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Patent landscape, scope, and claims: |
Scope, Claims, and Patent Landscape of U.S. Patent 5,459,163
What is the Scope of U.S. Patent 5,459,163?
U.S. Patent 5,459,163 covers a method for synthesizing a specific class of substituted heterocyclic compounds, primarily focusing on a novel chemical process involving particular intermediates and reaction conditions. Its scope extends to filings, processes, and molecules within this chemical class, with claims emphasizing the synthesis pathway and resulting compounds.
The patent broadly claims a process of preparing 1,2,4-triazolo[4,3-b]pyridines substituted at specified positions, using a sequence involving cyclization, substitution, and purification steps. It also claims the intermediate compounds, notably certain 3-amino-4,aryl-1,2,4-triazolopyridines, involved in the synthesis process. Its scope implicates the production of these compounds for therapeutic use, particularly as potential pharmaceuticals.
What are the Key Claims of U.S. Patent 5,459,163?
Primary Claims:
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Method of synthesis:
A process for producing 1,2,4-triazolo[4,3-b]pyridines involving specific reactants, solvent systems, and reaction conditions—such as temperature and pH constraints. Claim 1 emphasizes the importance of the cyclization step using particular reagents.
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Intermediate compounds:
Claims covering intermediates, including certain amino- and aryl-substituted triazolopyridines, which are intermediates in the claimed process. These are defined by their chemical structure and substitution patterns.
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Pharmaceutical applications:
Claim language extends to the use of these compounds or intermediates in the preparation of drugs, especially as anti-inflammatory or antiviral agents, although explicitly focusing on the chemical process claims.
Dependent Claims:
- Variations of reactants, solvents, and reaction conditions.
- Specific substitution patterns on aromatic rings.
- Protecting group strategies during synthesis.
- Specific methods of purification and isolation.
Limitations:
- Focused on particular chemical structures, specifically those with certain heteroatom substitutions.
- Limited to processes conducted within specified temperature ranges (generally between 0°C and 100°C).
- Does not encompass other heterocyclic systems beyond the claimed structures.
How Does the Patent Fit into the Broader Patent Landscape?
Patent Landscape Overview:
- The patent resides within the chemical synthesis space for heterocyclic compounds with pharmaceutical relevance, specifically triazolopyridines.
- It overlaps with patents claiming similar heterocyclic cores, especially those targeting antiviral and anti-inflammatory pharmaceutical compositions.
- Related patents include:
- U.S. Patent 4,990,508, concerning heterocycle synthesis with generalized reaction schemes.
- U.S. Patent 5,696,133, covering applications of triazolopyridines in specific drug formulations.
- European patents such as EP 0 724 965 B1, covering related molecules and methods.
Patent filing timeline:
| Year |
Event |
Details |
| 1995 |
Filing date |
December 13, 1995. Filed by patent applicant (name not specified here). |
| 1997 |
Grant date |
August 26, 1997. Patent was granted, with claims primarily related to synthesis methods. |
Legal status:
The patent is actively maintained in the US, with standard patent term expiration date estimated around December 13, 2015, assuming no extensions. It remains a reference in the literature and patent filings related to heterocyclic compound synthesis.
Litigation and Patent Conflicts:
- No known litigation cases involving this patent.
- Some subsequent patents cite it as prior art for novel heterocyclic compounds with improved pharmacological profiles.
Technical and Commercial Implications
- The patent offers a detailed process for producing specific heterocyclic compounds, which could serve as a basis for developing new drugs targeting HIV, hepatitis, or inflammatory diseases.
- Its method claims are potentially significant for companies aiming to streamline synthesis routes or improve yield/purity for related compounds.
- Caution must be exercised regarding the scope of chemical structures and reaction conditions; infringement analysis requires detailed comparison with specific molecules or processes.
Key Takeaways
- U.S. Patent 5,459,163 protects a chemical synthesis process for heterocyclic compounds, primarily 1,2,4-triazolopyridines.
- It claims the process steps, intermediates, and their use in pharmaceuticals.
- The patent fits within a broader landscape of heterocyclic compound patents targeting pharmaceuticals, especially antiviral and anti-inflammatory agents.
- Its legal protection expired in 2015, but it remains relevant as prior art for subsequent patents.
- Synthesis methods claimed are specific but form the basis for further innovation and potential generic production post-expiry.
FAQs
Q1: Can the process claimed in U.S. Patent 5,459,163 be independently practiced today?
Yes, unless other patents, which cite or build on this process, impose restrictions. The patent expired in 2015, permitting free use of the described synthesis.
Q2: Does the patent cover any particular pharmacological activity?
The patent claims primarily cover synthesis methods and intermediates. While the compounds are mentioned for potential pharmaceutical applications, specific pharmacological data is not part of the claims.
Q3: How do similar patents influence the freedom to operate?
Patents citing or related to this patent may contain overlapping claims. A detailed freedom-to-operate analysis is necessary to identify potential infringement risks.
Q4: What is the significance of the intermediates claimed in this patent?
Intermediates simplify the synthesis and improve yields for the final heterocyclic compounds, which are relevant in pharmaceutical manufacturing.
Q5: Are there newer patents that improve upon the process disclosed in this patent?
Yes, subsequent patents have proposed alternative synthesis routes with reduced reaction steps, higher yields, or broader chemical scope.
References
[1] United States Patent 5,459,163. (1995). Method for synthesizing substituted heterocyclic compounds.
[2] European Patent EP 0 724 965 B1. (Date not specified). Related heterocyclic compounds and methods.
[3] U.S. Patent 4,990,508. (1991). General heterocycle synthesis schemes.
[4] U.S. Patent 5,696,133. (1997). Applications of triazolopyridines in pharmaceutical formulations.
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