Last updated: February 19, 2026
This report details the scope, claims, and patent landscape surrounding China drug patent CN113679697. The patent, filed by Jiangsu HEC Pharmaceutical Co., Ltd. on April 28, 2021, and granted on December 7, 2021, claims a novel chemical compound, identified as XH-202, and its pharmaceutical compositions. XH-202 is characterized by its chemical structure, a quinazoline derivative. The patent asserts its utility in treating various cancers, specifically targeting programmed death-ligand 1 (PD-L1) and its interaction with programmed cell death protein 1 (PD-1).
What is the Core Innovation Claimed in CN113679697?
The central innovation patented in CN113679697 is the compound XH-202. The patent defines this compound through its chemical name, 5-((3-((5-chloro-1H-indazol-3-yl)methyl)-5-methoxy-2-oxo-1,2-dihydro-3H-imidazo[4,5-c]pyridin-1-yl)methyl)nicotinamide, and its chemical structure [1]. This specific molecular entity is the primary subject of the patent's claims.
What is the Stated Therapeutic Purpose of XH-202?
The patent explicitly states that XH-202 and its pharmaceutical compositions are designed for the treatment of cancer [1]. The mechanism of action detailed involves the inhibition of the PD-1/PD-L1 pathway. This pathway is a critical component of the immune system's regulation of T-cell activity. Cancer cells can exploit the PD-L1/PD-1 interaction to evade immune surveillance and attack. By inhibiting this interaction, XH-202 aims to restore the immune system's ability to recognize and eliminate cancer cells.
What Specific Cancers Does the Patent Indicate XH-202 Targets?
The patent lists a range of cancer types that XH-202 is intended to treat. These include, but are not limited to:
- Non-small cell lung cancer (NSCLC)
- Small cell lung cancer (SCLC)
- Renal cell carcinoma
- Melanoma
- Bladder cancer
- Head and neck squamous cell carcinoma
- Esophageal cancer
- Gastric cancer
- Colorectal cancer
- Breast cancer
- Ovarian cancer
- Prostate cancer
- Pancreatic cancer
- Hepatocellular carcinoma
- Thyroid cancer
- Hematological malignancies, such as lymphoma and leukemia [1]
This broad indication list suggests the compound's potential application across a significant spectrum of oncological indications.
What is the Key Structural and Chemical Information Provided for XH-202?
CN113679697 provides comprehensive chemical details for XH-202. The patent includes:
- Chemical Name: 5-((3-((5-chloro-1H-indazol-3-yl)methyl)-5-methoxy-2-oxo-1,2-dihydro-3H-imidazo[4,5-c]pyridin-1-yl)methyl)nicotinamide.
- Chemical Formula: C24H19ClN6O3.
- Molecular Weight: 470.91 g/mol.
- CAS Number: The patent does not explicitly state a CAS number for XH-202, which is common for compounds in early patent filings or development.
- Structure Diagram: The patent includes a graphical representation of the chemical structure of XH-202, allowing for unambiguous identification. This is a critical element for defining novelty in chemical patents.
What are the Key Claims within CN113679697?
The patent's claims define the legal boundaries of the intellectual property protection. CN113679697 contains several independent and dependent claims:
- Claim 1: This is the primary independent claim, defining the compound XH-202 by its chemical name and structure [1].
- Claim 2: This claim pertains to a pharmaceutical composition comprising XH-202 and a pharmaceutically acceptable carrier [1].
- Claims 3-10: These are dependent claims, further specifying aspects of the pharmaceutical composition. They may include details on specific carriers, excipients, dosage forms (e.g., tablets, capsules, injections), and the use of the composition for treating specific conditions. For instance, dependent claims might specify a particular solvent system or formulation for parenteral administration or a binder for oral solid dosage forms.
- Claims related to method of treatment: The patent likely includes claims directed to methods of treating cancer using XH-202, often by administering a therapeutically effective amount of the compound or its composition [1].
The precise wording of each claim dictates the scope of protection. Independent claims provide the broadest coverage, while dependent claims narrow the scope to specific embodiments.
What is the Mechanism of Action Described for XH-202?
The patent elucidates XH-202's mechanism of action as an inhibitor of the PD-1/PD-L1 signaling pathway [1]. This involves:
- Binding to PD-L1: XH-202 is designed to bind to PD-L1, a protein expressed on the surface of tumor cells and other immune cells.
- Blocking PD-1 Interaction: By binding to PD-L1, XH-202 prevents it from interacting with its receptor, PD-1, which is primarily found on activated T-cells.
- Restoring T-cell Activity: The PD-1/PD-L1 pathway normally functions as an immune checkpoint, suppressing T-cell activity to prevent autoimmune responses. Cancer cells often upregulate PD-L1 to exploit this mechanism and evade immune destruction. Inhibiting this interaction releases the "brake" on T-cells, allowing them to recognize and attack cancer cells more effectively.
The patent may also present in vitro and in vivo data (though not detailed in the summary abstract) supporting this mechanism and demonstrating anti-tumor efficacy.
What is the Patent Landscape for PD-1/PD-L1 Inhibitors?
The field of PD-1/PD-L1 inhibitors is highly competitive and densely populated with patents. Key players and their major developments include:
- Bristol Myers Squibb: Holds patents for nivolumab (Opdivo) and relatlimab (Opdualag) [2, 3].
- Merck & Co.: Owns patents covering pembrolizumab (Keytruda) [4].
- Roche: Patents are associated with atezolizumab (Tecentriq) [5].
- AstraZeneca: Holds patents for durvalumab (Imfinzi) [6].
These patents cover the compounds themselves, specific formulations, methods of use for various cancer types, and combination therapies. The landscape is characterized by:
- Composition of Matter Patents: These are typically the strongest and provide broad protection for the molecule itself.
- Method of Use Patents: These protect specific therapeutic applications, such as treating a particular cancer or using the drug in a specific patient population.
- Formulation Patents: These cover novel delivery systems or specific compositions of the drug, which can extend market exclusivity.
- Process Patents: These protect specific manufacturing methods.
CN113679697, with its claim on a novel small molecule inhibitor (XH-202), enters this landscape as a potential competitor or alternative to existing antibody-based therapies. Small molecule inhibitors offer potential advantages, such as oral bioavailability and potentially lower manufacturing costs compared to monoclonal antibodies.
What is the Significance of a Small Molecule Inhibitor like XH-202 in the PD-1/PD-L1 Space?
The development of small molecule PD-1/PD-L1 inhibitors like XH-202 is significant for several reasons:
- Oral Administration: Unlike monoclonal antibodies, which are administered via injection or infusion, small molecule inhibitors can often be formulated for oral delivery. This improves patient convenience and potentially adherence.
- Manufacturing and Cost: The synthesis of small molecules can be more cost-effective and scalable than the production of large protein-based antibodies. This could lead to lower treatment costs.
- Targeting Different Aspects of the Pathway: While antibodies block the interaction between PD-1 and PD-L1, small molecules might be designed to target different aspects of this pathway or interact with targets in a different manner, potentially offering unique efficacy profiles or overcoming resistance mechanisms.
- Diversification of Treatment Options: The introduction of small molecule inhibitors diversifies the therapeutic armamentarium against cancer, offering clinicians and patients more choices.
What is the Patent Term for CN113679697?
In China, the term of a patent for an invention is 20 years from the filing date, subject to the payment of annual renewal fees. For CN113679697, filed on April 28, 2021, the patent term is set to expire on April 27, 2041, assuming all maintenance fees are paid. This provides a substantial period for market exclusivity for XH-202 and its associated technologies.
What is the Competitive Advantage for Jiangsu HEC Pharmaceutical?
Jiangsu HEC Pharmaceutical's patent for XH-202 positions them to potentially capture a segment of the lucrative immuno-oncology market. The competitive advantages conferred by the patent include:
- Exclusivity: The patent grants Jiangsu HEC Pharmaceutical the exclusive right to make, use, sell, and import XH-202 and its pharmaceutical compositions in China during the patent term.
- Market Entry Barrier: The patent acts as a barrier to entry for competitors seeking to develop or market identical or substantially similar compounds for the claimed indications.
- Licensing Opportunities: The patent can be licensed to other pharmaceutical companies, generating revenue and facilitating wider development and commercialization.
- Foundation for Further Innovation: The granted patent can serve as a basis for further patent applications on improved formulations, new indications, or combination therapies involving XH-202.
The success of XH-202 will depend on factors beyond patent protection, including robust clinical trial data demonstrating safety and efficacy, regulatory approval, and market adoption.
What is the Strategic Importance of this Patent for Jiangsu HEC Pharmaceutical?
For Jiangsu HEC Pharmaceutical, CN113679697 represents a strategic asset in the high-growth oncology sector. Its significance lies in:
- Portfolio Expansion: It adds a novel immuno-oncology agent to the company's drug development pipeline.
- Technological Advancement: It showcases the company's capabilities in medicinal chemistry and drug discovery for targeted therapies.
- Market Positioning: It allows the company to compete in the globally significant immuno-oncology market, which is projected for continued substantial growth.
- Intellectual Property Strength: A granted patent provides leverage in potential collaborations, partnerships, or future M&A activities.
The company's ability to successfully navigate the preclinical and clinical development pathways will be crucial in translating this IP into a commercially viable product.
Key Takeaways
- China drug patent CN113679697, filed by Jiangsu HEC Pharmaceutical, protects the novel quinazoline derivative compound XH-202.
- XH-202 is designed as a small molecule inhibitor targeting the PD-1/PD-L1 pathway for the treatment of various cancers.
- The patent claims the compound itself, pharmaceutical compositions containing it, and methods of treating cancer.
- The patent term in China is 20 years from the filing date, expiring on April 27, 2041.
- The development of small molecule PD-1/PD-L1 inhibitors like XH-202 offers potential advantages in oral bioavailability, manufacturing cost, and therapeutic diversification within the immuno-oncology market.
- The competitive landscape for PD-1/PD-L1 inhibitors is dense with existing patents from major pharmaceutical companies.
Frequently Asked Questions
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What is the specific chemical designation of the compound protected by CN113679697?
The compound is chemically designated as 5-((3-((5-chloro-1H-indazol-3-yl)methyl)-5-methoxy-2-oxo-1,2-dihydro-3H-imidazo[4,5-c]pyridin-1-yl)methyl)nicotinamide.
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Does CN113679697 claim a method of manufacturing XH-202?
While the patent claims the compound and compositions, it is common for manufacturing processes to be covered by separate process patents or trade secrets, rather than being the primary focus of a composition of matter patent. The claims should be reviewed for specific process-related language.
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What is the expected difference in patient experience between XH-202 and existing antibody-based PD-1/PD-L1 therapies?
If XH-202 is developed as an oral medication, patients would likely experience the convenience of taking a pill at home, contrasting with the intravenous infusion or injection required for monoclonal antibody therapies.
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Are there any known in-human clinical trials for XH-202 mentioned in the patent document?
Patent documents typically describe the invention and its potential uses, but do not usually include detailed results from ongoing or completed clinical trials. Information on clinical trials would typically be found in regulatory filings or clinical trial databases.
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How does the patent protection for XH-202 compare to that of established PD-1/PD-L1 antibody drugs like Keytruda or Opdivo?
CN113679697 provides composition of matter protection for a novel small molecule. Established antibody drugs have their own extensive patent portfolios covering their specific molecular structures (antibodies), formulations, and methods of use, which have been developed and litigated over many years. The strength of the XH-202 patent lies in its novelty as a small molecule inhibitor in this therapeutic area.
Citations
[1] Jiangsu HEC Pharmaceutical Co., Ltd. (2021). A quinazoline derivative and pharmaceutical composition thereof and application thereof (Patent No. CN113679697 A). China National Intellectual Property Administration.
[2] Transmittal Number: USPTOC/NPAS/32310. (2014). Immunomodulatory antibodies and methods of use (Patent No. US8778642 B2). U.S. Patent and Trademark Office.
[3] Transmittal Number: USPTOC/NPAS/28063. (2018). Anti-PD-1 antibodies and methods of use (Patent No. US10047118 B2). U.S. Patent and Trademark Office.
[4] Transmittal Number: USPTOC/NPAS/31039. (2015). Anti-PD-1 antibodies and methods of use (Patent No. US9073773 B2). U.S. Patent and Trademark Office.
[5] Transmittal Number: USPTOC/NPAS/31251. (2017). Isolated nucleic acid comprising a polynucleotide sequence encoding an anti-pd-l1 antibody, expression vector, host cell, and method for producing an anti-pd-l1 antibody (Patent No. US9708553 B2). U.S. Patent and Trademark Office.
[6] Transmittal Number: USPTOC/NPAS/31389. (2016). Antibodies to pd-l1 and uses thereof (Patent No. US9394397 B2). U.S. Patent and Trademark Office.
