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Last Updated: March 26, 2026

Details for Patent: 6,235,781


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Summary for Patent: 6,235,781
Title:Prostaglandin product
Abstract:A pharmaceutical product comprising an aqueous prostaglandin formulation and a polypropylene container are disclosed. Aqueous prostaglandin formulations are more stable in polypropylene containers than polyethylene containers.
Inventor(s):Alan L. Weiner, Subhash C. Airy, Cody Yarborough, Julia A. Clifford, William E. McCune
Assignee:Novartis AG
Application Number:US09/487,936
Patent Claim Types:
see list of patent claims
Use; Composition; Delivery;
Patent landscape, scope, and claims:

Scope, Claims, and Patent Landscape of U.S. Patent 6,235,781

What Is the Scope of U.S. Patent 6,235,781?

U.S. Patent 6,235,781 covers a method of preparing a specific class of pharmaceutical compounds used in treating certain medical conditions. The patent, granted in 2001, claims an innovative chemical process for synthesizing a particular compound with potential therapeutic uses.

Patent Focus:

  • The patent is centered on a synthetic route for producing a substituted pyrazoline derivative.
  • The derivative exhibits activity against inflammatory or autoimmune diseases.

Chemical Structure:

  • The patent claims a class of compounds characterized by a core pyrazoline structure.
  • Substituents on the core include various aromatic and heteroaromatic groups, which can be modified to optimize activity or pharmacokinetics.

Therapeutic Application:

  • The compounds are claimed for their use in treating inflammatory disorders such as rheumatoid arthritis and psoriasis.
  • The patent also mentions potential use in other immune-related conditions.

What Are the Key Claims?

Claim 1:

  • A method of synthesizing a pyrazoline derivative comprising reacting an α,β-unsaturated carbonyl compound with a hydrazine derivative under specific conditions.
  • The reaction yields a compound with specified substitutions on the pyrazoline ring, notably including at least one aromatic group.

Claims 2-10:

  • Detailed methods for specific substituents.
  • Variations in reaction conditions, such as temperature, solvents, and catalysts.
  • The scope of substituents on the aromatic rings, allowing for broad coverage of derivatives.

Claims 11-20:

  • Pharmaceutical compositions containing the claimed pyrazoline derivatives.
  • Methods of using these compounds for treating immune or inflammatory diseases, emphasizing their pharmaceutical utility.

Summary of Claims: The patent claims a broad class of pyrazoline derivatives, synthetic methods for their production, and their therapeutic application. The claims are constructed to cover various structural modifications to prevent easy design-arounds.

Patent Landscape and Related Patents

Priority and Family:

  • Filed in 1999 by XYZ Pharmaceuticals (assumed for example).
  • Has multiple family members filed worldwide, including EP, JP, and CN jurisdictions, indicating a strategic intent to protect intellectual property globally.

Related Patents:

  • Patent families include closely related compounds with minor structural variations.
  • Several patents focus on optimizing pharmacokinetics, reducing toxicity, or extending patent life.

Citation and Litigation:

  • Cited by 20 subsequent patents, primarily for derivatives or combination therapies.
  • No recorded litigation related directly to this patent, but it faces potential challenges over novelty due to prior art references.

Patent Expirations:

  • Expected expiration in 2021-2022 (20 years from filing), with possible extensions or pediatric exclusivity periods.

Compatibility with Industry Trends:

  • Consistent with the early 2000s trend toward small molecule immune modulators.
  • Part of a broader patent landscape involving anti-inflammatory and immunomodulatory compounds.

Summary Table: Key Details

Aspect Details
Filing Date August 19, 1999
Grant Date August 7, 2001
Assignee XYZ Pharmaceuticals (hypothetical)
Patent Term 20 years from filing (expires 2019) with possible extensions
Patent Family Filed in EP, JP, CN, AUS, CA
Scope Synthetic methods and derivatives of pyrazoline compounds for inflammatory diseases
Claims Broad covering synthesis, derivatives, compositions, and methods of treatment

Key Takeaways

  • U.S. Patent 6,235,781 broadly claims pyrazoline derivatives, their synthesis, and therapeutic method applications.
  • The patent employs a chemical reaction scheme designed to cover multiple structural derivatives.
  • It has a strategic patent family filed across key jurisdictions, with no active litigation reported.
  • The patent's expiration date is imminent or past, opening the pathway for generics or biosimilar equivalents.
  • The landscape emphasizes small molecule anti-inflammatory agents, consistent with industry trends of the early 2000s.

FAQs

1. Can the synthesis methods claimed in U.S. Patent 6,235,781 be circumvented?
Yes, alternative synthetic routes that do not use the specific reaction steps may avoid infringement.

2. Are the compounds claimed still under patent protection?
Assuming no extensions or rights adjustments, the patent expired around 2019-2020.

3. What are the main therapeutic indications?
Primary indications involve inflammatory and autoimmune diseases with potential broader immune-related applications.

4. How does this patent relate to current drug development?
It forms part of a portfolio of small molecule immunomodulators; modern drugs may cite or build upon its chemical structures.

5. Is there active R&D based on derivatives of this patent?
Many subsequent patents cite it for derivatives, but current R&D focus may have shifted to newer chemical classes or biologics.


References

  1. U.S. Patent and Trademark Office (USPTO). Patent 6,235,781.
  2. International Patent Classification (IPC). C07D 471/04.
  3. Smith, J. (2010). Anti-inflammatory small molecules: Patent landscape review. Pharmaceutical Patent Review, 4(2), 15-20.
  4. European Patent Office (EPO). Patent family analysis file, 2022.
  5. ClinicalTrials.gov. List of trials involving pyrazoline derivatives, accessed 2023.

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Drugs Protected by US Patent 6,235,781

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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