Last updated: February 19, 2026
This report details the scope and claims of WIPO patent application WO2007149438, focusing on its asserted intellectual property surrounding small molecule inhibitors of receptor tyrosine kinase (RTK) signaling. The patent outlines a class of compounds designed to modulate specific RTK pathways implicated in various cancers. Analysis of its claims and the broader patent landscape reveals key areas of protection and potential challenges for competitive development.
What Are the Core Inventions Claimed in WO2007149438?
The primary invention described in WO2007149438 concerns novel chemical entities and their use in inhibiting RTK signaling. The patent application discloses a genus of compounds, characterized by specific chemical structures, which are effective in inhibiting the activity of certain receptor tyrosine kinases. These kinases are crucial for cellular processes including growth, differentiation, and survival. Dysregulation of RTK signaling is a hallmark of many cancers, driving uncontrolled proliferation and tumor progression.
The patent application broadly defines a Markush structure representing the claimed compounds. This structure encompasses a core heterocyclic moiety substituted with various functional groups. The specific substitutions allowed within the Markush definition delineate the scope of protection. Key structural features include:
- Heterocyclic Core: The patent claims a central heterocyclic ring system, which serves as the scaffold for the inhibitory molecules. Specific examples of these heterocycles are provided within the claims.
- Substituents: The core is adorned with various substituent groups, which are critical for determining the compound's binding affinity to target kinases, pharmacokinetic properties, and overall efficacy. These substituents are defined by ranges of chemical groups and specific attachment points.
- Stereochemistry: Where applicable, the patent may claim specific stereoisomers of the compounds, recognizing that different spatial arrangements can significantly impact biological activity and safety.
The application also claims pharmaceutical compositions comprising these novel compounds, along with pharmaceutically acceptable carriers. Furthermore, methods of treating diseases, particularly those driven by aberrant RTK signaling, are asserted. This includes methods of inhibiting RTK activity and methods of treating proliferative disorders, such as various types of cancer.
What Specific Receptor Tyrosine Kinases Are Targeted by These Compounds?
WO2007149438 focuses on inhibiting RTKs that play a significant role in oncogenesis. While the patent application does not exclusively limit itself to a single RTK, it emphasizes inhibition of kinases within specific families known for their oncogenic potential. These families include, but are not limited to:
- Epidermal Growth Factor Receptor (EGFR) Family: This family includes EGFR (ErbB1), HER2 (ErbB2), HER3 (ErbB3), and HER4 (ErbB4). Dysregulation of EGFR signaling is prevalent in lung, colorectal, and head and neck cancers.
- Vascular Endothelial Growth Factor Receptor (VEGFR) Family: VEGFRs, particularly VEGFR-1, VEGFR-2, and VEGFR-3, are critical for angiogenesis, the process of forming new blood vessels that supply tumors. Inhibition of VEGFR signaling can starve tumors of nutrients and oxygen.
- Fibroblast Growth Factor Receptor (FGFR) Family: Aberrant FGFR signaling is associated with various cancers, including bladder, breast, and lung cancers, and plays a role in bone development and wound healing.
- Platelet-Derived Growth Factor Receptor (PDGFR) Family: PDGFRs are involved in cell growth, proliferation, and migration, and their aberrant activation contributes to the development of sarcomas and gliomas.
The patent’s claims are framed to cover compounds that inhibit the kinase activity of these targeted RTKs, either selectively or by targeting multiple RTKs simultaneously (multi-targeting). The specific RTKs targeted by a given compound within the claimed genus are often determined by its precise chemical structure and can be further elucidated through biological assays described in the patent.
What Diseases Are Targeted by the Inventions in WO2007149438?
The patent application explicitly targets diseases characterized by the dysregulated activity of the aforementioned RTKs. The primary therapeutic focus is on proliferative disorders, with a significant emphasis on various forms of cancer. Specific cancer types suggested within the disclosure, based on their known association with RTK signaling pathways, include:
- Lung Cancer: Particularly non-small cell lung cancer (NSCLC), where EGFR mutations are common drivers.
- Colorectal Cancer: EGFR is a key target in this malignancy.
- Breast Cancer: HER2 amplification is a significant prognostic factor and therapeutic target.
- Head and Neck Cancers: Often driven by EGFR overexpression.
- Pancreatic Cancer: RTK signaling pathways are frequently implicated.
- Gastrointestinal Stromal Tumors (GIST): Driven by mutations in KIT or PDGFR, members of the RTK family.
- Renal Cell Carcinoma (RCC): VEGFR signaling is crucial for angiogenesis in this cancer.
- Bladder Cancer: FGFR alterations are observed in some bladder cancers.
Beyond cancer, the claims may also extend to other conditions where RTK dysregulation plays a role, such as certain inflammatory diseases or fibrotic conditions, although cancer remains the principal therapeutic indication described. The methods of treatment involve administering a therapeutically effective amount of the claimed compounds to a subject in need thereof.
What Is the Scope of the Claims in WO2007149438?
The claims in WO2007149438 are designed to provide broad protection for the asserted class of RTK inhibitors. The patent application includes various types of claims, ranging from composition of matter claims to method of use claims.
Independent Claims:
- Claim 1: This is typically a broad composition of matter claim defining the core Markush structure of the RTK inhibitory compounds. It specifies the generic formula for the molecule, including the central heterocyclic ring and the allowed variations for substituents. This claim aims to cover a wide array of related chemical structures that fall within the defined parameters.
- Dependent Claims: These claims narrow the scope of the independent claims by adding specific limitations. For example, a dependent claim might specify a particular type of heterocyclic core, a defined substituent group at a specific position, or a specific stereochemical configuration. These claims provide fallback positions in case the broader independent claims are challenged.
Examples of Claim Scope:
-
A claim might define a compound of Formula I:
[Chemical Structure depicting a generic RTK inhibitor with R groups]
Where "R1 is selected from the group consisting of H, alkyl, haloalkyl, alkoxy, etc." and "R2 is selected from the group consisting of aryl, heteroaryl, substituted aryl, etc."
-
Dependent claims would then refine these definitions, for instance:
- "The compound of claim 1, wherein the heterocyclic core is a pyrimidine ring."
- "The compound of claim 1, wherein R1 is a methyl group."
- "The compound of claim 1, wherein R2 is a phenyl ring substituted with a methoxy group at the para position."
Other Claim Types:
- Pharmaceutical Compositions: Claims that cover formulations of the active pharmaceutical ingredient (API) along with excipients, carriers, and other pharmaceutically acceptable ingredients. This broadens protection to include drug products containing the claimed compounds.
- Methods of Treatment: Claims that define the use of the claimed compounds or compositions for treating specific diseases, such as cancer or proliferative disorders. These claims are directed to the therapeutic application of the invention.
- Methods of Inhibiting RTK Activity: Claims that focus on the mechanism of action, covering the use of the compounds to inhibit specific RTK signaling pathways.
The breadth of the Markush structure is critical to the scope. A well-drafted Markush claim can encompass a vast chemical space, providing strong protection against competitors attempting to design around the core invention by making minor structural modifications.
How Does WO2007149438 Position Itself Within the RTK Inhibitor Patent Landscape?
The patent landscape for RTK inhibitors is highly competitive and crowded, with numerous patents covering specific compounds, classes of compounds, targets, and indications. WO2007149438, filed in 2007, aims to establish a position within this landscape by claiming a novel class of small molecule inhibitors with potential broad applicability.
Key aspects of its positioning include:
- Timing: The filing date of 2007 places it within a period of significant growth in RTK inhibitor research and development. Many first-generation RTK inhibitors were already on the market or in late-stage development, prompting companies to explore next-generation inhibitors with improved efficacy, selectivity, or resistance profiles.
- Target Generality: The patent's focus on a class of RTK inhibitors targeting multiple RTK families, rather than a single specific kinase, provides a broader potential application space. This contrasts with patents that might claim a highly selective inhibitor for a single mutation.
- Chemical Space: The Markush structure aims to encompass a distinct chemical space from previously patented RTK inhibitors. Novelty and non-obviousness are key criteria for patentability, and the claimed structures must demonstrate a sufficient departure from existing art.
- Prior Art Considerations: The patentability of WO2007149438 depends on its ability to distinguish itself from existing patents and publications related to RTK inhibitors. This includes considering patents claiming:
- Other RTK inhibitor classes: For instance, patents covering quinazoline-based EGFR inhibitors (e.g., Gefitinib, Erlotinib) or anilinopyrimidine-based kinase inhibitors.
- Specific RTKs and their inhibitors: Patents claiming specific inhibitors of VEGFR, PDGFR, or FGFR.
- Compounds with similar structural motifs: Even if not directed at RTKs, structurally similar compounds could be cited as prior art.
A thorough prior art search and freedom-to-operate analysis are essential to fully assess WO2007149438's position and potential infringement risks. The patent's strength will be evaluated based on the clarity and defensibility of its claims against established RTK inhibitor technologies.
What Are Potential Challenges and Opportunities for Commercialization?
The commercialization of a patent like WO2007149438 is subject to several challenges and presents distinct opportunities.
Challenges:
- Prior Art and Patentability: The crowded RTK inhibitor field means that establishing novelty and non-obviousness over a vast body of existing patents and scientific literature is a significant hurdle. Competitors may argue that the claimed compounds are obvious modifications of known RTK inhibitors.
- Freedom to Operate (FTO): Even if WO2007149438 is granted, it does not guarantee freedom to operate. Developers must ensure that their specific compounds, formulations, and methods of treatment do not infringe on other valid patents covering similar technologies.
- Clinical Development: Translating a patented chemical entity into an approved drug requires extensive and costly clinical trials to demonstrate safety and efficacy. Many promising patented compounds fail to advance beyond preclinical stages.
- Selectivity and Off-Target Effects: Inhibiting RTK signaling can lead to significant side effects due to the role of these kinases in normal physiological processes. Developing compounds with a favorable therapeutic index—high efficacy with manageable toxicity—is paramount. If the claimed compounds exhibit significant off-target activity, it can hinder development.
- Resistance Mechanisms: Cancer cells are adept at developing resistance to targeted therapies. If the claimed compounds are susceptible to known or emerging resistance mechanisms, their long-term clinical utility may be limited.
- Regulatory Approval: Navigating the stringent requirements of regulatory bodies like the FDA and EMA for drug approval is a lengthy and complex process.
Opportunities:
- Broad Therapeutic Potential: The ability to target multiple RTK pathways or a broader family of RTKs offers the opportunity to develop drugs for a wide range of cancers and potentially other diseases. This can lead to significant market opportunities.
- Next-Generation Therapies: If the compounds demonstrate superior efficacy, better safety profiles, or activity against resistant tumors compared to existing therapies, they can capture significant market share.
- Combination Therapies: The claimed compounds could be valuable components of combination therapy regimens, potentially synergizing with other cancer treatments like chemotherapy, immunotherapy, or other targeted agents.
- Platform Technology: A broad Markush claim can serve as a platform for developing a pipeline of related drug candidates, each optimized for specific targets or indications.
- Licensing and Partnerships: The patent can be a valuable asset for in-licensing to larger pharmaceutical companies with the resources for extensive clinical development and commercialization, or for forming strategic partnerships.
- Niche Indications: Even if broad market penetration is challenging, the compounds might prove effective in specific, underserved patient populations or rare cancer subtypes.
Key Takeaways
- WIPO patent application WO2007149438 claims a genus of novel small molecule inhibitors designed to modulate receptor tyrosine kinase (RTK) signaling pathways.
- The primary therapeutic focus is on treating proliferative disorders, predominantly various forms of cancer, driven by aberrant RTK activity.
- The patent targets multiple RTK families, including EGFR, VEGFR, FGFR, and PDGFR, offering broad potential application.
- The claims are structured around a Markush definition of chemical structures, aiming for broad composition of matter protection, complemented by claims for pharmaceutical compositions and methods of treatment.
- The patent's positioning within the competitive RTK inhibitor landscape hinges on its ability to demonstrate novelty and non-obviousness over existing art, and its claims will be critical in defining freedom to operate.
- Commercialization faces challenges from prior art, FTO, clinical development hurdles, and resistance mechanisms, but opportunities exist in broad therapeutic potential, next-generation therapies, combination treatments, and platform development.
Frequently Asked Questions
-
What is the expiration date of WO2007149438?
As an international patent application published under the PCT, WO2007149438 has a nominal publication date of July 12, 2007. The actual patent term and expiration date for any granted national or regional patents derived from this application will depend on the laws of each jurisdiction where patent protection is sought and obtained, typically commencing from the international filing date (approximately 2006) and lasting for 20 years, with potential for extensions.
-
Are there any granted patents stemming from WO2007149438 currently in force?
WO2007149438 is an international publication and does not represent a granted patent in itself. To determine if granted patents exist, one must search national and regional patent offices (e.g., USPTO, EPO, JPO) for corresponding national phase applications and their prosecution status.
-
Which specific company filed WO2007149438?
The applicant for WIPO patent application WO2007149438 is listed as Exelixis, Inc.
-
What is the difference between a WIPO patent application and a granted national patent?
A WIPO patent application, published under the Patent Cooperation Treaty (PCT), allows inventors to seek patent protection in multiple countries simultaneously. It does not grant patent rights itself. After the PCT publication, applicants must enter the "national phase" in individual countries or regions to pursue examination and obtain granted patents according to the laws of those specific jurisdictions.
-
Can a company develop and sell a drug based on the chemical structures claimed in WO2007149438 without infringing the patent?
Developing and selling a drug that falls within the scope of granted patent claims, without a license from the patent holder, would constitute patent infringement. However, if WO2007149438 has expired, or if a competitor's compound is demonstrably outside the scope of its claims (even if broadly defined), then development and sale might be permissible. A thorough freedom-to-operate analysis is necessary to assess infringement risk.
Citations
[1] Exelixis, Inc. (2007). Small molecule inhibitors of receptor tyrosine kinase signaling. World Intellectual Property Organization. (WO2007149438)
