Detailed Analysis of the Scope and Claims of United States Patent 8,168,793
Introduction
United States Patent 8,168,793, titled "Nitrocatechol derivatives as COMT inhibitors," is a significant patent in the pharmaceutical industry, particularly in the treatment of central and peripheral nervous system disorders. This patent, assigned to BIAL-Portela & CA, S.A., covers a range of compounds with potential therapeutic applications.
Background
The patent was issued on May 1, 2012, and is set to expire on May 12, 2027. The inventors include David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto Dos Santos Ferreira, and Patricio Manuel Vieira Araújo Soares da Silva[5].
Scope of the Patent
Pharmaceutical Properties
The patent describes new compounds of the nitrocatechol derivative class, which have valuable pharmaceutical properties. These compounds are designed to inhibit catechol-O-methyltransferase (COMT), an enzyme involved in the metabolism of catecholamines such as dopamine, norepinephrine, and epinephrine. COMT inhibitors are crucial in the treatment of Parkinson's disease and other neurological disorders[5].
Chemical Structure
The compounds covered by this patent are defined by a specific chemical structure, denoted as formula I. These nitrocatechol derivatives include various substitutions and modifications that enhance their pharmacological activity and stability. The detailed structural formulas and synthetic methods are outlined in the patent to ensure clarity and reproducibility[1][5].
Claims of the Patent
Independent Claims
The patent includes several independent claims that define the scope of the invention. These claims cover:
- The chemical compounds themselves, including their structural formulas and specific derivatives.
- Pharmaceutical formulations comprising these compounds, such as salts, esters, hydrates, solvates, and other derivatives.
- Methods of making these compounds and formulations, including synthetic routes and purification processes[1][5].
Dependent Claims
Dependent claims further specify the invention by detailing particular aspects of the compounds and methods. These include:
- Specific substituents and functional groups that can be attached to the core structure.
- Various solvents and reagents used in the synthesis.
- Conditions for the reactions, such as temperature and catalysts[1].
Patent Landscape
Related Patents
The patent landscape surrounding U.S. Patent 8,168,793 includes several related patents that expand on the original invention. These include:
- Patent 9,550,759: Also related to nitrocatechol derivatives as COMT inhibitors, issued on January 24, 2017.
- Patent 10,071,085: Covers pharmaceutical formulations comprising nitrocatechol derivatives, issued on September 11, 2018.
- Patent 10,583,130: Similar to the previous one, issued on March 10, 2020. All these patents have a common expiration date of March 31, 2030[5].
Patent Term Extension
The patent term for U.S. Patent 8,168,793, along with related patents (8,524,746, 9,550,759, and 10,071,085), has been subject to extension applications based on the FDA's approval of the drug ONGENTYS (opicapone). These applications were filed under 35 U.S.C. 156, which allows for patent term extension due to regulatory review periods[2].
Manufacturing and Intermediate Compounds
The patent also details methods for manufacturing the active pharmaceutical ingredient, opicapone, and its intermediates. These methods involve specific chemical reactions and conditions to ensure the production of high-quality compounds. For example, U.S. Patent 9,126,988 describes a method involving the nitration of vanillic acid and subsequent conversion steps to produce the desired intermediate compounds[4].
Clinical Applications
The compounds described in this patent are primarily used in the treatment of Parkinson's disease as adjunct therapy. Opicapone, the drug developed from these compounds, was approved by the European Medicines Agency (EMA) in 2016 and is marketed under the brand name ONGENTYS. It works by inhibiting COMT, thereby increasing the availability of levodopa in the brain, which is beneficial for patients with Parkinson's disease[4].
Exclusivity and Generic Availability
As of the current date, there is no therapeutically equivalent generic version of ONGENTYS available in the United States. The exclusivity period granted by the FDA, combined with the patent protection, ensures that BIAL-Portela & CA, S.A. maintains exclusive marketing rights for the drug until the patent expires[5].
Conclusion
United States Patent 8,168,793 is a pivotal patent in the field of neuropharmacology, particularly for the treatment of Parkinson's disease. The patent's scope encompasses a range of nitrocatechol derivatives with COMT inhibitory activity, along with detailed methods for their synthesis and formulation. The related patents and patent term extension applications further solidify the intellectual property landscape surrounding these compounds.
Key Takeaways
- Chemical Structure: The patent covers nitrocatechol derivatives with specific structural formulas.
- Pharmaceutical Applications: These compounds are used as COMT inhibitors in the treatment of Parkinson's disease.
- Manufacturing Methods: Detailed synthetic routes and conditions are provided for the production of the active pharmaceutical ingredient and its intermediates.
- Patent Landscape: Related patents extend the scope and protection of the original invention.
- Exclusivity: No generic version of ONGENTYS is currently available, ensuring exclusive marketing rights until patent expiration.
FAQs
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What is the primary use of the compounds described in U.S. Patent 8,168,793?
- The primary use is as COMT inhibitors in the treatment of Parkinson's disease.
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Who is the assignee of U.S. Patent 8,168,793?
- The assignee is BIAL-Portela & CA, S.A.
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When is the patent set to expire?
- The patent is set to expire on May 12, 2027.
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Is there a generic version of ONGENTYS available?
- No, there is currently no therapeutically equivalent generic version of ONGENTYS available in the United States.
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What is the significance of the patent term extension application for this patent?
- The patent term extension application was filed based on the FDA's approval of ONGENTYS, allowing for an extension of the patent term due to the regulatory review period.
Sources
- US8168793B2 - Nitrocatechol derivatives as COMT inhibitors - Google Patents
- United States Patent and Trademark Office - Regulations.gov
- Patent Claims and Patent Scope - SSRN
- Opicaphone and its intermediate manufacturing method - Google Patents
- Generic Ongentys Availability - Drugs.com
