Abstract: The present application provides a compound of formula I: or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R1-R10, m, n, p, and are as described herein. The present invention relates generally to FXR modulators and to methods of making and using said compounds.

Abstract: Disclosed is a compound of formula I or a pharmaceutically acceptable salt, active metabolite, tautomer, stereoisomer, or prodrug thereof as BTK (Bruton's Tyrosine Kinase) inhibitors, which is useful for the treatment of autoimmune disease, inflammatory disease, cancer and potentially allergies.

Abstract: This technology relates to immune system stimulating molecules to be used in the treatment of drug addiction and abuse and their synthesis processes. These molecules have a calixarene chemical structure, preferably calix[4]arene and/or calix[8]arene, coupled to an hapten analogous to cocaine, preferably GNE and/or GNC. An anti-drug vaccine, specifically anti-cocaine, is also described using such molecules. The anti-drug vaccine can be also used to prevent fetal exposure to drugs in pregnant women who use drugs and do not wish or cannot stop their use during pregnancy.

Abstract: 4-Hydroxyphenyl-2H-indazol-5-ol compounds are estrogen receptor beta ligands that have immunomodulatory properties and increase oligodendrocyte survival, differentiation, and remyelination. The compounds, compositions, and kits are useful in the treatment of multiple sclerosis and endometriosis.

Abstract: This document provides methods and materials for increasing TFEB polypeptide levels. For example, compounds (e.g., organic compounds) having the ability to increase TFEB polypeptide levels within cells and/or within a nucleus of cells, formulations containing compounds having the ability to increase TFEB polypeptide levels within cells and/or within a nucleus of cells, methods for making compounds having the ability to increase TFEB polypeptide levels within cells and/or within a nucleus of cells, methods for making formulations containing compounds having the ability to increase TFEB polypeptide levels within cells and/or within a nucleus of cells, methods for increasing TFEB polypeptide levels within cells and/or within a nucleus of cells, and methods for treating mammals (e.g., humans) having a condition responsive to an increase in TFEB polypeptide levels are provided.

Abstract: A crystalline form of treosulfan and methods to prepare it are described. This crystalline form of treosulfan is useful in pharmaceutical compositions for the treatment of cancer and for conditioning therapy before transplantation of bone marrow or blood stem cells.

Abstract: Disclosed is a compound represented by formula [I] according to the specification, or a salt thereof, a composition comprising the compound, a chemiluminescence method using the compound, a method for measuring chemiluminescence signal, a reagent comprising the compound, a reagent kit comprising the compound and a method for assaying analyte.

Abstract: Methods for asymmetric cis-dihydroxylation (“AD”) of quinones to produce cis-diols of quinones with high yield (i.e. a yield ?30%) and high enantioselectivity (i.e. an enantiometric excess ?30%) are disclosed. The method uses an iron-based catalyst, such as one or more Fe(II) complexes, as the catalyst, and can be performed under mild reaction conditions (e.g. a temperature ?50° C. at 1 atom in open air). The method generally includes: (i) maintaining a reaction mixture at a temperature for a period of time sufficient to form a product, where the reaction mixture contains a quinone, one or more iron-based catalyst(s), and a solvent, and where the product contains a chiral cis-diol. Optionally, the method also includes adding an oxidant into the reaction mixture prior to and/or during step (i), such as a hydrogen peroxide solution.

Abstract: The present disclosure relates to compounds useful as modulators of neurokinin receptor 3 (NK3) for the treatment of conditions or disorders.

Abstract: The present invention relates to 3-(1,2,3,6-tetrahydropyridin-2-yl)pyridine glutarate or a pharmaceutically acceptable solvate thereof, to a crystal thereof and to a polymorph of this crystal. It further relates to the medicinal use of each of these, in particular in the treatment or prophylaxis of substance addiction or inflammation.

Abstract: Provided herein are certain compounds useful as HTT modulators. Such compound are useful in the treatment of Huntington's disease.

Abstract: The present disclosure relates to compounds of formula I, which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions.

Abstract: Provided is a high-concentration and high-purity eicosapentaenoic acid-containing composition. A method for producing an eicosapentaenoic acid alkyl ester-containing composition, the method includes: (1) bringing a raw oil that contains an eicosapentaenoic acid alkyl ester into contact with an aqueous solution that contains a silver salt, and then collecting an aqueous layer; (2) adding an organic solvent to the aqueous layer, and then collecting an organic solvent layer; and (3) subjecting the organic solvent layer to vacuum distillation at a temperature of 180 to 188° C. and a tower top vacuum degree of 0.7 Pa or below, to recover the eicosapentaenoic acid alkyl ester from the organic solvent layer.

Abstract: Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.

Abstract: The present technology provides compounds, as well as compositions including such compounds, useful for imaging and/or treatment of a glioma, a breast cancer, an adrenal cortical cancer, a cervical carcinoma, a vulvar carcinoma, an endometrial carcinoma, a primary ovarian carcinoma, a metastatic ovarian carcinoma, a non-small cell lung cancer, a small cell lung cancer, a bladder cancer, a colon cancer, a primary, gastric adenocarcinoma, a primary colorectal adenocarcinoma, a renal cell carcinoma, and/or a prostate cancer.

Abstract: The present invention relates to the use of cannabidiol (CBD) for the treatment of tumours associated with Tuberous Sclerosis Complex (TSC). In particular the CBD was able to decrease the number and size of marker cells, pS6, in a zebrafish model of TSC. This is suggestive of a disease modifying effect whereby treatment with CBD could result in the reduction or prevention of the benign tumours that occur in TSC patients. Preferably the CBD used is in the form of a highly purified extract of cannabis such that the CBD is present at greater than 98% of the total extract (w/w) and the other components of the extract are characterised. In particular the cannabinoid tetrahydrocannabinol (THC) has been substantially removed, to a level of not more than 0.15% (w/w) and the propyl analogue of CBD, cannabidivarin, (CBDV) is present in amounts of up to 1%. Alternatively, the CBD may be a synthetically produced CBD. In use the CBD is given concomitantly with one or more other drugs used in the treatment of TSC.

Abstract: The invention provides a material comprising (i) a crown ether of formula (I), (ii) a crown ether of formula (II), and/or (iii) a crown ether of formula (III), or a salt thereof, wherein each m independently is an integer from 1 to 8, p is an integer from 1 to 1000, each “” designates an optionally present bond and/or structure, each X is an optionally present substituent, each * independently represents —H, ?O, or a bond to a remainder of the material, provided that at least one * is a bond to the remainder of the material, and wherein the remainder of the material is bound via a sp3-sp3 carbon-carbon bond, a method of making the material, and a method of using the material.

Abstract: Provided are a Rho kinase inhibitor, a method for preparing same and the uses thereof. The Rho kinase inhibitor designates a compound of Formula I, a stereoisomer thereof or pharmaceutically acceptable salt thereof. The Rho kinase inhibitor promotes endothelial cells and endothelin expression, prostenin expression, and vascular factors NO synthesis and secretion, has a promoting effect on proprostin expression independently of the doses used, shows lower toxicity, while being safer.

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.