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Expert Opinion on Therapeutic Patents

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https://www.readbyqxmd.com/read/30372652/t-type-calcium-channel-blockers-a-patent-review-2012-2018
#1
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
https://www.readbyqxmd.com/read/30366511/quorum-sensing-inhibitors-a-patent-review-2014-2018
#2
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
https://www.readbyqxmd.com/read/30359535/bicyclic-bis-heteroaryl-derivatives-as-inhibitors-of-the-%C3%AE-synuclein-protein-a-patent-evaluation-of-wo2018138088a1
#3
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
https://www.readbyqxmd.com/read/30280939/synthetic-toll-like-receptor-agonists-for-the-development-of-powerful-malaria-vaccines-a-patent-review
#4
REVIEW
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
https://www.readbyqxmd.com/read/30278800/chymase-inhibitors-for-the-treatment-of-cardiac-diseases-a-patent-review-2010-2018
#5
REVIEW
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
https://www.readbyqxmd.com/read/30273516/glutaminase-inhibitors-a-patent-review
#6
REVIEW
CanRong Wu, LiXia Chen, Sanshan Jin, Hua Li
The kidney-type glutaminase (GLS) controlling the first step of glutamine metabolism is overexpressed in many cancer cells. Targeting inhibition of GLS shows obvious inhibitory effects on cancer cell proliferation. Therefore, extensive research and development of GLS inhibitors have been carried out in industrial and academic institutions over the past decade to address this unmet medical need. Areas covered: This review covers researches and patent literatures in the field of discovery and development of small molecule inhibitors of GLS for cancer therapy over the past 16 years...
November 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/30259754/fxr-modulators-for-enterohepatic-and-metabolic-diseases
#7
REVIEW
Hong Wang, Qingxian He, Guangji Wang, Xiaowei Xu, Haiping Hao
Farnesoid X receptor (FXR), a nuclear receptor mainly expressed in enterohepatic tissues, is a master for bile acid, lipid and glucose homeostasis. Additionally, it acts as a cell protector with unclear mechanism but may be implicated in combating against inflammation, fibrosis and cancers. FXR is thus accepted as a promising target particularly for the enterohepatic diseases, and numerous FXR modulators have been patented and developed. Areas covered: This review provides an update on the development of FXR modulators for enterohepatic diseases and offers an in-depth perspective on new strategies for the development of novel FXR modulators...
November 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/30246568/novel-platinum-agents-and-mesenchymal-stromal-cells-for-thoracic-malignancies-state-of-the-art-and-future-perspectives
#8
REVIEW
Francesco Petrella, Isabella Rimoldi, Giorgio Facchetti, Lorenzo Spaggiari
Non-small cell lung cancer and malignant pleural mesothelioma represent two of the most intriguing and scrutinized thoracic malignancies, presenting interesting perspectives of experimental development and clinical applications. Areas covered: In advanced non-small cell lung cancer, molecular targeted therapy is the standard first-line treatment for patients with identified driver mutations; on the other hand, chemotherapy is the standard treatment for patients without EGFR mutations or ALK rearrangement or those with unknown mutation status...
November 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/30239247/therapeutic-potential-of-oxazole-scaffold-a-patent-review-2006-2017
#9
REVIEW
Ramandeep Kaur, Kezia Palta, Manoj Kumar, Meha Bhargava, Lalita Dahiya
Oxazoles are oxygen and nitrogen containing five membered heterocyclic ring systems that are present in various anticancer, antimicrobial, antihyperglycemic, anti-inflammatory agents etc. of natural origin. These pharmacologically active oxazole derivatives have attracted numerous researchers to explore this scaffold for the design and development of newer potential therapeutic agents. A large number of synthetic oxazole containing molecules have been reported over the period that exhibited wide spectrum of pharmacological profiles...
November 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/30217119/carbonic-anhydrase-inhibitors-and-their-potential-in-a-range-of-therapeutic-areas
#10
Claudiu T Supuran
No abstract text is available yet for this article.
October 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/30175635/applications-of-carbonic-anhydrases-inhibitors-in-renal-and-central-nervous-system-diseases
#11
REVIEW
Claudiu T Supuran
There are tissues and organs, among which kidneys and the central nervous system (CNS), rich in various isoforms of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). Their role is to regulate pH, to provide bicarbonate or H+ ions for electrolyte secretion and possibly a metabolic one. Considering these two systems, CA inhibitors are clinically used mainly as diuretics and antiepileptics, but novel applications in the management of drug-induced renal injury, sleep apnea, migraine, lowering intracranial pressure, cognitive impairment, neuropathic pain, and cerebral ischemia have emerged...
October 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/30074415/carbonic-anhydrase-inhibitors-as-antitumor-antimetastatic-agents-a-patent-review-2008-2018
#12
REVIEW
Alessio Nocentini, Claudiu T Supuran
Human carbonic anhydrases (CA, EC 4.2.1.1) IX and XII are tumor-associated proteins, being part of the molecular machinery that tumor cells build as adaptive responses to hypoxia and acidic conditions characteristic of the 'glycolytic shift' of many tumors. A wealth of research depicts CA IX and CA XII as biomarkers and therapeutic targets for various cancer types. Areas covered: The review presents an overview of the role of CA IX and CA XII in hypoxic tumors physio-pathology as well as the principal molecular, structural, and catalytic features of both isozymes...
October 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/30010459/carbonic-anhydrase-enzymes-for-regulating-mast-cell-hematopoiesis-and-type-2-inflammation-a-patent-evaluation-wo2017-058370
#13
Jean-Yves Winum
Activity modulators of carbonic anhydrases hold great potential for several therapeutic applications against ophthalmologic and neurological disease, cancer, and infectious diseases. The involvement of carbonic anhydrase in the regulation of mast cell response opens new ways for the treatment of mastocytosis, allergic inflammation, and parasite infection. Areas covered: The application claims the use of carbonic anhydrase activity modulators (inhibitors or activators) for treating allergic disease, bacterial infection, fungal infection, viral infection, mastocytosis, or mast cell-mediated inflammation...
October 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/29973089/biomedical-applications-of-prokaryotic-carbonic-anhydrases
#14
REVIEW
Claudiu T Supuran, Clemente Capasso
The hydration/dehydration of CO2 catalyzed by carbonic anhydrases (CAs, EC 4.2.1.1) is a crucial physiological reaction for the survival of all living organisms because it is connected with numerous biosynthetic and biochemical pathways requiring CO2 or HCO3 - , such as respiration, photosynthesis, carboxylation reactions, pH homeostasis, secretion of electrolytes, transport of CO2 , bicarbonate, etc. Areas covered: The bacterial genome encodes CAs belonging to the α-, β-, and γ-CA classes able to ensure the survival and/or satisfying the metabolic needs of the bacteria, as demonstrated by in vivo and in vitro experiments...
October 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/29972645/treatment-of-sleep-apnea-with-a-combination-of-a-carbonic-anhydrase-inhibitor-and-an-aldosterone-antagonist-a-patent-evaluation-of-ca2958110-and-in6616den2012
#15
Andrea Angeli, Claudiu T Supuran
Sleep apnoea syndrome (SAS), is a sleep disorder and characterized by very shallow breath or repetitive cessation of breathing during sleep (sleep apnoea). At present, no pharmacological agents have proved to be successful against SAS, and the syndrome is only treated by surgical interventions or devices such as intraoral mandibular advancement and Continuous Positive Air Pressure (CPAP) techniques. Areas covered: two patents published in 2016 describing a new pharmacological application of inhibitors of the metalloenzyme Carbonic Anhydrases (CAs, EC 4...
October 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/30185082/the-sigma-2-%C3%AF-2-receptor-a-review-of-recent-patent-applications-2013-2018
#16
REVIEW
Benjamin E Blass, John Patrick Rogers
The discovery of the sigma-2 receptor and the analogous sigma-1 receptor led to a decade-long quest to determine the true nature of this protein and novel ligands capable of modulating its activity. Despite this challenge, the sigma-2 receptor has been linked to several disease states, and multiple classes of sigma-2 ligands have been published in the 40+ years since its initial discovery. Areas covered: This review covers newly published patent applications that describe sigma-2 receptor ligands capable of modulating disease states...
September 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/30175633/technological-development-of-microemulsions-with-perspectives-for-pain-treatment-a-patent-review
#17
REVIEW
Marluce Pereira Damasceno Lima, Everton Moraes Lopes, Laércio da Silva Gomes, Ana Rita de Sousa França, Boris Timah Acha, André Luis Menezes Carvalho, Fernanda Regina de Castro Almeida
Microemulsions are thermodynamically stable translucent systems widely used for systemic delivery of drugs. The present study is the first to analyze the biotechnological potential of microemulsion systems for therapeutic purposes, through transdermal route, for pain treatment. Areas covered: Patents were searched in the World Intellectual Property Organization (WIPO), European Patent Office (Espacenet), United States Patent and Trademark Office (USPTO) and National Institute of Intellectual Property (INPI)...
September 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/30148408/site-specific-delivery-of-polymeric-encapsulated-microorganisms-a-patent-evaluation-of-us20170165201a1
#18
Inderbir Singh, Pradeep Kumar, Viness Pillay
Probiotics inculde live microorganisms therapeutically effective in the treatment of wide range of diseases. Probiotics possibly stimulates the growth of preferred microorganisms, crowds out potentially harmful microorganisms, and reinforces the body's natural defense mechanisms. Microencapsulation of probiotic microorganisms protects them from the destructive environment and prolongs their survival. Use of mucoadhesive and pH responsive polymers could impart extended retention, pH sensitive release and mucoadhesive properties to the system...
September 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/30124346/5-ht1a-receptor-ligands-and-their-therapeutic-applications-review-of-new-patents
#19
REVIEW
Jakub Staroń, Ryszard Bugno, Adam S Hogendorf, Andrzej J Bojarski
5-HT1A R was one of the first discovered serotonin receptors and is one of the most thoroughly studied. Dysfunctions associated with 5-HT1A R neurotransmission are linked to several psychiatric disorders, including anxiety, depression, and movement disorders. Areas covered: The current review covers patent literature published between January 2012 and May 2018. Queries were performed on Espacenet, SciFinder, clinicaltrials.gov, pharmacodia.com, and the websites of pharmaceutical companies. Expert opinion: Several novel therapeutic applications have been proposed for 5-HT1A R ligands, i...
September 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/30107136/a-patent-review-on-pd-1-pd-l1-antagonists-small-molecules-peptides-and-macrocycles-2015-2018
#20
REVIEW
Shabnam Shaabani, Harmen P S Huizinga, Roberto Butera, Ariana Kouchi, Katarzyna Guzik, Katarzyna Magiera-Mularz, Tad A Holak, Alexander Dömling
The protein-protein interaction PD1/PD-L1 is an important immune checkpoint and several recently approved monoclonal antibodies show promising anti cancer activities in the clinical practice. However, only a small percentage of cancer patients benefit from PD1/PD-L1 directed mAbs. Moreover, some patients experience immune related side effects upon treatment with these mAbs. Recently, several atomic-resolution structures of human PD1/PD-L1, and small molecules, peptides and mAbs with PD-L1 and PD1 open the field for structure based drug design...
September 2018: Expert Opinion on Therapeutic Patents
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