Expert Opinion on Therapeutic Patents最新文献

An updated patent review of small molecule KCNT1 inhibitors (2022 ‒ 2024). 小分子KCNT1抑制剂的最新专利审查（2022 - 2024）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-05-16 DOI: 10.1080/13543776.2025.2504460

Paul K Peprah, Kyle A Emmitte

{"title":"An updated patent review of small molecule KCNT1 inhibitors (2022 ‒ 2024).","authors":"Paul K Peprah, Kyle A Emmitte","doi":"10.1080/13543776.2025.2504460","DOIUrl":"https://doi.org/10.1080/13543776.2025.2504460","url":null,"abstract":"Introduction: Gain of function mutations in KCNT1 channels have been associated with severe childhood epilepsies. KCNT1 channels are sodium activated potassium channels in the CNS involved in neuronal excitability. Substantial efforts have been made by several groups to discover novel small molecule KCNT1 inhibitors to validate this approach as a therapeutic strategy for the treatment of KCNT1-related epilepsies.Areas covered: This review focusses on 10 published international patent applications from Praxis Precision Medicine that disclose novel small molecule KCNT1 inhibitors for the treatment of KCNT1-related neurological disorders. Features of compounds that contribute to KCNT1 inhibition and published in applications between 2022 and 2024 are discussed. Applications were identified and obtained through the online database, Patentscope, provided by the World Intellectual Property Organization (WIPO) using the search term 'KCNT1 inhibitors.'Expert opinion: Tremendous progress has been made toward the discovery of small molecule inhibitors of KCNT1 channels; however, much work remains to reach a viable therapeutic. Areas of work that will be critically important include further in vivo studies for efficacy, safety, and development of PK/PD relationships. Studies to better understand the binding of known ligands and determine the structural features that govern modulation of the channel are also much needed.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":""},"PeriodicalIF":5.4,"publicationDate":"2025-05-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144076644","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A patent review of IDH1 inhibitors (2018-present). IDH1抑制剂专利审查（2018年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-05-07 DOI: 10.1080/13543776.2025.2500959

Qing Liang, Fei Wen, Peilin Wang, Yitong Jiang, Yuting Geng, Xiaoming Zha

{"title":"A patent review of IDH1 inhibitors (2018-present).","authors":"Qing Liang, Fei Wen, Peilin Wang, Yitong Jiang, Yuting Geng, Xiaoming Zha","doi":"10.1080/13543776.2025.2500959","DOIUrl":"https://doi.org/10.1080/13543776.2025.2500959","url":null,"abstract":"Introduction: isocitrate dehydrogenase 1 (IDH1), a key metabolic enzyme in the cytosol, catalyzes the oxidative decarboxylation of isocitrate to produce α-ketoglutarate (α-KG) and NADPH in the TCA cycle. Pan-cancer studies have demonstrated that IDH1 exhibits a higher mutation frequency and is implicated in a broader range of cancer types, indicating its potential as a promising anti-tumor target.Areas covered: We summarized patents from 2018 to the present that identify novel molecules, compounds, formulations, and methods for inhibiting mIDH1. The literature was retrieved from Web of Science and PubMed. Patent information was obtained via the State Intellectual Property Office's Patent Search and Analysis platform. Clinical data were sourced from the Cortellis Drug Discovery Intelligence database. The date of the most recent search was .Expert opinion: Due to multiple signaling pathway dysregulations and compensatory pathways in solid tumor, monotherapies targeting mutant IDH1 (mIDH1) often fail to achieve desired therapeutic outcomes. Consequently, the combination of mIDH1 inhibitors with other therapeutic agents can enhance the efficacy of antitumor treatments and mitigate the risk of drug resistance. Moreover, the development of novel dual or multiple inhibitors and functional molecules targeting mIDH1 May represent a more promising approach.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-28"},"PeriodicalIF":5.4,"publicationDate":"2025-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143995051","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

P2Y₁₂R antagonists in antithrombotic therapy: a patent and literature review (2019-present). 抗血栓治疗中的P2Y12R拮抗剂：专利和文献综述（2019年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-05-01 Epub Date: 2025-02-19 DOI: 10.1080/13543776.2025.2467683

Xin-Yu Chen, Kai Wang, Jie Jia, Xiao-Tian Kong, Huan-Qiu Li, Sheng Tian

{"title":"P2Y12R antagonists in antithrombotic therapy: a patent and literature review (2019-present).","authors":"Xin-Yu Chen, Kai Wang, Jie Jia, Xiao-Tian Kong, Huan-Qiu Li, Sheng Tian","doi":"10.1080/13543776.2025.2467683","DOIUrl":"10.1080/13543776.2025.2467683","url":null,"abstract":"Introduction: P2Y12 receptor (P2Y12R) is a G protein-coupled receptor that plays a crucial role in regulating platelet activation and aggregation. P2Y12R is involved in various processes such as renal fibrosis, cancer, ischemic disease, and related complications, making it an appealing target for therapeutic interventions. Over the past decade, the discovery and development of P2Y12R antagonists have significantly advanced, offering novel treatment options that improve clinical outcomes.Areas covered: This review covers P2Y12R antagonists reported in patents issued in the online databases of the World Intellectual Property Organization and the European Patent Office from 2019 to 2024. This review introduces the development of existing antagonists and evaluates the therapeutic potential of these compounds.Expert opinion: Reversible P2Y12R antagonists offer a potentially safer alternative to the currently dominant irreversible antagonists on the market, as they allow for more controlled platelet inhibition and can reduce the toxicity and adverse effects associated with conventional drugs. Importantly, the integration of computational drug design and molecular docking studies in the discovery and optimization of P2Y12R antagonists represents a significant advancement in precision medicine. This not only provides valuable structural scaffolds but also stimulates novel ideas for developing promising drugs that are both safe and efficacious.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"515-532"},"PeriodicalIF":5.4,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143424804","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A review of the patent literature surrounding TRPV1 modulators. 关于TRPV1调制器的专利文献综述。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-05-01 Epub Date: 2025-02-20 DOI: 10.1080/13543776.2025.2467698

Isabel Devesa, Gregorio Fernández-Ballester, Asia Fernandez-Carvajal, Antonio Ferrer-Montiel

{"title":"A review of the patent literature surrounding TRPV1 modulators.","authors":"Isabel Devesa, Gregorio Fernández-Ballester, Asia Fernandez-Carvajal, Antonio Ferrer-Montiel","doi":"10.1080/13543776.2025.2467698","DOIUrl":"10.1080/13543776.2025.2467698","url":null,"abstract":"Introduction: TRPV1, a pivotal therapeutic target for chronic pain and pruritus, has been validated in the pathogenesis of several pathologies from diabetes to cancer. Despite the constellation of chemical structures and strategies, none of these molecules has yet been clinically developed as a new drug application due to safety concerns, particularly in thermoregulation. Thus, clinical development of TRPV1 modulators remains a challenge.Areas covered: This review covers the patent literature on TRPV1 modulators (2019-2024, PubMed, Google Patents, and Espacenet), from orthosteric ligands to innovative compounds of biotechnological origin such as interfering RNAs or antibodies, and dual modulators that can act on TRPV1 and associated proteins in different tissues.Expert opinion: Therapeutic strategies that preferentially act on dysfunctional TRPV1 channels appear essential, along with a superior understanding of the underlying mechanisms affecting changes in core body temperature (CBT). Recent findings describing differential receptor interactions of antagonists that do not affect CBT may pave the way to the next generation of orally active TRPV1 inhibitors. Although we have thus far experienced a bitter feeling in TRPV1 drug development, the recent progress in different disciplines, including human-based preclinical models, will set an interdisciplinary approach to design and develop clinically relevant TRPV1 modulators.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"477-491"},"PeriodicalIF":5.4,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143424792","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A patent review of CYP3A4 inhibitors (2018 - present). CYP3A4抑制剂专利审查（2018年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-05-01 Epub Date: 2025-02-24 DOI: 10.1080/13543776.2025.2470294

Dong-Zhu Tu, Xue-Yan Hu, Jing-Xuan Lei, Shu-Yan Liu, Zhang-Ping Xiao, Ling Yang, Guang-Bo Ge

{"title":"A patent review of CYP3A4 inhibitors (2018 - present).","authors":"Dong-Zhu Tu, Xue-Yan Hu, Jing-Xuan Lei, Shu-Yan Liu, Zhang-Ping Xiao, Ling Yang, Guang-Bo Ge","doi":"10.1080/13543776.2025.2470294","DOIUrl":"10.1080/13543776.2025.2470294","url":null,"abstract":"Introduction: Cytochrome P450 3A4 (CYP3A4), one of the most important xenobiotic-metabolizing enzymes, plays a central role in drug metabolism and acts as a key mediator in drug-drug interactions. CYP3A4 inhibitors can potentiate the in vivo therapeutic effects of CYP3A4-substrate drugs via enhancing their systematic exposure levels. Two CYP3A4 inhibitors (ritonavir and cobicistat) have already been approved for modulating the exposure levels of CYP3A4-substrate drugs.Areas covered: This review summarizes the newly patented CYP3A4 inhibitors in the period (2018-2024) by using the keywords 'CYP3A4' and 'inhibitor' in Espacenet database from academic institutions and industrial companies. The chemical structures and inhibition profiles of the patented CYP3A4 inhibitors, including the anti-CYP3A4 potency, inhibitory mechanisms, and other relevant information, are summarized and discussed.Expert opinion: Although diverse CYP3A4 inhibitors have been developed in the past few years, the development of more efficacious CYP3A4 inhibitors with favorable pharmacokinetic and safety profiles is still challenging. To maximize the benefit of CYP3A4 inhibitors, combination strategies should be used for the development of highly specific CYP3A4 inhibitors or degraders with efficacious anti-CYP3A4 effects and favorable pharmacokinetic profiles. Meanwhile, more efforts should be made to address the organ-targeting or tumor-targeting ability of CYP3A4 inhibitors for specific purposes.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"503-513"},"PeriodicalIF":5.4,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143457332","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Update on mGlu4 modulator patents: 2017 to present. mGlu4调制器专利更新：2017年至今。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-05-01 Epub Date: 2025-02-22 DOI: 10.1080/13543776.2025.2467679

Fahad Imtiaz Rahman, Thomas M Webster, Corey R Hopkins

{"title":"Update on mGlu4 modulator patents: 2017 to present.","authors":"Fahad Imtiaz Rahman, Thomas M Webster, Corey R Hopkins","doi":"10.1080/13543776.2025.2467679","DOIUrl":"10.1080/13543776.2025.2467679","url":null,"abstract":"Introduction: Metabotropic glutamate receptor 4 (mGluR4) regulates disease by modulating neurotransmitter release and synaptic plasticity and has been implicated in various diseases, including neurodegenerative disorders and psychiatric conditions, where its dysregulation can impact synaptic function and neuronal signaling.Areas covered: This review covers the patents and key literature concerning mGluR4 PAMs by utilizing the search engines: SciFinder, Google Patents, and PubMed from 2017 to 2024. It summarizes the key exemplified compounds, relevant SAR, and key biological data presented in the patents and primary literature. The key findings and potential path forward are also discussed.Expert opinion: The mGluR4 receptor serves as a novel target for the treatment of neurodegenerative disorders (namely Parkinson's disease), multiple sclerosis, and chronic pain along with other brain disorders. Two compounds have been advanced to early-stage clinical trials from Prexton Therapeutics and Appello Pharmaceuticals. The first compound from Prexton failed due to efficacy and the Appello compound has yet to have results disclosed. The results from this trial will be an important test for whether future mGluR4 PAMs are advanced into clinical trials.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"463-475"},"PeriodicalIF":5.4,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12048291/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143413897","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A patent review of hepatitis B virus core protein allosteric modulators (2019-present). 乙型肝炎病毒核心蛋白变构调节剂专利审查（2019年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-05-01 Epub Date: 2025-03-06 DOI: 10.1080/13543776.2025.2467699

Shuo Wang, Feiyue Ma, Kai Tang, Shujing Xu, Haiyong Jia, Xinyong Liu, Peng Zhan

{"title":"A patent review of hepatitis B virus core protein allosteric modulators (2019-present).","authors":"Shuo Wang, Feiyue Ma, Kai Tang, Shujing Xu, Haiyong Jia, Xinyong Liu, Peng Zhan","doi":"10.1080/13543776.2025.2467699","DOIUrl":"10.1080/13543776.2025.2467699","url":null,"abstract":"Introduction: The hepatitis B virus (HBV) core protein is a significant therapeutic target due to its essential role in HBV replication. Over the past five years, numerous structurally unique CpAMs have been patented. However, no compounds have been approved due to various issues such as poor pharmacokinetics (PK) and hepatotoxicity. As a result, there is an urgent need to develop novel CpAMs without these limitations.Areas covered: This review provides a comprehensive analysis of patents related to CpAMs from 2019 to the present, with the aim of delineating the chemical evolution that has occurred in the pursuit of more promising CpAMs. The sources of patent information included databases of the European Patent Office, the China Patent Office and the U.S.A. Patent Office, while relevant research articles were accessed through PubMed.Expert opinion: During the optimization of CpAMs, striking a good balance between activity and druggability usually poses a certain challenge while the emergence of drug resistance issues further complicates the development process. A comprehensive analysis of the structural features of CpAMs and identification of essential patterns in chemical evolution can reveal common principles that improve pharmacodynamic (PD) and PK profiles, thereby facilitating the discovery of next-generation CpAMs.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"441-461"},"PeriodicalIF":5.4,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143476414","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

JBI-802: the first orally available LSD1/HDAC6 dual inhibitor to enter clinical trials. JBI-802：首个进入临床试验的口服LSD1/HDAC6双抑制剂。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-05-01 Epub Date: 2025-02-20 DOI: 10.1080/13543776.2025.2468792

Jingya Zhang, Xiangli Ren, Yihui Song, Bin Yu

{"title":"JBI-802: the first orally available LSD1/HDAC6 dual inhibitor to enter clinical trials.","authors":"Jingya Zhang, Xiangli Ren, Yihui Song, Bin Yu","doi":"10.1080/13543776.2025.2468792","DOIUrl":"10.1080/13543776.2025.2468792","url":null,"abstract":"Introduction: Lysine-specific demethylase 1 (LSD1) and histone deacetylase 6 (HDAC6) are key epigenetic regulators involved in histone demethylation and deacetylation processes that impact chromatin structure and gene expression. JBI-802 marks a major advancement as the first novel, orally available LSD1/HDAC6 dual inhibitor currently in clinical trials.Areas covered: This review provides a comprehensive overview of the discovery and development of JBI-802, detailing its structure-activity relationship (SARs), chemical synthesis, biological activity, and clinical progress. Other dual LSD1/HDAC6 inhibitors and the challenges are briefly discussed, underscoring the therapeutic potential of dual inhibition in disease treatment. The literature search is performed using SciFinder, Google patent, ClinicalTrials databases, and PubMed.Expert opinion: The dual LSD1/HDAC6 inhibitor JBI-802 demonstrates robust anti-proliferative activity, significant antitumor effects in multiple hematologic malignancies, and superior efficacy in combination with checkpoint inhibitors in the CT-26 syngeneic mouse model. JBI-802 is currently undergoing phase I/II clinical trials in patients with advanced solid tumors, myeloproliferative neoplasms (MPN), and myelodysplastic/myeloproliferative neoplasms (MDS/MPN) with thrombocytosis. However, the potential on-target toxicity, off-target interactions and selectivity concerns deservee more attention.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"493-501"},"PeriodicalIF":5.4,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143440441","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A patent review of anti-coronavirus agents targeting the spike-ACE2 interaction (2019-present). 针对刺突- ace2相互作用的抗冠状病毒药物专利审查（2019年至今）

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-04-24 DOI: 10.1080/13543776.2025.2494860

Xing Huang, Heng Gao, Jiwei Zhang, Peng Zhan, Xinyong Liu

{"title":"A patent review of anti-coronavirus agents targeting the spike-ACE2 interaction (2019-present).","authors":"Xing Huang, Heng Gao, Jiwei Zhang, Peng Zhan, Xinyong Liu","doi":"10.1080/13543776.2025.2494860","DOIUrl":"https://doi.org/10.1080/13543776.2025.2494860","url":null,"abstract":"Introduction: The Angiotensin-converting enzyme 2 (ACE2) receptor, crucial for coronavirus recognition of host cells, is a key target for therapeutic intervention against SARS-CoV-2 and related coronaviruses. Therefore, thoroughly investigating the interaction mechanism between ACE2 and the Spike protein (S protein), as well as developing targeted inhibitors based on this mechanism, is vital for effectively controlling the spread of SARS-CoV-2 and preventing potential future pandemics caused by other coronaviruses.Areas covered: This article comprehensively reviews the mechanisms underlying ACE2-S protein interaction that facilitate SARS-CoV-2 entry into host cells. It also analyzes the patent landscape regarding inhibitors targeting the ACE2-S interface since 2019.Expert opinion: In the 5 years since the outbreak of SARS-CoV-2, numerous methods and design strategies have been employed to develop innovative therapeutics against coronaviruses. Among these approaches, inhibitors targeting both the ACE2 receptor and the S protein have gained significant interest due to their potential in blocking various coronaviruses. Despite facing challenges similar to other protein-protein interaction inhibitors, progress has been made in developing these inhibitors through virtual screening, covalent protein binding, and peptide modification strategies. However, obstacles persist in clinical translation, necessitating a multidisciplinary strategy that integrates state-of-the-art methodologies to optimize S-ACE2 interface-targeted drug discovery.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-12"},"PeriodicalIF":5.4,"publicationDate":"2025-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143990595","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Novel inhibitors of STAT3: an updated patent review (2022-present). STAT3的新型抑制剂：更新的专利审查（2022年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-04-22 DOI: 10.1080/13543776.2025.2494857

Keting Bao, Peiran Li, Dingding Gao

{"title":"Novel inhibitors of STAT3: an updated patent review (2022-present).","authors":"Keting Bao, Peiran Li, Dingding Gao","doi":"10.1080/13543776.2025.2494857","DOIUrl":"https://doi.org/10.1080/13543776.2025.2494857","url":null,"abstract":"Introduction: Signal transducer and activator of transcription 3 (STAT3), a member of the STAT protein family, serves as both a signal transducer and a transcription factor. Previous studies have highlighted its pivotal roles in regulating cell proliferation, differentiation, apoptosis, as well as immune and inflammatory responses. Consequently, targeting STAT3 has emerged as a promising therapeutic strategy for addressing related diseases.Areas covered: This review offers a comprehensive summary of the progress in discovering STAT3 inhibitors, with a focus on their structural diversity and structure-activity relationships as presented in patent literature from 2022 to the present.Expert opinion: Over the past decades, significant progress has transformed STAT3 into a target of interest for drug development. Despite these advances, no STAT3-targeting drugs have successfully progressed through late-phase clinical trials, largely due to challenges such as limited selectivity and undesirable side effects. These obstacles highlight the inherent complexity of developing safe and effective STAT3 inhibitors. Nevertheless, STAT3 remains a highly promising therapeutic target, and ongoing advancements in this field hold the potential to unlock novel strategies for addressing STAT3-related diseases.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-23"},"PeriodicalIF":5.4,"publicationDate":"2025-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144005104","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0