Thrombin receptor (PAR-1) antagonists as novel antithrombotic agents.

abstract：INTRODUCTION:Antimicrobial peptides (AMPs) represent the large group of endogenous compounds widely distributed in nature. Due to their broad spectrum of antibiotic activity, as well as anti-inflammatory and immunomodulatory properties, AMPs became a model for the discovery of novel antimicrobial drugs that could answe...

journal_title：Expert opinion on therapeutic patents

authors： Kosikowska P,Lesner A

更新日期：2016-06-01 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:Inhibitors of the renin angiotensin aldosterone system (RAAS) represent some of the most widely prescribed, successful and well-tolerated therapeutics of recent times and are of proven worth in the management/prevention of cardiovascular disease and diabetic nephropathy. However, as knowledge has grown about...

journal_title：Expert opinion on therapeutic patents

authors： Laight DW

更新日期：2009-06-01 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: 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: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

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：: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:Angiogenesis is an important component of certain normal physiological processes, but aberrant angiogenesis contributes to some pathological disorders and in particular to tumor growth. Activation of vascular endothelial growth factor receptor-2 (VEGFR-2) by vascular endothelial growth factor (VEGF) is a c...

journal_title：Expert opinion on therapeutic patents

authors： Peng FW,Liu DK,Zhang QW,Xu YG,Shi L

更新日期：2017-09-01 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:Melatonin is a neurohormone involved in the regulation of circadian rhythms, with potent antioxidant activity. It has a wide functional repertoire, with effects almost on all tissues and organs. It is mainly used as a dietary supplement for sleep regulation and re-synchronization of disrupted circadian rhy...

journal_title：Expert opinion on therapeutic patents

authors： Rivara S,Pala D,Bedini A,Spadoni G

更新日期：2015-04-01 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: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：: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: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：BACKGROUND:The application (WO2010075475) is involved in the diagnosis of angiogenesis-dependent diseases related with the soluble FMS-like tyrosine kinase-1 (sFlt-1) biomarker. OBJECTIVE:It aims to identify, characterize and produce antibodies raised against sFlt-1 for the diagnosis of preeclampsia as well as other c...

journal_title：Expert opinion on therapeutic patents

authors： Boyaud F,Inguimbert N

更新日期：2011-06-01 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：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: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：: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: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: 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:Leishmaniasis is a neglected tropical disease caused by protozoa of the genus Leishmania. Worldwide, approximately 1.5-2 million new cases of leishmaniasis and 20,000-30,000 deaths occurs each year. Effective treatment for all forms of leishmaniasis have numerous adverse effects contributing to poor adhere...

journal_title：Expert opinion on therapeutic patents

authors： Barbosa Gomes de Carvalho YM,Shanmugam S,Batista MS,Serafini MR,Araújo AAS,Quintans Júnior LJ

更新日期：2020-08-01 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

abstract：:This article evaluates a patent application from Solvay Pharmaceuticals, which claims spiro azepane-oxazolidinones as novel blockers of the voltage-gated potassium channel Kv1.3 for the treatment of diabetes, psoriasis, obesity, transplant rejection and T-cell mediated autoimmune diseases such as rheumatoid arthritis ...

journal_title：Expert opinion on therapeutic patents

authors： Wulff H

更新日期：2010-12-01 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：: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：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：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: 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