Expert Opinion on Therapeutic Patents最新文献

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 : 2024-11-04 DOI: 10.1080/13543776.2024.2423004

Özlen Güzel-Akdemir, Atilla Akdemir

引用次数: 0

A patent review of UNC-51-like kinase 1/2 inhibitors (2019-present). UNC-51 样激酶 1/2抑制剂专利回顾（2019 年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-11-04 DOI: 10.1080/13543776.2024.2423010

Zhiqi Zhang, Dejuan Sun, Yueying Yang, Samir Y Abbas, Hua Li, Lixia Chen

{"title":"A patent review of UNC-51-like kinase 1/2 inhibitors (2019-present).","authors":"Zhiqi Zhang, Dejuan Sun, Yueying Yang, Samir Y Abbas, Hua Li, Lixia Chen","doi":"10.1080/13543776.2024.2423010","DOIUrl":"10.1080/13543776.2024.2423010","url":null,"abstract":"Introduction: UNC-51-like kinase 1/2 (ULK1/2) are serine/threonine kinases that play a crucial role in autophagy activation and maintaining cellular homeostasis. Given their broad physiological relevance, ULK1/2 are candidate targets for treating various diseases. In recent years, ULK1/2 inhibitors have made significant progress, and the highly potent ULK1/2 inhibitors have entered clinical trials.Area covered: This review aims to provide an updated analysis of patents describing ULK1/2 inhibitors and their potential therapeutic applications that were disclosed between 2019 and 2024.Expert opinion: Due to their crucial role in various diseases, the invention of small-molecule drugs targeting ULK1/2 is particularly important, especially in cancer treatment. Despite the great success of ULK1/2 inhibitors development, ULK1/2 inhibitors are ATP competitive inhibitors of aminopyrimidines currently, and most ULK1/2 inhibitors are still in the preclinical research stage, with only DCC-3116 entered clinical research. Therefore, developing highly selective ULK1/2 inhibitors with low side effects and high bioavailability remains a challenging and promising research direction.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-11-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142521507","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

Menin-MLL protein-protein interaction inhibitors: a patent review (2021-present). Menin-mll 蛋白-蛋白相互作用抑制剂：专利回顾（2021 年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-11-03 DOI: 10.1080/13543776.2024.2422380

Fang Wang, Zhe Yang, Yujie Wu, Huanrong Bai, Minhang Xin

{"title":"Menin-MLL protein-protein interaction inhibitors: a patent review (2021-present).","authors":"Fang Wang, Zhe Yang, Yujie Wu, Huanrong Bai, Minhang Xin","doi":"10.1080/13543776.2024.2422380","DOIUrl":"10.1080/13543776.2024.2422380","url":null,"abstract":"Introduction: Acute leukemia harboring rearrangement of the Mixed lineage leukemia (MLL) and/or mutation of the nucleophosmin is a type of poorly prognostic and highly malignant leukemia which is extremely difficult to treat. Blocking the protein-protein interaction between Menin and MLL is a strategic approach for treating leukemias, as a new direction for drug discovery. Many biotech and pharmaceutical companies made great efforts to this drug development field, and a large number of small molecular Menin-MLL PPI inhibitors were reported during the recent three years.Areas covered: This review is to mainly summarize the Menin-MLL PPI inhibitors reported in the recent three years' patents.Expert opinion: Although the past 12 years have witnessed the progress of the Menin-MLL PPI inhibitors in the treatment of acute leukemia, especially for leukemia harboring rearranged KMT2A and/or mutated NPM1, recent studies showed Menin-MLL PPI inhibitors suffered from new issues such as toxicity, acquired resistance, and homogenization. Therefore, new drug discovery strategies should be considered in advance. The expert opinion was proposed from several aspects, such as developing diverse chemical structures, discovering covalent inhibitors, designing small molecular PROTACs, and targeting the amino acids mutations for next-generation inhibitors.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-11-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142497790","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 lactate dehydrogenase inhibitors (2014-present). 乳酸脱氢酶抑制剂专利回顾（2014 年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-11-01 Epub Date: 2024-10-06 DOI: 10.1080/13543776.2024.2412575

Giulia Bononi, Valeria Di Bussolo, Tiziano Tuccinardi, Filippo Minutolo, Carlotta Granchi

{"title":"A patent review of lactate dehydrogenase inhibitors (2014-present).","authors":"Giulia Bononi, Valeria Di Bussolo, Tiziano Tuccinardi, Filippo Minutolo, Carlotta Granchi","doi":"10.1080/13543776.2024.2412575","DOIUrl":"10.1080/13543776.2024.2412575","url":null,"abstract":"Introduction: Lactate dehydrogenase (LDH) is a key enzyme in glycolysis responsible for the conversion of pyruvate into lactate and vice versa. Lactate plays a crucial role in tumor progression and metastasis; therefore, reducing lactate production by inhibiting LDH is considered an optimal strategy to tackle cancer. Additionally, dysregulation of LDH activity is correlated with other pathologies, such as cardiovascular and neurodegenerative diseases as well as primary hyperoxaluria, fibrosis and cryptosporidiosis. Hence, LDH inhibitors could serve as potential therapeutics for treating these pathological conditions.Areas covered: This review covers patents published since 2014 up to the present in the Espacenet database, concerning LDH inhibitors and their potential therapeutic applications.Expert opinion: Over the past 10 years, different compounds have been identified as LDH inhibitors. Some of them are derived from the chemical optimization of already known LDH inhibitors (e.g. pyrazolyl derivatives, quinoline 3-sulfonamides), while others belong to newly identified chemical classes of LDH inhibitors. LDH inhibition has proven to be a promising therapeutic strategy not only for preventing human pathologies, but also for treating animal diseases. The published patents from both academia and the pharmaceutical industry highlight the persistent high interest of the scientific community in developing efficient LDH inhibitors.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142364978","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 challenging inhibition of Aldose Reductase for the treatment of diabetic complications: a 2019-2023 update of the patent literature. 抑制醛糖还原酶治疗糖尿病并发症的挑战：2019-2023 年专利文献更新。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-11-01 Epub Date: 2024-10-11 DOI: 10.1080/13543776.2024.2412573

Bianca Laura Bernardoni, Ilaria D'Agostino, Fabio Scianò, Concettina La Motta

{"title":"The challenging inhibition of Aldose Reductase for the treatment of diabetic complications: a 2019-2023 update of the patent literature.","authors":"Bianca Laura Bernardoni, Ilaria D'Agostino, Fabio Scianò, Concettina La Motta","doi":"10.1080/13543776.2024.2412573","DOIUrl":"10.1080/13543776.2024.2412573","url":null,"abstract":"Introduction: Aldose reductase (AKR1B1, EC: 1.1.1.21) is a recognized target for the treatment of long-term diabetic complications since its activation in hyperglycemia and role in the polyol pathway. In particular, the tissue-specificity of AKR1B1 expression makes the design of the traditional Aldose Reductase Inhibitors (ARIs) and the more recent Aldose Reductase Differential Inhibitors (ARDIs) exploitable strategies to treat pathologies resulting from diabetic conditions.Areas covered: A brief overview of the roles and functions of AKR1B1 along with known ARIs and ARDIs was provided. Then, the design of the latest inhibitors in the scientific scenario was discussed, aiming at introducing the research achievement in the field of intellectual properties. Patents dealing with AKR1B1 and diabetes filed in the 2019-2023 period were collected and analyzed. Reaxys, Espacenet, SciFindern, and Google Patents were surveyed, using 'aldose reductase' and 'inhibitor' as the reference keywords. The search results were then filtered by PRISMA protocol, thus obtaining 16 records to review.Expert opinion: Although fewer in number than in the early 2000s, patent applications are still being filed in the field of ARIs, with a large number of Chinese inventors reporting new synthetic ARIs in favor of the repositioning approach.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142371425","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

Therapeutic compounds targeting interleukin-1 receptor-associated kinase 4 (IRAK4): an updated patent review (2019 to present). 针对白细胞介素-1受体相关激酶4（IRAK4）的治疗化合物：最新专利回顾（2019年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-11-01 Epub Date: 2024-11-05 DOI: 10.1080/13543776.2024.2406825

Fei Xiang

{"title":"Therapeutic compounds targeting interleukin-1 receptor-associated kinase 4 (IRAK4): an updated patent review (2019 to present).","authors":"Fei Xiang","doi":"10.1080/13543776.2024.2406825","DOIUrl":"10.1080/13543776.2024.2406825","url":null,"abstract":"Background: It is more than two decades since IRAK4, a promising target for therapies against various medical conditions, was first reported, but no compounds targeting this enzyme are active on the market or under late-stage clinical development. So it is necessary to continue exploring new and/or improved chemotypes for IRAK4-targeting compounds, to which updated patent reviews are supposed to be of considerable contribution.Areas covered: PCT patents claiming IRAK4-targeting compounds and published through 2019 to present were retrieved, screened and reviewed for the title compounds disclosed therein, where chemotype-specific strategies were adopted for the said reviewing process. Included patents featuring non-Protac compounds were described in terms of generic formulas and variable-indicated moieties of the title compounds, as well as selected title compounds and relevant prior documents. Included patents featuring Protac-based compounds were described in terms of general examples of IRAK-binding moieties and ligase-binding moieties, as well as the presence of conventional linker types. Insights were finally extracted from the patent review.Expert opinion: The last five years has seen a steady increase in the number of PCT patents claiming IRAK4-targeting therapeutic compounds, with some of them being based on new chemotypes and/or discovered by new organizations as potential new players.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142344415","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

Ectonucleotidase inhibitors: an updated patent review (2017-2023). 外显子核苷酸酶抑制剂：最新专利综述（2017-2023 年）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-11-01 Epub Date: 2024-10-30 DOI: 10.1080/13543776.2024.2423023

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

{"title":"Ectonucleotidase inhibitors: an updated patent review (2017-2023).","authors":"Jamshed Iqbal, Sehrish Bano, Imtiaz Ali Khan, Jean Sévigny, Qing Huang","doi":"10.1080/13543776.2024.2423023","DOIUrl":"10.1080/13543776.2024.2423023","url":null,"abstract":"Introduction: The main enzymes that hydrolyzes nucleotides at the cell surface are nucleoside triphosphate diphosphohydrolases (NTPDases), ecto-nucleotide pyrophosphatases/phosphodiesterases (ENPPs), alkaline phosphatases (APs) and ecto-5'- nucleotidase (e5'NT, CD73) and by regulating the concentration of nucleotides at the cell surface, these enzymes have the potential to affect various conditions such as fibrosis, cancer metastasis, pruritus, inflammation, and autoimmune diseases. Thus, they represent a prospective therapeutic target.Area covered: A number of molecules, including nucleoside/nucleotide and non-nucleoside analogues, and bicyclic compounds, have shown strong potential as ectonucleotidase inhibitors. This review covers the chemistry and clinical uses of ectonucleotidase inhibitors patented between 2017 and 2023.Expert opinion: By binding to their specific P1 and P2 receptors at the cell surface, nucleosides and nucleotides regulate a number of pathophysiological events such as inflammation, fibrosis, cancer, and autoimmune diseases. Interestingly, these nucleotides can be hydrolyzed to nucleosides by several cell surface enzymes called ectonucleotidases. The development of small molecules that modulate ectonucleotidase activity is, therefore, of therapeutic value. This review provides valuable insights into recent advancements, including combination therapy and enhanced selectivity, which are poised to shape the future of ectonucleotidase inhibition through a comprehensive analysis of patents.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142497789","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

Trispecific anti-CD3/BCMA/CD38 antibodies for multiple myeloma: a patent evaluation of US20240132615. 用于多发性骨髓瘤的三特异性抗 CD3/BCMA/CD38 抗体：US20240132615 的专利评估。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-10-29 DOI: 10.1080/13543776.2024.2423018

Cindy Bandala, Donaciano Flores-Robles, Pavel Sierra-Martínez, Alejandro Millán-Vega, Eunice Ruíz González, Martin Perez-Santos

引用次数: 0

Coumarin derivatives as therapeutic candidates: a review of their updated patents (2017-present). 作为候选疗法的香豆素衍生物：其最新专利回顾（2017 年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-10-28 DOI: 10.1080/13543776.2024.2419827

Kalfagianni Malamati-Konstantina, Hadjipavlou-Litina Dimitra

{"title":"Coumarin derivatives as therapeutic candidates: a review of their updated patents (2017-present).","authors":"Kalfagianni Malamati-Konstantina, Hadjipavlou-Litina Dimitra","doi":"10.1080/13543776.2024.2419827","DOIUrl":"https://doi.org/10.1080/13543776.2024.2419827","url":null,"abstract":"Introduction: Coumarins constitute a family of heterocyclic compounds that have been extensively studied as possible drugs in the pharmaceutical research to support human health.Areas covered in this review: A survey of patent publications from 2017 to mid-2024, taken from Google Scholar, Web of Science, Scopus, or PubMed analyzes coumarins and their derivatives. It covers synthetic methods, hybridization techniques, and assessments of their biological effects in laboratory and biological studies, such as cytotoxic, antitumor, anticancer, cardiovascular, anti-atheromatic, antidiabetic, anti-asthmatic and antioxidant properties. Additionally, it presents and discusses several pharmaceutical applications for treatment and compositions involving these compounds. Structural activity relationships and mechanism of action are presented and discussed.Expert opinion: The authors suggest that (i) numerous areas of biology-pharmacology need to be considered: selectivity, in vivo studies, toxicity, bioavailability and drug-likeness, the mechanism of action in animals and humans, evaluation of more efficient and selective biological tests; (ii) synthetic technique outbalance in the discovery and production of coumarins with greater selectivity. Their clinical evaluation will be critical to assess therapeutic utility. The coumarins, for which extended biological investigations confirmed their mechanism of action, can serve as lead or hit structures for the design of new libraries with more potent molecules.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-10-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142497788","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

An updated patent review of SOS1 inhibitors (2022-present). SOS1 抑制剂最新专利回顾（2022 年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-10-25 DOI: 10.1080/13543776.2024.2419825

Guizhen Zhou, Chuan Zhou, Xinyi Ma, Jiahang Xu, Zehui Zhou, Tianfeng Xu, Mingyue Zheng, Sulin Zhang

{"title":"An updated patent review of SOS1 inhibitors (2022-present).","authors":"Guizhen Zhou, Chuan Zhou, Xinyi Ma, Jiahang Xu, Zehui Zhou, Tianfeng Xu, Mingyue Zheng, Sulin Zhang","doi":"10.1080/13543776.2024.2419825","DOIUrl":"10.1080/13543776.2024.2419825","url":null,"abstract":"Introduction: SOS1 is a crucial guanine nucleotide exchange factor for KRAS. It facilitates the transition of KRAS from inactive GDP-bound state to active GTP-bound state. The activation of KRAS triggers downstream signaling pathways, promoting tumor initiation and progression. Inhibiting SOS1 to prevent KRAS activation is an effective strategy for treating tumors driven by KRAS.Areas covered: This review identified patents claiming to be SOS1 inhibitors or SOS1-KRAS interaction modulators published between January 2022 and June 2024 using Cortellis Drug Discovery Intelligence. A total of 15 patent applications from 5 different applicants were assessed.Expert opinions: In KRAS-driven tumors, inhibiting SOS1 significantly affect cell proliferation and migration by modulating the RAS/MAPK and PI3K/AKT/mTOR signaling pathways. Since 2022, numerous patents for SOS1 inhibitors have been published. The majority of SOS1 inhibitors are currently in the preclinical phase of development, with only a few progressing to clinical trials. However, these inhibitors face significant challenges in clinical studies, including limited efficacy of monotherapies, safety concerns, and the necessity to enhance PK properties. Despite their excellent in vitro performance, SOS1 inhibitors must address issues related to safety, pharmacokinetics, and pharmacodynamics in clinical applications.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142461593","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