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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, β-thalassemia, and sickle cell anemia. Until today, there is no efficacious treatment available for managing iron overload targeting ferroportin inhibition via oral administration.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.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.

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.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.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.

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.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.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.

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.

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.