Signal transducer and activator of transcription 3 inhibitors: a patent review.

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: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：INTRODUCTION:Since the 1970s, the treatment options for asthma and chronic obstructive pulmonary disease have increasingly relied upon the use of inhaled drug formulations, generally from handheld inhaler devices. The introduction of combinations of a corticosteroid with a long-acting β2 agonist has dramatically transf...

journal_title：Expert opinion on therapeutic patents

authors： Norman P

更新日期：2015-01-01 00:00:00

abstract：INTRODUCTION:HIV/AIDS is one of the most devastating diseases in the world affecting > 40 million people worldwide. Morbidity and mortality from AIDS are significantly reduced due to the advent of highly active antiretroviral therapy (HAART). Long-term toxicity, emergence of drug resistant HIV strains and drug-drug int...

journal_title：Expert opinion on therapeutic patents

authors： Singh IP,Chauthe SK

更新日期：2011-02-01 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: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: DNA-dependent protein kinase (DNA-PK) plays a crucial role in the repair of DSBs via non-homologous end joining (NHEJ). Several DNA-PK inhibitors are being investigated for potential anticancer treatment in clinical trials. Area covered: This review aims to give an overview of patents published since 201...

journal_title：Expert opinion on therapeutic patents

authors： Hu S,Hui Z,Lirussi F,Garrido C,Ye XY,Xie T

更新日期：2020-12-21 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: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:New classes of synthetic and semi-synthetic β-glucan inhibitors have recently emerged, providing analogs that, in some cases, have been proven to have a high degree of activity against fungi, offering the prospect of alternatives to the commercially available lipopeptide/echinocandin agents caspofungin, mi...

journal_title：Expert opinion on therapeutic patents

authors： Hector RF,Bierer DE

更新日期：2011-10-01 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: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：INTRODUCTION:The Rho kinase/ROCK is critical in vital signal transduction pathways central to many essential cellular activities. Since ROCK possess multiple substrates, modulation of ROCK activity is useful for treatment of many diseases. AREAS COVERED:Significant progress has been made in the development of ROCK inh...

journal_title：Expert opinion on therapeutic patents

authors： Feng Y,LoGrasso PV

更新日期：2014-03-01 00:00:00

abstract：INTRODUCTION:The activation of leukocytes and the subsequent immune cascade play an essential role in sterile and infectious inflammation. Dysregulation of these immune responses or excess leukocyte activation can induce tissue damage, organ dysfunction and mortality. Formyl peptide receptors (FPRs) are functionally di...

journal_title：Expert opinion on therapeutic patents

authors： Tsai YF,Yang SC,Hwang TL

更新日期：2016-10-01 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: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: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：: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: 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: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：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:Dipeptidyl peptidase 4 (DPP-4) belongs to the family of serine proteases and is involved in the degradation of GLP-1 and GIP hormones, which enhance the production and release of insulin. Targeting DPP-4 inhibitors is increasingly being considered as promising paradigms to treat type 2 diabetes mellitus an...

journal_title：Expert opinion on therapeutic patents

authors： Hussain H,Abbas G,Green IR,Ali I

更新日期：2019-07-01 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 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:There is an unmet need of strategies for ex-vivo expansion of hematopoetic stem cells (HSCs) without loss of their primitive nature or stemness. We evaluate here a patent that attempts to address this need via key small molecules 1 and 40 that possess a pyrimido[4,5-b]indole core. Areas covered: (i) Discus...

journal_title：Expert opinion on therapeutic patents

authors： Agarwal S,Agarwal H,Zaware N

更新日期：2017-11-01 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: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：INTRODUCTION:Apoptosis is an important and extensively studied pathway of programmed cell death, which is central to different physiological processes. Varied pathological implications, not limited to cancer and neurodegenerative diseases, occur if a slight dysfunction happens in the intricate apoptotic pathway. Theref...

journal_title：Expert opinion on therapeutic patents

authors： Kamal A,Faazil S,Malik MS

更新日期：2014-03-01 00:00:00

abstract：INTRODUCTION:Non-nucleoside reverse transcriptase inhibitors (NNRTIs) form the backbone of antiretroviral treatment for many HIV-infected individuals. The unique antiviral activity, high specificity and low toxicity associated with this class of agents make them a frequent choice for first-line therapy. However, the ef...

journal_title：Expert opinion on therapeutic patents

authors： Zhan P,Liu X

更新日期：2011-05-01 00:00:00