United States Patent 8,420,629: A Detailed Analysis
Introduction
The United States Patent 8,420,629, titled "Azetidinone and Cyclobutane Derivatives as JAK Inhibitors," was granted to Incyte Corporation on April 16, 2013. This patent is significant in the pharmaceutical industry, particularly in the development of Janus kinase (JAK) inhibitors, which are crucial for treating various autoimmune and inflammatory diseases.
Inventors and Assignee
The patent was invented by James D. Rodgers and Stacey Shepard, with the assignee being Incyte Corporation, based in Wilmington, Delaware[4].
Background and Context
JAK inhibitors are a class of drugs that target the Janus kinase family of enzymes, which play a key role in the signaling pathways of cytokines and growth factors. These inhibitors have been developed to treat conditions such as rheumatoid arthritis, psoriasis, and certain types of cancer. The development of these inhibitors is a complex process involving extensive research and clinical trials.
Claims and Description
The patent describes and claims azetidinone and cyclobutane derivatives that act as JAK inhibitors. Here are the key aspects:
Chemical Compounds
The patent details the synthesis and structure of specific azetidinone and cyclobutane derivatives. These compounds are designed to inhibit the activity of JAK enzymes, which are involved in the signaling pathways of various cytokines and growth factors[4].
Synthesis Method
The patent includes a detailed description of the synthesis process for these compounds. This involves several steps, including the treatment of reaction mixtures with aqueous sodium hydroxide solutions and other chemical processes to achieve the desired derivatives[4].
Pharmacological Activity
The compounds claimed in the patent are shown to have potent inhibitory activity against JAK enzymes. This pharmacological activity is crucial for their therapeutic use in treating autoimmune and inflammatory diseases.
Patent Scope and Claims
The patent includes multiple claims that define the scope of the invention:
Independent Claims
The patent has several independent claims that describe the chemical structure of the azetidinone and cyclobutane derivatives. These claims specify the molecular formula, the presence of specific functional groups, and the stereochemistry of the compounds[4].
Dependent Claims
Dependent claims further narrow down the scope by specifying additional features or limitations of the compounds. These claims may include specific substituents, stereochemical configurations, or other structural details[4].
Patent Landscape
The patent landscape surrounding US 8,420,629 is complex and involves several other patents and legal considerations:
Related Patents
The patent is part of a larger family of patents related to JAK inhibitors. For example, the application for this patent was a division of a previous application (No. 12/401,348), which was granted as Patent No. 8,158,616. This indicates a continuous development and refinement of JAK inhibitors by Incyte Corporation[4].
Litigation and Settlements
Patents related to pharmaceuticals, including JAK inhibitors, are often involved in litigation and settlement agreements. For instance, other patents related to similar compounds have been the subject of ANDA (Abbreviated New Drug Application) litigation, where generic manufacturers challenge the validity or enforceability of the patents[5].
Expiry and Extensions
The term of the patent is subject to the provisions of 35 U.S.C. ยง 154(b), which allows for adjustments or extensions under certain conditions. However, according to the patent document, there were no extensions or adjustments made to the term of this patent[4].
Impact on Pharmaceutical Industry
The development and patenting of JAK inhibitors like those described in US 8,420,629 have a significant impact on the pharmaceutical industry:
Therapeutic Applications
These compounds have been approved for various therapeutic uses, including the treatment of rheumatoid arthritis, psoriatic arthritis, and other autoimmune diseases. The patent protects the intellectual property of Incyte Corporation, allowing them to market these drugs exclusively for a period of time.
Research and Development
The patent landscape in this area encourages continuous research and development. Companies like Incyte Corporation invest heavily in discovering new compounds and improving existing ones, driven by the potential for exclusive market rights granted by patents.
Key Takeaways
- Chemical Structure: The patent describes specific azetidinone and cyclobutane derivatives as JAK inhibitors.
- Synthesis Method: Detailed synthesis processes are outlined in the patent.
- Pharmacological Activity: The compounds have potent inhibitory activity against JAK enzymes.
- Patent Scope: The patent includes independent and dependent claims defining the scope of the invention.
- Patent Landscape: The patent is part of a larger family of patents related to JAK inhibitors and is subject to litigation and settlement agreements.
- Impact: The patent has significant implications for the therapeutic use of JAK inhibitors and drives research and development in the pharmaceutical industry.
FAQs
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What is the main subject of United States Patent 8,420,629?
- The main subject is azetidinone and cyclobutane derivatives that act as JAK inhibitors.
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Who are the inventors of this patent?
- The inventors are James D. Rodgers and Stacey Shepard.
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What is the assignee of this patent?
- The assignee is Incyte Corporation.
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What is the significance of JAK inhibitors in the pharmaceutical industry?
- JAK inhibitors are crucial for treating autoimmune and inflammatory diseases such as rheumatoid arthritis and psoriasis.
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How does this patent fit into the broader patent landscape of JAK inhibitors?
- It is part of a larger family of patents related to JAK inhibitors and is subject to ongoing research, development, and legal considerations.
Cited Sources
- United States Patent and Trademark Office. US 8,420,629 B2: Azetidinone and Cyclobutane Derivatives as JAK Inhibitors. April 16, 2013.
- U.S. Food & Drug Administration. ANDA 217542 ANDA APPROVAL Aurobindo Pharma USA, Inc. December 15, 2023.
- National Bureau of Economic Research. The Feasibility of Using Bayh-Dole March-In Rights to Lower Drug Prices. Working Paper No. 32217.
