United States Patent 5,712,279: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 5,712,279, titled "Inhibitors of microsomal triglyceride transfer protein and method," is a significant patent in the field of pharmaceuticals, particularly in the treatment of hyperlipidemia and atherosclerosis. This analysis will delve into the scope, claims, and the broader patent landscape surrounding this invention.
Background
The patent, filed on October 24, 1995, and granted on January 27, 1998, pertains to compounds that inhibit microsomal triglyceride transfer protein (MTP). MTP is crucial in the assembly and secretion of very-low-density lipoproteins (VLDL) from the liver, and its inhibition can lead to reduced serum lipid levels, thereby treating conditions such as hyperlipidemia and atherosclerosis[1].
Scope of the Patent
The scope of the patent encompasses a range of compounds designed to inhibit MTP. These compounds are described in detail, including their chemical structures and the methods for their synthesis. The patent also covers the therapeutic use of these compounds in treating disorders associated with hyperlipidemia.
Chemical Compounds
The patent describes various chemical compounds that act as MTP inhibitors. These include heterocyclic compounds containing two or more hetero rings, with specific substitutions and linkages. For example, the patent details compounds where R12 can be hydrogen, alkyl, alkenyl, aryl, or other functional groups, and Z can be a bond, oxygen, sulfur, nitrogen-alkyl, or alkylene/alkenylene chains of up to 5 carbon atoms[1].
Therapeutic Use
The therapeutic scope of the patent is focused on treating hyperlipidemia and atherosclerosis. By inhibiting MTP, these compounds reduce the secretion of VLDL from the liver, leading to lower serum lipid levels. This is particularly beneficial for patients with elevated cholesterol and triglyceride levels, who are at risk of developing cardiovascular diseases.
Claims of the Patent
The patent includes several claims that define the scope of protection for the invention.
Independent Claims
- Claim 1 describes the chemical compounds that inhibit MTP, specifying the structural requirements and functional groups.
- Claim 2 covers the method of treating hyperlipidemia and atherosclerosis using these compounds.
- Claim 3 pertains to pharmaceutical compositions containing the MTP inhibitors and a pharmaceutically acceptable carrier[1].
Dependent Claims
The dependent claims further specify the types of compounds, their synthesis methods, and the dosage forms of the pharmaceutical compositions. These claims provide a detailed description of the preferred embodiments of the invention.
Patent Landscape
The patent landscape surrounding US 5,712,279 is complex and involves various other patents and research in the field of lipid metabolism and cardiovascular diseases.
Related Patents
Other patents, such as the Canadian Patent Application CA 2626422, also focus on methods for treating disorders associated with hyperlipidemia. These patents often involve different mechanisms of action or alternative compounds but share the common goal of reducing serum lipid levels[2].
Research and Development
The development of MTP inhibitors is part of a broader research effort into lipid metabolism and cardiovascular health. Studies and patents in this area often intersect with other fields such as genetics, nutrition, and pharmacology.
Industry Impact
The invention covered by US 5,712,279 has significant implications for the pharmaceutical industry. Companies involved in the development of cardiovascular treatments have shown interest in MTP inhibitors as a potential therapeutic option. However, the landscape is also marked by challenges such as regulatory approvals, clinical trials, and competition from other therapeutic approaches.
Legal Status and Expiration
The patent US 5,712,279 has expired, as it was granted for a term of 20 years from the filing date. This expiration means that the invention is now in the public domain, and the compounds and methods described can be freely used without infringing on the original patent.
Impact on Public Health
The compounds and methods described in this patent have the potential to significantly impact public health by providing effective treatments for hyperlipidemia and atherosclerosis. These conditions are major risk factors for cardiovascular diseases, which are among the leading causes of mortality worldwide.
"By inhibiting MTP, these compounds reduce the secretion of VLDL from the liver, leading to lower serum lipid levels. This is particularly beneficial for patients with elevated cholesterol and triglyceride levels, who are at risk of developing cardiovascular diseases."[1]
Challenges and Future Directions
Despite the potential benefits, the development and use of MTP inhibitors face several challenges. These include the need for extensive clinical trials to ensure safety and efficacy, regulatory approvals, and the ongoing competition from other therapeutic approaches.
Clinical Trials
Clinical trials are crucial for establishing the safety and efficacy of MTP inhibitors. These trials must demonstrate that the compounds can effectively reduce serum lipid levels without significant adverse effects.
Regulatory Approvals
Obtaining regulatory approvals is a critical step in bringing these compounds to market. Regulatory bodies such as the FDA in the United States and similar agencies in other countries must review the data from clinical trials before approving these drugs for use.
Market Competition
The market for cardiovascular treatments is highly competitive, with various existing and emerging therapies. MTP inhibitors must demonstrate a significant advantage over existing treatments to gain market share.
Key Takeaways
- Invention Scope: The patent covers compounds that inhibit microsomal triglyceride transfer protein (MTP) and their use in treating hyperlipidemia and atherosclerosis.
- Chemical Compounds: The patent describes specific chemical structures and synthesis methods for these compounds.
- Therapeutic Use: The compounds are used to reduce serum lipid levels by inhibiting VLDL secretion from the liver.
- Patent Expiration: The patent has expired, making the invention public domain.
- Public Health Impact: The invention has significant potential to improve public health by providing effective treatments for cardiovascular risk factors.
FAQs
What is the primary mechanism of action of the compounds described in US 5,712,279?
The primary mechanism of action is the inhibition of microsomal triglyceride transfer protein (MTP), which reduces the secretion of very-low-density lipoproteins (VLDL) from the liver.
What conditions are treated by the compounds described in this patent?
The compounds are used to treat hyperlipidemia and atherosclerosis.
Has the patent US 5,712,279 expired?
Yes, the patent has expired, as it was granted for a term of 20 years from the filing date.
What are the challenges in developing MTP inhibitors as therapeutic agents?
The challenges include the need for extensive clinical trials, regulatory approvals, and competition from other therapeutic approaches.
How do MTP inhibitors impact public health?
MTP inhibitors can significantly impact public health by providing effective treatments for hyperlipidemia and atherosclerosis, which are major risk factors for cardiovascular diseases.
Are there other patents related to treating hyperlipidemia?
Yes, there are other patents and research efforts focused on treating hyperlipidemia, often involving different mechanisms of action or alternative compounds.
Sources
- US5712279A - Inhibitors of microsomal triglyceride transfer protein and method - Google Patents
- Patent 2626422 Summary - Canadian Patents Database
- Patent Claims Research Dataset - USPTO
- Search for patents - USPTO
- PTAB Institutes Kyle Bass IPRs Against Juxtapid Patents | Foley & Lardner LLP - JD Supra
