Abstract: The present invention relates to an amide derivative and use thereof in medicine, and specifically to an amide derivative shown as general formula (I) or a stereoisomer, solvate, metabolite, deuteride, prodrug, pharmaceutically acceptable salt or cocrystal thereof, a pharmaceutical composition containing the same, and use of the compound or the composition disclosed herein in preparing an NLRP3 inhibitor.

Abstract: An intermediate compound is prepared and used for the synthesis of halichondrin B, eribulin or an analog thereof, particularly a structural fragment C27-C35 thereof. The starting materials of the synthetic route are readily available, and the optical purity of the starting materials can be ensured, so that the optical purity of the structural fragment C27-C35 in halichondrin B, eribulin or the analog thereof is ensured. Steps for constructing a chiral center of the structural fragment C27-C35 feature higher diastereoselectivity and yield, in particular preparation methods of compounds of formulae (X), (XI), (XVI) and (XV). By-products of partial reactions can be removed only by recrystallization, which results in easy purification and significant reduce in cost.

Abstract: Embodiments of the disclosure include methods and compositions for treatment of lung disease, including at least chronic obstructive pulmonary disease (COPD). In particular cases, fibroblasts (including activated fibroblasts) and/or exosomes thereof are provided to an individual for the treatment of COPD. In particular cases the fibroblasts are activated and/or express one or more particular markers.

Abstract: An 8-(3-chlorobenzylideneamino)naphthalene-1,3-disulfonic acid compound, its synthesis, and its use as an antioxidant agent.

Abstract: A 4-(1-(2-Hydroxypropyl)-4,5-diphenyl-1H-imidazol-2-yl)pyridin-3-ol compound, its synthesis, and its use as an antimicrobial agent.

Abstract: This invention provides for compounds of the formula: wherein the variables are defined herein, or salt thereof, compositions comprising these compounds, and method for the treatment, control or prevention of a parasitic infestation or infection in an animal in need thereof by administering an effective amount of these compounds to said animal.

Abstract: The invention provides methods of inhibiting the growth or metastasis of a cancer in a mammal by inhibiting a Ral GTPase in the mammal. The invention also provides small molecule inhibitors of Ral GTPases useful in the methods of the invention and pharmaceutical compositions containing the therapeutically effective compounds of the invention, and methods of using the same.

Abstract: The invention relates to a novel linker for use in bioconjugates such as antibody-drug-conjugates. The linker according to the invention is represented by formula: wherein: BM is a branching moiety; E is a capping group; SG is a sulfamide group; b, c, d, e, g, i, k, l are independently 0 or 1; f is an integer in the range of 1 to 10; Sp1, Sp2, Sp3, Sp4, Sp5 and Sp6 are a spacer moieties; Z1 and Z2 are connecting groups. The linker according to the invention is useful in the preparation of linker-conjugates and bioconjugates, and can be used for (a) improving conjugation efficiency in the preparation of the bioconjugate, (b) reducing aggregation during the preparation of the bioconjugate and/or of the bioconjugate, (c) increasing stability of the bioconjugate, and/or (d) increasing therapeutic index of the bioconjugate.

Abstract: The disclosure provides at compounds of Formula I, compositions comprising the same, and methods of using the same, including use in treating a disease and/or a symptom of a disease caused by a coronavirus.

Abstract: The present disclosure provides ammonium compounds, e.g., compounds according to Formula I as set forth herein, which are useful as antimicrobial agents. Methods for the treatment of bacterial infections and associated conditions, e.g., gastrointestinal conditions, are also described, as well as methods for altering the microbiome of subjects such as humans.

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: 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 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: FGFR3-related chondrodysplasias represent a group of rare diseases. Among them, achondroplasia, a nonlethal form of chondrodysplasia, is the most common type of dwarfism. The mutation, which produce an increase of FGFR3 function, affects many tissues, most strikingly the cartilaginous growth plate and bone in the growing skeleton, leading to a variety of manifestations and complications. In attempt to find a new therapeutic approach for FGFR3-related chondrodysplasia, the inventors purified (?)-epicatechin from T. cacao and showed that (?)-epicatechin treatment significantly increases the length of the Fgfr3Y367C/+ femurs comparing to Fgfr3+/+ femurs and improves the whole growth plate cartilage. The present invention thus relates to the use of (?)-epicatechin for the treatment of FGFR3-related chondrodysplasias.

Abstract: In immunoglobulin light chain amyloidosis (AL), the unique antibody light chain (LC) protein that is secreted by monoclonal plasma cells in each patient misfolds and/or aggregates, a process leading to organ degeneration. For treating AL patients, such as those with substantial cardiac involvement who have difficulty tolerating existing chemotherapy regimens, provided herein are small molecule compounds of Formula Ia, Formula Ib, and Formula II that are kinetic stabilizers of the native dimeric structure of full-length LCs, which compounds can slow or stop the amyloidogenicity cascade at its origin.

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: A process for the preparation of midostaurin with high purity, particularly a process for the preparation of midostaurin with a content of oxidation impurities lower than 0.1% comprising the treatment of crude midostaurin or staurosporine with strong organic or inorganic acids in a water-immiscible solvent and, optionally, also with reducing silanes is described.

Abstract: This application is directed to inhibitors of RAD51 represented by the following structural formula, and methods for their use, such as to treat cancer, autoimmune diseases, immune deficiencies, or neurodegenerative diseases.

Abstract: Provided is a pharmaceutical composition for preventing or treating osteoarthritis, the pharmaceutical composition including, as an active ingredient, obtusifolin, a derivative thereof, or a pharmaceutically acceptable salt thereof. The composition according to an aspect inhibits cartilage destruction-promoting factors and alleviates inflammatory responses, thereby exhibiting significantly excellent effects for preventing or treating osteoarthritis.

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