Expert Opinion On Therapeutic Patents[JOURNAL]
Sun
200 papers
AKR1C3 inhibitors and exploiters for the treatment and therapeutic monitoring of cancer: a patent review 2020-present.
Case AM, Smith MM, Mack CA … +1 more , Trippier PC
Expert Opin Ther Pat · 2026 Jul · PMID 42396977 · Publisher ↗
INTRODUCTION: Aldo-keto reductase 1C3 (AKR1C3) is a drug target for the treatment of various androgen dependent malignancies, including castration-resistant prostate canceras well as hematological cancers. The enzyme pla...
INTRODUCTION: Aldo-keto reductase 1C3 (AKR1C3) is a drug target for the treatment of various androgen dependent malignancies, including castration-resistant prostate canceras well as hematological cancers. The enzyme plays a key role in the conversion of androgen precursors into potent androgen receptor ligands and the conversion of prostaglandins from pro-differential to pro-proliferative, facilitating progression of these malignancies. Additionally, AKR1C3 plays a role in chemotherapy resistance, reducing therapeutics to inactive forms and stabilizing expression of mutant androgen receptors. AREA COVERED: This article reviews patents, obtained from WIPO and SciFinder, published since 2020 covering AKR1C3 inhibitors, compounds that exploitAKR1C3 for prodrug activation, and the use of AKR1C3 expression levels as a biomarker for measuring disease and therapeutic response. As well as inhibitors, this article reviews the first reported AKR1C3/AR-v7 dual degrader. EXPERT OPINION: Multiple compounds have been reported to potently and selectively inhibit AKR1C3 eliciting tumor growth inhibition as stand-alone agents and when used in combination with clinically approved chemotherapeutics. With drug resistance an ever-present issue, exploration of alternative routes for treating malignancies via AKR1C3 targeting offers tremendous potential. Translation to clinical trials and their effect in patients is expected to be revealed in the coming years.
An updated patent review of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitors (2020-present).
Abdallah M, Keddis PM, Keddis TM … +5 more , El-Gamil DS, Abadi AH, Kii I, Engel M, Abdel-Halim M
Expert Opin Ther Pat · 2026 Jul · PMID 42334856 · Publisher ↗
INTRODUCTION: Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a conserved CMGC serine/threonine kinase with an autophosphorylation-dependent activation mechanism. As a dosage-sensitive regulator...
INTRODUCTION: Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a conserved CMGC serine/threonine kinase with an autophosphorylation-dependent activation mechanism. As a dosage-sensitive regulator of transcription, RNA splicing, cell-cycle progression, and signaling, DYRK1A is implicated in neurological, oncological, cardiovascular, metabolic, immune, and infectious diseases. These roles have driven drug discovery, from early probes to advanced clinical-stage inhibitors. AREAS COVERED: This review covers patent literature related to the discovery of DYRK1A inhibitors and degraders published from January 2020 to the review cutoff date. The literature search was conducted in WIPO, Reaxys, SciFinder, Lens.org, Espacenet, USPTO, and Google Patents. EXPERT OPINION: Recent patents indicate that DYRK1A inhibition is no longer a single pharmacological concept but an indication-driven strategy shaped by tissue access, delivery, and mechanistic pharmacodynamic biomarkers. The most credible programs prioritize functional pathway modulation and meaningful target engagement at therapeutically achievable exposure rather than maximal biochemical potency alone, with selectivity defined by disease biology rather than as an absolute requirement. Delivery-advantaged indications such as osteoarthritis and peripheral inflammatory disorders may provide the earliest clinical validation, whereas CNS programs will require brain-penetrant compounds with controlled, likely partial, target modulation. Degraders and macrocycles broaden the toolbox, but biomarker-guided translation remains the key determinant of success.
Takeda G-protein-coupled receptor 5 and farnesoid X receptor agonists for diabetes treatment: a patent review and clinical advancements (2015-present).
Sharma S, Kumar V, Kumar S … +1 more , Wadhwa P
Expert Opin Ther Pat · 2026 Jul · PMID 42331759 · Publisher ↗
INTRODUCTION: Takeda G-protein-coupled receptor 5 (TGR5) and farnesoid X receptor (FXR) are bile acid-activated receptors involved in glucose, lipid, and energy homeostasis, making them promising therapeutic targets for...
INTRODUCTION: Takeda G-protein-coupled receptor 5 (TGR5) and farnesoid X receptor (FXR) are bile acid-activated receptors involved in glucose, lipid, and energy homeostasis, making them promising therapeutic targets for type 2 diabetes mellitus (T2DM) and metabolic liver diseases. AREAS COVERED: This review critically analyzes patents published between 2015 and 2025 retrieved from WIPO Patentscope, Espacenet, USPTO, and Google Patents using keyword- and IPC-based strategies. Major patented chemotypes include modified bile acids, benzoic acid-cholane hybrids, heteroaryl scaffolds, and sulfonylurea/sulfonamide derivatives. Several compounds demonstrated sub micromolar (µM) to nanomolar (nM) TGR5/FXR agonistic activity, while gut-restricted agonists showed enhanced GLP-1 secretion with reduced systemic adverse effects such as gallbladder filling and pruritus. Comparative patent analysis revealed a progressive transition from classical steroidal scaffolds toward tissue-selective and gut-restricted modulators designed to improve receptor selectivity, pharmacokinetics, and translational safety. EXPERT OPINION: Despite strong preclinical promise, the clinical translation of TGR5 and FXR agonists remains limited by mechanism-driven toxicities and inadequate long-term tolerability. Future progress will likely depend on tissue-selective, pathway-biased, and gut-restricted modulation rather than further increases in receptor potency.
A patent review of GPR84 receptor antagonists (2020-present).
Mi T, Yin J, Chen L … +1 more , Nan F
Expert Opin Ther Pat · 2026 Jun · PMID 42331362 · Publisher ↗
INTRODUCTION: GPR84 is a pro‑inflammatory, metabolite‑sensing Class A GPCR implicated in a range of inflammatory, fibrotic, metabolic, and neuropathic processes. Its inducible expression and role in amplifying innate imm...
INTRODUCTION: GPR84 is a pro‑inflammatory, metabolite‑sensing Class A GPCR implicated in a range of inflammatory, fibrotic, metabolic, and neuropathic processes. Its inducible expression and role in amplifying innate immune responses have driven sustained interest in GPR84 antagonists as potential therapeutic agents. AREAS COVERED: This review summarizes recent advances in GPR84 antagonist discovery, focusing on patent applications and research articles retrieved from SciFinder covering 2020 to January 2026. EXPERT OPINION: Recent work and patent filings reflect continued diversification of GPR84 antagonist chemotypes, but the translational outlook remains constrained by biological uncertainty and limited clinical validation. With only a small number of candidatest-such as BAY‑3178275 and BGT‑004-currently in active development, further progress will require deeper mechanistic understanding and clearer definition of disease contexts in which GPR84 modulation may offer therapeutic benefit.
SLIT2 and ROBO-Axis inhibitors for the treatment of cancer: a patent review (2020-2026).
Al-Ruweidi MK, Gabr MT
Expert Opin Ther Pat · 2026 Jun · PMID 42311159 · Publisher ↗
INTRODUCTION: The SLIT2-ROBO signaling axis plays a context-dependent role in cancer, functioning as either a tumor suppressor or oncogenic driver. This bidirectionality creates both therapeutic opportunity and significa...
INTRODUCTION: The SLIT2-ROBO signaling axis plays a context-dependent role in cancer, functioning as either a tumor suppressor or oncogenic driver. This bidirectionality creates both therapeutic opportunity and significant challenges for drug development and patent strategy. AREAS COVERED: This review analyzes patents targeting SLIT2-ROBO axis inhibition in cancer from 2020-2026. Patent families were retrieved from Google Patents, Espacenet, and WIPO PATENTSCOPE, consolidated by INPADOC family, and evaluated for mechanistic relevance and experimental enablement. Therapeutic modalities include antagonistic antibodies, ligand traps, small molecule and macrocyclic PPI disruptors, nucleic-acid approaches, and bispecific constructs. Each family was assessed using an enablement framework and a directionality-risk checklist, with emphasis on biomarker gating and translational feasibility. EXPERT OPINION: The current patent landscape is limited by lack of biomarker-driven stratification and incomplete enablement. Future progress will depend on integrating robust assay-to-asset pipelines with biomarker-guided deployment strategies to ensure both clinical efficacy and durable intellectual property.
New insights on anticancer glucocorticoid receptor modulators: a patent review (2020-present).
Franzin M, Lucafò M, Curci D … +2 more , Decorti G, Stocco G
Expert Opin Ther Pat · 2026 Jul · PMID 42289083 · Publisher ↗
INTRODUCTION: Selective glucocorticoid receptor modulators (SGRM) have emerged as promising agents to counteract glucocorticoid‑driven chemoresistance, immune suppression, and poor prognosis in solid tumors by modulating...
INTRODUCTION: Selective glucocorticoid receptor modulators (SGRM) have emerged as promising agents to counteract glucocorticoid‑driven chemoresistance, immune suppression, and poor prognosis in solid tumors by modulating glucocorticoid receptor (GR) signaling without losing anticancer immune activity. AREAS COVERED: This review provides a focused update to a previous patent review on SGRM (2014-2020) by summarizing Espacenet-indexed patent applications published between 2020 and 30 April 2026 (PCT/US2020/055498, PCT/US2021/017259, PCT/US2022/042475) describing anticancer strategies. EXPERT OPINION: Collectively, these patents support SGRM in addition to cytotoxic and immunotherapeutic regimens in solid tumors. Preclinical and early‑phase clinical evidence (phase I/II) describes how GR antagonism, continuously or intermittently, lowers elevated neutrophil-to-lymphocyte ratio (NLR), modulates GR‑target transcriptional signatures, and enhances responses to nab‑paclitaxel and anti‑PD‑1 antibodies. Key limitations of these patents consist of evidence based on still limited clinical sample sizes, requiring confirmation in phase III trials, and on benefit enriched in biologically defined subpopulations. From a clinical perspective, these agents could be realistically integrated into anticancer protocols, as they work synergistically with other chemotherapeutics.
An updated review of discoidin domain receptor 1 (DDR1) modulators (2020-present).
Zhang Y, Wang Z, Ding K
Expert Opin Ther Pat · 2026 Jul · PMID 42240164 · Publisher ↗
INTRODUCTION: As a unique collagen-activated receptor tyrosine kinase, discoidin domain receptor 1 (DDR1) mediates signaling essential for cell proliferation, survival, adhesion, and matrix remodeling. Conversely, its dy...
INTRODUCTION: As a unique collagen-activated receptor tyrosine kinase, discoidin domain receptor 1 (DDR1) mediates signaling essential for cell proliferation, survival, adhesion, and matrix remodeling. Conversely, its dysregulation is implicated in cancer, tissue fibrosis, atherosclerosis, and other inflammatory diseases. Emerging research reveals that the non-catalytic functions of DDR1 are critically involved in tumor progression, metastasis, and immune exclusion. Selectively inhibiting the catalytic and/or non-catalytic functions of DDR1 presents a promising therapeutic strategy for various diseases. AREAS COVERED: This article summarizes current progress on the development of inhibitors, degraders and biomolecules targeting DDR1 and their potential therapeutic application during the period from 2020 to 2025. EXPERT OPINION: Significant efforts have been made to develop small-molecule DDR1 kinase inhibitors, yet achieving high selectivity remains a challenge. Degraders have been developed to inhibit both its catalytic and noncatalytic functions. Although these molecules offer conceptual advantages over traditional kinase inhibitors, they suffer from suboptimal pharmacokinetic properties. Alternatively, biologics such as antibodies and peptides can block the DDR1-collagen interaction, specifically inhibiting non-catalytic signaling, and one antibody is currently under clinical evaluation. Moving forward, the development of highly selective inhibitors and improvement of pharmacokinetic profiles for degraders will be pivotal for translating DDR1 targeting into viable therapies.
Recent advances in the discovery of PKMYT1-targeting drugs: a patent review (2021-2025).
Wang Y, Wang C, Ren F … +2 more , Zhavoronkov A, Ding X
Expert Opin Ther Pat · 2026 Jun · PMID 42165607 · Publisher ↗
INTRODUCTION: PKMYT1, a member of the WEE family of kinases that regulates mitotic entry by phosphorylating CDK1 at Thr14, has recently gained prominence as a promising synthetic lethal target for oncology. Since the fir...
INTRODUCTION: PKMYT1, a member of the WEE family of kinases that regulates mitotic entry by phosphorylating CDK1 at Thr14, has recently gained prominence as a promising synthetic lethal target for oncology. Since the first-in-class PKMYT1 inhibitor entered clinical trials in 2021, the field has experienced explosive growth, marked by a surge in patents for both inhibitors and degraders and the advancement of five candidates into clinical development. AREAS COVERED: This review covers an update of clinical trial reports and patent literature on PKMYT1 inhibitors from 2021 to December 2025, drawing on patent retrieved from the World Intellectual Property Organization (WIPO), the European Patent Office, and the Cortellis Drug Discovery Intelligence database. EXPERT OPINION: The rapid advancement of PKMYT1 inhibitors and degraders underscores their potential as a synthetic‑lethal therapeutic strategy for cancers with CCNE1 amplification or FBXW7 alterations. Clinical proof‑of‑concept for this approach has been established by RP‑6306 trial outcomes, while insights from this comprehensive review are expected to inform strategies addressing the current limitations in this field.
An update on PDGFR inhibitors: a patent review (2020 - present).
Nandi S, Ahmed S, Barma S … +2 more , Dey R, Samadder A
Expert Opin Ther Pat · 2026 Jul · PMID 42160193 · Publisher ↗
INTRODUCTION: Platelet-derived growth factor receptors (PDGFRs) play essential roles in cell growth, angiogenesis, and tissue repair, while their dysregulation is implicated in cancer and fibrotic disorders. PDGFR inhibi...
INTRODUCTION: Platelet-derived growth factor receptors (PDGFRs) play essential roles in cell growth, angiogenesis, and tissue repair, while their dysregulation is implicated in cancer and fibrotic disorders. PDGFR inhibitors have become important in precision medicine by enabling targeted therapy, slowing disease progression, and overcoming drug resistance which warrants search of new inhibitors. AREAS COVERED: A patent survey (2020-2025) focused on small-molecule PDGFR inhibitors has been carried out. Key aspects discussed include PDGFR inhibitory activity, antiproliferative effects, structural features critical for activity, and clinical relevance. EXPERT OPINION: The PDGFR inhibitors, as summarized in discussed patents, reveal that among the nitrogen containing heterocycles, the most active belonged to pyrazolopyrimidines, pyrazolothiazole carboxamides, and pyrrolo[1,2-b] pyridazines classes where hydrophobicity plays an important role in their activity. Although some of the compounds were specific to either the α or β receptor, many reported compounds lacked selectivity to other kinases as well. The smaller number of patents could also indicates a larger scope to address these issues and simultaneously identify novel PDGFR inhibitors.
An updated patent review of histone deacetylase 6 inhibitors in neurodegenerative diseases (2020-2025).
Shen S
Expert Opin Ther Pat · 2026 Jul · PMID 42142330 · Publisher ↗
INTRODUCTION: Histone deacetylase 6 (HDAC6) inhibitors have been widely explored as potential therapeutic approaches for oncological, autoimmune, cardiovascular, and neurodegenerative disorders. Recent clinical advanceme...
INTRODUCTION: Histone deacetylase 6 (HDAC6) inhibitors have been widely explored as potential therapeutic approaches for oncological, autoimmune, cardiovascular, and neurodegenerative disorders. Recent clinical advancements in non-hydroxamate-based HDAC6 inhibitors highlight favorable drug-like properties and improved safety margins, enhancing suitability for long-term treatment. AREA COVERED: This review updates the clinical status of HDAC6 inhibitors, the evolution of HDAC6 inhibitor pharmacophores, and patent disclosures from 2020 to 2025 identified by SciFinder search and manual confirmation. It also describes pharmacological assessment of new selective HDAC6 inhibitors in and models of neurodegenerative diseases. EXPERT OPINION: Expanding interest in the development of 2-(difluoromethyl)-1,3,4-oxadiazole (1,3,4-DFMO) derivatives has yielded a diverse set of HDAC6 inhibitors with superior HDAC6 potency and selectivity and enhanced oral pharmacokinetic profiles. These characteristics have facilitated the identification of optimized drug candidates for treating both peripheral and central nervous neurodegenerative diseases. Among the emerging therapeutic applications, Charcot-Marie-Tooth (CMT) disease has become the leading focus in preclinical and early clinical development using HDAC6 inhibitors.
Small molecule agonists of Toll-like receptors 7 and 8: an updated patent review 2021 - 2025.
Patel AM, Chernyak N, Seganish WM
Expert Opin Ther Pat · 2026 Jun · PMID 42132243 · Publisher ↗
INTRODUCTION: Toll-like receptors 7 (TLR7) and 8 (TLR8) are endosomal receptors that sense single‑stranded RNA and activate MyD88‑dependent inflammatory signaling, linking innate immune detection to adaptive immune respo...
INTRODUCTION: Toll-like receptors 7 (TLR7) and 8 (TLR8) are endosomal receptors that sense single‑stranded RNA and activate MyD88‑dependent inflammatory signaling, linking innate immune detection to adaptive immune responses. Translational and clinical studies across therapeutic areas have underscored both the therapeutic potential and safety challenges of modulating TLR7/8 activity, driving growing interest in small‑molecule agonists and delivery strategies that enable precise control of receptor engagement. AREAS COVERED: This review highlights recent patent activity on small-molecule TLR7/8 agonists, as well as derived conjugates and alternative modalities. This review covers patents published between January 2021 and August 2025 found using Scifinder-n and Cortellis database searches. We report relevant chemical scaffolds, key trends in structure-activity relationships, innovative conjugation strategies, and, where disclosed, insights from preclinical animal models and clinical data. EXPERT OPINION: Recent patent activity reflects a marked expansion in small‑molecule TLR7/8 agonist development, with increasing emphasis on delivery‑gated strategies. Although systemic agonists and early antibody conjugates have shown preclinical efficacy and tolerability, limited clinical translatability suggests that future progress will depend on integrating agonist design with optimized delivery, linker chemistry, antigen selection, and translational assessment to better balance efficacy and tolerability.
A patent review of LPAR1 antagonists (2010 - present).
Zhao J, Li Y, Zheng W … +7 more , Liu Y, Yang Y, Leng Y, Wei S, Lou J, Shang X, Tang D
Expert Opin Ther Pat · 2026 Jun · PMID 42132000 · Publisher ↗
INTRODUCTION: Lysophosphatidic acid receptor 1 (LPAR1), a G protein-coupled receptor, mediates diverse biological effect. Substantial evidence from human patients and experimental models demonstrates that pathological hy...
INTRODUCTION: Lysophosphatidic acid receptor 1 (LPAR1), a G protein-coupled receptor, mediates diverse biological effect. Substantial evidence from human patients and experimental models demonstrates that pathological hyperactivation of LPAR1 in fibroblasts and myofibroblasts contributes to disease progression, establishing it as a key pathological driver in idiopathic pulmonary fibrosis (IPF). AREAS COVERED: This review systematically analyzes peer-reviewed literature retrieved from Web of Science and PubMed, alongside publicly disclosed patents obtained via the IncoPat Patent Search and Analysis platform, covering the period from 2010 to the present. Clinical data were sourced from the Cortellis Drug Discovery Intelligence database. EXPERT OPINION: Small-molecule LPAR1 antagonists show promise as novel therapeutics for IPF, as evidenced by their attenuation of disease progression in two phase II clinical trials. Despite these advancements, LPAR1 antagonist development faces several medicinal chemistry challenges, including the absence of rational structure-based drug design and difficulties in optimizing ADMET properties. Future development avenues include exploring combination therapies, expanding indications, developing long-acting formulations, and investigating novel modalities such as LPAR1-targeting proteolysis-targeting chimeras (PROTACs) and small-interfering RNA (siRNA) therapeutics directed against LPAR1.
PCSK9 inhibitors: an updated patent review 2024-2025.
Fassi EMA, Albani M, D'Adduzio L … +3 more , Milano EG, Lammi C, Grazioso G
Expert Opin Ther Pat · 2026 Jun · PMID 42131889 · Publisher ↗
INTRODUCTION: Proprotein convertase subtilisin/kexin 9 (PCSK9) modulates the circulating levels of low-density lipoprotein cholesterol (LDL-C). Consequently, PCSK9 inhibition, at any level, from the mRNA transcription to...
INTRODUCTION: Proprotein convertase subtilisin/kexin 9 (PCSK9) modulates the circulating levels of low-density lipoprotein cholesterol (LDL-C). Consequently, PCSK9 inhibition, at any level, from the mRNA transcription to the final interaction with LDL-R, through suitable ligands, has been established as a corroborated therapeutic strategy for fighting hypercholesterolemia, preventing the risks of cardiovascular diseases. AREA COVERED: Patent literature published between 2024 and 2025 in the Espacenet database, an international repository containing more than 150 million documents from over 100 patent‑granting authorities, focusing on disclosures claiming novel compounds designed to bind and inhibit the PCSK9 protein. EXPERT OPINION: The clinical development of small-molecule PCSK9 inhibitors, such as MK-0616 (enlicitide) and AZD0780 (laroprovstat), demonstrates that PCSK9 is still a drug target of great interest for both academic and pharmaceutical companies. Numerous patents deposited in the last two years cover compounds that are structurally related to previously deposited general structures as well as newly developed scaffolds that include quinolines and isoquinolines, peptides, pyridine, and benzothiazole derivatives. However, with mAbs and siRNAs dominating the market, small molecules are required to prove superior cost-efficiency, combination value, and cardiovascular advantages that extend beyond LDL-C reduction.
Activin receptor-like kinase 5 (ALK5) inhibitors: a patent review (2013-present).
Huang XY, Yu CQ, Wang X … +2 more , Guo Z, Jin CH
Expert Opin Ther Pat · 2026 May · PMID 41984152 · Publisher ↗
INTRODUCTION: Activin receptor-like kinase 5 (ALK5) is a pivotal component of the transforming growth factor β (TGF-β) signaling pathway. Currently, 10 ALK5 inhibitors are under clinical investigation, with numerous othe...
INTRODUCTION: Activin receptor-like kinase 5 (ALK5) is a pivotal component of the transforming growth factor β (TGF-β) signaling pathway. Currently, 10 ALK5 inhibitors are under clinical investigation, with numerous others in preclinical stages, demonstrating broad therapeutic potential. However, no systematic review of ALK5 inhibitor-related patents has been conducted to date. Therefore, this study systematically reviews patents related to ALK5 inhibitors from 2013 to the present, providing a theoretical basis for discovering structurally novel, safe, and effective ALK5 inhibitors. AREAS COVERED: This paper briefly outlines ALK5 inhibitors currently in clinical development and ALK5-related patents published since 2013, retrieved through databases such as Google Patents, CAS SciFinder and PatSnap. EXPERT OPINION: ALK5 inhibitors have garnered significant interest in recent years for the treatment of TGF-β-related diseases, with encouraging outcomes observed in clinical trials. However, certain structural classes have been associated with adverse effects such as cardiotoxicity and bone toxicity. This review consolidates patent literature on ALK5 inhibitors, offering insights to support the development of novel, highly efficient, and low-toxicity inhibitors with improved pharmacokinetic profiles.
A patent review of VEGFR-2 inhibitors: an update (2022 - present).
Farghaly TA, Harras MF, Alsaedi AMR … +5 more , Al-Hussain SA, Al-Qurashi NT, Riyadh SM, Zaki MEA, Hussein SM
Expert Opin Ther Pat · 2026 May · PMID 41983527 · Publisher ↗
INTRODUCTION: A complicated process called angiogenesis creates new blood vessels from existing ones. Oxygen and nutrients from angiogenesis support tumor development, invasion, and metastasis. Many biological agents cau...
INTRODUCTION: A complicated process called angiogenesis creates new blood vessels from existing ones. Oxygen and nutrients from angiogenesis support tumor development, invasion, and metastasis. Many biological agents cause angiogenesis. EGF, FGF, VEGF, transcription factors, cytokines, adhesion molecules, proteinases, and growth factors. VEGF-A, B, C, and D are necessary for angiogenesis. VEGF family members interact with VEGFR-1,-2, and-3. Overexpression of VEGF proteins and receptors occurs during cancer progression. Novel signaling pathways, transcription factors, and mechanisms may help cure cancers by inhibiting angiogenesis. AREAS COVERED: This review discusses VEGFR-2 inhibitors patented since 2022 and their potential use in the management of angiogenesis-related disorders like cancer. EXPERT OPINION: Small-molecule VEGFR-2 inhibitors have minimal selectivity and cause fatigue, anorexia, hypertension, hemorrhage, and bleeding due to their affinity for PDGF, EGFR, and RAF, which is conserved in many tyrosine kinases. Poor pharmacokinetics, side effects, and high manufacturing costs may limit biomolecule adoption despite clinical success. Proangiogenic and non-tumor proangiogenic chemicals and myeloid cells produced treatment resistance. Thus, multimodal targeted medications or combination therapy with anti-angiogenic therapies, chemotherapeutic agents, immune checkpoint inhibitors, or gene therapy are needed to block pathological angiogenesis and increase selectivity, safety, diagnosis, and therapy response.
A patent review of NLRP3 inhibitors for inflammatory diseases (2023-present).
Namme JN, Xu Y, McClendon E … +2 more , Zhang C, Zhang S
Expert Opin Ther Pat · 2026 May · PMID 41933486 · Publisher ↗
INTRODUCTION: With increasing knowledge and understanding of the molecular mechanisms of the NOD-like receptor family pyrin domain-containing 3 (NLRP3) inflammasome and its role in inflammatory diseases, NLRP3 has emerge...
INTRODUCTION: With increasing knowledge and understanding of the molecular mechanisms of the NOD-like receptor family pyrin domain-containing 3 (NLRP3) inflammasome and its role in inflammatory diseases, NLRP3 has emerged as a highly druggable target. This is reflected in extensive efforts to develop small molecule NLRP3 inhibitors with diverse chemical scaffolds and mechanisms of action (MOAs), aimed to achieve disease intervention. AREAS COVERED: The current review summarizes recent patents on NLRP3 inhibitor development from 2023 to present. In addition, the molecular mechanisms underlying NLRP3 activation and its involvement in inflammatory diseases were also discussed. The second objective is to get a comprehensive analysis of currently available patent applications and priority filings on NLRP3-targeted therapies with emphasis on new indications. EXPERT OPINION: This review provides an organized, systematic, and coherent overview of recent progress in NLRP3-targeted therapeutics and highlights the increasing diversity of chemical classes of new NLRP3 inhibitors, as well as the overall trend toward increased strategic activity across patent jurisdictions and territories.
Patent landscape and therapeutic evolution of mazdutide: a dual GLP-1/Glucagon receptor agonist for obesity and type 2 diabetes.
Abdul Fasi M
Expert Opin Ther Pat · 2026 May · PMID 41820018 · Publisher ↗
INTRODUCTION: Mazdutide is a dual glucagon-like peptide-1 receptor (GLP-1 R) and glucagon receptor (GCGR) agonist representing a new generation of incretin-based therapeutics for obesity and type 2 diabetes. While its cl...
INTRODUCTION: Mazdutide is a dual glucagon-like peptide-1 receptor (GLP-1 R) and glucagon receptor (GCGR) agonist representing a new generation of incretin-based therapeutics for obesity and type 2 diabetes. While its clinical efficacy is increasingly recognized, the intellectual property framework that underpins its development and long-term positioning has not been systematically examined. AREAS COVERED: This review presents a comprehensive patent landscape analysis of mazdutide and related oxyntomodulin analogs. Patent documents were identified using the Patentscope database, covering filings between 2015 and 2025. Twelve patent families were analyzed, encompassing composition-of-matter, process chemistry, formulation technologies, dosing regimens, and therapeutic applications. The analysis traces the evolution of innovation from early peptide design by Eli Lilly to later formulation, clinical, and indication-expansion strategies led by Innovent Biologics, including obesity, type 2 diabetes, hyperuricemia, and adolescent obesity. EXPERT OPINION: Mazdutide illustrates how layered patent strategies integrating molecular design, manufacturability, formulation stability, and clinical use claims can secure durable exclusivity. This approach provides a strategic model for future dual and multi-receptor peptide therapeutics.
An updated patent review of isoflavones and isocoumarins (2018-2024).
Hussain H
Expert Opin Ther Pat · 2026 Apr · PMID 41784354 · Publisher ↗
INTRODUCTION: It is well established that isocoumarins and isoflavones exhibit intriguing biological effects. During the period 2018-2024 isocoumarins and isoflavones chemistry has attracted attention due to their biolog...
INTRODUCTION: It is well established that isocoumarins and isoflavones exhibit intriguing biological effects. During the period 2018-2024 isocoumarins and isoflavones chemistry has attracted attention due to their biological and pharmaceutical properties. AREAS COVERED: This review focuses on patents relating to the therapeutic properties of isocoumarins and isoflavones between 2018 and 2024. The latest patented studies of isocoumarin and isoflavone are summarized by using the keywords 'isocoumarin' and 'isoflavone' in SciFinder, PubMed, and Google Patents databases in the year from 2018 to 2024. EXPERT OPINION: A wide range of important pharmaceutical properties are exhibited by isocoumarins and isoflavones and their synthetic analogs. In addition, isocoumarins and isoflavones have the potential to couple with other biologically active molecules, synergistically enhancing delivery and biological effects. In addition, scientists should direct their efforts toward the synthesis of halo-substituted and functionalized heterocyclic ring derivatives of isocoumarins and isoflavones, with a view to obtaining lead compounds. The lack of pharmacology and pharmacokinetics data along with in vivo studies for isocoumarins and isoflavones, prevents effective regulatory decisions from being proposed. In addition, detailed efficacy studies in well-established disease models are required to determine the clinical effects of isocoumarins and isoflavones.
5'-Ectonucleotidase (CD73) inhibitors: a patent review (2021-present).
Wang Z, Junker A
Expert Opin Ther Pat · 2026 Apr · PMID 41748480 · Publisher ↗
INTRODUCTION: Adenosine-mediated immunosuppression is a major mechanism of tumor immune escape and is largely driven by ecto-5'-nucleotidase (CD73), which catalyzes the formation of extracellular adenosine and limits the...
INTRODUCTION: Adenosine-mediated immunosuppression is a major mechanism of tumor immune escape and is largely driven by ecto-5'-nucleotidase (CD73), which catalyzes the formation of extracellular adenosine and limits the efficacy of cancer immunotherapies. Consequently, CD73 has emerged as a key immune checkpoint and an attractive target for therapeutic and diagnostic intervention. AREAS COVERED: This review summarizes patent literature on CD73 inhibitors published from 2021 to the present. The analysis covers advances in nucleotide-derived inhibitors, including structure-guided optimization and strategies enabling peroral bioavailability, as well as the maturation of non-nucleotide small-molecule inhibitors with alternative binding modes. In addition, CD73-targeted antibodies, nanobodies, and positron emission tomography (PET) tracers are discussed in the context of translational development, patient stratification, and combination therapy. Patent databases were systematically surveyed to identify relevant disclosures and emerging trends. EXPERT OPINION: Recent patents indicate a shift from maximizing enzymatic potency toward balanced optimization of potency, pharmacokinetics, and combinatorial compatibility. Perorally bioavailable small molecules and CD73-targeted imaging agents are positioning CD73 inhibition as a mature and versatile therapeutic and theranostic strategy.
LSD1 inhibitors for anticancer therapy: an updated patent review (2022-2025).
Zhang Z, Li J, Wang Z … +4 more , Zhou J, Xiong X, Hou W, Li H
Expert Opin Ther Pat · 2026 Apr · PMID 41718540 · Publisher ↗
INTRODUCTION: Lysine-specific demethylase 1 (LSD1) is a key epigenetic enzyme relying on flavin adenine dinucleotide to regulate gene expression via histone H3 demethylation and non-histone substrate modification. Discov...
INTRODUCTION: Lysine-specific demethylase 1 (LSD1) is a key epigenetic enzyme relying on flavin adenine dinucleotide to regulate gene expression via histone H3 demethylation and non-histone substrate modification. Discovered in 2004, it overturned the view that histone modifications are irreversible. Abnormal LSD1 overexpression drives solid tumor and hematological malignancy initiation, progression, and drug resistance, making it a key oncology target. AREAS COVERED: This review discusses recent innovations in LSD1 inhibitor development, focusing on small-molecule patents published from 2022 to 2025. A systematic search of SciFinder, Derwent Innovation, and WIPO databases was conducted for this period. It categorizes these novel inhibitors into six classes and summarizes their structural features, biological data, design strategies and LSD1 interaction mechanisms. EXPERT OPINION: In recent years, LSD1 inhibitors have demonstrated structural diversification, innovative mechanisms, and expanded indications. Concurrently, breakthroughs have been achieved in optimizing structure, mechanism of action, dual-target strategies, selectivity and safety, and indications. Future efforts should focus on further validating dual-target strategies, and elucidating binding mechanisms to advance their application as a core targeted therapy in epigenetics for more malignant tumors therapy.
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