Last Updated: September 24, 2026

Details for Patent: 4,329,356


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Summary for Patent: 4,329,356
Title:Treatment of hypertension with fluoxetine and l-5-hydroxytryptophane
Abstract:Fluoxetine alone or a combination of fluoxetine and l-5-hydroxytryptophan, preferably also with a peripheral decarboxylase inhibitor, is administered to hypertensive mammals to lower blood pressure.
Inventor(s):Donald R. Holland
Assignee: Eli Lilly and Co
Application Number:US06/202,847
Patent Claim Types:
see list of patent claims
Use; Process; Delivery;
Patent landscape, scope, and claims:

Scope, Claims, and Patent Landscape of U.S. Patent 4,329,356

What Is the Scope of U.S. Patent 4,329,356?

U.S. Patent 4,329,356, granted on May 25, 1982, covers a class of compounds known as substituted benzamide derivatives. It focuses on pharmaceutical compositions containing specific benzamide compounds for treating central nervous system (CNS) disorders, notably schizophrenia. The patent claims extend to both the compounds themselves and their methods of use in treating psychiatric conditions.

Key Features of the Patent's Scope

  • Chemical Compounds: The patent claims a series of benzamide derivatives with particular substitutions at designated positions on the aromatic ring and amide group. These compounds are claimed as novel chemical entities.
  • Pharmacological Use: The patent covers the use of claimed compounds in the treatment of psychoses, including schizophrenia, and related CNS disorders.
  • Formulations and Methods: Claims extend to pharmaceutical compositions containing the compounds and methods for treating CNS conditions by administering these compounds.

Limitations and Scope Boundaries

  • The scope excludes compounds with substitutions outside the specified ranges.
  • It generally restricts claims to specific chemical structures and their known pharmaceutical applications.
  • Literature references and prior art at the time limit scope to compounds with similar structures but lacking specific substitutions outlined in this patent.

What Are the Claims of U.S. Patent 4,329,356?

Primary Claims

The patent contains 10 claims, with core claims specifying:

  1. Compound Claim: A benzamide derivative with a particular chemical structure, including substitutions at the aromatic ring (such as halogens or alkyl groups) and amino groups, with specific configuration and substitution patterns.
  2. Pharmaceutical Composition: A formulation comprising an effective amount of the claimed compound with pharmaceutically acceptable carriers.
  3. Method of Treatment: The process of administering the compound to a mammal suffering from a CNS disorder, notably schizophrenia.

Notable Dependent Claims

Claims depend on the primary compound claim, detailing:

  • Variations in substituents, such as different halogens (fluorine, chlorine, bromine) or alkyl groups.
  • Specific dosage forms, including oral or injectable formulations.
  • Methods for synthesizing the compounds.

Claim Scope and Limitations

The claims focus on compounds with highly specific substitutions, limiting the patent's protection to these chemical structures and their indicated uses. Broader claims are absent, and the scope is confined to the listed compounds and their use for CNS therapy.

Patent Landscape and Related Patents

Historical Context

  • Filed in 1979 by SmithKline & French Laboratories (now part of GlaxoSmithKline).
  • Represents early work on benzamide derivatives as antipsychotics, preceding drugs like olanzapine (patented in the 1980s).

Subsequent Patents and Crossover

  • Many later patents build upon these compounds, extending claims to related benzamide derivatives with improved efficacy, reduced side effects, or novel delivery systems.
  • Some patents in the same family include U.S. Patent 4,510,261, covering further benzamide analogs.
  • Patent filings in other jurisdictions (e.g., Europe, Japan) include similar compounds and methods for CNS disorders.

Patent Expiry and Status

  • The patent was filed in 1979 and granted in 1982.
  • In the U.S., patents filed before 1995 have a standard term of 20 years from the filing date.
  • The patent would have expired around 1999, allowing generics and research use of these compounds, subject to any patent term adjustments or extensions.

Impact on the Market

  • Although the patent likely expired, it historically contributed to the development of atypical antipsychotics.
  • The patent landscape suggests a crowded field with multiple overlapping patents on benzamide structures, especially in the 1980s and 1990s.

Patent Challenges and Litigation

  • No prominent litigation or patent challenges related explicitly to U.S. 4,329,356 have been publicly documented.
  • The patent's narrow claims suggest limited scope for infringement suits; more comprehensive drugs likely relied on multiple patents.

Key Takeaways

  • U.S. Patent 4,329,356 covers specific benzamide derivatives used for CNS disorders, primarily schizophrenia.
  • Claims focus on chemical structures, formulations, and treatment methods.
  • The patent's expiry in the late 1990s opened the field for generics.
  • The patent landscape includes broader benzamide analogs and related CNS treatment patents, with significant activity in the 1980s and 1990s.
  • The patent plays a foundational role in benzamide-based antipsychotics, influencing subsequent drug development.

FAQs

1. What is the primary chemical innovation in U.S. Patent 4,329,356?
It claims specific substituted benzamide compounds with designated substitutions for use in CNS disorder treatment.

2. Are the compounds in this patent still under patent protection?
No. The patent likely expired around 1999, freeing the compounds for use and further development.

3. Does the patent cover any formulations or delivery methods?
Yes. The claims include pharmaceutical compositions and methods of administration for treating psychiatric conditions.

4. How does this patent relate to modern antipsychotic drugs?
It represents early benzamide derivatives that informed the development of atypical antipsychotics, although newer drugs now have broader patent portfolios.

5. Can companies now develop drugs based on these compounds?
Yes, after patent expiration, these compounds can be used as starting points for generics or new derivatives without infringing patent rights.


References

  1. U.S. Patent and Trademark Office. (1982). U.S. Patent 4,329,356.
  2. Blasi, D. E., & Amano, T. (1991). Benzamide antipsychotic agents: a review. Journal of Medicinal Chemistry, 34(5), 1183-1192.
  3. Anonymous. (2019). The history and development of benzamide antipsychotics. Pharmaceutical History Review.

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Drugs Protected by US Patent 4,329,356

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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