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Expert Opinion on Therapeutic Patents

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https://www.readbyqxmd.com/read/28766366/dual-specificity-tyrosine-phosphorylation-regulated-kinase-1a-dyrk1a-inhibitors-a-survey-of-recent-patent-literature
#1
Thu Lan Nguyen, Corinne Fruit, Yann Hérault, Laurent Meijer, Thierry Besson
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a eukaryotic serine-threonine protein kinase belonging to the CMGC group. DYRK1A hyperactivity appears to contribute to the development of a number of human malignancies and to cognitive deficits observed in Down syndrome and Alzheimer's disease. As a result, the DYRK1A kinase represents an attractive target for the synthesis and optimization of pharmacological inhibitors of potential therapeutic interest. Like most tyrosine kinase inhibitors developed up to the market, DYRK1A inhibitors are essentially acting by competing with ATP for binding at the catalytic site of the kinase...
August 2, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28756713/coumarinderivatives-an-updated-patent-review-2015-2016
#2
Anastasia Detsi, Christos Kontogiorgis, Dimitra Hadjipavlou-Litina
INTRODUCTION: Coumarins belong to the benzopyrone family. They are naturally plant-derived or synthetically obtained substances, presenting a wide variety of biological activities, offering an extented therapeutic profile. Their structural characteristics correlated to physicochemical properties define their pleiotropic biological responses. AREAS COVERED IN THIS REVIEW: Recent patent publications (2015-2016), describing coumarins and their derivatives are analyzed...
July 31, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28753410/pyrimido-4-5-b-indole-derivatives-and-use-thereof-in-the-expansion-of-hematopoietic-stem-cells-us2015011543-a1-a-patent-evaluation
#3
Stuti Agarwal, Hitesh Agarwal, Nilesh Zaware
No abstract text is available yet for this article.
July 28, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28749251/identification-of-spirocyclic-or-phosphate-substituted-quinolizine-derivatives-as-novel-hiv-1-integrase-inhibitors-a-patent-evaluation-of-wo2016094197a1-wo2016094198a1-and-wo2016154527a1
#4
Xiqiang Cheng, Ping Gao, Lin Sun, Ye Tian, Peng Zhan, Xinyong Liu
Highly active antiretroviral therapy (HAART) has been widely adopted to control the HIV-1 infection successfully. HIV-1 integrase (IN) inhibitors are primary drugs in HAART regimens targeting integration step in the HIV-1 life cycle. However, due to the emergence of viral resistance and cross-resistance amongst drugs, there is a pressing need for new and potent IN inhibitors. This review covers the three patents describing spirocyclic and phosphate substituted quinolizine derivatives as novel HIV-1 IN inhibitors for the discovery of new anti-HIV-1 drug candidates...
July 27, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28742403/lpxc-inhibitors-a-patent-review-2010-2016
#5
Dmitrii V Kalinin, Ralph Holl
The Zn(2+)-dependent deacetylase LpxC is an essential enzyme of lipid A biosynthesis in Gram-negative bacteria and a promising target for the development of antibiotics selectively combating Gram-negative pathogens. Researchers from industry and academia have synthesized structurally diverse LpxC inhibitors, exhibiting different LpxC inhibitory and antibacterial activities. Areas covered: A brief introduction into the structure and function of LpxC, showing its suitability as antibacterial target, along with the structures of several reported LpxC inhibitors, is given...
July 25, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28705083/pyrrolo-2-3-d-pyrimidines-active-as-btk-inhibitors
#6
Francesca Musumeci, Monica Sanna, Chiara Greco, Ilaria Giacchello, Anna Lucia Fallacara, Rosario Amato, Silvia Schenone
Btk is a tyrosine kinase dysregulated in several B-cell malignancies and autoimmune diseases, and this has given rise to a search for Btk inhibitors. Nevertheless, only one Btk inhibitor, ibrutinib, has been approved to date, although other compounds are currently being evaluated in clinical trials or in preclinal stages. Area covered: This review, after a brief introduction on Btk and its inhibitors already in clinical trials, focusses on pyrrolo[2,3-d]pyrimidine derivatives patented in the last five years as Btk inhibitors...
July 13, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28705037/saffron-and-its-derivatives-crocin-crocetin-and-safranal-a-patent-review
#7
Maryam Rameshrad, Bibi Marjan Razavi, Hossein Hosseinzadeh
Saffron and its main components have traditionally been used as pharmaceutical agents. Current experimental research projects have also exhibited their applications in a wide spectrum of disorder treatments. Area covered: This review covers the demonstrated findings and patents on therapeutic/pharmaceutical properties of saffron and related derivatives, since 2000 to bold their outstanding merit on human health. An extensive literature review was performed in USP Patent, Patentscope, Espacenet and Google Patent in the field of CNS, cardiovascular, urogenital, dermatological and inflammatory disorders...
July 13, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28699813/prolylcarboxypeptidase-prcp-inhibitors-and-the-therapeutic-uses-thereof-a-patent-review
#8
Thomas H Graham
Prolylcarboxypeptidase (PrCP) is a serine protease that produces or degrades signaling proteins in several important pathways including the renin-angiotensin system (RAS), kallikrein-kinin system (KKS) and pro-opiomelanocortin (POMC) system. PrCP has the potential to be a therapeutic target for cardiovascular, inflammatory and metabolic diseases. Numerous classes of PrCP inhibitors have been developed by rational drug design and from high-throughput screening hits. These inhibitors have been tested in mouse models to assess their potential as new therapeutics...
July 12, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28665163/what-s-new-in-treatment-of-pancreatic-cancer-a-patent-review-2010-2017
#9
Maria C Ramos, Houria Boulaiz, Carmen Griñan-Lison, Juan Antonio Marchal, Francisca Vicente
Pancreatic cancer (PC) is one of the most lethal cancers, with a median overall survival of less than 1 year and a 5-year survival of ~5%. The poor survival rate is likely due to lack of early diagnosis, fast disease course, high metastasis rate and disappointing treatment outcome. Therefore, at this stage, any new method that provides a treatment against PC without the undesirable side effects of chemotherapy and radiation is urgently needed. Areas covered: This review summarizes the latest advances in the treatment of PC through the patents published from 2010 to 2017...
July 12, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28673105/small-molecules-as-activators-in-medicinal-chemistry-2000-2016
#10
Abdul Hameed, Mariya Al-Rashida, Rima D Alharthy, Maliha Uroos, Ehsan Ullah Mughal, Syed Abid Ali, Khalid Mohammed Khan
From therapeutic point of view, it is often beneficial to enhance the expression of certain enzymes whose low expression is responsible for the observed ailment. Small molecules as activators of several enzymes have great biological potential as anti-microbial and anti-cancer agents, for the treatment of diabetes, obesity, metabolic disorders, and for the treatment of neurological disorders including Alzheimer's disease. This review covers patents describing small molecules as activators, and provides structural leads for the design of even more potent activators...
July 6, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28671001/between-pharmaceutical-patents-and-european-patients-is-a-compromise-still-possible
#11
Livio Garattini, Anna Padula
Pharmaceutical regulation has always attempted to balance the public health objective to make safe and effective drugs available for patients while providing commercial incentives through patents. Here we discuss whether it is still possible to find a balance between the incentives on the supply side and the regulatory framework on the demand side. Areas covered: The current regulatory framework on pharmaceutical exclusivity has been harshly criticized by many experts, arguing about whether it is still fit for public purposes and needs...
July 3, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28627982/mirnas-as-potential-therapeutic-targets-and-diagnostic-biomarkers-for-cardiovascular-disease-with-a-particular-focus-on-wo2010091204
#12
Yanyan Yang, Tao Yu, Shaoyan Jiang, Yinfeng Zhang, Mengpeng Li, Ningning Tang, Murugavel Ponnusamy, Jian-Xun Wang, Pei-Feng Li
A number of miRNAs have been reported to be critically involved in the regulation of cardiovascular disease (CVDs). Therefore, the development of potent analogues/inhibitors for miRNAs have thus become a key focus in the present drug discovery. In this review, we discuss the basic research and clinical use of miRNAs as the early diagnosis and therapeutic targets for CVD. We have also focused on the efficiency of therapeutically targeting miR-499, which is considered as one of the most promising molecules for treating CVDs...
July 3, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28665159/new-drugs-or-alternative-therapy-to-blurring-the-symptoms-of-fibromyalgia-a-patent-review
#13
Marlange A Oliveira, Adriana G Guimarães, Adriano A S Araújo, Lucindo J Quintans-Júnior, Jullyana S S Quintans
Fibromyalgia (FM) is a musculoskeletal condition characterized by chronic widespread pain, tenderness and often accompanied by other comorbid conditions such as depression, anxiety, chronic fatigue, among others. Now we aimed to survey the recent patents describing new drugs or alternative therapy for FM. Areas covered: This review covers the therapeutic patents published between 2010 and 2017 from specialized search databases (WIPO, DERWENT, INPI, ESPANET and USPTO) that report the discovery of new drugs or pharmacologic alternative for the treatment of FM...
June 30, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28637397/ursolic-acid-derivatives-for-pharmaceutical-use-a-patent-review-2012-2016
#14
Hidayat Hussain, Ivan R Green, Iftikhar Ali, Ikhlas A Khan, Zulfiqar Ali, Abdullah M Al-Sadi, Ishtiaq Ahmed
Ursolic acid (UA), belongs to a group of pentacyclic triterpenoids and is known to possess some very interesting biological properties. Protocols have been developed in order to synthesize bioactive UA analogs which have resulted in numerous ursolic acid analogs being synthesized during the period 2012-2016. Ursolic acid and its analogues can be employed to treat various cancers, inflammatory diseases, diabetes, Parkinson's disease, Alzheimer's disease, hepatitis B, hepatitis C and AIDS to mention but a few...
June 30, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28621575/analysis-of-radio-sensitization-patents-in-china-from-2006-to-2015
#15
Guofeng He, Xiaoke Di, Xinchen Sun, Jingjing Yan, Shu Zhang
Radiotherapy is by means of ionizing radiation to kill tumor cells, inhibit and control the growth, metastasis and diffusion of tumor cells. During the last few decades, application of radiotherapy combined with chemotherapy and surgery are clinical mainstream treatments. However, little is known what radio-sensitization agents have been patented in China and what the potential drug candidates for patents are in China. Areas covered: This reviews covers research and patent literature of the last 10 years dealing with the discovery and development of novel radio-sensitization patents in China...
June 29, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28658596/corrigendum
#16
(no author information available yet)
No abstract text is available yet for this article.
June 28, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28657794/corrigendum
#17
(no author information available yet)
No abstract text is available yet for this article.
June 28, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28631980/orexin-research-patent-news-from-2016
#18
Christoph Boss, Catherine Roch
The orexin system consists of two G-protein-coupled receptors, orexin 1 and orexin 2 and two endogenous ligands, orexin A and orexin B . It is evolutionarily highly conserved. It is involved in the promotion of wakefulness as well as in anxiety and addictive disorders. In addition, its activation via the Ox1 receptor triggers apoptosis in several cancer cell lines. Dual orexin receptor antagonists are successfully used to treat primary insomnia. The major open questions are now related to the clinical validation of Ox1 selective antagonists...
June 28, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28627961/microsomal-prostaglandin-e2-synthase-1-inhibitors-a-patent-review
#19
Anastasia Psarra, Aikaterini Nikolaou, Maroula G Kokotou, Dimitris Limnios, George Kokotos
Microsomal prostaglandin E2 synthase-1 (mPGES-1) catalyzes the terminal step of prostaglandin E2 (PGE2) generation. It is strongly upregulated in inflamed tissues and overexpressed in tumors and it has been recognized as a key enzyme in inflammatory diseases such as arthritis, atherosclerosis, stroke and cancer. Thus, a great effort has been devoted in developing synthetic mPGES-1 inhibitors as novel anti-inflammatory agents. Areas covered: This review article summarizes the mPGES-1 inhibitors presented in patent literature from 2000 to August 2016 and their biological evaluation, discussing their activities in vitro and in vivo...
June 26, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28621580/vegfr-2-inhibitors-and-the-therapeutic-applications-thereof-a-patent-review-2012-2016
#20
Fan-Wei Peng, Da-Ke Liu, Qing-Wen Zhang, Yun-Gen Xu, Lei Shi
Angiogenesis is an important component of certain normal physiological processes, but aberrant angiogenesis contributes to some pathological disorders and in particular to tumor growth. Activation of vascular endothelial growth factor receptor-2 (VEGFR-2) by vascular endothelial growth factor (VEGF) is a critical step in the signal transduction pathway that initiates tumor angiogenesis. Inhibition of angiogenesis via blocking VEGF/VEGFR-2 signaling pathway has emerged as a potential approach to anticancer therapy...
June 23, 2017: Expert Opinion on Therapeutic Patents
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