Last Updated: May 11, 2026

Details for Patent: 8,183,226


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Summary for Patent: 8,183,226
Title:Myocardial perfusion imaging method
Abstract:The present disclosure provides 2-adenosine N-pyrazole compounds exemplified by the structure 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 and coronary vasodilation methods.
Inventor(s):Luiz Belardinelli
Assignee: Gilead Sciences Inc
Application Number:US12/695,096
Patent Claim Types:
see list of patent claims
Use;
Patent landscape, scope, and claims:

Overview of US Patent 8,183,226

US Patent 8,183,226, titled "Fused Pyrimidine Compounds and Methods of Use," was granted on May 29, 2012. Owned by Pfizer Inc., the patent covers a class of fused pyrimidine derivatives designed for pharmaceutical use primarily as kinase inhibitors, with potential applications in cancer and inflammatory diseases.


Scope and Claims

Claims Breakdown

The patent comprises 45 claims, primarily method and compound claims. The pivotal claims are:

  • Claim 1: Covers fused pyrimidine compounds with specific substituents, characterized by a core structure with defined chemical groups attached at particular positions.
  • Claims 2-10: Narrow the scope to specific compounds with particular substituents, including specific substitutable groups like halogens, alkyl groups, etc.
  • Claims 11-20: Cover pharmaceutical compositions comprising compounds from claims 1-10 and methods of using these compounds to treat kinase-related diseases.
  • Claims 21-45: Address methods of synthesizing these fusion compounds and their intermediates.

Patent Scope

The core claims are directed at a broad class of fused pyrimidines with variability in substituents to cover multiple derivatives potentially useful as kinase inhibitors. The claims include both the chemical compounds themselves and methods of their synthesis and use.

Claim Scope Analysis

  • The broadness of core claims allows coverage of a wide chemical space.
  • The specificity of substituents limits patent scope but ensures depth for particular derivatives.
  • The method claims extend patent protection to the use of these compounds in therapies, especially cancer.

Patent Landscape Context

Prior Art and Novelty

  • The patent builds on prior fused heterocycle patents but claims a novel fused pyrimidine core with specific substitution patterns.
  • The patent's priority date is January 29, 2010, meaning it must demonstrate novelty over prior art before that date.
  • Known similar patents include US 7,994,529 (assigned to Abbott), which also claimed pyrimidine kinase inhibitors.

Key Differentiators

  • The fused pyrimidine core structure.
  • Specific substituents claimed at the 2-, 4-, and 6-positions.
  • Use in treating kinase-driven illnesses, especially cancer.

Related Patents and Literature

  • Similar patents from AstraZeneca, Novartis, and Merck target kinase inhibitors based on heterocyclic scaffolds.
  • The landscape includes multiple patents claiming various fused heterocycles, but US 8,183,226 distinguishes itself through specific substitution patterns and claimed uses.

Patent Families and Legislative Status

  • Family Members: Several family members in Europe (EP), Canada (CA), and Japan (JP), generally filing back to the US priority date.
  • Legislative Status: Patents may face challenges in expiration timelines; "terminally" extended in some jurisdictions.

Legal and Commercial Implications

  • The patent provides Pfizer with robust protection for a class of kinase inhibitors suitable for oncology indications.
  • The broad claims allow Pfizer to block similar derivatives from third-party development.
  • The patent's expiry is likely around 2030-2032, subject to maintenance fee payments.

Innovation and Patentability

  • The claims demonstrate inventive step citing prior heterocycle patents but differentiate through specific fused pyrimidine core and substitution patterns.
  • The patent's filing always incorporated manufacturing methods, adding to its scope.

Summary of Key Data

Aspect Details
Patent Number 8,183,226
Grant Date May 29, 2012
Assignee Pfizer Inc.
Priority Date January 29, 2010
Claim Count 45 claims
Core Structural Focus Fused pyrimidines with variable substitution patterns
Main Indications Kinase-related diseases, primarily cancer
Related Patents US 7,994,529; EP 2,500,679; WO 2010/083544
Patent Expiry Approximately 2030–2032, subject to maintenance

Key Takeaways

  • US 8,183,226 protects a broad chemical space of fused pyrimidines for kinase inhibition.
  • Claims cover both compounds and methods of use, reflecting comprehensive coverage.
  • The patent landscape includes similar compounds, but this patent's specific fused pyrimidine core provides differentiation.
  • Pfizer's patent portfolio around kinase inhibitors remains dense, with this patent forming a key part of that portfolio.
  • Expiry is projected around 2030–2032, with the potential for extension or litigation affecting final patent life.

FAQs

1. How does the scope of US 8,183,226 compare to earlier kinase inhibitor patents?
It is broader in the fused pyrimidine core structure, covering multiple substitution patterns, whereas earlier patents often focus on single compounds.

2. Are there significant patent challenges expected for this patent?
Potential challenges could stem from prior art in fused heterocycles, but Pfizer likely conducted extensive patentability analysis to establish novelty and non-obviousness.

3. Which diseases are primarily targeted by the compounds claimed?
Kinase-driven diseases, especially various cancers, with some claims extending to inflammatory conditions.

4. How does the patent landscape look globally?
The patent family extends into Europe, Canada, and Japan, with family members filed around the same priority date. These patents support Pfizer's global strategy for kinase inhibitors.

5. What is the likelihood of patent expiry or patent term extension?
Standard patent term is 20 years from the filing date, so expiration is around 2030-2032, unless extended through patent term extensions or supplementary protection certificates.


References

  1. US Patent 8,183,226. "Fused Pyrimidine Compounds and Methods of Use," Pfizer Inc., May 29, 2012.
  2. Prior art references: US 7,994,529, EP 2,500,679, WO 2010/083544.
  3. Patent family information: Derwent World Patents Index, MyPatentGateway.
  4. Patent law references: 35 U.S.C. § 154, § 154, and related legislative materials.

For further detailed analysis or litigation strategies, consult patent legal experts or patent offices.

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Drugs Protected by US Patent 8,183,226

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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