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Patent landscape, scope, and claims: |
Scope, Claims, and Patent Landscape of U.S. Patent 6,103,262
What Are the Patent’s Core Claims and Scope?
U.S. Patent 6,103,262, granted to Eli Lilly and Company in August 2000, covers a class of compounds characterized as substituted 4-(3H)-quinazolinones. These compounds are disclosed for their utility as kinase inhibitors, particularly targeting epidermal growth factor receptor (EGFR) and related receptor tyrosine kinases.
Main Claim Categories:
- Chemical Skeleton: The patent claims compounds with a quinazolinone core structure substituted at specific positions. General structure focuses on a 4-quinazolinone scaffold with various R groups at designated positions, notably on the 2-, 4-, and 7-positions.
- Substituent Variability: The claims encompass a broad range of substituents, including alkyl, aryl, heteroaryl, and heterocyclic groups, attached via specified positions, which define the scope of potential chemical variations.
- Pharmacological Use: The patent claims compounds for use as kinase inhibitors, with specific mention of treatment of proliferative disorders, such as cancer, and inflammatory conditions.
Claims Breakdown:
- Claim 1: Defines a compound with a specific quinazolinone structure, with variable substituents at R1, R2, R3, and R4, where R groups can be hydrogen, alkyl, aryl, or heteroaryl groups.
- Dependent Claims: Narrow the scope, specifying particular R groups, such as methyl or phenyl, or particular substitutions that increase potency or selectivity for EGFR.
- Method Claims: Cover methods of use for treating diseases associated with abnormal kinase activity, specifically by administering compounds within the claimed class.
The scope covers a broad chemical space while focusing on kinase inhibition relevant to cancer therapy.
Patent Landscape and Related Patents
Related Litigation and Licensing
- The patent has been referenced in multiple patent families related to kinase inhibitors, especially those targeting EGFR.
- It has experienced licensing and legal challenges mainly centered on its broad claims, with some patent offices questioning the scope of its claims during prosecution of subsequent applications.
Competitors and Follow-On Patents
- Several pharmaceutical companies filed patent applications for similar quinazolinone derivatives or focused on specific substitutions to improve pharmacokinetics, potency, or selectivity.
- Notable patents include:
- U.S. Patent 6,582,734: Covers specific quinazoline derivatives with enhanced kinase inhibitory activity.
- U.S. Patent 7,070,926: Focuses on formulations and specific substituted quinazolinones with improved bioavailability.
- International filings: Similar families filed within Europe (EP patents) and Japan, indicating global patent strategies.
Patent Expiry and Market Implications
- The patent was filed in 1998 and granted in 2000, with a standard 20-year term, expiring around August 2018, subject to patent term adjustments.
- Its expiration opens the space for generic manufacturers to develop competing products, provided they do not infringe remaining patent rights or exclusivities.
Patent Filing Strategies
- Original patent aimed to secure broad coverage across multiple variations of quinazolinone compounds, consistent with pharmaceutical filings in the late 1990s.
- Follow-up applications targeted narrower claims or formulations, a common strategy to extend patent life or carve out specific market niches.
Implications for R&D and Market Entry
- The broad scope of originally granted claims potentially blocks competitors from developing similar kinase inhibitors unless they design around the patent.
- The expiry allows generic development but must consider secondary patents and regulatory data exclusivities.
- Companies developing next-generation kinase inhibitors often reference or design around this patent's scope, focusing on different scaffolds or substitution patterns.
Summary
U.S. Patent 6,103,262 covers a broad class of substituted quinazolinone compounds as kinase inhibitors, with claims spanning chemical structures and therapeutic uses. It has influenced a landscape populated by follow-up patents aimed at optimizing these compounds for clinical use. Its expiry in 2018 cleared the way for generics but left a complex patent estate surrounding kinase inhibitors in the same therapeutic space.
Key Takeaways
- The patent's broad chemical claims initially limited competitors' design space but are now mostly expired, enabling generic development.
- Follow-up patents have refined the chemical space or focused on specific formulations, but many of these are narrower.
- Significant patent filings globally focus on similar compounds, extending patent protections or creating landscape barriers.
- Litigation and licensing activities have shaped the commercial importance of the patent.
- Patent expiration coincides with increased generic opportunities in EGFR kinase inhibitor markets.
FAQs
1. Can new kinase inhibitors that differ from the compounds claimed in U.S. patent 6,103,262 avoid infringement?
Yes, if they do not fall within the structural or functional scope of claims, especially if they use different scaffolds or substitution patterns.
2. Are there existing patents that extend beyond the expiration of U.S. patent 6,103,262?
Yes, follow-on patents exist that cover specific derivatives, formulations, or uses, some of which may still be in force.
3. What diseases are targeted by compounds in this patent?
Primarily cancers driven by abnormal kinase activity, such as non-small-cell lung cancer (NSCLC) associated with EGFR mutations.
4. How has patent law affected the scope of this patent’s claims?
Legal challenges and examiner rejections during prosecution led to some narrowing of claim scope, though the original claims remained broad.
5. Does the patent landscape include international protections?
Yes, similar patent families have been filed in Europe, Japan, and other jurisdictions, extending the patent coverage globally.
References
- U.S. Patent 6,103,262. (2000). Quinazolinone derivatives as kinase inhibitors. Eli Lilly and Company.
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