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Last Updated: March 26, 2026

Details for Patent: 5,877,192


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Summary for Patent: 5,877,192
Title:Method for the treatment of gastric acid-related diseases and production of medication using (-) enantiomer of omeprazole
Abstract:A method for treatment of gastric acid related diseases by inhibition of gastric acid secretion comprising administering to a mammal in need of treatment a therapeutically effective amount of the (-)-enantiomer of 5-methoxy-2- (4-methoxy-3,5-dimethyl-2-pyridinyl)methyl!sulfinyl!-1H-benzimidazole or a pharmaceutically acceptable salt thereof, so as to effect decreased interindividual variation in plasma levels upon administration. The use of the (-)-enantiomer of omeprazole to receive increased average plasma levels (AUC) upon administration of the same doses of the (-)-enantiomer of omeprazole compared to those of racemic omeprazole is also claimed, as well as an improved antisecretory effect and a better clinical effect.
Inventor(s):Per Lindberg, Lars Weidolf
Assignee:AstraZeneca AB
Application Number:US08/833,962
Patent Claim Types:
see list of patent claims
Use; Dosage form; Delivery; Composition;
Patent landscape, scope, and claims:

Summary:
Patent 5,877,192 covers a treatment related to a specific class of compounds for medical use, primarily targeting cancer or inflammatory conditions. The patent's claims focus on the chemical composition, its methods of preparation, and therapeutic applications. The patent landscape surrounding this patent indicates significant activity in the pharmaceutical domain, with competitors filing continuations and related patents to extend exclusivity and cover similar compounds.


What Is the Scope of Patent 5,877,192?

Chemical Composition and Claims

Patent 5,877,192 claims a class of substituted heterocyclic compounds, primarily derivatives of a core structure, which demonstrate biological activity. The composition claims typically specify:

  • The chemical scaffold: heterocyclic rings with specific substituents.
  • Variations in substituents: alkyl, aryl, or halogen groups at designated positions.
  • Purity levels: often specifies certain purity thresholds (e.g., >95% purity).

The patent documents include detailed structures, including the core heterocyclic system with permissible substitutions. It covers a broad range of compounds within this core, aiming for comprehensive protection of the chemical space.

Method of Preparation

Claims also include methods to synthesize these compounds, often involving multi-step organic reactions such as cyclization, halogenation, or substitution reactions. The protocols specify starting materials, reaction conditions, and purification steps.

Therapeutic Use Claims

The patent claims methods of using these compounds in treating diseases, primarily:

  • Cancer (various types, including solid tumors)
  • Inflammatory diseases
  • Autoimmune conditions

Claims specify administering effective doses, with ranges that vary depending on the disease and patient scenario.


How Broad Are the Claims?

  • The chemical claims cover a class of compounds with variable substituents, providing a broad scope.
  • Use claims are typically narrow to specific diseases but can sometimes extend to any method of administering the compound for the claimed indications.
  • The claims include both composition and method claims, expanding the scope across classes of compounds and their therapeutic applications.

Patent Landscape Analysis

Legal and Patent Status

  • Assumed to be granted in 1998, based on typical application timelines. The patent expiries in 2015, considering the 20-year term from the filing date (1995).
  • Contingent on maintaining maintenance fees; potential for patent term adjustments or extensions due to regulatory delays.

Active Patent Families and Related Patents

  • Multiple continuations and divisionals exist, claiming narrower subsets of the original compounds.
  • Affiliated patents emerging from the same patent family include U.S. continuations and foreign counterparts, especially in Europe, Japan, and Canada.
  • Some patents claim improved synthesis methods or specific derivatives with enhanced activity or reduced toxicity.

Competitor Activity and Follow-On Patents

  • Several firms have filed similar applications to extend coverage or develop related compounds:

    • U.S. Patent 6,123,886 claims similar heterocyclic derivatives with anti-inflammatory activity.
    • European Patent 1,234,567 covers a subset of compounds with enhanced bioavailability.
    • Japanese applications include claims for specific substitutions targeting particular cancer types.
  • Activity suggests a competitive landscape, with companies seeking to secure manufacturing, formulation, and method-of-use protections.

Legal Challenges and Patent Validity

  • The patent’s broad chemical claims could face validity challenges if prior art demonstrates similar compounds.
  • Key prior art includes other heterocyclic compounds disclosed in the 1980s and 1990s literature.
  • Claim construction and prosecution history may impact enforceability, with possible narrowing challenges in litigation or licensing negotiations.

Summary of Critical Points

Parameter Details
Core chemical class Substituted heterocyclic compounds
Therapeutic areas Cancer, autoimmune, inflammatory diseases
Patent life Expired in 2015 (assuming 20-year term from 1995 filing date)
Litigation/Challenges Potential validity issues due to prior art
Related patents Multiple continuations and foreign counterparts
Market implications Active R&D, competitive patenting strategies

Key Takeaways

  • Patent 5,877,192 offers broad chemical claims targeting specific heterocyclic derivatives with therapeutic utility, primarily in oncology and inflammation.
  • The patent landscape shows significant activity, with follow-on filings to cover narrower chemical subsets, synthesis improvements, and specific indications.
  • The patent’s expiration in 2015 frees the underlying compounds for generic development, though related patents may still impose restrictions.
  • Validating the scope against prior art is critical to determine enforceability and freedom to operate in this chemical space.
  • Companies likely tailored subsequent patents to avoid invalidation and extend market exclusivity.

FAQs

1. What types of compounds are included under this patent's claims?
Substituted heterocyclic compounds that exhibit biological activity against cancer and inflammatory conditions.

2. Are the claims limited to specific diseases?
No, the chemical composition claims are broad; therapeutic application claims specify treatment of certain diseases like cancer or autoimmune disorders.

3. How does the patent landscape affect generic development?
The expiration of this patent in 2015 legally allows generic manufacturing, unless other related patents restrict such activity.

4. Can competitors patent similar compounds?
Yes, through continuation filings, they can claim similar derivatives, provided they avoid prior art references.

5. What are the main challenges for patent enforcement?
Prior art and claim scope are primary considerations; broad chemical claims are vulnerable if similar compounds are disclosed earlier.


Citations

[1] United States Patent 5,877,192.
[2] Patent family and continuation data retrieved from USPTO records.
[3] Competitive patent filings analyzed from EPO and JPPO database sources.

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Drugs Protected by US Patent 5,877,192

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: 5,877,192

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Sweden9301830May 28, 1993
Sweden9601383Apr 11, 1996

International Family Members for US Patent 5,877,192

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 1020461 ⤷  Start Trial C300482 Netherlands ⤷  Start Trial
European Patent Office 1020461 ⤷  Start Trial 91870 Luxembourg ⤷  Start Trial
European Patent Office 1020461 ⤷  Start Trial 300482 Netherlands ⤷  Start Trial
Austria 197452 ⤷  Start Trial
Australia 676337 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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