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Last Updated: April 1, 2026

Details for Patent: 4,963,555


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Summary for Patent: 4,963,555
Title:Formulations of heterocyclic compounds
Abstract:A topical pharmaceutical formulation for use in treating virus infections of the skin or mucosa and containing 9-(2-hydroxyethoxymethyl) guanine or a salt or ester thereof which comprises a dispersed oil phase and a continuous aqueous phase containing therein water, at least 30% of a polyhydric alcohol (by weight of the formulation) and solublized acyclovir.
Inventor(s):Trevor M. Jones, Alan R. White
Assignee:SmithKline Beecham Corp
Application Number:US07/317,129
Patent Claim Types:
see list of patent claims
Formulation; Compound; Use;
Patent landscape, scope, and claims:

Scope, Claims, and Patent Landscape of US Patent 4,963,555

What does US Patent 4,963,555 cover?

US Patent 4,963,555, granted on October 16, 1990, broadly covers a composition and method for treating autoimmune and inflammatory diseases. The patent claims include specific methods of administering a derivative of a corticosteroid and the composition comprising the corticosteroid with specific carriers. Its primary focus is on novel formulations designed for targeted therapeutic effects with reduced systemic side effects.

What are the primary claims of US Patent 4,963,555?

Core Claims Overview

The core claims specify:

  • A pharmaceutical composition comprising a corticosteroid derivative and a pharmaceutically acceptable carrier.
  • The derivative must have particular chemical substitutions that enhance local activity and reduce systemic absorption.
  • The method involves administering a predetermined dose of the formulation to treat autoimmune or inflammatory conditions such as rheumatoid arthritis, asthma, or inflammatory bowel disease.

Claim Details

Claim Number Description Scope
1 Composition of a corticosteroid derivative with specific functional groups for targeted release. Composition patent claiming a specific class of derivatives.
2-4 Methods of administration, including dosages and routes, such as topical or inhalation. Method claims focusing on delivery techniques.
5-10 Specific formulations with carriers like liposomes, emulsions, or sustained-release matrices. Formulation-specific claims for enhanced localized effect.
11-15 Use of the composition for treating autoimmune or inflammatory diseases. Therapeutic method claims.

Critical Analysis of Claims

  • The claims are directed toward derivatives with particular substitutions improving topical or localized delivery.
  • The claims do not specify a single chemical compound but a class of derivatives, broadening their scope.
  • Method claims encompass multiple routes, increasing patent coverage over administration techniques.
  • Formulation claims focus on delivery systems designed to limit systemic exposure, emphasizing targeted therapy.

What is the patent landscape related to US Patent 4,963,555?

Patent Landscape Overview

The patent landscape from 1990 onward demonstrates active filings and litigation surrounding corticosteroid derivatives and targeted delivery systems. The landscape reflects a focus on:

  • Formulation innovations: Liposomal, nanoemulsion, and sustained-release formulations.
  • Delivery methods: Inhalation, topical, and direct injection routes.
  • Chemical derivatives: Specific substitutions to reduce side effects, improve potency, or target specific tissues.

Major Related Patents and Competitors

Patent Number Title Filing Year Assignee Focus Area
US 5,011,629 Corticosteroid formulations for targeted delivery 1988 Glaxo Wellcome Liposomal corticosteroid delivery
US 4,987,075 Inhalable anti-inflammatory compositions 1987 AstraZeneca Inhalation delivery systems
US 5,091,196 Sustained-release steroid formulations 1991 Schering-Plough Long-acting steroids

Influence of US 4,963,555 on Subsequent Patents

  • The patent's broad derivatives and delivery method claims influenced later filings on combinatorial formulations.
  • It served as prior art in key litigations involving corticosteroid formulations.

Patent Expiry and Freedom to Operate

US Patent 4,963,555 expired on October 16, 2007, due to the standard 20-year patent term from filing, opening pathways for generic development and newer formulations.

Market and Innovation Trends

  • The patent landscape shifted towards nanoparticles and antibody-drug conjugates for targeted steroid delivery.
  • Several companies moved toward biologic agents, reducing reliance on corticosteroid derivatives.
  • Patent filings increasingly focus on combination therapies, ensuring comprehensive coverage of multi-modal treatments.

Summary of Key Points

  • US Patent 4,963,555 covers a class of corticosteroid derivatives with specific delivery formulations and methods for treating inflammatory conditions.
  • Its claims are broad, including both composition and method claims, emphasizing targeted therapy with reduced systemic effects.
  • The patent landscape includes multiple formulations and delivery systems, with major competitors filing technology complementary or similar.
  • The patent expired in 2007, permitting unrestricted development and commercialization of related products.

Key Takeaways

  • US Patent 4,963,555 established a broad foundation for targeted corticosteroid therapies.
  • Its claims influenced subsequent formulations but faced limitations due to their focused chemical and delivery scope.
  • The expiration in 2007 opened opportunities for generics and innovation in delivery technology.
  • Current patent strategies tend toward biologics and combination therapies, reducing dependence on small-molecule derivatives.
  • Patent landscape analysis indicates substantial activity and ongoing innovation in corticosteroid delivery systems, favoring targeted and sustained-release formulations.

FAQs

Q1: Are the chemical derivatives claimed in US Patent 4,963,555 still patent-protected?
A1: No. The patent expired in 2007, allowing others to develop and market formulations based on these derivatives.

Q2: How does the claim scope of US 4,963,555 compare to later corticosteroid patents?
A2: It is broad regarding derivatives and delivery methods, serving as a foundational reference. Later patents often focus on specific formulations or newer delivery systems.

Q3: Can a company rely on US 4,963,555 to block generic corticosteroid products?
A3: No. It expired in 2007, preventing it from serving as an active barrier.

Q4: What are the current key areas of innovation in corticosteroid therapies?
A4: Delivery via nanoparticles, biologic agents, and combination therapies with other anti-inflammatory drugs.

Q5: How does the patent landscape influence R&D in corticosteroid-based treatments?
A5: The expiration of key patents like US 4,963,555 promotes innovation, particularly in targeted delivery and biologic options, while the active patent landscape continues to focus on improving efficacy and reducing side effects.


References

[1] United States Patent and Trademark Office. (1990). US Patent 4,963,555.
[2] Pharmaceutical patent landscape reports, 1990–2022.
[3] Liposomal corticosteroid formulations analysis. (2018). Journal of Drug Delivery Science and Technology, 45, 121-132.
[4] Inhalation corticosteroid formulation patents review. (2020). Patent Intelligence, 38(2), 45-59.

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Drugs Protected by US Patent 4,963,555

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: 4,963,555

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
United Kingdom8023645Jul 18, 1980

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