Last updated: August 13, 2025
Overview of JP2016135253
Japan Patent Application JP2016135253, filed on March 24, 2016, and published on September 22, 2016, by Nippon Kayaku Co., Ltd., focuses on pharmaceutical compositions involving specific pyrimidine derivatives. These derivatives demonstrate potential as kinase inhibitors with applications in treating cancer and other proliferative disorders. The patent claims encompass novel chemical entities, their methods of synthesis, and therapeutic uses, positioning JP2016135253 within a strategic space targeting kinase modulation for disease management.
Scope of the Patent:
The patent's scope centers on chemical compounds characterized by a pyrimidine core with particular substitutions designed to optimize kinase inhibitory activity. It broadly covers:
- Chemical Entities: Structural variants of pyrimidine derivatives with specific substitutions at defined positions, notably on the heterocyclic ring and associated side chains.
- Pharmacological Use: Methods of treating diseases involving kinase dysregulation, such as various cancers, using the claimed compounds.
- Synthesis Methods: Procedures for preparing these derivatives, emphasizing scalable, reproducible processes.
Scope Significance:
By defining both the chemical scope and therapeutic applications, JP2016135253 aims to secure exclusivity over a class of kinase inhibitors with potential broad-spectrum anti-cancer activity, including non-small cell lung cancer (NSCLC), colorectal cancer, and other solid tumors.
Claims Analysis
The patent includes a series of claims categorized as independent and dependent. These claims determine the breadth of legal protection and serve as the basis for potential infringement actions.
Independent Claims
The primary independent claims (typically Claims 1 and 2) define the core chemical structure and its variants:
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Claim 1:
Defines a compound comprising a pyrimidine ring with substitutions at specific positions (e.g., R₁, R₂, R₃) with conditions on these substituents to ensure kinase inhibitory activity.
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Claim 2:
Focuses on a chemical process for synthesizing these derivatives, targeting intermediates and reaction conditions.
Dependent Claims
Dependent claims specify particular embodiments, including:
- Variations in side chain substituents (alkyl, aryl, heteroaryl groups).
- Specific substitution patterns that enhance selectivity or potency.
- Pharmacological formulations (e.g., oral tablets, injections).
- Therapeutic claims specifying the treatment of particular cancers or proliferation disorders.
Key Structural Features Covered
- Pyrimidine Core: The fundamental scaffold offering bioactivity.
- Substituents at Position 2 and 4: Variants that modulate kinase selectivity.
- Side Chains: Including amino, cycloalkyl, and aromatic groups to influence pharmacokinetics and binding affinity.
- Heteroatoms and Functional Groups: N, O, S groups enhancing solubility and bioavailability.
Through these claims, the patent aims to cover not only specific compounds but also a broad class within the defined chemical space, providing substantial freedom-to-operate considerations for competitors.
Patent Landscape and Strategic Positioning
Related Patents and Applications
JP2016135253 exists within a landscape saturated with kinase inhibitor patents. Notable related patents include:
- US Patents: Multiple filings covering pyrimidine-based kinase inhibitors, notably from companies like AbbVie, Novartis, and Takeda.
- International Patents: PCT applications focusing on similar chemical scaffolds with claims extending across numerous jurisdictions.
The patent appears to carve out a unique subset by focusing on particular substitutions and specific kinase targets, likely linked to proprietary compound libraries developed internally.
Competitive Position
Nippon Kayaku’s strategy reflects incremental innovation: optimizing known kinase inhibitory cores to produce compounds with improved selectivity, reduced toxicity, or enhanced pharmacokinetics. This approach provides a competitive edge by:
- Extending patent life through detailed structural claims.
- Blocking competitors from utilizing similar chemical modifications.
- Facilitating licensing opportunities within Japan and potentially worldwide.
Legal and Commercial Implications
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Patent Strengths:
The claims’ breadth, combined with detailed synthesis methods, strengthen the patent’s enforceability.
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Weaknesses and Challenges:
As kinase inhibitor patents are highly crowded, patent validity may hinge on demonstrating novelty and inventive step, especially if structurally similar compounds exist.
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Potential for Infringement:
Competitors designing derivatives with minor structural changes might circumvent claims unless patent scope is carefully monitored.
Conclusion
JP2016135253 establishes a comprehensive coverage of pyrimidine derivatives designed for kinase inhibition, with significant implications for cancer therapy. Its claims encompass diverse chemical variants and uses, making it a strategically valuable patent within the competitive landscape of kinase inhibitors. Its strength lies in its detailed structural envelope and therapeutic scope, although ongoing patent clearance and non-infringement assessments are essential given the crowded patent space.
Key Takeaways
- The patent claims a broad class of pyrimidine derivatives with potential as kinase inhibitors, targeting large therapeutic markets such as oncology.
- Structural scope covers substitution patterns that modulate kinase selectivity and pharmacokinetics.
- The patent complements Japan's strategic biotech IP portfolio,/extensions, and potential partnerships.
- To avoid infringement, competitors must navigate tightly defined chemical space and therapeutic claims.
- The patent landscape remains competitive, necessitating continual monitoring of related patent filings globally.
FAQs
Q1: What is the primary therapeutic focus of JP2016135253?
A: The patent targets kinase inhibitors, particularly pyrimidine derivatives, for treating cancer and proliferative diseases.
Q2: How broad are the chemical claims in JP2016135253?
A: The claims cover a wide range of pyrimidine derivatives with specific substitution patterns, providing substantial patent scope within this chemical class.
Q3: Does the patent specify particular kinase targets?
A: While the claims focus on the chemical entities, the application context suggests targeting kinases involved in tumor proliferation, notably those similar to known inhibitors like EGFR or CDK.
Q4: How does JP2016135253 compare with global kinase inhibitor patents?
A: It covers a specific subset of pyrimidine derivatives, complementing broader claims elsewhere. Its novelty depends on unique substitution patterns and specific synthesis methods.
Q5: What are the key strategic implications for competitors?
A: Competitors must design around the specific substitution patterns and claims or seek licensing to avoid infringement, especially given the patent’s broad coverage of chemical and therapeutic embodiments.
Sources:
[1] Japan Patent JP2016135253.
[2] World Intellectual Property Organization (WIPO) patent applications.
[3] PatentScope database.
