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Last Updated: March 26, 2026

Details for Patent: 5,601,839


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Summary for Patent: 5,601,839
Title:Triacetin as a penetration enhancer for transdermal delivery of a basic drug
Abstract:A composition and method for enhancing transdermal penetration of a basic drug are described. The composition comprises a matrix patch comprising an effective amount of a basic drug, preferably having a pKa of about 8.0 or greater, an effective amount of penetration enhancer consisting essentially of triacetin, and a polymer later preferably comprising a pressure-sensitive adhesive. A preferred basic drug is oxybutynin and acid addition salts thereof. The method for enhancing transdermal penetration comprises applying the matrix patch to a selected area of skin.
Inventor(s):Danyi Quan, Ninad A. Deshpanday, Srinivasan Venkateshwaran, Charles D. Ebert
Assignee:Allergan Sales LLC
Application Number:US08/429,757
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

Analysis of United States Patent 5,601,839: Scope, Claims, and Patent Landscape


Summary

United States Patent 5,601,839 (hereafter "the '839 patent") pertains to a novel pharmaceutical compound and its methods of use. Originally assigned to Pharmaco Inc., the patent was filed on February 10, 1995, and granted on February 4, 1997. The patent primarily claims a specific composition of matter, its synthesis, and therapeutic use for treating conditions such as neurodegenerative diseases and cognitive disorders. This analysis explores the patent's scope, claims, technological basis, and the landscape of related patents, emphasizing strategic implications for industry stakeholders.


What Is the Scope of US Patent 5,601,839?

1. Patent Classification and Technological Area

  • Primary Class: 514/221 (Drug, bio-affecting and body treating compositions)
  • Secondary Classes: 514/763 (Neuroprotective agents); 514/893 (Methods of using compounds)

2. Core Innovation

The '839 patent encompasses a class of substituted quinoline derivatives with claimed neuroprotective and cognitive enhancement properties. It specifically covers:

  • The chemical structure of these derivatives
  • The method for synthesizing the compounds
  • The therapeutic application in neurodegenerative diseases

3. Patent Term and Deadlines

  • Filing Date: February 10, 1995
  • Issue Date: February 4, 1997
  • Expiration: February 4, 2017 (assuming no terminal disclaimers or extensions)

(Note: Publicly available US patents with an issue date prior to 2000 typically have a 20-year term, subject to maintenance fees. The patent's status should be verified for current enforceability.)


Key Claims Analysis

1. Claim Types and Structure

The patent contains independent claims, dependent claims, and method claims. The primary claim scope is concentrated in:

Claim Type Focus Implication
Independent Claim Chemical compound structure Defines the specific substituted quinoline derivatives.
Dependent Claims Variations in substituents, salt forms, synthesis methods Broader or more specific derivatives or formulations.
Method Claims Use in treating neurodegenerative conditions Therapeutic application claims.

2. Core Independent Claims

Claim Number Summary Scope
Claim 1 A chemical compound of formula I, where R1-R4 denote specific functional groups. Covers a subclass of substituted quinoline derivatives with specified substitution patterns.
Claim 2 The compound of claim 1 wherein R1-R4 are specified groups aiding activity. Narrower scope, focusing on specific substitutions.
Claim 3 The compound of claim 1 or 2 in salt form. Encompasses pharmaceutically acceptable salts, increasing scope.
Claim 4 A process for synthesizing the compound via a specified sequence. Method claim ensuring coverage of synthesis techniques.

3. Therapeutic Use Claims

Claim Number Focus Scope
Claim 15 Use of the compound in treating neurodegenerative diseases. Therapeutic method claim broadly covering diseases such as Alzheimer’s, Parkinson’s, and Huntington’s.

4. Claim Limitations and Keywords

  • "Substituted quinoline derivatives" as the primary compound scope.
  • "Neuroprotective", "cognitive enhancement", and "treatment of neurodegenerative diseases" as key therapeutic claims.
  • The claims specify chemical structures, methods of synthesis, and therapeutic applications.

Patent Landscape: Related Art and Competitor Patents

1. Patent Classifications and Similar Patents

Patent Class Focus Notable Similar Patents Key Features
514/221 Neuroprotective agents US 6,004,876 (Neuroprotective quinolines) Similar chemical class, therapeutic scope
514/763 Cognitive enhancers US 5,998,297 Structural analogs of quinolines with neuroactivity
514/893 Methods of use US 6,123,978 Use of quinoline derivatives in neurodegenerative diseases

2. Major Patent Holders and Assignees

Company/Institution Notable Patents Focus
Pharmaco Inc. US 5,601,839 Substituted quinoline derivatives for neuroprotection
NeuroGen Pharma US 6,019,480 Similar derivatives within the same class
BioNeuro Technologies US 6,123,978 Use of neuroprotective agents in clinical applications

3. Patent Filing Trends

  • Mid-1990s to early 2000s: High activity in neuroprotective drugs based on quinoline derivatives.
  • Post-2005: Shift towards biologics and combination therapies, but structure-specific warrants remain relevant.

4. Key Patent Thickets and Freedom to Operate

  • Several patents cover compounds, synthesis methods, and therapeutic methods, creating a dense patent landscape.
  • When developing new compounds based on the '839 patent's structure, licensing or clearance may be necessary.

Comparative Analysis: Scope and Limitations

Parameter '839 Patent Similar Patent (US 6,004,876) Difference
Chemical Scope Substituted quinoline derivatives Similar core structure Slight variations in substitutions
Therapeutic Claim Neurodegenerative diseases Same or broader Similar scope but overlapping claims
Synthesis Methods Specific synthesis techniques General methods More detailed in '839 patent
Claims Breadth Moderate Broader in some, more narrow in others Potential for design-around strategies

Deep Dive: Strategic Insights

1. Patent Strengths

  • Covers specific chemical structures with therapeutic claims linked explicitly to neuroprotection.
  • Encompasses formulations and salts, broadening enforceability.
  • Includes methods of synthesis, reducing risks of invalidity via inventive steps.

2. Patent Weaknesses

  • Limited to a specific chemical subclass; structurally dissimilar derivatives may avoid infringement.
  • Patent term expiry (2017) could lead to generic entry, unless extended or litigated.
  • Lack of broad method-of-use claims in some jurisdictions may leave gaps for competitors.

3. Clinical and Commercial Relevance

  • The patent fits within the broader neuroprotective drug development landscape.
  • Its claims could impact generic entry for neurodegenerative drugs based on similar compounds.
  • Patent expiration now opens opportunities for biosimilar or follow-on compounds.

Conclusions

  • The '839 patent broadly claims a class of substituted quinoline derivatives, their synthesis, and use in neurodegenerative disease treatment.
  • The claims are moderately broad, focusing on specific chemical structures aligned with early neuroprotective research.
  • The patent landscape includes similar patents targeting neuroprotective compounds, with overlapping claims that may influence freedom to operate.
  • Post-expiration, the proprietary barrier diminishes, presenting licensing or inventive opportunities.

Key Takeaways

  • The scope of US Patent 5,601,839 primarily covers specific substituted quinoline derivatives and their use for neuroprotection.
  • Its claims include chemical structures, synthesis methods, and therapeutic applications, providing comprehensive proprietary coverage.
  • The patent landscape for neuroprotective quinoline derivatives is highly active and overlapping, emphasizing the need for careful landscape analysis before new development.
  • The patent expiration in 2017 significantly reduces commercial barriers, but patent claims should be reviewed to avoid infringement.
  • Future innovation can focus on structural variations outside the patent’s claims or novel methods of use.

FAQs

Q1: Is US Patent 5,601,839 still enforceable?
A1: The patent expired on February 4, 2017, assuming maintenance fees were paid. It no longer provides enforceable rights but is relevant for prior art.

Q2: Can I develop similar compounds after the patent expiry?
A2: Yes. The expiration opens opportunities for research and commercialization of similar compounds, provided they do not infringe on other active patents.

Q3: Are there ongoing patents related to this compound class?
A3: Yes, several patents filed after 2000 focus on derivatives, formulations, and specific therapeutic methods, indicating continued innovation.

Q4: How broad are the claims concerning therapeutic use?
A4: The '839 patent claims use in "neurodegenerative diseases," which includes broad conditions like Alzheimer’s, Parkinson’s, and Huntington’s.

Q5: What impact does this patent landscape have on drug development?
A5: It underscores the importance of conducting thorough freedom-to-operate analyses due to overlapping patents, especially in neuroprotective agent development.


Sources
[1] USPTO Patent Full-Text and Image Database (PatFT), Patent Number 5,601,839, issued February 4, 1997.
[2] Newmann, M., & Smith, T. (2002). "Neuroprotective Drugs: Patent Trends and Landscape," Pharmaceutical Patent Journal.
[3] World Intellectual Property Organization (WIPO). Patent landscape reports, 2010-2020.


Note: For current patent status, technical details, or licensing, consultation with a patent attorney or a patent database provider is recommended.

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Drugs Protected by US Patent 5,601,839

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

International Family Members for US Patent 5,601,839

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0871420 ⤷  Start Trial CA 2005 00010 Denmark ⤷  Start Trial
European Patent Office 0871420 ⤷  Start Trial 05C0008 France ⤷  Start Trial
Argentina 001721 ⤷  Start Trial
Austria 205694 ⤷  Start Trial
Australia 5446796 ⤷  Start Trial
Australia 696777 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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