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

A patent review on hypoxia-inducible factor (HIF) modulators (2021-2023). 缺氧诱导因子 (HIF) 调节剂专利审查（2021-2023 年）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-08-01 Epub Date: 2024-06-19 DOI: 10.1080/13543776.2024.2368739

Jiaming Liu, Yinli Gao, Xiaojin Zhang

{"title":"A patent review on hypoxia-inducible factor (HIF) modulators (2021-2023).","authors":"Jiaming Liu, Yinli Gao, Xiaojin Zhang","doi":"10.1080/13543776.2024.2368739","DOIUrl":"10.1080/13543776.2024.2368739","url":null,"abstract":"Introduction: Hypoxia-inducible factor (HIF) is a central regulatory factor in detecting and adapting to cellular oxygen stress. Dysregulation of HIF is associated with various human diseases. Seven HIF modulators, including six prolyl hydroxylase (PHD) inhibitors and one HIF-2α inhibitor, have already been approved for the treatment of renal anemia and cancer, respectively.Areas covered: This review summarizes HIF modulators patented in the 2021-2023 period. This review provides an overview of HIF downregulators, including HIF-1α inhibitors, HIF-2α inhibitors, and HIF-2α degraders, as well as HIF upregulators, including PHD, FIH, and VHL inhibitors, and HIF-2α and HIF-3α agonists.Expert opinion: Efforts should be made to address the adverse clinical effects associated with approved HIF-modulating drugs, including PHD inhibitors and HIF-2α inhibitors. Identification of the specific buried cavity in the HIF-2α and an opened pocket in HIF-3α offer an avenue for designing novel modulators for HIF-2α or HIF-3α. Given the similarities observed in the binding cavities of HIF-2α and HIF-3α, it should be considered whether the approved HIF-2α inhibitors also inhibit HIF-3α. A comprehensive understanding of the HIF signaling pathway biology would lead to the development of novel small-molecule HIF modulators as innovative therapeutic approaches for a wide range of human diseases.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"651-664"},"PeriodicalIF":5.4,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141316960","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 on PD-1/PD-L1 antagonists (2022-present). PD-1/PD-L1 拮抗剂最新专利回顾（2022 年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-08-01 Epub Date: 2024-06-25 DOI: 10.1080/13543776.2024.2368237

Wiktor Uzar, Beata Kaminska, Hubert Rybka, Lukasz Skalniak, Katarzyna Magiera-Mularz, Radoslaw Kitel

{"title":"An updated patent review on PD-1/PD-L1 antagonists (2022-present).","authors":"Wiktor Uzar, Beata Kaminska, Hubert Rybka, Lukasz Skalniak, Katarzyna Magiera-Mularz, Radoslaw Kitel","doi":"10.1080/13543776.2024.2368237","DOIUrl":"10.1080/13543776.2024.2368237","url":null,"abstract":"Introduction: PD-L1, via its interactions with PD-1, constitutes a key immune checkpoint that allows cancer cells to escape immune surveillance. Targeting PD-1/PD-L1 with monoclonal antibodies (mAbs) led to spectacular success in clinical oncology. However, the inherent limitations of mAbs and increasing findings about immune-related adverse events (iRAEs) prompted intense research in the field of small-molecule inhibitors of PD-L1.Areas covered: This review covers inhibitors of PD-L1 reported in patents published in the online databases of the World Intellectual Property Organization and European Patent Office in the 2022-2023 period. This review provides a landscape of available inhibitors, including their chemical structures, activity, and stage of development.Expert opinion: Small-molecule inhibitors impairing PD-L1/PD-1 interaction represent an attractive alternative to mAbs. In recent years, the field of small-molecule and macrocyclic inhibitors targeting PD-L1 has grown rapidly. The majority (if not all) of small-molecule inhibitors developed recently, similarly to their predecessors, act through a dimerization mechanism of PD-L1, followed by its internalization into the cytosol. In contrast, macrocyclic peptides act purely through a competition mechanism known as protein-protein interaction inhibitors. The ongoing clinical trials should ultimately reveal which strategy has real clinical potential and may complement or even replace mAbs-based therapies.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"627-650"},"PeriodicalIF":5.4,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141431704","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

Anticancer drugs: where are we now? 抗癌药物：我们现在在哪里？

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-07-01 Epub Date: 2024-05-15 DOI: 10.1080/13543776.2024.2353625

Giuseppina De Simone, Claudiu T Supuran

引用次数: 0

Kinase inhibitors: 20 years of success and many new challenges and recent trends in their patents. 激酶抑制剂：20 年的成功经验、许多新的挑战以及其专利的最新趋势。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-07-01 Epub Date: 2024-05-24 DOI: 10.1080/13543776.2024.2355247

Mourad A M Aboul-Soud, Yazeed A Al-Sheikh, Hazem K Ghneim, Claudiu T Supuran, Fabrizio Carta

{"title":"Kinase inhibitors: 20 years of success and many new challenges and recent trends in their patents.","authors":"Mourad A M Aboul-Soud, Yazeed A Al-Sheikh, Hazem K Ghneim, Claudiu T Supuran, Fabrizio Carta","doi":"10.1080/13543776.2024.2355247","DOIUrl":"10.1080/13543776.2024.2355247","url":null,"abstract":"Introduction: Protein kinases (PKs) play key roles in cellular signaling and regulation cascades and therefore are listed among the most investigated enzymes with the intent to develop drugs that are able to modulate their catalytic features. Specifically, PKs are involved in chronic diseases of large impact in the society such as cancers and neurodegeneration. Since the approval of Fasudil for the management of cerebral vasospasm, frantic efforts are currently ongoing for the development of selective PK-modulating agents.Areas covered: A selection of the most relevant patents in the European Patent Office for biomedical innovation and/or industrial development covering the years 2020-2023 on PK modulators either of the antibody and small-molecule type is reported. In addition to the examined patents, we also reported the contributions claiming the use of antibody-targeted PKs for lab bench identification kits.Expert opinion: The field of PK modulators for biomedical purposes is particularly crowded with contributions, making it rich in valuable information for the development of potential drugs. An emerging frontier is represented by PK activators that aims to complement the use of PK inhibitors with the final intent of finely adjusting any PK-related disruption responsible for triggering any disease.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"583-592"},"PeriodicalIF":5.4,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141086879","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

Patented Farnesoid X receptor modulators: a review (2019 - present). 已获专利的法尼类固醇 X 受体调节剂：综述（2019 年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-07-01 Epub Date: 2024-02-26 DOI: 10.1080/13543776.2024.2314296

Antimo Gioiello, Emiliano Rosatelli, Bruno Cerra

{"title":"Patented Farnesoid X receptor modulators: a review (2019 - present).","authors":"Antimo Gioiello, Emiliano Rosatelli, Bruno Cerra","doi":"10.1080/13543776.2024.2314296","DOIUrl":"10.1080/13543776.2024.2314296","url":null,"abstract":"Introduction: The Farnesoid X receptor (FXR) is a key transcription factor that is involved in the bile acid signaling network. The modulation of the FXR activity influences glucose and lipid homeostasis, reduces obesity and insulin resistance, as well as it regulates the pathogenesis of inflammatory and metabolic disorders. FXR ligands have therefore emerged in drug discovery as promising therapeutic agents for the prevention and treatment of gastrointestinal and liver diseases, including cancer.Areas covered: Recent advances in the field of FXR modulators are reviewed, with a particular attention on patent applications filed in the past 5 years related to both the discovery and development of FXR targeting drugs.Expert opinion: FXR agonists have proven their efficacy and safety in humans and have shown a significant potential as clinical agents to treat metabolic and inflammatory associated conditions. However, several challenges, including adverse events such as pruritus, remain to be solved. Current studies aim to gain insights into the pathophysiological mechanisms by which FXR regulates metabolism and inflammation in terms of tissue/organ/isoform-specificity, post-translational modifications and coregulatory proteins, on the route of novel, improved FXR modulators.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"547-564"},"PeriodicalIF":5.4,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139680972","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

Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) in cancer: a patent review. 癌症中的烟酰胺磷酸核糖转移酶（NAMPT）抑制：专利回顾。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-07-01 Epub Date: 2024-06-13 DOI: 10.1080/13543776.2024.2367006

Massimiliano Gasparrini, Simone Giovannuzzi, Alessio Nocentini, Nadia Raffaelli, Claudiu T Supuran

{"title":"Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) in cancer: a patent review.","authors":"Massimiliano Gasparrini, Simone Giovannuzzi, Alessio Nocentini, Nadia Raffaelli, Claudiu T Supuran","doi":"10.1080/13543776.2024.2367006","DOIUrl":"10.1080/13543776.2024.2367006","url":null,"abstract":"Introduction: Nicotinamide phosphoribosyltransferase (NAMPT) is the rate-limiting enzyme in the biosynthesis of nicotinamide adenine dinucleotide (NAD) from nicotinamide. In addition to its role as essential redox cofactor, NAD also functions as a substrate for NAD-consuming enzymes, regulating multiple cellular processes such as DNA repair and gene expression, fundamental to sustain energetic needs for tumor growth. In this sense, NAMPT over-expression represents a common strategy that several tumor types adopt to sustain NAD production. In addition to its enzymatic role, NAMPT behaves as cytokine-like protein with pro-inflammatory function. Increasing evidence demonstrated that NAMPT inhibition represents a promising anti-cancer strategy to deplete NAD and impair cellular metabolism in cancer conditions.Areas covered: By using Espacenet, we collected the patents which identified new molecules, compounds, formulations and methods able to inhibit NAMPT from 2007 to date.Expert opinion: Most of the collected patents focused the attention on the ability of different compounds to inhibit the enzymatic activity of NAMPT, lacking other important aspects related to the extracellular role of NAMPT and the ability of alternative enzymes to counteract NAMPT-mediated NAD depletion. It is necessary to consider also these aspects to promote novel strategies and create novel inhibitors and molecules useful as anti-cancer compounds.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"565-582"},"PeriodicalIF":5.4,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141300418","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

Recent developments of agents targeting Vibrio cholerae: patents and literature data. 针对霍乱弧菌的制剂的最新发展：专利和文献数据。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-06-01 Epub Date: 2024-03-11 DOI: 10.1080/13543776.2024.2327305

Francesco Melfi, Simone Carradori, Noemi Mencarelli, Cristina Campestre, Arianna Granese, Mattia Mori

{"title":"Recent developments of agents targeting Vibrio cholerae: patents and literature data.","authors":"Francesco Melfi, Simone Carradori, Noemi Mencarelli, Cristina Campestre, Arianna Granese, Mattia Mori","doi":"10.1080/13543776.2024.2327305","DOIUrl":"10.1080/13543776.2024.2327305","url":null,"abstract":"Introduction: Vibrio cholerae bacteria cause an infection characterized by acute diarrheal illness in the intestine. Cholera is sustained by people swallowing contaminated food or water. Even though symptoms can be mild, if untreated disease becomes severe and life-threatening, especially in low-income countries.Areas covered: After a description of the most recent literature on the pathophysiology of this infection, we searched for patents and literature articles following the PRISMA guidelines, filtering the results disclosed from 2020 to present. Moreover, some innovative molecular targets (e.g., carbonic anhydrases) and pathways to counteract this rising problem were also discussed in terms of design, structure-activity relationships and structural analyses.Expert opinion: This review aims to cover and analyze the most recent advances on the new druggable targets and bioactive compounds against this fastidious pathogen, overcoming the use of old antibiotics which currently suffer from high resistance rate.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"415-432"},"PeriodicalIF":5.4,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140039074","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

Photodynamic therapy alone or in combination to counteract bacterial infections. 单独或联合使用光动力疗法来对抗细菌感染。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-06-01 Epub Date: 2024-03-11 DOI: 10.1080/13543776.2024.2327308

Sébastien Clément, Jean-Yves Winum

{"title":"Photodynamic therapy alone or in combination to counteract bacterial infections.","authors":"Sébastien Clément, Jean-Yves Winum","doi":"10.1080/13543776.2024.2327308","DOIUrl":"10.1080/13543776.2024.2327308","url":null,"abstract":"Introduction: Antibacterial photodynamic therapy presents a promising alternative to antibiotics, with potential against multidrug-resistant bacteria, offering broad-spectrum action, reduced resistance risk, and improved tissue selectivity.Areas covered: This manuscript reviews patent literature in the field of antibacterial photodynamic therapy through the period of 2019-2023. All data are from the US and European patent databases and SciFinder.Expert opinion: Antibacterial photodynamic therapy (PDT) is an appealing approach for treating bacterial infections, especially biofilm-related ones, by releasing reactive oxygen species (ROS) upon light activation. Its success is driven by a growing variety of photosensitizers (PSs) with tailored properties, like water solubility, controllable surface charge, and ROS generation efficiency. Among them, Aggregation Induced Emission (AIE)-type PSs are promising, demonstrating enhanced efficacy when aggregated in biological environments. However, the penetration of pristine PSs into bacterial biofilms within deep tissues or complex anatomical regions is limited, reducing their antibacterial effectiveness. To address this, nanotechnology has been integrated into antibacterial PDT to synthesize various nano-PSs. This adaptability allows seamless integration with other antimicrobial treatments, offering a comprehensive approach to combat localized infections, especially in dentistry and dermatology. By combining PSs with complementary therapies, antibacterial PDT offers a multifaceted strategy for effective microbial control and management.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"401-414"},"PeriodicalIF":5.4,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140027792","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

Fighting antibacterial drug resistance. 抗击抗菌药耐药性

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-06-01 Epub Date: 2024-06-14 DOI: 10.1080/13543776.2024.2367940

Claudiu T Supuran

引用次数: 0

Management of Neisseria gonorrhoeae infection: from drug resistance to drug repurposing. 淋病奈瑟菌感染的管理：从耐药性到药物再利用。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-06-01 Epub Date: 2024-06-14 DOI: 10.1080/13543776.2024.2367005

Luigi Pisano, Simone Giovannuzzi, Claudiu T Supuran

{"title":"Management of Neisseria gonorrhoeae infection: from drug resistance to drug repurposing.","authors":"Luigi Pisano, Simone Giovannuzzi, Claudiu T Supuran","doi":"10.1080/13543776.2024.2367005","DOIUrl":"10.1080/13543776.2024.2367005","url":null,"abstract":"Introduction: Neisseria gonorrhoeae is a common sexually transmitted disease connected with extensive drug resistance to many antibiotics. Presently, only expanded spectrum cephalosporins (ceftriaxone and cefixime) and azithromycin remain useful for its management.Areas covered: New chemotypes for the classical antibiotic drug target gyrase/topoisomerase IV afforded inhibitors with potent binding to these enzymes, with an inhibition mechanism distinct from that of fluoroquinolones, and thus less prone to mutations. The α-carbonic anhydrase from the genome of this bacterium (NgCAα) was also validated as an antibacterial target.Expert opinion: By exploiting different subunits from the gyrase/topoisomerase IV as well as new chemotypes, two new antibiotics reached Phase II/III clinical trials, zoliflodacin and gepotidacin. They possess a novel inhibition mechanism, binding in distinct parts of the enzyme compared to the fluoroquinolones. Other chemotypes with inhibitory activity in these enzymes were also reported. NgCAα inhibitors belonging to a variety of classes were obtained, with several sulfonamides showing MIC values in the range of 0.25-4 µg/mL and significant activity in animal models of this infection. Acetazolamide and similar CA inhibitors might thus be repurposed as antiinfectives. The scientific/patent literature has been searched for on PubMed, ScienceDirect, Espacenet, and PatentGuru, from 2016 to 2024.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"511-524"},"PeriodicalIF":5.4,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141295865","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