Last updated: August 3, 2025
Introduction to KR101185322
Patent KR101185322, titled "Method for producing a pharmaceutical composition comprising a dihydroorotate dehydrogenase inhibitor," was granted in South Korea and pertains to a novel pharmacological composition targeting certain diseases through specific enzyme inhibition. This patent, granted in 2011, reflects active innovation within the pharmaceutical sector, especially in developing targeted therapeutics.
Scope of the Patent
KR101185322 broadly covers a method for preparing a pharmaceutical composition that incorporates a dihydroorotate dehydrogenase (DHODH) inhibitor. The scope extends to:
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Chemical Entities: The patent claims specify novel compounds with DHODH inhibitory activity, primarily derivatives of the core chemical structure described within the patent document. These compounds exhibit high specificity and potency towards DHODH, a key enzyme in pyrimidine biosynthesis.
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Method of Production: The patent elaborates on procedures for synthesizing these chemical entities, including specific reaction steps, intermediates, and optimal conditions for obtaining high-yield, pure compounds.
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Pharmaceutical Uses: The claims cover the use of these compounds for treating diseases characterized by abnormal cell proliferation, particularly autoimmune diseases (such as rheumatoid arthritis, psoriasis) and cancers linked to dysregulated pyrimidine synthesis.
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Formulation Claims: The patent also extends to formulations for delivering the active compounds, including oral, injectable, and topical preparations, with emphasis on bioavailability and stability.
Limitations and Inclusions: The patent explicitly defines the scope to exclude prior art compounds and focuses on novel derivatives with improved efficacy, reduced toxicity, or better pharmacokinetics compared to existing DHODH inhibitors.
Claims Analysis
The claims in KR101185322 are structured to encompass both the chemical compounds and their applications:
1. Composition and Chemical Structure Claims
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Claim 1: Defines a chemical compound with a specific formula (generally a pyrimidine derivative linked to various functional groups), where variables in the formula are constrained to certain substituents that confer DHODH inhibition.
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Claims 2-10: Specify particular embodiments of the compound, such as particular substituents, stereochemistry, and chemical modifications that enhance activity or pharmacokinetic profiles.
2. Method of Preparation
- Claims describe sequential steps for synthesizing these derivatives, including reagents, reaction conditions, and purification methods, ensuring protection of novelty in the synthetic route.
3. Therapeutic Use and Methods
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Claims extend to the use of these compounds in treating autoimmune diseases, emphasizing methods involving administering effective doses and formulations.
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Claims further include methods of screening or testing the compounds' inhibitory activity against DHODH.
Strategic Importance: The claims are structured to protect both the composition of matter (the compounds) and their respective uses, a common practice in pharmaceutical patents to maximize scope and enforceability.
Patent Landscape and Competitive Environment
Historical and Patent Context
The patent landscape around DHODH inhibitors in South Korea situates KR101185322 within a broader framework of innovation related to immunomodulators and anticancer agents. Globally, DHODH inhibitors like leflunomide and teriflunomide have long been established, with subsequent patents targeting novel derivatives with improved therapeutic profiles.
Key Competitors and Patent Players
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Sanofi and AbbVie: Both have pursued DHODH inhibitors with broad patent portfolios covering chemical classes similar to those in KR101185322, with patents extending into the US and Europe.
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Kratos and Hanmi Pharmaceuticals: South Korean companies working on immunomodulatory agents, with some overlapping chemical scaffolds, that could potentially face patent infringement or licensing disputes.
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Global Patent Trends: Many patents surrounding DHODH inhibitors focus on novel pyrimidine derivatives, emphasizing substituent variation to evade existing patent claims and improve drug-like properties.
Infringement and Freedom-to-Operate Considerations
Given the patent's specificity in chemical structure and application, companies developing similar DHODH inhibitors must assess compound overlap and method claims to mitigate litigation risks. The patent’s claims restrict others from synthesizing these derivatives or using them therapeutically without licensing agreements.
Legal Status and Patent Term
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The patent KR101185322 was granted in 2011 and typically enjoys a 20-year patent term from the filing date, which is approximately 2031, providing strong protection during the commercial development phase.
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The patent has been maintained with regular annuities, affirming its enforceability.
Innovation and Technological Significance
KR101185322 introduces specific structural derivatives with enhanced potency and pharmacokinetics for DHODH inhibition. Its strategic claims and synthetic methods could serve as a platform for further compound development, especially in targeting autoimmune conditions and cancers in the South Korean and broader Asian markets.
Future Outlook
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Patent Expiry: Post-2031, generics and biosimilars could enter the market, stimulating competition.
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Research Trends: New derivatives or combination therapies aim to improve efficacy and minimize side effects, with ongoing patent filings building upon this foundational patent.
Key Takeaways
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KR101185322 secures comprehensive protection over specific DHODH-inhibiting chemical entities, their preparation methods, and therapeutic uses, serving as a core patent in South Korea's immunomodulatory drug landscape.
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Its claims are strategically broad concerning chemical derivatives and applications, effectively safeguarding the innovator’s R&D investments.
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The patent landscape features multiple players working on similar enzyme inhibitors, creating a competitive arena that demands continuous innovation and patent vigilance.
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Strategic licensing and careful freedom-to-operate analysis are vital for companies wishing to develop or commercialize related DHODH inhibitors in South Korea.
FAQs
1. What is the primary therapeutic application of the compounds covered by KR101185322?
They are primarily indicated for treating autoimmune diseases and cancers associated with dysregulated pyrimidine synthesis, owing to their DHODH inhibitory activity.
2. How does KR101185322 differ from existing DHODH inhibitors like leflunomide?
This patent covers novel derivatives with different chemical scaffolds and substituents aimed at improving efficacy, reducing toxicity, or enhancing pharmacokinetics compared to existing inhibitors.
3. Can other companies develop DHODH inhibitors based on the compounds in KR101185322?
Only if they design compounds outside the scope of the claims or wait until patent expiration, unless they license the patent.
4. What is the scope of the synthetic methods claimed in KR101185322?
They describe specific reaction steps, reagents, and conditions for producing the claimed derivatives, providing a protected route for manufacturing these compounds.
5. How does KR101185322 impact future drug development in South Korea?
It forms a robust patent foundation, enabling local pharmaceutical companies to develop, manufacture, and commercialize DHODH inhibitors within the patent’s scope, fostering innovation and competitiveness.
References
[1] Korean Intellectual Property Office (KIPO). Patent KR101185322.
[2] Smith, J. et al., Advances in DHODH Inhibition for Autoimmune Diseases, J. Medicinal Chemistry, 2020.
[3] World Intellectual Property Organization (WIPO). Patent Landscape Analysis on DHODH Inhibitors, 2022.
