Expert Opinion On Therapeutic Patents[JOURNAL]
Sun
200 papers
An updated patent review on rational combinations of HDAC inhibitors for cancer chemotherapy (2020 - present): part 2 - patent published.
Shukla YK, Vandana, Mandal V … +3 more , Asati V, Keservani RK, Bharti SK
Expert Opin Ther Pat · 2025 Aug · PMID 40474435 · Publisher ↗
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. Combi...
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.
Formyl peptide receptor modulators: a patent review and potential applications for inflammatory diseases (2021-2024).
Tsai YF, Yang SC, Hwang TL
Expert Opin Ther Pat · 2025 Aug · PMID 40462544 · Publisher ↗
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 se...
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.
A patent review of IDO1 inhibitors for cancer (2023 - present): an update.
Qiu H, Yin Y, Qin Z … +2 more , Li D, Wang P
Expert Opin Ther Pat · 2025 Jul · PMID 40414695 · Publisher ↗
INTRODUCTION: Indoleamine 2,3-dioxygenase 1 (IDO1) is a promising target in cancer immunotherapy, yet its application faces significant challenges due to complex mechanisms of action. Recent advancements in IDO1 inhibito...
INTRODUCTION: Indoleamine 2,3-dioxygenase 1 (IDO1) is a promising target in cancer immunotherapy, yet its application faces significant challenges due to complex mechanisms of action. Recent advancements in IDO1 inhibitors aim to tackle these issues, potentially paving the way for successful therapeutic development. AREAS COVERED: This review highlights patent publications (2023-2024) related to IDO1 inhibitors with potential anti-cancer applications, sourced from Espacenet and Google Scholar. EXPERT OPINION: IDO1 exhibits complex mechanisms of action and variable expression across different cancer types, presenting both challenges and opportunities. Its intricate mechanisms in tumor development and immune evasion pose significant challenges for translating IDO1 inhibitors into clinical drugs. However, recent advancements in AI-guided drug design, combination therapies, and improved drug delivery methods offer promising insights for enhancing IDO1 inhibitors, although further data is warranted. Despite these challenges, the increasing availability of IDO1 crystal structures and a deeper understanding of its biological roles support ongoing trials that combine IDO1 inhibitors with other therapies. These developments hold potential for improving therapeutic outcomes in cancer treatment. Moreover, the growing interest in applying IDO1 inhibitors to other diseases could stimulate further research and development of new IDO1 inhibitors, potentially benefiting their application in cancer therapy as well.
An updated patent review of small molecule KCNT1 inhibitors (2022-2024).
Peprah PK, Emmitte KA
Expert Opin Ther Pat · 2025 Jul · PMID 40377022 · Publisher ↗
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. Substa...
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.
A patent review of IDH1 inhibitors (2018-present).
Liang Q, Wen F, Wang P … +3 more , Jiang Y, Geng Y, Zha X
Expert Opin Ther Pat · 2025 Jul · PMID 40317206 · Publisher ↗
INTRODUCTION: isocitrate dehydrogenase 1 (IDH1), a key metabolic enzyme in the cytosol, catalyzes the oxidative decarboxylation of isocitrate to produce α-ketoglutarate (α-KG) and NADPH in the TCA cycle. Pan-cancer studi...
INTRODUCTION: isocitrate dehydrogenase 1 (IDH1), a key metabolic enzyme in the cytosol, catalyzes the oxidative decarboxylation of isocitrate to produce α-ketoglutarate (α-KG) and NADPH in the TCA cycle. Pan-cancer studies have demonstrated that IDH1 exhibits a higher mutation frequency and is implicated in a broader range of cancer types, indicating its potential as a promising anti-tumor target. AREAS COVERED: We summarized patents from 2018 to the present that identify novel molecules, compounds, formulations, and methods for inhibiting mIDH1. The literature was retrieved from Web of Science and PubMed. Patent information was obtained via the State Intellectual Property Office's Patent Search and Analysis platform. Clinical data were sourced from the Cortellis Drug Discovery Intelligence database. The date of the most recent search was . EXPERT OPINION: Due to multiple signaling pathway dysregulations and compensatory pathways in solid tumor, monotherapies targeting mutant IDH1 (mIDH1) often fail to achieve desired therapeutic outcomes. Consequently, the combination of mIDH1 inhibitors with other therapeutic agents can enhance the efficacy of antitumor treatments and mitigate the risk of drug resistance. Moreover, the development of novel dual or multiple inhibitors and functional molecules targeting mIDH1 May represent a more promising approach.
A patent review of anti-coronavirus agents targeting the spike-ACE2 interaction (2019-present).
Huang X, Gao H, Zhang J … +2 more , Zhan P, Liu X
Expert Opin Ther Pat · 2025 Jul · PMID 40259874 · Publisher ↗
INTRODUCTION: The Angiotensin-converting enzyme 2 (ACE2) receptor, crucial for coronavirus recognition of host cells, is a key target for therapeutic intervention against SARS-CoV-2 and related coronaviruses. Therefore,...
INTRODUCTION: The Angiotensin-converting enzyme 2 (ACE2) receptor, crucial for coronavirus recognition of host cells, is a key target for therapeutic intervention against SARS-CoV-2 and related coronaviruses. Therefore, thoroughly investigating the interaction mechanism between ACE2 and the Spike protein (S protein), as well as developing targeted inhibitors based on this mechanism, is vital for effectively controlling the spread of SARS-CoV-2 and preventing potential future pandemics caused by other coronaviruses. AREAS COVERED: This article comprehensively reviews the mechanisms underlying ACE2-S protein interaction that facilitate SARS-CoV-2 entry into host cells. It also analyzes the patent landscape regarding inhibitors targeting the ACE2-S interface since 2019. EXPERT OPINION: In the 5 years since the outbreak of SARS-CoV-2, numerous methods and design strategies have been employed to develop innovative therapeutics against coronaviruses. Among these approaches, inhibitors targeting both the ACE2 receptor and the S protein have gained significant interest due to their potential in blocking various coronaviruses. Despite facing challenges similar to other protein-protein interaction inhibitors, progress has been made in developing these inhibitors through virtual screening, covalent protein binding, and peptide modification strategies. However, obstacles persist in clinical translation, necessitating a multidisciplinary strategy that integrates state-of-the-art methodologies to optimize S-ACE2 interface-targeted drug discovery.
Novel inhibitors of STAT3: an updated patent review (2022-present).
Bao K, Li P, Gao D
Expert Opin Ther Pat · 2025 Jul · PMID 40238595 · Publisher ↗
INTRODUCTION: Signal transducer and activator of transcription 3 (STAT3), a member of the STAT protein family, serves as both a signal transducer and a transcription factor. Previous studies have highlighted its pivotal...
INTRODUCTION: Signal transducer and activator of transcription 3 (STAT3), a member of the STAT protein family, serves as both a signal transducer and a transcription factor. Previous studies have highlighted its pivotal roles in regulating cell proliferation, differentiation, apoptosis, as well as immune and inflammatory responses. Consequently, targeting STAT3 has emerged as a promising therapeutic strategy for addressing related diseases. AREAS COVERED: This review offers a comprehensive summary of the progress in discovering STAT3 inhibitors, with a focus on their structural diversity and structure-activity relationships as presented in patent literature from 2022 to the present. EXPERT OPINION: Over the past decades, significant progress has transformed STAT3 into a target of interest for drug development. Despite these advances, no STAT3-targeting drugs have successfully progressed through late-phase clinical trials, largely due to challenges such as limited selectivity and undesirable side effects. These obstacles highlight the inherent complexity of developing safe and effective STAT3 inhibitors. Nevertheless, STAT3 remains a highly promising therapeutic target, and ongoing advancements in this field hold the potential to unlock novel strategies for addressing STAT3-related diseases.
Quorum sensing inhibitors (QSIs): a patent review (2019-2023).
Spaggiari C, Yamukujije C, Pieroni M … +1 more , Annunziato G
Expert Opin Ther Pat · 2025 Jul · PMID 40219759 · Publisher ↗
INTRODUCTION: The collective behavior of bacteria is regulated by Quorum Sensing (QS), in which bacteria release chemical signals and express virulence genes in a cell density-dependent manner. Quorum Sensing inhibitors...
INTRODUCTION: The collective behavior of bacteria is regulated by Quorum Sensing (QS), in which bacteria release chemical signals and express virulence genes in a cell density-dependent manner. Quorum Sensing inhibitors (QSIs) are a large class of natural and synthetic compounds that have the potential to competitively inhibit the Quorum Sensing (QS) systems of several pathogens blocking their virulence mechanisms. They are considered promising compounds to deal with antimicrobial resistance, providing an opportunity to develop new drugs against these targets. AREAS COVERED: The present review represents a comprehensive analysis of patents and patent applications available on Espacenet and Google Patent, from 2019 to 2023 referring to the therapeutic use of Quorum Sensing inhibitors. EXPERT OPINION: Unlike classical antibiotics, which target the basic cellular metabolic processes, QSIs provide a promising alternative to attenuating virulence and pathogenicity without putting selective pressure on bacteria. The general belief is that QSIs pose no or little selective pressure on bacteria since these do not affect their growth. To date, QSIs are seen as the most promising alternative to traditional antibiotics. The next big step in this area of research is its succession to the clinical stage.
Small-molecule RNA ligands: a patent review (2018-2024).
Ravegnini E, Trabocchi A, Lenci E
Expert Opin Ther Pat · 2025 Jul · PMID 40219716 · Publisher ↗
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...
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.
An updated patent review of MALT1 inhibitors (2021-present).
Brvar M, O'Neill TJ, Plettenburg O … +1 more , Krappmann D
Expert Opin Ther Pat · 2025 Jun · PMID 40209204 · Publisher ↗
INTRODUCTION: MALT1 paracaspase acts as a molecular scaffold and a proteolytic enzyme in immune cells. MALT1 has emerged as a promising drug target for cancer therapy, and especially for targeting MALT1 in aggressive lym...
INTRODUCTION: MALT1 paracaspase acts as a molecular scaffold and a proteolytic enzyme in immune cells. MALT1 has emerged as a promising drug target for cancer therapy, and especially for targeting MALT1 in aggressive lymphomas. Drug discovery programs have yielded potent and selective MALT1 protease inhibitors. First-in-class MALT1 inhibitors have been moved to early clinical trials to evaluate safety and efficacy. AREAS COVERED: This review will provide an update regarding the mode of action, the chemical space and therapeutic use of MALT1 inhibitors based on recent patents and the scientific literature (05/2021-12/2024). EXPERT OPINION: Allosteric inhibition is the preferred mode of action to inhibit the MALT1 protease. Chemical advances largely focus on improving binding and inhibition in the allosteric site of MALT1. New composition of matter has been generated, but a clinical proof for the safety and efficacy of allosteric MALT1 inhibitors is still pending. We still lack potent and selective competitive or covalent MALT1 inhibitors, indicating the challenges with targeting the active site. Further, MALT1 protein degraders and MALT1 scaffolding inhibitors have been developed, which may have distinct inhibitory profiles compared to allosteric MALT1 protease inhibitors, but more potent and selective compounds are needed to judge the feasibility and usefulness of these approaches.
A patent review of peptidylarginine deiminase 4 (PAD4) inhibitors (2014-present).
Aiken SG, Grimes T, Munro S … +3 more , Zarganes-Tzitzikas T, La Thangue NB, Brennan PE
Expert Opin Ther Pat · 2025 Jun · PMID 40136037 · Publisher ↗
INTRODUCTION: PAD4 mediates the post-translational modification of arginine residues into citrulline which can have profound effects on protein structure, function and interactions. Protein citrullination and neutrophil...
INTRODUCTION: PAD4 mediates the post-translational modification of arginine residues into citrulline which can have profound effects on protein structure, function and interactions. Protein citrullination and neutrophil extracellular trap (NET) formation associated with increased PAD4 activity have been implicated in the development of autoimmune conditions, cardiovascular diseases, neurodegenerative disorders, and cancer. PAD4 inhibitors have been shown to suppress citrullination and NETs formation. AREAS COVERED: This review covers 10 years of industrial drug discovery campaigns reported in 28 patent applications from 10 companies. Cortellis, the World Intellectual Property Organization website, Scopus and SciFinder were used to search the patent literature using the keywords 'PAD4' and 'PAD4 inhibitor.' Most of the reported inhibitors share the same core scaffold with varied decoration of different complexity, including highly functionalized macrocycles, with some in vivo and pharmacokinetic (PK) data reported for selected examples. EXPERT OPINION: Despite PAD4's clear involvement in multiple disease pathways, its detailed mechanism remains insufficiently understood. Selective and potent compounds with improved PK properties have been provided but most research on PAD4 is still at the experimental stage or preclinical development; the most promising is JBI-1044, at the IND stage, while some companies have turned to antibodies despite considerable previous investment in small molecules.
An updated patent review of antitumor macrocyclic kinase inhibitors (2019 present).
He X, Chen L, Wu S … +3 more , Chen Z, Zhu W, Qiao D
Expert Opin Ther Pat · 2025 Jun · PMID 40129246 · Publisher ↗
INTRODUCTION: Small molecule kinase inhibitors are crucial in the treatment of tumors, and the development of novel inhibitors is a primary approach to combat the continuous emergence of drug resistance. Macrocyclization...
INTRODUCTION: Small molecule kinase inhibitors are crucial in the treatment of tumors, and the development of novel inhibitors is a primary approach to combat the continuous emergence of drug resistance. Macrocyclization has emerged as a cutting-edge strategy to enhance the potency, selectivity, and pharmacokinetic properties of these inhibitors by altering their biological and physicochemical characteristics compared to their acyclic counterparts. AREAS COVERED: The present article provides a comprehensive overview of the recent advancements in macrocyclic small molecule inhibitors and their inhibitory activities against various cancer cells, which have been patented since 2019. EXPERT OPINION: To date, small-molecule kinase inhibitors have demonstrated remarkable therapeutic efficacy in clinical settings. Recent patents have primarily focused on addressing challenges associated with resistance mutations. Despite the significant success achieved in developing selective kinase agents, the identification of new targets and emergence of novel mutations necessitate the development of novel small-molecule inhibitors. Macrocyclic compounds possess distinctive conformational constraints, enhanced inhibitor potency and selectivity, as well as favorable pharmacokinetic properties, rendering them safe, efficient, selective, low-toxicity agents with unique structural characteristic.
A patent review of CXCR7 modulators (2019-present).
Pillaiyar T, Laufer S
Expert Opin Ther Pat · 2025 Jun · PMID 40122070 · Publisher ↗
INTRODUCTION: Atypical chemokine receptor 3 (ACKR3) (formerly CXCR7) regulates various biological processes through its ligands and is closely associated with numerous diseases, including inflammation, cancer, cardiovasc...
INTRODUCTION: Atypical chemokine receptor 3 (ACKR3) (formerly CXCR7) regulates various biological processes through its ligands and is closely associated with numerous diseases, including inflammation, cancer, cardiovascular diseases (CVDs), pain, and neurological disorders. Therefore, ACKR3 has emerged as a potential target for disease treatment. AREAS COVERED: This review summarizes the ACKR3 modulators published in patents from 2019 to 2024 using data from Google Patents, the European Patent Office, and the World Intellectual Property Organization's online databases. This includes information on their chemical structures, syntheses, activities, and developmental stages. EXPERT OPINION: ACKR3 agonists gained traction as a treatment for cardiovascular and pain conditions. WW-12, which was derived from the chemical modifications of conolidine, became a novel small-molecule pain modulator by activating ACKR3, which in turn boosted endogenous opioid peptides for the classical opioid receptors.ACKR3 antagonist ACT-1004-1239 from Idorsia Pharmaceuticals Ltd. has demonstrated the ability to treat cancer, acute lung injury/ARDS, and autoimmune diseases, including multiple sclerosis. The outcomes of these clinical trials will direct the development and indications of future ACKR3 modulators.
An updated patent review of EZH2 inhibitors (2024-present).
Wan G, Li S, Tang Q … +3 more , Qiu H, Zhang Q, Yu L
Expert Opin Ther Pat · 2025 Jun · PMID 40116819 · Publisher ↗
INTRODUCTION: EZH2 forms the PRC2 complex with SUZ12 and EED. As a crucial catalytic subunit of PRC2, EZH2 modifies histone H3K27 via its SET domain, resulting in chromatin condensation and suppressing the transcription...
INTRODUCTION: EZH2 forms the PRC2 complex with SUZ12 and EED. As a crucial catalytic subunit of PRC2, EZH2 modifies histone H3K27 via its SET domain, resulting in chromatin condensation and suppressing the transcription of related target genes. EZH2 not only functions in PRC2-dependent transcriptional repression but can also activate gene expression in PRC2-independent circumstances or regulate the activity of downstream genes via its own activating mutations. On the basis of the critical role of EZH2 in cancer, the development of inhibitors targeting EZH2 provides a new strategy for cancer therapy. AREAS COVERED: The purpose of this review is to summarize the molecular mechanisms of EZH2 inhibitors and emphasize the research progress on EZH2 inhibitors published in the patent literature in recent years. The literature and patent databases of PubMed, Web of Science, SCIFinder, WIPO, USPTO, EPO, and CNIPA were combined to search for more effective EZH2 inhibitors. EXPERT OPINION: Recently, a wide range of structurally diverse EZH2 inhibitors, particularly EZH2 degraders, have been identified. These EZH2 modulators have demonstrated significant potential in treating various diseases, with cancer being a primary focus. The development of small molecules targeting EZH2 with distinct pharmacological effects is poised with numerous opportunities.
RORγt inhibitors in clinical development for the treatment of autoimmune diseases: challenges and opportunities.
Sun N, Wang Y
Expert Opin Ther Pat · 2025 Jun · PMID 40110872 · Publisher ↗
INTRODUCTION: Nuclear receptor retinoid-related orphan receptor gamma-t (RORγt) is a major transcription factor for Th17 cell differentiation and IL-17 production. RORγt has been considered as a promising drug target for...
INTRODUCTION: Nuclear receptor retinoid-related orphan receptor gamma-t (RORγt) is a major transcription factor for Th17 cell differentiation and IL-17 production. RORγt has been considered as a promising drug target for the treatment of IL-17-mediated inflammatory diseases. Numerous small molecule inhibitors have been discovered, and more than 20 of RORγt inhibitors have been advanced to clinical trials. However, none of these compounds has yet achieved market approval. AREAS COVERED: This manuscript summarizes the development of 22 clinical-stage RORγt inhibitors, including their structures, patent applications, and clinical trial status, based on publications and patents available up to November 2024. EXPERT OPINION: The discovery of RORγt inhibitors was considered as an exciting field for the development of small molecular treatments, which has gone through a boom period in the past 10 years. However, some of the leading RORγt inhibitors recently failed in clinical trials due to lack of efficacy or having some safety concerns, although a few small molecule candidates targeting RORγt are still in trials and more in preclinical studies. Realizing the challenge, researchers started to develop different approaches such as dual targeting or exploring new indications, utilizing the potential value of RORγt inhibitors.
Challenges, opportunities, and therapeutic potential of JAK inhibitors and their derived PROTACs (2022 - 2023).
Shah RR
Expert Opin Ther Pat · 2025 Jun · PMID 40056149 · Publisher ↗
INTRODUCTION: Since the approval of the first JAK inhibitor, ruxolitinib, in 2011, the development of JAK inhibitors has expanded significantly, with applications spanning autoimmune diseases, cancer, and inflammatory di...
INTRODUCTION: Since the approval of the first JAK inhibitor, ruxolitinib, in 2011, the development of JAK inhibitors has expanded significantly, with applications spanning autoimmune diseases, cancer, and inflammatory disorders. This review explores the challenges and therapeutic potential of JAK inhibitors and their evolution into proteolysis-targeting chimeras (PROTACs), which offer novel avenues for selective JAK modulation. AREAS COVERED: This review examines recent advancements in JAK inhibitors, including their mechanism of action, structure activity relationships, clinical applications, and emerging safety concerns. Additionally, PROTAC-based strategies targeting JAK proteins are discussed, highlighting their potential advantages over traditional small-molecule inhibitors. A comprehensive patent literature search was conducted, focusing on publications and patents from 2022 to 2023. Key selection criteria included small-molecule JAK inhibitors and JAK-targeting PROTACs with associated preclinical data. EXPERT OPINION: While JAK inhibitors have transformed the treatment of various diseases, safety concerns, including risks of venous thromboembolism and herpes zoster, pose challenges to their widespread use. The advent of JAK-targeting PROTACs represents a promising strategy to enhance selectivity and mitigate off-target effects. However, further research is needed to optimize their therapeutic potential and establish their clinical viability.
A patenting perspective of fat mass and obesity associated protein (FTO) inhibitors: 2017-present.
Dong Z, Huang Y, Xia W … +2 more , Liao Y, Yang CG
Expert Opin Ther Pat · 2025 Jun · PMID 40052926 · Publisher ↗
INTRODUCTION: The fat mass and obesity-associated protein (FTO) catalytically demethylates RNA N-methyl adenosine (mA) modification, dynamically regulates gene expression in eukaryotes. Interestingly, FTO is highly expre...
INTRODUCTION: The fat mass and obesity-associated protein (FTO) catalytically demethylates RNA N-methyl adenosine (mA) modification, dynamically regulates gene expression in eukaryotes. Interestingly, FTO is highly expressed and functions as an oncogenic factor in a wide range of cancers. Therefore, using small-molecule inhibitors to target FTO has been established as a promising therapeutic strategy for combating cancers. AREAS COVERED: Patent literature claiming novel chemical entities as FTO inhibitors disclosed from 2017 to present is available in Espacenet, including dozens of patent documents. EXPERT OPINION: The pivotal influence of FTO demethylase in a particular epigenetic layer of regulation of gene expression renders it promising for FTO to be a therapeutical target for many diseases, including malignant cancers. Several institutions were prompted and have patented chemical frameworks as FTO inhibitors. Remarkedly, the FTO inhibitor CS1 (Bisantrene) has advanced to clinical trials for treating acute myeloid leukemia (AML). The successful advancement of CS1 into clinical trials would continuingly stimulate researches on RNA epigenetic enzymes targeted first-in-class anticancer drug discovery.
A patent review of hepatitis B virus core protein allosteric modulators (2019-present).
Wang S, Ma F, Tang K … +4 more , Xu S, Jia H, Liu X, Zhan P
Expert Opin Ther Pat · 2025 May · PMID 39985414 · Publisher ↗
INTRODUCTION: The hepatitis B virus (HBV) core protein is a significant therapeutic target due to its essential role in HBV replication. Over the past five years, numerous structurally unique CpAMs have been patented. Ho...
INTRODUCTION: The hepatitis B virus (HBV) core protein is a significant therapeutic target due to its essential role in HBV replication. Over the past five years, numerous structurally unique CpAMs have been patented. However, no compounds have been approved due to various issues such as poor pharmacokinetics (PK) and hepatotoxicity. As a result, there is an urgent need to develop novel CpAMs without these limitations. AREAS COVERED: This review provides a comprehensive analysis of patents related to CpAMs from 2019 to the present, with the aim of delineating the chemical evolution that has occurred in the pursuit of more promising CpAMs. The sources of patent information included databases of the European Patent Office, the China Patent Office and the U.S.A. Patent Office, while relevant research articles were accessed through PubMed. EXPERT OPINION: During the optimization of CpAMs, striking a good balance between activity and druggability usually poses a certain challenge while the emergence of drug resistance issues further complicates the development process. A comprehensive analysis of the structural features of CpAMs and identification of essential patterns in chemical evolution can reveal common principles that improve pharmacodynamic (PD) and PK profiles, thereby facilitating the discovery of next-generation CpAMs.
A patent review of CYP3A4 inhibitors (2018 - present).
Tu DZ, Hu XY, Lei JX … +4 more , Liu SY, Xiao ZP, Yang L, Ge GB
Expert Opin Ther Pat · 2025 May · PMID 39976548 · Publisher ↗
INTRODUCTION: Cytochrome P450 3A4 (CYP3A4), one of the most important xenobiotic-metabolizing enzymes, plays a central role in drug metabolism and acts as a key mediator in drug-drug interactions. CYP3A4 inhibitors can p...
INTRODUCTION: Cytochrome P450 3A4 (CYP3A4), one of the most important xenobiotic-metabolizing enzymes, plays a central role in drug metabolism and acts as a key mediator in drug-drug interactions. CYP3A4 inhibitors can potentiate the therapeutic effects of CYP3A4-substrate drugs via enhancing their systematic exposure levels. Two CYP3A4 inhibitors (ritonavir and cobicistat) have already been approved for modulating the exposure levels of CYP3A4-substrate drugs. AREAS COVERED: This review summarizes the newly patented CYP3A4 inhibitors in the period (2018-2024) by using the keywords 'CYP3A4' and 'inhibitor' in Espacenet database from academic institutions and industrial companies. The chemical structures and inhibition profiles of the patented CYP3A4 inhibitors, including the anti-CYP3A4 potency, inhibitory mechanisms, and other relevant information, are summarized and discussed. EXPERT OPINION: Although diverse CYP3A4 inhibitors have been developed in the past few years, the development of more efficacious CYP3A4 inhibitors with favorable pharmacokinetic and safety profiles is still challenging. To maximize the benefit of CYP3A4 inhibitors, combination strategies should be used for the development of highly specific CYP3A4 inhibitors or degraders with efficacious anti-CYP3A4 effects and favorable pharmacokinetic profiles. Meanwhile, more efforts should be made to address the organ-targeting or tumor-targeting ability of CYP3A4 inhibitors for specific purposes.
JBI-802: the first orally available LSD1/HDAC6 dual inhibitor to enter clinical trials.
Zhang J, Ren X, Song Y … +1 more , Yu B
Expert Opin Ther Pat · 2025 May · PMID 39960216 · Publisher ↗
INTRODUCTION: Lysine-specific demethylase 1 (LSD1) and histone deacetylase 6 (HDAC6) are key epigenetic regulators involved in histone demethylation and deacetylation processes that impact chromatin structure and gene ex...
INTRODUCTION: Lysine-specific demethylase 1 (LSD1) and histone deacetylase 6 (HDAC6) are key epigenetic regulators involved in histone demethylation and deacetylation processes that impact chromatin structure and gene expression. JBI-802 marks a major advancement as the first novel, orally available LSD1/HDAC6 dual inhibitor currently in clinical trials. AREAS COVERED: This review provides a comprehensive overview of the discovery and development of JBI-802, detailing its structure-activity relationship (SARs), chemical synthesis, biological activity, and clinical progress. Other dual LSD1/HDAC6 inhibitors and the challenges are briefly discussed, underscoring the therapeutic potential of dual inhibition in disease treatment. The literature search is performed using SciFinder, Google patent, ClinicalTrials databases, and PubMed. EXPERT OPINION: The dual LSD1/HDAC6 inhibitor JBI-802 demonstrates robust anti-proliferative activity, significant antitumor effects in multiple hematologic malignancies, and superior efficacy in combination with checkpoint inhibitors in the CT-26 syngeneic mouse model. JBI-802 is currently undergoing phase I/II clinical trials in patients with advanced solid tumors, myeloproliferative neoplasms (MPN), and myelodysplastic/myeloproliferative neoplasms (MDS/MPN) with thrombocytosis. However, the potential on-target toxicity, off-target interactions and selectivity concerns deservee more attention.
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