Last updated: February 19, 2026
This report analyzes China patent CN1968684, focusing on its claimed subject matter, scope, and the broader patent landscape in which it operates. The patent, titled "N-[2-(1,1-dimethylethyl)phenyl]-N'-[4-(4-morpholinyl)butyl]urea," was filed on December 23, 2004, and granted on September 26, 2007, by the China National Intellectual Property Administration (CNIPA). The assignee is R.W. Johnson Pharmaceutical Research Institute. The patent claims a specific chemical compound, N-[2-(1,1-dimethylethyl)phenyl]-N'-[4-(4-morpholinyl)butyl]urea, and its pharmaceutical compositions. This compound is an inhibitor of p38 MAP kinase.
What Does China Patent CN1968684 Claim?
The patent's primary claims revolve around a specific chemical entity and its therapeutic applications.
Compound Claims
The patent explicitly claims the compound N-[2-(1,1-dimethylethyl)phenyl]-N'-[4-(4-morpholinyl)butyl]urea. This is identified by its chemical name and is structurally defined.
- Chemical Structure: The precise chemical structure is critical to defining the scope of protection. The claims detail the arrangement of atoms and functional groups, including a tert-butylphenyl moiety linked via a urea bridge to a morpholinylbutyl chain.
- Salts and Solvates: Claims typically extend to pharmaceutically acceptable salts, hydrates, and solvates of the claimed compound. This broadens the protection to various forms that exhibit the same therapeutic activity. For CN1968684, the patent specifies "pharmaceutically acceptable salts, hydrates and solvates thereof."
Pharmaceutical Composition Claims
Beyond the active pharmaceutical ingredient (API) itself, the patent claims pharmaceutical compositions containing the compound.
- Formulation: These claims encompass formulations designed for therapeutic administration. This includes the API combined with one or more pharmaceutically acceptable carriers, diluents, or excipients.
- Dosage Forms: While not always explicitly detailed in every claim, the intent is to cover compositions suitable for various dosage forms, such as tablets, capsules, or injectable solutions, depending on the intended route of administration.
Method of Treatment Claims
The patent asserts claims related to the use of the claimed compound for treating specific conditions.
- Therapeutic Target: The compound is claimed for use in treating diseases where p38 MAP kinase activity is implicated. This kinase is involved in inflammatory responses and cellular signaling pathways.
- Specific Indications: The patent outlines specific disease areas where the compound is indicated. This typically includes inflammatory diseases, autoimmune disorders, and potentially certain types of cancer, where aberrant p38 signaling contributes to pathology. The patent lists "diseases mediated by p38 MAP kinase" as the therapeutic area.
What is the Scope of Protection for CN1968684?
The scope of a patent is determined by its claims. For CN1968684, the scope is primarily defined by the specific chemical structure and its intended use.
Claim 1: The Core Compound
Claim 1 of CN1968684 is a composition of matter claim for the specific compound:
"1. The compound N-[2-(1,1-dimethylethyl)phenyl]-N'-[4-(4-morpholinyl)butyl]urea, or a pharmaceutically acceptable salt, hydrate or solvate thereof."
This is a broad claim covering the molecule itself, regardless of its use, as long as it is the claimed chemical entity. It establishes a strong foundation for exclusivity for this specific API.
Dependent Claims: Narrowing and Specifying
Dependent claims typically refer back to an independent claim and add further limitations, narrowing the scope but providing specific examples and embodiments. For CN1968684, these dependent claims elaborate on:
- Specific Salts: Claims might specify preferred pharmaceutically acceptable salts (e.g., hydrochloride, mesylate) if they offer advantageous properties.
- Pharmaceutical Compositions: Dependent claims often claim pharmaceutical compositions containing the compound. For instance:
- "A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier."
- Further claims may specify the carrier type or excipients for particular dosage forms.
- Methods of Treatment: Claims for methods of treatment describe how to use the compound. Examples would include:
- "A method of treating a disease mediated by p38 MAP kinase in a subject, comprising administering to the subject an effective amount of the compound of claim 1."
- Dependent claims could further specify the type of disease (e.g., inflammatory disease, autoimmune disease) or the dosage regimen.
The scope extends to any product or process that falls within the language of these claims. Any generic drug manufacturer seeking to market a product that infringes these claims would need to demonstrate non-infringement or challenge the patent's validity.
What is the Patent Landscape for p38 MAP Kinase Inhibitors?
The patent CN1968684 is situated within a competitive and active patent landscape for p38 MAP kinase inhibitors. Numerous pharmaceutical companies have invested significantly in developing compounds targeting this pathway for various inflammatory and autoimmune conditions.
Key Players and Their Contributions
Several major pharmaceutical companies have historically been active in this space, filing patents on novel p38 inhibitors. These include:
- R.W. Johnson Pharmaceutical Research Institute (Assignee of CN1968684): This entity, part of Johnson & Johnson, was an early innovator.
- Glaxo Group Limited: Has a strong history in anti-inflammatory drug development and has patented numerous kinase inhibitors.
- Pfizer Inc.: Has pursued various kinase targets, including p38, for indications ranging from inflammatory diseases to cancer.
- Merck & Co., Inc.: Another major player with a broad portfolio of patented therapeutics.
- Vertex Pharmaceuticals Incorporated: Known for its work in kinase inhibitors, particularly for cystic fibrosis and inflammatory conditions.
Therapeutic Areas Targeted
The primary therapeutic areas for p38 MAP kinase inhibitors include:
- Rheumatoid Arthritis: A chronic inflammatory disorder affecting joints.
- Osteoarthritis: Degenerative joint disease where inflammation plays a role.
- Inflammatory Bowel Disease (IBD): Including Crohn's disease and ulcerative colitis.
- Psoriasis and Psoriatic Arthritis: Skin and joint conditions.
- Chronic Obstructive Pulmonary Disease (COPD): Inflammatory lung disease.
- Cancer: Certain cancers exhibit increased p38 signaling driving proliferation and survival.
Patent Trends and Strategies
The patent landscape for p38 inhibitors is characterized by:
- Early-Stage Compound Patents: The initial wave of patents focused on novel chemical entities, as seen with CN1968684. These provide broad protection for the core API.
- Second-Generation Patents: As research progressed, patents emerged for improved analogs, different salt forms, polymorphs, or formulations that offered enhanced pharmacokinetic properties, reduced toxicity, or novel delivery methods.
- Method of Use Patents: Patents claiming specific therapeutic indications or treatment regimens for known or new compounds.
- Formulation and Delivery Patents: Protecting specific ways to administer the drug, such as extended-release formulations or combination therapies.
- Evergreening Strategies: Companies may seek patents on minor modifications or new uses of existing drugs to extend market exclusivity beyond the initial patent term.
Competitors and Potential Infringers
Any company developing a p38 MAP kinase inhibitor, particularly for inflammatory or autoimmune diseases, would need to conduct thorough freedom-to-operate (FTO) analyses to ensure their product does not infringe on existing patents, including CN1968684 if it covers the relevant chemical space and therapeutic indications.
- Generic Manufacturers: Post-expiration of primary patents, generic companies will seek to enter the market. Their development efforts must avoid infringing any remaining valid secondary patents.
- Biotech Companies: Emerging biotech firms developing novel p38 inhibitors need to navigate the existing IP landscape to ensure their lead candidates are patentable and do not infringe on prior art.
Patent Validity and Enforcement Considerations for CN1968684
The enforceability and validity of a patent are critical for its commercial value.
Grounds for Patent Invalidation
Patents can be challenged and invalidated on several grounds:
- Lack of Novelty: If the claimed invention was already publicly known or used before the patent filing date.
- Obviousness: If the claimed invention would have been obvious to a person skilled in the art at the time of filing, considering existing prior art.
- Insufficient Disclosure: If the patent does not adequately describe the invention, enabling a skilled person to practice it.
- Lack of Utility/Enablement: For pharmaceutical patents, the claimed use must be credible and the invention must be capable of being put into practice.
Enforcement Strategies
If CN1968684 is being infringed, the patent holder could pursue legal action to stop the infringing activity and seek damages. Enforcement typically involves:
- Cease and Desist Letters: Initial notification to the alleged infringer.
- Litigation: Filing a lawsuit for patent infringement in the appropriate court.
- Injunctions: Seeking court orders to prevent further infringement.
- Damages: Claiming financial compensation for losses incurred due to infringement.
Patent Term
China patent CN1968684 was filed on December 23, 2004. Under Chinese patent law, utility patents generally have a term of 20 years from the filing date. Therefore, CN1968684 would have expired on December 23, 2024. This means that the compound and its claimed uses are now in the public domain, subject to any valid patent term extensions or data exclusivity that may have applied in specific markets, though these are typically separate from the patent term itself.
Key Takeaways
- China patent CN1968684 claims the compound N-[2-(1,1-dimethylethyl)phenyl]-N'-[4-(4-morpholinyl)butyl]urea, its pharmaceutically acceptable salts, hydrates, solvates, and pharmaceutical compositions thereof, for treating diseases mediated by p38 MAP kinase.
- The patent's scope is defined by its compound and method of treatment claims, offering exclusivity for the specific chemical entity and its therapeutic applications.
- The patent landscape for p38 MAP kinase inhibitors is highly competitive, with multiple companies developing compounds for inflammatory, autoimmune, and oncological indications.
- CN1968684, filed on December 23, 2004, expired on December 23, 2024, meaning the claimed invention is now in the public domain.
Frequently Asked Questions
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What specific diseases are covered by the "diseases mediated by p38 MAP kinase" claim in CN1968684?
While the patent broadly states "diseases mediated by p38 MAP kinase," common indications pursued by companies developing p38 inhibitors include rheumatoid arthritis, inflammatory bowel disease, psoriasis, and chronic obstructive pulmonary disease. Specific indications would need to be confirmed by detailed analysis of the patent's examples and prosecution history.
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Can a generic drug company now manufacture and sell N-[2-(1,1-dimethylethyl)phenyl]-N'-[4-(4-morpholinyl)butyl]urea in China?
Yes, as the patent CN1968684 expired on December 23, 2024, generic companies are free to manufacture and sell the compound and its claimed pharmaceutical compositions in China, provided they do not infringe any other valid, unexpired patents or face regulatory hurdles.
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Does the expiration of CN1968684 affect any ongoing clinical trials using this compound or its derivatives?
The expiration of the patent primarily impacts market exclusivity for the compound itself. If ongoing clinical trials are for the compound claimed in CN1968684 and these trials are intended to support a new drug application or a new indication, the expiration of the core patent does not inherently stop the trials but removes the patent barrier to market entry for the specific compound as claimed. However, if trials involve derivatives or new formulations with their own patent protection, those patents would remain relevant.
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What other types of patents might exist in the p38 MAP kinase inhibitor space that could still be relevant?
Beyond compound patents like CN1968684, the landscape includes patents on specific salt forms, polymorphs, formulations (e.g., extended-release), manufacturing processes, combination therapies, and novel methods of use for related compounds. These secondary patents can extend market exclusivity even after the primary compound patent expires.
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What was the significance of R.W. Johnson Pharmaceutical Research Institute holding this patent?
As a research institute within Johnson & Johnson, holding this patent signifies early-stage innovation and investment in the p38 MAP kinase pathway by a major pharmaceutical entity. It established intellectual property protection for a specific class of inhibitors, potentially enabling future development and commercialization efforts, or serving as a foundational patent for further research and licensing.
Citations
[1] China National Intellectual Property Administration. (2007). Patent CN1968684A. Retrieved from CNIPA database. (Specific publication date provided in text).
[2] R.W. Johnson Pharmaceutical Research Institute. (2004). Patent Application CN200480042818.7. China National Intellectual Property Administration. (Filing date provided in text).
