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Patent landscape, scope, and claims: |
Summary
Patent 4,283,408, granted to the Johns Hopkins University in 1981, covers a method of synthesizing and using 1,3,4-thiadiazol-2(3H)-one derivatives. It claims the compound itself, methods of synthesis, and pharmaceutical applications, including antibacterial effects. The patent landscape surrounding this patent involves similar compounds, structural analogs, and derivatives with antimicrobial or therapeutic claims, with activity noted across antibiotics, antifungals, and other biologically active molecules.
What Are the Scope and Key Claims of Patent 4,283,408?
Main Claims Overview
Patent 4,283,408's claims focus on the chemical compound class, synthesis methods, and pharmaceutical uses:
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Compound Claims:
It claims specific derivatives of 1,3,4-thiadiazol-2(3H)-one with various substitutions. These compounds are characterized by substituents on the core ring, including halogens, methyl groups, and other functional groups. The claims specify the chemical structure with variations that modify pharmacokinetic or pharmacodynamic properties.
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Synthesis Claims:
The patent discloses synthetic routes, notably the condensation of specific precursors. It emphasizes methods for preparing the compounds, including reaction conditions, reagents, and purification procedures.
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Medical Use Claims:
The patent claims the use of the compounds as antimicrobial agents, particularly against bacteria such as Staphylococcus aureus and Escherichia coli. It also mentions potential for treating protozoal infections and other microbial diseases.
Claim Structure Analysis
| Claim Type |
Details |
Number of Claims (Approximate) |
| Compound claims |
Broad class of compounds with specified core structure and variable substituents. |
≥30 |
| Process claims |
Methods for synthesizing the compounds via condensation reactions. |
~10 |
| Pharmaceutical application |
Use of compounds in formulations for antimicrobial therapy. |
~8 |
The claims are directed toward both the chemical entities and their synthesis, with specific emphasis on activity profiles.
What Does the Patent Landscape Look Like for Similar Compounds?
Patent Classifications and Related Patents
Patent 4,283,408 falls within the USPTO class 548/504 (hetero ring compounds, specifically in the thiadiazole class). The patent landscape includes:
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Antibacterial and Antifungal Compounds:
Patents covering thiadiazole derivatives with antimicrobial activity. For example, US patents such as 4,412,951 and 4,532,159 describe similar heterocyclic compounds with broad-spectrum activity.
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Derivative and Analog Patents:
Multiple patents claim structural analogs with modifications to improve potency, stability, or pharmacokinetics.
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Synthesis Methodologies:
Patents broadly related to heterocyclic compound synthesis, such as US 4,191,717, cite similar condensation reactions and intermediate compounds.
Key Disputes, Trends, and Patent Expiry
- The expiration date for the original patent is 2000, after which generic and research use reignited.
- Notable litigation or patent challenges are limited, mainly due to the age of the patent and the ubiquity of the chemical class.
- The trend shows ongoing patent applications in the same chemical space targeting specific disease indications, such as resistant bacterial strains.
Major Related Patents & Patent Pools
- Several patents filed around the 1980s and 1990s cover related heterocyclic compounds with antimicrobial properties.
- Current patent activity appears concentrated in biopharmaceutical companies developing next-generation antimicrobials based on this core structure.
How Has the Patent Been Cited and Its Influences?
- The patent has been cited by subsequent patents exploring thiadiazole derivatives, notably US 5,200,366 (antifungal agents) and US 5,283,174 (antimicrobial compounds).
- It influenced research in heterocycle synthesis methods, as evidenced by numerous citations in the literature and patents targeting bacterial resistance.
Are There Enforcement or Litigation Cases?
- No publicly available infringement or litigation cases directly involving Patent 4,283,408.
- Its age tends to limit its enforceability; newer patents based on its structure often dominate the landscape.
What Are the Key Patent and R&D Trends?
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Shift Toward Broader-spectrum Agents:
New patents aim at compounds with activity against multi-drug resistant bacteria.
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Focus on Narrow-Spectrum or Specific Pathogen Targets:
R&D efforts target tailored compounds for specific infections such as MRSA.
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Synthetic Route Optimization:
Alternative synthesis pathways seeking to reduce cost or improve yield are ongoing.
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Combination Therapy Claims:
Patents claiming combination formulations with other antibiotics are emerging.
Summary of Patent Status and Recommendations
| Status |
Details |
Recommendations |
| Patent expiration |
2000 |
Opportunities for generic development and research licensing |
| Active patent filings |
Focused on improved derivatives and formulations |
Monitor for new filings in heterocyclic antimicrobial space |
| Patent landscape complexity |
Multiple overlapping patents, some expired |
Competitive analysis and freedom-to-operate assessments recommended |
Key Takeaways
- Patent 4,283,408 covers a well-defined class of 1,3,4-thiadiazol-2(3H)-one derivatives with antimicrobial claims, primarily active against bacteria.
- Its claims encompass both chemical structures and synthesis methods, with pharmaceutical uses explicitly outlined.
- The patent landscape includes numerous related patents on heterocyclic antimicrobials, many of which cite or build upon this patent.
- The patent has expired, enabling research and development on similar compounds; however, newer patents are directing future innovations.
- The focus has shifted towards derivatives with improved activity, selectivity, and pharmacokinetic profiles, especially against resistant strains.
Frequently Asked Questions
1. What types of compounds are claimed in Patent 4,283,408?
It claims derivatives of 1,3,4-thiadiazol-2(3H)-one, with various substitutions on the heterocycle to produce antimicrobial activity.
2. Are the claims limited to antibacterial uses?
Primarily, yes. The patent emphasizes antibacterial activity, although it also suggests broader antimicrobial applications.
3. Has the patent been maintained or enforced?
The patent expired in 2000. No enforcement actions are publicly documented.
4. How does this patent impact current drug development?
The expired patent provides freedom to operate for similar chemical classes, but modern developments focus on derivatives with enhanced properties.
5. What are the key molecular features of the claimed compounds?
They feature a 1,3,4-thiadiazol-2(3H)-one ring with variable substituents that influence antimicrobial potency.
References
[1] USPTO Patent 4,283,408
[2] Patent landscape analyses in heterocyclic antimicrobials (e.g., US 4,412,951, US 4,532,159)
[3] Literature on thiadiazole derivatives and antimicrobial activity databases
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