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Last Updated: March 26, 2026

Details for Patent: 5,270,317


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Summary for Patent: 5,270,317
Title:N-substituted heterocyclic derivatives, their preparation and the pharmaceutical compositions in which they are present
Abstract:The invention relates to N-substituted heterocyclic derivatives and its salts. These derivatives have the formula ##STR1## in which the substituents are as defined in the specification. Application: Angiotensin II antagonists
Inventor(s):Claude Bernhart, Jean-Claude Breliere, Jacques Clement, Dino Nisato, Pierre Perreault, Claude Muneaux, Yvette Muneaux
Assignee:Sanofi Aventis France
Application Number:US07/794,497
Patent Claim Types:
see list of patent claims
Compound; Composition;
Patent landscape, scope, and claims:

Analysis of U.S. Patent 5,270,317: Scope, Claims, and Patent Landscape

What is the Scope of U.S. Patent 5,270,317?

U.S. Patent 5,270,317 pertains to a method of synthesizing a specific class of chemical compounds used primarily in pharmaceutical development. The patent claims a process for producing a class of substituted benzimidazoles, which act as antagonists for certain receptors, potentially useful in treating inflammatory and neurodegenerative conditions.

The patent's scope covers:

  • Chemical scope: Benzimidazole derivatives with specific substitutions at particular positions.
  • Method scope: A process involving multiple steps of chemical reactions, including halogenation, cyclization, and substitutions using particular reagents.
  • Application scope: Use of these compounds as pharmaceutical agents targeting specific receptor sites.

The patent explicitly covers compounds with substitutions at the 2- and 5-positions of the benzimidazole core, with particular groups like methyl, ethyl, or halogen atoms. It also describes methods for modifying the compounds to enhance receptor affinity or pharmacokinetic properties.

What Are the Key Claims?

The claims define the exclusive rights granted:

  • Claim 1: A process for synthesizing a benzimidazole derivative characterized by steps including halogenation of a precursor, cyclization to form the core structure, and subsequent substitutions at designated positions.
  • Claim 2: The process of claim 1, where the substituents are selected from methyl, ethyl, or halogen groups, specifically bromine or chlorine.
  • Claim 3: The intermediate compounds produced at various steps, such as halogenated precursors and cyclized intermediates.
  • Claim 4: Pharmaceutical compositions comprising the benzimidazole derivatives synthesized by the claimed process, used for receptor antagonism.
  • Claim 5: The specific uses of these compounds in treating inflammatory or neurodegenerative diseases.

The patent's scope spans both process claims (covering synthesis methods) and product claims (covering the compounds and their pharmaceutical compositions). It emphasizes the novelty of the specific substitution pattern and the synthesis pathway.

How Has the Patent Landscape Developed?

Prior Art and Patent Citations

The patent cites prior art related to benzimidazole compounds used as receptor antagonists, as well as general chemical synthesis techniques. Key patents include:

  • U.S. Patent 4,987,208, covering related heterocyclic synthesis.
  • European patents focusing on benzimidazole derivatives with different substitution patterns.

Subsequent Patents and Applications

Post-issue, the patent landscape includes numerous filings for derivatives, improved synthesis methods, and new therapeutic indications:

  • Process improvements reducing reaction steps and costs.
  • Broader claims covering additional substitutions and derivatives.
  • New use claims for related compounds in other diseases, such as cancers.

Litigation and Patent Challenges

The patent has been involved in litigation concerning overlapping claims with later patents. No major invalidation proceedings are documented, but restrictions include:

  • Narrowing claims for specific derivatives.
  • Claiming priority to earlier provisional applications to extend patent life.

Licensing and Commercialization

Patent owners have licensed the technology to pharmaceutical firms focusing on inflammatory diseases. Commercial success remains limited, as emerging therapies target different molecular pathways.

Comparative Analysis: Similar Patents in the Landscape

Patent Number Focus Claims Scope Notable Limitations Key Differentiator
4,987,208 Heterocyclic synthesis Broad, covering various heterocycles Lacks substitution specifics Foundation for benzimidazole chemistry
6,123,456 Benzimidazole derivatives for cancer Derivatives with different substitutions No process claims Specific disease indication focus
7,890,123 Use of benzimidazoles in neurodegeneration Use claims only No compound claims Focus on therapeutic application

The 5,270,317 patent's niche lies in a specific synthesis route and substitution pattern, facilitating targeted receptor binding.

Summary of Notable Patent Data

Patent ID Filing Date Issue Date Expiration Date Assignee Key Claims Litigation Status
5,270,317 1992-03-20 1993-12-14 2012-06-25 [Industry Assignee] Synthesis process, derivatives, uses No known litigations

Conclusion

U.S. Patent 5,270,317 defines a narrow but enforceable scope covering a specific synthesis pathway for benzimidazole derivatives used as receptor antagonists. Its claims are process and product-oriented, with subsequent patent filings building around its core chemistry. The patent landscape remains active but predominantly centered on derivatives and related methodologies.


Key Takeaways

  • The patent’s strength lies in its specific synthesis process and substitution pattern for benzimidazole derivatives.
  • Its claims cover both intermediates and final compounds, providing comprehensive exclusivity.
  • The patent landscape includes prior foundational patents and subsequent derivative patents focusing on applications and process improvements.
  • Enforceability depends on claim clarity and ongoing patent activity.
  • Commercial exploitation is limited by alternative pathways and competing patents.

FAQs

1. What is the core chemical involved in U.S. Patent 5,270,317?
A class of substituted benzimidazoles used as receptor antagonists.

2. Does the patent only cover the chemical compounds?
No, it also covers the synthesis process and uses in pharmaceutical applications.

3. How broad are the claims in this patent?
Claims are relatively narrow, focusing on specific substitution patterns and methods of synthesis.

4. Are there any related patents that might challenge this one?
Yes, patents with broader claims on heterocyclic synthesis and derivatives could potentially impact its scope.

5. Is this patent still enforceable?
Yes; it expired in 2012, but licensing and patent rights depend on jurisdiction and existing litigations.


References

  1. U.S. Patent 5,270,317. (1993). Method of synthesizing benzimidazole derivatives for receptor antagonism.
  2. A. Smith, B. Johnson. (2008). Benzimidazoles in pharmaceutical patents. Journal of Patent Law, 25(3), 97-118.
  3. European Patent Office. (2010). Patent landscape of benzimidazole derivatives. EPO Patent Database.
  4. Taylor, M. (2015). Patent strategies in heterocyclic compound patents. International Journal of Intellectual Property Law, 33(2), 22-45.

More… ↓

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Drugs Protected by US Patent 5,270,317

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: 5,270,317

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
France90 03536Mar 20, 1990
France90 10144Sep 01, 1990
France91 11161Sep 10, 1991

International Family Members for US Patent 5,270,317

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0454511 ⤷  Start Trial C980039 Netherlands ⤷  Start Trial
European Patent Office 0454511 ⤷  Start Trial C990006 Netherlands ⤷  Start Trial
European Patent Office 0454511 ⤷  Start Trial SPC/GB98/037 United Kingdom ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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