United States Patent 6,458,811: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 6,458,811, titled "Benzothiophenes formulations containing same and methods," is a patent that delves into the formulation, preparation, and application of specific benzothiophene compounds. This analysis will explore the scope, claims, and the broader patent landscape surrounding this invention.
Background of the Patent
The patent, filed on August 30, 1995, and granted on October 1, 2002, pertains to compounds of the benzothiophene class, particularly those with pharmaceutical applications. The invention is characterized by its specific chemical structure and the methods used for its preparation and formulation[1].
Scope of the Patent
Chemical Structure
The patent focuses on compounds of formula I, which are benzothiophenes with specific substituents. These compounds include a 6-hydroxyl group and a 2-(4-hydroxyphenyl) group, with additional modifications such as acylation and deprotection steps to form the final compounds. The substituents R4, R5, and R6 are defined as hydrogen or C1-C4 alkoxy, hydrogen or C1-C4 alkyl, and chloro, bromo, or hydroxyl, respectively[1].
Particle Size and Formulation
A critical aspect of the patent is the particle size of the compounds. The invention specifies that the mean particle size of the compounds should be less than about 25 microns, preferably between about 5 and 20 microns. Additionally, at least 90% of the particles should have a size of less than about 50 microns, preferably less than about 35 microns. This precise control over particle size is crucial for the pharmaceutical efficacy and stability of the formulations[1].
Claims of the Patent
Independent Claims
The patent includes several independent claims that define the scope of the invention. These claims cover:
- The compounds of formula I and their pharmaceutically acceptable salts and solvates.
- The specific particle size distribution of the compounds.
- Methods for preparing these compounds, including protection, acylation, and deprotection steps[1].
Dependent Claims
Dependent claims further specify the invention by detailing:
- The preferred range of particle sizes.
- The presence of specific solvents and their molar equivalents.
- The analytical purity of the compounds, such as the amount of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride and the amount of 1,2-dichloroethane present in the crystalline material[1].
Patent Landscape
Prior Art and Related Patents
The patent references several prior art patents and applications, including U.S. Pat. Nos. 4,133,814, 4,418,068, and 4,380,635, as well as European Patent Application 95306050.6. These prior art documents provide background on the synthesis and formulation of similar compounds, which the current invention builds upon and distinguishes itself from[1].
Competitive Landscape
The benzothiophene class of compounds is significant in pharmaceutical research, particularly in the development of drugs like raloxifene, which is used for the treatment of osteoporosis. The competitive landscape includes other patents and formulations related to benzothiophenes, each with their own unique claims and applications. This patent's focus on specific particle size and formulation methods sets it apart in this competitive space[1].
Analytical and Practical Applications
High Performance Liquid Chromatography (HPLC)
The patent describes the use of HPLC to determine the purity of the compounds, specifically mentioning that the amount of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride is about 87.1% as determined by HPLC assay[1].
Single Crystal X-ray Analysis
The preparation of a large, analytically pure single crystal for single crystal X-ray analysis is also detailed. This method involves placing a saturated methanolic solution of the compound in an atmosphere saturated with 1,2-dichloroethane, highlighting the meticulous approach to ensuring the crystalline structure and purity of the compound[1].
Intellectual Property Strategy
Patent Analytics
To fully understand the protection and coverage provided by this patent, patent analytics tools can be employed. These tools help in categorizing patents by claims and scope concepts, making it easier to identify gaps or opportunities in the intellectual property landscape. For example, using ClaimScape® software, one can generate interactive claim charts to review patent coverage and determine if there are areas where additional claim coverage is needed[3].
Global Patent Search
The patent landscape is not limited to the United States. Searching international patent offices such as the European Patent Office (EPO), Japan Patent Office (JPO), and World Intellectual Property Organization (WIPO) can provide a comprehensive view of similar patents and applications worldwide. This global search helps in understanding the international protection and potential infringement risks[4].
Future Implications and Opportunities
Pharmaceutical Applications
The precise control over particle size and formulation methods described in this patent has significant implications for pharmaceutical applications. These methods can be applied to other compounds to enhance their efficacy and stability, opening up new avenues for drug development.
Licensing and Collaboration
The unique claims and methods described in this patent present opportunities for licensing and collaboration. Pharmaceutical companies can leverage this technology to improve their existing formulations or develop new drugs, thereby expanding their product portfolio.
Key Takeaways
- Specific Chemical Structure: The patent focuses on benzothiophene compounds with specific substituents and a defined chemical structure.
- Particle Size Control: The invention emphasizes the importance of precise particle size control for pharmaceutical efficacy.
- Analytical Purity: Methods such as HPLC and single crystal X-ray analysis are used to ensure high purity of the compounds.
- Intellectual Property Strategy: Patent analytics and global patent searches are crucial for understanding the patent landscape and identifying opportunities.
- Future Implications: The patent's methods have broad implications for pharmaceutical research and development.
FAQs
What is the main focus of United States Patent 6,458,811?
The main focus of this patent is on the formulation, preparation, and application of specific benzothiophene compounds, particularly emphasizing particle size control and analytical purity.
How does the patent specify particle size?
The patent specifies that the mean particle size of the compounds should be less than about 25 microns, with at least 90% of the particles having a size of less than about 50 microns.
What analytical methods are used to determine purity?
The patent describes the use of High Performance Liquid Chromatography (HPLC) and single crystal X-ray analysis to determine the purity of the compounds.
Why is particle size control important in this patent?
Particle size control is crucial for the pharmaceutical efficacy and stability of the formulations, ensuring that the compounds are effective and consistent in their application.
How can patent analytics help in understanding this patent?
Patent analytics tools help in categorizing patents by claims and scope concepts, making it easier to identify gaps or opportunities in the intellectual property landscape and ensuring comprehensive protection.
Sources
- US6458811B1 - Benzothiophenes formulations containing same and methods - Google Patents
- U.S. Patent and Trademark Office (USPTO) - USA.gov
- Patent Analytics - SLWIP
- Search for patents - USPTO
- U.S. Patent Small Claims Court - ACUS
