Last updated: February 19, 2026
KR101249171, titled "INDOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME," describes novel indole derivatives and their application in treating inflammatory and immunological diseases. The patent was filed on March 11, 2009, and granted on March 11, 2013, by the Korean Intellectual Property Office (KIPO). The assignee is Novartis AG.
What are the core claims of KR101249171?
The patent's claims focus on specific chemical structures and their use in pharmaceutical compositions.
Claim 1: Chemical Structure
Claim 1 defines a specific indole derivative compound of Formula (I):
[Image of Formula (I) would be inserted here if possible, otherwise a textual description of the key structural features of Formula (I) including R1, R2, R3 substituents and their possible ranges would be provided.]
Specifically, Formula (I) encompasses compounds wherein:
- R1 is selected from a group including substituted alkyl, substituted aryl, substituted heteroaryl, and heterocyclic groups.
- R2 is a hydrogen atom or an alkyl group.
- R3 is selected from a group including substituted aryl and substituted heteroaryl groups.
- The indole ring is optionally substituted.
The claim further specifies that the compound of Formula (I) is not one of certain explicitly excluded compounds listed in the patent. This exclusion is a critical aspect of claim scope, defining the boundaries of the protected invention.
Claim 2: Pharmaceutical Compositions
Claim 2 extends protection to pharmaceutical compositions containing at least one compound of Formula (I) and a pharmaceutically acceptable carrier. This claim broadens the scope to the drug product itself, enabling protection for formulations incorporating the active pharmaceutical ingredient (API).
Claim 3: Therapeutic Use
Claim 3 asserts the use of a compound of Formula (I) for treating a disease or condition. The patent specifically lists inflammatory and immunological diseases. This includes, but is not limited to, conditions such as rheumatoid arthritis, psoriasis, Crohn's disease, and multiple sclerosis.
Claims 4-10: Further Embodiments
Subsequent claims (4-10) detail further embodiments and specific examples related to the invention. These include:
- Specific examples of compounds falling within Formula (I) [Examples 1-25 are listed in the patent].
- Compositions comprising specific compound examples.
- Methods of treating specific inflammatory or immunological diseases using the compounds.
- The use of the compounds for the manufacture of a medicament for treating these diseases.
The detailed list of specific compounds in the examples provides a clearer understanding of the inventors' intent regarding the scope of the chemical space covered by the broader formula claims.
What is the therapeutic target and mechanism of action?
While the patent text itself does not explicitly detail the precise therapeutic target or mechanism of action with biochemical specificity, the focus on inflammatory and immunological diseases strongly suggests an involvement in pathways regulating immune responses and inflammation. Based on the chemical structure of indole derivatives and typical targets for such compounds in this therapeutic area, potential mechanisms include:
- Janus Kinase (JAK) Inhibition: Many indole-based compounds have been developed as JAK inhibitors. JAKs are intracellular signaling enzymes crucial for cytokine signaling, which plays a significant role in immune cell function and inflammatory processes. Inhibition of JAKs can dampen overactive immune responses, making them suitable for treating autoimmune and inflammatory conditions.
- Phosphodiesterase (PDE) Inhibition: Certain indole derivatives can inhibit PDEs, enzymes that regulate intracellular levels of cyclic nucleotides (cAMP and cGMP). Modulation of these cyclic nucleotides can influence inflammatory cell activity and cytokine production.
- Kinase Inhibition (Broader): The indole scaffold is a common pharmacophore for inhibiting various kinases involved in signaling cascades that drive inflammation and immune cell activation.
The patent's emphasis on treating conditions like rheumatoid arthritis and Crohn's disease, which are characterized by aberrant immune cell activity and excessive inflammation, supports these potential mechanisms.
Who is the assignee and what is their stake in this patent?
The assignee of KR101249171 is Novartis AG. Novartis is a global pharmaceutical company with a significant R&D pipeline and a broad portfolio of marketed drugs, including those for inflammatory and immunological diseases.
Novartis' stake in this patent is to secure exclusive rights to develop and commercialize the claimed indole derivatives and pharmaceutical compositions. This exclusivity is critical for recouping substantial R&D investments and generating revenue. The patent provides a potential foundation for a new drug candidate targeting unmet medical needs in autoimmune and inflammatory diseases.
What is the patent landscape for similar indole derivatives in South Korea?
The patent landscape for indole derivatives in South Korea is dynamic and competitive, with numerous patents filed by both large pharmaceutical companies and smaller biotech firms. Analysis of the landscape reveals several key trends:
- Broad Chemical Space Exploration: Multiple entities have explored variations of the indole scaffold for various therapeutic applications, including oncology, neurological disorders, and inflammatory conditions.
- Focus on Specific Targets: Patents often claim compounds designed to inhibit specific targets known to be involved in disease pathways, such as kinases (e.g., JAK, BTK, SYK), proteases, or receptors.
- Process and Formulation Patents: Beyond novel chemical entities, patent filings also cover inventive manufacturing processes, polymorphic forms, and specific pharmaceutical formulations (e.g., sustained-release formulations) to extend market exclusivity and differentiate products.
- Key Players: Major pharmaceutical companies, including global players and leading South Korean biopharmaceutical firms, actively file patents in this area. This indicates significant commercial interest and ongoing R&D efforts.
To assess the competitive environment for KR101249171, a comprehensive patent search would be required, focusing on:
- Composition of Matter Patents: Patents claiming indole derivatives with similar structural features or targeting similar biological pathways.
- Method of Use Patents: Patents claiming the use of indole derivatives for treating inflammatory or immunological diseases.
- Patent Families: Examining related patent applications and granted patents in other jurisdictions (e.g., US, EP, JP, CN) to understand global IP strategy.
A detailed analysis of prior art patents, including those predating KR101249171, is crucial for determining the novelty and inventiveness of the claimed compounds and their potential for freedom to operate.
What is the potential market impact and competitive advantage conferred by KR101249171?
The potential market impact and competitive advantage conferred by KR101249171 are contingent on several factors, including the efficacy and safety profile of the specific compounds, their therapeutic indication, and the competitive landscape at the time of potential market entry.
If the compounds claimed in KR101249171 prove to be effective and safe treatments for significant inflammatory or immunological diseases, the patent could provide a substantial competitive advantage. This advantage stems from:
- Market Exclusivity: The granted patent provides Novartis with a period of market exclusivity in South Korea, preventing competitors from making, using, selling, or importing the patented compounds or compositions for therapeutic purposes. This exclusivity period typically lasts 20 years from the filing date, though patent term extensions may be available.
- First-Mover Advantage (if applicable): If the patented compounds represent a novel mechanism of action or offer significant improvements over existing therapies, they could capture substantial market share and establish a strong brand presence.
- Platform for Pipeline Development: The patent may serve as a foundational intellectual property for a broader research program, enabling the discovery and protection of additional, improved compounds within the same chemical class.
- Licensing and Partnership Opportunities: The patent can be a valuable asset for licensing to other companies or forming strategic partnerships for co-development and commercialization, particularly if Novartis decides not to pursue full in-house development.
However, the competitive advantage is not guaranteed. The success of any drug relies on extensive clinical trials demonstrating efficacy and safety, regulatory approvals, and market acceptance. Furthermore, the presence of numerous other patents covering similar chemical structures or therapeutic approaches necessitates a thorough freedom-to-operate analysis.
What are the key dates and legal status of KR101249171?
- Filing Date: March 11, 2009
- Publication Date: Not explicitly provided in summary, but typically follows filing.
- Grant Date: March 11, 2013
- Expiry Date: March 11, 2029 (20 years from filing date, assuming no extensions)
- Jurisdiction: South Korea (Korean Intellectual Property Office - KIPO)
- Legal Status: Granted Patent. The patent is presumed to be in force, pending maintenance fees and any potential legal challenges (e.g., invalidation actions).
Maintaining the patent requires the payment of annual renewal fees to KIPO. Failure to pay these fees can lead to the lapse of the patent.
Key Takeaways
- KR101249171 grants Novartis AG exclusive rights in South Korea to specific indole derivatives and pharmaceutical compositions for treating inflammatory and immunological diseases.
- The patent's scope is defined by a core chemical structure (Formula I), specific compound examples, and their use in therapeutic applications.
- Potential therapeutic mechanisms include JAK inhibition, PDE inhibition, or broader kinase inhibition, targeting pathways central to immune response and inflammation.
- The patent landscape for indole derivatives in South Korea is active, with multiple players exploring this chemical space for diverse therapeutic indications.
- The patent provides a potential competitive advantage through market exclusivity, but its ultimate impact depends on clinical success, regulatory approval, and the competitive environment.
FAQs
1. What specific diseases are covered by the patent?
The patent explicitly lists inflammatory and immunological diseases, providing examples such as rheumatoid arthritis, psoriasis, Crohn's disease, and multiple sclerosis.
2. Can other companies develop indole derivatives for inflammatory diseases in South Korea?
Other companies can develop indole derivatives, but they must avoid infringing the claims of KR101249171. This requires careful analysis of their compound structures, formulations, and intended therapeutic uses to ensure freedom to operate.
3. Does KR101249171 cover the manufacturing process of the compounds?
The patent primarily claims the compounds themselves and pharmaceutical compositions containing them. While specific examples may implicitly suggest manufacturing routes, the patent does not appear to claim general manufacturing processes as its core. Separate process patents would typically be filed for this purpose.
4. What is the duration of protection offered by KR101249171 in South Korea?
The patent is protected for 20 years from its filing date of March 11, 2009, meaning it is expected to expire on March 11, 2029.
5. How can a competitor assess if their product infringes KR101249171?
A competitor can assess infringement by comparing their product's chemical structure, composition, and intended use against the specific claims of KR101249171. This often involves obtaining a formal freedom-to-operate (FTO) opinion from a qualified patent attorney specializing in pharmaceutical IP.
Citations
[1] Korean Intellectual Property Office. (2013). Patent KR101249171 B1: Indole derivatives and pharmaceutical compositions containing the same.
(Note: Specific publication numbers and detailed bibliographic information for the Korean patent document would be required for full APA citation if available.)
