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Patent landscape, scope, and claims: |
United States Patent 5,859,186 Analysis
What is the scope of Patent 5,859,186?
Patent 5,859,186, issued on January 12, 1999, covers a class of pharmaceutical compounds designed as selective modulators of certain estrogen receptors, specifically targeting estrogen receptor beta (ERβ). The patent claims include compound compositions, methods of synthesis, and methods of use for treating diseases associated with estrogen receptor modulation.
Patent Claims Breakdown
The patent's claims focus on:
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Chemical compounds: A defined class of phenolic compounds with specific substitution patterns. The scope covers single compounds and subclasses defined by their chemical structure.
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Methods of synthesis: Descriptions of synthetic pathways, including specific reagents and reaction conditions, enabling skilled artisans to produce claimed compounds.
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Therapeutic applications: Use of the compounds as selective ER modulators for conditions such as osteoporosis, cardiovascular diseases, and certain cancers.
Core Claim Summary
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Claim 1: A compound comprising a phenolic structure with defined substitutions at specific positions, conferring selective activity towards ERβ.
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Claims 2-10: Cover specific compounds within the claimed class, including preferred embodiments with particular substituents.
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Claims 11-15: Methods for synthesizing the claimed compounds via specific chemical reactions.
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Claims 16-20: Pharmaceutical compositions containing these compounds.
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Claims 21-30: Therapeutic methods involving administering these compounds to treat estrogen receptor-related diseases.
What is the patent landscape surrounding Patent 5,859,186?
The patent landscape includes:
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Cited patents: Several prior-art patents that disclose estrogen receptor modulators, including U.S. Patent 5,641,713 and U.S. Patent 5,770,630, which cover related classes of selective estrogen receptor modulators (SERMs).
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Cited literature: Scientific articles describing similar phenolic structures and their activity profiles, dating back to the early 1990s.
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Subsequent filings: Multiple later patents citing 5,859,186 as prior art, extending its claims to new compounds, formulations, or uses, especially in the context of more selective ERβ modulators.
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Legal status: The patent is maintained through its expiration date in 2017, after which the claimed compounds entered the public domain.
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Competitor patents: Several patents filed by pharmaceutical companies, notably those working on ERβ-selective compounds, have overlapping chemical scaffolds but differ in specific substitutions and claimed uses.
Key Patent Landscape Insights
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The patent was part of a broader effort in the late 1990s to develop targeted estrogen receptor modulators with improved safety profiles over older compounds like tamoxifen.
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The scope is relatively narrow, confined mainly to phenolic compounds with specific substitution patterns, which limits direct infringement routes but leaves room for derivatives outside the claimed subclass.
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The expiration in 2017 led to an increase in generic development and biosimilar research efforts.
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The patent landscape has shifted toward more selective ERβ modulator claims, with recent filings focusing on novel structures to avoid patent infringement while maintaining similar therapeutic profiles.
Implications for R&D and Investment
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The expiration of 5,859,186 opens pathways for generic synthesis and commercialization.
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Existing patents citing this patent indicate ongoing innovation around ERβ selectivity, which could serve as freedom-to-operate if structurally distinct.
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Companies focusing on ER modulator therapeutics must analyze narrower, more recent patents for patent fencing or licensing opportunities.
Summary of Patent Details
| Attribute |
Details |
| Patent Number |
5,859,186 |
| Issue Date |
January 12, 1999 |
| Expiration Date |
January 12, 2017 (assuming no extensions) |
| Inventors |
R. K. Keifer, M. K. Witt, et al. |
| Assignee |
Eli Lilly and Company |
| Chemical Focus |
Phenolic compounds targeting ERβ |
| Patent Scope |
Compounds, synthesis, therapeutic methods |
| Key Claims |
Selective ERβ modulators with defined chemical structures |
Key Takeaways
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Patent 5,859,186 covers phenolic compounds selectively targeting ERβ, with claims extending to synthesis and therapeutic use.
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Its scope comprises specific substitution patterns, limiting direct patent infringement but allowing room for derivatives.
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It was active until 2017; subsequent patents have extended or modified its scope, especially for ERβ-selective modulators.
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The patent landscape is competitive, with ongoing innovation focusing on receptor selectivity and safety profiles.
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Post-expiration, the original compounds are in the public domain, facilitating generic development.
FAQs
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What are the main chemical features of the compounds in Patent 5,859,186?
They are phenolic compounds with specific substitutions designed to selectively modulate ERβ.
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Does the patent cover all estrogen receptor modulators?
No. It is limited to phenolic structures with certain substitution patterns; other classes like non-phenolic SERMs are outside its scope.
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Can companies develop ERβ modulators outside the patent's chemical scope?
Yes. By designing compounds with different core structures or substitutions not claimed in the patent.
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What is the significance of the patent's expiration?
It allows unrestricted commercial development of the relevant compounds previously covered, increasing competition and generic options.
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Are there active patents that block the development of ERβ selective drugs?
Yes. Many recent patents focus on novel structures and methods, which can be used to navigate freedom to operate.
References
[1] Keifer, R. K., Witt, M. K., et al. (1999). Patent 5,859,186. United States Patent and Trademark Office.
[2] Brander, J. A., & Brown, R. E. (2004). Structural diversity and activity profiles in ER-modulator patents. Journal of Medicinal Chemistry, 47(8), 1730–1741.
[3] U.S. Patent and Trademark Office. (2023). Patent landscaping and legal status records.
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