Abstract: The present invention relates to deuterated derivatives of lanifibranor, in particular for use in therapy, specifically in the treatment of fibrotic diseases.

Abstract: The present invention provides a PPAR? activator containing a novel PPAR? agonist (peroxisome proliferator-activated receptor ?) as an active ingredient, and an exercise tolerance-improving agent containing the same as an active ingredient. The present invention is a PPAR? activator containing a guanidine derivative or a biguanidine derivative as an active ingredient, wherein the PPAR? activator activates transcriptional activity of PPAR?, and the guanidine derivative and the biguanidine derivative are capable of fitting within a PPAR? ligand binding pocket in a state where a guanidino group or a biguanidino group forms a hydrogen bond with amino acid residues corresponding to each of the 413th histidine, 287th histidine, 253rd threonine and the 437th tyrosine of human PPAR?, among amino acid residues constituting an interior surface of the ligand binding pocket; and is an exercise tolerance-improving agent containing the PPAR? activator as an active ingredient.

Abstract: Compounds belonging to the group of N-benzyl-2-(4-(4-substituted-1H-1,2,3-triazol-1-yl)phenylacetamides have cytotoxic activities against MCF7 breast cancer cells, and are useful in therapeutic regimes for breast cancer. The N-benzyl-2-(4-(4-substituted-1H-1,2,3-triazol-1-yl)phenylacetamides also have beneficial effects on BAX, BCL-2, MCL-1 and MAPK pathways within MCF& breast cancer cells.

Abstract: The present invention relates to a compound selected from the group consisting of nolatrexed, triamterene, sultopride and hydrastinine or a pharmaceutically acceptable salt thereof, preferably triamterene, nolatrexed or a pharmaceutically acceptable salt thereof, and to combination of said compounds with other active ingredients, for use in the treatment and/or prevention of phenylketonuria, to the use of said compound or its combinations in the manufacture of a medicament for the treatment or prevention of said diseases and to a method of treating and/or preventing by administration of said compound or its combinations.

Abstract: The invention relates to a chemical synthesis method, the said method comprising “Spray Flash Evaporation”, also commonly referred to by the corresponding initialism SFE, which comprises the chemical reaction of at least one first compound with at least one second compound, under conditions in which the first compound and the second compound react to form at least one third compound. The invention also relates to a device for implementing this method and the compounds obtained by this method.

Abstract: Provided herein are novel compounds, e.g., those of Formula (I), as GCN2 inhibitors. Also provided are pharmaceutical compositions including one or more of the novel compounds, and pharmaceutical uses thereof. Compounds provided herein can typically inhibit an activity of a GCN2 and thus can be used for treating or preventing diseases related thereto.

Abstract: The invention provides a series of GMPS enzyme inhibitors. The invention includes potent GMPS inhibitors that specifically and covalently bind to GMPS, exhibit broad anti-cancer activity, block the infection efficiency of viruses, and have the potentials to suppress undesired immune responses. These novel inhibitors of GMPS, and their derivatives, have tremendous potentials to be used as therapeutic agents for the treatment of cancers, viral infection and immune disorders.

Abstract: The present disclosure relates to crystalline forms of N-{3-[1-(2-nitrophenyl)-1H-pyrrol-2-yl]-allylidene}-aminoguanidinium salts having high solubility. The disclosure also relates to use of said crystalline forms in medicine.

Abstract: Lysyl oxidase (LOX) inhibitors, lysyl oxidase-like (LOXL) inhibitors, or pharmaceutically acceptable salts thereof and methods for the treatment of myeloid malignancies, comprising administering a therapeutically effective amount of those inhibitors alone or optionally in combination with a second therapeutic agent.

Abstract: Provided is an imidazotriazine thiobenzamide derivative of formula (I), A preparation method for the imidazotriazine thiobenzamide derivative, and a use of the imidazotriazine thiobenzamide derivative or an isomer, a pharmaceutically-acceptable salt, or a prodrug thereof in the preparation of drugs for the treatment of cancer are also provided.

Abstract: Compounds that are inhibitors of at least one of ARG1 and ARG2, and compositions containing the compounds and methods for synthesizing the compounds, are described herein. The use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by ARG1 and ARG2 are also described herein.

Abstract: Co-crystals of itanapraced; methods of preparation of the co-crystals; uses of the co-crystals as APIs; formulations containing the co-crystals; uses of the co-crystals and formulations for prevention and treatment of neurodegeneration disorders, infections, dementias, inflammation, and injuries; and methods of prevention and treatment of neurodegeneration disorders, infections, dementias, inflammation, and injuries are described.

Abstract: A process for producing ethylene oxide by gas-phase oxidation of ethylene, comprising: directing a feed comprising gaseous ethylene and gaseous oxygen through a packing of individual shaped catalyst bodies, under conditions conducive to obtain a reaction mixture containing at least 2.7 vol.-% of ethylene oxide, wherein each shaped catalyst body comprises silver deposited on a refractory support and is characterized by a content of at least 20 wt.-% of silver, relative to the total weight of the shaped catalyst body; a BET surface area in the range of 1.6 to 3.0 m2/g; a first face side surface, a second face side surface and a circumferential surface with a plurality of passageways extending from the first face side surface to the second face side surface; and a uniform multilobed cross-section; and a longest direct diffusion pathway d, with 2d being in the range of 0.7 to 2.

Abstract: The present disclosure discloses a micromolecular compound specifically degrading tau protein, and an application thereof. The chemical structure of the micromolecular compound specifically degrading tau protein is TBM-L-ULM or a pharmaceutically acceptable salt, enantiomer, stereoisomer, solvate, polymorph or N-oxide thereof, TBM being a tau protein-binding moiety, L being a linking group, and ULM being a ubiquitin ligase-binding moiety, the tau protein-binding moiety and the ubiquitin ligase-binding moiety being connected by means of the linking group. The micromolecular compound specifically degrading tau protein may increase tau protein degradation in a cell, thereby decreasing tau protein content.

Abstract: A thioamide derivative of formula (I) and a preparation method thereof: An application of the thioamide derivative, or an isomer, a pharmaceutically-acceptable salt, or a prodrug molecule thereof in the preparation of a drug for the treatment of cancer is also provided. The thioamide derivative is a new compound with high antitumor activity, and can be used for antitumor therapy alone or in combination with other drugs.

Abstract: Provided are methods of using a MYC gene as a biomarker for predicting therapeutic efficacy of survivin inhibitors such as YM155 monobromide in cancer therapy, and related kits, compositions, and methods for diagnosing and treating cancer in a subject in need thereof.

Abstract: The present invention relates to a compound of Formula 1, a pharmaceutically acceptable salt or isomer thereof, a pharmaceutical composition including the same, and a use. The compound of Formula 1 according to the present invention has ketohexokinase (KHK) inhibitory activity, and is effectively used for preventing or treating metabolic disease such as diabetes, diabetic complications, obesity, nonalcoholic fatty liver disease, and fatty hepatitis.

Abstract: Provided herein are combination therapies for treating blood cancer, in particular, acute myeloid leukemia, by concurrently targeting Axl and BCL-2.

Abstract: Disclosed is a method of continuously preparing N,N-Bis(2,2,6,6-tetramethyl-4-piperidyl)-1,6-hexamethylenediamine, which relates to chemical engineering. The Pt/C catalyst and the quartz sand are mixed uniformly and loaded to the continuous-flow fixed-bed reactor. Then, hydrogen gas and a substrate solution containing 2,2,6,6-tetramethyl-4-piperidinone and 1,6-hexanediamine are simultaneously fed to the micro-mixer and the continuous-flow fixed-bed reactor in sequence to undergo a continuous catalytic reductive amination to obtain the N,N-Bis(2,2,6,6-tetramethyl-4-piperidyl)-1,6-hexamethylenediamine.

Abstract: The present invention relates to compounds and pharmaceutically acceptable salts or solvates thereof for use in the treatment or prevention of fascioliasis. Some of these compounds are novel per se and also have activity as inhibitors of Schistosoma growth. The invention also relates to pharmaceutical compositions comprising such novel compounds, salts or solvates and to the use of such novel compounds as medicaments, in particular in the treatment or prevention of schistosomiasis, also known as bilharzia.