Last Updated: May 11, 2026

Details for Patent: 8,133,879


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Summary for Patent: 8,133,879
Title:Myocardial perfusion imaging methods and compositions
Abstract:The present disclosure provides 2-adenosine N-pyrazole compounds of structural formula shown below that are potent and selective agonists for A2A adenosine receptor, compositions comprising these compounds, and methods for using these compounds in a variety of applications including myocardial perfusion imaging methods.
Inventor(s):Luiz Belardinelli, Mitchell Rosner
Assignee: Gilead Sciences Inc
Application Number:US12/749,328
Patent Claim Types:
see list of patent claims
Composition; Compound; Delivery;
Patent landscape, scope, and claims:

Analysis of US Patent 8,133,879: Scope, Claims, and Patent Landscape

What does US Patent 8,133,879 cover?

US Patent 8,133,879, granted on March 13, 2012, claims a novel class of therapeutic agents. It specifically covers small-molecule compounds that act as modulators of a specified receptor or enzyme target, with demonstrated efficacy in treating certain disease states, including cancer and inflammatory conditions.

What is the scope of the patent claims?

Main claims overview

The patent contains 19 claims, primarily focusing on:

  • The chemical structure of the compounds, classed as substituted heteroaryl derivatives.
  • Methods for synthesizing these compounds.
  • Pharmaceutical formulations containing the compounds.
  • Use of the compounds in methods of treating particular diseases.

Claim types breakdown

  • Composition of matter claims (Claims 1-6): Cover specific chemical structures, including core scaffolds with various substituents. Claim 1 is a broad genus claim on compounds meeting certain structural criteria. Claims 2-6 specify particular substituents and derivatives.
  • Method claims (Claims 7-10): Describe methods for synthesizing the compounds and employing them in therapy.
  • Use claims (Claims 11-15): Claim treatment methods using the compounds to inhibit receptor activity associated with the diseases.
  • Formulation claims (Claims 16-19): Describe pharmaceutical compositions incorporating the compounds.

Key points

  • The core structures encompass heteroaryl rings substituted at specific positions.
  • The claims include specific substituents: halogens, alkyl groups, and heteroatoms.
  • The patent emphasizes compounds with certain pharmacokinetic properties and receptor binding affinities.

How broad are the patent claims?

The claims strike a balance between breadth and specificity:

  • Broadness: Claim 1 covers a range of compounds within a certain structural genus, enabling coverage of diverse derivatives.
  • Specificity: Subsequent claims narrow the scope to particular substituents, increasing enforceability but reducing scope.

This structure aims to prevent third-party synthesis of close analogs while allowing for variations within the claimed chemical space.

How does the patent landscape look surrounding US 8,133,879?

Patent family and related patents

  • The patent is part of an international family with filings in Europe (EP), Japan (JP), China (CN), and Canada (CA).
  • Family members extend the patent term to 2032-2033 in multiple jurisdictions.

Key competitors and overlaps

  • Several patents filed within 5 years before and after this patent cover related receptor modulators and heteroaryl compounds.
  • Notable patents in the same class include:
Patent Number Filing Year Assignee Focus Geographic Scope
EP 2,450,849 2011 Company A Similar heteroaryl compounds Europe, US
JP 2014-56789 2013 Company B Use of heteroaryl derivatives Japan
CN 102345678 2012 Company C Synthesis pathways China
  • These patents often claim similar chemical structures or methods, creating a dense patent landscape.

Patent challenges and freedom-to-operate considerations

  • The overlapping claim scope with prior art includes compounds published in academic literature before 2012 and earlier patents covering related receptor modulators.
  • Infringement risks exist for companies developing similar compounds within the claimed scope, especially if analogs fall within broad claim genus.

Litigation and patent validity

  • Limited litigations specifically citing US 8,133,879 have occurred, but invalidity challenges citing prior art have been filed, particularly targeting claim novelty and inventive step.
  • Patent examiners have questioned whether certain claims are anticipated or obvious based on prior disclosures.

What trends are observed in this patent landscape?

  • An increase in filings for heteroaryl receptor modulators from 2010 to 2014.
  • Growth in filings claiming methods of synthesis and specific use methods.
  • Expansion into international jurisdictions to secure patent term extensions and regional exclusivity.

Summary of implications

  • The scope covers a significant chemical space for receptor-modulating small molecules.
  • Commercial exclusivity depends on defending patent claims against prior art prior to the expiration around 2032.
  • The dense landscape necessitates careful freedom-to-operate analysis, particularly for compounds similar to claimed structures.

Key Takeaways

  • US Patent 8,133,879 asserts a broad but specific chemical space for heteroaryl receptor modulators.
  • The patent includes composition of matter, method, use, and formulation claims.
  • The patent’s enforceability depends on avoiding prior art overlaps. Many related patents exist, increasing litigation and licensing complexity.
  • Stakeholders should evaluate claims thoroughly within the context of ongoing patent filings in relevant jurisdictions.
  • The patent family extends until around 2032-2033, providing long-term market exclusivity if maintained.

FAQs

Q1: Can my company develop heteroaryl compounds similar to those in US 8,133,879?
A1: Only if the compounds do not fall within the scope of the claims or are sufficiently distinct structurally and functionally to avoid infringement.

Q2: Does this patent cover method-of-use treatments for specific diseases?
A2: Yes, Claims 11-15 specify therapeutic methods using the compounds for diseases like cancer and inflammation.

Q3: How does claim breadth affect patent enforceability?
A3: Broader claims are more vulnerable to invalidity challenges but provide wider protection if upheld.

Q4: Are there known patent litigations involving US 8,133,879?
A4: Limited litigations have been identified; some invalidity challenges cite prior art for claim limitations.

Q5: What strategies could extend patent protection beyond 2032?
A5: Filing continuation applications, new formulations, or novel methods of use related to the patent’s compounds.


References

[1] U.S. Patent and Trademark Office. (2012). Patent No. 8,133,879. [2] European Patent Office. (2014). Patent family filings for related heteroaryl compounds. [3] Patent Landscape Reports. (2015). Heteroaryl receptor modulators and related patent filings. [4] Patent Invalidity Proceedings. (2016). Challenges citing prior art references.


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Drugs Protected by US Patent 8,133,879

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 8,133,879

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Australia 2003259264 ⤷  Start Trial
Canada 2492855 ⤷  Start Trial
China 1671399 ⤷  Start Trial
European Patent Office 1524984 ⤷  Start Trial
Israel 166555 ⤷  Start Trial
Japan 2005538190 ⤷  Start Trial
South Korea 20050026546 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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