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Expert Opinion on Therapeutic Patents

Vincenza Andrisano, Marina Naldi, Angela De Simone, Manuela Bartolini
Butyrylcholinesterase (BuChE) has obtained a renewed interest as a therapeutic target in Alzheimer's disease (AD), when changes in BuChE activity and expression along disease progression were highlighted as well as correlation between BuChE levels and cognitive function. Areas covered. During the last seven years, fourteen patents on BuChE inhibitors (BuChEI) have been submitted. Only three of them relate to BuChE selective inhibitors, while four of them focus on multitarget inhibitors which address different key pathological factors other than BuChE...
May 14, 2018: Expert Opinion on Therapeutic Patents
Elena Cichero
No abstract text is available yet for this article.
May 14, 2018: Expert Opinion on Therapeutic Patents
Amit Kumar Halder, Ana S Moura, M Natalia D S Cordeiro
Quantitative Structure-Activity Relationship (QSAR) models are becoming one of the most interesting fields for developing therapeutics and therapeutics related patents. At present, QSAR methodologies comprise a series of possibilities, including joining forces with machine learning methods and increasing even more the swiftness they might bring to the prospective development of therapeutics in the Health Sciences scope. Areas covered: After evaluating the period from 2010 to the end of 2018, the areas covered by the reviewed QSAR based therapeutics patents comprise three main fields (drug development, risk assessment and novel QSAR methodologies), and several areas, from cancer and cancer related symptomatology to neurodegenerative diseases, such as Parkinson's disease, or even monitoring several chemical particles carrier-mediums or interface frontiers...
May 10, 2018: Expert Opinion on Therapeutic Patents
Alessio Nocentini, Claudiu T Supuran, Jean-Yves Winum
Benzoxaborole is a versatile boron-heterocyclic scaffold which has found in the last 10 years a broad spectrum of applications in medicinal chemistry, due to its physicochemical and drug-like properties. Use of benzoxaborole moiety in the design of compounds led to the discovery of new classes of anti-bacterial, anti-fungal, anti-protozoal, anti-viral as well as anti-inflammatory agents with interesting drug development perspectives. Areas covered: This article reviews the patent literature as well as chemistry literature during the period 2010-2018 where in several benzoxaborole derivatives with therapeutic options were reported...
May 4, 2018: Expert Opinion on Therapeutic Patents
Camila Kiyomi Conegundes de Jesus, Mario Sergio Salerno
Patents and patent portfolios are gaining attention in the last decades, from the called "pro-patent era" to the recent billionaire transactions involving patent portfolios. The field is growing in importance, both theoretically and practically and despite having substantial literature on new product development portfolio management, we have not found an article relating this theory to patent portfolios. Areas covered: The paper develops a systematic literature review on patent portfolio management to organize the evolution and tendencies of patent portfolio management, highlighting distinctive features of patent portfolio management...
May 2, 2018: Expert Opinion on Therapeutic Patents
Ireen Denya, Sarel Malan, Jacques Joubert
Indazoles are heterocyclic moieties rarely found in nature. They are nitrogen containing chemical compounds composed of a pyrazole ring condensed with a benzene ring. Various indazole derivatives have been described with a wide variety of biological activities. This has aroused great interest in the development of novel indazole based therapeutic agents. Areas covered: Forty-two patents published within the last 5 years (2013-2017) describing derivatives with the indazole scaffold and their therapeutic applications were analysed...
May 2, 2018: Expert Opinion on Therapeutic Patents
Olga A Luzina, Nariman F Salakhutdinov
Usnic acid (UA) is a lichen-derived secondary metabolite with a unique dibenzofuran skeleton and is commonly found in lichenized fungi of the genera Usnea, Ramalina, and Cladonia. Usnic acid has been incorporated for years in cosmetics, perfumery, and traditional medicines. The structural characteristics of UA combined with its physicochemical properties are responsible for its pleiotropic biological effects. It has a wide range of bioactivities, including antimicrobial, antiviral, anticancer, anti-inflammatory, and analgesic properties...
May 2, 2018: Expert Opinion on Therapeutic Patents
Micaela Faria Freitas, Muriel Cuendet, Philippe Bertrand
Zinc-dependent histone deacetylases (HDAC) inhibitors represent an important class of biologically active compounds with four of them approved by the FDA. A wide range of molecules has been reported for applications in several human diseases.Area covered: This review covers recent efforts in the synthesis and applications of HDAC inhibitors from 2013-2017.Expert opinion: HDAC inhibitors represent an important class of biologically active compounds for single or combination therapies. The current synthetic methodologies are oriented towards selective HDAC isoforms to achieve better therapeutic effects...
April 19, 2018: Expert Opinion on Therapeutic Patents
Valentina Sepe, Eleonora Distrutti, Stefano Fiorucci, Angela Zampella
The nuclear receptor FXR regulates the expression of genes involved in bile acids, glucose and lipid homeostasis. For its role as guardian of metabolism, FXR has been identified a promising pharmacological target in liver bile acid and lipid accumulation, such as cholestasis and non-alcoholic fatty liver disease (NAFLD). The field of FXR research is extremely competitive with a large number of patents and articles published in the last decades identifying promising hit compounds. Areas covered. The present review summarizes recent patent activity (2014-to date) filing for synthetic and natural FXR ligands, including bile acid derivatives and non-steroidal compounds, alongside their in vitro and in vivo efficacy as well as their therapeutic applications...
April 13, 2018: Expert Opinion on Therapeutic Patents
Josynaria Araújo Neves, Josyanne Araújo Neves, Rita de Cassia Meneses Oliveira
Rosmarinus officinalis L. is an aromatic plant with a number of biological properties. Recently, has been studied regarding its therapeutic potential. The objective of this study was to perform a systematic review on R. officinalis essential oil for its pharmacological properties and biotechnological applications. Areas covered: The databases were searched for articles (Science Direct, Pub Med and Web of Science) and patents (INPI, WIPO and EPO) with publications on R. officinalis and associations with essential oil (EO-Ro), cardiovascular system, hypertension and cyclodextrin...
April 10, 2018: Expert Opinion on Therapeutic Patents
Yang He, Jingshan Shen
alpha 7 subtype nicotinic acetylcholine receptor (α7 nAChR) ligands, that is, ligands that interact with the orthosteric or allosteric binding sites of α7 nAChR, hold great potential for several therapeutic applications. Numerous compounds have been designed targeting α7 nAChR but most of them cannot be used therapeutically for various reasons. Areas covered: The patent application describes a series of germinal substituted aminobenzisoxazole compounds as α7 nAChR ligands. These compounds were claimed as potential therapeutics for treating and/or improving cognitive function...
March 23, 2018: Expert Opinion on Therapeutic Patents
Hidayat Hussain, Ivan R Green, Umair Shamraiz, Muhammad Saleem, Amin Badshah, Ghulam Abbas, Najeeb Ur Rehman, Muhammad Irshad
Glycyrrhetinic acids (GAs) viz., 18β-glycyrrhetinic acid and 18α-glycyrrhetinic acid, are oleanane-type triterpenes having a carboxylic acid group at C-30, and are extracted from the Chines herbal medicine licorice (Glycyrrhiza uralensis). Although the pharmacological properties of GAs have long been known, attention to them has greatly increased in recent times due to their cytotoxic activity. Areas Covered: This review represents the patents granted about natural and synthetic glycyrrhetinic acid analogs from January 2010 to December 2017, the advances made by research groups in conjunction with pharmaceutical companies in the discovery of new natural or synthetic glycyrrhetinic acid analogs...
March 20, 2018: Expert Opinion on Therapeutic Patents
Guoqing Chen, Yong Li, Wei Wang, Liping Deng
Introduction Mangosteen as a rare and precious fruit looks like a queen crown, known as "Queen of Fruit". α-Mangostin (α-MG) is the most representative xanthone isolated from the pericarp of mangosteen, possessing extensive biological activities and pharmacological properties, which can be considered as an antineoplastic agent, antioxidant, anti-proliferation and induces apoptosis in various types of human cancer cells, and has protective effect on induced apoptotic damage. Areas covered The bioactivity and pharmacological Properties of α-MG are being actively investigated by various industrial and academic institutions...
March 20, 2018: Expert Opinion on Therapeutic Patents
Jae Eun Cheong, Anil Ekkati, Lijun Sun
Indoleamine 2,3-dioxygenase 1 (IDO1) is overexpressed by cancer cells and the antigen presenting dendritic cells in the tumor microenvironment (TME). Activation of IDO1 depletes tryptophan and produces kynurenine, which induces T cell anergy and suppresses tumor control by the immune system. When combined with an immune checkpoint inhibitor, IDO1 inhibitors have shown promising anticancer activity in preclinical tumor models as well as in early stage clinical trials. Areas covered: IDO1 inhibitors disclosed in the patent literature from 2013-2017 are categorized, when applicable, according to their structural similarity to the clinical development candidates indoximod and PF-06840003, navoximod, epacadostat, KHK2455 and aryl-1,2-diamines, and BMS-986205 among others, respectively...
April 2018: Expert Opinion on Therapeutic Patents
Xinran Wang, Wei Li, Lijuan Hao, Honglei Xie, Chenzhou Hao, Chunchi Liu, Wenyan Li, Xuqiong Xiong, Dongmei Zhao
Epidemiological studies have identified that high levels of low-density lipoprotein-cholesterol (LDL-C) and low levels of high-density lipoprotein-cholesterol (HDL-C) are two independent causes of cardiovascular disease (CVD). Statins, niacin and fibrate are used for the treatment of CVD. However, some defects are shown in the treatment process. Thus, there is a demand for better treatment strategies that confer preferable efficacy with fewer side effects. Cholesteryl ester transfer protein (CETP) promotes the movement of CEs from HDL to LDL and VLDL in exchange for triglycerides (TGs)...
April 2018: Expert Opinion on Therapeutic Patents
Kunmeng Liu, Hui-Heng Lin, Rongbiao Pi, Shinghung Mak, Yifan Han, Yuanjia Hu
Today, over 20 million people suffer from Alzheimer's disease (AD) worldwide. AD has become a critical issue to human health, especially in aging societies, and therefore it is a research hotspot in the global scientific community. The technology flow method differs from traditional reviews generating an informative overview of the research and development (R&D) landscape in a specific technological area. We need such an updated method to get a general overview of the R&D of anti-AD drugs in light of the dramatic developments in this area in recent years...
April 2018: Expert Opinion on Therapeutic Patents
Xiaofang Zuo, Zhipeng Huo, Dongwei Kang, Gaochan Wu, Zhongxia Zhou, Xinyong Liu, Peng Zhan
To deal with the rapid emergence of drug resistance challenges, together with the difficulty to eradicate the virus, off-target effects and significant cumulative drug toxicities, it is still imperative to develop next-generation anti-HIV agents with novel chemical classes or new mechanisms of action. Areas covered: We primarily focused on current strategies to discover novel anti-HIV agents. Moreover, examples of anti-HIV lead compounds were mainly selected from recently patented publications (reported between 2014 and 2017)...
April 2018: Expert Opinion on Therapeutic Patents
Kate E Donald, K M Mohibul Kabir, William A Donald
Many commercial and academic institutions protect their commercially valuable research information using patents, making the patent literature a rich and early source of cutting-edge research. While scientists and students often create the data that finds its way into patents, some rarely read the patent literature. Here, we provide an informal and brief collection of hints and tips that may assist scientists and students who do not regularly read the patent literature to locate the key scientific findings that are disclosed by patentees...
April 2018: Expert Opinion on Therapeutic Patents
(no author information available yet)
No abstract text is available yet for this article.
March 2018: Expert Opinion on Therapeutic Patents
Marie Godar, Hans de Haard, Christophe Blanchetot, Jacobus Rasser
Bispecific antibodies have become increasingly of interest by enabling new therapeutic applications such as retargeting cellular immunity towards tumor cells. About 23 bispecific antibody platforms have therefore been developed, generating about 62 molecules which are currently being evaluated for potential treatment of a variety of indications, such as cancer and inflammatory diseases, among which three molecules were approved. This class of drugs will represent a multi-million-dollar market over the coming years...
March 2018: Expert Opinion on Therapeutic Patents
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