Expert Opinion on Therapeutic Patents最新文献_第3页

An updated patent review of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitors (2020-present). 双特异性酪氨酸磷酸化调节激酶1A （DYRK1A）抑制剂的最新专利审查（2020年至今）。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-08-01 Epub Date: 2026-07-02 DOI: 10.1080/13543776.2026.2694586

Mennatallah Abdallah, Parthiena M Keddis, Trevina M Keddis, Dalia S El-Gamil, Ashraf H Abadi, Isao Kii, Matthias Engel, Mohammad Abdel-Halim

{"title":"An updated patent review of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitors (2020-present).","authors":"Mennatallah Abdallah, Parthiena M Keddis, Trevina M Keddis, Dalia S El-Gamil, Ashraf H Abadi, Isao Kii, Matthias Engel, Mohammad Abdel-Halim","doi":"10.1080/13543776.2026.2694586","DOIUrl":"10.1080/13543776.2026.2694586","url":null,"abstract":"Introduction: Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a conserved CMGC serine/threonine kinase with an autophosphorylation-dependent activation mechanism. As a dosage-sensitive regulator of transcription, RNA splicing, cell-cycle progression, and signaling, DYRK1A is implicated in neurological, oncological, cardiovascular, metabolic, immune, and infectious diseases. These roles have driven drug discovery, from early probes to advanced clinical-stage inhibitors.Areas covered: This review covers patent literature related to the discovery of DYRK1A inhibitors and degraders published from January 2020 to the review cutoff date. The literature search was conducted in WIPO, Reaxys, SciFinder, Lens.org, Espacenet, USPTO, and Google Patents.Expert opinion: Recent patents indicate that DYRK1A inhibition is no longer a single pharmacological concept but an indication-driven strategy shaped by tissue access, delivery, and mechanistic pharmacodynamic biomarkers. The most credible programs prioritize functional pathway modulation and meaningful target engagement at therapeutically achievable exposure rather than maximal biochemical potency alone, with selectivity defined by disease biology rather than as an absolute requirement. Delivery-advantaged indications such as osteoarthritis and peripheral inflammatory disorders may provide the earliest clinical validation, whereas CNS programs will require brain-penetrant compounds with controlled, likely partial, target modulation. Degraders and macrocycles broaden the toolbox, but biomarker-guided translation remains the key determinant of success.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"713-741"},"PeriodicalIF":4.7,"publicationDate":"2026-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148301551","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 histone deacetylase 6 inhibitors in neurodegenerative diseases (2020-2025). 组蛋白去乙酰化酶6抑制剂在神经退行性疾病中的最新专利审查（2020-2025）。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-07-01 Epub Date: 2026-05-20 DOI: 10.1080/13543776.2026.2676080

Sida Shen

{"title":"An updated patent review of histone deacetylase 6 inhibitors in neurodegenerative diseases (2020-2025).","authors":"Sida Shen","doi":"10.1080/13543776.2026.2676080","DOIUrl":"10.1080/13543776.2026.2676080","url":null,"abstract":"Introduction: Histone deacetylase 6 (HDAC6) inhibitors have been widely explored as potential therapeutic approaches for oncological, autoimmune, cardiovascular, and neurodegenerative disorders. Recent clinical advancements in non-hydroxamate-based HDAC6 inhibitors highlight favorable drug-like properties and improved safety margins, enhancing suitability for long-term treatment.Area covered: This review updates the clinical status of HDAC6 inhibitors, the evolution of HDAC6 inhibitor pharmacophores, and patent disclosures from 2020 to 2025 identified by SciFinder search and manual confirmation. It also describes pharmacological assessment of new selective HDAC6 inhibitors in in vitro and in vivo models of neurodegenerative diseases.Expert opinion: Expanding interest in the development of 2-(difluoromethyl)-1,3,4-oxadiazole (1,3,4-DFMO) derivatives has yielded a diverse set of HDAC6 inhibitors with superior HDAC6 potency and selectivity and enhanced oral pharmacokinetic profiles. These characteristics have facilitated the identification of optimized drug candidates for treating both peripheral and central nervous neurodegenerative diseases. Among the emerging therapeutic applications, Charcot-Marie-Tooth (CMT) disease has become the leading focus in preclinical and early clinical development using HDAC6 inhibitors.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"643-664"},"PeriodicalIF":4.7,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147959892","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 review of discoidin domain receptor 1 (DDR1) modulators (2020-present). 盘状蛋白结构域受体1 （DDR1）调节剂的最新综述（2020年至今）。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-07-01 Epub Date: 2026-06-10 DOI: 10.1080/13543776.2026.2685624

Yunliang Zhang, Zhen Wang, Ke Ding

{"title":"An updated review of discoidin domain receptor 1 (DDR1) modulators (2020-present).","authors":"Yunliang Zhang, Zhen Wang, Ke Ding","doi":"10.1080/13543776.2026.2685624","DOIUrl":"10.1080/13543776.2026.2685624","url":null,"abstract":"Introduction: As a unique collagen-activated receptor tyrosine kinase, discoidin domain receptor 1 (DDR1) mediates signaling essential for cell proliferation, survival, adhesion, and matrix remodeling. Conversely, its dysregulation is implicated in cancer, tissue fibrosis, atherosclerosis, and other inflammatory diseases. Emerging research reveals that the non-catalytic functions of DDR1 are critically involved in tumor progression, metastasis, and immune exclusion. Selectively inhibiting the catalytic and/or non-catalytic functions of DDR1 presents a promising therapeutic strategy for various diseases.Areas covered: This article summarizes current progress on the development of inhibitors, degraders and biomolecules targeting DDR1 and their potential therapeutic application during the period from 2020 to 2025.Expert opinion: Significant efforts have been made to develop small-molecule DDR1 kinase inhibitors, yet achieving high selectivity remains a challenge. Degraders have been developed to inhibit both its catalytic and noncatalytic functions. Although these molecules offer conceptual advantages over traditional kinase inhibitors, they suffer from suboptimal pharmacokinetic properties. Alternatively, biologics such as antibodies and peptides can block the DDR1-collagen interaction, specifically inhibiting non-catalytic signaling, and one antibody is currently under clinical evaluation. Moving forward, the development of highly selective inhibitors and improvement of pharmacokinetic profiles for degraders will be pivotal for translating DDR1 targeting into viable therapies.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"581-592"},"PeriodicalIF":4.7,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148156154","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

Takeda G-protein-coupled receptor 5 and farnesoid X receptor agonists for diabetes treatment: a patent review and clinical advancements (2015-present). 武田g蛋白偶联受体5和法内酯X受体激动剂治疗糖尿病：专利审查和临床进展（2015-至今）。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-07-01 Epub Date: 2026-06-28 DOI: 10.1080/13543776.2026.2682837

Shivank Sharma, Vanktesh Kumar, Shubham Kumar, Pankaj Wadhwa

{"title":"Takeda G-protein-coupled receptor 5 and farnesoid X receptor agonists for diabetes treatment: a patent review and clinical advancements (2015-present).","authors":"Shivank Sharma, Vanktesh Kumar, Shubham Kumar, Pankaj Wadhwa","doi":"10.1080/13543776.2026.2682837","DOIUrl":"10.1080/13543776.2026.2682837","url":null,"abstract":"Introduction: Takeda G-protein-coupled receptor 5 (TGR5) and farnesoid X receptor (FXR) are bile acid-activated receptors involved in glucose, lipid, and energy homeostasis, making them promising therapeutic targets for type 2 diabetes mellitus (T2DM) and metabolic liver diseases.Areas covered: This review critically analyzes patents published between 2015 and 2025 retrieved from WIPO Patentscope, Espacenet, USPTO, and Google Patents using keyword- and IPC-based strategies. Major patented chemotypes include modified bile acids, benzoic acid-cholane hybrids, heteroaryl scaffolds, and sulfonylurea/sulfonamide derivatives. Several compounds demonstrated sub micromolar (µM) to nanomolar (nM) TGR5/FXR agonistic activity, while gut-restricted agonists showed enhanced GLP-1 secretion with reduced systemic adverse effects such as gallbladder filling and pruritus. Comparative patent analysis revealed a progressive transition from classical steroidal scaffolds toward tissue-selective and gut-restricted modulators designed to improve receptor selectivity, pharmacokinetics, and translational safety.Expert opinion: Despite strong preclinical promise, the clinical translation of TGR5 and FXR agonists remains limited by mechanism-driven toxicities and inadequate long-term tolerability. Future progress will likely depend on tissue-selective, pathway-biased, and gut-restricted modulation rather than further increases in receptor potency.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"593-625"},"PeriodicalIF":4.7,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148301613","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

New insights on anticancer glucocorticoid receptor modulators: a patent review (2020-present). 抗癌糖皮质激素受体调节剂的新见解：专利审查（2020年至今）。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-07-01 Epub Date: 2026-06-19 DOI: 10.1080/13543776.2026.2689602

Martina Franzin, Marianna Lucafò, Debora Curci, Giuliana Decorti, Gabriele Stocco

{"title":"New insights on anticancer glucocorticoid receptor modulators: a patent review (2020-present).","authors":"Martina Franzin, Marianna Lucafò, Debora Curci, Giuliana Decorti, Gabriele Stocco","doi":"10.1080/13543776.2026.2689602","DOIUrl":"10.1080/13543776.2026.2689602","url":null,"abstract":"Introduction: Selective glucocorticoid receptor modulators (SGRM) have emerged as promising agents to counteract glucocorticoid‑driven chemoresistance, immune suppression, and poor prognosis in solid tumors by modulating glucocorticoid receptor (GR) signaling without losing anticancer immune activity.Areas covered: This review provides a focused update to a previous patent review on SGRM (2014-2020) by summarizing Espacenet-indexed patent applications published between 2020 and 30 April 2026 (PCT/US2020/055498, PCT/US2021/017259, PCT/US2022/042475) describing anticancer strategies.Expert opinion: Collectively, these patents support SGRM in addition to cytotoxic and immunotherapeutic regimens in solid tumors. Preclinical and early‑phase clinical evidence (phase I/II) describes how GR antagonism, continuously or intermittently, lowers elevated neutrophil-to-lymphocyte ratio (NLR), modulates GR‑target transcriptional signatures, and enhances responses to nab‑paclitaxel and anti‑PD‑1 antibodies. Key limitations of these patents consist of evidence based on still limited clinical sample sizes, requiring confirmation in phase III trials, and on benefit enriched in biologically defined subpopulations. From a clinical perspective, these agents could be realistically integrated into anticancer protocols, as they work synergistically with other chemotherapeutics.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"665-677"},"PeriodicalIF":4.7,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148249688","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 update on PDGFR inhibitors: a patent review (2020 - present). PDGFR抑制剂的最新进展：专利审查（2020年至今）。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-07-01 Epub Date: 2026-05-27 DOI: 10.1080/13543776.2026.2678333

Sisir Nandi, Sarfaraz Ahmed, Soubhik Barma, Rishita Dey, Asmita Samadder

{"title":"An update on PDGFR inhibitors: a patent review (2020 - present).","authors":"Sisir Nandi, Sarfaraz Ahmed, Soubhik Barma, Rishita Dey, Asmita Samadder","doi":"10.1080/13543776.2026.2678333","DOIUrl":"10.1080/13543776.2026.2678333","url":null,"abstract":"Introduction: Platelet-derived growth factor receptors (PDGFRs) play essential roles in cell growth, angiogenesis, and tissue repair, while their dysregulation is implicated in cancer and fibrotic disorders. PDGFR inhibitors have become important in precision medicine by enabling targeted therapy, slowing disease progression, and overcoming drug resistance which warrants search of new inhibitors.Areas covered: A patent survey (2020-2025) focused on small-molecule PDGFR inhibitors has been carried out. Key aspects discussed include PDGFR inhibitory activity, antiproliferative effects, structural features critical for activity, and clinical relevance.Expert opinion: The PDGFR inhibitors, as summarized in discussed patents, reveal that among the nitrogen containing heterocycles, the most active belonged to pyrazolopyrimidines, pyrazolothiazole carboxamides, and pyrrolo[1,2-b] pyridazines classes where hydrophobicity plays an important role in their activity. Although some of the compounds were specific to either the α or β receptor, many reported compounds lacked selectivity to other kinases as well. The smaller number of patents could also indicates a larger scope to address these issues and simultaneously identify novel PDGFR inhibitors.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"627-641"},"PeriodicalIF":4.7,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147981438","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 advances in the discovery of PKMYT1-targeting drugs: a patent review (2021-2025). pkmyt1靶向药物的最新发现进展：专利审查（2021-2025）。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-06-01 Epub Date: 2026-05-21 DOI: 10.1080/13543776.2026.2674071

Yazhou Wang, Chao Wang, Feng Ren, Alex Zhavoronkov, Xiao Ding

{"title":"Recent advances in the discovery of PKMYT1-targeting drugs: a patent review (2021-2025).","authors":"Yazhou Wang, Chao Wang, Feng Ren, Alex Zhavoronkov, Xiao Ding","doi":"10.1080/13543776.2026.2674071","DOIUrl":"10.1080/13543776.2026.2674071","url":null,"abstract":"Introduction: PKMYT1, a member of the WEE family of kinases that regulates mitotic entry by phosphorylating CDK1 at Thr14, has recently gained prominence as a promising synthetic lethal target for oncology. Since the first-in-class PKMYT1 inhibitor entered clinical trials in 2021, the field has experienced explosive growth, marked by a surge in patents for both inhibitors and degraders and the advancement of five candidates into clinical development.Areas covered: This review covers an update of clinical trial reports and patent literature on PKMYT1 inhibitors from 2021 to December 2025, drawing on patent retrieved from the World Intellectual Property Organization (WIPO), the European Patent Office, and the Cortellis Drug Discovery Intelligence database.Expert opinion: The rapid advancement of PKMYT1 inhibitors and degraders underscores their potential as a synthetic‑lethal therapeutic strategy for cancers with CCNE1 amplification or FBXW7 alterations. Clinical proof‑of‑concept for this approach has been established by RP‑6306 trial outcomes, while insights from this comprehensive review are expected to inform strategies addressing the current limitations in this field.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"555-579"},"PeriodicalIF":4.7,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147981426","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

PCSK9 inhibitors: an updated patent review 2024-2025. PCSK9抑制剂：更新的专利审查2024-2025

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-06-01 Epub Date: 2026-05-21 DOI: 10.1080/13543776.2026.2674748

Enrico Mario Alessandro Fassi, Marco Albani, Lorenza D'Adduzio, Erica Ginevra Milano, Carmen Lammi, Giovanni Grazioso

{"title":"PCSK9 inhibitors: an updated patent review 2024-2025.","authors":"Enrico Mario Alessandro Fassi, Marco Albani, Lorenza D'Adduzio, Erica Ginevra Milano, Carmen Lammi, Giovanni Grazioso","doi":"10.1080/13543776.2026.2674748","DOIUrl":"10.1080/13543776.2026.2674748","url":null,"abstract":"Introduction: Proprotein convertase subtilisin/kexin 9 (PCSK9) modulates the circulating levels of low-density lipoprotein cholesterol (LDL-C). Consequently, PCSK9 inhibition, at any level, from the mRNA transcription to the final interaction with LDL-R, through suitable ligands, has been established as a corroborated therapeutic strategy for fighting hypercholesterolemia, preventing the risks of cardiovascular diseases.Area covered: Patent literature published between 2024 and 2025 in the Espacenet database, an international repository containing more than 150 million documents from over 100 patent‑granting authorities, focusing on disclosures claiming novel compounds designed to bind and inhibit the PCSK9 protein.Expert opinion: The clinical development of small-molecule PCSK9 inhibitors, such as MK-0616 (enlicitide) and AZD0780 (laroprovstat), demonstrates that PCSK9 is still a drug target of great interest for both academic and pharmaceutical companies. Numerous patents deposited in the last two years cover compounds that are structurally related to previously deposited general structures as well as newly developed scaffolds that include quinolines and isoquinolines, peptides, pyridine, and benzothiazole derivatives. However, with mAbs and siRNAs dominating the market, small molecules are required to prove superior cost-efficiency, combination value, and cardiovascular advantages that extend beyond LDL-C reduction.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"537-553"},"PeriodicalIF":4.7,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147928043","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 LPAR1 antagonists (2010 - present). LPAR1拮抗剂专利回顾（2010年至今）。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-06-01 Epub Date: 2026-05-17 DOI: 10.1080/13543776.2026.2671884

Jiaxing Zhao, Yuxing Li, Wangshan Zheng, Yang Liu, Yan Yang, Yan Leng, Shiyu Wei, Jun Lou, Xiaofei Shang, Deping Tang

{"title":"A patent review of LPAR1 antagonists (2010 - present).","authors":"Jiaxing Zhao, Yuxing Li, Wangshan Zheng, Yang Liu, Yan Yang, Yan Leng, Shiyu Wei, Jun Lou, Xiaofei Shang, Deping Tang","doi":"10.1080/13543776.2026.2671884","DOIUrl":"10.1080/13543776.2026.2671884","url":null,"abstract":"Introduction: Lysophosphatidic acid receptor 1 (LPAR1), a G protein-coupled receptor, mediates diverse biological effect. Substantial evidence from human patients and experimental models demonstrates that pathological hyperactivation of LPAR1 in fibroblasts and myofibroblasts contributes to disease progression, establishing it as a key pathological driver in idiopathic pulmonary fibrosis (IPF).Areas covered: This review systematically analyzes peer-reviewed literature retrieved from Web of Science and PubMed, alongside publicly disclosed patents obtained via the IncoPat Patent Search and Analysis platform, covering the period from 2010 to the present. Clinical data were sourced from the Cortellis Drug Discovery Intelligence database.Expert opinion: Small-molecule LPAR1 antagonists show promise as novel therapeutics for IPF, as evidenced by their attenuation of disease progression in two phase II clinical trials. Despite these advancements, LPAR1 antagonist development faces several medicinal chemistry challenges, including the absence of rational structure-based drug design and difficulties in optimizing ADMET properties. Future development avenues include exploring combination therapies, expanding indications, developing long-acting formulations, and investigating novel modalities such as LPAR1-targeting proteolysis-targeting chimeras (PROTACs) and small-interfering RNA (siRNA) therapeutics directed against LPAR1.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"485-513"},"PeriodicalIF":4.7,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147928024","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 agonists of Toll-like receptors 7 and 8: an updated patent review 2021 - 2025. toll样受体7和8的小分子激动剂：更新的专利审查2021 - 2025。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-06-01 Epub Date: 2026-05-15 DOI: 10.1080/13543776.2026.2669076

Akash M Patel, Natalia Chernyak, W Michael Seganish

{"title":"Small molecule agonists of Toll-like receptors 7 and 8: an updated patent review 2021 - 2025.","authors":"Akash M Patel, Natalia Chernyak, W Michael Seganish","doi":"10.1080/13543776.2026.2669076","DOIUrl":"10.1080/13543776.2026.2669076","url":null,"abstract":"Introduction: Toll-like receptors 7 (TLR7) and 8 (TLR8) are endosomal receptors that sense single‑stranded RNA and activate MyD88‑dependent inflammatory signaling, linking innate immune detection to adaptive immune responses. Translational and clinical studies across therapeutic areas have underscored both the therapeutic potential and safety challenges of modulating TLR7/8 activity, driving growing interest in small‑molecule agonists and delivery strategies that enable precise control of receptor engagement.Areas covered: This review highlights recent patent activity on small-molecule TLR7/8 agonists, as well as derived conjugates and alternative modalities. This review covers patents published between January 2021 and August 2025 found using Scifinder-n and Cortellis database searches. We report relevant chemical scaffolds, key trends in structure-activity relationships, innovative conjugation strategies, and, where disclosed, insights from preclinical animal models and clinical data.Expert opinion: Recent patent activity reflects a marked expansion in small‑molecule TLR7/8 agonist development, with increasing emphasis on delivery‑gated strategies. Although systemic agonists and early antibody conjugates have shown preclinical efficacy and tolerability, limited clinical translatability suggests that future progress will depend on integrating agonist design with optimized delivery, linker chemistry, antigen selection, and translational assessment to better balance efficacy and tolerability.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"515-535"},"PeriodicalIF":4.7,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147940376","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