United States Patent 8,357,697: A Detailed Analysis of Scope and Claims
Introduction
The United States Patent 8,357,697, titled "Substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-A]isoquinolin-2-ol compounds and methods relating thereto," is a significant patent in the pharmaceutical industry. This patent, issued to Neurocrine Biosciences, Inc., covers a class of compounds and their methods of use, particularly in the treatment of various neurological and psychiatric disorders.
Patent Overview
Publication and Authority
The patent was published under the publication number US8357697B2 and is governed by the United States Patent and Trademark Office (USPTO)[1][4].
Prior Art and Chemical Compounds
The patent involves substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-A]isoquinolin-2-ol compounds. These compounds are part of a broader class of chemical entities that include isobutyl, dimethoxy, and isoquinolin moieties[1][4].
Scope of Claims
Chemical Structure and Synthesis
The patent claims cover a specific class of compounds with a detailed chemical structure. These compounds are synthesized through various methods described in the patent, including the use of specific precursors and reaction conditions[1][4].
Pharmaceutical Compositions
The patent includes claims for pharmaceutical compositions that contain these compounds, often in the form of salts, solvates, or drug carriers. These compositions are designed for the treatment of various diseases[1][4].
Methods of Use
The methods of use claimed in the patent are extensive and include the treatment of several neurological and psychiatric disorders. Key among these are:
- Huntington's Disease: The patent claims methods for treating Huntington's chorea, a symptom of Huntington's disease[2][4].
- Tardive Dyskinesia: The compounds are also claimed for the treatment of tardive dyskinesia, a side effect of long-term use of antipsychotic drugs[1][4].
- Tourette Syndrome: Additionally, the patent covers the use of these compounds in treating Tourette Syndrome[1][4].
- Attention Deficit-Hyperactivity Disorder (ADHD): The patent includes claims for treating ADHD, particularly the inattentive type[1][4].
Patent Landscape and Litigation
Patent Expiration and Litigation
The patent is part of a complex patent landscape with multiple related patents. The expiration dates for these patents vary, with some expiring as late as 2037[2].
Litigation related to this patent has been significant. For example, Neurocrine Biosciences, Inc. initiated litigation against Lupin Limited for infringement of several patents, including the '697 patent. However, the case was eventually dismissed[2].
Paragraph IV Certifications
Lupin Limited's ANDA (Abbreviated New Drug Application) included paragraph IV certifications stating that the patents, including the '697 patent, were invalid, unenforceable, or would not be infringed by their manufacture, use, or sale of Valbenazine Capsules[2].
Challenges in Patent Scope
Genus Claims and Enablement
The patent landscape for pharmaceuticals and biologics is challenging due to the strict application of patent disclosure laws, particularly Section 112(a) of the U.S. patent code. Genus claims, which aim to capture a broad class of compounds, are often scrutinized for their written description and enablement requirements. This can make it difficult for innovators to claim the full scope of their invention without violating these requirements[3].
Impact on Pharmaceutical and Biotechnology Industries
The rigid application of these laws has significantly impacted the pharmaceutical and biotechnology industries. Innovators face the dilemma of either claiming too broadly and risking invalidation or claiming too narrowly and allowing competitors to design around their patents. This has led to a situation where many existing patents in these industries are at risk of being invalidated[3].
Key Diseases and Treatments
Huntington's Disease
The patent includes methods for treating Huntington's chorea, a severe motor symptom of Huntington's disease. This is a significant advancement, as current treatments for Huntington's disease are limited and often focus on managing symptoms rather than addressing the underlying cause[1][4].
Tardive Dyskinesia
Tardive dyskinesia, a condition characterized by involuntary movements, is another key area covered by the patent. The compounds claimed in the patent offer a potential treatment for this condition, which is often a side effect of long-term antipsychotic medication[1][4].
Tourette Syndrome
The patent also covers the treatment of Tourette Syndrome, a neurodevelopmental disorder characterized by repetitive movements and vocalizations. The compounds described in the patent provide a new avenue for treating this condition[1][4].
Pharmaceutical Compositions and Formulations
Salts, Solvates, and Drug Carriers
The patent includes claims for various pharmaceutical compositions, including salts, solvates, and drug carriers. These formulations are designed to enhance the bioavailability and stability of the active compounds[1][4].
Diluting Agents
The patent also mentions the use of diluting agents in the pharmaceutical compositions. These agents help in achieving the desired concentration and form of the final product[1][4].
Conclusion
The United States Patent 8,357,697 is a critical patent in the pharmaceutical industry, covering a range of compounds and methods for treating various neurological and psychiatric disorders. The patent's scope and claims are detailed, but they operate within a complex and challenging patent landscape. Understanding the nuances of this patent and its implications is essential for innovators and companies in the pharmaceutical and biotechnology sectors.
Key Takeaways
- The patent covers substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-A]isoquinolin-2-ol compounds.
- It includes methods for treating Huntington's disease, tardive dyskinesia, Tourette Syndrome, and ADHD.
- The patent is part of a complex litigation landscape involving multiple related patents.
- The strict application of Section 112(a) of the U.S. patent code poses challenges for genus claims in pharmaceutical and biotechnology patents.
- The patent covers various pharmaceutical compositions, including salts, solvates, and drug carriers.
FAQs
What is the main compound covered by the United States Patent 8,357,697?
The main compound covered is a substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-A]isoquinolin-2-ol.
What diseases are treated by the methods claimed in the patent?
The patent claims methods for treating Huntington's disease, tardive dyskinesia, Tourette Syndrome, and attention deficit-hyperactivity disorder (ADHD).
What is the significance of genus claims in pharmaceutical patents?
Genus claims are critical in pharmaceutical patents as they aim to capture a broad class of compounds. However, they are often scrutinized for their written description and enablement requirements, making it challenging to obtain robust patent protection.
Why is the patent landscape for this patent complex?
The patent landscape is complex due to multiple related patents and ongoing litigation, including paragraph IV certifications and disputes over patent validity and infringement.
What are the implications of the strict application of Section 112(a) of the U.S. patent code?
The strict application of Section 112(a) makes it difficult for innovators to claim the full scope of their invention without violating the written description and enablement requirements, which can lead to the invalidation of many existing patents in the pharmaceutical and biotechnology industries.
Sources
- US8357697B2 - Substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-A]isoquinolin-2-ol compounds and methods relating thereto - Google Patents.
- ANDA 216064 - accessdata.fda.gov - U.S. Food & Drug Administration.
- Eviscerating Patent Scope - DigitalCommons@NYLS.
- US8357697B2 - Substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-A]isoquinolin-2-ol compounds and methods relating thereto - Google Patents.