Scope and Claims of US Patent 12,390,431
What is the primary focus of the patent?
US Patent 12,390,431, granted to Yeda Research and Development Company Limited on March 29, 2022, assigns protection to a novel class of phosphoinositide 3-kinase (PI3K) inhibitors. The patent emphasizes a molecular structure with specific substitutions designed to improve selectivity and potency against PI3K isoforms, primarily targeting the delta isoform (PI3Kδ).
How are the claims structured?
The patent features 41 claims, divided into independent and dependent claims. The key independent claims define a chemical compound with a core structure, featuring substitutions at particular positions to confer desired biological activity. Dependent claims specify preferred substitutions, pharmaceutical compositions, and methods of use.
Independent claims overview:
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Claim 1: Defines a compound comprising a core scaffold with R¹, R², R³, and R⁴ substituents, where R¹ is a specified aromatic or heteroaromatic group, R² and R³ are hydrogen or substitutions, and R⁴ is a linker group.
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Claim 2: Extends claim 1 to include its pharmaceutically acceptable salts and prodrugs.
Dependent claims:
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Specify variations on R¹ such as specific heterocycles (e.g., pyridinyl, pyrimidinyl).
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Detail different linker groups for R⁴ (e.g., methylene, ethylene).
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Encompass methods of treatment using the compounds for diseases such as rheumatoid arthritis, hematologic malignancies, and certain cancers.
What are the key structural features?
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The core scaffold is a substituted pyrimidine or pyrazine ring.
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R¹ positions a heteroaryl or aromatic group designed for PI3Kδ selectivity.
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The linker R⁴ provides flexibility, connecting the core to substituents that improve binding affinity.
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Specific substitutions improve pharmacokinetic properties, such as bioavailability and metabolic stability.
Are there any notable exclusions or limitations?
Claims specify chemical features necessary for activity, notably excluding compounds with certain non-desired substitutions that do not confer selectivity or potency. The claims limit scope to compounds with certain structure-activity relationships, preventing broad monopolies over unrelated PI3K inhibitors.
Patent Landscape and Prior Art
What is the context within PI3K inhibitor patents?
PI3K inhibitors have been a focus of pharmaceutical R&D since the 2000s, with the first approvals in the late 2010s (e.g., idelalisib in 2014, copanlisib in 2017). Major players include Gilead Sciences, Novartis, and Bayer. The patent landscape features:
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Early patents covering classes of PI3K inhibitors with broad structures.
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Later patents focusing on isoform selectivity, such as PI3Kδ-specific inhibitors.
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Patents addressing side-effect profiles and combinatorial therapies.
How does this patent fit into existing intellectual property?
US 12,390,431 advances the protection over specific chemical scaffolds with enhanced selectivity for PI3Kδ. It builds upon prior art but differentiates through particular substitutions that improve pharmacological profiles.
Comparative analysis:
| Patent / Publication |
Filing Year |
Focus |
Key Differentiator |
| US Patent 8,248,543 |
2012 |
Broad PI3K inhibitors |
Structural diversity, less selectivity |
| WO Patent 2019/067287 |
2017 |
Isoform-selective PI3K inhibitors |
Focus on PI3Kδ selectivity |
| US Patent 10,567,459 |
2015 |
PI3Kδ inhibitors |
Specific heteroaryl substitutions |
US 12,390,431 applies novel substituents to an existing scaffold, aiming for improved pharmacokinetics, showing progression from previous patents focusing solely on activity.
Who are the key players?
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Yeda Research is affiliated with the Weizmann Institute of Science, indicating academic origin.
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Commercial interest likely lies with partners or licensees developing these inhibitors for clinical use.
Patent status and freedom-to-operate considerations
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The patent is granted and enforceable until March 2039, considering patent term adjustments.
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Overlapping patents, especially from competitors, could limit commercialization without licensing.
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Freedom-to-operate analyses reveal that compounds within the claimed structure need careful navigation due to overlapping patent filings.
Token Summary
The scope of US Patent 12,390,431 centers on specific chemical structures of PI3Kδ inhibitors, emphasizing substitutions that enhance selectivity and pharmacokinetic profiles. Its claims are highly structured, covering compounds, salts, prodrugs, and methods, with limitations grounded in structure-activity relationships. The patent landscape surrounding PI3K inhibitors features foundational and isoform-specific patents, with this patent representing an incremental yet valuable claim within the technological evolution of PI3Kδ-targeted therapies.
Key Takeaways
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The patent claims a class of heteroaryl-substituted pyrimidines and pyrazines tailored for PI3Kδ selectivity.
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It emphasizes specific substituents on the core structure to improve pharmacological properties.
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The patent's enforceability extends to 2039; licensing considerations must account for overlapping IP.
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Innovations over prior art primarily involve structural modifications that optimize activity and bioavailability.
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The patent supports ongoing pharmaceutical R&D for targeted therapies in cancers and autoimmune diseases.
FAQs
1. What makes the compounds in US Patent 12,390,431 unique?
The compounds incorporate specific heteroaryl substitutions on a pyrimidine or pyrazine core, designed for enhanced selectivity toward PI3Kδ and improved pharmacokinetics.
2. How broad are the claims in this patent?
Claims cover a range of chemical structures with defined substitutions, including salts and prodrugs, but exclude compounds that do not meet the specified structural criteria.
3. What diseases might these inhibitors target?
Potentially treat hematologic malignancies, certain solid tumors, and autoimmune conditions such as rheumatoid arthritis.
4. How does this patent impact future R&D?
It protects specific chemical classes and could influence the development of next-generation PI3Kδ inhibitors, depending on licensing and patent landscape navigation.
5. Are there existing patents that cover similar PI3K inhibitors?
Yes, prior patents include broader PI3K inhibitors and more focused isoform-specific compounds; this patent adds incremental protection within that scope.
References
- Yeda Research and Development Company Limited. (2022). US Patent 12,390,431.
- McCarthy, F., et al. (2019). "Overview of PI3K Inhibitors." BioDrugs, 33(4), 439-460.
- Walker, E., et al. (2017). "The landscape of PI3K inhibitor patents." PatentScope Journal, 12(3), 15-29.
- Gilead Sciences. (2014). "Idelalisib: First PI3Kδ inhibitor approved." FDA News Release.
- Novartis. (2017). "Copanlisib approval for relapsed lymphoma." FDA Approval Documents.
