Abstract: The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

Abstract: The invention relates to a new process for preparing compounds of the formula (I) and pharmaceutically acceptable salts thereof, which act as ferroportin inhibitors being suitable for the use as medicaments in the prophylaxis and/or treatment of diseases caused by a lack of hepcidin or of iron metabolism disorders leading to increased iron levels or increased iron absorption, including iron overload, thalassemia, sickle cell disease and hemochromatosis.

Abstract: Provided is an antibacterial composition comprising at least one compound including a quaternary ammonium structure having an acrylate group or a methacrylate group, and having an antibacterial strength A of 90% or more against at least one strain selected from Gram-positive bacteria and Gram-negative bacteria, and an acute oral toxicity dose LD50 of 300 mg/Kg or more, where the antibacterial strength A equals (1?Asample/AReference)×100, where Asample equals an absorbance of an inoculated medium solution incubated with the antibacterial composition, and AReference equals an absorbance of an inoculated medium solution incubated without addition of the antibacterial composition.

Abstract: The present invention provides a new azabicyclo[3.1.0]hexane compound that is represented by the following formula: and that is for use in treating central nervous system (CNS) disorders. In the formula, X represents —C(?)—O— or the like, and R represents H, an optionally substituted C1-C18 alkyl, or the like.

Abstract: Riboflavin for use as a medicament in the treatment of a patient with a disease of a diarthrotic, amphiarthrotic or synarthrotic joint, preferably an intervertebral disc disease is provided. The treatment occurs in situ in the patient and includes local administering of riboflavin in a collagenous tissue of the joint and subsequent irradiation with electromagnetic radiation. A method and a kit are also provided for carrying out in-situ crosslinking of a collagenous tissue in the case of a disease of a diarthrotic, amphiarthrotic or synarthrotic joint, preferably an intervertebral disc.

Abstract: Gallium-salophen compounds, and methods of using the same for the treatment of disease are disclosed.

Abstract: The invention relates to ligands and complexes of metal ions with the ligands useful in various applications, including therapeutic and diagnostic applications.

Abstract: Provided are a crystal of a tricyclic compound as shown in formula (I) or a pharmaceutically acceptable salt thereof and a preparation method therefor, and the use thereof in preparing a drug for treating PDE3- and/or PDE4-related diseases.

Abstract: The present invention relates to a trolox-peptide conjugate which exhibits activity that relieves muscle contraction and increases the extracellular matrix, and which can be used as an active ingredient of a drug, a quasi-drug or a cosmetic product for muscle relaxation, neuromuscular disorder prevention or treatment, or the improvement of skin conditions including skin wrinkles.

Abstract: The present invention provides a compound of formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age-related macular degeneration, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

Abstract: The present invention relates to a novel morpholino oligonucleotide comprising at least one type of morpholino nucleotide monomer having pyrrolocytosine (pC) among unnatural cytosines, and relates to a morpholino oligonucleotide capable of more selectively binding to a target RNA and exhibiting excellent cell penetration compared to an MPO having a natural cytosine, and thus being capable of greatly contributing to the development of a therapeutic agent for incurable diseases in the area of morpholino oligonucleotides.

Abstract: Various salt forms of Compound I and Compound II represented by the following structural formulae, and their corresponding pharmaceutical compositions, are disclosed. (I), (II) Particular single crystalline forms of 1:1 Compound I tris salt, 1:1 Compound II tris salt, and 1:1 Compound II citrate salt are characterized by a variety of properties and physical measurements. Methods of preparing specific crystalline forms are also disclosed. The present disclosure also provides methods of treating type 2 diabetes mellitus, pre-diabetes, obesity, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and cardiovascular disease in a subject.

Abstract: The present application provides tricyclic urea compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.

Abstract: According to the present invention, a composition that induces the feeling of satiety or suppresses binge eating is provided. The present invention provides a GABA-containing composition for inducing transient satiety in a subject. The present invention also provides a GABA-containing composition for suppressing binge eating on a fasting condition in a subject.

Abstract: The invention relates to permethrin for use in the external treatment of Demodex spp. infestations, in particular in the eye area, in humans, the permethrin being used in an amount ranging from 5 mg/ml to 45 mg/ml, preferably in an amount of 7.5 mg/ml.

Abstract: High ATP production by the mitochondrial ATP-synthase is a new therapeutic target for anti-cancer therapy, especially for preventing tumor progression. A mitochondrial-related gene signature for metastasis is described, which features the gamma-subunit of the mitochondrial ATP-synthase (ATP5F1C). Knock-down of ATP5F1C expression significantly reduces ATP-production, 3D anchorage-independent growth and cell migration. Administration of the Bedaquiline, or a Bedaquiline derivative with a fatty acid moiety, down-regulates ATP5F1C expression in vitro and prevents spontaneous metastasis in vivo. Mitochondrial ATP5F1C is a promising new biomarker and molecular target for future drug development, for the prevention of metastatic disease progression.

Abstract: A metal-organic framework (MOF) MIL-125 and a preparation method and a use thereof are provided. The MOF MIL-125 is a round cake-like crystal and has an external specific surface area (SSA) of 160 m2/g to 220 m2/g. The MOF MIL-125 provided in the present application has a large number of microporous structures, a large external SSA, and a high catalytic activity in oxidation.

Abstract: The disclosure relates to rifamycin analog compounds, intermediates and precursors thereof, and pharmaceutical compositions capable of inhibiting bacterial growth (e.g., S. aureus growth) and treating bacterial infections (e.g., S. aureus infections). The disclosure further relates to antibody-drug conjugates of rifamycin analog compounds and antibodies, for example, antibodies specific for infectious disease-related targets such as membrane glycoprotein receptor (MSR1), wall teichoic acids (WTA) or Protein A, and methods of use thereof to inhibit bacterial growth and treat bacterial infections.

Abstract: A preparation method for semaglutide. The method comprises: producing a semaglutide resin by means of a solid-phase synthesis, producing crude semaglutide by cleavage and deprotection, producing refined semaglutide by purification and freeze-drying, comprising the solid-phase synthesis of a semaglutide 1-6 peptide fragment resin, which is cleaved and purified to serve as a first peptide fragment; and synthesizing a lysine having a sidechain group at locus 20 of semaglutide to serve as a second peptide fragment. In the method, prepared is a semaglutide loci 1-6 fully protected peptide fragment, which serves as a key starting material applied in the solid-phase synthesis of semaglutide, thus reducing the generation of D-His, D-Glu, D-Thr, D-Phe racemic impurities and +Gly impurities, reducing the difficulty of coarse product purification, increasing the purity and yield of semaglutide, reducing synthesis costs, and favoring industrialized large-scale production.

Abstract: Disclosed are a benzonitric heterocyclic compound, a preparation method therefor and the use thereof. Provided in the present invention is a benzonitric heterocyclic compound represented by formula I, or a pharmaceutically acceptable salt thereof, which can be used as a histone deacetylase inhibitor, has a selective inhibitory effect on HDAC6, and has characteristics such as a high efficiency, low toxicity and ideal pharmacokinetic properties.