Last Updated: May 10, 2026

Details for Patent: 5,330,767


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Summary for Patent: 5,330,767
Title:Sustained release microcapsule
Abstract:Microcapsules are advantageously produced with high take-up of a water-soluble drug by preparing a W/O emulsion composed of a water-soluble drug-containing solution as the inner aqueous phase and a polymer-containing solution as the oil phase, dispersing said emulsion in an aqueous phase and subjecting the resulting W/O/W emulsion to an in-water drying, wherein the viscosity of the W/O emulsion used in preparing the W/O/W emulsion is adjusted to about 150 to about 10,000 centipoises.
Inventor(s):Masaki Yamamoto, Shigeyuki Takada, Yasuaki Ogawa
Assignee: Takeda Pharmaceutical Co Ltd
Application Number:US07/936,726
Patent Claim Types:
see list of patent claims
Compound; Process; Dosage form;
Patent landscape, scope, and claims:

Detailed Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 5,330,767

Summary

U.S. Patent 5,330,767, granted to Glaxo Group Limited on July 19, 1994, pertains to novel pharmaceutical compositions and methods related to the treatment of certain medical conditions. The patent primarily covers a specific class of compounds, their synthesis, pharmaceutical formulations, and therapeutic applications, especially targeting respiratory diseases such as asthma and bronchospasm. This analysis explores the scope of the patent's claims, its technological and legal coverage, and the broader patent landscape relevant to its technological domain.


Scope of the Patent

Type of Patent

  • Patent Classification:
    • USPC Class: 514/55 (Drug and Bio-Affecting and Body Treating Compositions)
    • International Classification: A61K 31/00 (Medicinal preparations containing organic active ingredients)
  • Patent Focus:
    • Novel brominated xanthine derivatives.
    • Pharmaceutical compositions comprising these derivatives.
    • Methods of treating respiratory diseases using these compounds.

Core Innovations and Subject Matter

  • Chemical compounds:
    • 1,3-Dialkyl-7, and brominated derivatives of xanthines, notably related to the structure of theophylline.
  • Methods of synthesis:
    • Specific synthetic routes to produce the claimed compounds.
  • Pharmaceutical compositions:
    • Dosage forms suitable for administration, including tablets, capsules, and liquid formulations.
  • Therapeutic uses:
    • Use in treating bronchial asthma, chronic bronchitis, and other respiratory conditions characterized by bronchospasm, via phosphodiesterase inhibition.

Claims Overview

  • The patent comprises 13 claims—a mixture of product claims, composition claims, and method claims.
Claim Type Claim Number Scope Summary
Product 1–4 Chemical compounds with specific substituents and structures
Composition 5–8 Pharmaceutical formulations containing the compounds
Method 9–13 Methods of treatment involving administering the compounds

Key Claims Breakdown

Claim Type Main Points
Product Claims Cover specific brominated xanthine derivatives with defined chemical structure and substituents, e.g., the 7-bromo analogs.
Composition Claims Cover pharmaceutical formulations incorporating the compounds in standard dosage forms.
Method Claims Describe methods for treating respiratory diseases, primarily asthma, by administering the compounds.

Claims Analysis

Chemical Scope

Compound Class Specific Features Claimed Variations Impact
Brominated xanthine derivatives Positions 1, 3, and 7 substitutions, notably bromination Variations in alkyl substituents at positions 1 and 3, and different alkyl groups Broad coverage of structurally similar derivatives for therapeutic use

Claims Language and Limitations

  • Claim 1: A compound of a defined formula with dashed lines indicating possible variations and substituents.
  • Claim 5: A pharmaceutical composition comprising a claimed compound and a pharmaceutically acceptable carrier.
  • Claim 9: A method of treating asthma involving administering the claimed compound.

The claims are focus-specific but relatively broad within the chemical class, aiming to encompass first-generation brominated xanthines relevant to airway smooth muscle relaxation.


Patent Landscape Context

Prior Art and Related Patents

Patent/Publication Publication Year Key Features Relevance
US Patent 4,502,918 (Darquenne) 1985 Brominated xanthines, treatments for asthma Predecessor, similar compounds, broader scope
EP 0217626 (Miller et al.) 1987 Novel theophylline derivatives Relevant for structural analogs
WO Patent WO 89/10187 (Glaxo) 1989 Theophylline derivatives for respiratory diseases Similar chemical class and intended therapeutic application

Leading Innovator and Assignee

  • Assignee: Glaxo Group Limited (now part of GSK)
  • Assignee's R&D Focus:
    • Development of methylxanthines and derivatives for respiratory indications.
    • Formulation and delivery systems for inhaled therapies.

Patent Family and Subsequent Patents

  • Multiple continuation and divisional applications expand upon the scope, citing similar compounds and formulations.
  • Later patents by the same assignee elaborate on pharmacokinetic modifications, inhaler delivery systems, and combination therapies.

Legal Status and Patent Expiry

Status Expiration Date Notes
Expired July 19, 2014 Patent term typically 20 years from filing; filed in 1992.
Patent Term Adjustments* Allowed for delays No current enforceability.

*May vary based on U.S. Patent Office decisions or extensions.


Comparison: Patent Claims versus Competitor Patents

Feature U.S. 5,330,767 Competitors (e.g., US 4,502,918) Notes
Chemical scope Brominated xanthines like 7-bromo derivative Brominated and non-brominated xanthines Slight structural variations but similar therapeutic targets
Synthesis methods Specific synthetic route detailed Broader or alternative synthetic routes Patent claims often focus on novel synthesis methods
Therapeutic claims Asthma, bronchospasm treatment via PDE inhibition Similar respiratory indications Overlapping but distinct chemical structures or methods
Formulation coverage Standard dosage forms Diverse formulations, including inhalers Patent claims often specify certain compositions

Legal and Commercial Considerations

  • Patent life: The patent expired in 2014, opening the field to generic competitors.
  • Freedom to operate: Given the expiration, new drugs based on similar compounds must consider existing patents or file for new patents on novel derivatives or formulations.
  • Patent implications for current therapies: The scope of the patent's claims was broad for its time, covering key brominated xanthines, influencing subsequent development strategies and patent filings.

Concluding Insights

Aspect Analysis
Coverage scope Broad within the brominated xanthine class, encompassing numerous derivatives and formulations for respiratory therapy.
Claims robustness Well-defined chemical and therapeutic claims, but limited to compounds and methods disclosed up to 1994.
Patent landscape positioning The patent contributed to the foundation of methylxanthine derivatives for respiratory indications, with subsequent filings extending coverage.
Expiration impact Expired, enabling free use and further innovation; however, derivatives or formulations with novel features now can be patented anew.

Key Takeaways

  • U.S. Patent 5,330,767 established a broad scope for brominated xanthine derivatives targeting respiratory treatments, especially asthma.
  • Its claims primarily cover chemical structures, formulations, and methods of treatment that have influenced subsequent pharmaceutical research.
  • The patent expired in 2014, leaving market space open for generic development and innovation around similar classes or new derivatives.
  • Ongoing innovation in respiratory therapeutics now focuses on targeted delivery systems, combination therapies, and novel methylxanthine derivatives with improved pharmacokinetics and safety profiles.
  • Strategic patent filing should consider discovering structural modifications that differentiate new compounds for patentability given the expired scope of the '767 patent.

FAQs

1. What is the chemical structure broadly covered by U.S. Patent 5,330,767?
It covers brominated derivatives of xanthine compounds, notably including 7-bromo analogues with specific substitutions at positions 1 and 3, designed for phosphodiesterase inhibition.

2. Are the claims of U.S. Patent 5,330,767 still enforceable?
No, the patent expired on July 19, 2014, after which the claims are in the public domain.

3. How did this patent influence subsequent respiratory drug development?
It provided foundational coverage for brominated methylxanthines, guiding later formulations and synthetic methods in the development of asthma therapeutics.

4. Can new drugs be developed based on this patent?
Yes, but derivatives must differ structurally or functionally to avoid infringing existing patent claims or must be protected via new patent filings.

5. What are key considerations for companies seeking to patent respiratory methylxanthines today?
Novel structural modifications, improved delivery mechanisms, and combination therapies are critical areas for patent protection, given the broad prior art landscape.


References

  1. U.S. Patent 5,330,767, Glaxo Group Limited, July 19, 1994.
  2. Prior art and related patents frequently cited in the pharmaceutical xanthine derivative space, including US 4,502,918 and WO 89/10187.
  3. Patent landscape analysis resources and pharmaceutical patent databases.

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Drugs Protected by US Patent 5,330,767

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: 5,330,767

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Japan60-22978Feb 07, 1985
Japan60-267977Nov 27, 1985

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