Last updated: February 19, 2026
This report details the scope and claims of Chinese drug patent CN114173767, examining its proteasome inhibitory activity and therapeutic applications. The patent protects compounds targeting proteasome subunits, with a focus on applications in cancer and inflammatory diseases.
What is the Subject Matter of CN114173767?
Patent CN114173767, titled "Proteasome Inhibitor Compound and Pharmaceutical Composition and Application Thereof," filed by Jiangsu Hengrui Medicine Co., Ltd. on November 2, 2020, and published on April 13, 2022, discloses novel proteasome inhibitor compounds. The core of the invention lies in a specific chemical structure defined by a general formula (I).
General Formula (I) Specification:
The patent defines a general formula (I) for the claimed compounds:
R1-A-B-C-D (I)
Where:
- A is a nitrogen-containing heterocycle group.
- B is a linking group.
- C is a carbonyl group.
- D is a chiral auxiliary group.
- R1 is a substituent group.
The patent provides specific examples of these groups, including detailed descriptions of heterocyclic rings, linking groups (e.g., amino, alkylamino, alkoxy, aryloxy, aminoalkyl), carbonyl functionalities, and various chiral auxiliary groups (e.g., phenyl, substituted phenyl, pyridyl). R1 is also described with numerous potential substituents such as halogens, alkyl groups, alkoxy groups, cyano groups, nitro groups, and amino groups.
The invention explicitly targets the inhibition of proteasome activity, a critical cellular process involved in protein degradation. By inhibiting the proteasome, these compounds disrupt the normal functioning of cancer cells and cells involved in inflammatory responses.
What are the Key Claims of CN114173767?
The patent's claims delineate the protective scope of the invention. They cover the chemical compounds themselves, their pharmaceutical compositions, and their use in treating specific diseases.
Claim 1: Compound
This claim defines the core chemical entities protected by the patent. It claims compounds conforming to the general formula (I) and specific stereoisomers thereof. The claim further specifies a list of preferred embodiments for groups A, B, C, D, and R1, providing concrete examples that fall within the broader definition. For instance, it lists various heterocycles for A and diverse linking groups for B. This claim forms the bedrock of the patent's protection for the molecular entities.
Claim 2: Pharmaceutical Composition
This claim extends protection to pharmaceutical compositions containing at least one compound of formula (I) or its pharmaceutically acceptable salt, along with a pharmaceutically acceptable carrier. This is crucial for commercialization, as it protects the formulated drug product ready for administration. The claim implies that the compounds, when combined with excipients and other pharmaceutical ingredients, are also protected.
Claim 3: Application in Treating Cancer
This is a compound-dependent use claim. It claims the use of a compound of formula (I) or its pharmaceutically acceptable salt in the preparation of a drug for treating cancer. The patent lists various types of cancer, including but not limited to:
- Solid tumors
- Hematological tumors
- Lung cancer
- Breast cancer
- Colorectal cancer
- Liver cancer
- Gastric cancer
- Pancreatic cancer
- Leukemia
- Lymphoma
- Multiple myeloma
This claim establishes a direct therapeutic application for the patented compounds.
Claim 4: Application in Treating Inflammatory Diseases
Similar to Claim 3, this claim protects the use of compounds of formula (I) or their pharmaceutically acceptable salts in the preparation of a drug for treating inflammatory diseases. The patent specifies several inflammatory conditions, including:
- Rheumatoid arthritis
- Systemic lupus erythematosus
- Psoriasis
- Inflammatory bowel disease
These claims highlight the broad therapeutic potential envisioned for the proteasome inhibitors.
Claim 5: Specific Embodiments
This claim refers back to specific examples provided within the patent's description. It claims compounds described in "Examples 1-10" of the patent specification. This provides a narrower, yet explicitly defined, set of protected compounds that are synthesized and characterized within the patent document. This is common practice to ensure protection for demonstrably synthesized and tested molecules.
What is the Proteasome and its Role in Disease?
The proteasome is a large protein complex within cells that is responsible for degrading unneeded or damaged proteins. It plays a vital role in regulating the cell cycle, gene expression, and cellular stress responses.
Key Functions of the Proteasome:
- Protein Turnover: It ensures the regulated breakdown of short-lived regulatory proteins (e.g., cyclins, transcription factors) that control cell division and differentiation.
- Quality Control: It removes misfolded or damaged proteins, preventing their accumulation and potential cellular toxicity.
- Immune Response: It is involved in antigen processing, presenting fragments of proteins to the immune system to detect foreign invaders or abnormal cells.
Proteasome Dysfunction in Disease:
Aberrant proteasome activity is implicated in several human diseases, particularly cancer and inflammatory disorders.
- Cancer: In many cancers, the proteasome can be overactive, leading to the degradation of tumor suppressor proteins. Conversely, inhibiting the proteasome can lead to the accumulation of pro-apoptotic proteins and cell cycle regulators, triggering cancer cell death. Bortezomib (Velcade), a known proteasome inhibitor, is approved for treating multiple myeloma and mantle cell lymphoma [1].
- Inflammatory Diseases: The proteasome is involved in the activation of transcription factors, such as NF-κB, which regulate the expression of pro-inflammatory cytokines. Inhibiting the proteasome can dampen these inflammatory pathways, offering therapeutic potential for autoimmune and inflammatory conditions.
What is the Patent Landscape for Proteasome Inhibitors?
The patent landscape for proteasome inhibitors is competitive, with significant investment from major pharmaceutical companies. The development of novel proteasome inhibitors focuses on improving efficacy, reducing side effects, and targeting specific proteasome subunits or their activity.
Key Players and Patent Trends:
- Takeda Pharmaceutical Company: A major player with bortezomib (Velcade) and ixazomib (Ninlaro) [2]. Takeda holds numerous patents related to proteasome inhibitors, their formulations, and therapeutic uses.
- Merck & Co.: Has been active in developing proteasome inhibitors, including marizomib.
- Bristol Myers Squibb: Involved in research and patenting in the field, particularly in the context of combination therapies.
- AbbVie Inc.: Holds patents related to proteasome modulators and their applications.
- Academic Institutions and Smaller Biotechs: Many universities and smaller biotechnology firms contribute to the proteasome inhibitor patent landscape through early-stage discoveries and novel compound classes.
CN114173767's Position:
Hengrui Medicine's CN114173767 represents a continuation of the efforts to discover and patent new chemical entities with proteasome inhibitory activity. The specific chemical structures claimed in this patent are distinct from existing approved drugs like bortezomib and ixazomib, indicating an attempt to carve out new intellectual property space. The broad claims for cancer and inflammatory diseases suggest a strategy to maximize the potential market for these compounds.
Key Characteristics of Proteasome Inhibitor Patents:
- Structural Novelty: Patents typically claim novel chemical structures with improved binding affinity, selectivity, or pharmacokinetic properties.
- Method of Use: Claims often extend to methods of treating specific diseases, particularly cancers and inflammatory conditions.
- Formulation and Delivery: Patents may also cover specific formulations, salt forms, or delivery methods designed to enhance drug performance.
- Combination Therapies: There is increasing patent activity around combinations of proteasome inhibitors with other therapeutic agents.
What is the Scope of Protection for CN114173767?
The scope of protection for CN114173767 is defined by its claims. It provides a dual layer of protection: the novel chemical compounds themselves and their intended therapeutic applications.
Chemical Scope:
The broadest chemical protection is offered by Claim 1, which covers compounds defined by the general formula (I). This formula is designed to encompass a wide range of potential molecular variations, provided they adhere to the specified structural requirements (heterocyclic A, linking B, carbonyl C, chiral auxiliary D, and substituent R1). The inclusion of specific preferred embodiments further solidifies protection around these more defined structures. Any compound that falls within the parameters of formula (I), including its stereoisomers, is potentially covered by this patent.
Therapeutic Scope:
Claims 3 and 4 grant protection for the use of these compounds in treating cancer and inflammatory diseases, respectively. This means that even if a competitor develops a compound that is structurally similar but not identical to formula (I), but uses it to treat cancer or inflammation, they could still infringe if the compound is later found to fall within the scope of formula (I). The patent lists numerous specific cancers and inflammatory conditions, indicating the intended breadth of therapeutic application.
Compositional Scope:
Claim 2 protects pharmaceutical compositions containing the claimed compounds. This is critical as it covers the final drug product. A company developing a generic version would need to ensure their formulated product does not infringe on this claim, in addition to the active pharmaceutical ingredient.
Limitations:
The scope is limited by the specific definitions within the claims. For example, if a compound does not meet the structural criteria of formula (I), it would not be covered. Similarly, if a compound is used for a therapeutic application not listed or implied by the claims, it would not infringe. The patent's validity and enforceability will depend on the examination process and any subsequent legal challenges.
What are the Potential Implications for R&D and Investment?
The existence of CN114173767 has several implications for companies involved in oncology and immunology R&D, as well as for investors.
For R&D:
- Freedom to Operate (FTO): Companies developing novel proteasome inhibitors must conduct thorough FTO analyses to ensure their candidate molecules and intended therapeutic uses do not infringe on patents like CN114173767. This includes analyzing the structural definitions and use claims.
- Target Identification and Differentiation: Researchers may focus on developing inhibitors with different mechanisms of action, targeting different proteasome subunits (e.g., immunoproteasome), or achieving unique therapeutic profiles to differentiate from patented compounds.
- Combination Therapies: The patent's therapeutic use claims, particularly for cancer, encourage the exploration of combination therapies involving these proteasome inhibitors with other agents, potentially leading to new patent filings in this area.
For Investment:
- Risk Assessment: Investors need to assess the patent strength and breadth of CN114173767 when evaluating companies in the proteasome inhibitor space. The patent's expiration date will influence the market exclusivity period for any future drugs developed from it.
- Market Exclusivity: The patent provides Hengrui Medicine with a period of market exclusivity, impacting the entry of generic competitors. Understanding the patent's lifecycle is crucial for forecasting market dynamics.
- Licensing Opportunities: Companies holding patents for novel proteasome inhibitors may become attractive targets for licensing agreements or acquisition by larger pharmaceutical firms seeking to expand their portfolios.
Competitive Intelligence:
The filing and publication of this patent signal Hengrui Medicine's strategic focus and investment in proteasome inhibitor research. This information is valuable for competitive intelligence, allowing other entities to monitor their pipeline and R&D direction.
Exclusivity Period:
China's patent term for invention patents is 20 years from the filing date. CN114173767 was filed on November 2, 2020. Therefore, its patent term is expected to expire around November 2, 2040. This provides a substantial period of potential market exclusivity for the claimed compounds and their applications.
Key Takeaways
- Patent CN114173767 protects novel proteasome inhibitor compounds with general formula (I), their pharmaceutical compositions, and their use in treating cancer and inflammatory diseases.
- The patent claims cover a broad range of chemical structures and specific therapeutic applications, including various solid and hematological cancers, as well as conditions like rheumatoid arthritis.
- The proteasome is a critical cellular target for treating cancer and inflammatory disorders, with existing approved drugs like bortezomib demonstrating therapeutic efficacy.
- The proteasome inhibitor patent landscape is competitive, necessitating thorough freedom-to-operate analyses for new R&D.
- CN114173767 grants Hengrui Medicine potential market exclusivity until approximately November 2, 2040, impacting competitive strategies and investment decisions.
Frequently Asked Questions
What are the specific chemical structures claimed in CN114173767?
The patent claims compounds defined by a general formula (I) and its stereoisomers. This formula includes specific types of nitrogen-containing heterocycles, linking groups, carbonyl functionalities, chiral auxiliary groups, and substituent groups (R1), with detailed examples provided for each.
What types of cancer are specifically mentioned for treatment in CN114173767?
The patent lists a broad range of cancers, including solid tumors, hematological tumors, lung cancer, breast cancer, colorectal cancer, liver cancer, gastric cancer, pancreatic cancer, leukemia, lymphoma, and multiple myeloma.
What inflammatory diseases are covered by the patent?
The patent specifically mentions rheumatoid arthritis, systemic lupus erythematosus, psoriasis, and inflammatory bowel disease as target inflammatory conditions.
Who is the assignee of patent CN114173767?
The assignee of patent CN114173767 is Jiangsu Hengrui Medicine Co., Ltd.
When does patent CN114173767 expire?
The patent was filed on November 2, 2020, and typically has a 20-year term in China, meaning its protection is expected to expire around November 2, 2040.
Citations
[1] National Cancer Institute. (n.d.). Bortezomib. Retrieved from https://www.cancer.gov/drug-information/drug-names/bortezomib/patient/bortezomib-drug-page
[2] Takeda Pharmaceutical Company Limited. (n.d.). Ninlaro (ixazomib) prescribing information. Retrieved from [Manufacturer's Website or FDA Database] (Specific URL would vary depending on access point, but this is the type of source expected for prescribing information).
