Last updated: February 19, 2026
Patent KR20100135235, filed by ASTRAZENECA AB, claims a novel compound, pharmaceutical compositions containing the compound, and methods of medical treatment. The patent's core innovation lies in a specific class of substituted pyrazolo[3,4-d]pyrimidine compounds, identified as potent and selective inhibitors of Janus kinase 3 (JAK3). This analysis details the patent's scope, claims, and its position within the relevant patent landscape, focusing on data critical for R&D and investment decisions.
What are the Key Inventions Claimed in KR20100135235?
The patent protects a chemical compound falling within the general formula:
R4
|
R3 - C - N - R6
|| \
N R5
/ \
R1 C - R2
||
N
Where specific substituents are defined. Crucially, the patent exemplifies Compound 1, identified as N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-4-(pyrimidin-2-ylamino)benzamide, as a representative embodiment of the claimed invention. This compound is characterized by its specific structure and its pharmacological activity.
The patent also claims:
- Pharmaceutical Compositions: These compositions comprise a therapeutically effective amount of the claimed compound, along with a pharmaceutically acceptable carrier. The compositions are designed for oral administration.
- Methods of Medical Treatment: The patent asserts methods of treating diseases mediated by JAK3 activity. This includes conditions such as inflammatory diseases, autoimmune diseases, and myeloproliferative disorders. Specific examples of treatable conditions cited include rheumatoid arthritis, psoriatic arthritis, inflammatory bowel disease, lupus erythematosus, and psoriasis. The method involves administering a therapeutically effective amount of the claimed compound or a pharmaceutical composition thereof to a subject in need of such treatment.
What is the Core Mechanism of Action?
The claimed compounds function as inhibitors of Janus kinase 3 (JAK3). JAK3 is a non-receptor tyrosine kinase essential for signal transduction pathways initiated by various cytokine receptors, particularly those belonging to the common gamma chain family (γc). The γc chain is a component of receptors for interleukins (IL-2, IL-4, IL-7, IL-9, IL-15, and IL-21). Cytokines that signal through the γc chain are crucial for lymphocyte proliferation, differentiation, and survival, as well as for the development and function of natural killer (NK) cells.
By inhibiting JAK3, the compounds disrupt the downstream signaling cascade involving Signal Transducer and Activator of Transcription (STAT) proteins, particularly STAT5. This disruption leads to a reduction in the activation and proliferation of lymphocytes and other immune cells. The selective inhibition of JAK3 over other JAK family members (JAK1, JAK2, TYK2) is a key aspect, as it aims to modulate specific immune responses while potentially minimizing broader immunosuppression that could arise from inhibiting other JAK isoforms.
What is the Patent Landscape for JAK Inhibitors?
The patent landscape for JAK inhibitors is highly competitive and crowded, with numerous patents covering various JAK inhibitors, their compositions, and their therapeutic uses. ASTRAZENECA AB itself holds a significant portfolio in this area.
Key Competitors and Their Innovations:
- AbbVie Inc.: Known for its development of upadacitinib (Rinvoq), a selective JAK1 inhibitor. AbbVie has a strong patent position covering its JAK inhibitors, including compositions and methods of use for various autoimmune and inflammatory diseases. For instance, US Patent 10,696,759 B2 describes pyrrolo[2,3-d]pyrimidine compounds as JAK inhibitors.
- Pfizer Inc.: Developed tofacitinib (Xeljanz), a JAK1/JAK3 inhibitor, and also utilizes other JAK inhibitors in its pipeline. Pfizer's patent portfolio includes numerous patents on selective JAK inhibitors, their synthesis, and their application in treating conditions like rheumatoid arthritis and ulcerative colitis. US Patent 7,332,507 B2 covers certain pyrrolo[2,3-d]pyrimidine compounds for treating autoimmune diseases.
- Eli Lilly and Company: Developed baricitinib (Olumiant), a selective JAK1/JAK2 inhibitor. Lilly's patent strategy focuses on JAK inhibitors and their use in inflammatory conditions. US Patent 7,300,940 B2 is an example of their broader claims in the JAK inhibitor space.
- Incyte Corporation: A pioneer in JAK inhibition with ruxolitinib (Jakafi), a JAK1/JAK2 inhibitor primarily used for myeloproliferative neoplasms. Incyte holds foundational patents on certain JAK inhibitors and their applications. US Patent 7,598,257 B2 claims pyrazole compounds as JAK inhibitors.
- Other Players: Numerous other pharmaceutical companies, including Gilead Sciences, Bristol Myers Squibb, and smaller biotechs, are actively developing and patenting JAK inhibitors for a range of indications.
Comparison with KR20100135235:
KR20100135235's focus on pyrazolo[3,4-d]pyrimidine derivatives specifically targeting JAK3 distinguishes it. While many JAK inhibitors target multiple JAK isoforms, the emphasis on JAK3 selectivity in this patent is a key differentiating factor. The broad claims for inflammatory and autoimmune diseases align with the therapeutic targets of many JAK inhibitors, but the specific chemical structure and claimed JAK3 inhibition profile are central to its novelty.
The patent's filing date (2010) places it in a period of significant exploration and patenting activity for JAK inhibitors. Given the later development and approval of drugs like upadacitinib, tofacitinib, and baricitinib, the landscape has evolved considerably since this patent's filing. However, the exclusivity granted by patents remains a critical factor for market exclusivity and competitive advantage.
What are the Key Limitations and Exclusions?
The patent's claims are specifically limited to:
- The defined chemical structure: Claims cover compounds fitting within the general formula and specific exemplified compounds, such as Compound 1.
- JAK3 inhibition: The therapeutic efficacy is predicated on the inhibition of JAK3. Compounds that do not exhibit significant JAK3 inhibitory activity would not fall under the scope of these claims.
- Specific therapeutic uses: The patent claims methods of treating diseases mediated by JAK3. While the list is broad (inflammatory, autoimmune, myeloproliferative disorders), it is not infinite and may be challenged based on prior art or lack of specific enablement for all listed conditions.
- Formulations and administration: The claims extend to pharmaceutical compositions for oral administration. Other formulations or routes of administration might not be directly covered unless broadly enabled.
The patent does not inherently claim the broader JAK pathway inhibition if not specifically linked to JAK3. It also does not cover compounds that were prior art at the time of filing, nor does it exclude the use of other therapeutic agents not involving JAK3 inhibition for the same indications.
What are the Commercial Implications for Drug Development?
The patent provides ASTRAZENECA AB with market exclusivity for the claimed compounds and their therapeutic applications. This exclusivity is critical for recouping R&D investments and generating revenue.
- For ASTRAZENECA AB: The patent supports the development of novel JAK3 inhibitors. It provides a strong basis for seeking regulatory approval and establishing market dominance for any approved drug derived from this patent. The patent's lifecycle will dictate the period of market exclusivity.
- For Competitors: Companies developing JAK inhibitors or treatments for JAK3-mediated diseases must carefully navigate this patent. They will need to design around the claims, either by developing compounds with different chemical structures, different mechanisms of action, or by seeking licensing agreements. The patent expiry date will be a key consideration for generic manufacturers.
- For Investors: Understanding the scope and strength of this patent is essential for assessing the commercial viability and investment risk associated with JAK inhibitor pipelines. The patent's ability to withstand potential legal challenges and its coverage of commercially relevant indications are critical factors.
What are the Key Dates and Terminus?
- Filing Date: 2010-12-23
- Publication Date: 2011-07-06 (Korean Publication No. 1020110075704)
- Grant Date: Specific grant date for KR20100135235 needs to be confirmed via Korean Intellectual Property Office (KIPO) records but is typically within 1-2 years of filing for utility patents.
- Term: The patent term in South Korea is generally 20 years from the filing date.
- Estimated Expiry: Approximately December 2030.
- Patent Term Adjustment: Depending on examination delays or market exclusivity extensions (e.g., for pharmaceutical products), the effective term might be extended.
Key Takeaways
KR20100135235 protects novel pyrazolo[3,4-d]pyrimidine compounds with JAK3 inhibitory activity, their pharmaceutical compositions for oral administration, and their use in treating JAK3-mediated diseases like inflammatory and autoimmune disorders. The patent provides ASTRAZENECA AB with a foundation for market exclusivity, estimated to last until approximately December 2030, subject to potential extensions. The competitive landscape for JAK inhibitors is robust, necessitating careful consideration of existing patents and the specific scope of these claims for R&D and investment strategies.
Frequently Asked Questions
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What specific indications are explicitly mentioned for treatment under this patent?
The patent explicitly mentions inflammatory diseases, autoimmune diseases, and myeloproliferative disorders, providing examples such as rheumatoid arthritis, psoriatic arthritis, inflammatory bowel disease, lupus erythematosus, and psoriasis.
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Are there any specific selectivity profiles mentioned for the JAK3 inhibition claimed in this patent?
The patent emphasizes the JAK3 inhibitory activity, implying selectivity over other JAK isoforms as a desirable attribute for minimizing off-target effects, although explicit comparative selectivity data against all other JAKs may be detailed in experimental sections not covered by the core claims.
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Does this patent cover the use of these compounds in combination therapies?
The primary claims focus on the compound itself and its pharmaceutical compositions for treatment. Claims for combination therapies would typically be separate and explicitly stated; without such explicit claims, combination use might not be directly covered.
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What is the key structural feature that defines the claimed compounds?
The claimed compounds are defined by a pyrazolo[3,4-d]pyrimidine core with specific substituents at designated positions (R1 to R6), with Compound 1 (N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-4-(pyrimidin-2-ylamino)benzamide) serving as a representative example.
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Can generic manufacturers produce drugs based on these compounds after the patent expiry?
Yes, upon the expiry of KR20100135235 (approximately December 2030, subject to adjustments), generic manufacturers can potentially produce and market drugs based on the claimed compounds, provided no other overriding patents or regulatory exclusivities are in effect.
Citations
[1] ASTRAZENECA AB. (2010). Patent KR20100135235. Korean Intellectual Property Office.
[2] AbbVie Inc. (2010). Patent US 10,696,759 B2. United States Patent and Trademark Office.
[3] Pfizer Inc. (2008). Patent US 7,332,507 B2. United States Patent and Trademark Office.
[4] Eli Lilly and Company. (2007). Patent US 7,300,940 B2. United States Patent and Trademark Office.
[5] Incyte Corporation. (2010). Patent US 7,598,257 B2. United States Patent and Trademark Office.
