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Expert Opinion on Therapeutic Patents

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...
September 21, 2018: Expert Opinion on Therapeutic Patents
Claudiu T Supuran
No abstract text is available yet for this article.
September 14, 2018: Expert Opinion on Therapeutic Patents
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 14, 2018: Expert Opinion on Therapeutic Patents
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 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...
September 10, 2018: Expert Opinion on Therapeutic Patents
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 10, 2018: Expert Opinion on Therapeutic Patents
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,,, and the websites of pharmaceutical companies. Expert opinion: Several novel therapeutic applications have been proposed for 5-HT1A R ligands, i...
September 7, 2018: Expert Opinion on Therapeutic Patents
Benjamin E Blass, John Patrick Rogers
The discovery of the sigma-2 receptor and the analogous sigma-1 receptor led to a decades 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 6, 2018: Expert Opinion on Therapeutic Patents
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 6, 2018: Expert Opinion on Therapeutic Patents
Alessio Nocentini, Claudiu T Supuran
Human carbonic anhydrases (CA, EC 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...
August 9, 2018: Expert Opinion on Therapeutic Patents
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...
July 19, 2018: Expert Opinion on Therapeutic Patents
Claudiu T Supuran, Clemente Capasso
The hydration/dehydration of CO2 catalyzed by carbonic anhydrases (CAs, EC 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...
July 16, 2018: Expert Opinion on Therapeutic Patents
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...
July 16, 2018: Expert Opinion on Therapeutic Patents
Rakhi Dhankhar, Pooja Gulati, Sanjay Kumar, Rajeev Kumar Kapoor
Rise in incidence of various cancers and growing adoption of biological therapy to avoid side effects of conventional cancer therapies is driving the growth of the cancer biotherapy market globally. One such therapy available for the treatment of certain tumors employs arginine-lowering enzymes (ALEs). Several patents have been filed in this technology domain, and many Phase I/II clinical trials of the ALEs especially arginine deiminase (ADI) are underway. Areas covered: Patents and clinical trials in the domain of ALEs for the treatment of cancer were studied with an objective to understand technology trends, targeted areas, key players, and inventors involved...
August 2018: Expert Opinion on Therapeutic Patents
Tulshidas S Patil, Ashwini S Deshpande
Tuberculosis (TB) is a disease caused due to an infection of Mycobacterium tuberculosis (M TB) bacilli affecting millions of people worldwide. It is the ninth leading cause of death and ranks above the HIV/AIDS. The unique intracellular life cycle, more dangerous drug-resistant forms of bacilli, and insufficient investments in the TB research and development hindered the occurrence of optimum diagnostic, preventive, and treatment strategy against this disease. Areas covered: The aim of this review is to provide an update and overview of the current trends in the diagnosis, prevention, and treatment of the disease...
August 2018: Expert Opinion on Therapeutic Patents
Juliana Santos-Gandelman, Márcio Lourenço Rodrigues, Alice Machado Silva
Cryptococcosis is one of the most devastating human fungal infections. Despite its impact, none of the standard antifungals were developed after 1990. New, improved, less toxic, affordable and widely available treatment is, therefore, imperative. Areas covered: This review offers an insight into technological developments for cryptococcosis disclosed in patent literature. From a broad search of patent documents claiming cryptococcosis treatment and having earliest priority between 1995 and 2015, we selected and summarized compounds/molecules (i) revealed in documents disclosing in vivo activity against Cryptococcus spp...
August 2018: Expert Opinion on Therapeutic Patents
Yuan-Yuan Liang, Cheng-Mei Zhang, Zhao-Peng Liu
There are great potential in the development of selective HDAC6 inhibitors for the treatment of infectious diseases, neoplasms, endocrine diseases, and other diseases associated with HDAC6 activity. Areas covered: The application claims 1,3,4-oxadiazole sulfamide derivatives as selective HDAC6 inhibitors for the treatment of infectious diseases, neoplasms, endocrine, nutritional, and metabolic diseases; mental and behavioral disorders; neurological diseases; diseases of the eye and adnexa; cardiovascular diseases; respiratory diseases; digestive diseases; diseases of the skin and subcutaneous tissue; disease of the musculoskeletal system and connective tissue; or congenital malformations, deformations and chromosomal abnormalities...
August 2018: Expert Opinion on Therapeutic Patents
Lei Zhang, Yuan Zhang, Yanfang Zhao, Yu Wang, Han Ding, Sheng Xue, Peifeng Li
Coronary artery disease (CAD) contributes to a huge number of human death worldwide. The early diagnosis can arrest the development of CAD and effectively lower the mortality rate. Recently, circulating miRNAs emerged as CAD biomarkers. Area covered: Many efforts were paid to explore early diagnostic biomarkers of CAD. Some proteins have been used as diagnostic golden standard. However, the diagnostic and prognostic value of them is limited. MicroRNAs (miRNAs), a class of small noncoding RNAs, have been illustrated to regulate gene expression...
August 2018: Expert Opinion on Therapeutic Patents
(no author information available yet)
No abstract text is available yet for this article.
August 2018: Expert Opinion on Therapeutic Patents
Rodrigo Ayres de Oliveira, Iolanda M Fierro
Rheumatoid arthritis (RA) is a chronic autoimmune disease characterized by an inflammatory process, with a global prevalence ranging from 0.3% to 1%. The overall cost of RA drugs is estimated in $20 billion worldwide and projected to grow to $36 billion by 2021. The current RA treatment strategy consists of the aggressive therapy directed to specific targets, after diagnostic confirmation and the stepped therapy directed by the stage of the disease, aiming at the clinical remission. Conventional (methotrexate, sulfasalazine, leflunomide) and biological (infliximab, adalimumab, tocilizumab) disease-modifying antirheumatic drugs may fail, produce only partial responses, or unwanted side effects, and consequently new antirheumatic drugs are being developed to overcome these limitations...
August 2018: Expert Opinion on Therapeutic Patents
Cristina Possas, Adelaide Maria de Souza Antunes, Flavia Maria Lins Mendes, Valdiléa Veloso, Reinaldo Menezes Martins, Akira Homma
This article provides a global overview of patent deposits for broadly neutralizing antibodies (bNAbs), which have emerged as a key strategy for HIV cure and future HIV vaccines. Scientific and technological barriers to the discovery of an effective HIV vaccine in the last 40 years have raised concerns on the potential for relevant advances in this area. Nevertheless, recent breakthrough studies have identified novel immune pathways for new innovative HIV vaccine and HIV cure strategies. Areas covered: In our patent study, we have identified in a global scale, in the last decade, a sharp increase in the number of bNAbs' patent deposits related to HIV prevention and treatment strategies, reaching 90 bNAbs in 2017, protected by 184 different patent deposits...
July 2018: Expert Opinion on Therapeutic Patents
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