United States Patent 11,117,871: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 11,117,871, titled "Crystalline forms of GSK1278863, preparation method and pharmaceutical use thereof," is a significant patent in the pharmaceutical industry, particularly in the field of hypoxia-inducible factor prolyl hydroxylase inhibitors. This patent, assigned to GlaxoSmithKline Intellectual Property (No.2) Limited, covers crucial aspects of the crystalline forms of the compound GSK1278863, their preparation methods, and their pharmaceutical applications.
Technical Field and Background
The patent pertains to the field of pharmaceuticals, specifically focusing on crystalline forms of GSK1278863, a hypoxia-inducible factor prolyl hydroxylase inhibitor. This compound is important in treating conditions related to hypoxia, and the crystalline forms described in the patent enhance its pharmaceutical properties[4].
Crystalline Forms CS1 and CS9
The patent discloses two specific crystalline forms of GSK1278863, designated as Form CS1 and Form CS9. These forms are distinguished by their superior properties compared to prior art solids:
- Solubility and Dissolution Profiles: Forms CS1 and CS9 exhibit good solubility in simulated biological media and pure water, ensuring effective dissolution and absorption of the drug substance in the human body[4].
- Chemical Stability: These crystalline forms have high purity and are stable under various storage conditions, such as 25° C./60% RH, 40° C./75% RH, and 60° C./75% RH[4].
- Hygroscopicity: Unlike prior art solids, Forms CS1 and CS9 have low hygroscopicity, making them more suitable for pharmaceutical formulations[1].
Preparation Methods
The patent details the methods for preparing these crystalline forms. The process involves specific conditions and solvents to achieve the desired crystalline structures. For instance, the use of solvents like acetone or methyl isobutyl ketone is mentioned in the preparation process[1].
Pharmaceutical Use
The crystalline forms of GSK1278863 are intended for therapeutic use, particularly in treating conditions related to hypoxia. The patent describes pharmaceutical compositions that include a therapeutically effective amount of Form CS1 or Form CS9, along with pharmaceutically acceptable carriers, diluents, or excipients[4].
Patent Claims
The patent includes 16 claims that cover various aspects of the crystalline forms, their preparation, and their use:
- Claims to Crystalline Forms: Specific claims are made to the crystalline forms CS1 and CS9, detailing their structural characteristics and properties[1].
- Claims to Preparation Methods: The patent claims the methods for preparing these crystalline forms, including the use of specific solvents and conditions[1].
- Claims to Pharmaceutical Compositions: Claims are also made to pharmaceutical compositions that include these crystalline forms, ensuring their therapeutic efficacy[4].
Patent Landscape and Regulatory Implications
The patent landscape for pharmaceuticals, especially for crystalline forms of active pharmaceutical ingredients (APIs), is complex and heavily regulated.
- Orange Book Listings: Patents like US 11,117,871 can be listed in the FDA's Orange Book, which affects the approval of generic versions of the drug. Improper listing of patents can delay the entry of generic products, as seen in cases like Teva Branded Pharmaceutical Products R&D, Inc. v. Amneal Pharmaceuticals[2].
- Enablement and Written Description Requirements: The Federal Circuit's recent jurisprudence on 35 U.S.C. § 112 has introduced heightened standards for enablement and written description, particularly affecting genus claims in pharmaceutical and biotechnology patents. This has created uncertainty and challenges for innovators in claiming the full scope of their inventions[3].
Impact on Pharmaceutical Industry
The patent has significant implications for the pharmaceutical industry:
- Innovation and Competition: The patent protects GlaxoSmithKline's innovation in developing superior crystalline forms of GSK1278863, providing a competitive edge in the market. However, the stringent requirements for patent claims under 35 U.S.C. § 112 can make it challenging for other innovators to secure similar protections[3].
- Drug Bioavailability and Efficacy: The good solubility, dissolution profiles, and chemical stability of Forms CS1 and CS9 ensure better drug absorption and efficacy, which is crucial for patient outcomes[4].
Challenges and Future Directions
The current patent landscape presents several challenges:
- Navigating Regulatory Requirements: Innovators must carefully navigate the regulatory requirements, especially the enablement and written description standards, to secure robust patent protection[3].
- Balancing Broad and Narrow Claims: The need to balance between claiming the full scope of an invention and avoiding overly broad claims that might be invalidated is a significant challenge. Narrow claims, while safer, can be easily circumvented by competitors[3].
Key Takeaways
- Superior Crystalline Forms: The patent covers superior crystalline forms of GSK1278863 with enhanced solubility, dissolution profiles, and chemical stability.
- Regulatory Implications: The patent's listing in the Orange Book and compliance with 35 U.S.C. § 112 requirements are critical for its validity and enforcement.
- Industry Impact: The patent affects innovation, competition, and drug efficacy in the pharmaceutical industry.
- Challenges: Innovators face challenges in navigating regulatory requirements and balancing claim breadth.
Frequently Asked Questions (FAQs)
What are the key benefits of the crystalline forms CS1 and CS9 of GSK1278863?
The key benefits include good solubility, high dissolution rates, and high purity, which enhance drug absorption and efficacy.
How do the preparation methods for Forms CS1 and CS9 differ from prior art methods?
The preparation methods involve specific solvents and conditions that result in crystalline forms with superior properties compared to prior art solids.
What are the regulatory implications of listing this patent in the FDA's Orange Book?
Listing this patent in the Orange Book can delay the approval of generic versions of the drug, as it requires the FDA to withhold approval for 30 months if the listed patent is not delisted.
How has the Federal Circuit's jurisprudence on 35 U.S.C. § 112 affected pharmaceutical patents?
The Federal Circuit's recent interpretations have introduced heightened standards for enablement and written description, making it challenging for innovators to secure robust patent protection for genus claims.
What are the potential challenges for innovators in the pharmaceutical industry due to this patent landscape?
Innovators face challenges in balancing between broad and narrow claims, navigating regulatory requirements, and ensuring compliance with 35 U.S.C. § 112 standards.
Cited Sources:
- United States Patent and Trademark Office. US11117871B2 - Crystalline forms of GSK1278863, preparation method and pharmaceutical use thereof. September 14, 2021.
- United States Court of Appeals for the Federal Circuit. Teva Branded Pharmaceutical Products R&D, Inc. v. Amneal Pharmaceuticals. December 20, 2024.
- University of Illinois Chicago. Eviscerating Patent Scope. May 2, 2022.
- Google Patents. US11117871B2 - Crystalline forms of GSK1278863, preparation method and pharmaceutical use thereof. September 14, 2021.
