Detailed Analysis of the Scope and Claims of United States Patent 7,846,961
Introduction
United States Patent 7,846,961, granted to Les Laboratoires Servier, pertains to the α crystalline form of the arginine salt of perindopril, a process for its preparation, and pharmaceutical compositions containing it. This patent is crucial for the development and use of perindopril, an angiotensin-converting enzyme (ACE) inhibitor, in treating cardiovascular diseases such as arterial hypertension and heart failure.
Background and Context
Perindopril is a well-known ACE inhibitor used to manage hypertension and heart failure. The stability and processability of its crystalline forms are critical for its pharmaceutical applications. The inventors, Gérard Coquerel, Loïc Lefebvre, Jean-Claude Souvie, and Pascale Authouart, have developed a specific crystalline form of the arginine salt of perindopril that enhances its stability, filtration, drying, and formulation properties[2][4].
Scope of the Patent
Crystalline Form
The patent specifically describes the α crystalline form of the arginine salt of perindopril, characterized by distinct powder X-ray diffraction peaks. These peaks are measured using a diffractometer with a copper anti-cathode and expressed in terms of the angle 2 theta (°). The key peaks are at 4.5, 7.9, and 13.5 degrees, with additional peaks at 17.5 and 20.6 degrees for a more detailed characterization[1][4].
Process for Preparation
The patent outlines a method for preparing this crystalline form. Perindopril is dissolved in water with L-arginine, followed by the addition of an apolar solvent (e.g., methylcyclohexane, cyclohexane, toluene) and a polar solvent (e.g., dimethyl sulphoxide). The resulting crystals are then filtered, washed, and dried[1][4].
Claims of the Patent
The patent includes several claims that protect the specific crystalline form, the process for its preparation, and the pharmaceutical compositions containing it.
Independent Claims
- Claim 1: The α crystalline form of the arginine salt of perindopril characterized by specific X-ray diffraction peaks.
- Claim 2: The process for preparing the α crystalline form.
- Claim 3: Pharmaceutical compositions containing the α crystalline form of the arginine salt of perindopril[2][4].
Dependent Claims
These claims further specify the conditions and materials used in the process, such as the types of solvents and the steps involved in filtering, washing, and drying the crystals[2][4].
Patent Landscape
Family Applications
The patent is part of a global patent family with applications in various countries, including the United States, Europe, Japan, Korea, China, Australia, Brazil, Canada, and others. This extensive coverage ensures broad protection for the invention across different jurisdictions[4].
Priority Dates
The patent has a priority date of February 28, 2006, based on the French patent application FR0601748. The international application PCT/FR2007/000335 was filed on February 26, 2007[4].
Related Patents and Publications
The patent references several prior art documents, including publications on solid-state chemistry of drugs and drug delivery reviews. These references highlight the importance of crystalline forms in pharmaceuticals and the challenges associated with their preparation and stability[2].
Impact on Pharmaceutical Industry
Stability and Processability
The α crystalline form of the arginine salt of perindopril offers significant improvements in stability, filtration, drying, and ease of formulation. These characteristics are crucial for the manufacture and storage of pharmaceutical products, ensuring consistent quality and efficacy[1][4].
Therapeutic Applications
Perindopril, as an ACE inhibitor, plays a critical role in treating cardiovascular diseases. The specific crystalline form described in this patent enhances the therapeutic benefits by ensuring a stable and effective formulation[4].
Patent Analytics and Claim Coverage
To fully understand the protection and value of this patent, patent analytics tools can be employed. These tools help in categorizing patents by claims and scope concepts, identifying gaps or opportunities in the patent landscape, and determining the coverage of specific technologies. For instance, a Claim Coverage Matrix can show which patents and claims are actively protecting the intellectual property related to perindopril and its crystalline forms[3].
Key Takeaways
- The patent protects a specific α crystalline form of the arginine salt of perindopril, characterized by distinct X-ray diffraction peaks.
- The process for preparing this crystalline form involves dissolving perindopril in water with L-arginine and adding apolar and polar solvents.
- The patent includes claims for the crystalline form, the preparation process, and pharmaceutical compositions.
- The patent is part of a global family with extensive jurisdictional coverage.
- The invention significantly improves the stability and processability of perindopril, enhancing its therapeutic applications.
FAQs
What is the significance of the α crystalline form of the arginine salt of perindopril?
The α crystalline form of the arginine salt of perindopril is significant because it enhances the stability, filtration, drying, and formulation properties of perindopril, making it more suitable for pharmaceutical applications.
How is the α crystalline form of the arginine salt of perindopril prepared?
The α crystalline form is prepared by dissolving perindopril in water with L-arginine, followed by the addition of an apolar solvent and a polar solvent. The resulting crystals are then filtered, washed, and dried.
What are the therapeutic applications of perindopril?
Perindopril is used to treat cardiovascular diseases, particularly arterial hypertension and heart failure, by inhibiting the angiotensin-converting enzyme (ACE).
Why is patent analytics important for this invention?
Patent analytics helps in understanding the scope and coverage of the patent, identifying gaps or opportunities in the patent landscape, and determining the value of the patent claims in protecting the intellectual property related to perindopril.
What is the global coverage of this patent?
The patent is part of a global family with applications in multiple countries, including the United States, Europe, Japan, Korea, China, Australia, Brazil, Canada, and others.
Cited Sources
- United States Patent and Trademark Office, "α crystalline form of the arginine salt of perindopril, a process for its preparation and pharmaceutical compositions containing it," US7846961B2.
- Justia Patents, "α crystalline form of the arginine salt of perindopril, a process for its preparation and pharmaceutical compositions containing it," US7846961B2.
- SLWIP, "Patent Analytics | Intellectual Property Law."
- Google Patents, "α crystalline form of the arginine salt of perindopril, a process for its preparation and pharmaceutical compositions containing it," US7846961B2.
