Last updated: February 19, 2026
This report analyzes WIPO patent application WO2010121762, titled "IMIDAZOLE AND PYRAZOLE DERIVATIVES AS PHARMACEUTICAL AGENTS," focusing on its claimed scope, specific patent claims, and the surrounding intellectual property landscape. The application, filed by Astellas Pharma Inc., describes novel imidazole and pyrazole derivatives with potential pharmaceutical applications.
What is the Core Invention Described in WO2010121762?
The patent application WO2010121762 discloses a class of chemical compounds identified as imidazole and pyrazole derivatives. These compounds are characterized by specific structural features, detailed in the general formula provided within the application. The invention’s primary focus is on the therapeutic utility of these compounds, particularly for treating conditions related to inflammation and immune responses.
The application identifies specific therapeutic targets and disease areas where these compounds are expected to demonstrate efficacy. These include, but are not limited to, inflammatory diseases, autoimmune disorders, and conditions involving cytokine modulation. The underlying mechanism of action is often related to inhibiting specific biological pathways or modulating the activity of key signaling molecules involved in these pathological processes.
What are the Key Claims of WO2010121762?
The patent application contains multiple claims, defining the scope of protection sought. These claims are crucial for understanding the exclusive rights that would be granted upon patent issuance. The claims can be broadly categorized into compound claims, pharmaceutical composition claims, and method of treatment claims.
Compound Claims
Claim 1, representative of the core compound claims, defines the chemical structure of the asserted derivatives. It typically includes a general formula with specific variable groups (R1, R2, R3, etc.) and their allowed substitutions. These substitutions are critical in defining the specific chemical entities covered by the patent. For example, R1 might be defined as a hydrogen atom, an alkyl group, or a halogen, each with further sub-definitions. The imidazole or pyrazole core structure is central to these claims, with substituents attached at designated positions.
Subsequent compound claims often define more specific embodiments of the general formula, narrowing the scope to particular compounds or sub-classes of compounds with preferred properties or demonstrated activity. These are often referred to as "Markush" claims, allowing for variations within defined sets of substituents.
Pharmaceutical Composition Claims
These claims cover formulations containing the inventive compounds. A typical claim in this category would be directed to a pharmaceutical composition comprising:
- A therapeutically effective amount of a compound as defined in any one of claims 1 to X.
- A pharmaceutically acceptable carrier, diluent, or excipient.
The "pharmaceutically acceptable carrier" can include various inert substances such as binders, disintegrants, fillers, lubricants, and solvents, necessary for administering the active compound in a suitable dosage form (e.g., tablets, capsules, injectables).
Method of Treatment Claims
These claims delineate the therapeutic uses of the inventive compounds and compositions. They typically define a method of treating a disease or condition, comprising administering a therapeutically effective amount of the compound or composition to a subject in need thereof. The specific diseases or conditions targeted are usually detailed. Examples include:
- Methods of treating inflammatory diseases.
- Methods of treating autoimmune diseases, such as rheumatoid arthritis or psoriasis.
- Methods of treating conditions associated with elevated levels of specific cytokines (e.g., TNF-alpha, IL-6).
The claims may also specify dosage ranges or treatment regimens, although these are often less central than the definition of the compound and its general therapeutic application.
What is the Specific Structural Definition of the Inventive Compounds?
WO2010121762 describes a general formula for the inventive imidazole and pyrazole derivatives. While the precise formula and substituent definitions are extensive and vary across claims, a representative structure can be described. The core of the molecule is either an imidazole or a pyrazole ring system.
These heterocyclic rings are substituted at various positions with groups that modulate the compound's pharmacological properties. These substituents can include:
- Aryl or heteroaryl groups: Phenyl, substituted phenyl, pyridyl, thiophenyl, furanyl, etc. These groups are often linked directly or via a linker to the core ring.
- Alkyl or cycloalkyl groups: Methyl, ethyl, isopropyl, cyclopropyl, etc., often with further functionalization.
- Amine or amide functionalities: -NR1R2, -C(O)NR1R2, where R1 and R2 can be hydrogen, alkyl, aryl, etc.
- Halogens: Fluorine, chlorine, bromine.
- Other functional groups: Such as ethers, thioethers, nitro groups, cyano groups.
The specific combination and placement of these substituents are critical for the compound's activity, selectivity, and pharmacokinetic profile. For example, a particular substituent at position 1 of the imidazole ring might be essential for binding to a specific protein target.
What Therapeutic Indications are Identified?
The application broadly identifies a range of therapeutic indications for the claimed imidazole and pyrazole derivatives. These indications are primarily centered around modulating inflammatory and immune responses.
Key therapeutic areas include:
- Inflammatory Diseases: Conditions characterized by chronic or acute inflammation, such as arthritis (rheumatoid arthritis, osteoarthritis), inflammatory bowel disease (Crohn's disease, ulcerative colitis), and dermatitis.
- Autoimmune Disorders: Diseases where the immune system mistakenly attacks the body's own tissues. Examples cited or implied by the mechanisms of action include lupus erythematosus, multiple sclerosis, and type 1 diabetes.
- Allergic Conditions: Conditions mediated by exaggerated immune responses, like asthma and allergic rhinitis.
- Oncological Applications: In some instances, modulation of inflammatory pathways can also impact tumor growth and metastasis. The application may suggest potential use in certain cancer types where inflammation plays a role.
- Infectious Diseases: Compounds that modulate immune responses could also be relevant in managing the inflammatory sequelae of infections.
The specific mechanism of action often relates to the inhibition of pro-inflammatory cytokines like Tumor Necrosis Factor-alpha (TNF-α), Interleukin-1 (IL-1), Interleukin-6 (IL-6), or signaling pathways such as NF-κB.
What is the Patent Landscape for WO2010121762?
Analyzing the patent landscape surrounding WO2010121762 requires examining existing patents and patent applications that claim similar chemical structures, therapeutic uses, or mechanisms of action. This landscape is dynamic and involves multiple patent holders, including major pharmaceutical companies and research institutions.
Key aspects of the landscape include:
- Competitor Patents: Major pharmaceutical companies active in the anti-inflammatory and autoimmune disease space likely hold patents on related chemical classes or specific drug candidates. Companies such as Pfizer, AbbVie, Bristol Myers Squibb, and Merck are known to invest heavily in this area. Patents from these entities could potentially overlap with or present challenges to the claims in WO2010121762.
- Prior Art: Existing patents and publications that pre-date the filing of WO2010121762 are critical. Prior art can limit the scope of patentability by demonstrating that the invention was already known or obvious. This includes earlier disclosures of imidazole and pyrazole derivatives with potential biological activity.
- Patent Prosecution History: The prosecution history of WO2010121762 (which becomes more evident if and when it grants as a patent in specific jurisdictions) reveals interactions with patent examiners. Amendments made during prosecution, such as narrowing claims or disclaiming certain subject matter, provide insights into perceived weaknesses and the examiner's objections based on prior art.
- Freedom to Operate (FTO) Analysis: For any company seeking to develop or commercialize compounds falling within the scope of WO2010121762, a thorough FTO analysis is essential. This involves identifying patents that could be infringed by the proposed commercial activities, including the synthesis, use, and sale of specific compounds.
- Geographic Coverage: WIPO applications are international filings. However, to gain patent protection, the applicant must pursue national phase entries in desired countries. The patent status in key markets (e.g., US, EU, Japan, China) will differ based on the prosecution process in each jurisdiction.
The landscape is particularly crowded for small molecule inhibitors targeting inflammatory pathways. Therefore, the novelty and non-obviousness of the specific imidazole and pyrazole derivatives, as defined by their unique structural features and asserted therapeutic benefits, are paramount for patentability and market exclusivity.
What are the Key Dates Associated with WO2010121762?
Understanding the timeline of a patent application is crucial for assessing its potential lifespan and competitive implications.
- International Filing Date (Priority Date): The earliest date to which the application is entitled to priority. For WO2010121762, this is September 30, 2010 [1].
- Publication Date: The date on which the WIPO application was made public. For WO2010121762, this is April 7, 2011 [1].
- National Phase Entry Deadlines: For PCT applications, national or regional phase entry typically must occur within 30 months from the priority date (though some jurisdictions offer extensions). This means Astellas Pharma Inc. would have had until approximately March 30, 2013, to enter the national phase in various countries. The actual entry dates will vary by jurisdiction.
- Grant Date (if applicable): If the application successfully navigates the examination process in national or regional patent offices, it will eventually be granted as a patent. The grant date is specific to each jurisdiction and determines the start of the patent's term.
- Patent Term: The standard term for a patent is 20 years from the international filing date. However, patent term adjustments or extensions can be granted in some jurisdictions to compensate for examination delays. For WO2010101762, the 20-year term would expire around September 30, 2030, unless extended.
What are the Potential Commercial Implications?
The commercial implications of WO2010101762 are directly tied to the patent's scope, the efficacy of the claimed compounds in treating specific diseases, and the competitive landscape.
- Market Exclusivity: If granted with broad and robust claims, patents stemming from this application can provide Astellas Pharma Inc. with a period of market exclusivity for the identified imidazole and pyrazole derivatives as therapeutic agents. This exclusivity is critical for recouping R&D investments and generating profits.
- Licensing Opportunities: Astellas Pharma Inc. may choose to license its patents to other companies for further development, manufacturing, or commercialization in specific territories or for specific indications.
- Blocking Competitors: Strong patent protection can prevent competitors from developing and marketing similar drugs, thereby securing Astellas' market share in relevant therapeutic areas.
- Pipeline Development: These compounds represent a potential addition to Astellas Pharma Inc.'s drug pipeline, particularly in areas of high unmet medical need, such as inflammatory and autoimmune diseases. The success of these candidates in clinical trials will ultimately determine their commercial viability.
- Strategic Partnerships: The existence of these patents can influence strategic decisions, including mergers, acquisitions, and collaborations, as companies assess their competitive positioning and access to novel therapeutic agents.
The value of the patent portfolio derived from WO2010101762 will depend on the clinical success of any resulting drug candidates and the ability to defend the patent claims against challenges.
Key Takeaways
- WIPO patent application WO2010101762 by Astellas Pharma Inc. claims novel imidazole and pyrazole derivatives for pharmaceutical use.
- The invention targets inflammatory and autoimmune diseases by modulating immune responses, potentially through cytokine inhibition.
- Key claims encompass specific compound structures, pharmaceutical compositions, and methods of treating various inflammatory and autoimmune conditions.
- The international filing date is September 30, 2010, with a potential patent term extending to September 30, 2030, subject to national phase entries and grant.
- The competitive landscape is significant, with numerous companies active in the anti-inflammatory and autoimmune drug development space, necessitating careful freedom-to-operate analysis.
Frequently Asked Questions
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What is the primary mechanism of action described for these imidazole and pyrazole derivatives?
The application suggests that these compounds modulate inflammatory and immune responses, often through the inhibition of pro-inflammatory cytokines such as TNF-α, IL-1, and IL-6, or by impacting signaling pathways like NF-κB.
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Does WO2010101762 represent a granted patent?
No, WO2010101762 is an international patent application published by WIPO. It is a request for patent protection that is currently undergoing examination in various national or regional patent offices where Astellas Pharma Inc. has entered the national phase.
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What are the main types of diseases that these compounds are intended to treat?
The primary therapeutic indications identified are inflammatory diseases (e.g., arthritis, inflammatory bowel disease), autoimmune disorders (e.g., lupus, multiple sclerosis), and allergic conditions.
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Can other companies manufacture or sell compounds covered by WO2010101762 today?
As WO2010101762 is an application, it does not yet grant exclusive rights. However, once patents are granted in specific countries, any commercial activity related to the patented compounds or compositions in those countries without a license would constitute infringement. A thorough freedom-to-operate analysis is required to determine current manufacturing and sales risks.
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What is the significance of the "priority date" of September 30, 2010?
The priority date is the earliest date from which novelty and inventiveness are assessed for the patent application. Any prior art published or disclosed before this date can be used to challenge the patentability of the invention. It also sets the starting point for calculating the 20-year patent term.
Citations
[1] World Intellectual Property Organization. (2011). International Application Number PCT/JP2010/066904, Publication Number WO2010/121762 A1. Retrieved from https://patents.google.com/patent/WO2010121762A1/en
