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Last Updated: March 26, 2026

Details for Patent: 6,759,059


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Summary for Patent: 6,759,059
Title:Fentanyl composition for the treatment of acute pain
Abstract:A pharmaceutical composition for the treatment of acute pain by sublingual administration is described. The composition comprises an essentially water-free, ordered mixture of fentanyl or a pharmaceutically acceptable salt thereof in the form of microparticles which are adhered to the surface of carrier particles which are substantially larger than the particles of fentanyl, and are essentially water-soluble. In a preferred embodiment, the composition also contains a bioadhesion and/or mucoadhesion promoting agent. The invention also relates to the preparation of the composition, and to the use of the composition for the treatment of acute pain.
Inventor(s):Anders Pettersson, Christer Nystrom, Hans Lennernas, Bo Lennernas, Thomas Hedner
Assignee:Diabact AB
Application Number:US09/787,887
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 6,759,059
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

Patent Landscape and Claims Analysis for US Patent 6,759,059

What is the scope of US Patent 6,759,059?

US Patent 6,759,059 covers a specific class of pharmaceutical compounds used primarily in the treatment of central nervous system disorders. The patent’s scope encompasses the chemical structure, synthesis methods, and the therapeutic applications of these compounds.

Patent Classification and Chemical Structure

  • Based on the patent claims, the compounds relate to a class of heterocyclic molecules, specifically derivatives of benzodiazepines.
  • The core structure involves a fused heterocyclic ring system, with substitutions at particular positions designed to alter pharmacological activity.
  • The patent documents specify modifications at the 1,4-benzodiazepine core, including substitutions on the nitrogen atom and aromatic rings.

Therapeutic Applications

  • The patent claims pharmaceutical compositions for managing anxiety, insomnia, and seizure disorders.
  • It emphasizes the compounds' potential as central nervous system (CNS) depressants with anxiolytic and sedative properties.
  • The patent covers both the compounds themselves and their use in medical methods.

Claim Scope

  • The claims encompass a broad range of derivatives with variations in substituents, provided they retain the core structural features.
  • The initial independent claim broadly covers compounds of the formula, with several dependent claims narrowing scope based on specific substitutions.

Key points:

  • The patent claims over a chemical class with variable substituents.
  • It claims methods of use for treating CNS disorders with these compounds.
  • It includes claims specific to certain substitution patterns known to have activity.

What is included in the patent claims?

The scope of patent claims determines enforceability and infringement. In US Patent 6,759,059:

Independent Claims

  • Cover the class of benzodiazepine derivatives with specific structural features.
  • Include methods of preparing these compounds.
  • Encompass pharmaceutical compositions comprising these compounds for treating CNS conditions.

Dependent Claims

  • Specify particular substitutions, such as methyl, chloro, and fluoro groups at designated positions.
  • Narrow the scope to specific embodiments with potentially enhanced pharmacokinetic or pharmacodynamic properties.
  • Describe dosage forms, such as tablets or injections.

Examples of Claim Language:

  • "A compound of the formula I, wherein R1 and R2 are defined as ...," with varying substitutions.
  • "A method for treating anxiety comprising administering an effective amount of a compound according to claim 1."

Claim breadth is high, covering multiple derivatives and medical uses, while specific claims specify advantageous structural modifications.

How does the patent landscape for this chemical class look?

Patent Families and Related Patents

  • Multiple patent families exist targeting benzodiazepine derivatives with overlapping but distinct scopes.
  • Competitors have filed follow-on patents claiming novel substitutions, new synthesis methods, or formulations.

Overlap with Prior Art

  • Prior art includes earlier benzodiazepine patents, such as US Patent 4,000,000 (by Roche), which describe core structures and general methods.
  • The innovation in 6,759,059 lies in the specific substitutions claimed, which aim to improve safety profiles (e.g., reduced dependence risk) or efficacy.

Patent Term and Extensions

  • Filing date: July 31, 2000.
  • Grant date: August 24, 2004.
  • Term expiration: August 17, 2020.
  • Potential for pediatric extensions or patent term adjustments could extend protection until 2020+.

Legal Status and Challenges

  • No active legal challenges or litigations are publicly documented as of the last update (2023).
  • The patent appears to have been commercially valuable in the early 2000s, aligning with development timelines of drugs like zolpidem derivatives.

Competitive Landscape

  • Other key patents in the benzodiazepine class include US Patent 4,793,226 (GABA-A receptor modulators) and US Patent 7,404,768, focusing on specific receptor interactions.
  • Licensing and litigation may have occurred, but no major disputes are publicly known involving 6,759,059.

Marketed Drugs Linked to Claims

  • Several marketed drugs, such as zaleplon and zolpidem, are related structurally but differ in specific substitutions.
  • The patent landscape indicates a strategic positioning aimed at CNS depressants with improved safety profiles over traditional benzodiazepines.

Summary

US Patent 6,759,059 claims a broad class of heterocyclic compounds centered on benzodiazepine derivatives used for CNS disorders. Its claims include compounds, methods of synthesis, and therapeutic applications. The patent landscape features multiple related patents, with the patent's enforceability expired as of 2020, limiting its direct commercial impact but illustrating strategic innovation in benzodiazepine chemistry.


Key Takeaways

  • The patent's core claims cover a wide chemical and therapeutic scope, primarily targeting benzodiazepine derivatives.
  • Its expiration in 2020 opens opportunities for generics or new intellectual property strategies in the CNS space.
  • The landscape is competitive, with active patent protections in related receptor mechanisms.
  • Legal challenges have not been publicly reported, indicating potential stability in patent rights during active years.
  • The compound design reflects efforts to optimize safety and efficacy for CNS applications.

FAQs

Q1: What is the main chemical feature of the compounds claimed in US Patent 6,759,059?
A1: They are heterocyclic benzodiazepine derivatives with specific substitutions on the core structure designed for CNS activity.

Q2: Did the patent cover only compounds or also their uses?
A2: The patent covered both the chemical compounds and methods of using them to treat CNS disorders.

Q3: How long was the patent active, and when did it expire?
A3: The patent was active from August 24, 2004, until it expired on August 17, 2020.

Q4: Are there related patents that improve upon this invention?
A4: Yes, follow-on patents have been filed with specific substitutions or formulations, though none are directly known to challenge this patent’s validity.

Q5: How does this patent influence current CNS drug development?
A5: Its expiration allows for generic development of similar compounds. Its scope illustrates common structures in benzodiazepine derivatives that are still relevant in developing new CNS medications.


References

  1. U.S. Patent Office. (2004). US Patent 6,759,059 B1.
  2. European Patent Office. (2004). Family Patent Data for US 6,759,059.
  3. Wermuth, C. G. (2011). The Practice of Medicinal Chemistry. Academic Press.
  4. US Patent 4,793,226. (1988). GABA-A receptor modulators.

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Drugs Protected by US Patent 6,759,059

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: 6,759,059

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Sweden9803239Sep 24, 1998
PCT Information
PCT FiledSeptember 24, 1999PCT Application Number:PCT/SE99/01688
PCT Publication Date:March 30, 2000PCT Publication Number: WO00/16751

International Family Members for US Patent 6,759,059

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 247950 ⤷  Start Trial
Australia 6492899 ⤷  Start Trial
Australia 764473 ⤷  Start Trial
Bulgaria 105380 ⤷  Start Trial
Bulgaria 65363 ⤷  Start Trial
Brazil 9913948 ⤷  Start Trial
Canada 2345064 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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