Trends in covalent drug discovery: a 2020-23 patent landscape analysis focused on select covalent reacting groups (CRGs) found in FDA-approved drugs.

INTRODUCTION: Covalent drugs contain electrophilic groups that can react with nucleophilic amino acids located in the active sites of proteins, particularly enzymes. Recently, there has been considerable interest in using covalent drugs to target non-catalytic amino acids in proteins to modulate difficult targets (i.e. targeted covalent inhibitors). Covalent compounds contain a wide variety of covalent reacting groups (CRGs), but only a few of these CRGs are present in FDA-approved covalent drugs. AREAS COVERED: This review summarizes a 2020-23 patent landscape analysis that examined trends in the field of covalent drug discovery around targets and organizations. The analysis focused on patent applications that were submitted to the World International Patent Organization and selected using a combination of keywords and structural searches based on CRGs present in FDA-approved drugs. EXPERT OPINION: A total of 707 patent applications from >300 organizations were identified, disclosing compounds that acted at 71 targets. Patent application counts for five targets accounted for ~63% of the total counts (i.e. BTK, EGFR, FGFR, KRAS, and SARS-CoV-2 Mpro). The organization with the largest number of patent counts was an academic institution (Dana-Farber Cancer Institute). For one target, KRAS G12C, the discovery of new drugs was highly competitive (>100 organizations, 186 patent applications).

3D printing chronicles in medical devices and pharmaceuticals: tracing the evolution and historical milestones.

The objective of this study is to collect the significant advancements of 3D printed medical devices in the biomedical area in recent years. Especially related to a range of diseases and the polymers employed in drug administration. To address the existing limitations and constraints associated with the method used for producing 3D printed medical devices, in order to optimize their suitability for degradation. The compilation and use of research papers, reports, and patents that are relevant to the key keywords are employed to improve comprehension. According to this thorough investigation, it can be inferred that the 3D Printing method, specifically Fuse Deposition Modeling (FDM), is the most suitable and convenient approach for preparing medical devices. This study provides an analysis and summary of the development trend of 3D printed implantable medical devices, focusing on the production process, materials specially the polymers, and typical items associated with 3D printing technology. This study offers a comprehensive examination of nanocarrier research and its corresponding discoveries. The FDM method, which is already facing significant challenges in terms of achieving optimal performance and cost reduction, will experience remarkable advantages from this highly valuable technology. The objective of this analysis is to showcase the efficacy and limitations of 3D-printing applications in medical devices through thorough research, highlighting the significant technological advancements it offers. This article provides a comprehensive overview of the most recent research and discoveries on 3D-printed medical devices, offering significant insights into their study.

Functional metamaterials for wireless antenna applications - A review abetted with patent landscape analysis.

The communication network made the globe a single entity and easily acessible by everyone at any time. Growth in communication networks is unimaginable and advanced nowadays. It is growing every day by means of medium or components used in communication. There are various significant components that are generally used in the communication networks. Specifically, wireless communication (WC) is the dominant in today's communication world. It is supported by the transmitting and receiving nodes at each end of communication. The common components in communication antennas are the transmitters and receivers. It has been unalterable for many decades but their capabilities have been improved through various methods including their manufacturing by the use of alternative materials. This article focuses on metamaterial (MM) based wireless antennas. The growth of metamaterials utilization in the fabrication of microstrip antennas has been discussed comprehensively and its future scope has been envisaged through patent landscape analysis. It is done meticulously using the patent database and in addition, the growth of some of the metamaterials was also predicted using the landscape analysis. Some significant technologies related with metamaterials in WC that were patented have been discussed comprehensively along with the reference to recently published articles. This articles serves as a guide to the researchers working in the communication field to envisage the future advancements.

The global patent landscape of emerging infectious disease monkeypox.

BACKGROUND: Monkeypox is an emerging infectious disease with confirmed cases and deaths in several parts of the world. In light of this crisis, this study aims to analyze the global knowledge pattern of monkeypox-related patents and explore current trends and future technical directions in the medical development of monkeypox to inform research and policy. METHODS: A comprehensive study of 1,791 monkeypox-related patents worldwide was conducted using the Derwent patent database by descriptive statistics, social network method and linear regression analysis. RESULTS: Since the 21st century, the number of monkeypox-related patents has increased rapidly, accompanied by increases in collaboration between commercial and academic patentees. Enterprises contributed the most in patent quantity, whereas the initial milestone patent was filed by academia. The core developments of technology related to the monkeypox include biological and chemical medicine. The innovations of vaccines and virus testing lack sufficient patent support in portfolios. CONCLUSIONS: Monkeypox-related therapeutic innovation is geographically limited with strong international intellectual property right barriers though it has increased rapidly in recent years. The transparent licensing of patent knowledge is driven by the merger and acquisition model, and the venture capital, intellectual property and contract research organization model. Currently, the patent thicket phenomenon in the monkeypox field may slow the progress of efforts to combat monkeypox. Enterprises should pay more attention to the sharing of technical knowledge, make full use of drug repurposing strategies, and promote innovation of monkeypox-related technology in hotspots of antivirals (such as tecovirimat, cidofovir, brincidofovir), vaccines (JYNNEOS, ACAM2000), herbal medicine and gene therapy.

The Patent Landscape of mTOR and PTEN Targets.

BACKGROUND: PTEN and mTOR signaling have many roles, including antiinflammatory, immunosuppressant and cancer. OBJECTIVE: US patents were retrieved to show the current landscape of the mTOR and PTEN targets. METHODS: PTEN and mTOR targets were analyzed by patent analysis. The U.S. granted patents from January 2003 to July 2022 were performed and analyzed. RESULTS: The results showed that the mTOR target was more attractive in drug discovery than the PTEN target. Our findings indicated that most large global pharmaceutical companies focused the drug discovery related to the mTOR target. The present study demonstrated that mTOR and PTEN targets showed more applications in biological approaches compared to BRAF and KRAS targets. The chemical structures of the inhibitors of the mTOR target demonstrated some similar features to those of the inhibitors of KRAS targets. CONCLUSION: At this stage, the PTEN target may not be an ideal target subjected to new drug discovery. The present study was the first one which demonstrated that the group of O=S=O may play a critical role in the chemical structures of mTOR inhibitors. It was the first time to show that a PTEN target may be suitably subjected to new therapeutic discovery efforts related to biological applications. Our findings provide a recent insight into therapeutic development for mTOR and PTEN targets.

An Overview of the Additive Manufacturing of Bast Fiber-Reinforced Composites and Envisaging Advancements Using the Patent Landscape.

Natural fiber composites attract attention owing to their environmentally friendly attributes. Many techniques, including fiber treatment, coatings, and fiber orientations, are used to improve the strength of natural fiber-reinforced composites. Still, the strength needs to be improved as expected. At present, some automation in manufacturing is also supported. Recently, additive manufacturing (AM) of natural fiber-reinforced composites has attracted many researchers around the globe. In this work, researchers' attention to various natural fibers that are 3D printed is articulated and consolidated, and the future scope of the additive manufacturing of natural fiber-reinforced composite is envisaged using the patent landscape. In addition, some of the advancements in additive manufacturing of natural fiber composites are also discussed with reference to the patents filed lately. This may be helpful for the researchers working on AM of natural fiber composites for taking their research into new orientations.

Patent landscaping and citation network analysis to reveal the global research trends in biopriming using microbial inoculants: an insight toward sustainable agriculture.

As an alternative to harmful chemical fertilizers and toward fulfilling Sustainable Development Goals (SDGs) of the United Nations, growth promoting rhizobacterial bioinoculants, emerged as potential players. These act in multifunctional ways, including seed colonization, seed germination, stress tolerance and many more, leading to proper growth and development of plants. Biopriming seeds with these beneficial multi-trait microbes is an effective way to introduce them in the soil, and this is an example of bottom-up approach of rhizosphere engineering. Using such sustainable approach is promising and, to investigate and analyze, their research trends are of prime importance. Thus, data were retrieved using Lens and Scopus databases and used for patent landscaping and citation network analysis, respectively. For patent landscaping, documents obtained using customized keyword search were broadly from the past 35 years (1987-2022) and yielded 114 patents which were manually curated in title, abstract and claims (TAC). From the year 2000, interest in this area was observed which further gained momentum from the year 2008, and a maximum peak was observed in the year 2021. Patent profile (filed, granted and published) showed an upward trend during this tenure (1987-2022). In this research article, we aim to provide an overview of current research in this field, identify research hotspots, project future development prospects and make recommendations for further research. Patent landscaping and citation network analysis were used to analyze the recent trends in biopriming approaches using microbial bioinoculants for the first time to identify progress and hotspots in the field of seed priming with PGPRs.

Antibacterial and Antimalarial Therapeutic Agents: A Patent Perspective.

BACKGROUND: Antibacterial and antimalarial drugs play a critical role in combating infectious diseases. It is a continuous work to develop new types of antibacterial and antimalarial drugs. OBJECTIVES: To better understand current landscape and association of antibacterial and antimalarial agents, the European patent analysis was performed. METHODS: Antibacterial and antimalarial agents were analyzed by patent analysis. Patent documents from January 2003 to May 2022 were retrieved and analyzed. RESULTS: The present study indicated there were virtually three therapeutic approaches for antibacterial agents, including chemical drugs, biological products and siRNA technology. Chemical drugs were a mainstream therapeutic approach for development of both antibacterial and antimalarial agents. However, the present study found that in contrast to antimalarials, siRNA technology had been initially explored as therapeutic strategy for antibacterial agents. Also, our study is the first to show that there is a low correlation between antibacterial and antimalarial agents. CONCLUSION: Globally, our study is the first one to show that it may be not a fast approach to discover antimalarial drugs from antibacterial agents based on drug repurposing. siRNA technology as therapeutic strategy had been explored and used in antibacterial field.

Current landscape and future prospects of RET and ROS1 targets.

RET and ROS1 are becoming key targets for targeted therapy. To show current landscape of ROS1 and RET targets, a patent analysis was performed. The present results indicated that inhibitor structures of ROS1 target demonstrated unique elements compared with inhibitor structures of RET or BRAF targets. Our study was the first time to uncover that a number of inhibitor structures of ROS1 target contained sulfur and boron elements. The inhibitors of RET target could be developed for treatment of various cancers, including lung cancer, thyroid cancer, and other solid tumor, while the inhibitors of ROS1 target are virtually developed for treatment of lung cancer. Our findings provide a new insight for drug discovery of ROS1 and RET target.

Emerging Gene Therapy Approaches in the Management of Spinal Muscular Atrophy (SMA): An Overview of Clinical Trials and Patent Landscape.

Spinal muscular atrophy (SMA) is a rare autosomal recessive neuromuscular disease that is characterized by progressive muscle atrophy (degeneration), including skeletal muscles in charge of the ability to move. SMA is caused by defects in the SMN1 gene (Survival of Motor Neuron 1) which encodes a protein crucial for the survival and functionality of neuron cells called motor neurons. Decreased level of functioning SMN protein leads to progressive degeneration of alpha-motor neurons performing muscular motility. Over the past decade, many strategies directed for SMN-level-restoration emerged, such as gene replacement therapy (GRT), CRISPR/Cas9-based gene editing, usage of antisense oligonucleotides and small-molecule modulators, and all have been showing their perspectives in SMA therapy. In this review, modern SMA therapy strategies are described, making it a valuable resource for researchers, clinicians and everyone interested in the progress of therapy of this serious disorder.

A review of technological developments in lipid nanoparticle application for mRNA vaccination.

Lipid nanoparticle (LNP) technology is critical to the advancement of mRNA vaccines. However, most studies focus on technical aspects and neglect the patent landscape. Moreover, there is a lack of differentiation of LNP technology differences among mRNA, mRNA vaccines, and COVID-19 mRNA vaccines, leading to confusing comparisons. This study fills this gap by analyzing LNP technology in academic journals and patents for mRNA, mRNA vaccines, and COVID-19 mRNA vaccines. The results show (1) academic impact on journal articles and patents, but no direct positive correlation; (2) the USA leads in academic research and patents, with China following closely; and (3) many cited articles have sponsors, indicating the importance of industry-university collaboration. This research aids strategic planning in government, academia, and industry, by providing trend analysis of LNP technology in journals and patents.

Patent landscape of platelet growth factor receptor and c-KIT targets.

Type III receptor tyrosine kinase, e.g., PDGFR, are associated with various autoimmune diseases. To show the status of PDGFR and c-KIT targets, we performed the US patent analysis. The present study showed that the R&D of c-KIT target was much earlier than the R&D of PDGFR targets. Currently, the PDGFR-based target demonstrates more applications in the development of biological therapy. Our findings indicated that some inhibitors of c-KIT target contained sulfur elements or 1,3-diazine rings. The c-KIT target has more competitive edges for chemical drug discovery than the PDGFR target. c-KIT and PDGFR targets are currently preferable for drug discovery in autoimmune diseases. This study was the first to show R&D differentiation between PDGFR and c-KIT targets in drug development.

Nanocomposite hydrogels: an optimistic insight towards the treatments of ocular disorders.

BACKGROUND: The distinct anatomy and physiology of the eye represent it as a specialized organ. The noumenal physiological barriers, whose prominent role is to prevent the entrance of extracellular substances, reduce the bioavailability of medicines taken locally. Nanocarriers offer many advantages, such as site-specific drug delivery, reduced dose-related side effects, more drug loading capacity, etc. Nanoparticles, nano micelles, Nanostructured Lipid Carriers (NLCs), Solid Lipid Nanoparticles (SLNs), liposomes, polymeric nanoparticles, microspheres, microemulsions, etc., have all undergone significant analysis to overcome numerous static and dynamic obstacles. OBJECTIVE: Among the several methods of delivering drugs, one of the most captivating and demanding is ocular drug delivery (ODD). The intent of developing formulations for an extended period can be partially achieved via thermoresponsive hydrogels. It is feasible to store fluids inside a cross-linked gel system for efficient long-term administration owing to hydrogels, which are hydrophilic polymeric networks with excellent three-dimensional structures and water or biological fluid absorption capacities. Hydrogels can be incorporated into nanocarriers to achieve site-specific action and prolonged release. METHOD: Related patents and research reports with various platforms like Science Direct, Springer, PubMed, Google Scholar, Shodhganga, and Patseer were used to gather the data, and a search methodology was availed. RESULT: The paper thoroughly summarizes the strategies for incorporating drugs with hydrogel into a nanocarrier to provide sustained release and prolonged therapeutic effects. According to the comprehensive review of literature and patents like (US2015374633A1), (US10980882B2), and (WO2011018800A2), nanocarrier-loaded thermoresponsive hydrogels show promising results. CONCLUSION: Due to their propensity to alter state in reaction to temperature changes, thermoresponsive hydrogels can improve medication bioavailability. Intervening nanocarriers loaded hydrogels directly on the targeted site displays local intervention and site-specificity. Thus, the use of nanocarriers in ocular drug delivery is encouraging.

Mapping the Nanotechnology Patent Landscape in the Field of Cancer.

BACKGROUND: Currently, cancer is still a significant disease that seriously endangers human health. Therefore, advanced diagnostic technology and treatment protocols are urgently needed. The rapid development of nanotechnology is expected to provide new ideas for cancer diagnosis and treatment. OBJECTIVE: The research aims to comprehensively demonstrate the hotspots of nanotechnology applications in cancer. METHODS: In this study, an International Patent Classification codes co-occurrence network is constructed to visualize the technology landscape by simultaneously locating and ranking technologies that play an integral role in nanotechnology diffusion and bridging in the field of cancer. In addition, community identification and topic modeling highlight the latent topics in patent documents. RESULTS: The visualization results of the patent network yield five main clusters: Cluster 0 is a nanoparticle composition delivery system with liposomes as the primary carrier. Cluster 1 is mainly represented by nano-immunotherapy with immune checkpoint inhibitors. Cluster 2 is nano phototherapy based on photodynamic therapy and photothermal therapy. Cluster 3 is diagnostic imaging involving nanotechnology. Cluster 4 is a drug delivery system with nanovesicles and albumin nanoparticles as carriers. CONCLUSION: It was found that carriers represented by liposomes, vesicles, and albumin nanoparticles are essential nanomaterials in the current anticancer drug delivery systems. Integrating next-generation immunosuppressants and nanotechnology will become an important development direction for future immunotherapy. Organic/inorganic nanomaterials are pivotal in cancer imaging diagnosis and phototherapy.

Artificial intelligence enabled carbon capture: A review.

Carbon capturing is imperative to fight climate change as much carbon emissions are liberated into the atmosphere, leading to adversely negative environmental impacts. Today's world addresses all the issues with the aid of digital technologies like data pooling and artificial intelligence (AI). Accordingly, this study is articulated based on AI-assisted carbon capturing. Techniques including machine learning (ML), deep learning (DL), and hybrid techniques being adopted in carbon capture are discussed. The role of AI tools, frameworks, and mathematical models are also discussed herein. Furthermore, the confluence of AI in carbon capture patent landscape is explored. This study would allow researchers to envision the growth of AI-assisted carbon capture in mitigating climate change and meeting SDG 13 - climate action.

STING as an emerging therapeutic target for drug discovery: Perspectives from the global patent landscape.

BACKGROUND: The STimulator of INterferon Genes (STING) plays an essential role in the innate immune system by inducing the expression of type I interferons (IFNs) and inflammatory cytokines upon sensing cytosolic DNA. Although modulating STING has shown promise as a potential treatment for cancers and inflammatory and autoimmune diseases in substantial pre-clinical studies, current preliminary clinical results of STING agonists have demonstrated limited anti-tumor efficacy. Currently, there is ongoing R&D targeting STING and focusing on the delivery of next-generation therapeutics. Whereas no comprehensive analysis on the STING patent landscape has been conducted to fill the gap between basic research progress and drug development and commercialization. AIM OF REVIEW: This study summarized the current agents in the clinical stage and global patenting profiles to help identify the current status, development trends, and emerging technologies of the nascent field of STING modulation. KEY SCIENTIFIC CONCEPTS OF REVIEW: Rapidly increasing R&D efforts and outcomes targeting STING were indicated by the recently increasing number and pharmacologic classes of drug candidates in clinic as well as in emergent technological patenting activities. Despite the overall fragmental ownership of patents, several pioneers that have advanced the clinical evaluation of novel STING agonists have established the basis of STING-relevant inventions through their influential patents in the field. These patents also facilitated progress on novel STING modulators, relevant delivery systems, pharmaceutical compositions, and combination strategies with the potential for further enhancing therapeutic outcomes by targeting STING.

A 20-year patent review and innovation trends on hydrogel-based coatings used for medical device biofabrication.

This patent review encapsulates information that could be used as a reference by researchers in the fields of coatings and interfaces, biofabrication, tissue engineering, biomaterials, and biomedical engineering, as well as those especially interested in the formulation of hydrogel coatings. The state has been reviewed by introducing what has been innovated, invented, and patented in relation to hydrogel coatings. A detailed analysis of the patentability of hydrogel applications, such as the coating of medical devices to enhance their clinical performance, has been provided. During a search, 2937 patent documents were found. 2012 was the year with the most patent documents (177). Based on the patent classification, all patent documents and most inventions are intended for biomaterials for coating prostheses characterized by their function or physical properties, such as macromolecular materials, hydrogels, and biologically active materials. Additionally, research based on medicinal formulations with unique physical forms is concentrated in the majority of patents, according to knowledge clusters and expert driving factors. Finally, to demonstrate the innovation trends in hydrogel-based coatings, a selection of relevant patent applications and granted patents is proposed at the end of this paper, along with some examples of commercial products based on the patented technologies.

The Patent Landscape of BRAF Target and KRAS Target.

BACKGROUND: KRAS and BRAF targets are involved in the epidermal growth factor receptor pathway. KRAS and BRAF targets are the most frequent driver mutations in cancer. OBJECTIVE: The objective of the study was to present the recent developments in the KRAS target and the BRAF target. METHODS: KRAS target and BRAF target were analyzed by US patent analysis. All US granted patent documents from January 2002 to November 2021 were retrieved. RESULTS: The results showed both KRAS and BRAF targets to be attractive targets for developing anticancer drugs. The technology of RNA interference has been developed for drug discovery related to the KRAS target. Our study indicates that the structural screening of inhibitors between the KRAS target and the BRAF target should be an inverse option. CONCLUSION: The chemical structures of inhibitors of BRAF target exhibited a unique classification of C07D405. The inhibitors of BRAF target could be used for the treatment of various cancers. However, the inhibitors of KRAS target did not show this feature. The present study provides new insight into drug discovery involving KRAS and BRAF targets.

The worldwide patent landscape of dental implant technology.

In an aging society, quality of life improvement is emerging as an important issue, and as implants are accepted as the core of oral rehabilitation treatment, competition for leadership in developing related technologies is intensifying. In this trend, unlike what is evident in the literature, the patent landscape shows the status of industrial-based technology development. A database analysis of a total of 32,237 dental implant patents shows improvements in technology, diverse geographical characteristics, and new advances toward technological convergence in this field. Technologically, dental implant technology has shown a tendency to develop from conventional implant materials and surface treatment technologies to new material technologies making use of substances such as pure zirconium and tantalum or software technologies related to diagnosis and prognosis. Regionally, dental implant technology, which was developed mainly in Europe and the Unites States in the past, is growing explosively in East Asian countries accompanied by the recent growth of the Asian market. In summary, dental implant technology seems to be developing while trying to converge with various technological areas based on the local market environment. Therefore, it is necessary to develop a new dental implant material technology that is highly applicable to the development of hybrid information/communication technology and is suitable for a new manufacturing method. Our study may provide important information to help basic and translational researchers and their financial supporters set their research directions in advancing the development of dental implants.

Critical food and nutrition science challenges for plant-based meat alternative products.

A reduced reliance on animal-based diets with a move towards a more plant-based diet has driven the market demand for new generation sustainable plant-based meat alternatives. This review covers science and business perspectives relating to the development of plant-based meat alternatives. A conceptual framework to help inform the innovation pathway is provided. The market opportunity, consumer perspectives, the science that underpins the development of plant-based meat alternatives and patent information relating to these products are discussed. Careful navigation through the public domain science literature and patent landscape is necessary for informing the choice of ingredients, formulations and processes for producing plant-based meat alternatives. Attention to design of ingredient systems for optimization of flavor, texture, binding, color and nutrition is necessary for development of plant-based meat alternatives with desirable consumer attributes. Recommendations for further research for developing superior formulations for consumer-acceptable plant-based meat alternative products for improving sustainability outcomes are suggested.