Abstract: The present disclosure concerns at least one entity chosen from compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the variable groups X, R1, R2, R3 m, n and p are as defined herein. The present disclosure also relates to methods for the preparation of at least one such entity, and intermediates useful in the preparation thereof, to pharmaceutical compositions containing at least one such entity, to the use of at least one such entity in the preparation of medicaments, and to the use of at least one such entity in the treatment of conditions such as, for example, allergic diseases, autoimmune diseases, viral diseases, and cancer.

Abstract: The present invention relates to a novel azole derivative as an apelin receptor agonist and a method for treating cardiovascular disease, diabetic disease, renal disease, hypertension, and arteriosclerosis, etc., using the same. The present invention provides a compound represented by formula (I) or a pharmacologically acceptable salt thereof wherein X1 represents —N? or —CH?, X2 represents —CH? or —N?, R1 and R2 each represent a C1 to C6 alkoxy group or the like, R3 represents a heteroaryl group (the heteroaryl group is optionally substituted by a methyl group or the like) or the like, and R4 represents a C1 to C6 alkylthio group or a C2 to C6 alkenyl group (the C1 to C6 alkylthio group and the C2 to C6 alkenyl group are each optionally substituted by one carboxy group or the like) or the like.

Abstract: The present technology provides a system for monitoring quorum-sensing in bacteria comprising bacteria that release at least one membrane-lytic toxin when the bacteria are at a quorum-sensing density; synthetic lipid vesicles comprising an environmentally sensitive indicator, wherein the synthetic lipid vesicles release the environmentally sensitive dye in the presence of an effective amount of the membrane-lytic toxins; and a growth medium; wherein the bacteria and synthetic lipid vesicles are in contact with the growth medium. Methods using the system and compounds discovered with the system (e.g., compounds of Formulas I and II) are also disclosed.

Abstract: The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

Abstract: Disclosed are novel C4-carboxylic acid-substituted tryptamine derivative compounds and pharmaceutical and recreational drug formulations containing the same. The pharmaceutical formulations may be used to treat brain neurological disorders.

Abstract: The present invention relates to an immunosuppressant comprising TSAHC or a pharmaceutically acceptable salt thereof as an active ingredient. TSAHC treatment suppressed the expression and secretion of cytokines/chemokines such as IL6, IL1?, TNF?, CXCL1, CXCL2, CXCL3, CXCL6, CXCL8, CCL2, CCL5, CCL20, CXCL10 and CCR10 according to the expression of TM4SF5 gene and protein, and the cytokines or chemokines mediated by the expression of TM4SF5 induced abnormalities in the inflammatory response and metabolic function of liver tissues, hepatic epithelial cells and macrophages, and correlated with liver tissue damage and immune cell recruit in TM4SF5 transgenic animals. Therefore, a composition comprising TSAHC or a pharmaceutically acceptable salt thereof as an active ingredient can be effectively used as an immunosuppressant.

Abstract: A method of determining a dose of a treatment compound for treating a subject having systemic lupus erythematosus (SLE), comprising obtaining a sample from the subject and measuring the gene expression level of IKZF3 and/or the gene expression levels of IFI27, IFI44, IFI44L, and RSAD2 in the sample.

Abstract: The present disclosure provides endosomal disruptors, which are useful for facilitating delivery of a macromolecule to the cytoplasm of a cell. The present disclosure provides compositions comprising an endosomal disruptor and a macromolecule. The present disclosure provides methods of delivering a macromolecule to the cytoplasm of a cell.

Abstract: Compounds of formula (I): as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

Abstract: The invention is based on the finding that Airway Basal Cells (ABCs) play a key role in the pathobiology of various lung diseases. The invention therefore provides approaches for the treatment and prevention of lung diseases such as fibrotic disorders, pre stages of fibrosis, Chronic Obstructive Lung Diseases (COPD) or other lung disorders. Diseases treatable with the means and methods of the invention are characterized by a cellular remodelling in the alveolar compartment of the lung. Furthermore, the invention provides screening approaches to identify compounds suitable for the treatment of lung diseases.

Abstract: The invention relates to a novel compound manufactured with the procedure of synthesis of bouncing Carvacrol and Lidocaine into one stable compound. Use of the compound as an active compound/potent antimicrobial for the treatment of bacterial infections in humans caused by pathogens resistant to antibiotics, such as Methicillin-resistant Staphylococcus aureus (MRSA), Streptococcus faecalis, Mycobacterium tuberculosis, Escherichia spp. E. coli, Salmonella spp. Pasteurella spp., Corynebacterium spp., Bacillus spp., Bacillus anthracis, Clostridium spp., Spherophorus spp., Candida spp., Trichophyton spp., Microsporum spp., Mycobacterium spp., Vibrio spp., Cryptosporidium spp., Microsporidia spp., Listeria monocytogenes, Lawsonia intracellularis, Treponema dysenteriae, Enterococcus spp., Haemophilus spp., Campylobacter spp., Chlamydia spp., Brucella spp., and other pathogenic bacterial species.

Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are biased agonists, or ?-Arrestin agonists of the angiotensin II receptor, which may be used as medicaments.

Abstract: Disclosed are chelating co-polymer compositions that are soluble in aqueous media and chelate essential metals, methods of preparation and uses thereof. The chelating compositions are comprised of two or more different monomers, at least one of which possesses metal binding or metal chelating activity. The chelating compositions are synthesized by reversible addition-fragmentation transfer (RAFT) polymerization with the aid of a suitable RAFT-mediating agent. Also described are chelating compositions that comprise hydroxypyridinone chelating groups. The ability of the chelating compositions to bind metals affects the activity of a living cells and organisms, which require the metals for cellular functions.

Abstract: Described herein are methods and systems for using an alkaloid, such as manzamine A, for anti-proliferative effects at relatively low and non-cytotoxic concentrations (up to 4 ?M) wherein manzamine A blocks cell cycle progression in cervical cancer cell lines and regulates cell cycle-related genes, including restoration of p21 and p53 expression inducing apoptosis.

Abstract: In production of crops of agriculture and horticulture or the like, damage caused by diseases is still large, and, due to factors such as occurrence of resistant diseases to existing drugs, development of new agrohorticultural fungicides is desired. The present invention provides an agrohorticultural fungicide and a method of use thereof of, an active ingredient thereof being a compound represented by the general formula (I) or salts thereof: {wherein X1, X2, X3 and X4 denote a hydrogen atom or the like, A, B, Y, denote a single bond or carbonyl group or the like, Q denotes a (C1-C6)alkyl group or hetero ring or the like, R5 and R6 denote a hydrogen atom or (C1-C6)alkyl group or the like.}.

Abstract: The present disclosure relates to a chlorin derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, an anti-tumor composition including the chlorin derivative or the pharmaceutically acceptable salt thereof, use of the chlorin derivative or the pharmaceutically acceptable salt thereof in the treatment of a tumor, and a combination of the chlorin derivative or the pharmaceutically acceptable salt thereof and an ultrasound medical system. The chlorin derivative or the pharmaceutically acceptable salt thereof has a structure represented by formula (I), and the ultrasonic medical system comprises a transducer ultrasonic bed and a contact agent. The chlorin derivative of the present disclosure can be used in photodynamic therapy and sonodynamic therapy, thereby effectively inhibiting and treating cancer.

Abstract: An aqueous microemulsion containing at least one phenolic compound, specifically thymol and/or carvacerol, a solubilizer and water. This microemulsion can be applied to surfaces to provide disinfectant properties.

Abstract: The present invention is related to a pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound represented by the following structural formula: The present invention is also related a method of treating a subject with a disease which can be ameliorated by inhibition of poly(ADP-ribose)polymerase (PARP). The definitions of the variables are provided herein.

Abstract: Methods of inhibiting endosomal trafficking of PD-L1, inducing PD-L1 secretion via exosomes, decreasing PD-L1 level at a surface of a cancer or tumor cell, and treating a cancer or tumor through promoting T cell immune response in a subject suffering from a cancer or tumor, includes the step of administering a compound of Formula I to various cells. Also, a composition to treat a cancer or a tumor, includes a compound of Formula I and an anti-PD-1 antibody.

Abstract: In various embodiments, the present disclosure provides methods reducing the risk of heart failure in a subject on statin therapy by administering to the subject a pharmaceutical composition comprising about 1 g to about 4 g of eicosapentaenoic acid ethyl ester or a derivative thereof.