Sulfonamide inhibitors: a patent review 2013-present.

abstract：INTRODUCTION:Xanthine oxidase (XO) is a molybdoflavoprotein that catalyzes the oxidative hydroxylation of purines to produce uric acid and reactive oxygen species. These reaction products can cause severe disease conditions like hyperuricemia which makes XO enzyme, an important therapeutic target in diseases like gout....

journal_title：Expert opinion on therapeutic patents

authors： Singh JV,Bedi PMS,Singh H,Sharma S

更新日期：2020-10-01 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：IMPORTANCE OF THE FIELD:Survivin is a prominent anti-apoptotic molecule expressed widely in the majority of cancers. Overexpression of survivin leads to uncontrolled cancer cell growth and drug resistance. Efficient downregulation of survivin expression and its functions can sensitise the tumour cells to various therap...

journal_title：Expert opinion on therapeutic patents

authors： Kanwar JR,Kamalapuram SK,Kanwar RK

更新日期：2010-12-01 00:00:00

abstract：INTRODUCTION:Hypoxia-inducible factor (HIF)-1α regulates the expression of genes involved in angiogenesis, cellular energy metabolism, and cell survival during cancer development. The increased expression of HIF-1α in most solid tumors is associated with poor prognoses and therapeutic outcomes. Therefore, HIF has been ...

journal_title：Expert opinion on therapeutic patents

authors： Ban HS,Uto Y,Won M,Nakamura H

更新日期：2016-01-01 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：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: 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：:In addition to its central role in haemostasis and wound healing, thrombin activates platelets and smooth muscle cells by proteolytic activation of cell surface protease-activated receptor-1 (PAR-1), which is also known as the thrombin receptor. Thrombin is the most potent activator of human platelets and, as such, a ...

journal_title：Expert opinion on therapeutic patents

authors： Chackalamannil S,Xia Y

更新日期：2006-04-01 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: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: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: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: 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:Nuclear factor (NF)-κB, as transcription factor, is linked to the expression of various genes and plays an essential role in immune and inflammatory responses. Abnormal NF-κB signaling results in human diseases, such as immune disorders, inflammation and various cancers. Therefore, regulation of NF-κB may ...

journal_title：Expert opinion on therapeutic patents

authors： Kwak JH,Jung JK,Lee H

更新日期：2011-12-01 00:00:00

abstract：INTRODUCTION:Chymase is primarily found in mast cells (MCs), fibroblasts, and vascular endothelial cells. MC chymase is released into the extracellular interstitium in response to inflammatory signals, tissue injury, and cellular stress. Among many functions, chymase is a major extravascular source for angiotensin II (...

journal_title：Expert opinion on therapeutic patents

authors： Ahmad S,Ferrario CM

更新日期：2018-11-01 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: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: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：:Introduction: The most conventional drug delivery systems exist with limitations such as drug degradation, toxicity and low bioavailability. Also, hypodermic injections can cause pain, compromising patient compliance. Due to this, transdermal drug delivery systems can minimize several problems associated with conventi...

journal_title：Expert opinion on therapeutic patents

authors： Queiroz MLB,Shanmugam S,Santos LNS,Campos CA,Santos AM,Batista MS,Araújo AAS,Serafini MR

更新日期：2020-06-01 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：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: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：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: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：:The two patent applications describe two novel compounds in the benzimidazole class of GyrB/ParE antibacterial agents and multiple phosphate prodrugs derived from these compounds. The new benzimidazole compounds have excellent antibacterial activity on Gram-positive strains. But like previous benzimidazoles, they have...

journal_title：Expert opinion on therapeutic patents

authors： Finn J

更新日期：2013-09-01 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:Following FDA approval of vorinostat in 2006, several novel HDAC inhibitors (HDACis) have entered clinical trials, and there are numerous published patent applications claiming novel HDACis which were optimized as potential drug candidates, designed for regional or systemic release, and created ...

journal_title：Expert opinion on therapeutic patents

authors： Wang H,Dymock BW

更新日期：2009-12-01 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：: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:Melanogenesis is the process of producing the melanin pigment, in which a series of chemical and enzymatic pathways are involved. Modulation at any level of this process would become an important approach in the treatment of hyper- or hypopigmentation-related diseases. Since hyperpigmentation covers import...

journal_title：Expert opinion on therapeutic patents

authors： Pillaiyar T,Manickam M,Jung SH

更新日期：2015-07-01 00:00:00