Abstract: Provided are a photoactive fluorophore, a photoactive ligand, and a photoactive complex. The photoactive fluorophore includes a photoactivatable derivative of an azetidine-containing Janelia-Fluor dye. The photoactive ligand includes a photoactive fluorophore and a protein tag. The photoactive complex includes a photoactive ligand conjugated to a protein. Also provided are methods of in vivo labeling with and photoactivation of the photoactive fluorophore, ligand, and complex.

Abstract: Provided are a method of preparing a malononitrile oxime ether compound and an intermediate compound. The malononitrile oxime ether compound has a structure as shown in formula (VII), wherein W is selected from aryl or heteroaryl. The preparation method comprises: reacting a first raw material with a second raw material in the presence of a first solvent and a catalyst to obtain the intermediate compound, wherein the first raw material has a structure as shown in formula (IV), and the second raw material has a structure as shown in formula (V); and subjecting the intermediate compound, and a dehydrant to a dehydration reaction in the present of a second solvent to obtain the malononitrile oxime ether compound. Furthermore, the malononitrile oxime ether compound is obtained through one-step dehydration reaction. using the preparation method, is advantageous for improving the yield of malononitrile oxime ethers and reducing the cost.

Abstract: The present disclosure relates to the field of epoxide resin, and more particularly to an epoxide with a low total chlorine content and no heavy metal residues, and a preparation method thereof. Disclosed is an epoxide prepared from raw materials including an unsaturated cycloaliphatic compound containing a double bond, hydrogen peroxide, an organic acid compound, a solvent and an alkaline salt; wherein a molar ratio of the organic acid compound to the unsaturated cycloaliphatic compound containing a double bond is (1-1.5):1. The obtained epoxides obtained in the present disclosure have a high purity, a high yield, a low solvent content, low chroma, and a low chlorine and metal ion content; the reaction system is simple, environmentally friendly, safe and controllable, and the production cost is low, which can meet the technical and economic requirements and are suitable for large-scale industrial production.

Abstract: This invention relates to crystalline forms of anhydrous Compound (1) and pharmaceutical compositions thereof. Also disclosed herein are methods of making crystalline solid forms of Compound (1), and methods of using the crystalline forms of Compound (1) and pharmaceutical compositions thereof for modulating GABA activity (e.g., positive allosteric modulation of GABA activity) and treating CNS-related disorders.

Abstract: The present technology provides compounds according to Formula I or Formula III as well as compositions including such compounds useful for the treatment of metastatic cancer and/or glaucoma.

Abstract: An 8-((2-hydroxy-5-methylphenyl)diazenyl)naphthalene-1,3-disulfonic acid compound, its synthesis, and its use as an antioxidant agent.

Abstract: The invention relates to compounds of formula I wherein R1, R2 and - - - - - are as defined herein, pharmaceutical compositions comprising the compounds and methods of treating COVID-19 in a patient by administering therapeutically effective amounts of the compounds and methods of inhibiting or preventing replication of SARS-CoV-2 with the compounds.

Abstract: Disclosed are a [1,2,4]triazolo[1,5-a]pyridine compound as JAK inhibitor and an application thereof in preparing a drug for treating a disease related to JAK1 or/and TYK2. Specifically, the present invention relates to a compound represented by formula (I), or an isomer or pharmaceutically acceptable salt thereof.

Abstract: [Problem] A compound which is useful as a STING inhibitor is provided. [Means for Solution] The present inventors have found aryl alkynamide derivatives having an inhibitory action on STING. The aryl alkynamide derivatives of the present invention have an inhibitory action on STING and can be used as an agent for treating an autoimmune disease, a neurodegenerative disease, a type I interferonopathy and/or other STING-mediated disease.

Abstract: A 2-(benzo[d]oxazol-2-yl)-N?-(4-(dimethylamino)benzoyloxy)acetimidamide compound, its synthesis, and its use as an antimicrobial agent.

Abstract: Provided are compounds of Formula (I?), including compounds of Formulas (I), (II), (III), (IIIA) and (IIIB), wherein L, R1, R3 and n are as defined herein, and pharmaceutically acceptable salts thereof, and methods for their use and production. These compounds can be useful, e.g., in the treatment of disorders responsive to the inhibition of apoptosis signal-regulating kinase 1 (ASK1).

Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: R1, R2, R3, and R4 are defined herein. Also disclosed are methods of using such compounds to inhibit the activity of one or both of diacylglycerol kinase alpha (DGK ?) and diacylglycerol kinase zeta (DGK?), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.

Abstract: A pyridinylmethylenepiperidine derivatives and uses thereof, specifically, the present invention relates to a novel pyridinylmethylenepiperidine compound and a pharmaceutical composition containing this compound, which may be used for activating 5-HT1F receptor. The present invention also relates to methods of preparing this compound and pharmaceutical composition, and their use in the manufacture of a medicament for treating a 5-HT1F receptor-related disease, especially migraine.

Abstract: A full continuous-flow preparation method of vitamin B1 includes: (S1) feeding 3-chloro-4-oxopentyl acetate, 2-methyl-4-amino-5-(aminomethyl) pyrimidine and carbon disulfide to a first continuous-flow reactor for addition; (S2) allowing the reaction mixture to flow into a first continuous filtration and reaction device to collect a filter cake; subjecting the filter cake and hydrochloric acid solution to cyclization; transporting the reaction mixture and an aqueous inorganic base solution to a micromixer and a second continuous-flow reactor for hydrolysis to obtain thiothiamine; (S3) transporting the thiothiamine to a third continuous-flow reactor with hydrogen peroxide for oxidation to obtain thiamine sulfate; and (S4) allowing the thiamine sulfate to enter a second continuous filtration and reaction device for filtration to collect a filter cake; and subjecting the filter cake to reaction with organic hydrochloric acid solution followed by filtration and drying to obtain vitamin B1.

Abstract: The present invention relates to salts and crystalline forms of 2-(3-(8-Amino-6-(trifluoromethyl)imidazo[1,2-a]pyrazin-3-yl)-4-methylphenyl)-3,3,3-trifluoro-2-hydroxypropanamide, crystalline forms of 8-amino-N-(2-hydroxy-2-methylpropyl)-3-(2-methyl-5-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl)imidazo[1,2-a]pyrazine-6-carboxamide, and crystalline forms of 8-amino-N-(2-hydroxy-2-methylpropyl)-3-(2-(methyl-d3)-5-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl)imidazo[1,2-a]pyrazine-6-carboxamide, which are PI3K inhibitors useful in the treatment of cancer and other diseases.

Abstract: Adrenergic receptor modulating compounds and methods of using the same are provided. Also provided are methods of treating a subject for a disease or condition associated with an adrenergic receptor including administering a therapeutically effective amount of the subject compound. Aspects of the disclosure include a method of modulating an inflammatory pathway in a cell, such as the production of TNF-alpha in the cell. The method can include contacting a cell with ?1-selective adrenergic receptor modulating compound to selectively activate a cAMP pathway over a beta-arrestin pathway in the cell. Pharmaceutical compositions and kits which include the subject compounds are provided.

Abstract: Disclosed are benzimidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R1, R2, R3, R4, Y and X are as described herein. In certain embodiments, a compound disclosed herein activates AMPK, and can be used to treat disease by activating the AMPK pathway.

Abstract: The present disclosure relates to crystalline particles of N—((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide (I) having specific surface area (SSA) in the range from about 8 to about 16 m2/g, preferably from about 10 to about 15 m2/g, and to the method for the preparation of such particles. Compound (I) is a potent androgen receptor (AR) modulator which is useful as a medicament for example in the treatment of prostate cancer.

Abstract: The invention provides a compound of formula 1 or a pharmaceutically-acceptable salt thereof, that is useful as a JAK inhibitor. The invention also provides crystalline forms of the compound, pharmaceutical compositions comprising the compound, methods of using the compound to treat diseases amenable to a JAK inhibitor, and processes and intermediates useful for preparing the compound.

Abstract: The invention provides a compound for use in the treatment of T-Cell Acute Lymphoblastic Leukaemia (T-ALL), the compound having the formula (1): or being a pharmaceutically acceptable salt thereof; wherein: n is 0, 1 or 2; Ar1 is selected from an optionally substituted phenyl, pyridyl, thienyl and furanyl; Q1 is selected from C(?O), S(?O) and SO2; A is absent or is NR2; R1 is selected from: hydrogen; an optionally substituted C1-6 non-aromatic hydrocarbon group; and optionally substituted 3- to 7-membered non-aromatic carbocyclic and heterocyclic rings containing one or two heteroatom ring members selected from O, N and S, and bridged bicyclic heterocyclic rings of seven to nine ring members of which one or two are nitrogen atoms, the carbocyclic and heterocyclic rings and bridged bicyclic heterocyclic rings; R2 is selected from hydrogen and C1-4 alkyl; or NR1R2 forms an optionally substituted 4- to 7-membered non-aromatic nitrogen-containing heterocyclic ring optionally containing a second hete