Formyl peptide receptor modulators: a patent review and potential applications for inflammatory diseases (2012-2015).

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：: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:Biotech patents are facing increasingly stern challenges. The patent statue holds that a multi-step method patent is not directly infringed unless all steps are carried out and attributed to a single entity. When separate steps are performed jointly by two or more parties, those parties are liable for divi...

journal_title：Expert opinion on therapeutic patents

authors： Chen FC

更新日期：2017-04-01 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：:Novel 1-anilino-4-phenylphthalazine derivatives, compositions containing them, and their use as JAK1 inhibitors and for the treatment of cancer, inflammatory and autoimmune diseases are claimed. This represents a novel scaffold for JAK inhibitors and is highly distinct from the JAK1 inhibitors previously described, al...

journal_title：Expert opinion on therapeutic patents

authors： Norman P

更新日期：2012-09-01 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: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: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: 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: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：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：BACKGROUND:The family of G-protein-coupled receptors (GPCRs) serves as the target for almost a third of currently marketed drugs and provides the predominant mechanism through which extracellular factors transmit signals to the cell. GPCRs have been proved to be good therapeutic targets for metabolic disorders. In rece...

journal_title：Expert opinion on therapeutic patents

authors： Bharate SB,Nemmani KV,Vishwakarma RA

更新日期：2009-02-01 00:00:00

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: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:Despite significant scientific advances over the past 60 years towards the development of a safe, nontoxic and effective radiation countermeasure for the acute radiation syndrome (ARS), no drug has been approved by the US FDA. A radiation countermeasure to protect the population at large from the effects o...

journal_title：Expert opinion on therapeutic patents

authors： Singh VK,Newman VL,Romaine PL,Wise SY,Seed TM

更新日期：2014-11-01 00:00:00

abstract：INTRODUCTION:Na/K-ATPase is a heterodimeric transmembrane protein that regulates neuronal signaling, ion homeostasis, muscle contraction and substrate transportation. Modulators of Na/K-ATPase inhibit Na(+)/K(+) exchange and increase cytosolic Ca(2+) to induce inotropic activity in heart failure patients. Besides produ...

journal_title：Expert opinion on therapeutic patents

authors： Wang HY,O'Doherty GA

更新日期：2012-06-01 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：: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：INTRODUCTION:Monoacylglycerol lipase (MAGL) belongs to the endocannabinoid system and is responsible for the inactivation of endocannabinoid 2-arachidonoylglycerol. Importantly, it was found that MAGL degradation of lipids in cancer cells enhances the availability of free fatty acids for new cellular membrane formation...

journal_title：Expert opinion on therapeutic patents

authors： Bononi G,Poli G,Rizzolio F,Tuccinardi T,Macchia M,Minutolo F,Granchi C

更新日期：2020-11-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:c-Met kinase is the receptor for hepatocyte growth factor. Primarily expressed on epithelial and mesenchymal cells its normal function is associated with wound healing, liver regeneration and embryo development. However, dysregulation of c-Met through overexpression, gene amplification, mutation...

journal_title：Expert opinion on therapeutic patents

authors： Porter J

更新日期：2010-02-01 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: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：: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:The non-receptor tyrosine kinase, inducible tyrosine kinase (Itk), plays an important role in thymus(T)-cell signalling and the production of pro-inflammatory cytokines. Itk, and the other Tec family members, Rlk and Tec, are viewed as attractive drug targets for new agents for the treatment of autoimmune ...

journal_title：Expert opinion on therapeutic patents

authors： Norman P

更新日期：2014-09-01 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：:A small series of aryl(1-arylamino)ethyl,1,5-naphthyridine derivatives that selectively inhibit PI3Kδ was prepared. The compounds are claimed to be useful in the treatment of cancer, inflammatory and autoimmune diseases. The compounds represent further variations around a structural motif explored in a number of previ...

journal_title：Expert opinion on therapeutic patents

authors： Norman P

更新日期：2011-11-01 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：: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: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: 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