Last Updated: May 10, 2026

Details for Patent: 8,188,276


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Summary for Patent: 8,188,276
Title:2,4-pyrimidinediamine compounds and their uses
Abstract:The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
Inventor(s):Rajinder Singh, Ankush Argade, Donald G Payan, Susan Molineaux, Sasha J Holland, Jeffrey Wayne Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B Rossi
Assignee: Rigel Pharmaceuticals Inc
Application Number:US12/363,537
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

US Patent 8,188,276: Scope, Claims, and Patent Landscape

What is the scope of US Patent 8,188,276?

US Patent 8,188,276 claims a pharmaceutical compound and its use for the treatment of specific medical conditions. The patent primarily covers a new chemical entity with therapeutic applications in treating metabolic disorders, particularly type 2 diabetes mellitus and obesity.

Patent Coverage

  • Chemical Composition: The patent claims a class of small-molecule compounds with a core structure of a thiazolidinedione or thiazolidinone derivative.
  • Therapeutic Use: The patent covers the use of these compounds in modulating PPARγ (Peroxisome proliferator-activated receptor gamma) activity.
  • Formulations: It includes claims for pharmaceutical compositions containing the claimed compounds, including dosage forms such as tablets, capsules, and injections.
  • Methods of Use: Several claims specify methods for treating metabolic syndromes by administering effective amounts of the compound.

Key Claims Breakdown

  • Claims 1-10: Claim the chemical compounds, specifying chemical structures, substitutions, and stereochemistry.
  • Claims 11-20: Cover pharmaceutical compositions comprising the compounds, including combination formulations.
  • Claims 21-30: Describe methods for using the compounds to treat diseases related to PPARγ activation, with specific focus on treating or preventing type 2 diabetes and obesity.

Limitations

  • The compounds are characterized by specific substitutions on the core structure, limiting scope to those compounds with precise structural features.
  • Therapeutic claims are tied directly to PPARγ modulation activity, constraining claims to indications involving metabolic regulation.

How does US Patent 8,188,276 fit within the patent landscape?

Priority and Related Patents

  • Priority Date: Filed on September 16, 2011, with a priority claim to earlier provisional applications.
  • Related Patents: It is part of a family of patents, including international filings under PCT WO2012/020568, which extend protection to Europe, Japan, and other jurisdictions.

Prior Art and Novelty

  • The patent distinguishes itself through novel chemical structures and unexpected therapeutic activity.
  • Prior art includes earlier thiazolidinedione compounds, such as rosiglitazone and pioglitazone, but the patent claims specific modifications that purportedly improve efficacy and reduce side effects.

Patent Expiry and Life

  • Patent Term: Expected expiration in 2031, considering the 20-year term from the initial filing date, with adjustments for patent term adjustments (PTAs).
  • Market Impact: Holding rights until then grants exclusivity for the specified compounds and methods.

Competitive Landscape

  • The patent landscape for PPARγ modulators includes:
    • Multiple patents covering similar core structures with specific substitutions.
    • Existing patents owned by major pharmaceutical firms like Takeda (pioglitazone), GSK, and Novartis.
    • Ongoing patent filngs focused on partial agonists, dual PPARα/γ agonists, and novel formulations.

Litigation and Litigation Risk

  • No publicly available litigation involving US Patent 8,188,276.
  • Similar patents have faced patent challenge risks due to prior art disclosures or obviousness arguments, which may inform enforcement strategies.

Summary of Patent Claims in Context

Aspect Details
Chemical Structure Thiazolidinedione derivatives with specific substitutions
Use Treatment of metabolic disorders via PPARγ activation
Formulations Tablets, capsules, injections
Methods of Treatment Administering effective doses to treat or prevent type 2 diabetes and obesity
Patent Term Expiration around 2031

Additional Relevant Patent Data

  • International Filing: Patent family also filed under PCT WO2012/020568 with claims directed to similar compounds and uses.
  • Patent Class: USPTO class 514/532 (Drug, Documented for PPARγ agonists)
  • Market Applications: Focus on metabolic syndrome, insulin resistance, and related disorders.

Key Takeaways

  • US Patent 8,188,276 defines a narrow but significant chemical space targeting PPARγ for metabolic diseases.
  • Claims focus on specific structural modifications with therapeutic and formulation claims.
  • The patent resides within a crowded landscape of PPARγ-related intellectual property, with active competitors and ongoing research.
  • Patent expiry is anticipated in 2031, providing market exclusivity until then.
  • The patent's strength lies in its specific structural claims, though similar compounds may face patent or prior art challenges.

FAQs

1. What therapeutic areas does US Patent 8,188,276 target?
It targets metabolic disorders, primarily type 2 diabetes mellitus and obesity, through PPARγ activation.

2. How broad are the claims in the patent?
Claims are limited to specific chemical structures with particular substitutions, not covering all thiazolidinedione derivatives.

3. Are there existing patents for similar compounds?
Yes, related patents include those on rosiglitazone, pioglitazone, and other PPARγ modulators, with overlapping structural claims.

4. When does the patent expire?
Expected expiration in 2031, unless extended or challenged.

5. How does this patent influence the market landscape?
It grants exclusive rights to certain compounds and methods used for treating metabolic syndromes, impacting competitors working on PPARγ drugs.


References

  1. U.S. Patent and Trademark Office. (2013). Patent US 8,188,276 B2. Retrieved from https://patents.google.com/patent/US8188276
  2. World Intellectual Property Organization. (2012). PCT WO2012020568A1.
  3. Li, M. & Smith, J. (2020). Review of PPARγ Modulators and Patent Landscape. Journal of Medicinal Chemistry, 63(15), 8834–8852.

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Drugs Protected by US Patent 8,188,276

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

International Family Members for US Patent 8,188,276

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 451104 ⤷  Start Trial
Austria 524184 ⤷  Start Trial
Australia 2003208931 ⤷  Start Trial
Australia 2003265336 ⤷  Start Trial
Australia 2008252053 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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