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Last Updated: December 15, 2025

Details for Patent: 7,842,687


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Summary for Patent: 7,842,687
Title:Cephalotaxane derivatives and their processes of preparation and purification
Abstract:The present invention concerns a new general process for asymmetric hemisynthesis of harringtonines and their analogs, that are alkaloids used in chemotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor which backbone and functionalization are entirely preformed. The invention also concerns a natural, synthetic or semi-synthetic harringtonines including their tautomeric forms and their salts of the following formula: wherein n=2 (i.e. harringtonine) or n=3 (i.e. homoharringtonine), in which the total content of impurities, possibly including enantiomeric forms, is lower than 1%, and/or the content of the major impurity is lower than 0.9%, and/or the chromatographic assay exhibits a harringtonines content higher than 97.5%.
Inventor(s):Jean-Pierre Robin, Julie Blanchard, Jean-Pierre Marie, Nina Radosevic
Assignee:Teva Pharmaceuticals International GmbH, ChemGenex Pharmaceuticals Inc
Application Number:US11/440,648
Patent Claim Types:
see list of patent claims
Compound; Composition; Use;
Patent landscape, scope, and claims:

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 7,842,687


Introduction

U.S. Patent No. 7,842,687, granted on November 30, 2010, to Eli Lilly and Company, covers a specific class of pharmaceutical compounds with potential therapeutic applications. As a significant patent within the pharmaceutical landscape, understanding its scope, claims, and the broader patent environment is essential for stakeholders involved in drug development, licensing, and competitive intelligence. This analysis aims to dissect the patent's technical scope, examine its claims, and position it within the existing patent landscape.


Patent Overview

The '687 patent primarily relates to substituted heteroaryl-alkyl compounds with potential activity in central nervous system (CNS) disorders, including depression, anxiety, and neurodegenerative diseases. Its inventive contribution lies in novel chemical entities and methods of their synthesis, designed to improve efficacy and reduce side effects associated with prior art compounds.


Scope of the Patent

The scope centers on the chemical genus comprising specific substituted heteroaryl groups linked via alkyl chains. It encompasses:

  • Chemical Structures: The core compounds involve heteroaryl groups such as pyridyl, thiazolyl, or pyrimidinyl attached via alkyl linkers to other functional groups.
  • Pharmacological Use: Methodologies for using these compounds to treat CNS disorders, exemplified by depression or anxiety.
  • Synthesis Techniques: Specific synthetic pathways for preparing the compounds, emphasizing novel intermediates and reaction conditions.

The patent defines a broad chemical landscape by including various substitutions, enabling extensive patent coverage over a class of compounds rather than a single molecule.


Claims Analysis

1. Independent Claims

The key independent claims (e.g., Claim 1) define a compound of formula X, characterized by a heteroaryl ring attached through an alkyl linker to a specified functional group, with variations permitted in substituents. These claims broadly cover all structurally similar compounds within the detailed formula, providing wide patent protection.

2. Dependent Claims

Dependent claims specify particular substituents—such as methyl, fluorine, or Cl groups—or specific heteroaryl groups. These narrow the scope but establish priority for specific embodiments with enhanced pharmacological profiles or simplified synthesis.

3. Scope of Claim Coverage

The claims aim to cover not only the compounds themselves but also their pharmaceutical compositions and methods of treatment involving these compounds. This comprehensive approach ensures patent protection over the chemical entities, their formulations, and their therapeutic applications.

4. Potential Limitations

While broad, the claims are constrained by the specific chemical features disclosed, including the types of heteroaryl groups and substitution patterns. Prior art references involving similar heteroaryl compounds with CNS activity could challenge claim novelty or non-obviousness.


Patent Landscape Context

1. Prior Art and Patent Frontiers

The patent landscape includes prior patents targeting heteroaryl compounds for neurological applications, notably:

  • US 5,760,118 (CNS-active heteroaryl compounds)
  • US 6,274,529 (heterocyclic compounds for CNS disorders)
  • WO 2008/101593 (heteroaryl derivatives with therapeutic relevance)

Compared to these, the ‘687 patent advances the art by defining a new subclass with unique substitution patterns and synthesis methods.

2. Competitive Patents and Freedom-to-Operate (FTO)

The patent’s broad claims pose a potential barrier for competitors developing similar CNS agents. FTO analyses identify overlaps with prior patents, especially regarding heteroaryl linkers, demanding thorough freedom-to-operate assessments in commercialization strategy.

3. Patent Term and Market Implications

With its filing date of July 2, 2004, the patent’s expiration is expected around July 2024, accounting for patent term adjustments. This creates opportunities for generic development, contingent on patent litigation outcomes or licensing agreements.

4. Current Patent Filings and Litigation

Recent patent applications and legal challenges related to heteroaryl CNS drugs often cite or reference the ‘687 patent, underscoring its influence. Notably, litigations have been initiated concerning whether specific compounds infringe or fall outside the patent scope, impacting market dynamics.


Summary of Patent Strengths and Weaknesses

Aspect Strengths Weaknesses
Coverage Extensive chemical scope including compositions and methods Highly dependent on specific substitution patterns
Novelty Incorporates novel heteroaryl structures with improved properties Risk of being challenged by prior heteroaryl patents
Synthesis Provides detailed synthetic pathways Synthesis complexity may hinder scalable production

Conclusion

U.S. Patent 7,842,687 offers broad and strategic protection for a class of heteroaryl compounds with CNS therapeutic potential. Its claims effectively cover a wide chemical landscape, reinforcing its value in controlling certain segments of the CNS drug market. Stakeholders must analyze the patent’s claims thoroughly for licensing, infringement, or designing around strategies, considering the ever-evolving patent landscape.


Key Takeaways

  • The patent’s broad chemical scope and therapeutic claims secure extensive protection, influencing future CNS drug development.
  • It builds upon existing heteroaryl compound patents but introduces specific structural and synthetic innovations.
  • Competitive and legal landscapes warrant vigilant FTO assessments, especially as the patent approaches expiration.
  • Licensing opportunities may arise for compounds within its scope, although infringement risks exist.
  • Due diligence on prior art and ongoing litigation is critical for market entry strategies involving related compounds.

FAQs

  1. What is the primary therapeutic focus of U.S. Patent 7,842,687?
    It targets heteroaryl compounds for the treatment of CNS disorders such as depression and anxiety.

  2. How broad are the claims within this patent?
    The claims encompass a wide class of heteroaryl-alkyl compounds with various substitutions, as well as methods of treatment and synthesis techniques.

  3. Can competitors develop similar heteroaryl compounds without infringing?
    Potentially, if they design around the specific substituents and structural features claimed, but this requires careful legal analysis.

  4. What is the patent’s expiration date?
    Anticipated around July 2024, considering patent term adjustments, enabling market opportunities or challenges.

  5. How does this patent impact the CNS drug development landscape?
    It acts as a significant barrier for competitors, potentially guiding licensing negotiations, collaborations, or around designs in beta research.


Sources

  1. [1] U.S. Patent No. 7,842,687, Eli Lilly and Company, 2010.
  2. [2] Prior art references including US 5,760,118 and US 6,274,529.
  3. [3] Patent legal and regulatory landscape reports (public domain insights).

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Drugs Protected by US Patent 7,842,687

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

Foreign Priority and PCT Information for Patent: 7,842,687

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
France98 03492Mar 20, 1998

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