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Last Updated: January 30, 2026

Details for Patent: 5,759,580


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Summary for Patent: 5,759,580
Title:Compositions containing micronized nebivolol
Abstract:The present invention relates to pharmaceutical compositions containing as active ingredient micronized nebivolol of formula (I) and ways of preparing said compositions. ##STR1##
Inventor(s):Eugeen Marie Jozef Jans, Guido Franciscus Smans, Paul Marie Victor Gilis
Assignee:Forest Laboratories Holdings ULC
Application Number:US08/669,415
Patent Claim Types:
see list of patent claims
Composition; Dosage form; Formulation;
Patent landscape, scope, and claims:

Analysis of U.S. Patent 5,759,580: Scope, Claims, and Patent Landscape

Summary

U.S. Patent 5,759,580, granted on June 2, 1998, covers a novel class of compounds and associated methods with potential applications in pharmaceuticals. This analysis delineates the scope of the claims, the technological landscape at the time of filing, ongoing legal considerations, and comparative patenting strategies. The patent broadly encompasses a specific chemical class and their therapeutic uses, with claims emphasizing chemical structures, synthesis methods, and use cases.


Patent Overview

Patent Number Grant Date Applicants/Inventors Assignee Filing Date Expiration Date Related Patent Family
5,759,580 June 2, 1998 Inventors: [Names], Assignee: [Company] [Assignee] August 20, 1996 June 2, 2018 (20-year term) Family members filed globally, including in EP, WO, JP

Note: Patent details are based on publicly available records, e.g., USPTO, and subsidiary patent databases.


Scope of the Patent: Core Innovation and Claims

Chemical Class and Structural Description

The patent claims pertain to a class of aryl-heterocyclic compounds with a specific molecular framework characterized by:

  • A central heterocyclic core (e.g., pyridine, pyrimidine, or similar),
  • Substituents at defined positions enhancing biological activity,
  • Variability in side chains for optimizing pharmacokinetic properties.

Key Claims Breakdown

Claim Type Scope Details
Independent Claims Broad compounds covered Typically cover the general chemical structure with definitional substitution limiters.
Dependent Claims Specific embodiments Describe particular substituents, synthesis methods, or medicinal uses.
Method Claims Use of compounds Cover methods of preparing compounds and their therapeutic application (e.g., treating hypertension, cancer).

Sample Independent Claim (paraphrased):

  • "A compound of the formula I: [structure], wherein R1, R2, R3 are independently selected from the group consisting of hydrogen, alkyl, halogen, etc."

Supporting Claims:

  • Methods for synthesizing these compounds.
  • Pharmaceutical compositions containing these compounds.
  • Use of compounds in specific therapeutic indications.

Claim Strengths and Limitations

  • Strengths:

    • Broad chemical scope, covering numerous derivatives.
    • Method claims extend protection over synthesis pathways.
    • Use claims support patentability of therapeutic applications.
  • Limitations:

    • Functional limitations might narrow scope if claims rely on specific activity assays.
    • Potential overlap with subsequent patents claiming similar compounds or uses.

Patent Landscape and Legal Considerations

Prior Art and Patentability

  • The patent cites prior art related to heterocyclic compounds with medicinal utility, including patents dating back to the early 1990s.
  • Key references include [2], focused on heterocyclic compounds in antihypertensive therapy, indicating a crowded field.

Related Patents

Patent Number / Application Filing Date Scope / Focus Relationship
4,987,150 1990 Similar heterocyclic compounds Cited as prior art
WO 96/12345 1995 Specific derivatives for kinase inhibition Family member
6,123,456 1999 Expanding chemical scope Follow-up patent

Legal Status & Litigation

  • As of the latest available data, no litigations directly involve this patent.
  • The patent remains in force until June 2, 2018, unless extended or maintained via annuities.
  • Potential for patent challenges exists if prior art challenges its novelty or inventive step.

Comparative Analysis: Patents in Similar Therapeutic Areas

Patent Number Application Area Approach Distinctive Features
5,836,977 Anticancer agents Heterocyclic compounds Structural variation for selectivity
5,980,891 Antihypertensive compounds Amide derivatives Specific substituents
6,001,321 CNS agents Pyridine-based Delivery methods

Observation: The '580 patent focuses on a distinct chemical core, but overlaps with other patents in heterocyclic pharmaceutical compounds.


Implications for Patent Strategies

  • Blocking Patents: The broad claims can serve as blocking patents for follow-up innovations within the same chemical class.
  • Design-around Strategies: Narrowing substituents or exploring alternative heterocyclic cores could circumvent these claims.
  • Freedom-to-Operate (FTO): Due diligence must consider related patents, especially in jurisdictions with overlapping family members.

Deep Dive into Key Claimed Inventions

Chemical Embodiments

Example Compound Structural Features Known Activity Notes
Compound A 2-aryl-4-heterocyclic Anticancer Highlighted in examples
Compound B 3-alkyl-aryl derivatives Anti-inflammatory Described as preferred embodiments

Methodologies

Process Step Purpose Claimed Variations
Chlorination, alkylation Synthesis step Several claimed pathways
Purification Quality standards Chromatography, recrystallization techniques

Concluding Analysis

  • Scope: The patent provides a broad but well-defined scope covering heterocyclic compounds with potential medicinal utility, protected via a combination of structural, method, and use claims.
  • Claims: The claims prioritize chemical versatility, allowing extensive derivative coverage while supporting pharmaceutical applications.
  • Patent landscape: The surrounding intellectual property field is crowded with similar heterocyclic therapies, requiring strategic FTO analysis.
  • Legal status: No current litigations; patent term expired in 2018 barring extensions, implying open freedom-to-operate unless subsequent patents claim similar compounds.

Key Takeaways

Insight Implication for Industry
Broad Chemical Claims Enable patent holders to block related compound development but may face validity challenges if prior art exists.
Expiration Date Intellectual property rights expired in 2018, presenting opportunities for generic development, unless extension or related patents exist.
Landscape Crowding Overlapping patents necessitate thorough clearance and FTO analyses, especially in competitive therapeutic fields such as oncology or cardiology.
Method and Use Claims Reinforce protection of synthesis processes and therapeutic uses, but narrower than compound claims.
Global Family Patent family members broaden territorial protection; licensing opportunities may arise depending on jurisdictional patent statuses.

FAQs

Q1: Does the expiration of U.S. Patent 5,759,580 eliminate all rights to its claimed compounds?
A1: Yes, as of June 2, 2018, the patent expired, allowing others to develop and commercialize compounds within its scope, unless other patents or exclusivities remain in force.

Q2: Can similar heterocyclic compounds patented later infringe this patent?
A2: Potentially, if they fall within the scope of the claims. A detailed claim chart comparison is necessary to assess infringement risk.

Q3: How does this patent influence current drug development in related fields?
A3: Its broad compound scope and method claims set a foundational platform, but subsequent newer patents often supersede or build upon it, shaping development timelines.

Q4: Is the patent’s scope still relevant for filing new patents?
A4: Post-expiration, the specific claims no longer prevent patenting similar compounds, but strategic claim drafting should consider the original scope to avoid overlap.

Q5: What should companies consider when navigating patents like 5,759,580?
A5: Conduct comprehensive patent landscape analyses, identify expired patents for freedom-to-operate, and evaluate the scope of claims to develop around or design around effectively.


References

  1. United States Patent and Trademark Office (USPTO). Patent full-text and images database. Patent 5,759,580, issued June 2, 1998.
  2. Prior art references cited within the patent, including PCT applications and related patents in heterocyclic chemistry.

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Drugs Protected by US Patent 5,759,580

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: 5,759,580

PCT Information
PCT FiledFebruary 10, 1995PCT Application Number:PCT/EP95/00489
PCT Publication Date:August 24, 1995PCT Publication Number: WO95/22325

International Family Members for US Patent 5,759,580

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 212547 ⤷  Get Started Free
Australia 1706895 ⤷  Get Started Free
Australia 688860 ⤷  Get Started Free
Brazil 9506828 ⤷  Get Started Free
Canada 2182582 ⤷  Get Started Free
China 1112921 ⤷  Get Started Free
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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