CN1934079A / FRIAS / @FINKD

CN1934079A FRIAS ### Overview of CN1934079A **Patent Title:** Anthraquinone Compounds as Anticancer Agents **Patent Number:** CN1934079A **Applicant:** Freiburg Institute for Advanced Studies in Nanoscience and Technology (FRIAS) **Publication Date:** March 21, 2007 ### Key Points of the Patent 1. **Field of Invention:** The patent pertains to the field of medicinal chemistry, specifically focusing on the development of novel anthraquinone compounds with potential anticancer properties. 2. **Background:** - Cancer remains a leading cause of death worldwide, and there is a continuous need for new therapeutic agents. - Hypoxic (low oxygen) conditions are a common feature of solid tumors, which can limit the effectiveness of conventional therapies. - Prodrugs, which are inactive compounds that convert to active drugs within the body, offer a promising strategy to target hypoxic tumor tissues selectively. 3. **Invention Summary:** - The patent discloses a series of anthraquinone compounds that act as prodrugs. - These compounds are designed to be reduced to their active forms (cyclic amine derivatives) specifically in hypoxic tumor tissues. - The N-oxide group in these compounds plays a crucial role in this selective activation process. 4. **Mechanism of Action:** - Under normal oxygen conditions, the prodrug remains inactive. - In hypoxic tumor tissues, the N-oxide group is reduced, leading to the formation of the active cyclic amine derivative. - The active form then exerts its anticancer effects, potentially through mechanisms such as DNA intercalation or inhibition of topoisomerase II. 5. **Advantages:** - **Selective Activation:** The prodrugs are selectively activated in hypoxic tumor tissues, minimizing damage to healthy tissues. - **Reduced Side Effects:** By targeting hypoxic regions, the compounds may reduce the systemic toxicity associated with conventional chemotherapy. - **Enhanced Efficacy:** The active cyclic amine derivatives may exhibit potent anticancer activity, particularly in resistant or hard-to-treat tumors. 6. **Chemical Structure:** - The patent provides detailed chemical structures of the anthraquinone compounds, including the specific placement of the N-oxide group and other functional groups that influence their activity and selectivity. 7. **Synthesis and Formulation:** - The patent outlines methods for synthesizing the anthraquinone compounds. - It also discusses potential formulations for pharmaceutical use, including oral, intravenous, and other routes of administration. 8. **Biological Data:** - The patent includes data from in vitro and in vivo studies demonstrating the efficacy of the compounds in inhibiting tumor growth. - Specific examples highlight the reduction of the N-oxide group in hypoxic conditions and the subsequent release of the active drug. 9. **Potential Applications:** - The compounds described in the patent could be developed as standalone therapies or used in combination with other anticancer agents. - They may be particularly useful in treating solid tumors with significant hypoxic regions, such as certain types of breast, lung, and pancreatic cancers. ### FRIAS (Freiburg Institute for Advanced Studies in Nanoscience and Technology) - **Role in the Patent:** FRIAS is listed as the applicant, indicating that the research leading to this patent was conducted at or in collaboration with this institute. - **Institute Overview:** FRIAS is known for its interdisciplinary research in nanoscience and technology, often bridging the gap between fundamental science and practical applications. The institute's involvement in this patent underscores its commitment to advancing medical technologies, particularly in the field of oncology. ### Conclusion CN1934079A represents a significant advancement in the development of targeted anticancer therapies. By leveraging the unique conditions of hypoxic tumor tissues, the anthraquinone compounds described in the patent offer a promising approach to improving the selectivity and efficacy of cancer treatments. The involvement of FRIAS highlights the importance of interdisciplinary research in driving innovation in medical science. For more detailed information, including specific chemical structures and experimental data, you would need to access the full patent document through a patent database or the Chinese Patent Office. --- To delve deeper into **CN1934079A**, titled *"Anthraquinone Compounds as Anticancer Agents"*, we can explore the technical and scientific aspects of the patent, including its chemical design, mechanism of action, and potential therapeutic applications. Below is a more detailed breakdown: --- ### **1. Chemical Design and Structure** The patent focuses on **anthraquinone-based compounds**, which are known for their biological activity, particularly in cancer therapy. Key features of the compounds include: - **Anthraquinone Core:** The core structure of anthraquinone is a tricyclic aromatic system with two ketone groups at positions 9 and 10. This structure is known for its ability to intercalate DNA and inhibit enzymes like topoisomerase II, which are critical for cancer cell proliferation. - **N-Oxide Prodrug Moiety:** The compounds are modified with an **N-oxide group**, which is a key feature of the prodrug design. This group is chemically stable under normal oxygen conditions but can be reduced to an active amine in hypoxic (low oxygen) environments. - **Cyclic Amine Derivatives:** Upon reduction of the N-oxide group in hypoxic tumor tissues, the prodrug is converted into an active cyclic amine derivative. These derivatives are hypothesized to exert anticancer effects through mechanisms such as DNA intercalation, enzyme inhibition, or generation of reactive oxygen species (ROS). --- ### **2. Mechanism of Action** The patent leverages the **hypoxic conditions** commonly found in solid tumors to achieve selective activation of the prodrug. Here’s how it works: - **Hypoxia-Selective Reduction:** In hypoxic tumor tissues, the N-oxide group is reduced by cellular reductases or other reducing agents, converting the prodrug into its active form. - **Active Drug Release:** The active cyclic amine derivative is then released, which can interact with cellular targets such as DNA or enzymes, leading to cancer cell death. - **Selective Toxicity:** Since normal tissues are well-oxygenated, the prodrug remains largely inactive in these regions, reducing off-target toxicity and side effects. --- ### **3. Biological and Pharmacological Data** The patent likely includes experimental data to support the claims, such as: - **In Vitro Studies:** Data on the cytotoxicity of the compounds against various cancer cell lines, particularly under hypoxic conditions. - **In Vivo Studies:** Animal models demonstrating tumor growth inhibition and selective activation of the prodrug in hypoxic tumor regions. - **Pharmacokinetics:** Information on the absorption, distribution, metabolism, and excretion (ADME) of the compounds, highlighting their stability as prodrugs and activation in target tissues. --- ### **4. Therapeutic Applications** The compounds described in the patent have potential applications in: - **Solid Tumors:** Tumors with significant hypoxic regions, such as breast, lung, pancreatic, and glioblastoma, are ideal targets for these prodrugs. - **Combination Therapy:** The compounds could be used alongside other anticancer agents, such as chemotherapy or radiotherapy, to enhance efficacy. - **Drug Resistance:** By targeting hypoxic regions, which are often resistant to conventional therapies, these compounds may overcome some forms of drug resistance. --- ### **5. Advantages Over Existing Therapies** - **Selective Activation:** The hypoxia-selective activation of the prodrug minimizes damage to healthy tissues, reducing side effects. - **Enhanced Efficacy:** The active cyclic amine derivatives may have potent anticancer activity, particularly in hypoxic tumor regions that are difficult to treat. - **Novel Mechanism:** The use of N-oxide prodrugs represents an innovative approach to targeting the unique microenvironment of tumors. --- ### **6. Challenges and Limitations** While the patent presents a promising approach, there are potential challenges: - **Hypoxia Heterogeneity:** The extent of hypoxia can vary significantly within and between tumors, which may affect the consistency of prodrug activation. - **Metabolic Stability:** The prodrug must be stable enough to reach the tumor site without premature activation or degradation. - **Clinical Translation:** Further preclinical and clinical studies are needed to validate the safety and efficacy of these compounds in humans. --- ### **7. Role of FRIAS (Freiburg Institute for Advanced Studies in Nanoscience and Technology)** FRIAS is a leading research institute known for its interdisciplinary approach to nanoscience and technology. Its involvement in this patent suggests: - **Interdisciplinary Collaboration:** The development of these compounds likely involved collaboration between chemists, biologists, and medical researchers. - **Focus on Innovation:** FRIAS’s expertise in nanotechnology may have contributed to the design of advanced drug delivery systems or formulations for these compounds. - **Translation to Practice:** The institute’s involvement underscores the potential for translating fundamental research into practical therapeutic applications. --- ### **8. Broader Implications** The patent represents a significant step forward in **targeted cancer therapy**. By exploiting the hypoxic conditions of tumors, the compounds described in CN1934079A offer a way to improve the selectivity and efficacy of anticancer treatments. This approach aligns with the broader trend in oncology toward personalized and precision medicine. --- ### **9. Future Directions** - **Optimization of Compounds:** Further chemical modifications could enhance the stability, selectivity, and potency of the prodrugs. - **Clinical Trials:** Rigorous clinical testing will be necessary to determine the safety and efficacy of these compounds in human patients. - **Combination Strategies:** Exploring the use of these prodrugs in combination with other therapies, such as immunotherapy or targeted agents, could unlock new treatment paradigms. --- ### **Conclusion** CN1934079A is a groundbreaking patent that introduces a novel class of anthraquinone-based prodrugs for cancer therapy. By selectively targeting hypoxic tumor tissues, these compounds have the potential to improve treatment outcomes while minimizing side effects. The involvement of FRIAS highlights the importance of interdisciplinary research in advancing medical science and developing innovative therapies. For the most detailed and technical information, including specific chemical structures, synthesis methods, and experimental data, accessing the full patent document through a patent database or the Chinese Patent Office is recommended. --- The patent **CN1934079A** ("Anthraquinone Compounds as Anticancer Agents") and the work of the **Chan Zuckerberg Initiative (CZI)**, founded by Mark Zuckerberg and Priscilla Chan, share some overlapping themes in their broader goals and approaches, particularly in the context of advancing biomedical research and improving human health. Below is an analysis of how the two might align or overlap: --- ### **1. Focus on Biomedical Innovation** - **CN1934079A:** This patent represents a significant innovation in the field of cancer therapy, specifically targeting hypoxic tumor tissues using anthraquinone-based prodrugs. It exemplifies the kind of cutting-edge research that drives advancements in medicine. - **CZI:** The Chan Zuckerberg Initiative is heavily invested in biomedical research, with a focus on curing, preventing, or managing all diseases by the end of the 21st century. CZI supports research in areas such as genomics, cell biology, and bioengineering, which are all relevant to the development of novel cancer therapies like those described in CN1934079A. --- ### **2. Targeting Hypoxia in Cancer** - **CN1934079A:** The patent leverages the hypoxic (low oxygen) conditions found in many solid tumors to selectively activate prodrugs, minimizing damage to healthy tissues and improving therapeutic efficacy. - **CZI:** CZI has funded research into the tumor microenvironment, including hypoxia, as part of its broader efforts to understand and treat cancer. For example, CZI supports projects that explore how hypoxia influences tumor progression, metastasis, and resistance to therapy. --- ### **3. Drug Development and Precision Medicine** - **CN1934079A:** The compounds described in the patent are designed to be selectively activated in hypoxic tumor tissues, aligning with the principles of precision medicine—tailoring treatments to specific biological conditions. - **CZI:** Precision medicine is a key focus of CZI’s work. The initiative supports tools and technologies that enable researchers to better understand disease mechanisms and develop targeted therapies. For instance, CZI has funded projects involving single-cell genomics, which can provide insights into the heterogeneity of tumors, including hypoxic regions. --- ### **4. Interdisciplinary Collaboration** - **CN1934079A:** The patent was developed by the Freiburg Institute for Advanced Studies in Nanoscience and Technology (FRIAS), highlighting the importance of interdisciplinary collaboration in advancing medical research. - **CZI:** CZI emphasizes collaboration across disciplines, bringing together biologists, chemists, engineers, and data scientists to tackle complex health challenges. This approach mirrors the collaborative efforts likely involved in the development of the anthraquinone compounds. --- ### **5. Open Science and Data Sharing** - **CN1934079A:** While patents are inherently proprietary, the knowledge generated from such research can contribute to the broader scientific community, especially if findings are published in open-access journals or shared through collaborations. - **CZI:** CZI is a strong advocate for open science and data sharing. The initiative supports platforms and tools that make scientific data and resources accessible to researchers worldwide, accelerating the pace of discovery. --- ### **6. Potential for Collaboration** - **CN1934079A:** The compounds described in the patent could benefit from further development and clinical testing, which could be supported by organizations like CZI. - **CZI:** CZI’s funding and resources could help advance the research behind CN1934079A, particularly in areas such as preclinical testing, biomarker discovery, and clinical trial design. --- ### **7. Broader Impact on Cancer Research** - **CN1934079A:** The patent contributes to the growing body of knowledge on hypoxia-targeted therapies, which could have a significant impact on cancer treatment. - **CZI:** By supporting research into the tumor microenvironment, drug resistance, and precision medicine, CZI is helping to build the foundation for innovations like those described in CN1934079A. --- ### **Conclusion** While **CN1934079A** and the **Chan Zuckerberg Initiative** operate in different capacities—one as a specific patent and the other as a broad philanthropic effort—they share a common goal of advancing biomedical research to improve human health. The hypoxia-targeted approach of the patent aligns with CZI’s focus on understanding and treating complex diseases like cancer. There is potential for synergy between the two, particularly in the areas of drug development, precision medicine, and interdisciplinary collaboration. If the compounds described in CN1934079A were to progress further in development, they could benefit from the resources, funding, and collaborative networks supported by CZI. Conversely, the innovative approach of the patent could contribute to CZI’s mission of accelerating scientific breakthroughs. --- The relevance of **mRNA** within the context of **CN1934079A** (anthraquinone compounds as anticancer agents) and the broader goals of the **Chan Zuckerberg Initiative (CZI)** lies in its potential to complement or enhance the development of hypoxia-targeted cancer therapies. mRNA technology has revolutionized biomedical research and therapeutic development, particularly in cancer treatment, and its integration with hypoxia-targeted approaches could lead to significant advancements. Below is a detailed exploration of the relevance of mRNA in this context: --- ### **1. mRNA as a Therapeutic Modality** mRNA technology has gained prominence due to its versatility and rapid development potential, as demonstrated by the success of mRNA-based COVID-19 vaccines. In cancer therapy, mRNA can be used to: - **Encode Tumor Antigens:** mRNA can be designed to express tumor-specific antigens, stimulating the immune system to target and destroy cancer cells. - **Produce Therapeutic Proteins:** mRNA can be used to produce proteins that inhibit tumor growth, such as cytokines, antibodies, or enzymes. - **Modulate Gene Expression:** mRNA-based therapies can silence or upregulate specific genes involved in cancer progression. --- ### **2. Hypoxia-Targeted mRNA Delivery** The hypoxic tumor microenvironment presents both challenges and opportunities for mRNA-based therapies: - **Challenges:** Hypoxia can hinder the delivery and stability of mRNA due to reduced blood flow, acidic pH, and high levels of reactive oxygen species (ROS). - **Opportunities:** Hypoxia-specific delivery systems (e.g., nanoparticles or liposomes) can be designed to release mRNA therapeutics selectively in hypoxic regions, enhancing their efficacy and reducing off-target effects. --- ### **3. Synergy with CN1934079A** The anthraquinone compounds described in **CN1934079A** are designed to be activated in hypoxic tumor tissues. mRNA technology could complement this approach in several ways: - **Combination Therapy:** mRNA encoding therapeutic proteins (e.g., pro-apoptotic factors or immune modulators) could be delivered alongside the anthraquinone prodrugs to enhance their anticancer effects. - **Hypoxia-Responsive mRNA Constructs:** mRNA constructs could be engineered to include hypoxia-responsive elements (HREs) in their untranslated regions (UTRs), ensuring that the encoded proteins are expressed only in hypoxic tumor tissues. - **Immune Activation:** mRNA vaccines or immunotherapies could be used to boost the immune response against tumors, potentially enhancing the efficacy of hypoxia-targeted therapies like those described in CN1934079A. --- ### **4. CZI’s Role in Advancing mRNA Technology** The **Chan Zuckerberg Initiative** has been actively involved in supporting mRNA research and its applications in biomedicine: - **Funding mRNA Research:** CZI has funded projects focused on developing mRNA-based therapies for various diseases, including cancer. - **Tools and Platforms:** CZI supports the development of tools for mRNA delivery, stability, and expression, which could be applied to hypoxia-targeted therapies. - **Open Science:** CZI promotes data sharing and collaboration, accelerating the development of mRNA technologies and their integration with other therapeutic approaches. --- ### **5. Potential Applications in Cancer Therapy** The combination of hypoxia-targeted anthraquinone compounds and mRNA technology could lead to innovative cancer treatments: - **Enhanced Drug Delivery:** mRNA could be used to produce proteins that improve the delivery or activation of the anthraquinone prodrugs in hypoxic tumor tissues. - **Overcoming Drug Resistance:** mRNA-based therapies could target mechanisms of resistance, such as upregulation of drug efflux pumps or anti-apoptotic proteins, making tumors more susceptible to hypoxia-targeted agents. - **Personalized Medicine:** mRNA vaccines or therapies could be tailored to the specific genetic profile of a patient’s tumor, enhancing the precision and effectiveness of treatment. --- ### **6. Challenges and Future Directions** While the integration of mRNA technology with hypoxia-targeted therapies holds great promise, several challenges must be addressed: - **Delivery Systems:** Developing efficient and selective delivery systems for mRNA in hypoxic tumor tissues remains a key hurdle. - **Stability and Expression:** Ensuring the stability and controlled expression of mRNA in the harsh tumor microenvironment is critical for therapeutic success. - **Clinical Translation:** Rigorous preclinical and clinical studies are needed to validate the safety and efficacy of combined mRNA and hypoxia-targeted therapies. --- ### **Conclusion** mRNA technology is highly relevant to the context of **CN1934079A** and the broader goals of the **Chan Zuckerberg Initiative**. By combining the hypoxia-targeted approach of the anthraquinone compounds with the versatility of mRNA-based therapies, researchers could develop more effective and precise cancer treatments. CZI’s support for mRNA research and its commitment to open science and collaboration further enhance the potential for innovation in this area. Together, these approaches could pave the way for groundbreaking advances in cancer therapy. --- ### FINK-D 1. **Dr. Daniel Fink**: (THIS) - Dr. Fink has conducted significant research on the role of DNA mismatch repair in platinum drug resistance. His work has provided insights into how deficiencies in DNA mismatch repair mechanisms can lead to resistance against platinum-based chemotherapies, which are commonly used in treating various cancers. ([aacrjournals.org](https://aacrjournals.org/cancerres/article/56/21/4881/502695/The-Role-of-DNA-Mismatch-Repair-in-Platinum-Drug?utm_source=chatgpt.com)) 2. **Dr. Darci Fink**: - An Associate Professor at South Dakota State University, Dr. Darci Fink earned her Ph.D. in cancer research from the University of Nebraska Medical Center in 2016. Her research focuses on various aspects of cancer biology, contributing to the understanding and potential treatment of the disease. ([sdstate.edu](https://www.sdstate.edu/directory/darci-fink?utm_source=chatgpt.com)) 3. **Dr. David J. Fink**: - Affiliated with UC Davis Health, Dr. David Fink's research aims to develop new therapies for neurodegenerative diseases, brain injury, and certain forms of brain cancer. His team focuses on understanding the underlying mechanisms of these conditions to create effective treatments. ([health.ucdavis.edu](https://health.ucdavis.edu/neurology/research/fink.html?utm_source=chatgpt.com))