United States Patent 7,501,409: A Detailed Analysis of Scope and Claims
Introduction
The United States Patent 7,501,409, titled "Preparations for oral administration," is a significant patent in the pharmaceutical field, particularly focusing on formulations for oral drugs. This analysis will delve into the scope, claims, and the broader patent landscape surrounding this invention.
Patent Overview
Publication and Status
The patent was published on March 10, 2009, and has since expired. It was assigned the publication number US7501409B2[1].
Scope of the Patent
Medicinal Substance
The patent revolves around preparations for oral administration containing a medicinal substance with cGMP-specific phosphodiesterase inhibitory activity, commonly known as PDE-V inhibitors. These substances are particularly useful in treating conditions such as penile erectile dysfunction, pulmonary hypertension, and various cardiovascular diseases[1].
Solubility Characteristics
A key aspect of the patent is the solubility profile of the medicinal substance. The substance must show a decrease in solubility in neutral and alkaline regions (pH 4 or above), with solubility at pH 6.8 being 1/10 or less compared to the solubility at pH 1.2[1].
Claims of the Patent
Active Ingredients
The patent claims include various formulations of PDE-V inhibitors, such as those with specific chemical structures. For example, the claims cover compounds with an optionally substituted lower alkyl group, a group of the formula —NH-Q-R3, or a group of the formula —NH—R4, where R3 and R4 are defined as specific types of heterocyclic and cycloalkyl groups, respectively[1].
Pharmaceutical Formulations
The patent describes the preparation of solid pharmaceutical formulations, including tablets, pills, and other oral forms. These preparations can be made using conventional methods, involving the compounding of the medicinal substance with acidic substances and optionally calcium carbonate, along with other pharmaceutically acceptable additives[1].
Specific Examples
The patent includes specific examples of formulations, such as those described in Examples 7 and 8, which detail the preparation and dissolution profiles of the medicinal substances. These examples illustrate how the claimed formulations can be prepared and their performance in terms of dissolution rates[1].
Pharmaceutical Applications
Therapeutic Uses
The patent highlights the therapeutic applications of the PDE-V inhibitors, which include the treatment of penile erectile dysfunction, pulmonary hypertension, gastroparesis diabeticorum, hypertension, angina pectoris, myocardial infarction, chronic and acute heart failure, female sexual dysfunction, prostatic hyperplasia, asthma, diarrhea, constipation, and achalasia[1].
Stability and Operationality
The patent also addresses the stability and operationality of the compounds. It notes that compounds which show disadvantages regarding stability or operationality in the form of acid addition salts can be conveniently used in the free form in these preparations[1].
Patent Landscape
Related Patents and Litigation
The patent landscape around US7501409B2 involves various other patents and legal disputes. For instance, the discussion around patent claims and their validity is a common theme, as seen in cases like Nalpropion Pharmaceuticals, Inc. v. Actavis Labs. FL, Inc., where the validity of patent claims was challenged based on written description and obviousness grounds[2].
Metrics for Patent Scope
Research on patent scope, such as the paper by SSRN, highlights the importance of metrics like independent claim length and independent claim count in measuring patent breadth. These metrics can influence the examination process and the likelihood of patent grant, which is relevant when analyzing the scope and claims of US7501409B2[3].
Industry Impact
Pharmaceutical Development
The patent has significant implications for pharmaceutical development, particularly in the formulation of oral drugs. Companies like VIVUS Inc., which focus on developing innovative drug candidates, would need to consider the scope and claims of such patents to avoid infringement and ensure the novelty of their own formulations[4].
Key Takeaways
- Medicinal Substance: The patent focuses on PDE-V inhibitors with specific solubility characteristics.
- Formulations: It describes various solid pharmaceutical formulations and their preparation methods.
- Therapeutic Uses: The patent covers a wide range of therapeutic applications, including erectile dysfunction and cardiovascular diseases.
- Stability and Operationality: It addresses the use of compounds in free form to overcome stability and operational issues.
- Patent Landscape: The patent is part of a broader landscape involving legal disputes and metrics for patent scope.
FAQs
What is the main focus of United States Patent 7,501,409?
The main focus of the patent is on preparations for oral administration containing medicinal substances with cGMP-specific phosphodiesterase inhibitory activity (PDE-V inhibitors).
What are the therapeutic applications of the PDE-V inhibitors described in the patent?
The therapeutic applications include the treatment of penile erectile dysfunction, pulmonary hypertension, gastroparesis diabeticorum, hypertension, and various other cardiovascular and non-cardiovascular conditions.
How are the formulations described in the patent prepared?
The formulations are prepared using conventional methods involving the compounding of the medicinal substance with acidic substances and optionally calcium carbonate, along with other pharmaceutically acceptable additives.
What is the significance of solubility characteristics in the patent?
The solubility characteristics are crucial as the substances must show a decrease in solubility in neutral and alkaline regions (pH 4 or above), which affects their bioavailability and efficacy.
How does the patent impact pharmaceutical development?
The patent impacts pharmaceutical development by providing specific formulations and methods for preparing oral drugs, which other companies must consider to avoid infringement and ensure the novelty of their own formulations.
What metrics are used to measure the scope of patents like US7501409B2?
Metrics such as independent claim length and independent claim count are used to measure the scope of patents, which can influence the examination process and the likelihood of patent grant.
Sources
- US7501409B2 - Preparations for oral administration - Google Patents
- Nalpropion Pharmaceuticals, Inc. v. Actavis Labs. FL, Inc.
- Patent Claims and Patent Scope - Search eLibrary :: SSRN
- VIVUS INC - Annual Reports
