Radiation countermeasure agents: an update (2011-2014).

abstract：INTRODUCTION:Caffeic acid (CA) is broadly distributed in several species of the plant kingdom and is widely consumed in human diet. CA and derivatives have been extensively studied in the past years, which unveiled a broad spectrum of biological activities and potential therapeutic applications. As a result, there has ...

journal_title：Expert opinion on therapeutic patents

authors： Silva T,Oliveira C,Borges F

更新日期：2014-11-01 00:00:00

abstract：INTRODUCTION:Hypertension represents a substantial cardiovascular risk factor. Among anti-hypertensive drugs, diuretics play an important role. Nevertheless, they present adverse effects such as hypokalemia or hyperkalemia. In this panorama, inhibitors of the renal outer medullary potassium (ROMK) channels are emerging...

journal_title：Expert opinion on therapeutic patents

authors： Martelli A,Testai L,Breschi MC,Calderone V

更新日期：2015-01-01 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：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:Inhibitors of programmed cell death 1 (PD-1) and its ligands are producing a paradigm shift in cancer treatment. The promising clinical outcomes and a multi-billion dollar market have prompted active research and development and resulted in relentless patent protection. However, the global patent landscape...

journal_title：Expert opinion on therapeutic patents

authors： Kong X,Zhang Q,Lai Y,Hu H,Chen X,Hu Y

更新日期：2018-01-01 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：: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

abstract：:In recent years, the involvement of the Hedgehog (Hh) signaling pathway in various human diseases and dysfunctions has been clearly demonstrated. Smoothened (Smo), one of the upstream signal transducers, has been the most druggable target of the Hh pathway. However, the emergence of resistance to Smo inhibitors and th...

journal_title：Expert opinion on therapeutic patents

authors： Manetti F,Petricci E

更新日期：2016-01-01 00:00:00

abstract：INTRODUCTION:Bitopic M ligands, that is, ligands that interact both with the ortho- and allosteric binding sites of the M receptor subtypes, hold great potential as novel selective for muscarinic acetylcholine (M) ligands for several therapeutic applications. Areas covered: The patent application describes a set of com...

journal_title：Expert opinion on therapeutic patents

authors： Holzgrabe U,Decker M

更新日期：2017-02-01 00:00:00

abstract：INTRODUCTION:Indazoles are heterocyclic moieties rarely found in nature. They are nitrogen containing chemical compounds composed of a pyrazole ring condensed with a benzene ring. Various indazole derivatives have been described with a wide variety of biological activities. This has aroused great interest in the develo...

journal_title：Expert opinion on therapeutic patents

authors： Denya I,Malan SF,Joubert J

更新日期：2018-06-01 00:00:00

abstract：INTRODUCTION:Therapeutic antibodies have grown to become an important product class within the biopharmaceutical market. A prerequisite to their commercialization is adequate patent protection. Disclosure requirements and the types of claims available in different jurisdictions can impact the scope of protection availa...

journal_title：Expert opinion on therapeutic patents

authors： De Luca C,Trifonova A

更新日期：2017-08-01 00:00:00

abstract：INTRODUCTION: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 c...

journal_title：Expert opinion on therapeutic patents

authors： Peng FW,Liu DK,Zhang QW,Xu YG,Shi L

更新日期：2017-09-01 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: 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:With the introduction of mucoadhesion in 1980, pharmaceutical researchers have gained interest in mucoadhesive compositions. This interest has led to the development of mucoadhesive drug delivery systems aiming (I) to target a specific tissue, (II) to overcome barriers to absorption as well as (III) to con...

journal_title：Expert opinion on therapeutic patents

authors： Laffleur F

更新日期：2016-01-01 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：: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：:Neurostatin, a natural glycosphingolipid inhibitor of astroblast and astrocytoma division, present in mammalian brain, is the modified ganglioside O-acetylated GD1b. It is cytostatic for rat astroblasts, C6 glioma cells and various human astrocytoma lines grades III and IV, with median inhibitory dose values ranging 1...

journal_title：Expert opinion on therapeutic patents

authors： Nieto-Sampedro M,Doncel-Pérez E,Fernández-Mayoralas A

更新日期：2004-04-01 00:00:00

abstract：INTRODUCTION:Dendrimers were widely used in cancer diagnosis and therapy during the past decade. The surface functionalities allow bioactive molecules such as imaging probes, therapeutic compounds, targeting ligands to be present on dendrimer surface in a multivalent fashion. In addition, the interior pockets as well a...

journal_title：Expert opinion on therapeutic patents

authors： Cai X,Hu J,Xiao J,Cheng Y

更新日期：2013-04-01 00:00:00

abstract：INTRODUCTION:New drug formulations against hypertension have a vital role in the quality of human life, as this risk factor for cardiovascular disease can be life threatening. A modern life style characterized by less exercise, smoking, drinking and poor diet has increased the risk of developing hypertension, the so-ca...

journal_title：Expert opinion on therapeutic patents

authors： Kellici TF,Liapakis G,Tzakos AG,Mavromoustakos T

更新日期：2015-01-01 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：:The application is in the field of adult neurogenesis and its therapeutic potential. It aims to characterize the activity of apigenin and related compounds on adult neurogenesis in vivo and in vitro. Apigenin and related compounds are derivatives used in food products. They were administered intraperitoneally and oral...

journal_title：Expert opinion on therapeutic patents

authors： Taupin P

更新日期：2009-04-01 00:00:00

abstract：INTRODUCTION:Antimicrobial peptides (AMPs) represent the large group of endogenous compounds widely distributed in nature. Due to their broad spectrum of antibiotic activity, as well as anti-inflammatory and immunomodulatory properties, AMPs became a model for the discovery of novel antimicrobial drugs that could answe...

journal_title：Expert opinion on therapeutic patents

authors： Kosikowska P,Lesner A

更新日期：2016-06-01 00:00:00

abstract：INTRODUCTION:The bacterial topoisomerases DNA gyrase and topoisomerase IV are validated targets for development of novel antibacterial agents. Fluoroquinolones inhibit the catalytic GyrA and/or ParC(GrlA) subunit and have been commonly used, although these have toxicity liabilities that restrict their use. The ATPase G...

journal_title：Expert opinion on therapeutic patents

authors： Durcik M,Tomašič T,Zidar N,Zega A,Kikelj D,Mašič LP,Ilaš J

更新日期：2019-03-01 00:00:00

abstract：:Increasing pharmacological studies have demonstrated that organic cation transporter 3 (OCT3) plays an important role in controlling the extracellular concentrations of released monoamine neurotransmitter, suggesting that OCT3 might be a promising target in the treatment of depression. As a consequence, compounds show...

journal_title：Expert opinion on therapeutic patents

authors： Hu T,Wang L,Pan X,Qi H

更新日期：2016-08-01 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：INTRODUCTION:Monoacylglycerol lipase (MAGL) belongs to the endocannabinoid system and is responsible for the inactivation of endocannabinoid 2-arachidonoylglycerol. Importantly, it was found that MAGL degradation of lipids in cancer cells enhances the availability of free fatty acids for new cellular membrane formation...

journal_title：Expert opinion on therapeutic patents

authors： Bononi G,Poli G,Rizzolio F,Tuccinardi T,Macchia M,Minutolo F,Granchi C

更新日期：2020-11-01 00:00:00

abstract：INTRODUCTION:Over the past three years numerous patents and patent applications have been published relating to scientific advances in the use of the green tea polyphenol epigallocatechin gallate (EGCG) (the most abundant, and bioactive compound in green tea) and its analogs as anticancer agents. EGCG affects multiple ...

journal_title：Expert opinion on therapeutic patents

authors： Landis-Piwowar K,Chen D,Foldes R,Chan TH,Dou QP

更新日期：2013-02-01 00:00:00

abstract：INTRODUCTION:Leishmaniasis is a neglected tropical disease caused by protozoa of the genus Leishmania. Worldwide, approximately 1.5-2 million new cases of leishmaniasis and 20,000-30,000 deaths occurs each year. Effective treatment for all forms of leishmaniasis have numerous adverse effects contributing to poor adhere...

journal_title：Expert opinion on therapeutic patents

authors： Barbosa Gomes de Carvalho YM,Shanmugam S,Batista MS,Serafini MR,Araújo AAS,Quintans Júnior LJ

更新日期：2020-08-01 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