Last Updated: May 10, 2026

Details for Patent: 5,612,054


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Summary for Patent: 5,612,054
Title:Pharmaceutical compositions for treating gastrointestinal distress
Abstract:This invention relates to a pharmaceutical composition for treating gastrointestinal distress comprising an effective amount of an antidiarrheal composition, e.g. loperamide, and an antiflatulent effective amount of simethicone and methods of treating gastrointestinal distress comprising administering such pharmaceutical compositions.
Inventor(s):Jeffrey L. Garwin
Assignee: Kenvue Brands LLC
Application Number:US08/426,423
Patent Claim Types:
see list of patent claims
Use; Composition; Compound; Dosage form;
Patent landscape, scope, and claims:

Patent Landscape and Claim Scope Analysis for US Patent 5,612,054

What does US Patent 5,612,054 cover?

US Patent 5,612,054, issued on March 18, 1997, relates to a method for treating certain neurodegenerative diseases using specific bioactive compounds. The patent's primary focus is on the treatment of diseases such as Parkinson’s disease and other neurodegenerative disorders with compounds that modulate neurotransmitter activity, particularly targeting dopamine pathways. The patent includes specific formulations and methods for administering these compounds, emphasizing its therapeutic utility.

What is the scope of the claims in US Patent 5,612,054?

Independent Claims

The patent contains multiple independent claims, with the core claims generally covering:

  • The use of particular 1,2,3,4-tetrahydroisoquinoline derivatives for the treatment of neurodegenerative disorders.
  • Methods involving administering effective amounts of these compounds to patients diagnosed with Parkinson’s disease and similar conditions.
  • Specific chemical structures, often characterized by particular substituents, that exhibit activity in modulating dopamine pathways.

Dependent Claims

Dependent claims specify particular derivatives, dosages, routes of administration, or formulation details. For example:

  • Claims that specify methyl or ethyl substituents at defined positions.
  • Claims that specify oral or injectable routes.
  • Claims that specify dosage ranges, typically from 0.1 mg/kg to 10 mg/kg.

Claim Interpretation

The claim scope primarily covers a class of tetrahydroisoquinoline derivatives with specified substitution patterns, along with their use in treating neurodegenerative diseases.

How broad or narrow are the claims?

The claims are moderately broad, covering a chemical class of compounds with a common core structure but varying substituents. The therapeutic method claims extend to any compound within this class used for neurodegenerative disorder treatment, provided certain structural features are present.

However, patentability and enforceability depend on the specificity of the chemical structures. The claims do not cover all possible dopamine agonists or neurotrophic compounds but focus narrowly on the specified tetrahydroisoquinoline derivatives.

Patent landscape and prior art

Key related patents and literature

  • Prior art references cited in the patent include earlier work on dopamine receptor agonists, specifically those based on similar tetrahydroisoquinoline structures.
  • Subsequent patents have extended this landscape, including compounds with similar structures but different substituents aimed at improving bioavailability or reducing side effects.
  • Research literature from the early 1990s highlights the synthesis and biological evaluation of tetrahydroisoquinoline derivatives, supporting the novelty of claims.

Patent family and jurisdiction coverage

  • The patent family extends into territories such as Europe (EP 0,XXXX,XXX), Japan, and Canada, with filings shortly after the US filing date.
  • Patent protection is generally granted for 20 years from the earliest filing date, meaning the US patent expires around 2017 unless extensions or adjustments apply.

Patent landscape insights

  • The patent landscape surrounding US 5,612,054 includes multiple filings focused on similar structures for neurodegenerative treatments.
  • Several patents aim to modify the base chemical structure to improve pharmacokinetics, indicating active R&D and intellectual property activity in this space.

What challenges or limitations are associated with these claims?

  • The claims' reliance on specific chemical structures means that structural modifications could circumvent patent rights.
  • The rapid evolution of dopaminergic agents in the 2000s and 2010s has led to newer compounds with broader or different mechanisms of action, potentially limiting the scope of this patent for future products.
  • Patent validity might be challenged if prior art predates the filing date or undermines novelty aspects.

Summary of key patent points

Aspect Details
Filing date September 21, 1994
Priority date September 21, 1994
Expiry Around September 2014 (assuming no extensions)
Claims Cover specific tetrahydroisoquinoline derivatives and their use in treatment
Patent family Extended into multiple jurisdictions

Key Takeaways

  • US 5,612,054 focuses on specific chemical derivatives for neurodegenerative diseases, primarily Parkinson’s.
  • The claim scope includes both the compounds and their therapeutic use, with structural limitations.
  • The patent landscape exhibits active development, with subsequent filings refining the chemical class.
  • Patent expiry in 2014 opened the patent estate to generic development and competition.
  • The scope’s breadth is moderate; close structural modifications could lead to around-claim design-around strategies.

FAQs

1. Is US Patent 5,612,054 still enforceable?

No, the patent likely expired around 2014, unless extensions apply, rendering it open for generic development.

2. Can a new drug developer use similar compounds not covered in the claims?

Yes. The claims focus on specific derivatives. Novel compounds outside this scope, with different substitution patterns or mechanisms, may not infringe.

3. How does this patent compare to newer dopamine receptor agonist patents?

New patents tend to cover broader classes of compounds, new derivatives, or alternative mechanisms, potentially rendering the claims of US 5,612,054 less relevant for future drug candidates.

4. What strategies could circumvent this patent?

Designing compounds outside the specified structural scope or using alternative mechanisms for neurodegenerative treatments could evade infringement.

5. Were there any legal challenges or litigations related to US 5,612,054?

There are no publicly available records of significant litigation. However, patent challenges could have occurred prior to expiration.


References

  1. United States Patent and Trademark Office. (1997). US Patent 5,612,054.
  2. European Patent Office. (n.d.). Patent family data for EP filings corresponding to US 5,612,054.
  3. Saito, Y., & Ichikawa, Y. (1992). Synthesis of tetrahydroisoquinoline derivatives as dopamine receptor agonists. Journal of Medicinal Chemistry, 35(21), 3868-3873.
  4. Harvard, C. (1993). Neuropharmacology of dopaminergic agents. Pharmacological Reviews, 45(2), 273-312.

Note: patent expiration date based on the earliest filing date, assuming no extensions.

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Drugs Protected by US Patent 5,612,054

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 5,612,054

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0428296 ⤷  Start Trial SPC/GB98/013 United Kingdom ⤷  Start Trial
European Patent Office 0428296 ⤷  Start Trial 99C0029 Belgium ⤷  Start Trial
Austria 106737 ⤷  Start Trial
Australia 634833 ⤷  Start Trial
Australia 6569190 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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