Sevki Adem, Azhar Rasul, Saba Riaz, Ayesha Sadiqa, Matloob Ahmad, Muhammad Shahid Nazir, Mudassir Hassan
{"title":"Pyruvate kinase modulators as a therapy target: an updated patent review 2018-2023.","authors":"Sevki Adem, Azhar Rasul, Saba Riaz, Ayesha Sadiqa, Matloob Ahmad, Muhammad Shahid Nazir, Mudassir Hassan","doi":"10.1080/13543776.2024.2403616","DOIUrl":"10.1080/13543776.2024.2403616","url":null,"abstract":"<p><strong>Introduction: </strong>Cancer cells adopt a glycolytic phenotype to fulfill their energy needs in unfavorable conditions. In metabolic rewiring, cancer cells upregulate the expression of glycolytic pathway regulators including glucose transporter 1, hexokinase 2, and PKM2 (pyruvate kinase) into its M2 splice form. Among these regulators, PKM2 plays a major role in metabolic reprogramming and is overexpressed in various diseases, including cancer. Dimerization of PKM2 causes the generation of synthetic precursors from glycolytic intermediates, which are essential for cellular growth and cancer cell proliferation.</p><p><strong>Covered areas: </strong>This article is focused on examining recent patents (2018-2023) on PKM2 activators, inhibitors and their biological and synthesis properties by using the advanced search service of the European Patent Office (EPO). Moreover, other databases including PubMed, Google Scholar and Elsevier were also examined for scientific data. On basis of their chemical structures, PKM2 activators and inhibitors are classified into pyrazole, pyrolidine-pyrazole, phenol, benzoxazine, isoselenazolo-pyridinium, phthalazine, and propiolylamide derivatives.</p><p><strong>Expert opinion: </strong>Activating PKM2 reduces proliferation and development of cells by reducing the quantity of biomolecules needed for cell formation. PKM2 activators and inhibitors are highly effective in treating many cancer pathogens. It is important to find new, more potent and selective molecules for PKM2 activation and inhibition.</p>","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"953-962"},"PeriodicalIF":5.4,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142282772","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}
Zonghui Ma, Cun Zhang, Andrew A Bolinger, Jia Zhou
{"title":"An updated patent review of BRD4 degraders.","authors":"Zonghui Ma, Cun Zhang, Andrew A Bolinger, Jia Zhou","doi":"10.1080/13543776.2024.2400166","DOIUrl":"10.1080/13543776.2024.2400166","url":null,"abstract":"<p><strong>Introduction: </strong>Bromodomain-containing protein 4 (BRD4), an important epigenetic reader, is closely associated with the pathogenesis and development of many diseases, including various cancers, inflammation, and infectious diseases. Targeting BRD4 inhibition or protein elimination with small molecules represents a promising therapeutic strategy, particularly for cancer therapy.</p><p><strong>Areas covered: </strong>The recent advances of patented BRD4 degraders were summarized. The challenges, opportunities, and future directions for developing novel potent and selective BRD4 degraders are also discussed. The patents of BRD4 degraders were searched using the SciFinder and Cortellis Drug Discovery Intelligence database.</p><p><strong>Expert opinion: </strong>BRD4 degraders exhibit superior efficacy and selectivity to BRD4 inhibitors, given their unique mechanism of protein degradation instead of protein inhibition. Excitingly, RNK05047 is now in phase I/II clinical trials, indicating that selective BRD4 protein degradation may offer a viable therapeutic strategy, particularly for cancer. Targeting BRD4 with small-molecule degraders provides a promising approach with the potential to overcome therapeutic resistance for treating various BRD4-associated diseases.</p>","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"929-951"},"PeriodicalIF":5.4,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11427152/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142105968","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Caspase inhibitors: a review on recently patented compounds (2016-2023).","authors":"Shivani Kasana, Shivam Kumar, Preeti Patel, Balak Das Kurmi, Shweta Jain, Sanjeev Sahu, Ankur Vaidya","doi":"10.1080/13543776.2024.2397732","DOIUrl":"10.1080/13543776.2024.2397732","url":null,"abstract":"<p><strong>Introduction: </strong>Caspases are a family of protease enzymes that play a crucial role in apoptosis. Dysregulation of caspase activity has been implicated in various pathological conditions, making caspases an important focus of research in understanding cell death mechanisms and developing therapeutic strategies for diseases associated with abnormal apoptosis.</p><p><strong>Areas covered: </strong>It is a comprehensive review of caspase inhibitors that have been comprising recently granted patents from 2016 to 2023. It includes peptide and non-peptide caspase inhibitors with their application for different diseases.</p><p><strong>Expert opinion: </strong>This review categorizes and analyses recently patented caspase inhibitors on various diseases. Diseases linked to caspase dysregulation, including neurodegenerative disorders, and autoimmune conditions, are highlighted to accentuate the therapeutic relevance of the patented caspase inhibitors. This paper serves as a valuable resource for researchers, clinicians, and pharmaceutical developers seeking an up-to-date understanding of recently patented caspase inhibitors. The integration of recent patented compounds, structural insights, and mechanistic details provides a holistic view of the progress in caspase inhibitor research and its potential impact on addressing various diseases.</p>","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1047-1072"},"PeriodicalIF":5.4,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142105969","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}
{"title":"Patenting perspective of modulators of ClpP endopeptidase: 2019-present","authors":"Zhenyu Wang, Liqing He, Ziheng Fan, Youfu Luo","doi":"10.1080/13543776.2024.2404233","DOIUrl":"https://doi.org/10.1080/13543776.2024.2404233","url":null,"abstract":"ClpP is a highly conserved serine protease that plays a crucial role in maintaining protein homeostasis in both bacterial cells and human mitochondria. Several studies have demonstrated the potenti...","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":"1 1","pages":""},"PeriodicalIF":6.6,"publicationDate":"2024-09-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142269626","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}
{"title":"MEK inhibitors in oncology: a patent review and update (2016 - present)","authors":"Anjali Suryavanshi, Vandana, Yugal Kishor Shukla, Vipul Kumar, Pragya Gupta, Vivek Asati, Debarshi Kar Mahapatra, Raj K. Keservani, Sanmati Kumar Jain, Sanjay Kumar Bharti","doi":"10.1080/13543776.2024.2403634","DOIUrl":"https://doi.org/10.1080/13543776.2024.2403634","url":null,"abstract":"Mitogen-activated protein kinase (MEK) is one of the important components of Ras/Raf/MEK/ERK signaling pathway, transduces signal for cell growth, differentiation, and development. Deregulation of ...","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":"19 1","pages":""},"PeriodicalIF":6.6,"publicationDate":"2024-09-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142265491","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}
Massimiliano Tognolini,Francesca Romana Ferrari,Alfonso Zappia,Carmine Giorgio
{"title":"Ephrin receptor type-A2 (EphA2) targeting in cancer: a patent review (2018-present).","authors":"Massimiliano Tognolini,Francesca Romana Ferrari,Alfonso Zappia,Carmine Giorgio","doi":"10.1080/13543776.2024.2402382","DOIUrl":"https://doi.org/10.1080/13543776.2024.2402382","url":null,"abstract":"INTRODUCTIONEphA2 is a tyrosine kinase receptor and is considered a promising target in cancer. Different approaches are used to target EphA2 receptor, and a lot of preclinical data demonstrate the potential exploitation of this receptor in clinical oncology for diagnosis and cancer therapy, including immunotherapy.AREAS COVEREDIn this review, we have summarized the recent patents involving the EphA2 targeting in cancer. For this aim, we used the patent database Patentscope covering the time period of 2018-present. Preclinical and clinical data of the inventions were considered when published on peer reviewed journals. Moreover, the clinicalTrial.gov identifiers (NCT numbers) were included when available. For an easier and more immediate reading, we classify the patents in different categories, considering the nature (aptamers, small molecules, antibodies, peptides, antigens and chimeric antigen receptors) of the inventions exploiting EphA2 in clinical oncology.EXPERT OPINIONDespite the availability of a plethora of chemically diverse agents, there are no approved anticancer drugs targeting EphA2 yet. However, these intellectual properties, some of which supported by strong preclinical evidence, keep the hope that, after more than 30 years from its discovery, we will finally see the first EphA2 targeting agent approved in clinical oncology.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":"42 1","pages":"1-10"},"PeriodicalIF":6.6,"publicationDate":"2024-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142209570","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}
{"title":"Helicase-primase inhibitors for the treatment of herpes simplex virus infections - patent evaluation of WO2023/225162 from gilead sciences inc.","authors":"Christian Gege,Gerald Kleymann","doi":"10.1080/13543776.2024.2403618","DOIUrl":"https://doi.org/10.1080/13543776.2024.2403618","url":null,"abstract":"Helicase-primase is an interesting target for small molecule therapy of herpes simplex virus (HSV) infections. With amenamevir already approved for varicella-zoster virus and herpes simplex in Japan and with pritelivir's granted breakthrough therapy designation for the treatment of acyclovir-resistant HSV infections in immunocompromised patients, the target has sparked interest in helicase-primase inhibitors (HPIs). Here we analyze the first patent application from Gilead in this field, which pursued a me-too approach combining elements from an old Bayer together with a recent Medshine HPI application (which covers the Phaeno Therapeutics drug candidate HN0037). The asset was contributed to Assembly Biosciences, where it is under development as ABI-1179 at the investigational new drug (IND) enabling stage for high-recurrence genital herpes. A structure proposal for indolinoyl derivative ABI-1179 is presented, showing its potential opportunities and limitations compared to other HPIs.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":"13 1","pages":""},"PeriodicalIF":6.6,"publicationDate":"2024-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142209601","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}
{"title":"SGLT2 inhibitors for the treatment of diabetes: a patent review (2019-23).","authors":"Rahul Baghel, Nikita Chhikara, Pawan Kumar, Akhilesh Kumar Tamrakar","doi":"10.1080/13543776.2024.2379929","DOIUrl":"10.1080/13543776.2024.2379929","url":null,"abstract":"<p><strong>Introduction: </strong>The sodium-glucose co-transporter 2 (SGLT2) inhibitors are FDA-approved class of drugs for diabetes management. They improve glycemic control by inducing glucosuria. Notwithstanding with potent anti-hyperglycemic activity, SGLT2 inhibitors are emerging as drugs with multifaceted therapeutic potential, evidenced for cardioprotective, renoprotective, antihypertensive, and neuroprotective activities. Continuous attempts are being accomplished through structural modification, development of new formulation, or combination with other drugs, to enhance the bioactivity spectrum of SGLT2 inhibitors for better management of diabetes and related complications.</p><p><strong>Areas covered: </strong>This review comprises a summary of patent applications, acquired using the Espacenet Patent Search database, concerning SGLT2 inhibitors from 2019 to 2023, with focus on improving therapeutic potentials in management of diabetes and metabolic complications.</p><p><strong>Expert opinion: </strong>SGLT2 inhibitors have provided an exciting treatment option for diabetes. Originally developed as anti-hyperglycemic agents, SGLT2 inhibitors exert pleiotropic metabolic responses and have emerged as promising antidiabetic agents with cardio-protective and reno-protective activities. Given their distinct therapeutic profile, SGLT2 inhibitors have revolutionized the management of diabetes and associated complications. Emerging evidences on their therapeutic potential against cancer, male reproductive dysfunctions, and neurodegenerative diseases indicate that further research in this field may unfold novel prospective on their plausible use in the management of other chronic conditions.</p>","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"807-823"},"PeriodicalIF":5.4,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141792360","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}
Mohammad Mahboubi-Rabbani, Amir Hossein Abdolghaffari, Mahsa Ghesmati, Ali Amini, Afshin Zarghi
{"title":"Selective COX-2 inhibitors as anticancer agents: a patent review (2018-2023).","authors":"Mohammad Mahboubi-Rabbani, Amir Hossein Abdolghaffari, Mahsa Ghesmati, Ali Amini, Afshin Zarghi","doi":"10.1080/13543776.2024.2373771","DOIUrl":"10.1080/13543776.2024.2373771","url":null,"abstract":"<p><strong>Introduction: </strong>COX-2 is a crucial enzyme in the manufacture of prostaglandins. The enzyme's metabolites might have an important function as regulators of the inflammatory response and other medical conditions such as cancer. Selective COX-2 inhibitors are believed to enhance or reverse the response of cancer chemotherapeutics.</p><p><strong>Areas covered: </strong>This study addresses the chemical structures as well as the antitumor activity of new COX-2 inhibitors produced in the recent five years, aiming to provide an insight into the mechanism of COX-2 induced PGE<sub>2</sub> powerful signal in cancer development.</p><p><strong>Expert opinion: </strong>The significance of selective COX-2 inhibitors as an efficient superfamily of compounds with anti-inflammatory, anti-Alzheimer's, anti-Parkinson's disease, and anticancer properties has piqued the passion of academics in the field of drug development. Long-term usage of selective COX-2 inhibitors, such as celecoxib has been proven in clinical trials to lower the incidence of several human malignancies. Furthermore, celecoxib has the potential to greatly increase the effectiveness of chemotherapy. Our extensive understanding of selective COX-2 inhibitor SAR may aid in the development of safer and more effective selective COX-2 inhibitors as cancer chemopreventive agents. This review focuses on the different structural classes of selective COX-2 inhibitors, with a particular emphasis on their SAR.</p>","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"733-757"},"PeriodicalIF":5.4,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141491528","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}