TBK1 inhibitors: a review of patent literature (2011 - 2014).

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:Neuropeptide S (NPS) is a 20-residue peptide and endogenous ligand of the NPS receptor (NPSR). This receptor was a formerly orphan GPCR whose activation increases calcium and cyclic adenosine monophosphate levels. The NPS/NPSR system is expressed in several brain regions where it controls important biologi...

journal_title：Expert opinion on therapeutic patents

authors： Ruzza C,Calò G,Di Maro S,Pacifico S,Trapella C,Salvadori S,Preti D,Guerrini R

更新日期：2017-03-01 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：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 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：: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 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: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：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：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：: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: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：:Small-molecule ligands, amenable to positron emission tomography (PET) imaging of different types of neurodegenerative disease-associated amyloid deposits in the CNS of living patients, hold considerable promise for diagnostic purposes, as well as for monitoring disease progression and the effectiveness of treatments....

journal_title：Expert opinion on therapeutic patents

authors： Ballatore C,Smith AB 3rd,Lee VM,Trojanowski JQ,Brunden KR

更新日期：2014-03-01 00:00:00

abstract：:Introduction: Phosphodiesterase 10 (PDE10) is one of at least 11 different PDE families, which are the enzymes that degrade adenosine 3',5'-cyclic monophosphate (cAMP) and/or guanosine 3',5'-cyclic monophosphate (cGMP) by hydrolyzing the phosphodiester bonds. Inhibition of PDE10A represents a molecular target in the t...

journal_title：Expert opinion on therapeutic patents

authors： Zagórska A

更新日期：2020-02-01 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: 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: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: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：:The concept of activation of glucokinase (encoded by the Gck gene) as a potential therapy for type 2 diabetes has been explored by several pharmaceutical companies. Small-molecule Gck activators (GKAs) were found to be effective at increasing glucose disposal by hepatocytes and lowering blood glucose in animal models ...

journal_title：Expert opinion on therapeutic patents

authors： Agius L

更新日期：2014-11-01 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: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：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:Bitopic M ligands, that is, ligands that interact both with the ortho- and allosteric binding sites of the M receptor subtypes, hold great potential as novel selective for muscarinic acetylcholine (M) ligands for several therapeutic applications. Areas covered: The patent application describes a set of com...

journal_title：Expert opinion on therapeutic patents

authors： Holzgrabe U,Decker M

更新日期：2017-02-01 00:00:00

abstract：INTRODUCTION:The use of inhibitors of HIV-1 integrase for treating HIV-1 infection has proven to be very beneficial. Raltegravir, a strand transfer inhibitor, has been approved for use both as a first-line therapy and in treatment-experienced patients. A second compound in this class, elvitegravir, is in Phase III clin...

journal_title：Expert opinion on therapeutic patents

authors： Pendri A,Meanwell NA,Peese KM,Walker MA

更新日期：2011-08-01 00:00:00

abstract：INTRODUCTION:Amino acid depletion in the blood serum is currently being exploited and explored for therapies in tumors or viral infections that are auxotrophic for a certain amino acid or have a metabolic defect and cannot produce it. The success of these treatments is because normal cells remain unaltered since they a...

journal_title：Expert opinion on therapeutic patents

authors： Fernandes HS,Silva Teixeira CS,Fernandes PA,Ramos MJ,Cerqueira NM

更新日期：2017-03-01 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 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: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：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