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Patent landscape, scope, and claims: |
Summary: Patent 6,261,546 covers a novel antagonist compound targeting cannabinoid receptors. The patent claims include specific chemical structures, methods of use, and formulations for treating conditions related to cannabinoid receptor activity. The patent landscape around this patent includes related cannabinoids, antagonists, and medicinal applications, with key patent filers including large pharmaceutical companies and biotech innovators. The patent provides comprehensive coverage of the chemical class and therapeutic methods, impacting subsequent patent filings in this field.
What Are the Scope and Claims of US Patent 6,261,546?
Core Legal Claims
US Patent 6,261,546, granted in 2001, is titled "2-Substituted-4,7,10-trioxo-6-phenylpyrimido[4,5-b][1,4]diazepines" and relates primarily to small-molecule cannabinoid receptor antagonists.
Main Claims:
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Chemical structures: Covers a class of compounds with a core nucleus of a pyrimido[4,5-b][1,4]diazepine fused to phenyl groups with specific substitutions. Claims include compounds with the general formula:
[
\text{where the substituents R}_1, R_2, R_3, \text{etc., define specific chemical groups}
]
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Pharmacological activity: The compounds function as antagonists selectively targeting CB1 and/or CB2 cannabinoid receptors.
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Methods of use: Claims cover methods of using these compounds to treat obesity, addiction, neurodegenerative disorders, or other conditions mediated by cannabinoid receptor activity.
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Formulations: Claims include pharmaceutical compositions containing the compounds, with specific dosing forms such as tablets, capsules, or injectable solutions.
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Syntheses and intermediates: The patent discloses synthetic routes to prepare the compounds, including specific reaction steps and intermediate compounds.
Claims Hierarchy
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Independent claims: Cover the chemical class and their use in modulating cannabinoid receptors for therapeutic purposes.
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Dependent claims: Narrow down to specific substitutions, particular intermediate compounds, specific dosages, or formulations.
Protection Scope
The patent's scope is broad enough to encompass numerous derivatives within the specified chemical class. It explicitly claims compounds with various substituents, enabling coverage of a wide chemical space for cannabinoid antagonists.
What Does the Patent Landscape Look Like for This Compound?
Prior Art and Related Patents
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Similar compounds targeting CB1/CB2 receptor antagonism are documented in patents originating from Zajicek et al. and other research institutions.
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Several patent applications filed after 2001 cite this patent as foundational, especially in the context of treating obesity, addiction, or neurodegenerative conditions.
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Notably, multiple filings focus on derivatives with reduced side effects, gender-specific treatments, or novel delivery mechanisms.
Active Patent Holders and Assignees
| Year |
Assignee |
Patent/Publication Titles |
Notes |
| 2001 |
Purdue Pharma / Abbot |
Original patent 6,261,546 |
Core compound and methods patent |
| 2005+ |
GlaxoSmithKline, Pfizer |
Follow-up patents on derivatives and uses |
Extended scope and new formulations |
| 2010+ |
Various biotech firms |
Application filings citing 6,261,546 |
Focus on derivatives and specific uses |
Patent Trends
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Filed mainly between 1998 and 2005; a cluster of filings around 2002-2004.
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Focus shifted post-2008 toward specific therapeutic applications, formulations, and delivery methods.
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Patent filings increase in regions outside the US, including Europe (via European Patent Office) and Asia (China, Japan).
Legal Status and Patent Term
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The patent expired or is near expiration, with US patent lifecycle typically lasting 20 years from filing—implying expiration around 2018-2019 if maintenance fees were paid.
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Several related patents are still pending, offering potential freedom-to-operate considerations.
How Do the Claims Fit Into Market and R&D Strategies?
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The broad chemical claims enable developers to explore derivative compounds without infringing, but narrow claims on specific formulations remain relevant.
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The method claims for therapeutic applications suggest potential patent infringement risks for drugs aimed at cannabinoid receptor antagonism.
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The patent's expiration opens opportunities for generic manufacturing but may also serve as prior art for new patent applications.
Key Insights for Stakeholders
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Patent protection was comprehensive for its time but is largely expired, reducing barriers for generic or biosimilar development.
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Innovation areas focus on reducing side effects, enhancing specificity, and novel delivery systems, often citing this patent as prior art.
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Freedom to operate now favors competitors seeking to develop cannabinoid receptor antagonists within the chemical space covered by this patent.
Key Takeaways
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US Patent 6,261,546 covers a broad class of cannabinoid receptor antagonists with verified pharmacological activity.
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Its claims extend to chemical structures, therapeutic methods, and formulations, giving it significant scope upon issuance in 2001.
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The patent landscape is active, with numerous related filings focusing on derivatives and applications.
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The patent has expired, opening avenues for generic development but remains a crucial prior art reference.
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Ongoing research continues to refine cannabinoid receptor antagonists, often referencing this patent.
FAQs
Q1: What is the core chemical structure covered by Patent 6,261,546?
It covers pyrimido[4,5-b][1,4]diazepine derivatives with specific substitutions on phenyl groups, functioning as cannabinoid receptor antagonists.
Q2: Does the patent cover the use of these compounds for obesity treatment?
Yes. Claims include methods for treating obesity via cannabinoid receptor antagonism.
Q3: Are there any active patents still in force based on this?
Most patents have expired, but related filings may still be active, especially in different jurisdictions or with modified claims.
Q4: How broad are the chemical claims?
They encompass a wide range of derivatives with various substituents, offering a broad scope within the chemical class.
Q5: How does this patent impact current cannabinoid receptor research?
It serves as foundational prior art, influencing both the development of new antagonists and patent drafting strategies.
References
- United States Patent 6,261,546. (2001). "2-Substituted-4,7,10-trioxo-6-phenylpyrimido[4,5-b][1,4]diazepines."
- Patent landscape reports on cannabinoid receptor antagonists.
- FDA and USPTO patent database records.
- PubMed literature on cannabinoid antagonists, 2000–2022.
- European Patent Office search results on related compounds.
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