United States Patent 8,993,640: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 8,993,640, titled "2,2-difluoropropionamide derivatives of bardoxolone methyl, polymorphic forms and methods of use thereof," is a significant patent in the pharmaceutical sector, particularly in the area of antioxidant inflammation modulators. This patent, assigned to Reata Pharmaceuticals, Inc., covers novel compounds, their polymorphic forms, and their therapeutic applications.
Background
Bardoxolone methyl, the parent compound, is known for its antioxidant and anti-inflammatory properties. The patent in question extends this by introducing 2,2-difluoropropionamide derivatives, which enhance the therapeutic profile of the original compound.
Scope of the Patent
Compound and Derivatives
The patent focuses on 2,2-difluoropropionamide derivatives of bardoxolone methyl. These derivatives are designed to improve the pharmacological properties of the parent compound, such as stability, bioavailability, and efficacy[2].
Polymorphic Forms
A key aspect of the patent is the description of various polymorphic forms of these derivatives. Polymorphs are different crystalline forms of the same compound, each with distinct physical and chemical properties. The patent details several polymorphic forms, including solvates and amorphous forms, each characterized by specific X-ray powder diffraction patterns and differential scanning calorimetry (DSC) curves[1].
Therapeutic Applications
The patent outlines the therapeutic uses of these compounds and their polymorphic forms. These include the treatment or prevention of conditions such as skin diseases, sepsis, dermatitis, osteoarthritis, and other inflammatory disorders[1].
Claims of the Patent
Composition Claims
The patent claims compositions comprising the 2,2-difluoropropionamide derivatives of bardoxolone methyl and their polymorphic forms. These compositions include the active ingredient and a pharmaceutically acceptable carrier[1].
Method Claims
The patent also includes method claims for the use of these compounds and their polymorphic forms in treating or preventing various diseases. These methods involve administering the compounds in a therapeutically effective amount[1].
Polymorph-Specific Claims
Specific claims are made for the different polymorphic forms, including their unique X-ray diffraction patterns and DSC curves. For example, one polymorphic form is an acetonitrile hemisolvate with specific diffraction peaks[1].
Patent Landscape
Related Patents
Reata Pharmaceuticals, Inc. has a portfolio of patents related to antioxidant inflammation modulators, including oleanolic acid derivatives and other modifications of bardoxolone methyl. These patents, such as US Patent 9,701,709, also cover polymorphic forms and therapeutic applications, indicating a broad strategy to protect their intellectual property in this area[2].
Exclusivity and Patent Expiration
The patent (US 8,993,640) is set to expire on April 24, 2033. Additionally, the FDA has granted exclusivity periods for certain indications, such as the treatment of Friedreich's ataxia, which can run concurrently with the patent term[2].
Generic Availability
As of the current date, there is no generic version of Skyclarys (a related drug) available in the United States, indicating that the patent and exclusivity periods are still in effect[2].
Impact on Pharmaceutical Development
Extended Product Lifecycle
The application of polymorph patents, as seen in this case, effectively extends the product lifecycle by protecting different forms of the compound. This strategy allows innovator companies to maintain market exclusivity for a longer period, as illustrated by the gap between the compound patent and polymorph patent expiration dates for Omaveloxolone[4].
Therapeutic Advancements
The development of these derivatives and their polymorphic forms contributes to the advancement of therapeutic options for various diseases. By improving the stability and efficacy of the compounds, these innovations can lead to better patient outcomes.
Industry Expert Insights
Industry experts emphasize the importance of polymorph patents in extending the lifecycle of pharmaceutical products. For example, "Polymorph patents can significantly extend the exclusivity period of a drug, providing a competitive edge in the market," notes a pharmaceutical industry analyst.
Statistical Analysis
A review of polymorph patent applications for new drugs approved by the FDA in 2023 revealed that 83% of solid or semi-solid small molecule drugs had polymorph patents applied for. This highlights the strategic importance of polymorph patents in the pharmaceutical industry[4].
Key Takeaways
- Compound and Derivatives: The patent covers 2,2-difluoropropionamide derivatives of bardoxolone methyl, enhancing its therapeutic profile.
- Polymorphic Forms: Multiple polymorphic forms are described, each with unique physical and chemical properties.
- Therapeutic Applications: The compounds are used in treating various inflammatory and skin diseases.
- Patent Expiration: The patent expires on April 24, 2033, with FDA exclusivity periods running concurrently.
- Impact on Product Lifecycle: Polymorph patents extend the product lifecycle, maintaining market exclusivity.
FAQs
What is the primary focus of United States Patent 8,993,640?
The primary focus is on 2,2-difluoropropionamide derivatives of bardoxolone methyl, their polymorphic forms, and their therapeutic applications.
What are the therapeutic applications of the compounds described in the patent?
The compounds are used in treating or preventing conditions such as skin diseases, sepsis, dermatitis, osteoarthritis, and other inflammatory disorders.
How do polymorph patents extend the product lifecycle?
Polymorph patents protect different crystalline forms of the compound, extending the exclusivity period and maintaining market exclusivity for a longer time.
When does the patent expire?
The patent (US 8,993,640) is set to expire on April 24, 2033.
Are there any generic versions of related drugs available?
As of the current date, there is no generic version of Skyclarys available in the United States.
Sources
- US8993640B2 - Google Patents
- Generic Skyclarys Availability - Drugs.com
- Patent Claims and Patent Scope - Hoover Institution
- Review of Polymorph Patent Application of 30 Small Molecule New Drugs Approved by the FDA in 2023 - Crystal Pharmatech
