Expert Opinion on Therapeutic Patents最新文献_第9页

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

An insight into the last 5-year patents on Porphyromonas gingivalis and Streptococcus mutans, the pivotal pathogens in the oral cavity. 深入了解最近 5 年有关牙龈卟啉单胞菌和变异链球菌（口腔中的主要病原体）的专利情况。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-06-01 Epub Date: 2024-05-20 DOI: 10.1080/13543776.2024.2349739

Bianca Laura Bernardoni, Ilaria D'Agostino, Concettina La Motta, Andrea Angeli

{"title":"An insight into the last 5-year patents on Porphyromonas gingivalis and Streptococcus mutans, the pivotal pathogens in the oral cavity.","authors":"Bianca Laura Bernardoni, Ilaria D'Agostino, Concettina La Motta, Andrea Angeli","doi":"10.1080/13543776.2024.2349739","DOIUrl":"10.1080/13543776.2024.2349739","url":null,"abstract":"Introduction: The oral cavity harbors an extensive array of over 700 microorganisms, forming the most complex biome of the entire human body, with bacterial species being the most abundant. Oral diseases, e.g. periodontitis and caries, are strictly associated with bacterial dysbiosis. Porphyromonas gingivalis and Streptococcus mutans stand out among bacteria colonizing the oral cavity.Areas covered: After a brief overview of the bacterial populations in the oral cavity and their roles in regulating (flora) oral cavity or causing diseases like periodontal and cariogenic pathogens, we focused our attention on P. gingivalis and S. mutans, searching for the last-5-year patents dealing with the proposal of new strategies to fight their infections. Following the PRISMA protocol, we filtered the results and analyzed over 100 applied/granted patents, to provide an in-depth insight into this R&D scenario.Expert opinion: Several antibacterial proposals have been patented in this period, from both chemical - peptides and small molecules - and biological - probiotics and antibodies - sources, along with natural extracts, polymers, and drug delivery systems. Most of the inventors are from China and Korea and their studies also investigated anti-inflammatory and antioxidant effects, being beneficial to oral health through a prophylactic, protective, or curative effect.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"433-463"},"PeriodicalIF":5.4,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140862018","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 trends and challenges to overcome Pseudomonas aeruginosa infections. 克服铜绿假单胞菌感染的最新趋势和挑战。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-06-01 Epub Date: 2024-05-03 DOI: 10.1080/13543776.2024.2348602

Alessandra Ammazzalorso, Arianna Granese, Barbara De Filippis

{"title":"Recent trends and challenges to overcome Pseudomonas aeruginosa infections.","authors":"Alessandra Ammazzalorso, Arianna Granese, Barbara De Filippis","doi":"10.1080/13543776.2024.2348602","DOIUrl":"10.1080/13543776.2024.2348602","url":null,"abstract":"Introduction: Pseudomonas aeruginosa (PA) is a Gram-negative bacterium that can cause a wide range of severe infections in immunocompromised patients. The most difficult challenge is due to its ability to rapidly develop multi drug-resistance. New strategies are urgently required to improve the outcome of patients with PA infections. The present patent review highlights the new molecules acting on different targets involved in the antibiotic resistance.Area covered: This review offers an insight into new potential PA treatment disclosed in patent literature. From a broad search of documents claiming new PA inhibitors, we selected and summarized molecules that showed in vitro and in vivo activity against PA spp. in the period 2020 and 2023. We collected the search results basing on the targets explored.Expert opinion: This review examined the main patented compounds published in the last three years, with regard to the structural novelty and the identification of innovative targets. The main areas of antibiotic resistance have been explored. The compounds are structurally unrelated to earlier antibiotics, characterized by a medium-high molecular weight and the presence of heterocycle rings. Peptides and antibodies have also been reported as potential alternatives to chemical treatment, hereby expanding the therapeutic possibilities in this field.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"493-509"},"PeriodicalIF":5.4,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140862657","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 stimulator of interferon genes agonists (2021 - present). 最新的干扰素基因激动剂刺激剂专利回顾（2021 年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-05-01 Epub Date: 2024-06-13 DOI: 10.1080/13543776.2024.2365409

Guo-Feng Xin, Nan-Nan Chen, Lin-Lin Li, Xue-Chun Liu, Chun-Chen Che, Bei-Duo Wu, Qi-Dong You, Xiao-Li Xu

{"title":"An updated patent review of stimulator of interferon genes agonists (2021 - present).","authors":"Guo-Feng Xin, Nan-Nan Chen, Lin-Lin Li, Xue-Chun Liu, Chun-Chen Che, Bei-Duo Wu, Qi-Dong You, Xiao-Li Xu","doi":"10.1080/13543776.2024.2365409","DOIUrl":"10.1080/13543776.2024.2365409","url":null,"abstract":"Introduction: Stimulator of Interferon Genes (STING) is an innate immune sensor. Activation of STING triggers a downstream response that results in the expression of proinflammatory cytokines (TNF-α, IL-1β) via nuclear factor kappa-B (NF-κB) or the expression of type I interferons (IFNs) via an interferon regulatory factor 3 (IRF3). IFNs can eventually result in promotion of the adaptive immune response including activation of tumor-specific CD8+ T cells to abolish the tumor. Consequently, activation of STING has been considered as a potential strategy for cancer treatment.Areas covered: This article provides an overview on structures and pharmacological data of CDN-like and non-nucleotide STING agonists acting as anticancer agents (January 2021 to October 2023) from a medicinal chemistry perspective. The data in this review come from EPO, WIPO, RCSB PDB, CDDI.Expert opinion: In recent years, several structurally diverse STING agonists have been identified. As an immune enhancer, they are used in the treatment of tumors, which has received extensive attention from scientific community and pharmaceutical companies. Despite the multiple challenges that have appeared, STING agonists may offer opportunities for immunotherapy.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"297-313"},"PeriodicalIF":5.4,"publicationDate":"2024-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141287975","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 estrogen receptor degraders (SERDs) and covalent antagonists (SERCAs): a patent review (July 2021-December 2023). 选择性雌激素受体降解剂（SERDs）和共价拮抗剂（SERCAs）：专利回顾（2021 年 7 月至 2023 年 12 月）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-05-01 Epub Date: 2024-06-12 DOI: 10.1080/13543776.2024.2364803

James S Scott, Teresa C M Klinowska

{"title":"Selective estrogen receptor degraders (SERDs) and covalent antagonists (SERCAs): a patent review (July 2021-December 2023).","authors":"James S Scott, Teresa C M Klinowska","doi":"10.1080/13543776.2024.2364803","DOIUrl":"10.1080/13543776.2024.2364803","url":null,"abstract":"Introduction: Breast cancer is the most frequently diagnosed cancer worldwide. With around 70% of breast cancers expressing the estrogen receptor (ER), molecules capable of antagonizing and degrading ER (SERDs) or covalently binding to and antagonizing ER (SERCAs) are at the forefront of efforts to bring better treatments to patients.Areas covered: This review summarizes patent applications that claim estrogen receptor degraders (SERDs) and covalent antagonists (SERCAs) identified using SciFinder between the period July 2021 to December 2023. A total of 91 new patent applications from 32 different applicants are evaluated with stratification into acidic SERDs, basic SERDs, SERCAs and miscellaneous degraders.Expert opinion: The widespread adoption of fulvestrant in the treatment of ER+ breast cancer continues to stimulate research into orally bioavailable SERDs and SERCAs. A number of molecules have entered clinical development and, although some have been discontinued, a cohort of potential new treatments have generated encouraging efficacy and safety data. Notably, the first example of an oral SERD, elacestrant, has now been approved by the FDA and EMA, providing further encouragement for this class of targeted therapies.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"333-350"},"PeriodicalIF":5.4,"publicationDate":"2024-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141247701","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