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Expert Opinion on Therapeutic Patents

Farha Quadri, Manasi Telang, Anita Mandhare
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 analysed 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...
May 16, 2019: Expert Opinion on Therapeutic Patents
Shinya Fujii, Hiroyuki Kagechika
Androgen receptor (AR) is one of the most promising targets of drug discovery because of its importance in male reproductive systems and homeostasis of bone and muscle. Various AR-modulating agents have been developed and used clinically to treat androgen-dependent disorders, including prostate cancer, and some new-generation antiandrogens have recently been approved. Intensive studies are underway to develop various AR-modulating compounds, including conventional antagonists, tissue-specific AR modulators (SARMs), degraders, and nonconventional AR-modulating compounds that target sites other than the ligand-binding domain (LBD), such as the N-terminal domain (NTD) or the DNA-binding domain (DBD)...
May 16, 2019: Expert Opinion on Therapeutic Patents
Marcello Leopoldo, Patrizia Nardulli, Marialessandra Contino, Francesco Leonetti, Gert Luurtsema, Nicola Antonio Colabufo
P-glycoprotein is a complex ATP-ase transporter involved in physiological and pathological functions. In particular, it is involved in the onset of multidrug resistance in cancer, in ocular disease, Chronic Rhinosinusitis, CNS diseases such as Alzheimer, Parkinson and epilepsy. One of the aims of clinicians and pharmacologists is to monitor P-gp activity through the inhibitors and to use its activity and/or expression in physiological barriers for the early diagnosis of several pathologies. Considering P-glycoprotein activity, several substrates have been characterized but the challenge is to design "pure" P-glycoprotein inhibitors...
May 11, 2019: Expert Opinion on Therapeutic Patents
Xiao-Na Wang, Xiao-Xuan Su, Sui-Qi Cheng, Zhi-Yin Sun, Zhi-Shu Huang, Tian-Miao Ou
The important role of MYC in tumorigenesis makes it particularly important to design MYC modulators. Over the past decade, researchers have raised a number of strategies for designing MYC modulators, some of which are already in clinical trials. This paper aims to review the patents of MYC modulators. Areas covered: The important biological relevance of c-MYC and the regulation pathways related to c-MYC are briefly introduced. Base on that, the MYC modulators reported in published patents and references primarily for cancer treatment are outlined, highlighting the structures and biological activities...
May 8, 2019: Expert Opinion on Therapeutic Patents
Karla S Romero-Aguilar, Ivonne M Arciniega-Martínez, Eunice D Farfán-García, Rafael Campos-Rodríguez, Aldo A Reséndiz-Albor, Marvin A Soriano-Ursúa
Boron-containing compounds induce effects on immune responses. Such effects are interesting to the biomedical field for the development of therapeutic tools to modulate the immune system. Areas covered: The scope of BCC use to modify immune responses is expanding, mainly with regard to inflammatory diseases. The information was organized to demonstrate the breadth of reported effects. BCCs act as modulators of innate and adaptive immunity, with the former including regulation of cluster differentiation and cytokine production...
May 7, 2019: Expert Opinion on Therapeutic Patents
Debarshi Kar Mahapatra, Vivek Asati, Sanjay Kumar Bharti
Chalcone or benzylideneacetophenone or 1,3-diphenyl-2-propene-1-one is a natural product comprising of two aromatic rings connected together by a three-carbon α, β unsaturated carbonyl bridge. It is one of the most privileged scaffolds in medicinal chemistry that can be synthesized in the laboratory and can be converted into several therapeutically active heterocyclic scaffolds. It exhibits multifarious pharmacological activities and also plays a key role in several non-pharmacological scientific applications...
April 29, 2019: Expert Opinion on Therapeutic Patents
Mariel Dourado Alcorte, Mari Cleide Sogayar, Marcos Angelo Demasi
Recessive Dystrophic Epidermolysis Bullosa (RDEB) is a monogenetic inherited genodermatosis associated with deleterious mutations in the gene encoding type VII collagen (COL7A1). COL7A1 is essential for promoting attachment of the epidermis to the dermis, and its dysfunction may lead to generalized mucosal and cutaneous blistering associated to severe deformities. Currently, management of RDEB patients is limited to supportive care, being aimed at treating and preventing common complications associated with this condition...
April 24, 2019: Expert Opinion on Therapeutic Patents
Martin Perez-Santos, Maricruz Anaya-Ruiz, Jorge Cebada, Irma Herrera-Camacho
LAG-3 is checkpoint inhibitor in cancer that coordinates the down regulation of the proliferation of antigen-specific lymphocytes. There is a great need to discover and develop new therapies focused on inhibiting the action of LAG-3 and consequently improving the immune response in the various types of cancer. Authors of patent US2018271940 propose a method to eradicate cancer that utilizes the combination of LAG-3Ig and anti-PD-1 or anti-PD-L1 antibodies. Areas covered: Patent US2018271940 describes a method consisting of the utilization of either a pharmaceutical cocktail containing LAG-3Ig and an anti-PD-1 or anti-PD-L1 antibody for activation of T cells as a potential for the treatment of cancer...
April 16, 2019: Expert Opinion on Therapeutic Patents
Pravin Shinde, Paromita Banerjee, Anita Mandhare
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...
March 22, 2019: Expert Opinion on Therapeutic Patents
Simona Sestito, Simona Rapposelli
3-Phosphoinositide-dependent kinase 1 (PDK1), the "master kinase of the AGC protein kinase family", plays a key role in cancer development and progression. Although it has been rather overlooked, in the last decades a growing number of molecules have been developed to effectively modulate the PDK1 enzyme. Areas covered: This review collects different PDK1 inhibitors patented from October 2014 to December 2018. The molecules have been classified on the basis of the chemical structure/type of inhibition and for each general structure examples have been discussed in extenso...
March 21, 2019: Expert Opinion on Therapeutic Patents
George Amato, Nayaab Khan, Rangan Maitra
The endocannabinoid system is an important regulator of various physiological processes. Preclinical and clinical studies indicate that attenuation of the endocannabinoid system via antagonism of the type 1 cannabinoid receptor (CB1) is an excellent strategy to treat obesity, metabolic syndrome and associated disorders. However, centrally acting antagonists of CB1 also produce adverse effects like depression and anxiety. Current efforts are geared towards discovery and optimization of antagonists and modulators of CB1 that have limited brain penetration...
March 20, 2019: Expert Opinion on Therapeutic Patents
Yifan Feng, Weiming Duan, Xiaochuan Cu, Chengyuan Liang, Xin Minhang
Bruton's tyrosine kinase (BTK) plays a critical role in the regulation of survival, proliferation, activation and differentiation of B-lineage cells. It participates by regulating multiple cellular signaling pathways, including B cell receptor and FcR signaling cascades. BTK is abundantly expressed and constitutively active in the pathogenesis of B cell hematological malignancies, as well as several autoimmune diseases. Therefore, BTK is considered as an attractive target for treatment of B-lineage lymphomas, leukemias, and some autoimmune diseases...
March 19, 2019: Expert Opinion on Therapeutic Patents
Robert Watson
No abstract text is available yet for this article.
March 6, 2019: Expert Opinion on Therapeutic Patents
Jyotsana Pandey, Akhilesh K Tamrakar
The sodium-glucose co-transporter 2 (SGLT2) is ascribed to target renal tubular glucose re-absorption, and its inhibition has been proved to induce glucosuria which improves the glycemic index. Accordingly, SGLT2 inhibitors have found to be the promising class of antidiabetic agents for the management of type 2 diabetes mellitus. A large number of SGLT2 inhibitors have developed through structural modification and investigated for their ability to selectivity inhibit SGLT2 transporters with better bioavailability...
May 2019: Expert Opinion on Therapeutic Patents
Sarah A Holstein
Bisphosphonates (BPs) are widely used to manage a variety of bone disorders, including osteoporosis, metastatic bone disease and myeloma bone disease. The nitrogen-containing BPs (NBPs) target osteoclast activity by disrupting protein prenylation via inhibition of farnesyl diphosphate synthase (FDPS). Areas covered: This review summarizes the recent advances in BPs with a focus on the latest patents (2015-2018). Patents involving novel BPs, new modes of BP delivery, as well as use of BPs to deliver other drugs to bone are discussed...
May 2019: Expert Opinion on Therapeutic Patents
William T McElroy
Interleukin-1 receptor-associated kinase 4 (IRAK4) is the most upstream kinase in Toll/Interleukin-1 receptor (TIR) signaling. Human and rodent genetics support the role of IRAK4 in immune function and the involvement of IRAK4-dependent signaling in certain cancers is hypothesized. The accumulating evidence has motivated the discovery of IRAK4 inhibitors that could be used therapeutically. Areas covered: This review summarizes patents published in 2016-2018 claiming IRAK4 inhibitors. Representative analogues from each patent are presented with a focus on compounds that have been profiled in cellular and in vivo assays...
April 2019: Expert Opinion on Therapeutic Patents
Lukasz Skalniak, Ewa Surmiak, Tad A Holak
MDM2 and MDMX proteins provide the inhibition of p53 tumor suppressor, thus allowing for accelerated mutation-driven cancer microevolution. A pharmacological blockade of MDM2/X-p53 interaction results in p53 reactivation in p53wt cells, leading to cancer growth inhibition. Throughout the past 20 years, multiple chemical entities have been proposed to reactivate p53 by antagonizing MDM2/X proteins. Areas covered: This manuscript reviews 2014-2018 therapeutic patents in the field of MDM2/X antagonists and is a continuation of previous reviews on similar matter...
March 2019: Expert Opinion on Therapeutic Patents
Abdul Hameed, Mariya Al-Rashida, Maliha Uroos, Syeda Uroos Qazi, Sadia Naz, Marium Ishtiaq, Khalid Mohammed Khan
Urease is a nickel-containing metalloenzyme that is commonly found in different bacteria, plants, algae, and fungi and mediates the growth of many pathogenic bacteria in the acidic environment of the stomach. Despite the large number of molecules known to have excellent urease inhibitory activity, there is an alarming lack of urease inhibitor drugs on the market. Area covered: This review aims to provide a comprehensive overview of the different types of molecules patented as potent urease inhibitors from the year 2012 to 2018...
March 2019: Expert Opinion on Therapeutic Patents
Luca Quattrini, Concettina La Motta
Aldose reductase (ALR2) is both the key enzyme of the polyol pathway, whose activation under hyperglycemic conditions leads to the development of chronic diabetic complications, and the crucial promoter of inflammatory and cytotoxic conditions, even under a normoglycemic status. Accordingly, it represents an excellent drug target and a huge effort is being done to disclose novel compounds able to inhibit it. Areas covered: This literature survey summarizes patents and patent applications published over the last 5 years and filed for natural, semi-synthetic and synthetic ALR2 inhibitors...
February 14, 2019: Expert Opinion on Therapeutic Patents
Steven B Ouellette
Personalized diagnostic testing (PDx) is a key component of the precision medicine toolkit and has shown the most development in cancer applications. Recent changes in the regulatory and legal landscapes regarding PDx development and commercialization have brought uncertainties to both intellectual property strategies and business model development. While the regulatory and legal uncertainties have been well-documented, there has been little reported analysis of the recent patent landscape and movement of IP into the PDx market...
February 2, 2019: Expert Opinion on Therapeutic Patents
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