United States Patent 4,231,938: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 4,231,938, titled "Hypocholesteremic Fermentation Products and Process of Preparation," was granted on November 4, 1980, to inventors Richard L. Monaghan, Alfred W. Alberts, Carl H. Hoffman, and George Albers-Schonberg, and assigned to Merck & Co., Inc. This patent is significant in the field of pharmaceuticals, particularly for its contributions to the development of hypocholesteremic and hypolipemic medicaments.
Background of the Invention
The patent addresses the need to reduce cholesterol levels in the mammalian body, given the potential link between high blood cholesterol and atherosclerosis. Previous efforts had led to the discovery of fermentation products that inhibit cholesterol biosynthesis, such as ML236B (compactin) described by Endo et al.[4].
Summary of the Invention
The invention involves the isolation of compounds from the cultivation of a microorganism belonging to the genus Aspergillus. The primary compound, designated MSD803, has a lactone structure and is highly active in reducing cholesterol and lipid levels. The patent also covers the free hydroxy acid form of MSD803, as well as its salts and esters, which are useful as medicaments against hypercholesteremia and hyperlipemia[4].
Claims
The patent includes one claim that encompasses the compounds and their preparation process:
- Claim 1: The compound MSD803, its free hydroxy acid form, and its salts and esters, along with the process of cultivating Aspergillus microorganisms to produce these compounds.
Detailed Description of the Invention
Microorganism Cultivation
The process involves cultivating a microorganism, specifically Aspergillus MF-4833 or MF-4845, in a culture medium. The medium composition includes ingredients such as corn steep liquor, tomato paste, oatmeal, glucose, and trace elements. The cultivation is followed by the recovery of the desired compounds from the cultured broth[4].
Compound Structure and Properties
MSD803 has a specific lactone structure and exhibits potent hypocholesteremic and hypolipemic activities. It also shows antifungal properties, making it useful for controlling various fungal strains[4].
Preparation Examples
The patent provides detailed examples of the fermentation process, including the preparation of the culture medium and the recovery of MSD803. For instance, Example 1 describes the aseptic suspension of lyophilized culture MF-4833 in a seed flask containing medium A, followed by fermentation and compound recovery[4].
Patent Landscape
Related Patents
The patent is part of a broader landscape of inventions related to cholesterol reduction. For example, U.S. Patents 4,049,495 and 3,983,140 by Endo et al. describe similar fermentation products like compactin. These patents collectively contribute to the development of statins, a class of drugs widely used to lower cholesterol levels[4].
International Context
The invention is not isolated to the U.S. patent system. Similar research and patents exist in other countries, such as those filed with the European Patent Office (EPO) and the Japan Patent Office (JPO). These international patents often cover related compounds and processes, reflecting a global effort to address cardiovascular diseases[1].
Economic and Research Impact
Patent Claims Research Dataset
The USPTO's Patent Claims Research Dataset, which includes detailed information on claims from U.S. patents granted between 1976 and 2014, can provide insights into the scope and impact of patents like 4,231,938. This dataset helps in understanding the trends and measurements of patent scope, which can be crucial for economic and research analyses[3].
Industry Impact
The development of hypocholesteremic medicaments has had a significant impact on the pharmaceutical industry. Patents like 4,231,938 have paved the way for the creation of blockbuster drugs such as lovastatin and simvastatin, which are widely used to treat high cholesterol and reduce the risk of cardiovascular diseases[5].
Search and Analysis Tools
For researchers and inventors, tools like the USPTO's Patent Public Search, Global Dossier, and the Common Citation Document (CCD) are essential for conducting thorough searches and analyses of prior art. These tools help in identifying related applications, office actions, and citation data, ensuring that new inventions build upon existing knowledge without infringing on existing patents[1].
Public Access and Resources
The USPTO provides various resources for public access to patent information, including the Public Search Facility in Alexandria, VA, and the Patent and Trademark Resource Centers (PTRCs). These resources are invaluable for anyone seeking to understand the patent landscape and conduct detailed analyses of patents like 4,231,938[1].
Conclusion
United States Patent 4,231,938 is a landmark patent in the field of pharmaceuticals, particularly for its role in the development of hypocholesteremic and hypolipemic medicaments. The patent's scope and claims are well-defined, and its impact on the industry is significant. Understanding this patent within the broader patent landscape, using tools provided by the USPTO and other international intellectual property offices, is crucial for researchers, inventors, and business professionals.
Key Takeaways
- Invention Scope: The patent covers compounds isolated from Aspergillus microorganisms and their use in reducing cholesterol levels.
- Claims: One claim encompasses the compounds and their preparation process.
- Impact: Significant contribution to the development of statins and the pharmaceutical industry.
- Related Patents: Part of a broader landscape including patents by Endo et al. and other international patents.
- Research Tools: Utilize USPTO tools like Patent Public Search and Global Dossier for thorough analyses.
FAQs
Q: What is the main compound described in U.S. Patent 4,231,938?
A: The main compound is MSD803, a lactone structure isolated from Aspergillus microorganisms.
Q: What is the primary use of MSD803?
A: MSD803 is used as a hypocholesteremic and hypolipemic medicament to reduce cholesterol and lipid levels.
Q: Who are the inventors of U.S. Patent 4,231,938?
A: The inventors are Richard L. Monaghan, Alfred W. Alberts, Carl H. Hoffman, and George Albers-Schonberg.
Q: What is the significance of this patent in the pharmaceutical industry?
A: This patent contributed significantly to the development of statins, a class of drugs widely used to lower cholesterol levels.
Q: How can one access detailed information about this patent and related patents?
A: One can use the USPTO's Patent Public Search, Global Dossier, and other international patent databases to access detailed information.
Sources
- USPTO - Search for patents: https://www.uspto.gov/patents/search
- PubChem - Preparation of rosuvastatin: https://pubchem.ncbi.nlm.nih.gov/patent/US-2007167625-A1
- USPTO - Patent Claims Research Dataset: https://www.uspto.gov/ip-policy/economic-research/research-datasets/patent-claims-research-dataset
- Google Patents - United States Patent 4,231,938: https://patentimages.storage.googleapis.com/c9/33/a7/f3c16b72d538c3/US4231938.pdf
- Google Patents - Coenzyme Q10 avec inhibiteurs: https://patents.google.com/patent/EP0383432A1/fr
