Expert Opinion on Therapeutic Patents最新文献_第2页

P2Y₁₂R antagonists in antithrombotic therapy: a patent and literature review (2019-present).

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-19 DOI: 10.1080/13543776.2025.2467683

Xin-Yu Chen, Kai Wang, Jie Jia, Xiao-Tian Kong, Huan-Qiu Li, Sheng Tian

{"title":"P2Y12R antagonists in antithrombotic therapy: a patent and literature review (2019-present).","authors":"Xin-Yu Chen, Kai Wang, Jie Jia, Xiao-Tian Kong, Huan-Qiu Li, Sheng Tian","doi":"10.1080/13543776.2025.2467683","DOIUrl":"10.1080/13543776.2025.2467683","url":null,"abstract":"Introduction: P2Y12 receptor (P2Y12R) is a G protein-coupled receptor that plays a crucial role in regulating platelet activation and aggregation. P2Y12R is involved in various processes such as renal fibrosis, cancer, ischemic disease, and related complications, making it an appealing target for therapeutic interventions. Over the past decade, the discovery and development of P2Y12R antagonists have significantly advanced, offering novel treatment options that improve clinical outcomes.Areas covered: This review covers P2Y12R antagonists reported in patents issued in the online databases of the World Intellectual Property Organization and the European Patent Office from 2019 to 2024. This review introduces the development of existing antagonists and evaluates the therapeutic potential of these compounds.Expert opinion: Reversible P2Y12R antagonists offer a potentially safer alternative to the currently dominant irreversible antagonists on the market, as they allow for more controlled platelet inhibition and can reduce the toxicity and adverse effects associated with conventional drugs. Importantly, the integration of computational drug design and molecular docking studies in the discovery and optimization of P2Y12R antagonists represents a significant advancement in precision medicine. This not only provides valuable structural scaffolds but also stimulates novel ideas for developing promising drugs that are both safe and efficacious.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-18"},"PeriodicalIF":5.4,"publicationDate":"2025-02-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143424804","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

Small molecule and peptide CXCR4 antagonists. A patent review from 2019 to 2024.

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-18 DOI: 10.1080/13543776.2025.2462848

Zafer Sahin, Yesim A Tahirovic, Jiafeng Geng, Lawrence J Wilson, Dennis C Liotta

{"title":"Small molecule and peptide CXCR4 antagonists. A patent review from 2019 to 2024.","authors":"Zafer Sahin, Yesim A Tahirovic, Jiafeng Geng, Lawrence J Wilson, Dennis C Liotta","doi":"10.1080/13543776.2025.2462848","DOIUrl":"10.1080/13543776.2025.2462848","url":null,"abstract":"Introduction: The chemokine receptor CXCR4 has been under intense study due to the central role it plays in immune system regulation and the pathology of human disease. Although the first CXCR4 drug plerixafor emerged over a decade ago (2007), recently the first peptide (motixafortide, 2023) and the first oral small molecule (mavorixafor, 2024) CXCR4 antagonists became FDA approved.Areas covered: This article describes patent documents published during the period of 2019 through 2024 for both small molecule and peptides. This IP includes few new chemotypes, with most being extensions of existing structural classes. There is also less significant IP covering peptide-based therapeutics than those covering small molecules. Notably, multiple therapeutic uses have also emerged. Patents were searched from SciFinder (CAS) and Google Patents with the term CXCR4 antagonists. Patents were selected according to whether they fit into the classification of small molecules or peptides.Expert opinion: In the last 5 years there has been significant advancement in CXCR4 antagonists as gauged by the FDA approval of two drugs. The search for second and third generation compounds will be the focus of future efforts with new uses and better properties which likely could come from some of the IP described herein.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-13"},"PeriodicalIF":5.4,"publicationDate":"2025-02-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143381980","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

Updated patent review for hematopoietic progenitor kinase (HPK1) inhibitors and degraders (2021-present).

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-16 DOI: 10.1080/13543776.2025.2462834

Ying-Hui Yuan, Jia-Ying Mao, Ji-Fan Yue, Meng-Lan He, Zi Hui, Hang Yin, Jianshe Wang, Xiang-Yang Ye

{"title":"Updated patent review for hematopoietic progenitor kinase (HPK1) inhibitors and degraders (2021-present).","authors":"Ying-Hui Yuan, Jia-Ying Mao, Ji-Fan Yue, Meng-Lan He, Zi Hui, Hang Yin, Jianshe Wang, Xiang-Yang Ye","doi":"10.1080/13543776.2025.2462834","DOIUrl":"10.1080/13543776.2025.2462834","url":null,"abstract":"Introduction: Hematopoietic progenitor cell kinase (HPK1) is a serine/threonine kinase of MAP4K family. It negatively regulates T cell receptor and B cell signal transduction. The loss of HPK1 kinase function increases the secretion of cytokines and enhances T cell signal transduction, virus clearance and tumor growth inhibition. Therefore, HPK1 is considered as a promising drug target for tumor immunotherapy.Area covered: This article surveys the patents published since 2021 aiming to analyze the structural features of scaffolds and the patent landscape. It also discusses the recent clinical developments and provides perspectives on the challenges and the future directions.Expert opinion: HPK1 kinase is a viable drug target, and there is an increasing number of clinical studies on HPK1 inhibitors. In the clinical research of HPK1 inhibitors, there are mainly two ways: monotherapy and combination therapy. In recent years, HPK1 degraders derived from PROTAC technology have shown promises along with HPK1 inhibitors. It is hopeful that small molecule inhibitors or degraders targeting HPK1 will gain FDA approval for treatment of human diseases in the near future.Databases searched and inclusive dates: A rapid survey of literature reports using keyword 'HPK1' in SciFinder® search engine yielded about 180 papers since 2021.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-22"},"PeriodicalIF":5.4,"publicationDate":"2025-02-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143413900","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

Small molecules targeting immune checkpoint proteins for cancer immunotherapy: a patent and literature review (2020-2024).

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-16 DOI: 10.1080/13543776.2025.2462849

Qiaohong Geng, Juanjuan Xu, Chunsheng Du, Deheng Zhang, Yanrui Jin, Jiatong Song, Wenjing Qu, Changnan Zhang, Gaoxing Su, Peifu Jiao

{"title":"Small molecules targeting immune checkpoint proteins for cancer immunotherapy: a patent and literature review (2020-2024).","authors":"Qiaohong Geng, Juanjuan Xu, Chunsheng Du, Deheng Zhang, Yanrui Jin, Jiatong Song, Wenjing Qu, Changnan Zhang, Gaoxing Su, Peifu Jiao","doi":"10.1080/13543776.2025.2462849","DOIUrl":"10.1080/13543776.2025.2462849","url":null,"abstract":"Introduction: Targeting immune checkpoint proteins (ICPs) via small molecules open a new window for cancer immunotherapy. Herein, we summarize recent advances of small molecules with novel chemical structures targeting ICPs, discusses their anti-tumor efficacies, which are important for the development of novel small molecules for cancer immunotherapy.Areas covered: In this review, the latest patents and literature were gathered through the comprehensive searches in the databases of European Patent Office (EPO), Cortellis Drug Discovery Intelligence (CDDI), PubMed and Web of Science using ICPs and compounds as key words.Expert opinion: To develop novel weapons to fight against cancer, small molecules targeting ICPs including CTLA-4, LAG-3, PD-L1, Siglec-9, TIM-3, TIGIT, and VISTA have been synthesized and evaluated in succession. Chief among them are the small molecules targeting PD-L1, which have been intensively investigated in recent years. Various in vitro assays such as ALPHA, HTRF binding assay, NFAT assay have been successfully developed to screen novel IPCs inhibitors. However, the in vivo assay, for example, using double-humanized PD-1/PD-L1 (hPD-1/hPD-L1) mouse as evaluation model, are seldom reported. Novel pharmacophores with new working mechanisms such as proteolysis targeting chimeras (PROTACs) and peptides are needed to enhance the therapeutic efficacy.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-32"},"PeriodicalIF":5.4,"publicationDate":"2025-02-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143188655","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 BRD4 inhibitors (2020-present).

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-14 DOI: 10.1080/13543776.2025.2463150

Yanfang Chen, Huanmin Zhou, Jiamin Yu, Jing Gao, Shengyu Xue, Hong Ding, Hua Lin, Cheng Luo

{"title":"A patent review of BRD4 inhibitors (2020-present).","authors":"Yanfang Chen, Huanmin Zhou, Jiamin Yu, Jing Gao, Shengyu Xue, Hong Ding, Hua Lin, Cheng Luo","doi":"10.1080/13543776.2025.2463150","DOIUrl":"10.1080/13543776.2025.2463150","url":null,"abstract":"Introduction: Bromodomain-containing protein 4 (BRD4) stands as a pivotal member within the Bromodomain and Extra-Terminal Domain (BET) family, contributing significantly to epigenetic control and gene expression. Given its association with various cancers, BRD4 emerges as a promising therapeutic target, suggesting a substantial role in the treatment of diverse pathological conditions.Areas covered: The present review is centered on patent applications concerning inhibitors targeting BRD4's bromodomain site, published from 2020 to present. A comprehensive evaluation was conducted on a total of 70 applications. The latest patented studies of BRD4 are summarized by using the keywords 'BRD4' in SciFinder, PubMed, and The lens Patents and databases in the year from 2020 to present.Expert opinion: Despite the substantial progress achieved in the clinical research of numerous BET bromodomain inhibitors, their development remains fraught with challenges. To mitigate the dose-limiting toxicity (DLT) and other clinical adverse effects associated with pan-BET inhibitors, current research efforts are increasingly focus on the development of selective BRD4-BD1 or -BD2 inhibitors. These selective inhibitors exhibit considerable potential as more efficacious candidate drugs, thereby paving the way for novel avenues in both fundamental and translational research within this domain.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-16"},"PeriodicalIF":5.4,"publicationDate":"2025-02-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143364208","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

Patenting perspective on Keap1 inhibitors (2019-2024).

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-10 DOI: 10.1080/13543776.2025.2462844

Yongfu Luo, Ziyu Yang, Yuan Zhang, Shutong Jiang, Jingyu Zhu, Xiangyang Li, Qidong You, Mengchen Lu

引用次数: 0

A patent review of von Hippel-Lindau (VHL)-recruiting chemical matter: E3 ligase ligands for PROTACs and targeted protein degradation (2019-present). von Hippel-Lindau （vhl）招募化学物质：用于PROTACs和靶向蛋白降解的E3连接酶配体的专利审查（2019年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-06 DOI: 10.1080/13543776.2024.2446232

Aina Urbina, Alex J Hallatt, Jack Robertson, Alessio Ciulli

{"title":"A patent review of von Hippel-Lindau (VHL)-recruiting chemical matter: E3 ligase ligands for PROTACs and targeted protein degradation (2019-present).","authors":"Aina Urbina, Alex J Hallatt, Jack Robertson, Alessio Ciulli","doi":"10.1080/13543776.2024.2446232","DOIUrl":"10.1080/13543776.2024.2446232","url":null,"abstract":"Introduction: The von Hippel-Lindau (VHL) E3 ubiquitin ligase has seen extensive research due to its involvement in the ubiquitin proteasome system and role as a tumor suppressor within the hypoxia signaling pathway. VHL has become an attractive target for proteolysis targeting chimeras (PROTACs), bifunctional molecules that can induce degradation of neo-substrate proteins. The development of VHL inhibitors and PROTACs has seen rapid development since disclosure of the first non-peptidic VHL ligand (2012).Areas covered: Due to the demand for more diverse and sophisticated VHL ligands that can be applied to PROTACs, the number of patents disclosed has risen significantly in the past 5 years. Herein, the wide range of VHL modifications that have been patented since 2019 is covered. Specifically, any new or unique chemical modification to established VHL ligands or PROTACs will be discussed.Expert opinion: The VHL chemical space continues to expand within the patent literature. There are exciting new modifications that can enhance the physiochemical properties of VHL PROTACs and other alterations can improve the affinity of the VHL ligand itself. Further optimization of the VHL chemical space will no doubt lead to the development of more VHL-based therapies and clinical candidates.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-42"},"PeriodicalIF":5.4,"publicationDate":"2025-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11875441/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143002867","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

A patent review of small molecular inhibitors targeting EGFR exon 20 insertion (Ex20ins) (2019-present). 靶向EGFR外显子20插入（Ex20ins）的小分子抑制剂专利审查（2019-至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-01 Epub Date: 2024-12-27 DOI: 10.1080/13543776.2024.2446220

Wenjian Zhu, Junping Pei, Xiaoyun Lu

{"title":"A patent review of small molecular inhibitors targeting EGFR exon 20 insertion (Ex20ins) (2019-present).","authors":"Wenjian Zhu, Junping Pei, Xiaoyun Lu","doi":"10.1080/13543776.2024.2446220","DOIUrl":"10.1080/13543776.2024.2446220","url":null,"abstract":"Introduction: Mutations in epidermal growth factor receptor (EGFR) kinase domain consistently activate downstream signaling pathways, such as the PI3K/AKT/mTOR and RAS/RAF/MEK, thereby promoting tumor growth. Although the majority of non-small cell lung cancer (NSCLC) patients harboring EGFR mutations are sensitive to existing EGFR tyrosine kinase inhibitors (EGFR-TKIs), there remains an unmet clinical need for effective therapies targeting EGFR Ex20ins mutations, making direct targeting EGFR Ex20ins mutations a promising therapeutic strategy.Areas covered: This review covers the progress of clinical studies targeting EGFR Ex20ins inhibitors and summarizes recent (1 January 2019 - 30 April 2024) patents disclosing EGFR Ex20ins inhibitors available in the Espacenet and CAS SciFinder databases.Expert opinion: An increasing number of EGFR Ex20ins inhibitors are being developed and reported. Existing inhibitors are focused on enhancing the efficacy of EGFR Ex20ins inhibitors and addressing the challenge of targeted resistance by optimizing the second - or third-generation EGFR inhibitors and developing innovative skeleton molecules. Moreover, the development of targeted protein degraders, allosteric inhibitors, and combination therapies provide additional approaches to address EGFR Ex20ins mutations. However, bypass resistance, selectivity, and drug sensitivity still pose challenges in this field.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"91-110"},"PeriodicalIF":5.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142871905","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 xanthine oxidase inhibitors (2021-present). 黄嘌呤氧化酶抑制剂专利回顾（2021年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-01 Epub Date: 2024-12-30 DOI: 10.1080/13543776.2024.2446222

Chang Liu, Qing Mao, Bing Zhang, Xuefeng Fu, Tingjian Zhang, Shaojie Wang

{"title":"A patent review of xanthine oxidase inhibitors (2021-present).","authors":"Chang Liu, Qing Mao, Bing Zhang, Xuefeng Fu, Tingjian Zhang, Shaojie Wang","doi":"10.1080/13543776.2024.2446222","DOIUrl":"10.1080/13543776.2024.2446222","url":null,"abstract":"Introduction: Xanthine oxidase (XO) catalyzes the oxidation of both hypoxanthine and xanthine in the last two steps of the purine metabolic pathway, serving as a rate-limiting enzyme for uric acid production as well as a key target for the treatment of gout and other hyperuricemia-related conditions.Areas covered: This paper reviews XO inhibitors in patents from 2021 to the present. We summarize in detail the structural classes and characteristics, in vitro and in vivo biological results, and structure‒activity relationships of synthetic inhibitors, as well as the sources, specific structures, research methods, and biological activities of XO inhibitors from natural products.Expert opinion: (1) Benefiting from the discovery of many high-affinity inhibitors, the binding modes of small molecules in the active pocket of XO have been further elucidated, and this information will contribute to future development; (2) natural products remain one of the important sources in the discovery of XO inhibitors; (3) with a deeper exploration of XO and URAT1 targets, XO/URAT1 dual target inhibitors may be a future research hotspot; and (4) the search for high-affinity, small-molecule scaffolds remains a key challenge and an important direction for the future development.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"79-89"},"PeriodicalIF":5.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142893203","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 JAK1 inhibitors and the therapeutic applications thereof: a patent review (2016-2023). 选择性JAK1抑制剂及其治疗应用：专利审查（2016-2023）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-02-01 Epub Date: 2024-12-25 DOI: 10.1080/13543776.2024.2446223

Yuhui Gao, Li Lan, Cheng Wang, Yuwei Wang, Lei Shi, Liping Sun

{"title":"Selective JAK1 inhibitors and the therapeutic applications thereof: a patent review (2016-2023).","authors":"Yuhui Gao, Li Lan, Cheng Wang, Yuwei Wang, Lei Shi, Liping Sun","doi":"10.1080/13543776.2024.2446223","DOIUrl":"10.1080/13543776.2024.2446223","url":null,"abstract":"Introduction: The family of Janus kinases (JAKs) consists of four intracellular non-receptor tyrosine kinases: JAK1, JAK2, JAK3, and tyrosine kinase 2 (TYK2). Among these four subtypes, JAK1 is the only isoform that can form heterodimers with all three JAKs, and JAK1 dysfunction can lead to inflammation and severe autoimmune diseases. Interest in JAK1 inhibitors has grown tremendously, and the number of inhibitors targeting JAK1 continues to rise annually.Areas covered: This paper reviews JAK1 small molecule inhibitors that were reported in patent literature from January 2016 to December 2023. Web of Science, SciFinder, PubMed, WIPO, EPO, USPTO, and CNIPA databases were used for searching the literature and patents for JAK1 inhibitors.Expert opinion: JAK1 inhibitors show great promise in treating cytokine dysregulated disorders; nevertheless, nonselective JAK1 inhibitors have more severe side effects, which restricts the therapy's safety and use. Therefore, developing highly selective JAK1 inhibitors can mitigate potential risks and lead to next-generation therapies with improved efficacy and safety profiles.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"181-195"},"PeriodicalIF":5.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142881254","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