United States Patent 10,946,015: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 10,946,015, titled "Stable Pharmaceutical Compositions Comprising a Pyrimidine-Sulfamide," is a significant patent in the pharmaceutical industry, particularly in the development of stable formulations for certain drugs. Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.
Background and Invention
This patent, issued on March 16, 2021, relates to stable pharmaceutical compositions that include a pyrimidine-sulfamide compound or its pharmaceutically acceptable salts, solvates, hydrates, or morphological forms. The invention is crucial for the formulation of drugs like macitentan, used as endothelin receptor antagonists, such as in the treatment of pulmonary arterial hypertension[4][5].
Scope of the Patent
The scope of the patent is defined by its claims, which outline the specific aspects of the invention that are protected. Here are some key aspects:
Claims Overview
The patent includes multiple claims that cover various aspects of the pharmaceutical composition:
- Active Ingredient: The claims specify the use of a pyrimidine-sulfamide compound and its derivatives.
- Formulation Components: The patent details the inclusion of excipients such as sodium starch glycolate, lubricants, and other intra-granular and extra-granular materials[4].
- Manufacturing Process: The claims describe the process of blending, granulation, drying, milling, and compression into tablets or other dosage forms[4].
Specific Claim Details
- Claim 1: This independent claim defines the pharmaceutical composition comprising the pyrimidine-sulfamide compound, along with specified excipients and their proportions.
- Dependent Claims: These claims further specify the types of excipients, their amounts, and the manufacturing steps involved in preparing the composition[4].
Patent Landscape
The patent landscape surrounding US 10,946,015 is complex and involves several related patents and legal actions.
Related Patents
- US 7,094,781: This earlier patent, titled "Sulfamides and Their Use as Endothelin Receptor Antagonists," covers the use of sulfamide compounds as endothelin receptor antagonists. It is closely related to the '015 patent and is also owned by Actelion Ltd[5].
- US 8,367,685 and US 9,265,762: These patents are part of the same family and cover various aspects of the pharmaceutical compositions and their manufacturing processes[2].
Litigation and Legal Actions
The '015 patent has been involved in several legal actions, particularly in the context of generic drug approvals:
- Actelion vs. Mylan: Actelion Inc. has initiated litigation against Mylan for infringement of the '015 patent, among others, in relation to Mylan's Abbreviated New Drug Application (ANDA) for generic macitentan tablets[5].
- Paragraph IV Certifications: Mylan's ANDA included Paragraph IV certifications stating that the patents, including the '015 patent, are invalid, unenforceable, or will not be infringed by their generic product[2].
Examination and Grant Process
The examination process for this patent, like many others, involved narrowing the scope of the claims to ensure clarity and validity:
- Claim Length and Count: Research indicates that narrower claims, both in terms of length and count, are more likely to be granted and result in a shorter examination process[3].
- Patent Maintenance: The patent's maintenance payments and forward citations are indicators of its scope and impact within the industry[3].
Manufacturing Process
The patent details a specific manufacturing process that ensures the stability of the pharmaceutical composition:
- Blending and Granulation: The process involves blending intra-granular materials in a high shear mixer, followed by granulation, drying, and milling[4].
- Tablet Formation: The final steps include blending the milled granules with extra-granular materials, adding lubricants, and compressing the mixture into tablets[4].
Stability and Efficacy
The stability of the pharmaceutical composition is a critical aspect of the patent:
- Dissolution Profiles: The patent includes data on the dissolution profiles of the tablets, ensuring that the active ingredient is released in a controlled manner[4].
- Shelf Life: The stable formulations described in the patent are designed to maintain their efficacy over a longer shelf life, which is essential for pharmaceutical products.
Industry Impact
This patent has significant implications for the pharmaceutical industry:
- Generic Drug Approvals: The litigation surrounding this patent highlights the challenges generic drug manufacturers face in obtaining approvals without infringing on existing patents[5].
- Innovation Incentives: The patent's scope and the associated legal actions influence the incentives for innovation in the pharmaceutical sector, as broader patents can increase licensing and litigation costs[3].
Key Takeaways
- Stable Pharmaceutical Compositions: The patent focuses on stable formulations of pyrimidine-sulfamide compounds.
- Manufacturing Process: The detailed manufacturing process ensures the stability and efficacy of the final product.
- Legal Landscape: The patent is part of a complex legal landscape involving related patents and litigation over generic drug approvals.
- Industry Impact: The patent affects innovation and generic drug approvals in the pharmaceutical industry.
Frequently Asked Questions (FAQs)
What is the main subject of US Patent 10,946,015?
The main subject is stable pharmaceutical compositions comprising a pyrimidine-sulfamide compound or its derivatives.
Who owns the '015 patent?
The '015 patent is owned by Actelion Ltd.
What is the significance of the manufacturing process described in the patent?
The manufacturing process ensures the stability and efficacy of the pharmaceutical composition by detailing specific steps such as blending, granulation, drying, milling, and compression.
Why is this patent involved in litigation?
The patent is involved in litigation due to generic drug manufacturers seeking approval for similar products, which may infringe on the existing patent.
How does this patent impact the pharmaceutical industry?
The patent impacts the industry by influencing innovation, generic drug approvals, and the costs associated with licensing and litigation.
Cited Sources
- US Patent No. 10,946,015 B2 - Stable pharmaceutical compositions comprising a pyrimidine-sulfamide[4].
- FDA Approval Letter for ANDA 211195 - Apotex, Corp. U.S. Agent for Apotex Inc.[2].
- Patent Claims and Patent Scope - Hoover Institution[3].
- Case 1:23-cv-00088-TSK Document 1 - Actelion Inc. vs. Mylan[5].
