Dipeptidyl peptidase IV inhibitors as a potential target for diabetes: patent review (2015-2018).

abstract：INTRODUCTION:Aldose reductase (ALR2) is both the key enzyme of the polyol pathway, whose activation under hyperglycemic conditions leads to the development of chronic diabetic complications, and the crucial promoter of inflammatory and cytotoxic conditions, even under a normoglycemic status. Accordingly, it represents ...

journal_title：Expert opinion on therapeutic patents

authors： Quattrini L,La Motta C

更新日期：2019-03-01 00:00:00

abstract：INTRODUCTION:The N-acylhydrazone (NAH) moiety has been characterized as a privileged structure, capable of providing ligands points for more than one type of bioreceptor. Modifications of the subunits bonded to its acyl and imine functions resulted in several derivatives, which modulate a great diversity of molecular t...

journal_title：Expert opinion on therapeutic patents

authors： Maia Rdo C,Tesch R,Fraga CA

更新日期：2014-11-01 00:00:00

abstract：INTRODUCTION:Transglutaminases (TGases) are a class of enzymes that play multifunctional roles. Their protein-crosslinking activity has been linked to fibrosis and Huntington's disease, their glutamine deamidation activity has been related to celiac disease and their GTP-binding activity has been implicated in cancer. ...

journal_title：Expert opinion on therapeutic patents

authors： Keillor JW,Apperley KY

更新日期：2016-01-01 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: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: 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: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: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：BACKGROUND:The application (US20100233143) is in the field of embryonic stems cells (ESCs) and the generation of ESCs from parthenogenetically activated human oocytes. OBJECTIVE:It aims at determining optimal conditions for parthenogenetically activating human oocytes. METHODS:Oocytes isolated from female donors were...

journal_title：Expert opinion on therapeutic patents

authors： Taupin P

更新日期：2011-08-01 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

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: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: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：: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：:Diabetes mellitus is a major threat to global public health that requires long-term medical attention. In view of the potentially devastating effects of diabetes on ocular health, it highlights the urgent need of therapeutic drugs for the prevention and treatment of the diabetic complications. The patent described in ...

journal_title：Expert opinion on therapeutic patents

authors： Hao X,Han Z,Zhu C

更新日期：2016-06-01 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 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: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：BACKGROUND:Severe acute respiratory syndrome (SARS) coronavirus emerged fleetingly in the winter of 2002 and again in the winter of 2003, resulting in the infection of ~8,000 people and the death of ~800. The identification of the putative natural reservoir suggests that a re-emergence is possible. The functions of man...

journal_title：Expert opinion on therapeutic patents

authors： Tong TR

更新日期：2009-03-01 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：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: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: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: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：: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: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: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:PROTACs represent a novel class of heterobifunctional molecules that simultaneously bind to a target protein and to an E3 ligase complex, resulting in the transfer of ubiquitin and initiating a process ultimately causing the proteasomal degradation of the target protein. This mechanism of action imbues PRO...

journal_title：Expert opinion on therapeutic patents

authors： Benowitz AB,Jones KL,Harling JD

更新日期：2021-01-01 00:00:00