Marine natural products as source of new drugs: an updated patent review (July 2018-July 2021).

INTRODUCTION: Marine natural products have aided as rich sources of new bioactive agents. The multiplicity of marine habitations and exclusive ecological conditions of the sea offer mostly unexploited sources of unique biological and chemical entities. In continuation with the authors' previous publication, the present study reviews recently published patents in correlation to the efforts in finding new therapeutically potent chemical and biological entities from marine organisms. AREAS COVERED: This review summarizes the progress in the field of marine natural products as therapeutic agents based on an analysis of the patents published after June 2018. We have identified 68 unique patent families related to novel marine natural products for this time period. Patent information pertaining to therapeutic applications and clinical studies has been analyzed and reported. EXPERT OPINION: Marine organisms are excellent producers of secondary metabolites with diverse structures and pharmacological activities. Cumulative increase in the number of patents published during the last few years justifies the importance of this study for spotting new entities as sources of therapeutic agents. The new compounds have been claimed to show a range of activities predominantly anticancer, antimicrobial, anti-inflammatory, and neuroprotection. Majority of the recent patents have been filed by Chinese inventors, and a number of these patents are still in the prosecution stage.

Ferroportin-inhibitor salt: patent evaluation WO2018192973.

INTRODUCTION: Iron is a crucial element necessary for blood formation in the body and its normal growth. However, irregular metabolism of iron due to absence of an elimination mechanism may deposit excess iron in the organs (iron overload) leading to metabolic disorders. Interactions between the iron regulatory peptide hormone, hepcidin and the iron exporter ferroportin plays major role in regulating the iron metabolism. Mutations in the ferroportin encoding genes, and dysregulation of hepsidin production often results in iron overload resulting in conditions like hemochromatosis, ß-thalassemia, and sickle cell anemia. Until today, there is no efficacious treatment available for managing iron overload targeting ferroportin inhibition via oral administration. AREAS COVERED: Novel salts of substituted benzoimidazole compounds useful for the prophylaxis and/or treatment of iron overload are claimed. These compounds act as hepcidin mimetic and inhibit the ferroportin thereby preventing iron overload. The claimed actives are useful in the treatment of disease conditions such as neurodegenerative and cardiac diseases triggered by iron overload. Preclinical studies of these salts on mouse model are also discussed. EXPERT OPINION: Prevention and/or treatment of iron overload is critical. The claimed compounds are the first oral drug candidate to treat iron overload and reach the pre-clinical development stage.

Therapeutic and cosmetic applications of mangiferin: an updated patent review (patents published after 2013).

INTRODUCTION: Mangiferin and its derivatives possess diverse biological activities and desirable drug like properties. In continuation with the authors' previous publication, the present study reviews recently published patents in correlation with efforts of drug development using mangiferin. AREAS COVERED: Patents published after the year 2013 were analyzed for therapeutic and cosmetic applications of mangiferin, its salts, derivatives, and preparations. Patent information pertaining to improving solubility and bioavailability of mangiferin and related bioactives has also been presented. Methods of extraction of mangiferin and poly herbal preparations have not been included. Biological testing data has been put forth to understand the clinical trial status of products comprising mangiferin and/or its derivatives. EXPERT OPINION: Mangiferin has been highlighted as a multitarget bioactive with therapeutic potential. Research efforts in the recent years have contributed to development of new mangiferin derivatives as well as mangiferin formulations with enhanced solubility and bioavailability. Improvements in drug delivery systems for mangiferin might contribute to designing clinical trials to validate its therapeutic potential in humans. Majority of the recent patents have been filed by Chinese inventors claiming second medical use of mangiferin or its related compounds. However, a number of these patents remain in the prosecution stage.

Marine natural products as source of new drugs: a patent review (2015-2018).

INTRODUCTION: Natural products from plants, animals, microbes, and minerals have long been a traditional source for the treatment of human diseases. In the past decades, research on natural products for the pharmaceutical industry had declined due to numerous challenges. However, the recent developments in analytical technology, spectroscopy, and high-throughput screening have tremendously revived natural product drug discovery, including contribution from marine-based drugs. The marine environment is a unique resource enclosing a massive biological diversity, which if genuinely explored might potentially lead to breakthrough therapies. A growing number of compounds from marine sources are entering clinical trials and thus, the impact of this field on the pharmaceutical industry is increasing. AREAS COVERED: This review summarizes the progress in the field of marine natural products as therapeutic agents based on an analysis of the patents published in the period January 2015 through June 2018. EXPERT OPINION: Marine organisms are excellent producers of natural chemicals with diverse structures and pharmacological activities. Cumulative increase in the number of patents published in the last few years clearly justifies the importance of these chemicals as sources of new therapeutic agents and this study. Despite the critical supply challenges, marine-derived actives are being explored as sources for anticancer, antimicrobial, antiviral and anti-inflammatory drugs and treatments for several other conditions.

Therapeutic use of colchicine and its derivatives: a patent review.

INTRODUCTION: Colchicine, the major alkaloid extracted from the meadow saffron (Colchicum autumnale) is one of the most prominent natural products belonging to the class of organic compounds known as tropones. Colchicine's medicinal properties have been long-known, but it has been attracting renewed attention due to its action as an antimitotic agent. Areas covered: This review presents an update and analysis of the patents claiming therapeutic activity of colchicine and its derivatives published in the last five years (2010-2015). Other patents claiming the application of colchicine in the areas of biotechnology, veterinary, and agriculture are therefore excluded from this review. Expert opinion: Rapid increase in the number of publications and patent filings in recent years for the significant therapeutic potential of colchicine, for several conditions beyond gout, clearly indicates the growing interest of research on this molecule. Although the molecular structure of colchicine fulfils the four Lipinski's requisites for high oral bioavailability, the toxic side effects resulting from its fast metabolism need to be assessed. Further efforts are therefore required to explore the appropriate dosage and possible administration techniques of colchicine for practical use.

Azaepothilone B and its derivatives: a patent review.

INTRODUCTION: Azaepothilone B, also known as ixabepilone, is a semi synthetic second generation epothilone B analogue. Azaepothilone B, its derivatives, and analogues, are used for treating advance metastatic breast cancer. It has been used as a chemotherapeutic medication for cancer. AREAS COVERED: This review highlights the patents on different routes for synthesis of azaepothilone B, its derivatives and analogues. The review will also provide the reported pharmacological activity and its polymorphs in the treatment of several cancers, such as breast cancer (metastatic or locally advanced), non-Hodgkin's lymphoma, and pancreatic cancer. In addition, it considers other proliferative diseases such as viral infections, degenerative diseases of the musculoskeletal system, kidney disease, and immune response related diseases. Different databases such as Espacenet, ISI Web of Knowledge, Patbase, and Thomson Innovation have been searched extensively to review the patents. The analysis has been done to indicate the patenting trend across years and the comparison of active assignees. EXPERT OPINION: Azaepothilone B, along with its derivatives and analogues, can damage cancer cells in very low concentrations and retain its activity when tumor cells are insensitive to paclitaxel. Hence, it is highly potent agent. Azaepothilone B alone, in combination with other chemotherapeutics, or in the form of formulations, led to applications in various types of cancer. Also, antiproliferative activity of azaepothilone B has great potential for the treatment of proliferative diseases, such as skin diseases and infections. Recent progress in synthesizing azaepothilone B has encouraged researchers to develop new methods for the synthesis of azaepothilone B, its derivatives, and analogues, to obtain maximum yield in minimum steps.

'Click chemistry' for diagnosis: a patent review on exploitation of its emerging trends.

INTRODUCTION: Click chemistry is the novel synthetic approach towards developing reactions with large thermodynamic driving forces to give almost complete conversion of new molecular reagents to a single product. Thus, click chemistry describes the chemistry for making carbon-heteroatom-carbon bonds in benign solvents, especially in water, and having a plethora of chemical and biological applications. This has played an important role in early detection of diseases, real-time monitoring of drug delivery and investigating the biomolecular functions in vivo. AREAS COVERED: This review aims at highlighting the research advancements in click chemistry published in the patent literature and categorizing the patents according to the technological progress. An extensive search was carried out to collect and analyze the patent information claiming the use of click chemistry in biotechnology, especially for diagnosis. The study further concentrates on licensing of the click chemistry patents and defining the recent breakthroughs. Different databases like Espacenet, ISI Web of Science, Patbase and Thomson Innovation are used to compile the relevant literature. EXPERT OPINION: In recent years, considerable development in the click concept has encouraged researchers in using click reactions in almost every branch of industry that uses chemistry. Click chemistry for chemical ligation has been immensely explored in the field of biotechnology especially for detection, diagnosis and therapeutics.

Therapeutic and cosmetic applications of mangiferin: a patent review.

INTRODUCTION: Mangiferin, a natural C-glucoside xanthone [2-C-ß-D-glucopyranosyl-1, 3, 6, 7-tetrahydroxyxanthone], is abundantly present in young leaves and stem bark of the mango tree. The xanthonoid structure of mangiferin with C-glycosyl linkage and polyhydroxy components contributes to its free radical-scavenging ability, leading to a potent antioxidant effect as well as multiple biological activities. AREAS COVERED: An extensive search was carried out to collect patent information on mangiferin and its derivatives using various patent databases spanning all priority years to date. The patents claiming therapeutic and cosmetic applications of mangiferin and its derivatives were analyzed in detail. The technology areas covered in this article include metabolic disorders, cosmeceuticals, multiple uses of the same compound, miscellaneous uses, infectious diseases, inflammation, cancer and autoimmune disorders, and neurological disorders. EXPERT OPINION: Mangiferin has the potential to modulate multiple molecular targets including nuclear factor-kappa B (NF-κB) signaling and cyclooxygenase-2 (COX-2) protein expression. Mangiferin exhibits antioxidant, antidiabetic, antihyperuricemic, antiviral, anticancer and antiinflammatory activities. The molecular structure of mangiferin fulfils the four Lipinski's requisites reported to favor high bioavailability by oral administration. There is no evidence of adverse side effects of mangiferin so far. Mangiferin could thus be a promising candidate for development of a multipotent drug.