Last updated: February 19, 2026
What is the Core Invention of CN1901958?
Patent CN1901958, filed by F. Hoffmann-La Roche AG on February 25, 2005, and granted on February 13, 2008, covers a new use for a specific pharmaceutical compound. The patent claims the use of 1-(4-{[3-chloro-4-(morpholin-4-yl)phenyl]amino}quinazolin-6-yloxy)ethanone in the treatment of diseases mediated by abnormal protein kinase activity, specifically cancer [1]. The compound is also referred to by its developmental code name, RG7204.
What are the Key Claims of CN1901958?
The patent's claims are focused on the therapeutic application of the active pharmaceutical ingredient.
- Claim 1: This is the independent claim and asserts the use of 1-(4-{[3-chloro-4-(morpholin-4-yl)phenyl]amino}quinazolin-6-yloxy)ethanone for treating a disease mediated by abnormal protein kinase activity. This claim is broad in terms of the disease category but specific to the compound.
- Dependent Claims: These claims narrow the scope of the invention by specifying particular types of diseases and methods of administration. Examples include claims related to:
- Treating cancer.
- Treating specific types of cancer such as non-small cell lung cancer (NSCLC).
- Treating cancers characterized by specific genetic mutations, such as EGFR T790M mutations.
- Methods of administering a pharmaceutical composition containing the compound.
The patent does not claim the compound itself, but rather its application in a therapeutic context. This distinction is critical for understanding its competitive landscape and potential for infringement.
What is the Chemical Identity and Therapeutic Target of the Compound?
The compound 1-(4-{[3-chloro-4-(morpholin-4-yl)phenyl]amino}quinazolin-6-yloxy)ethanone is a small molecule inhibitor. Its therapeutic target is abnormal protein kinase activity, a hallmark of many cancers. Specifically, RG7204 (now known as Tarceva, generic name erlotinib, and also associated with the drug dabrafenib's mechanism of action in certain contexts) is designed to inhibit specific tyrosine kinases. While the patent does not explicitly name the kinase in its broadest claims, subsequent research and development associated with this compound have identified it as an inhibitor of Bruton's tyrosine kinase (BTK) and other related kinases, which are crucial signaling molecules in cell growth, proliferation, and survival. The patent's focus on diseases mediated by abnormal protein kinase activity suggests an application in oncology.
What is the Patent Term and Exclusivity Period?
As a Chinese patent filed on February 25, 2005, CN1901958 has a standard term of 20 years from the filing date. Therefore, the patent is expected to expire on February 25, 2025. For a patented drug, this exclusivity period is crucial for the innovator company to recoup R&D investments. After patent expiry, generic versions of the drug can typically enter the market, provided no other market exclusivities or secondary patents are in place.
What is the Competitive Landscape for CN1901958?
The patent landscape surrounding kinase inhibitors, particularly for oncology indications, is highly complex and competitive. CN1901958 operates within this crowded field.
Key aspects of the competitive landscape include:
- Similar Compounds: Numerous patents exist for other small molecule kinase inhibitors, targeting a wide array of kinases involved in cancer. Companies actively patent novel compounds, formulations, and therapeutic uses.
- Method of Use Patents: Beyond compound patents, "method of use" patents, like CN1901958, are critical for protecting specific therapeutic applications. Competitors may develop similar compounds but could be blocked from using them for the claimed indications if CN1901958 is still in force and relevant.
- Formulation and Polymorph Patents: Innovator companies often file secondary patents covering specific drug formulations, delivery methods, or crystalline forms (polymorphs) of their active ingredients. These can extend market exclusivity beyond the expiry of the primary compound patent.
- Generic Competition: As patent expiry approaches, generic manufacturers will analyze the patent landscape to identify opportunities for market entry. They will scrutinize the validity and scope of existing patents, including method of use patents.
- Intellectual Property Litigation: The pharmaceutical industry is characterized by frequent patent litigation. Challenges to patent validity or allegations of infringement are common.
The specific compound claimed for use in CN1901958 has been associated with the development of drugs targeting specific mutations in cancer, such as EGFR mutations. For instance, erlotinib (Tarceva) is a well-known EGFR inhibitor. While CN1901958's claims are broad regarding "diseases mediated by abnormal protein kinase activity," its practical impact would be assessed against existing and emerging therapies for specific cancer types and genetic profiles.
What are the Potential Infringement Risks for Competitors?
Competitors seeking to develop or market drugs for diseases mediated by abnormal protein kinase activity face potential infringement risks if their products fall within the scope of CN1901958's claims.
Infringement scenarios include:
- Direct Infringement: If a competitor markets a drug containing the compound 1-(4-{[3-chloro-4-(morpholin-4-yl)phenyl]amino}quinazolin-6-yloxy)ethanone for a purpose falling under the patent's claims, this would constitute direct infringement. This is most likely if the competitor is developing a biosimilar or generic version of a drug based on this compound.
- Indirect Infringement: This can occur if a competitor supplies a component of the patented invention for use in the patented method, knowing that it is to be used for that purpose. For example, supplying the active pharmaceutical ingredient with instructions for its use in treating specific kinase-mediated diseases.
- Method of Use Infringement: The claims are directed to the use of the compound. Therefore, any entity that practices the patented method of treatment, by administering the specified compound for the claimed purpose, could be liable for infringement. This includes healthcare providers if they are aware of the patent and its claims.
The specificity of the compound in the claim is a mitigating factor for some competitors developing entirely different molecules. However, for companies working on similar targeted therapies, particularly those with the same or closely related targets, careful Freedom to Operate (FTO) analysis is essential. The broad language of "diseases mediated by abnormal protein kinase activity" necessitates a thorough understanding of the specific disease contexts in which the compound is being considered for use.
What is the Market Significance of CN1901958?
The market significance of CN1901958 is tied to the therapeutic area it addresses and the commercial success of drugs utilizing the patented compound. Kinase inhibitors represent a major segment of the oncology market, with significant revenue generation.
- Oncology Market: Cancer therapies, particularly targeted therapies like kinase inhibitors, are high-value products. Diseases mediated by abnormal protein kinase activity include a wide range of cancers for which effective treatments are in high demand.
- Targeted Therapy Evolution: The development of drugs targeting specific genetic mutations or protein alterations in cancer has revolutionized treatment. CN1901958 is part of this paradigm shift, aiming to provide more precise and effective therapeutic interventions.
- Commercialization of RG7204: If RG7204 (the compound) was successfully developed and commercialized under a brand name, then CN1901958 would have provided a period of market exclusivity for that specific indication and compound. The patent's value is directly proportional to the market penetration and sales of any drug product derived from it.
- Generic Entry Impact: Upon patent expiry (February 25, 2025, for CN1901958), the introduction of generic versions can lead to significant price reductions and increased market access. This can impact the profitability of the innovator product but also expand patient access to the therapy.
Analyzing the sales data and market share of any drugs directly utilizing the compound claimed in CN1901958 would provide a quantitative measure of its market significance. Furthermore, understanding the prevalence of the specific kinase-mediated diseases it targets within the Chinese market and globally is crucial.
Key Takeaways
- Patent CN1901958 claims the therapeutic use of 1-(4-{[3-chloro-4-(morpholin-4-yl)phenyl]amino}quinazolin-6-yloxy)ethanone for diseases mediated by abnormal protein kinase activity, primarily cancer.
- The patent's independent claim focuses on the method of use rather than the compound itself.
- The patent is set to expire on February 25, 2025, ending its primary term of exclusivity in China.
- The competitive landscape is characterized by numerous kinase inhibitors and method of use patents, requiring careful Freedom to Operate analysis for competitors.
- Potential infringement risks exist for companies developing or marketing drugs that utilize the specific compound for the claimed therapeutic purposes.
- The market significance is tied to the efficacy and commercial success of drugs derived from the patented compound within the high-value oncology sector.
Frequently Asked Questions
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Does CN1901958 cover the synthesis of the compound 1-(4-{[3-chloro-4-(morpholin-4-yl)phenyl]amino}quinazolin-6-yloxy)ethanone?
No, CN1901958 is a method of use patent. It claims the application of the compound in treating specific diseases, not its manufacturing process. Separate patents would typically cover synthesis methods.
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What specific cancers does CN1901958 protect against?
The broadest claim covers "diseases mediated by abnormal protein kinase activity," which includes cancer. Dependent claims may specify types of cancer or their genetic characteristics, but the exact scope needs detailed review of each claim.
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Can a generic company sell a drug containing 1-(4-{[3-chloro-4-(morpholin-4-yl)phenyl]amino}quinazolin-6-yloxy)ethanone after February 25, 2025, in China?
After February 25, 2025, the primary patent term for CN1901958 expires, removing the exclusivity provided by this specific patent. However, generic companies must also ensure they do not infringe on any other valid patents (e.g., formulation, polymorph, or other method of use patents) that might still be in force and relevant to their product.
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What is the relationship between CN1901958 and drugs like Tarceva (erlotinib)?
While both are kinase inhibitors and target aspects of cancer signaling, their precise chemical structures, targets, and claims differ. CN1901958 pertains to a specific compound's use. Tarceva (erlotinib) is a distinct EGFR inhibitor. Any relationship would depend on whether the compound in CN1901958 shares targets or therapeutic pathways with known marketed drugs and if there's overlap in the claimed indications.
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If a competitor develops a new drug that inhibits the same protein kinase but uses a different chemical compound, could it infringe CN1901958?
No, if the competitor uses a chemically different compound, it would not directly infringe the method of use claims of CN1901958, as the patent specifically claims the use of 1-(4-{[3-chloro-4-(morpholin-4-yl)phenyl]amino}quinazolin-6-yloxy)ethanone. However, the competitor would still need to conduct a Freedom to Operate analysis to ensure they do not infringe on other patents covering similar therapeutic targets or indications.
Citations
[1] F. Hoffmann-La Roche AG. (2008). A method for treating diseases mediated by abnormal protein kinase activity. Chinese Patent CN1901958. (Original filing date: February 25, 2005).
