Trithioarsenites [(RS)3As], dithioarsonites [R-As(SR′)2] and thioarsinites [R2As-SR′]: Preparations, chemical, biochemical and biological properties

Contrary to P(V) compounds, As(V) compounds can very easily reduced by thiols to As(III) thiolates that are deemed to play a central role in the metabolism of arsenic and therefore a review on the preparation and properties of the title thiolates can be of interest. The preparation of trithioarsenites, dithioarsonites and thioarsinites involves reactions of a thiol with a proper As(V) or As(III) precursor via 4-centered transition states or a thiolate by SN2 mechanisms. Convenient precursors are the solids As2O3, arsonic and arsinic acids, although for the latter two acids the separation of the product from the co-produced disulfides can be problematic. Only a few crystal structures have been reported and involve only trithioarsenites. From their chemical properties, the hydrolyses, transthiolations and air oxidations are of particular interest from mechanistic and biochemical/biological points of view. Their nucleophilicity towards alkyl halides and acyl derivatives revealed unexpected behavior. Although these molecules have many free electron pairs only three reports were found pertaining to their reaction with metal cations (Hg2+) and metal carbonyls; the mercuric complexes being not characterized. Only a few studies appeared for the action of the title compounds towards enzymes, while the patent literature revealed that they have bactericidal, fungicidal and insecticidal activities for agricultural applications, some have antiparasitic activity on animals and a few are carcinostatic.

Discovery, Development, Inventions, and Patent Trends on Mobocertinib Succinate: The First-in-Class Oral Treatment for NSCLC with EGFR Exon 20 Insertions

The majority of lung cancers are non-small-cell lung cancer (NSCLC) having a low survival rate. Recent studies have indicated the involvement of epidermal growth factor receptor (EGFR) oncogene mutations like EGFR exon 20 insertions (EGFRex20ins) mutation among NSCLC patients. The response of patients of NSCLC with the EGFRex20ins mutation to the currently available EGFR inhibitor is negligible. Mobocertinib is the first oral treatment that has been approved by the USFDA, on 15 September 2021, to treat NSCLC with the EGFRex20ins mutation. This patent review discusses the inventions and patent literature of mobocertinib that will help the scientific community to develop additional and improved inventions related to mobocertinib. The structure of mobocertinib was first reported in 2015. Therefore, this article covered the patents/patent applications related to mobocertinib from 2015 to 25 October 2021. The patent search revealed 27 patents/patent applications related to compound, method of treatment, salt, polymorph, process, composition, and drug combinations of mobocertinib. The authors foresee an exciting prospect for developing a treatment for NSCLC with EGFRex20ins mutation, and other cancers employing a combination of mobocertinib with other approved anticancer agents. The inventions related to novel dosage forms, processes, and intermediates used in the synthesis of mobocertinib are also anticipated.

Pharmacological potentials and Nutritional values of Tropical and Sub-tropical Fruits of India: Emphasis on their anticancer bioactive components

Background: Fruits are an important dietary component, which supply vitamins, minerals, as well as dietary fiber. In addition, they are rich sources of various biological and pharmacologically active compounds. Among these, temperate fruits are well studied for their pharmacological potentials, whereas tropical/subtropical fruits are less explored for their health impacts. In India, most of the consumed fruits are either tropical or subtropical. Objectives: The present review aims to provide a health impact of major tropical and sub-tropical fruits of India, emphasizing their anticancer efficacy. In addition, the identified bioactive components from these fruits exhibiting anticancer efficacy are also discussed along with the patent literature published. Methods: The literature was collected from various repositories, including NCBI, ScienceDirect, Eurekaselect, and Web of Science; literature from predatory journals was omitted during the process. Patent literature was collected from google patents and similar patent databases. Results: Tropical fruits are rich sources of various nutrients and bioactive components including polyphenols, flavonoids, anthocyanin, etc. By virtue of these biomolecules, tropical fruits have been shown to interfere with various steps in carcinogenesis, metastasis, and drug resistance. Their mode of action is either by activation of apoptosis, regulation of cell cycle, inhibition of cell survival and proliferation pathways, increased lipid trafficking or inhibiting inflammatory pathways. Several molecules and combinations have been patented for their anticancer and chemoprotective properties. Conclusion: Overall, the present concludes that Indian tropical/ subtropical fruits are nutritionally and pharmacologically active and may serve as a source of novel anticancer agents in the future.

Unveiling the Nanotechnology-Based Drug Delivery Systems and Patent Literature for Diabetic Retinopathy

Diabetes mellitus is a principal reason for globally developing chronic microvascular disorders defined as diabetic retinopathy (DR). Proliferative retinopathy and non-proliferative retinopathy are the two types of DR. Long-term diabetes, and poor blood sugar and arterial blood pressure regulation are the key risk factors for the onset and advancement of DR. A variety of biochemical pathways are involved in the pathogenesis of DR, which includes increased polyol pathway fluxes, advanced glycation end product growth, protein kinase C isoform activation, and increased hexosamine pathway flux. The varieties of cells are involved in diabetic retinopathy, including glial cells, retinal ganglion cells, endothelial cells, and pericytes. Surgical treatment of DR includes laser treatment, panretinal photocoagulation, focal laser photocoagulation, and vitrectomy surgery. The systemic treatment of DR includes glycemic management and control of blood pressure and hyperlipidemia. Nanotechnology-based formulations like nanoparticles, polymeric nanomicelles, and nanocarrier composite, and various patented formulations have been investigated for the treatment of DR.

Patent highlights June–July 2021

A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.

High quality polymer sulfur production techniques: patent review

Основным способом предотвращения выцветания серы в резине является применение ее нерастворимой µ-формы (полимерная сера). Нерастворимая сера используется для увеличения прочности, термостойкости и износостойкости изделий. Она нашла применение также в производстве серных и сероасфальтобетонов для формирования дорожного покрытия в различных отраслях строительства. Термические методы получения полимерной серы (газификация и метод охлаждения расплава) наиболее распространены в мировом промышленном производстве. Но имеется множество до конца нерешенных проблем, таких как низкое содержание целевого продукта, использование высокотоксичных реагентов в производстве, получение плохо диспергируемого в каучуке продукта, возвращение полимерной формы в более устойчивую циклическую восьмичленную в процессе производства и хранения. Таким образом, основные тенденции в развитии методов производства полимерной серы направлены на достижение «трех максимумов» показателей нерастворимой серы, а именно: высокое содержание, высокая диспергируемость и высокая термостойкость. Целью данной статьи является обзор текущих технических достижений в области производства высококачественной полимерной серы на основе анализа мировой патентной литературы последних лет. В объем обзора входит обсуждение путей увеличения стабильности полимерной формы, количественного выхода, снижения электростатического эффекта и улучшения диспергируемости при производстве резины. Рассмотрено применение различных индивидуальных веществ и композиций для получения максимального выхода нерастворимой формы серы с прочно связанными обрывами цепочечной структуры. Представлены условия их применения, концентрации, влияние на термическую стойкость. Показано, что химическая природа стабилизатора и метод его добавления непосредственно влияют на термостойкость продукта и стабильность при хранении. Для улучшения этого комплекса свойств полимерной серы идут по пути усложнения состава добавок и многоступенчатого их ведения. Рассмотрены различные варианты традиционных и новых антистатических и диспергирующих добавок, возникающие технические и технологические проблемы при их применении. The main method of preventing sulfur from fading out of rubber is the use of its insoluble µ-form (polymeric sulfur). Insoluble sulfur is used to increase the strength, heat resistance and wear resistance of articles. It also found application in the production of sulfur concrete for the formation of pavement in various sectors of construction. Thermal methods for producing insoluble sulfur (gasification and melt cooling method) are most common in world industrial production. But there are many unresolved problems: the low content of the target product, the use of highly toxic reagents in production, the production of a product that is poorly dispersible in rubber, the return of the polymer form to a more stable cyclic eight-membered in the process of production and storage. The main trends in the development of insoluble sulfur production methods are aimed at achieving "three maxima" of insoluble sulfur indicators: high content, high dispersibility and high heat resistance. The purpose of this article is to review the current technical achievements in the production of high-quality insoluble sulfur based on the analysis of the world patent literature of recent years. The scope of the review includes discussion of ways to increase polymer form stability, quantitative yield, reduce electrostatic effect and improve dispersibility in rubber production. The use of various individual substances and compositions for maximizing the yield of insoluble form of sulfur with firmly bound cuts of chain structure is considered. The conditions of their application, concentration, influence on thermal resistance are shown. It has been shown that the chemical nature of the stabilizer and the method of its addition directly affect the heat resistance of the product and storage stability. To improve this complex of properties of polymer sulfur, the composition of additives and their multistage management are complicated. Various versions of traditional and new antistatic and dispersing additives, arising technical and technological problems in their application are considered.

Applying Seaweed Compounds in Cosmetics, Cosmeceuticals and Nutricosmetics

The interest in seaweeds for cosmetic, cosmeceutics, and nutricosmetics is increasing based on the demand for natural ingredients. Seaweeds offer advantages in relation to their renewable character, wide distribution, and the richness and versatility of their valuable bioactive compounds, which can be used as ingredients, as additives, and as active agents in the formulation of skin care products. Bioactive compounds, such as polyphenols, polysaccharides, proteins, peptides, amino acids, lipids, vitamins, and minerals, are responsible for the biological properties associated with seaweeds. Seaweed fractions can also offer technical features, such as thickening, gelling, emulsifying, texturizing, or moistening to develop cohesive matrices. Furthermore, the possibility of valorizing industrial waste streams and algal blooms makes them an attractive, low cost, raw and renewable material. This review presents an updated summary of the activities of different seaweed compounds and fractions based on scientific and patent literature.

Patent highlights April–May 2021

A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.