Boron-Containing Small Molecules as Anti-Inflammatory Agents: A Detailed Analysis of US Patent 8,168,614
Introduction
The use of boron-containing small molecules as anti-inflammatory agents has been a significant area of research and development, particularly highlighted in United States Patent 8,168,614. This patent, issued to Anacor Pharmaceuticals, Inc., discloses methods for treating various anti-inflammatory conditions using these unique molecules.
Patent Overview
Issuance and Expiration
US Patent 8,168,614 was issued on May 1, 2012, and is set to expire on January 20, 2030[2].
Inventors and Assignees
The patent was invented by a team of researchers including Stephen J. Baker, Virginia Sanders, Tsutomu Akama, Carolyn Bellinger-Kawahara, Yvonne Freund, Kirk R. Maples, Jacob J. Plattner, Yong-Kang Zhang, Huchen Zhou, and Vincent S. Hernandez. The assignee is Anacor Pharmaceuticals, Inc.[2].
Claims and Scope
Anti-Inflammatory Conditions
The patent covers the use of boron-containing small molecules for treating a wide range of anti-inflammatory conditions. These include rheumatoid arthritis, inflammatory bowel disease (such as Crohn's disease and ulcerative colitis), psoriasis, Alzheimer's disease, Parkinson's disease, and other neurodegenerative diseases[1].
Mechanism of Action
The boron-containing small molecules act by inhibiting proinflammatory pathways, particularly those involving interleukin-6 (IL-6) and interleukin-10 (IL-10). This inhibition helps in reducing the severity of inflammatory responses in various diseases[1].
Pharmaceutical Compositions
The patent describes various pharmaceutical compositions that include these boron-containing small molecules. These compositions can be formulated for different routes of administration, including topical, oral, and parenteral routes. The patent also details the use of pharmaceutical excipients and vehicles to enhance the stability and efficacy of these compositions[1].
Diseases Treated
Rheumatoid Arthritis
The patent highlights the potential of boron-containing small molecules in treating rheumatoid arthritis, a chronic autoimmune disorder that causes inflammation in the joints[1].
Inflammatory Bowel Disease
Conditions such as Crohn's disease and ulcerative colitis are also targeted, as these molecules can reduce inflammation in the gastrointestinal tract[1].
Psoriasis
Psoriasis, a skin condition characterized by excessive skin cell growth and inflammation, is another area where these molecules show promise[1].
Neurodegenerative Diseases
The patent includes methods for treating neurodegenerative diseases like Alzheimer's and Parkinson's, suggesting a broader therapeutic potential beyond traditional inflammatory conditions[1].
Manufacturing Process
The patent details the manufacturing process for these boron-containing small molecules, including the synthesis of the compounds and their intermediates. This process is crucial for ensuring the quality and consistency of the final product[1].
Patent Landscape
Related Patents
Anacor Pharmaceuticals, Inc. has been granted several related patents, including US Patent 8,039,451, US Patent 8,501,712, and US Patent 9,682,092, all of which pertain to the use of boron-containing small molecules as anti-inflammatory agents. These patents have varying expiration dates, with some expiring as early as 2027 and others in 2030[2].
Exclusivity and Generic Availability
Currently, there are no therapeutically equivalent generic versions of the drugs covered by these patents available in the United States. This exclusivity period, combined with the patent protection, ensures that Anacor Pharmaceuticals, Inc. maintains a monopoly on these treatments until the patents expire[2].
Metrics for Patent Scope
Independent Claim Length and Count
The scope of the patent can be analyzed using metrics such as independent claim length and independent claim count. These metrics help in understanding the breadth and clarity of the patent claims. Narrower claims with fewer words and fewer independent claims generally indicate a more focused and clearer patent scope, which can be associated with a higher probability of grant and a shorter examination process[3].
Impact on Innovation
Patent Quality and Litigation
The quality of patent claims, including their breadth and clarity, can significantly impact innovation. Broad and unclear claims can lead to increased litigation costs and may impede innovation by creating uncertainty and barriers to entry for other researchers and companies[3].
Key Takeaways
- Boron-containing small molecules are effective in treating various anti-inflammatory conditions.
- Patent coverage includes a wide range of diseases such as rheumatoid arthritis, inflammatory bowel disease, psoriasis, and neurodegenerative diseases.
- Manufacturing process is detailed to ensure quality and consistency.
- Related patents provide a comprehensive landscape of Anacor Pharmaceuticals, Inc.'s intellectual property in this area.
- Exclusivity and generic availability ensure that the company maintains a monopoly until the patents expire.
FAQs
What is the primary focus of US Patent 8,168,614?
The primary focus of US Patent 8,168,614 is the use of boron-containing small molecules as anti-inflammatory agents.
Which diseases are targeted by the boron-containing small molecules?
The patent covers treatments for rheumatoid arthritis, inflammatory bowel disease, psoriasis, Alzheimer's disease, Parkinson's disease, and other neurodegenerative diseases.
Who are the inventors and assignees of the patent?
The inventors include Stephen J. Baker, Virginia Sanders, Tsutomu Akama, and others, with Anacor Pharmaceuticals, Inc. as the assignee.
When does the patent expire?
The patent is set to expire on January 20, 2030.
Are there any generic versions of the drugs covered by this patent available?
Currently, there are no therapeutically equivalent generic versions available in the United States.
How does the patent scope impact innovation?
The clarity and breadth of the patent claims can affect innovation by influencing litigation costs and the ease of entry for other researchers and companies.
Sources
- US8168614B2 - Boron-containing small molecules as anti-inflammatory agents - Google Patents
- Generic Eucrisa Availability - Drugs.com
- Patent Claims and Patent Scope - Hoover Institution
