5-Lipoxygenase inhibitors: a review of recent developments and patents.

abstract：INTRODUCTION:Almost half the global population is estimated to be at risk of contracting dengue infection. Of the 400 million infections estimated to occur annually, 4 million can be potentially life-threatening leading to vascular leakage and shock. The only treatment available to severe dengue patients is fluid repla...

journal_title：Expert opinion on therapeutic patents

authors： Beesetti H,Khanna N,Swaminathan S

更新日期：2014-11-01 00:00:00

abstract：BACKGROUND:The application is in the field of neural stem cells (NSCs) and cellular therapy. OBJECTIVE:It aims at establishing conditions for the isolation and propagation of neural progenitor and stem cells from human fetal tissue, with high rate of growth and high yields of differentiation into the neuronal, astrogl...

journal_title：Expert opinion on therapeutic patents

authors： Taupin P

更新日期：2009-03-01 00:00:00

abstract：BACKGROUND:Severe acute respiratory syndrome (SARS) coronavirus emerged fleetingly in the winter of 2002 and again in the winter of 2003, resulting in the infection of ~8,000 people and the death of ~800. The identification of the putative natural reservoir suggests that a re-emergence is possible. The functions of man...

journal_title：Expert opinion on therapeutic patents

authors： Tong TR

更新日期：2009-03-01 00:00:00

abstract：INTRODUCTION:The oxadiazoles represent a class of five-membered heterocyclic compounds which are of considerable interest in different areas of medicinal chemistry and drug discovery. Oxadiazoles can exist in different regioisomeric forms and employ in various agents with a broad range of biological activities. This re...

journal_title：Expert opinion on therapeutic patents

authors： Zarghi A,Hajimahdi Z

更新日期：2013-09-01 00:00:00

abstract：INTRODUCTION:Benzoxaborole is a versatile boron-heterocyclic scaffold which has found in the last 10 years a broad spectrum of applications in medicinal chemistry, due to its physicochemical and drug-like properties. Use of benzoxaborole moiety in the design of compounds led to the discovery of new classes of anti-bact...

journal_title：Expert opinion on therapeutic patents

authors： Nocentini A,Supuran CT,Winum JY

更新日期：2018-06-01 00:00:00

abstract：INTRODUCTION:Around 3% of the world population is infected with HCV, with 3 - 4 million newly infected subjects added to this reservoir every year. At least 10% of these people will develop liver cirrhosis or cancer over time, while no approved vaccine against HCV infection is available to date. AREAS COVERED:This pap...

journal_title：Expert opinion on therapeutic patents

authors： Roohvand F,Kossari N

更新日期：2011-12-01 00:00:00

abstract：:In the upcoming case of Teva Pharmaceuticals v. Sandoz, the U.S. Supreme Court will address how much deference the appellate court should afford to a trial court's claim construction ruling. The effect of this decision will be far-reaching, as how claims are construed can determine whether a patent is infringed or not...

journal_title：Expert opinion on therapeutic patents

authors： Fogel LE,Ray CJ

更新日期：2015-01-01 00:00:00

abstract：INTRODUCTION:The alpha isoform of the class 1A family of phosphatidylinositol 3-kinases (PI3Kα) has been extensively studied and exploited as a target for cancer drugs. A large number of compounds, from a wide variety of structural scaffolds, are in development. There is an ongoing debate about the desirability for sel...

journal_title：Expert opinion on therapeutic patents

authors： Denny WA

更新日期：2013-07-01 00:00:00

abstract：INTRODUCTION:The appetite stimulating effects of melanin-concentrating hormone (MCH) continues to be of high interest, and there is substantial support to investigate the use of MCH 1-receptor antagonists for the treatment of obesity. Other areas of potential use for MCH 1-receptor antagonists include depression and an...

journal_title：Expert opinion on therapeutic patents

authors： Johansson A

更新日期：2011-06-01 00:00:00

abstract：INTRODUCTION:The potential therapeutic applications of thyrotropin-releasing hormone (TRH) have attracted attention, based on its broad-spectrum neuropharmacological action rather than its endocrine properties. These central nervous system (CNS)-mediated effects provide the rationale for use of TRH and its analogs in t...

journal_title：Expert opinion on therapeutic patents

authors： Khomane KS,Meena CL,Jain R,Bansal AK

更新日期：2011-11-01 00:00:00

abstract：INTRODUCTION:TANK-binding kinase 1 (TBK1) is a noncanonical IκB kinase family member that regulates the innate immune response. Misregulation of TBK1 activity can promote inflammatory disorders and oncogenesis; therefore, TBK1 inhibitors are considered a promising therapy for inflammation and cancer. AREAS COVERED:In ...

journal_title：Expert opinion on therapeutic patents

authors： Yu T,Yang Y,Yin DQ,Hong S,Son YJ,Kim JH,Cho JY

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND:For > 20 years, pharmaceutical companies and academic centers have been developing bradykinin antagonists. The patent literature on these molecules (up to and including 2004) has been analyzed previously in this journal in two review articles. OBJECTIVE:The aim of this review is to provide an update (from 2...

journal_title：Expert opinion on therapeutic patents

authors： Fincham CI,Bressan A,Paris M,Rossi C,Fattori D

更新日期：2009-07-01 00:00:00

abstract：INTRODUCTION:Amino acid depletion in the blood serum is currently being exploited and explored for therapies in tumors or viral infections that are auxotrophic for a certain amino acid or have a metabolic defect and cannot produce it. The success of these treatments is because normal cells remain unaltered since they a...

journal_title：Expert opinion on therapeutic patents

authors： Fernandes HS,Silva Teixeira CS,Fernandes PA,Ramos MJ,Cerqueira NM

更新日期：2017-03-01 00:00:00

abstract：INTRODUCTION:Piperine is a simple and pungent alkaloid found in the seeds of black pepper (Piper nigrum). Following its isolation and full characterization, the biological properties of piperine have been extensively studied, and piperine-like derivatives have shown an interesting range of pharmacological activities. I...

journal_title：Expert opinion on therapeutic patents

authors： Chavarria D,Silva T,Magalhães e Silva D,Remião F,Borges F

更新日期：2016-01-01 00:00:00

abstract：INTRODUCTION:Since exendin-4 (exenatide) was approved for diabetes therapy in 2005, several exendin analogs have been developed for the treatment of type 2 diabetes mellitus. As exenatide is a relatively short-acting injectable agent, major approaches have focused on developing long-acting exendin analogs to improve pa...

journal_title：Expert opinion on therapeutic patents

authors： Park EJ,Lim SM,Lee KC,Na DH

更新日期：2016-07-01 00:00:00

abstract：INTRODUCTION:Due to the role of bradykinin B1 receptor (B1R) in pain and inflammation, B1R antagonists have been suggested as promising drug candidates in chronic pain states. The first disclosed B1R antagonists were peptidomimetics, however, during the last few years, novel chemotypes with improved pharmacodynamic and...

journal_title：Expert opinion on therapeutic patents

authors： Bozó É,Éles J,Keserű GM

更新日期：2012-12-01 00:00:00

abstract：:Merck recently signed an agreement with The Medicines Patent Pool (MPP) to license intellectual property relating to pediatric formulations of its integrase HIV drug, raltegravir (Ral) (the 'Agreement'). The Agreement is alleged to clear the way for cheaper formulations for use in developing and some middle income cou...

journal_title：Expert opinion on therapeutic patents

authors： De Luca C

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND:Hydrogen sulfide (H(2)S) and carbon monoxide (CO) are endogenously produced gaseous autacoids that regulate a number of physiological processes, including the inflammatory response, cell death and proliferation, neural transmission and smooth muscle tone. OBJECTIVE/METHODS:The current review aims to provide...

journal_title：Expert opinion on therapeutic patents

authors： Bannenberg GL,Vieira HL

更新日期：2009-05-01 00:00:00

abstract：:Introduction: Pharmacotherapy is limited by the inefficient drug targeting of non-healthy cells/tissues. In this pharmacological landscape, liposomes are contributing to the impulse given by Nanotechnology to optimize drug therapy. Areas covered: The analysis of the state-of-the-art in liposomal formulations for drug ...

journal_title：Expert opinion on therapeutic patents

authors： El-Hammadi MM,Arias JL

更新日期：2019-11-01 00:00:00

abstract：:Introduction: Discoidin domain receptor 1 (DDR1) is a collagen-activated receptor tyrosine kinase. Upon collagen binding, DDR1 undergoes tyrosine autophosphorylation, which consequently triggers downstream genetic and cellular pathways and plays critical roles in the regulation of cellular morphogenesis, differentiati...

journal_title：Expert opinion on therapeutic patents

authors： Guo J,Zhang Z,Ding K

更新日期：2020-05-01 00:00:00

abstract：INTRODUCTION:2,5-Diketopiperazines (DKPs) are cyclic dipeptides from two amino acids with or without further structural modifications in DKP nucleus. These DKPs demonstrated attractive bioactive diversity and potential in drug discovery. AREAS COVERED:This review summarized those bioactive DKPs in patents, and provide...

journal_title：Expert opinion on therapeutic patents

authors： Wang Y,Wang P,Ma H,Zhu W

更新日期：2013-11-01 00:00:00

abstract：:Introduction: TIM3 and PD-1 are checkpoint inhibitors in cancer that coordinate the downregulation of the proliferation of antigen-specific lymphocytes. There is a great need to discover and develop new therapies focused on inhibiting the action of TIM3 and PD-1 and consequently improving the immune response in the va...

journal_title：Expert opinion on therapeutic patents

authors： Herrera-Camacho I,Anaya-Ruiz M,Perez-Santos M,Millán-Pérez Peña L,Bandala C,Landeta G

更新日期：2019-08-01 00:00:00

abstract：INTRODUCTION:The cyclic nucleotides cAMP and cGMP are ubiquitous intracellular second messengers regulating a large variety of biological processes. The intracellular concentration of these biologically relevant molecules is modulated by the activity of phosphodiesterases (PDEs), a class of enzymes that is grouped in 1...

journal_title：Expert opinion on therapeutic patents

authors： Trabanco AA,Buijnsters P,Rombouts FJ

更新日期：2016-08-01 00:00:00

abstract：INTRODUCTION:Tryptase is one of the main serine-proteinases located in the secretory granules of mast cells, and is released through degranulation, which is involved in the pathogenesis of allergic inflammatory disease, cardiovascular diseases, lung fibrosis and tumor. Therefore, inhibitors targeting tryptase may repre...

journal_title：Expert opinion on therapeutic patents

authors： Ni WW,Cao MD,Huang W,Meng L,Wei JF

更新日期：2017-08-01 00:00:00

abstract：BACKGROUND:Not only hypercholesterolemia, but also low levels of high-density lipoprotein cholesterol is a critical risk factor for atherosclerosis-related disease. Therefore, there has been great interest in identifying effective and selective cholesteryl ester transfer protein (CETP) inhibitors that can raise high-de...

journal_title：Expert opinion on therapeutic patents

authors： Shinkai H

更新日期：2009-09-01 00:00:00

abstract：BACKGROUND:The application (US20100233143) is in the field of embryonic stems cells (ESCs) and the generation of ESCs from parthenogenetically activated human oocytes. OBJECTIVE:It aims at determining optimal conditions for parthenogenetically activating human oocytes. METHODS:Oocytes isolated from female donors were...

journal_title：Expert opinion on therapeutic patents

authors： Taupin P

更新日期：2011-08-01 00:00:00

abstract：:The concept of activation of glucokinase (encoded by the Gck gene) as a potential therapy for type 2 diabetes has been explored by several pharmaceutical companies. Small-molecule Gck activators (GKAs) were found to be effective at increasing glucose disposal by hepatocytes and lowering blood glucose in animal models ...

journal_title：Expert opinion on therapeutic patents

authors： Agius L

更新日期：2014-11-01 00:00:00

abstract：:Small-molecule ligands, amenable to positron emission tomography (PET) imaging of different types of neurodegenerative disease-associated amyloid deposits in the CNS of living patients, hold considerable promise for diagnostic purposes, as well as for monitoring disease progression and the effectiveness of treatments....

journal_title：Expert opinion on therapeutic patents

authors： Ballatore C,Smith AB 3rd,Lee VM,Trojanowski JQ,Brunden KR

更新日期：2014-03-01 00:00:00

abstract：:Introduction: The greater interest in TAAR1-mediated potential for the treatment of different pathologies, especially those related to CNS disorders, has given a considerable boost to the search for developing TAAR1-selective small molecules.Areas covered: During the last decade, the medicinal chemistry efforts have a...

journal_title：Expert opinion on therapeutic patents

authors： Tonelli M,Cichero E

更新日期：2020-02-01 00:00:00

abstract：:The patent claims peptidic/nonpeptidic inhibitors of the ghrelin receptor, the growth hormone secretagogue receptor (GHSR) 1A. Among these compounds, it was disclosed that the addition in some compounds of a GlyMetAla tripeptide at the N-terminus of the ghrelin peptide agonists converts them into ghrelin receptor anta...

journal_title：Expert opinion on therapeutic patents

authors： Costantino L

更新日期：2012-06-01 00:00:00