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Patent landscape, scope, and claims: |
Scope, Claims, and Patent Landscape of U.S. Patent 4,695,392
What Is the Scope of U.S. Patent 4,695,392?
U.S. Patent 4,695,392, issued September 22, 1987, covers a novel class of compounds used as adrenergic agonists. It primarily claims substituted phenylethanolamines with specific substitutions at the 4-position of the aromatic ring, resulting in highly selective alpha-adrenergic receptor activity.
The patent emphasizes compounds' topological configurations, substituents on the phenyl ring, and their respective pharmacological profiles. It claims compounds with potential therapeutic application in vasoconstriction, hypotension, and related cardiovascular conditions. The scope extends to both the chemical compounds themselves and their pharmaceutical compositions.
What Are the Key Claims in U.S. Patent 4,695,392?
Core Claims
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Chemical Structure Claims
Cover compounds with a general formula:
[ \text{Ar—CH(OH)—R} ]
where Ar denotes a substituted phenyl group, and R is an organic radical with specific substitutions.
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Substituent Variations
Claims specify substitutions at the para position of the aromatic ring, such as halogens (fluorine, chlorine), alkyl groups, or nitro groups, which modulate receptor selectivity and activity.
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Pharmaceutical Composition Claims
Claims include formulations containing these compounds dissolved or dispersed in carriers suitable for injection or oral administration.
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Methods of Use
Includes methods for producing vasoconstriction or increasing blood pressure by administering effective doses of the compounds.
Limitations and Exclusions
- The scope explicitly excludes compounds outside the defined substituent range.
- The patent does not claim methods employing the compounds for non-vascular therapeutic areas.
Claim Specificity
The claims are narrow compared to broader adrenergic agent patents; they focus on specific phenylethanolamine derivatives with known receptor activity profiles, reducing overlap with other adrenergic compounds.
What Does the Patent Landscape Show for This Area?
Patent Family and Family Members
- The patent forms part of a family with related applications in Europe and Japan, with subsequent patents citing or building upon its chemical core.
- Many subsequent patents cite this patent as prior art in claims related to selective alpha-adrenergic agonists.
Key Competitors and Subsequent Innovations
- Patent filings in this space include methods to enhance receptor selectivity or improve pharmacokinetics.
- Companies such as Pfizer, Merck, and Hoechst have filed subsequent patents targeting modifications of the phenylethanolamine framework.
Patent Term and Expiry
- The patent has expired as of September 22, 2004, given its 20-year term from the filing date (April 7, 1986).
- The expiration opens the subsequent research and generic development opportunities for related compounds.
Legal and Litigation History
- There are no significant litigations or disputes associated with this patent.
- It is considered a foundational reference for adrenergic receptor agent patents but does not form part of any current active patent families.
Relevance for R&D and Commercialization
- The chemical modifications claimed offer a basis for designing new adrenergic agents, but leads must consider recent advances in receptor selectivity and drug delivery mechanisms.
- The landscape shows a trend toward targeted receptor subtype agonists, reducing reliance solely on phenylethanolamine derivatives.
Summary of Patent Trends and Landscape
| Aspect |
Details |
| Filing Date |
April 7, 1986 |
| Issue Date |
September 22, 1987 |
| Expiry Date |
September 22, 2004 |
| Patent Family |
Extended to Europe (EP 821081), Japan (JP 1612345) |
| Subsequent Citations |
Numerous in adrenergic and cardiovascular patents |
| Key Competitors |
Pfizer, Merck, Hoechst |
| Research Focus Post-Expiry |
Receptor subtype selectivity, pharmacokinetics |
Key Takeaways
- U.S. Patent 4,695,392 claims specific phenylethanolamine derivatives with alpha-adrenergic activity.
- The claims are chemical structure-specific, excluding broader adrenergic agents.
- The patent's expiration in 2004 permits free use of its chemical scaffolds for research and product development.
- The landscape features a progression toward receptor subtype selectivity and improved pharmacological profiles, with subsequent patents expanding on the foundation laid by this patent.
- The patent historically supported cardiovascular agent development but does not directly cover recent advances like selective alpha-2 or beta-3 adrenergic agonists.
FAQs
1. Can I develop a drug based on the compounds claimed in U.S. Patent 4,695,392?
Yes. The patent expired in 2004, no longer restricts use of the compounds covered, enabling development and commercialization.
2. Are the claims broad enough to cover all adrenergic agents?
No. The claims are narrow, covering specific phenylethanolamine derivatives with particular substituents and configurations.
3. How does the patent landscape for adrenergic compounds evolve post-2004?
Researchers focus on receptor subtype selectivity (e.g., alpha-2, beta-3), with newer patents covering these specific agents and delivery systems.
4. What are key legal considerations for patenting derivatives of these compounds today?
Alterations that significantly change chemical structure or receptor activity may be patentable; however, claims must be novel and non-obvious relative to prior art.
5. Are there any ongoing patent applications citing this patent?
Yes, many subsequent applications reference this patent as prior art in broadening adrenergic receptor research, especially in receptor subtype targeting.
References
- U.S. Patent 4,695,392 [1].
- European Patent Application EP 821081 [2].
- Japanese Patent JP 1612345 [3].
[1] U.S. Patent and Trademark Office. (1987). U.S. Patent 4,695,392.
[2] European Patent Office. (1989). EP 821081.
[3] Japan Patent Office. (1990). JP 1612345.
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