Expert Opinion on Therapeutic Patents最新文献_第5页

Trends in covalent drug discovery: a 2020-23 patent landscape analysis focused on select covalent reacting groups (CRGs) found in FDA-approved drugs. 共价药物发现的趋势：2020-23 年专利状况分析，重点关注 FDA 批准药物中发现的部分共价反应基团 (CRG)。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-10-01 Epub Date: 2024-09-11 DOI: 10.1080/13543776.2024.2400175

Jan Felix Scholtes, Cristobal Alhambra, Philip A Carpino

{"title":"Trends in covalent drug discovery: a 2020-23 patent landscape analysis focused on select covalent reacting groups (CRGs) found in FDA-approved drugs.","authors":"Jan Felix Scholtes, Cristobal Alhambra, Philip A Carpino","doi":"10.1080/13543776.2024.2400175","DOIUrl":"10.1080/13543776.2024.2400175","url":null,"abstract":"Introduction: Covalent drugs contain electrophilic groups that can react with nucleophilic amino acids located in the active sites of proteins, particularly enzymes. Recently, there has been considerable interest in using covalent drugs to target non-catalytic amino acids in proteins to modulate difficult targets (i.e. targeted covalent inhibitors). Covalent compounds contain a wide variety of covalent reacting groups (CRGs), but only a few of these CRGs are present in FDA-approved covalent drugs.Areas covered: This review summarizes a 2020-23 patent landscape analysis that examined trends in the field of covalent drug discovery around targets and organizations. The analysis focused on patent applications that were submitted to the World International Patent Organization and selected using a combination of keywords and structural searches based on CRGs present in FDA-approved drugs.Expert opinion: A total of 707 patent applications from >300 organizations were identified, disclosing compounds that acted at 71 targets. Patent application counts for five targets accounted for ~63% of the total counts (i.e. BTK, EGFR, FGFR, KRAS, and SARS-CoV-2 Mpro). The organization with the largest number of patent counts was an academic institution (Dana-Farber Cancer Institute). For one target, KRAS G12C, the discovery of new drugs was highly competitive (>100 organizations, 186 patent applications).","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"843-861"},"PeriodicalIF":5.4,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142105970","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

Pyruvate kinase modulators as a therapy target: an updated patent review 2018-2023. 作为治疗靶点的丙酮酸激酶调节剂：2018-2023年最新专利回顾。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-10-01 Epub Date: 2024-09-20 DOI: 10.1080/13543776.2024.2403616

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":"Introduction: 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.Covered areas: 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.Expert opinion: 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.","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}

引用次数: 0

An updated patent review of BRD4 degraders. BRD4 降解剂的最新专利回顾。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-10-01 Epub Date: 2024-09-04 DOI: 10.1080/13543776.2024.2400166

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":"Introduction: 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.Areas covered: 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.Expert opinion: 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.","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}

引用次数: 0

Caspase inhibitors: a review on recently patented compounds (2016-2023). Caspase抑制剂：最新专利化合物综述（2016-2023年）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-10-01 Epub Date: 2024-08-29 DOI: 10.1080/13543776.2024.2397732

Shivani Kasana, Shivam Kumar, Preeti Patel, Balak Das Kurmi, Shweta Jain, Sanjeev Sahu, Ankur Vaidya

{"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":"Introduction: 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.Areas covered: 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.Expert opinion: 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.","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}

引用次数: 0

Correction. 更正。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-09-27 DOI: 10.1080/13543776.2024.2410095

引用次数: 0

Patenting perspective of modulators of ClpP endopeptidase: 2019-present ClpP内肽酶调节剂的专利前景：2019年至今

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-09-16 DOI: 10.1080/13543776.2024.2404233

Zhenyu Wang, Liqing He, Ziheng Fan, Youfu Luo

引用次数: 0

MEK inhibitors in oncology: a patent review and update (2016 - present) 肿瘤学中的 MEK 抑制剂：专利回顾与更新（2016 年至今）

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-09-14 DOI: 10.1080/13543776.2024.2403634

Anjali Suryavanshi, Vandana, Yugal Kishor Shukla, Vipul Kumar, Pragya Gupta, Vivek Asati, Debarshi Kar Mahapatra, Raj K. Keservani, Sanmati Kumar Jain, Sanjay Kumar Bharti

引用次数: 0

Ephrin receptor type-A2 (EphA2) targeting in cancer: a patent review (2018-present). 癌症中的Ephrin受体A2型（EphA2）靶向治疗：专利回顾（2018年至今）。

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-09-11 DOI: 10.1080/13543776.2024.2402382

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}

引用次数: 0

Helicase-primase inhibitors for the treatment of herpes simplex virus infections - patent evaluation of WO2023/225162 from gilead sciences inc. 用于治疗单纯疱疹病毒感染的螺旋酶-primase 抑制剂--对吉利德科学公司的 WO2023/225162 的专利评估。

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-09-11 DOI: 10.1080/13543776.2024.2403618

Christian Gege,Gerald Kleymann

引用次数: 0

SGLT2 inhibitors for the treatment of diabetes: a patent review (2019-23). 用于治疗糖尿病的 SGLT2 抑制剂：专利回顾（2019-23）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2024-09-01 Epub Date: 2024-08-02 DOI: 10.1080/13543776.2024.2379929

Rahul Baghel, Nikita Chhikara, Pawan Kumar, Akhilesh Kumar Tamrakar

{"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":"Introduction: 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.Areas covered: 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.Expert opinion: 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.","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}

引用次数: 0