Abstract: In vitro or ex vivo methods for screening a quinoline derivative, or anyone of its pharmaceutically acceptable salt, presumed effective in treating and/or preventing an inflammatory disease, the method including: providing an eukaryotic cell, bringing into contact said cell with a quinoline derivative, measuring an expression of miR-124 in the cell, and selecting the candidate presumed effective in treating and/or preventing an inflammatory disease when the level of expression of miR-124 measured is increased relatively to a reference value.

Abstract: The present invention refers to oxadiazole compounds suitable as HDAC6 inhibitors. Processes for their preparation and their medical uses in treating HDAC6-related diseases or disorders are also disclosed.

Abstract: Para-acyl substituted diazacyclohexenes, medical formulations thereof and methods for making and using the same.

Abstract: Novel Halogenated Benzylidine derivatives are provided which exhibit activity for the treatment of immunological diseases and inflammation.

Abstract: Disclosed is a 5-methylchromone and the preparation method and application thereof, the 5-methylchromone has the following structure: wherein R1 and R2 are alkyl groups. The substituted chromone has the biological activity of inhibiting tyrosinase. The preparation method uses 3,5-dihydroxytoluene as a raw material, and synthesis of chromones substituted with different groups at 2-C through acylation, esterification, rearrangement and cyclization reactions, etc. The 5-methylchromone is a completely new compound in condition that R1 is —CH2CH2CH3, and R2 is —CH2CH3, or that R1 is —C(CH3)3, and R2 is H. All the compounds have obvious inhibitory activity against tyrosinase, and can be used to prepare tyrosinase inhibitors or whitening agents.

Abstract: A rapid synthesis method for a biomass-based amine, including: using formamide as an amine source, formic acid as a hydrogen source, and biomass aldehyde or ketone as a raw material, conduct rapid heating promoting direct addition of formamide and aldehyde or ketone compound through microwave-assisted heating and without a solvent and catalyst, and carrying out formic acid reduction preparing and obtaining a corresponding formamide derivative; selectively converting the formamide derivative under the action of a base into a corresponding primary amine through alcoholysis.

Abstract: Described herein are polymorphic forms of a CB1 modulator, methods of making such forms, pharmaceutical compositions and medicaments comprising such forms, and methods of using such forms in the treatment of conditions, diseases, or disorders that would benefit from modulation of the CB1 receptor.

Abstract: The present invention relates to a new intermediate, (2,2-dimethyl-N-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-propanamide) useful in the synthesis of lasmiditan, to a method for obtaining same, to the use of said intermediate for preparing lasmiditan, to a method for preparing lasmiditan making use of said intermediate, and to a method for preparing an intermediate ((6-amino-pyridin-2-yl)-(1-methyl-piperidin-4-yl)-methanone) from (2,2-dimethyl-N-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-propanamide).

Abstract: Disclosed herein is a tricyclic octacationic cyclophane and complexes comprising the tricyclic octacationic cyclophane and a perylene diimide dye complexed therein and methods of using and making the cyclophane and complexes.

Abstract: The present invention provides turn-ON dioxetane-based chemiluminescence probes based on the Schapp's adamantylidene-dioxetane probe, which are capable of detecting or imaging, more specifically, determining the presence, or measuring the level, of proteases, as well as compositions and uses thereof.

Abstract: The present invention relates to a method for preparing 2-alkoxy-4-amino-5-methylpyridines of the formula (I) and/or 2-alkoxy-4-alkylamino-5-methylpyridines of the formula (II) from the corresponding 2-haloaminopyridines and the appropriate alcohols in the presence of base, and to the compounds resulting therefrom.

Abstract: The present invention relates to pharmaceutical compounds of Formula (I): as further described herein, and pharmaceutical compositions containing such compounds, as well as methods of using these compounds to modulate the activity of aryl hydrocarbon receptor (AhR) and to treat conditions comprising inflammation inside the intestinal tract and certain disorders of the central nervous system affected by the gut-brain axis, including IBD, ulcerative colitis, Crohn's disease, Huntington's disease, and multiple sclerosis.

Abstract: The present invention relates to compounds of formula (I): (I) wherein Q is selected from O or S; R1 is an optionally substituted hydrocarbyl group which may optionally include one or more heteroatoms N, O or S in its carbon skeleton, provided that the hydrocarbyl group includes at least one heteroatom N, O or S in its carbon skeleton or is substituted with a substituent comprising at least one heteroatom N, O or S, and provided that the atom of R1 which is attached to the sulfur atom of the remainder of the molecule is not a ring atom of a cyclic group; R2 is an ?,??-substituted cyclic group which may optionally be further substituted; R3 and R4 are each independently hydrogen, halogen, —OH, —NH2, —CN, —R5, —OR5, —NHRs or —N(R5)2; or R3 and R4 together with the carbon atom to which they are attached may form a 3- to 7-membered saturated or unsaturated, optionally substituted cyclic group; and R5 is independently optionally substituted C1-C4 alkyl.

Abstract: The compounds represented by Formula (I), which are peripheral alkyl and alkenyl chains extended benzene derivatives, are useful as dual autotaxin (ATX)/histone deacetylase (HD AC) inhibitors. These compounds may be included in a pharmaceutical composition along with a pharmaceutically acceptable carrier, and be used in a therapeutically effective amount for prophylaxis or treatment of various diseases and disorders.

Abstract: A 4,4?-divinylazoarylene-bridged diruthenium catalyst bearing two Ru(CO)(3-methoxypyridin-2-olate)(PiPr3)2 moieties, its synthesis, and its use as a catalyst.

Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

Abstract: The present invention provides a compound having an excellent control effect on a harmful arthropod.

Abstract: Described herein are heterocycle substituted pyridine derivative antifungal agents and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of fungal diseases and infections.

Abstract: The present invention provides crystalline forms of (E)-6-(4-Phenylcyclohexyl)-5-(3-trifluoromethylbenzyl)-1H-pyrimidine-2,4-dione, and methods of making and using the same.

Abstract: The present disclosure provides compounds that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.