Abstract: The present invention relates to compounds of formula (I) and their use for treating or preventing a bacterial infection or as an antibacterial agent and/or as a ?-lactamase inhibitor.

Abstract: The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto.

Abstract: Novel dual 5-LO inhibitors of well validated electrophilic Michael acceptors and nitrogen-heterocycles are presented and designed to maintain specific structural features of currently known dual 5-LO inhibitors and to overcome their drawbacks. The Michael acceptor scaffold will act as a carrier and will provide a stable anchorage via covalent binding to cysteine/histidine residues within the catalytic cleft and/or the surface interface of the 5-LO; whereas, the nitrogen-heterocycles will ensure the access to the Fe(II) catalytic center. These combinations offer potential for more than one mode of iron chelation and 5-LO inhibition.

Abstract: Problem to be solved: An object of the present invention is to provide a novel fat absorption inhibiting agent. Solution to the problem: The present invention provides a fat absorption inhibiting agent comprising pulverized defatted sesame seeds or a processed product thereof. The present invention also provides a fat absorption inhibiting agent comprising defatted sesame seeds having a 50th percentile particle size of 1 to 200 ?m as determined by laser diffraction/scattering and a compressibility index of 30 to 80%. The fat absorption inhibiting agent of the present invention preferably has lipase inhibitory activity. The present invention also provides a food comprising the agent. The present invention also provides defatted sesame seeds having a 50th percentile particle size of 1 to 200 ?m as determined by laser diffraction/scattering and a compressibility index of 30 to 80%.

Abstract: This application relates to the treatment of lysosomal storage disorders resulting from a deficiency of acid maltase and/or acid ?-glucosidase by administering active barley in comminuted form. Also disclosed are methods of replacing acid maltase and/or acid ?-glucosidase by administering active barley in comminuted form. Further disclosed are compositions for carrying out these methods.

Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain substituted 1-methyl-4-[(4-phenylphenyl)sulfonylmethyl]cyclohexanol and 1-methyl-4-[[4-(2-pyridyl)phenyl]sulfonylmethyl]cyclohexanol compounds (collectively referred to herein as CHMSA compounds) that are useful, for example, in the treatment of disorders (e.g., diseases) including, e.g., multiple myeloma, diffuse large B-cell lymphoma, acute myeloid leukemia, eosinophilic leukemia, glioblastoma, melanoma, ovarian cancer, chemotherapy resistant cancer, radiation resistant cancer, inflammatory arthritis, rheumatoid arthritis, psoriatic arthritis, psoriasis, ulcerative colitis, Crohn's disease, systemic lupus erythematosus (SLE), lupus nephritis, asthma, chronic obstructive pulmonary disease (COPD), non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), autoimmune hepatitis, hidradenitis suppurativa, etc.

Abstract: Compounds as STAT3 inhibitors are described. A pharmaceutical composition comprising the same, methods of making the same, and a method for treating or preventing conditions such as cancer, chronic inflammation, and fibrosis using the same, are described.

Abstract: Embodiments relate to a method for treatment of blepharitis in a patient in need thereof comprising administering to a subject in need thereof a pharmaceutical composition comprising a pharmaceutically effective amount of at least one cannabinoid, via the topical route. Optionally, the pharmaceutical composition is administered in combination with an additional agent selected from the group consisting of: an essential oil, a steroid, an antibiotic, an anti-parasitic, a disinfectant, an anesthetic, a terpene, a moisturizer and a vitamin.

Abstract: A method of attenuating, treating or preventing cognitive aging in an individual who does not have dementia includes administering to the individual a therapeutically effective amount of a composition containing an omega-3 fatty acid and choline. The method can achieve a benefit that is one or more of decreasing brain atrophy, increasing or maintaining number of synapses, increasing amyloid-? phagocytosis, or decreasing or maintaining neuroinflammation in the non-demented individual. The method can prevent dementia in an individual at risk thereof, for example an elderly human. The composition can be administered to the individual in a daily dose that provides 5.5 mg/day to 5,500 mg/day of the choline, for example 85 mg/day to 3,500 mg/day of the choline.

Abstract: The present disclosure provides methods of treating COVID-19 by administering a pharmaceutical composition providing inhibition of severe acute respiratory syndrome-coronavirus 2 (SARS-CoV-2) main protease (MPro) in a patient. The disclosure also provides other methods as well as pharmaceutical formulations for use in treating COVID-19 patients.

Abstract: Described herein is the use of a LOXL2 inhibitor in the treatment or prevention of conditions, diseases, or disorders associated with LOXL2 activity.

Abstract: Compounds that are inhibitors of retinoic acid inducible P450 (CYP26) enzymes. The compounds have retinoid activity, are resistant to CYP26-mediated catabolism, act as inhibitors of CYP26B1, and are used for treating diseases that are responsive to retinoids.

Abstract: Disclosed herein are methods for increasing circulating mesenchymal stem cells by administering a compound having the general formula 1 as defined herein, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to three-dimensional self-assembled nucleic acid nanoparticles, a drug delivery system comprising the same, and a pharmaceutical composition for the prevention or treatment of acute kidney injury, which comprises the same. The three-dimensional self-assembled nucleic acid nanoparticles of the present invention, which have a tetrahedral structure, exhibit an excellent renal-targeting ability, and thus the nanoparticles conjugated with the pharmaceutically active ingredient for p53 exhibit excellent p53 and caspase 3 expression reductions in vitro and in vivo, and can thereby be applied to the prevention or treatment of acute kidney injury.

Abstract: The present invention relates to the field of prostate cancer treatment, and in particular the field of prostate cancer treatment by Androgen Deprivation Therapy (ADT). The present treatment involves oral administration of an estetrol component in conjunction with ADT.

Abstract: The present invention relates to a new class of non-fused thiophene derivatives and their uses for treating diseases such as infection, cancer, metabolic diseases, cardiovascular diseases, iron storage disorders and inflammatory disorders.

Abstract: The invention provides compositions and methods for reducing the volume of menstrual blood loss in a patient, such as a human patient, for instance, that has uterine fibroids, by administration of a gonadotropin-releasing hormone (GnRH) antagonist. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxypheny I]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof.

Abstract: Described herein are protein steroid conjugates that are useful, for example, for the target-specific delivery of glucocorticoids (GCs) to cells.

Abstract: The present invention belongs to the technical field of medicine, and specifically relates to use of succinic acid in increasing sensitivity of bacteria to antibiotics. The present invention found that the succinic acid can increase proton motive force of bacteria, thereby increasing the number of antibiotics entering the bacteria, and eventually killing the bacteria. Therefore, the succinic acid can increase the sensitivity of bacteria to antibiotics, thereby overcoming the problem of bacterial drug resistance. Combining succinic acid with antibiotics can significantly improve the bactericidal effect of the antibiotics, which has better effects and higher safety and operability compared with only using antibiotics as antibacterial drugs at present.

Abstract: The present disclosure is directed in part to methods of treating fibrosis, e.g., hepatic fibrosis and/or intestinal fibrosis, comprising administering to a patient in need thereof an effective amount of a disclosed compound.