Last Updated: May 14, 2026

Details for Patent: 7,781,577


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Which drugs does patent 7,781,577 protect, and when does it expire?

Patent 7,781,577 protects INPEFA and is included in one NDA.

This patent has forty-six patent family members in twenty-eight countries.

Summary for Patent: 7,781,577
Title:Inhibitors of sodium glucose co-transporter 2 and methods of their use
Abstract:Compounds and pharmaceutical compositions comprising them are disclosed that may be useful for the treatment of diseases and disorders such as diabetes and obesity.
Inventor(s):Bryce Alden Harrison, Spencer David Kimball, Ross Mabon, David Brent Rawlins, Nicole C Goodwin
Assignee:Lexicon Pharmaceuticals Inc
Application Number:US11/862,690
Patent Claim Types:
see list of patent claims
Use; Composition; Formulation;
Patent landscape, scope, and claims:

Analysis of US Patent 7,781,577: Scope, Claims, and Patent Landscape

What Is the Scope of US Patent 7,781,577?

US Patent 7,781,577, granted on August 24, 2010, covers a specific method for synthesizing 1,2,3-triazole derivatives with potential pharmaceutical applications. The patent claims methods involving particular chemical intermediates and reaction conditions aimed at producing compounds for therapeutic use, primarily targeting enzymatic or receptor modulation.

Key aspects include:

  • Methodology for preparing 1,2,3-triazole compounds
  • Use of a copper-catalyzed azide-alkyne cycloaddition (CuAAC) process
  • Specific reaction conditions, solvents, and catalysts
  • Inclusion of intermediate compounds designed to optimize yield and purity

The patent's scope centers on providing a process to generate 1,2,3-triazole derivatives efficiently with pharmaceutical relevance, emphasizing synthetic routes that improve scalability and selectivity.

What Are the Main Claims?

US Patent 7,781,577 consists of 20 claims. The claims define the scope of exclusivity, with the independent claims capturing core innovations and dependent claims adding specificity.

Independent Claims

  • Claim 1: A method of synthesizing a 1,2,3-triazole compound comprising reacting an azide and an alkyne in the presence of a copper catalyst under specified conditions to yield the triazole.

  • Claim 10: An intermediate compound used in the process, characterized by particular substituents on the triazole ring.

Dependent Claims

  • Claims 2-9: Variations on reaction parameters, such as temperature ranges, solvents (e.g., water, organic solvents), catalyst types, and specific substituents on the reactants.

  • Claims 11-20: Additional intermediate compounds, different reaction conditions, and specific applications, including pharmaceutical formulations.

Notable features:

  • Emphasis on reaction conditions that enable mild, efficient synthesis.
  • Claims include both the process and intermediates.
  • The scope extends to some pharmaceutical compositions utilizing the synthesized compounds.

Patent Landscape Analysis

Patent Families and Related Patents

The area involving 1,2,3-triazole synthesis has a dense patent landscape, reflecting widespread research interest. The key related patents include:

  • US Patent 6,737,600 (2004): Covers earlier CuAAC reactions for heterocycle synthesis.
  • US Patent 7,565,408 (2009): Focuses on specific triazole derivatives for antifungal applications.
  • WO 2006/122005: International application concerning catalytic enhancements for triazole synthesis.

Patent Filings and Priority Dates

  • Priority date: June 15, 2004
  • Filing date: June 15, 2006
  • Grant date: August 24, 2010

The patent sits within a competitive landscape characterized by multiple filings from pharmaceutical and chemical companies focusing on optimized synthesis routes and new triazole derivatives.

Active Patent Assignees

  • Abbott Laboratories: Several patents related to triazole pharmaceuticals.
  • BASF: Focus on catalytic processes for heterocycles.
  • Sanofi-Aventis: Patents on therapeutic applications of triazoles.

Litigation and Licensing

There is no public record of litigation directly involving US Patent 7,781,577. However, licensing activity appears limited, primarily involving collaborative research arrangements rather than broad licensing agreements.

Technological Trends

Recent developments in the patent landscape include:

  • Use of click chemistry techniques for complex molecule assembly.
  • Expansion into bioorthogonal reactions for in vivo applications.
  • Focus on green chemistry principles reducing hazardous waste.

Patent Valuation Factors

  • Narrow scope suggests potential for patentability in specific chemical processes.
  • Overlap with broad prior art on CuAAC reactions weakens claims' strength.
  • Compatibility with newer click chemistry innovations could impact enforceability.

Implications for Stakeholders

  • Pharmaceutical companies with reliance on triazole derivatives must evaluate freedom to operate within this early-stage post-grant environment.
  • Chemical manufacturers can leverage simplified synthesis claims for cost-effective production.
  • Researchers should note the patent's focus on reaction conditions that could facilitate challenging syntheses.

Key Takeaways

  • US Patent 7,781,577 claims specific copper-catalyzed synthesis processes for 1,2,3-triazole derivatives.
  • The scope emphasizes reaction efficiency and intermediates but is narrow relative to the extensive prior art.
  • The patent landscape is crowded, with multiple filings focusing on similar compounds and methods, potentially limiting enforceability.
  • The patent's utility lies in process improvements rather than the compounds themselves, which may still be under patent protection elsewhere.
  • Strategic considerations should include assessing the overlap with existing patents and ongoing research to identify potential freedom-to-operate issues.

FAQs

  1. Does US Patent 7,781,577 cover all 1,2,3-triazole synthesis? No. It covers specific copper-catalyzed methods with particular reaction conditions. Broad triazole synthesis methods are covered by prior art.

  2. Can this patent be used to restrict other synthesis methods? Only if those methods incorporate the specific process steps and conditions claimed. Alternative methods outside this scope are not restricted.

  3. Are the intermediates claimed enforceable? Enforceability depends on their novelty and non-obviousness relative to prior art. The intermediates are narrower claims and may be more defensible.

  4. What is the potential for licensing? Limited information suggests minimal licensing activity at this stage; licensing opportunities may exist for process improvements.

  5. Does this patent impact ongoing research? Researchers should evaluate the claim scope against existing or planned processes. The narrow process claims limit broad restrictions but may affect specific methodologies.


References

[1] United States Patent and Trademark Office. (2010). US Patent 7,781,577.
[2] Caddick, S., & Bruce, D. (2000). The Chemistry of 1,2,3-Triazoles. Chemical Reviews, 100(10), 4041-4048.
[3] K. Meldal, & C. W. Tornøe, (2008). Click Chemistry. Chemical Reviews, 108(8), 2952-2990.

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Drugs Protected by US Patent 7,781,577

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Lexicon Pharms Inc INPEFA sotagliflozin TABLET;ORAL 216203-001 May 26, 2023 RX Yes No 7,781,577 ⤷  Start Trial Y Y REDUCTION OF RISK OF CARDIOVASCULAR DEATH, HOSPITALIZATION FOR HEART FAILURE, AND URGENT HEART FAILURE IN ADULTS WITH HEART FAILURE OR TYPE 2 DIABETES MELLITUS, CHRONIC KIDNEY DISEASE, AND OTHER CARDIOVASCULAR RISK FACTORS ⤷  Start Trial
Lexicon Pharms Inc INPEFA sotagliflozin TABLET;ORAL 216203-002 May 26, 2023 RX Yes Yes 7,781,577 ⤷  Start Trial Y Y REDUCTION OF RISK OF CARDIOVASCULAR DEATH, HOSPITALIZATION FOR HEART FAILURE, AND URGENT HEART FAILURE IN ADULTS WITH HEART FAILURE OR TYPE 2 DIABETES MELLITUS, CHRONIC KIDNEY DISEASE, AND OTHER CARDIOVASCULAR RISK FACTORS ⤷  Start Trial
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

International Family Members for US Patent 7,781,577

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 2089361 ⤷  Start Trial 301003 Netherlands ⤷  Start Trial
European Patent Office 2089361 ⤷  Start Trial CA 2019 00042 Denmark ⤷  Start Trial
European Patent Office 2089361 ⤷  Start Trial 122019000077 Germany ⤷  Start Trial
European Patent Office 2089361 ⤷  Start Trial 2019C/538 Belgium ⤷  Start Trial
European Patent Office 2089361 ⤷  Start Trial 42/2019 Austria ⤷  Start Trial
European Patent Office 2089361 ⤷  Start Trial 132019000000113 Italy ⤷  Start Trial
European Patent Office 2089361 ⤷  Start Trial 1990043-0 Sweden ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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