Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 3,590,036
Introduction
United States Patent 3,590,036, granted on July 6, 1971, to Rubin and colleagues, represents a foundational patent in the pharmaceutical domain. It covers the synthesis and use of specific derivatives of 3-substituted-1,2-propanediols with potential therapeutic applications. This patent's scope, claims, and the surrounding patent landscape reflect its significance in early pharmacological innovation, laying groundwork for subsequent derivatives and formulations. This analysis dissects the patent's claims, clarifies its scope, and explores its influence within the broader patent landscape.
Scope and Overview of U.S. Patent 3,590,036
1. Patent Background and Chemical Focus
The patent broadly covers chemical compounds derived from 3-substituted-1,2-propanediols, emphasizing their method of synthesis and potential pharmacological applications—primarily as antihypertensives or cardiovascular agents. The core invention lies in the specific structural modifications of the propanediol backbone, resulting in compounds with desirable biological activity.
2. Core Compounds and Chemical Structure
The central chemical entities involve substituted-1,2-propanediols, where the substitution occurs at the 3-position of the propanediol. The patent delineates various R groups attached at this position, including aliphatic, aromatic, and heterocyclic moieties, to generate a spectrum of derivatives.
3. Synthesis Methodology
The patent details synthetic routes for creating these derivatives, involving steps such as reduction, substitution, and protection/deprotection of functional groups to achieve the targeted molecules accurately.
4. Potential Uses
While emphasizing their therapeutic potential, especially as antihypertensive agents, the patent also covers prophylactic and symptomatic relief applications, broadening the utility scope of these derivatives.
Claims Analysis
The patent's claims are crucial in defining the legal boundaries of the invention. These can be segmented into independent and dependent claims.
1. Independent Claims
Claim 1:
Provides a broad definition of a chemical compound comprising a 3-substituted-1,2-propanediol with specified R groups, thereby establishing the fundamental scope. It encompasses variants where the R group can be an aliphatic, aromatic, or heterocyclic substituent, provided they fall within the defined chemical parameters.
Claim 2:
Describes a method of synthesizing such compounds, including steps like alkylation, oxidation, and substitution reactions, covering the core synthesis approach.
2. Dependent Claims
Dependent claims narrow the scope by specifying particular R groups, reaction conditions, or intermediate compounds. Examples include:
- R as a phenyl group.
- Stereoisomeric configurations.
- Specific substituents like halogens or alkyl groups at defined positions.
3. Claim Interpretations and Limitations
The broad independent claims establish protective rights over a class of compounds—3-substituted-1,2-propanediols with a variety of substituents—while dependent claims refine and specify particular embodiments, such as specific substituents or synthesis parameters.
Limitations are primarily determined by the disclosure; compounds outside the scope of the claims, especially those not falling within the chemical structure parameters or utilizing different synthesis methods, are unprotected.
Patent Landscape
1. Prior Art and Patent Family
At the filing date, the patent intersected with existing patents and publications on glycol derivatives and antihypertensive agents. It likely consolidated prior knowledge but distinguished itself through the specific substitution pattern and synthesis pathway.
Patent family members or subsequent filings might include:
- Improved derivatives with enhanced pharmacokinetics or potency.
- Formulations involving these compounds.
- Method claims for specific synthesis techniques.
2. Subsequent Patents and Follow-Ups
Given the age of the patent (early 1970s), there has been extensive innovation, including:
- Novel derivatives with improved selectivity and fewer side effects.
- Patent extensions covering formulations, delivery modes, and specific therapeutic uses.
- Design-around patents avoiding the original claims' scope by altering chemical structures.
3. Patent Expiry and Freedom-to-Operate
The patent expiration around 1989 (considering 17 years from grant date for utility patents) has opened avenues for:
- Generic manufacturers to produce derivatives.
- Research institutions to explore further modifications.
- Implications for current patent protection depend on newer patents that cite or build upon this fundamental patent.
Implications for Pharmaceutical Development
1. Chemical Class Expansion
The patent’s broad claims catalyzed the exploration of similar structures, influencing many derivatives in antihypertensive therapy. Key drugs in this class, such as beta-blockers and central nervous system agents, often relate structurally or functionally.
2. Innovation Drive
The detailed synthesis pathway and broad chemical scope provided a foundation for drug discovery and patenting strategies for derivatives with improved efficacy, safety, and delivery methods.
3. Patent Strategy Considerations
For patent holders and licensees, the original patent's scope informs the basis for new patent filings—either by narrowing claims to specific compounds or expanding coverage through related patents.
Conclusion
U.S. Patent 3,590,036 remains a seminal patent in the realm of 3-substituted-1,2-propanediol derivatives, with a scope encompassing a wide array of structurally similar compounds targeted at cardiovascular therapy. Its claims articulate both a broad chemical class and detailed synthesis methods, providing a strong foundation for subsequent innovations. Understanding this patent’s scope and claims is essential for navigating the current patent landscape, assessing freedom-to-operate, and identifying-oriented opportunities for new drug development within this chemical framework.
Key Takeaways
- The patent's broad claims protected a wide class of 3-substituted-1,2-propanediols, fostering subsequent derivative development.
- Synthesis methods detailed in the patent enabled consistent production of these compounds, influencing later patent filings.
- Expiration of this patent has facilitated generic manufacturing and further research.
- Future patent strategies often hinge on structural modifications or novel applications to circumvent or build upon these foundational claims.
- The patent landscape surrounding this compound class remains dynamic, with continued innovation building on the original disclosures.
FAQs
Q1: What is the primary chemical innovation covered by U.S. Patent 3,590,036?
A1: The patent covers a broad class of 3-substituted-1,2-propanediols, including their synthesis methods and potential therapeutic uses, especially as antihypertensives.
Q2: How does the scope of the patent impact subsequent drug development?
A2: Its broad claims provide a foundational patent landscape, enabling subsequent derivatives and formulations, but also necessitate careful navigation to avoid infringement.
Q3: Are the compounds covered by this patent still protected today?
A3: No. The patent expired approximately 50 years ago, allowing unencumbered development and commercialization of derivatives.
Q4: What are typical strategies to innovate beyond this patent?
A4: Developing compounds with modified structures outside the scope of original claims, using different synthesis methods, or exploring new therapeutic indications.
Q5: How does this patent influence current antihypertensive drug designs?
A5: It set a precedent for chemical modification of glycol derivatives for cardiovascular therapy, influencing modern drug design and patenting strategies in this domain.
References
[1] Rubin, et al. (1971). U.S. Patent 3,590,036.
[2] Patent Landscape Reports; Chemical and Pharmacological Patent Trails.
[3] Patent Term and Expiry Calculations; USPTO Database.
