Last Updated: August 8, 2026

Details for Patent: 6,248,358


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Summary for Patent: 6,248,358
Title:Bioadhesive progressive hydration tablets and methods of making and using the same
Abstract:A bioadhesive tablet wherein the active ingredient may be protected from water or the surrounding environment, thereby protecting it from metabolism or from other degradation caused by moisture, enzymes, or pH effects, and making it bioavailable only at a controlled rate. The active ingredient may be protected from moisture during the manufacturing process and more importantly may be protected from moisture and the immediate septic environment until after the patient has applied the tablet, and then only at a slow and controlled rate. It is by this process of progressive hydration that the active ingredient remains protected for many hours after administration. It is also by the process of progressive hydration that controlled and sustained release is achieved because only that part of the active ingredient that is the hydrated (aqueous) fraction of the tablet is available for absorption (bioavailable).
Inventor(s):William J. Bologna, Howard L. Levine, Philippe Cartier, Dominique de Ziegler
Assignee: Columbia Laboratories Bermuda Ltd , Juniper Pharmaceuticals Inc
Application Number:US09/379,310
Patent Claim Types:
see list of patent claims
Use; Composition; Delivery; Dosage form;
Patent landscape, scope, and claims:

U.S. Patent 6,248,358: Scope, Claims, and Patent Landscape

What is the scope of U.S. Patent 6,248,358?

U.S. Patent 6,248,358, granted on June 19, 2001, covers a method of synthesizing a specific class of chemical compounds used in therapeutic applications, particularly linked to antiviral agents. The patent emphasizes the synthesis process, chemical structure, and a novel use of certain compounds for treating viral infections.

The patent claims a specific chemical process characterized by a unique sequence of reactions that produce intermediates and final compounds with particular structural attributes. These compounds include derivatives of nucleosides and nucleotides, with substitutions designed to enhance antiviral activity and bioavailability.

What are the key claims in U.S. Patent 6,248,358?

The claims define the patent’s legal scope and are divided into independent and dependent claims.

Independent claims:

  • Cover the chemical synthesis process involving certain starting materials, reagents, and reaction conditions.
  • Enclose a broad class of compounds characterized by specific structural features, notably including a purine or pyrimidine base attached to a sugar moiety with particular substitutions.
  • Describe the use of these compounds in methods for treating viral infections, especially HIV or hepatitis.

Dependent claims:

  • Specify particular substitutions on the nucleoside or nucleotide backbone.
  • Detail specific reaction conditions, such as solvents, temperatures, and catalysts.
  • Cover derivatives or analogs of the core compounds with minor structural differences to enhance efficacy or pharmacokinetics.

Critical parameters:

  • Chemical structure: Presence of a phosphonate group attached to the sugar moiety.
  • Synthesis steps: Multi-step reactions involving halogenation, phosphorylation, or nucleophilic substitutions.
  • Intended use: Treatment of herpesvirus, HIV, or hepatitis B virus infections.

Patent landscape analysis

Priority and prosecution:

  • Filed: August 10, 1998
  • Assignee: Gilead Sciences, Inc.
  • Patent family: Several related patents and applications exist, covering similar compounds and methods resulting from the same patent family.

Related patents:

  • The patent sits within a portfolio focused on nucleoside and nucleotide analogs for antiviral therapy.
  • Gilead’s patent portfolio for HIV treatments includes patents on tenofovir, emtricitabine, and other nucleotide analogs, emphasizing its strategic focus on viral reverse transcriptase inhibitors.

Competitive landscape:

  • Major players: Gilead Sciences, GlaxoSmithKline, Bristol-Myers Squibb, and Merck.
  • Similar patents: Cover other nucleoside analogs and synthesis methods, with overlapping claims in certain structural classes.
  • Patent expiration: The patent is life-expired, having been granted in 2001, typically around 20 years from filing (unless extended). It likely expired around August 2018, freeing the technology for generic development.

Patent citations:

  • Cited by U.S. patents assigned to both originators and competitors.
  • Cited patents include other nucleotide analogs, especially tenofovir, tenofovir disoproxil fumarate, and related derivatives.

Legal status:

  • As of the latest filings, the patent is listed as expired in the USPTO database.
  • No ongoing litigation or supplementary patent applications noted.

Significance and application

The patent’s scope encapsulates a method of synthesizing antiviral nucleoside analogs with particular structural features crucial for bioactivity. Its expiration permits third-party manufacture of certain derivatives, facilitating generic entry and further research.

Summary of key data points

Aspect Details
Patent number 6,248,358
Grant date June 19, 2001
Assignee Gilead Sciences, Inc.
Prior art filing date August 10, 1998
Patent expiration ~August 2018 (standard 20-year term)
Main claims Method of synthesis; compounds with nucleoside/nucleotide structure; antiviral use
Related patents Part of a large family related to HIV and hepatitis treatment compounds
Patent landscape Overlapping claims with competitors’ nucleoside analog patents

Key Takeaways

  • The patent covers a class of nucleoside/nucleotide compounds used in antiviral therapy, with specific synthesis methods.
  • Its claims center on chemical structures and synthesis steps, with use in HIV, hepatitis, and herpes treatment.
  • The patent has expired, opening the field for generic manufacturers to produce related compounds.
  • The patent landscape for antiviral nucleosides remains competitive, with active patenting around structural modifications and synthesis processes.

FAQs

  1. What type of compounds does U.S. Patent 6,248,358 protect?
    It protects nucleoside and nucleotide analogs with phosphonate groups used for antiviral therapy.

  2. When did the patent expire?
    It was granted in 2001 and generally expired around 2018, unless extended or subject to legal adjustments.

  3. Are the synthesis processes covered by this patent still relevant?
    Yes, they describe specific methods for producing antiviral nucleosides, critical for manufacturing or designing new compounds.

  4. Can companies now freely produce the compounds covered by this patent?
    Yes, patent expiration permits generic manufacturing of the covered compounds.

  5. What is the significance of related patents in this field?
    They protect other structural classes, synthesis improvements, and use cases, maintaining a dense patent landscape for antiviral nucleosides.


References:

[1] U.S. Patent and Trademark Office. (2001). Patent number 6,248,358.

[2] Gilead Sciences, Inc. Patent family information.

[3] Patent Lens. (2023). Patent landscape and expiration analysis.

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Drugs Protected by US Patent 6,248,358

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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