Expert Opinion On Therapeutic Patents[JOURNAL]
Sun
200 papers
Patents involving monoamine oxidase (MAO): a comprehensive update (2022-2025) on its inhibitors and applications.
Shaldam MA, Carradori S, Balaha M … +4 more , Guglielmi P, Diomede F, D'Agostino I, Tawfik HO
Expert Opin Ther Pat · 2026 Apr · PMID 41699413 · Publisher ↗
INTRODUCTION: Monoamine oxidases (MAOs) A and B are key enzymes for the oxidative deamination of monoamine neurotransmitters, including dopamine, serotonin, norepinephrine, and tyramine. Selective MAO-B inhibitors are cl...
INTRODUCTION: Monoamine oxidases (MAOs) A and B are key enzymes for the oxidative deamination of monoamine neurotransmitters, including dopamine, serotonin, norepinephrine, and tyramine. Selective MAO-B inhibitors are clinically employed as adjuvant therapies for neurodegenerative disorders, whereas selective MAO-A inhibitors are mainly considered third-line options in the treatment of depression. However, due to their function in regulating synaptic activity and exogenous monoamine metabolism, research in this field is continually expanding. AREAS COVERED: This review summarizes patents on MAO inhibitors between 2022 and 2025. For the most investigated chemotypes (14 synthetic cores along with compounds from natural sources), biological activities were analyzed. The compounds are divided into two main categories, naturally occurring molecules and newly synthesized derivatives, with a total of 114 compounds discussed. To provide a more comprehensive perspective on the therapeutic potential of these inhibitors, additional treatment alternatives are also outlined. EXPERT OPINION: Recently patented MAO inhibitors show notable properties, including significant isoform selectivity and therapeutic potential toward other diseases, such as fibromyalgia, CDKL5-deficient disorder, neuropathic pain, and Alzheimer's disease.
Recent advances in factor XII(a) inhibitors: an updated patent landscape (2020-present).
Kalinin DV
Expert Opin Ther Pat · 2026 Apr · PMID 41640375 · Publisher ↗
INTRODUCTION: Factor XII (FXII) is a liver-derived plasma zymogen that autoactivates on anionic surfaces to FXIIa, which drives the contact blood coagulation pathway, kallikrein-kinin signaling, fibrinolysis, and classic...
INTRODUCTION: Factor XII (FXII) is a liver-derived plasma zymogen that autoactivates on anionic surfaces to FXIIa, which drives the contact blood coagulation pathway, kallikrein-kinin signaling, fibrinolysis, and classical complement. Although congenital FXII(a) deficiency is largely asymptomatic, dysregulated activity is linked to thrombosis, hereditary angioedema (HAE), and neuroinflammation, making FXII(a) an attractive therapeutic target. AREAS COVERED: This review provides a brief overview of FXII/FXIIa structure and function to highlight its suitability as a therapeutic target. It then summarizes patents published between 2020 and 2025 (patent search using Espacenet, Google Patents, and SciFinder) covering FXII(a)-targeting agents across diverse modalities, including small molecules, proteins and peptides, monoclonal antibodies, oligonucleotides, and siRNAs. EXPERT OPINION: Patent analysis indicates that most FXII(a) inhibitors remain in early preclinical development, though a growing subset has shown efficacy in models of thrombosis, HAE, sepsis, and neuroinflammation. The breadth and pace of 2020-2025 filings, together with accumulating translational data, should accelerate progression from patents to clinical candidates, particularly for contact-activation indications (e.g. device-related thrombosis). Resolving full-length FXII/α-FXIIa structures would further enable allosteric inhibitors design.
Protein tyrosine phosphatase 1B (PTP1B) inhibitors as potential anti-diabetes agents: updated patent review (2019-2023).
Ashfaq R, Hussain H
Expert Opin Ther Pat · 2026 Mar · PMID 41565465 · Publisher ↗
INTRODUCTION: Inhibition of protein tyrosine phosphatase 1B (PTP1B) is a key strategy for improving insulin sensitivity in various cells. This strategy is supported by human genetic data. PTP1B inhibitors are considered...
INTRODUCTION: Inhibition of protein tyrosine phosphatase 1B (PTP1B) is a key strategy for improving insulin sensitivity in various cells. This strategy is supported by human genetic data. PTP1B inhibitors are considered an attractive target for the treatment of T2DM because they improve insulin receptor sensitivity and have the ability to reverse insulin resistance-related diseases. AREAS COVERED: This review provides an overview of the patents that were published between January 2019 and December 2023. The efficacy of potent PTP1B inhibitors for the treatment of T2DM is described in this review. The latest patented studies of PTP1B inhibitors (are summarized by using the keywords 'PTP1B inhibitors,' in PubMed, SciFinder, and Google Patents. EXPERT OPINION: There has been tremendous progress in PTP1B drug discovery. Progress has been made with natural products, semi-synthetic natural product derivatives and heterocyclic hybrid compounds. A number of protocols are being pursued in order to enhance the biological effects of PTP1B inhibitors. In addition, these new advances suggest that it may be possible to obtain small-molecule inhibitors of PTP1B with the required potency and selectivity. In addition, future efforts using an integrated medicinal chemistry and structural biology strategy are expected to lead to potent and selective PTP1B inhibitors.
Novel fatty acid amide hydrolase (FAAH) inhibitors: a patent review from 2015 to 2025.
Landolfi L, Brindisi M, Onnis V … +2 more , Moraca F, Catalanotti B
Expert Opin Ther Pat · 2026 Mar · PMID 41559860 · Publisher ↗
INTRODUCTION: Over the past decade, significant efforts have been made to develop and patent selective fatty acid amide hydrolase (FAAH) inhibitors with favorable pharmacokinetic and safety profiles to modulate pain, inf...
INTRODUCTION: Over the past decade, significant efforts have been made to develop and patent selective fatty acid amide hydrolase (FAAH) inhibitors with favorable pharmacokinetic and safety profiles to modulate pain, inflammation, and neurological disorders. Recently, attention has shifted toward dual inhibitors that combine FAAH inhibition with other targets, such as COXs, MAGL, and sEH, aiming to improve therapeutic outcomes. This review highlights the most significant patents from the last 10 years in this evolving field of research. AREAS COVERED: Patents of selective and nonselective FAAH inhibitors published from 2015 to 2025. Patent searches were conducted on Espacenet, WIPO (World Intellectual Property Organization), and Google Patents databases, while literature search was performed using the Artificial Intelligence (AI) visual tools Connected Papers and Research Rabbit. EXPERT OPINION: The search for novel and clinically relevant FAAH inhibitors starts with newly disclosed chemical entities. However, reducing translation gaps also requires advances in identifying key biomarkers and developing relevant animal models that mimic target diseases. Additionally, disclosing of innovative chemical templates, including those for allosteric modulation of FAAH, and the identification of suitable and innovative multitarget directed ligands will likely establish FAAH inhibitors as a validated therapeutic option for several diseases.
A patent review of galectin-1 and galectin-3 inhibitors and their potential therapeutic applications (2022-present): an update.
Sethi A, Alvala M
Expert Opin Ther Pat · 2026 Mar · PMID 41537711 · Publisher ↗
INTRODUCTION: Galectin-1 (Gal-1) & Galectin-3 (Gal-3) are carbohydrate-binding proteins implicated in diverse pathological processes. These galectins have emerged as key therapeutic targets, with significant presence in...
INTRODUCTION: Galectin-1 (Gal-1) & Galectin-3 (Gal-3) are carbohydrate-binding proteins implicated in diverse pathological processes. These galectins have emerged as key therapeutic targets, with significant presence in drug discovery pipelines and clinical investigations. Their unique glycan-binding properties and immunomodulatory effects have prompted the development of inhibitors to modulate their function. AREAS COVERED: This review presents a comprehensive summary of 19 small-molecule patents targeting Gal-1 and Gal-3, published from January 2022 to June 2025. A systematic search of Reaxys and WIPO databases yielded patents spanning modified monosaccharides & disaccharides, non-carbohydrate chemotypes and metal-coordinated complexes. EXPERT OPINION: The patent landscape is dominated by β-D-galactopyranose and thiodigalactoside scaffolds, with limited innovation and unresolved issues in selectivity, drug-likeness, and efficacy, highlighted by GB0139's Phase II failure. Moreover, only a few patents provide structural evidence and strong in vitro/in vivo data, limiting confidence in their therapeutic outcome. By contrast, some diversification has emerged, including spirocyclic sugars, ruthenium-conjugates and non-carbohydrate ligands such as heterocycles and repurposed drugs. These highlight underexploited avenues with promise. Yet, robust biochemical data and structural proof of binding remain scarce. To move the field forward, future patents must diversify chemotypes, substantiate binding modes with crystallography or NMR, and demonstrate translation in relevant disease models.
A patent review of DNA polymerase theta (Polθ) targeted therapies (2019-2025).
Ma L, Luo M, Xiang H … +1 more , Luo G
Expert Opin Ther Pat · 2026 Mar · PMID 41518123 · Publisher ↗
INTRODUCTION: DNA Polymerase theta (Polθ), a critical multifunctional DNA repair enzyme in the alternative non-homologous end joining (alt-NHEJ) pathway, has recently emerged as a new promising synthetic lethal target fo...
INTRODUCTION: DNA Polymerase theta (Polθ), a critical multifunctional DNA repair enzyme in the alternative non-homologous end joining (alt-NHEJ) pathway, has recently emerged as a new promising synthetic lethal target for homologous recombination (HR) deficient cancers. Since the first-in-class Polθ polymerase inhibitor entered clinical trials in 2021, this field has witnessed explosive growth in interest, underscored by a surge in Polθ inhibitor patents and nine candidates progressing to clinical trials. AREAS COVERED: This comprehensive patent review focuses on structural features and biochemical profiles of both Polθ inhibitors reported between 2019 and 2025, leveraging patents retrieved from the databases of World Intellectual Property Organization (WIPO), United States Patent and Trademark Office (USPTO), Cortellis Drug Discovery Intelligence, and China National Intellectual Property Administration (CNIPA). EXPERT OPINION: The rapid progress of Polθ inhibitors highlights their potential as a synthetic lethal strategy for HR-deficient cancers. Recently, an increasing number of patents and articles on inhibitors targeting Polθ have been published. At present, a total of nine Polθ inhibitors are under study in early clinical trials. Artios' Polθ inhibitor ART6043 has excellent clinical data. The results of these trials will influence the future development of Polθ inhibitors for HR-deficient cancers.
LAG-3 antagonists for cancer treatment: an updated patent review (2020-2025).
Pérez-Santos M, Landeta G, Anaya-Ruiz M … +8 more , Martínez-Morales P, Flores-Robles D, Jaramillo-Loranca B, Vargas-Hernández G, Ramos-Enriquez R, Dublán-García O, Guerrero-González T, Marroquín-Gutiérrez F
Expert Opin Ther Pat · 2026 Feb · PMID 41504154 · Publisher ↗
INTRODUCTION: LAG-3 is a molecule overexpressed on the surface of CD4+ and CD8+ cells in the tumor microenvironment that prevents T-cell activation and production of IL-2 and IFN-γ. AREAS COVERED: Using the patent databa...
INTRODUCTION: LAG-3 is a molecule overexpressed on the surface of CD4+ and CD8+ cells in the tumor microenvironment that prevents T-cell activation and production of IL-2 and IFN-γ. AREAS COVERED: Using the patent databases of the State Patent and Trademark Office, the European Patent Office, the World Intellectual Property Organization, the Japanese Patent Office, the State Intellectual Property Office of China, and the Korean Intellectual Property Office, a detailed patent landscape of LAG-3 antagonists was generated, categorizing them as monospecific anti-LAG-3 antibodies, multispecific anti-LAG-3 antibodies, LAG-3 binding peptides, LAG-3 binding small molecules, and LAG-3 therapeutics. EXPERT OPINION: The trend shows that monospecific antibodies against LAG-3 continue to be the main antagonists, followed by multispecific t, treatment methods using known LAG-3 antagonists, LAG-3 binding peptides, and LAG-3 binding small molecules. The monospecific antibodies encelimab, miptenalimab, and the bispecific antibodies tobemstomig, IBI323, ABL501, fanastomig, and FS118 are added, during this period, to the potential drugs targeting LAG-3.
A patent review of KDM4 histone demethylase inhibitors (2014-present).
Yang X, Han Y, Yu L … +1 more , Xu S
Expert Opin Ther Pat · 2026 Mar · PMID 41504014 · Publisher ↗
INTRODUCTION: The KDM4 family of histone demethylases, characterized by a conserved JmjC catalytic domain, comprises six subtypes: KDM4A - F. Aberrant expression of these enzymes has been associated with tumorigenesis ac...
INTRODUCTION: The KDM4 family of histone demethylases, characterized by a conserved JmjC catalytic domain, comprises six subtypes: KDM4A - F. Aberrant expression of these enzymes has been associated with tumorigenesis across various malignancies, highlighting their potential as therapeutic targets in oncology. To date, a series of KDM4 inhibitors have been developed, among which TACH101 is undergoing clinical evaluation for cancer treatment. AREAS COVERED: This review provides a comprehensive overview of the patent literature on KDM4 inhibitors, derived from a systematic search utilizing the Cortellis Drug Discovery Intelligence database. A total of 17 patent applications, published within the period from June 2014 to May 2025, were identified and critically analyzed. EXPERT OPINION: Significant progress has been achieved in the development of KDM4 inhibitors; however, most current compounds continue to face major challenges, including poor membrane permeability, limited cellular potency, and low isoform specificity. Strategies such as designing inhibitors with novel scaffolds, developing covalent inhibitors, advancing protein degraders, and targeting non-catalytic domains may provide viable solutions to these limitations. In addition, the physiological and pathological roles of KDM4 remain insufficiently characterized. Further in-depth investigations into the biological functions of KDM4 will be essential to guide the rational design and facilitate the clinical translation of KDM4-targeted therapeutics.
The future of BRD9 inhibitors: a patent perspective (2019-present).
Boccia E, Terracciano S, Chini MG … +2 more , Bifulco G, Lauro G
Expert Opin Ther Pat · 2026 Feb · PMID 41409030 · Publisher ↗
INTRODUCTION: Bromodomain-containing protein 9 (BRD9) is an epigenetic reader component of the non-canonical BAF (BRG1/BRM-Associated Factors) chromatin remodeling complex, involved in the regulation of transcription. Th...
INTRODUCTION: Bromodomain-containing protein 9 (BRD9) is an epigenetic reader component of the non-canonical BAF (BRG1/BRM-Associated Factors) chromatin remodeling complex, involved in the regulation of transcription. The ncBAF complex differs from the other two complexes, the canonical BAF and PBAF, as it contains unique subunits encoded by genes including BRD9, GLTSCR1 (Glioma Tumor Suppressor Candidate Region 1), and GLTSCR1L (GLTSCR1-Like). In recent years, BRD9 has emerged as a promising therapeutic target in several diseases. AREAS COVERED: This review explores the most compelling patents released from 2019 to 2025 concerning compounds, classified as small molecules and protein degraders (PROTACs), interfering with BRD9 activity. Relevant patents were identified through searches in European Patent Office (EPO) and World Intellectual Property Organization WIPO databases. EXPERT OPINION: The patent landscape reflects a growing interest in BRD9 as an epigenetic target for its key role in various pathologies. The recent patent data show how selective BRD9 degraders represent a significant step forward in terms of efficacy and selectivity, with promising results in preclinical models of acute myeloid leukemia (AML), synovial sarcoma (SS), and Huntington's disease (HD). Despite several critical issues, the selective degradation of this epigenetic target shows great potential to be an innovative therapeutic strategy.
Impact of patent-granting differences between Japan and the United States on patent protection for medical methods: insights from genome editing patents.
Matsuoka T, Kano S
Expert Opin Ther Pat · 2026 Feb · PMID 41396047 · Publisher ↗
INTRODUCTION: Securing patents in multiple countries has become essential for the development of global medical products. However, differences in national patent systems result in varying patentability standards. Althoug...
INTRODUCTION: Securing patents in multiple countries has become essential for the development of global medical products. However, differences in national patent systems result in varying patentability standards. Although global claim construction strategies have been applied in practice, these approaches have not yet been systematically organized. AREA COVERED: This study examines how the patent scope for patent families of international applications related to genome editing technologies filed in 2013, differs between Japan, where medical method patents are prohibited, and the United States, where such patents are permitted. EXPERT OPINION: For CRISPR-Cas system patents, claim structures varied significantly, even among the corresponding family patents. To navigate these differences, the following strategies were proposed for filing patents in countries that prohibit medical method patents such as Japan: Convert medical method claims in the U.S. into composition claims that include product inventions, as this process ensures that such claims allow for the enforcement of rights against the suppliers of infringing products.Clearly define the scope of the claimed use-inventions when specifying the characteristics of the product based on its effects.Explicitly describe cells produced by a specific manufacturing method within the claimed rights.
An updated patent review of acetylcholinesterase inhibitors for the treatment of Alzheimer's disease (2021-present).
Begines P, Fernández-Bolaños JG, López Ó
Expert Opin Ther Pat · 2026 Feb · PMID 41378779 · Publisher ↗
INTRODUCTION: Alzheimer's disease (AD) is a multifactorial neurodegenerative disorder with a complex and not fully elucidated etiology. An exponential rise in its incidence underscores the urgent need for effective thera...
INTRODUCTION: Alzheimer's disease (AD) is a multifactorial neurodegenerative disorder with a complex and not fully elucidated etiology. An exponential rise in its incidence underscores the urgent need for effective therapeutic strategies. AD imposes a significant economic burden on public healthcare systems and on patient's families. AREAS COVERED: This manuscript focuses on the review of potent acetylcholinesterase (AChE) inhibitors, either through chemical synthesis or isolation from natural sources, aimed at restoring acetylcholine levels. Most of the compounds discussed act as multitarget agents and are categorized into four groups: drug derivatives (9 patents), heterocyclic scaffolds (16 patents), natural products from plant extracts (12 patents), and synthetic compounds inspired by natural templates (18 patents). EXPERT OPINION: AChE inhibition remains a compelling target in AD drug design, as it enhances acetylcholine levels and can alleviate cognitive decline. Furthermore, inhibitors that interact with the peripheral anionic site (PAS) of AChE may reduce β-amyloid self-aggregation, thereby preventing the deposition of neurotoxic peptides in the brain. However, targeting AChE alone is insufficient for the development of effective therapeutics. A multitarget approach, combining AChE inhibition with pharmacophores addressing β-amyloid aggregation, neuroinflammation, oxidative stress, and other pathological hallmarks, holds greater promise for the development of more efficient anti-Alzheimer's agents.
Tricyclic boronic acids as broad-spectrum serine and metallo-β-lactamase inhibitors with activity against : a patent evaluation (US 2025/0223303).
Krajnc A
Expert Opin Ther Pat · 2026 Feb · PMID 41376240 · Publisher ↗
INTRODUCTION: With β-lactams remaining the most widely prescribed antibacterials worldwide, their continuing clinical efficacy remains an important therapeutic goal. Rapid spread of serine and metallo-ß-lactamases (SBLs...
INTRODUCTION: With β-lactams remaining the most widely prescribed antibacterials worldwide, their continuing clinical efficacy remains an important therapeutic goal. Rapid spread of serine and metallo-ß-lactamases (SBLs and MBLs, respectively), which can inactivate β-lactams, is increasingly threatening this objective. Finding clinically useful inhibitors of MBLs, for which no FDA- carbapenem-resistant infections approved treatment currently exists, is of interest. AREAS COVERED: This article concisely reviews structurally novel xeruborbactam-inspired tricyclic boronate SBL/MBL inhibitors (as reported in US 2025/0223303) with promising inhibitory activities . The literature search was conducted using SciFinder and Patentscope. By introducing novel thioether-based C5 sidechains onto the previously optimized bicyclic boronate core, the inventors explored novel chemical space yielding SBL/MBL inhibitors with promising activities against carbapenem-resistant (CR) , , and, importantly, , when used in combination with meropenem and/or biapenem (at least with respect to taniborbactam, i.e. boronate inhibitor in late-stage clinical development). EXPERT OPINION: Due to the major societal importance of β-lactams for modern medicine, and the clearly demonstrated clinical potential of functionalized (bi)cyclic boronates as potent dual-acting SBL/MBL inhibitors when used in combination therapies, there is ample opportunity and scope for continued investigation of this pharmacophore, particularly in the context of discovering new therapeutic options for CR infections.
Lysine demethylase (KDM) inhibitors for the treatment of cancer: a patent review (2015-present).
Sarno F, Conte M, Muro A … +6 more , Dell'Aversana C, Sgueglia G, Carafa V, Del Gaudio N, Nebbioso A, Altucci L
Expert Opin Ther Pat · 2026 Jan · PMID 41368926 · Publisher ↗
INTRODUCTION: Lysine demethylases (KDMs) are crucial epigenetic regulators that modulate gene expression via demethylation of histone and non-histone proteins, playing a pivotal role in cancer progression. Dysregulation...
INTRODUCTION: Lysine demethylases (KDMs) are crucial epigenetic regulators that modulate gene expression via demethylation of histone and non-histone proteins, playing a pivotal role in cancer progression. Dysregulation of KDM activity, particularly in KDM1A, KDM4, KDM5, and KDM6, has been linked to several cancers, including leukemia and breast, lung, and prostate cancers, leading to the emergence of KDM inhibitors (KDMi) as promising therapeutic agents. These inhibitors target KDMs by mimicking cofactors, chelating metal ions, or competing with histone substrates to disrupt demethylation. Some of the most studied KDMi are those targeting KDM1A. AREAS COVERED: In this review, we critically explore the complex roles of KDMs in cancer, provide a detailed overview of patents describing KDMi published from 2015 to the present, and assess European clinical trials investigating KDMi developed for cancer therapy. EXPERT OPINION: Despite the promising potential of KDMi, their clinical development is hampered by significant challenges including safety concerns, suboptimal patient enrollment, and difficulties in optimizing dosing regimens and identifying reliable biomarkers. Future research must focus on refining dosing protocols, discovering predictive biomarkers, and developing effective combination therapies to maximize patient outcomes, ultimately realizing the full promise of KDMi in cancer treatment.
Coactivator-associated arginine methyltransferase 1 (CARM1) inhibitors: a patenting perspective (2018-present).
Viviano M, Cipriano A, Feoli A … +3 more , Milite C, Castellano S, Sbardella G
Expert Opin Ther Pat · 2026 Feb · PMID 41351327 · Publisher ↗
INTRODUCTION: CARM1 (Coactivator-associated arginine methyltransferase 1), also known as PRMT4 (Protein Arginine Methyltransferase 4), is a type I PRMT that regulates gene expression by methylating both histone and non-h...
INTRODUCTION: CARM1 (Coactivator-associated arginine methyltransferase 1), also known as PRMT4 (Protein Arginine Methyltransferase 4), is a type I PRMT that regulates gene expression by methylating both histone and non-histone substrates. Its overexpression and functional dysregulation have been linked to the progression of several cancer types, including breast, prostate, and hematological malignancies, positioning CARM1 as a compelling target for therapeutic intervention. In this scenario, the development of selective and potent CARM1 inhibitors holds great promise for the treatment of cancer by modulating epigenetic pathways and altering oncogenic transcriptional programs. However, designing effective inhibitors is challenging due to the conserved nature of the PRMT catalytic domain and the need for high selectivity to minimize off-target effects. AREAS COVERED: This review aims at giving an overview of the recent patent literature of CARM1 inhibitors between 2018 and 2025. WIPO, EPO, USPTO, and SciFinder databases were used for the search of patents. EXPERT OPINION: Although the development of selective CARM1 inhibitors presents significant challenges, it remains a highly promising endeavor due to its potential to greatly advance anticancer drug discovery. Various strategies, including PROTACs can be employed to inactivate the protein, leading to antitumor effects.
A patent review of Mpro protease inhibitors for the treatment of COVID-19 infections (2020 - present).
Mik V, Benz LS, Voller J … +3 more , Dunzendorfer-Matt T, Weiss MS, Kryštof V
Expert Opin Ther Pat · 2026 Jan · PMID 41348159 · Publisher ↗
INTRODUCTION: The SARS-CoV-2 main protease (Mpro, also known as 3CLpro or nsp5) is essential for viral replication. As there are no close human homologs, it represents an attractive and specific target for antiviral ther...
INTRODUCTION: The SARS-CoV-2 main protease (Mpro, also known as 3CLpro or nsp5) is essential for viral replication. As there are no close human homologs, it represents an attractive and specific target for antiviral therapy against COVID-19. Its well-defined active site and conserved substrate specificity have enabled structure-guided drug design with high precision. AREAS COVERED: This review examines the patent landscape for small-molecule inhibitors of SARS-CoV-2 Mpro published between 2020 and early 2025. Compounds were grouped by scaffold type and mechanism of action, covering covalent and non-covalent inhibitors, orthosteric and allosteric binders and unique modalities such as PROTACs. Clinically advanced agents including nirmatrelvir, ensitrelvir, simnotrelvir, zevotrelvir and leritrelvir are highlighted alongside structurally novel leads and broad-spectrum candidates. EXPERT OPINION: A number of Mpro inhibitors have progressed into preclinical and clinical stages, underscoring the rapid advancement in this field. The accumulation of structural knowledge, chemical diversity and mechanistic insight has laid a robust foundation for future antiviral development and may further enhance the utility of Mpro inhibitors against evolving coronaviruses.
Patent landscape in hydroxamic acid-based HDAC inhibitors (2020-2024): structure-activity relationships and mechanistic insights.
Shirbhate E, Singh V, Prabha V … +5 more , Karthikeyan C, Tiwari AK, Veerasamy R, Yasin HKA, Rajak H
Expert Opin Ther Pat · 2026 Jan · PMID 41251288 · Publisher ↗
INTRODUCTION: The hydroxamic acid-based histone deacetylase (HDAC) inhibitors play a crucial role as anticancer chemotherapeutics. It controls cellular pathways and epigenetically modifies gene expression, making them im...
INTRODUCTION: The hydroxamic acid-based histone deacetylase (HDAC) inhibitors play a crucial role as anticancer chemotherapeutics. It controls cellular pathways and epigenetically modifies gene expression, making them important for tackling the complicated character of cancer etiology. AREAS COVERED: The action of current HDAC inhibitors on different target proteins and multiple-cancer cell lines are studied. The study underlines a comprehensive summary of different compounds published as patents from 2020 to 2024 and retrieved from Google patents, paying special attention to their structural differences and possible applications in cancer treatment. It stands out in today's scenario by providing structure-activity relationships (SAR) and mechanistic insights for heterocyclic scaffold-like pyrimidine, quinazoline, oxadiazole, thiadiazole, thiazole, piperazine, pyridine, indole and chromane rings used in the design of HDAC inhibitor. EXPERT OPINION: Results reveal significant development in the synthesis of selective HDAC inhibitors with IC values in the nano and micromolar range, exceeding conventional inhibitors as vorinostat. Dual-targeting approaches have also evolved as sensible substitutes using molecules that improve treatment efficacy while reducing side effects. Thorough investigation on SAR across various heterocyclic scaffolds benefits future drug development projects, aimed at improving selectivity and minimizing side effects in cancer treatment.
A patent review of topoisomerase 1 inhibitors (2021-present).
Fuertes M, Martín-Encinas E, Selas A … +1 more , Alonso C
Expert Opin Ther Pat · 2026 Jan · PMID 41236376 · Publisher ↗
INTRODUCTION: Among the different topoisomerases, essential enzymes that play an important role in DNA processes such as replication and transcription, type I enzymes are targets of particular clinical importance for ant...
INTRODUCTION: Among the different topoisomerases, essential enzymes that play an important role in DNA processes such as replication and transcription, type I enzymes are targets of particular clinical importance for anticancer and antiparasitic drugs. Bearing this in mind, in the last 5 years specific inhibitors, both poison and suppressor types, have been patented for this target. AREAS COVERED: This review covers the patent literature on topoisomerase 1 inhibitors and their application published between late 2020-present. EXPERT OPINION: TOP1 inhibitors are being used in combination with synergistic therapies within a multimodal approach, including targeted therapies, adaptive immunotherapy, and the blockade of DNA repair mechanisms. Advances in drug delivery systems, especially antibody-drug conjugates (ADCs), are revolutionizing chemotherapy by enabling localized and tumor-specific drug release. In addition to traditional inhibitors like irinotecan and topotecan, new agents such as deruxtecan and govitecan have been approved, expanding therapeutic options. Moreover, small new molecules with more promising clinical potential are being developed.
Sirtuin modulators: a review of patents from 2020 to 2024.
Fabbrizi E, Fiorentino F, Mai A … +1 more , Rotili D
Expert Opin Ther Pat · 2026 Jan · PMID 41186927 · Publisher ↗
INTRODUCTION: Sirtuins have gained significant prominence in scientific research due to their involvement in a wide array of biological processes, including DNA repair, genome stability, transcription modulation, and sig...
INTRODUCTION: Sirtuins have gained significant prominence in scientific research due to their involvement in a wide array of biological processes, including DNA repair, genome stability, transcription modulation, and signal transduction. Dysregulation of their function has been implicated in various pathologies, including cancer, where sirtuins exhibit context-dependent effects. Consequently, the development of sirtuin inhibitors and activators remains an exceptionally important field of research, focusing on the design of selective modulators targeting individual sirtuin isoforms. AREAS COVERED: This review includes the patents regarding sirtuin modulators released from 2020 to 2024 and provides a concise overview of the most relevant modulators developed so far. Relevant patents were systematically identified through comprehensive searches in PubMed (https://pubmed.ncbi.nlm.nih.gov), Google Patents (https://patents.google.com), and Espacenet (https://worldwide.espacenet.com). EXPERT OPINION: Sirtuin modulators are pivotal in addressing aging, metabolism, cancer, and neurodegeneration. Sirtuins regulate key cellular processes like DNA repair, genome stability, and mitochondrial function. Activators show promise in mitigating many age-related diseases such as type 2 diabetes and neurodegeneration. Inhibitors demonstrate efficacy in oncology and neurodegenerative conditions. Advances in PROTAC technology enable selective degradation of specific isoforms, enhancing therapeutic precision. With progress in drug design and high-throughput screening, sirtuin modulators hold immense potential to revolutionize treatments for complex medical challenges.
Therapeutic applications of benzoxaborole compounds: a patent and literature analysis (2019-2024).
Giovannuzzi S, Nocentini A, Supuran CT … +1 more , Winum JY
Expert Opin Ther Pat · 2025 Dec · PMID 41104783 · Publisher ↗
INTRODUCTION: Benzoxaborole is a boron-based heterocyclic scaffold with remarkable potential in medicinal chemistry. Its unique chemical structure and compatibility with biological systems have enabled the development of...
INTRODUCTION: Benzoxaborole is a boron-based heterocyclic scaffold with remarkable potential in medicinal chemistry. Its unique chemical structure and compatibility with biological systems have enabled the development of innovative drug candidates. Benzoxaborole derivatives exhibit diverse biological activities, including antibacterial, antifungal, antiparasitic, antiviral, anticancer, and anti-inflammatory effects, making them valuable in addressing various medical challenges. AREAS COVERED: This manuscript reviews the medicinal chemistry literature and patent landscape from 2019 to 2024, focusing on the therapeutic potential of benzoxaborole-based compounds. EXPERT OPINION: Benzoxaboroles are gaining recognition as a versatile and innovative class of therapeutics with strong potential in infectious diseases, oncology, and inflammatory conditions. Their unique boron-containing scaffold enables diverse biological interactions and favorable pharmacokinetic properties. While clinical data are still emerging, early results and robust patent activity suggest significant therapeutic value. Advances in synthetic methods, targeted delivery, and computational design are accelerating their development. With continued focused research and strategic clinical validation, benzoxaboroles are well-positioned to address pressing medical challenges, particularly antimicrobial resistance, and could become an integral part of future treatment paradigms across multiple therapeutic areas.
Medicinal chemistry perspective of ERK1/2 inhibitors in cancer treatment: an updated patent review (2019-present).
Singh AK, Chauhan A, Prajapati V … +4 more , Kumar A, Singh H, Verma A, Kumar P
Expert Opin Ther Pat · 2025 Dec · PMID 41084128 · Publisher ↗
INTRODUCTION: The mitogen-activated protein kinase (MAPK) pathway also known as the RAS/RAF/MEK/ERK pathway is a vital intracellular signaling cascade that regulates apoptosis, differentiation, proliferation, and signal...
INTRODUCTION: The mitogen-activated protein kinase (MAPK) pathway also known as the RAS/RAF/MEK/ERK pathway is a vital intracellular signaling cascade that regulates apoptosis, differentiation, proliferation, and signal transduction. AREA COVERED: This review focuses on the critical role of ERK1/2 in the MAPK pathway and its implication in various cancers. It presents a detailed analysis of ERK1/2 inhibitors currently undergoing clinical evaluation, along with recently patented ERK1/2 inhibitors. The data were compiled by systematically searching databases including SciFinder, PubMed, Scopus, Google Scholar, and Google Patents using the keyword 'ERK' for the period 2019 to the present. EXPERT OPINION: Since 2019, several heterocyclic ERK1/2 inhibitors have shown promise in overcoming resistance within the MAPK cascade. However, detailed investigations into mutant versus wild-type ERK1/2 binding dynamics remain sparse, and the development of non-traditional approaches like PROTAC-mediated ERK degradation is still in its nascent stage. To successfully transition ERK1/2 inhibitors from bench to bedside, several strategic directions must be prioritized. First, overcoming resistance remains a critical challenge. Future ERK inhibitors must effectively target downstream components. Second, there is a pressing need to move beyond traditional ATP-competitive inhibitors. In addition, the pharmacological properties of ERK-targeting agents to enhance clinical efficacy and safety.
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