Abstract: The present invention relates to a novel phenoxyacetic acid derivative represented by the general formula (I), preparation method thereof and use of a pharmaceutical composition containing the derivative in preparing a medicament for treating diabetes and metabolic syndrome. The phenoxyacetic acid derivatives have excellent in vivo hypoglycemic activity, which can be used for preventing or treating diabetes.

Abstract: A benzo[b]selenophene STING regulator, a preparation method therefore and use thereof are disclosed. The structure of the compound is shown in Formula I. A derivative, salt, stereoisomer, prodrug molecule and pharmaceutical composition of the present invention can serve as an immune regulator to effectively activate an innate immune regulation passageway to kill tumor cells.

Abstract: Disclosed in the present invention are a naphthalenesulfonamide compound, a preparation method, and an application. The naphthalenesulfonamide compound provided by the present invention can interfere with Keap1-Nrf2 binding and activate Nrf2 to relieve inflammatory damage and improve an inflammatory microenvironment, has a potential anti-inflammatory activity, and can be used for preparing an anti-inflammatory drug for inflammatory damage of various inflammation-related diseases, including chronic obstructive pulmonary disease (COPD), Alzheimer's disease, Parkinson's disease, atherosclerosis, chronic kidney disease (CKD), diabetes, intestinal Inflammations, rheumatoid arthritis, etc.

Abstract: A hydroxamic acid-containing compound represented by formula I, and a preparation method, and a use thereof are provided. An inhibitory activity of the hydroxamic acid-containing compound on acid sphingomyelinase (ASM) is evaluated by a biological experiment. The compound is further subjected to in vivo pharmacodynamic investigation, and the results show that the compound exhibits significant anti-depression and anti-atherosclerosis (AS) activities, which provides feasibility for the further development of an ASM inhibitor.

Abstract: The present disclosure relates to the field of pharmaceutical chemistry, in particular to a class of PARP/PI3K double-target inhibitors (I) containing structures of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine and phthalazin-1(2H)-one and a preparation method thereof. As proved by pharmacodynamic tests, the compounds of the present disclosure have PARP/PI3K double-target inhibitory activity and can be used for anti-tumor.

Abstract: A composition containing SUMO inhibitor, and belongs to the technical field of medicine includes FXR agonist and SUMO inhibitor. In activated hepatic stellate cells, the FXR agonist does not have an effect in inhibiting the activation of hepatic stellate cells. After the FXR agonist and the SUMO inhibitor are compounded according to the present invention, the activation of hepatic stellate cells can also be inhibited for those cells under activated state. Of note, the hepatic stellate cells of an individual with hepatic fibrosis symptoms have been in an activated state, therefore a good anti-fibrotic effect cannot be achieved by using the FXR agonist alone.

Abstract: The present application relates to a hydrogen peroxide-responsive Keap1-Nrf2 PPI inhibitor prodrug, and a preparation method therefor. The hydrogen peroxide-responsive Keap1-Nrf2 PPI inhibitor prodrug pro2 has a chemical structure as shown below. By modifying a key carboxyl pharmacophore in a Keap1-Nrf2 inhibitor with a H2O2-responsive thiazolidinone moiety, a novel ROS-responsive antioxidant prodrug pro2 is synthesized. The H2O2 activated prodrug pro2 can simultaneously achieve targeted activation of Nrf2 and enhancement of therapeutic efficacy in the body. The prodrug is based on the concept of ROS activation-ROS clearance therapy, is the first example of a H2O2-responsive prodrug suitable for oral administration, and is expected to be used clinically by virtue of the characteristics of druggability and high targeting ability.

Abstract: It discloses a proteolysis targeting chimeric molecule, a preparation method and an application thereof. The proteolysis targeting chimeric molecule provided by the disclosure can inhibit the expression of BCR-ABL and/or CRBN protein in BCR-ABL and/or CRBN positive leukemia K562 cells to varying degrees, and thus can be used to prepare drugs for treating BCR-ABL and/or CRBN positive leukemia, wherein the proteolysis targeting chimeric molecule with n=3 has excellent photo-isomerization activity, and can be used in preparation of the reagents or drugs for light-regulated degradation of BCR-ABL and/or CRBN protein. The disclosure also provides a method for synthesizing the series of proteolysis targeting chimeric molecules.

Abstract: The present disclosure relates to the field of medicinal chemistry, in particular to a phenyl triazole MLL1-WDR5 protein-protein interaction inhibitor (I) and a preparation method thereof, and pharmacodynamics experiments prove that the compound of the present disclosure has relatively strong MLL1-WDR5 protein-protein interaction inhibition activity.

Abstract: Disclosed are the preparing method of a pentacyclic triterpenoid saponin compound and a drug composition, and in particular the method of the pentacyclic triterpenoid saponin compounds as shown in formulae (I) to (XVI) in the preparation of a drug for preventing or treating a disease mediated by AMPK and/or ERR?, comprising the preparation of a drug for preventing or treating diseases such as a liver disease, respiratory system disease, metabolic disease, autoimmune disease, cardiovascular and cerebrovascular disease, kidney disease, central nervous system disease or muscular dystrophy. The definition of formulae (I) to (XVI) is the same as the definition in the specification.

Abstract: Disclosed in the present invention are a naphthalenesulfonamide compound, a preparation method, and an application. The naphthalenesulfonamide compound provided by the present invention can interfere with Keap1-Nrf2 binding and activate Nrf2 to relieve inflammatory damage and improve an inflammatory microenvironment, has a potential anti-inflammatory activity, and can be used for preparing an anti-inflammatory drug for inflammatory damage of various inflammation-related diseases, including chronic obstructive pulmonary disease (COPD), Alzheimer's disease, Parkinson's disease, atherosclerosis, chronic kidney disease (CKD), diabetes, intestinal Inflammations, rheumatoid arthritis, etc.

Abstract: A pathophysiological effect of a transient receptor potential cation channel, subfamily V, member 3 (TRPV3) on psoriasis, which can be used to develop a drug for preventing or treating psoriasis. The invention further discloses an application of Scutellarein as a TRPV3 inhibitor in preparing a drug for preventing or treating psoriasis. When a drug containing the TRPV3 inhibitor discovered according to the invention or provided by the invention is used for preventing or treating psoriasis, good prevention or treatment effects can be achieved.

Abstract: Provided are four crystal forms, A, B, C and D, of demethyleneberberine hydrochloride, and a preparation method therefor, and further provided are X-ray powder diffraction characteristic absorption peaks, infrared absorption peaks and DSC spectra of the four crystal forms. The X-ray powder diffraction characteristic diffraction peaks of the crystal forms are at about 8.205°, 8.805°, 10.817°, 14.835°, 15.479°, 16.668°, 17.492°, 18.529°, 20.656°, 21.536°, 23.538°, 25.657°, 26.192°, and 28.808°. A preparation method for the four crystal forms of the demethyleneberberine hydrochloride is also involved. The preparation method has a simple process, a high yield and a low cost; and has a high product purity and a stable quality.

Abstract: The disclosure discloses a use of cyclic adenosine monophosphate (cAMP), derivative or prodrug thereof in preparation of drug for preventing and/or treating depression. Using the established model of depressed mice caused by social defeat stress, cAMP is intraperitoneally injected upon constructing the model or directly injected into the nucleus accumbens brain region of depressed mice after modeling, which can significantly improve the depression-like behavior of mice. The disclosure discloses the prevention and treatment effect of cAMP on depression, and provides a candidate drug with new mechanism for clinical prevention and treatment of depression.

Abstract: A cosmetic composition containing ?-mangostin, and use thereof are disclosed. The cosmetic composition includes ?-mangostin and a sunscreen agent. The ?-mangostin is a pure ?-mangostin or an ?-mangostin-containing extract. The sunscreen agent is an inorganic sunscreen agent or an organic sunscreen agent. Herein, the inorganic sunscreen agent is one or more selected from a group of zinc oxide and titanium dioxide. The organic sunscreen agent is a sunscreen agent having a sun protection wavelength range that can be complementary to that of the ?-mangostin or a sunscreen agent that is easily decomposed or easily oxidized under UV exposure. The organic sunscreen agent is one or more selected from a group of butyl methoxydibenzoylmethane, octocrilene, ethylhexyl salicylate, octyl salicylate, homosalate, ethylhexyl methoxycinnamate and terephthalylidene dicamphor sulfonic acid.

Abstract: Disclosed are an inflammation-targeted neutrophil granulocyte drug delivery system and use thereof, wherein the drug delivery system includes neutrophil granulocytes and a therapeutic substance or a detectable substance loaded into the neutrophil granulocytes or onto the surface of the neutrophil granulocytes in a direct or indirect way. By using the neutrophil granulocytes as a carrier of a drug, the drug is actively targeted to an inflammatory site, thereby increasing the drug concentration at the inflammatory site. Under the stimulation of cytokines, the neutrophil granulocytes arriving at the inflammatory site are abnormally activated, disintegrate rapidly, and die in the way of “Neutrophil extracellular traps (NETs)”. This helps to rapidly release the loaded drug to the targeted site, so as to improve the therapeutic effect and reduce the toxic and side effects.

Abstract: The disclosure provides a high-activity long-acting hypoglycemic fusion protein, which is formed by connecting, via a linker peptide or directly, a high-activity Exendin-4 mutant with an optimally mutated Fc fragment of a human immunoglobulin IgG1. The optimally mutated Fc fragment of the human immunoglobulin IgG1 comprises an optimally mutated human IgG1 hinge region and human IgG1 constant regions CH2 and CH3.

Abstract: The present invention relates to a type of aryl benzofuran amidated derivatives, the medical use thereof, and the preparation method; said derivatives have antioxidation activity, and xanthine oxidase inhibitory activity, and can be used for antioxidation and for preparing compositions, drugs and health products and treating gout and hyperuricemia.

Abstract: A heterocyclic urea compound, and specifically discloses an indoleamine-2,3-dioxygenase inhibitor of a heterocyclic urea compound, which solves the problems of weak curative effect and larger toxic and side effects of existing immunological therapy drugs. The invention further provides a preparation method for an indoleamine-2,3-dioxygenase inhibitor of a heterocyclic urea compound, and an application of the indoleamine-2,3-dioxygenase inhibitor of a heterocyclic urea compound or a pharmaceutically acceptable salt thereof in preparing drugs for treating or preventing tumors.

Abstract: Bifunctional fusion proteins having Tumstatin active fragments and CD137L extracellular regions are provided. The proteins exhibit activities to inhibit the proliferation of human umbilical vein endothelial cells and to costimulate the proliferation of T cells. They can be used for the treatment of various tumor-related diseases and the regulation of angiogenesis and immunological effects in humans.