Antimicrobial peptides (AMPs) as drug candidates: a patent review (2003-2015).

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: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: 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：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:Hepatitis B disease is caused by the hepatitis B virus (HBV), which is a DNA virus that belongs to the Hepadnaviridae family. It is a considerable health burden, with 257 million active cases globally. Long-standing infection may create a fundamental cause of liver disease and chronic infections, including...

journal_title：Expert opinion on therapeutic patents

authors： Wei F,Kang D,Cherukupalli S,Zalloum WA,Zhang T,Liu X,Zhan P

更新日期：2020-09-01 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：: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：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: 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: 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：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: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：INTRODUCTION:Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that localizes at sites of cell adhesion to the extracellular matrix (ECM) and mediates signalling events downstream of integrin engagement of the ECM. FAK is known to regulate cell survival, proliferation and migration. AREAS COVERED:FAK expre...

journal_title：Expert opinion on therapeutic patents

authors： Lv PC,Jiang AQ,Zhang WM,Zhu HL

更新日期：2018-02-01 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：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: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:Retinoid X receptors (RXRs) are nuclear receptors that act as ligand-dependent transcription factors. RXRs function as homodimers or as heterodimers with other nuclear receptors, such as retinoic acid receptors, PPARs, liver X receptors, farnesoid X receptor, vitamin D receptor or thyroid hormone receptors...

journal_title：Expert opinion on therapeutic patents

authors： Yamada S,Kakuta H

更新日期：2014-04-01 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: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：: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: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：: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：: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 orexin system consists of two G-protein-coupled receptors, orexin 1 and orexin 2 and two endogenous ligands, orexin A and orexin B . It is evolutionarily highly conserved. It is involved in the promotion of wakefulness as well as in anxiety and addictive disorders. In addition, its activation via the O...

journal_title：Expert opinion on therapeutic patents

authors： Boss C,Roch C

更新日期：2017-10-01 00:00:00

abstract：:Since the discovery of MK-0518 (raltegravir, the first FDA-approved integrase inhibitor) in October 2007, Merck Co. researchers have continued to patent original new heterocycles related to raltegravir as powerful strand transfer inhibitors. Among the most recent patented works hexahydrodiazocino-naphthyridinetriones ...

journal_title：Expert opinion on therapeutic patents

authors： Cotelle P

更新日期：2009-01-01 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：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：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：: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: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