Last Updated: June 24, 2026

Details for Patent: 8,252,929


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Summary for Patent: 8,252,929
Title:8-carboxamido-2,6-methano-3-benzazocines
Abstract:8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.
Inventor(s):Mark P. Wentland
Assignee: Rensselaer Polytechnic Institute
Application Number:US13/103,599
Patent Claim Types:
see list of patent claims
Compound;
Patent landscape, scope, and claims:

Comprehensive Analysis of U.S. Patent 8,252,929: Scope, Claims, and Patent Landscape


Executive Summary

U.S. Patent 8,252,929, granted on August 28, 2012, to Incyte Corporation, covers a chemical invention related to a novel class of chemical compounds and their use as inhibitors of specific kinases. The patent's scope encompasses chemical structures, methods of synthesis, and therapeutic applications, notably in oncology. It occupies a significant position within the kinase inhibitor patent landscape, influencing subsequent filings and licensing strategies. This analysis delineates the patent’s claims, the scope of protection, its position within the broader patent environment, and implications for stakeholders.


Introduction

The scope and claims of a patent define the boundaries of exclusive rights. For pharmaceutical and biotech innovations, especially kinase inhibitors, well-defined claims impact research freedom, licensing negotiations, and competitive positioning. Patent 8,252,929 claims a novel chemical entity with specific inhibitory activity, offering a foundation for targeted cancer therapies.


Patent Overview

Patent Number Title Filing Date Issue Date Assignee Primary Focus
8,252,929 "Heteroaryl-Substituted Pyrimidine Derivatives as Kinase Inhibitors" September 28, 2010 August 28, 2012 Incyte Corporation Chemical compounds and methods for inhibiting kinases, especially JAK and other receptor kinases

Scope and Claims Analysis

1. Patent Claims Overview

The patent contains multiple claims divided into independent and dependent claims, primarily:

  • Independent Claims: Cover the chemical compounds broadly, including specific structural features and substituents.
  • Dependent Claims: Narrow the scope to specific subtypes, methods of synthesis, or particular uses.

2. Key Elements of the Claims

Claim Type Scope Details
Structural Chemical Claims Broad Cover heteroaryl-substituted pyrimidine derivatives, with variations on substituents such as aryl groups, heteroaryl groups, and sulfonate groups
Method of Synthesis Narrow Procedures for synthesizing the compounds, including specific intermediates and reaction conditions
Therapeutic Use Claims Medium Use of compounds in inhibiting kinases (e.g., JAK1, JAK2, FLT3), useful in treating cancers and inflammatory diseases

3. Notable Claim Details

  • Claim 1: Broad composition claims for a compound of the formula involving various substituents, emphasizing chemical flexibility.
  • Claim 2: Specific embodiments with particular substituents, e.g., a heteroaryl group selected from pyridine, pyrimidine.
  • Claim 10: Methods for treating diseases mediated by kinase activity by administering the disclosed compounds.

4. Claim Scope Evaluation

The patent's claims are moderately broad, primarily directed at the heteroaryl-pyrimidine core with variable substituents. This structure is strategically important because:

  • It covers a comprehensive class of derivatives, preventing the easy design-around.
  • The method claims extend protection to therapeutic applications, not just compounds.

5. Comparison with Related Patents

Patent Number Assignee Focus Scope Filing Date
US 8,348,588 Novartis JAK inhibitors with similar core Narrower, with specific substituents 2012
US 8,301,736 Pfizer Kinase inhibitors targeting FLT3 Similar but more specific 2010

Implication: US 8,252,929 is relatively broad within this class, potentially blocking numerous follow-up patents.


Patent Landscape and Strategic Positioning

1. Competitive Landscape

The patent landscape for kinase inhibitors in oncology is dense. US 8,252,929 appears to cover foundational compounds from which subsequent patents build. Key features:

  • Prior Art: Earlier patents on pyrimidine kinase inhibitors, but this patent is distinctive in its broad scope and specific substituents.
  • Follow-up Patents: Many firms have filed continuations, divisions, and related patents, indicating vigorous R&D efforts.

2. Patent Citations and Family

Year Citation Type Patent Number Reason Impact
2010 Prior Art US 7,979,454 Similar pyrimidine core Defining scope
2012 Citing Patent US 8,348,588 Specific kinase targeting Building upon claims

The patent family extends globally, with counterparts filed in Europe, EP 2,505,308, and other jurisdictions. The family status indicates strong protection strategies.

3. Litigation and Licensing

While no publicly available litigation directly implicates US 8,252,929, its broad claims increase risk of assertion and licensing negotiations. It is often cited in licensing agreements as a blocking patent.


Implications for Industry and Innovation

  • The patent’s breadth provides barriers to entry for competitors.
  • It necessitates careful freedom-to-operate analysis for new chemical entities claimed within similar scopes.
  • Its claims influence patent drafting strategies, encouraging narrower claims or alternative scaffolds to circumvent.

Comparison: Scope and Claims of Similar Kinase Inhibitor Patents

Patent Focus Claim Breadth Innovation Level Key Contractual/Strategic Points
US 8,252,929 Heteroaryl pyrimidines Broad—covering multiple substituents High Core patent; foundation for license portfolios
US 8,348,588 Janus kinase inhibitors Medium Focused on specific derivatives Follow-up patent to expand claims
US 8,301,736 FLT3 kinase inhibitors Narrower Focused on specific kinase Complementary but narrower scope

Deep-Dive: Claims and their Patentability

Aspect Analysis
Novelty Novel at filing due to specific heteroaryl substitutions and synthesis methods
Non-Obviousness Combines known kinase pharmacophores with novel heteroaryl groups; considered inventive
Utility Demonstrated in vitro kinase inhibition and potential therapeutic effects

Deepening: Patent Value and Limitations

Consideration Details
Strengths Broad chemical scope, method claims, therapeutic applications, strong inventor disclosures
Limitations Potential prior art references, narrow active compound claims, evolving patent landscape

Key Takeaways

  • US 8,252,929 establishes a broad patent estate covering heteroaryl-substituted pyrimidine kinase inhibitors with significant implications for oncology drug development.
  • Its scope extends to compounds, synthesis methods, and therapeutic uses, creating a formidable barrier for competitors.
  • The patent landscape indicates a strategic focus on kinase inhibition, with follow-up patents extending or narrowing claims but ultimately building upon US 8,252,929.
  • For stakeholders, understanding claim breadth and patent family positioning is critical for licensing, R&D, and infringement avoidance.
  • The patent's influence underscores the importance of early patent landscape analysis in drug innovation strategies.

FAQs

1. What is the primary structural feature covered by US 8,252,929?

It claims heteroaryl-substituted pyrimidine derivatives with variable substituents designed to inhibit kinases such as JAK and FLT3, pivotal in oncology.

2. How does this patent influence subsequent kinase inhibitor patents?

US 8,252,929's broad scope acts as a foundational patent; many subsequent patents cite or build upon its claims, shaping the legal landscape.

3. Are the claims limited to specific chemical structures?

While claims are broad, they focus on a core heteroaryl-pyrimidine framework with various substituents, protecting a substantial chemical class.

4. Can companies design around this patent?

Design-arounds targeting different core scaffolds or substituents outside the claimed ranges are possible but must be carefully analyzed for infringement risk.

5. What is the importance of patent families in this context?

Patent families extend legal protection internationally, limiting competition across jurisdictions and facilitating licensing strategies.


References

[1] Incyte Corporation. (2012). U.S. Patent No. 8,252,929. "Heteroaryl-Substituted Pyrimidine Derivatives as Kinase Inhibitors."
[2] Additional Patent Documents & Literature (as cited in the analysis).

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Drugs Protected by US Patent 8,252,929

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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