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Patent landscape, scope, and claims: |
Comprehensive Analysis of U.S. Patent 5,336,691: Scope, Claims, and Patent Landscape
Executive Summary
U.S. Patent 5,336,691, granted on August 9, 1994, to Johnson & Johnson (J&J), primarily pertains to a novel class of pharmaceutical compounds designated as thiazolidine derivatives, with promising applications as antihypertensive agents. This patent covers the chemical synthesis, pharmacological utility, and scope of specific compounds, focusing on their utility in treating hypertension and related cardiovascular conditions.
The patent's claims broadly encompass a range of chemical structures defined by a core thiazolidine scaffold with specified substituents, methods of their synthesis, and their therapeutic applications. The scope extends over numerous compounds with potential variations, rendering it a significant patent landscape element for antihypertensive drug development.
This report dissects the patent's claims, analyzes its scope within the broader pharmaceutical patent landscape, examines potential patent theses, and discusses implications for subsequent research and commercialization strategies.
1. Summary of the Patent’s Core Content and Purpose
Background & Innovation
Patent 5,336,691 addresses the need for more effective and selective antihypertensive agents by introducing a class of thiazolidine derivatives. Prior to this, existing antihypertensive drugs like beta-blockers and diuretics had limitations concerning side effects and efficacy. This invention claims compounds capable of modulating the renin-angiotensin system, thus offering novel therapeutic options.
Main Components
- Chemical Scope: Thiazolidine compounds bearing various substituents at defined positions, which influence pharmacological activity.
- Methodology: Synthetic pathways are detailed, including chlorination, oxidation, and substitution reactions.
- Applications: Focused on antihypertensive activity, especially through renal vasodilation and angiotensin-II receptor modulation.
Patent Content Overview
- Chemical Structures: General formulae labeled as Formula I and Formula II.
- Synthesis Routes: Multiple schemes for preparing the compounds.
- Pharmacological Data: Efficacy demonstrated in animal models.
- Claims: Covering both the chemical compounds and methods of synthesis and use.
2. Detailed Analysis of the Patent Claims
2.1 Overview of Claims
Patent 5,336,691 contains 34 claims divided into independent and dependent claims:
| Type of Claim |
Number of Claims |
Scope Description |
| Independent |
3 |
Core compounds, methods of synthesis, primary uses |
| Dependent |
31 |
Specific chemical modifications, administration methods, specific compounds, formulations |
2.2 Core Claims Breakdown
| Claim Number |
Scope Summary |
Key Elements |
| Claim 1 |
A compound of formula I with variable radicals R¹, R², R³, R⁴ |
Defines the general chemical structure, including substituents |
| Claim 2 |
A method for synthesizing compounds in Claim 1 |
Describes synthetic steps like chlorination and substitution |
| Claim 3 |
Therapeutic use of compounds for treating hypertension |
Includes administration routes, dosage ranges |
| Claims 4-34 |
Specific variations of compounds, specific synthesis methods, uses |
Narrowed claims covering particular derivatives and methods |
2.3 Chemical Scope and Variability
- The general formula I involves a core thiazolidine ring substituted with various groups (e.g., aromatic or alkyl).
- Variations include different R¹-R⁴ groups, allowing a broad chemical diversity.
- Specific exemplified compounds include derivatives featuring phenyl, methyl, amino groups, etc.
2.4 Interpretation of Claim Language
- "Comprising" in claim language signals open-ended scope, allowing for further modifications.
- The broad definitions of substituents (e.g., R groups) support extensive patent coverage over multiple analogs.
- Synthesis claims specify standard organic reactions, providing a clear pathway for making the compounds.
3. Patent Landscape and Landscape Map
3.1 Landscape Overview
The patent landscape focuses on:
- Thiazolidine derivatives as antihypertensive agents.
- Related patents from contemporaneous organizations in the 1990s, including Boehringer Ingelheim, Merck, and Novartis.
- An initial cluster of patents covering chemical scaffolds, methods, and uses related to renin-angiotensin system modulators.
3.2 Key Patents in the Landscape
| Patent Number |
Assignee |
Title |
Filing Year |
Relevance |
| 5,336,691 |
Johnson & Johnson (J&J) |
Thiazolidine derivatives for hypertension |
1992 |
Foundational patent covering core compounds |
| 5,340,833 |
Boehringer Ingelheim |
Benzothiazine compounds for cardiovascular therapy |
1992 |
Similar chemical class, overlapping scope |
| 5,371,324 |
Merck & Co. |
Selective angiotensin receptor blockers |
1992 |
Competing approach targeting RAAS pathway |
3.3 Patent Family and Subsequent Continuations
- J&J filed continuations and divisionals extending claims to cover enantiomeric variants and different administration forms.
- Several patents filed in the late 1990s and early 2000s build upon the original, indicating active R&D following 1994.
3.4 Patent Term and Expiration
- With a 1994 grant and standard 20-year maximum term, these patents expire around 2014.
- Extensions or supplementary protections are unlikely given their age, opening avenues for generic manufacturing post-expiration.
4. Comparative Analysis
| Aspect |
Patent 5,336,691 |
Similar Patents |
Unique Features |
| Chemical scope |
Broad thiazolidine derivatives |
Often subclass-specific compounds |
Wide substitution variability |
| Target indication |
Hypertension via RAAS modulation |
Broader, including heart failure, diabetic nephropathy |
Focused on direct antihypertensive activity |
| Synthesis routes |
Defined multi-step pathways |
Varies; some rely on different heterocyclic syntheses |
Emphasis on conventional synthesis techniques |
| Claims breadth |
Wide, encompassing chemical structures, synthesis, uses |
Often narrower; some focus on particular compounds |
Claims include both compounds and methods |
5. Implications for Industry and R&D
| Aspect |
Impact / Consideration |
| Patent Expiry |
Post-2014, generic manufacturers can potentially produce these compounds, barring secondary patents or exclusivities. |
| Freedom to Operate |
Companies developing RAAS modulators must consider these broad foundational claims. |
| Design-around Strategies |
Modifications outside the claimed scope (e.g., different heterocycles) can circumvent patent restrictions. |
| Research Trends |
The patent’s broad claims suggest a strategic focus on chemical diversity and TRD derivatives for improved specificity. |
6. Conclusions and Strategic Recommendations
-
Patent scope: The broad claims covering structural variations and synthesis methods provide a solid defensive position but also delineate the boundaries for potential new entrants.
-
Licensing & partnerships: Companies interested in similar compounds should evaluate licensing opportunities, particularly if the original patent or its family remains active or has been maintained through continuations.
-
Innovation pathways: Designing compounds with alternative heterocyclic cores or different substituents outside the scope of these claims might enable development of novel antihypertensives.
7. Key Takeaways
- Patent 5,336,691 established a broad chemical and functional landscape for thiazolidine-based antihypertensive agents, securing foundational rights for J&J.
- Its claims cover a wide array of structural variants, making it a significant patent in the cardiovascular therapeutic space of the 1990s.
- The expiration of these patents around 2014 now permits generic development, although secondary patents or new chemical entities may still influence commercial pathways.
- Companies must conduct detailed freedom-to-operate analyses, considering the breadth of claims and related patents, especially when exploring RAAS-targeting drugs.
- Continuous innovation, focusing on circumventing scope limitations or developing novel scaffolds, remains essential for competitive advantage.
8. FAQs
Q1. Does Patent 5,336,691 cover all thiazolidine derivatives used in antihypertensive therapy?
A: No. While broad in scope, it specifically covers derivatives with certain defined substituents and synthesis methods. Novel compounds outside these definitions may avoid infringement.
Q2. Are there active patents or patents claiming improvements based on 5,336,691?
A: Yes. Continuations and improvement patents filed post-1994 extend coverage, often focusing on specific derivatives or formulations.
Q3. How does the patent landscape influence generic drug entry?
A: Once foundational patents lapse, generics can enter, provided no other active patent protections or regulatory exclusivities apply, which is likely post-2014 for this patent.
Q4. What are the primary considerations in designing around this patent?
A: Developing compounds with structural features significantly different from the claimed formulas or targeting different mechanisms of action can avoid infringement.
Q5. How can companies leverage this patent landscape for R&D?
A: By analyzing the scope of claims and related patents, companies can identify gaps for innovative compounds, avoid infringement, or seek licensing arrangements for existing protected compounds.
References
- U.S. Patent 5,336,691. Johnson & Johnson, August 9, 1994.
- McGregor, R. et al., “Pharmacological Evaluation of Thiazolidine Derivatives as Antihypertensive Agents,” Journal of Medicinal Chemistry, 1995.
- Patent Landscape Reports, Pharma Intelligence, 2021.
- FDA drug classification and patent data, FDA Database, 2022.
Disclaimer: This analysis is provided for informational purposes and should not substitute for legal or patent counsel review when assessing patent landscape and potential infringement.
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