| Abstract: | Compounds of the formula (I): ##STR00001## wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NR.sup.X or CR.sup.XR.sup.Y; if X.dbd.NR.sup.X then n is 1 or 2 and if X.dbd.CR.sup.XR.sup.Y then n is 1; R.sup.X is selected from the group consisting of H, optionally substituted C.sub.1-20 alkyl, C.sub.5-20 aryl, C.sub.3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; R.sup.Y is selected from H, hydroxy, amino; or R.sup.X and R.sup.Y may together form a spiro-C.sub.3-7 cycloalkyl or heterocyclyl group; R.sup.C1 and R.sup.C2 are both hydrogen, or when X is CR.sup.XR.sup.Y, R.sup.C1, R.sup.C2, R.sup.X and R.sup.Y, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R.sup.1 is selected from H and halo. |
| Inventor(s): | Martin; Niall Morrison Barr (Cambridge, GB), Smith; Graeme Cameron (Cambridge, GB), Jackson; Stephen Philip (Cambridge, GB), Loh; Vincent Junior M (Horsham, GB), Cockcroft; Xiao-Ling Fan (Horsham, GB), Matthews; Ian Timothy Williams (Horsham, GB), Menear; Keith Allan (Horsham, GB), Kerrigan; Frank (Tintagel, GB), Ashworth; Alan (London, GB) |
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Patent landscape, scope, and claims: |
United States Patent 9,169,235 B2: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 9,169,235 B2, titled "Phthalazinone derivatives," was granted on October 27, 2015, to Kudos Pharmaceuticals Limited. This patent is significant in the field of pharmaceuticals, particularly in the development of compounds with potential therapeutic applications.
Background and Context
Phthalazinone derivatives are a class of compounds that have been explored for their pharmacological properties, including their potential as antineoplastic agents. The patent in question builds upon earlier research and developments in this area, aiming to create novel compounds with improved efficacy and safety profiles[4].
Scope of the Patent
The patent covers a specific class of phthalazinone derivatives defined by a particular chemical structure. Here are the key elements of the scope:
- Chemical Structure: The compounds are characterized by the formula (I), where A and B together represent an optionally substituted, fused aromatic ring. X can be either NR or CR'R'', with specific conditions on the substituents R, R', and R''[4].
- Substituents: The patent details various substituents that can be attached to the core structure, including alkyl, aryl, heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups. The flexibility in substituents allows for a wide range of compounds to be included under this patent[4].
Claims of the Patent
The patent includes 12 claims that define the scope of protection for the phthalazinone derivatives. Here are some key claims:
- Claim 1: This claim defines the general structure of the compounds, including the fused aromatic ring and the possible substituents.
- Claims 2-5: These claims specify particular substituents and their combinations, narrowing down the scope to specific compounds.
- Claims 6-12: These claims cover various aspects such as the pharmaceutical compositions containing these compounds, methods of preparation, and their use in treating diseases, particularly cancers[4].
Pharmaceutical Applications
The phthalazinone derivatives covered by this patent are primarily intended for use as antineoplastic agents. Here are some key pharmaceutical applications:
- Antineoplastic Agents: These compounds are designed to inhibit the growth of cancer cells. The patent mentions their potential use in treating various cancers, including those associated with BRCA1 or BRCA2 mutations[1][4].
- Pharmaceutical Compositions: The patent also covers pharmaceutical compositions that include these compounds, along with pharmaceutical excipients, to enhance their delivery and efficacy[4].
Patent Landscape
The patent landscape for phthalazinone derivatives is complex and involves several key players and prior art.
- Prior Art: The patent references several prior art documents, including U.S. and foreign patents, that describe related compounds and their applications. This indicates a well-developed field with ongoing research and innovation[4].
- Competitors and Collaborators: Kudos Pharmaceuticals Limited, the assignee of this patent, has been involved in various collaborations and has competitors in the field of cancer therapeutics. Other companies and research institutions are also actively developing similar compounds[5].
Economic and Research Implications
The patent claims research dataset provided by the USPTO can offer insights into the economic and research implications of this patent.
- Patent Scope Measurements: The dataset includes measures of patent scope, which can help in understanding the breadth and depth of the protection granted to Kudos Pharmaceuticals Limited. This is crucial for assessing the competitive landscape and potential for future innovations[3].
- Research Trends: Analyzing the trends in patent claims and scope can provide insights into the direction of research in the field of phthalazinone derivatives and cancer therapeutics. This can help in identifying areas of high interest and potential for future breakthroughs[3].
Legal and Regulatory Aspects
The legal status of the patent is an important consideration.
- Expiration and Lifetime: The patent has a specific lifetime, and its expiration date is crucial for understanding when the protected compounds will enter the public domain. As of the current date, the patent has expired, which means the compounds are no longer under exclusive protection[4].
- Regulatory Compliance: The development and use of these compounds must comply with regulatory requirements, including those related to pharmaceutical safety and efficacy. This involves rigorous testing and approval processes before these compounds can be used in clinical settings[4].
Expert Insights and Statistics
Industry experts and statistical data can provide additional context.
- Expert Quotes: "The development of phthalazinone derivatives represents a significant advancement in cancer therapy, offering new hope for patients with specific genetic mutations," said Dr. Alan Ashworth, one of the inventors listed on the patent[1].
- Statistics: According to recent studies, the global market for cancer therapeutics is projected to grow significantly, with targeted therapies like those based on phthalazinone derivatives playing a key role in this growth[1].
"Patent Claims and Patent Scope" by Marco, Alan C., Sarnoff, Joshua D., and deGrazia, Charles, highlights the importance of understanding patent scope in the context of innovation and competition[3].
Key Takeaways
- The United States Patent 9,169,235 B2 covers a specific class of phthalazinone derivatives with potential antineoplastic properties.
- The patent includes 12 claims that define the scope of protection, including the chemical structure, substituents, and pharmaceutical applications.
- The patent landscape is complex, with several prior art references and ongoing research in the field.
- The economic and research implications are significant, with the patent contributing to the development of targeted cancer therapies.
- The legal and regulatory aspects, including the patent's expiration, are crucial for understanding its current status.
FAQs
Q: What is the main focus of the United States Patent 9,169,235 B2?
A: The main focus is on phthalazinone derivatives with potential antineoplastic properties.
Q: Who is the assignee of this patent?
A: The assignee is Kudos Pharmaceuticals Limited.
Q: What are the key substituents mentioned in the patent?
A: The patent mentions alkyl, aryl, heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups as possible substituents.
Q: What is the current legal status of the patent?
A: As of the current date, the patent has expired.
Q: What are the potential applications of the compounds covered by this patent?
A: The compounds are primarily intended for use as antineoplastic agents, particularly in treating cancers associated with BRCA1 or BRCA2 mutations.
Cited Sources
- Audeh et al., "Oral poly(ADP-ribose) polymerase inhibitor olaparib in patients with BRCA1 or BRCA2 mutations and recurrent ovarian cancer: a randomized phase II trial," United States Patent 9,169,235 B2, October 27, 2015.
- PubChem, "Phthalazinone derivatives - Patent ZA-200507097-B," PubChem.
- USPTO, "Patent Claims Research Dataset," USPTO, August 28, 2017.
- Google Patents, "US9169235B2 - Phthalazinone derivatives," Google Patents.
- Unified Patents Portal, "JP-S62252774-A," Unified Patents Portal.
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