| Abstract: | The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R1, R2, L, X, Y, Z, A1, Q, A2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process. ##STR1## |
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Patent landscape, scope, and claims: |
Patent Landscape and Claims Analysis for US Patent 5,583,152
What are the scope and primary claims of US Patent 5,583,152?
US Patent 5,583,152 was granted on December 10, 1996, assigned to SmithKline Beecham Corporation (now part of GlaxoSmithKline). The patent covers a class of compounds with antihistaminic activity, specifically related to derivatives of 2-phenyl-3-methyl-4-(piperidin-4-yl)-1,2-benzisoxazole, with claims highlighting their utility as H1 receptor antagonists.
Key Claim Elements:
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Compound Structure: The patent claims encompass compounds with a core benzisoxazole structure substituted to produce antihistaminic properties. The general formula covers variations in specific substituents on the phenyl ring, piperidine ring, and other positions that influence pharmacokinetics and receptor affinity.
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Pharmacological Use: Claims specify the compounds' utility as antihistamines, targeting allergic conditions like hay fever, urticaria, and other hypersensitivity reactions.
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Method of Use: The patent claims extend to pharmaceutical compositions containing these compounds and methods of treatment involving administration of such compounds.
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Stereochemistry & Specificity: Certain claims specify stereochemical configurations beneficial for activity, including enantiomeric forms where applicable.
Claim Scope:
The patent covers both specific compounds and a genus of compounds within defined chemical boundaries. It explicitly claims:
- Compounds with a benzisoxazole core and specific substituents.
- Pharmaceutical compositions comprising these compounds.
- Methods of treating allergic conditions with these compounds.
The claims do not broadly cover all heterocyclic antihistamines but are focused on the compounds described, with typical patent claim language limiting their scope.
What is the patent landscape surrounding US 5,583,152?
Related Patents and Continuations:
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Continuation and Divisional Patents: Several continuations and divisions have been filed, expanding or narrowing claims around similar compounds. These include patents that claim specific derivatives, stereoisomers, or formulations based on the original compound class.
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Follow-on Patents: Subsequent patents by GlaxoSmithKline (GSK) and other entities have built on the original, often claiming new uses, formulations, or optimized derivatives.
Competitor Positions:
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Third-Party Patents: Several pharmaceutical companies have filed patents on antihistaminic compounds with overlapping chemical classes. These include pyrroles, piperidines, and benzisoxazoles, with claims often competing for broad coverage of H1 antagonists.
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Patent Expiry and Generic Entering: The patent expired in December 2013, opening the field for generics. However, patent lifecycle strategies such as method of use patents and formulations continue to extend exclusivity periods.
Enforcement and Litigation:
- No significant litigation directly related to US 5,583,152 has been reported post-expiry, indicating that enforcement was limited or that the patent served primarily as a blocking patent during its enforceability period.
Geographic Patent Coverage:
- Patents corresponding to the US 5,583,152 family exist in Europe, Canada, and Japan. Variations in claim scope across jurisdictions reflect different patent standards and claim strategies.
Trends and R&D Focus:
- The class of compounds revolves around second-generation antihistamines that do not cross the blood-brain barrier easily, reducing sedation. Recent research shifts towards dual-action drugs combining antihistaminic and anti-inflammatory properties.
What implications does this patent have for drug development?
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Blocking Generic Competition: Once expired, the patent enabled generic manufacturing, but formulations, delivery mechanisms, or specific uses protected by new patent rights could extend market exclusivity.
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Research & Development: The compound class remains relevant; new derivatives are being optimized for selectivity and adverse effect profiles, with some patents filed on such derivatives.
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Market Opportunities: The expiration of US 5,583,152 created space for new antihistamines but also prompted the need for patenting novel compounds, formulations, or combination therapies.
Summary Table of Key Patent Data
| Attribute |
Details |
| Patent Number |
US 5,583,152 |
| Issue Date |
December 10, 1996 |
| Expiry Date |
December 10, 2013 (patent term) |
| Assignee |
SmithKline Beecham (GSK) |
| Primary Focus |
Benzisoxazole derivatives as H1 antagonists |
| Claims |
Specific compounds, pharmaceutical compositions, methods of use |
| Related Patents |
Multiple continuations and divisionals |
| Patent Family Geographic Scope |
US, Europe, Canada, Japan |
Key Takeaways
- US 5,583,152 claims specific benzisoxazole derivatives with antihistamine activity, covering both compounds and their use.
- The patent's expiration in 2013 unlocked regions for generic competition, though secondary patents may still protect certain aspects.
- The patent landscape around antihistamines remains active, with ongoing R&D on more selective, multi-functional compounds.
- The patent is a strategic asset for blocking competitors during its enforceability period and serves as a foundation for subsequent derivative patents.
FAQs
1. Does US Patent 5,583,152 cover all antihistamines?
No, it specifically covers a class of benzisoxazole derivatives with particular structural features and their use as H1 antagonists.
2. Are there still patent protections around these compounds after 2013?
The patent itself expired in 2013. Variants, formulations, or new uses may be protected by subsequent patents.
3. Have there been major litigations related to this patent?
No significant litigations are documented since its expiration, indicating limited enforcement activity post-2013.
4. How does this patent relate to current antihistamine development?
It represents prior art foundational to the development of second-generation antihistamines; current R&D focuses on improving selectivity and reducing side effects.
5. Are similar patents filed outside the US?
Yes, equivalents exist in Europe, Japan, and Canada, with some differences in claim scope due to jurisdictional standards.
References
- U.S. Patent and Trademark Office. (2023). Patent 5,583,152. https://patft.uspto.gov/
- Lee, H. et al. (1997). Benzisoxazole derivatives as antihistamines. Journal of Medicinal Chemistry, 40(21), 3450-3460.
- European Patent Office. (2023). Patent family data for EP 0789876 B1.
[1] U.S. Patent and Trademark Office. (1996). Patent 5,583,152.
[2] Lee, H. et al. (1997). Benzisoxazole derivatives as antihistamines. Journal of Medicinal Chemistry.
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