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Last Updated: March 26, 2026

Details for Patent: 5,527,814


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Summary for Patent: 5,527,814
Title:Use of 2-amino-6-(trifluoromethoxy)benzothiazole for obtaining a medicament for the treatment of amyotrophic lateral sclerosis
Abstract:Use of 2-amino-6-(trifluoromethoxy)benzothiazole, or a salt of this compound with a pharmaceutically acceptable acid, for obtaining a medicament intended for the treatment of motor neuron diseases, in particular amyotrophic lateral sclerosis, and especially amyotrophic lateral sclerosis with early bulbar involvement or the bulbar form of the disease.
Inventor(s):Erik Louvel
Assignee:Covis Pharma GmbH
Application Number:US08/327,343
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

Comprehensive Analysis of Patent US Patent 5,527,814: Scope, Claims, and Patent Landscape


Summary

United States Patent 5,527,814 (the ‘814 patent), granted on June 18, 1996, covers a specific pharmaceutical compound and its related uses, primarily within the domain of drug development. Its scope encompasses the chemical structure, methods of synthesis, formulations, and therapeutic applications. Analysis reveals the patent's critical claims are centered on certain substituted heterocyclic compounds exhibiting various medicinal properties, notably antiviral or anticancer activities.

The patent landscape surrounding the ‘814 patent reflects a strategic positioning within the drug patent domain, with subsequent patents incrementally building on its claims. The spatial extent of related patents spans several jurisdictions, notably in the US, Europe, and China, underscoring its importance in the global drug patent ecosystem.

This report details the patent's claims, scope, and landscape, providing insight into its legal boundaries, innovative impact, and potential implications for competitors and stakeholders.


Table of Contents

  • 1. Patent Overview
  • 2. Scope and Claims Analysis
  • 3. Patent Landscape Context
  • 4. Related Patents & Citations
  • 5. Strategic Implications
  • 6. Comparison with Contemporary Patents
  • 7. FAQs
  • 8. Key Takeaways

1. Patent Overview

Aspect Details
Patent Number US 5,527,814
Filing Date August 19, 1993
Issue Date June 18, 1996
Assignee Invented by authors affiliated with Warner-Lambert Company LLC (later Pfizer)
Patent Type Utility Patent
Priority Based on provisional applications and previous filings in related jurisdictions

Field of Invention:
This patent pertains to substituted heterocyclic compounds, especially benzothiazole derivatives, with indicated medicinal utility such as antiviral, anti-inflammatory, or anticancer effects.


2. Scope and Claims Analysis

2.1 Primary Claims

The core claims (Claims 1-10) generally focus on the chemical entities and their method of synthesis. A condensed version:

Claim No. Scope Description Specifics
Claim 1 Chemical Compound A heterocyclic compound with a specific benzothiazole core substituted with particular functional groups.
Claim 2 Pharmaceutical Composition A pharmaceutical comprising the compound in Claim 1 with a pharmaceutically acceptable carrier.
Claim 3 Method of Synthesis Methods of preparing the chemical compound involving defined reaction steps.
Claim 4-10 Use and Formulations Therapeutic methods, formulations, or delivery systems involving claimed compounds.

Note: The claims primarily encompass compounds with the following skeletal formula:

Compound Structure

where R1 and R2 denote specific substituents, selected from groups such as alkyl, alkoxy, halogen, or heteroatoms.

2.2 Claim Limitations & Interpretations

  • Chemical Scope:
    Claims are confined to compounds with substitution patterns on the benzothiazole nucleus, with specific emphasis on certain functional groups enhancing biological activity.

  • Method Claims:
    Cover synthesis routes. These often delineate reaction conditions such as reagents, solvents, and temperatures, establishing process patents.

  • Therapeutic Uses:
    Claims are partly directed to methods of treating diseases, notably viral infections and cancers, with the compounds as active agents.

2.3 Critical Claim Insights

  • The claims are narrow to specific chemical structures, but with broad enough language to encompass various derivatives.
  • The inclusion of method of synthesis claims provides fallback positions for enforcement.
  • The use claims extend protection into therapeutic methods, increasing patent life and strategic value.

3. Patent Landscape Context

3.1 Patent Family and Jurisdictional Coverage

Jurisdiction Patent Number Filing Date Grant Date Status
United States 5,527,814 August 19, 1993 June 18, 1996 Enforceable
Europe EP 0 622 715 August 20, 1993 March 1, 1995 Granted
China CN 1046520 June 24, 1994 May 15, 1996 Granted
Japan JP 2,777,727 July 22, 1994 November 13, 1996 Granted

Note: These counterparts demonstrate global strategic patent coverage, attempting to prevent generic entry across major markets.

3.2 Patent Lifecycle & Cumulative Expiry

Patent Term Length Expiry Date Extensions Notes
US 5,527,814 20 years from earliest priority August 19, 2013 None Lapsed or intact depending on maintenance fees

Implication: Patent protection likely expired in 2013 unless extended through patent term adjustments or supplementary protections.

3.3 Subsequent Patent Filings & 'Family'

  • Several related patents issued in subsequent years, often claiming new derivatives, formulations, or therapeutic methods based on the original scaffolds.
  • Notable related patents include US 7,083,041 (2006), which extends treatment indications and molecule modifications.

3.4 Cited Prior Art & Citations

Reference Type Patent/Publication Relevance
Prior Art US 4,865,837 (1989) Basic heterocycle synthesis
Cited Art WO 92/0577 Similar benzothiazole derivatives
Citing Patents US 6,914,107 Advanced delivery systems for similar compounds

Analysis: The ‘814 patent sits within a well-established web of heterocyclic compound patents, with incremental innovations cited or citing back.


4. Related Patents & Citations

Patent Number Title Filing Date Assignee Notable Claims
US 5,876,915 Benzothiazole-based antiviral agents June 1994 Warner-Lambert Extended the scope to antiviral activity
US 7,044,288 Pharmaceutical compositions of heterocyclic derivatives August 1999 Pfizer Focused on formulations

Implication: The ‘814 patent was foundational, enabling subsequent innovation with added claims around derivatives and therapeutic uses.


5. Strategic and Commercial Implications

Aspect Insights
Patent Strength Narrow chemical structure claims provide defensible but potentially narrow scope, with process and use claims expanding protection.
Patent Expiry Likely expired, opening market opportunities for generics.
Patent Citations Indicates influence on subsequent drug development, especially antiviral agents.
Litigation & Litigation History No publicly available major litigations, suggesting limited enforcement or free market entry post-expiry.

6. Comparison with Contemporary Patents

Patent Similarities Differences Innovation Level
US 5,527,814 Benzothiazole core, therapeutic utility Specific substitution patterns Foundational scaffold
US 7,093,753 Broader derivative claims Focus on newer substitutions Incremental improvement
WO 92/0577 Similar heterocyclic compounds Expanded synthesis methods Related but distinct scope

Conclusion: The ‘814 patent established a core chemical class used as a platform for further innovation.


7. FAQs

Q1: What is the primary chemical scope of US 5,527,814?
A1: It covers substituted benzothiazole derivatives with specific functional groups, primarily claimed as therapeutic agents.

Q2: Does the patent cover synthesis methods?
A2: Yes, several claims focus on methods of preparing the compounds, adding a process dimension to the patent.

Q3: Are the patent protections still valid?
A3: Likely expired in 2013, given standard 20-year terms from priority date, unless extended or granted in other jurisdictions.

Q4: How does this patent impact generic drug development?
A4: Once expired, it facilitates the production of generic equivalents; while during active term, it served as a barrier.

Q5: What subsequent innovations were built upon this patent?
A5: Later patents added derivatives with enhanced activity, optimized formulations, or novel therapeutic applications, broadening the original scope.


8. Key Takeaways

  • Scope: The ‘814 patent primarily protects a class of heterocyclic compounds with medicinal utility, focusing on chemical structure and synthesis methods.
  • Patent Lifecycle: Likely expired, opening opportunities for generic manufacturing and further innovation.
  • Landscape: It served as a foundational patent, cited by many later patents and influencing subsequent drug development in antiviral and anticancer fields.
  • Strategic Positioning: Its narrow chemical claims were balanced by broad process and use claims, strengthening its protective scope during active years.
  • Market Impact: Post-expiry, the patent's disappearance reduced barriers, but during its enforceable period, it functioned as a significant intellectual property asset for patent holders.

References

  1. U.S. Patent No. 5,527,814. (June 18, 1996). Issued to Warner-Lambert Company LLC.
  2. European Patent EP 0622715 B1. (March 1, 1995).
  3. China Patent CN 1046520. (May 15, 1996).
  4. Japan Patent JP 2,777,727. (November 13, 1996).
  5. “Heterocyclic compounds as antiviral agents,” Journal of Medicinal Chemistry, 1990–2000.
  6. Patent citation analysis tools (e.g., Derwent Innovation, Espacenet).

More… ↓

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Drugs Protected by US Patent 5,527,814

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: 5,527,814

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
France92 02696Mar 06, 1992

International Family Members for US Patent 5,527,814

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 149833 ⤷  Start Trial
Australia 2948292 ⤷  Start Trial
Australia 666150 ⤷  Start Trial
Canada 2117466 ⤷  Start Trial
Czech Republic 281293 ⤷  Start Trial
Czech Republic 9402120 ⤷  Start Trial
Germany 69218255 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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