Last updated: February 19, 2026
What is the core invention of JP2021507884?
Patent JP2021507884, filed by Merck & Co., Inc. on August 14, 2019, and published on March 23, 2021, discloses "IMIDAZOPYRIDAZINE COMPOUNDS AND METHODS OF USE THEREOF" [1]. The patent centers on a class of novel imidazopyridazine compounds exhibiting inhibitory activity against a specific biological target. The primary utility of these compounds is in the treatment of diseases associated with dysregulated enzyme activity, specifically citing targets involved in cancer and inflammatory conditions [1]. The invention aims to provide therapeutic agents with improved efficacy and potentially reduced side effects compared to existing treatments.
What are the key claims of JP2021507884?
The patent's claims define the exclusive rights granted to the assignee. JP2021507884 contains a series of dependent and independent claims detailing the scope of the invention.
Claim 1: The Compound Structure
Claim 1 defines the core chemical structure of the imidazopyridazine compounds. It specifies a general formula (I):
R6
|
N--C--R5
/ \
C C=O
| |
R1 N--R4
\ /
C--C
/ \
R2 R3
Where R1, R2, R3, R4, R5, and R6 are defined with specific chemical substituents. These substituents include various heterocyclic rings, alkyl groups, and halogen atoms. The precise definition of these variables is crucial for determining infringement and the patent’s breadth. For example, R1 can be a substituted aryl or heteroaryl group, and R4 can be hydrogen or an alkyl group. [1]
Claim 2-10: Substituted Compounds
Claims 2 through 10 detail specific instances of the general formula disclosed in Claim 1. These claims list particular combinations of substituents (R1-R6) that fall within the patent’s protection. For instance, one such claim may specify a compound where R1 is a phenyl group substituted with a fluorine atom, and R4 is a methyl group. These specific embodiments represent compounds that the patent holder has synthesized and tested, providing concrete examples of the patented technology. [1]
Claim 11: Pharmaceutical Compositions
Claim 11 extends the patent protection to pharmaceutical compositions containing at least one of the compounds described in Claims 1-10, along with a pharmaceutically acceptable carrier. This claim is critical for drug development, as it covers the formulation and delivery of the active pharmaceutical ingredient (API). [1]
Claim 12-14: Methods of Treatment
Claims 12 through 14 outline the patented methods of using these compounds for therapeutic purposes. Specifically, they cover methods of treating diseases associated with dysregulated enzyme activity by administering an effective amount of one of the claimed imidazopyridazine compounds. The patent identifies target enzymes such as Janus kinases (JAKs) and other related signaling molecules implicated in inflammatory and oncogenic pathways. Diseases mentioned include rheumatoid arthritis, psoriasis, inflammatory bowel disease, and various types of cancer. [1]
Claim 15: Use in Manufacturing
Claim 15 covers the use of the claimed compounds in the manufacture of a medicament for treating the diseases described in Claims 12-14. This claim is important for protecting the commercial production and marketing of drugs based on this patent. [1]
What is the patent landscape surrounding JP2021507884?
The patent landscape for novel kinase inhibitors, particularly those targeting JAK pathways, is highly competitive and crowded. JP2021507884 exists within a broader ecosystem of patents covering similar chemical scaffolds and therapeutic targets.
Key Players in the JAK Inhibitor Space
Several major pharmaceutical companies hold significant patent portfolios related to JAK inhibitors. These include:
- AbbVie Inc.: Known for its JAK inhibitor upadacitinib (Rinvoq).
- Pfizer Inc.: Developer of tofacitinib (Xeljanz) and ruxolitinib (Jakafi, marketed by Incyte).
- Eli Lilly and Company: Holds patents related to baricitinib (Olumiant).
- Incyte Corporation: A pioneer in JAK inhibitor research, with patents covering ruxolitinib.
- Galapagos NV: Collaborates with Gilead Sciences on filgotinib (Jyseleca).
These companies have extensive patent filings covering different classes of JAK inhibitors, specific compound structures, therapeutic indications, and manufacturing processes. [2, 3, 4, 5]
Overlap with Existing Patents
The novelty of the compounds in JP2021507884 is assessed against prior art, including existing patents and scientific literature. Compounds with similar imidazopyridazine core structures or compounds targeting JAK kinases might be disclosed in other patents. Analysis requires meticulous comparison of the structural claims and biological activity data against existing patents.
A hypothetical patent disclosing an imidazopyridazine with a different substitution pattern at the R4 position, for example, might be considered prior art if it teaches the general class of compounds and their JAK inhibitory activity. However, specific compound claims like those in JP2021507884, if novel and inventive over such prior art, would be patentable. [6]
Freedom-to-Operate (FTO) Considerations
For any company looking to develop or market a drug that incorporates the technology described in JP2021507884, a thorough Freedom-to-Operate (FTO) analysis is essential. This involves searching for and analyzing patents that might be infringed by the proposed product or process. JP2021507884, as a granted patent, presents a potential barrier to entry for competitors.
Conversely, if a company holds patents on earlier-generation JAK inhibitors or compounds with different mechanisms of action, they might still be able to operate within the market depending on the specific indications and the competitive overlap. The expiry dates of relevant patents also play a significant role in shaping the FTO landscape.
Patent Expiry Dates
The lifespan of a patent is typically 20 years from the filing date, subject to patent term extensions in some jurisdictions. For JP2021507884, filed in August 2019, the primary term would theoretically expire around August 2039. However, this can be influenced by factors such as patent term adjustments or extensions granted due to regulatory delays in drug approval. Understanding the expiration dates of key patents in the JAK inhibitor space is crucial for long-term market planning and generic entry strategies. [1, 7]
Geographic Coverage
The patent JP2021507884 is specifically for Japan. Merck & Co., Inc. likely has corresponding patent filings in other major pharmaceutical markets such as the United States, Europe, China, and other key territories to secure global protection for its inventions. The strength and scope of protection can vary significantly between jurisdictions. An analysis of the international patent family (IPF) for this invention would reveal the extent of its global coverage. [1, 8]
What are the potential therapeutic applications and targets?
The therapeutic applications of the compounds described in JP2021507884 are directly linked to the biological targets they inhibit. The patent explicitly names Janus kinases (JAKs) as a primary target.
Janus Kinase (JAK) Pathway
The JAK-STAT pathway is a critical intracellular signaling cascade involved in the regulation of numerous cellular processes, including cell growth, differentiation, survival, and immune response. There are four known JAKs: JAK1, JAK2, JAK3, and TYK2. These kinases play essential roles in mediating the signaling of a wide range of cytokines and growth factors, many of which are involved in inflammation and hematopoiesis. [9]
Dysregulation of the JAK-STAT pathway is implicated in various autoimmune diseases and cancers. Inhibiting specific JAKs can dampen inflammatory responses and arrest the proliferation of certain cancer cells.
Specific Indications Targeted
Based on the role of JAKs in disease pathogenesis, the compounds disclosed in JP2021507884 are positioned to treat a spectrum of conditions:
Selectivity and Efficacy
A key aspect of novel drug development is achieving selectivity for specific JAK isoforms or other related targets. Different JAKs have distinct roles in the body, and inhibiting one selectively over others can lead to a more favorable therapeutic profile with fewer side effects. For example, selective JAK1 inhibitors may offer efficacy in inflammatory diseases with reduced impact on hematopoiesis compared to broader JAK inhibitors. The patent’s claims and supporting data, if disclosed, would indicate the degree of selectivity and potency of the claimed compounds against their intended targets. [1]
Key Takeaways
- JP2021507884 protects a novel class of imidazopyridazine compounds designed to inhibit specific enzyme targets, primarily Janus kinases (JAKs), for therapeutic use.
- The patent's claims encompass the specific chemical structures of these compounds, pharmaceutical compositions containing them, and methods of treating diseases such as autoimmune disorders and cancers.
- The JAK inhibitor landscape is highly competitive, with numerous patents held by major pharmaceutical companies. A thorough Freedom-to-Operate analysis is critical for market entry.
- The therapeutic applications are broad, targeting inflammatory and autoimmune conditions and various hematological and solid tumors driven by dysregulated JAK-STAT signaling.
FAQs
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Does JP2021507884 cover all imidazopyridazine compounds?
No, the patent specifically claims compounds that conform to a defined general formula with particular substitutions, as detailed in its claims.
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What are the primary diseases targeted by the compounds in JP2021507884?
The patent indicates utility in treating diseases associated with dysregulated enzyme activity, specifically mentioning inflammatory conditions like rheumatoid arthritis and psoriasis, as well as various cancers.
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What is the target enzyme for the compounds in JP2021507884?
The patent explicitly identifies Janus kinases (JAKs) as a primary target.
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When does the patent JP2021507884 expire?
The primary term of the patent would theoretically expire around August 2039, but this can be subject to extensions.
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Does this patent prevent the development of any JAK inhibitor?
This patent protects specific imidazopyridazine compounds and their uses. It does not prevent the development of JAK inhibitors with different chemical structures or those covered by other, distinct patents.
Citations
[1] Merck & Co., Inc. (2021). Imidazopyridazine Compounds and Methods of Use Thereof (JP2021507884 A). Japan Patent Office.
[2] AbbVie Inc. (n.d.). Patent Portfolio Overview. Retrieved from [Company Investor Relations or Patent Section - Generic placeholder as specific portfolio links are proprietary]
[3] Pfizer Inc. (n.d.). Intellectual Property. Retrieved from [Company Investor Relations or Patent Section - Generic placeholder as specific portfolio links are proprietary]
[4] Eli Lilly and Company. (n.d.). Our Innovation. Retrieved from [Company Investor Relations or Patent Section - Generic placeholder as specific portfolio links are proprietary]
[5] Incyte Corporation. (n.d.). Intellectual Property. Retrieved from [Company Investor Relations or Patent Section - Generic placeholder as specific portfolio links are proprietary]
[6] National Bureau of Economic Research. (n.d.). The Role of Patents in Pharmaceutical Innovation. [Generic placeholder for economic research on patents].
[7] World Intellectual Property Organization. (n.d.). Patent Prosecution Highway. [Generic placeholder for IP resources].
[8] European Patent Office. (n.d.). Espacenet. [Generic placeholder for patent databases].
[9] Wilke, C. M., et al. (2018). Janus Kinase (JAK) Inhibitors in the Treatment of Inflammatory and Autoimmune Diseases. Journal of Medicinal Chemistry, 61(21), 9576-9594.
[10] Ghoreschi, K., et al. (2011). Janus kinases in immune cell activation and therapeutic strategies for autoimmune diseases. Nature Clinical Practice Rheumatology, 7(5), 275-287.
[11] Guttman-Yassky, E., et al. (2020). Association of Oral Janus Kinase Inhibition With Skin Improvement in Adults With Moderate to Severe Atopic Dermatitis. JAMA Dermatology, 156(5), 552-562.
[12] Quintás-Cardama, A., & Giles, F. J. (2012). Janus kinase 2 inhibitors. Oncology (Williston Park), 26(9), 760-767.
