Abstract: The present application relates to azaaromatic amide derivatives for the treatment of cancer. Specifically, the present application relates to a preparation method and use of azaaromatic amide derivatives. The present application relates to azaaromatic amide derivatives and anilino-pyrimidine compounds represented by formula (I), formula (II), formula (III), formula (IV), and formula (V), and pharmaceutically acceptable salts thereof; the compounds or salts thereof can be used to treat or prevent a disease or disorder by regulating certain mutant forms of epidermal growth factor receptors. The present application also relates to a pharmaceutical composition comprising the compounds or salts thereof, and a method for treating various diseases mediated by EGFR, or HER2, or HER4 by using the compounds and salts thereof.

Abstract: Hydantoin based compounds useful as inhibitors of matrix metalloproteinases (MMPs), particularly macrophage elastase (MMP-12) are described. Also described are related compositions and methods of using the compounds to inhibit MMP-12 and treat diseases mediated by MMP-12, such as asthma, chronic obstructive pulmonary disease (COPD), emphysema, acute lung injury, idiopathic pulmonary fibrosis (IPF), sarcoidosis, systemic sclerosis, liver fibrosis, nonalcoholic steatohepatitis (NASH), arthritis, cancer, heart disease, inflammatory bowel disease (IBD), acute kidney injury (AKI), chronic kidney disease (CKD), Alport syndrome, and nephritis.

Abstract: The present disclosure provides a bio-based epoxy chain extender and a preparation method thereof, belonging to the technical field of chain extenders, and the preparation method includes the following steps: (1) mixing ESO and CD and carrying out catalytic reaction to obtain ESOn-CD; and (2) mixing and heating the ESOn-CD with concentrated sulfuric acid, dropwise adding a mixture of glacial acetic acid and hydrogen peroxide for stirring reaction, and after the stirring reaction, carrying out extraction and separation to remove a solvent to obtain the bio-based epoxy chain extender. The present disclosure also provides a bio-based epoxy chain extender prepared by the preparation method.

Abstract: The present technology provides compounds of Formula I and related methods for treating a bacterial infection as well as methods for inhibiting interaction of a bacterioferritin and a bacterioferritin-associated ferredoxin.

Abstract: Concentrated liquid pharmaceutical compositions comprising a) a pharmaceutically effective amount of bendamustine or a pharmaceutically acceptable salt thereof, b) a non-aqueous solvent, and c) at least about 2% water, suitable, after dilution, for administration to a mammal by injection are provided. The concentrated liquid pharmaceutical compositions can comprise a non-aqueous solvent comprising at least one organic polymeric compound solvent and at least one organic small molecule solvent. Methods of treating a cancer in a mammal in need of such treatment comprising administering to the mammal an effective amount of a concentrated liquid bendamustine pharmaceutical composition of the invention are also provided.

Abstract: The disclosure is directed to methods of using dantrolene, dantrolene prodrugs, or pharmaceutically acceptable salts thereof, to treat radiation exposure.

Abstract: Provided is a preparing method of linear carbonate compounds, including performing a coupling reaction of carbon dioxide in the presence of a titanium dioxide complex. The titanium dioxide complex includes an anatase phase and a rutile phase, a reduced titanium dioxide which is formed by selectively reducing any one of the anatase phase and the rutile phase, and a metallic oxide bound to the reduced titanium dioxide.

Abstract: The invention relates to an indane compound according to Formula (I), or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, L, n and p are as defined herein. The compounds are useful for treating antibacterial infection either as stand-alone antibiotics, or in combination with further antibiotics.

Abstract: Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.

Abstract: Provided herein are compositions and methods for treating or preventing a neurodegenerative disease, a myodegenerative disease, a prion disease or a lysosomal storage disease in a subject.

Abstract: Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFN?, by acting on Tyk-2 to cause signal transduction inhibition.

Abstract: The present invention provides various compositions, including compounds of Formula (I) or (Ia), or a species thereof, and pharmaceutically acceptable salts, solvates (e.g., hydrates), stereoisomer, tautomers, isotopic and other specified forms thereof. Also provided are methods (or uses) and kits involving the compounds or pharmaceutically acceptable compositions containing them for treating or preventing a disease (e.g., a proliferative disease such as cancer) in a subject. Administration of a compound or pharmaceutical composition described herein is expected to inhibit cyclin-dependent kinase 7 (CDK7), and thereby, induce apoptosis in tumor cells in the subject.

Abstract: Described herein are methods for the continuous preparation of 1,2-di(furan-2-yl)ethane-1,2-diol from furan-2-carbaldehyde. The methods can proceed chemically or electrochemically. In certain examples, the methods further comprise the application of a static mixer. The present methods produce 1,2-di(furan-2-yl)ethane-1,2-diol in greater yield, purity, chemoselectivity, and stereoselectivity than traditional batch methods.

Abstract: The present disclosures are directed to processes for synthesizing (S)-2-(((S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)amino)-N-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide (“nirogacestat”).

Abstract: The invention discloses herein related to synergistic combination of exogenous bioactives for activating intracellular secondary messenger (cAMP) signalling pathway. Particularly, the invention relates to synergistic compositions comprising combination of therapeutically effective amount of (3R)-3-acetyloxy-4-(trimethylazaniumyl) butanoate and N-4-aminobutylguanidine and salts thereof present in a weight ratio of 1:0.01 to 1:2 along with pharmaceutically acceptable excipients. Furthermore, the composition is useful for treating disease conditions or disorders related to depletion of secondary messenger pathway. The present invention further provides method of treating disease conditions related mental illness or disorder.

Abstract: The present invention relates to a pharmaceutical composition for preventing or treating neurodegenerative diseases comprising a diterpene, or a pharmaceutically acceptable salt thereof. Specifically, the diterpene of the present invention can prevent or treat neurodegenerative diseases caused by inhibition of Nurr1 activity by activating Nurr1 and inhibiting the inflammatory response.

Abstract: Provided is a method for administering a corticosteroid to a patient in need thereof, comprising: determining a target threshold for the ratio of urinary (tetrahydrocortisol+allotetrahydrocortisol) to urinary tetrahydrocortisone for the patient; and administering an HSD1 inhibitor to the patient. Also provided is a method for reducing or preventing the side effects associated with corticosteroid administration to a patient in need thereof, comprising: determining a target threshold for the ratio of urinary (tetrahydrocortisol+allotetrahydrocortisol) to urinary tetrahydrocortisone for the patient; and administering an HSD1 inhibitor to the patient.

Abstract: In accordance with the purpose(s) of the present disclosure, as embodied and broadly described herein is versatile polyene cyclization strategy that exploits conjugated ?-ionyl derivatives. Photomediated disruption of the extended ?-system within these chromophores unveils a contra-thermodynamic polyene that engages in a Heck-type cyclization to afford [4.4.1]-propellanes. The connectivity of overbred polycycles generated from this process is controlled by the position of the requisite C-Halide bond. Thus, compared to conventional biomimetic polyene cyclization, this approach allows for complete control of regiochemistry and facilitates incorporation of both electron-rich and electron-deficient (hetero)aryl groups. This strategy was successfully applied to the total synthesis of abietanes such as, for example, taxodione and salviasperanol, two isomeric abietane-type diterpenes that previously could not be prepared along the same synthetic pathway.

Abstract: The invention relates to the field of medicine and to the chemical and pharmacological industry, and concerns medicaments for the treatment of breast cancer. In particular the invention relates to a use of 3-O-sulfamoyloxy-7?-methyl-D-homo-6-oxaestra-1,3,5 (10),8(9)-tetraen-17a-one as an anti-cancer agent in monotherapy and adjuvant therapy of breast cancer, including the triple negative breast cancer.

Abstract: Described is a stable buffered aqueous colchicine solution or suspension being free of benzyl alcohol, comprising colchicine, a water miscible solvent and a preservative, characterized in that the solution comprises 0.01-1.0 w/v % colchicine, 2.5-15.0 w/v % glycerol and 0.05-1 w/v % preservative, the pH of the solution or suspension being 4.5-7.0. A method for the preparation thereof is also disclosed.