Detailed Analysis of the Scope and Claims of United States Patent 4,818,816
Introduction
United States Patent 4,818,816, titled "Process for the organic synthesis of oligosaccharides and derivatives thereof," is a significant patent in the field of organic chemistry, particularly in the synthesis of oligosaccharides and their derivatives. This patent, filed by applicants who have developed a flexible and specific process for synthesizing these compounds, has far-reaching implications in medicine and biological research.
Scope of the Patent
The patent revolves around the organic synthesis of oligosaccharides, which are fragments of acid mucopolysaccharides. These oligosaccharides are crucial components of biologically active derivatives, such as heparin and heparan sulfate[1].
Key Components
- Oligosaccharides and Derivatives: The patent describes the synthesis of oligosaccharides and their derivatives, which are essential for their biological properties. These compounds are particularly valuable for their medicinal properties, including high anti-thrombotic activity[1].
- Protecting Groups: The process involves the use of temporary protecting groups to selectively block positions on the amino-sugar (A) and uronic acid (U) units. These groups are removable, allowing for the elongation of the glucid skeleton through repeated glycosylation reactions[1].
Claims of the Patent
The patent includes several key claims that define its scope:
Synthesis Process
- The patent claims a process for the organic synthesis of oligosaccharides, which involves the use of protecting groups to control the glycosylation reactions. This process allows for the synthesis of oligosaccharides with varied enchainments and stereo-specificity[1].
Novel Oligosaccharides
- The patent claims novel oligosaccharides and their derivatives, which possess biological properties making them useful as medicaments or laboratory reagents. These oligosaccharides are particularly interesting for their anti-thrombotic activities[1].
Biological Uses
- The claims extend to the biological uses of these oligosaccharides, including their application as active medicinal substances, laboratory agents, or reference substances for structural studies[1].
Patent Landscape Analysis
Technological Domain
The patent falls within the technological domain of organic chemistry, specifically in the synthesis of oligosaccharides and their derivatives. This domain is critical for the development of anticoagulant drugs and other biologically active compounds.
Key Players
- The original patent (US4818816A) was a pioneering work in this field. Subsequent patents, such as those related to the production of Fondaparinux sodium (WO2015011517A1, WO2015011519A1), have built upon this foundational work. These later patents aim to improve the production processes of specific oligosaccharide derivatives like Fondaparinux sodium, which is an anticoagulant drug[2][4].
Trends and Innovations
- The trend in this domain is towards more efficient and scalable production processes. For example, later patents have focused on overcoming the limitations of the original process, such as low yields and additional reaction times, to achieve more economic and efficient synthesis methods[2][4].
Citations and Evolution
- The original patent has been cited in numerous subsequent patents, indicating its significant impact on the field. Later patents have evolved the synthesis process, incorporating new steps and reagents to improve yield and efficiency[2][4].
Competitive Landscape
- The competitive landscape in this domain is characterized by continuous innovation in synthesis processes and the development of new oligosaccharide derivatives. Companies and researchers are actively working to improve existing methods and to discover new compounds with valuable biological properties[3].
Impact and Applications
Medicinal Properties
- The oligosaccharides synthesized through this process have significant medicinal properties, particularly as anticoagulants. Fondaparinux sodium, for example, is used to prevent deep vein thrombosis and treat pulmonary embolism[2].
Laboratory Reagents
- These oligosaccharides are also valuable as laboratory reagents and reference compounds for structural studies. They help in understanding the biological activities of similar compounds and in developing new therapeutic agents[1].
Challenges and Limitations
- One of the challenges in this field is the complexity of the synthesis process. The original patent's process, while flexible, is not suitable for large-scale production due to issues like low yields and extended reaction times[2].
- Later patents have addressed these challenges by introducing new methods and reagents, but the synthesis of oligosaccharides remains a complex and demanding task.
Key Takeaways
- Flexible Synthesis Process: The patent describes a flexible process for synthesizing oligosaccharides with varied enchainments and stereo-specificity.
- Biological Properties: The synthesized oligosaccharides have valuable biological properties, including high anti-thrombotic activity.
- Improvements Needed: Later patents have focused on improving the efficiency and scalability of the synthesis process.
- Competitive Landscape: The domain is highly competitive, with ongoing innovations in synthesis processes and the development of new oligosaccharide derivatives.
Frequently Asked Questions (FAQs)
What is the main focus of United States Patent 4,818,816?
The main focus is on the organic synthesis of oligosaccharides and their derivatives, particularly those constituting fragments of acid mucopolysaccharides.
What are the key components of the synthesis process described in the patent?
The process involves the use of temporary protecting groups to control glycosylation reactions and the synthesis of oligosaccharides with varied enchainments and stereo-specificity.
What are the biological uses of the oligosaccharides synthesized through this process?
These oligosaccharides are useful as medicaments, laboratory agents, or reference substances for structural studies, particularly for their anti-thrombotic activities.
How has the original patent influenced later innovations in the field?
The original patent has been cited in numerous subsequent patents and has served as a foundation for improving synthesis processes, such as those for Fondaparinux sodium.
What are the challenges in scaling up the synthesis process described in the patent?
The original process is not suitable for large-scale production due to issues like low yields and extended reaction times, which later patents have addressed through new methods and reagents.
Sources Cited
- US4818816A - Process for the organic synthesis of oligosaccharides and derivatives thereof - Google Patents
- WO2015011517A1 - Process for the production of fondaparinux sodium - Google Patents
- How to Do Patent Landscape Analysis - Goldstein Patent Law
- WO2015011519A1 - Process for the production of fondaparinux sodium - Google Patents
- Analytical method for detecting sulfated oligosaccharides - Justia Patents
