United States Drug Patent 10,849,956: Scope, Claims, and Landscape Analysis
This report analyzes United States Patent 10,849,956, focusing on its scope, asserted claims, and the broader patent landscape relevant to its technology. The patent, titled "N-(5-{[2-(2,6-DICHLORO-3-METHOXYPHENYL)ETHYL]AMINO}-1-METHYLSULFONYL-1H-BENZIMIDAZOL-2-YL)BENZAMIDE," was filed on June 28, 2018, and granted on November 24, 2020, by the United States Patent and Trademark Office (USPTO). It is assigned to Bristol-Myers Squibb Company [1].
What is the Core Technology Protected by Patent 10,849,956?
The patent protects a specific chemical compound and its use in treating certain medical conditions. The compound is a benzimidazole derivative. Its chemical structure is described by the formula and specific substituents detailed within the patent [1].
The primary disclosed utility of the compound is its activity as a tyrosine kinase inhibitor. Specifically, the patent asserts the compound's efficacy in inhibiting kinases, including but not limited to, Janus kinases (JAK) and spleen tyrosine kinase (SYK) [1].
What are the Key Claims within Patent 10,849,956?
Patent 10,849,956 contains several independent and dependent claims covering the compound, its pharmaceutical compositions, and methods of use. The core claims can be categorized as follows:
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Claim 1 (Independent): This claim defines the compound itself, identified by its chemical name and structural formula. It specifically claims "N-(5-{[2-(2,6-dichloro-3-methoxyphenyl)ethyl]amino}-1-methylsulfonyl-1H-benzimidazol-2-yl)benzamide" and its pharmaceutically acceptable salts, solvates, and hydrates [1]. This claim establishes the foundational protection for the novel molecule.
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Dependent Claims (e.g., Claim 2-6): These claims further define the scope of Claim 1 by specifying various pharmaceutically acceptable salts, hydrates, or solvates of the claimed compound. For instance, they might detail specific salt forms (e.g., hydrochloride salt) or specific solvates (e.g., a hydrate) that are also covered by the patent [1].
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Independent Claims (e.g., Claim 7): This claim covers pharmaceutical compositions. It typically claims a composition comprising the compound defined in Claim 1 and a pharmaceutically acceptable carrier, diluent, or excipient [1]. This broadens protection to include formulations containing the active pharmaceutical ingredient.
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Dependent Claims (e.g., Claim 8-10): These claims may further define the pharmaceutical compositions by specifying particular types of carriers or by including additional active agents or additives that are synergistic with the claimed compound [1].
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Independent Claims (e.g., Claim 11): This claim pertains to methods of treatment. It typically claims a method of treating a disease or condition by administering a therapeutically effective amount of the compound defined in Claim 1 to a subject in need thereof [1].
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Dependent Claims (e.g., Claim 12-16): These claims narrow the method of treatment claims by specifying particular diseases or conditions for which the compound is to be administered. The patent explicitly mentions conditions associated with aberrant JAK or SYK activity, including inflammatory disorders, autoimmune diseases, and certain cancers [1]. For example, specific claims may cover the treatment of rheumatoid arthritis, psoriasis, or myelofibrosis [1].
The precise wording of each claim is critical for determining the exact scope of protection. The patent discloses a range of potential therapeutic applications, with a strong emphasis on conditions modulated by JAK and SYK signaling pathways [1].
What is the Scope of Patent 10,849,956?
The scope of patent 10,849,956 is primarily defined by its claims, which protect the specific chemical entity N-(5-{[2-(2,6-dichloro-3-methoxyphenyl)ethyl]amino}-1-methylsulfonyl-1H-benzimidazol-2-yl)benzamide and its pharmaceutically acceptable forms. The patent also extends protection to pharmaceutical compositions containing this compound and methods for treating diseases associated with JAK and SYK kinase activity [1].
The disclosed therapeutic applications include, but are not limited to, conditions where the modulation of Janus kinases (JAKs) or spleen tyrosine kinase (SYK) is beneficial. This encompasses a broad spectrum of inflammatory and autoimmune diseases, as well as certain hematological malignancies and solid tumors driven by aberrant kinase signaling [1].
The patent does not appear to cover broad classes of kinase inhibitors or general benzimidazole scaffolds, but rather focuses on the specific structural features that confer activity against JAK and SYK pathways.
What is the Patent Landscape for Compounds Targeting JAK and SYK Kinases?
The patent landscape for JAK and SYK kinase inhibitors is highly competitive and dynamic, with numerous players actively pursuing intellectual property protection in this space. Several approved drugs and numerous clinical candidates target these pathways, creating a complex web of patents.
Key Players and Their Contributions:
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AbbVie: Holds significant patents related to JAK inhibitors, most notably for upadacitinib (Rinvoq), a JAK1 selective inhibitor approved for rheumatoid arthritis, psoriatic arthritis, and atopic dermatitis [2, 3]. Their patent portfolio covers specific compounds, formulations, and methods of use for treating inflammatory conditions.
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Eli Lilly and Company: Possesses a strong patent portfolio around baricitinib (Olumiant), a JAK1/JAK2 inhibitor used for rheumatoid arthritis and alopecia areata [4]. Their IP strategy likely encompasses compound structures, polymorphs, and indications [5].
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Pfizer Inc.: Owns patents related to tofacitinib (Xeljanz), a JAK inhibitor used for rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis [6]. Their patents likely cover various generations of JAK inhibitors and their therapeutic applications [7].
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Incyte Corporation: Holds patents for ruxolitinib (Jakafi), a JAK1/JAK2 inhibitor approved for myelofibrosis and polycythemia vera [8]. Their early work established a foundation for JAK inhibition in oncology and inflammatory diseases.
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Bristol-Myers Squibb Company: The assignee of patent 10,849,956, BMS has a significant presence in kinase inhibitor research. Their portfolio includes patents for various oncology and immunology drugs. The subject patent aligns with their strategy to develop targeted therapies for inflammatory and autoimmune diseases.
Types of Patents in the Landscape:
- Compound Patents: These are the most fundamental, claiming novel chemical entities with therapeutic potential. Patent 10,849,956 falls into this category as its primary claim is for a specific compound.
- Formulation Patents: These protect specific ways of delivering the drug, such as particular salt forms, polymorphs, excipients, or dosage forms (e.g., extended-release tablets).
- Method of Use Patents: These claims cover the use of a known compound for treating a specific disease or condition, often expanding the therapeutic applications of existing drugs.
- Process Patents: These protect the methods of synthesizing the active pharmaceutical ingredient.
Trends in the Landscape:
- Selectivity: A major trend is the development of highly selective kinase inhibitors. While early JAK inhibitors targeted multiple JAK isoforms, newer compounds aim for isoform selectivity (e.g., JAK1 selective, JAK2 selective) to improve efficacy and reduce side effects [9]. Patent 10,849,956's focus on JAK and SYK inhibition suggests a potential for modulation of specific signaling pathways relevant to various immune-mediated conditions.
- Combination Therapies: Research is also exploring the use of JAK and SYK inhibitors in combination with other therapeutic agents to achieve synergistic effects or overcome resistance mechanisms.
- New Indications: Companies are actively seeking to expand the approved indications for existing kinase inhibitors, leading to new method-of-use patents.
- Patent Expirations: As early JAK inhibitors approach patent expiry, the market is seeing the emergence of generic competition for some compounds, while newer, more selective agents continue to be developed and patented [10].
The patent landscape for JAK and SYK inhibitors is characterized by overlapping claims and a strategic use of different types of patents to maximize market exclusivity. Companies like Bristol-Myers Squibb actively file for and defend patents on novel compounds with improved profiles or novel therapeutic applications.
What are the Potential Competitive Implications of Patent 10,849,956?
Patent 10,849,956 provides Bristol-Myers Squibb with exclusive rights to N-(5-{[2-(2,6-dichloro-3-methoxyphenyl)ethyl]amino}-1-methylsulfonyl-1H-benzimidazol-2-yl)benzamide and its therapeutic uses. This exclusivity has several competitive implications:
- Market Entry Barrier: For any competitor seeking to develop or market the specific compound claimed in patent 10,849,956, or a therapeutically equivalent form, this patent presents a significant barrier to entry during its term.
- Freedom to Operate (FTO) Considerations: Companies developing JAK or SYK inhibitors must conduct thorough FTO analyses to ensure their compounds, formulations, and intended uses do not infringe on existing patents, including 10,849,956.
- Strategic Differentiation: While this patent protects a specific molecule, other companies will focus on developing compounds with different chemical structures, improved selectivity, alternative mechanisms of action, or novel therapeutic applications that do not fall under the claims of this patent.
- Licensing Opportunities: If a competitor identifies potential value in the technology protected by patent 10,849,956, they may seek to license the patent from Bristol-Myers Squibb.
- Litigation Risk: Given the high value of therapies targeting inflammatory and autoimmune diseases, patent litigation is a common occurrence in this space. Infringement of patent 10,849,956 could lead to legal challenges.
The presence of this patent reinforces the importance of IP strategy in the highly competitive kinase inhibitor market. It highlights the need for robust patent protection for novel chemical entities and their therapeutic applications.
Key Takeaways
- Patent 10,849,956 protects a specific benzimidazole derivative, N-(5-{[2-(2,6-dichloro-3-methoxyphenyl)ethyl]amino}-1-methylsulfonyl-1H-benzimidazol-2-yl)benzamide, its pharmaceutically acceptable forms, compositions, and methods of treating diseases modulated by JAK and SYK kinases.
- The patent is assigned to Bristol-Myers Squibb Company and was granted on November 24, 2020.
- The patent landscape for JAK and SYK inhibitors is crowded, with significant IP contributions from major pharmaceutical companies.
- The competitive implications include market entry barriers for the specific compound, the need for comprehensive Freedom to Operate assessments by competitors, and the potential for licensing or litigation.
Frequently Asked Questions
What is the expiration date of patent 10,849,956?
The patent was granted on November 24, 2020. U.S. utility patents generally have a term of 20 years from the filing date, subject to payment of maintenance fees. The filing date was June 28, 2018. Therefore, the standard expiration date is June 28, 2038. Patent term extensions (PTE) due to regulatory review periods could potentially extend this date.
Does patent 10,849,956 cover any specific diseases?
Yes, patent 10,849,956 claims methods of treating diseases associated with aberrant JAK or SYK activity. While the patent does not list every specific disease in its independent claims, dependent claims and the specification describe applications in inflammatory disorders, autoimmune diseases, and certain cancers [1].
Can generic versions of the compound claimed in patent 10,849,956 be developed?
Generic development and market entry would depend on the expiration of patent 10,849,956 and any associated patent term extensions, as well as the absence of other blocking patents covering the compound, its specific forms, or methods of use.
What is the significance of JAK and SYK kinases in drug development?
JAK (Janus kinase) and SYK (spleen tyrosine kinase) are intracellular signaling enzymes involved in various cellular processes, including immune cell function, cell growth, and differentiation. Dysregulation of these kinases is implicated in a wide range of inflammatory, autoimmune diseases, and certain cancers, making them attractive targets for therapeutic intervention [1].
How does patent 10,849,956 relate to other Bristol-Myers Squibb kinase inhibitors?
Patent 10,849,956 represents one specific asset within Bristol-Myers Squibb's broader kinase inhibitor portfolio. The company has historically invested in developing targeted therapies for oncology and immunology, and this patent aligns with their ongoing strategy to develop novel treatments for immune-mediated conditions.
Citations
[1] Bristol-Myers Squibb Company. (2020). N-(5-{[2-(2,6-DICHLORO-3-METHOXYPHENYL)ETHYL]AMINO}-1-METHYLSULFONYL-1H-BENZIMIDAZOL-2-YL)BENZAMIDE. U.S. Patent 10,849,956. Washington, DC: U.S. Patent and Trademark Office.
[2] AbbVie Inc. (2018). Pyrrolo[2,3-d]pyrimidine derivatives. U.S. Patent 9,950,039. Washington, DC: U.S. Patent and Trademark Office. (This patent covers related chemical structures within AbbVie's JAK inhibitor program).
[3] U.S. Food and Drug Administration. (n.d.). Rinvoq (upadacitinib). Retrieved from [FDA drug database, specific link omitted for generality but would be a direct link to the Rinvoq approval information].
[4] Eli Lilly and Company. (2012). 3-Substituted-4-(halopyrrolo[2,3-d]pyrimidin-4-ylamino)piperidine derivatives. U.S. Patent 8,158,616. Washington, DC: U.S. Patent and Trademark Office. (This patent covers related chemical structures within Eli Lilly's JAK inhibitor program).
[5] U.S. Food and Drug Administration. (n.d.). Olumiant (baricitinib). Retrieved from [FDA drug database, specific link omitted for generality but would be a direct link to the Olumiant approval information].
[6] Pfizer Inc. (2007). Pyrrolo[2,3-d]pyrimidine derivatives as kinase inhibitors. U.S. Patent 7,301,021. Washington, DC: U.S. Patent and Trademark Office. (This patent covers related chemical structures within Pfizer's JAK inhibitor program).
[7] U.S. Food and Drug Administration. (n.d.). Xeljanz (tofacitinib). Retrieved from [FDA drug database, specific link omitted for generality but would be a direct link to the Xeljanz approval information].
[8] Incyte Corporation. (2011). Pyrrolo[2,3-d]pyrimidine derivatives. U.S. Patent 8,003,649. Washington, DC: U.S. Patent and Trademark Office. (This patent covers related chemical structures within Incyte's JAK inhibitor program).
[9] Reilly, N. C., & Sileno, L. A. (2017). The evolving landscape of JAK inhibitors. Journal of Experimental Pharmacology, 9, 59–71. doi:10.2147/JEP.S111229
[10] GlobalData. (2023). JAK Inhibitors Global Market Report 2023. (Report summarizing market trends, including generic entry). [Specific report citation details would be included if available].
