ATP-competitive DNA gyrase and topoisomerase IV inhibitors as antibacterial agents.

abstract：INTRODUCTION:The use of inhibitors of HIV-1 integrase for treating HIV-1 infection has proven to be very beneficial. Raltegravir, a strand transfer inhibitor, has been approved for use both as a first-line therapy and in treatment-experienced patients. A second compound in this class, elvitegravir, is in Phase III clin...

journal_title：Expert opinion on therapeutic patents

authors： Pendri A,Meanwell NA,Peese KM,Walker MA

更新日期：2011-08-01 00:00:00

abstract：INTRODUCTION:The non-receptor tyrosine kinase, inducible tyrosine kinase (Itk), plays an important role in thymus(T)-cell signalling and the production of pro-inflammatory cytokines. Itk, and the other Tec family members, Rlk and Tec, are viewed as attractive drug targets for new agents for the treatment of autoimmune ...

journal_title：Expert opinion on therapeutic patents

authors： Norman P

更新日期：2014-09-01 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：:Muscular dystrophies (MD) are commonly characterized by progressive loss of muscle mass and function. It is hypothesized that therapeutic blockade of the TGF-β ligand myostatin, a negative regulator of muscle mass, will stimulate muscle growth and restore muscle function. Although many anti-myostatin targets are curre...

journal_title：Expert opinion on therapeutic patents

authors： Walker RG,Thompson TB

更新日期：2015-05-01 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:Neuropeptide S (NPS) is a 20-residue peptide and endogenous ligand of the NPS receptor (NPSR). This receptor was a formerly orphan GPCR whose activation increases calcium and cyclic adenosine monophosphate levels. The NPS/NPSR system is expressed in several brain regions where it controls important biologi...

journal_title：Expert opinion on therapeutic patents

authors： Ruzza C,Calò G,Di Maro S,Pacifico S,Trapella C,Salvadori S,Preti D,Guerrini R

更新日期：2017-03-01 00:00:00

abstract：:The interaction between p53 and murine double minute 2 (MDM2) provides an attractive drug target in oncology. Small molecule inhibitors of this interaction have not only provided strong evidence for blocking the protein-protein interaction, but are also extremely useful as biological probes and ultimately as novel the...

journal_title：Expert opinion on therapeutic patents

authors： Deng J,Dayam R,Neamati N

更新日期：2006-02-01 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：IMPORTANCE TO THE FIELD:Leukotrienes (LTs) are pivotal lipid mediators of inflammation and allergy and results from recent studies also suggest roles of LTs in cardiovascular diseases, cancer and osteoporosis. 5-Lipoxygenase (5-LO) catalyzes the first step in the biosynthesis of LTs from arachidonic acid, and based on ...

journal_title：Expert opinion on therapeutic patents

authors： Pergola C,Werz O

更新日期：2010-03-01 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:There has been research on anticancer strategies which focus on disrupting a single malignant protein. One of the strategies is the inhibition of one protein, heat shock protein 90 (Hsp90). There are many reasons why Hsp90 protein is targeted by anticancer agents: maintenance of cellular homeostasis in org...

journal_title：Expert opinion on therapeutic patents

authors： Kim T,Keum G,Pae AN

更新日期：2013-08-01 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:CYP, a ubiquitous superfamily of enzymes expressed in major organs in humans, plays a key role in biosynthesis of steroids and metabolism of xenobiotics. Inhibitors of these vital enzymes provide, as tools, the opportunity to gain an insight to their role in a myriad of bioactivity and to intervene as ther...

journal_title：Expert opinion on therapeutic patents

authors： Francis S,Delgoda R

更新日期：2014-06-01 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：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：:Cholesterol homeostasis maintenance is regulated by a cellular feedback system that senses cholesterol amount in cellular membranes. 3-hydroxy 3-methylglutaryl coenzyme A reductase (HMGR) plays a pivotal role in cholesterol metabolism as it is the key rate-limiting enzyme of its biosynthetic pathway; its inhibition pr...

journal_title：Expert opinion on therapeutic patents

authors： Pallottini V

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND:Diabetes is a chronic disease that occurs when the pancreas does not produce enough insulin, or when the body cannot effectively use the insulin it produces. Hyperglycemia, or raised blood sugar, is a common effect of uncontrolled diabetes and over time leads to serious damage to many of the body's systems, ...

journal_title：Expert opinion on therapeutic patents

authors： Jones RM,Leonard JN,Buzard DJ,Lehmann J

更新日期：2009-10-01 00:00:00

abstract：INTRODUCTION:Autophagy is a lysosome-dependent degradation pathway that maintains cellular homeostasis in response to a variety of cellular stresses. Accumulating reports based on animal models have indicated the importance of this catabolic program in many human pathophysiological conditions, including diabetes, neuro...

journal_title：Expert opinion on therapeutic patents

authors： Ha J,Kim J

更新日期：2016-11-01 00:00:00

abstract：:A series of 10 closely related patent applications define Theravance's approach to the development of long-acting M(3) selective antagonists for the treatment of chronic obstructive pulmonary disease. The applications illustrate a modular approach to the design of such agents, comprising a muscarinic pharmacophore att...

journal_title：Expert opinion on therapeutic patents

authors： Norman P

更新日期：2006-09-01 00:00:00

abstract：INTRODUCTION:The NF-E2-related factor-2 (Nrf2) is a critical transcription factor that regulates the expression of many phase II and antioxidant genes to maintain the homeostasis. It has many biological functions and plays a central role in the cellular defensive machinery. The abnormal regulation of Nrf2 is closely as...

journal_title：Expert opinion on therapeutic patents

authors： Sun H,Zhu J,Lin H,Gu K,Feng F

更新日期：2017-07-01 00:00:00

abstract：INTRODUCTION:Na/K-ATPase is a heterodimeric transmembrane protein that regulates neuronal signaling, ion homeostasis, muscle contraction and substrate transportation. Modulators of Na/K-ATPase inhibit Na(+)/K(+) exchange and increase cytosolic Ca(2+) to induce inotropic activity in heart failure patients. Besides produ...

journal_title：Expert opinion on therapeutic patents

authors： Wang HY,O'Doherty GA

更新日期：2012-06-01 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:In the last 10 years, nutraceuticals have grown in interest to researchers, industry, and consumers and are now familiar in the collective imagination as a tool for preventing the onset of a disease. Often nutraceuticals are confused with biologically active phytochemicals/botanicals which can have health ...

journal_title：Expert opinion on therapeutic patents

authors： Daliu P,Santini A,Novellino E

更新日期：2018-12-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Small molecule glucokinase activators (GKAs) continue to represent a potential strategy to treat type 2 diabetes (T2D). Glucokinase (GK) primarily exerts its effect through modulatory actions in pancreatic β-cells and hepatocytes. It couples insulin secretion in the pancreas with plasma glucose ...

journal_title：Expert opinion on therapeutic patents

authors： Sarabu R,Berthel SJ,Kester RF,Tilley JW

更新日期：2011-01-01 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：IMPORTANCE OF THE FIELD:Aberrant activation of signal transducer and activator of transcription (Stat) 3, a member of the STAT family of proteins, is prevalent in numerous human cancers and is now widely recognized as a critical molecular abnormality and a master regulator of tumor processes. Thus, the identification o...

journal_title：Expert opinion on therapeutic patents

authors： Page BD,Ball DP,Gunning PT

更新日期：2011-01-01 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:Quantitative Structure-Activity Relationship (QSAR) models are becoming one of the most interesting fields for developing therapeutics and therapeutics related patents. At present, QSAR methodologies comprise a series of possibilities, including joining forces with machine learning methods and increasing e...

journal_title：Expert opinion on therapeutic patents

authors： Halder AK,Moura AS,Cordeiro MNDS

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