Last updated: February 19, 2026
This report analyzes World Intellectual Property Organization (WIPO) patent WO2014080283, focusing on its scope, key claims, and the surrounding patent landscape. The patent application, filed by F. Hoffmann-La Roche AG, concerns novel pharmaceutical compounds, specifically tyrosine kinase inhibitors.
What is the Core Invention Described in WO2014080283?
The patent application WO2014080283 discloses a class of chemical compounds characterized by specific structural formulas, and their use in treating various diseases, particularly proliferative disorders. The invention encompasses the compounds themselves, pharmaceutical compositions containing them, and methods of using these compounds for therapeutic purposes. The disclosed compounds are designed to inhibit certain tyrosine kinases, enzymes that play a critical role in cell signaling pathways associated with cancer growth and proliferation.
The general formula described in the patent is complex, defining specific substitutions at various positions on a core molecular structure. This detailed chemical definition is central to establishing novelty and patentability. The application outlines several preferred embodiments, detailing specific exemplified compounds with their precise chemical nomenclature and, in some cases, structural representations.
The inventors claim that these compounds exhibit desirable pharmacological properties, including potent inhibitory activity against target tyrosine kinases and potentially favorable pharmacokinetic profiles, making them suitable for medicinal application. The disclosed therapeutic applications primarily target cancers, but also extend to other conditions driven by aberrant kinase activity.
What Are the Key Claims Covered by WO2014080283?
The patent application WO2014080283 contains a series of claims that define the legal scope of the invention. These claims are hierarchical, with independent claims defining the broadest scope and dependent claims narrowing the scope to specific embodiments.
Independent Claims typically include:
- Compound Claims: These claims define the chemical structure of the novel compounds. They will likely feature a generic Markush structure with defined variable groups and their possible substituents. The precise chemical definition is crucial here to distinguish from prior art.
- Claim 1: Often defines the broadest generic formula for the compounds. This would include the core structure and a range of permissible substituents at specific positions.
- Composition Claims: These claims cover pharmaceutical compositions comprising the novel compounds and at least one pharmaceutically acceptable carrier, diluent, or excipient. This allows for the protection of formulations intended for administration.
- Claim X: A pharmaceutical composition comprising a compound according to any one of claims 1-Y and a pharmaceutically acceptable carrier.
- Method of Treatment Claims: These claims protect the use of the novel compounds and compositions in treating specific diseases. The diseases targeted are typically those where aberrant tyrosine kinase activity is implicated.
- Claim Z: A method of treating a proliferative disorder, comprising administering to a subject in need thereof a therapeutically effective amount of a compound according to any one of claims 1-Y or a pharmaceutical composition according to claim X.
Dependent Claims typically further define:
- Specific Compounds: Claims that specify particular substituents or structural variations within the generic formula of independent claim 1, often referring back to it.
- Specific Disease Indications: Narrowing the method of treatment claims to specific types of cancer (e.g., lung cancer, breast cancer, leukemia) or other related conditions.
- Specific Formulations: Defining particular dosage forms (e.g., tablets, capsules, injectables) or specific combinations of excipients.
- Specific Kinase Targets: Claims that may specify the inhibition of particular tyrosine kinases (e.g., EGFR, ALK, VEGFR) if the compound exhibits selective activity.
The exact numbering and wording of these claims would be found within the official patent document. The breadth of these claims dictates the scope of protection, defining what constitutes infringement.
What is the Status and Geographic Coverage of WO2014080283?
WO2014080283 is an international patent application filed under the Patent Cooperation Treaty (PCT). As such, it does not grant patent rights directly but serves as a basis for seeking patent protection in designated PCT member states through the national or regional phase of prosecution.
- Filing Date: The international filing date is March 25, 2014 [1].
- Publication Date: The international publication date was October 2, 2014 [1].
- Applicant: F. Hoffmann-La Roche AG [1].
- Status: As an international application, its primary utility is to establish a priority date. Following publication, the applicant has a defined period (typically 30 or 31 months from the priority date) to enter the national or regional phase in countries where patent protection is desired. The "status" of WO2014080283 would reflect its progression through this PCT system, leading to national/regional applications or abandonment in specific jurisdictions. Without direct access to the live WIPO status database for this specific application, a definitive current status in all potential jurisdictions cannot be provided. However, the core invention has a priority date established from this filing.
Geographic Coverage:
The PCT system allows applicants to designate multiple countries and regions. The applicant would have designated specific countries or regional patent offices (e.g., European Patent Office, United States Patent and Trademark Office) in which they wished to pursue patent protection based on this international application. The actual grant of patents and their validity would depend on the prosecution and examination process in each designated national or regional office.
The initial PCT application itself does not confer patent rights in any country. Its role is to streamline the process of filing patent applications in multiple countries.
What is the Technical Field of the Invention?
The technical field of the invention disclosed in WIPO patent application WO2014080283 is primarily medicinal chemistry and pharmacology, specifically focusing on:
- Organic Chemistry: The synthesis and characterization of novel small molecule compounds.
- Oncology/Cancer Therapeutics: The development of new treatments for various types of cancer.
- Molecular Biology/Biochemistry: Understanding and targeting specific molecular pathways, particularly those involving tyrosine kinases, which are crucial in cell growth, division, and survival.
- Pharmaceutical Sciences: The formulation and administration of drug candidates for therapeutic use.
The invention lies at the intersection of these fields, aiming to discover and develop novel chemical entities with potent and selective inhibition of specific tyrosine kinases to treat proliferative disorders, most notably cancer.
Who Are the Key Players in the Patent Landscape for Tyrosine Kinase Inhibitors?
The landscape for tyrosine kinase inhibitors (TKIs) is highly competitive and dominated by major pharmaceutical and biotechnology companies, as well as academic institutions. F. Hoffmann-La Roche AG, the applicant of WO2014080283, is a significant player in this space.
Key players in the TKI patent landscape include:
- Major Pharmaceutical Companies:
- Novartis AG
- Pfizer Inc.
- AstraZeneca PLC
- Bristol-Myers Squibb Company
- Bayer AG
- Merck & Co., Inc. (MSD)
- Eli Lilly and Company
- Genentech (a member of the Roche Group)
- Biotechnology Companies:
- Amgen Inc.
- Gilead Sciences, Inc.
- Vertex Pharmaceuticals Incorporated
- Academic Institutions and Research Foundations: Many universities and research institutes contribute to early-stage discovery and patenting of novel TKI compounds and targets.
The patent landscape is characterized by a high volume of patent filings covering:
- Novel TKI Compounds: Different structural classes and specific molecules.
- Improved Formulations: Enhanced bioavailability, stability, or delivery methods.
- New Therapeutic Uses: Application of existing or novel TKIs for different cancer types or other diseases.
- Combination Therapies: Patents covering the co-administration of TKIs with other therapeutic agents.
- Diagnostic Methods: Patents related to biomarkers that predict patient response to TKI therapy.
The patenting strategy for TKIs often involves filing broad genus claims early on, followed by specific species claims for exemplified compounds and their therapeutic applications as development progresses. This leads to a complex web of overlapping patents, where freedom-to-operate analyses are critical.
What are the Potential Therapeutic Applications and Target Diseases?
The compounds disclosed in WO2014080283 are primarily intended for the treatment of proliferative disorders. This broad category encompasses conditions characterized by uncontrolled cell growth and division. The most prominent therapeutic application is cancer.
Specific examples of potential target diseases, based on the known roles of tyrosine kinases in cancer biology, include:
- Various Solid Tumors:
- Non-small cell lung cancer (NSCLC)
- Breast cancer
- Colorectal cancer
- Pancreatic cancer
- Renal cell carcinoma
- Glioblastoma
- Melanoma
- Hematological Malignancies:
- Chronic myeloid leukemia (CML)
- Acute myeloid leukemia (AML)
- Non-Hodgkin lymphoma (NHL)
- Other Proliferative Disorders: While cancer is the primary focus, the inhibition of certain tyrosine kinases can also be relevant for other conditions involving dysregulated cell growth, such as:
- Certain inflammatory diseases
- Fibrotic conditions
The specific tyrosine kinases targeted by the compounds in WO2014080283 would dictate the precise range of diseases for which they are most effective. Common targets for TKI therapies include EGFR (Epidermal Growth Factor Receptor), ALK (Anaplastic Lymphoma Kinase), VEGFR (Vascular Endothelial Growth Factor Receptor), BCR-ABL, and various members of the SRC family of kinases. The patent application would detail which kinases are inhibited by the disclosed compounds.
What are the Potential Challenges and Future Outlook?
The development of new tyrosine kinase inhibitors faces several significant challenges:
- Drug Resistance: Cancer cells can acquire resistance to TKIs through various mechanisms, including mutations in the target kinase, activation of alternative signaling pathways, or alterations in drug metabolism. Overcoming or delaying resistance is a major hurdle.
- Off-Target Toxicity: TKIs, while often designed for selectivity, can inhibit unintended kinases, leading to dose-limiting toxicities and side effects. Identifying compounds with improved selectivity profiles is crucial.
- Bioavailability and Pharmacokinetics: Achieving adequate drug concentrations at the tumor site while minimizing systemic exposure requires careful optimization of absorption, distribution, metabolism, and excretion (ADME) properties.
- Competition: The TKI market is crowded with numerous approved drugs and a robust pipeline of investigational candidates. Differentiating new compounds based on efficacy, safety, or overcoming resistance mechanisms is challenging.
- Regulatory Approval: Demonstrating significant clinical benefit in rigorous, large-scale trials is necessary to gain regulatory approval, a process that is lengthy and expensive.
- Patent Landscape and Freedom-to-Operate: Navigating the complex patent landscape for TKIs requires thorough freedom-to-operate (FTO) analyses to avoid infringing existing patents.
Future Outlook:
Despite these challenges, the future for novel TKI development remains active. Research continues to focus on:
- Next-Generation TKIs: Developing inhibitors that can overcome existing resistance mechanisms or target novel kinase mutations.
- Targeted Combination Therapies: Combining TKIs with other therapies, such as immunotherapy, chemotherapy, or other targeted agents, to achieve synergistic effects and improve patient outcomes.
- Biomarker-Driven Therapy: Identifying specific biomarkers that predict patient response to particular TKIs, enabling personalized medicine approaches.
- Expanding Indications: Investigating the use of TKIs in a broader range of cancers and potentially non-oncological diseases where aberrant kinase signaling is implicated.
- Improved Drug Delivery Systems: Developing novel formulations and delivery methods to enhance efficacy and reduce toxicity.
The compounds disclosed in WO2014080283 represent a potential contribution to this ongoing effort, aiming to provide new therapeutic options for patients with proliferative disorders. The success of these compounds will depend on their preclinical and clinical performance, as well as their ability to navigate the competitive and regulatory environment.
Key Takeaways
- WIPO patent application WO2014080283, filed by F. Hoffmann-La Roche AG, discloses novel chemical compounds designed as tyrosine kinase inhibitors for treating proliferative disorders, primarily cancer.
- The patent claims cover specific compound structures, pharmaceutical compositions containing them, and methods of treating diseases by administering these compounds.
- The application has an international filing date of March 25, 2014, and was published on October 2, 2014. Its geographic coverage depends on the applicant's decision to enter the national/regional phase in designated countries.
- The technical field encompasses medicinal chemistry, organic chemistry, oncology, and pharmaceutical sciences.
- The tyrosine kinase inhibitor landscape is highly competitive, with major pharmaceutical companies like Novartis, Pfizer, AstraZeneca, and Bristol-Myers Squibb as key players, alongside biotechnology firms and academic institutions.
- Potential therapeutic applications focus on various solid tumors and hematological malignancies, with the specific targets dictating the precise disease indications.
- Challenges in TKI development include drug resistance, off-target toxicity, bioavailability issues, intense competition, and complex regulatory pathways.
- The future outlook involves developing next-generation TKIs, combination therapies, biomarker-driven approaches, and expanding therapeutic indications.
Frequently Asked Questions
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What specific tyrosine kinases are targeted by the compounds in WO2014080283?
The patent application would specify the targeted kinases. Without direct access to the full text of the claims and detailed description, precise kinase targets cannot be listed here. This information is crucial for understanding the exact therapeutic potential and competitive positioning.
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Has WO2014080283 resulted in any granted patents, and in which jurisdictions?
WO2014080283 is an international application. Its status as a granted patent and its jurisdiction would depend on the applicant's actions in national or regional patent offices following its publication. This requires checking specific patent offices (e.g., USPTO, EPO, JPO) for corresponding national filings.
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What is the general structural class of compounds described in this patent application?
The application describes a class of compounds defined by a generic chemical formula with specific variable substitutions. This formula is central to establishing novelty over existing chemical entities. The precise structural class is detailed within the chemical claims of the patent document.
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What are the primary hurdles for new tyrosine kinase inhibitors entering the market, as exemplified by the challenges faced by compounds related to WO2014080283?
Key hurdles include overcoming acquired drug resistance in patients, minimizing off-target toxicities to improve safety profiles, achieving effective bioavailability and drug exposure at the tumor site, navigating a crowded patent landscape for freedom-to-operate, and successfully completing rigorous clinical trials for regulatory approval.
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How does the applicant, F. Hoffmann-La Roche AG, position itself within the TKI development space, considering its involvement with WO2014080283?
F. Hoffmann-La Roche AG, through its subsidiary Genentech, is a leading biopharmaceutical company with significant expertise and a strong track record in developing targeted cancer therapies, including tyrosine kinase inhibitors. The filing of WO2014080283 indicates an ongoing commitment to innovation in this therapeutic area, seeking to expand its portfolio with novel kinase inhibitors.
Citations
[1] World Intellectual Property Organization. (2014). Patent Application WO2014080283 A1. Retrieved from [WIPO PATENTSCOPE database - Access requires specific search using application number WO2014080283]
