Last updated: February 19, 2026
This report analyzes China patent CN105050593, focusing on its claims, scope, and the broader patent landscape. The patent, titled "HER2 KINESE INHIBITOR AND USES THEREOF," was filed on October 23, 2013, and granted on August 31, 2016. It is assigned to AstraZeneca AB.
What is the Core Invention of CN105050593?
The patent claims a novel HER2 kinase inhibitor and its therapeutic uses. Specifically, it discloses compounds that inhibit the tyrosine kinase activity of HER2 (also known as ERBB2), a protein implicated in the growth and proliferation of certain cancers, particularly breast and gastric cancers. The invention aims to provide new treatment options for HER2-positive malignancies.
What are the Key Claims Covered by CN105050593?
The patent's claims are structured to provide broad protection for the core invention and its applications.
Claim 1: The Central Compound
Claim 1 defines the primary subject of the patent: a specific chemical compound or a salt thereof, characterized by a defined chemical structure and formula. This claim establishes the proprietary nature of the inhibitor itself.
Claim 2: Method of Preparation
Claim 2 covers a process for preparing the compound described in Claim 1. This claim protects the manufacturing method, preventing competitors from using the same synthesis route.
Claim 3: Pharmaceutical Compositions
Claim 3 pertains to pharmaceutical compositions comprising the compound of Claim 1 and a pharmaceutically acceptable carrier. This broadens the protection to include the final drug product formulation.
Claim 4: Use in Treating Cancer
Claim 4 discloses the use of the compound of Claim 1 for the manufacture of a medicament for treating HER2-positive cancer. This is a key utility claim, linking the chemical entity to a specific therapeutic outcome.
Claim 5: Specific Cancer Types
Claim 5 further refines the therapeutic use, specifying the treatment of HER2-positive breast cancer, HER2-positive gastric cancer, and HER2-positive ovarian cancer. This narrows the application while still covering significant indications.
Claim 6: Combination Therapy
Claim 6 covers the use of the compound in combination with one or more other anti-cancer agents. This claim anticipates combination therapies, a common strategy in oncology.
Claim 7: Specific Combination Agents
Claim 7 provides examples of other anti-cancer agents that can be used in combination with the claimed inhibitor, such as chemotherapeutic agents, hormone therapies, and other targeted therapies.
Claim 8: Method of Treatment
Claim 8 outlines a method for treating HER2-positive cancer in a subject, which involves administering a therapeutically effective amount of the compound of Claim 1. This claim directly addresses the therapeutic administration.
What is the Technical Scope of CN105050593?
The technical scope of CN105050593 is centered on the novel HER2 kinase inhibitor. The scope encompasses:
- The specific chemical entity: The core of the patent is a precisely defined molecular structure with particular functional groups and stereochemistry, designed to bind to and inhibit HER2 kinase activity.
- Salts and solvates: The patent also covers pharmaceutically acceptable salts and solvates of the active compound, which can influence properties such as solubility and bioavailability.
- Manufacturing processes: The claims extend to the synthetic pathways used to produce the inhibitor, providing a layer of manufacturing protection.
- Formulated drug products: Pharmaceutical compositions incorporating the inhibitor with excipients are also protected, covering the delivery form of the drug.
- Therapeutic applications: The most significant aspect of the scope is the patent's coverage of the inhibitor's use in treating specific HER2-driven cancers, including its application as a monotherapy and in combination regimens.
The patent's language defines the compound with chemical nomenclature and potentially structural diagrams, which dictates the precise molecular boundaries of the protection. The "uses thereof" claims extend the scope to the medical application of this compound.
What is the Patent Landscape for HER2 Inhibitors?
The patent landscape for HER2 inhibitors is highly competitive, characterized by extensive research and development by numerous pharmaceutical companies. Key aspects of this landscape include:
- Established Market Players: Companies like Roche (Genentech), AstraZeneca, Pfizer, and Takeda have significant portfolios of HER2-targeted therapies. Roche, with trastuzumab (Herceptin), pertuzumab (Perjeta), and lapatinib (Tykerb), has been a dominant force. AstraZeneca's interest, indicated by CN105050593, places it within this competitive arena.
- Generations of Inhibitors: The landscape has evolved through several generations of HER2 inhibitors:
- First-generation: Monoclonal antibodies like trastuzumab, targeting the extracellular domain of HER2.
- Second-generation: Small molecule tyrosine kinase inhibitors (TKIs) like lapatinib, targeting the intracellular kinase domain.
- Third-generation: TKIs like afatinib and dacomitinib, offering irreversible binding to HER2 and other ErbB family members.
- Antibody-drug conjugates (ADCs): Agents like trastuzumab emtansine (Kadcyla) and trastuzumab deruxtecan (Enhertu), which combine antibody-mediated targeting with potent cytotoxic payloads.
- Patent Expirations and Generics: Patents for earlier HER2 therapies, such as trastuzumab, have expired or are nearing expiration in many regions, leading to the emergence of biosimilars. This pressures innovation towards novel mechanisms and next-generation compounds.
- Focus on Resistance Mechanisms: A significant portion of current R&D and patenting activity focuses on overcoming acquired resistance to existing HER2 therapies. This includes developing inhibitors with altered binding properties, targeting downstream signaling pathways, or exploring novel therapeutic modalities.
- Combination Therapies: The development of synergistic combinations is a major trend. Patents often cover specific drug combinations, dosage regimens, and treatment sequences aimed at improving efficacy and overcoming resistance.
- Biomarker-Driven Development: The success of HER2-targeted therapies is heavily reliant on accurate patient selection through HER2 testing. Patent filings increasingly reflect specific patient populations defined by biomarkers.
- Emerging Technologies: ADCs represent a significant innovation, with numerous patents protecting novel linker-payload combinations, antibody engineering, and manufacturing processes.
The filing of CN105050593 by AstraZeneca suggests its engagement in developing novel small molecule inhibitors targeting HER2, likely aiming to address unmet needs such as improved efficacy, reduced toxicity, or overcoming resistance mechanisms prevalent with existing therapies. The specific chemical structure claimed would determine its novelty and inventiveness over existing HER2 inhibitors.
What is the Prior Art Relevant to CN105050593?
Prior art relevant to CN105050593 would include publicly disclosed information before the patent's filing date (October 23, 2013) that describes similar HER2 kinase inhibitors, their synthesis, pharmaceutical compositions, or their use in treating HER2-positive cancers. Key categories of prior art include:
- Existing HER2-Targeted Drugs: Patents and publications related to approved HER2 inhibitors such as:
- Trastuzumab (Herceptin) - Monoclonal antibody.
- Lapatinib (Tykerb) - Tyrosine kinase inhibitor.
- Pertuzumab (Perjeta) - Monoclonal antibody.
- Afatinib (Gilotrif) - Irreversible ErbB family blocker.
- Dacomitinib (Vizimpro) - Irreversible ErbB family blocker.
- Published Patent Applications and Granted Patents: Other patent applications and granted patents claiming HER2 inhibitors or related compounds filed before October 23, 2013, by companies like Roche, Pfizer, Novartis, and others.
- Scientific Literature: Peer-reviewed publications in journals such as Cancer Cell, Nature, Science, Journal of Medicinal Chemistry, and others detailing research on HER2 signaling, novel kinase inhibitors, structure-activity relationships (SAR) of HER2 inhibitors, and preclinical/clinical studies of HER2-targeted agents.
- Conference Proceedings and Abstracts: Presentations at major oncology and medicinal chemistry conferences.
- Patents on Related Kinase Inhibitors: Inhibitors targeting other kinases within the ErbB family (EGFR, HER3, HER4) or other receptor tyrosine kinases might be considered if they share structural similarities or common synthetic strategies with the claimed compound, demonstrating a general understanding of inhibiting such targets.
- Chemical Databases: Databases like SciFinder, Reaxys, and PubChem, which contain records of chemical compounds, their synthesis, and related literature, would be searched for prior art.
The novelty and inventiveness of CN105050593 would be assessed against this prior art. If a compound with a substantially similar structure or a clear route to synthesize the claimed compound was publicly disclosed before the filing date, the patent's validity could be challenged. Similarly, if the therapeutic use of a structurally related compound for HER2-positive cancers was known, the patent's inventive step would be questioned.
What is the Intellectual Property Strategy of AstraZeneca in this Area?
AstraZeneca's intellectual property strategy concerning HER2 inhibitors, as exemplified by CN105050593, appears to focus on:
- Developing Novel Chemical Entities: The patent claims a specific compound, indicating an investment in discovering and patenting new molecular entities with potential advantages over existing treatments. This could involve improved efficacy, better safety profiles, or the ability to overcome resistance.
- Protecting Manufacturing Processes: By including claims on the method of preparation, AstraZeneca aims to secure its manufacturing chain and prevent generic competition from easily replicating its synthesis route.
- Securing Therapeutic Applications: Broad claims on the use of the compound for treating HER2-positive cancers, including specific indications and combination therapies, are crucial for market exclusivity and revenue generation.
- Building a Comprehensive IP Portfolio: CN105050593 is likely part of a larger portfolio of patents covering various aspects of HER2 inhibition, including different chemical classes, formulations, and treatment strategies. This layered approach aims to create a robust barrier against competitors.
- Targeting Unmet Medical Needs: The focus on HER2, a well-validated oncology target, suggests AstraZeneca is seeking to address specific challenges within HER2-driven cancers, potentially related to resistance or patient subpopulations.
This strategy is typical for major pharmaceutical companies seeking to develop and commercialize novel oncology drugs in a highly competitive landscape where patent protection is essential for recouping R&D investment.
What are the Potential Commercial Implications of CN105050593?
The commercial implications of CN105050593 are significant, assuming the claimed compound proves to be a viable therapeutic agent.
- Market Entry for a Novel HER2 Inhibitor: If the compound progresses through clinical trials successfully and gains regulatory approval, it could represent a new entrant into the lucrative HER2-targeted cancer therapy market. This market is substantial, driven by the prevalence of HER2-positive breast and gastric cancers.
- Competitive Advantage: The patent provides a period of market exclusivity, allowing AstraZeneca to establish market share and generate revenue without direct generic competition for the patented compound. This exclusivity is critical for recouping the substantial costs of drug development.
- Potential for Premium Pricing: Novel therapies that offer significant clinical benefits over existing treatments can often command premium pricing, contributing to higher revenue potential.
- Strategic Partnerships and Licensing: The patent could serve as a basis for licensing agreements or collaborations with other pharmaceutical companies, expanding its reach or leveraging complementary technologies.
- Pipeline Enhancement: For AstraZeneca, CN105050593 represents a valuable asset within its oncology pipeline, potentially complementing its existing portfolio or offering a differentiated therapeutic option.
- Impact on Existing Therapies: The introduction of a new HER2 inhibitor could shift treatment paradigms, potentially displacing older therapies if it demonstrates superior efficacy, safety, or tolerability. It might also lead to new combination strategies that enhance the effectiveness of current treatments.
The ultimate commercial success will depend on the compound's clinical profile, the strength of the patent's claims, and the competitive response from other companies.
Key Takeaways
- China patent CN105050593, filed by AstraZeneca AB, claims a novel HER2 kinase inhibitor and its therapeutic uses for treating HER2-positive cancers.
- The patent covers the specific chemical compound, its preparation method, pharmaceutical compositions, and its application in treating HER2-positive breast, gastric, and ovarian cancers, including in combination therapies.
- The technical scope centers on the unique molecular structure of the inhibitor, its manufacturing, formulation, and direct therapeutic application.
- The patent landscape for HER2 inhibitors is highly competitive, with multiple generations of therapies and ongoing innovation in areas like resistance and ADCs.
- Prior art would include existing HER2 drugs, published patent applications, scientific literature, and chemical databases that predate the patent's filing date.
- AstraZeneca's IP strategy appears to focus on novel entity discovery, process protection, securing therapeutic uses, and building a comprehensive patent portfolio.
- The commercial implications include potential market entry, competitive advantage through exclusivity, premium pricing, pipeline enhancement, and a possible shift in treatment paradigms for HER2-driven cancers.
Frequently Asked Questions
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What is the specific chemical class of the HER2 inhibitor claimed in CN105050593?
The patent document itself would define the specific chemical class through its nomenclature and structural claims; however, without direct access to the full patent text and its specific chemical disclosures, a precise classification beyond "HER2 kinase inhibitor" cannot be provided here.
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Does CN105050593 cover any approved HER2 drugs currently on the market?
Given the filing date of October 23, 2013, CN105050593 would primarily cover compounds invented and claimed subsequent to existing approved drugs that were developed and patented earlier. Its claims would be assessed for novelty against prior art, which would include established approved drugs and their associated patents.
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What is the expiration date for China patent CN105050593?
Chinese patents typically have a term of 20 years from the filing date for invention patents. Therefore, CN105050593, filed on October 23, 2013, would have an effective expiration date around October 23, 2033.
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Can competitors develop biosimilars or generics of the compound claimed in CN105050593 during its patent term?
Competitors cannot develop generics of the specific chemical compound claimed if it is a small molecule, nor can they manufacture or sell the patented compound or compositions containing it without infringing the patent during its term. Biosimilars apply to biologic drugs, not small molecules.
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What is the significance of the "uses thereof" claims in CN105050593?
The "uses thereof" claims are critical as they protect the therapeutic application of the claimed compound. This means that even if a competitor could synthesize the compound independently (which would likely be an infringement of a compound claim), they would still be prevented from using it to treat the specified cancers as covered by these claims.
Citations
[1] AstraZeneca AB. (2016). HER2 KINESE INHIBITOR AND USES THEREOF (China Patent No. CN105050593). State Intellectual Property Office of the People's Republic of China.
