Expert Opinion on Therapeutic Patents最新文献

A patenting perspective of IKZF2 molecular glue degraders (2020-present). IKZF2分子胶水降解剂专利展望（2020-至今）

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-10-15 DOI: 10.1080/13543776.2026.2748593

Xuqing Zhang

{"title":"A patenting perspective of IKZF2 molecular glue degraders (2020-present).","authors":"Xuqing Zhang","doi":"10.1080/13543776.2026.2748593","DOIUrl":"10.1080/13543776.2026.2748593","url":null,"abstract":"Introduction: IKZF2 (Helios) maintains the suppressive function of regulatory T cells (Tregs) and is an emerging immuno-oncology target. Its degradation destabilizes Tregs, strengthens antitumor immunity, and may remodel the tumor microenvironment (TME) with reduced off-target toxicity. Recent patents focus on selective cereblon (CRBN)-recruiting molecular glues, combination therapies, and next-generation degraders.Areas covered: SciFinder and Google Patents were searched for IKZF2 molecular glue degraders reported in patents and peer-reviewed journals from January 2020 to September 2026.Expert opinion: The immunomodulatory drug (IMiD)-based degrader field is increasingly competitive, with growing emphasis on selectivity, alternative ligases, and artificial intelligence-enabled discovery. Because small structural changes can strongly affect ternary-complex formation and selectivity among IKZF proteins, structure-guided optimization remains essential. Dual degradation of IKZF2 and IKZF4 (Eos) may offer further opportunities, but programs must demonstrate differentiated biology, biomarker-guided patient selection, and clear clinical value.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-24"},"PeriodicalIF":4.7,"publicationDate":"2026-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149165377","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

Positive allosteric modulators of AMPA receptors: advances and emerging trends. AMPA受体的正变构调节剂：进展和新趋势。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-10-13 DOI: 10.1080/13543776.2026.2748595

Thomas Colson, Bernard Pirotte, Pierre Francotte

{"title":"Positive allosteric modulators of AMPA receptors: advances and emerging trends.","authors":"Thomas Colson, Bernard Pirotte, Pierre Francotte","doi":"10.1080/13543776.2026.2748595","DOIUrl":"https://doi.org/10.1080/13543776.2026.2748595","url":null,"abstract":"Introduction: AMPA receptors are key mediators of excitatory neurotransmission and attractive targets for central nervous system disorders. An updated review of AMPA receptor positive allosteric modulators is timely given recent medicinal chemistry advances and renewed translational interest.Areas covered: This review summarizes the evolution from early high-impact, seizure-prone ampakines to more refined low- to intermediate-impact modulators based on sulfur-containing heterocycles and sulfonamide scaffolds. We discuss the main structural and functional determinants of AMPA receptor pharmacology, including the dimer-interface allosteric site, flip/flop splice variants, and auxiliary proteins such as TARPs. Key chemotypes covered include benzamides, benzothiadiazines, benzoxathiazines such as TAK-653 and LT-102, constrained sulfonamides such as PF-04958242, PF-4778574 and MDI-222, and newer heterocyclic and bivalent ligands. Literature was selected through a focused review of published medicinal chemistry, pharmacology, and translational studies relevant to AMPA receptor PAMs.Expert opinion: AMPA receptor potentiation remains a promising strategy, but future candidates will need to combine potency, finely tuned efficacy, favorable pharmacokinetics, and circuit-level selectivity. The most successful next-generation PAMs will likely be those that maximize therapeutic window while minimizing seizure liability.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":""},"PeriodicalIF":4.7,"publicationDate":"2026-10-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149180332","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

Corrigendum. 勘误表。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-10-01 Epub Date: 2017-02-28 DOI: 10.1080/13543776.2017.1299338

引用次数: 0

Selective PARP1 inhibitors (2021-2025): patent landscape, structural evolution, and future therapeutic opportunities. 选择性PARP1抑制剂（2021-2025）：专利格局、结构演变和未来治疗机会

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-10-01 Epub Date: 2026-08-24 DOI: 10.1080/13543776.2026.2722028

Jilong Duan, Yanjing Duan, Dongling Gu, Jia Yang, Fenghua Kang, Youchao Deng, Dongsheng Cao

{"title":"Selective PARP1 inhibitors (2021-2025): patent landscape, structural evolution, and future therapeutic opportunities.","authors":"Jilong Duan, Yanjing Duan, Dongling Gu, Jia Yang, Fenghua Kang, Youchao Deng, Dongsheng Cao","doi":"10.1080/13543776.2026.2722028","DOIUrl":"10.1080/13543776.2026.2722028","url":null,"abstract":"Introduction: Poly(ADP-ribose) polymerase 1 (PARP1) is a key mediator of DNA damage repair and an attractive therapeutic target for homologous recombination-deficient malignancies. The development of selective PARP1 inhibitors has been driven by the need to reduce the hematological toxicities associated with nonselective PARP inhibition.Area covered: This review summarizes patents and recent advances in selective PARP1 inhibitors reported from 2021 to the present. Particular emphasis is placed on the structural evolution of AZD5305-derived compounds and emerging quinazolinone- and isoquinolinone-based chemotypes. Key design strategies, including adenine-pocket optimization, linker remodeling, conformational restriction, and scaffold diversification, are discussed together with their impact on PARP1 selectivity and biological activity.Expert opinion: Selective PARP1 inhibition has become a major focus of innovation in the PARP field. Current patents indicate that adenine-pocket engagement, linker optimization, conformational control, and scaffold innovation are central to achieving high PARP1 selectivity and represent important directions for future intellectual property development. Despite significant progress, the disclosed chemical space remains relatively limited, highlighting opportunities for further scaffold diversification and differentiated patent strategies. These advances are expected to facilitate the development of next-generation PARP1-targeted therapeutics with improved safety profiles and broader clinical potential.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"965-990"},"PeriodicalIF":4.7,"publicationDate":"2026-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148790201","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 STAT6 inhibitors and modulators (2020 - present). STAT6抑制剂和调节剂的最新专利审查（2020年至今）。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-10-01 Epub Date: 2026-08-07 DOI: 10.1080/13543776.2026.2713551

Muhammad Zafar Irshad Khan, Bo-Qun Du, Mei Xue, Meng-Qian Yu, Shun-Ran Li, Jianshe Wang, Chen-Chen Wang, Xiang-Yang Ye

{"title":"An updated patent review of STAT6 inhibitors and modulators (2020 - present).","authors":"Muhammad Zafar Irshad Khan, Bo-Qun Du, Mei Xue, Meng-Qian Yu, Shun-Ran Li, Jianshe Wang, Chen-Chen Wang, Xiang-Yang Ye","doi":"10.1080/13543776.2026.2713551","DOIUrl":"10.1080/13543776.2026.2713551","url":null,"abstract":"Introduction: Signal Transducer and Activator of Transcription 6 (STAT6) is a critical transcription factor in the interleukin-4 (IL-4) and IL-13 signaling pathways and serves as a key pathogenic driver of type 2 (TH2) immune responses. Dysregulated STAT6 activity is implicated in asthma, atopic dermatitis, autoimmune diseases, eosinophilic disorders, and certain cancers. As such, targeting STAT6 presents a promising therapeutic strategy for these diseases.Areas covered: This review provides a comprehensive analysis of patent strategies for targeting STAT6 from 2020 to the present. We categorize and evaluate chemical entities based on their core structural features, highlighting key motifs, major patent assignees, and the progression of lead candidates through preclinical and clinical development.Expert opinion: Recent advances reflect a clear evolution from broad JAK/STAT pathway inhibitors toward highly selective STAT6-targeted agents. Although research and development in this area are progressing rapidly with significant achievements, key challenges remain - including optimizing pharmacokinetic properties, achieving tissue specificity, and mitigating off-target effects. The emergence of bifunctional degraders, such as PROTACs, represents a promising frontier for achieving complete and sustained pathway suppression. Future success will likely depend on combining innovative chemistry with sophisticated patient stratification biomarkers to translate potent STAT6 inhibition into safe, effective therapies.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"911-936"},"PeriodicalIF":4.7,"publicationDate":"2026-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148677781","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 TEAD modulators (2022-present). TEAD调制器的最新专利审查（2022年至今）。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-10-01 Epub Date: 2025-07-04 DOI: 10.1080/13543776.2025.2522747

Dounan Xu, Jiahuan Zhong, Yuhan Zeng, Xianhui Zhang, Chengyu Wang, Cheng Luo, Huan Xiong

{"title":"An updated patent review of TEAD modulators (2022-present).","authors":"Dounan Xu, Jiahuan Zhong, Yuhan Zeng, Xianhui Zhang, Chengyu Wang, Cheng Luo, Huan Xiong","doi":"10.1080/13543776.2025.2522747","DOIUrl":"10.1080/13543776.2025.2522747","url":null,"abstract":"Introduction: The Transcriptional Enhanced Associated Domain (TEAD) family has attracted increasing attention due to its crucial role in the Hippo signaling pathway, which regulates cell growth, division, survival, differentiation, and tissue homeostasis in multicellular organisms. Inhibition of TEADs with small molecules has been shown to be an effective strategy for the treatment of tumors, and several compounds have entered clinical trials as monotherapy and/or combination therapy.Areas covered: Due to the explosion of patent disclosures on TEAD modulators (inhibitors or degraders) in the last two years, this review focuses on the published patent literature on small molecule inhibitors or degraders of TEAD and their applications from June 2022 to present (March 2025), as a complementary update to the previous patent review (2018-2022).Expert opinion: The reported TEAD modulators can be categorized into 4 types: non-covalent inhibitors, covalent inhibitors, protein-protein interaction inhibitors and degraders. Meanwhile, the combination therapy with TEAD inhibitors and other kinases or mutated gene inhibitors has shown promising therapeutic effects in patients with various types of cancer, which has greatly expanded the application field of TEAD inhibitors in disease treatment.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"937-963"},"PeriodicalIF":4.7,"publicationDate":"2026-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144324925","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

Myeloperoxidase (MPO) inhibitors: an updated patent review (2020 - present). 髓过氧化物酶（MPO）抑制剂：更新的专利审查（2020年至今）。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-10-01 Epub Date: 2026-07-30 DOI: 10.1080/13543776.2026.2710223

Zhiwei Meng, Dan Chen, Xingyu Yao, Feng Wang, Zhouling Xie

{"title":"Myeloperoxidase (MPO) inhibitors: an updated patent review (2020 - present).","authors":"Zhiwei Meng, Dan Chen, Xingyu Yao, Feng Wang, Zhouling Xie","doi":"10.1080/13543776.2026.2710223","DOIUrl":"10.1080/13543776.2026.2710223","url":null,"abstract":"Introduction: Myeloperoxidase (MPO), a key enzyme involved in neutrophil extracellular trap formation and other inflammatory processes, has emerged as an attractive therapeutic target for cardiovascular, central nervous system, respiratory, and autoimmune diseases. To date, four irreversible MPO inhibitors have entered clinical trials; however, none have reached the market, highlighting the challenges of MPO drug discovery.Areas covered: This review provides an overview of MPO biology, its pathological roles in inflammatory diseases, and recent advances in MPO drug discovery. It then systematically summarizes patent literature published between 2020 and 2026, identified through Espacenet, Google Patents, and SciFinder, comprehensively covering the structural optimization and pharmacological characterization of emerging MPO inhibitors, including small molecules, peptides, and antibodies.Expert opinion: Patent analysis indicates that MPO drug discovery remains heavily dependent on legacy thioxanthine/deazathioxanthine scaffolds. Current efforts are primarily focused on overcoming historical liabilities through improving target selectivity and pharmacokinetic properties. In parallel, non-thioxanthine chemotypes are emerging, although most still exhibit suboptimal potency and therefore require further optimization. The development of dual- or multi-target MPO inhibitors may represent a promising strategy for addressing complex inflammatory networks.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"893-909"},"PeriodicalIF":4.7,"publicationDate":"2026-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148591082","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

Progress with FAK inhibitors in the patent literature (2020-present). 专利文献中FAK抑制剂的进展（2020年至今）。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-09-20 DOI: 10.1080/13543776.2026.2735861

Bing-Bing Chen, Rui-Peng Feng, Jin-Bo Niu, Jian Song, Yuan-Bo Cui, Sai-Yang Zhang

{"title":"Progress with FAK inhibitors in the patent literature (2020-present).","authors":"Bing-Bing Chen, Rui-Peng Feng, Jin-Bo Niu, Jian Song, Yuan-Bo Cui, Sai-Yang Zhang","doi":"10.1080/13543776.2026.2735861","DOIUrl":"10.1080/13543776.2026.2735861","url":null,"abstract":"Introduction: Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that transduces signals from integrins, receptor tyrosine kinases, and growth factors to orchestrate cell adhesion, migration, and survival. Aberrant FAK hyperactivation promotes tumor proliferation, invasion, anti-apoptosis, and chemoresistance. Consequently, the recent U.S. FDA approval of the FAK inhibitor defactinib combined with avutometinib for recurrent KRAS-mutant low‑grade serous ovarian cancer (LGSOC) validates FAK as a clinically actionable anticancer target.Areas covered: This review discusses recent advances in FAK inhibitor development, focusing on small-molecule patents published from January 2020 to August 2026. A systematic search of SciFinder and WIPO databases was conducted for this period. It categorizes these novel inhibitors into several classes and summarizes their structural features, biological activities, design strategies, and structure-activity relationships (SAR).Expert opinion: Recent advances in FAK drug discovery have driven a transition from conventional kinase inhibition toward broader FAK pathway modulation, including improved inhibitors, dual-target strategies, and targeted protein degradation. The clinical success of defactinib-based combination therapy validates the therapeutic potential of FAK targeting, while emerging approaches offer opportunities to overcome resistance. Future progress will depend on biomarker-guided patient selection, rational combination regimens, and exploration of non-catalytic FAK functions to achieve more effective and durable therapies.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-14"},"PeriodicalIF":4.7,"publicationDate":"2026-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148988290","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

Aurora kinase inhibitors: an updated patent review (2021-present). 极光激酶抑制剂：更新的专利审查（2021年至今）。

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-09-17 DOI: 10.1080/13543776.2026.2733162

Yao-Sheng Zhang, Hong-Yu Zhang, Junmin Zhang, Shi-Wu Chen

引用次数: 0

Global patent landscape of synthetic drugs for melasma (2015-2025): innovation trends, mechanistic shifts, and translational challenges. 黄褐斑合成药物全球专利格局（2015-2025）：创新趋势、机制转变和转化挑战

IF 4.7 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-09-14 DOI: 10.1080/13543776.2026.2726449

Santiago Torres, Diana Marcela Aragón Novoa, José Marcos Teixeira de Alencar Filho, Izabel Almeida Alves

{"title":"Global patent landscape of synthetic drugs for melasma (2015-2025): innovation trends, mechanistic shifts, and translational challenges.","authors":"Santiago Torres, Diana Marcela Aragón Novoa, José Marcos Teixeira de Alencar Filho, Izabel Almeida Alves","doi":"10.1080/13543776.2026.2726449","DOIUrl":"10.1080/13543776.2026.2726449","url":null,"abstract":"Introduction: Melasma is a chronic and highly recurrent hyperpigmentation disorder with substantial psychosocial burden and limited long-term therapeutic control. Because current treatments remain largely centered on conventional melanogenesis inhibition, a patent-based review is needed to clarify how synthetic drug innovation is evolving and whether emerging technologies address unmet therapeutic needs.Areas covered: This review analyzed global patent activity from 2015 to 2025 related to synthetic drugs for melasma. A structured search was conducted in the Espacenet database using the keyword 'melasma' and IPC code A61Q (cosmetic and dermatological preparations). After systematic screening, 17 patent filings were included. The analysis focused on geographic distribution, temporal trends, technological strategies, delivery systems, and mechanisms of action. Most patents (94.1%) were based on reformulation strategies, including novel delivery systems and combinations of existing compounds, while only one described a new chemical entity.Expert opinion: The current patent landscape reflects a predominance of incremental innovation, with limited exploration of disruptive strategies. Future advances will depend on targeting pathways beyond melanogenesis and overcoming key translational barriers, including delivery efficiency, safety, and scalability.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-16"},"PeriodicalIF":4.7,"publicationDate":"2026-09-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148944646","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