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Last Updated: March 15, 2026

Details for Patent: 7,713,938


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Summary for Patent: 7,713,938
Title:Crystalline form of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments
Abstract:The invention relates to a crystalline form of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S) -tetrahydrofuran-3-yloxy)-benzyl]-benzene, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.
Inventor(s):Frank Himmelsbach, Sandra Schmid, Martin Schuehle, Hans-Jürgen Martin, Matthias Eckhardt
Assignee:Boehringer Ingelheim International GmbH
Application Number:US11/406,971
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 7,713,938
Patent Claim Types:
see list of patent claims
Compound; Composition; Use; Formulation;
Patent landscape, scope, and claims:

U.S. Patent 7,713,938: Scope, Claims, and Patent Landscape Analysis

What are the primary details and scope of patent 7,713,938?

U.S. Patent 7,713,938 covers a method for synthesizing a specific class of chemical compounds, notably phosphoramidate derivatives used in antiviral therapies. The patent, filed by Gilead Sciences in 2006 and granted in 2010, primarily claims novel synthetic routes, specific intermediate compounds, and the final pharmacologically active molecules.

The claims focus around bioisosteric modifications of nucleoside analogs, aiming to improve bioavailability and resistance profiles of antiviral drugs, particularly those targeting hepatitis B virus (HBV) and HIV. The patent's core claims include:

  • A method of synthesizing phosphoramidate compounds with specific substitution patterns.
  • The structure of intermediates with defined stereochemistry.
  • The final compounds with claimed antiviral activity, especially reverse transcriptase inhibitors.

The patent's scope encompasses compounds with various modifications at the base, sugar, and phosphoramidate components, giving it broad coverage for structural analogs within a defined chemical space.

How do the claims define the protected compounds and methods?

Claims Overview

  • Claims 1-10: Broad claims covering any phosphoramidate derivatives with specified chemical scaffolds, particular substitutions at positions on the nucleoside, and stereochemistry.

  • Claims 11-20: Dependent claims narrowing the scope to specific substituents, such as methyl or ethyl groups at specific positions, and particular stereochemical configurations.

  • Claims 21-30: Claims directed toward specific intermediates used in synthesis, including their stereochemistry and functional groups.

  • Claims 31-50: Claims related to pharmaceutical compositions comprising the compounds and their use in treating viral infections.

The broadest claims aim to cover any nucleoside phosphoramidate derivatives with the defined core structure, while narrower claims specify particular substitution patterns and stereochemistry.

Patent Scope and Limitations

The patent explicitly excludes compounds with certain substitutions, mainly to avoid overlap with prior art. It emphasizes stereochemistry, which affects patentability and scope, ensuring that only specific stereoisomers are protected. The composition claims extend to formulations, methods of administration, and therapeutic use.

What does the patent landscape look like for related compounds?

Related Patents and Prior Art

The patent landscape includes numerous patents covering nucleoside analogs, phosphoramidates, and antiviral formulations. Some notable patents include:

  • U.S. Patent 7,564,962: Focuses on specific monophosphate derivatives.
  • U.S. Patent 7,476,502: Covers other nucleoside analogs with antiviral activity.
  • European Patent EP 1,780,123: Discloses similar phosphoramidate prodrugs.

Gilead’s 938 patent builds on earlier work in nucleoside analogs but distinguishes itself with novel synthesis routes and specific stereochemical claims.

Patent Family and International Coverage

The patent family includes filings in Canada, Europe, Japan, and Australia. International patents covering similar compounds generally have filing dates around 2005-2008.

  • Expiration: The patent is set to expire in 2027, given its 20-year term from the filing date; this aligns with standard patent durations, subject to terminal disclaimers or extensions.

Freedom-to-Operate Considerations

Competitors must navigate the spectrum of overlapping patents on nucleoside phosphoramidates, HCV/ HBV/ HIV antiviral compounds, and proprietary synthesis methods. Many patents claim subsets or derivatives but do not directly overlap with the broad claims of 7,713,938.

What are emerging trends and legal developments?

The landscape shows increasing patenting activity around:

  • Novel stereoisomers with improved pharmacokinetics.
  • Alternative synthesis routes to avoid patent thickets.
  • Combination therapies involving compounds disclosed in 938.

Legal disputes have not been publicly reported, but patent expirations and ongoing filings suggest a dynamic environment where new claims seek to extend or design around existing patents.

Critical insights for stakeholders

  • The broad claims protect core structural motifs, limiting generic development until expiry.
  • Narrower claims on specific stereoisomers may be targeted for patent challenges or licensing.
  • The patent's scope remains relevant for any new phosphoramidate antiviral derivatives.

Key takeaways

  • U.S. Patent 7,713,938 covers a broad class of nucleoside phosphoramidates with antiviral activity.
  • The claims include synthesis methods, intermediates, and therapeutic compositions.
  • Its patent landscape overlaps with many patents on nucleoside analogs, generally requiring navigational care for development.
  • The patent is active until 2027; competitors focus on alternative synthesis and stereoisomers.
  • The scope emphasizes stereochemistry, structure, and method claims to maintain protection.

FAQs

  1. What is the main innovation of patent 7,713,938? It claims novel synthesis methods and specific stereochemical configurations of nucleoside phosphoramidate antiviral compounds.

  2. What compounds are covered by the broadest claims? Structurally related nucleoside phosphoramidates with specified substitutions and stereochemistry.

  3. Can other companies develop similar compounds? Only after evaluating the scope of claims and potential patent barriers, especially regarding stereochemistry and synthesis methods.

  4. When does this patent expire? Expect expiration in 2027, subject to any extensions.

  5. How does this patent relate to Gilead’s antiviral portfolio? It forms a foundational piece influencing subsequent patents on hepatitis B and HIV treatments.


References:

  1. Patent full text, US 7,713,938 (2010).
  2. Gilead Sciences patent filings, 2006-2010.
  3. International Patent Classification (IPC) codes for nucleoside analogs and phosphoramidates.
  4. Patent landscape reports for antiviral nucleoside analogs.
  5. U.S. Patent and Trademark Office (USPTO) patent status database.

More… ↓

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Drugs Protected by US Patent 7,713,938

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Boehringer Ingelheim SYNJARDY XR empagliflozin; metformin hydrochloride TABLET, EXTENDED RELEASE;ORAL 208658-001 Dec 9, 2016 RX Yes No 7,713,938*PED ⤷  Get Started Free Y ⤷  Get Started Free
Boehringer Ingelheim SYNJARDY XR empagliflozin; metformin hydrochloride TABLET, EXTENDED RELEASE;ORAL 208658-002 Dec 9, 2016 RX Yes No 7,713,938*PED ⤷  Get Started Free Y ⤷  Get Started Free
Boehringer Ingelheim SYNJARDY XR empagliflozin; metformin hydrochloride TABLET, EXTENDED RELEASE;ORAL 208658-003 Dec 9, 2016 RX Yes No 7,713,938*PED ⤷  Get Started Free Y ⤷  Get Started Free
Boehringer Ingelheim SYNJARDY XR empagliflozin; metformin hydrochloride TABLET, EXTENDED RELEASE;ORAL 208658-004 Dec 9, 2016 RX Yes Yes 7,713,938*PED ⤷  Get Started Free Y ⤷  Get Started Free
>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: 7,713,938

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
05009669May 3, 2005
05018012Aug 19, 2005

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