Expert Opinion on Therapeutic Patents最新文献

Recent advances in tropomyosin receptor kinase (TRK) inhibitors: a 2023-2024 patent landscape review. 原肌球蛋白受体激酶（TRK）抑制剂的最新进展：2023-2024年专利回顾

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-08-01 Epub Date: 2025-07-10 DOI: 10.1080/13543776.2025.2529217

Minh Le, Elena Timakova, Ralf Schirrmacher, Justin J Bailey

{"title":"Recent advances in tropomyosin receptor kinase (TRK) inhibitors: a 2023-2024 patent landscape review.","authors":"Minh Le, Elena Timakova, Ralf Schirrmacher, Justin J Bailey","doi":"10.1080/13543776.2025.2529217","DOIUrl":"10.1080/13543776.2025.2529217","url":null,"abstract":"Introduction: The rise of tissue-agnostic therapies has revolutionized cancer treatment, with therapies targeting NTRK fusions leading the way. TRK inhibitors like larotrectinib and entrectinib marked a paradigm shift - prioritizing molecular alterations over the tumor's anatomical location. Acquired resistance remains a significant challenge, with next-generation inhibitors and combination strategies at the forefront of efforts to enhance the clinical efficacy of TRK-targeted therapies.Areas covered: This review discusses patents published in 2023 and 2024 covering inhibitors of the TRK family, extending our ongoing review series on TRK inhibitors. Patent searches were conducted using the key word 'TRK*' and 'inhibitor' in Google Patents database to identify novel TRK-targeting inhibitors and therapeutic strategies.Expert opinion: Ongoing advancements in TRK inhibitor development, combination therapies, and precision diagnostics continue to elevate the potential of treatment outcomes. Recent patent filings reflect the expanding promise of TRK inhibitors for NTRK fusion-driven cancers. However, widespread adoption of high-throughput screening remains crucial unlocking their full therapeutic value and delivering truly precision-guided care. Combination therapies with TRK inhibitors are emerging as a key strategy to enhance efficacy and overcome resistance. The FDA's recent approval of repotrectinib underscores progress in the TRK inhibitor landscape, while highlighting the continued need for innovation.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"901-914"},"PeriodicalIF":4.6,"publicationDate":"2025-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144567337","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 rearranged during transfection (RET) kinase inhibitors (2022-present). 重组转染（RET）激酶抑制剂的最新专利回顾（2022年至今）。

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-08-01 Epub Date: 2025-06-17 DOI: 10.1080/13543776.2025.2519642

Daniel Armstrong, Maha Hanafi, Brendan Frett

{"title":"An updated patent review of rearranged during transfection (RET) kinase inhibitors (2022-present).","authors":"Daniel Armstrong, Maha Hanafi, Brendan Frett","doi":"10.1080/13543776.2025.2519642","DOIUrl":"10.1080/13543776.2025.2519642","url":null,"abstract":"Introduction: Rearranged during transfection (RET) is a receptor tyrosine kinase essential for cell signaling processes such as proliferation, differentiation, and migration. RET alterations, including point mutations and gene fusions, contribute to oncogenesis. Recent advances in precision oncology have led to the development of selective RET inhibitors with improved safety and efficacy profiles.Areas covered: This review discusses recent innovations in RET inhibitor development, with a focus on small-molecule patents published from 2022 to 2024. A comprehensive literature search was conducted using SciFinder and PatentScope with the keywords 'RET' and 'RET inhibitor.' The review summarizes the structural classes, target profiles, and potential advantages of newly patented compounds, particularly those designed to overcome known resistance mechanisms.Expert opinion: While selective RET inhibitors such as selpercatinib have shown clinical success and expanded indications, their use is limited by adverse events and emerging resistance mechanisms. Next-generation RET inhibitors that address these limitations represent a critical frontier in drug development.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"859-873"},"PeriodicalIF":4.6,"publicationDate":"2025-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144274595","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

Formyl peptide receptor modulators: a patent review and potential applications for inflammatory diseases (2021-2024). 甲酰基肽受体调节剂：专利审查和炎症疾病的潜在应用（2021-2024）。

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-08-01 Epub Date: 2025-06-11 DOI: 10.1080/13543776.2025.2515882

Yung-Fong Tsai, Shun-Chin Yang, Tsong-Long Hwang

{"title":"Formyl peptide receptor modulators: a patent review and potential applications for inflammatory diseases (2021-2024).","authors":"Yung-Fong Tsai, Shun-Chin Yang, Tsong-Long Hwang","doi":"10.1080/13543776.2025.2515882","DOIUrl":"10.1080/13543776.2025.2515882","url":null,"abstract":"Introduction: Formyl peptide receptors (FPRs) belong to the family of class A G-protein-coupled receptors that are important for immune modulation and inflammation and are emerging as potential therapeutic targets for several inflammatory diseases. FPRs have shown therapeutic roles in the management of cardiovascular diseases, neuroinflammation, and cancer. Biased agonists are an active topic in the further revisions that encompass the utilization of a definite subset of signaling pathways to improve therapeutic maladies, in parallel with reducing the negative effects.Areas covered: This review surveys the modulators of FPR1 and FPR2 that have been published in patents from 2021 to 2024, to summarize the categorization of agonists and antagonists and discuss their possible clinical uses. A targeted patent search was performed using the Taiwan Patent GO Showcases database (https://tiponet.tipo.gov.tw/gpss/).Expert opinion: We examine newly disclosed patents concerning FPR modulators, with all specified compounds classified as either FPR1 or FPR2 modulators. Receptor cross-reactivity, ligand promiscuity, and receptor variations across species are challenges encountered during drug formulation. Further research into different types of biased agonists and the synthesis of potent and selective ligands is essential to overcome these obstacles and facilitate the eventual therapeutic use of biased signaling in inflammation and diseases.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"839-857"},"PeriodicalIF":4.6,"publicationDate":"2025-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144215382","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

Rho kinase inhibitors: a patent review (2017-2023). Rho激酶抑制剂：专利审查（2017 - 2023）。

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-08-01 Epub Date: 2025-06-24 DOI: 10.1080/13543776.2025.2522735

Daniela Rodrigues de Oliveira, Heber Victor Tolomeu, Carlos Alberto Manssour Fraga, Lídia Moreira Lima

引用次数: 0

An updated patent review on rational combinations of HDAC inhibitors for cancer chemotherapy (2020 - present): part 2 - patent published. 癌症化疗中合理组合HDAC抑制剂的最新专利审查（2020年至今）：第2部分-专利公布。

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-08-01 Epub Date: 2025-06-14 DOI: 10.1080/13543776.2025.2516785

Yugal Kishor Shukla, Vandana, Vivekananda Mandal, Vivek Asati, Raj K Keservani, Sanjay Kumar Bharti

{"title":"An updated patent review on rational combinations of HDAC inhibitors for cancer chemotherapy (2020 - present): part 2 - patent published.","authors":"Yugal Kishor Shukla, Vandana, Vivekananda Mandal, Vivek Asati, Raj K Keservani, Sanjay Kumar Bharti","doi":"10.1080/13543776.2025.2516785","DOIUrl":"10.1080/13543776.2025.2516785","url":null,"abstract":"Introduction: The emergence of drug resistance poses a serious threat to cancer chemotherapy by a single agent. Tumor cell heterogeneity, mutation, and/or desensitization of receptor render monotherapy ineffective. Combination encompassing multiple targets or biochemical pathways seems promising for cancer treatment. Combination of HDAC inhibitor(s) with other inhibitor(s) has shown synergistic activity in cancer chemotherapy by modulating a variety of therapeutic targets including epigenetic target of cancer cells by restoring acetylation and reactivating tumor suppressor genes leading to cell cycle arrest, promoting apoptosis, and thus inhibiting cancer cell proliferation.Areas covered: A comprehensive published patent literature (2020-present) on rational combinations of HDAC inhibitor(s) for cancer chemotherapy has been retrieved and reviewed from various patent databases including Google Patents, Espacenet, Patentscope, WIPO, and USPTO to analyze the rational combinations for better, optimized, and precise cancer therapy. In this second part of two-part review, we highlighted the patent published for the combination.Expert opinion: The HDAC inhibitor(s) in combination with other therapeutically relevant inhibitor(s) such as MAPK, GSK3, PI3K/mTOR, PARP, CDK9, HSP90, BTK, BRD4, JAK, VEGF, ALK, PD-1, or PDE inhibitor showed synergistic anti-cancer activity. These combinations not only overcame drug resistance but also acted against relapsed/refractory cancers.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"875-900"},"PeriodicalIF":4.6,"publicationDate":"2025-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144233681","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

Nurr1 modulators - a patent review (2019-present). Nurr1调制器-专利审查（2019年至今）。

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-08-01 Epub Date: 2025-06-18 DOI: 10.1080/13543776.2025.2516780

Markus Egner, Daniel Merk

{"title":"Nurr1 modulators - a patent review (2019-present).","authors":"Markus Egner, Daniel Merk","doi":"10.1080/13543776.2025.2516780","DOIUrl":"10.1080/13543776.2025.2516780","url":null,"abstract":"Background: Nuclear receptor related 1 (Nurr1) is a ligand-activated transcription factor and considered as neuroprotective and anti-neuroinflammatory target. Several lines of evidence support potential of Nurr1 modulation in treating neurodegenerative diseases as well as in certain cancers, but potent and selective Nurr1 modulators are rare.Areas covered: Development of small molecule Nurr1 modulators is gaining momentum which is also reflected in recent patent applications (published between 01/2019 and 09/2024, available on Google Patents). The claimed Nurr1 ligands are derived from the natural ligands prostaglandin A and dihydroxyindole as well as synthetic scaffolds. Their proposed use mainly refers to neurodegenerative disease and cancer treatment.Expert opinion: Nurr1 modulation is emerging as new therapeutic concept in neurodegeneration and beyond and considerable progress has been made in Nurr1 ligand discovery with several promising compounds covered by patent applications. However, some reported and claimed ligands seem to lack validation and some claims appear very broad without presenting respective examples.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"795-810"},"PeriodicalIF":4.6,"publicationDate":"2025-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144247232","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

Glycogen synthase kinase 3β (GSK-3β) inhibitors - a patent update (2019-2024). 糖原合成酶激酶3β (GSK-3β)抑制剂-专利更新（2019-2024）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-07-23 DOI: 10.1080/13543776.2025.2536003

Swanand Vinayak Joshi, Devandla Soujanya, Manchella Sai Supriya, Venkata Madhavi Yaddanapudi, Srinivas Nanduri

{"title":"Glycogen synthase kinase 3β (GSK-3β) inhibitors - a patent update (2019-2024).","authors":"Swanand Vinayak Joshi, Devandla Soujanya, Manchella Sai Supriya, Venkata Madhavi Yaddanapudi, Srinivas Nanduri","doi":"10.1080/13543776.2025.2536003","DOIUrl":"10.1080/13543776.2025.2536003","url":null,"abstract":"Introduction: Glycogen synthase kinase-3β (GSK-3β) is a proline-directed serine/threonine kinase identified over 40 years ago. It is the key enzyme involved in glycogen biosynthesis and is expressed in all human tissues. Overexpression of GSK-3β is linked to several diseases, including diabetes mellitus, neurodegenerative disorders such as Alzheimer's disease, and cancer. Owing to its critical role in the pathophysiology of these diseases, GSK-3β has emerged as a validated and potential target for therapeutic intervention. In recent years, significant progress has been made in developing novel GSK-3 inhibitors. Some of these new inhibitors have shown promising results in treating some of these diseases.Areas covered: This review covers patent literature on various GSK-3β inhibitors published between 2019 and 2024. This review also discusses the recent clinical developmental status of some of the promising GSK-3 inhibitors.Expert opinion: Although many heterocyclic compounds from natural as well as synthetic origin have shown promising inhibitory effects against GSK-3β, most of them have not yet progressed to the development stage. However, a critical review of their structures and biological profiles reveals significant potential for further development.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-13"},"PeriodicalIF":5.4,"publicationDate":"2025-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144689697","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

Overcoming triple mutant EGFR-tyrosine kinase barriers in the therapeutics of non-small cell lung cancer: a patent review on fourth-generation inhibitors (2017-2024). 克服非小细胞肺癌治疗中三重突变egfr -酪氨酸激酶屏障：第四代抑制剂专利审查（2017-2024）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-07-22 DOI: 10.1080/13543776.2025.2536006

Narendra R Nagpure, Harun M Patel

{"title":"Overcoming triple mutant EGFR-tyrosine kinase barriers in the therapeutics of non-small cell lung cancer: a patent review on fourth-generation inhibitors (2017-2024).","authors":"Narendra R Nagpure, Harun M Patel","doi":"10.1080/13543776.2025.2536006","DOIUrl":"10.1080/13543776.2025.2536006","url":null,"abstract":"Introduction: Non-small cell lung cancer (NSCLC) remains a leading cause of cancer mortality, with epidermal growth factor receptor (EGFR) mutations being the primary driver of tumor progression. This review highlights the significance of fourth-generation EGFR tyrosine kinase inhibitors (EGFR-TKIs) in addressing acquired resistance mechanisms, such as the C797S mutation, which compromises the efficacy of third-generation inhibitors like Osimertinib and explores their potential to revolutionize NSCLC treatment through enhanced molecular specificity.Areas covered: This review covers the latest progress in patented fourth-generation EGFR-TKIs and their clinical trial status for the treatment of NSCLC from 2017 to the present.Expert opinion: Osimertinib, a third-generation EGFR inhibitor, revolutionized treatment for T790M mutations but is limited by resistance from C797S mutations. Fourth-generation EGFR inhibitors, incorporating scaffolds like aminopyrimidine and quinazoline, are designed to selectively target resistant EGFR variants, including L858R/T790M/C797S. Preclinical trials highlight the potential of sulfonyl and phosphine oxide-based compounds for their potency, selectivity, and favorable pharmacokinetics. Promising clinical trials with inhibitors like BDTX-1535, JIN-A02, and HS-10504 could redefine NSCLC treatment, with future success likely relying on innovative strategies, such as combination therapies, to combat resistance and enhance efficacy.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-21"},"PeriodicalIF":5.4,"publicationDate":"2025-07-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144642192","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 small molecule KCNT1 inhibitors (2022-2024). 小分子KCNT1抑制剂的最新专利审查（2022 - 2024）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-07-01 Epub Date: 2025-05-21 DOI: 10.1080/13543776.2025.2504460

Paul K Peprah, Kyle A Emmitte

{"title":"An updated patent review of small molecule KCNT1 inhibitors (2022-2024).","authors":"Paul K Peprah, Kyle A Emmitte","doi":"10.1080/13543776.2025.2504460","DOIUrl":"10.1080/13543776.2025.2504460","url":null,"abstract":"Introduction: Gain-of-function mutations in KCNT1 channels has been associated with severe childhood epilepsies. KCNT1 channels are sodium activated potassium channels in the CNS involved in neuronal excitability. Substantial efforts have been made by several groups to discover novel small molecule KCNT1 inhibitors to validate this approach as a therapeutic strategy for the treatment of KCNT1-related epilepsies.Areas covered: This review focuses on 10 published international patent applications from Praxis Precision Medicine that disclose novel small molecule KCNT1 inhibitors for the treatment of KCNT1-related neurological disorders. Features of compounds that contribute to KCNT1 inhibition and published in applications between 2022 and 2024 are discussed. Applications were identified and obtained through the online database, Patentscope, provided by the World Intellectual Property Organization (WIPO) using the search term 'KCNT1 inhibitors.'Expert opinion: Tremendous progress has been made toward the discovery of small molecule inhibitors of KCNT1 channels; however, much work remains to reach a viable therapeutic. Areas of work that will be critically important include further in vivo studies for efficacy, safety, and development of PK/PD relationships. Studies to better understand the binding of known ligands and determine the structural features that govern modulation of the channel are also much needed.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"775-794"},"PeriodicalIF":5.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144076644","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 RNA ligands: a patent review (2018-2024). 小分子RNA配体：专利审查（2018-2024）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-07-01 Epub Date: 2025-04-16 DOI: 10.1080/13543776.2025.2492759

Elia Ravegnini, Andrea Trabocchi, Elena Lenci

{"title":"Small-molecule RNA ligands: a patent review (2018-2024).","authors":"Elia Ravegnini, Andrea Trabocchi, Elena Lenci","doi":"10.1080/13543776.2025.2492759","DOIUrl":"10.1080/13543776.2025.2492759","url":null,"abstract":"Introduction: Targeting three-dimensional RNA structures with traditional drug-like small molecules is gaining wide attention in both the academia and the pharmaceutical industries, due to their good oral bioavailability, cheap production cost, and the possibility of fine-tuning ADMET properties, which represent a powerful alternative to the current RNA-targeted therapies, including ASO and siRNA. As RNAs are involved in nearly all the physiological and pathological processes, small molecules RNA ligands can have a plethora of different therapeutic applications, spanning from cancer to infectious and neurological diseases.Areas covered: This review describes patents concerning small molecules RNA ligands published within January 2018 and October 2024, searched through Espacenet, Patentscope, and Google Patents databases.Expert opinion: The number of patents that has been released in the last few years demonstrates the relevance of targeting RNA structures for the development of next generation chemotherapeutic agents and antiviral/antibacterial drugs, even though this field is still in its infancy and many issues still need to be resolved, in particular related to selectivity. An emerging approach to considerably limiting side effects is presented by RIBOTAC derivatives, as promoting a selective RNase-L mediated RNA degradation allows to significantly reduce the dose of the compound.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"675-693"},"PeriodicalIF":5.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143964166","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