Expert Opinion on Therapeutic Patents最新文献_第7页

Targeting the relaxin-3/RXFP3 system: a patent review for the last two decades 以松弛素-3/RXFP3 系统为靶标：过去二十年的专利回顾

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-04-04 DOI: 10.1080/13543776.2024.2338099

Md Toufiqur Rahman, Hetti Handi Chaminda Lakmal, Javeena Hussain, Chunyang Jin

引用次数: 0

Type II & III inhibitors of tropomyosin receptor kinase (Trk): a 2020-2022 patent update. 肌球蛋白受体激酶（Trk）的 II 型和 III 型抑制剂：2020-2022 年专利更新。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-04-01 Epub Date: 2024-05-30 DOI: 10.1080/13543776.2024.2358818

Petar Iliev, Carolin Jaworski, Carmen Wängler, Björn Wängler, Brent D G Page, Ralf Schirrmacher, Justin J Bailey

{"title":"Type II & III inhibitors of tropomyosin receptor kinase (Trk): a 2020-2022 patent update.","authors":"Petar Iliev, Carolin Jaworski, Carmen Wängler, Björn Wängler, Brent D G Page, Ralf Schirrmacher, Justin J Bailey","doi":"10.1080/13543776.2024.2358818","DOIUrl":"10.1080/13543776.2024.2358818","url":null,"abstract":"Introduction: The Trk family proteins are membrane-bound kinases predominantly expressed in neuronal tissues. Activated by neurotrophins, they regulate critical cellular processes through downstream signaling pathways. Dysregulation of Trk signaling can drive a range of diseases, making the design and study of Trk inhibitors a vital area of research. This review explores recent advances in the development of type II and III Trk inhibitors, with implications for various therapeutic applications.Areas covered: Patents covering type II and III inhibitors targeting the Trk family are discussed as a complement of the previous review, Type I inhibitors of tropomyosin receptor kinase (Trk): a 2020-2022 patent update. Relevant patents were identified using the Web of Science database, Google, and Google Patents.Expert opinion: While type II and III Trk inhibitor development has advanced more gradually compared to their type I counterparts, they hold significant promise in overcoming resistance mutations and achieving enhanced subtype selectivity - a critical factor in reducing adverse effects associated with pan-Trk inhibition. Recent interdisciplinary endeavors have marked substantial progress in the design of subtype selective Trk inhibitors, with impressive success heralded by the type III inhibitors. Notably, the emergence of mutant-selective Trk inhibitors introduces an intriguing dimension to the field, offering precise treatment possibilities.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"231-244"},"PeriodicalIF":5.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141086799","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

Synthetic lethality: targeting the SMARCA2 bromodomain for degradation in SMARCA4-deficient tumors - a review of patent literature from 2019-June 2023. 合成致死：靶向SMARCA2溴链降解SMARCA4缺陷肿瘤--2019年至2023年6月专利文献综述。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-04-01 Epub Date: 2024-05-20 DOI: 10.1080/13543776.2024.2355258

Esther C Y Lee, Kyle D Reichl, Ariamala Gopalsamy

{"title":"Synthetic lethality: targeting the SMARCA2 bromodomain for degradation in SMARCA4-deficient tumors - a review of patent literature from 2019-June 2023.","authors":"Esther C Y Lee, Kyle D Reichl, Ariamala Gopalsamy","doi":"10.1080/13543776.2024.2355258","DOIUrl":"10.1080/13543776.2024.2355258","url":null,"abstract":"Introduction: SMARCA2 and SMARCA4 are subunits of the SWI/SNF complex which is a chromatin remodeling complex and a key epigenetic regulator that facilitates gene expression. Tumors with loss of function mutations in SMARCA4 rely on SMARCA2 for cell survival and this synthetic lethality is a potential therapeutic strategy to treat cancer.Areas covered: The current review focuses on patent applications that claim proteolysis-targeting chimeras (PROTAC) degraders that bind the bromodomain site of SMARCA2 and are published between January 2019-June 2023. A total of 29 applications from 9 different applicants were evaluated.Expert opinion: SMARCA2/4 bromodomain inhibitors do not lead to desired effects on cancer proliferation; however, companies have converted bromodomain binders into PROTACs to degrade the protein, with a preference for SMARCA2 over SMARCA4. Selective degradation of SMARCA2 is most likely required to be efficacious in the SMARCA4-deficient setting, while allowing for sufficient safety margin in normal tissues. With several patent applications disclosed recently, interest in targeting SMARCA2 should continue, especially with a selective SMARCA2 PROTAC now in the clinic from Prelude Therapeutics. The outcome of the clinical trials will influence the evolution of selective SMARCA2 PROTACs development.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"211-229"},"PeriodicalIF":5.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140916195","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 P2X7 receptor antagonists to treat inflammatory diseases (2018-present). 治疗炎症性疾病的 P2X7 受体拮抗剂专利回顾（2018 年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-04-01 Epub Date: 2024-06-11 DOI: 10.1080/13543776.2024.2363885

Jamshed Iqbal, Sehrish Bano, Imtiaz Ali Khan, Qing Huang

{"title":"A patent review of P2X7 receptor antagonists to treat inflammatory diseases (2018-present).","authors":"Jamshed Iqbal, Sehrish Bano, Imtiaz Ali Khan, Qing Huang","doi":"10.1080/13543776.2024.2363885","DOIUrl":"10.1080/13543776.2024.2363885","url":null,"abstract":"Introduction: The purinergic P2X7 receptor (P2X7R) is expressed on the surface of many different types of cells, including immune cells. Targeting P2X7R with antagonists has been studied for its potential therapeutic effects in a variety of inflammatory illnesses.Area covered: Many chemical substances, including carboxamides, benzamides and nitrogen containing heterocyclic derivatives have demonstrated promising inhibitory potential for P2X7 receptor. The chemistry and clinical applications of P2X7R antagonists patented from 2018- present are discussed in this review.Expert opinion: Purinergic receptor inhibitor discovery and application has demonstrated the potential for therapeutic intervention, as demonstrated by pharmacological research. Few chemical modalities have been authorized for use in clinical settings, despite the fact that breakthroughs in crystallography and chemical biology have increased the knowledge of purinergic signaling and its consequences in disease. The many research projects and pharmaceutical movements that sustain dynamic P2X receptor programs over decades are evidence of the therapeutic values and academic persistence in purinergic study. P2X7R is an intriguing therapeutic target and possible biomarker for inflammation. Although several companies like Merck and AstraZeneca have published patents on P2X3 antagonists, the search for P2X7R antagonists has not stopped. Numerous pharmaceutical companies have disclosed different scaffolds, and some molecules are presently being studied in clinical studies.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"263-271"},"PeriodicalIF":5.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141199485","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

Protein tyrosine phosphatase inhibitors: a patent review and update (2012-2023). 蛋白酪氨酸磷酸酶抑制剂：专利回顾与更新（2012-2023 年）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-04-01 Epub Date: 2024-06-19 DOI: 10.1080/13543776.2024.2362203

Lakshmi Mounika Kelam, Vaishnavi Chhabra, Sarika Dhiman, Deevena Kumari, M Elizabeth Sobhia

{"title":"Protein tyrosine phosphatase inhibitors: a patent review and update (2012-2023).","authors":"Lakshmi Mounika Kelam, Vaishnavi Chhabra, Sarika Dhiman, Deevena Kumari, M Elizabeth Sobhia","doi":"10.1080/13543776.2024.2362203","DOIUrl":"https://doi.org/10.1080/13543776.2024.2362203","url":null,"abstract":"Introduction: Protein tyrosine phosphatases (PTPs), essential and evolutionarily highly conserved enzymes, govern cellular functions by modulating tyrosine phosphorylation, a pivotal post-translational modification for signal transduction. The recent strides in phosphatase drug discovery, leading to the identification of selective modulators for enzymes, restoring interest in the therapeutic targeting of protein phosphatases.Areas covered: The compilation of patents up to the year 2023 focuses on the efficacy of various classes of Tyrosine phosphatases and their inhibitors, detailing their chemical structure and biochemical characteristics. These findings have broad implications, as they can be applied to treating diverse conditions like cancer, diabetes, autoimmune disorders, and neurological diseases. The search for scientific articles and patent literature was conducted using well known different platforms to gather information up to 2023.Expert opinion: The latest improvements in protein tyrosine phosphatase (PTP) research include the discovery of new inhibitors targeting specific PTP enzymes, with a focus on developing allosteric site covalent inhibitors for enhanced efficacy and specificity. These advancements have not only opened up new possibilities for therapeutic interventions in various disease conditions but also hold the potential for innovative treatments. PTPs offer promising avenues for drug discovery efforts and innovative treatments across a spectrum of health conditions.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":"34 4","pages":"187-209"},"PeriodicalIF":5.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141450177","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

HDAC3 inhibitors: a patent review of their broad-spectrum applications as therapeutic agents. HDAC3 抑制剂：关于其作为治疗剂的广泛应用的专利综述。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-04-01 Epub Date: 2024-06-25 DOI: 10.1080/13543776.2024.2363890

Thabo Brighton Makgoba, Erika Kapp, Samuel Egieyeh, Jacques Joubert

{"title":"HDAC3 inhibitors: a patent review of their broad-spectrum applications as therapeutic agents.","authors":"Thabo Brighton Makgoba, Erika Kapp, Samuel Egieyeh, Jacques Joubert","doi":"10.1080/13543776.2024.2363890","DOIUrl":"10.1080/13543776.2024.2363890","url":null,"abstract":"Introduction: Histone deacetylases (HDACs) are a class of zinc-dependent enzymes. They maintain acetylation homeostasis, with numerous biological functions and are associated with many diseases. HDAC3 strictly requires multi-subunit complex formation for activity. It is associated with the progression of numerous non-communicable diseases. Its widespread involvement in diseases makes it an epigenetic drug target. Preexisting HDAC3 inhibitors have many uses, highlighting the need for continued research in the discovery of HDAC3-selective inhibitors.Area covered: This review provides an overview of 24 patents published from 2010 to 2023, focusing on compounds that inhibit the HDAC3 isoenzyme.Expert opinion: HDAC3-selective inhibitors - pivotal for pharmacological applications, as single or combination therapies - are gaining traction as a strategy to move away from complications laden pan-HDAC inhibitors. Moreover, there is an unmet need for HDAC3 inhibitors with alternative zinc-binding groups (ZBGs) because some preexisting ZBGs have limitations related to toxicity and side effects. Difficulties in achieving HDAC3 selectivity may be due to isoform selectivity. However, advancements in computer-aided drug design and experimental data of HDAC3 3D co-crystallized models could lead to the discovery of novel HDAC3-selective inhibitors, which bear alternative ZBGs with balanced selectivity for HDAC3 and potency.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"273-295"},"PeriodicalIF":5.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141316961","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

Carbonic anhydrase and bacterial metabolism: a chance for antibacterial drug discovery 碳酸酐酶与细菌新陈代谢：抗菌药物发现的契机

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-03-20 DOI: 10.1080/13543776.2024.2332663

Clemente Capasso, Claudiu T. Supuran

引用次数: 0

Successes and challenges in the development of BD1-selective BET inhibitors: a patent review 开发 BD1 选择性 BET 抑制剂的成功与挑战：专利回顾

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-03-05 DOI: 10.1080/13543776.2024.2327300

Monica Viviano, Alessandra Cipriano, Emanuele Fabbrizi, Alessandra Feoli, Sabrina Castellano, Gianluca Sbardella, Antonello Mai, Ciro Milite, Dante Rotili

引用次数: 0

Targeting the PI3K/AKT signaling pathway in anticancer research: a recent update on inhibitor design and clinical trials (2020-2023). 在抗癌研究中靶向 PI3K/AKT 信号通路：抑制剂设计和临床试验的最新进展（2020-2023 年）。

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-03-01 Epub Date: 2024-04-09 DOI: 10.1080/13543776.2024.2338100

Dima A Sabbah, Rima Hajjo, Sanaa K Bardaweel, Haizhen A Zhong

{"title":"Targeting the PI3K/AKT signaling pathway in anticancer research: a recent update on inhibitor design and clinical trials (2020-2023).","authors":"Dima A Sabbah, Rima Hajjo, Sanaa K Bardaweel, Haizhen A Zhong","doi":"10.1080/13543776.2024.2338100","DOIUrl":"10.1080/13543776.2024.2338100","url":null,"abstract":"Introduction: Recent years have witnessed great achievements in drug design and development targeting the phosphatidylinositol 3-kinase/protein kinase-B (PI3K/AKT) signaling pathway, a pathway central to cell growth and proliferation. The nearest neighbor protein-protein interaction networks for PI3K and AKT show the interplays between these target proteins which can be harnessed for drug discovery. In this review, we discuss the drug design and clinical development of inhibitors of PI3K/AKT in the past three years. We review in detail the structures, selectivity, efficacy, and combination therapy of 35 inhibitors targeting these proteins, classified based on the target proteins. Approaches to overcoming drug resistance and to minimizing toxicities are discussed. Future research directions for developing combinational therapy and PROTACs of PI3K and AKT inhibitors are also discussed.Area covered: This review covers clinical trial reports and patent literature on inhibitors of PI3K and AKT published between 2020 and 2023.Expert opinion: To address drug resistance and drug toxicity of inhibitors of PI3K and AKT, it is highly desirable to design and develop subtype-selective PI3K inhibitors or subtype-selective AKT1 inhibitors to minimize toxicity or to develop allosteric drugs that can form covalent bonds. The development of PROTACs of PI3Kα or AKT helps to reduce off-target toxicities.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"141-158"},"PeriodicalIF":6.6,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140335336","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 on HMGB1 inhibitors for the treatment of liver diseases. 关于治疗肝病的 HMGB1 抑制剂的专利综述。

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-03-01 Epub Date: 2024-04-09 DOI: 10.1080/13543776.2024.2338105

Richa Raj, Pingping Shen, Boyang Yu, Jian Zhang

{"title":"A patent review on HMGB1 inhibitors for the treatment of liver diseases.","authors":"Richa Raj, Pingping Shen, Boyang Yu, Jian Zhang","doi":"10.1080/13543776.2024.2338105","DOIUrl":"10.1080/13543776.2024.2338105","url":null,"abstract":"Introduction: HMGB1 is a non-histone chromatin protein released or secreted in response to tissue damage or infection. Extracellular HMGB1, as a crucial immunomodulatory factor, binds with several different receptors to innate inflammatory responses that aggravate acute and chronic liver diseases. The increased levels of HMGB1 have been reported in various liver diseases, highlighting that it represents a potential biomarker and druggable target for therapeutic development.Areas covered: This review summarizes the current knowledge on the structure, function, and interacting receptors of HMGB1 and its significance in multiple liver diseases. The latest patented and preclinical studies of HMGB1 inhibitors (antibodies, peptides, and small molecules) for liver diseases are summarized by using the keywords 'HMGB1,' 'HMGB1 antagonist, HMGB1-inhibitor,' 'liver disease' in Web of Science, Google Scholar, Google Patents, and PubMed databases in the year from 2017 to 2023.Expert opinions: In recent years, extensive research on HMGB1-dependent inflammatory signaling has discovered potent inhibitors of HMGB1 to reduce the severity of liver injury. Despite significant progress in the development of HMGB1 antagonists, few of them are approved for clinical treatment of liver-related diseases. Developing safe and effective specific inhibitors for different HMGB1 isoforms and their interaction with receptors is the focus of future research.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"127-140"},"PeriodicalIF":6.6,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140335335","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