Expert Opinion on Therapeutic Patents最新文献_第2页

A patent review of small molecular inhibitors targeting EGFR exon 20 insertion (Ex20ins) (2019-present). 靶向EGFR外显子20插入（Ex20ins）的小分子抑制剂专利审查（2019-至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-01 Epub Date: 2024-12-27 DOI: 10.1080/13543776.2024.2446220

Wenjian Zhu, Junping Pei, Xiaoyun Lu

{"title":"A patent review of small molecular inhibitors targeting EGFR exon 20 insertion (Ex20ins) (2019-present).","authors":"Wenjian Zhu, Junping Pei, Xiaoyun Lu","doi":"10.1080/13543776.2024.2446220","DOIUrl":"10.1080/13543776.2024.2446220","url":null,"abstract":"Introduction: Mutations in epidermal growth factor receptor (EGFR) kinase domain consistently activate downstream signaling pathways, such as the PI3K/AKT/mTOR and RAS/RAF/MEK, thereby promoting tumor growth. Although the majority of non-small cell lung cancer (NSCLC) patients harboring EGFR mutations are sensitive to existing EGFR tyrosine kinase inhibitors (EGFR-TKIs), there remains an unmet clinical need for effective therapies targeting EGFR Ex20ins mutations, making direct targeting EGFR Ex20ins mutations a promising therapeutic strategy.Areas covered: This review covers the progress of clinical studies targeting EGFR Ex20ins inhibitors and summarizes recent (1 January 2019 - 30 April 2024) patents disclosing EGFR Ex20ins inhibitors available in the Espacenet and CAS SciFinder databases.Expert opinion: An increasing number of EGFR Ex20ins inhibitors are being developed and reported. Existing inhibitors are focused on enhancing the efficacy of EGFR Ex20ins inhibitors and addressing the challenge of targeted resistance by optimizing the second - or third-generation EGFR inhibitors and developing innovative skeleton molecules. Moreover, the development of targeted protein degraders, allosteric inhibitors, and combination therapies provide additional approaches to address EGFR Ex20ins mutations. However, bypass resistance, selectivity, and drug sensitivity still pose challenges in this field.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"91-110"},"PeriodicalIF":5.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142871905","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 xanthine oxidase inhibitors (2021-present). 黄嘌呤氧化酶抑制剂专利回顾（2021年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-01 Epub Date: 2024-12-30 DOI: 10.1080/13543776.2024.2446222

Chang Liu, Qing Mao, Bing Zhang, Xuefeng Fu, Tingjian Zhang, Shaojie Wang

{"title":"A patent review of xanthine oxidase inhibitors (2021-present).","authors":"Chang Liu, Qing Mao, Bing Zhang, Xuefeng Fu, Tingjian Zhang, Shaojie Wang","doi":"10.1080/13543776.2024.2446222","DOIUrl":"10.1080/13543776.2024.2446222","url":null,"abstract":"Introduction: Xanthine oxidase (XO) catalyzes the oxidation of both hypoxanthine and xanthine in the last two steps of the purine metabolic pathway, serving as a rate-limiting enzyme for uric acid production as well as a key target for the treatment of gout and other hyperuricemia-related conditions.Areas covered: This paper reviews XO inhibitors in patents from 2021 to the present. We summarize in detail the structural classes and characteristics, in vitro and in vivo biological results, and structure‒activity relationships of synthetic inhibitors, as well as the sources, specific structures, research methods, and biological activities of XO inhibitors from natural products.Expert opinion: (1) Benefiting from the discovery of many high-affinity inhibitors, the binding modes of small molecules in the active pocket of XO have been further elucidated, and this information will contribute to future development; (2) natural products remain one of the important sources in the discovery of XO inhibitors; (3) with a deeper exploration of XO and URAT1 targets, XO/URAT1 dual target inhibitors may be a future research hotspot; and (4) the search for high-affinity, small-molecule scaffolds remains a key challenge and an important direction for the future development.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"79-89"},"PeriodicalIF":5.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142893203","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

Selective JAK1 inhibitors and the therapeutic applications thereof: a patent review (2016-2023). 选择性JAK1抑制剂及其治疗应用：专利审查（2016-2023）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-01 Epub Date: 2024-12-25 DOI: 10.1080/13543776.2024.2446223

Yuhui Gao, Li Lan, Cheng Wang, Yuwei Wang, Lei Shi, Liping Sun

{"title":"Selective JAK1 inhibitors and the therapeutic applications thereof: a patent review (2016-2023).","authors":"Yuhui Gao, Li Lan, Cheng Wang, Yuwei Wang, Lei Shi, Liping Sun","doi":"10.1080/13543776.2024.2446223","DOIUrl":"10.1080/13543776.2024.2446223","url":null,"abstract":"Introduction: The family of Janus kinases (JAKs) consists of four intracellular non-receptor tyrosine kinases: JAK1, JAK2, JAK3, and tyrosine kinase 2 (TYK2). Among these four subtypes, JAK1 is the only isoform that can form heterodimers with all three JAKs, and JAK1 dysfunction can lead to inflammation and severe autoimmune diseases. Interest in JAK1 inhibitors has grown tremendously, and the number of inhibitors targeting JAK1 continues to rise annually.Areas covered: This paper reviews JAK1 small molecule inhibitors that were reported in patent literature from January 2016 to December 2023. Web of Science, SciFinder, PubMed, WIPO, EPO, USPTO, and CNIPA databases were used for searching the literature and patents for JAK1 inhibitors.Expert opinion: JAK1 inhibitors show great promise in treating cytokine dysregulated disorders; nevertheless, nonselective JAK1 inhibitors have more severe side effects, which restricts the therapy's safety and use. Therefore, developing highly selective JAK1 inhibitors can mitigate potential risks and lead to next-generation therapies with improved efficacy and safety profiles.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"181-195"},"PeriodicalIF":5.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142881254","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

Strategies for the treatment of acute myeloid leukemia with FLT3 mutations: a patent review. FLT3突变的急性髓系白血病的治疗策略：专利审查。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-01 Epub Date: 2025-01-05 DOI: 10.1080/13543776.2024.2446224

Lukas Gorecki, Eva Reznickova, Vladimir Krystof, Martina Rezacova, Martina Ceckova, Jan Korabecny

{"title":"Strategies for the treatment of acute myeloid leukemia with FLT3 mutations: a patent review.","authors":"Lukas Gorecki, Eva Reznickova, Vladimir Krystof, Martina Rezacova, Martina Ceckova, Jan Korabecny","doi":"10.1080/13543776.2024.2446224","DOIUrl":"10.1080/13543776.2024.2446224","url":null,"abstract":"Introduction: Approximately one-third of all AML patients have a mutation in the Fms-like tyrosine kinase 3 (FLT3) gene, which is associated with a poor prognosis in these individuals. The 2017 approval of midostaurin, the first FLT3 inhibitor, spurred extensive development of more potent and selective inhibitors with an improved safety profile.Areas covered: This review analyzes patent inventions for the treatment of AML using FLT3 inhibitors, covering developments from the earliest to the most recent, disclosed in 2024. Our search using the global Espacenet database identified numerous compounds with low nanomolar inhibitory concentrations against FLT3-ITD and FLT3-TKD mutants. These compounds have shown promise in preclinical studies. Co-inhibition strategies and combinatorial therapies to overcome resistance and enhance anti-leukemic efficacy are also discussed.Expert opinion: Recent patents highlight advances in the field of FLT3 inhibitors with a focus on overcoming resistance, improving selectivity and potency. Future strategies may include third-generation inhibitors such as type III allosteric inhibitors, irreversible inhibitors, or PROTACs. Personalized medicine approaches utilizing genetic profiling to tailor therapies are emphasized. Exploration of novel combination regimens with emerging therapies like CAR T-cell therapy, immune checkpoint inhibitors, and small molecules targeting critical AML pathways is ongoing to further enhance anti-leukemic efficacy.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"137-164"},"PeriodicalIF":5.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142881469","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

Patent review of novel compounds targeting opioid use disorder (2018-2024). 针对阿片类药物使用障碍的新型化合物专利审查（2018-2024）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-01 Epub Date: 2025-01-26 DOI: 10.1080/13543776.2024.2446230

Samuel Obeng, Lance R McMahon, Edward Ofori

{"title":"Patent review of novel compounds targeting opioid use disorder (2018-2024).","authors":"Samuel Obeng, Lance R McMahon, Edward Ofori","doi":"10.1080/13543776.2024.2446230","DOIUrl":"10.1080/13543776.2024.2446230","url":null,"abstract":"Introduction: Opioids have served as a cornerstone in pain management for decades. However, the emergence of increasingly potent synthetic analogs brings forth a range of side effects, including respiratory depression, tolerance, dependence, constipation, and, more importantly, the development of severe and debilitating opioid use disorder (OUD). Search for therapeutics to mitigate OUD has been challenging, and this has called for novel approaches that include the design of small molecules targeting neuronal circuits involved in addiction (opioid, dopamine, serotonin, norepinephrine, and glutamate receptors, etc.).Areas covered: In this review, we retrieve and discuss two dozen (24) relevant patents filed in the past six (6) years that focus on novel small-molecule therapeutics for OUD. The chemical entities disclosed were highlighted, and specific examples were provided where necessary.Expert opinion: Several chemical entities targeting both opioid and non-opioid targets are under consideration for treating OUD. Our search for patents covering such compounds revealed embodiments with diverse chemistry. Understanding the public impact of OUD and the rapidly evolving landscape of substance abuse underscores the urgent need for a thorough reevaluation of strategies to address these challenges. This includes the development of small molecules with unique mechanisms of action for OUD treatment.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"165-180"},"PeriodicalIF":5.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143002869","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

Small molecule ATM inhibitors as potential cancer therapy: a patent review (2003-present). 小分子ATM抑制剂作为潜在的癌症治疗：专利审查（2003年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-01 Epub Date: 2025-01-06 DOI: 10.1080/13543776.2024.2446228

Yan A Ivanenkov, Alexander S Malyshev, Victor A Terentiev, Anastasia A Korzhenevskaya, Sergei A Evteev, Sergey Z Vatsadze, Aleksei V Medved'ko, Petr V Shegai, Andrey D Kaprin

{"title":"Small molecule ATM inhibitors as potential cancer therapy: a patent review (2003-present).","authors":"Yan A Ivanenkov, Alexander S Malyshev, Victor A Terentiev, Anastasia A Korzhenevskaya, Sergei A Evteev, Sergey Z Vatsadze, Aleksei V Medved'ko, Petr V Shegai, Andrey D Kaprin","doi":"10.1080/13543776.2024.2446228","DOIUrl":"10.1080/13543776.2024.2446228","url":null,"abstract":"Introduction: The ataxia telangiectasia mutated kinase (ATM) is key in coordinating the DDR signaling network essential for responding to double-strand breaks (DSBs). Several ATM inhibitors are being investigated for potential anticancer treatment in clinical trials.Areas covered: This review aims to provide a comprehensive overview of patents and patent applications since 2003, with a particular focus on the structural properties, activity and efficacy of the claimed ATM kinase small-molecule inhibitors. The search was conducted using SciFinder, Cortellis Drug Discovery Intelligence Database, and Espacenet. After filtering, 44 records were identified for further analysis. This paper also discusses the recent progress in the clinical trials and development history.Expert opinion: ATM kinase is a promising target for cancer therapy. Small-molecule ATM kinase inhibitors hold significant potential in cancer treatment by enhancing the efficacy of existing DNA-damaging therapies. Patent analysis revealed that the majority of these compounds contain imidazo[4,5-c]quinolinone scaffold or its bioisosteric variations which are optimal in terms of good ATM inhibitory activity and selectivity over closely related enzymes. Clinical trials explore combinations with RT or DNA-targeted compounds like PARP inhibitors, which induce DSBs. The medicinal chemistry field anticipates that these therapeutic options will soon be available on the pharmaceutical market.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"111-136"},"PeriodicalIF":5.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142893208","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

The role of patent analysis in target selection. 专利分析在目标选择中的作用。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-01-08 DOI: 10.1080/13543776.2024.2447070

Daniel H O Donovan, Weiping Wang, Jim Sheppeck, Gerjan de Bruin

引用次数: 0

Histamine H₃ receptor antagonists/inverse agonists: a patent review (October 2017 - December 2023) documenting progress. 组胺H3受体拮抗剂/逆激动剂：专利审查（2017年10月- 2023年12月）记录进展。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-01-05 DOI: 10.1080/13543776.2024.2446227

Dorota Łażewska, Katarzyna Kieć-Kononowicz

{"title":"Histamine H3 receptor antagonists/inverse agonists: a patent review (October 2017 - December 2023) documenting progress.","authors":"Dorota Łażewska, Katarzyna Kieć-Kononowicz","doi":"10.1080/13543776.2024.2446227","DOIUrl":"https://doi.org/10.1080/13543776.2024.2446227","url":null,"abstract":"Introduction: Histamine H3 receptor antagonists/inverse agonists, since the discovery of histamine H3 receptor (H3R), are important ligands in the search for new potential drugs. The most interesting are CNS diseases as these receptors are mainly there present.Areas covered: The current review covers patent applications/patents that were published during the last 6 years (October 2017 - December 2023). Documents were found in two free available patent databases: Espacenet and PatentScope and divided into three basic categories such as methods, compounds, and therapeutic indications. It provides an overview of 51 patent applications/patents. Many pharmaceutical compositions with H3R antagonists/inverse agonists have been claimed. Furthermore, PubMed, Scopus, and ClinicalTrials databases were searched for literature to prepare this review.Expert opinion: Interest in the H3R field is still high and has remained almost unchanged over the last 10 years in the number of publications, but the type of publications has changed (fewer new ligands, more pharmacological studies). Currently, the search for new H3R ligands is focused on multi-target compounds. The first crystal structure of H3R with a ligand appeared. New therapeutic indications, such as autism, fatigue, and Prader-Willi syndrome, are verified in clinical trials.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-25"},"PeriodicalIF":5.4,"publicationDate":"2025-01-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142931106","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

Urease inhibitors for the treatment of H. pylori. 治疗幽门螺杆菌的尿素酶抑制剂。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-01-01 Epub Date: 2024-11-10 DOI: 10.1080/13543776.2024.2423004

Özlen Güzel-Akdemir, Atilla Akdemir

引用次数: 0

CBL-B - An upcoming immune-oncology target. 关于治疗专利的专家意见 - 手稿编号 EOTP-2024-ST-0024 已在线提交。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-01-01 Epub Date: 2024-11-25 DOI: 10.1080/13543776.2024.2412567

Riccardo Fusco, Zeinab Saedi, Imma Capriello, Andriy Lubskyy, Alexander Dömling

{"title":"CBL-B - An upcoming immune-oncology target.","authors":"Riccardo Fusco, Zeinab Saedi, Imma Capriello, Andriy Lubskyy, Alexander Dömling","doi":"10.1080/13543776.2024.2412567","DOIUrl":"10.1080/13543776.2024.2412567","url":null,"abstract":"Introduction: The E3 ubiquitin ligase Cbl-b is a novel target in immune-oncology, with critical roles in regulating T-cell activation and signaling pathways. By facilitating the ubiquitination and degradation of key signaling proteins, Cbl-b modulates immune responses, maintaining immune homeostasis and preventing unwarranted T-cell proliferation. The therapeutic potential of Cbl-b as a cancer immunotherapy target is underscored by its contribution to an immunosuppressive tumor microenvironment, with efforts currently underway to develop small-molecule inhibitors.Areas covered: We reviewed the small molecules, and antibody-drug conjugates targeting Cbl-b from 2018 to 2024. The patents were gathered through publicly available databases and analyzed with in-house developed cheminformatic workflow, described within the manuscript.Expert opinion: Targeting Cbl-b presents a promising approach in immuno-oncology, offering a novel pathway to potentiate the immune system's ability to combat cancer beyond PDL1/PD1 inhibition. The development and clinical advancement of Cbl-b inhibitors, as evidenced by the ongoing trials, mark a significant step toward harnessing this target for therapeutic benefits. Overall, the strategic inhibition of Cbl-b holds substantial promise for improving cancer immunotherapy outcomes, heralding a new era in the fight against cancer.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"47-64"},"PeriodicalIF":5.4,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142709494","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