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Expert Opinion on Therapeutic Patents

Gabriella Marucci, Diego Dal Ben, Catia Lambertucci, Aleix Martí Navia, Andrea Spinaci, Rosaria Volpini, Michela Buccioni
The GPR17 receptor, phylogenetically related to both purinergic P2Y and CysLT receptors, is mainly expressed in the CNS and, in general, in organs that can typically undergo ischemic damage. This receptor is involved in various pathologies including stroke, brain and spinal cord trauma, multiple sclerosis and in all diseases characterized by neuronal and myelin dysfunction. Therefore, there is a strong needed to identify molecules capable of binding specifically to GPR17 receptors. Areas covered: The review provides a summary of patents, published between 2009 and 2018, on chemicals and biologics and their clinical use...
January 14, 2019: Expert Opinion on Therapeutic Patents
Xiao Li, Chen Wang, Hao Jiang, Cheng Luo
Protein arginine methyltransferases (PRMTs) are fundamental enzymes that specifically modify the arginine residues of versatile substrates in cells. The aberrant expression and abnormal enzymatic activity of PRMTs are associated with many human diseases, especially cancer. PRMTs are emerging as promising drug targets in both academia and industry. Areas covered: This review summarizes the updated patented inhibitors targeting PRMTs from 2010 to 2018. The authors illustrate the chemical structures, molecular mechanism of action, pharmacological activities as well as the potential clinical application including combination therapy and biomarker-guided therapy...
January 14, 2019: Expert Opinion on Therapeutic Patents
Jingwen Qua, Jiahong Lua, Yuanjia Hua
By 2020, nearly one million people will live with Parkinson's disease (PD) in the U.S. This disorder has a significant impact on patients' quality of life and is a burden on families and society. Protracted efforts have been made to treat the disease. Cumulative technological innovations are encapsulated by patents, and patent citations have been used to analyze technology diffusion processes in R&D, which is essential to identifying technology evolution trends and providing a review of PD treatment from the perspective of technology flows...
January 11, 2019: Expert Opinion on Therapeutic Patents
Xingrui He, Xiabin Chen, Hancheng Zhang, Tian Xie, Xiang-Yang Ye
Tyrosine kinase 2 (Tyk2) is a non-receptor tyrosine-protein kinase, an enzyme that in humans is encoded by the TYK2 gene. Tyk2, together with three other family subtypes namely Jak1, Jak2, and Jak3, belong to the JAK family. Before 2014, far more publications and patents appeared in public domain attributing to the development of selective Jak2 and Jak3 inhibitors than those for selective Tyk2 and Jak1 inhibitors. Areas covered: This review sought to give an overview of patents related to small molecule selective Tyk2 inhibitors published from 2015 to 2018...
January 8, 2019: Expert Opinion on Therapeutic Patents
Sávia Francisca Lopes Dias, Layane Carneiro Alves Pereira, Rosimeire Ferreira Dos Santos, Aldeidia Pereira de Oliveira, Lívio César Cunha Nunes
Primary dysmenorrhea (PD) is another term for idiopathic menstrual cramps. Treatments include the use of oral non-steroidal anti-inflammatory drugs (NSAIDs). These drugs have several side effects. The objective of this study was to perform a systematic review on the transdermal administration of drugs and the use of alternative therapies for the treatment of PD. Areas covered: The article bases were Web of Science, PubMed and Sciencedirect and the patent bases were INPI, EPO and WIPO with publications on Primary Dysmenorrhea and associations with Transdermal Administration; Complementary Therapies and Medicinal Plants...
December 27, 2018: Expert Opinion on Therapeutic Patents
Eric Aian P Silva, Jéssica S Carvalho, Adriana G Guimarães, Rosana de S S Barreto, Márcio R V Santos, André S Barreto, Lucindo J Quintans-Júnior
Terpenes are a class of secondary metabolites that can be found in a variety of animal and plants species. They are considered the most structurally diversified and abundant of all natural compounds. Several studies have shown the application of terpenes, such as carvacrol, linalool, and limonene in many pharmaceutical and medicinal fields, including cardiovascular disorders, the leading cause of death worldwide. Areas covered: In this review, the authors outlined patents from the last 10 years relating to the therapeutic application of terpenes for the treatment and/or prevention of cardiovascular diseases found in different databases, emphasizing the possibility of these compounds becoming new drugs that may help to decrease the burden of these disorders...
December 24, 2018: Expert Opinion on Therapeutic Patents
Giuseppina De Simone
Based on the initial studies of J. Folkman in 1970s, which led to the proposal of the antiangiogenic therapy, many drugs targeting VEGF or its receptors have been developed with some of them approved for cancer treatment. However, these molecules so far have shown only a limited effect on survival benefits in patients. Thus, new approaches are needed to treat this disease. Considering that cancer utilizes both aerobic and anaerobic glycolytic pathway, authors of patents US2016279084 and US2017056350 propose a method to eradicate the disease, able to affect both metabolic pathways...
December 17, 2018: Expert Opinion on Therapeutic Patents
Arina Kozlova, Raphaël Frédérick
Tryptophan-2, 3-dioxygenase (TDO2) is a tryptophan-degrading enzyme constitutively expressed in the liver and to a lesser extend in the brain. Before its link to cancer immunotherapy was discovered in 2011, the search for TDO2 inhibitors was initially driven by depression therapy. In the recent years, TDO2 has drawn an increasing attention as a promising target in both cancer and neuropsychiatric diseases. Areas covered: Patent literature regarding Tryptophan-2, 3-dioxygenase inhibitors is reviewed. Compounds are categorized by chemical structure...
December 10, 2018: Expert Opinion on Therapeutic Patents
Arezoo Rajabian, Maryam Rameshrad, Hossein Hosseinzadeh
Ginseng, Panax ginseng, has been used for various diseases and proven its great efficacy in managing central nervous system diseases. Area covered: This article covers the therapeutic potential of patents on ginseng and its active constituents to develop therapies for neurodegenerative and neurological disorders, since 2010. The literature review was provided using multiple search engines including Google Patent, Espacenet and US Patent in the field of neurodegenerative diseases, Alzheimer's disease, Parkinson's disease, cognitive, and neurological disorders...
December 4, 2018: Expert Opinion on Therapeutic Patents
Patricia Daliu, Antonello Santini, Ettore Novellino
In the last ten years, nutraceuticals have grown in interest to researchers, industry, and consumers and are now familiar in the collective imagination as a tool for preventing the onset of a disease. Often nutraceuticals are confused with biologically active phytochemicals/botanicals which can have health benefits. This is a misunderstanding however as the term nutraceutical refers to a product that must have a beneficial effect on health proven by clinical testing. Areas covered: A search has been performed on both recent patents and the literature regarding nutraceuticals focusing on the beneficial and proven health effects on pathological conditions to give an overview of the state-of-the-art developments in this area...
November 28, 2018: Expert Opinion on Therapeutic Patents
James J Crawford, Sarah M Bronner, Jason R Zbieg
The Hippo pathway represents a new and intriguing opportunity for the treatment of cancer. Activation or overexpression of YAP or TAZ has been shown to lead to cell transformation and tumor development. To date, no small molecule compounds targeting this pathway have progressed to the clinic, illustrating both its potential and its infancy. Areas covered: The present review seeks to summarize published patent applications from assignee companies that have disclosed direct small molecule inhibitors of the YAP/TAZ -TEAD interaction...
November 27, 2018: Expert Opinion on Therapeutic Patents
Qing-Wen Zhang, Zi-Dan Ye, Lei Shi
The receptor tyrosine kinase c-Met is involved in the formation, metastasis and invasion of various malignant tumors thus it has been an attractive target for anti-tumor drug designing. Many compositions targeting c-Met have been developed in pharmaceutical industry for cancer therapy and some of them are in clinical study now. Among them, Crizotinib was the first small molecular inhibitor approved by FDA in 2011. Areas covered: This review briefly summarizes the signal transduction pathway about c-Met, its role in oncogenesis, most recent patents of small-molecule inhibitors and antibodies of c-Met from 2014 to 2017...
November 24, 2018: Expert Opinion on Therapeutic Patents
Xin Li, Ekinci Elmira, Sagar Rohondia, Jicang Wang, Jinbao Liu, Q Ping Dou
Ubiquitin-Proteasome System (UPS) has been validated as a novel anticancer drug target in the past 20 years. The UPS contains two distinct steps: ubiquitination of a substrate protein by ubiquitin activating enzyme (E1), ubiquitin conjugating enzyme (E2), and ubiquitin ligase (E3), and substrate degradation by the 26S proteasome complex. The E3 enzyme is the central player in the ubiquitination step, and has a wide range of specific substrates in cancer cells, offering great opportunities for discovery and development of selective drugs...
November 19, 2018: Expert Opinion on Therapeutic Patents
Hao Li, Shi-Ying Huang, Fang-Hong Shi, Zhi-Chun Gu, Shun-Guo Zhang, Ji-Fu Wei
The α4 β7 integrin is heterodimeric cell surface receptors expressed on most leukocytes. Mucosal addressing cell adhesion molecule 1(MAdCAM-1) is an exclusive ligand for α4 β7 integrin. Areas covered: This article will highlight the progress that has been made in the discovery and development of α4 β7 integrin inhibitors, and their use in the treatment of inflammatory bowel diseases, multiple sclerosis, asthma, hepatic disorders, human immunodeficiency virus, allergic conjunctivitis and type 1 diabetes...
November 16, 2018: Expert Opinion on Therapeutic Patents
Barnali Maiti, Balamurali M M, Kaushik Chanda
There is great potential in the synthetic development of rufinamide to treat childhood onset epilepsy known as Lennox-Gastaut syndrome (LGS). Areas covered: 1,4-disubstituted triazole ring formed by 1,3-dipolar cycloaddition reaction is an important structural motif widely used to construct diverse chemotypes in chemical, biological and material fields. 1,2,3-triazole ring containing rufinamide, an antiepileptic drug developed by Novartis is useful in combination with other antiepileptic medicaments for the treatment of childhood onset epilepsy known as Lennox-Gastaut syndrome (LGS)...
November 15, 2018: Expert Opinion on Therapeutic Patents
Ghilsoo Nam
T-type calcium channels are attractive targets for potential treatment of epilepsy inflammatory or neuropathic pain, insomnia, Parkinson's disease, and cancer. Three isoforms having different biophysical functions are expressed in peripheral and central nerve. Since the withdrawal of mibefradil, the first compound marketed for selective T-type calcium channel blockade, extensive efforts have been made to identify more selective T-type calcium channel blockers. Areas covered: This review covers the 43 patents describing 'organic small molecules as T-type calcium channel blockers'-published since 2012...
October 29, 2018: Expert Opinion on Therapeutic Patents
Xin Chen, Likun Zhang, Mingxiang Zhang, Huayu Liu, Panrui Lu, Kejiang Lin
Quorum sensing (QS) is a cell density-dependent phenomenon in which specific pathways are activated after autoinducers (AIs) outside the microorganism reach a threshold concentration. QS creates a positive feedback loop that induces a cascade of gene expression and causes biofilm formation, virulence and sporulation. QS signals are diverse, acyl-homoserine lactone (AHL), AI peptide (AIP) and AI-2 are three major categories of QS signals. QS inhibitors (QSIs) can disrupt or prevent the formation of biofilm and reduce virulence while exerting less selective pressure on the bacteria, suggesting that QSIs are potential alternatives for antibiotics...
October 26, 2018: Expert Opinion on Therapeutic Patents
Jacques Joubert
Neurodegenerative diseases commonly present misfolding and aggregation of one or more proteins, including α-synuclein, β-amyloid and tau. Several research efforts have been made to develop therapeutic agents able to reduce the neurotoxic effects of aggregated proteins. Among these, the inhibition of α-synuclein by small molecules has been considered a promising approach. Areas covered: New bis-heteroaryl derivatives based on the N-[1-(1H-indol-3-yl)hexan-2-yl]-1,3-thiazole-5-carboxamide scaffold with different heterocyclic substitutions at the 2-thiazole position showed interesting ability to inhibit self-aggregation of α-synuclein in vitro and were claimed as potential therapeutics for various neurodegenerative diseases...
October 25, 2018: Expert Opinion on Therapeutic Patents
Arshpreet Kaur, Deepika Kannan, Surinder K Mehta, Shailja Singh, Deepak B Salunke
Currently, there is no efficient vaccine available against clinical malaria. However, continuous efforts have been committed to develop powerful antimalarial vaccine by discovery of novel antigens with in-depth understanding of its nature, immunogenicity, and presentation (delivery adjuvants). Moreover, another important part of vaccine development includes discovery of better immunostimulatory formulation components (immunostimulants). A protective vaccine against malaria requires antigen-specific B and T helper cell responses as well as cytotoxic T lymphocyte (CTL) responses...
November 2018: Expert Opinion on Therapeutic Patents
Sarfaraz Ahmad, Carlos M Ferrario
Chymase is primarily found in mast cells (MCs), fibroblasts, and vascular endothelial cells. MC chymase is released into the extracellular interstitium in response to inflammatory signals, tissue injury, and cellular stress. Among many functions, chymase is a major extravascular source for angiotensin II (Ang II) generation. Several recent pre-clinical and a few clinical studies point to the relatively unrecognized fact that chymase inhibition may have significant therapeutic advantages over other treatments in halting progression of cardiac and vascular disease...
November 2018: Expert Opinion on Therapeutic Patents
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