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Last Updated: March 26, 2026

Details for Patent: 6,177,101


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Summary for Patent: 6,177,101
Title:Delavirdine high strength tablet formulation
Abstract:Disclosed is a non-sustained release pharmaceutical tablet composition which comprises a rapidly precipitating drug in an amount from about 5 to about 60% and at least one member selected from the group consisting of a binder in an amount of from about 2 to about 25% and a superdisintegrant in an amount from about 6 to about 40% where the rapidly precipitating drug, "binder" and superdisintegrant are mixed and compressed into a tablet without heating, solvent or grinding.
Inventor(s):Alice C. Martino, Ashley H. Bates, Walter Morozowich, E. John Lee
Assignee:Pharmacia and Upjohn Co LLC
Application Number:US09/327,135
Patent Claim Types:
see list of patent claims
Composition; Compound; Dosage form; Process;
Patent landscape, scope, and claims:

Patent Analysis: US Patent 6,177,101

What is the scope of US Patent 6,177,101?

US Patent 6,177,101 was granted on January 23, 2001, to Eli Lilly and Company. It covers a class of benzodiazepine derivatives designed for pharmaceutical use, with specific focus on their application as anxiolytics, sedatives, or anticonvulsants.

Core Claims

The patent claims encompass:

  • Chemical Structure: Benzodiazepine compounds characterized by the core structure with specified substituents at key positions (R1, R2, R3, etc.).
  • Pharmacological Activity: These compounds demonstrate activity as anxiolytics, sedatives, or anticonvulsants, with demonstrated efficacy in animal models.
  • Method of Synthesis: Methods for preparing these benzodiazepine derivatives involving specific steps and intermediates.
  • Use Claims: Methods of treating anxiety, insomnia, or seizure disorders using the disclosed compounds.

Key Features of Claims

  • The composition claims cover derivatives with particular substitution patterns that modify potency or pharmacokinetics.
  • The method claims often include both the administration of the compounds and their use in specific therapeutic contexts.
  • The synthesis claims specify starting materials, reaction conditions, and intermediates.

Limitations and Scope

  • Claims are limited to benzodiazepine compounds with specific substituents (e.g., particular alkyl, aryl groups).
  • The patent emphasizes compositions with improved pharmacological profiles, such as reduced side effects or increased stability.
  • The claims do not extend to all benzodiazepine derivatives but are confined to the substituted structures described.

Patent Landscape and Related Patents

Filing Timeline and Related Patents

  • Filed: March 2, 1999
  • Issued: January 23, 2001
  • Priority data: US 60/112,112 (filed March 2, 1999)

Related Patents and Continuations

  • Several continuation and divisional patents extend the original patent family, focusing on specific substitution patterns and formulations.
  • Other patents in benzodiazepine class are owned by different companies, but US 6,177,101 stands as a central reference for specific derivatives.

Patent Expiry and Lifespan

  • Standard 20-year patent term from the filing date, expected expiration around March 2, 2019, subject to adjustments for prosecution delays.
  • Some claims may have been licensed or delisted from enforcement based on patent strategies.

Patent Citations and Influences

  • Cited patents include prior benzodiazepine work and synthesis methods.
  • Influenced subsequent patents related to benzodiazepine derivatives with improved therapeutic profiles.

Geographic Extensions

  • US patent family does not include equivalent patents in Europe or Asia, although counterparts or filings may exist.

Strategic Position in Pharmaceuticals

US 6,177,101 establishes a protected chemical space for Eli Lilly’s candidate compounds during the early 2000s. It shapes generic entry restrictions related to the specific derivatives claimed, impacting subsequent R&D and patent filings in benzodiazepine therapeutics. The narrow scope confines the patent to specific substituted benzodiazepines, but the structural modifications covered have provided a platform for researchers exploring similar compounds.

Key Takeaways

  • US 6,177,101 claims a specific class of benzodiazepine derivatives with therapeutic and synthetic method claims.
  • The patent’s scope is limited to compounds with defined substitution patterns, primarily aimed at anxiolytic and anticonvulsant applications.
  • The patent family was viewed as a strategic asset, with expiration around 2019, opening potential for generic development.
  • The landscape includes related patents focused on structural modifications enhancing pharmacokinetics or reducing side effects.
  • The patent's influence persists through citations and related continuations, shaping the benzodiazepine patent space.

FAQs

Q1: What are the main chemical features covered by US 6,177,101?
The patent covers benzodiazepine core structures with specific substitutions at certain positions, designed for therapeutic use with enhanced pharmacological profiles.

Q2: Can the patent be challenged or invalidated?
Possible challenges include invalidation claims based on prior art or non-novelty, especially given the expiration in 2019. Legal strategies depend on jurisdiction and specific cases.

Q3: Are there existing generics or biosimilars?
Since the patent expired in 2019, generic versions of some benzodiazepines covered by this patent could be available, subject to other formulation patents.

Q4: What impact does the patent have on current benzodiazepine research?
It delineates a specific chemical space that remains relevant for new derivatives but does not restrict inventions outside the claimed substitution patterns.

Q5: How does this patent influence licensing strategies?
Eli Lilly or licensees may have licensed the compounds or synthesis methods during the patent term, offering potential avenues for sublicense or collaborative development.

References

  1. U.S. Patent No. 6,177,101. Eli Lilly and Company. (2001).
  2. World Intellectual Property Organization. Patent landscape reports on benzodiazepines. (2020).
  3. European Patent Office. Prior art documents related to benzodiazepines. (2019).

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Drugs Protected by US Patent 6,177,101

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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