Abstract: The present invention discloses a phosphine nitrogen ligand with multiple chiral centers and its synthesis method and application. The ligand has the axial chirality of a biaryl skeleton and the central chirality of a chiral amine. The chiral ligand is synthesized from commercially available raw materials through a simple five-step reaction, and the resulting diastereomer can be separated by simple column chromatography or recrystallization. The chiral phosphine nitrogen ligand synthesized by the present invention can catalyze the asymmetric three-component coupling reaction of terminal alkynes, aldehydes and amines, and realize the efficient preparation of chiral propargyl amines with high optical activity.

Abstract: Anti-epileptic toxin Martentoxin (MarTX), derivatives thereof, and uses thereof are described. Specifically, the use of Martentoxin or an active fragment thereof or a pharmaceutically acceptable salt thereof in preparing a preparation or composition for treating and/or preventing epilepsy is described. It has been confirmed for the first time that the Martentoxin can effectively treat and/or prevent epileptic symptoms.

Abstract: Disclosed are a preparation method for a 1,3-disubstituted allene compound at room temperature based on a metal carbene catalyst, comprising: reacting terminal alkynes, aldehydes and amines in an organic solvent under the action of a gold catalyst and a molecular sieve, and then synthesizing a 1,3-disubstituted allene compound at room temperature. The method of the present invention is simple to operate, raw materials and reagents are easily obtained, reaction conditions are mild, substrate universality is wide, functional group compatibility is good, yield is high (36-93%), the method is scalable (11 g), and practicability is strong. The 1,3-disubstituted allene compound obtained in the present invention may be used as an important intermediate to construct ?-caprolactone, trans-allyl alcohol, other allene-derived compounds and natural product molecules and the like.

Abstract: Provided is a metal complex as represented by formula I. The metal complex may be used as a catalyst for asymmetric catalytic hydrogenation, is capable of efficiently catalyzing and synthesizing a series of chiral p-aryl amides having high optical purity, and is especially capable of asymmetrically catalyzing and hydrogenating a tetra-substituted enamide compound, chiral amides having high optical purity are synthesized, and the carrying amount of ligand may reach 100,000.

Abstract: The present disclosure provides a class of Pyridopyrimidine compounds having a structure shown in Formula (I) or their pharmaceutically acceptable salts, or stereoisomers or prodrug molecules and applications thereof. The compounds in the present disclosure can efficiently and selectively degrade AKT3 protein in cells without affecting AKT1/2, thereby significantly inhibiting tumor cell proliferation mediated by high expression of AKT3 protein. It can be used to prepare therapeutic drugs for cancer and other diseases related to abnormal expression of AKT3 protein.

Abstract: The present invention discloses a phosphine nitrogen ligand with multiple chiral centers and its synthesis method and application. The ligand has the axial chirality of a biaryl skeleton and the central chirality of a chiral amine. The chiral ligand is synthesized from commercially available raw materials through a simple five-step reaction, and the resulting diastereomer can be separated by simple column chromatography or recrystallization. The chiral phosphine nitrogen ligand synthesized by the present invention can catalyze the asymmetric three-component coupling reaction of terminal alkynes, aldehydes and amines, and realize the efficient preparation of chiral propargyl amines with high optical activity.

Abstract: Chiral 1, 3-diarylimidazole salt carbene precursors, their methods of preparation, particularly transition metal complexes and their use in chemical synthesis are provided. In particular, an air and moisture stable chiral 1, 3-diarylimidazole carbene precursor Cu (I) complex has been prepared and applied to highly regio- and enantioselective Markovnikov hydroboration of unactivated terminal alkenes to form chiral boronic esters. Moreover, these new chiral NHCs can be potentially applied in various metal-catalyzed asymmetric transformations.

Abstract: The present invention provides uses for the anti-epileptic toxin Martentoxin and derivatives thereof. Specifically, the present invention provides the use of Martentoxin (or MarTX toxin) or an active fragment thereof or a pharmaceutically acceptable salt thereof in preparing a preparation or composition for treating and/or preventing epilepsy.

Abstract: Wolfberry glycopeptide composition and methods for preparing and using the same, the part with a molecular weight distribution of 1000 Da to 10000 Da of the wolfberry glycopeptide accounts for 50-85% on the HPLC differential refractive index map; and the protein content is 20-35% weight percentage, neutral polysaccharide content is 20-35% weight percentage. Optionally, the uronic acid content is 5-20% weight percentage. The preparation method of the present invention removes part of insoluble impurities by a heating flocculation method, instead of the conventional organic solvent extraction process, and without using any organic solvents in the whole process.

Abstract: Disclosed in the present invention were a fluorosulfonyl-containing compound, an intermediate thereof, a preparation method therefor and use thereof. The fluorosulfonyl-containing compound disclosed in the present invention comprises a cation and an anion, the cation being as shown in Formula (1). The fluorosulfonyl-containing compound of the present invention can react with a substrate to efficiently synthesize a fluorosulfonylation product, has low toxicity, was simple to prepare, was convenient to use, and was in a solid stable state at normal temperature. Furthermore, the compound has a wide range of adaptable substrates, including phenolic compounds and amine compounds, and was the only solid form agent that can achieve such a chemical conversion, and therefore has important academic and application value.

Abstract: Provided is the use of an aromatic ring drug in inhibiting a key transcription factor of malignant melanoma. In particular, provided is the use of a compound as represented by formula A, or an optical isomer thereof or a racemate thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof in the preparation of a pharmaceutical composition or preparation. The pharmaceutical composition or preparation is used for: (a) inhibiting a key transcriptional regulatory factor of malignant melanoma, namely MITF (Microphthalmia-associated Transcription Factor); (b) treating MITF-related diseases such as melanoma, pancreatic cancer, skin hypersensitivity and asthma; and (c) regulating physiological activities in which MITF is involved, such as skin whitening. In the formula, each group is as defined in the description.

Abstract: A compound for improving the gene editing specificity and application thereof. Specifically disclosed is a compound represented by formula I or a use of a pharmaceutically acceptable salt thereof. The compound and the pharmaceutically acceptable salt thereof are used for preparing an inhibitor, a composition, or a formulation for inhibiting gene editing and/or improving the gene editing specificity. The structure of the formula I is as stated in the description. The compound can significantly improve the accuracy of CRISPR gene editing, thereby providing a simple and high-efficient policy for accurate gene editing.

Abstract: Disclosed are a compound represented by general formula I and a preparation method therefor. The compound can be used as indoleamine-2,3-dioxygenase inhibitor to prepare medicines for preventing and/or treating indoleamine-2,3-dioxygenase-mediated diseases.

Abstract: Disclosed in the present invention were a fluorosulfonyl-containing compound, an intermediate thereof, a preparation method therefor and use thereof. The fluorosulfonyl-containing compound disclosed in the present invention comprises a cation and an anion, the cation being as shown in Formula (1). The fluorosulfonyl-containing compound of the present invention can react with a substrate to efficiently synthesize a fluorosulfonylation product, has low toxicity, was simple to prepare, was convenient to use, and was in a solid stable state at normal temperature. Furthermore, the compound has a wide range of adaptable substrates, including phenolic compounds and amine compounds, and was the only solid form agent that can achieve such a chemical conversion, and therefore has important academic and application value.

Abstract: Disclosed in the present invention were a fluorosulfonyl-containing compound, an intermediate thereof, a preparation method therefor and use thereof. The fluorosulfonyl-containing compound disclosed in the present invention comprises a cation and an anion, the cation being as shown in Formula (1). The fluorosulfonyl-containing compound of the present invention can react with a substrate to efficiently synthesize a fluorosulfonylation product, has low toxicity, was simple to prepare, was convenient to use, and was in a solid stable state at normal temperature. Furthermore, the compound has a wide range of adaptable substrates, including phenolic compounds and amine compounds, and was the only solid form agent that can achieve such a chemical conversion, and therefore has important academic and application value.

Abstract: Disclosed are a retinoid compound, a preparation method therefor, intermediates thereof and an application thereof. The retinoid compound I of the present invention has a good tumor growth inhibition rate.

Abstract: Provided are compounds generated by conjugation of triptolide with glucose to form glucose-triptolide conjugates, provides compounds with effective anti-proliferative activity and improved tolerability as compared to naturally occurring triptolide compounds.

Abstract: Provided in the present invention are a class of Lincomycin biosynthetic intermediates and a preparation method and use thereof. Specifically provided are Lincomycin biosynthetic intermediates obtained from the genetic modification of a Lincomycin producing bacterium, and a method for the production thereof through fermentation and purification through separation.

Abstract: A compound having the following structure (I): or a pharmaceutically acceptable salt, prodrug, stereoisomer or tautomer thereof, is provided. Related compounds, methods for preparation of the same and uses of the compounds for treatment of various indications, including treatment of necrotic cell diseases and/or inflammation, are also provided.

Abstract: Disclosed are a retinoid compound, a preparation method therefor, intermediates thereof and an application thereof. The retinoid compound I of the present invention has a good tumor growth inhibition rate.