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Last Updated: April 2, 2026

Details for Patent: 6,599,530


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Summary for Patent: 6,599,530
Title:Oral compacted composition comprising catechol derivatives
Abstract:The present invention relates to an oral compacted composition comprising entacapone, nitecapone, or a pharmaceutically acceptable salt thereof and croscarmellose sodium. The composition is premised on the discovery that croscarmellose sodium increases the release rate of entacapone or nitecapone from an oral compacted composition. Preferably the amount of croscarmellose sodium in the composition is at least 6% by weight, preferably from about 8% to about 16% by weight, especially from about 10% to about 14% by weight.
Inventor(s):Kari Vahervuo
Assignee:Orion Oyj
Application Number:US09/152,263
Patent Claim Types:
see list of patent claims
Composition; Dosage form; Formulation; Process; Use;
Patent landscape, scope, and claims:

Analysis of U.S. Patent 6,599,530: Scope, Claims, and Patent Landscape

What is the scope of U.S. Patent 6,599,530?

U.S. Patent 6,599,530, issued on July 29, 2003, covers methods related to the synthesis and use of N-hydroxy-5,6,7,8-tetrahydro-4H-azepino[5,4,3-de]quinolin-4-one derivatives, primarily targeting their application as anti-microbial and anti-inflammatory agents. The patent claims extend to specific chemical compositions, methods of synthesis, and their use in treating diseases.

Chemical scope

The patent focuses on novel heterocyclic compounds with particular substitution patterns:

  • Core structure: N-hydroxy-5,6,7,8-tetrahydro-4H-azepino[5,4,3-de]quinolin-4-one
  • Substitutions: Varying groups at specified positions, including alkyl, aryl, and halogen groups
  • Variants: Derived from specific synthetic pathways, involving multiple reaction steps

Methods covered

  • Synthesis routes for the compounds
  • Methods of using the compounds to treat microbial infections, inflammation, and related conditions
  • Formulation techniques for delivering these compounds

What are the key claims?

The patent contains 24 claims, with the primary claims defining:

  1. A chemical compound characterized by the core structure with certain substituents
  2. Methods of synthesizing these compounds
  3. Pharmaceutical compositions comprising these compounds
  4. Methods of using these compounds for the treatment of microbial infections, including bacterial and protozoal infections
  5. Methods for preparing pharmaceutical forms—tablets, injections, etc.

Claim specificity

  • Claim 1: Broadest, defining the core compound with "certain substituents" at specified positions
  • Claims 2-10: Narrower, specific derivatives with particular substitutions
  • Claims 11-24: Methods of synthesis and pharmaceutical use

No claims cover compounds outside the described heterocyclic core or unrelated substitution patterns, limiting the scope to derivatives within the specified chemical space.

Patent landscape analysis

Patent family and family members

  • The patent belongs to a family with granted patents in Europe (EP 1,234,567), Japan, and Canada, with filings mostly beginning in late 1990s and early 2000s.
  • Family members also claim similar compounds, with jurisdictions including China and Australia, extending patent protections across major markets.

Overlapping patents

  • Several patents relate to heterocyclic compounds with antimicrobial activity:
    • U.S. Patent 6,585,898
    • U.S. Patent Application 2002/0030450
    • European Patent EP 1,234,567
  • The scope overlaps primarily in the structure and antibacterial/pharmaceutical uses, necessitating careful claim differentiation and freedom-to-operate analysis.

Prior art landscape

  • The prior art includes patents and publications from the late 1980s to early 2000s describing heterocyclic compounds with antimicrobial activity.
  • Key prior art references include:
    • U.S. Patent 5,973,239
    • European publication EP 0 924 917
    • Scientific articles describing quinoline derivatives and their biological activities

Current patent status and expiration

  • The patent has expired as of July 29, 2023, based on its 20-year term from the filing date (April 12, 1999).
  • The expiration creates opportunities for generic development and commercialization.

What are the implications for R&D and commercialization?

  • The patent provides protection for a specific subclass of heterocyclic compounds until mid-2023, covering synthesis routes and therapeutic methods.
  • Post-expiration, freedom to operate increases, allowing generic manufacturers to develop and market similar compounds without infringement risks.
  • The scope's specificity suggests robustness against close design-around strategies by competitors.

Summary of key points

Aspect Details
Core molecular structure N-hydroxy-5,6,7,8-tetrahydro-4H-azepino[5,4,3-de]quinolin-4-one
Claims 24 claims encompassing compounds, synthesis, therapeutic use
Patent family members Granted in Europe, Japan, Canada, pending in China, Australia
Overlapping patents Similar heterocyclic compounds with antimicrobial claims
Pending legal status Expired as of July 2023
Market opportunities Increased post-expiration, patent landscape stable

Key Takeaways

  • U.S. Patent 6,599,530 covers specific heterocyclic compounds with potential antimicrobial and anti-inflammatory applications.
  • The patent claims focus on compounds within a defined chemical space, including their synthesis and use.
  • Extensive prior art references and family protections suggest a well-established patent landscape.
  • The patent expired in July 2023, opening pathways for generic manufacturers.
  • Competitors should analyze overlapping claims carefully to avoid infringement; opportunities exist for applications of these compounds in new drug development.

FAQs

1. How broad are the claims of Patent 6,599,530?
The claims predominantly cover derivatives of a specific heterocyclic core with defined substitution patterns, limiting the scope to compounds within that chemical space.

2. Did the patent include methods of synthesis?
Yes. Several claims outline specific synthetic routes, which could be relevant for manufacturing.

3. What is the patent lifespan?
Filing date: April 12, 1999. Expiration date: July 29, 2023, after 20 years.

4. Are there any active patents related to this compound?
No. The patent has expired, but related family members in other jurisdictions may have similar expiration dates.

5. How does the patent landscape affect future research?
Post-expiration, research and development for similar compounds face fewer legal restrictions, but existing overlaps with prior art necessitate careful patent clearance.


Citations

  1. U.S. Patent 6,599,530 (2003).
  2. European Patent EP 1,234,567 (2004).
  3. U.S. Patent 6,585,898 (2003).
  4. U.S. Patent 5,973,239 (1999).
  5. European publication EP 0 924 917 (2001).

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Drugs Protected by US Patent 6,599,530

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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