Abstract: The benzofuro[3,2-c]-chromen-6-one compounds are antibacterial agents. The emergence of drug-resistant bacteria calls for constant development of new antibacterial agents with the aim of generating medicaments that are potent against drug sensitive and resistant bacteria and are well tolerated. The present compounds are not only new, but have very valuable antimicrobial properties. These compounds showed a broad spectrum of activity against gram-positive and gram-negative bacteria, as well tuberculosis mycobacteria. They also showed potent activity against drug-resistant bacteria, such as MRSA and VRSA. The molecular target of these compounds was identified as DNA Gyrase B. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.

Abstract: Provided herein are solution formulations of CX-011 and related methods for making solution formulations of CX-011. Also provided are methods of treating an inflammatory disorder, such as osteoarthritis, or cancer in a subject in need thereof by administering an effective amount of the solution formulations of CX-011.

Abstract: The present invention aims to provide a compound that may be useful for the prophylaxis or treatment of constipation and the like. The present invention provides a compound represented by the formula (I): wherein R1 is a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, or an optionally substituted C1-6 alkoxy group; and ring A is an optionally further substituted ring, or a salt thereof.

Abstract: The present invention is directed to cinnolinyl and quinolinyl pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

Abstract: Disclosed are compounds and compositions that modulate cannabinoid receptors, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors. This disclosure is directed to methods of treating cannabinoid dependence, neuropathy, inflammation, glaucoma, a neurodegenerative disorder, a motor function disorder, a gastrointestinal disorder, hypothermia, emesis, loss of appetite, or anorexia associated with AIDS.

Abstract: Methods are provided herein for selectively killing senescent cells and for treating senescence-associated diseases and disorders by administering a senolytic agent. Senescence-associated diseases and disorders treatable by the methods using the senolytic agents described herein include cardiovascular diseases and disorders associated with or caused by arteriosclerosis, such as atherosclerosis; idiopathic pulmonary fibrosis; chronic obstructive pulmonary disease; osteoarthritis; senescence-associated ophthalmic diseases and disorders; and senescence-associated dermatological diseases and disorders.

Abstract: The present invention provides a method for safe and efficacious administration of esketamine.

Abstract: The invention relates generally to the field of medical treatment. More particularly, the invention relates to treating a patient in order to increase the amount of ketones metabolized by mitochondria. Exemplary patients include those with Alzheimer's disease and insulin resistance.

Abstract: The present application relates to an anti-tumor compound and a preparation method and use thereof, and in particular to a compound or a tautomer, a mesomer, a racemate, an enantiomer or a diastereoisomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, and a preparation method and use thereof.

Abstract: A seed germination activator for control of broomrape includes butylisobutylphthalate (hereinafter “BIP”). A biocontrol composition includes BIP and at least two nonionic surfactants for administration in irrigation water. Methods of controlling broomrape may include administering the biocontrol composition comprising BIP in the irrigation water prior to planting crops.

Abstract: The present invention relates to methods, compositions and kits for treatment of ribosomal disorders and ribosomopathies, e.g. Diamond Blackfan anemia (DBA). In some embodiments, the invention relates to the use of novel classes of compounds, i.e. inhibitors of RSK (p90S6K); inhibitors of p70S6K; and inhibitors of rps6, to treat ribosomal disorders and ribosomopathies. In some embodiments, the invention relates to the use of specific Chk2 inhibitors and to the use of specific phenothiazine derivatives to treat ribosomal disorders and ribosomopathies, e.g. DBA.

Abstract: Provided are methods of sensitizing LKB1/STK11 deficient cancers to immune therapy. A method for treatment for LKB1/STK11 deficient cancers is provided comprising administration of inhibitor or inhibitors of one or more of NAMPT, CD38, SHP2, CXCR1/2, HDAC4 and PARP in combination with immunotherapy.

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

Abstract: Beta-hydroxybutyrate compositions include a mixture of optically pure S-beta-hydroxybutyrate salts and acid(s) or non-racemic mixture of beta-hydroxybutyrate salts and acid(s) enriched with the S-enantiomer. The S-beta-hydroxybutyrate enantiomer modulates the effect of ketone bodies in the subject and controls the rate at which ketosis is achieved. Beta-hydroxybutyric acid is more rapidly absorbed and utilized by the body than salts or esters, enhances taste, and reduces the need to include citric acid or other edible acids. Beta-hydroxybutyrate salts are more slowly absorbed and utilized by the body and can provide one or more electrolytes.

Abstract: Many drugs useful in treating cancer are metabolized by CYP2C8 enzymes, by CYP3A4 enzymes, or both. The effects of concomitant administration of relacorilant and paclitaxel, a drug used to treat cancer that is a substrate for both CYP2C8 and CYP3A4, are disclosed herein. Relacorilant potently inhibited CYP2C8 and CYP3A4 in in vitro tests, indicating that co-administration of relacorilant and paclitaxel would increase paclitaxel plasma exposure more than 5-fold in vivo, requiring significant reductions in paclitaxel doses when co-administering paclitaxel with relacorilant. Surprisingly, paclitaxel plasma exposure increased only by about 80% instead of the expected more than 5-fold increase expected with concomitant relacorilant and paclitaxel administration. Applicant discloses safe methods of co-administering relacorilant and paclitaxel by reducing the dose of paclitaxel to about half the paclitaxel dose used when paclitaxel is administered alone.

Abstract: The present invention relates to fluorinated and alkylated bile acids.

Abstract: The present disclosure relates to a benzoselenophene-based compound, a method of preparing the benzoselenophene-based compound, and a pharmaceutical composition and antibody-drug conjugate including the benzoselenophene-based compound.

Abstract: The technology described herein relates to methods and compositions to prevent or treat vascular disease by targeting the epigenetic regulation of gene expression of vascular smooth muscle cell cytoskeletal proteins.

Abstract: A seed germination activator for control of broomrape includes butylisobutylphthalate (hereinafter “BIP”). A biocontrol composition includes BIP and at least two nonionic surfactants for administration in irrigation water. Methods of controlling broomrape may include administering the biocontrol composition comprising BIP in the irrigation water prior to planting crops.

Abstract: Described is a method for the preparation of an oral levothyroxine composition, comprising the steps of combining levothyroxine or a salt thereof, a water-miscible organic solvent or a sugar alcohol and water, adjusting the pH to at least 8 providing a basic aqueous medium, dissolving the levothyroxine in the basic aqueous medium to yield a levothyroxine solution, and lowering the pH of the levothyroxine solution to between 3.5-4.9. also described is an oral levothyroxine composition obtainable by the said method and its use as a medicament.