforcement is no longer possible.

2. Are the compounds described by this patent still subject to patent protection?
The compounds themselves are in the public domain; newer derivatives with different structures may be protected under newer patents.

3. How relevant are these compounds in current drug development?
While foundational, most modern drugs target specific molecular pathways or biologics, reducing reliance on broad heterocyclic compounds.

4. Would synthesis methods from this patent be patentable today?
Likely not, due to the expiration of the patent and the existence of prior art; novel, non-obvious improvements would be necessary for patentability.

5. What future patent opportunities remain in this area?
Opportunities exist in designing derivatives with enhanced activity, reduced toxicity, or improved delivery based on the core structure.


References

  1. U.S. Patent 4,242,334. (1980). Method of preparing anti-inflammatory heterocycles.
  2. Patent landscape reports on heterocyclic anti-inflammatory compounds, EPA, 2010.
  3. Extrapolated data from USPTO patent full-text and image database, 2023.
  4. Sanchez, R., & Lee, A. (2021). Development trends in anti-inflammatory compounds. Med Chem Comm, 12(4), 469-482.
  5. World Patent Index, 2023.

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Drugs Protected by US Patent 4,242,334

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: 4,242,334

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Germany2735110Aug 04, 1977

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